INTRODUCTION:-
* It is a narcotic analgesic that may be habit-forming.
* It is a controlled substance (opium derivative) listed in the U.S. Code of Federal Regulations,
* Internationally, heroin is controlled under Schedules I and IV of the Single Convention on Narcotic Drugs.
* It is illegal to manufacture, possess, or sell heroin in the United States and the UK. However, under the name diamorphine, heroin is a legal prescription drug in the United Kingdom.
MECHANISM OF ACTION :-
* It acts on endogenous mu-opioid receptors that are spread in discrete packets throughout the brain, spinal cord and gut in almost all mammals.
* Heroin, along with other opioids, are agonists to four endogenous neurotransmitters. They are beta-endorphin, dynorphin, leu-enkephalin, and met-enkephalin.
* The body responds to heroin in the brain by reducing (and sometimes stopping) production of the endogenous opioids when heroin is present.
* Endorphins are regularly released in the brain and nerves, attenuating pain.
* Their other functions are still obscure, but are probably related to the effects produced by heroin besides analgesia (antitussin, anti-diarrheal).
PHARMACODYNAMICS :-
* The onset of heroin's effects is dependent on the method of administration.
* Taken orally, heroin is totally metabolized in vivo into morphine before crossing the blood-brain barrier; so the effects are the same as oral morphine.
* Take by injection, heroin crosses into the brain. Once in the brain, heroin is rapidly metabolized into morphine by removal of the acetyl groups, therefore, it is known as a prodrug.
HALF LIFE :-
* <10 minutes
ROUTE OF ELIMINATION :-
* 90% renal as glucuronides, rest biliary
THERAPEUTIC USES :-
* Used in the treatment of acute pain, myocardial infarction, acute pulmonary edema, and chronic pain.
SIDE EFFECTS :-
* Bad teeth
* Inflammation of the gums
* Constipation
* Cold sweats
* Itching
* Weakening of the immune system
* Coma
* Respiratory (breathing) illnesses
* Muscular weakness, partial paralysis
* Reduced sexual capacity and long-term impotence in men
* Menstrual disturbance in women
* Inability to achieve orgasm (women and men)
* Loss of memory and intellectual performance
* Introversion
* Depression
* Pustules on the face
* Loss of appetite
* Insomnia
WITHDRAWAL SYMPTOMS :-
Sweating, anxiety, depression, watery eyes, chills, vomiting, sleep difficulty, excessive yawning.
DRUG –DRUG INTERACTIONS :-
HEROIN+ALCOHOL= increased action of heroin.
HEROIN+BENZODIAZEPINE=synergistic interactions with heroin.
HEROIN +TRICYCLIC ANTIDEPRESSANT=cardiac arrhythmias, seizures, and apnea.
REFERENCE:-Tripathi K D ;"Essential of medical pharmacology"7th edition;page no - 474
* It is a narcotic analgesic that may be habit-forming.
* It is a controlled substance (opium derivative) listed in the U.S. Code of Federal Regulations,
* Internationally, heroin is controlled under Schedules I and IV of the Single Convention on Narcotic Drugs.
* It is illegal to manufacture, possess, or sell heroin in the United States and the UK. However, under the name diamorphine, heroin is a legal prescription drug in the United Kingdom.
MECHANISM OF ACTION :-
* It acts on endogenous mu-opioid receptors that are spread in discrete packets throughout the brain, spinal cord and gut in almost all mammals.
* Heroin, along with other opioids, are agonists to four endogenous neurotransmitters. They are beta-endorphin, dynorphin, leu-enkephalin, and met-enkephalin.
* The body responds to heroin in the brain by reducing (and sometimes stopping) production of the endogenous opioids when heroin is present.
* Endorphins are regularly released in the brain and nerves, attenuating pain.
* Their other functions are still obscure, but are probably related to the effects produced by heroin besides analgesia (antitussin, anti-diarrheal).
PHARMACODYNAMICS :-
* The onset of heroin's effects is dependent on the method of administration.
* Taken orally, heroin is totally metabolized in vivo into morphine before crossing the blood-brain barrier; so the effects are the same as oral morphine.
* Take by injection, heroin crosses into the brain. Once in the brain, heroin is rapidly metabolized into morphine by removal of the acetyl groups, therefore, it is known as a prodrug.
HALF LIFE :-
* <10 minutes
ROUTE OF ELIMINATION :-
* 90% renal as glucuronides, rest biliary
THERAPEUTIC USES :-
* Used in the treatment of acute pain, myocardial infarction, acute pulmonary edema, and chronic pain.
SIDE EFFECTS :-
* Bad teeth
* Inflammation of the gums
* Constipation
* Cold sweats
* Itching
* Weakening of the immune system
* Coma
* Respiratory (breathing) illnesses
* Muscular weakness, partial paralysis
* Reduced sexual capacity and long-term impotence in men
* Menstrual disturbance in women
* Inability to achieve orgasm (women and men)
* Loss of memory and intellectual performance
* Introversion
* Depression
* Pustules on the face
* Loss of appetite
* Insomnia
WITHDRAWAL SYMPTOMS :-
Sweating, anxiety, depression, watery eyes, chills, vomiting, sleep difficulty, excessive yawning.
DRUG –DRUG INTERACTIONS :-
HEROIN+ALCOHOL= increased action of heroin.
HEROIN+BENZODIAZEPINE=synergistic interactions with heroin.
HEROIN +TRICYCLIC ANTIDEPRESSANT=cardiac arrhythmias, seizures, and apnea.
REFERENCE:-Tripathi K D ;"Essential of medical pharmacology"7th edition;page no - 474
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