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Narcotics Analgesics
Mohd Asad Farooqi
Analgesics
An analgesic, or painkiller, is any member of the group
of drugs used to achieve analgesia — relief from pain.
Major classes of Analgesic Drugs include:
➢ Opioids
➢ NSAIDs
➢ Acetaminophen/ PCM
➢ Flupirtine
➢ Ziconotide
NarcoticsAnalgesic/Opioids
Narcotic analgesics are drugs that relieve pain,
by binding to opioid receptors, which are
present in the central and peripheral nervous
system, can cause numbness and induce a state
of unconsciousness.
Classified into:
Natural Compounds: Morphine, Codeine, Papaverine
Semi-Synthetic: Diacetylmorphine (Heroin), benzylmorphine
and ethylmorphine
Synthetic Derivatives: Fentanyl, Pethidine, Methadone,
Tramadol and Propoxyphene
Loperamide, an opiate that does not enter the brain and
therefore lacks analgesic activity.
Mechanism of Action
All opioid receptors are G-protein
coupled receptors and inhibit
adenylate cyclase.
They are also involved in
➢ Postsynaptic hyperpolarization
(increasing K+ efflux)
➢ Reducing presynaptic Ca++ influx
thus inhibits neuronal activity.
Opioid Receptors
All opioid receptors are linked through G-proteins to
inhibition of adenylate cyclase. They also facilitate
hyperpolarisation) and inhibit
opening of potassium channels
opening of
(causing
calcium
channels (inhibiting transmitter release).
They are of 4 types:
➢ μ receptor
➢ σ receptor
➢ δ receptor
➢ Κ receptor
μ-Receptors are thought to be responsible for most of the
analgesic effects of opioids, and for some major unwanted
effects. Most of the analgesic opioids are μ-receptor
agonists.
➢ κ-Receptors contribute to analgesia at the spinal level and
may elicit sedation and dysphoria, but produce relatively
few unwanted effects and do not contribute to
dependence.
➢ δ-Receptors are probably more important in the periphery
and may also contribute to analgesia.
➢ σ-Receptors are not true opioid receptors and it is unclear
that what delta actually responsible for but may regulate
mu receptor activity.
Morphine
Morphine is the major analgesic drug contained in crude
opium and is the prototype strong agonist.
Morphine may be given by injection (intravenous or
intramuscular) or by mouth, often as slow-release tablets.
It is metabolized to morphine-6-glucuronide, which is
more potent as an analgesic.
Actions of Morphine:
➢Analgesia
➢Euphoria and sedation
➢Respiratory depression and suppression of cough
➢Nausea and vomiting
➢Reduced gastrointestinal motility, causing constipation
➢Histamine release, causing bronchoconstriction.
Disadvantage:
➢ Drug of addiction due to euphoric effect
➢ Over dose causes poisoning i.e. Coma and Respiratory
Depression.
➢ Cause dryness of mouth, mental clouding, vomiting,
headache, fatigue, constipation etc.

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pharmacology of Narcotics Analgesics

  • 2. Analgesics An analgesic, or painkiller, is any member of the group of drugs used to achieve analgesia — relief from pain. Major classes of Analgesic Drugs include: ➢ Opioids ➢ NSAIDs ➢ Acetaminophen/ PCM ➢ Flupirtine ➢ Ziconotide
  • 3. NarcoticsAnalgesic/Opioids Narcotic analgesics are drugs that relieve pain, by binding to opioid receptors, which are present in the central and peripheral nervous system, can cause numbness and induce a state of unconsciousness.
  • 4. Classified into: Natural Compounds: Morphine, Codeine, Papaverine Semi-Synthetic: Diacetylmorphine (Heroin), benzylmorphine and ethylmorphine Synthetic Derivatives: Fentanyl, Pethidine, Methadone, Tramadol and Propoxyphene Loperamide, an opiate that does not enter the brain and therefore lacks analgesic activity.
  • 5. Mechanism of Action All opioid receptors are G-protein coupled receptors and inhibit adenylate cyclase. They are also involved in ➢ Postsynaptic hyperpolarization (increasing K+ efflux) ➢ Reducing presynaptic Ca++ influx thus inhibits neuronal activity.
  • 6. Opioid Receptors All opioid receptors are linked through G-proteins to inhibition of adenylate cyclase. They also facilitate hyperpolarisation) and inhibit opening of potassium channels opening of (causing calcium channels (inhibiting transmitter release). They are of 4 types: ➢ μ receptor ➢ σ receptor ➢ δ receptor ➢ Κ receptor
  • 7. μ-Receptors are thought to be responsible for most of the analgesic effects of opioids, and for some major unwanted effects. Most of the analgesic opioids are μ-receptor agonists.
  • 8. ➢ κ-Receptors contribute to analgesia at the spinal level and may elicit sedation and dysphoria, but produce relatively few unwanted effects and do not contribute to dependence. ➢ δ-Receptors are probably more important in the periphery and may also contribute to analgesia. ➢ σ-Receptors are not true opioid receptors and it is unclear that what delta actually responsible for but may regulate mu receptor activity.
  • 9. Morphine Morphine is the major analgesic drug contained in crude opium and is the prototype strong agonist. Morphine may be given by injection (intravenous or intramuscular) or by mouth, often as slow-release tablets. It is metabolized to morphine-6-glucuronide, which is more potent as an analgesic. Actions of Morphine: ➢Analgesia ➢Euphoria and sedation ➢Respiratory depression and suppression of cough ➢Nausea and vomiting ➢Reduced gastrointestinal motility, causing constipation ➢Histamine release, causing bronchoconstriction.
  • 10. Disadvantage: ➢ Drug of addiction due to euphoric effect ➢ Over dose causes poisoning i.e. Coma and Respiratory Depression. ➢ Cause dryness of mouth, mental clouding, vomiting, headache, fatigue, constipation etc.