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Pharmacology > TB, Anti-fungals, Anti-viral Charts > Flashcards

TB, Anti-fungals, Anti-viral Charts Flashcards

1
Q

What is the MOA of Isoniazid

A

inhibits cell wall synthesis (mycolic acid)
-bactericidal
[intracellular]

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2
Q

What is the absorption and metabolism of isoniazid

A
  • well absorbed orally

- metabolized by acetylation (fast and slow acetylators)

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3
Q

What is the spectrum of Isoniazid

A

Tuberculosis

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4
Q

What are the adverse reactions of Isoniazid

A
  1. Allergic rxns
  2. Hepatotoxicity (fast acetylators)
  3. Neuritis (slow acetylators)-> tx w/ vit. B6 (pyridoxine)
  4. Insomina
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5
Q

The primary reason for the use of drug combinations in the treatment of tuberculosis is to:
A.  Reduce the incidence of adverse effects
B.  Enhance activity against metabolically inactive mycobacteria
C.  Ensure patient compliance with the drug regimen
D.  Delay of prevent the emergence of resistance
E.  Provide prophylaxis against other bacterial infections

A

D.  Delay of prevent the emergence of resistance

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6
Q

Initial therapy for active TB is typically

A

Initial therapy 2 months: “RIPE”

Rifampin + INH (isoniazid) + PZA (pyrazinamide) + Ethambutol

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7
Q

Multidrug therapy is recommended for most mycobacterial infections. However, which of the following may be treated with a single drug?
A.  Disseminated M. avium complex infections
B.  Latent TB infections
C.  Leprosy
D.  Systemic tuberculosis
E.  None of the above

What is the drug that can be used?

A

B.  Latent TB infections

Isoniazid

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8
Q

How do you treat latent TB infection

A

Isoniazid daily or 2x week DOT [6-9months]

OR if INH sensitive:
Isoniazid + pyridoxine (vit. B6 for 9 months

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9
Q 
A 24-year-old patient receiving combination therapy for the treatment of tuberculosis becomes pregnant, although she had been using oral contraceptives (estrogen + progestin). Which of the following drugs is responsible for the interfering with the contraceptive action, resulting in medication failure?
A.  Ethambutol
B.  Isoniazid
C.  Pyrazinamide
D.  Rifampin
E.  Streptomycin
A

D.  Rifampin

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10
Q

How do you treat active TB in someone who is pregnant

A

INH + Rifampin + ethambutol (+ pyrazinamide if co-infected w/ HIV or suspected drug resistance)

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11
Q

Which statement about the use of isoniazid (INH) in the treatment of TB is FALSE?
A.  INH is bactericidal against actively growing tubercle bacilli
B.  Native Americans are fast acetylators and may require higher doses
C.  Symptoms of peripheral neuritis may occur during treatment
D.  INH may induce the metabolism of certain drugs
E.  Patients should take pyridoxine (vitamin B6) daily

A

D.  INH may induce the metabolism of certain drugs

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12
Q 
Mycolic acids are major components of mycobacterial cell walls. Which of the following drugs inhibits the synthesis of this component? 
A.  Ethambutol 
B.  Isoniazid 
C.  Pyrazinamide 
D.  Rifampin 
E.  Streptomycin
A

B.  Isoniazid

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13
Q

What is the MOA of rifampin

A

-inhibition of RNA polymerase
-bactericidal
[intracellular]

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14
Q

What is the absorption and elimination of rifampin

A
  • well absorbed orally

- hepatobillary excretion (DQCRIMES)

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15
Q

What is the spectrum of rifampin

A
  1. Tuberculosis
  2. Gram positive cocci
  3. Gram negative rods: pseudomonas, H. influenza, Legionella
  4. Anerobes
  5. Atypicals: mycoplasma, chlamydia
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16
Q

What are adverse reactions of rifampin

A
  1. Hepatotoxic
  2. Colors secretions orange/red (urine, sweat, tears, permanent staining of contact lenses)
  3. INDUCER of CYP1A2, 2C9-19, 3A4
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17
Q

