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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
º´¿ë±Ý±â :
[amiodarone hydrochloride]
[dronedarone]
[dronedarone]
[oxymetazoline hydrochloride]
[pimozide]
[selegiline hydrochloride]
[»óÈ£ÀÛ¿ë/º´¿ë±Ý±â°Ë»ö]
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| Mechanism of Action |
Imipramine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Imipramine works by inhibiting the re-uptake of the neurotransmitters norepinephrine and serotonin by nerve cells. It binds the Sodium-dependent serotonin transporter and Sodium-dependent noradrenaline transporter, preventing or reducing the reuptake of norepinephrine and serotonin by nerve cells. As norepinephrine and serotonin are used to stimulate the synapse, and depression has been linked to a lack of stimulation of the recipient neuron at a synapse, slowing the reuptake of these neurotransmitters allows them to remain in the synaptic gap longer than it normal, increasing the stimulation of the recipient neuron and relieving the symptoms of depression. However, it does not act primarily by stimulation of the central nervous system. The clinical effect is also hypothesized as being due to potentiation of adrenergic synapses by blocking uptake of norepinephrine at nerve endings.
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| Pharmacology |
Imipramine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Imipramine is a tricyclic antidepressant with general pharmacological properties similar to those of structurally related tricyclic antidepressant drugs such as amitriptyline and doxepin. A tertiary amine, imipramine inhibits the reuptake of serotonin more so than most secondary amine tricyclics, meaning that it blocks the reuptake of neurotransmitters serotonin and noradrenaline almost equally. It is also effective in migraine prophylaxis, but not in abortion of acute migraine attack.
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| Metabolism |
Imipramine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)Monoamine oxidase type A (MAO-A)Monoamine oxidase type B (MAO-B)Cytochrome P450 2C9 (CYP2C9)Cytochrome P450 2C19 (CYP2C19)UDP-glucuronosyltransferase 1-4 (UGT1A4)Cytochrome P450 2D6 (CYP2D6)
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| Protein Binding |
Imipramine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 89–95%
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| Half-life |
Imipramine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 11–25 hours
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| Absorption |
Imipramine¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly and well absorbed after oral administration
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| Biotransformation |
Imipramine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Exclusively hepatic. Imipramine is converted in the liver to desipramine and 2-hydroxydesipramine, both active metabolites.
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| Toxicity |
Imipramine¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral, rat LD50: 355 to 682 mg/kg. Toxic signs proceed progressively from depression, irregular respiration and ataxia to convulsions and death.
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| Drug Interactions |
Imipramine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Altretamine Risk of severe hypotensionAtazanavir Atazanavir increases the effect and toxicity of tricyclicsCarbamazepine The tricyclic increases the effect of carbamazepineCimetidine Cimetidine increases the effect of tricyclic agentCisapride Increased risk of cardiotoxicity and arrhythmiasGrepafloxacin Increased risk of cardiotoxicity and arrhythmiasMesoridazine Increased risk of cardiotoxicity and arrhythmiasSparfloxacin Increased risk of cardiotoxicity and arrhythmiasTerfenadine Increased risk of cardiotoxicity and arrhythmiasThioridazine Increased risk of cardiotoxicity and arrhythmiasTranylcypromine Possibility of severe adverse effectsRasagiline Possibility of severe adverse effectsPhenelzine Possibility of severe adverse effectsIsocarboxazid Possibility of severe adverse effectsClonidine The tricyclic decreases the effect of clonidineDihydroquinidine barbiturate Quinidine increases the effect of tricyclic agentQuinidine Quinidine increases the effect of tricyclic agentQuinidine barbiturate Quinidine increases the effect of tricyclic agentDobutamine The tricyclic increases the sympathomimetic effectDopamine The tricyclic increases the sympathomimetic effectEphedra The tricyclic increases the sympathomimetic effectEphedrine The tricyclic increases the sympathomimetic effectEpinephrine The tricyclic increases the sympathomimetic effectFenoterol The tricyclic increases the sympathomimetic effectGuanethidine The tricyclic decreases the effect of guanethidineIsoproterenol The tricyclic increases the