Pharm 11 Anesthetics Flashcards
General Anesthetic definition
Loss of awareness, memory, and perception, not actual loss of sensation
Stage 1 of anesthesia
Analgesia
Stage 2
Excitement
Irregular respiration
Vomiting
Stage 3
Surgical
Regular respiration
Reflexes (eyelash) are abolished
Stage 4
Medullary depression
Need full circulatory and respiratory support
Speed of induction correlations:
- Gas concentration
- Pulmonary ventilation
- Blood solubility
- Pulmonary circulation
- A-V concentration gradient
- Direct
- Direct
- Inverse
- Inverse
- Inverse
Blood:gas partition coefficient
High solubility = high coefficient = slow induction
Redistribution
Gas solubility in other body tissues, important for determining elimination from the brain
Minimum Alveolar Concentration
Low MAC = High Potency
-Concentration that produces absence of response in 50% of patients
Elderly MAC
Lower than normal
Halothane effect on heart
Sensitization to catecholamines -> arrhythmias
Halothane effect on liver
Occasional severe hepatitis
Drug causing nephrotoxic effect
Methoxyflurane (due to inorganic fluoride release)
Effect on pregnancy
Increase in abortions, no mutations
-Thiopental-
Speed
Elimination
30s onset, 10m duration
Redistribution
-Thiopental-
Action
SE
Sedative (barbiturate), poor analgesia
Decrease HR (Hypotension) Decrease Resp
-Benzodiazepines-
Speed
Slower than Thiopental
-Benzodiazepines-
Action
SE
Sedative, no analgesia
Anterograde amnesia
Prolong recovery
-Narcotics-
Action
SE
Good analgesia, no anesthesia
Respiratory depression
-Ketamine-
Action
MOA
SE
Dissociative Anesthesia
NMDA antagonist
CV stimulation
Post-op illusions
-Propofol-
Action
Speed
Anestesia (most popular)
Anti-emetic
Fast
-Propofol-
SE
Respiratory depression
-Etomidate-
Action
SE
Rapid hypnotic
No analgesia
Nausea, Vomiting
-Promazine-
Adjunct
- Anti-emetic
- Sedation
-Promethazine-
Adjunct
- Anti-emetic
- Sedation
Local anesthetic basic action
Prevent pain by interruption nerve conduction
Local anesthetic specific action
Block voltage-gated sodium channels
Local anesthetic pH effects
Weak base
- Uncharged at body pH (for uptake)
- Cationic and higher pKa (for action)
Differential sensitivity
Attack fast firing channels (pain) first because Na channel needs to be open for action
Ester metabolism
Rapidly hydrolyzed in blood by pseudocholinesterase
Amide metabolism
Redistributed first, then hydrolyzed in liver by CYP450. Liver disease causes toxicity
Local anesthetic problem
Vasodilation leads to systemic absorption. Give with epinephrine
Lidocaine (amide) CNS effect
Drowsiness -> Activation -> Depression -> Respiratory failure
Local anesthetic CV problem
Decrease excitability -> antiarrhythmic
Epidural LA issues
Hypotension due to sympathetic blockade
Cocaine toxicity
Hypertensive vasoconstriction
Arrhythmias
LA hypersensitivity
Esters metabolized to PABA - some patients allergic
LA for burn patients
Benzocaine - hydrophobic, stays on wound
LA for arrhythmia
Lidocaine and Procainamide
-Cocaine- E/A Use action SE
Ester
Useful for vasoconstriction
Medium
Systemic toxicity
-Procaine- E/A Use action SE
Ester
Novicaine
Short
few
-Tetracaine- E/A Use action SE
Ester
Topical, spinal
Long
Toxic (lipophilic)
-Benzocaine- E/A Use action SE
Ester
Surface only (wounds)
surface only
surface only
-Lidocaine- E/A Use action SE
Amide
Patients with Ester Sensitivity, better than procaine
Medium
none
-Mepivacaine- E/A Use action SE
Amide
Obstetrics
Medium
neuro effects in baby
-Bupivacaine- E/A Use action SE
Amide Post-op nerve blocks, obstetric epidural Long Toxic (lipophilic) better for baby