PHARMACOLOGY

SPECIFIC ANTIBIOTICS SHIFT 3

REVIEWER 1
REVIEWER | MAY 2020

OUTLINE LEGEND
I. Beta lactam drugs C. Lincosamides
A. Penicillins D. Streptogramins
B. Cephalosporins E. Chloramphenicol
C. Monobactams F. Oxazolidinones MUST KNOW SAMPLEX
D. Carbapenems G. Aminoglycosides  
II. Glycopeptide antibiotics IV. Sulfonamides
III. Inhibitors of bacterial protein synthesis V. Trimethoprim-Sulfamethoxazole
A. Tetracycline VI. Fluoroquinolones
B. Macrolides VII. Metronidazole

PENICILLINS
DRUGS MOT ACTIVITY / CLINICAL USES PK/PD ADVERSE EFFECTS MECHANISM OF
RESISTANCE 
NARROW • Bactericidal DOC: syphilis (PEN G)  • Pen G • Allergic reactions  • Inactivation of
SPECTRUM • Cell wall • Streptococci → Crystalline/Aqueous (IV) • Diarrhea  antibiotic β-
Penicillin G synthesis → Streptococcus pyogenes (skin → Procaine, Benzathine (IM) → Ampicillin lactamase
Penicillin V inhibitors: and soft tissue infection) • Pen V → Co-amoxiclav • Modification of
binds to → Susceptible streptococcus → Oral • Maculopapular rash target PBPs
penicillin- pneumoniae → Poor bioavailability even on • Nausea and vomiting • Impaired
binding • Staphylococci empty stomach → Co-amoxiclav in children penetration of drug
protein → Non-β-lactamase → Administer 1-2 hours before • Pseudomembranous colitis 
to target PBPs
(PBP) staphylococcus aureus or after a meal • Antibiotic efflux
causing → Ampicillin
• Enterococcus faecalis • Time-dependent killing
inhibition of • Hematologic disturbance
• Neisseria meningitidis
transpeptida • Anaphylactic shock
• Leptospira spp.
se → IgE-mediated
• Actinomyces
→ Skin testing recommended for
• Other uses: pharyngitis (Pen V) patients with history of penicillin
reaction
VERY NARROW • “Anti-Staphylococcal Penicillins” • IV: Nafcillin, oxacillin • Interstitial nephritis
SPECTRUM • Methicillin-sensitive S. aureus • Oral: Cloxacillin (acid-stable) → Methicillin
Nafcillin (MSSA) • Time-dependent killing • Neutropenia
Oxacillin • NO activity against Enterococci → Nafcillin
Cloxacillin and Gram (-)  → Reversible
• Hepatitis
BROAD • Susceptible S. pneumoniae • IV: Ampicillin → Oxacillin
SPECTRUM • NO activity against P. aeruginosa • Oral: Amoxicillin (not impaired → Reversible
Amoxicillin • Other uses (Ampicillin) by food) , Ampicillin (lower • Seizures 
Ampicillin → Shigella spp. bioavailability compared to Amox)
→ ↑ concentrations of β-lactams
→ Salmonella typhi • Time-dependent killing in the CNS
→ E. coli
→ Listeria monocytogenes
→ Enterococcus faecalis

EXTENDED • Pseudomonas aeruginosa  • IV: Piperacillin, Ticarcillin

SPECTRUM → Piperacillin > Ticarcillin • Time-dependent killing
Reviewer 3.1 PREPARED BY: Rayos, Al Kim and Suarez, Rina 1 of 13
 PHARMA REVIEWER 1: Specific Antibiotics 2 of 13

Piperacillin • Enterococcus faecalis

Ticarcillin → Piperacillin > Ticarcillin
• Enterobacteriaceae
→ Broader coverage compared to
aminopenicillins (amox and
ampi)

BETA • UTI, otitis media, sinusitis • IV: Ampicillin + Sulbactam,

LACTAMASE • URTI, LRTI, bones, joints, and soft Piperacillin + Tazobactam
INHIBITORS tissue infections • Oral: Co-amoxiclav (unstable in
Amoxicillin + • Nosocomial pneumonia parenteral form), Sultamicillin
Clavulanic Acid (prodrug of Ampi + Sulbactam)
Ampicillin + • Time-dependent killing
Sulbactam
Piperacillin +
Tazobactam

