ANALGESIC

ANALGESIC
 All those drugs which are used to reduce pain
sensation are called analgesic

Pain
 Pain is unpleasant sensation OR emotional
behavior to the body due to actual or
potential tissue damage
 Nociception is the mechanism whereby noxious
peripheral stimuli are transmitted to the central
nervous system.
 Analgesia – absence of pain
 Pain receptors in our bodies are nerves that
transmit pain. These are located in various body
tissues that respond to thermal, mechanical and
chemical stimuli. When stimulated, these pain
receptors generate an impulse which is carried to
the CNS. Called nociceptors
 Nociceptive pain: it results from activation of
nociceptors (Pain receptors)
 Neuropathic pain: it results from direct injury to
nerves in the peripheral nervous system.
 Somatic pain
Superficial: stimulation of receptors in skin
Deep: stimulation of receptors in muscles, joints and
tendons
 Visceral pain
Stimulation of receptors in internal organs, abdomen
and skeleton
 Referred Pain: Pain experienced at a point distant to its
point of origin
 Somatogenic pain is a pain originating from an actual
physical cause e.g. trauma, ischaemia etc
 Psychogenic pain is pain for which there is no
physical cause
 CLASSIFICATION OF ANALGESIC

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NARCOTICS ANALGESIC OPIOIDS
 The term opioids refers to all those drugs
(natural or synthetic) which acts on opioids
receptors produce analgesia and narcosis
(drowsiness)
 Opioids derived from poppy (opium)
papaver somniferous
CLASSIFICATION OF OPIOIDS
AGONIST

Natural

Semi synthetic

Synthetic
NATURAL

Penantherine group Morphine Benzyl iso qunoline group

codeine papaverine noscopine
SEMI SYNTHETIC

Hydro
morphine
Morphine dihydromorph
derivative ine (heroine)
Oxy morphine

Codeine hydrocodine
derivative oxycodine
SYNTHETIC
Phenylpe •Mepridine, Pithidine,
•Fentanyle, alfentanyle sufantanyle,
pradine Remifentanyle, tramadol

Phenyle •Propoxyphone
hepthamine •Metadone

Morphini •Levorpphinole
•Butorpinl
ne •Dextrometherphsn
MIXED AGONIST ANTAGONIST
Nulbupin

Buprinorphi Pentazoci
ne ne

Phenazoci Nalaropin
ne e
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OPIOIDS RECEPTOR
Opioids receptor belong to glycoprotein
coupled family with seven transmembrane
extracellular N-terminal and intracellular
C-terminal
OPIOIDS RECEPTOR
Receptor Place where present Response to
stimulation

μ (MPO) Receptor Peripheral Analgesia

OP3 inflammation pre and Sedation
post synaptic neuron of Euphoria
spinal cord
pre aqueduct gray Respiratory
matter depression
limbic system
caudate putamen Constipation
thalamus
cerebral cortex
RECEPTORS
RECEPTORS PLACE WHERE RESPONSE TO
PRESENT STIMULATION
k receptor (KOP) MID brain Spinal analgesia
OP1 Hypothalamus Sedation
KAPA Spinal cord Miosis
Nucleus raphe
Magnus
δ(delta) receptor (DOP) OLFACTORY CENTERS Cardiac stimulation
OP2 CEREBRAL CORTEX Analgesia
CAUDATE PUTAMEN Dysphoria
SPINAL CORD
NOP FQ receptor Nucleus raphe
Nociceptive orphanin Magnus
Spinal cord
Afferent neuron
MECHANISM OF ACTION
 Natural Painkillers OR opiopeptides
 Endorphins and Enkephalins are the natural
opiates found in the part of the brain and the
spinal cord. They are able to bind to neuro-
receptors in the brain and produce relief from
pain. The temporary loss of pain immediately
after an injury is associated with the production
of these chemicals.
MECHANISM OF ACTION
 Acts on specific opioids receptor
 Exogenous opioids mimic the action of
endogenous opioids
 Block the adenylete cyclase which further
inhabit the neurotransmitter (substance P
and glutamate) from the neural cell which
caring painful stimulus
PHARMACOKINETICS
 Absorption
 All opioids are week base and highly ionized
state
 Rapid absorption from GIT
 Many opioids undergoes first pass effect
 Parentally 100% bioavailability IM, IV,
sublingual, subcutaneous, nasal mucosa,
 Highly lipid soluble absorbed from skin e.g.
alfentanyle pitch
DISTRIBUTION
 Lipid soluble distribution depend upon
Lipid solubility
Concentration gradient
Binding to glycoprotein

