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St. Francis Clinical Prep - Drugs
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Fentanyl MOA
Conc.: 50 mcg/mL
100 x more potent than morphine
MOR agonist
High lipid solubility
Rapid onset, short duration
Fentanyl Class
MOR opioid agonist
Fentanyl Induction Dose
1-2 mcg/kg
Fentanyl Maintenance Dose
1-3 mcg/kg/hr (prolonged effects if used as gtt)
Fentanyl Pharmacokinetics
Almost immediate maximal analgesic effect
Respiratory effects may take several minutes
Duration after 100 mcg is 30-60 min.
Half-life 2-4 hours
Hepatic metabolism, excreted by kidney (<10%)
Fentanyl Antagonist
naloxone (Narcan)
Lidocaine MOA
Conc.: 2% (20 mg/mL)
IV: Suppresses vent. arrhythmias and elevates fibrillation threshold by reducing velocity of electrical impulse through conductive system.
LA: Blocks conduction by decreasing permeability of Na+ on the nerve membrane, inhibiting pain conduction.
Lidocaine Class
1B anti-arrhythmic (membrane stabilizing with mild Na+ effects)
LA: amide
Lidocaine Induction Dose
1-1.5 mg/kg IV (blunts dysrhythmias and tachycardia)
Lidocaine Dose Limit
300 mg/hr IV
Lidocaine Pharmacokinetics
Onset: 45-90
Half-life initial: 7-30 minutes
Half-life terminal: 1.5-2 hours
Hepatic elimination
No antagonist
Propofol MOA
Conc.: 10 mg/mL
Modulates GABA receptors, increasing Cl- conduction, hyperpolarizes post-synaptic cell membrane.
Increases duration of opening of Cl- channels and prolongs hyper polarization and thus creates sedative and hypnotic effects.
Propofol Class
IV Sedative-Hypnotic
Propofol Induction Dosing
Adults: 1-3 mg/kg
Peds: 2.5-3.5 mg/kg
> 65 y.o.: 1-1.5 mg/kg (smaller central compartment and slower clearance)
Propofol Maintenance Dose
100-300 mcg/kg/min
Propofol Pharmacokinetics
Onset: < 1 min.
High Lipid Solubility
Redistribution Half-Life: 1-2 minutes
Elimination Half-Life: 0.5-1.5 hours
CSHT: < 40 min. after an 8-hour infusion
Metabolism: 60% hepatic, 40% renal
No reversal - D/C and support hemodynamics if propofol infusion syndrome suspected
Etomidate MOA
Conc.: 2 mg/mL
Binds GABA and enhances GABA affinity for neurotransmitter
Preferred over propofol in unstable patients or cardiac patients
Etomidate Class
GABA mimetic
Etomidate Induction Dose
0.3-0.6 mg/kg
Etomidate Maintenance Dose
Not recommended - depresses adrenocortical function
Etomidate Pharmacokinetics
Onset: 30-40 sec.
Peak: 1 min.
Duration: 3-10 min.
Half-Life: 2-5 hours
No reversal
Ketamine MOA
Conc.: 50 mg/mL
Binds non-competitively to NMDA
Ketamine Class
Phencyclidine derivative
NMDA Antagonist
Ketamine Induction Dose
IV: 1-2 mg/kg
IM: 6/12 mg/kg
Peds IV: 1/2 mg/kg
Peds IM: 6-13 mg/kg
Trauma TIVA: 200 mg and 10 mg midazolam
Ketamine Maintenance Dose
1-2 mg/kg/hr
Ketamine Pharmacokinetics
Onset: 30 sec.
Peak: 3-5 min.
Duration: 8-15 min.
Half-life: 45 min.
No reversal
Rocuronium MOA
Conc.: 5 mg/mL
Competitive antagonism of ACh at the nACHR (NMJ). Reversible by competitive antagonism of ACh: cholinesterase inhibitors increase ACh at the NMJ displacing the NDNMB
Rocuronium Class
NDNMB (aminosteroidal)
Rocuronium Induction Dose
0.6 mg/kg
RSI: 1.2 mg/kg
(ED95 is 0.3 mg/kg, so 2-3x ED95)
Rocuronium Maintenance Doses
0.15 mg/kg
Rocuronium Pharmacokinetics
Onset: 1-2 min.
Duration: 30 min. for 0.6 mg/kg dose; 67 min. for 1.2 mg/kg dose
Half-life: 60-70 min.; 2x as long in hepatic dysfunction
Rocuronium Reversal
Sugammadex or neostigmine
Succinylcholine MOA
Conc.: 20 mg/mL
Mimics ACh at the NaCHR, causing depolarization.
