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SEE NCE Boards CoreConcepts > Pharmacology EXAM > Flashcards

Pharmacology EXAM Flashcards

1
Q

The route of administration associated with the lowest degree of bioavailability is:

A

intrathecal

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2
Q

By definition, intravenous administration is associated with bioavailability _____%

A

100%

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3
Q

y. Intramuscular and sublingual administration is associated with______ bioavailability.

A

60 - 100%

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4
Q

The oil/gas coefficient of an inhaled anesthetic agent best corresponds to the agent’s:

A

potency

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5
Q

What characteristics of a gas indicates potency?

A

Oil/gas coefficient

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6
Q

The higher the solubility ______the drug (more or less potent)

A

More

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7
Q

The antiemetic effects of ondansetron are the result of the drug’s:(MOA)

A

antagonistic properties at serotonin type-3 receptors

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8
Q

This agent is a Selective serotonin type-3 receptor antagonist

A

Ondansetron

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9
Q

Drugs used in the preoperative preparation of the hyperthyroid patient,

A

Methimazole

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10
Q

What is the mechanism of action of Methimazole ?i

A

Inhibit organification of iodine and synthesis of thyroid hormone

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11
Q

What is the most important goal in managing the hyperthyroid patient?

A

is to make the patient euthyroid before any surgery, if possible. T

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12
Q

What are 2 THIOUREA derivatives drugs?

A

Propylthiouracil and Methimazole

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13
Q

What is the mechanism of THIOUREA derivatives drugs?

A

inhibit organification of iodide and the synthesis of thyroid hormone.

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14
Q

Respiratory insufficiency has been associated with the administration of which drug? (class III antiarrhythmic)

A

amiodarone

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15
Q

How does Amiodarone affects pulmonary disease?

A

chronic interstitial pneumonitis, organizing pneumonia, ARDS or a solitary mass of fibrosis.

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16
Q

Prevalence of pulmonary disease with the use of amiodarone?

A

5 - 15%

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17
Q

Generalized pruritis associated with administration

A

neuraxial fentanyl

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18
Q

Pruritis mechanism appears to be through interaction with which receptor?

A

central μ-receptor interaction.

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19
Q

Pruritus associated with ______administration

A

Intrathecal

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20
Q

Opiates frequently produce a______and a feeling of _______in what areas of the body?

A

Rash, itching and a feeling of warmth in the area of the face, upper chest, and arms.

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21
Q

Non-HISTAMINE releasing OPIOIDS

A

FENTANYL

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22
Q

Noncompetitive and nonselective α-blockade can be achieved with the administration of:

A

phenoxybenzamine

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23
Q

Phenoxybenzamine has what kind of activity at receptors? Phenoxybenzamine is used in the preoperative preparation of patients with pheochromocytoma.

A

has both α1- and α2-blocking activity.

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24
Q

Phenoxybenzamine The α-receptors are(competitiveness and reversibility)

A

noncompetitively and irreversibly bound.

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25
Q

Rise and Fall of inhaled anesthetic agent in body compartment? (all brain must be fat)

A

Alveoli
Brain
Muscle
Fat

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26
Q

Medication to treat Hyponatremic HYPERVOLEMIC CHF ??

A

Tolvaptan

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27
Q

What is Tolvaptan mechanism of action ?

A

Inhibit arginine vasopressin receptors

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28
Q

Tolvaptan inhibit arginine vasopressin receptors where in the renal ?

A

Collecting ducts.

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29
Q

Agents have proven to be safe and efficacious in hyponatremic patients, appearing to have particular value in patients with hypervolemic hyponatremia secondary to congestive heart failure.

A

Vasopressin receptor blocking agents

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30
Q

Name some vasopressin antagonists?

A

Conivaptan, Tolvaptan, -Vaptan

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31
Q

The vasopressin receptor antagonists produce a selective

A

water diuresis without affecting sodium and potassium excretion.

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32
Q

Identify this molecule: CF3-CHF-O-CHF2

A

Desflurane

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33
Q

Identify this molecule: N=N=O

A

Nitrous Oxide

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34
Q

Identify this molecule: (CF3)2 - CH- O-CH2F

A

Sevoflurane

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35
Q

Identify this molecule: CF3- CHCl- O-CH2F

A

Isoflurane

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36
Q

The onset of action of a local anesthetic agent is closely correlated to its (what properties)

A

pKa

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37
Q

Since local anesthetic agents need to first _______ to have an effects

A

gain access to the interior of the neuron to have effect,

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38
Q

Local anesthetic agents with lower pKa,

A

Lidocaine
Mepivacaine
Prilocaine

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39
Q

Lower pKa have a _______onset of action

A

more rapid

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40
Q

High pKa have a________ onset of action

A

Slower

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41
Q

Local anesthetics agents with

A

Bupivacaine
Tetracaine
Procaine

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42
Q

A patient is undergoing debridement of wounds under hyperbaric conditions. If the pressure in the hyperbaric chamber is 2 atmospheres, the minimum alveolar concentration of desflurane would be expected to be:

A

3%

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43
Q

MAC as originally defined depends on

A

atmospheric pressure.

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44
Q

However, when agent concentration is expressed as a partial pressure, MAC becomes independent

A

of ambient pressure.

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45
Q

MAC, expressed as a percentage,________ with increasing ambient pressure.

A

decreases

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46
Q

MAC expressed as percentage and relationship with ambient pressure

A

Inverse relationship

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47
Q

MAC of desflurane @ 1 ATM =

A

6% of 760 mm Hg = 45.6 mm Hg

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48
Q

MAC of desflurane @ 2 ATM =

A

45.6 mm Hg / 1520 mm Hg = 0.03 or 3%

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49
Q

What is the CNS effects of Nitrous oxide?

A

a decrease in cerebrovascular tone, an uncoupling of CBF and (CMRO2)

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50
Q

Nitrous oxide on cerebral vascular tone and CMRO2

A

decreases cerebral vascular tone significantly and increases CMRO2.

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51
Q

Nitrous and CMRO2 and CBF coupling?

