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ÄÚ¸®Åõ»ì½Ã·´ CORITUSSAL SYR.[Carbinoxamine Maleate , Dextromethorphan HBr , Phenylpropanolamine HCl]
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µå·°ÀÎÆ÷¿¡¼´Â ÀǾàǰ ÀÎÅÍ³Ý ÆÇ¸Å¸¦ ÇÏÁö ¾Ê½À´Ï´Ù. |
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ÀÌ¿ëÇÏ½Ç ¼ö ÀÖ½À´Ï´Ù.
À¯·áÁ¤º¸¸ñ·ÏÀº Àü¹®È¸¿øÀ¸·Î
·Î±×ÀÎ ÇϽøé È®ÀÎ °¡´ÉÇÕ´Ï´Ù.
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û±¸ÄÚµå(KDÄÚµå) ºñ±Þ¿©Á¡°ËÄÚµå »óÇÑ±Ý¾× |
[A13101271]
[º¸ÇèÄڵ忡 µû¸¥ ¾àǰ±âº»Á¤º¸ Á÷Á¢Á¶È¸]
\0 ¿ø/1ml(2005.06.01)(ÇöÀç¾à°¡)
\14 ¿ø/1ml(2000.07.01)(º¯°æÀü¾à°¡)
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[Áúº´ÄÚµåÁ¶È¸]
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1SYR |
| È¿´ÉÈ¿°ú |
[ÀûÀÀÁõ º° °Ë»ö]
±âħ, Ä๰, ÄÚ¸·Èû, Àçä±â
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| Related FDA Approved Drug |
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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
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| µ¶¼ºÁ¤º¸ |
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 |
Carbinoxamine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Carbinoxamine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Carbinoxamine's anticholinergic action appears to be due to a central antimuscarinic effect, which also may be responsible for its antiemetic effects, although the exact mechanism is unknown.
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.
Phenylpropanolamine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Phenylpropanolamine acts directly on alpha- and, to a lesser degree, beta-adrenergic receptors in the mucosa of the respiratory tract. Stimulation of alpha-adrenergic receptors produces vasoconstriction, reduces tissue hyperemia, edema, and nasal congestion, and increases nasal airway patency. PPA indirectly stimulates beta-receptors, producing tachycardia and a positive inotropic effect.
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| Pharmacology |
Carbinoxamine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Carbinoxamine is an antihistamine of the ethanolamine class. Ethanolamine antihistamines have significant antimuscarinic activity and produce marked sedation in most patients. In addition to the usual allergic symptoms, the drug also treats irritant cough and nausea, vomiting, and vertigo associated with motion sickness. It also is used commonly to treat drug-induced extrapyramidal symptoms as well as to treat mild cases of Parkinson's disease. Rather than preventing the release of histamine, as do cromolyn and nedocromil, carbinoxamine competes with free histamine for binding at HA-receptor sites. Carbinoxamine competitively antagonizes the effects of histamine on HA-receptors in the GI tract, uterus, large blood vessels, and bronchial muscle. Ethanolamine derivatives have greater anticholinergic activity than do other antihistamines, which probably accounts for the antidyskinetic action of carbinoxamine.
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.
Phenylpropanolamine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Phenylpropanolamine (PPA), a sympathomimetic agent structurally similar to pseudoephedrine, is used to treat nasal congestion. Phenylpropanolamine is found in appetite suppressant formulations and with guaifenesinin in cough-cold formulations. In 2000, the FDA requested that all drug companies discontinue marketing products containing phenylpropanolamine, due to an increased risk of hemorrhagic stroke in women who used phenylpropanolamine.
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| Metabolism |
Dextromethorphan¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2D6 (CYP2D6)
Phenylpropanolamine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Monoamine oxidase type A (MAO-A)
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| Protein Binding |
Phenylpropanolamine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available
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| Half-life |
Carbinoxamine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 10 to 20 hours
Dextromethorphan¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 3-6 hours
Phenylpropanolamine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2.1 to 3.4 hours.
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| Absorption |
Dextromethorphan¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly absorbed from the gastrointestinal tract.
Phenylpropanolamine¿¡ ´ëÇÑ Absorption Á¤º¸ Reduced bioavailability (about 38%) from gastrointestinal tract because of first pass metabolism by monoamine oxidase in the stomach and liver.
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| Pharmacokinetics |
Carbinoxamine MaleateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ëÁö¼Ó½Ã°£ : 3-6 ½Ã°£
- ¹Ý°¨±â : 10-20 ½Ã°£
Dextromethorphan HBrÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÁøÇØÀÛ¿ë ¹ßÇö½Ã°£ : 15~30ºÐ À̳»
- ÀÛ¿ëÁö¼Ó½Ã°£ : 6½Ã°£±îÁö
- ´ë»ç : °£´ë»ç
- ¼Ò½Ç : ÁÖ·Î ½Å¹è¼³
Phenylpropanolamine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : °æ±¸ : Àß Èí¼öµÊ
- »ýü³»ÀÌ¿ë·ü : °ÅÀÇ 100%
- ´ë»ç : °£¿¡¼ norephedrineÀ¸·Î ´ë»çµÊ
- ¹Ý°¨±â : 4.6-6.6 ½Ã°£
- ¼Ò½Ç : ÁÖ·Î ¹Ìº¯Èü·Î¼(80-90%) ´¢¸¦ ÅëÇØ ¹è¼³µÊ
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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.
