Salmeterol xinafoate
Salmeterol xinafoate Uses, Dosage, Side Effects, Food Interaction and all others data.
Salmeterol xinafoate stimulates intracellular adenyl cyclase, the enzyme that catalyses the conversion of ATP to cyclic-3',5'-adenosine monophosphate (cAMP) resulting in relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from mast cells.
Salmeterol xinafoate is a long acting beta-2 adrenergic receptor agonist that binds to both the active and exo sites of the beta-2 adrenergic receptor. Salmeterol xinafoate has a longer duration of action than other beta-2 agonists like salbutamol. Patients should be counselled regarding the risks of long acting beta agonist (LABA) monotherapy, hypokalemia, hypoglycemia, and not to take this drug with another LABA.
| Trade Name | Salmeterol xinafoate |
| Availability | Prescription only |
| Generic | Salmeterol |
| Salmeterol Other Names | Salmaterol, Salmeterol, Salmeterolum |
| Related Drugs | Dupixent, Xolair, ProAir Digihaler, albuterol, montelukast, Symbicort, Singulair, ProAir HFA, Breo Ellipta, Ventolin |
| Type | |
| Formula | C25H37NO4 |
| Weight | Average: 415.5656 Monoisotopic: 415.272258677 |
| Protein binding | Salmeterol is 96% protein bound in plasma to albumin and alpha-1-acid glycoprotein. |
| Groups | Approved |
| Therapeutic Class | Long-acting selective β2-adrenoceptor stimulants |
| Manufacturer | |
| Available Country | Russia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Inhaled Salmeterol xinafoate exerts a significant bronchodilating effect within 10 to 20 minutes of single-dose administration with asthma and this effect lasts for up to 12 hours or more. Salmeterol xinafoate has a beneficial effect on airway mucociliary clearance that will reduce the incidence of respiratory tract infections.
Salmeterol xinafoate produces a significant protective effect against Exercise Induced Asthma (EIA) for up to 9 to 12 hours in both adolescents and adults.
Salmeterol xinafoate improves the overnight PEFR (Peak Expiratory Flow Rate) and controls the symptoms of the patients with nocturnal asthma. The use of Salmeterol xinafoate avoids exposure of children to theophylline or high-dose corticosteroid, with their attendants risks.
Addition of Salmeterol xinafoate to inhaled corticosteroid therapy is significantly more effective in terms of an improvement in lung function, symptom control and a reduction in the use of rescue bronchodilator therapy (use of short acting beta2-agonist).
Addition of Salmeterol xinafoate to inhaled corticosteroid therapy also significantly reduces the use of inhaled corticosteroids
Salmeterol xinafoate is also used to associated treatment for these conditions: Asthma, Chronic Obstructive Pulmonary Disease (COPD), Exercise-Induced Bronchospasm
How Salmeterol xinafoate works
Beta-2 adrenoceptor stimulation causes relaxation of bronchial smooth muscle, bronchodilation, and increased airflow.
Salmeterol xinafoate is hypothesized to bind to 2 sites on the beta-2 adrenoceptor. The saligenin moiety binds to the active site of the beta-2 adrenoceptor. The hydrophilic tail of salmeterol binds to leucine residues in the exo-site of the beta-2 adrenoceptor almost irreversibly, allowing salmeterol to persist in the active site, which is responsible for it's long duration of action.
Another hypothesis is that the lipophilic drug diffuses into lipid bilayer of smooth muscle cells and provides a depot of drug to the cells over a longer period of time.
Dosage
Salmeterol xinafoate dosage
Inhalation/Respiratory-
Chronic asthma:
- Adult: As metered dose aerosol or dry powder inhaler: 50 mcg bid, or up to 100 mcg bid if necessary, in asthma patients with more severe airways obstruction.
- Child: 4-12 yr 50 mcg bid.
Prophylaxis of exercise-induced asthma:
- Adult: As metered dose aerosol or dry powd inhaler: 50 mcg at least 30 min prior to exercise.
- Child: ≥4 yr Same as adult dose.
Chronic obstructive pulmonary disease:
- Adult: As metered dose aerosol or dry powder inhaler: 50 mcg bid.
Side Effects
Dose related tremor, subjective palpitations and headaches are usually mild and transient. Skin reactions, muscle cramps, non-specific chest pain, local irritation and arthralgia have been reported.
