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SRNAPharmacology I > Basics of Pharmacology Pharmacokinetics Part I > Flashcards

Basics of Pharmacology Pharmacokinetics Part I Flashcards

Pharmacodynamics, Pharmacokinetics

1
Q

6 concepts of pharmacokinetics measurementsVECBEC

A 
Bioavailability
Volume of distribution
Clearance
Elimination
Context-sensitive half-time
Effect site equilibration time
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2
Q

What are two concepts more useful to the anesthesia providers more than elimination half-life?

A

Context sensitive half time

Effect-site equilibration time

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3
Q

Define Absorption

A

Is the passage of the drugs through physiological and biological membranes before reaching the systemic circulation

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4
Q

What happens when drugs are given extra-vascularly? What must take place?

A

Absorption

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5
Q

Define Pharmacokinetics? List the four processes that is studies?

A

It is the quantitative study of Absorption, Distribution, Metabolism, and Excretion of the drug and its metabolites

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6
Q

Pharmacokinetics is what the______does to the ______

A

Body ; drugs

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7
Q

Pharmacokinetics is the relationship between the

A

Drug dose and concentration in plasma or at the site of action

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8
Q

Systemic absorption depends on multiple physiochemical properties of the drug : What are 4 physio-chemical properties of the drugs that absorption depends on (2 most important first) DDMP

A

a) Drug lipid solubility
b) Degree of Ionization of the drugs
c) Molecular size
d) pKa

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9
Q

The anatomy and physiology functions at the site of absorption may also affect absorption? how?

A

Cell membrane
pH at the site of absorption
Surface area at the site of absorption
Blood flow to the site of absorption

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10
Q

What form of the drug can pass through the cell membrane? Ionized or non-ionized? Why?

A

NON-IONIZED: Because the non-ionized form is lipophilic.

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11
Q

REMEMBER: The cell membrane is highly permeable to _______ ______substances

A

Lipid soluble

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12
Q

Define passive diffusion? Is energy required from passive diffusion?

A

It is the PASSIVE movement of molecules from an area of high concentration to an area of low concentration.
NO

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13
Q

What is the main process by which most drugs cross the cell membrane ?

A

Passive diffusion

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14
Q

What determines the driving force of passive diffusion ? The greater the concentration , the (slow/fast) ______the movement

A

it is the difference in drug concentration between the 2 sides of the cell membrane.

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15
Q

What does the Fick’s Principle or Law describes?

A

The rate of transfer of drug molecules across the membrane.

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16
Q

The rate of diffusion across a membrane is calculated by which formula? Explain variables
Q/t? K? A? Cp ? Ct? D?

A

Q/t = KxAx (Cp - Ct) / D

q/t : rate of diffusion
K: Diffusion coefficient
A: Surface area of the membrane over which the drug may be absorbed
Cp - Ct is the concentration gradient , (P) plasma and (t) tissues
D: The thickness of the membrane.

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17
Q

2 additional factors affecting rate of diffusion?

A

Molecular size and Blood flow

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18
Q

How does solubility affect the rate of diffusion?

A

The greater the lipid solubility, the faster the rate of diffusion

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19
Q

Define ACTIVE TRANSPORT? is energy needed for active transport?

A

Active transport is the movement of molecules from an area of low concentration to an area of high concentration. YES, ATP or other molecules

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20
Q

What is the movement of molecules against a concentration gradient?

A

ACTIVE TRANSPORT

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21
Q

Active transport requires a ________that bind to the drug and to form a _______ -______Complex that shuttles the drug across the membrane then dissociates on the other side of the membrane/

A

CARRIER, drug-carrier

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22
Q

IMPORTANT: _______ _______(2) Plays an important role in ______ and _______ secretions of drugs and their metabolites.

A

ACTIVE TRANSPORT

Renal and biliary

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23
Q

What is the difference between facilitated diffusion and PASSIVE Diffusion? How are they similar?

A

Facilitated diffusion requires a carrier? They both move drugs molecules from area of high concentration to an area of low concentration.

