ANTHELMINTIC DRUGS
Helminths are macroscopic, multiceullar
organism having their own digestive system,
excretory, reproductive and nervous sy...
Nematodes (Nemathelminths)







Long, round bodies, unsegmented worms,
tapered at both ends.
Most found primarily in...
ROUND WORM

filariasis

Hookworm

Pin worm male, female
Tapeworm

Onchocerciasis

whipworm

Fasiola hepatica
Hydateid cyct
Symptoms: Abdomianl pain
 Diarrhoea
 Pruritis
 In severe condition cause anaemia
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






Thread worm - small intestine.
Remain asymptomatic for years but in
immuno compromised person there may
tissu...


Filarial worms differ from other nematodes thread like and are found in blood tissues and
lymphatics.



Enter - bite ...




Chronic infestation may cause elephantiasis
lymphatic obstruction
Migrate to other subcutaneous tissue may
produce n...
Platyhelminths
Trematodes (Flukes)
Ex:-

Cestodes( Tape worm)
Ex:-

Blood flukes ( Schistosomiasis)
Liver flukes (Clonorch...
Trematodes (Flukes)
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Non segmented
Acquired - ingestion of food
Mature in intestinal track
Migrate and mature in...
Liver flukes:




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Bile duct obstruction
Liver enlargement
Cirrhosis of liver
Diarrhoea

Lung flukes:




Cough
Ha...
Blood flukes:
Skin
Lung
Liver
Mature
Blood
Haematuria
Frequent & painful micturation
Abdominal pain
Cestodes:
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Ribbon shaped
Intestinal parasites
Head, neck followed by segments
Head hold- intestinal walls
No d...


WORM INFESTATION GLOBAL HEALTH PROBLEM.

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MORE SO IN TROPICAL COUNTRIES.



WORMS CAN CAUSE G. I. T. AND GENERAL SYM...


Drugs used to get the body rid off the helminths
(worm) are called anthelmintic drugs.

Vermicide
 Vermifuge




Act...


Against nematodes:
Pyrantel (NMJ)
Levimasole “
Piperazine “(GABA)
Ivermectin “
Diethyl carbamazine
Thiabendazole



Tr...


Against cestodes:
Niclosamide (ATP, Energy)



Against trematodes & cestodes
Praziquantel Ca+2



Broad spectrum anth...


MEBENDAZOLE :

B. S. ANTHELMINTIC EFFECTIVE AGAINST :
* ASCARIASIS.(R)
* ENTROBIASIS. (P)
* TRICHURIS. (Whip)
* ANKYLO ...
MOA:


Helminths cytoskeketal structuers Mictofilaments,
microtubles, β-tubulins



Microtubles formation by β-tubulins
...
* Immobilization and slow death
* Selective disappearance of cytoplasmic micro
tubules in worms
* These effect not seen in...
UNTOWARD EFFECTS :
WEL TOLERATED
ALLERGY
NEUTROPAENIA
ALOPECIA
CI:-

Liver cirrhosis
Pregnancy teratogenic

Childrens <1y
...
ALBENDAZOLE (ZENTEL)

* Broad spectrum anthelmintic

* Actions similar to mebendazole
PHARMACOKINETICS :

* Single dose th...
THERAPEUTIC USES OF MEBENDAZOLE :
ASCARIASIS AND ANKYLOSTOMIASIS(HOOK) (M+ Pyrental)
400 MG. SINGLE DOSE.
ENTEROBIASIS.
1O...
THIABENDAZOLE :

M. O. A. : inhibits mitochondrial fumarate reeducates in helminths.
SPECTRUM :
effective against wide var...
PYRENTAL :
NN agonist – release Ach
It inhibits cholinestrase enzyme
Persistent depolarization type neuromuscular block.
S...
PHARMACOKINETICS :


POORLY ABSORBED

SIDE EFFECTS :









MILD
G. I. T. SYMPTOMPS
HEADACHE
DIZZINESS
FEVER
SGO...
Levamisole:








Rapid absorbed-git
Metabolized by liver
Half life 3-4hr
restricted to ascariasis and hook worm
M...
PIPERAZINE :


M. O. A. -* GABA agonist , Cl- muscle , hyperpolarization
* Causes flascid paralysis.
* live worms are exp...
IVERMECTIN : (MECTIZAN)

* Macrocylic lactone antibiotics
* Acts as GABA agonist
* Cause paralysis of parasite
SPECTRUM :
...
ADVERSE REACTIONS :
* MOSTLY DUE TO DEATH OF MICROFILARIA
* ITCHING.
* SKIN EDEMA.
* ARTHRALGIA.
* HEADACHE

* FEVER.

