PHARMACOLOGY

ANALGESIC & ANTIMIGRAINE

 Butorphanol  Naloxone
 Dihydroergotamine  Propoxyphene

 Fentanyl  Sumatriptan

 Meperidine  Tramadol

 Methadone

 Morphine
BUTORPHANOL
 Opioid analgesic  Dysphoria
 Nightmares
 Mixed opioid agonist-antagonist
 w/drawal in pts dependent on full
opioid agonists
 Partial agonist or antagonist @
opioid μ receptors  AVOID MAOI
 Agonist @ κ receptors @ spinal  Potentially fatal
& supraspinal sites
 Inhibits spinothalamic pain
neurotransmission

 Moderate-severe pain
 Admin intranasally

 ↓ respiratory depression,
constipation, dependence than full
μ receptor agonists
DIHYDROERGOTAMINE
 Antimigraine  N, V
 Ergot alkaloid  Stiff neck, shoulder, extremities
 Leg weakness
 5-HT 1B/1D receptor agonist  Numbness & tingling in fingers
& toes
 Activates 5-HT 1B/1D receptors
 Pial & dural vessel constriction
 Presynaptic inhibition of
trigeminal peptide
neurotransmitter release
 Inhibitions brainstem activation
of trigeminal neurons
 Vascular HA
 Migraine & cluster
 Injection or nasal spray
FENTANYL
 Opioid analgesic  Sedation
 Phenylpiperidine  Confusion
 Respiratory depression
 Activates opioid μ receptors
 Anorexia
 Inhibits pain transmission
 N, V
@ spinal & supraspinal  Constipation
sites
 AVOID MAOI in past 14d
 Chronic pain
 Breakthrough for cancer pain

 Transdermal patch
MEPERIDINE
 Opioid analgesic  Confusion
 Sedation
 Strong opioid agonist  Constipation
 N, V
 Activates opioid receptors  Dependence
 Inhibits pain transmission  Toxic metabolite  CNS
excitation, convulsions,
 Generalized CNS depression tremors

 Moderate-severe pain  AVOID MAOI

 Analgesia during labor  Potentially fatal
 Preoperative sedation

 Lacks antitussive activity

METHADONE
 Opioid analgesic  Respiratory depression
 Constipation
 Strong opioid agonist  Confusion
 Sedation
 Activates opioid receptors
 Inhibits pain transmission  AVOID MAOI
 Suppresses opioid w/drawl
Sx w/ euphoria or
dependence

 Moderate-severe pain
 Prevention of opioid abuse

 Orally, once per day

MORPHINE
 Opioid analgesic  Sedation
 Strong opioid μ receptor agonist  Confusion
 Hypotension
 Constipation
 Activates μ receptors  Respiratory depression
 ↑ cAMP
 Opens K & closes Ca channels  AVOID MAOI w/ 14 d
 ↓ release substance P  Potentially fata
 Inhibits pain @ spinal &
supraspinal sites

 Severe pain w/ MI
 Pulmonary edema

 Active metabolite
 Morphine glucuronate
NALOXONE
 Opioid antagonist
 Opioid receptor antagonist

 Blocks opioid μ, δ, κ
receptors
 Rapidly reverses effects of
opioid agonists

 Opioid OD, dependence

 Short half-life needs

repeated doses
PROPOXYPHENE
 Opioid analgesic  Dizziness
 Weakness
 Weak opioid agonist
 N
 dependence
 Activates opioid receptors
 Inhibits pain transmission

 Mid-moderate pain

 Combined w/ acetaminophen
or aspirin
SUMATRIPTAN
 Antimigraine  Dizziness
 5-HT 1B/1D receptor agonist  Vertigo
 Tingling
 Warm sensation
 Activates 5-HT 1B/1D receptors  Tight feeling head & chest
 Pial & dural vessel constriction  Coronary vasospasm
 Presynaptic inhibition of
trigeminal peptide  AVOID
neurotransmitter release  MAOI
 Inhibitions brainstem activation  SSRI
of trigeminal neurons
 Vascular HA
 Migraine & cluster

 Oral, nasal, & subQ

TRAMADOL
 Analgesic  Dizziness
 Dual action  HA
 Constipation
 Lowers seizure threshold
 Activates μ opioid receptors
 Inhibits neuronal reuptake
5-HT & NE  AVOID MAOI
 ↑ inhibition of pain
 ↑ risk seizures w/ high
 Moderate pain doses
 Chronic pain
 Penicillins
 Phenothiazines

 Naloxone reverses some

but NOT all Sx
ANESTHETICS
 Benzocaine  Midazolam
 Bupivacaine  Nitrous oxide

 Halothane  Propofol

 Ketamine  Sevoflurane

 Lidocaine
BENZOCAINE
 Local anesthetic  Cross-sensitivity w/ other ester-
type anesthetics
 Ester-type

 Blocks Na channels & nerve

conduction
 Topical anesthetic
 Pain
 Itching
 Inflammation
 Burns
 Insect bites
 Contact dermatitis
 Wounds
 Irritates skin when 1st applied
 Use caution w/ sunburn & large
areas of skin
BUPIVACAINE
 Local anesthetic  Cross-sensitivity
w/
 Amide-type amide-type anesthetics

 Blocks Na channels &

nerve conduction

 Local or regional
anesthetic
 Surgical
 Diagnostic

 Obstetrical

 therapeutic
HALOTHANE
 General anesthetic  Sensitizes heart to
catecholamine-induced cardiac
 Inhalational, halogenated arrhythmia
hydrocarbon  Hepatotoxic
 Fluoride metabolites
 Potentiates GABA binding to
GABA-A Cl ion channel
 Suppresses sensory processing
in thalamus

 General anesthetic

 High blood:gas partition

coefficient
 Slow rate of induction &
recovery
KETAMINE
 IV anesthetic  Delirium
 Glutamate antagonist  Hallucination
 Irrational behavior during
 Blocks glutamate NMDA recovery
receptors  ↑ BP
 Dissociate anesthesia
 Analgesia
 Immobility
 Amnesia

 Does NOT depression

respiration or cause LOC
 Anesthesia
 Minor surgical & diagnostic
procedures
 Children
LIDOCAINE
 Local anesthetic  Cross-reactivity w/ amide-
 Amide-type type anesthetics

 Blocks Na channels & nerve

conduction

 Topical
 Infiltration
 Nerve block
 Epidural
 Spinal anesthesia
 Eutectic mixture
 Lidocaine & prilocaine
 Anesthetize intact skin for
venipuncture
 IV cannulation
 Circumcism
MIDAZOLAM
 Sedative-hypnotic-anxiolytic  Apnea
 Short-acting BZDP  Laryngospasm
 Respiratory depression
 Potentiates GABA binding to  Cardiac arrest
GABA-A Cl ion channel
 Sedation
 Hypnosis
 Amnesia

 Preoperative sedation &

anxiolysis
 Sedation of mechanically
vented pts
NITROUS OXIDE
 Inhalation general anesthetic
 Anesthetic gas

 Potentiates GABA binding to

GABA-A Cl ion channel
 Suppresses sensory processing
in thalamus
 Minor surgery & dental
procedures

 Rapid induction & recovery

 Euphoria – laughing gas
PROPOFOL
 General anesthesia  Bradycardia
 IV anesthetic  Hypotension
 Diisopropyl phenol

 Potentiates GABA binding

GABA-A Cl ion channel
 Hypnosis
 Anesthesia
 Amnesia
 NO analgesic effect
 Intubation & maintenance of
general anesthesia
 Sedation of intubated pts in
ICU
SEVOFLURANE
 General anesthetic
 Inhalation anesthetic

 Potentiates GABA binding

to GABA-A Cl channel
 Suppresses sensory
processing in thalamus
 Causes LOC

 General anesthesia
ANTI-INFECTIVE
 Acyclovir  Cefepime
 Albendazole  Cetriaxone

 Amantadine  Ciprofloxacin

 Amoxicillin-clavulanate  Clindamycin

 Amphotericin B  Doxycycline

 Azithromycin  Efavirenz

 Aztreonam  Enfuvirtide

 Caspofungin  Erythromycin

 Cefazolin  Ethambutol
 Foscarnet  Linezolid
 Fosfomycin  Mefloquine

 Ganciclovir  Metronidazole

 Gentamicin  Mupirocin

 Griseofulvin  Nafcillin

 Imipenem-cilastatin  Nitrofurantoin

 Isoniazid  Oseltamivir

 Itraconazole  Paromomycin

 Ivermectin  Penicillin G

 Levofloxacin
 Pentamidine  Rifampin
 Piperacillin-tazobactam  Ritonavir-lopinavir

 Praziquantel  Streptomycin

 Primaquine  Terbinafine

 Pyrimethamine  Trifluridine

 Pyrantel  TMP-SMX

 Quinine  Vancomycin

 Quinpristein-dalfopristin  Zidovudine

 Ribavirin
ACYCLOVIR
 Antiviral  Dizziness
 Diarrhea
 Nucleoside analogue
 N
 Nephrotoxicity
 Converted to acyclovir triphosphate
by viral & host cell kinases  Probenecid ↑ serum levels
 Incorporated into DNA by viral
DNA polymerase causing DNA
chain termination

 HSV2
 Herpes zoster
 Shingles
 Chickenpox – varicella

 ↓ viral shedding, pain, & healing

time
ALBENDAZOLE
 Antihelmintic  GI distress
 Benzimidazole
 Constipation or diarrhea
 Hepatitis & hematologic toxicity w/ high
doses
 Binds & inhibits polymerization of
tubulin dimmers to form cytoplasmic
microtubules
 Impairs glucose uptake & deplete
glycogen stores

 Intestinal nematode infections

 Hookworm
 Pinworm
 Whipworm
 Ascariasis
 Capillariasis
 Trichinosis
 Use w/ corticosteroid
 Cysticercosis & echinococcus
 Microsporidiosis
AMANTADINE
 Anti-influenza,  Ataxia
antiparkinson  Dizziness
 Tricyclic amine  Insomnia
 Skin mottling & livedo
reticularis
 Inhibits influenza-A M2  Blurred vision
proton channel &  Dry mouth
acidification of virus
particle
 Prevents viral protein-
protein dissociation &
uncoating of viral particles

 Influenza A
AMOXICILLIN-CLAVULANATE
 β-lactam ABX  Diarrhea
 Extended spectrum aminopenicillin & β-
 Superinfection
lactamase inhibitor  Pseudomembranous colitis
 Allergic rxn
 Rash
 Amoxicillin  Serum sickness
 Binds PBP  anaphylaxis
 Inhibits cross-linking of cell wall
peptidoglycan  Probenecid inhibits renal tubular excretion
 Clavulanate  ↑ serum levels
 Inhibits class-A β-lactamase
 Protects amoxicillin from destruction
 NOT antimicrobial by itself

 Respiratory tract infections

 Otitis, sinusitis, pneumonia
 Skin or skin structure infections
 Bite wounds
AMPHOTERICIN B
 Antifungal  Chills
 Polyene ABX
 Fever
 Diarrhea
 N, V
 Binds ergosterol & ↑  Nephrotoxicity
membrane permeability  Hypokalemia
 Leakage of cell contents
 ↑ toxicity w/ cyclosporine,
antineoplastics
 Candidiasis  Thiazides, & corticosteroids ↑
 Cryptococcal meningitis hypokalemia
 Aspergillosis
 Blastomycosis
 Coccidioidomycosis
 Histoplasmosis
 Mucormycosis
AZITHROMYCIN
 Macrolide
 Protein synthesis inhibitor

 Binds 50s ribosome

 Prevents peptide elongation &
translocation from acceptor site to
peptidyl site

 Respiratory infections d/t strep,

pneumo, H. influenzae, Legionella
 Otitis media, sinusitis
 Single-dose Tx for chlamydial
urethritis, chancroid, MAI infections
AZTREONAM
 β-lactam ABX  Thrombophlebitis
 Monobactam  Allergic rxn

 Binds PBP including

transpeptidase
 Inhibits cross-linking of
cell wall peptidoglycan

 Drug resistant gram (-)

infections including
Pseudomonas aeruginosa &
Enterobacteriaceae
CASPOFUNGIN
 Antifungal  HA
 Echinocandin  Fever
 Phlebitis
 Abnormal LFTs
 Inhibits synthesis of cell
wall component
 β-1,3-D-glucan

 Candida albicans
 Invasive aspergillosis

 IV admin
 Not absorbed well by gut
CEFAZOLIN
 β-lactam ABX  Rash
 Diarrhea
 2nd generation cephalosporin
 Pseudomembranous colitis
 Superinfection
 Binds PBP including transpeptidase
 Inhibits cross-linking of cell wall  Probenecid inhibits excretion & ↑
peptidoglycan serum levels

 Surgical wound infections

 Infections d/t
 Staph, strep, E. coli, Klebsiella
pneumoniae, Proteus mirabilis

 NOT active against MRSA

CEFEPIME
 β-lactam ABX  Rash
 Diarrhea
 4th generation cephalosporin  Pseudomembranous colitis
 Superinfection
 Binds multiple PBP
 Inhibits cross-linking of cell  Probenecid inhibits excretion & ↑
wall peptidoglycan serum levels
 Resistant to many β-
lactamases

 Drug-resistant gram (-) bacteria

 Citrobacter
 Enterobacter
CEFTAZIDIME
 β-lactam ABX  Rash
 Diarrhea
 3rd generation cephalosporin
 Pseudomembranous colitis
 Superinfection
 Binds PBP including transpeptidase
 Inhibits cross-linking of cell wall  Probenecid inhibits excretion & ↑
peptidoglycan serum levels

