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93 Cards in this Set

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