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 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
Narcotic analgesic
(opioids)
Non-narcotic
analgesic (NSAID)
 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
Antagonist
Mixed agonist+ antagonist
Agonist
On the basis of receptors
Natural
Semi synthetic
Synthetic
Penantherine
group
Morphine
codeine
Benzyl iso
qunoline group
papaverine
noscopine
Morphine
derivative
Hydro morphine
dihydromorphine
(heroine)
Oxy morphine
Codeine
derivative
hydrocodine
oxycodine
• Mepridine, Pithidine,
• Fentanyle, alfentanyle sufantanyle,
Remifentanyle, tramadol
Phenylpepradine
• Propoxyphone
• Metadone
Phenyle
hepthamine
• Levorpphinole
• Butorpinl
• Dextrometherphsn
Morphinine
Nulbupin
Pentazocine
Nalaropine
Phenazocine
Buprinorphine
Nalaxone
Naltraxone
(long acting)
Nalmefin
Opioids receptor belong to glycoprotein
coupled family with seven transmembrane
extracellular N-terminal and intracellular
C-terminal
Receptor Place where present Response to
stimulation
μ (MPO) Receptor
OP3
Peripheral
inflammation pre and
post synaptic neuron of
spinal cord
pre aqueduct gray
matter
limbic system
caudate putamen
thalamus
cerebral cortex
Analgesia
Sedation
Euphoria
Respiratory
depression
Constipation
RECEPTORS PLACE WHERE
PRESENT
RESPONSE TO
STIMULATION
k receptor (KOP)
OP1
KAPA
MID brain
Hypothalamus
Spinal cord
Nucleus raphe
Magnus
Spinal analgesia
Sedation
Miosis
δ(delta) receptor (DOP)
OP2
NOP FQ receptor
Nociceptive orphanin
OLFACTORY CENTERS
CEREBRAL CORTEX
CAUDATE PUTAMEN
SPINAL CORD
Nucleus raphe
Magnus
Spinal cord
Afferent neuron
Cardiac stimulation
Analgesia
Dysphoria
 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.
 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
 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
 Lipid soluble distribution depend upon
Lipid solubility
Concentration gradient
Binding to glycoprotein
 Only a small amount enter in to the brain
 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
Analgesic
Sedation
Euphoria
Dysphoria
Miosis
Respiratory
depression
Anti tussive
 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)
 Produce spasm of GIT muscle
 Reduce peristalsis causing constipation
 Decrease the secretion of stomach
 Decrease the motility of sphincters and
produce contraction of sphinctors
 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
 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
 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
 Decrease thyroid hormones
 Decrease BMR
 Decrease the level of LH, FSH, Testosterone
and cortisol
 Increase ADH
Long Bone Fracture
Myocardial Infarction
Terminal stages of cancer
Burn patients
Postoperative patients
Visceral pains
Biliary colic and renal colic
Intraoperative & premedication
TIVA
Bronchial asthma
Respiratory insufficiency
Head Injury
Shock – Hypotension
Infant ,pregnancy ,obstructed labour
Meningitis
Hepatic and renal failure
 Drug tolerance means reduced response to
a drug following its repeated use. Increasing its
dosage may re-amplify the drug's effect
 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
Muscle aches
Restlessness
Anxiety
Lacrimation
Runny nose
Excessive sweating
Inability to sleep
Diarrhea
Confused
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

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ANALGASIC slides for all medical students

  • 1.
  • 2.  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
  • 3.  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
  • 4.  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
  • 5.  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
  • 7.  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
  • 12. • Mepridine, Pithidine, • Fentanyle, alfentanyle sufantanyle, Remifentanyle, tramadol Phenylpepradine • Propoxyphone • Metadone Phenyle hepthamine • Levorpphinole • Butorpinl • Dextrometherphsn Morphinine
  • 15. Opioids receptor belong to glycoprotein coupled family with seven transmembrane extracellular N-terminal and intracellular C-terminal
  • 16. Receptor Place where present Response to stimulation μ (MPO) Receptor OP3 Peripheral inflammation pre and post synaptic neuron of spinal cord pre aqueduct gray matter limbic system caudate putamen thalamus cerebral cortex Analgesia Sedation Euphoria Respiratory depression Constipation
  • 17. RECEPTORS PLACE WHERE PRESENT RESPONSE TO STIMULATION k receptor (KOP) OP1 KAPA MID brain Hypothalamus Spinal cord Nucleus raphe Magnus Spinal analgesia Sedation Miosis δ(delta) receptor (DOP) OP2 NOP FQ receptor Nociceptive orphanin OLFACTORY CENTERS CEREBRAL CORTEX CAUDATE PUTAMEN SPINAL CORD Nucleus raphe Magnus Spinal cord Afferent neuron Cardiac stimulation Analgesia Dysphoria
  • 18.  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.
  • 19.  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
  • 20.
  • 21.
  • 22.  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
  • 23.  Lipid soluble distribution depend upon Lipid solubility Concentration gradient Binding to glycoprotein  Only a small amount enter in to the brain
  • 24.  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
  • 26.  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)
  • 27.  Produce spasm of GIT muscle  Reduce peristalsis causing constipation  Decrease the secretion of stomach  Decrease the motility of sphincters and produce contraction of sphinctors
  • 28.  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
  • 29.  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
  • 30.  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
  • 31.  Decrease thyroid hormones  Decrease BMR  Decrease the level of LH, FSH, Testosterone and cortisol  Increase ADH
  • 32. Long Bone Fracture Myocardial Infarction Terminal stages of cancer Burn patients Postoperative patients Visceral pains Biliary colic and renal colic Intraoperative & premedication TIVA
  • 33. Bronchial asthma Respiratory insufficiency Head Injury Shock – Hypotension Infant ,pregnancy ,obstructed labour Meningitis Hepatic and renal failure
  • 34.  Drug tolerance means reduced response to a drug following its repeated use. Increasing its dosage may re-amplify the drug's effect
  • 35.  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
  • 36. Muscle aches Restlessness Anxiety Lacrimation Runny nose Excessive sweating Inability to sleep Diarrhea Confused
  • 37. 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