Ontel D (zee)
Ontel D (zee) Uses, Dosage, Side Effects, Food Interaction and all others data.
Desloratadine is a long-acting, tricyclic, non-sedating, selective peripheral histamine H1-receptor antagonist which inhibits the release of pro-inflammatory mediators from human mast cells and basophils.
Desloratadine is a long-acting second-generation H1-receptor antagonist which has a selective and peripheral H1-antagonist action. Histamine is a chemical that causes many of the signs that are part of allergic reactions, such as the swelling of tissues. Histamine is released from histamine-storing cells (mast cells) and attaches to other cells that have receptors for histamine. The attachment of the histamine to the receptors causes the cell to be "activated," releasing other chemicals which produce the effects that we associate with allergies. Desloratadine blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Desloratadine does not enter the brain from the blood and, therefore, does not cause drowsiness.
Montelukast is a selective leukotriene receptor antagonist that inhibits the effects of cysteinyl leukotrienes in the airways. Cysteinyl leukotrienes and leukotriene receptor occupation have been correlated with the pathophysiology of asthma, including airway oedema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma.
Montelukast is a leukotriene receptor antagonist that demonstrates a marked affinity and selectivity to the cysteinyl leukotriene receptor type-1 in preference to many other crucial airway receptors like the prostanoid, cholinergic, or beta-adrenergic receptors. As a consequence, the agent can elicit substantial blockage of LTD4 leukotriene-mediated bronchoconstriction with doses as low as 5 mg. Moreover, a placebo-controlled, crossover study (n=12) demonstrated that montelukast is capable of inhibiting early and late phase bronchoconstriction caused by antigen challenge by 75% and 57% respectively.
In particular, it has been documented that montelukast can cause bronchodilation as soon as within 2 hours of oral administration. This action can also be additive to the bronchodilation caused by the concomitant use of a beta agonist. Nevertheless, clinical investigations performed with adults 15 years of age and older revealed that no additional clinical benefit is obtained when doses of montelukast greater than 10 mg a day are used.
Additionally, in clinical trials with adults and pediatric asthmatic patients aged 6 to 14 years, it was also determined that montelukast can reduce mean peripheral blood eosinophils by about 13% to 15% from baseline in comparison to placebo during double-blind treatment periods. At the same time, in patients aged 15 years and older who were experiencing seasonal allergic rhinitis, the use of montelukast caused a median reduction of 13% in peripheral blood eosinophil counts when compared to placebo as well.
| Trade Name | Ontel D (zee) |
| Generic | Desloratadine + Montelukast |
| Type | Tablet |
| Therapeutic Class | |
| Manufacturer | Zee Laboratories Ltd |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
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.
Montelukast is used for-
- The prophylaxis and chronic treatment of asthma in adults and paediatric patients 12 months of age and older.
- The relief of symptoms of seasonal allergic rhinitis in adults and paediatric patients 2 years of age and older.
Ontel D (zee) is also used to associated treatment for these conditions: Allergic Rhinitis (AR), Asthma, Chronic Idiopathic Urticaria, Common Cold, Nasal Congestion, Perennial Allergic Rhinitis (PAR), Seasonal Allergic Rhinitis, Nasal symptoms, Non-nasal symptoms, AntihistamineAsthma, Exercise-Induced Bronchospasm, Perennial Allergic Rhinitis (PAR), Seasonal Allergic Rhinitis
How Ontel D (zee) works
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.
Cysteinyl leukotrienes (CysLT) like LTC4, LTD4, and LTE4, among others, are eicosanoids released by a variety of cells like mast cells and eosinophils. When such CysLT bind to corresponding CysLT receptors like CysLT type-1 receptors located on respiratory airway smooth muscle cells, airway macrophages, and on various pro-inflammatory cells like eosinophils and some specific myeloid stem cells activities that facilitate the pathophysiology of asthma and allergic rhinitis are stimulated.
In particular, CysLT-mediated airway bronchoconstriction, occluding mucous secretion, vascular permeability, and eosinophil recruitment are all types of effects that facilitate asthma. Alternatively, in allergic rhinitis, CysLTs are released by the nasal mucosa when exposed to allergens during both early and late phase reactions and participate in eliciting symptoms of allergic rhinitis like a congested nose and airway.
Subsequently, montelukast is a leukotriene receptor antagonist that binds with high affinity and selectivity to the CysLT type 1 receptor, which consequently assists in inhibiting any physiological actions of CysLTs like LTC4, LTD4, and LTE4 at the receptor that may facilitate asthma or allergic rhinitis.
Dosage
Ontel D (zee) dosage
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
General information: Montelukast should be taken once daily. For asthma, the dose should be taken in the evening. For seasonal allergic rhinitis, the time of administration may be individualised to suit patients needs. Patients with both asthma and seasonal allergic rhinitis should take only one tablet daily in the evening.
Adults and adolescents 15 years of age and older with asthma or seasonal allergic rhinitis: The dosage is one 10 mg tablet daily.
Paediatric patients 6 to 14 years of age with asthma or seasonal allergic rhinitis: The dosage is one 5 mg tablet daily. No dosage adjustment within this age group is necessary.
