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

The oxycodone component is an opioid and is responsible for the pain-relieving effects. Naloxone opposes the effects of opioids but is poorly absorbed into the body when given orally, meaning almost all the dose stays within the gastrointestinal tract and reduces the local side effects from the oxycodone, namely constipation as the naloxone binds to the opioid receptors in the gut, preventing the opioid from attaching. This does not affect its analgesic efficacy compared to Oxycontin. Constipation was significantly relieved in a 2008 study. [6] The drug was released in 2006 in Germany and is available in some other European countries since 2009. In the UK, 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 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 an 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 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 a Schedule II Controlled Substance.

<span class="mw-page-title-main">Methadone</span> Opioid medication used for pain; also to treat opioid use disorder

Methadone, sold under the brand names Dolophine and Methadose among others, is a synthetic opioid agonist used for chronic pain and also for opioid use disorder. It is used to treat chronic pain, and it is also used to treat addiction to heroin or other opioids. Prescribed for daily use, the medicine relieves cravings and removes 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 various brand names such as Roxicodone and OxyContin, is a strong, semi-synthetic opioid used medically for 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 a medication used to reverse or reduce the effects of opioids sold under various brands. It is used to counter decreased breathing in opioid overdose. Effects begin within two minutes when given intravenously, and within five minutes when injected into a muscle. The medicine can also be administered by spraying it into a person's nose. Naloxone blocks the effects of opioids for 30 to 90 minutes. Multiple doses may be required, as the duration of action of some opioids is greater than that of naloxone. Emergency medical services data from Massachusetts found that 93.5% of people given naloxone survived their overdose.

<span class="mw-page-title-main">Tramadol</span> Medication of the opioid type

Tramadol, sold under the brand name Ultram among others, is an opioid pain medication 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 drug 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.

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, it is typically started when withdrawal symptoms have begun and for the first two days of treatment under direct observation of a health-care provider.

<span class="mw-page-title-main">Oxymorphone</span> Chemical compound

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">Ropinirole</span> Medication

Ropinirole, sold under the brand name Requip among others, is a medication used to treat Parkinson's disease (PD) and restless legs syndrome (RLS). In PD the dose needs to be adjusted to the effect and treatment should not be suddenly stopped. It is taken by mouth.

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

Tilidine, Leart or tilidate is a synthetic opioid painkiller, used mainly in Belgium, Bulgaria, Germany, 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 oral administration.

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

Tapentadol, brand names Nucynta among others, is a centrally acting opioid analgesic of the benzenoid class with a dual mode of action as an agonist of the μ-opioid receptor and as a norepinephrine reuptake inhibitor (NRI). Analgesia occurs within 32 minutes of oral administration, and lasts for 4–6 hours.

<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">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.

Clinical Opiate Withdrawal Scale (COWS) is a method used by registered practitioners to measure the severity of a patient's opioid withdrawal symptoms. This method consists of a series of 11 topics each comprising 4 - 5 common symptoms experienced by a patient undergoing opioid withdrawal. In each topic a rank is given depending on what the patient responds to. Generally, 0 is considered to be no symptom shown and 4 or 5 is considered to be the most common and severe symptom shown. These results are then added up and a final diagnosis is made based on the value obtained. This test is crucial as it allows the practitioner to assess the physiological and psychological behaviours of the patient as well as the severity of each symptom during the duration of the examination. The results are grouped into 3 categories of mild, moderately severe and severe. Mild consists of 5 to 12 points, moderately severe consists of 13 to 24 points and anything above 36 points is severe and requires direct medical attention.

References

  1. http://www.ebs.tga.gov.au/servlet/xmlmillr6?dbid=ebs/PublicHTML/pdfStore.nsf&docid=355284&agid=%28PrintDetailsPublic%29&actionid=1 [ bare URL ]
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  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 "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 2013-01-26. Retrieved 2009-04-09.
  7. Mundipharma (2009-01-26). "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 2009-03-17. Retrieved 2009-04-09.
  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.
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  10. de Oliveira CO, Carvalho LB, Carlos K, Conti C, de Oliveira MM, Prado LB, Prado GF (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.