ANTIHELMINTHIC THERAPY

Dr. Dumlao | April 25, 2020

Trans by: Del Rosario

OUTLINE - Absorption is increased with ingestion of fatty

meals
I. Introduction III. Miscellaneous
II. Antihelminthic Drugs Antihelminthic Drugs • Uses: Whipworm infections (drug of choice), Trichinosis,
A. Albendazole A. Metrifonate Visceral Larval Migrans (back up drug), Ascariasis,
B. Mebendazole B. Oxamniquine Pinworm
C. Thiabendazole C. Piperazine • SE: GI irritation, Elevated liver enzymes, Alopecia
D. Diethylcarbamazine D. Bithionol
E. Ivermectin IV. References C. THIABENDAZOLE
F. Pyrantel pamoate V. Appendix • Benzimidizole compound
G. Praziquantel • Use: Alternative for Ivermectin or Albendazole.
H. Niclosamide • MOA: Inhibits fumarate reductase and selectively inhibits
microtubule synthesis and also glucose uptake in
I. INTRODUCTION nematodes
• Ovicidal
• Helminths/Worms are multicellular organisms that infect • Pharmacokinetics:
very large number of humans and cause a broad range of - Rapidly absorbed after ingestion
diseases. - May also be absorbed from the skin
- Halflife: 1.2 hours
- Completely metabolized in liver
- Excreted in urine
• Uses: Trichinosis (drug of choice), Strongyloidiasis (back
up drug)
• SE: GI irritation, Hepatoxicity (Intrahepatic cholestasis and
liver failure) – Peculiar SE
• Contraindication: Pregnant patients

Figure 1. Antihelmintic Drugs [ Katzung& Trevor]
II. ANTIHELMINTHIC DRUGS
A. ALBENDAZOLE
• Broad spectrum oral antihelminthic
• MOA: inhibits microtubule assemble
• Both larvicidal and ovicidal
• Pharmacokinetics:
- After oral administration, albendazole rapidly
undergoes First Pass Metabolism
- Absoprtion is increased with fatty meals
• Uses: Hydatid disease (drug of choice), Whipworm
infections, Cutaneous & Visceral Larva migrans,
Cysticercosis (larval stages of T. solium), Angiostrongylus
cantonensis, Capillaria philippinensis, Ascariasis,
Hookworm, Pinworm infections
• SE: Alopecia, Bone marrow supression, Elevation of
liver function test (most specific SE)
• Contraindication: Patients with hepatic diseases such as
cirrhosis
B. MEBENDAZOLE
• Synthetic benzimidazole with wide spectrum of activity
• MOA: Selectively inhibits microtubule synthesis and
glucose uptake in nematodes
• Ovicidal
• Pharmacokinetics:
- Orally administered (<10% absorbed)
- Half-life: 2-6 hrs; Excreted in urine
D. DIETHYLCARBAMAZINE
• Synthetic piperazine derivative
• MOA: Immobilzes microfilariae (by an unknown
mechanism) and alters their surface structure ➡
helminths become more susceptible to host defense
mechanisms
• Uses: Filariasis (drug of choice), Eye Worm Disease,
Onchocerciasis (back up drug)
• Pharmacokinetics:
- Rapidly absorbed in GI tract
- Half life: 2-3 hours
- Excreted via urine
• SE: Headache, Weakness, Anorexia, Filarial fever (most
peculiar) ➡ fever, rashes, ocular damage, joint and
muscle pain, lymphangitis
E. IVERMECTIN
• Semi-synthetic macrocyclic lactone derived from the
Streptomyces avermitilis
• MOA: Intensifies GABA-mediated neurotransmission in
nematodes therefore, immobilizing the parasite
• Uses: Drug of choice for Strongyloidiasis and
Onchocerciasis, Back up drug for Cutaneous Larva
Migrans and Filariasis
• Pharmacokinetics:
- Rapidly absorbed with wide tissue distribution
- Half-life: 16 hours (longest)
- Excreted via feces
• SE: Mazzoti reaction characterized by fever, headache,
dizziness, rashes, paint in joints, muscles and lymph
glands
• Condraindication: Pregnancy and Children and other
drugs that may enhance GABA activity such as
barbiturates and benzodiazepines

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 C. PIPERAZINE D. BITHIONOL
• MOA: Stimulates nicotinic receptors at neuromuscular • An alternative to triclabendazole for the treatment of
junctions of nematodes therefore causing depolarization- fascioliasis (sheep liver fluke) and an alternative to
induced paralysis praziquantel for the treatment of paragonimiasis
• Uses: Drug of choice for Pinworm infections, Ascariasis, • SE: GI distress, skin rashes and headache
Hookworm
• SE: GI distress, headaches and weakness IV. REFERENCES
• Condraindication: Patients with hepatic dysfunction.
• Dr. Dumlao’s powerpoint presentation
• Katzung, B. & Trevor A. Pharmacology: Examination and
G. PRAZIQUANTEL Board Review 11th Edition. San Francisco, CA: McGraw
• Synthetic isoquinoline-pyrazine derivative Hill
• MOA: Increases membrane permeability to calcium • Basic and Clinical Pharmacology by Katzung, 14th ed
therefore causing paralysis and death
• Uses: Drug of choice for trematodes and cestodes
• SE: GI distress, headache, dizziness, skin rash, nausea,
drowsiness, arthralgia, myalgia, pruritus and skin rash.
• Pharmacokinetics:
- Rapidly absorbed
- Metabolized to inactive mono and poly hydroxylated
products after first pass effect in liver
- Excreted mainly in kidneys (60-80%) and biles (15-
35%)
- Half life: 0.8 to 1.5 hours
- Plasma concentration is increased with high
carbohydrate meals and cimetidine
- Bioavailability is reduced with phenytoin,
carbamazepine and corticosteroids

H. NICLOSAMIDE
• Salicylamide derivative
• MOA: uncouples oxidative phosphorylation or stimulation
of ATPase activity; it will kill cestode segments but has no
effect in ova
• Uses: Cestodes (alternative drug) adult worms are rapidly
killed; Second line drug for treatment of most of
tapeworms
• Minimally absorbed in GI tract
• SE: GI distress, headache, rash fever
• Contraindication: Ethanol consumption (Avoid 48 hours
upon administration)

III. MISCELLANEOUS ANTIHELMINTHIC

A. METRIFONATE
• Organophosphate compound
• MOA: Causes paralysis by inhibiting cholinesterase
• SE: Cholinergic symptoms (DUMBBELS- Diarrhea,
Urination, Miosis, Bradycardia, Bronchospasm,
Emesis, Lacrimation, Salivation)

B. OXAMNIQUINE
• Alternative to praziquantel for Schistosoma mansoni
• SE: Dizziness and drowsiness (Advise patient not to
operate heavy machineries)

C. PIPERAZINE
• Alternative drug for ascariasis
• MOA: Blocks Acetylcholine at the myoneural junction
thereby expulsion via neural peristalsis

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 V. APPENDIX

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