Some Opioids Based Medications for Pain

Tramadol

Tramadol is a rather weak opioid in terms of its analgesic effect, it is only about 0.1 times as effective as morphine – yet it has a strong euphoric potential and should not be underestimated. Tramadol is only available on prescription, but you shouldn’t be carried away by the fallacy that it is harmless. The addiction potential is roughly on par with other opioids. It flows in and out very slowly and has a half-life of up to 10 hours including that of the active metabolites.
Due to its special mechanisms of action, tramadol is more of a stimulant in moderate doses; some users even attribute a slight MDMA (XTC) – similar effect – to tramadol without the negative aspects that MDMA brings with it. Others, on the other hand, don’t care that much. In general, however, tramadol is quite popular.
Epileptics or people with a tendency to seizures should avoid it in any case.
Lethal dose: The dl50 in rats is given by some sources as 250 mg / kg body weight for tramadol – in humans this value is probably lower, here, for an average adult weighing 70 kg, 10-20 mg / kg body weight can be fatal if there is tolerance the value on tramadol is correspondingly higher (the tolerance to tramadol is especially important here, as this has special mechanisms of action (see detailed info), although there are cross-tolerances to other opioids.
Application forms:
capsule, prolonged-release tablet, drops, injection solution, suppository, effervescent tablet
Status: Prescription requirement, not subject to the BtmG

Meptazionol

Meptazinol is a very rarely used, partially agonistic
opioid. With a half-life of only 2 hours, it is also effective for a relatively short time.
For example, it is occasionally used in obstetrics to relieve pain in labor
. In terms of potency, it is about the level of tramadol, its
partially agonistic properties suggest that the euphoric
potential is rather low (I haven’t been able to test it myself so far, who has had
experience with it, but is welcome to describe it in the forum).
Application form: Inj. Solution
Status: Prescription requirement, not subject to the BtmG
Dextropropoxyphene
Dextropropoxyphene is an opioid (trade name: Develin®) that is no longer approved in Germany, which was used for analgesia and substitution. Somewhat weaker than codeine in terms of potency.
Former status: prescription requirement – was not subject to the BtmG, but now in Annex II.

Codeine

Codeine is a well-known and widely used opioid, both for dry coughs and pain. Codeine is available in the form of many combination and monopreparations. Codeine has a half-life of about 3-6 hours including the effects of the active metabolites.
Codeine also produces pronounced euphoric effects, but compared to tramadol, codeine is a sedating opioid, while tramadol is more active. Also, the drainage of codeine is faster and not quite as gentle as that of tramadol.
Changes to the structure have created even more effective codein derivatives. The best known are hydrocodone (potency ~ 15x) and oxycodone (potency ~ 30x).
Application forms: juice, drops, tablets, capsules
Status: Prescription requirement – Codeine is not subject to the BtmG up to 100mg codeine / divisible unit or 2.5% / ml

Dihydrocodeine

DHC is about 1.1-1.5x as potent as codeine, otherwise similar to codeine.
The constipating (constipating) effect is more pronounced than that of codeine, and it also has a somewhat shorter effect. The main clinical area of ​​application is the treatment of severe dry coughs, as it, like codeine, has an antitussive effect. It is also used as an analgesic for severe pain; in this country it is no longer approved as a substitute for opioid addiction.
Application forms: prolonged-release tablet, drops, juice
Status: Like Codeine!

Tilidine

Tilidine is the strongest fully agonistic opioid analgesic that is still available in Germany without a prescription for anesthetic.
However, this Btm exemption only applies to tilidine-naloxone combinations with a proportion of 8% naloxone (based on the base). With this combination, two things should be achieved:
On the one hand, to put a stop to high-dose abuse from 300-400mg.
On the other hand, and for this reason it was considered to be even more important, that these combination preparations cannot be administered parenterally (e.g. iv) by addicts, because the naloxone takes effect immediately and antagonistically occupies the receptors in high concentrations, which leads to withdrawal symptoms. More on this on the detail page.
Tilidine is a popular analgesic due to its pronounced analgesic effect, and also has a very pronounced euphoric effect.
At this point it should be mentioned again that the contained naloxone
does not protect against addiction, nor does it in principle prevent abuse – only very high doses or parenteral administration are not possible with it.
Application forms: tablet, prolonged-release tablet, capsule, drops, solution for injection
Status: Solution for injection: Btm; Tilidine / naloxone combinations: prescription required

Pethidine

In the past it was even used for intravenous anesthesia, today pethidine is only used in postoperative, acute or, in rare cases, long-term analgesia.
Pethidine is not significantly stronger than Tilidine, it also works a little shorter, but the onset of action is generally a little faster. Pethidine also has a pronounced euphoric component, but it also has a special feature: the active metabolite norpethidine has antispasmodic properties and also accumulates with continuous pethidine administration, which in many cases makes it impractical, if not unusable, for long-term analgesia. This is also a problem with a strong dependency, which is why you should definitely switch to another opioid.
In the case of occasional use (e.g. brief periods of pain), this problem can be neglected, provided one has no pre-existing predisposition to seizures and does not combine it with other unsuitable substances.
Application forms: prolonged-release tablet, solution for injection
Status: Btm

