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USMLE Micro: Pharm
Terms in this set (55)
Antiviral. Inhibits DNA synthesis in HSV, VZV, and EBV. Activated by viral thymidine kinase (TK- strains are resistant). Tox: Nephrotoxicity (crystalluria). Famciclovir, penciclovir, and valacyclovir are similar but with longer half-lives.
Antiviral. Blocks viral penetration/ uncoating (M2 protein). Also causes the release of dopamine from intact nerve terminals. Uses: Prophylaxis and treatment for Influenza A. Parkinson's Dz. Tox: Ataxia, Dizziness, slurred speech.
Antifungal: Polyene drug of choice for some serious systemic mycoses; binds to ergosterol to disrupt fungal cell membrane permeability. Tox: Nephrotoxicity, chills and fever, hypotension, (dose limiting; less with liposomal forms).
Penicillin: wider spectrum than penicillin G, susceptible to penicillinases unless used with sulbactam. Activity similar to that of penicillin G, plus E coli, H influenzae, P mirabilis,
Shigella. Synergy with aminoglycosides versus Enterococcus and Listeria. Tox: penicillin allergy; more adverse effects on GI
tract than other penicillins; maculopapular skin rash, pseudomembernous colitis.
Macrolide. Block translocation (50s). Similar to erythromycin but greater activity against H influenza, chlamydiae, and streptococci; long half-life because of tissue accumulation; renal elimination. Tox: GI distress but no inhibition of drug metabolism. Clarithromyin is similar but has a shorter half-life, inhibits drug metabolism, and is contraindicated in pregnancy.
Monobactam resistant to Beta Lactamases. Inhibits cell wall synthesis. Synergistic with aminoglycosides. Uses: Gram negative rods only. Penicillin allergic patients. Tox: Few
Antifungal. Inhibits cell wall synthesis by inhibiting synthesis of Beta Glucan. Uses: INVASIVE ASPERGILLOSIS. Tox: GI upset, flushing
First-generation cephalosporin. Bactericidal beta lactam inhibitor of cell wall synthesis. Active against gram positive cocci, Proteus, E coli, K pneumoniae, but does not enter CSF. Tox: potential allergy; partial cross-reactivity with penicillins. PEcK
Fourth-generation cephalosporin. Increased activity against Pseudomonas and gram-positive organisms.
Cefoxitin, Cefaclor, Cefuroxime, Cefotetan
Second-generation cephalosporin: active against a wide spectrum of gram-negative bacteria, including anaerobes (B fragilis). H. Flu, Enterobacter, Neisseria. Does not enter the CNS. HEN PEcK
Ceftriaxone, Cefotaxime, Ceftrazidime (Pseudomonas)
Third-generation cephalosporin: active against many bacteria, including pneumococci, gonococci (a drug of choice), and gramnegative rods. Enters the CNS and is used in bacterial meningitis.
Broad-spectrum agent; inhibits protein synthesis (50S); Uses restricted to backup drug for bacterial MENINGITIS, infections due to anaerobes, Salmonella. Tox: Aplastic anemia, reversible
myelosuppression, gray baby syndrome.
Antimalarial. Used for treatment and as a chemosuppressant where P falciparum is susceptible. Blocks plasmodium heme polymerase, leading to accumulation of toxic hemeoglobin breakdown products. Tox: GI distress, skin rash at low doses; peripheral neuropathy, auditory and visual impairment, quinidine-like cardiotoxicity at high doses.
Ciprofloxacin, Norfloxacin, etc.
Second-generation fluoroquinolone antibiotic: bactericidal inhibitor of topoisomerases; Gram negative rods of urinary and GI tracts (Neisseria, some gram + orgs). Tox: CNS dysfunction, GI distress collagen dysfunction (avoid in children and pregnant women). Interactions: inhibits metabolism of caffeine, theophylline, warfarin.
Clavulanic acid, Sulbactam, Tazobactam (CAST)
Beta Lactamase inhibitors. Often added to penicillin antibiotics to protect the antibiotic from destruction by Penicillinase.
Lincosamide. Bacteriostatic inhibitor of protein synthesis (50S); ANAEROBIC INFECTIONS. Active against gram-positive cocci, B fragilis. Tox: GI distress, pseudomembranous colitis.
Efavirenz, Declaviridine, Nevirapine
Antiviral. Nonnucleoside reverse transcriptase inhibitor (NNRTI): used in
combination regimens for HIV. Tox: skin rash, CNS effects.
Antiviral. Bind viral gp41 subunit. Inhibit conformational change required for fusion with CD4 cells, blocking entry and replication. Used in patients with persistent viral replication despite antiretroviral therapy. Tox: Hypersensitivity.
