TDRD Flashcards
So What makes a drug an Ideal Agent?
Hypnosis and amnesia
Rapid onset and rapid metabolism to inactive metabolites
Minimal CV or respiratory depression
No histamine release, non-toxic, nonirritating
No untoward neurologic issues (seizures, myoclonus or neurotoxicity)
Good analgesic, antiemetic and cardio protective
5 rights
Right drug, patient, dose, route, time
Propofol (Diprivan)
Stimulation of GABA, highly lipid soluble
Uses: TIVA, induction, antiemetic qualities, outpatient surgery, endoscopy, MAC
Contraindicated in allergies to eggs, egg products, soybeans or soy products (?)
Pain on injection (Lidocaine: to mix or not to mix)
Can support bacteria
Good up to 12 hours in opened vial
Good for 6 hours after being drawn into a syringe
CV: decrease HR and BP, decreased SVR
Dose dependent respiratory depression
Minimal residual CNS effects
Decrease in CBF and ICP
Protein binding: 97% to 99%
Dosing:
1-2.5 mg/kg IV induction (2 mg); 25-200 mcq/kg/min sedation/maintenance
Pharmacodynamics
Onset: 30 sec
Duration: dose and rate dependent
Elderly:
More sensitive, prolonged effects possibly due to decreased CO and clearance
Children:
Large volume of distribution and quicker clearance (may need larger dose)
Obese:
Base dosing on lean body weight
Chronic Alcoholism? CV Disease?
Lidocaine
Dose: 0.5-1.5 mg/kg (adjusted dependent on the patient)
Older adults: 0.5-1 mg/kg
- Hemodynamically unstable: keep less then .5mg/kg
- Keep it on the lower side if they are less than 60 kg (?)
Administered to:
- Suppress the coughing reflex during laryngoscopy and intubation
- Reduce airway responsiveness to noxious stimuli
- Reduces pain caused by IV injection agents
It might increase the hypotensive effects of sedative-hypnotic agents
Careful in cardiac patients
Ketamine (Ketalar)
Noncompetitive NMDA receptor antagonist that blocks glutamate
Stimulates SNS: inhibits the re-uptake of Norepinephrine, dissociative anesthetic
Indications: induction, sedation, CV collapse, sedation for mentally challenged, “bad” epidural/spinal
Effects:
Intense analgesia (review the opioid receptors)
CV: increase in BP, HR, CO, PAP, CVP, CI
Respiratory: minimal depression, maintains upper airway reflexes, increased oral secretions (Glyco), bronchodilator
Emergence delirium: low lights, quiet room, VERSED
Increases in ICP?
Phencyclidine derivative, hallucinogenic, use VERSED
Norketamine is an active metabolite, 1/3 to 1/5th as potent as Ketamine
Dosing
Induction: 1-2 mg/kg IV, 4-5 mg/kg IM, titrated for effect
In Low doses it can be opioid sparing
Pharmacodynamics
Onset: IV in 30 sec; IM in 2-4 min
Duration: 10-15 min (IV), 15-25 min (IM)
Can use Ketamine in Bronchospastic Patients
**Know it*
Thiopental (Pentathol)
Introduced in 1934
No longer available in the United States or elsewhere
Short acting barbiturate, activates GABA
Uses: Sedative, hypnotic, anticonvulsant, treatment of ICP (neuro cases), induction of anesthesia
Effects:
Hypotension
Decrease in CBP and ICP
