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DARVOCET-N 50 (ACETAMINOPHEN; PROPOXYPHENE NAPSYLATE)
DOLENE AP-65 (ACETAMINOPHEN; PROPOXYPHENE HYDROCHLORIDE)
DRIXORAL PLUS (ACETAMINOPHEN; DEXBROMPHENIRAMINE MALEATE; PSEUDOEPHEDRINE SULFATE)
DURADYNE DHC (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
EMPRACET W/ CODEINE PHOSPHATE #3 (ACETAMINOPHEN; CODEINE PHOSPHATE)
EMPRACET W/ CODEINE PHOSPHATE #4 (ACETAMINOPHEN; CODEINE PHOSPHATE)
HYDROCODONE BITARTRATE AND ACETAMINOPHEN (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
HY-PHEN (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
INFANTS' FEVERALL (ACETAMINOPHEN)
INJECTAPAP (ACETAMINOPHEN)
LORCET-HD (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
LORTAB (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
NEOPAP (ACETAMINOPHEN)
NORCET (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
NORCO (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
OXYCET (ACETAMINOPHEN; OXYCODONE HYDROCHLORIDE)
OXYCODONE 2.5/APAP 500 (ACETAMINOPHEN; OXYCODONE HYDROCHLORIDE)
OXYCODONE 5/APAP 500 (ACETAMINOPHEN; OXYCODONE HYDROCHLORIDE)
OXYCODONE AND ACETAMINOPHEN (ACETAMINOPHEN; OXYCODONE HYDROCHLORIDE)
PAPA-DEINE #3 (ACETAMINOPHEN; CODEINE PHOSPHATE)
PAPA-DEINE #4 (ACETAMINOPHEN; CODEINE PHOSPHATE)
PERCOCET (ACETAMINOPHEN; OXYCODONE HYDROCHLORIDE)
PHENAPHEN W/ CODEINE NO. 2 (ACETAMINOPHEN; CODEINE PHOSPHATE)
PHENAPHEN W/ CODEINE NO. 3 (ACETAMINOPHEN; CODEINE PHOSPHATE)
PHENAPHEN W/ CODEINE NO. 4 (ACETAMINOPHEN; CODEINE PHOSPHATE)
PHENAPHEN-650 W/ CODEINE (ACETAMINOPHEN; CODEINE PHOSPHATE)
PHRENILIN (ACETAMINOPHEN; BUTALBITAL)
PHRENILIN FORTE (ACETAMINOPHEN; BUTALBITAL)
PROPACET 100 (ACETAMINOPHEN; PROPOXYPHENE NAPSYLATE)
PROPOXYPHENE HYDROCHLORIDE AND ACETAMINOPHEN (ACETAMINOPHEN; PROPOXYPHENE HYDROCHLORIDE)
PROPOXYPHENE NAPSYLATE AND ACETAMINOPHEN (ACETAMINOPHEN; PROPOXYPHENE NAPSYLATE)
PROVAL #3 (ACETAMINOPHEN; CODEINE PHOSPHATE)
ROXICET (ACETAMINOPHEN; OXYCODONE HYDROCHLORIDE)
ROXICET 5/500 (ACETAMINOPHEN; OXYCODONE HYDROCHLORIDE)
ROXILOX (ACETAMINOPHEN; OXYCODONE HYDROCHLORIDE)
SEDAPAP (ACETAMINOPHEN; BUTALBITAL)
TALACEN (ACETAMINOPHEN; PENTAZOCINE HYDROCHLORIDE)
TAVIST ALLERGY/SINUS/HEADACHE (ACETAMINOPHEN; CLEMASTINE FUMARATE; PSEUDOEPHEDRINE HYDROCHLORIDE)
TENCON (ACETAMINOPHEN; BUTALBITAL)
TRAMADOL HYDROCHLORIDE AND ACETAMINOPHEN (ACETAMINOPHEN; TRAMADOL HYDROCHLORIDE)
TRIAPRIN (ACETAMINOPHEN; BUTALBITAL)
TYCOLET (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
TYLENOL (ACETAMINOPHEN)
TYLENOL (CAPLET) (ACETAMINOPHEN)
TYLENOL (GELTAB) (ACETAMINOPHEN)
TYLENOL W/ CODEINE (ACETAMINOPHEN; CODEINE PHOSPHATE)
TYLENOL W/ CODEINE NO. 1 (ACETAMINOPHEN; CODEINE PHOSPHATE)
TYLENOL W/ CODEINE NO. 2 (ACETAMINOPHEN; CODEINE PHOSPHATE)
TYLENOL W/ CODEINE NO. 3 (ACETAMINOPHEN; CODEINE PHOSPHATE)
TYLENOL W/ CODEINE NO. 4 (ACETAMINOPHEN; CODEINE PHOSPHATE)
TYLOX (ACETAMINOPHEN; OXYCODONE HYDROCHLORIDE)
TYLOX-325 (ACETAMINOPHEN; OXYCODONE HYDROCHLORIDE)
ULTRACET (ACETAMINOPHEN; TRAMADOL HYDROCHLORIDE)
VICODIN (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
VICODIN ES (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
VICODIN HP (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
WYGESIC (ACETAMINOPHEN; PROPOXYPHENE HYDROCHLORIDE)
ZYDONE (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
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Acetaminophen ¿¡ ´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
Acetaminophen¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Acetaminophen is thought to act primarily in the CNS, increasing the pain threshold by inhibiting both isoforms of cyclooxygenase, COX-1 and COX-2, enzymes involved in prostaglandin (PG) synthesis. Unlike NSAIDs, acetaminophen does not inhibit cyclooxygenase in peripheral tissues and, thus, has no peripheral anti-inflammatory affects. While aspirin acts as an irreversible inhibitor of COX and directly blocks the enzyme's active site, studies have found that acetaminophen indirectly blocks COX, and that this blockade is ineffective in the presence of peroxides. This might explain why acetaminophen is effective in the central nervous system and in endothelial cells but not in platelets and immune cells which have high levels of peroxides. Studies also report data suggesting that acetaminophen selectively blocks a variant of the COX enzyme that is different from the known variants COX-1 and COX-2. This enzyme is now referred to as COX-3. Its exact mechanism of action is still poorly understood, but future research may provide further insight into how it works.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.