CEPHALOSPORINS
DRUGS MOT ACTIVITY / CLINICAL USES PK/PD ADVERSE EFFECTS
1st Gen • Bactericidal • Active against Gram (+) organisms including staph. and strep. (minor skin • Oral: Cephalexin • Thrombophlebitis
Cephalexin • Cell wall and soft tissue infections) • IV: Cefazolin • Cefaclor: serum-sickness like
Cefazolin synthesis • Surgical prophylaxis  except for colorectal procedure: Cefazolin • Does not enter CSF reaction (rash and arthritis)
inhibitors: • Prophylaxis for recurrent UTI: Cephalexin • Renal excretion • Cefoperazone: moderate to
binds to severe diarrhea
2nd Gen penicillin- • Same spectrum of activity as 1st gen but improved activity against Gram (-) • Oral: Cefaclor, Cefuroxime • Allergy or hypersensitivity
Cefaclor binding protein organisms resistant to the 1st gen including Klebsiella spp. axetil reactions
Cefuroxime (PBP) causing → H. influenza: Cefuroxime and Cefaclor  • IV: Cefoxitin, Cefuroxime → Patients with hx of
Cefoxitin inhibition of • Does not cross BBB anaphylaxis to penicillins,
→ Serratia or B. fragilis: Cefoxitin 
transpeptidase • Cefaclor is more susceptible SHOULD NOT receive
• Surgical prophylaxis in colorectal surgery + appendectomy: Cefoxitin
• More stable to to β-lactamase hydrolysis first and second
many bacterial • CAP: Cefuroxime 
→ Usefulness is generation
β lactamases → Active against β-lactamase-producing H. influenza, K. pneumoniae, cephalosporins
and most pneumococci diminished
→ Third and fourth gen
→ Active against penicillin-non-susceptible pneumococci CAN BE GIVEN but
• NO activity against Pseudomonas  should be monitored
cautiously
3rd Gen • Expanded Gram (-) coverage compared to 2nd gen agents including • Oral: Cefixime, Cefpodoxime • Cefamandole, Cefmetazole,
Cefoperazone Providencia and Serratia marcescens • IV: Ceftriaxone, Ceftazidime, Cefotetan, Cefoperazone:
Cefotaxime • Effective against β-lactamase-producing strains of Neisseria, Haemophilus Cefotaxime, Cefoperazone → Hypoprothrombinemia
Ceftazidime Proteus, Klebsiella, and E. coli • Some can cross BBB: and bleeding disorder
Ceftriaxone • Active against P. aeruginosa: Ceftazidime and Cefoperazone  (₱) Ceftriaxone + Cefotaxime → Disulfiram-like reactions
Cefixime • Not reliably active against Enterobacter spp. & ESBL • Penetrate the body fluids and 
Cefpodoxime • Cefixime: less active against pneumococci + poor activity against S. aureus tissues well
• Ceftriaxone and Cefotaxime • Excreted in urine except:
→ Treatment of meningitis Cefoperazone and
→ Penicillin-non-susceptible strains of pneumococci Ceftriaxone (biliary tract) 
• Ceftazidime: neutropenic febrile immunocompromised patients
• Reserved for serious infections except:
→ Ceftriaxone (parenteral) and Cefixime (oral)  for gonorrhea
 PHARMA REVIEWER 1: Specific Antibiotics 3 of 13

4th Gen • Gram (+) activity of 1st gen + wider Gram (-) spectrum of 3rd gen • IV only
Cefepime • Good activity against P. aeruginosa, Enterobacter, S. aureus, and S. • Widely distributed in body
pneumoniae fluids and tissues
• More resistant to hydrolysis of β-lactamases but hydrolyzed by ESBL • Renal excretion
• Highly active against Haemophilus and Neisseria sp.
• Has better activity against most penicillin-non-susceptible strains of
streptococci compared with Ceftazidime
• Useful in treatment of Enterobacter infections 
• Used in severe infections due to susceptible Gram (-) resistant to other
cephalosporins
• Used in severe, mixed Gram (+) and Gram (-) infections
• Empiric monotherapy in febrile neutropenic patients 

5th Gen • Good activity against MRSA 

Ceftaroline • Some activity against Enterococci and Gram (-) spectrum like Ceftriaxone
• NO activity against ESBL
• Approved for treatment of skin and soft tissue infections and CAP
• CURRENTLY NOT AVAILABLE IN THE PHILIPPINES! 

MONOBACTAM
MOT ACTIVITY CLINICAL USES PK/PD ADVERSE EFFECTS
• Bactericidal • pseudoMONAs  • Limited to patients allergic to • IV • GI toxicity with possible
• Cell wall • enteroBACTer  penicillin with serious infections such • Poor oral absorption superinfections
synthesis • limited to Gram (-) bacteria as pneumonia, meningitis, and • Widely distributed in body • Vertigo and headache
inhibitors: → E. coli sepsis caused by susceptible Gram fluids and tissues • NO cross-allergenicity with
binds to → Serratia (-) pathogens  penicillin
penicillin- → Proteus • EXHIBITS cross-reactivity
binding protein → Salmonella with CEFTAZIDIME due to
(PBP) causing → Hemophilus similarity in structure
inhibition of → Klebsiella
transpeptidase
• No G+ and anaerobes coverage 
• Closely resembles activity of aminoglycoside