 Gram (+), gram (-), & anaerobics –

Pseudomonas aeruginosa

 Pneumonia, meningitis, UTI, skin

structures, bones, jts
CETRIAXONE
 β-lactam ABX  Rash
 Diarrhea
 3rd generation cephalosporin
 Pseudomembranous colitis
 Superinfection
 Binds PBP including transpeptidase
 Inhibits cross-linking of cell wall  Probenecid inhibits excretion & ↑
peptidoglycan serum levels

 Infection d/t
 Pneumococci, gonococci,
meningococci, H. influenzae,
Moraxella catarrhalis, Borrelia
burgdorferi

 Single IM injection Tx acute otitis

media or gonorrhea
CIPROFLOXACIN
 Antibacterial  Insomnia
 Fluoroquinolone
 Diarrhea
 N

 Inhibits bacterial DNA topoisomerase  Absorption ↓ by cations

type II (DNA gyrase) & type IV  Antacids
 Prevents DNA replication & separation  Iron
of chromosomes  Zinc
 bismuth
 Urinary tract, prostate, intraabdominal w/
metronidazole, bone or jt, skin
 Inhalational anthrax
 Gonorrhea
 Infectious diarrhea

 Gram (+), gram (-), Pseudomonas

aeruginosa
CLINDAMYCIN
 Aminosugar ABX  C. difficile superinfection
 Diarrhea
 Protein synthesis inhibitor
 Pseudomembranous colitis

 Binds 50s ribosome

 Prevents translocation of
nascent peptide from
acceptor site to peptidyl site

 Strep, staph, gram (+)

 Acne vulgaris
 Anaerobes including Bacteroides
DOXYCYCLINE
 Tetracycline ABX  AVOID
 Protein synthesis inhibitor
 Pregnancy & children > 8 y/o
 Outdated preparations are
nephrotoxic
 Binds 30s ribosome
 Reversibly inhibits binding of  Permanent teeth discoloration
 Photosensitivity
transfer RNA to acceptor site
 Diarrhea
 N, V
 Rickettsia, Chlamydia, Mycoplasma,
Borrelia
 Acne
 Cholera
 Gonorrhea & syphilis in PCN
allergic pts
 Brucellosis & ehrlichiosis
EFAVIRENZ
 Antiretroviral  N
 Rash
 Non-nucleoside reverse  Drowsiness
transcriptase inhibitor  Depression

 Binds reverse transcriptase &

disrupts catalytic site

 HIV in combo w/ nucleoside

reverse transcriptase inhibitor –
synergistic

 High fat meal ↑ absorption

ENFUVIRTIDE
 Antiretroviral  Injection site rxn
 HIV fusion inhibitor
 Rotate sites daily

 Binds HIV virus gp41 &

blocks fusion of HIV w/
host cells CD4 Thelper
lymphocytes

 Drug-resistant HIV
ERYTHROMYCIN
 Macrolide ABX  Activates motilin receptors
causing uncoordinated peristalsis
 Protein synthesis inhibitor  Anorexia
 N, V
 Binds 50s ribosome
 Prevents peptide elongation &
translocation from acceptor site
to peptidyl site

 Pharyngitis, otitis media, sinusitis,

pneumonia d/t
 Strep, pneumococci,
Mycoplasma, Chlamydia,
Legionella, MAI
ETHAMBUTOL
 Antitubercular  Dose-related retrobulbar
 Synthetic butanol
optic neuritis
 Impaired red-green color
derivative
discrimination
 Monitor pts color
 Bacteriostatic against discrimination regularly
mycobacteria  Gouty arthritis
 Inhibits RNA synthesis

 M.tuberculosis
 MAI
FOSCARNET
 Antiviral  HA
 Pyrophosphate
 Diarrhea
 V
 Renal failure
 Blocks pyrophosphate-  Hypocalcemia
binding site on viral DNA  Hypokalemia
polymerase  Hypomagnesemia
 Prevents attachment of
 Anemia
nucleotide precursors to DNA  Arthralgia
 Myalgia
 CMV retinitis in HIV pts
 Acyclovir-resistant HSV in  Pentamidine causes life-
immunocompromised threatening hypocalcemia
FOSFOMYCIN
 ABX
 Cell wall synthesis inhibitor

 Inhibits enopyruvyl
transferase & addition of
phosphenolpyruvate to N-
acetylglucosamine to form N-
acetylmuramic acid

 Cystitis d/t E. coli or Enterococcus

faecalis

 Single dose Tx for UTI

GANCICLOVIR
 Antiviral ↓ visual acuity
 Nucleoside analogue  Neutropenia
 Thrombocytopenia
 Anemia
 Converted to
ganciclovir
triphosphate
 Inhibits
viral DNA
polymerase

 CMV infection in
immunocompromised &
transplants
GENTAMICIN
 Aminoglycoside ABX  Nephrotoxicity
 Ototoxicity
 Protein synthesis inhibitor
 Vestibular & cochlear
 ↑ w/ loop diuretics
 Binds 30s ribosome
 Prevents initiation of protein
synthesis
 Misreading of genetic code

 Gram (-) bacilli including

Enterobacteriaceace & P. aeruginosa
 Strep, enterococcal, & staph infections

 Monitor serum levels

GRISEOFULVIN
 Antifungal  HA
 Fungistatic ABX
 Induces CYP450
 Reduces plasma levels
 Deposits in keratin warfarin & OCP
precursor cells of skin,
hair, & nails
 Disrupts microtubules &
mitotis of dermatophytes

 Dermatophyte infections
 NOT Candida
IMIPENEM-CILASTATIN
 β-lactam ABX  Allergic rxns
 Diarrhea
 Carbapenem ABX &
 V
dehydropeptidase inhibitor
 Seizures
 ↑ risk w/ ganciclovir or
 Imipenem cyclosporine
 Binds PBP & inhibits cross-linking
cell wall peptidoglycan  Probenecid inhibits secretion & ↑
 Cilastatin serum levels
 Inhibits renal dehydropeptidase &
degradation of imipenem

 Endocarditis, pneumonia, UTI, pelvic,

abdominal d/t aerobic & anaerobic
ISONIAZID
 Antitubercular
 Nicotinic acid derivative
 Reduces catalase-peroxidase
 Inhibits synthesis of mycolic
acid component of cell wall
 Hepatitis
 Toxic metabolite acetyl-
hydrazine
 Peripheral neuropathy
 Vit. B6 deficiency

 TB

 Bimodal distribution d/t fast &

slow acetylation
 Inactivates vit. B6
ITRACONAZOLE
 Antifunal  GI distress
 Rash
 Synthetic triazole
 Hepatitis

 Inhibits 14-α-demethylase
 CYP450 enzyme that converts
lanosterol  ergosterol

 Blastomycosis, candidiasis,
coccidioidomycosis,
histoplasmosis
 Onychomycosis – nail beds
IVERMECTIN
 Antiparasitic  Vertigo
 Sedation
 Antihelmintic ABX

 Activates glutamate-gated Cl
ion channel
 Pharyngeal m.
hyperpolarization & paralysis

 Strongyloidiasis
 Cutaneous larva migrans
 Onchocerciasis filiariasis
 W. bancrofti
LEVOFLOXACIN
 Antibacterial
 Fluoroquinolone

 Inhibits bacterial DNA

topoisomerase type II (DNA gyrase)
& type IV
 Prevents DNA replication &
separation of chromosomes

 Community-acquired pneumonia
 UTI
 Gynecologic & skin infections

 Gram (+), gram (-), P. aeruginosa,

Mycoplasma, Mycobacterium
LINEZOLID
 Antibacterial  Inhibits MAO
 Oxazolidinone protein
synthesis inhibitor

 Binds 23s ribosomal RNA

of 50S subunit
 Prevents formation of 70s
initiation complex

 VRE, MS/MRSA, PCN-

sensitive pneumococci
MEFLOQUINE
 Antimalarial  Neuropsychiatric syn
 4-quinolone methanol derivative
 Hallucination
 Anxiety
 Confusion
 Inhibits erythrocytic schizogony  Seizure
 Inhibit nucleic acid synthesis  Coma

 Malaria
 Chloroquine-susceptible/resistant
trains of P. falciparum & P. vivax

 Perform CBC during chronic

prophylactic Tx
METRONIDAZOLE
 Antiprotozoal  GI pain
 Nitroimidazole  Anorexia
N
 Dizziness
 Reduced by
pyruvate:ferredoxin to  Alcohol
form nitro-free radicals causes disulfiram-
like effect
that attack DNA &
proteins

 Amebiasis, giardiasis,
trichomoniasis
 Balantidium coli, C. difficile,
B. fragilis
MUPIROCIN
 ABX
 Protein synthesis inhibitor

 Competes w/ isoleucine for

binding bacterial isoleucyl
tRNA synthetase
 Prevents addition of
isoleucine during protein
synthesis

 Impetigo by staph or strep

 Eradicate nasal colonization of
MRSA
 Infected traumatic skin lesions
NAFCILLIN
 β-lactam ABX  Diarrhea
 Superinfection
 Antistaphylococcal,
 Pseudomembranous colitis
penicillinase-resistant  Allergic rxn
penicillin  Rash
 Serum sickness
 Anaphylaxis
 Binds PBP
 Inhibits cross-linking of cell wall
peptidoglycan
 Probenecid inhibits renal tubular
secretion & ↑ serum levels
 Methicillin-sensitive
penicillinase producing staph
 Bone, jt, UTI, respiratory, skin,
endocarditis, meningitis
NITROFURANTOIN
 Urinary tract antibacterial  Anorexia
 Nitrofuran  N,V
 Neurotoxicity
 Pneumonitis
 Inhibits bacterial enzymes

 UTI  Probenecid inhibits urinary

 E. coli, S. saprophyticus excretion
OSELTAMIVIR
 Antiviral
 Neuraminidase inhibitor

 Inhibits influenza A & B

neuraminidase
 Prevents release &
spreading of viral particles

 Influenza A&B
PAROMOMYCIN
 Antiprotozoal  Nephrotoxic & ototoxic if
 Aminoglycoside ABX
given IV

 Inhibits protein synthesis

 Intestinal
amebiasis
 Cryptosporidiosis in
immunocompromised pts
PENICILLIN G
 β-lactam ABX  Diarrhea

 Narrow-spectrum  Superinfection
 Pseudomembranous colitis
penicillin
 Allergic rxn
 Rash
 Binds PBP  Serum sickness
 Inhibitscross-linking of cell  Anaphylaxis
wall peptidoglycan
 Probenecid inhibits renal
 Strep,pneumococcal, tubular secretion
meningococcal
 Syphilis
PENTAMIDINE
 Antiprotozoal  Nephrotoxic

 Amidino-pentane  Hematologic toxicity

 Hypoglycemia
derivative
 Allergic rxn
 Anaphylaxis
 Disrupts nucleic acid
synthesis in protozoa  Erythromycin ↑ fatal
arrhythmias
 P. carinii
 Early stage African
trypanosimiasis – sleeping
sickness
PIPERACILLIN-TAZOBACTAM
 β-lactam ABX  Diarrhea
 Superinfection
 Antipseudomonal penicillin & β-
 Pseudomembranous colitis
lactamase inhibitor
 Allergic rxn
 Rash
 Piperacillin  Serum sickness
 Binds PBP  Anaphylaxis
 Inhibits cross-linking of cell wall
peptidoglycan  Probenecid inhibits renal tubular
 Tazobactam secretion
 Inhibits class A β-lactamases

 Gram (-) bacilli, P. aeruginosa

PRAZIQUANTEL
 Antihelmintic  Malaise
 Isoquinoline derivative  Anorexia
 Drowsiness
 dizziness
 ↑ Ca permeability of
schistosome tegument
 Contraction & exposing
antigens to host immunity

 Schistosomiasis
 Chinese liver fluke
 Lung fluke
 Cestodes – tapeworms
PRIMAQUINE
 Antimalarial  Hemolytic anemia in G6PD
 8-aminoquinoline
deficiency
 methemoglobinemia

 Converted to oxidizing
quinoline-quinone
intermediates

 Eradicate exo-erythrocytic
forms of P. vivax & P. ovale
PYRIMETHAMINE
 Antiprotozoal  N
 Anorexia
 Folate reductase inhibitor
 Hypersensitivity rxn

 Inhibits folate reductase

 Folate deficiency in protozoa

 Malaria in combo w/ sulfadoxine

 Toxoplasmosis in combo w/
sulfadoxine

 NOT effective against P. vivax

PYRANTEL
 Antihelmintic  Abdominal cramps
 Pyrimidine analogue  Anorexia
 Diarrhea
V
 Activates cholinergic
nicotinic receptors in
somatic m. of nematodes
 Produces depolarizing NM
blockade

 Ascariasis
 Hookworm & pinworm
QUININE
 Antimalarial  Abdominal cramps
 Diarrhea
 4-aminoquinoline  V

 Binds plasmodial DNA &  Cinchonism

prevents replication &  Tinnitus
transcription during  Blurred vision
erythrocytic schizogony
 Metabolism
 Chloroquine-resistant malaria
 Cimetidine inhibits
 Rifampin induce
 Admin w/ doxycycline or
pyrimethamine-sulfadoxine
QUINUPRISTIN-DALFOPRISTIN
 Streptogramin ABX  Infusion site rxn
 Protein synthesis inhibitor

 Binds 50s ribosomal subunit

 Quinupristin
 Inhibits aminoacyl tRNA
synthesis & addition of AA
 Dalfopristin
 Inhibits peptidyl transferase

