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Pharmacology > 1D1 > Flashcards

1D1 Flashcards

1
Q

IV abbreviation

A

intravenous

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2
Q

IM abbreviation

A

intramuscular

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3
Q

SC abbreviation

A

subcutaneous

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4
Q

what are the barriers that the drug can pass

A

GI tract - enteral

IV - parental “around GI”

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5
Q

BSA equation

A

square root (ht*wt/3600)

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6
Q

inches to cm

A

2.54 cm/in

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7
Q

lbs to kg

A

1kg/2.2lbs

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8
Q

what is the full flow in adults

A

50 cc/kg

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9
Q

what is the full flow in neonates

A

150 cc/kg

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10
Q

what is the CI full flow for adults

A

2.4

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11
Q

what is the CI full flow for neonates

A

2.6-3.0

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12
Q

what is pharmacokinetics

A

what the body does to a drug

refers to the movement of drug into, through, and out of the body

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13
Q

pharmacokinetics is the time course of its

A

absorption, bioavailability, distribution, metabolism, and excretion

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14
Q

what is pharmacodynamics

A

what a drug does to the body

the relationship b/w drug concentration at the site of action and the resulting effect

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15
Q

what does pharmacodynamics involve

A

receptors, binding, post receptor effects, and chemical interactions

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16
Q

the effect of a drug present at the site of action is determined by

A

that drug’s binding with a. receptor

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17
Q

what is drug absorption

A

is the transfer of a drug from the site of administration to systemic circulation.

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18
Q

the main factor that relates to absorption is

A

the route the drug enters the body

it come in contact w/ several membranes. Drugs pass some membranes but not others

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19
Q

Two major routes of administration

A

– Enteral: Administration by mouth, enters through mucosal membrane
– Parenteral: Administration of a drug directly into systemic circulation or vascular tissue

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20
Q

Physiological considerations in absorption are :

A

– blood flow
– total surface area
– time of arrival of the drug and time of drug at absorption site.

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21
Q

Other considerations for absorption are

A

solubility, chemical stability and how soluble the drug is in lipids

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22
Q

Enteral Administration (PO)

A

Oral Administration, Sublingual, Buccal, and Rectal

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23
Q

advantages of enteral admin

A

Can be self administered and over-dose can be over come by antidote (activated charcoal).

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24
Q

disadvantages of enteral admin

A

Drugs absorbed in the GI tract enter portal (hepatic) circulation before being distributed into systemic circulation. These drugs will undergo first pass metabolism in the liver which limits the efficacy of the drug. First pass metabolism decreases the amount of drug that enters systemic circulation.

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25
Q

Parenteral

A

direct delivery of drugs into systemic circulation

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26
Q

what are some examples of parenteral delivery

A 
– Intramuscular (IM) Lipid based drugs are absorbed slowly and aqueous based drugs are absorbed rapidly.
– Intravascular (IV)
– Subcutaneous (SC)
– Intrathecal (IT)
– Intraperitoneal (IP)
– Intradermal (ID)
– Inhalation
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27
Q

advantages of parenteral delivery

A

Provides rapid onset of pharmacologic effect and maximum control over circulating levels of drug. A

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28
Q

disadvantages of parenteral delivery

A

Unlike drugs administered via the GI tract, drugs given IV cannot be recalled by strategies like emesis or binding to activated charcoal. Requires specialized training to gain IV access. Potential risk of systemic infection from IV site.

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29
Q

Bioavailability

A

is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation

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30
Q

if 100 mg of a drug is given and 70 mg are absorbed unchanged into systemic circulation, what is the bioavailability

A

0.7 or 70 %.

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31
Q

Factors that influence bioavailability include:

A

irst pass hepatic metabolism

– Solubility of the drug!

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32
Q

fat is very hydrophilic drugs are poorly absorbed because

A

they cannot pass through lipid dense cell membranes.

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33
Q

Extremely hydrophobic drugs are also poorly absorbed because

A

the are insoluble in aqueous body fluids.

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34
Q

what drugs are absorbed most readily

A

small non-ionized lipid soluble drugs

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35
Q

drug associated factors

A
  • passive diffusion
  • facililtated diffusion
  • aqueous channels
  • active transport
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36
Q

Passive diffusion:

A

fast for lipophilic, nonionic and small molecules. Slow for hydrophilic Ionics, or large molecules

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37
Q

Facilitated diffusion

A

is the process of spontaneous passive transport of molecules or ions across a biological membrane via specific transmembrane integral proteins
Chemically similar drugs compete for a carrier

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38
Q

Aqueous Channels

A

Small hydrophilic drugs diffuse by concentration gradients (high&raquo_space;>low) thru aqueous pores.

