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Hydrocodone/paracetamol

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Hydrocodone/paracetamol
Combination of
HydrocodoneOpioid analgesic
ParacetamolAnilide analgesic
Clinical data
Trade namesHycet, Lorcet, Lorcet Plus, Lortab, Maxidone, Norco, Vicodin, Vicodin ES, Vicodin HP, Zamicet, and Zydone (possibly others)
AHFS/Drugs.comhydrocodone/paracetamol
Routes of
administration		Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability>80%
Metabolismfor hydrocodone: extensively hepatic, primarily CYP3A4; for acetaminophen: hepatic, CYP2E1
Elimination half-lifefor hydrocodone: 228-294 mins (3.8-4.9 hrs); for acetaminophen: 120-240 mins (2-4 hrs)
Excretionfor hydrocodone: urinary; for acetaminophen: urinary (10-15% unchanged)
Identifiers
PubChem CID
ChemSpider
CompTox Dashboard (EPA)
Chemical and physical data
3D model (JSmol)
  • O=C(Nc1ccc(O)cc1)C.O=C4[C@@H]5Oc1c2c(ccc1OC)C[C@H]3N(CC[C@]25[C@H]3CC4)C
  • InChI=1S/C18H21NO3.C8H9NO2/c1-19-8-7-18-11-4-5-13(20)17(18)22-16-14(21-2)6-3-10(15(16)18)9-12(11)19;1-6(10)9-7-2-4-8(11)5-3-7/h3,6,11-12,17H,4-5,7-9H2,1-2H3;2-5,11H,1H3,(H,9,10)/t11-,12+,17-,18-;/m0./s1 checkY
  • Key:DQGPYIDMOHQZSY-RNWHKREASA-N checkY
  (verify)

Hydrocodone/paracetamol, hydrocodone/acetaminophen, or hydrocodone/APAP (or under brand names such as Lortab, Norco and Vicodin) is a combination opioid narcotic analgesic drug consisting of hydrocodone and paracetamol (acetaminophen) used to relieve moderate to severe pain.[1]

Formulations

Hydrocodone/paracetamol is a two-ingredient combination formula consisting of the opioid hydrocodone and the nonopioid analgesic paracetamol.

Medical uses

Hydrocodone/paracetamol is indicated for relief of moderate to moderately severe pain of acute, chronic or postoperative types.[1]

Side effects

Common side effects of narcotic analgesics are nausea, vomiting, constipation, and dry mouth.[1]

Nonmedical uses

Further information: Hydrocodone § Recreational use

Hydrocodone diversion and recreational use has escalated in recent years. In 2009 and 2010, hydrocodone was the second-most frequently encountered opioid pharmaceutical in drug evidence submitted to U.S. federal, state, and local forensic laboratories as reported by DEA’s National Forensic Laboratory Information System and System to Retrieve Information from Drug Evidence.[2]

Market

In 2007, 99% of hydrocodone was consumed in the United States.[3] It was the most commonly prescribed opioid in the United States as of 2012. About 142 million prescriptions were dispensed in the US for hydrocodone-combination products, and the hydrocodone/acetaminophen combination was the most common of those.[2]

Pharmacodynamics

Hydrocodone acts at μ-opioid receptors.[4] It is metabolized to hydromorphone by the activity of cytochrome P450 2D6. Cytochrome 3A4 forms the substrate norhydrocodone. This conversion is only somewhat responsible for the effects of hydrocodone.[5] Hydrocodone passes through the blood–brain barrier because of its modifications. The brain is typically where the analgesic effects are being carried out. Many of the side effects of this drug are caused because it so readily crosses the blood–brain barrier. The half-life of hydrocodone is around 3.8 hrs.

The major active metabolites of paracetamol are sulphates and glucuronide conjugates. Its main mode of action is to inhibit the activity of the enzyme cyclooxygenase (COX). COX enzymes are necessary for the production of prostaglandins. Prostaglandins are a form of hormone (although rarely classified as such) that are indicated to be mediators of pain, fever, and inflammation. The half-life of paracetamol may be measured either by salivary or by plasma counts. Both measurements give a varying half-life between 1 and 4 hours.[6] Peak levels are reached 40–60 minutes after ingestion. It has been proposed that paracetamol aids in the reduction of pain by increasing serotonergic neurotransmissions.[7]

Regulatory status

United States

Although hydrocodone-containing combination products containing up to 15 mg of hydrocodone per dosage unit had been classified as Schedule III medications in the United States,[8] all hydrocodone-containing products were moved to Schedule II on October 6, 2014.[9]

Politics

Proposed U.S. ban

On June 30, 2009, a U.S. Food and Drug Administration (FDA) advisory panel voted by a narrow margin to advise the FDA to remove Vicodin and another painkiller, Percocet, from the market because of "a high likelihood of overdose from prescription narcotics and acetaminophen products". The panel cited concerns of liver damage from their acetaminophen component, which is also the main ingredient in commonly used nonprescription drugs such as Tylenol.[10] Each year, acetaminophen overdose is linked to about 400 deaths and 42,000 hospitalizations.[11]

