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124 Cards in this Set
- Front
- Back
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Give example of ultra-short acting NMBD and duration of action.
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Succinylcholine - 5-10 min.
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Give example of a short-acting NMBD.
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n/a
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Give examples of intermediate acting NMBD and duration of action.
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atracurium
cisatracurium vecuronium rocuronium 30-60 min |
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Give example of a long-acting NMBD.
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pancuronium
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What is the chemical structure of the 'curiums?
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benzylisoquinolines
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What is the chemical structure of 'roniums?
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steroidal
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What is the Hz of single twitch test? TOF? Double-burst? Tetanus? Posttenanic Count?
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Single - 0.1-1.0
TOF - 2 Double Burst - 50 Tetanus - 30,50, or 100 Posttetanic - 50 for 5 sec, 3 sec pause, single twitches of 1Hz |
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Which twitch test requires baseline before drug admin?
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single twitch
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Which test is easier to detect fade than TOF?
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double burst
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Which test tells how much over 100% paralyzed they are?
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posttetanic count
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Regarding posttetanice count - the higher the number, the ____ paralyzed they are.
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less
0= really paralyzed 7-8 = about ready to recover |
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time from drug administration to maximum effect...
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onset time
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time from drug administration to 25% recovery of twitch responses...
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clinical duration
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time from drug administration to 90% recovery of twitch response...
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total duration of action
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compares 4th twitch of TOF to 1st twitch, and when 4th twitch is 90% of 1st = recovery indicated.
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TOF ratio
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If patient has 4 twitches, but TOF ratio is _____, they are still 70% blocked.
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<90%
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Which site is best for onset?
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orbicularis oculi (facial nerve stimulated)
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Which site is best for offset?
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adductor policis (ulnar nerve)
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What is the sequence of onset for muscle paralysis and recovery?
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eye lids
extremities chest abdominal muscles diaphragm (recovery in opposite order) |
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4 twitches = _____ block or less
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70%
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4 twiches = ______ block (TOFR > 90%)
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70-75%
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3 twitches = _______ block
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75-80%
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2 twitches = ________block
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80-85%
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1 twitch = _______ block
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90-95%
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0 twitch = _____ block
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100%
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Does succ have a fade when testing twitches?
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No, everything goes out and comes back together.
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Describe Phase I block
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-Depolarizing (succ)
-muscle fasciculations precede onset of block -abscence of posttenatic potentiation -block potentiated by anticholinesterse drugs |
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Describe Phase II block
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-nondepolarizing
-no fasciculations -reverse with anticholinesterase drugs |
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Phase II block can occur with OD and desensitization with succ at doses > ____
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6mg/kg
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Tests for recovery from blockade that reveal 80% receptors still occupied:
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Tidal Volume 5ml/kg
Single Twitch Strength (75-80%) |
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Tests for recovery that reveal 70% receptors still occupied:
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-TOF
-sustained tetanus 50 Hz 5sec -vital capacity -double burst (60-70%) |
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Tests for recovery that reveal 50% receptors still occupied:
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-sustained tetanus at 100Hz
-inspiratory force 40cmH20 -head lift 5 seconds -hand grip -sustained bite |
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Which drugs are broken down by pseudocholinesterase?
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succinylcholine, ester LA, neostigmine, edrophonium
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Which drugs are broken down by non-specific esterases?
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atracurium, cisatracurium, remifentanil, clevidipine, etomidate
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Which drugs are broken down by RBC esterases?
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esmolol
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low dibucaine # + normal activity =
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atypical enzyme
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normal dibucaine # + low activity =
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normal enzyme with low levels present
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low dibucaine # + low activity =
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atypical enzyme with low levels present
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normal dibucaine # + normal activity =
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normal enzyme and amount
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above ____ normal activity = good
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60%
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What is the 100% safe cure for prolonged blockade?
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sedate, ventilate, and wait
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What are the side effects of succinylcholine?
