Dextromethorphan + Pseudoephedrine + Triprolidine

Uses

This is used for the symptomatic relief of upper respiratory tract disorders accompanied by non-productive cough which benefits from the administration of a nasal decongestant, a histamine H1 receptor antagonist and an antitussive combination.

Dextromethorphan + Pseudoephedrine + Triprolidine is also used to associated treatment for these conditions: Allergic cough, Common Cold, Common Cold/Flu, Cough, Cough caused by Common Cold, Coughing caused by Allergies, Coughing caused by Bronchitis, Coughing caused by Flu caused by Influenza, Fever, Flu caused by Influenza, Headache, Irritative cough, Itching of the nose, Itching of the throat, Nasal Congestion, Pseudobulbar affect, Rhinorrhoea, Sneezing, Upper respiratory symptoms, Watery itchy eyes, Airway secretion clearance therapy, Bronchodilation, Oropharyngeal antisepsisAllergic Rhinitis (AR), Allergies, Common Cold, Common Cold Associated With Cough, Common Cold/Flu, Cough, Cough caused by Common Cold, Eye allergy, Fever, Flu caused by Influenza, Headache, Irritative cough, Nasal Allergies, Nasal Congestion, Nasal Congestion caused by Common Cold, Pain, Perennial Allergy, Priapism, Respiratory Allergy, Rhinorrhoea, Seasonal Allergic Rhinitis, Seasonal Allergies, Sinus Congestion, Sinusitis, Sneezing, Sore Throat, Symptoms of Acute Bronchitis Accompanied by Coughing, Throat irritation, Upper Respiratory Tract Infection, Upper respiratory tract congestion, Upper respiratory tract signs and symptoms, Dry cough, Minor aches and pains, Sinus pain, Watery itchy eyes, Airway secretion clearance therapyNasal Congestion, Perennial Allergic Rhinitis (PAR), Seasonal Allergic Conjunctivitis, Seasonal Allergic Rhinitis, Upper respiratory tract signs and symptoms, Vasomotor Rhinitis, Mild Angioedema, Mild urticaria, Upper respiratory discomfort

How Dextromethorphan + Pseudoephedrine + Triprolidine works

Dextromethorphan is an agonist of NMDA and sigma-1 receptors. It is also an antagonist of α3/β4 nicotinic receptors.[A10589] However, the mechanism by which dextromethorphan's receptor agonism and antagonism translates to a clinical effect is not well understood.

Pseudoephedrine acts mainly as an agonist of alpha adrenergic receptors and less strongly as an agonist of beta adrenergic receptors.[A10896] This agonism of adrenergic receptors produces vasoconstriction which is used as a decongestant and as a treatment of priapism. Pseudoephedrine is also an inhibitor of norepinephrine, dopamine, and serotonin transporters.

The sympathomimetic effects of pseudoephedrine include an increase in mean arterial pressure, heart rate, and chronotropic response of the right atria. Pseudoephedrine is also a partial agonist of the anococcygeal muscle. Pseudoephedrine also inhibits NF-kappa-B, NFAT, and AP-1.

Triprolidine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.

Dosage

Dextromethorphan + Pseudoephedrine + Triprolidine dosage

Adults: 2 tea-spoon three times daily.

Children:

• Over 12 years: 2 tea-spoon three times daily.
• 6 to 12 years: 1 tea-spoon three times daily.
• 2 to 5 years: 1/2 tea-spoon three times daily.
• 6 months to 2 years: 1/4 tea-spoon three times daily or on advice of a physician only.

Side Effects

Central nervous system depression or excitation may occur, drowsiness being reported most frequently. Sleep disturbance and rarely, hallucinations have been reported. Skin rashes with without irritation, tachycardia, dryness of mouth, nose and throat have occasionally been reported. Urinary retention has been reported occasionally in male patients in which prostatic enlargement could be an important predisposing.

Toxicity

A dextromethorphan overdose may present as nausea, vomiting, stupor, coma, respiratory depression, seizures, tachycardia, hyperexcitability, toxic psychosis, ataxia, nystagmus, dystonia, blurred vision, changes in muscle reflexes, and serotonin syndrome. Overdose should be managed through symptomatic and supportive measures.

