pharm - ID2.txt

zanamivir (Relenza), oseltamivir (Tamiflu), peramivir

viruses have 2 surface proteins. hemagglutinins are responsible for the binding and uptake of the virus, while neuraminidases are responsible for release of new virus (via sialic acid cleavage). NIs block this cleavage, preventing release of new virus.

Tamiflu oral, Relenza inhaled (so not for folks c respiratory disease)

influenza

GI. Tamiflu unusual dreams. Relenza possible bronchospasm

amantadine (Symmetrel), rimantadine (Flumadine)

flu A: thought to prevent influx of protons through viral M2 channels that causes the pH-dependent process of RNA-protein coat dissociation. parkinsons: amantadine may increase dopamine release and block ACh receptors, enhancing motor control.

amantadine more lipophilic, so more CNS SE than rimantadine (but better for Parkinsons)

viral enzymes convert nucleoside analogues to active nucleoside triphosphates, which are then incorporated and mess with viral DNA strands.

nephrotoxicity. ganciclovir BBW hematologic toxicity, carcinogen, aspermatogenesis. cidofovir BBW nephrotoxicity, neutropenia, carcinogen.

oral antivirals (nucleoside analogues)

cidofovir (high propensity for nephrotoxicity)

ALL THE CYCLOVIRS. acyclovir (Zorivax), valacyclovir (Valtrex), codofovir (Vistide)

acyclovir, famciclovir, penciclovir

ganciclovir

cidofovir IV

penciclovir topical

ALL THE AZOLES. fluconazole (Diflucan), 2G voriconazole (Vfend)

block the synthesis of ergosterol, a fundamental constituent of the fungal cell membrane

superficial topical fungi (candida, dermatophytes), uncomplicated/health pt systemic fungi

direct CYP450 inhibitors. inhibit warfarin metabolism (increase INR)

ketoconazole BBW hepatotoxicity. itraconazole BBW CHF (negative ionotropic effects).

ALL THE FUNGINS. caspofungin (Cancidas), anindulafingin (Eraxis), micafungin (Mycamine).

inhibits glucan synthase in fungal cell walls, an enzyme responsible for rigidity (causes weak cell walls that lyse).

severe invasive fungal infections (candida, aspergillus)

watch for anaphylaxis

inhibits fungal cell division by binding to proteins like tubulin.

deposited into keratin precurson cells, increasing their resistance to infection.

dermatophyte infections o skin/hair (trichophyton, microsporum, epidermophyton)

porphyria, pregnancy, hepatic failures. caution if sensitive to penicillin.

CYP3A4 inducer.

photosensitivity, rash

amphotericin B, Nystatin

bind sterols, such as ergosterol found in fungal cell membranes (puts pores in membrane, ions leak, cell dies). also b/c it binds sterols, also binds cholesterols causing its SEs.

amphotericin B has long half life (15 days) b/c it is accumulated in tissues and released slowly. Nystatin too toxic for parenteral, but works good for topical/oral rinse due to low absorption.

amphotericin B: serious invasive/systemic fungal infections. Nystatin: noninvasive candidal infections.

nephrotoxicity, INFUSION REACTIONS, electrolyte abnormalities.

flucytosin (Ancoban)

taken up by cytosine permease, an enzyme present only in fungi. it is then metabolized (> 5-FU > 5-FDUMP) and goes on to inhibit thymidine synthetase (needed for DNA replication)

severe fungal infections. use in combo with amphotericin B to prevent resistance.

N/V (give capsules a few at a time over a 15 min period). BBW renal impairment. lots of other kick ass SE including TEN.

ALL THE QUINES. chloroquine (Aralen), hydroxychloroquine (Plaquenil).

largely unknown. chloroquine possibly concentrates in parasitic food vacules, causing toxic heme buildup. primaquine is the only drug that works on both the exoerythrocytic and erythrocytic phases of malarial infection (P vivax, P ovale).

malaria (chloroquine first line). also RA, SLE, cutaneous skin disorders. quinine+clindamycin also for babesial infections.

mefloquine seizures, some psych issues.

quinine+mefloquinine (QT prolongation, seizures). quinine+Aluminum antacids (messes c absorption/excretion).

chloroquine visual disturbances (hydroxychloroquine is a less toxic alternative). quinine cinchonism (tinnitus, HA, nausea, dizziness, flushing, visual disturbances)

slow elimination of mefloquine (second line) allows for single dose treatment (f/u c primaquine for liver bugs)

praziquantal ocular infection, CNS lesions, seizure hx.

albendazole alopecia, reversible leukopenia, elevated liver enzymes.

nematodes (roundworms), trematodes (flukes), cestodes (tapeworms)

mebendazole (-worms), diethylcarbamazine (filial), piperazine (ascaris), ivermectin/Stromectal (strongyloides, onchocerciasis - also scabies)

praziquantal/Biltricide

praziquantal/Biltricide, albendazole/Albenza (neurocysticercosis, Hydatid disease)

disrupts microtubule formation, impairs glucose uptake. also larvicidal, ovicidal.

immobilize microfilariae and render them more susceptible to host defenses

paralyzes (increases Ca++ permiability)

paralyzes (promotes GABA)

paralyzes (intensifies GABA via Cl- channel activation)

pentamidine (Pentam), melarsoprol, nifurtimox, iodoquinol (Yodoxin)

melarsoprol disrupts protozoal enzymatic activity. nifurtimox inhibits trypanothione reductase.

pneumocystis, African trypanosomiasis, leishmaniasis

trypanosomiasis

American trypanosomiasis (Chagas disease)

pentamidine hypotension/tachycardia, nephrotoxicity*, by IV hypoglycemia (so IM). melarsoprol reactive encephalopathy, polyneuropathy.