Pharmacology

Analgesic & Antimigraine


Butorphanol

Dihydroergotamine

Fentanyl

Meperidine

Methadone

Morphine

Naloxone

Propoxyphene

Sumatriptan

Tramadol

Butorphanol

Opioid analgesic

Mixed opioid agonist-antagonist

Partial agonist or antagonist @
opioid receptors

Agonist @ receptors @ spinal
& supraspinal sites

Inhibits spinothalamic pain
neurotransmission
 Moderate-severe pain
 Admin intranasally
 respiratory depression,
constipation, dependence than full
receptor agonists

 Dysphoria
 Nightmares
 w/drawal in pts dependent on full
opioid agonists
 AVOID MAOI

Potentially fatal

Dihydroergotamine

Antimigraine

Ergot alkaloid

5-HT 1B/1D receptor agonist

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






N, V
Stiff neck, shoulder, extremities
Leg weakness
Numbness & tingling in fingers
& toes

Fentanyl

Opioid analgesic

Phenylpiperidine

Activates opioid receptors
 Inhibits pain transmission
@ spinal & supraspinal
sites

 Sedation
 Confusion
 Respiratory depression
 Anorexia
 N, V
 Constipation
 AVOID MAOI in past 14d

 Chronic pain
 Breakthrough for cancer
pain
 Transdermal patch

Meperidine

Opioid analgesic

Strong opioid agonist

Activates opioid receptors
 Inhibits pain transmission
 Generalized CNS
depression
 Moderate-severe pain
 Analgesia during labor
 Preoperative sedation
 Lacks antitussive activity








Confusion
Sedation
Constipation
N, V
Dependence
Toxic metabolite  CNS
excitation, convulsions,
tremors

 AVOID MAOI

Potentially fatal

Methadone

Opioid analgesic

Strong opioid agonist

Activates opioid receptors
 Inhibits pain transmission
 Suppresses opioid w/drawl
Sx w/ euphoria or
dependence
 Moderate-severe pain
 Prevention of opioid abuse
 Orally, once per day






Respiratory depression
Constipation
Confusion
Sedation

 AVOID MAOI

Morphine

Opioid analgesic

Strong opioid receptor
agonist

Activates receptors
 cAMP

Opens K & closes Ca
channels

release substance P

Inhibits pain @ spinal &

supraspinal sites
 Severe pain w/ MI
 Pulmonary edema
 Active metabolite

Morphine glucuronate







Sedation
Confusion
Hypotension
Constipation
Respiratory depression

 AVOID MAOI w/ 14 d

Potentially fata

Naloxone

Opioid antagonist

Opioid receptor antagonist

Blocks opioid , ,
receptors

Rapidly reverses effects of
opioid agonists

 Opioid OD, dependence

 Short half-life needs
repeated doses

Propoxyphene

Opioid analgesic

Weak opioid agonist

Activates opioid
receptors
 Inhibits pain transmission
 Mid-moderate pain
 Combined w/
acetaminophen or aspirin

 Dizziness
 Weakness
N
 dependence

Sumatriptan

Antimigraine

5-HT 1B/1D receptor agonist

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

 Oral, nasal, & subQ








Dizziness
Vertigo
Tingling
Warm sensation
Tight feeling head & chest
Coronary vasospasm

 AVOID

MAOI

SSRI

Tramadol

Analgesic

Dual action

Activates opioid receptors
 Inhibits neuronal reuptake
5-HT & NE
 inhibition of pain
 Moderate pain
 Chronic pain
 Naloxone reverses some
but NOT all Sx

 Dizziness
 HA
 Constipation
 Lowers seizure threshold
 AVOID MAOI
 risk seizures w/ high
doses

Penicillins

Phenothiazines

Anesthetics


Benzocaine

Bupivacaine

Halothane

Ketamine

Lidocaine

Midazolam

Nitrous oxide

Propofol

Sevoflurane

Benzocaine

Local anesthetic

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

 Cross-sensitivity w/ other estertype anesthetics

Bupivacaine

Local anesthetic

Amide-type

Blocks Na channels &
nerve conduction
 Local or regional
anesthetic

Surgical

Diagnostic

Obstetrical

therapeutic

Cross-sensitivity w/
amide-type anesthetics

Halothane

General anesthetic

Inhalational, halogenated
hydrocarbon

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

 Sensitizes heart to
catecholamine-induced
cardiac arrhythmia
 Hepatotoxic

Fluoride metabolites

Ketamine

IV anesthetic

Glutamate antagonist

Blocks glutamate NMDA
receptors
 Dissociate anesthesia

Analgesia

Immobility

Amnesia

Does NOT depression
respiration or cause LOC
 Anesthesia

Minor surgical & diagnostic
procedures

Children

 Delirium
 Hallucination
 Irrational behavior during
recovery
 BP

Lidocaine

Local anesthetic

Amide-type

Blocks Na channels & nerve
conduction







Topical
Infiltration
Nerve block
Epidural
Spinal anesthesia
Eutectic mixture

Lidocaine & prilocaine

Anesthetize intact skin for
venipuncture

IV cannulation

Circumcism

 Cross-reactivity w/ amide-type
anesthetics

Midazolam

Sedative-hypnotic-anxiolytic

Short-acting BZDP

Potentiates GABA binding to
GABA-A Cl ion channel
 Sedation
 Hypnosis
 Amnesia
 Preoperative sedation &
anxiolysis
 Sedation of mechanically
vented pts

 Apnea
 Laryngospasm
 Respiratory depression
 Cardiac arrest

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

IV anesthetic

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

 Bradycardia
 Hypotension

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
Albendazole
Amantadine
Amoxicillin-clavulanate
Amphotericin B
Azithromycin
Aztreonam
Caspofungin
Cefazolin

Cefepime
Cetriaxone
Ciprofloxacin
Clindamycin
Doxycycline
Efavirenz
Enfuvirtide
Erythromycin
Ethambutol



Foscarnet
Fosfomycin
Ganciclovir
Gentamicin
Griseofulvin
Imipenem-cilastatin
Isoniazid
Itraconazole
Ivermectin
Levofloxacin

Linezolid
Mefloquine
Metronidazole
Mupirocin
Nafcillin
Nitrofurantoin
Oseltamivir
Paromomycin
Penicillin G



Pentamidine
Piperacillin-tazobactam
Praziquantel
Primaquine
Pyrimethamine
Pyrantel
Quinine
Quinpristein-dalfopristin
Ribavirin

Rifampin
Ritonavir-lopinavir
Streptomycin
Terbinafine
Trifluridine
TMP-SMX
Vancomycin
Zidovudine

Acyclovir

Antiviral

Nucleoside analogue

Converted to acyclovir
triphosphate by viral & host cell
kinases

Incorporated into DNA by viral
DNA polymerase causing DNA
chain termination
 HSV2
 Herpes zoster

Shingles

Chickenpox varicella

 viral shedding, pain, & healing

time






Dizziness
Diarrhea
N
Nephrotoxicity

 Probenecid serum levels

Albendazole

Antihelmintic

Benzimidazole

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

 GI distress
 Constipation or diarrhea
 Hepatitis & hematologic toxicity w/ high
doses

Amantadine

Anti-influenza,
antiparkinson

Tricyclic amine

Inhibits influenza-A M2
proton channel &
acidification of virus
particle
 Prevents viral proteinprotein dissociation &
uncoating of viral
particles
 Influenza A

 Ataxia
 Dizziness
 Insomnia
 Skin mottling & livedo
reticularis
 Blurred vision
 Dry mouth

Amoxicillin-clavulanate

-lactam ABX

Extended spectrum aminopenicillin
& -lactamase inhibitor

Amoxicillin
 Binds PBP

Inhibits cross-linking of cell wall
peptidoglycan

Clavulanate
 Inhibits class-A -lactamase

Protects amoxicillin from
destruction

 NOT antimicrobial by itself

 Respiratory tract infections

Otitis, sinusitis, pneumonia

 Skin or skin structure infections

Bite wounds






Diarrhea
Superinfection
Pseudomembranous colitis
Allergic rxn

Rash

Serum sickness

anaphylaxis

 Probenecid inhibits renal tubular

excretion

serum levels

Amphotericin B

Antifungal

Polyene ABX

Binds ergosterol &
membrane permeability
 Leakage of cell contents








Candidiasis
Cryptococcal meningitis
Aspergillosis
Blastomycosis
Coccidioidomycosis
Histoplasmosis
Mucormycosis








Chills
Fever
Diarrhea
N, V
Nephrotoxicity
Hypokalemia

 toxicity w/ cyclosporine,
antineoplastics
 Thiazides, & corticosteroids
hypokalemia

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

-lactam ABX

Monobactam

Binds PBP including
transpeptidase

Inhibits cross-linking of
cell wall peptidoglycan
 Drug resistant gram (-)
infections including
Pseudomonas aeruginosa
& Enterobacteriaceae

 Thrombophlebitis
 Allergic rxn

Caspofungin

Antifungal

Echinocandin

Inhibits synthesis of
cell wall component
 -1,3-D-glucan
 Candida albicans
 Invasive aspergillosis
 IV admin

Not absorbed well by gut

 HA
 Fever
 Phlebitis
 Abnormal LFTs

Cefazolin

-lactam ABX

2nd generation cephalosporin

Binds PBP including
transpeptidase

Inhibits cross-linking of cell
wall peptidoglycan
 Surgical wound infections
 Infections d/t

Staph, strep, E. coli, Klebsiella
pneumoniae, Proteus mirabilis

 NOT active against MRSA






Rash
Diarrhea
Pseudomembranous colitis
Superinfection

 Probenecid inhibits excretion &

serum levels

Cefepime
Rash
Diarrhea
Pseudomembranous colitis
Superinfection

-lactam ABX

4th generation
cephalosporin






Binds multiple PBP

Inhibits cross-linking of
cell wall peptidoglycan

Resistant to many lactamases

 Probenecid inhibits excretion

& serum levels

 Drug-resistant gram (-)

bacteria

Citrobacter

Enterobacter

Ceftazidime

-lactam ABX

3rd generation cephalosporin

Binds PBP including
transpeptidase

Inhibits cross-linking of cell
wall peptidoglycan
 Gram (+), gram (-), & anaerobics
Pseudomonas aeruginosa
 Pneumonia, meningitis, UTI, skin
structures, bones, jts






Rash
Diarrhea
Pseudomembranous colitis
Superinfection

 Probenecid inhibits excretion &

serum levels

Cetriaxone

-lactam ABX

3rd generation cephalosporin

Binds PBP including
transpeptidase

Inhibits cross-linking of cell
wall peptidoglycan
 Infection d/t

Pneumococci, gonococci,
meningococci, H. influenzae,
Moraxella catarrhalis, Borrelia
burgdorferi

