Veterinary Drug Handbook (VDH) is the reference veterinarians turn to when they want an independent source of information on the drugs that are used in veterinary medicine today.

ALBUTEROL SULFATE

Chemistry - A synthetic sympathomimetic amine, albuterol sulfate occurs as a white, almost tasteless crystalline powder. It is soluble in water and slightly soluble in alcohol. One mg of albuterol is equivalent to 1.2 mg of albuterol sulfate. Albuterol is also known as salbutamol.

Storage, Stability, Compatibility

Oral albuterol sulfate products should be stored at 2-30°C.
The capsules containing powder for inhalation should be left in the original packaging until just before use.

Pharmacology - ALBUTEROL SULFATE

Like other beta-agonists, albuterol is believed to act by stimulating production ofcyclic AMP through activation of adenyl cyclase. Albuterol is considered to be predominantly abeta2 agonist (relaxation of bronchial, uterine, and vascular smooth muscles). At usual doses, albuterol possesses minimal beta1 agonist (heart) activity. beta adrenergics can promote a shift ofpotassium away from the serum and into the cell, perhaps via stimulation of Na+-K+-ATPase.
Temporary decreases in either normal or high serum potassium levels are possible.

Uses, Indications

Albuterol is used principally in dogs and cats for its effects on bronchialsmooth muscle to alleviate bronchospasm or cough. It potentially could also be used in horses as abronchodilator.

Pharmacokinetics - ALBUTEROL SULFATE

The specific pharmacokinetics of this agent have apparently not been thoroughly studied in domestic animals. In general, albuterol is absorbed rapidly and well after oraladministration. Effects occur within 5 minutes after oral inhalation, and 30 minutes after oraladministration (e.g., tablets). It does not cross the blood-brain barrier, but does cross the placenta.
Duration of effect generally persists for 3-6 hours after inhalation and up to 12 hours (dependingon dosage form) after oral administration. The drug is extensively metabolized in the liver, principally to the inactive metabolite, albuterol 4'-O-sulfate. After oral administration, the serum half lifein humans has been reported as 2.7-5 hours.

Contraindications, Precautions, Reproductive Safety

Albuterol is contraindicated in patientshypersensitive to it. One veterinary school formulary (Schultz 1986) states that a related drug(terbutaline), is contraindicated in dogs and cats with heart disease, particularly when CHF or cardiomyopathy is present. It should be used with caution in patients with diabetes, hyperthyroidism, hypertension, seizure disorders, or cardiac disease (especially with concurrent arrhythmias).
In very large doses, albuterol is teratogenic in rodents. It should be used (particularly the oraldosage forms) during pregnancy only when the potential benefits outweigh the risks. Like someother beta agonists, it may delay pre-term labor after oral administration. It is unknown whether thedrug crosses into maternal milk.

Adverse Effects, Warnings

Most adverse effects are dose-related and are those that would beexpected with sympathomimetic agents including increased heart rate, tremors, CNS excitement(nervousness) and dizziness. These effects are generally transient and mild and usually do not require discontinuation of therapy. Decreased serum potassium values may be noted; rarely ispotassium supplementation required.
Overdosage, Acute Toxicity - Symptoms of significant overdose after systemic administrationmay include arrhythmias (bradycardia, tachycardia, heart block, extrasystoles), hypertension, fever, vomiting, mydriasis, and CNS stimulation. Hypokalemia may also be noted. If recently ingested(orally), and if the animal does not have significant cardiac or CNS effects, it should be handled likeother overdoses (empty gut, give activated charcoal and a cathartic). If cardiac arrhythmias requiretreatment, a beta-blocking agent (e.g., propranolol) can be used, but may precipitatebronchoconstriction. The oral LD50 in rats is reported to be greater than 2 g/kg. Contact a poisoncontrol center for further information.

Drug Interactions

Use of albuterol with other sympathomimetic amines may increase therisk of developing adverse cardiovascular effects. Beta-adrenergic blocking agents (e.g., propranolol) may antagonize the actions of albuterol. Tricyclic antidepressants or monoamineoxidase inhibitors may potentiate the vascular effects of albuterol. Use with inhalation anesthetics(e.g., halothane, isoflurane, methoxyflurane), may predispose the patient to ventricular arrhythmias, particularly in patients with preexisting cardiac disease¯use cautiously. Use withdigitalis glycosides may increase the risk of cardiac arrhythmias.
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