Help
Options
Didn't know it?
click below
click below
Knew it?
click below
click below
Don't Know
Remaining cards (0)
Know
retry
shuffle
restart
0:00
Embed Code - If you would like this activity on your web page, copy the script below and paste it into your web page.
Normal Size Small Size show me how
Normal Size Small Size show me how
Non-Opioids
| Question | Answer |
|---|---|
| The primary inhibitory neurotransmitter in the CNS is ___ | GABA |
| GABA Type A contains ____ glycoprotein subunits which are: ___, ____, ___, ____, & ____ | Five; GABA; barbiturates; benzos; steroids; picrotoxin |
| GABA type A works by increasing transmembrane ____ ____, thereby making the cell become ____ | Chloride; conductance; hyperpolarized |
| Benzos ____ the efficiency of the coupling of GABA to ____ channels, causing hyperpolarization | Increase; chloride |
| Barbiturates and ____ work on the same receptor site and have similar mechanisms of action | Propofol |
| Propofol is ____ at baseline, thus needing other substances (___ & ____) to make an emulsion that can be injected | Insoluble; soy bean; egg |
| The dose of Propofol that can be used to cause unconsciousness within 30 seconds is ____ | 1.5 - 2.5 mg/kg |
| Propfol injection can be painful, therefore ___ can be used | Lidocaine |
| The main mechanism by which Propofol works is through enhancing the activity of ___-activated ____ channels | GABA; chloride |
| Other mechanisms of action of Propofol include the following: ____, ____, & ____ | Blocking ion channels at the nicotinic ACh receptors in the CNS; blocking ion channels in the cerebral cortex; inhibiting the LP signal transduction |
| Propofol is extensively and rapidly metabolized in the ____ to ____ sulfate and ____ metabolites | Liver; inactive; glucuronide |
| The peak effect of Propofol is ___ to ____ seconds | 90; 100 |
| The initial distribution half-time of Propofol is ____ to ____ minutes | 2; 8 |
| The half-time elimination of Propofol is ___ to ___ | 0.5 hrs; 1.5 hrs |
| Propofol readily crosses the ____ and is cleared by the neonatal circulation | Placenta |
| The three main uses for Propofol include ___, ___, & ____ | Induction of anesthesia; maintenance of anesthesia; IV sedation |
| When giving Propofol to the elderly, the dose must be decreased by ___ to ____% | 25; 50 |
| The three main reasons that Propofol is the most commonly used IV agent for induction of anesthesia include: ____, ____, & ____ | Rapid onset; rapid recovery; low incidence of n/v |
| A typical infusion rate for maintaining sedation with Propofol is ____ | 25 - 100 mcg/kg/min |
| The typical infusion rate for maintenance of anesthesia with Propofol is ____ | 100 - 300 mcg/kg/min |
| Three additional uses of Propofol include: ___, ____ & ____ | Anti-emetic; anti-pruritic; anti-convulsant |
| How does Propofol function as an anti-emetic? | Blocks dopamine & serotonin in the area postrema; depresses the CTZ; blocks the vagal nucleus |
| What are the typical sub-hypnotic doses of Propofol that are used to prevent n/v? | Continuous infusion rate of 10 mcg/kg/min for chemo patients & 10 - 15 mg IV for others |
| How does Propofol work as an anti-pruritic and what is the typical dose that is given? | It has an inhibitory effect on the dorsal horn, where epidurals and spinal blocks work. The typical dose is 10 mg IV. |
| The anti-convulsant effects of Propofol are controversial and ___-____ | Dose-dependent |
| What is the dose of Propofol that is used to prevent seizure activity? | > 1 mg/kg IV |
| The main neuro/CNS effects that Propofol exerts are... | Decreased CPP, decreased ICP, decreased cerebral metabolic O2 requirement, burst suppression |
| Burst suppression is characterized by low voltage, high ___ complexes on the EEG | Amplitude |
| What are the main hemodynamic/CV effects that Propofol exerts? | Decreased SBP, decreased MAP, bradycardia, asystole, vasodilation, decreased SNS activity, negative ionotropy, decreased stress response to intubation/LMA |
| The main side effects of Propofol include... | Allergic rxn, bacterial growth (E-Coli & pseudomonas), seizure activity, abuse potential, pain on injection, lactic acidosis |
