Drugs Used in Anesthesia

DRUGS USED IN
ANESTHESIA
ANESTHESIA
I. Pre-anesthesia evaluation, preparation
II. Pre-anesthesia medication
III. Anesthesia steps:
i- Induction
ii- Maintenance
iii- Recovery
Monitoring
Anesthesia Medications
I. Pre-anesthesia medications:
I. Benzodiazepines
II. Anticholinergics
III. Antiemetics
IV. Opioid analgesics
II. General Anesthesia Drugs

I. Inhalational
II. I.V.
III. Muscle Relaxants
IV. Analgesics
III. Local Anesthetics

Steps of Anesthesia
• Induction  the period of time from the onset
of administration of the anesthetic to the
development of effective surgical anesthesia in
the patient.
• Maintenance  A sustained surgical anesthesia
• Recovery  time from discontinuation of
administration of the anesthesia until
consciousness and protective physiologic
reflexes are regained.
•Inhalational Anesthetics
• Inhaled anesthetics are the mainstay of anesthesia.
• It is used primarily for the maintenance of anesthesia
after administration of an intravenous agent.
• It has a benefit over intravenous agents in that the
depth of anesthesia can be rapidly altered by
changing the concentration of the drug.
• It is also reversible, because most are rapidly
eliminated from the body by exhalation.
• Modern inhalational anesthetics are nonflammable,
nonexplosive agents that include the gas nitrous
oxide, as well as a number of volatile, halogenated
hydrocarbons.
• As a group, these agents ↓ cerebrovascular
resistance, ↓ myocardial contractility in a dose
dependent manner → ↓ arterial blood pressure.
• Also as a group these agents cause bronchodilation
• All halogenated anesthetics have been reported
to cause hepatitis, but at a much lower
incidence than with halothane.
• Till now the mechanism of action of inhalational
anesthetic agents is not known.
Non-Volatile Anesthetic Agents
Barbiturates :-
Thiopental is a potent anesthetic but a week

analgesic.
It is an ultra-short acting barbiturate and has a
high lipid solubility.
When these agents are administered i.v. they quickly
enter CNS and depress function often in less than one
minute
However , diffusion out of the brain can occur very

rapidly as well because of redistribution of the drug to
other body tissues, including skeletal muscles and
ultimately adipose tissues.
These adipose tissues serves as a reservoir of
drugs from which the agent slowly leaks out
and is metabolized and excreted.
Thus, metabolism of thiopental is much
slower than it's tissue redistribution.
Thiopental may contribute to severe
hypotension in hypovolemic or shock
patients.
All barbiturates can cause
apnea
coughing
chest wall spasm
laryngospasm
bronchospasm
Propofol :-
It induces a general anesthesia through
facilitation of inhibitory neurotransmission
mediated by GABA.
It`s high lipid solubility results in a fast onset of
action as that of thiopental.
Recovery from propofol is more rapid with less
hangover than recovery from thiopental.
This last property makes propofol a good agent for
outpatient anesthesia.
A unique characteristic of propofol is it`s antipruritic

and antiemetic effect.
Both thiopental and propofol are potent

anticonvulsant.
Ketamine :-
It has multiple effects throughout the central nervous
system.
In contrast to the depression of the reticular activating
system induced by barbiturates, Ketamine
functionally dissociates the thalamus
This last state is called Dissociative Anesthesia in

which patient appear conscious ( e.g. eye opening,
swallowing, muscle contracture ) but unable to
process or respond to sensory stimuli.
It has a good analgesic and amnesic effect.

In contrast to other anesthetic agents ketamine
increases BP, HR, and CO, due to central stimulation
of the sympathetic nervous system.
This last property is beneficial in patients with either

hypovolemic or cardiogenic shock, as well as in
patients with asthma.
On the other hand ketamine should be avoided in

patients with coronary artery disease, uncontrolled
hypertension, and cerebral stroke.
It is lipophilic and enter brain circulation very
quickly → redistribute to other organs.
It is used mainly in children, and infrequent in

adults because it can induces postoperative
hallucinations.
Benzodiazepines
They have anti-anxiety, amnesic, and sedative effects
seen at low doses that progress to stupor and
unconsciousness at induction doses.
Benzodiazepines have no direct analgesic properties.

