farm 2-5
Terms
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- drugs for TB
-
isoniazid
rifampin
pyrazinamide
ethambutol
others: streptomycin, amikacin, fluoroquinolones - Isoniazid
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Isonizaid
Class:
MOA: activated by catalase-peroxidase, inhibits long-chain fatty acid reductase involved in mycolic acid synthesis
Use: M. tuberculosis, M. kansasii, prophylaxis and rx
AE: hepatitis (age related, monitor hepatic enzymes).. peripheral neuritis (pyridoxine (B6 def), reversible.. seizures, hematologic toxicity, optic neuritis, hypersensitivity - rash/fever
Contra: avium-intracellulaire
Interaction: potentiate AE phenytoin - nystagmus/ataxia
Admin: oral - impaired with food - Ethambutol
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Ethambutol
Class: static
MOA: inhibit cell wall synthesis enzyme
Use: M. tuberculosis, M. avium-intracellulaire - when resistant to other drugs
AE: optic neuritis (dose dependent), impaired color vision (reversible)
Contra:
Interaction:
Admin: - Pyrazinamide
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Pyrazinamide
Class:
MOA: metab to pyrazinoic acid by susceptible mycobacteria - lowers pH to level that they can't grow
Use: shortens course of rx - used w/ rifampin, isoniazid (given 1st 2 months)
AE: hyperuricemia, gout, rash, joint ache, hepatitis, hematologic effects
Contra:
Interaction:
Admin: - Rifampin
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Rifampin
Class: derivative rifamycin
MOA: inhibit RNA synthesis, initiation step
Use: most mycobacteria, staph, legionella, never use alone, prophylaxis of meningo and H. influenza, leprosy
AE: hepatitis, hypersensitivity reactions, discoloration tears, saliva, urine, GI upset
Contra: hepatic failure - jaundice
Interaction: induce P450 enzymes, decrease t1/2 so need higher doses.. decreases levels of HIV drugs, warfarin, and others
Admin: wide distribution, enterohepatic cycling, biliary excretion - drugs for M. avium intracellulaire
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Rifabutin
Azithromycin
clarithromycin
ethambutol
ciprofloxacin - Dapsone
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Dapsone
Class:
MOA: inhibit folic acid synthesis, bacteriostatic folate antagonists
Use: long term leprosy rx
AE: G6PD - hemolytic anemia, methemoglobinemia, peripheral neuropathy, erythema nodosa
Contra:
Interaction:
Admin: - Clofazimine
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Clofazimine
Class: phenazine dye
MOA:
Use: leprosy - M. tuberculosis, M. leprae, M. avium-intracellulaire, enhances phagocytic activity of neutrophils/macrophages, rx erythema nodosum leprosum (type II hypersensitivity)
AE: accumulated by macrophages, concentrated in liver, lungs, lymph nodes, spleen, other tissues
Contra:
Interaction: highly lipophilic, 55% bioavailable, excreted unchanged in bile and kidneys
Admin: - Thalidomide
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Thalidomide
Class:
MOA: stimulate human T cell - CD8+
Use: orphan drug for TB, leprosy, erythema nodosum leprosum
AE: phocomelia (absence of limbs in pregnancy)
Contra:
Interaction:
Admin: - drugs for leprosy
-
sulfone,
rifampin,
clofazimine,
thalidomide - what do you use to rx tuberculoid leprosy
- dapsone + rifampin
- what do you use to rx lepromatous leprosy
-
dapsone + rifampin + clofazimine
consider thalidomide - what do you give to prevent TB in neonates/children < 5 years old who are exposed?
- isoniazid for 3 months
- what do you give for latent TB?
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isoniazid for 9 months
alt: rifampin for 4 months if isoniazid resistant