| How does Propofol cause lactic acidosis? | At infusion rates of 75 mcg/kg/min for greater than 24 hours, the drug makes the person resort to anaerobic metabolism as if they have a mitochondrial abnormality |
| Describe the mechanism of action of barbiturates | They decrease the rate of dissociation of GABA from its receptor and increase the rate at which chloride channels open by directly activating them |
| Thiopental is a competitive ____ at ____ ____ receptors in the CNS | Antagonist; nicotinic; ACh |
| The two most important determinants of distribution of barbiturates are: ____ & ____ | High lipid solubility; blood flow to tissues |
| How much protein binding do barbiturates have? | 72-86% |
| What is pK? | pK is the ionization constant; it is the pH of a drug for which 50% is ionized |
| What is the pK of barbiturates? | 7.6, which is very close to blood pH so it remains ionized |
| ____ favors the non-ionized fraction of barbiturates | Acidosis |
| Methohexital is broken down in the ____ and has water-soluble, ____ metabolites, whereas Thiopental is broken down in the ____ | Hepatocytes; inactive; kidneys |
| Barbiturates are filtered in renal ___ but because of their high protein binding, the magnitude of ___ is limited | Glomeruli; filtration |
| The high ___-___ of barbiturates favors reabsorption into the blood and <1% of most barbiturates are excreted ____ in the urine | Lipid-solubility; unchanged |
| ____ is the only barbiturate that is excreted unchanged in the urine | Phenobarb |
| The renal excretion of Phenobarb can be increased by ____ or ____ ____ | Alkalinization; osmotic diuresis |
| Methohexital has a ___ elimination half-time than Thiopental due to greater ___ ____ | Shorter; hepatic clearance |
| Thiopental has a ____ elimination half-time in obese patients due to greater ___ ____ ____ | Longer; volume of distribution |
| Pediatric elimination half-time of barbiturates is ___ than in adults due to greater ___ ____ | Shorter; hepatic clearance |
| How does increased age affect the passage of Thiopental from central to peripheral compartments? | Older people have a slower rate of intercompartmental clearance, which results in increased plasma concentrations of Thiopental for greater distribution into the brain |
| The four main clinical uses for barbiturates include... | Induction of anesthesia, anti-convulsant, decreasing ICP, sedative/hypnotic |
| Some disadvantages to barbiturates include: lack of ____ of effect in the CNS, ___ therapeutic index than benzos, tolerance, greater liability for ___, high risk of drug ____ | Specificity; lower; abuse; interactions |
| Thiopental was first used in the year ____ before ___ came about in 1989 | 1934; Propofol |
| What is the dose of Thiopental that causes unconsciousness within 30 seconds? | 3 - 5 mg/kg |
| What is the typical dose of Methohexital that is used? | 1 - 1.5 mg/kg |
| Methohexital may cause increased ___ phenomena and is dose-dependent and may be decreased with use of ___ | Excitatory; opioids |
| What is one main reason for using Methohexital over using Thiopental? | For ECT therapy; it creates a better seizure which will ultimately make the patient have a better outcome from the therapy |
| How do barbiturates work to treat increased ICP? | By decreasing cerebral blood flow, decreasing cerebral metabolic O2 requirements, and increasing the perfusion to metabolism ratio |
| Two major side effects to be aware of when administering barbiturates are ___ and ___ | Myocardial depression; hypotension |
| The purpose of the isoelectric EEG is to confirm the ___ barbiturate-induced depression of ____ | Maximal; cerebral metabolic O2 requirements |
| Despite barbiturates' indication for increased ICP, ____ outcomes for head trauma patients has still not been ____ | Improved; observed |
| Describe how barbiturates may help with focal cerebral ischemia | They induce metabolic suppression which exceeds the decrease in cerebral blood flow which may be protective for poorly perfused areas in the brain |