Paediatric patients 2 to 5 years of age with asthma or seasonal allergic rhinitis: The dosage is one 4 mg tablet daily.
Paediatric patients 12 to 23 months of age with asthma: The dosage is one 4 mg tablet daily to be taken in the evening. Safety and effectiveness in paediatric patients younger than 12 months of age have not been established.
Side Effects
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.
Adolescents and Adults 15 years of age and older: In placebo-controlled clinical trials, Montelukast has been evaluated for safety in approximately 2600 adolescent and adult patients of 15 years and older, the following adverse experiences reported with Montelukast occurred in greater than or equal to 1% of patients.
- General: Asthenia/fatigue, Fever, Pain
- Gastrointestinal: Dyspepsia, Gastroenteritis; Nervous
- System/Psychiatric: Dizziness, Headache
- Respiratory System: Congestion, Cough, Influenza
- Skin: Rash; Laboratory adverse experiences: ALT increase, AST increase, Pyuria.
Paediatric patients 6 to 14 years of age: In paediatric patients receiving montelukast, the following events occurred with a frequency 2% are diarrhoea, laryngitis, pharyngitis, nausea, otitis, sinusitis, and viral infection. With prolonged treatment, the adverse profile did not change significantly.
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.
The adverse effects associated with overdosage of montelukast include abdominal pain, somnolence, thirst, headache, vomiting, psychomotor hyperactivity, and less frequently, convulsion.
The oral LD50 value determined for mice and rats is >5000 mg/kg.
Montelukast has not been studied in pregnant women. Consequently, it should be used during pregnancy only if clearly needed.
Additionally, as it is unknown whether montelukast is excreted into human breast milk, there is also caution regarding the use of the medication in nursing mothers.
The plasma half-life of montelukast is somewhat prolonged in elderly patients, although no dosage adjustment is generally necessary.
Precaution
Hepatic and renal impairment. Pregnancy and lactation.
Montelukast is not indicated for use in the reversal of bronchospasm in acute asthma attacks (in case of status asthmaticus). Patients with known aspirin sensitivity should continue avoidance of aspirin or other NSAID, while taking Montelukast.
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. Physician should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients. A causal association between Montelukast and these underlying conditions has not been established.
Interaction
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.
Montelukast has been administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma with no apparent increase in adverse reactions. In drug interaction studies, the recommended clinical dose of montelukast did not have clinically important effects on the pharmacokinetics of the following drugs: Theophylline, Prednisolone, oral contraceptives (Norethindrone 1 mg/Ethinyl Oestradiol 35 mg), 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 clinically evident adverse interactions. These medications included thyroid hormones, sedative hypnotic, 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.
Volume of Distribution
The steady-state volume of distribution recorded for montelukast is an average between 8 to 11 litres.
Elimination Route
Desloratadine administered orally for ten days to healthy volunteers as a 5 mg tablet once daily resulted in a mean Tmax of approximately 3 hours, a mean steady-state Cmax 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.
It has been observed that montelukast is quickly absorbed following administration by the oral route. The oral bioavailability documented for the drug is 64%. Furthermore, it seems that having a regular meal in the morning or even a high fat snack in the evening does not affect the absorption of montelukast.
Half Life
Desloratadine has a mean plasma elimination half-life of approximately 27 hours.
Studies have demonstrated that the mean plasma half-life of montelukast varies from 2.7 to 5.5 hours when observed in healthy young adults.
Clearance
The plasma clearance documented for montelukast is an average of 45 mL/min when observed in healthy adults.
Elimination Route
Approximately 87% of a C-desloratadine dose was equally recovered in urine and feces as metabolic products.
It has been reported that montelukast and its metabolites are almost exclusively excreted in the bile and into the feces.
Pregnancy & Breastfeeding use
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.
Pregnancy: Montelukast crosses the placenta following oral dosing in rats and rabbits. There are, however, no adequate and well controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, Montelukast should be used during pregnancy only if clearly needed.
Lactation: It is not known if Montelukast is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Montelukast is given to a nursing mother.
Contraindication
Desloratadine is contraindicated in patient having hypersensitivity to this medication or to any of its ingredients or Loratadine.
Montelukast is contraindicated to patients with hypersensitivity to any component of this product.
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.
Paediatric use: Safety and efficacy of Montelukast has been established in adequate and well controlled studies in paediatric patients with asthma and allergic rhinitis between age 1 to 14 years. Long term trials evaluatingthe effect of chronic administration of Montelukast on linear growth in paediatric patients have not been conducted.
Geriatric use: Of the total number of subjects in clinical studies of Montelukast, 3.5% were 65 years of age and over and 0.4% were 75 years of age and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects. But greater sensitivity of some older individuals cannot be ruled out.
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.
Symptoms: Abdominal pain, somnolence, thirst, headache, vomiting, and psychomotor hyperactivity.
Management: Supportive and symptomatic treatment. If indicated, unabsorbed material should be removed from the GI tract.
Storage Condition
Store in a cool and dry place, protected from light.
Store at 25° C. Protect from moisture and light.
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