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39
Q

Active transport:

A

Same as facilitated diffusion except that ATP powered drug transport against concentration gradient (low»high)

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40
Q

Patient-associated factors that affect drug absorption

A

– food in GI tract
– renal disease
– liver disease

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41
Q

Drug Distribution

A

drug leaves the bloodstream and enters the extra-cellular fluid and or cells of tissue.

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42
Q

Drugs are distributed into

A

major body fluids

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43
Q

Delivery of a drug to the extra-cellular fluid depends on: (4)

A
  1. blood flow
  2. capillary permeability: membrane permeability
  3. degree of protein binding to plasma proteins
  4. relative solubility of the drug
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44
Q

Some drugs can not cross the blood-brain barrier therefore

A

they will not work in the brain

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45
Q

what are some barriers the drug must break thru

A

blood brain barrier
blood-placenta barrier
blood-testes barrier

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46
Q

the binding of drugs to proteins such as albumin results

A

in less drugs free (not bound) in the blood available to enter the target organ.

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47
Q

Depot Storage

A

a body area in which a substance, e.g., a drug, can be accumulated, deposited, or stored and from which it can be distributed

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48
Q

Lipophilic drugs get stored and accumulate in

A

fat

these drugs are released slowly from fat stores

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49
Q

calcium binding drugs accumulate in

A

teeth and bone

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50
Q

heparin is heavily bound to

A

proteins

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51
Q

Volume of distribution (Vd ):

A

calculated value of volume that would be required to contain the d
administered dose that was evenly distributed at the concentration measured in plasma.

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52
Q

if the Vd = 3 liters, where does it get distributed to?

A

distributed in plasma only (plasma volume = 3 liters).

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53
Q

Vd = 16 liters is likely distributed in

A

extracellular water (3L+13L)

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54
Q

Vd >46 liters is likely sequestered in

A

a depot because the body only contains 40-46 liters of fluid.

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55
Q

In general, drugs with a short T1/2 have

A

a small VD and rapid clearance

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56
Q

Drugs with a long T1/2 (lipid soluble) have

A

a larger VD and slower elimination rate.

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57
Q

Drug Metabolism

A

the biotransformation process of making a drug more polar and water soluble

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58
Q

Biotransformation occurs mainly in

A

the liver and is therefore often called hepatic metabolism.

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59
Q

Metabolic reactions can transform

A

– An active drug into less-active or inactive forms

– a PRODRUG (inactive or less-active drug) into a more active drug (Plavix)

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60
Q

drug metabolism is split into what two phase

A
  • phase 1 (non-synthetic)

- phase 2 (synthetic)

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61
Q

phase 1 of drug metabolism is when

A

drugs oxidized or reduced to a more polar form

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62
Q

what is an example of phase 1 drug metabolism

A

Cytochrome P450 (liver microsomal) drug oxidation, reduction and hydrolysis

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63
Q

phase 2 of drug metabolism is when

A

a polar group is conjugated to the drug

this increase the clarity of the drug

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64
Q

Drugs undergoing phase II reactions may have already undergone

A

Phase 1

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65
Q

what is an example of phase 2 drug metabolism

A

glutathione

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66
Q

Drug Excretion

A

the elimination of the un-metabolized drug and its metabolites from the body

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67
Q

most drugs are excreted in

A

urine via active glomerular filtration

-others in feces or expired air

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68
Q

what is enters-hepatic ciruclation

A

when drugs are excreted in the feces, the bile may become concentrated before entering into the intestines

this can extend the duration of the drug in the body

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69
Q

Drug excretion in the urine is affected by

A

Glomerular filtration
Tubular Secretion
Tubular Reabsorption

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70
Q

Because drugs, metabolites, and toxins are concentrated in the kidney, the kidney is at risk for what

A

chemical induced toxicity

-renal failure patients may be due to drug accumulation

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71
Q

drug clearance

A

Volume of fluid that would be completley cleared of drug per unit time

  • can be directly measured in the body
  • calculated value in liters/hr
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72
Q

clearance equation

A

Elimination rate (mg/hr)/ Drug Concentration (mg/L)

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73
Q

Elimination half-time (t 1/2)

A

time necessary for plasma concentration to decrease by 50%.

