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| Off-label Usage |
[Á¶È¸]
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| Related FDA Approved Drug |
±âÁØ ¼ººÐ: GUAIFENESINMUCINEX (GUAIFENESIN)
MUCINEX D (GUAIFENESIN; PSEUDOEPHEDRINE HYDROCHLORIDE)
MUCINEX DM (DEXTROMETHORPHAN HYDROBROMIDE; GUAIFENESIN)
±âÁØ ¼ººÐ: DEXTROMETHORPHAN HBR±âÁØ ¼ººÐ: CHLORPHENIRAMINE MALEATEADVIL ALLERGY SINUS (CHLORPHENIRAMINE MALEATE; IBUPROFEN; PSEUDOEPHEDRINE HYDROCHLORIDE)
ANTAGONATE (CHLORPHENIRAMINE MALEATE)
CHILDREN'S ADVIL ALLERGY SINUS (CHLORPHENIRAMINE MALEATE; IBUPROFEN; PSEUDOEPHEDRINE HYDROCHLORIDE)
CHLOROHENIRAMINE MALEATE AND PHENYLPROPANOLAMINE HYDROCHLORIDE (CHLORPHENIRAMINE MALEATE; PHENYLPROPANOLAMINE HYDROCHLORIDE)
CHLORPHENIRAMINE MALEATE (CHLORPHENIRAMINE MALEATE)
CHLORPHENIRAMINE MALEATE AND PHENYLPROPANOLAMINE HYDROCHLORIDE (CHLORPHENIRAMINE MALEATE; PHENYLPROPANOLAMINE HYDROCHLORIDE)
CHLOR-TRIMETON (CHLORPHENIRAMINE MALEATE)
CODIMAL-L.A. 12 (CHLORPHENIRAMINE MALEATE; PSEUDOEPHEDRINE HYDROCHLORIDE)
COLD CAPSULE IV (CHLORPHENIRAMINE MALEATE; PHENYLPROPANOLAMINE HYDROCHLORIDE)
COLD CAPSULE V (CHLORPHENIRAMINE MALEATE; PHENYLPROPANOLAMINE HYDROCHLORIDE)
CONTAC (CHLORPHENIRAMINE MALEATE; PHENYLPROPANOLAMINE HYDROCHLORIDE)
CONTAC 12 HOUR (CHLORPHENIRAMINE MALEATE; PHENYLPROPANOLAMINE HYDROCHLORIDE)
DEMAZIN (CHLORPHENIRAMINE MALEATE; PHENYLPROPANOLAMINE HYDROCHLORIDE)
DEXCHLORPHENIRAMINE MALEATE (DEXCHLORPHENIRAMINE MALEATE)
DRIZE (CHLORPHENIRAMINE MALEATE; PHENYLPROPANOLAMINE HYDROCHLORIDE)
EFIDAC 24 CHLORPHENIRAMINE MALEATE (CHLORPHENIRAMINE MALEATE)
ISOCLOR (CHLORPHENIRAMINE MALEATE; PSEUDOEPHEDRINE HYDROCHLORIDE)
KLOROMIN (CHLORPHENIRAMINE MALEATE)
ORNADE (CHLORPHENIRAMINE MALEATE; PHENYLPROPANOLAMINE HYDROCHLORIDE)
PHENETRON (CHLORPHENIRAMINE MALEATE)
PHENYLPROPANOLAMINE HYDROCHLORIDE W/ CHLORPHENIRAMINE MALEATE (CHLORPHENIRAMINE MALEATE; PHENYLPROPANOLAMINE HYDROCHLORIDE)
POLARAMINE (DEXCHLORPHENIRAMINE MALEATE)
PSEUDOEPHEDRINE HYDROCHLORIDE AND CHLORPHENIRAMINE MALEATE (CHLORPHENIRAMINE MALEATE; PSEUDOEPHEDRINE HYDROCHLORIDE)
PYRIDAMAL 100 (CHLORPHENIRAMINE MALEATE)
TELDRIN (CHLORPHENIRAMINE MALEATE)
TRIAMINIC-12 (CHLORPHENIRAMINE MALEATE; PHENYLPROPANOLAMINE HYDROCHLORIDE)
±âÁØ ¼ººÐ: ACETAMINOPHENACEPHEN (ACETAMINOPHEN)
ACETAMINOPHEN (ACETAMINOPHEN)
ACETAMINOPHEN AND CODEINE PHOSPHATE (ACETAMINOPHEN; CODEINE PHOSPHATE)
ACETAMINOPHEN AND HYDROCODONE BITARTRATE (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
ACETAMINOPHEN AND PENTAZOCINE HYDROCHLORIDE (ACETAMINOPHEN; PENTAZOCINE HYDROCHLORIDE)
ACETAMINOPHEN, ASPIRIN AND CAFFEINE (ACETAMINOPHEN; ASPIRIN; CAFFEINE)
ACETAMINOPHEN, ASPIRIN, AND CODEINE PHOSPHATE (ACETAMINOPHEN; ASPIRIN; CODEINE PHOSPHATE)
ACETAMINOPHEN, BUTALBITAL AND CAFFEINE (ACETAMINOPHEN; BUTALBITAL; CAFFEINE)
ACETAMINOPHEN, CAFFEINE, AND DIHYDROCODEINE BITARTRATE (ACETAMINOPHEN; CAFFEINE; DIHYDROCODEINE BITARTRATE)
ALLAY (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
ANEXSIA (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
ANEXSIA 5/325 (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
ANEXSIA 7.5/325 (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
ANEXSIA 7.5/650 (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
ANOQUAN (ACETAMINOPHEN; BUTALBITAL; CAFFEINE)
BANCAP (ACETAMINOPHEN; BUTALBITAL)
BANCAP HC (ACETAMINOPHEN; HYDROCODONE BITARTRATE)
BUCET (ACETAMINOPHEN; BUTALBITAL)
BUTALBITAL ACETAMINOPHEN AND CAFFEINE (ACETAMINOPHEN; BUTALBITAL; CAFFEINE)
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)
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)
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)
ROXICET (ACETAMINOPHEN; OXYCODONE HYDROCHLORIDE)
ROXICET 5/500 (ACETAMINOPHEN; OXYCODONE HYDROCHLORIDE)
ROXILOX (ACETAMINOPHEN; OXYCODONE HYDROCHLORIDE)