| How do barbiturates work in terms of helping with global ischemia post-cardiac arrest? | It is unlikely because in order for it to work, the EEG must remain active. The EEG is flat about 20-30 seconds after cardiac arrest, so if you are able to give the barbiturate within that time frame it may work. |
| What are the main CV side effects associated with barbiturates? | 10-20 mmHg decrease in BP, 15-20 bpm increase in HR, dilation of peripheral vessels, histamine release, vasodilation of cutaneous vessels |
| Why must you be careful when administering barbiturates to a patient who is hypovolemic? | They are less able to compensate for decreases in BP; make sure the patient has enough volume on board before giving barbiturates |
| What are the main respiratory side effects associated with barbiturates? | Apnea (esp when used with other sedatives & dose-dependent depression of ventilatory centers in pons/medulla |
| What reflexes are still intact when patients are given barbiturates? | Laryngeal and cough reflexes |
| Barbiturates can cause a decrease in ___ blood flow and a moderate decrease in renal ____ ___ and ____ | Hepatic; blood flow; glomerular filtration rate |
| Barbiturates can cause enzyme induction of drugs such as: ___, ____, & ____ as well as endogenous substances like: ___, ___, & ____ | Phenytoin; oral anticoagulants; tricyclics; Vitamin K; bile salts; corticosteroids |
| Barbiturates can cross the ___ within ___ minute of administration but is cleared by the fetal ___ and diluted | Placenta; one; liver |
| What is one major side effect that can occur with barbiturate use? | Intra-arterial injection can cause immediate, intense vasoconstriction, pain, blanching followed by cyanosis and gangrene with permanent nerve damage |
| How is intra-arterial injection of barbiturates treated? | Dilute drug immediately, prevent arterial spasm with Papaverine/Lidocaine, sustain adequate blood flow to extremity with urokinase |
| The five principal pharmacological effects of benzos include: ___, ____, ____, ____, & ____ | Anxiolysis; sedation; anti-convulsant; anterograde amnesia; spinal-cord mediated skeletal muscle relaxation |
| In comparison to barbiturates, benzos are... | Less addicting, less chance for tolerance, greater margin of safety, fewer drug interactions, do not induce hepatic microsomal enzymes |
| The main side effects associated with benzos are... | Drowsiness, decreased motor coordination, impaired cognitive function, anterograde amnesia, suppression of HPA axis, withdrawal, may inhibit platelet aggregation |
| How do benzos inhibit platelet aggregation? | Via inhibition of Phospholipase C and arachidonic acid |
| What are the three main s/s of benzo withdrawal? | Irritability, insomnia, tremors |
| When in a pH of less than 4, benzos become more ___-____; at physiologic pH, benzos convert to a highly ___-____ drug | Water-soluble; lipid-soluble |
| Benzos are rapidly absorbed but have a ___ first-pass effect, approximately ___% | Large; 50% |
| Because of their lipid-solubility, benzos pass readily into the ___ ____ ____, though they are extensively bound to plasma ___ | Blood brain barrier; proteins |
| Benzos are rapidly redistributed and undergo rapid ___ ____ | Hepatic clearance |
| The elimination half-time for benzos is ___ to ___ hours | 1; 4 |
| Elderly and obese patients have a ___ volume of distribution of benzos | Larger |
| Describe how benzos are metabolized | Extensive hepatic metabolism via CYP4503A group; glucuronide conjugates excreted in the kidney |
| Name two drugs that inhibit the metabolism of benzos | Antibiotics (ie: Erythromycin); calcium channel blockers |
| What happens if you give Fentanyl and Midaz together? | They have synergistic effects |
| What are the CNS/neuro effects that benzos exert? | Decreased cerebral metabolic O2 requirements, potent anticonvulsant, cerebral vasomotor response to CO2 is preserved |
| What are the CV side effects associated with benzos? | Decreased systemic BP, but cardiac output is not altered which allows us to give large doses for induction of anesthesia |
