Cetrilin-plus- (Levocetrizine+Montekulast)- Film coated tablets- TAJ PHARMA
Montelukast and Levocetirizine as Treatment for Allergic Rhinitis
COMPOSITION
Each tablet contains:
Montelukast sodium equivalent to montelukast 10 mg and Levocetirizine dihydrochloride 5 mg
Product Description
Montelukast sodium is a selective and orally active leukotriene receptor antagonist that inhibits the cysteinyl leukotriene (CysLT 1 ), receptor. Levocetirizine is the R-enantiomer of cetirizine. Levocetirizine is an orally active, potent, selective and long acting H 1 -histamine receptor antagonist with no anticholinergic activity.
INDICATIONS
Cetrilin Tabletsare indicated for relief of symptoms of allergic rhinitis [seasonal or perennial], as prophylaxis in seasonal allergic rhinitis and treatment of comorbid asthma and allergic rhinitis in patients 15 years of age and over.
Cetrilin Tablets for Kids are indicated for the relief of symptoms of allergic rhinitis [seasonal or perennial], as prophylaxis in seasonal allergic rhinitis and treatment of comorbid asthma and allergic rhinitis in patients 2 to 5 years of age.
DOSAGE & ADMINISTRATION
Adults [>15years]: 1 Cetrilin Tablet once daily
Children (2-5years): One Cetrilin Kid Tablet once daily Due to the lack of clinical data, the administration of this product to infants less than 2 years of age is not recommended.
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CONTRAINDICATIONS
Cetrilin is contraindicated in patients with known hypersensitivity to montelukast sodium, levocetirizine or cetirizine or to any other component of this product. Cetrilin is also contraindicated in patients with severe renal impairment at less than 10ml/min creatinine clearance. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medication.
WARNINGS & PRECAUTIONS
MONTELUKAST
Eosinophilic Conditions
In rare cases, patients on therapy with Montelukast may present with systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition, which is often treated with systemic corticosteroid therapy. These events usually, but not always, have been associated with the reduction of oral corticosteroid therapy.
LEVOCETIRIZINE
Patients should avoid engaging in hazardous occupation requiring complete mental alertness such as driving or operating machinery when taking levocetirizine. Precaution is recommended with intake of alcohol and in those who are on CNS depressants.
DRUG INTERACTIONS
MONTELUKAST In drug-interaction studies, the recommended clinical dose of montelukast did not have clinically important effects on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (norethindrone 1 mg/ethinyl estradiol 35 mcg), terfenadine, digoxin, and warfarin. Although additional specific interaction studies were not performed, montelukast was used concomitantly with a wide range of commonly prescribed drugs in clinical studies without evidence of clinical adverse interactions. These medications included thyroid hormones, sedative hypnotics, non-steroidal anti-inflammatory agents, benzodiazepines, and decongestants. Phenobarbital, which induces hepatic metabolism, decreased the AUC of montelukast approximately 40% following a single 10-mg dose of montelukast. No dosage adjustment for montelukast is recommended. It is reasonable to employ appropriate clinical monitoring when potent cytochrome P450 enzyme inducers, such as phenobarbital or rifampin, are co-administered with montelukast.
LEVOCETIRIZINE In vitro data indicate that levocetrizine is unlikely to produce pharmacokinetic interactions through inhibition or induction of liver drug-metabolizing enzymes. No in vivo drug-drug interaction studies have been performed with levocetrizine. Drug interaction studies have been performed with racemic cetrizine. Pharmacokinetic interaction studies performed with racemic cetrizine demonstrated that cetrizine did not interact with antipyrine, pseudoephedrine, erythromycin, azithromycin, ketoconazole and cimetidine. There was a small decrease (~16%) in the clearance of cetrizine caused by a 400 mg dose of theophylline. It is possible that higher theophylline doses could have a greater effect. Ritonavir increased the plasma AUC of cetrizine by about 42% accompanied by an increase in half-life (53%) and a decrease in clearance (29%) of cetrizine. The disposition of ritonavir was not altered by concomitant cetrizine administration.
Renal Impairment
As levocetrizine is mainly excreted through urine, dosage adjustment may be required in patients with impaired renal function. Hence this combination should be used with caution in such patients.
Hepatic Impairment
As montelukast is mainly excreted through bile, caution is to be exercised while prescribing this combination in patients with impaired hepatic function.
Pregnancy
There are no adequate and well-controlled studies of either montelukast or levocetrizine in pregnant women. Hence this combination should not be used during pregnancy.
Lactation
Since levocetirizine is excreted in breast-milk the combination is not recommended during lactation.