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)
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
Chlorpheniramine¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Dextromethorphan¿¡ ´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.
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.
Dextromethorphan¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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.
Guaifenesin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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.
Thiamine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ It is thought that the mechanism of action of thiamine on endothelial cells is related to a reduction in intracellular protein glycation by redirecting the glycolytic flux.
|
| 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.
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.
Dextromethorphan¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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.
Guaifenesin¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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.
Thiamine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Thiamine is a vitamin with antioxidant, erythropoietic, cognition-and mood-modulatory, antiatherosclerotic, putative ergogenic, and detoxification activities. Thiamine has been found to protect against lead-induced lipid peroxidation in rat liver and kidney. Thiamine deficiency results in selective neuronal death in animal models. The neuronal death is associated with increased free radical production, suggesting that oxidative stress may play an important early role in brain damage associated with thiamine deficiency. Thiamine plays a key role in intracellular glucose metabolism and it is thought that thiamine inhibits the effect of glucose and insulin on arterial smooth muscle cell proliferation. Inhibition of endothelial cell proliferation may also promote atherosclerosis. Endothelial cells in culture have been found to have a decreased proliferative rate and delayed migration in response to hyperglycemic conditions. Thiamine has been shown to inhibit this effect of glucose on endothelial cells.
|
| Metabolism |
Acetaminophen¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)Cytochrome P450 2E1 (CYP2E1)
Chlorpheniramine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)Cytochrome P450 2D6 (CYP2D6)
Dextromethorphan¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2D6 (CYP2D6)
|
| Protein Binding |
Chlorpheniramine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 72%
Thiamine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 90-94%
|
| Half-life |
Acetaminophen¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 1 to 4 hours
Chlorpheniramine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 21-27 hours
Dextromethorphan¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 3-6 hours
Guaifenesin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 1 hour
|
| Absorption |
Acetaminophen¿¡ ´ëÇÑ Absorption Á¤º¸ Rapid and almost complete
Chlorpheniramine¿¡ ´ëÇÑ Absorption Á¤º¸ Well absorbed in the gastrointestinal tract.
Dextromethorphan¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly absorbed from the gastrointestinal tract.
Guaifenesin¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly absorbed from the GI tract
Thiamine¿¡ ´ëÇÑ Absorption Á¤º¸ Absorbed mainly from duodenum, by both active and passive processes
|
| Pharmacokinetics |
AcetaminophenÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ´Ü¹é°áÇÕ : 20-50%
- ´ë»ç :
- »ó¿ë·®¿¡¼ : °£¿¡¼ sulfate¿Í glucuronide Æ÷ÇÕü·Î ´ë»çµÇ¸ç, ¼Ò·®Àº microsomal mixed function oxidases¿¡ ÀÇÇØ ¹ÝÀÀ¼ºÀÌ ¸Å¿ì ³ôÀº Áß°£´ë»çü(acetylimidoquinone)·Î ´ë»çµÈ ÈÄ glutathione Æ÷ÇÕÀ¸·Î ºñȰ¼ºÈµÈ´Ù.
