Coftime
Coftime 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.
Desloratadine is a long-acting, tricyclic, non-sedating, selective peripheral histamine H1-receptor antagonist which inhibits the release of pro-inflammatory mediators from human mast cells and basophils.
Desloratadine is a long-acting second-generation H1-receptor antagonist which has a selective and peripheral H1-antagonist action. Histamine is a chemical that causes many of the signs that are part of allergic reactions, such as the swelling of tissues. Histamine is released from histamine-storing cells (mast cells) and attaches to other cells that have receptors for histamine. The attachment of the histamine to the receptors causes the cell to be "activated," releasing other chemicals which produce the effects that we associate with allergies. Desloratadine blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Desloratadine does not enter the brain from the blood and, therefore, does not cause drowsiness.
Guaifenesin possesses a storied history, having been originally formally approved by the US FDA in 1952 and continues to be one of very few - if not perhaps the only drug that is readily available and used as an expectorant . Since that time the agent has been a combination component of various prescription and non-prescription over-the-counter cough and cold products and is currently a widely available over-the-counter generic medication . Although it is principally believed that guaifenesin elicits an action to facilitate productive cough to manage chest congestion , it is not known whether the agent can reliably mitigate coughing.
Regardless, on March 1, 2007, the FDA received a petition asking the FDA to notify the public that some antitussives, expectorants, decongestants, antihistamines, and cough/cold combinations are not known to be safe and effective in children under the age of 6 years . After the negotiation between FDA and major manufacturers, a voluntary transition of labels for not using guaifenesin in children under the age of 4 years was endorsed by FDA in 2008 .
Furthermore, there has also been contemporary research to suggest that guaifenesin possesses and is capable of demonstrating anticonvulsant and muscle relaxant effects to some degree possibly by acting as an NMDA receptor antagonist .
| Trade Name | Coftime |
| Generic | Ambroxol + Desloratadine + Guaifenesin + Menthol |
| Type | Syrup |
| Therapeutic Class | |
| Manufacturer | Rhine Biogenics Pvt Ltd |
| 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.
Allergic Rhinitis: Desloratadine is used for the relief of the nasal and non-nasal symptoms of allergic rhinitis (Both seasonal and perennial) in patients 2 years of age and older.
Chronic Idiopathic Urticaria: Desloratadine is also used for the symptomatic relief of pruritus, reduction in the number of hives, and size of hives, in patients with chronic idiopathic urticaria 2 years of age and older.
Guaifenesin is an expectorant commonly found in OTC products for the symptomatic relief from congested chests and coughs associated with cold, bronchitis, and/or other breathing illnesses.
Guaifenesin is an expectorant that is indicated for providing temporary symptomatic relief from congested chests and coughs which may be due to a cold, bronchitis, and/or other breathing illnesses .
Coftime is also used to associated treatment for these conditions: Airway secretion clearance therapyAllergic Rhinitis (AR), Asthma, Chronic Idiopathic Urticaria, Common Cold, Nasal Congestion, Perennial Allergic Rhinitis (PAR), Seasonal Allergic Rhinitis, Nasal symptoms, Non-nasal symptoms, AntihistamineAllergic Reaction, Asthma, Asthma, Allergic, Bronchial Asthma, Bronchitis, Bronchospasm, Chronic Bronchitis, Chronic Obstructive Respiratory Diseases, Common Cold, Cough, Cough caused by Common Cold, Coughing caused by Allergies, Coughing caused by Flu caused by Influenza, Drug Allergy, Emphysema, Fever, Flu caused by Influenza, Food Allergy, Headache, House dust allergy, Irritative cough, Laryngitis, Nasal Congestion, Nasal Congestion caused by Common Cold, Phlegm, Pollen Allergy, Productive cough, Rash, Rhinorrhoea, Sneezing, Sore Throat, Tracheitis, Urticaria, Whooping Cough, Acute Rhinitis, Chest congestion, Chills occurring with fever, Dry cough, Excess mucus or phlegm, Mild to moderate pain, Minor aches and pains, Airway secretion clearance therapy, Expectorant
How Coftime 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.
Like other H1-blockers, Desloratadine competes with free histamine for binding at H1-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms (eg. nasal congestion, watery eyes) brought on by histamine.
Although the exact mechanism of action of guaifenesin may not yet be formally or totally elucidated, it is believed that expectorants like guaifenesin function by increasing mucus secretion . Moreover, it is also further proposed that such expectorants may also act as an irritant to gastric vagal receptors, and recruit efferent parasympathetic reflexes that can elicit glandular exocytosis that is comprised of a less viscous mucus mixture . Subsequently, these actions may provoke coughing that can ultimately flush difficult to access, congealed mucopurulent material from obstructed small airways to facilitate a temporary improvement for the individual .
