Analgesic potency

The analgesic potency (or analgesic equivalence ) is a measure of the dose-dependence of the analgesic effect of a substance, usually a drug , primarily opioids . Morphine , which is given the reference value “1”, serves as the basis . Medicines that produce pain inhibition in lower doses than morphine have an analgesic potency> 1. Active ingredients that require a higher dosage receive a value below 1. The analgesic potency is not to be equated with the potency. Active ingredients can have a lower maximum effect than morphine, although their analgesic potency is greater than 1.

To clarify, an example with Tramadol: The analgesic potency is 0.1. This means that 10 times the amount of the active ingredient is required to achieve the same analgesic effect as morphine. With the same amount of active ingredient, the analgesic effect is less than that of morphine.

Overview

Many active ingredients with high analgesic potency are subject to narcotics regulations. In Germany, marketable narcotics and prescription drugs may only be dispensed in accordance with the Narcotics Prescription Ordinance (BtMVV). Trading and dispensing of non-marketable narcotics is prohibited.

For comparison, some substances are listed here that are not or hardly usable in medicine and have only proven their analgesic potency in laboratory tests.

Surname	analgesic potency	BtM according to BtMG (D)	comment
Dihydroetorphine	11,000	Yes (Appendix 1 - not marketable and prescribable)	Used in China as sublingual tablets and in plasters.
Ohmefentanyl	6300	n / a	no medical use; Modifications of this substance achieve analgesic potencies of 18,000 (insertion of fluorine at position 4 in the phenethyl ring) to 30,000 (ethoxy group at position 4 of the piperidine ring).
Carfentanyl	5000-7500	Yes (Appendix 1 - not marketable and prescribable)	Big game stunning
3-methylfentanyl (mefentanyl)	3000	Yes (Appendix 1 - not marketable and prescribable)
Etorphine	1000-3000	Yes (Appendix 3 - marketable and prescribable)	Big game stunning.
Sufentanil	about 1000	Yes (Appendix 3 - marketable and prescribable)	Most powerful human analgesic.
Ziconotide	about 1000	n / a	Polypeptide , derived from the venom of the cone snail Conus magus , is very rarely used because it has to be applied intrathecally .
Epibatidine	approx. 200	n / a	Alkaloid from the skin secretion of a frog. Does not create habit or addiction, but is too toxic for medical use. Acts on the nicotinic acetylcholine receptor .
Remifentanil	100-200	Yes (Appendix 3 - marketable and prescribable)
Fentanyl	120	Yes (Appendix 3 - marketable and prescribable)	To Neuroleptanalgesia suitable.
Alfentanil	30-40	Yes (Appendix 3 - marketable and prescribable)
Buprenorphine	30-70	Yes (Appendix 3 - marketable and prescribable)	Partial agonist at the μ-opioid receptor. Is used, among other things, to replace heroin addicts.
β- endorphin	18.5		31 amino acid polypeptide, naturally found in the hypothalamus and pituitary gland .
Oxymorphone	10	Yes (Appendix 2 - marketable, but not prescribable)
Hydromorphone	7.5	Yes (Appendix 3 - marketable and prescribable)	Opioid analgesic.
Butorphanol	5	n / a
Opiorphin	3-6	n / a	Polypeptide, also found in saliva .
Levomethadone	4th	Yes (Appendix 3 - marketable and prescribable)	Cumulation and strong increase in half-life with daily administration. Is used, among other things, for the substitution of heroin addicts.
Diacetylmorphine	2.5	Yes (Appendix 3 - can only be marketed or prescribed with exceptions )	Only in preparations that are approved for substitution.
rac - methadone	2	Yes (Appendix 3 - marketable and prescribable)	Cumulation and strong increase in half-life with daily administration. Is used, among other things, for the substitution of heroin addicts.
Oxycodone	2	Yes (Appendix 3 - marketable and prescribable)	Opioid analgesic.
Morphine	1	Yes (Appendix 3 - marketable and prescribable)	Reference substance for opioids.
Piritramide	0.7	Yes (Appendix 3 - marketable and prescribable)	is often used for PCA (patient-controlled analgesia).
Nalbuphine	0.5-0.7	No.
Tapentadol	0.3-0.6	Yes (Appendix 3 - marketable and prescribable)	Opioid analgesic.
Pentazocine	0.3	Yes (Appendix 3 - marketable and prescribable)
Flupirt	0.2-1	No.	has analgesic and muscle relaxing properties, but is not a “classic analgesic”.
Hydrocodone	0.15 and 0.59, respectively	Yes (Appendix 3 - marketable and prescribable)	The analgesic effect is possibly not only caused by hydrocodone itself, but also by its metabolite hydromorphone, which is formed by O-demethylation.
Dihydrocodeine	0.2	Yes (Appendix 3 - marketable and prescribable, with exceptions)	Weak opioid analgesic. Exceptions: Preparations which, without another substance from Annexes I to III, contain up to 2.5 percent or, per divided form, up to 100 mg of dihydrocodeine, calculated as base. For preparations that are prescribed for people dependent on narcotics or alcohol, however, the regulations on prescribing and dispensing narcotics apply.
Pethidine	0.1-0.2	Yes (Appendix 3 - marketable and prescribable)
Tilidine	0.1-0.2	Yes (Appendix 3 - marketable and prescribable, with exceptions)	Weak opioid analgesic. Exceptions: solid preparations with delayed release of active ingredients which, without another substance from Annexes I to III, contain up to 300 mg of tilidine per divided form, calculated as the base, and, based on this amount, at least 7.5% naloxone hydrochloride.
Codeine	0.1	Yes (Appendix 3 - marketable and prescribable, with exceptions)	Contained in many cough preparations. Weak opioid analgesic. Exceptions: Preparations which, without another substance from Annexes I to III, contain up to 2.5 per cent or, depending on the divided form, up to 100 mg codeine, calculated as a base. For preparations that are prescribed for people dependent on narcotics or alcohol, however, the regulations on prescribing and dispensing narcotics apply.
Meptazinol	0.1	No.
Tramadol	0.1	No.	Weak opioid analgesic.
Metamizole	0.1	No.	Non-opioid analgesic, also antipyretic effect.
Dextropropoxyphene	0.06	Yes (Appendix 2 - marketable, but not prescribable)	Opioid analgesic.
Diflunisal	0.007		Non-opioid analgesic, also antipyretic effect.
Acetylsalicylic acid	0.003	No.	Non-opioid analgesic, also antipyretic, anti-inflammatory, and anticoagulant effects.
Naloxone	against 0		Opioid receptor antagonist, use in emergency medicine (opiate overdose) and diagnosis of opiate addictions.
Naltrexone	against 0		Orally active opioid receptor antagonist.
Loperamide	against 0		Anti-diarrhea agent, only works on opioid receptors outside the central nervous system.
Apomorphine	against 0		Agonist at dopamine receptors, treatment for Parkinson's disease .

