54 Tables of Anti Infecti 2015 Mandell Douglas and Bennett S Principles

631
Tables of Anti-infective Agent

54 Pharmacology
Manjunath P. Pai and Joseph S. Bertino, Jr.
This chapter serves as a centralized source of pharmacologic informa- are summarized for the user. However, these forms of renal replace-
tion on anti-infective agents. The first table provides an index of all the ment therapies now encompass multiple potential modalities, such as
tables that are included in this chapter (Table 54-1). Tables detailing (1) hi-flux hemodialysis; (2) nocturnal hemodialysis; (3) slow-low effi-
generic and trade name for anti-infective agents are provided in an ciency hemodialysis; and (4) continuous veno-venous hemodiafiltra-
alphabetized sequence (Tables 54-2 and 54-3). Tables describing exist- tion. Specific dosing guidance may not be present for these various
ing dosage formulations are also categorized by chemical or pharma- dialysis modalities and so will require an educated decision based on
cologic class (Tables 54-4 through 54-16). Available information the pharmacology of the anti-infective. An alternative to the elongation
regarding the usual doses in adults and children, pharmacokinetic of the interval between doses is a reduction of the daily dose given at
information, and dose adjustment in renal impairment is provided by the usual dosing interval. Anti-infective serum concentrations should
chemical or pharmacologic class (Tables 54-17 through 54-30). Several be determined and patient-specific dosage adjustments made on the
anti-infective agents are substrates, inducers, and inhibitors of drug basis of these determinations, when appropriate. In the absence of
metabolism enzymes and transporters. Tables categorizing these therapeutic drug monitoring, a surrogate biomarker of this impaired
potential mechanisms for drug-drug interactions as either the victim drug clearance mechanism is used. Serum creatinine is the most com-
or perpetrator drug are included (Tables 54-31 through 54-35). monly used clinical biomarker for estimation of renal function and
drug dosage adjustment in patients with chronic kidney disease. The
DOSING GUIDELINES production of creatinine is regulated by numerous factors such as diet
The selection of an appropriate dose of an anti-infective agent is based composition and amount, patient muscle mass, liver function, age, and
on the site of infection, identity and known or presumed antibiotic sex, which can bias the value of this biomarker. The elimination of
susceptibility of the infecting organism, dose-related drug toxicity, and creatinine is regulated by renal function that includes both glomerular
patient’s ability to eliminate the drug (see Chapter 19). Generally, filtration and tubular secretion. Creatinine clearance (CrCl) equates to
dosage selections from the higher end of the dosage range are recom- an estimate of both elimination processes when using serum creati-
mended for severe, life-threatening infections (e.g., sepsis, meningitis). nine. The Cockcroft-Gault equation is the most common equation that
Known organisms with intermediate susceptibility (i.e., high minimal has been used to define creatinine clearance and to inform the dose
inhibitory concentration [MIC]) should also prompt the use of higher adjustments in the drug labels approved by regulatory bodies. Newer
dosages. More recent data with various types of anti-infectives suggest equations to estimate the glomerular filtration rate (GFR) have been
that higher doses or use of extended infusions of certain agents may developed to estimate kidney function in patients with chronic kidney
increase the probability of response against some resistant organisms. disease (<60 mL/min/1.73 m2). Specific estimates of GFR may be auto-
This may be true with agents that concentrate at the infection site and matically reported with the measurement of serum creatinine in the
that concentrate in the phagocytes that clear the organisms, such as clinical setting using the Modification of Diet in Renal Disease
quinolones and macrolides or azalides. (MDRD) equation.
The lowest dosages are typically used for urinary tract infections or The estimated CrCl and GFR calculations derived from these equa-
when the isolated pathogen is extremely susceptible to the anti- tions may yield comparable results, but it is important to remember
infective. A sizable range in dosing intervals exists for some anti- that these values may not be interchangeable. As such, this is a source
infective agents, with longer durations between doses appropriate for of major controversy when applied to drug dosing. A fundamental
less severe infections in which a critical threshold level in serum or point of consideration is that patients with serious infections are likely
other site of infection (e.g., central nervous system) is not mandatory, to be in a dynamic physiologic state that can influence the production
or the drug concentrates significantly at the site of infection (e.g., urine, and elimination of serum creatinine. Calculation of GFR and CrCl
bile). Lower dosages are also appropriate when the patient has impair- using these equations serves only as a point estimate for a patient under
ment in the function of excreting organs. conditions of physiologic stability. These equations are not reliable in
Knowledge regarding the optimal dosing of an anti-infective agent patients with changing renal function (increase or decrease), malnutri-
is limited at the time that a drug is approved by regulatory bodies. This tion (overestimation), elderly patients (overestimation), low serum
limited optimal dosing information is especially true in “special popu- creatinine (overestimation), and moderate to severe liver disease (over-
lations,” including pediatric, geriatric, or pregnant patients; those with estimation). Improvement in the estimation of kidney function is more
liver and kidney disease; and those who are obese. Patients treated with likely to occur with the use of exogenously administered substrates
anti-infectives may also concurrently be receiving other medications, (e.g., inulin, iohexol) or endogenous substrates such as cystatin C that
minerals, herbal supplements, and foods that may be associated with are less confounded by clinical variables. However, use of these novel
drug-drug or drug-food interactions. These interactions and resultant biomarkers to guide drug dosing will be difficult to validate in the
untoward effects may not be apparent during drug development. near term.
Hence, dosing recommendations for all agents will change as research
into them evolves. To prevent dosing errors, the recommendations DOSAGE ADJUSTMENT FOR
discussed in this chapter should be compared with the most recent HEPATIC IMPAIRMENT
scientific literature, package labeling, and other current reference In theory, although hepatic impairment can impair drug clearance,
sources. accurate biomarkers of hepatic function and correlation with dosage
adjustment are generally not available. Several drug labels include dose
DOSAGE ADJUSTMENT FOR adjustment recommendations that are based on pharmacokinetic
RENAL IMPAIRMENT studies performed in patients with cirrhosis that are classified using
Drug half-lives in adults with impaired renal function and changes the three category Child-Pugh score (A, B, or C). This scoring system
related to dialysis procedures (e.g., hemodialysis, peritoneal dialysis) Text continued on p. 653
631
631.e1
KEYWORDS
antibacterials; antifungals; antimycobacterials; antiparasitic;
antiretrovirals; antivirals; dosage form; drug-drug interactions;
Chapter 54 Tables of Anti-infective Agent Pharmacology

pharmacology; trade name
632
TABLE 54-1 Index of Tables Included in This Chapter

TABLE NUMBER TABLE TITLE
Part I Basic Principles in the Diagnosis and Management of Infectious Diseases
Anti-infective Names (organized alphabetically)

54-2 Generic and Trade Names
54-3 Trade and Generic Names
Anti-infective Dosage Forms
54-4 Penicillin Dosage Forms
54-5 Cephalosporin Dosage Forms
54-6 Aminoglycoside Dosage Forms
54-7 Tetracycline and Related Products Dosage Forms
54-8 Macrolide, Azalide, Ketolide, Lincosamide, Chloramphenicol, and Metronidazole Dosage Forms
54-9 Miscellaneous Agent Dosage Forms
54-10 Folate Antagonist Dosage Forms
54-11 Quinolone and Urinary Anti-infective Dosage Forms
54-12 Antimycobacterial Dosage Forms
54-13 Antifungal Dosage Forms
54-14 Antiparasitic Dosage Forms
54-15 Antiviral Dosage Forms
54-16 Antiretroviral Dosage Forms
Clinical Pharmacology
54-17 Anti-infective Agent Pharmacology: Penicillins
54-18 Anti-infective Agent Pharmacology: Cephalosporins
54-19 Anti-infective Agent Pharmacology: Miscellaneous β-Lactams
54-20 Anti-infective Agent Pharmacology: Aminoglycosides
54-21 Anti-infective Agent Pharmacology: Tetracyclines and Glycyclines
54-22 Anti-infective Agent Pharmacology: Azalides, Macrolides, Ketolides, Lincosamides, Chloramphenicol, and Metronidazole
54-23 Anti-infective Agent Pharmacology: Miscellaneous Gram-Positive Agents and Polymyxins, Fusidic Acid
54-24 Anti-infective Agent Pharmacology: Sulfonamides and Trimethoprim
54-25 Anti-infective Agent Pharmacology: Quinolones and Urinary Anti-infectives
54-26 Anti-infective Agent Pharmacology: Antimycobacterials
54-27 Anti-infective Agent Pharmacology: Antifungal Agents
54-28 Anti-infective Agent Pharmacology: Antiparasitic Agents
54-29 Anti-infective Agent Pharmacology: Antiviral Agents
54-30 Anti-infective Agent Pharmacology: Antiretroviral Agents
Drug-Drug Interactions
54-31 Key Drug Substrates by Cytochrome P-450 (CYP) Drug Metabolizing Isozymes
54-32 Drug Inhibitors by Cytochrome P-450 (CYP) Drug Metabolizing Isozymes
54-33 Drug and Chemical Inducers by Cytochrome P-450 (CYP) Drug Metabolizing Isozymes
54-34 Select Drug Transporter Localization with Representative Substrates, Inducers, and Inhibitors
54-35 Adverse Drug Interactions Involving Anti-infective Agents
TABLE 54-2 Generic and Trade Names

GENERIC NAME TRADE NAME CLASS
Abacavir Epzicom,* Kivexa,* Trizivir,* Ziagen, Ziagenavir Antiretroviral
Acyclovir Lipsovir,* Zovirax Antiviral
Adefovir dipivoxil Hepsera Antiviral
Albendazole Albenza, Eskazole, Zentel Antiparasitic
Amantadine hydrochloride Symadine, Symmetrel Antiviral
Amdinocillin Coactin Penicillin
Amikacin sulfate Biclin, Biklin, Likacin Aminoglycoside
Aminosalicylic acid Paser Antimycobacterial
Amoxicillin Amoxil, Clamoxyl, Doxamil, Hiconcil, Polymox, Prevpac,* Trimox Penicillin
Amoxicillin/clavulanate potassium Amoxiclav,* Augmentin,* Augmentin XR,* Calvepen* Penicillin/β-lactamase inhibitor
Amphotericin B Amphocin, Fungilin, Fungizone Antifungal
Amphotericin B cholesteryl sulfate complex Amphotec Antifungal
Amphotericin B lipid complex Abelcet Antifungal
Amphotericin B liposomal AmBisome Antifungal
Ampicillin — Penicillin
Ampicillin sodium Polycillin-N, Totacillin-N Penicillin
Ampicillin trihydrate Polycillin, Totacillin Penicillin
Ampicillin/probenecid Probampacin* Penicillin/tubular secretion inhibitor
Ampicillin/sulbactam Bacimex,* Combactam,* Unasyn* Penicillin/β-lactamase inhibitor
633
TABLE 54-2 Generic and Trade Names—cont’d


Anidulafungin Eraxis Antifungal
Artemether Coartem,* Paluther, Riamet* Antimalarial
Artesunate Plasmotrim (CDC†) Antimalarial
Atazanavir Reyataz Protease inhibitor
Atovaquone Mepron, Wellvone Antiparasitic
Atovaquone/proguanil Malarone* Antimalarial
Azithromycin Azitromax, Sumamed, Zithromax, Zithromax Tri-Pak, Zitromax, Zmax, Z-Pak Azalide
Azlocillin Securopen Penicillin
Aztreonam Azactam, Monobac, Primbactam, Urobactam Monobactam
Bacampicillin Ambaxin, Bacampicin, Penglobe, Spectrobid Penicillin
Bacitracin Baci-IM Polypeptide
Balofloxacin Baloxin Fluoroquinolone
Bithionol Bitin, Lorothidol (CDC†) Antiparasitic
Boceprevir Victrelis Antiviral (hepatitis C)
Butoconazole nitrate Femstat 3, Gynazole-1, Gynomyk, Mycelex-3 Antifungal
Capreomycin sulfate Capastat Sulfate Antimycobacterial
Carbenicillin indanyl sodium — Penicillin
Carbol-fuchsin Fungol Antifungal
Caspofungin Cancidas Antifungal
Cefaclor Distaclor, Keftid, Vercef Cephalosporin
Cefadroxil Baxam, Cefamox, Duracef, Duricef, Ultracef Cephalosporin
Cefamandole nafate Mandokef, Mandol Cephalosporin
Cefazolin sodium Ancef, Cefacidal, Cefamezin, Zolicef Cephalosporin
Cefdinir Cefzon, Omnicef Cephalosporin
Cefditoren pivoxil Spectracef Cephalosporin
Cefepime Maxcef, Maxipime Cephalosporin
Cefixime Cefspan, Denvar, Suprax Cephalosporin
Cefonicid sodium Monocid Cephalosporin
Cefoperazone sodium Cefobid, Cefodie, Cefoperazin* Cephalosporin
Cefoperazone/sulbactam Sulperazon,* Sulperazone* Cephalosporin/β-lactamase inhibitor
Ceforanide Precef Cephalosporin
Cefotaxime sodium Claforan Cephalosporin
Cefotetan disodium — Cephalosporin
Cefoxitin sodium Mefoxitin Cephalosporin
Cefpirome Cedixen, Cefrom, Cefron Cephalosporin
Cefpodoxime proxetil Orelox, Podomexef, Vantin Cephalosporin
Cefprozil Cefzil, Procef Cephalosporin
Cefsulodin Cefomonil, Monaspor Cephalosporin
Ceftaroline Teflaro Cephalosporin
Ceftazidime Ceptaz, Fortam, Fortaz, Fortum, Kefadim, Tazicef, Tazidime Cephalosporin
Ceftibuten Cedax, Keimax Cephalosporin
Ceftizoxime sodium Cefizox Cephalosporin
Ceftobiprole Zeftera Cephalosporin
Ceftriaxone sodium Rocephalin, Rocephin, Rocephine Cephalosporin
Cefuroxime axetil Ceftin, Zinnat Cephalosporin
Cefuroxime sodium Kefurox, Zinacef Cephalosporin
Cephalexin Cefanex, Ceporex, Keflex Cephalosporin
Cephalothin sodium Ceporacin, Keflin Cephalosporin
Cephapirin sodium Cefadyl Cephalosporin
Cephradine Anspor, Lisacef, Velosef Cephalosporin
Chloramphenicol Chloromycetin Chloramphenicol
Chloramphenicol palmitate Chloromycetin Palmitate Chloramphenicol
Chloramphenicol sodium succinate Chloromycetin Sodium Succinate Chloramphenicol
Chloroquine hydrochloride Aralen Hydrochloride Antimalarial
Chloroquine phosphate Aralen Phosphate Antimalarial
Ciclopirox Loprox Antifungal
Cidofovir Vistide Antiviral
Cinoxacin — Quinolone
Ciprofloxacin hydrochloride Ciflox, Ciloxan, Cipro, Ciprodex,* Cipro HC,* Ciproxin, Cipro XR, Fluoroquinolone
Proquin XR
Ciprofloxacin lactate Cipro IV Fluoroquinolone
Continued
634

Clarithromycin Biaxin, Biaxin XL, Biclar, Klacid, Prevpac,* Zeclar Macrolide

Clindamycin hydrochloride Cleocin, Dalacin C Lincosamide
Clindamycin palmitate hydrochloride Cleocin Pediatric Lincosamide
Clindamycin phosphate Cleocin Phosphate Lincosamide
Clioquinol Corque,* Diproform* Antifungal
Clofazimine Lampren, Lamprene Antimycobacterial
Clotrimazole Canesten, Cruex, Desenex, FemCare, Fungoid, Gyne-Lotrimin, Lotrimin, Antifungal
Lotrisone, Mycelex
Cloxacillin sodium Bactopen, Cloxapen, Orbenin Penicillin
Colistimethate sodium Coly-Mycin M Polymyxin
Cyclacillin Calthor, Cyclapen Penicillin
Cycloserine Seromycin Antimycobacterial
Dapsone — Sulfone
Daptomycin Cidecin, Cubicin, Dapcin Cyclic lipopeptide
Darunavir Prezista Antiretroviral
Dehydroemetine Mebadin (CDC†) Amebicide
Delavirdine Rescriptor Antiretroviral
Demeclocycline hydrochloride Declomycin Tetracycline
Dicloxacillin sodium Diclocil, Dycill, Pathocil Penicillin
Didanosine Videx, Videx EC Antiretroviral
Diethylcarbamazine Hetrazan, DEC (CDC†) Antiparasitic
Diloxanide furoate Entamide, Furamide Antiparasitic
Dirithromycin Dynabac, Dynabac D5-Pak Macrolide
Dolutegravir Tivicay Antiretroviral
Doripenem Doribax, Finibax Carbapenem
Doxycycline calcium Vibramycin Calcium Tetracycline
Doxycycline hyclate Doryx, Doxy 100, Doxy Caps, Periostat, Vibramycin Hyclate, Vibra-Tabs Tetracycline
Doxycycline monohydrate Vibramycin Monohydrate, Monodox Tetracycline
Econazole nitrate Ecostatin, Gyno-Pevaryl, Pevisone, Spectazole Antifungal
Efavirenz Atripla,* Stocrin, Sustiva, Viraday* Antiretroviral
Atripla,* Coviracil, Emtriva, Truvada,* Viraday* Antiretroviral
Elvitegravir Stribild* Antiretroviral
Emtricitabine Emtriva, Stribild,* Truvada,* Complera* Antiretroviral
Enfuvirtide Fuzeon Fusion inhibitor
Enoxacin Comprecin, Enoxor, Penetrex Fluoroquinolone
Entecavir Baraclude Antiviral
Ertapenem Invanz Carbapenem
Erythromycin Akne-Mycin, Benzamycin,* E-Base, E-Mycin, ERYC, Ery-Tab, PCE, Macrolide
Robimycin
Erythromycin estolate Ilosone Macrolide
Erythromycin ethylsuccinate E.E.S., EryPed, Eryzole,* E.S.P.,* Pediazole,* Sulfimycin* Macrolide
Erythromycin gluceptate Ilotycin Macrolide
Erythromycin lactobionate Erythrocin Macrolide
Erythromycin stearate Erythrocin Stearate, Wyamycin Macrolide
Ethambutol hydrochloride Myambutol, Servambutol Antimycobacterial
Ethionamide Trecator Antimycobacterial
Etravirine Intelence Antiretroviral
Famciclovir Famvir Antiviral
Fidaxomicin Dificid Macrolide
Flomoxef Flumarin Cephalosporin
Flucloxacillin Floxapen, Flucil, Flucillin, Fluclox Penicillin
Fluconazole Diflucan Antifungal
Flucytosine Ancobon, Ancotil Antifungal
Fosamprenavir Lexiva, Telzir Antiretroviral
Foscarnet sodium Foscavir Antiviral
Fosfomycin tromethamine Monuril, Monurol Urinary anti-infective
Furazolidone Furoxone Antiprotozoal
Ganciclovir sodium Cymevene, Cytovene, Vitrasert Antiviral
Gatifloxacin Zymar Fluoroquinolone
Gemifloxacin Factive Fluoroquinolone
Gentamicin sulfate Cidomycin, Garamycin, Genoptic, Jenamicin, Storz-G Aminoglycoside
Gentian violet — Antifungal
635


Griseofulvin Fulcin, Fulvicin P/G, Fulvicin U/F, Grifulvin V, Grisactin, Grisactin Ultra, Antifungal
Grisovin, Gris-PEG
Halofantrine Halfan Antiparasitic
Hydroxychloroquine sulfate Plaquenil Sulfate Antimalarial
Imipenem/cilastatin Primaxin,* Tienam* Carbapenem
Indinavir Crixivan Protease inhibitor
Interferon alfa-2a recombinant Roferon-A Antiviral
Interferon alfa-2b recombinant Intron A, Rebetron* Antiviral
Interferon alfacon-1 Infergen Antiviral
Interferon alfa-n3 Alferon N Antiviral
Iodoquinol Yodoxin M, Yodoxin Amebicide
Isoniazid Laniazid, Nydrazid, Rifamate,* Rifater,* Rifinah,* Rimactane/INH* Antimycobacterial
Itraconazole Sporanox Antifungal
Ivermectin Mectizan, Stromectol Antiparasitic
Josamycin Josalid Macrolide
Kanamycin sulfate Anamid Aminoglycoside
Ketoconazole Fungoral, Nizoral Antifungal
Lamivudine (3TC) Combivir,* Epivir, Epivir-HBV, Epzicom,* Kivexa,* Trizivir,* Zeffix Antiretroviral
Levofloxacin Cravit, Levaquin, Quixin, Tavanic Fluoroquinolone
Lincomycin hydrochloride Lincocin Lincosamide
Linezolid Zyvox, Zyvoxam Oxazolidinone
Lomefloxacin hydrochloride Maxaquin, Okacin, Uniquin Fluoroquinolone
Lopinavir/ritonavir Kaletra* Antiretrovirals
Loracarbef Lorabid Carbacephem
Lumefantrine Coartem* Antimalarial
Mafenide Sulfamylon Sulfonamide
Maraviroc Selzentry, Celsentri Antiretroviral
Mebendazole — Anthelmintic
Mefloquine Lariam Antimalarial
Meglumine antimonate Glucantim, Glucantime Antiparasitic
Melarsoprol Arsobal, Mel B (CDC†) Antiparasitic
Meropenem Meronem, Merrem Carbapenem
Methacycline Rondomycin Tetracycline
Methenamine hippurate Hiprex, Urex Urinary anti-infective
Methenamine mandelate Mandelamine Urinary anti-infective
Metronidazole Elyzol, Flagyl, Flagyl ER, Flagyl 375, Helidac,* MetroGel, Protostat, Rozex Nitroimidazole
Mezlocillin sodium Baypen Penicillin
Micafungin Mycamine Antifungal
Miconazole Daktacort,* Daktarin, Gyno-Daktarin, Micatin, Monistat Antifungal
Minocycline hydrochloride Dynacin, Minocin, Myrac, Vectrin Tetracycline
Moxalactam Moxam Cephalosporin
Moxifloxacin Avelox, Vigamox Fluoroquinolone
Mupirocin Bactroban Pseudomonic acid
Nadifloxacin Acuatim, Nadoxin, Nadixa Fluoroquinolone
Nafcillin sodium Nafcil, Unipen Penicillin
Naftifine Naftin Antifungal
Nalidixic acid NegGram Quinolone
Natamycin Natacyn Antifungal
Nelfinavir Viracept Protease inhibitor
Neomycin sulfate Kenacomb,* Maxitrol,* Mycifradin Sulfate, Neosporin* Aminoglycoside
Netilmicin sulfate Netilyn, Netromycin Aminoglycoside
Nevirapine Viramune Antiretroviral
Niclosamide Niclocide, Yomesan Anthelmintic
Nifurtimox Bayer 2502, Lampit (CDC†) Antiparasitic
Nitazoxanide Alinia Antiprotozoal
Nitrofurantoin Furadantin, Macrobid, Macrodantin Urinary anti-infective
Norfloxacin Floxacin, Noroxin Fluoroquinolone
Novobiocin sodium Albamycin —
Nystatin Kenacomb,* Mycostatin, Mycostatin Filmlok, Nilstat Antifungal
Ofloxacin Exocin, Floxin, Ocuflox, Tarivid Fluoroquinolone
Oritavancin diphosphate — Glycopeptide
Continued
636

Oseltamivir phosphate Tamiflu Antiviral

Oxacillin sodium — Penicillin
Oxamniquine Mansil Anthelmintic
Oxiconazole nitrate Oxistat Antifungal
Oxolinic acid Oribiox Quinolone
Oxytetracycline hydrochloride Uri-Tet, Urobiotic Tetracycline
Palivizumab Synagis Antiviral
Paromomycin sulfate Humatin Amebicide
Pazufloxacin Pasil, Pazucross Fluoroquinolone
Pefloxacin Peflacine, Peflox Fluoroquinolone
Peginterferon alfa-2a Pegasys Antiviral
Peginterferon alfa-2b Pegetron,* PEG-Intron Antiviral
Penciclovir Denavir, Vectavir Antiviral
Penicillin G benzathine Bicillin,* Bicillin C-R,* Bicillin C-R 900/300,* Bicillin L-A, Permapen Penicillin
Penicillin G + phenoxymethyl penicillin Kesso-pen* Penicillin
Penicillin G potassium Pfizerpen Penicillin
Penicillin G procaine Bicillin C-R,* Bicillin C-R 900/300,* Crysticillin AS, Pfizerpen-AS, Wycillin Penicillin
Penicillin G sodium — Penicillin
Penicillin V potassium — Penicillin
Pentamidine isethionate NebuPent, Pentacarinat, Pentam Antiprotozoal
Phenazopyridine/sulfisoxazole Azo Gantrisin* Symptomatic bladder therapy/sulfonamide
Pipemidic acid Dolcol Quinolone
Piperacillin sodium Pipracil, Pipril Penicillin
Piperacillin sodium/tazobactam sodium Tazocin,* Zosyn* Penicillin/β-lactamase inhibitor
Piperazine citrate — Anthelmintic
Pivmecillinam Mecillin 200, Selexid Penicillin
Polymyxin B sulfate Aerosporin, Neosporin* Polymyxin
Posaconazole Noxafil Antifungal
Praziquantel Biltricide Anthelmintic
Primaquine phosphate — Antimalarial
Proguanil Paludrine Antiparasitic
Pyrantel pamoate Antiminth, Ascarel, Combantrin, Pin-X, Reese’s Pinworm Medicine Anthelmintic
Pyrazinamide Rifater,* Zinamide Antimycobacterial
Pyrimethamine Daraprim Antimalarial
Quinacrine hydrochloride Atabrine Anthelmintic
Quinine sulfate Qualaquin Antimalarial
Quinupristin/dalfopristin Synercid* Streptogramin
Raltegravir Isentress Antiretroviral
Retapamulin Altabax Anti-impetigo
Ribavirin Copegus, Pegetron,* Rebetol, Rebetron,* Ribasphere, Virazole Antiviral
Rifabutin Mycobutin Antimycobacterial
Rifampin Rifadin, Rifamate,* Rifinah,* Rimactane, Rimactane/INH* Antimycobacterial
Rifapentine Priftin Antimycobacterial
Rifaximin Lumenax, Xifaxan Rifamycin
Rilpivirine Complera,* Edurant Antiretroviral
Rimantadine Flumadine, Roflual Antiviral
Ritonavir Norvir Protease inhibitor
Rosoxacin Eradacil Quinolone
Roxithromycin Rulid, Rulide, Surlid Macrolide
Rufloxacin Uroflox Fluoroquinolone
Saquinavir Fortovase, Invirase Protease inhibitor
Sertaconazole Ertaczo Antifungal
Silver sulfadiazine Silvadene, Thermazene Sulfonamide
Sitafloxacin Gracevit Fluoroquinolone
Sodium stibogluconate Pentostam (CDC†) Antiparasitic
Sodium thiosulfate Versiclear Antifungal
Sparfloxacin Zagam Fluoroquinolone
Spiramycin Rovamycin, Rovamycine Macrolide
Stavudine (d4T) Zerit Antiretroviral
Streptomycin sulfate — Aminoglycoside
Sulconazole Exelderm Antifungal
Sulfabenzamide/sulfacetamide/sulfathiazole Sultrin,* Triple Sulfa* Sulfonamide
637


Sulfadiazine — Sulfonamide
Sulfamethizole — Sulfonamide
Sulfamethoxazole — Sulfonamide
Sulfanilamide AVC Sulfonamide
Sulfisoxazole Azo-Sulfisoxazole,* Gantrisin Sulfonamide
Sulfisoxazole acetyl Eryzole,* Pediazole* Sulfonamide
Suramin Antrypol, Belganyl, Germanin, Naphuride (CDC†) Antiparasitic
Teicoplanin Targocid Glycopeptide
Lipoglycopeptide
Telaprevir Incivek Antiviral (hepatitis C)
Telavancin Vibativ Lipopeptide
Telbivudine Tyzeka Antiviral
Telithromycin Ketek Ketolide
Tenofovir Atripla,* Complera,* Stribild,* Truvada,* Viraday,* Viread Antiretroviral
Terbinafine Lamisil Antifungal
Terconazole Terazol, Zazole Antifungal
Tetracycline hydrochloride Achromycin V, Helidac,* Panmycin, Robitet, Sumycin, Tetrachel, Tetralan Tetracycline
Thiabendazole Mintezol Anthelmintic
Thiacetazone — Antimycobacterial
Ticarcillin disodium Tarcil Penicillin
Ticarcillin disodium/clavulanate potassium Timentin* Penicillin/β-lactamase inhibitor
Tigecycline Tygacil Glycylcycline
Tinidazole Tindamax Antiparasitic
Tioconazole Vagistat-1 Antifungal
Tipranavir Aptivus Antiretroviral
Tobramycin sulfate Nebcina, Obracin, TobraDex,* Tobrex Aminoglycoside
Tobramycin inhalation solution TOBI Aminoglycoside
Tolnaftate Mycil,* Tinactin, Tinaderm Antifungal
Tosufloxacin Ozex, Tosacin Fluoroquinolone
Trifluridine Viroptic Antiviral
Trimethoprim Monotrim, Primsol, Proloprim, Trimopan, Trimpex Folate antagonist
Trimethoprim/ Bactrim,* Bactrim DS,* Cotrim,* Cotrim D.S.,* Septra,* Septra DS,* Folate antagonists
sulfamethoxazole Sulfatrim,* Sulfoxaprim,* Uroplus*
Trimetrexate glucuronate NeuTrexin Antiprotozoal
Tripanavir Aptivus Antiretroviral
Trisulfapyrimidines — Sulfonamide
Troleandomycin Tao Macrolide
Undecylenic acid Fungi-Nail Antifungal
Valacyclovir Valtrex, Zelitrex Antiviral
Valganciclovir Valcyte Antiviral
Vancomycin hydrochloride Lyphocin, Vancocin, Vancoled, Vancor Glycopeptide
Vidarabine Vira-MP Antiviral
Voriconazole Vfend Antifungal
Zanamivir Relenza Antiviral
Zidovudine Combivir,* Retrovir, Trizivir* Antiretroviral
*A combination product.
†
CDC, Centers for Disease Control and Prevention Drug Service for distribution to U.S. clinicians.
TABLE 54-3 Trade and Generic Names

TRADE NAME GENERIC NAME CLASS
Abelcet Amphotericin B lipid complex Antifungal
Achromycin V Tetracycline hydrochloride Tetracycline
Acuatim Nadifloxacin Fluoroquinolone
Aerosporin Polymyxin B sulfate Polymyxin
Akne-Mycin Erythromycin Macrolide
Albamycin Novobiocin sodium —
Albenza Albendazole Antiparasitic
Alferon N Interferon alfa-n3 Antiviral
Alinia Nitazoxanide Antiprotozoal
Continued
638
TABLE 54-3 Trade and Generic Names—cont’d

Altabax Retapamulin Anti-impetigo

Ambaxin Bacampicillin Penicillin
AmBisome Amphotericin B liposomal Antifungal
Amoxiclav* Amoxicillin/clavulanate potassium Penicillin/β-lactamase inhibitor
Amoxil Amoxicillin Penicillin
Amphocin Amphotericin B Antifungal
Amphotec Amphotericin B cholesteryl sulfate complex Antifungal
Anamid Kanamycin Aminoglycoside
Ancef Cefazolin sodium Cephalosporin
Ancobon Flucytosine Antifungal
Ancotil Flucytosine Antifungal
Anspor Cephradine Cephalosporin
Antiminth Pyrantel pamoate Anthelmintic
Antrypol Suramin Antiparasitic
Aptivus Tipranavir Antiretroviral
Aralen Hydrochloride Chloroquine hydrochloride Antimalarial
Aralen Phosphate Chloroquine phosphate Antimalarial
Arsobal Melarsoprol Antiparasitic
Ascarel Pyrantel pamoate Anthelmintic
Atabrine Quinacrine hydrochloride Anthelmintic
Atripla* Efavirenz/tenofovir/emtricitabine Antiretroviral
Augmentin* Amoxicillin/clavulanate potassium Penicillin/β-lactamase inhibitor
Augmentin XR* Amoxicillin/clavulanate potassium Penicillin/β-lactamase inhibitor
AVC Sulfanilamide Sulfonamide
Avelox Moxifloxacin Fluoroquinolone
Azactam Aztreonam Monobactam
Azitromax Azithromycin Azalide
Azo-Sulfisoxazole* Sulfisoxazole Sulfonamide
Bacampicin Bacampicillin Penicillin
Baci-IM Bacitracin Polypeptide
Bacimex* Ampicillin/sulbactam Penicillin/β-lactamase inhibitor
Bactopen Cloxacillin Penicillin
Bactrim, Bactrim DS* Trimethoprim/sulfamethoxazole Folate antagonists
Bactroban Mupirocin Pseudomonic acid
Baloxin Balofloxacin Fluoroquinolone
Baraclude Entecavir Antiviral
Baxam Cefadroxil Cephalosporin
Bayer 2502 Nifurtimox Antiparasitic
Baypen Mezlocillin Penicillin
Belganyl Suramin Antiparasitic
Benzamycin* Erythromycin/benzoyl peroxide Macrolide/antiseptic
Biaxin, Biaxin XL Clarithromycin Macrolide
Bicillin C-R* Penicillin G procaine/benzathine Penicillin
Bicillin L-A Penicillin G benzathine Penicillin
Biclar Clarithromycin Macrolide
Biclin Amikacin Aminoglycoside
Biklin Amikacin Aminoglycoside
Biltricide Praziquantel Anthelmintic
Bitin Bithionol Antiparasitic
Calthor Cyclacillin Penicillin
Cancidas Caspofungin Antifungal
Canesten Clotrimazole Antifungal
Capastat Sulfate Capreomycin sulfate Polypeptide
Cedax Ceftibuten Cephalosporin
Cedixen Cefpirome Cephalosporin
Cefacidal Cefazolin Cephalosporin
Cefadel Cefmetazole Cephalosporin
Cefadyl Cephapirin sodium Cephalosporin
Cefamezin Cefazolin Cephalosporin
Cefamox Cefadroxil Cephalosporin
Cefanex Cephalexin Cephalosporin
Cefizox Ceftizoxime sodium Cephalosporin
639