CARBAPENEMS
DRUGS MOT ACTIVITY / CLINICAL USES PK/PD ADVERSE EFFECTS
Doripenem • Bactericidal • Extended-spectrum β-lactamase (ESBL)-producing Gram (-) bacteria • IV • Nausea and vomiting
Imipenem • Cell wall • Serious mixed aerobic and anaerobic infections • Imipenem is inactivated by • Diarrhea
Meropenem synthesis • Enterobacter spp. renal dehydropeptidases • Skin rashes
Ertapenem inhibitors: • Penicillin-nonsusceptible strains of pneumococci → Given with • Seizures
binds to • Good activity against many Gram (-), Gram (+), and anaerobes CILASTATIN to → ↑ concentrations of
penicillin- → Gram (+): Imipenem > other carbapenems prolong half-life and IMIPENEM in patients
binding protein → Gram (-): Doripenem and meropenem > other carbapenems decrease with renal failure
(PBP) causing • P. aeruginosa and Acinetobacter nephrotoxicity • Adverse effects are more
inhibition of → Ertapenem is less active • Widely distributed in body common in IMIPENEM 
transpeptidase fluids and tissues
• Febrile neutropenic patients (except Ertapenem)
• NO activity against MRSA 
 PHARMA REVIEWER 1: Specific Antibiotics
DRUGS MOT
Vancomycin • Bactericidal
• Cell wall synthesis inhibitors:
binds firmly to D-Ala-D-ala
terminus of nascent
peptidoglycan pentapeptide
Telavancin
Daptomycin • Cell wall synthesis inhibitor:
depolarizes the cell
membrane with K+ efflux
leading to rapid cell death
Fosfomycin • Cell wall synthesis inhibitor:
inhibits cytosolic enolpyruvate
transferase in the early stage
of cell wall synthesis
Bacitracin • Cell wall synthesis inhibitor:
interferes with
dephosphorylation in cycling
of the lipid carrier that
transfers the peptidoglycan
Mupirocin subunits to the growing cell
wall
4 of 13
GLYCOPEPTIDES
ACTIVITY / CLINICAL USES PK/PD ADVERSE EFFECTS
DOC  • Usually IV due to poor absorption in • “Red man” or “red neck”
• Active only against GRAM (+) bacteria and intestinal tract syndrome 
aneorobes  • Only used orally for treatment of → Infusion-related flushing
→ MRSA  colitis caused by C. difficile → Due to histamine release
→ S. pneumoniae • Widely distributed in body fluids and • Phlebitis to injection site
→ S. aureus tissues • GI disturbance
→ S. viridans • Serum trough concentration • Ototoxicity
→ S. epidermidis monitoring is required in patients → reversible
→ Penicillin-resistant strain of pneumococcus with prolonged course of therapy • Nephrotoxicity
(combined with cefotaxime, ceftriaxone, or • Recommended trough → reversible
rifampin) concentrations
• NO activity against Gram (-) organisms  → 10-15mcg/mL (mild to
• Metronidazole-resistant C. difficile (colitis)  moderate infections)
→ 15-20mcg/mL (serious
infections)
• Time-dependent killing
• Complicated skin and soft tissue infections • Same as vancomycin except for a • Potentially teratogenic
• Hospital-acquired pneumonia longer half-life • Must avoid administration to
• Monitoring of telavancin levels is pregnant women
not required
• Spectrum of activity same as vancomycin but active • IV only due to poor oral absorption • Myopathy
against vancomycin-resistant enterococci and S. • Distributed mainly into plasma and → Creatine phosphoinase
aureus  intersittial fluid should be monitored
• Not used to treat pneumonia (antagonized by pulmonary • Concentration-dependent killing • Allergic pneumonitis
surfactant)
• Active against both Gram (+) & Gram (-) organisms • PO, IV • Safe for use in pregnancy
• Uncomplicated lower urinary tract infections in • Half-life: 4 hours
women • Excreted by the kidney
• Active against Gram (+) organisms • TOPICAL USE ONLY! • Highly nephrotoxic when
• Limited success for eradication of nasal carriage of administered systematically
Staphylococcus
• Irrigation of meninges intraoperatively
• Active against MSSA, MRSA, and Strep. pyogenes • No systemic toxicity
• Highly effective in eradicating S. aureus nasal
carriage
 PHARMA REVIEWER 1: Specific Antibiotics 5 of 13

