SUMMARY OF PRODUCT CHARACTERISTICS

1    NAME OF THE MEDICINAL PRODUCT

Allergy Relief Antihistamine 2mg/5ml Syrup

Boots Allergy Relief 1 Year Plus Antihistamine 2mg/5ml Syrup

Chlorphenamine Maleate 2mg/5ml Oral Solution

Boots Allergy Relief 1 Year Plus Antihistamine 2mg/5ml Oral Solution

2    QUALITATIVE AND QUANTITATIVE COMPOSITION

Active ingredient    mg/5ml

Chlorpheniramine maleate    2.0

(INN Name: Chlorphenamine maleate)

For excipients, see 6.1

3    PHARMACEUTICAL FORM

Syrup

4    CLINICAL PARTICULARS

4.1    Therapeutic indications

For the symptomatic relief of hayfever, vasomotor rhinitis, urticaria, angioneurotic oedema, reactions to food or medicines, serum reactions and insect bites.

4.2    Posology and method of administration

Adults and children over 12 years

Two 5ml doses every four to six hours up to a maximum of six doses in 24 hours as required.

Children 6 to 12 years

One 5ml dose every four to six hours up to a maximum of six doses in 24 hours as required.

Children 2 to 5 years

One 2.5ml dose every four to six hours up to a maximum of six doses in 24 hours as required.

Children 1 to 2 years

One 2.5ml dose twice a day up to a maximum of two doses in 24 hours as required. Children under 1 year Not recommended.

Elderly

The normal adult dose is appropriate for the elderly.

For oral administration.

4.3 Contraindications

Acute asthma, hypersensitivity to any of the ingredients or other antihistamines. Premature infants or neonates because of their increased susceptibility to the antimuscarinic effects. This medicine should not be given to patients taking monoamine oxidase inhibitors (MAOIs) or within 14 days of stopping such treatment.

4.4 Special warning and precautions for use

This medicine should be given with caution to patients with epilepsy, severe cardiovascular disorders, liver disorders, glaucoma, urinary retention, prostatic enlargement, pyloroduodenal obstruction, asthma, bronchitis, bronchiectasis, thyrotoxicosis and severe hypertension.

Special care should be taken when using chlorpheniramine maleate in children and the elderly as they are more prone to developing neurological anticholinergic effects.

Warning: May cause drowsiness. If affected do not drive or operate machinery. Avoid alcoholic drink.

If symptoms do not go away within 5 days talk to your pharmacist or doctor. Keep all medicines out of the reach of children.

Although most antihistamines should be avoided by patients with porphyria, chlorpheniramine maleate has been used and is thought to be safe.

Patients with rare hereditary problems of fructose intolerance should not take this medicine (maltitol content).

4.5 Interaction with other medicinal products and other forms of interaction

This medicine may enhance the sedative effects of alcohol, hypnotics, anxiolytics sedatives, opioid analgesics and neuroleptics.

The antimuscarinic effects of chlorpheniramine are enhanced by other antimuscarinic drugs and both antimuscarinic and sedative effects are enhanced by monoamine oxidase inhibitors (concurrent therapy with which is contraindicated, see 4.3 above) and tricyclic antidepressants.

Metabolism of phenytoin may be inhibited by chlorpheniramine with the possible development of phenytoin toxicity.

4.6 Pregnancy and lactation

There are no adequate controlled studies of chlorpheniramine in pregnant women and this medicine should therefore not be used during pregnancy. Chlorpheniramine may be secreted in breast milk and its use is not recommended in nursing mothers because of the risk of adverse effects, such as unusual excitement or irritability in infants. Chlorpheniramine may also inhibit lactation.

4.7 Effects on ability to drive and use machines

Chlorpheniramine may cause blurred vision, dizziness, drowsiness and interfere with human performance and therefore may seriously influence the ability to drive and operate machinery.

4.8 Undesirable effects

The product may cause drowsiness, which may progress to deep sleep, headache, dizziness, psychomotor impairment, inability to concentrate, lassitude, irritability and antimuscarinic effects such as urinary retention, dry mouth and blurred vision. Gastrointestinal disturbances may occur including abdominal pain, dyspepsia and anorexia. Paradoxical CNS stimulation may occur especially in children or after high doses. Skin rashes including exfoliative dermatitis and photosensitivity reactions and hypersensitivity reactions including urticaria may occur. Other side effects include convulsions, sweating, myalgia, paraesthesia, tinnitus, palpitations, tachycardia, arrhythmias, chest pain, haemolytic anaemia and other blood dyscrasias, extrapyramidal effects, tremor, liver dysfunction, including hepatitis and jaundice, sleep disturbances, including nightmares, depression, hypotension, hair loss, thickening of bronchial secretions and confusional psychosis in the elderly.