May increase N/V
Some histamine release
500mg vial
Contraindicated in:
Acute Intermittent Porphyria or Variegate Porphyria
Status Asthmaticus
Protein Binding: 72%-86%
Avoid extravasation necrosis
Dosing:
Induction: 3-5 mg/kg IV in adults
Pharmacodynamics
Onset: 30-60 sec
Duration: 5-30 min
Hepatic metabolism
Etomidate (Amidate)
Ultrashort-acting nonbarbiturate hypnotic, depresses RAS
Uses: induction, procedural sedation
Effects:
Minimal CV effects, decrease in CMR, CBF, ICP
Respiratory depression
Potential for increased N/V and pain on injection (per Dr. Havenstein and Crosse??????). WHY can it burn? glycerol
Myoclonic movements can be decreased with opioids
Temporary Adrenocortical suppression limits long-term use
Protein Binding: 76%
Dosing:
Induction: 0.2-0.3 mg/kg
Pharmacodynamics
Onset: 30-60 seconds
Hepatic enzyme and plasma esterase hydrolysis
Dexmedetomidine (Precedex)
Highly selective, potent central acting Alpha2 adrenergic agonist, results in inhibition of norepinephrine release
Uses: procedural sedation, analgesia, awake fiberoptic intubation, postop sedation, pediatrics
Effects:
Bradycardia, sinus arrest and hypotension (tx with atropine, ephedrine and volume)
Dose dependent analgesia, anxiolysis and sedation with minimal respiratory depression
Protein Binding: 94%
Dosing RANGES:
Procedural sedation: 0.5 -1 mcg/kg over 10 min: infusion .3-.7 mcg/kg/hour
Awake Fiberoptic intubation: 1 mcg/kg over 10 min: infusion 0.7 mcg/kg/hour until intubated
Pharmacodynamics
Onset: 5-10 min; peaks in 15-30 min
Duration: 60-120 min (dose dependent)
Hepatic metabolism
Urinary excretion
Methohexital (Brevital)
Rapid Ultrashort-acting barbiturate, enhances effects of GABA
Uses: ECT(gold standard), ENDO, very short procedures
Effects: deep sedation, skeletal muscle hyperactivity, pain on injection
Must be reconstituted into a 1% (10mg/cc) solution for intermittent IV use
Shortest acting barbiturate and does NOT have anticonvulsant activity (lowers the seizure threshold)
Great for Electroconvulsive Therapy
Pharmacodynamics
Dose: 1-1.5 mg/kg
Onset: < 1 min
Duration: 5-7 minutes
Hepatic metabolism
Urinary Excretion
RAPID redistribution
What are 3 ways to cause muscle relaxation?
Regional, neuromuscular blocker, inhalational anesthetic
Neuromuscular blockers listed
Depolarizing – succinylcholine (Anectine, SCH)
Nondepolarizing:
Rocuronium (Zemuron)
Vecuronium (Norcuron)
Pancuronium (Pavulon)
Benzylisoquinolines:
Mivacurium (Mivacron)
Atracurium (tracrium)
Cisatracurium (Nimbex)
Depolarizing Relaxant
Succinylcholine (suxamethonium, Quelicin, SCH or Anectine) (200mg - 20mg/ml)
Binds to 2 alpha subunits of nicotinic cholinergic receptors, allows sodium and calcium influx, potassium efflux, resulting depolarization of muscle
Remains depolarized until SCH diffuses away from receptor
Mimics action of Acetylcholine (AcH)
Uses: rapid muscle relaxation, routine intubation, very short cases, OB, RSI, Laryngospasm
What you should know about SUX!