TETRACYCLINES
DRUGS MOT ACTIVITY / CLINICAL USES PK/PD ADVERSE EFFECTS
Tetracycline • Bacteriostatic DOC  • Oral: Doxycycline, • Tigecycline: Black box
Doxycycline • Protein • Chlamydia: Doxycycline Minocycline warning (significant ↑ death)
Minocycline synthesis → Urethritis • IV: Tigecycline • Deposit in growing bones +
Tigecycline inhibitor: → Pelvic inflammatory disease • Absorption impaired by: teeth 
reversibly → Lymphogranuloma venereum → food EXCEPT → Discoloration
bind to 30s → Psittacosis doxycycline, minocycline → Enamel dysplasia
subunit • Rickettsial infection → Ca, Mg, Fe, Al, Zn → Bone deformity
→ Rocky Mountain spotted fever → Dairy products → Growth inhibition
→ Typhus fever → Antacids → Avoid in pregnant + < 8
• Lyme disease, relapsing fever → Alkaline pH yrs
• Brucellosis (with streptomycin) • Minocycline: ↑ concentration • Nausea, vomiting, diarrhea
• Melioidosis in tears + saliva → → Take with food
• Plaque: Cholera, Tularemia eradication of → Reduce dose
• Granuloma inguinale meningococcal carrier state → Discontinue
• Mycobacterium fortuitum infection: Doxycycline • Cross placenta (teratogenic) • Alter normal GI flora results in:
• Mycobacterium marinum infection: Minocycline • Excreted in breast milk → Intestinal functional
• Malaria: Doxycycline • Shorter half-life due to: disturbance
• Leptospirosis: Doxycycline Carbamazepine, phenytoin, → Anal pruritus
barbiturates, chronic alcohol → Vaginal/oral candidiasis
Other uses: • Excreted in bile + urine → Clostridium difficile-
• Adjuvant therapy in intestinal amebiasis • Doxycycline, Tigecycline: associated colitis
• Alternative therapy in: eliminated nonrenal, no • Impair hepatic fxn
dosage adjustment in renal • Renal tubular acidosis
→ Actinomycosis
failure • Fanconi syndrome (w/
→ Rat bite fever
→ Syphilis outdated/expired drugs)
→ Tularemia • Nephrotoxicity (given with
→ Yersinia enterocolitica enteritis diuretics) except doxycycline
→ Penicillinase producing gonococci • Minocycline, ↑ dose
→ Mycoplasma pneumoniae doxycycline: dizziness,
→ Leprosy: Minocycline (with rifampin + ofloxacin) vertigo, N/V
→ Community acquired MRSA of skin + soft tissue infections
• Severe acne
 PHARMA REVIEWER 1: Specific Antibiotics 6 of 13

MACROLIDES
SPECIFIC ACTIVITY / ADVERSE
DRUGS MOT GENERAL ACTIVITY PK/PD NOTES
CLINICAL USES EFFECTS
Erythromycin • Bacteriostatic DOC: Atypical pathogens  • Corynebacterial infections • ↑ concentrations of: • Anorexia, N/V, Macrolides
(prototype) • Protein • G+ → Diphtheria → Theophylline diarrhea  used in:
synthesis → Pneumococci (↑ macrolide → Corynebacterial sepsis → Warfarin (less with • Pneumonia:
inhibitors: resistance) → Erythrasma → Cyclosporine clarithromycin) added to
reversibly → Staphylococci • Respiratory, neonatal, → Methylprednisolone • Acute penicillin to
bind to 50s → Streptococci ocular or genital chlamydial → Oral digoxin cholestatic cover
subunit → Corynebacteria infections hepatitis atypical
→ Mycoplasma pneumonia (↑ • Penicillin substitute in (fever, organisms
macrolide resistance) penicillin-allergic individuals jaundice, (e.g.
(like aztreonam) impaired liver Legionella,
→ Legionella pneumophilia
Clarithromycin • Prophylaxis for • Improved acid stability + function) Mycoplasma)
→ Chlamydia
(semisynthetic endocarditis (dental oral absorption than • Prolong QT • Peptic ulcer
trachomatis/psittaci/pneumoniae
derivative) procedure in valvular heart erythromycin interval disease: in
→ Helicobacter pylori
disease) • Longer half-life (6 hours) = → Torsades combo with
→ Listeria monocytogenes
• More active against 2x daily dose (less de pointes other drugs
→ Certain mycobacteria Mycobacterium avium frequent dosing) against H.
arrythmia
• G- complex • Metabolized in liver pylori
→ ↑ risk of
→ Neisseria sp. • Mycobacterium leprae • Metabolite: 14- cardiac
→ Bordetella • Toxoplasma gondii hydroxyclarithromycin death
pertussis/henselae/quintana • Hemophilus influenzae (with antibacterial activity)
→ Hemophilus influenzae (more than erythromycin) • Eliminated in urine; dose
(erythromycin is least reduction for creatine
susceptible) clearance <30ml/min
• Same drug interactions as
erythromycin
Azithromycin Active against: • Penetrates into most
(semisynthetic • Mycobacterium avium tissues (except CSF) and
derivative) complex phagocytic cells, ↑ tissue
• Toxoplasma gondii concentrations
• Hemophilus influenzae (best • Slowly released from
coverage of the 3) tissues, elimination half-
life: 3 days = take once
Less active against: daily for 3 days
• Staphylococci • Administered 1 hr before /
• Streptococci 2 hrs after meals
• No drug interactions
(does not inactivate
cytochrome p450
enzymes)
 PHARMA REVIEWER 1: Specific Antibiotics 7 of 13

