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33 Cards in this Set
- Front
- Back
Non-Depolarizing
Antagonists |
Aminosteroids (Pancuronium, Vecuronium & Rocuronium);
Benzylisoquinolines (Doxacurium, Atracurium, Cis-Atracurium & Mivacurium) |
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Factors contributing to prolonged effects of Succinylcholine
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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) |
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Genetic prevalence of pseudocholinesterse defect
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Heterozygous - 1 in 50 people
Homozygous 1 in 3000 |
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CV Effects of Succinycholine
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Children:
Sinus Bradycardia Junctional Rhythm Sinus Arrest Adults: Tachycardia Hypertension Hyperkalemia |
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Adverse effects of succinycholine
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Myalgia;
Increased ICP/IOP/IGP Trismus Malignant Hyperthermia Histamine Release Hyperkalemia |
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Treatment of Hyperkalemia
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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) |
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Succinylcholine Contraindications
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Renal Disease, SCI, CVA, Immobility, Hyperkalemia,
Burns, Crush Injuries, Sepsis, Acidosis, Atypical Pseudocholinesterase, MH, Children **** (ASA recommendation), icreased ICP/IOP. |
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Characteristics of Non-Depolarizers?
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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. |
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Characteristics of Aminosteroids
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Vagolytic - (Pancuronium > Rocuronium > Vecuronium
No Histamine Release Organ Dependent Elimination ( Kidneys & Liver) |
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Characteristics of
Benzylisoquinolines |
Absence of Vagolytic Effect;
Histamine Release: dTc (curare)> Atracurium > Mivacurium > Cisatracurium Generally Organ-independent Elimination; Non-cumulative; |
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Characteristics of Non Depolarizing Muscle Relaxants
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Nicotinic Antagonist;
Muscle Relaxation Occurs When Receptors are 80-90% Blocked; |
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Long Acting (> 60 Minutes)
NDMR |
Pancuronium, Doxacurium & d-Tubocurarine
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Intermediate Acting (30 – 45 Minutes) NDMR
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Atracurium, Cisatracurium, Rocuronium & Vecuronium
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Short Acting (12 – 20 Minutes) NDMR
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Mivacurium
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General Pharmacological Characteristics of NDMR
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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 |
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Pancuronium (Pavulon)- characteristics
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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. |
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Vecuronium (Norcuron)- characteristics
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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. |
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Rocuronium (Zemuron)- characteristics
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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. |
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Doxacurium (Neuromax)
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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 |
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Atracurium (Tracrium)
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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. |
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Cisatracurium (Nimbex)
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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 |
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Mivacurium (Mivacron)
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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. |
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Endogenous Esterases
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Acetylcholinesterase,
Pseudocholinesterase & Nonspecific Plasma Esterases |
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Action of AChEI at the NMJ
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Accelerate Reversal of NDMR activity by inhibiting AChE --> increase ACh concentration at NMJ
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Cholinesterase Inhibitors have Effects at All Cholinergic Receptors.
What are their CV effects? |
CV - Dec HR, causes dsrhythmias.
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Pulmonary effects of Cholinesterase Inhibitors
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Bronchospasm,
Increased Bronchial Secretions |
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CNS effects of Cholinesterase Inhibitors
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Diffuse Excitation
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Action of Anticholinergics Anitmuscarinic
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Antagonism Of Cholinergic Stimuli At Muscarinic Receptors With Little To No Effect At Nicotinic Receptors.
Competitively Blocks Muscarinic Receptors |
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Pharmacologic Characteristics of Anticholinergics Anitmuscarinic
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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). |
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NEOSTIGMINE - dose, onset, duration & recommended anticholinergic
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0.04 - 0.08 mg / kg;
5-10 minutes; 45-90 minutes; Glycopyrrolate - 0.2 mg per 1 mg Neostigmine |
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EDROPHONIUM - dose, onset, duration of action and recommended anticholinergic
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0.5-1.0 mg/Kg;
Within 5 Minutes; 30-60 Mins; Atropine - 0.014 mg per 1 mg Edrophonium |
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PYRIDOSTIGMINE - dose, onset, duration of action and recommended anticholinergic
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0.1-0.4 mg/kg;
10-20 minutes; 60-120 minutes; Glycopyrrolate - 0.05 mg per 1 mg Pyridostigmine |
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What test determines pseudocholinesterase abnormality?
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The Dibucaine test.
Dibucaine number of 80% = normal, 40-60%=heterozygous, 20%=homozygous. Dibucaine number represents the quality of the Pseudocholinesterase NOT QUANTITY. |