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Anthelmintic Drugs
1
2
3
Nematode
4
Cestode
5
Trematode
6
Helminths
Roundworms Flatworms
(nematodes)
Flukes Tapeworms
(Trematodes) (Cestodes)
7
Anthemintics
ā€¢ Drugs used in the treatment of infestation
with helminths in the intestinal tract or tissues
of the body
ā€¢ Anthelmintics that kill worms are called
vermicides
ā€¢ Those that help to expel the worms are called
vermifuges
8
For Roundworm
Hookworm, Pinworm
Albendazole
Mebendazole
Pyrantel pamoate
Piperazine
Levamisole
For Hydatid disease
Albendazole
Mebendazole
For Threadworm
Ivermectin
Albendazole For Filariasis
Diethycarbamazine
Ivermectin
Albendazole
For Tapeworms
Praziquantel
Niclosamide
Albendazole
For Wipworm,
Trichinella spiralis
Albendazole
Mebendazole
ANTHELMINTIC DRUGS
9
Mebendazole
ā€¢ Broad spectrum of anthelmintic activity
ā€¢ Binds to Ī²-tubulin & inhibits microtubule
polymerization
ā€¢ Also blocks glucose transport into the parasite
ā€¢ So, intestinal parasites are immobilized or die
slowly
10
Mebendazole
Pharmacokinetics:
Administered orally, poorly absorbed from GIT,
highly bound to plasma proteins & metabolized in
liver, excreted in faeces
Adverse effects:
GI- anorexia, nausea, vomiting, diarrhoea &
abdominal discomfort.
Skin rashes, itching, drug fever
Contraindicated in pregnancy & children below one
year
11
Mebendazole
Uses: highly effective against intestinal
nematodes ā€“ roundworm. Hookworm,
whipworm, pinworm & mixed worm
infestations.
Mebendazole 100mg orally b.d for 3 days
12
Albendazole
ā€¢ Mechanism of action similar to Mebendazole
ā€¢ Given orally, fatty food increases its
absorption, metabolized in liver
ā€¢ Side effects are nausea, vomiting, diarrhoea &
epigastric distress, hepatic dysfuntion,
headache dizziness, fever, etc
ā€¢ Dose: single oral dose of 400mg
13
Albendazole
Uses
1. Nematodes: highly effecive against intestinal
nematodes.
2. Neurocysticercosis: preferred than praziquantel
because ā€“ cheaper, short duration of action,
reaches high concentration in brain & CSF, less
toxic,
3. Hydatid disease
4. Filariasis : given with diethycarbamzine or
ivermectin
14
Thiabendazole
ā€¢ Effective against nematodes
ā€¢ Mechanism of action similar to Mebendazole
ā€¢ Rarely used because of high incidence of
toxicity
15
Piperazine
ā€¢ Effective agaisnt roundworm & pinworm
ā€¢ Causes flaccid paralysis of worms that later
expelled by perstaltic movements
ā€¢ Produces convulsions & contraindicated in
epileptics
ā€¢ Safe during pregnancy
16
Levamisole
ā€¢ Effective against roundworm & hookworm
infestations
ā€¢ Immunomodulator
ā€¢ Used as an adjuvct in rheumatoid arthritis &
cancer chemotherapy
17
Pyrantel Pamoate
Pyrantel pamoate inhibits cholinesterases in worm
Stimulates nicotonic increases Ach concentration
Receptors in the worm
Persistent depolarization
Spastic paralysis
Worms are expelled
18
Pyrantel Pamoate
ā€¢ Dose ā€“ single oral dose of 11mg/kg for
Ancylostoma & Enterobius
ā€¢ Remarkably free of side effects
ā€¢ Contraindicated in infants
19
Diethylcarbamazine Citrate (DEC)
ā€¢ Effective in filariasis & tropical eosinophilia caused by
W.bancrofti & B.malayi
ā€¢ Acts on microfilariae but adult worms are killed
ā€¢ Safe during pregancy
Adverse Effects:
ā€¢ drug induced effects ā€“ anorexia, nausea, vomiting,
headace & dizziness
ā€¢ parasite inuced reactions ā€“ due to release of proteins
from dying parasites-In onchocerciasis, DEC produces
severe reaction called Mazzotti reaction(severe itching,
fever, skin rashes, nausea, vomiting, headache, joint
pain)
20
Diethylcarbamazine Citrage (DEC)
Uses
1. Filariasis: DOC for filariasis due to W.bancrofti
& B.malayi- orally 6mg/kg/day in 3 divide
doses for 3 weeks, additional of single dose
of albendazole 400mg ā€“ to reduce
transmission of filariasis
2. Tropical eosinophilia: 100mg TDS for 3 weeks
21
Ivermectin
ā€¢ DOC in onchocerciasis & strongyloidiasis
Mechanism of action:
Ivermectin
Activats gluatmate-gated chloride channels
Increases GABA trasmission in worms
Hyperpolarization & paralysis of worms
Death / phagocytosis of worms
22
Ivermectin
Uses :
1. DOC for onchocerciasis- kills microfilariae ā€“ relieves
pruritus & skin disease
2. Very effective in stonglyoidiasis, ascariasis & cutaneous
larva migrans
3. Uses orally in scabies & pediculosis
4. Mass chemotherapy of filariasis as sigle annual dose
along with albendazole
Advers effects:
Itching, skin rashes , oedema, headache, fever, can cause
Mazzoti reaction, contraindiated in pregnancy &
children
23
Praziquantel
MOA:
Praziquantel
Increase influx of Ca in the
tegument
Incresed muscular
contraction & spastic
paralysis
At higher concentration
Damages tegument
Death of parasite
Effective in trematodes & cestodes but not for
nematodes
24
Praziquantel
Uses
1. Schistosomiasis ā€“ DOC ā€“ 40mg/kg single oral
dose
2. Tapeworm infestation
3. Neurocysticercosis
25
Niclosamide
ā€¢ Second drug of choice for T.saginata, D.latum
& H. nana
ā€¢ Inhibits oxidative phosphorylation in
mitochondria- kills adult worm but not ova
ā€¢ Orally given in the form of chewable tablets
26
27
ā€¢ An 18 months old boy was brought to a
community health center by his mother with a
problem of a small white worm in his rectum.
