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Dave Vaness Pharmacology Review
Dave Vaness Pharmacology Review
76
Medical
Graduate
07/19/2015

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Term
Tolvaptan works to treat symptoms of congestive heart failure related to hyponatremia, hypervolemia by
Definition
acting as a competitive vasopressin II antagonist. It assists in diuretic therapy and is not associated with hypokalemia or hypotension! And with no kidney dysfunction. Avoid in liver disease patients.
Term
An agonist action on the kappa receptor will result in what Sx
Definition
1. dyphoria
2. Negative regulation against ADH
3. resp depression
4. meoisis
5. hallucinations
6. constipation
Term
describe the occupancy theory about receptors
Definition
t is based on mass-action kinetics and attempts to link the action of a drug to the proportion of receptors occupied by that drug at equilibrium.[9][10] In particular, the magnitude of the response is directly proportional to the amount of drug bound, and the maximum response would be elicited once all receptors were occupied at equilibrium
Term
benefits of etomidate at induction are
Definition
1. maintenance of cerebral perfusion pressure while also decreasing CBF and decrease CRMO2
2. Minimal ventilatory depression
3. Minimal hemodynamic changes
4. No histamine release
5. Short acting and fast onset
Term
what are the benefits of clevidipine
Definition
1. highly selective to vascular smooth muscle
2. Near NO effect on cardiac myocyte and does not cause coronary steal syndrome
3. Almost entirely metabolized by blood esterases so can be safe in liver and renal failure patinets
4. IV only
5. E1/2 1 minute
Term
which local anesthetics have intrinsic abilities to produce vasoconstriction
Definition
cocaine and mepivicaine
Term
What is vasoplegic syndrome and what kind of patients may you see this the most
Definition
A massive drop in SVR with high CO and BP that is refractory to any pressors. Seen most commonly in cardiac surgery patients but also SEEN WITH PTS ON ACE-I.
Term
the normal blood pressure is maintained by what three systems in the body
Definition
1. Sympathetic nervous system
2. Renin-Angiotensinogen & aldosterone System
3. vasopressinergic system
Term
refractory hypotension can be treated with what dose of vasopressin.. then start an iv gtt at a rate of?
Definition
Bolus 0.5 units of vaso then start a gtt at 0.03 units/min
Term
primary means of roc elminiation is via
Definition
biliary elimination of unchanged drug
Term
plasma cholinesterase will metabolize what three drugs we commonly use
Definition
1. sux
2. mivatracurium
3. chloroprocaine
Term
explain the effects of opioids on endocrine function in the body long term
Definition
1. increase TSH
2. Decrease Prolactin
3. Decrease Gonadtropin relaeasing hormone.
Term
how does precedex work
Definition
Alpha 2 agonist in the locus coernelus produces sedation and analgesia is achieved in the dorsal horn of the spinal cord to modulate release of substance p
Term
what is fospropofol and how does it work
Definition
it is a prodrug converted to propofol by alkaline phosphatases.
Term
The route of administration associated with the lowest degree of bioavailability
Definition
intrathecal

By definition, intravenous administration is associated with 100% bioavailability. Intramuscular and sublingual administration is associated with 60 - 100% bioavailability. Intrathecal administration circumvents the blood-brain barrier, but is associated with very low overall bioavailability.
Term
what antiarrythmic is associated with respiratory insufficiency
Definition
Respiratory insufficiency has been associated with the administration of: amiodarone

Pulmonary disease from amiodarone occurs with 5 - 15% prevalence and takes the form of chronic interstitial pneumonitis, organizing pneumonia, ARDS or a solitary mass of fibrosis.
Term
The central nervous system effects of nitrous oxide include
Definition
The central nervous system effects of nitrous oxide include: a decrease in cerebrovascular tone, an uncoupling of CBF and (CMRO2)

