Each 5 ml contains:

active ingredients: guaifenesin – 100.0 mg, chlorpheniramine maleate- 2.0 mg, phenylpropanolamine HCl – 5.0 mg;

excipients: sucrose, sorbitol 70% solution, sodium citrate, citric acid, methylparaben, propylparaben, aroma, color, ethanol 96%, water purified.

Guaifenesin acts as an expectorant by increasing the volume and reducing the viscosity of secretions in the trachea and bronchi. Thus, it may increase the efficiency of the cough reflex and facilitate removal of the secretions.

Phenylpropanolamine hydrochloride is a sympathomimetic amine, which provides temporary relief of nasal congestion.

Chlorpheniramine maleate is an antihistamine that provides temporary relief of runny nose, sneezing and watery and itchy eyes.

The propose therapeutic dose in adults is 5 ml of syrup every 6-8 hours. The usual therapeutic dose in pediatric between 2-6 years old is 1.25-2.5 ml every 6-8 hours. The usual therapeutic dose in pediatric between 6-12 years old is 2.5-5 ml every 6-8 hours.

Do not take more than 4 doses a day.

Unless your doctor approves, do not use these products if you have heart disease, high blood pressure, thyroid disease, diabetes, high pressure within the eye (glaucoma), an enlarged prostate gland, or a breathing problem such as emphysema or chronic bronchitis.

If you become dizzy or nervous, or have trouble sleeping, stop taking these products and check with your doctor.

You should also check with your doctor immediately if you have a severe sore throat that lasts for more than 2 days, or if your sore throat is accompanied or followed by fever, headache, rash, nausea, or vomiting.

These products may cause drowsiness. Be especially cautious when driving, and when operating machinery. This formulation can also cause excitability, especially in children.

Check with your doctor before using these products if you consume 3 or more alcoholic drinks a day. The acetaminophen they contain can cause liver damage.

If you are taking a tranquilizer, or a sleep aid, do not take this medication without your doctor’s approval; the combination could cause extreme drowsiness. For the same reason, avoid alcohol while taking these products.

Guaifenesin is reported to increase the volume and reduce the viscosity of tenacious sputum and is used as an expectorant for productive cough. Guaifenesin is thought to act as an expectorant by increasing the volume and reducing the viscosity of secretions in the trachea and bronchi. Thus, it may increase the efficiency of the cough reflex and facilitate removal of the secretions; however evidence for this is limited and conflicting.

Pharmacokinetics

Guaifenesin is absorbed from the gastrointestinal tract. It is metabolized and then excreted in the urine, as inactive metabolites.

Uses and administration

Guaifenesin is indicated as an expectorant in the temporary symptomatic management of cough due to minor upper respiratory infections and related conditions, such as sinusitis, pharyngitis, and bronchitis, when these conditions are complicated by viscous mucus and congestion.

Guaifenesin has been given by mouth in doses of 200 to 400 mg every 4 hours. Children aged 6 to 12 years may be given 100 to 200 mg every 4 hours, and children aged 2 to 6 years 50 to 100 mg every 4 hours.

Adverse effects and precautions

Gastrointestinal discomfort, nausea, and vomiting have occasionally been reported with guaifenesin, particularly in very large doses.

Abuse: urinary calculi have been reported in patients consuming large quantities of over-the counter preparations containing guaifenesin.

Porphyria: guaifenesin is considered to be unsafe in patients with porphyria because it has been shown to be porphyrogenic in animals.

Pregnancy: pregnancy category C.

Breast-feeding: it is known whether Guaifenesin is distributed into breast milk. However, problems in humans have not been documented.

Pediatric: caution is recommended in children up to 12 years of age with persistent or chronic cough, such as occurs with asthma, or if the cough is accompanied by excessive phlegm (mucus). The condition of these children may need a physician’s evaluation before Guaifenesin is administered.

Guaifenesin should not be given to children younger than 2 years of age unless recommended by physician.

Pharmacology

Phenylpropanolamine is largely indirect-acting sympathomimetic with an action similar to that of ephedrine but less active as a CNS stimulant.

