meds; muscle relaxants Flashcards
succ brand name
anectine
succ dose
1-1.5 mg/kg
succ concentration
20 mg/ml
succ onset
30-60 seconds
succ duration
5-10 min
succ structure
two ach molecules combined by and acetate methyl linkage
succ moa
depol muscle relaxant -> fasisculation
binds to alpha 1 subunit
succ phase 2 block
high dose for long time = screwed up receptors that dont work well
succ metabolism
pseudocholinesterase/ butyrylcholinesterase -> plasma cholinesterase (from liver)
hydrolyze acetate methyl -> succinylmonocholine-» succinic acid and choline
dibucaine and succ relationship
dibucaine inhibits the breakdown of plasma cholinesterase. The number reflects the % of normal enzyme that is inhibited by Dibucaine.
normal ; 80
< 20 = succ can last 3 hrs = atypical variant of plasmacholinesterase.
Succ side effects
MH
histamine release
inc K by 0.5meq/L
myalgia
increase ICP (hyperventilate)
increased IOP
cardiac dysrhythmia
myoglobinuria
inc ingragastric pressure
inc LES pressure
massetter muscle contraction
Contraindications for Succ
MG; inc dose of succ (fewer R)
stroke/ immobility
Duchcennes
Burns after 24 hrs
denervating Dz
skm trauma
upper motor neuron lesion
Peds
ELMS; give less
increased risk of allergic rxn
cisatricurium brand name
nimbex
Cis dose
0.1 mg/kg
Cis concentration
2 mg/ml
Cis onset
2-3 min
Cis duration
40-75 min
Cis structure
Benzylisoquinalone
cis isomer of atricurium
least likely NMBD to have an allergic rxn
cis
Cis gtt dose
1 – 2 mcg/kg/min
cis metabolism
hoffman elimination; ph/temp dependent
hypothermic and acidotic = prolonged elimination
Side effects of cis
elderly = delay in recovery d/t CO
obese= increased duration of action /t VD
Vec brand name
norcuron
Vec dose
0.1mg/kg
*IBW
Vec concentration
1 mg/ml
supplied as powder. mix with water
vec onset
2-3 min
Vec duration
45-90 min
Vec structure
Aminosteroid
Vec gtt dose
1 – 2 mcg/kg/min. Can be infused but not the best choice because of accumulation
Vec metabolism
liver
active metabolites thats 80% as potent
in renal failure E1/2 is prolonged
Vec specific side effect
respiratory acidosis after NMBD = prolonged blockade
Contraindications for Vec
renal failure/ ERCP
liver failure
Elderly = delayed recovery from gtt
OB; difficult to clear in 3rd trimester because of progesterone and prolonged duration in post partum
Rocuronium brand name
zemuron
Roc gtt dose
5 – 12 mcg/kg/min. Much less accumulation then Vecuronium
Roc dose
0.6 mg/kg
1.2 mg/ kg(RSI)
*IBW
Roc concentration
10 mg/ml
Roc onset
2-3 (1.5) min
Roc duration
35-75 min
Roc structure
Aminosteroid
Roc metabolism
Excreted unchanged in bile / renal
Roc contraindications
longer duration in Elderly and liver failure dt decreased clearance
prolonged in elderly and pregnancy
pancuronium brand name
Pavulon
Panc dose
0.1mg/kg
Panc concentration
2 mg/ml
Panc onset
2-3 min
Panc duration
60-120 min
Panc structure
aminosteroid
Panc metabolism
urine
renal failure - give less
liver dz; give inc initial dose/ lasts longer
Panc side effects
inc hr map and co
vagal blockade/ inc sns activity
MOA for non depol NMBD
bind to both alpha subunits on ach R and antagonize ach
no depol
binds to alpha autoreceptor on the presynaptic neuron that stimulates ach release and causes fade
**Volatiles increase sensitivity
Common side effects amongst all non depol NMBD
increased hearing acuity, ptosis, diplopia, dysphagia, mandibular muscle wkns
how is pseudocholinesterase activity affected in pregnancy?
decreased due to estrogen
how is pseudocholinesterase activity affected in obesity
increased
how is pseudocholinesterase activity affected in renal failure?
