START WITH THE NAME OF

ALLAH
THE MOST BENEFICIENT,
THE MOST MERCIFUL
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 Analgesics

Drugs used for alleviation of pain

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 Pain
A signal for the injury or insult of an area

A protective and diagnostic method

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 Types of pain
 Pricking, burning, itching pain
 Dull or sharp
 Superficial
 Visceral pain

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 Mechanism of pain
 Painful stimuli
 Pain neurotransmittors
 Prostaglandins, substance P
 Pain receptors
 Pain perceiving neurons
 Inhibitory neurotransmittors
 Endorphins
 Receptors for Endorphins and Opiate narcotics
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 Therapeutic approach for analgesic
1. General anesthetics  animal unconscious,
sensory block
 Total inhibition of lower and higher areas of brain by producing
anesthesia
2. Analgesic drugs
 Increasing the thresh hold of pain in the centrally pain perceiving
areas of brain
a) Opioid Narcotics
Morphine Nulbuphine
Codeine Pentazocine
Pethadine Oxymorphone
Fentanyl Mepridine
Butyrophenol
Sufentanil
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 b) Antiprostaglandins
Drugs which block the synthesis of
prostaglandins thus pain neurotransmitters not
released and pain perception is reduced
Salicylates Paracetamol
Meclofenamic acid Phenylbutazone
Flunixin meglumine Naproxen
c) α2 – agonists
Xylazine, Detomidine,
Medetomadine, Clonidine

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3. Anti-inflammatory drugs
• These may reduce inflammation and swelling at
peripheral site and stop the penetration of
painful stimuli
a) Steroids  Prednisolone, Dexamethasone,
Flumethazone, Betamethazone
b) Non-steroids  Aspirin, Phenylbutazone,
Indomethacin, DMSO,
Meclofenamic acids, Naproxin

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4. Anti-spasmodic drugs:
 Reduce the painful stimuli from spasms of smooth
muscles
a) G.I.T.
Opium alkaloids
Antiprostaglandins
Antihistamines
Relaxants
b) Uterus
Relaxants
Antiprostaglandins
5. Muscle relaxants
 Reduce the painful stimuli from skeletal muscle spasms
with muscle relaxants that act on spinal cord.
Guaifenesin
Valium
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6. Local Anaesthetics
 May use local anaesthetics to block the
generation and or conduction of painful
stimuli
These may be applied locally or by
infiltration
Procaine
Lidocaine
Hexylcaine

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 Measurement of analgesic properties
1. Thermal method
Hotplate 55oC, mice lick feet after 12
seconds
2. Electrical method
Metal pulp of teeth, electric stimulation
3. Mechanical method
Pricking of tail
4. Chemical method
Acetic acid
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 Analgesic Drugs
1. Narcotic Analgesics
(Have addiction property)
a) Opioids
b) Opiates
2. Non-Narcotic Analgesics
(Non addictive)
a) Antiprostaglandins
b) Sedative – analgesics (α2 agonists)
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 NARCOTIC ANALGESICS

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 Opioids
 Opioids:
The drugs which bind to the opioid receptors. It
may be synthetic, semisynthetic or naturally
occuring.
Naturally occuring Opioids:
Endorphins, Enkephlins, Dynorphins
Opioid Receptors:
Mu (μ), Kappa, Delta
 Opiates:
The drugs which are derived from poppy plant
(Opium)
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 Narcotics:
Used for opioid analgesics
They induce sleep, analgesia and dependency
Receptors:
Opioid receptors are naturally occuring sites in
the body which respond to endogenous opiate –
like substances (enkephlins, dymorphins,
endorphins)
Site:
Present in various tissues such as brain & spinal
cord, urinary tract, G.I.T, vas deference, etc.