 VRE, MS/MRSA
RIBAVIRIN
 Broad-spectrum antiviral  Anemia
 Hypotension
 Guanosine analogue  Cardiac arrest

 Converted to ribavirin
triphosphate
 Depletes guanosine
triphosphate
 Inhibits viral RNA & protein
synthesis

 RSV in infants or children

 Chronic hepatitis C
 Viral hemorrhagic fever – Lass
fever
RIFAMPIN
 Antitubercular  Red discoloration of tears, urine,
saliva, sweat
 Rifampin derivative  Abdominal pain
 V
 Inhibits DNA-dependent RNA  Diarrhea
polymerase  Hepatitis

 TB  Induces CYP450
 Leprosy  ↓ levels
 Prophylaxis meningococcal meningitis  Warfarin
& H. flu B infections  Theophylline
 Itraconazole
 Steroids
 Opioids
 Phenytoin
 Verapamil
RITONAVIR-LOPINAVIR
 Antiretroviral  Anorexia
 HIV protease inhibitor V
 Altered taste
 Abnormal thinking
 Inhibits HIV protease &  Hyperlipidemia
conversion of gag-pol  Hyperlgycemia
polyprotein to functional
proteins
 Ritonavir
↑ lopinavir levels

 HIV in combo w/ nucleoside

reverse transcriptase inhibitor
STREPTOMYCIN
 Aminoglycoside  Nephrotoxic
 Ototoxic
 Protein synthesis inhibitor  ↑ w/ loop diuretics

 Binds 30s ribosome

 Prevents initiation of protein
synthesis
 Misreading of genetic code

 Drug-resistant TB
 Plague
 Tularemia

 IV admin
TERBINAFINE
 Antifungal  Itching
 Rash
 Allylamine  Diarrhea
 Anorexia
 Inhibits squalene oxygenase
& formation of squalene  Metabolism
epoxide during fungal  Cimetidine inhibits
membrane ergosterol  Rifampin induce
synthesis

 Topical
 Tinea corporis, cruris, pedis,
versicolor
 Oral
 Onychomycosis – fungal nail
infection
TRIFLURIDINE
 Antiviral  Ocular irritation
 Thymidine analogue
 Redness
 Itching

 Inhibits HSV DNA

polymerase

 Herpetickeratitis
 Keratoconjunctivitis

 Topical ocular admin

TRIMETHOPRIM-SULFAMETHOXAZOLE
 Antibacterial  N, V
 Rash
 Folate antagonist
 Stevens-Johnson syn
 Allergic rxn
 Sulfamethoxazole  Anemia
 Inhibits folate synthesis
 Hemolytic anemia
 Megalobalstic anemia
 Trimethoprim  Leukopenia
 Inhibits folate reduction  Thrombocytopenia
 Crystalluria
 UTI, traveler’s diarrhea
 Shigella enteritis  Added folate deficiency w/
 P. carinii & Nocardia pneumonia phenytoin or MTX
VANCOMYCIN
 Glycopeptide ABX
 Cell wall synthesis inhibitor
 Binds D-alanyl-D-alanine
portion of peptidoglycan
 Prevents cross-linking of D-
alanine & pentaglycine chain
 Red man syn
 Extensive rate of infusion
 Erythematous rash on face &
upper body
 Ototoxicity
 Vestibular & cochlear

 MRSA, penicillin-resistant
enterococci, C. difficile
ZIDOVUDINE
 Antiretroviral  Anemia
 Nucleoside reverse transcriptase
inhibitor

 Activated nucleotide triphosphate

incorporated into DNA causing
chain termination

 HIV
 Prevent maternal-fetal HIV
transmission

 1st line Tx for HIV infections

 Zidovudine w/ lamivudine or
emtricitabine & efavirenz or
lapinavir-ritonavir
ANTINEOPLASTIC
 Anastrozole  Imatinib
 Bleomycin  Leuprolide
 Busulfan  Meraptopurine
 Carmustine  Methotrexate
 Cisplatin  Paclitaxel
 Cyclophosphamide  Tamoxifen
 Doxorubicin  Trastuzumab
 Etoposide  Vincristine
 Fluorouracil
 Gemtuzumab ozogamicin
ANASTROZOLE
 Estrogen antagonist N
 Nonsteroidal aromatase  HA
inhibitor  Hotflashes
 Back pain
 Inhibits aromatase & conversion
to estrone precursor to estradiol
 Lowers estrogen levels
 Halts progression of estrogen-
sensitive breast cancers

 Breast cancer in postmenopausal

women
BLEOMYCIN
 Antitumor  Pneumonitis & pulmonary
 DNA intercalating fibrosis
 Hyperpigmentation
 Mucocutaneous toxicity
 Complexes iron-forming
oxygen free radicals that  Hematology toxicity
cause single strand breaks
 G2 phase specific

 Lymphomas
 SCC
 Testicularcarcinoma
 Choriocarcinoma
BUSULFAN
 Antineoplastic  N, V
 Alkyl sulfonate bifunctional  Myelosuppression
alkylating agent  Pulmonary fibrosis

 Cross-links DNA strands by

covalently bonding guanine
residues
 Prevents DNA replication &
transcription

 CML

 Use w/ cyclophosphamide prior

allogenic hematopoietic progenitor
cell transplant for CML
CARMUSTINE
 Antineoplastic  N, V
 Nitrosurea bifunctional  Hepatotoxicity
akylating agent  Anemia
 Leucopenia
 Cross-links DNA strands by  Thrombocytopenia
covalently bonding guanine  Pulmonary fibrosis
residues
 Prevents DNA replication &
transcription

 Brain tumors
 Myeloma
 Lymphoma

 Causes prolonged myelosuppression

CISPLATIN
 Antineoplastic  SevereN, V
 Platinum compound  Ototoxicity & tinnitus
 Hypocalcemia
 Forms reactive metabolites that  Hypokalemia
covalently bond DNA bases &  Hypomagnesemia
cross-link DNA strands
 Anemia

 Testicular, ovarian, cervical,

bladder, lung, head/neck cancers

 Less bone marrow suppression

CYCLOPHOSPHAMIDE
 Antineoplastic  Anorexia
 Nitrogen mustard bifunctional
 N, V
akylating agent
 Hemorrhagic cystitis & hematuria
 Alopecia
 Thrombocytopenia
 Cross-links DNA strands by  Leukopenia
covalently bonding guanine residues  Anemia
 Prevents DNA replication &
transcription  Rifampin induces CYP & ↑ toxicity

 Hodgkin’s ds
 Lymphomas, myeloma
 Leukemia
 Ovarian & breast tumors
 RA

 Converted to active metabolites by

CYP enzymes
DOXORUBICIN
 Antitumor  Colors urine red
 DNA intercalating agent
 Cardiomyopathy – dose-
limiting
 Inserts b/w DNA bases
 Causes deformation & uncoupling
 Anemia
 Complexes iron forming hydroxyl
 Leukopenia
free radicals that cause strand  Thrombocytopenia
breaks  Diarrhea
 Inhibits topoisomerase II  V
 Causes strand breaks  Stomatitis
 S phase specific  Alopecia

 Breast, ovarian, bladder tumors

 Bronchogenic carcinoma
 Lymphoma & leukemia
ETOPOSIDE
 Antineoplastic  N,V
 Podophyllotoxin, topoisomerase  Leukopenia
inhibitor  Thrombocytopenia
 Alopecia
 Inhibits mammalian
topoisomerase II & prevents
resealing of nicked DNA strands
 G2 phase specific

 Testicular, small cell lung

carcinoma
 Lymphoma
 Leukemia
FLUOROURACIL
 Antineoplastic  Diarrhea
 Pyrimidine antimetabolite V
 Stomatitis
 Converted to active nucleotide  Alopecia
form  Maculopapular rash
 Inhibits thymidylate  Anemia
synthetase
 Leukopenia
 S phase specific
 Thrombocytopenia
 Colon, breast, rectal, gastric,
pancreatic cancer
 Topical for basal cell carcinoma
& actinic keratosis
GEMTUZUMAB OZOGAMICIN
 Antineoplastic  Severe myelosuppression &
 Monoclonal Ab & cytotoxic hypersensitivity rxn
ABX calicheamicin  anaphylaxis
 Severe pulmonary rxns
 Gemtuzumab  Chills
 Binds CD33 Ag on hematopoietic  Fever
cells & sequesters lysosomes where
calicheamicin is released  N
 Calicheamicin  Dyspnea
 Causes DNA dbl strand breaks

 CD33 (+) AML

IMATINIB
 Antineoplastic  Cough
 Dyspnea
 Tyrosine kinase inhibitor
 Pharyngitis
 Pneumonia
 Inhibits oncoprotein bcr-abl
 Abdominal pain
tyrosine kinase expressed by
Philadelphia chromosome V
 Petechiae
 Inhibits leukemic cell
proliferation & induced  Pruritis
apoptosis  Rash
 Night sweats
 CML  Myalgia
 Cause hematologic & cytogenetic  Arthralgia
remission  Thrombocytopenia
 Neutropenia
LEUPROLIDE
 Antineoplastic, agent for precocious  Transient ↑ in testosterone w/ 1st
puberty dose
 Use flutamide or other androgen
 GnRH analogue antagonist
 Hot flashes
 Pulsatile admin ↑ FSH & LH
release
 Continuous admin down-regulates
GnRH receptors & ↓ FSH & LH

 Central precocious puberty

 Advanced prostate cancer
 Endometriosis
 Uterine fibroids

 IM depot & implants for prostate

cancer
MERCAPTOPURINE
 Antineoplastic  Cross-react w/ thioguanine
 Purine antimetabolite  Myelosuppression
 Hyperuricemia
 Converted to nucleotide  Hepatotoxicity
triphosphate by phosphoribosyl
transferase  Allopurinol inhibits degradation
 Inhibits purine biosynthesis &
salvage pathways
 S phase specific

 Acute leukemia
 CML
 Lymphomas

 Tumors that delete phosphoribosyl-

transferase acquire resistance
METHOTREXATE
 Antineoplastic  N, V
 Folate reductase inhibitor  Stomatitis
 Hepatotoxicity
 Anemia
 Inhibits dihydrofolate reductase  Leukopenia
 Prevents formation of active folate &  Thrombocytopenia
addition of single carbon units to DNA  Nephropathy
base precursors
 S phase specific

 Choriocarcinoma, trophoblastic tumors

 Leukemia
 Breast, head, neck, lung cancers
 Severe psoriasis
 RA
 Mycosis fungoides

 Leucovorin used to minimized hematologic

toxicity & Tx OD
PACLITAXEL
 Antineoplastic D
 Mitotic inhibitor  N,V
 Alopecia
 Anemia
 Binds tubulin & prevents
 Leukopenia
depolymerization of
microtubules of mitotic spindle  Thrombocytopenia
 M phase specific  Peripheral neuropathy
 Arthralgia
 Advanced ovarian cancer w/  Myalgia
cisplatin
 Non-small-cell lung cancer
 Metastatic ovarian or breast
cancer
TAMOXIFEN
 Antineoplastic  CI during pregnancy &
 Estrogen receptor antagonist & lactation
partial agonist
N
 Hotflashes
 Competes w/ estrogen for
 Menstrual irregularities
receptors in breast & other
tissues
 Suppresses breast tumor growth

 Breast cancer & ductal carcinoma

following surgery & radiation
 Advanced breast cancer
TRASTUZUMAB
 Antineoplastic  Abdominal pain
 Monoclonal Ab  Anorexia
 Diarrhea
 Binds human epidermal growth  V
factor-2 (HER2) receptor on breast
cancer cells
 Back pain
 Prevents receptor stim. & cell
 Chills
proliferation  Fever
 Regression of breast cancer  Allergic rxns
metastases
 Doxorubicin ↑ risk of
 Metastatic breast cancer w/
overexpression HER2 cardiotoxicity

 Combined w/ paclitaxel
 ↑ blood levels
VINCRISTINE
 Antineoplastic  N, V
 Vinca alkaloid, mitotic inhibitor  Alopecia
 Peripheral neuropathy
 Binds tubulin & prevents
polymerization of tubulin dimers
forming microtubules of mitotic
spindle
 M phase specific

 Hodgkin’s ds
 Lymphoma
 Leukemia
 Neuroblastoma
 Rhabdomyosarcoma
 Wilm’s tumor
AUTONOMIC &
NEUROMUSCULAR
 Atenolol  Pralidoxime
 Atropine  Propranolol
 Dobutamine  Pseudoephrine
 Edrophonium  Pyridostigmine
 Epinephrine  Rocuronium
 Phenoxybenzamine  Sildenafil
 Phentolamine  Succinylcholine
 Phenylephrine  Tamsulosin
 Pilocarpine  Terazosin
ATENOLOL
 Sympatholytic,  Bronchoconstriction w/
antihypertensive high doses b/c β1
 Β1 receptor antagonist blockade

 Additive hypotension
 β1 receptor antagonist
w/ nitrates
 Angina
 PostMI
 Hypertension
ATROPINE
 Anticholinergic  Mydriasis & cycloplegia
 Muscarinic receptor  Warm, dry, flushed skin
antagonist  Tachycardia
 Delirium
 Muscarinic receptor  Hallucinations
blocker

 Bradycardia
 IBS
 Anticholinesterase
poisoning
 Antisecretory agent
DOBUTAMINE
 Sympathomimetic, cardiac  Tachycardia
stimulant  Arrhythmia
 β1 receptor agonist

 Selective β1 receptor agonist

 β1 > β2 > α1

 Cardiac contractility &

output
 Acute heart failure
 Cardiogenic shock

 Synergistic on cardiac output

w/ nitroprusside
EDROPHONIUM
 Diagnostic agent  Muscarinic effects
 Cholinesterase inhibitor  Miosis
 Salivation

 Reversible
cholinesterase inhibitor

 Dx myasthenia gravis
EPINEPHRINE
 Sympathomimetic,  HTN
bronchodilator, vasopressor  Tachycardia
 Nonselective adrenergic  Ischemia
agonist  Hyperglycemia

 Activates α & β receptors

 ↑ IP3 & cAMP
 α1 – vasoconstrict & ↑ BP

 β1 – ↑ HR, conduction, &

contractility
 β2 – vasodilate, ↓ BP,
bronchodilate

 Cardiac arrest, V fib

 Shock, asthma
 COPD
PHENOXYBENZAMINE
 Vasodilator  Postural hypotension
 Irreversible α receptor
antagonist  Hypotension w/ β blockers
& Ca channel blockers
 α receptor antagonist
 α1 > α2

 Presurgical
Tx of HTN d/t
pheochromocytoma
PHENTOLAMINE
 Hypotension
 Vasodilator
 α receptor antagonist
 Severe hypotension w/
Epi
 Blocks α1 & α2
receptors

 Control BP during
surgical removal of
pheochromocytoma

 IV admin only
PHENYLEPHRINE
 Vasocontrictor, decongestant  Rebound nasal congestion
 HTN
 Selective α1 receptor
agonist  MAOI cause severe HTN

 Activates α1 receptor
 Increase IP3 causing
contraction of vascular
smooth m.

