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INTRODUCTION TO
ANAESTHESIA DRUGS
BY DR ADEKUNBI O. OSHUNPIDAN
OUTLINE
• Brief history of Anaesthesia
• Definition of Anaesthesia
• Drugs Definition and classification
 Premedications
 Induction Agents
 Muscle Relaxants
 Reversal Agents
 Analgesics
 Local Anaethetics
• Conclusion
HISTORY
• WTG Morton on the 16th of October in 1846 performed the first
public demonstration of anaesthesia.
DEFINITION
•Anaesthesia is a branch of medicine
that deals with reversible loss of
consciousness and pain control.
PREMEDICATIONS
• Reduction of anxiety and pain
• Promotion of amnesia
• Reduction of secretions
• Reduction of volume and increase PH of gastric contents
• Reduction of postoperative nausea and vomiting
• Enhancing the hypnotic effects of general anaesthesia
• Reduction of vagal reflexes to intubation
• Prophylaxis against allergic reactions
A’S OF PREMEDICATION
GLYCOPYROLATE
• Anticholinergic used as premedicant
• Reduces salivary and sweat gland activity therefore used as
antisialogogue
• Used with acetylcholinesterase inhibitors to prevent muscarinic
effects
ATROPINE
• Used for premedication
• Used to reduce muscarinic effects of acetylcholinesterase
• Used for treatment of bradycardia and asystole
• It should be avoided in pyrexial patients
TYPES OF ANAESTHESIA
• General
• Regional – Neuraxial : Subarachnoid Block
Epidural Anaesthesia
Nerve Block
• Local Anaesthesia
TRIAD OF GENERAL ANAESTHESIA
INTRAVENOUS ANAESTHETICS
• These are drugs expected to cause loss of consciousness in “one arm brain circulation”
• Characteristics of Ideal Intravenous Anaesthetics
 Simple preparation
 Painless on administration
 High potency and efficacy
 Rapid and predictable offset of effect
 Absence of toxic effects or adverse properties
 Compactible with other agents and IV fluids
 Depression of airway reflexes for intubation
 Rapid metabolism and minimal hangover
CLASSES OF INTRAVENOUS AGENTS
• BARBITURATES : Thiopental, Methohexital
• PHENOLS : Propofol
• IMIDAZOLES : Etomidate
• PHENYLCYCLIDINES : Ketamine
• BENZODIAZEPINES : Midazolam, Lorazepam, Diazepam.
• OPIODS : Morphine, Fentanyl
THIOPENTONE
• This is an ultra-short acting barbiturate with a rapid onset
• Used for induction of anaesthesia and the preferred drug of use in
Neuroanesthesia because it reduces cerebral blood flow and
intracranial pressure.
• Potent anaesthetic, weak analgesic effect with little muscle relaxation
• Usually comes in 5 or10% solution and has to be constituted to 2.5%
before use.
• Causes laryngospasm and not ideal for asthmatics
• Causes respiratory and circulatory depression
PROPOFOL
• Usually comes as a white emulsion of 1 or 2%
• Good for induction and maintenance of anaesthesia with a
short duration of action, safe for use in day-case surgery.
• It causes pain on injection
• Causes more respiratory and cardiovascular depression than
barbiturates
• Has anti –emetic properties
KETAMINE
• Causes ‘dissociative’ anaesthesia, has a slow onset
• Causes amnesia without loss of consciousness
• Has analgesic properties
• Causes cardiovascular stimulation therefore it is Useful for
patients with Hypotension but no respiratory depression
INHALATIONAL ANAESTHETICS
• Vapors used for induction and maintenance of anaesthesia.
They are delivered to the respiratory system to produce
anaesthesia.
PHYSICAL PROPERTIES OF AN IDEAL
INHALATIONAL ANAESTHETIC AGENT
1. Non-flammable, non-explosive at room temperature
2. Stable in light.
3. Liquid and vaporisable at room temperature i.e. low latent heat of vaporisation.
4. Stable at room temperature, with a long shelf life
5. Stable with soda lime, as well as plastics and metals
6. Environmentally friendly - no ozone depletion
7. Cheap and easy to manufacture
BIOLOGICAL PROPERTIES OF AN IDEAL
INHALATIONAL ANAESTHETIC AGENT
1. Pleasant to inhale, non-irritant, induces bronchodilatation
2. Low blood: gas solubility - i.e. fast onset
3. High oil: water solubility - i.e. high potency
4. Minimal effects on other systems - e.g. cardiovascular, respiratory,
hepatic, renal or endocrine
5. No biotransformation - should be excreted ideally via the lungs, unchanged
6. Non-toxic to operating theatre personnel
NITROUS OXIDE
• Colourless, odourless gas at room temperature
• Stored in blue cylinders
• Causes rapid induction of anaesthesia and rapid emergence.
