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SGU Pharmacology
AntiMYCO-Bacterials
20
Medical
Professional
08/31/2010

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Term
What are the 5 main Rxs used to Tx TB?
Definition
Isoniazid (INH), Rifampin (Apart of Rifamycins: Rifabutin, Rifapentine), Pyrazinamide, Ethanbutol, Streptomycin
Term
What is the first line Tx for TB?
Definition
Rifampin w/ combo
Term
Isoniazid (INH)
Definition
Narrow spec., CNS (A/Es), Inhibits P450, Peripheral neuritis (Tx with Vit. B12), ProRx -> Rx via KatG and acts on AcpM & KasA, is both static and cidal, is broken down by N-acetylation, dont take w/ food (esp carbs or aluminum coated antacids)
Term
Rifampin
Definition
Inhibits RNA synthesis via binding to beta-subunit, broad spec., -cidal, Taken orally, enters CNS, leaves in bile and urine, sole Rx in Tx INH intolerant pts, prophylaxsis 4 meningitis pts, A/Es: light chain proteinuria, flu-like syndrome, harmless orange fluids
Term
Rifabutin
Definition
Used in HIV pts, A/Es: uveitis, skin hyperpigmentation, neutropenia
Term
Rifapentine
Definition
Long T 1/2
Term
Pyrazinamide
Definition
Is a pro-> pyrazinoic acid (broken down by pyrazinamidase) via hydrolase, -cidal, given in combo, MAO?, oral, CNS, A/Es: asym hyperuremia, nongouty polyarthralgia, photo sens, hepatotoxicity, myalgia, GI irritation, porphyria, avoid in preg
Term
Ethanbutol
Definition
Narrow spec., CNS, -static, unchanged & in urine, gout, can combo, inhibits cell wall syn., dose dependent eye probs
Term
Streptomycin
Definition
Used for Rx resistant strains that cause millilary desemmination, A/Es: oto & nephro -toxicity, vertigo, permenent hearing loss
Term
Amikacin
Definition
Used for streptomycin- or multi-Rx-resistant strains, used in combo
Term
Ciprofloxacin
Definition
Used when resistance is to 1st line, used in combo
Term
Ethionamide
Definition
Congener of INH (no cross resistance), severe GI irritation + adverse neurologic effects
Term
How is latent TB Tx?
Definition
INH for 6-9 mos, Rifampin 4 mos
Term
What is the standard regimen for empirical Tx of pulmonary TB?
Definition
3 Rxs (INH, rifampin, pyrazinamide), if pt is susceptible and HIV -ve then pyrazineamide can be discontinued after 2mos and the other 2 continued for 4 mos
Term
What is the Alternative regimens?
Definition
If fully susceptible then: INH+rifampin (9 mo); INH+ethambutol (18 mo); intermittent (2 or 3 X wkly) high does 4 Rx regimens
Term
What if there is resistance (>4%)?
Definition
Initial Rx regimen shud include ethambutol or streptomycin;
INH resistance strains shud get Rifampin+pyrazinamide+ethambutol or streptomycin (6 mo);
Multi-Rx resistant strains: 3 or more Rxs for 18 mos until culture negative then continue for yet another 12 mos
Term
Leprosy (aka Hansen's Dz) causes?
Definition
Granulomatous Dz of peripheral nerves + mucosa of URT
Term
What is the WHO Tx for Leprosy?
Definition
Dapsone
Clofazimine
Rifampin
Term
Dapsone
Definition
Structurally related to sulfonamides, thus inhibit folate syn via dihydropteroate synthetase I, -static, Tx of PJP, distributed to high levels in skin (and cause its inflammatory -> erythema nodosum leprosum, Tx w/ corticosteroids or thalidomide), hepatic acetylation (& into bile?), urine, ACEdapsone is the repositiry form, forms alot of oxidising agents thus hemolysis (esp in G6PD def pts), GI irritation, methemoglobinemia, peripheral neuropathy
Term
Clofazimine
Definition
Phenazine dye, binds to DNA + inhibits replication, may produce cytotoxic free radicals, bactericidal to MAC aswell, oral w/ no CNS, A/Es: red-brown skin (w/out erythema nodosum as has anti-inflammatory axn), eosinophilic enteritis
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