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Overview
| Generic Names: | Metaproterenol; Metaproterenol Sulfate; Orciprenalina [INN-Spanish]; Orciprenaline Sulfate; Orciprenalinum [INN-Latin] |
|---|---|
| Trade Names: | Alotec; Alupent; Metaprel; Metaproterenol Polistirex; Novasmasol; Prometa |
| PharmGKB Accession Id: | PA450390 |
Description
A beta-adrenergic agonist used in the treatment of asthma and bronchospasms. PubChem (source: Drug Bank)
Indication
For the treatment of bronchospasm, chronic bronchitis, asthma, and emphysema. (source: Drug Bank)
ATC Therapeutic Categories
- R03AB:Non-selective beta-adrenoreceptor agonists
- R03CB:Non-selective beta-adrenoreceptor agonists
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Orciprenaline is a moderately selective beta(2)-adrenergic agonist that stimulates receptors of the smooth muscle in the lungs, uterus, and vasculature supplying skeletal muscle, with minimal or no effect on alpha-adrenergic receptors. Intracellularly, the actions of orciprenaline are mediated by cAMP, the production of which is augmented by beta stimulation. The drug is believed to work by activating adenylate cyclase, the enzyme responsible for producing the cellular mediator cAMP. (source: Drug Bank)
Pharmacology
Orciprenaline (also known as metaproterenol), a synthetic amine, is structurally and pharmacologically similar to isoproterenol. Orciprenaline is used exclusively as a bronchodilator. The pharmacologic effects of beta adrenergic agonist drugs, such as orciprenaline, are at least in part attributable to stimulation through beta adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic- 3',5'- adenosine monophosphate (c-AMP). Increased c-AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. (source: Drug Bank)
Food Interactions
Avoid high doses of caffeine.
Take without regard to meals.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic and gastric. The major metabolite, orciprenaline-3-0-sulfate, is produced in the gastrointestinal tract. Orciprenaline is not metabolized by catechol-0-methyltransferase nor have glucuronide conjugates been isolated to date. (source: Drug Bank)
Absorption
3% (oral bioavailability of 40%) (source: Drug Bank)
Toxicity
Symptoms of overdose include angina, hypertension or hypotension, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise and insomnia. LD<sub>50</sub>=42 mg/kg (orally in rat). (source: Drug Bank)
Isomeric SMILES Code:
CC(C)NC[C@@H](C1=CC(=CC(=C1)O)O)O (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
ADRB2 |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| ADRB2 |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| acebutolol |
|
Antagonism (source: Drug Bank) |
| amitriptyline |
|
The tricyclic increases the sympathomimetic effect (source: Drug Bank) |
| amoxapine |
|
The tricyclic increases the sympathomimetic effect (source: Drug Bank) |
| atenolol |
|
Antagonism (source: Drug Bank) |
| betaxolol |
|
Antagonism (source: Drug Bank) |
| bisoprolol |
|
Antagonism (source: Drug Bank) |
| carvedilol |
|
Antagonism (source: Drug Bank) |
| clomipramine |
|
The tricyclic increases the sympathomimetic effect (source: Drug Bank) |
| desipramine |
|
The tricyclic increases the sympathomimetic effect (source: Drug Bank) |
| doxepin |
|
The tricyclic increases the sympathomimetic effect (source: Drug Bank) |
| esmolol |
|
Antagonism (source: Drug Bank) |
| imipramine |
|
The tricyclic increases the sympathomimetic effect (source: Drug Bank) |
| isocarboxazid |
|
Increased arterial pressure (source: Drug Bank) |
| l-methyldopa |
|
Increased arterial pressure (source: Drug Bank) |
| linezolid |
|
Possible increase of arterial pressure (source: Drug Bank) |
| metoprolol |
|
Antagonism (source: Drug Bank) |
| moclobemide |
|
Moclobemide increases the sympathomimetic effect (source: Drug Bank) |
| nadolol |
|
Antagonism (source: Drug Bank) |
| nortriptyline |
|
The tricyclic increases the sympathomimetic effect (source: Drug Bank) |
| oxprenolol |
|
Antagonism (source: Drug Bank) |
| pargyline |
|
Increased arterial pressure (source: Drug Bank) |
| phenelzine |
|
Increased arterial pressure (source: Drug Bank) |
| pindolol |
|
Antagonism (source: Drug Bank) |
| propranolol |
|
Antagonism (source: Drug Bank) |
| protriptyline |
|
The tricyclic increases the sympathomimetic effect (source: Drug Bank) |
| reserpine |
|
Increased arterial pressure (source: Drug Bank) |
| sotalol |
|
Antagonism (source: Drug Bank) |
| timolol |
|
Antagonism (source: Drug Bank) |
| tranylcypromine |
|
Increased arterial pressure (source: Drug Bank) |
| trimipramine |
|
The tricyclic increases the sympathomimetic effect (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
Asthma |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.