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OPIOID AUTOCOIDS
PRESENTED BY
Sushma Arikella
Application no: d9b9687df31511e9b781cb6f05b890ea
Department of Pharmacology
G.Pulla reddy college of pharmacy
1
o Autacoid : Auta - self , Coid - Healing
o Autacoid is self healing substances.
o Autacoids also known as local harmones , and mostly
originated from diffused tissues and transported to various target
sites.
o Autacoids play an important role in physiological and
pathological process and act as neurotransmitters and
neuromodulators.
2
OPIOIDS
• Opioid is a psychoactive chemical that works by binding to
opioid receptors which are found principally in the CNS , PNS
and GIT.
• The receptors in these organ system mediate both the benificial
and side effects of opiods.
• Opioid drug function as agonist , partial agonist , antagonist.
3
CLASSIFICATION OF OPIOID
RECEPTORS
4
Opioid
receptors
µ
µ 1 µ 2
δ k
k1 k2
5
µ RECEPTOR K RECEPTOR δ RECEPTOR
LOCATION µ1 – supra spinal
µ2 - spinal
K1 – spinal
K3 – supra spinal
Spinal
Supra spinal
Analgesia
Respiratory depression
Sedation
Euphoria
Meiosis
Physical dependence
Loss of GI motility
Spinal analgesia
Dysphoria
Sedation
Psychomimetic
Physical
dependence
Spinal analgesia
Effective behaviour
Respiratory depression
Reduced GI motility
AGONISTS Morphine, codeine ,
fentanyl ,
pentazocine
pentazocine enkephalins
ANTAGONISTS Naloxone
Naltrexone
nalmefene
Naloxone
Naltrexone
nalmefene
Naloxone
Naltrexone
nalmefene
EFFECTS
6
Pharmacological action
 On CNS : Analgesic effect
Respiratory depression
sedation
 On Eyes : shows myosis
 On heart : shows bradycardia
 On Blood vessels : decrease BP
7
Classification of opioids
8
TRADITION ORIGIN FUNCTION
STRONG
Morphine
Pethidine
Fentanyl
Alfentanil
Remifentanil
Sufentanil
NATURALLY OCCURRING
Morphine
Codeine
Papavarine
Thebaine
PURE AGONISTS
Morphine
Fentanyl
Alfentanil
Remifentanil
Sufentanil
PARTIAL AGONIST
Buprenorphine
INTERMEDIATE
Buprenorphine
Pentazocine
Butorphanol
Nalbuphine
SEMISYNTHETIC
Diamorphine
Dihydrocodeine
Buprenorphine
AGONISTS-ANTAGONISTS
Pentazocine
Nalbuphine
Nalorphine
WEAK
Codeine
SYNTHETIC
Phenylpyperidines:
pethidine, fentanyl, alfentanil, sufentanil
Diphenylpropylamines:
methadone, dextropropoxyphene
Morphinans: butorphanol, levorphanol
PURE ANTAGONISTS
Naloxone
Naltrexone
9
Mechanism of action
10
acknowledgement
Academic writing
11
THANK YOU
12

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swayam-191031174644.pdf

  • 1. OPIOID AUTOCOIDS PRESENTED BY Sushma Arikella Application no: d9b9687df31511e9b781cb6f05b890ea Department of Pharmacology G.Pulla reddy college of pharmacy 1
  • 2. o Autacoid : Auta - self , Coid - Healing o Autacoid is self healing substances. o Autacoids also known as local harmones , and mostly originated from diffused tissues and transported to various target sites. o Autacoids play an important role in physiological and pathological process and act as neurotransmitters and neuromodulators. 2
  • 3. OPIOIDS • Opioid is a psychoactive chemical that works by binding to opioid receptors which are found principally in the CNS , PNS and GIT. • The receptors in these organ system mediate both the benificial and side effects of opiods. • Opioid drug function as agonist , partial agonist , antagonist. 3
  • 6. µ RECEPTOR K RECEPTOR δ RECEPTOR LOCATION µ1 – supra spinal µ2 - spinal K1 – spinal K3 – supra spinal Spinal Supra spinal Analgesia Respiratory depression Sedation Euphoria Meiosis Physical dependence Loss of GI motility Spinal analgesia Dysphoria Sedation Psychomimetic Physical dependence Spinal analgesia Effective behaviour Respiratory depression Reduced GI motility AGONISTS Morphine, codeine , fentanyl , pentazocine pentazocine enkephalins ANTAGONISTS Naloxone Naltrexone nalmefene Naloxone Naltrexone nalmefene Naloxone Naltrexone nalmefene EFFECTS 6
  • 7. Pharmacological action  On CNS : Analgesic effect Respiratory depression sedation  On Eyes : shows myosis  On heart : shows bradycardia  On Blood vessels : decrease BP 7
  • 9. TRADITION ORIGIN FUNCTION STRONG Morphine Pethidine Fentanyl Alfentanil Remifentanil Sufentanil NATURALLY OCCURRING Morphine Codeine Papavarine Thebaine PURE AGONISTS Morphine Fentanyl Alfentanil Remifentanil Sufentanil PARTIAL AGONIST Buprenorphine INTERMEDIATE Buprenorphine Pentazocine Butorphanol Nalbuphine SEMISYNTHETIC Diamorphine Dihydrocodeine Buprenorphine AGONISTS-ANTAGONISTS Pentazocine Nalbuphine Nalorphine WEAK Codeine SYNTHETIC Phenylpyperidines: pethidine, fentanyl, alfentanil, sufentanil Diphenylpropylamines: methadone, dextropropoxyphene Morphinans: butorphanol, levorphanol PURE ANTAGONISTS Naloxone Naltrexone 9