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Pharm1 Test3 IV Anesthetics

Zaleplon(Sonata), Zolpidem(Ambien), and Eszopiclone(Lunesta) all have similar half-lives(<8 hrs) so that they don't interfere with the next day's activities. What are their relative potencies? Zaleplon(Sonata) potency of 1, Zolpidem(Ambien)potency of 1, and Eszopiclone(Lunesta) potency of 7X.
Zaleplon(Sonata), Zolpidem(Ambien), and Eszopiclone(Lunesta)act similarly to Benzos on the GABA-A receptor complex. How do they act? Bind to specific GABA receptor (alpha-1) subpopulations better and have greater effects on sleep (alpha-2 agonists anti-anxiety and anticonvulsant effects).
Propofol(Diprivan) belongs to a new class of anesthetics, called... 2,6-diisopropylphenol.
How does Propofol(Diprivan) act? Acts by interaction with GABAA receptor, decreasing the rate of GABA dissociation from the receptor.
True or false: Propofol(Diprivan) is fairly selective with few perceivable effects at other receptors. True.
Propofol(Diprivan) is not very water soluble, so it's prepared in an emulsion vehicle which contains what two potential allergens? Soybean oil and egg lecithin(reactions are rare).
True or false: a patient with an allergy to the egg in Propofol(Diprivan) is allergic to the yolk portion. False. It is the white portion.
What does the brand-name Diprivan use as a preservative? Disodium edenate.
What does the generic Propofol use as a preservative? Sodium metabisulfate.
What is a potential problem of the preservative sodium metabisulfate used in the generic Propofol? Patients with sulfite allergies.
What is Fospropofol(Lucedra)? A Propofol prodrug recently approved by the FDA which is cleaved to Propofol on administration by endothelial alkaline phosphatases.
What cleves Fospropofol(Lucedra) to Propofol on administration? Endothelial alkaline phosphatases.
Why does Fospropofol(Lucedra) have no pain on injection? It is water soluble.
Propofol(Diprivan) causes induction in 15-30 seconds. Why should it be administered more slowly than Thiopental? It causes burning on administration.
What two things can we do to reduce Propofol(Diprivan)'s burning on administration? Using a large vein, preadministering 1% Lidocaine.
Why can't we mix Lidocaine and Propofol(Diprivan) in the same syringe? Co-mixing with Lidocaine may increase risk of pulmonary embolism due to breaking emulsion and the formation of soybean oil droplets.
True or false: patients awake faster from Propofol(Diprivan) than those induced with other agents. True.
True or false: patients wake up from Propofol(Diprivan) with a hangover. False. Patients often report an elevated post-op mood.
Why does Propofol(Diprivan) rapidly distribute to the brain? High blood flow.
In addition to being a great IV anesthetic, what are some other benefits of Propofol(Diprivan)? Also possesses antiemetic, antipruritic, and anticonvulsant actions.
Does Propofol(Diprivan) increase pain sensitivity? No.
How does Propofol(Diprivan) decrease BP? Blood pressure is decreased due to decreased cardiac output and vascular resistance.
Why does Propofol decrease BP more than Thiopental? Blood pressure is decreased more than seen with Thiopental by inhibition of sympathetic vasoconstriction.
Use of Propofol has a higher risk of bradycardia-related death. Why? Inhibition of cardiac sarcolemmal calcium release.
Propofol depresses respirations, with apnea reported in what percentage of patients? 30%.
Propofol-induced apnea may be increased with with use of what other drug class? Opioids.
Does Propofol trigger MH? No.
Why are we in a Propofol shortage? One mfg. discovered particulate matter in vials and at the same time, another mfg. recalled vials due to possible microbial contamination (and has not stated when shipments will resume).
What is Propoven? Propofol in a different vehicle formulation – more lipids, but no preservative, so short vial life, approved by FDA.
Propofol pumps utilize syringe infusion pumps. They can be combined with what monitor? Bis.
What are the two anesthetic uses of Propofol? Induction and continuous infusion.
Propofol may be administered as part of a balanced anesthesia plan or alone. It may increase plasma <blank> levels. Triglyceride.
Lactic acidosis has been reported in patients receiving continuous Propofol administration for greater than... 24 hours.
What can be a problem with mixing Lidocaine with Propofol in an attempt to reduce pain on injection? May cause lipid oil droplet formation by breakdown of emulsion and subsequent pulmonary embolism.
Propofol's SE of bradycardia, pain, and hypertriglyceridemia all attributed to... Its lipid emulsion vehicle.
Etomidate(Amidate) has a structure unlike any other anesthetic. What is its MOA? Mechanism believed to be via GABA-activity enhancement like barbiturates and benzodiazepines.
Etomidate(Amidate) is a weak base. What percentage is unionized at physiological pH? 99% unionized at physiological pH.
What is Etomidate(Amidate) mixed with for injection? Propylene glycol.
True or false: Termination of Propofol anesthesia due to redistribution to fatty tissues and metabolism. True.
