Lecope Dx

Uses

Dextromethorphan is used for Chronic dry cough or unproductive cough; Acute dry cough which is interfering with normal function or sleep.

Levocetirizine Dihydrochloride is used for the treatment of symptoms associated with allergic conditions such as seasonal allergic rhinitis, perennial allergic rhinitis and chronic idiopathic urticaria.

Pseudoephedrine is an alpha and beta adrenergic agonist used to treat nasal and sinus congestion, as well as allergic rhinitis.

Pseudoephedrine is a sympathomimetic amine used for its decongestant activity.

Lecope Dx 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), Chronic Idiopathic Urticaria, Common Cold, Nasal Congestion, Perennial Allergic Rhinitis (PAR), Seasonal Allergic RhinitisAllergic 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 therapy

How Lecope Dx 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.

Levocetirizine selectively inhibits histamine H₁ receptors. This action prevents histamine from activating this receptor and causing effects like smooth muscle contraction, increased permeability of vascular endothelium, histidine uptake in basophils, stimulation of cough receptors, and stimulation of flare responses in the nervous system.

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.

Dosage

Lecope Dx dosage

Adults and Children over 12 years: 15 to 30 mg three to four times per day. However, 60 mg doses up to four times per day have been used without increased side effects.

Children between 6 and 12 years: 5-15 mg up to four times per day.

Children between 2 and 6 years: 2.5-5 mg up to four times per day.

Adults and children 12 years of age and older: 5 mg once daily in the evening

Children 6 to 11 years of age: 2.5 mg once daily in the evening

Children 6 months to 5 years of age: 1.25 mg (1/2 teaspoon oral solution) once daily in the evening

Renal Impairment: Adjust the dose in patients 12 years of age and older with decreased renal function

Side Effects

Adverse effects with Dextromethorphan are rare, but nausea and dizziness sometimes occur. The drug produces no analgesia or addiction and little or no CNS depression. Excitation, confusion and respiratory depression may occur after overdosage.

The most common adverse reactions (rate ≥2% and > placebo) were somnolence, nasopharyngitis, fatigue, dry mouth, and pharyngitis in subjects 12 years of age and older, and pyrexia, somnolence, cough, and epistaxis in children 6 to 12 years of age. In subjects 1 to 5 years of age, the most common adverse reactions (rate ≥2% and > placebo) were pyrexia, diarrhea, vomiting, and otitis media. In subjects 6 to 11 months of age, the most common adverse reactions (rate ≥3% and > placebo) were diarrhea and constipation.

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.

Patients experiencing an overdose may present with drowsiness. Children may become agitated and restless before drowsiness. Patients should be treated with supportive measures. Dialysis will not assist in removing the drug from the body.

The maximal nonlethal dose in mice and rats is 240mg/kg.

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.

Precaution

Do not use Dextromethorphan to control a cough that is associated with smoking, asthma, or emphysema, or a cough that is productive (produces sputum or phlegm).

Epileptic patients and patients at risk of convulsions. Renal impairment. Pregnancy and lactation.

Interaction

The following medicines should be taken carefully while concomitantly use with Dextromethorphan: Amiodarone, Fluoexetine, Quinidine, CNS depressants and Monoamine oxidase (MAO) inhibitors.

Volume of Distribution

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

The volume of distribution of levocetirizine is 0.33±0.02L/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.

Following a 5mg oral dose of levocetirizine, a C_max of 0.27±0.04µg/mL with a T_max of 0.75±0.50h. The AUC of levocetirizine is 2.31±0.50µg*h/mL. Taking levocetirizine with food does not affect the AUC but delays T_max by 1.25 hours and lowers C_max by 36%.

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.

Half Life

Dextromethorphan has a half life of 3-30 hours.

The average half life of levocetirizine is 7.05±1.54 hours.

The mean elimination half life of pseudoephedrine is 6.0h.

Clearance

The average clearance of levocetirizine is 0.57±0.18mL/min/kg.

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

Elimination Route

168 hours post dose an average of 85.4% of a radiolabeled dose was recovered with an average of 80.8% in the urine and 9.5% in the feces. In the urine, 77% of the dose was recovered as unchanged drug, 0.5% as the M8 and M9 metabolites, 0.4% as the M10a metabolite, 0.4% as the M10b metabolite, 0.3% as the M3 metabolite, 0.3% as the M4 and M5 metabolite, 0.2% as the M2 metabolite, and 0.1% as the M1 metabolite. In the feces, 9.0% of the dose was recovered as unchanged drug, 1.0% as the M4 and M5 metabolite, and 0.1% as the M1 metabolite.

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

Pregnancy & Breastfeeding use

Pregnancy: Adequate and well-controlled studies in human have not been done. However, Dextromethorphan has not been reported to cause birth defects.

Lactation: It is not known whether dextromethorphan passes into breast milk. However, Dextromethorphan has not been reported to cause problems in nursing babies.

Pregnancy: The safety of Levocetirizine in pregnancy has not been established. Therefore, it should be used with caution during pregnancy and only if the potential benefits to the mother outweigh any risks to the foetus.

Lactation: Levocetirizine passes into breast milk. So, it should be used with caution in nursing mothers and only if the expected benefit to the mother is greater than the risk to the nursing infant.

Contraindication

Hypersensitivity to Dextromethorphan or any other component.

It is contraindicated in patients who are hypersensitive to this medication or to any of its ingredients.

Special Warning

Paediatric use: Not recommended for use in children less than 6 years of age.

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.

Symptoms: Drowsiness, agitation, restlessness, confusion, diarrhoea, dizziness, fatigue, headache, malaise, mydriasis, pruritus, sedation, somnolence, stupor, tachycardia, tremor and urinary retention.

Management: Symptomatic and supportive treatment. Gastric lavage must be considered shortly following ingestion.

Storage Condition

Store at 15-30° C

Store between 20-25°C.

Innovators Monograph

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