Miscellaneous Quiz / anti-mycotic / anti-leprosy drugs

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Can you name the anti-mycotic / anti-leprosy drugs?

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Cycloserine class
Levofloxacin class
SE: hemolysis (esp in G6PD deficiency), erythema nodosum leprosum
Resistance via mutations in pncA gene which encodes ___________
Rifampin class
MOA: Cell wall synthesis inhibitor taken with pyridoxine. SE: peripheral neuropathy, CNS dysfunction - monitor serum concentration
Dapsone class
Excreted mainly through the liver/bile. SE: reddish color in urine, sweat, tears, and contact lenses; rashes; renal failure (nephritis); thrombocytopenia; cholestatic jaundice; hep
MOA: Inhibits mycobacterial arabinosyl transferase; bacteriostatic
Resistance via overexpression of the arabinosyl transferase
Contraindicated in HIV pts d/t high relapse rate with rifampin resistant strains
SE: hepatotoxicity, n/v, fever, hyperuricemia, polyarthralgia
Clarithromycin class
Tx of M. kansaii
Ciprofloxacin class
MOA: Inhibits bacterial RNA synthesis by binding to the b subunit of bacterial RNA polymerase; used against active TB and as an anti-leprosy agent
Contraindicated with certain meds (warfarin, digoxin, quinidine, cyclosporine, ketoconazole, phenytoin, anti-HIV agents, oral contraceptives) d/t strong inducer of P450
MOA: Injectable protein synthesis inhibitor for tx of drug-resistant TB
Ethionamide class
MOA: Aminoglycoside injectable drug which causes irreversible inhibition of 30S ribosome
Inhibits P450 enzymes; SE increased serum aminotransferase --> hepatotoxicity; peripheral neuropathy d/t pyridoxine deficiency; seizures (d/t decreased GABA)
Azithromycin class
MOA: Unknown; Active against mycobacteria in the acidic lysosomes; structurally related to nicotinamide
Rifabutin class
Amikacin class
M. leprae tx
Isoniazid class
MOA: inhibits bacterial folate synthesis by inhibiting dihydropteroate synthase
Resistance via point mutations of rpoB gene --> decreases binding of __________ to RNA polymerase
p-Aminosalicyclic Acid class
Tx of M. avium complex (MAC)
MOA: similar to INH, mycolic acid synthesis inhibitor. SE: GI upset, hepatitis, hemolysis
Ethambutol class
M. tuberculosis complex tx
SE: concentration and time dependent - ototoxicity and nephrotoxicity. Resistance via ribosomal binding site
Used for sulfone resistant leprosy or when pts are intolerant to sulfones. Useful for the tx of erythema nodosum leprosum
Strains of TB resistant to at least 2 of the main 1st line drugs (INH and RIF)
MOA: aminoglycoside - inhibits protein synthesis used in the tx of streptomycin-resistant TB
Used as a combo with rifampin and clofazimine recommended to prevent resistance
Streptomycin class
MOA: rifamycin derivative - bacterial RNA polymerase inhibitor; inhibits P450 enzymes
Strains of TB also resistant to the best 2nd line meds (fluoroquinolone and at least one of the three IV drugs - amikacin, kanamycin, or capreomycin)
SE: GI intolerance, dry skin, and discoloration
MOA: macrolide that binds to and inhibits 50S ribosomes
Tx of MB leprosy
Capeomycin class
MOA: phenazine dye that can be used as an alternative to dapsone. Inhibits bacterial DNA synthesis
Clofazimine class
MOA: Fluroquinolone - DNA synthesis inhibitor active against M. tuberculosis and atypical mycobacteria
Tx of PB leprosy
Resistance via mutations in the InhA gene and/or mutation or deletion of katG gene
Pyrazinamide class
Contraindicated in _____ allergy, hepatotoxicity, and acute liver dz. Also inhibits P450 mediated drug metabolism (caution for increased concentration of phenytoin, carbamazepine,
Rifapentine class
MOA: Inhibits mycolic acid synthesis by targeting InhA; penetrates into macrophages; needs activation; most active drug
MOA: similar to PABA - folate synthesis inhibitor
SE: neprotoxicity and ototoxicity
Accumulates in RF. SE: dose-related retrobulbar neuritis (loss of visual acuity and red-green color blindness)
Used in place of rifampin for tx of TB in HIV-infected pts who are receiving concurrent anti-retroviral tx

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