Chlorpheniramine에 대한 Mechanism_Of_Action 정보 Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Dextromethorphan에 대한 Mechanism_Of_Action 정보 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. Guaifenesin에 대한 Mechanism_Of_Action 정보 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.
Pharmacology
Chlorpheniramine에 대한 Pharmacology 정보 In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Chlorpheniramine, is a histamine H1 antagonist (or more correctly, an inverse histamine agonist) of the alkylamine class. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies. Dextromethorphan에 대한 Pharmacology 정보 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. Guaifenesin에 대한 Pharmacology 정보 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.
Absorption
Chlorpheniramine에 대한 Absorption 정보 Well absorbed in the gastrointestinal tract. Dextromethorphan에 대한 Absorption 정보 Rapidly absorbed from the gastrointestinal tract. Guaifenesin에 대한 Absorption 정보 Rapidly absorbed from the GI tract
Pharmacokinetics
Chlorpheniramine Maleate의 약물동력학자료
단백결합 : 69-72%
대사 : 간대사
반감기 : 20-24 시간
소실 : 대사체, 약물(3-4%)이 신배설되며, 48시간내에 전체의 35%가 소실된다.
Dextromethorphan HBr의 약물동력학자료
진해작용 발현시간 : 15~30분 이내
작용지속시간 : 6시간까지
대사 : 간대사
소실 : 주로 신배설
Guaifenesin의 약물동력학자료
흡수 : 위장관으로부터 잘 흡수됨.
대사 : 60%가 간대사됨.
소실 : 대사체 및 미변화체로 신배설됨.
Toxicity
Chlorpheniramine에 대한 Toxicity 정보 LD50 = 306 mg/kg in humans, mild reproductive toxin to women of childbearing age. Dextromethorphan에 대한 Toxicity 정보 Not Available Guaifenesin에 대한 Toxicity 정보 LD50 1510 mg/kg (rat, oral)
Drug Interactions
Chlorpheniramine에 대한 Drug_Interactions 정보 Donepezil Possible antagonism of actionGalantamine Possible antagonism of actionRivastigmine Possible antagonism of actionEthotoin The antihistamine increases the effect of hydantoinFosphenytoin The antihistamine increases the effect of hydantoinMephenytoin The antihistamine increases the effect of hydantoinPhenytoin The antihistamine increases the effect of hydantoin Dextromethorphan에 대한 Drug_Interactions 정보 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 Guaifenesin에 대한 Drug_Interactions 정보 Not Available
CYP450 Drug Interaction
[CYP450 Table직접조회] Dextromethorphan에 대한 P450 table Chlorpheniramine에 대한 P450 table
Chlorpheniramine에 대한 Description 정보 A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than promethazine. [PubChem] Dextromethorphan에 대한 Description 정보 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] Guaifenesin에 대한 Description 정보 An expectorant that also has some muscle relaxing action. It is used in many cough preparations. [PubChem]
Dosage Form
Chlorpheniramine에 대한 Dosage_Form 정보 Syrup OralTablet OralTablet, extended release Oral Dextromethorphan에 대한 Dosage_Form 정보 Capsule OralLiquid OralLozenge OralStrip OralSuspension OralSyrup OralTablet Oral Guaifenesin에 대한 Dosage_Form 정보 Liquid OralSyrup Oral
Drug Category
Chlorpheniramine에 대한 Drug_Category 정보 Anti-Allergic AgentsAntihistaminesAntipruriticsHistamine H1 Antagonists Dextromethorphan에 대한 Drug_Category 정보 Analgesics, OpioidAntitussive AgentsExcitatory Amino Acid Antagonists Guaifenesin에 대한 Drug_Category 정보 Expectorants
Smiles String Canonical
Chlorpheniramine에 대한 Smiles_String_canonical 정보 CN(C)CCC(C1=CC=C(Cl)C=C1)C1=CC=CC=N1 Dextromethorphan에 대한 Smiles_String_canonical 정보 COC1=CC2=C(CC3C4CCCCC24CCN3C)C=C1 Guaifenesin에 대한 Smiles_String_canonical 정보 COC1=CC=CC=C1OCC(O)CO
Smiles String Isomeric
Chlorpheniramine에 대한 Smiles_String_isomeric 정보 CN(C)CC[C@H](C1=CC=C(Cl)C=C1)C1=CC=CC=N1 Dextromethorphan에 대한 Smiles_String_isomeric 정보 COC1=CC2=C(C[C@H]3[C@H]4CCCC[C@@]24CCN3C)C=C1 Guaifenesin에 대한 Smiles_String_isomeric 정보 COC1=CC=CC=C1OC[C@H](O)CO
InChI Identifier
Chlorpheniramine에 대한 InChI_Identifier 정보 InChI=1/C16H19ClN2/c1-19(2)12-10-15(16-5-3-4-11-18-16)13-6-8-14(17)9-7-13/h3-9,11,15H,10,12H2,1-2H3 Dextromethorphan에 대한 InChI_Identifier 정보 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 Guaifenesin에 대한 InChI_Identifier 정보 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
Chemical IUPAC Name
Chlorpheniramine에 대한 Chemical_IUPAC_Name 정보 3-(4-chlorophenyl)-N,N-dimethyl-3-pyridin-2-ylpropan-1-amine Dextromethorphan에 대한 Chemical_IUPAC_Name 정보 Not Available Guaifenesin에 대한 Chemical_IUPAC_Name 정보 3-(2-methoxyphenoxy)propane-1,2-diol
Drug-Induced Toxicity Related Proteins
MALEATE 의 Drug-Induced Toxicity Related Protein정보 Replated Protein:Intercellular adhesion molecule 1 Drug:maleate Toxicity:hepatic injury. [바로가기]
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최근정보수정일 2024-06-13
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