Characteristics of the preparation Salbutamol (Ventolin)
- Pharmacological group: beta-adrenomimetics, tocolytics
- Pharmacological action: bronchodilator, tocolytic.
- Effects on receptors: beta2-adrenergic receptors (agonist)
- Systematic (IUPAC) name: (RS) -4- [2- (tert-butylamino) -1-hydroxyethyl] -2- (hydroxymethyl) phenol
- Legal status: available only on prescription
- Application: oral, inhalation, intravenous
- Metabolism: liver
- Half-life: 1.6 hours
- Excretion: kidney
- Formula: C13H21NO3
- The pier. weight: 239.311
Salbutamol (an international nonproprietary name) or Albuterol (the name established in the US) is an agonist of beta2-adrenergic short-acting receptors. The drug is used to relieve bronchospasm in diseases such as asthma and chronic obstructive pulmonary disease. Among the brands of the drug can be called Ventolin.
Salbutamol is the first selective beta2 receptor agonist released on the market in 1968. For the first time, the Allen & Hanburys company starts selling the drug under the trademark Ventolin. The drug has gained instant success, and since then and to this day is used to treat asthma.
Salbutamol sulfate is available under the brand names Ventolin HFA, ProAir or Proventil. Usually Salbutamol is used by inhalation, which provides a direct effect on the smooth muscles of the bronchi. Usually, metered-dose inhalers (MDIs), nebulizers or other proprietary products (eg, Rotahaler or Autohaler) are used. With this application, the maximum effect of Salbutamol can be observed in 5-20 minutes after administration, but some relief may be noticeable immediately after use. The drug can also be administered intravenously.
Albuterol sulfate is a selective beta-2 adrenergic agonist, very similar in structure and action to Clenbuterol. Unlike clenbuterol, however, Salbutamol is readily available as a prescription drug in the United States called Albuterol. Salbutamol is most often found in the form of an inhaler designed to inhale a certain amount of the drug immediately and directly into the bronchi during an asthma attack. This form provides the lowest possible systemic activity of the drug, which minimizes undesirable cardiovascular side effects.
Salbutamol is also available as oral tablets, which provides systemic dosing of the drug. They are used among bodybuilders and athletes, and under the right conditions can provide significant stimulation of beta-2 and measurable loss of fat in the body.
Salbutamol was introduced into the US pharmaceutical market in 1980, and sold under the brand Ventolin. The oral version of the drug has become one of the most popular in history for the treatment of acute asthma attacks. As a result, many other companies began to invest in the drug market.
Ventolin is still available in the US, but the FDA has also approved a number of other generics and brand names. In most developed countries, Salbutamol is now also sold in inhaler and oral formulations. Popular trade names include Aerolin, Airomir, Asmasal, Asthalin, Asthavent, Asmol, Butahale, Buventol, ProAir, Proventil, Salamol, Sultanol and Volmax.
Salbutamol is most often supplied in the form of oral metered-dose inhalers and tablets of 2 mg, 4 mg or 8 mg each.
Albuterol sulfate (salbutamol sulfate) is a short-acting 2-adrenergic receptor agonist. This is a racemic preparation with the chemical designation (+/-) a1 - [(t-butylamino) methyl] -4-hydroxy-m-xylene, a1-diol sulfate (2: 1) (salt).
Instructions for use Salbutamol (Ventolina)
The usual initial dose for adults and children 12 years and older for controlling asthma is 2-4 mg 3-4 times a day. When used (not for its intended purpose) to burn fat, an effective dose of albuterol usually begins in the range of 1-2 tablets of 4 mg per day (1 tablet 1-2 times a day).
When an addictive dose is often increased to 4 mg 3-4 times a day. Particularly sensitive to the stimulant side effects of beta-agonists, users usually start with a low dose of 2 mg. The application intervals are distributed as evenly as possible to prevent seizures and maintain the active concentration of the drug in the blood throughout the day, as far as possible. As a marker of the effectiveness of the drug, athletes and bodybuilders often use body temperature readings.
An increase in temperature by a degree or two heights as a result of the use of the drug indicates an effective stimulation of lipolysis (removal of fatty acids stored in adipose tissue).
As noted when taking all beta-agonists, tolerance to the thermogenic benefits of this drug develops very quickly. This usually occurs when the body temperature is normalized. In connection with the potential side effects of these drugs to maintain their effectiveness is not recommended a constant dose increase. Instead, it is better for the user to stop using the medication for a while (4 weeks or longer) so that the body can restore normal concentrations of beta-adrenergic receptors. More recently, antihistamine Zaditen (Ketotifen) has become popular, a potent enhancer of beta-adrenergic receptors, especially beta-2 receptors. This drug can increase the thermogenic potential of beta-agonists, as well as the potential of the drug and the frequency of side effects.
