INTRAVENOUS

ANESTHESIA

Intravenous Anesthetics
widely used to facilitate rapid
induction of anesthesia or to
provide sedation during
monitored anesthesia care
(MAC)

NON-OPIOID
IV ANESTHETICS

PROPOFOL

Induction of anesthesia
Maintenance of anesthesia
Sedation
Antiemetic

PROPOFOL
Acts through potentiation of the chloride
current through the -aminobutryric acid
Type A (GABA-A) receptor complex
2,6 diisopropylphenol
Alkyl phenol with HYPNOTIC properties
Usually contains:
10% soybean oil
2.25% glycerol
1.2% lecithin

PROPOFOL

Milky-white
Slightly viscous
pH ~ 7
Rapidly metabolized in the liver
Excreted through the kidneys

PROPOFOL

Cardiovascular Effects
Vasodilation
systemic blood pressure (SBP) is more
pronounced
Exacerbates hypotensive effect
Profound bradycardia and asystole

PROPOFOL
Respiratory Effects
Potent respiratory depressant >>
produces apnea post-induction
Reduction in tidal volume and respiratory
rate
Reduces upper airway reflexes >>
Hence, the use of laryngeal mask airway
Decreases incidence of wheezing and
tracheal intubation among healthy and
asthmatic patients

Barbituric acid

BARBITURATES

Thiopental

Methohexital

BARBITURATES
Induction of Anesthesia
NMBDs are often administered
shortly after the barbiturate to
produce skeletal muscle relaxation
Thiopental + Succinylcholine:
Classic drug regimen for rapid
sequence induction of anesthesia
Neuroprotection

BARBITURATES
Lacks hypnotic effect
Formulated as sodium salts mixed with
anhydrous sodium carbonate
After reconstitution with water and NSS,
the solution is alkaline with pH >10
prevents bacterial growth and helps
increase the shelf-life

BARBITURATES

Central Nervous System Effects

Sedation to general anesthesia in induction
doses
No analgesic effect (reduces the pain
threshold)
Potent cerebral vasoconstrictor
Decrease CBF, CBV, ICP
Useful in management of patient with
space-occupying intracranial lesions

BARBITURATES
Cardiovascular System Effects
Decreases BP
Vasodilation
Barbiturate-induced depression
of the medullary vasomotor
center and decreased
sympathetic nervous system
outflow from the CNS

BARBITURATES

Respiratory System Effects

Depresses the respiration >> leads
to decreased minute ventilation
through reduced tidal volume and
RR.
Induction doses induces transient
apnea
Decreases ventilatory response to
hypercapnia and hypoxia

BENZODIAZEPINES

Diazepam
Midazolam

Flumazenil
Lorazepam

BENZODIAZEPINES
Preoperative medication
Intravenous sedation
Intravenous induction of
anesthesia
Suppression of seizure activity

BENZODIAZEPINES
Activation of GABAA receptor
complex and enhancement of
GABA-mediated chloride
currents leads to
hyperpolarization of neurons
and reduced excitability

BENZODIAZEPINES
Spectrum of EFFECTS:
Sedative-hypnotic
Mediated through the
Amnestic
-subunit of the GABA
Used to treat seizure
receptors
Anxiolysis
Mediated through the
1

-subunit of the GABA

receptors

BENZODIAZEPINES
Highly lipid soluble
Rapid onset of action
Metabolism in the liver through
microsomal oxidation, Ndealkylation and aliphatic
hydroxylation or glucuronide
conjugation
Midazolam has the shortest
context-sensitive half-time, which
makes it the only one that is
suitable for continuous infusion

KETAMINE

KETAMINE
Induction and Maintenance of
Anesthesia
Analgesia (CS and neuraxial
anesthesia)

KETAMINE
- Phencyclidine derivative
- Produces significant analgesia
- Known as dissociative anesthesia patients eyes remain open with a slow
nystagmus gaze (cataleptic gaze)
- Partially water-soluble, but highly lipophilic

