Drug
Penicillins
Penicillin G
Penicillin V
Methicillin
Nafcillin
Dicloxacillin
Ampicillin
Class
-lactam
(parenteral)
-lactam
(oral)
Anti-Staph PCN
(IV dose)
Anti-Staph PCN
(IV dose)
Anti-Staph PCN
(oral)
Extended-spectrum PCN
Gram(-) rods
Amoxicillin
Extended-spectrum PCN
(oral)
Ticarcillin
Anti-Pseudomonal PCN
Piperacillin
Anti-Pseudomonal PCN
Cephalosporins
Cephalexin
1st-generation
(oral)
Cefazolin
(Keflex)
1st-generation
(parenteral)
Cefuroxime
2nd-generation
(parenteral, longer t1/2)
Cefuroxime axetil
2nd-generation
(oral)
2nd-generation
(parenteral)
Cefoxitin
Cefixime
3rd-generation
(oral)
Ceftriaxone
(Rocephin)
3rd-generation
(parenteral, longest t1/2)
Ceftazidime
3rd-generation
(parenteral)
4th-generation
Cefepime
Other Cell Wall Synthesis Inhibitors
Imipenem
Carbapenems
(very broad spectrum)
Uses
DOC Strep, Enterococci,
Pneumococci, spirochetes,
B. anthracis, Clostridium,
non--lactamase Staph
DOC syphilis (IM dose)
Minor infections
(mixed oral infections)
-lactamase Staph
Serious systemic -lactamase
Staph
NOT Enterococci & MRSA
Mild local Staph in kids
Serious anaerobes,
Enterococci, Listeria, Gram(-)
cocci & bacilli
NOT Klebsiella, Enterobacter,
or Pseudomonas
DOC URI, sinusitis, otitis, LRI
Dental prophylaxis
Gram(-) bacilli (Klebsiella,
Enterobacter, Pseudomonas)
Hospital-acquired,
neutropenic patients
Gram(-) bacilli (Klebsiella,
Enterobacter, Pseudomonas)
Hospital-acquired,
neutropenic patients
PCN-G organisms + Proteus,
E. coli, & Klebsiella (PEcK)
NOT MRSA, Listeria,
Clostridium, Enterococci
Same as above
Surgical prophylaxis against
skin microbes
Same as 1st-generation + H.
influenzae, Enterobacter, &
Neisseria (HENPEcK)
Same as above
-lactamase organisms
Anaerobes (esp. Bacteroides)
Intraabdominal & GYN sepsis
Surgical prophylaxis
HENPEcK + most enterics +
Serratia
Less against Gram(+) cocci
DOC meningitis; PCNresistant Neisseria;
DOC Lyme dz
Pseudomonas
Side effects
Allergies, seizures (high dose
w/ renal failure)
Allergies, nephrotoxic
(Naficillin preferred)
Allergies
Allergies
Allergies, GI upset,
superinfections, non-allergic
skin rashes
Allergies, GI upset,
superinfections, non-allergic
skin rashes
Allergies
Allergies
Allergies
Potentially nephrotoxic
Crosses BBB
Bronchitis & pneumonia in
elderly & imczd
Well-absorbed
Allergies
Potentially nephrotoxic
Allergies
Potentially nephrotoxic
Once-a-day dosing
Allergies
Potentially nephrotoxic
Crosses BBB & bone
Excreted in bile (good for
renal dz)
NOT E. faecium, MRSA,
Clostridium (metallo--lactamase)
(slow IV drip, oral for colitis)
Serious Gram(+), MRSA,
Clostridial colitis, heart valve
implant, endocarditis
NOT Gram(-)
Penetrates bone
Allergies
Potentially nephrotoxic
GI upset, rash, infusion site
rxn, seizures (renal dz)
Vancomycin
Combo w/ Clavulanate
Combo w/ aminoglycoside
(Tobramycin) to avoid