LINCOSAMIDES: CLINDAMYCIN
MOT ACTIVITY CLINICAL USES PK/PD ADVERSE EFFECTS
• Bacteriostatic • G+: S. pneumonia, S. pyogenes, • Anaerobic infections outside CNS  • Penetrates well • Diarrhea, nausea,
• Protein S. aureus, S. viridans → Bacteroides fragilis into abscesses skin rashes
synthesis • Others: Anaerobes, Plasmodium, → Intraabdominal infections • Diarrhea and
inhibitor: Pneumocystis → Polymicrobial infections (with aminoglycoside/aztreonam) colitis due to C.
reversibly • No G- coverage  (d/t poor • Community acquired MRSA infection of skin + soft tissues difficile
bind to 50s permeability) • Sometimes:
subunit → Good to pair with Alternative therapy in: → Impaired liver
aminoglycosides (G- • Osteomyelitis + Septic arthritis (allergy to penicillin/cephalosporin) function
coverage) • Actinomycosis (allergy to penicillin G) → Neutropenia
• Gardnerella vaginalis vaginosis (than metronidazole)
• Toxoplasmosis, Pneumocystis jirovecci pneumonia (than cotrimoxazole)
• Prophylaxis for endocarditis in valvular heart disease (allergy to penicillin,
preferred over erythromycin)

DRUGS
Quinupristin (Streptogramin B)
- Dalfopristin (Streptogramin A)
combination (30:70)
STREPTOGRAMINS
MOT ACTIVITY CLINICAL USES PK/PD
• Bactericidal • Rapidly bactericidal against most • Multidrug resistant G+ pathogens • Prolonged post-
• Protein synthesis G+ except E. faecium (slow) → e.g. vancomycin-resistant E. faecium antibiotic effect (10
inhibitor: reversibly • NO activity against E. faecalis  • Septicemia or respiratory tract infection caused by: hrs)
bind to 50s subunit → MRSA
→ Resistant streptococci
→ Penicillin-resistant S. pneumoniae
• Reserved for treatment of serious, life-threatening
systemic infections 

CHLORAMPHENICOL
MOT ACTIVITY CLINICAL USES PK/PD ADVERSE EFFECTS
• Bacteriostatic • Aerobic and anaerobic G+ • Life-threatening infections d/t H. influenzae • Oral (↑ bioavailability) • N/V, diarrhea (adult)
except against:  and G- → Meningitis > IV  • Oral/vaginal candidiasis
→ S. pneumoniae • Rickettsia → Epiglottitis • Widely distributed • Dose-related reversible
→ H. influenzae • Not active against → Septicemia including CNS, suppression of red cell
→ N. meningitidis Chlamydia → Severe pneumonia concentration in brain production
• Protein synthesis • Severe infections by: tissue = concentration • Aplastic anemia (prolonged use)
inhibitor: reversibly → Salmonella typhi in serum • Gray baby syndrome 
bind to 50s subunit → Bacteroides sp. (meningitis, brain abscess) (>50mg/kg/day)
• Bacterial meningitis by:  → Vomiting
→ Meningococcal → Flaccidity
→ Pneumococcal → Hypothermia
→ H. influenzae → Gray color
• Intraocular infections by sensitive microorganisms  → Shock
→ Vascular collapse
Alternative therapy in: • ↑ concentrations of:
• Pneumococcal + meningococcal meningitis (allergic to → Phenytoin
penicillin G) → Tolbutamide
• Severe rickettsial infections (hypersensitive to → Chlorpropamide
tetracyclines + pregnant) → Warfarin
• Brucellosis, glanders, plague, tularemia
 PHARMA REVIEWER 1: Specific Antibiotics 8 of 13

OXAZOLIDINONES: LINEZOLID
MOT CLINICAL USES PK/PD ADVERSE EFFECTS
• Bacteriostatic • Vancomycin-resistant E. faecium infections • Oral (100% • Hematologic 
• Protein • Nosocomial pneumonia + skin infection bioavailability)  → Thrombocytopenia (if >2 weeks)
synthesis • Multiply resistant G+ bacterial infections (MRSA, PRSP) (like chloramphenicol)
→ Anemia
• Neither an
inhibitors: • MDR-TB + XDR-TB → Neutropenia
inducer/inhibitor
reversibly → Bacteroides fragilis • Optic and peripheral neuropathy + lactic acidosis
of cytochrome
bind to 50s → Intraabdominal infections p450 enzymes • MAO inhibitor
subunit → Polymicrobial infections (with aminoglycoside/aztreonam) → Severe hypertension (if taken with tyramine-rich food)
• Community-acquired MRSA infection of skin + soft tissues → Serotonin syndrome (fever, agitation, mental status
change, tremors) if taken with serotonergic drugs- SSRIs

