Alupent - General Information
A beta-adrenergic agonist used in the treatment of asthma and bronchospasms.
Pharmacology of Alupent
Alupent (also known as metaproterenol), a synthetic amine, is structurally and pharmacologically similar to isoproterenol. Alupent 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.
Alupent for patients
Patient's Instructions for Use Alupent
(metaproterenol sulfate USP) Inhalation Aerosol
- Insert metal canister into clear end of mouthpiece.
- Remove protective cap, invert canister and shake well before each use.
- Avoid spraying in eyes.
- Enclose mouthpiece with the lips. The base of the canister should be held vertically. The Alupent canister is to be used only with the white Alupent Inhalation Aerosol mouthpiece. This mouthpiece should not be used with other aerosol medications.
- Exhale deeply, then inhale slowly through the mouth and at the same time firmly press once on the upended canister base; continue to inhale deeply. Hold your breath for a few seconds and then remove the mouthpiece from the mouth and exhale slowly. One inhalation is often enough to obtain relief. The inhalation can be repeated once or twice, if necessary, or as your physician directs. Wait at least two minutes before repeating the inhalation. In most cases, the dose should not be repeated more often than every 3 to 4 hours. No more than 12 inhalations should be taken in one day.
- Replace protective cap after use.
Do not exceed the dose prescribed by your physician. If difficulty in breathing persists, contact your physician immediately.
Note: When full, the container holds enough medication for at least 200 inhalations: at least 100 inhalations are in the sample unit. Check regularly, by shaking the cylinder or container, to determine whether it contains any medication. When it first seems empty, there are still about ten doses left. Refill containers for the plastic mouthpiece are available when prescribed by your physician.
Keep the mouthpiece clean. Wash with hot water. If soap is used, rinse thoroughly with plain water.
Never open the container holding the medication. Opening it is dangerous and renders the contents useless.
Caution: Contents Under Pressure. Do not puncture or incinerate container. Do not expose to heat or store at temperatures above 120 oF. Keep out of reach of small children
Note: The indented statement below is required by the Federal government's Clean Air Act for all products containing or manufactured with chlorofluorocarbons (CFCs): This product contains trichloromonofluoromethane (CFC-11), dichlorodifluoromethane (CFC-12) and dichlorotetrafluoroethane (CFC-114), substances which harm the environment by destroying ozone in the upper atmosphere.
Your physician has determined that this product is likely to help your personal health. USE THIS PRODUCT AS DIRECTED, UNLESS INSTRUCTED TO DO OTHERWISE BY YOUR PHYSICIAN. If you have any questions about alternatives, consult with your physician.
Other beta adrenergic aerosol bronchodilators should not be used concomitantly with Alupent (metaproterenol sulfate USP) because they may have additive effects. Beta adrenergic agonists should be administered with caution to patients being treated with monoamine oxidase inhibitors or tricyclic antidepressants, since the action of beta adrenergic agonists on the vascular system may be potentiated.
Use in patients with cardiac arrhythmias associated with tachycardia is contraindicated.
Although rare, immediate hypersensitivity reactions can occur. Therefore, Alupent (metaproterenol sulfate USP) Inhalation Aerosol is contraindicated in patients with a history of hypersensitivity to any of its components.
Additional information about Alupent
Alupent Indication: For the treatment of bronchospasm, chronic bronchitis, asthma, and emphysema.
Mechanism Of Action: Alupent 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.
Drug Interactions: Acebutolol Antagonism
Trimipramine The tricyclic increases the sympathomimetic effect
Protriptyline The tricyclic increases the sympathomimetic effect
Amitriptyline The tricyclic increases the sympathomimetic effect
Nortriptyline The tricyclic increases the sympathomimetic effect
Moclobemide Moclobemide increases the sympathomimetic effect
Imipramine The tricyclic increases the sympathomimetic effect
Doxepin The tricyclic increases the sympathomimetic effect
Desipramine The tricyclic increases the sympathomimetic effect
Clomipramine The tricyclic increases the sympathomimetic effect
Amoxapine The tricyclic increases the sympathomimetic effect
Alseroxylon Increased arterial pressure
Deserpidine Increased arterial pressure
Isocarboxazid Increased arterial pressure
Linezolid Possible increase of arterial pressure
Methyldopa Increased arterial pressure
Midodrine Increased arterial pressure
Pargyline Increased arterial pressure
Phenelzine Increased arterial pressure
Rasagiline Increased arterial pressure
Reserpine Increased arterial pressure
Tranylcypromine Increased arterial pressure
Food Interactions: Not Available
Generic Name: Orciprenaline
Synonyms: Metaproterenol Sulfate; Orciprenalina [Inn-Spanish]; Orciprenalinum [Inn-Latin]; Metaproterenol; Orciprenaline Sulfate
Drug Category: Tocolytic Agents; Bronchodilator Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Orciprenaline: Alotec; Alupent; Metaprel; Metaproterenol Polistirex; Novasmasol; Prometa;
Absorption: 3% (oral bioavailability of 40%)
Toxicity (Overdose): Symptoms of overdose include angina, hypertension or hypotension, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise and insomnia. LD50=42 mg/kg (orally in rat).
Protein Binding: Not Available
Biotransformation: Hepatic and gastric. The major metabolite, orciprenaline-3-0-sulfate, is produced in the gastrointestinal tract. Orciprenaline is not metabolized by catechol-0-methyltransferase nor have glucuronide conjugates been isolated to date.
Half Life: 6 hours
Dosage Forms of Alupent: Syrup Oral
Chemical IUPAC Name: 5-[1-hydroxy-2-(propan-2-ylamino)ethyl]benzene-1,3-diol
Chemical Formula: C11H17NO3
Orciprenaline on Wikipedia: http://en.wikipedia.org/wiki/Orciprenaline
Organisms Affected: Humans and other mammals