A

Since the increase in CMRO2 exceeds the elevation in CBF there is an uncoupling of these parameters.

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52
Q

What can you do to ATTENUATE the increase in CBF?

A

Mild hyperventilation can attenuate the increase in CBF that accompanies the use of nitrous oxide.

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53
Q

Action of succinylcholine on HR? and how?

A

Succinylcholine may cause bradycardia as a result of its action on cardiac: muscarinic receptors

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54
Q

Succinlycholine has no action on_________ but may cause bradycardia by an action on_______

A

ganglionic nicotinic receptors; cardiac cholinergic muscarinic receptors.

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55
Q

In considering the two-compartment model of drug distribution, the central compartment comprise what % of the body mass?

A

Represents approximately 10% of the body mass

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56
Q

In the two-compartment model, the first compartment is termed the and is composed of

A

central compartment

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57
Q

What is the central compartment composed of ?

A

intravascular fluid and the highly perfused tissues such as the heart, lungs, brain, liver and kidneys.

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58
Q

The central compartment represents only about _____of the body mass in the adult;

A

10%; ;

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59
Q

Central compartment receives how much % of the cardiac ouptut?

A

75% of the cardiac output

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60
Q

Central compartment also referred to as the

A

vessel-rich group.

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61
Q

Actions produced by opiate agonistic action on the kappa receptor include:

A

Analgesia, inhibition of ADH release, antishivering

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62
Q

Antishivering opiate agonist through which receptor?

A

Kappa

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63
Q

Inhibition of ADH release opiate agonist through which receptor?

A

Kappa

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64
Q

A low-dose infusion of epinephrine would be expected to produce: with skeletal muscles

A

increased blood flow to the skeletal muscles

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65
Q

With low doses of epinephrine which EFFECT dominate?

A

Beta dominates, few alpha

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66
Q

The propofol infusion syndrome (PRIS): results in

A

cardiac and peripheral muscle necrosis

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67
Q

What is the CAuse of PROPOFOL INFUSION syndrome syndrome? PRIS is likely the result of the iSymptoms include Risk factors include

pp 109-110

A

Inhibition of oxidative phosphorylation by propofol.

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68
Q

What are symptoms of Propofol infusion syndrome (PRIS)

A 
severe metabolic acidosis,
Rhabdomyolosis
Renal failure 
Bradycardia and 
Refractory heart failure.
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69
Q

Risk factors of Propofol infusion syndrome (PRIS)?

A 
young age (children more likely
doses greater than 4 - 5 mg/kg/hr, 
critical illness and an infusion duration greater than 48 hours.
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70
Q

Relief of anginal pain by nitroglycerine is primarily the result of:

A

decreased preload and cardiac work

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71
Q

Which medication given for angiona causes venodilation and a resultant decrease in preload?

A

Nitroglycerine

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72
Q

The occupancy theory states that:

A

the magnitude of a drug’s effect is proportional to the number of receptors occupied

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73
Q

The occupancy theory holds that the magnitude of a drug’s effect is

A

proportional to the number of receptors occupied.

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74
Q

The duration of action of a local anesthetic agent is closely correlated to its:

A

degree of protein binding

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75
Q

The duration of action of local anesthetics demonstrates a relationship to

A

protein binding and lipid solubility.

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76
Q

In theory, drugs that have a high affinity for protein,

A

attach more firmly to the sodium channel receptor and have a greater duration of action.

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77
Q

Diffusion hypoxia is a potential problem following the administration of:

A

nitrous oxide

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78
Q

During emergence, when high concentrations of nitrous oxide have been given, Explain the drug exit and its significance on the body?

A

the drug exits the body quickly and can result in the dilution of normal respiratory gases such as oxygen and carbon dioxide.

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79
Q

How do you prevent the occurrence of diffusion hypoxia with nitrous?

A

The administration of 100% oxygen for several minutes following the termination nitrous oxide entirely avoids this potential problem.

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80
Q

Ventilatory effects of the volatile anesthetic agents include

A

Increases in Ventilatory rate, PaCO2, the apneic threshold

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81
Q

What are the effects of Volatile anesthetic agents responsiveness to CO2?

A

Decrease responsiveness to CO2

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82
Q

The compensatory mechanism for the decreased tidal volume is an________; however, this is

A

increase in rate; insufficient to prevent an increase in PaCO2.

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83
Q

Hypoxic drive and Volatile agents

A

Depression of the hypoxic drive occurs with very low concentrations of volatile agents

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84
Q

VA and bronchial tone :

A

decreased with resultant bronchodilation.

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85
Q

Hydrolysis of succinylcholine by plasma cholinesterase results in the formation of:

A

succinic acid, choline, succinylmonocholine

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86
Q

Succinylcholine undergoes _______catalyzed ________

A

Ester Hydrolysis

Plasma cholinesterase

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87
Q

The typical Vd, normalized for the body weight of a 70 Kg adult, would be the

A

quantity of total body water (42 L) divided by the body weight (70 kg). This results in a Vd of 0.6 L/Kg.

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88
Q

Stimulation of opioid receptors has been shown to:

A

inhibit adenylate cyclase in the cell

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89
Q

Opioid receptors are what kind of receptors?. This causes in a d

A

G- Protein Coupled receptors

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90
Q

Opioid receptors are GPCRs , what do they do?

A

Inhibit the activity of adenylate cyclase inside cells

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91
Q

Opioids receptors are GPCR that inhibit the action of adenylate cyclase which causes what? what about calcium and K+?

A

decreases conductance of the voltage-gated calcium channels and open potassium channels, resulting in decreased neuronal activity.

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92
Q

Generally absent with low-dose norepinephrine infusions

A

Positive chronotropic effects

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93
Q

NE infusion at low doses on vascular resistance>

A

increase in vascular resistance inducing reflex vagal activity

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94
Q

In low doses, norepinephrine show ________the end results is ________

A

little β2 activity and the end result is largely unopposed α-receptor stimulation.

