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Cestodes
Nematodes
Trematodes
Helminthes
Anthelmintics
Vermicide
Vermifuge
Mebendazole
Benzimidazole ,
Broad spectrum activity ,
It produced nearly 100% cure rates in egg counts
in roundworms , hookworms ,
enterobius , trichuris infestation .
But H.Nana is insensitivity .
Mech. Of Action
Blocks glucose uptake
Binds with β tubulin & inhibits
microtubules polymerization
Minimal intestinal absorption
75 – 90 % of an oral dose is passed in the faeces
First pass metabolism
Pk
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,
USES…
• 100 mg BD x 3 daysRound worms
Ascaris lumbricoides
• 100 mg BD x 3 daysHook worm
Ancylocystoma duodenale
Necator americanus
• 100 mg OD x 2-3 wksThread worm
Enterobius vermicularis
• 100 mg BD x 3 daysWhip worm
Trichuris trichura
As first choice of drug…
As Alternative drug…
• 200 mg BD x 4 days
Whipworm
Trichinella sprialis
• 200-400 mg BD/TDS x 3-4 wk
Dog tapeworm
Hydatid disease
Albendazole
Congener of mebendazole
One dose treatment has cure rates in ascariasis, hook
worm, enterobius
3 day treatment has cure rate in H.nana
MOA – similar to mebendazole
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
Adv. effects
Well tolerated
G.I. side effects
Dizziness
Prolonged use in hydatid & cysticercosis –
headache, fever, alopecia, neutropenia, jaundice
C/I
 Occular cysticercosis
Uses…
• 400 mg single dose(adults)
• 200 mg single dose(1-2 yrs)
Round worms
Ascaris lumbricoides
• 400 mg single dose(adults)
• 200 mg single dose(1-2 yrs)
Hook worm
Ancylocystoma duodenale
Necator americanus
• 400 mg single dose(adults)
• 200 mg single dose(1-2 yrs)
Thread worm
Enterobius vermicularis
As first choice of drug…
• 400 mg OD x 3 daysWhipworm
Trichinella spiralis
• 400 mg BD x 8-15 days
• Paed. Dose -15 mg/kg/day
Tapeworm
Neurocysticercosis
• 400 mg BD x 4 wks
• Repeat 2-3 wks if requried
• Upto 3 courses
Dog tapeworm
hydatid disease
As Alternative drug…
Thread worm-Strongyloides stercoralis
400 mg single dose(adults) & 200 mg single dose(1-2 yrs)
Whipworm-Trichuris trichura
400 mg single dose(adults) & 200 mg single dose(1-2 yrs)
Filariasis
Tapeworm
Taenia saginata,taenia solium
THIOBENDAZOLE
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
USES…
Symptomatic relief in
 Cutaneous larvae migrans
 Guinea worm disease
In Strongyloidosis & Trichinosis
DOSE:
 25 mg/kg/day – 2 divided dose - after meals
 Chewable tablets
Pyrantel
Pamoate
 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 .
Mech. Of Action
Contracture & Spastic Paralysis of worm
Persistant Depolarization
Activation of nicotinic cholinergic receptors in worm
USES…
• Singledose of 10mg/kg is
required
Round worm
Ascaris lumbricoides
• Singledose of 10mg/kg is
required
Hook worm
Ancylocstoma
duodenale
• Singledose of 10mg/kg
is required
Thread worm
Enterobius
vermicularis
AS FIRST CHOICE OF DRUG,
PIPERAZINE
It highly active drugs against ascaris ,
enterobius .
It safe during Pregnancy .
Mech. Of action
Flaccid paralysis & Expels alive worms
Hyperpolarization & Relaxation of ascaris muscle
Gaba agonistic action openning cl- channels
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 to
Resp. failure
C/I
 Renal insufficiency , epileptics .
Uses…
As second choice of drug ,
• 4g OD x 2 day(A)
• 0.75g/years of age(C)
Round worm
Ascaris
lumbricoides
• 50 mg/kg OD x 7 Days
Thread worm
Enterobius
vermicularis
Levamisole &
Tetramisole
Both are active against many nematodes , but use
is restricted to ascariasis & ancylocystomiasis.
