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Potassium¿¡ ´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 |
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.
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.
Potassium¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Potassium is the major cation (positive ion) inside animal cells, while sodium is the major cation outside animal cells. The concentration differences of these charged particles causes a difference in electric potential between the inside and outside of cells, known as the membrane potential. The balance between potassium and sodium is maintained by ion pumps in the cell membrane. The cell membrane potential created by potassium and sodium ions allows the cell generate an action potential?”a "spike" of electrical discharge. The ability of cells to produce electrical discharge is critical for body functions such as neurotransmission, muscle contraction, and heart function. Potassium is also an essential mineral needed to regulate water balance, blood pressure and levels of acidity.
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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.
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.
Potassium¿¡ ´ëÇÑ Pharmacology Á¤º¸ Not Available
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| Metabolism |
Caffeine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)
Potassium¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 11B2 (CYP11B2)
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| Protein Binding |
Caffeine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Low (25 to 36%).
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| Half-life |
Caffeine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 3 to 7 hours in adults, 65 to 130 hours in neonates
Carbinoxamine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 10 to 20 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.
Potassium¿¡ ´ëÇÑ Absorption Á¤º¸ Not Available
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| Pharmacokinetics |
Caffeine anhydrousÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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- 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
Carbinoxamine MaleateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ëÁö¼Ó½Ã°£ : 3-6 ½Ã°£
- ¹Ý°¨±â : 10-20 ½Ã°£
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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).
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| Toxicity |
Caffeine¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=127 mg/kg (orally in mice)
Potassium¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
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| Drug Interactions |
Caffeine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
Potassium¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Amiloride Increased risk of hyperkaliemiaBenazepril Increased risk of hyperkaliemiaCandesartan Increased risk of hyperkaliemiaCaptopril Increased risk of hyperkaliemiaCilazapril Increased risk of hyperkaliemiaDrospirenone Increased risk of hyperkaliemiaEnalapril Increased risk of hyperkaliemiaEplerenone This association presents an increased risk of hyperkaliemiaEprosartan Increased risk of hyperkaliemiaForasartan Increased risk of hyperkaliemiaFosinopril Increased risk of hyperkaliemiaIrbesartan Increased risk of hyperkaliemiaLisinopril Increased risk of hyperkaliemiaLosartan Increased risk of hyperkaliemiaMoexipril Increased risk of hyperkaliemiaPerindopril Increased risk of hyperkaliemiaPolystyrene sulfonate Antagonism of actionQuinapril Increased risk of hyperkaliemiaRamipril Increased risk of hyperkaliemiaSaprisartan Increased risk of hyperkaliemiaSpirapril Increased risk of hyperkaliemiaSpironolactone Increased risk of hyperkaliemiaTasosartan Increased risk of hyperkaliemiaTelmisartan Increased risk of hyperkaliemiaTrandolapril Increased risk of hyperkaliemiaTriamterene Increased risk of hyperkaliemiaValsartan Increased risk of hyperkaliemia
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Potassium¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
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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&
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.
Potassium¿¡ ´ëÇÑ Description Á¤º¸ Potassium is the major cation (positive ion) inside animal cells, while sodium is the major cation outside animal cells. The concentration differences of these charged particles causes a difference in electric potential between the inside and outside of cells, known as the membrane potential. The balance between potassium and sodium is maintained by ion pumps in the cell membrane. The cell membrane potential created by potassium and sodium ions allows the cell generate an action potential?”a "spike" of electrical discharge. The ability of cells to produce electrical discharge is critical for body functions such as neurotransmission, muscle contraction, and heart function. Potassium is also an essential mineral needed to regulate water balance, blood pressure and levels of acidity.
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| Dosage Form |
Caffeine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule OralElixir OralLiquid OralPill OralSolution OralSolution / drops OralSuppository RectalSuspension OralSyrup OralTablet OralTablet, extended release Oral
Carbinoxamine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Solution / drops OralSyrup OralTablet OralTablet, extended release Oral
Potassium¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Aerosol OralCapsule OralCapsule, extended release OralElixir OralLiquid IntravenousLiquid OralLiquid SublingualPowder OralPowder, for solution OralSolution IntravenousSolution OralSolution / drops OralTablet OralTablet, extended release Oral
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| Drug Category |
Caffeine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anorexigenic AgentsCentral Nervous System StimulantsPhosphodiesterase Inhibitors
Carbinoxamine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antihistamines
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| Smiles String Canonical |
Caffeine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN1C=NC2=C1C(=O)N(C)C(=O)N2C
Carbinoxamine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(C)CCOC(C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Potassium¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ Not Available
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| Smiles String Isomeric |
Caffeine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN1C=NC2=C1C(=O)N(C)C(=O)N2C
Carbinoxamine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(C)CCO[C@@H](C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Potassium¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ Not Available
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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
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
Potassium¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ Not Available
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| Chemical IUPAC Name |
Caffeine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 1,3,7-trimethylpurine-2,6-dione
Carbinoxamine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-N,N-dimethylethanamine
Potassium¿¡ ´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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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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