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- hyperkalemia
-dysrhythmias -myalgia -myoglobinemia -increased gastric pressure -increased ICP -increased IOP -MH -masseter spasm |
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How are the 'curiums eliminated?
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Hoffman elimination + nonspecific esterases (nonorgan dependent)
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How is rocuronium eliminated?
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renal; hepatic
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How is vecuronium eliminated?
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renal 20-30%; hepatic 40-80%
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How is pancuronium eliminated?
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primarily renal; some hepatic
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How is succ eliminated?
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plasma cholinesterase
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What are the effects when H1 is stimulated?
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- inc cap perm
-bronchoconstriction -intestinal contraction - neg dromotropic |
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What are the effects when H2 is stimulated?
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-inc gastric acid
-systemic/cerebral vasodilation - pos inotropic and dromotropic |
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What are two agents that release histamine?
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atracurium (major) and succ (minor)
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What are the cardiac effects of atracurium?
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histamine release -- decreased BP and increased HR
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What are the cardiac effects of pancuronium?
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vagolytic and indirect sympathomimetic - increased HR
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What are the cardiac effects of succ?
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slight tachycardia
repeat doses = bradycardia |
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What are factors that prolong paralysis?
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hypokalemia, hypocalcemia, hypothermia
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Drugs that prolong paralysis?
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CCB, BB, lasix, steroids, IHA, lithium, mag sulfate, dantrolene
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Antibiotics that prolong paralysis?
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aminoglycosides, polymixin B, clindamycin, tetracycline
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What is MOA of neostigmine?
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inhibits cholinesterase breakdown of Ach - increases circulating Ach that competitively binds to both nicotinic and muscarinic receptors
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What is MOA of robinul?
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binds muscarinic receptors prohibiting parasymp response
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What are some side effects of neostigmine?
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bronchospasm, increased secretions, bradycardia
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What is max dose of neostigmine?
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5mg
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What is max dose of edrophonium? And what do you give with it?
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1mg/kg
atropine |
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Succ is only NMBD that is an agonist and ______?
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antagonist
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Which drug with increase arousal d/t incr Ach in brain d/t crossing BBB?
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physiostigmine
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If you have a TOF 2-3 twitches, how long will recovery take with intmd acting drugs? long acting?
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4-15 min; 30 min
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What type of muscle does not get paralyzed with NMBD? and ex?
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smooth and cardiac: heart, bronchi, uterus, bowel
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What is the chemical structure of succ?
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2 Ach molecules
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Main site of action of NMBD:
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nicotinic cholinergic receptor and endplate of muscle
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What are the 3 properties of all LA?
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1. benzene ring
2. quaternary amine 3. intermediate chain (ester - O or amide- N) |
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What is the MOA of LA?
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1.equilibration of ionized and nonionized form outside of nerve membrane
2. nonionized form enters nerve - reequilibration - ionized form moves up into inside of Na channel and binds = blocks depolarization |
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True or False: all LA are acids
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false = all are bases
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What does the addition of HCO3- do to the solution?
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Increased pH = increases lipid solubitlity = faster onset
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The close pKa is to body pH = the ______ the ______.
(exception?) |
faster the onset
exception = chloroprocaine - still fastest regardless of pKa |
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What does protein binding affect?
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duration of action
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Adding epi _____ onset time (except for spinals)
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decreases
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What are 3 reasons to put epi in LA?
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1. hemostasis
2. inc. duration of block 3. dec risk of toxicity |
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What are 4 properties that affect LA toxicity?
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1. vascularity
2. speed of injection 3. addition of epi 4. pH of area |
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How are esters metabolized?
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hydrolysis of cholinesterases
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How are amides metabolized?
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by liver in cytochrome enzymes
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Which LA are more allergenic?
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esters
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What are s/s LAST in order?
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1. lightheadedness, tinnitus, tongue numbness
2. visual disturbances 3. muscular twitching 4. convulsions 5. unconscious 6. coma 7. resp arrest 8. CV arrest |
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What are 4 ways to prevent LAST?
