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BUTALBITAL AND ACETAMINOPHEN (ACETAMINOPHEN; BUTALBITAL)
BUTALBITAL, ACETAMINOPHEN AND CAFFEINE (ACETAMINOPHEN; BUTALBITAL; CAFFEINE)
BUTALBITAL, ACETAMINOPHEN, AND CAFFEINE WITH CODEINE PHOSPHATE (ACETAMINOPHEN; BUTALBITAL; CAFFEINE; CODEINE PHOSPHATE)
BUTALBITAL, ACETAMINOPHEN, CAFFEINE AND CODEINE PHOSPHATE (ACETAMINOPHEN; BUTALBITAL; CAFFEINE; CODEINE PHOSPHATE)
BUTALBITAL; ACETAMINOPHEN; CAFFEINE; CODEINE (BUTALBITAL; ACETAMINOPHEN; CAFFEINE; CODEINE PHOSPHATE)
BUTAPAP (ACETAMINOPHEN; BUTALBITAL)
CAPITAL AND CODEINE (ACETAMINOPHEN; CODEINE PHOSPHATE)
CODEINE, ASPIRIN, APAP FORMULA NO. 2 (ACETAMINOPHEN; ASPIRIN; CODEINE PHOSPHATE)
CODEINE, ASPIRIN, APAP FORMULA NO. 3 (ACETAMINOPHEN; ASPIRIN; CODEINE PHOSPHATE)
CODEINE, ASPIRIN, APAP FORMULA NO. 4 (ACETAMINOPHEN; ASPIRIN; CODEINE PHOSPHATE)
CODRIX (ACETAMINOPHEN; CODEINE PHOSPHATE)
CO-GESIC (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
DARVOCET (ACETAMINOPHEN; PROPOXYPHENE HYDROCHLORIDE)
DARVOCET A500 (ACETAMINOPHEN; PROPOXYPHENE NAPSYLATE)
DARVOCET-N 100 (ACETAMINOPHEN; PROPOXYPHENE NAPSYLATE)
DARVOCET-N 50 (ACETAMINOPHEN; PROPOXYPHENE NAPSYLATE)
DHC PLUS (ACETAMINOPHEN; CAFFEINE; DIHYDROCODEINE BITARTRATE)
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)
ESGIC (ACETAMINOPHEN; BUTALBITAL; CAFFEINE)
ESGIC-PLUS (ACETAMINOPHEN; BUTALBITAL; CAFFEINE)
EXCEDRIN (MIGRAINE) (ACETAMINOPHEN; ASPIRIN; CAFFEINE)
FEMCET (ACETAMINOPHEN; BUTALBITAL; CAFFEINE)
FIORICET (ACETAMINOPHEN; BUTALBITAL; CAFFEINE)
FIORICET W/ CODEINE (ACETAMINOPHEN; BUTALBITAL; CAFFEINE; 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)
MEDIGESIC PLUS (ACETAMINOPHEN; BUTALBITAL; CAFFEINE)
NEOPAP (ACETAMINOPHEN)
NORCET (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
NORCO (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
PAPA-DEINE #3 (ACETAMINOPHEN; CODEINE PHOSPHATE)
PAPA-DEINE #4 (ACETAMINOPHEN; CODEINE PHOSPHATE)
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)
PHRENILIN WITH CAFFEINE AND CODEINE (ACETAMINOPHEN; BUTALBITAL; CAFFEINE; CODEINE PHOSPHATE)
PROPACET 100 (ACETAMINOPHEN; PROPOXYPHENE NAPSYLATE)
PROPOXYPHENE HYDROCHLORIDE AND ACETAMINOPHEN (ACETAMINOPHEN; PROPOXYPHENE HYDROCHLORIDE)
PROPOXYPHENE NAPSYLATE AND ACETAMINOPHEN (ACETAMINOPHEN; PROPOXYPHENE NAPSYLATE)
PROVAL #3 (ACETAMINOPHEN; CODEINE PHOSPHATE)
SEDAPAP (ACETAMINOPHEN; BUTALBITAL)
SYNALGOS-DC-A (ACETAMINOPHEN; CAFFEINE; DIHYDROCODEINE BITARTRATE)
TALACEN (ACETAMINOPHEN; PENTAZOCINE HYDROCHLORIDE)
TAVIST ALLERGY/SINUS/HEADACHE (ACETAMINOPHEN; CLEMASTINE FUMARATE; PSEUDOEPHEDRINE HYDROCHLORIDE)
TENCON (ACETAMINOPHEN; BUTALBITAL)
TRAMADOL HYDROCHLORIDE AND ACETAMINOPHEN (ACETAMINOPHEN; TRAMADOL HYDROCHLORIDE)
TRIAD (ACETAMINOPHEN; BUTALBITAL; CAFFEINE)
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)
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.
