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Definition
blood schizonticide
MOA
-trapped in acidic parasite food vacuoles
-drug binding to hematin prevents biocrystallization of toic hematin
Resistanc--mutated vacualor efflux transporter
Lots of resistance
can be used in pregnant women
ADVERSE--GI, headache, pruritis |
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Term
| Quinine (oral, quinidine (parenteral) |
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Definition
blood schizonticide
MOA--like chloroquine
not for propylaxis
off label--leg cramps
Quinidine--severe falciparium malaria--also anti-arrhythmic agent
metabolized by CYP314=drug interactions
Cinchonism, arrythmias, thrombocytopenia, hemolytic uremic syndrome, hypoglycemia due to insulin release |
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Definition
blood schizonticide
MOA--unclear--heme iron in food vacuole cleaves endoperoxide bridge forming free radicals
rapid absorption, short half life--not for prophylaxis
first line treatment of MDR falciparum malria
replaces quinidine in severe malaria, replacement for cholorquine in pregnant patients
neurotoxicity, potential embryotoxicity |
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Definition
blood schizonticide
MOA-disrupts electron transfer
selectivity due to a.a. sequence in cytochrome b1 in humans
fixed dose combo w/ proguanil for propylaxis/treatment of chloroquine resistant malaire
ADVERSE--rash |
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Definition
blood schizonticide
MOA--inhibits DHFR, but folate can be absorbed by parasite
resistance due to DHFR
Uses--fixed combo with dihydropteroate synthetase inhibitor
acture chlorquine-resistante falciparum malaria
preventative therapy in africa
Pyrimethamine--folic acid deficiency
Selfadoxine--hypersensitivity |
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Term
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Definition
tissue (liver) schizonticide
unknown MOA
radical cure of vivax/ovale malaria with chloroquine
terminal prophylaxis after travel to v/o endemic areas
primary prophylaxis against all species if other agents are inappropriate
well tolerated in G6PD-normal patients
cyanosis due to methemoglobinemia
contraindicated in G6PD-deficient due to anemia, and in pregnancy bc G6PD status of fetus unknown |
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Definition
systemic anti-protozoal agent
prodrug--becomes DNA damaging metabolite
amebiasis, giardiasis, trichomoniasis
low colon levels--given with lumin amebicide (iodoquinol) to eradicate survivors |
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Term
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Definition
luminol antiprotozoal
MOA-aminoglycoside binds to 30S subunit of E. hystolytic
not absorbed from GI tract--no systemic
GI distress
used w/ metronidazole sometimes |
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Definition
anti-helminthic agent
inhibits polymerization of B-tubulin--no microtubules
no motility and DNA rep
first pass metabolism to active form
fatty meal--tissue parasites
no meal--nematodes
neurocysticercosis--tapeworm cysts in brain
Teratogenic in animals, liver toxicity |
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anti-helminthic
MOA--increases permeability of parasite membranes to Ca++
DOC for schistosomiasis and other trematode and cestode infections
also cysticercosis |
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Definition
MOA--depolarizine neuromuscular blockade
effective only in GI tract
activates parasitic ACh receptors and inhibits AChE
broad spectrum anthelmintic
neuromusc. blockade if given parenterally |
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Term
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Definition
MOA--tonic muscle paralysis--activation of glutamate Cl- channels
hyperpolarization of cell membrane
P-glyco efflux transporter keeps it out of CNS
broad spectrum
onchocerciasis (river blindness)--lymphatic filariasis and intenstinal nematodes
Mazzotti rxn--immune reaction to dying worms
Teratogenic in animals |
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Definition
| Active against RNA viruses Interferes with M2 protein Inhibit dissociation of ribonucleoprotein complex amantidine--renal excretion Rimantidine--live GI complaints, CNS effects Contraindicated in pregnancy Treats and prevents diseases caused by type A influenza both well absorbed from GI tract |
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Definition
neuraminidase inhibitor
anti-influeza
plumonary side effects
low oral bioavailability, so intranasal or oral powder
Adverse--pulmonary effects |
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Term
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Definition
selective neuraminidase inhibitor
well absorbed orally
prophylaxis/treatment of influ. A & B
ADVERSE-nausea, abdominal discomfort, emesis |
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Definition
nucleoside analog--DNA polymerase inhibitor
--herpes eye infections
