Inhaled Anesthetics No. 9

Pharmacology Dr. Hussein T.
Alkaisey
Anesthetics
General anesthesia is a reversible state of CNS depression, resulting in

loss of response to and perception of external stimuli. Anesthesia
provides five important benefits :
1. Sedation and reduction of anxiety 2. Lack of awareness and amnesia
3. Skeletal muscle relaxation 4. Suppression of undesirable reflexes
5. Analgesia
No single agent provides all these properties, so, several categories of
drugs are used in combination to produce optimal anesthesia.
PREANESTHETIC MEDICATIONS
1. Antacids: (H2 blockers) prevent gastric acid secretion.
2. Anticholinergics: prevent bradycardia and secretion of fluids into the
respiratory tract.
3. Antiemetics: prevent aspiration of stomach contents and postsurgical
nausea and vomiting.
4. Antihistamines: prevent allergic reactions.
5. Benzodiazepines: relieve anxiety.
6. Opioids: Provide analgesia.
7. Neuromuscular blocking agents: facilitate intubation of the trachea
and suppress muscle tone (relaxation).
Potent general anesthetics are delivered via inhalation and/or intravenous
(IV) injection. With the exception of nitrous oxide, modern inhaled
anesthetics are all volatile, halogenated hydrocarbons. IV anesthetic
agents are used for the rapid induction of anesthesia.
PATIENT FACTORS IN SELECTION OF ANESTHESIA

1. Nature of the surgical or diagnostic procedure.
2. Patient’s physiologic, pathologic, and pharmacologic state.
STAGES OF ANESTHESIA
General anesthesia can be divided into three stages:
1. Induction: The period of time from the onset of administration of the
anesthetic to the development of effective surgical anesthesia.
2. Maintenance: provides a sustained surgical anesthesia.
3. Recovery: is the time from discontinuation of administration of
anesthesia until consciousness and physiologic reflexes are regained.
A. Induction:
1
Pharmacology Dr. Hussein T. Alkaisey
General anesthesia in adults is normally induced with:

1. An IV anesthetic like propofol, which produces unconsciousness
within 30–40 seconds.
2. Additional inhalation and/or IV drugs (anesthetic combination) may
be given to produce the desired depth of surgical anesthesia.
3. Coadministration of an IV skeletal muscle relaxant such as
rocuronium, vecuronium, or succinylcholine to facilitate intubation
and muscle relaxation.
B. Maintenance of anesthesia
The patient’s vital signs and response to various stimuli are monitored
continuously throughout the surgical procedure to balance the amount of
drug inhaled and/or infused with the depth of anesthesia. Anesthesia is
commonly maintained by the administration of:
1. Volatile anesthetics, which offer good control over the depth of
anesthesia.
2. Opioids such as fentanyl are often used for pain relief. along with
inhalation agents, because the latter are not good analgesics.
C. Recovery
Postoperatively, the anesthetic admixture is withdrawn, and the patient
is monitored for the return of consciousness. If skeletal muscle relaxants
have not been fully metabolized, reversal agents may be used. The patient
should be monitored to ensure that he or she is fully recovered.
Depth of anesthesia
Stage I—Analgesia: Loss of pain sensation, the patient progresses from
conscious to drowsy, amnesia and reduced awareness of pain.
2. Stage II—Excitement: The patient experiences delirium, rise and
irregularity in BP and respiration as well as a risk of laryngospasm. To
shorten or eliminate this stage, a rapid acting agent, such as propofol, is
given intravenously before inhalation anesthesia is administered.
3. Stage III—Surgical anesthesia: There is gradual loss of muscle tone
and reflexes. Regular respiration and relaxation of skeletal muscles with
loss of spontaneous movement occur in this stage. Continuous careful
monitoring is required to prevent undesired progression into Stage IV.
4. Stage IV—Medullary paralysis: Severe depression of the respiratory
and vasomotor centers occur during this stage and death can rapidly occur
unless measures are taken to maintain circulation and respiration.
2
GENERAL ANESTHETICS: INHALED

Modern inhalation anesthetics are nonflammable, nonexplosive agents
that include the gas nitrous oxide and a number of volatile, halogenated
hydrocarbons. These agents decrease cerebrovascular resistance, resulting
in increased perfusion of the brain. They also cause bronchodilation and
decrease volume of air per unit time moved into or out of the lungs.
Mechanism of action
No specific receptor has been identified as the site of general anesthetic
action. The focus is now on interactions of the inhaled anesthetics with
proteins comprising ion channels.
1. The general anesthetics increase the sensitivity of the γ-aminobutyric acid
(GABAA) receptors to the neurotransmitter, GABA. Postsynaptic
neuronal excitability is, thus, diminished. Also, the activity of the
inhibitory glycine receptors in the spinal motor neurons is increased.
2. The inhalation anesthetics block the excitatory postsynaptic current of the
nicotinic receptors. The mechanism by which the anesthetics perform
these modulatory roles is not understood.
1. Halothane:
Halothane is a potent anesthetic but a relatively weak analgesic. So, it is
usually coadministered with nitrous oxide, opioids, or local anesthetics. It
is a potent bronchodilator, relaxes both skeletal and uterine muscle, and it
can be used in obstetrics when uterine relaxation is indicated. Halothane
is not hepatotoxic in pediatric patients and its pleasant odor makes it
suitable in children for inhalation induction, although sevoflurane is now
the agent of choice for inhalation induction if cost is not a factor
Adverse effects: Bradycardia, arrhythmias, hypotension.
2. Isoflurane
Isoflurane (eye-soe-FLUR-ane) undergoes little metabolism, so it is not
toxic to the liver or kidney. It does not induce cardiac arrhythmias and
does not sensitize the heart to the action of catecholamines. However, It
produces dose-dependent hypotension due to peripheral vasodilation. It
has a pungent odor and stimulates respiratory reflexes (breath-holding,
salivation, coughing, and laryngospasm) and is, therefore, not used for
inhalation induction.
3. Desflurane
3
Desflurane [DES-flure-ane] provides very rapid onset and recovery due to

its low blood solubility. So, it has made it a popular anesthetic for
outpatient surgery. Desflurane is not used for inhalation inductions
because it is irritating to the airway and can cause laryngospasm,
coughing, and excessive secretions. Its degradation is minimal, and,
therefore, tissue toxicity is rare.
4. Sevoflurane
Sevoflurane [see-voe-FLOOR-ane] has low pungency, allowing rapid
induction without irritating the airway, thus making it suitable for
inhalation induction in pediatric patients. It is replacing halothane for this
purpose. This agent has rapid onset and recovery due to low blood
solubility. Sevoflurane is metabolized by the liver, and compounds
formed in the anesthesia circuit may be nephrotoxic if fresh gas flow is
too low.
5. Nitrous oxide
Nitrous oxide [NYE-truss-OX-ide] is non-irritating and a potent analgesic
but a weak general anesthetic. For example, nitrous oxide is frequently
employed at concentrations of 30–50 percent in combination with oxygen
for analgesia, particularly in dental surgery. This anesthetic does not
depress respiration, and it does not produce muscle relaxation, moderate
to no effect on the cardiovascular system or on increasing cerebral blood
flow, and it is the least hepatotoxic of the inhalation anesthetics.
Therefore, it is probably the safest of these anesthetics.

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Pharmacology Dr. Hussein T.

General anesthesia is a reversible state of CNS depression, resulting in

PATIENT FACTORS IN SELECTION OF ANESTHESIA

General anesthesia in adults is normally induced with:

GENERAL ANESTHETICS: INHALED

Desflurane [DES-flure-ane] provides very rapid onset and recovery due to

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