Acetylcysteine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Acetylcysteine may protect against acetaminophen overdose-induced hepatotoxicity by maintaining or restoring hepatic concentrations of glutathione. Glutathione is required to inactivate an intermediate metabolite of acetaminophen that is thought to be hepatotoxic. In acetaminophen overdose, excessive quantities of this metabolite are formed because the primary metabolic (glucuronide and sulfate conjugation) pathways become saturated. Acetylcysteine may act by reducing the metabolite to the parent compound and/or by providing sulfhydryl for conjugation of the metabolite. Experimental evidence also suggests that a sulfhydryl-containing compound such as acetylcysteine may also directly inactivate the metabolite. Inhalation - Acetylcysteine exerts its mucolytic action through its free sulfhydryl group, which opens the disulfide bonds and lowers mucus viscosity. This action increases with increasing pH and is most significant at pH 7 to 9. The mucolytic action of acetylcysteine is not affected by the presence of DNA.
Pharmacology
Acetylcysteine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Acetylcysteine has been shown to reduce the extent of liver injury following acetaminophen overdose. It is most effective when given early, with benefit seen principally in patients treated within 8-10 hours of the overdose. Acetylcysteine likely protects the liver by maintaining or restoring the glutathione levels, or by acting as an alternate substrate for conjugation with, and thus detoxification of, the reactive metabolite.
Acetylcysteine¿¡ ´ëÇÑ Absorption Á¤º¸ Bioavailability is 6??0% following oral administration and less than 3% following topical administration.
Pharmacokinetics
AcetylcysteineÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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ÈíÀÔ : 5-10ºÐ À̳»
ÀÛ¿ëÁö¼Ó½Ã°£ : 1½Ã°£ ÀÌ»ó
Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£
°æ±¸ : 1-2 ½Ã°£
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°æ±¸ : 0.33-0.47 L/kg
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°æ±¸ : 50%
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ȯ¿øÇü acetylcysteine : 2½Ã°£
Àüü acetylcysteineÀ¸·Î¼ 5.5 ½Ã°£
Biotransformation
Acetylcysteine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. Deacetylated by the liver to cysteine and subsequently metabolized.
Toxicity
Acetylcysteine¿¡ ´ëÇÑ Toxicity Á¤º¸ Single intravenous doses of acetylcysteine at 1000 mg/kg in mice, 2445 mg/kg in rats, 1500 mg/kg in guinea pigs, 1200 mg/kg in rabbits and 500 mg/kg in dogs were lethal. Symptoms of acute toxicity were ataxia, hypoactivity, labored respiration, cyanosis, loss of righting reflex and convulsions.
Drug Interactions
Acetylcysteine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
Acetylcysteine¿¡ ´ëÇÑ Description Á¤º¸ The N-acetyl derivative of cysteine. It is used as a mucolytic agent to reduce the viscosity of mucous secretions. It has also been shown to have antiviral effects in patients with HIV due to inhibition of viral stimulation by reactive oxygen intermediates. [PubChem]
The database contains the following fields: The generic name of each chemical For module A10 (liver enzyme composite module): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method) Number of endpoints at which each compound is marginally active (M) Number of endpoints at which each compound is active (A) For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method) Number of ADR reports for each compound, given as <4 or ¡Ã4 Reporting Index value for each compound, except where no shipping units were available (NSU) Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period. ACETYLCYSTEINE [GGT Increase] [Composite Activity] (Score) NA (Marginal) 0 (Active) 1
[Alkaline Phosphatase Increase] (Activity Score) NA (Number of Rpts) NA (Index value) NA
[SGOT Increase] (Activity Score) NA (Number of Rpts) NA (Index value) NA