• it has weak anesthetic and powerful analgesic effects
• Used as an adjunct to supplement other inhalationals
• Risk of bone-marrow suppression with prolonged
administration.
HALOTHANE
• Volatile liquid at room temperature
• Light sensitive
• High fat solubility
• Excreted unchanged through the lungs
• Stored in amber colored bottles with thymols as the
preservative
• Causes reduced myocardial contractility and cause hypotension
ISOFLURANE
• Has a pungent smell therefore not ideal for induction of
anaesthesia
• Causes a progressive respiratory depression and hypotension.
• Useful for cardiac anaesthesia
SEVOFLURANE
• It has a pleasant smell, non-irritant and good for use in
paediatrics, cardiac and neuroanaesthesia.
• Produces a fast induction and emergence.
• Fairly expensive therefore not readily used in our environment
MUSCLE RELAXANTS
• Divided into two
Depolarising – Suxamethonium
Non – Depolarising : Divided into 2
1. Aminosteriods – Rocuronium,
Vecuronium, Pancuronium
2. Benzylisoquinoloniums – Atracurium,
Cisatracurium,
Mivacurium.
SUXAMETHONIUM
• The depolarising neuromuscular blocker of choice
• It is widely used due to rapid onset and short duration of action
• Ideal for Rapid Sequence Induction
• The depolarising effect causes fasciculation and flaccid
paralysis
• Paralysis occurs one minute after administration and lasts 7 –
12minutes
• Metabolised by plasma pseudocholinesterase
ATRACURIUM
• An intermediate acting muscle relaxant with onset of 60 -90
seconds
• Effect lasts 20 – 30 minutes
• Causes histamine release
• The drug of choice in renal and hepatic impairment
PANCURONIUM
• Can be used to aid tracheal intubation after 2 – 3 minutes
• The effect lasts 40 – 60 minutes
• May increase heart rate, BP and cardiac output by vagolytic and
sympathomimetic actions.
• Elimination is delayed in renal and hepatic impairment
therefore avoided in them.
VECURONIUM
• Provides intubating condition in 90seconds
• Relaxation is 20 – 30 minutes but can last up to 80minutes with
a dose 250mcg/kg
• Has minimal effect on Bp and pulse
• Metabolised in the liver to an active form of 3-
deactylvecuronium
REVERSAL AGENTS/ANTICHOLINESTERASE
• NEOSTIGMINE
Reverses non depolarising muscle blockade
Used with atropine or glycopyrrolate to reduce the muscarinic
effects it causes
Active within 1 minute of injection and lasts up to 20 –
30minutes
ANALGESICS
• Simple – Paracetamol
• NSAID – Diclofenac, Ibuprofen
• Opioids - Morphine, Fentanyl
• Others – Ketamine, Clonidine
PARACETAMOL
• Also called Acetaminophen
• Inhibits central prostaglandin synthesis and has a central
antipyretic
• Used to treat minor pain
• Rapidly absorbed with oral administration
• Side effects includes nausea, vomiting and rashes.
DICLOFENAC
• Useful for post-op analgesia thereby reducing requirements for
opioids
• 1mg/kg IM up to 75mg or IV over 15minutes
• Can also begiven rectally
• Could be used with caution in renal impairment and
asthsmatics
MORPHINE
• Used for premedication and as analgesic
• Causes CNS depression
• Induces vomiting
• Releases histamine
• Should be used with caution in renal and hepatic impairment
FENTANYL
• 100 times more potent than morphine
• Used for premedication, induction and sedation in ICU
• Onset is 1-2 minutes and duration of action of 20-60minutes.