Pentazocine

Pentazocine is a partial agonist which antagonistically occupies the µ-receptor and therefore binds to the kappa receptor.
In its therapeutic potency about 1.5 times as strong as pethidine, it is mainly used for acute analgesia. Pentazocine is not supposed to “wind up” like other opioids, which may be due to the fact that it is only a
partial agonist.
Application forms: capsules, suppositories, solution for injection

Nalbuphine

Nalbuphine is a partial agonist. It agonizes the kappa receptors and partially agonizes the µ receptors.
With a potency of 0.5-0.6 it is quite strong and despite this only requires a prescription, since nalbuphin is probably not considered to be that dangerous.
Application forms: Inj. Solution
Status: Prescription requirement, not subject to the BtmG

Piritramide

Piritramid (Dipidolor®) is the strongest, low-potency opioid currently in clinical use. It has a strong euphoric component and it relieves pain really well.
It seems to be quite unknown among consumers who do not socialize with medical experts or who deal more intensively with the topic.
Clinically, it is only used for acute analgesia (e.g. after operations) in the case of severe to very severe pain.
With a half-life of 5-10 hours it is also effective for a comparatively long time.
Application form: solution for injection
Status: Btm (subject to the BtmG)

Morphine

Morphine is the “grandpa” of clinical opioid analgesics.
It is the main alkaloid of the opium poppy and was first isolated ~ 1805; It was synthesized for the first time in 1952.
Morphine is used in today’s medicine for acute / long-term analgesia and, in very rare cases, for anesthesia and against severe diarrhea.
It also has a strong euphoric effect, but its sedative component is stronger than that of piritramide, which overshadows the euphoria somewhat and you don’t notice what’s going on around you after anesthesia (although these are relative subtleties, since piritramide also sedates significantly ). Although it is Btm, morphine is the second most common Btm opioid on the scene
Morphine is the reference substance for the calculation of the potency
among the pharmaceutical opioids (with a potency of 1).
Application forms: tablet, prolonged-release tablet, drops, injection solution, dry
substance, suppository
Status: Btm

Hydrocodone

Relatively rarely used antitussive. It is rarely used as an analgesic in this country; in other countries, paracetamol / hydrocodone combinations have
become established, almost like the paracetamol / codeine combinations here.
Application forms: tablet, solution for injection
Status: Btm

Diacetylmorphine

(Heroin)

Diacetylmorphine (Heroin®, “Schore”, “Braunes” …) was produced around 1890 by what was then “Farbenfabriken vorm. BAYER & Co.” synthesized and sold without a prescription as a kind of “universal drug”. At that time they did not know about the high potential for dependence. Only later did it require a prescription, then Btm.
Diacetylmorphine is not worse in terms of substance than other strong opioids (e.g. morphine, fentanyl, …). The quality of the “Strassen-Schore” is bad, and that will probably not change in the future either. In addition, pure diacetylmorphine is to be used again in Germany to replace addicts, but the conditions for this have so far been poor.
The quality of the “street hero” is on average 3-8% (!) – you only rarely get better!
Status: Btm Annex I (not marketable Btm, means: May not be used in clinics either)

Methadone

Methadone has a potency of 2.5 and has been used as a substitute for severely opioid addicts for years. The withdrawal is a little more difficult than that of DAM, however. The HWZ is very long.
Methadone is not available as a ready-made preparation; this is made from the substance in the pharmacy according to the doctor’s wishes.
Application forms: Individual preparation according to prescription
Status: Btm

Levomethadone

Levomethadone is basically the same substance as methadone, except that levomethadone does not refer to the racemate.
Levomethadone does not contain the barely effective dextro-enantiomer, which is why the difference in potency comes about.
is used both for substitution and – albeit rarely – for analgesia and as an antitussive in very severe cases.
Due to the very long elimination half-life, treatment in the event of overdosing is difficult, but on the other hand there are also possibilities for pain therapy – it is not for nothing that one sometimes (even if not entirely expertly) speaks of “natural retardation”.
Application forms: drops, solution for injection, solution
Status: Btm

Oxycodone

Oxycodone has a potency of ~ 3 and is also referred to by some as “the heroin of the rich”, which probably has two causes: On the one hand, oxycodone is said to be very euphoric, at least as strong as heroin (I can’t judge it myself, because I have this Opioid have not yet tested). On the other hand, the prices for oxycodone tablets are extremely high, there is no injection solution in this country and otherwise it seems to be very rare. Clinically, it is very often used for long-term analgesia in patients with chronic pain. Oxycodone is a more compatible alternative to morphine.
Application forms: prolonged-release tablet (in other countries also solution for injection)
Status: Btm

