ANTI-MALARIAL DRUGS

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ANTI-MALARIAL DRUGS

  1. 1. Prophylaxis, treatment & prevention ofrelapse.Aims of antimalarial drugsTo prevent & treat clinical attack of malariaTo completely eradicate the parasite from pt.To reduce the human reservoir of infec.,
  2. 2. CLASSIFICATIONTissue schizontocides• PrimaquineBlood schizontocides• Chloroquine• Mefloquine• Quinine• Proguanil• Pyrimethamine• Artemisinin derivatives• Tetracyclines• Halofantrine• lumefantrine
  3. 3. CHLOROQUINE4-Aminoquinoline derivative….
  4. 4. Other actions…Anti inflammatoryLocal anaestheticWeak smooth muscle relaxantAnti histaminicAnti arrhythmic
  5. 5. PHARMACOKINETICSPlasma t1/2-3-10 days
  6. 6. USESClinical cure & SuppressiveprophylaxisExtra intestinal amoebiasisRheumatoid arthritisDLELepra reactionPhotogenic reactionInfectious mononucleosis
  7. 7. PRIMAQUINE8-Aminoquinoline…
  8. 8. MECHANISM OF ACTIONAs OxidantsSchizonticidal actionHemolysisMethemoglobinemia
  9. 9. PHARMACOKINETICSPlasma t1/2-3-6 hrs
  10. 10. Adverse effectsAbd. PainG.I. upsetWeakness in chestCNS & CVS symptomsLeucopeniaHemolysisMethaemoglobinemiaTachypnoeaCyanosis
  11. 11. UsesRadical cure of vivax malariaPrimaquine 15 mg for adult,0.25mg/kg for children - daily for 2weeks with G6PD status testing.Primaquine 45 mg(0.75mg/kg) +Chloroquine 300 mg once a weekfor 8-10 week without G6PD testing.Radical cure of Falciparum malariaPrimaquine 45 mg single dose +Curative dose of Chloroquine
  12. 12. MEFLOQUINEQuinoline – Methanol derivatives…
  13. 13. PKPlasma t1/2 – 2-3 weeksHigh affinity to plasma proteinAdverse effectBitter in tasteDizziness, nausea, vomitingDiarrhoeaAbd. PainSinus bradycardiaRare events are haematological,hepatic, cutaneous toxicity.
  14. 14. InteractionsHalofantrine/Quinidine/Quinine – QTc lengthβ blocker/Ca channel blocker/Digitalis/Anti depressant –exagerrated bradycardia/arrhythmiaUsesMulti drug resistant P.falciparumProphylaxis of malaria amongtravellers 5 mg/kg/week x 2-3 week
  15. 15. QUININE/QUINIDINECinchona bark derivatives….
  16. 16. MOA is similar to ChloroquineLess effective & more toxicOther actionsLocal irritant & anaestheticSystemic action Gastric secretionWeak analgesic & antipyreticCardiac depressant,anti arrhythmicHypotensiveHypoglycemia
  17. 17. PKOral absorbtion is complete70% plasma bound – α1 acid glycoproteinAdverse effectCinchonismRinging in earsNauseaVomitingHead acheMental confusionVertigoDifficulty in hearing and visual defectDiarrhoeaMarked perspiration
  18. 18. Uses…MalariaUncomplicated resistant falciparummalaria2nd line to S/P – ACTQuinine + Doxycycline x 7 daysComplicated & severe malariaQuinine i.v. – DOC for cerebral malariaNocturanal muscle crampsΔsis of myasthenia gravisAlong with Urethane in Varicose vein
  19. 19. PYRIMETHAMINEDiaminopyrimedine derivative….
  20. 20.  Mechanism of action Directly acting inhibitor of plasmodial DHFRase PK Oral absorbtion is good Plasma t1/2 – 4 days Adverse effect Nausea Rashes Folate deficiency Megaloblastic anaemia & granulocytopenia
  21. 21. SULFONAMIDE-PYRIMETHAMINECOMBINATION
  22. 22. Sulfadoxine & Sulfamethopyrazine –Ultra long acting SulfonamidesAlong with artesunate,used inchloroquine resistant malariaS/P – DOC for Toxoplasmosis
  23. 23. TETRACYCLINES
  24. 24. Slow & weak erythrocyticschizontocidal actionAlong with quinine/S-P, used inchloroquine resistant malariaDoxycycline 200 mg/day + Artesunateto treat Mefloquine/chloroquine/S-Presistant P.falciparumDoxycycline 100 mg/day – 2nd lineprophylactic for travellers
  25. 25. ARTEMISININDERIVATIVESShort acting drug
  26. 26. Lysis in the parasiteInhibits protein synthesisDamages ERCauses lipid peroxidationBinds with membrane proteinReleases free radicalsHaeme interacts with Endoperoxide bridge in artemisinin
  27. 27. ArtesunateProdrug(t½ - 30-60 min)Active metabolite –Dihydroartemisinin(t½ - 2-4 hrs)Oral , i.v., i.m.ArtemetherProdrug(t½ - 3-10 hrs)α/β Arteethert ½ - 23 hrsPHARMACOKINETICS
  28. 28. Adverse effectNausea, vomitng, abd. Pain, itching & drugfeverAbnormal bleeding, dark urine, ST segmentchanges, QT prolongation, 1* A-V blockTransient reticulopenia & leucopeniaUsesOrally – uncomplicated chloroquine/multidrug resistant P.falciparum malariaParenterally - severe & complicatedP.falciparum malaria
  29. 29. ARTEMISININ-BASED COMBINATIONTHERAPY(ACT)
  30. 30. • Artesunate 100 mg BD x 3days + Mefloquine 750 mg on2nd day & 500 mg on 3rd dayArtesunate -Mefloquine• Artemether 80 mg BD +Lumefantrine 480 mg BD x 3daysArtemether-Lumefantrine• Artesunate 100 mg BD x 3 day+ Sulfadoxine 1500 mg +pyrimethamine 75 mg singledoseArtesunate-sulfadoxine +Pyrimethamine
  31. 31. Thank U…!

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