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Heroin (diacetylmorphine, or diamorphine in medicine) is a fast-acting semisynthetic opioid made by acetylating morphine. It is a prodrug; the body strips the acetyl groups off to release 6-monoacetylmorphine and morphine, which switch on mu-opioid receptors to produce pain relief, a rush of euphoria, and dangerous slowing of breathing.
- Powerful, fast relief of severe pain (as medical diamorphine)
- Intense but short-lived euphoria or rush
- Strong sedation and relief of anxiety or distress
- Suppresses cough and calms the gut
- Used in UK palliative care and, in supervised clinics, as heroin-assisted treatment for refractory dependence
- Respiratory depression and fatal overdose, made far worse by fentanyl-contaminated supply
- Rapid tolerance, physical dependence, and addiction
- Withdrawal: cramps, diarrhea, sweating, insomnia, and severe craving
- Constipation, nausea, itching, and pinpoint pupils
- Injection harms: abscesses, endocarditis, and HIV or hepatitis C from shared needles
- Often deadly when combined with alcohol or benzodiazepines
Overview
Heroin is diacetylmorphine, formula C21H23NO5, molar mass about 369.4 g/mol, CAS 561-27-3, PubChem CID 5462328. Chemically it is just morphine with two acetyl groups bolted on, and that small change is the whole story; the acetyl groups make the molecule far more fat-soluble, so it slips across the blood-brain barrier within seconds of reaching the bloodstream. Once inside, enzymes clip the acetyl groups back off, turning it into 6-monoacetylmorphine and then morphine, the compounds that actually do the work at opioid receptors.
That fast entry is why an injection or a smoke of heroin hits harder and quicker than the same amount of morphine, and it is a big part of why the drug is so strongly reinforcing. Bayer first sold it in 1898 as a cough remedy, marketed as a supposedly non-addictive morphine substitute, which turned out to be badly wrong. Today it has essentially no legal recreational status; it sits in Schedule I in the United States, while the same molecule is used as a tightly controlled medicine called diamorphine in the United Kingdom.
Mechanism
Heroin is best understood as a delivery vehicle rather than the active drug itself. The parent molecule binds only weakly to opioid receptors, because the acetyl group on the 3 position masks the hydroxyl that receptors need to grab; what heroin is genuinely good at is crossing membranes. Its high lipophilicity lets it flood into the brain almost immediately, where carboxylesterases and cholinesterases in blood and tissue deacetylate it in stages. First it becomes 6-monoacetylmorphine (6-MAM), which is itself a potent mu-opioid and already carries the free 3-hydroxyl needed for binding; then it is hydrolyzed further to morphine.
Both 6-MAM and morphine are full agonists at the mu-opioid receptor (MOR), with weaker activity at the kappa and delta receptors. Activating MOR in the brain and spinal cord blunts pain signaling, triggers release in the reward pathway (the source of the euphoric rush), and quiets the gut and cough reflex; the catch is that the same receptors in the brainstem also control breathing, so a large enough dose simply switches off the drive to breathe. The half-lives tell the story of speed: heroin itself lasts only a few minutes in blood, 6-MAM around 15 to 20 minutes, and morphine roughly 2 to 3 hours, with the morphine glucuronides lingering longer.
receptor fingerprint
crosses rapidly
Carboxylesterases and cholinesterasedeacetylated by
Mu-opioid receptor (MOR)agonist (via 6-MAM and morphine)
Kappa-opioid receptor (KOR)agonist
Delta-opioid receptor (DOR)agonist
Diacetylmorphine (parent molecule)binds directly
Safetyrisks and cautions, not medical advice
The headline risk with heroin is that it stops you breathing. Because mu-opioid agonism suppresses the brainstem respiratory centers, an overdose brings slow shallow breathing, pinpoint pupils, blue lips, unconsciousness, and death if nobody intervenes; it can be reversed if the opioid antagonist naloxone (Narcan) is given in time, which is why keeping naloxone on hand saves lives. The danger has grown far worse on the illicit market, because much of what is sold as heroin is now cut with or outright replaced by illicitly made fentanyl, which is roughly fifty times more potent by weight; the user has no reliable way to know the real dose, and a small miscalculation is fatal.
