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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.
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
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 pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।" data-rx-term="migraine" data-rx-definition="Migraine is a recurring headache disorder often with throbbing pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।">migraine headache;
- pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating; or
More common
- Abdominal or stomach pain, discomfort, or pain when an area is touched or pressed. সহজ বাংলা: চাপ দিলে ব্যথা।" data-rx-term="tenderness" data-rx-definition="Tenderness means pain when an area is touched or pressed. সহজ বাংলা: চাপ দিলে ব্যথা।">tenderness
- chills or fever
- difficulty with moving
- a headache, severe and throbbing
- joint or pain: Back pain means pain in the spine, muscles, discs, joints, or nerves of the back. সহজ বাংলা: পিঠ/কোমরের ব্যথা।" data-rx-term="back pain" data-rx-definition="Back pain means pain in the spine, muscles, discs, joints, or nerves of the back. সহজ বাংলা: পিঠ/কোমরের ব্যথা।">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)
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
