Oxycodone/naloxone

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Oxycodone/naloxone
Oxycodone.svg
Naloxone.svg
Combination of
Oxycodone Opioid analgesic
Naloxone Opioid receptor antagonist
Clinical data
Trade names Targin, Targiniq, Targinact, others
AHFS/Drugs.com International Drug Names
UK Drug Information
License data
Pregnancy
category
  • AU:C
Routes of
administration
By mouth
ATC code
Legal status
Legal status
Identifiers
CAS Number
   (verify)

Oxycodone/naloxone, sold under the brand name Targin among others, is a combination pain medication available as modified-release tablets administered by mouth. [5]

The oxycodone component is an opioid and is responsible for the pain-relieving effects. Naloxone, an opioid antagonist, opposes the effects of opioids but is poorly absorbed into the blood stream when administered orally; therefore, most of the dose remains in the gastrointestinal tract. This local presence reduces opioid-induced constipation by preventing oxycodone from binding to gut opioid receptors, without diminishing overall analgesic efficacy compared to oxycodone alone. A 2008 study demonstrated a significant reduction in constipation. [6] Oxycodone/naloxone was released in 2014 in the United States, [5] in 2006 in Germany, and has been available in some other European countries since 2009. In the United Kingdom, the 10 mg oxycodone / 5 mg naloxone and 20 mg / 10 mg strengths were approved in December 2008, and the 40 mg / 20 mg and 5 mg / 10 mg strengths received approval in July 2019. [7]

Preliminary evidence suggests that oxycodone/naloxone may be an effective treatment for severe, refractory restless legs syndrome if first-line therapies have not been effective. [8] [9] [10]

Adverse effects

Related Research Articles

<span class="mw-page-title-main">Hydrocodone</span> Opioid drug used in pain relief

Hydrocodone, also known as dihydrocodeinone, is a semi-synthetic opioid used to treat pain and as a cough suppressant. It is taken by mouth. Typically, it is dispensed as the combination acetaminophen/hydrocodone or ibuprofen/hydrocodone for pain severe enough to require an opioid and in combination with homatropine methylbromide to relieve cough. It is also available by itself in a long-acting form sold under the brand name Zohydro ER, among others, to treat severe pain of a prolonged duration. Hydrocodone is a controlled drug: in the United States, it is classified as a Schedule II Controlled Substance.

<span class="mw-page-title-main">Methadone</span> Opioid medication

Methadone, sold under the brand names Dolophine and Methadose among others, is a synthetic opioid used medically to treat chronic pain and opioid use disorder. Prescribed for daily use, the medicine relieves cravings and opioid withdrawal symptoms. Withdrawal management using methadone can be accomplished in less than a month, or it may be done gradually over a longer period of time, or simply maintained for the rest of the patient's life. While a single dose has a rapid effect, maximum effect can take up to five days of use. After long-term use, in people with normal liver function, effects last 8 to 36 hours. Methadone is usually taken by mouth and rarely by injection into a muscle or vein.

<span class="mw-page-title-main">Oxycodone</span> Opioid medication

Oxycodone, sold under the brand name Roxicodone and OxyContin among others, is a semi-synthetic opioid used medically for the treatment of moderate to severe pain. It is highly addictive and is a commonly abused drug. It is usually taken by mouth, and is available in immediate-release and controlled-release formulations. Onset of pain relief typically begins within fifteen minutes and lasts for up to six hours with the immediate-release formulation. In the United Kingdom, it is available by injection. Combination products are also available with paracetamol (acetaminophen), ibuprofen, naloxone, naltrexone, and aspirin.

<span class="mw-page-title-main">Naloxone</span> Opioid receptor antagonist

Naloxone is an opioid antagonist: a medication used to reverse or reduce the effects of opioids. For example, it is used to restore breathing after an opioid overdose. It is also known as Narcan. Effects begin within two minutes when given intravenously, five minutes when injected into a muscle, and ten minutes as a nasal spray. Naloxone blocks the effects of opioids for 30 to 90 minutes.

<span class="mw-page-title-main">Tramadol</span> Opioid pain medication

Tramadol, sold under the brand name Ultram among others, is an opioid pain medication and a serotonin–norepinephrine reuptake inhibitor (SNRI) used to treat moderately severe pain. When taken by mouth in an immediate-release formulation, the onset of pain relief usually begins within an hour. It is also available by injection. It is available in combination with paracetamol (acetaminophen).

<span class="mw-page-title-main">Hydromorphone</span> Opioid medication used for pain relief

Hydromorphone, also known as dihydromorphinone, and sold under the brand name Dilaudid among others, is a morphinan opioid used to treat moderate to severe pain. Typically, long-term use is only recommended for pain due to cancer. It may be used by mouth or by injection into a vein, muscle, or under the skin. Effects generally begin within half an hour and last for up to five hours. A 2016 Cochrane review found little difference in benefit between hydromorphone and other opioids for cancer pain.

