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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
º´¿ë±Ý±â :
°í½ÃµÈ º´¿ë±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
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| Mechanism of Action |
Maprotiline¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Maprotiline exerts its antidepressant action by inhibition of presynaptic uptake of catecholamines, thereby increasing their concentration at the synaptic clefts of the brain. In single doses, the effect of maprotiline on the EEG revealed a rise in the alpha-wave density, a reduction of the alpha-wave frequency and an increase in the alpha-wave amplitude. However, as with other tricyclic antidepressants, maprotiline lowers the convulsive threshold. Maprotiline acts as an antagonist at central presynaptic ¥á2 adrenergic inhibitory autoreceptors and hetero-receptors, an action that is postulated to result in an increase in central noradrenergic and serotonergic activity. Maprotiline is also a moderate peripheral ¥á1 adrenergic antagonist, which may explain the occasional orthostatic hypotension reported in association with its use. Maprotiline also inhibits the amine transporter, delaying the reuptake of noradrenaline and norepinephrine. Lastly, maprotiline is a strong inhibitor of the histamine H1 receptor, which explains its sedative actions.
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| Pharmacology |
Maprotiline¿¡ ´ëÇÑ Pharmacology Á¤º¸ Maprotiline is a tetracyclic antidepressant. Although its main therapeutic use is in the treatment of depression, it has also been shown to exert a sedative effect on the anxiety component that often accompanies depression. In one sleep study, it was shown that maprotiline increases the duration of the REM sleep phase in depressed patients, compared to imipramine which reduced the REM sleep phase. Maprotiline is a strong inhibitor of noradrenaline re-uptake in the brain and peripheral tissues, however it is worthy to note that it is a weak inhibitor of serotonergic uptake. In addition, it displays strong antihistaminic action (which may explain its sedative effects) as well as weak anticholinergic action. Maprotiline also has lower alpha adrenergic blocking activity than amitriptyline.
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| Protein Binding |
Maprotiline¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 88%
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| Half-life |
Maprotiline¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 27-58 hours
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| Absorption |
Maprotiline¿¡ ´ëÇÑ Absorption Á¤º¸ Completely absorbed following oral administration
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| Pharmacokinetics |
Maprotiline HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : ¼¼È÷ Èí¼öµÊ
- ´Ü¹é°áÇÕ : 88%
- ´ë»ç : °£¿¡¼ Ȱ¼ºÇü ¹× ºñȰ¼º ´ë»çü·Î ´ë»çµÊ
- ¹Ý°¨±â : 27-58 ½Ã°£ (Æò±Õ 43½Ã°£)
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 12½Ã°£ À̳»
- ¼Ò½Ç : ´¢ ¹è¼³(70%), ´ëº¯ ¹è¼³(30%)
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| Biotransformation |
Maprotiline¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. Maprotiline is metabolized by N-demethylation, deamination, aliphatic and aromatic hydroxylations and by formation of aromatic methoxy derivatives.
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| Toxicity |
Maprotiline¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=~900 mg/kg (Orally in rats); LD50=90 mg/kg (Orally in women); Signs of overdose include motor unrest, muscular twitching and rigidity, tremor, ataxia, convulsions, hyperpyrexia, vertigo, mydriasis, vomiting, cyanosis, hypotension, shock, tachycardia, cardiac arrhythmias, impaired cardiac conduction, respiratory depression, and disturbances of consciousness up to deep coma.
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| Drug Interactions |
Maprotiline¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Cisapride Increased risk of cardiotoxicity and arrhythmiasMesoridazine Increased risk of cardiotoxicity and arrhythmiasThioridazine Increased risk of cardiotoxicity and arrhythmiasDonepezil Possible antagonism of actionGalantamine Possible antagonism of actionRivastigmine Possible antagonism of actionPropranolol Propranolol increases the serum levels of cisapride
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Maprotiline¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals. Limit caffeine intake.
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| Drug Target |
[Drug Target]
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| Description |
Maprotiline¿¡ ´ëÇÑ Description Á¤º¸ A bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use. [PubChem]
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| Dosage Form |
Maprotiline¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
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| Drug Category |
Maprotiline¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic Uptake InhibitorsAntidepressantsAntidepressive Agents, Second-Generation
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| Smiles String Canonical |
Maprotiline¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CNCCCC12CCC(C3=CC=CC=C13)C1=CC=CC=C21
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| Smiles String Isomeric |
Maprotiline¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CNCCC[C@@]12CC[C@@H](C3=CC=CC=C13)C1=CC=CC=C21
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| InChI Identifier |
Maprotiline¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C20H23N/c1-21-14-6-12-20-13-11-15(16-7-2-4-9-18(16)20)17-8-3-5-10-19(17)20/h2-5,7-10,15,21H,6,11-14H2,1H3
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| Chemical IUPAC Name |
Maprotiline¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ N-Methyl-9,10-ethanoanthracene-9(10H)-propanamine
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| Drug-Induced Toxicity Related Proteins |
MAPROTILINE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:CYP2D6 Drug:Maprotiline Toxicity:Toxicity and inefficacy. [¹Ù·Î°¡±â]
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»ó¼¼Á¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×À» Åä´ë·Î ÀÛ¼ºµÇ¾úÀ¸¸ç ¿ä¾àÁ¤º¸´Â »ó¼¼Á¤º¸ ¹× ±âŸ¹®ÇåÀ» ±â¹ÝÀ¸·Î µå·°ÀÎÆ÷¿¡¼ ÆíÁýÇÑ ³»¿ëÀÔ´Ï´Ù. Á¦Ç°Çã°¡»çÇ×ÀÇ ¸ñÂ÷¿Í ´Ù¼Ò »óÀÌÇÒ ¼ö ÀÖ½À´Ï´Ù. |
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µå·°ÀÎÆ÷ ÀǾàÇмúÁ¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×, Çмú¹®Çå, Á¦¾àȸ»ç Á¦°øÁ¤º¸ µîÀ» ±Ù°Å·Î ÀÛ¼ºµÈ Âü°í Á¤º¸ÀÔ´Ï´Ù.
Á¤º¸ÀÇ Á¤È®¼ºÀ» À§ÇØ ³ë·ÂÇϰí ÀÖÀ¸³ª ÆíÁý»óÀÇ ¿À·ù, Çã°¡»çÇ× º¯°æ, Ãß°¡ÀûÀÎ Çмú¿¬±¸ ¶Ç´Â Àӻ󿬱¸ ¹ßÇ¥ µîÀ¸·Î ÀÎÇØ ¹ß»ýÇÏ´Â ¹®Á¦¿¡ ´ëÇØ µå·°ÀÎÆ÷´Â
Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù. ÀÚ¼¼ÇÑ ³»¿ëÀº ¡°Ã¥ÀÓÀÇ ÇÑ°è ¹× ¹ýÀû°íÁö¡±¸¦ ÂüÁ¶ÇØ ÁֽʽÿÀ.
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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