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

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.

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.

Indications of Metaproterenol/Orciprenaline

Asthma Bronchial
Bronchospasm
Chronic Bronchitis
Pulmonary Emphysema
Asthma, acute
Asthma, Maintenance
COPD, Acute
COPD, Maintenance
For the treatment of bronchospasm, chronic bronchitis, asthma, and emphysema.

Contra-Indications of Metaproterenol/Orciprenaline

Overactive thyroid gland
Diabetes
High blood pressure
Coronary artery disease
Disease of Inadequate Blood Flow to the Heart Muscle
Chronic heart failure
Seizures
Fast Heartbeat
Allergies to beta-Adrenergic Agents

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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.

Side Effects of Metaproterenol/Orciprenaline

The most common

nausea, diarrhea, upset stomach,
dry mouth
a sore throat
a cough
constipation
blurred vision or vision changes
pain with urination
stomach pain or cramping
a headache
dizziness
confusion
stomach pain;
back pain, joint or muscle pain.
problems with your vision (including color vision);
sudden chest pain or trouble breathing;
pain or swelling in one or both legs;
a migraine headache;
pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating; or

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More common

Abdominal or stomach pain, discomfort, or tenderness
chills or fever
difficulty with moving
a headache, severe and throbbing
joint or back pain
muscle aching or cramping
muscle pains or stiffness
chest pressure or squeezing pain in the chest
discomfort in arms, shoulders, neck or upper back
excessive sweating
feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
sudden tingling or coldness in an arm or leg
sudden slow or difficult speech
sudden drowsiness or need to sleep
fast breathing
sharp pain when taking a deep breath
fast or slow heartbeat
coughing up blood
rust colored urine
decreased amount of urine

Rare

Anxiety
change in vision
chest pain or tightness
confusion
a cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
extra heartbeats
fainting
hallucinations
headache
irritability
lightheadedness
mood or mental changes
muscle pain or cramps
muscle spasm or jerking of all extremities
nervousness

Drug Interactions of Metaproterenol/Orciprenaline

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

antihistamines (e.g,. cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
beta 2 agonists (e.g., salbutamol, formoterol, terbutaline)
beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
long-acting beta agonists (e.g., indacaterol, salmeterol)
citalopram
decongestant cold medications (e.g., phenylephrine, pseudoephedrine)
decongestant eye drops and nose sprays (e.g., naphazoline, oxymetazoline, xylometazoline)
diuretics (e.g., furosemide, hydrochlorthiazide)
domperidone
escitalopram
ipratropium
macrolide antibiotics (e.g., clarithromycin, erythromycin, telithromycin)
methadone
mirabegron
monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline, selegiline, tranylcypromine)
quinolone antibiotics (e.g., levofloxacin moxifloxacin ofloxacin)
serotonin antagonists (anti-emetic medications; e.g., ondansetron granisetron, )
theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
thiazide diuretics (water pills; e.g., hydrochlorothiazide, indapamide, metolazone)
tolterodine
topiramate
tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)

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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.