Pharmacology Reviewer  RENAL AND HEPATIC- can

interfere in the metabolism and

Chapter 27: General and excretion of the body which
Local Anesthetic Agents can lead to delayed absorption
of anesthesia
Two types of Anesthesia:
BALANCED ANESTHESIA
 General- loss of pain and
- therapeutic effects needs to be
consciosness
balanced with potential adverse
 Local- loss of pain in a
effects// given before general
designated area without
anesthetics and/or during
systemic effects
- example is the NMJ
GENERAL ANESTHESIA BLOCKER (stop muscle
activity and is a rapid acting IV
- it blocks body reflexes which
anesthetics)
prevents involuntary reflex
response that can injure the Involves following agents:
body and can prevent jerking
 Preoperative- aims to decrease
movements during a surgery.
secretion and prevent
Has following goals: bradychardia associated with
renal depression
 Analgesia- loss of pain
perception  Sedative Hypnotics- relaxes
patients, facilitates amnesia and
 Unconsciousness- loss of
sympathetic stimulation
awareness
 Antiemetics- decreases nausea
 Amnesia- inability to recall
and vomiting associated with
what happened
slowing of GI activity
RISK FACTORS:  Antihistamine- decreases
 CNS FACTORS- risk for allergic rx and dries up
abnormal rx to CNS depressing secretion
and relaxing effect  Narcotics- facilitates analgesia
 CV- risk for inadequate blood and sedation
supply
 RESPI- can complicate
delivery of gas anesthetics
STAGES/ DEPTHS OF consciousness, movement and
ANESTHESIA ability to communicate occurs
 Stage 1/ Analgesia Stage- loss
of pain sensation, patient still GENERAL ANESTHETIC
unconscious but able to AGENTS
communicate
 Stage 2/ Excitement Stage- e.g. Barbiturate, nonbarbiturate
period of excitement, termed as anesthetics, gas anesthetics and
a combative behavior, volatile liquids
stimulates tachycardia, increase BARBITURATE
of respiration and change in the
Blood Pressure THERAPEUTIC ACTIONS AND
 Stage 3/ Surgical Anesthesia- INDICATIONS
relaxation of skeletal muscles,  Thiopental (Pentothal)- most
return of regular respiration, widely used IV anesthetics. No
pupil dilation, progressive loss analgesic properties. May need
of eye reflexes; stage where additional analgesics after
surgery can be performed surgery.
 Stage 4/ Medullary Paralysis- Methohexital (Brevital)- lacks
Medulla Oblongata which analgesic property. May
controls the vital fx of the require postoperative
body: termed as a crucial stage analgesics.
for the patient due to possible
occurrence of death PHARMACOKINETICS

PHASES OF ANESHESIA  Thiopental- very rapid onset

usually within 10-30 secs.
 Induction- starts at the Ultrashort recovery period of 5-
beginning of stage 1 to stage 3, 8 mins.
e.g. NMJ Blocker + general  Methohexital- rapid onset.
anesthetics Recovery period of 3-4 mins.
 Maintenance- from stage 3
until it is completed, slower Lipophilic. Dissolved in water and
more predicatble phase, e.g. gas diffuse to brain rapidly
anesthetics
 Recovery- discontinuation of
CONTRAINDICATIONS AND
anesthetic until regained
CAUSES
Methohexital cannot come into metronidazole, quinidine,
contact with silicone like rubber carbamazepine.
stopper and disposable syringe due to
Barbiturate Anesthetics +
easy break down of silicone.
Narcotics= apnea more commonly
Methohexital and Thiopental should than occurs with other analgesics.
not be used until medical staffs are
ready and equipped for intubation and
NON BARBITURATE
respiratory support. Because of the Midazolam (Versea)
rapid onset of drug that can cause Doperidol (Inapsine)
respi depression and apnea
Etominadole (Amidate)
Pregnancy and Lactating. Should
Fospropofol (Lusedra)
not be used unless it clearly
outweighs the potential fetal risk. Ketamine (Keralar)
Because of CNS depressive effects Propofol (Diprivan)
ADVERSE EFFECTS THERAPEUTIC ACTIONS AND
Related to suppression of CNS with: INDICATIONS