Cefmetazon Cefmetazole Cephalosporin
Cefobid Cefoperazone Cephalosporin
Cefodie Cefoperazone Cephalosporin
Cefomonil Cefsulodin Cephalosporin
Cefoperazin* Cefoperazone/lidocaine Cephalosporin
Cefrom Cefpirome Cephalosporin
Cefron Cefpirome Cephalosporin
Cefspan Cefixime Cephalosporin
Ceftin Cefuroxime axetil Cephalosporin
Cefzil Cefprozil Cephalosporin
Cefzon Cefdinir Cephalosporin
Celsentri Maraviroc Antiretroviral
Ceporacin Cephalothin Cephalosporin
Ceporex Cephalexin Cephalosporin
Ceptaz Ceftazidime Cephalosporin
Chloromycetin Chloramphenicol Chloramphenicol
Chloromycetin Palmitate Chloramphenicol palmitate Chloramphenicol
Chloromycetin Sodium Succinate Chloramphenicol sodium succinate Chloramphenicol
Cidecin Daptomycin Cyclic lipopeptide
Cidomycin Gentamicin Aminoglycoside
Ciflox Ciprofloxacin hydrochloride Fluoroquinolone
Ciloxan Ciprofloxacin hydrochloride Fluoroquinolone
Cipro Ciprofloxacin hydrochloride Fluoroquinolone
Ciprodex* Ciprofloxacin/dexamethasone Fluoroquinolone/steroid
Cipro HC* Ciprofloxacin/hydrocortisone Fluoroquinolone/steroid
Cipro IV Ciprofloxacin lactate Fluoroquinolone
Ciproxin Ciprofloxacin hydrochloride Fluoroquinolone
Cipro XR Ciprofloxacin Fluoroquinolone
Claforan Cefotaxime sodium Cephalosporin
Clamoxyl Amoxicillin Penicillin
Clavepen* Amoxicillin/clavulanate potassium Penicillin/β-lactamase inhibitor
Cleocin Clindamycin hydrochloride Lincosamide
Cleocin Pediatric Clindamycin palmitate hydrochloride Lincosamide
Cleocin Phosphate Clindamycin phosphate Lincosamide
Cloxapen Cloxacillin sodium Penicillin
Coactin Amdinocillin Penicillin
Coartem* Artemether/Lumefantrine Antimalarial
Coly-Mycin M Colistimethate sodium Polymyxin
Combactam* Ampicillin/sulbactam Penicillin/β-lactamase inhibitor
Combantrin Pyrantel pamoate Anthelmintic
Combivir* Lamivudine/zidovudine Antiretroviral
Complera Emtricitabine/rilpivirine/tenofovir Antiretroviral
Comprecin Enoxacin Fluoroquinolone
Copegus Ribavirin Antiviral
Corque* Clioquinol/hydrocortisone Antifungal
Cotrim, Cotrim D.S.* Trimethoprim/sulfamethoxazole Folate antagonists
Coviracil Emtricitabine Antiretroviral
Cravit Levofloxacin Fluoroquinolone
Crixivan Indinavir Protease inhibitor
Cruex Clotrimazole Antifungal
Crysticillin Penicillin G procaine Penicillin
Cubicin Daptomycin Cyclic lipopeptide
Cyclapen Cyclacillin Penicillin
Cymevene Ganciclovir sodium Antiviral
Cytovene Ganciclovir sodium Antiviral
Daktacort* Miconazole/hydrocortisone Antifungal
Daktarin Miconazole Antifungal
Dalacin C Clindamycin hydrochloride Lincosamide
Dapcin Daptomycin Cyclic lipopeptide
Daraprim Pyrimethamine Antimalarial
DEC Diethylcarbamazine Antiparasitic
Continued
640

Declomycin Demeclocycline hydrochloride Tetracycline

Denavir Penciclovir Antiviral
Denvar Cefixime Cephalosporin
Desenex Clotrimazole Antifungal
Diclocil Dicloxacillin Penicillin
Dificid Fidaxomycin Macrolide
Diflucan Fluconazole Antifungal
Diproform* Clioquinol/betamethasone Antifungal
Distaclor Cefaclor Cephalosporin
Dolcol Pipemidic acid Quinolone
Doribax Doripenem Carbapenem
Doryx Doxycycline hyclate Tetracycline
Doxamil Amoxicillin Penicillin
Doxy 100 Doxycycline hyclate Tetracycline
Doxy Caps Doxycycline hyclate Tetracycline
Duracef Cefadroxil Cephalosporin
Duricef Cefadroxil Cephalosporin
Dycill Dicloxacillin sodium Penicillin
Dynabac, Dynabac D5-Pak Dirithromycin Macrolide
Dynacin Minocycline Tetracycline
Dynapen Dicloxacillin Penicillin
E.E.S. Erythromycin ethylsuccinate Macrolide
E-Base Erythromycin Macrolide
Ecostatin Econazole Antifungal
Edurant Rilpivirine Antiretroviral
Elyzol Metronidazole Nitroimidazole
Emtriva Emtricitabine Antiretroviral
E-Mycin Erythromycin Macrolide
Enoxor Enoxacin Fluoroquinolone
Entamide Diloxanide furoate Antiparasitic
Epivir, Epivir-HBV Lamivudine (3TC) Antiretroviral
Epzicom* Abacavir/lamivudine Antiretroviral
Eradacil Rosoxacin Quinolone
Eraxis Anidulafungin Antifungal
Ertaczo Sertaconazole Antifungal
ERYC Erythromycin Macrolide
EryPed Erythromycin ethylsuccinate Macrolide
Ery-Tab Erythromycin Macrolide
Erythrocin Erythromycin lactobionate Macrolide
Erythrocin Stearate Erythromycin stearate Macrolide
Eryzole* Erythromycin ethylsuccinate/sulfisoxazole Macrolide/sulfonamide
Eskazole Albendazole Antiparasitic
E.S.P.* Erythromycin ethylsuccinate/sulfisoxazole Macrolide/sulfonamide
Exelderm Sulconazole Antifungal
Exocin Ofloxacin Fluoroquinolone
Factive Gemifloxacin Fluoroquinolone
Famvir Famciclovir Antiviral
Femcare Clotrimazole Antifungal
Femstat 3 Butoconazole Antifungal
Finibax Doripenem Carbapenem
Flagyl Metronidazole Nitroimidazole
Flagyl ER Metronidazole Nitroimidazole
Flagyl 375 Metronidazole Nitroimidazole
Floxacin Norfloxacin Fluoroquinolone
Floxapen Flucloxacillin Penicillin
Floxin Ofloxacin Fluoroquinolone
Flucil Flucloxacillin Penicillin
Flucillin Flucloxacillin Penicillin
Fluclox Flucloxacillin Penicillin
Flumadine Rimantadine Antiviral
Flumarin Flomoxef Cephalosporin
Fortam Ceftazidime Cephalosporin
641


Fortaz Ceftazidime Cephalosporin
Fortovase Saquinavir Protease inhibitor
Fortum Ceftazidime Cephalosporin
Foscavir Foscarnet sodium Antiviral
Fulcin Griseofulvin Antifungal
Fulvicin P/G Griseofulvin Antifungal
Fulvicin U/F Griseofulvin Antifungal
Fungilin Amphotericin B Antifungal
Fungizone Amphotericin B Antifungal
Fungi-nail Undecylenic acid Antifungal
Fungoid Clotrimazole Antifungal
Fungol Carbol-fuchsin Antifungal
Fungoral Ketoconazole Antifungal
Furadantin Nitrofurantoin Urinary anti-infective
Furamide Diloxanide furoate Antiparasitic
Furoxone Furazolidone Antiprotozoal
Fuzeon Enfuvirtide Fusion inhibitor
Gantrisin Sulfisoxazole Sulfonamide
Garamycin Gentamicin Aminoglycoside
Geninax Garenoxacin Des-quinolone
Genoptic Gentamicin Aminoglycoside
Germanin Suramin Antiparasitic
Glucantim Meglumine antimonate Antiparasitic
Glucantime Meglumine antimonate Antiparasitic
Gracevit Sitafloxacin Fluoroquinolone
Grifulvin V Griseofulvin Antifungal
Grisactin Griseofulvin Antifungal
Grisactin Ultra Griseofulvin Antifungal
Grisovin Griseofulvin Antifungal
Gris-PEG Griseofulvin Antifungal
Gynazole-1 Butoconazole nitrate Antifungal
Gyne-Lotrimin Clotrimazole Antifungal
Gyno-Daktarin Miconazole Antifungal
Gynomyk Butoconazole Antifungal
Gyno-Pevaryl Econazole Antifungal
Halfan Halofantrine Antiparasitic
Helidac* Bismuth/metronidazole/tetracycline Anti-Helicobacter
Hepsera Adefovir dipivoxil Antiviral
Hetrazan Diethylcarbamazine Antiparasitic
Hiconcil Amoxicillin Penicillin
Hiprex Methenamine hippurate Urinary anti-infective
Humatin Paromomycin sulfate Amebicide
Ilosone Erythromycin estolate Macrolide
Ilotycin Erythromycin gluceptate Macrolide
Incivek Telaprevir Antiretroviral
Infergen Interferon alfacon-1 Antiviral
Intelence Etravirine Antiretroviral
Intron A Interferon alfa-2b recombinant Antiviral
Invanz Ertapenem Carbapenem
Invirase Saquinavir Protease inhibitor
Isentress Raltegravir Antiretroviral
Isepacin Isepamicin Aminoglycoside
Jenamicin Gentamicin sulfate Aminoglycoside
Josalid Josamycin Macrolide
Kaletra* Lopinavir/ritonavir Antiretroviral
Kefadim Ceftazidime Cephalosporin
Keflex Cephalexin Cephalosporin
Keflin Cephalothin sodium Cephalosporin
Kefurox Cefuroxime sodium Cephalosporin
Keimax Ceftibuten Cephalosporin
Kenacomb* Neomycin/nystatin Aminoglycoside/antifungal
Continued
642

Kesso-pen* Penicillin G/phenoxymethyl penicillin Penicillins

Ketek Telithromycin Ketolide
Kivexa* Abacavir/lamivudine/zidovudine Antiretroviral
Klacid Clarithromycin Macrolide
Lamisil Terbinafine Antifungal
Lampit Nifurtimox Antiparasitic
Lampren Clofazimine Antimycobacterial
Lamprene Clofazimine Antimycobacterial
Laniazid Isoniazid Antimycobacterial
Lariam Mefloquine Antimalarial
Levaquin Levofloxacin Fluoroquinolone
Lexiva Fosamprenavir Antiretroviral
Likacin Amikacin Aminoglycoside
Lincocin Lincomycin Lincosamide
Lisacef Cephradine Cephalosporin
Loprox Ciclopirox Antifungal
Lorabid Loracarbef Carbacephem
Lorothidol Bithionol Antiparasitic
Lotrimin Clotrimazole Antifungal
Lotrisone Clotrimazole Antifungal
Lumenax Rifaximin Rifamycin
Lyphocin Vancomycin hydrochloride Glycopeptide
Macrobid Nitrofurantoin Urinary anti-infective
Macrodantin Nitrofurantoin Urinary anti-infective
Malarone* Atovaquone/proguanil Antimalarial
Mandelamine Methenamine mandelate Urinary anti-infective
Mandokef Cefamandole Cephalosporin
Mandol Cefamandole Cephalosporin
Mansil Oxamniquine Anthelmintic
Maxaquin Lomefloxacin Fluoroquinolone
Maxcef Cefepime Cephalosporin
Maxipime Cefepime Cephalosporin
Maxitrol* Dexamethasone/neomycin/polymyxin B Antifungal/polymyxin
Mebadin Dehydroemetine Amebicide
Mecillin 200 Pivmecillinam Penicillin
Mectizan Ivermectin Antiparasitic
Mefoxitin Cefoxitin Cephalosporin
Mel B Melarsoprol Antiparasitic
Mepron Atovaquone Antiparasitic
Meronem Meropenem Carbapenem
Merrem Meropenem Carbapenem
Metazol Cefmetazole sodium Cephalosporin
MetroGel Metronidazole Nitroimidazole
Micatin Miconazole Antifungal
Minocin Minocycline hydrochloride Tetracycline
Mintezol Thiabendazole Anthelmintic
Monaspor Cefsulodin Cephalosporin
Monistat Miconazole Antifungal
Monobac Aztreonam Monobactam
Monocid Cefonicid sodium Cephalosporin
Monodox Doxycycline monohydrate Tetracycline
Monotrim Trimethoprim Folate antagonist
Monuril Fosfomycin tromethamine Urinary anti-infective
Monurol Fosfomycin tromethamine Urinary anti-infective
Moxam Moxalactam Cephalosporin
Myambutol Ethambutol hydrochloride Antimycobacterial
Mycamine Micafungin Antifungal
Mycelex Clotrimazole Antifungal
Mycelex-3 Butoconazole Antifungal
Mycifradin Sulfate Neomycin sulfate Aminoglycoside
Mycil* Tolnaftate Antifungal
Mycobutin Rifabutin Antimycobacterial
643


Mycostatin (Filmlok) Nystatin Antifungal
Myrac Minocycline Tetracycline
Nadixa Nadifloxacin Fluoroquinolone
Nadoxin Nadifloxacin Fluoroquinolone
Nafcil Nafcillin sodium Penicillin
Naftin Naftifine Antifungal
Naphuride Suramin Antiparasitic
Natacyn Natamycin Antifungal
Nebcina Tobramycin Aminoglycoside
NebuPent Pentamidine isethionate Antiprotozoal
NegGram Nalidixic acid Quinolone
Neosporin* Neomycin/polymyxin B Aminoglycoside/polymyxin
Netilyn Netilmicin Aminoglycoside
Netromycin Netilmicin Aminoglycoside
NeuTrexin Trimetrexate Antiprotozoal
Niclocide Niclosamide Anthelmintic
Nilstat Nystatin Antifungal
Nizoral Ketoconazole Antifungal
Noroxin Norfloxacin Fluoroquinolone
Norvir Ritonavir Protease inhibitor
Noxafil Posaconazole Antifungal
Nydrazid Isoniazid Antimycobacterial
Nyotran Liposomal nystatin Antifungal
Obracin Tobramycin Aminoglycoside
Ocuflox Ofloxacin Fluoroquinolone
Okacin Lomefloxacin Fluoroquinolone
Omnicef Cefdinir Cephalosporin
Orbenin Cloxacillin Penicillin
Orelox Cefpodoxime proxetil Cephalosporin
Oribiox Oxolinic acid Quinolone
Oxistat Oxiconazole nitrate Antifungal
Ozex Tosufloxacin Fluoroquinolone
Paludrine Proguanil Antiparasitic
Paluther Artemether Antimalarial
Panmycin Tetracycline hydrochloride Tetracycline
Paser Aminosalicylic acid Antimycobacterial
Pasil Pazufloxacin Fluoroquinolone
Pathocil Dicloxacillin sodium Penicillin
Pazucross Pazufloxacin Fluoroquinolone
PCE Erythromycin Macrolide
Pediazole* Erythromycin ethylsuccinate/sulfisoxazole Macrolide/sulfonamide
Peflacine Pefloxacin Fluoroquinolone
Peflox Pefloxacin Fluoroquinolone
Pegasys Peginterferon alfa-2a Antiviral
Pegetron* Peginterferon alfa-2b/ribavirin Antiviral
PEG-Intron Peginterferon alfa-2b Antiviral
Penetrex Enoxacin Fluoroquinolone
Penglobe Bacampicillin Penicillin
Pentacarinat Pentamidine isethionate Antiprotozoal
Pentam Pentamidine isethionate Antiprotozoal
Pentostam Sodium stibogluconate Antiparasitic
Periostat Doxycycline Tetracycline
Permapen Penicillin G benzathine Penicillin
Pevisone Econazole Antifungal
Pfizerpen Penicillin G potassium Penicillin
Pfizerpen-AS Penicillin G procaine Penicillin
Pin-X Pyrantel pamoate Anthelmintic
Pipracil Piperacillin Penicillin
Pipril Piperacillin Penicillin
Plaquenil Sulfate Hydroxychloroquine sulfate Antimalarial
Plasmotrim Artesunate Antimalarial
Continued
644

Podomexef Cefpodoxime proxetil Cephalosporin

Polycillin Ampicillin trihydrate Penicillin
Polycillin-N Ampicillin sodium Penicillin
Polymox Amoxicillin Penicillin
Precef Ceforanide Cephalosporin
Prevpac* Amoxicillin/clarithromycin/lansoprazole Anti-Helicobacter
Prezista Darunavir Antiretroviral
Priftin Rifapentine Antimycobacterial
Primaxin* Imipenem, cilastatin Carbapenem
Primbactam Aztreonam Monobactam
Primsol Trimethoprim Folate antagonist
Probampacin* Ampicillin/probenecid Penicillin/tubular secretion inhibitor
Procef Cefprozil Cephalosporin
Proloprim Trimethoprim Folate antagonist
Proquin XR Ciprofloxacin Fluoroquinolone
Protostat Metronidazole Nitroimidazole
Qualaquin Quinine sulfate Antimalarial
Quixin Levofloxacin Fluoroquinolone
Rebetol Ribavirin Antiviral
Rebetron* Interferon alfa-2b recombinant/ribavirin Antiviral
Reese’s Pinworm Medicine Pyrantel pamoate Anthelmintic
Relenza Zanamivir Antiviral
Rescriptor Delavirdine Antiretroviral
Retrovir Zidovudine Antiviral
Reyataz Atazanavir Protease inhibitor
Riamet* Artemether/lumefantrine Antimalarial
Ribasphere Ribavirin Antiviral
Rifadin Rifampin Antimycobacterial
Rifamate* Rifampin/isoniazid Antimycobacterial
Rifater* Rifampin/pyrazinamide Antimycobacterial
Rifinah* Rifampin/isoniazid Antimycobacterial
Rimactane Rifampin Antimycobacterial
Rimactane/INH* Rifampin/isoniazid Antimycobacterial
Robimycin Erythromycin Macrolide
Robitet Tetracycline hydrochloride Tetracycline
Rocephalin Ceftriaxone Cephalosporin
Rocephin Ceftriaxone Cephalosporin
Rocephine Ceftriaxone Cephalosporin
Roferon-A Interferon alfa-2a recombinant Antiviral
Roflual Rimantadine Antiviral
Rondomycin Methacycline Tetracycline
Rovamycin Spiramycin Macrolide
Rovamycine Spiramycin Macrolide
Rozex Metronidazole Nitroimidazole
Rulid Roxithromycin Macrolide
Rulide Roxithromycin Macrolide
Securopen Azlocillin Penicillin
Selexid Pivmecillinam Penicillin
Selzentry Maraviroc Antiretroviral
Septra, Septra DS* Trimethoprim/sulfamethoxazole Folate antagonists
Seromycin Cycloserine Antimycobacterial
Servambutol Ethambutol Antimycobacterial
Silvadene Silver sulfadiazine Sulfonamide
Spectazole Econazole nitrate Antifungal
Spectracef Cefditoren pivoxil Cephalosporin
Spectrobid Bacampicillin hydrochloride Penicillin
Sporanox Itraconazole Antifungal
Stocrin Efavirenz Antiretroviral
Storz-G Gentamicin sulfate Aminoglycoside
Stribild Elvitegravir/cobicistat/emtricitabine/tenofovir Antiretroviral
Stromectol Ivermectin Antiparasitic
Sulfamylon Mafenide Sulfonamide
645


Sulfatrim* Trimethoprim/sulfamethoxazole Folate antagonists
Sulfoxaprim* Trimethoprim/sulfamethoxazole Folate antagonists
Sulperazon* Cefoperazone/sulbactam Cephalosporin/β-lactamase inhibitor
Sulperazone* Cefoperazone/sulbactam Cephalosporin/β-lactamase inhibitor
Sultrin Triple Sulfa* Sulfabenzamide/sulfacetamide/sulfathiazole Sulfonamide
Sumamed Azithromycin Azalide
Sumycin Tetracycline hydrochloride Tetracycline
Suprax Cefixime Cephalosporin
Surlid Roxithromycin Macrolide
Sustiva Efavirenz Antiretroviral
Symadine Amantadine hydrochloride Antiviral
Symmetrel Amantadine hydrochloride Antiviral
Synagis Palivizumab Antiviral
Synercid* Quinupristin/dalfopristin Streptogramin
Tamiflu Oseltamivir Antiviral
Tao Troleandomycin Macrolide
Tarcil Ticarcillin disodium Penicillin
Targocid Teicoplanin Glycopeptide
Tarivid Ofloxacin Fluoroquinolone
Tavanic Levofloxacin Fluoroquinolone
Tazicef Ceftazidime Cephalosporin
Tazidime Ceftazidime Cephalosporin
Tazocin* Piperacillin/tazobactam Penicillin/β-lactamase inhibitor
Teflaro Ceftaroline Cephalosporin
Telzir Fosamprenavir Antiretroviral
Terazol Terconazole Antifungal
Tetrachel Tetracycline hydrochloride Tetracycline
Tetralan Tetracycline hydrochloride Tetracycline
Thermazene Silver sulfadiazine Sulfonamide
Tienam* Imipenem/cilastatin Carbapenem
Timentin* Ticarcillin disodium/clavulanate potassium Penicillin/β-lactamase inhibitor
Tinactin Tolnaftate Antifungal
Tinaderm Tolnaftate Antifungal
Tindamax Tinidazole Antiparasitic
Tivicay Dolutegravir Antiretroviral
TOBI Tobramycin inhalation solution Aminoglycoside
TobraDex* Tobramycin/dexamethasone Aminoglycoside/corticosteroid
Tobrex Tobramycin Aminoglycoside
Tosacin Tosufloxacin Fluoroquinolone
Totacillin Ampicillin trihydrate Penicillin
Totacillin-N Ampicillin sodium Penicillin
Trecator Ethionamide Antimycobacterial
Trimopan Trimethoprim Folate antagonist
Trimox Amoxicillin Penicillin
Trimpex Trimethoprim Folate antagonist
Triple Sulfa* Sulfabenzamide/sulfacetamide/sulfathiazole Sulfonamide
Trizivir* Abacavir/lamivudine/zidovudine Antiretroviral
Trobicin Spectinomycin hydrochloride Aminocyclitol
Truvada* Emtricitabine/tenofovir Antiretroviral
Tygacil Tigecycline Glycylcycline
Tyzeka Telbivudine Antiviral
Ultracef Cefadroxil Cephalosporin
Unasyn* Ampicillin/sulbactam Penicillin/β-lactamase inhibitor
Unipen Nafcillin sodium Penicillin
Uniquin Lomefloxacin Fluoroquinolone
Urex Methenamine hippurate Urinary anti-infective
Uri-Tet Oxytetracycline hydrochloride Tetracycline
Urobactam Aztreonam Monobactam
Urobiotic Oxytetracycline hydrochloride Tetracycline
Uroflox Rufloxacin Fluoroquinolone
Uroplus* Trimethoprim/sulfamethoxazole Folate antagonists
Continued
646

Valcyte Valganciclovir Antiviral

Valtrex Valacyclovir Antiviral
Vancocin Vancomycin hydrochloride Glycopeptide
Vancoled Vancomycin hydrochloride Glycopeptide
Vancor Vancomycin hydrochloride Glycopeptide
Vantin Cefpodoxime proxetil Cephalosporin
Vectavir Penciclovir Antiviral
Vectrin Minocycline Tetracycline
Velosef Cephradine Cephalosporin
Vercef Cefaclor Cephalosporin
Versiclear Sodium thiosulfate Antifungal
VFend Voriconazole Antifungal
Vibativ Televancin Lipopeptide
Vibramycin Calcium Doxycycline calcium Tetracycline
Vibramycin Hyclate Doxycycline hyclate Tetracycline
Vibramycin Monohydrate Doxycycline monohydrate Tetracycline
Vibra-Tabs Doxycycline hyclate Tetracycline
Victrelis Boceprevir Antiviral (hepatitis C)
Videx Didanosine Antiretroviral
Videx EC Didanosine Antiretroviral
Vigamox Moxifloxacin Fluoroquinolone
Viracept Nelfinavir Protease inhibitor
Viraday* Efavirenz/emtricitabine/tenofovir Antiretroviral
Vira-MP Vidarabine Antiviral
Viramune Nevirapine Antiretroviral
Virazole Ribavirin Antiviral
Viread Tenofovir Antiretroviral
Viroptic Trifluridine Antiviral
Vistide Cidofovir Antiviral
Vitrasert Ganciclovir Antiviral
Wellvone Atovaquone Antiparasitic
Wyamycin Erythromycin stearate Macrolide
Wycillin Penicillin G procaine Penicillin
Xifaxan Rifaximin Rifamycin
Xigris Drotrecogin alfa (activated) Antisepsis
Yodoxin Iodoquinol Amebicide
Yodoxin M Iodoquinol Amebicide
Yomesan Niclosamide Anthelmintic
Zagam Sparfloxacin Fluoroquinolone
Zazole Terconazole Antifungal
Zeclar Clarithromycin Macrolide
Zeffix Lamivudine Antiretroviral
Zeftera Ceftobiprole Cephalosporin
Zelitrex Valacyclovir Antiviral
Zentel Albendazole Antiparasitic
Zerit Stavudine (d4T) Antiretroviral
Ziagen Abacavir Antiretroviral
Ziagenavir Abacavir Antiretroviral
Zinacef Cefuroxime sodium Cephalosporin
Zinamide Pyrazinamide Antimycobacterial
Zinnat Cefuroxime axetil Cephalosporin
Zithromax Azithromycin Azalide
Zithromax Tri-Pak Azithromycin Azalide
Zitromax Azithromycin Azalide
Zmax Azithromycin Azalide
Zolicef Cefazolin sodium Cephalosporin
Zosyn* Piperacillin/tazobactam Penicillin/β-lactamase inhibitor
Zovirax Acyclovir Antiviral
Z-PAK Azithromycin Azalide
Zymar Gatifloxacin Fluoroquinolone
Zyvox Linezolid Oxazolidinone
Zyvoxam Linezolid Oxazolidinone
*A combination product.
647
TABLE 54-4 Penicillin Dosage Forms

FORMULATIONS

Oral
GENERIC NAME Tablets/Capsules (mg) Liquid (mg/mL) Parenteral (g)
Amoxicillin 125,* 250,* 400,* 250, 500, 875, 1000, 3000 50/1, 125/5, 250/5, 400/5, 500/5 0.25, 0.5, 1
Amoxicillin/clavulanate† 125, 125,* 200,* 250,* 375, 400,* 250, 500, 125/5, 200/5, 250/5, 400/5 0.5, 1
875, 1000‡
Ampicillin 125,* 250, 500, 1000 100/1, 125/1.25, 125/5, 250/5, 500/5 0.1, 0.125, 0.25, 0.5, 1, 2, 10
Ampicillin/sulbactam 375 1.5, 3
Azlocillin 0.5, 1, 2, 3, 4
Bacampicillin 400, 800 125/5
Carbenicillin 1, 5
Carbenicillin indanyl sodium 382, 500
Cloxacillin 250, 500 125/5 0.25, 0.5, 1, 2
Cyclacillin 250, 500 125/5, 250/5
Dicloxacillin 125, 250, 500 62.5/5
Flucloxacillin 250, 500 125/5, 250/5 0.25, 0.5, 1
Methicillin 1, 2, 4, 6, 10
Mezlocillin 0.5, 1, 2, 3, 4, 5
Nafcillin 250, 500 250/5 0.5, 1, 2, 4, 10
Oxacillin 250, 500 250/5 0.25, 0.5, 1, 2, 4, 10
Penicillin G§ 0.1 MU, 0.2 MU, 0.25 MU, 0.4 MU, 0.5 MU, 0.2 MU/5, 0.25 MU/5, 0.5 MU/5 0.3 MU, 0.5 MU, 1 MU, 5 MU, 10 MU,
0.8 MU, 4 MU 20 MU
Penicillin G benzathine 0.3 MU, 0.6 MU, 1.2 MU, 2.4 MU
Penicillin G procaine 0.3 MU, 0.6 MU, 1.2 MU, 2.4 MU
Penicillin V potassium 125,* 250, 300, 312.5, 500, 625, 937.5 125/5, 180/5, 250/5, 300/5
Piperacillin 1, 2, 3, 4, 40
Piperacillin/tazobactam 2.25, 3.375, 4.5
Pivmecillinam 200
Ticarcillin 1, 3, 6, 20, 30
Ticarcillin/clavulanate 3.1, 31
*Chewable.
†
Doses based on amoxicillin content.
‡
Extended release.
§
400,000 IU = 0.4 MU = 250 mg.
TABLE 54-5 Cephalosporin Dosage Forms

FORMULATIONS
Oral
First Generation
Cefadroxil 250, 500, 1000 125/5, 250/5, 500/5, 500/10
Cefazolin 0.25, 0.5, 1, 2, 5, 10, 20
Cephalexin 250, 500, 1000 100/1, 125/1.25, 125/5, 250/5, 375/5, 500/5
Cephalothin 1, 2, 4, 20
Cephapirin 0.5, 1, 2, 4, 20
Cephradine 250, 500, 1000 125/5, 250/5 0.25, 0.5, 1, 2
Second Generation
Cefaclor 250, 375,* 500, 500* 125/5, 187/5, 250/5, 375/5
Cefamandole 0.5, 1, 2, 10
Cefonicid 0.5, 1
Cefotetan 0.5, 1, 2, 10
Cefoxitin 0.5, 1, 2, 10
Cefprozil 250, 500 125/5, 250/5
Cefuroxime 125, 250, 500 125/5, 250/5 0.25, 0.75, 1.5, 7.5
Third Generation
Cefdinir 300 125/5
Cefditoren pivoxil 200
Cefixime 50, 100, 200, 400 100/5
Cefoperazone 0.25, 0.5, 1, 2, 10
Cefotaxime 0.5, 1, 2, 10, 20
Cefpodoxime 100, 200 50/5, 100/5
Continued
648
TABLE 54-5 Cephalosporin Dosage Forms—cont’d

FORMULATIONS
Oral
Cefsulodin 0.5, 1, 2
Ceftazidime 0.25, 0.5, 1, 2, 6, 10
Ceftibuten 218, 400, 435 90/5, 98/5, 196/5
Ceftriaxone 0.25, 0.5, 1, 2, 10
Moxalactam 0.25, 0.5, 1, 2, 10
Fourth Generation
Cefepime 0.5, 1, 2
Fifth Generation
Ceftobiprole 0.5
Ceftaroline 0.4, 0.6
*Sustained release.
TABLE 54-6 Aminoglycoside Dosage Forms TABLE 54-7 Tetracycline and Related Products
FORMULATIONS Dosage Forms
Oral FORMULATIONS
GENERIC Tablets/ Liquid Oral
NAME Capsules (mg) (mg/mL) Parenteral (g) GENERIC Tablets/Capsules Liquid
Amikacin 0.1, 0.25, 0.35, 0.5, 0.75, 1 NAME (mg) (mg/mL) Parenteral (g)
Gentamicin 0.01, 0.02, 0.04, 0.08, 0.8 Demeclocycline 75, 150, 300
Kanamycin 500 0.075, 0.5, 1 Doxycycline 20, 50, 100, 100* 25/5, 50/5 0.1, 0.2
Neomycin 350, 500 125/5 0.5 Methacycline 150, 300 75/5
Netilmicin 0.05, 0.1, 0.15, 0.2, 2 Minocycline 50, 75, 100 50/5 0.1
Streptomycin 1 Oxytetracycline 125, 250 100/1, 125/5 0.05, 0.25
Tobramycin 300* 0.02, 0.04, 0.06, 0.08, 0.3, Tigecycline 0.05
1.2, 2 Tetracycline 50, 100, 250, 500 125/5 0.1, 0.25, 0.5
*For inhalation. *Sustained release.
TABLE 54-8 Macrolide, Azalide, Ketolide, Lincosamide, Chloramphenicol, and Metronidazole Dosage Forms
FORMULATIONS
Oral
Azithromycin 250, 500, 600, 1000 100/5, 200/5, 2000/60* 0.5
Clarithromycin 250, 500, 500* 125/5, 125/15, 187.5/5, 250/5
Dirithromycin 250
Erythromycin base 250, 250,* 333, 333,* 500, 500*
Erythromycin stearate 100, 250, 500 100/2.5, 125/5, 200/5, 250/5
Erythromycin ethylsuccinate 200,† 400, 600 100/2.5, 125/5, 200/5, 400/5
Erythromycin lactobionate 0.5, 1
Erythromycin gluceptate 0.5, 1
Erythromycin estolate 125, 125,† 250,† 250, 500 100/1, 125/1, 125/5, 250/1, 250/5
Fidaxomycin 200
Roxithromycin 150, 300
Telithromycin 800
Clindamycin 75, 150, 300 75/5 0.3, 0.6, 0.9
Lincomycin 250, 500 50/1, 250/5 0.3, 0.6
Chloramphenicol 250 30/1, 125/5 1
Metronidazole 200, 250, 375, 400, 500, 500,‡ 750,* 1000‡ 200/5 0.5
*Sustained release.
†
Chewable.
‡
Vaginal suppository.
649
TABLE 54-9 Miscellaneous Agent Dosage Forms TABLE 54-10 Folate Antagonist Dosage Forms
FORMULATIONS FORMULATIONS