See also

• analgesia
• Opiate
• Opioid

Individual evidence

1. ↑ Eckhard Beubler: Compendium of drug pain therapy. Effects, side effects and possible complications. 6th edition. Springer, Berlin / Heidelberg 2016, ISBN 978-3-662-48826-3 , p. 62.
2. ^ V. De Vos: Immobilization of free-ranging wild animals using a new drug . In: Vet Rec. , 1978 July 22, 103 (4), pp. 64-68
3. ↑ Eberhard Klaschik : Pain therapy and symptom control in palliative medicine. In: Stein Husebø , Eberhard Klaschik (ed.): Palliative medicine. 5th edition, Springer, Heidelberg 2009, ISBN 3-642-01548-4 , pp. 207-313, here: p. 233.
4. ↑ CE Inturrisi, JG Umans, D. Wolff, AS Stern, RV Lewis, S. Stein, S. Udenfriend: Analgesic activity of the naturally Occurring heptapeptide [Met] enkephalin-Arg6-Phe 7. In: Proceedings of the National Academy of Sciences . Volume 77, Number 9, September 1980, pp. 5512-5514, Table 1, PMID 6933569 , PMC 350091 (free full text).
5. ↑ JournalMed.de (registration required)
6. ^ Forth, Henschler, Rummel, Förstermann, Starke: General and special pharmacology and toxicology . 8th edition. Urban & Fischer, Munich 2001, ISBN 3-437-42520-X , page 252.
7. ↑ ^{a b} Technical information Hydrocodone Streuli 5 mg / 10 mg , as of September 2012.
8. ↑ PD Mellar: Hydrocodone . In: PD Mellar et al .: Opioids in Cancer Pain . Oxford University Press, 2009, pp. 89 ff., Books.google.de
9. ↑ H. Schneider, P. Husslein, KTM Schneider: Die obstetrics . 2nd Edition. Springer Verlag, Berlin / Heidelberg 2004, ISBN 3-642-18574-6 , p. 889.

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