Select the FALSE statement concerning rifamycin antibiotics:
A.  Rifampin can be used as chemoprophylaxis in close contacts of patients with meningococcal disease
B.  Rifapentine can be given once weekly for treatment of active TB infections
C.  Rifabutin is a weaker inducer of CYP450 and is preferred over rifampin for TB treatment in HIV patients on HAART
D.  Rifamycins are inhibitors of DNA-dependent RNA polymerase
E.  Rifamycins are bacteriostatic against M. tuberculosis

A

B.  Rifapentine can be given once weekly for treatment of active TB infections

E.  Rifamycins are bacteriostatic against M. tuberculosis

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18
Q

What is the MOA of pyrazinamide

A

uncertain
[intracellular]
-basteriostatic

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19
Q

Describe the absorption, distribution and elimination of pyrazinamide

A
  1. well absorbed orally
  2. widely distrubted (100% to CNS)
  3. hepatic metabolism

*dosage reduction required in both renal and hepatic impairment

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20
Q

What is the spectrum of pyrazinamide

A

Tuberculosis

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21
Q

What are adverse reactions of pyrazinamide

A
  1. Hepatotoxicity
  2. Hyperuricemia–> gout
  3. Drug rash
  4. Avoid in children unless crucial to therapy
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22
Q

What is the MOA of ethambutol

A
  • inhibits cell wall synthesis (arabinosyltransferase)

- bacteriostatic

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23
Q

Describe the absorption, distribution and elimination of ethambutol

A
  1. well absorbed orally
  2. concentrates in lungs
  3. renal and fecal excretion
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24
Q

What are adverse reactions of ethambutol

A
  1. Optic neuritis (visual acuity reduction, retinal damage)

2. Avoid in children bc of difficulty monitoring visual acuity

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25
Q 
A 34-year-old male has returned to the for his 1-month check-up after starting treatment for tuberculosis. He is receiving isoniazid, rifampin, ethambutol, and pyrazinamide. He states that he feels fine, but now is having difficulty reading his morning newspaper and feels he may need to get glasses. Which of the TB drugs may be causing his decline in vison? 
A.  Ethambutol 
B.  Isoniazid 
C.  Pyrazinamide 
D.  Rifampin
A

A.  Ethambutol

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26
Q 
A 27-year-old male, former heroin user, has been on methadone maintenance for the past 13 months. Two weeks ago he had a positive TB skin test (PPD) and chest radiograph evidence of upper lobe infection. He was started on standard 4 drug antimycobacterial therapy. He has come to the ED complaining of “withdrawal symptoms” and seeking more methadone. Which of the following antimycobacterial drugs is likely to have caused the patient’s acute withdrawal reaction? 
A.  Ethambutol 
B.  Isoniazid 
C.  Pyrazinamide 
D.  Rifampin 
E.  Streptomycin
A

D.  Rifampin

*to prevent w/drawal == Rifabutin?

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27
Q

What are polyene detergents antifungal agents?

A
  1. amphotericin B

2. Nyastatin

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28
Q

What are Imidazole antifungal agents

A
  1. Ketoconazole
  2. Clotrimazole
  3. Miconazole
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29
Q

What are Triazole antifungal agents

A
  1. fluconazole

2. itraconazole

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30
Q

What are allylamine antifungal agents

A

Terbinafine

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31
Q

How do you treat dermatophyte fungal infections (cutaneous mucocutaneous)

A
  1. Generally conservative with use of topical antifungal agents (clotrimazole, miconazole, terbinafine)
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32
Q

How do you typically treat fungal nail infections

A
  • generally requires systemic therapy

- Itraconazole or terbinafine

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33
Q

How do you treat Candida (esp. albicans)

A
  1. Topical clotrimazole or
    nystatin for mucocandidiasis
    2.  Try fluconazole via systemic (oral) route if no response
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34
Q

How do you treat systemic fungal infections?