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95
Q

Why is the chronotropic effect seen with β1-receptor stimulation is generally absent with low-dose norepinephrine?

A

because of the increase in SVR, which induces reflex vagal activity.

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96
Q

CV and properties of etomidate include: (Select 3) hydrolysis by plasma esterases,, adrenocortical suppression with induction doses

A

minimal hemodynamic changes with induction

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97
Q

Metabolism of Etomidate is by

A

hepatic microsomal enzymes and HYDROLYSIS by plasma esterases.

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98
Q

What you should know about Etomidate induction dose?

A

Adrenal suppression with induction dose

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99
Q

What accounts for the EXTREMETLY short duration of action of Etomidate?

A

Rapid redistribution

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100
Q

What is the primary clinical advantage of Etomidate?

A

Hemodynamic stability upon induction

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101
Q

Etomidate action of adrenal hormone is that it ?

A

Decrease the adrenal hormone levels for up to 24 hours after etomidate administration

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102
Q

What is the cause of Etomidate’s addrenal suppression?

A

11 Beta-hydroxylase inhibition

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103
Q

Clevidipine: is

A

highly selective for vascular smooth muscle

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104
Q

What is clevidipine class o

A

Dihydropyridine L-type CCB

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105
Q

Clevidine is used as an

A

IV antihypertensive

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106
Q

Why is the good thing about clevidine?

A

Highly selective for vascular muscle and does NOT AFFECT Myocardial contractility or conduction

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107
Q

The graded dose-response curve has a: hyperbolic shape

A

Hyperbolic shape

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108
Q

The graded dose-response curve, which is plotted in linear fashion, characterizes

A

the changes in measured response as an administered dose is increased.

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109
Q

The response curve has a

A

hyperbolic shape.

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110
Q

When plotted on a logarithmic scale, the dose-response curve takes

A

on a sigmoid, or ‘S’, shape.

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111
Q

Vasoconstrictive properties are associate with use of what 3 local anesthetics?

pg. 131

A

cocaine, lidocaine, ropivacaine

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112
Q

What are the only parenterally administered local anesthetics with vasoconstrictive properties?

A

Ropivacaine and lidocaine

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113
Q

Cocaine also has vasoconstrictive properties because of its

A

ability to block the reuptake of norepinephrine.

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114
Q

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:

A

1500 mL

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115
Q

A compliant airspace, such as a pneumothorax, will

A

increase in volume during nitrous oxide administration.

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116
Q

Theoretically, at 50% inspired nitrous oxide, the gas bubble would

A

double in volume.

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117
Q

Theoretically, at 67% nitrous oxide

A

could triple the volume of a gas bubble

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118
Q

The chemical interaction of sevoflurane with desiccated soda lime has been associated with:

A

anesthesia machine fires

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119
Q

Sevoflurane can react chemically with desiccated soda lime and yield

A

excessive temperatures that produce anesthesia machine fires and patient injuries.

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120
Q

The proposed mechanism of Sevoflurane and dessicated soda lime fires?

A

he proposed mechanism is a dehydrohalogenation of the sevoflurane with the release of hydrogen gas.

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121
Q

3 Causes of increased pseudocholinesterase activity include: thyroid disease

A

Thyroid disease, nephrotic syndrome and obesity

Cognitively impaired children

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122
Q

Characteristically, drugs with large volumes of distribution are: in terms of Lipid solubility and protein binding

A

lipid soluble with little protein binding

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123
Q

Drugs that are free, unbound to plasma proteins and lipid soluble

A

easily cross membranes to tissues and therefore have large calculated volumes of distribution with low plasma concentrations.

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124
Q

Drugs with Large volume of distribution have a _____Plasma concentration

A

low plasma concentrations

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125
Q

The production of a neurotoxic metabolite has been associated with the use of what opiods?

A

meperidine

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126
Q

Meperidine is biotransformed by

A

Liver

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127
Q

Meperidine is biotransformed by the live to

A

Normeperidine, a neurotoxic metabolite,

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128
Q

Normeperidine half life is

A

12 - 16-hour half-life.

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129
Q

Repetitive dosing of meperidine can cause accumulation of normeperidine, which may

A

precipitate tremulousness, myoclonus, and seizures

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130
Q

Low-dose dopamine infusion causes increased urine output as a result of

A

an increase in renal blood flow

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131
Q

The stimulation of dopamine receptors in the renal artery promotes

A

an increase in renal blood flow and a resultant increase in glomerular filtration rate and urine output.

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132
Q

Ketamine MOA is

t increases pulmonary compliance in patients with bronchospastic disease.

A

antagonizes NMDA receptors in the brain,noncompetitively inhibits the NMDA receptor in the brain producing amnesia and a profound analgesic state.

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133
Q

Ketamine on ICP and CBF

A

Increases ICP ; Increases CBF and CMRO2

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134
Q

Ketamine and Immune system?

A

Ketamine It inhibits tumor necrosis factor-alpha and interleukin-6, accounting for its antiinflammatory action.

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135
Q

How is Ketamine metabolized?

A

Ketamine is metabolized by hepatic microsomal enzymes.

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136
Q

Ketamine on the cardiovascular system?

A

Centrally mediated increase in sympathetic tone with an increase in heart rate and blood pressure.

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137
Q

Ketamine and pulmonary system

A

It increases pulmonary compliance in patients with bronchospastic disease.

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138
Q

Vasoplegic syndrome has been seen with the induction of anesthesia in patients receiving what class of medication?

A

ACE inhibitors

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139
Q

What is Vasoplegic syndrome (VS)?

A

unexpected refractory hypotension resulting from low systemic vascular resistance

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140
Q

The incidence of VS in surgical patients may be as high as 50% in persons receiving

A

renin-angiotensin system antagonists.

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141
Q

The therapeutic safety margin of a drug is defined as the:

A

lethal dose in 1% divided by the effective dose in 99% of the population : LD1/ED99

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142
Q

Therapeutic index or margin is

A

ED

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143
Q

The lower the margin of safety of a drug

A

the more likely toxic effects will be seen.