Nitrous oxide decreases cerebral vascular tone significantly and increases CMRO2. Since the increase in CMRO2 exceeds the elevation in CBF there is an uncoupling of these parameters. Mild hyperventilation can attenuate the increase in CBF that accompanies the use of nitrous oxide.
Term
Actions produced by opiate agonistic action on the kappa receptor include
Definition
Actions produced by opiate agonistic action on the kappa receptor include: (Select 3) analgesia, inhibition of ADH release, antishivering
Term
risk factors for propofol infusion syndrome (PRIS)
Definition
Risk factors include young age, doses greater than 4 - 5 mg/kg/hr, critical illness and an infusion duration greater than 48 hours.
Term
propofol infusion syndrome Symptoms include
Definition
propofol infusion syndrome Symptoms include severe metabolic acidosis, bradycardia and refractory heart failure.
Term
The propofol infusion syndrome (PRIS) results in damamge where
Definition
The propofol infusion syndrome (PRIS): results in cardiac and peripheral muscle necrosis
Term
the primary mechanism of action of nitroglycerin is
Definition
Relief of anginal pain by nitroglycerine is primarily the result of: decreased preload and cardiac work

Nitroglycerine causes venodilation and a resultant decrease in preload. Its primary mechanism of action in the relief of angina is a decrease in preload and cardiac work.
Term
Drug X is quickly distributed to the total body water of a 70 Kg patient. The estimated volume of distribution (Vd) is drug X is:
Definition
Drug X is quickly distributed to the total body water of a 70 Kg patient. The estimated volume of distribution (Vd) is drug X is:
(Enter numerical answer in box below. Click 'Next' when completed.): 0.6 L/Kg

The typical Vd, normalized for the body weight of a 70 Kg adult, would be the quantity of total body water (42 L) divided by the body weight (70 kg). This results in a Vd of 0.6 L/Kg.
Term
Stimulation of opioid receptors has been shown to do what intracellularly via its receptor
Definition
Stimulation of opioid receptors has been shown to: inhibit adenylate cyclase in the cell

Opioid receptors are GPCRs and inhibit the activity of adenylate cyclase inside cells. This causes in a decrease in intracellular cAMP, which decreases conductance of the voltage-gated calcium channels and open potassium channels, resulting in decreased neuronal activity.
Term
Pharmacokinetic and pharmacodynamic properties of etomidate include:
Definition
hydrolysis by plasma esterases, minimal hemodynamic changes with induction, adrenocortical suppression with induction doses
Term
describe etomidate propertieis
Definition
Etomidate is rapidly metabolized by hepatic microsomal enzymes and plasma esterases. However, rapid redistribution accounts for its extremely short duration of action. The primary clinical advantage of etomidate is the hemodynamic stability upon induction. Adrenal hormone levels decrease for up to 24 hours after etomidate administration, largely as a result of 11β-hydroxylase inhibition.
Term
The graded dose-response curve has a ___ shape
Definition
The graded dose-response curve has a: hyperbolic shape
Term
local anesthetics with vasoconstrictive include 3x
Definition
Vasoconstrictive properties are associate with use of: (Select 3) cocaine, lidocaine, ropivacaine
Term
A 23-year-old man is undergoing a thoracotomy for resection of blebs. He is currently has a 500 mL pneumothorax present. If the patient is anesthetized with an anesthetic of desflurane with nitrous oxide and oxygen in a 2:1 ratio, the resultant volume of the pneumothorax will approach:
Definition
1500 mL

VF/VO = 1/ (1-F N20)
Term
The chemical interaction of sevoflurane with desiccated soda lime has been associated with
Definition
The chemical interaction of sevoflurane with desiccated soda lime has been associated with: anesthesia machine fires
Term
Causes of increased pseudocholinesterase activity include
Definition
1. Thyroid disease
2. nephrotic syndrome
3. obesity
4. cognitively impaired children.
Term
Characteristically, drugs with large volumes of distribution are
Definition
Characteristically, drugs with large volumes of distribution are: lipid soluble with little protein binding

Drugs that are free, unbound to plasma proteins and lipid soluble easily cross membranes to tissues and therefore have large calculated volumes of distribution with low plasma concentrations.
Term
repetivie dosing of demerol can cause seizures due to
Definition
Its neurotoxic active metabolite called normeperidine. Repetitive dosing of meperidine can cause accumulation of normeperidine, which may precipitate tremulousness, myoclonus, and seizures.

