Opioid Notes

Opium Alkaloids

Thebaine - 6,14 Dimethoxy version of Oxymorphone. Stimulant rather than an analgesic.

Narceine - Bitter, Crystalline, formerly used as a substitute for Morphine.

Noscapine - Acts on the Sigma receptor. Non painkilling. Used commonly in Antitussives. Blocks Bradykinine B-2 receptors in Stroke patients.

Alkaloid Salt Mixtures

Pantopon - Preparation of all alkaloids present in opium without plant matter. Injectable and slightly less potent than Morphine.

Morphine Family

6-MDDM - 80x the potency of Morphine, has a faster onset and less body load then the prior.

Azidomorphine - 40x the potency of Morphine, has a high affinity for μ.

Hydromorphinol - Derivative of Morphine, yet more potent, with a steeper-dose-response curve and a longer half life. Scripted in Sweden.

Methyldesorphin - 15x the potency of Morphine. Is found in some mixtures of Krokodil.

MR-2096 - Oxymorphone analogue that is roughly the same potency.

N-Phenethylnormorphine - 8-14x the potency of Morphine.

RAM-378 - N-Phenethyl analogue of Hydromorphinol. It is probably more potent as a result.

3,6 Morphine Diesters

Diacetyldihydromorphine - Occasionally used as an alternative to diamorphine, of which it is faster acting, longer lasting and has less side effects such as euphoria and addiction. However it is equipotent with Morphine.

Dipropanoylmorphine - Ester of Morphine used to treat severe pain. Rarely used but considered to be safer and less addictive than Morphine. As such carries less side effects, such as euphoria. Slower acting, longer lasting and slightly more potent than Morphine.

Nicomorphone - 2-3x the potency of Morphine and commonly prescribed in German speaking countries.

Codeine-Dionine Family

Heterocodeine - Reverse isomer of codeine. 6x the potency of Morphine, while Codeine is a prodrug, Heterocodeine is a direct agonist.

Myrophine - Acts as a prodrug to Morphine. Has a slow onset and longer duration, but reduced potency. Does NOT produce addiction or dependence regardless of dose.

Acetyldihydrocodeine - Used in Germany. Close relative of Thebacon, where only the 6-7 cond is unsaturated. 6-Acetyl derivative of Dihydrocodeine. Metabolizes into Dihydromorphine. Higher lipophilicity than codeine. Would probably be more potent and longer lasting as a result. Higher oral BA than Codeine.

Morphinones and Morphols

14-Cinnamoyloxycodeinone - 100x the potency of Morphine.

14-Methoxymetopon - 500x the potency of Morphine. Can be up to one million times the potency of Morphine if injected into the spine.

14-Phenylpropoxymetopon - 2000x potency of Morphine. When injected into the spine up to one million times the potency of Morphine. 14-Methoxymetopon has a ceiling effect on respiratory depression, but the above has been left untested.

3-Acetyloxymorphone - Acetylated analogue of Oxymorphone.

7-Spiroindanyloxymorphone - Odd Oxymorphone analogue that is selective at dopamine.

Acetylmorphone - Acetoxy version of Hydromorphone, has a higher bioavailability as a result.

Chloroxymorphamine - Derivative of Oxymorphone and irreversible full agonist.

Methyldihydromorphone - Related to Heterocodieine not dihydrocodeine. Is 6-9x the potency of Morphine.

Metopon - Methylated Hydromorphone, less potent. More than likely would have more euphoria as a result.

N-Phenethyl-14-Ethoxymetopon - 60x the potency of Morphine, but produces less constipation. d & u agonist.

Oxymorphol - 6-Hydrogenated Oxymorphone.

Pentamorphone - Few times more potent than Fentanyl. Short duration, yet low respiratory depression.

Semorphone - 2 times the potency of Morphine. Partial u agonist and has a ceiling effect on both analgesia and respiratory depression.

Thebacon - Thebaine analogue, that is fairly uninteresting. 6-8x the potency of Codeine.

Hydrazones

Oxymorphazone - Half the potency of Oxymorphone, yet higher doses last up to 48 hours.