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144
Q

Of the following, the rapidity of local anesthetic absorption is the greatest with:

A

interpleural block

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145
Q

The absorption of local anesthetics generally occurs in the following order of rapidity: Excluding blocks of the airway, (PleuCoCauEBSciSub)

A

Interpleural block > intercostal block > caudal block > epidural block > brachial plexus block > sciatic-femoral block > subcutaneous blocks.

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146
Q

For LA, the closer the pka is to physiologic pH

A

the faster the onset of action

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147
Q

How does adding sodium bicarbonate help with local anesthetics?

A

Raises the pH and increases the concentration of NONIONIZED free base. SPEED up the onset of NEURAL BLOCKADE

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148
Q

Sequence of CLINICAL anesthesia: COMPLETE BLOCKADE OF PERIPHERAL NERVE progresses in the following order:
Vaso-PTProToPreMO

A 
sympathetic block with peripheral vasodilatation and skin temperature elevation
Loss of pain and temperature sensation
Loss of proprioception
Loss of Touch and pressure sensation
Motor paralysis
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149
Q

Cardiodepressant potency GREAT to least

A

Bupi>lidocaine>Chloroprocaine

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150
Q

The more potent,lipid soluble LA will result in ______systemic absorption

A

Decrease

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151
Q

The greater the lipid solubility of LA the more likely it will

A

Sequestered in the lipid rich compartment of both the axonal membrane and perineural tissues.

152
Q

2 LA metabolized to PABA

A

Procaine and Benzocaine

153
Q

What is the only Aminoamide LA that is hydrolized to o-toluidine?

A

Prilocaine

154
Q

Prilocaine is hydrolized to ______?

A

O-toluidine

155
Q

What is the significance of hydrolysis to O-toluidine?

A

Can oxidize hemoglobin to methemoglobin in a dose dependent fashion, can produce enough to cause cynanosis (methemeglobinemia)

156
Q

Clinical conditions causing decrease plasma proteins?

A

Cirrhosis
Newborn
Pregnancy
Leading to decrease binding capacity.

157
Q

Neonates and microsomal enzymes

A

Immature hepatic microsomal enzymes leading to decrease elimination of of aminoamide LA.

158
Q

The greatest degree of anesthetic metabolism is seen with the use of:

A

sevoflurane

159
Q

Although approximately____-% of sevoflurane is metabolized, the release of

A

5%; free fluoride anion does not seem to cause any clinically significant toxicity.

160
Q

Disruption of DNA synthesis through the inactivation of methionine synthetase has been associated with the prolonged administration of:

A

nitrous oxide

161
Q

Administration of Nitrous and DNA

A

Disruption of DNA synthesis through the inactivation of methionine synthetase

162
Q

Prolonged or chronic exposure to nitrous oxide can lead to what deficiency of Vitamin?

A

inactivation of the vitamin B12 component of methionine synthetase. This can disrupt DNA synthesis.

163
Q

The primary means of rocuronium elimination is:

A

biliary elimination of unchanged drug

164
Q

Rocuronium % of renal excretion

A

Approximately one-third undergoes renal excretion

165
Q

Rocuronium and renal patients –>

A

prolonged neuromuscular blockade can be expected in patients with significant hepatic or renal disease

166
Q

In the two-compartment drug distribution curve shown below, the α-phase is largely the result of:

A

dispersal of the drug into the tissue compartments

the steep drop from top to bottom

167
Q

In 2 compartment drugs: what is the first phase of the curve?

A

The first phase of the curve is the α-phase, or distribution phase, which represents the initial dispersal of drug into the tissue compartments from the central compartment.

168
Q

Respiratory effects of opiate agonists include: a

.

A

reduction in the responsiveness of the respiratory centers to increasing PaCO2

169
Q

All opiate agonists produce a ____________ of respirations via effects on what receptors?

A

dose-dependent depression of respirations via effects on mu and delta receptors

170
Q

OPIOIDS reduce the responsiveness of the respiratory centers to

A

both increasing carbon dioxide and decreasing oxygen levels.

171
Q

OPIOIDS and the Oxyhemoglobin dissociation curve?

A

produce a shift to the right of the CO2-response curve

172
Q

OPIOIDS effects on MV

A

increase in tidal volume with a decrease in ventilatory rate.

173
Q

Pharmacodynamic properties of isoproterenol include: (Select 2):

A

bronchodilation, increased heart rate

174
Q

Isoproterenol has profound

A

The profound β1 stimulation of isoproterenol results in both positive inotropic and chronotropic effects

175
Q

Isoproterenol has profound B1 stimulation resulting in positive inotropic and chronotropic effects which causes what as far as oxygen in the heart?

A

a dramatic increase in myocardial oxygen consumption.

176
Q

Isoproterenol is also a potent

A

bronchial dilator and pulmonary vasodilator.

177
Q

What is the benzodiazepine with the LONGEST elimination half life?

A

Diazepam

178
Q

Diazepam has the longest elimination half-life of the available benzodiazepines, approximately

A

36 - 50 hours.

179
Q

Diazepam also exhibits a near-linear relationship between elimination half-life and what patients characteristics?

A

patient age, which can result in prolonged effect in the elderly.

180
Q

What is Entacapone action?

A

inhibits catechol-O-methyltransferase

181
Q

Ephedra other name is

A

Ma Huang

182
Q

Ma Huang (Ephedra)

A

Think ephedrine because it has sympathomimetic with positive inotropic and chronotropic effects, alpha and beta.

183
Q

Ginger can

A

potentiate anticoagulants effet

184
Q

Ginkgo effects

A

Inhibits platelet aggregation put the patient at risk for bleeding.

185
Q

Gingseng can

A

Lower blood sugar

Can cause hypertension and tachycardia

186
Q

Gingseng and warfarin

A

decrease effectiveness of warfarin

187
Q

Herbs that can potentiate effects of barbuiturates

A

Valerian

188
Q

ST John’s Wort action with general

A

Inducers

May lead to serotonin syndrome

189
Q

Entacapone and tolcapone are used for the treatment of

A

Parkinson’s disease.

