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Spring 2018 Pharm Exam 4 > #3: Drugs for TB > Flashcards

#3: Drugs for TB Flashcards

1
Q

What are the 3 major Tx challenges of TB

A

3I’s

  1. Impermeable cell wall
  2. Intrinsic resistance (d/t lot of efflux pumps)
  3. Inaccessible (b/c intracellular in macrophages)
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2
Q

Where is TB located in latent vs active phase, why does this matter

A

Latent phase –> inside macrophages

Active –> outside macrophage
- can be transmitted

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3
Q

What are the 4 1st line drugs for txting TB?

A

1st line drugs for txting TB = “RIPE”

  1. Rifampin
  2. INH
  3. Pyrazinamide
  4. Ethambutol
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4
Q

Which of the 1st line TB drugs are cell wall inhibitors? (3)

A

Cell wall inhibitors for TB

  1. INH
  2. Pyrazinamide
  3. Ethambutol
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5
Q

Which 2 cell wall synthesis inhibitors can penetrate macrophages

A

Cell wall synthesis inhibitors that penetrate macrophages

  1. INH
  2. Pyrazinamide
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6
Q

Which cell wall synthesis inhibitor inhibits mycolic acid synthesis and dihydrofolate reductase

A

INH

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7
Q

Which cell wall synthesis inhibitor is the MOST effective in susceptible strains of TB

A

INH

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8
Q

What does INH’s t 1/2 depend on

A

INH’s t 1/2 depends on:

NAT2 polymorphisms/ acteylation rate

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9
Q

INH Acteylation rate

  1. what does fast acteylation mean for metab + result?
  2. what does slow acetylation mean for metab + result?
A

INH Acteylation rate

  1. Fast acteylation = fast metab –> drug ineff
  2. Slow acteylation = slow metab –> toxicity
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10
Q

INH AEs

  • 4 major a/w this drug
  • which is MC
A

INH AEs

  1. Hepatic toxicity = MC
  2. PN (Peripheral Neuropathy)
  3. Rash, fever
  4. OD
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11
Q

INH AEs: Hepatic toxicity (+/- fatal)

  1. what is it incr w/ (2 things)
A

INH AEs: Hepatic toxicity (+/- fatal)

  1. incr w/ slow acteylators and age (> 35)
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12
Q

INH AEs: PN (Peripheral Neuropathy)

  1. what type of ppl it is incr in
  2. what is it d/t
  3. Tx for it
A

INH AEs: PN

  1. incr in slow acteylators
  2. d/t = Vit B6/Pyroxodine defic
  3. Tx for it = Vit B6
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13
Q

What 4 drugs have interactions w/INH

A

Drug interactions w/INH

  1. Acetaminophen
  2. Warfarin
  3. Diazepam
  4. Phenytoin
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14
Q

Drug Interactions w/INH

  1. Acetaminophen - what does CYP2E1 induction cause
  2. Warfarin - what type of inhibition may cause incr bleedin
  3. Diazepam - what type of inhibition leads to sedation/resp depression (2)
  4. Phenytoin - what does CYP2C19 inhibition cause
A

Drug Interactions w/INH

  1. Acetaminophen
    - CYP2E1 induction–> hepatotoxicity
  2. Warfarin
    - CYP2C9 inhibition may–> incr bleedin
  3. Diazepam
    - CYP3A/2C19 –> sedation/resp depression
  4. Phenytoin
    - CYP2C19 inhibition–> neuro toxicity
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15
Q

Cell Wall Synthesis Inhibitors: Pyrazinamide

  1. what converts Pyrazinamide –> pyrazinoic acid (POA)
    (converts it from prodrug to active)
  2. what does POA inhibit + then block the synthesis of
A

Cell Wall Synthesis Inhibitors: Pyrazinamide

  1. pncA (myocbacterial pyrazinamidase) converts Pyrazinamide –> pyrazinoic acid (POA)
    (converts it from prodrug to active)
  2. POA blocks FAS1 –> inhibits mycolic acid synthesis
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16
Q

Cell Wall Synthesis Inhibitors: Pyrazinamide

  1. at what pH is this drug active at
    - b/c of this where is it active
A

Cell Wall Synthesis Inhibitors: Pyrazinamide

  1. active at acidic pH –> active in macrophages/TB lesions (acidic)
17
Q

Cell Wall Synthesis Inhibitors: Pyrazinamide

what types of mutations–> resistance

A

Cell Wall Synthesis Inhibitors: Pyrazinamide

pncA mutations –> resistance

18
Q

Cell Wall Synthesis Inhibitors: Pyrazinamide

  • what are the 3 AEs a/w this drug
A

Cell Wall Synthesis Inhibitors: Pyrazinamide AEs

  1. Hepatoxicity
  2. Hyperuricemia (exacerbates gout)
  3. Arthralgias
19
Q

Cell Wall Synthesis Inhibitors: Ethambutol

  1. MOA: what does it inhibit that utimately stops the growth of the bacteria
  2. What mutations lead to resistance
  3. What is the major but rare AE
A

Cell Wall Synthesis Inhibitors: Ethambutol

  1. MOA: it inhibits mycobacterial arabinosyl transferase (embAB operon) –> incr BACTERIAL cell wall permeability –> stop bacterial growth
  2. embB mutations resistance
  3. major but rare AE = Optic Neuritis
20
Q