In January 2011, the FDA asked manufacturers of prescription combination products that contain acetaminophen to limit the amount of acetaminophen to no more than 325 mg in each tablet or capsule.[12][13][14][15] Manufacturers had three years to limit the amount of acetaminophen in their prescription drug products to 325 mg per dosage unit.[13][15] The FDA also required manufacturers to update labels of all prescription combination acetaminophen products to warn of the potential risk for severe liver injury.[12][13][15]

Manufacture

The opioid constituent hydrocodone has the same basic structure as morphine, but is metabolized by different enzymes. Hydrocodone, like oxycodone, is an intermediate-strength analgesic that has similar effects as morphine; hydrocodone is approximately twice as potent as morphine by mouth for acute use. The theory of using the mix comes from the idea that these drugs alleviate pain using different mechanisms and also that the adverse side effects of each separate drug are reduced by using reduced dosages of both drugs to get the same analgesic effect.[16]

Both hydrocodone and paracetamol are white crystalline powders, which are then manufactured into tablet form.

Hydrocodone/paracetamol, in all strengths by all manufacturers, has been the #1 prescription filled in the US since 2002, with an estimated 136.7 million prescriptions filled in 2011.[17][18]

In popular culture

Television

In the television series House, the titular character Gregory House is addicted to Vicodin as a result of permanent pain in his leg. The theme of addiction is explored throughout the show, and House is often seen taking Vicodin.

See also

References

  1. ^ a b c "Acetaminophen and Hydrocodone". drugs.com.
  2. ^ a b "Hydrocodone (Trade Names: Vicodin, Lortab, Lorcet-HD, Hycodan, Vicoprofen)" (PDF). US DOJ - DEA. April 2013. Retrieved 21 May 2013.
  3. ^ International Narcotics Control Board Report 2008. United Nations Pubns. 2009. p. 20. ISBN 9211482321.
  4. ^ Zacny JP, Gutierrez S, Bolbolan SA (June 2005). "Profiling the subjective, psychomotor, and physiological effects of a hydrocodone/acetaminophen product in recreational drug users". Drug Alcohol Depend. 78 (3): 243–52. doi:10.1016/j.drugalcdep.2004.11.009. PMID 15893155.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  5. ^ "Inhibition of Cytochrome P450 2D6 Metabolism of Hydrocodone to Hydromorphone Does Not Importantly Affect Abuse Liability". aspetjournals.org.
  6. ^ Lee, HS; Ti, TY; Lye, WC; Khoo, YM; Tan, CC (January 1996). "Paracetamol and its metabolites in saliva and plasma in chronic dialysis patients". Br J Clin Pharmacol. 41 (1): 41–7. doi:10.1111/j.1365-2125.1996.tb00157.x. PMID 8824692.
  7. ^ Garrone, B., Polenzani L., De Santi, S., Moreci, W., and Guglielmotti, A. (2007). "Paracetamol reduces neuropathic pain-like behaviour in rats by potentiating serotonergic neurotransmission" (PDF). Int J Integ Biol. 1 (3): 196–205. ISSN 0973-8363.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  8. ^ "Resources - Controlled Substance Schedules". usdoj.gov.
  9. ^ "Federal Register - Schedules of Controlled Substances: Rescheduling of Hydrocodone Combination Products From Schedule III to Schedule II". usa.gov.
  10. ^ "FDA advisers vote to take Vicodin, Percocet off market". cnn.com.
  11. ^ Reasons Not to Panic Over a Painkiller, The New York Times
  12. ^ a b "FDA limits acetaminophen in prescription combination products; requires liver toxicity warnings" (Press release). U.S. Food and Drug Administration. January 13, 2011. Retrieved January 13, 2011.
  13. ^ a b c "FDA Drug Safety Communication: Prescription Acetaminophen Products to be Limited to 325 mg Per Dosage Unit; Boxed Warning Will Highlight Potential for Severe Liver Failure". U.S. Food and Drug Administration (FDA). January 13, 2011. Retrieved January 13, 2011.
  14. ^ Matthew Perrone (January 13, 2011). "FDA orders lowering pain reliever in Vicodin". The Boston Globe. Associated Press. Retrieved January 13, 2011.
  15. ^ a b c Gardiner Harris (January 13, 2011). "F.D.A. Plans New Limits on Prescription Painkillers". The New York Times. Retrieved January 13, 2011.
  16. ^ Beaver WT, McMillan D (October 1980). "Methodological considerations in the evaluation of analgesic combinations: acetaminophen (paracetamol) and hydrocodone in postpartum pain". Br J Clin Pharmacol. 10 Suppl 2: 215S–223S. doi:10.1111/j.1365-2125.1980.tb01803.x. PMC 1430165. PMID 7192153.
  17. ^ "The Use of Medicines in the United States". IMS Institute for Healthcare Informatics. The Use of Medicines in the United States. June 2012. p. 40. Archived from the original (PDF) on 28 September 2012.
  18. ^ Mike McEvoy (June 12, 2008). "Hydrocodone/APAP: Drug Whys". EMS1. Archived from the original on 2012-07-10. Popularity: First most commonly prescribed drug between 2002-2007 (U.S.)

External links

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