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Allerstat 180

Interpharma Industries Ltd
28/30 Salvation Road, Opebi-Ikeja, Lagos; 47 Morison Cres, Oregun Ikeja, Lagos
Tel: 01-8045232, 3451454-5
Fax: 01-3451175
Website: http://cadilapharma.com

Brand Name

Allerstat 180

Manufacturer

Manufactured by CADILA PHARMACEUTICALS LIMITED 1389, Dholka -387 810, INDIA

Therapeutic Class

Antihistamines, Systemic

Dosage Form, Composition & NAFDAC Registration Number (NRN)

Tablet(NRN:-): COMPOSITION: Each film coated tablet of Allerstat 180 contains: Fexofenadine Hydrochloride 180 mg Pack Size: Presentation: Pack of 10 tablets

Pharmacology

PROPERTIES: Fexofenadine, a pharmacologically active metabolite of Terfenadine, is an non-sedating antihistamine with selective peripheral H1 receptor antagonist activity. PHARMACOLOGICAL PROPERTIES: Pharmacodynamic properties: Fexofenadine hydrochloride is a non-sedating antihistamine Fexofenadine is an antihistamine with selective peripheral H1-receptor antagonist activity. Fexofenadine inhibited antigen-induced bronchospasm in sensitized guinea pigs and histamine release from peritoneal mast cells in rats. In laboratory animals, no anticholinergic or alpha 1 - adrenergic-receptor blocking effects were observed. Moreover, no sedative or other central nervous system effects were observed. Radiolabeled tissue distribution studies in rats indicated that fexofenadine does not cross the blood-brain barrier. Fexofenadine hydrochloride inhibits skin wheal and flare responses produced by histamine Injection. Following single and twice daily oral dose administration. Antihistaminic effects occurred within 1 hour, achieved a maximum of 2-3 hours, and lasted a minimum of 12. Maximum inhibition in skin wheal and flare areas were greater than 80%. There is no evidence of tolerance to these effects after 28 days of dosing. Clinical studies conducted in allergic rhinitis have shown that a dose of 120 mg is sufficient for 24 hour efficacy. Fexofenadine at concentrations 32 times greater than the therapeutic concentration in man had no effect on the delayed rectifier K+channel cloned from human heart. No Significant differences in QTc intervals were observed in allergic rhinitis patients given fexofenadine hydrochloride upto 240 mg twice daily for 2 weeks when compared to placebo Also, no significant change in QTc intervals was observed in healthy subjects given fexofenadine hydrochloride upto 60 mg twice daily for 6 months, and 240 mg once daily for up to 70 days, when compared to placebo. Fexofenadine inhibited antigen Induced bronchospasm in sensitised guinea pigs and inhibited histamine release from peritoneal mast cells. Pharmacokinetic properties: Fexofenadine hydrochloride is rapidly absorbed into the body following oral administration, with Tmax occurring at approximately 1-3 hours post dose. The mean Cmax value was approximately 427ng/mL and 494ng/mL following the administration of a 120 mg and 180 mg dose (once dally) respectively. Fexofenadine is 60-70% plasma protein bound. Fexofenadine undergoes negligible metabolism, as it was the only major compound identified in urine and faeces of animal and man. The plasma concentration profiles of fexofenadine follow a bi-exponential decline with a terminal elimination half-life ranging from 11 to 16 hours after multiple dosing. The single and multiple dose pharmacokinetics of fexofenadine are linear between 40 mg and 240 mg taken daily. The major route of elimination is believed to be via biliary excretion while upto 10% of ingested dose is excreted unci tanged through the urine PRECLINICAL SAFETY DATA: Dogs tolerated 450 mg/kg administered twice daily for 6 months and showed no toxicity other than occasional emesis Radiolabelled fexofenadine hydrochloride in tissue distribution studies of the rat indicated that fexofenadine did not cross the blood brain barrier Fexofenadine hydrochloride was found to be non-mutagenic in various in vitro and in vivo mutagenicity tests. The carcinogenic potential of fexofenadine hydrochloride was assessed using terfenadine studies with supporting pharmacokinetic studies showing fexofenadine hydrochloride exposure (via plasma AUC values). No evidence of carcinogenicity was observed in rats and mice given terfenadine (upto 150 mg/kg/day).

Indications

INDICATIONS: Allerstat is indicated for the relief of symptoms associated with allergic rhinitis and allergic skin conditions eg. chronic urticaria.

