Anesthesia and Muscle Relaxants
Subclass, Drug Mechanism of Action
Inhalational Anesthetics: Laughing gas
Gaseous: Potent analgesic but a weak
anesthetic in the sense that it
Nitrous Oxide does not produce adequate
muscular relaxation
Explosive and flammable
Cyclopropane property
Xenon
Volatile halogenated: Nonether derivative (ethane)
Can cause dose dependent
reduction of arterial blood
Halothane pressure due to: direct
(2 bromo-1, 1, 1- depression of myocardium,
triflouroethane) normal baroreceptor
mediated tachycardia
Halogenated ether derivative
Enflurane Produces mild stimulation of
(2 chloro-112-trifluroethyl- salivation and
Difluromethlether) tracheobronchial secretion
Halogenated ether derivative
Isoflurane
(1 chloro-222-trifluroethyl-
Difluromethylether)
Clear, colorless liquid with
sweet fruity odor
Methoxyflurane Most potent of the
(2,2 dichloro-1,1- inhalational anesthetic
difluroethymethylether) Most toxic of the inhalational
anesthetic
Fluorinated methy ethyl
ether
Desflurane
Effects Clinical Applications P, T, I
Sweet smelling, non-irritating Hematoxicity (megaloblastic
colorless gas anemia)
The only inorganic gas in
common use possessing
anesthetic properties
Sensitizes the myocardium to Malignant hyperthermia,
epinephrine and circulating cardiotoxic, hepatotoxic,
catecholamines halothane hepatitis,
bradycardia
Seizure-like EEG activity Seizure-like attack Cardiotoxic, nephrotoxic
Free-fluoride radical Spike and wave pattern on
the EEG
Agent of choice for cardiac
surgery coronary steal
syndrome
Formerly used for obstetric Nephrotoxic, hepatotoxic,
anesthesia and analgesia cardiotoxic
A newer inhalational
anesthetic that differ from
isoflurane only by
substitution of a fluoride
1
 atom from chlorine
Pungent odor
Fluorinated methy ethyl Seizure-like EEG activity
ether
Sevoflurane Low pungency, good for
pediatric patients
Nonhalogenated: First anesthetic discovered
Seldom used today because
Ether of its flammability and
explosive property
No longer use today because
Chloroform of its liver toxicity
Nonexplosive, nonflammable
Intravenous Anesthetics: DOC for induction of Garlic or onion taste Absolute contraindication:
anesthesia in patients with acute intermittent porphyria
elevated ICP
Barbiturates Methohexital = DOC for ECT
[Thiopental, Methohexital,
Thiamylal]
Most commonly used for Midazolam = more rapid Erythromycin prolongs Anterograde amnesia
preop medication, DLM, IV onset, steeper dose response effects of benzodiazepines
Benzodiazepines sedation, and suppression of curve, more favorable
[Diazepam, Lorazepam, seizure activity Antagonist: flumazenil
Midazolam] DOC for premedication
Chest wall rigidity > fentanyl Adjunct to provide
Alfentanil + remifentanil > SA perioperative analgesia
Opioid Analgesics Neuroleptanesthesia >
[Morphine, Fentanyl, [fentanyl + butyrophenone
Sufentanil, Remifentanil] droperidol (Innovar)
2,6-diisoprophylphenol Used during maintenance of Effects: hypnosis, metabolic Propofol infusion syndrome
Most frequently anesthesia and is common acidosis, respiratory (metabolic acidosis)
administered drug for choice for sedation in the depression, hypotension,
induction of anesthesia and setting of monitored apnea
Propofol has largely replaced anesthesia care
barbiturates for this use Agent of choice for
ambulatory surgery

2
 Water soluble prodrug of
propofol
Fospropofol Metabolized by alkaline
phosphatase, producing
propofol, phosphate, and
formaldehyde
Carboxylated imidazole
An IV anesthetic with
Etomidate hypnotic but not analgesic
effects and is often chosen
for its minimal hemodynamic
effects
Arylcyclohexylamine
Blocks glutamic acid at
Ketamine NMDA receptor
Used for induction of
dissociative anesthesia
A highly selective a2-
adrenergic agonist
Dexmedetomidine Water soluble and available
as a parenteral formulation
Local Anesthetics: Amide derivative of xylidine
Amides: First amide in clinical practice
Has a rapid onset, which is
Lidocaine related to its tendency to
spread well to tissues
Amide derivative of xylidine
Mepivacaine
Amide derivative of toluidine
Highest clearance of the
Prilocaine aminoamide anesthetics,
imparting reduced risk of
systemic toxicity
4x more potent than
lidocaine but <4x as toxic
Bupivacaine AOC for epidural infusions
Available formulation: sterile,
aqueous, colorless, and clear
solution
Approved for sedation during
monitored anesthesia care
An alternative to propofol Dose-dependent inhibition of Pain on injection site,
and barbiturates for the 11-beta-hydroxylase myocardial contractility,
rapid IV induction of adrenocortical suppression
