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12 ¼¼ ÀÌÇÏ |
20170086 |
2017-11-06 |
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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
º´¿ë±Ý±â :
°í½ÃµÈ º´¿ë±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
[»óÈ£ÀÛ¿ë/º´¿ë±Ý±â°Ë»ö]
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Codeine¿¡ ´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 |
Codeine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Codeine's analgesic activity is, most likely, due to its conversion to morphine. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
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| Pharmacology |
Codeine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Codeine, an opiate agonist in the CNS, is similar to other phenanthrene derivatives such as morphine. Codeine, in combination with guaifenesin or iodinated glycerol, is used as a cough suppressant and, as a single agent or in combination with acetaminophen or other products, is used for pain control and as an antidiarrheal agent.
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| Metabolism |
Codeine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2D6 (CYP2D6)
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| Protein Binding |
Codeine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 7-25%
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| Half-life |
Codeine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2-4 hours
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| Absorption |
Codeine¿¡ ´ëÇÑ Absorption Á¤º¸ Well absorbed following oral administration with a bioavailability of approximately 90%.
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| Pharmacokinetics |
Codeine phosphateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ë¹ßÇö½Ã°£
- °æ±¸ : 0.5-1 ½Ã°£
- ±ÙÀ°ÁÖ»ç : 10-30 ºÐ
- ÃÖ´ëÈ¿°ú ¹ßÇö½Ã°£
- °æ±¸ : 1-1.5 ½Ã°£
- ±ÙÀ°ÁÖ»ç : 0.5-1 ½Ã°£
- ÀÛ¿ëÁö¼Ó½Ã°£ : 4-6 ½Ã°£
- Èí¼ö : °æ±¸ : ÀûÀýÈ÷ Èí¼öµÊ.
- ºÐÆ÷ : ÅÂ¹Ý Åë°ú, À¯Áó ºÐÆ÷
- ´Ü¹é°áÇÕ : 7%
- ´ë»ç : °£¿¡¼ morphine(Ȱ¼ºÇü)À¸·Î ´ë»ç
- ¹Ý°¨±â : 2.5-3.5 ½Ã°£
- ¼Ò½Ç : 3-16%°¡ ¹Ìº¯Èü, norcodeine, À¯¸®Çü ¹× Æ÷ÇÕÇü morphineÀ¸·Î¼ ´¢¸¦ ÅëÇØ ¹è¼³µÊ.
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| Biotransformation |
Codeine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. Codeine is a prodrug, itself inactive, but demethylated to the active morphine by the liver enzyme CYP2D6.
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| Toxicity |
Codeine¿¡ ´ëÇÑ Toxicity Á¤º¸ Respiratory depression, sedation and miosis and common symptoms of overdose. Other symptoms include nausea, vomiting, skeletal muscle flaccidity, bradycardia, hypotension, and cool, clammy skin. Apnea and death may ensue.
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| Drug Interactions |
Codeine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Cimetidine Cimetidine increases the effect of the narcoticDihydroquinidine barbiturate Quinidine decreases the analgesic effect of codeineNaltrexone Naltrexone may precipitate a withdrawal syndrome in opioid-dependent individualQuinidine Quinidine decreases the analgesic effect of codeineQuinidine barbiturate Quinidine decreases the analgesic effect of codeine
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Codeine¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 2D6
Beta Blockers:
S-metoprolol
propafenone
timolol
Antidepressants:
amitriptyline
clomipramine
desipramine
imipramine
paroxetine
Antipsychotics:
haloperidol
risperidone
thioridazine
aripiprazole
**codeine**
dextromethorphan
duloxetine
flecainide
mexiletine
ondansetron
tamoxifen
tramadol
venlafaxine
INHIBITORS
CYP 2D6
amiodarone
buproprion
chlorpheniramine
cimetidine
clomipramine
duloxetine
fluoxetine
haloperidol
methadone
mibefradil
paroxetine
quinidine
ritonavir
INDUCERS
CYP 2D6
N/A
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| Food Interaction |
Codeine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Take with food, food reduces irritation.To avoid constipation: increase your daily intake of fiber (beans, whole grains, vegetables).
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| Drug Target |
[Drug Target]
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| SNP Á¤º¸ |
Name:Codeine (DB00318)
Interacting Gene/Enzyme:Cytochrome P450 2D6 (Gene symbol = CYP2D6) Swissprot P10635
SNP(s):CYP2D6*5 (Deletion, homozygote)
Effect:Poor drug metabolizer, lower dose requirements
Reference(s):Desmeules J, Gascon MP, Dayer P, Magistris M: Impact of environmental and genetic factors on codeine analgesia. Eur J Clin Pharmacol. 1991;41(1):23-6. [PubMed]
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| Description |
Codeine¿¡ ´ëÇÑ Description Á¤º¸ An opioid analgesic related to morphine but with less potent analgesic properties and mild sedative effects. It also acts centrally to suppress cough. [PubChem]
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| Drug Category |
Codeine¿¡ ´ëÇÑ Drug_Category Á¤º¸ AnalgesicsAnalgesics, OpioidAntitussive AgentsAntitussivesNarcoticsOpiate Agonists
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| Smiles String Canonical |
Codeine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=C2OC3C(O)C=CC4C5CC(C=C1)=C2C34CCN5C
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| Smiles String Isomeric |
Codeine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=C2O[C@H]3[C@@H](O)C=C[C@H]4[C@H]5CC(C=C1)=C2[C@@]34CCN5C
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| InChI Identifier |
Codeine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C18H21NO3/c1-19-8-7-18-11-4-5-13(20)17(18)22-16-14(21-2)6-3-10(15(16)18)9-12(11)19/h3-6,11-13,17,20H,7-9H2,1-2H3/t11-,12+,13-,17-,18-/m0/s1
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| Chemical IUPAC Name |
Codeine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (5(,6()-7,8-didehydro-4,5-epoxy-3-methoxy-17-methylmorphinan-6-ol
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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.
¹Ýµå½Ã Á¦Á¶¡¤¼öÀÔ»ç, ÆÇ¸Å»ç, ÀÇ»ç, ¾à»ç¿¡°Ô ÃÖÁ¾ÀûÀ¸·Î È®ÀÎÇϽñ⠹ٶø´Ï´Ù.
ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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