Covil A

Covil A Uses, Dosage, Side Effects, Food Interaction and all others data.

Ambroxol is a metabolite of Bromhexine. It possesses mucokinetic (improvement in mucus transport) and secretolytic (liquefies secretions) properties. Ambroxol stimulates the serous cells of the glands of the mucous membrane of bronchi, increasing the content of mucus secretion. The mucolytic effect is associated with depolymerization and splitting of mucoproteins and mucopolysaccharide fibres, which leads to reduction in the viscosity of mucus. Expectoration of mucus is facilitated and breathing is eased considerably. Ambroxol stimulates production of phospholipids of surfactant by alveolar cells. Ambroxol has anti-inflammatory properties. In patients with COPD, it improves airway patency. Beside these, Ambroxol also exhibits anti-oxidant activity. Long-term use is possible because of the good tolerability of the preparation.

Chlorpheniramine is an alkylamine antihistamine. It is one of the most potent H1 blocking agents and is generally effective in relatively low doses. Chlorpheniramine is not so prone to produce drowsiness, readily absorbed from the gastro-intestinal tract, metabolised in the liver and excreted usually mainly as metabolised in the urine.

In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Chlorpheniramine, is a histamine H1 antagonist (or more correctly, an inverse histamine agonist) of the alkylamine class. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.

Terbutaline is a relatively selective β2-adrenergic bronchodilator that has little or no effect on alpha-adrenergic receptors. The drug has exerts a preferential effect on β2-adrenergic receptors but stimulates beta-adrenergic receptors less selectively than relatively selective β2-agonists. Terbutaline appears to have a greater stimulating effect on beta-receptors of the bronchial, vascular, and uterine smooth muscles (β2 receptors) than on the beta-receptors of the heart (β1 receptors). This drug relaxes smooth muscle and inhibits uterine contractions, but may also cause some cardiostimulatory effects and CNS stimulation.

The pharmacologic effects of terbutaline are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic- 3',5'- adenosine monophosphate (c-AMP). Increased c-AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.

Terbutaline is a beta-2 adrenergic receptor agonist indicated to treat reversibly bronchospasm in asthmatic patients with bronchitis and emphysema. It has a short duration as the inhaled form is taken up to three times daily, and the therapeutic window is wide.

Covil A
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Covil A
Generic	Ambroxol + Chlorpheniramine + Guaiphenesin + Terbutaline
Type	Syrup, Tablet
Therapeutic Class
Manufacturer	Blubell Pharma
Available Country	India
Last Updated:	September 19, 2023 at 7:00 am

Uses

• Acute and chronic diseases of respiratory tracts associated with viscid mucus including acute and chronic bronchitis
• Productive cough
• Inflammatory diseases of Rhinopharyngeal tract (e.g. Laryngitis, Pharyngitis, Sinusitis and Rhinitis) associated with viscid mucus
• Asthmatic bronchitis, Bronchial asthma with difficult departure of mucus
• Bronchiectasis
• Chronic pneumonia.

Indicated mainly in allergic conditions including urticaria, sensitivity reactions, angioneurotic oedema, seasonal hay fever, vasomotor rhinitis, cough, common cold, motion sickness.

Used to open up the airways in people with asthma, bronchitis and other breathing problems.Used to relieve trouble breathing upon exertion.For the prevention and reversal of bronchospasm in patients 12 years of age and older with reversible, obstructive airway disease.Symptomatic management of reversible bronchospasm associated with bronchitis and emphysema.

Covil A is also used to associated treatment for these conditions: Airway secretion clearance therapyAllergic Contact Dermatitis, Allergic Reaction, Allergic Rhinitis (AR), Allergic cough, Allergies, Allergies caused by Serum, Allergy to House Dust, Allergy to vaccine, Angioneurotic Edema, Asthma, Bronchial Asthma, Bronchitis, Common Cold, Conjunctival congestion, Conjunctivitis, Conjunctivitis allergic, Cough, Cough caused by Common Cold, Coughing caused by Flu caused by Influenza, Drug Allergy, Eye allergy, Fever, Flu caused by Influenza, Food Allergy, Headache, Headache caused by Allergies, Itching of the nose, Itching of the throat, Migraine, Nasal Congestion, Nasal Congestion caused by Common Cold, Pollen Allergy, Productive cough, Pruritus, Rash, Rhinorrhoea, Seasonal Allergic Conjunctivitis, Sinus Congestion, Sinusitis, Sneezing, Transfusion Reactions, Upper Respiratory Tract Infection, Upper respiratory tract hypersensitivity reaction, site unspecified, Urticaria, Vasomotor Rhinitis, Acute Rhinitis, Allergic purpura, Conjunctival hyperemia, Dry cough, Excess mucus or phlegm, Itchy throat, Mild bacterial upper respiratory tract infections, Ocular hyperemia, Throat inflammation, Upper airway congestion, Upper respiratory symptoms, Watery eyes, Watery itchy eyes, Airway secretion clearance therapyAsthma, Bronchospasm, Chronic Cough (CC), Chronic Obstructive Pulmonary Disease (COPD), Cough, Premature Labour, Productive cough, Airway secretion clearance therapy

