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heroin

Prodrug (to 6-monoacetylmorphine and morphine) · Analgesic (illicit use)

Prodrug (to 6-monoacetylmorphine and morphine)Analgesic (illicit use)
CDSCO approved
EXCRETION
not curated
INTERACTIONS
1 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 2
  • Cns DepressantsSevereTextbookG&G 14e

Mechanism

Heroin (diacetylmorphine) is rapidly hydrolyzed to 6-monoacetylmorphine (6-MAM), which is then hydrolyzed to morphine. Heroin and 6-MAM are more lipid soluble than morphine, allowing faster entry into the brain. Morphine then acts as a mu-opioid receptor agonist.

Indications

Not listed as a therapeutic indication in the context of this chapter, but implicitly 'analgesia' due to conversion to morphine.

Pharmacokinetics

Metabolism
Rapidly hydrolyzed to 6-monoacetylmorphine (6-MAM), then to morphine
Excretion
Mainly in the urine, largely as free and conjugated morphine

Contraindications

  • Combined with CNS depressants

Side effects

Common
sedative (less prominent than morphine)emetic (less prominent than morphine)hypotensive (less prominent than morphine)
Serious
  • Respiratory depression
  • Increased fatalities when combined with CNS depressants
  • Pulmonary infections (especially tuberculosis)
  • Bacterial infections
  • Skin abscesses
  • Endocarditis
  • Viral infections (Hepatitis C, AIDS)
  • more euphoriant (especially on i.v. injection)
  • highly addicting

Drug interactions

Cns Depressants
Severe
Textbook

Increased fatalities.

Avoid combination.

Source: G&G 14e

Cocaine
Moderate
Textbook

Improved euphoria; reduction of negative side effects from each substance.

Not explicitly stated as this is a combination of illicit drugs.

Source: G&G 14e

Related guidelines

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Sources: KD Tripathi 7e, Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team