Dr. RAGHU PRASADA M S
MBBS,MD
ASSISTANT PROFESSOR
DEPT. OF PHARMACOLOGY
SSIMS & RC.
1
 Drugs used to treat parasitic worm infections:
helmintic infections
 Unlike protozoa, helminths are large and have
comp...
NEMATELMINTHS(ROUND)
 ROUND.W-ASCARIS.L
 HOOKW-NECATOR A
 WHIPW-TRICHURIST
 THREADW-
STRONGYLOIDES.S
 PINW-ENTEROBIUS...
Against Nematodes-ALBENDAZOLE, MEBENDAZOLE
PYRANTEL PAMOATE, LEVIMASOLE, PIPERAZINE,
IVERMECTIN, DIETHYLCARBAMAZINE,
THIAB...
PYRANTEL PAMOATE
MOA-Blocks acetylcholine at the neuromuscular
junction, resulting in paralysis of the worms, which
are th...
 Benzimidazoles
 (ALBENDAZOLE &
 MEBENDAZOLE )
MOA-binds to beta tubulinprevents
polymerisationbreak down of
cytoplas...
Mebendazole is absorbed after oral – 10%
Fatty meal increases absorption Albendazole,
mebendazole
It is rapidly metabolis...
1. Ascariasis, hook worm, pin worm infections
2. Hydatid disease-BD for 1 month
3. Neurocysticercosis- along with corticos...
Benzimidazoles-ADR-Well tolerated, less side effects
If used for >3months as in hydatid disease
Epigastric distress, alopa...
Anthelmintic and immunomodulator belonging to a
class of synthetic imidazothiazole derivatives
It is effective in infectio...
Anthelmintic
Levamisole has been used to treat a variety of
dermatologic conditions-
skin infections,
leprosy, warts,
lich...
MOA-It reversibly inhibits neuromuscular transmission in
the worm
It probably by acting like GABA/GABA-gated chloride
chan...
It is highly effective broad-spectrum antiparasitic
First choice of drug for the treatment of filarial infections
and is v...
Uses :It has also given good results against W.
bancrofti, which causes elephantiasis.
A single dose kills the immature mi...
Diethylcarbamazine is a piperazine derivtve
It is active in filarial infections caused by W. bancrofti
It mainly act by ma...
Uses
chemoprophylaxis
Filariasis- 2-3mg/kg for 2-3 weeks
Tropical eosinophilia for 7 days
loiasis
Side effects
Fever, head...
MOA:
Its action has been ascribed to inhibition of the parasite's
mitochondrial anaerobic phosphorylation of ADP which
pro...
Adverse effects
Unwanted effects are few,
infrequent and transient.
Nausea and vomiting can occur.
Drowsiness, dizziness, ...
It is the drug of choice for all forms of schistos and for
cestode infections like cysticercosis.
MOA: Permeability of the...
 METRIFONATE, OXAMNIQUINE, BITHIONOL,
TRICLABENDAZOLE
MITRIFONATE –organophosphorus compound so is
cholinesterase inhibit...
OXAMNIQUINE-tertahydroquinoline dervt
Used against Scistosoma mansoni
It is the drug of choice for all forms of schistosom...
BITHIONOL-orally well absorbed
DOC-for fascioliasis(sheep liver fluke)
30-50mg for 10-15 days on alternate
days
Pulmonay p...
Worms (helminths) Drug of choice
Tapeworms (cestodes) Niclosamide or Praziquantel or
Albendazole
Roundworms (nematodes)
•E...