Consequently, while it is generally proposed that guaifenesin functions as an expectorant by helping to loosen phlegm (mucus) and thin bronchial secretions to rid the bronchial passageways of bothersome mucus and make coughs more productive, there has also been research to suggest that guaifenesin possesses and is capable of demonstrating anticonvulsant and muscle relaxant effects to some degree possibly by acting as an NMDA receptor antagonist .
Dosage
Coftime 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.
Pediatric drops :
- Child 6 -11 months of age: 2 ml drops once daily
- Child 1 -2 years of age: 2.5 ml drops once daily
Syrup:
- Child 6-11 months of age: 2 ml once daily
- Child 1-5 years of age: 2.5 ml once daily
- Child 6-11 years of age: 5 ml once daily
- Adults & > 12 years of age: 10 ml once daily
Tablet:
- Adults and children 12 years of age and over: 5 mg daily
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.
Desloratadine is generally well tolerated. However, dry mouth, fatigue, somnolence and myalgia are commonly reported side-effects. Less common side-effects may include dizziness, headache and nausea. Rarely rash, pruritus and urticaria may occur.
Toxicity
Information regarding desloratadine overdose is limited, although somnolence has been reported. In case of overdose, symptomatic and supportive treatment, including removing the unabsorbed drug, is recommended; note, however, that desloratadine and its active metabolite 3-hydroxydesloratadine cannot be eliminated by hemodialysis.
In animal studies, lethality was observed at or above doses of 250 mg/kg in rats and of 353 mg/kg in mice (oral LD50), doses that represent 120 and 290 times the human exposure based on the recommended daily oral dose. In monkey, no deaths occurred at doses up to 250 mg/kg, representing an exposure roughly 810 times that of the recommended dose in humans.
The most prevalent signs and symptoms associated with an overdose of guaifenesin have been nausea and vomiting .
Although adequate and well-controlled studies in pregnant women have not been performed, the Collaborative Perinatal Project monitored 197 mother-child pairs exposed to guaifenesin during the first trimester . An increased occurrence of inguinal hernias was found in the neonates . However, congenital defects were not strongly associated with guaifenesin use during pregnancy in 2 large groups of mother-child pairs .
Moreover, guaifenesin is excreted in breast milk in small quantities . Subsequently, caution should be exercised by balancing the potential benefit of treatment against any possible risks .
Additionally, an LD50 value of 1510 mg/kg (rat, oral) has been reported for guaifenesin .
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.
Hepatic and renal impairment. Pregnancy and lactation.
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.
Concomitant administration of Erythromycin, Ketoconazole, Azithromycin, Fluoxetine, and Cimetidine with Desloratadine increased the plasma concentration of Desloratadine. But there were no clinically relevant changes in the safety profile of Desloratadine.
Volume of Distribution
The geometric mean apparent volume of distribution of guaifenesin determined in healthy adult subjects is 116L (CV=45.7%) .
Elimination Route
Rapid and almost complete.
Desloratadine administered orally for ten days to healthy volunteers as a 5 mg tablet once daily resulted in a mean Tmax of approximately 3 hours, a mean steady-state Cmax of 4 ng/ml, and a mean steady-state AUC of 56.9 ng*hr/ml. A similar profile was observed using 10 ml of an oral solution containing 5 mg of desloratadine. Food was found not to affect desloratadine absorption.
Studies have shown that guaifenesin is well absorbed from and along the gastrointestinal tract after oral administration .
Half Life
7-12 hours
Desloratadine has a mean plasma elimination half-life of approximately 27 hours.
The half-life in plasma observed for guaifenesin is approximately one hour .
Clearance
The mean clearance recorded for guaifenesin is about 94.8 L/hr (CV=51.4%) .
Elimination Route
Approximately 87% of a C-desloratadine dose was equally recovered in urine and feces as metabolic products.
After administration, guaifenesin is metabolized and then largely excreted in the urine .
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: There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, Desloratadine should be used in pregnancy only if clearly needed.
Lactation: Desloratadine passes into breast milk. Therefore, a decision should be made whether to discontinue nursing or to discontinue Desloratadine, taking into account the importance of the drug to the mother.
Contraindication
Contraindicated in known hypersensitivity to Ambroxol or Bromhexine.
Desloratadine is contraindicated in patient having hypersensitivity to this medication or to any of its ingredients or Loratadine.
Special Warning
Paediatric Use: The safety and effectiveness of Desloratadine in pediatric patients under 2 years of age have not been established.
Geriatric Use: In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
In adult patients with liver or renal impairment: A starting dose of one 5 mg tablet every other day is recommended based on pharmacokinetic data.
Acute Overdose
No clinically relevant adverse events have been reported in case of overdosage. However, in the event of overdosage, symptomatic and supportive treatment is recommended.
Storage Condition
Store in a cool and dry place, protected from light.
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