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Pharmacology 1 > Pharmacodynamics / Pharmacokinetics (1) > Flashcards

Pharmacodynamics / Pharmacokinetics (1) Flashcards

1
Q

Hyperreactive definition

A

low dose produces a pharmacologic effect

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2
Q

Hypersensitive definition

A

Allergic type reactions

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3
Q

Hyporeactive definition

A

Need a larger dose to get pharmacologic effect

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4
Q

idiosyncracy definition

A

rare / unpredictable reaction from a drug administration, unrelated to dose or normal mechanism
- e.g. child takes Benadryl = excitation response (from underdeveloped neurological system)

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5
Q

Proteins have 4 major levels of structure: Primary:

A

determined by the sequence of amino acids

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6
Q

Proteins have 4 major levels of structure: Secondary:

A

Determined by interaction of negative and positively charged atoms (alpha helix, beta pleated sheet)

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7
Q

Proteins have 4 major levels of structure: Tertiary

A

Determined by ionic and covalent bods, gives 3D structure

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8
Q

Proteins have 4 major levels of structure: Quaternary:

A

Determined by binding of two or more independent proteins

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9
Q

Binding site on receptor is affected by (in order strongest to weakest)

A

(Stronger) Covalent > Ionic > hydrogen > VanderWaals forces (weaker)

binding is rarely caused by just one interaction

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10
Q

Covalent

A

Shares electrons - often not reversible

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11
Q

Phosphorylation

A

Turns protein on or off - Very important in many receptor systems

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12
Q

Pharmacodynamics

A

What the Drug Does to the body - study of the intrinsic sensitivity or responsiveness of receptors to a drug and the mechanisms by which these effects occur

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13
Q

Pharmacokinetics

A

What the body does to a drug (ADME)

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14
Q

ADME

A

Absorption, distribution, metabolism, excretion

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15
Q

Pharmacodynamics important factors:

A

hydrophilic / hydrophobic
Ionization state (pKa)
Conformation and stereochemistry

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16
Q

Ion channel binding, spanning the plasma membrane have what gates?

A

Ligand gated (hypnosis, benzos, muscle relaxants, ketamine)

Voltage gated (local anesthetics)

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17
Q

Heptahelical receptors:

A

Spain the plasma membrane coupled to intracellular G proteins (2nd messenger, GPCRs) - most common in humans

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18
Q

Binding to extracellular side of transmembrane receptor acts on intracellular enzyme (receptor linked enzymes) eg =

A

GH, Insulin, PDE

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19
Q

These drugs diffuse through the plasma membrane

A

lipophilic drugs

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20
Q

Extracellular enzymes:

A

target is outside the plasma membrane

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21
Q

Nicotinic Acetylcholine receptor is comprised of these 5 subunits

A

2 x Alpha (when both alpha subunits are bound the channel opens)
Beta
Gamma
Delta

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22
Q

What is bound to the alpha subunit when it is attached to the GPCR?

A

GDP (think docked)

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23
Q

When a signaling molecule joins with the GPCR, a conformational change occurs and _______ replaces _______ on the alpha subunit. As a result the subunits (alpha, beta, gamma) dissociate into two parts.

A

GTP replaces GDP (GTP think Transformational change, transfer, or transport)

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24
Q

2nd messengers include:

A

Calcium, cAMP, cGMP, inositol

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25
Q

GPCR alpha subunits possess intrinsic:

A

GTPase activity (hydrolyzes GTP to GDP) causing re-association of the alpha subunit with the Beta Gamma complex

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26
Q

***What is - Potentiation?

A

Medication is enhanced by another that has no activity

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27
Q

***Potentiation examples:

A

Epinephrine with Local Anesthetic (LA): vasoconstrictor keeps LA there longer but doesn’t itself give you anesthesia

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28
Q

Agonist

A

Binds to and changes function of the receptor

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29
Q

Antagonist

A

Binds to receptor without changing function - prevents agonist from binding/stimulating

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30
Q

(Antagonist) Competitive:

A

increasing concentrations of antagonist progressively inhibit the response of an agonist - high doses prevent response completely

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31
Q

(Antagonist) Non-Competitive

A

agonist cannot act on the receptor even in high doses

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32
Q

Inverse Agonist

A

a ligand binds to a receptor activating an inverse response (“turn off” receptor activity)

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33
Q

Partial agonist

A

a ligand binds to a receptor resulting in a partial activating and partial inactivating response - never have full effect of an agonist

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34
Q

Partial agonist - if they have antagonist activity they are referred to as:

A

agonist- antagonists
eg. butorphanol

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35
Q

Affinity

A

degree of attraction

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36
Q

Efficacy

A

ability to produce the desired effect under ideal conditions

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37
Q

ED50

A

effective dose in 50% of the population

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38
Q

ED95

A

effective dose in 95% of the population

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39
Q

LD50

A

Lethal dose in 50% of the population

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40
Q

LD95

A

Lethal dose in 95% of the population

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41
Q

Therapeutic index:

A

Margin of safety between therapeutic and toxic/lethal

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42
Q

The larger the Therapeutic index:

A

generally the safer the drug (further distance between effective dose and lethal dose)

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43
Q

Generally a drug has a good safety profile if its Therapeutic index is greater than:

A

10

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44
Q

Sensitivity

A

can up-regulate or down-regulate in number in response to specific stimuli

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45
Q

Selectivity

A

the affinity of a drug for a specific receptor

46
Q

Specificity

A

Stimulation of the receptor by an agonist ALWAYS yields the same specific response

