Pcol II quiz 1
Terms
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- Cyclopropane
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First inhaled anesthetic
Explosive and hepatotoxic - Ethyl ether
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Inhaled anesthetic
Explosive and irritating
Largely replaced by halothane - Halothane (Fluothane)
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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)
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Inhaled anesthetic
Metabolized to toxic F ion
Smells good - Isoflurane (Forane)
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Inhaled anesthetic
Not metabolized to F ion
Causes respiratory depression - Methoxyflurane (Penthrane)
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Inhaled anesthetic
Very rapid hepatic metabolism produces F ion - Nitrous oxide
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Inhaled anesthetic
Laughing gas used by dentists - Desflurane (Suprane)
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Inhaled anesthetic, new
Rapid induction & recovery - Sevoflurane (Ultane)
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Inhaled anesthetic, new
Rapid induction & recovery - Ketamine
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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)
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IV anesthetic
Probably works at GABA receptor - Propofol (Diprivan)
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IV anesthetic
Not water soluble, given in oil emulsion -
Diazepam (Valium)
Lorazepam (Ativan)
Mitazolam (Versed) -
IV anesthetic
Benzodiazepines
Work on modulatory site of GABA receptor
Mitazolam (Versed) is relatively water soluble -
Morphine
Sulfentanil (Sulfenta)
Alfentanil (Alfenta) -
IV anesthetic
Opioid analgesics - Inovar = droperidol (Inapsine) + fentanyl (Sublimaze)
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Tranquilizer/Neuroleptic + Opioid
Droperidol wears off first - GABA-A receptors
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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
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Ionotropic: coupled to Cl channels
Slow and sustained responses - Uses of barbiturates
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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
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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
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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)
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Barbiturate
Very lipid soluble
Short-acting
Used for induction of anesthesia - Phenobarbital
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Barbiturate
Not very lipid soluble
Long-acting - Chloral hydrate
- Non-barbituate sedative/hypnotic
- Ethchorvyol (Placidyl)
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Non-barbituate sedative/hypnotic
Interacts w/ TCA - Glutethemide (Doriden)
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Non-barbituate sedative/hypnotic
Withdrawn from market. - Methylprolon (Noludar)
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Non-barbituate sedative/hypnotic
Used mostly in hospital settings - Methaqualone (Quaalude)
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Non-barbituate sedative/hypnotic
Withdrawn from market. - Paraldehyde
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Non-barbituate sedative/hypnotic
Simple structure
Used mainly in hospital setting
Unstable compound in heat/light - Meprobamate (Equanil)
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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
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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
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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
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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.