Pharmacokinetics

Phenylpropanolamine is readily and completely absorbed from the gastrointestinal tract, peak plasma concentrations being achieved about 1 to 2 hours after oral administration. It undergoes some metabolism in the liver, to an active hydroxylated metabolite, but up to 80 to 90% of a dose is excreted unchanged in the urine within 24 hours. The half-life has been reported to be about 3 to 5 hours.

Uses and administration

Phenylpropanolamine is given by mouth as the hydrochloride for the symptomatic treatment of nasal congestion. It is frequently used in combination preparations for relief of cough and cold symptoms.

In the management of nasal congestion, Phenylpropanolamine hydrochloride is given in usual doses of up to 25 mg three of four times daily by mouth (a maximum dose 100 mg).

Other uses of Phenylpropanolamine include the control of urinary incontinence in some patients. It has also been given in the management of some forms of priapism. Phenylpropanolamine has been used to suppress appetite in the management of obesity, but the use of stimulants in no longer recommended.

Adverse effects

The commonest adverse effects of Phenylpropanolamine are tachycardia, anxiety, restlessness, and insomnia. Tremor, dry mouth, impaired circulation to the extremities, hypertension, and cardiac arrythmias may also occur.

Paranoid psychosis, delusions, and hallucinations may also follow Phenylpropanolamine overdosage.

Tolerance to the therapeutic effects of Phenylpropanolamine has been reported with prolonged administration.

Precautions

Phenylpropanolamine should be given with care to patients with hyperthyroidism, diabetes mellitus, renal impairment, or angle-closure glaucoma. In patients with prostatic enlargement, Phenylpropanolamine may increase difficulty with micturition.

Irritability and distributed sleep have been reported in breast-fed infants.

Interactions

Administration of Phenylpropanolamine may cause a hypertensive crisis in patients receiving and MAOI (including an RIMA). Phenylpropanolamine should be avoided or used with care in patients undergoing anaesthesia with cyclopropane, halothane, or other volatile anaesthetics. An increased risk of arrhythmias may occur if given to patients receiving cardiac glycosides, quinidine, or trycyclic antidepressants, and there is an increased risk of vasoconstrictor or pressor effects in patients receiving ergot alkaloids or oxytocin.

Pharmacology

Chlorpheniramine maleate, an alkylamine derivative, is a sedating antihistamine that causes a moderate degree of sedation; it also has antimuscarinic activity. Chlorpheniramine maleate diminishes or abolishes the major actions of histamine in the body by competitive, reversible blockade of histamine H1-receptor sites on tissues; it does not inactivate histamine or prevent its synthesis, nor, in most cases, its release. Histamine H1 receptors are responsible for vasodilation, increased capillary permeability, flare and itch reactions in the skin, and to some extent for contraction of smooth muscle in the bronchi and gastrointestinal tract.

Chlorpheniramine is a racemic mixture; the dextrorotatory isomer, dexchlorpheniramine, has approximately twice the activity of Chlorpheniramine by weight.

Pharmacokinietics

Chlorpheniramine maleate is absorbed relatively slowly from the gastrointestinal tract, peak plasma concentrations occurring about 2.5 to 6 hours after administration by mouth. Bioavailability is low, values of 25 to 50% having been reported. Chlorpheniramine appears to undergo considerable first-pass metabolism. About 70% of Chlorpheniramine in the circulation is bound to plasma proteins. There is wide inter-individual variation in the pharmacokinetics of Chlorpheniramine; values ranging from 2 to 43 hours have been reported for the half-life. Chlorpheniramine is widely distributed in the body, including passage into the CNS.

Chlorpheniramine maleate is extensively metabolized. Metabolites include desmethyl- and didesmethylchlorpheniramine. Unchanged drug and metabolites are excreted primarily in the urine; excretion is dependent on urinary pH and flow rate: Only trace amounts have been found in the feces.

A duration of action of 4 to 6 hours has been reported; this is shorter than may be predicted from pharmacokinetic parameters.

