Term
thiopental
(class, mechanism, advantage/disadvantage, indication, contraindication, adverse effects, pharmacokinetics) |
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Definition
Class: general anesthetic, intravenous
Mechanism: enhance GABA(A) receptor activity; rapid onset, terminated by redistribution
Advantages: anti-seizure activity Disadvantages: poor analgesia, little muscle relaxation
Indication: induction of anesthesia (rapid onset), neonates req. higher dose for induction
Contraindication: PORPHYRIA
Adverse effects: (decreased cerebral metabolism, decreased cerebral blood flow, decreased BP, depressed respiration)
Pharmacokinetics: CONTEXT-SENSTIVE HALF-LIFE, terminal half-life is substantially longer w/ continuous infusion |
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Term
propofol
(class, mechanism, advantage/disadvantage, indication, adverse effects, pharmacokinetics) |
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Definition
Class: intravenous general anesthetic
Mechanism: enhances GABA(A) receptor activity
Advantages: high degree of clearance (hepatic --> rapid recovery, less hangover than thiopental Disadvantages: poor analgesia, slight muscle relaxation
Indication: induction or maintenance anesthesia
Adverse effects: (decreased cerebral metabolism, decreased cerebral blood flow, decreased BP, depressed respiration), PAIN AT INJECTION, ABUSE POTENTIAL (anesthesiology residents)'
Pharmacokinetics: redistribution plays are role in action duration and half-life |
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Term
etomidate
(class, mechanism, advantage/disadvantage, indication, adverse effects) |
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Definition
Class: intravenous general anesthetic
Mechanism: enhance GABA(A) receptor activity
Advantages: rapid onset, cardio stable (use for patients who have risks if hypotensive) Disadvantage: poor analgesic
Indication: induction of anesthesia
Adverse effects: (decreased cerebral metabolism, decreased cerebral blood flow, depressed respiration), SIGNIFICANT NAUSEA/VOMITING, PROLONGED SUPPRESSION OF ADRENOCORTICAL STRESS RESPONSE (up to weeks post-operative) |
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Term
ketamine
(class, mechanism, advantage/disadvantage, indication, adverse effects, drug interaction) |
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Definition
Class: intravenous general anesthetic
Mechanism: blocks glutamate receptors
Advantages: increases BP, ANALGESIC, good for kids, amnesic dissociate state
Indication: alone for short procedures (maintenance), induction for longer procedures
Adverse effects: INCREASED cerebral blood flow, cataleptic state (muscle rigidity), emergence delirium (<16y/o usually), analog of PCP (hallucinogenic, abuse potential)
Drug interactions: potentiates affects of non-depolarizing muscle relaxants; w/ theophylline predisposes to seizures |
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Term
halothane
(IUSM know the adverse effects and pharmacokinetics) |
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Definition
Class: volatile general anesthetic
Advantage: bronchodilator, some skeletal muscle relaxation; VERY POTENT MAC 0.75% Disadvantage: high blood/gas coefficient (slow induction), weak analgesic
Adverse effects: liver toxicity (due to metabolite), MALIGNANT HYPERTHERMIA (esp. this halogenated GA)
Pharmacokinetics: significant hepatic metabolism to trifluroacetylchloride (hepatotoxic)
Special: discontinued in US |
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Term
enflurane
(IUSM know the adverse effects) |
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Definition
Class: volatile general anesthetic
MAC 1.6%
Advantages: bronchodilator, significant skeletal muscle relaxation Disadvantages: high blood/gas coefficient (slow induction)
Indication: induction (not much in US)
Adverse effect: SEIZURE ACTIVITY
Pharmacokinetics: 2-8% metabolized |
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Term
isoflurane
(class, advantage/disadvantage, MAC, indication, contraindication, adverse effects, pharmacokinetics) |
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Definition
Class: volatile general anesthetic
Advantage: low blood/gas coefficient, induction <10min, good muscle relaxant Disadvantages: pungent odor (not used for induction b/c of this)
MAC 1.2%
Indication: maintenance of anesthesia
Contraindication: CHD
Adverse effects: DILATES CORONARY ARTERIES (CORONARY STEAL), malignant hyperthermia, general halogenated GAs
Pharmacokinetics: eliminated unchanged in exhalation (>99%) |
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Term
Adverse effects of halogenated volatile GAs |
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Definition
tachycardia, peripheral vasodilation, hypotension, concentration dependent depression of ventilation, dilates cerebral arteries w/ possible increase in intracranial pressure |