Salbutamol is usually used to treat bronchospasm (caused by any cause, for example, allergic asthma or physical exertion), as well as chronic obstructive pulmonary diseases. The dosage of Salbutamol is still a contentious issue. The drug is supplied in the form of a metered-dose inhaler, spraying an average of 90 micrograms of substance in one application. To relieve the symptoms of asthma, it is most often recommended to take 2 breaths, if necessary, every 4 hours. Thus, a single dose of the drug is on average 180 ?g. For emergency assistance, aerosol spraying with salbutamol is recommended at a dose> 7.5 mg / h. Treatment continues until side effects including tremor or tachycardia are not irritating to the patient. In general, patients tolerate such large doses well enough. It is logical to recommend patients to change the dosage of Salbutamol and carry out 2 to 10 breaths for 45 minutes, with the proviso that using the drug in a larger amount will cause a worsening of the patient's condition.
The drug is also used for cystic fibrosis, in combination with ipratropium bromide, acetylcysteine ??and Pulmozyme and with subtypes of congenital myasthenic syndromes associated with Dok-7 protein mutations.
As a beta-2 agonist, Salbutamol is also used in obstetrics. Intravenously, Salbutamol is used as a tocolytic substance to relax the smooth muscle of the uterus, in order to delay premature delivery. Although the drug is more preferable compared to such drugs as atosiban and ritodrin, its role is largely replaced by a calcium channel blocker nifedipine, a more effective substance with better tolerability and applied orally.
Salbutamol was used to treat acute hyperkalemia due to its potassium-non-sparing characteristics and the ability to stimulate the flow of potassium into the cells.
Salbutamol was also used for spinal muscular atrophy. It is assumed that the drug is capable of modulating the alternative splicing of the SMN2 gene by increasing the amount of the SMN protein whose deficiency is considered to be the main cause of the disease.
Side effects of Salbutamol (Ventolina)
The most common side effects of Salbutamol are small tremor, anxiety, headache, muscle cramps, dry mouth and palpitations. Other symptoms may include tachycardia, arrhythmia, flushing, myocardial ischemia (rarely), and sleep and behavioral disorders. Rarely occurring, but important, side effects include allergic reactions of paradoxical bronchospasm, urticaria, Quincke's edema, hypotension and collapse. High doses can cause hypokalemia, which can be dangerous for patients with kidney failure and patients using certain diuretics and xanthine derivatives. Salbutamol is a stimulant of the central nervous system, which has the potential for a deadly overdose. Symptoms of overdose may include increased respiration, blood pressure disorders, irregular heartbeats, unconsciousness, tremors, panic, extreme anxiety, severe nausea, vomiting, or diarrhea.
The use of salbutamol in bodybuilding
It has been shown that Salbutamol causes an increase in muscle mass in rats. Some scientists say that the drug may become an alternative to Clenbuterol, a drug used for fat burning and muscle mass, although no studies have been conducted on the use of the drug for this purpose. Abuse of the drug can be detected by determining its presence in plasma and urine, in amounts usually exceeding 1000 µg / l.
In clinical trials, it has not been possible to demonstrate conclusive evidence that Salbutamol and other beta2-agonists can cause increased performance in healthy athletes. Despite this, Salbutamol is indicated in the "Declaration on Use in accordance with the International Standard for Exemptions on Therapeutic Use" on the list of substances prohibited by WADA (World Anti-Doping Agency) 2010. This requirement was relaxed in 2011, and the use of "Salbutamol (maximum 1600 micrograms within 24 hours) and Salmeterol taken by inhalation according to the manufacturer's recommended dosages and administration" was allowed.
According to two small and limited studies with the participation of 8 and 16 patients, respectively, it has been shown that salbutamol increases productivity even in patients who do not suffer from asthma.
However, another study contradicts this data. A double-blind, randomized trial involving 12 athletes without asthma showed that Salbutamol had no significant effect on endurance. Nevertheless, the study also showed that the bronchodilator action of the drug can improve respiratory adaptation at the beginning of the exercise.
Methods for detecting Salbutamol in the body
A quantitative measurement of Salbutamol in blood or plasma is possible, in order to confirm the diagnosis of poisoning in hospitalized patients or assist in forensic medical examination. Concentrations of salbutamol in urine are often measured in competitive sports programs, where a level of more than 1000 µg / l is considered an abuse. The detection window for urine testing is only about 24 hours, given the relatively short half-life of the drug.
The tertiary butyl group of Salbutamol (or Albuterol) makes the substance more selective for beta2 receptors. The drug is sold as a racemic mixture, mainly because the (S) -enantiomer blocks the metabolic pathways when the (R) -enantiomer shows its activity.
Synthesis of Salbutamol
Salbutamol can be produced from an acetophenone derivative, which is made from salicylic acid.
Analogues of Salbutamol
The drug is available under the brand names Ventolin, Ventoline, Ventilan, Aerolin or Ventorlin from GlaxoSmithKline; Asthalin and Asthavent from Cipla; Proventil from Schering-Plow, ProAir, Salamol or Airomir from Teva, AZMASOL from Beximco (Bangladesh), Ventosol from Ad-din Pharma and Asmol from Alphapharm.
Salbutamol is a beta-adrenomimetic with a predominant effect on beta2-adrenergic receptors. The drug is available in most pharmacies on the territory of the Russian Federation. The drug is released by prescription.