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| Related FDA Approved Drug |
±âÁØ ¼ººÐ: GUAIFENESINMUCINEX (GUAIFENESIN)
MUCINEX D (GUAIFENESIN; PSEUDOEPHEDRINE HYDROCHLORIDE)
MUCINEX DM (DEXTROMETHORPHAN HYDROBROMIDE; GUAIFENESIN)
±âÁØ ¼ººÐ: DEXTROMETHORPHAN HBR±âÁØ ¼ººÐ: D-CHLORPHENIRAMINE MALEATE
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| µ¶¼ºÁ¤º¸ |
Chlorpheniramine¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Dextromethorphan¿¡ ´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 |
Dextromethorphan¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Dextromethorphan is an opioid-like drug that binds to and acts as antagonist to the NMDA glutamatergic receptor, it is an agonist to the opioid sigma 1 and sigma 2 receptors, it is also an alpha3/beta4 nicotinic receptor antagonist and targets the serotonin reuptake pump. Dextromethorphan is rapidly absorbed from the gastrointestinal tract, where it enters the bloodstream and crosses the blood-brain barrier. The first-pass through the hepatic portal vein results in some of the drug being metabolized into an active metabolite of dextromethorphan, dextrorphan, the 3-hydroxy derivative of dextromethorphan.
Guaifenesin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Guaifenesin may act as an irritant to gastric vagal receptors, and recruit efferent parasympathetic reflexes that cause glandular exocytosis of a less viscous mucus mixture. Cough may be provoked. This combination may flush tenacious, congealed mucopurulent material from obstructed small airways and lead to a temporary improvement in dyspnea or the work of breathing.
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| Pharmacology |
Dextromethorphan¿¡ ´ëÇÑ Pharmacology Á¤º¸ Dextromethorphan suppresses the cough reflex by a direct action on the cough center in the medulla of the brain. Dextromethorphan shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist and acts as a non-competitive channel blocker. It is one of the widely used antitussives, and is also used to study the involvement of glutamate receptors in neurotoxicity.
Guaifenesin¿¡ ´ëÇÑ Pharmacology Á¤º¸ Guaifenesin is an expectorant which increases the output of phlegm (sputum) and bronchial secretions by reducing adhesiveness and surface tension. The increased flow of less viscous secretions promotes ciliary action and changes a dry, unproductive cough to one that is more productive and less frequent. By reducing the viscosity and adhesiveness of secretions, guaifenesin increases the efficacy of the mucociliary mechanism in removing accumulated secretions from the upper and lower airway.
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| Metabolism |
Dextromethorphan¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2D6 (CYP2D6)
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| Half-life |
Dextromethorphan¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 3-6 hours
Guaifenesin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 1 hour
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| Absorption |
Dextromethorphan¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly absorbed from the gastrointestinal tract.
Guaifenesin¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly absorbed from the GI tract
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| Pharmacokinetics |
GuaifenesinÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : À§Àå°üÀ¸·ÎºÎÅÍ Àß Èí¼öµÊ.
- ´ë»ç : 60%°¡ °£´ë»çµÊ.
- ¼Ò½Ç : ´ë»çü ¹× ¹Ìº¯Èü·Î ½Å¹è¼³µÊ.
D-chlorpheniramine maleateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ´Ü¹é°áÇÕ : 69-72%
- ´ë»ç : °£´ë»ç
- ¹Ý°¨±â : 20-24 ½Ã°£
- ¼Ò½Ç : ´ë»çü, ¾à¹°(3-4%)ÀÌ ½Å¹è¼³µÇ¸ç, 48½Ã°£³»¿¡ ÀüüÀÇ 35%°¡ ¼Ò½ÇµÈ´Ù.
Dextromethorphan HBrÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÁøÇØÀÛ¿ë ¹ßÇö½Ã°£ : 15~30ºÐ À̳»
- ÀÛ¿ëÁö¼Ó½Ã°£ : 6½Ã°£±îÁö
- ´ë»ç : °£´ë»ç
- ¼Ò½Ç : ÁÖ·Î ½Å¹è¼³
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| Biotransformation |
Dextromethorphan¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. Rapidly and extensively metabolized to dextrorphan (active metabolite). One well known metabolic catalyst involved is a specific cytochrome P450 enzyme known as 2D6, or CYP2D6.
