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anesthetics agents
Objective
Introduction
Local anesthetic
General anesthetic
Introduction
 Drugs that temporarily blocks sensory/pain signals from nerves
to the centers in the brain
 We have different types of anesthetics according to type of
surgical intervention
o Local anesthetics
o Sedation anesthetics
o General anesthetics
Local Anesthetic
 In local anesthetics we block the sensations of a small section of the
body
 Commonly used include lidocaine , bupivacaine ropivacaine,procaine
 Mechanism of action reversibly inhibit nerve transmission by binding
voltage-gated sodium channels in the nerve plasma membrane which
prevents action potential initiation and propagation
 Clinical application during lumbar puncture , spinal anesthesia , cataract
surgery & root canal
Local anesthetic side
effects
 Local anesthetic can readily cross the blood brain barrier
and lead to Generalized CNS depression leading to
respiratory depression and arrest
Local anesthetic can also cause cardiac toxicity
1. hypotension
2. Dysrthmias
3. myocardial depression
4. Decreased contractility
General Anesthetics
 General Anesthetics is a medically induced coma with loss of protective
reflexes
 General Anesthetics are usually administered via intravenously or as
inhalation anesthetic
 Performed in patients undergoing surgical manipulation procedures that
require deep relaxation for longer periods of time
 Used in major surgery like heart surgery , knee or hip replacement
surgery
 Examples include isoflurane , desflurane ,propofol etc
Classification of General
Anesthetics
Inhaled Gas
Anesthetics
 We have nitrous oxide also known as laughing gas which is a colourless gas
with sweet scent and taste
 Commonly administered in combination with opioid or volatile anesthetics
 Mechanism of action is they inhibit the NMDA receptor which causes a
dissociative anesthesia with catalepsy amnesia and analgesia
 Common side effects include nausea ,vomiting , fatigue & dizziness serious
side effects is they inactivate vitamin b12 and lead vitamin deficiency and they
are not given to patient with vitamin b12 deficiency
Volatile liquids
Anesthetics
 Halothane , isoflurane , desflurane & sevoflurane , the most potent of all is
isoflurane and does not undergo any deterioration during storage due to
its great physical stability
 Mechanism of action is they act as an positive allosteric modulator of
GABA receptors , potentiate glycine receptors & inhibit NMDA receptors
 Side effects include shivering , nausea , vomiting serious side effects
include hepatic toxicity due to fact of formation reactive species
trifluoroacetylated reactive intermediate(TFA) in the case of halothane and
isoflurane while sevoflurane is much safer as it doesn’t produce TFA but a acyl
halide hexafluroisopropanol which doesn’t stimulate hepatitis antibodies
Barbiturates
Anesthetics
 Thiopental , Thiamylal & methohexital
 Barbiturates have two main classes oxybarbiturates & thiobarbiturates
 Barbiturates solution are highly alkaline which lead to the formation of water
solube salts
 Mechanism of Action is that they act as a GABAa receptor agoinst anf hence
produce cns depression they also reduce cerebral metabolic rate of oxygen
which inturn lead to decreased cerebral blood flow and decreased intracranial
pressure they also increase blood flow to ischemic part of the brain
 Side effect include caughing , sneezing , respiratory depression ,severe
hypotension cardiac arrhythmia and is contraindicated in patients with acute
intermittent porphyria as they increase porphyrin synthesis
Dissociative
Anesthetics
 Ketamine is an analog of phencyclidine which is also known as angel dust
 Mechanism of action is they binds preferentially to the NMDA receptors on
inhibitory interneurons in the cortex, limbic system, and hippocampus that
promote uncoordinated increase in neuronal activity and an active EEG
pattern, and produce unconsciousness
 Side effects include psychogenic reactions like hallucinations and out of
body experience they also cause tachycardia &hypertensio also cause
hypoxia & increased salvation leading to laryngospsm
Opiods Anesthetics
 Opiods are used in perioperative care treat acute postoperative pain
 Morphine , fentanyl , naloxone , heroin , remifentanyl
 Mechanism of action is they are Mu opiate receptor agonist and NMDA receptor
antagonist
 Clinical use anlagesia and sedation
 Side effects include vomiting , nausea , delayed gastric emptying, constipation, bowel
distension, paralytic ileus, sphincter of Oddi spasm, urinary retention, histamine
release, miosis, muscle rigidity, diffuse CNS effects dizziness, light headedness,
sedation, drowsiness, euphoria, dysphoria , cognitive dysfunction memory loss,
inability to concentrate or focus attention, hallucinations, and cardiovascular effects.