sympathomimetic effectMephentermine The tricyclic increases the sympathomimetic effectTerbutaline The tricyclic increases the sympathomimetic effectTerbinafine Terbinafine increases the effect and toxicity of the tricyclicSalbutamol The tricyclic increases the sympathomimetic effectRitonavir Ritonavir increases the effect and toxicity of tricyclicsPseudoephedrine The tricyclic increases the sympathomimetic effectProcaterol The tricyclic increases the sympathomimetic effectPirbuterol The tricyclic increases the sympathomimetic effectPhenylpropanolamine The tricyclic increases the sympathomimetic effectPhenylephrine The tricyclic increases the sympathomimetic effectOrciprenaline The tricyclic increases the sympathomimetic effectNorepinephrine The tricyclic increases the sympathomimetic effectMethoxamine The tricyclic increases the sympathomimetic effectMetaraminol The tricyclic increases the sympathomimetic effectDonepezil Possible antagonism of actionDuloxetine Possible increase in the levels of this agent when used with duloxetineGalantamine Possible antagonism of actionFluoxetine Fluoxetine increases the effect and toxicity of tricyclicsFluvoxamine Fluvoxamine increases the effect and toxicity of tricyclicsRivastigmine Possible antagonism of actionFluconazole The imidazole increases the effect and toxicity of the tricyclicKetoconazole The imidazole increases the effect and toxicity of the tricyclicMoclobemide Possible severe adverse reaction with this combinationRifabutin The rifamycin decreases the effect of tricyclicsRifampin The rifamycin decreases the effect of tricyclicsSibutramine Increased risk of CNS adverse effects
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Imipramine¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 1A2
clozapine
cyclobenzaprine
**imipramine**
mexiletine
naproxen
riluzole
tacrine
theophylline
INHIBITORS
CYP 1A2
cimetidine
fluoroquinolones
fluvoxamine
ticlopidine
INDUCERS
CYP 1A2
tobacco
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| Food Interaction |
Imipramine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Take with food.Avoid excessive quantities of coffee or tea (Caffeine).Avoid St.John's Wort.Do not take fibers at the same time.
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| Drug Target |
[Drug Target]
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| SNP Á¤º¸ |
Name:Imipramine (DB00458)
Interacting Gene/Enzyme:Cytochrome P450 2D6 (Gene symbol = CYP2D6) Swissprot P10635
SNP(s):CYP2D6*4 rs3892097 (A Allele)
Effect:Poor drug metabolizer, lower dose requirements, higher risk for adverse side effects
Reference(s):Bijl MJ, Visser LE, Hofman A, Vulto AG, van Gelder T, Stricker BH, van Schaik RH: Influence of the CYP2D6*4 polymorphism on dose, switching and discontinuation of antidepressants. Br J Clin Pharmacol. 2008 Apr;65(4):558-64. Epub 2007 Dec 7. [PubMed]
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| Description |
Imipramine¿¡ ´ëÇÑ Description Á¤º¸ The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group. [PubChem]
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| Drug Category |
Imipramine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic Uptake InhibitorsAntidepressive Agents, TricyclicNorepinephrine-Reuptake Inhibitors
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| Smiles String Canonical |
Imipramine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(C)CCCN1C2=CC=CC=C2CCC2=CC=CC=C12
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| Smiles String Isomeric |
Imipramine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(C)CCCN1C2=CC=CC=C2CCC2=CC=CC=C12
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| InChI Identifier |
Imipramine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C19H24N2/c1-20(2)14-7-15-21-18-10-5-3-8-16(18)12-13-17-9-4-6-11-19(17)21/h3-6,8-11H,7,12-15H2,1-2H3
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| Chemical IUPAC Name |
Imipramine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3-(5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N-dimethylpropan-1-amine
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| Drug-Induced Toxicity Related Proteins |
IMIPRAMINE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Ornithine decarboxylase Drug:imipramine Toxicity:stimulated ornithine decarboxylase activity. [¹Ù·Î°¡±â] Replated Protein:S-adenosylmethionine decarboxylase proenzyme Drug:imipramine Toxicity:stimulated ornithine decarboxylase activity. [¹Ù·Î°¡±â] Replated Protein:Alpha-2A adrenergic receptor Drug:imipramine Toxicity:anxiety. [¹Ù·Î°¡±â] Replated Protein:Alpha-2A adrenergic receptor Drug:imipramine Toxicity:insensitive to the antidepressant effects. [¹Ù·Î°¡±â]
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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
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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