Oxycodone¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Oxycodone acts as a weak agonist at mu, kappa, and delta opioid receptors within the central nervous system (CNS). Oxycodone primarily affects mu-type opioid receptors, which are coupled with G-protein receptors and function as modulators, both positive and negative, of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine, and noradrenaline is inhibited. Opioids such as oxycodone also inhibit the release of vasopressin, somatostatin, insulin, and glucagon. Opioids close N-type voltage-operated calcium channels (kappa-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (mu and delta receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
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| 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.
Oxycodone¿¡ ´ëÇÑ Pharmacology Á¤º¸ Oxycodone, a semisynthetic opiate agonist derived from the opioid alkaloid, thebaine, is similar to other phenanthrene derivatives such as hydrocodone and morphine. Oxycodone is available in combination with aspirin or acetaminophen to control pain and restless leg and Tourette syndromes.
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| Protein Binding |
Oxycodone¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 45%
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| Half-life |
Acetaminophen¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 1 to 4 hours
Oxycodone¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 4.5 hours
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| Absorption |
Acetaminophen¿¡ ´ëÇÑ Absorption Á¤º¸ Rapid and almost complete
Oxycodone¿¡ ´ëÇÑ Absorption Á¤º¸ Well absorbed with an oral bioavailability of 60% to 87%
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| Pharmacokinetics |
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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.
Oxycodone¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic
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| 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.
Oxycodone¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, bradycardia, hypotension, and death.
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| 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 effect
Oxycodone¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Cimetidine Cimetidine increases the effect of the narcoticCitalopram Increased risk of serotonin syndromeEscitalopram Increased risk of serotonin syndromeFluoxetine Increased risk of serotonin syndromeFluvoxamine Increased risk of serotonin syndromeSertraline Increased risk of serotonin syndromeParoxetine Increased risk of serotonin syndromeNaltrexone Naltrexone may precipitate a withdrawal syndrome in opioid-dependent individuals
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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
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| Drug Target |
[Drug Target]
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| 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]
Oxycodone¿¡ ´ëÇÑ Description Á¤º¸ Semisynthetic derivative of codeine that acts as a narcotic analgesic more potent and addicting than codeine. [PubChem]
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| Dosage Form |
Acetaminophen¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule OralElixir OralLiquid OralSolution OralSolution / drops OralSuppository RectalSuspension OralSyrup OralTablet OralTablet, effervescent OralTablet, extended release Oral
Oxycodone¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Suppository RectalTablet OralTablet, extended release Oral
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| Drug Category |
Acetaminophen¿¡ ´ëÇÑ Drug_Category Á¤º¸ Analgesics, Non-NarcoticAntipyretics
Oxycodone¿¡ ´ëÇÑ Drug_Category Á¤º¸ Analgesics, OpioidAntitussivesNarcoticsOpiate Agonists
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| Smiles String Canonical |
Acetaminophen¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(=O)NC1=CC=C(O)C=C1
Oxycodone¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=C2OC3C(=O)CCC4(O)C5CC(C=C1)=C2C34CCN5C
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| Smiles String Isomeric |
Acetaminophen¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(=O)NC1=CC=C(O)C=C1
Oxycodone¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=C2O[C@H]3C(=O)CC[C@@]4(O)[C@H]5CC(C=C1)=C2[C@@]34CCN5C
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| 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/h9H
Oxycodone¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C18H21NO4/c1-19-8-7-17-14-10-3-4-12(22-2)15(14)23-16(17)11(20)5-6-18(17,21)13(19)9-10/h3-4,13,16,21H,5-9H2,1-2H3/t13-,16+,17+,18-/m1/s1
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| Chemical IUPAC Name |
Acetaminophen¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ N-(4-hydroxyphenyl)acetamide
Oxycodone¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 4, 5-epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one
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| 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-dehydrogenase Drug:acetaminophen Toxicity:drug-induced hemolysis. [¹Ù·Î°¡±â] Replated Protein:Ornithine decarboxylase Drug:acetaminophen Toxicity:hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein:Lactate dehydrogenase Drug: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 aminotransferase Drug:acetaminophen Toxicity:hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein:Beta-glucuronidase Drug:acetaminophen Toxicity:hepatotoxin-induced effects. [¹Ù·Î°¡±â] Replated Protein:CYP2E1 Drug:Acetaminophen Toxicity:idiosyncratic hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein:Cytochrome P450 2E1 Drug:acetaminophen Toxicity:hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein:Sulfotransferase family cytosolic Drug: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 P450 Drug:acetaminophen (APAP) Toxicity:renal functional changes, strain-dependent histopathological changes. [¹Ù·Î°¡±â]
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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