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Pharmacology TL > Exam 1 > Flashcards

Exam 1 Flashcards

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1
Q

What are the components of general anesthesia?

A

Unconsciousness, Amnesia, Analgesia, Inhibition of autonomic reflexes, Skeletal muscle relaxation

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2
Q

What properties enhance a compound’s ability to cross a physiologic membrane?

A

High lipophilicity, Low degree of ionization, Low protein binding

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3
Q

What is the general mechanism of action for intravenous anesthetics?

A

Ligand-gated ion channels and lipid mechanisms

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4
Q

Which ligand-gated ion channels are involved in intravenous anesthetics?

A

GABA-type A, Glycine, NMDA (n-methyl-D-aspartate)

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5
Q

What is the relationship between potency and lipophilicity in intravenous anesthetics?

A

Potency is directly proportional to lipophilicity/hydrophobicity

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6
Q

What are the characteristics of GABA and Glycine ligand-gated ion channels?

A

Chloride sensitive, Inhibitory neurotransmitter receptors

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7
Q

Where are Glycine receptors abundant?

A

In the spinal cord and brainstem

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8
Q

Where are GABA A receptors found?

A

In higher brain regions

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9
Q

What are the mechanisms of action for Barbiturates in intravenous anesthetics?

A

Barbiturates act on GABA A, AMPA, kainate glutamate, adenosine, and neuronal nicotinic acetylcholine receptors. They have no activity at glycine or NMDA receptors and enhance and directly activate GABA A modulator receptor agonists.

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10
Q

What is the activity of Barbiturates at glycine receptors?

A

Barbiturates have very weak activity at glycine receptors.

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11
Q

What is the mechanism of action of Etomidate?

A

Etomidate is a selective GABA agonist.

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12
Q

What is the mechanism of action of Propofol?

A

Propofol is a selective GABA agonist.

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13
Q

What is dissociative anesthesia?

A

Dissociative anesthesia includes sedation, immobility, amnesia, marked analgesia, and dissociation from the environment without true unconsciousness.

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14
Q

What are the adverse effects of Ketamine?

A

Hallucinations can occur as an adverse event, especially in adults.

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15
Q

What receptors does Ketamine inhibit?

A

Ketamine inhibits the NMDA subtype of glutamate receptor and neuronal acetylcholine receptors; it has no activity at GABA.

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16
Q

When was thiopental first introduced into practice?

A

Thiopental was first introduced into practice in 1934.

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17
Q

What are the four main groups of barbiturates?

A
  1. Oxybarbiturates 2. Thiobarbiturates (thiopental) 3. Methylbarbiturates (methohexital) 4. Methylthiobarbiturates (very potent, but with marked excitatory effects thus not used clinically)
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18
Q

What is the solubility and pH of thiopental?

A

Thiopental is a pale yellow powder with poor water solubility; it dissolves in alkaline solution of sodium carbonate with a resultant pH of 10.5.

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19
Q

What is the onset of action for thiopental related to?

A

Rapid onset related to rapid uptake across the blood-brain barrier (highly lipid soluble and low degree of ionization at physiologic pH).

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20
Q

What are the uses of thiopental?

A
  1. Induction of anesthesia 2. Maintenance of anesthesia by intermittent bolus or by infusion in combination with analgesics 3. Anticonvulsant 4. Sedation and control of ICP in head injured patients.
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21
Q

What are the drawbacks of thiopental as an induction agent?

A
  1. Extremely irritating if injected outside of vasculature due to high alkalinity 2. Minimal increase in sensitivity to somatic pain.
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22
Q

What are the advantages of thiopental?

A

Minimal cardiovascular depression and cerebral protection during ischemic episodes.

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23
Q

What is the dosing for induction of thiopental?

A

3-5 mg/kg (recovery to awakening occurs within 15-20 minutes); children may require 2-7 mg/kg.

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24
Q

What is the dosing for thiopental as an anticonvulsant?

A

1.5-3 mg/kg and repeated as necessary (3-10 mg/kg/hr).

