Salius Pharma introduced a new once daily Formulation CROHIST-MK for Allergic rhinitis and Asthma
04/25/2013

LEVOCETIRIZINE AND MONTELUKAST COMBINATION THERAPY IMPROVES THE QUALITY OF LIFE OF THE PATIENTS IN ALLERGIC RHINITIS AND ASTHMA MONOTHERAPIES

Online PR News – 25-April-2013 – Mumbai/Maharashtra – Well Known for its global quality standards in healthcare segment and become a formidable force in Respiratory segment,Salius pharma come out with a new novel formulation for treatment of Allergic rhinitis and Asthma.

Allergic rhinitis is a symptomatic disorder and an IgE-mediated inflammatory response of the nasal membranes induced by allergen exposure. It is an allergic condition like asthma, where the body tends to over react to certain types of outside substances. In one way it overreacts by producing antibodies that signal your immune system to release histamine and other chemicals. The symptoms include rhinorrhoea, nasal obstruction, nasal itching and sneezing of the nose, coughing, tearing of the eyes, sore throat, wheezing and headache. It affects social life, sleep, school and as a whole the quality of life of patients gets impaired.

Asthma is linked with allergies, heredity and environment. In a normal person various airborne allergens (triggers) induce the production of antibodies and other chemicals in controlled quantity, which destroy the allergen but don’t harm the body. But in allergic individual who have asthma there is over production of antibodies and other chemicals which causes inflammation of the airways, cough, wheezing, dyspnoea, airflow obstruction, tendency towards allergic disease like eczema, allergic rhinitis, allergic conjunctivitis.

All of us like to lead a comfortable life. However, a life with asthma keeps us bothering about how to manage the burden of asthma attack. The reasons of asthma may include the type of air you breathe, dust at home, molds underneath the sheets, stress and too much exertion of physical activities.

Although several drugs are marketed under distinct brand names with various compositions,with its dedicated team of highly specialised technocrats and Pharmacists Salius Pharma has able to introduce this innovative once daily medication CROHIST-MK for both adults and kids for the treatment of Allergic Rhinitis (both Seasonal and Perennial) and in the chronic treatment of Asthma.

CROHIST-MK TABLET / CROHIST-MK KID SYRUP

Montelukast & Levocetirizine Hydrochloride

COMPOSITION:-

CROHIST-MK Tablets

Each film coated tablet contains

Montelukast Sodium Eq. to Montelukast ………………..10 mg

Levocetirizine Dihydrochloride …………… ………….5mg

CROHIST-MK KID SYRUP

Each 5ml contains

Montelukast Sodium Eq. to Montelukast ………………….4 mg

Levocetirizine Dihydrochloride ………………………2.5mg

CROHIST–MK is a combination medication of Montelukast sodium and Levocetirizine hydrochloride. Montelukast sodium is an orally active compound that binds with high affinity and selectivity to the Cysteinyl Leukotriene (CysLT1) receptor. Levocetirizine, the R-enantiomer of cetirizine, is a potent, selective and long acting H1 -histamine receptor antagonist with no anticholinergic activity.

INDICATIONS:-

CROHIST–MK & CROHIST-MK KID is indicated for the treatment of Allergic Rhinitis (Seasonal and Perennial) and in the chronic treatment of Asthma.

Recommended dose of CROHIST-MK

One tablet to be taken once daily in the evening.

Recommended dose of CROHIST-MK KID

For the children of 2-5 years – 2.5 ml is given once daily in the evening

PHARMCOLOGY:-

Pharmacodynamics
Montelukast:
Montelukast,(Leukotriene receptor antagonist) acts by binding to Cysteinyl Leukotriene (CysLTs) receptors which are potent inflammatory eicosanoids.

Levocetirizine:
Levocetirizine, the (R) enantiomer of cetirizine, is a potent and selective antagonist of peripheral H1-receptors.

PHARMACOKINETICS

Montelukast
Absorption
Montelukast is rapidly absorbed orally and the mean oral bioavailability is 64%.

Distribution
Montelukast is bound to plasma proteins more than 99%. The steady-state volume of distribution of Montelukast averages about 8 to 11 litres.

Metabolism
Montelukast is extensively metabolized and plasma concentrations are undetectable at steady state in adults and pediatric patients.

Elimination
Montelukast and its metabolites are excreted almost exclusively through the bile.

Levocetirizine

Absorption
Levocetirizine is rapidly and extensively absorbed following oral administration. Peak plasma concentrations are achieved 0.9 g h after dosing.

Distribution
Levocetirizine is widely distributed and 90% bound to plasma proteins.

Biotransformation
The extent of metabolism of Levocetirizine in humans is less than 14% of the dose. Metabolic pathways include aromatic oxidation, N- and O-dealkylation and taurine conjugation.

CONTRAINDICATIONS:

Patients those who are hypersensitive to Montelukast, Levocetirizine, Piperazine derivatives or to any other components of the formulation and renal impaired patients are not supposed to take this medication.

WARNINGS AND PRECAUTIONS

Montelukast

Eosinophilic conditions

Some patients on treatment with Montelukast may show symptoms of eosinophilia, presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, a disease condition, which is often treated with systemic corticosteroid therapy.

Levocetirizine

It is recommended not to use in patients who has eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, etc.

DRUG INTERACTIONS

Montelukast:
Phenobarbital, which induces hepatic metabolism, decreased the AUC of Montelukast approximately 40% following a single 10-mg dose of Montelukast.

Levocetirizine:
In sensitive patients the simultaneous administration of cetirizine or Levocetirizine and alcohol or other CNS depressants may have effects on the central nervous system.

Pregnancy

This combination should not be used during pregnancy since no well-controlled studies of either Montelukast or Levocetirizine have been conducted in pregnant women.

Lactation

Levocetirizine is excreted in breast-milk and thus the combination is not recommended during lactation.

SIDE-EFFECTS

Montelukast

Common side effects include dyspepsia, abdominal pain, rash, dizziness, headache, fatigue, fever, trauma, cough, nasal congestion, etc.

Levocetirizine

Somnolence, Fatigue, Nasopharyngitis, dry mouth, and Pharyngitis were observed in subjects 12 years of age and older.

OVERDOSAGE

No data is available to prove the overdosage of this combination. However, overdosage has been

reported with individual molecules.

Montelukast

There have been reports of acute over-dosage in post-marketing experience and clinical studies

with Montelukast with a dose as high as 1000 mg.The most frequently occurring adverse experiences included abdominal pain, somnolence, thirst, headache, vomiting and psychomotor hyperactivity.

Levocetirizine

Symptoms of overdose may include drowsiness in adults and initially agitation and restlessness

followed by drowsiness, in children.