[Blastomycosis, Coccidioidomycosis, Cryptococcosis, Histoplasmosis]

A
  1. Long term therapy with systemic amphotericin B infusions generally required
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35
Q

How do you treat opportunistic systemic fungal infections?

[Candida albicans, Aspergillus fumigatus, Pneumocystis carinii]

A
  1. Candidiasis: Fluconazole
  2. Aspergillosis: Amphotericin B
  3. Pneumocystis pneumonia: TMP-SMX
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36
Q

___ are the most broad ABX and can cause fungal infections

A

Tetracyclines

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37
Q 
Interactions between this drug and cell membrane components can result in the formation of pores lined by hydrophilic groups present in the drug molecule: 
A.  Fluconazole 
B.  Amphotericin B 
C.  Itraconazole 
D.  Nystatin 
E.  Ketoconazole 
F.   Terbinafine
A

B.  Amphotericin B

D.  Nystatin

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38
Q

What is the MOA of amphotericin B and nyastatin

A
  • binds to ergosterol, forming pores in membranes with loss of vital intracellular constituents
  • fungicidal
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39
Q

What is the absorption and elimination of amphotericin B

and nyastatin

A
  • poor oral: IV or topical only
  • slowly excreted by kidneys plus hepatobiliary (half life= 15 days)
  • *CANNOT CROSS BBB

Nystatin: topical only

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40
Q

amphotericin B has LESS selective toxicity because it also binds to __ in mammalian cells

A

cholesterol components

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41
Q

What is the spectrum of amphotericin B

A 
*broad-- choice for life threatening systemic infections (esp. immunocompromised)
A-Aspergillosis
B-Blastomyces
C-Cryptococcosis
D-Deep candida
E- Extracutaneous sporotrichosis
42
Q

What are adverse reactions of amphotericin B

A
  1. Nephrotoxicity (80%–nearly in all)
  2. infusion rxn w/ fever/chills—> tx w/ acetaminophine- diphenhydramine prior)
  3. anemia (secondary to nephrotoxicity and decreased erythropoeitin synthesis)
43
Q 
The dose-limiting toxicity of amphotericin B is: 
A.  Hepatitis 
B.  Hypotension 
C.  Infusion-related adverse effects 
D.  Myelosuppression 
E.  Renal tubular acidosis
A

E.  Renal tubular acidosis

*nephrotoxic

44
Q

What is the use of Nystatin

A

superficial candidal infections

45
Q

what are adverse reactions of Nystatin

A

well tolerated topically

-mild GI upset if swallowed

46
Q 
Which of the following antifungal agents is most commonly associated with renal insufficiency? 
A.  Fluconazole
B.  Amphotericin B 
C.  Itraconazole 
D.  Nystatin 
E.  Ketoconazole
A

B.  Amphotericin B

47
Q

What is the MOA of triazoles

A

like imidazole, but more selective inhibition of fungal P450

48
Q

Describe the absorption and elimination of triazoles
Fluconazole:
Itraconazole:

A

Fluconazole:

  • IV/PO
  • renal excretion
  • enters CNS for meningitis***

Itraconazole:

  • IV/PO/topical
  • hepatic metabolism
49
Q

Describe the spectrum/clinical use of Fluconazole

A
  1. Vaginal candidiasis (single dose)
  2. Oropharyngeal and esophageal candidiasis
  3. Cryptococcal meningitis
50
Q

Describe the spectrum/clinical use of Itraconazole

A

**BROADER THAN fluconazole (includes aspergilliosis)

  1. systemic therapy for superficial dermatophytosis and onychomycosis (nails)
51
Q 
Which drug is most appropriate for oral (systemic) use in the treatment of vaginal candidiasis? 
A.  Clotrimazole 
B.  Fluconazole 
C.  Flucytosine 
D.  Nystatin 
E.  Amphotericin
A

B.  Fluconazole

52
Q

What are adverse effects of fluconazole

A

*well tolerated

  1. Lesser effect on CYP450 metabolism
  2. alopecia
  3. GI upset
  4. Hepatitis
53
Q

What are adverse effects of itraconazole

A
  1. CHF
  2. HA
  3. Inhibits CYP450 drug metabolism (similar to ketoconazole)
  4. N/V/D
54
Q

