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Heroin is a semisynthetic derivative of opium. The opioid family includes the following:
- Drugs that occur naturally in opium (from the poppy plant)
- Semisynthetic derivatives (e.g., hydromorphone, oxycodone)
- Synthetic compounds (e.g., meperidine, fentanyl, methadone)
- 23 years of age: mean age of 1st use (2012)
- ~50% of those who have used an opioid pain reliever for nonmedical uses state they obtained it for free from a friend or relative.
- Nonmedical use of opioid pain relievers can lead to eventual injection heroin use.
- Fetal exposure commonly involves polysubstance abuse.
- 60–80% of heroin-exposed infants develop withdrawal—dependent on maternal dosing and length of use.
- Most use experimentally or intermittently; few become addicted and use daily.
- Use of opioid analgesics has increased dramatically over the last 10 years and has become more common than heroin use.
- Most common substances were oxycodone, hydrocodone, and methadone
- Up to 1/3 of heroin users experience nonfatal overdose.
- Most occur in the home and with other people present.
- Risk factors include length of injecting history, concurrent use of CNS depressants, recent completion of substance abuse program, and recent release from prison.
- Most heroin deaths occur when drug is administered IV.
- Most deaths in patients in their late 20s or 30s, with significant drug dependence
- Males are 4 times more likely to die than females from heroin-related causes.
- Multiple drug use common in heroin-related death
- As of 2011, opioid pain relievers are responsible for more overdose fatalities than heroin and cocaine combined.
- Precise estimates of prevalence of use difficult
- ~2.9 million people used at least once.
- ~467,000 used in 2012 (double since 2001).
- Prevalence of fetal exposure <1–3.7%
- Well-absorbed from gastrointestinal (GI) tract, nasal mucosa, pulmonary capillaries, and SC and IM injection sites
- Oral dose less potent than parenteral because of 1st-pass hepatic metabolism
- IV heroin peaks in <1 minute; intranasal and IM heroin peak in 3–5 minutes.
- Very lipid soluble; crosses blood–brain barrier within 15–20 seconds
- Extensive distribution into skeletal muscle, kidneys, liver, intestine, lungs, spleen, brain, and placenta
- Rapidly crosses the placenta, entering fetal tissues within 1 hour
- Crosses into breast milk in quantities sufficient to cause addiction
- Excreted in urine as morphine
- Receptor types
- Mu (or OP3)
- Located in CNS, GI tract, and sensory nerve endings
- Effect: analgesia, euphoria, respiratory depression, physical dependence, GI dysmotility, miosis, pruritus, bradycardia
- Kappa (or OP2)
- Located in CNS
- Effect: analgesia, miosis, diuresis, dysphoria
- Delta (or OP1)
- Located in CNS
- Effect: spinal analgesia, modulation of mu receptors/dopaminergic neurons
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