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24
Q

Weak acids and weak bases are administered in solution as _______ forms of the drugs

A

SALTS

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25
Q

Characteristics of Ionized vs non-ionized drug molecules: Pharmacological effect : Ionized (Y/N) non-ionized (Y/N)

A

I -> NO

NI -> YES

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26
Q

Characteristics of Ionized vs non-ionized drug molecules: SOLUBILITY

A

I –> WATER

NI –>LIPIDS

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27
Q

Characteristics of Ionized vs non-ionized drug molecules: CROSS LIPID BARRIERS (BBB, GI, Placenta)

A

I –>NO

NI–> YES

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28
Q

Characteristics of Ionized vs non-ionized drug molecules: RENAL EXCRETION

A

I –>YES

NI–> NO

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29
Q

Characteristics of Ionized vs non-ionized drug molecules: HEPATIC METABOLISM

A

I –>NO

NI–> YES

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30
Q

IMPORTANT: Identifying weak acids and bases with drug names: Weak ACID (donate/accepts)______hydrogen ions and combine with (cation/anion)
to form ________. The name of the ______is written first, followed by the name of the _________

A

Donate hydrogen ion
Combine with CATION
Salts
Cation is written first, followed by the salt from of the drug

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31
Q

Give 2 examples of salt form of weak acids?

A

sodium Thiopental
Naproxen sodium
Phenytoin sodium
Any drug starting with “sodium….” “calcium….” magnesium…”

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32
Q

IMPORTANT: Identifying weak acids and bases with drug names: Weak BASE (donate/accepts)______hydrogen ions and combine with (cation/anion)
to form ________. The name of the ______is written first, followed by the name of the _________

A

Accepts hydrogen ion
Combine with ANIONs
Salts
Name of the salt form of the drug is listed followed by the anions

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33
Q

3 examples of salt form of weak bases ?

A

Lidocaine HCL
Bupivacaine HCL
Mepivacaine HCL

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34
Q

Morphine sulfate is a weak (acid or base ) ? think about the charge of sulfate..

A

Base

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35
Q

What is the function of the Henderson Hasselbach Equation?

A

Helps predict the degree of ionization of a drug in solution, given the pH of the solution and the pKa of the drug.

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36
Q

General formula of the Henderson Hasselback Equation?

A

pH = pKa + log [base/acid]

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37
Q

General formula of the Henderson Hasselback Equation for weak acid?

A

pH = pKa + log [A-] / [AH]

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38
Q

General formula of the Henderson Hasselback Equation for weak acid?

A

pH = pKa + log [B] / [BH+]

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39
Q

What characteristics of the drug determines the relative amount/fraction of the drug in the ionized /non-ionized form Also affects

A

pH

Absorption and the drugs onset of action

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40
Q

What are 2 examples of drugs that we cannot determine whether or not they are acids or bases based solely on their names?

A

Propofol

Etomidate

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41
Q

Define pKa?

A

It is the pH at which, the drugs is 50% iodized and 50% non-iodized.

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42
Q

When the pH = pKa?

A

50% of the drug is iodized and 50% of the drug is non-iodized

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43
Q

The lower the pKa –> the _______ acid ;

A

Stronger

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44
Q

the Higher the pKa –> the ______base;

A

base

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45
Q

GENERAL PRINCIPLE

  • when the pH < pKa, the ____________ or_____ form dominates
  • when the pH > pKa, the Fa__________or _________form dominates
A

NON-IONIZED form or PROTONATED

IONIZED FORM or UNprotonated form dominates

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46
Q

IMPORTANT: For weak ACID, when the pH is LOWER than the pKa, the __________form dominates

A

non-ionized form

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47
Q

IMPORTANT: For weak ACID, when the pH is LOWER than the pKa, the __________form dominates

A

non-ionized form (lipid soluble)

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48
Q

IMPORTANT: For weak ACID, when the pH is HIGHER than the pKa, the ___________form dominates

A

IONIZED form (water soluble)

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49
Q

IMPORTANT: For weak BASE, when the pH is LOWER than the pKa, the ___________form dominates

A

IONIZED (water soluble)

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50
Q

IMPORTANT: For weak BASE, when the pH is HIGHER than the pKa, the ___________form dominates

A

Non-ionized form (lipid soluble)

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51
Q

REMEMBER: The nonionized portion of the drug is more ________soluble therefore can cross the membrane

A

lipid

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52
Q

If a patient with has an altered pH or the tissues where the drug is being administered is altered, what will happen?