 Single IM injection Tx acute

otitis media or gonorrhea






Rash
Diarrhea
Pseudomembranous colitis
Superinfection

 Probenecid inhibits excretion &

serum levels

Ciprofloxacin

Antibacterial

Fluoroquinolone

Inhibits bacterial DNA
topoisomerase type II (DNA gyrase)
& type IV

Prevents DNA replication &
separation of chromosomes
 Urinary tract, prostate, intraabdominal
w/ metronidazole, bone or jt, skin
 Inhalational anthrax
 Gonorrhea
 Infectious diarrhea
 Gram (+), gram (-), Pseudomonas
aeruginosa

 Insomnia
 Diarrhea
 N
 Absorption by cations

Antacids
Iron
Zinc
bismuth

Clindamycin

Aminosugar ABX

Protein synthesis
inhibitor

Binds 50s ribosome

Prevents translocation of
nascent peptide from
acceptor site to peptidyl
site
 Strep, staph, gram (+)
 Acne vulgaris
 Anaerobes including
Bacteroides

 C. difficile superinfection
 Diarrhea
 Pseudomembranous colitis

Doxycycline

Tetracycline ABX

Protein synthesis inhibitor

Binds 30s ribosome

Reversibly inhibits binding of
transfer RNA to acceptor site
 Rickettsia, Chlamydia,
Mycoplasma, Borrelia
 Acne
 Cholera
 Gonorrhea & syphilis in PCN
allergic pts
 Brucellosis & ehrlichiosis

 AVOID

Pregnancy & children > 8 y/o

Outdated preparations are
nephrotoxic






Permanent teeth discoloration

Photosensitivity
Diarrhea
N, V

Efavirenz

Antiretroviral

Non-nucleoside reverse
transcriptase inhibitor

Binds reverse
transcriptase & disrupts
catalytic site
 HIV in combo w/ nucleoside
reverse transcriptase inhibitor
synergistic
 High fat meal absorption






N
Rash
Drowsiness
Depression

Enfuvirtide

Antiretroviral

HIV fusion inhibitor

Binds HIV virus gp41 &
blocks fusion of HIV w/
host cells CD4 Thelper
lymphocytes
 Drug-resistant HIV

 Injection site rxn

Rotate sites daily

Erythromycin

Macrolide ABX

Protein synthesis inhibitor

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

 Activates motilin receptors

causing uncoordinated
peristalsis

Anorexia

N, V

Ethambutol

Antitubercular

Synthetic butanol
derivative

Bacteriostatic against
mycobacteria

Inhibits RNA synthesis
 M. tuberculosis
 MAI

 Dose-related
retrobulbar optic
neuritis
 Impaired red-green
color discrimination

Monitor pts color
discrimination
regularly

 Gouty arthritis

Foscarnet

Antiviral

Pyrophosphate

Blocks pyrophosphatebinding site on viral
DNA polymerase
 Prevents attachment of
nucleotide precursors to
DNA
 CMV retinitis in HIV pts
 Acyclovir-resistant HSV in
immunocompromised












HA
Diarrhea
V
Renal failure
Hypocalcemia
Hypokalemia
Hypomagnesemia
Anemia
Arthralgia
Myalgia

 Pentamidine causes lifethreatening hypocalcemia

Fosfomycin

ABX

Cell wall synthesis
inhibitor

Inhibits enopyruvyl
transferase & addition of
phosphenolpyruvate to Nacetylglucosamine to
form N-acetylmuramic
acid
 Cystitis d/t E. coli or
Enterococcus faecalis
 Single dose Tx for UTI

Ganciclovir

Antiviral

Nucleoside
analogue

Converted to
ganciclovir
triphosphate
 Inhibits viral DNA
polymerase
 CMV infection in
immunocompromise
d & transplants

 visual acuity
 Neutropenia
 Thrombocytopenia
 Anemia

Gentamicin

Aminoglycoside ABX

Protein synthesis inhibitor

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

 Nephrotoxicity
 Ototoxicity

Vestibular & cochlear

w/ loop diuretics

Griseofulvin

Antifungal

Fungistatic ABX

Deposits in keratin
precursor cells of skin,
hair, & nails

Disrupts microtubules
& mitotis of
dermatophytes
 Dermatophyte infections
 NOT Candida

 HA
 Induces CYP450

Reduces plasma levels
warfarin & OCP

Imipenem-cilastatin

-lactam ABX

Carbapenem ABX &
dehydropeptidase inhibitor

Imipenem
 Binds PBP & inhibits crosslinking cell wall peptidoglycan

Cilastatin
 Inhibits renal dehydropeptidase
& degradation of imipenem
 Endocarditis, pneumonia, UTI,
pelvic, abdominal d/t aerobic &
anaerobic






Allergic rxns
Diarrhea
V
Seizures

risk w/ ganciclovir or
cyclosporine

 Probenecid inhibits secretion &

serum levels

Isoniazid

Antitubercular

Nicotinic acid derivative

 Hepatitis

Toxic metabolite acetylhydrazine

 Peripheral neuropathy

Reduces catalaseperoxidase
 Inhibits synthesis of
mycolic acid component of
cell wall
 TB
 Bimodal distribution d/t fast
& slow acetylation
 Inactivates vit. B6

Vit. B6 deficiency

Itraconazole

Antifunal

Synthetic triazole

Inhibits 14--demethylase
 CYP450 enzyme that
converts lanosterol 
ergosterol
 Blastomycosis, candidiasis,
coccidioidomycosis,
histoplasmosis
 Onychomycosis nail beds

 GI distress
 Rash
 Hepatitis

Ivermectin

Antiparasitic

Antihelmintic ABX

Activates glutamate-gated
Cl ion channel
 Pharyngeal m.
hyperpolarization &
paralysis
 Strongyloidiasis
 Cutaneous larva migrans
 Onchocerciasis filiariasis

W. bancrofti

 Vertigo
 Sedation

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

Oxazolidinone protein
synthesis inhibitor

Binds 23s ribosomal
RNA of 50S subunit
 Prevents formation of
70s initiation complex
 VRE, MS/MRSA, PCNsensitive pneumococci

 Inhibits MAO

Mefloquine

Antimalarial

4-quinolone methanol
derivative

Inhibits erythrocytic
schizogony

Inhibit nucleic acid synthesis
 Malaria
 Chloroquinesusceptible/resistant trains of
P. falciparum & P. vivax
 Perform CBC during chronic
prophylactic Tx

 Neuropsychiatric syn

Hallucination
Anxiety
Confusion
Seizure
Coma

Metronidazole

Antiprotozoal

Nitroimidazole

Reduced by
pyruvate:ferredoxin to
form nitro-free radicals
that attack DNA &
proteins
 Amebiasis, giardiasis,
trichomoniasis
 Balantidium coli, C.
difficile, B. fragilis

 GI pain
 Anorexia
N
 Dizziness
 Alcohol causes
disulfiram-like effect

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

-lactam ABX

Antistaphylococcal,
penicillinase-resistant
penicillin

Binds PBP
 Inhibits cross-linking of cell
wall peptidoglycan
 Methicillin-sensitive
penicillinase producing
staph

Bone, jt, UTI, respiratory,
skin, endocarditis,
meningitis






Diarrhea
Superinfection
Pseudomembranous colitis
Allergic rxn

Rash

Serum sickness

Anaphylaxis

 Probenecid inhibits renal

tubular secretion & serum
levels

Nitrofurantoin

Urinary tract
antibacterial

Nitrofuran

Anorexia
N, V
Neurotoxicity
Pneumonitis

Inhibits bacterial
enzymes

Probenecid inhibits
urinary excretion

UTI

E. coli, S.
saprophyticus

Oseltamivir

Antiviral

Neuraminidase inhibitor

Inhibits influenza A & B
neuraminidase
 Prevents release &
spreading of viral
particles
 Influenza A & B

Paromomycin

Antiprotozoal

Aminoglycoside ABX

Inhibits protein
synthesis
 Intestinal amebiasis
 Cryptosporidiosis in
immunocompromised pts

 Nephrotoxic & ototoxic

if given IV

Penicillin G

-lactam ABX

Narrow-spectrum
penicillin

Binds PBP
 Inhibits cross-linking of
cell wall peptidoglycan
 Strep, pneumococcal,
meningococcal
 Syphilis

 Diarrhea
 Superinfection
 Pseudomembranous
colitis
 Allergic rxn

Rash

Serum sickness

Anaphylaxis

 Probenecid inhibits
renal tubular secretion

Pentamidine

Antiprotozoal

Amidino-pentane
derivative

Disrupts nucleic acid
synthesis in protozoa
 P. carinii
 Early stage African
trypanosimiasis
sleeping sickness

 Nephrotoxic
 Hematologic toxicity
 Hypoglycemia
 Allergic rxn

Anaphylaxis

 Erythromycin fatal
arrhythmias

Piperacillin-tazobactam

-lactam ABX

Antipseudomonal penicillin & lactamase inhibitor

Piperacillin
 Binds PBP

Inhibits cross-linking of cell
wall peptidoglycan

Tazobactam
 Inhibits class A -lactamases
 Gram (-) bacilli, P. aeruginosa






Diarrhea
Superinfection
Pseudomembranous colitis
Allergic rxn

Rash

Serum sickness

Anaphylaxis

 Probenecid inhibits renal tubular

secretion

Praziquantel

Antihelmintic

Isoquinoline derivative

Ca permeability of
schistosome tegument
 Contraction & exposing
antigens to host
immunity
 Schistosomiasis
 Chinese liver fluke
 Lung fluke
 Cestodes tapeworms

 Malaise
 Anorexia
 Drowsiness
 dizziness

Primaquine

Antimalarial

8-aminoquinoline

Converted to oxidizing
quinoline-quinone
intermediates
 Eradicate exo-erythrocytic
forms of P. vivax & P.
ovale

 Hemolytic anemia in
G6PD deficiency
 methemoglobinemia

Pyrimethamine

Antiprotozoal

Folate reductase inhibitor

Inhibits folate reductase

Folate deficiency in protozoa
 Malaria in combo w/ sulfadoxine
 Toxoplasmosis in combo w/
sulfadoxine
 NOT effective against P. vivax

 N
 Anorexia
 Hypersensitivity rxn

Pyrantel

Antihelmintic

Pyrimidine analogue

Activates cholinergic
nicotinic receptors in
somatic m. of
nematodes

Produces depolarizing
NM blockade
 Ascariasis
 Hookworm & pinworm

 Abdominal cramps
 Anorexia
 Diarrhea
V

Quinine

Antimalarial

4-aminoquinoline

 Abdominal cramps
 Diarrhea
V

Binds plasmodial DNA &

prevents replication &
transcription during
erythrocytic schizogony

 Cinchonism

Tinnitus

Blurred vision

 Metabolism
 Chloroquine-resistant malaria
 Admin w/ doxycycline or
pyrimethamine-sulfadoxine