Pharmacology
Acetaminophen¿¡ ´ëÇÑ Pharmacology Á¤º¸ Acetaminophen (USAN) or Paracetamol (INN) is a popular analgesic and antipyretic drug that is used for the relief of fever, headaches, and other minor aches and pains. It is a major ingredient in numerous cold and flu medications and many prescription analgesics. It is extremely safe in standard doses, but because of its wide availability, deliberate or accidental overdoses are not uncommon. Acetaminophen, unlike other common analgesics such as aspirin and ibuprofen, has no anti-inflammatory properties or effects on platelet function, and so it is not a member of the class of drugs known as non-steroidal anti-inflammatory drugs or NSAIDs. In normal doses acetaminophen does not irritate the lining of the stomach nor affect blood coagulation, the kidneys, or the fetal ductus arteriosus (as NSAIDs can). Like NSAIDs and unlike opioid analgesics, acetaminophen does not cause euphoria or alter mood in any way. Acetaminophen and NSAIDs have the benefit of being completely free of problems with addiction, dependence, tolerance and withdrawal. Acetaminophen is used on its own or in combination with pseudoephedrine, dextromethorphan, chlorpheniramine, diphenhydramine, doxylamine, codeine, hydrocodone, or oxycodone.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.
Metabolism
Acetaminophen¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)Cytochrome P450 2E1 (CYP2E1)Caffeine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)
Protein Binding
Caffeine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Low (25 to 36%).
Half-life
Acetaminophen¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 1 to 4 hoursCaffeine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 3 to 7 hours in adults, 65 to 130 hours in neonates
Absorption
Acetaminophen¿¡ ´ëÇÑ Absorption Á¤º¸ Rapid and almost completeCaffeine¿¡ ´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.
Pharmacokinetics
AcetaminophenÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
´Ü¹é°áÇÕ : 20-50%
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Èí¼ö : °æ±¸ : ½Å¼ÓÇϰÔ, ¿ÏÀüÈ÷ Èí¼öµÊ (99%)
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½Å»ý¾Æ : 0.92 L/kg
¼ºÀÎ : 0.58 L/kg
´Ü¹é°áÇÕ : 15-35%
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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°£)
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Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : 15-45ºÐ
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Biotransformation
Acetaminophen¿¡ ´ëÇÑ Biotransformation Á¤º¸ Approximately 90 to 95% of a dose is metabolized in the liver via the cytochrome P450 enzyme pathways (primarily by conjugation with glucuronic acid, sulfuric acid, and cysteine). An intermediate metabolite is hepatotoxic and most likely nephrotoxic and can accumulate after the primary metabolic pathways have been saturated.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).
