Med Chem 2 - 04/12 General Anesthetics

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33 Terms

1
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Analgesia

Loss of consciousness

Relax muscles

Reduce reflex

Reversible CNS depression

What are the functions of general anesthetics and basically how does it occur?

2
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Inhaled (volatile liquid, gas)

Inj

What are the types of general anesthetics?

3
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Mostly structurally nonspecific: no specific receptor, activity based on physicochemical props

Highly lipophilic

What are the characteristics of inhaled anesthetics?

4
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NOT USED ANYMORE

Meyer-Overton

Anesthetic action directly related to partition coeff

Mullins

Anesthetic action related to lipophilicity + volume it occupies

Critical volume causes membrane fluidization and ion channel distortion leading to NT depression

What are the lipid hypotheses of general anesthetics?

5
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Anesthetics interact w/ or near inhibitory NT receptors like GABA-A

Explains why anesthetic potency increases to a certain point and then decreases though log P continues to increase b/c size of molecule > receptor pocket

What is the protein hypothesis of general anesthetics?

6
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1: analgesia

2: excitement/delirium w/ amnesia, irregular resp, vomiting

3: surgical w/ regular resp

4: medullary depression w/ resp stop

What are the stages of general anesthesia?

7
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NONE OF HAVE ALL

Nonflammable

Good chem and metabolic stability (dont want toxic metabolites)

Low myocardial effects

Rapid induction and emergence from anesthesia

Low hepatic/renal damage

Adequate SkM relxation

Wide margin of safety

What are the ideal inhaled anesthetic properties?

8
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Blood-gas partition coefficient (BGPC): conc of blood/gas; want low value b/c faster recovery

Minimum alveolar conc (MAC): conc of drug in alveoli needed for 50% of pt to have no motor response as ATM; want low value b/c more potent b/c need less drugs

What are the important parameters of inhaled anesthetics and what do they relate to?

9
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N2O

Cyclopropane

Ethylene

What are the gas inhaled general anesthetics?

10
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Nitrous oxide (laughing gas)

Gaseous inhaled general anesthetic

BGPC: 0.47 (VERY QUICK RECOVERY)

MAC: 104% (LEAST POTENT)

Quick onset and recovery

Very safe

No SkM relaxation

Given w/ other anesthetic

Name?

Type?

MAC?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>MAC?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
11
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Cyclopropane

Gaseous inhaled general anesthetic

MAC: 17% (MOST POTENT GASEOUS)

Quick onset and recovery

SkM relaxation

Explosive

Not used anymore

Name?

Type?

MAC?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>MAC?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
12
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Ethylene

Gaseous inhaled general anesthetic

MAC: 80% (LESS POTENT THAN CYCLOPROPANE)

Quick onset and recovery

NoSkM relaxation

Explosive

Not used anymore

Name?

Type?

MAC?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>MAC?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
13
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Halothane

Enflurane

Isoflurane

Desflurane

Sevoflurane

What are the liquid inhaled general anesthetics?

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Halothane

Liquid inhaled general anesthetic

Prototypical

RACEMIC

BGPC: 2.5 (SLOWEST ONSET)

MAC: 0.74% (MOST POTENT)

BP: 50.2C

Quick onset and recovery

Potent

20% metabolism releasing Br, Cl, F, TFA

TFA: strong acid

Br & Cl: arrhythmias

F: kidney/renal problems

Not used anymore

Name?

Type?

BGPC?

MAC?

BP?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>BGPC?</p><p>MAC?</p><p>BP?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
15
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Enflurane

Liquid inhaled general anesthetic

RACEMIC

Orange cap

BGPC: 1.9 (MORE RAPID THAN HALOTHANE)

MAC: 1.7% (LESS POTENT THAN HALOTHANE)

BP: 56.5C

Quick onset and recovery

Potent

SkM relaxation

5% metabolism releasing Cl, F (< halothane)

F: kidney/renal problems

Cl: arrhythmias

Name?

Type?

Cap?

BGPC?

MAC?

BP?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>Cap?</p><p>BGPC?</p><p>MAC?</p><p>BP?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
16
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Isoflurane

Liquid inhaled general anesthetic

RACEMIC

Isomer of enflurane

Purple cap

BGPC: 1.4 (MORE RAPID THAN ENFLURANE)

MAC: 1.17% (MORE POTENT THAN ENFLURANE)

BP: 48.5C

Quick onset and recovery

Potent

SkM relaxation

0.2% metabolism releasing F, Cl (< enflurane)

F: kidney/renal problems

Cl: arrhythmias

Name?

Type?

Cap?

BGPC?

MAC?

BP?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>Cap?</p><p>BGPC?</p><p>MAC?</p><p>BP?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
17
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Desflurane

Liquid inhaled general anesthetic

RACEMIC

Blue cap (different b/c very volatile)

BGPC: 0.42 (MOST RAPID OF FLURANES)

MAC: 6% (LEAST POTENT OF FLURANES)

BP: 23.5C (LOWEST REQUIRING DIFF CAP)

Quick onset and recovery

Potent

SkM relaxation

<0.02% metabolism (LOWEST)

Airway irritation: not good for prolonged induction, peds

Name?

Type?

BGPC?

MAC?

BP?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>BGPC?</p><p>MAC?</p><p>BP?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
18
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Sevoflurane

Liquid inhaled general anesthetic

ACHIRAL

Yellow cap

BGPC: 0.68

MAC: 2.05%

BP: 58.6C (HIGHEST)

Quick onset and recovery

Very safe

SkM relaxation

Pleasant taste/smell

5% metabolism releasing F

F: kidney/hepatic problems

Usable in peds

Name?

