Английская Википедия:Equianalgesic

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Шаблон:Short descriptionШаблон:Cs1 configAn equianalgesic chart is a conversion chart that lists equivalent doses of analgesics (drugs used to relieve pain). Equianalgesic charts are used for calculation of an equivalent dose (a dose which would offer an equal amount of analgesia) between different analgesics.Шаблон:Sfn Tables of this general type are also available for NSAIDs, benzodiazepines, depressants, stimulants, anticholinergics and others.

Format

Equianalgesic tables are available in different formats, such as pocket-sized cards for ease of reference.Шаблон:Sfn A frequently-seen format has the drug names in the left column, the route of administration in the center columns and any notes in the right column.Шаблон:SfnШаблон:Sfn

Purpose

There are several reasons for switching a patient to a different pain medication. These include practical considerations such as lower cost or unavailability of a drug at the patient's preferred pharmacy, or medical reasons such as lack of effectiveness of the current drug or to minimize adverse effects. Some patients request to be switched to a different narcotic due to stigma associated with a particular drug (e.g. a patient refusing methadone due to its association with opioid addiction treatment).Шаблон:Sfn Equianalgesic charts are also used when calculating an equivalent dosage of the same drug, but with a different route of administration.Шаблон:Citation needed

Precautions

An equianalgesic chart can be a useful tool, but the user must take care to correct for all relevant variables such as route of administration, cross tolerance, half-life and the bioavailability of a drug.Шаблон:Sfn For example, the narcotic levorphanol is 4–8 times stronger than morphine, but also has a much longer half-life. Simply switching the patient from 40 mg of morphine to 10 mg of levorphanol would be dangerous due to dose accumulation, and hence frequency of administration should also be taken into account.

There are other concerns about equianalgesic charts. Many charts derive their data from studies conducted on opioid-naive patients. Patients with chronic (rather than acute) pain may respond to analgesia differently. Repeated administration of a medication is also different from single dosing, as many drugs have active metabolites that can build up in the body.Шаблон:Sfn Patient variables such as sex, age, and organ function may also influence the effect of the drug on the system. These variables are rarely included in equianalgesic charts.Шаблон:SfnШаблон:SfnШаблон:Sfn

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Opioid equivalency table

Шаблон:Contradicts other Opioids are a class of compounds that elicit analgesic (pain killing) effects in humans and animals by binding to the µ-opioid receptor within the central nervous system. The following table lists opioid and non-opioid analgesic drugs and their relative potencies. Values for the potencies represent opioids taken orally unless another route of administration is provided. As such, their bioavailabilities differ, and they may be more potent when taken intravenously.Шаблон:Citation needed

