Hydrocodone/paracetamol
Combination of | |
---|---|
Hydrocodone | Opioid analgesic |
Paracetamol | Anilide analgesic |
Clinical data | |
Trade names | Lorcet, Norco, Vicodin, others |
Other names | Hydrocodone/acetaminophen, hydrocodone/APAP |
AHFS/Drugs.com | Professional Drug Facts |
License data | |
Routes of administration | By mouth |
ATC code | |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Bioavailability | >80% |
Metabolism | Hydrocodone: extensively liver, primarily CYP3A4; /Paracetamol: liver, CYP2E1 |
Elimination half-life | for hydrocodone: 228–294 mins (3.8–4.9 hrs); for paracetamol: 120–240 mins (2–4 hrs) |
Excretion | for hydrocodone: urinary; for paracetamol: urinary (10–15% unchanged) |
Identifiers | |
CAS Number | |
PubChem CID | |
ChemSpider | |
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Hydrocodone/paracetamol (also known as hydrocodone/acetaminophen) is the combination of the
Common side effects include dizziness, sleepiness,
Hydrocodone/paracetamol was approved for medical use in the United States in 1982.
Uses
Medical
Hydrocodone/paracetamol is a
Recreational
Hydrocodone diversion and recreational use has escalated due to its opioid effects.
Pregnancy and breastfeeding
Prolonged use of hydrocodone/paracetamol during pregnancy can result in neonatal opioid withdrawal syndrome.[1] Hydrocodone/paracetamol passes into breast milk and may harm the baby.[1]
Kidney and liver impairment
Use with caution due to possible risk of toxicity.[1]
Side effects
Most common
- Lightheadedness[2]
- Dizziness[2]
- Euphoria[citation needed]
- Sedation[2]
- Nausea and vomiting[2]
- Headaches
Less common
- Central nervous system: drowsiness, confusion, lethargy, anxiety, fear, unease, dependence, mood changes, impairment of mental and physical performance[2]
- Gastrointestinal system: constipation[2]
- Genitourinary system: inability to urinate, bladder spasms[2]
- Respiratory depression: decreased rate and effort of breathing[2]
- Hearing impairment, permanent hearing loss[2]
- Dermatological: rash, itching[2]
Black box warning
"Paracetamol has been associated with cases of acute liver failure, at times resulting in liver transplant and death. Most of the cases of liver injury are associated with the use of paracetamol at doses that exceed 4000 milligrams per day, and often involve more than one paracetamol-containing product."[2]
In the US, the label for hydrocodone/paracetamol contains a
Overdose
Hydrocodone: Respiratory depression, extreme somnolence progressing towards coma, muscle limpness, cold and clammy skin, slow heart rate, low blood pressure, abrupt loss of heart function, and death may occur.[2]
Paracetamol: Liver and kidney failure, low blood sugar coma may occur.[2]
Interactions
Hydrocodone may demonstrate an enhanced respiratory depressant effect when combined with other sedatives such as other opioids, benzodiazepines, nonbenzodiazepine sedatives, psychotropics, and anticonvulsants.[14]
Concurrent use of paracetamol with alcohol products may increase the risk of acute liver failure.[2]
Monitoring
Laboratory function tests should be used to monitor therapy in people with severe liver or renal disease.[2]
Pharmacology
Hydrocodone
- Mechanism of action: Hydrocodone acts primarily as an agonist at the mu-opioid receptors, but is also a weak agonist against the delta opioid and kappa opioid receptors.[15]
- Absorption/distribution: The oral formulation can be absorbed from the gastrointestinal tract and remain 20–50% bound to plasma proteins.[15] The onset of analgesia is about 20 to 30 minutes with duration of 4 to 8 hours and t1/2 of 3 to 4 hours.[15] Maximum serum levels are achieved at 1.3 hours.[16]
- Metabolism/excretion: It is metabolized to
- Metabolites: Hydromorphone, the major active metabolite, has a 10-33-fold higher binding affinity for the mu-opioid receptor than hydrocodone. It may be up to >100-fold higher in some patients.[19]
Paracetamol
- Mechanism of action: Paracetamol acts to inhibit COX enzyme, which is responsible for prostaglandin synthesis.[6] Prostaglandins increase the perception of pain. Inhibition of prostaglandin production helps to alleviate pain.[20]
- Absorption/distribution: The half-life of oral paracetamol is 1.25 to 3 hours and peak level is reached by 10–60 minutes after ingestion.[21]
- Metabolism/excretion: Paracetamol is metabolized primarily in the liver via glucuronidation and sulfation to mostly non-toxic metabolites and some highly reactive metabolites, which is inactivated by glutathione.[21] 85% of the oral dose is excreted via the kidneys.[2] At high doses, the supply of glutathione cannot meet its demand, thus results in the accumulation of highly reactive compounds leading to liver damage.[21]
Society and culture
Legal status
On 30 June 2009, a U.S.