Oral Oral
Tablets/ Liquid Parenteral Tablets/ Liquid
GENERIC NAME Capsules (mg) (mg/mL) (g) GENERIC NAME Capsules (mg) (mg/mL) Parenteral (g)
Aztreonam 0.5, 1, 2 Trimethoprim/ 20/80, 100/400, 8/40/1, 0.080/0.400,
Colistimethate 25/5 0.15 sulfamethoxazole 160/800 40/200/5, 0.160/0.800
80/400/5
Daptomycin 0.5
Trimethoprim 100, 200, 300 50/5 0.020/1 mL
Doripenem 0.5
Sulfisoxazole 500 500/5
Ertapenem 1
Sulfamethoxazole 500, 1000 500/5
Fusidic acid 250 246/5
Sulfamethizole 500, 1000 100/5
Imipenem 0.25, 0.5, 0.75
Sulfadiazine 500
Linezolid 400, 600 100/5 0.2, 0.4, 0.6
Dapsone 25, 100
Loracarbef 200, 400 100/5, 200/5
Trimetrexate 0.040
Meropenem 0.25, 0.5, 1
Quinupristin/dalfopristin 0.15, 0.35
Rifaximin 200
Telavancin 0.25, 0.75
Teicoplanin 0.4
Vancomycin 125, 250 0.5, 1, 5, 10
TABLE 54-11 Quinolone and Urinary Anti-infective Dosage Forms

FORMULATIONS
Oral
Quinolones
Cinoxacin 250, 500
Ciprofloxacin 100, 200, 250, 500, 750 50/1, 100/1, 250/5, 500/5 0.2, 0.4
Enoxacin 200, 400
Gemifloxacin 320
Levofloxacin 250, 500, 750 0.25, 0.5, 0.75
Lomefloxacin 400
Moxifloxacin 400 0.4
Nalidixic acid 250, 500, 1000 50/1, 250/5
Norfloxacin 100, 400
Ofloxacin 100, 200, 300, 400 0.1, 0.2, 0.4
Pazufloxacin 0.5
Pefloxacin 400 0.4
Pipemidic acid 250
Rosoxacin 150
Rufloxacin 200
Sitafloxacin 50
Sparfloxacin 200
Urinary Anti-infectives
Fosfomycin 3000
Methenamine mandelate 250, 500, 1000 250/5, 500/5
Nitrofurantoin 25, 50, 100 25/5
TABLE 54-12 Antimycobacterial Dosage Forms

FORMULATIONS
Oral
Aminosalicylic acid 4000
Capreomycin 1
Clofazimine 50, 100
Cycloserine 250
Ethambutol 100, 400
Ethionamide 125, 250
Isoniazid 50, 100, 300 10/1, 50/5 0.1
Continued
650
TABLE 54-12 Antimycobacterial Dosage Forms—cont’d

FORMULATIONS
Oral
Pyrazinamide 500
Rifabutin 150
Rifampin 150, 300, 450, 600 100/5 0.6
Rifapentine 150
Streptomycin 1
TABLE 54-13 Antifungal Dosage Forms

FORMULATIONS
Oral
Amphotericin B 10, 100 100/1 0.05
Amphotericin B cholesteryl sulfate complex 0.05, 0.1
Amphotericin B lipid complex 0.1
Amphotericin B liposomal 0.05
Anidulafungin 0.05, 0.1
Caspofungin 0.05, 0.07
Clotrimazole 10, 100,* 200,* 500*
Econazole 50,* 150*
Fluconazole 50, 100, 150, 200 10/1, 40/1, 50/5, 200/5 0.2, 0.4
Flucytosine 200, 250, 500 2.5
Griseofulvin 125, 165, 250, 330, 500 125/5
Itraconazole 100 10/1 0.25
Ketoconazole 200, 400* 20/1, 100/5
Micafungin 0.05, 0.1
Miconazole 100,* 200,* 250, 400* 0.01
Nystatin 100,000 U, 100,000 U,* 200,000 U, 500,000 U 100,000 U/1, 500,000 U/5
Posaconazole 40/1
Terbinafine 125, 250
Terconazole 80,* 240*
Tinidazole 250, 500
Voriconazole 50, 200 0.2
*Vaginal tablet, ovule, suppository form.
TABLE 54-14 Antiparasitic Dosage Forms

FORMULATIONS
Oral
Albendazole 200
Artemether/lumefantrine 20/120
Artesunate 0.11
Atovaquone 750/5
Atovaquone/proguanil 250/100, 62.5/25
Bithionol 200
Chloroquine phosphate 150, 300
Diethylcarbamazine 50, 200, 400
Diloxanide furoate 500
Furazolidone 100
Halofantrine 250
Hydroxychloroquine sulfate 155
Iodoquinol 210, 650
Ivermectin 3
Mebendazole 100
Mefloquine 250
Meglumine antimonate 0.085
Melarsoprol 900
Niclosamide 500
651
TABLE 54-14 Antiparasitic Dosage Forms—cont’d

FORMULATIONS

Oral
Nifurtimox 30, 120
Nitazoxanide 500 100/5
Paromomycin sulfate 250
Pentamidine isethionate 0.3
Piperazine citrate 250
Praziquantel 600
Primaquine 7.5, 15
Proguanil 100
Pyrantel pamoate 62.5 250/5
Pyrimethamine 25
Quinine sulfate 324
Sodium stibogluconate 10
Suramin 1
Thiabendazole 500/5
Tinidazole 250
Trimetrexate glucuronate 0.2
TABLE 54-15 Antiviral Dosage Forms*

FORMULATIONS
Oral
Acyclovir 200, 400, 800 200/5 0.1, 0.5, 1
Adefovir 10
Amantadine 50, 100 50/5
Boceprevir 200
Cidofovir 0.375
Entecavir 0.5, 1 0.05/1
Famciclovir 125, 250, 500
Foscarnet 6, 12
Ganciclovir 250, 500 0.5
Interferon alfa-2a 3 MIU, 4.5 MIU, 6 MIU, 9 MIU, 18 MIU, 36 MIU
Interferon alfa-2b 1 MIU, 3 MIU, 3.5 MIU, 5 MIU, 10 MIU, 18 MIU, 30 MIU, 35 MIU, 50 MIU
Interferon alfacon-1 9 µg, 15 µg, 30 µg
Interferon alfa-n3 5 MIU
Oseltamivir 75 12/1
Palivizumab 0.1
Peginterferon alfa-2a 180 µg
Peginterferon alfa-2b 74 µg, 118.4 µg, 177.6 µg, 222 µg
Peginterferon alfa-2b/ribavirin 50 µg/200 mg, 80 µg/200 mg, 100 µg/200 mg, 120 µg/200 mg, 150 µg/200 mg
Ribavirin 200, 400, 500, 600 40/1 6†
Rimantadine 100, 200, 400 50/5
Telaprevir 375
Telbivudine 600
Valacyclovir 500, 1000
Valganciclovir 450 50/1
Zanamivir 5†
*Not including antiretrovirals, which are listed in Table 54-16.
†
Powder for oral inhalation.
652
TABLE 54-16 Antiretroviral Dosage Forms

FORMULATIONS
Oral
Abacavir 300 20/1
Abacavir/lamivudine 600/300
Abacavir/lamivudine/zidovudine 300/150/300
Darunavir 300, 600
Delavirdine 100, 200
Didanosine 25, 50, 100, 125,* 150, 200, 200,* 250,* 400* 10/1
Dolutegravir 50
Efavirenz 50, 200, 600
Efavirenz/emtricitabine/tenofovir 600/200/300
Elvitegravir/cobicistat/emtricitabine/tenofovir 150/150/200/300
Emtricitabine 200 10/1
Emtricitabine/tenofovir 200/300
Emtricitabine/rilpivirine/tenofovir 200/25/300
Enfuvirtide 0.09
Etravirine 100
Fosamprenavir 700 50/1
Indinavir 100, 200, 333, 400
Lamivudine 150, 300 10/1
Lopinavir/ritonavir 100/25, 200/50 80/20/1
Maraviroc 150, 300
Nelfinavir 250, 625 50 mg/g†
Nevirapine 200 50/5
Raltegravir 400
Rilpivirine 25
Ritonavir 100 80/1
Saquinavir 200
Stavudine 15, 20, 30, 40 1/1
Tenofovir 300
Tipranavir 250
Zidovudine 100, 300 50/5 0.2
*Extended release.
†
Oral 50 mg/g off-white powder containing 50 mg (as nelfinavir free base) in each level scoopful (1 g).
TABLE 54-17 Anti-infective Agent Pharmacology: Penicillins
DOSAGE RECOMMENDATIONS
SERUM AND URINE Newborn

CONCENTRATION— (Parenteral):
SELECTED DOSES Adults Children: Dose/Interval Dose/Interval
Peak or Dose (g)/Interval Serious

DRUG (ORAL Peak Range, Infection
ABSORPTION, Serum Urine Daily Dose
%) Dose (g) (µg/mL) (µg/mL) Oral Parenteral (g) Oral Parenteral Up to 1 wk 1-4 wk
Amdinocillin 10 mg/kg 50 1260 10 mg/kg 10 mg/kg q4-6h
q4-6h (not approved)
Amoxicillin1 (74-92) 0.25 PO2 3.5-5 0.25-2 q8h 4 20-90 mg/kg/day
0.5 PO2 5.5-11 in 3 doses3
Amoxicillin/ 0.25 PO 3.7-4.8 381 0.25-2 4 20-90 mg/kg/day
clavulanate 0.5 PO 6-9.7 q8-12h in 3 doses4
0.875 PO 11.6
Ampicillin1 (30-55) 0.25 PO2 1.8-2.9 0.25-0.5 0.5-2 q4-6h 4 PO, 12 IV 6.25-255 mg/kg 6.25-25 mg/kg 25 mg/kg q12h 25 mg/kg q8h
0.5 PO2 3-6 q6h q6h q6h6
2 IV 47.6
Ampicillin/sulbactam 1.5 IV 40-71 1.5-3 q6h 12 25-50 mg/kg q6h
3 IV 109-150
Azlocillin (minimal) 2 IV7 165 2200-8100 2-4 q4-6h 24 75 mg/kg q6h
3 IV7 214 (not approved)6
9
Bacampicillin 0.4 PO 5.8-8.3 0.4-1.6 3.2 12.5-25 mg/kg
(80-98) 0.8 PO 12.0-15.9 q12h q12h
1.6 PO 18.6-20.1
653
was developed as a tool to predict mortality during surgery and the height-based dosing. As an example, if an anti-infective dose is
necessity for liver transplantation. Newer scoring systems such as the approved as 10 mg/kg/day in an adult, then the dose will be 600 mg
Model for End-Stage Liver Disease (MELD) have been developed as (60 kg) and 1200 mg (120 kg) if dosed on total body weight. If the
prognostic tools. However, these categorical estimates have limited 60-kg and 120-kg adults are male and 69 inches (175 cm) in height,

clinical validity when considering dose modification. Many anti- then the ideal body weight is 70.7 kg and both individuals would
infective agents have a high therapeutic-to-toxic ratio and thus, dosage receive the same dose of 707 mg if dosed on ideal body weight. In
adjustment in hepatic impairment is not necessary, even in the face of contrast, the lean body weight would be 51.1 kg and 73.5 kg in the
impaired body clearance. In circumstances where narrow therapeutic- 60-kg and 120-kg adults, respectively. So the doses would be 511 and
to-toxic ratios are seen, clinical judgment and appropriate treatment 735 mg (1.4-fold difference) across this twofold difference in total body
of infection should take precedence in drug dosing. weight. If the anti-infective had been approved as 12 mg/kg/day on the
basis of lean body weight, the dose would be 613 mg and 882 mg in
DOSAGE ADJUSTMENT FOR BODY the 60- and 120-kg individuals. This last solution meets empirical
SIZE (OBESE AND UNDERWEIGHT) observations that drug clearance typically increases by approximately
The dosage of drugs in adults is often based on a fixed dose (no regard 50% across this twofold weight distribution. Unfortunately, early-phase
to body size), weight, or body surface area (height and weight metric). clinical trials that define the dose for evaluation in phase 3 trials often
Several anti-infective agents have traditionally been dosed on the basis exclude obese and underweight subjects. So this narrow weight distri-
of body weight (mg/kg). Although this approach may be reasonable bution in early-phase trials limits our ability to define drug-specific
during maturation (birth to 2 years of age), the reliability of this body dose extrapolation for body size. Regrettably, consensus on a universal
size metric has been called into question because drug clearance mech- approach to dose extrapolation has not been reached and so specific
anisms do not increase proportionately with weight (>2 years of age). guidance for anti-infective dosing in the obese and the underweight
The underlying mathematical assumptions and dosing errors that may should be sought on a drug-by-drug basis.
occur as a consequence of using weight or an alternate body size
descriptor have been recently reviewed. In general, computing main- DRUG-DRUG INTERACTIONS
tenance anti-infective doses on total body weight has the potential to Drug-drug interactions are categorized into pharmacodynamic and
overdose (obese) and underdose (underweight) individuals at the pharmacokinetic interactions. Many interactions deemed pharmaco-
extremes of the weight distribution. Over time, several alternate body dynamic are really the exposure-response effects of a pharmacokinetic
size descriptors such as body surface area, ideal body weight, adjusted interaction leading to greater pharmacologic effect. These pharmaco-
body weight, and lean body weight have been developed to fix this dynamic interactions are often exploited in anti-infective therapy; thus,
dosing problem. Adjusted body weight and lean body weight are math- combination therapy results in synergy. Quantitation of pharmacody-
ematically similar to body surface area as metrics for dosing adults. namic interactions is at best difficult.
In contrast, ideal body weight is computed by sex using height only Pharmacokinetic interactions are somewhat more “predictable” but
and so using this body size descriptor is conceptually equivalent to still show large variability in the population.
Text continued on p. 707
STANDARD DOSE WITH DOSING

SERUM HALF-LIFE (hr) INTERVALS IN RENAL IMPAIRMENT
With
Normal
and Anuric
CrCl
Values With Dosage with
(mL/min) Dialysis For CrCl Ranges (mL/min) Dialysis Body Fluid Concentrations
Newborn Breast
During Serum/ Milk/ Aqueous
USUAL PD CSF/ Maternal Maternal Bile/ Humor/
ADULT <10 (daily Serum Serum Serum Serum Serum
>80 <10 HD PD DOSE >80 80-50 50-10 (anuric) After a dose) (%)b (%) (%) (%) (%)
0.8-1 3.4-5.6 1.8 10 mg/kg 4 4 6-8 8 10 mg/kg 400
0.7-1.4 7.4-21 0.25-0.5 8 8 8-12 12-16 0.25-0.5 5-10 25-33 5 100- Negligible
3000
1.1-1.3 7.5 0.25-2.0 8-12 8-12 0.25- 0.25-0.5 0.25-0.5 0.25 6 Low 1100
0.5 q24h q12h
q12h
0.7-1.4 7.4-21 0.5-2 4-6 4-6 8 12 0.5-2 1-4 100 11 100- 2-8
3000
1 9 1.5-3.0 6-8 6-8 8-12 24
1 5 1.5-2.6 2-4 4-6 4-6 8 12 3 13.38
0.7-1.4 7.4-21 0.4-1.6 12 12 12 65-75 1.7-3.6 17
Continued
654
TABLE 54-17 Anti-infective Agent Pharmacology: Penicillins—cont’d

CONCENTRATION— (Parenteral):

ABSORPTION, Serum Urine Daily Dose
%) Dose (g) (µg/mL) (µg/mL) Oral Parenteral (g) Oral Parenteral Up to 1 wk 1-4 wk
Carbenicillin 1 IV 45-71 1000 5-6 q4h 30 25-100 mg/kg 66.7-100 mg/ 400 mg/kg/day
3 IV10 278 4165 q4-6h kg q8h q6-8h
11
Carbenicillin indanyl 0.382 PO 6.5 0.576-1.13 0.382-0.764 3
sodium (30-40) q6h
Cloxacillin1 (37-60) 0.5 PO 6.9-15 0.25-1 q6h 2 12.5-25 mg/kg
q6h
Cyclacillin 0.25 PO 6-7 0.25-0.5 2 12.5-25 mg/kg
0.5 PO 11-12 q6h
1
Dicloxacillin (35-76) 0.5 PO 10-18 0.125-0.5 2 3.125-6.255 mg/
kg q6h
Flucloxacillin1 (50-70) 0.25 PO 6-9 0.25 q6h 0.25 q6h 8 62.5-125 mg 62.5-250 mg q6h
0.50 PO 11-20 q6h
Methicillin 1 IV10 59.8 1-2 q4-6h 12 25-100 mg/kg 25-50 mg/kg 25-50 mg/kg
1 IM 9-18 q4-6h12 q12h q8h
2 IM 13.8
Mezlocillin 1 IV10 64-143 4000 3-4 q4-6h 24 50-75 mg/kg q4h 75 mg/kg q12h 75 mg/kg
2 IV10 161-364 q6-8h13
5 IV10 199-597
Nafcillin1 (36) 1 PO 7.7 0.5-1 q6h 0.5-2 q4-6h 2 PO, 9 IV 12.5-25 mg/kg 12.5-25 mg/kg 25 mg/kg 25 mg/kg
1 IM 40 q6h5 q6h5 q8-12h14 q6-8h13
7.6
0.5 IV10
Oxacillin1 (30-35) 0.25 PO 1.65 0.5-1 q4-6h 0.5-2 q4-6h 4 PO, 12 IV 12.5-25 mg/kg 12.5-50 mg/kg 25-50 mg/kg 25-50 mg, kg
0.5 PO 2.6-3.9 q6h5 q8-12h14 q6-8h13
0.5 IV 52-63
q6h5
Penicillin G1 (15-30) 400,000 U PO 0.5 U/mL15 0.5-1 q6h 1-4 mU q4-6h 4 PO, 24 mU 25,000- 25,000- 50,000- 75,000-
2 mU q2h IV 20 IV 90,000 U/kg/ 400,000 U/kg/ 150,000 U/ 200,000 U/
day in 3-6 day q4-6h16 kg/day kg/day
doses q8-12h14 q6-8h13
Penicillin G 1.2 mU IM 0.15 U/mL 0.6-1.2 mU 2.4 mU 0.6 mU IM × 13 50,000 U/kg
benzathine IM × 1 IM × 1
Penicillin G procaine 0.6 mU IM 1.6 0.6-1.2 mU 4.8 mU 25,000-50,000 50,000 U/kg/
1.2 mU IM 1.95 IM q12h U/kg/day IM16 day IM
Penicillin V 0.25 PO 2.3-2.7 0.25-0.5 2 25,000-

potassium1 0.5 PO 4.9-6.3 q6h 100,000 U/kg/
(60-73) day in 3-6
doses
Piperacillin 2 IV10 4 IV10 159-615 8500 3-4 q4-6h 18 50 mg/kg q4h16
6 IV10 389-484 14,100
695-849
Piperacillin/ 3.375 IV7 209 3.375-4.5 13.5
tazobactam 4.5 IV7 224 q6-8h
Ticarcillin 1 IV10 70-100 650-250011 3 q4-6h 18 200-300 mg/kg/ 75 mg/kg 75 mg/kg q8h
2 IV10 200-218 day q4-6h5 q8-12h14 if <2 kg;
3 IV10 257 100 mg/kg
q8h if >2 kg
Ticarcillin/clavulanate 3.1 IV 324 1500 3.1 q4-8h 18.6 50 mg/kg q4-6h
1
Decreased rate or extent of absorption, or both, when given with food.
2
Fasting.
3
Children <20-27 kg.
4
Children <40 kg should not receive the 250-mg film-coated tablet.
5
Children <40-50 kg.
6
16.7-33.3 mg/kg q4h for meningitis.
7
Infusion over 15-30 min.
8
Mean concentration.
9
100% of bacampicillin is metabolized to ampicillin.
10
IV push (over 2-10 min).
11
Over 3 hr.
12
Depending on severity of infection.
13
q6h if >2 kg; q8h if <2 kg.
14
q8h if >2 kg; q12h if <2 kg.
15
Higher when given with probenecid.
16
Dosage should not exceed adult dosage.
a
Specified dose is supplemental to that after hemodialysis.
b
Inflamed meninges.
655


With
Normal
and Anuric
CrCl
Newborn Breast
>80 <10 HD PD DOSE >80 80-50 50-10 (anuric) After a dose) (%)b (%) (%) (%) (%)
0.78-1 9.4- 6 4.2-7.4 5-6 4 4 2-3 q6h Avoid 0.75-2 2 q6-12h 9.49 50-100 0.4 50-75 Up to 3
23.4
0.78-1 9.4-
23.4
0.4-0.8 0.8-2.3 0.5-1 6 6 6 6 Usual Usual
regimen regimen
0.25-0.5 6 6 12-24 24
0.6-0.8 1-2.2 1-2.2 1-2.2 0.125-0.5 6 6 6 6 Usual Usual Minimal 0-10 5-8
regimen regimen
0.75- 0.75- 0.75-1.5 0.75- 0.25 6-8 6-8 6-8 6-8 Usual Usual
1.5 1.5 1.5 regimen regimen
0.4-0.5 4-6 4-6 4-6 1-2 4-6 4-6 8 12 10 50-100 ≥100 Negligible
0.71- 1.6-14 1.6-14 3-4 4-6 4-6 8 2 g q8h 2-3 3 g q8h 1.2- 70-500 Low 1000
1.3 11.79
0.5-1.5 1.8-2.8 1.8-2.8 1.8-2.8 0.5-2 4-6 4-6 4-6 4-6 Usual Usual 9-20 10-15 ≥100 Negligible
regimen regimen
0.3-0.8 0.5-2 0.5-2 0.5-2 0.5-2 4-6 4-6 4-6 4-6 Usual Usual 10-15 ≤3.5 20-30 0
regimen regimen
0.4-0.9 6-20 6-20 1-4 mU 4-6 4-6 4-6 0.5-2 mU 500, 0-10 100 6 200-800
q4-6h 000 U
Days
24 Minimal
0.6-1.2 mU 12 12 12 12
0.5 7-10 0.25-0.5 6 6 6 6 0.25
0.6-1.3 2.1-6 2.1-6 3-4 4-6 4-6 8 12 1 g post, 1 3000-

then 6000
2 g q8h
0.7-1.1 1.9-3.5 2.5-4.5 6-8 6-8 >100
0.93- 13.5- 3 4-6 4-6 6-8 6-8 3 g post, 3 g q12h 39
1.3 16.2 then
2 g
q12h
1.1-1.5 8.5 3.1 4-6 4-6 2-3.1 g 2 g q12h 3.1 3.1 q12h Low
q6h
656
TABLE 54-18 Anti-infective Agent Pharmacology: Cephalosporins

SERUM
DOSAGE RECOMMENDATIONS HALF-LIFE (hr)
SERUM AND URINE Newborn With Normal and

CONCENTRATION— Children: Dose/ (Parenteral): Anuric CrCl
SELECTED DOSES Adults Interval Dose/Interval Values (mL/min)
Peak
or Dose (g)/Interval Serious
ABSORPTION, Dose Serum Urine Daily Up to
%) (g) (µg/mL) (µg/mL) Oral Parenteral Dose (g) Oral Parenteral 1 wk 1-4 wk >80 <10
First Generation
Cefadroxil (100) 0.5 PO 10-18 1800 0.5-1 2 30 mg/kg/ 1.1-2 20-25
1 PO 24-35 q12-24h day q12h
Cefazolin 1 IV 188 4000 0.5-2 q8h 6 25-100 mg/ 1.2-2.2 18-36
1 IM 64-76 kg/day
q6-8h
Cephalexin (100) 0.25 PO 9 2000 0.25-1 q6h 2 25-100 mg/ 0.5-1.2 5-30
kg/day in
4 doses
0.5 PO 15-18
Cephalothin 1 IM 15-21 2500 0.5-2 12 80-160 mg/ 0.5-0.9 3-8
kg/day q6h
1 IV 30
q4-6h
Cephapirin 1 IV 67 2560 0.5-2 q4-6h 12 40-80 mg/kg/ 0.6-0.9 2.4
day q6h
Cephradine1 (>90) 0.25 PO 9 1600 0.25-1 q6h 0.5-2 q4-6h 2 PO, 8 IV 25-100 mg/ 50-100 mg/ 0.7-2 8-15
kg/day kg/day q6h
q6h or
q12h
0.5 PO 15-18 3200
8 IV
1 IV 86
Second Generation
Cefaclor1 (>52) 0.25 PO 5-7 600 0.25-0.5 1.5 20-40 mg/ 0.5-1 2.8
q8h kg/day
q8h2
0.5 PO 13-15 900
Cefamandole 1 IV3 139 750 0.5-2 q4-8h 8 50-150 mg/ 0.5-2.1 12.3-18
2 IV3 214 1400 kg/day
3 IV3 534 q4-8h4
Cefmetazole 2 q6-12h 8 1.2
0.5-2 q24h
Cefonicid 7.5 mg/ 95-156 1020 3.5-5.8 50-60
kg IV3
2 3.5-5.8 50-60
0.5 IV 91
1 IV 221
Cefotetan 1 IV3 142-179.6 1400- 1-2 q12h 4 40-60 mg/kg/ 2.8-4.6 12-30
2000 day q12h
(not
approved)
2 IV3 237 3500-
4000
Cefoxitin 1 IM
22-24 3000 1-2 q6-8h 8 80-160 mg/ 0.7-1.1 13-22
kg/day
q4-8h5
1 IV3 110-125
2 IV3 221
Cefprozil (95) 0.25 PO 5.6-6.8 250 0.25-0.5 1 15 mg/kg 0.9-1.5 5.9
q12-24h q12h
0.5 PO 8.2-10.4 1000
1 PO 15.5-19.9 2900
Cefuroxime 0.5 PO 7 1150 0.125-0.5 0.75-1.5 q8h 1 PO, 4.5 IV 0.125-0.25 50-100 mg/ 10 mg/kg 1-2 20
(37-52)6 0.75 IV7 q12h q12h8 kg/day q12h (not
q6-8h9 approved)
51.1
Third Generation
Cefdinir1 (36) 0.2 PO 0.7-1.7 0.3-0.6 0.6 14 mg/kg/ 1.1-4.4
0.6 PO 2.4 q12-24h day
Cefditoren (14-16) 0.2 2.5-3 0.2-0.4 0.8 3-6 mg/kg 1.3-2 4.7
q12h q8h
0.4 4.4-4.6
657
STANDARD DOSE WITH DOSING INTERVALS IN

RENAL IMPAIRMENT

With
Dialysis For CrCl Ranges (mL/min) Dosage with Dialysis Body Fluid Concentrations
Newborn Breast
Serum/ Milk/ Aqueous
USUAL During CSF/ Maternal Maternal Bile/ Humor/
ADULT <10 PD (daily Serum Serum Serum Serum Serum
HD PD DOSE >80 80-50 50-10 (anuric) Aftera dose) (%)b (%) (%) (%) (%)
0.5-1 12-24 12-24 0.5 q12-24h 0.5 q36 0.5-1 50 0.9-1.9 22
0.5-2 8 8 0.5-1 q8-12h 0.5-1 0.25-0.5 1-4 35-69 3 29-300 <1.7

q18-24h
0.25-1 6 6 8-12 24-48 0.25-1 Minimal 60 2 216 11
0.5-2 4-6 4-6 1-1.5 q6h 0.5 q8h 0.5-2 ≤6 mg/L/ 1.2-5.6 16-41 22-172 4
dialysate
0.5-2 4-6 6 8 12 7.5-15 mg/kg 60 7

before, then
q12h postdialysis
0.25-1.0 6 6 0.5 q6h 0.25 q12h 0.25 before, 0.5 q6h ≤1 9-22 14-20 10-400 5-9
then 12 and
36-48 hr
later
0.25-0.5 8 8 8 8 0.25-0.5 2 ≥60 1-3
0.5-2 4-8 6 8 0.5-1 q12h 0.5-1 2 2.4 300-400 1.5
1-2 6-12 12 16-24 48
0.5-2 4-8 6 8 0.5-1 q12h 0.5-1 2 2.4 300-400 1.5
0.5-2 24 8-25 mg/ 4-15 mg/kg 3-15 mg/ None <1 <10 0.2

kg q24-48h kg q3-5
q24h day
1-2 12 12 24 48 25% 2.3 2-21

nondialysis
days, 50%
dialysis days
1-2 6-8 8-12 12-24 0.5-1 g 1-2 2.8 100 ≤3 280 4-7
q12-48h
0.25-0.5 12-24 12-24 50% q12-24h 50%

q12-24h
0.125-0.5 12 12 12 0.25 g 0.75 15 mg/kg 17-88 20-33 ≤3 35-80 10-14

PO q24h postdialysis
0.75-1.5 8 8 8-12 0.75 g

IV q24h
0.3-0.6 12-24
Continued
658
TABLE 54-18 Anti-infective Agent Pharmacology: Cephalosporins—cont’d

SERUM
SERUM AND URINE Newborn With Normal and

CONCENTRATION— Children: Dose/ (Parenteral): Anuric CrCl
SELECTED DOSES Adults Interval Dose/Interval Values (mL/min)
Peak
Cefixime1 (30-50) 0.4 PO 3.7 15.7-305 0.4 q24h 0.4 8 mg/kg/day 2.4-4 11.5
tabs 4.6 15.7-305 q24h
0.4 PO
susp
Cefoperazone 1 IV7 153 2200 1-2 q6-12h 12 25-100 mg/kg 25-100 mg/ 1.6-2.6 2-2.5
2 IV7 253 kg q12h
(not
approved)
Cefotaxime 0.5 IM 11.7-11.9 90-3261 0.5-2 q8-12h 12 50-200 mg/ 50 mg/kg 50 mg/kg 0.9-1.7
kg/day q12h q6-8h
q4-8h
1 IV3 102.4
2 IV3 214.1
Cefpodoxime11 0.1 PO 1.4 60 0.1-0.4 0.8 5 mg/kg 1.9-3.2 9.8
(50) q12h q12h12
0.2 PO 2.3
0.4 PO 3.9
Cefsulodin (85 IM) 1 IV 65 0.5-2 q6-8h 12 60-200 mg/ 1.6-1.9 13
kg/day in
3-4 doses
Ceftazidime14 0.5 IV7 42 1-2 q8-12h 6 25-50 mg/kg 30-50 mg/ 30 mg/kg 1.4-2 11.9-35
q8h kg q8h15 q8h
1 IV7 69
2 IV7 159-185.5
Ceftibuten (80) 0.4 PO 15 0.2-0.4 0.6 9 mg/kg/day 1.5-2.9 18-29
q12-24h
Ceftizoxime 1 IV7 84.4 >6000 1-3 q6-8h 12 33-50 mg/kg 1.4-1.8 25-35
q6-8h5
2 IV 131.8
3 IV 221.1
Ceftriaxone 1 IV7 123.2- 504-995 0.5-2 q12-24h 4 50-100 mg/ 50 mg/kg 50-75 mg/ 5.4-10.9 12.2-18.2
150.7 kg/day q24h kg q24h17
q12-24h
2 IV7 223-276
2 IV16 216-281
Moxalactam 1 IV7 60-100 2100 0.5-4 1218 50 mg/kg 50 mg/kg 50 mg/kg 2 20
q8-12h18 q6-8h18,19 q12h18,19 q8h18,19
3
2 IV 150-200 4200
Fourth Generation
Cefepime 1 IV 81.7 0.5-2 q8-12h 6 50 mg/kg 2 13.5
q8-12h
2 IV 163.9
Fifth Generation
Ceftobiprole 0.5 IV 34.2 0.5 q8h 1.5 3 3
Ceftaroline 0.6 21.3 0.6 q8h 1.8 1.6-2.7 6
1
2
Should not exceed 1 g.
3
IV push (over 2-10 min).
4
Dosage should not exceed adult dosage.
5
Should not exceed 12 g.
6
52% after food.
7
Infusion over 15-30 min.
8
0.125 g q12h for children <2 yr.
9
200-240 mg/kg/day q6-8h for meningitis.
10
Microbiologic activity in hepatic bile/microbiologic activity serum.
11
Should be given with food to increase absorption.
12
No more than 400 mg/day for otitis or 100 mg/day for pharyngitis, tonsillitis.
13
Creatinine clearance <30 mL/min.
14
Arginine component not approved for children <12 yr.
15
30-50 mg/kg q12h for <2 kg; 30 mg/kg q8h for >2 kg.
16
2g q24h at steady state.
I7
50 mg/kg/day for <2 kg; 50-75 mg/kg/day for >2 kg.
18
Bleeding time should be monitored in patients receiving more than 4 g/day for more than 3 days. Prophylactic vitamin K, 10 mg/wk, should be given to patients treated with moxalactam.
19
For gram-negative meningitis in children, the manufacturer recommends an initial loading dose of 100 mg/kg.
a
Specified dose is supplemental to that after hemodialysis.
b
Inflamed meninges.
659