They have mild muscle relaxant property mediated at
the spinal cord level, not at the neuromuscular
junction.
They are very effective in preventing and controlling

grand mal seizures.
Benzodiazepines interact with specific receptors
in CNS, particularly in cerebral cortex →
enhances the inhibitory effects of various
neurotransmitters.
Flumazenil is a specific benzodiazepine- receptor

antagonist that effectively reverses most of the
CNS effect of benzodiazepines.
Opioids or Narcotics
The term opioid refers to all drugs, synthetic and natural,

that have morphine-like actions, including antagonist
action.
Narcotic is derived from the Greek word for stupor.
While opioids provide some degree of sedation, they are
most effective at producing analgesia.
These drugs give their analgesic effect through binding
to specific receptors located throughout CNS and other
tissues.
Naloxone:
Naloxone is a competitive antagonist at opioid
receptors.
Naloxone reverses the agonist activity of opioids, a
dramatic response is the reversal of unconsciousness
that occurs in a patient with opioid overdose who has
received naloxone.
Abrupt reversal of opioid analgesia can result in
sympathetic stimulation ( tachycardia, ventricular
irritability, hypertension, pulmonary edema ) caused
by pain perception.
Neuromuscular Blocking Agents
Skeletal muscle relaxation can be produced by deep

inhalational anesthesia, regional nerve block, or
neuromuscular junction blocking agents ( commonly
called muscle relaxants ).
Muscle relaxation does not ensure unconsciousness,
amnesia, or analgesia.
Neuromuscular blocking agents can be divided into two
classes: depolarizing and nondepolarizing.
Specific reversal agents ( e.g. cholinesterase
inhibitors ) inhibit acetylcholinesterse enzyme activity
→ ↑ amount of Ach available at the neuromuscular
junction to compete with the nondepolarizing agents.
Clearly, the reversal agents are of no benefit in

reversing a depolarizing block.
The only depolarizing MR in general use today is

succinylcholine ( suxamethonium or diacetylcholine ),
It consists of two joined Ach molecules.
Local Anesthetics
Local anesthetics reversibly block nerve conduction,
they are used to provide regional anesthesia for
surgery & for postoperative analgesia.
L.As in tracheal intubation, ↓ coughing during

intubation and extubation, and are antiarrhythmic.
Classification:
Aminoesters
Aminoamides .
•Commonly used amides
lidocaine
bupivacaine
mepivacaine
ropivacaine
Commonly used esters include
procaine
chloroprocaine
cocaine
tetracaine
L.As produce it`s effects through blockade of sodium
channel and consequent inhibition of Na
conductance.
The rate of systemic absorption is proportionate to the
vascularity of the site of injection : intravenous >
tracheal > intercostal > caudal > paracervical >
epidural > brachial plexus > sciatic > subcutaneous.
Systemic toxicity is due to elevated plasma local
anesthetic levels, most often a result of inadvertent
i.v. injection and less frequent a result of systemic
absorption of L.As from injection site.
Toxicity involves cardiovascular and CNS :
CNS toxicity :
Circumoral numbness, tongue paresthesia, dizziness,
tinnitus, blurred vision, restlessness, agitation,
nervousness, followed by slurred speech, drowsiness,
and coma.
Cardiotoxicity:
Hypertension, tachycardia, decreased contractility and
C.O, Hypotension, sinus bradycardia, ventricular
dysrhythmias, circulatory arrest.
Bupivacaine is the most cardiotoxic local anesthetic.
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Drugs Used in Anesthesia

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Drugs Used in Anesthesia

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DRUGS USED IN

II. General Anesthesia Drugs

III. Local Anesthetics

Thiopental is a potent anesthetic but a week

However , diffusion out of the brain can occur very

A unique characteristic of propofol is it`s antipruritic

Both thiopental and propofol are potent

This last state is called Dissociative Anesthesia in

It has a good analgesic and amnesic effect.

This last property is beneficial in patients with either

On the other hand ketamine should be avoided in

It is used mainly in children, and infrequent in

Benzodiazepines have no direct analgesic properties.

They are very effective in preventing and controlling

Flumazenil is a specific benzodiazepine- receptor

The term opioid refers to all drugs, synthetic and natural,

Skeletal muscle relaxation can be produced by deep

Clearly, the reversal agents are of no benefit in

The only depolarizing MR in general use today is

L.As in tracheal intubation, ↓ coughing during

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