Katana VentraIP

Opioid

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.[2][3]

The terms 'opioid' and 'opiate' are sometimes used interchangeably, but there are key differences based on the manufacturing processes of these medications.[4]


Medically they are primarily used for pain relief, including anesthesia.[5] Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, reversing opioid overdose, and suppressing cough.[5] Extremely potent opioids such as carfentanil are approved only for veterinary use.[6][7][8] Opioids are also frequently used recreationally for their euphoric effects or to prevent withdrawal.[9] Opioids can cause death and have been used for executions in the United States.


Side effects of opioids may include itchiness, sedation, nausea, respiratory depression, constipation, and euphoria. Long-term use can cause tolerance, meaning that increased doses are required to achieve the same effect, and physical dependence, meaning that abruptly discontinuing the drug leads to unpleasant withdrawal symptoms.[10] The euphoria attracts recreational use, and frequent, escalating recreational use of opioids typically results in addiction. An overdose or concurrent use with other depressant drugs like benzodiazepines commonly results in death from respiratory depression.[11]


Opioids act by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract. These receptors mediate both the psychoactive and the somatic effects of opioids. Opioid drugs include partial agonists, like the anti-diarrhea drug loperamide and antagonists like naloxegol for opioid-induced constipation, which do not cross the blood–brain barrier, but can displace other opioids from binding to those receptors in the myenteric plexus.


Because opioids are addictive and may result in fatal overdose, most are controlled substances. In 2013, between 28 and 38 million people used opioids illicitly (0.6% to 0.8% of the global population between the ages of 15 and 65).[12] In 2011, an estimated 4 million people in the United States used opioids recreationally or were dependent on them.[13] As of 2015, increased rates of recreational use and addiction are attributed to over-prescription of opioid medications and inexpensive illicit heroin.[14][15][16] Conversely, fears about overprescribing, exaggerated side effects, and addiction from opioids are similarly blamed for under-treatment of pain.[17][18]

Medical uses[edit]

Pain[edit]

The weak opioid codeine, in low doses and combined with one or more other drugs, is commonly available in prescription medicines and without a prescription to treat mild pain.[26][27][28] Other opioids are usually reserved for the relief of moderate to severe pain.[27]

[76][77][78]

calcium channel blockers

magnesium[79][80] and zinc[81]

intrathecal

such as dextromethorphan, ketamine,[82] and memantine.[83]

NMDA antagonists

such as proglumide[84][85][86]

cholecystokinin antagonists

Newer agents such as the ibudilast have also been researched for this application.[87]

phosphodiesterase inhibitor

Natural : alkaloids contained in the resin of the opium poppy, primarily morphine, codeine, and thebaine, but not papaverine and noscapine which have a different mechanism of action

opiates

opiates: slightly chemically altered but more natural than the semi-synthetics, as most are morphine prodrugs, diacetylmorphine (morphine diacetate; heroin), nicomorphine (morphine dinicotinate), dipropanoylmorphine (morphine dipropionate), desomorphine, acetylpropionylmorphine, dibenzoylmorphine, diacetyldihydromorphine;[261][262]

Esters of morphine

: created from either the natural opiates or morphine esters, such as hydromorphone, hydrocodone, oxycodone, oxymorphone, ethylmorphine and buprenorphine;

Semi-synthetic opioids

: such as fentanyl, pethidine, levorphanol, methadone, tramadol, tapentadol, and dextropropoxyphene;

Fully synthetic opioids

opioid peptides, produced naturally in the body, such as endorphins, enkephalins, dynorphins, and endomorphins.

Endogenous

Endogenous opioids, non-peptide: Morphine, and some other opioids, which are produced in small amounts in the body, are included in this category.

Natural opioids, non-animal, non-opiate: the leaves from (kratom) contain a few naturally-occurring opioids, active via Mu- and Delta receptors. Salvinorin A, found naturally in the Salvia divinorum plant, is a kappa-opioid receptor agonist.[263]

Mitragyna speciosa

Froehde reagent

Opiate comparison

Opioid epidemic

Opioid tapering

Archived 10 August 2018 at the Wayback Machine—Information about Opioid and opiate withdrawal issues

Opioid Withdrawal Symptoms

World Health Organization guidelines for the availability and accessibility of controlled substances

CDC Guideline for Prescribing Opioids for Chronic Pain — United States, 2016

Reference list to the previous publication

Links to all language versions of the previous publication

Video: Opioid side effects (YouTube)—A short educational film about the practical management of opioid side effects.

(Vimeo)