| What are the respiratory side effects associated with benzos? | Dose-dependent decrease in ventilation, transient apnea, swallowing reflex can be depressed & upper airway activity can be decreased |
| What are the four main clinical uses for benzos? | Preop medication, IV sedation, induction of anesthesia, maintenance of anesthesia |
| What are the typical preop doses of benzos? | 0.5 mg/kg PO for children; 0.05 - 0.1 mg/kg IM |
| What is the typical benzo dose used for IV sedation? | 1 - 2.5 mg for brief procedures |
| What is the benzo dose used for induction of anesthesia? | 0.1 - 0.2 mg/kg, facilitated with small doses of Fentanyl |
| In terms of maintenance of anesthesia, what other drugs are used in conjuction with benzos? | Opioids, propofol, inhalation agents |
| Diazepam is the ___ used benzo preoperatively taken by mouth for ___ patients | Most-commonly; adult |
| Diazepam is rapidly ___ from the GI tract and reaches peak concentration in ____ hour; there is rapid uptake into the ___ and the volume of distribution is ____ because it is highly ___-____ | Absorbed; one; brain; large; lipid-soluble |
| Though lipid-soluble, Diazepam is extensively bound by ___ and can rapidly cross the ____ | Proteins; placenta |
| Diazepam has a more ___ duration of action when compared to other drugs in its class | Prolonged |
| Describe the metabolism of Diazepam | Metabolized in the liver into two active metabolites; drowsiness returns in 6-8 hours |
| ___ is a drug that can delay Diazepam clearance | Cimetidine |
| The elimination half-time of Diazepam is ___ to ___ hours, while the elimination half-time of its metabolite is ___ to ___ hours | 21;37;48;96 |
| Lorazepam is a ___ potent ___ and ____ than Midazolam and Diazepam | More; sedative; amnestic |
| Lorazepam is conjugated into ___ metabolites and its elimination half-time is ___ to ___ hours | Inactive; 10; 20 |
| When given orally, Lorazepam has ___ absorption and maximal plasma concentration occurs in ___ to ____ hours, and therapeutic levels are maintained for up to ___ to ___ hours | Reliable; 2; 4; 24; 48 |
| The typical dose of PO Lorazepam that is given is... | 50 mcg/kg; dose not to exceed 4 mg |
| What is the typical IV dose of Lorazepam, how quick is its onset of action, and what is its duration of action? | 1 - 4 mg; 1 - 2 minutes; 6 - 10 hours |
| ____ is the benzodiazepine antagonist; it is a ____ antagonist | Flumazenil; competitive |
| What is the usual total dose of Flumazenil that is given for benzo reversal and what is its duration of action? | 0.3 - 0.6 mg; 30 minutes |
| What is the dosing of Flumazenil when given as a continuous infusion? | 0.1 - 0.4 mg/hour |
| What are the four major side effects associated with Flumazenil? | Acute anxiety; hypertension; tachycardia; neuroendocrine evidence of stress response |
| ___ is a very chemically-unique drug in comparison to other sedative agents | Etomidate |
| What is the mechanism of action of Etomidate? | It produces CNS depression via enhancement of GABA-A and augmenting GABA-gated chloride channels |
| The volume of distribution of Etomidate is ___, the drug is ___-soluble and penetrates the brain ____; ___% of it is unionized at ____ pH | Large; lipid-soluble; rapidly; 99; physiologic |
| Peak levels of Etomidate are reached within ___ minute, ___% of the drug is bound to albumin, and it is rapidly metabolized by ____ | One; 76; hydrolysis |
| What are some clinical uses of Etomidate? | Alternative induction agent; potent cerebral vasoconstrictor for TBI patients and lowers cerebral blood flow/cerebral metabolic O2 requirements |
| Why do some people argue that Etomidate may actually active seizure foci? | It may result due to an alteration in the balance between inhibitory and excitatory influences on the thalamocortical tract |
| Etomidate does not typically cause hemodynamic ___ | Instability |
| What is the main limiting factor of Etomidate? | It suppresses adrenocortical function; produces dose-dependent inhibition of the conversion of cholesterol to cortisol which can last 4-8 hours after induction dose; this is why Etomidate should not be given to septic patients |