THANKYOU
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Authorstream/presentations/raghuprasada
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Class antihelmintics 4
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Class antihelmintics 4

  1. 1. Dr. RAGHU PRASADA M S MBBS,MD ASSISTANT PROFESSOR DEPT. OF PHARMACOLOGY SSIMS & RC. 1
  2. 2.  Drugs used to treat parasitic worm infections: helmintic infections  Unlike protozoa, helminths are large and have complex cellular structures  Drug treatment is very specific  It is very important to identify the causative worm  Done by finding the parasite ova or larvae in feces, urine, blood, sputum, or tissue
  3. 3. NEMATELMINTHS(ROUND)  ROUND.W-ASCARIS.L  HOOKW-NECATOR A  WHIPW-TRICHURIST  THREADW- STRONGYLOIDES.S  PINW-ENTEROBIUSV  FILARIASIS-W BANCROFTI  ONCHOCERCIASIS- O.VOLVULUS  GUINEAW-DRACANCULUS M PLATYHELMINTHS  TREMATODES-FLUKES  BLOOD F- SCISTOSOMIASIS  LIVER F-CLONORCHIASIS  INTESTINAL F- FASCIOLOPSIASIS  LUNG F-PARAGONIMIASIS CESTODES BEEFTW-T.SAGINAT PORKTW-T.SOLIUM FISHTW-DIPHYLLOBO THRIUM DWARFTW- HYMENOLEPIS.NANA
  4. 4. Against Nematodes-ALBENDAZOLE, MEBENDAZOLE PYRANTEL PAMOATE, LEVIMASOLE, PIPERAZINE, IVERMECTIN, DIETHYLCARBAMAZINE, THIABENDAZOLE, DOXYCYCLINE Against trematodes METRIFONATE, OXAMNIQUINE, BITHIONOL, TRICLABENDAZOLE Against Cestodes NICLOSAMIDE Against trematodes and Cestodes-PRAZIQUANTEL
  5. 5. PYRANTEL PAMOATE MOA-Blocks acetylcholine at the neuromuscular junction, resulting in paralysis of the worms, which are then expelled through the GI tract P/K-small amount is absorbed, so high levels are achieved in intestinal walls luminal antihelmintic Uses –round w, hook w, Pin w—10mg/kg S/E-may cause hypersensitivity reactions, neurological symptoms (including “worm wobble”) and may precipitate epilepsy.
  6. 6.  Benzimidazoles  (ALBENDAZOLE &  MEBENDAZOLE ) MOA-binds to beta tubulinprevents polymerisationbreak down of cytoplasmic microtubulesthey Inhibit uptake of glucose and other nutrients, depletion of glycogen stores decrease of ATPleading to autolysis and death of the parasitic worm
  7. 7. Mebendazole is absorbed after oral – 10% Fatty meal increases absorption Albendazole, mebendazole It is rapidly metabolised, the products being excreted in the urine and the bile within 24-48 hours. Single dose for threadworm, BD daily for 3 days for hookworm and roundworm infestations. Thiabendazole is rapidly absorbed orally Albendazole is metabolised extensively by first-pass metabolism to the sulfoxide so has t1/2 -8-10 hrs
  8. 8. 1. Ascariasis, hook worm, pin worm infections 2. Hydatid disease-BD for 1 month 3. Neurocysticercosis- along with corticosteroids 4. Cutaneous larvae migrans-400mg for 3 days 5. Visceral larvae migrans- 6. Toxocariasis 7. Giadiasis ans tianiasis 8. Emperical treatment-Persistant eosinophilia
  9. 9. Benzimidazoles-ADR-Well tolerated, less side effects If used for >3months as in hydatid disease Epigastric distress, alopacia, insomnia, Teratogenic in animals Thiabendazole inhibits cellular enzymes of susceptible helminths. Inhibits the helminth-specific enzyme, fumarate reductase S/E-Gastrointestinal, neurological and hypersensitivity reactions, liver damage, and crystallurea may be induced.
  10. 10. Anthelmintic and immunomodulator belonging to a class of synthetic imidazothiazole derivatives It is effective in infections with the common round-worm as well as hook worm MOA: It has a nicotine-like action, stimulating and subsequently blocking the neuromuscular junctions. The paralysed worms are then expelled in the faeces. Ova are not killed. Phamacokinetics: The drug is given orally, is rapidly absorbed and is widely distributed. It crosses the blood-brain barrier.
  11. 11. Anthelmintic Levamisole has been used to treat a variety of dermatologic conditions- skin infections, leprosy, warts, lichen planus, and aphthus ulcers Side effects: Gastrointestinal disturbances, Dizziness and skin eruptions. High concentrations can have nicotinic actions on autonomic ganglia in the mammalian host. There are some reports of encephalopathy
  12. 12. MOA-It reversibly inhibits neuromuscular transmission in the worm It probably by acting like GABA/GABA-gated chloride channels in nematode muscle. The paralyzed worms are expelled alive Uses for Ascariasis -4g * 2 days and Pin worm- 4g * 7 days ADR- nausea, vomiting, rarely neurotoxic and allergic reactions nitrosamine metabolite-carcinogenic and teratogenic potential D/I- Should not be used concurrently with pyrantel pamoate
  13. 13. It is highly effective broad-spectrum antiparasitic First choice of drug for the treatment of filarial infections and is very effective in onchocerciasis MOA: It kill the worm by opening glutamate-gated chloride channels (found only in invertebrates) and increasing Cl- conductance; by binding to a novel allosteric site on the acetylcholine nicotinic receptor to cause an increase in transmission, leading to motor paralysis; or by binding to aminobutyric acid receptors.