-decreased pulse  Midazolam- Prototype. Very

potent amnesiac. Acts in
-hypotension reticular activating system and
-suppressed respiration limbic system to potentiate
effects of gamma amino butyric
-Decreased GI activity acid. Widely used to produce
-Nausea and vomiting: amnesia or sedation, induce
common after recovery anesthesia and for continuous
sedation for intubated and
DRUG TO DRUG mechanically ventilated
INTERACTIONS patients
Cannot be used with any other CNS  Doperidol- produces marked
suppressants. sedation and a state of mental
detachment. Has antiemetic
Barbiturates can cause decreased
effects, reducing the nausea and
effectiveness of theophylline, oral
vomiting in surgical in
anticoagulants, beta-blockers,
diagnostic procedure.
corticosteroids, hormonal
 Etomidate- general anesthetic,
contraceptives, phenylbutazones,
sometimes used to sedate
 patients receiving mechanical Propofol- very short acting
ventilation. anesthetic. 30-60 secs onset.
 Fospropofol- Monitored CONTRAINDICATIONS AND
sedation during therapeutic and CAUSES
diagnostic procedure. Will be
very relaxed and amnesic. Midazolam- cause nausea and
 Ketamine- associated with vomiting, used with caution who
bizarre state of could compromised by vomiting.
unconsciousness- awake but Associated with respiratory
unconscious and can’t feel depression and respiratory arrest. Life
pain. Causes sympathetic support should be ready and available.
stimulation with increase in bp Droperidol- used with cautions with
and heart rate- may be helpful renal and hepatic failure. Used with
in situations when cardiac extreme care w/ prolonged QT
depression is dangerous. interval or who’s at risk for it.
Propofol- Short procedures- very Etomidate- Not recommended for
rapid clearance, muchless of a children younger than 10 yrs. of age.
hangover effect, allows quick
recovery, maintain on mechanical Fospropofol- causes marked
ventilation relaxation and amnesia. Should not be
permitted to drive after use of drug.
PHARMACOKINETICS
ADVERSE EFFECTS
Midazolam- Rapid onset. Does not
reach peak effectiveness to 30-60  Risk for skin breakdown (not
mins. be able to move)
 Decubitus ulcer formation
Droperidol- 3 mins. onset. Ultrashort
 Midazolam- Respiratory
recovery time.
Depression and CNS
Etomidate- 1 min onset. 3-5 min suppression.
recovery period.
During recovery…
Fospropofol- Rapid onset. Peaks
 Droperidol may cause
within -13 mins-half life of nearly an
hypotension, chills,
hour. Slow recovery period.
hallucinations and drowsiness,
Ketamine- 30 secs onset. 5mins QT prolongation (puts at risk to
recovery period. cardiac arrythmmias)
  Etomidate- myoclonic and
tonic movements, nausea and GAS
vomiting
 Ketamine- crosses the blood • Inhaled drugs; enters the
brain barrier. Hallucinations, bronchi and alveoli rapidly
dreams and psychotic episodes. passes in capillary system, to
 Propofol- local burning on heart pumped to the body.
injection, bradychardia, • Very high affinity to fatty
hypotension, pulmonary edema. tissues. Lipophilic, includes
 Fospropofol- sensation of lipid membrane of the nerves in
perinial burning, stinging, CNS.
tingling and rash- usually
mild,lasting over a short time, • Gas passes quickly to the brain
don’t req. intervention but causing CNS depression. In
patient should be alerted that stage 3, regulates amount,
this occur and will pass. ensures it is sufficient to keep
unconscious but not cause
DRUG TO DRUG severe CNS depression
INTERACTIONS
• Decreasing the concentration of
Ketamine + Halothane= severe gas that flows into the bronchi,
cardiac depression with hypotension creating a concentration
and bradychardia. gradient= results in movement
X = Droperidol + drugs that of gas in opp direction.- out of
prolong QT interval the tissues and back to expired
air.
Ketamine- can potentiate muscular
blocking of NMJ blockers, may • Once the best way to achieve
require prolonged periods of anesthesia, but very flammable
respiratory support. and associated with toxic
adverse effect. Newer agents
Midazolam + Inhaled anesthetics, with less toxicity has replaced
CNS Depressants, Narcotics, the drug. Nitrous oxide (blue
propofol, thiopental = increased cylinder) is still used
toxicity and length of recovery
THERAPEUTIC ACTIONS • Acute sinus and middle ear
AND INDICATIONS pain, bowel obstruction,
pneumothorax
• Nitrous oxide- Very potent
analgesic- used freq for dental • Inactivates vit b12
surgery. Moves quickly in and (neurological immune and
out- hematological complications)
• Doesn’t cause muscle DRUG TO DRUG
relaxation. Usually combined INTERACTIONS
with other agents for anesthetic
• Caution- combined with other
use.
drug that causes CNS
PHARMACOKINETICS depression.
• Nitrous oxide- 1 -2 min onset • Halothane and ketamine=
of action. Rapid recovery severe cardiac arrest with
period. Timing of recovery hypotension and bradycardia.
depends on other drug being
VOLATILE
used.
Halothane (Fluothane)
CONTRAINDICATIONS AND Pesflurane (Suprane)
CAUSES Eflurane (Ethrane)
Isoflurane (Forane)
• Nitrous oxide can block the Sevoflurane (Ultane)
reuptake of oxygen after • Liquids that are unstable at
surgery and cause hypoxia. Due room temp and release gases.
to this, its always given in
combination with oxygen. • Acts like gas anesthetics

