CNS Depressants - Quiz 1 (copy)

Hu Lectures

The ideal Inhalation Anesthetic

• nonflammable

• good chemical and metabolic stability

• low incidence of myocardial effects

• low incidence of hepatic and renal damage

• rapid induction and emergence from anesthesia

• adequate skeletal muscle relaxation

• wide margin of safety

*not one drug has ALL properties, combo of agents often used

BGPC

⬇ coefficient (ex: 0.5) = ⬆ gas phase, ⬇ blood (anesthetic will be removed quickly → fast recovery

MAC

minimum alveolar conc.

→ ⬇ (polar) 1% needed to produce = stronger

⬆ the #, the weaker the potency

Lipid Hypothesis of 1899

+original, modification

The Meyer-Overton hypothesis: lipophilic, don’t produce anesthetic? property

Mullins Modification 1953: also related to volume

Protein Hypothesis

GABAa receptors - chloride ion channels

• enhance binding of GABA to receptor

• ex: propofol, midazolam

NMDA (excitatory receptor)

• glutamate

• antagonists:

Name this molecule

+class, formulation

Nitrous Oxide (N2O)

aka laughing gas

gaseous general anesthetics

formulation: inhalation

• need cyclinder!

• N.S. (no skeletal muscle relaxation)

• gas @ room temp.

• good analgesic

• weak anesthetic

• BGPC = 0.47

  • mostly in gas phase

• MAC = 104% (weak potency)

  • extrapoled

• fast effect, fast recovery (no hangover)

Name this molecule

+class, formulation

Cyclopropane

gaseous general anesthetics

formulation: inhalation

• carbon based

• S.R. (skeletal muscle relaxation)

• flammable when mixed w/ O2

  • explosive

• MAC = 17.5%

Name this molecule

+class, formulation

Ethylene

gaseous general anesthetics

formulation: inhalation

• N.S.

• MAC = 80%

• flammable when mixed w/ O2

  • explosive

Name this molecule

+brand, class, formulation

Halothane (Fluothane)

Volatile Liquid General Anesthetics

formulation: inhalation

• NO LONGER USED

• 2-Bromo-2-chloro-1,1,1-trifluoroethane

• ethane derivative

• halogenated alkanes replace H w/ F

• ⬆ halogens, ⬇ burn

• 5 halogens

• b.p. : 50.2*C

• room temp = liquid

• BGPC = 2.5 (favors blood)

• MAC = 0.74%

• rapid induction

Volatile Liquid General Anesthetics (Cont’d)

Volatile - vapor on top of liquid

Liquid - CH3 - CH3 - O - CH3

b.p.: 7.8*C

@ room temp = gas

fluranes = safer → new b.p.:

chiral centers don’t matter bc activity relies on lipophilicity

fluoride tox : sevo >/= en » 180 > des

Name this molecule

+brand, class, formulation

Enflurane (Ethrane)

Volatile Liquid General Anesthetics

formulation: inhalation

• derivative of methylethyl ether

• S.R.??

• b.p. : 58.5*C??

• BGPC = 1.9

• MAC = 1.7%

• acid + ions

Name this molecule

+brand, class, formulation

Desflurane (Suprane)

Volatile Liquid General Anesthetics

formulation: inhalation

• airway irritant, not suitable for

• Ethane, 2-(Difluoromethoxy)-1,1,1,2-tetrafluoro-,(±)-

• b.p.: 23.5*C

• BGPC = 0.42

• MAC = 6%

• EASILY VAPORIZED!!

• WANT TO KEEP IN BOTTLE!!

• < 0.02% metabolism

• rapid induction + emergence

  • can use output

Name this molecule

+brand, class, formulation

Isoflurane (Forane)

Volatile Liquid General Anesthetics

formulation: inhalation

• -Chloro-2,2,2-trifluoroethyl difluoromethyl ether

• different in 10 of halogens compared to Enflurance, Ethrane

• S.R.

• b.p.: 48.5*C

• BGPC = 1.4

• MAC = 1.17%

• potency: halothane > 150 > em > sevo > des (6% MAC)

Name this molecule

+brand, class, formulation

Sevoflurane (Ultane)

Volatile Liquid General Anesthetics

formulation: inhalation

• Propane, 1,1,1,3,3,3-Hexafluoro-2-(flurormethoxy)-

• b.p.: 58.6*C

• BGPC = 0.68

• MAC = 2.05%

• hepatic & kidney tox→

General Side Effects of Volatile Liquid General Anesthetics

+cause, ADEs/: bromide, chloride, fluoride, storage conditions

Side effects are due to halide metabolites

Bromide and Chloride effects

• sensitizes the heart to NE and EPI causing ventricular fibrillation (heart beats faster, gets out of sync, and then stops beating)

• arrhythmia (abnormal heart beat)

Fluoride

• kidney and liver damage due to bioaccumulation

Storage = 15-30°C

Packaging of Fluranes

Color-coded

• sevoflurane = yellow

• isoflurane = purple

• enflurane = orange

• desflurane = blue

Advantages of injectable anesthetics

• no special equipment needed to administer

• many have faster onset than inhaled agents

• rapid recovery; suitable for outpatients

Name this molecule

+brand, aka, formulation

Ketamine HCl (Ketalar)

aka “Special K”

formulation: IV anesthetic

Name this molecule

+brand, formulation

Esketamine (Spravato)

formulation: IV anesthetic

Name this molecule

+aka, formulation

Phencyclidine

aka: “Angle Dust, PCP”

formulation: IV anesthetic

Name this molecule

+brand, formulation

Propofol (Diprivan)

formulation: IV anesthetic

Name this molecule

+brand, formulation

Midazolam HCl (Versed)

formulation: IV anesthetic

Name this molecule

+brand, formulation

Fospropofol (Lusedra)

formulation: IV anesthetic

Name this molecule

+brand, formulation

Remimazolam (Byfavo)

formulation: IV anesthetic

Name this molecule

+brand, formulation

Etomidate (Amidate)

formulation: IV anesthetic

Name this molecule

+brand, formulation

Methohexital Sodium (Brevital Sodium)

formulation: IV anesthetic

Name this molecule

+brand, formulation

Thiopental Sodium (Sodium Pentothal)

formulation: IV anesthetic

Sedative def.

a drug that exerts a calming effect with little to no effect on motor or mental functions

Hypnotic def.

a drug that produces drowsiness and encourages the onset and maintenance of sleep

• resembling as close as possible natural sleep

Anxiolytic def.

a drug that specifically relieves excessive anxiety, a sense of apprehensive expectation that is either appropriate to the situation or excessive

• panic attacks, phobias, etc.

Sedative and hypnotics

+moa, receptors