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Antifungal Agents/Antitubercular Agents - Updated
Pharm Assessment 13
51
Pharmacology
Graduate
02/10/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
What antifungal agent binds to ergosterol in fungal cell membranes?
Definition

Polyenes:

Amphotericin B

 

allows leakage of small molecules

Term
What are the 2 different formulations of Amphotericin B?
Definition

Non-Lipid Based - (Deoxycholate)

 

Three lipid-based forms - (Abelcet, AmBisome, Amphotec)

Term
How is Amphotericin B administered? What is it bound to in the Plasma?
Definition
Primarily used IV 90% bound to B-lipoprotein
Term
What adverse side effect of Amphotericin B is potentiated by sodium depletion?
Definition
Nephrotoxicity Reversible at normal dose Residual damage at high doses
Term
What can be done to treat/prevent Fever and chills caused by Amphotericin B?
Definition

Premedicate with steroids or antipyretic

 

Merperidine may help abort if already started

Term
What 5 Adverse effects can Amphotericin B cause?
Definition
Nephrotoxicity Thrombophlebitis at injection site Fever and Chills Hypersensitivity Reaction Shock-like hypotension
Term
What are the therapeutic uses for Amphotericin B?
Definition

Candida albicans Histoplasmosis Cryptococcus Aspergillus Blastomyces

 

Deep Fungal infxns in Pregnant woman

Term
What is the preferred treatment for deep fungal infections in Pregnancy?
Definition
Amphotericin B
Term
What antibiotic inhibits thymidylate synthase and DNA synthesis?
Definition
5-Flucytosine
Term
What drug is 5-Flucytosine almost always used in combination with?
Definition
Amphotericin B
Term
How is 5-Flucytosine activated in cell?
Definition
5-Flucytosine --cytosine deaminase--> 5-FU --UMP pyrophosphorylase--> 5-FUMP --ribonudleotide reductase--> 5-FdUMP --> inhibits thymidylate synthase
Term
How does resistance develop to 5-Flucytosine?
Definition

Lack of permease

Defective or decreased cytosine deaminase

Term
What antifungal agents inhibit synthesis of ergosterol?
Definition

Azoles:

Voriconazole

Ketoconazole

Term
What organisms are the Azoles active against?
Definition
Yeasts (Candida) Dermatophytes (Epidermophyton) Systemic mycoses (Histoplasma)
Term
What azole can cause visual disturbances?
Definition
Voriconazole (Transient, blurred vision, photophobia, altered perception of color or image)
Term
How should Voriconazole be administered in patients with creatinine clearance <50?
Definition
give orally
Term
What organisms is Voriconazole used for?
Definition
Invasive aspergillosis Scedosporium Fusarium Invasive fluconazole-resistant Candida
Term
What Azole has a common side effect of anorexia, nausea, and vomiting?
Definition
Ketoconazole
Term
What adverse side effects occur with Ketoconazole?
Definition
Decrease plasma testosterone conc. Gynecomastia decreased libido and loss of potency in men Menstrual irregularities in women Adrenal steroidogenesis inhibited with high doses
Term
What Azoles have hepatic elimination?
Definition
Voriconazole
Term
What antifungals should be used to treat Blastomycosis and Histoplasmosis?
Definition
Amphotericin B - life threatening infections
Term
What antifungals should be used to treat Cryptococcus?
Definition
Amphotericin B +/- 5-Flucytocine
Term
What antifungals should be used to treat superficial/mucosal Candida Albicans?
Definition
Ketoconazole
Term
What antifungals should be used to treat disseminated Candida albicans?
Definition
Amphotericin B
Term
What antifungals should be used to treat Non-albicans candidiasis? (Torulopsis glbrata, Candida krusei)
Definition
Amphotericin B
Term
What antifungal inhibits squalene epoxidase, necessary for egosterol synthesis?
Definition
Terbinafine
Term
What drug concentrates in the hair and nail beds?
Definition
Terbinafine
Term
What drug has an adverse side effect of occasional taste disturbance?
Definition
Terbinafine
Term
What are the frequent side effects of Terbinafine?
Definition
Headache and GI disturbance
Term
What is the treatment of Onychomycosal fungal infections? (ringworm of the nails)
Definition
Terbinafine
Term
What antifungal disrupts mitotic spindle structures of fungal cells?
Definition
Griseofulvin (Fungistatic)
Term
Where is Griseofulvin deposited in the body? How is it absorbed?
Definition

Keratin precursor cells

 

well absorbed with ultramicro size form and fatty meal

Term
What antifungal is used to treat Dermatophytes? (Epidermophyton, Micosporum, Trichophyton)
Definition
Griseofulvin
Term
What drugs does Griseofulvin accelerate the metabolism of?
Definition
Coumarin Estrogens Oral contraceptives
Term
What is the 1st line therapy for M. tuberculosis?
Definition
Isoniazid + rifampin + pyrazinamide + ethambutol or streptomycin
Term
What is the 1st line therapy for M. Avium complex?
Definition
Clarithromycin + ethambutol or clofazimine or ciprofloxacin or amikacin
Term
What are the drugs used for Mycobacterum tuberculosis?
Definition
Isoniazid Rifampin Ethambutol
Term
What TB drug interferes with mycolic acid synthesis?
Definition
Isoniazid
Term
What cells is Isoniazid Cidal for? What is it static for?
Definition

Cidal - rapidly dividing bacilli (extracellular cavitary lesions)

 

Static for slow growing (closed caseous lesions and macrophages)

Term
What does Isoniazid compete with that can cause Peripheral neuropathy? Who is it more frequent in? How is treated?
Definition

pyridoxal phosphate

More frequent in malnourished, diabetics, and alcoholics Corrected with vitamine B6 supplements

Term
What causes Hepatotoxicity from Isoniazid use?
Definition
Due to toxic metabolite from acetylation of isoniazid
Term
What drug interactions does Isoniazid have?
Definition
Antacids w/ Al+++ decrease absorption Corticosteriods decrease efficacy Inhibits P450 for phenytoin
Term
What is the complex relationship between Isoniazid and Corticosteriods?
Definition
Prednisone reduces plasma conc of INH INH inhibits the hepatic metabolism of cortisol
Term
What TB drug inhibits RNA synthesis by binding Beta subunit of RNA polymerase?
Definition
Rifampin
Term
What is the absorption of Rifampin imparied by?
Definition
Food or para-aminosalicylic acid
Term
What TB drug has an adverse side effect of orange-red tears, urine, and saliva?
Definition
Rifampin
Term
What drug interactions does Rifampin have?
Definition
P450 inducer (oral anticoagulants and contracepives less effective) Probenecide increases rifampin serum concentrations
Term
What is the first line therapy against mycobacterium tuberculosis?
Definition
Rafampin
Term
What else, besides TB, is Rafampin used for?
Definition
MRSA and S. epidermidis (w/ vancomycin or gentimicin) Prophylactic against meningitis by meningococci or H. influenzae Eradication of staph in nasal carriers Antileprosy
Term
What TB drug has an adverse reaction of Optic Neuritis?
Definition
Ethambutol
Term
What TB drugs can cause Hyperuricemia?
Definition
Ethambutol
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