 Nasal & ocular decongestant

 Dilate pupil for opthalmoscopy
 Mydriasis w/o cycloplegia
 Paralysis of accommodation
PILOCARPINE
 Antiglaucoma,  Miosis
sialogogue  Blurred vision
 Muscarinic receptor  Accommodative spasm
agonist

 Activates muscarinic
receptors in ciliary m. &
salivary gland

 Sjogren’s syn
 Glaucoma
 Ciliary m. ↑ aqueous humor
 Xerostomia
 Salivary gland ↑ salivation
PRALIDOXIME
 Organophosphate antidote
 Cholinesterase reactivator

 Binds phosphorous & breaks

organophosphate bond w/
cholinesterase

 Organophosphate toxicity
 Reverses muscle weakness
PROPRANOLOL
 Sympatholytic,  Bronchoconstriction
antihypertensive  Inhibits glycogenolysis
 Nonselective β receptor  Nightmares & depression
antagonist

 Blocks β1 & β2 receptors

 Angina
 HTN
 Benign tremor
 Migraine prophylaxis
 thyrotoxicosis
 Post-MI

 Highly lipophilic  CNS

effects
PSEUDOEPHEDRINE
 Decongestant  Tachycardia

 Indirect/direct-acting  CNS stim.

↑ BP
adrenergic receptor
agonist
 MAOI cause severe HTN
 ↑ release NE directly
activates adrenergic
receptors causing
vasoconstriction &
cardiac stim.

 Allergic & viral rhinitis

PYRIDOSTIGMINE
 Antimyasthenic  Muscarinic effects
 Cholinesterase
 Miosis
 Salivation
inhibitor, cholinergic
agonist
 Prolongs effects of
succinylcholine
 Reversibly inhibits
cholinesterase

 Tx myasthenia gravis
 Reverse nondepolarizing
NM blockers
ROCURONIUM
 Paralytic agent  Respiratory m. paralysis
 Nondepolarizing NM blockade  Apnea

 Blocks nicotinic receptors in

skeletal m.

 Skeletal m. relaxation for

intubation, surgery, ECT

 Effects reversed by
neostigmine & edrophonium
SILDENAFIL
 Vasodilator  HA
 Phosphodiesterase  Nasalcongestion
inhibitor  Back pain
 Visual disturbances

 Inhibits type 5
phosphodiesterase &
degradation of cGMP
 vasodilationin corpus
cavernosum d/t Ach
release from sacral PNS
neurons

 Erectile dysfunction
SUCCINYLCHOLINE
 Respiratory m. paralysis
 Paralytic agent
 Apnea
 Depolarizing NM blockade

 Binds nicotinic receptors

causing prolonged
depolarization of skeletal m. &
paralysis

 Skeletal m. relaxation for

intubation & surgery

 Transient m. fasciculations
TAMSULOSIN
 Urologic agent  Dizziness
 Uroselective α1 receptor  HA
antagonist  Postural hypotension

 Blocks α1A receptors in  Cimetidine increases

prostate
blood levels & effects
 Tx urinary outflow
obstruction d/t prostatic
hyperplasia
TERAZOSIN
 Antihypertensive,  1st dose syncope
urologic agent
 Selective α1 receptor
antagonist

 Blocks α1 receptors

 HTN
 Outflow obstruction d/t
prostate hyperplasia
CARDIOVASCULAR
 Acetazolamide Hydrochlorothiazide
 Adenosine  Labetalol
 Amiloride  Mannitol
 Amiodarone  Methyldopa
 Amlodipine  Minoxidil
 Carvedilol  Nesiritide
 Clonidine  Nitroglycerin
 Digoxin  Nitroprusside
 Diltiazem  Propafenone
 Dofetilide  Quinidine
 Enalapril  Sotalol
 Esmolol  Spironolactone
 Fenoldopam  Valsartan
 Furosemide  verapamil
 Hydralazine
ACETAZOLAMIDE
 Diuretic  Parasthesia
 Carbonic anhydrase inhibitor  Urinary stone formation
 Inhibits interconversion of
carbonic acid & bicarbonate
 ↑ NaHCO3 excretion
 Inhibit aqueous humor
formation
 Hyperchloremic metabolic
acidosis
 Tx open-angle glaucoma
 Mtn sickness
 Metabolic alkalosis
ADENOSINE
 Antiarrhythmic  Transient asystole
 Purine nucleoside, cardiac
node membrane stabilizer

 Opens K channels &

blocks Ca influx in SA &
AV nodes
 Slows AV conduction
 ↑ AV refractory period

 Terminate SVT
AMILORIDE
 K-sparring diuretic  Hyperkalemia

 Epithelial Na channel
blocker

 Blocks Na Channel distal

tubule & collecting duct
 InhibitsNa reabsorption &
K excretion

 Prevent & Tx hypokalemia

AMIDARONE
 Antiarrhythmic  Hypo/hyperthyroidism

 Cardiac ion channel blocker  Photosensitivity

 Blue-gray skin
 Corneal microdeposits
 Blocks K, Na, Ca channels  Pulmonary fibrosis
& β receptors
 Prolongs repolarization
 ↑ refractory period
 Slows HR
 ↑ PR & QT intervals

 SVT, VT, VF
AMLODIPINE
 Antihypertensive,  HA
antianginal  Edema
 Dihydropyridine Ca
 Hypotension
channel blocker
 Effects ↑ w/ grapefruit
 Ca channel blocker in
vascular smooth m. juice
 Arteriolar vasodilation &
↑ coronary blood flow

 HTN
 Angina pectoris
CARVEDILOL
 Antihypertensive & heart  Orthostatic hypotension
failure Tx  Dizziness
 Nonselective adrenergic
 Bradycardia
receptor agonist

 Blocks β1, β2, α1 receptors

 Cause vasodilation

 HTN
 Heart failure
 ↓ remodeling
CLONIDINE
 Antihypertensive  Abrupt w/drawal  severe
 α2 receptor agonist rebound HTN
 Sedation
 Central α2 receptor agonist  Dry mouth
 ↓ sympathetic outflow from
vasomotor center
 Inhibits pain neurotransmission
in spinal cord

 HTN
 Opioid w/drawal
DIGOXIN
 Cardiac stimulant  Arrhythmias
 Digitalis glycoside  N,V
 Blurred vision
 Yellow vision
 Inhibits Na/K ATPase
↑ IC Ca & cardiac
contractility
 ↓ AV conduction
 ↑ AV refractory period

 Heart failure
 Serum levels assess dosage &
toxicity
DILTIAZEM
 Vasodilator, antiarrhythmic  Dizziness
 Non-dihydropyridine Ca  Hypotension
channel blocker  Peripheraledema
 Constipation
 Block Ca channels in cardiac  Gingival hyperplasia
tissue & vascular smooth m.
 Vasodilation
 ↓ HR & conduction  Grapefruit juice ↑ serum
 ↓ contractility levels

 HTN
 Angina pectoris
 SVT
DOFETILIDE
 Antiarrhythmic  QT prolongation
 K channel blocker  Torsade de pointes

 Blocks delayed K channels in

cardiac tissue
 Slows repolarization & prolongs
refractory period
 ↑ QT interval

 AF, A flutter

 Monitor QT interval during initial

dose titration
ENALAPRIL
 Antihypertensive  Cough & angioedema
 ACE inhibitor  Inhibits bradykinin
degradation
 Inhibits ACE & formation of AT II  Hypotension
 Vasodilation
 ↓ aldosterone secretion  Taste disturbances
 ↑ CO
 ↓ V remodeling
 ↑ survival in heart failure

 HTN
 Heart failure
 Post-MI
 ↓ progression of diabetic nephropathy
ESMOLOL
 Antiarrhythmic  Hypotension
 Class II
 Bradycardia
 Selective β1 blocker

 Blocks SNS stim. SA & AV nodes

 ↓ HR
 ↓ AV conduction
 ↑ AV refractory period

 Sinus tachycardia & SVT during/after

surgery

 Rapidly metabolized by plasma

esterase
FENOLDOPAM
 Antihypertensive ↓ serum K levels
 D1-like receptor agonist
 Monitor for hypokalemia

 D1 receptor agonist
 Arteriolar vasodilation
 Afferent & efferent renal
arterioles
↑ renal blood flow

 Hypertensive emergencies
FUROSEMIDE
 Loop-acting diuretic  Hypokalemia
 Membrane ion transport inhibitor  Metabolic alkalosis
 Hyperuricemia
 Hypomagnesemia
 Inhibits Na/K/2Cl cotransporter in
ascending loop of Henle
 Blocks NaCl reabsorption  ↑ ototoxicity of aminoglycoside
ABX
 Edema
 Heart failure
 HTN
 Hypercalcemia

 ↑ Ca excretion
 ↑ Na/K exchange in collecting duct
HYDRALAZINE
 Antihypertensive. heart failure  Edema
 Vasodilator  Reflextachycardia & MI
 Lupus syndrome

 Alters IC Ca metabolism
 Relaxes arteriolar smooth m.
 vasodilation
 ↓ afterload

 Heart failure in combo w/

isosorbide dinitrate
 More effective than ACEI in
black people
 Moderate-severe HTN
HYDROCHLOROTHIAZIDE
 Antihypertensive  Hypokalemia

 Thiazide diuretic  Metabolicalkalosis

 Hyperuricemia & gout

 Inhibits NaCl transporter ↓ excretion of lithium

in distal tubule
↑ excretion Na, K, Cl
 ↓ Ca excretion

 HTN
 Nephrogenic DI
 Nephrolithiasis
LABETOLOL
 Antihypertensive  Postural hypotension
 Adrenergic α & β receptor  Abrupt w/drawal cause
antagonist life-threatening HTN,
arrhythmias, or MI
 Selective α1 & nonselective
β1, β2 blockers

 HTN
MANNITOL
 Diuretic  Electrolyteimbalances
 Osmotic Diuretic  Transient volume expansion
 Pulmonary edema or heart
failure
 Osmotic attraction of
edematous & ocular fluid
 Filtered by glomerulus
↑ electrolyte excretion

 Oliguric renal failure

 Cerebral edema – ↑ ICP
 Acute glaucoma
METHYLDOPA
 Antihypertensive  Positive direct Coomb’s test
 Adrenergic α2 receptor
agonist

 Converted to active form

methyl-norepinephrine
which activates central α2
receptor agonist
↓ SNS outflow from
vasomotor center

 HTN
 HTN in pregnancy
MINOXIDIL
 Antihypertensive, hair growth  Systemic admin.
stimulant  Reflex tachycardia
 Vasodilator, K channel opener  Angina pericarditis

 Pulmonary HTN

 hypertrichosis
 Opens K channels in vascular
smooth m.
 Hyperpolarization
 m. relaxation
 vasodilation
 Stim. resting hair follicle 
growth follicles
 Severe HTN
 Topical for alopecia
NESIRITIDE
 Heart failure Tx  Hypotension
 Recombinant human B-type
natriuretic peptide

 Activate guanylate cyclase  ↑

cGaMP
 Dilates venous & arterial smooth
m.
 ↓ venous pressure, cardiac
preload, vascular congestion, &
dyspnea

 Decompensated heart failure

NITROGLYCERIN
 Antianginal  HA
 Organic nitrate  Hypotension
 Syncope
 Reflex tachycardia
 Releases NO in vascular smooth
m.
 Vasodilation ↑ vasodilative effect of
 ↑ coronary blood flow sildenafil, tadalafil,
 ↓ myocardial O2 demand vardenafil

 Angina pectoris
 Sublingual or lingual admin.
 Short half-life
NITROPRUSSIDE
 Antihypertensive  CN toxicity
 Vasodilator  Hypotension
 HA

 Relaxes venous & arteriolar

smooth m.
 Metabolized to CN & thiocyanate
 Tx toxicity w/ sodium nitrite &
sodium thiosulfate