pg. 1621
Term
describe ketamine
Definition
Ketamine noncompetitively inhibits the NMDA receptor in the brain producing amnesia and a profound analgesic state. It inhibits tumor necrosis factor-alpha and interleukin-6, accounting for its antiinflammatory action. Ketamine is metabolized by hepatic microsomal enzymes. It increases CMRO2, CBF and ICP. Ketamine causes a centrally-mediated increase in sympathetic tone with an increase in heart rate and blood pressure. It increases pulmonary compliance in patients with bronchospastic disease.
Term
explain vasoplegic syndrome
Definition
Vasoplegic syndrome (VS) is defined as unexpected refractory hypotension resulting from low systemic vascular resistance. The incidence of VS in surgical patients may be as high as 50% in persons receiving renin-angiotensin system antagonists.
Term
The therapeutic safety margin of a drug is defined as the:
Definition
The therapeutic safety margin of a drug is defined as the: lethal dose in 1% divided by the effective dose in 99% of the population

The effective dose 99% (ED99) and lethal dose 1% (LD1) identify the therapeutic safety margin of a drug. The lower the margin of safety of a drug, the more likely toxic effects will be seen.
Term
absoprtion of local anestehtics generally occurs in order from greatest to least with the following...
1. intercostal block
2. sciatic femoral block
3. brachial plexus block
4. epidural block
5. caudal block
6. interp leural block
7. subcutaneous block
Definition
Excluding blocks of the airway, the absorption of local anesthetics generally occurs in the following order of rapidity: interpleural block > intercostal block > caudal block > epidural block > brachial plexus block > sciatic-femoral block > subcutaneous blocks.
Term
The greatest degree of inhaled anesthetic metabolism is seen with the use of which agent
Definition
The greatest degree of anesthetic metabolism is seen with the use of: sevoflurane

Although approximately 5% of sevoflurane is metabolized, the release of free fluoride anion does not seem to cause any clinically significant toxicity.
Term
The primary means of rocuronium elimination is
Definition
The primary means of rocuronium elimination is: biliary elimination of unchanged drug

Biliary elimination of rocuronium is the primary means of elimination. Approximately one-third undergoes renal excretion. As a result, prolonged neuromuscular blockade can be expected in patients with significant hepatic or renal disease
Term
In the two-compartment drug distribution curve shown below, the α-phase is largely the result of:
Definition
In the two-compartment drug distribution curve shown below, the α-phase is largely the result of: dispersal of the drug into the tissue compartments
Term
All opiate agonists produce a dose-dependent depression of respirations via effects on what opioid receptors
Definition
All opiate agonists produce a dose-dependent depression of respirations via effects on mu and delta receptors.
Term
Pharmacodynamic properties of isoproterenol include
Definition
Pharmacodynamic properties of isoproterenol include: (Select 2): bronchodilation, increased heart rate

The profound β1 stimulation of isoproterenol results in both positive inotropic and chronotropic effects and causes a dramatic increase in myocardial oxygen consumption. Isoproterenol is also a potent bronchial dilator and pulmonary vasodilator
Term
The benzodiazepine with the longest elimination half-life is:
Definition
he benzodiazepine with the longest elimination half-life is: diazepam
Term
Entacapone and tolcapone are used for the treatment of Parkinson's disease. They are are selective and reversible inhibitors of ?
Definition
Entacapone and tolcapone are used for the treatment of Parkinson's disease. They are are selective and reversible inhibitors of COMT
Term
what is Chemical antagonism
Definition
Chemical antagonism occurs when a drug's action is blocked by the antagonist's chemical binding of the drug. This occurs in the case of positively charged protamine forming an ionic bond with heparin or the chemical binding of rocuronium by γ-cyclodextrin.
Term
MAC is decreased by how much as we age
Definition
The MAC of inhalational agents is decreased by 4% per decade of age over 40 years
Term
the mac for a 80 year old iS?
Definition
The MAC of inhalational agents is decreased by 4% per decade of age over 40 years

80 year old mac is 0.84.
Term
MAC for a 60 year old is?
Definition
The MAC of inhalational agents is decreased by 4% per decade of age over 40 years

