Presented by:

Dr. Sugandha Sharma

1
st
year PG
Essentials of Medical Pharmacology
- K.D.Tripathi (5
th
Ed.)
Pharmacology and therapeutics for dentistry
- Neidle and Yagiela (3
rd
Ed.)
Pharmacotherapeutics in Dentistry
-Gangarosa, Ciarlone, Jeske
Pharmacology
- Dale,Rang and Ritter (4
th
Ed.)
Basic & Clinical Pharmacology
- Bertran And Katzung

Pain
Analgesics-Definition
Classification

Routes of administration
Opioids-Classification
Opioid receptors
Mechanism of action
Morphine-Actions
Morphine analgesia
Pharmacological actions
Pharmacokinetics
Adverse effects
Therapeutic uses
Contraindications




Codeine
Fentanyl
Tramadol
Pethidine
Methadone
Pentazocine
Naloxone
Strategies To Minimize Side Effects
Uses in dentistry
Conclusion


An unpleasant sensory & emotional experience
associated with actual or potential tissue
damage, or described in terms of such
damage
IASP

Types of pain:
A. Nociceptive (Tissue) Pain
B. Neuropathic (Nerve) Pain




Definition:
Analgesic is a drug that selectively relieves pain by acting in
the CNS or on peripheral pain mechanisms, without
significantly altering consciousness.

Classification
A. Opioid/Narcotic/Morphine like analgesics

B. Non opioid/Non narcotic/Nonsteroidal anti-
inflammatory drugs.
Oral
Intramuscular Inj.
Intravenous Inj.
PCA: patient controlled
analgesia
Epidural Administration
Transdermal, Creams,
gels and foam

Opium
Classification of Narcotic-Analgesics
1. Natural Opium Alkaloids
-Morphine
-Codeine
-Papaverine
2. Semisynthetic Opiates
-Heroin
-Pholcodeine
-Oxycodone
3. Synthetic Opioids
- Meperidine
- Fentanyl
- Methadone
- Dextropropoxyphene
- Tramadol
Mu

Kappa

Delta

Analgesia Analgesia Analgesia
Respiratory depression

Respiratory depression

Respiratory depression

Sedation

Sedation

Affected behavior
Euphoria

Dysphoria,
hallucination

Reinforced action
miosis

miosis

-
Reduced gi motility

Reduced gi motility

Physical dependence
(morphine type)
Physical
dependence(nalorphine
type)

-

CNS

Depressant effects:

(a) Analgesia
Strong analgesic
Relief of dull, poorly localized visceral pain
Nociceptive pain relieved better than neuretic pain
Suppression of pain perception is selective.

(b) Sedation

(c) Mood and Subjective effects

(d) Respiratory centre

(e) Cough centre

(f) Temperature regulating centre

(g) Vasomotor centre
Stimulant effects:

(a) CTZ

(b) Edinger Westphal Nucleus

(c) Vagal centre
CVS
Causes Vasodilatation due to
- Decreasing tone of blood vessels
- Histamine release

GIT
- Constipation.

NEUROENDOCRINE EFFECTS
- Hypothalmic influence on pituitary is reduced.
- Decreases levels of LH, FSH, ACTH whereas
PROLACTIN & GH levels are increased.



Smooth muscles
- Biliary tract

- Urinary bladder

- Bronchi
Oral absorption-Unreliable
(High First pass Metabolism).
Primarily metabolised in liver.
Freely crosses the placenta &
can effect the foetus.

1) Side Effects:
Sedation, mental clouding, lethargy
Vomiting
Constipation
Respiratory depression
Blurring of vision
Urinary retention

2) Idiosyncrasy & allergy


3) Apnoea
- This may occur in new born when morphine is given to
mother during labour.
-Treatment of choice Naloxone 10 ug /kg injected in the chord.



4)Acute morphine poisoning
It is accidental ,suicidal or seen in drug abusers
Symptoms
Shallow & occasional breathing ,cyanosis ,pinpoint pupil ,fall
in BP & shock .
Treatment
Respiratory support and maintenance of BP
Specific antidote Naloxone 0.4-0.8mg i.v

5) Tolerance & dependence
High degree of tolerance if used repeatedly .
Withdrawal symptoms
Lacrimation ,sweating ,anxiety ,fear ,restlessness, tremor ,insomnia,
abdominal colic, diarrhoea.
Treatment Withdrawal of morphine &
substitution with methadone

As analgesic
Preanaesthetic medications
Relief of anxiety & apprehension
Acute left ventricular failure
Diarrhoea
Cough

DOSE: 10-15 mg i.m/ s.c
MORPHINE SULPHATE 10, 15 mg inj.

Bronchial Asthma
Infants & Elderly
Head Injury
Undiagnosed Acute
Abdominal pain.
Respiratory diseases
(Emphysema, COPD)

One tenth the potency
(analgesic) of morphine.
More selective COUGH
SUPPRESSANT.
Good activity by Oral Route.
Abuse Liability is low.

AVAILABLE : COREX ,
COMTUS syp. (10 mg / 5 ml)

Equal analgesic efficacy to morphine

UNLIKE MORPHINE:
- Less histamine release
(Safer in ASTHMATICS)
- Less constipation

Used primarily as an analgesic (substitute of morphine)
DOSE : 50-100 mg i.m, s.c/ orally
(PETHIDINE HCL) 100mg/ 2ml inj.;50-100mg Tab.)

80 to 100 times more potent than
morphine

Rapidly Onset of action (5 min)

Used for anesthesia and analgesia


Durogesic
Transdermal patch (25-75g/hr)

Transdermal fentanyl
(Durogesic)
Fentanyl lozenges
(Actiq)
Centrally Acting Analgesic.
Has dual Norepinephrine & Serotonin reuptake inhibitory
effects .
10 times potent than morphine & produces less adverse
effects.
Used in mild to medium intensity short
lasting pain.
DOSE: 50-100 mg oral/ i.v. 4-6 hrly
(CONTRAMAL, DOMADOL)

Pharmacological activity &
potency same as morphine.
Long duration of activity( PPB >90%).
Powerful pain reliever.
Used as SUBSTITUTION Therapy of opioid
dependence.

DOSE: 10 mg inj. PHYSEPTONE

Mixed opioid agonist-antagonist action.
Efficacy lower than morphine.
Useful in Mild-Moderate pain conditions.
Causes Tachycardia & rise in BP.
Should not be used in opioid dependent subjects.

DOSE: 50-100 mg oral , 30-60 mg i.m /s.c
(FORTWIN, FORTSTAR)
No analgesic activity at all.
Competitive antagonist at opioid
receptor & reverses all actions of morphine.
Drug of choice for Morphine Poisoning.
Diagnosis of opioid dependence -it will precipitate
withdrawal reactions.

DOSE: 0.4 mg in 1 ml (NARCOTAN)


Slow titration of doses.
Changing the dosing regimen or route of
administration.
Using a Nonopioid or Adjuvant Analgesic for an
opioid sparing effect.
Adding a drug to counteract the side effect.
Constipation prophylaxis.

Preanaesthetic medication

Postoperative pain

Fracture pain

Carcinoma

Although opioids as a class are effective pain relievers, some
commonly used formulas show poor efficacy for dental pain.

Other drugs with fewer severe side effects can have similar results.

Opioids are particularly useful when additional relief of pain is
required.

Their effectiveness in combination therapy (combining opiods with
acetaminophen and NSAIDs) is better than that in monotherapy.