HD4 Pharm Flashcards
Artemether/Iumafantrine (coartem)
Mech: unknown
Route: oral – CYP 450 metab.
Use: for acute P. falciparum malaria (*NOT for prophylaxis or severe)
SE: hypersensitivity (urticaria & angioedema)
Malarone
(combo of atovaquone & proguanil)
Mech: block pyrimidine synthesis
Route: oral; biliary & urinary excretion.
Use: to Tx malaria from P. falciparum (acute, uncomplicated)
(SE: headache, GI)
Nitazoxanide
Mech: interferes w/ energy production Route: oral, hepatic metab (but NOT CYP) Use: diarrhea from Giardia lamblia or Cryptosporidium parvum SE: none *NOT effective if immunocompromised
Paromycin
Mech: blocks protein synthesis
Route: oral, poor absorption –> Luminal
Use: intestinal amoebiasis (NOT for systemic inf)
SE: nausea, abdominal crampls, diarrhea
Types of malaria
- Plasmodium falciparum: => malignant tertiary fever (deadly), most drug resistance.
- Plasmodium vivex, ovale, malariae: => benign tertiary fever, relapse common.
three types/approaches to treatment for malaria
- clinical cure: eliminate all erythrocytic forms
- radical cure: eliminate all erythrocytic AND exoerythrocytic forms
- prophylaxis (prevention/protection)
Drugs used for superficial fungal infections (skin, gut, oral cavity, eyes)
*rarely life-threatening, unless immuno-compromised.
1. Nystatin
2. Griseofulvin
3. Clotrimazole
4. Terbinafine
(mostly used superficially only too toxic for systemic use)
drugs used for systemic fungal infections
- Amphotericin B
- Flucytosine
- Fluconazole
- caspogungin
Terbinafine
Mech: inhibits ergosterol synth. fungistatic OR fungicidal
Route: topical or oral & hepatic metab.
Use: onychomycosis (on fingernails), candida, trychophyton
SE: *watch for P450 induction/inhibition, liver dysfunction
Caspofungin
Mech:
Route:
Use: for aspergillous (esp. invasive) or candida
SE:
Nystatin
Mech: binds to ergosterol (same as ampho B)
Route: topical (to skin & mucous membranes), poor absorption
Use: candida infections (skin, bowel, etc.)
SE: —
Clotrimazole
Mech: inhibit ergosterol
Route: topical (NOT oral)
Use: candidiasis
SE: —
Prednisone
Mech: glucocorticoid, modulates gene expression
Use: immune-suppressant for RA, SLE, severe psoriasis, neoplasia
Route: prodrug, metab @ liver
SE: (not very selective) -> insomnia, weight gain, Cushings, susceptible to infection
Sirolimus
Anti-proliferative immune-suppressant
Mech: binds FKB-12 -> complex inhibits mTOR, so –l T cell activation
Use: kidney rejection prophylaxis or chronic rejection
*(NOT liver or lung)
Route: metab in liver
SE: edema, HTN, risk infections & malignancy
Drugs that inhibit CYP450
- Ca2+ blockers
- Anti-fungals (fluconazole, ketoconazole)
- erythromycin
- HIV protease inhibitors
Drugs that induce CYP450
- Rifampin
2. Phenytoin
Azathioprine
Anti-proliferative immune-suppressant prodrug
Mech: blocks de novo purine synthesis (active as 6-mercaptopurine)
Use: prevent kidney rejection OR refractory RA
SE: hepatotoxicity, myelosuppression, mucositis, GI Sxs, *teratogen & carcinogen!
Cyclophosphamide
anti-proliferative immune-suppressant, Prodrug (metab by liver)
Mech: electrophile cross-linking of DNA
Use: BMT conditioning, RA (off-label)
SE: myelosuppression, GI, bladder toxicity, ovarian failure & sterility