Can cause Hyperkalemia
Triggering Agent for Malignant Hyperthermia
Minimal Histamine release
Decrease HR due to muscarinic stimulation
SCH apnea/Psuedocholinesterase Abnormality
Phase I normally
Phase II block from large or repeated doses
Fasciculation’s can cause muscle pain Postop
In children, increased risk of increased K and cardiac arrest from undiagnosed myopathies
Metabolism:
Butyrylcholinesterase (synthesized by the liver and found in the plasma) also called plasma cholinesterase
SCH diffuses away from the NMJ, hydrolyzed in the plasma by plasma cholinesterase
Decreased levels of pseudocholinesterase can prolong the block (pregnancy, liver disease)
Succinylmonochline is a weak active metabolite
Dosing:
1-1.5 mg/kg IV for rapid sequence, 2 mg/kg IV in smaller children, 3-5 mg/kg IM, 20 mg IV for laryngospasm
Onset: 30-60 sec IV, 2-5 min IM
Duration: < 10 min IV, 10-30 min IM
Drug errors? most common pic
Misc biggest category …Succinylcholine 17.1% , inhalational 13.2, opioids, local,
Malignant Hyperthermia
Succinylcholine, inhalational anesthetics - releases Ca++ - sarcoplasmic reticulum, Mutations in the RYR1 gene (ryanodine receptor)- increased ETCO2
Nondepolarizing Relaxants intro
Compete with/block Ach at the nicotinic receptor alpha subunits on motor endplate inhibiting depolarization
Uses: Muscle Relaxation for surgery, intubation
Aminosteroids
Primarily liver breakdown, kidney excretion, minimal histamine release, highly ionized at physiologic pH, small volume of distribution, limited lipid solubility
Potential for allergic reactions
Nondepolarizing Relaxants
Rocuronium (Zemuron)
Rocuronium (Zemuron) (50mg/100mg vials, 10mg/ml)
Intermediate action, rare histamine release, no effect of BP or HR, can be used to defasciculate with SUX
Dose:
0.6/1.2 mg/kg (higher dose for RSI and lower dose for routine intubation/surgical relaxation)
5 mg for defasciculating dose with SUX
Maintenance/Repeat dose of 0.1-0.2 mg/kg as needed
Pharmacodynamics
Onset: 1-2 min depending on dose
Duration: about 30 min
Eliminated primarily by the liver
Nondepolarizing Relaxants- Vecuronium
Vecuronium (Norcuron) (10mg 1mg/ml)
Intermediate NMB, no histamine release, cardiac stable, might precipitate with Thiopental
Dose:
Induction/intubation: 0.08-0.1 mg/kg
Pretreatment/priming with 10% of intubation dose Maintenance for surgical relaxation: 0.01 mg/kg
Pharmacodynamics
Onset: 2-3 min (good intubating conditions); 3-5 min (maximal blockade)
Nondepolarizing Relaxant- Pancuronium
Pancuronium (Pavulon) (10mg - 1mg/ml)
Long acting, no histamine release, modest tachycardia due to antimuscarinic stimulation, norepinephrine release and reduced uptake of norepinephrine by adrenergic nerves
Increase in BP, careful in any patient that will not tolerate increase HR and cardiac output
Dose:
Initial: .08-.12 mg/kg
Maintenance: 0.01 mg/kg
Pharmacodynamics
Onset: 2-3 min
Duration: 60-100 min
Benzylisoquinolines Intro
Hofmann Elimination
Ester hydrolysis
Plasma cholinesterase metabolism
Histamine release
Some changes to BP and HR
Hofmann Elimination
Spontaneous, non-enzymatic, non-organ dependent chemical breakdown at physiologic temperature and pH
Temperature increase and pH increases……. Increased metabolism
Temperature decreases and pH decreases……. Decreased metabolism
Benzylisoquinolines- Mivacurium (Mivacron)
10mg/20mg vial 2mg/ml -
HISTAMINE RELEASE when given quickly
Spontaneous recovery from the block is rapid
Metabolism:
Hydrolysis by plasma cholinesterase
Dose: .15-.2 mg/kg (intubation) 4-10 mcg/kg/min infusion
Pharmacodynamics:
Onset: 1 min
Duration: 10-20 minutes
Benzylisoquinolines- Atracurium (Tracrium)
50mg 10mg/ml
Intermediate acting, Hofmann Elimination and nonspecific ester hydrolysis, small histamine release, minimal change in BP
Primary metabolite is Laudanosine, which can produce rare seizure activity (tertiary amine)
Dose: 0.3-0.6 mg/kg
Pharmacodynamics
Onset: 2-3 minutes
Duration: 20-35 min, 95% recovery in 60-70 min
Benzylisoquinolines - Cisatrcurium (Nimbex)
20mg 2mg/ml
Intermediate/long acting, predominantly Hofmann elimination, NO histamine release, NO changes in BP/HR
Dose: 0.1-.15 mg/kg IV
Onset: 2-3 min, peaks in 3-5 min
Duration: 40-70 min; 20-35 min to begin recovery: up to 93 min for 90% return