Espirol (Clenbuterol Hydrochloride)
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02 Details
Espirol
(Clenbuterol Hydrochloride)
Espirol 25mcg/tab 100 tabs
Clenbutérol, chlorhydrate de; Clenbuteroli hydrochloridum; Hidrocloruro de clenbuterol; Klenbuterol hydrochlorid; Klenbuterolhidroklorid; Klenbuterolhydroklorid; Klenbuterolihydrokloridi; Klenbuterolio hidrochloridas; NAB-365 (clenbuterol). 1-(4-Amino-3,5-dichlorophenyl)-2-tert-butylaminoethanol hydrochloride. Кленбутерола Гидрохлорид
C12H18Cl2N2O,HCl = 313.7.
CAS — 37148-27-9 (clenbuterol); 21898-19-1 (clenbuterol hydrochloride).
ATC — R03AC14; R03CC13.
ATC Vet — QR03AC14; QR03CC13. (clenbuterol)
Pharmacopoeias. In Chin.and Eur.(see p.vii). Ph. Eur. 6.2(Clenbuterol Hydrochloride). A white or almost white crystalline powder. Soluble in water and in alcohol; slightly soluble in acetone. A 5% solution in water has a pH of 5.0 to 7.0.
USP 31(Dyphylline). A white, odourless, amorphous or crystalline solid. Freely soluble in water; sparingly soluble in alcohol and in chloroform; practically insoluble in ether. A 1% solution in water has a pH of 5.0 to 7.5. Store in airtight containers.
Pharmacologic Category
Dosage Range
Adults:
Oral: 25-50 mcg twice daily
Inhalation: 25 mcg 3 times/day
Use
Bronchodilator in reversible airway obstruction due to asthma or COPD
Dosage Forms
Tablet, as hydrochloride: 25 mcg, 50 mcg
Storage/Stability
Store at room temperature of 15°C to 30°C (59°F to 86°F). Protect from light, heat, and excessive humidity.
Mechanism of Action
Clenbuterol hydrochloride is a direct-acting sympathomimetic with mainly beta-adrenergic activity and a selective action on beta2receptors (a beta2agonist). It has properties similar to those of salbutamol. It is used as a bronchodilator in the management of reversible airways obstruction, as in asthma and in certain patients with chronic obstructive pulmonary disease. A usual oral dose is 20 micrograms twice daily; doses of up to 40 micrograms twice daily have occasionally been given. Clenbuterol hydrochloride has also been given by inhalation. In patients with asthma, as-required beta agonist therapy is preferable to regular use. An increased need for, or decreased duration of effect of, clenbuterol indicates deterioration of asthma control and the need for review of therapy.
Abuse. Clenbuterol has been used illicitly in animal feeds in an attempt to promote weight gain and to increase muscle to lipid mass.
Pharmacodynamics/Kinetics
After oral administration, peak plasma levels of clenbuterol occur 2 hours after administration and the average half-life is about 10 – 13 hours. The duration of effect varies from 6 – 8 hours. After multiple oral doses, the drug’s volume of distribution is approximately 1.6 L/kg and clearance was 94 mL/kg/hr. Urinary concentrations of clenbuterol are approximately 100X those found in plasma and can persist at quantifiable levels for 288 hours (12 days) in urine after the last oral
Anatomic Therapeutic Chemical (ATC) Classification
- R03AC14
- R03CC13
Contraindications/Precautions/Warnings
The drug is contraindicated in food producing animals (legal ramifications). The label states that the drug should not be used in horses suspected of having cardio vascular impairment as tachycardia may occur.
Adverse Effects
Muscle tremors, sweating, restlessness, urticaria, and tachycardia may be noted, particularly early in the course of therapy. Creatine kinase elevations have been noted in some and, rarely, ataxia can occur. Clenbuterol is reported to induce abortion.
Clenbuterol has been touted in some body building circles as an alternative to anabolic steroids for muscle development and body fat reduction.
Pregnancy Risk Factor
X
Category X: Studies in animals or human beings have demonstrated fetal abnormalities, or there is evidence of fetal risk based on human experience, or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.
Pregnancy Considerations
Adverse events were observed in animal reproduction studies.
Lactation
Excretion in breast milk unknown/use caution
Breast-Feeding Considerations
It is not known if Clenbuterol is excreted into breast milk. Caution be used if administered to nursing women.
Overdosage/Acute Toxicity
Some case reports of clenbuterol overdoses have been reported in various species. In recent years, clenbuterol has been used as an adulterant in illicit heroin. Depending on dosage and species, emptying gut may be appropriate, otherwise supportive therapy and administration of parenteral beta-blockers to control heart rate and rhythm and elevated blood pressure may be considered. All of this should be done in a hospital.
Drug Interactions
The following drug interactions have either been reported or are theoretical in humans or animals receiving clenbuterol and may be of significance in patients:
Inhalation Anesthetics: Use with inhalation anesthetics (e.g., halothane, isoflurane, methoxyflurane), may predispose the patient to ventricular arrhythmias, particularly in pa tients with preexisting cardiac disease—use cautiously
Beta-blockers (e.g., propranolol): May antagonize clenbuterol’s effects.
Digoxin: Use with digitalis glycosides may increase the risk of cardiac arrhythmias
Dinoprost: Clenbuterol may antagonize the effects of dinoprost (prostaglandin F2alpha)
Oxytocin:Clenbuterol may antagonize the effects of oxytocin.
Sympathomimetics (e.g., terbutaline, albuterol): Concomitant administration with other sympathomimetic amines) may enhance the adverse effects of clenbuterol
Antidepressants: May potentiate the vascular effects of clenbuterol.
Patient Monitoring and Laboratory Tests
Monitor heart rate during treatment. Clenbuterol can be detected in urine for 12 days.
Local Anesthetic/Vasoconstrictor Precautions
No information available to require special precautions
Effects on Dental Treatment
No significant effects or complications reported
Effects on Bleeding
No information available to require special precautions