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Ephedrine¿¡ ´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 |
Loratadine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Like other H1-blockers, loratadine competes with free histamine for binding at H1-receptors in the GI tract, uterus, large blood vessels, and bronchial muscle. Loratadine also has a weak affinity for acetylcholine and alpha-adrenergic receptors.
Pseudoephedrine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Pseudoephedrine acts directly on both alpha- and, to a lesser degree, beta-adrenergic receptors. Through direct action on alpha-adrenergic receptors in the mucosa of the respiratory tract, pseudoephedrine produces vasoconstriction. Pseudoephedrine relaxes bronchial smooth muscle by stimulating beta2-adrenergic receptors. Like ephedrine, pseudoephedrine releasing norepinephrine from its storage sites, an indirect effect.
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| Pharmacology |
Loratadine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Loratadine, a non-sedating H1-blocker similar in structure to cyproheptadine and azatadine, is used to treat seasonal allergic rhinitis. Unlike other H1-blockers, loratidine does not penetrate the CNS effectively and has a low affinity for CNS H1-receptors.
Pseudoephedrine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Pseudoephedrine is a sympathomimetic agent, structurally similar to ephedrine, used to relieve nasal and sinus congestion and reduce air-travel-related otalgia in adults. The salts pseudoephedrine hydrochloride and pseudoephedrine sulfate are found in many over-the-counter preparations either as single-ingredient preparations, or more commonly in combination with antihistamines and/or paracetamol/ibuprofen. Unlike antihistamines, which modify the systemic histamine-mediated allergic response, pseudoephedrine only serves to relieve nasal congestion commonly associated with colds or allergies. The advantage of oral pseudoephedrine over topical nasal preparations, such as oxymetazoline, is that it does not cause rebound congestion (rhinitis medicamentosa).
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| Protein Binding |
Loratadine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available
Pseudoephedrine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Pseudoephedrine does not bind to human plasma proteins over the concentration range of 50 to 2000 ng/mL
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| Half-life |
Loratadine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 8.4 hours
Pseudoephedrine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 9-16 hours
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| Absorption |
Loratadine¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly absorbed following oral administration (40% bioavailability)
Pseudoephedrine¿¡ ´ëÇÑ Absorption Á¤º¸ Pseudoephedrine is readily and almost completely absorbed from the GI tract and there is no evidence of first-pass metabolism.
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| Pharmacokinetics |
LoratadineÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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- Èí¼ö : ½Å¼ÓÈ÷ Èí¼ö
- ´ë»ç : °£¿¡¼ Ȱ¼ºÇü ´ë»çü·Î ´ë»ç
- ¹Ý°¨±â : 12-15 ½Ã°£
- ¼Ò½Ç : À¯ÁóÀ¸·Îµµ »ó´ç·® ¹è¼³
Pseudoephedrine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ºñÃæÇ÷Á¦°Å È¿°úÀÇ ¹ßÇö½Ã°£ (°æ±¸Åõ¿©½Ã) : 15-30ºÐ
- ÀÛ¿ëÁö¼Ó½Ã°£ : 4-6 ½Ã°£ (¼¹æÇü Á¦Á¦´Â 12½Ã°£ Áö¼Ó)
- ´ë»ç : °£¿¡¼ ÀϺΠ´ë»ç
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- ¼Ò½Ç : Åõ¿©·®ÀÇ 70-90%°¡ ¹Ìº¯Èü·Î, 1-6%°¡ norpseudoephedrineÀ¸·Î ¼Òº¯À¸·Î ¹è¼³µÊ. ½Å¹è¼³Àº ´¢ pH¿Í ´¢·®¿¡ ÀÇÇØ º¯ÈµÇ¸ç ¾ËÄ®¸®´¢´Â pseudoephedrineÀÇ ½Å¹è¼³À» °¨¼Ò½ÃÅ´.
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| Biotransformation |
Loratadine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic
Pseudoephedrine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic.