Cimetidine inhibits

Rifampin induce

Quinupristin-dalfopristin

Streptogramin ABX

Protein synthesis
inhibitor

Binds 50s ribosomal
subunit

Quinupristin
 Inhibits aminoacyl tRNA
synthesis & addition of AA

Dalfopristin
 Inhibits peptidyl transferase
 VRE, MS/MRSA

 Infusion site rxn

Ribavirin

Broad-spectrum antiviral

Guanosine analogue

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

 Anemia
 Hypotension
 Cardiac arrest

Rifampin

Antitubercular

Rifampin derivative

Inhibits DNA-dependent RNA
polymerase
 TB
 Leprosy
 Prophylaxis meningococcal
meningitis & H. flu B infections

 Red discoloration of tears,

urine, saliva, sweat
 Abdominal pain
 V
 Diarrhea
 Hepatitis
 Induces CYP450
 levels

Warfarin
Theophylline
Itraconazole
Steroids
Opioids
Phenytoin
Verapamil

Ritonavir-lopinavir

Antiretroviral

HIV protease inhibitor

Inhibits HIV protease &
conversion of gag-pol
polyprotein to
functional proteins

Ritonavir
 lopinavir levels
 HIV in combo w/
nucleoside reverse
transcriptase inhibitor

 Anorexia
V
 Altered taste
 Abnormal thinking
 Hyperlipidemia
 Hyperlgycemia

Streptomycin

Aminoglycoside

Protein synthesis
inhibitor

Binds 30s ribosome

Prevents initiation of
protein synthesis
 Misreading of genetic code
 Drug-resistant TB
 Plague
 Tularemia
 IV admin

 Nephrotoxic
 Ototoxic

w/ loop diuretics

Terbinafine

Antifungal

Allylamine

Inhibits squalene
oxygenase & formation of
squalene epoxide during
fungal membrane
ergosterol synthesis
 Topical

Tinea corporis, cruris,
pedis, versicolor

 Oral

Onychomycosis fungal
nail infection






Itching
Rash
Diarrhea
Anorexia

 Metabolism

Cimetidine inhibits

Rifampin induce

Trifluridine

Antiviral

Thymidine analogue

Inhibits HSV DNA
polymerase
 Herpetic keratitis
 Keratoconjunctivitis
 Topical ocular admin

 Ocular irritation

Redness

Itching

Trimethoprim-sulfamethoxazole

Antibacterial

Folate antagonist

Sulfamethoxazole
 Inhibits folate synthesis

Trimethoprim
 Inhibits folate reduction
 UTI, travelers diarrhea
 Shigella enteritis
 P. carinii & Nocardia
pneumonia







N, V
Rash
Stevens-Johnson syn
Allergic rxn
Anemia

Hemolytic anemia

Megalobalstic anemia

 Leukopenia
 Thrombocytopenia
 Crystalluria
 Added folate deficiency w/
phenytoin or MTX

Vancomycin

Glycopeptide ABX

Cell wall synthesis
inhibitor

 Red man syn

Extensive rate of infusion

Erythematous rash on
face & upper body

 Ototoxicity

Binds D-alanyl-D-alanine
portion of peptidoglycan

Prevents cross-linking of
D-alanine & pentaglycine
chain
 MRSA, penicillin-resistant
enterococci, C. difficile

Vestibular & cochlear

Zidovudine

Antiretroviral

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

 Anemia

Antineoplastic



Anastrozole
Bleomycin
Busulfan
Carmustine
Cisplatin
Cyclophosphamide
Doxorubicin
Etoposide
Fluorouracil
Gemtuzumab
ozogamicin

Imatinib

Leuprolide

Meraptopurine

Methotrexate

Paclitaxel

Tamoxifen

Trastuzumab

Vincristine

Anastrozole

Estrogen antagonist

Nonsteroidal aromatase
inhibitor

Inhibits aromatase &
conversion to estrone
precursor to estradiol

Lowers estrogen levels

Halts progression of
estrogen-sensitive breast
cancers
 Breast cancer in
postmenopausal women

N
 HA
 Hot flashes
 Back pain

Bleomycin

Antitumor

DNA intercalating

Complexes ironforming oxygen free
radicals that cause
single strand breaks

G2 phase specific
Lymphomas
SCC
Testicular carcinoma
Choriocarcinoma

 Pneumonitis &
pulmonary fibrosis
 Hyperpigmentation
 Mucocutaneous toxicity
 Hematology toxicity

Busulfan

Antineoplastic

Alkyl sulfonate bifunctional
alkylating agent

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

 N, V
 Myelosuppression
 Pulmonary fibrosis

Carmustine

Antineoplastic

Nitrosurea bifunctional
akylating agent

Cross-links DNA strands by
covalently bonding guanine
residues

Prevents DNA replication &
transcription
 Brain tumors
 Myeloma
 Lymphoma
 Causes prolonged
myelosuppression

 N, V
 Hepatotoxicity
 Anemia
 Leucopenia
 Thrombocytopenia
 Pulmonary fibrosis

Cisplatin

Antineoplastic

Platinum compound

Forms reactive metabolites
that covalently bond DNA
bases & cross-link DNA
strands
 Testicular, ovarian, cervical,
bladder, lung, head/neck
cancers
 Less bone marrow
suppression

 Severe N, V
 Ototoxicity & tinnitus
 Hypocalcemia
 Hypokalemia
 Hypomagnesemia
 Anemia

Cyclophosphamide

Antineoplastic

Nitrogen mustard bifunctional
akylating agent

Cross-links DNA strands by
covalently bonding guanine
residues

Prevents DNA replication &
transcription






Hodgkins ds
Lymphomas, myeloma
Leukemia
Ovarian & breast tumors
RA

 Converted to active metabolites

by CYP enzymes









Anorexia
N, V
Hemorrhagic cystitis & hematuria
Alopecia
Thrombocytopenia
Leukopenia
Anemia

 Rifampin induces CYP & toxicity

Doxorubicin

Antitumor

DNA intercalating agent

Inserts b/w DNA bases
 Causes deformation & uncoupling

Complexes iron forming

hydroxyl free radicals that
cause strand breaks

Inhibits topoisomerase II
 Causes strand breaks

S phase specific
 Breast, ovarian, bladder tumors
 Bronchogenic carcinoma
 Lymphoma & leukemia

 Colors urine red

 Cardiomyopathy doselimiting
 Anemia
 Leukopenia
 Thrombocytopenia
 Diarrhea
V
 Stomatitis
 Alopecia

Etoposide

Antineoplastic

Podophyllotoxin,
topoisomerase inhibitor

Inhibits mammalian
topoisomerase II & prevents
resealing of nicked DNA
strands

G2 phase specific
 Testicular, small cell lung
carcinoma
 Lymphoma
 Leukemia

 N, V
 Leukopenia
 Thrombocytopenia
 Alopecia

Fluorouracil

Antineoplastic

Pyrimidine antimetabolite

Converted to active
nucleotide form
 Inhibits thymidylate
synthetase

S phase specific
 Colon, breast, rectal, gastric,
pancreatic cancer
 Topical for basal cell
carcinoma & actinic
keratosis

 Diarrhea
V
 Stomatitis
 Alopecia
 Maculopapular rash
 Anemia
 Leukopenia
 Thrombocytopenia

Gemtuzumab ozogamicin

Antineoplastic

Monoclonal Ab & cytotoxic
ABX calicheamicin

Gemtuzumab
 Binds CD33 Ag on
hematopoietic cells &
sequesters lysosomes where
calicheamicin is released

Calicheamicin
 Causes DNA dbl strand breaks
 CD33 (+) AML

 Severe myelosuppression &

hypersensitivity rxn

anaphylaxis

 Severe pulmonary rxns

 Chills
 Fever
N
 Dyspnea

Imatinib

Antineoplastic

Tyrosine kinase inhibitor

Inhibits oncoprotein bcr-abl
tyrosine kinase expressed
by Philadelphia
chromosome

Inhibits leukemic cell
proliferation & induced
apoptosis
 CML

Cause hematologic &
cytogenetic remission

 Cough
 Dyspnea
 Pharyngitis
 Pneumonia
 Abdominal pain
V
 Petechiae
 Pruritis
 Rash
 Night sweats
 Myalgia
 Arthralgia
 Thrombocytopenia
 Neutropenia

Leuprolide

Antineoplastic, agent for
precocious puberty

GnRH analogue

Pulsatile admin FSH & LH
release

Continuous admin downregulates GnRH receptors &
FSH & LH





Central precocious puberty

Advanced prostate cancer
Endometriosis
Uterine fibroids

 IM depot & implants for prostate

cancer

 Transient in testosterone w/
1st dose

Use flutamide or other
androgen antagonist

 Hot flashes

Mercaptopurine

Antineoplastic

Purine antimetabolite

Converted to nucleotide
triphosphate by phosphoribosyl
transferase

Inhibits purine biosynthesis &
salvage pathways

S phase specific
 Acute leukemia
 CML
 Lymphomas
 Tumors that delete
phosphoribosyl-transferase
acquire resistance

 Cross-react w/ thioguanine
 Myelosuppression
 Hyperuricemia
 Hepatotoxicity
 Allopurinol inhibits degradation

Methotrexate

Antineoplastic

Folate reductase inhibitor

Inhibits dihydrofolate reductase

Prevents formation of active folate
& addition of single carbon units to
DNA 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









N, V
Stomatitis
Hepatotoxicity
Anemia
Leukopenia
Thrombocytopenia
Nephropathy

Paclitaxel

Antineoplastic

Mitotic inhibitor

Binds tubulin & prevents
depolymerization of
microtubules of mitotic
spindle

M phase specific
 Advanced ovarian cancer w/
cisplatin
 Non-small-cell lung cancer
 Metastatic ovarian or breast
cancer

D
 N, V
 Alopecia
 Anemia
 Leukopenia
 Thrombocytopenia
 Peripheral neuropathy
 Arthralgia
 Myalgia

Tamoxifen

Antineoplastic

Estrogen receptor
antagonist & partial agonist

Competes w/ estrogen for
receptors in breast & other
tissues

Suppresses breast tumor
growth
 Breast cancer & ductal
carcinoma following surgery &
radiation
 Advanced breast cancer

 CI during pregnancy &

lactation
N
 Hot flashes
 Menstrual irregularities

Trastuzumab

Antineoplastic

Monoclonal Ab

Binds human epidermal growth
factor-2 (HER2) receptor on
breast cancer cells

Prevents receptor stim. & cell
proliferation

Regression of breast cancer
metastases
 Metastatic breast cancer w/
overexpression HER2
 Combined w/ paclitaxel

blood levels

 Abdominal pain
 Anorexia
 Diarrhea
V
 Back pain
 Chills
 Fever
 Allergic rxns
 Doxorubicin risk of
cardiotoxicity