• Causes post operative respiratory depression especially with
large doses
• Causes minimal histamine release or cardiovascular changes
LOCAL ANAESTHETICS
• Can be given in the following forms
Topical
Superficial injection ( infiltration)
Nerve Block
Intravenous
Epidural
Spinal
DIVISION OF LA’S
• Ester – they are hydrolysed by blood esterases with a short
half-life.
Examples include Procaine, Cocaine, Benzocaine, Tetracaine,
Chlorprocaine.
• Amides – they are metabolized in the liver and usually have a
long half-life.
Examples include Bupivacaine, Lignocaine, Ropivacaine,
Prilocaine, Articaine.
BUPIVACAINE
• A local anaesthetic agent of longer duration compared to
lidocaine
• For epidural anaesthesia, lasts 3-4 hours and up to 12hours for
nerve blocks
• Usually comes as 0.5%
• Also used for SAB
• Tend to cause more cardiotoxicity compared to neurotoxicity
LIDOCAINE
• Onset is rapid by all routes
• Usual duration of action is 1hour but increases to about 2hours
with the addition of adrenaline
• Used as a local anaesthetic, for nerve blocks, SAB and epidural
anaesthesia.
• Used to depress laryngeal and tracheal reflexes
• Causes more of neurotoxic effects when given in high doses
QUESTIONS
• 1. which of the following will not cause respiration depression
• (a) Propofol
• (b) Ketamine
• (c) Thiopentone
• (d) Midazolam
• (e) Fentanyl
• 2. which of the following has a sweet smell
(a)Nitrous oxide
(b)Halothane
(c)Isoflurane
(d)Desflurane
(e)oxygen
• 3. which on of the following is a depolarising muscle relaxant
(a)Atracurium
(b)Pancuronium
(c)Vecuronium
(d)Suxamethonium
(e)mivacurium
• 4. which of the following is a good post-operative analgesic
• (a) ibuprofen
• (b) acetaminophen
• (c)diclofenac
• (d) cocodamol
• (e) lignocaine
• 5. which one of the following is an amide local anaesthetic
(a)Lignocaine
(b)Procaine
(c)benzocaine
(d)chloroprocaine
(e)cocaine
THEORY
• What are the 6 A’s of premedication
• Write short note on propofol

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INTRODUCTION TO ANAESTHESIA DRUGS.pptx

  • 1. INTRODUCTION TO ANAESTHESIA DRUGS BY DR ADEKUNBI O. OSHUNPIDAN
  • 2. OUTLINE • Brief history of Anaesthesia • Definition of Anaesthesia • Drugs Definition and classification  Premedications  Induction Agents  Muscle Relaxants  Reversal Agents  Analgesics  Local Anaethetics • Conclusion
  • 3. HISTORY • WTG Morton on the 16th of October in 1846 performed the first public demonstration of anaesthesia.
  • 4. DEFINITION •Anaesthesia is a branch of medicine that deals with reversible loss of consciousness and pain control.
  • 5. PREMEDICATIONS • Reduction of anxiety and pain • Promotion of amnesia • Reduction of secretions • Reduction of volume and increase PH of gastric contents • Reduction of postoperative nausea and vomiting • Enhancing the hypnotic effects of general anaesthesia • Reduction of vagal reflexes to intubation • Prophylaxis against allergic reactions
  • 7. GLYCOPYROLATE • Anticholinergic used as premedicant • Reduces salivary and sweat gland activity therefore used as antisialogogue • Used with acetylcholinesterase inhibitors to prevent muscarinic effects
  • 8. ATROPINE • Used for premedication • Used to reduce muscarinic effects of acetylcholinesterase • Used for treatment of bradycardia and asystole • It should be avoided in pyrexial patients
  • 9. TYPES OF ANAESTHESIA • General • Regional – Neuraxial : Subarachnoid Block Epidural Anaesthesia Nerve Block • Local Anaesthesia
  • 10. TRIAD OF GENERAL ANAESTHESIA
  • 11. INTRAVENOUS ANAESTHETICS • These are drugs expected to cause loss of consciousness in “one arm brain circulation” • Characteristics of Ideal Intravenous Anaesthetics  Simple preparation  Painless on administration  High potency and efficacy  Rapid and predictable offset of effect  Absence of toxic effects or adverse properties  Compactible with other agents and IV fluids  Depression of airway reflexes for intubation  Rapid metabolism and minimal hangover
  • 12.