- Áßµ¶·®¿¡¼ (4gÀ» ´Ü ÇÏ·ç º¹¿ëÇÑ Á¤µµ±îÁöµµ Æ÷ÇԵȴÙ) : glutathione Æ÷ÇÕÀÌ Á¡Á¡ ºÒÃæºÐÇÏ°Ô µÇ¾î acetylimidoquinone ³óµµ°¡ Áõ°¡ÇÏ°Ô µÇ¸ç À̰ÍÀÌ °£¼¼Æ÷ ±«»ç¸¦ À¯¹ßÇÏ´Â °ÍÀ¸·Î ¿©°ÜÁö°í ÀÖ´Ù.
- ¹Ý°¨±â
- ½Å»ý¾Æ : 2-5 ½Ã°£
- ¼ºÀÎ
- Á¤»ó ½Å±â´É : 1-3 ½Ã°£
- ¸»±â ½ÅÁúȯ : 1-3 ½Ã°£
- ÃÖ´ëÇ÷Áß³óµµ µµ´Þ½Ã°£
- °æ±¸ : »ó¿ë·® º¹¿ë½Ã 10-60ºÐ, ±Þ¼º Áßµ¶·® º¹¿ë½Ã Áö¿¬µÉ ¼ö ÀÖ´Ù.
Thiamine nitrateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö :
- °æ±¸ : ÃÖ´ëÈí¼ö·® : 8-15 mg/day
- ±ÙÀ°ÁÖ»ç : ½Å¼ÓÇÏ°í ¿ÏÀüÇÏ°Ô Èí¼öµÈ´Ù.
- ºÐÆ÷ : Ãּҿ䱸·® (¾à 1 mg/day)À» Ãʰú ¼·Ãë½Ã Á¶Á÷ ÀúÀå¿¡ Æ÷Ȱ¡ ³ªÅ¸³´Ù.
- ¼Ò½Ç : °úÀ× ¼·ÃëµÈ ¾çÀº ´¢¸¦ ÅëÇØ ¹è¼³µÈ´Ù.
Dextromethorphan HBrÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÁøÇØÀÛ¿ë ¹ßÇö½Ã°£ : 15~30ºÐ À̳»
- ÀÛ¿ëÁö¼Ó½Ã°£ : 6½Ã°£±îÁö
- ´ë»ç : °£´ë»ç
- ¼Ò½Ç : ÁÖ·Î ½Å¹è¼³
GuaifenesinÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : À§Àå°üÀ¸·ÎºÎÅÍ Àß Èí¼öµÊ.
- ´ë»ç : 60%°¡ °£´ë»çµÊ.
- ¼Ò½Ç : ´ë»çü ¹× 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.
|
| 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.
Chlorpheniramine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic via Cytochrome P450 (CYP450) enzymes.
Dextromethorphan¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. Rapidly and extensively metabolized to dextrorphan (active metabolite). One well known metabolic catalyst involved is a specific cytochrome P450 enzyme known as 2D6, or CYP2D6.
Guaifenesin¿¡ ´ëÇÑ Biotransformation Á¤º¸ Rapidly hydrolyzed (60% within seven hours) and then excreted in the urine, with beta-(2-methoxyphenoxy)-lactic acid as its major urinary metabolite.
Thiamine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic
|
| 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.
Chlorpheniramine¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50 = 306 mg/kg in humans, mild reproductive toxin to women of childbearing age.
Dextromethorphan¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
Guaifenesin¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50 1510 mg/kg (rat, oral)
Thiamine¿¡ ´ëÇÑ Toxicity Á¤º¸ Thiamine toxicity is uncommon; as excesses are readily excreted, although long-term supplementation of amounts larger than 3 gram have been known to cause toxicity. Oral mouse LD50 = 8224 mg/kg, oral rat LD50 = 3710 mg/kg.
|
| 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
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
Dextromethorphan¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ 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
Guaifenesin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
Thiamine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
|
CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Dextromethorphan¿¡ ´ëÇÑ P450 table Chlorpheniramine¿¡ ´ëÇÑ P450 table Acetaminophen¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 2E1
**acetaminophen**
chlorzoxazone
ethanol
INHIBITORS
CYP 2E1
disulfiram
INDUCERS
CYP 2E1
ethanol
isoniazid
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
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
|
| Food Interaction |
Acetaminophen¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.Avoid alcohol (may increase risk of hepatotoxicity).
