- Joined
- Feb 2, 2024
- Messages
- 83
- Reaction score
- 69
- Points
- 18
This table is from wiki Equianalgesic page. It is a bit inaccurate and far from being complete list, but I'll later add more interesting compounds.
You should note that this is combined data from different methods of measuring potency on different animals, especially for the most potent ones. So carefully translate this data for the human potency.
For example, Ohmefentanyl potency here is listed as 6300, but it has 8 isomers, one of it - (3R,4S,βS) is considerably stronger than others, or around 6300 stronger than morphine for mouses, BUT for monkeys it is EXTREMELY potent, up to 50.000 times or even more compared to morphine (it was very hard to measure precisely), so more likely it will be similar case for humans. This makes it one of the most potent compounds EVER, not only as pain killers, but also as plain killers, pushing such classical warfare nerve agents as VX out of the game.
Another case is comparison of carfentanil and lofentanil (carfentanil with 3-Methyl group on piperidine ring), later is listed here as 10k-100k potency, but in animal studies is about twice less potent than carfentanil, the opposite case is for humans - it is more potent, and many times more toxic, because it lasts up to 3 days.
There are already compounds with potency rate up to million times compared to morphine (not only by instraspinally route) and likely later appear even more ones, as a result of success in AI prediction of protein folding and binding, but I don't want to list it here, as working with such materials is disaster.
Those who continue the war with amateur and clandestine chemistry should clearly understand that with their actions they only push people to work with more and more potent substances, because year by year it become harder and harder to order chemicals in necessary quantities.
Nonlinearities
This chart measures pain relief versus mass of medication. Not all medications have a fixed relationship on this scale. Methadone is different from most opioids because its potency can vary depending on how long it is taken. Acute use (1–3 days) yields a potency about 1.5× stronger than that of morphine and chronic use (7 days+) yields a potency about 2.5 to 5× that of morphine. Similarly, the effect of tramadol increases after consecutive dosing due to the accumulation of its active metabolite and an increase of the oral bioavailability in chronic use.Comparison to oral morphine
Analgesic | Strength (relative) | Equivalent dose (10 mg oral morphine) | |||||
---|---|---|---|---|---|---|---|
Paracetamol (non-opioid) | 1⁄360 | 3600 mg | 63–89% | 1–4 | 37 min(PO); 8 min(IV) | 5–6 hours | |
Aspirin(NSAID, non-opioid) | 1⁄360 | 3600 mg | 80–100% | 3.1–9 | |||
Ibuprofen[10](NSAID, non-opioid) | 1⁄222 | 2220 mg | 87–100% | 1.3–3 | |||
Diflunisal(NSAID, non-opioid) | 1⁄160 | 1600 mg | 80–90% | 8–12 | |||
Naproxen[10](NSAID, non-opioid) | 1⁄138 | 1380 mg | 95% | 12–24 | |||
Piroxicam (NSAID non-opioid) | 1⁄120 (est.) | ||||||
Indomethacin (NSAID non-opioid) | 1⁄64 (est.) | ||||||
Diclofenac[10][11](NSAID, non-opioid) | 1⁄10 (est.) (same as Codeine) | 100 mg (est.) | 50–60% | 1–4 | |||
Ketorolac[12](NSAID, non-opioid) | 1⁄3 (est.) | 30 mg IV (est.) | 80–100% | 5–7 | |||
Nefopam (Centrally-acting non-opioid) | 5⁄8 (est.) | 16 mg IM (est.) | Nefopam: 3–8, Desmethylnefopam 10–15 | ||||
Dextropropoxyphene[13] | 1⁄13–1⁄20 | 130–200 mg | |||||
Codeine | 1⁄10–3⁄20 | 100–120 mg(PO) | ~90% | 2.5–3(C6G 1.94;[14] morphine 2–3) | 15–30 min(PO) | 4–6 hours | |
Tramadol | 1⁄10 | ~100 mg | 75% (IR), 85–90% (ER) | 6.0–8.8[15] (M1) | |||
Opium(oral) | 1⁄10 | ~100 mg | ~25%(morphine) | 2.5–3.0(morphine, codeine) | |||
Tilidine | 1⁄10 | 100 mg | |||||
