Metaproterenol/Orciprenaline; Indications, Dosage, Side effects, Interactions

Metaproterenol








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Metaproterenol Sulfate is the sulfate salt form of metaproterenol, a short-acting and selective sympathomimetic beta-receptor agonist with bronchodilator activity. Metaproterenol sulfate binds beta-2 adrenergic receptors in bronchial smooth muscle and stimulates intracellular adenyl cyclase, thereby increasing the production of cyclic adenosine monophosphate (cAMP). Increased cAMP levels cause relaxation of the bronchial smooth muscle, improve mucociliary clearance and reduce inflammatory cell mediator release, especially from mast cells.

or

Orciprenaline, also known as metaproterenol, is a bronchodilator used in the treatment of asthma. Orciprenaline is a moderately selective β2 adrenergic receptor agonist that stimulates receptors of the smooth muscle in the lungs, uterus, and vasculature supplying skeletal muscle, with minimal or no effect on α adrenergic receptors. The pharmacologic effects of β adrenergic agonist drugs, such as orciprenaline, are at least in part attributable to stimulation through β adrenergic receptors of intracellular adenylyl cyclase, the enzyme which catalyzes the conversion of ATP to cAMP.

Mechanism of Action of Metaproterenol/Orciprenaline

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.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.

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Indications of Metaproterenol/Orciprenaline

Contra-Indications of Metaproterenol/Orciprenaline

The dosage of Metaproterenol/Orciprenaline

Strengths: 0.65 mg/inh; 0.4%; 0.6%; 5%; 10 mg/5 mL; 10 mg; 20 mg

Asthma – Acute

  • Oral: 20 mg 3 to 4 times a day.
  • Inhalation aerosol: 2 to 3 inhalations every 3 to 4 hours, up to 12 inhalations/day.
  • Inhalation solution: 10 to 15 mg (0.2 to 0.3 mL of 5% solution) every 4 to 6 hours.

Asthma – Maintenance

  • Oral: 20 mg 3 to 4 times a day.
  • Inhalation aerosol: 2 to 3 inhalations every 3 to 4 hours, up to 12 inhalations/day.
  • Inhalation solution: 10 to 15 mg (0.2 to 0.3 mL of 5% solution) every 4 to 6 hours.

Chronic Obstructive Pulmonary Disease – Acute

  • Oral: 20 mg 3 to 4 times a day.
  • Inhalation aerosol: 2 to 3 inhalations every 3 to 4 hours, up to 12 inhalations/day.
  • Inhalation solution: 10 to 15 mg (0.2 to 0.3 mL of 5% solution) every 4 to 6 hours.

Chronic Obstructive Pulmonary Disease – Maintenance

  • Oral: 20 mg 3 to 4 times a day.
  • Inhalation aerosol: 2 to 3 inhalations every 3 to 4 hours, up to 12 inhalations/day.
  • Inhalation solution: 10 to 15 mg (0.2 to 0.3 mL of 5% solution) every 4 to 6 hours.

Pediatric Dose for Asthma 

  • Infants and children: Nebulizer: 0.5 to 1 mg/kg ( 0.01 to 0.02 mL/kg of 5% solution); minimum dose: 5 mg (0.1 mL); maximum dose: 15 mg (0.3 mL); every 4 to 6 hours.
  • Children less than 2 years of age: Oral: 0.4 mg/kg/dose in 3 to 4 divided doses a day. In infants, the dose can be given every 8 to 12 hours.
  • Children 2 to 6 years of age: Oral: 1.3 to 2.6 mg/kg/day divided every 6 to 8 hours.
  • Children 6 to 9 years of age: Oral: 10 mg 3 to 4 times a day.
  • Children more than 9 years of age: Oral: 20 mg 3 to 4 times a day.
  • Children more than 12 years of age: Inhalation aerosol: 2 to 3 inhalations every 3 to 4 hours, up to 12 inhalations in 24 hours.
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Side Effects of Metaproterenol/Orciprenaline

The most common

More common

Rare

Drug Interactions of Metaproterenol/Orciprenaline

Orciprenaline or  metaproterenol may interact with following drugs, supplement & may change the efficacy of drugs

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Pregnancy Catagory of Metaproterenol/Orciprenaline

Pregnancy Risk Catagory C

Pregnancy

Alupent (metaproterenol sulfate) has been shown to be teratogenic and embryotoxic in rabbits when given in doses corresponding to 640 times the maximum recommended dose. These effects included skeletal abnormalities, hydrocephalus and skull bone separation. Results of other studies in rabbits, rats or mice have not revealed any teratogenic, embryocidal or fetotoxic effects. There are no adequate and well-controlled studies in pregnant women. Alupent (metaproterenol sulfate) should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation

It is not known whether Alupent (metaproterenol sulfate) is excreted in human milk; therefore, Alupent (metaproterenol sulfate) should be used during nursing only if the potential benefit justifies the possible risk to the newborn.

References

 

Metaproterenol

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