A

refer to pka and ph relationships in both weak acid and weak bases

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53
Q

What is the most important determinant of Drug distribution?

A

Lipid solubility

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54
Q

The more lipid soluble _________ (smaller, larger) volume of distribution.

A

The LARGER the volume of distribution

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55
Q

What is Distribution?

A

The passage of drugs from the bloodstream to the body tissues and organs

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56
Q

What is the VOLUME OF DISTRIBUTION? (IMPORTANT)

A

IMPORTANT: Relates the amount of drug in the body to the measured concentration in the plasma or blood

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57
Q

EASIER youtube definition of Volume of distribution?

A

How extensive the drugs is distributed to the rest of the body when compared to plasma or blood.

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58
Q

What is the formula for Vd?

A

Vd = Dose (Amount of Drug)/ Concentration

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59
Q

VD Definition you tube

A

Ratio of the total amount of drug in the body TO the CONCENTRATION In Plasma

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60
Q

Knowing the Vd allows you to estimate: (PAT)

A

Peak serum levels of the drug following an
IV bolus
Amount of drug in the body
The clearance of a drug

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61
Q

Vd is IMPORTANT because it determines the ________dose of the drugs required to achieve a particular ______ _______ _________immediately after the dose is administered

A

Loading; steady state concentration of the drug

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62
Q

Describe the relationship of Vd to Protein binding

A

Vd is INVERSELY PROPORTIONAL to protein binding

63
Q

The extent of protein binding is directly related to_________

A

LIPID SOLUBILITY

64
Q

As protein binding increases, drug clearance ________

} as protein binding decreases, drug clearance ________

A

decreases

increases

65
Q

What is the major Plasma proteins that bind to ACIDIC drugs?

A

ALBUMIN

66
Q

What is the major plasma proteins that bind to BASIC drugs.

A

Alpha 1 Acid GLYCOPROTEIN

67
Q

Proteins plasma that bind to drug include

A 
AALIE
Albumin
Alpha 1 Acid glycoprotin
Liproprotein
Immunoglobulin
Erythrocytes
68
Q

For a drug metabolized by the liver, binding to plasma proteins prevents the drug from entering the __________ (what cells) resulting in
(increased/decreased )drug metabolism

A

decreased

69
Q

List 4 drugs that are highly protein bound?

A

Propanolol
Diazepam
Phenytoin
warfarin

70
Q

Alterations in protein binding are only important for drugs that are highly
protein bound.

A

PROTEIN BOUND

71
Q

True or False: Drug metabolism can result in the formation of inactive metabolites OR active metabolites whose
pharmacologic activity is equal to, greater than, less
than, or completely different from that of the parent
drug

A

True

72
Q

What is the primary organ responsible for drug metabolism

A

Liver

73
Q

The majority of drugs is catalyzed by the _________ ________system

A

CYP 450 enzymes system

74
Q

Most, but not all, anesthetic drugs are cleared by _________ -___________

A

Hepatic biotransformation

75
Q

__________must be metabolized by several liver CYP 450 enzymes to its active metabolite

A

Clopidogrel

76
Q

PRODRUGS

A

Inactive, until metabolized into active metabolites

77
Q

What is the net effect of METABOLISM

A

the net effect of metabolism is to render drugs more POLAR, and into WATER SOLUBLE METABOLITES so that they can be excreted through the kidneys

78
Q

When Lipid-soluble pharmacologically active drug is converted into more water-soluble and often pharmacologically inactivemetabolites. This results in:
________ (inc/Dec) vd and ______ (inc/dec)clearance by the _______ and _________

A

Decrease in the Vd in the body

Increase clearance by the kidneys and liver.

79
Q

What does the enzyme of a phase I reaction do?

