Drug intelligence / Profile preview

diamorphine

Development stage
Phase 3
Lead developer
Bayer
Modality
Small Molecules
Administration
Intravenous, Intramuscular, Subcutaneous, Inhalation, Intranasal, Intrathecal, Oral
01

Overview

Diamorphine, also known as diacetylmorphine or heroin, is a semisynthetic opioid analgesic derived from morphine. It is primarily used in some countries for the management of severe pain, such as that associated with cancer, myocardial infarction, palliative care, pulmonary edema, and postoperative pain[2][4][6]. Diamorphine acts as a prodrug; it rapidly crosses the blood-brain barrier due to its high lipid solubility and is then metabolized into 6-monoacetylmorphine and morphine[4][5][6]. These metabolites act as potent agonists at μ-opioid (mu), κ-opioid (kappa), and δ-opioid (delta) receptors in the central nervous system[5][6], leading to analgesia by inhibiting neural activity and reducing pain transmission. The drug produces effects such as euphoria, sedation, respiratory depression, nausea, constipation, tolerance development, physical dependence and withdrawal symptoms upon cessation[5]. Diamorphine is more potent than morphine but has a very short plasma half-life of about 2–3 minutes due to rapid metabolism[5][7]. While illegal for use or sale in many countries including the United States under the name heroin[1][4], it remains an approved prescription medication for severe pain management in some regions like the United Kingdom.

Brand names
Diamorphine
Other names
heroin
02

Targets

MOR (Mu opioid receptor)

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