0.92
Term
Electroencephalographic evidence of seizure activity has been associated with the administration of what inhaled anesthetic
Definition
Electroencephalographic evidence of seizure activity has been associated with the administration of: sevoflurane

Sevoflurane, unlike desflurane, isoflurane or nitrous oxide can predispose patients to epileptic activity.

pp. 90, 97
Term
how is atracurium metabolized compared to cisatracurium
Definition
ATracurium: hoffmans, nonspecific esterases

Cisatracurium: hoffman. NO ESTERASE INVOLVEMENT, liver metabolism too.
Term
what drugs undergo ester hydrolysis compared to what drugs under go pseudocholinesterase metabolism
Definition
Pseudocholinestease metabolism 1. sux 2. cocaine 3. procaine 4. chloroprocaine 5. tetracaine 6. neostigmine 7. pyridostigmine Nonspecific esterases 1. remifentanil 2. atracurium 3. esmolol 4. clevidipine 5. etomidate
Term
endocrine effects of opiate administration during surgery include: 6x
Definition
Endocrine effects of opiate administration during surgery include
1. increase release of Vasopressin
2. immunosuppresion
3. reduced stress response
4. inhibition of corticotropin
5. inhibition of gonadotropin
6. inhibition of release of thyrotropin
Term
describe milirinione
Definition
Milrinone is a phosphodiesterase type-3 inhibitor, which produces positive inotropic action and vasodilation without producing tachycardia. In smooth muscle, milrinone causes an efflux of calcium with resultant relaxation and vasodilation.
Term
The primary antidysrhythmic effect of adenosine
Definition
The primary antidysrhythmic effect of adenosine: is to interrupt reentrant AV nodal tachycardia

The primary antidysrhythmic effect of adenosine is to interrupt reentrant AV nodal tachycardia, which most likely relates to its K+ current rather than Ca2+ current effects.
Term
Maximum dosage guidelines for the infiltrative injection of local anesthetic state that the maximum cumulative (per procedure) dose of lidocaine with and without epi
Definition
The maximum cumulative dose of lidocaine per procedure is: 4.5 mg/kg; not to exceed 300 mg dose. If epinephrine is added to the lidocaine, the dose can be increased to: 7 mg/kg; not to exceed 400 mg dose.
Term
The anesthetic effect of volatile agents is greatly attenuated or lost if what changes in its chemistry function?
Definition
The anesthetic effect of volatile agents is greatly attenuated or lost if: the length of the agent's molecules exceeds 5 carbon atoms

The length of anesthetic molecules is significant in that immobility (anesthetic effect) is attenuated or lost if carbon atom chain length exceeds a distance of 5 - 6 carbon atoms.
Term
Awakening after an induction dose of propofol is a result of:
Definition
Awakening after an induction dose of propofol is a result of: redistribution of the drug to the peripheral compartment
Term
describe precedex
Definition
Dexmedetomidine is an α2-receptor agonist, which produces sedation with central sympatholysis. This results in a reduction in blood pressure and heart rate. dexmedetomidine does not interfere with neurologic monitoring or cause significant ventilatory depression.
Term
describe the pk/pd of ritonavir
Definition
Ritonavir is a protease inhibitor used in the treatment of HIV infection. Ritonavir can cause changes in the function of the cytochrome system and may reduce fentanyl clearance and increase its half-life.
Term
ocal anesthetics that have been associated with the production of methemoglobin include:
Definition
Two local anesthetics, benzocaine and prilocaine, can cause methemoglobin formation. Prilocaine can produce methemoglobin as a result of the hemoglobin oxidizing effect one of its metabolites, o-toluidine.
Term
Propofol is prepared in a 1% lipid emulsion because of its
Definition
high pKa

Propofol is prepared in a lipid emulsion as a result of its lack of solubility in water, as reflected by its high pKa of 11.high pKa

Propofol is prepared in a lipid emulsion as a result of its lack of solubility in water, as reflected by its high pKa of 11.
Term
Concerning the pharmacokinetics of neuromuscular blockers in elderly patients and onset and recovery
Definition
Concerning the pharmacokinetics of neuromuscular blockers in elderly patients: (Select 2) onset or relaxation is delayed, recovery is delayed

