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Prof. Shaikh Abusufiyan
Assistant Professor,
AIKTC-School of Pharmacy,
New Panvel-410206
Anthelminthic Drugs
Pharma Learning Forever
At the end of this e-learning session you are able to…
A. Discuss type of helminths.
B. Explain pharmacology of
Anthelminthic Drugs.
Activity I: Self learning of e-content
● Many human harbour --> helminths (Worms) of one
species or another.
● In some cases these infection --> results mainly in
discomfort and do not cause ill health. eg. Threadworms
in children.
● Other worm infections, such as Schistosomiasis and
hookworm disease --> can produce very serious
morbidity.
Sexual reproduction of worms:
● Most worm reproduce sexually in human host (Primary
host)
Produces egg or larvae
When passes out the body
it infect the secondary host
Type of worm infections
Those in which
1. worm lives in alimentary canal
2. worms lives in other tissue of the host body
Worm lives in alimentary canal
1. Tapeworm (Cestodes)
The usual intermediate hosts of tapeworm are
● cattle
● pigs
● and fresh water fish.
● Human become infected --> by eating raw or under
cooked meat of these animals or fishes.
2. Intestinal Round worms (Nematodes): 4 types
1. Common round worm
2. Thread worm
3. Whipe-worm
4. Hookworms
Worms lives in the host tissues
1. Trematodes or flukes:
• Infection caused by trematodes or flukes is
called as Schistosomiasis (bilharzia).
2. Tissue round worms: are of 2 types
a. Guinea worms
b. Filariae worms
a. Guinea worms
●The gravid female migrate to the S.C tissues of the leg
or the foot and protrude through an ulcer in the
skin.
●The worm may be up to a meter in length and has to
be removed surgically
●Or by slow mechanical windning of the worm on to the
stick over a period of days.
b. Filariae worm:
● Major filarial disease are caused by wuchereria
which caused obstruction of the lymphatic vessels
producing elephantiasis.
Q&A: Activity II
Q.1 Enlist types of worm infection.
Q.2 Name worm which migrate to the S.C
tissues of the leg or the foot and protrude
through an ulcer in the skin?
Q.3 How Filariae worm causes
elephantiasis.
Anthelmintic Drugs
● To be an effective anthelmintic drugs
● it must be able to --> penetrate the cuticle of the
worms
● or gain access --> to alimentary tract.
• Limitation: This lead to difficulties for the design of
good anthelmintic drugs.
● Some worms are exclusively --> haemophagous
(blood eating) while other are tissue gazers.
Therefore root and dose of anthelmintic --> is
Important and must be chosen carefully.
MOA of anthelmintic drugs
1. Paralysis of worms or damages worm cuticle
Leading to partial digestion or rejection by immune
system.
2. Interfere with --> metabolism of the worm
Classification
1. For roundworm
eg. Mebendazole, Albendazole, Pyrantal, Piperazine, Levamisole,
Ivermectin.
2. For hookworm
eg. Mebendazole, Albendazole, Pyrantal, Levamisole
3. For threadworm
eg. Mebendazole, Albendazole, Pyrantal, Piperazine
4. For whipworm
Eg. Mebendazole, Albendazole
5. For filariasis
eg. Albendazole, Ivermectin
6. For tapeworms
Albendazole, Praziquantal
Benzimidazole
● Eg. Mebendazole, Albendazole, Thiabendazole
● Are broad spectrum agents
MOA: Polymerization
● Beta- Tubulin Microtubule
Benzimidazole
Glucose uptake by the worm
MOA:
●Benzimidazole Bind to free beta tubulin
And inhibit its polymerization and thus interfere with
Microtubulin dependent glucose uptake by the worm.
● The action is selective on the helminth microtubules
– 250 to 400 times more potent in helminth then
mammalian tissue.
● Effect take time to develop --> Worms may not be
expelled for several days.
Pharmacokinetics
Absorption:
● Only 10% of drug is absorbed after oral
administration.
● Fatty meal – Increases absorption
Metabolism:
● Rapidly metabolised in liver
Excretion:
● Excreted in urine and bile
Pharmacokinetics
Dose:
●Given as single daily dose--> for thread worm
●Twice a daily --> for 3 days for hook worm and round
worm infection.
Unwanted effect
●Very few
●GIT Disturbance
Q&A: Activity III
Q.1 What is the use of Ivermectin?
Q.2 Give mechanism of action of
Benzimidazole anthelmintic drugs?
Q.3 Recommend food to enhance
absorption of Benzimidazole anthelmintic
drugs.