190
Q

What are the actions of entacapone and tolcapone?

A

They are are selective and reversible inhibitors of COMT.

191
Q

Inhbitors of COMT: Caution should be used when administering

A

catecholamines as their half-life may be significantly prolonged and effects may be exaggerated.

192
Q

Reversal of heparin-induced anticoagulation by

A

protamine sulfate

193
Q

Chemical antagonism occurs when a drug’s action is

A

blocked by the antagonist’s chemical binding of the drug.

194
Q

the chemical binding of rocuronium by

A

γ-cyclodextrin.

195
Q

This occurs in the case of positively charged protamine forming an

A

ionic bond with heparin

196
Q

The addition of epinephrine, in a concentration of 1:200,000, to lidocaine has been shown to:

A

result in a more profound block

197
Q

The addition of a vasoconstrictor to local anesthetics has been shown to reduce _____Allowing for ______

A

the rate of absorption, allowing more of the drug to stay in the area where it was injected.

198
Q

What allows for increased neuronal uptake and a longer and more profound block.

A

Adding vasoconstrictive drugs.

199
Q

Vasoconstricitive drugs added to LA causes a reduction in the

A

peak plasma concentration of the drug, thereby reducing systemic toxicity.

200
Q

As compared to a 40-year-old adult, the required dose (MAC) of inhaled anesthetic agents in a 6-month-old infant is approximately:

A

increased by 50 - 80%

201
Q

The MAC or required dose of anesthetics AND AGE: when is highest and lowest?

A

higher in infants and children and decreases with increasing age.

202
Q

Infants aged 6 months have a MAC

A

1.5 to 1.8 times higher than a 40-year-old adult.

203
Q

The MAC of inhalational agents is decreased by

A

4% per decade of age over 40 years.

204
Q

Electroencephalographic evidence of seizure activity has been associated with the administration of:

A

sevoflurane

205
Q

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

A

epileptic activity.

206
Q

Non-specific esterases are involved in the metabolism of which NDNMB:

A

atracurium

207
Q

Metabolism of Atracurium is via

A

Nonspecific esterases and Hofmann elimination are responsible for the metabolism of atracurium.

208
Q

Cisatracurium undergoes

A

Hofmann elimination;

209
Q

Not involved in the metabolism of cisatracurium.

A

Esterases

210
Q

2 Drugs that undergo pseudocholinesterase catalyzed phase I hydrolysis include

A

succinylcholine, chloroprocaine

211
Q

Drugs that Pseudocholinesterase catalyzed ester hydrolysis? -tigmine

A

Neostigmine and pyridostigmine

212
Q

Drugs that undergo pseudocholinesterase catalyzed Ester hydrolysis. LA

A

Cocaine, procaine, chloroprocaine, tetracaine

213
Q

For some drugs, although do undergo ester hydrolysis, the hydrolysis is accomplished by

A

nonspecific esterases.

214
Q

DRUGS that they hydrolysis is accomplished by NONSPECIFIC ESTERASES

A

remifentanil, atracurium, esmolol and clevidipine

215
Q

Endocrine effects of opiate administration during surgery include the increased release of

A

: vasopressin

216
Q

Stress response to surgery and Opiates

A

reduce the stress response to surgery and have an immunosuppressant effect.

217
Q

OPIOIDS Endocrinologic effects include the release of

A

vasopressin and inhibition of the stress-induced release of corticotropin and gonadotropins.

218
Q

OPIOIDS and Release of thyrotropin

A

Release of thyrotropin is also inhibited.

219
Q

Primary Pharmacodynamic properties of milrinone include

A

increased inotropy

220
Q

What class of medication is milrinone?

A

Phosphodiesterase type-3 inhibitor, which produces positive inotropic action and vasodilation without producing tachycardia.

221
Q

Milrinone produces positive inotropic action and ______without ____

A

Vasodilation ; Tachycardia.

222
Q

Action of milrinone on Smooth muscle?

A

In smooth muscle, milrinone causes an efflux of calcium with resultant relaxation and vasodilation.

223
Q

Flumazenil half life

A

short half-life as compared to most benzodiazepines

224
Q

Flumazenil is a

A

Competitive benzodiazepine antagonist, which produces prompt reversal of benzodiazepine effects. I

225
Q

Good to remember about Flumazenil

A

Relatively short half-life and duration of action make the possibility of resedation clinically relevant.

226
Q

Flumazenil can produce does not

A

withdrawal reactions in patients who are benzodiazepine dependent.

227
Q

Limitation of Flumazenil

A

reverse the actions of ethanol or barbiturates.

228
Q

The primary antidysrhythmic effect of adenosine: is to

A

interrupt reentrant AV nodal tachycardia

229
Q

The primary antidysrhythmic effect of adenosine is to interrupt reentrant AV nodal tachycardia, which most likely relates to its

A

K+ current rather than Ca2+ current effects.

230
Q

What is an INVERSE AGONIST ?

A

A drug that binds to a receptor, resulting in the opposite action of the agonist.

231
Q

What is an AGONIST?

A

A drug that binds to a specific receptor and

triggers a response.

232
Q

What Is A PARTIAL AGONIST?

A

A drug that activates the receptor, but cannot

produce a maximal response.

233
Q

What is an ANGATONIST?

A

A drug that has affinity for the receptor, but

no efficacy.

234
Q

Maximum dosage guidelines for the infiltrative injection of local anesthetic state that the maximum cumulative (per procedure) dose of lidocaine, without epinephrine, is:

A

4.5 mg/kg; not to exceed 300 mg dose

235
Q

If epinephrine is added to the lidocaine, the dose can be increased to

A

7 mg/kg; not to exceed 400 mg dose.

236
Q

The anesthetic effect of volatile agents is greatly attenuated or lost if:

A

the length of the agent’s molecules exceeds 5 carbon atoms

237
Q

The length of anesthetic molecules is significant in that immobility (anesthetic effect) is attenuated or lost if carbon atom chain length

A

exceeds a distance of 5 - 6 carbon atoms.

