Antimycobacterial Drugs Flashcards

1
Q

First line of drugs for TB

A
RIPE
R Rifampin
I  Isoniazid
P Pyrazinamide
E Ethambutol
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2
Q

What is LTBI?

A

Latent Tuberculosis Infection. Infected with tuberculosis without sign and symptoms of active TB.

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3
Q

Treatment for LTBI?

A
  1. Isoniazid (monotherapy for 9 months)

2. Isoniazid + Rifapentine (12 once weekly higher doses)

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4
Q

Duration of susceptible TB therapy?

A

6 months

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5
Q

Treatment last for 2 years of?

A

Multidrug resistant TB (MDR-TB)

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6
Q

Drugs for extensively drug resistant TB (XDR-TB)?

A

Clofazimine and linezolid

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7
Q

What is DOT?

A

Directly Observed Therapy. Patients take drugs under supervision of health care team. Decreases drug resistance and improves cure rates.

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8
Q

Isoniazid is activated by?

A

KatG, catalase-peroxidase

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9
Q

MOA of Isoniazid?

A

Targets InhA and KasA, inhibits mycolic acid synthesis, disrupting bacterial cell wall

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10
Q

Isoniazid also called?

A

INH

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11
Q

Resistance of Isoniazid develops as?

A
  1. Mutations/deletion of KatG
  2. Mutation of InhA (acyl carrier protein)
  3. Overexpression of InhA
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12
Q

Pharmacokinetics of Isoniazid

A

Oral administration. Food impairs absorption
Undergoes n-acetylation
90 minutes half life
Excreted through kidney

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13
Q

Adverse effects of Isoniazid?

A

Hepatitis
Paresthesia of hand n feet (pins and needles sensation)
Convulsions, rashes, fever, nystagmus, ataxia

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14
Q

Why Isoniazid causes paresthesia?

A

Due to pyridoxine deficiency. Should take daily pryidoxine (VITAMIN B6)

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15
Q

Drugs of Rifamycins?

A

Rifampin
Rifabutin
Rifapentine

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16
Q

MOA of Rifampin?

A

Blocks RNA transcription.

By beta subunit of mycobacterium DNA dependent RNA polymerase

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17
Q

NTM species?

A

Non Tuberculosis Mycobacterium
M.avium
M.kansasii
M.leprae

18
Q

Rifampin is used for?

A

TB
M.kansasii and M.avium
Prophylactically for meningitis
Higly active for M.leprae

19
Q

Pharmacokinetics of Rifampin?

A
Oral administration 
Distribution to all body fluids/organs
Undergoes hepatic metabolism 
INDUCE HEPATIC CYTOCHROME P450
Half life 1 to 2 weeks
Excreted in bile and faeces
20
Q

Orange red colour urine/faeces seen due to?

A

Rifampin intake

21
Q

Adverse effects of Rifampin?

A
Nausea
Vomiting 
Rash
Hepatic dysfunction 
Flu like syndrome (fever chills myalgia)
22
Q

Drug given for TB + HIV patients?

A

Rifabutin

23
Q

Derivative of Rifampin causing hyperpigmentation and neutropenia?

A

Rifabutin

24
Q

Drug for LTBI with minimal TB?

A

Rifapentine (once weekly)

25
Q

Active form of Pyrazinamide?

A

Pyrazinoic acid (hydrolyzed by pyrozinamidase)

26
Q

Drugs that may cause gout?

A

Pyrazinamide

Ethambutol

27
Q

MOA of Ethambutol?

A

Inhibits arabinosyl transferase which is necessary for cell wall synthesis.

28
Q

Drug causing optic neuritis and diminished visual acuity?

A

Ethambutol

29
Q

Ethambutol causes loss of ability to discriminate which two colours?

A

Red and green

30
Q

Why second line drugs are used?

A
  1. Patient unable to tolerate 1st line drugs

2. Resisting TB

31
Q

2nd line drugs for MDR-TB?

A

Para-aminosalicyclic acid (PAS)
Capreomycin
Fluoroquinolones (Moxifloxacin)
Bedaquiline

32
Q

2nd line TB drug given parenterally?

A

Capreomycin

33
Q

Drug causing CNS disturbances (confusion, lethargy, anxiety, suicidal thoughts)?

A

Cycloserine (penetrates CSF)

34
Q

QT prolongation drugs?

A

Bedaquiline

Fluoroquinolones (rarely)

35
Q

Drug for M.avuim complex (MAC)?

A

Azithromycin

36
Q

Drugs for Leprosy?

A

Dapsone
Rifampin
Clofazimine

37
Q

MOA of Dapsone?

A

Inhibits dihydropteroate synthase, blocks folate synthesis pathway

38
Q

Adverse effects of Dapsone?

A

Hemolysis (G6PD deficient)
Methomoglobinemia
Peripheral neuropathy

39
Q

Dapsone, bactericidal? Clofazimine?

A

Dapsone is bacteriostatic

Clofazimine is bactericidal

40
Q

WHO recommended for MDR-TB?

A

Clofazimine (9 -12 months)

41
Q

Pinkish brown discoloration of skin?

A

Clofazimine

42
Q

Clofazimine decreases risk of?

A

Erythema nodosum leprosum