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Heroin

Generic: Diamorphine
Common Name: Diacetylmorphine, Diamorphine

Medicinal Chemistry

Molecular Weight 369.42
Molecular Formula C21H23NO5
IUPAC Name
(5alpha,6alpha)-7,8-didehydro-4,5-epoxy-17-methylmorphinan-3,6-diol diacetate

Pharmacognosy

Biological Source

Semi-synthetic from Morphine (Papaver somniferum)

Active Constituents

Morphine (precursor)

Pharmacology & Synthesis

Mechanism of Action

Rapidly crosses BBB and is deacetylated to 6-MAM and morphine; potent mu-opioid agonist.

Pharmacokinetics (ADME)

A: Rapidly absorbed via IV/Inhalation.
D: Highly lipophilic, extremely rapid BBB crossing.
M: Rapid hydrolysis by blood esterases.
E: Renal.

Pharmacodynamics

Intense euphoria, profound analgesia, severe respiratory depression.

Synthesis Pathway

Acetylation of morphine with acetic anhydride.

Safety, Warnings & Interactions

Adverse Effects

Addiction, respiratory depression, constipation.

Contraindications

Non-medical use; severe respiratory instability.

Drug Interactions

Severe synergy with alcohol and CNS depressants.

Pharmaceutics & Compendia

Dosage Forms Injection, Illicit powders
Official Compendia BP
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