orciprenaline

medtigo

orciprenaline

Brand Name :

Metaprel

Synonyms :

orciprenaline, metaproterenol, orciprenalina

Class :

Action and Spectrum

Mechanism of action

orciprenaline, or metaproterenol, is a beta-adrenergic receptor agonist that primarily acts on beta-2 adrenergic receptors. Its mechanism of action involves binding to these receptors and stimulating the production of cyclic adenosine monophosphate (cAMP), which leads to the relaxation of smooth muscles, particularly in the airways

As a result, orciprenaline is mainly used as a bronchodilator for managing reversible airway obstruction in conditions such as asthma, chronic obstructive pulmonary disease (COPD), and bronchitis. It may also be used to prevent exercise-induced bronchospasm

In addition to its bronchodilator effects, orciprenaline has some beta-1 adrenergic receptor activity, which can increase heart rate and cardiac output. This activity is less significant than its beta-2 receptor activity, and orciprenaline is not typically used for its cardiac effects

Spectrum

The spectrum of orciprenaline activity primarily focuses on its ability to relax smooth muscles in the airways and improve breathing in individuals with obstructive airway diseases

Dosing & Uses

Drug Interaction

Adverse Reaction

Frequency defined:

>10%

Nervousness (5-20%)

Tachycardia (6-17%)

Tremor (2-17%)

1-10%

Headache (4%)

Palpitation (4%)

Dizziness (1-4%)

Weakness (1%)

Exacerbation of asthma (2%)

Increased Diaphoresis (4%)

Heartburn (4%)

Pharyngitis (4%)

Insomnia (2%)

Nausea (1-4%)

<1%

Hypertension

Syncope

Chest pain

Weakness

Spasms

Black Box Warning

Contraindication / Caution

Contraindications

Allergy: Individuals with a known allergy or hypersensitivity to orciprenaline or its ingredients should not use this medication.
Cardiac arrhythmias: orciprenaline can increase heart rate and may exacerbate cardiac arrhythmias, such as tachycardia or atrial fibrillation. Therefore, it is generally contraindicated in individuals with significant cardiac arrhythmias
Hypertension: orciprenaline can cause an increase in blood pressure and should be used with caution in individuals with hypertension or uncontrolled high blood pressure
Diabetes: orciprenaline can mask symptoms of hypoglycemia (low blood sugar) in individuals with diabetes. Therefore, it should be used with caution in individuals with diabetes
Severe liver or kidney disease: orciprenaline is metabolized by the liver and excreted by the kidneys and may accumulate in individuals with severe liver or kidney disease. Therefore, it should be used cautiously and at lower doses in these individuals.

Caution

Cardiovascular disease: orciprenaline can increase heart rate and exacerbate cardiovascular conditions such as angina, myocardial infarction, or heart failure.
Hyperthyroidism: Orciprenaline can worsen symptoms of hyperthyroidism, a condition where the thyroid gland produces too much thyroid hormone.
Seizure disorders: orciprenaline can lower the seizure threshold and increase the risk of seizures in individuals with seizure disorders.
Other medications: orciprenaline can interact with other medications, such as beta-blockers and monoamine oxidase inhibitors (MAOIs), and may cause adverse effects or reduce the effectiveness of these medications.
Glaucoma: orciprenaline can increase intraocular pressure and may worsen symptoms of glaucoma. Therefore, it should be used with caution in individuals with glaucoma
Elderly patients: orciprenaline should be used with caution in elderly patients, as they may be more sensitive to its effects

Pregnancy / Lactation

Pregnancy consideration: may decrease the contraction of the uterus if used during childbirth; Observed tachycardia in the mother and foetus

Lactation: Excretion of the drug in human breast milk is known

Pregnancy category:

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology

The primary pharmacological effects of orciprenaline are bronchodilation and increased airflow in the lungs due to its action on the beta-2 receptors in the smooth muscle of the bronchial tree. This makes it helpful in managing reversible airway obstruction in conditions such as asthma and chronic obstructive pulmonary disease (COPD)

Pharmacodynamics

orciprenaline, a synthetic amine known as metaproterenol, resembles isoproterenol structurally and pharmacologically. The only application of orciprenaline is as a bronchodilator. The intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3′,5′-adenosine monophosphate, is stimulated through beta-adrenergic receptors, which is at least partially responsible for the pharmacological effects of beta-adrenergic agonist drugs like orciprenaline (c-AMP). Bronchial smooth muscles relax when cAMP levels rise, and the release of inflammatory mediators from mast cells that contribute to the development of acute hypersensitivity is inhibited

Pharmacokinetics

Absorption

the onset of action of orciprenaline for bronchodilation is typically around 30 minutes following oral administration, with a peak effect at around 1 hour and a duration of 2 to 6 hours regardless of the route of administration. It is well absorbed orally.

Distribution

It is distributed to various tissues, including the lungs, heart, and skeletal muscle, where it exerts its pharmacological effects. It has a moderate volume of distribution and low protein binding, which allows it to diffuse into tissues readily

Metabolism

It is primarily metabolized in the liver by various cytochrome P450 enzymes, including CYP1A2, CYP2D6, and CYP3A4, as well as by other enzymes such as catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO). The major metabolites of orciprenaline are 3-O-methyl metaproterenol (also known as terbutaline) and 3,4-dihydroxy metaproterenol

Elimination/Excretion

The metabolites of orciprenaline are eliminated primarily in the urine, with a small amount being eliminated in the feces. The elimination half-life of orciprenaline is approximately 3 hours, regardless of the route of administration

Adminstartion

Administration

Give without thinking about food. If Gastrointestinal discomfort happens, you might give it with meals

Patient Information Leaflet

Patient information leaflet

Generic Name: orciprenaline

Why do we use orciprenaline?

A beta-2 adrenergic agonist called orciprenaline is used to treat COPD, asthma, and bronchospasm

orciprenaline

No data available for drug.

DRUG INTERACTION

orciprenaline

&

orciprenaline +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

orciprenaline

No data available for drug.

DRUG INTERACTION

orciprenaline

&

orciprenaline +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

medtigo

orciprenaline

Brand Name :

Synonyms :

Class :

Action and Spectrum

Dosing & Uses

Drug Interaction

Adverse Reaction

Black Box Warning

Contraindication / Caution

Pregnancy / Lactation

Pharmacology

Adminstartion

Patient Information Leaflet

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