Guaifenesin¿¡ ´ëÇÑ Biotransformation Á¤º¸ Rapidly hydrolyzed (60% within seven hours) and then excreted in the urine, with beta-(2-methoxyphenoxy)-lactic acid as its major urinary metabolite.
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| Toxicity |
Dextromethorphan¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
Guaifenesin¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50 1510 mg/kg (rat, oral)
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| Drug Interactions |
Dextromethorphan¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Dihydroquinidine barbiturate Quinidine increases the toxicity of dextromethorphanQuinidine Quinidine increases the toxicity of dextromethorphanQuinidine barbiturate Quinidine increases the toxicity of dextromethorphanFluoxetine Combination associated with possible serotoninergic syndromeIsocarboxazid Possible severe adverse reactionMemantine Increased risk of CNS adverse effectsMoclobemide Increased CNS toxicityParoxetine Combination associated with possible serotoninergic syndromePhenelzine Possible severe adverse reactionRasagiline Possible severe adverse reactionSelegiline Combination associated with possible serotoninergic syndromeSibutramine Combination associated with possible serotoninergic syndromeTerbinafine Terbinafine increases dextromethorphan levelsTranylcypromine Possible severe adverse reaction
Guaifenesin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Dextromethorphan¿¡ ´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 |
Guaifenesin¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with a full glass of water.Take without regard to meals.
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| Drug Target |
[Drug Target]
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| SNP Á¤º¸ |
Name:Dextromethorphan (DB00514)
Interacting Gene/Enzyme:Cytochrome P450 2D6 (Gene symbol = CYP2D6) Swissprot P10635
SNP(s):CYP2D6*6 rs5030655 (T deletion, homozygote)
Effect:Poor drug metabolizer, lower dose requirements
Reference(s):Bradford LD, Gaedigk A, Leeder JS: High frequency of CYP2D6 poor and "intermediate" metabolizers in black populations: a review and preliminary data. Psychopharmacol Bull. 1998;34(4):797-804. [PubMed]
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| Description |
Dextromethorphan¿¡ ´ëÇÑ Description Á¤º¸ The d-isomer of the codeine analog of levorphanol. Dextromethorphan shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (receptors, N-methyl-D-aspartate) and acts as a non-competitive channel blocker. It is one of the widely used antitussives, and is also used to study the involvement of glutamate receptors in neurotoxicity. [PubChem]
Guaifenesin¿¡ ´ëÇÑ Description Á¤º¸ An expectorant that also has some muscle relaxing action. It is used in many cough preparations. [PubChem]
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| Dosage Form |
Dextromethorphan¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule OralLiquid OralLozenge OralStrip OralSuspension OralSyrup OralTablet Oral
Guaifenesin¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid OralSyrup Oral
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| Drug Category |
Dextromethorphan¿¡ ´ëÇÑ Drug_Category Á¤º¸ Analgesics, OpioidAntitussive AgentsExcitatory Amino Acid Antagonists
Guaifenesin¿¡ ´ëÇÑ Drug_Category Á¤º¸ Expectorants
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| Smiles String Canonical |
Dextromethorphan¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=CC2=C(CC3C4CCCCC24CCN3C)C=C1
Guaifenesin¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=CC=CC=C1OCC(O)CO
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| Smiles String Isomeric |
Dextromethorphan¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=CC2=C(C[C@H]3[C@H]4CCCC[C@@]24CCN3C)C=C1
Guaifenesin¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=CC=CC=C1OC[C@H](O)CO
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| InChI Identifier |
Dextromethorphan¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C18H25NO/c1-19-10-9-18-8-4-3-5-15(18)17(19)11-13-6-7-14(20-2)12-16(13)18/h6-7,12,15,17H,3-5,8-11H2,1-2H3/t15-,17+,18-/m1/s1
Guaifenesin¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C10H14O4/c1-13-9-4-2-3-5-10(9)14-7-8(12)6-11/h2-5,8,11-12H,6-7H2,1H3
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| Chemical IUPAC Name |
Dextromethorphan¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ Not Available
Guaifenesin¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3-(2-methoxyphenoxy)propane-1,2-diol
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| Drug-Induced Toxicity Related Proteins |
MALEATE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Intercellular adhesion molecule 1 Drug:maleate Toxicity:hepatic injury. [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.
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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