Toxicity
Patients experiencing an overdose have presented with metabolic acidosis, hyperlactatemia, anxiety, palpitations, chest pain, sinus tachycardia, ST depression, hypokalemia, hypophosphatemia. Though patients may also present with seizures, angina, hypertension or hypotension, arrhythmia, headache, tremor, muscle cramps, dry mouth, nausea, dizziness, fatigue, malaise, insomnia, and hyperglycemia. Patients should be given symptomatic and supportive treatment which may include intravenous fluids, potassium supplementation, a cardioselective beta-blocker, and cardiac monitoring.
Data regarding the LD50 of salmeterol is not readily available.
Precaution
Patient with CV disease, CNS disorders, DM, hyperthyroidism, hypokalaemia, seizure disorders, ketoacidosis. Not intended for the relief of acute bronchospasm. Hepatic impairment. Pregnancy and lactation.
Interaction
As with all the other beta2-agonists there may be interaction with betablocking agents at the receptor site when given concomitantly.
Monoamino Oxidase Inhibitors and Tricyclic Antidepressants : These agent should be used with caution because Salmeterol xinafoate may be potentiated by these agents.
Food Interaction
No interactions found.Salmeterol xinafoate Hypertension interaction
[Moderate] Adrenergic bronchodilators can stimulate cardiovascular beta- 1 and beta- 2 receptors, resulting in adverse effects such as tachycardia, palpitation, peripheral vasodilation, blood pressure changes, and ECG changes (e.g., flattening of the T wave; prolongation of the QT interval; ST segment depression).
Direct stimulation of cardiac tissues is mediated by beta- 1 receptors and thus less likely to occur with beta-2-selective agents such as albuterol.
However, beta-2-selectivity is not absolute and can be lost with larger doses.
High dosages of these agents have been associated with precipitation or aggravation of angina, myocardial ischemia, and cardiac arrhythmias.
Therapy with adrenergic bronchodilators should be administered cautiously in patients with sensitivity to sympathomimetic amines, hyperthyroidism, and The recommended dosages should not be exceeded.
Salmeterol xinafoate Drug Interaction
Moderate: duloxetine, escitalopram, budesonide / formoterol, albuterolMinor: fluticasone / salmeterolUnknown: aspirin, aspirin, ipratropium, amoxicillin / clavulanate, celecoxib, rosuvastatin, heparin, atorvastatin, acetaminophen, clopidogrel, montelukast, tiotropium, cyanocobalamin, ascorbic acid, cholecalciferol
Salmeterol xinafoate Disease Interaction
Moderate: cardiovascular, diabetes, hypokalemia, seizures, hepatic dysfunction
Volume of Distribution
In asthmatic patients, the volume of distribution of the central compartment is 177L and the volume of distribution of the peripheral compartment is 3160L.
Elimination Route
In asthmatic patients, a 50µg dose of inhaled salmeterol powder reaches a Cmax of 47.897pg/mL, with a Tmax of 0.240h, and an AUC of 156.041pg/mL/h.
Half Life
The half life of salmeterol is 5.5h.
Clearance
The average clearance of salmeterol in a group of asthmatic patients was 392L/h. Further data regarding the clearance of salmeterol is not readily available.
Elimination Route
Salmeterol xinafoate is 57.4% eliminated in the feces and 23% in the urine. Less than 5% of a dose is eliminated in the urine as unchanged salmeterol.
Pregnancy & Breastfeeding use
Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Contraindication
Monotherapy in the treatment of asthma. Treatment of status asthmaticus, other acute episodes of asthma or COPD.
Special Warning
Hepatic Impairment: Because Salmeterol xinafoate is extensively metabolised by the liver, patients with hepatic impairment receiving the drug should be closely monitored.
Acute Overdose
Symptoms: Dizziness, HTN or hypotension, tremor, headache, tachycardia, hypokalaemia, seizures, angina, arrhythmias, nervousness, muscle cramps, dry mouth, palpitations, nausea, fatigue, malaise, insomnia, hyperglycaemia, metabolic acidosis.
Management: Symptomatic and supportive treatment. β-blockers may be considered but should be used with caution.
Storage Condition
Store between 20-25° C. Protect from heat or sunlight.
Innovators Monograph
You find simplified version here Salmeterol xinafoate
Salmeterol xinafoate contains Salmeterol see full prescribing information from innovator Salmeterol xinafoate Monograph, Salmeterol xinafoate MSDS, Salmeterol xinafoate FDA label
FAQ
What is Salmeterol xinafoate used for?
