Malarial Drugs

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four types of malarial species that infect humans are

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plasmodium falciparum
malaria
vivax
ovale

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viviax and ovale

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known for dormant hypnozoite/exoerythrocytic phase in the liver. From whicj parasite can emerge and cause relapses.

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falciparum

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does not grow in Rbc containing S,F,C(sickel cells)

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Viviax

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cannot enter duffy blood gp (people from west africa.

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P. falciparum
malariae

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no persistent exoerythrocytic phase

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chloroquine

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acts on erythrocytic stage
drug of choice for all forms of malaria except chloroquine reisitent forms of P. falciparum.

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drug accmulate in food vacuole of plasmodium,
prevent polymerization hemoglobin ; BREAK DOWN product heme is toxic to the parasite.

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chloroquine.

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chloroquine resistent parasites can expel the drug via

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p-glycoprotein pump.

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prophylaxis in all forms malaria

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chloroquine
primaquine

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to treat persistent stages of malaria in acute stages

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chloroquine
and
primaquine

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in abemic liver absess

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chloroquine and
emetine

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collagen disorder(autoimmne disorder), SLE, RA

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chloroquine

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CI: in psoriasis
and porphyria

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chloroquine

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toxicity of chloroquine

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GI: irritation
epigatric pain
exfolitive dermatitis
neuropahy
auditory impairment
rarely: Myocardial depression.

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used in acute attacks
no effect on liver phase
used in prophylaxis of all species except in endemic areas where falciparum is resistent.

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chloroquine

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safe in pregnency

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chloroquine

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is 8aminoquinoline
used in exoerythrocytic phase

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Primaquine

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drug forms quinoline -quinone metabolite nad causes hemolysis in G6PD deficient patients

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Primaquine

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is aschizonticide and ganmetocidal agent

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Primaquine

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side effects are methemoglobinemia
agranulocytosis
pruritus

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Primaquine

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used in the eradication of exoerythrocytic phase
prophylasis in endemic areas of ovale and vivax

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Primaquine

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inhibits DHFR and forms into cycloguanil

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antifolates: pyrimethamine
proguanil

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used in the prophylaxis of resistent falciparum

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proguanil
atovaquone
quinine

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syergetic blocking effect in folate pathway

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pyrimethamine
sulfadoxine
used in prophylaxis in chloroquine sensitive regions, also used in toxoplasmosis

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megalobastic anemia
sulfas crystalluria
hemolysis
steven-johnson syndrome

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pyrimethamine

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complex double standard DNA and prevents separation of strands. Thus prevents DNA replication and transcrriptions to RNA

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Quinine

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alkaloid deravitive from cinchona tree

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Quinine

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used in the cases of chloroquine resistent cases

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Quinine

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often used with doxycycline or clindamycin or pyrimethamine to shorten the therapy and limit toxicity

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Quinine

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not used for prophylaxis

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Quinine

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used in the resistent forms of P. falciparum and have no action on exoerythrocytic phase.

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Quinine

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Quinine often used with two drugs to shorten the therapy and limit toxicity.

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doxycycline or clindamycin

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used in chloroquine resistent cases

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Quinine

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not used for prophylaxis

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quinine

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used to relieve nocturnal leg cramps associated with arthritis, diabetes, atherosclerosis or thrombophebelitis

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quinine

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used in cases of myotonia congenita (curare like effect on motor endplate, reducing response to the Ach) and as sclerosing agent

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quinine

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cinchonism (heasdache, vertigo, tinnitis,blurred vision, GI distress) dose dependent is a side effect of

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quinine

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overdose can cause cardiac contraction abnormalities

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quinine

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black water fever
intervascular hemolysis

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quinine

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Ci : in pregnancy(catagory X)

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quinine
thalaomide
HMG co reducatse

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Catagory D: in pregnancy

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evidence of embrotoxicity but potentional benefit may outweigh the risks
aminoglycosides
teracycline
fluroquinolones

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synthetic 4 quinoline

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mefloquine

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has long t half life of 6 days due to enterohepatic circulation

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mefloquine

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first line of drug for prophylaxis

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mefloquine

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AE: cardiac conduction abnormalitis
psychiatric disorders
serizures
neurological abnormalities

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mefloquine

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effective against all 4 malarial species, including chloroquine resistent cases and effcetive in erythrocytic phase

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halofantrine

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cardiotoxicvity with QT prolongation as well as embrotoxicity

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halofantrine

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good prophylatic agent in areas with chloroqiuine resistent and mefloquine ressitent falciparum

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doxycycline

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inhibits e transport system _ATP synthesis(complex 3 of e tranport system) resistence is not seen

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Atovaquone

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active against PCP, trophozoites, cysts forms of T. Gondii

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arthemether

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effcetive in chloroquine reisstence P. falciparum. metabolized in food vacuole of parasite forming toxic free radicals.
Is a blood schizonticidal agent
short half lives so not good choices for chemoprophylaxia

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artemether

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safe in pregnancy

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in chloroquine resist areas: mefloquine

in endemic areas with P. falciparum: chloroquine or hydroxychloroquine
Both are active against P. falciparum.