anesthesia, especially in
patients with compromised
myocardial contractility
DOC for induction of Useful premedication in Emergence phenomena,
anesthesia in children and mentally challenged and postop disorientation,
hypotensive patients uncooperative patients since sensory and perceptual
it can be administered in illusion and vivid dreams
multiple routes
Principally used for the short-
term sedation of intubated
and ventilated patients in an
ICU setting
Can be used intravenously to Transient neurologic
treat cardiac arrhythmias and symptoms
to depress laryngeal and
pharyngeal reflex
Not effective topically, but it
is for infiltration, nerve block
and regional anesthesia
Used for infiltration, block Hemoglobinuria,
and regional anesthesia methemoglobinemia (can be
treated with IV methylene
blue or ascorbic acid
Used for infiltration, block Major advantage: slow onset, Most cardiotoxic local
and regional anesthesia longest duration of action anesthetic
(<1.5 hours)
3
 used for postop pain control
and for labor analgesia
Poor blockade property Used for infiltration, nerve
because it produces block and epidural
Etidocaine differential block (more of Inverse differential block
motor blockade rather than
sensory blockade)
Most potent local anesthesia
Inhibits normal enzyme by
Dibucaine 80% and abnormal enzyme
by 20%
Most recent, long-acting local Popular choice for epidural
Ropivacaine anesthetic infusions for control of labor
and postop pain
Esters: Slow onset of action AOC in the management of
Rapidly metabolized in the an arterial spasm by
Procaine plasma to PABA and inadvertently intraarterial
diethylamino ethanol injection of basic solution
Fast onset, short-acting Useful for topical anesthesia
Chlorprocaine
Ester of PABA, long-acting
Use for spinal anesthesia
Tetracaine with a maximal dose of 20
mg
Ester of benzoic acid Topical anesthesia for ear,
Only local anesthetic that nose, and throat procedures
Cocaine causes definite where its intense
vasoconstriction vasoconstriction can serve to
Has high abuse or addiction reduce bleeding
potential
Dental anesthetic
Articaine
Topical use but has toxicity of Methemoglibinemia
Benzocaine methemoglobinemia
Lipid sink
Levobupivacaine Less cardiotoxic
Lidocaine and prilocaine can Commonly used in pediatrics
EMLA combine to form such a to anesthetize the skin prior

4
 mixture which is marketed as to venipuncture for IV
EMLA catheter replacement
Skeletal Muscle Prototype Causes initial depolarization May stimulate ganglionic Arrhythmias, hyperkalemia,
Relaxants: 2 Ach molecules linked end- resulting to transient muscle nicotinic Ach and cardiac transient increased
to-end contractions muscarinic Ach receptors intraabdominal, IOP, postop
Neuromuscular Blocking Placement of endotracheal Agonist at nicotinic Ach Depolarization is then muscle pain
Drugs: tube at start of anesthetic receptors especially at followed by repolarization
Depolarizing: procedure neuromuscular junctions that is also accompanied by
Succinylcholine Depolarizes paralysis
Nondepolarizing: Prototype Prevents depolarization by Prolonged relaxation for Histamine release,
Competitive antagonist at Ach, causes flaccid paralysis surgical procedures hypotension, prolonged
nAch receptors, especially at Can cause histamine release Superseded by newer apnea
d-Tubocurarine neuromuscular junctions with hypotension nondepolarizing agents
Weak block of cardiac
muscarinic Ach receptors
Hofmann elimination
Atracurium Metabolite is laudanosine
Doxacurium
Shortest DOA of all NMDR Hypotension, flushing,
Mivacurium but slower than bronchospasm
succinylcholine
Slight-to-moderate block of Moderate increase in HR and
Pancuronium muscarinic effects smaller increase in cardiac
output
Intermediate duration
Vecuronium Metabolized in the liver
Pipecuronium
Most rapid onset of 60-120 Like cisatracurium but slight Useful in patients with renal Like cisatracurium
seconds antimuscarinic effect impairment
Rocuronium Least potent NMDR
Fastest onset and shortest
DOA
Less dependent on hepatic Like tubocurarine but lacks Prolonged relaxation for Prolonged apnea but less
inactivation, produces less histamine release and surgical procedures toxic than atracurium
Cisatracurium laudanosine antimuscarinic effects Relaxation of respiratory
Less likely to release muscles to facilitate

5
 histamine mechanical ventilation in
intensive care unit (ICU)
Ultra short-acting
Gantacurium isoquinolone with very rapid
onset and short DOA
Slowly metabolized by the
liver
Laudanosine Longer elimination half-life
(150 min.)