Macrolide antibiotic: bacteriostatic inhibitor of protein synthesis (50S); Uses: ATYPICAL PNEUMONIAS. Includes gram-positive cocci and bacilli, M pneumoniae, Legionella pneumophila, C trachomatis. Tox: cholestatic jaundice (avoid estolate in pregnancy), inhibits liver drug-metabolizing enzymes.
Imidazole antifungal: inhibits ergosterol synthesis. Used in esophageal and vaginal CANDIDIASIS, in coccidioidomycosis,
and in the prophylaxis and treatment of CRYPTOCOCCAL meningitis. Adverse effects similar to those of ketoconazole but less severe.
Antifungal. Inhibit DNA synthesis by conversion to 5-fluorouracil. Uses: Systemic fungal infections in combination with Amphotericin B. Tox: N/V, Diarrhea, Myelosupression
Antiviral. Viral DNA polymerase inhibitor that binds to the pyrophosphate-binding site of the enzyme. Does not require activation by viral kinase. Uses: CMV retinitis in immunocomp pts. when gancyclovir fails. Tox: Nephrotoxicity.
Antiviral. Inhibits DNA synthesis. Effective against herpes viruses CMV and HSV; for CMV requires bioactivation via viral phosphotransferase. Tox:myelosuppression, nephrotoxicity, neurotoxicity.
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
Aminoglycosides (Bactericidal). Inhibit formation of the initiation complex and cause misreading of mRNA. Ineffective against anaerobes because need O2 for uptake. Uses: Gram-negative rods. Tox: Ototoxicity, Nephrotoxicity (TN), Teratogens.
Antifungal. Interferes with microtubule function; disrupts mitosis. Deposits in keratin-containing tissues. Uses: Oral treatment of superficial infections. Inhibits growth of DERMATOPHYTES. Tox: Teratogenic, carcinogenic, CYP450 INDUCER.
Idinavir, Amprenavir, Nelfinavir, Ritonavir, Saquinavir
Antiviral: HIV protease (pol) inhibitor (PI) used as a component of combination regimens in AIDS. Tox: Anemia, nephrolithiasis, metabolic disorders, inhibits P450 drug metabolism. Other PIs: amprenavir, nelfinavir, ritonavir (major P450 inhibitor), and saquinavir.
Imipenem/ cilastatin, Meropenem
Carbapenem antibiotic: active against many aerobic and anaerobic bacteria; bactericidal inhibitor of cell wall synthesis. Used with Cilastatin to decrease drug inactivation. Tox: allergy (partial crossreactivity with penicillins), seizures. Meropenem does not require cilastatin and is less likely to cause seizures.
Antiviral. Glycoproteins synthesized by virus-infected cells block replication of both RNA and DNA viruses. INF-a (used in
hepatitis B and C and in cancer), INF-b (used in multiple sclerosis), INF-g (used in NADPH oxidase deficiency). Tox: Neutropenia
Antimycobacterial: Decreases synthesis of mycolic acids. Primary drug in combination regimens for tuberculosis; used as sole agent in prophylaxis. Metabolic clearance via N-acetyltransferases (genetic variability). Tox: Hepatotoxicity (age dependent), peripheral neuropathy (reversed by pyridoxine-B6), hemolysis (in G6PD deficiency). Also Ethambutol (Decreased carbohydrate polymerization of bac. cell wall. Tox - Optic Neuritis).
Anthelmintic. Drug of choice for onchocerciasis and threadworm
infections. Intensifies GABA-mediated neurotransmission in nematodes, but no access to CNS in humans. Tox: in
onchocerciasis causes headache, fever, hypotension, joint pain.
Antifungal azole: inhibits the synthesis of ergosterol. Used for C albicans, dermatophytosis, and non-life-threatening systemic mycoses. Tox: hepatic dysfunction, inhibits steroid synthesis and CYP450. Gynecomastia.
Mebendazole, Albendazole, Thiabendazole
Anthelmintic. Important drug for pinworm and whipworm infections. Inhibits microtubule synthesis and glucose uptake in
nematodes. Tox: GI distress, caution in pregnancy.
Antimalarial. Unknown mechanism of action. Used for prophylaxis against and treatment of chloroquine-resistant malaria. Tox: GI distress, dizziness, seizures in overdose,
Antiprotozoal. Inhibigts sulfyhdryl groups in parasite enzymes. CNS involvment. Used in AFRICAN SLEEPING SICKNESS.
Methicillin, Nafcillin, Dicloxacillin
Penicillinase-resistant penicillin: used for suspected or known staphylococcal infections; not active against MRSA. Tox:
Antiprotozoal antibiotic: drug of choice in extraluminal amebiasis and trichomoniasis; effective against bacterial anaerobes, including B fragilis and in antibiotic-induced colitis resulting from C difficile. Tox: Peripheral neuropathy, GI distress, ethanol intolerance, mutagenic potential.
