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33 Cards in this Set

  • Front
  • Back
Non-Depolarizing
Antagonists
Aminosteroids (Pancuronium, Vecuronium & Rocuronium);
Benzylisoquinolines (Doxacurium, Atracurium, Cis-Atracurium & Mivacurium)
Factors contributing to prolonged effects of Succinylcholine
Hypothermia,
Low Pseudocholinesterase
Pregnancy (causes dilutional effect),
Liver disease (it is made in liver),
Renal disease
Certain drugs
Genetic defect (Homozygous - prolongs block 4-8hrs & Heterozygous - about 55mins)
Genetic prevalence of pseudocholinesterse defect
Heterozygous - 1 in 50 people
Homozygous 1 in 3000
CV Effects of Succinycholine
Children:
Sinus Bradycardia
Junctional Rhythm
Sinus Arrest
Adults:
Tachycardia
Hypertension
Hyperkalemia
Adverse effects of succinycholine
Myalgia;
Increased ICP/IOP/IGP
Trismus
Malignant Hyperthermia
Histamine Release
Hyperkalemia
Treatment of Hyperkalemia
Calcium Chloride / Gluconate (gluconate has 3x as much as Ca chloride);
Insulin & Glucose; Hyperventilation;
Sodium Bicarbonate;
Beta 2 Agonist (Albuterol); Lasix;
Sodium Polystyrene Sulfonate (Kayexalate)
Succinylcholine Contraindications
Renal Disease, SCI, CVA, Immobility, Hyperkalemia,
Burns, Crush Injuries, Sepsis,
Acidosis,
Atypical Pseudocholinesterase,
MH, Children **** (ASA recommendation), icreased ICP/IOP.
Characteristics of Non-Depolarizers?
Quaternary Ammonium Groups;
Highly Ionized;
Water Soluble Compounds at Physiological pH;
Limited Lipid Solubility;
Do not Cross Lipid Membrane (BBB, Renal Tubular Epithelium, GI Epithelium,
Placenta);
No CNS Effects.
Characteristics of Aminosteroids
Vagolytic - (Pancuronium > Rocuronium > Vecuronium
No Histamine Release
Organ Dependent Elimination ( Kidneys & Liver)
Characteristics of
Benzylisoquinolines
Absence of Vagolytic Effect;
Histamine Release:
dTc (curare)> Atracurium > Mivacurium > Cisatracurium
Generally Organ-independent Elimination;
Non-cumulative;
Characteristics of Non Depolarizing Muscle Relaxants
Nicotinic Antagonist;
Muscle Relaxation Occurs When Receptors are 80-90% Blocked;
Long Acting (> 60 Minutes)
NDMR
Pancuronium, Doxacurium & d-Tubocurarine
Intermediate Acting (30 – 45 Minutes) NDMR
Atracurium, Cisatracurium, Rocuronium & Vecuronium
Short Acting (12 – 20 Minutes) NDMR
Mivacurium
General Pharmacological Characteristics of NDMR
Hypothermia (decreases metabolism by decreasing enzymes activity in the liver);
pH
Hypokalemia / Hypocalcemia / Hypermagnesemia - augments the block;
Age;
Drugs (IA, dantrolene, myacins potentiate)
Dilatin causes resistance to ND blocking action);
Diseases;
Up & Down Regulation
Pancuronium (Pavulon)- characteristics
Long Acting Aminosteroid;
Dose:
Intubating = .12 mg / kg
2-3 mins for intubating conditions;
Maintenance dose -0.01 - 0.04 mg / kg (may use infusion).
Metabolism / Excretion -
Liver / Renal to Active Metabolite = Muscle Relaxation
Increase HR, BP & CO;
Vagal Blockade / Sympathetic Stimulation.
Vecuronium (Norcuron)- characteristics
Intermediate Acting Aminosteroid;
Dose:
Intubating: 0.12 mg /kg
Maintenance: 0.01 to 0.04 mg / kg (may use infusion or give bolus based on twitches and duration time).
Metabolism / Excretion -
Liver / Biliary & Renal.
Will accumulate with infusion b/c of active metabolite which will augment block.
Devoid of CV Effects.
