Koftrodex

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.

Koftrodex 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, Antihistamine

How Koftrodex 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.

Dosage

Koftrodex 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.

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.

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 T_max of approximately 3 hours, a mean steady-state C_max 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.

Half Life

7-12 hours

Desloratadine has a mean plasma elimination half-life of approximately 27 hours.

Elimination Route

Approximately 87% of a C-desloratadine dose was equally recovered in urine and feces as metabolic products.

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.

Innovators Monograph

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