  • 13. CLASSES OF INTRAVENOUS AGENTS • BARBITURATES : Thiopental, Methohexital • PHENOLS : Propofol • IMIDAZOLES : Etomidate • PHENYLCYCLIDINES : Ketamine • BENZODIAZEPINES : Midazolam, Lorazepam, Diazepam. • OPIODS : Morphine, Fentanyl
  • 14. THIOPENTONE • This is an ultra-short acting barbiturate with a rapid onset • Used for induction of anaesthesia and the preferred drug of use in Neuroanesthesia because it reduces cerebral blood flow and intracranial pressure. • Potent anaesthetic, weak analgesic effect with little muscle relaxation • Usually comes in 5 or10% solution and has to be constituted to 2.5% before use. • Causes laryngospasm and not ideal for asthmatics • Causes respiratory and circulatory depression
  • 15. PROPOFOL • Usually comes as a white emulsion of 1 or 2% • Good for induction and maintenance of anaesthesia with a short duration of action, safe for use in day-case surgery. • It causes pain on injection • Causes more respiratory and cardiovascular depression than barbiturates • Has anti –emetic properties
  • 16. KETAMINE • Causes ‘dissociative’ anaesthesia, has a slow onset • Causes amnesia without loss of consciousness • Has analgesic properties • Causes cardiovascular stimulation therefore it is Useful for patients with Hypotension but no respiratory depression
  • 17.
  • 18. INHALATIONAL ANAESTHETICS • Vapors used for induction and maintenance of anaesthesia. They are delivered to the respiratory system to produce anaesthesia.
  • 19. PHYSICAL PROPERTIES OF AN IDEAL INHALATIONAL ANAESTHETIC AGENT 1. Non-flammable, non-explosive at room temperature 2. Stable in light. 3. Liquid and vaporisable at room temperature i.e. low latent heat of vaporisation. 4. Stable at room temperature, with a long shelf life 5. Stable with soda lime, as well as plastics and metals 6. Environmentally friendly - no ozone depletion 7. Cheap and easy to manufacture
  • 20. BIOLOGICAL PROPERTIES OF AN IDEAL INHALATIONAL ANAESTHETIC AGENT 1. Pleasant to inhale, non-irritant, induces bronchodilatation 2. Low blood: gas solubility - i.e. fast onset 3. High oil: water solubility - i.e. high potency 4. Minimal effects on other systems - e.g. cardiovascular, respiratory, hepatic, renal or endocrine 5. No biotransformation - should be excreted ideally via the lungs, unchanged 6. Non-toxic to operating theatre personnel
  • 21. NITROUS OXIDE • Colourless, odourless gas at room temperature • Stored in blue cylinders • Causes rapid induction of anaesthesia and rapid emergence. • it has weak anesthetic and powerful analgesic effects • Used as an adjunct to supplement other inhalationals • Risk of bone-marrow suppression with prolonged administration.
  • 22. HALOTHANE • Volatile liquid at room temperature • Light sensitive • High fat solubility • Excreted unchanged through the lungs • Stored in amber colored bottles with thymols as the preservative • Causes reduced myocardial contractility and cause hypotension
  • 23. ISOFLURANE • Has a pungent smell therefore not ideal for induction of anaesthesia • Causes a progressive respiratory depression and hypotension. • Useful for cardiac anaesthesia
  • 24. SEVOFLURANE • It has a pleasant smell, non-irritant and good for use in paediatrics, cardiac and neuroanaesthesia. • Produces a fast induction and emergence. • Fairly expensive therefore not readily used in our environment
  • 25. MUSCLE RELAXANTS • Divided into two Depolarising – Suxamethonium Non – Depolarising : Divided into 2 1. Aminosteriods – Rocuronium, Vecuronium, Pancuronium 2. Benzylisoquinoloniums – Atracurium, Cisatracurium, Mivacurium.