  • shortened with small Vd and rapid clearance
  • Prolonged with high lipid solubility and large Vd.
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74
Q

Zero order kinetics

A

rate of elimination is constant, independent of drug concentration (i.e. alcohol, phenytoin, salicylates)

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75
Q

First order kinetics

A

rate of elimination occurs dependent of drug concentration

- the higher the t1/2, the less percentage of drug remains

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76
Q

if the t 1/2 = 1, how much remains

A

1/2

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77
Q

if t 1/2 = 5, how much remains?

A

3.125%

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78
Q

anesthetic properties of hypothermia

A

Increased solubility of volatile anesthetics

79
Q

during hypothermia, fluid shifts from ____ space to ____ space altering ___

A

intravascular space to interstitial space altering Vd

80
Q

hypothermia causes a ____ absorption of drugs administered routes other than IV

A

decreased

81
Q

drugs with pulmonary uptake are sequestered during

A

CPB and released when CPB is terminated

82
Q

hepatic clearance of drugs altered by

A

altered hepatic blood flow and drugs administered during CPB like vasopressors

83
Q

hypothermia causes activation of what

A

autonomic and endocrine reflexes which alters peripheral vasoconstriction

84
Q

peripheral vasoconstriction results in decreased re-uptake of

A

drugs from peripheral tissues

85
Q

hypothermia inhibits

A

enzyme function therefore decreasing metabolic function

86
Q

hypothermia decreases in clearance causes

A

increased t1/2

drug excretion secondary to decreased GFR, renal perfusion, and tubular secretion

87
Q

hypothermia causes a decrease release of

A

excitatory neurotransmitters such as glutamate and glycine

88
Q

hemodilution causes a sudden increase in

A

Vd due to prime volume

89
Q

hemodilution cases a decrease in _____, which will result in alteration of bound vs free fraction of drugs

A

protein binding

90
Q

hemodilution causes a immediate decrease in what? which will ultimately affects drugs sequestered to RBCs

A

Hematocrit

91
Q

hemodilution dilutes

A

plasma level of drugs

92
Q

hemodilution alters what, which will affect distribution and clearance

A

blood organ flow affecting distribution and clearance

93
Q

once hemodilution occurs, ,the drug travels where?

A

down it’s concentration gradient to facilitate equilibrium, restoring the state of increased free fraction during and after CPB

94
Q

hemodilution causes ____ ____ between central and peripheral compartments

A

volume distribution

95
Q

during Hemodilation, what acid and base and electrolyte changes occur? (3)

A

a) Acidosis from CPB affects response to catecholamine
b) pH vs alpha stat blood gas strategy affect degree of ionization and protein binding
c) acid-base changes can alter electrolyte balance

96
Q

what size membrane is the hemoconcentration?

A

70 kDa membrane to remove plasma water

97
Q

what can and can’t pass through hemoconcentrator

A

can’t b/c too large: cellular components in blood, RBC, WBC, Plasma, platelets

can: small water soluble drugs, ions, metabolites

98
Q

Sieving Coefficient

A

is the ratio of ultrafiltrate [Cf ] of a solute to the plasma [ Cp]
of that solute. In other words, how readily a solute is pulled off

99
Q

cell save causes a loss of what

A

blood plasma

drugs that are bound to plasma proteins and drugs that are circulating free in plasma

100
Q

in cell saver, there is an increase in _____ and decrease in _____

A

increase in edema

decrease in oncotic pressure

101
Q

pharmacodynamics is

A

what a drug does to the body

102
Q

pharmacodynamics involves

A
  • receptor binding
  • post receptor effects
  • chemical interactions
103
Q

pharmacodynamics is the relationship b/w

A

drug concentration at the site of action and the resulting effect

including: time course, intensity, adverse effects

104
Q

the effect of a drug present at the site of action is determined by

A

that drug’s binding with a receptor

105
Q

the plasma membrane of a human cell has what kind of permeable and what does it help control?

A

selectively permeable

helps control what moves in and out of the cell

106
Q

the surfaces of plasma membranes generally have what on them

A

studded with proteins that perform different functions

107
Q

protein molecules are referred to as

A

receptors

108
Q

molecules which bind to receptors are called

A

ligands

109
Q

what is an example of ligands

A

neurotransmitters

hormones or drugs

110
Q

Drug receptors

A

Any cellular macromolecule that a drug binds to initiate its effects.

111
Q

receptors are

A

proteins or glycoprotein present on the cell surface, on an organelle within the cell, or in the cytoplasm

112
Q

when a drug bind to a receptor, one of these actions occur:

A
  1. ion channel is opened or closed
  2. biochemical messenger “2nd messender” is activated
  3. a normal cellular function is physically inhibited
  4. a cellular function is “turned on”
113
Q

definition of drug

A

chemical substance that interacts with a biological system to produce a physiologic effect.

