Anesthetics Drugs
By: Muhammad Aurangzeb
Lecturer-INS/KMU
Objectives
By the completion of this section the learners will be able to:
• Define the term anesthesia and anesthetic agents
• Differentiate between different types of anesthesia
• Identify the stages of general anesthesia
• Describe Characteristics of general and local anesthetic agents.
• Identify most commonly used anesthetic agents
• Discuss factors considered when choosing anesthetic agents.
• Compare general and local anesthesia in terms of administration, client’s safety
and nursing care.
• Discuss the rationale for using adjunctive drugs before and during surgical
procedures.
• Describe the nursing role in related to anesthetics and adjunctive drugs.
• Discuss the action, indication and side effects of neuro-muscular blocking agent
• Calculate the drug dosage of injectable anesthetic agent
Anesthesia
• The word anesthesia is coined from two Greek words: "an"
meaning "without" and "aesthesis“ meaning "sensation".
• Anesthesia refers to the practice of administering
medications either by injection or by inhalation (breathing
in) that block the feeling of pain and other sensations, or
that produce a deep state of unconsciousness that
eliminates all sensations, which allows medical and
surgical procedures to be undertaken without causing
undue distress or discomfort.
Anesthesia
• It is a pharmacologically induced and reversible state of amnesia,
analgesia, loss of responsiveness, loss of skeletal muscle reflexes or
decreased stress response, or all simultaneously.
• An alternative definition is a "reversible lack of awareness," including
a total lack of awareness (e.g. a general anesthetic) or a lack of
awareness of a part of the body such as a spinal anesthetic.
• The pre-existing word anesthesia was suggested by Oliver Wendell
Holmes, Sr. in 1846 as a word to use to describe this state.
• Anesthesiology is a special branch of medicine.
• Nurses working in this area need to have knowledge and skill to care
for the patient who is being given premedication, under anesthesia
and recovering.
Anesthetic Agents
• Anesthetic drugs are the agents that produces
anesthesia or bring about reversible
loss of sensation .
• Two types a) General anesthetics
b) Local anesthetics
Types of Anesthesia
Classified into 2 major types. They are :
1. General anesthesia.
2. Local & regional anesthesia.
General anesthesia
• General anesthesia refers to inhibition of sensory, motor and
sympathetic nerve transmission at the level of the brain,
resulting in unconsciousness and lack of sensation.
• General anesthesia – for surgical procedure to render the
patient unaware / unresponsive to the painful stimuli
• Drugs producing General Anesthesia – are called General
Anesthetics
Local anesthesia
• Local anesthesia - reversible inhibition of impulse generation
and propagation in nerves. In sensory nerves, such an effect is
desired when painful procedures must be performed, e.g.,
surgical or dental operations
• Drugs producing Local Anesthesia – are called Local
Anesthetics e.g. Procaine, Lidocaine and Bupivacaine etc.
• Local anesthesia inhibits sensory perception within a specific
location on the body, such as a tooth or the urinary bladder
Regional Anesthesia
• Regional Anesthesia : Regional anesthesia renders a larger
area of the body insensate by blocking transmission of nerve
impulses between a part of the body and the spinal cord.
• Two frequently used types of regional anesthesia are spinal
anesthesia and epidural anesthesia.
Spinal Anesthesia
• Spinal Anesthesia: it is achieved by injection 1.8 ml of 5%
lignocaine solution into the subarachnoid space through a
lumber puncture.
• Other drugs which can be used are cinchocaine, procaine and
amethocaine.
• It can cause serious hypotension.
Epidural Anesthesia
• Epidural Anesthesia: It is achieved by injection 1 to 2 % of
lignocaine solution in the epidural space.
• It blocks the nerves which traverse the epidural space.
• It can cause hypotension, which is less severe than with spinal
analgesia.
• For prolonged operations, a catheter may be passed into the
epidural space for intermittent administration of local
anesthesia.
