New Zealand Data Sheet APO-LORATADINE
Loratadine 10mg Tablets
APO-LORATADINE 10mg tablets are white, oval tablets (7.6mm x 5.1mm), deep-scored, engraved 'LO' over '10' on one side, 'APO' on the other. Each tablet contains 10mg of loratadine and typically weighs 105mg and
APO-LORATADINE is indicated for the relief of:
Symptoms associated with seasonal and perennial allergic rhinitis, such as sneezing, nasal discharge and itching, and ocular itching and burning.
Symptoms and signs of chronic urticaria and other allergic dermatological disorders.
Adults and children 12 years of age and over:
One APO-LORATADINE tablet once daily.
Children 2 - 12 years of age:
Bodyweight >30kg: one APO-LORATADINE tablet once daily. Bodyweight <30kg: Half an APO-LORATADINE tablet once daily.
APO-LORATADINE is contraindicated in patients who have shown hypersensitivity or idiosyncrasy to the drug or its components.
Do not exceed the recommended dose. In an 18-month carcinogenicity study in mice and a 2-year study in rats, loratadine was administered in the diet at doses up to 12 mg/kg (mice) and 25 mg/kg (rats). Male mice given 12 mg/kg had a significantly higher incidence of hepatocellular tumors. The 2-year study in rats showed no increase in the incidence of carcinogenicity in doses up to 25 mg/kg/day. In a 17-month study in monkeys, loratadine demonstrated no functional impairment of the immune system as indicated by mortality, peripheral leucocyte count or incidences of inflammatory reactions, autoimmune disease and malignancy. Specific studies investigating the effect of loratadine on immune function in man have not been performed. Adverse effects on male fertility have occurred when loratadine was administered to rats at doses greater than 24 mg/kg/day. The clinical relevance of this observation is unknown.
Use in Pregnancy and Lactation
Category B1 The safe use of loratadine during pregnancy or lactation has not been established and therefore the compound should only be used if the potential benefit outweighs the potential risk to the fetus or the infant. Since loratadine is excreted in breast milk and because of the increased risk of antihistamines for infants, particularly newborns and premature infants, a decision should be made whether to discontinue nursing or discontinue loratadine use.
Use in Children
The safety and efficacy of APO-LORATADINE in children younger than 2 years of age have not been established. Long term safety and efficacy of APO-LORATADINE in children between the ages of 2 and 12 have not been demonstrated. Therefore it is desirable that APO-LORATADINE not be administered to children between the ages of 2 and 12 for longer than 14 days, unless recommended by a physician.
Use in patients with Liver Impairment
Patients with severe liver impairment should be administered a lower initial dose because they may have reduced clearance of loratadine; an initial dose of 5mg once daily or 10mg every other day is recommended.
Driving/Use of Machinery
APO-LORATADINE is no more likely than placebo to cause sedation. APO-LORATADINE is presumed to be safe or unlikely to produce an effect on the ability to drive or use machinery. However, the individual response should be determined before driving or performing other tasks that require alertness.
In clinical studies, the incidence of adverse effects associated with loratadine has been comparable to that of placebo. In these trials, loratadine has shown no clinically significant sedative or anticholinergic properties. The most commonly reported side effects for loratadine in excess of placebo include headache, sedation, fatigue, nausea and dry mouth. Adverse effects occurring very rarely during the post-marketing period are listed below: Immune system disorders: Anaphylaxis Nervous system disorders: Dizziness Cardiovascular disorders: Hypertension, hypotension, palpitation, tachycardia, syncope Gastrointestinal disorders: Dyspepsia, diarrhoea, constipation, abdominal/gastric pain Hepatobiliary disorders: Abnormal hepatic function Skin and subcutaneous tissue disorders: Rash, alopecia, pruritus, angioedema
When administered concomitantly with alcohol, loratadine has no potentiating effects as measured by psychomotor performance studies. Increases in plasma concentrations of loratadine have been reported after concomitant use with ketoconazole, erythromycin or cimetidine in controlled clinical trials, but without clinically significant changes (including electrocardiographic). Other drugs known to inhibit hepatic function metabolism should be coadministered with caution until definitive interaction studies can be completed.
Laboratory Test Interactions
APO-LORATADINE should be discontinued approximately 48 hours prior to skin testing procedures since antihistamine may prevent or diminish otherwise positive reactions to dermal reactivity indicators.
Somnolence, tachycardia and headache have been reported with overdoses of loratadine. A single acute ingestion of 160mg produced no adverse effects. In the event of overdosage, treatment, which should be started immediately, is symptomatic and supportive. Discontinuation of use, gastric lavage or induction of emesis (except in patients with impaired consciousness) and support of vital functions are advised.
Loratadine, a piperidine derivative, is a potent long-acting, non-sedating tricyclic antihistamine with selective peripheral H1-receptor antagonistic activity. Loratadine has no significant sedative or antimuscarinic activity. Loratadine does not readily penetrate into the CNS. Loratadine exhibits greater affinity for peripheral H1-receptors than for central H1-receptors. Loratadine does not exhibit anticholinergic activity in animals.
Loratadine is rapidly absorbed from the gastro-intestinal tract after oral administration with peak plasma levels occurring about one hour after dosing. Bioavailability is increased and time to peak plasma concentrations delayed when administered with food. Loratadine is extensively metabolised. The major metabolite, descarboethoxyloratadine (desloratadine or SCH 34117), has potent antihistamine activity and this metabolite corresponds to 1-2% of the dose. Loratadine is approximately 98% bound to plasma proteins. Descarboethoxyloratadine is less extensively bound (approximately 75%). Loratadine and its metabolites have been detected in breast milk but do not appear to cross the blood-brain barrier to a significant extent. Approximately 82% of the dose is excreted in the urine (40%) and faeces (42%) mainly in the form of metabolites over a 10 day period. Approximately 27% of the dose is eliminated in the urine during the first 24 hours largely in the conjugated form. The half-life of loratadine in normal volunteers is 15 hours, while that of descarboethoxyloaratadine is 12 hours. The terminal elimination phase half-life, based on plasma radioactivity, is approximately 46 hours. Onset of action occurs rapidly after oral administration. Symptom relief will occur in as little as 10 to 20 minutes from the first dose, with a mean onset of relief obtainable in 27 minutes in patients receiving 10mg of loratadine. By 45 minutes all patients should experience relief.
Other
Chemical Structure
List of excipients
Croscarmellose sodiumHydrated silica Lactose monohydrate Magnesium stearate Microcrystalline cellulose
36 months from date of manufacture Store below 25C. Protect from heat, light and moisture.
Bottles of 100 tablets. Blister packs of 15 and 30 tablets. Not all pack sizes may be available.
Pharmacy Only Medicine
Apotex NZ Ltd 32 Hillside Road Glenfield Private Bag 102-995 North Shore Mail Centre Auckland Tel: (09) 444-2073 Fax: (09) 444 2951
12 September 2013