A

It introduces the drug or expose a functional group that makes the drug more water soluble

80
Q

What does the net effect of phase I reaction in terms of phase II and excretions

A

Phase I reaction prepare the drug for phase II conjugation reaction or excretion

81
Q

Phase I reactions generally result in drug (activation/inactivation) __________although this is not always the case, for example__________

A

inactivation: Prodrugs

82
Q

Enzymes responsible for phase I reactions are called

A

Phase I enzymes

83
Q

What is the main enzyme responsible for phase I reactions?

A

Cytochrome P450 Enzymes family

84
Q

The enzyme systems involved in phase 1 reactions are located PRIMARILY in the _______ _____(organelles)

A

ENDOPLASMIC RETICULUM

85
Q

List most common enzymes in phase I reactions

A

Hepatic microsomal enzymes: CYP and
Flavin containing monooxygenases (FMOs)
Non-Hepatic microsomal enzyms: Alcohol dehydrogenase

86
Q

What are the hepatic microsomal enzymes in phase I reactions

A

CYP 450 and FMO(flavin containing monooxygenases)

87
Q

What are the NON-hepatic microsomal enzymes in phase I reactions

A

Alcohol dehydrogenase

88
Q

Phase I Reactions all require

A

Oxygen
NADPH
NADPH Cytochrome p450 reductase

89
Q

The CYP 450 oxidation reaction process splits _______one_______atom goes to form H2O and the other produces an oxidized molecule of drug (R=O)

A

oxygen ; oxygen

90
Q

Examples of oxidative metabolism reactions include:

A

Hydroxylation (midazolam)
Deamination (remove amine (-NH3)
Desulfuration (remove sulfur (-S)
Dealkylation (remove -CH3) (Morphine –>Normorphine)

91
Q

_________system is essential for _________ reactions

A

Cyp 450; reduction

92
Q

Reduction: Occurs under_______oxygen states and CYP 450 enzymes transfer electrons directly to a substrate

A

low

93
Q

Define hydrolysis?

A

reaction that add water to a molecule making the molecule more water soluble.

94
Q

is CYP 450 involved in HYDROLYSIS REACTIONS

A

NO

95
Q

Involved in hydrolysis reactions,name 2 enzymes and what they do?

A

Esterase (hydrolysis of ester bonds)

Amidase (hydrolysis of amide bonds )

96
Q

What are they types of Phase I reactions

A

Oxidation
Reduction (occurs in low oxygen states)
Hydrolysis

97
Q

Meperidine and local anesthetics (i.e.: lidocaine HCl, cocaine HCl) all undergo what kind of reaction? ________ does it require CYP 450 enzymes?

A

all undergo hydrolysis reactions

98
Q

Phase I hydrolysis of succinylcholine by_______ __________

A

plasma

butyrylcholinesterase

99
Q

Phase II conjugation reactions involve the addition of an

_______ ________called __________agent onto another molecule

A

ENDOGENOUS Susbstrate; conjugating agent

100
Q

3 examples of conjugating agents

A

Glucuronic acid
Glutathione
Glycine

101
Q

What is the net effect of the binding of a conjugating agent to the drug?

A

The drug become highly polar and THERE IS A COVALENT BOND to facilitate excretion through kidney or bile

102
Q

Conjugation reactions increase ______,_______,-_______ of the drugs.

A

Hydrophilicity, detoxification and excretion

103
Q

What is the most common type II conjugation reaction

A

GLUCURONIDATION

104
Q

Glucuronidation is an important metabolic pathway for several drugs used during anesthesia, _______ ,________,_______

A

propofol, morphine, and

midazolam

105
Q

All of the phase II reactions occur in the _______, with the exception of glucuronidation which occurs in the ________ _______

A

cytosol; endoplasmic reticulum

106
Q

*****Phase II reactions generally (begin/Terminate) -_________the biological activity ofthe drug, however, there are some exceptions to this rule. Morphine undergoes a ____________reaction to form the __________ which is a more _______ opioid than morphine itself.