Stages of General Anesthesia
Four stages of anesthesia
• Stage I Analgesia
• Stage II Excitement
• Stage III Surgical anesthesia
• Stage IV Medullary paralysis
Stages Cont…
Stage I Analgesia
• Loss of pain sensation
• Drowsiness
• Amnesia and reduced awareness of pain
Stage II Excitement
• Delirium
• Rise and irregularity in blood pressure and respiration
• Risk of laryngospasm
• To shorten this period a rapid acting anesthetic like propofol
is administered IV before inhaled anesthetic
Stages Cont…
Stage III: Surgical anesthesia
• Loss of muscle tone and reflexes
• Ideal stage for surgery
• Requires careful monitoring
Stage IV: Medullary paralysis
• Severe depression of the respiratory and vasomotor centers
• Death can occur unless respiration and circulation are
maintained
Practically what is done in OT ???
•There are 3 (three) phases:
• – Induction, Maintenance and Recovery
• Induction (Induction time): It is the period of time which
begins with the beginning of administration of anesthesia to
the development of surgical anesthesia (Induction time).
Induction is generally done with IV anesthetics like
Thiopentone Sodium and Propofol
• Maintenance: Sustaining the state of anesthesia. Usually
done with an admixture of Nitrous oxide and halogenated
hydrocarbons
• Recovery: At the end of surgical procedure administration of
anesthetic is stopped and consciousness regains (recovery
time)
General anesthetics (Defn.)
• General Anesthetics are the drugs which produce reversible
loss of all sensation and consciousness, or simply, a drug that
brings about a reversible loss of consciousness
• Remember !!! These drugs are generally administered by an
anesthesiologist in order to induce or maintain general
anesthesia to facilitate surgery
• General anesthetics are – mainly inhalation or intravenous
• Local anesthetics are drugs which upon topical application or
local injection cause reversible loss of sensory perception,
especially of pain in a localized area of the body
What are the Drugs used as GA ?
(Classification)
• Inhalation:
• Intravenous:
1. Gas: Nitrous Oxide
1. Inducing agents:
2. Volatile liquids:
• Ether • Thiopentone,
• Halothane Methohexitone sodium,
propofol and
• Enflurane
etomidate
•
Isoflurane 2. Benzodiazepines (slower
•
Desflurane acting):
•
Sevoflurane • Diazepam,
Lorazepam,
Midazolam
3. Other drugs
• Ketamine
• Fentanyl
Local Anaesthetics
Ester Linkage Amide Linkage (2 Eyes!!)
PROCAINE LIDOCAINE
procaine (Novocaine) lidocaine (Xylocaine)
tetracaine (Pontocaine) mepivacaine (Carbocaine)
benzocaine bupivacaine (Marcaine)
cocaine etidocaine (Duranest)
ropivacaine (Naropin)
Factors considered when choosing
anesthetic agents
• Choice of anesthetic drugs are made to provide safe
and efficient anesthesia based on the nature of the
surgical or diagnostic procedures and patient’s
physiologic, pathologic and pharmacologic state
Patients Factors in selection of Anesthesia
• 2 factors are important
– Status of organ system
• Cardiovascular system
• Respiratory system
• Liver and kidney
• Nervous system
• Pregnancy
– Concomitant use of drugs
• Multiple adjunct agents
• Non-anesthetic drugs
Status of the Organ System
Cardiovascular system:
• Anesthetic agents suppress cardiovascular functions.
