Singukast : Montelukast for the prophylaxis and chronic treatment of asthma-أدوية

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Singukast : Montelukast for the prophylaxis and chronic treatment of asthma

المحتويات Contents

مصدر الموضوع

Singukast is indicated in adult and pediatric patients for the prophylaxis and chronic treatment of asthma, including the prevention of day-and night-time symptoms, the treatment of aspirin sensitive asthmatic patients, and the prevention of exercise-induced bronchoconstriction. It also used to help control the symptoms of seasonal allergic rhinitis in adults and children two years old and older.

Generic Name

Montelukast

Pharmacology

Singukast (montelukast sodium) is a selective and orally active leukotriene receptor antagonist that specifically inhibits the cysteinyl leukotriene CysL T1 receptor.

Pharmacokinetics

Absorption:

 Montelukast is rapidly absorbed following oral administration. After administration of the 10 mg tablet to fasted adults, the mean peak montelukast plasma concentration (Cmax) is achieved in 3 to 4 hours).

The mean oral bioavailability is 64%. The oral bioavailability and Cmax are not influenced by a standard meal in the morning.

For the 5 mg chewable tablet, the mean Cmax is achieved in 2 to 2.5 hours after administration to adults in the fasted state. The mean oral bioavailability is 73% in the fasted state versus 63% when administered with a standard meal in the morning.

The safety and efficacy of Singukast in patients with asthma were demonstrated in clinical trials in which the 10 mg tablet and 5 mg chewable tablet formulations were administered in the evening without regard to the time of food ingestion.

The safety and efficacy of Singukast in patients with seasonal allergic rhinitis were demonstrated in clinical trials in which the 10 mg tablet was administered in the morning or evening without regard to the time of food ingestion.

The comparative pharmacokinetics of montelukast when administered as two 5-mg chewable tablets versus one 10 mg tablet have not been evaluated.

Distribution:

Montelukast is more than 99% bound to plasma proteins. The steady state volume of distribution of montelukast averages 8 to 11 liters,

Metabolism:

Montelukast is extensively metabolized. In studies with therapeutic doses, plasma concentrations of metabolites of montelukast are undetectable at steady state in adults and pediatric patients.

Elimination:

The plasma clearance of montelukast averages 45 ml/min in healthy adults. Following an oral dose of radio labeled montelukast, 86% of the radioactivity was recovered in 5-day fecal collections and<O.2% was recovered in urine. Coupled with estimates of montelukast oral bioavailability, this indicates that montelukast and its metabolites are excreted almost exclusively via the bile.

Indications

Singukast is indicated in adult and pediatric patients for the prophylaxis and chronic treatment of asthma, including the prevention of day-and night-time symptoms, the treatment of aspirin sensitive asthmatic patients, and the prevention of exercise-induced bronchoconstriction. It also used to help control the symptoms of seasonal allergic rhinitis in adults and children two years old and older.

Dosage and Administration

Adults 15 years of age and older : 10 mg (one Singukast1 0 tablet) daily to be taken at bedtime.

Pediatric patients 6 to 14 years of age: 5 mg (one Singukast 5 chewable tablet or half Singukast 10 tablet) daily to be taken at bedtime. No dosage adjustment within this age group is necessary.

Pediatric patients 2 to 5 years of age: 5 mg (one Singukast 5 chewable tablet) daily to be

taken at bedtime.

Contraindications

Hypersensitivity to any component of this product.

Side effects

Montelukast is well tolerated. Side effects are mild, and generally did not require discontinuation of therapy.

The safety in pediatric patients is generally similar to that in the adults. The following adverse reactions have been reported:

Blood and lymphatic System disorders: Increased bleeding tendency.

Immune System disorders: Hypersensetivity reaction including anaphylaxis, very rarely

hepatic eosinophilic infilteration.

Psychiatric disorders: Agitation including aggressive behavior, anxiousness, dream abnormalities, hallucination, depression, irritability, restlessness, suicidal thinking & behavior (including suicide), tremor and insomnia.

Nervous System disorders: Drowsiness, paraesthesia / hypoethesia, very rarely seizures.

Cardiac disorders: Palpitations

Gastrointestinal disorders: Diarrhea, dyspepsia, nausea, very rarely pancreatitis, vomiting.

Hepatobiliary disorders: Rare cases of cholestatic hepatitis, hepatocellular liver-injury, and

mixed-pattern liver injury have been reported in patients treated with montelukast. Most of these occurred in combination with other confounding factors, such as use of other medications, or when montelukast was administered to patients who had underlying potential for liver disease such as alcohol use or other forms of hepatitis.

Skin & Subcutaneous tissue disorders: Angioedema, bruising, erythema nodosum, pruritus, urticaria.

Musculoskeletal and connective tissue disorders: Arthralgia, myalgia including muscle cramps.

General disorders & administration site conditions: Edema.

In rare cases, patients with asthma on therapy with montelukast may present with systemic

eosinophilia.

Drug interactions

Montelukast may be administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma.

Pregnancy & lactation

Montelukast should be used during pregnancy only if clearly needed. Caution should be exercised when montelukast is given to a nursing mother.

Precautions & Warnings

Oral montelukast tablets should not be used to treat acute asthma attacks. Patients should be advised to have appropriate rescue medication available.

While the dose of concomitant inhaled corticosteroid may be reduced gradually under medical supervision, montelukast should not be abruptly substituted for inhaled or oral corticosteroids. The reduction in systemic corticosteroid dose in patients receiving anti-asthma agents including leukotriene receptor antagonists has been followed in rare cases by the occurance of one or more of the following: eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and / or neuropathy sometimes diagnosed as Churg-Strauss syndrome, a systemic eosinophilic vasculitis.

Although a causal relationship with leucotriene receptor antagonism has not been established, caution and appropriate clinical monitoring are recommended when systemic corticosteroids reduction is considered in patients receiving montelukast.

Montelukast should not be used as monotherapy for the treatment and management of exercise-induced bronchospasm.

Patient with known aspirin sensitivity should continue avoidance of aspirin or non-steroidal anti-inflammatory agents while taking montelukast.

Use in Elderly:In clinical studies, there were no age-related differences in the efficacy or safety profiles of montelukast.

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