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.Шаблон:Citation needed

Comparison to oral morphineШаблон:Efn
Analgesic Strength
(relative)
Equivalent dose
(10 mg oral morphine)Шаблон:Efn
Bioavailability Half-life of active metabolites
(hours)
Oral-to-parenteral ratio Speed of onset Duration
Paracetamol (non-opioid) Шаблон:Frac 3600 mg 63–89% 1–4 37 min (PO); 8 min (IV) 5–6 hours
Aspirin (NSAID, non-opioid) Шаблон:Frac 3600 mg 80–100% 3.1–9
Ibuprofen[1] (NSAID, non-opioid) Шаблон:Frac 2220 mg 87–100% 1.3–3
Diflunisal (NSAID, non-opioid) Шаблон:Frac 1600 mg 80–90% 8–12
Naproxen[1] (NSAID, non-opioid) Шаблон:Frac 1380 mg 95% 12–24
Piroxicam (NSAID non-opioid) Шаблон:Frac (est.)
Indomethacin (NSAID non-opioid) Шаблон:Frac (est.)
Diclofenac[1][2] (NSAID, non-opioid) Шаблон:Frac (est.) (same as Codeine) 100 mg (est.) 50–60% 1–4
Ketorolac[3] (NSAID, non-opioid) Шаблон:Frac (est.) 30 mg IV (est.) 80–100% 5–7
Nefopam (Centrally-acting non-opioid) Шаблон:Frac (est.) 16 mg IM (est.) Nefopam: 3–8, Desmethylnefopam 10–15
Dextropropoxyphene[4] Шаблон:FracШаблон:Frac 130–200 mg
Codeine Шаблон:FracШаблон:Frac 100–120 mg (PO) ~90% 2.5–3 (C6G 1.94;[5] morphine 2–3) 15–30 min (PO) 4–6 hours
Tramadol Шаблон:Frac ~100 mg 75% (IR), 85–90% (ER) 6.0–8.8[6] (M1)
Opium (oral) Шаблон:Frac ~100 mg ~25% (morphine) 2.5–3.0 (morphine, codeine)
Tilidine Шаблон:Frac 100 mg
Dihydrocodeine Шаблон:Frac 50 mg 20% 4
Anileridine[7] Шаблон:Frac 40 mg
Alphaprodine Шаблон:FracШаблон:Frac 40–60 mg
TapentadolШаблон:Sfn Шаблон:Frac 32 mg 32% (fasting)
Pethidine (meperidine) Шаблон:Frac 30 mg SC/IM/IV, 300 mg (PO) 50–60% 3–5
Benzylfentanyl Шаблон:Frac
AH-7921 Шаблон:Frac
Hydrocodone 1 10 mg 70%[8] 3.8–6 (Instant Release; PO) 10–30 min (Instant Release; PO) 4–6
Metopon 1 10 mg
Pentazocine lactate (IV)[9] 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)[10] 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)[11]
Spiradoline 1.5
Nicomorphine 2–3 3.33–5 mg 20% 4
Oxycodone (IV)[12] 3 3.33 mg 96% 1.5–3 (IV) 5 min (IV)[12] 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)[13][14] 3–4 2.5–3.33 mg 40–90% 15–60 2:1
Methadone (chronic)[14] 2.5–5 2–4 mg 40–90% 15–60 2:1
Phenazocine 4 ~2.5 mg
Diamorphine (Heroin; IV/IM)[15] 4–5 (iv, im) 2–2.5 (insufflated)[16] 2–2.5 mg 100% <0.6 (morphine prodrug)[17] 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
HydromorphoneШаблон:SfnШаблон:SfnШаблон:Sfn 10–15 (SC, IV, IM)
3.75–5 (PO)
0.75 mg (SC, IV, IM)
2 mg (PO)
62% 2–3 5:1
Oxymorphone[10] 8 3.33 mg (PO), 1 mg (IV,IM & Interlaminar) 10%–PO, ≈ 25% Sublabial, ≈ 28% Buccal, (35–40%) Sublingual & Intranasal 43% BA. 7.25–9.43 35 min (PO), Instantaneously (from 5 to 15 sec)(IV) 6–8 hours
U-47700 7.5 1.5 mg 1.5–3
Levorphanol[18] 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)[4] 40 0.25 mg 30% (SL);[19] ~100% (TD); 65% (buccal);[20][21] 48% (INS)[22] 20–70, mean 37 3:1 45 min 12–24 hours
N-Phenethyl-14-ethoxymetopon 60 160 µg
Etonitazene 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)
Acrylfentanyl (50–100+)
Buprenorphine (Transdermal)[23][24] 100–115 0.1 mg (100 µg) 30% (SL);[19] ~100% (TD); 65% (buccal);[20][21] 48% (INS)[22] 3:1 45–60 minutes 12–24 hours
14-Cinnamoyloxycodeinone 177 77 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
Ocfentanil 125–250 40–80 µg
Ro4-1539 240–480 20-40 µg
Sufentanil 500–1,000 10–20 µg 4.4
BDPC 504 ~20 µg
C-8813 591
4-Phenylfentanyl 800
3-Methylfentanyl 1000–1500
Etorphine 1,000–3,000 3.3–10 µg
Ohmefentanyl 6300
Acetorphine 8700 1.33 µg
Dihydroetorphine[25] 1,000–12,000 0.83–10 µg (20–40 µg SL)
Carfentanil[26] 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)[27] (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.

See also

  • Oripavine – for more on the comparative strength of oripavine derivatives

Explanatory notes

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Citations

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General and cited references

Books

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Articles

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Websites

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Шаблон:Analgesics Шаблон:Opioid receptor modulators

  1. 1,0 1,1 1,2 Шаблон:Cite web
  2. Шаблон:Cite web
  3. Pharma Guide Pre-Work 3rd Edition
  4. 4,0 4,1 Шаблон:Cite book
  5. Шаблон:Cite journal
  6. Шаблон:Cite web
  7. Шаблон:Cite web
  8. Шаблон:Cite journal
  9. Шаблон:Cite web
  10. 10,0 10,1 Шаблон:Cite web
  11. Шаблон:Cite journal
  12. 12,0 12,1 Шаблон:Cite journal
  13. Tabla de equivalencia opiáceos
  14. 14,0 14,1 Шаблон:Cite journal Table 2: Conversion Ratio of Oral Morphine to Methadone.
  15. Шаблон:Cite journal
  16. Шаблон:Cite journal
  17. Шаблон:Cite journal
  18. Шаблон:Cite web
  19. 19,0 19,1 Mendelson J, Upton RA, Everhart ET, Jacob P 3rd, Jones RT (1997). "Bioavailability of sublingual buprenorphine". Journal of Clinical Pharmacology. 37 (1): 31–7. doi:10.1177/009127009703700106. PMID 9048270
  20. 20,0 20,1 Шаблон:Cite web
  21. 21,0 21,1 BUNAVAIL (buprenorphine and naloxone) buccal film, CIII [prescribing information online]. BioDelivery BioDelivery Sciences International, Inc. (BDSI), Raleigh, NC. Jun 2014.
  22. 22,0 22,1 Eriksen J, Jensen NH, Kamp-Jensen M, Bjarnø H, Friis P, Brewster D (1989). "The systemic availability of buprenorphine administered by nasal spray". J. Pharm. Pharmacol. 41 (11): 803–5. doi:10.1111/j.2042-7158.1989.tb06374.x
  23. Khanna, IK; Pillarisetti, S (2015). "Buprenorphine - an attractive opioid with underutilized potential in treatment of chronic pain". Journal of pain research. 8: 859–70. doi:10.2147/JPR.S85951. PMID 26672499
  24. Cote, J; Montgomery, L (July 2014). "Sublingual buprenorphine as an analgesic in chronic pain: a systematic review". Pain medicine (Malden, Mass.). 15 (7): 1171–8. doi:10.1111/pme.12386. PMID 24995716
  25. Шаблон:Cite journal
  26. Шаблон:Cite web
  27. Шаблон:Cite journal