Salmeterol xinafoate is used to control wheezing, shortness of breath, coughing, and chest tightness in people with chronic obstructive pulmonary disease.
How safe is Salmeterol xinafoate?
Salmeterol xinafoate may increase the risk of asthma-related death. Use only the prescribed dose of this medication, and do not use it for longer than your doctor recommends. Follow all patient instructions for safe use. Talk with your doctor about your individual risks and benefits of using salmeterol inhalation.
What are the common side effects of Salmeterol xinafoate?
Salmeterol xinafoate may common side effects are include:
- shaking of a part of your body that you cannot control
- headache
- nervousness
- dizziness
- cough
- stuffed nose
- runny nose
- ear pain
- muscle pain, stiffness, or cramps
- joint pain
- sore, irritated throat
- flu-like symptoms
- nausea
- heartburn
- tooth pain
- dry mouth
- sores or white patches in the mouth
- red or irritated eyes
- difficulty falling asleep or staying asleep
- burning or tingling of the hands or feet
Is Salmeterol xinafoate safe during pregnancy?
Salmeterol xinafoate has been considered a medication of choice if long-acting beta agonist treatment is needed during pregnancy. If a woman's asthma was well-controlled with Salmeterol xinafoate before pregnancy, it may be recommended to continue using it during pregnancy.
Is Salmeterol xinafoate safe during breastfeeding?
Using a Salmeterol xinafoate inhaler is not thought to cause high enough levels in the mother's bloodstream to pass into breast milk in large amounts. Using inhaled bronchodilators is usually thought to be compatible with breastfeeding.
Can I drink alcohol with Salmeterol xinafoate?
Yes, you can drink alcohol with Salmeterol xinafoate.
Can I drive after taking Salmeterol xinafoate ?
Monitor serum potassium level while taking Salmeterol xinafoate. It may cause dizziness, do not drive a car or operate machinery while taking Salmeterol xinafoate.
When should Salmeterol xinafoate be taken?
Salmeterol xinafoate is usually used twice a day, in the morning and evening, about 12 hours apart. Use Salmeterol xinafoate at around the same times every day.
How long does it take for Salmeterol xinafoate to work?
Salmeterol xinafoate is called a long-acting bronchodilator. Its effects are usually felt within 20 minutes and last for around 12 hours.
Is Salmeterol xinafoate a reliever?
Salmeterol xinafoate is called a long-acting bronchodilator. It is usually used with both a fast-acting reliever and preventer medicine.
Is Salmeterol xinafoate fast acting?
Salmeterol xinafoate is a partial agonist, has a relatively slow onset of action (10 to 30 minutes)
Does Salmeterol xinafoate increase blood pressure?
Salmeterol xinafoate can increase heart rate, blood pressure, and cause chest pain and excitement, especially if used in higher doses than recommended or used in those with coronary heart disease or high blood pressure.
Can Salmeterol xinafoate cause anxiety?
Possible side effects include nervousness, sweating, fast heartbeat, and anxiety.
Can I overdose on Salmeterol xinafoate?
If this medication is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.
Does Salmeterol xinafoate cause thrush?
Salmeterol xinafoate may cause a fungus infection of the mouth or throat (thrush).
What happens if I miss a dose?
Skip the missed dose and continue your regular dosing schedule. Do not inhale a double dose to make up for a missed one.
Is Salmeterol xinafoate inhaler a steroid?
Salmeterol xinafoate a combination of a steroid plus a long-acting bronchodilator. fluticasone furoate(Trelegy Ellipta) a combination of a steroid, an anticholinergic, and a long-acting bronchodilator drug.
Can I stop using Salmeterol xinafoate?
Do not stop using Salmeterol xinafoate without talking to your doctor. If you suddenly stop using Salmeterol xinafoate, your symptoms may worsen. Before you use the Salmeterol xinafoate inhaler the first time, ask your doctor, pharmacist, or respiratory therapist to show you how to use it.
How do you stop taking Salmeterol xinafoate?
Do not stop using Salmeterol xinafoate inhalation without first talking to your doctor. Your asthma symptoms may get worse after you stop using the medication. If you also use a steroid medication, you should not stop using it suddenly. Follow your doctor's instructions about tapering your dose.