CI:...
PRAZEQUENTEL :
M. O. A. :
* Permeability to calcium and
vacuolations.
* Produce muscle contraction
* Tegumental damage and...
THERAPEUTIC USES :
I – TAENIA SOLIUM.
II – SCHISTOSOMIASIS.

DOSE : TAENIASIS – 10 MG/KG.SINGLE DOSE POST
TREATMENT PURGAT...
NICLOSAMIDE :
M. O. A. :Inhibit aerobic phosphorylation of ADP
Energy production.
Produce vermicidal action.
SPECTRUM :
Ef...
THERAPEUTICS USES : D. O. C. FOR :
T. SAGINATA
Dwarf tape warm
D. LATUS
Against T. Solium effective but should be avoided ...
BEPHENIUM : ( ALCOPAR)
* Inhibition of oxidative phosporylation cause ATP
synthesis
* It acts as vermifuge
spectrum :
ROUN...
DIETHYL CARBAMAZINE (HETRAZEN) :
* Piperazine derivative
* Inactive in vitro
* Sensitizes microfilaria surface - become
su...
THERAPEUTIC USES :

* FILARIASIS
6 – 12 MG / KG DAILY X 2 WKS.
* Tropical eosinophilia
6 MG./ KG. DAILY X 7 – 10 DAYS
DRUG...
Metrifonate:
 It is OP compound.
 Effective only against Schistosoma
haematobium.
 P t1/2 2hrs, but metabolite eliminat...
OXAMNIQUINE:
 Tetrahydroquinoline derivative
 Effective only against Schistosoma mansoni
MOA:
 Fluke first esterifies o...
ANTHELMINTIC DRUGS IN NUT SHELL
1
ROUND WORM

2
HOOK WORM

3
THREAD WORM

4
T. ECHINCOCUS

5
T. SOLIUM

6
T. SAGINATA

MEB...
15. anthelmantic
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15. anthelmantic

