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First Line antimycobaterials |
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Definition
Isoniazid
Rifampacin
Pyrinizinamide
Ethambutol |
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Inhibits mycolic acid synthesis |
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p450 inhibitor metabolized in liver various rates of acetylation |
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All tissues- w/ high intracellular concentrations |
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Hepatitis B6 defficiency- peripheral neuropathy, give pyridoxine Inhibition of Phenytoin metabolism- ataxma |
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binds to beta subunit of Mb RNA pol --> inhibits transcription |
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Reddish/ brown Urine Hepatitis Abdominal discomfort fever skin eruptions |
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inc elimination of other drugs esp Birth control and HIV proteases- monitor the level |
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doesn't affect CYP450 so use in AIDs patients so don't inc elimination of PI |
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Pyrizinamidase converts it to pyrizinmatoic acid --> unknown MOA |
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well distributed in tissues but concentrates in cells |
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active in acidic environments ie lysozomes inside of macropahges |
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Hyperuricemia- Pyrazinoic acid inhibits renal secretion of Uric acid --> Gout monitor SGOT (liver enzyme) and uric acid Heptatitis Arthralgia, fever, skin rashes |
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inhibits arabinosyl tranferase --> inhibits bac wall synthesis Bacerial static |
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most tissues, including CNS --> used for TB meningitis |
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Retrobulbar neuritis- Optic neuritis w/o swelling of optic disc. R/G color blindness- Monthly tests for visual acuity Peripheral neuritis HA Rash |
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occationally used in conjunction with first line tx |
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distributes to tissues, but doens't concentrate in cells |
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Excreted unchanged in urine, no liver metabolism |
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Ototoxicity- vistibular and auditory renal injury hypersensitivity |
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binds 30s subunit of bac ribosome- prevents initiation complex formation. Inhibits translation |
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Paraminosalicylic Acid- PSA- MOA |
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Definition
competes with PABA for Mb dihyropterase synthase, interferes with folic acid and thus DNA synthesis bacteriastatic |
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oral well absorbed always with food |
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GI- nausea, abdominal pain, diarrhea, nausea if not given w/ food Goiter, hypothyroidism Anemia |
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Inhibits mycolic acid synthesis |
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Ethionamide- distribution |
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Definition
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Liver metabolizes it to ethionamide sulphoxide |
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Definition
ethionamide sulphoxide- kidney excretion |
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pyridoxine deficiency GI- N/D/ pain hepatotoxicity allergic reactions |
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widely concentrates in reticuloendothelil system and is slowly let out, partially accounts for long half life |
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metabolized to several inactive metabolites and excreted in the feces and urine |
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Drug accumulation in tissues turns- skin, urine, and feces a red brown color, so people with leprosy don't like it b/c it marks them GI disturbances |
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Cycloserine/ kanamycin- MOA |
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inhibits cell wall synthesis |
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Cycloserine/ Kanmycin- use |
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rarely used due to poor efficacy and adverse eventes |
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Ciprofloxacin Moxifloxacin Levofloxacin |
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Fluroquinolones- disrtibution |
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Low intracellular concentration |
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inhibits folate synthesis |
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excreted into bile, reabsorbed, excreted in urine |
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well tolerated Fever, GI, rash, exoliative dermatitis |
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Dapsone Contratindications |
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Definition
Don't give to someone with sulfa drug allergies |
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Definition
Streptomyocin Paramino Salacylic Acid Ethionamide Clofazamine Cyloserine/ Kanomycin Fluroquinolones, capreomycin |
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Rifampin& Dapsone for 6 mnths Single lesion- Rifampin, ofloxacin, Minocycline |
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Definition
Rifampin, Dapsone, Clofazamine- 12 mos |
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Azithromycin Ethambutol Rifabutin Fluroquinolones |
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