Mech. Of action
 Ganglia in worms are stimulated causing tonic
paralysis & expulsion of live worms .
 Interfere with carbohydrate metabolism –
inhibition of fumarate reductase also contributing .
 Nausea, Abd. Pain, gudiness, fatigue .
Adv. effects
Uses...
As second choice of drug,
Round worm – Ascaris lumbricoides
• Single dose - 50mg ( C )
Hook worm – Ancylocystoma duodenale
• Single dose – 150mg ( A )
Diethyl Carbamazine
Citrate
[ DEC]
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
Mech. Of action
• Alternation of Mf membrane
Phagocytosed by tissue fixed monocytes
• But not by circulating phagocytes.
• Affect muscular activity and cause
hyperpolarisation due to piperazine
moiety.
Adv. effects
Nausea, headache, loss of appetite, weakness,
dizziness .
Febile reaction with rash, lymphnode enlargement,
Bp .
 leukocytosis , mild albiminuria .
Uses …
Filariasis – Wucharia bancrofti
• 2mg/kg TDS – Rapid symptomatic Relief
Tropical eosinophilia
• 2 – 4mg/kg TDS x 2-3 wks
Loa loa & o.volvulus – but it give 25-
50mg test dose to avoid severe
reations to dying .
Ivermecti
n
Potent semisynthetic derivative
Obtained from Streptomyces avermitilis
Mech. Of action
Tonic paralysis
Acts via glutamate gated Cl˜ channels
PK
 Orally absorbed
 Wide distribution
 T½ - 2-3 days
Adv. Eff.
 Pruritis
 Nausea
 Abd. Pain
 Constipation
 Lethargy
 Transient ECG changes
USES…
Thread worm-Strongyloides stercoralis
Filaria-Wucheria bancroftia
Cutaneous larvae migrans & River Blindness
ascariasis
Scabies & pediculosis – In orally
Praziquantel
Novel anthelmintic
Active against Schistosomes ,Trematodes & Cestodes
Mech. Of action
worm loses its grip in git & expelled out
Contracture & Paralysis
Acts by causing leakage of IC Ca from the membrane
PK
 Rapidly absorbed from intestine , T½ - 1.5 hours
 First pass metabolism , excreted in urine
 Along with food, absorbtion
 Enzyme inducers - metabolism
Adv. Eff.
 No systemic toxicity
 Bitter in taste – nausea & abd. Pain
 Head ache, dizziness & sedation
 rashes, urticaria, fever, itching & body pain
C/I - Occular cysticercosis
USES…. • T.saginata,T.solium-10 mg/kg single dose in
morning
• H.nana,D.latum-15-25 mg/kg single dose in
morning
• In heavy infestation, retreatment aft. a week
is desirable
Tapeworm
• First to be effective-2nd drug of choice
• 50-100 mg/kg daily in 3 doses x 15 days
Neurocysticercosis
• 40-75 mg/kg once as single/divided
dose
Schistosomes
• DOC for fluke infestations except Fasciola
hepatica
• 75 mg/kg/day x one/two days
Others flukes
NICLOSAMIDE
 It effective against cestodes infesting man –
T.saginata , T.sollium , D.latum , H.nana , thread
worm .
 It safe during pregnancy
Mech. Of action
Cause injury & partly digested in the intestine
Interfere with anaerobic generation of ATP by the tapeworm
Inhibit oxydative phosphorylation in mitochondria
Adv. effects
 Tasteless & non irritating
 No systemic toxicity
 Minor abd. Symptoms
 Malaise, pruritis, light headedness
Uses
 As 1st line drug – T.saginata
 As 2nd line drug – T.sollium
Treatment of
Neurocysticercosis
 Causative agent: T.solium
 Due to: migration of larvae from gut to various tissue via
blood stream.
 On anthelmintic treatment ,the larvae dies and its
product induce an intense focal reaction results in
seizures and other neurological symptoms.