Glycerol may cause headache, stomach upset and diarrhoea.

Sodium benzoate is a mild irritant to the skin, eyes and mucous membranes. It may increase the risk of jaundice in newborn babies.

Overdose

Overdosage with chlorpheniramine is associated with antimuscarinic, extrapyramidal, gastrointestinal and CNS effects. In infants and children, CNS stimulation predominates over CNS depression, causing ataxia, excitement, tremors, psychosis, hallucinations and convulsions. Hyperpyrexia may also occur. Other symptoms of overdosage in children include dilated pupils, dry mouth, facial flushing. Deepening coma and cardiorespiratory collapse may follow, and even death. In adults CNS depression is more common with drowsiness, coma and convulsions, progressing to respiratory failure or possibly cardiovascular collapse including arrhythmias.

In severe overdosage the stomach should be emptied. Activated charcoal has been given as have saline laxatives. Convulsions may be controlled with diazepam or phenytoin, although it has been suggested that CNS depressants should be avoided. Other treatment is supportive and symptomatic and may include artificial respiration, external cooling for hyperpyrexia and intravenous fluids. Vasopressors such as noradrenaline or phenylephrine may be used to counteract hypotension. Forced diuresis, peritoneal dialysis or haemodialysis appear to be of limited benefit.

5 PHARMACOLOGICAL PROPERTIES

5.1 Pharmacodynamic properties

Chlorpheniramine antagonises competitively the effects of histamine on H₁-receptors and also has weak antimuscarinic and moderate antiserotonin and local anaesthetic actions. It penetrates the brain and causes stimulation or sedation in animals.

5.2 Pharmacokinetic properties

Chlorpheniramine maleate is almost completely absorbed after administration by mouth, peak plasma concentrations occurring at about 2.5 to 6 hours. The drug is widely distributed including passage into the CNS, with a volume of distribution of between 1 and 10L/KG. About 70% of chlorpheniramine in the circulation is protein-bound. Chlorpheniramine undergoes some first pass metabolism and enterohepatic recycling. Chlorpheniramine is extensively metabolised, principally to inactive desmethylated metabolites which are excreted primarily in the urine, together with about 35% unchanged drug.

Only trace amounts are excreted in the faeces. The mean elimination half life has been reported to be about 30 hours, with mean values ranging from 2 to 43 hours.

5.3 Preclinical safety data

The antihistaminic potency of chlorpheniramine is confined mainly to its (+)-isomer. The racemate is similarly or slightly more toxic because of the contribution of (-)-isomer. The toxicity may therefore be non-specific, perhaps attributable to local anaesthetic action and the toxic effects (excitation/sedation, coma, convulsions and death) resemble those of other classic ^antihistamines. Toxic doses may cause hypotension attributable to myocardial depression, an effect which is clearer with the (-)-isomer.

The experimental data on the carcinogenicity and mutagenicity of chlorpheniramine indicate lack of these adverse effects, but the racemate and the (+)-isomer have shown some embryotoxicity in fertility tests.

Effective antihistaminic concentrations of chlorpheniramine in vitro are about 1-10pg/L and oral doses of 0.2-1 mg/kg antagonise histamine-induced bronchospasm in guinea pigs.

6    PHARMACEUTICAL PARTICULARS

6.1    List of excipients

Maltitol liquid Glycerol

Citric acid monohydrate Sodium benzoate

Flavour natural mint 513484E (including ethyl alcohol)

Purified water

6.2 Incompatibilities

Not applicable.

6.3 Shelf-Life 36 months.

6.4 Special Precautions for Storage

None.

6.5    Nature and contents of container

150ml, 200ml, 250ml and 300ml amber PET bottle with a child resistant polypropylene cap fitted with an expanded polyethylene liner and, when supplied with a syringe, a polyethylene plug.

Syringe composed of a natural polypropylene barrel and polyethylene pigmented white plunger (optional).

6.6    Instructions for Use, Handling and Disposal

Not applicable.

7    MARKETING AUTHORISATION HOLDER

The Boots Company PLC 1 Thane Road West Nottingham NG2 3AA

Trading as: BCM

8    MARKETING AUTHORISATION NUMBER

PL 00014/0606

9 DATE OF FIRST AUTHORISATION / RENEWAL OF THE AUTHORISATION

10 December 2003

10 DATE OF REVISION OF THE TEXT

12/11/2013