Dihydrocodeine | 1⁄5 | 50 mg | 20% | 4 | |||
Anileridine[16] | 1⁄4 | 40 mg | |||||
Alphaprodine | 1⁄4–1⁄6 | 40–60 mg | |||||
Tapentadol[17] | 3⁄10 | 32 mg | 32% (fasting) | ||||
Pethidine (meperidine) | 1⁄3 | 30 mg SC/IM/IV, 300 mg(PO) | 50–60% | 3–5 | |||
Benzylfentanyl | 1⁄2 | ||||||
AH-7921 | 4⁄5 | ||||||
Hydrocodone | 1 | 10 mg | 70%[18] | 3.8–6(Instant Release; PO) | 10–30 min(Instant Release; PO) | 4–6 | |
Metopon | 1 | 10 mg | |||||
Pentazocine lactate (IV)[19] | 1 | 10 mg SC/IV/IM, 150 mg(PO) | |||||
Morphine (oral) | 1 | 10 mg | ~25% | 2–4 | 3:1 | 30 min(PO) | 3–6 hours |
Oxycodone(oral)[20] | 1.5 | 6.67 mg | 60-87% | 2–3 hours(Instant Release)(PO); 4.5 hours(Controlled Release)(PO) | 10–30 min(Instant Release)(PO); 1 hour(Controlled Release)(PO) | 3–6 hours(Instant Release)(PO); 10–12 hours(Controlled Release)(PO)[21] | |
Spiradoline | 1.5 | ||||||
Nicomorphine | 2–3 | 3.33–5 mg | 20% | 4 | |||
Oxycodone(IV)[22] | 3 | 3.33 mg | 96% | 1.5–3 (IV) | 5 min(IV)[22] | 2-4 hours | |
Morphine(IV/IM) | 3 | 3.33 mg | 100% | 2–3 | 3:1 | Instantaneously (from 5 to 15 sec; IV); 5–15 min(IM) | 3–7 hours |
Clonitazene | 3 | 3.33 mg | |||||
Methadone (acute)[23][24] | 3–4 | 2.5–3.33 mg | 40–90% | 15–60 | 2:1 | ||
Methadone (chronic)[24] | 2.5–5 | 2–4 mg | 40–90% | 15–60 | 2:1 | ||
Phenazocine | 4 | ~2.5 mg | |||||
Diamorphine (Heroin; IV/IM)[25] | 4–5 (iv, im) 2–2.5 (insufflated)[26] | 2–2.5 mg | 100% | <0.6 (morphine prodrug)[27] | Instantaneously (from 5 to 15 sec; IV); 2 to 5 min(IM) | 3 to 7 hours | |
Dezocine | 4–6 | 1.6–2.5 mg | 97% (IM) | 2.2 | |||
Hydromorphone[28][29][17] | 10(SC, IV, IM) 3–3.75(PO) | 0.5-0.75 mg (SC, IV, IM) 2.5 mg (PO) | Orally: 30–35%, Intranasal: 52- 58% IV/IM: 100% 62% | 2–3 | 5:1 | ||
Oxymorphone[20] | 10(SC, IV, IM) 3–4(PO) | 3.33 mg(PO), 0.333 mg(IV,IM & Interlaminar) | PO: 10% Buccal: 28% Sublingual:37.5% Intranasal: 43% IV, IM & IT: 100% | 7.25–9.43 | 35 min(PO), Instantaneously (from 5 to 15 sec)(IV) | 6–8 hours orally 2-6 hours parenteral | |
U-47700 | 7.5 | 1.5 mg | 1.5–3 | ||||
Levorphanol[30] | 8 | 1.25 mg | 70% | 11–16 | 1:1 | ||
Desomorphine (Krokodil) | 8–10 | 1–1.25 mg | ~100%(IV) | 2–3 | Instantaneously (from 5 to 15 sec)(IV); 2–5 min(IM) | 3–4 hours | |
N-Phenethylnormorphine | 8–14 | ||||||
Alfentanyl | 10–25 | 1.5 (90–111 minutes) | Instantaneously (from 5 to 15 sec); 4× more rapid than fentanyl | 0.25 hr (15 min); up to 54 minutes until offset of effects | |||
Trefentanil | (10–25)+ | ||||||
Brifentanil | (10–25)+ | ||||||
Acetylfentanyl | 15 | ||||||
7-Hydroxymitragynine | 17 | ~0.6 mg | |||||
Furanylfentanyl | 20 | ||||||
Butyrfentanyl | 25 | ||||||
Enadoline | 25 | 15 μg (threshold) and 0.160 mg/kg (dissociative effects) | |||||
Buprenorphine(SL)[13] | 40 | 0.25 mg | 30%(SL);[31] ~100%(TD); 65% (buccal);[32][33] 48%(INS)[34] | 20–70, mean 37 | 3:1 | 45 min | 12–24 hours |
N-Phenethyl-14-ethoxymetopon | 60 | 160 μg | |||||
Phenomorphan | 60–80 | 0.13–0.16 mg | |||||
N-Phenethylnordesomorphine | 85 | ||||||
Phenaridine | (50–100)− | ||||||
Fentanyl | 50–100 | 0.1 mg (100 μg) IM/IV | 33%(SL); 92%(TD); 89%(INS); 50%(buc) | 0.04 (IV); 7(TD) | 5 min(TD/IV) | 30–60 minutes(IV) | |
Metonitazene | 100 | 0.1 mg/100 μg | |||||
Acrylfentanyl | (50–100+) | ||||||
Buprenorphine(Transdermal)[35][36] | 100–115 | 0.1 mg (100 μg) | 30%(SL);[31] ~100%(TD); 65% (buccal);[32][33] 48%(INS)[34] | 3:1 | 45–60 minutes | 12–24 hours | |
14-Cinnamoyloxycodeinone | 177 | 77 μg | |||||
Etonitazepyne | 180-190 | 55-60 μg | |||||
Protonitazepyne | 180-190 | 55-60 μg | |||||
Remifentanil | 100–200 | 50–100 μg | 0.05 (3–6 min context-sensitive half-life; 7–18min elimination half-life) | Instantaneously (from 5 to 15 sec) | 15 minutes; rapid offset of effects necessitates continuous infusion for maintenance of anesthesia | ||