 Treatment :
 Albendazole and Praziquantel.
 Corticosteroids
 Anti-convulsants.
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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ANTI-HELMINTHIC DRUGS

  • 4.
  • 6. Benzimidazole , Broad spectrum activity , It produced nearly 100% cure rates in egg counts in roundworms , hookworms , enterobius , trichuris infestation . But H.Nana is insensitivity .
  • 7. Mech. Of Action Blocks glucose uptake Binds with β tubulin & inhibits microtubules polymerization
  • 8. Minimal intestinal absorption 75 – 90 % of an oral dose is passed in the faeces First pass metabolism Pk
  • 9. 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,
  • 11. • 100 mg BD x 3 daysRound worms Ascaris lumbricoides • 100 mg BD x 3 daysHook worm Ancylocystoma duodenale Necator americanus • 100 mg OD x 2-3 wksThread worm Enterobius vermicularis • 100 mg BD x 3 daysWhip worm Trichuris trichura As first choice of drug…
  • 12. As Alternative drug… • 200 mg BD x 4 days Whipworm Trichinella sprialis • 200-400 mg BD/TDS x 3-4 wk Dog tapeworm Hydatid disease
  • 14. Congener of mebendazole One dose treatment has cure rates in ascariasis, hook worm, enterobius 3 day treatment has cure rate in H.nana MOA – similar to mebendazole
  • 15. 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
  • 16. Adv. effects Well tolerated G.I. side effects Dizziness Prolonged use in hydatid & cysticercosis – headache, fever, alopecia, neutropenia, jaundice C/I  Occular cysticercosis
  • 18. • 400 mg single dose(adults) • 200 mg single dose(1-2 yrs) Round worms Ascaris lumbricoides • 400 mg single dose(adults) • 200 mg single dose(1-2 yrs) Hook worm Ancylocystoma duodenale Necator americanus • 400 mg single dose(adults) • 200 mg single dose(1-2 yrs) Thread worm Enterobius vermicularis As first choice of drug…
  • 19. • 400 mg OD x 3 daysWhipworm Trichinella spiralis • 400 mg BD x 8-15 days • Paed. Dose -15 mg/kg/day Tapeworm Neurocysticercosis • 400 mg BD x 4 wks • Repeat 2-3 wks if requried • Upto 3 courses Dog tapeworm hydatid disease
  • 20. As Alternative drug… Thread worm-Strongyloides stercoralis 400 mg single dose(adults) & 200 mg single dose(1-2 yrs) Whipworm-Trichuris trichura 400 mg single dose(adults) & 200 mg single dose(1-2 yrs) Filariasis Tapeworm Taenia saginata,taenia solium
  • 22. 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
  • 23. USES… Symptomatic relief in  Cutaneous larvae migrans  Guinea worm disease In Strongyloidosis & Trichinosis DOSE:  25 mg/kg/day – 2 divided dose - after meals  Chewable tablets
  • 25.  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 .
  • 26. Mech. Of Action Contracture & Spastic Paralysis of worm Persistant Depolarization Activation of nicotinic cholinergic receptors in worm
  • 28. • Singledose of 10mg/kg is required Round worm Ascaris lumbricoides • Singledose of 10mg/kg is required Hook worm Ancylocstoma duodenale • Singledose of 10mg/kg is required Thread worm Enterobius vermicularis AS FIRST CHOICE OF DRUG,
  • 30. It highly active drugs against ascaris , enterobius . It safe during Pregnancy . Mech. Of action Flaccid paralysis & Expels alive worms Hyperpolarization & Relaxation of ascaris muscle Gaba agonistic action openning cl- channels
  • 31. 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 to Resp. failure C/I  Renal insufficiency , epileptics .
