relukast
relukast Uses, Dosage, Side Effects, Food Interaction and all others data.
relukast 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.
relukast 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 | relukast |
| Availability | Prescription only |
| Generic | Montelukast |
| Montelukast Other Names | Montelukast, Montélukast, Montelukastum |
| Related Drugs | Dupixent, Xolair, Trelegy Ellipta, ProAir Digihaler, prednisone, albuterol, cetirizine, loratadine, fluticasone nasal, promethazine |
| Weight | 10mg, 4mg, 5mg |
| Type | Tablet, Film Coated, Chewable |
| Formula | C35H36ClNO3S |
| Weight | Average: 586.183 Monoisotopic: 585.21044242 |
| Protein binding | It has been determined that the protein binding of montelukast to plasma proteins exceeds 99%. |
| Groups | Approved |
| Therapeutic Class | Leukotriene receptor antagonists |
| Manufacturer | Hexal Ag |
| Available Country | Saudi Arabia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
relukast 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.
relukast is also used to associated treatment for these conditions: Asthma, Exercise-Induced Bronchospasm, Perennial Allergic Rhinitis (PAR), Seasonal Allergic Rhinitis
How relukast works
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
relukast dosage
General information: relukast 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
Adolescents and Adults 15 years of age and older: In placebo-controlled clinical trials, relukast has been evaluated for safety in approximately 2600 adolescent and adult patients of 15 years and older, the following adverse experiences reported with relukast 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
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.
relukast 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
relukast 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 relukast.
In rare cases, patients on therapy with relukast 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 relukast and these underlying conditions has not been established.
Interaction
relukast 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, relukast 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 relukast approximately 40% following a single 10 mg dose of relukast. No dosage adjustment for relukast 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 relukast.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
relukast Drug Interaction
Unknown: fluticasone / salmeterol, aspirin, aspirin, diphenhydramine, ubiquinone, duloxetine, omega-3 polyunsaturated fatty acids, fluticasone nasal, pregabalin, metoprolol, metoprolol, albuterol, budesonide / formoterol, levothyroxine, acetaminophen, albuterol, cyanocobalamin, ascorbic acid, cholecalciferol, cetirizine
relukast Disease Interaction
Major: neuropsychiatric disordersModerate: liver disorder, PKU, pulmonary disorders
Volume of Distribution
The steady-state volume of distribution recorded for montelukast is an average between 8 to 11 litres.
Elimination Route
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
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
It has been reported that montelukast and its metabolites are almost exclusively excreted in the bile and into the feces.
Pregnancy & Breastfeeding use
Pregnancy: relukast 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, relukast should be used during pregnancy only if clearly needed.
Lactation: It is not known if relukast is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when relukast is given to a nursing mother.
Contraindication
relukast is contraindicated to patients with hypersensitivity to any component of this product.
Special Warning
Paediatric use: Safety and efficacy of relukast 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 relukast on linear growth in paediatric patients have not been conducted.
Geriatric use: Of the total number of subjects in clinical studies of relukast, 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
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 at 25° C. Protect from moisture and light.
Innovators Monograph
You find simplified version here relukast
relukast contains Montelukast see full prescribing information from innovator relukast Monograph, relukast MSDS, relukast FDA label
FAQ
What is relukast used for?
relukast is used to prevent the symptoms of asthma. It's usually prescribed when asthma is mild and can stop it from getting worse.
How safe is relukast?
relukast was well tolerated. Adverse drug reactions occurred in 14 out of 6158 patients. None of the adverse events was serious. Accordingly, relukast 10mg is a safe and effective treatment for patients with both asthma and allergic rhinitis.
Do relukast make me sleepy?
No, relukast should not make you sleepy. Antihistamines are a group of medications that are commonly used to treat allergies and one of the side effects of antihistamines is drowsiness.
Why is relukast taken at night?
relukast exerts an increased action at night because of higher plasma concentration at the moment.
Does relukast help with Covid 19?
Treatment with relukast resulted in fewer incidents of clinical deterioration in hospitalized patients with COVID-19, suggesting that this treatment option may have clinical activity, according to study results published in the Journal of Asthma.
What does relukast do for allergies?
relukast is a drug that has been used to treat allergies and asthma for years. It helps to treat sneezing, nasal congestion and eye symptoms in patients with allergies. It also helps to treat inflammation in some patients with asthma.
