Thebaine

Opium poppy alkaloids are akin to special receptors in the brain that are responsible for emotional background, pain, mood and regulate the functioning of major organs and systems. Thebaine is a substance that used to be positioned as a waste product, but it began to be used to synthesize strong narcotic analgesics.

Tebaine’s Latin trade and chemical name

Tebain in Latin is Tebainum. The chemical name is 4,5-alpha-Epoxy-3,6-dimethoxy-N-methyl-6,8-morphinadiene. Known by the trade name of the same name, Tebain. The synonym is considered to be paramorphine.

Pharmacological group

Refers to the pharmacological group – opioid narcotic analgesics. Substances of natural or synthetic origin, considered opioid receptor antagonists, stimulate the CNS.

They are classified into 3 major subtypes:

OR1 (δ or delta),
OR2 (k or kappa),
OR3 (μ or mu).

When using opioid medications, all 3 receptor subtypes are involved in the analgesic effect on the body. But the main role is assigned to the OR3 (μ or mu)-receptor. Its excitation leads to inhibition of respiratory center, euphoria and addiction to the drug. Peripheral opioid receptors can also cause constipation (obstipation), since they are responsible for the motility of the intestines.

Pure (natural) antagonists are considered: promedol, morphine, methadone, etc. Weak ones: propoxyphene, codeine, hydrocodone. Mixed: tramadol, buprenorphine, and pure opioid receptor antagonists: nalmefen, naloxone, etc.

In world practice, the number of deaths from overdose of opioid analgesics is increasing. The leader is USA. In Russia, their use is ambiguous, on the one hand, they are necessary for treatment of pain in inoperable stages, and on the other hand, they are considered especially dangerous because of the low knowledge base of their use by doctors.

Active ingredient and structural formula of the drug

The structural gross formula is C19H21NO3. Paramorphine is extracted from Papaver somniferum. The heads of unripe poppies are cut, the milky juice is excreted, which is collected and dried in a special way. This is followed by a mixture containing 0.2-1% thebaine.

It is not used in its original form; it is a highly toxic substance that is used to make powerful narcotic drugs. These include oxycodone, buprenorphine, and it is also part of omnopon. To obtain codeine from a technical mixture, a specific Meyerhein-Pandorff-Verlei reaction is carried out.

In extraction form, 3,6-dimethoxy-N-methyl-4,5-oxymorphinadiene-6,8 has a crystalline powder form. It is not opium in its pure form, far from morphine; in fact, the resulting compound is a poison. Tebaine, or the better known active ingredient, paramorphine, is banned for all purposes. It can only be found in trace amounts in a number of drugs that are strictly controlled by the government.
Mechanism of action of the drug

Tebaine is a Schedule II drug, the circulation of this substance, as well as other opiates (codeine, morphine) is strictly controlled. Restrictions are applied due to the fact that the effect of pure paramorphine negatively affects the work of organs and systems. The following effects may occur when taking thebaine:

• Severe irritability, the person behaves unpredictably.
• Agitation, hyperreflexivity.
• Motor activity is excessive, the person who has taken thebaine literally finds no place.
• Muscle spasms in the chest and throat.
• Tonicity and activity of the gastrointestinal tract is increased.
• Strong respiratory stimulation unlike morphine, which acts depressingly.

When administered, thebaine has an antispasmodic effect similar to strychnine. Blood pressure is severely lowered; for natural hypotensives, this can lead to collapse and death.

Need to know! Tebaine is more of a stimulant, similar to its structural analogues, with little sedative effect. Opium has very little of it, so it cannot suppress the psychoactive effect of morphine. However, it can provoke side effects and intensify the toxic effects of the drugs.

The component is processed and included in the composition of the following drugs:

Codeinum (codeine).
Naltrexone (naltrexone).
NaloxoneATX (naloxone).
Oxymorphonum.
Buprenorphine.

Under laboratory conditions, using the Dils-Alder reaction, thebaine is synthesized into Oxidone, Etorphine, Nalbuphine, etc.
Addiction Formation and Consequences of Use in Addicts

A crystalline substance, thebaine, comes in powder form. Insoluble in ether, alcohol, quickly diluted in chloroform.

According to the laws, the toxic effect of paramorphine on people has not been studied. In animals, on which experiments were conducted, the variability of action and consequences was noted. It is not possible to determine how the effects of taking pure thebaine will be addictive, or exactly what the consequences will be in humans.

It is assumed that long-term ingestion of the drug can theoretically be addictive. But the psychotropic effect is weak, so it is difficult to study it in detail. When taking it, the symptoms of acute poisoning are more likely to appear, which is difficult to compare with the pleasure expected from a narcotic substance.