AMINOGLYCOSIDES
DRUGS MOT ACTIVITY / CLINICAL USES PK/PD ADVERSE EFFECTS
Streptomycin • Bactericidal DOC: G- infections  • IV as 30-60 minute • Nephrotoxicity 
Amikacin • Protein • Serious infections with G- bacteria: In combo w/ B-lactam infusion, 2-3 equally → Non-oliguric renal failure
Gentamycin synthesis antibiotic (for G+ coverage) divided doses/day OR → Polyuria
Tobramycin inhibitors: • G+ endocarditis: In combo w/ vancomycin/ B lactam antibiotic single daily injection → Potentiated by use with loop diuretics or
Netilmicin reversibly (for G+ coverage) → Concentration- other nephrotoxic agents (vancomycin,
Spectinomycin bind to 30s • TB dependent killing amphotericin)
subunit → Post-antibiotic → Neomycin > kanamycin, amikacin,
effect gentamycin, netilmicin > tobramycin >
• Highly polar: streptomycin
concentration in tissue not • Ototoxicity 
high except in renal → Tinnitus
cortex → nephrotoxic → High frequency hearing loss
• Excluded from CNS and → Vertigo, ataxia, loss of balance
eye
→ Neomycin (cochlear) > streptomycin
• Measure peak and (vestibular) > kanamycin (cochlear) >
trough levels (like vancomycin) amikacin, gentamycin, tobramycin,
netilmicin
Streptomycin • 2nd line for M. tuberculosis (M. avium complex, M. kansasii) • 8th CN damage (vestibular)
• Enterococcal endocarditis, Streptococcus viridans: In combo with
Pen G
• Plague, tularemia, brucellosis: In combo with oral tetracycline
Gentamycin • P. aeruginosa • Irreversible vestibular damage
• Reversible renal damage
→ Risk ↓ by once daily dose
Amikacin • P. aeruginosa
• 2nd line for MDR-TB (including streptomycin-resistant M.
tuberculosis)
Spectinomycin • Gonorrhea caused by strains resistant to first-line drugs
 PHARMA REVIEWER 1: Specific Antibiotics 9 of 13

SULFONAMIDES
MOT ACTIVITY CLINICAL USES ADVERSE EFFECTS
• Bacteriostatic • Formerly susceptible • 1st line  • Most common: fever, skin rashes,
• Inhibition of DNA species but now resistant → Burkholderia cepacia exfoliative dermatitis, photosensitivity,
synthesis → Meningococci → Stenotrophomonas maltophilia urticaria, N/V, diarrhea
→ Interfere with → Pneumococci • Respiratory tract infections d/t H. influenzae + S. pneumoniae • Steven-Johnson syndrome 
folic acid → Streptococci → Chronic bronchitis • Urinary Tract disturbances 
synthesis → Staphylococci → Otitis media → Crystalluria (Tx: ↑ fluid intake, NaHCO3)
→ Competitive → Gonococci → Sinusitis → Hematuria
antagonism of • Thus, infrequently used as → Pneumonia → Obstruction
PABA, thus single agents → Bone + joint infections → Nephrosis
inhibition of • Toxoplasmosis (sulfadiazine + pyrimethamine) → Allergic nephritis
dihydrofolic acid • Dermatitis herpetiformis (sulfapyridine) • Hematopoietic disturbances
formation → Hemolytic/aplastic anemia
• Topical agents:
→ Sodium sulfacetamide ophthalmic solution/ointment for eye infection, → Agranulocytopenia
bacterial conjunctivitis and adjunct therapy for trachoma → Leukemoid reactions
→ Silver sulfadiazine for burns → Hemolytic reactions in G6PD deficient
• Oral sulfasalazine: ulcerative colitis + regional ileitis → Kernicterus in newborns 

Alternative therapy in:

• H. ducreyi infection (chancroid)
• Bacillary (shigella) dysentery
• Dermatitis herpetiformis (sulfapyridine)
• 2nd line: Falciparum malaria (sulfadoxine + pyrimethamine / sulfalene +
pyrimethamine)

TRIMETHOPRIM-SULFAMETHOXAZOLE
MOT ACTIVITY CLINICAL USES PK/PD ADVERSE EFFECTS
• Bactericidal • Most Staphylococcus • DOC • Renal dose • Antifolate drug
• Inhibition of DNA aureus strains → Pneumocystis jirovecci pneumonia  adjustments → Megaloblastic anemia
synthesis → MSSA → Toxoplasmosis • Trimethoprim: → Leukopenia
→ Interfere with → MRSA → Nocardiosis antibacterial activity → Granulocytopenia
folic acid • Respiratory tract • [oral] Effective treatment for: in prostatic and • Adverse reactions associated
synthesis pathogens → Shigellosis vaginal fluids with sulfonamides
• Sulfonamide: → Pneumococcus → Systemic salmonella infections → N/V
competitive → Haemophilus sp. → UTIs → Drug fever
antagonism of → Moraxella catarrhalis → Prostatitis → Vasculitis
PABA, thus inhibition → K. pneumoniae → Nontuberculous mycobacterial infections pneumonia → Renal damage
of dihydrofolic acid • NOT active against • [IV] Effective treatment for → CNS disturbances
formation • Patients with AIDS +
Mycoplasma pneumoniae → Moderate severe-severe pneumocystis pneumonia
• Trimethoprim: • ↑ resistance of E coli + → G- bacterial sepsis by Enterobacter + Serratia pneumocystis pneumonia:
inhibits dihydrofolic pneumococci strains → Fever
→ Shigellosis
acid reduction to
→ Typhoid fever → Rashes
tetrahydrofolate
→ Leukopenia
→ Diarrhea
→ ↑ hepatic aminotransferases
→ Hyperkalemia
→ Hyponatremia
 PHARMA REVIEWER 1: Specific Antibiotics 10 of 13

