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79 Cards in this Set

  • Front
  • Back
Succinylcholine is 2 ____ put together
ACh
NM blocking agents interfere with the transmission of ____ impulses b/w somatic motor neurons and skeletal muscle fibers
Cholinergic
Specificity for the _______ occurs only with therapeutic doses of NM blockers
(in higher amts --> extends to addtl sites and causes ADRs)
NM jx
NM do not effectively penetrate the _____ at therapeutic levels
BBB
(so minimal CNS effects)
Most NM blocking agents (older) cause the release of ______ from intracellular stores
Histamine
NM release of histamine causes (5)
- Bronchospasm
- Inc salivary and mucosal secretions
- Hypotension
- Tachycardia
- Urticaria
Affected by low dose NM blocking agents (3)
Rapid contracting small muscles
- Eyes and eyelids
- Speech and swallowing
- Fingers
Anesthesiologist monitors NM blocking with ____
Stimulator on finger (1st thing NM affects)
Affected by medium dose NM blockers (3)
- Limbs
- Neck
- Trunk
Affected by high dose NM blockers (2)
Respiration
- Intercostal muscles
- Diaphragm
NM blockers have ____ margin b/w effective and toxic dose
small
2 types of NM blocking agents
- Depolarizing
- Nondepolarizing
Depolarizing NM blockers MOA
- Depolarizes receptors initially --> muscle stimulation
- Persistant occupation delays repolarization and blocks recovery
Nondepolarizing NM blockers MOA
Competively antagonizes ACh at R site
--> prevents depolarization
- Produces flaccid paralysis
NM blocking agent uses (4)
- Adjuncts to GA
- Facilitates intubation
- Improves breathing on ventilator (pt can't fight)
- Decs injury in shock therapy
Drugs that cause additive effects with NM blocking agents (6)
- Abx
- Inhalation GAs
- Ketamine
- LAs
- Lithium
- Quinidine
Meds that dec effects of NM blocking agents (4)
- Cholinergic drugs
- Corticosteroids
- Ranitidine
- Theophylline
Abx that have additive effects with NM blocking agents (3)
- Aminoglycosides
- Lincosamides
- Polymixins
Addtl meds needed for pain control with NM blockers, b/c they do not (2)
- Reduce conscious
- Provide analgesia

(need to pinch skin and pay attn to HR)
Depolarizing NM blockers have a _____ action
Biphasic
Biphasic action of depolarizing NM blockers
- Depolarization of motor end plate initially
- Persistant ocupation of R site
Initial depolarizing of motor end plate in depolarizing NM blockers causes
Brief muscle ctxs (fasciculations)
Secondary persistant occupation of R sites in depolarizing NM blockers causes
- Desensitization of R site to ACh (may last beyond drug action --> possible conformation change)
- Prevents repolarization
- Paralysis
Secondary persistant occupation of R sites with depolarizing NM blockers lasts
10-30 mins
Prototype Depolarizing NM blocker
Succinylcholine
Succinylcholine is rapidly hydrolyzed by plasma cholinesterase to _______
Succinylmonocholine
Succinylcholine is rapidly hydrolyzed to Succinylmonocholine by
Plasma cholinesterase
Succinylmonocholine is a _____ metabolite of Succinylcholine
Active
- Weaker than parent drug
- Slowly hydrolyzed
- Accumulates with prolonged/lg doses
- May result in lengthy paralysis
Succinylmonocholine
Muscle paralysis from succinylcholine lasts _____
8-10mins
Onset of succinylcholine occurs after ____ with IV
1 min
Max effects of succinylcholine occur in
2-4 mins
ADRs:
- Muscle twitch/pain
- Tachycardia
- HTN
- Arrhythmia
- Resp depression
- Apnea
- Excessive salivation
- Inc IOP
- Malig Hyperthermia
Succinylcholine
3 main ADRs of succinylcholine
- Muscle twitch
- Muscle pain
- Malignant hyperthermia
Early signs of malignant hypertheramia (4)
- Muscle rigidity
- Tachycardia
- Metabolic acidosis
- Hyperthermia
Need to monitor body temp when administer succinylcholine to prevent
Malignant Hyperthermia
Inc change of this ADR for succinylcholine if given with GA
Malignant Hyperthermia
Succinylcholine contraindications (4)
- Hx of malignant hyperthermia
- Narrow angle glaucoma (further inc pressure --> crush optic nerve = blind)
- Genetic deficiency of plasma pseudocholinesterase
- Pts on digitalis or quinidine --> may cause arrhythmias
