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.