ā€¢ According to his mother every night the patient
cried aloud because it felt itchy around his
rectum. The patient also had mild fever in the last
3 days and did not want to eat.
ā€¢ The doctor completed the examination with
laboratory examination and found that the
Hemoglobin count was only 7.4.
ā€¢ The patientā€™s mother had a history of worms last
month, but there were no symptoms and no
complaints at this time.
28
ā€¢ The biological diagnosis was anemia caused by
a pinworm disease (Oxyuris vermicularis) with
alleged white pinworm exiting out of the
rectum at night, as well as the possibility of
mother-to-child transmission, and the risk of
poor hygiene and sanitation in the preparation
of food so that worm eggs entered through
contaminated food or air.
29
ā€¢ The problem in this case was not about medical
treatment of a pinworm disease, which was probably
easily treated with antihelmintic within 1-2 days.
ā€¢ At a glance this problem seems trivial, however, the
interesting and challenging aspects of the above case
are:
ā€¢ 1) How to maintain the sustainability of clean and
healthy life behavior by patients and their families, so
the risk of worm infection does not occur in the future;
2) Behavior and use of latrines in the family where only
1 exists for all family members, to be healthy and
regularly managed and
3) How to educate the mother of the patient that this
worm infection can occur in an outbreak, if the healthy
lifestyle is not properly done while she keeps selling
candle ice for elementary school children near their
home
30
Thank You
31

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Antihelmintic drugs in MBBS 2nd year.pptx

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  • 8. Anthemintics ā€¢ Drugs used in the treatment of infestation with helminths in the intestinal tract or tissues of the body ā€¢ Anthelmintics that kill worms are called vermicides ā€¢ Those that help to expel the worms are called vermifuges 8
  • 9. For Roundworm Hookworm, Pinworm Albendazole Mebendazole Pyrantel pamoate Piperazine Levamisole For Hydatid disease Albendazole Mebendazole For Threadworm Ivermectin Albendazole For Filariasis Diethycarbamazine Ivermectin Albendazole For Tapeworms Praziquantel Niclosamide Albendazole For Wipworm, Trichinella spiralis Albendazole Mebendazole ANTHELMINTIC DRUGS 9
  • 10. Mebendazole ā€¢ Broad spectrum of anthelmintic activity ā€¢ Binds to Ī²-tubulin & inhibits microtubule polymerization ā€¢ Also blocks glucose transport into the parasite ā€¢ So, intestinal parasites are immobilized or die slowly 10
  • 11. Mebendazole Pharmacokinetics: Administered orally, poorly absorbed from GIT, highly bound to plasma proteins & metabolized in liver, excreted in faeces Adverse effects: GI- anorexia, nausea, vomiting, diarrhoea & abdominal discomfort. Skin rashes, itching, drug fever Contraindicated in pregnancy & children below one year 11
  • 12. Mebendazole Uses: highly effective against intestinal nematodes ā€“ roundworm. Hookworm, whipworm, pinworm & mixed worm infestations. Mebendazole 100mg orally b.d for 3 days 12
  • 13. Albendazole ā€¢ Mechanism of action similar to Mebendazole ā€¢ Given orally, fatty food increases its absorption, metabolized in liver ā€¢ Side effects are nausea, vomiting, diarrhoea & epigastric distress, hepatic dysfuntion, headache dizziness, fever, etc ā€¢ Dose: single oral dose of 400mg 13
  • 14. Albendazole Uses 1. Nematodes: highly effecive against intestinal nematodes. 2. Neurocysticercosis: preferred than praziquantel because ā€“ cheaper, short duration of action, reaches high concentration in brain & CSF, less toxic, 3. Hydatid disease 4. Filariasis : given with diethycarbamzine or ivermectin 14
  • 15. Thiabendazole ā€¢ Effective against nematodes ā€¢ Mechanism of action similar to Mebendazole ā€¢ Rarely used because of high incidence of toxicity 15
  • 16. Piperazine ā€¢ Effective agaisnt roundworm & pinworm ā€¢ Causes flaccid paralysis of worms that later expelled by perstaltic movements ā€¢ Produces convulsions & contraindicated in epileptics ā€¢ Safe during pregnancy 16
  • 17. Levamisole ā€¢ Effective against roundworm & hookworm infestations ā€¢ Immunomodulator ā€¢ Used as an adjuvct in rheumatoid arthritis & cancer chemotherapy 17