A

terminate; glucuronidation ; 6-glucuronide metabolite; potent

107
Q

Name other phase 2 REACTIONS other than glucuronidation

MAGS

A

Methylation
Acetylation
Sulfation
Glutathione conjugation

108
Q

All phase II reactions occur in the __________while GLUCURONIDATION occurs in the ___________

A

Cytosol; Endoplasmic Reticulum

109
Q

Weak acids are excreted RAPIDLY in ______(base/acidic) urine. why?

A

Base or ALKALINE; Because alkalinization of the urine results in more IONIZED drug that cannot be reabsorbed (reabsorption only lipid soluble ions) but can readily cross the renal membrane (Because they are ionized)

110
Q

Renal blood flow and Creatinine Clearance is inversely correlated with _____

A

Age

111
Q

Pharmacokinetics assume that plasma will

A

equillibrate with an effect compartment to produce pharmacodynamic activity.

112
Q

ph of plasma ~7.4, favoring the

A

IONIZED FORM of the drug.

113
Q

If you’re using a local anesthetics, and the skin is inflammed? is it the same pH

A

Inflammed skin may have different pH

114
Q

Ion trapping mechanism

A
  1. Concentration difference develop on two sides of the membrane that separates fluids with different pH’s
  2. because of the pH difference, the degree of ionization of a drug is also different on each side of the membrane
  3. the non-ionized lipid-soluble fraction of a drug equilibrates across cell membranes but the total concentration of drug is very different on each side of the membrane because of the impact of pH on the fraction of drug that exists on the ionized form.
115
Q

Explain the ion trapping mechanism

A
  1. Concentration difference develop on two sides of the membrane that separates fluids with different pH’s
  2. because of the pH difference, the degree of ionization of a drug is also different on each side of the membrane
  3. the non-ionized lipid-soluble fraction of a drug equilibrates across cell membranes but the total concentration of drug is very different on each side of the membrane because of the impact of pH on the fraction of drug that exists on the ionized form.
116
Q

Acetylsalicyclic acid is a weak organic acid with pKa of 3.5. what form of ionization will predominate at physiologic ph =7.4

A

Since the pH>Pka the weak acid drug Acetylsalicylic acid will exist PREDOMINATELY in it IONIZED FORM at physiologic pH

117
Q

Base molecules in an ACIDIC environment will stay _______ and will/will not ____cross membranes

A

IONIZED; not

118
Q

Base molecules in a more ALKALINE ph will become _________ and will/will not ______cross membranes

A

non-ionized

119
Q

Examples of ion trapping

A

Local anesthetics via epidural can cross placenta. Become trapped in the fetus and accumulate because the fetus is more acidic than the mother pH .

120
Q

Fetal pH _____ than the mother pH. can lead to ____ toxicity

A

lower; fetal

121
Q

The _____ -soluble _____fraction of local anesthetics crosses the placenta is converted to the poorly lipid-soluble ________fraction in the more ______environment of the fetus.
The ionized fraction in the fetus can/cannot easily cross the placenta to the maternal circulation and thus is effectively “trapped” in the fetus But the conversion of the NON-IONIZED To IONIZED

A

lipid; non-ionized; ionized; acidic
Cannot; “trapped”
Maintains a gradient for continued passage of local anesthetics from mom into the fetus.

122
Q

________ _______and fetal_______ wil most facilitate

A

trapping of local anesthetics in the fetus.

123
Q

To increase urinary excretion of weak acid and weak base you do what ? why?

A

you need to change the urinary pH to favor the charged form of the drug .
Because the charged form of the drug cannot readily pass through biological membranes and will not be reabsorbed from the nephron.

124
Q

Weak acids are excreted faster in ? why? what do you do then ?

A

ALKALINE pH; because anion form favored; ALKALINIZE the urine

125
Q

Weak bases are excreted faster in ? why? what do you do then ?

A

ACIDIC pH: because cation form favored; so you ACIDIFY the urine.