Propofol
 Most frequently used IV anesthetics and has rapid onset & rapid emergence
from anesthesia
 Propofol is primarily metabolised by the liver and excreted by the kidneys
 Mechanism of action is they are GABAa receptor agonist and they also reduce
cerebral metabolism of oxygen and inturn reduce cerebral blood flow and
cerebral intracranial pressure
 Side effects include pain on injection,serious side effect include PRIS which
contains unexplained metabolic acidosis, hyperkalemia, hyperlipidemia,
rhabdomyolysis, hepatomegaly, renal failure and most importantly ECG
changes, arrhythmias, and progression to cardiac failure
Etomidate
 Etomidate is imidazole derivative and is not stable in neutral ph
 First introduced as an induction agent
 Mechanism of action is they act as GABAa receptor agonist and lead
to inhibitory effect on the CNS
 Side effects include adrenal suppression by acting on the 11β-
hydroxylase and prevent the converson of cholesterol into cortisol ,
pain on injection , thrombophlebitis & myoclonus
Sources
 https://www.medscape.com/viewarticle/492432_2
 https://www.sciencedirect.com/topics/medicine-and/intravenous-
anesthetic-agent
 https://en.m.wikipedia.org/wiki/Inhalational_anesthetic
 Clinical anesthesias / edited by Paul. G Barash 8th edition
 https://my.clevelandclinic.org/health/treatments/15286-anesthesia
 https://www.sciencedirect.com/topics/medicine-and-dentistry/mu-opiate-
receptor-agonist
 https://www.uptodate.com/contents/perioperative-uses-of-intravenous-
opioids-in-adults-general-
considerations#:~:text=Intravenous%20(IV)%20opioids%20are%20commo
nly,in%20the%20immediate%20postoperative%20period.
anest ppt.pptx

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anest ppt.pptx

  • 3. Introduction  Drugs that temporarily blocks sensory/pain signals from nerves to the centers in the brain  We have different types of anesthetics according to type of surgical intervention o Local anesthetics o Sedation anesthetics o General anesthetics
  • 4. Local Anesthetic  In local anesthetics we block the sensations of a small section of the body  Commonly used include lidocaine , bupivacaine ropivacaine,procaine  Mechanism of action reversibly inhibit nerve transmission by binding voltage-gated sodium channels in the nerve plasma membrane which prevents action potential initiation and propagation  Clinical application during lumbar puncture , spinal anesthesia , cataract surgery & root canal
  • 5. Local anesthetic side effects  Local anesthetic can readily cross the blood brain barrier and lead to Generalized CNS depression leading to respiratory depression and arrest Local anesthetic can also cause cardiac toxicity 1. hypotension 2. Dysrthmias 3. myocardial depression 4. Decreased contractility
  • 6. General Anesthetics  General Anesthetics is a medically induced coma with loss of protective reflexes  General Anesthetics are usually administered via intravenously or as inhalation anesthetic  Performed in patients undergoing surgical manipulation procedures that require deep relaxation for longer periods of time  Used in major surgery like heart surgery , knee or hip replacement surgery  Examples include isoflurane , desflurane ,propofol etc
  • 8. Inhaled Gas Anesthetics  We have nitrous oxide also known as laughing gas which is a colourless gas with sweet scent and taste  Commonly administered in combination with opioid or volatile anesthetics  Mechanism of action is they inhibit the NMDA receptor which causes a dissociative anesthesia with catalepsy amnesia and analgesia  Common side effects include nausea ,vomiting , fatigue & dizziness serious side effects is they inactivate vitamin b12 and lead vitamin deficiency and they are not given to patient with vitamin b12 deficiency
