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28 Cards in this Set
- Front
- Back
Short-acting NM blockers
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Succinylcholine
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Depolarizing NM blockers
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Succinylcholine
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Intermediate-acting NM blockers
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Rocuronium
Vecuronium Atracurium Cis-atracurium |
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Long-acting NM blockers
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Doxacurium
Pancuronium d-Tubocurare (curare) |
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Succinylcholine
a. Structure b. ED 95 c. Onset of action d. Duration of action e. Metabolism and excretion |
a. Two-linked acetylcholine molecules
b. n/a c. < 1-1.5 min after 1-1.5 mg/kg intubating dose d. 5-10 min after 1-1.5 mg/kg bolus e. Plasma cholinesterases |
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Rocuronium
a. Structure b. ED 95 c. Onset of action d. Duration of action e. Metabolism and excretion |
Intermediate-acting
a. Aminosteroid b. 259-305 mug/kg c. 90-110 sec after 570-850 mug/kg d. 2-45 min after 570-850 mug/kg e. No active metabolite Most drug excreted in bile. DOA not significantly changed in ESRF DOA increased in hepatic disease |
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Vecuronium
a. Structure b. ED 95 c. Onset of action d. Duration of action e. Metabolism and excretion |
Intermediate-acting
a. Aminosteroid b. 50 mug/kg c. 3-5 min after 0.06-0.10 mg/kg d. 20-35 min after 0.06-0.10 mg/kg e. Hepatic clearance accounts for 50% Renal clearance accounts for 25% NB: 3-desacetyl vecuronium in 70% as potent as vecuronium |
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Atracurium
a. Structure b. ED 95 c. Onset of action d. Duration of action e. Metabolism and excretion |
Intermediate-acting
a. Benzylisoquinoline b. 0.25 mg/kg c. 3-5 min after 2x ED95 d. 35-45 min after 2x ED95 e. Hoffman elimination (minor route => nonspecific esterases) NB: Laudanosine metabolite may accumulate in renal failure ?clinical relevance |
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Cis-atracurium
a. Structure b. ED 95 c. Onset of action d. Duration of action e. Metabolism and excretion |
Intermediate-acting
a. Benzylisoquinoline b. 0.05 mg/kg c. 4.6-5.8 min after 2x ED95 d. 33-45 min after 2x ED95 e. Hoffman elimination 77%; renal 16%; other organs 7% |
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Doxacurium
a. Structure b. ED 95 c. Onset of action d. Duration of action e. Metabolism and excretion |
Long-acting
a. Benzylisoquinoline b. 25-30 mug/kg c. 4.5 min after 40-60 mug/kg bolus d. 75-100 min after 40-60 mug/kg bolus e. Renal and hepatic DOA doubled in renal disease DOA mild increase in hepatic disease |
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Pancuronium
a. Structure b. ED 95 c. Onset of action d. Duration of action e. Metabolism and excretion |
Long-acting
a. Steroidal b. 0.06 mg/kg c. 3-4 min after 0.07-0.1 mg/kg bolus d. ~1.5 hrs after 0.07-0.1 mg/kg bolus e. Some taken up by liver 5-10% deacetylated to form OH-metabolites Mostly excreted unchanged in urine Clearance reduced in hepatic, renal disease and in elderly |
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d-Tubocurare
a. Structure b. ED 95 c. Onset of action d. Duration of action e. Metabolism and excretion |
Long-acting
a. Naturally occurring b. 0.5 mg/kg c. 5 min after 0.5 mg/kg bolus d. > 1.5 hrs after 0.5-0.6 mg/kg bolus e. No active metabolites Most eliminated unchanged in urine 12% in bile DOA increased with renal failure and minimal increase with hepatic failure |
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Succinylcholine: Advantages/Disadvantages
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Rapid onset
Elevated K+; increased w/ 1. Sepsis 2. Recent burns 3. Trauma 4. UMN/LMN diseases Muscle pain Myoglobinuria Bradycardia secondary to vagal activity |
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Hyperkalemia a/w succinylcholine increased with...
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1. Sepsis
2. Recent burns 3. Trauma 4. UMN/LMN diseases |
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Rocuronium: Advantages/Disadvantages
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Rapid onset of NMB
Hemodynamic stability |
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Vecuronium: Advantages/Disadvantages
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Hemodynamic stability
Most frequently a/w prolonged NMB |
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Most frequently a/w prolonged NMB
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Vecuronium
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Atracurium: Advantages/Disadvantages
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Histamine release w/rapid bolus of 2x ED95
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Cis-atracurium: Advantages/Disadvantages
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Hemodynamic stability
Little-to-no histamine release w/conventional doses |
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Doxacurium: Advantages/Disadvantages
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Hemodynamic stability
Little-to-no histamine release w/conventional doses |
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Pancuronium: Advantages/Disadvantages
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May cause tachycardia particularly w/bolus dose
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d-Tubocurare (curare): Advantages/Disadvantages
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Hypotension w/bolus dose secondary to ganglion blockade and histamine release
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Lorazepam
a. Potency b. Half-life c. Solubility d. Metabolism and excretion e. Factors affecting pharmokinetics |
Intermediate-acting
a. 5 times more potent than diazepam b. 14 hours c. Increased water-solubility => reduces volume of distribution & serum elimination half-life d. Hepatic glucouronidation => inactive metabolites (75% excreted in urine as glucuronide) 1. Little effect by hepatic disease/CYP450 modulators 2. Prolonged half-life with renal disease e. No significant alteration in elderly or critically ill |
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Midazolam
a. Potency b. Half-life c. Solubility d. Metabolism and excretion |
a. 3 times as potent as diazepam
b. 2-3 hours c. At physiologic pH, ring closes => increased lipophilicity => rapid CNS penetration & redistribution d. Hepatic oxidation to hydroxymidazolam Clearance reduced by concurrent use of CCB, EES, triazole antifungal agents |
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Diazepam
a. Potency b. Half-life c. Solubility d. Metabolism and excretion |
a. N/A
b. 20-40 hours c. Highly lipophilic d. Hepatic metabolism to oxazepam and desmethyldiazepam |
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Half-life of desmethyldiazepam...
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96 hours
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Short-acting benzodiazepines w/no active metabolites
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Oxazepam
Temazepam |
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Propofol
a. MOA b. Distribution half-life c. Elimination half-life d. Solubility e. Metabolism and excretion f. Factors affecting clearance/elimination |
a. Appears to be modulation GABA-A receptor
b. 2-8 hours c. Up to 7 hours d. Highly lipid-soluble e. Mysterious Sulfate & glucuronide conjugate or hydroxylated metabolited excreted in urine Clearance exceeds hepatic blood flow (?extrahepatic metabolic route?) f. Unchanged elimination a/w hepatic/renal disease Decreased elimination a/w geriatrics |