resistance
Combo w/ Tazobactam
Combo w/ aminoglycoside
(Tobramycin) to avoid
resistance
More resistant to lactamases
DOC Enterobacter
Gram(+) & (-), anaerobes
Gram(-) rods
NOT Gram(+) or anaerobes
Combo w/ Sulbactam (lactamase inhibitor)
Widespread resistance
(NOT for UTI, meningitis,
or typhoid fever)
Combo w/ Clavulanate
(Augmentin)
Allergies (5-15% crossreactivity w/ PCN allergies,
ONLY w/ delayed-type rxn)
Nephrotoxic
Same as above
Enterobacter (more resistant
to -lactamases)
Monobactams
(narrow spectrum, IV dose)
MUST combine w/
aminoglycoside for
Enterococci
Amoxicillin preferred
Allergies
Potentially nephrotoxic
Allergies
Potentially nephrotoxic
Aztreonam
Features
Rash, serum
aminotransferases
Expensive
Reserved
Crosses BBB & bone
Combo w/ Cilastatin
(Primaxin) prevents renal
inactivation
Renal excretion
(well-tolerated w/ PCN-allergies)
Fever, chills, infusion site rxn,
tachycardia, hypotension, red
man syndrome (histamine
release), ototoxicity,
nephrotoxicity (w/ AGs)
Crosses BBB w/
inflammation
Renal excretion
Nucleic Acid Inhibitors
Metronidazole
(fragments bacterial DNA)
Rifampin
(inhibits RNA-polymerase)
(oral)
Ciprofloxacin
Fluoroquinolones
(synthetic ABX)
Inhibitors of Metabolism
Binds dihydrofolate reductase
Trimethoprim
(folic acid  tetrahydrofolate)
combo w/ Sulfamethoxazole
(Co-Trimaoxazole)
Sulfamethoxazole
Structural analog of PABA binds
dihydropteroate synthetase
(PABA  folic acid)
DOC Bacteroidies & Clostridium
endocarditis, brain abscesses
vaginitis (obligate anaerobes)
Anti-protozoal
Combo w/ Isoniazid for TB
Prophylaxis for meningitis
Leprosy
UTIs & prostatitis, Gram(-)
Pseudomonas w/ CF
Gonorrhea (NOT syphilis)
NOT Gram(+) or anaerobes
(some newer drugs)
Nausea, headache, dizziness
Peripheral neuropathy (longterm)
CI—EtOH (Disulfiram-like)
Hepatotoxicity
Induces microsomal enzymes
(oral anticoagulants, OCs,
estrogens, glucocorticoids)
Red-orange color body fluids
N/V, headache, dizziness,
nephrotoxic, phototoxic
CI—pregnancy, <18yo (arthropathy)
Inhibits P450
Seizures (potentiated displacement of
GABA w/ NSAIDs)
Crosses BBB & bone
Hepatic metabolism w/
renal excretion
Penetrates intracellularly
Crosses BBB
Hepatic metabolism w/ bile
secretion (prolongs t1/2)
Well-absorbed (NOT w/
antacids, Zn or Fe)
Renal & bile excretion
Synergism w/ -lactams
Accumulate in developing bone
UTI, prostatitis (FQs preferred),
PCNase-producing GU infections,
Legionella; otitis, bronchitis,
sinusitis, Pneumocystis
pneumonia
Folate deficiency, permanent
renal damage
AIDS (rash, neutropenia,
Stevens-Johnson syndrome,
pulmonary infiltrates)
20-50X more potent than
sulfonamides
Concentrates in acidic
prostatic & vaginal fluids
UTI (mono if untreated OR combo
w/ Trimethoprim if chronic)
Otitis, bronchitis, sinusitis,
Pneumocystis pneumonia
Trachoma, Nocardiosis
