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ANTI MALARIAL.pptx
This document discusses various anti-malarial drugs used for treatment, prophylaxis, and prevention of malaria, which is caused by protozoan parasites of the Plasmodium genus. It outlines the drug classifications, mechanisms of action, pharmacodynamics, and potential adverse effects of commonly used anti-malarials like chloroquine, mefloquine, and artemisinin derivatives. Additionally, it emphasizes nursing implications for monitoring and ensuring proper adherence to treatment regimens.
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ANTI MALARIAL.pptx
- 1. ANTI- MALARIAL DRUGS NEHA BHARTI M.Sc. N(MEDICALSURGICAL NURSING) NURSING TUTOR, SMVDCoN
- 2. MALARIA • It isan infectious disease of humans caused by parasitis protozoans belonging to the genus plasmodium. • It is endemic in most parts of India and other tropical countries. • As per WHO, malaria causes one death every minute globally and about 40,000 annual deaths in India.
- 3. • The diseaseis transmitted by the bite of an infected female Anopheles mosquito. • Four species of protozoa plasmodium can cause malaria which are P. falciparum, P. vivax, P. ovale and P. malariae.
- 4. INTRODUCTION • These arethe drugs which are used for the treatment, prophylaxis and prevention of relapses of malaria. • The treatment of malaria is available since 17 century. During those times, the bark of Cinchona tree was used in the crude form. • Later in 1820, quinine was isolated from the bark. • Since 1920, quinine and other drugs are commercially available in the market
- 5. OBJECTIVES IN USEOF ANTIMALARIAL DRUGS • The various objectives are: To prevent clinical attack of malaria. To treat clinical attack of malaria. To completely eradicate the parasite from the patient’s body. To cut down human to mosquito transmission.
- 7. THERAPEUTIC CLASSIFICATION 1. CAUSALPROPHYLACTICS: (Destroy parasite in liver cells and prevent invasion of erythrocytes) e.g. primaquine, pyrimethamine 2.BLOOD SCHIZONTOCIDES SUPPRESIVES (destroy parasites in the RBC and terminate clinical attacks of malaria): e.g. chloroquine, quinine, mefloquine, halofantrine, pyrimethamine 3. TISSUE SCHIZONTOCIDES used to prevent relapse: act vivax and P. ovale that produce replapses. E.g. primaquine 4. GAMETOCIDAL DRUGS: primaquine, chloroquine, quinine.
- 8. CLASSIFICATION OF ANTIMALARIAL DRUGS 1. CHLOROQUINE 2PRIMAQUIN 3. MEFLOQUIN 6. ARTEMETHER 4. PYRIMETHAMINE 5. PROGUANOIL
- 9. 1. CHLOROQUINE • Itacts as erythrocytic schizontocide against all species of plasmodia. • The parasite disappears from peripheral blood in 1-3 days. It control the clinical attacks of malaria within 1-2 days.
- 10. • It doesn’thave any gametocidal activity. • It is bitter in taste, so patient should be advised ‘not to chew the tablet’ it is used for the treatment of malaria during pregnancy: no teratogenic effects have been reported.
- 11. MECHANISM OF ACTION Itsgets concentrated in the infected RBCs and then is actively taken up by the susceptible plasmodia. The chloroquine binds to the heme and forms chloroquine heme complex. Complex inhibits the formation of hemozoin and also damages the Plasmodium memberane
- 12. PHARMACOKINETICS • It iswell absorbed orally. • 50% of the drug is plasma protein bound, gets concentrated in liver, spleen, kidneys, lungs, skin and leukocytes. • The plasma half life is 3-10 days, whereas the terminal half life is 1-2 months. On prolonged use, it gets accumulated selectively in the retina and causes ocular toxicity. • It is partially metabolized in liver and slowly excreted in urine.
- 13. INDICATIONS ADVERSE EFFECTS •Clinical drug of choice for malaria. • Extraintestinal amoebiasis. • Rheumatoid arthritis • Infectious mononucleosis. • Mild side effects like nausea, vomiting, anorexia, uncontrollable itching, epigastric pain, uneasiness are quite frequent. • On prolonged use, it may lead to loss of vision.
- 14. 1.i. AMODIAQUINE Amodiaquine ishaving similar properties to chloroquin, except: • It is fast acting and less bitter in taste. • It is useful in uncomplicated falciparum malaria. • In combination with artesunate, it is the first line treatment of falciparum malaria.
- 15. • Itching isless common with it, other side effects are same as that of chloroquine. • It is given in a dose of 25-30mg/kg over 3 days for the treatment of acute attack of malaria.
- 16. 2. PRIMAQUINE • Itis a poor erythrocytic schizontocide but more active against P. falciparum. • It differs from all other available antimalarial in having an additional effect on primary as well as secondary hepatic phases on the malarial parasite. • It also highly active against gametocytes.
- 17. • Mechanism OfAction is not clearly known. • Pharmacokinetics: it is given orally and has rapid and complete absorption. • Metabolized in liver and excreted slowly in urine. Its half life is 6-8 hours and excreted in urine within 24 hrs.
- 18. INDICATIONS ADVERSE EFFECTS •Indicated for radical cure of relapsing malaria caused by P. Ovale and P. Vivax. In India 15mg/day for 2 weeks is given along with full curative dose of Chloroquine . • Falciparum malaria: a single 45 mg dose of primaquine is given with the curative dose of chloroquine to kill the gametes and cut down transmission to mosquito. • Mild side eefcts are Nausea, Vomiting, Anorexia and epigastric pain. • It should not be given in pregnancy, because the fetus is deficient in G6PD.
