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79 Cards in this Set
- Front
- Back
Succinylcholine is 2 ____ put together
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ACh
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NM blocking agents interfere with the transmission of ____ impulses b/w somatic motor neurons and skeletal muscle fibers
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Cholinergic
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Specificity for the _______ occurs only with therapeutic doses of NM blockers
(in higher amts --> extends to addtl sites and causes ADRs) |
NM jx
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NM do not effectively penetrate the _____ at therapeutic levels
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BBB
(so minimal CNS effects) |
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Most NM blocking agents (older) cause the release of ______ from intracellular stores
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Histamine
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NM release of histamine causes (5)
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- Bronchospasm
- Inc salivary and mucosal secretions - Hypotension - Tachycardia - Urticaria |
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Affected by low dose NM blocking agents (3)
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Rapid contracting small muscles
- Eyes and eyelids - Speech and swallowing - Fingers |
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Anesthesiologist monitors NM blocking with ____
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Stimulator on finger (1st thing NM affects)
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Affected by medium dose NM blockers (3)
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- Limbs
- Neck - Trunk |
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Affected by high dose NM blockers (2)
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Respiration
- Intercostal muscles - Diaphragm |
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NM blockers have ____ margin b/w effective and toxic dose
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small
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2 types of NM blocking agents
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- Depolarizing
- Nondepolarizing |
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Depolarizing NM blockers MOA
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- Depolarizes receptors initially --> muscle stimulation
- Persistant occupation delays repolarization and blocks recovery |
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Nondepolarizing NM blockers MOA
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Competively antagonizes ACh at R site
--> prevents depolarization - Produces flaccid paralysis |
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NM blocking agent uses (4)
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- Adjuncts to GA
- Facilitates intubation - Improves breathing on ventilator (pt can't fight) - Decs injury in shock therapy |
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Drugs that cause additive effects with NM blocking agents (6)
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- Abx
- Inhalation GAs - Ketamine - LAs - Lithium - Quinidine |
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Meds that dec effects of NM blocking agents (4)
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- Cholinergic drugs
- Corticosteroids - Ranitidine - Theophylline |
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Abx that have additive effects with NM blocking agents (3)
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- Aminoglycosides
- Lincosamides - Polymixins |
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Addtl meds needed for pain control with NM blockers, b/c they do not (2)
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- Reduce conscious
- Provide analgesia (need to pinch skin and pay attn to HR) |
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Depolarizing NM blockers have a _____ action
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Biphasic
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Biphasic action of depolarizing NM blockers
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- Depolarization of motor end plate initially
- Persistant ocupation of R site |
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Initial depolarizing of motor end plate in depolarizing NM blockers causes
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Brief muscle ctxs (fasciculations)
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Secondary persistant occupation of R sites in depolarizing NM blockers causes
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- Desensitization of R site to ACh (may last beyond drug action --> possible conformation change)
- Prevents repolarization - Paralysis |
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Secondary persistant occupation of R sites with depolarizing NM blockers lasts
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10-30 mins
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Prototype Depolarizing NM blocker
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Succinylcholine
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Succinylcholine is rapidly hydrolyzed by plasma cholinesterase to _______
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Succinylmonocholine
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Succinylcholine is rapidly hydrolyzed to Succinylmonocholine by
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Plasma cholinesterase
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Succinylmonocholine is a _____ metabolite of Succinylcholine
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Active
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- Weaker than parent drug
- Slowly hydrolyzed - Accumulates with prolonged/lg doses - May result in lengthy paralysis |
Succinylmonocholine
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Muscle paralysis from succinylcholine lasts _____
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8-10mins
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Onset of succinylcholine occurs after ____ with IV
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1 min
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Max effects of succinylcholine occur in
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2-4 mins
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ADRs:
- Muscle twitch/pain - Tachycardia - HTN - Arrhythmia - Resp depression - Apnea - Excessive salivation - Inc IOP - Malig Hyperthermia |
Succinylcholine
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3 main ADRs of succinylcholine
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- Muscle twitch
- Muscle pain - Malignant hyperthermia |
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Early signs of malignant hypertheramia (4)
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- Muscle rigidity
- Tachycardia - Metabolic acidosis - Hyperthermia |
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Need to monitor body temp when administer succinylcholine to prevent
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Malignant Hyperthermia
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Inc change of this ADR for succinylcholine if given with GA
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Malignant Hyperthermia
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Succinylcholine contraindications (4)
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- 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 |
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If use succinylcholine in patient with ____, may cause blindness
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narrow angle glaucoma