Select the true statement regarding the pharmacology of fluconazole:
A.  It is an inducer of hepatic drug-metabolizing enzymes
B.  It does not penetrate the blood-brain barrier
C.  It is highly effective in the treatment of aspergillosis
D.  It has the least effect of all azoles of hepatic drug metabolism
E.  Oral bioavailability is less than that of ketoconazole

A

D.  It has the least effect of all azoles of hepatic drug metabolism

55
Q

What is the MOA of Imidazole

A

inhibit P450 ergosterol synthesis, altering membrane permeability

56
Q

Describe the absorption, distribution, and elimination of imidazole:

  1. Ketoconazole:
  2. Clotrimazole/Miconazole:
A
  1. Ketoconazole:
    - IV/PO/Topical
    - crosses placental but poorly into CNS
    * *MUST TAKE W/ FOOD (best absorption w/ low pH)
    - hepatic metabolism
    - excreted in breast milk
  2. Clotrimazole/Miconazole:
    - topical only
57
Q

Describe the spectrum/clinical use of Ketoconazole

A
  1. systemic infections (ie. candidiasis)

* declining use due to toxicity

58
Q

Describe the spectrum/clinical use of Clotrimazole/Miconazole

A

oral and vaginal candidiasis

59
Q

what are adverse reactions of ketoconazole

A
  1. Blocks adrenal steroid synthesis (decrease testosterone)
  2. Rash
  3. Urticaria
  4. N/V/anorexia
  5. Cyp450 inhibition
  6. Hepatotoxicity (increase LFTs)
  7. Gynecomastia
60
Q 
If amphotericin B is administered to patient CK, she should be premedicated with: 
A.  Diphenhydramine 
B.  Ibuprofen 
C.  Prednisone 
D.  Fentanyl 
E.  Scopolamine
A

A.  Diphenhydramine
B.  Ibuprofen
C.  Prednisone

61
Q

What is the MOA of Terbinafine

A

inhibits squalene oxidase reducing ergosterol synthesis

62
Q

Describe the absorption, distribution, and elimination of Terbinafine

A
  • well absorbed PO/topical
  • distributed well
  • metabolized by hepatic P450
63
Q

What are the clinical uses of Terbinafine

A
  1. oral for toe/finger nail infection-onychomycosis

2. topical for athletes foot - tinea cruris, tinea corporis

64
Q

What are adverse reactions of Terbinafine

A
  1. Taste alteration
  2. HA
  3. Inhibition of CYP450
  4. Rash
  5. Diarrhea
65
Q 
A 56-year-old female with diabetes presents for routine foot evaluation with her podiatrist. The patient complains of thickening of the nail on the right big toe and a change in the color (yellow). The podiatrist diagnoses the patient with onychomycosis of the toenails. Which of the following is the most appropriate choice for treating this infection? 
A.  Itraconazole 
B.  Ketoconazole 
C.  Nystatin topical 
D.  Terbinafine 
E.  Clotrimazole topical
A

D.  Terbinafine

66
Q 
Cryptococcal meningitis is a serious life-threatening opportunistic fungal infection that is a concern in immunosuppressed patients. The drug that is commonly used as a prophylactic measure in HIV and bone marrow transplant patients is: 
A.  Clotrimazole 
B.  Amphotericin B 
C.  Fluconazole 
D.  Itraconazole 
E.  Trimethoprim-sulfamethoxazole
A

C.  Fluconazole

67
Q

What are anti-influenza drugs

A
  1. Oseltamivir/Zanamivir

2. Amantadine/Rimantadine

68
Q

What are drugs for HSV-VZV

A
  1. Acyclovir
  2. Valacyclovir
  3. Ganciclovir
69
Q

What is the MOA of Oseltamivir/Zanamivir

A

*Neuramindidase inhibitors

Inhibit viral neuramindase to decrease viral budding
decrease infectivity

70
Q 
Neuraminidase inhibitors are most effective when started how long after symptom onset? 
A.  Within 24 hours 
B.  Within 48 hours 
C.  Within 72 hours 
D.  Within 96 hours 
E.  Within 5 days
A