  • 32. Uses… As second choice of drug , • 4g OD x 2 day(A) • 0.75g/years of age(C) Round worm Ascaris lumbricoides • 50 mg/kg OD x 7 Days Thread worm Enterobius vermicularis
  • 34. Both are active against many nematodes , but use is restricted to ascariasis & ancylocystomiasis. Mech. Of action  Ganglia in worms are stimulated causing tonic paralysis & expulsion of live worms .  Interfere with carbohydrate metabolism – inhibition of fumarate reductase also contributing .  Nausea, Abd. Pain, gudiness, fatigue . Adv. effects
  • 35. Uses... As second choice of drug, Round worm – Ascaris lumbricoides • Single dose - 50mg ( C ) Hook worm – Ancylocystoma duodenale • Single dose – 150mg ( A )
  • 37. 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
  • 38. Mech. Of action • Alternation of Mf membrane Phagocytosed by tissue fixed monocytes • But not by circulating phagocytes. • Affect muscular activity and cause hyperpolarisation due to piperazine moiety.
  • 39. Adv. effects Nausea, headache, loss of appetite, weakness, dizziness . Febile reaction with rash, lymphnode enlargement, Bp .  leukocytosis , mild albiminuria .
  • 40. Uses … Filariasis – Wucharia bancrofti • 2mg/kg TDS – Rapid symptomatic Relief Tropical eosinophilia • 2 – 4mg/kg TDS x 2-3 wks Loa loa & o.volvulus – but it give 25- 50mg test dose to avoid severe reations to dying .
  • 42. Potent semisynthetic derivative Obtained from Streptomyces avermitilis Mech. Of action Tonic paralysis Acts via glutamate gated Cl˜ channels
  • 43. PK  Orally absorbed  Wide distribution  T½ - 2-3 days Adv. Eff.  Pruritis  Nausea  Abd. Pain  Constipation  Lethargy  Transient ECG changes
  • 44. USES… Thread worm-Strongyloides stercoralis Filaria-Wucheria bancroftia Cutaneous larvae migrans & River Blindness ascariasis Scabies & pediculosis – In orally
  • 46. Novel anthelmintic Active against Schistosomes ,Trematodes & Cestodes Mech. Of action worm loses its grip in git & expelled out Contracture & Paralysis Acts by causing leakage of IC Ca from the membrane
  • 47. PK  Rapidly absorbed from intestine , T½ - 1.5 hours  First pass metabolism , excreted in urine  Along with food, absorbtion  Enzyme inducers - metabolism Adv. Eff.  No systemic toxicity  Bitter in taste – nausea & abd. Pain  Head ache, dizziness & sedation  rashes, urticaria, fever, itching & body pain C/I - Occular cysticercosis
  • 48. USES…. • T.saginata,T.solium-10 mg/kg single dose in morning • H.nana,D.latum-15-25 mg/kg single dose in morning • In heavy infestation, retreatment aft. a week is desirable Tapeworm • First to be effective-2nd drug of choice • 50-100 mg/kg daily in 3 doses x 15 days Neurocysticercosis • 40-75 mg/kg once as single/divided dose Schistosomes • DOC for fluke infestations except Fasciola hepatica • 75 mg/kg/day x one/two days Others flukes
  • 50.  It effective against cestodes infesting man – T.saginata , T.sollium , D.latum , H.nana , thread worm .  It safe during pregnancy Mech. Of action Cause injury & partly digested in the intestine Interfere with anaerobic generation of ATP by the tapeworm Inhibit oxydative phosphorylation in mitochondria
  • 51. Adv. effects  Tasteless & non irritating  No systemic toxicity  Minor abd. Symptoms  Malaise, pruritis, light headedness Uses  As 1st line drug – T.saginata  As 2nd line drug – T.sollium
  • 53.  Causative agent: T.solium  Due to: migration of larvae from gut to various tissue via blood stream.  On anthelmintic treatment ,the larvae dies and its product induce an intense focal reaction results in seizures and other neurological symptoms.  Treatment :  Albendazole and Praziquantel.  Corticosteroids  Anti-convulsants.
  • 54. Advantages of albendazole over praziquantel  Short course of treatment  High cure rate  Corticosteroiods enhances the absorption of albendazole.  Albendazole is cheaper.