• Ischemic injury to tissues may follow reduced perfusion
pressure if a hypotensive episode occurs during anesthesia,
treatment with vasoactive substances may be necessary
• Some anesthetics like halothane sensitize the heart to
arrhythmogenic effects of sympathomimetics
Status of the Organ System
Respiratory system
• Asthma may complicate control of inhalation anesthetic
• Inhaled anesthetics depress the respiratory system
• IV anesthetics and opioids suppress respiration
• These effects may influence the ability to provide adequate
ventilation and oxygenation
Status of the Organ System
Liver and kidneys
• Affect distribution and clearance of anesthetics, and might be
affected by anesthetic toxic effects
• Their physiology must be considered
Nervous system
• Presence of neurologic disorders like epilepsy, myasthenia
gravis, problems in cerebral circulation
Pregnancy
• Effects of anesthetic agents on the fetus
• Nitric oxide causes aplastic anemia in the unborn child
• Benzodiazepines might cause oral clefts in the fetus
Concomitant use of drugs
Multiple adjunct agents
• Multiple agents are administered before anesthesia, these
agents facilitate induction of anesthesia and lower the
needed dose of anesthetics
• They may enhance adverse effects of anesthesia like
hypoventilation
Concomitant use of additional non-anesthetic drugs
– Example: Opioid abusers may be intolerant to opioids
Other Conditions to be Considered before
Anesthesia
Some specific conditions increase the risk to the patient undergoing
general anesthetic:
• Obstructive sleep apnea Seizures
• Existing heart, kidney or lung conditions
• High blood pressure
• Alcoholism
• Smoking
• History of reactions to anesthesia
• Medications that can increase bleeding - aspirin, for example
• Drug allergies
• Diabetes
Obstructive sleep apnea - a condition where individuals stop
Rationale for using adjunctive drugs before and
during surgical procedures.
• For patients undergoing surgical and other medical
procedures anesthesia provides these benefits:
– Sedation and reduction of anxiety
– Lack of awareness and amnesia
– Skeletal muscle relaxation
– Suppression of undesirable reflexes
– Analgesia
• Because no single agent can provide all those benefits,
several drugs are used in combination to produce optimal
anesthesia
Adjunctive drugs or pre-anesthetic
medications
Serve to calm the patient, relieve the pain and protect against
undesirable effects of anesthetics or the surgical procedure
• Antacids (neutralize stomach acidity)
• H2 blockers like famotidine (Reduce gastric acidity)
• Anticholinergics like atropine and glycopyrrolate (Prevent
bradycardia and secretion of fluids)
• Antiemetics like ondansetron (Prevent aspiration of stomach
contents and postsurgical nausea and vomiting and)
• Antihistamine (Prevent allergic reactions)
• Benzodiazepines like diazepam (Relieve anxiety)
• Opioids like fentanyl (Provide analgesia)
• Neuromuscular blockers (Facilitate intubation and relaxation)
Skeletal Muscle Relaxants
• It facilitate intubation of the trachea and suppress muscle
tone to the degree required for surgery
• Following neuromuscular blockers or skeletal muscle relaxant
are commonly used
– Pancuronium
– Atracurium (acuron)
– Succinylcholine
Characteristics of general and local
anesthetic agents
Potent general anesthetics are delivered via
inhalati on or IV injecti on
◦ Inhaled general anesthetics
◦ Intravenous general anesthetics
Local anesthetics
Desflurane
Halothane
Isoflurane
Sevoflurane
Nitrous oxide
Used for maintenance of anesthesia after
administration of an IV agent
The depth of anesthesia can be altered rapidly
by changing inhaled concentration of the
drug
Narrow therapeutic index (from 2 - 4)
The difference between the dose causing no
effect, surgical anesthesia and severe cardiac
and respiratory depression is small
No antagonists exist
Potency of inhaled anesthetic is defined as
the minimum alveolar concentration
(MAC)
MAC: the concentration of anesthetic gas
needed to eliminate movement among
50% of patients
Expressed as the percentage of gas in a
mixture required to achieve the effect
The smaller MAC is the more potent the
drug
Nitrous oxide alone cannot
produce complete anesthesia
The more the blood solubility, the
more the anesthetic dissolves in the
blood and the longer the induction
and recovery time needed and slower
changes in the depth of anesthesia
occur as we change the concentration
of inhaled drug
Halothane> isoflurane>
sevoflurane>nitrous oxide >desflurane
Cardiac output affects the removal of anesthetic to
peripheral tissues (not the site of action)
The higher the cardiac output, the more the
anesthetic is removed, the slower the induction
time
Mechanism of action
◦ No specific receptor has been identified as the locus of
general anesthetic action
◦ Anesthetics increase the sensitivity of GABA receptors to
the neurotransmitter GABA prolonging the inhibitory
chloride ion current after GABA release, reducing the
postsynaptic neurons excitability
◦ Anesthetics increase the activity of the inhibitory glycine
receptors in the spinal motor neuron
◦ Anesthetics block excitatory postsynaptic nicotinic
currents
◦ The mechanism by which the anesthetics perform these
modulatory roles is not understood
Potent anesthetic, weak analgesic.