FLUOROQUINOLONES
DRUGS MOT ACTIVITY CLINICAL USES PK/PD ADVERSE EFFECTS
1st GEN: • Bactericidal • Least active against G- and G- • Lower UTIs • Oral absorption • Well-tolerated
Nalidixic acid • Inhibition of DNA • Acute entero-invasive diarrhea (e.g. shigellosis) impaired by: • Most common: N/V,
synthesis → Di/trivalent diarrhea
→ Inhibit bacterial cations • Prolongation of QTc
topoisomerase II → Antacids interval:
2nd GEN: (DNA gyrase) + • Excellent against G- aerobic • UTIs • Taken 2 hours → Gatifloxacin
Ciprofloxacin topoisomerase bacteria but limited activity vs G+ • Diarrhea before or 4 → Levofloxacin
Ofloxacin IV → S. aureus (MSSA) → Shigella hours after any → Gemifloxacin
→ L. monocytogenes → Salmonella products with → Moxifloxacin
→ Enterobacteriaceae → Toxigenic E coli cations • Gatifloxacin (not in sale)
→ N. meningitidis → Campylobacter → Hyperglycemia in
→ N. gonorrhea • Ciprofloxacin: Highest activity against diabetics
→ H. influenzae P. aeruginosa among fluroquinolones  → Hypoglycemia in
→ M. catarrhalis → ONLY oral drug for P. aeruginosa  patients taking oral
→ Campylobacter jejuni → Prophylaxis + treatment for anthrax hypoglycemic
→ Shigella → Chlamydial urethritis / cervicitis agents
→ Chlamydia sp. → Tuberculosis + atypical mycobacterial • Damage growing
→ M. pneumoniae infections cartilage, arthropathy
• NO activity against MRSA, → Eradicate meningococci from carriers → Not recommended
anaerobes → Prophylaxis of infection in neutropenic for <18 years
cancer patients → May be used in
• Ofloxacin: bactericidal vs M. tuberculosis some cases (treat
• Infections of soft tissues, bones, joints, pseudomonal
intraabdominal + respiratory infections infections in
patients with cystic
3rd GEN: • Superior activity vs G+ • Levofloxacin, Moxifloxacin
fibrosis)
Levofloxacin • P. aeruginosa is LESS → Bactericidal vs M. tuberculosis
Moxifloxacin susceptible → Atypical mycobacterial infections
Gemifloxacin • B. fragilis is NOT susceptible → Eradicate meningococci from carriers
• Respiratory fluoroquinolones → Prophylaxis of infection in neutropenic
→ Enhanced G+ activity cancer patients
→ Activity against atypical • Moxifloxacin: MOST ACTIVE fluoroquinolone
pneumonia (chlamydia, against M. tuberculosis 
mycoplasma, legionella) • Levofloxacin: Chlamydial urethritis / cervicitis
• UTIs (except moxifloxacin)
• Diarrhea
• Infections of soft tissues, bones, joints,
intraabdominal + respiratory infections
 PHARMA REVIEWER 1: Specific Antibiotics 11 of 13

METRONIDAZOLE
MOT ACTIVITY CLINICAL USES PK/PD ADVERSE EFFECTS
• Bactericidal • Antiprotozoal As antibacterial agent: • Oral or IV • Nausea
• Inhibits nucleic acid • Antibacterial • Tetanus, all forms- C. tetani • Penetrates • Diarrhea
synthesis and against • Anaerobic infections- B. fragilis  well into • Stomatitis
damages DNA anaerobes → Intraabdominal infection CSF + • Peripheral neuropathy
• Little effect on → Female pelvic infection brain • Disulfiram-like effect
human cells + → Brain abscess → Like cefoperazone
aerobic bacteria → Endocarditis → Avoid alcohol
→ Meningitis • Teratogenic in some
• Antibiotic-induced pseudomembranous colitis due to Clostridium difficile  animals
→ 2nd line: oral vancomycin *not in PH
• Gardnerella vaginalis vaginitis
• Combination therapy for H. pylori in peptic ulcer disease
• Prophylaxis of anaerobic infections associated with colorectal + gynecological surgery
→ In combo with aminoglycosides for aerobes

As antiprotozoal agent:
• [DOC] Trichomonal vaginitis
• [DOC] symptomatic amebiasis (tissue amebicide)
• Giardiasis

• Tinidazole [structurally similar]

→ Trichomonas infection, giardiasis, amebiasis, bacterial vaginosis
→ NOT for anaerobic infections

NOTES/SUMMARY
NONE of the CEPHALOSPORINS currently used in the country is active AGAINST Nitrofurantoin: Urinary Antiseptic
• Enterococcus • Antibacterial activity in urine
• Listeria monocytogenes • Little/no systemic antibacterial effect
• MRSA • Oral agent for uncomplicated UTIs
• Clostridium difficile
• Chlamydial sp. Avoid in Pregnancy: CTT SCAM
• Chloramphenicol: Gray baby syndrome / CV collapse
TAG @ 30 / AT 30 • Tetracycline: Tooth discoloration, enamel/bone hypoplasia, maternal liver
• Tetracyclines toxicity
• Aminoglycosides • Telavancin
• Sulfonamides: neonatal jaundice/ hemolytic anemia if given close to
50 CELLS delivery
• Chloramphenicol • Ciprofloxacin: fetal cartilage damage (animal studies)
• Erythromycin (Macrolides) • Aminoglycosides: fetal ototoxicity
• Lincosamides • Metronidazole: conflicting data, some suggest teratogenicity; avoid if
• Linezolid possible
• Streptogramins

