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Orciprenaline-also known as metaproterenol

Orciprenaline (INN), also known as metaproterenol (USAN), is a bronchodilator used in the treatment of asthma. More

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Description

Orciprenaline (INN), also known as metaproterenol (USAN), is a bronchodilator used in the treatment of asthma.

Generic Name

Orciprenaline-also known as metaproterenol

Chemical names

Metaproterenol; Alupent; Metaprel; Metaproterenol sulfate

Brand names

Alupent

IUPAC name

5-{1-hydroxy-2-[(propan-2-yl)amino]ethyl}benzene-1,3-diol

Pharmacokinetics

Actions

It is a synthetic amine, 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 ATP (adenosine triphosphate) to c-AMP (cyclic- 3',5'- adenosine monophosphate). 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.

Dosage/Dosage form

20 mg 3-4 times a day as oral route, single dose as inhalation.

Therapeutic uses

For the treatment of bronchospasm, chronic bronchitis, asthma, and emphysema.

Adverse effects/Side effects

Paradoxical bronchospasm, tachycardia, increased serum glucose, tremor, headache, increased potassium levels, palpitation, dizziness, insomnia, nausea, nervousness, vomiting, bad taste, heartburn, xerostomia, trembling, muscle cramps, weakness, coughing, pharyngitis, increased diaphoresis, hypertension, chest pain, angina, drowsiness, diarrhoea, taste change.

Interaction

  • Increased risk of malignant arrhythmias with halothane.
  • Effects may be antagonised by β-blockers e.g. propranolol.
  • Increased adverse effects with MAOIs, TCAs, sympathomimetics.
  • Duration of bronchodilation may be increased with inhaled ipratropium. 

Contraindications

Contraindicated in patients with hypersensitivity, fast heart beat and abnormal heart rhythm. 

Storage

Store at 15-25°C. 

Information

Molecular weight

211.2576

Molecular formula

C11H17NO3

CAS number

586-06-1

Precautions

CV disease, DM, glaucoma, hyperthyroidism, hypokalaemia, seizure disorders. Pregnancy and lactation.