How Covil A works

Ambroxol is a mucolytic agent. Excessive Nitric oxide (NO) is associated with inflammatory and some other disturbances of airways function. NO enhances the activation of soluble guanylate cyclase and cGMP accumulation. Ambroxol has been shown to inhibit the NO-dependent activation of soluble guanylate cyclase. It is also possible that the inhibition of NO-dependent activation of soluble guanylate cyclase can suppress the excessive mucus secretion, therefore it lowers the phlegm viscosity and improves the mucociliary transport of bronchial secretions.

Chlorpheniramine 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.

Terbutaline is a selective beta-2 adrenergic receptor agonist. Agonism of these receptors in bronchioles activates adenylyl cyclase, increasing intracellular cyclic adenosine monophosphate (cAMP). Increased cAMP decreases intracellular calcium, activating protein kinase A, inactivating myosin light-chain kinase, activating myosin light-chain phosphatase, and finally relaxing smooth muscle in the bronchiole.

Dosage

Covil A dosage

Average daily dose (preferably after meal):Pediatric Drops:

0-6 months: 0.5 ml 2 times a day
6-12 months: 1 ml 2 times a day
1-2 years: 1.25 ml 2 times a day

Syrup:

2-5 years: 2.5 ml (1/2 teaspoonful) 2-3 times a day
5-10 years: 5 ml (1 teaspoonful) 2-3 times a day
10 years and adults: 10 ml (2 teaspoonful) 3 times a day.

Sustained release capsule:

Adult and children over 12 years old: 1 capsule once daily

Specific application features: Ambroxol may be prescribed to patients suffering from diabetes mellitus.

Adults: 4 mg 3-4 times daily.

Children:

Up to 1( one) year: 1 mg twice daily
1-5 years: 1 mg 3-4 times daily
6-12 years: 2 mg 3-4 times daily or as directed by the physician

The recommended adult dose for treating asthma, emphysema or bronchitis is 2.5-5 mg 3 times daily approximately 6 hours apart while awake. The maximum dosage is 15 mg/day. Shake the inhaler several times and uncap the mouthpiece. Breathe out fully. For best results, hold the inhaler 1 to 2 inches in front of your open mouth or attach a spacer to the inhaler and place the spacer in your mouth, above your tongue and past your teeth. Take a deep, slow breath as you push down on the canister. Hold your breath for 10 seconds, then exhale slowly. Use nebulizer machine for better response.

Side Effects

Gastrointestinal side-effects like epigastric pain, gastric fullness may occur occasionally. Rarely allergic responses such as eruption, urticaria or angioneurotic edema may occur.

Drowsiness, dizziness, headache, psychomotor impairment, urinary retention, dry mouth, blurred vision and gastro intestinal disturbances, paradoxical stimulation may rarely occur, especially in high dosage or in children.

Dry mouth, irritated throat, nausea, dizziness, headache, heartburn, loss of appetite, altered taste sensation, restlessness, anxiety, nervousness, trembling, and sweating may occur but should subside as your body adjusts to the medication.

Toxicity

Oral LD50 (rat): 306 mg/kg; Oral LD50 (mice): 130 mg/kg; Oral LD50 (guinea pig): 198 mg/kg [Registry of Toxic Effects of Chemical Substances. Ed. D. Sweet, US Dept. of Health & Human Services: Cincinatti, 2010.] Also a mild reproductive toxin to women of childbearing age.

Patients experiencing an overdose may present with abdominal pain, agitation, palpitations, seizures, angina, hypertension, hypotension, tachycardia, arrhythmias, nervousness, headache, tremor, dry mouth, nausea, dizziness, fatigue, malaise, insomnia. Discontinue treatment with terbutaline and initiate symptomatic and supportive therapy.

