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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 MOR

A

katG mutation

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6
Q

INH- AE

A

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

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7
Q

Rifampin- MOA

A

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

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8
Q

RIF & liver enzymes

A

CYP450 inducer

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9
Q

RIF excretion

A

mostly feces, some urine

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10
Q

<p>

| RIF AE</p>

A

<p>

| Reddish/ brown Urine, skin eruptions</p>

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11
Q

RIF drug interactions

A

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

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12
Q

RIfabutin

A

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

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13
Q

Rifampimicin

A

Used for leprosy

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14
Q

Pyrizinamide (PZA)- MOA

A

Pyrizinamidase converts it to pyrizinmatoic acid –> unknown MOA

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15
Q

PZA 1/2 life

A

9 hr

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16
Q

PZA- distribution

A

well distributed in tissues but concentrates in cells

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17
Q

PZA activity

A

active in acidic environments ie lysozomes inside of macropahges

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18
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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19
Q

Ethambutol MOA

A

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

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20
Q

Ethambutol distribution

A

most tissues, including CNS –> used for TB meningitis

21
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

22
Q

Streptomycin (SM)- use

A

occasionally used in conjunction with first line tax

23
Q

SM- admin

A

IV/ IM

24
Q

SM- AE

A

Ototoxicity- vistibular and auditory, renal injury, hypersensitivity

25
Q

SM- MOA

A

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

26
Q

Paraminosalicylic Acid- PSA- MOA

A

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

27
Q

PSA- admin

A

oral, well absorbed, always with food

28
Q

PSA toxicity

A

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

29
Q

Ethionamide- MOA

A

Inhibits mycolic acid synthesis

30
Q

Ethionamide excretion

A

ethionamide sulphoxide- kidney excretion

31
Q

Ethionamide - AE

A

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

32
Q

Clofazamine- uses

A

Leprosy and Tb

33
Q

Clofazoamine- MOA

A

inhibits DNA synthesis

34
Q

Clofazamine T1/2

A

10 days

35
Q

Clofazamine distribution

A

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

36
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

37
Q

Cycloserine/ kanamycin- MOA

A

inhibits cell wall synthesis

38
Q

Cycloserine/ Kanmycin- use

A

rarely used due to poor efficacy and adverse eventes

39
Q

Fluroquinolones-

A

Ciprofloxacin, Moxifloxacin, Levofloxacin

40
Q

Fluroquinolones- MOA

A

inhibit topoisomerase II

41
Q

Dapsone- use

A

Tx leprosy

42
Q

Dapsone- MOA

A

inhibits folate synthesis

43
Q

Dapsone- excretion

A

excreted into bile, reabsorbed, excreted in urine

44
Q

Dapsone- AE

A

well tolerated. Fever, GI, rash, exoliative dermatitis

45
Q

Dapsone Contratindications

A

Don’t give to someone with sulfa drug allergies

46
Q

Second line Tb tx

A

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

47
Q

Paucibacillary Tb- Tx

A

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

48
Q

Lepromatous MB- Tx

A

Rifampin, Dapsone, Clofazamine- 12 mos

49
Q

M. avium Tx

A

Azithromycin, Ethambutol, Rifabutin, Fluroquinolones

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