Drugs 2 Flashcards
(24 cards)
Amphotericin B
Class: Systemic Anti-Fungal
Use: Used for severe systemic mycoses initial intervention, then switch to other anti-fungal
MOA: Binds ergosterol in fungal membranes
Adverse Effects: Fever, chills, nausea, vomiting, headache, nephrotoxicity is common and ofter irreversible (pre-medicate with antipyretics, antihistamines, and analgesics)
*Liposomal ampho B is a “reservoir” for amphotericin
Flucytosine (5-flurocytosine)
Class: Systemic Anti-Fungal
Use: Cryptococcus and some candida
MOA: Need fungal channel and activated by fungal cytosine deaminase
Adverse Effects: Major toxicity is due to death of fungal cells and release of active drug to local tissue
Ketoconazole
Class: Systemic Anti-Fungal
Use: 1st effective oral anti-fungal for systemic use
MOA: Inhibit ergosterol synthesis
Adverse Effects: N and V or anorexia, hepatotoxicity, and blocks adrenal steroidogenesis leading to gynecomastia
Itraconazole
Class: Systemic Anti-Fungal
Use: Histoplasma, blastomyces, sporothrix
MOA: Inhibits ergosterol synthesis
Adverse Effects: Less effects on mammalian cells that ketoconazole
Fluconazole (Diflucan)
Class: Systemic Anti-Fungal
Use: Most widely used antifungal - cryptococcal meningitis, candidemia, mucocutaneous candidiasis
MOA: Inhibit ergosterol synthesis
Adverse Effects: More selective for fungal CYPs
Voriconazole
Class: Systemic Anti-Fungal
Use: Newest triazole - candida, dimorphic fungi, invasive aspergillus
MOA: Inhibits ergosterol synthesis
Adverse Effects: Little mammalian CYP inhibition. Visual disturbances in 30% of patients
Nystatin
Class: Mucocutaneous Anti-Fungal
Use: Topical only
MOA: Similar to amphotericin B, but too toxic for systemic use
Griseofulvin
Class: Mucocutaneous Anti-Fungal
Use: Systemic for ringworm and athlete’s foot
MOA: Concentrates in keratinized tissue
Terbinafine
Class: Mucocutaneous Anti-Fungal
Use: Systemic or topical for topical fungal infections
MOA: Inhibits squalene epoxidase (ergosterol synthesis)
Caspofungin
Class: Inhibitor of fungal cell wall synthesis
Use: Candida, empiric anti-fungal therapy (in febrile neutropenia), salvage therapy for amphotericin resistant aspergillus
MOA: Inhibits synthesis of β(1-3)glucan which is necessary for cell wall
Adverse Effects: Minor GI effects, flushing (some inflammatory response)
Chloroquine
Class: Anti-Malarial
Use: Blood schizonticide. Curative for P. malaria, and susceptible P. falciparum
MOA: Altered metabolism of hemoglobin by parasite, also blocks nucleic acid synthesis
Adverse Effects: Generally well tolerated, pruritus, GI, mild headache, may exacerbate psoriasis or porphyria
*used w/ Primaquine for P. vivax P. ovale
Mefloquine
Class: Anti-Malarial
Use: Prophylaxis or treatment for chloroquine-resistant malaria
MOA: unknown
Adverse Effects: GI, CNS, possible psychotropic effects
Quinine
Class: Anti-Malarial
Use: Chloroquine resistant P. falciparum
MOA: Inhibits nucleic acid and protein synthesis, glycolysis, actual mechanism unclear
Adverse Effects: Cinchonism (headache, sweating, nausea, tinnitus, dizziness, blurred vision) and QT prolongation
Atovaquonel
Class: Anti-Malarial
Use: Used for prophylaxis or treatment for resistant P. falciparum. Combo w/ atovaquonel + produanil = “Malarone”
MOA: Inhibits electron transport chain
Adverse Effects: GI (abdominal pain, nausea, vomiting), headache, anorexia, and dizziness
*poorly absorbed
Proguanil
Class: Anti-Malarial
Use: Used for prophylaxis or treatment for resistant P. falciparum. Combo w/ atovaquonel + produanil = “Malarone”
MOA: Inhibits protozoal dihydrofolate reductase - active metabolite (cycloguanil)
Adverse Effects: GI (abdominal pain, nausea, vomiting), headache, anorexia, and dizziness
Primaquine
Class: Anti-Malarial
Use: Tissue schizonticide
MOA: Affects tissue schizonts (hepatic stage)
Adverse Effects: Some GI distress, hemolytic anemia in G6PD deficiency
*use in combo w/ chloroquine for prophylaxis or cure of P. vivax and P. ovale
Pyrimathamin-Sulfadoxine (Fansidar)
Class: Anti-Malarial
Use: Effective blood schizonticide for P. falciparum - chloroquine resistant P. falciparum = slow acting, cannot be used along for attacks
MOA: anti-folate combination - blocks synthesis/utilization of folic acid
Adverse Effects: Some GI distress, cutaneous reactions - sometimes severe
Artesunate
Class: Anti-Malarial
Use: Multidrug resistant P. falciparum. Rapidly acting blood schizonticide
*semisynthetic form of artemisinin (traditional Chinese medicine)
Metronidazole
Class: Anti-Protozoal
Use: Intestinal, extraintestinal, and urogenital protozoal infections (trichomoniasis, giardiasis, amebiasis), anaerobic infections
MOA: Tissue amebecide
Adverse Effects: Nausea, headache, dry mouth, leukopenia, Disulfiram effect
Nitozoxamide
Class: Anti-Protozoal
Use: Giardia lamblia and cryptosporidia parvum. Useful against metronidazole resistant strains
MOA: Inhibits electron transport chain - pyruvate-ferridoxin oxidoreductase (PFOR)
Adverse Effects: Few adverse effects, far better tolerated than metronidazole
Pentamidine
Class: Anti-Protozoal
Use: Aerosol used for treatment and prophylaxis for pneumocystis pneumonia
MOA: Unknown
Adverse Effects: Can cause respiratory stimulation followed by depression (primarily with IV), hypotension, anemia, adverse effects less common with aerosol administration
Albendazole
Class: Anti-Helminthic
Use: Wide spectrum anti-helminthic
MOA: Interferes w/ microtubule aggregation and alters glucose uptake
Mebendazole
Class: Anti-Helminthic
Use: Wide spectrum anti-helminthic - pinworm, hookworm, Ascaris
MOA: Blocks microtubule synthesis, blocks vesicle and organelle movement
Adverse Effects: Dose limited by GI effects, possibly embryotoxic
Ivermectin
Class: Anti-Helminthic
Use: Intestinal strongyloidiasis nad onchocercasias
MOA: Inhibits chloride channels causing paralysis and death
Adverse Effects: Very minor effects on human GABA receptors - headache, dizziness, and drowsiness may occur
