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93 Cards in this Set
- Front
- Back
What is pharmacodynamics?
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The study of the actions and effects of the drug IN the body
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What is the effect of increasing the concentration of agonist in the presence of a non-competitive antagonist
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No effect
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What is Pharmacokinetics?
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The study of the factors that affect concentration of drug in the body: absorption, distribution, metabolism, and elimination
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What are the drug binding proteins in the blood?
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Albumin
Alpha 1-acid glycoprotein |
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What pathways of hepatic metabolism constitute Phase I reactions?
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Oxidation, Reduction and Hydrolysis
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Which pathway of hepatic metabolism constitutes Phase II reaction? What is its purpose
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Conjugation. Another chemical group is added to the metabolite to increase polarity to allow subsequent elimination by the kidney
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What common medication used to treat reflux is not to be given with Diazepam? Why?
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Cimetidine (Tagamet) because cimetidine inhibits the hepatic enzymes that metabolize diazepam, prolonging its effects
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What is Hofmann elimination?
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Spontaneous degradation of drugs at physiologic pH and temperature
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What is the alpha half-life of a drug?
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The fall of 50% of the plasma concentration of a drug secondary to redistribution
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What is the beta half-life of a drug?
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The removal of 50% of the drug from the body via metabolism and/or elimination
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What is the effect of Benzodiazepenes binding to GABA receptors?
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binding to the GABA A subunit increases the inward flow of chloride ions, hyperpolarizing cell membranes and reducing neuronal transmission
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If benzos don't produce analgesia, what good are they?
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Sedation, anxiolysis, anterograde amnesia, muscle relaxation, anti-convulsant
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What is the reversal agent for benzodiazepenes?
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Flumazenil
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Lingering sedative effects of diazepam is due to what?
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1) active metabolites desmethyldiazepam and oxazepam
2) drug accumulation in fat tissues |
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Is midazolam lipid or water soluble?
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Both. Water soluble at pH <4 Lipid soluble at higher pH
This is due to an imidazole ring attached to chemical structure |
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What is the dosing scheme for Midazolam?
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IV: 0.05 to 0.15mg/kg (1-2 mg boluses every few mins)
IM: 0.5mg/kg (max 10-15mg) PO: 0.5-1mg/kg (max 15mg) |
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Why is Lorazepam not used for IV sedation?
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Slow onset and long-acting. Best used as a pre-op anxiolysis the night before
0.05mg/kg (not to exceed 4mg) |
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What is the brand name of Triazolam?
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Halcion (either 0.125mg or 0.25mg tablets)
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How is triazolam different from lorazepam?
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It is very short acting
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What patients would you worry about giving Flumazenil to?
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Epileptic patients (remember, benzos are anti-convulsants)
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How is Flumazenil administered?
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In emergency: 0.5 to 1mg bolus
Normally: 0.2mg initially folowed by 0.1 mg each minute for a total of 1mg |
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Which opioid receptors are responsible for analgesia?
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Mu and Kappa
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What is the most common side effect of Mu receptor agonists?
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Respiratory depression
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Although most opioids are metabolized in the liver, remifentanil is metabolized where?
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By plasma esterases
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Which opioids do not cause histamine release?
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Fentanyl, Remifentanil, Sufentanil, Alfentanil, Nalbuphine
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What is the reason for the decrease in blood pressure seen with opioids?
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Vasodilation.
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Why is morphine preferred for post-operative pain management rather than IV sedation?
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Slow onset and long duration of action
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Which active metabolite of morphine is more potent than morphine and thus is a problem with patients with renal problems?
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Morphine-6-glucuronide
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What is the dosing for morphine?
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1 to 2 mg IV in increments
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What is the dosing for meperidine?
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12.5mg to 25mg IV increments
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What class of drugs when used in conjunction with meperidine produce an excitatory hyperthermic rxn?
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MAOI's
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What makes Meperidine different from the other opioids?