 HTN crisis
 Acute heart failure or cardiogenic
shock
 Controlled hypotension during
pregnancy
PROPAFENONE
 Antiarrhythmic  Proarrhythmic 1st 2 wks
 Class IC Na channel  Monitor ECG when starting
blocker Tx
 GI disturbances
 Blocks Na channel in
cardiac tissue ↑ digoxin levels
 ↓ conduction & prevent re-
entry
 ↑ PR, QRS, & QT duration

 SVT & life-threatening V

arrhythmias
QUINIDINE
 Antiarrhythmic  Cinchonism
 Class IA Na channel  Blurred vision
blocker  Tinnitus

 Photophobia

 Blocks Na & K channels in

cardiac tissue ↑ levels w/
 ↓ conduction
 Amiodarone
 ↑ QRS & QT duration
 Cimetidine

 Diltiazem
 SVT & VT  Verapamil
 D-isomer = quinine, used
 Grapefruit juice
to treat malaria pts
SOTALOL
 Antiarrhythmic  Torsades de pointes
 Class III K channel blocker

 Blocks K channels in cardiac

tissue
 Prolongs repol.
 ↑ refractory period & ↑ QT
interval
 Blocks adrenergic β receptors

 SVT & life-threatening

arrhythmias
SPIRONOLACTONE
 K-sparring diuretic  Gynecomastia
 Aldosterone antagonist  Impotence
 Hyperkalemia
 Blocks aldosterone
receptors
 ↑ Na excretion
 ↓ K excretion

 Primary
hyperaldosteronism
 HTN
 hypokalemia
VALSARTAN
 Antihypertensive
 Angiotensin receptor antagonist

 Blocks AT II receptor in
vascular smooth m. & adrenal
cortex
 Vasodilation & ↓ aldosterone
secretion

 HTN
 Nephropathy

 Less cough & angioedema than

ACEI
VERAPAMIL
 Antihypertensive, antianginal  Peripheral edema
 Non-dihydropyridine Ca channel  Constipation
blocker  Gingival hyperplasia

 Blocks Ca channels in cardiac m. &

vascular smooth m.
 Vasodilation
 ↓ HR & conduction
 ↓ contractility
 Suppress contractility more than
other Ca channel blockers

 HTN
 Angina pectoris
 SVT
 Prevent migraine HA
CNS DEPRESSANTS
 Buspirone  Lorazepam
 Carbamazepine  Phenobarbital

 Diazepam  Phenytoin

 Disulfiram  Topiramate

 Ethosuximide  Valproate

 Flumazeil  Zolpidem

 Gabapentin

 Lamotrigine
BUSPRIONE
 Antianxiety  Dizziness
 5-HT1A partial agonist  Drowsiness
 Fatigue
 HA
 Activates presynaptic 5-HT1A  Excitement
receptors in dorsal raphe  Nervousness
nucleus  Blurred vision
 ↓ firing serotonergic neurons  Tachycardia
 N
 Generalized anxiety disorder  Rash
 Myalgia
 NO  Sweating
 Drug dependence
 Significant sedation
 Muscle relaxation
 ↑ levels by
 Anticonvulsant effects
 Erythromycin
 Itraconazole
 Grapefruit juice
CARBAMAZEPINE
 Anticonvulsant  Ataxia
 Neuronal Na channel blocker  Drowsiness
 Blurred vision
 Agranulocytosis
 Blocks Na channels in CNS  Aplastic anemia
 ↓ firing of ectopic foci &
spread of epileptic seizures
 Thrombocytopenia

 Partial seizures & generalized

 Induces its own metabolism
tonic-clonic seizures
 Bipolar disorders
 Trigeminal neuralgia
 Neuropathic pain
DIAZEPAM
 Antianxiety  Drowsiness
 Lethargy
 Benzodiazepine
 Physical/psychological
dependence
 Binds ω receptors on GABA  Tolerance
operated Cl ion channel
 ↑ channel affinity for GABA &
frequency of channel opening
 Potentiates inhibitory effects of
GABA

 Anxiety
 Status epilepticus
 Muscle spasm
 Alcohol w/drawal
 Anterograde amnesia

 Long-lasting active metabolites

DISULFIRAM
 Alcohol abuse Tx  Drowsiness
 Acetaldehyde dehydrogenase
inhibitor

 Inhibits acetaldehyde
degradation following alcohol
ingestion
 Blurred vision
 Chest pain
 Dizziness
 Palpitations
 N, V
 HA
 Weakness

 Reinforcement of alcohol
abstinence
ETHOSUXIMIDE
 Anticonvulsant  Dizziness
 Succimide  Drowsiness
 Gastric distress
 Binds T-type Ca N
channels in thalamic
neurons
 Suppresses nerve
transmissions to
motor cortex

 Generalized absence
seizures
 Petit mal epilepsy
FLUMAZENIL
 Antidote  Seizures
 Benzodiazepine  Dizziness
receptor antagonist  Emotional lability

 Blocks benzodiazepine
receptors

 Counteract adverse
effects of
benzodiazepines
 Respiratory depression d/t
IV OD

 CI in status epilepticus
GABAPENTIN
 Anticonvulsant  Ataxia
 GABA analogue  Dizziness
 Drowsiness
 Nystagmus
 ↑ GABA release from  Tremor
central neurons
 Inhibits neuronal
discharges from seizure
foci
 Inhibits pain
neurotransmission

 Partial
seizures
 Chronic pain
 Migraine prophylaxis
LAMOTRIGINE
 Skin rash in 1st 8 wk of
 Anticonvulsant
Tx
 Phenyltriazine  Can progress to Stevens-
Johnson syn
 Blocks voltage-sensitive  Ataxia
Na channels  Dizziness
 Release of glutamate  Drowsiness
 Prevents spread of seizure  Photosensitivity
foci discharges
↓ metabolism & ↑ ADR w/
 Adjunct/monotherapy for valproate
partial seizures in adults
LORAZEPAM
 Sedative-hypnotic, anxiolytic  Dizziness
 Drowsiness
 Benzodiazepine  Apnea & cardiac arrest w/ rapid IV
admin
 Binds benzodiazepine ω
receptors on GABA operate Cl
 Additive depression w/ alcohol & other
depressants
ion channel
 ↑ channel affinity for GABA &
frequency of channel opening
 Potentiates inhibitory effects of
GABA

 Anxiety
 Insomnia
 Preoperative sedation
 Light anesthesia
 Anterograde amnesia

 Flumazenil used to counteract

severe OD
PHENOBARBITAL
 Sedative-hypnotic,  Drowsiness
anticonvulsant  Lethargy
 Barbiturate
 Delirium
 Hangover
 Physical & psychological
 Binds GABA operated Cl ion dependence
channel increasing duration of
channel opening  Induces CYP P450 ↑ metabolism
 ↑ Cl influx in absence of of drugs
GABA

 Tonic-clonic & partial seizures

 Febrile seizures in children
 Preoperative sedation
 Short-term hypnotic

 ↑ folate requirement during

long-term Tx
PHENYTOIN
 Anticonvulsant  Ataxia
 Diplopia
 Hydantoin
 Nystagmus
 Gingival hyperplasia
 Blocks voltage-sensitive Na
channels
 Release glutamate
 Prevents spread of seizure foci
discharges

 Partial seizures
 Generalized tonic-clone seizures
 Status epilepticus following IV
diazepam

 Zero-order @ high doses

 Fosphenytoin for IV use
TOPIRAMATE
 Anticonvulsant  Ataxia
 Monosaccharide derivative  Dizziness
 Drowsiness
 Fatigue
 Block voltage-sensitive Na  Impaired concentration &
channels memory
 Augments GABA activation  Psychomotor slowing
of GABA receptors
 Blocks glutamate receptors
 Speech problems
 Diplopia
 Partial & tonic-clonic seizures
 Nystagmus

 Decrease dose in pts w/ renal

impairment
VALPROATE
 Anticonvulsant  Indigestion
 Branched-chain FA  N, V
 Dizziness
 Sedation
 ↑ GABA levels by ↑ release  Hepatotoxicity
or ↓ metabolism or reuptake
 Reduced Na dependent
action potentials

 Simple & complex absence

seizures
 Complex partial seizures
 Tonic-clonic seizures
 Myoclonic seizures
 Migraine prevention
 Manic phase of bipolar
ZOLPIDEM
 Non-benzodiazepine hypnotic
 Imidazopyridine

 Activates ω BZBP receptors

on GABA operated Cl ion
channel
 ↑ channel affinity for GABA
& frequency of channel
opening
 Neuronal
hyperpolarization

 Insomnia
ENDOCRINE
 Acarbose  Insulin
 Alendronate  Levothyroxine
 Calcitonin  Medroxyprogesterone
 Danazol  Metformin
 Desmopressin  Methimazole
 Ergocalciferol  Mifepristone

 Ethinyl estradiol &  Octreotide

drospirenone  Oxytocin
 Ethinyl estradiol &  Pioglitazone
norethindrone  Prednisone
 Finasteride  Raloxifene
 Fludrocortisone  Repaglinide
 Glyburide  Somatropin
 Hydrocortisone  Testosterone
ACARBOSE
 Antidiabetic  Intestinalbloating
 α-glucosidase inhibitor  Flatulence

 Inhibits intestinal enzyme ↑

that converts oral bioavailability of
oligosaccharides & metformin
disaccharides to glucose  ↓ iron absorption
 ↓ digestion of starch &
sucrose
 ↓ postprandial blood glucose
& HbA1c

 Type II DM
ALENDRONATE
 Bone resorption inhibitor  Absorption ↓ by Ca
 Bisphosphonate supplements, antacids,
foods, beverages (except
water)
 Prevents attachment of
osteoclast precursor cells to
bone
 ↓ metabolic activity of
osteoclasts & ability to
resorb bone

 Prevent/Tx
 Osteoporosis
 Corticosteroid-induced
osteoporosis
 Paget’s ds of bone
 hypercalcemia
CALCITONIN
 Ca hormone
 Thyroid gland hormone

 Binds calcitonin receptor on

osteoclasts
 ↑ cAMP & inhibits
osteoclast activity
 ↓ bone resorption, bone pain,
& serum [Ca]

 Postmenopausal osteoporosis
 Paget’s ds of bone
 hypercalcemia
DANAZOL
 Ovarian inhibitor  CI in pregnancy –
 Synthetic androgen, androgenic effects on
antiestrogen female fetus

 Feedback inhibits pituitary  Emotional lability

FSH & LH secretion ↓
ovarian estrogen secretion &  Deepening voice
stim. endometrial & breast  Acne
tissue.
 Hirsutism
 Endometriosis  Amenorrhea
 Fibrocystic breast ds  ↓ breast size
 Hereditary angioedema
 ↑ C1 esterase inhibitor &
C4 complement component
DESMOPRESSIN
 Posterior pituitary hormone
 Vasopressin, ADH analogue

 Mimics natural vasopression

 Increases water
reabsorption in kidneys
 Vasoconstriction

 DI
 Nocturnal enuresis
 Control bleeding in
hemophilia & wWF’s ds

 Intranasal, oral, or IV
ERGOCALCIFEROL
 Vit. D  Hypercalcemia
 Fat-soluble  Hypercalciuria

 Activated in liver & kidneys  Cholestyramine inhibits

to form calcitriol vit. D absorption
 ↑ Ca & phosphorus  Induce vit. D
absorption from gut metabolism
 Phenytoin
 Vit. D deficiency  Barbiturates
 Rickets, osteomalacia
 Chronic renal failure
 Familial hypophosphatemia
 Hypocalcemia d/t
hypoparathyroidism
 Postoperative & idiopathic
tetany
ETHINYL ESTRADIOL & DROSPIRENONE
 OCP  Drospirenone
 Estrogen & progesterone  Antiandrogenic
 Blocks aldosterone
 Feedback inhibit GnRH  ↓ salt & water retention
 ↓ BP
 Estrogen
 ↓ FSH secretion &
maturation of dominant  Thromboembolism
follicle  ↑ risk w/ smoking
 Progesterone  Edema
 Inhibits midcycle LH surge
& ovulation
 Efficacy ↓ w/
 Contraception  ABX
 Regulate menstrual cycle  Carbamazepine
 Acne in women  phenytoin
ETHINYL ESTRADIOL &
NORETHINDRONE
 OCP  Norethidrone
 Estrogen & progesterone  Slightly androgenic

 Feedback inhibit GnRH

 Thromboembolism
 Estrogen
 ↓ FSH secretion &  Edema
maturation of dominant  Depression
follicle
 Progesterone  Gallbladder ds
 Inhibits midcycle LH surge
& ovulation
 Contraception

 Regulate menstrual cycle

 Acne in women
FINASTERIDE
 Androgen synthesis inhibitor  CI pregnancy
 5-α-reductase inhibitor  Risk to male fetus
 Do NOT handle tablets

 Inhibits conversion
testosterone 
 Impotence
dihydrotestosterone & ↓
androgenic stimulation of
prostate & skin
 ↓ prostate size & promotes
hair growth

 BPH
 Male pattern baldness
FLUDROCORTISONE
 Corticosteroid  Hypokalemia
 Mineralocorticoid  ↑ by thiazide & loop
diuretics
 Activates aldosterone
receptors in renal distal
tubule
 ↑ Na reabsorption
 ↑ K & H excretion

 Adrenal insufficiency
 Addison’s ds
 Congenital adrenogenital syn

 Tx idiopathic orthostatic
hypotension w/ ↑ Na intake
GLYBURIDE
 Antidiabetic  Photosensitivity
 Sulfonylurea hypoglycemia  Hypoglycemia