Administered with nitrous oxide, opioids or
local anesthetics
Being replaced by other agents due to its adverse
effects
Adverse effects
◦ Cardiac effects: Vagomimetic effects, bradycardia, can
cause cardiac arrhythmias
◦ Malignant hyperthermia:
Rare and life threatening condition
Uncontrolled increase in skeletal muscle oxidative
metabolism, which overwhelms the body’s capacity to
supply oxygen, remove carbon dioxide, and regulate
body temperature
If untreated would cause circulatory collapse and
death
Treatment: Dantrolene administration
Dantrolene sodium is a postsynaptic muscle
relaxant that lessens excitation-contraction
coupling in muscle cells. It achieves this by
Undergoes little metabolism, not toxic to the
liver or kidney
Does not induce cardiac arrhythmias
Produces dose-dependent hypotension due to
peripheral vasodilation
Provides very rapid onset and recovery due to its
low blood solubility, the lowest of all the
volatile anesthetics
Popular anesthetic for outpatient surgery
Irritating to the airway and can cause
laryngospasm, coughing, and excessive
secretions,
Degradation is minimal, tissue toxicity
is rare
Low pungency, allowing rapid induction without
irritating the airway, making it suitable for
inhalation induction in pediatric patients
Replacing halothane for this purpose
Metabolized by the liver, and compounds formed
in the anesthesia circuit may be nephrotoxic
Non-irritating and a potent analgesic but a weak general anesthetic
Nitrous oxide is frequently employed at concentrations of 30–50% in
combination with oxygen for analgesia.
Nitrous oxide at 80 percent (without adjunct agents) cannot produce
surgical anesthesia
Combined with other, more potent agents to attain pain-free
anesthesia
Mechanism of action is unresolved, might involve activity on GABAA and
NMDA receptors
Least hepatotoxic of all inhaled anestheticsm
The N-methyl-D-aspartate receptor, is a glutamate receptor and ion
channel protein found in nerve cells. The NMDA receptor is one of three
types of ionotropic glutamate receptors. The other receptors are the
Used in situations that require short duration
anesthesia (outpatient surgery)
Primarily used as adjuncts to inhalationals
Administered first
Rapidly induce unconsciousness
In lower doses, they may be used to provide
sedation
Induction
After entering the blood stream, a percentage of the drug
binds to the
plasma proteins, and the rest remains unbound (free)
The drug is carried by venous blood to the heart
The majority of the CO (70%) flows to the brain, liver, and
kidney
Once the drug has penetrated the CNS tissue, it exerts its
effects
The exact mechanism of action of IV anesthetics is unknown
Recovery
Recovery from IV anesthetics is due to redistribution from
sites in the CNS
Propofol
Fospropofol
Barbiturates
Benzodiazepines
Opioids
Ketamine
IV sedative/hypnotic used in the induction or
maintenance of anesthesia
Widely used and has replaced thiopental as first choice
for anesthesia induction and sedation, because it
does not cause postanesthetic nausea and vomiting
The induction of anesthesia occurs within 30–40
seconds of administration
Supplementation with narcotics for analgesia is
required
Propofol decreases blood pressure without
depressing the myocardium
It also reduces intracranial pressure due to systemic
vasodilation
Approved only for sedation
Prodrug of propofol
The barbiturates are not signifi cantly analgesic, require some
type of supplementary analgesic administrati on during
anesthesia to avoid objecti onable changes in blood pressure
and autonomic functi on
Can cause apnea, coughing, chest wall spasm,
laryngospasm, and bronchospasm
Thiopental
◦ Potent anesthetic but a weak analgesic
◦ Ultrashort-acting barbiturate
◦ Has minor effects on the cardiovascular system, but it may
contribute to severe hypotension in patients with hypovolemia
or shock.