Protonitazene | 200 | 50 μg | |||||
Ocfentanil | 125–250 | 40–80 μg | |||||
Ro4-1539 | 240–480 | 20-40 μg | |||||
Isotonitazene | 500 | 20 μg | |||||
Sufentanil | 500–1,000 | 10–20 μg | 4.4 | ||||
BDPC | 504 | ~20 μg | |||||
C-8813 | 591 | ||||||
4-Phenylfentanyl | 800 | ||||||
Etonitazene | 1000-1500 | 6,6-10 μg | |||||
3-Methylfentanyl | 1000-1500 | ||||||
N-Desetylisotonitazene | 1000-2000 | 5-10 μg | |||||
Etorphine | 1,000-3,000 | 3.3–10 μg | |||||
Ohmefentanyl | 6300 | ||||||
Acetorphine | 8700 | 1.33 μg | |||||
Dihydroetorphine[37] | 1,000–12,000 | 0.83–10 μg (20–40 μg SL) | |||||
Carfentanil[38] | 10,000 | 1.0 μg | 7.7 | ||||
2-Fluorohmefentanil | 18,000 | ||||||
4-Carboethoxyohmefentanil | 30,000 | ||||||
Ohmecarfentanil | (30,000) | ||||||
R-30490 | (10,000–100,000)− | ||||||
Lofentanil | (10,000–100,000)+ | ||||||
14-Methoxymetopon (intraspinally)[39] | (1,000,000) |
PO: oral • IV: intravenous injection • IM: intramuscular injection • SC: subcutaneous injection • SL: sublingual • TD: transdermal
"Strength" is defined as analgesic potency relative to oral morphine.
Tolerance, sensitization, cross-tolerance, metabolism, and hyperalgesia may be complex factors in some individuals.
Interactions with other drugs, food and drink, and other factors may increase or decrease the effect of certain analgesics and alter their half-life.
Because some listed analgesics are prodrugs or have active metabolites, individual variation in liver enzymes (e.g., CYP2D6 enzyme) may result in significantly altered effects.
"Strength" is defined as analgesic potency relative to oral morphine.
Tolerance, sensitization, cross-tolerance, metabolism, and hyperalgesia may be complex factors in some individuals.
Interactions with other drugs, food and drink, and other factors may increase or decrease the effect of certain analgesics and alter their half-life.
Because some listed analgesics are prodrugs or have active metabolites, individual variation in liver enzymes (e.g., CYP2D6 enzyme) may result in significantly altered effects.
You should note that this is combined data from different methods of measuring potency on different animals, especially for the most potent ones. So carefully translate this data for the human potency.
For example, Ohmefentanyl potency here is listed as 6300, but it has 8 isomers, one of it - (3R,4S,βS) is considerably stronger than others, or around 6300 stronger than morphine for mouses, BUT for monkeys it is EXTREMELY potent, up to 50.000 times or even more compared to morphine (it was very hard to measure precisely), so more likely it will be similar case for humans. This makes it one of the most potent compounds EVER, not only as pain killers, but also as plain killers, pushing such classical warfare nerve agents as VX out of the game.
Another case is comparison of carfentanil and lofentanil (carfentanil with 3-Methyl group on piperidine ring), later is listed here as 10k-100k potency, but in animal studies is about twice less potent than carfentanil, the opposite case is for humans - it is more potent, and many times more toxic, because it lasts up to 3 days.
There are already compounds with potency rate up to million times compared to morphine (not only by instraspinally route) and likely later appear even more ones, as a result of success in AI prediction of protein folding and binding, but I don't want to list it here, as working with such materials is disaster.
Those who continue the war with amateur and clandestine chemistry should clearly understand that with their actions they only push people to work with more and more potent substances, because year by year it become harder and harder to order chemicals in necessary quantities.