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If use succinylcholine in pt with __________ , pt won't be able to metabolize and may inc length of time of drug
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Deficiency of plasma pseudocholinesterase
(don't test for, just are ready to deal with it if it occurs) |
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Succinylcholine may cause arrhythmias in pts on (2)
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Digitalis
Quinidine |
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Nondepolarizing agents are antagonists --> have enough affinity for ____
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R area but doesn't activate it
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aka antidepolarizing, stabilizing or curariform drugs
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Nondepolarizing NM blockers
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Nondepolarizing NM blockers also called curariform drugs b.c used to be used in ___________ collectively called curare
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South America arrow poisonings
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All nondepolarizing agents have quaternary nitrogen like ________-
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d-tubocurarine
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Nondepolarizing agents are _____ antagonists of ACh at postsynaptic NM cholinergic (nicotininc 2) R sites
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Reversible
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Isoquinolone derivative Nondepolarizing NM blocking agent used to dx myasthenia gravis --> if have it, will inc muscle weakness with even a small dose
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Tubocurarine
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Isoquinolone derivative nondepolarizing NM blocking agents (4)
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- Tubocurarine
- Atracurarine - Doxacurium - Metocurine - Mivacurium |
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Isoquinolone derivative that causes histamine release
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Tubocurarine
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Use of this with diazepam may inc risk of malignant hyperthermia
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Tubocurarine
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Isoquinolone derivative that is less likely to cause histamine release
- Hypotensive effect minimal at recommended dose - Metabolized quickly |
Atracurium
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If administer this under isoflurane or enflurane, have to decrease the dose by 1/3
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Atracurium
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Atracurium onset is ____ after IV injection
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2-5 mins
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- Rapidly inactivated in plasma
- Recovery occurs within 20-30 mins --> is complete in 1 hr |
Atracurium
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Atracurium repeated doses have no cumulative effects on duration of NM block if recommended _______
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Dosage intervals are followed
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Atracurium ADRs (3)
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- Flushing
- Mild hypotension - At inc dose, have histamine ADRs |
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Isoquinolone with little to no release of histamine
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Doxacurium
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Max effect and duration of action of Doxacurium
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Max = 2-3mins
Duration: 20-30 mins |
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- May accumulate in body with repeated dose
- Excreted largely unchanged in urine |
Doxacurium
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Effects of may be increased in presence of:
- Hypokalemia - Dec renal clearance |
Doxacurium
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2 Isoquinolones that have no other notes except that they cause histamine release
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- Metocurine
- Mivacurium |
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Nodepolarizing NM blockers that are steroid derivatives (3)
--> all have minimal histamine release |
- Pancuronium
- Pipecuronium - Vecuronium |
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OD of nondepolarizing NM blockers treated by (3)
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- Artificial respiration with O2
- Vasopressors - Cholinesterase inhibitors |
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Vasopressors = aka
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Vasoconstrictors
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Things used to tx OD of nondepolazing agents are contraindicated for depolarizing agents b/c (2)
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- Will further stimulate cholinergic R's
- Can intensify muscle paralysis |
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Direct acting skeletal muscle relaxants differ from NM blocking agents because
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No interference with transmission of impulse b/w motor neurons and muscle
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Direct Skeletal Muscle relaxants MOA
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- Dec Ca2+ release from SR --> Dec ctx of muscle
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Direct acting skeletal muscle relaxants affect ____ > _____
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Fast twitch (reflex) > Slow (voluntary)
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Prototype direct acting skeletal muscle relaxant
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Dantrolene
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Dantrolene used in oral form to tx muscle spasticity from ______-
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Chronic neuro disorders
(CP, MS, Spinal injury, stroke) |
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t1/2 of Dantrolene
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9 hrs
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Therpeutic effects of Dantrolene may not occur until _____
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1-2 wks after initiation
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Given IV for emergency management of malignant hyperthermia
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Dantrolene
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Dantrolene used to tx malignant hyperthermia MOA (3)
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- Dec Ca2+ from SR
- Impairs catabolism in muscle cells - Decs potential lethal elevation in body temp |
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Major Dantrolene ADR --> esp with high doses or long term tx
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Hepatotoxicity
(have to monitor LFTs!) |
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Risk of Hepatic injury with Dantrolene is highest in
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F - 35 yrs+
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Discontinue Dantrolene if no benefit seen within ____ days
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45
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CNS ADRs of Dantrolene (3)
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Dizziness
Drowsiness Weakness |
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Dantrolene ADRs in addition to hepatic and CNS effects (3)
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- GI probs - Constipation & Diarrhea
- Dysphagia - Photosensitization |