Activity IV: Self learning of e-content
Albendazole
●Broad spectrum anthelmintics
●After oral administration, it is rapidly absorbed and
metabolised to sulfoxide and sulfone.
Responsible for anthelminthic action
● The plasma concentration of metabolites --> is 100
times greater then that of mebendazole.
Unwanted effect:
● GIT disturbance
Praziquantel:
● Highly effective broad spectrum anthelmintic drug.
● Drug of choice for all form of schistosomiasis--> used
in large scale schistosome eradication programmes.
MOA
●It apparently disturb the calcium homeostasis in the
parasite
Induces the calcium influx
Rapid and prolonged contraction of the musculature
Paralysis and death of worm
Pharmacokinetics
● Given orally - the praziquantel is well
absorbed
● Metabolised in the liver
● Metabolites are excreted in the urine
● The plasma half life – 60 to 90 min.
Unwanted effects:
● GIT disturbance
● Dizziness
● Aching in muscle
● Joint skin eruption
● And low grade fever
●It is safe for pregnant and lactating women.
● Piperazine:
● Used to treat infection with common round worm
infection and thread worms.
MOA:
●It irreversibly inhibit neuromuscular transmission in
the worms (by acting like GABA- the inhibitory
neurotransmitter).
leads to paralysis of worm and the paralysed worm are
expelled alive.
Pharmacokinetics
●It is given orally- some but not all is absorb
●It is partly metabolized and remainder is
eliminated unchanged via the kidney.
Unwanted effect
● GIT disturbance
● Urticaria
● Bronchospasm- occur occasionally
● Some patient experiences
● dizziness
● paraesthesia's
● vertigo
● And incoordination.
Q&A: Activity V
Q.1 Give mechanism of action of
Praziquantel?
Q.3 Recommend food to enhance
absorption of Benzimidazole anthelmintic
drugs.
Reference:
• H.P Rang. M M Dale, J.M Ritter, R.J Flower, G
Henderson. Pharmacology, Seventh Edition. Elsevier
Churchill Livengston Publication. Page no:668-672
Anthelmintics drugs.pdf
Anthelmintics drugs.pdf

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Anthelmintics drugs.pdf

  • 1. Prof. Shaikh Abusufiyan Assistant Professor, AIKTC-School of Pharmacy, New Panvel-410206 Anthelminthic Drugs Pharma Learning Forever
  • 2. At the end of this e-learning session you are able to… A. Discuss type of helminths. B. Explain pharmacology of Anthelminthic Drugs.
  • 3. Activity I: Self learning of e-content
  • 4. ● Many human harbour --> helminths (Worms) of one species or another. ● In some cases these infection --> results mainly in discomfort and do not cause ill health. eg. Threadworms in children. ● Other worm infections, such as Schistosomiasis and hookworm disease --> can produce very serious morbidity.
  • 5. Sexual reproduction of worms: ● Most worm reproduce sexually in human host (Primary host) Produces egg or larvae When passes out the body it infect the secondary host
  • 6. Type of worm infections Those in which 1. worm lives in alimentary canal 2. worms lives in other tissue of the host body
  • 7. Worm lives in alimentary canal 1. Tapeworm (Cestodes) The usual intermediate hosts of tapeworm are ● cattle ● pigs ● and fresh water fish. ● Human become infected --> by eating raw or under cooked meat of these animals or fishes.
  • 8. 2. Intestinal Round worms (Nematodes): 4 types 1. Common round worm 2. Thread worm 3. Whipe-worm 4. Hookworms
  • 9. Worms lives in the host tissues 1. Trematodes or flukes: • Infection caused by trematodes or flukes is called as Schistosomiasis (bilharzia). 2. Tissue round worms: are of 2 types a. Guinea worms b. Filariae worms
  • 10. a. Guinea worms ●The gravid female migrate to the S.C tissues of the leg or the foot and protrude through an ulcer in the skin. ●The worm may be up to a meter in length and has to be removed surgically ●Or by slow mechanical windning of the worm on to the stick over a period of days.
  • 11.
  • 12. b. Filariae worm: ● Major filarial disease are caused by wuchereria which caused obstruction of the lymphatic vessels producing elephantiasis.
  • 13.
  • 14. Q&A: Activity II Q.1 Enlist types of worm infection. Q.2 Name worm which migrate to the S.C tissues of the leg or the foot and protrude through an ulcer in the skin? Q.3 How Filariae worm causes elephantiasis.
