ANTI-HELMINTHIC DRUGS

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ANTI-HELMINTHIC DRUGS

  1. 1. BYSV.VIVEK
  2. 2. CestodesNematodesTrematodesHelminthes
  3. 3. AnthelminticsVermicideVermifuge
  4. 4. Mebendazole
  5. 5. Benzimidazole ,Broad spectrum activity ,It produced nearly 100% cure rates in egg countsin roundworms , hookworms ,enterobius , trichuris infestation .But H.Nana is insensitivity .
  6. 6. Mech. Of ActionBlocks glucose uptakeBinds with β tubulin & inhibitsmicrotubules polymerization
  7. 7. Minimal intestinal absorption75 – 90 % of an oral dose is passed in the faecesFirst pass metabolismPk
  8. 8. Adverse effect• Diarrhoea ,• Nausea ,• Abd. Pain .In heavy infestation cases,• Granulocytopenia ,• Allergic reaction ,• Loss of hair .In high dose,• Expulsion of ascaris – mouth & nose .Due to starvation & slow death,
  9. 9. USES…
  10. 10. • 100 mg BD x 3 daysRound wormsAscaris lumbricoides• 100 mg BD x 3 daysHook wormAncylocystoma duodenaleNecator americanus• 100 mg OD x 2-3 wksThread wormEnterobius vermicularis• 100 mg BD x 3 daysWhip wormTrichuris trichuraAs first choice of drug…
  11. 11. As Alternative drug…• 200 mg BD x 4 daysWhipwormTrichinella sprialis• 200-400 mg BD/TDS x 3-4 wkDog tapewormHydatid disease
  12. 12. Albendazole
  13. 13. Congener of mebendazoleOne dose treatment has cure rates in ascariasis, hookworm, enterobius3 day treatment has cure rate in H.nanaMOA – similar to mebendazole
  14. 14. PKModerate oral administrationWidely distributed in bodyIt enters brainFirst pass metabolismExcreted in urineT½ - 8.5 hrsAlong with fatty meals,  absorbtion
  15. 15. Adv. effectsWell toleratedG.I. side effectsDizzinessProlonged use in hydatid & cysticercosis –headache, fever, alopecia, neutropenia, jaundiceC/I Occular cysticercosis
  16. 16. Uses…
  17. 17. • 400 mg single dose(adults)• 200 mg single dose(1-2 yrs)Round wormsAscaris lumbricoides• 400 mg single dose(adults)• 200 mg single dose(1-2 yrs)Hook wormAncylocystoma duodenaleNecator americanus• 400 mg single dose(adults)• 200 mg single dose(1-2 yrs)Thread wormEnterobius vermicularisAs first choice of drug…
  18. 18. • 400 mg OD x 3 daysWhipwormTrichinella spiralis• 400 mg BD x 8-15 days• Paed. Dose -15 mg/kg/dayTapewormNeurocysticercosis• 400 mg BD x 4 wks• Repeat 2-3 wks if requried• Upto 3 coursesDog tapewormhydatid disease
  19. 19. As Alternative drug…Thread worm-Strongyloides stercoralis400 mg single dose(adults) & 200 mg single dose(1-2 yrs)Whipworm-Trichuris trichura400 mg single dose(adults) & 200 mg single dose(1-2 yrs)FilariasisTapewormTaenia saginata,taenia solium
  20. 20. THIOBENDAZOLE
  21. 21. First benzimidazole polyanthelminticIt inhibits development of eggs of worms & kills larvaeIt has analgesic,antiinflammatory & antipyretic actionMOA-similar as mebendazolePK-well absorbed from GI tractAdv. eff.-nausea,vomiting,loss of appetite,giddiness,itching,abd. pain,diarrhoea
  22. 22. USES…Symptomatic relief in Cutaneous larvae migrans Guinea worm diseaseIn Strongyloidosis & TrichinosisDOSE: 25 mg/kg/day – 2 divided dose - after meals Chewable tablets
  23. 23. PyrantelPamoate
  24. 24.  It was introduced for thread worm infestation in children ;use soon extend to roundworm , hook worm. It inactive against trichuris & other worms. Piperazine antagonizes the action of pyrantel Pamoate.Pk - 10-15% of an oral dose is absorbed.Adv. Effects – G.I symptoms, headache,dizziness, tasteless .
  25. 25. Mech. Of ActionContracture & Spastic Paralysis of wormPersistant DepolarizationActivation of nicotinic cholinergic receptors in worm
  26. 26. USES…
  27. 27. • Singledose of 10mg/kg isrequiredRound wormAscaris lumbricoides• Singledose of 10mg/kg isrequiredHook wormAncylocstomaduodenale• Singledose of 10mg/kgis requiredThread wormEnterobiusvermicularisAS FIRST CHOICE OF DRUG,
  28. 28. PIPERAZINE
  29. 29. It highly active drugs against ascaris ,enterobius .It safe during Pregnancy .Mech. Of actionFlaccid paralysis & Expels alive wormsHyperpolarization & Relaxation of ascaris muscleGaba agonistic action openning cl- channels
  30. 30. Pk Moderate oral absorption , Partly metabolized in liver & excreted in urine .Adv. Effects Nausea, vomiting, abd. Discomfort, utricaria High dose – dizziness, excitement Toxic dose – convulsions, paralysis due toResp. failureC/I Renal insufficiency , epileptics .
