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[Drugbank ÀÇ ¼ººÐÁ¤º¸¿¶÷] [Doxylamine]
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| Brandname Á¤º¸ |
Doxylamine
Brand Names/Synonyms
- Decapryn
- Dossilamina [DCIT]
- Doxilminio [INN-Spanish]
- Doxylamine Succinate
- Doxylaminum [INN-Latin]
- Unisom
Brand Name Mixtures
- Diclectin (Doxylamine Succinate + Pyridoxine Hydrochloride)
- Extra Strength Tylenol Sinus Nighttime Caplet (Acetaminophen + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
- Mercodol with Decapryn (Doxylamine Succinate + Etafedrin Hydrochloride + Hydrocodone Bitartrate + Sodium Citrate)
- Neocitran Cold & Flu Syrup (Acetaminophen + Dextromethorphan Hydrobromide + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
- Night Relief Cold and Flu Liquid Capsules (Acetaminophen + Dextromethorphan Hydrobromide + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
- Nighttime Cold and Flu Liquid Capsules (Acetaminophen + Dextromethorphan Hydrobromide + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
- Nighttime Cold and Flu Relief (Acetaminophen + Dextromethorphan Hydrobromide + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
- Nighttime Liquid Capsules Cold/Flu Medicine (Acetaminophen + Dextromethorphan Hydrobromide + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
- Nitetime Cold Medicine (Acetaminophen + Dextromethorphan Hydrobromide + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
- Nyquil Liquicaps (Acetaminophen + Dextromethorphan Hydrobromide + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
- Regular Strength Sinus Medication (Acetaminophen + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
- Sinus Medication (Acetaminophen + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
- Sinus Medication Night Tablets (Acetaminophen + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
- Tylenol Cold & Flu Nighttime (Acetaminophen + Dextromethorphan Hydrobromide + Doxylamine Succinate + Pseudoephedrine Hydrochloride)
Chemical IUPAC NameN,N-dimethyl-2-(1-phenyl-1-pyridin-2-yl-ethoxy)-ethanamine
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| º¸°ü»ó ÁÖÀÇ |
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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
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| µ¶¼ºÁ¤º¸ |
Doxylamine¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Ãâó: ±¹¸³µ¶¼º°úÇпø µ¶¼º¹°ÁúÁ¤º¸DB : http://www.nitr.go.kr/nitr/contents/m134200/view.do |
| Mechanism of Action |
Doxylamine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Like other antihistamines, doxylamine acts by competitively inhibiting histamine at H1 receptors. It also has substantial sedative and anticholinergic effects.
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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| Pharmacology |
Doxylamine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Doxylamine is an antihistamine commonly used as a sleep aid. This drug is also used to relieve symptoms of hay fever (allergic rhinitis), hives (rash or itching), and other allergic reactions. Doxylamine is a member of the ethanolamine class of antihistamines and has anti-allergy power far superior to virtually every other antihistamine on the market, with the exception of diphenhydramine (Benadryl). It is also the most powerful over-the-counter sedative available in the United States, and more sedating than many prescription hypnotics. In a study, it was found to be superior to even the barbiturate, phenobarbital for use as a sedative. Doxylamine is also a potent anticholinergic.
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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| Metabolism |
Doxylamine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
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| Protein Binding |
Doxylamine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available
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| Half-life |
Doxylamine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 10 hours
Orciprenaline¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 6 hours
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| Absorption |
Doxylamine¿¡ ´ëÇÑ Absorption Á¤º¸ Readily absorbed via the gastrointestinal tract.
Orciprenaline¿¡ ´ëÇÑ Absorption Á¤º¸ 3% (oral bioavailability of 40%)
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| Pharmacokinetics |
Bromhexine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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Doxylamine SuccinateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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Orciprenaline sulfateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- °æ±¸ Åõ¿©
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- ÃÖ°íÈ¿°ú ¹ßÇö½Ã°£ : 2-4½Ã°£
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- Èí¼ö : Æò±Õ 40%
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| Biotransformation |
Doxylamine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic.
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 |
Doxylamine¿¡ ´ëÇÑ Toxicity Á¤º¸ Signs of overdose include wheezing, tightness in the chest, fever, itching, bad cough, blue skin color, fits, swelling of face, lips, tongue, or throat.
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 |
Doxylamine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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 |
Doxylamine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
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 |
Doxylamine¿¡ ´ëÇÑ Description Á¤º¸ Histamine H1 antagonist with pronounced sedative properties. It is used in allergies and as an antitussive, antiemetic, and hypnotic. Doxylamine has also been administered in veterinary applications and was formerly used in parkinsonism. [PubChem]
Orciprenaline¿¡ ´ëÇÑ Description Á¤º¸ A beta-adrenergic agonist used in the treatment of asthma and bronchospasms. [PubChem]
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| Dosage Form |
Doxylamine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
Orciprenaline¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Syrup Oral
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| Drug Category |
Doxylamine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Allergic AgentsAntiemeticsAntitussive AgentsHistamine H1 AntagonistsHypnotics and Sedatives
Orciprenaline¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic beta-AgonistsBronchodilator AgentsSympathomimeticsTocolytic Agents
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| Smiles String Canonical |
Doxylamine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(C)CCOC(C)(C1=CC=CC=C1)C1=CC=CC=N1
Orciprenaline¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(C)NCC(O)C1=CC(O)=CC(O)=C1
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| Smiles String Isomeric |
Doxylamine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(C)CCO[C@](C)(C1=CC=CC=C1)C1=CC=CC=N1
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 |
Doxylamine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C17H22N2O/c1-17(20-14-13-19(2)3,15-9-5-4-6-10-15)16-11-7-8-12-18-16/h4-12H,13-14H2,1-3H3
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 |
Doxylamine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ N,N-dimethyl-2-(1-phenyl-1-pyridin-2-ylethoxy)ethanamine
Orciprenaline¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 5-[1-hydroxy-2-(propan-2-ylamino)ethyl]benzene-1,3-diol
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