  • 18. Pyrantel Pamoate Pyrantel pamoate inhibits cholinesterases in worm Stimulates nicotonic increases Ach concentration Receptors in the worm Persistent depolarization Spastic paralysis Worms are expelled 18
  • 19. Pyrantel Pamoate ā€¢ Dose ā€“ single oral dose of 11mg/kg for Ancylostoma & Enterobius ā€¢ Remarkably free of side effects ā€¢ Contraindicated in infants 19
  • 20. Diethylcarbamazine Citrate (DEC) ā€¢ Effective in filariasis & tropical eosinophilia caused by W.bancrofti & B.malayi ā€¢ Acts on microfilariae but adult worms are killed ā€¢ Safe during pregancy Adverse Effects: ā€¢ drug induced effects ā€“ anorexia, nausea, vomiting, headace & dizziness ā€¢ parasite inuced reactions ā€“ due to release of proteins from dying parasites-In onchocerciasis, DEC produces severe reaction called Mazzotti reaction(severe itching, fever, skin rashes, nausea, vomiting, headache, joint pain) 20
  • 21. Diethylcarbamazine Citrage (DEC) Uses 1. Filariasis: DOC for filariasis due to W.bancrofti & B.malayi- orally 6mg/kg/day in 3 divide doses for 3 weeks, additional of single dose of albendazole 400mg ā€“ to reduce transmission of filariasis 2. Tropical eosinophilia: 100mg TDS for 3 weeks 21
  • 22. Ivermectin ā€¢ DOC in onchocerciasis & strongyloidiasis Mechanism of action: Ivermectin Activats gluatmate-gated chloride channels Increases GABA trasmission in worms Hyperpolarization & paralysis of worms Death / phagocytosis of worms 22
  • 23. Ivermectin Uses : 1. DOC for onchocerciasis- kills microfilariae ā€“ relieves pruritus & skin disease 2. Very effective in stonglyoidiasis, ascariasis & cutaneous larva migrans 3. Uses orally in scabies & pediculosis 4. Mass chemotherapy of filariasis as sigle annual dose along with albendazole Advers effects: Itching, skin rashes , oedema, headache, fever, can cause Mazzoti reaction, contraindiated in pregnancy & children 23
  • 24. Praziquantel MOA: Praziquantel Increase influx of Ca in the tegument Incresed muscular contraction & spastic paralysis At higher concentration Damages tegument Death of parasite Effective in trematodes & cestodes but not for nematodes 24
  • 25. Praziquantel Uses 1. Schistosomiasis ā€“ DOC ā€“ 40mg/kg single oral dose 2. Tapeworm infestation 3. Neurocysticercosis 25
  • 26. Niclosamide ā€¢ Second drug of choice for T.saginata, D.latum & H. nana ā€¢ Inhibits oxidative phosphorylation in mitochondria- kills adult worm but not ova ā€¢ Orally given in the form of chewable tablets 26
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  • 28. ā€¢ An 18 months old boy was brought to a community health center by his mother with a problem of a small white worm in his rectum. ā€¢ According to his mother every night the patient cried aloud because it felt itchy around his rectum. The patient also had mild fever in the last 3 days and did not want to eat. ā€¢ The doctor completed the examination with laboratory examination and found that the Hemoglobin count was only 7.4. ā€¢ The patientā€™s mother had a history of worms last month, but there were no symptoms and no complaints at this time. 28
  • 29. ā€¢ The biological diagnosis was anemia caused by a pinworm disease (Oxyuris vermicularis) with alleged white pinworm exiting out of the rectum at night, as well as the possibility of mother-to-child transmission, and the risk of poor hygiene and sanitation in the preparation of food so that worm eggs entered through contaminated food or air. 29
  • 30. ā€¢ The problem in this case was not about medical treatment of a pinworm disease, which was probably easily treated with antihelmintic within 1-2 days. ā€¢ At a glance this problem seems trivial, however, the interesting and challenging aspects of the above case are: ā€¢ 1) How to maintain the sustainability of clean and healthy life behavior by patients and their families, so the risk of worm infection does not occur in the future; 2) Behavior and use of latrines in the family where only 1 exists for all family members, to be healthy and regularly managed and 3) How to educate the mother of the patient that this worm infection can occur in an outbreak, if the healthy lifestyle is not properly done while she keeps selling candle ice for elementary school children near their home 30