Phase 1 Block: sustained opening of receptor channels in depolarized post-junctional membrane cannot respond to further ACh
Phase 2 Block: desensitized, depolarized post-junctional membrane remains unresponsive to ACh
Succinylcholine Class
Depolarizing NMB
Succinylcholine Induction Dose
1-1.5 mg/kg
Resistance to School after NDNMB (dose should be increased)
Succinylcholine Pharmacokinetics
Onset: 1 min.
Duration: 7-13 min. (dependent on dibucaine #)
Rapid metabolism
No reversal
Cisatricurium MOA
NDNMB with competitive antagonism of ACh at nACHR (NMJ)
Reversible by competitive antagonism by ACh: cholinesterase inhibitors
Cisatracurium Class
NDMB (benzylisoquinolinium)
Cisatracurium Induction Dose
0.15-0.2 mg/kg (ED95 is 0.05 mg/kg, so 2-3x)
*IBW
Cisatracurium Maintenance Dose
0.03 mg/kg
Cisatracurium Pharmacokinetics
Onset: 2-3 min.
Peak/Maximum block: 3-7 min.
Duration: 50 min.
Half-life: 22-29 min.
Cisatracurium Reversal
Neostigmine
Phenylephrine Concentrations
Vial: 10mg/mL
One 10 mg vial in 250 mL is 40 mcg/mL
Two 10 mg vials in 250 mL is 80 mcg/mL
Phenylephrine MOA
Sympathomimetic alpha-adrenergic agonist.
Constricts both arterial and venous blood vessels, increasing SVR without changing cardiac dynamics.
Phenylephrine Class
Alpha adrenergic agonist
Phenylephrine Intermittent Dosing
5-20 mcg/kg bolus
Phenylephrine Continuous Dosing
10-200 mcg/min.
OR
0.1-2 mcg/kg/min
Phenylephrine Pharmacokinetics
Onset: immediate
Duration: 15-20 min.
Phenylephrine Antagonism
Hydralazine or labetalol
Ephedrine MOA
Conc.: 50 mg/mL
Sympathomimetic amine that directly acts as an agonist at alpha- and beta-adrenergic receptors and indirectly causes the release of norepinephrine from sympathetic neurons.
Results: increased HR, BP, CO, and PVR
Ephedrine Class
Alpha/Beta Adrenergic Agonist
Ephedrine Initial Dosing
5-10 mg IV bolus
Ephedrine Subsequent Dosing
5-10 mg bolus as needed, not to exceed total of 50 mg
Ephedrine Pharmacokinetics
Onset: immediate
Duration: 1 hour
Half-life: 2.5-3.6 hours
Ephedrine Antagonism
Hydralazine or labetalol
Norepinephrine Concentrations
Typically
8 mg/250 mL (32 mcg/mL)
Norepinephrine MOA
Acts on both alpha-1 and alpha-2 adrenergic receptors to cause vasoconstriction.
Increases HR and BP, triggers release of glucose stores, increases BF to skeletal muscle, reduces GI BF, and inhibits voiding and GI motility.
Caution: extravasation
Norepinephrine Class
Alpha adrenergic agonist
Norepinephrine Intermittent Dosing
10-12 mcg IV bolus for hypotension related to sympathectomy from spinal anesthesia
Norepinephrine Continuous Dosing
0.05-0.5 mcg/kg/min
Norepinephrine Pharmacokinetics
Onset: immediate
Duration: 1-2 min. after infusion stopped
Half-life: 2 min.
Dexamethasone MOA
Conc.: 4 mg/mL
Decreases vasodilation and permeability of capillaries, decreases leukocyte migration to sites of inflammation.
At low-dose: anti-inflammatory
At high-dose: immunosuppressive
Dexamethasone Class
Corticosteroid
Dexamethasone Dosing
Adults: 8 mg IVP
Peds: 0.25 mg/kg
Dexamethasone Pharmacokinetics
Onset: immediate
Duration: variable for IV administration, 36 hours following PO
Half-life: 36-72 hours
Ondansetron MOA
Conc.: 4 mg/mL or 2 mg/mL
Blocks serotonin receptors in CTZ, reducing the communication to the vomiting center in the brain and decreases N/V
Ondansetron Class
5-HT3 Receptor Antagonist
Ondansetron Dosing
Adult: 4-8 mg IVP
Peds: 0.1 mg/kg
Ondansetron Pharmacokinetics
Onset: 10 min.