Pediatric Use:
Montelukast
The safety of Montelukast 4-mg chewable tablets in pediatric patients aged 2 to 14 years with allergic rhinitis is supported by data from studies conducted in pediatric patients aged 2 to 14 years with asthma. A safety study in pediatric patients 2 to 14 years of age with seasonal allergic rhinitis demonstrated a similar safety profile. The safety and effectiveness in pediatric patients below the age of 12 months with asthma and 6 months with allergic rhinitis have not been established.
Levocetirizine: The safety and effectiveness of Levocetirizine in pediatric patients under 2 years of age have not been established. The effectiveness of Levocetirizine 2.5 mg once daily for the treatment of the symptoms of seasonal and perennial allergic rhinitis in children 2 to 6 years of age is supported by the extrapolation of demonstrated efficacy of Levocetirizine 5 mg once daily in patients 12 years of age and older and by the pharmacokinetic comparison in adults and children. In children 2 to 6 years of age the recommended dose of 2.5 mg once daily should not be exceeded. Geriatric Use Montelukast: No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Levocetirizine: Clinical studies of levocetirizine for each approved indication did not include sufficient numbers of patients aged 65 years and older to determine whether they respond differently than younger patients. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy.
UNDESIRABLE EFFECTS
Montelukast Common side effects include dyspepsia, abdominal pain, rash, dizziness, headache, fatigue, fever, trauma, cough, nasal congestion.
Levocetirizine Use of levocetirizine has been associated with somnolence, fatigue, nasopharyngitis, dry mouth, and pharyngitis in subjects 12 years of age and older. Further uncommon incidences of adverse reactions like asthenia or abdominal pain were observed.
OVERDOSAGE
MONTELUKAST
There have been reports of acute over-dosage in post-marketing experience and clinical studies with montelukast. These include reports in adults and children with a dose as high as 1000 mg.
consistent with the safety profile in adults and pediatric patients. There were no adverse experiences in the majority of over-dosage reports. The most frequently occurring adverse experiences were consistent with the safety profile of montelukast and included abdominal pain, somnolence, thirst, headache, vomiting and psychomotor hyperactivity. It is not known whether montelukast is removed by peritoneal dialysis or hemodialysis.
LEVOCETIRIZINE
Symptoms of overdose may include drowsiness in adults and initially agitation and restlessness followed by drowsiness, in children. There is no known specific antidote to levocetrizine. Should overdose occur, symptomatic or supportive treatment is recommended. Levocetrizine is not effectively removed by dialysis and dialysis will be ineffective unless a dialyzable agent has been concomitantly ingested.
STORAGE
Store in a cool dry place. Protect from moisture and light.
Montelukast and Levocetirizine as Treatment for Allergic Rhinitis
COMPOSITION
Each tablet contains:
Montelukast sodium equivalent to montelukast 10 mg and Levocetirizine dihydrochloride 5 mg
Product Description
Montelukast sodium is a selective and orally active leukotriene receptor antagonist that inhibits the cysteinyl leukotriene (CysLT 1 ), receptor. Levocetirizine is the R-enantiomer of cetirizine. Levocetirizine is an orally active, potent, selective and long acting H 1 -histamine receptor antagonist with no anticholinergic activity.
INDICATIONS
Cetrilin Tabletsare indicated for relief of symptoms of allergic rhinitis [seasonal or perennial], as prophylaxis in seasonal allergic rhinitis and treatment of comorbid asthma and allergic rhinitis in patients 15 years of age and over.
Cetrilin Tablets for Kids are indicated for the relief of symptoms of allergic rhinitis [seasonal or perennial], as prophylaxis in seasonal allergic rhinitis and treatment of comorbid asthma and allergic rhinitis in patients 2 to 5 years of age.
DOSAGE & ADMINISTRATION
Adults [>15years]: 1 Cetrilin Tablet once daily
Children (2-5years): One Cetrilin Kid Tablet once daily Due to the lack of clinical data, the administration of this product to infants less than 2 years of age is not recommended.
Cetrilin is contraindicated in patients with known hypersensitivity to montelukast sodium, levocetirizine or cetirizine or to any other component of this product. Cetrilin is also contraindicated in patients with severe renal impairment at less than 10ml/min creatinine clearance. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medication.
WARNINGS & PRECAUTIONS
MONTELUKAST
Eosinophilic Conditions
In rare cases, patients on therapy with Montelukast may present with systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition, which is often treated with systemic corticosteroid therapy. These events usually, but not always, have been associated with the reduction of oral corticosteroid therapy.
LEVOCETIRIZINE
Patients should avoid engaging in hazardous occupation requiring complete mental alertness such as driving or operating machinery when taking levocetirizine. Precaution is recommended with intake of alcohol and in those who are on CNS depressants.
