Rapicet Dec

Uses

Diethylcarbamazine is used for Filariasis, Lymphatic filariasis, Pulmonary eosinophilia, Loiasis, Toxocariasis.

Levocetirizine Dihydrochloride is used for the treatment of symptoms associated with allergic conditions such as seasonal allergic rhinitis, perennial allergic rhinitis and chronic idiopathic urticaria.

Rapicet Dec is also used to associated treatment for these conditions: Filarial Infection, OnchocerciasisAllergic Rhinitis (AR), Chronic Idiopathic Urticaria, Common Cold, Nasal Congestion, Perennial Allergic Rhinitis (PAR), Seasonal Allergic Rhinitis

How Rapicet Dec works

The mechanism of action of diethylcarbamazine is thought to involve sensitizing the microfilariae to phagocytosis. One study showed that diethylcarbamazine's activity against Brugia malayi microfilariae is dependent on inducible nitric-oxide synthase and the cyclooxygenase pathway. It confirmed the important role of the arachidonic acid metabolic pathway in diethylcarbamazine's mechanism of action in vivo and showes that in addition to its effects on the 5-lipoxygenase pathway, it targets the cyclooxygenase pathway and COX-1.

Levocetirizine selectively inhibits histamine H₁ receptors. This action prevents histamine from activating this receptor and causing effects like smooth muscle contraction, increased permeability of vascular endothelium, histidine uptake in basophils, stimulation of cough receptors, and stimulation of flare responses in the nervous system.

Dosage

Rapicet Dec dosage

Inital: 1 mg/kg/day, may increase to 6 mg/kg/day over 3 days, then maintain for 3 wk. Prophylaxis of loiasis 300 mg/wk.

Adults and children 12 years of age and older: 5 mg once daily in the evening

Children 6 to 11 years of age: 2.5 mg once daily in the evening

Children 6 months to 5 years of age: 1.25 mg (1/2 teaspoon oral solution) once daily in the evening

Renal Impairment: Adjust the dose in patients 12 years of age and older with decreased renal function

Side Effects

Fever, headache, vomiting, dizziness, drowsiness, nausea, chills.

Potentially Fatal: Severe hypersensitivity reactions may occur especially in the treatment of onchocerciasis where rare Mazzotti reaction characterised by rash, itching, headache, muscle and joint pains, tachycardia, postural hypotension may start within 2 hr of drug administration. Encephalitis and retinal haemorrhage.

The most common adverse reactions (rate ≥2% and > placebo) were somnolence, nasopharyngitis, fatigue, dry mouth, and pharyngitis in subjects 12 years of age and older, and pyrexia, somnolence, cough, and epistaxis in children 6 to 12 years of age. In subjects 1 to 5 years of age, the most common adverse reactions (rate ≥2% and > placebo) were pyrexia, diarrhea, vomiting, and otitis media. In subjects 6 to 11 months of age, the most common adverse reactions (rate ≥3% and > placebo) were diarrhea and constipation.

Toxicity

Oral LD₅₀ in rat and mouse is 1400 mg/kg and 660 mg/kg, respectively.

Patients experiencing an overdose may present with drowsiness. Children may become agitated and restless before drowsiness. Patients should be treated with supportive measures. Dialysis will not assist in removing the drug from the body.

The maximal nonlethal dose in mice and rats is 240mg/kg.

Precaution

Patients with poor health.

Lactation: not known if excreted in breast milk.

Epileptic patients and patients at risk of convulsions. Renal impairment. Pregnancy and lactation.

Interaction

There are no known drug interactions and none well documented.

Volume of Distribution

The volume of distribution of levocetirizine is 0.33±0.02L/kg.

Elimination Route

Readily absorbed following oral administration.

Following a 5mg oral dose of levocetirizine, a C_max of 0.27±0.04µg/mL with a T_max of 0.75±0.50h. The AUC of levocetirizine is 2.31±0.50µg*h/mL. Taking levocetirizine with food does not affect the AUC but delays T_max by 1.25 hours and lowers C_max by 36%.

Half Life

Approximately 8 hours.

The average half life of levocetirizine is 7.05±1.54 hours.

Clearance

The average clearance of levocetirizine is 0.57±0.18mL/min/kg.

Elimination Route

168 hours post dose an average of 85.4% of a radiolabeled dose was recovered with an average of 80.8% in the urine and 9.5% in the feces. In the urine, 77% of the dose was recovered as unchanged drug, 0.5% as the M8 and M9 metabolites, 0.4% as the M10a metabolite, 0.4% as the M10b metabolite, 0.3% as the M3 metabolite, 0.3% as the M4 and M5 metabolite, 0.2% as the M2 metabolite, and 0.1% as the M1 metabolite. In the feces, 9.0% of the dose was recovered as unchanged drug, 1.0% as the M4 and M5 metabolite, and 0.1% as the M1 metabolite.

Pregnancy & Breastfeeding use

Pregnancy Category- X. Studies in animals or humans have demonstrated fetal abnormalities and/or there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience, and the risks involved in use of the drug in pregnant women clearly outweigh potential benefits.

Pregnancy: The safety of Levocetirizine in pregnancy has not been established. Therefore, it should be used with caution during pregnancy and only if the potential benefits to the mother outweigh any risks to the foetus.

Lactation: Levocetirizine passes into breast milk. So, it should be used with caution in nursing mothers and only if the expected benefit to the mother is greater than the risk to the nursing infant.

Contraindication

Pregnancy, hypersensitivity; lactation; infants, elderly or debilitated patients; impaired renal function; cardiac disease.

It is contraindicated in patients who are hypersensitive to this medication or to any of its ingredients.

Special Warning

Paediatric use: Not recommended for use in children less than 6 years of age.

Acute Overdose

Symptoms: Drowsiness, agitation, restlessness, confusion, diarrhoea, dizziness, fatigue, headache, malaise, mydriasis, pruritus, sedation, somnolence, stupor, tachycardia, tremor and urinary retention.

Management: Symptomatic and supportive treatment. Gastric lavage must be considered shortly following ingestion.

Storage Condition

Store between 20-25°C.

Innovators Monograph

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