How is Propofol metabolized? Hepatic and extrahepatic P-450 oxidative metabolism and phase II glucuronide and sulfate conjugation.
True or false: Propofol has high levels of lung cell and is primarily metabolized by lung tissue. False: High levels of lung cell uptake but released mainly unchanged.
What is Propofol's duration of effect? Duration of effect typically 5-10 minutes.
How does Propofol compare to Thiopental? Half life of 2-3 hours, so it does not accumulate as much as Thiopental, and can be used for maintenance by continuous infusion.
How does Propofol affect the fetus? Easily crosses placenta to fetus, but is rapidly metabolized by fetus.
How do liver and kidney disease affect Propofol metabolism? Liver and renal disease do not appear to appreciably affect elimination.
What percentage of Propofol is protein bound? Highly protein bound (95% - 99%).
About what percentage of Etomidate(Amidate) is protein bound? 75%.
True or false. Etomidate(Amidate) has a small volume of distribution. False. Vd is large (tissue distribution).
How long for Etomidate(Amidate) to reach peak brain concentration. Reaches peak brain concentration within one minute following IV administration.
Why does Etomidate(Amidate) have rapid recovery? Rapid recovery due to rapid lipid redistribution and partly due to metabolism.
How is Etomidate(Amidate) metabolized? Metabolized rapidly mainly via hydrolysis of side chain ester group by plasma esterases and hepatic P-450 system.
Etomidate(Amidate)'s induction is as rapid as Thiopental's, with emergence in... 5-10 minutes.
What is Etomidate's elimination half-life? 2-5 hours.
Etomidate has minimal cardiovascular effects, which makes it a better choice than barbiturates or propofol for patients with... Cardiovascular instabilities.
Etomidate has less ventilatory depression than with barbiturates or propofol, however occasional apnea with... Rapid administration.
What percentage of patients experience myoclonus with rapid administration of Etomidate? About 80%.
What is myoclonus? A clonic spasm of a muscle or muscle group.
Why is Etomidate not recommended for long-term use? Depresses steroid (cortisol) synthesis in adrenals.
There is increased risk of Etomidate-induced steroid (cortisol) synthesis depression in what two situations? Sepsis and hemorrhage.
What is an alpha-2 agonist indicated for the control of stress, anxiety and pain? Dexmedetomidine (Precedex).
When used alone, Dexmedetomidine(Precedex) produces sedation with the ability to... Rouse the patient, allowing the medical staff to communicate with the patient if needed.
What is the volume of distribution of Dexmedetomidine(Precedex)? Vd ~ 118 liters.
What is the half-life of Dexmedetomidine(Precedex)? t1/2 ~ 2 hrs.
What is the clearance of Dexmedetomidine(Precedex)? Cl ~ 39 L/hr.
About what percentage of Dexmedetomidine(Precedex) is protein bound? Approximately 95% protein bound.
Metabolism of Dexmedetomidine(Precedex) is almost complete, mainly via... Glucuronidation and P-450 hydroxylation.
The dosage requirements of Dexmedetomidine(Precedex) is unchanged with age, however adjustments may be necessary in patients with... Hepatic disease.
How is Dexmedetomidine(Precedex) administered? Via continuous IV infusion.
What is Midazolam(Versed)? A benzodiazepine with strong hypnotic properties.
What is Midazolam(Versed)'s duration of effects? Duration of effects approximately 15 minutes.
True or false: Midazolam(Versed) is a good amnesiac but significantly drops BP. False. Midazolam(Versed) is a good amnesiac with minimal CV effects.
How much protein binding for Midazolam(Versed)? 95% plasma protein bound (similar to other benzodiazepines).
Ketamine(Ketlar) is used for rapid induction with IV duration of approximately... 15 minutes.
What does Ketamine(Ketlar) do to the CV system? Increases heart rate, cardiac output, and blood pressure.
How does Ketamine(Ketlar) affect pain and memory? It is a good analgesic and amnesiac.
How does Ketamine(Ketlar) work? Blocks glutamate excitatory NMDA receptors in CNS.
Ketamine(Ketlar) is <blank> lipid soluble and has <blank> protein binding. HIGHLY lipid soluble with MINIMAL protein binding.
What is catalepsy? Dissociative amnesia. The appearance of being awake, although patients are unresponsive.
Why should patients who've received Ketamine(Ketlar) be kept in a quiet place upon emergence? It stimulates the CNS in the recovery phase.
What is Ketamine(Ketlar)'s active metabolite? What is it's relative potency? Norketamine. 0.25(25%).
What breaks Ketamine down into Norketamine? P450. It is N-demethylated.
What is the metabolite of Norketamine? Is it active? Hydroxynorketamine. It is inactive.
How is Norketamine broken down into Hydroxynorketamine? P450. It is hydroxylated.
What happens to Hydroxynorketamine? It is glucuronated and excreted in urine.
Ketamine is used for induction and... Maintenance.
What is the nature of the dangers associated with Ketamine? Based on the potential of overdosing the patient and the irrevocable nature of IV administration.
Created by: 1592042303



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