Toxicity
Acetaminophen¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral, mouse: LD50 = 338 mg/kg; Oral, rat: LD50 = 1944 mg/kg. Acetaminophen is metabolized primarily in the liver, where most of it is converted to inactive compounds by conjugation with sulfate and glucuronide, and then excreted by the kidneys. Only a small portion is metabolized via the hepatic cytochrome P450 enzyme system. The toxic effects of acetaminophen are due to a minor alkylating metabolite (N-acetyl-p-benzo-quinone imine), not acetaminophen itself nor any of the major metabolites. This toxic metabolite reacts with sulfhydryl groups. At usual doses, it is quickly detoxified by combining irreversibly with the sulfhydryl group of glutathione to produce a non-toxic conjugate that is eventually excreted by the kidneys. The toxic dose of paracetamol is highly variable. In adults, single doses above 10 grams or 140 mg/kg have a reasonable likelihood of causing toxicity. In adults, single doses of more than 25 grams have a high risk of lethality.Caffeine¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50 =127 mg/kg (orally in mice)
Drug Interactions
Acetaminophen¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Anisindione Acetaminophen increases the anticoagulant effectWarfarin Acetaminophen increases the anticoagulant effectImatinib Increased hepatic toxicity of both agentsIsoniazid Risk of hepatotoxicityDicumarol Acetaminophen increases the anticoagulant effectDicumarol Increases the anticoagulant effectAcenocoumarol Increases the anticoagulant effectCaffeine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
CYP450 Drug Interaction
[CYP450 TableÁ÷Á¢Á¶È¸] Acetaminophen¿¡ ´ëÇÑ P450 table SUBSTRATES
CYP 2E1
**acetaminophen**
chlorzoxazone
ethanol
INHIBITORS
CYP 2E1
disulfiram
INDUCERS
CYP 2E1
ethanol
isoniazid
Food Interaction
Acetaminophen¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.Avoid alcohol (may increase risk of hepatotoxicity).
Drug Target
[Drug Target]
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]
Description
Acetaminophen¿¡ ´ëÇÑ Description Á¤º¸ Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage. [PubChem]Caffeine¿¡ ´ëÇÑ Description Á¤º¸ A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine&
Dosage Form
Acetaminophen¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule OralElixir OralLiquid OralSolution OralSolution / drops OralSuppository RectalSuspension OralSyrup OralTablet OralTablet, effervescent OralTablet, extended release OralCaffeine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule OralElixir OralLiquid OralPill OralSolution OralSolution / drops OralSuppository RectalSuspension OralSyrup OralTablet OralTablet, extended release Oral
Drug Category
Acetaminophen¿¡ ´ëÇÑ Drug_Category Á¤º¸ Analgesics, Non-NarcoticAntipyreticsCaffeine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anorexigenic AgentsCentral Nervous System StimulantsPhosphodiesterase Inhibitors
Smiles String Canonical
Acetaminophen¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(=O)NC1=CC=C(O)C=C1Caffeine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN1C=NC2=C1C(=O)N(C)C(=O)N2C
Smiles String Isomeric
Acetaminophen¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(=O)NC1=CC=C(O)C=C1Caffeine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN1C=NC2=C1C(=O)N(C)C(=O)N2C
InChI Identifier
Acetaminophen¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C8H9NO2/c1-6(10)9-7-2-4-8(11)5-3-7/h2-5,11H,1H3,(H,9,10)/f/h9HCaffeine¿¡ ´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
Chemical IUPAC Name
Acetaminophen¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ N-(4-hydroxyphenyl)acetamideCaffeine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 1,3,7-trimethylpurine-2,6-dione
Drug-Induced Toxicity Related Proteins
ACETAMINOPHEN ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸Replated Protein :Alpha-2A adrenergic receptor Drug :acetaminophen Toxicity :hepatic injury . [¹Ù·Î°¡±â] Replated Protein :Myeloperoxidase Drug :acetaminophen Toxicity :respiratory burst. [¹Ù·Î°¡±â] Replated Protein :Glucose-6-phosphate 1-dehydrogenaseDrug :acetaminophen Toxicity :drug-induced hemolysis. [¹Ù·Î°¡±â] Replated Protein :Ornithine decarboxylaseDrug :acetaminophen Toxicity :hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein :Lactate dehydrogenaseDrug :acetaminophen Toxicity :hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein :Transcription factor AP-1(JUN)Drug :acetaminophen Toxicity :hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein :Haptoglobin Drug :acetaminophen Toxicity :drug-induced hemolysis. [¹Ù·Î°¡±â] Replated Protein :Alanine aminotransferaseDrug :acetaminophen Toxicity :hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein :Beta-glucuronidase Drug :acetaminophen Toxicity :hepatotoxin-induced effects. [¹Ù·Î°¡±â] Replated Protein :CYP2E1Drug :Acetaminophen Toxicity :idiosyncratic hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein :Cytochrome P450 2E1 Drug :acetaminophen Toxicity :hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein :Sulfotransferase family cytosolicDrug :acetaminophen Toxicity :chronic hypoxia. [¹Ù·Î°¡±â] Replated Protein :Cytochrome P450 3A4 Drug :acetaminophen Toxicity :hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein :Caspase recruitment domain-containing protein Drug :acetaminophen Toxicity :hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein :Cytochrome P450 1A2 Drug :acetaminophen Toxicity :hepatotoxicity. [¹Ù·Î°¡±â] ACETAMINOPHEN (APAP) ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸Replated Protein :Cytochrome P450Drug :acetaminophen (APAP) Toxicity :renal functional changes, strain-dependent histopathological changes. [¹Ù·Î°¡±â] CAFFEINE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸Replated Protein :MetallothioneinDrug :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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