DRUG INTERACTIONS
MONTELUKAST In drug-interaction studies, the recommended clinical dose of montelukast did not have clinically important effects on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (norethindrone 1 mg/ethinyl estradiol 35 mcg), terfenadine, digoxin, and warfarin. Although additional specific interaction studies were not performed, montelukast was used concomitantly with a wide range of commonly prescribed drugs in clinical studies without evidence of clinical adverse interactions. These medications included thyroid hormones, sedative hypnotics, non-steroidal anti-inflammatory agents, benzodiazepines, and decongestants. Phenobarbital, which induces hepatic metabolism, decreased the AUC of montelukast approximately 40% following a single 10-mg dose of montelukast. No dosage adjustment for montelukast is recommended. It is reasonable to employ appropriate clinical monitoring when potent cytochrome P450 enzyme inducers, such as phenobarbital or rifampin, are co-administered with montelukast.
LEVOCETIRIZINE In vitro data indicate that levocetrizine is unlikely to produce pharmacokinetic interactions through inhibition or induction of liver drug-metabolizing enzymes. No in vivo drug-drug interaction studies have been performed with levocetrizine. Drug interaction studies have been performed with racemic cetrizine. Pharmacokinetic interaction studies performed with racemic cetrizine demonstrated that cetrizine did not interact with antipyrine, pseudoephedrine, erythromycin, azithromycin, ketoconazole and cimetidine. There was a small decrease (~16%) in the clearance of cetrizine caused by a 400 mg dose of theophylline. It is possible that higher theophylline doses could have a greater effect. Ritonavir increased the plasma AUC of cetrizine by about 42% accompanied by an increase in half-life (53%) and a decrease in clearance (29%) of cetrizine. The disposition of ritonavir was not altered by concomitant cetrizine administration.
Renal Impairment
As levocetrizine is mainly excreted through urine, dosage adjustment may be required in patients with impaired renal function. Hence this combination should be used with caution in such patients.
Hepatic Impairment
As montelukast is mainly excreted through bile, caution is to be exercised while prescribing this combination in patients with impaired hepatic function.
Pregnancy
There are no adequate and well-controlled studies of either montelukast or levocetrizine in pregnant women. Hence this combination should not be used during pregnancy.
Lactation
Since levocetirizine is excreted in breast-milk the combination is not recommended during lactation.
Pediatric Use:
Montelukast
The safety of Montelukast 4-mg chewable tablets in pediatric patients aged 2 to 14 years with allergic rhinitis is supported by data from studies conducted in pediatric patients aged 2 to 14 years with asthma. A safety study in pediatric patients 2 to 14 years of age with seasonal allergic rhinitis demonstrated a similar safety profile. The safety and effectiveness in pediatric patients below the age of 12 months with asthma and 6 months with allergic rhinitis have not been established.
Levocetirizine: The safety and effectiveness of Levocetirizine in pediatric patients under 2 years of age have not been established. The effectiveness of Levocetirizine 2.5 mg once daily for the treatment of the symptoms of seasonal and perennial allergic rhinitis in children 2 to 6 years of age is supported by the extrapolation of demonstrated efficacy of Levocetirizine 5 mg once daily in patients 12 years of age and older and by the pharmacokinetic comparison in adults and children. In children 2 to 6 years of age the recommended dose of 2.5 mg once daily should not be exceeded. Geriatric Use Montelukast: No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Levocetirizine: Clinical studies of levocetirizine for each approved indication did not include sufficient numbers of patients aged 65 years and older to determine whether they respond differently than younger patients. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy.
Montelukast Common side effects include dyspepsia, abdominal pain, rash, dizziness, headache, fatigue, fever, trauma, cough, nasal congestion.
Levocetirizine Use of levocetirizine has been associated with somnolence, fatigue, nasopharyngitis, dry mouth, and pharyngitis in subjects 12 years of age and older. Further uncommon incidences of adverse reactions like asthenia or abdominal pain were observed.
OVERDOSAGE
MONTELUKAST
There have been reports of acute over-dosage in post-marketing experience and clinical studies with montelukast. These include reports in adults and children with a dose as high as 1000 mg.
consistent with the safety profile in adults and pediatric patients. There were no adverse experiences in the majority of over-dosage reports. The most frequently occurring adverse experiences were consistent with the safety profile of montelukast and included abdominal pain, somnolence, thirst, headache, vomiting and psychomotor hyperactivity. It is not known whether montelukast is removed by peritoneal dialysis or hemodialysis.
LEVOCETIRIZINE
Symptoms of overdose may include drowsiness in adults and initially agitation and restlessness followed by drowsiness, in children. There is no known specific antidote to levocetrizine. Should overdose occur, symptomatic or supportive treatment is recommended. Levocetrizine is not effectively removed by dialysis and dialysis will be ineffective unless a dialyzable agent has been concomitantly ingested.
STORAGE
Store in a cool dry place. Protect from moisture and light.
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