Quick Guide to Common Opiates: Difference between revisions

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* <div>Azidomorphine - 40x potency of M with high affinity to μ</div>
* <div>Myrophine* - Morphine + 3-benzyl & 6-myristyl chain and acts as a prodrug to M. Has a slow onset of effects and longer duration but reduced potency. Does NOT produce addiction or dependance regardless of dose.</div>
* <div>6-MDDM - 80x potency of M, faster onset and less body load</div>
* <div>Dipropanoylmorphine - Ester of M used to treat severe pain. Rarely used but considered to be safer and less adictive than M. As such carries less side effects, such as euphoria. Slower acting, longer lasting and slightly more potent than M.</div>
* <div>Methyldihydromorphine - Related to heterocodeine not dihydrocodeine. Could be 6-9x potency of morphine and a drug of abuse.</div>
* <div>Diacetyldihydromorphine - Occasionally used 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.</div>
* <div>Heterocodeine - Reverse isomer of codeine. 6x potency of M, while Codeine is a prodrug, HC is a direct agonist.</div>
* <div>Methyldesorphin - 15x potency of M. Is found in Krokodil</div>
* <div>14-Cinnamoyloxycodeinone - 100x potency of M, interesting.</div>
* <div>3-Acetyloxymorphone - Acetylated analogue of OM</div>
* <div>Oxymorphazone - half potency as OM but higher doses last up to 48hrs - irreversible full μ agonist</div>
* <div>Chloroxymorphamine - Derivative of OM and irreversible full agonist</div>
* <div>Nicomorphine - 2-3x the potency of M and commonly prescribed in German speaking countries</div>
* <div>Apomorphine -</div>
* <div>Metamizol -</div>
* <div>Metopon - Methylated Hydromorphone, less potent. Interesting though, could have more euphoria</div>
* <div>14-Phenylpropoxymetopon - 2000+x potency of M, when injected into spine up to 1,000,000x. 14-MOP has ceiling effect on respiratory depression (!!) but 14-PPOP untested</div>
* <div>MT-45 - 80% of M. mixed ant.-ag. and mild NMDA antagonist</div>
* <div>Tapentadol - μ & σ agonist & SNRI. Potency in between M & Tram.</div>
* <div>Ciramadol - Opioid related to PCP, Tramadol & Tapentadol. mixed ant.-ag. for μ, low abuse potential and ceiling on respiratory depression.</div>
* <div>7-Spiroindanyloxymorphone - odd OM analogue, selective d agonist</div>
* <div>Oxymorphol - 6-hydrogenated OM, coming soon...</div>
* <div>Pentamorphone - few x stronger than fent. short duration but low respiratory depression.</div>
* <div>Morphinan-6-one (MR-2096) - OM analogue at roughly 5-7mg dosage. RC. FULL NAME: (N-tetrahydrofurfuryl)noroxymorphone</div>
* <div>Hydromorphinol - Derivative of M but more potent, with a steeper dose-response curve and a longer half life. Script in Sweden.</div>
* <div>RAM-378* - N-Phenethyl analogue of Hydromorphinol. It is probably more potent as a result.</div>
* <div>Ro4-1539 (Furethylnorlevorphanol) - 30-60x the potency of M. One of the more potent u agonists from the Morphans.</div>
* <div>Carfentanil - 100x potency of fent., 10000x the potency of M. Used in spetznaz hostage crisis. 10,000x potency of M. Activity in humans starts at 1μg.</div>
* <div>Lofentanil - more potent and with a longer duration than carfentanil.</div>
* <div>Remifentanil - Potent ultra short acting fent. analogue. Potency from between 20 and 100ug. Used in medicine as an anaesthetic under Ultiva.</div>
* <div>3-Methylfentanyl - 400-6000x potency of M depending on isomer (cis-iso more potent)</div>
* <div>Ohmefentanyl - 6300x morphine at it's most active isomer. Analogues of this are even stronger with one possessing 30,000x the potency of M.</div>
* <div>Alfentanil - 1/4 the potency and 1/3 the duration of fent but 4x quicker onset. The businessman's lunch of opiates.</div>
* <div>Betahydroxythiofentanyl - one of the more favoured fent. analogues by addicts, implying euphoria.</div>
* <div>Sufentanil - 5-10x potency of fent.</div>
* <div>R-30490 - analogue of carfentanil. Most selective μ agonist of all fentanyl analogues</div>
* <div>Mirfentanil - fent. analogue with strong selevtivity over μ. Lower doses it antagonises effects caused by lesser opioids but at higher doses is resistant to antagonists, suggesting it has non-opioid mechanisms.</div>
* <div>7-PET - 300x potency of M, 3-OH derivative is 2200x potency of M. Unscheduled.</div>
* <div>Etorphine - 1000-3000x potency of M. μ, κ & δ opioid agonist. weak affinity for ORL1 nociceptin/orphanin FQ receptor.</div>
* <div>Dihydroetorphine -1000-12000x potency of M depending on RoA. Less addictive than other opiates and is used in a similar fashion to Subutex in China.</div>
* <div>Acetorphine - 8700x potency of M</div>