RENAL IMPAIRMENT

With
Newborn Breast
7 0.2-0.4 12 12 0.2 q12-24h >100
0.4 24 24 0.3 q24h 48 None 15-50
1-2 6-12 6-12 6-12 6-12 Dose after 1.8-3.1 20-50 ≤1.5 800- 1-6
dialysis 1200
0.5-2 8-12 8-12 12-24 24 0.5-2 27 Up to 3-8 15-7510 0.5-4
2.1-2.6 8.9 0.1-0.4 12 12 2413 24 Usual dose 3 × 102-127

wk
16 0.5-2 6-8 6-8 0.25-1 q6-12h 0.5-2 q24h 60% of usual 1 q24h <10 Minimal
dose
1-2 8-12 8-12 12-24 0.5 g 1-g load, then 0.5 g q24h or 20-40 7 13-54 3-12
q24-48h 1 g 250 mg/2 L
postdialysis dialysate
0.2-0.4 12-24 12-24 24 0.1 q24h 0.4 0.2 q24h Negligible
1-3 6-8 0.5-1.5 g 0.25-1 q12h 0.5 q24h Dose 3 g q48h 22.5 28-33 1-6 34-82 3.6-6
q8h postdialysis
12.2- 12.2- 0.5-2 12-24 12-24 12-24 12-24 None 16-32 18-25 3-4 200-500
18.2 18.2
4 16.7 0.5-4 8-12 3 g q8h 2-3 g q12h 1 g 1-2 g 0.5 g q18-24h 4-55 30-40 2.7 152-224 1-16
q12-24h postdialysis
13.5 19 0.5-2 8-12 12-24 24 0.25-0.5 0.25 1-2 q48h 0.5 mg/1 L

q24h milk
0.5 8 8 0.25-0.5 q12h

0.6 12 12 0.3-0.4 q12h 0.2 q12h 0.2 q12h
660
TABLE 54-19 Anti-infective Agent Pharmacology: Miscellaneous β-Lactams

SERUM
HALF-LIFE
DOSAGE RECOMMENDATIONS (hr)

With
Normal
and
Anuric
SERUM AND URINE Newborn CrCl
CONCENTRATION— Children: (Parenteral): Values
SELECTED DOSES Adults Dose/Interval Dose/Interval (mL/min)
Peak
Aztreonam 1 IV2 90-164 3000- 1-2 q6h 6 30-50 mg/kg 30-50 mg/ 1.3-2.2 6-9
2 IV2 204-255 3500 q6-8h kg
5600- q8-12h
6600
Doripenem 0.5 IV 23 601 0.5 q8h 1.5 1
Ertapenem (90 1 IV2 155 1-2 q24h 2 4 14

IM)
Imipenem 0.25 14-24 50 0.5-1 q6h 2 15-25 mg/kg 25 mg/ 25 mg/kg 0.8-1 3.5
IV2 q6h kg q8h
q12h
0.5 IV2 21-58 100
1 IV2 41-83 >100
Loracarbef1 (90) 0.2 PO 8 0.20-0.40 0.8 15-30 mg/ 1 32
cap q12-24h kg/day
q12h
0.4 PO 14
cap
0.4 PO 17
ssp.
Meropenem 0.5 IV2 26 0.5-2 q8-12h 6 20-40 mg/kg 0.8-1 6-20
q8h
1 IV2 55-62
1
2
IV infusion over 15-30 min.
3
2.7 hr during dialysis, 7-9 hr between dialysis sessions.
a
Specified dose is supplemental to that in hemodialysis.
b
Inflamed meninges.
661

INTERVALS IN RENAL IMPAIRMENT
With
Newborn Breast
2.7 1-2 6 8-12 12-18 24 1/8 initial Usual 3-52 0.1-0.6 115-405 5-14
7.93 dose loading
postdialysis dose, then
1 usual
4
dose at
usual
interval
0.5 8 8 0.25 117
q8-12h
1-2 24 24 0.5-2 0.5 q24h 0.15 Minimal
q24h
0.5-1 6 0.5 g 0.5 g 0.25-0.5 g 0.25-0.5 1-10 Minimal 3
q6-8h q8-12h q12h post-HD
then q12h
4 0.2-0.4 12-24 12-24 24-48 3-5 days 0.2-0.4

post-HD
0.5-2 8-12 8-12 0.5-1 0.5 q24h 0.5 12 40

q12h
662
TABLE 54-20 Anti-infective Agent Pharmacology: Aminoglycosides

SERUM
HALF-LIFE

With
Normal
and
Anuric
SERUM AND URINE Newborn CrCl
CONCENTRATION— Children: (Parenteral): Values
SELECTED DOSES Adults Dose/Interval Dose/Interval (mL/min)
Peak
Amikacin1 0.500 38 832 15 mg/kg/day 15 mg/kg 15 mg/kg/day Not Not 2-3 30-86
IM q8-12h3 q8-12h3 approved approved
7.5 mg/
kg IV2
Gentamicin5 1 mg/kg 4-7.6 113-423 3-5 mg/kg/ 3-5 mg/kg 3-7.5 mg/kg/ 2.5 mg/kg 7.5 mg/kg/ 2-3 24-60
IM day q8h3 day q8h3 q12h3 day q8h3
1 mg/kg 4-7.6
IV6
Isepamicin 15 mg/ 51 8-15 mg/kg 15 mg/kg 7.5 mg/kg/24 7.5 mg/kg 2-2.5
kg IV2 q24h hr7 q12h7
1 IM 38
Kanamycin1 (1) 7.5 mg/ 22 15 mg/kg/day 1.5 15 mg/kg/day 15-20 mg/ 15 mg/kg/ 2-4 27-80
kg IM q8-12h3 q8-12h3 kg/day day
7.5 mg/ 22 q12h3,8 q8-12h3
kg IV2
Neomycin9 (3) 4 g PO 2.5-6.1 50 mg/ 3 PO 2-3 12-24
kg/day
q6h
Netilmicin10 2 mg/kg 16.6 4-6.5 mg/kg/ 3.9 mg/kg 3-7.5 mg/kg/ 4-6.5 mg/ 4-6.5 mg/ 2-2.5 30
IV2 day day kg/day kg/day
2 mg/kg 7 q8-12h3 q8-12h3 q12h3,8 q12h3,11
IM
Spectinomycin 2 g IM 100 2 g/day IM 2 Not approved Not Not 1.2-
approved approved 2.8
Streptomycin12 0.5 IM 5-12 400 0.5-1 g q12h 1 20-40 mg/kg/ 2-3 Up to
1 IM 25-50 ≥1000 day q6-12h 110
Tobramycin5 1 mg/kg 4-6 75-100 3-5 mg/kg/ 3-5 mg/kg 3-6 mg/kg/ 4 mg/kg/ 3-5 mg/kg/ 2-3 5-70
IM 4-6 day q8h3 day q8h3 day day q8h3
1 mg/kg q12h3
IV2
1
Desired concentrations: peak 15-30 µg/mL; trough <5-10 µg/mL.
2
Infused over 30-60 min.
3
The dosing strategy for aminoglycosides involves the use of ideal (lean) body weight (IBW) for dosage calculation. In obese patients, this approach would result in serum
aminoglycoside concentrations less than expected. Alternative dosing recommendations that account for the change in drug distribution volume with obesity have been
proposed: (1) IBW + 40% of excess weight, defined as total body weight (TBW) minus IBW (J Infect Dis. 1978;138:499-505); (2) IBW + 58% of excess weight (TBW – IBW)
(Clin Pharmacol Ther. 1979; 26:508); (3) IBW + 38% of excess weight (TBW – IBW) (Am J Hosp Pharm. 1980;37:519-522).
4
Dosing at creatinine clearance ≤10 mL/min should be assisted with serum concentrations.
5
Desired concentrations: peak, 4-10 µg/mL; trough, <2 µg/mL.
6
Infused over 2 hr.
7
q24h for infants <16 days old; q12h for ≥16 days old.
8
15  mg/kg/day q12h for ≤2 kg; 20 mg/kg/day q12h for >2 kg.
9
Parenteral administration of neomycin is no longer recommended.
10
Desired concentrations: peak 6-12 µg/mL; trough <2 µg/mL.
11
For premature or full-term infants <6 wk.
12
Desired concentrations: peak 5-25 µg/mL; trough <5 µg/mL.
a
b
Inflamed meninges.
663

With Dosage with

Dialysis For CrCl Ranges (mL/min) Dialysis Body Fluid Concentrations
Newborn Breast
4
5-7.5 mg/ 8 8-12 12-48 48 2.5- 2.5 mg/kg/ 15-24 20 30 Minimal
kg 3.75 mg/ day
kg
post-HD
1-1.7 mg/ 8 8-12 12-48 484 1.0-1.7 mg/ 1 mg/2 L 10-30 30-40 30-60 Minimal
kg kg dialysate
post-HD removed
8 mg/kg 24 24 48-72 96
7.5 mg/ 8-12 8-12 12-48 ≥484 4-5 mg/kg 3.75 mg/ 43 50 35 Minimal

kg post-HD kg/day
Minimal
2-2.2 mg/ 8 8-12 12-48 484 2 mg/kg 21-26 Minimal

kg post-HD
2 g 24 24 24 24 Minimal
0.5-1 12 7.5 mg/kg 7.5 mg/kg 7.5 mg/kg 0.5 g 20 10-40 <25 40-300 Minimal

q24h q24-72h q72-96h post-HD
1-1.7 mg/ 8 8-12 12-48 48 1 mg/kg 1 mg/2 L 14-23 50 10-20 18
kg post-HD dialysate
removed
664
TABLE 54-21 Anti-infective Agent Pharmacology: Tetracyclines1 and Glycyclines

SERUM
SERUM AND URINE Newborn With Normal

CONCENTRATION— Children: (Parenteral): and Anuric CrCl
SELECTED DOSES Adults Dose/Interval Dose/Interval Values (mL/min)
ABSORPTION, Dose Serum Urine Daily
%) (g) (µg/mL) (µg/mL) Oral Parenteral Dose (g) Oral Parenteral Up to 1 wk 1-4 wk >80 <10
Demeclocycline2 0.15 PO 0.9-1.2 0.6/day 0.6 6.6-13.2 mg/ Not 10-17 42-68
(60-80) q6-12h kg/day recommended
q6-12h
0.3 PO 1.5-1.7
Doxycycline 0.1 PO 1.5-2.1 0.1 q12h 0.1 q12h 0.2 2.2 mg/kg 2.2 mg/kg Not 14-24 18-30 18-30
(90-100) 0.1 IV3 2.5 q12-24h q12-24h recommended
Methacycline2 (58) 0.15 PO 1.3 0.15 q6h 1.2 6.6-13.2 mg/ Not 7-15 Up to
or 0.3 kg/day recommended 44
q12h q6-12h
0.3 PO 2.4
Minocycline 0.2 PO 2-3.5 0.1 q12h 0.1 q12h 0.2 2 mg/kg 2 mg/kg q12h Not 11-26 12-30
(90-100) q12h recommended
Oxytetracycline2 0.25 PO 1.3-1.4 1-2/day 0.25 IM q24h 2 25-50 mg/ 15-25 mg/kg/ Not 6-10 47-66
(60) q6h kg/day day recommended
q6h q8-12h4
0.5 PO 4-4.2
Tetracycline2 0.25 PO 1.5-2.2 0.25-0.5 2 25-50 mg/ Not 6-12 57-120
(75-80) q6h kg/day recommended
q6-12h
0.5 PO 3-4.3
0.5 PO5 2-5
Tigecycline 0.1 IV 1.45 0.1 load, then 0.1 Not 27-42 27-42 27-42
0.05 q12h recommended
1
The tetracyclines cause a brown discoloration of the teeth and may retard the growth of bone in the human fetus and children. The American Academy of Pediatrics recommends that tetracyclines be
used in children who are 9 yr of age or older.
2
All tetracyclines should be given 1 hr before or 2 hr after meals.
3
Infused over 60 min.
4
No more than 250 mg/day.
5
At steady state.
a
b
Inflamed meninges.
TABLE 54-22 Anti-infective Agent Pharmacology: Azalides, Macrolides, Ketolides, Lincosamides,

Chloramphenicol, and Metronidazole
SERUM AND URINE

CONCENTRATION— Newborn (Parenteral):

%) (g) (µg/mL) (µg/mL) Oral Parenteral Dose (g) Oral Parenteral 1 wk 1-4 wk
Azithromycin1 0.5 PO 0.09-0.44 8.64-26.8 0.5 q24h × 3 0.5 q24h 0.5 IV 5-12 mg/kg/day 10-12 mg/kg/
(35-40) days day2
0.5 IV 3.63
0.3 PO 0.5
Clarithromycin 0.25 PO3 1 0.25-0.5 q12h 1 7.5 mg/kg q12h
(50-55)
3
0.5 PO 2-3
0.5 PO3 14
Dirithromycin5 (6-14)
0.5 PO 0.3-0.4 Minimal 0.5 q24h 0.5 0.5 q24h6
Erythromycin base7,8 0.25 PO 0.1-2 0.25-0.5 q6h 2 30-50 mg/kg/day

q6h
Erythromycin 0.25 PO 0.1-2 0.25-0.5 q6h 2 30-50 mg/kg/day
stearate8 q6h
Erythromycin ethyl 0.4 PO 0.1-2 0.4 q6h 2 30-50 mg/kg/day
succinate8 q6h
665
STANDARD DOSE WITH DOSING INTERVALS IN RENAL

IMPAIRMENT

With Dosage with
Newborn Breast Aqueous
USUAL During CSF/ Serum/ Milk/ Bile/ Humor/
ADULT <10 PD (daily Serum Maternal Maternal Serum Serum
HD PD DOSE >80 80-50 50-10 (anuric) Aftera dose) (%)b Serum (%) Serum (%) (%) (%)
0.15-0.3 6-12 Not Minimal 70 200-3200 10-30
recommended
0.1 12 12 12 12 0.1 g 0.1 g 26 30-40 200-3200 10-13

q12h q12h
0.15-0.3 6-12 Not
recommended
0.1 12 12 12 12 0.1 g 0.1 g 77 8-26 200-3200 17

q12h q12h
0.25-0.5 6 6 Use doxycycline Minimal 20-140 200-3200
PO 24 24
0.25 IM
0.25-0.5 6 6 Use doxycycline 7 60-70 25-150 200-3200 9-11
0.1 load, 12 12 12 12 12 >100

then
0.05

With Normal
and Anuric
CrCl Values With Dosage with
Newborn Breast
>80 <10 HD PD DOSE >80 80-50 50-10 (anuric) Aftera dose) (%)b (%) (%) (%) (%)
68 68 68 68 0.5 24 24 24 24 24 24 >100
5-7 0.25-0.5 12 12 12-24 24 Minimal 30 7000
20-50 20-50 20-50 0.5 24 24 24 24 Usual Usual

regimen regimen
1.5-2 6 0.25-0.5 6 6 6 6 Usual Usual 2-13 5-20 50
regimen regimen
1.5-2 6 0.25-0.5 6 6 6 6 Usual Usual 2-13 5-20 50
regimen regimen
1.5-2 6 0.4 6 6 6 6 Usual Usual 2-13 5-20 50
regimen regimen
Continued
666
TABLE 54-22 Anti-infective Agent Pharmacology: Azalides, Macrolides, Ketolides, Lincosamides,

Chloramphenicol, and Metronidazole—cont’d
SERUM AND URINE

CONCENTRATION— Newborn (Parenteral):

Erythromycin 0.2 IV 3-4 0.5-1 q6h 4 15-20 mg/kg/
lactobionate9, 10 day q6h
Erythromycin 0.2 IV 3-4 15-20 mg/kg/ 4 15-20 mg/kg/
gluceptate9 day q6h day q6h
11
Erythromycin 0.25 PO 0.1-2 0.25-0.5 q6h 2 30-50 mg/kg/day
estolate8 q6h
Fidaxomycin 0.2 PO 0.0052 0.2 q12h
Josamycin (>90) 0.5 PO 0.65 200-400 0.5-1 q8-12h 3 30-75 mg/kg/day
0.5 PO3 1.64 q6-12h
Roxithromycin 0.15 PO 6 0.15-0.3 0.3 5-7.5 mg/kg/day
q12-24h q12h
0.3 PO 10
Spiramycin (33-40) 1 PO 0.96 1 q6-12h 4-5
2 PO 1.65
0.5 IV 2.28
Telithromycin 0.8 PO 1.4-2.4 0.8 q24h 0.8
Clindamycin7 (90) 0.15 PO 1.9-3.9 0.15-0.3 q6h 0.3-0.9 q6-8h 1.2 PO, 2.7 8-25 mg/kg/day 15-40 mg/kg/ 15 mg/kg/day 15-20 mg/kg/day q6-8h13
IV q6-8h day q6-8h q6-8h13
0.6 IV12 10
Lincomycin7 (20-30) 0.5 PO 1.8-5.3 0.5 q6-8h 0.6-1 q8-12h 8 30-60 mg/kg/day 10-20 mg/kg/ Not indicated
q6-8h day q8-12h
0.6 IM
9.3-18.5
0.6 IV14 15.9-20.9
Chloramphenicol15 1 PO 11 0.25-0.75 q6h 0.25-1 q6h 4 50-100 mg/kg/ 50-100 mg/ 25 mg/kg/day 50 mg/kg/day q12-24h17
(75-90) day q6h kg/day q6h q24h16
1 PO3 18
1 IV 4.9-12
Metronidazole7 (80) 0.25 PO 4.6-6.5 0.25-0.75 q8h 0.5 q6h 30 mg/kg
7.5 mg/kg3 26
Tinidazole (~100) 2 PO 47.7 1-2 q24h 2 50 mg/kg/day
1
Decreased extent of absorption of capsule formulation only when given with food.
2
No studies to support; extrapolated from adult conversion.
3
At steady state.
4
Of 14-hydroxyclarithromycin (active metabolite).
5
Must be given with food.
6
Not approved for children <12 yr of age.
7
Denotes decreased rate or extent of absorption, or both, when given with food.
8
Erythromycin and its derivatives have varying degrees of bioavailability (18%-45%).
9
Oral erythromycin therapy should replace IV therapy as soon as possible.
10
Because of local irritative effects, the drug must not be administered rapidly by direct IV injection (IV push).
11
Higher serum concentrations have been reported in patients taking erythromycin estolate versus other derivatives.
12
Over 20 min.
13
When IV clindamycin is given to neonates and infants, organ system functions should be monitored.
14
When given over 2 hr.
15
Chloramphenicol dosage should be administered to maintain plasma concentrations of 10-25 mg/L for peak and 5-10 mg/L for trough.
16
<2 wk.
17
>2 wk.
a
b
Inflamed meninges.
667

With Normal
and Anuric
Newborn Breast
1.5-2 6 0.5-1 6 6 6 6 Usual Usual 2-13 5-20 50
regimen regimen
1.5-2 6 15-20 mg/kg/ 6 6 6 6 Usual Usual 2-13 5-20 50
day regimen regimen
1.5-2 6 0.25-0.5 6 6 6 6 Usual Usual 2-13 5-20 50
regimen regimen
11 11 11 11 0.2 12 12 12 12 12 12
0.9-2 0.5-1 6-12 6-12
12 ~12 0.15-0.3 12-24 12-24 12-24 24-48 30-40 0.05 50-200
5-6 0.5-1 6-12 >100
10-13 0.8 24 24 24
2-3 2-3.5 0.15-0.3 PO 6 6 6 6 Usual Usual Minimal 46 38-50 250-300
0.3-0.9 IV 6-8 6-8 6-8 6-8 regimen regimen
4-6.4 10 0.5 PO 6-8 6-8 6-8 24 18 25 13 250-400 8.75

0.6-1 IV 8-12 8-12 8-12 24-36
1.5-4.1 3-7 3-7 0.25-0.75 PO 6 6 6 6 Schedule Usual 45-89 30-80 100 100 33-50
0.25-1 IV 6 6 6 6 dose regimen
post-HD
6-14 8-15 8-15 0.25-0.75 PO 8 8 8 8 Usual Usual ≥100 97 100

0.5 IV 6 6 6 6 regimen regimen
12-14 12-14 4.9 1-2 PO 24 24 24 24 Schedule
dose
post-HD
668
TABLE 54-23 Anti-infective Agent Pharmacology: Miscellaneous Gram-Positive Agents and Polymyxins,
Fusidic Acid
SERUM AND URINE

CONCENTRATION—SELECTED Children:
DOSES Adults Dose/Interval Newborn (Parenteral): Dose/Interval

ABSORPTION, Serum Urine Daily
%) Dose (g) (µg/mL) (µg/mL) Oral Parenteral Dose (g) Oral Parenteral Up to 1 wk 1-4 wk
Colistimethate1 0.15 IM 5-7.5 200-270 2.5-5 mg/kg/ 5 mg/kg1 5-15 mg/ 2.5-5 mg/kg/ Not
day q6-12h1 kg/day day q6-12h recommended
q8h2
Polymyxin B3 20,000- 1-8 15,000- 25,000 U/ 15,000- Not
40,000 U/ 25,000 U/kg/ kg/day 25,000 U/ recommended
kg/IM day q12h q12h kg/day
q12h
Vancomycin 1 IV 25 0.5-2 g/ 1g q12h 1 PO/2 IV 40 mg/kg/ 40 mg/kg/day 15-mg/kg load, 10 mg/kg q8h
(minimal) day day q6-12h then 10 mg/
q6-8h q6-8h5 kg q12h
Teicoplanin 3 mg/kg IV6 53 0.2-0.4 q24h 10 mg/kg 6 mg/kg q24h 6 mg/kg q24h (preliminary)
q24h (preliminary)
6 mg/kg IV6 112
Fusidic acid 0.5 PO 14-387 <1 0.5-1 0.58 q8h8 6.6- 6.6 mg/kg
q8h 16.6 mg/ q8-12h
kg q8h
Quinupristin- 7 mg/kg IV 5 7.5 mg/kg 22.5 mg/kg/ 7.5 mg/kg
dalfopristin q8-12h day q8h
Evernimicin 6 mg/kg IV 49-55 1-12 mg/kg/

day9
Linezolid (100) 0.4 PO 8.1 0.4-0.6 0.4-0.6 q12h 1.2 10 mg/kg 10 mg/kg q8h 10 mg/kg q8h 10 mg/kg q8h
q12h q8h
0.6 PO 12.7
0.6 IV 15.1
Dalbavancin 1 day 1, 0.5 325 1 on day 1, 0.5 1
day 8 IV day 8
Daptomycin 4 mg/kg IV 57.8 4-6 mg/kg 6 mg/kg10
q24h
6 mg/kg IV 93.9
Oritavancin 3 mg/kg IV 31
Telavancin 7.5 mg/kg IV 87.5 10 mg/kg q24h 10 mg/kg
15 mg/kg IV 186
1
Colistimethate is the sulfamethyl derivative of colistin and the doses are based on colistin base activity. This agent should be used in combination treatment regimens, when applied against
multidrug-resistant gram-negative pathogens. Although 300 mg/day is considered to be the maximum daily dose, doses up to 480 mg/day (colistin base activity) may be necessary but are likely to also
increase the risk for toxicity.
2
Colistin is absorbed to some extent in infants.
3
Bioavailability can be 10% in infants.
4
Although recommendations to reduce the polymyxin B dose to 7500-12,500 U/kg/day q12h for patients with a creatinine clearance 5-20 mL/min exist, recent data suggest that no dosage
adjustment is required on the basis of renal function.
5
Not to exceed 2 g/day.
6
5-min infusion.
7
Accumulation occurs with multiple doses of 0.5 g given q8h; a mean serum concentration of 71 µg/mL has been reported after 96 hr of therapy.
8
Diethanolamine fusidate, 580 mg = 500 mg sodium fusidate.
9
Based on early phase I studies.
10
Some experts recommend the use of daptomycin 8-10 mg/kg in patients with infective endocarditis, persistent MRSA bacteremia, or vancomycin treatment failures in adults. Alternatively, an
empiric fixed daily dose of 750 mg may be optimal in critically ill patients, whereas doses >1000 mg/day are likely to increase the probability of skeletal muscle toxicity without significantly increasing
the probability of effect.
a
b
Inflamed meninges.
669
STANDARD DOSE WITH DOSING INTERVALS

SERUM HALF-LIFE (hr) IN RENAL IMPAIRMENT
With
Normal and
Anuric CrCl
Newborn Breast
1.5-8 48-72 2.5-5 mg/ 6-12 2.5-3.8 mg/ 2.5 mg/kg/ 1.5 mg/kg Minimal 50 18 25-30
kg/day kg/day day q36h
IV q12-24h q12-24h
4.3-6 48-72 15,000- 12 124 124 2250- Minimal
25,000  3750 U/
U/kg/ kg/day
day q12h
4-6 44.1- 15 mg/kg 12 See Matzke et al 1984 1 g/wk 0.5-1 g/ 7.21 50 Minimal
406.4 wk
40-70 125 163 0.4 g 24 48 48 72
1.3- 0.5-1 PO 8 8 8 8
1.5
8.6 7.5 mg/kg 8-12 8-12 8-12 8-12 10-20 mg/

kg/day
q12h
1-12 mg/ 24 24
kg9
5.5 0.4-0.6 g 12 12 12 12 30% of 20
dose
>150
9.4 27.8 29.8 4-6 mg/kg 24 24 24-48 48 4-6 mg/kg 4-6 mg/kg

q48h q48h
≈200
6-7.5 10 mg/kg 24 24
670
TABLE 54-24 Anti-infective Agent Pharmacology: Sulfonamides and Trimethoprim
SERUM AND URINE

CONCENTRATION—SELECTED Newborn (Parenteral):
DOSES Adults Children: Dose/Interval Dose/Interval

ABSORPTION, Serum Urine Daily
%) Dose (g) (µg/mL) (µg/mL) Oral Parenteral Dose (g) Oral Parenteral Up to 1 wk 1-4 wk
Trimethoprim/ 0.16/0.8 PO 1-2/40-602 0.16/0.8 q12-24h 3-5 mg/kg 1.2 IV3 6-12 mg/kg/day 6-12 mg/kg/ Not recommended 8-15/7-12
sulfamethoxazole1 0.16/0.8 IV 9/1052 q6-8h3 q6-12h3 day
(85-90) q6-12h3
Trimethoprim (80) 0.1 PO 1 30-60 0.1 q12h 0.2 4 mg/kg/day q12h6 8-15 24
0.2 PO 2
Sulfisoxazole1 2-4 PO 11.2-25 0.5-1 q6h 25 mg/kg q6h 4 120-150 mg/kg/day Not recommended 3-7
(70-90) 2-4 IM 11.2-25 q4-6h
Sulfamethoxazole1 2 PO 50-120 1 q8-12h 2 50-60 mg/kg/day Not recommended 7-12
(70-90) q12h
Sulfamethizole1 2 PO 60 0.5-1 q6-8h 6 30-45 mg/kg/day q6h Not recommended 4-8
(70-90)
1
Sulfadiazine (70-90) 3 PO 50 2-4 g/day q4-8h 4 120-150 mg/kg/day 100 mg/kg/ Not recommended 17
q4-6h day q6-8h
Dapsone 0.2 PO 0.1-72 0.05-0.1 q24h 0.1 1-2 mg/kg/day q24h 20-30
1
2
At steady state.
3
Based on the trimethoprim component.
4
Uninflamed meninges.
5
Amniotic fluid concentrations (µg/mL).
6
Not approved for children <12 yr.
a
b
Inflamed meninges.
TABLE 54-25 Anti-infective Agent Pharmacology: Quinolones and Urinary Anti-infectives

SERUM
HALF-LIFE
With Normal
SERUM AND URINE Newborn and Anuric
CONCENTRATION—SELECTED Children: (Parenteral): CrCl Values
DOSES Adults Dose/Interval Dose/Interval (mL/min)

ABSORPTION, Dose Serum Urine Daily 1-4 
%) (g) (µg/mL) (µg/mL) Oral Parenteral Dose (g) Oral Parenteral Up to 1 wk wk >80 <10
Cinoxacin (97) 0.25 PO 8 400 0.25 q6h 0.5 q12h2 1 1.5 8.4
0.5 PO 16 or
Ciprofloxacin1 0.5 PO 1.6-2.9 350 0.25-0.75 0.2-0.4 1.5 PO, 1.2 25 mg/kg/ 3.2-12.5 mg/ 3-5 5-10
(50-85) 0.75 PO 2.5-4.3 q12h q8-12h IV day q12h kg/day
0.4 IV5 4.6 q12h
Enoxacin1 (80-90) 0.4 PO 2.8-3.6 250-300 0.4 q12h 0.4 q12h 0.8 5-7 40
0.6 PO 4 337
0.2 IV 1.8
Garenoxacin1 0.4 PO 5.9 0.4-0.6 0.6 14
q24h
Gemifloxacin 0.32 PO 1.48 0.32 q24h 0.32 6.65
Levofloxacin (99) 0.5 PO 5.7 0.25-0.75 0.25-0.75 1 6-8
0.5 IV5 6.2 q24h q24h
0.75 PO 7.1
Lomefloxacin 0.2 PO 2.1 170 0.4 q24h 0.4 7-8.5 21
(>95) 0.4 PO 3-4.7
Moxifloxacin (90) 0.4 PO 3.1 0.4 q24h 0.4 q24h 0.4 9-16
0.4 IV 3.9
1
Nalidixic acid 1 PO 20-40 1q6h 4 1.1-2.5 21
(100)
Norfloxacin1 0.4 PO 1.3-1.9 ≥200 0.4 q12h 0.8 2.3-4 7.6
(30-50)
Ofloxacin1 0.4 PO 2.9-5.6 200 0.2-0.4 0.2-0.4 q12h 0.8 4-8 16.9- 8-12/
(85-100) 0.2 PO 1.5-2.7 q12h 28.4 13-4811
0.4 IV5 4
671


With Normal
and Anuric
Newborn Breast
USUAL PD CSF/ Maternal Maternal Humor/
ADULT <10 (daily Serum Serum Serum Bile/Serum Serum
24/22-50 3-5 mg/kg 6-12 18 24 Avoid 4-5 mg/kg 0.16/0.8 50/404 80/505 125/10 100-200/40-70 10-45/20-30
IV3 post-HD3 q48h
0.1 12 12 18-24 Avoid 30-50 70-100 100 100 10
6-12 1-2 6 6 1 q8-12h 1 q12-24h 8-574 ≥50 10 40-70 20-30
22-50 1 8-12 25-30 ≥50
58 0.5-1 6-8 ≥50
34 0.5-1 4-6 50-80 ≥50
0.05-0.1 24 69

RENAL IMPAIRMENT
With
Newborn Breast
ADULT (daily Serum Serum Serum Serum Serum
HD PD DOSE >80 80-50 50-10 <10 (anuric) Aftera dose) (%)b (%)3 (%) (%) (%)
3-4.4 0.25-0.5 6-12 0.25 0.25 q12-24h Not recommended <100 (18-78)4
q8h
3.2/5.86 0.25-0.75 12 12 0.25-0.5 q12h 0.25-0.5 q18h 0.25-0.5 0.25-0.5 11-46 400 2800-4500 3-227
PO 8-12 8-12 12-24 0.2-0.4 q18-24h q24h q24h
0.2-0.4 IV post-HD
9.8 0.2-0.4 12 12 0.1-0.2 q12h8 0.1-0.2 q12h 67 900
0.4-0.6 24 24 35-449
0.32 24 24
0.25-0.75 24 24 24-48 0.25 q48h 0.25 q48h 0.25 q48h 15 100
0.4 24 24 0.2 q24h 0.2 q24h 0.4 load, then 700