114
Q

the more of an agonist drug occupying a receptor…

A

the greater the response

115
Q

antagonsists are drugs that

A
  • bind to their targets and form a drug- receptor complex without causing activation or response
  • can block the receptor to its endogenous activator, therefore blocking normal function
116
Q

agonists activate the receptors of a produce a response known as

A

full agonists

-have positive efficacy

117
Q

receptor occupancy by antagonists is important if the drug is a

A

competitive antagonist

competes for occupancy with another drug or with the receptor’s normal mediator

118
Q

the amount of drug occupying will determine

A

any response

119
Q

Competitive Antagonist

A

A drug that “competes” with the endogenous ligand for binding to the active site on a receptor.

120
Q

how can competitive antagonist be overcome

A

by increasing the concentration of the agonist.

121
Q

Chemical Antagonist

A

: a drug that binds with another drug that rendering it inactive

122
Q

Irreversible Antagonist:

A

A drug antagonist that cannot be overcome by increasing the agonist concentration (covalent modification).

123
Q

Affinity

A

is a measure of the tightness(strength) that a drug binds to the receptor

124
Q

Intrinsic activity

A

is a measure of the ability of a drug once bound to the receptor to generate an effect activating stimulus and producing a change in cellular activity.

125
Q

drugs that interact with receptors can be classified as being

A

agonists or antagonists

126
Q

Agonists once bound to the receptor can….

A

activate or enhance cellular activity

can be full, partial, or inverse

127
Q

Antagonists can prevent

A

the binding and the action of agonists

128
Q

Antagonists can be

A

competitive or non-competitive

129
Q

Dissociation Constant (KD)

A

the concentration of drug required in solution to achieve 50% occupancy of its receptors

130
Q

Efficacy

A

the degree a drug is able to induce maximal effect.

131
Q

If drug A decrease MAP by 20 mmHg and drug B decreases MAP by 10 mmHg, which has greater efficacy?

A

A has greater efficacy than drug B

132
Q

Potency

A

amount of drug required to produce 50% of the maximal response
that the drug is capable of inducing

133
Q

Effective Concentration 50% (EC50)

A

Concentration of drug which induces a specific clinical effect in 50% of the subjects to which the drug is given

134
Q

Lethal Dose 50% (LD50)

A

Concentration of drug which induces death in 50% of the subjects which the drug is given

135
Q

Therapeutic Index

A

measure of the safety of a drug.

Calculated by dividing LD50/ EC5

136
Q

Margin of Safety

A

margin between therapeutic and lethal dose of drug

137
Q

Altered Absorption

A

drug may inhibit absorption of another drug across biological membrane: ie: anti-ulcer drugs coat the stomach and decrease GI absorption of other drugs

138
Q

Altered Metabolism

A

drugs can alter P450 isoenzymes wich affect other drug actions.

139
Q

Plasma Protein competition

A

drugs that bind plasma proteins may compete w/other drugs for that binding site

140
Q

Altered Excretion

A

drugs may act on the kidney to reduce excretion of specific agents

141
Q

addition

A

response elicited by combined drugs is Equal to the combined responses to the individual drugs. 1+ 1 = 2

142
Q

Synergism

A

response elicited by combined drugs is Greater than the combined responses of individual drugs. 1 +1 = 3

143
Q

Potentiation

A

a drug which has no effect enhances the effect of the second drug. 0 + 1 = 2

144
Q

Antagonism:

A

rug inhibits the effect of another drug. Usually, antagonist has no inherent activity. 1 + 1 = 0

145
Q

Tolerance

A

a decreased response to a drug. Clinically, the dose of a drug must be increased to achieve same effect: ie long term pain management is a metabolic tolerance

146
Q

Downregualtion

A

is decrease number of receptors binding sites ( tolerance) caused by continuous stimulation

147
Q

Upregulation

A

occurs by lack of stimulation causing an increase in the number of receptor binding sites (sensitivity)

148
Q

Dependence

A

a patient needs a drug to “function normally”. Detected when drug is stopped a withdrawal symptoms occur.

149
Q

Withdrawal

A

drug is no longer administered to dependent patient. Symptoms often are the opposite of the effects achieved by the drug.

150
Q

Cross tolerance / cross dependence:

A

tolerance or dependence develops to different drugs which are chemically or mechanistically related. : Methadone replaces heroin

151
Q

how is drug metabolism related to age?

A

drug metabolism is underdeveloped in infants and depressed in the elderly.

