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PHARMACOLOGY > Antimycobacterial agents > Flashcards

Antimycobacterial agents Flashcards

1
Q

non-tuberculous mycpbacteria

A

M. avium

M. intracellulare

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2
Q

primary drugs used in TB

A

Isoniazid
Rifampicin
Pyrazinamide
Ethambutol

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3
Q

most active TB drugs

A

Isoniazid and rifampicin

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4
Q

Isoniazid and rifampicin

Initial intensive phase of tx is recommended for the first __ months

A

2

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5
Q

how many active agents should be used to treat active TB to prevent emergence of resistance during therapy

A

at least 2

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6
Q

primary tx tb

A

2 months of HRZE and

4 months of HR

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7
Q

maximum dose of H

A

300mg/day

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8
Q

Max dose of rifampicin

A

600mg/day

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9
Q

category 1

for pulmonary and extrapulmonary meninges, bones or joints

A

2 HRZE

4 HR

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10
Q

Category 1a

for extrapulmonary TB of meninges, bones, and joints

A

2 HRZE
10 HR

max 1 yr

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11
Q

Category 2

for retx of confirmed rifampicin-sensitive pulmonary and extra-PTB except meninges, bones or joints

A

2HRZES
1HRE
5HRE

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12
Q

for retreatment of confirmed rifampicin-sensitive extra-PTB of meninges, bones, or joints

A

2HRZES
1HRE
9HRE

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13
Q

most active drug for the tx of TB caused by susceptible strains

A

isoniazid

sim struc: pyridoxine

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14
Q

isoniazid inhibits most tubercle bacilli at a concentration of __

A

0.2 mcg/mL

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15
Q

isoniazid MOA

A

inh synth of mycolic acids

bactericidal

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16
Q

Isoniazid resistance

A

overexpression of inhA
mutation or deletion of the katG gene
overexpression of ahpC
mutations in kasA

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17
Q

isoniazid is readily absorbed from GIT optimally on an _____

A

empty stomach

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18
Q

rapid acetylators (inh)

A

<1-hour half life

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19
Q

slow acetylators (INH)

A

around 3 hours

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20
Q

sleeping tb

A

latent tb

diagnosis: PPD or interferon gamma release assay or positive IgA test for TB.

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21
Q

dosage for latent TB

A

INH 300mg/day or 900mg twice weekly (9 months; ph: 6 months)

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22
Q

isoniazid immunologic rxn

A

fever and skin rashes

SLE

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23
Q

Direct toxicity

A

hepatitis (most common major toxic effect)

24
Q

10-20% of patients given doses are greater than 5mg/kg/d, but it is frequently seen with the standard 300mg adult dose (INH)

A

peripheral neuropathy

25
Q

neuropathy is reversed by

A

pyridoxine b6 10mg/d (25-50mg/day)

26
Q

antibiotic produced by Amycolaptosis rifamycinica

A

Rifampin (S. mediterranei)

27
Q

rifampicin is active in vitro against

A

gram +
some gram - (neisseria and haemophilus)
mycobacteria
Chlamydiae

28
Q

Rifampin MOA

A

binds to the B subunit of bacterial DNA-dependent RNA polymerase and thereby inhibits RNA synthesis

29
Q

Rifampin resistance

A

mutations in rpoB

30
Q

rifampin is excreted mainly through the____

A

liver and bile

31
Q

Latent tb

-single agent alternative to isoniazid dosage is ______

A

600mg/day for 4 months

32
Q

dosage meningococcal carriage elimination

A

600mg BID x 2 days

33
Q

H. influenzae type b disease prophylaxis

A

600mg OD x 4 days

34
Q

AE of rifampin

A

harmless orange color urine, sweat and tears
Rashes, thrombocytopenia, and nephritis
cholestatic jaundice and occasionally hepatitis

35
Q

synthetic water-soluble, heat-stable compound

A

Ethambutol

36
Q

the dextro isomer of the structure is dispensed as

A

dihydrochloride salt

37
Q

ethambutol MOA

A

inh mycobacterial arabinosyl transferases, which are encoded by the embCAB operon

38
Q

ethambutol resistance

A

Due to the mutations resulting in overexpression of emb gene products or within the embB structural gene

39
Q

accumulates in renal failure, the dose should be reduced to 3x weekly if creatinine clearance is less than 30mL/min

A

Ethambutol

40
Q

most common serious AE of ethambutol

A

retrobulbar neuritis (x visual acuity and red-green color blindness)

41
Q

relative of nicotinamide, and it is only used for treatment of tuberculosis

A

Pyrazinamide

42
Q

active form of pyrazinamide

A

Pyrazinoic acid

43
Q

pyrazinamide resistance

A

due to impaired uptake of pyrazinamide or mutations in pncA that impair conversion of PZA to its active form

44
Q

important front-line drug used in conjunction with isoniazid and rifampin in short-course regimens as a “sterilizing agent” active against residual intracellular organisms that may cause relapse

A

Pyrazinamide

45
Q

AE pyrazinamide

A 
Hepatotoxicity
Hyperuricemia
Nausea
Vomiting
Drug fever
Photosensitivity
46
Q

2nd line TB

A

streptomycin

47
Q

streptomycin resistance

A

point mutation rpsL (s12) gene or rrs gene (16s)

48
Q

streptomycin AE

A

Ototoxic

Nephrotoxicity

49
Q

MAC

A

M avium

M intracellulare

50
Q

recommended for initial therapy of lepromatous leprosy

A

dapsone

51
Q

dapsone may also be used to prevent and treat ______ in aids patients

A

Pneumocystis jirovecii pneumonia

52
Q

AE dapsone

A

Hemolysis
Methemoglobinemia
Erythema nodosum leprosum

53
Q

highly effective drug in leprosy

A

rifampin 600mg daily

54
Q

phenazine dye used in the tx of multibacillary leprosy

A

clofazimine

55
Q

common dosage of clofamizine

A

100-200mg/day orally

56
Q

most prominent adverse effect of clofamizine is

A

discoloration of the skin and conjunctivae

PHARMACOLOGY (13 decks)

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