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1. use lowest dose
2. incremental injections 3. aspirate 4. use IV marker |
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3 drugs that should be avoided in the tx of LAST?
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vasopressin, CCB, BB
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Cocaine is the only LA that _____?
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vasoconstricts
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Which drug is an isomer of bupivicaine but has less cardiotoxicity?
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ropivicaine
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What are the 3 naturally occurring catecholamines in the body?
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dopamine, NE, epi
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What is the synthesis of catecholamines?
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tyrosine -- dopa-- dopamine--NE--epi
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Where is the enzyme COMT found?
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in the synapse
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Where is the enzyme MAO found?
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mitochondria
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What is an example of a drug that interferes with synthesis of NT?
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demser - sympatholytic
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What is the MOA of methyldopa?
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formation of false NT
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What are two examples of drugs that block reuptake of NE?
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cocaine, hemicholinium
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What is the MOA for vesamicol and reserpine?
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block transport system of storage vesicle
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What is an example of a drug that promotes release of catecholamines?
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amphetamines and ephedrine
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What is the MOA for clonidine and precedex?
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prevent release of catecholamines
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What are examples of drugs that mimic NT at postjunctional sites?
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neo, dobutamine, precedex
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What are examples of drugs that block postsynaptic receptor?
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atropine, lopressor, atenolol
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What is MOA of neostigmine and MAOI?
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inhibition of breakdown of transmitter
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What are drugs that interfere with 2nd messenger system?
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milrinone, viagra
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What happens to the radial muscle if alpha receptors stimulated?
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contraction - mydriasis
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What happens to sphincter muscle is muscarinic receptors stimulated?
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contraction - miosis
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Stimulating Beta 2 receptors in the periphery will cause:
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dilation
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Stimulating Alpha 1 and 2 receptors in the periphery will cause:
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constriction
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Cerebral arteries are unique and have only alpha 1 receptors. True or False?
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True - no beta
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Stimulating M2M3 receptors in the GI tract is mainly :
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stimulating (except sphincters relax)
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Kidneys have _____ receptors that increase renin secretion.
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beta 1
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Stimulating M3M2 receptors in the bladder will cause the detrusor muscle to _____
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constrict
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Stimulating the beta 2 receptors in the bladder will cause the detrusor muscle to _____
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relax
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Stimulating the alpha 1 receptors in the bladder will cause which things to contract?
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the trigone and sphincter
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Stimulating which receptors in the bladder will cause the trigone and sphincter to relax?
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M3M2
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Which receptors cause lypolysis?
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alpha 1, beta 1,2,3
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Stimulating which receptors in the liver will cause glycogenolysis and gluconeogenesis?
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alpha 1 and beta 2 - increase BG
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Stimulating which receptor will cause decreased insulin secretion in the pancreas?
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alpha 2
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Stimulating which receptor will cause increased insulin secretion in the pancreas?
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beta 2
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What are some side effects of alpha agonists?
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ocular decongestion, nasal decongestion, goosebumps, constipation, nervousness, sweating, HA, restlessness
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Name 3 side effects of alpha blockers.
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nasal congestion, HA, impotence
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Name 6 effects of beta agonists.
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tachycardia, bronchodilation, vasodilation, decreased GI motility, uterine relaxation, increased BG
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Name 4 effects from cholinergic agonists.
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miosis, bradycardia, bronchoconstriction, increased GI motility
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Which drug will cause increased BP and SVR, and reflex bradycardia?
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neo
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Which drug will cause increased BP, HR, and SVR?
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Norepi
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Which drug will cause increased SBP and HR, and decreased DBP and SVR.
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epi
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Dopamine will cause which receptor effects at 2-5 mkm.
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beta
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What are the effects of ephedrine?
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indirect and direct acting - centrally and peripherally
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Which anticholinergic drug does not cross the BBB and is 100% ionized?
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robinul
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Why do LA not work on infected tissues?
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they have a pH around 5 , and injecting a basic LA into that area will cause it to be 100% ionized.
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