The oral LD₅₀ of pseudoephedrine is 2206mg/kg in rats and 726mg/kg in mice.

Patients experiencing an overdose of pseudoephedrine may present with giddiness, headache, nausea, vomiting, sweating, thirst, tachycardia, precordial pain, palpitations, difficulty urinating, muscle weakness, muscle tension, anxiety, restlessness, insomnia, toxic psychosis, cardiac arrhythmias, circulatory collapse, convulsions, coma, and respiratory failure. Treat overdose with symptomatic and supportive treatment including removal of unabsorbed drug.

Symptoms of overdose include drowsiness, weakness, inco-ordination, difficulty with micturition, respiratory depression, hypotension, agitation, irritability, convulsions, hypertension, palpitation and tachycardia.

Precaution

This combination may cause drowsiness and impair performance in tests of auditory vigilance. It may also impair the patients ability to drive and also to use machineries. Although there are no objective data, users of this syrup should avoid the concomitant use of alcohol nor other centrally acting sedatives.

Although pseudoephedrine has virtually no blood pressure effect in patients with normal blood pressure, this combination should be used with caution in patients taking antihypertensive agents, tricyclic antidepressants or other sympathomimetic agents such as decongestant, appetite suppressants and amphetamine like psychostimulants. As with other sympathomimetic agents caution should be exercised in patients with hypertension, heart disease, diabetes, hyperthyroidism, elevated intraocular pressure and prostatic enlargement.

This combination should not be used for persistent or chronic cough such as occurs with smoking, asthma, or emphysema or where cough is accompanied by excessive secretions unless directed by a physician.

Interaction

Concomitant use of this combination with sympathomimetic agents such as decongestants, tricyclic antidepressants, appetite suppressants and amphetamine- like psychostimulants or with monoamine oxidase inhibitors which interfere with the catabolism of sympathomimetic amines may occasionally cause a rise in blood pressure. Because of its pseudoephedrine content, this syrup partially reverse the hypotensive action of drugs which interfere with sympathetic activity including guanethidine, methyldopa, alpha-adrenergic blocking agents.

Volume of Distribution

The volume of distribution of dextromethorphan is 5-6.7L/kg.

The apparent volume of distribution of pseudoephedrin is 2.6-3.3L/kg.

Elimination Route

A 30mg oral dose of dextromethorphan reaches a C_max of 2.9 ng/mL, with a T_max of 2.86 h, and an AUC of 17.8 ng*h/mL.

A 240mg oral dose of pseudoephedrine reaches a C_max of 246.3±10.5ng/mL fed and 272.5±13.4ng/mL fasted, with a T_max of 6.60±1.38h fed and 11.87±0.72h fasted, with an AUC of 6862.0±334.1ng*h/mL fed and 7535.1±333.0ng*h/mL fasted.

Rapidly absorbed in the intestinal tract.

Half Life

Dextromethorphan has a half life of 3-30 hours.

The mean elimination half life of pseudoephedrine is 6.0h.

4 to 6 hours.

Clearance

A 60mg oral dose of pseudoephedrine has a clearance of 5.9±1.7mL/min/kg.

Elimination Route

55-75% of an oral dose is detected in the urine as unchanged pseudoephedrine.

Pregnancy & Breastfeeding use

There are no specific data on use of this combination during pregnancy. Caution should therefore be exercised by balancing the potential benefits of treatment of the mother against any possible hazards to the developing fetus.

Contraindication

This combination is contraindicated in patients with a known hypersensitivity to dextromethorphan, pseudoephedrine or triprolidine. Contraindicated in persons under treatment with monoamine oxidase within 2 weeks of stopping such treatment. It is contraindicated in patients with severe hypertension or severe coronary artery disease.

Acute Overdose

Symptoms: In mild overdose, tachycardia, hypertension, vomiting, mydriasis, diaphoresis, nystagmus, euphoria, loss of motor coordination, and giggling; in moderate intoxication, in addition to those listed above, hallucinations and a plodding ataxic gait; in severely intoxication, agitation or somnolence.

Management: treatment is symptomatic and supportive. Naloxone may be useful in reversing toxicity.

Storage Condition

Store in a dry & cool place. Do not refrigerate. Protect from direct sunlight

Innovators Monograph

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