 Closes ATP-sensitive K
channels preventing K efflux
& depolarizing pancreas B
cells
 Influx Ca & relaxing insulin
 ↑ amount of insulin secreted
during each pulse

 Type II DM
HYDROCORTISONE
 Short-acting corticosteroid,
low-potency topical
corticosteroid
 Glucocorticoid

 Replaces endogenous cortisol

in deficiency states
 Suppresses inflammation &
immune response – topical

 Adrenocortical insufficiency
 Topical
 Insect bites
 Contact dermatitis
INSULIN
 Antidiabetic  Hypoglycemia
 Pancreatic hormone

 β-blockers mask signs

 Replaces endogenous of hypoglycemia &
insulin prolong recovery

 DM

 Rapid acting – lispro

 Intermediate acting –
lente
 Long acting – ultralente
LEVOTHYROXINE
 Thyroid hormone  Insomnia
 Tetraiodothyronine  Irritability
 Tachycardia
 Binds nuclear receptors  Wt loss
& ↑ gene transcription
↑ metabolic rate, protein
synthesis,  Bileacid sequestrants ↓
gluconeogenesis, cell absorption
growth & differentiation,
& CNS development
 Converted to T3 in
tissues

 Hypothyroidism
MEDROXYPROGESTERONE
 Progestin, contraceptive  Amenorrhea
 Progesterone analogue  Breakthroughbleeding
 Dysmenorrhea
 ↓ endometrial hyperplasia in
women receiving estrogen
 Prevents conception by
thickening cervical mucus

 Estrogen-progestin HRT
 Injectable contraceptive
 Progestin-only injectable
contraceptive

 IM depot injection lasts 3mo

METFORMIN
 Antidiabetic  N,V, D
 Biguanide, antihyperglycemic  Abdominal bloating

 ↑ # & affinity of insulin

receptors in peripheral tissues
 ↓ hepatic glucose output
 ↓glucose absorption from gut
 ↑ glucose uptake & utilization in
skeletal m. & adipose tissue

 Type II DM

 Used in combo w/ sulfonylureas

METHIMAZOLE
 Antithyroid  Rash
 Thiourea, thyroid  Agranulocytosis
hormone synthesis
inhibitor

 Inhibits peroxidase &

iodination & coupling of
tyrosine residue of
thyroglobulin
 ↓ thyroxine secretion

 Hyperthyroidism –
Grave’s ds
MIFEPRISTONE
 Abortificient  Abdominal pain
 Progesterone antagonist  Diarrhea
 N,V
 Partial agonist or antagonist  Uterine bleeding
progesterone receptors
 Cramping
 Medical termination of
pregnancy through 49d
gestation

 Single dose + prostaglandin

for 48hr stim. uterine
contractions
OCTREOTIDE
 GH inhibitor, antidiarrheal  Arrhythmias
 Somatostatin analogue w/  Hyperglycemia
greater effects on GH than  Hypoglycemia
insulin secretion  Constipation
 Diarrhea
 Suppresses secretion of GH,  Flatulence
insulin-like growth factors, 5-
HT & GI peptides – gastrin,
 N
motilin, secretin, & VIP

 Acromegaly
 Severe diarrhea & flushing d/t
carcinoid tumors & VIP
tumors
 Bleeding GE varices
 Complications of pancreatic
surgery
OXYTOCIN
 Oxytocic  Excessive & painful
 Posterior pituitary hormone uterine contractions

 Stim. Uterine smooth m. &

induce labor
 Stim. mammary gland
smooth m. & lactation

 Induce labor @ term

 Facilitate uterine contractions
 Postpartum control of uterine
bleeding
 Promote milk let-down

 IV for uterine stim.

 Nasal for milk let-down
PIOGLITAZONE
 Antidiabetic
 Thiazolidinedione
antihyperglycemic

 Activates peroxisome
proliferator-activated receptor-γ
in adipose tissue, skeletal m., &
liver
 ↑ gene transcription, insulin
sensitivity, & glucose transports
in muscle & adipose tissue
 Suppresses hepatic glucose
output

 Type II DM

 Used w/ metformin
PREDNISONE
 Anti-inflammatory  Depression or euphoria
 Corticosteroid  HTN
 Acne
 Suppresses  Impaired wound healing
inflammation &  Adrenal suppression
immune response
 Muscle wasting
 Inflammatory, allergic,  Osteoporosis
autoimmune, & neoplastic  Cushingoid appearance
ds
 Prevent organ transplant
 Moon facies
 Buffalo hump
rejection
 Asthma ↑ susceptibility to
infection
RALOXIFENE
 Bone resorption inhibitor  Hot flashes
 Selective estrogen receptor
modulator – SERM  Cholestyramine inhibits
absorption
 Estrogen-like effect on bone
& lipid metabolism
 Estrogen antagonist in breast
& uterine tissue
 ↑ bone mineral density & ↓
vertebral fractures

 Osteoporosis in
postmenopausal women

 Used in woman @ risk for

breast cancer
REPAGLINIDE
 Antidiabetic  Hypoglycemia
 Meglitinide hypoglycemic

 Closes ATP-sensitive K
channels & ↑ insulin
secretion
 ↓ postprandial blood glucose
& [HbA1c]

 Taken before meals to control

postprandial hyerglycemia

 Used w/ metformin
 NOT sulfonylureas
SOMATROPIN
 GH
 Recombinant somatotropin

 ↑ release of insulin-like
growth factors in liver &
cartilage
 Stim. skeletal growth, AA
transport, protein synthesis,
nucleic acid synthesis & cell
prolif.

 Short stature in children d/t

GH deficiency
 Turner syn
 Chronic renal failure
 Prader-Will syn
TESTOSTERONE
 Androgen  Edema
 Gonadal steroid  Acne
 Gynecomastia
 Activated gene transcription &  Impotence
development of male sex organs &
secondary sex characteristics
 Oligospermia
 ↑ lean body mass
 Priapism
 Stim. skeletal growth
 Accelerates epiphyseal closure
 ↑ sebaceous gland sebum production
 ↑ EPO secretion
 ↓ HDL levels

 Hypogonadism in androgen-deficient
men
 Delayed puberty in males
GASTROINTESTINAL
 Bisacodyl  Misoprostol
 Calcium carbonate  Omeprazole
 Dicyclomine  Ondansetron
 Docusate  Promethazine
 Lactulose  Ranitidine
 Loperamide  Sucralfate
 Mesalamine  Tegaserod
 Metoclopramide
BISACODYL
 Stimulant laxative  Cramping
N
 Inhibits GI fluid  Fluid & electrolyte
reabsorption & depletion
stimulates peristalsis  Hypokalemia

 Bowel evacuation prior

colonoscopy or surgery
 Acute constipation
CALCIUM CARBONATE
 Antacid, Ca supplement  Constipation
 Ca salt
 ↓ absorption of drugs
 Tetracyclines
 Neutralizes gastric acid  Fluoroquinolones
 Provides Ca supplementation  Phenytoin
 Iron salts
 Dyspepsia
 Hypocalcemia
 Prevention of osteoporosis

 Admin 1-1.5hr after meals &

@ bedtime
DICYCLOMINE
 Antispasmodic  Constipation
 Muscarinic receptor  Dyspepsia
antagonist  Dry mouth
 Urinary retention
 Blurred vision
 Blocks PNS stim.  Decreased sweating
intrinsic nervous system
& ↓ GI tone & motility
 Directly
relaxes GI
smooth m.

 IBS – cramping & pain

DOCUSATE
 Stool softener, laxative
 Surface-active agent

 Facilitates hydration of
fecal material & softens
feces

 Constipation
 Fecalimpaction – rectal
enema
LACTULOSE
 Laxative  Cramping
 Abdominal distention
 Osmotic agent
 Flatulence

 ↑ water content & softens

feces
 Lowers pH of colon
 Converts ammonia 
ammonium ion & ↓
ammonia absorption &
blood levels

 Chronic constipation
 Hepatic encephalopathy
 Improves mental status
LOPERAMIDE
 Antidiarrheal  Constipation
 Opioid analogue
 Drowsiness

 Additive effects
 Activates opioid receptors in GI  Kava
smooth m.  Chamomile
 Segmental contraction & inhibits  Valerian
peristalsis

 Mild-moderate acute diarrhea

 Chronic diarrhea d/t IBD
 ↓ volume of ileostomy drainage

 AVOID
 Pregnancy
 Lactation
 Children < 2 y/o
MESALAMINE
 GI anti-inflammatory
 Salicylate – 5-ASA

 Inhibits prostaglandin synthesis

& migration of inflammatory
cells into bowel wall
 Scavenges superoxide-free
radicals

 IBD
 UC
 Proctitis

 Sulfasalazine  mesalamine &

sulfapyridine
METOCLOPRAMIDE
 Promotility & antiemetic  CI in Parkinson’s ds & seizure
disorders
 D2 receptor antagonist
 Drowsiness
 Blocks relaxant effect of D on  EPS rxns
GI smooth m.  restlessness
 Blocks presynaptic D receptors
& ↑ Ach release & stim. smooth
m.
 Blocks D2 receptors in
chemoreceptor trigger zone &
vomiting center

 Chemotherapy-induced emesis
 Gastric stasis – postsurgical &
diabetic
 GE reflux
MISOPROSTOL
 Cytoprotective  CI in pregnancy
 Synthetic PGE1
analogue  Abdominal pain
D
 Miscarriage
 ↓ gastric mucosal
secretion & ↑ secretion
of bicarbonate & mucus

 Prevent gastric mucosal

injury from NSAIDs
 Abortificient in combo w/
mifepristone
OMEPRAZOLE
 Antiulcer  Abdominal pain
 Proton pump inhibitor
 Inhibits metabolism
 Diazepam
 Irreversibly inhibits H/K  Cyclosporine
ATP pump in gastric parietal  Phenytoin
cells
 Prevents gastric acid
secretion

 Peptic ulcer ds
 GE reflux
 Zollinger-Ellison syn
 dyspepsia
ONDANSETRON
 Antiemetic  HA
 Constipation
 5-HT3 receptor antagonist
 D

 Blocks 5-HT3 receptors in

GI vagal afferent nerves,
solitary tract nucleus, &
chemoreceptor trigger zone

 Prevent N, V from
chemotherapy & radiation
therapy
 Postoperative N, V
PROMETHAZINE
 Antiemetic, antihistamine,  Neuroleptic malignant syn
sedative
 H1 receptor antagonist,  Sedation
phenothiazine  Confusion
 Disorientation

 Blocks H1 & M1 receptors

 Inhibits stim. chemoreceptor
trigger zone & vomiting
center

 N, V
 Preoperative sedation
 Allergic rxns
RANITIDINE
 Antiulcer
 H2 receptor antagonist

 Blocks H2 receptors in
gastric parietal cells
↓ gastric acid secretion

 Pepticulcer ds
 GE reflux
 Dyspepsia
SUCRALFATE
 Antiulcer  Constipation
 Cytoprotective, sulfated
polysaccharide  ↓ absorption
 Fat soluble vitamins
 fluoroquinolones
 Adheres ulcer crater & forms
protective barrier
 Prevents acid secretion & pepsin
hydrolysis of mucosal proteins
 Stim. prostaglandin synthesis

 Peptic ulcer ds
 GE reflux
 Prevent NSAID-induced gastric
injury
TEGASEROD
 GI motility agent  Diarrhea
 Partial agonist @ 5-HT4  Ischemic colitis
receptors

 Activates 5-HT4
receptors on sensory
neurons in enteric
nervous system
 Release
neurotransmitters & ↑
peristalsis

 IBS in women w/
constipation
HEMATOLOGIC
 Abciximab  Epoetin
 Alteplase  Eptifibatide
 Aspirin  Ezetimibe
 Atorvastatin  Filgrastim
 Bivalirudin  Folic acid
 Cholestyramine  Gemfibrozil
 Cilostazol  Heparin
 Clopidogrel  Niacin
 Cyclosporine  Sirolimus
 Enoxaparin  Warfarin
ABCIXIMAB
 Antithrombotic  Bleeding

 Monoclonal Ab  Thrombocytopenia

 Inactivates platelet gp
llb/llla receptors
 Prevents platelet
aggregation

 Preventthrombosis during
coronary angioplasty & stent
placement
ALTEPLASE
 Thrombolytic  Reperfusion arrhythmia
 Plasminogen activator
 Contraindications
 Internal bleeding
 Converts plasminogen   Recent CNS surgery or trauma
plasmin
 Degrades fibrin & fibrinogen

 AMI
 Acute ischemic stroke
 Occluded central venous access
devices

 Streptokinase & urokinase for

pulmonary embolism
ATORVASTATIN
 Cholesterol lowering agent  Myalgia
 HMG-CoA reductase inhibitor  Myositis
 Rhabdomyolysis
 Hepatitis
 HMG-CoA reductase, rate-  GI distress
limiting enzyme for cholesterol
 ↑ hepatic cholesterol uptake
 ↓ LDL levels
 Effects ↑ w/
 Grapefruit juice
 Azole antifungals
 Hypercholesterolemia  cyclosporine
 Cholesterol-lowering effects ↑ w/
ezetimibe & bile acid-binding
agents
BIVALIRUDIN
 Anticoagulant  Bleeding
 Hirudin analogue

 Inhibits thrombin
 Prevents blood coagulation

 Thrombosis in unstable angina

 AMI
 Stent insertion

 Used in pts w/ heparin-induced

thrombocytopenia
CHOLESTYRAMINE
 Cholesterol-lowering agent  Constipation
 Bile-acid binding resin  Abdominal discomfort