  14. 14. Uses :It has also given good results against W. bancrofti, which causes elephantiasis. A single dose kills the immature microfilariae of O. volvulus- river blindness The drug also has activity against infections with some roundworms: common roundworms, whipworms, and threadworms It works best if repeated at 6–12-month intervals. Side effects: skin rashes, fever, giddiness, headaches and pains in muscles, joints and lymph glands
  15. 15. Diethylcarbamazine is a piperazine derivtve It is active in filarial infections caused by W. bancrofti It mainly act by make opsonisation of worm that detected by our immune system It immobilizes microfilariae and alters their surface structure makes them susceptible for host defence The drug is absorbed by oral administration Urinary excretion unchanged and N-oxide metabolite
  16. 16. Uses chemoprophylaxis Filariasis- 2-3mg/kg for 2-3 weeks Tropical eosinophilia for 7 days loiasis Side effects Fever, headache, anorexia, malaise, urticaria, vomiting, and asthmatic attacks following the first dose are due to products of destruction of the parasite, and reactions are minimised by slow increase in dosage over the first 3 days.
  17. 17. MOA: Its action has been ascribed to inhibition of the parasite's mitochondrial anaerobic phosphorylation of ADP which produces usable energy The scolex and a proximal segment are irreversibly damaged by the drug The worm separates from the intestinal wall and is expelled There is negligible absorption of the drug from the gastrointestinal tract. Uses-Taenia solium, the drug is given in a single dose after a light meal, followed by a purgative 2 hours
  18. 18. Adverse effects Unwanted effects are few, infrequent and transient. Nausea and vomiting can occur. Drowsiness, dizziness, Malaise, anorexia, as well as gastrointestinal upsets. It is contradicted in pregnant women or nursing mothers. Drug interaction: Enzyme inducers dexamethasone, phenytoin, and carbamazepine increase metabolism Cimetidine, known to inhibit cytochrome P-450 isozymes,
  19. 19. It is the drug of choice for all forms of schistos and for cestode infections like cysticercosis. MOA: Permeability of the cell membrane to calcium is increased, causing contracture and paralysis of the both adult worms and larvae. Pharmacokinetics: It is rapidly absorbed after oral administration and distributes into the cerebrospinal fluid. S/E-It may cause nausea, headache, dizziness, and drowsiness; it cures with a single dose (or divided doses in one day).
  20. 20.  METRIFONATE, OXAMNIQUINE, BITHIONOL, TRICLABENDAZOLE MITRIFONATE –organophosphorus compound so is cholinesterase inhibitors. It is safe and cost effective for schistosoma infection. It has good oral absorption Orally active and t1/2 =1-5 hrs S/E-cholinergic side effects -diarrhoea, tremors, bronchospasm C/I- pregnancy
  21. 21. OXAMNIQUINE-tertahydroquinoline dervt Used against Scistosoma mansoni It is the drug of choice for all forms of schistosomiasis -given orally MOA- flukes esterifies drug to produce reactive metabolite  alkylates DNA of flukes. It intercalated with parasite DNA and inactivate it S/E- CNS-drowsiness, dizziness pruritis, urticaria
  22. 22. BITHIONOL-orally well absorbed DOC-for fascioliasis(sheep liver fluke) 30-50mg for 10-15 days on alternate days Pulmonay paragonimiasis ADR- anorexia, nausea, vomiting avoided in children below 8yrs TRICLABENDAZOLE narrow spectrum benzimidazole DOC for treating human fasciola hepatica
  23. 23. Worms (helminths) Drug of choice Tapeworms (cestodes) Niclosamide or Praziquantel or Albendazole Roundworms (nematodes) •Enterobius vermicularis (pinworm) •Ascaris lumbricoides •Trichuris trichiura (whipworm) •Trichinella spiralis (trichinellosis) •Strongyloides stercoralis •Necator americanus (hookworm) •Ancylostoma duodenale •Onchocerca volvulus (Onchocercosis) •Wuchereria bancrofti (Elephantiasis) Mebendazole or Pyrantel Mebendazole or Pyrantel Mebendazole or Albendazole Mebendazole and Thiabendazole Thiabendazole Mebendazole or Pyrantel Mebendazole, Pyrantel, or Albendazole Ivermectin Diethylcarbamazine Flukes (trematodes) •Schistzoma (Schistozomes) Praziquantel
  24. 24. THANKYOU Download slides from Authorstream/presentations/raghuprasada Slideshare/presentations/raghuprasada Youtube/raghuprasada
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