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39 Cards in this Set
- Front
- Back
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Structural congener of pyridoxine
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Isoniazid
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Metabolism of Isoniazid
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acetylation via the liver, and is under genetic control. Some pts may be fast or slow acetylators. The proportion of fast acetylators is higher among Asians(Native Americans included). These pts may require a higher dosage for equivalen therapeutic effects.
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Fast acetylators
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Asians and Native Americans
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MOA of isoniazid
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Inhibition of mycolic acids, characteristic components of mycobacterial cell walls.
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Prodrug that is activated via a catalase-peroxidase ezyme via the KatG gene
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isoniazid:
Resistance occurs through deletion of the KatG gene |
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Bacteriocidal for active tubercule bacilli, but is less effective against dormant organisms. What is used for latent tuberculosis?
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isoniazid
Rifampin |
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Single most important drug used in tuberculosis, and is used in most combo regimens
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Isoniazid
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Meningitis prophylaxis in exposed pts
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Rifampin
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Bacteriocidal TB drugs
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Isoniazid, Rifampin, Ethambutol
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Bacteriostatic TB drug
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Pyrazinamide
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Red urine discoloration and orange feces
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SE of Rifampin
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Neurotoxic effects include, peripheral neuritis, restlessness, muscle twitching and insomnia. Txmt?
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Isoniazid
pyrodoxine(B6) |
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Besides its neurotoxic effects, what other major side effect does INH carry?
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Hepatoxic:
Causes hepatitis, jaundice |
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Inhibits DNA-dependent RNA polymerase
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Rifampin:
Resistance is via changes in polymerase |
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May be used as the sole drug in txmt of latent tuberculosis
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Rifampin
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This drug, when used for M. leprae, delays the resistance to dapsone
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Rifampin
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Inhibits arabinosyl transferases involved in the synthesis of arabinogalactan, a component of mycobacterial cell walls
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Ethambutol
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SE include visual disturbances, such as decreased visual acuity, red-green color blindness, optic neuritis, and possible retinal damage.
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Ethambutol
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DOC for leprosy txmt
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Dapsone, rifampin, and clofazimin combo
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Drug whose bacteriostatic action requires conversion via pyrazinamidases
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Pyrazinamide
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Commonly causes light chain proteinuria and may impair antibody responses
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rifampin
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If given less than 2x weekly, this drug may cause a flu-like illness and anemia
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Rifampin
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About 40% of pts using this drug develop nongouty polyarthralgia and asymptomatic hyperuricemia
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Pyrazinamide
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Use of this TB drug is important factor in the success of "short course" txmt
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Pyrazinamide
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Used principally in drug combos for the txmt of life-threatening TB disease, including meningitis, miliary dissemination, and severe organ TB
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streptomycin
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Most active drug against M. leprae. MOA?
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dapsone:
Inhibitor of folic acid synthesis |
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SE include GI irritation and skin discoloration ranging from red-brown to black
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clofazimine:
used to combo with dapsone and rifampin for leprosy |
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Initial txmt regimen for non-resistant TB strains
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INH, rifampin, and pyrazinamide
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Repository form of rifampin that provides inhibitory plasma concentrations for several months
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Acedapsone
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Txmt regimen for INH resistant TB strains
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RIPE:
instead of ethambutol, may also give streptomycin |
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Txmt for M avium complex (MAC) in AIDS pts
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clarithromycin or azithromycin with or w/o rifubatin for prophylaxis in pts with CD counts less than 50.
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SE include loss of equilibrium and auditory damage
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Amikacin:
Common among aminoglycosides. Use is for TB resistant to streptomycin or multi-drug resistant TB strains |
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Indicated for txmt of streptomycin-resistant TB or multi-drug resistant mycobacterial strains
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Amikacin
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Txmt regimen for TB resistant to both INH and Rifampin
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RIPE plus streptomycin and a floroquinolone (Ciprofloxacin or ofloxacin).
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Once weekly administration of what drug has prophylactic activity against bacteremia caused by M avium complex in AIDS pts
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Azithromycin
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Mechanism of high-level INH resistance of M tuberculosis
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Reduced expression of the katG gene
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Used in prophylactic txmt of TB in those who have close contact (siblings/parents/partners) with TB positive persons
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INH
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Drug that increases CP450 metabolism, and may increase the rate of elimination of anticoags, keticonazole, methodone, and steroids
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Rifampin
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Drug that decreases the effectiveness of oral contraceptives
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Rifampin:
Via CYP450 activation |
