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,
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
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
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 .
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.