  31. 31. Uses…As second choice of drug ,• 4g OD x 2 day(A)• 0.75g/years of age(C)Round wormAscarislumbricoides• 50 mg/kg OD x 7 DaysThread wormEnterobiusvermicularis
  32. 32. Levamisole &Tetramisole
  33. 33. Both are active against many nematodes , but useis restricted to ascariasis & ancylocystomiasis.Mech. Of action Ganglia in worms are stimulated causing tonicparalysis & expulsion of live worms . Interfere with carbohydrate metabolism –inhibition of fumarate reductase also contributing . Nausea, Abd. Pain, gudiness, fatigue .Adv. effects
  34. 34. Uses...As second choice of drug,Round worm – Ascaris lumbricoides• Single dose - 50mg ( C )Hook worm – Ancylocystoma duodenale• Single dose – 150mg ( A )
  35. 35. Diethyl CarbamazineCitrate[ DEC]
  36. 36. It is the 1st drug for fillariasis .It highly selective effect on microfilariae .PkWell oral absorptionWidely distributed in the bodyMetabolized in liver & excreted in urinePlasma t½ - 4 -12 hrs
  37. 37. Mech. Of action• Alternation of Mf membranePhagocytosed by tissue fixed monocytes• But not by circulating phagocytes.• Affect muscular activity and causehyperpolarisation due to piperazinemoiety.
  38. 38. Adv. effectsNausea, headache, loss of appetite, weakness,dizziness .Febile reaction with rash, lymphnode enlargement,Bp . leukocytosis , mild albiminuria .
  39. 39. Uses …Filariasis – Wucharia bancrofti• 2mg/kg TDS – Rapid symptomatic ReliefTropical eosinophilia• 2 – 4mg/kg TDS x 2-3 wksLoa loa & o.volvulus – but it give 25-50mg test dose to avoid severereations to dying .
  40. 40. Ivermectin
  41. 41. Potent semisynthetic derivativeObtained from Streptomyces avermitilisMech. Of actionTonic paralysisActs via glutamate gated Cl˜ channels
  42. 42. PK Orally absorbed Wide distribution T½ - 2-3 daysAdv. Eff. Pruritis Nausea Abd. Pain Constipation Lethargy Transient ECG changes
  43. 43. USES…Thread worm-Strongyloides stercoralisFilaria-Wucheria bancroftiaCutaneous larvae migrans & River BlindnessascariasisScabies & pediculosis – In orally
  44. 44. Praziquantel
  45. 45. Novel anthelminticActive against Schistosomes ,Trematodes & CestodesMech. Of actionworm loses its grip in git & expelled outContracture & ParalysisActs by causing leakage of IC Ca from the membrane
  46. 46. PK Rapidly absorbed from intestine , T½ - 1.5 hours First pass metabolism , excreted in urine Along with food, absorbtion Enzyme inducers - metabolismAdv. Eff. No systemic toxicity Bitter in taste – nausea & abd. Pain Head ache, dizziness & sedation rashes, urticaria, fever, itching & body painC/I - Occular cysticercosis
  47. 47. USES…. • T.saginata,T.solium-10 mg/kg single dose inmorning• H.nana,D.latum-15-25 mg/kg single dose inmorning• In heavy infestation, retreatment aft. a weekis desirableTapeworm• First to be effective-2nd drug of choice• 50-100 mg/kg daily in 3 doses x 15 daysNeurocysticercosis• 40-75 mg/kg once as single/divideddoseSchistosomes• DOC for fluke infestations except Fasciolahepatica• 75 mg/kg/day x one/two daysOthers flukes
  48. 48. NICLOSAMIDE
  49. 49.  It effective against cestodes infesting man –T.saginata , T.sollium , D.latum , H.nana , threadworm . It safe during pregnancyMech. Of actionCause injury & partly digested in the intestineInterfere with anaerobic generation of ATP by the tapewormInhibit oxydative phosphorylation in mitochondria
  50. 50. Adv. effects Tasteless & non irritating No systemic toxicity Minor abd. Symptoms Malaise, pruritis, light headednessUses As 1st line drug – T.saginata As 2nd line drug – T.sollium
  51. 51. Treatment ofNeurocysticercosis
  52. 52.  Causative agent: T.solium Due to: migration of larvae from gut to various tissue viablood stream. On anthelmintic treatment ,the larvae dies and itsproduct induce an intense focal reaction results inseizures and other neurological symptoms. Treatment : Albendazole and Praziquantel. Corticosteroids Anti-convulsants.
  53. 53. Advantages of albendazole over praziquantel Short course of treatment High cure rate Corticosteroiods enhances the absorption of albendazole. Albendazole is cheaper.

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