- 19. 3. MEFLOQUINE • Mefloquineis a fast acting erythrocytic schizontocide, but slower than chloroquine. • It is effective against choloquine sensitive as well as resistant Plasmodium. • It has good activity against Chloroquine resistant P. falciparum.
- 20. • It isbitter in taste, so patient should be advised ‘not to chew the tablet’ MECHANISM OF ACTION: Similar to chloroquine, it accumulates in the infected RBC’s binds to hence and this complex damages the cell memberanes of parasite.
- 21. PHARMACOKINETICS • It isgiven orally and is absorbed very slowly. • It is highly plasma protein bound and gets concentrated in various organs such as liver, lungs and intestine. • It is metabolized in liver and excreted in bile. • It’s half life is long i.e. 2-3 weeks
- 22. INDICATIONS ADVERSE EFFECTS •Multi drug resistance P. Falciparum malaria. • In conbination of artesunate based combination therapy for uncomplicated falciparum including chloroquine resistant and chloroquine+sulfa pyrimethamine resistant cases. • For the prophylaxis of malaria among travellers to areas with multidrug resistance;5mg/kg(adults 250mg) per week is started preferably 1-2 weeks before travel. • Mild side effects are Nausea, Vomiting, anorexia, epigastric pain. • Some patients may experience neuropsychiatric reactions i.e. disturbed sense of balance, ataxia, errors in operating machinery, These reactions subside after 2-3 weeks of discontinuation of treatment.
- 23. 4. PYRIMETHAMINE • Itis a slow acting erythrocytic schizontocide for P. Falciparum.. • It has good but slow oral absorption. • It is more potent and relatively safer than Proguanil. • It is excreted slowly in nature. • It is used in combination with sulfonamide for chloroquine resistant P.Falciparum.
- 24. 5. PROGUANIL • Itis pre erythrocytic schizontocide for P. Falciparum and erythrocytic schizontocide for both P. Falciparum and P. Vivax. • It is a prodrug and the active metabolite is cycloguanil. • MECHANISM OF ACTION: It inhibits the plasmodial dihydrofolate reductase thymidylate synthase in parasite, thereby exerting the cidal effect.
- 25. • PHARMACOKINETICS: Itis given orally and having slow but complete absorption. It is metabolized in liver and excreted in urine. Its half life is 16-20 hours.
- 26. • ADVERSE EFFECTS:It is well tolerated with mild abdominal discomfort. Rarely vomiting, stomatitis, hematuria, rashes and transient loss of hair may be seen. • INDICATIONS: It is used in prophylaxis and treatment of Chloroquine resistant P. Falciparum malaria.
- 27. 6. ARTEMISININ DERIVATIVES •It is the active ingredient of the chinese traditional medicine ‘Quinghaosu’ which is obtained from the planet Artemisia Annua. • Ms Tu YOUYOU was awarded half nobel prize in 2015 for the discovery of Artemisinin.
- 28. • These derivativesare better tolerated, safer and highly efficacious. • They are very potent and rapidly acting anti-malarial drugs. • They also have good gametocidal activity but do not affect hepatic forms. • They are effective in erythrocytic stage of all malarial parasites.
- 29. • MECHANISM OFACTION: Exact mechanism is unknown. • INDICATIONS: Uncomplicated falciparum malaria. Severe and complicated falciparum malaria.
- 30. ADVERSE EFFECTS: • Mildside effects are nausea, vomiting, • Abdominal pain, itching
- 31. PHARMACOKINETICS • Artemether islipid soluble and is administered by oral or IM administration only.
- 32. QUININE • It isan erythrocyte schizontocide for all species of plasmodia. • It is effective against Chloroquine and multidrug resistance strains of P. falciparum. • It is less effective and more toxic than chloroquine. • Mechanism of action is same that of chloroquine. • PHARMACOKINETICS: It is given orally and is absorbed rapidly and completely. It is 70% plasma protein bound. It is metabolized in liver and excreted in bile. Its half life is 10-12 hrs.
- 33. INDICATIONS • Uncomplicated Chloroquineresistant P. Fa,ciparum malaria. • Complicated malaria
- 34. ADVERSE EFFECTS • Theadverse effects are generally dose related. • Mild side effects are Nausea, vomiting, anorexia, epigastric pain. • At higher doses, Patient experiences nausea vomiting, headache, tinnitus, vertigo, visual defects and mental confusions.
- 35. PROPHYLACTIC THERAPY IN INDIA •DOXYCYCLINE 100mg daily starting ‘day before travelling to endemic areas and taken ‘till 4 weeks after return from endemic area’ for chloroquine resistant P. Falciparum. • MEFLOQUINE 250mg started 1-2 weeks before and taken weekly till 4 weeks return from endemic area has been used for areas where Chloroquine resistant P. Falciparum is prevelant. • In India, use of mafloquine for prophylaxis is not allowed among indians residen, but may be used by forein travellers.
- 36. NURSING IMPLICATIONS • Nurseshould enquire the patient about unusual visual and auditory sensations. • Drug should be given with food to decrease the GI irritation. • Monitoring of urine output is mandatory during antimalarial therapy because it leads to renal damage. • Closely monitor the vital signs. • Closely monitor the blood glucose levels in patients receiving quinine therapy, as rapid iv injection can cause hypoglycemia. • Nurse should check that antimalarial regimen is followed properly.