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25
What is the recovery time for thiopental?
Recovery (t1/2 alpha 2-7 minutes) occurs by decline in blood and brain concentrations due to redistribution.
26
How can thiopental be used for maintenance of anesthesia?
Thiopental may be used for maintenance of anesthesia at 150-300 mcg/kg/min in combination with either nitrous oxide or an opioid.
27
What is Methohexital?
A barbiturate with a better kinetic profile for both induction and maintenance of anesthesia compared to thiopental.
28
What are the dosing recommendations for Methohexital?
Induction—2-2.5 mg/kg; Maintenance—100 mcg/kg/min.
29
What are the drawbacks of Methohexital?
Excitatory movements, pain on injection, predisposition to convulsions, drug/drug binding interactions, and significant respiratory depression when combined with nitrous oxide in opioid premedicated patients.
30
What are the absolute contraindications for barbiturates?
Porphyria, proven allergy to thiopental or other barbiturates, airway obstructions, and history of epilepsy.
31
What is porphyria?
A disruption in the biosynthesis of heme leading to pain, numbness, tingling, paralysis, vomiting, and constipation.
32
What precautions should be taken when using barbiturates?
Marked hypovolemia, cardiovascular collapse, severe uremia, severe asthma, and severe cardiac disease.
33
What is the solubility of Etomidate?
Etomidate is unstable in water and is solubilized in either 33% propylene glycol or as an emulsion.
34
What are the physical properties of Etomidate?
Etomidate has a pH of 8.1, a pKa of 4.2, is a base with 99% of the drug unionized in the blood, and has 75% protein binding.
35
How is Etomidate metabolized?
Metabolism occurs in the liver and via ester hydrolysis in the plasma, with 2% excreted unchanged in the urine.
36
What is the induction dose of Etomidate for adults?
The induction dose for adults is 0.3 mg/kg.
37
What is the induction dose of Etomidate for the elderly?
The induction dose for the elderly is 0.15-0.2 mg/kg.
38
What is the induction dose of Etomidate for children younger than 15 years?
The induction dose for children younger than 15 years of age is up to 0.39 mg/kg.
39
What are the advantages of using Etomidate?
Advantages include cardiostability, reduction of cerebral blood flow, cerebral metabolic rate, and ICP, no release of histamine, low rate of allergic reaction, and minimal respiratory depression.
40
What are the drawbacks or adverse events associated with Etomidate?
Drawbacks include high incidence of nausea/vomiting, pain on injection, thrombophlebitis, excitatory movements, myoclonia, and reversible inhibition of adrenal steroidogenesis.
41
What are the absolute contraindications for Etomidate?
Absolute contraindications include porphyria, depressed adrenocortical activity, and known sensitivity to etomidate.
42
When was Propofol first formulated?
Propofol was first formulated in 1977 in cremophor.
43
What are the physical properties of Propofol?
Propofol is an aqueous emulsion containing soy bean oil and egg phosphatide, with a pH of 7.4, pKa of 11.0, 99.75% non-ionized, and highly lipid soluble. Plasma protein binding is greater than 96%.
44
How is Propofol metabolized?
Propofol is rapidly metabolized to inactive metabolites within the liver by CYP 2C9 and others.
45
What is the typical induction dose of Propofol?
The induction dose of Propofol is 1.5-2.5 mg/kg, but dosing is highly variable and generally titrated to effect.
46
What are the hemodynamic effects of Propofol?
Hemodynamic effects are similar to barbiturates, with profound hypotension possible due to vasodilation, vagotonic effects, and blunted baroreceptor reflex.
47
What ventilatory effects does Propofol have?
Propofol decreases tidal and minute volumes, may cause episodes of apnea, and decreases ribcage and abdominal components.
48
What is the mechanism of Propofol's antiemetic effects?
The mechanism is unknown, but Propofol does not act as an antidopaminergic agent and has been effective in preventing cisplatin-induced nausea/vomiting.
49
What central nervous system effects does Propofol have?
Propofol decreases cerebral blood flow and ICP via vasodilation. It has been used during cerebral aneurysm surgery and has EEG effects such as initial increased beta activity and increased theta activity with unconsciousness.
50
What are some neuroexcitatory events associated with Propofol?
Neuroexcitatory events include opisthotonos, hyperreflexia, hypertonus, involuntary movements, choreoathetosis, and seizure-like activity.
51
What are the cardiorespiratory effects of Propofol?
Rarely, severe bradycardia, sinus arrest, heart block, and asystole may occur, along with depression of pharyngeal reflexes.
52
What are some drawbacks or adverse events of Propofol?
Drawbacks include pain on injection, hypotension/bradycardia, apnea, epileptiform movements, allergic reactions, and Propofol Infusion Syndrome (PRIS).
53
What is Propofol Infusion Syndrome (PRIS)?
PRIS is characterized by cardiac failure, rhabdomyolysis, severe metabolic acidosis, and renal failure, with risk factors including severe traumatic brain injury and prolonged duration of use.