B.  Within 48 hours

71
Q

Describe the absorption and elimination of Oseltamivir

A
  • administered PO as prodrug

- renal elimination

72
Q

Describe the absorption and elimination of Zanamivir

A
  • inhaled to respiratory tract

- renal elimination

73
Q

What are the clinical uses of Oseltamivir

A
  1. prophylaxis and tx of Influenza A and B– start w/in 48 hrs of sx
  2. decreases severity and duration
  3. can use in children 1+ and adults
74
Q

What are the clinical uses of Zanamivir

A
  1. prophylaxis and tx of influenza A and B– start w/in 2 days of sx
  2. decreases LRT complications and duration
  3. Can use in 7y/o+
75
Q 
Antiviral treatment is recommended for which of the following with suspected influenza? 
A.  Adults ≥ 65 years old 
B.  Residents of nursing homes 
C.  Immunosuppressed patients 
D.  All of the above

Influenza vaccination is recommended for?

A

D.  All of the above

anyone over 6 months

76
Q

What are adverse reactions of Oseltamivir

A
  1. N/V/Abdominal pain
    * Decreased if taken w/ food
  2. HA
  3. Fatigue
  4. Preg . C
77
Q

What are adverse reactions of Zanamivir

A
  1. transient nasal and throat discomfort
  2. Bronchospasm/cough
  3. Preg. C
78
Q 
A 75-year-old man with chronic obstructive pulmonary disease is diagnosed with suspected influenza based on his complaints of flu-like symptoms that began 24 hours ago. Which of the following agents is most appropriate to initiate for the treatment of influenza? 
A.  Ribavirin 
B.  Oseltamivir 
C.  Rimantadine 
D.  Acyclovir 
E.  Zanamivir
A

B.  Oseltamivir

79
Q

A 28-year-old woman in her 4th month of pregnancy was exposed to family members with documented influenza and she has had influenza-like symptoms for one day. When you suggest treatment with an antiviral drug, she asks whether the drug could hurt her baby. You could her that:
A.  Pregnant women are at high risk for complications of influenza
B.  Oseltamivir appears to be safe for use during pregnancy
C.  No adequate studies of oseltamivir have been done in pregnancy
D.  Oseltamivir is pregnancy category C
E.  All of the above

A

E.  All of the above

80
Q

What is the MOA of Amantadine/Rimanadine

A

inhibit viral uncoating by block of viral M2 proton channel

81
Q

Describe the absorption, distribution and elimination of Amantadine/Rimanadine

A
  • good oral (PO)
  • accumulates in lungs
  • R has poor CNS penetration
82
Q

What is the clinical uses of Amantadine/Rimanadine

A

-Prophylaxis and treatment of influenza A— limited current use due to resistance **

83
Q

What are adverse reactions of Amantadine/Rimanadine

A

[A]:

  1. Concentration difficulty
  2. HA
  3. Insomina
  4. LH
  5. GI upset

[R]:
better tolerated– poor CNS penetration

84
Q 
A patient receives a drug that is converted to acyclovir in the body. Which antiviral action is exerted by this agent? 
A.  Inhibition of viral uncoating 
B.  Inhibition of DNA polymerase 
C.  Inhibition of viral entry 
D.  DNA chain termination 
E.  Prevention of viral maturation
A

B.  Inhibition of DNA polymerase

D.  DNA chain termination

85
Q

What is the MOA of acyclovir and analogs (Valacyclovir)

A
  • phosphorylated by viral thymidine kinase–> inhibits viral DNA
  • Selectively toxic - 1st phosphorylation step by Herpes- encoded thymidine kinase (only occurs in infected cells)
86
Q