 Binds intestinal bile acids

 Prevents reabsorption
 ↑ cholesterol utilization
 ↓ LDL levels

 Hypercholesterolemia
 Diarrhea d/t excess bile acids
CILOSTAZOL
 Antiplatelet  HA
 Platelet aggregation inhibitor
 Effects ↑ w/ CYP3A4 inhibitors
 Inhibits phosphodiesterase III &  Azole antifungals
↑ cAMP in platelet & blood  Erythromycin
vessels  Grapefruit juice
 Inhibit platelet aggregation
 Causes vasodilation

 Intermittent claudication
 Improves blood flow & walking
distance

 Additive effects w/ aspirin

CLOPIDOGREL
 Antiplatelet  Hypersensitivity reaction
 Platelet aggregation inhibitor

 Irreversibly inhibits binding of

ADP to platelet receptors
 ↓ gp IIb/IIIa mediated
aggregation

 Stroke
 MI
 Peripheral vascular ds

 Additive effects w/ aspirin

CYCLOSPRINE
 Immunosuppressant  HTN
 IL2 expression inhibitor  Nephrotoxic
 Gingival hyperplasia
 Hirsutism
 Bind immunophilins  Tremor
 Complex binds calcineurin
 inhibits transcription of
IL2 gene  Induce metabolism
 Rifampin
 Barbiturates
 Prevent rejection of renal,
 Carbamazepine
cardiac or hepatic allografts
 Severe RA & psoriasis
 Inhibits metabolism
 Grapefruit juice
ENOXAPARIN
 Parenteral anticoagulant  Thrombocytopenia
 LMWH

 Binds/potentiates antithrombin III

on factor Xa

 Prevent
 DVT
 Pulmonary embolism after knee, hip,
or abdominal surgery
 Thrombosis in unstable angina & non
Q-wave MI

 Effects reversed w/ protamine

sulfate
 NO monitoring w/ PTT
EPOETIN
 Hematopoietic growth factor  HTN
 Recombinant human EPO

 Binds receptors on erythroid

progenitor cells & stim. cell
maturation & prolif.
 Reticulocytosis & ↑ Hct

 Anemia d/t
 CRF
 Chemotherapy
 Zidovudine therapy
 Hematologic malignancy
 lymphoma

 Used as performance-enhancing drug

by athletes
EPTIFIBATIDE
 Antiplatelet
 GP IIb/IIIa receptor antagonist  Bleeding

 Reversibly inhibits fibrinogen

binding to gp IIb/IIIa receptors
 Prevents platelet aggregation

 Prevent coronary thrombosis in

 Unstable angina or non-ST
segment elevation MI
 Coronary angioplasty or stent
placement
EZETIMIBE
 Cholesterol-lowering agent
 Cholesterol absorption inhibitor

 Disrupts annexin-caveolin complex

mediating cholesterol transport
intestinal brush border
 Inhibits absorption of biliary
dietary cholesterol
 Pro-drug converted to active
glucuronide metabolite

 Hypercholesterolemia

 Additive effect w/ statins

FILGRASTIM
 Hematopoietic growth factor  Bone pain
 Recombinant human GCSF

 Binds receptors on myeloid

progenitor cells & stim. maturation
& prolif.
 Accelerates neutrophil recovery
after myelosuppressive
chemotherapy
 ↓ infection incidence

 Neutropenia assoc/ w/ chemotherapy

& bone marrow transplants

 Avoid 24 hrs prior & after

chemotherapy
FOLIC ACID
 Vitamin, hematologic agent  Absorption ↓ by
 Metabolic cofactor for DNA  Phenytoin
synthesis  Cholestyramine

 Folate reductase inhibited by

 Activated folate transfer one- MTX
carbon units to purine &
pyrimidine precursors

 Megaloblastic anemia
 Fetal neural tube defects
 Coronary artery ds

 Pregnant woman have ↑

requirements
GEMFIBROZIL
 Lipid-lowering agent  GI distress
 Myositis
 Fibric acid derivative
 Statins ↑ risk rhabdomyolisys
 Activates peroxisome
proliferator activated receptor-α
 Oxidizes FA & apo-AI & AII
 ↓ plasma triglycerides
 ↑ HDL

 Hypertriglyceridemia
 ↓ HDL levels

 Monitor LFTs throughout Tx

HEPARIN
 Parenteral anticoagulant Thrombocytopenia
 Antithrombotic

 Binds/potentiates antithrombin III

 ↑ inactivation factor Xa & thrombin

 Venous thromboembolism
 Pulmonary embolism
 AF w/ embolism
 Consumptive coagulopathies
 In vitro & catheter coagulation

 Monitor PTT
 Protamine sulfate for OD
NIACIN
 Vitamin, lipid-lowering agent  Flushing
 G-protein coupled receptor  Pruritis
ligand  GI distress, peptic ulcer
 Hyperglycemia
 Hepatotoxicity
 Activates G-protein coupled
receptor
 Inhibits lipolysis & release of FA
 Statins ↑ risk rhabdomyolysis
 ↓ hepatic triglyceride synthesis
& VLDL secretion

 Hypertriglyceridemia
 ↑ HDL
 Hypercholesterolemia
 Pellagra
SIROLIMUS
 Immunosuppressant  Leukopenia
 T-lymphocyte inhibitor  Thrombocytopenia
 Hyperlipidemia
 Rash
 Inhibits regulatory kinase
in cytokine-driven T-cell  ↑↑
prolif. blood levels
 Combo
 Cyclosporine
w/ corticosteroid &  Azole antifungals
cyclosporine
 Erythromycin

 Grapefruit juice
 Prevent
 Cimetidine
 Rejection renal allograph
 Coronary stent restenosis
WARFARIN
 Oral anticoagulant  Fetal malformations
 Abnormal bone development
 Coumarin vit. K antagonist

 Inhibits reduction of oxidized

vit. K
 Prevents vit. K dependent
carboxylation of glutamate
residues of factors II, VII, IX, X,
proteins C & S

 Delayed onset d/t circulating

coagulation factors

 Monitor INR
 Give vit. K if bleeding
MUSCULOSKELETAL
 Acetaminophen  Indomethacin
 Allopurinol  Infliximab

 Celecoxib  Ketorolac

 Cyclobenaprine  Probenecid & colchicine

 Etanercept

 Ibuprofen
ACETAMINOPHEN
 Analgesic, antipyretic  OD cause fatal hepatic failure
 COX-3 inhibitor
 ↑ hepatotoxicity w/ alcohol
 ↑ renal toxicity w/ salicylates &
 Inhibits COX-3 selectively NSAIDs
 Inhibits synthesis of PG causing
pain & fever

 Mild-moderate pain
 Fever

 Lacks anti-inflammatory &

antiplatelet activity
ALLOPURINOL
 Antigout  Rash
 Xanthine oxidase inhibitor
 Inhibits metabolism
 Mercaptopurine
 Inhibits xanthine oxidase
& catabolism of purines 
xanthine & uric acid
↓ uric acid levels

 Prevent hyperuricemia &

gout
CELECOXIB
 NSAID  GI bleeding
 COX-2 inhibitor  ↑ risk stroke & MI

 Inhibits COX-2 &

synthesis of PG causing
pain, fever, &
inflammation

 OA
 RA
 Inflammatory jt ds
CYCLOBENZAPRINE
 Skeletal m. relaxant  Dizziness

 Tricyclic central-acting m.  Drowsiness

 Dry mouth
relaxant
 AVOID MAOI
 Acts on brainstem & spinal
cord to reduce tonic
somatic m. activity via γ &
α motor neurons

 Acute muscle spasm

ETANERCEPT
 Antirheumatic agent,  URI
antitumor necrosis factor  HA
 Antitumor necrosis factor
– p57 combined w/ Fc of ↓ Ab response to live virus
IgG vaccines

 Binds TNF-α & ↓ jt

inflammation & pain
 Slows progression of RA

 RA
IBUPROFEN
 NSAID  GI bleeding
 Nonselective COX inhibitor  N, V
 Dyspepsia
 Allergic rxns
 Inhibits COX-1 & COX-2 &  Hepatitis & renal failure
synthesis of PG causing pain,
fever, & inflammation

 Mild-moderate pain or
dysmenorrhea
 Inflammatory disorders
 OA
 RA

 ↓ risk colon, breast, lung, &

prostate cancers
INDOMETHACIN
 NSAID  GI bleeding
 Nonselective COX inhibitor  N, V
 Dyspepsia
 Allergic rxns
 Inhibits COX-1 & COX-2  Dizziness
 Drowsiness
 Inflammatory disorders  HA
 Gouty arthritis
 OA
 RA
 Ankylosing spondylitis
 PDA in premature neonates
INFLIXIMAB
 Ds modifying antirheumatic  Fatigue
 Monoclonal Ab to TNF-α  N,V
 URI

 Inactivates TNF-α & ↓ jt

inflammation, pain, &
destruction
 ↓ Sx of Crohn’s ds

 RA
 Crohn’s ds
KETOROLAC
 NSAID  Aspirin-allergy
 Allergic rxn in pt w/ asthma
 Nonselective COX inhibitor
 Nasal polyps

 Inhibits COX-1 & COX-2 &

synthesis of PG causing pain,
fever, & inflammation

 Short-term pain management

 Prolongs bleeding time

 Limit use to < 5d
PROBENECID & COLCHICINE
 Antigout  Probenecid
 Uricosuric – probenicid  Inhibits renal tubular secretion of
Penicillins
 Anti-inflammatory – colchicine  Used to ↑ penicillin serum levels
 Colchicine
 Probenecid  D
 Inhibits renal reabsorption of uric  N, V
acid & ↑ uric acid secretion  Agranulocytosis & aplastic anemia
 Colchicine
 Inhibits leukocyte response to
monosodium urate crystals in jt

 Acute gouty arthritis

 Prevent gouty arthritis
NEURODEGENERATIVE
 Baclofen  Levodopa-carbidopa
 Benztropine  Memantine

 Donepezil  Pergolide

 Entacapone  Selegiline

 Interferon-beta-1b
BACLOFEN
 Antispasticity  Drowsiness
 Dizziness
 GABA-B receptor agonist
 Fatigue
 Weakness
 ↓ neuronal cAMP & Ca influx
 ↑ K influx
 ↓ motor neuron excitability &
 Additive effects
 Alcohol
inhibits spinal reflexes  Kava
 Valerian
 Spasticity  Chamomile
 MS
 Spinal cord injury
 ALS
BENZTROPINE
 Anti-Parkinson  Blurred vision
 Central anticholinergic  Dry eyes
 Constipation
 Dry mouth
 Blocks cholinergic receptors &  Urinary retention
restores neurotransmitter
balance in basal ganglia

 Parkinson’s ds
 Drug-induced EPS

 ↓ tremor > bradykinesia &

rigidity
DONEPEZIL
 Anti-Alzheimer  N, D
 HA
 Cholinesterase inhibitor

 Inhibits cholinesterase in CNS

 ↑ Ach neurotransmission
 Slows decline in cognitive
function

 Alzheimer’s ds

 Does NOT prevent ds

progression
ENTACAPONE
 Anti-Parkinson  Rhabdomyolysis
 Neuroleptic malignant syndrome
 Catechol-O-methyltransferase
inhibitor

 Inhibits catechol-o-
methyltransferase inactivation
of levodopa
 ↑ levodopa in CNS
 Prolongs response to levodopa & ↓
S/Sx Parkinson’s ds

 Adjunct to levodopa/carbidopa for

Parkinson’s ds

 AVOID nonselective MAOI

INTERFERON-BETA-1B
 Anti-multiple sclerosis  HA
 Interferon  Weakness
 GI distress
 Sweating
 Binds cell surface  Neutropenia
receptors producing  Myalgia
immuno-suppressive  Chills
effects  Fever
↓ relapse & slows physical
disability in MS

 Relapsing-remitting MS

 SubQ daily
LEVODOPA-CARBIDOPA
 Anti-Parkinson  Dyskinesia – involuntary movements
 Dopamine precursor, decarboxylase
 N, V
inhibitor  Hallucinations

 ↑ arrhythmia w/ halothane
 Levodopa
 Converted to D in CNS
 Augments neurotransmission in basal
ganglia
 Carbidopa
 Inhibits peripheral dopa-decarboxylase
 ↑ levodopa availability in CNS

 Parkinson’s ds

 HTN crisis w/ MAOI

MEMANTINE
 Anti-Alzheimer
 Glutamate antagonist

 Glutamate NMDA
receptor antagonist
 Prevent excitotoxic effects
of glutamate causing
neuronal loss
 Slows decline in cognitive
function

 Alzheimer’s ds
PERGOLIDE
 Anti-Parkinson  Dyskinesia
 Hallucination
 Dopamine receptor
 Orthostatichypotension
agonist
 Constipation

 Activates D receptors in
basal ganglia

 Parkinson’sds in conjunction
w/ levodopa/carbidopa
SELEGILINE
 Anti-Parkinson  AVOID
 Meperidine & opioids
 Type B MAOI  Fatal rxn
 Excitation
 Rigidity
HTN
Converted to active form by

  coma
MAO  SSRI
Serotonin syn
Irreversibly inhibits D


 Tricyclics
degradation by MAO  Asystole
 ↑ response to levodopa/carbidopa Tx  HTN
 Syncope
 Rigidity
 Parkinson’s ds w/  seizures
levodopa/carbidopa