238
Q

Awakening after an induction dose of propofol is a result of:
. Rapid redistribution from the central compartment to the peripheral compartments produces a quick initial decline. Metabolism plays little role in the initial awakening of the patient.

A

redistribution of the drug to the peripheral compartment

239
Q

Rapid distribution following an induction dose of propofol into the brain results in

A

fast onset of generally one circulation time

240
Q

LA pka ranges from

A

7.6 -8.9

241
Q

Ph LA rangs from

A

3.9- 6.47

242
Q

2 highest protein bound LA

A

Bupivacaine

Ropivacaine

243
Q

With propofol Rapid redistribution from the central compartment to the peripheral compartments produces

A

a quick initial decline.

244
Q

Plays little role in the initial awakening of the patient.

A

Metabolism

245
Q

Histamine release has been associated with the use of:

A

atracurium

246
Q

Releases modest amounts of histamine.

A

Atracurium

247
Q

The rates of rise of the inhalational agents are

A 
Nitrous
Desflurane
Sevoflurane
Isoflurane
Halothane
248
Q

The opioid with the greatest degree of lipid solubility is

A

Sufentanil (measured by octanol/water coefficient)

249
Q

Sufentanil vs morphine in potency is approximately

A

1750 times more lipid soluble than morphine.

250
Q

When treating maternal hypotension, as compared to phenylephrine, ephedrine

A

produces an increase in fetal acidosis as a result of causing: an increase in fetal metabolic rate

251
Q

Ephedrine produces increases in fetal metabolic rate leading to

A

to fetal acidosis due to beta stimulation, whereas phenylephrine does not.

252
Q

Mechanism of opioid analagesia in spinal cord

A

Inhibit the release of substance P from primary sensory neurons, in the dorsal horn attenuation the transmission of painful stimuli from peripheral nerves to the cerebral cortex

253
Q

Mechanism of opioid analagesia in spinal cord

A

Act at descending inhibitory pathway s to attenuate painful stimuli.

254
Q

Dexmedetomidine produces ______With ______causes______in BP and ______in HR.

A

produces sedation with central sympatholysis, causes a decrease in blood pressure and heart rate

255
Q

Dexmedetomidine does not

A

interfere with neurologic monitoring or cause significant ventilatory depression.

256
Q

Ritonavir: What kind of medication is it?

A

is a protease inhibitor used in the treatment of HIV infection.

257
Q

Ritonavir and opioids?

A

may increase the plasma half-life of fentanyl

258
Q

Ritonavir can cause changes in the function of the

A

cytochrome system and may reduce fentanyl clearance and increase its half-life

259
Q

Ion trapping can occur with the

A

placental transfer of lidocaine to the fetus as a result of the: lower pH of fetal blood

260
Q

The lipid-soluble fraction of basic agents such as lidocaine crosses

A

the placenta easily. However, once there, because of the lower pH of the fetus, the drug becomes more ionized and cannot easily cross the lipid bilayer of the placenta, resulting in accumulation of drug in the fetus.

261
Q

2 Local anesthetics that have been associated with the production of methemoglobin?

A

prilocaine, benzocaine

262
Q

Prilocaine can produce methemoglobin as a result of the

A

hemoglobin oxidizing effect one of its metabolites, o-toluidine.

263
Q

Factors shown to INCREASE the minimum alveolar concentration (MAC) of inhaled anesthetics include:
CHYRAH

A 
Chronic alcohol consumption
Hyperthyroidism
Youth
Red Headed Females 
Acute Amphetamine administration 
Hyperthermia
264
Q

Propofol is prepared in a 1% lipid emulsion why?

A

Because its high pKa

265
Q

Propofol is prepared in a lipid emulsion as a result of its

A

Lack of solubility in water, as reflected by its high pKa of 11.

266
Q

Concerning the pharmacokinetics of neuromuscular blockers in elderly patients:onset and recovery

A

nset or relaxation is delayed, recovery is delayed

267
Q

Why is the onset times of NMBAs delayed in the elderly?

A

The onset times of the NMBAs are generally delayed in the elderly due to slower circulation times.

268
Q

Why is the onset times of NMBA slows and delayed in elderly? Changes in

A

hepatic and renal clearance and an increased volume of distribution account for the increased duration.

269
Q

Vd and elderly

A

Increase in Vd

270
Q

During drug metabolism, the products of phase II reactions:

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.

A

are more polar compounds than the parent drug

271
Q

Phase II reactions are also referred to as

A

synthetic reactions

272
Q

Phase II reactions are also referred to as synthetic reactions in which the body

A

actually synthesizes a new compound by donating a functional group. T

273
Q

The products of Phase II reactions have

A

little or no biologic activity and are more polar compounds that are more highly ionized and easily extractible by the kidneys.

274
Q

There is a significant drug interaction that can occur between meperidine and

A

the first-generation monamine oxidase-inhibiting drugs. Hyperthermia, seizures and death have been reported.

275
Q

What can happen if you give MEPERIDINE for a patient taking MAOI?

A

Seizures, hyperthermia and death

276
Q

Vasodilation in both arterioles and veins, through selective α1-receptor blockade is seen in patients receiving:

A

Prazosin

277
Q

Those agents are selective α1-receptor antagonists used the the treatment of hypertension (3)

A

Prazocin, doxazosin and terazosin

278
Q

Benefits of selective alpha 1 receptor antagonists areheir

A

lack of α2-blocking activity indicates that they have no effect on norepinephrine levels and are associated with less tachycardia than seen with the use of nonselective α-blockers.

279
Q

Effects of Prazosin

A

Vasodilation in both arterioles and veins, through selective α1-receptor blockade

280
Q

Concerning the action of local anesthetics, a phasic block refers to:

A

a faster onset of block in nerves repetitively depolarized

281
Q

Local anesthetics work faster as the sodium channels are

A

repetitively depolarized.This is termed as use-dependent or phasic block.