0.2 q24h
0.4 24 24 24 24
1 6 6 6 Avoid10 Minimal
0.4 12 12 24 24 1000
0.2-0.4 12 12 24 0.1-0.2 q24h 0.2 load, then 28-87 96-112 210-1886

PO/IV 0.1 q24h
Continued
672
TABLE 54-25 Anti-infective Agent Pharmacology: Quinolones and Urinary Anti-infectives—cont’d

SERUM
HALF-LIFE

With Normal

ABSORPTION, Dose Serum Urine Daily 1-4 
%) (g) (µg/mL) (µg/mL) Oral Parenteral Dose (g) Oral Parenteral Up to 1 wk wk >80 <10
Oxolinic acid 0.75 PO 0.9-3.6 45-100 0.75 q12h2 2 6-7
(poor)
Pefloxacin (98) 0.4 PO 3.8-5.6 100-115 0.4 8-12 11-15
0.4 IV5 5.8 q12-24h
Sparfloxacin (92) 0.4 PO 1-2 0.4 day 1, 0.4 16-30
then 0.2
q24h
Urinary Anti-infectives
Fosfomycin (37) 3 PO 26.1 706 3 × 1 dose 3 5.7 40 40
Methenamine 1 PO 40 1 q6h2 4 12.5- Not 3-6
hippurate12 (formaldehyde) 18.75 mg/ recommended
kg q6h2
Methenamine 1 PO 70-100 ≈50 1 q12h2 2 12.5-25 mg/ Not 3-6
mandelate12 µmol/L (formaldehyde) kg q12h2 recommended
Nitrofurantoin 0.1 PO <2 50-150 0.05-0.1 0.4 5-7 mg/kg/ Not 0.3 1
(good but q6-8h day q6h recommended
variable)
1
2
Use primarily for the treatment of urinary tract infections.
3
Use during pregnancy not recommended.
4
Animal pharmacology studies indicate the presence of drug in the milk of lactating rats receiving oral doses of cinoxacin. Human data are not currently available.
5
6
3.2 hr during dialysis, 5.8 hr in between sessions.
7
Case report.
8
For creatinine clearance < 30 mL/min; for >30 mL/min, use normal dose.
9
12-24 hr after dose.
10
Ineffective urinary concentrations expected with compromised renal function.
11
8-12 hr during dialysis, 13-48 hr in between sessions.
12
Usually co-administered with an acidifying agent to convert the methenamine salts in urine to ammonia and bactericidal formaldehyde (pH < 5.5). Mandelic acid and hippuric acid are mildly
antiseptic and contribute to urine acidification.
13
Nitrofurantoin accumulates in the serum of patients with creatine clearance <60 mL/min, which leads to systemic toxicity.
14
Although only small amounts of nitrofurantoin have been detected in breast milk, the drug could cause hemolytic anemia in a glucose-6-phosphate dehydrogenase-deficient infant exposed in this
manner.
a
b
Inflamed meninges.
TABLE 54-26 Anti-infective Agent Pharmacology: Antimycobacterials

SERUM
With Normal
CONCENTRATION— (Parenteral): CrCl Values
SELECTED DOSES Adults Children: Dose/Interval Dose/Interval (mL/min)

Aminosalicylic acid 4 PO 76-104 150 mg/kg/ 12 150-360 mg/kg/ 1 23
day q6-12h day q6-8h
Capreomycin3 1 IM 20-47 1 g IM q24h4 1 10-20 mg/kg/ 10-20 mg/ 4-6 29.4-55.5
day q24h kg/day
(not q24h (not
approved) approved)
Clofazimine1 0.1 PO5 0.76 0.1 q24h 0.1 8 days/70
(45-70) days7
8
Cycloserine 0.25 PO 10 0.25-0.5 1 10-20 mg/kg/day 10
(70-90) q12h q12h (not
approved)
673

RENAL IMPAIRMENT
With
Newborn Breast
ADULT (daily Serum Serum Serum Serum Serum
HD PD DOSE >80 80-50 50-10 <10 (anuric) Aftera dose) (%)b (%)3 (%) (%) (%)
0.75 12 Not Not 200-300
recommended recommended10
52-58 200-600
0.4 load, 24 24 48 48
then 0.2
3 Once Once Once

1 6 6 Avoid10
1 12 12 Avoid10 50 70-100
0.05-0.1 6 6 Avoid 10,13

100 <2514 200-400

RENAL IMPAIRMENT
Dosage with
With Dialysis For CrCl Ranges (mL/min) Dialysis Body Fluid Concentrations
Newborn Breast
150 mg/ 6-12 10-50
kg/day
1 24 24 7.5 mg/kg 7.5 mg/kg Minimal
q24-48h 2×/wk
0.1 8 8 8 8
0.25-0.5 12 12 24 0.25 q24h 80-100 100 72
Continued
674
TABLE 54-26 Anti-infective Agent Pharmacology: Antimycobacterials—cont’d

SERUM
With Normal
CONCENTRATION— (Parenteral): CrCl Values
SELECTED DOSES Adults Children: Dose/Interval Dose/Interval (mL/min)

Ethambutol 25 mg/ 2-5 15 mg/kg 15 mg/kg 10-15 mg/kg 3.3 ≥7
(75-80) kg q24h q24h (not
PO recommended)
Ethionamide (80) 1 PO 20 0.25-0.5 1 15-20 mg/kg/ 3 9
q12h day9 q24h (not
approved)
Isoniazid2,10 7 mg/ 4.5/111 0.3 q24h 0.3 IM q24h 0.3 10-20 mg/kg/day 10-20 mg/kg/ 0.5-4 2-10
kg q12-24h day
PO q12-24h
Pyrazinamide 0.5 PO 9-12 15-30 mg/kg 2 30 mg/kg/day 10-16
q24h q12-24h (not
approved)
Rifabutin (≥20) 0.3 PO 0.375 0.3 q24h 0.3 4-18.5 mg/kg 16-69
q24h12
Rifampin (100) 0.6 PO 7 0.6 q24h 0.6 q24h 0.6 10-20 mg/kg/day 2-5 2-5
0.6 IV13 17.5 q12-24h
Rifapentine (70) 0.6 PO 15.05 0.6 twice 0.6 13.19
weekly
Streptomycin 1 IM 25-50 ≥1000 1 IM q24h 1 20-40 mg/kg/ 2-3
day q24h
1
Should be taken with food.
2
Decreased rate or extent, or both, of absorption when given with food.
3
Pharmacokinetics similar to streptomycin.
4
Administer for 60-120 days followed by 1q 2-3×/wk.
5
In leprosy patients.
6
At steady state.
7
8-day serum half-life, 70-day tissue half-life.
8
Dosage should be adjusted to maintain plasma concentrations <30 µg/mL.
9
Limited evidence suggests that 20 mg/kg daily given as a single dose in children is more likely to produce cerebrospinal fluid concentrations exceeding the minimal inhibitory concentration of
2.5 µg/mL for Mycobacterium tuberculosis.
10
To minimize risk of polyneuritis from isoniazid-induced pyridoxine deficiency, pyridoxine (15-50 mg) is often given concurrently.
11
4.5 µg/mL in slow inactivators, 1.0 µg/mL in rapid inactivators.
12
Dose varies significantly by age group; see manufacturer’s recommendations before prescribing.
13
14
Desirable serum concentrations: peak, 5-25 µg/mL; trough, <5 µg/mL.
a
b
Inflamed meninges.
TABLE 54-27 Anti-infective Agent Pharmacology: Antifungal Agents

SERUM
HALF-LIFE
With Normal
Amphotericin B 0.03 IV2 1 0.25-1 mg/kg 1 mg/kg5 0.25-1 mg/kg 0.1-1 mg/ 0.1-1 mg/ 24 or 24 or
(poor) 0.05 IV2 2 q24h3,4 q24-48h3 kg/day3 kg/day3 more more
Anidulafungin 0.1 IV 7.2 0.1-0.2 load, 0.1 0.75-1.5 mg/ 26-50 26-50
then 0.05-0.1 kg/day
q24h
Caspofungin 0.07 load, then 9-11 9-11 9-11
0.05 q24h
Fluconazole (≥90) 0.4 PO 6.72 0.05-0.4 0.05-0.4 q24h 0.4 3-12 mg/ 3-12 mg/kg 20-50 48
0.1 IV6 3.86-4.96 q24h kgq24h q24h
1,7
Flucytosine 2 PO 30-45 50-150 mg/ 150 mg/kg 50-150 mg/ 3-6 30-250
(75-90) kg/day kg/day
q6h q6h
Griseofulvin 0.5/0.25 0.4-2/0.4-2 0.5-1 q24h/ 1 15 mg/kg/ 24 24
(50/>50)8 PO 0.33-0.66 day
q24h q24h
675

RENAL IMPAIRMENT

Dosage with
With Dialysis For CrCl Ranges (mL/min) Dialysis Body Fluid Concentrations
Newborn Breast
15-25 mg/ 24 15 mg/kg 15 mg/kg 15 mg/kg 15 mg/kg/ 15 mg/kg/day 25-50 ∼100
kg q24h q24-36h q48h day
post-HD
0.25-0.5 12 12 12 5 mg/kg q24h 100
0.3 PO/IM 24 24 24 1 dose in slow 5 mg/kg/ Daily dose 100 High 100
2
acetylators day postdialysis
post-HD
15-30 mg/ 24 24 24 12-20 mg/kg 100
kg q24h
0.3 24 24
Minimal 0.6 24 24 24 24 10-20 33 20-60 10,000

change
0.6 Twice Twice
weekly weekly
Up to 110 114
24 7.5 mg/kg/ 7.5 mg/kg/day 7.5 mg/kg/ 0.5 post-HD 20 10-40 <25 40-300
day q24-72h day
q24h q72-96h

With
During Newborn Breast
USUAL PD CSF/ Serum/ Milk/ Aqueous
ADULT <10 (daily Serum Maternal Maternal Bile/ Humor/
HD PD DOSE >80 80-50 50-10 (anuric) Aftera dose) (%)b Serum (%) Serum (%) Serum (%) Serum (%)
0.25-1 mg/kg 24 24 24 24 Usual regimen Usual 3 50 25
regimen
26-50 26-50 0.05-0.1 24 24 24 24 Usual regimen Usual
regimen
0.05 24 24 24 24 Usual regimen
71 0.05-0.4 24 24 50% of 25% of Usual dose 50-94 85

dose dose after
37 mg/kg 6 6 12-24 15-25 mg/ 20-37.5 mg/ 60-100
kg q24h kg post-HD
0.5-1/0.33- 24/24 24/24 24/24 24/24 80

0.66
Continued
676
TABLE 54-27 Anti-infective Agent Pharmacology: Antifungal Agents—cont’d

SERUM
HALF-LIFE

With Normal
Itraconazole 0.2 PO11 2.3/3.512 0.2-0.4 0.2 q24h 0.4 3-5 mg/kg 21-6013
(99.8)9,10 q24h q24h
Ketoconazole10 0.2 PO 4.2 0.2-0.4 0.8 5-10 mg/ 8 8
q12-24h kg/day
q12-24h
Micafungin 0.1 IV 8.17 0.0125-0.15 2-3 mg/kg 15 15
q24h q24h
Miconazole (50)14 0.0514 0.05 q24h
Nystatin (minimal) All doses Not detectable 0.4-1 mU 2 mU 0.4-0.6 mU 0.1 mU 0.1 mU
q8h q6h q6h q6h
Posaconazole 0.2 PO9 0.512 0.2 q8h-0.4 0.8 35 35
q12h
Terbinafine (80) 0.25 PO 1 0.125-0.5 0.5 0.062-0.25 22-30
q12-24h q24h
Voriconazole (96)1
0.2 PO 15
2.08 0.2-0.3 6 mg/kg q12h × 4 mg/kg 0.1-0.2 6 mg/kg q12h 6
3 mg/kg 3.06 q12h 1 day, then q12h16 × 1 day,
IV15 4 mg/kg q12h then 4 mg/
kg q12h16
1
2
Infused over several hr.
3
A test dose of 1 mg infused over 15 min is often given to assess febrile reactions before proceeding to higher doses.
4
Should be administered by slow infusion; rapid IV infusion should be avoided because potentially serious adverse effects (e.g., hypotension, hypokalemia, arrhythmias, shock) may occur.
5
Or 1.5 mg/kg every other day.
6
Infused over 30 min; ascertained on days 6-7.
7
Peak concentrations should be 25 µg/mL to avoid development of resistance but should not exceed 100-120 µg/mL to avoid side effects.
8
Microsize, ultramicrosize.
9
When given with meals.
10
Gastric acid-suppressing agents decrease bioavailability to <5%.
11
Taken 2× day for 15 days.
12
Parent drug, active metabolite (hydroxyitraconazole).
13
Half-life extends as dosing continues.
14
Oral buccal tablet.
15
Administered q12h × 10 days after day 1 loading doses.
16
≥12 yr.
a
b
Inflamed meninges.
TABLE 54-28 Anti-infective Agent Pharmacology: Antiparasitic Agents

CONCENTRATION—SELECTED (Parenteral):
Peak or
Peak Range, Dose (g)/Interval Serious
DRUG (ORAL Serum Urine Infection Up to
ABSORPTION, %) Dose (µg/mL) (µg/mL) Oral Parenteral Daily Dose Oral Parenteral 1 wk 1-4 wk
Albendazole 0.4 g 0.4 0.4 15 mg/kg
Artemether/lumefantrine1 20 mg/120 mg 4 tablets × 61 4 tablets × 61 1-4 tablets × 61
Artesunate 2.4 mg/kg 4-5 2.4 mg/kg × 52 2.4 mg/kg × 52 2.4 mg/kg × 52
Atovaquone (23-47) 0.75-1.5 g 12 0.75-1.5 g 0.75-1.5 g 20 mg/kg
Chloroquine 1 g 1.0 0.5-1 g 0.5-1 g 0.5-1 g 5 mg/kg 5 mg/kg 5 mg/kg 5 mg/kg
Diethylcarbamazine 0.5 0.15-0.25 2 mg/kg tid 0.5-2 mg/kg
Ivermectin 50-200 µg/kg 0.003-0.008 50-200 µg/kg 50-200 µg/kg 50-200 µg/kg
Mebendazole 0.1 g 0.006-0.051 0.1 g bid 0.1 g
Niclosamide 2 g 2 g 2 g 1-2 g
Nitazoxanide 0.5 g 3.0 0.5 g bid 0.5 g 0.1-0.5 g bid
Paromomycin 8-12 mg/kg 8-12 mg/kg tid 8-12 mg/kg 8-12 mg/kg
Pentamidine 3-4 mg/kg 0.5-3.4 3-4 mg/kg 4 mg/kg qd 3-4 mg/kg qd
Praziquantel 25 mg/kg 2-8 25 mg/kg tid 25 mg/kg tid 25 mg/kg tid
Pyrimethamine 0.025-0.075 g 0.26-4.7 0.05-0.075 g qd 0.1/0.05-0.075 g qd 1 mg/kg
Sodium stibogluconate 0.02 g/kg 9-12 0.02 g/kg qd 0.02 g/kg qd 20 mg/kg
677

With
During Newborn Breast
USUAL PD CSF/ Serum/ Milk/ Aqueous
ADULT <10 (daily Serum Maternal Maternal Bile/ Humor/
HD PD DOSE >80 80-50 50-10 (anuric) Aftera dose) (%)b Serum (%) Serum (%) Serum (%) Serum (%)
0.2-0.4 24 24 <10
0.2-0.4 12-24 12-24 12-24 12-24 Usual regimen Usual Minimal Minimal ∼10
regimen
0.012 24 24 24 24 Undetectable Low
0.05 24 24 24 24
0.4-1 mU 8 8 8 8
35 35 0.2-0.4 8-12 8-12 8-12 8-12 Usual regimen Usual

regimen
0.125-0.25 12-24 12-24 Unsafe
4 mg/kg 12 12 12 Try to 42-67

avoid

With Normal
and Anuric
Newborn Breast
0.4
4 tablets x 61
2.4 mg/kg x 52
0.75-1.5g <1
5 mg/kg 0.5-1 0.25-0.5
2 mg/kg
50-200 µg/kg
0.1 g
2 g
0.5 g
8-12 mg/kg
3-4 mg/kg/qd
25 mg/kg
0.1/0.05-0.075 g
0.02 g/kg
Continued
678
TABLE 54-28 Anti-infective Agent Pharmacology: Antiparasitic Agents—cont’d

CONCENTRATION—SELECTED (Parenteral):
Peak or
Peak Range, Dose (g)/Interval Serious
DRUG (ORAL Serum Urine Infection Up to
ABSORPTION, %) Dose (µg/mL) (µg/mL) Oral Parenteral Daily Dose Oral Parenteral 1 wk 1-4 wk
Spiramycin 1 g 0.96 1 q6-12h 4-5
Suramin3 1 g 1 g/day 20 mg/kg
Thiabendazole 1.5 g 0.25-1.5 g bid 0.25-1.5 g
Tinidazole 2 g 42-60 2 g qd 2 g 50 mg/kg
Triclabendazole 10 mg/kg 10 mg/kg 10 mg/kg × 2 10 mg/kg × 2
1
A 3-day regimen of 6 doses of the co-formulated artemether/lumefantrine (20 mg/120 mg per tablet) is recommended on the basis of weight category (adult and pediatric) as an initial oral dose
followed by an oral dose 8 hours later, then the oral dose twice a day for the following 2 days. The dose is stratified by weight: 5-<15 kg (1 tablet per dose), 15-<25 kg (2 tablets per dose),
25- <35 kg (3 tablets per dose), ≥35 kg (4 tablets per dose)
2
5-dose regimen given at 0, 12, 24, 48, and 72 hours.
3
Suramin treatment courses require single-dose administrations on days 1, 3, 7, 14, and 21 of a treatment course.
a
b
Inflamed meninges.
TABLE 54-29 Anti-infective Agent Pharmacology: Antiviral Agents*

SERUM
With Normal
ABSORPTION, Serum Urine Daily Dose Up to
%) Dose (g) (µg/mL) (µg/mL) Oral Parenteral (g) Oral Parenteral 1 wk 1-4 wk >80 <10
Acyclovir (15-30)2 0.2 PO3 0.83 0.2-0.8 2-5 5-12 mg/kg 4 PO, 30 mg/ 0.2 5 days 25-50 mg/kg/ 2.1-3.5 19.5
0.8 PO3 1.61 days q8h kg IV day q8h
5 mg/kg IV4 7.7
Adefovir (59) 0.01 PO 0.018 0.01-0.12 0.12 7.5
q24h
3
Amantadine 0.1 PO 0.302 0.1 q12h 0.2 5-8 mg/kg/ 10-14 170 7-10.3
(85-90) day q12h days
Boceprevir2 0.8 PO 0.1723 0.8 tid 2.4 3.4 3.4
Cidofovir 10 mg/kg IV 24 5 mg/kg qwk5 5 mg/kg 2.5
Entecavir1 0.5 mg PO 0.004 0.5-1 mg 1 mg 128-149

1 mg PO 0.008 q24h
Famciclovir (75-77) 0.5 PO 4 0.125-0.75 2.25 2-2.3
0.75 PO 5.1-5.3 q8-12h
3 6
Foscarnet 0.09 IV 218 60 mg/kg 120-180 mg/ 0.1-17
q8h7 kg
Ganciclovir (5) 5 mg/kg IV4 9 1.0 q8h 5 mg/kg 5 mg/kg 30 mg/kg 5 mg/kg 2.5-5 10
1.0 PO 0.98 q12h8 maintenance q8h q12h8
Interferon alfa-2a 3-6 MU 3×/wk 3.7-8.5

(80 IM, 90 SC)
Interferon alfa-2b 3-5 MU q24h 3-6 MU/m2 2-3
(80 IM, 90 SC) 3×/wk9 3×/wk
Interferon alfa-2b/ 1-1.2 q24h 3-5 MU 3×/wk 0.2-0.4 3 MU/m2 3×/ 6.5/298
ribavirin10 q12h wk11
(33-69-ribavirin)
Interferon-alfa-n3 3 MU 3×/wk 4.43-6.76
Interferon 9 µg 3×/wk 0.5-7
alfacon-1 (80)
Oseltamivir (75) 0.075 PO 0.0652 0.075 0.15 0.03-0.075 6-10
q12-24h q12-24h
Palivizumab 15 mg/kg IV 313 15 mg/kg 15 mg/kg 13-27
qmo qmo days
Peginterferon 22-60
alfa-2b
Ribavirin 0.82 mg/kg/hr12 0.275 0.4-0.6 40-150 µg 1.2 PO 15
24-36
0.82 mg/kg/hr13 1.1 q12h14 qwk
Rimantadine (100) 0.2 0.05- 0.1 q12h 0.2 PO 5 mg/kg/ 19.8-36.5
0.086 day
q12-24h
679


With Normal
and Anuric
Newborn Breast
5-6 0.5-1 6-12
1 g 1
1.5 g bid
2 g qd 50% dose
10 mg/kg ×2

RENAL IMPAIRMENT
With Dosage with

During Newborn Breast Aqueous
USUAL PD CSF/ Serum/ Milk/ Bile/ Humor/
ADULT <10 (daily Serum Maternal Maternal Serum Serum
Minimal 0.2-0.8 PO 2-5×/ 2-5×/day 2-5×/day 0.2-0.8 q24h 0.5 post-HD 2.5 mg/ 50 ≥100 37
change 5-12 mg/kg day 8 8 12-24 2.5-6 mg/kg kg/day
IV q24h
0.01 24 24 48-72 0.01 qwk
0.1 12 24 0.1-0.2 0.1-0.2 qwk 0.2 qwk 50

2-3×/wk
0.8 g 8 8 8 8 8 8 <1
5 mg/kg qwk qwk Do not use Do not use Do not use Do not
use
0.5-1.0 mg 24 24 Give after HD
0.125-0.75 8-12 8-12 0.125-0.5 0.125-0.25 0.125-0.25

q12-24h q24h post-HD
60 mg/kg 8 12 24 45-60 mg/kg 13-103
5 mg/kg 12 2.5 mg/kg 2.5 mg/kg 1.25 mg/kg 1.25 mg/kg 24-68 40

q12h q24h q24h 3×/wk
post-HD
3-6 MU 3×/wk 3×/wk 3×/wk 3×/wk 3×/wk 3×/wk
3-5 MU q24h; q24h; 3×/ q24h; 3×/wk q24h; 3×/wk

3×/wk wk
3-5 MU; 3×/wk; 3×/wk; Not to be Not to be used
1-1.2 q24h q24h used
3 MU 3×/wk 3×/wk 3×/wk 3×/wk

9 µg 3×/wk 3×/wk
0.075 12-24 12-24 24-48
40-150 µg qwk qwk
Not to be Not to be used None 7016

used
0.1 12 12 12 24 Not to be
used
Continued
680
TABLE 54-29 Anti-infective Agent Pharmacology: Antiviral Agents*—cont’d

SERUM
With Normal
ABSORPTION, Serum Urine Daily Dose Up to
%) Dose (g) (µg/mL) (µg/mL) Oral Parenteral (g) Oral Parenteral 1 wk 1-4 wk >80 <10
Telaprevir 0.75 PO 0.75 tid 2.25 9-11 9-11
Telbivudine 0.6 PO3 3.69 0.6 q24h 0.6 40-49
Valacyclovir (55) 2 PO3 8.49 0.5-2 4 2.5-3.617 20
q8-24h
Valganciclovir18 0.45 PO 3.1 0.9 1.8 PO 3.7-4.6
(60) q12-24h
Vidarabine 10 mg/kg IV 0.2-0.4/ 10-15 mg/kg/ 15 mg/kg 10-15 mg/kg/ 15-30 mg/ 15-30 mg/ 1.5/3.3
3-619 day over day over kg/day kg/day
12h 12h over over
12h 12h
Zanamivir (2) 0.01 PO 0.017- 10 mg 10 mg 1.6-5.1
0.142 q12h21 q12h21
*Not including antiretrovirals, which are listed in Table 54-30.
1
2
Bioavailability decreases as dosage is increased.
3
At steady state.
4
Infused over 1 hour.
5
qwk × 2 wk, then qowk.
6
µmol/L.
7
For 14-21 days as initial induction therapy, then 90 mg/kg q24h as maintenance.
8
For 14-21 days as induction therapy; then 5 mg/g q24h.
9
3 MU 3×/wk for hepatitis C; 5 MU q24h for hepatitis B.
10
PO doses are ribavirin; parenteral doses are interferon.
11
Based on weight.
12
Inhaled over 5 hr each day for 3 days.
13
Inhaled over 8 hr each day for 3 days.
14
Mist of 190 µg/L via SPAG-2 aerosol generator; rate of 12.5 L mist/min × 16-18 hr/day 1 of influenza A or B infection, then × 12 hr/day on days 2 and 3; then × 4 hr on day 4 (not approved in
United States).
15
Mist of 190 µg/L via SPAG-2 aerosol generator; rate of 12.5 L mist/min × 12-18 hr/day for 3-7 days.
16
After administration for 4-7 wk in acquired immunodeficiency syndrome (AIDS) or AIDS-related complex patients.
17
Half-life of valacyclovir is <30 min but its metabolite, acyclovir, has a half-life of 2.5-3.6 hr.
18
Should be taken with food.
19
Vidarabine, ara-hypoxanthine (less active metabolite).
20
With normal meninges.
qowk, every other week; qwk, every week; qmo, every month.
21
Dose administered by oral inhalation.
a
b
Inflamed meninges.
TABLE 54-30 Anti-infective Agent Pharmacology: Antiretroviral Agents
SERUM AND URINE


Abacavir (83) 0.3 PO 3.3 0.3 q12h 0.6 8 mg/kg q12h
Atazanavir4 0.4 PO 5.226 0.4 q24h 0.4
Darunavir (82*)4 0.6 PO 0.6-0.8 q12-24h 1.2
Delavirdine (60-100) 0.4 PO5 356 0.4 q8h 1.2 0.4 q8h7
Didanosine1 33 mg/kg 29.86 0.125-0.25 q12h 12 mg/kg/day 120 mg/m2 q12h 100 mg/m2 q12h
(21-43)8,9 PO
Dolutegravir 0.05 PO 3.67 0.05 q12-24h10 0.05-0.1 0.0510

5
Efavirenz 0.6 PO 4.5 0.6 q24h 0.6 0.2-0.6 q24h11
Elvitegravir 0.15 PO 1.7 0.15 q24h 0.15 q24h
Emtricitabine 0.2 PO 2.1 0.2 q24h 0.2 PO
Enfuvirtide 0.1 q12h 0.2
Etravirine4 0.2 q12h 0.4
Fosamprenavir 1.4 PO* 7.9 0.7-1.4 q12-24h 2.8 18-30 mg/kg q12h
681

RENAL IMPAIRMENT

With Dosage with
During Newborn Breast Aqueous
USUAL PD CSF/ Serum/ Milk/ Bile/ Humor/
ADULT <10 (daily Serum Maternal Maternal Serum Serum
0.75 8 8 8 8
0.6 24 24 48-72 72-96 Give after HD
0.5-1 8-12 8-12 12-24 24 0.5-1 Normal 170
0.9 12-14 12-24
15 mg/kg/ Over 12 Over 12 Over 12 10 mg/kg/day Schedule 33-3520

day over 12h post-HD
10 mg 12 12 12 12 12 12

With Normal
and Anuric
Newborn Breast
1.2 1.2 0.3 12 12 12 18-33
5-8 0.4 24 24
15 0.6-0.8 12-24 12-24 12-24
2-11 0.4 8 0.4
1.3-1.6 4.5 0.125-0.4 12-24 12-24 0.1-0.2 0.075-0.125 25% usual 21-46
q24h q24h dose
daily
14 12-24 12-24 12-24 <2
40-55 10 0.6 24 24 24 24 0.6 q24h 0.6 q24h 1.19
12.9 0.15 24 24 D/C D/C D/C D/C
2.5-7 0.2 24 24
0.1 12 12
41 0.2 12 12 12
7.7 7.7 0.7-1.4 12-24 12-24 12-24 12-24
Continued
682
TABLE 54-30 Anti-infective Agent Pharmacology: Antiretroviral Agents—cont’d
SERUM AND URINE


Indinavir1 (30) 0.8 PO5,9 251-12,61711 0.8 q8h 2.4 350 mg/m2 q8h
Lamivudine (82-87) 2-8 mg/kg 1.725-5.815 0.1-0.3 q12-24h 0.6 3-4 mg/kg q12h13

PO
Lopinavir/ritonavir4 0.4/0.05 6 (lopinavir) 0.4/0.1 q12h14 0.8/0.2 10-12/2.5-3 mg/kg
PO q12h
Maraviroc (23-33) 0.3 PO5 0.888 0.15-0.6 q12h 1.2
Nelfinavir4 0.75 PO5 2.9 0.75-1.25 q8-12h4 2.5 20-30 mg/kg q8h4
Nevirapine (>90) 0.4 PO 2.9-3.4 0.2 q12h 0.4 4 mg/kg q12h
maintenance maintenance15
Raltegravir 0.4 q12h 0.8
Rilpivirine 0.025 PO 0.079 0.025 q24h 0.025
Ritonavir16 (80) 0.6 PO 5 11.2 0.6 q12h 1.2 400 mg/m2 q12h

1.2 PO
Saquinavir4 0.6 PO 0.066 0.6-1.2 q8h17,18 7.2
Stavudine (80) 4 mg/kg 4.2 0.03-0.04 q12h 2 mg/kg/day 2 mg/kg/day19 0.5 mg/kg 1 mg/kg q12h PO
PO q12h PO
Tenofovir4 (40) 0.3 PO 0.296 0.3 q24h 0.3 PO
Tipranavir4 0.5 PO* 94.8 mcM 0.5 q12h 1
Zidovudine (50-76)20 0.2-0.3 q8-12h 1 mg/kg q4h21 0.6 160 mg/m2 q8h
1
4
Give with food.
5
At steady state.
6
µmol/L.
7
For children ≥13 yr old.
8
Bioavailability decreases as dosage is increased.
9
In human immunodeficiency virus–positive patients.
10
Dosed once a day in HIV-1 integrase strand transfer inhibitor (INSTI) naïve patients but should be used twice daily in INSTI-experience with certain or clinically suspected resistance substitutions or
used in combination with UGT1A/CYP3A inhibitors.
11
Based on weight.
12
nmol.
13
>12 yr of age, 150 mg q12h.
14
Needs dosage adjustment if given with nevirapine or efavirenz in treatment-experienced patients when reduced susceptibility to lopinavir is suspected.
15
>9 yr, 120 mg/m2.
16
In animals.
17
Lower dose for saquinavir mesylate.
18
600  mg q8h for saquinavir mesylate and 1200 mg q8h for plain saquinavir (Fortovase).
19
Children >30 kg should receive adult dosage.
20
Reaches systemic circulation as unchanged drug.
21
An IV dose of 1 mg/kg q4h is equivalent to an oral dose of 100 mg q4h.
*When administered with ritonavir.
a
b
Inflamed meninges.
683


With Normal
and Anuric
Newborn Breast
1.5-2 1.5-2 0.8 8 8 8 8 Usual 5-9 Unsafe
regimen
3-7 0.15-0.3 12-24 12-24 0.05-0.15 0.025 q24h 0.025 6-11 ∼100 ∼100
q24h q24h
5-6 0.4/0.1 12 12
14-18 0.15-0.6 12 12
3.5-5 3.5-5 3.5-5 3.5-5 0.75-1.25 8-12 8-12 8-12 8-12 None Normal 0
25-30 25-30 0.2 12 12 12 12 Usual Usual 60
regimen regimen
9 9 0.4 12 12 12 12 Dose after
HD
50 0.025 24 24 Usual
regimen
3-3.5 3-3.5 0.6 12 12 12 None 0.2
13 13 0.6 or 8 8 8 8 None 0.2

1.217
0.9-1.6 5.7 5.3 0.04 12 12 0.02 0.02 q24h 0.015-0.02 24-94
q12-24h q24h
4-8 0.3 24 24
4.8-6 0.5 12 12 12
0.5-3 1.4 0.2-0.3 8-12 8-12 8-12 0.1 q6-8h 0.1 q6-8h 50-70 100 100
684
TABLE 54-31 Key Drug Substrates, Organized by Cytochrome P-450 (CYP) Drug-Metabolizing Isozymes
CYP1A2 CYP2B6 CYP2C8 CYP2C9 CYP2C19 CYP2D6 CYP2E1 CYP3A
Amitriptyline Bupropion Amodiaquine Amitriptyline Carisoprodol Alprenolol Acetaminophen Alfentanil Pimozide