Hydromorphone

Used for acute and long-term analgesia in particularly severe cases when other analgesics are not sufficient. The analgesic effect is very strong, as is the euphoric one. It sedates only a little and therefore belongs to the group of opioids that are more active.
Hydromorphone has a potency of 7-7.5. It is perhaps worth mentioning here that the side effects are lower than those of morphine, which is due, among other things, to the fact that it is not metabolized to the likewise active morphine-6-glucuronide. Hydromorphone is an excellent alternative to morphine in pain therapy, precisely because it does not sedate as much and the side effects are significantly lower.
Application forms: prolonged-release tablet, solution for injection
Status: Btm

Oxymorphone

Oxymorphone is a relatively rare, fully agonistic opioid, which is probably even more powerful than oxycodone in terms of euphoria.
It has a therapeutic potency of around 10. Trade name: Numorphan® (however, it is not used in this country and is also not available). It is used for severe to severe pain
Application forms: solution for injection
Status: Not approved in Germany, Global Btm

Alfentanil

Alfentanil belongs to the group of anilinopiperidines and has a potency of ~ 25.
It is used for anesthesia and is quite a dangerous opioid. The onset of action of alfentanil is quite quick. Consumption without medical supervision is too dangerous, if only because of the high respiratory depressive potential.
Application forms: Injection solution
Status: Btm

Buprenorphine

Buprenorphine is a partial agonist, ie it does not agonize all receptors or it also has antagonistic properties.
Its analgesic effectiveness is not always given: Despite a potency of 30, it is only insufficiently effective in many pain patients, in contrast to whom the pain relief occurs with piritramide, which is only 0.04 times as potent.
Buprenorphine has a very high affinity so that it cannot be antagonized by naloxone, or only inadequately.
The substance is not Btm in all countries. Buprenorphine should also not be underestimated when it comes to the potential for dependence! Buprenorphine is used for substitution.
Application forms: sublingual tablet, injection solution, membrane plaster
Status: In this country Btm

Fentanyl

Fentanyl is the best known representative of the anilinopiperidines.
It is also a highly potent opioid and has a potency of ~ 100. It is used for anesthesia and acute / long-term analgesia when other measures are unsuccessful.
The doses for acute analgesia are around 100-300µg, for anesthesia it is 100-500µg initially.
In contrast to the other opioids, the anilinopiperidines do not induce histamine release, which leads to fewer side effects. The analgesic component is very strong, as is the sedative component. Fentanyl also has a pronounced euphoric component, but due to the strong sedation you don’t notice much of it (I can say from my own experience, since I’ve already had some anesthesia with fentanyl as an analgesic).
It is a very dangerous opioid and should never be used without professional supervision and naloxone availability as it can easily lead to respiratory depression / paralysis.
Exceptions are patients who have been clinically adjusted to the application of fentanyl membrane patches and have been under clinical surveillance for at least 7 days.
The pharmacokinetics of fentanyl is quite complex: Due to its high lipophilicity, it is quickly deposited in fat and muscle tissue, which is why the half-life increases disproportionately with the duration of application.
Application forms: membrane plaster, lollipop, injection solution
Status: Btm

Remifentanil

Ultra-short-acting opioid of the anilinopiperidine type which is used for short TIVA (total intravenous anesthesia (s)). In contrast to fentanyl, there is no extension of the half-life with increasing application time, since the remifentanil is immediately broken down by the body esterases. Thus, a TIVA can also be tapered off without any problems and (if properly organized) is even an ideal solution. Remifentanil is also very dangerous and must not be used without supervision and also with Remifentanil the euphoric component is partially overlapped by the sedating one
Application form: Inj. Solution
Status: Btm

Sufentanil

The clinical reference opioid since its inception.
With a potency of 700-1000 it is the current top among the medically used opioids.
It is often used for major cardiological interventions and also for obstetric anesthesia it is a frequently used opioid with the help of the local anesthetic bupivacaine.
Sufentanil should not be used without professional supervision / naloxone availability.
Application forms: solution for injection
Special opioids
Special opioids:
Dextromethorphan (DXM): DXM only has slight opioid-like effects in very high doses, which, however, do not come into play because the dissociative effects predominate.
Papaverine: An opiate without opioid effects, pure antispasmodic.

Cataleptics: The following opioids are used for catalepsy (immobilization) in large animals:

3-Methylfentanyl: Potency: ~ 3300, highly toxic, highly affinity
Etorphine: Potency: ~ 5000, very toxic, high affinity
Carfentanil: Potency: ~ 7500, very toxic, high affinity
Any handling of these 3 substances brings with it an incalculable risk. By the way, carfentanil is the strongest opioid.
Loperamide: A very strong opioid, but after overcoming the BBB it is transported out of the CNS in the opposite direction by active transport, which is why it only mediates peripheral effects (mainly constipation). It is then used in this area (against diarrhea).

opium
Opium is the dried milk sap of the opium poppy. It contains about 30 alkaloids. The most important are morphine, codeine, papaverine, narcotine and thebaine.
Opium can be smoked or eaten.

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