| Ketamine is a ____ derivative and causes ____ anesthesia which is observed on EEG tracings | PCP; dissociative |
| Not only is Ketamine a dissociative anesthetic, it can also act as an ____ at ___ receptors | Analgesic; Mu |
| The main receptor that Ketamine works at is the ___ receptor; Ketamine acts as a ____-_____ antagonist | NMDA; non-competitive |
| The other receptors that Ketamine may exert effects at include: ___, ___, ___, & ____ | MAO; Muscarinic; voltage-sensitive Na+ and L-type calcium channels |
| Unlike other sedative/hypnotics, Ketamine is not extensively bound to ___ ___ | Plasma proteins |
| Ketamine has a rapid onset and relatively ___ duration of action; it is highly ___-____, making it have a larger ___ of ____ | Short; lipid-soluble; volume of distribution |
| Peak plasma concentration of Ketamine are reached in ___ minute for IV, and in ___ minutes for IM | One; five |
| The elimination half-time of Ketamine is ___ to ___ hours | 2;3 |
| What are the main clinical uses of Ketamine? | Induction of anesthesia; analgesia; sedation for burn patients |
| Describe the analgesic effects of Ketamine | Dose = 0.2 - 0.5 mg/kg IV; targets the thalamic & limbic systems; thought to be greater for somatic than visceral pain; used during labor without depression of neonate |
| Describe Ketamine in terms of its use for induction of anesthesia | Dose = 1-2 mg/kg IV or 4-8 mg/kg IM; return of consciousness in 10 - 20 min; can maintain pharyngeal & laryngeal reflexes |
| What are the main CV side effects associated with Ketamine? | SNS stimulation; increased SBP/PAP/HR/CO & myocardial O2 requirements; platelet aggregation inhibitor; enhances dysrhythmogenicity of epinephrine |
| How does Ketamine inhibit platelet aggregation? | Probably through suppression of IP3 formation and something to do with the Ca2+ concentration in the cytosol |
| Ketamine is questionable in ___ patients since it stimulates sympathetic ganglia, but is a ___ so can be used for asthmatics and is cardiovascularly-stable so can also be used for ____ patients | Questionable; bronchodilator; hypovolemic |
| Ketamine is avoided in patients with ____, _____, & ____ | CAD; pulmonary hypertension; increased ICP |
| What are the CNS/neuro effects associated with Ketamine? | Increased cerebral blood flow/ICP/cerebral metabolic O2 requirements; emergence delirium |
| What kind of drug should you give prior to giving a patient Ketamine? | Benzodiazepine, namely Midazolam |
| What, in terms of sedation, makes Precedex different from other agents? | It resembles physiologic sleep through activation of endogenous sleep pathways |
| How does Precedex cause sedation and analgesia? | Hypnosis via stimulation of alpha-2 receptors in the locus ceruleus and analgesia at the spinal level |
| How can tolerance to Precedex develop? | Tolerance & dependence can develop due to the decrease in cerebral blood flow without changing ICP/cerebral metabolic O2 requirements |
| What are the clinical uses of Precedex? | Short-term sedation in ICU; adjunct to general anesthesia or to provide sedation during regional anesthesia |
| What is the typical loading dose of Precedex that is given, and what is the usual infusion dosing range? | Loading dose: 0.5 - 1 mcg/kg over 10 - 15 min; infusion dose: 0.2 - 0.7 mcg/kg/hour |
| What are the main CV side effects associated with Precedex? | Moderate decrease in HR, SVR, & BP, though bolus doses may increase BP |
| What are the respiratory side effects associated with Precedex? | Small-moderate decrease in TV, small change in RR, upper airway obstruction due to sedation |
| The ___ response to CO2 remains unchanged when Precedex is given | Ventilatory |
| Precedex exerts ____ effects when other sedative-hypnotic agents are given concurrently | Synergistic |
| Precedex undergoes rapid hepatic metabolism and ___; metabolites are secreted in ___ and ___ | Conjugation; urine; bile |
| Precedex has a ___ clearance rate, about ___ to ___ mL/kg/min and the elimination half-time is ___ to ___ hours | High; 10; 30; 2; 3 |
Created by:
SRNADani