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gen anesthetics
UVa med pharmacology block 2
Question | Answer |
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Isoflurane | Halogenated Ether - anesthesia maintenance - activates GABAa receptors ->incr inhibition Partition coef: 1.4, MAC 1.15, modest solubility sidefx: initial incr RR decr TV->resp depression, incr doses->decr BP, incr HR |
Sevoflurane | Halogenated Ether - anesthesia maintenance - activates GABAa receptors ->incr inhibition part coeff: .6 MAC 2.0 solubility btw iso & des sidefx: same as isoflurane, mild odor |
Desflurane | Halogenated Ether - anesthesia maintenance - activates GABAa receptors ->incr inhibition part coeff .42 MAC 6.0 lowest solubility sidefx: same as Isoflurane, irritates airway, can cause incr BP, tachycardia |
Nitrous Oxide | anesthesia maintenance - inhibs NMDA glutamate receptors-> decr activation Part coeff .47 MAC 101 very low solubility fx: use w/other drugs |
Thiopental | Barbituate for clinical anesthesia - activates GABAa receptor->inhibition fx: can cause significant cardiac depression - action terminated by redistribution |
Midazolam | Benzo for anxiolysis/sedation - activate GABAa receptor->inhibition |
Propofol | General anesthetic - induction for general anesthesia/sedation - activates GABAa receptor->inhibition |
Etomidate | General anesthesia - activate GABAa receptors->inhibition fx: pain on injection, myoclonic mvmnts, decr cortisol/aldosterone synth |
Ketamine | General anesthesia - inhibs NMDA glutamate receptors - causes analgesia, loss of aweareness sidefx: may cause hallucinations, incr salivation |
Characteristics of Desflurane | Very similar to isoflurane Less soluble irritant to airway, can cause hypertension and tachycardia |
True or False: "less solublility means faster onset" Why or why not? | TRUE More solubility would mean that a larger portion of the drugs needs to dissolved before an appreciable tension builds up. |
Which stage of anesthesia is really an overdose? Define this stage. | Stage 4 Depression of vital medullary centers, cardiorespiratory depression |
Which of these is solubility, concentration and which one is tensions? 1) Gas that is truly in solution 2) Gas suspended in microscopic gas phase | 1) Solubility 2) Tension 1 + 2) Concentration |
Charactersitcs of Sevoflurane | Solubility between isoflurane and desflurane Mild odor, good for mask induction |
What is the clinical goal of anesthesia? In terms of stages. Define this stage. | Make duration of stage 2 as brief as possible Stage 2: blockade of inhibitory pathways, facilitation of excitatory transmission --> disinhibtion, excitement, amnesia, irregular respirations, vomiting, incontinence |
What observation suggests that hydrophobic pockets within receptor channels may be the target of anesthesia? | The Meyer-Overton relationship still holds when studying proteins in a lipid-free environment |
What else causes membrane expansion that does not induce anesthesia? | Minor temperature increases |
What is the driving force for partitioning of inhaled anesthetics? What does this mean about their pharmacokinetics? | Driving force is partial pressure NOT concentration, so pharmacokinetics are different from injected drugs |
What do Nitrous Oxide (NO2) and Xe primarly inactivate? | NMDA glutamate receptors |
What is Porpofol's main use? What else can it be used for? | Most commonly used to induce anesthesia Also effective for sedation |
What do halogenated ethers primarily activate? | GABA receptors |
What is the respiratory effect of all inhaled anesthetics? | First, increase respiration and decrease tidal volume Later, respiratory depressions |
How do isoflurane, desflurane, and sevoflurane decrease BP? What does this mean for HR? | The decrease peripheral vascular resistance, thus they INCREASE HR |
Which Barbituate is most commonly used in clinical anesthetia? Dangerous side effect? | Thiopenthal Can cause significant cardiac depression |
Where is immobilization mediated by anesthesia? Where is unconsicousness mediated by anesthesia? What is the evidence? | Immobilization at the spinal cord, unconsciousness at the cerebral level It takes much higher doses to achieve immobilization in response to pain at the cerebral level alone |
How does Ketamine's mechanism of action differ from other IV anesthetics? What side effects can it cause? What can block this side effect? | Acts via NMDA receptor blockade. May cause hallucinations but these are blocks by BDZ's |
What is the current thinking about the interactions of most inhaled anesthetics? | Most interact with membrane lipids and/or proteins |
Characterisitcs of Isoflurane | inhaled anesthetic less used these days, but standard for comparison moderately soluble |
What are the blood pressure of effect of all inhaled anesthetics? When do they occur? | They all decrease BP at HIGHER concentrations |
How does Etomidate compare to thiopenthal? What are some drawbacks of using this drug? | Does not decrease cardiac function as much Pain upon injection, myoclonic movements, and inhibts cortisol and aldosterone synthesis in adrenal cortex |
What is Midazolam primarily used for? | Anxiolysis and sedation |
What are some issues that complicate anesthesia investigation? | - multiple sites of action - different techniques can yield very similar results - no good depth-of-anesthesia measurements - no structure-function relationships |
What are gas concentration, tension, and gas solubitlity analogous to when considering injected drugs (bound to plasma proteins)? | Concentration : total plasma concentration Tension : unbound, free plasma concentration which is the driving force for transport Solubility : degree of protein binding |
Characteristics of Nitrous Oxide. What is a dangerous side effect | High MAC (101%) Requires other drugs (analgesic at lower concentrations) Very low solubility, few hemodynamic effects INACTIVATES METHIONINE SYNTHASE --> can depress bone marrow and fetal tissue at prolonged exposures |
What is the interpretation of the Meyer-Overton relationship? What does this suggest? What evidence supports this suggestion? | For virtually all inhaled anesthetics, when applied at equipotent pressure, a concentration of 70mM is reached in a CNS site with chemical properties resembling olive oil. Suggests direct interaction with neuronal membranes |
How does Halothane decrease BP? What does this mean for its effect on HR? | Depresses myocardial function, so it does not increase HR |
What are the four anesthetic body-compartments and what are their anesthetic characteristics? | 1) vessel-rich (brain, heart,kidney, viscera) 2) Muscle groups (muscle, skin) 3) Vessel poor group (bone, ligament, cartilage) 4) Fat |
How do most INTRAVENOUS anesthetics work? | activate GABA receptors, thus hyperpolarizing neurons and inhibiting their function |
What are the three kinds of anesthesia? What are their characteristics? How are they typically induced? | Gen - unconsciousness, amnesia, immob, analgesia, reflex inhib, skel muscle relax inhalation, intravenous, combo Region-loss of sensation and muscle relax subarach/epidural; periph blockade Local-loss of sensation due to infiltration or topica |