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15. anthelmantic

  1. 1. ANTHELMINTIC DRUGS
  2. 2. Helminths are macroscopic, multiceullar organism having their own digestive system, excretory, reproductive and nervous systems Helminths NEMATHELMINTHS PLATYHELMINTHS Pseudosacelom Acoelom ate TREMATODES CESTODES
  3. 3. Nematodes (Nemathelminths)     Long, round bodies, unsegmented worms, tapered at both ends. Most found primarily in intestine. Attached to the mucosa and feed host blood and tissue fluid. EX: Ascaris lumbricoides (roundworm), Trichuris trichiura (whipworm), Enterobius vermicularis (pinworm), Ancylostoma duodenale & Necator americanes (hookworms) Enterobius vermicularis(Pin worm) Wuchereria bacncrofti (Filarias) »Contd.,
  4. 4. ROUND WORM filariasis Hookworm Pin worm male, female
  5. 5. Tapeworm Onchocerciasis whipworm Fasiola hepatica
  6. 6. Hydateid cyct
  7. 7. Symptoms: Abdomianl pain  Diarrhoea  Pruritis  In severe condition cause anaemia
  8. 8.      Thread worm - small intestine. Remain asymptomatic for years but in immuno compromised person there may tissue invasion. Guinea worm – ingestation. larvae which are inhabit in ponds. Penetrate to intestinal wall and migrate through connective tissue, develop female produce larvae.
  9. 9.  Filarial worms differ from other nematodes thread like and are found in blood tissues and lymphatics.  Enter - bite of infected fly or mosquito.  Larvae then enter lymphatics and lymph nodes causing fever, eosinophilia and lymphadenitis. »Contd.,
  10. 10.   Chronic infestation may cause elephantiasis lymphatic obstruction Migrate to other subcutaneous tissue may produce nodules and blindness.
  11. 11. Platyhelminths Trematodes (Flukes) Ex:- Cestodes( Tape worm) Ex:- Blood flukes ( Schistosomiasis) Liver flukes (Clonorchiasis) Lung Flukes (Paragonimiasis) Intestinal flukes(Fasciolopsiasis) Beef tape worm (Taenia saginata) Pork tape warm (Taenia solium) Fish tape worm (Diphyllobothrum latum) Dwarf tape warm (Hymenolepis nana) »Contd.,
  12. 12. Trematodes (Flukes)      Non segmented Acquired - ingestion of food Mature in intestinal track Migrate and mature in liver- Liver flukes Lung – Lung flukes Causes: Diarrhoea  Abdominal pain  Anorexia  »Contd.,
  13. 13. Liver flukes:     Bile duct obstruction Liver enlargement Cirrhosis of liver Diarrhoea Lung flukes:    Cough Haemoptysis Chest pain »Contd.,
  14. 14. Blood flukes: Skin Lung Liver Mature Blood Haematuria Frequent & painful micturation Abdominal pain
  15. 15. Cestodes:      Ribbon shaped Intestinal parasites Head, neck followed by segments Head hold- intestinal walls No digestive system - host nutrients
  16. 16.  WORM INFESTATION GLOBAL HEALTH PROBLEM.  MORE SO IN TROPICAL COUNTRIES.  WORMS CAN CAUSE G. I. T. AND GENERAL SYMPTOMS.
  17. 17.  Drugs used to get the body rid off the helminths (worm) are called anthelmintic drugs. Vermicide  Vermifuge   Act by: Neuromuscular function  Microtubular function  Ca2+ permeability  Energy metabolism 
  18. 18.  Against nematodes: Pyrantel (NMJ) Levimasole “ Piperazine “(GABA) Ivermectin “ Diethyl carbamazine Thiabendazole  Trematodes: Metrifonate NMJ Oxamniauine Bithionol (ATP,Energy) Tribendazole »Contd.,
  19. 19.  Against cestodes: Niclosamide (ATP, Energy)  Against trematodes & cestodes Praziquantel Ca+2  Broad spectrum anthelmintics Benzimidazole group M- Mebendazole A- Albendazole N- Niclosamide I- Ivermectin P- Pyrantel A- Albendazole* L- Levamisole P- Praziquantel D- DEC