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| Toxicity |
Loratadine¿¡ ´ëÇÑ Toxicity Á¤º¸ somnolence, tachycardia, and headache LD50=mg/kg (orally in rat)
Pseudoephedrine¿¡ ´ëÇÑ Toxicity Á¤º¸ Common adverse reactions include nervousness, restlessness, and insomnia. Rare adverse reactions include difficult/painful urination, dizziness/lightheadedness, heart palpitations, headache, increased sweating, nausea/vomiting, trembling, troubled breathing, unusual paleness, and weakness.
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| Drug Interactions |
Loratadine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Nefazodone Increased risk of cardiotoxicity
Pseudoephedrine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Alseroxylon Increased arterial pressureIsocarboxazid Increased arterial pressureLinezolid Possible increase of arterial pressureMethyldopa Increased arterial pressureBromocriptine The sympathomimetic increases the toxicity of bromocriptineTranylcypromine Increased arterial pressureMidodrine Increased arterial pressureMoclobemide Moclobemide increases the sympathomimetic effectPargyline Increased arterial pressurePhenelzine Increased arterial pressureRasagiline Increased arterial pressureReserpine Increased arterial pressureTrimipramine The tricyclic increases the sympathomimetic effectProtriptyline The tricyclic increases the sympathomimetic effectNortriptyline The tricyclic increases the sympathomimetic effectAmitriptyline The tricyclic increases the sympathomimetic effectAmoxapine The tricyclic increases the sympathomimetic effectClomipramine The tricyclic increases the sympathomimetic effectImipramine The tricyclic increases the sympathomimetic effectDesipramine The tricyclic increases the sympathomimetic effectDoxepin The tricyclic increases the sympathomimetic effectDeserpidine Increased arterial pressureGuanethidine The agent decreases the effect of guanethidine
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Drug Target |
[Drug Target]
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| Description |
Loratadine¿¡ ´ëÇÑ Description Á¤º¸ A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (histamine H1 antagonists) it lacks central nervous system depressing effects such as drowsiness. [PubChem]
Pseudoephedrine¿¡ ´ëÇÑ Description Á¤º¸ An alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used in the treatment of several disorders including asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists. [PubChem]
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| Dosage Form |
Loratadine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Syrup OralTablet Oral
Pseudoephedrine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid OralSyrup OralTablet OralTablet, extended release Oral
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| Drug Category |
Loratadine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Allergic AgentsAntihistaminesAntipruriticsHistamine H1 Antagonists, Non-Sedating
Pseudoephedrine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic AgentsBronchodilator AgentsCentral Nervous System AgentsNasal DecongestantsSympathomimeticsVasoconstrictor Agents
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| Smiles String Canonical |
Loratadine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCOC(=O)N1CCC(CC1)=C1C2=C(CCC3=C1N=CC=C3)C=C(Cl)C=C2
Pseudoephedrine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CNC(C)C(O)C1=CC=CC=C1
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| Smiles String Isomeric |
Loratadine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CCOC(=O)N1CC\C(CC1)=C1/C2=C(CCC3=C1N=CC=C3)C=C(Cl)C=C2
Pseudoephedrine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN[C@@H](C)[C@@H](O)C1=CC=CC=C1
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| InChI Identifier |
Loratadine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C22H23ClN2O2/c1-2-27-22(26)25-12-9-15(10-13-25)20-19-8-7-18(23)14-17(19)6-5-16-4-3-11-24-21(16)20/h3-4,7-8,11,14H,2,5-6,9-10,12-13H2,1H3
Pseudoephedrine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C10H15NO/c1-8(11-2)10(12)9-6-4-3-5-7-9/h3-8,10-12H,1-2H3/t8-,10+/m0/s1
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| Chemical IUPAC Name |
Loratadine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylic acid ethyl ester
Pseudoephedrine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (1S,2S)-2-methylamino-1-phenylpropan-1-ol
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