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Opioide (of lat. "opium similarly ") are medicaments of the group of the means against the pain (analgesics).
The name of the group of materials is derived from the natural material mixture Opium, whose components of Opiate are called, under what among other things morphine is.
Most Opiate interact with the Opioidrezeptoren. Opioide all materials are generally called, which work as ligands to the Opioidrezeptoren, under what also substances are, which do not belong to the natural Opiaten, like for example the Methadon, as well as body-own Opiode.
Opioide are used as analgesics. In addition, they are as craze means of importance. They are subject to the (Germany) and/or craze central law (Austria).
The group of the Opioide is a chemically heterogeneous sub-group of the analgesics: They unfold their characteristics by reciprocal effect with special receptors (molecular connection places) on the surface of the nerve cells and other kinds of cells generally speaking bodies, which are called Opioidrezeptoren.
The body-own ligands of the Opioidrezeptoren are endogenous Peptide (Enkephaline and Endorphine), which are in the stress answer of importance. The Opioiderezeptoren comes most frequently in the brain at the soil 4. Ventricle forwards. They are besides in the periphery to find among other things in the intestine.
Exemplarily for a Opioid with effect exclusively outside of the brain is Loperamid, a means against failure (diarrhea). It overcomes the blood-brain barrier normally not and can therefore not in the brain, but only in the body work. It causes a slowing down of the Darmmotorik.
Opioide unfold their analgetische effect priority contrary to the Nichtopioid analgesics in the central nervous system (ZNS).
Several different types and Subtypen of the Opioidrezeptoren are differentiated
| Type | Localization | Effect |
|---|---|---|
| (M1) and (M2) | Brain | Analgesie, breath depression, heart cycle effects |
| spinal | Analgesie, stomach intestine effect, euphoria, craze | |
| peripheral | Analgesie, stomach intestine effect, itching | |
| (Kappa) | Brain, spinal | Analgesie, sedation, Dysphorie |
| d (delta) | Brain, spinal, peripheral | Stomach intestine effect, modulating effect |
| so far not identified receptor | Miosis, nausea, vomiting |
The individual substances knew different affinities for the individual receptor types and there effects release or them block. Some Opioide works thereby specifically on only one type of receptor, some nonspecific on several or all.
If a substance releases an activating effect at the receptor with the Andocken, one speaks of a Opioidagonisten. So e.g. are. Morphium and heroin pure and cause thus pronounced pain satisfying in addition, breath depression.
Opioidantagonisten dock likewise at the receptor on, do not solve him however not out he "are clogged" and are not available for the Andocken of Agonisten occasionally not. Therefore antagonists can block effects of Agonisten or waive their effect. Thus for example Naloxon waives the effect of Morphium and heroin. This circumstance becomes in the emergency medicine with the treatment of (e.g. Heroin overdose with dependent ones) used.
| relative power | Period of effectiveness | Receptor specification | Remark | |
|---|---|---|---|---|
| Morphine | 1 | 3 hr. | purely | |
| Fentanyl | 100-300 | 30 min | ||
| Alfentanil | 40-50 | 7-10 min | ||
| Remifentanil | 200 | 1 min (8 min [1]) | Due to the short period of effectiveness Remifentanil is considered as very good controllable. It is therefore used in the framework of the TIVA preferentially. Since the effect arrests rapidly after the end of the infusion, considerations must be employed to the post office-operational pain fight. If necessary Remifentanil is already necessary under strictly controlled conditions in minimum dosage is continued to give before the Narkoseausleitung the application of a longer effective Opioids or. With small invasiven interferences frequently the gift of a potent Nichtopioid analgesic is enough. | |
| Sufentanil | 1000-1500 | |||
| Buprenorphin | 40-50 | 1-1,5 | partial -antagonist | works with exclusive gift pain-satisfying, in combination with Agonisten antagonistically! |
| Naloxon | 30-45 min | pure antagonist , d) |
Opioide pain means, which are not subject to the :
Opioide pain means, which are subject to the BtMG:
As withdrawal symptoms immediately after setting all Opiate and other medicines off unrest, unfounded pain feeling, depressions, vomiting and gastrospasms, failure, exhaustion or flu-similar indications can appear. Convulsions do not arise in the Opioidentzug.
The withdrawal of Opioiden belongs to the lengthiest at all. So still another one year of late aftereffects such as sleep disturbances or can occur with preceded strongly regular consumption, which decrease however with the time in frequency and strength.
See also physical withdrawal
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