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Pharmacology > Respo Module - TB Drugs > Flashcards

Respo Module - TB Drugs Flashcards

All about tb drugs

1
Q

First line of agents for TB ?

A

Isoniazid, rifampin , ethambutol , pyrazinamide for 2 months

  • isoniazid and rifampin for 4 months more
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2
Q

Drugs regime for px with past hx of TB or multidrug resistant tb

A

Isoniazid+rifampin+ethambutol+pyrazinamide (1st line of drug choice)

1st drug + aminoglycoside / injectable capreomycin / fluoroquinolone / 2nd line TB drug

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3
Q

MOA of isoniazid

A

Inhibit enzyme that synthesize mycolic acid

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4
Q

Name the enzymes that synthesize mycolic acid

A
  • enoyl acyl carrier protein reductase (InhA)

- b-ketoacyl ACP synthase

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5
Q

What activates isoniazid?

A

Isoniazid is prodrug that is activated by mycobacterial catalase peroxidase (KatG)

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6
Q

Isoniazid is bacteriostatic in

A

Stationary phase

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7
Q

In rapidly dividing organism isoniazid is

A

Bacteriocidal

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8
Q

ROA of isoniazid

A

Oral administration

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9
Q

Adverse effects of isoniazid

A 
Peripheral neuritis 
Hepatitis 
Mental abnormalities
Optic neuritis
Hypersensitivity = rash and fever
Idiosyncratic hepatotoxicity
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10
Q

How isoniazid is inactivated before excretion

A

N acetylation , hydrolysis

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11
Q

-ve drug interactions of isoniazid

A

Phenytoin , carbamazepine, and benzodiazepines.

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12
Q

____ has broader antimicrobial activity

A

Rifampin

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13
Q

Mechanism of action of rifampin

A

Blocks transcription by interacting with the the beta subunit of bacterial but not human DNA dependent RNA polymerase

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14
Q

Rifamycin family

A

Rifapentin
Rifabutin
Rifampin

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15
Q

Rifampin is bactericidal?

A

True

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16
Q

Rifampin is also given in treatment of?

A

Meningitis caused by Meningococi and haemophilus influenza.

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17
Q

ROA of rifampin

A

Oral administration

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18
Q

Adverse effects of rifampin

A
  • nausea , vomiting , rash
  • hepatitis
  • fever , chills , myalgia (when given intermittently or daily dosage of 1.2gm or greater)
  • acute renal failure
  • hemolytic anemia
  • shock
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19
Q

Name of drug that is given to px infected with tb and hiv

A

Rifabutin

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20
Q

Adverse effect of rifabutin

A 
Neutropenia
Hyperpigmentation
Uveitis
Nausea , vomiting , rash
Hepatitis
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21
Q

MOA of ethambutol

A

Ethambutol inhibits mycobacterial arabinosyl transferases,

22
Q

mycobacterial arabinosyl is encoded by

A

embCAB operon

23
Q

Arabinosyl transferases are involved in

A

the polymerization reaction of arabinoglycan, component of mycobacterial cell wall

24
Q

roa of ethambutol ? absorption from gut ?

A

oral adminsitration , well absorbed from the gut.

25
Q

excretion of ethambutol

A

by kidney , glomerual filtration and tubular secretion.

26
Q

adverse effect of ethambutol

A

gout exacerbate
retrobulbar/ optic neuritis neuritis, resulting in loss of visual acuity and red-green color blindness
Hypersensitivity is rare.

27
Q

ethambutol is contraindicated in ?

A

children too young to permit assessment of visual acuity and red-green color discrimination.

28
Q

higher doses of ethambutol is given in ?

A

tuberculosis meningitis

29
Q

body excretion color changes in ?

A

rifampin adminstration

30
Q

Pyrazinamide (PZA) is ?

A

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

31
Q

prodrug form / active form of PZA

A

pyrazinoic acid

32
Q

PZA is converted into its active form by

A

mycobacterial pyrazinamidase

33
Q

action of pyrazinoic acid

A

disrupts mycobacterial cell membrane metabolism and transport functions.

34
Q

roa and absorption of PZA

A

oral , well absorbed from gut

35
Q

distribution of PZA

A

widely distributed in body tissues, including inflamed meninges.

36
Q

aminoglycoside

A

streptomycin

37
Q

2nd line drugs for TB

A

Aminoglycoside, macrolide , fluoroquinolone , caperomycin , cycloserine , ethianoamide , aminosalicyic acid.

38
Q

drug for leprosy

A

clofazimine , dapsone , rifampin

39
Q

roa of streptomycin

A

Streptomycin sulfate is used when an injectable drug

40
Q

adverse effect of streptomycin

A

ototoxic and nephrotoxic. Vertigo and hearing loss are the most common adverse effects and may be permanent.

41
Q

MOA of ethanoamide

A

chemically related to isoniazid and similarly blocks the synthesis of mycolic acids.

42
Q

adverse effect of ethanoamide

A

hepatotoxic

43
Q

roa of capreomycin

A

intramuscularly

44
Q

moa of capreomycin

A

peptide protein synthesis inhibitor antibiotic

45
Q

capreomycin adverse effect

A

nephrotoxic and ototoxic. Tinnitus, deafness, and vestibular disturbances occur. The injection causes significant local pain, and sterile abscesses may develop.

46
Q

moa of cycloserine

A

inhibits cell wall synthesis,

47
Q

cycloserine adverse effects

A

serious toxic effects are peripheral neuropathy and central nervous system dysfunction, including depression and psychoses.

48
Q

Aminosalicylic acid moa

A

folate synthesis antagonist that is active almost exclusively against M tuberculosis

49
Q

aminosalicylic acid adverse effect

A

Peptic ulceration and hemorrhage may occur. Hypersensitivity reactions manifested by fever, joint pains, skin rashes, hepatosplenomegaly, hepatitis, adenopathy, and granulocytopenia often occur after 3–8 weeks of PAS therapy, making it necessary to stop administration temporarily or permanently

50
Q

WHO recommendation about fluoroquinolone usage

A

World Health Organization recommends using a later generation fluoroquinolone such as moxifloxacin or levofloxacin.

51
Q

adverse effect of linezolid

A

bone marrow suppression and irreversible peripheral and optic neuropathy, (prolonged courses of therapy that are necessary for treatment of tuberculosis)

52
Q

linezolid is used

A

in combo with 2nd or 3rd line of drug , treatment of px with multi-drug resistant strain

Pharmacology (2 decks)

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