LEVOCYN -5

LEVOCYN 5

Levocetirizine hydrochloride (5 mg)

Levocetirizine hydrochloride, an antihistamine, is a major metabolite of hydroxyzine and is a rectomic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioclema, and urticaria. The structural similarity of levocetirizine to hydroviazine, and its derivatization from piperazine, has been shown to characterize adverse reactions and properties similar to other piperazine derivatives.

 Mechanism Of Action:

Levocetirizine, a human metabolite of hydroxyzine, is an antihistamine; Its major effects are mediated through selective inhibition of peripheral H1 receptors. The antihistaminic activity of levocetirizine has been documented in a wide variety of animal and human models. In vivo and ex vivo, animal models have shown negligible anticholinergic and antiserotonergic activity. In clinical studies, however, dry mouth was more common with cetirizine than citroba. In vitro receptor binding studies have shown no measurable relationship other than H1 receptors. Autoradiographic studies with radiolabeled levocetirizine in rats have shown negligible penetration into the brain. Ex vivo experiments in the mouse have shown that systematically administered levocetirizine does not significantly capture cerebral H1 receptors.

Half-Life of Levocetirizine Hydrochloride:

8.3 Hours

Protein binding:

~93%

Indications:

· Management of seasonal and perennial allergic rhinitis

· Treatment of chronic, idiopathic urticaria

· Treatment of year-round allergic rhinitis and chronic idiopathic urticaria in infants > 6 months

Pregnancy & Breast-Feeding:

If you are trying to become pregnant or are pregnant, or are breastfeeding, you should seek medical advice before taking this medicine. You should not take cetirizine 10 mg tablet during lactation because cetirizine passes into breast milk.

The onset of Action:

20 to 60 min.

Duration:

At least 24 h.

Drug Abuse & Dependence:

There is no information to indicate that abuse or dependency occurs with Levocetirizine hydrochloride.

Pharmacokinetic Properties:

Levocetirizine is a potent and highly selective antagonist of peripheral histamine H1-receptor on effector cells in the GI tract, blood vessels, and respiratory tract.

Absorption: Rapidly absorbed from the GI tract (oral); Peak plasma concentrations after 1 hour. Rate of absorption absorbed by food, but not range.

Distribution: Enters into breast milk; Crosses the blood-brain barrier (insignificant volume). Protein-binding: Highly bound.

Excretion: in the form of urine (unchanged); 10 hours (elimination half-life).

Drug-Drug interactions:

Increased INR and risk of epistaxis when taken together with warfarin.

Potentially fatal: CNS depressant and anticholinergics may potentiate CNT depressant cetirizine.

Precautions:

Hepatic or renal impairment; elderly; tasks requiring mental alertness eg, driving or operating heavy machinery; pregnancy.

Fertility:

For levocetirizine no clinical data are available

Dosage:

For adults and children over 6 years of age, the initial recommended dose is 5 mg or 10 mg as a single dose, depending on the severity of the symptom. For children 2–5 years of age, the initial recommended dose is 2.5 mg daily, a maximum of 5 mg daily.

Duration of action:

After oral administration of a dose of 5 mg of Levocetirizine dihydrochloride oral solution for healthy adult subjects, mean peak plasma concentrations were achieved at approximately 0.5 hours post-dose.

Adverse Reaction:

Drowsiness, fatigue, and dry mouth may occur. Fever or cough may also occur, especially in children. If any of these effects persist or worsen, tell your doctor or pharmacist immediately.

Storage:

Oral: Store at 20-25°C.

Overdosage:

Do not overdose. If someone takes too much something serious can happen, immediately go to the doctor

Contraindictions:

Those patients with a known hypersensitivity to it or its parent compound, hydroxyzine.

Side Effects of Levocetirizine Hydrochloride:

Somnolence, insomnia, malaise, headache, dizziness; GI discomfort, dry mouth, abdominal pain, diarrhea, nausea, vomiting; occasional hypersensitivity; epistaxis, pharyngitis, bronchospasm.

Warnings:

This drug contains levocetirizine. If you are allergic to levocetirizine or any of the ingredients contained in this medicine, do not take Zial Allergy 24HR Tablet, Zia Allergy 24HR Oral Solution, or Ziyazal.

Keep out of reach of children. In case of an overdose, seek medical attention or contact a toxin control center immediately.

Pregnancy

Contraindicated; since Cetrizine and Ambroxol are contraindicated in pregnancy; the combination generic are contraindicated in pregnancy.

Breast Feeding

Contraindicated; since Cetrizine and Ambroxol are contraindicated in breastfeeding; the combination generic is contraindicated in breastfeeding mothers.