  • 26. SUXAMETHONIUM • The depolarising neuromuscular blocker of choice • It is widely used due to rapid onset and short duration of action • Ideal for Rapid Sequence Induction • The depolarising effect causes fasciculation and flaccid paralysis • Paralysis occurs one minute after administration and lasts 7 – 12minutes • Metabolised by plasma pseudocholinesterase
  • 27. ATRACURIUM • An intermediate acting muscle relaxant with onset of 60 -90 seconds • Effect lasts 20 – 30 minutes • Causes histamine release • The drug of choice in renal and hepatic impairment
  • 28. PANCURONIUM • Can be used to aid tracheal intubation after 2 – 3 minutes • The effect lasts 40 – 60 minutes • May increase heart rate, BP and cardiac output by vagolytic and sympathomimetic actions. • Elimination is delayed in renal and hepatic impairment therefore avoided in them.
  • 29. VECURONIUM • Provides intubating condition in 90seconds • Relaxation is 20 – 30 minutes but can last up to 80minutes with a dose 250mcg/kg • Has minimal effect on Bp and pulse • Metabolised in the liver to an active form of 3- deactylvecuronium
  • 30. REVERSAL AGENTS/ANTICHOLINESTERASE • NEOSTIGMINE Reverses non depolarising muscle blockade Used with atropine or glycopyrrolate to reduce the muscarinic effects it causes Active within 1 minute of injection and lasts up to 20 – 30minutes
  • 31. ANALGESICS • Simple – Paracetamol • NSAID – Diclofenac, Ibuprofen • Opioids - Morphine, Fentanyl • Others – Ketamine, Clonidine
  • 32. PARACETAMOL • Also called Acetaminophen • Inhibits central prostaglandin synthesis and has a central antipyretic • Used to treat minor pain • Rapidly absorbed with oral administration • Side effects includes nausea, vomiting and rashes.
  • 33. DICLOFENAC • Useful for post-op analgesia thereby reducing requirements for opioids • 1mg/kg IM up to 75mg or IV over 15minutes • Can also begiven rectally • Could be used with caution in renal impairment and asthsmatics
  • 34. MORPHINE • Used for premedication and as analgesic • Causes CNS depression • Induces vomiting • Releases histamine • Should be used with caution in renal and hepatic impairment
  • 35. FENTANYL • 100 times more potent than morphine • Used for premedication, induction and sedation in ICU • Onset is 1-2 minutes and duration of action of 20-60minutes. • Causes post operative respiratory depression especially with large doses • Causes minimal histamine release or cardiovascular changes
  • 36. LOCAL ANAESTHETICS • Can be given in the following forms Topical Superficial injection ( infiltration) Nerve Block Intravenous Epidural Spinal
  • 37. DIVISION OF LA’S • Ester – they are hydrolysed by blood esterases with a short half-life. Examples include Procaine, Cocaine, Benzocaine, Tetracaine, Chlorprocaine. • Amides – they are metabolized in the liver and usually have a long half-life. Examples include Bupivacaine, Lignocaine, Ropivacaine, Prilocaine, Articaine.
  • 38. BUPIVACAINE • A local anaesthetic agent of longer duration compared to lidocaine • For epidural anaesthesia, lasts 3-4 hours and up to 12hours for nerve blocks • Usually comes as 0.5% • Also used for SAB • Tend to cause more cardiotoxicity compared to neurotoxicity
  • 39. LIDOCAINE • Onset is rapid by all routes • Usual duration of action is 1hour but increases to about 2hours with the addition of adrenaline • Used as a local anaesthetic, for nerve blocks, SAB and epidural anaesthesia. • Used to depress laryngeal and tracheal reflexes • Causes more of neurotoxic effects when given in high doses
  • 40.
  • 41. QUESTIONS • 1. which of the following will not cause respiration depression • (a) Propofol • (b) Ketamine • (c) Thiopentone • (d) Midazolam • (e) Fentanyl
  • 42. • 2. which of the following has a sweet smell (a)Nitrous oxide (b)Halothane (c)Isoflurane (d)Desflurane (e)oxygen
  • 43. • 3. which on of the following is a depolarising muscle relaxant (a)Atracurium (b)Pancuronium (c)Vecuronium (d)Suxamethonium (e)mivacurium
  • 44. • 4. which of the following is a good post-operative analgesic • (a) ibuprofen • (b) acetaminophen • (c)diclofenac • (d) cocodamol • (e) lignocaine
  • 45. • 5. which one of the following is an amide local anaesthetic (a)Lignocaine (b)Procaine (c)benzocaine (d)chloroprocaine (e)cocaine
  • 46. THEORY • What are the 6 A’s of premedication • Write short note on propofol