  • 9. Volatile liquids Anesthetics  Halothane , isoflurane , desflurane & sevoflurane , the most potent of all is isoflurane and does not undergo any deterioration during storage due to its great physical stability  Mechanism of action is they act as an positive allosteric modulator of GABA receptors , potentiate glycine receptors & inhibit NMDA receptors  Side effects include shivering , nausea , vomiting serious side effects include hepatic toxicity due to fact of formation reactive species trifluoroacetylated reactive intermediate(TFA) in the case of halothane and isoflurane while sevoflurane is much safer as it doesn’t produce TFA but a acyl halide hexafluroisopropanol which doesn’t stimulate hepatitis antibodies
  • 10. Barbiturates Anesthetics  Thiopental , Thiamylal & methohexital  Barbiturates have two main classes oxybarbiturates & thiobarbiturates  Barbiturates solution are highly alkaline which lead to the formation of water solube salts  Mechanism of Action is that they act as a GABAa receptor agoinst anf hence produce cns depression they also reduce cerebral metabolic rate of oxygen which inturn lead to decreased cerebral blood flow and decreased intracranial pressure they also increase blood flow to ischemic part of the brain  Side effect include caughing , sneezing , respiratory depression ,severe hypotension cardiac arrhythmia and is contraindicated in patients with acute intermittent porphyria as they increase porphyrin synthesis
  • 11. Dissociative Anesthetics  Ketamine is an analog of phencyclidine which is also known as angel dust  Mechanism of action is they binds preferentially to the NMDA receptors on inhibitory interneurons in the cortex, limbic system, and hippocampus that promote uncoordinated increase in neuronal activity and an active EEG pattern, and produce unconsciousness  Side effects include psychogenic reactions like hallucinations and out of body experience they also cause tachycardia &hypertensio also cause hypoxia & increased salvation leading to laryngospsm
  • 12. Opiods Anesthetics  Opiods are used in perioperative care treat acute postoperative pain  Morphine , fentanyl , naloxone , heroin , remifentanyl  Mechanism of action is they are Mu opiate receptor agonist and NMDA receptor antagonist  Clinical use anlagesia and sedation  Side effects include vomiting , nausea , delayed gastric emptying, constipation, bowel distension, paralytic ileus, sphincter of Oddi spasm, urinary retention, histamine release, miosis, muscle rigidity, diffuse CNS effects dizziness, light headedness, sedation, drowsiness, euphoria, dysphoria , cognitive dysfunction memory loss, inability to concentrate or focus attention, hallucinations, and cardiovascular effects.
  • 13. Propofol  Most frequently used IV anesthetics and has rapid onset & rapid emergence from anesthesia  Propofol is primarily metabolised by the liver and excreted by the kidneys  Mechanism of action is they are GABAa receptor agonist and they also reduce cerebral metabolism of oxygen and inturn reduce cerebral blood flow and cerebral intracranial pressure  Side effects include pain on injection,serious side effect include PRIS which contains unexplained metabolic acidosis, hyperkalemia, hyperlipidemia, rhabdomyolysis, hepatomegaly, renal failure and most importantly ECG changes, arrhythmias, and progression to cardiac failure
  • 14. Etomidate  Etomidate is imidazole derivative and is not stable in neutral ph  First introduced as an induction agent  Mechanism of action is they act as GABAa receptor agonist and lead to inhibitory effect on the CNS  Side effects include adrenal suppression by acting on the 11β- hydroxylase and prevent the converson of cholesterol into cortisol , pain on injection , thrombophlebitis & myoclonus
  • 15. Sources  https://www.medscape.com/viewarticle/492432_2  https://www.sciencedirect.com/topics/medicine-and/intravenous- anesthetic-agent  https://en.m.wikipedia.org/wiki/Inhalational_anesthetic  Clinical anesthesias / edited by Paul. G Barash 8th edition  https://my.clevelandclinic.org/health/treatments/15286-anesthesia  https://www.sciencedirect.com/topics/medicine-and-dentistry/mu-opiate- receptor-agonist  https://www.uptodate.com/contents/perioperative-uses-of-intravenous- opioids-in-adults-general- considerations#:~:text=Intravenous%20(IV)%20opioids%20are%20commo nly,in%20the%20immediate%20postoperative%20period.