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Systemic Pharm I > Antimycobacterials > Flashcards

Antimycobacterials Flashcards

1
Q

First line antimycobacterial drugs:

A

ethambutol, isoniazid, pyrazinamide, rifampin, rifabutin, refapentine

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2
Q

Mycobacteria morphology

A

rod-shaped bacteria with unusually waxy cell walls containing mycolic acid (fatty acids)

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3
Q

What do mycobacteria infections result in?

A

slow-growing, granulomatous lesions that cause tissue destruction and become resistant to antibiotics easily

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4
Q

T/F mycobacteria are resistant to most antibiotics

A

true

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5
Q

What are characteristics of mycobacteria?

A

grow slowly, can be dormant, cell wall impermeable to many drugs, intracellular pathogens, can develop resistance

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6
Q

What is the most widely encountered mycobacterial infection? (and leading cause of death from infection)

A

tuberculosis

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7
Q

What action of tuberculosis is responsible for pulmonary tissue distruction?

A

granulomatous lesions

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8
Q

What mycobacterium condition is treated in a similar way to tuberculousis?

A

leprosy

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9
Q

What organism causes tuberculosis and where is the most common site of infection?

A

Mycobacterium tuberculosis, lungs

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10
Q

How long does it take to treat tuberculosis?

A

months to years, partially because of delayed diagnosis

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11
Q

Why does TB become resistant quickly?

A

prior treatment and pt failure to adhere to protocol

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12
Q

What is characteristic of a latent TB infection?

A

no symptoms, noninfectious, positive TB skin test, should be treated

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13
Q

What is characteristic of an active TB infection?

A

patient is sick (chest pain, cough, weakness, fatigue, weight loss), can be spread, more aggressive treatment

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14
Q

How many people worldwide are infected with TB and how many die each year?

A

1/3 of the world’s population, 2 million die

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15
Q

What are strategies for addressing drug resistance of TB?

A

multi-drug therapy that is continued well beyond the disappearance of clinical disease

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16
Q

What is directly observed therapy?

A

patient reports to doctor’s office for medication, increases compliance and decreases mortality rates

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17
Q

Which agent is the most potent?

A

isoniazid

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18
Q

What is Isoniazid’s MOA?

A

bactericidal, inhibits mycolic acid synthesis in the cell wall (resistance develops quickly if used alone)

19
Q

Describe the development of resistance to isoniazid

A

associated with several chromosomal mutations (cross resistance does not occur)

20
Q

What is isoniazids pharmacokinetics?

A

readily absorbed orally but impaired with food, effective against intracellular bacteria, metabolized by P450 (liver), excreted by kidney

21
Q

What are the adverse effects of isoniazid?

A

hepatitis/idiosyncratic hepatotoxicity, peripheral neuropathies, mental abnormalities, convulsion, optic neuritis, hypersensitivity

22
Q

Why does isoniazid create hepatitis?

A

when broken down in the liver, the metabolite is toxic and incidence increases with age and those who drink alcohol daily

23
Q

What peripheral neuropathies does isoniazid cause?

A

paresthesia (numbness) of hands and feet

24
Q

What are the three rifamycins?

A

rifampin, rifabutin, rifapentine

25
Q

Which drugs are considered the first line therapy for mycobacterium?

A

rifamycins

26
Q

T/F rifamycins can be given alone

A

false, never given as a single agent

27
Q

Do rifamycins have broader or narrower antimicrobial activity than isoniazid?

A

broader

28
Q

What is the MOA of rifamycins?

A

interact with bacterial RNA polymerase to block transcription

29
Q

What does rifampin treat?

A

gram -/+ bacteria, mycobacteria, leprosy, prophylactic meningitis

30
Q

How is resistance to rifampin created?

A

mutation decreasing affinity of RNA polymerase for the drug or decreased permeability of the drug

31
Q

How is rifampin excreted?

A

liver metabolism and excretion!!

32
Q

What are drug considerations with rifampin?

A

may require dose adjustments, it is a potent inducer of CYP450 enzymes and can shorten the half-life of many drugs

33
Q

Which drug creates orange-red secretions?

A

rifampin

34
Q

What are the adverse effects of rifampin?

A

nausea, vomiting and rash

35
Q

How is rifabutin different than rifampin?

A

less CYP450 induction which leads to fewer drug interactions

36
Q

What is a unique side effect to rifabutin not in rifampin?

A

uveitis

37
Q

Which rifamycin is preferred for HIV patients?

A

rifabutin

38
Q

Which rifamycin has the longest half life?

A

rifapentine (weekly dosing after 2 months)

39
Q

What is the MOA of pyrazinamide?

A

bactericidal to actively dividing organisms, lowers intracellular pH and inhibits growth

40
Q

What are adverse effects of pyrazinamide?

A

liver dysfunction (when combined w/ isoniazid or rifampin) and hyperuricemia (precipitate gout)

41
Q

What is the MOA of ethambutol?

A

interferes with cell wall synthesis probably by inhibition of mycolic acid synthesis

42
Q

T/F resistance is not a problem with ethambutol when given with other drugs

A

true

43
Q

What are the adverse effects of ethambutol?

A

unilateral optic neuritis with decreased vision and loss of R/G, reversed upon discontinuation

Systemic Pharm I (13 decks)

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