Vincristine

Antineoplastic

Vinca alkaloid, mitotic inhibitor

Binds tubulin & prevents
polymerization of tubulin dimers
forming microtubules of mitotic
spindle

M phase specific







Hodgkins ds
Lymphoma
Leukemia
Neuroblastoma
Rhabdomyosarcoma
Wilms tumor

 N, V
 Alopecia
 Peripheral neuropathy

Autonomic & Neuromuscular


Atenolol

Atropine

Dobutamine

Edrophonium

Epinephrine

Phenoxybenzamine

Phentolamine

Phenylephrine

Pilocarpine

Pralidoxime

Propranolol

Pseudoephrine

Pyridostigmine

Rocuronium

Sildenafil

Succinylcholine

Tamsulosin

Terazosin

Atenolol

Sympatholytic,
antihypertensive

1 receptor antagonist

Bronchoconstriction w/
high doses b/c 1
blockade

1 receptor antagonist

Additive hypotension w/
nitrates

 Angina
 Post MI
 Hypertension

Atropine

Anticholinergic

Muscarinic receptor
antagonist

Muscarinic receptor
blocker
Bradycardia
IBS
Anticholinesterase
poisoning
Antisecretory agent

 Mydriasis & cycloplegia

 Warm, dry, flushed skin
 Tachycardia
 Delirium
 Hallucinations

Dobutamine

Sympathomimetic, cardiac
stimulant

1 receptor agonist

Selective 1 receptor
agonist
 1 > 2 > 1
 Cardiac contractility &
output
 Acute heart failure
 Cardiogenic shock
 Synergistic on cardiac output
w/ nitroprusside

 Tachycardia
 Arrhythmia

Edrophonium

Diagnostic agent

Cholinesterase
inhibitor

Reversible
cholinesterase
inhibitor
Dx myasthenia gravis

Muscarinic effects

Miosis

Salivation

Epinephrine

Sympathomimetic,
bronchodilator, vasopressor

Nonselective adrenergic
agonist

Activates & receptors
 IP3 & cAMP

1 vasoconstrict & BP

1 HR, conduction, &
contractility

2 vasodilate, BP,
bronchodilate
 Cardiac arrest, V fib
 Shock, asthma
 COPD






HTN
Tachycardia
Ischemia
Hyperglycemia

Phenoxybenzamine

Vasodilator

Irreversible
receptor antagonist

receptor
antagonist
1 > 2
 Presurgical Tx of HTN d/t
pheochromocytoma

Postural hypotension
Hypotension w/
blockers & Ca channel
blockers

Phentolamine

Vasodilator

receptor antagonist

Blocks 1 & 2
receptors
 Control BP during surgical
removal of
pheochromocytoma
 IV admin only

 Hypotension
 Severe hypotension w/
Epi

Phenylephrine

Vasocontrictor, decongestant

Selective 1 receptor

agonist

Activates 1 receptor
 Increase IP3 causing
contraction of vascular
smooth m.
 Nasal & ocular decongestant
 Dilate pupil for opthalmoscopy
 Mydriasis w/o cycloplegia

Paralysis of accommodation

 Rebound nasal congestion

 HTN
 MAOI cause severe HTN

Pilocarpine

Antiglaucoma, sialogogue

Muscarinic receptor
agonist

Activates muscarinic
receptors in ciliary m. &
salivary gland
 Sjogrens syn

Glaucoma
Ciliary m. aqueous
humor

Xerostomia
Salivary gland
salivation

 Miosis
 Blurred vision

Accommodative spasm

Pralidoxime

Organophosphate antidote

Cholinesterase reactivator

Binds phosphorous &
breaks organophosphate
bond w/ cholinesterase
 Organophosphate toxicity
 Reverses muscle weakness

Propranolol

Sympatholytic,
antihypertensive

Nonselective receptor
antagonist

Blocks 1 & 2 receptors







Angina
HTN
Benign tremor
Migraine prophylaxis
thyrotoxicosis
Post-MI

 Highly lipophilic  CNS

effects

 Bronchoconstriction
 Inhibits glycogenolysis
 Nightmares & depression

Pseudoephedrine

Decongestant

Indirect/direct-acting
adrenergic receptor
agonist

 Tachycardia
 CNS stim.
 BP
 MAOI cause severe HTN

release NE directly
activates adrenergic
receptors causing
vasoconstriction &
cardiac stim.
 Allergic & viral rhinitis

Pyridostigmine

Antimyasthenic

Cholinesterase
inhibitor, cholinergic
agonist

Reversibly inhibits
cholinesterase
 Tx myasthenia gravis
 Reverse nondepolarizing
NM blockers

 Muscarinic effects

Miosis

Salivation

 Prolongs effects of
succinylcholine

Rocuronium

Paralytic agent

Nondepolarizing NM blockade

Blocks nicotinic receptors in
skeletal m.
 Skeletal m. relaxation for
intubation, surgery, ECT
 Effects reversed by
neostigmine & edrophonium

 Respiratory m. paralysis
 Apnea

Sildenafil

Vasodilator

Phosphodiesterase
inhibitor

Inhibits type 5
phosphodiesterase &
degradation of cGMP
 vasodilation in corpus
cavernosum d/t Ach
release from sacral PNS
neurons
 Erectile dysfunction

 HA
 Nasal congestion
 Back pain
 Visual disturbances

Succinylcholine

Paralytic agent

Depolarizing NM blockade

Binds nicotinic receptors
causing prolonged
depolarization of skeletal m.
& paralysis
 Skeletal m. relaxation for
intubation & surgery
 Transient m. fasciculations

 Respiratory m. paralysis
 Apnea

Tamsulosin

Urologic agent

Uroselective 1
receptor antagonist

Dizziness
HA
Postural hypotension

Blocks 1A
receptors in
prostate

Cimetidine increases
blood levels & effects

Tx urinary outflow

obstruction d/t prostatic
hyperplasia

Terazosin

Antihypertensive,
urologic agent

Selective 1
receptor antagonist

Blocks 1 receptors
HTN
Outflow obstruction d/t
prostate hyperplasia

1st dose syncope

Cardiovascular



Acetazolamide
Adenosine
Amiloride
Amiodarone
Amlodipine
Carvedilol
Clonidine
Digoxin
Diltiazem
Dofetilide
Enalapril
Esmolol
Fenoldopam
Furosemide
Hydralazine

Hydrochlorothiazide
Labetalol
Mannitol
Methyldopa
Minoxidil
Nesiritide
Nitroglycerin
Nitroprusside
Propafenone
Quinidine
Sotalol
Spironolactone
Valsartan
verapamil

Acetazolamide

Diuretic

Carbonic anhydrase
inhibitor

Inhibits interconversion of
carbonic acid & bicarbonate

NaHCO3 excretion

Inhibit aqueous humor
formation

Hyperchloremic metabolic
acidosis
 Tx open-angle glaucoma
 Mtn sickness
 Metabolic alkalosis

 Parasthesia
 Urinary stone formation

Adenosine

Antiarrhythmic

Purine nucleoside,
cardiac node membrane
stabilizer

Opens K channels &
blocks Ca influx in SA &
AV nodes

Slows AV conduction

AV refractory period
Terminate SVT

 Transient asystole

Amiloride

K-sparring diuretic

Epithelial Na channel
blocker

Blocks Na Channel
distal tubule &
collecting duct
 Inhibits Na reabsorption
& K excretion
 Prevent & Tx hypokalemia

 Hyperkalemia

Amidarone

Antiarrhythmic

Cardiac ion channel
blocker

Blocks K, Na, Ca
channels & receptors
 Prolongs repolarization
 refractory period
 Slows HR
 PR & QT intervals
 SVT, VT, VF

 Hypo/hyperthyroidism
 Photosensitivity
 Blue-gray skin
 Corneal microdeposits
 Pulmonary fibrosis

Amlodipine

Antihypertensive,
antianginal

Dihydropyridine Ca
channel blocker

HA
Edema
Hypotension

Ca channel blocker in
vascular smooth m.
Arteriolar vasodilation
& coronary blood
flow

Effects w/ grapefruit
juice

HTN
Angina pectoris

Carvedilol

Antihypertensive & heart
failure Tx

Nonselective
adrenergic receptor
agonist

Blocks 1, 2, 1
receptors
Cause vasodilation
HTN
Heart failure

remodeling

Orthostatic hypotension
Dizziness
Bradycardia

Clonidine

Antihypertensive

2 receptor agonist

Central 2 receptor agonist
 sympathetic outflow from
vasomotor center
 Inhibits pain
neurotransmission in spinal
cord
 HTN
 Opioid w/drawal

 Abrupt w/drawal 
severe rebound HTN
 Sedation
 Dry mouth

Digoxin

Cardiac stimulant

Digitalis glycoside

Inhibits Na/K ATPase
 IC Ca & cardiac
contractility
 AV conduction
 AV refractory period
 Heart failure
 Serum levels assess
dosage & toxicity

 Arrhythmias
 N, V
 Blurred vision
 Yellow vision

Diltiazem

Vasodilator, antiarrhythmic

Non-dihydropyridine Ca
channel blocker

Block Ca channels in cardiac
tissue & vascular smooth m.
 Vasodilation
 HR & conduction
 contractility
 HTN
 Angina pectoris
 SVT

 Dizziness
 Hypotension
 Peripheral edema
 Constipation
 Gingival hyperplasia
 Grapefruit juice serum
levels

Dofetilide

Antiarrhythmic

K channel blocker

Blocks delayed K channels
in cardiac tissue
 Slows repolarization &
prolongs refractory period
 QT interval
 AF, A flutter
 Monitor QT interval during
initial dose titration

 QT prolongation
 Torsade de pointes

Enalapril

Antihypertensive

ACE inhibitor

Inhibits ACE & formation of AT
II






Vasodilation
aldosterone secretion
CO
V remodeling
survival in heart failure






HTN
Heart failure
Post-MI
progression of diabetic
nephropathy

 Cough & angioedema

Inhibits bradykinin
degradation

 Hypotension
 Taste disturbances

Esmolol

Antiarrhythmic

Class II

Selective 1 blocker

Blocks SNS stim. SA & AV
nodes
 HR
 AV conduction
 AV refractory period
 Sinus tachycardia & SVT
during/after surgery
 Rapidly metabolized by plasma
esterase

 Hypotension
 Bradycardia

Fenoldopam

Antihypertensive

D1-like receptor agonist

D1 receptor agonist
 Arteriolar vasodilation

Afferent & efferent renal
arterioles

 renal blood flow

 Hypertensive
emergencies

 serum K levels

Monitor for
hypokalemia

Furosemide

Loop-acting diuretic

Membrane ion transport
inhibitor

Inhibits Na/K/2Cl cotransporter
in ascending loop of Henle
 Blocks NaCl reabsorption