In January 2011, the FDA asked manufacturers of prescription combination products that contain paracetamol to limit the amount of paracetamol to no more than 325 mg in each tablet or capsule within three years.[24][25][26][27] The FDA also required manufacturers on all paracetamol containing products to issue a black box warning indicating the potential risk for severe liver injury and a warning highlighting potential for allergic reactions.[24][25][27]
On 22 August 2014, the Drug Enforcement Administration (DEA) announced that all hydrocodone combination products (HCPs) will be rescheduled from Schedule III to Schedule II of the Controlled Substances Act (CSA), effective on 6 October 2014.[11] In 2010, more than 16,000 deaths were attributed to abuse of opioid drugs.[11] Even though there are legitimate medical uses for HCPs, data suggest that a significant number of individuals misuse them.[11]
Popular culture
Actor Matthew Perry struggled with his addiction to Vicodin for many years after a jetski accident in 1997.[28]
In May 2017,
Brand names
Brand names include Adol, Hycet, Lortab, Lorcet, Norco, and Vicodin among others.[33]
References
- ^ a b c d e f g h i j k l m n o p q "Norco (Hydrocodone Bitartrate and Acetaminophen Tablets, USP) CII Revised: March 2021". DailyMed. Retrieved 23 November 2022.
- ^ a b c d e f g h i j k l m n o p q r s t "Vicodin Vicodin ES Vicodin HP (Hydrocodone Bitartrate and Acetaminophen Tablets, USP) Rx only CS-II". DailyMed. Retrieved 23 November 2022.
- ^ ISBN 9780763781170.
- ISBN 9781412941655.
- PMID 23709306.
- ^ S2CID 38261222.
- ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
- ^ "Acetaminophen; Hydrocodone - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
- ^ Atkins L (16 August 2001). "Know what a Vike is?". The Guardian. Retrieved 23 December 2018.
- ^ "Co-codamol 30/500 Tablets - Summary of Product Characteristics (SmPC) - (eMC)". www.medicines.org.uk. Retrieved 7 August 2019.
- ^ a b c d "Schedules of Controlled Substances: Rescheduling of Hydrocodone Combination Products From Schedule III to Schedule II". Federal Register. 22 August 2014. Retrieved 23 November 2022. This article incorporates text from this source, which is in the public domain.
- ^ "Norco Addiction". The Fix. 21 January 2015. Retrieved 4 November 2015.
- ^ "Hydrocodone (Trade Names: Vicodin, Lortab, Lorcet-HD, Hycodan, Vicoprofen)" (PDF). Drug Enforcement Administration. April 2013. Archived (PDF) from the original on 18 April 2013. Retrieved 21 May 2013.
- PMID 21410363.
- ^ PMID 21785485.
- ^ "Labeling-Package Insert: Hydrocodone/acetaminophen 7.5 mg/325 mg" (PDF). Drugs@FDA: FDA-Approved Drugs. Chartwell. 18 October 2013. Retrieved 22 January 2024.
- PMID 28931.
- ^ ISBN 9781461489481.
- ^ Hydrocodone and acetaminophen (paracetamol): Drug information (Version 390.0 ed.). Lexicomp®. 2024.
- ISBN 978-0-7817-8355-2.
- ^ ISBN 978-0-521-14450-6.
- ^ a b "FDA advisers vote to take Vicodin, Percocet off market". CNN.
- ISSN 0362-4331. Retrieved 4 November 2015.
- ^ a b "FDA limits acetaminophen in prescription combination products; requires liver toxicity warnings" (Press release). U.S. Food and Drug Administration. 13 January 2011. Retrieved 13 January 2011.
- ^ U.S. Food and Drug Administration(FDA). 13 January 2011. Retrieved 13 January 2011.
- ^ Perrone M (13 January 2011). "FDA orders lowering pain reliever in Vicodin". The Boston Globe. Associated Press. Retrieved 13 January 2011.
- ^ a b Harris G (13 January 2011). "F.D.A. Plans New Limits on Prescription Painkillers". The New York Times. Retrieved 13 January 2011.
- ISSN 0307-1235. Retrieved 17 December 2023.
- ^ "Police release dashcam footage of Tiger Woods' DUI arrest". Guardian. Associated press. 1 June 2017. Retrieved 1 June 2017.
- ^ Murray E (29 May 2017). "Tiger Woods says medication, not alcohol led to Florida DUI arrest". The Guardian. Retrieved 1 June 2017.
- ^ "Pilot". House, M.D. Season 1. Episode 1. 16 November 2004.
- ^ "Twenty Vicodin". House, M.D. Season 8. Episode 1. 3 October 2011.
- ^ "Adol (Hydrocodone-Acetaminoph) Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing – WebMD". WebMD. Retrieved 26 July 2017.
External links
- Vicodin U.S. Federal Regulations Archived 18 January 2017 at the Wayback Machine