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57 Cards in this Set

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What is pharmacokinetics?
How drug gets to effective site
What is pharmacodynamics?
Drug effect as a result of receptor binding
To which organs do anesthetics first (most rapidly) got to?
1. Brain

2. Heart

3. Kidney
What organs receive drug later on?
Muscle, Fat
What does half life depend on with anesthetics?
Duration of infusion
What happens to elimination time the longer an anesthetic is infused?
Longer it takes to eliminate
Do very fat soluble drugs ever reach steady state?
NO
What are the 4 main induction agents discussed in this lecture?
1. Propofol

2. Etomidate

3. Thiopental

4. Ketamine
What is the major clinical use of propofol?
Induction of general anesthesia
What terminates the effect of propofol after a single dose?
REDISTRIBUTION (not metabolism)
If the "central compartment" increases in size, what will happen to propofol concentration?
It will drop
A drop in propofol concentration do to an increase in central compartment has what practical implication?
Kids need higher doses
What is MOA of propofol?
Potentiates the effects of GABA
What DOESN"T propofol affect?
Pain
What are the cardiovascular effects of propofol?
1. Hypotension

2. Vasodilation
What are the respiratory effects of propofol?
1. Hypopnea/apnea (decreased breathing)

2. Decreased response to hypoxia

3. Bronchodilation
What are the neurologic effects of propofol?
1. Decreased cerebral metabolism --> burst suppression

2. Decreased cerebral blood flow --> brain relaxation
What are the 4 adverse effects of propofol?
1. Pain on injection

2. Propofol related infusion syndrome

3. Pancreatitis

4. Decreased PMN chemotaxis
What are the 2 absolute contraindication to propofol?
1. Allergy to propofol

2. Allergy to egg
Can propofol be used as an outpatient anesthetic?
NO
What makes propofol abused?
Increases dopamine concentration in the nucleus accumbens (like cocaine)
What is the major clinical use of etomidate?
Induction of general anesthesia
What terminates the effect of etomidate after a single dose?
REDISTRIBUTION!
What is etomidate metabolized by?
The liver
What is the MOA of etomidate?
Probably potentiates GABA
Does etomidate effect pain?
NO (like propofol)
What type of suppresion can etomidate cause?
Adrenocortical suppresion
What are the cardiovascular effects of etomidate?
Very few (small hypotension)
What are the respiratory effects of etomidate?
Very few (slight depression)
What are the neurological effects of etomidate?
1. Decreased cerebral metabolism --> burst suppression

2. Decreased cerebral blood blow --> Brain relaxation

3. can cause seizures
What are the 2 main adverse effects of etomidate?
1. Adrenal Suppresion (especially in the critically ill)

2. Increased post-op nausea
What are the 3 relative contraindication to etomidate?
1. Adrenal Insufficiency

2. Critical Illness (especially septic shock)

3. History of post-op nausea
What drug is used in lethal injections?
Thiopental
What type of anesthetic/drug is Thiopental?
Barbiturate
What is thiopental's important clinical use?
Induction of general anesthesia
What is more widely used, propofol or thiopental?
Propofol
What NT do barbiturates potentiate?
GABA and also directly activate ion flow through post synaptic chloride channels in the absence of GABA
What terminates the effect of thiopental after a single dose?
Redistribution!
What is the metabolism process of thiopental?
Hepatic biotransformation --> renal excretion
In what disorder is thiopental contraindicated?
Acute Intermittent Porphyria
What type of kinetics does thiopental exhibit at supratherapeutic doses?
Zero order (constant rate decayed, like alcohol)
What is the MOA of thiopental?
Potentiates GABA
All of the effects (cardiovascular, respiratory, neurological) of thiopental are the same as what?
propofol
What is the exception to the similarity between thiopental and propofol?
Methohexital DECREASES seizure threshold
What are the 4 main adverse effects of thiopental?
1. Garlic/Onion Taste

2. Tissue Necrosis (possibly)

3. Stimulation of porphyrin formation

4. ANTI-analgesic effect
What are the 2 relative contraindications to thipental?
1. Hemodynamic instability (ie shock)

2. Questionable IV access
Ketamine is most like what street drug?
PCP
Which ketamine enantiomer has good clinical effects?
S
What is the metabolism of ketamine?
Hepatic degradation, excretion in urine
What is the primary MOA of ketamine?
NMDA receptor antagonist

But "dirty", also affects other receptor types (GABA, 5-HT, Nicotinic AchR)
In terms of cardiovascular effects, what is postive effect of ketamine?
Retains sympathetic tone so does NOT cause hypotension
What can increase (negatively) with katamine?
ICP
What are the 3 main adverse effects of ketamine?
1. Salivation

2. Dysphoria, dissociation

3. Sympathetic stimulation: tachycardia, hypertension
What are 4 relative contraindications of ketamine?
1. Psychosis

2. Compromised myocardial infarction

3. Inability to tolerate tachycardia, hypertension (ex: carotid dissection)

4. Intracranial hypertension
What are the other 2 important classes of sedative/hypnotics?
1. Benzodiazepines

2. Opioids
Drugs that cause sedation often have what type of effect/activity?
Anti-emetic (nausea/vomiting)
Does ketamine inhibit pain?
Yes