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Term
sevoflurane
(class, advantage/disadvantage, MAC, indication, adverse effect, pharmacokinetic) |
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Definition
Class: volatile general anesthetic
Advantage: low blood gas coefficient (0.65), rapid onset, rapid recovery, potent bronchodilator, direct relax of skeletal muscle, NO TACHYCARDIA Disadvantage: expensive
MAC 2%
Indication: induction or maintenance of anesthesia; widely used for outpatient procedures and pediatrics
Adverse effects: PRODUCES NEPHROTOXIC COMPOUND A WITH RECIRCULATION, malignant hyperthermia, general halogenated GAs
Pharmacokinetics: 3% metabolized, organic fluoride as by-product |
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Term
desflurane
(class, advantage/disadvantage, MAC, indication, adverse effects, pharmacokinetics) |
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Definition
Class: volatile general anesthetic
Advatanges: LOWEST BLOOD/GAS COEFFICIENT (0.42), low fat solublility, very rapid onset, rapid changes and recovery (5-10min), bronchodilator, direct skeletal muscle relax Disadvantages: not very potent, expensive
MAC 6%
Indication: outpatient surgeries, maintenance only of anesthesia
Adverse effects: COUGH/SALIVATION/BRONCHOSPASM when awaken, STRONG AIRWAY IRRITANT (not used for induction), produces CO with recirculation (so don't recirculate), malignant hyperthermia, general halogenated AEs
Pharmacokinetics: <1% metabolized |
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Term
methoxyflurane
(IUSM know the adverse effects) |
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Definition
Class: volatile general anesthetic
DETRIMENTAL TO KIDNEYS - 65% metabolized to FLUORIDE IONS that are nephrotoxic |
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Term
nitrous oxide
(class, advantage/disadvantage, MAC, indication, contraindication, adverse effects, pharmacokinetics) |
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Definition
Class: volatile general anesthetic
Advantages: insoluble, significant analgesia Disadvantages: weak anesthetic and very low potency
MAC 105%
Indication: adjunct to other inhalation or intravenous anesthetic (NEVER ABOVE 80%)
Contraindication: PULMONARY HYPERTENSION
Adverse effects: BOWEL DISTENTION, PNEUMOTHORAX, INNER EAR PAIN, DIFFUSIONAL HYPOXIA (req. 100% post-operative), increased cerebral blood flow w/ potential increases in intracranial pressure
Pharmacokinetics: 99.9% eliminate unchanged in lungs |
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Term
order of nerves blocked for local anesthetics |
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Definition
pain (A-delta), autonomic C-fibers cold warmth touch deep pressure motor |
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Term
use-depedendent block of local anesthetics |
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Definition
the greater the rate of nerve stimulation the greater the ability of the LA to block the VG-gated sodium channel |
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Term
what determines time to onset of local anesthetics |
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Definition
pka of drug (pH of tissues determines drug access to intracellular compartment) |
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Term
what determines duration of local anesthetic |
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Definition
(contact time with nerve) affected by: drug absorption (site of injection, dosage, adjunct) drug distribution/redistribution (blood flow, ppb status, adjunct) drug elimination (ester hydrlosis or amide metabolism by liver) |
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Term
metabolism of ester LA vs. amide LA |
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Definition
ester - plasma cholinesterase amides - hepatic CYP450 system |
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Term
unique adverse effect of ester LAs |
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Definition
potential allergic reaction due to metabolite (para-amino benzoic acid) |
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Term
what determines the potency of a local anesthetic |
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Definition
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Term
patient characteristics of importance in local anesthetics |
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Definition
liver disease - don't use amides low esterase activity - don't use esters neonates - lower plasma proteins, higher sensitivity to drugs pregnancy - drugs more effective (??why??) patients w/ spinal cord disease - use in spine w/ caution, may be useful in fixed spinal cord injury |
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Term
uses of local anesthetics |
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Definition