Caffeine Cyclophos- Cerivastatin Celecoxib Chloramphenicol Amitriptyline Chlorzoxazone Alprazolam Progesterone
Clomipramine phamide Paclitaxel Diclofenac Citalopram Amphetamine Enflurane Amlodipine Quetiapine
Clozapine Efavirenz Torsemide Fluoxetine Clomipramine Aripiprazole Ethanol Aprepitant Quinidine
Cyclobenzaprine Ifosfamide Repaglinide Fluvastatin Cyclophosphamide Atomoxetine Halothane Aripiprazole Quinine
Estradiol Methadone Glipizide Esomeprazole Carvedilol Isoflurane Artemisinins Risperidone
Fluvoxamine Glyburide Hexobarbital Chlorpheniramine Methoxyflurane Astemizole Ritonavir
Haloperidol Ibuprofen Indomethacin Chlorpromazine Sevoflurane Atazanavir Salmeterol
Mexiletine Irbesartan Lansoprazole Clomipramine Atorvastatin Saquinavir
Naproxen Lornoxicam Moclobemide Codeine Boceprevir Sildenafil
Olanzapine Losartan Nelfinavir Debrisoquine Buspirone Simvastatin
Ondansetron Meloxicam Nilutamide Desipramine Cafergot Sirolimus
Phenacetin Nateglinide Omeprazole Dexfenfluramine Chlorpheniramine Tacrolimus
Propranolol Omeprazole Pantoprazole Dextromethorphan Cilostazol Tadalafil
Riluzole Phenytoin Phenobarbital Duloxetine Clarithromycin Taxol
Ropivacaine Piroxicam Phenytoin Encainide Cocaine Telaprevir
Tacrine Rosiglitazone Primidone Flecainide Cyclosporine Telithromycin
Theophylline Rosuvastatin Progesterone Fluoxetine Dapsone Terfenadine
Tizanidine S-warfarin Proguanil Fluvoxamine Darunavir Testosterone
Verapamil Tamoxifen Propranolol Haloperidol Dexamethasone Tipranavir
R-warfarin Tolbutamide Rabeprazole Imipramine Dextromethorphan Trazodone
Zileuton Torsemide Teniposide Lidocaine Diltiazem Triazolam
Zolmitriptan Voriconazole Methoxyamphetamine Docetaxel Troleandomycin
Metoclopramide Domperidone Vardenafil
Paroxetine Eplerenone Verapamil
Perphenazine Erythromycin Vincristine
Propafenone Estradiol Zaleplon
S-metoprolol Etravirine Ziprasidone
Thioridazine Felodipine Zolpidem
Timolol Fentanyl
Finasteride
Fosamprenavir
Haloperidol
Hydrocortisone
Imatinib
Indinavir
Irinotecan
Lidocaine
Lovastatin
Midazolam
Nateglinide
Nelfinavir
Nifedipine
Nisoldipine
Nitrendipine
Ondansetron
TABLE 54-32 Drug Inhibitors* by Cytochrome P-450 (CYP) Drug-Metabolizing Isozymes

Amiodarone Ticlopidine Gemfibrozil Amiodarone Cimetidine Amiodarone Disulfiram Amiodarone
Cimetidine Thiotepa Montelukast Fenofibrate Esomeprazole Bupropion Aprepitant
Ciprofloxacin Pioglitazone Fluconazole Felbamate Celecoxib Cimetidine
Fluvoxamine Quercetin Fluvastatin Fluoxetine Chlorpheniramine Clarithromycin
Interferon Rosiglitazone Fluvoxamine Fluvoxamine Chlorpromazine Cobicistat
Methoxsalen Trimethoprim Isoniazid Indomethacin Cimetidine Delavirdine
Probenecid Ketoconazole Citalopram Diltiazem
Sertraline Lansoprazole Clemastine Elvitegravir
Sulfamethoxazole Modafinil Clomipramine Erythromycin
Teniposide Omeprazole Cocaine Fluconazole
Voriconazole Oxcarbazepine Diphenhydramine Fluvoxamine
Zafirlukast Pantoprazole Doxepin Gestodene
Probenecid Doxorubicin Imatinib
Rabeprazole Duloxetine Indinavir
Ticlopidine Escitalopram Itraconazole
Topiramate Fluoxetine Ketoconazole
Halofantrine Mibefradil
Hydroxyzine Mifepristone
Metoclopramide Nefazodone
Mibefradil Nelfinavir
Midodrine Norfloxacin
Moclobemide Norfluoxetine
Paroxetine Posaconazole
Perphenazine Ritonavir
Quinidine Saquinavir
Ranitidine Telithromycin
Ritonavir Verapamil
Sertraline Voriconazole
Terbinafine
Ticlopidine
*Anti-infectives are bold.
685
TABLE 54-33 Drug and Chemical Inducers* by Cytochrome P-450 (CYP) Drug-Metabolizing Isozymes

Cigarette smoking Phenobarbital Rifampin Rifampin Carbamazepine Dexamethasone Ethanol Barbiturates
Marijuana smoking Rifampin Secobarbital Norethindrone Rifampin Isoniazid Carbamazepine
Modafinil Prednisone Efavirenz
Nafcillin Rifampin Glucocorticoids
Modafinil
Nevirapine
Oxcarbazepine
Phenobarbital
Phenytoin
Pioglitazone
Rifabutin
Rifampin
St. John’s wort
TABLE 54-34 Select Drug Transporter Localization with Representative Substrates, Inducers, and Inhibitors*
FAMILY SOLUTE-LIKE CARRIER (SLC) TRANSPORTERS
ATP-BINDING CASETTE (ABC) Organic Anion Organic Cation
Subgroup TRANSPORTERS Transporters (OATs) OAT Polypeptide Transporters (OCT)
Breast Cancer
Resistant P-glycoprotein
Transporter Protein (BCRP) (P-gp) OAT1 OAT3 OATP1B1 OATP1B3 OCT2
Organ/Tissue Breast Adrenal Brain Brain Liver Liver Brain
Localization Intestine Brain Kidney Kidney Kidney
Liver Intestine
Placenta Kidney
Liver
Placenta
Testes
Substrates Imatinib Digoxin Adefovir Acyclovir Atrasentan Atorvastatin Amantadine
Methotrexate Fexofenadine Captopril Bumetanide Atorvastatin Olmesartan Amiloride
Mitoxantrone Indinavir Furosemide Ciprofloxacin Bosentan Pitavastatin Cimetidine
Irinotecan Vincristine Lamivudine Famotidine Ezetimibe Rosuvastatin Dopamine
Lapatinib Colchicine Methotrexate Furosemide Fluvastatin Telmisartan Famotidine
Rosuvastatin Topotecan Oseltamivir Methotrexate Glyburide Valsartan Memantine
Sulfasalazine Paclitaxel Tenofovir Zidovudine Olmesartan Metformin
Topotecan Zalcitabine Oseltamivir Pitavastatin Pindolol
Zidovudine Carboxylate Pravastatin Procainamide
Penicillin G Repaglinide Ranitidine
Pravastatin Rifampin Varenicline
Rosuvastatin Rosuvastatin Oxaliplatin
Sitagliptin Simvastatin acid
Valsartan
Inhibitors Cyclosporine Amiodarone Cefadroxil Cimetidine Atazanavir Atazanavir Cimetidine
Eltrombopag Azithromycin Cefamandole Diclofenac Cyclosporine Cyclosporine Quinidine
Gefitinib Captopril Cefazolin Probenecid Eltrombopag Lopinavir/
Carvedilol Probenecid Gemfibrozil rifampin
Clarithromycin Lopinavir/ Ritonavir
Conivaptan rifampin Saquinavir
Cyclosporine Ritonavir
Diltiazem Saquinavir
Dronedarone Tipranavir
Erythromycin
Felodipine
Itraconazole
Ketoconazole
Lopinavir/
ritonavir
Quercetin
Quinidine,
Ranolazine
Verapamil
Inducers Not yet identified Avasimibe Not yet Not yet Not yet Not yet Not yet identified
Carbamazepine identified identified identified identified
Phenytoin
Rifampin
St John’s wort
Tipranavir/
ritonavir
686
TABLE 54-35 Adverse Drug Interactions Involving Anti-infective Agents*

INTERACTING DRUGS ADVERSE EFFECT PROBABLE MECHANISM
Abacavir with
Amprenavir Increased amprenavir effect, toxicity Increased bioavailability
Methadone Decreased methadone effect Mechanism not established
Ribavirin Increased risk of lactic acidosis Mechanism not established
Acyclovir, Valacyclovir with
Aminoglycosides Increased nephrotoxicity and/or neurotoxicity Mechanism not established
Cimetidine Increased acyclovir toxicity Mechanism not established
Cyclosporine Increased risk of nephrotoxicity Mechanism not established
Narcotics Increased meperidine effect Decreased renal excretion
Phenytoin Decreased phenytoin effect Altered gastrointestinal (GI) transit, pH
Probenecid Possible increased acyclovir toxicity Decreased renal excretion
Valproic acid Decreased valproic acid effect Altered GI transit, pH
Zidovudine Increased neurotoxicity (profound drowsiness and lethargy) Additive toxicity
Amantadine with
Anticholinergics Hallucinations, confusion, nightmares Mechanism not established
Antihistamines Increased CNS adverse reactions Additive anticholinergic effects
Bupropion Increased adverse events Mechanism not established
Central nervous system (CNS) stimulants Additive CNS stimulant effects Mechanism not established
Dopamine agonists Decreased amantadine effect Antagonism
Triamterene CNS toxicity Decreased renal clearance
Trimethoprim CNS toxicity Decreased renal clearance
Aminoglycoside Antibiotics with
Acyclovir Increased nephrotoxicity and/or neurotoxicity Additive toxicity
Amphotericin B Nephrotoxicity Synergism
Anticoagulants, oral Potentiation of anticoagulation effects Decreased GI absorption or synthesis of vitamin K
Bacitracin Increased nephrotoxicity Additive toxicity
Bumetanide Increased ototoxicity Additive toxicity
Capreomycin Increased nephrotoxicity and/or neurotoxicity Additive toxicity
Carboplatin Increased ototoxicity Additive toxicity
Cephalosporins Increased nephrotoxicity Mechanism not established
Cidofovir Increased nephrotoxicity Additive toxicity
Cisplatin Increased nephrotoxicity Mechanism not established
Colistimethate Increased nephrotoxicity and/or neurotoxicity Additive toxicity
Cyclosporine Increased renal toxicity Possibly additive or synergistic
Digoxin Probable decreased digoxin effect with oral gentamicin or Decreased absorption
neomycin
Ethacrynic acid Increased ototoxicity Additive toxicity
Furosemide Increased ototoxicity and nephrotoxicity Additive toxicity
Magnesium sulfate Increased neuromuscular blockade Additive toxicity
Methotrexate Possible increased methotrexate toxicity with kanamycin Mechanism not established
Possible decreased methotrexate effect with oral aminoglycosides Decreased absorption
Methoxyflurane Increased nephrotoxicity Additive toxicity
Miconazole Possible decreased tobramycin concentration Mechanism not established
Neuromuscular blocking agents Neuromuscular blockade Additive toxicity
Nonsteroidal anti-inflammatory drugs Possible aminoglycoside toxicity in preterm infants with Decreased renal clearance
(NSAIDs) indomethacin given for patent ductus closure
Penicillins Decreased aminoglycoside effect with high concentrations of Inactivation
carbenicillin or ticarcillin
Polymyxins Falsely low aminoglycoside levels In vitro inactivation
Increased nephrotoxicity; neuromuscular blockade Additive toxicity
Tacrolimus Increased nephrotoxicity Additive toxicity
Vancomycin Possible increased nephrotoxicity and ototoxicity Additive toxicity
Aminosalicylic Acid (PAS) with
Anticoagulants, oral Enhanced hypoprothrombinemic effects Mechanism not established
Ammonium chloride Increased probability of crystalluria Acidification of urine
Bacillus Calmette-Guérin (BCG) vaccine Negates BCG effect Negates immune response
Digoxin Decreased digoxin effect Decreased absorption with time
Diphenhydramine Decreased effect of PAS Decreases GI absorption
Ethionamide GI distress, hepatotoxicity Additive
Isoniazid Increased Isoniazid (INH) serum concentrations Decreased metabolism
Probenecid Increased PAS toxicity Decreased renal excretion
Rifampin Rifampin effectiveness may be decreased; separate doses by Decreased GI absorption due to excipient
8-12 hr bentonite
687
TABLE 54-35 Adverse Drug Interactions Involving Anti-infective Agents—cont’d

Amphotericin B with

Aminoglycoside antibiotics Nephrotoxicity Synergism
Antineoplastics Possible increased renal toxicity, bronchospasm, and hypotension Mechanism not established
Capreomycin Increased nephrotoxicity Additive toxicity
Cisplatin Increased nephrotoxicity Additive toxicity
Colistin Increased nephrotoxicity Additive toxicity
Corticosteroids Increased hypokalemia Additive toxicity
Cyclosporine Increased renal toxicity Possible synergism
Digitalis glycosides Increased digitalis toxicity Hypokalemia
Imidazole antifungals Possible antagonism in animal models Mechanism not established
Neuromuscular blocking agents Increased neuromuscular blocking effects Hypokalemia
Pentamidine Increased nephrotoxicity Additive toxicity
Polymyxins Increased nephrotoxicity Additive toxicity
Tacrolimus Increased nephrotoxicity Additive toxicity
Vancomycin Increased nephrotoxicity Additive toxicity
Zidovudine Potential for increased myelotoxicity and nephrotoxicity Mechanism not established
Anidulafungin with
Cyclosporine Increased anidulafungin exposure Mechanism not established
Azithromycin with
Aluminum/magnesium antacids Decreased peak; no effect on overall exposure Mechanism not established
Cyclosporine Possible increased cyclosporine effect, toxicity Mechanism not established
Digoxin Increased digoxin concentrations Destruction of intestinal Eubacterium lentum in
10% of digoxin patients
Nelfinavir Increased azithromycin exposure P-glycoprotein competition
Warfarin Possible increased warfarin effect, toxicity Decreased vitamin K–producing gut flora
Aztreonam with
Chloramphenicol Possible in vitro antagonism; administer a few hours apart Mechanism not established
Bacitracin with
Aminoglycosides Increased nephrotoxicity Additive toxicity
Anesthetics Potentiation of neuromuscular blocking effects Additive toxicity
Neuromuscular blocking drugs Potentiation of neuromuscular blocking effects Additive toxicity
Capreomycin with
Aminoglycosides Increased nephrotoxicity and/or ototoxicity Additive toxicity
BCG vaccine Negates BCG effect Negates immune response
Polymyxin B Increased nephrotoxicity Additive toxicity
Vancomycin Increased nephrotoxicity and/or ototoxicity Additive toxicity
Caspofungin with
Carbamazepine Decreased caspofungin effect Increased metabolism
Cyclosporine Increased caspofungin effect, toxicity Mechanism not established
Dexamethasone Decreased caspofungin effect Increased metabolism
Efavirenz Decreased caspofungin effect Increased metabolism
Nelfinavir Decreased caspofungin effect Increased metabolism
Nevirapine Decreased caspofungin effect Increased metabolism
Phenytoin Decreased caspofungin effect Increased metabolism
Rifamycins Decreased caspofungin effect Increased metabolism
Tacrolimus Decreased tacrolimus effect Mechanism not established
Cefditoren with
Antacids Decreased cefditoren effect Decreased bioavailability
H2 receptor antagonists Decreased cefditoren effect Decreased bioavailability
Proton pump inhibitors Decreased cefditoren effect Decreased bioavailability
Cephalosporins with
Alcohol Disulfiram-like effect with cefamandole, cefmetazole, cefotetan, Inhibition of intermediary metabolism of alcohol
cefoperazone, and moxalactam; cefonicid also in animals, but
not shown in humans
Aminoglycoside antibiotics Increased nephrotoxicity Mechanism not established
Ampicillin In vitro antagonism with ceftazidime versus group B streptococci Mechanism not established
and Listeria
Continued
688

Anticoagulants, oral Possible increased anticoagulant effect with moxalactam, Mechanism not established
cefamandole, cefmetazole, or cefoperazone
Aspirin Possible increased bleeding risk with moxalactam Additive toxicity
Chloramphenicol In vitro antagonism Mechanism not established
Diuretics Increased nephrotoxicity with some cephalosporins Mechanism not established
Ethacrynic acid Increased nephrotoxicity Mechanism not established
Furosemide Increased nephrotoxicity Mechanism not established
Heparin Possible increased bleeding risk with moxalactam Additive toxicity
Penicillins Possible increased cefotaxime toxicity with azlocillin in patients Decreased excretion
with renal impairment
Probenecid Higher and prolonged cephalosporin concentrations Competitive inhibition of tubular secretion
Salicylates Decreased cefixime concentration and area under the serum Displacement from protein-binding sites
anti-infective concentration curve (AUC)
Cethromycin with
Ranitidine Decreased cethromycin exposure Mechanism not established
Chloramphenicol with
Acetaminophen Possible decreased chloramphenicol effect Increased metabolism
Anticoagulants, oral Increased dicumarol effect Decreased metabolism
Aminoglycosides In vitro antagonism; not seen in vivo Mechanism not established
Aztreonam Antagonism; administer chloramphenicol separately a few hours Mechanism not established
later
Barbiturates Increased barbiturate effect; decreased chloramphenicol effect Decreased/increased metabolism
Cephalosporins Antagonism Mechanism not established
Cimetidine Aplastic anemia Possibly additive or synergistic
Cyclophosphamide Decreased cyclophosphamide effect Decreased clearance
Etomidate Prolonged anesthesia Decreased metabolism
Folic acid Delayed response to folic acid Mechanism not established
Hypoglycemics, sulfonylurea Increased hypoglycemic effect Mechanism not established
Iron Delayed response to iron Mechanism not established
Lincomycin Decreased lincomycin effect Target site antagonism
Penicillins In vitro antagonism; not seen in vivo Mechanism not established
Phenytoin, fosphenytoin Increased phenytoin toxicity Decreased metabolism
Possible increased chloramphenicol toxicity Mechanism not established
Rifampin, rifabutin Decreased chloramphenicol effect Increased metabolism
Vitamin B12 Delayed response to vitamin B12 Mechanism not established
Chloroquine with
Ampicillin Decreased ampicillin effect Decreased bioavailability
Aurothioglucose Blood dyscrasias Additive toxicity
Cholestyramine Decreased effect Decreased bioavailability
Cimetidine Increased toxicity Decreased clearance
Cyclosporine Increased cyclosporine toxicity Decreased clearance
Magnesium antacids Decreased efficacy Decreased bioavailability
Methotrexate (MTX) Decreased MTX efficacy Increased clearance
Rabies vaccine Decreased vaccine effect Interference with antibody response
Ritonavir Increased chloroquine toxicity Decreased metabolism
Succinylcholine Increased neuromuscular blockade Decreased clearance
Cidofovir with
Aminoglycosides Increased risk of nephrotoxicity Additive toxicity
Foscarnet Increased risk of nephrotoxicity Additive toxicity
Pentamidine Increased risk of nephrotoxicity Additive toxicity
Clarithromycin with
Astemizole Increased risk of cardiotoxicity Decreased metabolism
Benzodiazepines (BZDs) Increased CNS toxicity Decreased metabolism
Carbamazepine (CBZ) Increased CBZ toxicity Decreased metabolism
Cimetidine Decreased clarithromycin concentrations Prolonged absorption
Cisapride Increased cisapride effect, toxicity Decreased metabolism
Clindamycin In vitro antagonism; not documented clinically Mechanism not established
Corticosteroids Increased steroid effect, toxicity Decreased excretion
Coumarin derivatives Increased coumarin effect, toxicity Decreased metabolism
Cyclosporine Increased cyclosporine toxicity Decreased metabolism
689


Delavirdine Increased clarithromycin toxicity Decreased metabolism
Digoxin Increased digoxin effect Decreased gut metabolism, increased absorption
Disopyramide Increased disopyramide effect, toxicity Mechanism not established
Ergot alkaloids Increased ergot effect, toxicity Mechanism not established
Fluoxetine Increased fluoxetine effect, toxicity Decreased metabolism
Hydroxymethylglutaryl-coenzyme A Increased risk of rhabdomyolysis Decreased metabolism
(HMG-CoA) reductase inhibitors
Loratadine Increased loratadine exposure, toxicity (?) Decreased metabolism
Omeprazole Increased omeprazole effect, toxicity; increased clarithromycin Decreased metabolism; mechanism not
gastric tissue exposure established
Phenytoin Possible increased or decreased effect Altered metabolism
Pimozide Increased pimozide effect, toxicity Decreased metabolism
Rifamycins Decreased clarithromycin concentrations, increased rifamycin toxicity Increased/decreased metabolism
Ritonavir Increased clarithromycin effect, toxicity Decreased metabolism
Saquinavir Increased saquinavir effect, toxicity Decreased metabolism
Sildenafil Increased sildenafil effect, toxicity Decreased metabolism
Tacrolimus Increased tacrolimus effect, toxicity Decreased metabolism
Terfenadine Increased risk of cardiotoxicity Decreased metabolism
Theophylline Increased theophylline effect, toxicity Decreased metabolism
Zidovudine Decreased zidovudine effect Mechanism not established
Clindamycin with
Neuromuscular blocking agents Increased neuromuscular blockade Additive toxicity
Saquinavir Increased clindamycin toxicity Decreased metabolism
Clofazimine with
Dapsone Possible decrease or nullification of clofazimine’s anti-inflammatory Opposing effects on neutrophil motility and
activity lymphocyte transformation
Isoniazid Increased clofazimine serum and urine concentrations, decreased Mechanism not established
skin concentrations
Phenytoin Decreased efficacy Increased phenytoin clearance
Rifampin Decreased rate of absorption, time to reach peak, and AUC of Mechanism not established
rifampin
Colistimethate
Same as polymyxin B
Cycloserine with
Alcohol Increased alcohol effect or convulsions Mechanism not established
Anticoagulants, oral Increased effect Mechanism not established
Ethionamide Increased neurotoxicity Additive toxicity
Isoniazid CNS effects, dizziness, drowsiness; increased neurotoxicity Mechanism not established, additive toxicity
Phenytoin Increased phenytoin effect, toxicity Decreased metabolism
Dapsone with
Aniline Increased risk of hemolysis in glucose-6-phosphate dehydrogenase Additive toxicity
(G6PD) deficiency
Clofazimine Decreased or nullification of clofazimine’s anti-inflammatory Opposing effects on neutrophil motility and
effects lymphocyte transformation in vitro
Delavirdine Increased dapsone toxicity Decreased metabolism
Didanosine Increased incidence of Pneumocystis jirovecii (formerly P. carinii) Mechanism not established
pneumonia recurrence
Folic acid antagonists Increased risk of hematologic toxicity Additive toxicity
Naphthalene Increased risk of hemolysis in G6PD deficiency Additive toxicity
Niridazole Increased risk of hemolysis in G6PD deficiency Additive toxicity
Nitrite Increased risk of hemolysis in G6PD deficiency Additive toxicity
Nitrofurantoin Increased risk of hemolysis in G6PD deficiency Additive toxicity
Phenylhydrazine Increased risk of hemolysis in G6PD deficiency Additive toxicity
Primaquine Increased risk of hemolysis in G6PD deficiency Additive toxicity
Pyrimethamine Increased risk of hematologic toxicity Additive toxicity
Rifampin/rifabutin Decreased dapsone serum concentrations Hepatic enzyme induction
Saquinavir Increased dapsone toxicity Decreased metabolism
Trimethoprim Increased dapsone serum concentrations; increased risk of adverse Mechanism not established
effects
Zidovudine Increased risk of hematologic toxicity Additive toxicity
Daptomycin with
HMG-CoA reductase inhibitors Possible increased risk of myopathy Mechanism not established
Tobramycin Possible increased exposure to daptomycin, possible decreased Mechanism not established
exposure to tobramycin
Continued
690

Darunavir with
Antihistamines Increased antihistamine exposure, toxicity CYP3A inhibition

BZDs Increased benzodiazepine exposure, toxicity CYP3A inhibition
Cisapride Increased cisapride exposure, toxicity CYP3A inhibition
CYP3A metabolized agents Increased exposure CYP3A inhibition
Ergot derivatives Increased ergot exposure, toxicity CYP3A inhibition
Pimozide Increased pimozide exposure, toxicity CYP3A inhibition
Delavirdine with
Acenocoumarol Increased acenocoumarol effect, toxicity Decreased metabolism
Alfentanil Increased alfentanil effect, toxicity Decreased metabolism
Amiodarone Increased amiodarone effect, toxicity Decreased metabolism
Amprenavir Decreased amprenavir clearance; increased delavirdine clearance Cytochrome P-450 (CYP) 3A4 interaction
Antacids Decreased delavirdine effect Decreased bioavailability
Atorvastatin Increased exposure and statin side effects Decreased metabolism
Barbiturates Increased barbiturate effect, toxicity; decreased delavirdine effect Decreased/increased metabolism
Bepridil Increased bepridil effect, toxicity Decreased metabolism
BZDs Increased BZD effect, toxicity Decreased metabolism
Calcium channel blockers Increased calcium blocker effect, toxicity Decreased metabolism
CBZ Increased CBZ toxicity; decreased delavirdine effect Decreased/increased metabolism
Clarithromycin Increased clarithromycin, delavirdine effect, toxicity Decreased metabolism
Clindamycin Increased clindamycin effect, toxicity Decreased metabolism
Corticosteroids Increased steroid effect, toxicity Decreased metabolism
Cyclosporine Increased cyclosporine effect, toxicity Decreased metabolism
Cyclophosphamide Increased cyclophosphamide toxicity; decreased delavirdine effect Decreased/increased metabolism
Dapsone Increased dapsone effect, toxicity Decreased metabolism
Daunorubicin Increased daunorubicin effect, toxicity Decreased metabolism
Doxorubicin Increased doxorubicin effect, toxicity Decreased metabolism
Ergot derivatives Increased ergot effect, toxicity Decreased metabolism
Erythromycin Increased erythromycin, delavirdine effect, toxicity Decreased metabolism
Fluoxetine Increased delavirdine effect, toxicity Decreased metabolism
Fluvastatin Increased exposure and statin side effects Decreased metabolism
Garlic supplements Decreased delavirdine effect Increased metabolism
Glimepiride Increased glimepiride exposure, effects Decreased metabolism
Glipizide Increased glipizide exposure, effects Decreased metabolism
Glyburide Increased glyburide exposure, effects Decreased metabolism
H2 receptor antagonists Decreased delavirdine effect Decreased bioavailability
Ifosfamide Increased ifosfamide effect, toxicity Decreased metabolism
Itraconazole Increased itraconazole effect, toxicity Decreased metabolism
Ketoconazole Increased delavirdine effect, toxicity Decreased metabolism
Lidocaine Increased lidocaine effect, toxicity Decreased metabolism
Lovastatin Increased exposure and statin side effects Decreased metabolism
Metronidazole Increased metronidazole effect, toxicity Decreased metabolism
Nefazodone Increased nefazodone effect, toxicity Decreased metabolism
Paclitaxel Increased paclitaxel toxicity Decreased metabolism
Phenytoin Increased phenytoin effect, toxicity; decreased delavirdine effect Decreased/increased metabolism
Pioglitazone Possible increased pioglitazone exposure, effects; possible CYP inhibition; CYP induction
decreased delavirdine exposure
Proton pump inhibitors Decreased delavirdine effect Decreased bioavailability
Quinidine Increased quinidine effect, toxicity Decreased metabolism
Repaglinide Increased repaglinide exposure, effects Decreased metabolism
Rifamycins Increased rifamycin effect, toxicity; decreased delavirdine effect Decreased/increased metabolism
Simvastatin Increased exposure and statin side effects Decreased metabolism
Sirolimus Increased sirolimus effect, toxicity Decreased metabolism
St. John’s wort Decreased delavirdine effect Increased metabolism
Tolbutamide Increased tolbutamide exposure, effects Decreased metabolism
Warfarin Increased warfarin effect, toxicity Decreased metabolism
Zolpidem Increased zolpidem effect, toxicity Decreased metabolism
691

Didanosine (DDI) with

Allopurinol Increased DDI effect, toxicity Decreased DDI clearance
Antacids Increased toxicity caused by ingredients in both Additive toxicity
Aurothioglucose Increased peripheral neuropathy Additive toxicity
BZDs Increased confusion Mechanism not established
Bisphosphonates Decreased effect of bisphosphonates Decreased bioavailability
Chloramphenicol Increased peripheral neuropathy Additive toxicity
Cisplatin Increased peripheral neuropathy Additive toxicity
Dapsone Decreased dapsone effect, increased peripheral neuropathy Decreased dapsone bioavailability, additive toxicity
Delavirdine Decreased delavirdine, DDI effect Mechanism not established
Disulfiram Increased peripheral neuropathy Additive toxicity
Ethambutol Increased peripheral neuropathy, ocular toxicity Additive toxicity
Ethionamide Increased peripheral neuropathy Additive toxicity
Fluoroquinolones Decreased fluoroquinolone, DDI effects Decreased bioavailability
Ganciclovir Increased peripheral neuropathy, pancreatitis Altered bioavailability of both
Glutethimide Increased peripheral neuropathy Additive toxicity
Hydralazine Increased peripheral neuropathy Additive toxicity
Indinavir Decreased indinavir effect Decreased bioavailability
Iodoquinol Increased peripheral neuropathy Additive toxicity
Isoniazid Increased peripheral neuropathy Additive toxicity
Itraconazole Decreased itraconazole effect Decreased bioavailability
Ketoconazole Decreased ketoconazole effect Decreased bioavailability
Methadone Decreased DDI effect Decreased bioavailability
Metronidazole Increased peripheral neuropathy Additive toxicity
Nitrofurantoin Increased peripheral neuropathy Additive toxicity
Pentamidine Increased risk of pancreatitis Additive toxicity
Phenytoin Increased peripheral neuropathy Additive toxicity
Ribavirin Increased risk of toxicity Additive toxicity
Tetracyclines Decreased tetracycline effect Decreased bioavailability
Trimethoprim/sulfamethoxazole Increased pancreatitis Additive toxicity
Vincristine Increased peripheral neuropathy Additive toxicity
Zalcitabine Increased neurotoxicity Additive toxicity
Dirithromycin with
Digoxin Increased digoxin effect, toxicity Change in GI flora
Warfarin Increased warfarin effect, toxicity Change in GI flora
Dolutegravir with
Antacids Decreased dolutegravir exposure with polyvalent cation containing Decreased absorption
medications
Carbamazepine Decreased dolutegravir exposure Increased metabolism
Efavirenz Decreased dolutegravir exposure Increased metabolism
Etravirine Decreased dolutegravir exposure Increased metabolism
Fosamprenavir Decreased dolutegravir exposure Increased metabolism
Metformin Increased metformin exposure Tubular secretion inhibition
Nevirapine Decreased dolutegravir exposure Increased metabolism
Oxcarbazepine Decreased dolutegravir exposure Increased metabolism
Phenobarbital Decreased dolutegravir exposure Increased metabolism
Phenytoin Decreased dolutegravir exposure Increased metabolism
St. John’s wort Decreased dolutegravir exposure Increased metabolism
Tripanavir Decreased dolutegravir exposure Increased metabolism
Doripenem with
Probenecid Increased doripenem exposure Tubular secretion inhibition
Valproic acid Decreased valproic acid exposure Mechanism not established
Efavirenz with
Acenocoumarol Decreased acenocoumarol effect Increased metabolism
Amiodarone Decreased amiodarone effect Increased metabolism
Barbiturates Decreased barbiturate, efavirenz effects Increased metabolism
Bupropion Decreased bupropion effect Increased metabolism
Benzodiazepines (BZDs) Decreased BZI effect Increased metabolism
CBZ Decreased CBZ, efavirenz effects Increased metabolism
Continued
692