More rapid and extensive absorption, faster clearance, and a shorter half-life have been reported in children.

Uses and administration

Chlorpheniramine maleate is used for symptomatic relief of allergic conditions including urticaria and angioedema, rhinitis, and conjunctivitis, and in pruritic skin disorders. It is common ingredient of compound preparations for symptomatic treatment of coughs and common cold.

Chlorpheniramine maleate is given by mouth in doses of 4 mg every 4 to 6 hours up to a maximum of 24 mg daily. Doses for children are: 1 to 2 years, 1 mg twice daily; 2 to 5 years, 1 mg every 4 to 6 hours (maximum 6 mg daily); 6 to 12 years, 2 mg every 4 to 6 hours (maximum 12 mg daily).

Adverse effects and treatment

The most common side-effect of the sedating antihistamines in CNS depression, with effects varying from slight drowsiness to deep sleep, and including lassitude, dizziness, and in coordination (although paradoxical stimulation may occasionally occur, especially at high doses in children or the elderly). These sedative effects, when they occur, may diminish after a few days of treatment.

Other side effects include headache, psychomotor impairment, and antimuscarinic effects, such as dry mouth, thickened respiratory-tract secretions, blurred vision, urinary difficulty or retention, constipation, and increased gastric reflux.

Occasional gastrointestinal side-effects include nausea, vomiting, diarrhea, or epigastric pain.

Palpitaions and arrhythmias have been reported.

Blood disorders, including agranulocytosis, leucopenia, haemolytic anaemia, and thrombocytopenia, although rare, have been reported.

Other adverse effects include convulsions, sweating, myalgia, paraesthesias, extrapyramidal effects, tremor, sleep disturbances, depression, confusion, tinnitus, hypotension, and hair loss.

Exfoliative dermatitis may develop.

Overdosage

Overdosage with sedating antihistamines is associated with antimuscarinic, extrapyramidal, and CNS effects. When CNS stimulation predominates over CNS depression, which is more likely in children or the elderly, it causes ataxia, excitement, tremors, psychoses, hallucinations, and convulsions; hyperpyrexia may also occur. Deepening coma and cardiorespiratory collapse may follow. In adults, CNS depression is more common with drowsiness, coma, and convulsions, progressing to respiratory failure and cardiovascular collapse.

Treatment of overdosage: treatment is symptomatic and supportive.

Precautions

Drowsiness is a major problem with the chlorpheniramine and those affected should not drive or operate machinery; alcohol should be avoided.

Because of its antimuscarinic actions chlorpheniramine should be used with care in conditions such as angle-closure glaucoma, urinary retention, prostatic hyperplasia, or pyloroduodenal obstruction.

Occasional reports of convulsions in patients taking chlorpheniramine also calls for caution in patients with epilepsy.

The dosage reduction may be necessary in renal impairment.

Chlorpheniramine should not be given to neonates owing to its increased susceptibility to antimuscarinic effects. Elderly patients are also more susceptible to many of the adverse effects of chlorpheniramine and, in particular, its inappropriate use for postural giddiness should be avoided.

Interactions

Chlorpheniramine may enhance the sedative effects of CNS depressants including alcohol, barbiturates, hypnotics, opioid analgesics, anxiolytic sedatives, and antipsychotics.

Chlorpheniramine has an additive antimuscarinic action with other antimuscarinic drugs, such as atropine and some antidepressants (both tricyclics and MAOIs).

Chlorpheniramine may suppress the cutaneous histamine response to allergen extracts and should be stopped several days before skin testing.

Chlorpheniramine might have delayed the hepatic metabolism of phenytoin thereby increasing the plasma concentrations.

A clear reddish colored, cherry flavored syrupy liquid.

Amber glass bottles containing 60 ml packed with leaflet in cardboard box.

3 years. Shelf life after opening the bottle is 6 months. Do not use after the expiration date.

To be dispensed without prescription.

Store in dry place at a temperature not higher than 15⁰C, out of the reach of children. Protect from light.