1. local and regional anesthesia (topical, infiltration, intravenous) 2. peripheral nerve block 3. central nerve block 4. treatment of acute labor pain 5. analgesia in operative or post-op period 6. management of chronic pain (where local anesthetic may have prolonged effect) 7. aid in diagnosis and management prior to neurolytic procedures |
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Term
major adverse effects of anesthetics |
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Definition
1. CNS - stimulation (restlessness, tremor, convulsions), depression (drowsiness, sedation, respiratory failure)
2. CV - heart (dec. conduction/force of contraction/excitability), vascular smooth muscle relaxation (dec. BP)
3. Smooth muscle - decrease bowel and uterine contraction
4. hypersensitivity rxns - dermatitis, asthmatic attack
5. nausea - procaine 17%
6. methoglobinemia - prilocaine, benzocaine |
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Term
mechanism of action for local anesthetics |
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Definition
block VG-sodium channels from opening block generation of an AP at post-synaptic cell |
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Term
lidocaine (anesthetic)
(class, features) |
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Definition
Class: local anesthetic, amide type most popular doses producing CNS toxicity cause cardiovascular depression |
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Term
etidocaine
(class, features) |
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Definition
Class: local anesthetic, amide type BLOCKS MOTOR AND SENSORY ACTIVITY EQUALLY |
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Term
bupivacaine
(class, features) |
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Definition
Class: local anesthetic, amide type more cardiotoxic than lidocaine long-acting levo-bupivacaine = s-enantiomer |
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Term
ropivacaine
(class, features) |
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Definition
Class: local anesthetic, amide type less cardiotoxic than bupivacaine long-acting |
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Term
prilocaine
(class, features) |
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Definition
Class: local anesthetic, amide type methoglobinemia assoc. |
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Term
procaine
(class, features) |
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Definition
Class: local anesthetic, ester type slow onset, short duration metabolized to para-amino benzoic acid - potential allergic rxn |
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Term
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Definition
Class: local anesthetic, ester type blocks NE (catecholamine) uptake vasoconstrictor abuse potential used primarily in upper respiratory tract surgeries |
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Term
benzocaine
(class, features) |
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Definition
Class: local anesthetic, ester type low sobulility (low potency) MC topical agent methemobglobinemia assoc. |
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Term
tetracaine
(class, features) |
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Definition
Class: local anesthetic, ester type slower metabolism/more systemic toxicity assoc. |
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Term
topical local anesthetics |
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Definition
MC - benzocaine cocaine - ear, nose, throat only lidocaine lidocaine/prilocaine mixture - for 5mm depth (bridge between topical and infiltrative) |
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Term
infiltrative local anesthetics |
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Definition
intradermal or subq injection procaine - short duration lidocaine - intermediate duration bupivacaine - long duration |
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Term
intravenous local anesthetics |
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Definition
tourniquet-occluded limb (forearm and hand = MC) lidocaine w/o epi is most frequent agent |
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Term
peripheral nerve block local anesthetics |
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Definition
onset determined by: proximity, cocnetration, volume and ionization of drug to nerve lidocaine and bupivacaine MC |
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Term
central neural block local anesthetics |
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Definition
epidural or intrathecal vasodilation from sympathetic blockade BARICITY - determines direction of migration lidocaine shorter than bupivacaine < tetracaine |
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Term
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Definition
lidocaine, prilocaine, bupivacaine, ropivacaine |