Clarithromycin Increased efavirenz effect, toxicity Decreased metabolism

Corticosteroids Decreased efavirenz, steroid effects Increased metabolism
Cyclosporine Decreased cyclosporine effect; increased efavirenz effect, toxicity Increased/decreased metabolism
Ergot alkaloids Increased ergot effect, toxicity Decreased metabolism
Erythromycin Increased efavirenz effect, toxicity Decreased metabolism
Fluconazole Increased efavirenz effect, toxicity Decreased metabolism
Fluoxetine Increased risk of serotonin syndrome Decreased metabolism
Garlic supplements Decreased efavirenz effect Increased metabolism
Indinavir Decreased indinavir concentrations Increased metabolism
Itraconazole Decreased itraconazole effect; increased efavirenz effect, toxicity Increased/decreased metabolism
Ketoconazole Decreased ketoconazole effect; increased efavirenz effect, toxicity Increased/decreased metabolism
Methadone Decreased methadone effect; withdrawal Increased metabolism
Oral contraceptives Decreased contraceptive effect Increased metabolism
Paclitaxel Decreased paclitaxel effect Increased metabolism
Phenytoin Decreased phenytoin, efavirenz effects Increased metabolism
Repaglinide Decreased repaglinide effect Increased metabolism
Rifamycins Decreased efavirenz effect Increased metabolism
Ritonavir Decreased ritonavir concentration Increased metabolism
St. John’s wort Decreased efavirenz effect Increased metabolism
Warfarin Decreased warfarin effect Increased metabolism
Zidovudine Decreased zidovudine concentration Increased metabolism
Elvitegravir/Cobicistat/Emtricitabine/Tenofovir with
Alfuzosin Increased alfuzosin exposure Decreased metabolism
Cisapride Cardiac arrhythmias Decreased metabolism
Ergotamine derivatives Life-threatening ergot toxicity Decreased metabolism
Lovastatin Myopathy including rhabdomyolysis Decreased metabolism
Midazolam (PO) Prolonged sedation or respiratory depression Decreased metabolism
Pimozide Cardiac arrhythmias Decreased metabolism
Rifampin Decreased elvitegravir exposure Increased metabolism
Sildenafil Visual disturbance, syncope, priapism, and hypotension Decreased metabolism
Simvastatin Myopathy including rhabdomyolysis Decreased metabolism
St. John’s wort Decreased elvitegravir exposure Increased metabolism
Triazolam Prolonged sedation or respiratory depression Decreased metabolism
Entecavir with
Probenecid Increased entecavir exposure Tubular secretion inhibition
Ertapenem with
Probenecid Increased ertapenem effect, toxicity Decreased tubular secretion
Erythromycin with
Alfentanil Increased alfentanil toxicity Decreased metabolism
Bromocriptine Increased toxicity Increased bioavailability
BZDs Increased BZD toxicity Decreased metabolism
CBZ Increased CBZ toxicity Decreased metabolism
Cisapride Cardiotoxicity Decreased metabolism
Clindamycin Antagonism Target site competition
Clozapine Increased clozapine toxicity Decreased metabolism
Corticosteroids Increased steroid effect, toxicity Decreased excretion
Cyclosporine Increased cyclosporine toxicity Decreased metabolism
Digoxin Increased digoxin effect Decreased GI metabolism and increased
absorption
Disopyramide Cardiac arrhythmias Decreased metabolism
Ergot alkaloids Increased ergot toxicity Mechanism not established
Felodipine Increased toxicity Decreased metabolism
HMG-CoA reductase inhibitors Increased risk of rhabdomyolysis Decreased clearance
Loratadine Increased loratadine exposure, toxicity Decreased metabolism
Lidocaine Decreased clearance; increased monoethylglycinexylidide (MEGX) Decreased metabolism
concentration
Phenytoin Possible increased or decreased effect Altered metabolism
Ritonavir Increased erythromycin toxicity Decreased metabolism
693


Tacrolimus Increased tacrolimus toxicity Decreased metabolism
Theophylline Increased theophylline effect and possible toxicity Decreased metabolism
Trimetrexate Increased trimetrexate toxicity Decreased metabolism
Valproic acid Increased toxicity Decreased metabolism
Vinblastine Increased vinblastine toxicity Decreased metabolism
Zafirlukast Decreased zafirlukast effect Mechanism not established
Ethionamide with
Aminosalicylic acid Increased GI distress, hepatotoxicity Mechanism not established
Cycloserine Increased neurotoxicity Additive toxicity
Ethambutol Increased ethambutol toxicity Mechanism not established
Isoniazid Increased neurotoxicity Additive toxicity
Pyrazinamide Increased hepatotoxicity Additive toxicity
Rifampin, rifabutin Increased hepatotoxicity Additive toxicity
Etravirine with
Antiarrhythmic agents Decreased antiarrhythmic exposure Metabolism induction
Anticonvulsants Decreased etravirine exposure, effect Metabolism induction
Atazanavir/ritonavir Increased etravirine and decreased atazanavir concentrations, Metabolism inhibition and induction
effects
Clarithromycin Decreased clarithromycin and increased 14-hydroxyclarithromycin Metabolism induction
exposures
Darunavir/ritonavir Decreased etravirine exposure Metabolism induction
Dexamethasone Decreased etravirine exposure Mechanism not established
Diazepam Increased diazepam exposure Metabolism inhibition
Fluconazole Increased etravirine exposure Metabolism inhibition
Fosamprenavir/ritonavir Increased amprenavir exposure, toxicity Metabolism inhibition
HMG-CoA reductase inhibitors Decreased lovastatin, simvastatin, increased fluvastatin exposures Metabolism induction, inhibition
Immunosuppressants Possible decreased cyclosporine, sirolimus, and tacrolimus Metabolism induction
exposures
Itraconazole Increased etravirine, decreased itraconazole exposures Metabolism inhibition, induction
Ketoconazole Increased etravirine, decreased ketoconazole exposures Metabolism inhibition, induction
Lopinavir/ritonavir Increased etravirine exposure Metabolism inhibition
Methadone Minimal change —
Non-nucleoside reverse transcriptase Decreased etravirine exposure with efavirenz or nevirapine, Metabolism induction, inhibition
inhibitors increased etravirine exposure with delavirdine
Phosphodiesterase inhibitors Possible decreased sildenafil effect Mechanism not established
Posaconazole Increased etravirine exposure Metabolism inhibition
Protease inhibitors Must ensure low-dose ritonavir is given with any etravirine/ Mechanism not established
protease inhibitor combinations
Rifamycins Decreased etravirine exposures Metabolism induction
Ritonavir Significant decrease in etravirine exposure Metabolism induction
Saquinavir/ritonavir Decrease etravirine exposure Metabolism induction
St. John’s wort Decreased etravirine exposure Metabolism induction
Tipranavir/ritonavir Decreased etravirine effect Metabolism induction
Voriconazole Increased etravirine and voriconazole exposures Metabolism competition, inhibition
Warfarin Increased warfarin exposure Metabolism inhibition
Fluconazole with
Amitriptyline Increased amitriptyline toxicity Decreased metabolism
Amphotericin B Possible antagonism in animal models Mechanism not established
BZDs Increased CNS toxicity Decreased metabolism
Cimetidine Decreased fluconazole effect Decreased bioavailability
Cisapride Increased risk of cardiotoxicity Decreased metabolism
Coumarin anticoagulants Increased prothrombin times Mechanism not established
Cyclosporine Increased cyclosporine concentration Mechanism not established
Dihydropyridines Increased dihydropyridine toxicity Decreased metabolism
Etravirine Increased etravirine concentration Metabolism inhibition
HMG-CoA reductase inhibitors Increased risk of rhabdomyolysis Mechanism not established
Phenytoin Increased phenytoin concentration Decreased metabolism
Quetiapine Possible increased quetiapine concentration Decreased metabolism
Rifampin/rifabutin Decreased fluconazole concentration Mechanism not established
Continued
694

Sulfonylureas Increased plasma concentration, decreased metabolism of Mechanism not established

tolbutamide, glyburide, glipizide
Thiazides Increased fluconazole concentrations and AUC of fluconazole Decreased renal clearance
Zidovudine Increased zidovudine concentrations Decreased metabolism
Fluoroquinolones with
Antacids Decreased fluoroquinolone effect with aluminum or magnesium Decreased absorption
antacids
Anticoagulants, oral Prolonged prothrombin times Mechanism not established
Chloramphenicol Inhibition in vitro of norfloxacin bactericidal activity Mechanism not established
Cyclosporine Increased risk of nephrotoxicity; increased serum cyclosporine Mechanism not established
concentration
DDI Decreased fluoroquinolone effect Decreased GI absorption
Iron Decreased serum fluoroquinolone concentration Decreased GI absorption
Mineral fortified foods Decreased fluoroquinolone concentration Decreased GI absorption
Nitrofurantoin Decreased norfloxacin activity In vitro antagonism
NSAIDs Possible increased risk of CNS stimulation Mechanism not established
Oral contraceptives Possible decreased effect of trovafloxacin, moxifloxacin Increased metabolism of quinolones
Oral hypoglycemics Increased incidence, severity of hypoglycemia Unknown mechanism with gatifloxacin
Pirenzepine Decreased rate of fluoroquinolone absorption Mechanism not established
Probenecid Increased serum concentrations; prolonged AUCs Decreased tubular secretion
Rifampin/rifabutin Inhibition in vitro of norfloxacin bactericidal activity Mechanism not established
Riluzole Increased risk of riluzole toxicity Decreased elimination
Ropivacaine Increased risk of ropivacaine toxicity Decreased metabolism
Scopolamine Decreased rate of fluoroquinolone absorption Mechanism not established
Sucralfate Decreased serum fluoroquinolone concentration Decreased GI absorption
Tetracycline Inhibition in vitro of norfloxacin bactericidal activity Mechanism not established
Theophylline Possible theophylline toxicity Decreased metabolism
Zinc Decreased serum fluoroquinolone concentrations Decreased GI absorption
Fosamprenavir with
Antacids Decreased amprenavir exposure Mechanism not established
Antiarrhythmics Increased antiarrhythmic exposure, toxicity Metabolism interaction
Anticonvulsants Decreased amprenavir exposure, increased anticonvulsant Metabolism site competition
exposure
Azole antifungals Increased azole and amprenavir exposures Metabolism interaction
BZDs Increased benzodiazepine exposure, toxicity Metabolism interaction
Calcium channel blockers Increased calcium channel blocker exposures, toxicity Metabolism interaction
Cisapride Increased cisapride exposure, toxicity Metabolism interaction
Oral contraceptives Decreased amprenavir concentration, change in oral contraceptive Metabolism interaction
exposure
Corticosteroids Increased corticosteroid exposure Metabolism interaction
CYP3A4 inhibitors Increased amprenavir exposure Metabolism interaction
Delavirdine Increased amprenavir and decreased delavirdine exposures Metabolism interaction
Dexamethasone Decreased amprenavir exposure Metabolism interaction
Efavirenz/ritonavir Increased amprenavir exposure Metabolism interaction
Ergot derivatives Increased ergot exposure, toxicity Metabolism interaction
Esomeprazole Increased esomeprazole exposure Metabolism interaction
H2 receptor antagonists Decreased amprenavir exposure Mechanism not established
HMG-CoA reductase inhibitors Increased HMG-CoA exposure, toxicity, decreased amprenavir Metabolism interaction
exposure
Immunosuppressants Increased immunosuppressant exposure Metabolism interaction
Indinavir Increase in amprenavir and decrease in indinavir exposures Metabolism interaction
Lopinavir/ritonavir Decreased amprenavir, increased lopinavir-ritonavir exposures Metabolism interaction
Methadone Decreased amprenavir and methadone exposures Metabolism interaction
Nevirapine Decreased amprenavir, increased nevirapine exposures Metabolism interaction
Opiates Increased opiate exposure, toxicity Metabolism interaction
Paroxetine Decreased paroxetine exposure Metabolism interaction
Phenytoin Decreased phenytoin exposure Metabolism interaction
Phosphodiesterase inhibitors Increased phosphodiesterase inhibitor exposure, toxicity Metabolism interaction
Pimozide Increased pimozide exposure, toxicity Metabolism interaction
Ranolazine Increased ranolazine exposure, toxicity Metabolism interaction
695


Rifabutin Increased rifabutin and amprenavir exposures Metabolism interaction
Rifampin Decreased amprenavir exposure Metabolism interaction
Saquinavir Decreased amprenavir exposure Metabolism interaction
St. John’s wort Decreased amprenavir exposure Metabolism interaction
Trazodone Increased trazodone exposure, toxicity Metabolism interaction
Tricyclic antidepressants Increased tricyclic exposure, toxicity Metabolism interaction
Warfarin Possible change in warfarin exposure Mechanism not established
Zidovudine Increased amprenavir and zidovudine exposures Metabolism interaction
Foscarnet with
Acyclovir Increased nephrotoxicity Additive toxicity
Cotrimoxazole Increased nephrotoxicity Additive toxicity
Pentamidine Increased nephrotoxicity; increased hypocalcemia Additive toxicity
Probenecid Increased foscarnet serum concentration; increased possibility of Decreased tubular secretion
adverse effects
Suramin Increased nephrotoxicity Additive toxicity
Furazolidone with
Alcohol Disulfiram-like effect Either inhibition of aldehyde dehydrogenase or
inhibition of monoamine oxidase
Antidepressants Increased adverse effects Additive
Sympathomimetics Hypertensive crisis Increased norepinephrine availability
Ganciclovir/Valganciclovir with
Amphotericin B Increased nephrotoxicity; replication inhibition of rapidly dividing Additive toxicity; additive
host cells
Cotrimoxazole Replication inhibition of rapidly dividing host cells Additive
Cyclosporine Increased nephrotoxicity Additive toxicity
Cytotoxic antineoplastics Replication inhibition of rapidly dividing host cells Additive
Dapsone Replication inhibition of rapidly dividing host cells Additive
DDI Increased DDI effect, toxicity Increased bioavailability
Flucytosine Replication inhibition of rapidly dividing host cells Additive
Imipenem Generalized seizures Mechanism not established
Immunosuppressives Increased suppression of bone marrow and immune system Additive toxicity
Nucleoside analogues Replication inhibition of rapidly dividing host cells Additive
Pentamidine Replication inhibition of rapidly dividing host cells Additive
Probenecid Increased ganciclovir concentration; prolonged AUC Decrease in tubular secretion
Pyrimethamine Replication inhibition of rapidly dividing host cells Additive
Tacrolimus Increased risk of nephrotoxicity Additive toxicity
Zidovudine In vitro antiretroviral antagonism; increased risk of hematologic Mechanism not established; additive toxicity
toxicity
Griseofulvin with
Alcohol Increased alcohol effects, tachycardia and flushing Mechanism not established
Anticoagulants, oral Decreased anticoagulant effect Mechanism not established
Contraceptives, oral Decreased contraceptive effect Increased metabolism
Phenobarbital Decreased griseofulvin concentrations Decreased absorption or hepatic enzyme
induction
Halofantrine with
Grapefruit juice Increased Q-T interval prolongation Decreased metabolism
Hydroxychloroquine with
Digoxin Increased digoxin effect Mechanism not established
Imipenem with
Aztreonam Antagonism β-Lactamase induction
Cephalosporins Antagonism β-Lactamase induction
Chloramphenicol Antagonism; administer a few hr after imipenem Mechanism not established
Cyclosporine Increased cyclosporine and imipenem/cilastatin exposures, toxicities Mechanism not established
Extended-spectrum penicillins Antagonism β-Lactamase induction
Ganciclovir Generalized seizures Mechanism not established
Probenecid Increased imipenem/cilastatin exposure Decreased tubular secretion
Interferon Alfa with
Captopril Increased hematologic toxicity Mechanism not established
Colchicine Decreased interferon alfa-2a effect Mechanism not established
Enalapril Increased hematologic toxicity Mechanism not established
Continued
696

Theophylline Increased theophylline effect, toxicity Mechanism not established

Zidovudine Increased risk of hematologic toxicity Additive toxicity
Isoniazid (INH) with
Alcohol Increased incidence of hepatitis Mechanism not established
Decreased INH effect in some alcoholic patients Increased metabolism
Aluminum antacids Decreased INH effect Decreased absorption
Aminosalicylic acid Increased INH concentration Reduced acetylation
Anticoagulants, oral Possible increased anticoagulant effect Decreased metabolism
BCG vaccine Vaccine may be ineffective INH inhibits multiplication of BCG
BZDs Pharmacologic effects of BZDs may be increased; documented Decreased metabolism
with diazepam and triazolam
CBZ Increased toxicity of both drugs Altered metabolism
Cycloserine CNS effects, dizziness, drowsiness Mechanism not established
Disulfiram Psychotic episodes, ataxia Altered dopamine metabolism
Enflurane Possible nephrotoxicity Increased metabolism of enflurane caused
increased fluoride concentration
Ethionamide Increased CNS adverse effects Additive
Itraconazole Decreased itraconazole activity Increased metabolism
Ketoconazole Decreased ketoconazole effect Decreased concentration
Meperidine Increased risk of serotonin syndrome Additive toxicity
Phenytoin/fosphenytoin Increased phenytoin toxicity Decreased metabolism
Rifampin/rifabutin Possible increased INH hepatotoxicity Possible increased toxic metabolites
Selective serotonin reuptake inhibitor (SSRI) Increased risk of serotonin syndrome Additive toxicity
antidepressants
Itraconazole with
Alfentanil Increased alfentanil exposure Decreased metabolism
Amphotericin B In vitro antagonism Mechanism not established
Antacids Possible decreased itraconazole bioavailability Mechanism not established
Anticoagulants, oral Increased anticoagulant effect Decreased metabolism
Aripiprazole Increased aripiprazole exposure Decreased metabolism
Barbiturates Decreased itraconazole effect Increased metabolism
Buspirone Increased buspirone exposure Metabolism interaction
BZDs Increased CNS effects Decreased metabolism
CBZ Decreased itraconazole effect Increased metabolism
Celiprolol Increased celiprolol effect Increased absorption via P-glycoprotein (PGP)
Clarithromycin Increased itraconazole exposure Decreased metabolism
Corticosteroids Increased corticosteroid exposure Metabolism interaction
Cyclosporine Possible increased cyclosporine concentrations Mechanism not established
DDI Decreased itraconazole effect Decreased bioavailability
Digoxin Increased digoxin toxicity Decreased metabolism
Dihydropyridines Increased dihydropyridine effect Decreased metabolism
Docetaxel Increased docetaxel exposure Decreased metabolism
Dofetilide Increased dofetilide effect, toxicity Decreased metabolism
Eletriptan Increased eletriptan exposure Decreased metabolism
Ergot alkaloids Increased ergot alkaloid exposure, toxicity Metabolism interaction
Erythromycin Increased itraconazole exposure Decreased metabolism
H2 receptor antagonists Decreased itraconazole bioavailability Decreased gastric acidity
HMG-CoA reductase inhibitors Increased risk of rhabdomyolysis Decreased metabolism
Nevirapine Decreased itraconazole exposure Increased metabolism
Omeprazole/lansoprazole Decreased itraconazole bioavailability Decreased gastric acidity
Oral hypoglycemics Increased oral hypoglycemic effects Decreased metabolism
Phenytoin Decreased itraconazole effect Increased metabolism
Phosphodiesterase inhibitors Increased phosphodiesterase inhibitor exposure Decreased metabolism
Protease inhibitors Increased protease inhibitor exposure, increased itraconazole Decreased metabolism
exposure
Rifamycins Decreased systemic bioavailability of itraconazole Hepatic enzyme induction
Sirolimus Increased sirolimus exposure Decreased metabolism
697


Tolterodine Increased tolterodine exposure Decreased metabolism
Trimetrexate Increased trimetrexate exposure Decreased metabolism
Vinca alkaloids Increased vinca toxicity Mechanism not established
Ketoconazole with (see Itraconazole for Others)
Alcohol Possible disulfiram-like reaction Mechanism not established
Antacids Decreased ketoconazole effect Decreased absorption
Anticoagulants, oral Increased anticoagulant effect Mechanism not established
BZDs Increased CNS toxicity Decreased metabolism
Corticosteroids Increased methylprednisolone effect Decreased metabolism
Cyclosporine Increased concentration of cyclosporine in blood Mechanism not established
Delavirdine Increased delavirdine concentration Mechanism not established
DDI Decreased ketoconazole effect Decreased absorption
Dihydropyridines Increased dihydropyridine effect Decreased metabolism
Donepezil Increased cholinomimetic effects Decreased metabolism
H2 receptor antagonists Possible decreased antifungal effect Decreased absorption
Hepatotoxic agents Increased hepatotoxicity Additive toxicity
Indinavir Increased indinavir toxicity Decreased metabolism
INH Decreased ketoconazole effect Decreased blood concentrations
Loratadine Increased loratadine concentration Decreased metabolism
Omeprazole/lansoprazole Decreased ketoconazole bioavailability Decreased gastric acidity
Phenytoin Altered effects of one or both drugs Altered metabolism
Quetiapine Increased risk of quetiapine toxicity Decreased metabolism
Rifampin/rifabutin Decreased rifampin and ketoconazole effects Decreased blood concentration
Ritonavir Increased ketoconazole concentration Decreased metabolism
Saquinavir Increased saquinavir concentration Decreased metabolism
Theophylline Decreased theophylline concentration Mechanism not established
Lamivudine with
Nelfinavir Increased lamivudine concentration Decreased clearance
Pentamidine Increased risk of pancreatitis Additive toxicity profiles
Sulfonamides Increased lamivudine concentration Decreased clearance
Trimethoprim Increased lamivudine concentration Decreased clearance
Trimethoprim/sulfamethoxazole Increased risk of pancreatitis Additive toxicity profiles
Zidovudine Increased zidovudine concentration Mechanism not established
Linezolid with
Adrenergic agents Increased adrenergic agent effects Mechanism not established
Bupropion Increased bupropion exposure, toxicity Mechanism not established
Entacapone/tolcapone Decreased catecholamine metabolism Mechanism not established
Monoamine oxidase (MAO) inhibitors Increased MAO inhibitor actions, toxicity Additive toxicity
Meperidine Increased risk of serotonin syndrome Decreased serotonin degradation
Selective norepinephrine-serotonin reuptake Increased risk of serotonin syndrome Decreased serotonin degradation
inhibitor (SNRI) antidepressants
SSRI antidepressants Increased risk of serotonin syndrome Decreased serotonin degradation
Tramadol Increased risk of seizures Mechanism not established
Tricyclic antidepressants Increased risk of serotonin syndrome Mechanism not established
Triptans Increased triptan exposure, toxicity Metabolism interaction
Maraviroc with
CYP3A inhibitors Increased maraviroc exposure CYP3A inhibition
CYP3A inducers Decreased maraviroc exposure CYP3A induction
Mebendazole with
CBZ Decreased mebendazole concentrations Hepatic microsomal enzyme induction
Phenytoin Decreased mebendazole concentrations Hepatic microsomal enzyme induction
Meropenem with
Probenecid Increased meropenem effect, toxicity Decreased tubular secretion
Continued
698

Methenamine with
Sulfonamides Increased risk of crystalluria; precipitate formation between Acidification of the urine
formaldehyde and sulfamethizole
Metronidazole with
Alcohol Mild disulfiram-like symptoms Possible inhibition of intermediary metabolism of
alcohol
Anticoagulants, oral Increased anticoagulant effect Decreased metabolism
Azathioprine Transient neutropenia Mechanism not established
Barbiturates Decreased metronidazole effect with phenobarbital Probably increased metabolism
Cimetidine Possible increased metronidazole toxicity Decreased metabolism
Disulfiram Organic brain syndrome Mechanism not established
Fluorouracil Transient neutropenia Mechanism not established
Lithium Lithium toxicity Mechanism not established
Micafungin with
Cyclosporine Increased cyclosporine exposure Mechanism not established
Itraconazole Increased itraconazole exposure Mechanism not established
Nifedipine Increased nifedipine exposure Mechanism not established
Sirolimus Increased sirolimus exposure Mechanism not established
Miconazole with
Aminoglycosides Possible decreased tobramycin concentration Mechanism not established
Amphotericin B Possible antagonism in in vitro studies Mechanism not established
Cisapride Increased cardiotoxicity Decreased metabolism
Cyclosporine Increased nephrotoxicity Decreased metabolism
Hypoglycemics, sulfonylurea Severe hypoglycemia Mechanism not established
Phenytoin Increased phenytoin toxicity Decreased metabolism
Nalidixic Acid with
Antacids Decreased nalidixic acid effect Decreased bioavailability
Anticoagulants, oral Increased anticoagulant effect Displacement from binding sites
Nevirapine with
Acenocoumarol Decreased acenocoumarol effect Increased metabolism
Amiodarone Decreased amiodarone effect Increased metabolism
Barbiturates Decreased barbiturate, nevirapine effects Increased metabolism
Bupropion Decreased bupropion effect Increased metabolism
BZDs Decreased BZD effect Increased metabolism
CBZ Decreased CBZ, nevirapine effects Increased metabolism
Cimetidine Increased nevirapine effect, toxicity Decreased metabolism
Clarithromycin Increased nevirapine effect, toxicity Decreased metabolism
Corticosteroids Decreased nevirapine, steroid effects Increased metabolism
Cyclosporine Decreased cyclosporine effect; increased nevirapine effect, toxicity Increased, decreased metabolism
Erythromycin Increased nevirapine effect, toxicity Decreased metabolism
Garlic supplements Decreased nevirapine effect Increased metabolism
Indinavir Decreased indinavir concentration Increased metabolism
Itraconazole Decreased itraconazole effect; increased nevirapine effect, toxicity Increased, decreased metabolism
Ketoconazole Decreased ketoconazole effect; increased nevirapine effect, Increased, decreased metabolism
toxicity
Methadone Decreased methadone effect; withdrawal Increased metabolism
Oral contraceptives Decreased contraceptive effect Increased metabolism
Paclitaxel Decreased paclitaxel effect Increased metabolism
Phenytoin Decreased phenytoin, nevirapine effects Increased metabolism
Repaglinide Decreased repaglinide effect Increased metabolism
Rifamycins Decreased nevirapine effect Increased metabolism
Ritonavir Decreased ritonavir concentrations Increased metabolism
St. John’s wort Decreased nevirapine effect Increased metabolism
Warfarin Decreased warfarin effect Increased metabolism
Zidovudine Decreased zidovudine concentration Increased metabolism
Nitrofurantoin with
Antacids Possible decreased nitrofurantoin effect Decreased absorption
Fluoroquinolones In vitro antagonism of quinolone activity Mechanism not established
699


Probenecid Increased nitrofurantoin serum concentration Inhibition of renal excretion
Sulfinpyrazone Increased nitrofurantoin serum concentration Inhibition of renal excretion
Pentamidine with
Amphotericin B Increased nephrotoxicity Additive toxicity
Capreomycin Increased nephrotoxicity Additive toxicity
Foscarnet Hypocalcemia Mechanism not established
Grepafloxacin Increased cardiotoxicity Additive toxicity
Sparfloxacin Increased cardiotoxicity Additive toxicity
Piperazine with
Chlorpromazine Seizures Mechanism not established
Pyrantel pamoate Decreased piperazine and pyrantel pamoate activity Antagonism
Polymyxin B with
Aminoglycoside antibiotics Increased nephrotoxicity; increased neuromuscular blockade Additive toxicity
Neuromuscular blocking agents Increased neuromuscular blockade Additive toxicity
Parenteral quinidine Increased neurotoxicity Additive toxicity
Parenteral quinine Increased neurotoxicity Additive toxicity
Posaconazole with
Astemizole Increased astemizole effect, toxicity Decreased metabolism
BZDs Increased benzodiazepine effect, toxicity Decreased metabolism
Calcium channel blockers Increased calcium channel blocker effect, toxicity Decreased metabolism
Cimetidine Decreased posaconazole effect Unknown mechanism
Halofantrine Increased halofantrine effect, toxicity Decreased metabolism
HMG-CoA reductase inhibitors Increased statin effect, toxicity Decreased metabolism
Immunosuppressants Increased immunosuppressant effect, toxicity Decreased metabolism
Phenytoin Decreased posaconazole effect, increased phenytoin effect, toxicity Metabolism interaction
Rifabutin Decreased posaconazole effect, increased rifabutin effect, toxicity Metabolism interaction
Terfenadine Increased terfenadine effect, toxicity Decreased metabolism
Vinca alkaloids Increased vinca effect, toxicity Decreased metabolism
Primaquine with
Aurothioglucose Increased blood dyscrasias Additive
Quinacrine Increased toxicity to the antimalarial Additive
Ritonavir Increased primaquine concentrations Decreased metabolism
Protease Inhibitors (except Ritonavir) with
Alfentanil Increased alfentanil effects, toxicity Decreased metabolism
Amiodarone Increased amiodarone toxicity Decreased metabolism
Antacids Decreased efficacy of indinavir, tipranavir Decreased bioavailability
Antiarrhythmic agents Increased antiarrhythmic effects, toxicities Decreased metabolism
Astemizole Increased cardiotoxicity Decreased metabolism
Atorvastatin Increased AUC and statin side effects Decreased metabolism
Azithromycin Possible decreased nelfinavir efficacy PGP interaction
Barbiturates Decreased protease effect, increased barbiturate effect, toxicity Increased, decreased metabolism
Bepridil Increased bepridil effects, toxicity Decreased metabolism
Bupropion Possible increased bupropion toxicity Decreased metabolism
BZDs Increased CNS BZD toxicity Decreased metabolism
Calcium channel antagonists Increased calcium channel blocker effects Decreased metabolism
CBZ Decreased protease effect, increased CBZ effect Increased, decreased metabolism
Cisapride Increased cardiotoxicity Decreased metabolism
Clarithromycin Increased protease toxicity Decreased metabolism
Clindamycin Increased clindamycin toxicity Decreased metabolism
Continued
700

Corticosteroids Increased risk of hypercorticoidism Decreased metabolism

Coumarin derivatives Increased coumarin derivative toxicity Decreased metabolism
Cyclophosphamide Increased cyclophosphamide toxicity, decreased protease effect Decreased, increased metabolism
Cyclosporine Increased protease, cyclosporine toxicity Decreased metabolism
Dapsone Increased dapsone toxicity with saquinavir Decreased metabolism
Daunorubicin Increased risk of cardiotoxicity Decreased metabolism
Delavirdine Increased protease toxicity, increased hepatotoxicity, decreased Decreased metabolism
delavirdine effect
Desipramine Increased desipramine effect, toxicity Decreased metabolism
Diltiazem Increased diltiazem effect, toxicity Decreased metabolism
Dihydropyridines Increased dihydropyridine toxicity Decreased clearance
Doxorubicin Increased risk of cardiotoxicity Decreased metabolism
Ergot derivatives Increased ergot toxicity Decreased metabolism
Erythromycin Increased erythromycin, protease effect, toxicity Decreased metabolism
Fluconazole Possible decreased effect indinavir, increased effect nelfinavir Increased, decreased metabolism
Fusidic acid Increased saquinavir, fusidic acid toxicity Decreased metabolism
Garlic supplements Decreased protease effect Increased metabolism
Gamma-hydroxybutyrate (GHB) Increased GHB toxicity Decreased metabolism
Grapefruit juice Decreased indinavir effect, increased saquinavir effect Increased, decreased metabolism
H2 receptor antagonists Decreased indinavir effect Decreased bioavailability
Ifosfamide Increased ifosfamide toxicity Decreased metabolism
Interferon alfa-2 Increased indinavir toxicity Decreased metabolism
Isotretinoin Increased isotretinoin effect, toxicity Decreased metabolism
Itraconazole Increased itraconazole, protease effect, toxicity Decreased metabolism
Ketoconazole Increased ketoconazole, protease effect, toxicity Decreased metabolism
Levodopa Increased levodopa effect, toxicity Decreased metabolism
Lidocaine Increased risk of lidocaine toxicity Decreased metabolism
Loperamide Decreased protease efficacy Decreased bioavailability
Lovastatin Increased AUC and statin side effects Decreased metabolism
Methadone Decreased methadone, protease effect Increased metabolism
Metronidazole Increased metronidazole effect, toxicity Decreased metabolism
Nefazodone Increased nefazodone effect, toxicity Decreased metabolism
Oral contraceptives Altered efficacy of birth control possible Increased, decreased metabolism
Paclitaxel Increased effect, toxicity of paclitaxel Decreased metabolism
Phenytoin Decreased protease, increased phenytoin effects Increased, decreased metabolism
Phosphodiesterase inhibitors Increased phosphodiesterase inhibitor effect, toxicity Decreased metabolism
Pimozide Increased pimozide toxicity Decreased metabolism
Pravastatin Decreased pravastatin effect or nothing Possible increased metabolism
Primidone Decreased protease effect Increased metabolism
Proton pump inhibitors Decreased effect of indinavir Decreased bioavailability
Raloxifene Possible decreased raloxifene effect with nelfinavir Increased metabolism
Ranolazine Increased ranolazine effect, toxicity Decreased metabolism
Repaglinide Increased repaglinide exposure, effects Decreased metabolism
Rifampin/rifabutin Decreased protease effect, increased rifamycin toxicity Increased, decreased metabolism
Risperidone Increased risperidone toxicity Decreased metabolism
Ritonavir Increased protease toxicity Decreased metabolism
Simvastatin Increased AUC and statin toxicity Decreased metabolism
SSRI antidepressants Increased SSRI effect, toxicity Decreased metabolism
St. John’s wort Decreased protease effect Increased metabolism
Verapamil Increased verapamil effect, toxicity Decreased metabolism
Zolpidem Increased zolpidem effect, toxicity Decreased metabolism
Pyrantel Pamoate with
Piperazine Decreased pyrantel pamoate and piperazine activity Antagonism
Theophylline Increased theophylline toxicity Decreased metabolism
Quinacrine with
Alcohol Possible disulfiram-like reaction Accumulation of acetaldehyde
701