Nephrotoxic (crystalluria)
Kernicterus (displace bilirubin to
CNS), anemia, allergies
Potentiates oral anticoagulants,
anticonvulsants, hypoglycemics
NOT w/ Methenamine
(condenses to formaldehyde)
CI—newborns & pregnancy
Aminoglycosides
Streptomycin
TB (2nd-line), plague,
tularemia (combo w/ PCN)
Aerobic Gram(-) endocarditis
Serious Pseudomonas,
Klebsiella, Proteus, Serratia,
Enterococci
Severe refractory UTIs
Gentamicin
Nephrotoxic, ototoxic,
vestibular damage (irreversible)
Nephrotoxic, ototoxic,
vestibular damage (irreversible)
NMJ paralysis (high doses)
Renal excretion
Rapid resistance
Combo w/ -lactams
Renal excretion
PAE (once-a-day dosing)
NOT anaerobes (O2-dependent uptake)
Tobramycin
Tetracyclines
Tetracycline
(oral, q6h)
More effective Pseudomonas
Less Serratia & Enterococci
Same as above
Combo w/ -lactams
Renal excretion
Expensive
DOC Rickettsia, cholera,
Borrelia, Brucella
Discolors teeth (concentrates in
bone), microflora disturbance,
phototoxic, inhibits P450, direct
GI irritation
CI—pregnancy, <8yo, renal dz
Dairy, antacids, di- &
trivalent ions chelate
Renal excretion
Widespread resistance
Mycoplasma, Chlamydia, acne
Periodontal dz (subgingivally)
Hepatic excretion (for renal dz)
Doxycycline
Macrolides
Erythromycin
DOC Chlamydial GU
infections during pregnancy
Clarithromycin
(Biaxin)
Greater spectrum
Azithromycin
(Zithromax)
DOC Legionnaire’s, URI,
community-acquired pneumonia
GI upset (direct stimulates
motility), ototoxic (temporary)
Inhibits P450
CI—hepatic dysfxn
Less GI upset
Inhibits P450
Less GI upset
NOT interact w/ P450
Hepatic excretion
Alternative to PCN-G
Destroyed by gastric acid
(enteric coated)
Renal elimination
Improved acid lability
Longer t1/2
Once-a-day dosing
Shorter Rx duration
Same spectrum as PCN-G
Other Protein Synthesis Inhibitors
Clindamycin
DOC severe anaerobic
(Bacteroides & mixed)
Refractory bone infections
ALT prophylaxis dental Rx
Diarrhea (ABX-associated
colitis), hematopoietic effects
(IV dose), NMJ paralysis
Gray baby syndrome
ABX-associated colitis, allergies
(rash, fever, black tongue), bone
marrow aplasia, superinfections
Inhibits P450
Infusion site rxn, arthralgias,
myalgias
Inhibits P450 enzyme 3A4
(Ca2+-channel blockers &
Cyclosporine)
Crosses BBB
Static
Thrombocytopenia, GI
distress, headache, rash
NOT inhibit P450
Renal elimination (NO dosage
adjustment for renal dz)
Static (Enterococci & Staph)
Cidal (Strep)
Chloramphenicol
Binds 50S & inhibits
peptidyltranferase
(broad spectrum)
Salmonella typhi, refractory
meningitis, brain abscesses,
intraabdominal anaerobes;
Rickettsia, Brucella, Bacteroides
Streptogramins
Bind 2 sites on 50S &
prevent translocation
(slow IV drip)
Vancomycin-resistant E. faecium,
Prevents formation of 70S
w/ initiator f-met tRNA
Newest ABX class in 30y
Resistant S. aureus, E.