If use succinylcholine in patient with ____, may cause blindness
narrow angle glaucoma
If use succinylcholine in pt with __________ , pt won't be able to metabolize and may inc length of time of drug
Deficiency of plasma pseudocholinesterase
(don't test for, just are ready to deal with it if it occurs)
Succinylcholine may cause arrhythmias in pts on (2)
Digitalis
Quinidine
Nondepolarizing agents are antagonists --> have enough affinity for ____
R area but doesn't activate it
aka antidepolarizing, stabilizing or curariform drugs
Nondepolarizing NM blockers
Nondepolarizing NM blockers also called curariform drugs b.c used to be used in ___________ collectively called curare
South America arrow poisonings
All nondepolarizing agents have quaternary nitrogen like ________-
d-tubocurarine
Nondepolarizing agents are _____ antagonists of ACh at postsynaptic NM cholinergic (nicotininc 2) R sites
Reversible
Isoquinolone derivative Nondepolarizing NM blocking agent used to dx myasthenia gravis --> if have it, will inc muscle weakness with even a small dose
Tubocurarine
Isoquinolone derivative nondepolarizing NM blocking agents (4)
- Tubocurarine
- Atracurarine
- Doxacurium
- Metocurine
- Mivacurium
Isoquinolone derivative that causes histamine release
Tubocurarine
Use of this with diazepam may inc risk of malignant hyperthermia
Tubocurarine
Isoquinolone derivative that is less likely to cause histamine release
- Hypotensive effect minimal at recommended dose
- Metabolized quickly
Atracurium
If administer this under isoflurane or enflurane, have to decrease the dose by 1/3
Atracurium
Atracurium onset is ____ after IV injection
2-5 mins
- Rapidly inactivated in plasma
- Recovery occurs within 20-30 mins --> is complete in 1 hr
Atracurium
Atracurium repeated doses have no cumulative effects on duration of NM block if recommended _______
Dosage intervals are followed
Atracurium ADRs (3)
- Flushing
- Mild hypotension
- At inc dose, have histamine ADRs
Isoquinolone with little to no release of histamine
Doxacurium
Max effect and duration of action of Doxacurium
Max = 2-3mins
Duration: 20-30 mins
- May accumulate in body with repeated dose
- Excreted largely unchanged in urine
Doxacurium
Effects of may be increased in presence of:
- Hypokalemia
- Dec renal clearance
Doxacurium
2 Isoquinolones that have no other notes except that they cause histamine release
- Metocurine
- Mivacurium
Nodepolarizing NM blockers that are steroid derivatives (3)
--> all have minimal histamine release
- Pancuronium
- Pipecuronium
- Vecuronium
OD of nondepolarizing NM blockers treated by (3)
- Artificial respiration with O2
- Vasopressors
- Cholinesterase inhibitors
Vasopressors = aka
Vasoconstrictors
Things used to tx OD of nondepolazing agents are contraindicated for depolarizing agents b/c (2)
- Will further stimulate cholinergic R's
- Can intensify muscle paralysis
Direct acting skeletal muscle relaxants differ from NM blocking agents because
No interference with transmission of impulse b/w motor neurons and muscle
Direct Skeletal Muscle relaxants MOA
- Dec Ca2+ release from SR --> Dec ctx of muscle
Direct acting skeletal muscle relaxants affect ____ > _____
Fast twitch (reflex) > Slow (voluntary)
Prototype direct acting skeletal muscle relaxant
Dantrolene
Dantrolene used in oral form to tx muscle spasticity from ______-
Chronic neuro disorders
(CP, MS, Spinal injury, stroke)
t1/2 of Dantrolene
9 hrs
Therpeutic effects of Dantrolene may not occur until _____
1-2 wks after initiation
Given IV for emergency management of malignant hyperthermia
Dantrolene
Dantrolene used to tx malignant hyperthermia MOA (3)
- Dec Ca2+ from SR
- Impairs catabolism in muscle cells
- Decs potential lethal elevation in body temp
Major Dantrolene ADR --> esp with high doses or long term tx
Hepatotoxicity
(have to monitor LFTs!)
Risk of Hepatic injury with Dantrolene is highest in
F - 35 yrs+
Discontinue Dantrolene if no benefit seen within ____ days
45
CNS ADRs of Dantrolene (3)
Dizziness
Drowsiness
Weakness
Dantrolene ADRs in addition to hepatic and CNS effects (3)
- GI probs - Constipation & Diarrhea
- Dysphagia
- Photosensitization