OPIOIDS

ENDOGENEOUS OPIOID
PEPTIDES
ENDORPHIN
ENKEPHALIN
DYNORPHIN

ACTIONS OF OPIOID RECEPTORS

(Mu)

Physical

dependence
Euphoria
Analgesia supra spinal & Spinal
Respiratory depression
Constipation
Growth hormone
Prolactin Secretion
ACH Release

 (Kappa)
Sedation
Analgesia

spinal & Supra spinal

Miosis
Dysphoria
Disorientation
ADH release

 (Delta)
Analgesia (spinal & supra spinal)
Release of growth hormone

OPIOID ANALGESICS
STRONG AGONISTS

Morphine
Meperidine
Methadone
Fentanyl
Sufentanil
Remifentanil
Alfentanil

MODERATE AGONIST
Codeine
Oxycodone
Propoxyphene
PARTIAL AGONIST
Buprenorphine
Butorphanol
Pentazosine
Nalbuphine

ANTAGONISTS
Naloxone
Naltrexone
Nalmefene

Mech Of Action

Ca++ channels
K+ Channels

open

AFFINITY OF OPIOIDS FOR RECEPTORS

OPIOID PEPTIDES

ENDORPHIN

+++

+++

+++

ENKEPHALIN

++

+++

DYNORPHIN

++

+++

MORPHINE

+++

++

ETORPHINE

+++

+++

+++

PETHIDINE

++

PHENAZOCINE

++

++

++

NALORPHINE

++

++

++

NALOXONE

+++

++

++

OPIOID DRUGS

ANTAGONISTS

Pharmacological Actions

(Central)
Analgesia
Euphoria
Sedation
Decreased respiration rate
Suppression of Cough reflex
Miosis
Nausea & Vomiting
Truncal rigidity
Continu

Pharmacological Actions
(Peripheral)
GIT
Biliary

tract

CVS
Neuroendocrine
Histamine
uterus

release

Tolerance
Tolerance;

reversible

Starts after the first dose

(clinically 2-3 weeks)
(constipation, Miosis, Convulsions)

Physical

dependence
Abstinence Syndrome

THERAPEUTIC USES

Analgesia (MI, PERICARDITIS, PRE & POST

OP)
Pulmonary edema (LVF, CCF)
Cough suppression
Pre Anesthesia
Neuroleptic analgesia
Opioid dependence (Methadone &
buprenorphene)
Shivering (Meperidine)

CONTRA INDICATIONS
o
o
o
o
o
o

HEAD INJURY
COPD
USE OF PURE AGONIST WITH WEAK
PARTIAL AGONIST
HYPOTHYROIDISM, ADDISONS DISEASE
IN PTS WITH RENAL OR HEPATIC FAILURE
DURING PREGNANCY

ADVERSE EFFECTS
Behavioral disturbance
NAUSEA & VOMITING
POSTURAL HYPOTENSION
URINARY RETENSION
INCREASED INTRACRANIAL PRESSURE
HYPOTHERMIA
ITCHING, URTICARIA
CONTIPATION
TOLERANCE & DEPENDENCE

MEPERIDINE ( Pethidine)
Phenylpiperidine derivative
Potency 75-100mg = 10mg Morphine
T1/2 3 hrs
Metabolism to nor-meperidine a strong CNS
stimulant
Marked anticholinergic (Mydriasis, Tachycardia)
No antitussive effect
Drug dependence common in health workers

 Methadone
Diphenoxylate,Difenoxin,Lopramide
Levopropoxyphen,

Dextromethorphane

Detoxification of addicts
Psychosocial

intervention
Pharmacological

Methadone
Clonidine, Lofexidine

Prevention

LOMOTIL (diphenoxylate 2.5mg + atropine 0.025mg)

MORPHINE + NALOXONE 0.04mg

Oxycodone CR ( Cap Rimixy)

COMMON OPIOID ANALGESICS

Name

Oral
Duration of
Parenteral Analgesia
Potency
(Hours)
Ratio

Maximum
Efficiency

Addiction
Abuse
Liability

Morphine

Low

4-5

High

High

Hydromorphone

Low

4-5

High

High

Oxymorphone

Low

3-4

High

High

Methadone

High

4-6

High

High

Meperidine

Medium

2-4

High

High

Fentanyl

Parenteral
Only

1-1.5

High

High

Sufentanyl

Parenteral
Only

1-1.5

High

High

Alfentanil

Parenteral
Only

0.25-0.75

High

High
(Contd)

Name

Oral
Parenteral
Potency
Ratio

Duration
of
Analgesia

Maximum
Efficiency

Addiction
Abuse
Liability

Levorphanol

High

4-5

High

High

Codeine

High

3-4

Low

Medium

Oral Only

4-5

Very low

Low

Pentazocine

Medium

3-4

Moderate

Low

Nalbuphine

Parenteral
only

3-6

High

Low

Buprenorphine

Parenteral
only

4-8

High

Low

Butorphanol

Parenteral
only

3-4

High

Low

Propoxyphene

(Hours)