• Pregnancy. Not be used unless • Inhaled anesthetics can be

benefits clearly outweighs the volatile liquids
potential risk to fetus. THERAPEUTIC ACTIONS AND
• Nursing mothers. Should wait INDICATIONS
for 4hrs before nursing a baby • Halothane- prototype of
when they have been volatile liquids. Used as a
administered nitrous oxide maintenance of anesthesia.
ADVERSE EFFECTS Effective as an induction agent.

• Skin integrity
 • Desflurane- widely used in recommended in induction with
outpatient surgery (rapid onset pediatric patients
and quick recovery time)
• Enflurane- avoidance with
• Isoflurane- widely used to known cardiac or respiratory
maintain anesthesia after disease or renal dysfunction
induction. Can cause muscle
• Isoflurane and Sevoflurane-
relaxation.
be used with caution with
• Sevoflurane- used in outpatient respiratory depression
surgery as an induction agent
All of the drugs has potential to
and is rapidly cleared for quick
trigger malignant hyperthermia
recovery.
and never used with high risk
PHARMACOKINETICS developing it. Dantrolene should
be available.
• Halothane- rapid; 1-2 mins
onset. 20 min recovery. • Pregnancy and lactating.
Metabolized in liver Should be avoided unless the
benefit clearly outweighs the
• Desflurane, enflurane and
risk of fetus.
isoflurane- 1-2 min onset. 5-20
min recovery. ADVERSE EFFECTS
• Sevoflurane- newest of volatile • Halothane- recovery
liquids. 30 sec onset. 10 min syndrome characterized by
clearance. fever, anorexia, nausea,
vomiting , hepatitis which can
These drugs are all cleared
lead to fatal hepatic necrosis-
through the lungs.
rare. Should not be used freq
CONTRAINDICATIONS AND more than 3 weeks.
CAUSES
• Desflurane- collection of
• Halothane- avoidance with respiratory reactions (cough,
hepatic impairment. Associated increased secretion,
with bradycardia and larnygospasm)
hypotension.
• Isoflurane- hypotension,
• Desflurane- avoidance with hypercapnia, muscle soreness,
respiratory problems and with and a bad taste in mouth.
increased sensitivity. Not
• Enflurane- renal impairment
 • Sevoflurane- adverse effects More potential for adverse effects
are thought to be minimal
Types of nerve blocks:
DRUG TO DRUG
PERIPHERAL- blockage of sensory
INTERACTIONS
and motor aspects of a part of nerve
• Caution when any other drug is for relief of pain
combined with other CNS
CENTRAL- roots of nerves in spinal
suppressants
cord
LOCAL ANESTHESIA EPIDURAL- epidural word itself
TOPICAL- Includes application of means spaces where nerves emerge
lotion, cream, ointment or drop of from the spinal cord, typically used in
local anesthetic to traumatized skin to obstetric area
relieve pain. CAUDAL- sacral anal epidural
Involve application to the mucous SPINAL- spinal subarachnoid spaces
membranes.
IV REGIONAL ANESTHESIA-
INFILTRATION- Involves injecting Carefully draining all of the blood
