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BMS201: Antimalarial Pharmacology Lecturer: Mai Ahmed Ebeid Faculty of Medicine Fall 2024  Transmission Primaquine relapse Chloroquine Clinical...

BMS201: Antimalarial Pharmacology Lecturer: Mai Ahmed Ebeid Faculty of Medicine Fall 2024  Transmission Primaquine relapse Chloroquine Clinical manifestation  AIM OF DRUG THERAPY OF MALARIA Treatment Prophylaxis Chloroquine+Primaquine Chloroquine Chloroquine+Primaquine (in vivax &oval to prevent relapse) sensitive (in vivax &oval to prevent relapse) Atovaquone-proguanil Chloroquine Atovaquone-proguanil resistant or or mefloquine or mefloquine falciparum Quinine+doxycycline doxycycline  Antifolate 4-aminoquinolines antimalarial Cholroquine drugs Mefloquine Atovaquone quinine  4-aminoquinolines Chloroquine  Blood schizonticide.  Moderately effective gametocidal in all species except falciparum. Mechanism of action: highly concentrated in infected RBCs Inhibits parasite hemoglobin digestion → ↓ nutrient amino acids for parasite. Inhibits parasite heme polymerase → accumulation of toxic heme  4-aminoquinolines Chloroquine Therapeutic uses 1. Prophylaxis & treatment of chloroquine-sensitive malaria: Radical cure in falciparum & clinical cure in ovale & vivax (followed by primaquine to eradicate dormant form→ prevent relapse). 2. Amoebic hepatitis and amoebic liver abscess. 3. Rheumatoid arthritis (anti inflammatory effect).  4-aminoquinolines Chloroquine Adverse effects: 1. GIT: nausea, vomiting, dyspepsia & abdominal pain. 2. Skin: pruritis, rash & discoloration. 3. Eye: retinal degeneration – corneal opacities. 4. C.V.S.: quinidine like action (hypotension & arrhythmias if given IV). 5. C.N.S: headache 6. Hemolytic anemia: in G6PD-deficient subjects. Resistance  4-aminoquinolines Quinine Blood schizonticide with unknown mechanism of action. Therapeutic use: Treatment of chloroquine resistant falciparum but not in prophylaxis (too toxic). Adverse effects: 1. Quinidine like action  hypotension & arrhythmias. 2. Eye blurred vision and blindness. 3. Cinchonism: tinnitus - headache - dizziness and visual disturbances. 4. Black water fever & hemolysis. 5. Oxtytocic on uterus→ abortion  4-aminoquinolines Mefloquine Mechanism of action: Blood schizonticide with unknown mechanism of action. with more effective- longer acting - less toxic. Therapeutic Uses: Treatment & prophylaxis of chloroquine resistant falciparum.  Atovaquone Active against tissue and blood schizonts. Mechansm of action: Inhibits mitochondrial electron transport , ATP & pyrimidine biosynthesis. Therapeutic uses: Prevention & treatment of choloroquine resistant falciparum (plus proguanil). Adverse effects: 1. Headaches, nausea, vomiting, diarrhea. 2. Fever, rash.  Antifolate Antimalarial drugs Proguanil - Pyimethamine - Sulfadoxine. Blood schizonticides Mechanism of action  Antifolate Antimalarial drugs Proguanil - Pyimethamine - Sulfadoxine. Therapeutic uses: Chloroquine resistant falciparum Adverse effects: 1. GIT upset 2. hypersensitivity. 3. Megaloblastic anemia 4. haemolytic anemia (in G6PDD).  8-aminoquinolines Primaquine Tissue schizonticide & gametocide (unknown mechanism of action). Therapeutic uses: 1. Radical cure of relapsing malaria (eradicate dormant form). 2. Terminal prophylaxis of relapsing malaria (given after leaving the endemic are to ensure eradication of dormant forms) 3. Prevents transmission of disease to mosquito (gametocide).  8-aminoquinolines Primaquine Adverse effects: 1. Haemolytic anemia (in G6PDD) 2. Teratogenic. A group of college students are traveling to a chloroquine-resistant malaria area for a mission trip. Which of the following medications can be used for both prevention and treatment of malaria in these students? A. Pyrimethamine. B. Cholorquine. C. Atovaquone–proguanil. D. Primaquine A patient is infested by plasmodium ovale and is suffering from repeated relapses.which one of the following drugs can be used to prevent relapse? A. Cholorquine. B. Quinine C. Artenisinin D. Primaquine Rational Professional Prescription Thank You