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Pharmacology > Chapter 3 - Pharmacokinetics + Pharmacoynamics > Flashcards

Chapter 3 - Pharmacokinetics + Pharmacoynamics Flashcards

1
Q

Pharmacokinetics

A

Study of how a drug moves into, through, and out of the body

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2
Q

Pharmacodynamics

A

Study of how the drug produces its effects on the body

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3
Q

Therapeutic Range/Window

A

A desirable range of drug concentrations

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4
Q

Maximum Effective Concentration

A

The top concentration of the normal therapeutic range - represents the border between concentrations that are beneficial vs. toxic

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5
Q

Minimum Effective Concentration

A

The bottom concentration of the normal therapeutic range below which the drugs will not work sufficiently

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6
Q

Subtherapeutic Concentrations

A

Drug concentrations below the minimum effective concentration

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7
Q

Metabolism

A

The rate at which the body removes the drug by elimination

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8
Q

Route of Administration

A

Route by which the drug dose is to be administered

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9
Q

Loading Dose

A

A larger initial dose that “loads” the body with sufficient drug to establish therapeutic concentrations

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10
Q

Maintenance Dose

A

Smaller than the loading dose, and given at an amount and rate that matches the amount eliminated by the body

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11
Q

Total Daily Dose

A

The combined amount of drug (mass) times the number of doses administered in a given day (dose interval)

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12
Q

Peak Concentration

A

Highest drug concentration

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13
Q

Trough Concentration

A

Lowest drug concentration

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14
Q

Narrow Therapeutic Range

A

Drugs in which the maximum effective dose and the minimum effective dose are very close to each other

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15
Q

Narrow Therapeutic Index

A

The dose that causes the beneficial effect is close to the dose that produces toxic side effects

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16
Q

Parenterally Administered Drugs

A

Drugs are given by injection in the space between the outside of the intestinal tract and the surface of the skin

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17
Q

Intravenously (IV)

A

Drugs are given directly into the vein

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18
Q

IV Bolus

A

Drugs are given as a single large volume one time

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19
Q

CRI (Constant Rate Infusion)

A

Drugs are injected slowly or “dripped” into the vein over a period of several seconds, minutes, or hours resulting in a steady accumulation of drug concentrations

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20
Q

Steady State/Plateau

A

Occurs when peak and trough concentrations don’t change with subsequent doses (bucket analogy)

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21
Q

Extravascular/Perivascular Injection

A

Accidental injection of an IV drug outside the vein

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22
Q

Intraarterial Injection (IA)

A

Injecting a drug into an artery (delivering the full dose to a specific tissue/organ causing very high and potentially toxic concentrations of the drug)

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23
Q

Intramuscular (IM)

A

Parenteral route of administration where the drug is placed into the skeletal muscle

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24
Q

Subcutaneous (SQ)

A

Injections administered under the skin, but above the muscle

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25
Q

Intradermal (ID)

A

Uses very small needles to place drugs into, but not below the narrow layers of the skin (dermis)

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26
Q

Intraperitoneal (IP)

A

Administered into the abdominal cavity

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27
Q

Per Os (PO)

A

By mouth

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28
Q

Per Rectum (rectally)

A

Drugs give via the rectum, typically suppositories

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29
Q

Topically

A

Applied onto the surface of the skin

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30
Q

Aerosol

A

Delivered to the lungs by “air or gas solution”

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31
Q

Passive Diffusion

A

The random movement of drug molecules down the concentration gradient (high–>low concentration) (requires no energy)

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32
Q

Concentration Gradient

A

Movement of drug molecules from an area of high concentration of drug to an area of lower concentration or vice versa.