Chlorpheniramine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with food.Avoid alcohol.
Guaifenesin¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with a full glass of water.Take without regard to meals.
|
| Drug Target |
[Drug Target]
|
| SNP Á¤º¸ |
Name:Dextromethorphan (DB00514)
Interacting Gene/Enzyme:Cytochrome P450 2D6 (Gene symbol = CYP2D6) Swissprot P10635
SNP(s):CYP2D6*6 rs5030655 (T deletion, homozygote)
Effect:Poor drug metabolizer, lower dose requirements
Reference(s):Bradford LD, Gaedigk A, Leeder JS: High frequency of CYP2D6 poor and "intermediate" metabolizers in black populations: a review and preliminary data. Psychopharmacol Bull. 1998;34(4):797-804. [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]
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]
Dextromethorphan¿¡ ´ëÇÑ Description Á¤º¸ 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]
Guaifenesin¿¡ ´ëÇÑ Description Á¤º¸ An expectorant that also has some muscle relaxing action. It is used in many cough preparations. [PubChem]
Thiamine¿¡ ´ëÇÑ Description Á¤º¸ 3-((4-Amino-2-methyl-5-pyrimidinyl)methyl)-5-(2- hydroxyethyl)-4-methylthiazolium chloride. [PubChem]
|
| Dosage Form |
Acetaminophen¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule OralElixir OralLiquid OralSolution OralSolution / drops OralSuppository RectalSuspension OralSyrup OralTablet OralTablet, effervescent OralTablet, extended release Oral
Chlorpheniramine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Syrup OralTablet OralTablet, extended release Oral
Dextromethorphan¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule OralLiquid OralLozenge OralStrip OralSuspension OralSyrup OralTablet Oral
Guaifenesin¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid OralSyrup Oral
Thiamine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid IntramuscularLiquid IntravenousSolution IntravenousTablet Oral
|
| Drug Category |
Acetaminophen¿¡ ´ëÇÑ Drug_Category Á¤º¸ Analgesics, Non-NarcoticAntipyretics
Chlorpheniramine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Allergic AgentsAntihistaminesAntipruriticsHistamine H1 Antagonists
Dextromethorphan¿¡ ´ëÇÑ Drug_Category Á¤º¸ Analgesics, OpioidAntitussive AgentsExcitatory Amino Acid Antagonists
Guaifenesin¿¡ ´ëÇÑ Drug_Category Á¤º¸ Expectorants
Thiamine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-inflammatory AgentsEssential VitaminVitamin B ComplexVitamins (Vitamin B Complex)
|
| Smiles String Canonical |
Acetaminophen¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(=O)NC1=CC=C(O)C=C1
Chlorpheniramine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN(C)CCC(C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Dextromethorphan¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=CC2=C(CC3C4CCCCC24CCN3C)C=C1
Guaifenesin¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=CC=CC=C1OCC(O)CO
Thiamine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC1=NC=C(C[N+]2=CSC(CCO)=C2C)C(N)=N1
|
| Smiles String Isomeric |
Acetaminophen¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(=O)NC1=CC=C(O)C=C1
Chlorpheniramine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN(C)CC[C@H](C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Dextromethorphan¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=CC2=C(C[C@H]3[C@H]4CCCC[C@@]24CCN3C)C=C1
Guaifenesin¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=CC=CC=C1OC[C@H](O)CO
Thiamine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC1=NC=C(C[N+]2=CSC(CCO)=C2C)C(N)=N1
|
| 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
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
Dextromethorphan¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ 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
Guaifenesin¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ 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
Thiamine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C12H17N4OS/c1-8-11(3-4-17)18-7-16(8)6-10-5-14-9(2)15-12(10)13/h5,7,17H,3-4,6H2,1-2H3,(H2,13,14,15)/q+1/f/h13H2
|
| Chemical IUPAC Name |
Acetaminophen¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ N-(4-hydroxyphenyl)acetamide
Chlorpheniramine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3-(4-chlorophenyl)-N,N-dimethyl-3-pyridin-2-ylpropan-1-amine
Dextromethorphan¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ Not Available
Guaifenesin¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3-(2-methoxyphenoxy)propane-1,2-diol
Thiamine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-[3-[(4-amino-2-methylpyrimidin-5-yl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol
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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] 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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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
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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