 Slows progression of Parkinson’s ds

OTHER DRUGS
 Alprostadil  Latanoprost
 Bosentan  Mesna

 Epoprostenol  Succimer
ALPROSTADIL
 Vasodilator  IV infusion
 Prostaglandin E1  Apnea
 Hypotension
 Arrhythmia
 Activates PG EP receptors  Local products
 Vascular smooth m. relaxation  Prolonged/painful erection
& vasodilation  lightheadedness

 Maintain PDA in neonates

awaiting surgery
 IV infusion
 Male erectile dysfunction
 Local injection or pellets
BOSENTAN
 Vasodilator  CI in pregnancy
 Endothelin-1 receptor  Causes birth defects
antagonist
 ↑ serum aminotransferase levels
 Blocks endothelin A & B
receptors
 ↓ pulmonary vascular resistance
& dyspnea
 Improves walking distance

 Pulmonary arterial HTN

EPOPROSTENOL
 Vasodilator  Flushing
 Naturally occurring prostacyclin  Hypotension
(PGI2)  Tachycardia
 Diarrhea
 N, V
 Activated prostaglandin IP
receptors
 Vascular smooth m. relaxation
 ↑ pulmonary blood flow &
reduces dyspnea

 Pulmonary arterial HTN

LATANOPROST
 Ocular hypotensive agent  Alters color of iris causing
permanent eye color change by ↑
 Prostaglandin F2α analogue amount of melanin in melanocytes

 Activates prostaglandin FP
receptors
 ↑ aqueous humor outflow via
uveoscleral pathways
 Lowers intraocular pressure

 Chronic open-angle glaucoma

 Topical ocular admin

MESNA
 Antidote
 Sulfhydryl compound

 Detoxifies urotoxic
metabolites acrolein of
ifosfamide &
cyclophosphamide

 Hemorrhagic cystitis d/t

ifosfamide &
cyclophosphamide
SUCCIMER
 Antidote
 Metal chelating agent –
dimercaptosuccinic acid

 Chelates lead
 Water-soluble chelates to
excreted in urine
 ↓ blood lead levels
PSYCHOTHERAPEUTICS
 Amitriptyline
 Amphetamine &  Methylphenidate
dextroamphetamine  Mirtazapine
 Atomoxetine  Olanzapine
 Buproprion  Phenelzine
 Desipramine  Risperidone
 Fluoxetine  Thioridazine
 Haloperidol  Venlafaxine
 Lithium
AMITRIPTYLINE
 Antidepressant  Lethargy
 Sedation
 Tricyclic  Blurred vision
 Constipation
 Blocks neuronal reuptake of  Urinary retention
serotonin > norepinephrine  ↑ appetite & wt gain
 Blocks muscarinic & α-adrenergic  OD wide QRS complex VT
receptors
 Altered effects by drugs that inhibit/induce
CYP450
 Chronic pain  Carbamazepine
 Depression  Quinidine
 Rifampin
 Delayed onset of antidepressant effect
>4 wks

 AVOID
 MAOI
 SSRI
AMPHETAMINE
 CNS stimulant  Tachycardia
 Sympathomimetic amine
 HTN
 Anorexia
 Irritability
 ↑ neuronal release of  Insomnia
norepinephrine  Tremor
 Growth inhibition
 Drug dependence
 ADHD
 ↑ attention span  HTN crisis w/ MAOI
 ↓ motor restlessness
 Narcolepsy
 ↑ mental alertness
 ↓ drowsiness & fatigue
ATOMOXETINE
 ADHD agent  ↓ appetite
 Insomnia
 Selective NE reuptake
inhibitor
 Levels & effects altered by drugs
that inhibit/induce CYP2D6
 Inhibits neuronal reuptake of
NE in CNS

 ADHD in children/adults

 ↑ levels & effect in slow

metabolizers – CYP2D6
BUPROPION
 Antidepressant  Agitation
 Neuronal reuptake  HA
inhibitor  Dry mouth
N
 Inhibits neuronal reuptake  Tremor
of DA > 5-HT & NE  Impaired motor & cognitive
skills
 Depression
 Smoking cessation  MAOI ↑ adverse effects
 Seizure risks w/
 Delayed onset for phenothiazines
antidepressant effects
DESIPRAMINE
 Antidepressant  Lethargy
 Tricyclic  Sedation
 Blurred vision
 Constipation
 Blocks neuronal reuptake NE > 5-  Urinary retention
HT  ↑ appetite & wt gain
 Blocks muscarinic & α-adrenergic
receptors  OD wide QRS complex VT

 Depression
 Chronic pain

 Delayed onset for antidepressant

effects

 AVOID
 MAOI
 SSRI
FLUOXETINE
 Antidepressant  Anxiety
 SSRI
 Drowsiness
 Insomnia
 Nervousness
 Inhibits neuronal reuptake of serotonin  Sexual dysfunction
 Sweating
 Depression  Tremor
 OCD
 Bulimia nervosa  ↑ levels metabolized by CYP2D6
 Anorexia nervosa
 Fibromyalgia
 Panic attacks
 Phobias
 Prementsrual dysmorphic disorder

 Active metabolite 5-7d half-life

 AVOID MAOI
HALOPERIDOL
 Typical antipsychotic
 Butyrophenone
 Blocks D2 receptors in
mesolimbic area,
chemoreceptor trigger zone,
solitary tract, & basal ganglia
 Blocks muscarinic & α-
adrenergic receptors
 Psychotic disorders
 Schizophrenia
 Tourette’s syn
 Neuroleptic malignant syn
 Fever
 Respiratory distress
 Tachycardia
 Seizures
 Severe m. stiffness
 Altered BP
 Extrapyramidal rxns
 Tardive dyskinesia
 Blurred vision
 Constipation
 Dry mouth
 Urinary retention
 Hypotension
LITHIUM
 Mood stabilizer, antimanic  Polyuria
 Impaired memory
 Inorganic cation  Acne
 Tremor
 ↓ noradrenergic neurotransmission  ECG changes
or effects b/c of ↓ cAMP  GI distress
 Hypothyroidism
 Inhibition of inositol-1-phosphatase  Leukocytosis
 Depletion of inositol & IP3
 Improved Na transport via Na  NM toxicity w/ haloperidol
pump  ↑ toxicity
 Diuretics
 NSAIDS
 Bipolar affective disorder  Fluoxetine

 Monitor serum levels

 Toxicity > 2.5
METHYPHENIDATE
 CNS stimulant  Tachycardia
 Sympathomimetic amine  HTN
 Anorexia
 ↑ neuronal release NE  Irritability
 Insomnia
 ADHD  Tremor
 ↑ attention span  Growthinhibition
 ↓ motor restlessness
 Dependence
 Narcolepsy
 ↑ mental alertness
 ↓ drowsiness & fatigue  HTN crisis w/ MAOI
MIRTAZAPINE
 Antidepressant  ↑ appetite & wt gain
 Constipation
 Tetracyclic
 Dry mouth
 Drowsiness
 Inhibits presynaptic α2
autoreceptors &
heteroreceptors
 ↑ NE & 5-HT release

 Depression
 Appetite stimulation

 AVOID MAOI
 HTN, seizure, death
OLANZAPINE
 Atypical antipsychotic  Agitation
 Thienobenzodiazepine  Dizziness
 Restlessness
 Sedation
 Blocks D2 & 5-HT2 receptors in  Amblyopia
CNS  Orthostatic hypotension
 Blocks H1, muscarinic, & α-  Tachycardia
adrenergic receptors  Constipation
 Dry mouth
 Schizophrenia  Wt gain
 Manic episodes of biploar  Tremor
 Anorexia nervosa

 Oral tablets contain aspartame

 Avoid in phenylketonuria
PHENELZINE
 Antidepressant  Dizziness
 MAOI  Insomnia
 Restlessness
 Blurred vision
 Inhibits MAO & ↑ CNS levels of NE  Orthostatic hypotension
& 5-HT  Diarrhea
 Neurotic & atypical depression  Potentially fatal
 SSRI
 Avoid  Tricyclics
 Fluoxetine
 Tyramine  HTN crisis
 Tyramine
 Amphetamines
 Methyldopa
 Levodopa
RISPERIDONE
 Atypical antipsychotic  Aggressive behavior
 Benzisoxazole
 Extrapyramidal rxns
 Sleep disturbances
 Insomnia
 Blocks 5-HT2 > D2 receptors  Sedation
in CNS  Constipation or diarrhea
 Blocks H1 & α-adrenergic  Wt gain
receptors

 Schizophrenia
 Psychotic disorders

 Monitor pt for neuroleptic

malignant syn
THIORIDAZINE
 Typical antipsychotic  Extrapyramidal rxns
 Phenothiazine  Tardive dyskinesia
 Photosensitivity
 Potential for V arrhythmias
 Blocks D2 receptors in & sudden death
mesolimbic area,  Retinal pigmentation w/
chemoreceptor trigger high doses
zone, solitary tract, &  melanosis
basal ganglia
 Blocks muscarinic
receptors

 Psychoticdisorders
 Schizophrenia
VENLAFAXINE
 Antidepressant  Sexual dysfunction
 Phenethylamine  GI distress
 Dizziness
 Insomnia
 Inhibits neuronal reuptake  Nervousness
5-HT & NE

 Depression
 Generalized anxiety disorder

 AVOID MAOI
RESPIRATORY
 Albuterol  Montelukast
 Cromolyn  Omalizumab

 Diphenhydramine  Salmeterol

 Fluticasone  Theophylline

 Ipratropium  Zileuton

 Loratadine
ALBUTEROL
 Bonchodilator  Muscle tremor
 β2 receptor agonist  Nervousness
 Restlessness
 Tachycardia
 Activates β2 receptors in
bronchial smooth m.
 ↑ cAMP  activating kinases  HTN crisis w/ MAOI
 Inhibiting myosin phosphorylase
 m. relaxation

 Asthma
 Acute bronchospasm
 Prevent exercise-induced asthma
 Chronic bronchitis & emphysema
 Reversible airway obstruction
CROMOLYN
 Antiasthmatic & antiallergy  Nasal & throat irritation
 Mast cell stabilizer

 Prevents Ca influx &

stabilizes mast cell &
eosinophil membranes
 Prevents degranulation &
release of histamine,
leukotrienes
 Asthma prophylaxis
 Exercise-induced
bronchospasm
 Allergic disorders

 Oral or nasal inhalation

DIPHENHYDRAMINE
 Antihistamine, sedative,  Drowsiness
antiemetic  Blurred vision
 H1 receptor antagonist  Dry mouth
 Urinary retention
 Anorexia
 Blocks H1 & muscarinic
receptors
 Prevents histamine-
induced allergic rxns
 Prevents vestibular stim. of
vomiting center
 Sedation

 Allergic rxns
 Prevent motion sickness
 Insomnia
FLUTICASONE
 Anti-inflammatory  Nasal & throat irritation
 Corticosteroid  Oral candidiasis

 Inhibits cytokine production

by Thelper cells
 Prevents mediator release
from mast cells, basophils,
eosinophils
 Stabilizes lysosomal
membranes
 Vasoconstriction & ↓
capillary permeability
 Allergic rhinitis
 Chronic nasal inflammation
 Chronic asthma
IPRATROPIUM
 Bronchodilator  Cough
 Muscarinic receptor  Nasal dryness & irritation
antagonist

 Blocks muscarinic receptors in

bronchial smooth m. & nasal
mucosa
 Prevents vagal-stimulated
bronchoconstriction

 COPD
 Rhinitis
 Asthma

 Inhalation admin
LORATADINE
 Antihistamine
 H1 receptor antagonist

 Blocks H1 receptors in
nasal mucosa
 Prevents allergic rxns
 Seasonal rhinitis
 Chronic idiopathic
urticaria
 Lesssedating than
diphenhydramine
MONTELUKAST
 Antiasthmatic
 Leukotriene antagonist

 Blocks cysteinyl leukotriene-1

receptor for leukotrienes
C4, D4, E4
 Prevent airway inflammation,
edema, bronchoconstriction, &
secretion viscous mucus
 Inhibits early/late phase
bronchoconstriction

 Long-term asthma control

 Oral admin
OMALIZUMAB
 Antiasthmatic  Allergic rxns
 IgE antagonist  anaphylaxis

 Blocks IgE

 Severe asthma in
combo w/
corticosteroid therapy

 SubQ every 2-4 wks

SALMETEROL
 Bronchodilator  Tachycardia
 β2 agonist  Nervousness
 HA
 ↑ cAMP
 Relaxes bronchial smooth m.
 Inhibits late phase allergen-
induced bronchoconstriction
 Asthma
 Prevent nocturnal attacks
 Exercise-induced asthma
 NOT acute bronchospasm
 Inhalation admin
THEOPHYLLINE
 Bronchodilator  N, V
 Methylxanthine  Anxiety
 Insomnia
 Tachycardia
 Inhibits phosphodiesterase
isoenzymes & ↑ cAMP
 Relaxes bronchial smooth m.
 Inhibits T-lymphocyte proliferation
& cytokine production

 Chronic asthma
 Obstructive pulmonary ds
 Neonatal apnea – respiratory stim.

 Half-life
 Shorter in smokers & children
 Longer in elderly
 Monitor blood levels
ZILEUTON
 Antiasthmatic  Flu-like syn
 HA
 Leukotriene synthesis
 Drowsiness
inhibitor
 Dyspepsia
↑ serum aminotransferase
 Inhibits 5-lipoxygenase & levels & hepatitis
leukotriene synthesis
 Prevents airway  Inhibits CYP450 & 3A4
inflammation &  ↑ theophylline &
bronchoconstriction warfarin levels

 Long-term asthma control