  20. 20.  MEBENDAZOLE : B. S. ANTHELMINTIC EFFECTIVE AGAINST : * ASCARIASIS.(R) * ENTROBIASIS. (P) * TRICHURIS. (Whip) * ANKYLO STOMA DUODENALE. (Hook) * NECTAR AMERICANIS. (Hook) * ONCOCERCIASIS. * TAENIA ECHINOCOCUS. *DRUG OF CHOICE FOR TREATMENT OF HYDATID DISEASE »Contd.,
  21. 21. MOA:  Helminths cytoskeketal structuers Mictofilaments, microtubles, β-tubulins  Microtubles formation by β-tubulins  Inhibtion β-tubulines  Inhibition of glucose uptake  Disruption of metabolic pathway »Contd.,
  22. 22. * Immobilization and slow death * Selective disappearance of cytoplasmic micro tubules in worms * These effect not seen in host * Clearance of worms may take 3 days.  PHARMACOKINETICS : * POORLY ABSORBED FROM G.I.T. * RAPIDLY METABOLISE BY LIVER P.B -90% t1/2- 2-6hrs.  DOSE : 100 MG. B. D. X 3 Days. »Contd.,
  23. 23. UNTOWARD EFFECTS : WEL TOLERATED ALLERGY NEUTROPAENIA ALOPECIA CI:- Liver cirrhosis Pregnancy teratogenic Childrens <1y RARELY
  24. 24. ALBENDAZOLE (ZENTEL) * Broad spectrum anthelmintic * Actions similar to mebendazole PHARMACOKINETICS : * Single dose therapy 400mg * DOC for cestodes+ nematodes * well tolerated Benzimidazole carbamate * Administered orally , absorption increased with a fatty meal * Metabolized in the liver * active metabolite albendazole sulfoxide MAY CAUSE : G. I. T. DISTURBANCES LONG TERM THERAPY :ALOPAECIA, LIVER DAMAGE, BONE MARROW »Contd.,
  25. 25. THERAPEUTIC USES OF MEBENDAZOLE : ASCARIASIS AND ANKYLOSTOMIASIS(HOOK) (M+ Pyrental) 400 MG. SINGLE DOSE. ENTEROBIASIS. 1OO TO 200 MG. SINGLE DOSE REPEAT AFTER 4 WEEKS. HYDATID DISEASE 15 MG/KG. I.V. DAILY X 4 WEEKS. STRONGYLOIDASIS. 400 MG. DAILY X 3 DAYS . TRICHURIASIS. 400 MG. SINGLE DOSE. larvicidal in hydatid ,cysticercosis , ascariasis and hook worm infections.  Ovicidal in ascariasis ,hookworm , trichuriasis
  26. 26. THIABENDAZOLE : M. O. A. : inhibits mitochondrial fumarate reeducates in helminths. SPECTRUM : effective against wide variety of nematodes infesting G. I. T. THERAPEUTIC USES : D. O. C. for Strongyloides stercolis (Rw) Cutaneous larvamigrants Visceral larva migrants . Hydatid disease 15 mg/kg. i.v. daily x 4 weeks. Filariasis along with DEC SIDE EFFECTS : Anorexnia, Nausea, Vomiting Dizziness, Headache.
  27. 27. PYRENTAL : NN agonist – release Ach It inhibits cholinestrase enzyme Persistent depolarization type neuromuscular block. Spastic muscle paralysis. VERMIFUGE. SPECTRUM : highly effective against : Intestinal acc. pin worm round worm less effective against : hook worms. »Contd.,
  28. 28. PHARMACOKINETICS :  POORLY ABSORBED SIDE EFFECTS :        MILD G. I. T. SYMPTOMPS HEADACHE DIZZINESS FEVER SGOT DOSE : 10 MG./ KG. SINGLE DOSE
  29. 29. Levamisole:       Rapid absorbed-git Metabolized by liver Half life 3-4hr restricted to ascariasis and hook worm MOA: NN agonist It has immunostimulant properties SIDE EFFECTS : Usually mild * GIT Disturbances * Drowsiness
  30. 30. PIPERAZINE :  M. O. A. -* GABA agonist , Cl- muscle , hyperpolarization * Causes flascid paralysis. * live worms are expelled by normal peristalsis, acts as vermifuge. KINETICS : Rapid absoration p. o. 20 % excreted unchanged in urine DOSE : 3 to 5 gm on 2 consequitive CI: Pregnant teratogenic Epilepsy patient
  31. 31. IVERMECTIN : (MECTIZAN) * Macrocylic lactone antibiotics * Acts as GABA agonist * Cause paralysis of parasite SPECTRUM : Effective against broad range of parasites and arthopodes. widely used in veterinary practice. I – D. O. C. - Oncocerciasis (M.Filarial) 150 mg / Kg. Single dose II – SCABIES : 200 MCG / KG Single oral dose. »Contd.,
