Zorat 10Mg Tab 10 s

Potential Overview:

Generic Name:Levocetirizine

Brand Name:Zorat

Pack Size:Zorat 10 mg Tablets typically come in a pack size of 10 tablets (10s).

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Mechanism of Action (MOA):

Zorat (Levocetirizine) is an antihistamine that works by selectively inhibiting the histamine H1 receptors. Histamine is a substance in the body that causes allergic reactions such as itching, swelling, and irritation. By blocking these receptors, Levocetirizine reduces the allergic symptoms caused by histamine release, such as sneezing, runny nose, and itchy eyes.

Indications:

Zorat (Levocetirizine) is commonly prescribed for:

• Allergic Rhinitis: Treatment of seasonal or perennial allergic rhinitis (hay fever), which includes symptoms such as sneezing, runny nose, and itchy, watery eyes.
• Urticaria (Hives): To treat chronic idiopathic urticaria (long-term hives) that causes itching and rash.
• Other Allergic Conditions: It can also be used to manage other conditions involving allergic reactions or pruritus (itching).

Dosage:

The usual recommended dosage of Zorat 10 mg is:

• Adults and Children (12 years and older): One 10 mg tablet once daily, preferably taken in the evening.
• Children (6-11 years): One 5 mg tablet once daily or as prescribed.
• Children (2-5 years): Consult a healthcare provider for the exact dose, typically in liquid form.

Side Effects:

Common side effects include:

• Drowsiness: Although Levocetirizine is less sedating than first-generation antihistamines, drowsiness may still occur.
• Headache
• Dry Mouth
• Fatigue
• Dizziness
• Gastrointestinal disturbances: Nausea, abdominal pain, or diarrhea.
• Rash: Rare but can occur.

Precautions:

• Renal Impairment: Caution should be exercised in patients with kidney problems, as Levocetirizine is primarily excreted through the kidneys. Dosage adjustments may be necessary.
• Pregnancy and Lactation: Levocetirizine is classified as a Category B drug (safe during pregnancy in studies, but should still be used under medical advice). It is excreted in breast milk, so caution is recommended when breastfeeding.
• Driving and Operating Machinery: Since drowsiness can occur, patients should avoid driving or operating heavy machinery until they know how the medication affects them.
• Alcohol: Alcohol may enhance the sedative effect of Zorat, so it should be avoided.

Contraindications (CI):

• Hypersensitivity: Contraindicated in patients who are allergic to Levocetirizine or any of the ingredients in the formulation.
• Severe Renal Impairment: Levocetirizine should not be used in patients with severe renal impairment (CrCl < 10 mL/min) unless prescribed by a healthcare provider with dose adjustments.
• Children under 2 years of age: Typically contraindicated for use in very young children.

Pharmacist Related Data

Chemical Name and Formula:

• Chemical Name: (S)-2-[2-[4-(Chlorophenyl)-1-piperazinyl]ethoxy]ethanol
• Molecular Formula: C21H25ClN2O3
• IUPAC Name: (S)-2-[2-[4-(Chlorophenyl)-1-piperazinyl]ethoxy]ethanol

Half-Life:

• The half-life of Levocetirizine is approximately 8 to 9 hours in healthy adults.
• It may be longer in patients with renal impairment.

Metabolism:

• Levocetirizine is a R-enantiomer of cetirizine, a second-generation antihistamine.
• It is primarily metabolized in the liver to a minimal extent and undergoes glucuronidation.
• The drug’s metabolism does not involve significant cytochrome P450 enzyme interactions, making it less likely to cause drug-drug interactions.

Drug Interactions with Food and Medicine:

Drug Interactions:

• CNS Depressants: Combining Levocetirizine with other central nervous system (CNS) depressants (e.g., alcohol, sedatives, tranquilizers) can enhance drowsiness and sedation.
• Theophylline: Co-administration with theophylline (a drug used for respiratory conditions) can slightly increase the plasma concentration of Levocetirizine. Caution is needed with this combination.
• Ritonavir and Other CYP3A4 Inhibitors: Although Levocetirizine undergoes minimal metabolism via CYP450, medications that affect liver enzymes (like ritonavir) might affect its plasma concentration.

Food Interactions:

• Food does not significantly affect the absorption or efficacy of Levocetirizine, so it can be taken with or without food.

Pharmacodynamics:

• Mechanism of Action: Levocetirizine is a selective H1-receptor antagonist. It competes with histamine for binding to histamine receptors in various tissues (e.g., lungs, skin, and mucous membranes), inhibiting histamine-induced effects such as swelling, vasodilation, and itching.
• Effect on Allergic Reactions: It reduces symptoms of allergic rhinitis, such as sneezing, runny nose, and itchy eyes. It also alleviates the symptoms of chronic urticaria, such as itching and hives.
• Potency: As an antihistamine, Levocetirizine is more potent than its precursor cetirizine and has a reduced sedative effect, as it preferentially blocks the H1 receptor in peripheral tissues over the brain, resulting in less sedation.

Pharmacokinetics:

1. Absorption:
   • Levocetirizine is rapidly absorbed after oral administration.
   • The bioavailability is approximately 100%, meaning nearly all of the drug reaches the bloodstream.
   • Peak plasma concentrations (Cmax) are typically reached about 0.9 hours after oral administration.
2. Distribution:
   • Levocetirizine is widely distributed throughout the body, with a volume of distribution (Vd) of about 0.4 L/kg.
   • It is highly protein-bound (approximately 90% bound to plasma proteins).
3. Metabolism:
   • Levocetirizine is minimally metabolized in the liver, and only a small fraction undergoes phase I metabolism (mainly glucuronidation).
   • Unlike first-generation antihistamines, it does not cause significant liver enzyme induction or inhibition.
4. Excretion:
   • The drug is primarily excreted unchanged in the urine (approximately 85% of the administered dose).
   • The rest is excreted in the feces.
   • Its clearance is directly proportional to renal function, so patients with impaired renal function may require dose adjustments.