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33
Q

Hydrophilic

A

Readily absorbing moisture – “water-loving”

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34
Q

Lipophilic

A

Having an affinity for fat – “fat loving”

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35
Q

Equilibrium

A

The number of drug molecules moving from point A to point B is the same number of molecules moving from point B to point A

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36
Q

Facilitated Diffusion

A
  • Passive transport mechanism (no energy)
  • Uses a special carrier molecule from the cellular membrane to move the drug molecule across the membrane.
  • Revolving door*
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37
Q

Active Transport

A
  • Involves a special carrier molecule
  • Occurs only in one direction
  • Cell expands energy
  • Either move the drug molecule across the cell membrane or “resets” the carrier molecule after transportation is completed
  • Electrical pump*
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38
Q

Pinocytosis

A
  • Active transport (uses energy - less common)
  • Cellular uptake of extracellular fluid and its contents by enclosing them in vesicles derived from the plasma membrane
  • cell drinking*
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39
Q

Phagocytosis

A
  • Active transport (uses energy - less common)
  • Endocytosis of particulate material, such as microorganisms or cell fragments
  • The material is taken into the cell in membrane-bound vesicles (aka phagosomes) that originate as pinched-off invaginations of the plasma membrane
    “cell eating”
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40
Q

Saturated

A

Containing as much solute as may be dissolved under stated conditions
- All carrier molecules are continuously occupied in bringing drug molecules across the cell membrane

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41
Q

Transportation Maximum (T-Max)

A
  • Transport system is saturated
  • Transport system is then working at maximum speed
  • crowded toll road*
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42
Q

Aqueous Medium

A

Water-based medium

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43
Q

Polarized

A

Drug molecule contains both positive (+) and negative (-) charges at the ends of the molecule

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44
Q

Ionized/Nonionized

A

Drug molecule contains a net positive (+) OR a net negative (-) charge but not both

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45
Q

Hydrophilic (water-loving) drug molecules are either ______ or _______

A

Polarized or ionized

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46
Q

Lipophilic (fat-loving) drug molecules tend to be ________ and _________ molecules

A

Nonpolarized and nonionized

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47
Q

What are the 4 basic steps of drug Pharmacokinetics?

A

Absorption
Distribution
Metabolism
Excretion (or elimination)

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48
Q

Absorption

A

The movement of drug molecules from the site of administration to the systemic circulation (uptake of substances into or across tissues)

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49
Q

Distribution

A

Movement of a drug from the systemic circulation into tissues

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50
Q

Extracellular Fluid

A

Fluid/water outside of the cells

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51
Q

Basic/Alkaline

A

a pH of 10, 11, or 12

Less H+ ions present

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52
Q

Acidic

A

a pH of 1, 2, or 3

More H+ ions present

53
Q

Acid Drugs

A

A drug whose chemical structure causes it to release a hydrogen ion into its liquid environment as the drug is placed into increasingly alkaline environments
As pH increases, H ion releases

54
Q

Acidic pH

A

A liquid environment where there are many available hydrogen ions floating free in the liquid to react with drug molecules

55
Q

Base Drugs

A

A drug that becomes more ionized when it acquires a hydrogen ion from an acidic pH environment and becomes more nonionized when it releases a hydrogen ion into the liquid of an alkaline pH environment

56
Q

Drugs pKa

A

The negative logarithm of the ionization constant of an acid (Ka); The buffering power of a buffer system is greatest when its pKa equals the pH
Equal numbers of ionized and nonionized drug molecules - The pH level at which this occurs is the pKa

57
Q

Ion Trapping

A

Accumulation of lipophilic/nonionized drug molecules trapped in this body compartment because of their significant shift to the ionized/hydrophilic form.

58
Q

Reabsorption

A

The act of process of absorbing again

59
Q

P-glycoprotein (P-gp)

A

An active transport pump - found in the cells making up the barrier lining the intestinal tract (enterocytes). Actively transports selected molecules out of the cell and back into the lumen of the intestine, preventing their absorption

60
Q

Dissolution

A

Process of breaking down dosage forms to the individual molecules

61
Q

Gastric Motility

A

Stomach contractions that mix stomach contents and move the contents from the stomach into the small intestine

62
Q

Intestinal Motility

A

The mixing and peristaltic contractions of the intestine

63
Q

Hepatic Portal System

A

System of blood vessels that conducts the blood from the capillaries of the GI tract to the capillaries of the l River and allows the liver to remove poisons, toxins, and other potentially dangerous substances absorbed from the GI tract before they reach systemic circulation

64
Q

Xenobiotics

A

A chemical foreign to a given biological system (aka foreign substances or “poisons”)

65
Q

First-Pass Effect

A

The Phenomenon by which the liver removes so much of the drug that little reaches the systemic circulation