 Only a small amount enter in to the brain

METABOLISM
 Metabolism take place in the liver by phase I
and Phase II reaction converted to
glucoronides and water solvable metabolites

 Excretion
 Execrate through kidney in urine
 Bile excretion
ACTION ON CNS
Analgesic

Sedation

Euphoria

Dysphoria

Miosis

Respiratory depression

Anti tussive
CONTI…… CNS EFFECT
 Lead to cerebral vasodilatation increase
blood flow to brain which increase ICP
(THIS EFFECT ALSO DUE CO2)
REPIRATORY DEPRESSION
 Activate chemoreceptor trigger zone
produce nausea and vomiting
 Stimulation of endanger westphal nucleus
produce Miosis (Occulumoter nerve III
CN)
ACTION ON GIT
 Produce spasm of GIT muscle
 Reduce peristalsis causing constipation
 Decrease the secretion of stomach
 Decrease the motility of sphincters and
produce contraction of sphinctors
ACTION ON CVS

 In Normo volumic patient have no effect

 Orthostatic hypotension
 Depress the vasomotor center which depress
the vasomotor tone lead to vasodilatation it
is also due to histamine release produce
hypotension
ACTION ON RESPIRATORY
SYSTEM
 Produce constriction of bronchial smooth
muscle
 Decrease secretion of bronchioles
 Decrease respiratory rate due to central
depression
 Increased the rigidity of trunk muscle
(alfentanyle) child and old are more effected
 Decrease sensitivity of respiratory center to
CO2
GENATOURINARY SYSTEM
 Decrease blood flow to the kidney which
increase the secretion of ADH which lead to
Oliguria
 Produce spasm of urinary system retention of
urine
 Causes relaxation of uterus delay labour
 Decrease sexual activity in mail
 Libido in addict patient
 Delayed ejaculation
ACTION ON ENDOCRINE
 Decrease thyroid hormones
 Decrease BMR
 Decrease the level of LH, FSH, Testosterone
and cortisol
 Increase ADH
INDICATION
Long Bone Fracture

Myocardial Infarction

Terminal stages of cancer

Burn patients

Postoperative patients

Visceral pains

Biliary colic and renal colic

Intraoperative & premedication

TIVA
CONTRAINDICATION
Bronchial asthma

Respiratory insufficiency

Head Injury

Shock – Hypotension

Infant ,pregnancy ,obstructed labour

Meningitis

Hepatic and renal failure

DRUG TOLERANCE
 Drug tolerance means reduced response to
a drug following its repeated use. Increasing its
dosage may re-amplify the drug's effect
DEPENDENCY AND ABUSE
 Dependence develops when the neurons adapt to
the repeated drug exposure and only function
normally in the presence of the drug. When the
drug is withdrawn, several physiologic reactions
occur. Morphine act on specific areas of the
brain known as the limbic system, which controls
emotions, to create feelings of pleasure or
relaxation. Opiates work to reduce pain by
affecting the spinal cord, which sends messages
from the brain to the rest of the body, and vice
versa
WITHDRAWAL EFFECT
Muscle aches
Restlessness
Anxiety
Lacrimation
Runny nose
Excessive sweating
Inability to sleep
Diarrhea
Confused
SIDE EFFECT
M…MIOSIS

O..ORTHSTATIC HYPOTENSION

R… RESPIRATORY DEPRESSION

P..PHYSICAL DEPENDECE

H.. HISTAMINE REALESE FLUSING OF SKIN

I.. INCREASE ICP

N…NAUSEA AND VOMATING

E… EUPHORIA

S…SEDATION
THANK YOU