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20180088 |
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Codeine¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Ephedrine¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
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| Mechanism of Action |
Caffeine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Caffeine stimulates medullary, vagal, vasomotor, and respiratory centers, promoting bradycardia, vasoconstriction, and increased respiratory rate. This action was previously believed to be due primarily to increased intracellular cyclic 3¡Ç,5¡Ç-adenosine monophosphate (cyclic AMP) following inhibition of phosphodiesterase, the enzyme that degrades cyclic AMP. It is now thought that xanthines such as caffeine act as agonists at adenosine-receptors within the plasma membrane of virtually every cell. As adenosine acts as an autocoid, inhibiting the release of neurotransmitters from presynaptic sites but augmenting the actions of norepinephrine or angiotensin, antagonism of adenosine receptors promotes neurotransmitter release. This explains the stimulatory effects of caffeine. Blockade of the adenosine A1 receptor in the heart leads to the accelerated, pronounced "pounding" of the heart upon caffeine intake.
Chlorpheniramine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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.
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| Pharmacology |
Caffeine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Caffeine, a naturally occurring xanthine derivative like theobromine and the bronchodilator theophylline, is used as a CNS stimulant, mild diuretic, and respiratory stimulant (in neonates with apnea of prematurity). Often combined with analgesics or with ergot alkaloids, caffeine is used to treat migraine and other headache types. Over the counter, caffeine is available to treat drowsiness or mild water-weight gain.
Chlorpheniramine¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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.
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| Metabolism |
Caffeine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)
Chlorpheniramine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)Cytochrome P450 2D6 (CYP2D6)
Dihydrocodeine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2D6 (CYP2D6)
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| Protein Binding |
Caffeine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Low (25 to 36%).
Chlorpheniramine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 72%
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| Half-life |
Caffeine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 3 to 7 hours in adults, 65 to 130 hours in neonates
Chlorpheniramine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 21-27 hours
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| Absorption |
Caffeine¿¡ ´ëÇÑ Absorption Á¤º¸ Readily absorbed after oral or parenteral administration. The peak plasma level for caffeine range from 6-10mg/L and the mean time to reach peak concentration ranged from 30 minutes to 2 hours.
Chlorpheniramine¿¡ ´ëÇÑ Absorption Á¤º¸ Well absorbed in the gastrointestinal tract.
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| Pharmacokinetics |
Caffeine anhydrousÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : °æ±¸ : ½Å¼ÓÇϰÔ, ¿ÏÀüÈ÷ Èí¼öµÊ (99%)
- ºÐÆ÷ : ¸ðµç ü¾×¿¡ ºÐÆ÷Çϸç, ³úÇ÷°üÀ庮, ŹÝÀ» Åë°úÇϰí, À¯ÁóÀ¸·Îµµ ºÐºñµÊ
- ºÐÆ÷¿ëÀû :
- ½Å»ý¾Æ : 0.92 L/kg
- ¼ºÀÎ : 0.58 L/kg
- ´Ü¹é°áÇÕ : 15-35%
- ´ë»ç : ¼ºÀÎ : °ÅÀÇ ´ëºÎºÐÀÌ °£¿¡¼ ´ë»çµÇ¸ç, Å»¸ÞƿȵǾî paraxanthine (72%), theobromine (20%), theophylline (8%)À¸·Î ´ë»çµÊ
- ¹Ý°¨±â :
- ¹Ì¼÷¾Æ : 65-103 ½Ã°£
- ¿Ï¼÷¾Æ : 82½Ã°£
- 3-4°³¿ù ¿µ¾Æ : 14.4 ½Ã°£
- 5-6°³¿ù ¿µ¾Æ : 2.6 ½Ã°£
- ¼ºÀÎ : 3-7.5 ½Ã°£ (Æò±Õ 4.9 ½Ã°£)
- ÀӽźΠ: 18½Ã°£±îÁö
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 15-45ºÐ
- ¼Ò½Ç :
- ¼ºÀÎ : ¹Ìº¯Èü·Î ½Å¹è¼³µÇ´Â ¾çÀº 0.5-3.5%
- ½Å»ý¾Æ : °ÅÀÇ ´ëºÎºÐ ¹Ìº¯Èü·Î ½Å¹è¼³µÊ
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.
