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

Adults and children over 12 years

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

 

Children 6 to 12 years

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

 

Children 2 to 5 years

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

 

Children 1 to 2 years

One 2.5 ml 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.

§ 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.

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 (sorbitol content).

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.

§ 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.

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

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.

To report any side effect(s):

·   Saudi Arabia:

 

The National Pharmacovigilance and Drug Safety Centre (NPC) § Fax: +966-11-205-7662 § Call NPC at: +966-11-2038222, Ext.: 2317-2356-2353-2354-2334-2340. § Toll free phone: 8002490000 § E-mail: npc.drug@sfda.gov.sa § Website: www.sfda.gov.sa/npc

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.

ATC Code: R06AB04

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.

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.

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 H₁antihistamines. 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 1-10µg/L and oral doses of 0.2-1 mg/kg antagonise histamine- induced bronchospasm in guinea pigs.

The excipients in each 100 are:

 

Citric acid monohydrate

Sodium benzoate

Orange flavour

Glycerol

Sorbitol 70% solution

FD&C Yellow No. 6 (Sunset yellow)

Purified water to

Not applicable

5 years from the manufacturing date. The expiry date refers to the last day of the month.

§ Keep in a safe place, out of the reach and sight of children.

§ Store below 30º C, Protect from light.

§ Use within 3 months after opening

Zistan syrup is available with an amber colored type III glass bottle size of 100 ml with child resistant cap.

Not applicable