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Evaluation of analgesic Agents

Screening of Analgesics

454 PHL
Lab # 2

Outlines

Classification of analgesics
Morphine; MOA, Pharmacological
effects, Uses, Side effects
Morphine antagonists
Method of screening of narcotic
analgesic

March 5, 2007

454 PHL Lab II

Gamra Hamad

Analgesics
Narcotics
Ex. Morphine, Pethadine, Fentanyl

Non-narcotics
Ex. NSAID

March 5, 2007

454 PHL Lab II

Gamra Hamad

Morphine
Naturally occurring substance
Papaver Somniferous
Works on Opioid Receptors (mu),
(delta), and (kappa)
G-protein coupled receptors,
inhibition of adenylate cyclase
opening of Pot. Channels
(hyperpolarization of PSN)

opening of Cal. Channels ( NT)


March 5, 2007

454 PHL Lab II

Gamra Hamad

Morphine:
Pharmacological
Action s

Analgesia
Euphoria
Respiratory depression
Cough suppression
Nausea & vomiting
Pupillary constriction
Delay of gastric emptying
Histamine release

March 5, 2007

454 PHL Lab II

Gamra Hamad

Morphine: Side Effects

Sedation
Respiratory depression
Constipation
N&V
Itching
IOP
Tolerance & dependence
Euphoria
Hypotension

March 5, 2007

454 PHL Lab II

Gamra Hamad

Morphine Antagonists:
Naloxone
Competitive inhibitor
Blocks the actions of endogenous
opioid peptides as well as morphine
Treatment of respiratory depression
caused by opioid overdose

March 5, 2007

454 PHL Lab II

Gamra Hamad

Screening of Narcotic
Analgesics
Principle: record the response of animal to
a painful stimulus before & after
administration of analgesic

Thermal method
Hot plate method
Radiant heat method (light)
Tail-flick method (electronic current)

Mechanical method
tail clip method

March 5, 2007

454 PHL Lab II

Gamra Hamad

Screening of
Analgesic Action By
Hot Plate Method

Material
Drugs:

Morphine
Unknown

Instruments:

Cages
Stop watches
Thermostatically controlled hot plate
Thermometer

Animals: 30 mice
March 5, 2007

454 PHL Lab II

Gamra Hamad

Studying Morphine
Analgesic Action
Method
Group I, 6 mice
Test sensitivity of animal to heat (not
exceed 10 sec.)
Morphine (IP) 0.2ml/10 gm
Test sensitivity of animal to heat every 10
min for 60 min
Record ur results in the table

March 5, 2007

454 PHL Lab II

Gamra Hamad

Method: cont.
Method
Group II , 6 mice
Test sensitivity of animal to heat (not
exceed 10 sec.)
Unknown (IP) 0.2ml/10 gm
Test sensitivity of animal to heat every 10
min for 60 min
Record ur results in the table

March 5, 2007

454 PHL Lab II

Gamra Hamad

Table
Table 1 Change in the reaction time (sec.) over
60 min. in group injected with morphine using
hot-plate method
Anim 0
al # min.

10
min.

20
min.

30
min.

40
min.

50
min.

60
min.

1
2
3
4
5
6
Mea
n

March 5, 2007

454 PHL Lab II

Gamra Hamad

Graph
Unknown

Morphine

March 5, 2007

454 PHL Lab II

Gamra Hamad

Screening of Nonnarcotic Analgesics


MOA:
Inhibition of COX
Non-narcotic:
1- Electrical method
2- Chemical ( Writhing method)

March 5, 2007

454 PHL Lab II

Gamra Hamad

Writhing Method
Principle:
The painful stimulus is induced by IP
injection of an irritant substance
(e.g. acetic acid)
Writhing:
Stretching of the body, withdrawing of
the limb, retraction of the abdomen
& the stomach touches the ground
March 5, 2007

454 PHL Lab II

Gamra Hamad

Writhing method
Material
Animal: Mouse
Painful stimulus: Chemicals e.g. acetic
acid
Drug used: NSAID e.g. Na salicylate

March 5, 2007

454 PHL Lab II

Gamra Hamad

Drug

Onset of writhing

No. of writhing

Acetic acid (control)

Na salicylate
(100mg/kg)

Na salicylate
(200mg/kg)

March 5, 2007

454 PHL Lab II

Gamra Hamad

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