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Orciprenaline¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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.
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Orciprenaline¿¡ ´ëÇÑ Pharmacology Á¤º¸ Orciprenaline (also known as metaproterenol), a synthetic amine, is structurally and pharmacologically similar to isoproterenol. 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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Orciprenaline¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 6 hours
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Orciprenaline¿¡ ´ëÇÑ Absorption Á¤º¸ 3% (oral bioavailability of 40%)
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| Biotransformation |
Orciprenaline¿¡ ´ëÇÑ Biotransformation Á¤º¸ 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.
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| Toxicity |
Orciprenaline¿¡ ´ëÇÑ Toxicity Á¤º¸ 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).
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| Drug Interactions |
Orciprenaline¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Acebutolol AntagonismAtenolol AntagonismBetaxolol AntagonismBevantolol AntagonismBisoprolol AntagonismCarteolol AntagonismCarvedilol AntagonismEsmolol AntagonismLabetalol AntagonismMetoprolol AntagonismNadolol AntagonismOxprenolol AntagonismPenbutolol AntagonismPindolol AntagonismPractolol AntagonismTimolol AntagonismSotalol AntagonismPropranolol AntagonismTrimipramine The tricyclic increases the sympathomimetic effectProtriptyline The tricyclic increases the sympathomimetic effectAmitriptyline The tricyclic increases the sympathomimetic effectNortriptyline The tricyclic increases the sympathomimetic effectMoclobemide Moclobemide increases the sympathomimetic effectImipramine The tricyclic increases the sympathomimetic effectDoxepin The tricyclic increases the sympathomimetic effectDesipramine The tricyclic increases the sympathomimetic effectClomipramine The tricyclic increases the sympathomimetic effectAmoxapine The tricyclic increases the sympathomimetic effectAlseroxylon Increased arterial pressureDeserpidine Increased arterial pressureIsocarboxazid Increased arterial pressureLinezolid Possible increase of arterial pressureMethyldopa Increased arterial pressureMidodrine Increased arterial pressurePargyline Increased arterial pressurePhenelzine Increased arterial pressureRasagiline Increased arterial pressureReserpine Increased arterial pressureTranylcypromine Increased arterial pressure
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Orciprenaline¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.Avoid high doses of caffeine.
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| Drug Target |
[Drug Target]
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| Description |
Orciprenaline¿¡ ´ëÇÑ Description Á¤º¸ A beta-adrenergic agonist used in the treatment of asthma and bronchospasms. [PubChem]
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| Dosage Form |
Orciprenaline¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Syrup Oral
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| Drug Category |
Orciprenaline¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic beta-AgonistsBronchodilator AgentsSympathomimeticsTocolytic Agents
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| Smiles String Canonical |
Orciprenaline¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(C)NCC(O)C1=CC(O)=CC(O)=C1
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| Smiles String Isomeric |
Orciprenaline¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(C)NC[C@H](O)C1=CC(O)=CC(O)=C1
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| InChI Identifier |
Orciprenaline¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C11H17NO3/c1-7(2)12-6-11(15)8-3-9(13)5-10(14)4-8/h3-5,7,11-15H,6H2,1-2H3
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| Chemical IUPAC Name |
Orciprenaline¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 5-[1-hydroxy-2-(propan-2-ylamino)ethyl]benzene-1,3-diol
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