<span class="mw-page-title-main">Opioid</span> Psychoactive chemical

Opioids are a class of drugs that derive from, or mimic, natural substances found in the opium poppy plant. Opioids work in the brain to produce a variety of effects, including pain relief. As a class of substances, they act on opioid receptors to produce morphine-like effects.

<span class="mw-page-title-main">Clonidine</span> Pharmaceutical drug

Clonidine, sold under the brand name Catapres among others, is an α2A-adrenergic receptor agonist medication used to treat high blood pressure, ADHD, drug withdrawal, menopausal flushing, diarrhea, spasticity, and certain pain conditions. The drug is often prescribed off-label for tics. It is used orally, by injection, or as a transdermal skin patch. Onset of action is typically within an hour with the effects on blood pressure lasting for up to eight hours.

Oxycodone/aspirin is a combination drug marketed by Endo Pharmaceuticals. It is a tablet containing a mixture of 325 mg of aspirin and 4.8355 mg of oxycodone HCl ; it is an opioid/non-opioid combination used to treat moderate to moderately severe pain. The safety of the combination during pregnancy has not been established, although aspirin is generally contraindicated during pregnancy, and the drug has been placed in pregnancy category D. Inactive ingredients include D&C Yellow 10, FD&C Yellow 6, microcrystalline cellulose, and corn starch. Percodan was first marketed by DuPont Pharmaceuticals and prescribed in the United States in 1950. Once a widely prescribed painkiller, it has largely been replaced by alternative oxycodone compounds containing paracetamol (acetaminophen) instead of aspirin, such as Percocet.

<span class="mw-page-title-main">Buprenorphine</span> Opioid used to treat pain & opioid use disorder

Buprenorphine, sold under the brand name Subutex among others, is an opioid used to treat opioid use disorder, acute pain, and chronic pain. It can be used under the tongue (sublingual), in the cheek (buccal), by injection, as a skin patch (transdermal), or as an implant. For opioid use disorder, the patient must have moderate opioid withdrawal symptoms before buprenorphine can be administered under direct observation of a health-care provider.

<span class="mw-page-title-main">Oxymorphone</span> Opioid analgesic drug

Oxymorphone is a highly potent opioid analgesic indicated for treatment of severe pain. Pain relief after injection begins after about 5–10 minutes, after oral administration it begins after about 30 minutes, and lasts about 3–4 hours for immediate-release tablets and 12 hours for extended-release tablets. The elimination half-life of oxymorphone is much faster intravenously, and as such, the drug is most commonly used orally. Like oxycodone, which metabolizes to oxymorphone, oxymorphone has a high potential to be abused.

<span class="mw-page-title-main">Dihydrocodeine</span> Opioid

Dihydrocodeine is a semi-synthetic opioid analgesic prescribed for pain or severe dyspnea, or as an antitussive, either alone or compounded with paracetamol (acetaminophen) or aspirin. It was developed in Germany in 1908 and first marketed in 1911.

<span class="mw-page-title-main">Dextropropoxyphene</span> Withdrawn opioid medication

Dextropropoxyphene is an analgesic in the opioid category, patented in 1955 and manufactured by Eli Lilly and Company. It is an optical isomer of levopropoxyphene. It is intended to treat mild pain and also has antitussive and local anaesthetic effects. The drug has been taken off the market in Europe and the US due to concerns of fatal overdoses and heart arrhythmias. It is still available in Australia, albeit with restrictions after an application by its manufacturer to review its proposed banning. Its onset of analgesia is said to be 20–30 minutes and peak effects are seen about 1.5–2.0 hours after oral administration.

<span class="mw-page-title-main">Nalbuphine</span> Opioid analgesic

Nalbuphine, sold under the brand names Nubain among others, is an opioid analgesic which is used in the treatment of pain. It is given by injection into a vein, muscle, or fat.

<span class="mw-page-title-main">Tilidine</span> Synthetic opioid painkiller

Tilidine, sold under the brand name Valoron among others, is a synthetic opioid analgesic, used mainly in Belgium, Bulgaria, Germany, Albania, Luxembourg, South Africa, and Switzerland for the treatment of moderate to severe pain, both acute and chronic. Its onset of pain relief after oral administration is about 10–15 minutes and peak relief from pain occurs about 25–50 minutes after administration.

<span class="mw-page-title-main">Tapentadol</span> Opioid analgesic of benzenoid class

Tapentadol, sold under the brand names Nucynta and Palexia among others, is a synthetic opioid analgesic of the benzenoid class with a dual mode of action as a highly selective full agonist of the μ-opioid receptor and as a norepinephrine reuptake inhibitor (NRI). Tapentadol is used medically for the treatment of moderate to severe pain. It is addictive, a commonly abused drug, and poses a high risk of physical and/or mental dependence.