Type?

Cap?

BGPC?

MAC?

BP?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>Cap?</p><p>BGPC?</p><p>MAC?</p><p>BP?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
19
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Halide ADRs

Br, Cl: sensitize myocardium to NE and Epi leading to Vfib, arrhythmias

F: kidney/hepatic damage

Low flammability, enhanced partitioning into lipid layers

What are the advantages/disadvantages of halogenated anesthetics?

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Halothane >> sevoflurane > enflurane > isoflurane > desflurane

What is the comparative ADR profiles of liquid inhaled general anesthetics?

21
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Halothane > isoflurane > enflurane > sevoflurane > desflurane

What is the comparative potency profiles of liquid inhaled general anesthetics?

22
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Halothane > enflurane > isoflurane > sevoflurane > desflurane

What is the comparative recovery profiles (decreasing time) of liquid inhaled general anesthetics?

23
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No special equipment

Many w/ faster onset than inhaled (no absorption)

Rapid recovery (suitable for outpatient)

What are the advantages of IV general anesthetics?

24
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Ketamine

Esketamine

Propofol

Midazolam

Remimazolam

Etomidate

Methohexital

Thiopental

What are the IV general anesthetics?

25
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Ketamine

IV general anesthetic

RACEMIC

C3 drug

NMDA receptor antagonist

Oxidative demethylation to norketamine (1/3 as active but can be greater conc than parent)

Alpha-oxidation then glucuronidation or DB creation

No SkM relaxation

Abuse potential

Hallucinations for 24hrs (similar to PCP)

Dissociative amnesia w/o loss of consciousness

Diagnostic and treatment surgery not requiring SkM relaxation

Name?

Type?

Controlled?

MoA?

Metabolism?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>Controlled?</p><p>MoA?</p><p>Metabolism?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
26
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Esketamine

NASAL SPRAY (recently approved)

S-ketamine

C3 drug

Treatment-resistant depression w/ PO antidepressants

Name?

Type?

Controlled?

Use?

<p>Name?</p><p>Type?</p><p>Controlled?</p><p>Use?</p>
27
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Propofol

IV general anesthetic

Not controlled

Enhance GABA transmission (unsure of exacting binding)

<0.3% unchanged b/c rapid gluc or sulf conjugation

<1min onset

Rapid recovery

Antiemetic properties

SkM relaxation

Needs to be formulated as emulsion b/c very lipophilic which leads to allergies, bacterial growth, etc

Induction/maintenance of anesthesia

ICU

Drug of choice for ambulatory surgery

Name?

Type?

Controlled?

MoA?

Metabolism?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>Controlled?</p><p>MoA?</p><p>Metabolism?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
28
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Fospropofol

IV general anesthetic

Prodrug version of propofol

C4 drug

Enhance GABA transmission (unsure of exacting binding)

Activated by alkaline phosphatase which removes phosphate and triggers OCH2 removal

<0.3% unchanged b/c rapid gluc or sulf conjugation

Rapid recovery

Antiemetic properties

SkM relaxation

INCREASED SOLUBILITY

Slower onset than normal (4 to 8min)

Induction/maintenance of anesthesia

ICU

Drug of choice for ambulatory surgery

Name?

Type?

Controlled?

MoA?

Metabolism?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>Controlled?</p><p>MoA?</p><p>Metabolism?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
29
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Midazolam

IV general anesthetic (can be PO or IM but 10min onset)

Benzodiazepine

C4 drug

Methyl hydroxylation then conjugation

SkM relaxation

Can reverse prolonged activity w/ flumazenil (benzo antag)

Longer onset than propofol, barbs (<5min)

Long recovery (2 to 7hr HL)

Minor sedation, mechanical ventilator sedation

Name?

Type?

Controlled?

Metabolism?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>Controlled?</p><p>Metabolism?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
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Remimazolam

IV general anesthetic

R-enantiomer only

Benzodiazepine

C4 drug

Esterase hydrolysis to COOH to create 300x less active drug

SkM relaxation

Onset >1m (faster than midazolam)

Duration 15m (lower than midazolam)

VERY SHORT ACTING

Induction (inf over 1 min) and maintenance (over 15sec) of procedures <30min

Name?

Type?

Controlled?

Metabolism?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>Controlled?</p><p>Metabolism?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
31
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Etomidate

IV general anesthetic

Not controlled

Ester hydrolysis rapidly

Hypnosis w/in 1min

Lasts only 3 to 5min (VERY SHORT)

Less CV tox

No analgesia

No SkM relaxation

Cardioversion

Very short procedures

Name?

Type?

Controlled?

Metabolism?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>Controlled?</p><p>Metabolism?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
32
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Methohexital

IV general anesthetic

Ultrashort acting barbiturate

C4 drug

<1m onset

C5 branches including DB metabolized: <20min duration

No SkM relaxation

Induction of anesthesia, procedural sedation

Name?

Type?

Controlled?

Metabolism?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>Controlled?</p><p>Metabolism?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>
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Thiopental

IV general anesthetic

Ultrashort acting barbiturate

C3 drug

Can have S=O metabolized to C=O to create less lipophilic + increased duration product (PENTOBARBITAL)

Longer acting than methohexital

No SkM

Replaced by propofol

Name?

Type?

Controlled?

Metabolism?

Advantages?

Disadvantages?

Use?

<p>Name?</p><p>Type?</p><p>Controlled?</p><p>Metabolism?</p><p>Advantages?</p><p>Disadvantages?</p><p>Use?</p>