Opium alkaloids and derivatives
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Opium alkaloids
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Phenanthrenes naturally occurring in (opium):
Preparations of mixed opium alkaloids, including papaveretum, are still occasionally used.
Esters of morphine
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Diacetylmorphine (morphine diacetate; heroin)
Nicomorphine (morphine dinicotinate)
Dipropanoylmorphine (morphine dipropionate)
Ethers of morphine
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Semi-synthetic alkaloid derivatives
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Oxycodone (sold as OxyContin)
Synthetic opioids
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Anilidopiperidines
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Fentanyl (see also list of fentanyl analogues)
Benzimidazoles
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Main article: List of benzimidazole opioids
Benzimidazoles opioids are also known as nitazenes.
Metodesnitazene (Metazene)
Etodesnitazene (Etazene)
Phenylpiperidines
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Diphenylpropylamine derivatives
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Levomethadyl acetate (LAAM)
Loperamide (does cross the blood–brain barrier but is quickly pumped into the non-central nervous system by P-Glycoprotein. Mild opiate withdrawal in animal models exhibits this action after sustained and prolonged use including rhesus monkeys, mice, and rats.)
Benzomorphan derivatives
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Dezocine—agonist/antagonist
Pentazocine—agonist/antagonist
Oripavine derivatives
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Buprenorphine—partial agonist
Morphinan derivatives
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Butorphanol—agonist/antagonist
Nalbuphine—agonist/antagonist
Others
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Allosteric modulators
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Plain allosteric modulators do not belong to the opioids, instead they are classified as opioidergics.
Opioid antagonists
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Methylnaltrexone (Methylnaltrexone is only peripherally active as it does not cross the blood–brain barrier in sufficient quantities to be centrally active. As such, it can be considered the antithesis of loperamide.)
Naloxegol (Naloxegol is only peripherally active as it does not cross the blood–brain barrier in sufficient quantities to be centrally active. As such, it can be considered the antitheses of loperamide.)