126
Q

2 drugs with LARGE FIRST PASS HEPATIC MECHANISM? what does it cause

A

Lidocaine
Propofol
Different IV and PO doses

127
Q

What happens during first pass mechanism

A

Enzymes in the intestinal flora, intestinal mucosa, and liver can metabolize prior the medication reaching the systemic circulation

128
Q

When drugs are given EXTRAVASCULAR what must take place for the drug to reach the systemic Circulation

A

ABSORPTION MUST TAKE PLACE>

129
Q

Drugs administered intravascularly have a bioavailability of

A

100%

130
Q

Oral administration is the most _______ and _______.

A

convenient and common

131
Q

For most drugs, the optimum site for drug absorption after oral administration is the_______ _______ _____ why?

A

DUODENUM REGION OF THE UPPER PORTION of the SMALL INTESTINE
because increased surface area due to presence of MICROVILLI
Highly perfused with capillaries.

132
Q

Route of administration with most predictable plasma concentrations

A

IV

133
Q

What explains why SUBLINGUAL NTG is effective and oral NTG is ineffective

A

VENOUS DRAINAGE into the superior vena cava bypass the liver and AVOIDS first pass hepatic effect.

134
Q

Sustained therapeutic plasma concentration with decreased peak and valley route____daily dose

A

TRANSDERMAL ;10mg

135
Q

Transdermal absorption dependent one:

A

STRATUM CORNEUM THICKNESS rate limiting step accross layer

136
Q

Drugs administered in the proximal rectum are absorbed into the _________ and distal rectum admin bypass _______

A

SUPERIOR HEMORRHOIDAL VEINS

first pass effect.

137
Q

Determinants of drug distribution include

A 
Lipid solubility :  more better distribution
Protein binding
Blood flow rate to the tissue
Molecular size of the drug 
Degree of ionization .
138
Q

It is the only the ____, _____ drug that is available to cross membranes into tissues

A

Free, unbound

139
Q

Vd is the ____parameter which relates the ______ __ ______ to the Measured _________in the _________

A

Pk: amount of drug; concentration in the plasma

140
Q

High protein binding limits_______ ________ to leave the plasma and penetrate organs

A

Protein binding

141
Q

Highly plasma protein binding drugs are contained in plasma and have ______ Vd comared to drugs with low binding to plasma proteins

A

SMALLER

142
Q

The fraction of total drug plasma that is bound to protein is determined by

A

Plasma concentration of drug
Affinity of binding sites for the drug
The number of proteins binding site

143
Q

Know ______before you administer phenytoin

A

ALBUMIN LEVEL

144
Q

For drug metabolized by the liver, binding to plasma proteins prevents the drugs

A

from entering hepatocytes resulting in decreased drug metabolism

145
Q

For highly protein bound drug are _____molecules and they are unable to diffuse through capillaries as a result, _____ drugs is able to under _____ _______

A

LARGE: less drugs is able to undergo glomerular filtration

146
Q

Drug metabolism can result in the formation of _______ _______OR _____ metabolites whose pharmacologic activity is

A

equal, greater than, less than or completely different from parent drug.

147
Q

For LOW protein bound drugs changes in protein binding are not as

A

CLINICALLY SIGNIFICANT

148
Q

2 drugs metabolized through HOFFMAN ELIMINATION

A

CISATRACURIUM

ATRACURIUM

149
Q

PRIMARY net effect of DRUG METABOLISM

A

production of more polar, water-soluble metabolites that are MORE EASILY EXCRETED From the BODY.

150
Q

When metabolism transformed meds from lipid soluble to water-soluble what happens?

A

Decrease in the Vd

Increase clearance by liver and the kidney.

151
Q

2 drugs with active metabolites

A

DIAZEPAM

MEPERIDINE

152
Q

This drug _________Must be metabolized by several Liver CYP450 enzymes to its active metabolites

A

CLOPIDOGREL.

153
Q

Pathways of drug metabolism may be divided into 2 MAJOR GROUPS of reactions

A

Phase I functionalization reactions

Phase II CONJUGATION REACTIONS

154
Q

_________ of morphine to _______ which is the ______ ______

A

Demethylation; NORMORPHINE; active metabolites.

SRNAPharmacology I (29 decks)

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