Hexoprenaline

Hexoprenaline is a Sympathomimetic agent belonging to the Beta 2 Adrenergic Receptor Agonist Pharmacological class.

Hexoprenaline is approved as a Bronchodilator for the treatment of bronchial Asthma, and as well as the Tocolytic agent

The common side effects associated with Hexoprenaline are myocarditis, hypotension, severe renal disease, mitral valve defects, idiopathic hypertrophic subvalvular aortic stenosis, thyrotoxicosis, tachycardiac arrhythmias

Hexoprenaline belonging to the pharmacological class of Beta 2 Adrenergic Receptor Agonist, acts as an Anti-asthmatic/Bronchodilator therapeutic agent.

Hexoprenaline hence leads to Bronchodilation of the smooth muscles and reverses bronchospasm.

Hexoprenaline leads to an increased release of catecholamines .It also has alpha and beta-adrenergic properties. Hexoprenaline is said to have a shorter duration of action.

Hexoprenaline is available in tablet and intravenous formulations.

Tablet to be swallowed whole with water/liquid.

Parenteral to be given and administered intravenously.

Inhalation is to be administered with the help of a nebulizer.

Hexoprenaline can be used in the treatment of Asthma, Bronchodilation and Tocolysis.

Hexoprenaline can help to relax bronchial smooth muscle leading to Bronchodilation and improving the patient's respiration.

Hexoprenaline is approved for the following indications:

• Asthma
• Bronchodilation
• Tocolysis
• Acidosis
• Tachycardia

Dosage/Direction for Use

Oral Doses

While Relief in bronchoconstriction

Adult: 0.5-1 mg tid.

Intravenous Doses

In Premature labor

Adult: As sulfate: slow IV Inj of 10 mcg loading dose of hexoprenaline over 5-10 minutes, followed by an initial infusion rate of 0.3 mcg/minute. Prolonged infusion at 0.075 mcg/minute may be given if there is no cervical change.

Inhalation Doses

While Relief in bronchoconstriction

Adult: As sulfate: 100-200 mcg up to 6 times/day by aerosol inhalation. As HCl: 250-500 mcg every 4-6 hr by nebulisation; max: 3 mg/day for nebulization

10mcg, 100mcg, 250-5000mg, 0.5-1mg

Oral, Intravenous, Inhalation.

Hexoprenaline can be contraindicated in the following conditions as per the innovator:

• Angle-closure glaucoma
• Ischemic heart disease
• Hypertension
• Shock
• The first trimester of pregnancy
• Breastfeeding
• Placental abruption
• vaginal bleeding and endometritis
• Hyperthyroidism
• Cardiac arrhythmias, tachycardia
• Myocarditis, mitral valve disease, and aortic stenosis

The adverse effects of Hexoprenaline include the following:

• Myocarditis

• Hypotension

• Severe renal disease

• Mitral valve defects

• Idiopathic hypertrophic subvalvular aortic stenosis

• Thyrotoxicosis

• Tachycardiac arrhythmias

Clinically relevant drug interactions of Hexoprenaline are summarized here:

• Beta-blockers are found to reduce or neutralize the therapeutic effects of hexoprenaline
• Methylxanthines such as caffeine, theobromine, and theophylline, increase the action of Hexoprenaline.
• General anesthetics such as halothane and adrenergic receptor agonists may increase the risk of cardiovascular side effects, such as arrhythmia with the concomitant use of Hexoprenaline
• Hexoprenaline is contraindicated for simultaneous use with monoamine oxidase inhibitors (MAOIs), ergot alkaloids, dihydrotachysterol, and tricyclic antidepressant (TCAs)

The common side of Hexoprenaline includes the following:

• Myocarditis
• Hypotension
• Severe renal disease
• Mitral valve defects
• Idiopathic hypertrophic subvalvular aortic stenosis
• Thyrotoxicosis
• Tachycardiac arrhythmias

Pharmacodynamic :

In animals and humans, hexoprenaline has markedly longer action. Hexoprenaline is said to protect asthmatic patients against bronchoconstriction which is induced by histamine, acetylcholine, and other allergens. Hexoprenaline is most effective by inhalation, oral and intravenous routes, and is similar to salbutamol in onset and duration of action. Significant effects on the cardiovascular system have been observed after oral or inhaled doses whose levels are several folds greater than those required for significant bronchodilatation. Though a pronounced increase in heart rate occurs a few minutes after intravenous administration and a moderate increase in heart rate may occur after repeated oral dosage. Hexoprenaline has been given to asthmatic patients suffering from hypertension of all severity grades and to others with cardiac disease, by the oral, intravenous, and inhalation routes of administration without causing adverse cardiovascular effects. Hexoprenaline has a lipolytic and glycogenolytic effect. Hexoprenaline's inhibition of uterine activity, in the absence of significant cardiovascular effects, hexoprenaline may have therapeutic application in the suppression of labor contractions, at least by the intravenous route.

Pharmacokinetics

Studies with tritium-labeled hexoprenaline in rats have shown that it was rapidly absorbed after intratracheal or intramuscular administration, and was also absorbed from the intestine. Hexoprenaline undergoes only slow O-methylation. but The long duration of action of Hexoprenaline may also be due to the initial 3-O-methyl metabolite being an effective bronchodilator. Excretion mainly occurs through the urine in the form of sulfates and glucuronides of the mono- and di-3-O-methyl derivatives. Although unchanged hexoprenaline predominates initially.

• https://www.pharmacompass.com/chemistry-chemical-name/hexoprenaline
• https://www.tabletwise.net/medicine/hexoprenaline
• https://pubchem.ncbi.nlm.nih.gov/compound/Hexoprenaline#section=InChI-Key
• https://www.mims.com/india/drug/info/hexoprenaline?type=full&mtype=generic
• https://go.drugbank.com/drugs/DB08957
• https://drugs.ncats.io/drug/G9L6B3W684