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Pharm main > antimycobacterials > Flashcards

antimycobacterials Flashcards

1
Q

First Line antimycobaterials

A

Isoniazid, Rifampacin, Pyrinizinamide, Ethambutol

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2
Q

INH- MOA

A

Inhibits mycolic acid synthesis

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3
Q

INH activation

A

KatG- only in Mb

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4
Q

INH & liver enzymes

A

p450 inhibitor, metabolized in liver, various rates of acetylation

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5
Q

INH distribution

A

All tissues- w/ high intracellular concentrations

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6
Q

INH MOR

A

katG mutation

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7
Q

INH- AE

A

Hepatitis, B6 deficiency- peripheral neuropathy, give pyridoxine, Inhibition of Phenytoin metabolism- ataxia

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8
Q

INH method of admin

A

Oral

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9
Q

INH Tmax

A

1-2 hr

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10
Q

INH 1/2 life

A

.75-5h

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11
Q

INH excretion

A

Kidney

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12
Q

Rifampin- MOA

A

binds to beta subunit of Mb RNA pol –> inhibits transcription

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13
Q

RIF method of admin

A

Oral- well absorbed

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14
Q

RIF T1/2

A

2.5-5hr

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15
Q

RIF- distribution

A

all tissues

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16
Q

RIF & liver enzymes

A

CYP450 inducer

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17
Q

RIF excretion

A

mostly feces, some urine

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18
Q

RIF AE

A

Reddish/ brown Urine, Hepatitis, Abdominal discomfort, fever, skin eruptions

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19
Q

RIF drug interactions

A

inc elimination of other drugs esp Birth control and HIV proteases- monitor the level

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20
Q

RIfabutin

A

doesn’t affect CYP450 so use in AIDs patients so don’t inc elimination of PI

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21
Q

Rifampimicin

A

Used for leprosy

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22
Q

Pyrizinamide (PZA)- MOA

A

Pyrizinamidase converts it to pyrizinmatoic acid –> unknown MOA

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23
Q

PZA method of admin

A

Oral

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24
Q

PZA 1/2 life

A

9 hr

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25
Q

PZA- distribution

A

well distributed in tissues but concentrates in cells

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26
Q

PZA activity

A

active in acidic environments ie lysozomes inside of macropahges

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27
Q

PZA metabolism

A

Liver

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28
Q

PZA excretion

A

Kidney

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29
Q

PZA AE

A

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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30
Q

Ethambutol MOA

A

inhibits arabinosyl tranferase –> inhibits bac wall synthesis. Bacerial static

31
Q

Ethambutol admin

A

Oral

32
Q

Ethambutol 1/2 life

A

10 -15 h

33
Q

Ethambutol distribution

A

most tissues, including CNS –> used for TB meningitis

34
Q

Ethambutol excretion

A

Unchanged in urine

35
Q

Ethambutol AE

A

Retrobulbar neuritis- Optic neuritis w/o swelling of optic disc. R/G color blindness- Monthly tests for visual acuity. Peripheral neuritis, HA, Rash

36
Q

Streptomycin (SM)- use

A

occasionally used in conjunction with first line tax

37
Q

SM- admin

A

IV/ IM

38
Q

SM- tissue distribution

A

distributes to tissues, but doesn’t concentrate in cells

39
Q

SM- excretion

A

Excreted unchanged in urine, no liver metabolism

40
Q

SM- AE

A

Ototoxicity- vistibular and auditory, renal injury, hypersensitivity

41
Q

SM- MOA

A

binds 30s subunit of bac ribosome- prevents initiation complex formation. Inhibits translation

42
Q

Paraminosalicylic Acid- PSA- MOA

A

competes with PABA for Mb dihyropterase synthase, interferes with folic acid and thus DNA synthesis. bacteriastatic

43
Q

PSA- admin

A

oral, well absorbed, always with food

44
Q

PSA- T1/2

A

2 hr

45
Q

PSA metabolism

A

Liver

46
Q

PSA excretion

A

Kidney

47
Q

PSA toxicity

A

GI- nausea, abdominal pain, diarrhea, nausea if not given w/ food. Goiter, hypothyroidism. Anemia

48
Q

Ethionamide- MOA

A

Inhibits mycolic acid synthesis

49
Q

Ethionamide- admin

A

Oral- well absorbed

50
Q

Ethionamide- distribution

A

wide

51
Q

Ethionamide- metabolism

A

Liver metabolizes it to ethionamide sulphoxide

52
Q

Ethionamide excretion

A

ethionamide sulphoxide- kidney excretion

53
Q

Ethionamide - AE

A

pyridoxine deficiency , GI- N/D/ pain, hepatotoxicity, allergic reactions

54
Q

Clofazamine- uses

A

Leprosy and Tb

55
Q

Clofazoamine- MOA

A

inhibits DNA synthesis

56
Q

Clofazamine- Admin

A

Oral

57
Q

Clofazamine T1/2

A

10 days

58
Q

Clofazamine distribution

A

widely. Concentrates in reticuloendothelil system and is slowly let out, partially accounts for long half life

59
Q

Clofazamine- excretion

A

metabolized to several inactive metabolites and excreted in the feces and urine

60
Q

Clofazamine - AE

A

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

61
Q

Cycloserine/ kanamycin- MOA

A

inhibits cell wall synthesis

62
Q

Cycloserine/ Kanmycin- use

A

rarely used due to poor efficacy and adverse eventes

63
Q

Fluroquinolones-

A

Ciprofloxacin, Moxifloxacin, Levofloxacin

64
Q

Fluroquinolones- MOA

A

inhibit topoisomerase II

65
Q

Fluroquinolones- disrtibution

A

Low intracellular concentration

66
Q

Dapsone- use

A

Tx leprosy

67
Q

Dapsone- MOA

A

inhibits folate synthesis

68
Q

Dapsone- excretion

A

excreted into bile, reabsorbed, excreted in urine

69
Q

Dapsone- AE

A

well tolerated. Fever, GI, rash, exoliative dermatitis

70
Q

Dapsone Contratindications

A

Don’t give to someone with sulfa drug allergies

71
Q

Second line Tb tx

A

Streptomyocin, Paramino Salacylic Acid, Ethionamide, Clofazamine, Cyloserine/ Kanomycin, Fluroquinolones, capreomycin

72
Q

Paucibacillary Tb- Tx

A

Rifampin& Dapsone for 6 months. Single lesion- Rifampin, ofloxacin, Minocycline

73
Q

Lepromatous MB- Tx

A

Rifampin, Dapsone, Clofazamine- 12 mos

74
Q

M. avium Tx

A

Azithromycin, Ethambutol, Rifabutin, Fluroquinolones

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