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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

24
Q

SM- AE

A

Ototoxicity- vistibular and auditory, renal injury, hypersensitivity

25
SM- MOA
binds 30s subunit of bac ribosome- prevents initiation complex formation. Inhibits translation
26
Paraminosalicylic Acid- PSA- MOA
competes with PABA for Mb dihyropterase synthase, interferes with folic acid and thus DNA synthesis. bacteriastatic
27
PSA- admin
oral, well absorbed, always with food
28
PSA toxicity
GI- nausea, abdominal pain, diarrhea, nausea if not given w/ food. Goiter, hypothyroidism. Anemia
29
Ethionamide- MOA
Inhibits mycolic acid synthesis
30
Ethionamide excretion
ethionamide sulphoxide- kidney excretion
31
Ethionamide - AE
pyridoxine deficiency , GI- N/D/ pain, hepatotoxicity, allergic reactions
32
Clofazamine- uses
Leprosy and Tb
33
Clofazoamine- MOA
inhibits DNA synthesis
34
Clofazamine T1/2
10 days
35
Clofazamine distribution
widely. Concentrates in reticuloendothelil system and is slowly let out, partially accounts for long half life
36
Clofazamine - AE
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
Cycloserine/ kanamycin- MOA
inhibits cell wall synthesis
38
Cycloserine/ Kanmycin- use
rarely used due to poor efficacy and adverse eventes
39
Fluroquinolones-
Ciprofloxacin, Moxifloxacin, Levofloxacin
40
Fluroquinolones- MOA
inhibit topoisomerase II
41
Dapsone- use
Tx leprosy
42
Dapsone- MOA
inhibits folate synthesis
43
Dapsone- excretion
excreted into bile, reabsorbed, excreted in urine
44
Dapsone- AE
well tolerated. Fever, GI, rash, exoliative dermatitis
45
Dapsone Contratindications
Don't give to someone with sulfa drug allergies
46
Second line Tb tx
Streptomyocin, Paramino Salacylic Acid, Ethionamide, Clofazamine, Cyloserine/ Kanomycin, Fluroquinolones, capreomycin
47
Paucibacillary Tb- Tx
Rifampin& Dapsone for 6 months. Single lesion- Rifampin, ofloxacin, Minocycline
48
Lepromatous MB- Tx
Rifampin, Dapsone, Clofazamine- 12 mos
49
M. avium Tx
Azithromycin, Ethambutol, Rifabutin, Fluroquinolones

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