  • 15. Anthelmintic Drugs ● To be an effective anthelmintic drugs ● it must be able to --> penetrate the cuticle of the worms ● or gain access --> to alimentary tract. • Limitation: This lead to difficulties for the design of good anthelmintic drugs.
  • 16. ● Some worms are exclusively --> haemophagous (blood eating) while other are tissue gazers. Therefore root and dose of anthelmintic --> is Important and must be chosen carefully.
  • 17. MOA of anthelmintic drugs 1. Paralysis of worms or damages worm cuticle Leading to partial digestion or rejection by immune system. 2. Interfere with --> metabolism of the worm
  • 18. Classification 1. For roundworm eg. Mebendazole, Albendazole, Pyrantal, Piperazine, Levamisole, Ivermectin. 2. For hookworm eg. Mebendazole, Albendazole, Pyrantal, Levamisole 3. For threadworm eg. Mebendazole, Albendazole, Pyrantal, Piperazine
  • 19. 4. For whipworm Eg. Mebendazole, Albendazole 5. For filariasis eg. Albendazole, Ivermectin 6. For tapeworms Albendazole, Praziquantal
  • 20. Benzimidazole ● Eg. Mebendazole, Albendazole, Thiabendazole ● Are broad spectrum agents
  • 21. MOA: Polymerization ● Beta- Tubulin Microtubule Benzimidazole Glucose uptake by the worm
  • 22. MOA: ●Benzimidazole Bind to free beta tubulin And inhibit its polymerization and thus interfere with Microtubulin dependent glucose uptake by the worm.
  • 23. ● The action is selective on the helminth microtubules – 250 to 400 times more potent in helminth then mammalian tissue. ● Effect take time to develop --> Worms may not be expelled for several days.
  • 24. Pharmacokinetics Absorption: ● Only 10% of drug is absorbed after oral administration. ● Fatty meal – Increases absorption Metabolism: ● Rapidly metabolised in liver Excretion: ● Excreted in urine and bile
  • 25. Pharmacokinetics Dose: ●Given as single daily dose--> for thread worm ●Twice a daily --> for 3 days for hook worm and round worm infection.
  • 27. Q&A: Activity III Q.1 What is the use of Ivermectin? Q.2 Give mechanism of action of Benzimidazole anthelmintic drugs? Q.3 Recommend food to enhance absorption of Benzimidazole anthelmintic drugs.
  • 28. Activity IV: Self learning of e-content
  • 29. Albendazole ●Broad spectrum anthelmintics ●After oral administration, it is rapidly absorbed and metabolised to sulfoxide and sulfone. Responsible for anthelminthic action
  • 30. ● The plasma concentration of metabolites --> is 100 times greater then that of mebendazole. Unwanted effect: ● GIT disturbance
  • 31. Praziquantel: ● Highly effective broad spectrum anthelmintic drug. ● Drug of choice for all form of schistosomiasis--> used in large scale schistosome eradication programmes.
  • 32. MOA ●It apparently disturb the calcium homeostasis in the parasite Induces the calcium influx Rapid and prolonged contraction of the musculature Paralysis and death of worm
  • 33. Pharmacokinetics ● Given orally - the praziquantel is well absorbed ● Metabolised in the liver ● Metabolites are excreted in the urine ● The plasma half life – 60 to 90 min.
  • 34. Unwanted effects: ● GIT disturbance ● Dizziness ● Aching in muscle ● Joint skin eruption ● And low grade fever ●It is safe for pregnant and lactating women.
  • 35. ● Piperazine: ● Used to treat infection with common round worm infection and thread worms.
  • 36. MOA: ●It irreversibly inhibit neuromuscular transmission in the worms (by acting like GABA- the inhibitory neurotransmitter). leads to paralysis of worm and the paralysed worm are expelled alive.
  • 37. Pharmacokinetics ●It is given orally- some but not all is absorb ●It is partly metabolized and remainder is eliminated unchanged via the kidney.
  • 38. Unwanted effect ● GIT disturbance ● Urticaria ● Bronchospasm- occur occasionally ● Some patient experiences ● dizziness ● paraesthesia's ● vertigo ● And incoordination.
  • 39. Q&A: Activity V Q.1 Give mechanism of action of Praziquantel? Q.3 Recommend food to enhance absorption of Benzimidazole anthelmintic drugs.
  • 40. Reference: • H.P Rang. M M Dale, J.M Ritter, R.J Flower, G Henderson. Pharmacology, Seventh Edition. Elsevier Churchill Livengston Publication. Page no:668-672