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Term
spinal (intrathecal) agents |
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Definition
procaine, lidocaine, bupivacaine |
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Term
succinylcholine
(class, mechanism, onset, duration, elimination, special notes) |
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Definition
Class: neuromuscular blocker, depolarizing
Mechanism: binds nicotinic ACH receptors causing prolonged depolarization and paralysis; causes initial wave of fasciculation
Time to onset: 1-1.5 min Duration: 5-8 minutes
Elimination: hydrolysis by plasma esterases
Cholinesterase inhibitor effects: early on intensify blockade, later reverse blockade
Phase I - endplate depolarized Phase II - endplate partially repolarized |
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Term
d-Tubocurarine
(class, mechanism, duration, elimination) |
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Definition
Class: neuromuscular blocker, non-depolarizing, natural alkaloid
Mechanism: competitive antagonist at nicotinic receptor at NMJ; not orally active must be injected
Time to onset: 4-6min Duration: 80-120min (long)
Elimination: renal elimination, liver clearance |
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Term
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Definition
Class: neuromuscular blocker, non-depolarizing
Mechanism: competitive antagonist at nicotinic receptor at NMJ, nor orally active must be injected
Duration: 30-60 (intermediate)
Elimination: Hoffman, hydrolysis by esterases |
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Term
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Definition
Class: neuromuscular blocker, non-depolarizing
Mechanism: competitive antagonist at nicotinic receptor at NMJ, nor orally active must be injected
Duration: 80-100min (long)
Elimination: renal elimination |
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Term
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Definition
Class: neuromuscular blocker, non-depolarizing
Mechanism: competitive antagonist at nicotinic receptor at NMJ, nor orally active must be injected
Duration: 30-60min (intermediate)
Elimination: liver metabolism |
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Term
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Definition
Class: neuromuscular blocker, non-depolarizing
Mechanism: competitive antagonist at nicotinic receptor at NMJ, nor orally active must be injected
Duration: 60-90min (intermediate)
Elimination: liver metabolism, renal elimination |
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Term
non-depolarizing neuromuscular blocker adverse effects |
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Definition
GANGLION BLOCKADE: decreased BP (d-TC > pan > atra/veru) HISTAMINE RELEASE: decreased BP, bronchospasms, increased secretions (d-TC > atra >> pan/roc/veru) MUSCARINIC BLOCKADE: tachycardia (pan and veru) |
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Term
depolarizing neuromuscular blocker adverse effects |
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Definition
fsciculations myalgia hyperkalemia --> cardiac arrhythmias (esp. burn pts and soft-tissue injuries in paraplegics) prolonged paralysis with atypical peudocholinesterase activity MALIGNANT HYPERTHERMIA |
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Term
uses of neuromuscular blocker |
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Definition
major: surgical paralysis (NO ANALGESIC EFFECTS) |
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Term
sequence of paralysis in neuromuscular blockers |
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Definition
1. muscles of fine movement (fingers, eyes, jaw, larynx) 2. limbs 3. trunk 4. intercostal muscles 5. diaphragm - recovers first, breathing recovers first |
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Term
baclofen
(class, mechanism, indication, adverse effects, pharmacokinetics) |
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Definition
Class: skeletal muscle relaxant
Mechanism: GABA(A) receptor agonist, spinal cord action to prevent excitation to motor neurons presynpatically, maybe supraspinal CNS action
Indicatoin: spasticity asocc. w/ MS/spinal cord injury or disease; trigeminal neuralgia
Adverse effects: DROWSINESS, dizziness, lightheadedness, confusion, muscle weakness
Pharmacokinetics: oral and intrathecal admin, renal elimination |
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Term
dantrolene
(class, mechanism, indication, adverse effects, pharmacokinetics) |
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Definition
Class: skeletal muscle relaxant
Mechanism: inhibits calcium release from SR in muscles
Indication: malignant hyperthermia (reduce mortality from 80% to <10%)
Adverse effects: muscle weakness
Pharmacokinetics: oral or IV admin, hepatic metabolism |
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