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Pharmacology and Medical Chemistry I > Exam 3 - Lecture 27 & 28 General anesthetics, anxiolytics & sedatives, hypnotic drugs > Flashcards

Exam 3 - Lecture 27 & 28 General anesthetics, anxiolytics & sedatives, hypnotic drugs Flashcards

1
Q

General anesthetics

A

Can induce a state of systemic anesthesia, lack of feeling

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2
Q

Anxiolytics

A

reduce anxiety

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3
Q

Sedatives (tranquillizers)

A

CNS depressants that induce calm

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4
Q

Hypnotics (soporifics or sleeping pills)

A

Typically psychoactive drugs that induce sleep

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5
Q

Modes of Drug delivery Anesthetics

A

Inhalation or injection

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6
Q

What is MAC

A

MAC - Minimum alveolar concentration, equivalent of potency

The lower the MAC, more potent the anesthetic

MAC is ~20% higher in red heads, due to mutations in melanocortin-1 receptor

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7
Q

Moving MAC curve left

A

Hypoatraemia (low sodium), increased age, pregnancy, opioid use, benzo, intoxication

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8
Q

Moving MAC curve right

A

Chronic amphetamine, cocaine, ephedrine, chronic alcohol use, decreased age

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9
Q

MAC: Zur Theorie def Alkoholnarkose Arguments for

A

Simple, diverse structures argues against obvious SAR

Suggest physicochemical mechanisms of action;
Bilayer thickness, curvature, fluidity

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10
Q

MAC: Zur Theorie def Alkoholnarkose Arguments against

A

Stereoisomers have similar oil:gas partition coefficients but different MAC

Many lipophilic drugs are not anesthetics

Change in body temp alter membrane fluidity but is not anesthetic

Changes in chain length increase lipophilicity but not MAC

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11
Q

Using EEG to measure anesthesia?

A

Distinction between anesthesia and sleep

If sleeping you can be arousable but if you’re anesthetized then you are unarousable.

Nonphysiological Oscillations in anesthesia
physiological Oscillations in Sleep

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12
Q

MAC value

A

The lower the better it will cross from Alveoli, into blood and then into Brain.

For example, drug with MAC 0.47 will cross better than one with a MAC of 2.3

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13
Q

Other considerations besides MAC for potency

A

The age and life-style of the patient
How fat
Other medications
Hair color

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14
Q

Blood/Gas partition coefficients and induction/recovery rate

A

The lower the blood/gas partition coefficient, the faster the induction of effect and recovery rate

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15
Q

Effect of isoflurane on Nav Channels

A

Inhibiting Nav channels in CNS neurons reduces excitability

Concentration dependent,

decreasing excitability in the brain

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16
Q

Effects on K2P channels

A

Activating K2P channels in CNS neurons reduces excitability

Open channel = less excitability, decreasing epilepsy and increasing anesthesia effects

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17
Q

K2P channel structure

A

not voltage gated

2 subunits

Subunit made of 4 Transmembrane proteins, 2 P loops

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18
Q

Ether

A

Cheap & easy to make, no longer recommended by WHO

MoA:
Positive Allosteric modulator at GABAa receptor
Agonist at GABAa-receptor at higher dose

Sympathomimetic effect, maintains BP

Side effect:
Post operative nausea and vomiting
Seizures and tremors

V flammable and explosive mixed with Oxygen

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19
Q

Nitrous Oxide

A

Laughing gas, non-flammable roomtemp

MAC >100%

Fast acting, can cause euphoria

MoA:
Weak PAM of GABAa and glycine receptor
Weak activator K2P, blocker NMDA, AMPA, kainite and GABAc

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20
Q

Halothane (fluothane)

A 
MoA:
#1 - Agonist at GABAa receptors
Agonist at glycine receptors
Antagonist at NMDA receptors and Nav channels
Activates K2P channels

Side effect:
Arrhythmia
Respiratory depression
Hepatoxicity (metabolized into trichloroacetic acid = 30-70% mortality)

Not used in US anymore

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21
Q

Isoflurane (forane)

A

Widely used, non explosive

MoA:
#1 Agonist at GABAa receptors
Agonist at glycine receptors
Antagonist at NMDA receptors and Nav channels
Activates K2P channels

side effect:
Cardiac arrhythmia
Respiratory depression

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22
Q

Sevoflurane (Ultane, sojourn)

A

widely used, expensive bc hard to make

MoA:
#1 Positive allosetic modulator at GABAa (and GlyR?) receptors
NMDA receptor antagonist
Activated K2P channels

side effect:
Amongst safest agents available
All gas anesthetics associated with neurotoxicity
Neurodev/behavior abnormalities in kids?

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23
Q

Etomidate change % in BP/Heart Rate

A
  • BP (low, ~2%)/ + Heart Rate
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24
Q