54
What are the absolute contraindications for Propofol?
Absolute contraindications include hypersensitivity to Propofol or related compounds, including soy products, egg products, and sulfite compounds, as well as disorders of fat metabolism.
55
What are the uses of Propofol?
Propofol is used for induction of anesthesia, maintenance of anesthesia, and sedation.
56
What are the dosing guidelines for Propofol?
Induction: 1.5-2.5 mg/kg; Maintenance: 25-50 mg bolus doses or infusion of 4-12 mg/kg/hr; Sedation: initial doses of 0.3-2 mg/kg followed by 25-50 mg boluses.
57
What is Fospropofol?
Fospropofol is a water-soluble prodrug phosphate ester of propofol.
58
What are the peak and sustained levels of Fospropofol after IV administration?
Fospropofol shows lower peak levels and more sustained levels after IV administration.
59
What procedures is Fospropofol ideal for?
Fospropofol is ideal for short duration procedures such as upper endoscopy or colonoscopy.
60
What serum change has been observed with Fospropofol?
A slight rise in serum phosphorous has been seen without clinical sequelae.
61
What is the indication for Fospropofol?
Fospropofol is indicated for monitored anesthesia care in adult patients undergoing diagnostic or therapeutic procedures.
62
What is the onset of action for Fospropofol?
Fospropofol has an onset of action of 2-28 minutes, with a median of 8 minutes.
63
How does the duration of action for Fospropofol compare to Propofol?
Fospropofol has a duration of action of 5-18 minutes (median 5 min), compared to 3-10 minutes for Propofol.
64
What is the time to peak for Fospropofol?
The time to peak for Fospropofol is 12 minutes.
65
What is the half-life of Fospropofol?
The half-life of Fospropofol is 0.85-1.41 hours.
66
How does the elimination of Fospropofol compare to Propofol?
Fospropofol has a single-phase elimination, while Propofol has biphasic elimination (initial 40 min, terminal 4-7 hours).
67
What is the dosing for Fospropofol?
The dosing for Fospropofol is 6.5 mg/kg followed by a supplemental dose of 1.6 mg/kg every 4 minutes.
68
What is the recommended dosing adjustment for elderly patients?
Lower dosing is recommended for elderly patients.
69
What is the weight limitation for Fospropofol dosing?
Dosing is limited to patients who weigh 60-90 kg.
70
What are the most common adverse events associated with Fospropofol?
The most common adverse events are paresthesias (50-75%) and pruritis (8-28%).
71
Where are paresthesias most intense when using Fospropofol?
Paresthesias are most intense in the perineal region, causing burning, tingling, and stinging.
72
What is Ketamine?
Ketamine is a phencyclidine derivative.
73
What are the physical properties of Ketamine?
Ketamine is soluble in aqueous solution, has a pH of 5.6, a pKa of 7.5, is highly lipid soluble with 12-35% protein binding, and is 44% non-ionized at physiologic pH.
74
How is Ketamine metabolized?
Recovery occurs by distribution and metabolism via the CYP P450 system (demethylation and hydroxylation).
75
Does Ketamine have any active metabolites?
Yes, Ketamine possesses an active metabolite—norketamine, which has 30% potency of the parent compound.
76
How is Ketamine eliminated from the body?
Elimination occurs via kidneys as glucuronides with only 2.5% unchanged.
77
What are the uses of Ketamine?
Ketamine is used for induction of anesthesia, maintenance of anesthesia, sedation as a continuous infusion, and analgesia as a continuous infusion.
78
What is the dosing for Ketamine induction?
Induction dosing is 1-4.5 mg/kg IV (2 mg/kg provides anesthesia for 5-10 minutes) or 6.5-13 mg/kg IM (10 mg/kg provides 12-25 minutes of anesthesia for procedures or manipulations).
79
What is the maintenance dosing for Ketamine?
Maintenance dosing is 10-45 mcg/min as infusion.
80
What is the dosing for Ketamine analgesia?
Analgesia dosing is a bolus of 0.1-0.25 mg IV followed by 0.2-1 mg/kg/hr.
81
What are the advantages of Ketamine?
Ketamine is water soluble, has great analgesic properties at subanesthetic doses, can be given intramuscularly, and has less cardiorespiratory depressive effects than other induction agents.
82
What are the drawbacks/adverse events of Ketamine?
Drawbacks include emergence reactions in up to 30% of patients, elevations in heart rate, blood pressure, and ICP, salivation, and postoperative dreaming with vivid hallucinations.
83
How can emergence reactions from Ketamine be minimized?
Emergence reactions may be minimized by co-administration of benzodiazepine or propofol.
84
What are the absolute contraindications for Ketamine?
Absolute contraindications include elevated ICP or intraocular pressure and severe cardiac disease (arterial hypertension, ischemic).
85
What relative contraindications exist for Ketamine?
Relative contraindications include psychotic disorders.
86
What are the miscellaneous caveats of intravenous anesthetics?
Allergic reactions/anaphylaxis are mostly caused by neuromuscular blockers, with an overall incidence between 1/5000 and 1/20,000. More frequently seen with barbiturates and propofol.

Pharmacology TL (8 decks)

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