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N Acetylcysteine


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N Acetylcysteine

  1. 1. N-acetylcysteine (NAC)Trennette R. GilbertUniversity of Southern NevadaCollege of Pharmacy<br />
  2. 2. Description<br />N-acetyl derivative of L-cysteine<br />Pharmacologic category<br />Antidote<br />Mucolytic<br />2<br />
  3. 3. Indications<br />3<br />FDA labeled indications<br />Acetaminophen (APAP) overdose <br />Adjunctive mucolytic therapy <br />Diagnostic bronchial studies<br />Off-label use<br />Prevention of contrast-induced nephrotoxicity (CIN) <br />Helicobacter pylori infection <br />
  4. 4. Pathophysiology of APAP Overdose<br />4<br />APAP primarily metabolized via glucoronidation or sulphation<br />Secondary metabolism by CYP 450 system<br />In OD, primary route saturated -> CYP 450 system -> NAPQI production<br />NAPQI converted to non-toxic form by glutathione<br />In OD, glutathione stores consumed -> excess NAPQI -> covalent binding to hepatocytes<br />
  5. 5. Mechanisms of Action<br />5<br />APAP overdose <br />NAC -> cysteine-> glutathione (GSH)<br />Prevention of CIN<br />Possibly minimizes vasoconstriction and oxidative stress <br />Mucolysis<br />Lowers mucus viscosity<br />Free sulfhydryl group opens disulfide bonds in mucoproteins<br />H. pylori infection<br />May increase delivery of medications by ↓ mucus viscosity<br />
  6. 6. Dosage Forms<br />6<br />Injection solution (Rx)<br />Acetadote 20% (30 ml)<br />Inhalation solution (Rx)<br />Mucomyst, generic 10%, 20% (4 ml, 10 ml, 30 ml)<br />Capsules (OTC)<br />Generic 600 mg (60, 120)<br />Extemporaneous compounding<br />Inhalation solution may be used as IV<br />Inhalation solution may also be mixed w/soda to yield 5% oral solution<br />
  7. 7. IV vs. PO<br />7<br />Both routes are effective, differences minimal<br />IV route preferred if:<br />Vomiting<br />Contraindication to oral administration of medication<br />Hepatic failure<br />Refuses oral administration<br />Pricing:<br />Acetadote = $145.77/vial (30 ml)<br />NAC 10%, 20% inhalation solution = $1.32/vial (4 ml)<br />
  8. 8. Contraindications <br />8<br />Hypersensitivity to acetylcysteine<br />
  9. 9. Warnings/Precautions<br />9<br />Inhaled form may cause increased bronchial secretions, bronchospasm<br />Emesis<br />Oral form may aggravate vomiting <br />Encephalopathy <br />If present, consider discontinuing administration of NAC<br />Odor <br />Has slight disagreeable odor<br />
  10. 10. Adverse Reactions<br />Inhalation <br />Drowsiness<br />Chills/fever<br />N/V<br />Bronchospasm<br />Rhinorrhea<br />Unpleasant odor <br />IV<br />Anaphylactoid reactions<br />N/V<br />10<br />
  11. 11. Drug Interactions<br />11<br />No significant interactions<br />Adsorbed by activated charcoal <br />
  12. 12. Pharmacokinetics<br />12<br />Absorption<br />Bioavailability of oral form is low<br />Distribution<br />Vdss = 0.47 L/kg<br />Plasma protein binding = 83% <br />Metabolism<br />Deacetylated in the liver to cysteine<br />Elimination <br />T1/2 = (Adults) 5.5 hours, (Newborns) 11 hours<br />Primarily non-renal (70%), renal (30%)<br />
  13. 13. Pharmacokinetics - Special Populations<br />13<br />Pregnant women<br />In limited reports, shown to cross placenta<br />Pregnancy risk category: B<br />Hepatic dysfunction<br />May influence pharmacokinetics <br />T1/2 shown to increase by 80%<br />Renal clearance decreased by 30% <br />
  14. 14. Dosing <br />14<br />APAP toxicity<br />Children and adults (> 40 kg)<br />Loading dose should be given<br />Oral: 140 mg/kg <br />IV: 150 mg/kg infused over 60 minutes <br />Maintenance doses<br />Oral: 70 mg/kg q 4 hours x 17 doses<br />IV: 50 mg/kg infused over 4 hours, then 100 mg/kg infused over 16 hours (Total 300 mg/kg infused over 21 hours)<br />Patients < 40 kg <br />Fluid volume should be reduced<br />Weight-based dilution <br />
  15. 15. Dosing cont…<br />Respiratory conditions<br />Diagnostic bronchial studies<br />1 – 2 ml of 20% or 2 – 4 ml of 10% 2 – 3 times prior to procedure <br />Prevention of CIN<br />600 – 1200 mg PO BID x 2 days (begin day before procedure)<br />15<br />
  16. 16. Stability <br />16<br />IV solution<br />Stable for 24 hours after dilution w/D5W<br />Inhalation solution<br />Vials must be refrigerated after opening<br />Must be used w/in 96 hours <br />Opened vials may change color<br />Does not affect safety or efficacy<br />
  17. 17. Monitoring Parameters<br />17<br />Anaphylaxis<br />APAP overdose<br />APAP levels q 4 – 6 hours<br />LFTs<br />Scr, BUN<br />PT, INR<br />
  18. 18. Therapeutic Efficacy<br />18<br />APAP overdose<br />No trials to evaluate efficacy<br />Low incidence of hepatotoxicity when given early <br />Mucolysis<br />Studies suggest small benefit <br />Prevention of CIN<br />Conflicting results in available data<br />There is a trend towards benefit<br />
  19. 19. References <br />19<br />Acetadote [package insert]. Nashville, TN:Cumberland Pharmaceuticals, Inc.; February 2006.<br />Gurbuz AK, Ozel AM, Ozturk R, Yildirim S, Yazgan Y, Demirturk L. Effect of N-acetyl cysteine on Helicobacter pylori. South Med J. 2005;98:1095-1097<br />Lacy, CF, Armstrong, LL, Goldman, MP, Lance, LL. Drug information handbook.17th ed. Hudson: Lexi-Comp, Inc.; c2008. Acetylcysteine; p. 32-4.<br />N-Acetylcysteine, a Novel Treatment for Helicobacter pylori Infection. Dig Dis Sci. 2004 Nov-Dec;49(11-12):1853-61. <br />Pombrio JM, Giangreco A, Li L, Wempe MF, Anders MW, Sweet DH, Pritchard JB, Ballatori N. Mercapturic acids (N-acetylcysteine S-conjugates) as endogenous substrates for the renal organic anion transporter-1. Mol Pharmacol. 2001 Nov;60(5):1091-9.<br />Up to date online. Prevention of contrast-induced nephropathy. Rudnick, MR, Tumlin, JA. 2009 Sep.<br />Dribben WH, Porto SM, Jeffords BK. Stability and microbiology of inhalant N-acetylcysteine used as an intravenous solution for the treatment of acetaminophen poisoning. Ann Emerg Med. 2003 Jul;42(1):9-13<br />