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Pharmacology Exam I
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Anti-malarial agents are important for travelers to
South America
Africa
Asia
Types of Malaria
single cell invasion and multiplication
dormant hepatic stage
Single liver cell invation and multiplication
falciparum
malariae
Dormant hepatic stage
vivax
ovale
goal for treatment of falciparum and malaria
eradicate erythrocytic stage
goal for treatment of vivax and ovale
eradicate erythrocytic and hepatic stages
A single sporozoite infecting a liver cell can produce____ merozites within 6 days of infection
30-40K
agents that target stages of malaria
blood schizonticidal agent
tissue schizonticidal agent
gametocidal agent
Classes of antimalarial agents
4-aminoquinoline
quinoline
8-aminoquinoline
folate antagonists
artemisinins
antagonistic combinations
4-aminoquinolines
chloroquine
drug of choice
schizonticide and gametocide
3-5 day half life
Chloroquine is not effective against
falciparum
Chloroquine clinical use
prophylaxis 500mg weekly
must be used to cure dormant liver forms vivax and ovale
primaquine
chlorpquine mechanism of action
causes heme toxicity to parasite
Adverse effects with chloroquine
pruritus
hemolysis with G6PD deficiency
Chloroquine contraindications
psoriasis
visual field abnormalities
caution in liver disorders
cations (antidiarrheals) interfere with absorption
safe for use during pregnancy
chloroquine
Amodiaquine
similar to chloroquine but limited use due to toxicity
used for falciparam that is resistant to chloroquine
Toxicities with amodiaquine
agranulocytosis
hepatotoxicity
aplastic anemia
Quinoline class
quinine
quinidine
mefloquine
quinine and quinidine used for
protection against erythrocitic stage
not active against hepatic parasites
not gametocidal (falciparum)
Quinine and quinidine are not generally used for prophylaxis due to
toxicity
cardiac dysrhythmias and hypotension
tinnitus
chinchonism
Contraindications of quinine and quinidine
mefloquine
digoxin
warfarin
Mefloquine
potent blood schizonticide
used for chloroquine resistant parasites
prophylactic dose of mefloquine given
weekly
mefloquine usually recommended for
travelers
Mefloquine contraindicated with
seizures
psychosies
arrhythmias
children under 5kg
8-aminoquinoline class
primaquine
atovaquone
only agent effective agiainst hepatic stage of vivax and ovale
primaquine
Atovaquone
recommened for chloroquine resistance
disrupts mitochondrial electron transport
Atovaquone active against
falciparum but not vivax and ovale
Atovaquone bioavailability increased with
fatty food
Atovaquone + rifampin or tetracycline
decrease plasma concentrations by 50%
Folate metabolism antagonists
Pyrimethamine
Proguanil
erythrocytic stage
Sulfonamides and sulfones
active against erythrocytic stage
not used alone
Fansidar
sulfadoxine and pyrimethamine
for toxoplasmosis
no longer for malaria due to resistance
Fansidar is contraindicated in
3rd trimester of pregnancy
lactating mothers
Fansidar and sulfonamides act on
pteridine synthetase
pyrimethamine or proguanil act on
dihydrofolate reductase
Antibiotics used as co-therapy in malaria
doxycycline
clindamycin
azithromycin
Artemisinin
chinese herbal
no prophylaxis
irreversible neurotoxicity
avoid in pregnancy
Artesunate
artemisinin derivative
available through CDC
free radical production
active against multi drug resistant malaria
Drugs used for travelers
mefloquine
doxycycline
chloroquine
hydroxychloroquine
malarone
Prophylaxis dosing
2 weeks before travel and up to 1 month after return
Author
Rx2013
ID
61333
Card Set
Pharmacology Exam I
Description
Anti-malarial agents
Updated
2011-01-22T21:55:25Z
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