Dihydrocodeine TartrateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : °æ±¸ : 95-100%
- ºÐÆ÷ : Vd : 1.1 L/kg. ³úÇ÷°üÀ庮 Åë°ú, ÅÂ¹Ý Åë°ú, À¯Áó ºÐºñ
- ´ë»ç : ÃÊȸÅë°úÈ¿°ú Á¸Àç
- ¹Ý°¨±â :
- ¥á»ó : 16-20ºÐ
- ¥â»ó : 3.4-4.5 ½Ã°£
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 1.6-1.8 ½Ã°£
- ¼Ò½Ç : ½Å¹è¼³
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| Biotransformation |
Caffeine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic cytochrome P450 1A2 (CYP 1A2) is involved in caffeine biotransformation. About 80% of a dose of caffeine is metabolized to paraxanthine (1,7-dimethylxanthine), 10% to theobromine (3,7-dimethylxanthine), and 4% to theophylline (1,3-dimethylxanthine).
Chlorpheniramine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic via Cytochrome P450 (CYP450) enzymes.
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| Toxicity |
Caffeine¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=127 mg/kg (orally in mice)
Chlorpheniramine¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50 = 306 mg/kg in humans, mild reproductive toxin to women of childbearing age.
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| Drug Interactions |
Caffeine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
Chlorpheniramine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ 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
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Chlorpheniramine¿¡ ´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 |
Chlorpheniramine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with food.Avoid alcohol.
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| Drug Target |
[Drug Target]
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| SNP Á¤º¸ |
Name:Caffeine (DB00201)
Interacting Gene/Enzyme:Cytochrome P450 1A2 (Gene symbol = CYP1A2) Swissprot P05177
SNP(s):rs762551 (C allele)
Effect:Myocardial infarction
Reference(s):Cornelis MC, El-Sohemy A, Kabagambe EK, Campos H: Coffee, CYP1A2 genotype, and risk of myocardial infarction. JAMA. 2006 Mar 8;295(10):1135-41. [PubMed]
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| Description |
Caffeine¿¡ ´ëÇÑ Description Á¤º¸ A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine&
Chlorpheniramine¿¡ ´ëÇÑ Description Á¤º¸ 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]
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| Drug Category |
Caffeine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anorexigenic AgentsCentral Nervous System StimulantsPhosphodiesterase Inhibitors
Chlorpheniramine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Allergic AgentsAntihistaminesAntipruriticsHistamine H1 Antagonists
Dihydrocodeine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Analgesics, Opioid
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| Smiles String Canonical |
Caffeine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN1C=NC2=C1C(=O)N(C)C(=O)N2C
Chlorpheniramine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(C)CCC(C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Dihydrocodeine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=C2OC3C(O)CCC4C5CC(C=C1)=C2C34CCN5C
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| Smiles String Isomeric |
Caffeine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN1C=NC2=C1C(=O)N(C)C(=O)N2C
Chlorpheniramine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(C)CC[C@H](C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Dihydrocodeine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=C2O[C@H]3[C@@H](O)CC[C@H]4[C@H]5CC(C=C1)=C2[C@@]34CCN5C
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| InChI Identifier |
Caffeine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C8H10N4O2/c1-10-4-9-6-5(10)7(13)12(3)8(14)11(6)2/h4H,1-3H3
Chlorpheniramine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ 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
Dihydrocodeine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C18H23NO3/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,4-5,7-9H2,1-2H3/t11-,12+,13-,17-,18-/m0/s1
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| Chemical IUPAC Name |
Caffeine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 1,3,7-trimethylpurine-2,6-dione
Chlorpheniramine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3-(4-chlorophenyl)-N,N-dimethyl-3-pyridin-2-ylpropan-1-amine
Dihydrocodeine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ Not Available
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| Drug-Induced Toxicity Related Proteins |
CAFFEINE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Metallothionein Drug:caffeine Toxicity:hepatotoxicity. [¹Ù·Î°¡±â] 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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ÃÖ±ÙÁ¤º¸¼öÁ¤ÀÏ 2025-09-30
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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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