Injectable Anesthetics

A

More potent than gas ones

Not appropriate for long surgery, often used to induce anesthesia

25
Sodium Thiopental
Barbiturate sedative/anesthetic injection Rapid onset (20-45s) and rapid recovery (<10Min) very short acting Used to break status epileptics increases open time of GABAa receptor channels "truth serum", used Euthanasia distributes into greasier tissues due to its greasiness
26
Methohexital (Brevital)
Used for ECT, lowers threshold for seizures but other anesthetics must be used to break seizures Used to induce anesthesia, fast recovery Increase open time of GABAa receptor channels
27
Methohexital (Brevital)
Used for ECT, lowers threshold for seizures but other anesthetics must be used to break seizures Used to induce anesthesia, fast recovery Increase open time of GABAa receptor channels
28
Propofol (milk of amnesia)
Most used induction agent Anti emetic, and anti seizure...often used to break induced seizures or status epileptics MoA: Positive allosteric modulator at GABAa receptors, Nav channel blocker ``` Side effect: Drop BP Cause irregular breathing Pain at injection site Vasodilation - have to give with a drug to bring BP up ```
29
Etomidate
R 10X more potent than S Used in pt where history unclear/ BP is unstable MoA: PAM at B2, B3 GABAa receptors GABAa receptor agonist at higher conc side effect: Adreno-cortical insufficiency = lower cortisone production and more susceptible to infection Paradoxical effect = causes opposite effects of what is usually seen
30
Ketamine
Commonly used Europe for Off-site trauma..not much US MoA: NMDA-R antagonist with low potency effects at many other sites, including nAChRs and d and mORs = reduce excitation Side effect: Altered heart rhythms Hallucination Adverse drug interactions Potential for depression treatment but also drug of abuse
31
Ketamine treat depression?
Ketamine is a dissociative anesthetic - make patient feel removed from their problems
32
Esketamine (Spravato)
metabolite of ketamine MoA: Non-competitive antagonist at NMDA-receptor Suitable for induction in patients with hemorrhagic, anaphylactic or septic shock
33
Why regional anesthesia better?
Cheaper Fewer post-op issues Patient can be fully awake or sedated no risk of general anesthesia Decreased chance of DVT No drug-drug considerations
34
Why regional anesthesia better?
Cheaper Fewer post-op issues Patient can be fully awake or sedated no risk of general anesthesia Decreased chance of DVT No drug-drug considerations
35
Xenon
MoA: Antagonist at NMDA receptor ( no hallucination on emergence) Side effects: Very expensive....recycle?( isn't altered via metabolism) Minimal, including no nausea
36
Methoxycarbonyl - Etomidate
Removes the decrease in cortisone Keeps rapid onset of etomidate Maintain hemodynamic stability of etomidate Rapid metabolism by esterase's into etomidate, causing decrease cortisone later
37
Long acting Benzo
Diazepam Chlordiazepoxide Chlorazepate Flurazepam Long acting = many active metabolite formed
38
Intermediate acting Benzo
metabolized into glucuronides often, not usually active ``` Alprazolam Lorazepam Oxazepam Temazepam Clonazepam Estazolam Quazepam Clobazam ```
39
Short acting Benzo
Hydroxylated and eliminated fast relatively Midazolam Triazolam
40
Alprazolam (Xanax)
Triazolobenzodiazepine - Triazole ring stops it from having same metabolism as diazepam Used for: Anxiety + panic attacks Chemo nausea side effect: Sleepy, depression, memory problems Drug of abuse
41
Diazepam (valium)
classic sedative High chance for abuse and addiction, OD common due to street version of drug Side effect: Can change brainwave patterns, where patient uses it to sleep but then it'll cause worse sleep impair motor function, coordination and balance...in cerebellum
42
Midazolam (versed)
Commonly used in ICU/ critical care med Has diazole ring preventing diazepam metabolism pathway Most hydrophilic BDZ so can be used in saline infusion Used for people on vent, not much anymore Used for deep sedation of patients who are suffering and end of life care. Used as sedative for euthanasia ``` Side effect: Paradoxical reaction Amnesia Tolerance and dependence OD possible ```
43
Mechanism of tolerance/addiction Benzos
Increase GABA signaling decreases receptor density (increase amount internalized or decrease amount brought to membrane) Leads to equilibrium between higher conc of GABA and lower receptors Decrease GABA conc (withdrawal) and GABAergic inhibition of excitability is lost
44
Alcohol Withdrawal syndrome
Minor Withdrawal: Onset 6 - 36 hrs last drink Seizures: Onset 6 - 48 hrs last drink Alcoholic hallucinosis: Onset 12 - 48 hrs Delirium tremens: Onset 48 to 96 hrs
45
Alcohol Withdrawal syndrome treatment
preference is long-lasting benzo (Diazepam) In patients with cirrhosis or acute alcohol hepatitis then Lorazepam is preferred
46
Benzo bind to which subunits
Between alpha and gamma, increase open frequency (number of times open)
47
Barbiturate bind to which subunits
Between alpha and beta, increase amount of time each time it opens
48
Pentobarbital (Nembutal)
Used for euthanasia, Human (execution) and vet Sedative, hypnotic, short term anesthetic Active metabolite of thiopental Potential for OD Street drug - yellow jackets Can give Thiopental, gets metabolized into pentobarbital but then harder to predict how much you are giving in terms of dose
49
Meyer-Overton correlation for anesthetics
The lower the Mac value (more potent) the higher the Oil:gas partition coefficient (more lipophilic)
50
MAC Mechanisms of action
Easier something partitions into brain, faster it works
51
How to measure Mac
Measured at sea level due to pressure After 15 minute equilibration By end-tidal volume of the gas
52
Mac partition
Quickest partition between arterial blood and brain Over time it will leave brain to try and reach equilibrium with other tissues
53
Multimodal
Multiple low affinity receptor targets with complimentary effects
54
Phencyclidine (PCP)
antagonist NMDA receptor Agonist D2 and sigma2 associated with hallucination dissociative anesthetic
55
Thiopental % change in BP/HR
-8%, +14%
56
Methohexital % change in BP/HR
-8%, +15%
57
Propofol % change in BP/HR
-17%, +8%
58
Ketamine % change in BP/HR
+28%, +33%

Pharmacology and Medical Chemistry I (30 decks)

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