REFERENCES
Flores, D. (2020). Specific Antibiotics. Dept of Pharmacology. UST-FMS.
Pharmacology Handout on Antibiotics (2017)
Katzung’s Basic and Clinical Pharmacology 14th Edition
END OF REVIEWER
Prepared by: Rayos, Al Kim and Suarez, Rina
 PHARMACOLOGY

SPECIFIC ANTIBIOTICS
REVIEWER | MAY 2020

UNIVERSITY OF SANTO TOMAS

FACULTY OF MEDICINE AND SURGERY
D2022 Reviewer
Sample EXAMINATION
May 2020

Instructions:
1. There are 20 items in this questionnaire
2. CHOOSE THE BEST ANSWER.
3. Try to answer on your own (without the use of reviewers/trances)
4. Answers are given in a separate document.
5. God bless!
----------------------------------------------------------------------------------------------------------------------------- -------------------------------------
CHOOSE THE BEST ANSWER

MATCHING: Adverse Effects (4 points)

A. Metronidazole
B. Vancomycin
C. Clindamycin
D. Chloramphenicol

1. Histamine-related flushing
2. Aplastic anemia
3. C. difficile colitis
4. Disulfiram-like effect

MATCHING / MULTIPLE CHOICE: Mechanism of Action (4 points)

5. A 50-year-old woman with no significant past medical history presents to her physician with cough of two weeks
duration and fever of 4 days. Her physician prescribed a 3-day course of azithromycin. Which of the following
antibiotics has the same target site as azithromycin?
A. Vancomycin B. Ciprofloxacin C. Chloramphenicol D. Bacitracin

Match the antibiotic with the structure/enzyme it inhibits:

A. Trimethoprim
B. Ceftriaxone
C. Moxifloxacin
D. Sulfonamide

6. Penicillin binding proteins

7. Topoisomerase II
8. Dihydrofolate reductase

MULTIPLE CHOICE: Clinical Indications (7 points)

9. A 60-year-old female was rushed to the ER due to fever and chills. Blood culture later revealed E. coli. Which of the
following antibiotics is active against this microorganism?
A. Clindamycin B. Erythromycin C. Vancomycin D. Aztreonam

10. A 27-year-old patient is about to undergo colorectal surgery tomorrow. What antibiotic will be used for surgical
prophylaxis?
A. Cefoxitin B. Cephalexin C. Cefazolin D. Cefuroxime

11. A 55-year-old man is suspected to have Mycoplasma pneumonia. The most appropriate antibiotic to give is:
A. Ceftriaxone B. Azithromycin C. Co-amoxiclav D. Amikacin

12. Ciprofloxacin is NOT active against which of the following organisms:

A. H. influenza B. P. aeruginosa C. Enterobacteriaceae D. Bacteroides fragilis

Reviewer 3.1 PREPARED BY: Rayos, Al Kim and Suarez, Rina

 PHARMA REVIEWER 1: Specific Antibiotics

13. Penicillin G is one of the oldest drugs in the market. Due to this, many have abused its use and some bacteria have
already developed resistance to its effect. Despite this, it is still the drug of choice for this disease.
A. Gonorrhea B. Syphilis C. Genital herpes D. Chlamydia

14. The absorption of this antibiotic under the class of penicillins is not impaired by food.
A. Ampicillin B. Penicillin V C. Ticarcillin D. Amoxicillin

15. In which of the following infections is doxycycline not clinically useful?

A. Gonococcal urethritis B. Leptospirosis C. Cholera D. Chlamydial cervicitis

PRESCRIPTION
ERASURES MAY BE ALLOWED “BUT” COMPLAINTS ON THE ERASED ANSWER WILL NOT BE ENTERTAINED

16-20: A 29-year-old jeepney driver presented with difficulty of breathing upon consultation. He also had a runny nose and
a productive cough with yellowish phlegm a few days before. He was a smoker with a history of 20 pack years and was
diagnosed with diabetes last year. Upon PE, his body temperature is 38.9°C, his PR is 110 beats/min and regular, and his
RR is 18 breaths/min. CXR findings showed localized infiltrates in the lower part of the left lung. Upon calculation of the PSI
and CURB65, along with the clinical findings, the patient was diagnosed with low-risk community acquired pneumonia.
Make a prescription. Choose from the following drugs:

A. Amoxicillin Preparation: 500 mg capsule

Recommended dose: 1 gram every 8 hours for 1 week
B. Cefuroxime Axetil Preparation: 500 mg tablet
Recommended dose: 500 mg every 12 hours for 1 week

RSS2020//AKRR2020

- END OF QUIZ-
GOD BLESS!