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It is not associated with bradycardia
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Partial agonist activity at the kappa receptor means that meperidine is useful for what postoperatively?
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Reduces shivering post-op
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Why is Fentanyl the drug of choice for IV sedation?
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Fast onset and short duration
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What is the dosing for Fentanyl?
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25 to 50 ug increments towards a total of ~1-2ug/kg
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What is a dangerous effect of large bolus administration of fentanyl?
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Chest wall rigidity (can't ventilate)
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What property of remifentanil make it ideal for use in an infusion technique?
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Very short half time, no cumulative effects
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What type of opioid is nalbuphine?
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It is an agonist-antagonist opioid.
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What is a bad side effect of Naloxone use in patients taking opioids chronically?
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Withdrawal and acute congestive heart failure
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What is the dosing for Naloxone?
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Initially 0.4 to 2mg IV for acute reversal
0.04 mg increments for gradual withdrawal |
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Which barbiturates are used as anticonvulsants? What route?
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Pentobarbital (IV)
Phenobarbital (Oral) |
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Barbiturates are contraindicated in people with what rare blood disease?
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Porphyria
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What is the dosage of thiopental adminstered by IV for GA induction?
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3 to 5 mg/kg
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What is the preparation for methohexital?
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1% solution given at 1.5 to 2mg/kg
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Which patients should you not use methohexital on?
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Patients with seizures. Interesting that you use barbs with patients with seizures
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What would be a reason to use pentobarbital for IV sedation?
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The cardiovascular effects of low BP and tachycardia are more modest.
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What is the dosage used for propofol for deep sedation vs. General anesthesia?
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75-150ug/kg/min vs. 100-300ug/kg/minute.
Lots of overlap indicates lower margin of safety of drug |
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How does propofol reduce blood pressure?
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Centrally mediated vasodilation
Blocks sympathetic tone and blunts the reflex tachycardia that wouldnormally occur |
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Why would propofol be good for asthmatics?
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It has bronchodilatory properties
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Why is an egg allergy not necessarily a contraindication for propofol?
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Because the egg protein is Lecithin and most egg allergies are to egg albumin
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How is etomidate like midazolam?
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Both contain an imidazole ring and are thus both water and lipid soluble depending on the pH of the solution.
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How is etomidate administered?
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At an IV does of 0.2 to 0.4 mg/kg
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What are the main advantages of etomidate has as a sedative?
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Cardiovascular stability (less decrease in BP) and spontaneous respiration is maintained.
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What medical condition is associated with etomidate i continuous infusion doses?
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adrendocortical suppression
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When they describe ketamine as a dissociative anesthetic, what is it dissociating?
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The thalamocortical and limbic systems
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What is the MOA of ketamine?
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non-selective antagonist of N-MDA receptors. These deal with the excitatory neurotransmitter glutamate
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How is ketamine administered?
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1 to 2mg/kg IV
3 to 7mg/kg IM (for GA) or 2 to 3mg/kg IM for sedation |
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Why would you consider using glycopyrrolate if administering ketamine?
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Ketamine increases salivary secretions
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What is the blood:gas coefficient?
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The exten to which the anesthetic gas molecules from the alveolar spaces will dissolve into plasma bfore the plasma is saturated
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Which has a faster onset, a gas with a low or high blood:gas coefficient
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Low. Because once the plasma is saturated, extra gas is free to move across the blood/brain barrier
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What is the equivalent of the ED50 when talking about inhaled anesthetics?
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The MAC. This is the inhaled concentration of the agent required to prevent movement in 50% of patients to a surgical stimulus
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How does halothane differ from the other halogenated agents with respect to the heart?
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Blocks the baroreceptor reflex leading to steep drop in BP at higher doses.
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How does halothane cause cardiac dysrhythmias?
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It suprresses the SA node activity, sensitizes the myocardium to catecholamine (epi) related ventricular dysrhythmias
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Why should fresh gas flows of sevoflurane in particular be kept to at least 2L/min?