How does Acyclovirs have selective toxicity

A
  • 1st phosphorylation step by Herpes- encoded thymidine kinase (only occurs in infected cells)
  • Acyclovir triphosphate inhibits viral DNA polymerase (more sensitive than human DNA polymerase)
87
Q 
Acyclovir would be ineffective against HSV strains with loss of expression of: 
A.  M2 proton channel 
B.  Dihydrofolate reductase 
C.  Reverse transcriptase 
D.  Thymidine kinase 
E.  Neuraminidase
A

D.  Thymidine kinase

88
Q

The most common resistance in acyclovir/valacyclovir is ___

A

reduction or loss of expression of viral TK (thymidine kinase)

89
Q

Describe the absorption, distribution, and elimination of acyclovir

A
  • Poor oral (15-30%) Need 3-5 doses/day
  • Administered topical/PO, IV
  • cross cell membrane–> trapped intracellularly
  • Renal elimination
90
Q

Describe the absorption, and elimination of Valacyclovir

A
  • Prodrug of acyclovir (80-90% F)– BID

- renal elimination

91
Q 
Which of the following patient groups may require acyclovir dosage adjustments from the usual recommended mg/kg adult doses? 
A.  Neonates 
B.  Patients taking St. John’s wort 
C.  Patients taking cimetidine 
D.  Chronic kidney disease patients 
E.  Pregnant patients
A

A.  Neonates

D.  Chronic kidney disease patients

*poor renal fxn

92
Q 
A 24-year-old female is diagnosed with genital herpes simplex infection. Which of the following agents is indicated for use in this diagnosis? 
A.  Acyclovir 
B.  Cidofovir 
C.  Foscarnet 
D.  Ganciclovir 
E.  Valacyclovir 
F.   Zanamivir
A

A.  Acyclovir

E.  Valacyclovir

93
Q

What are the clinical uses of acyclovir and valacyclovir

A
  1. primary HSV1 and 2 infections (best w/in 48-72 hrs)
  2. Recurrent HSV 1 and 2 (episodic or chronic suppressive tx)
  3. Disseminated varicella zoster infection (IV)
  4. primary VZV– requires 2-3x higher dose than HSV
  5. recurrent VZV (shingles)- best if begun early <72hrs

*mucosal, genital, encephalitis

94
Q

What is the oral tx of primary HSV1 or 2

A

acyclovir (3-5 doses/day) or valacyclovir (bid) for 7-10d

95
Q 
The drug of choice for the treatment of serious or disseminated varicella-zoster infections is: 
A.  Famciclovir 
B.  Valacyclovir 
C.  IV acyclovir 
D.  Cidofovir 
E.  Foscarnet
A

C.  IV acyclovir

96
Q

What is the treatment for primary VZV infection (chicken pox)

A
  1. Symptomatic tx of fever in children
  2. Acyclovir QID for 5 d in adults if uncomplicated
  3. acyclovir IV TID for 7 d if severe or immuncompromised
97
Q 
Treatment of fever in an 8-year-old with chicken pox can be most safely managed with which of the following OTC antipyretic agents? 
A.  Acetaminophen 
B.  Aspirin 
C.  Celecoxib 
D.  Ibuprofen 
E.  Any of the above
A

A.  Acetaminophen

D.  Ibuprofen

98
Q

What is the treatment for shingles

A
  1. Oral acyclovir (3-5 doses/day) or valacyclovir (bid) for 7d
  2.   IV acyclovir (tid x 7d) if immunosuppressed or severe complications

**need higher doses of acyclovir for varicella zoster

99
Q

What are adverse reactions of Acyclovir/valacyclovir

A
  • generally tolerated orally
    1. HA
    2. N/V
    3. CNS effects w/ high dose ie. IV or VAL (confusion, hallucinations, seizures)
    4. Renal toxicity w/ IV route— minimize w/ hydration
    5. Preg. B
100
Q

What medication is OTC that treats HSV1 labialis (decrease healing time by 15 hrs 4.8–>4.1 days)

A

Docosanol (topical)

Pharmacology (31 decks)

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