Combining heroin with other depressants (alcohol, benzodiazepines such as Xanax, gabapentin, or other opioids) stacks the respiratory risk and is a common way people die. Regular use builds tolerance and physical dependence quickly, and stopping brings a miserable but rarely fatal withdrawal (aches, cramps, diarrhea, sweating, insomnia, and intense craving). Injecting carries its own harms: abscesses, endocarditis, and, when equipment is shared, HIV and hepatitis C. In the United States it is a Schedule I controlled substance, meaning no accepted medical use there; the legal medical form, diamorphine, exists only in a handful of countries such as the United Kingdom.
Subjective profileweighing the evidence above
There is no version of this worth recommending. It kills by stopping your breathing, the illicit supply is now widely replaced by fentanyl and cannot be dosed at all, and dependence arrives fast with brutal withdrawal. Anyone around opioids should keep naloxone within reach and never use alone.
Resources
No suppliers are provided for compounds like this. This entry is here for reference.
Research
- 1994first citedThe heroin metabolite, 6-monoacetylmorphine, activates delta opioid receptors to produce antino…
- 2010controlled trialSupervised injectable heroin or injectable methadone versus optimised oral methadone as treatme…
- 2017most recentExposure to fentanyl-contaminated heroin and overdose risk among illicit opioid users in Rhode…
- 1.The heroin metabolite, 6-monoacetylmorphine, activates delta opioid receptors to produce antinociception in Swiss-Webster mice.
- 2.Heroin and its metabolites: relevance to heroin use disorder (Translational Psychiatry, 2023)
- 3.Supervised injectable heroin or injectable methadone versus optimised oral methadone as treatment for chronic heroin addicts in England after persistent failure in orthodox treatment (RIOTT): a randomised trial.
- 4.Heroin maintenance for chronic heroin-dependent individuals (Cochrane Systematic Review, Ferri et al., 2011)
- 5.Exposure to fentanyl-contaminated heroin and overdose risk among illicit opioid users in Rhode Island: A mixed methods study.
- 6.Naloxone (StatPearls, NCBI Bookshelf)
- 7.Heroin, PubChem Compound Summary CID 5462328 (National Library of Medicine)
7 listed here; entry last updated August 2026
Reviews
My notesprivate to this device
FAQ
Is heroin the same thing as morphine?
Not quite; heroin is morphine with two acetyl groups added, which lets it reach the brain much faster. Once inside, your body converts it back into morphine, so morphine is essentially the active drug doing the work.
Why is fentanyl in heroin so dangerous?
Fentanyl is roughly fifty times stronger by weight and is often mixed into or sold as heroin. Because you cannot see or taste it, a normal-looking amount can hold a lethal dose, which is why overdose deaths have surged.
Does naloxone (Narcan) actually reverse a heroin overdose?
Yes; naloxone knocks opioids off the mu receptor and can restart breathing within minutes. It wears off faster than the opioids, though, so the person still needs emergency care in case the overdose returns.
Is heroin used as a medicine anywhere?
Yes, as diamorphine. The UK uses it for severe and palliative pain and, in supervised clinics, as heroin-assisted treatment for people who have not responded to methadone. In the US it is Schedule I with no approved medical use.
How addictive is it, and what is withdrawal like?
Very; tolerance and dependence can build within weeks of regular use. Withdrawal is intensely unpleasant (flu-like aches, cramps, diarrhea, sweating, insomnia, and craving) but is rarely life-threatening on its own, unlike alcohol or benzodiazepine withdrawal.
Adverse effects
- Respiratory depression and fatal overdose, made far worse by fentanyl-contaminated supply
- Rapid tolerance, physical dependence, and addiction
- Withdrawal: cramps, diarrhea, sweating, insomnia, and severe craving
- Constipation, nausea, itching, and pinpoint pupils
- Injection harms: abscesses, endocarditis, and HIV or hepatitis C from shared needles
- Often deadly when combined with alcohol or benzodiazepines