Edema
Heart failure
HTN
Hypercalcemia

 Ca excretion
 Na/K exchange in collecting duct






Hypokalemia
Metabolic alkalosis
Hyperuricemia
Hypomagnesemia

 ototoxicity of
aminoglycoside ABX

Hydralazine

Antihypertensive. heart failure

Vasodilator

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

 Edema
 Reflex tachycardia & MI
 Lupus syndrome

Hydrochlorothiazide

Antihypertensive

Thiazide diuretic

 Hypokalemia
 Metabolic alkalosis
 Hyperuricemia & gout

Inhibits NaCl
transporter in distal
tubule

 excretion of lithium

 excretion Na, K, Cl
 Ca excretion
 HTN
 Nephrogenic DI
 Nephrolithiasis

Labetolol

Antihypertensive

Adrenergic &
receptor antagonist

Selective 1 &
nonselective 1, 2
blockers
HTN

Postural hypotension
Abrupt w/drawal
cause life-threatening
HTN, arrhythmias, or
MI

Mannitol

Diuretic

Osmotic Diuretic

Osmotic attraction of
edematous & ocular
fluid

Filtered by glomerulus

 electrolyte excretion
 Oliguric renal failure
 Cerebral edema ICP
 Acute glaucoma

 Electrolyte imbalances
 Transient volume
expansion

Pulmonary edema or
heart failure

Methyldopa

Antihypertensive

Adrenergic 2 receptor
agonist

Converted to active
form methylnorepinephrine which
activates central 2
receptor agonist
 SNS outflow from
vasomotor center
 HTN
 HTN in pregnancy

 Positive direct Coombs

test

Minoxidil

Antihypertensive, hair growth
stimulant

Vasodilator, K channel
opener

Opens K channels in
vascular smooth m.
 Hyperpolarization
 m. relaxation
 vasodilation

Stim. resting hair follicle 

growth follicles
 Severe HTN
 Topical for alopecia

 Systemic admin.

Reflex tachycardia

Angina pericarditis

Pulmonary HTN

hypertrichosis

Nesiritide

Heart failure Tx

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

 Hypotension

Nitroglycerin

Antianginal

Organic nitrate

Releases NO in vascular
smooth m.
 Vasodilation
 coronary blood flow
 myocardial O2 demand
 Angina pectoris

Sublingual or lingual admin.

Short half-life

 HA
 Hypotension
 Syncope
 Reflex tachycardia
 vasodilative effect of
sildenafil, tadalafil,
vardenafil

Nitroprusside

Antihypertensive

Vasodilator

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

 CN toxicity
 Hypotension
 HA

Propafenone

Antiarrhythmic

Class IC Na channel
blocker

 Proarrhythmic 1st 2 wks

Monitor ECG when
starting Tx

 GI disturbances

Blocks Na channel in
cardiac tissue
 conduction & prevent
re-entry
 PR, QRS, & QT
duration
SVT & life-threatening
V arrhythmias

 digoxin levels

Quinidine

Antiarrhythmic

Class IA Na channel
blocker

Blocks Na & K channels
in cardiac tissue
 conduction
 QRS & QT duration
SVT & VT
D-isomer = quinine,
used to treat malaria
pts

 Cinchonism

Blurred vision

Tinnitus

Photophobia

 levels w/

Amiodarone

Cimetidine

Diltiazem

Verapamil

Grapefruit juice

Sotalol

Antiarrhythmic

Class III K channel blocker

Blocks K channels in cardiac
tissue
 Prolongs repol.
 refractory period & QT
interval

Blocks adrenergic
receptors
 SVT & life-threatening
arrhythmias

 Torsades de pointes

Spironolactone

K-sparring diuretic

Aldosterone antagonist

Blocks aldosterone
receptors
 Na excretion
 K excretion
Primary
hyperaldosteronism
HTN
hypokalemia

Gynecomastia
Impotence
Hyperkalemia

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

Non-dihydropyridine Ca
channel blocker

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

 Peripheral edema
 Constipation
 Gingival hyperplasia

CNS Depressants


Buspirone

Carbamazepine

Diazepam

Disulfiram

Ethosuximide

Flumazeil

Gabapentin

Lamotrigine

Lorazepam

Phenobarbital

Phenytoin

Topiramate

Valproate

Zolpidem

Busprione

Antianxiety

5-HT1A partial agonist

Activates presynaptic 5-HT1A
receptors in dorsal raphe
nucleus
 firing serotonergic neurons
 Generalized anxiety disorder
 NO

Drug dependence
Significant sedation
Muscle relaxation
Anticonvulsant effects














Dizziness
Drowsiness
Fatigue
HA
Excitement
Nervousness
Blurred vision
Tachycardia
N
Rash
Myalgia
Sweating

 levels by

Erythromycin

Itraconazole

Grapefruit juice

Carbamazepine

Anticonvulsant

Neuronal Na channel blocker

Blocks Na channels in CNS
 firing of ectopic foci &
spread of epileptic seizures
 Partial seizures & generalized
tonic-clonic seizures
 Bipolar disorders
 Trigeminal neuralgia
 Neuropathic pain








Ataxia
Drowsiness
Blurred vision
Agranulocytosis
Aplastic anemia
Thrombocytopenia

 Induces its own metabolism

Diazepam

Antianxiety

Benzodiazepine

Binds receptors on GABA
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

 Drowsiness
 Lethargy
 Physical/psychological
dependence
 Tolerance

Disulfiram

Alcohol abuse Tx

Acetaldehyde dehydrogenase
inhibitor

Inhibits acetaldehyde
degradation following alcohol
ingestion








Blurred vision
Chest pain
Dizziness
Palpitations
N, V
HA
Weakness

 Reinforcement of alcohol
abstinence

 Drowsiness

Ethosuximide

Anticonvulsant

Succimide

Binds T-type Ca
channels in thalamic
neurons
Suppresses nerve
transmissions to
motor cortex
Generalized absence
seizures

Petit mal epilepsy

 Dizziness
 Drowsiness
 Gastric distress
N

Flumazenil

Antidote

Benzodiazepine
receptor antagonist

Blocks benzodiazepine
receptors
 Counteract adverse
effects of
benzodiazepines

Respiratory depression
d/t IV OD

 CI in status epilepticus

 Seizures
 Dizziness
 Emotional lability

Gabapentin

Anticonvulsant

GABA analogue

GABA release from
central neurons
 Inhibits neuronal
discharges from seizure
foci
 Inhibits pain
neurotransmission
 Partial seizures
 Chronic pain
 Migraine prophylaxis

 Ataxia
 Dizziness
 Drowsiness
 Nystagmus
 Tremor

Lamotrigine

Anticonvulsant

Phenyltriazine

Blocks voltagesensitive Na channels
 Release of glutamate
 Prevents spread of
seizure foci discharges
 Adjunct/monotherapy for
partial seizures in adults

 Skin rash in 1st 8 wk of

Tx

Can progress to
Stevens-Johnson syn

 Ataxia
 Dizziness
 Drowsiness
 Photosensitivity
 metabolism & ADR w/
valproate

Lorazepam

Sedative-hypnotic, anxiolytic

Benzodiazepine

Binds benzodiazepine
receptors on GABA operate Cl
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

 Dizziness
 Drowsiness
 Apnea & cardiac arrest w/ rapid IV
admin
 Additive depression w/ alcohol & other
depressants

Phenobarbital

Sedative-hypnotic,
anticonvulsant

Barbiturate

Binds GABA operated Cl ion
channel increasing duration
of channel opening
 Cl influx in absence of
GABA





Tonic-clonic & partial seizures

Febrile seizures in children
Preoperative sedation
Short-term hypnotic

 folate requirement during

long-term Tx







Drowsiness
Lethargy
Delirium
Hangover
Physical & psychological
dependence

 Induces CYP P450 metabolism

of drugs

Phenytoin

Anticonvulsant

Hydantoin

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






Ataxia
Diplopia
Nystagmus
Gingival hyperplasia

Topiramate

Anticonvulsant

Monosaccharide derivative

Block voltage-sensitive Na
channels
 Augments GABA activation
of GABA receptors

Blocks glutamate
receptors

 Partial & tonic-clonic seizures

 Decrease dose in pts w/ renal
impairment











Ataxia
Dizziness
Drowsiness
Fatigue
Impaired concentration &
memory
Psychomotor slowing
Speech problems
Diplopia
Nystagmus

Valproate

Anticonvulsant

Branched-chain FA

GABA levels by release
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







Indigestion
N, V
Dizziness
Sedation
Hepatotoxicity

Zolpidem

Non-benzodiazepine hypnotic

Imidazopyridine

Activates BZBP receptors
on GABA operated Cl ion
channel
 channel affinity for GABA
& frequency of channel
opening

Neuronal
hyperpolarization

 Insomnia

Endocrine



Acarbose
Alendronate
Calcitonin
Danazol
Desmopressin
Ergocalciferol
Ethinyl estradiol &
drospirenone
Ethinyl estradiol &
norethindrone
Finasteride
Fludrocortisone
Glyburide
Hydrocortisone

Insulin
Levothyroxine
Medroxyprogesterone
Metformin
Methimazole
Mifepristone
Octreotide
Oxytocin
Pioglitazone
Prednisone
Raloxifene
Repaglinide
Somatropin
Testosterone

Acarbose

Antidiabetic

-glucosidase inhibitor

Inhibits intestinal enzyme
that converts
oligosaccharides &
disaccharides to glucose

digestion of starch &
sucrose

postprandial blood
glucose & HbA1c
 Type II DM

 Intestinal bloating
 Flatulence
 oral bioavailability of
metformin
 iron absorption

Alendronate

Bone resorption inhibitor

Bisphosphonate

Prevents attachment of
osteoclast precursor cells to
bone

metabolic activity of
osteoclasts & ability to
resorb bone
 Prevent/Tx

Osteoporosis

Corticosteroid-induced
osteoporosis

Pagets ds of bone

hypercalcemia

 Absorption by Ca
supplements, antacids,
foods, beverages (except
water)

Calcitonin

Ca hormone

Thyroid gland hormone

Binds calcitonin receptor on
osteoclasts
 cAMP & inhibits osteoclast
activity

bone resorption, bone

pain, & serum [Ca]
 Postmenopausal osteoporosis
 Pagets ds of bone
 hypercalcemia

Danazol

Ovarian inhibitor

Synthetic androgen,
antiestrogen

Feedback inhibits pituitary
FSH & LH secretion
ovarian estrogen secretion &
stim. endometrial & breast
tissue.
 Endometriosis
 Fibrocystic breast ds
 Hereditary angioedema

C1 esterase inhibitor &
C4 complement
component

 CI in pregnancy
androgenic effects on
female fetus
 Emotional lability
 Deepening voice
 Acne
 Hirsutism
 Amenorrhea
 breast size