282
Q

The anticoagulation effect of rivaroxaban is the result of:

A

inhibition of factor Xa

283
Q

Direct inhibitor factor Xa are : 2 drugs

A

rivaroxaban and apixaban, directly inhibit factor Xa

284
Q

Action of Direct inhibitor of Factor Xa

A

They prolong the PT and aPTT, but monitoring is not recommended and the INR should not be used

285
Q

If the absolute value of the pKa - pH of a drug is less than 1, then the drug will be:

A

partially ionized and partially nonionized

286
Q

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

A

will be partially ionized (hydrophilic) and partially nonionized (lipophilic

287
Q

Toxic effects to local anesthetics include:

A

myotoxicity

288
Q

When injected directly into skeletal muscle, local anesthetics are

A

mildly myotoxic

289
Q

Coagulation and Local anesthetics

A

depress normal blood coagulation by decreasing platelet aggregation and enhancing fibrinolysis.

290
Q

When given as a sole inhaled agent, what effect does nitrous have on CV?

A

increase in systemic vascular resistance, central venous pressure and arterial pressure can be seen with the administration of:

291
Q

Nitrous oxide activates the

A

sympathetic nervous system thereby increasing SVR, CVP and arterial pressure.

292
Q

Fospropofol is converted to propofol through the action of:

A

alkaline phosphatase

293
Q

The prodrug, fospropofol, is converted to

A

active propofol by alkaline phosphatase.

294
Q

Cholinesterase inhibitors that lack an ester linkage and competitively inhibit the enzyme include:

A

edrophonium

295
Q

Edrophonium is a simple alcohol that contains a

A

quaternary ammonium group.

296
Q

Because a true chemical bond is not formed, acetylcholine competes with

A

edrophonium for the binding site of cholinesterase.

297
Q

For practical purposes, drugs undergoing first-order elimination are regarded as being fully eliminated

he 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. After 5 half-lives a the remaining amount of drug has been reduced to 3.125%.

A

5 half-lives have past.

298
Q

For practical purposes, drugs undergoing first-order elimination are regarded as being fully eliminated afterAt this point, the amount of drug remaining is approximately:

A

3.125%.

299
Q

What is the elimination half-life?

A

time necessary for the plasma content of a drug to drop to half of its prevailing concentration

300
Q

When is thremaining amount of drug has been reduced to 3.125%?

A

After 5 half-lives

301
Q

After five half life how do you calculate

A

(0.5) ^5 = 0.03125 Then you times it by 100 you get 3.125%

302
Q

Opioids that possess antagonistic effects at the μ-receptor site, while retaining agonistic effects at the κ-receptor site include

A

nalbuphine and butorphanol

303
Q

Drugs that are classified as agonist-antagonist opioids.

A

Both nalbuphine and butorphanol

304
Q

Main action of the opioids antagonists Nalbuphine or butorphanol?

A

These drugs act as antagonists at the μ-receptor site while providing agonistic effects at the κ-receptor site.

305
Q

The rapid termination of effect after the discontinuation of an esmolol infusion is a result of rapid:

A

hydrolysis by nonspecific plasma esterases

306
Q

Onset time of Esmolol

A

2 minutes

307
Q

Half life of esmolol is about

A

9 minutes

308
Q

Esmolol is metabolized by nonspecific esterases found in the

A

Cytosol of RBCs.

309
Q

The effects of local anesthetics appear to be the

A

result of drug binding to receptors in: the inner gate of the sodium channels

310
Q

Local anesthetics must gain access to

A

the interior of the neuron to reach their receptor. Once inside the neuron, the ionized fraction binds to the receptor on the inside of the sodium channel.

311
Q

Bosentan mechanism of action?

A

reduces pulmonary artery pressure by: inhibiting endothelin

312
Q

Bosentan is the best studied of the

A

endothelin antagonists and through this action induces pulmonary vasodilation.

313
Q

The protein binding of acidic drugs is largely with:

A

albumin

314
Q

In the binding of drugs to plasma proteins, What is the most important?

A

albumin

315
Q

Plasma albumin binds, for the most part, while basic drugs may be bound by

A

acidic drugs,

316
Q

Basic drugs may be bound by

A

β-globulin and α1-acid glycoprotein.

317
Q

Treatment of systemic local anesthetic toxicity should include

If cardiac arrest occurs, vasopressin, calcium channel blockers and beta-blockers should be avoided. Lipid emulsion therapy should be administered at the first signs of LAST.

A

: the administration of lipid emulsion

318
Q

Treatment of LAST: _________is crucial to preventing hypoxia and acidosis

A

Prompt airway management

319
Q

known to potentiate local anesthetic systemic toxicity (LAST).

A

ACIDOSIS and HYPOXIA

320
Q

If cardiac arrest occurs with LAST, what are the MEDICATIONS that YOU MUST AVOID?

A

vasopressin, calcium channel blockers and beta-blockers should be avoided

321
Q

Lipid emulsion therapy should be administered at the

A

first signs of LAST

322
Q

The most marked attenuation of hypoxic pulmonary vasoconstriction is seen with the administration of which GAS?

A

nitrous oxide

323
Q

What are the 2 gases that may attenuate the HPV?

A

Hypoxic pulmonary vasoconstriction is attenuated to some extent by isoflurane administration, but is markedly attenuated or lost by the administration of nitrous oxide.

324
Q

Pharmacodynamic characteristics of propofol include in the Brain : comment on CBF, CMRO2 and ICP

A

in cerebral metabolic rate of oxygen consumption, a decrease in cerebral blood flow, an increase in myoclonia

325
Q

Induction drug that does not cause epileptiform activity on the EEG.

A

Propofol

326
Q

Propofol on CV as far as BP , HR, and SVR

A

causes a decrease in BP, heart rate and SVR.

327
Q

What is the preferred induction agent for a patient with ASTHMA?

A

Propofol: No histamine release

328
Q

Pathologic states associated with resistance to depolarizing neuromuscular blockade include

A

myasthenia gravis

329
Q

Myasthenia GRAVIS and SUCC ? What might offset the effect?