  32. 32. ADVERSE REACTIONS : * MOSTLY DUE TO DEATH OF MICROFILARIA * ITCHING. * SKIN EDEMA. * ARTHRALGIA. * HEADACHE * FEVER. CI: Not pregnancy <5 yrs
  33. 33. PRAZEQUENTEL : M. O. A. : * Permeability to calcium and vacuolations. * Produce muscle contraction * Tegumental damage and death. Spectrum : Effective against wide variety of cestodes and tremetodes. *SCHISTOSOMIASIS. - LIVER FLUKES. - LUNG FLUKES. *Taeniasis. *Neuro Cysticercosis. (ALBEN) KINETICS : Absorbed P. O. »Contd.,
  34. 34. THERAPEUTIC USES : I – TAENIA SOLIUM. II – SCHISTOSOMIASIS. DOSE : TAENIASIS – 10 MG/KG.SINGLE DOSE POST TREATMENT PURGATIVE SIDE EFFECTS : ABDOMINAL DISCOMFORT. NAUSEA. HEADACHE. HALLUCINATIONS. PSYCHOSIS.
  35. 35. NICLOSAMIDE : M. O. A. :Inhibit aerobic phosphorylation of ADP Energy production. Produce vermicidal action. SPECTRUM : Effective against cestodes all tape worms except t. echynococcus. * T. SAGINATA * T. SOLIUM * Hymenolepis nana * D. LATUS KINETICS : not absorbed p. o. »Contd.,
  36. 36. THERAPEUTICS USES : D. O. C. FOR : T. SAGINATA Dwarf tape warm D. LATUS Against T. Solium effective but should be avoided . Cystecercosis in T. solium as not effective on ova. SIDE EFFECTS : Well tolerated Occasional G. I. T. upset can cause  PURGATIVE SHOULD ALWAYS BE GIVEN.
  37. 37. BEPHENIUM : ( ALCOPAR) * Inhibition of oxidative phosporylation cause ATP synthesis * It acts as vermifuge spectrum : ROUND WORM HOOK WORM (ANKYLOSTOMA) WIPE WORM. ADVERSE EFFECTS : NAUSEA VOMTING DIARHEA OVER ALL SAFE DRUG CAN BE ADMINISTERES IN ANEEMIC, PREGNANT AND ELDERLY PATIENTS
  38. 38. DIETHYL CARBAMAZINE (HETRAZEN) : * Piperazine derivative * Inactive in vitro * Sensitizes microfilaria surface - become susceptible to phagocytosis. * It enhances cell mediated immunity KINETICS :  Rapid absorption p. o.  Metabolized in liver  Excreted in urine in 30 hrs. »Contd.,
  39. 39. THERAPEUTIC USES : * FILARIASIS 6 – 12 MG / KG DAILY X 2 WKS. * Tropical eosinophilia 6 MG./ KG. DAILY X 7 – 10 DAYS DRUG INDUCED EFFECTS : * ANOREXIA. * HEADACHE. * DROWSINESS. * ALLERGIC REACTIONS. PARASITE INDUCED EFFECTS: Dye worm-proteins, enzymes Fever, Skin rashes, severe itching, N, V, Headache, chest pain, Muscle & joint pain (MAZZOTTI reaction)
  40. 40. Metrifonate:  It is OP compound.  Effective only against Schistosoma haematobium.  P t1/2 2hrs, but metabolite eliminated 24-48 SD  Cholinergic side effect CI : pregnancy  NMJ
  41. 41. OXAMNIQUINE:  Tetrahydroquinoline derivative  Effective only against Schistosoma mansoni MOA:  Fluke first esterifies oxamniquine – alkylates parasite DNA  Intercalation in the parasite DNA.  Block protein & Nucleic acid SIDE EFFECS:  CNS most common: Drow,Dizzi,Dull  Seizures at high dose.
  42. 42. ANTHELMINTIC DRUGS IN NUT SHELL 1 ROUND WORM 2 HOOK WORM 3 THREAD WORM 4 T. ECHINCOCUS 5 T. SOLIUM 6 T. SAGINATA MEBENDAZOLE 400 M. G. SINGLE DOSE MEBENDAZOLE 400 MG. SINGLE DOSE MEGENDAZOLE 100 TO 200 MG. SINGLE DOSE REPEAT AFTER 4 WKS. MEBENDAZOLE 15 MG. / KG. I. V. DAILY X 4 WKS. PRAZIQUENTEL 10 MG/KG. SINGLE DOSE NICLOSAMIDE 1 GM 2 DOSE AT 1 HR. ALBENDAZOLE ALBENDAZOLE ALBENDAZOLE ALBENDAZOLE NICLOSAMIDE PRAZIQUENTEL PYRENTEL PYRENTEL PIPERAZINE ---------------------- --------------------- -------------------- PIPERAZINE BEPHENIUM BEPHENIUM ---------------------- ------------------------ ------------------------

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