non-toxic in opthalmic preparations |
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Term
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Definition
adenosine analog active against herpes viruses
competitive inhibitor of viral DNA polymerases and is also incorporated into DNA
--HS keratitis, HS encephalitis, herpes zoster |
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Term
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Definition
DNA polym. inhibitor, DNA chain terminator
Herpes infections (eye, genital, zoster)
ADVERSE--nephro/neurotoxicity
1st line agent, esp. in life threatening
poor oral bioavailability
NOT effective in CMV
contraindicated in pregnancy |
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Definition
Acyclovir pro-drug
requires less frequent admin. than acyclovir
better BA than acyclovir
Herpes of eye, genital, zoster
high doses for CMV
same effects as acyclovir, but worse |
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Definition
improved activity against CMV DNA polymerase inhibitor, nonnucleoside CMV infectinos
ADVERSE--bone marrow suppression,CNS--
usually IV or implants
NOT for pregnant folk |
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Definition
pro-drug of ganciclovir
rapidly absorbed and metabolized--better BA than ganciclovir
CMV
bone marrow suppression, CNS |
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Definition
broad spectrum--CMV, HSV, VZV, HIV
inhibits DNA polym. and reverse transcriptase
oral BA is poor--usually given IV
80% unchanged in urine
CMV, acyclovir resistant HSV, VZV
renal impairment, electrolyte disturbances, anemia, leukopenia, CNS |
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Term
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Definition
viral DNA polymerase
CMV in patients with aid
Nephro--major
also neutropenia and peripheral neuropathy |
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Definition
| 1st approved antisense therapy for viral infections--CMV |
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Definition
broad spectrum
synthetic nucleoside analog
interferes w/ formation of mRNA and RNA polym.
inhibits ribonucleoprotein synth.
oral BA is low
prediatric RSV
in combo with interferon for hepatitis C
anemia, serum bilirubin and uric acid, lethargy
when with interferon--fatigue, cough, rash pruritis, nausea, dyspnea--ANEMIA |
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Definition
stimulates a lot of stuff!
can have PEG that lessens dosing frequency
poorly absorbed orally
Uses--genital warts, chronic hepatitis C
bone marrow suppression, neurotiicity, flu-like symptoms and it affects about every system |
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Definition
| Lamivudine--useful against hepatitis B |
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Term
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Definition
phosporylated to triphosphate--inhibits viral reverse transcriptase--chain termination
cross BBB
used in combo
prevetns prenatal transmission
postexposure prophylaxis
ADVERSE--bone marrow suppresion, GI, lactic acidosis/sever steatosis |
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Term
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Definition
MOA--identical to AZT
oral BA is variable
used in three drug combo--mainly w/ AZT + PI or NNRTI
--NO hematological effects
painful peripheral neuropathy/pancreatitis--ABNORMAL |
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combo or after AZT failure
periperhal neuropathy
NRTI |
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NRTI
life-threatening hypersensitivity--most likely during 1st 6 weeks of treatment |
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NRTI
only once a day
less likely to cause mitochondrial toxicity
GI is common complaing |
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NRTI
Lamivudine + zidovudine |
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bind to reverse transcriptase at sites other than nucleoside catalytic site--allosteric inhibition
cross resistance is common within this class
metabolized by P450
excellent oral absorption
long half lives
ADVERSE--skin rash, liver enzyme elevation/hepatitis, fever, nausea, headache
Drug interactions--protease inhibitors and inducers of these enzymes (450) |
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bind to active site of HIV protease
--prevents processing of polyproteins
cross resistance among PIs
poor oral BA
metabolized by P450
mainly biliary excretion
ADVERSE-GI intolerance
many metabolic effects--kidney stones, hypertriclycerid, hyperglycemia, diabetes, fat wasting, abnormal fat distribution
Kidney stones--Indinavir
Drug interactions--Rifampin, P450 metabolized drugs |
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Definition
used if treated but viral replication continues
MOA--novel--peptide acts as HIV-1 fusion/inhibitor
prevents entry into cell
lacks cross resistance to other anti-HIV
ADVERSE--local injection site rxns, bacterial pneumonia, peripheral neuropathy |
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