A

Patients with myasthenia gravis are usually resistant to succinylcholine, with larger than usual doses required to produce complete blockade. This effect might be offset by the inhibition of plasma cholinesterase activity provided by pyridostigmine.

330
Q

Myasthenia Gravis and NDNMB

A

SENSITIVE TO NDNMB

331
Q

Zero-order drug elimination

A

results in the removal of a constant amount of drug per unit time

332
Q

First-order drug elimination implies that a (think FF)

A

constant fraction of drug is being eliminated per unit time

333
Q

This is the most common method of elimination of anesthetic drug

A

First Order Kinetics

334
Q

Implications of ZERO order kinetic , is it better than first order kinetics?

A

This is a much less efficient method of drug elimination and implies saturation of the metabolic or elimination pathway.

335
Q

Main action of spironolactone

A

Diuresis, through the competitive inhibition of aldosterone, can be achieved with the administration of:

336
Q

Aldosterone antagonist By blocking the action of aldosterone, which normally

A

stimulates Na+ reabsorption and K+ excretion by the collecting duct, spironolactone causes sodium and water loss with potassium retention.

337
Q

SIGNS OF CYANIDE TOXICITY?

A

Metabolic acidosis
Increased mixed venous oxygen content
Tachyphylaxis
Tachycardia

338
Q

When does NITROPRUSSIDE MORE LIKELY to generate Cyanide?

A

In general, when nitroprusside is administered faster than 2 μg/kg/min, cyanide is generated faster than the patient can eliminate it.

339
Q

What are the causes of CYANIDE TOXICITY?

A

may be seen with the high-dose administration of: nitroprusside

340
Q

Nerve fibers showing the least sensitivity to the effects of local anesthetics are the:

A

Aα fibers

341
Q

Aα fibers are responsible for

A

motor functions and proprioception.

342
Q

When LAs bind the sodium channel, they render it

A

impermeable to Na, which prevents action potential initiation and propagation

343
Q

LA binds more avidly to

A

Voltage gated Sodium channels in the ACTIVATED (Open) and INACTIVATED (not resting)

344
Q

What is the Henderson-Hasselbach equation

A

pKa= pH + log [ BH+ / B]

345
Q

The basis for classification of LA as either_____ or ______is the ______

A

Aminoamide or aminoester; nature of the chemical bond.

346
Q

Only unmyelinated fibers

A

C fibers

347
Q

Order of blockade first to last

A 
B
Adelta
AGamma
ABeta
AAlpha 
C fibers
348
Q

Neurons resting potentioal

A

-60 to -70mV

349
Q

NA+ K+ pump how many Na and K+?

A

3 sodium out

2 K+ in

350
Q

Conduction move from the one node to the next this is known as

A

Saltatory conduction

351
Q

Specialized regions where the voltage gated sodium channels are concentration

A

Nodes of Ranvier

352
Q

Sympathetics: sensitivity to LA

A

Most sensitive to local anesthetic agents (2-4 levels beyond motor)

353
Q

Pain/touch:sensitivity to LA

A

moderately sensitive (2-3 levels beyond motor)

354
Q

Motor fibers: sensitivity to LA

A

least sensitive

355
Q

Preganglionic autonomics fibers are

A

B fibers

356
Q

The most important physiologic alteration associated with an epidural (as well as a subarachnoid) block is

A

sympathetic blockade

357
Q

The most important physiologic alteration associated with an epidural (as well as a subarachnoid) block is sympathetic blockade – T1 to T4 are the

A

cardioaccelerator fibers which control heart rate and contractility, and their absence leaves one vulnerable to excessive vagal reflexes which can produce sinus arrest.

358
Q

Hypoglycemic agents that inhibit dipeptidyl peptidase-4 (DPP-4), thereby slowing the

A

degradation of incretin hormone and improving postprandial glucose control include: sitagliptin

359
Q

Slow degradation of incretin hormones and improve postprandial hyperglycemia.

A

Dipeptidyl-peptidase-4 inhibitors, such as sitagliptin [Januvia]

360
Q

Dipeptidyl peptidase-4 (DPP-4) Inhibitors medicaiton is

A

Sitagliptin (Januvia)

361
Q

Improve postprandial hyperglycemia.

A

Dipeptidyl peptidase-4 (DPP-4) inhibitors such as JANUVIA

362
Q

Methods of drug delivery that bypass the portal system’s first-pass effect include:

A

Sublingual
Intravenous
Distal rectal placement

363
Q

Routes of administration of drugs bypass the pre-systemic, portal systemic first-pass effect and are delivered rapidly to the superior vena cava

A

sublingual and buccal

364
Q

Drugs placed in the proximal rectum are absorbed into the

A

portal system

365
Q

Agents placed in the distal rectum do not undergo

A

presystemic elimination.

366
Q

Routes of administration of drugs bypass the pre-systemic, portal systemic first-pass effect and are delivered to where?

A

rapidly to the superior vena cava

367
Q

Etomidate: Induction doses are associated with frequent myoclonic movements secondary to

A

loss of cortical inhibition.

368
Q

The mechanism of action of etomidate appears to be

A

augmentation of GABA gated chloride currents.

369
Q

Etomidate inhibits

A

cortisol synthesis resulting in increased morbidity and mortality in ICU patients when used as a prolonged infusion

370
Q

This drug increase the plasma level of Etomidate as well as prolong the elimination half-life of the drug.

A

Fentanyl has been shown

371
Q

As compared with plasma osmolality, hypertonic crystalloid solutions include:

A

D5 0.45NS

372
Q

Normal plasma osmolality ranges between

A

280 - 290 mOsm/L.

373
Q

Both Ringer’s lactate and D5 0.25NS are isotonic solutions, with tonicities of

A

273 and 355 mOSm /L respectively.

374
Q

D5 0.45NS is hypertonic with a tonicity of

A

406 - 432 mOsm/L.

375
Q

D5W is hypotonic in relation to plasma, with a tonicity

A

253 mOsm/L.

SEE NCE Boards CoreConcepts (44 decks)

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