Antiprotozoal. Forms intracellular oxygen radicals, which are toxic to the organism. Used against TRYPANOSOMA CRUZI.
Mech. similar to Amphotericin B. Topical form because too toxic for systemic use. Use: Oral candidiasis and topical for diaper rash and vaginal candidasis.
Penicillin G (IV form)
PCN V (oral form)
MOA: bind PBP, block transpeptidase cross-linking of cell wall, activate autolytic enzymes.
Use: Bactericidial for gram + cocci, gram + rods, gram - cocci and spirochetes. Not PCNase resistant.
Tox: Hypersensitivity rxn, hemolytic anemia.
Piperacillin, Ticarcillin, Carbenicillin
Extended-spectrum penicillin active against selected gramnegative bacteria, including Pseudomonas aeruginosa (synergistic with aminoglycosides). Susceptible to
penicillinases unless used with tazobactam. Tox: penicillin allergy.
Antiprotozoal. Antifol inhibiting DHFR (P. FALCIPARUM) and synergistic, via sequential blockade, with sulfadiazine against Toxoplasma gondiioplasma gondii. Folinic acid is needed to offset hematologic toxicity.
Polymyxin B, Colistimethate
Bind to cell membranes of bacteria and disrupt their osmotic properties. Polymixins are cationic, basic proteins that act like detergents. Uses: Resistant gram negative infections. Tox: Neurotoxicity, ARTN
Anthelmintic: important drug for trematode (fluke) and cestode (tapeworm) infections. Increases membrane permeability to
Ca2+ causing muscle contraction followed by paralysis. Tox: headache, dizziness, GI distress, fever; potential abortifacient.
Antihelmintic.Stimulates nicatinic receptors at neuromuscular junctions. Contraction occurs, followed by depolarization-induced paralysis. Used for ASCARIS and hookworm infection.
Antimalarial. Blood schizonticide; no effect on liver stages. Interferes with nucleic acid metabolism in plasmodium. Isomer
of quinidine, same toxicity.
Antiviral. Inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase. Uses: RSV, Chronic Hep C. Tox: Hemolytic anemia. Severe teratogen.
Antimicrobial: Inhibitor of DNA-dependent RNA polymerase used in drug regimens for tuberculosis and the meningococcal
prophylaxis. Tox: Hepatic dysfunction, flu-like syndrome with intermittent dosing, CYP450 Inducer. Rifabutin similar but associated with fewer drug interactions.
Antiprotozoal. Inhibits glycolysis at PFK reaction. Used against LESHMANIA DONOVANI.
Anitprotozoal. Inhibits enzymes involved in energy metabolism. No CNS involvement. Used in AFRICAN SLEEPING SICKNESS.
Antifungal. Inhibits the fungal enzyme squalene epoxidase. Uses: Treat dermatophytoses (especially ONCHOMYCOSIS)
Tetracycline, Doxycycline, Demeclocycline, Minocycline
Tetracyclines. Bacteriostatic inhibitors of
protein synthesis (30S). Used for mycoplasmal, chlamydial, rickettsial infections, chronic bronchitis, acne, cholera; a backup drug in syphilis. Tox: GI upset and superinfections, Fanconi's syndrome, photosensitivity, dental enamel dysplasia.
Trimethoprim (TMP) - Sulfamethoxazole (SMX)
Antimicrobial drug combination: causes synergistic sequential blockade of folic acid synthesis. Active against many gram negative bacteria. Uses: UTIs, Shigella, Salmonella, P. Jiroveci. Tox: Mainly due to sulfonamide; includes hypersensitivity, myelotoxicity, kernicterus, and drug interactions caused by competition for plasma protein binding, also Megaloblastic anemia.
Inhibits cell wall mucopeptide formation by binding D-ala D-ala portion of cell wall precursor. Bactericidal. Drug of choice for MRSA and effective in antibiotic-induced colitis. Dose reduction required in renal impairment (or hemodialysis). Tox: Ototoxicity, hypersensitivity, renal dysfunction (rare).
Antiviral. Neuraminidase inhibitor: inhibits release and facilitates clumping of mature virions of influenza A and B and decreases
their infectivity. Shortens duration of flu symptoms.
Zidovudine, Abacavir, Didanosine (ddI), Lamivudine (3TC), Stavudine (d4T), and Zalcitabine (ddC).
Antiviral. NRTIs used in combinations for HIV infections and in prophylaxis for needlesticks and vertical transmission. Tox: severe myelosuppression.
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