Z-Deen

Loratadine.

A white, oval, biconvex tablet engraved with "
Click on icon to see table/diagram/image
" logo on one side and "L 10" on the other side.
Each tablet contains Loratadine 10 mg.

Pharmacology: Pharmacodynamics: Loratadine is a second generation antihistamine with non-sedating properties. It is also a potent long-acting antihistamine with selective peripheral H₁ receptor antagonist activity. Prolonged nature of antihistaminic effect may result from the drug slow dissociation from the H₁ receptors or the formation of the active metabolite, desloratadine. The presence of a carboxyethyl ester moiety in Loratadine may limit distribution of the drug across the blood-brain barrier into the CNS. While the drug exhibits less affinity for histamine H₁ receptor in the CNS, with a resultant decreased potential for adverse CNS effects, such as drowsiness, compare with many other antihistamines. Loratadine has low affinity for cholinergic receptor therefore possesses less anticholinergic-like effect such as dryness of the nose, mouth, throat, or lips. During clinical studies of patients receiving Loratadine for weeks (2-24 weeks), decreased efficacy of inhibition of skin reactivity to allergen or histamine does not occur, as in the therapy of first generation antihistamines.
Pharmacokinetics: Absorption: Following oral administration, Loratadine is rapidly absorbed from the GI tract. Antihistaminic effect appears within 1-4 hours. Peak effect results within 8-12 hours. The effect persists for 24 hours or longer. Food may increase bioavailability and delay time-to-peak plasma concentration of the drug and metabolite by about 1 hour.
Distribution: Loratadine is highly bound (97% to 99%) and its active major metabolite desloratadine moderately bound (73% to 77%) to plasma proteins. Loratadine and its active metabolites are distributed into breast milk. Non significant amount of the drug appears to cross the blood-brain barrier.
Metabolism: Loratadine is metabolized in the liver by the cytochrome P-450 (CYP) microsomal enzyme system, mediated principally by CYP3A4 and to a lesser extent by CYP2D6. In the presence of a CYP3A4 inhibitor, Loratadine is principally metabolized to desloratadine by the CYP2D6 isoenzyme. In patients with hepatic impairment, the half-life of Loratadine and desloratadine may be prolonged.
Elimination: The elimination half-life of Loratadine and desloratadine are 8.4 and 28 hours, respectively. 40% of Loratadine is excreted into the urine and 40% in the feces, mostly metabolites.

Relief of symptoms associated with allergic rhinitis, such as sneezing, nasal discharge (rhinorrhea) and itching, as well as ocular itching and burning. Relief of symptom and signs of chronic urticarial and other allergic dermatologic disorders.

Adult and children 12 years of age and older: 1 tablet (10 mg) once daily.

Overdose and Treatment: In adults, drowsiness, tachycardia, and headache have been reported after overdoses (40-180 mg) of Loratadine tablets. In children, extrapyramidal manifestations and palpitations have been reported with overdoses (exceeding 10 mg) of Loratadine syrup.
Treatment involves symptomatic and supportive care. In acute overdosage, the stomach should be emptied immediately by inducing emesis with ipecac syrup. Activated charcoal administered after emesis may be useful in preventing absorption of Loratadine. Gastric lavage with a 0.9% sodium chloride solution may be performed, if induction of vomiting is unsuccessful or contraindicated.
Loratadine is not removed by hemodialysis, and not known whether it is removed by peritoneal dialysis.

Z-DEEN (10 MG TABLET) is contraindicated in patients who are hypersensitive to Loratadine or any component of the formulation.

For allergy relief, not for common cold.
Warnings (based on the Ministry of Public Health's Announcement): 1. This medicine may cause drowsiness in some patients. Patients who drive or operate machinery or perform activities which may be at risk of falling from the height should take their response to the medicinal product into account.
2. Avoid ethanol or composition with alcohol.
3. Use with caution in children younger than 2 years of age, pregnancy in first trimesters, and women feeding breast milk.
4. If arrhythmia occurs, discontinue the drug and contact a clinician.
5. Use with caution in patients with hepatic impairment.
6. Concomitantly administration of Loratadine and macrolide antibiotics such as erythromycin, clarithromycin; or imidazole antifungals such as ketoconazole, itraconazole, fluconazole; or HIV protease inhibitors; or any CYP450 inhibitors such as cimetidine, metronidazole, zafirlukast, SSRIs, etc. increases drug plasma level 2-3 times. Prolonged QT interval have also been reported.
7. Avoid concomitantly administration of Loratadine with medications which prolonged QT interval such as calcium channel blockers (e.g. bepridil, verapamil), tricyclic antidepressant, cisapride, quinidine.

Patients with severe liver impairment should be administered a lower initial dose because they may have reduced clearance of Loratadine. An initial dose of 10 mg every other day is recommended for adults and children weighing more than 30 kg, and for children weighing 30 kg or less, 5 mg is recommended.
Effects on ability to drive or use machines: Loratadine had no or negligible influence on the ability to drive and use machines.

Pregnancy: Safety for use of Loratadine during pregnancy has not been established. The drug should be used during pregnancy only when the potential benefits justify the possible risks to the fetus.
Lactation: Loratadine is excreted in breast milk, therefore the use of Loratadine is not recommended in breast-feeding women.

Central nervous system: drowsiness, fatigue, headache.
Dermatologic: skin rash.
Gastrointestinal: gastritis, nausea, dry mouth.
Hypersensitivity: hypersensitivity reaction.
Rare: alopecia, anaphylaxis, dizziness, hepatic insufficiency, palpitations, seizure, tachycardia, angioedema.

Concomitantly administration of Loratadine with ketoconazole, erythromycin and cimetidine may increase plasma concentration of both Loratadine and active metabolite.

Store below 30°C.

Antihistamines & Antiallergics

R06AX13 - loratadine ; Belongs to the class of other antihistamines for systemic use.

NDD