Anti-Malarial drugs

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Anti-Malarial drugs by Mind Map: Anti-Malarial drugs

1. Blood schizontocidal drugs (To alleviate symptoms)

1.1. Artemisinin

1.1.1. features imporant because there's no resistance to it yet Fast acting blood blood schizontocide

1.1.2. preparations Artemisinin (T1/2= 4 hrs) Artesunate (t1/2= 45 min) Artemether t1/2= 4-11 hrs) preparations number 2 and 3 is synthestic forms of artemisinin which they are water-soluble becuse artemisinin = poorly soluble

1.1.3. MOA by Production of free radicals which kill the parasites

1.1.4. ADRs Trasniant heart block neutropenia Brief episode of fever neuro hepato and bone toxicity overall the drug is considered safe

1.1.5. Artemisin-Based Combination Therapies [ACTs] Indication of ACTs in severe malaria e.g cerebral malaria mild to moderate malaria ACTs Artemether + lumefantrine Artemether + amodiaquine Artemether + mefloquine Artemether + sulfadoxine-pyrimethamine

1.1.6. Why they should not be used as monotherapy? becuse of its short half life => Recrudescent (recurrence of symptoms) resistance

1.2. Chloroquine (in vivax only)

1.2.1. Uses Amebic liver abscess anti-inflammatory action Rheumatoid Arthritis SLE anti-malarial in acute attack of vivax ONLY! "eradicate blood schizonts of P. vivax" because resistanceti it has developed (Choroquine-resistance P. falciparum)

1.2.2. MOA inhibition of Heme polymerase when malaria parasite digest host cell's Hb to obtain amino acids, heme also produced which is toxic to the parasite , the parasite detoxifies it by enzyme heme polymerase which convert Heme to Hemozin (nontoxic to the parasite) ,Chloquine inhibit this enzyme accumulation of heme => parasite die. Chloroquine concentratedn1000-fold in food vacules of the parasites, Why? ion traping due to low pH. active uptake by parasite transporter. binding to specific receptor in the food vacule.

1.2.3. ADRs in short-term use as in malaria (3 days) prolong Use as in Rheumatoid Arthitis

1.2.4. Safe in pregnancy

1.2.5. Chloroquine resistance becuse of increased expression of human Multi Drug Resistance Trasporter P-Glycoprotein (MDR T P-GP) which cause efflux of chloroquine.

1.2.6. Phamacokinetic High volume of distribution concentrated into parasitised RBCs. Released slowly from tissues T 1/2: initially terminal