2. Introduction
Heroin is considered to be one of the most addicting drugs
of abuse
It is a lipid soluble "prodrug"
meaning that heroin itself is inactive but after crossing the
blood-brain barrier, heroin is metabolized into morphine.
3. Class of the prodrug
Heroin is a semi-synthetic opioid
Opioids are substances that act on opioid receptors to
produce morphine-like effects.
4. Indications
Heroin currently has no FDA-approved indications for use.
Medically are primarily used for pain relief and anesthesia
illegally, People inject, sniff, snort, or smoke heroin.
5. Why this prodrug is formed
Heroin, (diacetylmorphine), is very efficient prodrug and
more potent than morphine.
Many deaths are caused by heroin overdoses throughout the
world each year.
6. Biotransformation mechanism
(Heroin is produced by the direct acetylation of morphine)
heroin is rapidly hydrolyzed in the body to two products
namely, 6-monoacetylmorphine (MAM) and morphine
Which they are the active metabolite or active form of heroin
8. Mechanism of action
Heroin is synthetically derived from the morphine alkaloid in
opium and is approximately twice as potent as morphine.
Heroin acts agonistically on the central nervous system (CNS)
opioid receptors mu, kappa, and delta.
Mu receptor effects account for both the analgesic effects,
respiratory depression and euphoria. Activation of Mu receptors
also causes miosis, and physiologic dependence.
Kappa receptor activation causes some degree of analgesia as
well.
Delta receptors are more involved in spinal analgesia phenomena
