Heroin

Products

Heroin (med. diamorphine) is commercially available as an injectable and in tablet form (Diaphin). It has been approved as a drug in many countries since 2001.

Structure and properties

Heroin is a diacetylated derivative of the opium ingredient morphine and belongs to the opioid group. It is present in drugs as diamorphine hydrochloride monohydrate (C21H24ClNO5 – H2O, Mr = 423.9 g/mol) is present, a white crystalline powder that is readily soluble in water. Heroin is lipophilic and therefore passes readily through the blood–brain barrier into the central nervous system where it induces a “flash” when administered intravenously. It is a prodrug that is deacetylated to the active metabolites morphine and 6-ortho-monoacetylmorphine. It can be synthesized with morphine and acetic anhydride.

Effects

Heroin (ATC N02AA09) has analgesic, psychotropic, sedative (depressant), sedative, and cough-irritant properties. The effects are due to binding to µ-opioid receptors.

Indications

For substitution treatment of severe heroin dependence.

Abuse

Heroin is abused as a euphoric and depressant intoxicant.

Dosage

Heroin is primarily injected intravenously but may also be delivered perorally.

Contraindications

  • Hypersensitivity
  • Obstructive respiratory diseases
  • Respiratory depression
  • Intestinal obstruction
  • Increased intracranial pressure
  • Brain injuries
  • Headache and abdominal pain of unknown cause
  • Phaeochromocytoma
  • Concurrent use of MAO inhibitors.

For complete precautions, see the drug label.

Interactions

Drug-drug interactions include those with central depressant medications, alcohol, MAO inhibitors, and other intoxicants.

Adverse effects

The most common possible adverse effects include hypersensitivity reactions, vasodilatation, orthostatic discomfort, urticaria, pruritus, headache, loss of libido, constipation, poor appetite, nausea, and vomiting. Heroin can cause life-threatening respiratory paralysis. It rapidly induces physical and psychological dependence and causes withdrawal symptoms upon discontinuation. Contaminated syringes can cause infectious diseases such as hepatitis and HIV.

Overdose

Overdose is life-threatening. Symptoms include small pupils, respiratory depression, drop in blood pressure, shock, central disturbances, dullness, low body temperature, loss of skeletal muscle tone, circulatory failure, and coma.