<span class="mw-page-title-main">Hydrocodone/ibuprofen</span> Combination drug

Hydrocodone/ibuprofen (INNs), sold under the brand name Vicoprofen, is a fixed-dose combination analgesic medication used in short-term therapy to relieve severe pain. Vicoprofen combines the analgesic and antitussive properties of hydrocodone with the analgesic, anti-inflammatory, and antipyretic properties of ibuprofen. In contrast to hydrocodone/acetaminophen combination analgesics such as Vicodin, this hydrocodone/ibuprofen avoids some of the liver toxicity which may occur from acetaminophen, but still presents significant dangers in hydrocodone overdose, namely respiratory depression. Vicoprofen is supplied in a fixed dose combination tablet which contains hydrocodone bitartrate, USP 7.5 mg with ibuprofen, USP 200 mg. Additional strengths of generic Vicoprofen are now available, in combinations of 5 mg/200 mg and 10 mg/200 mg respectively.

<span class="mw-page-title-main">Naloxegol</span> Medication used in the treatment for Opioid-Induced Constipation

Naloxegol is a peripherally acting μ-opioid receptor antagonist developed by AstraZeneca, licensed from Nektar Therapeutics, for the treatment of opioid-induced constipation. It was approved in 2014 in adult patients with chronic, non-cancer pain. Doses of 25 mg were found safe and well tolerated for 52 weeks. When given concomitantly with opioid analgesics, naloxegol reduced constipation-related side effects, while maintaining comparable levels of analgesia.

<span class="mw-page-title-main">Buprenorphine/naloxone</span> Opioid treatment

Buprenorphine/naloxone, sold under the brand name Suboxone among others, is a fixed-dose combination medication that includes buprenorphine and naloxone. It is used to treat opioid use disorder, and reduces the mortality of opioid use disorder by 50%. It relieves cravings to use and withdrawal symptoms. Buprenorphine/­naloxone is available for use in two different forms, under the tongue or in the cheek.

References

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  2. "Oxonal (AU Pharma Pty Ltd)". Therapeutic Goods Administration (TGA). 28 September 2022. Archived from the original on 18 March 2023. Retrieved 9 April 2023.
  3. "Targin Product information". Health Canada. 22 October 2009. Archived from the original on 29 April 2023. Retrieved 9 April 2023.
  4. "Targinact 5 mg/2.5 mg prolonged-release tablets - Summary of Product Characteristics (SmPC)". (emc). 16 March 2021. Archived from the original on 10 April 2023. Retrieved 9 April 2023.
  5. 1 2 3 "Targiniq ER- oxycodone hydrochloride/naloxone hydrochloride tablet, film coated, extended release". DailyMed. 22 December 2016. Archived from the original on 18 March 2023. Retrieved 18 March 2023.
  6. Simpson K, Leyendecker P, Hopp M, Müller-Lissner S, Löwenstein O, De Andrés J, et al. (December 2008). "Fixed-ratio combination oxycodone/naloxone compared with oxycodone alone for the relief of opioid-induced constipation in moderate-to-severe noncancer pain". Current Medical Research and Opinion. 24 (12): 3503–3512. doi:10.1185/03007990802584454. PMID   19032132. S2CID   73061000. Archived from the original on 26 January 2013. Retrieved 9 April 2009.{{cite journal}}: CS1 maint: overridden setting (link)
  7. Mundipharma (26 January 2009). "Targin (oral oxycodone/naloxone prolonged-release tablet) now launching across Europe to control severe chronic pain with significantly reduced risk of opioid-induced constipation". Archived from the original on 17 March 2009. Retrieved 9 April 2009.
  8. de Biase S, Valente M, Gigli GL (2016). "Intractable restless legs syndrome: role of prolonged-release oxycodone-naloxone". Neuropsychiatric Disease and Treatment. 12: 417–425. doi: 10.2147/NDT.S81186 . PMC   4770072 . PMID   26966363.
  9. Trenkwalder C, Beneš H, Grote L, García-Borreguero D, Högl B, Hopp M, et al. (December 2013). "Prolonged release oxycodone-naloxone for treatment of severe restless legs syndrome after failure of previous treatment: a double-blind, randomised, placebo-controlled trial with an open-label extension". The Lancet. Neurology. 12 (12): 1141–1150. doi:10.1016/S1474-4422(13)70239-4. PMID   24140442. S2CID   35122538.{{cite journal}}: CS1 maint: overridden setting (link)
  10. de Oliveira CO, Carvalho LB, Carlos K, Conti C, de Oliveira MM, Prado LB, et al. (June 2016). "Opioids for restless legs syndrome". The Cochrane Database of Systematic Reviews. 2016 (6): CD006941. doi:10.1002/14651858.CD006941.pub2. PMC   6885031 . PMID   27355187.