* <div>BU-48 - Etorphine derivative. Selective δ agonist and produces only convulsions with slight antidepression.</div>
* <div>Etonitazene - 1000-1500x potency of M.</div>
* <div>AD-1211 - mixed ant.-ag. similar to Pentazocine. Little development of tolerance or dependance.</div>
* <div>AH-7921 - Selective μ agonist, with 80% potency of M. distributed as an RC, TRs show that it has very little euphoria, indicating euphoria comes from somewhere else. Perhaps sigma? Other opioids are heavily potentiated by it. Perhaps μ agonism is purely analgesic and high comes from a combination of μ & δ with each multiplying the affect of the other. This indicates ultimate opiate high would be moderately selective δ agonist</div>
* <div>Bromadol (BDPC) - 500-10,000x potency of M. Similar to PCP analogues & -HO bonds within them.</div>
* <div>3-HO-TCP - PCP analogue. More glutamergic than the PCP analogue.</div>
* <div>3-HO-BCP - substitutes for both cocaine and morphine at ~5mg (made-up)</div>
* <div>Ketobemidone - μ opioid antagonist & NMDA antagonist. More addictive than M</div>
* <div>Acetoxyketobemidone - Unschedualed analogue of ketobemidone</div>
* <div>Bemidone - Analogue of Pethidine but significantly less potent, however it has NMDA antagonism like KetoB.</div>
* <div>Dipipadone - Lost Ark of the Covenant.</div>
* <div>Phenadoxone - methadone analogue, similar dose to M, lasts 1-4 hours</div>
* <div>Levacetylmethadol - Methadone analogue with u agonism and noncompetitive a3b4 NACh antagonism. Brand name Orlaam, prescribed to those unresponsive to methadone or subutex. Long half life (3 days) and heavier affect.</div>
* <div>Dimenoxadol - Benzillic Acid derivative related to methadone. Banned due to high abuse potential it seems.</div>
* <div>Dimepheptadol - related to methadone, has two isomers which also have two isomers so 6 possible isomers including racemic</div>
* <div>Dioxaphetyl butyrate - Banned opioid similar to methadone. Possibly in use or previously in use as a med under the names Amidalgon & Spasmoxal.</div>
* <div>IC-26 - Methadone analogue with similar potency but Unscheduled.</div>
* <div>Lefetamine - Weak opiate on the same scale as codeine but has DRI properties.</div>
* <div>Norpipanone - Was not under international control until case reports of addiction arose.</div>
* <div>R-4066 - methadone analogue with 212x the potency but a much shorter duration at 3 hours.</div>
* <div>Piminodine - similar dose to M, used in 60's and 70's but was banned. It was probably abused widely.</div>
* <div>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.</div>
* <div>Benzethidine - 4-phenylpiperidine analogue of pethidine. Probably somewhat more potent and euphoric. Never scripted.</div>
* <div>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)</div>
* <div>Furethidine - 4-Phenylpiperidine analogue of pethidine. Probably a lot more potent and abuse prone. Never prescribed.</div>
* <div>Carperidine - fairly normal opiate but unused in medicine and currently LEGAL (08/06/2013)</div>
* <div>Morpheridine - related to meperidine but 4x the potency and does not cause convulsions</div>
* <div>Phenoperidine - 20-200x the potency of Pethidine. Less hypnotic and than morphine but more emetic (nausea). This can be cured by Haloperidol.</div>
* <div>Picenadol - Mixed antagonist-agonist, low affinity. Potential for expansion</div>
* <div>Allylprodine - Prodine analogue 23x potency of M</div>
* <div>Prosidol - Russian Prodine analogue</div>
* <div>Picenadol - R isomer (or Levopicenadol) is pure μ agonist while S is antagonist. Racemic is mixed that casues low abuse potential but has low κ activity</div>
* <div>Palfium (Dextomoramide) - 3x potency of M but shorter acting. High BA & fast acting, oral feels like shooting. Low LD50 & inconsistent potency (one day you may need 5mg, next day 3mg)</div>
* <div>Propiram - Slightly more potent than codeine, 3-6hr duration. mixed μ ant.-ag. favouring agonism. affinity for κ & δ, sigma and nmda. 97% oral BA!</div>
* <div>Diampromide - Banned Analgesic related to Propiram. Similar potency to M.</div>
* <div>BRL-52537 - Highly potent and selective κ agonist. Neuroprotective.</div>
* <div>C-8813 (Thiobromadol) - 591x potency of M. μ agonist & δ antagonist to reduce repiratory depression. Making the drug safer.</div>
* <div>Herkinorin - Analogue of Salvinorin A but the complete opposite. 100x higher μ affinity and 50x lower κ affinity. Also; "does not promote the recruitment of β-arrestin-2 to the intracellular domain of the μ-opioid receptor, or induce receptor internalization". This means Herkinorin may not produce tolerance or dependance.</div>
* <div>Methopholine - Isoquinilone derivative with same efficacy as codeine. Could produces corneal opacity. Analogues are more potent with 4'-nitromethopholine at 20x codeine.</div>