KETAMINE
Lacrimation and salivation are increased and
premedication with an anticholinergic is
indicated to limit the effect
EMERGENCE reactions:
Vivid colorful dreams
Hallucinations
Out-of body experience
Increased and distorted visual, tactile, and
auditory sensation
Associated with fear and confusion

ETOMIDATE
Carboxylated imidazole derivative
IV anesthetic with hypnotic but not
analgesic properties and with
minimal hemodynamic effects
Alternative to Propofol and
Barbiturates

ETOMIDAT
E
EFFECT on ENDOCRINE SYSTEM
Causes adrenocortical suppression by
producing a dose-dependent 11 hydroxylase, an enzyme necessary for the
conversion of cholesterol to cortisol
Suppression last 4 to 8 hours

DEXMEDETOMIDATE

Short-term sedation
Adjunct to general
anesthesia to provide
sedation

DEXMEDETOMIDATE

Active S-enantiomer of medetomidine

Used in veterinary medicine
Highly selective 2-adrenergic agonist

DEXMEDETOMIDATE

Hypnosis results from structure of 2

receptor in the locus ceruleus and the
analgesic effect at the level of spinal cord

OPIOID IV ANESTHETICS

30

OPIOIDS
Receptor

Mu

Kappa

Clinical Effect

Supraspinal analgesia (-1)

Respiratory depression (-2)
Physical dependence
Muscle rigidity

Sedation
Spinal analgesia

Agonists

Morphine
Met-enkephalin
Beta-endorphin
Fentanyl
Morphine
Nalbuphine
Butorphanol
Dynorphin
Oxycodone

Delta

Analgesia
Behavioral
Epiletogenic

Leu-enkephalin
Beta-endorphin

Sigma

Dysphoria
Hallucinations
Respiratory stimulation

Pentazocine
Nalorphine
Ketamine

31

OPIOIDS
Inhibits the presynaptic release
and postsynaptic response to
excitatory neurotransmitters
(acetylchloine, substance P)
from neurons.
Transmission of pain impulses
can be interrupted at the dorsal
horn of the spinal cord
32

OPIOIDS
Absorption
Fentanyl - low molecular weight
and high lipid solubility (rapid
onset = 10 min, but short duration
of action)
Morphine - low lipid solubility
(slows passage across the blood
brain barrier)

33

OPIOIDS
Excretion
Eliminated via kidneys (10% via biliary excretion)
Morphine 3-glucuronide & morphine 6glucuronide (morphine metabolites) that could
lead to narcosis and ventilatory depression in
renal failure
Normeperidine (meperidine end product) has an
excitatory effect on the CNS (myoclonic activity
and seizures)

34

OPIOIDS
Cardiovascular effects
Meperidine - increases heart rate
Morphine, fentanyl, sufentanil,
remifentanil, alfentanil - bradycardia (vagusmediated)
Meperidine & morphine - decrease BP and
systemic vascular resistance (histamine
release)
35

OPIOIDS
Respiratory effects
depress ventilation and respiratory
rate
Morphine and meperidine histamine induced bronchospasm
Fentanyl, sufentanil and alfentanil chest wall rigidity

36

OPIOIDS
Cerebral effects
reduce cerebral oxygen consumption,
cerebral blood flow and intracranial
pressure
nausea and vomiting are due to
stimulation of the medullary
chemoreceptor trigger zone
Meperidine - decreases shivering

37

OPIOIDS
Gastrointestinal
reduces peristalsis by slowing the
gastric emptying time
Biliary colic is due to opioid-induced
contraction of the sphincter of Oddi
Constipation due to decrease GI
motility
38

OPIOIDS
Endocrine
blocks the release of hormones
(catecholamines, antidiuretic
hormone and cortisol) during
surgical stimulation

39

"Anesthetics have been used for 160

years, and how they work is one of the
greatest mysteries of neuroscience,"
James Sonner,
M.D. (UCSF)

Thank You &Good Morning!