Duration: 2-7 hours
Half-life: 3 hours
Diphenhydramine MOA
Conc.: 50 mg/mL
Competitively inhibits the H1 receptors, alleviating symptoms cause by endogenous histamine on bronchial, capillary, and GI smooth muscles.
Prevents histamine-induced bronchoconstriction, vasodilation, increased capillary permeability, and GI smooth muscle spasms
Diphenhydramine Class
H1 receptor antagonist
Diphenhydramine Dosing
Adult: 25-50 mg
Peds: 1 mg/kg
Diphenhydramine Pharmacokinetics
Onset: immediate for IV, 15-30 min PO
Duration: 4-6 hours
Half-life: 5.4 hours
Hepatic metabolism, renal excretion
Neostigmine MOA
Conc.: 5 mg/10 mL (0.5 mg/mL)
Reversible inhibition of acetylcholinesterase by forming a carbamylated ester at the esteratic site, allowing massive accumulation of ACh at the NMJ
Neostigmine Class
Quaternary Anticholinergic
Neostigmine Dosing
0.02-0.08 mg/kg (0.07 at St. Francis)
Other method: (weight/2) x 0.1
Neostigmine Pharmacokinetics
Onset: 1-5 min.
Peak: 7-10 min
Duration: 30-60 min.
Half-life: 50 min.
Renal metabolism
Glycopyrrolate MOA
Conc.: 4 mg/20 mL (0.2 mg/mL)
Binds to mAChR and completely antagonizes ACh at that site.
Main use: decreases bradycardia
Glycopyrrolate Class
Quaternary Anticholinergic (Antimuscarinic)
Glycopyrrolate Dosing
With reversal:
neostigmine + glyco to prevent bradycardia: 0.2 mg glyco per 1 mg neo (1:5)
Anti-sialogogue:
0.1-0.2 mg IV
Vagolysis for mild bradycardia:
0.1-0.2 mg when ephedrine is not first choice
Glycopyrrolate Pharmacokinetics
Onset: immediate (< 1 min.)
Half-life: 50 min.
More rapid clearance than atropine (80% unchanged in urine)
Sugammadex MOA
Conc.: 100 mg/mL
Encapsulates aminosteroid NDNMB molecules in 1:1 ratio
Cyclodextrin that noncovalently binds the amino steroid within the sugar ring of sugammadex molecule, preventing amino steroid from binding the ACh receptors, permitting immediate reversal
Sugammadex Class
Selective muscle relaxant and reversal agent
Sugammadex Dosing
Based on TOF:
2-4 TOF: 2 mg/kg --> 1.5 min. reversal
0 TOF 1-2 PTT: 4 mg/kg --> 3 min. reversal
Emergency reversal (3 min. after max Roc intubating dose: 16 mg/kg --> 3 min reversal
Sugammadex Details
Doesn't require anticholinergic co-administration
Minimum wait time of 5 min. if sugammadex 2-4 mg/kg give to give redone of rocuronium 1.2 mg/kg.
If roc is reduced within 30 min. of sugammadex, onset of NMB delayed up to 4 min. and duration of NMB shorted to 15 min.
Dexmedetomidine MOA
Conc.: 4 mcg/mL
Binds with pre- and post-synaptic alpha-2 receptors --> decrease in NE levels --> sedative and analgesic effects
Dexmedetomidine Class
Alpha-2 agonist
Dexmedetomidine Side Effects
Bradycardia, hypotension, dry mouth
Dexmedetomidine Induction Dose
Bolus: 1 mcg/kg 10 min. before maintenance gtt
Awake intubation: 1 mcg/kg IV (then start maintenance gtt)
Dexmedetomidine Maintenance Dosing
0.2-1 mcg/kg/hr
Dexmedetomidine Pharmacokinetics
Onset: < 5 min.
Peak: 20-30 min.
Half-life: 2-3 hours, with almost complete biotransformation
Dexmedetomidine Reversal
Alpha 2 antagonists, such as atipamezole
Atropine MOA
Conc.: 1 mg/10 mL (0.1 mg/mL)
Competitvely antagonizes ACh at postganglionic mACHRs.
Atropine Class
Anticholinergic (antimuscarinic)
Atropine Dosing
Adults for symptomatic brady: 0.5 mg IV repeated q 3-5 min. up to 3 mg (6 doses)
Peds: 0.02 mg/kg IV, 0.02-0.04 mg/kg IM. Max single dose for child of 0.5 mg. Max for adolescent of 1.0 mg.
Atropine Pharmacokinetics
Duration: 2-5 hours
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