‫بسم هللا الرحمن الرحيم‬

Sudan International University

Faculty of Medicine
Department of Pharmacology

Qusay Osman Mohamed Abdalla

B. Pharm., M. Pharm., Clinical Pharmacology
qusaysiu@gmail.com
2022

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 [2] Intravenous anesthetic agents:
• They are widely used to facilitate rapid induction of anesthesia and
have replaced inhalation as the preferred method of anesthesia
induction in most settings except for pediatric anesthesia.

• Intravenous anesthetics act much more rapidly, producing

unconsciousness in about 20 seconds, as soon as the drug reaches
the brain from its site of injection.

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• Rate of their recovery is fast.

• Intravenous agents are also commonly used to provide sedation during

monitored anesthesia care and for patients in intensive care (ICU)
settings [Intubation].

• With the introduction of Propofol, intravenous anesthesia became an

option for the maintenance of anesthesia.

• Intravenous agents include: Thiopentone, Etomidate, Ketamine and

Propofol.
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• The currently available intravenous anesthetics are not ideal
anesthetic drugs in the sense of producing all five desired effects.

• Therefore, balanced anesthesia with multiple drugs (inhaled

anesthetics, sedative-hypnotics, opioids, neuromuscular blocking
drugs) is generally used to minimize unwanted side effects.

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1. Thiopentone:
• Thiopentone belongs to the barbiturate class of CNS depressants.
• It has very high lipid solubility, which results in its rapid action when
injected intravenously.
• Thiopentone causes unconsciousness within about 20 seconds, and
lasting for 5-10 minutes.
Actions:
• Its actions on the nervous system are very similar to those of inhalation
anesthetics.
• Has no analgesic effect.

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Drawbacks:
1. Respiratory depression, cardiac arrhythmias, prolonged
somnolence and recovery, sneezing, coughing, bronchospasm,
laryngospasm and shivering.
2. Decreases in arterial blood pressure, stroke volume, and cardiac
output (Dose-dependent with large doses).
3. Long after-effect: drowsiness and some degree of respiratory
depression persist for some hours.
4. Thiopentone, can precipitate an attack of porphyria in susceptible
individuals.
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2. Benzodiazepines:

• Including: Diazepam, Lorazepam, and Midazolam, are used in

anesthetic procedures.

• Benzodiazepines prolong the post-anesthetic recovery period (an

undesirable effect) but also cause a high incidence of anterograde
amnesia which is useful.

• Because it causes an amnesia (> 50%), midazolam is frequently given

intravenously 15-60 minutes before induction of general anesthesia.
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Clinical uses:
1. As anesthesia premedication.
2. Intraoperative sedation.
3. With other drugs, as part of balanced anesthesia.
The benzodiazepine antagonist flumazenil is used to accelerate
recovery from the sedative actions of intravenous benzodiazepines,
but its reversal effect of respiratory depression is less predictable.

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3. Opioid analgesics:

• Include: Morphine, Fentanyl, Alfentanil and Remifentanil.

• Large doses of opioid analgesics [mainly morphine or fentanyl] have

been used to achieve general anesthesia, particularly in patients
undergoing cardiac surgery or other major surgery when circulatory
reserve is minimal.

• Alfentanil and remifentanil are some times used for induction (rapid
onset of anesthetic action).
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• Fentanyl and droperidol together produce analgesia and amnesia and
are sometimes used with nitrous oxide to provide neuroleptic anesthesia.

Drawbacks:

• Intravenous opioids can increase chest wall rigidity, which may impair
ventilation, and postoperative respiratory depression may occur.

N.B: this effect requiring assisted ventilation and opioid antagonists, e.g.
Naloxone.

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4. Etomidate:
• Etomidate is a non-barbiturate hypnotic that acts at the level of the
reticular-activating system to produce anesthesia. It appears to depress
CNS function via GABA.
• Duration of action is intermediate between thiopental and
methohexital, and recovery from a single dose is rapid with little
residual depression.
• Like the barbiturates and propofol, etomidate is does not induce
analgesia.
• Etomidate produces loss of consciousness within seconds, with slight
hypotension.

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Drawbacks:
1. It causes minimal cardiovascular and respiratory depressant
effects.
2. Involuntary movements during induction.

3. Postoperative nausea and vomiting.

4. Suppress the adrenal cortex (with prolonged use) [increase
mortality in severely ill patients].
5. Prolonged infusion of etomidate may result in hypotension,
electrolyte imbalance, and oliguria.
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5. Propofol:
• Propofol is the most frequently administered drug for induction of
anesthesia and has largely replaced barbiturates for this indication.
• The action of propofol involves a positive modulation of the
inhibitory function of GABA
• The pharmacokinetics of Propofol allow it to be used as a
continuous infusion to maintain surgical anesthesia also without
the need for any inhalation agent.
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• Propofol is reported to have antiemetic actions.
• Very rapidly metabolized, and therefore results in rapid recovery
without any hangover effect.
• Fospropofol is a water-soluble prodrug of propofol
Clinical uses:

1. Facilitate induction of general anesthesia.

2. For maintenance of anesthesia.

3. Used for sedation of mechanically ventilated patients in the ICU.

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Drawbacks:
1. Propofol causes a marked decrease in systemic blood pressure during
induction of anesthesia, primarily through decreased peripheral
resistance.
2. It has greater negative inotropic effects on the heart.
3. Pain at the site of injection and apnea also occur.
4. Muscle movements; hypotonus, and rarely tremors have also been
reported following its use.
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6. Ketamine:
• A powerful analgesic intravenous anesthetic agent.
• Heart rate, arterial blood pressure, and cardiac output are usually
significantly increased [stimulating action].
• It is considered to be useful for patients in shock because of its
cardio-stimulatory properties.
• It is also used in outpatient anesthesia and in children undergoing
painful procedures such as dressing changes on burns
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Drawbacks:

• Ketamine has been associated with “emergence phenomena”

[disorientation, sensory and perceptual illusions, and vivid dreams].

• N.B: Diazepam, 0.2-0.3 mg/kg intravenously used 5 minutes before

administration of ketamine, is effective in reduction of the incidence
of this phenomena.

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 Any Qs?

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