1. ANTHELMINTIC DRUGS

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. 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. ROUND WORM
filariasis
Hookworm
Pin worm male, female

5. Tapeworm
Onchocerciasis
whipworm
Fasiola hepatica

6. Hydateid cyct

7. Symptoms: Abdomianl pain
 Diarrhoea
 Pruritis
 In severe condition cause anaemia

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. 
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. 

Chronic infestation may cause elephantiasis
lymphatic obstruction
Migrate to other subcutaneous tissue may
produce nodules and blindness.

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. 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. Liver flukes:




Bile duct obstruction
Liver enlargement
Cirrhosis of liver
Diarrhoea
Lung flukes:



Cough
Haemoptysis
Chest pain
»Contd.,

14. Blood flukes:
Skin
Lung
Liver
Mature
Blood
Haematuria
Frequent & painful micturation
Abdominal pain

15. Cestodes:





Ribbon shaped
Intestinal parasites
Head, neck followed by segments
Head hold- intestinal walls
No digestive system - host nutrients

16. 
WORM INFESTATION GLOBAL HEALTH PROBLEM.

MORE SO IN TROPICAL COUNTRIES.

WORMS CAN CAUSE G. I. T. AND GENERAL SYMPTOMS.

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. 
Against nematodes:
Pyrantel (NMJ)
Levimasole “
Piperazine “(GABA)
Ivermectin “
Diethyl carbamazine
Thiabendazole

Trematodes:
Metrifonate NMJ
Oxamniauine
Bithionol (ATP,Energy)
Tribendazole
»Contd.,

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. 
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. 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. * 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. UNTOWARD EFFECTS :
WEL TOLERATED
ALLERGY
NEUTROPAENIA
ALOPECIA
CI:-
Liver cirrhosis
Pregnancy teratogenic
Childrens <1y
RARELY

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. 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. 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. 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. PHARMACOKINETICS :

POORLY ABSORBED
SIDE EFFECTS :







MILD
G. I. T. SYMPTOMPS
HEADACHE
DIZZINESS
FEVER
SGOT
DOSE : 10 MG./ KG. SINGLE DOSE

29. Levamisole:




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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. 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. 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. ADVERSE REACTIONS :
* MOSTLY DUE TO DEATH OF MICROFILARIA
* ITCHING.
* SKIN EDEMA.
* ARTHRALGIA.
* HEADACHE
* FEVER.
CI:
Not pregnancy
<5 yrs

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. 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. 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. 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. 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. 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. 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. 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. 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. 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
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PIPERAZINE
BEPHENIUM
BEPHENIUM
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