Hepatotoxic agents Possible increased hepatotoxicity Additive
Primaquine Increased primaquine toxicity Release from tissue binding sites causing marked
increase in primaquine concentrations
Quinine with
Acetazolamide Increased quinine serum concentration; increased toxicity Decreased clearance from increased urinary pH
Aluminum antacids Decreased quinine serum concentration Decreased absorption
Anticoagulants, oral Potentiation of hypoprothrombinemic effects Hepatic suppression of synthesis of vitamin
K–dependent clotting factors
Astemizole Increased cardiotoxicity Decreased metabolism
Cimetidine Decreased quinine clearance; prolonged AUCs Hepatic enzyme inhibition
Digoxin/digitoxin Increased digoxin, digitoxin concentration Mechanism not established
Flecainide Increased flecainide toxicity Decreased metabolism
Heparin Decreased anticoagulant effect Mechanism not established
Mefloquine Increased cardiac events Additive
Neuromuscular blocking agents Potentiation of neuromuscular blocking effects Additive
Ritonavir Increased quinine toxicity Decreased metabolism
Sodium bicarbonate Increased quinine serum concentration; increased toxicity Decreased clearance from increased urinary pH
Raltegravir with
Atazanavir Increased raltegravir exposure Metabolism inhibition
Rifampin Decreased raltegravir exposure Metabolism induction
Tipranavir/ritonavir Decreased raltegravir exposure Metabolism induction
Ribavirin with
Abacavir Increased risk of lactic acidosis Mechanism not established
DDI Increased risk of lactic acidosis Mechanism not established
Lamivudine Increased risk of lactic acidosis Mechanism not established
Stavudine Increased risk of lactic acidosis Mechanism not established
Zalcitabine Increased risk of lactic acidosis; in vitro retroviral antagonism Mechanism not established; decreased
phosphorylation
Zidovudine Increased risk of lactic acidosis; in vitro retroviral antagonism Mechanism not established; decreased
phosphorylation
Warfarin Decreased warfarin exposure Mechanism not established
Rifamycins (except Rifaximin) with
Analgesics Possible decreased analgesic effect Increased metabolism
Anticoagulants, oral Possible decreased oral anticoagulant effect Increased metabolism
Anticonvulsants Possible decreased anticonvulsant effect Increased metabolism
Atovaquone Decreased atovaquone effect Increased metabolism
Barbiturates Possible decreased barbiturate effect Increased metabolism
β-Blockers Possible decreased β-blocker effect Increased metabolism
Cardiac glycosides Possible decreased cardiac glycoside effect Increased metabolism
Chloramphenicol Possible decreased chloramphenicol effect Increased metabolism
Clarithromycin Decreased clarithromycin concentration, increased rifamycin Increased, decreased metabolism
toxicity
Clofibrate Possible decreased clofibrate effect Increased metabolism
Contraceptives, oral Possible decreased oral contraceptive effect Increased metabolism
Corticosteroids Possible decreased corticosteroid effect Increased metabolism
Cyclosporine Possible decreased cyclosporine effect Increased metabolism
Dapsone Possible decreased dapsone effect Increased metabolism
Delavirdine Decreased delavirdine concentration, increased rifamycin toxicity Increased, decreased metabolism
Diazepam Possible decreased diazepam effect Increased metabolism
Digitalis Decreased digitoxin and digoxin effects Increased metabolism
Dihydropyridines Decreased dihydropyridine effect Increased metabolism
Disopyramide Possible decreased disopyramide effect Increased metabolism
Doxycycline Decreased doxycycline effect Increased metabolism
Estrogens Decreased estrogen concentrations Hepatic enzyme induction
Ethionamide Increased hepatotoxicity Additive
Fluconazole Decreased fluconazole effect Increased metabolism
HMG-CoA reductase inhibitors Decreased HMG effect Increased metabolism
Hypoglycemics, oral Possible decreased oral hypoglycemic effect Increased metabolism
Indinavir Decreased indinavir effect; increased rifamycin exposure Increased metabolism; decreased metabolism
Isoniazid Possible increased hepatotoxicity Possible increased toxic metabolites
Continued
702

Itraconazole Decreased itraconazole effect Increased metabolism

Ketoconazole Possible decreased ketoconazole effect Increased metabolism
Mexiletine Possible decreased mexiletine effect Increased metabolism
Narcotics Possible decreased narcotic effect Increased metabolism
Nelfinavir Decreased nelfinavir effect Increased metabolism
Nevirapine Decreased nevirapine effect Increased metabolism
Praziquantel Decreased praziquantel effect Increased metabolism
Progestins Possible decreased progestin effect Increased metabolism
Quinidine Possible decreased quinidine effect Increased metabolism
Ritonavir Decreased ritonavir effect, increased rifamycin toxicity Increased, decreased metabolism
Saquinavir Decreased saquinavir effect, increased rifamycin toxicity Increased, decreased metabolism
Tacrolimus Decreased tacrolimus effect Increased metabolism
Terbinafine Decreased terbinafine effect Increased metabolism
Theophylline Possible decreased theophylline effect Increased metabolism
Verapamil Possible decreased verapamil effect Increased metabolism
Zidovudine Decreased zidovudine concentrations, AUCs Mechanism not established
Rilpivirine with
Antacids Decreased rilpivirine exposure Decreased absorption
Delavirdine Increased rilpivirine exposure Decreased metabolism
Efavirenz Decreased rilpivirine exposure Increased metabolism
Etravirine Decreased rilpivirine exposure Increased metabolism
H2 receptor antagonists Decreased rilpivirine exposure Decreased absorption
Macrolides Increased rilpivirine exposure Decreased metabolism
Methadone Decreased methadone exposure Increased metabolism
Nevirapine Decreased rilpivirine exposure Increased metabolism
Ritonavir Increased rilpivirine exposure Decreased metabolism
Triazole antifungals Increased rilpivirine exposure Decreased metabolism
Ritonavir, Lopinavir/Ritonavir same as with all Protease Inhibitors Plus
Albendazole Altered albendazole efficacy Increased or decreased metabolism
Alimemazine Increased alimemazine, ritonavir effect, toxicity Decreased metabolism
Atovaquone Decreased atovaquone effect Increased phase II metabolism
Chlorpromazine Increased ritonavir, chlorpromazine effect, toxicity Decreased metabolism
Clozapine Decreased clozapine effect Increased metabolism
Codeine Decreased analgesic effect Decreased metabolism
Dextropropoxyphene Increased dextropropoxyphene effect, toxicity Decreased metabolism
Digoxin Increased digoxin effect, toxicity Decreased clearance
Disopyramide Increased disopyramide effect, toxicity Decreased metabolism
Disulfiram Disulfiram-like reactions Alcohol in protease dosage forms
Encainide Increased encainide effect, toxicity Decreased metabolism
Ethosuximide Increased ethosuximide effect, toxicity Decreased metabolism
Fentanyl Increased fentanyl effect, toxicity Decreased metabolism
Flecainide Increased flecainide effect, toxicity Decreased metabolism
Fusidic acid Increased ritonavir, fusidic acid effect, toxicity Decreased metabolism
Gemfibrozil Increased ritonavir effect, toxicity Mechanism not established
Haloperidol Increased haloperidol effect, toxicity Decreased metabolism
Loratadine Increased risk of loratadine toxicity Decreased metabolism
Meperidine Increased risk of normeperidine toxicity Increased metabolism of parent
Methadone Decreased methadone effect Increased metabolism
MDMA (3,4-methyl- Increased MDMA toxicity Decreased metabolism
enedioxymethamphetamine)
Metoprolol Increased metoprolol effect, toxicity Decreased metabolism
Metronidazole Disulfiram-like reactions Alcohol in protease dosage forms
Mexiletine Increased mexiletine effect, toxicity Decreased metabolism
Morphine Decreased morphine effect Increased metabolism
Olanzapine Decreased olanzapine effect Increased metabolism
Perphenazine Increased perphenazine, ritonavir effect, toxicity Decreased metabolism
Prochlorperazine Increased prochlorperazine, ritonavir effect, toxicity Decreased metabolism
Promethazine Increased promethazine, ritonavir effect, toxicity Decreased metabolism
Propafenone Increased propafenone effect, toxicity Decreased metabolism
Quinine Increased quinine effect, toxicity Decreased metabolism
Tamoxifen Increased tamoxifen effect, toxicity Decreased metabolism
703


Thalidomide Increased thalidomide effect, toxicity Decreased metabolism
Theophylline Decreased theophylline effect Increased metabolism
Thioridazine Increased thioridazine, ritonavir effect, toxicity Decreased metabolism
Timolol Increased timolol effect, toxicity Decreased metabolism
Tramadol Increased tramadol effect, toxicity Decreased metabolism
Tricyclic antidepressants Increased tricyclic effect, toxicity Decreased metabolism
Trifluoperazine Increased trifluoperazine, ritonavir effect, toxicity Decreased metabolism
Triflupromazine Increased triflupromazine, ritonavir effect, toxicity Decreased metabolism
Roxithromycin with
Digoxin Increased digoxin effect, toxicity Change in gut flora
Warfarin Increased warfarin effect, toxicity Change in gut flora
Spectinomycin with
Lithium Increased lithium toxicity Decreased renal excretion
Stavudine (D4T) with
Aurothioglucose Increased peripheral neuropathy Additive toxicity
Chloramphenicol Increased peripheral neuropathy Additive toxicity
Cisplatin Increased peripheral neuropathy Additive toxicity
Clarithromycin Possible decreased stavudine effect Decreased bioavailability (?)
Dapsone Increased peripheral neuropathy Additive toxicity
Disulfiram Increased peripheral neuropathy Additive toxicity
Ethionamide Increased peripheral neuropathy Additive toxicity
Fluconazole Possible decreased stavudine effect Decreased bioavailability (?)
Glutethimide Increased peripheral neuropathy Additive toxicity
Hydralazine Increased peripheral neuropathy Additive toxicity
INH Increased peripheral neuropathy Additive toxicity
Iodoquinol Increased peripheral neuropathy Additive toxicity
Methadone Decreased stavudine effect Decreased bioavailability
Metronidazole Increased peripheral neuropathy Additive toxicity
Nitrofurantoin Increased peripheral neuropathy Additive toxicity
Pentamidine Increased pancreatitis Additive toxicity
Phenytoin Increased peripheral neuropathy Additive toxicity
Ribavirin Increased peripheral neuropathy Additive toxicity
Rifabutin Decreased stavudine effect Decreased bioavailability (?)
Trimethoprim/sulfamethoxazole Increased pancreatitis Additive toxicity
Vincristine Increased peripheral neuropathy Additive toxicity
Sulfadoxine/Pyrimethamine with
Aurothioglucose Increased hematologic toxicity Additive toxicity
Lorazepam Mild hepatotoxicity Mechanism not established
Para-aminobenzoic acid (PABA) Decreased pyrimethamine effect Interference with pyrimethamine action
Sulfonamides Increased toxicity Additive toxicity
Trimethoprim Increased toxicity Additive toxicity
Sulfonamides with
Antibiotics Altered action of sulfasalazine Alteration of intestinal flora
Anticoagulants, oral Increased anticoagulant effect Decreased metabolism and displacement from
binding sites
Barbiturates Increased thiopental effect Decreased albumin binding
Chloroprocaine Possible antagonism of sulfonamide action Competition for PABA site
Cyclosporine Decreased cyclosporine effect with sulfamethazine Possible increased metabolism
Digoxin Possible decreased digoxin effect with sulfasalazine Decreased digoxin absorption
Folic acid Decreased absorption, metabolism, and concentrations with Inhibition of hepatic folate metabolism, intestinal
sulfasalazine transport of folic acid, and jejunal brush border
folate conjugase
Hypoglycemics, sulfonylurea Increased hypoglycemic effect Mechanism not established
Iron Decreased sulfasalazine serum concentration Chelation
Lamivudine Increased lamivudine toxicity Competition for renal clearance
Methenamine Crystallization of sulfonamides in the urine; precipitate of Acidification of the urine
formaldehyde, sulfamethizole
Methotrexate Possible increased methotrexate toxicity Decreased renal clearance and displacement from
binding
MAO inhibitors Possible increased phenelzine toxicity with sulfisoxazole Decreased metabolism
PABA Possible antagonism of sulfonamide action Competition for PABA site
Continued
704

Paraldehyde Crystallization of sulfonamides in the urine Acidification of the urine

Phenytoin Increased phenytoin effect, except possibly with sulfisoxazole Decreased metabolism
Piperocaine Possible antagonism of sulfonamide action Competition for PABA site
Procaine Possible antagonism of sulfonamide action Competition for PABA site
Propoxycaine Possible antagonism of sulfonamide action Competition for PABA site
Sulfinpyrazone Increased serum sulfonamide concentration Displacement from protein binding sites and
inhibition of tubular secretion
Tetracaine Possible antagonism of sulfonamide action Competition for PABA site
Thiopental Increased thiopental effect; decreased dose necessary when given Plasma protein binding competition
with sulfisoxazole
Teicoplanin with
Aminoglycosides Increased risk of nephrotoxicity, ototoxicity Additive toxicities
Amphotericin B Increased risk of nephrotoxicity, ototoxicity Additive toxicities
Cisplatin Increased risk of nephrotoxicity, ototoxicity Additive toxicities
Colistin Increased risk of nephrotoxicity, ototoxicity Additive toxicities
Cyclosporine Increased risk of nephrotoxicity, ototoxicity Additive toxicities
Loop diuretics Increased risk of nephrotoxicity, ototoxicity Additive toxicities
Telaprevir
Triazolam Prolonged sedation or respiratory depression Decreased metabolism
Telithromycin with
Antiarrhythmic agents Increased risk of cardiac arrhythmias Additive toxicities
BZDs Increased benzodiazepine effect, toxicity Decreased metabolism
Coumarin derivatives Increased coumarin effect, toxicity Change in GI flora
CYP3A4 inducers Decreased telithromycin effect Metabolism induction
Digoxin Increased digoxin effect, toxicity Change in GI flora
Itraconazole Increased telithromycin effect, toxicity Decreased metabolism
Ketoconazole Increased telithromycin effect, toxicity Decreased metabolism
Theophylline Increased theophylline effect, toxicity Decreased metabolism
Tenofovir with
DDI Increased DDI effect, toxicity Mechanism not established
Terbinafine with
Caffeine Increased caffeine effect, toxicity Decreased metabolism
Cimetidine Increased terbinafine effect, toxicity Decreased metabolism
Cyclosporine Decreased cyclosporine effect Increased metabolism
Rifampin Decreased terbinafine effect Increased metabolism
Tetracyclines with
Alcohol Decreased doxycycline effect in alcoholics Increased metabolism
Aminoglycosides In vitro antagonism; no in vivo support Mechanism not established
Antacids, oral Decreased oral tetracycline effects Decreased tetracycline absorption
Antidepressants, tricyclic Localized hemosiderosis with amitriptyline and minocycline Possible synergism
Barbiturates Decreased doxycycline effect Increased metabolism
Bismuth subsalicylate Decreased tetracycline effect Decreased absorption
CBZ Decreased doxycycline effect Increased metabolism
Contraceptives, oral Decreased contraceptive effect Possible decreased enterohepatic circulation of
estrogen
Digoxin Increased digoxin effect Decreased gut metabolism and increased
absorption
705


Iron, oral Decreased tetracycline effect, but not with doxycycline; decreased Decreased absorption
iron effect
Kaolin/pectin Decreased concentrations of tetracyclines Decreased absorption
Lithium Increased lithium toxicity Decreased renal excretion
Methotrexate Possible increased toxicity Mechanism not established
Methoxyflurane Increased nephrotoxicity Displacement from binding
Molindone Decreased tetracycline effect Calcium as an excipient inhibits absorption
Penicillins In vitro antagonism; rare in vivo support for this Mechanism not established
Phenformin Increased lactic acidosis Possible decreased phenformin excretion
Phenytoin Decreased doxycycline effect Increased metabolism
Rifampin/rifabutin Possible decreased doxycycline effect Increased metabolism
Theophylline Possible theophylline toxicity Mechanism not established
Zinc sulfate Decreased tetracycline effect Decreased absorption
Thiabendazole with
Theophylline Increased theophylline toxicity Decreased metabolism
Tinidazole with
Alcohol Increased alcohol side effects Decreased metabolism
Anticoagulants Increased anticoagulant effects Decreased metabolism
Cholestyramine Decreased tinidazole effect, toxicity Decreased absorption
CYP3A4 inducers Decreased tinidazole effect, toxicity Increased metabolism
CYP3A4 inhibitors Increased tinidazole effect, toxicity Decreased metabolism
Disulfiram Increased CNS toxicity Mechanism unknown
Fluorouracil Increased fluorouracil effect, toxicity Decreased clearance
Hydantoins Increased IV phenytoin effect, toxicity Mechanism unknown
Lithium Increased lithium effect, toxicity Mechanism unknown
Oxytetracycline Decreased tinidazole effect Antagonism
Trimethoprim with
Angiotensin-converting enzyme (ACE) Hyperkalemia Reduced potassium clearance
inhibitors
Amiloride Trimethoprim may potentiate hyponatremia because of Additive toxicity
concomitant use of amiloride with thiazide diuretics
Azathioprine Leukopenia Mechanism not established
Cerivastatin Increased risk of statin toxicity Inhibition of CYP2C8 metabolism
Cyclosporine Increased nephrotoxicity Synergism
Dapsone Increased dapsone toxicity Altered clearance
Digoxin Possible increased digoxin effect Decreased renal excretion and possibly decreased
metabolism
Methotrexate (MTX) Increased MTX toxicity Decreased clearance
Phenytoin Increased phenytoin serum concentrations—increased risk of Decreased metabolism; additive toxicity
phenytoin toxicity; increased risk of folate deficiency
Thiazide diuretics Trimethoprim may potentiate hyponatremia because of Additive toxicity
concomitant use of amiloride with thiazide diuretics
Tripanavir with
Vancomycin with
Aminoglycosides Possible increased nephrotoxicity and ototoxicity Possibly additive toxicity
Amphotericin B Increased nephrotoxicity Additive toxicity
Bacitracin Increased nephrotoxicity Additive toxicity
Cephalosporins Increased nephrotoxicity Additive toxicity
Continued
706

Digoxin Possible decreased digoxin effect Possibly decreased absorption

Paromomycin Increased nephrotoxicity Additive toxicity
Warfarin Increased risk of bleeding Mechanism not established
Vidarabine with
Allopurinol Increased nephrotoxicity Decreased metabolism
Theophylline Increased theophylline effect Decreased metabolism
Voriconazole with
Amprenavir Increased amprenavir/voriconazole effect, toxicity Decreased metabolism
Atorvastatin Increased atorvastatin effect, toxicity Decreased metabolism
Barbiturates Decreased voriconazole effect Increased metabolism
BZDs Increased BZD effect, toxicity Decreased metabolism
Calcium channel antagonists Increased calcium channel antagonist effect, toxicity Decreased metabolism
CBZ Decreased voriconazole effect Increased metabolism
Cerivastatin Increased cerivastatin effect, toxicity Decreased metabolism
Fosphenytoin, phenytoin Increased phenytoin effect, toxicity; decreased voriconazole effect Decreased, increased metabolism
Lovastatin Increased lovastatin effect, toxicity Decreased metabolism
Nelfinavir Increased nelfinavir, voriconazole effect, toxicity Decreased metabolism
Non-nucleoside reverse transcriptase Increased NNRTI effect, toxicity Decreased metabolism
inhibitors (NNRTIs)
Omeprazole Increased omeprazole effect, toxicity Decreased metabolism
Rifamycins Increased rifamycin effect, toxicity; decreased voriconazole effect Decreased, increased metabolism
Ritonavir Increased ritonavir, voriconazole effect, toxicity Decreased metabolism
Saquinavir Increased saquinavir, voriconazole effect, toxicity Decreased metabolism
Simvastatin Increased simvastatin effect, toxicity Decreased metabolism
Sulfonylureas Increased sulfonylurea effect, toxicity Decreased metabolism
Vinca alkaloids Increased vinca effect, toxicity Decreased metabolism
Zidovudine (ZDV) with
Acetaminophen Granulocytopenia Mechanism not established
Acyclovir Neurotoxicity Mechanism not established
Amphotericin B Increased risk of nephrotoxicity, hematologic toxicity Additive toxicity
Antimycobacterials Possible increased risk of hematologic toxicity Decreased phase II ZDV metabolism
Aspirin Possible increased risk of hematologic toxicity Decreased phase II ZDV metabolism
Atovaquone Possible increased risk of hematologic toxicity Decreased phase II ZDV metabolism
Chloramphenicol Possible increased risk of hematologic toxicity Decreased phase II ZDV metabolism
Cimetidine Possible increased risk of hematologic toxicity Decreased phase II ZDV metabolism
Clarithromycin Decreased ZDV concentrations and AUCs Mechanism not established
Cytotoxic/myelosuppressive agents Increased risk of hematologic toxicity Additive toxicity
Dapsone Increased neutropenia Additive toxicity
Fluconazole Increased risk of hematologic toxicity Decreased phase I metabolism
Flucytosine Increased hematologic toxicity Additive toxicity
Ganciclovir Decreased ZDV effect; hematologic toxicity Increased clearance; additive toxicity
Hydroxycarbamide Increased hematologic toxicity Additive toxicity
Indomethacin Possible increased risk of hematologic toxicity Mechanism not established; additive
Interferon alfa Increased hematologic toxicity Additive toxicity
Interferon beta Increased hematologic toxicity Additive toxicity
Methadone Increased risk of hematologic toxicity Decreased phase II ZDV metabolism
Nephrotoxic agents Increased risk of toxicity Increased serum concentrations; decreased
clearance
Nucleoside analogues Increased risk of hematologic toxicity Additive toxicity
Oral contraceptives Increased risk of hematologic toxicity Decreased phase II ZDV metabolism
Oxazepam Possible increased risk of hematologic toxicity Decreased phase II ZDV metabolism
Phenytoin Increased risk of hematologic toxicity Decreased clearance
707


Primaquine Increased risk of peripheral neuropathy Additive toxicity
Probenecid Increased risk of hematologic toxicity Decreased clearance, phase II metabolism
Pyrazinamide Decreased effect of pyrazinamide Mechanism not established
Pyrimethamine Increased hematologic toxicity Additive toxicity
Ribavirin In vitro antiretroviral antagonism Decreased phosphorylation of ZDV
Rifabutin Increased hematologic toxicity Additive toxicity
Rifamycins Decreased ZDV effect Increased phase II ZDV metabolism
Sulfadiazine Increased hematologic toxicity Additive toxicity
Trimethoprim Increased risk of hematologic toxicity Decreased ZDV clearance
Trimethoprim/sulfamethoxazole Increased hematologic toxicity Additive toxicity
Valproic acid Increased ZDV effect, toxicity Decreased phase II ZDV metabolism
*This table includes significant adverse drug interactions and is not a comprehensive list of all potential adverse drug interactions.
Pharmacokinetic drug-drug interactions can occur via a number of • Patients with a low genetic potential to make a drug-metabolizing
different mechanisms. These include the following: enzyme or transporter (poor or intermediate metabolizers/
• Reduction of drug absorption by concurrent drugs. The most transporters) have a small chance of an induction interaction
common absorption interactions occur by chelation of an anti- because they do not have the genetic potential to make more of
infective with a cation such as calcium, magnesium, or iron. A useful the enzyme or transporter when stimulated to do so.
rule of thumb is that oral anti-infectives should not be administered • Patients with normal or high genetic potential to make a drug-
1 hour before or 2 hours after the administration of oral divalent or metabolizing enzyme or transporter are at greater risk of an induc-
trivalent cations unless a study has clearly demonstrated a lack of tion interaction due to the greater genetic potential to make the
significant interaction with their co-administration. enzyme or transporter.
• Displacement from protein-binding sites: Although this interaction • Patients can undergo enzyme heterocyclic activation of a drug-
in theory could enhance anti-infective tissue distribution and effi- metabolizing enzyme, which increases the activity of the enzyme
cacy, homeostasis occurs in these types of drug interactions, result- approximately 33% where the peak effect occurs immediately,
ing in no substantial change in drug exposure due to increased drug unlike induction, which can take up to 2 weeks for the peak effect
elimination of unbound drug. to be seen. Heterocyclic activation is most often seen with CYP3A
• Inhibition or induction of drug-metabolizing enzymes or trans isozymes and CYP2B6.
porters: These drug interactions are by far the most important seen • Over the course of many infectious diseases, patients with infec-
in clinical practice. Most information on drug-drug interactions tions (acute and chronic) have the potential to substantially change
is generated in a limited number of individuals, often healthy over time in terms of their risk of drug-drug interactions; thus,
volunteers, and is usually not applicable to the general population. this is not a static process.
Some basic tenants of these drug interactions are important to We have provided a table of inducers, inhibitors, and substrates for
remember: important drug-metabolizing enzymes and transporters. Data on drug
• Genetic and environmental factors, as well as the microbiome interactions and transporters are much more limited and less under-
composition, can affect the baseline activity of drug-metabolizing stood because specific probes and biomarkers for transporters are not
enzymes and transporters and thus will affect the potential for well developed and validated.
drug-drug interactions. Although clinicians request a specific recommendation for dosage
• Not all patients experience a drug-drug interaction, even if this adjustment when a drug-drug interaction is identified, it is virtually
has been described in the literature. This is determined by both impossible to provide a specific recommendation due to the previously
genetic and environmental factors. mentioned factors. An approach that incorporates appropriate treat-
• Patients with low or null drug-metabolizing enzymes or trans- ment of an infection with the goal of optimizing efficacy, reducing the
porter activity have a low chance of drug-drug interactions; risk of resistance, and finally, attempting to avoid toxicity is recom-
however, if this low baseline activity is due to a reversible patho- mended. Being familiar with the toxic side effects of anti-infectives and
logic process, the potential for drug-drug interaction will increase how to monitor them is essential.
as the pathologic process is appropriately treated.
• Patients with normal or high drug-metabolizing enzymes or ACKNOWLEDGMENT
transporter activity have a high likelihood of drug-drug The authors acknowledge the previous work of the late Dr. Guy Amsden
interactions. for his compilation of several tables that are included in this chapter.
Suggested Readings Matzke GR, McGory RW, Halstenson CE, Keane WF. Pharmaco-
kinetics of vancomycin in patients with various degrees of renal
Seo SK, Nafziger AN. Non-genetic influences on drug metabo-
lism. In: Bertino JS Jr, Kashuba ADM, Ma JD, et al, eds. Phar-
Bennett WM, Arnoff GR, Berns JS, eds. Drug prescribing in renal
function. Antimicrob Agents Chemother. 1984;25:433-437. macogenomics: An Introduction and Clinical Perspective. 1st
failure: dosing guidelines for adults. 5th ed. Philadelphia:
Morrish GA, Pai MP, Green B. The effects of obesity on drug ed. New York: McGraw Hill; 2012.
American College of Physicians; 2007.
pharmacokinetics in humans. Expert Opin Drug Metab Stevens LA, Levey AS. Use of the MDRD study equation to
International Transporter Consortium, Giacomini KM, Huang
Toxicol. 2011;7:697-706. estimate kidney function for drug dosing. Clin Pharmacol
SM, et al. Membrane transporters in drug development. Nat
Pai MP. Drug dosing based on weight and body surface area: Ther. 2009;86:465-467.
Rev Drug Discov. 2010;9:215-236.
mathematical assumptions and limitations in obese adults. Verbeeck RK. Pharmacokinetics and dosage adjustment in
Lalonde RL, Wagner JA. Drug development perspective
Pharmacotherapy. 2012;32:856-868 patients with hepatic dysfunction. Eur J Clin Pharmacol.
on pharmacokinetic studies of new drugs in patients
Piscitelli SC, Rodvold KA, Pai MP, eds. Drug Interactions in 2008;64:1147-1161.
with renal impairment. Clin Pharmacol Ther. 2009;86:
Infectious Diseases. 3rd ed. New York: Humana Press; 2011.
557-561.

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Tables of Anti-infective Agent

Chapter 54 Tables of Anti-infective Agent Pharmacology

TABLE 54-1 Index of Tables Included in This Chapter

Anti-infective Names (organized alphabetically)

TABLE 54-2 Generic and Trade Names

TABLE 54-2 Generic and Trade Names—cont’d

Chapter 54 Tables of Anti-infective Agent Pharmacology

TABLE 54-2 Generic and Trade Names—cont’d

Clarithromycin Biaxin, Biaxin XL, Biclar, Klacid, Prevpac,* Zeclar Macrolide

TABLE 54-2 Generic and Trade Names—cont’d

Chapter 54 Tables of Anti-infective Agent Pharmacology

TABLE 54-2 Generic and Trade Names—cont’d

Oseltamivir phosphate Tamiflu Antiviral

TABLE 54-2 Generic and Trade Names—cont’d

Chapter 54 Tables of Anti-infective Agent Pharmacology

TABLE 54-3 Trade and Generic Names

TABLE 54-3 Trade and Generic Names—cont’d

Altabax Retapamulin Anti-impetigo

TABLE 54-3 Trade and Generic Names—cont’d

Chapter 54 Tables of Anti-infective Agent Pharmacology

TABLE 54-3 Trade and Generic Names—cont’d

Declomycin Demeclocycline hydrochloride Tetracycline

TABLE 54-3 Trade and Generic Names—cont’d

Chapter 54 Tables of Anti-infective Agent Pharmacology

TABLE 54-3 Trade and Generic Names—cont’d

Kesso-pen* Penicillin G/phenoxymethyl penicillin Penicillins

TABLE 54-3 Trade and Generic Names—cont’d

Chapter 54 Tables of Anti-infective Agent Pharmacology

TABLE 54-3 Trade and Generic Names—cont’d

Podomexef Cefpodoxime proxetil Cephalosporin

TABLE 54-3 Trade and Generic Names—cont’d

Chapter 54 Tables of Anti-infective Agent Pharmacology

TABLE 54-3 Trade and Generic Names—cont’d

Valcyte Valganciclovir Antiviral

TABLE 54-4 Penicillin Dosage Forms

Chapter 54 Tables of Anti-infective Agent Pharmacology

TABLE 54-5 Cephalosporin Dosage Forms

TABLE 54-5 Cephalosporin Dosage Forms—cont’d

Chapter 54 Tables of Anti-infective Agent Pharmacology

TABLE 54-11 Quinolone and Urinary Anti-infective Dosage Forms

TABLE 54-12 Antimycobacterial Dosage Forms

TABLE 54-12 Antimycobacterial Dosage Forms—cont’d

TABLE 54-13 Antifungal Dosage Forms

TABLE 54-14 Antiparasitic Dosage Forms

TABLE 54-14 Antiparasitic Dosage Forms—cont’d

Chapter 54 Tables of Anti-infective Agent Pharmacology

TABLE 54-15 Antiviral Dosage Forms*

TABLE 54-16 Antiretroviral Dosage Forms

TABLE 54-17 Anti-infective Agent Pharmacology: Penicillins

SERUM AND URINE Newborn

Peak or Dose (g)/Interval Serious

Chapter 54 Tables of Anti-infective Agent Pharmacology

STANDARD DOSE WITH DOSING

1 9 1.5-3.0 6-8 6-8 8-12 24

1 5 1.5-2.6 2-4 4-6 4-6 8 12 3 13.38

0.7-1.4 7.4-21 0.4-1.6 12 12 12 65-75 1.7-3.6 17

TABLE 54-17 Anti-infective Agent Pharmacology: Penicillins—cont’d

SERUM AND URINE Newborn

Peak or Dose (g)/Interval Serious

Penicillin V 0.25 PO 2.3-2.7 0.25-0.5 2 25,000-

STANDARD DOSE WITH DOSING

Chapter 54 Tables of Anti-infective Agent Pharmacology

0.6-1.3 2.1-6 2.1-6 3-4 4-6 4-6 8 12 1 g post, 1 3000-

0.5-2 4-6 6 8 12 7.5-15 mg/kg 60 7

0.5-2 24 8-25 mg/ 4-15 mg/kg 3-15 mg/ None <1 <10 0.2

0.125-0.5 12 12 12 0.25 g 0.75 15 mg/kg 17-88 20-33 ≤3 35-80 10-14

0.75-1.5 8 8 8-12 0.75 g

13.5 19 0.5-2 8-12 12-24 24 0.25-0.5 0.25 1-2 q48h 0.5 mg/1 L

7.5 mg/ 8-12 8-12 12-48 ≥484 4-5 mg/kg 3.75 mg/ 43 50 35 Minimal

2-2.2 mg/ 8 8-12 12-48 484 2 mg/kg 21-26 Minimal

0.5-1 12 7.5 mg/kg 7.5 mg/kg 7.5 mg/kg 0.5 g 20 10-40 <25 40-300 Minimal

Erythromycin base7,8 0.25 PO 0.1-2 0.25-0.5 q6h 2 30-50 mg/kg/day

0.1 12 12 12 12 0.1 g 0.1 g 26 30-40 200-3200 10-13

0.1 12 12 12 12 0.1 g 0.1 g 77 8-26 200-3200 17

Evernimicin 6 mg/kg IV 49-55 1-12 mg/kg/