Readily crosses BBB
Metocurine
Spasmolytic Drugs: Facilitates action of GABA in Produces sedation at doses Chronic spasm due to
the CNS > acts at GABAa required to reduce muscle cerebral palsy, stroke, spinal
synapses tone cord injury
Diazepam Central sedation Increases interneuron Acute spasm due to muscle
inhibition of primary motor injury
afferents in SC
p-chlorphenyl-GABA Agonist at GABAb receptors > Inhibits release of substance Impaired sternal ossification
orally active GABA-mimetic activation result in P (neurokinin-1) in the spinal and omphalocele,
agent hyperpolarization (probably cord > reduce pain in drowsiness, weakness,
GABAb agonist, facilitates secondary to potassium patients with spasticity increases seizure activity in
Baclofen spinal inhibition of motor conductance) Severe spasticity due to epileptic patients
neurons Pre- and postsynaptic cerebral palsy, MS, stroke
inhibition of motor output
Congener of clonidine Apha 2-adrenoceptor agonist Spasm due to MS, stroke, ALS Drowsiness, hypotension, dry
studied for its spasmolytic in the spinal cord mouth, asthenia, weakness,
Tizanidine actions Pre- and postsynaptic sedation
Significant a2-adrenoceptor inhibition of reflex motor
agonist effects output
Other Centrally Acting Antiepileptic drug
Spasmolytics: Spasmolytic agent in studies
involving patients with MS
Gabapentin
GABAa and GABAb agonist
Progabide Has active metabolites,
including GABA itself

6
 Inhibitory amino acid
neurotransmitter that
Glycine appears to possess
pharmacologic activity when
given orally
Readily passes the BBB
Newer drug for the tx of ALS
With spasm reducing effects
Idrocilamide possibly through inhibition of
glutamatergic transmission in
the CNS
Same as idrocilamide
Riluzole
Direct-acting muscle Direct-acting muscle relaxant Reduces smooth muscle RyR channel – plant alkaloid GMW, sedation, hepatitis,
relaxants: Hydrantoin derivative related strength by interfering with ryanodine combines with a muscle weakness
to phenytoin excitation-contraction receptor on the channel
DOC for malignant coupling in the muscle fibers protein thus releasing
Dantrolene hyperthermia Blocks calcium release in SM calcium
Spasm due to CP, SC injury,
MS
Ophthalmic purposes Flaccid paralysis Spasm due to CP, MS, Muscle weakness, falls
Local muscle spasm overactive bladder, migraine
Botulinum Toxin Cleaves fusion proteins in
nerve endings
Drugs Used to Treat Prototype Produces strong Reduction in hyperactive Strong antimuscarinic effects
Acute Local Muscle Structurally related to the antimuscarinic side effects > muscle reflexes
tricyclic antidepressants may cause significant Antimuscarinic effects
Spasm: Poorly understood inhibition sedation confusion, transient Acute spasm due to muscle
Cyclobenzaprine of muscle stretch reflex in visual hallucination injury
spinal cord Inflammation
Carisoprodol
Chlorphenesin
Chlorzoxazone
Metaxolone
Orphenadrine
7
Additional Drug: Antispasmodic drug Attractive choice for patients Reduction of myotonia Shock and anaphylactoid
Acts by relaxing both skeletal who require antispasmodic Improvement of circulation reactions, Steven Johnson
Eperisone muscles and vascular smooth therapy without reduction in Suppression of pain reflex syndrome
(Myonal) muscles alertness Improves dizziness and (oculomucocutaneous
tinnitus syndrome), toxic epidermal
Facilitates movement of the neurolysis
upper and lower extremities