Does relukast help with mucus?
relukast is a cysteinyl leukotriene antagonist, which also reduces sputum and blood eosinophils.
Is relukast safe during breastfeeding?
relukast is approved for use in children as young as 6 months of age and has been used in neonates in dosages far greater than the amounts in breastmilk. Amounts ingested by the infant would not be expected to cause any adverse effects in breastfed infants.
Is relukast safe during pregnancy?
Using relukast more commonly known as Singulair, during pregnancy is probably okay for your developing baby.
What are side effects of relukast?
Common side effects of relukast include upper respiratory infection, fever, headache, sore throat, cough, stomach pain, diarrhea, earache or ear infection, flu, runny nose, and sinus infection.
Does relukast cause night terrors?
In the UK, the most frequently reported suspected neuropsychiatric reactions associated with relukast have been nightmares/night terrors, depression, insomnia, aggression, anxiety and abnormal behaviour or changes in behaviour. These events were reported in all age groups.
Can I take relukast in the morning?
If you are taking relukast to prevent only allergies, take your dose either in the morning or the evening. If you are taking this medication to prevent breathing problems during exercise, take your dose at least 2 hours before exercise. Do not take more than one dose in 24 hours.
Is relukast an anti inflammatory?
relukast is a type of medicine known as a leukotriene receptor antagonist. It works by blockingthe action of leukotrienes which are chemicals released by the body as part of inflammatory reactions.
Is relukast an inhaler?
Take relukast regularly every evening. Your doctor will prescribe a reliever inhaler for you to use in case you have an asthma attack. Make sure that you keep it with you all the time.
Can I take relukast with Tylenol?
No interactions were found between relukast and Tylenol. This does not necessarily mean no interactions exist. Always consult your healthcare provider.
Can I take vitamins with relukast?
No interactions were found between multivitamin and Singulair. This does not necessarily mean no interactions exist. Always consult your healthcare provider.
Who should not take relukast?
The boxed warning advises health care providers to avoid prescribing relukast for patients with mild symptoms, particularly those with allergic rhinitis.
Is relukast for severe asthma?
relukast has proven to be particularly effective in exercise-induced asthma and in asthma associated with allergic rhinitis. Other phenotypes where relukast is effective include asthma in obese patients, asthma in smokers, aspirin-induced asthma and viral-induced wheezing episodes.
Is relukast bad for kidneys?
We can say that relukast prevent kidney damage with antioxidant effect, independently of no.
Does relukast make me dizzy?
May cause psychiatric-type effects including agitation, aggressive behavior, anxiety, depression, abnormal dreams, and hallucinations. These have been reported in people of all ages taking Singulair. May cause dizziness or drowsiness and affect a person's ability to drive and operate machinery.
Does relukast affect the liver?
Liver injury from relukast is self limited and resolves in 1 to 4 months.
Can I take relukast everyday?
Most people take relukast once a day in the evening to prevent asthma or allergy symptoms. However, if exercise makes your asthma worse, your doctor might tell you to take relukast 2 hours before you exercise. Never take more than 1 dose a day.
What can't I take with relukast?
Avoid situations or activities that may trigger an asthma attack. If your asthma symptoms get worse when you take aspirin, avoid taking aspirin or other NSAIDs (nonsteroidal anti-inflammatory drugs) while you are taking relukast.
What happens if I take too much relukast?
There were no side effects reported in the majority of overdose reports. The most frequently occurring symptoms reported with overdose in adults and children included abdominal pain, sleepiness, thirst, headache, vomiting, and hyperactivity. Try to take Singulair Paediatric as prescribed.
What happens when I stop taking relukast?
As far as long-term Singulair side effects, the side effects you might have from Singulair don't change much even with longer treatment. Stopping Singulair suddenly typically doesn't cause withdrawal symptoms that can make your asthma worse. But to be on the safe side, talk to your doctor before stopping.
Can diabetics take relukast?
relukast was efficacious in both prevention and delayed intervention approaches, which implies relevance to patients with newly-diagnosed diabetes as well as individuals living with diabetes of longer duration.
Can I drink alcohol with relukast?
Yes, you can drink alcohol while taking relukast. You do not need to avoid any food or drink while taking relukast.