Desmopressin

Posterior pituitary hormone

Vasopressin, ADH analogue

Mimics natural vasopression
 Increases water
reabsorption in kidneys
 Vasoconstriction
 DI
 Nocturnal enuresis
 Control bleeding in
hemophilia & wWFs ds
 Intranasal, oral, or IV

Ergocalciferol

Vit. D

Fat-soluble

 Hypercalcemia
 Hypercalciuria

Activated in liver & kidneys

to form calcitriol

 Cholestyramine inhibits
vit. D absorption
 Induce vit. D
metabolism

 Ca & phosphorus
absorption from gut
 Vit. D deficiency

Rickets, osteomalacia

 Chronic renal failure

 Familial hypophosphatemia
 Hypocalcemia d/t
hypoparathyroidism
 Postoperative & idiopathic
tetany

Phenytoin

Barbiturates

Ethinyl estradiol & drospirenone

OCP

Estrogen & progesterone

Feedback inhibit GnRH
 Estrogen

FSH secretion &
maturation of dominant
follicle

 Progesterone

Inhibits midcycle LH
surge & ovulation

 Contraception
 Regulate menstrual cycle
 Acne in women

Drospirenone
Antiandrogenic
Blocks aldosterone

salt & water retention

BP

Thromboembolism

risk w/ smoking

Edema
Efficacy w/

ABX

Carbamazepine

phenytoin

Ethinyl estradiol & norethindrone

OCP

Estrogen & progesterone

Feedback inhibit GnRH
 Estrogen

FSH secretion &
maturation of dominant
follicle

 Progesterone

Inhibits midcycle LH
surge & ovulation

 Contraception
 Regulate menstrual cycle
 Acne in women

Norethidrone
 Slightly androgenic
 Thromboembolism
 Edema
 Depression
 Gallbladder ds

Finasteride

Androgen synthesis inhibitor

5--reductase inhibitor

Inhibits conversion
testosterone 
dihydrotestosterone &
androgenic stimulation of
prostate & skin

prostate size & promotes
hair growth
 BPH
 Male pattern baldness

 CI pregnancy

Risk to male fetus

Do NOT handle tablets

 Impotence

Fludrocortisone

Corticosteroid

Mineralocorticoid

Activates aldosterone
receptors in renal distal
tubule
 Na reabsorption
 K & H excretion
 Adrenal insufficiency

Addisons ds

 Congenital adrenogenital syn

 Tx idiopathic orthostatic
hypotension w/ Na intake

 Hypokalemia

by thiazide & loop
diuretics

Glyburide

Antidiabetic

Sulfonylurea 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

 Photosensitivity
 Hypoglycemia

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

Pancreatic hormone

Replaces endogenous
insulin
 DM
 Rapid acting lispro
 Intermediate acting
lente
 Long acting ultralente

Hypoglycemia
-blockers mask signs
of hypoglycemia &
prolong recovery

Levothyroxine

Thyroid hormone

Tetraiodothyronine

Binds nuclear receptors
& gene transcription
 metabolic rate, protein
synthesis,
gluconeogenesis, cell
growth & differentiation,
& CNS development

Converted to T3 in
tissues
 Hypothyroidism

Insomnia
Irritability
Tachycardia
Wt loss
Bile acid sequestrants
absorption

Medroxyprogesterone

Progestin, contraceptive

Progesterone analogue

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

 Amenorrhea
 Breakthrough bleeding
 Dysmenorrhea

Metformin

Antidiabetic

Biguanide, antihyperglycemic

# & 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

 N, V, D
 Abdominal bloating

Methimazole

Antithyroid

Thiourea, thyroid
hormone synthesis
inhibitor

Inhibits peroxidase &
iodination & coupling of
tyrosine residue of
thyroglobulin

thyroxine secretion
 Hyperthyroidism
Graves ds

Rash
Agranulocytosis

Mifepristone

Abortificient

Progesterone antagonist

Partial agonist or antagonist
progesterone receptors
 Medical termination of
pregnancy through 49d
gestation
 Single dose + prostaglandin
for 48hr stim. uterine
contractions

 Abdominal pain
 Diarrhea
 N, V
 Uterine bleeding
 Cramping

Octreotide

GH inhibitor, antidiarrheal

Somatostatin analogue w/
greater effects on GH than
insulin secretion

Suppresses secretion of GH,
insulin-like growth factors,
5-HT & GI peptides gastrin,
motilin, secretin, & VIP
 Acromegaly
 Severe diarrhea & flushing d/t
carcinoid tumors & VIP
tumors
 Bleeding GE varices
 Complications of pancreatic
surgery









Arrhythmias
Hyperglycemia
Hypoglycemia
Constipation
Diarrhea
Flatulence
N

Oxytocin

Oxytocic

Posterior pituitary hormone

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

 Excessive & painful

uterine contractions

Pioglitazone

Antidiabetic

Thiazolidinedione
antihyperglycemic

Activates peroxisome
proliferator-activated receptor-
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

Corticosteroid

Suppresses
inflammation & immune
response
 Inflammatory, allergic,
autoimmune, & neoplastic
ds
 Prevent organ transplant
rejection
 Asthma

 Depression or euphoria
 HTN
 Acne
 Impaired wound healing
 Adrenal suppression
 Muscle wasting
 Osteoporosis
 Cushingoid appearance

Moon facies

Buffalo hump

 susceptibility to infection

Raloxifene

Bone resorption inhibitor

Selective estrogen receptor
modulator SERM

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

 Hot flashes
 Cholestyramine inhibits
absorption

Repaglinide

Antidiabetic

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

 Hypoglycemia

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

Gonadal steroid

Activated gene transcription &
development of male sex organs &
secondary sex characteristics

lean body mass

Stim. skeletal growth

Accelerates epiphyseal closure

sebaceous gland sebum
production

EPO secretion

HDL levels
 Hypogonadism in androgen-deficient
men
 Delayed puberty in males








Edema
Acne
Gynecomastia
Impotence
Oligospermia
Priapism

Gastrointestinal


Bisacodyl

Calcium carbonate

Dicyclomine

Docusate

Lactulose

Loperamide

Mesalamine

Metoclopramide

Misoprostol

Omeprazole

Ondansetron

Promethazine

Ranitidine

Sucralfate

Tegaserod

Bisacodyl

Stimulant laxative

Inhibits GI fluid
reabsorption &
stimulates
peristalsis
Bowel evacuation prior
colonoscopy or surgery
Acute constipation

Cramping
N
Fluid & electrolyte
depletion

Hypokalemia

Calcium carbonate

Antacid, Ca supplement

Ca salt

Neutralizes gastric acid

Provides Ca
supplementation
 Dyspepsia
 Hypocalcemia
 Prevention of osteoporosis
 Admin 1-1.5hr after meals &
@ bedtime

 Constipation
 absorption of drugs

Tetracyclines
Fluoroquinolones
Phenytoin
Iron salts

Dicyclomine

Antispasmodic

Muscarinic receptor
antagonist

Blocks PNS stim.
intrinsic nervous
system & GI tone &
motility
 Directly relaxes GI
smooth m.
 IBS cramping & pain

 Constipation
 Dyspepsia
 Dry mouth
 Urinary retention
 Blurred vision
 Decreased sweating

Docusate

Stool softener, laxative

Surface-active agent

Facilitates hydration of
fecal material & softens
feces
 Constipation
 Fecal impaction rectal
enema

Lactulose

Laxative

Osmotic agent

water content & softens
feces

Lowers pH of colon
 Converts ammonia 
ammonium ion & ammonia
absorption & blood levels
 Chronic constipation
 Hepatic encephalopathy

Improves mental status

 Cramping
 Abdominal distention
 Flatulence

Loperamide

Antidiarrheal

Opioid analogue

Activates opioid receptors in GI
smooth m.
 Segmental contraction & inhibits
peristalsis
 Mild-moderate acute diarrhea
 Chronic diarrhea d/t IBD
 volume of ileostomy drainage
 AVOID

Pregnancy

Lactation

Children < 2 y/o

 Constipation
 Drowsiness
 Additive effects

Kava

Chamomile

Valerian

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

D2 receptor antagonist

Blocks relaxant effect of D on
GI smooth m.

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

 CI in Parkinsons ds & seizure

disorders
 Drowsiness
 EPS rxns
 restlessness

Misoprostol

Cytoprotective

Synthetic PGE1
analogue

gastric mucosal
secretion & secretion
of bicarbonate & mucus
 Prevent gastric mucosal
injury from NSAIDs
 Abortificient in combo w/
mifepristone

 CI in pregnancy
 Abdominal pain
D
 Miscarriage

Omeprazole

Antiulcer

Proton pump inhibitor

Irreversibly inhibits H/K ATP
pump in gastric parietal cells
 Prevents gastric acid
secretion





Peptic ulcer ds
GE reflux
Zollinger-Ellison syn
dyspepsia

 Abdominal pain
 Inhibits metabolism

Diazepam

Cyclosporine

Phenytoin

Ondansetron

Antiemetic

5-HT3 receptor antagonist

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

 HA
 Constipation
D

Promethazine

Antiemetic, antihistamine,
sedative

H1 receptor antagonist,
phenothiazine

Blocks H1 & M1 receptors

Inhibits stim. chemoreceptor
trigger zone & vomiting
center
 N, V
 Preoperative sedation
 Allergic rxns

 Neuroleptic malignant syn

 Sedation
 Confusion
 Disorientation

Ranitidine

Antiulcer

H2 receptor antagonist

Blocks H2 receptors in
gastric parietal cells
 gastric acid secretion
 Peptic ulcer ds
 GE reflux
 Dyspepsia

Sucralfate

Antiulcer

Cytoprotective, sulfated
polysaccharide

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

 Constipation
 absorption

Fat soluble vitamins

fluoroquinolones

Tegaserod

GI motility agent

Partial agonist @ 5-HT4
receptors

Activates 5-HT4
receptors on sensory
neurons in enteric
nervous system
 Release
neurotransmitters &
peristalsis
 IBS in women w/
constipation

 Diarrhea
 Ischemic colitis

Hematologic



Abciximab
Alteplase
Aspirin
Atorvastatin
Bivalirudin
Cholestyramine
Cilostazol
Clopidogrel
Cyclosporine
Enoxaparin

Epoetin
Eptifibatide
Ezetimibe
Filgrastim
Folic acid
Gemfibrozil
Heparin
Niacin
Sirolimus
Warfarin

Abciximab

Antithrombotic

Monoclonal Ab

Inactivates platelet gp
llb/llla receptors
 Prevents platelet
aggregation
 Prevent thrombosis during
coronary angioplasty &
stent placement

 Bleeding
 Thrombocytopenia

Alteplase

Thrombolytic

Plasminogen activator

Converts plasminogen 
plasmin
 Degrades fibrin & fibrinogen
 AMI
 Acute ischemic stroke
 Occluded central venous
access devices
 Streptokinase & urokinase for
pulmonary embolism

