Labocof Cough Tablets

LABOCOF® COUGH TABLETS

Dextromethorphan Hydrobromide, Guaifenesin, Bromhexine HCl, Chlorpheniramine Maleate Tablets

For Medical/Pharmacy professional only.

 

DOSAGE FORM & STRENGTH

Tablets for oral administration.

Strength

Dextromethorphan Hydrobromide 10mg

Guaifenesin  100mg

Bromhexine HCl 8mg

Chlorpheniramine Maleate 1mg

 

HISTORY OF ACTIVE INGREDIENTS

Dextromethorphan is an oplioid like drug that binds to and acts as antagonist to the NMDA glutamate receptor, it is an agonist to the opioid sigma 1 and sigma 2 receptors, it is also an alpha3/beta4 nicotinic receptor antagonist and targets the serotonin reuptake pump.

Guaifenesin is thought to act as an expectorant by increasing the volume and reducing the viscosity of secretions in the trachea and bronchi. It also stimulates the flow of respiratory tract secretions, allowing ciliary movement to carry the loosened secretions upward toward the pharynx. Thus, it may increase the efficiency of the cough reflex and facilitate removal of the secretions.

Bromhexine is a mucolytic agent used in the treatment of respiratory disorders associated with viscid or excessive mucus.

Chlorpheniramine in the form of chlorpheniramine maleate is a first-generation alkylamine antihistamine used in the prevention of the symptoms of allergic conditions such as rhinitis and urticaria. Its sedative effects are relatively weak compared to other first-generation antihistamines.

 

NET CONTENT

COMPOSITION

Each uncoated tablet contains:

Dextromethorphan Hydrobromide BP 10mg

Guaifenesin  BP 100mg

Bromhexine HCl BP 8mg

Chlorpheniramine Maleate BP 1mg

Excipients q.s.

Colour: Erythrosine

 

CLINICAL PHARMACOLOGY

ATC COOE:

Chlorphenamine Meleate: R06AB04

Guaifenesin: RO5CAO3

Dextromethorphan: RO5DA09

Bromhexine: R05CB02

 

PHARMACODYNAMICS

Bromhexine HCl is a mucolytic used in the treatment of respiratory disorders associated with productive cough.

Chlorphenemine maleate is used for symptomatic relief of allergic conditions, in the management of nasal congestion and in symptomatic treatment of coughs.

Dextromethorphan Hydrobromide is a cough suppressant which has a central action on the cough centre in the medulla.

Guaifenesin is used to reduce chest congestion caused by the common cold, infections, or allergies.

 

PHARMACOKINETICS

Guaifenesin is rapidly absorbed after oral administration. It is rapidly metabolised by oxidation to β-(2 methyoxy-phenoxy) lactic acid, which is excreted in the urine.

Dextromethorphan is rapidly absorbed from the gastrointestinal tract, where it enters the bloodstream and crosses the blood-brain barrier. The first-pass through the hepatic portal vein results in some of the drug being metabolized into an active metabolite of dextromethorphan, dextrorphan, the 3-hydroxy derivative of dextromethorphan.

Bromhexine hydrochloride is rapidly absorbed from the gastrointestinal tract and undergoes extensive first-pass metabolism in the liver. Its oral bioavailability is stated to be only about 20%. It is widely distributed to body tissues and is highly bound to plasma proteins. About 85 to 90% of a dose is excreted in the urine mainly as metabolites. It has a terminal elimination half-life of up to about 12 hours. Bromhexine crosses the blood brain barrier and small amounts cross the placenta.

Chlorphenamine maleate is absorbed relatively slowly from the gastrointestinal tract, with peak plasma concentrations occurring about 2.5 to 6 hours after oral administration.

 

INDICATION AND USAGE

Labocof is a cough formulation containing 4 main components which act synergistically to relieve cough. These drugs competitively antagonize actions of histamine at the H1 receptors. They effectively block histamine induced broncho constriction, contraction of intestinal and other smooth muscle specially wheal, flare and itch.

Labocof is a cough formulation which acts directly at the cough centre for relieving cough, cold and allergic symptoms.

 

CONTRAINDICATION

Hypersensitivity to any active component or any of the other ingredients.

Hypertension, hyperthyroidism, diabetes, serious heart disease or those patients receiving or within two weeks of stopping therapy with monoamine oxidase inhibitors.

 

INTERACTIONS

Central nervous system (CNS) depressant (alcohol, sedatives, opioid analgesics. hypnotics), may cause an increase in sedation effects. Chlorphenamine when taken concomitantly with phenytoin may cause a decrease in phenytoin elimination.

Phenylephrine Hydrochloride may adversely interact with other sympathomimetics, vasodilators and beta blockers.

Guaifenesin interferes with urine tests for 5-hydroxytndoleacetic acid (5-HIAA) and vanilylmandelic acid (VMA).

 

WARNINGS

Use drug with caution in patients with predisposition to urinary retention, history of bronchial asthma, increased IOP, hyperthyroidism, CV disease, or hypertension. Avoid in patients with sleep apnea.

 

PREGNANCY AND LACTATION

Chlorphenamine maleate is excreted in breast milk. Therefore it is not recommended for breastfeeding mothers unless the potential benefits to the patient are weighed against the possible risk to the infant.

Keep all medicines out of the reach of children.

 


PRECAUTIONS

Chlorphenamine maleate may cause drowsiness and may increase the effects of alcohol.
Use with caution in patients with renal or hepatic impairment and in patients with epilepsy.

 

ADVERSE REACTION

CNS depressive effects include sedation and impaired performance (impaired driving performance, poor work performance, incoordination, reduced motor skills, and impaired information processing). Performance may be impaired in the absence of sedation and may persist the morning after a night-time dose.

CNS stimulatory affects may include anxiety, hallucinations, appetite stimulation, muscle dyskinesias and activation of epileptogenic foci.

High doses may cause nervousness, tremor, insomnia, agitation, and irritability.

 

DRUG ABUSE AND DEPENDENCE

Not Appliccable.

 

SYMPTOMS OF OVERDOSE AND ANTIDOTE

Overdosage may cause hallucinations, convulsions, and death. Antihistamines may diminish mental alertness. In young children, they may produce paradoxical excitation. Contraindicated in newbom or premature infants.

CNS depression (including sedation, apnea, CV collapse), CNS stimulation (including insomnia, hallucination, tremors, convulsions), tinnitus, blurred vision, dizziness, ataxia, hypotension. Stimulation and atropine-like signs and symptoms (including dry mouth, fixed dilated pupils, flushing, hyperthermia, GI symptoms) are more likely in children.
Treatment of overdose should be symptomatic & supportive. Gastric lavage may be of use.

 

DOSAGE AND ADMINISTRATION

Adults and children above 12 years old: 1-2 tablets 3-4 times daily.

Children between 6-12 years old: ½ -1 tablet 3-4 times daily

Children between 2-5 years old: ¼ – ½ tablet 3-4 times daily

or as directed by the physician.

 

THE PREPARATION FOR USE

Not Applicable

 

PRESENTATION

4 tablets packed in a unit carton along with patient information leaflet

 

STORAGE CONDITION

Store in a dry place at temperature not exceeding 30oC. Protect from light.

 

NAFDAC Reg. No.: 04-5059

 

MANUFACTURED IN INDIA BY

LABORATE PHARMACEUTICAL (INDIA)

E -11, IND. AREA, PANPAT – 132 103

 

Sole Agent

EMBASSY PHARMACEUTICAL & CHEMICALS LTD.

Lagos, Nigeria.