Anesthesia PHARMACOLOGY

Dr. Christopher Rey Dacanay, RPh, MD PHYSICIAN LICENSURE EXAM

OUTLINE ○ CV ________________
○ Smooth muscle relaxation → vessel dilatation → _ BP
I. Anesthesia 1
Ii. General Anesthesia 1 B. PRINCIPLES OF GENERAL ANESTHESIA
A. Generalities of General Anesthesia 1 ● Lipophilicity
B. Principles of General Anesthesia 1
○ __ Lipophilicity → __ ability to cross neuronal membranes →
C. Inhaled General Anesthetics 1
D. Intravenous General Anesthetics 2 __ potency
Iii. Local Anesthetics 2 ● Mean Alveolar Concentration
A. Physiology of Sensation 2 ○ Concentration of anesthetic agent that would bring effect (i.e.
B. Generalities of Local Anesthesia 2 prevent movement) in 50% of the patients
C. Local Anesthetic Agents 3 ○ Inversely proportional to potency
B. ADRs of Local Anesthesia 3

I. ANESTHESIA
PO
Anesthesia VS. Analgesia
● Analgesia
○ Loss of pain
MATE
● Anesthesia
○ Loss of pain + consciousness, reflexes, memory C NC
Stages of Anesthesia Y
Stage Feature ● Blood/Gas Partition Coefficient (α)
○ Ostwald coefficient
Patient is awake ○ Compares amount of drug in 1mL of blood to amount of drug
Amnesia in 1mL of alveolar gas
I: Analgesia
Which type of amnesia? ○ Measurement of __________ of the anesthetic agent
________________
○ ↑ Blood/Gas coefficient → ↑ solubility of anesthetic agent
Hyperactivity
II. Excitation and Irregularity of Vital Signs
Delirium ________________
________________
III. Surgical Anesthesia Regular RR
Depression of medulla
IV. Respiratory Cessation of
Depression ________________
Coma and death

Types of Anesthesia
1. General anesthesia
2. Local anesthesia
● Respiratory Rate
II. GENERAL ANESTHESIA ○ ↑ RR → _______ onset of action
A. GENERALITIES OF GENERAL ANESTHESIA C. INHALED GENERAL ANESTHETICS
● Site of Action: Central Nervous System
Inhaled
● Concentration is measured in Partial Pressure Must-knows
Anesthetic
○ The higher the partial pressure, the faster the onset
Fastest onset but least potent
● Potency is measured by Mean Alveolar Concentration ADRs:
● Onset of action depends on (2): Nitrous oxide Coughing
○ ________________ Respiratory irritation
○ ________________ Laughing

● Types of General Anesthesia: Halothane Hepatotoxic

Inhalational Intravenous Causes bronchoconstriction
DesFLURANE
Nitrous Oxide CI: ________________
Halothane Propofol Stimulates release of catecholamines
DesFLURANE Thiopental IsoFLURANE
CI: ________________
IsoFLURANE Midazolam
EnFLURANE Ketamine DesFLURANE
Cause ________________
SevoFLURANE IsoFLURANE
MethoxyFLURANE All FLURANES
MOA DesFLURANE
○ _ GABA IsoFLURANE
ADR: ________________
○ _ Glutamate EnFLURANE
ADR SevoFLURANE
○ CNS ________________ MethoxyFLURA
○ Respiratory ________________ NE

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MethoxyFLURA
Slow onset but most potent B Preganglionic autonomic <3 3 -15
NE

D. INTRAVENOUS GENERAL ANESTHETICS Thermal pain, slow pain,

Intravenous anesthetics have a faster onset so they are used C 0.4 - 1.2 0.5 - 2
for ____________ of anesthesia mechanoreceptor

Intravenous Postganglionic autonomic 0.3 - 1.3 0.7 - 2.3

Must-knows
Anesthetic
aka “Milk of amnesia”
Short acting, fast onset
MOA: Increases GABA-mediated inhibition
Propofol ADRs:
CNS Depression
CV Depression
________________

Ultra-short acting barbiturate

Thiopental MOA: Enhance GABA-mediated Cl channel
opening by increasing ________ of opening of the
channel

Benzodiazepine
Midazolam MOA: Enhance GABA-mediated Cl channel opening
by increasing ___________ of opening of the
channel
NMDA (N-Methyl-D-aspartate) antagonist
Only anesthetic agent which causes increase in BP
Ketamine
or CV ________________
ADR: ________________

Malignant Hyperthermia
● Peculiar ADR after administration of anesthetic
● Not dose related
● Symptoms:
○ High fever
○ Rigidity of muscles
○ Acidosis
● May occur with any muscle relaxant but occurs more commonly
with succinylcholine
● Management
○ DOC: ________________ (muscle relaxant)
■ MOA: Calcium channel blocker

PREVIOUS BOARD EXAM RECALL

1. Droperidol + Fentanyl?
2. Droperidol + Fentanyl + NO2?

Answers given in the lecture video.

III. LOCAL ANESTHETICS

A. PHYSIOLOGY OF SENSATION
● Sensation is an ascending pathway
● Smaller fibers get blocked first
○ Smaller fiber diameter = faster blocking
Table 4. Nerve Fiber Types
Diamet
Fiber CV
Function er
type (m/s)
(mu)

α Proprioception, somatomotor 12 - 20 100

β Touch, pressure 5 - 12 30-70

A
γ Motor to muscle spindle 3-6 15-30

Fast Pain, esp to cold,

δ 2-5 12 - 30
touch

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Pain Pathway

Dorsal Horn Gating

B. GENERALITIES OF LOCAL ANESTHESIA

● Site of Action: Site of administration
○ Local effect (area of application)
● Remove sensation
● All are ambiphilic
○ Substances with both a polar and nonpolar end

AMIN EST AROM

ER
O ATIC
POLAR NON-
END POLAR
END

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● All are weak bases

○ To make it more absorbable, put it in a ________________
medium → non-ionic/ lipid soluble
● All are Na channel blockers
○ Blocking Na channels → no depolarization → No AP → no
sensation
● With the EXCEPTION of COCAINE:
○ All are synthetic
○ All are vasodilators
○ All are CNS/CVS depressants

Ways of Administration of Local Anesthetics

1. Infiltration
2. Nerve Block
3. Regional Anesthesia

Pharmacokinetics
● Esters
○ Degraded by plasma esterase
● Amides
○ Degraded by hepatic amidase
Which has a shorter duration of action? ________________

C. LOCAL ANESTHETIC AGENTS

Table 2. Local Anesthetic agents
________________ ________________
Procaine Lidocaine
Tetracaine Prilocaine
Cocaine Etidocaine
Benzocaine Mepivacaine

EMLA (Eutectic Mixture of Local Anesthetics)

● Components
○ ________________ + ________________

Local Anesthetic Must-knows

Prilocaine ADR: Methemoglobinemia
ADR: ________________
Bupivacaine Most commonly used local anesthetic for
pregnant patients
Etidocaine Long Acting
Mepivacaine Amide

D. ADVERSE DRUG REACTIONS OF LOCAL ANESTHESIA

CNS Effects
● CNS depression
● Tremors
● Nausea
● Confusion

CVS Effects
● __ Cardiac output
● __ Heart rate
● __ Blood pressure

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