Orciprenaline is a drug of the group of non-selective β2-agonists, used to treat bronchial asthma and asthmatic bronchitis . 10 - 40 times less active than isoprenaline . Does not form metabolites with β-blocking activity. It is currently limited in use due to many side effects.
| Orciprenaline | |
|---|---|
| orciprenalinum | |
| Chemical compound | |
| IUPAC | ( RS ) -5- [1-Hydroxy-2 - [(1-methylethyl) amino] ethyl] -1,3-benzenediol (as sulfate or resinate); racemic mixture of two optically active isomers |
| Gross formula | C 11 H 17 NO 3 |
| Cas | |
| PubChem | |
| Drugbank | |
| Classification | |
| Farmakol. Group | non-selective β2 agonists |
| ATX | , |
| ICD-10 | |
| Pharmacokinetics | |
| The half-life. | 4 - 6 hours |
| Dosage Forms | |
| arosol | |
| Route of administration | |
| inhalation | |
| Other names | |
| Alupent, Astmopent, Alotec, Alupent, Astor, Dosalupent, Metaproterenolsulfat, Novasmasol, Orciprenaline sulfate | |
Content
General Information
In chemical structure and pharmacological properties it is close to isadrine (the base of orciprenaline differs from isadrin in the arrangement of hydroxyl groups in the benzene nucleus).
The drug is a stimulant of b- adrenergic receptors of a mixed type, acts on b1 and b2-adrenergic receptors, but in comparison with isadrine, it acts more selectively on the b2-adrenergic receptors of the bronchi than the heart, to a lesser extent it causes tachycardia and a decrease in blood pressure. It has a longer bronchodilator effect than isadrine. After inhalation of orciprenaline (alupent, astmopent), the effect occurs after 10-15 minutes, reaches a maximum after 1 hour and lasts up to 4-5 hours.
The main indications for use are the same as for isadrin: bronchial asthma, chronic asthmatic bronchitis, pneumosclerosis, pulmonary emphysema, as well as disorders of atrioventricular conduction.
Orciprenaline is used in the form of inhalations and parenteral.
To stop and prevent attacks of bronchial asthma, a special aerosol inhaler is used, when a valve is pressed, a constant dose of the drug is sprayed, equal to 0.75 mg. Usually one inhalacin is enough; if necessary, do a second inhalation after 5 minutes. Before pressing the valve, the inhaler is turned upside down.
To stop attacks of bronchial asthma, you can also administer the drug intramuscularly or subcutaneously: for adults, 0.5-1 mg (1-2 ml of a 0.05% solution), sometimes intravenously: - 1 ml of a 0.05% solution (0.5 mg ) administered slowly (over 3 minutes).
With prolonged therapy, orciprenaline in the form of tablets (0.02 g per tablet) is prescribed for the prevention of bronchial asthma attacks: for adults, 1 / 2-1 tablet 3-4 times a day; children - 1 / 4-1 / 2 tablets 2-4 times a day. The effect when taken orally occurs usually after 1 hour and lasts 4-6 hours.
With atrioventricular blockade, the drug is used with caution, slowly injecting 0.5-1 ml of a 0.05% solution, either intramuscularly or subcutaneously, 1-2 ml; if necessary, the drug is administered by slow intravenous infusion.
For infusion, the contents of 1-2 ampoules are diluted in 10 ml of a 0.05% solution (5-10 mg in total) in 250 ml of a 5% glucose solution or isotonic sodium chloride solution and administered at a rate of 10-20 drops per minute.
For the prevention of seizures in Adams-Stokes-Morgagni syndrome , in case of absolute bradyarrhythmia and intoxication with digitalis preparations, they are prescribed 1 / 2-1 tablets (adults) 6-10 times a day inside, changing the dose and frequency of doses depending on the heart rhythm.
Orciprenaline is usually better tolerated than isadrine, however, side effects are possible with its use, the same as with isadrine . With intravenous administration, a decrease in blood pressure is possible.
Release form
Method of release: in aerosol inhalers containing 400 single doses (0.75 mg each) of the drug; 0.05% solution in ampoules of 1 and 10 ml (0.5 and 5 mg); tablets of 0.02 g.
Storage
Storage: List B.
Medical Practice
Orciprenaline, like isoprenaline , is currently limitedly used for the symptomatic treatment of atrioventricular block and severe bradycardia. For the treatment of bronchial asthma, these drugs are not used due to many side effects.