Phenylpropanolamine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic
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| Toxicity |
Dextromethorphan¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
Phenylpropanolamine¿¡ ´ëÇÑ Toxicity Á¤º¸ May induce ventricular extrasystoles and short paroxysms of ventricular tachycardia, a sensation of fullness in the head and tingling of the extremities; LD50=1490mg/kg (orally in rat)
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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
Phenylpropanolamine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Acetophenazine Decreased anorexic effect, may increase psychotic symptomsChlorpromazine Decreased anorexic effect, may increase psychotic symptomsEthopropazine Decreased anorexic effect, may increase psychotic symptomsFluphenazine Decreased anorexic effect, may increase psychotic symptomsMethotrimeprazine Decreased anorexic effect, may increase psychotic symptomsGuanethidine The agent decreases the effect of guanethidineMesoridazine Decreased anorexic effect, may increase psychotic symptomsThioridazine Decreased anorexic effect, may increase psychotic symptomsMethdilazine Decreased anorexic effect, may increase psychotic symptomsTrimeprazine Decreased anorexic effect, may increase psychotic symptomsPropericiazine Decreased anorexic effect, may increase psychotic symptomsPerphenazine Decreased anorexic effect, may increase psychotic symptomsProchlorperazine Decreased anorexic effect, may increase psychotic symptomsPromazine Decreased anorexic effect, may increase psychotic symptomsPromethazine Decreased anorexic effect, may increase psychotic symptomsPropiomazine Decreased anorexic effect, may increase psychotic symptomsThiethylperazine Decreased anorexic effect, may increase psychotic symptomsTrifluoperazine Decreased anorexic effect, may increase psychotic symptomsTriflupromazine Decreased anorexic effect, may increase psychotic symptomsMoclobemide Moclobemide increases the sympathomimetic effectAmitriptyline The tricyclic increases the sympathomimetic effectAmoxapine The tricyclic increases the sympathomimetic effectBromocriptine The sympathomimetic increases the toxicity of bromocriptineClomipramine The tricyclic increases the sympathomimetic effectDesipramine The tricyclic increases the sympathomimetic effectDoxepin The tricyclic increases the sympathomimetic effectImipramine The tricyclic increases the sympathomimetic effectNortriptyline The tricyclic increases the sympathomimetic effectProtriptyline The tricyclic increases the sympathomimetic effectTrimipramine The tricyclic increases the sympathomimetic effectVenlafaxine Risk of serotoninergic syndromeFluvoxamine Risk of serotoninergic syndromeParoxetine Risk of serotoninergic syndromeFluoxetine Risk of serotoninergic syndromeAlseroxylon Increased arterial pressureDeserpidine Increased arterial pressureIsocarboxazid Increased arterial pressureLinezolid Possible increase of arterial pressureTranylcypromine Increased arterial pressureRasagiline Increased arterial pressureReserpine Increased arterial pressurePhenelzine Increased arterial pressurePargyline Increased arterial pressureMethyldopa Increased arterial pressureMidodrine Increased arterial pressure
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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 |
Phenylpropanolamine¿¡ ´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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| 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 |
Carbinoxamine¿¡ ´ëÇÑ Description Á¤º¸ Carbinoxamine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. In addition to the usual allergic symptoms, the drug also treats irritant cough and nausea, vomiting, and vertigo associated with motion sickness. Carbinoxamine's anticholinergic action appears to be due to a central antimuscarinic effect, which also may be responsible for its antiemetic effects, although the exact mechanism is unknown. It also is used commonly to treat drug-induced extrapyramidal symptoms as well as to treat mild cases of Parkinson's disease.
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]
Phenylpropanolamine¿¡ ´ëÇÑ Description Á¤º¸ Phenylpropanolamine has been withdrawn in Canada. In November 2000, the Food and Drug Administration (FDA) issued a public health advisory against the use of the drug.
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| Dosage Form |
Carbinoxamine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Solution / drops OralSyrup OralTablet OralTablet, extended release Oral
Dextromethorphan¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule OralLiquid OralLozenge OralStrip OralSuspension OralSyrup OralTablet Oral
Phenylpropanolamine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Not Available
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| Drug Category |
Carbinoxamine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antihistamines
Dextromethorphan¿¡ ´ëÇÑ Drug_Category Á¤º¸ Analgesics, OpioidAntitussive AgentsExcitatory Amino Acid Antagonists
Phenylpropanolamine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic alpha-AgonistsAppetite DepressantsNasal DecongestantsSympathomimetics
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| Smiles String Canonical |
Carbinoxamine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(C)CCOC(C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Dextromethorphan¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=CC2=C(CC3C4CCCCC24CCN3C)C=C1
Phenylpropanolamine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(N)C(O)C1=CC=CC=C1
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| Smiles String Isomeric |
Carbinoxamine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(C)CCO[C@@H](C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Dextromethorphan¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=CC2=C(C[C@H]3[C@H]4CCCC[C@@]24CCN3C)C=C1
Phenylpropanolamine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ C[C@@H](N)[C@@H](O)C1=CC=CC=C1
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| InChI Identifier |
Carbinoxamine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C16H19ClN2O/c1-19(2)11-12-20-16(15-5-3-4-10-18-15)13-6-8-14(17)9-7-13/h3-10,16H,11-12H2,1-2H3
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
Phenylpropanolamine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C9H13NO/c1-7(10)9(11)8-5-3-2-4-6-8/h2-7,9,11H,10H2,1H3/t7-,9-/m1/s1
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| Chemical IUPAC Name |
Carbinoxamine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-N,N-dimethylethanamine
Dextromethorphan¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ Not Available
Phenylpropanolamine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (1S,2R)-2-amino-1-phenylpropan-1-ol
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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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