Contra-indications

CONTRA-INDICATIONS: The product is contraindicated in patients with known hypersensitivity to any of Its ingredients.

Precautions/Warnings

Interactions

INTERACTION WITH OTHER MEDICAMENTS AND OTHER FORMS OF INTERACTION: Fexofenadine does not undergo hepatic biotransformation and is therefore unlikely to interact with drugs that rely upon hepatic metabolism. Fexofenadine hydrochoride at doses of 120 mg twice daily has been safely coadministered with erythromycin (500 mg three times daily) and ketoconazole (400 mg once daily) under steady state conditions in healthy volunteers. An increase in the level of fexofenadine in plasma of 2-times was observed after coadministration of erythromycin or ketoconazole but this was not associated with any increase in adverse event or effects on the QT interval, compared to that seen when the drugs were given singly. Animal Studies have shown that the increase in plasma levels of fexofenadine observed after coadministration of erythromycin or ketoconazole, appears to be due to an increase in gastrointestinal absorption and either a decrease in biliary clearance or gastrointestinal secretion respectively. PREGNANCY AND LACTATION: No evidence of teratogenicity was observed in animal reproduction studies when terfenadine was given throughout organogenesis. No effects on male or female fertility or on prenatal or post-natal development were observed in terfenadine animal studies at non-maternally toxic doses. Data from supporting pharmacokinetic studies showing the extent of exposure to fexofenadine (an active metabolite of terfenadine) in the terfenadine animal studies demonstrate that they are relevant to the assessment of fexofenadine hydrochloride However, the effects of foetal exposure at the higher doses of fexofenadine tolerated in animals have not been examined. Allerstat should be used in pregnancy only if the potential benefit outweighs the potential risk to the foetus. There is no data on the content of human milk after administering fexofenadine hydrochloride. However, when terfenadine was administered to nursing mothers fexofenadine was found to cross into human breast milk. Therefore, Allerstat is not recommended for mothers breast

Adverse Effects

EFFECTS ON ABILITY TO DRIVE AND USE MACHINES: On the basis of the pharmacodynamic profile and reported adverse events it is unlikely that fexofenadine hydrochloride tablets will produce an effect on the ability to drive or use machines. In objective tests, fexofenadine hydrochloride has been shown to have no significant effects on central nervous system function. This means that patients may drive or perform tasks that require concentration. Fexofenadine did not cross the blood brain barrier in animal studies. ADVERSE REACTIONS: In placebo-controlled trials, adverse events were comparable in fexofenadine- and placebo- treated patients. Adverse events reported with fexofenadine include: - Common. headache - Uncommon; fatigue, drowsiness, nausea, tachycardia, palpitations, dry mouth, nose and/or throat, dyspepsia, and gastrointestinal disturbances (including diarrhoea). - Rare: taste disturbances, anaphylactic/ anaphylactoid reactions, dyspnea, chest tightness, increased hair loss! hair thinning, photosensitivity, dysmenorrhea, menstrual disorders. As with other non-sedating antihistamines, dizziness, nervousness, agitation. sleep disorders, insomnia or paroniria may infrequently be reported by patients. The incidence of such reports under fexofenadine was similar to the incidence under placebo

Dosage & Administration

DOSAGE AND METHOD OF ADMINISTRATION: • Allergic rhinitis: Adults and children aged 12 years and over the recommended dose of fexofenadine hydrochloride for adults and children aged 12 years and over is 120 mg once dally. Allergic skin conditions, e.g. chronic urticaria Adults and children aged 12 years and over The recommended dose of fexofenadine hydrochloride for adults and children aged 12 years and over is 180 mg Once dally. Children under 12 years of age. The efficacy and safety of fexofenadine hydrochloride has not been studied in children under 12 Special risk groups Studies in special risk groups (elderly, renally or hepatically impaired patients) indicate that it is not necessary to adjust the dose of fexofenadine hydrochloride in these patients. OVERDOSE: Most reports of fexofenadine hydrochloride over-dose contain limited information. However, dizziness, drowsiness, and dry mouth have been reported. Single doses upto 800 mg and doses upto 690 mg BID for 1 month or 240 mg QD for 1 year were studied in healthy subjects without the development of clinically significant adverse events as compared to placebo.

Storage/Handling Recommendations

Expiry date: Do not use later than the date of expiry Storage: Store below 25

Review Date

2017-01-27 09:29:26