Orciprenaline

• Metaproterenol
• IUPAC: (RS ) -1 - (3,5- dihydroxyphenyl )-2- isopropylaminoethanol
• Latin: Orciprenalinum

• 586-06-1
• 5874-97-5 ( sulfate 2:1)

• R03CB03
• R03AB03

White to off- white, crystalline, slightly hygroscopic powder

β -agonists

100 ° C.

Slightly soluble in water and ethanol, practically insoluble in dichloromethane

Attention

Hemisulfate salt

0.015 mg · m-3

3370 mg · kg -1 ( LD50, rat, oral)

Template: Infobox chemical / molecular formula search available

Orciprenaline is a β -sympathomimetic, so a drug. It is chiral and is used as a racemate. Orciprenaline is approved only for the treatment of acute asthma attacks. It can increase the heart rate strong. It acts similar to the adrenaline, without, however, leading to a so pronounced increase in blood pressure. Orciprenaline is used as an emergency medicine at a very slow heart rate (bradycardia ) in medicine and veterinary medicine ( off- label use ). The trade name for orciprenaline in Germany is Alupent.

Dosage form

There used orciprenaline tablets, meanwhile, is only the intravenous administration available. 1 ml vial containing 0.5 mg Orciprenalinsulfat. There is also a concentrate for infusion vial. This contains 5 mg Orciprenalinsulfat in 10 ml, so that this concentrate may be given only diluted by syringe pump.

Onset and duration

• Onset of action under 1 min
• Duration: 2-5 min

Effect

Orciprenaline is a sympathomimetic on B1 and B2 -adrenoceptor -adrenoceptor.

• It leads to a bronchodilation
• It has a positive inotropic, positive chronotropic, positive dromotropic, whereby the cardiac output is increased.
• It can lead to vasodilation.

Applications

Orciprenaline is approved only for the treatment of acute asthma attacks, in this context, but rarely used as effective means such as reproterol are available.

In cardiology and emergency medicine orciprenaline is usually in an emergency - outside of the admission as an off -label use - used in bradycardic arrhythmias in order to bridge the time until the final pacemaker therapy. It is also used as an antidote ( antidote ) in relative and absolute overdose of beta-blockers.

Contraindications

For the following diseases orciprenaline must not be used or only with great caution:

• Severe hyperthyroidism
• Hypertrophic obstructive cardiomyopathy
• Pheochromocytoma
• Angle-closure glaucoma
• Recent heart attack
• Severity of coronary artery disease
• Simultaneous administration of diuretics and digitalis
• Tachycardic arrhythmia
• Myocarditis
• Mitral
• WPW syndrome
• Hypokalemia

Side effects

Under orciprenaline the heartbeat can be greatly increased, extrasystoles are possible. Whether vasodilation with fall in blood pressure or blood pressure increase occurs by increasing the heart rate, in a particular case can not be predicted and monitored by blood pressure measurement. In extreme cases, ventricular fibrillation, or angina pectoris may occur. Furthermore, allergic skin reactions (itching, rash, redness, edema ) are possible. On the muscles now and then a fine tremor occurs. Also psychological effects such as restlessness have been reported. At high doses, the blood sugar may increase; few show nausea, anxiety and sleep disorders.

Interactions

All other sympathomimetic and beta -mimetic antiasthmatic agents are amplified by orciprenaline in their effect and their side effects. With simultaneous use of diuretics and glycosides can be propagated premature beats and other heart rhythm disturbances.