* <div>Nortilidine - Equipotency of M. Opioid activity is in (1S,2R) iso, NMDA antagonism is in (1R,2S) iso. Also acts as a DRI.</div>
* <div>O-Desmethyltramadol - metabolite of Tramadol. Considerably more potent than Tramadol. Both (+) & (-) isomers lose SRI function but (-) retains NRI functionality. RC.</div>
* <div>SC-17599 - selective μ agonist with little or no affinity for δ & κ. Potency in between pethidine & morphine.</div>
* <div>RWJ-394674 - potent and selective δ agonist, however once inside body it is dealkylated to its monodesethyl metabolite RWJ-413216 which is a potent μ agonist with less affinity for δ. δ activity counteracts the respiratory depression the μ causes. Only prominent side effect is sedation (and euphoria!)</div>
* <div>TAN-67 - potent and selective δ1 agonist. Has analgesic properties & releases dopamine in the brain. Neuro & cardiac protective properties.</div>
* <div>W-15 - 5.4x Morphine. RC.</div>
* <div>W-18 - 10,000x potency of M, structure abstract from any other drug. These super potent opioids are used in vetenarian practice for tranquilising elephants.</div>
* <div>SoRI-9409 - mixed μ agonist & δ antagonist. moderate analgesia without development of tolerance. Anti-addictive effects for all dopaminergic drugs.</div>
* <div>'Synthetic Conotoxin' - Snail toxin derived painkiller 1000x potency of morphine. Non-addictive</div>
* <div>Loperamide - Peripheral opioid so it cannot cross BBB. useful anti-Diarrhoea med. When used in conjuction with Quinine or Omerprazole can cross BBB and opioid effects are seen.</div>
* <div>BW373U86 - Selective δ agonist at 15x stronger affinity. Analgesic and anti-depressant properties along with BDNF release. Produces convulsions at high doses and reverses respiratory depression produced by μ agonism. Also protects heart muscle cells from death during oxygen deprivation, a result of heart attacks.</div>
* <div>DPI-227 - highly selective δ agonist with antidepressant effects but produces fewer convulsions than most other dugs in it's family.</div>
* <div>DPI-3290 - Potent δ & μ agonist but produces little respiratory depression.</div>
* <div>Bezitramide - (Burgodin?)</div>
* <div>Piritramide - 0.65-0.75x M but still effect is strong and long lasting. Has a small but dedicated fanclub on the 'street'</div>
* <div>IBNtxA -</div>
* <div>Matrine -</div>
* <div>Thiambutenes - Dimethyl-TAB, Diethyl-TAB, Ethylmethyl-TAB. Used in vetinary medicine in Japan. Banned in virtually all countried due to high abuse potential. Anticholinergic and antihistamine properties!</div>
* <div>Dextropropoxyphene - Low potency opiate not absorbed by CYP2D6. Also is a potent, noncompetitive α3β4 NACh antagonist and a weak SRI.</div>
* <div>Deltorphin - High affinity and selectivity, naturally occuring δ opioid agonist.</div>
* <div>HZ-2 - κ-opioid agonist, same potency as morphine, long duration, high oral BA</div>
* <div>Dermorphin - South American Tree frog skin. Natural opioid peptide. High potency (30-40x M) and selectivity to μ but may be less likely to cause tolerance and addiction.</div>
* <div>Thebaine - 6, 14 dimethoxy version of OM. Stimulant rather than analgesic, high dose causes OD</div>
* <div>Thebacon - Thebaine analogue and fairly uninteresting</div>
* <div>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.</div>
* <div>Biphalin - endogenous eptide with high affinity for δ & μ receptors. Potency almost 7x greater than Etorphine and 7000x M. Low side effects; no dependancy caused.</div>
* <div>Opiorphin - Endogenous opioid isolated from human saliva.</div>
* <div>Met-enkephalin - Opioid Growth Factor (OGF), Endogenous opioid peptide. Primary ligand of the δ receptor along with Leu-enkephalin (high potency and selectivity at δ). Low BA & is metabolised rapidly.</div>
* <div>Leu-enkephalin - Endogeneous opioid petide that acts as a δ & μ agonist with strong selectivity for δ.</div>
* <div>Casomorphins - opiates found in Cow's milk.</div>
* <div>DAMGO - synthetic opiate peptide with high μ selectivity. When administered alongside M for 7 days, M had the same effect at the same dose as the first day. I.e. removes tolerance.</div>
* <div>Eseroline - Metabolite of the ACh inhibitor physostigmine but potent μ agonist</div>
* <div>Hodgkinsine - alkaloid found in Psychotria colorata plants. Has antiviral, antibacterial and antifungal properties. Also μ opioid agonist & NMDA antagonist.</div>
* <div>Mitragynine - Alkaloid in Kratom. Fairly selective μ agonist but little affinity for δ & κ.</div>
* <div>7-Hydroxymitragynine - Alkaloid in Kratom. Some 17x potency of M. 30x potency of Mitragynine.</div>

Latest revision as of 05:27, 5 December 2015