Miscellaneous Quiz / anti-mycotic / anti-leprosy drugs

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

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

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