Used in conjuncti on with anesthetics to sedate the pati ent
Midazolam
Diazepam
Lorazepam
Facilitate amnesia while causing sedation
Enhance the inhibitory effects of various
neurotransmitters, particularly GABA
Minimal cardiovascular depressant effect
Potential respiratory depressants
Can induce a temporary form of anterograde amnesia in
which the patient retains memory of past events, but new
information is not transferred into long-term memory
◦ Important treatment information should be repeated to the
patient after the effects of the drug have worn off
Commonly used with anesthetics due to their analgesic
property
The choice of opioid used perioperatively is based
primarily on the durati on of acti on needed
Fentanyl, remifentanil
◦ Induce analgesia more rapidly than morphine
◦ Administered intravenously, epidurally, intrathecally
Not good amnesics
Can cause hypotension, respiratory depression, muscle
rigidity and postanesthetic nausea and vomiting
Opioid effects can be antagonized by naloxone
A short-acti ng nonbarbiturate anesthetic
Used for short procedures
Induces a dissociated state in which the patient is
unconscious (but may appear to be awake) and does
not feel pain
This dissociative anesthesia provides sedation,
amnesia, and immobility
Interacts with the N-methyl-D-aspartate
receptor (NDMA)
Stimulates the central sympathetic outflow, which, in
turn, causes stimulation of the heart with increased
blood pressure and CO
◦ Beneficial in patients with hypovolemic or cardiogenic shock
and in patients with asthma)
◦ Not used in hypertensive or stroke patients
Causes post-operative hallucinations
Used to stop reflexes to facilitate tracheal
intubation, and to provide muscle relaxation as
needed for certain types of surgery
Mechanism of action is blockade of the nicotinic
acetylcholine receptors in the neuromuscular
junction
Include pancuronium, rocuronium,
succinylcholine, and vecuronium
Amides (lidocaine) and esters (procaine)
Cause loss of sensation and, in higher
concentrations, motor activity in a limited area of
the body
Applied or injected to block nerve conduction of
sensory impulses from the periphery to the
CNS
Mechanism:
◦ Local anesthesia is induced when propagation of
action potentials is prevented, so that
sensation cannot be transmitted from the
source of stimulation to the brain
◦ Work by blocking sodium ion channels to prevent
the transient increase in permeability of the nerve
membrane to sodium that is required for an
action potential to occur
Lidocaine
Bupivacaine
Procaine
Ropivacaine
Tetracaine
Mepivacaine
◦ Not used in obstetric anesthesia due to its increased
toxicity to the neonate
Local anesthetics cause vasodilation, which
leads to rapid diffusion away from the site of
action and results in a short duration of action
Adding the vasoconstrictor epinephrine to the
local anesthetic, the rate of local anesthetic
diffusion and absorption is decreased
This both minimizes systemic toxicity and
increases the duration of action
They are applied directly to the skin or
mucous membranes
Benzocaine is the major drug in this group
Lidocaine and tetracaine ca be used topically
They are used to relieve or prevent pain from minor
burns, irritation, itching
They are also used to numb an area before an
injection is given.
Expected adverse effects involve skin irritation and
hypersensitivity reactions
Comparison of general vs local
anesthesia
General anesthesia
• General anesthesia is a medically induced state of
unconsciousness with loss of protective reflexes, resulting
from the administration of one or more general anesthetic
agents.