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 Opioid receptors
Receptor type Physiological Role
Mu (μ)  μ1, μ2  Analgesia
 Sedation
 Cough depression
 Respiratory depression
 Cardiovascular depression
 Physical dependency
 Hypothermia
 Indifference

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 Delta (δ)  Probably analgesia
 Indifference

 Kappa (K)  Analgesia

K1, K2, K3  Sedation
 Ataxia

 Sigma (б)  Euphoria, dysphoria

 Hallucination
 Excitement
 Analgesia

 Epsilon (ε)  Analgesia

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 Mu Kappa Delta
Analgesia Yes Yes Yes

Euphoria Yes - -

Sedation Yes Mild -

Respiratory depression Yes - -

Miosis Yes Yes -

ADH release Increase Decrease -

G.I.T. Motility Decrease - -

Physical dependence Yes - -

Hypothermia Yes - -

Cardio-vascular Yes - -
depression
Subclass μ1,μ2 K1, K2, K3 D1

Location (Pain perceiving Spinal cord Brain & Spinal Limbic system
cord of brain
area)
 Addictive analgesic drugs
(Narcotic Analgesics)
1. Natural opium alkaloids
- Morphine
- Codeine
2. Synthetic derivatives of opiates
- Dihydromorphinone
- Diacetylmorphine (Heroin)
- Methyldihydromorphinone
- Oxymorphinone
- Hydrocodone

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3. Synthetic opiate like drugs
- Piminodine
- Mepridine (Pethadine)
- Anileridine
- Diphenoxylate (with asprin as lomotil)
- Methadone
- Lavophanol
- Phenazocine
- Alphaprodine
- Bupremorphine
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4. Synthetic opiate like drugs of low
addiction (Potency)
- Propoxyphene
- Ethoheptazine
- Pentazocin (Talwin, Sosegon)
- Pentazocaine
5. Narcotic antagonist
- Nalorphine
- Levollerphane
- Naloxone
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 Morphine
Prototype drug
PHARMACOLOGICAL EFFECTS
1. Analgesic and other CNS effects
- Depression: Pain, respiration, cough
- In some species, excitement e.g. cat,
horses, etc.
- Analgesia without making unconscious
- Atropine, scopolamine may reduce its
analgesic effects, so not given together
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2. Emesis
- Dogs vomit in 10 minutes after S/C injection
- Effect on CTZ
3. Effects on respiratory center
- Depression
4. Pupil
- Miosis when depression
- Dilation if excitement
5. G.I.T
- Reflex defecation
- Severe constipation also
- Depress normal defecation reflexes
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 Clinical Uses
 Not used in cats
 Less in horses and cattle
Three main uses
1) Pre-anaesthetic medication
- Smooth induction
- Analgesia
- Reduce the dose of anaesthetic
- Problems of vomation, salivation,
constipation, respiratory depression
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2) Intestinal sedation
- Chlorodyne mixture
(morphine + chloroform)
- Used with Kaolin, Catechu, chalk,
ginger
- Also used in spasmodic colic
3) Cough sedatives
- In dry cough – non productive
- Codeine superior than morphine

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 Relative opioids potencies
Drug Analgesic Potency Histamine release

Meperidine 0.1 – 0.2 Yes

Pentazocine 0.25 – 0.5
Nalbuphine 0.5 – 1.0
Morphine 1 Yes
Butorphanol 4–7
Oxymorphone 10
Alfentanil 7.5 – 25
Buprenorphine 30
Fentanyl 75 – 125
Sufentanil 375 – 1250
Etorphine 1000 – 10,000
Carfentanil 10,000
 Effects of Opioids on receptors
Opioids Receptors
Analgesic
Mu Kappa Delta Potency

Morphine Ag Ag Ag 1
Fentanyl Ag Ag ? 75 – 125
Oxymorphone Ag Ag ? 10
Etorphine Ag Ag ? 1000-10,000

Carfentanil Ag Ag ? 10,000
Meperidine Ag Ag ? 0.1 – 0.2
Pentazocine Antag Ag Ag 0.25 – 0.5
Butorphanol Antag Ag ? 4–7
 Nalbuphine Antag Ag ? 0.5 – 1.0
Nalorphine Antag P . Ag ?
Buprenorphine P. Ag Antag ? 30
Enkephalinst* O O Ag
Endorphinst* Ag Ag Ag
Dynorphinst* O Ag O
Naloxone Antag Antag Antag
Naltrexone Antag Antag Antag

Ag: Agonist Antag: Antagonist P.Ag: Partial agonist

O: No effect ? : Unknown effect * : Endogenous Opoids

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