Product Details

Class: Anthelmintic, Benzimidazole

Pharmacology

Mechanism of Action : Causes degeneration of cytoplasmic microtubule in intestinal and tegmental cells of intestinal helminths

Pharmacokinetics:

Absorption: <5%; may increase up to 4-5 times with a fatty meal

Distribution: Well inside hydatid cysts & CSF

Protein Bound: 70%

Metabolism: Hepatic; extensive first-pass effect; pathways include rapid sulfoxidation (major), hydrolysis, & oxidation

Half-life: 8-12 hr

Peak Plasma Time: 2-5 hr

Excretion: urine (<1% as active metabolite); feces

Dosage Forms & Strengths

tablet 200mg

• Neurocysticercosis (Taenia Solium Tapeworm)

>60 kg: 400 mg PO BID x 8-30 days

<60 kg: 15 mg/kg/day divided BID PO x 8-30 days; not to exceed 800 mg/day 

• Hydatid (Echinococcus Tapeworm)

>60 kg: 400 mg PO BID x 28 days, THEN 14 drug-free days x 3 cycles

<60 kg: 15 mg/kg/day divided BID PO, no more than 800 mg/day x 28 days, THEN 14 drug-free days x 3 cycles 

• Ancylostoma, Ascariasis, Hookworm, Trichostrongylus

400 mg PO once

• Capillariasis

400 mg PO qDay x10 days

• Larva Migrans, Cutaneous & Trichuriasis

400 mg PO qDay x 3 days

• Larva Migrans, Visceral

400 mg PO BID x 5 days

• Enterobius (Pinworm)

400 mg PO once, repeat in 2 weeks

• Fluke (Clonorchis Sinensis)

10 mg/kg PO qDay x7 days

• Gnathostomiasis, Microsporidiosis

400 mg BID x 21 days

Administration :

•     Administer with food.

•     Oral tablets may be crushed or chewed and swallowed with water.

Monitor:

•      Fecal specimens; 3 weeks after treatment.

•      CBC (at the beginning of each treatment cycle and every 2 weeks during treatment.

•       LFTs (transaminases)

Adverse Effects

>10%

Headache

• Neurocysticercosis (11%)

• Hydatid disease (1.3%)

Abnormal LFT

• Hydatid disease (15.6%)

• Neurocysticercosis (<1%)

1-10%

Abdominal pain

• Hydatid disease (6%)

Nausea/vomiting

• Hydatid disease (3.7%)

• Neurocysticercosis (6.2%)

Dizziness/vertigo

• Hydatid disease (1.2%)

• Neurocysticercosis (<1%)

Increased intracranial pressure

• Neurocysticercosis (1%)

Meningeal signs

• Neurocysticercosis (1%)

Alopecia (reversible)

• Hydatid disease (1.6%)

• Neurocysticercosis (<1%)

Fever

• Hydatid disease (1%)

  <1% (selected)

  Rash

  Urticaria

  Agranulocytosis

  Aplastic anemia

  Bone marrow suppression

  Granulocytopenia

  Pancytopenia

  Thrombocytopenia

  Hepatitis

  Acute liver failure

  Acute renal failure

Clinical Teaching:

• Advice female patient to avoid pregency during treatment and for one month after discontinuation.

• Warm patient to report symptoms of acute liver failure or hepatitis.

• Side effect may include; abdominal pain, nausea, vomiting, alopecia, fever, dizziness, headache, or vertigo.

• Instruct patient to take drug with food  

SOURCE : MEDSCAPE