Anti Myco Drug ish

Question 1

First Line TB drugs

Answer 1

Isoniazid
Rifampin 
Rifabutin( 1st line HIV) 
Ethambutol 
Pyrazinamide

Question 2

Second Line TB drugs

Answer 2

Amikacin
Levofloxacin
Ethionamide
Streptomycin

Question 3

Isoniazid

Answer 3

Class: Synthetic analog of pyridoxine, First line, combo in active, Sole in latent

MOA: Pro-drug activated by KatG, Targets enzymes involved in mycolic acid synth: InhA & KasA

USES: Specific for M. Tuberculosis

Resistance: mutation in KatG, mutation in acyl carrier proteins, overexpression of inhA

AE: Peripheral neuritis, Hepatotoxicity, CYP P450 inhibitor, Lupus-like syndrome

Prego- Safe in prego, should supplement Pyridoxine

Question 4

Rifampin

Answer 4

CLASS:Rifamycin, First line, Combo active, 2nd line sole latent

MOA: Blocks transcription by binding to B subunit of bacterial DNA-dependent RNA polymerase leading to inhibition of RNA synth.

USES: M. tuberculosis, M. kansasii (intra and extracellular) , Gram +/- organisms, MRSA ,

Also used to treat Leprosy

Resistance: rpoB gene ( B subunit of RNA poly),decreases affinity for bacterial DNA-dependent RNA poly

AE:Strongly induces CYP450, harless orange pee

Prego: Safe

Question 5

Rifabutin

Answer 5

CLASS:Rifamycin, First line, Combo active, 2nd line sole latent

MOA:Blocks transcription by binding to B subunit of bacterial DNA-dependent RNA polymerase leading to inhibition of RNA synth.

USES: Preferred drug for use in HIV patients( due to less induction of CYP)

Prego: NO

Question 6

Ethambutol

Answer 6

CLASS: First line, used in combination with pyrazinamide, isoniazid, & rifampin (resistance if used alone)

Specific strain of M. Tuberculosis and M. kansasii

MOA: Inhibits arabinosyltransferase leading to decreased carb polymerization of cell wall

AE: Red/green color blindness, cannot be used in children too young to receive eye test
HA, confusion, hyperuricemia, peripheral neuritis (rare)

Safe in pregnancy

Question 7

Pyrazinamide

Answer 7

CLASS: First line, used with isoniazid, rifampin, & ethambutol

MOA: Unsure, enzymatically hydrolyzed to active pyrazinoic acid

Well absorbed orally and well distributed (including CSF)

AE: Nongouty polyarthralgia, acute gouty arthritis, hyperuricemia, hepatotoxicity, photosensitivity, GI irritation, myalgia

Recommend in pregnancy only if benefits outweigh risks

Question 8

Streptomycin

Answer 8

CLASS: Aminoglycosides, used for drug resistant strains

Treat meningitis, military dissemination, and severe organ TB

MOA: Bind to 30s ribosomal subunit before ribosome formation, lead to irreversible inhibition of initiation complex. Misreading mRNA and blockade of translocation

AE; Ototoxiticity, nephrotoxicity

Question 9

Drugs for Leprosy

Answer 9

1. Dapsone
2. Clofazimine
3. Rifampin

Question 10

Dapsone

Answer 10

CLASS: related to sulfonamides, bacteriostatic

MOA: Inhibits folate synthesis

CYP P450 Inhibitor

Used to treat pneumonia (P. Jirovecii) in HIV
Well absorbed and distributed i skin

Acedapsone = repository form of dapsone

AE: Hemolysis, erythema nodosum leprosum

Question 11

Clofazamine

Answer 11

CLASS: Phenazine dye, bactericidal

MOA: Binds to DNA and inhibits replication

AE: Red-brown discoloration of skin, GI, eosinophilic enteritis

Question 12

Ethambutol

Answer 12

Class: first line

MOA: inhibits arabinosyltransferase leading to decreased carbohydrate polymerization

USE: Most strains of M. tuberculosis & M. Kansasii

Resistance: occurs rapidly if used alone, mutation in emb gene

AE: Red green color blindness, Headaches

Prego: safe

Question 13

Pyrazinamide

Answer 13

Class: First Line TB

MOA: enzymatically hydrolysed to active pyrazinoic acid

USE:N/A

Resistance: stains that lack pyrazinamidase

AE: Non Gouty polyarthralgia, gouty arthritis,

Prego: if benefits outway risk

Question 14

Strepomycin

Answer 14

Class: Aminoglycoside, second line

MOA: Same as Aminoglycosides

USES: serve life threatening tuberculosis

AE: joint pain inflammation

Question 15

Amikacin

Answer 15

Class: 2nd line

USE: Streptomycin or drug restestitant strains

AE: similar to Streptomycin, Teratogenic

Question 16

Levofloxacin

Answer 16

Class: 2nd lin

USE: Fist line drug resistant strains, ALWAYS IN COMBO

AE: Teratogenic

Question 17

Ethionamide

Answer 17

Class: 2nd line

USE: Congerer of INH ( no cross resistance)

AE: severe GI and neuro effect, Hepatotoxic and endocrine effects, Teratogenic

Question 18

Dapsone

Answer 18

Class: Leprosy drug, Bacteriostatic

MOA: Inhibits folate synthesis( via dihydropteroate synthetase inhibition)

USE: Leprosy and pneumonia(P. jiroveci in HIV patients)

AE: Hemolysis, Erythema nodosum leprosum( treat with corticosteroids) , GI issues, CYP P450 inhibitor

Question 19

Clofazimine

Answer 19

Class: Leprosy drug, Phazine dye

MOA: Bind to DNA and inhibits replication, redox properties may generate cytotoxic oxygen radicals.

USES: M. Leprae, M avium.

AE: Red brown discoloration of the skin GI irritation, Eosinophilic enteritis

Question 20

Acedapsone

Answer 20

repository form of dapsone