Method of administration of GA
2 Methods of administration
1. Inhaled anesthesia
2. IV route
Essential components of GA:
Cardinal Features:
– Loss of all sensations
– Sleep and Amnesia
– Immobility or Muscle
– relaxation
Abolition of reflexes –
somatic and
Clinically – What an Anaesthetist wants ???
autoonomic
– Triad of GA
• need for unconsciousness
• need for analgesia
• need for muscle relaxation
Advantages of general anesthesia
• Reduces intra-operative patient awareness and recall.
• Allows proper muscle relaxation for prolonged periods of
time.
• Facilitates complete control of the airway, breathing, and
circulation.
• Can be used in cases of sensitivity to local anesthetic agent.
• Can be administered rapidly and is reversible.
Disadvantages of general anesthesia
• Requires increased complexity of care and associated costs.
• Requires some degree of preoperative patient preparation.
• Can induce physiologic fluctuations that require active
intervention.
• Associated with malignant hyperthermia
Nursing role in GA
• Assessment:
– Prescription, non-prescription or any other Drug History
– Allergies
– Other risk factors – smoking, obesity,
alcoholism, CVS/renal/respiratory diseases
– Vital signs and laboratory data
• Interventions:
– Explain preoperative and post operative
recovery
– Postoperative requirements – early ambulation, deep
breathing, coughing, leg exercises, fluid balance and urine
output
– Monitor vital signs
– Response to pain medication
Local anesthesia
• Local anesthesia is the reversible loss of sensation in a
defined area of the body and is achieved by the topical
application or injection of agents that block the generation
and/or journey of nerve impulses in tissue.
Methods of administration
Surface anesthesia
- By direct application for skin & mucous membrane
Infiltration anesthesia
- By S.C injection to reach fine nerve branches and sensory nerve terminals.
Nerve block anesthesia
- By injection close to the appropriate nerve trunks (Brachial plexus) to produce
a loss of sensation peripherally.
.
Epidural anesthesia
- The LA is injected in the epidural space, between the dura & bony spinal canal
containing fat & connective tissue.
- It can be performed in sacral hiatus (Caudal anesthesia)
Spinal
- The LA is injected in the subarachnoid space in the lumbar region
Advantages of Local anesthetic
• During local anesthesia the patient remains conscious.
• Patient maintains own airway.
• Aspiration of gastric contents unlikely.
• Recovery is smooth as it requires less skilled nursing care
as compared to other anesthesia like general anesthesia.
• Postoperative analgesia.
• There is reduction surgical stress.
• Earlier discharge for outpatients.
• Expenses are less.
Disadvantages/side effects of LA
• Very rare allergies
• Bruises
• Temporary tingling sensation or burning in the area
Nursing Role in LA
• Assess for the mentioned cautions and contraindications (e.g.
drug allergies, hepatic and renal impairment, etc.) to prevent
any untoward complications.
• Inspect site for local anesthetic application to ensure integrity
of the skin and to prevent inadvertent systemic absorption of
the drug.
• Ensure that patients receiving spinal anesthesia or epidural
anesthesia are well hydrated and remain lying down for up to
12 hours after the anesthesia to minimize headache.
• Provide skin care to site of administration to reduce risk of
skin breakdown.
• Provide safety measures (e.g. adequate lighting, raised side
rails, etc.) to prevent injuries.
References
• Karch, A. M., & Karch. (2011). Focus on nursing pharmacology.
Wolters Kluwer Health/Lippincott Williams & Wilkins. [Link]
• Katzung, B. G. (2017). Basic and clinical pharmacology.
McGraw-Hill Education.
• Lehne, R. A., Moore, L. A., Crosby, L. J., & Hamilton, D. B.
(2004). Pharmacology for nursing care.
• Smeltzer, S. C., & Bare, B. G. (1992). Brunner & Suddarth’s
textbook of medical-surgical nursing. Philadelphia: JB
Lippincott.