Morphians

Butorphanol - partial ant.-ag. at μ opioid and competitive antagonist/partial agonist at κ opioid. dysphoria is common at normal dose.

Drotebanol - Morphinan derivative synthesised from Thebaine with analgesic effects several times more potent than codeine but weaker than morphine. Moderately addictive but limited physical dependance. Under Metabanyl when available as a script.

Dextromethorphan (-) - NMDA antagonist / σ1 & σ2 sigma agonist / a3b4, a4b2, a7 nACH antagonist, (very weak) μ, δ & κ opioid agonist, SERT & NET inhibitor, NADPH Oxidase inhibitor. (Race)Methorphan = racemic

Dextrorphan (-) - NMDA antagonist / σ1 & σ2 sigma agonist / a3b4, a4b2, a7 nACH antagonist, L-Type voltage-gated calcium channel (LVGCC) blocker, SRI.

Cyclorphan - mixed antagonist-agonist with affinity for κ

Levophenacylmorphan - 10x potency of M

Levofurethylnormorphanol (Ro4-1539) - potent μ opioid agonist 30-60x potency of Levorphanol.

Levomethorphan (+) - NDMA antagonist, σ1 & σ2 sigma agonist, μ, δ & κ opioid agonist.

Levorphanol (+) - μ, κ & δ agonist, 4-8x potency of M, long duration, no cross tolerance with morphine

Norlevorphanol - Opioid analgesic, uninteresting.

Phenomorphan - 10x potency of Levorphanol.

└--> N-(2-(2-furyl)ethyl) analogue - 60x Levorphanol └--> N-(2-(2-thienyl)ethyl) analogue - 45x Levorphanol

Proxorphan - partial κ agonist, lesser partial μ agonist

Ro4-1539 (Furethylnorlevorphanol) - 30-60x the potency of M. One of the more potent u agonists from the Morphans.

(Race)Methorphan: L(eft) (+) Levomethorphan >< Dextromethorphan (-) D(exter) --> l=OPIATE >< d=HALLUCINOGENIC OPIATE └--> Racemic mix of both isomers, embodying their properties.

Morphinan (Racemorphan): l (+) Levorphanol >< Dextrorphan (-) d --> l=OPIATE >< d=HALLUCINOGENIC OPIATE

└--> Racemic mix of both isomers, embodying their properties.

(Race)Allorphan: l (+) Levallorphan >< Dextrallorphan (-) d --> l= ANTI-OPIOID >< d=NMDA ANTAGONISTS └--> Racemic mix of both isomers, embodying their properties.

3-Hydroxymorphinan: l (+) Norlevorphanol >< Nordextrorphan (-) d --> l=OPIATE >< d=NOOTROPIC

└--> Racemic mix of both isomers, embodying their properties.

Oxilorphan: μ antagonist & weak partial κ agonist

Dimemorfan - SIGMAERGIC DRUG

Xorphanol - mixed ant.-ag. produces convulsions at highest dose tested.

Cyprodime - Selective μ opioid antagonist with no affinity for κ or δ receptors

Samidorphan - selective μ antagonist. potential for addiction treatment.

4-Phenylpiperidines

4-Fluoropethidine - In comparison to pethidine, it is 50% less potent as an analgesic but 50% more potent as a DRI. (4-iodo & 3, 4-dichloro only increase these differences)

Anileridine - Another banned pethidine analogue, probably abused. Higher analgesia than Meperidine due to n-aminophenyl group and acts withing 15 mins orally, lasting 2-3 hours.

Benzethidine - 4-phenylpiperidine analogue of pethidine. Probably somewhat more potent and euphoric. Never scripted.

Carperidine - fairly normal opiate but unused in medicine and currently LEGAL (08/06/2013)

Furethidine - 4-Phenylpiperidine analogue of pethidine. Probably a lot more potent and abuse prone. Never prescribed.

Morpheridine - related to meperidine but 4x the potency and does not cause convulsions

Phenoperidine - 20-200x the potency of Pethidine. Less hypnotic and than morphine but more emetic (nausea). This can be cured by Haloperidol.

Piminodine - similar dose to M, used in 60's and 70's but was banned. It was probably abused widely

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