faecium, S. pneumoniae
NOT Gram(-) & anaerobes
Quinupristin/Dalfopristin
(Synercid)
Linezolid
(Zyvox)
MRSA, S. pyogenes
Serious Gram(+) cocci
Reserved
Hepatic conjugation &
excretion
Anti-virals
Zanamavir
(Relenza)
Amantidine
Rimantidine
Acyclovir
Valacyclovir
(Valtrex)
Gancyclovir
Vidarabine
Ribavarin
Zidovudine (AZT)
Nevirapine
Phosphonoformate
(Foscarnet)
Saquinavir
T-20
Neuraminidase inhibitor
(inhaled)
Guanosine analog
(selective inhibition of viral
DNA polymerase)
Valine ester of Acyclovir
(converted to Acyclovir)
Guanosine analog
Purine analog
(selective inhibition of viral
DNA polymerase &
ribonucleotide reductase)
Guanosine analog
(inhibits DNA polymerase &
5’-capping of viral mRNA)
Pyrimidine analog
(competitive inhibitor of RT)
Pyrophosphate analogs
(non-nucleoside RT
inhibitors)
Protease inhibitors
Influenza A
(w/in 48h onset of Sx)
Herpes
DOC genital herpes &
varicella zoster
CMV retinitis (w/ AIDS)
Imidazoles
(topical)
Triazoles
(oral or IV)
Tinea corporis, tinea pedis,
vaginal candidosis
DOC recurrent candidosis,
Cryptococcal & Coccidioidal
meningitis
Terbinafine
Non-azole inhibitor of
squalene epoxidase
(topical)
Nail infections & tinea
Amphotericin B
Binds ergosterol
(disrupts cell membrane)
Broad spectrum
(severe infections)
Nystatin
Binds ergosterol
(disrupts cell membrane)
Candidosis
Flucytosine
Pyrimidine analog
(converted to 5-FU)
Severe infections
Griseofulvin
Disrupts mitotic spindles
(oral)
Microsporum,
Epidermophyton,
Trichophyton
2° malignancies common long-term
MOPP
Lymphycytic leukemia
Carmustine
Nitrosoureas
Streptozocin
Nitrosoureas
Busufan
Alkyl sulfonates
(oral)
Platinum complexes
Chronic granulocytic
leukemia
Alkylating agents
Hodgkin’s dz (MOPP)
Cisplatin
Carboplatin
Procarbazine
Lymphomas, 1° brain tumors,
meningeal leukemias
Prone to resistance
Well-distributed (little CSF)
Renal clearance
15-30% oral bioavailability
Improved oral absorption
MORE toxic
Crosses BBB
Rapid renal clearance
Minimal cross-resistance w/
nucleoside inhibitors
Virions produced but NOT
infectious
Protease normally cleaves
polymerase & gag proteins
Adjunct to RTIs & PIs
HIV
HIV
Chemotherapy (alkylating agents)
Mechloroethamine
Nitrogen mustards
(IV)
Cyclophosphamide
Nitrogen mustards
(Cytoxan)
(IV or oral)
Anti-cholinergic Sx
Broad spectrum
(BOTH DNA & RNA viruses)
Severe LRI in kids (aerosol)
HIV
(HAART = 2RTIs + PI)
HIV
HIV fusion inhibitor
(bolus IV)
Anti-fungals
Miconazole
(Micatin, Monistat)
Fluconazole
(Diflucan)
“plug drugs”
RNA viruses (Influenza)
Local burning, itching,
irritation
N/V, rash
Inhibits P450
Candida hypersensitivity
syndrome
Allergic rxns,
blood dyscrasia (reversible)
CI—liver failure, renal doseadjustment
Fever, chills, allergic rxns,
renal dysfxn, hypokalemia,
hypotension, normocytic
anemia (reversible),
thrombophlebitis
Minimal SE (minimal
absorption)
Parenteral dose highly toxic
Myelosuppression,
N/V/D (release of 5-FU by GI
flora)
Allergic rxns, headache,
nausea, liver toxicity
Induces P450
<1% absorbed into blood
Myelosuppression, nausea,
reproductive toxicity
Hemorrhagic (less
thrombocytopenia)
Cystitis (Rx w/ MESNA)
LESS mutagenic (long-term)
