INFORMATION FOR HEALTH PROFESSIONALS
Home | Consumers | Health Professionals | Regulatory | Other | Hot Topics | Search
Home | Consumers | Health Professionals | Regulatory | Other | Hot Topics | Search
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.
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.
APO-LORATADINE is indicated for the relief of:
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.
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.
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.
In clinical trials the incidences of adverse effects associated with
APO-LORATADINE have been comparable to that of the placebo. These trials showed
that there were no clinically significant sedative or anticholinergic
properties. During clinical trials fatigue, sedation, headache and dry mouth
were rarely reported. These adverse effects were also reported with similar
incidence in placebo-treated patients.
During the marketing of loratadine, alopecia, anaphylaxis and abnormal hepatic
function have been reported rarely.
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.
Pharmaceutical Precautions
Store below 25°C.
Protect from heat, light and moisture.
Pharmacy Only Medicine
Bottles of 100 tablets.
Blister packs of 15 and 30 tablets.
Further Information
Tablets contain Lactose.
Apotex NZ Ltd
32 Hillside Road
Glenfield
Private Bag 102-995
North Shore Mail Centre
Auckland
Tel: (09) 444-2073
Fax: (09) 444 2951
15 March 2001