 Reperfusion arrhythmia
 Contraindications

Internal bleeding

Recent CNS surgery or
trauma

Atorvastatin

Cholesterol lowering agent

HMG-CoA reductase
inhibitor

HMG-CoA reductase, ratelimiting enzyme for
cholesterol
 hepatic cholesterol uptake
 LDL levels
 Hypercholesterolemia
 Cholesterol-lowering effects
w/ ezetimibe & bile acidbinding agents







Myalgia
Myositis
Rhabdomyolysis
Hepatitis
GI distress

 Effects w/

Grapefruit juice

Azole antifungals

cyclosporine

Bivalirudin

Anticoagulant

Hirudin analogue

Inhibits thrombin
 Prevents blood coagulation
 Thrombosis in unstable
angina
 AMI
 Stent insertion
 Used in pts w/ heparininduced thrombocytopenia

 Bleeding

Cholestyramine

Cholesterol-lowering
agent

Bile-acid binding resin

Binds intestinal bile
acids
 Prevents reabsorption
 cholesterol utilization

LDL levels

 Hypercholesterolemia
 Diarrhea d/t excess bile
acids

 Constipation
 Abdominal discomfort

Cilostazol

Antiplatelet

Platelet aggregation
inhibitor

Inhibits phosphodiesterase
III & cAMP in platelet &
blood vessels
 Inhibit platelet aggregation
 Causes vasodilation
 Intermittent claudication

Improves blood flow &
walking distance

 Additive effects w/ aspirin

 HA
 Effects w/ CYP3A4 inhibitors

Azole antifungals

Erythromycin

Grapefruit juice

Clopidogrel

Antiplatelet

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

 Hypersensitivity reaction

Cyclosprine

Immunosuppressant

IL2 expression inhibitor

Bind immunophilins
 Complex binds
calcineurin  inhibits
transcription of IL2
gene
 Prevent rejection of renal,
cardiac or hepatic
allografts
 Severe RA & psoriasis

 HTN
 Nephrotoxic
 Gingival hyperplasia
 Hirsutism
 Tremor
 Induce metabolism

Rifampin

Barbiturates

Carbamazepine

 Inhibits metabolism

Grapefruit juice

Enoxaparin

Parenteral anticoagulant

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

 Thrombocytopenia

Epoetin

Hematopoietic growth factor

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

 HTN

Eptifibatide

Antiplatelet

GP IIb/IIIa receptor
antagonist

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

 Bleeding

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

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

 Bone pain

Folic acid

Vitamin, hematologic agent

Metabolic cofactor for DNA
synthesis

 Absorption by

Activated folate transfer

one-carbon units to purine &
pyrimidine precursors

 Folate reductase inhibited by

MTX

 Megaloblastic anemia
 Fetal neural tube defects
 Coronary artery ds
 Pregnant woman have
requirements

Phenytoin

Cholestyramine

Gemfibrozil

Lipid-lowering agent

Fibric acid derivative

 GI distress
 Myositis

Activates peroxisome
proliferator activated
receptor-

 Statins risk
rhabdomyolisys

 Oxidizes FA & apo-AI & AII

 plasma triglycerides
 HDL
 Hypertriglyceridemia
 HDL levels
 Monitor LFTs throughout Tx

Heparin

Parenteral anticoagulant

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

Thrombocytopenia

Niacin

Vitamin, lipid-lowering agent

G-protein coupled receptor
ligand

Activates G-protein coupled
receptor
 Inhibits lipolysis & release
of FA
 hepatic triglyceride
synthesis & VLDL secretion





Hypertriglyceridemia
HDL
Hypercholesterolemia
Pellagra







Flushing
Pruritis
GI distress, peptic ulcer
Hyperglycemia
Hepatotoxicity

 Statins risk
rhabdomyolysis

Sirolimus

Immunosuppressant

T-lymphocyte inhibitor

Inhibits regulatory
kinase in cytokinedriven T-cell prolif.
 Combo w/ corticosteroid
& cyclosporine
 Prevent

Rejection renal allograph

Coronary stent
restenosis

 Leukopenia
 Thrombocytopenia
 Hyperlipidemia
 Rash
 blood levels

Cyclosporine

Azole antifungals

Erythromycin

Grapefruit juice

Cimetidine

Warfarin

Oral anticoagulant

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

 Fetal malformations
 Abnormal bone
development

Musculoskeletal


Acetaminophen

Allopurinol

Celecoxib

Cyclobenaprine

Etanercept

Ibuprofen

Indomethacin

Infliximab

Ketorolac

Probenecid &
colchicine

Acetaminophen

Analgesic, antipyretic

COX-3 inhibitor

Inhibits COX-3 selectively

Inhibits synthesis of PG
causing pain & fever
 Mild-moderate pain
 Fever
 Lacks anti-inflammatory &
antiplatelet activity

 OD cause fatal hepatic failure

 hepatotoxicity w/ alcohol
 renal toxicity w/ salicylates &
NSAIDs

Allopurinol

Antigout

Xanthine oxidase
inhibitor

 Rash
 Inhibits metabolism

Mercaptopurine

Inhibits xanthine
oxidase & catabolism of
purines  xanthine &
uric acid
 uric acid levels
 Prevent hyperuricemia &
gout

Celecoxib

NSAID

COX-2 inhibitor

Inhibits COX-2 &
synthesis of PG
causing pain, fever, &
inflammation
 OA
 RA
 Inflammatory jt ds

 GI bleeding
 risk stroke & MI

Cyclobenzaprine

Skeletal m. relaxant

Tricyclic central-acting
m. relaxant

 Dizziness
 Drowsiness
 Dry mouth

Acts on brainstem &

spinal cord to reduce
tonic somatic m.
activity via & motor
neurons

 AVOID MAOI

 Acute muscle spasm

Etanercept

Antirheumatic agent,
antitumor necrosis factor

Antitumor necrosis
factor p57 combined
w/ Fc of IgG

Binds TNF- & jt
inflammation & pain

Slows progression of
RA
 RA

 URI
 HA
 Ab response to live
virus vaccines

Ibuprofen

NSAID

Nonselective COX inhibitor

Inhibits COX-1 & COX-2 &
synthesis of PG causing
pain, fever, & inflammation
 Mild-moderate pain or
dysmenorrhea
 Inflammatory disorders

OA

RA

 risk colon, breast, lung, &

prostate cancers







GI bleeding
N, V
Dyspepsia
Allergic rxns
Hepatitis & renal failure

Indomethacin

NSAID

Nonselective COX inhibitor

Inhibits COX-1 & COX-2
 Inflammatory disorders

Gouty arthritis
OA
RA
Ankylosing spondylitis

 PDA in premature neonates









GI bleeding
N, V
Dyspepsia
Allergic rxns
Dizziness
Drowsiness
HA

Infliximab

Ds modifying
antirheumatic

Monoclonal Ab to TNF

Inactivates TNF- & jt
inflammation, pain, &
destruction

Sx of Crohns ds
 RA
 Crohns ds

 Fatigue
 N, V
 URI

Ketorolac

NSAID

Nonselective COX inhibitor

Inhibits COX-1 & COX-2 &
synthesis of PG causing
pain, fever, & inflammation
 Short-term pain management
 Prolongs bleeding time

Limit use to < 5d

 Aspirin-allergy
 Allergic rxn in pt w/ asthma
 Nasal polyps

Probenecid & Colchicine

Antigout

Uricosuric probenicid

Anti-inflammatory colchicine

Probenecid

Probenecid

Colchicine

 Inhibits renal reabsorption of

uric acid & uric acid secretion

Colchicine
 Inhibits leukocyte response to
monosodium urate crystals in jt
 Acute gouty arthritis
 Prevent gouty arthritis

 Inhibits renal tubular secretion

of Penicillins

Used to penicillin serum
levels

 D
 N, V
 Agranulocytosis & aplastic
anemia

Neurodegenerative


Baclofen

Benztropine

Donepezil

Entacapone

Interferon-beta-1b

Levodopa-carbidopa

Memantine

Pergolide

Selegiline

Baclofen

Antispasticity

GABA-B receptor agonist

neuronal cAMP & Ca
influx
 K influx
 motor neuron excitability
& inhibits spinal reflexes
 Spasticity

MS

Spinal cord injury

ALS

 Drowsiness
 Dizziness
 Fatigue
 Weakness
 Additive effects

Alcohol
Kava
Valerian
Chamomile

Benztropine

Anti-Parkinson

Central anticholinergic

Blocks cholinergic
receptors & restores
neurotransmitter balance
in basal ganglia
 Parkinsons ds
 Drug-induced EPS
 tremor > bradykinesia &
rigidity

 Blurred vision
 Dry eyes
 Constipation
 Dry mouth
 Urinary retention

Donepezil

Anti-Alzheimer

Cholinesterase inhibitor

Inhibits cholinesterase in
CNS
 Ach neurotransmission
 Slows decline in cognitive
function
 Alzheimers ds
 Does NOT prevent ds
progression

 N, D
 HA

Entacapone

Anti-Parkinson

Catechol-Omethyltransferase inhibitor

Inhibits catechol-omethyltransferase
inactivation of levodopa
 levodopa in CNS
 Prolongs response to levodopa &
S/Sx Parkinsons ds
 Adjunct to levodopa/carbidopa for
Parkinsons ds
 AVOID nonselective MAOI

 Rhabdomyolysis
 Neuroleptic malignant syndrome

Interferon-beta-1b

Anti-multiple sclerosis

Interferon

Binds cell surface
receptors producing
immuno-suppressive
effects
 relapse & slows
physical disability in MS
 Relapsing-remitting MS
 SubQ daily

 HA
 Weakness
 GI distress
 Sweating
 Neutropenia
 Myalgia
 Chills
 Fever

Levodopa-carbidopa

Anti-Parkinson

Dopamine precursor,
decarboxylase inhibitor

 Dyskinesia involuntary movements

 N, V
 Hallucinations

Levodopa

 arrhythmia w/ halothane

 Converted to D in CNS

Augments neurotransmission in
basal ganglia

Carbidopa
 Inhibits peripheral dopadecarboxylase

levodopa availability in CNS

 Parkinsons 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
 Alzheimers ds

Pergolide

Anti-Parkinson

Dopamine receptor
agonist

Activates D receptors
in basal ganglia
 Parkinsons ds in
conjunction w/
levodopa/carbidopa

 Dyskinesia
 Hallucination
 Orthostatic hypotension
 Constipation

Selegiline

Anti-Parkinson

Type B MAOI

Converted to active form
by MAO

Irreversibly inhibits D
degradation by MAO
 response to
levodopa/carbidopa Tx
 Parkinsons ds w/
levodopa/carbidopa
 Slows progression of
Parkinsons ds

