Name: Lecture Notes on Four important Anti-Malarial Drugs - Pharmacology
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Lecture Notes on Four important Anti-Malarial Drugs - Pharmacology

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&nbsp; Four major species are identified namely P falciparum, P vivax, P ovale, P malariaeClinically Important Anti-Malarial Drugs, Prevention and&nbsp;Treatment of Malaria:The four most important and widely used drugs for the treatment of malaria:1.Chloroquine and Hydroxychloroquine2. Quinine3. Primaquine&nbsp;4. AntifolatesClinical Indication- Chloroquine (CQ) is mostly effective against all four types of malaria (except chloroquine-resistant P falciparum)&nbsp;- Hydroxychloroquine is the analog of a chloroquine, a less toxic metabolite of CQ.- Used in the treatment of acute malaria- Malaria prophylaxis- HCQ for rheumatoid arthritis or systemic lupus erythematosusMechanism of Action- Chloroquine is effective during an intraerythrocytic stage of the parasite.- The drug concentrates into the parasite-infected erythrocytes and enters the food vacuole of the parasite by an ion-trapping mechanism.Mechanism of action:&nbsp; &nbsp; - intercalation with DNA, inhibition of heme polymerase&nbsp; &nbsp; - interaction with Ca++-calmodulin mediated mechanism&nbsp;&nbsp; &nbsp; - inhibit peptide formation and phospholipases leading to parasite deathAbsorption, Metabolism, and Excretion&nbsp;- Rapidly absorbed from the intestine&nbsp;- approximately 50% bound to plasma proteins&nbsp;- about 70% of a dose is excreted unchanged in the urine&nbsp;- half live is 120 hoursToxicity (side effects)- mild headache, visual disturbances, gastrointestinal upsets &amp; pruritus are observed during short term therapy- After prolonged therapy, ocular damage, retinopathy (bulls-eye macula), lichenoid skin eruption, bleaching of hearing, etc. may be observedDrug Interaction- Chloroquine and quinine are antagonistic and should not be used in combination.Clinical Indications&nbsp;-&nbsp;Quinine is the main alkaloid of cinchona bark (tree).- drug of choice in the treatment of an acute attack of falciparum malaria where the parasite is known to be resistant to chloroquine.- may be given intravenously and then orally when patients start to improve- Doxycycline or clindamycin may be used as combination therapy with quinine.Mechanism of action:- the mechanism for anti-malarial activity remains unclear for quinine.Absorption, Metabolism, and Excretion- Quinine is almost completely absorbed in the upper part of the small intestine&nbsp;- peaks after 1-3 hours of ingestion&nbsp;- half live is approximately 10 hours&nbsp;- metabolized in the liver (95%) to inactive hydroxy derivatives- approximately 5% is excreted in urine as an unchanged drugToxicity (side effects)- Quinine may cause Cinchonism (neural, retinal and auditory toxicity)- Abdominal pain and diarrhea&nbsp;- Rashes, fever, renal failure, hemolytic anemia, thrombocytopenia (too low platelet count in blood), etc.3.&nbsp;Primaquine/&nbsp;Primaquine phosphateClinical Indication:- used to eradicate hepatic form of P vivax or P malariea&nbsp;infections after standard chloroquine therapy.- may be used prophylactically with chloroquineMechanism of action:- inhibits the electron transport chain in mitochondria (structurally similar to coenzyme Q) of parasiteAbsorption, Metabolism, and Excretion:-Primaquine is rapidly absorbed from the gastrointestinal tract- not bound to tissues- rapidly metabolized and the metabolites may be pharmacologically active as the parent compound- peaks after 4-6 hours after ingestion- short half-life and almost completely eliminated from the body by 24 hoursToxicity (side effects):- Primaquine have shown to cause lethal hemolysis in individuals with glucose-6-phosphate dehydrogenase deficiency&nbsp;- higher dose or prolonged exposure can cause;- limited use in malaria prophylaxis due to emergence of resistance

&nbsp; Four major species are identified namely P falciparum, P vivax, P ovale, P malariaeClinically Important Anti-Malarial Drugs, Prevention and&nbsp;Treatment of Malaria:The four most important and widely used drugs for the treatment of malaria:1.Chloroquine and Hydroxychloroquine2. Quinine3. Primaquine&nbsp;4. AntifolatesClinical Indication- Chloroquine (CQ) is mostly effective against all four types of malaria (except chloroquine-resistant P falciparum)&nbsp;- Hydroxychloroquine is the analog of a chloroquine, a less toxic metabolite of CQ.- Used in the treatment of acute malaria-...

Lecture Notes on Four important Anti-Malarial Drugs - Pharmacology

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