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61 Cards in this Set

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516 BARBITUATES
516 BARBITUATES
Thiopental
pH 10.5

Bacteriostatic

Not compatible with acidic drugs.
Refrigerated vs. non-refrigerated life span?
Refrigerated: 2 wks

Non: 1 wk

NOTE: anhydrous: good indefinitely.
What receptors do thiopental act on?
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.
What effect on the sympathetic nervous system does thiopental have?
Decreases transmission
For thiopental, what channel does GABA have direct action on?
Chloride channel
Pharmacology for barbituates
1. lipid solubility
2. protein binding
3. uptake char.
4. redistribution: the cause of quick recovery.
Lipid solubility char of barbituates?
Very lipid soluble. Easily crosses blood brain barrier.
Protein binding char of barb?
High likelihood

Binds albumin

NOTE: albumin binds to basic drugs.
What is the dose, onset, and duration for thiopental?
1. dose: 3-5 mg/kg
2. onset: 30-40 sec
3. duration: 5-8 mins.

NOTE: protein binding: 80%
Metabolism of thiopental?
1. slow
2. via liver
3. no active metabolites
How is the metabolism of methohexital compared to thiopental?
Methohexital is cleared much faster by the liver than thiopental.
What are the clinical uses of thiopental?
1. induction
2. treatment of ICP
3. cerebral protection
What year did propofol come into existence?
1989
How is the pt when he/she wakes up after using thiopental?
Hangover effect due to slow metabolism.
What are the chemical regulation of cerebral blood flow (CBF)?
1. cerebral metabolic rate (CMR).
2. PaCO2
3. PaO2
4. Temp
5. Anesthetic drugs
How does the decrease of CO2 affect cerebral blood flow?
Dec CO2 leads to a decrease of cerebral blood flow.

Therefore, hyperventilate would decrease flow.
Which anesthetic drug does NOT affect cerebral blood flow?
Ketamine

NOTE: ketamine actually RAISES CMR.
How is ICP therapy managed?
1. dec. metabolic O2 requirements.
2. dec. CBF
3. potential for decrease in cerebral profusion pressure
Cerebral protection wrt to global ischemia and focal ischemia?
NOT good for global ischemia

Great for focal ischemia
What are side effects of thiopental?
1. cardiovascular
2. histamine release
3. heat loss
How is the cardiovascular system affected?
Dec. systolic BP

Inc. HR
How is ventilation affected as thiopental's side effect?
Dec. ventilation
Does thiopental cross the placenta?
Yes, no harm comes to fetus.

Succinylcholine is always adm.
What are some reasons not to use thiopental?
1. HANGOVER
2. lower therapeutic index than other benzos.
3. quicker tolerance
4. risk of drug interaction
5. acute intermittent porphyria
Porphyria
Disorders of certain enzymes in the heme bio-synthetic pathway==> PORPHOBILOGEN DEAMINASE.
How is Methohexital compared to thiopental?
1. more lipid soluble than thio.
2. 1-1.5 mg/kg
3. hiccups
What type of liquid does propofol exist as at room temp?
Oil

Insoluble in aqueous soln.
What receptor does Propofol bind to?
Potentiates GABA-a receptor
GABA-a receptor
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.
Onset, duration, and recovery of propofol
1. onset: 30 sec with peak effect at 90-100 sec.
2. duration: 5-10 mins
3. recovery through distribution
Is it allowed to give propofol to pregnant women?
Yes. It does cross the placenta but causes no harm to fetus.
Keep in mind of the age factor
Inc age--> less required
What are the CNS effects due to propofol?
1. CMRO, CBF, and ICP all decrease.

2. Memory: antegrade amnesia
Effects of propofol on cardiovascular?
1. dec BP due to vasodilation effect.
2. HR slightly inc.
Effects of propofol on pulmonary?
RR dec

Vt dec
Effects of propofol on ICP and laryngoscopy?
ICP decreases

Blunts feelings to laryngoscopy.
Side effects of propofol?
1. allergic rxn
2. bacterial growth
3. PAIN on injection
Clinical uses of propofol?
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
What's unique about propofol concerning PONV?
The only drug that doesn't cause PONV.
Solubility of etomidate?
Water soluble in acidic pH

Lipid soluble in blood
What product is inside etomidate that causes the burning?
Glycerol (35%)
Onset and duration of etomidate
Onset: 30 sec

Duration: 3-5 mins

NOTE: peak time is 1 min.
Metabolism of etomidate
Via hydrolysis
What's a positive systemic effect of using etomidate?
CV stability: minimal changes
What are some side effects of using etomidate?
1. pain
2. myoclonus: sudden muscular movement.
3. PONV
4. adrenocortical suppression

NOTE: etomidate inhibits 11-beta hydroxylase enzyme
What are the clinical uses of etomidate?
1. pt with cardiac challenges
2. hypovolemia
3. mask ventilation
Char of ketamine use
1. Class phencyclidine
2. "dissociative anesthesia": can still have unintentional movement
3. ANALGESIC EFFECTS
4. EMERGENCE DELIRIUM: can give benzo to treat this.
What receptor does it work on?
NOT GABA!!!

but on:
1. NMDA
2. Opioid
3. MAO
4. muscurinic
What is the onset time for ketamine?
IV: 30 sec

IM: 3-4 mins
What is the duration for ketamine?
IV: 5-10 mins

IM: 10-25 mins
Clinical uses of ketamine?
Induction
IV and IM doses for ketamine
IV: 1-2mg/kg

IM: 4-8mg/kg
What is the effect of ketamine on ICP?
Both CMRO2 and CBF INCREASE
What is the effect of ketamine on ventilation?
NO depression
Cardiovascular effects of ketamine?
1. BP inc
2. HR inc
3. CMRO2 inc
4. CO inc
5. Myocardial depressant
Who is more susceptible to emergence delirium and what prevent it?
Pt 15+ age

Females

Use benzo's to treat it.
Good reasons for using ketamine?
1. doesn't burn
2. good for children
3. good for asthmatics
Bad reasons for using ketamine?
1. pts with elevated ICP
2. open eye surgery
3. pt with vascular aneurysm
4. psychotic diseases
What are the induction dose duration for propofol, ketamine, and etomidate?
1. propofol: 4-8 mins
2. ketamine: 10-15 mins
3. etomidate: 4-8 mins
Percentages of protein binding for propofol, ketamine, and etomidate?
Propofol: 98%

Ketamine: 27%

Etomidate: 76%