Sivoloratadine Loratadine Tablets USP

SIVOLORATADINE

Loratadine Tablets USP 10 mg

 

COMPOSITION

Each SIVOLORATADINE tablet contains 10 mg Loratadine USP.

 

PHARMACOLOGICAL CLASSIFICATION

A.5.7.1 Antihistaminics.

 

PHARMACOLOGICAL ACTION

Loratadine is a second generation histamine (H1)-receptor antagonist

Loratadine exerts its action by competing with histamine for H1-receptor sites on effector cells. It prevents but does not reverse, responses mediated by histamine.

Loratadine does not cross the blood-brain barrier to any extent.

Pharmacokinetics

After oral administration loratadine is well absorbed from the gastrointestinal tract and peak plasma concentrations are reached within 1.5 hours. Ingestion of food may enhance absorption of loratadine. Loratadine undergoes extensive first pass metabolism via the cytochrome P450 system.

The major metabolite, desloratadine, is active. Loratadine is 97% protein bound, while desloratadine is less extensively protein bound (73 % to 77 %). The mean elimination half life for loratadine and desloratadine are 8.4 and 28 hours, respectively.

 

INDICATIONS

SIVOLORATADINE is indicated for the symptomatic relief of seasonal allergic rhinitis and chronic urticaria.

 

CONTRAINDICATIONS

Hypersensitivity to SIVOLORATADINE or to any of the ingredients in the preparation.

Cross sensitivity to other antihistamines.

Porphyria.

 

WARNINGS

Safety of SIVOLORATADINE in the elderly has not been established.

Safety of SIVOLORATADINE in children under two years of age has not been established.

SIVOLORATADINE should be used with caution in patients with:

Severe liver impairment, as reduced clearance of loratadine may occur. Dosage adjustment may be needed (See “DOSAGE AND DIRECTIONS FOR USE”).

Renal impairment -A lower starting dose should be used. In patients with chronic renal impairment (creatinine clearance of 30 mL/minute or less), both oral bioavailability and peak plasma concentration of loratadine may be increased. However, the elimination half-lives of loratadine and its active metabolite appear to be similar to those in individuals with normal renal function.

SIVOLORATAOINE may lead to drowsiness and impaired concentration, which may be aggravated by simultaneous intake of alcohol or other nervous system depressants (e.g. sedative, and tranquillisers). Caution should be used when driving a motor vehicle or operating machinery or performing potentially dangerous tasks, where loss of concentration may lead to accidents.

 

INTERACTIONS

Concomitant use of SIVOLORATADINE with inhibitors of the cytochrome P450 enzyme system; such as cimetidine, ketoconazole; clarithromycin and erythromycin, may increase the plasma concentration of SIVOLORATADINE.

 

PREGNANCY AND LACTATION

Safety and efficacy in pregnancy and lactation have not been established.

Loratadine and its metabolites have been detected in breast milk. Small amounts of SIVOLORATADINE entering breast milk may cause drowsiness or excitement in Infants.

 

DOSAGE AND DIRECTIONS FOR USE

Children 2 to 12 years of age:

Body weight lass than or equal to 30 kg: 5 mg (½ tablet) once daily.

Body weight more than 30 kg: 10 mg (1 tablet) once daily.

Adults and children over 1 years of age:

10 mg (1 tablet) once daily.

Adults with severe liver function impairment:

Initial dose is 5 mg (½ tablet) once daily or 10 mg (1 tablet) on alternate days.

Use of SIVOLORATADINE should be limited to 14 days.

 

SIDE-EFFECTS AND SPECIAL PRECAUTIONS

Side-effects:

Immune system disorders:

Less frequent: Allergic reactions, anaphylaxis.

Neuropsychiatric system disorders:

Frequent: Headache, somnolence, nightmares.

Less frequent: Sedation, nervousness, confusion, fatigue, convulsions, increased appetite or loss of appetite, abnormal coordination, and tremor.

Disorders of the special senses:

Less frequent: Ringing or buzzing in the ears and blurred vision.

Cardiovascular system disorders:

Less frequent: Cardiac arrhythmias, palpitations, tachycardia, and oedema.

Gastrointestinal system disorders:

Frequent: Dry mouth, gastrointestinal disorders, such as nausea and gastritis.

Less frequent: Constipation, diarrhoea.

Hepatobiliary system disorders:

Less frequent: Abnormal hepatic function, hepatitis or cholestasis.

Skin and subcutaneous tissue disorders:

Less frequent: Rash, increased sweating, photosensitivity.

The following side-effects have been reported and frequencies are unknown:

Alopecia.

Renal and urinary system disorders:

Less frequent: Difficult or painful urination.

Reproductive system and breast disorders:

Less frequent: Early menses.

 

Special Precautions

SIVOLORATADINE should be discontinued prior to skin tests using allergen extracts, as it may inhibit the cutaneous histamine response, thus producing false-negative results.

SIVOLORATADINE should be discontinued at least 48 hours before such tests.

SIVOLORATADINE should be used with caution in patients using other medication metabolised by the cytochrome P450 system and/ or when the following medical conditions exist:

Emphysema, prostatic hypertrophy, narrow-angle glaucoma, cardiovascular disorders, epilepsy and during acute attacks of asthma.

 

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT

(See “SIDE-EFFECTS AND SPECIAL PRECAUTIONS”).

Symptoms of overdose

Tachycardia, somnolence and headaches have been reported. In children, extrapyramidal manifestations and palpitations have been reported.

Treatment of overdose:

Treatment is symptomatic and supportive. After overdosage of SIVOLORATADINE, the stomach should be emptied immediately by inducing emesis or by gastric Iavage. Administration of activated charcoal after emesis may be useful in preventing absorption of SIVOLORATADINE. Saline cathartics may be of value to rapidly dilute bowel contents. SIVOLORATADINE is not cleared by haemodialysis.

 

IDENTIFICATION

White to off white colour round shape uncoated tablets having both side plain.

 

PRESENTATION

Alu-Alu Blister packs of 10 tablets. Such 10 blister packed in one carton with pack insert.

 

STORAGE INSTRUCTIONS

Store in cool and dry place, protect from light.

 

KEEP OUT OF REACH OF CHILDREN.

 

Mfg. Lic. No.: G/25/1749 

NAFDAC No.: B4-0088

 

Manufactured in India by

Globela Pharma Pvt. Ltd.

357, G.I.D.C., Sachin Surat -394 230,

Gujarat (India)

www.globelapharma.com

 

Sole Agent

Adpharm Pharmaceuticals Industries Limited

No 60. Ajao Road, Surulere,

Lagos State, Nigeria.

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