Dimethylthiambutene

Dimethylthiambutene is a synthetic opioid analgesic drug, which is a derivative of thiambutene. It was developed in the 1950s during research into analogues of morphine and codeine that would retain their analgesic effects but be less addictive. Despite these aims, dimethylthiambutene is still capable of producing similar levels of physical dependence and is considered a controlled substance in many countries.

Pharmacology

Dimethylthiambutene acts as a mu-opioid receptor agonist. The mu-opioid receptors are a group of G-protein coupled receptors with opioids as ligands. The activation of these receptors opens the potassium channels (causing hyperpolarization) and closes calcium channels (preventing calcium influx). This reduces neuronal excitability, leading to the analgesic effects.

Medical Uses

Dimethylthiambutene is used for the treatment of moderate to severe pain. It can also be used as a part of an anesthesia protocol. However, due to its potential for abuse and addiction, its use is strictly regulated.

Side Effects

Common side effects of dimethylthiambutene include drowsiness, nausea, constipation, and dependence. In high doses, it can cause respiratory depression, which can be fatal.

Legal Status

In the United States, dimethylthiambutene is a Schedule I controlled substance, which means it has a high potential for abuse and no accepted medical use. In the United Kingdom, it is a Class A drug under the Misuse of Drugs Act 1971.

See Also

• Opioid
• Thiambutene
• Morphine
• Codeine