 AVOID

Meperidine & opioids

Fatal rxn
Excitation
Rigidity
HTN
coma

SSRI

Serotonin syn

Tricyclics

Asystole
HTN
Syncope
Rigidity
seizures

Other Drugs


Alprostadil

Bosentan

Epoprostenol

Latanoprost

Mesna

Succimer

Alprostadil

Vasodilator

Prostaglandin E1

Activates PG EP receptors
 Vascular smooth m.
relaxation & vasodilation
 Maintain PDA in neonates
awaiting surgery

IV infusion

 Male erectile dysfunction

Local injection or pellets

 IV infusion

Apnea

Hypotension

Arrhythmia

 Local products

Prolonged/painful erection

lightheadedness

Bosentan

Vasodilator

Endothelin-1 receptor
antagonist

Blocks endothelin A & B
receptors

pulmonary vascular
resistance & dyspnea

Improves walking distance
 Pulmonary arterial HTN

 CI in pregnancy

Causes birth defects

 serum aminotransferase
levels

Epoprostenol

Vasodilator

Naturally occurring
prostacyclin (PGI2)

Activated prostaglandin IP
receptors
 Vascular smooth m.
relaxation

pulmonary blood flow &

reduces dyspnea
 Pulmonary arterial HTN







Flushing
Hypotension
Tachycardia
Diarrhea
N, V

Latanoprost

Ocular hypotensive agent

Prostaglandin F2 analogue

Activates prostaglandin FP
receptors

aqueous humor outflow via
uveoscleral pathways

Lowers intraocular pressure
 Chronic open-angle glaucoma
 Topical ocular admin

 Alters color of iris causing

permanent eye color change
by amount of melanin in
melanocytes

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 &
dextroamphetamine

Atomoxetine

Buproprion

Desipramine

Fluoxetine

Haloperidol

Lithium

Methylphenidate
Mirtazapine
Olanzapine
Phenelzine
Risperidone
Thioridazine
Venlafaxine

Amitriptyline

Antidepressant

Tricyclic

Blocks neuronal reuptake of
serotonin > norepinephrine

Blocks muscarinic & adrenergic receptors
 Chronic pain
 Depression
 Delayed onset of antidepressant
effect >4 wks
 AVOID

MAOI

SSRI








Lethargy
Sedation
Blurred vision
Constipation
Urinary retention
appetite & wt gain

 OD wide QRS complex VT

 Altered effects by drugs that
inhibit/induce CYP450

Carbamazepine

Quinidine

Rifampin

Amphetamine

CNS stimulant

Sympathomimetic
amine

neuronal release of
norepinephrine
 ADHD

attention span

motor restlessness

 Narcolepsy

mental alertness

drowsiness & fatigue










Tachycardia
HTN
Anorexia
Irritability
Insomnia
Tremor
Growth inhibition
Drug dependence

 HTN crisis w/ MAOI

Atomoxetine

ADHD agent

Selective NE reuptake
inhibitor

Inhibits neuronal
reuptake of NE in CNS
 ADHD in children/adults
 levels & effect in slow
metabolizers CYP2D6

 appetite
 Insomnia
 Levels & effects altered by
drugs that inhibit/induce
CYP2D6

Bupropion

Antidepressant

Neuronal reuptake
inhibitor

Inhibits neuronal
reuptake of DA > 5-HT &
NE
 Depression
 Smoking cessation
 Delayed onset for
antidepressant effects

 Agitation
 HA
 Dry mouth
N
 Tremor
 Impaired motor &
cognitive skills
 MAOI adverse effects
 Seizure risks w/
phenothiazines

Desipramine

Antidepressant

Tricyclic

Blocks neuronal reuptake NE >
5-HT

Blocks muscarinic & adrenergic receptors
 Depression
 Chronic pain
 Delayed onset for antidepressant
effects
 AVOID

MAOI

SSRI








Lethargy
Sedation
Blurred vision
Constipation
Urinary retention
appetite & wt gain

 OD wide QRS complex VT

Fluoxetine

Antidepressant

SSRI

Inhibits neuronal reuptake of
serotonin









Depression
OCD
Bulimia nervosa
Anorexia nervosa
Fibromyalgia
Panic attacks
Phobias
Prementsrual dysmorphic disorder

 Active metabolite 5-7d half-life

 AVOID MAOI









Anxiety
Drowsiness
Insomnia
Nervousness
Sexual dysfunction
Sweating
Tremor

 levels metabolized by CYP2D6

Haloperidol

Typical antipsychotic

Butyrophenone

Blocks D2 receptors in
mesolimbic area,
chemoreceptor trigger
zone, solitary tract, &
basal ganglia

Blocks muscarinic & adrenergic receptors
 Psychotic disorders

Schizophrenia

 Tourettes 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

Inorganic cation

noradrenergic
neurotransmission or effects
b/c of cAMP

Inhibition of inositol-1phosphatase
 Depletion of inositol & IP3

Improved Na transport via Na

pump
 Bipolar affective disorder
 Monitor serum levels

Toxicity > 2.5










Polyuria
Impaired memory
Acne
Tremor
ECG changes
GI distress
Hypothyroidism
Leukocytosis

 NM toxicity w/ haloperidol
 toxicity

Diuretics

NSAIDS

Fluoxetine

Methyphenidate

CNS stimulant

Sympathomimetic
amine

neuronal release NE
 ADHD

attention span

motor restlessness

 Narcolepsy

mental alertness

drowsiness & fatigue

 Tachycardia
 HTN
 Anorexia
 Irritability
 Insomnia
 Tremor
 Growth inhibition
 Dependence
 HTN crisis w/ MAOI

Mirtazapine

Antidepressant

Tetracyclic

Inhibits presynaptic 2
autoreceptors &
heteroreceptors
 NE & 5-HT release
 Depression
 Appetite stimulation
 AVOID MAOI

HTN, seizure, death






appetite & wt gain

Constipation
Dry mouth
Drowsiness

Olanzapine

Atypical antipsychotic

Thienobenzodiazepine

Blocks D2 & 5-HT2 receptors in
CNS

Blocks H1, muscarinic, & adrenergic receptors
 Schizophrenia
 Manic episodes of biploar
 Anorexia nervosa
 Oral tablets contain aspartame

Avoid in phenylketonuria













Agitation
Dizziness
Restlessness
Sedation
Amblyopia
Orthostatic hypotension
Tachycardia
Constipation
Dry mouth
Wt gain
Tremor

Phenelzine

Antidepressant

MAOI

Inhibits MAO & CNS levels of
NE & 5-HT
 Neurotic & atypical depression
 Avoid

Fluoxetine

Tyramine








Dizziness
Insomnia
Restlessness
Blurred vision
Orthostatic hypotension
Diarrhea

 Potentially fatal

SSRI

Tricyclics

 HTN crisis

Tyramine
Amphetamines
Methyldopa
Levodopa

Risperidone

Atypical antipsychotic

Benzisoxazole

Blocks 5-HT2 > D2
receptors in CNS

Blocks H1 & -adrenergic
receptors
 Schizophrenia
 Psychotic disorders
 Monitor pt for neuroleptic
malignant syn









Aggressive behavior
Extrapyramidal rxns
Sleep disturbances
Insomnia
Sedation
Constipation or diarrhea
Wt gain

Thioridazine

Typical antipsychotic

Phenothiazine

Blocks D2 receptors in
mesolimbic area,
chemoreceptor trigger
zone, solitary tract, &
basal ganglia

Blocks muscarinic
receptors
 Psychotic disorders
 Schizophrenia

 Extrapyramidal rxns
 Tardive dyskinesia
 Photosensitivity
 Potential for V
arrhythmias & sudden
death
 Retinal pigmentation w/
high doses

melanosis

Venlafaxine

Antidepressant

Phenethylamine

Inhibits neuronal
reuptake 5-HT & NE
 Depression
 Generalized anxiety
disorder
 AVOID MAOI

 Sexual dysfunction
 GI distress
 Dizziness
 Insomnia
 Nervousness

Respiratory


Albuterol

Cromolyn

Diphenhydramine

Fluticasone

Ipratropium

Loratadine

Montelukast

Omalizumab

Salmeterol

Theophylline

Zileuton

Albuterol

Bonchodilator

2 receptor agonist

Activates 2 receptors in
bronchial smooth m.
 cAMP  activating kinases
 Inhibiting myosin
phosphorylase  m. relaxation
 Asthma

Acute bronchospasm

Prevent exercise-induced
asthma

 Chronic bronchitis & emphysema

Reversible airway obstruction

 Muscle tremor
 Nervousness
 Restlessness
 Tachycardia
 HTN crisis w/ MAOI

Cromolyn

Antiasthmatic & antiallergy

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

 Nasal & throat irritation

Diphenhydramine

Antihistamine, sedative,
antiemetic

H1 receptor antagonist

Blocks H1 & muscarinic
receptors
 Prevents histamineinduced allergic rxns
 Prevents vestibular stim.
of vomiting center
 Sedation
 Allergic rxns
 Prevent motion sickness
 Insomnia

 Drowsiness
 Blurred vision
 Dry mouth
 Urinary retention
 Anorexia

Fluticasone

Anti-inflammatory

Corticosteroid

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

 Nasal & throat irritation

 Oral candidiasis

Ipratropium

Bronchodilator

Muscarinic receptor
antagonist

Blocks muscarinic receptors
in bronchial smooth m. &
nasal mucosa

Prevents vagal-stimulated
bronchoconstriction
 COPD
 Rhinitis
 Asthma
 Inhalation admin

 Cough
 Nasal dryness & irritation

Loratadine

Antihistamine

H1 receptor antagonist

Blocks H1 receptors in
nasal mucosa

Prevents allergic rxns
Seasonal rhinitis
Chronic idiopathic
urticaria
Less sedating than
diphenhydramine

Montelukast

Antiasthmatic

Leukotriene antagonist

Blocks cysteinyl leukotriene1 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

IgE antagonist

Blocks IgE
Severe asthma in
combo w/ corticosteroid
therapy
SubQ every 2-4 wks

Allergic rxns

anaphylaxis

Salmeterol

Bronchodilator

2 agonist

cAMP

Relaxes bronchial smooth
m.

Inhibits late phase allergeninduced
bronchoconstriction
 Asthma

Prevent nocturnal attacks

Exercise-induced asthma

NOT acute bronchospasm

 Inhalation admin

 Tachycardia
 Nervousness
 HA

Theophylline

Bronchodilator

Methylxanthine

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






N, V
Anxiety
Insomnia
Tachycardia

Zileuton

Antiasthmatic

Leukotriene synthesis
inhibitor

Inhibits 5-lipoxygenase
& leukotriene synthesis
 Prevents airway
inflammation &
bronchoconstriction
 Long-term asthma control

Flu-like syn
HA
Drowsiness
Dyspepsia
 serum
aminotransferase levels
& hepatitis
Inhibits CYP450 & 3A4

theophylline &
warfarin levels