66
Q

Perfusion

A

The extent to which tissue is supplied with blood

67
Q

Vasoconstriction

A

Reduced blood flow to an area - decreases perfusion

68
Q

Vasodilation

A

Dilation of blood vessels - enhances perfusion

69
Q

Fenestrations

A

Small holes or “windows” in the capillary walls that allow water and small drug molecules to move readily back and forth between the blood and the surrounding tissue, while keeping larger molecules, proteins and RBCs within the capillary

70
Q

Blood-Brain Barrier

A

Provides an excellent defense against many poisons, but also prevents distribution of beneficial drugs to the brain or CNS.
(Made up of continuous capillary cell wall, membranes of the supporting cells surrounding the capillaries, and the P-glycoprotein active transport molecules)

71
Q

Redistribution

A

Relocating the drug to an area of the body that is less likely to produce adverse reactions

72
Q

Apnea

A

Cessation of breathing

73
Q

Protein Bound Drug

A

Drug molecules attached to the blood protein

74
Q

Free Form

A

Drug molecules not attached to the blood protein

75
Q

Depot-like Effect

A

A drug molecule intentionally formulated to bind to blood protein so that the drug is slowly distributed into the tissue over a more extended period of time

76
Q

Volume of Distribution (Vd)

A

A pharmacokinetic value that provides an approximation of the extent to which a drug is distributed throughout the body
Assessed by looking at the drug concentration in the blood shortly after an IV bolus is given

77
Q

Receptor

A

A specifically shaped protein located on the cells surface or within the cell

78
Q

Affinity

A

The drugs ability to bind or fit with the receptor

79
Q

Intrinsic Activity

A

The ability of a drug molecule to produce a cellular effect when it combines with the receptor

80
Q

Agonist

A

A drug with both a good affinity for the receptor and the ability to produce intrinsic activity

81
Q

Antagonist

A

A drug with good affinity, but little or no intrinsic activity
occupies the receptor site and blocks the effect of any other agonist drug trying to stimulate that receptor

82
Q

Reversal Agents/Inhibitors

A

Drugs that are capable of combing with with a receptor and blocking the receptor site from exogenous (from outside the body) agonist drugs and “reversing” or nullifying the effect of the agonist drug

83
Q

Blockers

A

Antagonist drugs that occupy a receptor and prevent endogenous (from within the body) agonist compounds (i.e hormones/neurotransmitters) from combining with the receptor and stimulating the cell

84
Q

Competitive Antagonist Drug

A

A CAD that nearly equally competes for the receptor site with the agonist drug (the drug that succeeds in occupying the receptor is usually determine by which drug is present in greater amounts)

85
Q

Surmountable/Reversible Antagonism

A

This is a form of competitive antagonism where the effect of the antagonist can be reversed by giving more of the agonist

86
Q

Noncompetitive Antagonist

A

A drug combines with a receptor very tightly,preventing other molecules from accessing the receptor site OR the noncompetitive antagonist drug modifies receptor so the agonist drug can no longer dock with the receptor

87
Q

Irreversible/Insurmountable Antagonism

A

Because NcAs have some advantage over the competing drugs, simply adding more of the competing drugs will not reverse the effect of the NcA. Usually the antagonism caused by the NcA drug is not truly irreversible, but it occurs very slowly.

88
Q

Partial Agonist

A

Causes effects with a lower potency than that of the natural ligand

89
Q

Ligand

A

Substance or drug that binds or inserts into the receptor

90
Q

Receptor Antagonist

A

A drug ligand blocks the normal action of the receptor (using a key that fits but doesn’t open the door)

91
Q

Receptor Agonist

A

Mimics an endogenous substance that normally interacts with the receptor

92
Q

Endogenous agonist

A

Natural bodily molecule that binds to and activates its receptor

93
Q

Full Agonist

A

Binds and activates the receptor with a potency equal to that of the natural ligand

94
Q

Superagonist

A

Binds to the receptor but produces a more potent action than that of the endogenous ligand

95
Q

Inverse Agonist

A

Both inhibits the function of the natural ligand and causes an effect opposite to that produces by the natural ligand

96
Q

Non receptor-Mediated Drug Reaction

A

Drug molecule does not attach to any cellular receptor to produce the desired effect

97
Q

Chelators

A

Type of chemical that combines with ions or other specific compounds and produces a biological effect by non receptor- mediated reactions

