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Pcol II quiz 1


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First inhaled anesthetic
Explosive and hepatotoxic
Ethyl ether
Inhaled anesthetic
Explosive and irritating
Largely replaced by halothane
Halothane (Fluothane)
Inhaled anesthetic (1956)
Largely replaced ether
Tends to decrease CO
Resets baroreceptors lower
Depresses respiration
Type I (mild, self-limiting) and Type II (severe, rare) hepatitoxicity
Enflurane (Ethrane)
Inhaled anesthetic
Metabolized to toxic F ion
Smells good
Isoflurane (Forane)
Inhaled anesthetic
Not metabolized to F ion
Causes respiratory depression
Methoxyflurane (Penthrane)
Inhaled anesthetic
Very rapid hepatic metabolism produces F ion
Nitrous oxide
Inhaled anesthetic
Laughing gas used by dentists
Desflurane (Suprane)
Inhaled anesthetic, new
Rapid induction & recovery
Sevoflurane (Ultane)
Inhaled anesthetic, new
Rapid induction & recovery
IV anesthetic
Dissociative anesthesia (causes disorganization)
Works on NMDA receptor at glutamine site
Must be used in soothing environment for adults
Often used for children
Thiopental (Pentothal)
Methohexital (Brevital)
Thiamylal (Surital)
IV anesthetic
Short-acting bartiturates
Etomidal (Amidate)
IV anesthetic
Probably works at GABA receptor
Propofol (Diprivan)
IV anesthetic
Not water soluble, given in oil emulsion
Diazepam (Valium)
Lorazepam (Ativan)
Mitazolam (Versed)
IV anesthetic
Work on modulatory site of GABA receptor
Mitazolam (Versed) is relatively water soluble
Sulfentanil (Sulfenta)
Alfentanil (Alfenta)
IV anesthetic
Opioid analgesics
Inovar = droperidol (Inapsine) + fentanyl (Sublimaze)
Tranquilizer/Neuroleptic + Opioid
Droperidol wears off first
GABA-A receptors
Ionotropic: coupled to Cl channels
Fast and transient response
Most common receptor, is responsible for sedative-hypnotic effect
Contains 6 alpha, 3 beta, 3 gamma, 1 delta, 1 epsilon, 1 pi, and 1 theta isoforms.
GABA-B receptors
Metabotropic: GPCR
GABA-C receptors
Ionotropic: coupled to Cl channels
Slow and sustained responses
Uses of barbiturates
Largely replaced by newer drugs like benzodiazepines.
Sought-after uses: Relief of tension, mental stress, and excessive motor activity
Medical use: Anti-epileptic (long-acting drugs); Adjunct to anesthesia (short-acting)
Barbiturate sites of action
Brain Stem - RAS: main site of action, responsible for arousal
Brain Stem Reticular Formation - calming effect on motor activity
Cerebral Cortex - can be depressed at high doses
Barbiturate mode of action
Non-selective effect: similar to general anesthetics, disruption of funciton (dose-related, no ceiling)
Selective effects: Antagonized GABA-A receptor complex (definite ceiling)
Increase GABA-mediated inhibition by keeping Cl channels open LONGER.
Thiopental (sodium pentothal)
Very lipid soluble
Used for induction of anesthesia
Not very lipid soluble
Chloral hydrate
Non-barbituate sedative/hypnotic
Ethchorvyol (Placidyl)
Non-barbituate sedative/hypnotic
Interacts w/ TCA
Glutethemide (Doriden)
Non-barbituate sedative/hypnotic
Withdrawn from market.
Methylprolon (Noludar)
Non-barbituate sedative/hypnotic
Used mostly in hospital settings
Methaqualone (Quaalude)
Non-barbituate sedative/hypnotic
Withdrawn from market.
Non-barbituate sedative/hypnotic
Simple structure
Used mainly in hospital setting
Unstable compound in heat/light
Meprobamate (Equanil)
Non-barbituate sedative/hypnotic
Produces less respiratory depression in the elderly.
Mechanism of action of ethyl alcohol
CNS effects: specific (increased GABA-induced inhibition) and nonspecific
Uses of benzodiazepines
Sought-after effects: Relief of tension, mental stress and anxiety; Positive feelings of calmness/relaxation
Medical uses: anxiolytic; sedative-hypnotic; premedication and induction of general anesthesia; anti-epileptics and muscle relaxants
Sites of action of benzodiazepines
Brain stem (RAS)
Cerebral cortex
Brain stem reticular formation
Limbic system (involved in anxiety rxn; only site of action different from barbiturates)
Mechanism of action of Benzodiazepines
Work on GABA-A receptor in the presence of GABA to hyperpolarize cells. They appear to phosphorylate the GABA-A receptor so that it has a higher affinity for GABA. This causes Cl channels to open more frequently and allow more Cl into cell.
gamma-2 subunit of GABA-A receptor is necessary for BZD binding and effect.

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