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61 Cards in this Set
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- Back
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516 BARBITUATES
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516 BARBITUATES
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Thiopental
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pH 10.5
Bacteriostatic Not compatible with acidic drugs. |
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Refrigerated vs. non-refrigerated life span?
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Refrigerated: 2 wks
Non: 1 wk NOTE: anhydrous: good indefinitely. |
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What receptors do thiopental act on?
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Act on the GABA-A receptor in the brain and spinal cord.
The GABA-A receptor is an inhibitory channel that decreases neuronal activity. Barbiturates enhance the inhibitory action of the GABA-A receptor. |
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What effect on the sympathetic nervous system does thiopental have?
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Decreases transmission
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For thiopental, what channel does GABA have direct action on?
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Chloride channel
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Pharmacology for barbituates
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1. lipid solubility
2. protein binding 3. uptake char. 4. redistribution: the cause of quick recovery. |
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Lipid solubility char of barbituates?
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Very lipid soluble. Easily crosses blood brain barrier.
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Protein binding char of barb?
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High likelihood
Binds albumin NOTE: albumin binds to basic drugs. |
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What is the dose, onset, and duration for thiopental?
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1. dose: 3-5 mg/kg
2. onset: 30-40 sec 3. duration: 5-8 mins. NOTE: protein binding: 80% |
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Metabolism of thiopental?
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1. slow
2. via liver 3. no active metabolites |
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How is the metabolism of methohexital compared to thiopental?
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Methohexital is cleared much faster by the liver than thiopental.
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What are the clinical uses of thiopental?
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1. induction
2. treatment of ICP 3. cerebral protection |
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What year did propofol come into existence?
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1989
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How is the pt when he/she wakes up after using thiopental?
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Hangover effect due to slow metabolism.
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What are the chemical regulation of cerebral blood flow (CBF)?
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1. cerebral metabolic rate (CMR).
2. PaCO2 3. PaO2 4. Temp 5. Anesthetic drugs |
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How does the decrease of CO2 affect cerebral blood flow?
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Dec CO2 leads to a decrease of cerebral blood flow.
Therefore, hyperventilate would decrease flow. |
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Which anesthetic drug does NOT affect cerebral blood flow?
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Ketamine
NOTE: ketamine actually RAISES CMR. |
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How is ICP therapy managed?
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1. dec. metabolic O2 requirements.
2. dec. CBF 3. potential for decrease in cerebral profusion pressure |
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Cerebral protection wrt to global ischemia and focal ischemia?
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NOT good for global ischemia
Great for focal ischemia |
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What are side effects of thiopental?
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1. cardiovascular
2. histamine release 3. heat loss |
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How is the cardiovascular system affected?
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Dec. systolic BP
Inc. HR |
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How is ventilation affected as thiopental's side effect?
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Dec. ventilation
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Does thiopental cross the placenta?
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Yes, no harm comes to fetus.
Succinylcholine is always adm. |
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What are some reasons not to use thiopental?
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1. HANGOVER
2. lower therapeutic index than other benzos. 3. quicker tolerance 4. risk of drug interaction 5. acute intermittent porphyria |
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Porphyria
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Disorders of certain enzymes in the heme bio-synthetic pathway==> PORPHOBILOGEN DEAMINASE.
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How is Methohexital compared to thiopental?
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1. more lipid soluble than thio.
2. 1-1.5 mg/kg 3. hiccups |
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What type of liquid does propofol exist as at room temp?
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Oil
Insoluble in aqueous soln. |
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What receptor does Propofol bind to?
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Potentiates GABA-a receptor
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GABA-a receptor
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Upon activation, the GABAA receptor selectively conducts Cl- through its pore, resulting in hyperpolarization of the neuron. This causes an inhibitory effect on neurotransmission by diminishing the chance of a successful action potential occurring.
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Onset, duration, and recovery of propofol
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1. onset: 30 sec with peak effect at 90-100 sec.
2. duration: 5-10 mins 3. recovery through distribution |
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Is it allowed to give propofol to pregnant women?
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Yes. It does cross the placenta but causes no harm to fetus.
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Keep in mind of the age factor
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Inc age--> less required
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What are the CNS effects due to propofol?
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1. CMRO, CBF, and ICP all decrease.
2. Memory: antegrade amnesia |
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Effects of propofol on cardiovascular?
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1. dec BP due to vasodilation effect.
2. HR slightly inc. |
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Effects of propofol on pulmonary?
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RR dec
Vt dec |
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Effects of propofol on ICP and laryngoscopy?
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ICP decreases
Blunts feelings to laryngoscopy. |
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Side effects of propofol?
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1. allergic rxn
2. bacterial growth 3. PAIN on injection |
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Clinical uses of propofol?
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1. induction (1-2.5 mg/kg)
2. IV sedation (25-100 mcg/kg/min) 3. GA TIVA (100-200 mcg/kg/min) 4. MAC 5. PONV prophylaxis |
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What's unique about propofol concerning PONV?
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The only drug that doesn't cause PONV.
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Solubility of etomidate?
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Water soluble in acidic pH
Lipid soluble in blood |
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What product is inside etomidate that causes the burning?
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Glycerol (35%)
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Onset and duration of etomidate
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Onset: 30 sec
Duration: 3-5 mins NOTE: peak time is 1 min. |
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Metabolism of etomidate
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Via hydrolysis
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What's a positive systemic effect of using etomidate?
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CV stability: minimal changes
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What are some side effects of using etomidate?
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1. pain
2. myoclonus: sudden muscular movement. 3. PONV 4. adrenocortical suppression NOTE: etomidate inhibits 11-beta hydroxylase enzyme |
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What are the clinical uses of etomidate?
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1. pt with cardiac challenges
2. hypovolemia 3. mask ventilation |
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Char of ketamine use
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1. Class phencyclidine
2. "dissociative anesthesia": can still have unintentional movement 3. ANALGESIC EFFECTS 4. EMERGENCE DELIRIUM: can give benzo to treat this. |
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What receptor does it work on?
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NOT GABA!!!
but on: 1. NMDA 2. Opioid 3. MAO 4. muscurinic |
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What is the onset time for ketamine?
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IV: 30 sec
IM: 3-4 mins |
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What is the duration for ketamine?
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IV: 5-10 mins
IM: 10-25 mins |
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Clinical uses of ketamine?
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Induction
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IV and IM doses for ketamine
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IV: 1-2mg/kg
IM: 4-8mg/kg |
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What is the effect of ketamine on ICP?
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Both CMRO2 and CBF INCREASE
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What is the effect of ketamine on ventilation?
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NO depression
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Cardiovascular effects of ketamine?
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1. BP inc
2. HR inc 3. CMRO2 inc 4. CO inc 5. Myocardial depressant |
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Who is more susceptible to emergence delirium and what prevent it?
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Pt 15+ age
Females Use benzo's to treat it. |
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Good reasons for using ketamine?
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1. doesn't burn
2. good for children 3. good for asthmatics |
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Bad reasons for using ketamine?
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1. pts with elevated ICP
2. open eye surgery 3. pt with vascular aneurysm 4. psychotic diseases |
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What are the induction dose duration for propofol, ketamine, and etomidate?
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1. propofol: 4-8 mins
2. ketamine: 10-15 mins 3. etomidate: 4-8 mins |
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Percentages of protein binding for propofol, ketamine, and etomidate?
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Propofol: 98%
Ketamine: 27% Etomidate: 76% |
