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Anthelmintic 408 stu

Anthelmintic 408 stu

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Published by Hassan.shehri

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Published by: Hassan.shehri on Feb 01, 2008
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AnthelminticsSory اهاعم يذه اتلكام رخاب  وص عط وم شب رس ةوتكد اعط 
Mebendazole, thiabendazoleAlbendazoleIntestinal capillariasisMebendazole,diethylcarbamazineAlbendazoleVisceral larva migransThiabendazole (topical)Albendazole, ivermectinCutaneous larva migransThiabendazole, mebendazoleMetronidazole
Guinea worm
DiethylcarbamazineIvermectin
O. volvulus
IvermectinDiethylcarbamazine
W. bancrofti and Brugiamalayi (Filariasis);tropical eosinophilia; Loaloa
SomaticnematodesThiabendazole, albendazoleIvermectin
Strongyloidiasis
Oxantel, pyrantelMebendazole, albendazole
Trichuriasis (whipworm)
thiabendazoleMebendazole, albendazole-add corticosteroids for severeinfection
Trichinosis (Trichinellaspiralis)
levamisol, thiabendazoleAlbendazole, mebendazole, pyrantel
AncylostomiasisNecator americanusAncylostoma. duodenale
Albendazole, piperazineMebendazole, pyrantel
Enterobiasis
Piperazine, levamisolAlbendazole, pyrantel,mebendazole
AscariasisAlternative drugsDrug of choiceWorm infestation1.Intestinal nematodes
BithionolPraziquantel, triclabendazole
Paragonimuswestermani(lung fluke)
AlbendazolePraziquantel
Clonorchissinensis(liver fluke)
Praziquantel, niclosamide
Fasciolabuski(large intestinal fluke)
-Bithionol, triclabendazole
Fasciolahepatica (sheep liver fluke)
-
Praziquantel
S. japonicum
OxamniquinePraziquantel
S. mansoni
MetrifonatePraziquantel
Schistosomahematobium (bilharziasis)3.Trematodes:Flukes
MebendazoleAlbendazole
Echinococcus granulosus (hydatidtapeworm)
 NiclosamidePraziquantelHymenolepis nana (dwarf tapeworm)-Praziquantel, niclosamideDiphyllobothrium latum (fish tapeworm)PraziquantelAlbendazoleCysticercosis cellulosae(pork tapewormlarval stage)-Praziquantel, niclosamide
Taeniasolium(pork tapeworm)
MebendazolePraziquantel, niclosamide
Taeniasaginata(beef tapeworm)2. Cestodes(tape worms)
Mechanism of action of anthelmintics
1.Against nematodesi.Depolarsing bloc
Pyrantel and levamisoleNN receptors agonists
and also i
ncrease ACh levelby
inhibiting ChE. They produce
depolarizing NM blockade
. Detached wormsare expelled in feces.
ii.Inhibitory action.
1
 
Piperazine:
is a
GABA agonist
, activates GABA gated Cl channel-
causehyperpolarization, flaccid paralysis, paralysed worms are expelled alive.
Ivermectin: activates glutamate-gated Cl channels which are inhibitory, cause hyperpolarization.
Diethylcarbamazine
: though a piperazine (causing hyperpolarization),mechanism of action is different:
it alters microfilarial membrane surfacecharacteristics so that they are phagocytosed by tissue fixed monocytes.2.Broad spectrum antheminticsBenzimidazole group:
Albendazol, mebendazole- broad spectrum anthelmintic (many nematodesand cestodes).
Thiabendazole and triclabendazole- restricted use.Benzimidazoles bind to β tubulins & prevent their assembly, i.e.depolymerisation resulting in breakdown of microtubules (cytoplasmic,tegumental and intestinal) with selective and irreversible inhibition of glucoseuptake. The end result is depletion of parasite’s glycogen stores, reducedformation of ATP, disruption of metabolic pathways and ultimately parasiticdeath.3.Against trematodes
Metrifonate
:
an organophosphate compound which gets converted todichlorovos which acts as an antiChE, produces depolarizing block of S.hematobium
.
Oxamniquine
:
acts by intercalation in the parasitic DNA
leading to death of Schistosome by blocking its nucleic acid and protein synthesis. The fluke firstesterifies oxamniquine to produce a reactive metabolite that alkylates parasiteDNA.
Bithionol
:
uncouples parasitic specific fumarate reductase mediated oxidativephosphorylation4.Against cestodes and against cestodes and trematodesAgainst cestodes:
Niclosamide
:
uncouples oxidative phosphorylation
in adult cestodes. It inhibitsanaerobic incorporation of energy rich inorganic phosphates into ATP which isharmful to the parasite.
5.Against trematodes and cestodes
.
Praziquantel:
 
causes influx of calcium from endogenous stores of the cestodesresulting in intense contraction and subsequent expulsion of the worm fromthe GIT. In schistosomes praziquantel induced influx of calcium damages thetegument, causing holes which exposes hidden parasite antigens, theantibodies in the host bind to these antigen and destroy them byphagocytosis
.
Individual drugs.Albendazole
Mechanism of action:
Has larvicidal effects
in hydatid disease, cysticercosis.
Has ovicidal effects
in ascariasis, ancylostomiasis and trichuriasis.
Uses
2
 
DOC for ascaris lumbricoides (AL), trichuris trichuria (TT), ancylostomaduodenale (AD) and Necator americanis (NA).
Preferred for cutaneous larva migrans, visceral larva migrans, intestinalcapillariasis.
.
DOC for neurocysticercosis
: given with corticosteroid to decrease theinflammatory reaction due to dying worm. It is
superior to praziquantel becauseof short duration , low cost and improved penetration in subarachnoid spaceand increased blood levels of drug when administered with corticosteroid.
Fo
hydatid disease
better results obtained when given with praziquantel.Treatment given for months 1-6 MAlternative for strongyloides stercoralis (SS), enterobius vermicularis (EV) andclonorchis sinensis.Albendazole + diethylcarbamazine or ivermectin is a synergistic combination for treating or controlling lymphatic filariasis.It is adm in empty stomach for intestinal worms and with fatty meal when usedagainst tissue parasites
Adverse effects
.Well tolerated with 3-5 days treatment, even with 1 month treatment for cysticercosis/hydatid disease not much adverse reactions. More than 3 months treatment may produce:
Mild and transient epigastric distress, nausea, diarrhea, abdominal distress
Headache, dizziness, lassitude, insomnia, fever, fatigue, alopecia, increased liver enzymes and pancytopenia.
Monitor LFT and CBC during prolonged therapy.
It is teratogenic- avoid long term use in pregnancy
Mebendazole
Mechanism of action: similar to albendazole.Like albendazole, it is also
wide spectrum anthelmintic
- effective against GInematodes (AL, EV, TT, AD, NA), intestinal capillariasis and hydatid disease.It is given orally, poorly absorbed, abs. increases with fatty meal. Has first passmetabolism. Tablet chewed before swallowing.
Uses:
DOC for AL, TT, NA, AD, EV .Alternative for trichinosis.Intestinal capillariasis.Visceral larva migrans.
Side effects:
Short term: Diarrhea, abdominal pain, nausea, vomitingLong term: increase in transaminases and urticaria, rash.
Contraindications
:PregnancyChildren below 2 years.Liver cirrhosis
Triclabendazole
Narrow spectrum benzimidazole- used primarily in veterinary practice.
DOC for fasciola hepatica
infection not responding to praziquantel.
Effective for lung fluke
.
Adverse reactions
:Not significant side effects3

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