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To minimize compound A accumulation in the CO2 absorber
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What color is the N2O gas tank?
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Blue
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What patients should Nitrous use be avoided in due to its ability to enter closed spaces
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Otitis Media, Sinus Infections, Emphysema
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What is the predecessor inhalation agent of the halogenated gases?
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Diethyl Ether
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What is the halogen side chain of the newer gases?
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Fluorine! Does that mean these gases are good for the teeth?
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Where is halothane partially metabolized in the body?
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In the liver
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Coronary steal phenomenon is associated with which gas?
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Isoflurane
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How is the only depolarizing agent administered?
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1-1.5mg/kg IV for induction of anesthesia
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Succinylcholine can cause a rise in what chemical element?
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Potassium, therefore it should be avoided in certain patients
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Which patients should not be administered succinylcholine?
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certain neuromuscular disorders, especially those with pseudocholinesterase abnormalities.
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Which non-depolarizing agent has the fastest onset?
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Rocuronium. Occurs in ~1minute
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Which of the non-depolarizing agents has the 1) longest duration of action? 2) the shortest?
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1) Pancuronium (longest)
2) Mivacurium (shortest) |
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There are 2 classes of non-depolarizing agents. What are they and what is their associated suffix?
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1) Aminosteroids: CURONIUM
2) Benzylisoquinoline:CURIUM |
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Why is the use of atracurium a problem with asthmatic patients?
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Because benzylisoquinolines cause histamine release, with flushing and peripheral vasodilation
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Which class of non-depolarizing agents are associated with increased heart rate?
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The aminosteroids. Bad for people with cardiac problems...
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Which non-depolarizing agent is like succinylcholine and affected by deficiency in pseudocholinesterase?
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Mivacurium (interesting that it also has a shortened duration like Sch)
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AmiNOsteroids and
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CurONium (just flipped backwards. grabbing at straws, but whatever works)
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Which of the non-depolarizing agents are eliminated by Hofmann elimination? What class of drugs do they belong to?
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Atracurium and Cistracurium
Benzylisoquinolines |
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What drugs do you use to reverse the muscle relaxants?
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Cholinesterases paired with anticholinergics to temper the bad side effects of increased ACh
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What are the common cholinesterase/anticholinergic pairings? How are they administered
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1. Neostigimine 0.4-0.8mg/kg with Glycopyrrolate 0.2mg/MG
2. Edrophonium 0.5-1.0mg/kg with atropine 0.014mg/MG |
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What are the 2 types of receptors bound by ACh?
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Nicotinic and Muscarinic
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Anticholinergics specifically block which of the receptors?
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Muscarinic
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Where are the muscarinic receptors found?
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At postganglionic sites of the PARAsympathetic system at the HEART, SALIVARY GLANDS, SMOOTH MUSCLE
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Where are the Nicotinic receptors found?
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At autonomic ganglia and neuromuscular junctions of skeletal muscle
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What is the benefit of using glycopyrrolate instead of atropine or scopalamine?
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Glycopyrrolate cannot cross the blood-brain barrier and thus does not cause sedation
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Central anticholinergic syndrome caused by high doses of the anticholinergics that can cross the blood-brain barrier can be reversed by what?
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The anticholinesterase Physostigmine because it can cross the blood brain barrier?
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Why would anticholinergic system not be a problem with glycopyrrolate?
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Because it cannot cross the blood brain barrier, atropine and scopalamine can though.
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Centrally medicaated nausea is in which part of the brain?
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The medulla, specifically at the chemoreceptor trigger zone
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What drugs beling to the 5-HT3 antagonists? What are they used for?
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Ondansetron and Dolasetron. These are centrally acting anti-nausea medications
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In addition to using dexamethasone as a post-operative anti-inflammatory agent, it can also be used for?
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Antinausea when administered at at least 8mg IV
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