Precaution

Ambroxol should be given cautiously to patients with gastric and duodenal ulceration or convulsive disorders. Patients with hepatic and renal insufficiency should take it with caution.

Chlorpheniramine may produce mild sedation and it is advised that patients under continuous treatment should avoid operating machinery. Not recommended during pregnancy & lactation.

Before you use this drug, tell your doctor if you have: any allergies, heart disease, high blood pressure, an overactive thyroid gland, seizures, diabetes. Tell your doctor if you ever had a bad reaction to albuterol, bitolterol, ephedrine, epinephrine, isoetharine, isoproterenol, metaproterenol, pseudoephedrine, or pirbuterol or other similar agents. Tell your doctor if you are pregnant before using this medication. Terbutaline is excreted into breast milk. Consult with your doctor before breast-feeding. Terbutaline is not recommended for children under the age of 6. Caution is advised in the elderly.

Interaction

Ambroxol has no interaction with cardioactive glycosides, corticosteroids, bronchodilators, diuretics and antibiotics (normally used in the treatment of bronchopulmonary affections). But Ambroxol should not be taken simultaneously with antitussives (e.g. Codeine) because mucus, which has been liquefied by Ambroxol, might not be expectorated.

Alcohol, CNS depressants, anticholinergic drugs, MAOIs.

Tell your doctor of all nonprescription and prescription medications you take, including: beta-blockers (e.g., propranolol, timolol), all asthma drugs, antidepressants, MAO inhibitors (e.g., furazolidone, linezolid, phenelzine, selegiline, tranylcypromine), diuretics (e.g., hydrochlorothiazide). Many nonprescription medications contain pseudoephedrine or ephedrine, so check the labels carefully. Do not take any of these medications without consulting your doctor. Do not start or stop any medicine without doctor or pharmacist approval.

Volume of Distribution

Terbutaline has a mean volume of distribution of 1.6 L/kg.

Elimination Route

Rapid and almost complete.

Well absorbed in the gastrointestinal tract.

A 0.5 mg subcutaneous dose of terbutaline reaches a mean C_max of 9.6 ± ng/mL, with a median T_max of 0.5 hours, and a mean AUC of 29.4 ± 14.2 h*ng/mL. A 5 mg oral terbutaline tablet reaches a mean C_max of 8.3 ± 3.9 ng/mL with a median T_max of 2 hours, and a mean AUC of 54.6 ± 26.8 h*ng/mL. A 5 mg oral terbutaline solution reaches a mean C_max of 8.6 ± 3.6 ng/mL, with a median T_max of 1.5 hours, and a mean AUC of 53.1 ± 23.5 h*ng/mL.

Oral terbutaline has an oral bioavailability of 14-15%.

Half Life

7-12 hours

21-27 hours

An oral dose of terbutaline has an elimination half life of 3.4 hours, while a subcutaneous dose has an elimination half life of 2.9 hours.

Clearance

The average clearance of terbutaline is 3.0 mL/min/kg.

Elimination Route

An oral dose of terbutaline is 40% eliminated in the urine after 72 hours. The major metabolite in the urine was the sulphate conjugated form of terbutaline. Parenteral doses of terbutaline are 90% eliminated in the urine, with approximately 2/3 as the unchanged parent drug. Less than 1% of a dose of terbutaline is eliminated in the feces.

Pregnancy & Breastfeeding use

Pregnancy: Teratogenic and fetal toxicity studies have shown no harmful effect of Ambroxol. However, it is advised not to use during pregnancy, especially in the 1st trimester.

Lactation: Safety during lactation has not been established.

Pregnancy Category B. Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Although no teratogenic effects have been observed in animals or in patients, Terbutaline should only be administered with caution during the first trimester of pregnancy. Terbutaline is secreted via breast milk, but effect on the infant is unlikely at therapeutic doses.

Contraindication

Contraindicated in known hypersensitivity to Ambroxol or Bromhexine.

There is no definite contraindication to therapy. It should be used with caution in epilepsy, prostatic hypertrophy, glaucoma and hepatic disease. The ability to drive or operate machinery may be impaired.

Do not use Terbutaline if

You are allergic to any ingredient in Terbutaline or to a sympathomimetic amine (eg, epinephrine, albuterol).
You need to treat prolonged (more than 48 to 72 hours) premature labor.