decreased
What drugs decrease pseudocholinesterase activity
neostigmine, reglan, chemo, insecticides, genetic atypical
or have decreased hepatic production
What enhances/ prolongs blockade
diuretics
LA’s
magnesium
metrocloprimide
sns drugs; dec onset time
dec sns drugs; increase onset time
hypothermia= double duration
women are more sensitive than men
the effects of hypokalemia and hyperkalemia on NMBD
Hypokalemia = hyperpolized cell
depol; dec sensitivity= give more
non depol; incr sensitivity= give less
hyperkalemia = closer to depolarizing
depol; inc sensitiivty = give less
non depol = dec sensitiivty; give more (more resistance to keep from depolarizing)
Drugs that antagonize the actions of non depolarizing NMBs (decrease duration)
steroids
calcium chloride
carbamazepine
Neostigmine dose
0.04-0.07 mcg/kg
Neostigmine onset
5-10 min
Neostigmine duration
60 min
Neostigmine MOA
Bind to ache/ decrease ache activity -> inc ach in the NMJ -> out compete paralytics for R site
neostigmine side effects
Bradycardia, dysrhythmias, decreased SVR, asystole
bronchoconstriction, increased salivation, hypoperistalsis, increased gastric fluid secretions, PONV, miosis
Neostigmine metabolism
Renal and hepatic clearance
renal failure = decreased clearance/ prolonged action
neostigmine max dose
5 mg (has ceiling effect)
glycopyrrolate MOA
anticholinergic
wont cross BBB because its a quaternary amine = polar
Glycopyrrolate dose
0.2 mg for every mg of neostigmine given
1 mg = max
Sugammadex brand name
bridion
sugammadex structure
Gama cyclodextrin
sugammadex dose
2-16 mg/kg
dose to give for sugammadex depends on
twitch response
fade = 2mg/kg
post tetanic = 4 mg/kg
extreme block = 8 mg/kg
sugammadex onset
1-4 min
sugammadex duration
1.5-3 hrs
sugammadex works best on what meds?
Roc > Vec > Panc
how soon after giving sugammadex can you redose roc
5 min
Sugammadex MOA
selective relaxant binding agent w/ aminosteroid
- highly water soluble
intermolecular forces (van der walls), thermodynamic (hydrogen) bonds and hydrophobic interactive -> tight reversal by encapsulation. binds to free drug in plasma
Who is sugammadex contraindicated in
renal impairment/dialysis
Sugammadex side effects
N/V , pruritis, uticaria
anaphylaxis, bradycardia
doesn’t work
binds to progesterone so oral contraceptives won’t work for up to 7 days
tormefene (antiestrogen); displaces NMBD from sugammadex
heparin/ LMWH; inc pt, PTT, INR
recurrarization w/ lower than the recommended dose
Sugammadex elimination
Urine
70% in 6 hrs
90% in 24 hrs
Why is the adductor pollicis checked for TOF?
laynx reflexes lost before adductor pollicis, so if TOF is 2/4 twitches on adductor pollicis then larynx is beyond that.
Where is the monitoring site that More closely reflects diaphragm and laryngeal muscle blockade
Orbicularis oculi
Normal defasiculating dose
Defasciculating dose = give 20% of normal intubating dose early.
1-10mg of ROC or 1/10th dose of succ
give lido, fent, defasic, prop, then rest of nmbd
Glycopyrolate onset
2-3min
What achEi is used in peds
Edrophonium
Glycopyrrolate duration
2 hrs
Edrophonium trade name
Tensilon
Glycopyrrolate concentration
0.2 mg/ml
Edrophonium onset
1-2 min
Edrophonium DOA
5 – 20 minutes.
Larger doses: up to 60 minutes
Edrophonium dose
max = 1-1.5mg/kg
Pyridostigmine trade name
Mestinan
Pyridostigmine dose
0.5-2mg
Pyridostigmine onset
16 minutes
Pyridostigmine DOA
90 minutes
Neostigmine trade name
Prostigmine
Vec after sux dose
0.05mg/kg
Roc after sux dose
0.3mg/kg
Nimbex after sux dose
0.1mg/kg