The onset times of the NMBAs are generally delayed in the elderly due to slower circulation times. Changes in hepatic and renal clearance and an increased volume of distribution account for the increased duration.
Term
purpose of phase II drug metabolism reactions
Definition
Phase II reactions are also referred to as synthetic reactions in which the body actually synthesizes a new compound by donating a functional group. The products of Phase II reactions have little or no biologic activity and are more polar compounds that are more highly ionized and easily extractible by the kidneys.
Term
Prazocin, doxazosin and terazosin are what type of drugs? Used to treat?
Definition
Prazocin, doxazosin and terazosin are selective α1-receptor antagonists used the the treatment of hypertension.
Term
Concerning the action of local anesthetics, a phasic block refers to
Definition
a faster onset of block in nerves repetitively depolarized

Local anesthetics work faster as the sodium channels are repetitively depolarized. This is termed as use-dependent or phasic block.
Term
If the absolute value of the pKa - pH of a drug is less than 1, then the drug will be
Definition
If the absolute value of the pKa - pH of a drug is less than 1, then the drug will be: partially ionized and partially nonionized

If the absolute value of the pKa - pH is less than 1, regardless of whether the pH is lower or higher than the pKa, the drug will be partially ionized (hydrophilic) and partially nonionized (lipophilic).
Term
Fospropofol is converted to propofol through the action of
Definition
Fospropofol is converted to propofol through the action of: alkaline phosphatase
Term
The elimination half-life is the time necessary for the plasma content of a drug to drop to half of its prevailing concentration. Clinically a drug is regarded as being fully eliminated when approximately ___% or more has been eliminated.
Definition
The elimination half-life is the time necessary for the plasma content of a drug to drop to half of its prevailing concentration. Clinically a drug is regarded as being fully eliminated when approximately 95% or more has been eliminated.
Term
For practical purposes, drugs undergoing first-order elimination are regarded as being fully eliminated after 5 half-lives have past. At this point, the amount of drug remaining is approximately___
Definition
For practical purposes, drugs undergoing first-order elimination are regarded as being fully eliminated after 5 half-lives have past. At this point, the amount of drug remaining is approximately: 3.125%

(0.5)^5 = 0.03125
Term
The rapid termination of effect after the discontinuation of an esmolol infusion is a result of
Definition
Esmolol has an onset time of 2 minutes and an elimination half-life of approximately 9 minutes. Esmolol is metabolized by nonspecific esterases found in the cytosol of red blood cells.
Term
Bosentan reduces pulmonary artery pressure by
Definition
Bosentan reduces pulmonary artery pressure by: inhibiting endothelin

Bosentan is the best studied of the endothelin antagonists and through this action induces pulmonary vasodilation.
Term
The protein binding of acidic drugs is largely with which protein
Definition
The protein binding of acidic drugs is largely with: albumin

In the binding of drugs to plasma proteins, albumin is the most important. Plasma albumin binds, for the most part, acidic drugs, while basic drugs may be bound by β-globulin and α1-acid glycoprotein.
Term
describe propofol
Definition
Propofol administration is associated with a decrease in CMRO2,CBF and ICP. Propofol can produce myoclonia; however, it does not cause epileptiform activity on the EEG. Propofol causes a decrease in BP, heart rate and SVR. It does not cause histamine release and is a preferred agent for induction in asthmatic patients.
Term
Diuresis, through the competitive inhibition of aldosterone, can be achieved with the administration of:
Definition
Diuresis, through the competitive inhibition of aldosterone, can be achieved with the administration of: spironolactone

By blocking the action of aldosterone, which normally stimulates Na+ reabsorption and K+ excretion by the collecting duct, spironolactone causes sodium and water loss with potassium retention.
Term
In general, when nitroprusside is administered faster than ___, cyanide is generated faster than the patient can eliminate it.
Definition
n general, when nitroprusside is administered faster than 2 μg/kg/min, cyanide is generated faster than the patient can eliminate it.
Term
Methods of drug delivery that bypass the portal system's first-pass effect include:
Definition
Methods of drug delivery that bypass the portal system's first-pass effect include: (Select 3): intravenous, sublingual, distal rectal placement
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