the anesthetic directly to the tissues to from patient’s arm or leg
be treated
Securing a tourniquet to prevent
FIELD BLOCK- Injecting the anesthetic from entering the general
anesthetic all around the area that will circulation, injecting anesthetic into
be affected by the procedure or the vein of the arm or leg.
surgery.
This technique is used for very
• More intense than infiltration specific surgical procedures
anesthesia
LOCAL ANESTHETIC AGENTS
• Often used for tooth extraction
• Used to prevent from feeling
NERVEBLOCK - Involves injecting pain for varying periods of
anesthetic at some point along the time.
nerve or nerves that run to and from
the region in which the loss of pain • Works by causing a temporary
sensation or muscle paralysis is interruption in production and
desired. conduction of nerve impulses.
• In increasing concentrations,
local anesthetic can also cause
 loss of: (1) temperature, (2) • Shock
touch, (3) proprioception, (4) • Decreased plasma esterases
skeletal muscle tone. • Pregnancy and lactating. Can
be used only if the benefit
• Powerful nerve blockers,
outweighs potential risk to
effects be limited to particular
fetus.
body area
ADVERSE EFFECTS
• Should not be absorbed • Local blocking of sensation,
systemically loss of skin integrity,
• Classifies as esters or amides. • CNS EFFECTS: headache,
restlessness, anxiety, dizziness,
THERAPEUTIC ACTIONS AND tremors, blurred vision,
INDICATIONS backaches
• Helps increase effectiveness by • GI EFFECTS: nausea,
delivering it directly to the vomiting,
affected area. • CARDIOVASCULAR
EFFECTS: peripheral
• Indicated for infiltration vasodilation, myocardial
anesthesia, peripheral nerve depression, arrhythmias
block, spinal anesthetic, and the • BP changes
relief of local pain • can lead to fatal cardiac arrest
PHARMACOKINETICS and respiratory arrest
DRUG TO DRUG
• Ester Local Anesthetics INTERACTIONS
broken down immediately in • Local anesthetics +
the plasma by enzymes. Succinylcholine = increased
(plasma esterases) and prolonged neuro muscular
• Amide Local Anesthetics blockage.
metabolized more slowly in the • Local anesthetics +
liver. Can possible lead to Epinephrine = less risk of
toxicity systemic absorption, increased
local effects

CONTRAINDICATIONS AND Definition of terms

CAUSES
• History of allergies
• Heartblock
 Gamma amino butyric acid-
promotes lean muscle growth,
burning fat, stabilizing BP
 QT Interval- time of
ventricular activity from both
depolarization to repolarization,
from QRS complex to end of T
wave/ .44 sec or 40 milisec
 Decubitus ulcer- bedsores,
injury to skin and underlysing
tissue due to prolonged
pressure
 Neuromuscular Junction
Blocker- Blocks activity of
muscle and is a rapid acting IV
anesthetic
 Depressants- reducing or
diminishing the function or
activity