Pranlukast

Pranlukast belongs to the pharmacological class Cysteinyl Leukotriene-1 Receptor Antagonist Pranlukast selectively binds to the LTD4 in the cysteinyl leukotriene receptor and antagonizes them , as it has greater affinity to this receptor.

Pranlukast has been approved for relieving symptoms and also for the treatment and maintenance of episodes of chronic bronchial asthma, and allergic rhinitis.

Pranlukast is having 12.5% of oral absorption. The Pranlukast is found to be metabolized by the cytochrome P450enzymes and metabolism is mainly due to glucuronic conjugation. The major route of elimination is fecal route

The common side effects associated with Pranlukast are headache, fever, diarrhea, and bilateral leg edema

Pranlukast is available in the form of tablets and dry syrup and is majorly used in japan.

Pranlukast belongs to the pharmacological class Cysteinyl Leukotriene-1 Receptor Antagonist Pranlukast selectively binds to the LTD4 in the cysteinyl leukotriene receptor and antagonizes them , as it has greater affinity to this receptor.

Hence Pranlukast inhibits the physiologic action of the LD₄ in CysLT₁ receptor without rendering any agonistic activity. This, in turn, reduces inflammations and relives from the symptoms associated with conditions such as allergic rhinitis and chronic bronchial asthma.

Pranlukast is available in tablets and should be swallowed whole with water.

Pranlukast can be used in the treatment of:

• Allergic rhinitis
• Chronic Bronchial Asthma

Pranlukast can help to relieve symptoms and also for the treatment and maintenance of episodes of chronic bronchial asthma, and allergic rhinitis.

Pranlukast is approved for use in the following clinical indications:

• Allergic rhinitis
• Chronic Bronchial Asthma

Pranlukast can be administered orally before/ after meals. The dosage and duration of treatment should be as per the clinical judgment of the treating physician.

Tablet: 112.5 mg, 225 mg

Dry oral syrup , Tablet

• Dosage Adjustments in Pediatric Patients:

As there is no or limited data available for use in pediatric populations, the dosage adjustments cannot be established.

Smoking cessation and maintaining health is a must.

Caffeine should be avoided or limited to use as it might lead to the risk of nausea, palpitations, nervousness, rapid heartbeat, etc.

Alcohol should be avoided in the patient’s especially with an underlying liver disorder or liver dysfunction

Diet containing food with a high glycemic index, saturated and trans fat food, red and processed meat, added sugar, salt, preservatives, refined and high energy-dense foods, low fiber, low antioxidants, and vitamins needs to be restricted.

The dietary restrictions is needed to be individualized as per the patient's requirements.

Avoid alcohol usage while on Pranlukast medication as alcohol can worsen the effects of any underlying disease condition, including conditions such as dizziness, blurred vision etc.

The safety and efficacy data during pregnancy is unavailable/limited.

No sufficient scientific evidence traceable regarding the use and safety of Pranlukast in concurrent use with any particular food. Pranlukast can be taken without the regard to the food or meals.

The common side effects of Pranlukast include the following:

• High temperatures
• Headaches
• Diarrhea
• Dizziness
• Bilateral leg edema

Physician should be knowledgeable and vigilant about the treatment pertaining to the identification and treatment of overdosage of Pranlukast.

Pharmacodynamics

Pranlukast is said to be a selective, competitive antagonist of the cysteinyl leukotrienes, Pharmacodynamic Profile leukotriene (LT) C4, LTD4 and LTE4, antagonising by binding at the cysteinyl leukotriene type 1 (CysLT1) receptor. Like the other commercially-available CysLT1 receptor antagonists Pranlukast and zafirlukast. Pranlukast inhibits the antigen-induced contraction of human bronchial smooth muscle in-vitro. In patients suffering from asthma, oral pranlukast at clinically relevant doses generally inhibit the presence of eosinophils in sputum and eosinophil activity in the late asthma response, reduce exhaled nitric oxide levels, improve allergen-induced decrease in forced expiratory volume in 1 second and reduce the magnitude of airway hyperresponsiveness. Pranlukast attenuates bronchoconstriction induced by exercise at doses of 450 mg/day for 14 days, LTD4 at doses of pranlukast 10–60mg as a single intravenous dose , aspirin and bronchial hyperresponsiveness induced by methacholine and cold air , but do not ameliorate the effects of histamine, alcohol or propranolol.

Pharmacokinetics

• Absorption

At least 12.5% of a dose of pranlukast is found to be absorbed after oral administration. The Pharmacokinetic Profile maximum plasma concentrations was achieved within 2–6 hours after taking Pranlukast after meals. Steady-state plasma concentrations of pranlukastwas found to be achieved within 7 days of two times a day oral administration. Bioavailability is found to be increased when the drug Pranlukast is administered before or after a meal. In addition, the bioavailability of pranlukast is found to be greater after evening than after morning administration.

• Metabolism

Although Pranlukast is metabolised by cytochrome CYP450 enzymes in vitro, in a clinical setting, pranlukast appears to be having low potential for drug-drug interactions via this system. Urinary 6β-hydroxycortisol excretion which is a surrogate marker of CYP3A4 activity, was found to be unchanged with oral pranlukast 112.5–675mg two times a day in healthy volunteers. Before treatment with clinically relevant doses of oral pranlukast which is 225mg twice daily, had no effect on the pharmacokinetics of intravenous aminophylline administered 4 hours after the final dose of pranlukast in healthy young adults.

• Elimination

Pranlukast is found to be approximately around 99% bound to plasma protein. The mean plasma elimination half-life of oral pranlukast ranges from 3–9 hours after repeated doses during pharmacokinetic studies. The drug Pranlukast is found to be cleared through metabolic transformation which is primarily glucuronic acid conjugation. The majority of an oral dose is found to be excreted via the faecal route, chiefly in the unchanged form of the drug, within 72 hours of administration.

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