Myelosuppression (delayed
BUT prolonged)
MOST reactive (t1/2 = 3min)
Renal & hepatic toxicity (less
bone marrow suppression)
Nephrotoxic
LEAST myelosuppressive
Crosses BBB
More expensive
Slower metabolism
Concentrates in skin & nail
beds
Resistance uncommon
Extremely bitter taste
Crosses BBB
Synergistic w/ Amphotericin B
(always in combo)
Concentrates in skin
Extensive metabolism
Hepatic metabolism
Crosses BBB
NOT cross-resistant w/
other drugs in class
Crosses BBB
Natural; NO cross-resistance
Synergistic (often combo)
Chemotherapy (DNA synthesis inhibitors)
Methotrexate (MTX)
Folic acid analogs
(oral)
5-Flurouracil
Cytarabine
Mercaptopurine
Pyrimidine analogs
(thymidylate synthetase
inhibitor)
Pyrimidine analogs
(improper DNA stacking
from 2’-OH)
Purine analogs
(competitive inhibitors of HGRT)
Thioguanine
Purine analogs
ALL, choriocarcinoma,
breast, head, neck, lung,
osteogenic sarcoma
Myelosuppression
Hepatic fibrosis (prolonged
use, Rx w/ Leucovorin)
Neurologic toxicity
AML
Leukemias,
immunosuppression,
anti-viral, gout
Same as above
NOT cross BBB
IV dose (erratic oral
absorption)
IV dose
Rxn w/ Allopurinol
Gradual myelosuppression,
hyperuricemia
Same as above (LESS toxic)
(competitive inhibitors of HGRT)
Hydroxyurea
Ribonucleotide reductase
inhibitors
Chemotherapy (natural agents)
Vincristine
Vinca alkaloids
(M-phase specific)
Vinblastine
Vinca alkaloids
(M-phase specific)
Paclitaxel
Anti-mitotic agent
(M-phase specific)
Doxorubicin
DNA topoisomerase
(Adriamycin)
inhibitors
Bleomycin
DNA fragmentation
(complex w/ Fe/O2)
Etoposide
Epipodophyllotoxins
Teniposide
(S-G2-phase specific)
L-Asparginase
Cervical, lung, head, neck
Hodgkin’s dz (MOPP),
leukemia, breast
Testicular, lymphomas
Leukemias, lymphomas,
breast, testicular
Breast, ovarian
Testicular
Synergistic w/ radiation
LESS myelosuppression,
alopecia, MORE neurotoxic
MORE myelosuppression,
alopecia, LESS neurotoxic
IV dose
Disrupts mitotic spindles
IV dose
Disrupts mitotic spindles
Hepatic metabolism
Myelosuppression
Cardiomyopathy (irreversible)
Minimal myelosuppression
Pulmonary fibrosis
Myelosuppression
Intercalation & ROS
generation
Combo Rx
Gastric distress, bleeding,
tinnitus, vertigo, deafness
CI—peptic ulcers, viral
infections in kids (Reye’s
syndrome)
Hepatic toxicity (esp. w/
EtOH)
Gastric distress
Dosage dependent
LESS gastric distress
Peripheral analgesic (at
lower doses than antiinflammatory action)
Enzyme
Chemotherapy (hormones)
Hydrocortisone
Corticosteroids
Prednisone
Leuprolide
GnRH antagonist
Stimulate topoisomerase to
cleave DNA
Synergism w/ Platins
Inhibits protein synthesis
by depleting Asp
Hematologic
(MOPP)
Prostate
(inhibits androgen synthesis)
Flutamide
(Eulexin)
Tamoxifen
NSAIDs
Aspirin
Acetaminophen
Indomethacin
Ibuprofen
Inhibits translocation of
androgen receptor
Competitive inhibitor of
estrogen receptors
Prostate
Suicide COX-1 inhibitor
Anti-inflammatory, analgesic,
anti-thrombotic
Lower risk of MI & colon CA
COX inhibitor
(central actions ONLY)
COX inhibitor
(acetic acids)
Analgesic, anti-pyretic
NOT anti-inflammatory
RA, osteoarthritis,
closure of ductus arteriosus