152
Q

drugs and pregnancy relationship

A

Some drugs can cross the placenta and affect the fetus. Some drugs enter the milk production

153
Q

drug metabolism and Smoking and drinking habits relationship

A

Both smoking and drinking induce P450 liver enzymes. This accelerates the metabolism of some drugs. Some prodrugs may be metabolized to more active forms and cause toxicity.

154
Q

drug metabolism and Liver and Kidney disease relationship

A

Dose reductions maybe necessary in patients with liver or kidney dysfunction. Failing kidneys excrete fewer drug metabolites. Failing livers metabolize drugs poorly.

155
Q

Pharmacogenetics:

A

some genetic conditions affect drug metabolism

156
Q

Drug interactions

A

what other medications are patients taking

157
Q

Psychosocial factors

A

poor patient compliance is cause of many drug failures.

158
Q

what does heparin cause

A

anticoagulation via binding with antithrombin III and increase its anticoagulant effect at least 1000-fold

159
Q

once AT III is activated by heparin, what happens

A

the major physiologic inhibitor of the conversion of prothrombin II to thrombin IIa and factors IXa and Xa

160
Q

pump prime dose of heparin

A

5,000 to 10,000 units

161
Q

full dose heparin

A

300-400 units/kg given by anesthesia prior to cannulation

162
Q

1/2 life of hepatin

A

1-2 hrs

163
Q

reversal of heparin

A

protamine sulfate (antagonist to heparin)

164
Q

what are antifibrinolytics

A

aminocaproic acid (Amicar) / tranexamic acid (TXA)

165
Q

both antifibrinolytics inhibit

A

fibrinolysis by binding with plasminogen

166
Q

once antifibinolytics bind with plasminogen, what does that cause

A

plasminogen cannot bind to fibrin and cannot activate plasmin
no plasmin activation = no clot breakdown

167
Q

pump prime dose of amicar and TXA

A

amicar: 10 grams
TXA: 1 gram

168
Q

what is albumin

A

blood volume expander

169
Q

5% albumin =

A

oncotically equal to human plasma

170
Q

25% albumin =

A

5x oncotically equal to human plasma

171
Q

albumin may be added to

A

increase the oncotic load of pump prime to help prevent third spacing of crystalloid prime

172
Q

what is mannitol

A

osmotic diuretic that prevents reabsorption of sodium and water in the renal tubule

173
Q

mannitol increase

A

unrinary output

174
Q

mannitol is a ___ ___ ____ scavenger

A

mannitol is an oxygen free radical scavenger

175
Q

what must you make sure before adding mannitol to prime

A

make sure your pt has working kidneys before adding to prime

176
Q

vasopressors treat

A

hypotention

177
Q

vasopressors are used to

A

increase systemic vascular resistance (SVR)

178
Q

what are two common vasopressors

A

phenylephrine and norepinephrine

179
Q

what does phenylephrine bind to and cause

A

binds to alpha1 receptors causing vasoconstriction

-mimics the effect of endogenous NE

180
Q

phenylephrine adult dose

A

100 mcg/ml

181
Q

what does norepinephrine acts at

A

alpha1 and alpha2 receptors to elicit vasoconstriction

182
Q

norepinephrine adult dose

A

16 mcg/ml

183
Q

which vasopressor is more potent vasoactive drug?

A

phenylephrine

184
Q

what are the anti-arrhythmia drug? (3)

A
  1. magnesium
  2. lidocaine
  3. amiodarone
185
Q

magnesium is given when

A

cross clamp is removed to prevent atrial dysthymia’s (SVT)

adult dose: usually 2 grams

186
Q

what is lidocaine

A

Sodium channel blocker that is given when cross- clamp is removed to prevent ventricular dysrhythmia’s

dose: 1-2 mg/kg

187
Q

what does amiodarone affect

A

Affects multiple channels: Potassium (K) channel
blockers
-extend the plateau phase of the action potential by blocking K+ channels
-They effectively prolong repolarization
dose: 150 mg

188
Q

vasodilators treat

A

hypertension

189
Q

what are some vasodilators

A

nitroglycerin and nitroprusside

190
Q

nitroglycerin works by

A

relaxing the vascular smooth muscle inside blood vessels and increasing the supply of blood and oxygen to the heart while reducing its workload

191
Q

what is nitroglycerin MOA

A

via release of nitric oxide (NO)
dilates venous system bigger then arterial system
used to treat high BP and angina

192
Q

nitroprusside primarily dilates

A

arterial system with little effect on venous system

193
Q

MOA of nitroprusside

A

via Nitric Oxide but liberated through different mechanism

-toxic at high doses over prolonged time

Pharmacology (3 decks)

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