Cell Wall Synthesis Inhibitors: Ethambutol AEs

- what are the 2 manif of Optic Neuritis

A

Cell Wall Synthesis Inhibitors: Ethambutol AEs: 2 manif of Optic Neuritis

  1. Loss of visual acuity
  2. red-green color blindness
21
Q

What is the prototype drug for Rifamycins

A

prototype drug for Rifamycins = Rifampin

22
Q

Rifampin

  1. does it penetrate macrophages
  2. bacteriostatic or cidal
A

Rifampin

  1. yes it penetrates macrophages
  2. bacteriocidal
23
Q

What is the general MOA for Rifampin

A

general MOA for Rifampin = inhibit RNA synthesis

24
Q

MOA for Rifampin: inhibits RNA synthesis

  1. how does it inhibit RNA synthesis (what does it bind to)
    - why is that important
A

MOA for Rifampin

1. inhbits RNA synthesis by binding to DNA dep RNA polyermase –> ONLY in bacterial cells (doesnt effect host)

25
Q

Rifampin

  1. what is mutations lead to resistance
  2. what is the major AE of this drug
A

Rifampin

  1. rpoB mutations lead to resistance
  2. major AE = turns urine, tears other body fluids red-orange
26
Q

Rifampin: Drug Interactions

  1. what does it induce the hepatic metabolism of
  2. What types of HIV drugs does it incr metab of
  3. if it decr the t 1/2/incr metab of many drugs what does this lead to
A

Rifampin: Drug Interactions

  1. induces the hepatic metabolism of MOST CYPs
  2. incr metab of PIs and RT inhibitors
    (HIV drugs)
  3. It decr t 1/2 of many drugs –> therapeutic failure (drugs ineff)
27
Q

Preferred TB Tx Regimens

  1. for Latent TB
  2. for Active TB
A

Preferred TB Tx Regimens

  1. for Latent TB –> INH (+ Vit B6) for 9 months
  2. for Active TB –> RIPE x 2 months –> RI x 4 months
28
Q

DOT and TB

  1. why is it recommended
  2. what 4 groups/types of Tx is it recommended for
A

DOT

  1. recommended b/c MC cause of TB Tx failure = non-compliance (length of Tx)
  2. recommended for
    - intermittent Tx, active TB Tx, Kids - daily Tx, drug resis TB
29
Q

What drug is approved for MDR (multi drug resistant) TB

A

Bedaquiline/Sirturo = for MDR TB

30
Q

Bedaquiline/Sirturo and MDR TB

  1. what does it inhibit (MOA)
  2. AEs: what does it incr the levels of
  3. what CYP does it interact w/ and therefore you cant give it w/ _______
A

Bedaquiline/Sirturo and MDR TB

  1. inhibits myocbacterial ATP synthase (stops NRG production in bacteria)
  2. AE: incr levels of hepatic transaminases
  3. interacts w/CYP34A —> CANT GIVE W/RIFAMPIN
31
Q

Bedaquiline/Sirturo and MDR TB

  • what are the 2 BBW for it
A

Bedaquiline/Sirturo and MDR TB: BBW

  1. incr risk of death
  2. QT prolongation `
32
Q

2nd line Tx for TB: Aminoglycosides

what is the main drug in this class

Note: other not discussed = Amikacin

A

2nd line Tx for TB: Aminoglycosides

drug = Streptomycin

33
Q

2nd line Tx for TB: Aminoglycosides (Streptomycin)

  1. what is this not 1st line
  2. what type of TB infxn can it only be used for + why
    (note used only for severe cases)
  3. what are the 2 major AEs
A

2nd line Tx for TB: Aminoglycosides (Streptomycin)

  1. not 1st line b/c of resistance to it
  2. ONLY for ACTIVE TB infxn b/c it cant enter cells
    (note used only for severe cases)
  3. 2 major AEs
    - oto/nephrotoxicity
    - risk in pregnancy
34
Q

What 2 other types of drugs used as 2nd line Tx for TB

A

2nd line Tx for TB

  1. Fluoroquinolones (Levo)
  2. Cycloserine
35
Q

XDR (Extremely drug resistant) TB

  • what 4 drugs is it resistant to
A

XDR TB: resistant to

  1. INH
  2. Rifampin
  3. Fluoroquinolone
  4. 1 IV 2nd line drug (ex: aminoglycoside)
36
Q

What is the Atypical Mycobacterium

- how are TB drugs affected by it

A

Atypical Mycobacterium = non TB infxn

- TB drugs less effective

37
Q

Atypical Mycobacterium: MAC

- what is the 3 drug regimen for it

A

Atypical Mycobacterium: MAC Tx

  1. Rifampin
  2. Ethambutol
  3. MACrolides

“Return of thE MAC”

38
Q

Leprosy/Hansen’s Dz (caused by M.leprae)

  1. why is multi drug Tx needed
  2. what is the 3 drug tx regimen
A

Leprosy/Hansen’s Dz (caused by M.leprae)

  1. multi drug Tx needed to avoid resistance
  2. 3 drug tx regimen
    - Rifampin
    - Dapsone
    - Clofazimine

“Hansen Really Didnt wanna Catch Leprosy”

Spring 2018 Pharm Exam 4 (7 decks)

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