98
Q

Biotransformation/Drug Metabolism

A

Drug structures being chemically altered by enzymes as they pass through the liver

99
Q

Metabolite

A

Altered drug molecule from biotransformation

100
Q

Hepatocytes

A

Liver cells, where most drug metabolism occurs

101
Q

Cytochrome P-450 (CYP)

A

Family of enzymes involved in enzymatic breakdown of drug molecules in the GI tract and Liver

102
Q

Mixed Function Oxidase Enzymes

A

Hepatic biotransformation enzymes

103
Q

Prodrugs

A

Drugs that are biotransformed into a more active form

104
Q

Conjugation (come together)

A

Metabolite is chemically combined to another molecule such as glucuronic acid, sulfate or gylcine

105
Q

Inducible Enzymes

A

When the Livers CYP enzymes are repeatedly exposed to and metabolize certain drug molecules, the cell is stimulated to produce additional CYP enzymes to increase the rate the drug molecules are metabolized

106
Q

Induced

A

When the metabolism of a drug is sped up by the inducible enzyme process it is said to be induced

107
Q

Metabolic Induction

A

When drug molecules have induced metabolism, they are inactivated at a faster rate than usual. So to produce the same degree of drug effect on the body the drug dose must increased

108
Q

Tolerance

A

Diminution of response to a stimulus after prolonged exposure (Ex someone ‘addicted’ to coffee)

109
Q

Elimination/Excretion

A

The movement of drug molecules out of the body, most typically into the feces or urine

110
Q

Renal Excretion/Elimination

A

Excretion by the kidney through the urine

111
Q

Hepatic/Biliary Excretion/Elimination

A

Excretion of drugs by the liver, through the livers bile duct and subsequently through the feces

112
Q

Renal Elimination Process

A

Circulating drugs eliminated through the kidney via filtration, active secretion, and reabsorption in different parts of the nephron

113
Q

Filtration

A

Passive diffusion that occurs as the blood flows from the afferent renal arteriole into the glomerulus

114
Q

Glomerulus

A

Specialized tuft of capillaries in the kidney

115
Q

Afferent Renal Arteriole

A

Incoming renal arteriole that carries blood to the glomerulus

116
Q

Efferent Renal Arteriole

A

Outgoing renal arteriole that carries blood away from the glomerulus (slightly smaller than afferent arteriole)

117
Q

Bowman’s Capsule

A

First part of the nephron - Cup-shaped end of a renal tubule or nephron enclosing a glomerulus (with the glomerulus, it is the site of filtration in the kidney)

118
Q

Proximal Convoluted Tubule

A

Segment of the nephron, twisted tubular segment that contains many active transport mechanisms for moving electrolytes, glucose, selected drug + other essential molecules back and forth between the urine and the renal tubular cell, and the renal tubular cell and the peritubular capillaries

119
Q

Peritubular capillaries

A

A continuation of the efferent renal arteriole by which blood exits the glomerulus, they surround the renal tubule

120
Q

Active Secretion

A

In the proximal convoluted tubule some drug molecules are actively transported from the peritubular capillaries into the urine (energy-requiring transport carrier mechanism - not reliant on concentration gradient*)

121
Q

Loop of Henle

A

Filtrate flows from the proximal convoluted tubule, along the nephron into the LOH where some of the drug molecules may reabsorb back into the body

122
Q

Reabsorption

A

A drug previously ‘eliminated’ into the urine by glomerular filtration or active secretion is now being reabsorbed back into the body via passive diffusion

123
Q

Sinusoids

A

A specialized liver blood cavity that drugs from the GI system enter the liver through

124
Q

Enterohepatic Circulation

A

Movement of drug from liver excreted into intestinal tract, reabsorbed back into systemic circulation, and eliminated again by the liver

125
Q

Cirrhosis

A

Replacement of functional liver cells by nonfunctional fibrous tissue

126
Q

Clearance

A

The rate at which drugs leave the body

127
Q

Half-Life of Elimination

A

A time value that describes how long it takes for the drug concentration, usually measured in the blood or plasma, to decrease by 50%

128
Q

Withdrawal Times

A

Amount of time that must pass from the last drug administration until the animal can be sent to market for slaughter or the eggs/milk can be safely used for human consumption (usually expressed in days)

Pharmacology (13 decks)

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