Rocuronium (Zemuron)- characteristics
Intermediate Acting Aminosteroid;
Dose:
Normal Intubation: 0.6 mg / kg;
RSI 1.2 mg / kg;
Maintenance: 0.15 mg /kg;
Infusions 5- 12 mcg/kg/min;
Duration with RSI dose 60-90mins.
Metabolism / Excretion - No Metabolism;
Excreted Unchanged via Bile / Urine / Feces.
Doxacurium (Neuromax)
Long Acting Benzylisoquinoline
Dose:
Intubating: 0.05-0.07 mg/kg (intubating conditions in 5mins);
Maintenance: 0.005 mg/kg
Metabolism / Excretion -
Slow Hydrolysis – Pseudocholinesterase.
Long duration of action -
Very Limited Clinical Use
Atracurium (Tracrium)
Intermediate Acting Benzylisoquinoline;
Dose:
Intubating: 0.5 mg/kg (Inject slowly to decrease histamine release – Intubate in 3-5 min.);
Maintenance: 0.1 - 0.25 mg / kg
Infusion: 5-10 mcg/kg/min. Good for infusion b/c of metabolism;
Metabolism / Excretion -
Ester Hydrolysis: Nonspecific Esterases & Hofmann Elimination - Nonenzymatic Chemical Breakdown That Occurs At physiological pH and Temperature.
Metabolite: Laudanosine
Histamine release --> Bronchospasm, increase SVR, HR & Allergic Reactions.
Cisatracurium (Nimbex)
Intermediate Acting Benzylisoquinoline;
Dose:Intubating:0.1-0.15 mg/kg (intubation conditions in 2 min).
Infusion: 1 – 2 mcg/kg/min (No Accumulation)
Metabolism / Excretion -
Hofmann Elimination.
Active Metabolite - Laudanosine
Mivacurium (Mivacron)
Short Acting Benzylisoquinoline
Dose: Intubating: .15 - .2 mg/kg (Intubating conditions in 2–3 mins);
Infusion: 4 – 10 mcg/kg/min(No Accumulation);
Metabolism / Excretion -
Pseudocholinesterase;
BOLO: For Pseudocholinesterase Deficiency.
Histamine release --> increased BP/hHR & Bronchospasm.
Endogenous Esterases
Acetylcholinesterase,
Pseudocholinesterase &
Nonspecific Plasma Esterases
Action of AChEI at the NMJ
Accelerate Reversal of NDMR activity by inhibiting AChE --> increase ACh concentration at NMJ
Cholinesterase Inhibitors have Effects at All Cholinergic Receptors.
What are their CV effects?
CV - Dec HR, causes dsrhythmias.
Pulmonary effects of Cholinesterase Inhibitors
Bronchospasm,
Increased Bronchial Secretions
CNS effects of Cholinesterase Inhibitors
Diffuse Excitation
Action of Anticholinergics Anitmuscarinic
Antagonism Of Cholinergic Stimuli At Muscarinic Receptors With Little To No Effect At Nicotinic Receptors.
Competitively Blocks Muscarinic Receptors
Pharmacologic Characteristics of Anticholinergics Anitmuscarinic
Tachycardia (atropine > glycopyrrolate > scopolamine);
Bronchdilation (moderate effects with atropine & glycopyrrolate, mild with scopolamine);
Sedation (high with scopolamine, slight with atropine, none with glycopyrrolate);
Antisialagogue (equally effective with glycopyrrolate & scopolamine. Moderate effects with atropine).
NEOSTIGMINE - dose, onset, duration & recommended anticholinergic
0.04 - 0.08 mg / kg;
5-10 minutes;
45-90 minutes;
Glycopyrrolate - 0.2 mg per 1 mg Neostigmine
EDROPHONIUM - dose, onset, duration of action and recommended anticholinergic
0.5-1.0 mg/Kg;
Within 5 Minutes;
30-60 Mins;
Atropine - 0.014 mg per 1 mg Edrophonium
PYRIDOSTIGMINE - dose, onset, duration of action and recommended anticholinergic
0.1-0.4 mg/kg;
10-20 minutes;
60-120 minutes;
Glycopyrrolate - 0.05 mg per 1 mg Pyridostigmine
What test determines pseudocholinesterase abnormality?
The Dibucaine test.
Dibucaine number of 80% = normal, 40-60%=heterozygous, 20%=homozygous.
Dibucaine number represents the quality of the Pseudocholinesterase NOT QUANTITY.