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20200710 |
Pseudoephedrine : ÀӺο¡ ´ëÇÑ ¾ÈÀü¼º ¹ÌÈ®¸³./Guaifenesin: - |
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1) ¾î¸°ÀÌÀÇ ¼ÕÀÌ ´êÁö ¾Ê´Â °÷¿¡ º¸°üÇÒ °Í.
2) Á÷»çÀϱ¤À» ÇÇÇÏ°í µÉ ¼ö ÀÖÀ¸¸é ½À±â°¡ Àû°í ¼´ÃÇÑ °÷¿¡ ¹ÐÀüÇÏ¿© º¸°üÇÒ °Í.
3) ÀǾàǰÀ» ¿ø·¡ ¿ë±â¿¡¼ ²¨³»¾î ´Ù¸¥ ¿ë±â¿¡ º¸°üÇÏ´Â °ÍÀº ÀǾàǰ ¿À¿ë¿¡ ÀÇÇÑ »ç°í ¹ß»ýÀ̳ª ÀǾàǰ ǰÁú ÀúÇÏÀÇ ¿øÀÎÀÌ µÉ ¼ö ÀÖÀ¸¹Ç·Î ¿ø·¡ÀÇ ¿ë±â¿¡ º¸°üÇÒ °Í. |
| Related FDA Approved Drug |
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º´¿ë±Ý±â :
[rasagiline mesylate (as rasagiline)]
[selegiline hydrochloride]
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Dextromethorphan¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Ephedrine¿¡ ´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.
Pseudoephedrine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Pseudoephedrine acts directly on both alpha- and, to a lesser degree, beta-adrenergic receptors. Through direct action on alpha-adrenergic receptors in the mucosa of the respiratory tract, pseudoephedrine produces vasoconstriction. Pseudoephedrine relaxes bronchial smooth muscle by stimulating beta2-adrenergic receptors. Like ephedrine, pseudoephedrine releasing norepinephrine from its storage sites, an indirect effect.
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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.
Pseudoephedrine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Pseudoephedrine is a sympathomimetic agent, structurally similar to ephedrine, used to relieve nasal and sinus congestion and reduce air-travel-related otalgia in adults. The salts pseudoephedrine hydrochloride and pseudoephedrine sulfate are found in many over-the-counter preparations either as single-ingredient preparations, or more commonly in combination with antihistamines and/or paracetamol/ibuprofen. Unlike antihistamines, which modify the systemic histamine-mediated allergic response, pseudoephedrine only serves to relieve nasal congestion commonly associated with colds or allergies. The advantage of oral pseudoephedrine over topical nasal preparations, such as oxymetazoline, is that it does not cause rebound congestion (rhinitis medicamentosa).
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| Metabolism |
Dextromethorphan¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2D6 (CYP2D6)
Pseudoephedrine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Monoamine oxidase type A (MAO-A)
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| Protein Binding |
Pseudoephedrine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Pseudoephedrine does not bind to human plasma proteins over the concentration range of 50 to 2000 ng/mL
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| Half-life |
Dextromethorphan¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 3-6 hours
Guaifenesin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 1 hour
Pseudoephedrine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 9-16 hours
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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
Pseudoephedrine¿¡ ´ëÇÑ Absorption Á¤º¸ Pseudoephedrine is readily and almost completely absorbed from the GI tract and there is no evidence of first-pass metabolism.
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| Pharmacokinetics |
Pseudoephedrine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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- ´ë»ç : °£¿¡¼ ÀϺΠ´ë»ç
- ¹Ý°¨±â : 9-16 ½Ã°£
- ¼Ò½Ç : Åõ¿©·®ÀÇ 70-90%°¡ ¹Ìº¯Èü·Î, 1-6%°¡ norpseudoephedrineÀ¸·Î ¼Òº¯À¸·Î ¹è¼³µÊ. ½Å¹è¼³Àº ´¢ pH¿Í ´¢·®¿¡ ÀÇÇØ º¯ÈµÇ¸ç ¾ËÄ®¸®´¢´Â pseudoephedrineÀÇ ½Å¹è¼³À» °¨¼Ò½ÃÅ´.
Dextromethorphan HBrÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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GuaifenesinÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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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.
Pseudoephedrine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic.
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| Toxicity |
Dextromethorphan¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
Guaifenesin¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50 1510 mg/kg (rat, oral)
Pseudoephedrine¿¡ ´ëÇÑ Toxicity Á¤º¸ Common adverse reactions include nervousness, restlessness, and insomnia. Rare adverse reactions include difficult/painful urination, dizziness/lightheadedness, heart palpitations, headache, increased sweating, nausea/vomiting, trembling, troubled breathing, unusual paleness, and weakness.
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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
Pseudoephedrine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Alseroxylon Increased arterial pressureIsocarboxazid Increased arterial pressureLinezolid Possible increase of arterial pressureMethyldopa Increased arterial pressureBromocriptine The sympathomimetic increases the toxicity of bromocriptineTranylcypromine Increased arterial pressureMidodrine Increased arterial pressureMoclobemide Moclobemide increases the sympathomimetic effectPargyline Increased arterial pressurePhenelzine Increased arterial pressureRasagiline Increased arterial pressureReserpine Increased arterial pressureTrimipramine The tricyclic increases the sympathomimetic effectProtriptyline The tricyclic increases the sympathomimetic effectNortriptyline The tricyclic increases the sympathomimetic effectAmitriptyline The tricyclic increases the sympathomimetic effectAmoxapine The tricyclic increases the sympathomimetic effectClomipramine The tricyclic increases the sympathomimetic effectImipramine The tricyclic increases the sympathomimetic effectDesipramine The tricyclic increases the sympathomimetic effectDoxepin The tricyclic increases the sympathomimetic effectDeserpidine Increased arterial pressureGuanethidine The agent decreases the effect of guanethidine
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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.
Pseudoephedrine¿¡ ´ëÇÑ Food Interaction Á¤º¸ 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]
Pseudoephedrine¿¡ ´ëÇÑ Description Á¤º¸ An alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used in the treatment of several disorders including asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists. [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
Pseudoephedrine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid OralSyrup OralTablet OralTablet, extended release 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
Pseudoephedrine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic AgentsBronchodilator AgentsCentral Nervous System AgentsNasal DecongestantsSympathomimeticsVasoconstrictor Agents
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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
Pseudoephedrine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CNC(C)C(O)C1=CC=CC=C1
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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
Pseudoephedrine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN[C@@H](C)[C@@H](O)C1=CC=CC=C1
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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
Pseudoephedrine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C10H15NO/c1-8(11-2)10(12)9-6-4-3-5-7-9/h3-8,10-12H,1-2H3/t8-,10+/m0/s1
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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
Pseudoephedrine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (1S,2S)-2-methylamino-1-phenylpropan-1-ol
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