Acute gouty attacks
RA, osteoarthritis,
dysmenorrheal, gout,
ankylosing spondylitis
RA, osteoarthritis, migraine,
fever
Celecoxib
(Celebrex)
2nd-generation COX
inhibitor
(propionic acids)
2nd-generation COX
inhibitor
(propionic acids)
1st-generation selective
COX-2 inhibitor
Rofecoxib
(Vioxx)
1st-generation selective
COX-2 inhibitor
Naproxen
Breast
NOT an NSAID
NO platelet affects
LESS gastric distress,
except in kids
RA & osteoarthritis
Less gastric distress
RA & osteoarthritis,
acute pain
Thrombosis, renal toxicity
(similar to other NSAIDs)
FDA approved in 1998
Long-term effects unknown
t1/2 = 11h
Long-term effects unknown
t1/2 = 17h
Gout
Colchicine
Indomethacin
Naproxen
Oxaprozin
Allopurinol
Natural alkaloid
(inhibits tubulin
polymerization)
DOC gouty attacks
Prophylaxis for recurrent gout
NSAIDs
(inhibit PG-mediated
inflammation & uric crystal
phagocytosis)
Less specific for gouty
attacks
Competitive inhibitor of
xanthine oxidase
Lower serum uric acid levels
Reserved for severe gout
Anti-neoplastic
Probenecid
Uricosurics
(inhibits renal tubular
reabsorption)
Gout prophylaxis
(NOT for acute gout)
Sulfinpyrazone
Uricosurics
(inhibits renal tubular
reabsorption)
Gout prophylaxis
Benzbromarone
Uricosurics
(reversible inhibitor of urateanion exchange in PTs)
Migraines
Metoclopramide
(Reglan)
Anti-emetics
(muscarinic agonist &
D2-antagonist)
Migraine w/ N/V
Ergotamine
Dihydroergotamine
(DHE)
Non-selective 5-HT-agonists
Severe migraines
Sumatriptan
(Imitrex)
Triptans
(selective 5-HT1B/D-agonist)
Severe migraines
Butorphanol
Rescue med for severe
migraines
Migraine prophylaxis
Propranolol
-antagonists
Methysergide
5-HT-antagonists
(periphery)
5-HT-agonist (CNS)
Anti-depressants
Reserved for refractory
migraine prophylaxis
Anti-convulsants
Migraine prophylaxis
Amitriptyline
Valproate
Divalproex
Migraine prophylaxis
D/N/V, abdominal pain, hair
loss, bone marrow
suppression, peripheral
neuritis & myopathy
Less SE
Uric acid stones
GI distress, induce gout,
bone marrow suppression,
allergic rxns, cataracts
Uric acid stones,
induces gout (20%)
CI—peptic ulcers, inhibited by
ASA
Gastric distress & ulcers,
hepatic toxicity of
Acetaminophen
hematopoiesis
Well-tolerated
Inhibited by ASA &
Sulfinpyrazone
Extrapyramidal (Parkinson’slike) effects, drowsiness,
fatigue, restlessness,
insomnia
CI—kids
Nausea (combo w/ Reglan),
rebound HA, ergotism (longterm use)
CI—pregnancy (oxytocic)
High rebound HA,
coronary vasospasms
CI—CAD, PVD, uncontrolled
HTN, concurrent Ergots,
MAOIs, SSRIs
Fatigue, orthostatic
hypotension, impotence
CI—asthma, AV block, DM
Fibrosis (NOT use >6m)
Drowsiness, weight gain,
anti-cholinergic Sx
Weight gain, hair loss, tremor
CI—pregnancy (teratogenic)
Response Dx for gout
NOT analgesic, NOT alter
uric acid metabolism OR
excretion
NOT combo w/
Sulfinpyrazone OR
Probenecid (clearance)
Additive w/ Sulfinpyrazone
Small doses actually
tubular reabsorption
Used in Europe
Pro-drug; excreted in bile
Combo w/ caffeine
(enhance absorption)
Nasal spray (NOT oral
absorption)
Faster onset of action
Self-administered nasal
spray
Mechanism unknown (NOT
CNS penetration OR
cardiac selective)