47
Q

Stereochemistry

A

chirality/Enantiomers (the pair): based on a center with three dimensional asymmetry, mirror images that cannot be superposed on each other
- chemically identical pair of molecules existing in two mirror image forms of each other
- dissolved in solution, described by rotation in polarized light (optical isomerism)
- right and left handed but cannot be superimposed
- Dextro (+) right
- Levo (-) left (in general, left rotated molecules have lower potency)
- Racemic - equal parts right and left

48
Q

Racemic

A

equal parts right and left

49
Q

(Stereochemistry) Dextro

A

Right

50
Q

(Stereochemistry) Levo

A

Left

51
Q

(Stereochemistry) Sinsiter

A

Left (depending on geometry of the molecule)

52
Q

(Stereochemistry) Rectus

A

Right (depending on geometry of the molecule)

53
Q

(Stereochemistry) Cis, trans

A

same chemical formula but vary based on where the side groups (functional groups) are located) (cis- same side, trans opposite sides)

54
Q

(Stereochemistry) Racemic examples:

A

STP methohexital, ketamine, epi

55
Q

(Stereochemistry) Levo examples:

A

1-morphone, 1-bupivacaine

56
Q

(Stereochemistry) dextro example:

A

dexmedetomidine

57
Q

(Stereochemistry) Sinsister isomeer example:

A

Ropivacaine

58
Q

Physiochemical properties that affect absorption:

A
  • Structure and size of molecule
  • Temperature
  • Solubility
  • Protein binding
  • Ionization affects solubility = most drugs are weak acids or bases
59
Q

Acids and neutrals bind to

A

Albumin

60
Q

Bases bind to

A

Alpha 1 glycoprotein

61
Q

pKa =

A

pH at which 50% of drug is ionized and 50% is unionized

62
Q

(Absorption) PO:

A

First-pass effect - hepatic- extensive metabolism - large difference between PO and IV doses

63
Q

(Absorption) IM, SQ:

A

dependent on local blood flow

64
Q

(Absorption) Sublingual/Buccal:

A

Bypass liver, no first pass.
(***rapid onset)

65
Q

(Absorption) IV:

A

***PREDICTABLE plasma concentrations (often defined as having 100% bioavailability)

66
Q

(Absorption) IV: First-pass pulmonary effect effects what drugs?

A

***Lidocaine, Propanolol, Fentanyl

67
Q

What is the First-pass pulmonary effect?

A

***as much as 75% of a dose of fentanyl is absorbed by pneumocytes (will release later) lungs subsequently serve as reservoir to release drug back into systemic circulation.

68
Q

Transdermal medication requirements:

A
  • Low molecular weight (<500 Da)
  • Affinity for both lipophilic and hydrophilic phases (lipophilic to cross membranes, hydrophilic to get into blood)
  • Low melting point (affects the release of drug) so it melts with heat of skin
  • non-ionized
  • High potency
69
Q

***What is the rate limiting step for transdermal medications

A

*** SKIN

70
Q

IV medication phases

A
  • rapid distribution (central compartment)
  • slow distribution (peripheral compartment)
  • terminal phase (elimination phase)
71
Q

Central compartment

A

Kidneys, Liver, Lungs, Heart, Brain (receives 75% of CO, only represents 10% of the body’s mass)

72
Q

Peripheral compartment

A

large calculated volume, extensive uptake of drug - fat, cartilage, muscle

73
Q

Volume of distribution equation

A

Vd = dose/CP
Vd = volume of distribution
CP = plasma concentration

74
Q

Vessel-rich group
Body mass
CO
Perfusion (mL/100g/min)

A

Body mass - 10%
CO - 75%
Perfusion (mL/100g/min) - 75

75
Q

Muscle group
Body mass
CO
Perfusion (mL/100g/min)

A

Body mass - 50%
CO - 19%
Perfusion (mL/100g/min) - 3

76
Q

Fat group
Body mass
CO
Perfusion (mL/100g/min)

A

Body mass - 20%
CO - 6%
Perfusion (mL/100g/min) - 3

77
Q

Vessel-poor group
Body mass
CO
Perfusion (mL/100g/min)

A

Body mass - 20%
CO - 1%
Perfusion (mL/100g/min) - 0

78
Q

Steady state is achieved after how many half-lives have occurred

A

4 to 5 half-lives

79
Q

Steady state is achieved when:

A

drug input = drug output (this means the drug is in all compartments, and the plasma has a steady amount

80
Q

Factors affecting steady state:

A
  • Bioavailability
  • clearance
  • dose
  • dosing interval or frequency of administration
81
Q

Bioavailability definition

A

Amount or concentration (Cp) of a drug that actually reaches the site of action (receptor) or a fluid or tissue reservoir with access to the receptor, regardless of route of administration

82
Q

For IV meds bioavailability =

A

1 (since it is injected directly into the bloodstream

83
Q

Drugs can be changed in these 4 ways

A
  • active to inactive
  • active to active or reactive (toxic metabolite)
  • inactive prodrug to active drug
  • unexcretable to excretable
84
Q

Phase 1 reactions (CYP450)

A

Hydrolysis (usually drugs w/ester bond)
Oxidation (electron loss)
Reduction (electron gain)

85
Q

Phase 2 reactions (conjugation reactions)

A

coupling of drug with endogenous substrate such as glucuronate, acetate, or amino acid so drug can be ionized and thus excreted)

86
Q

Example of Phase 2 enzymes:

A

Glutathione-S-transferase and
N-acetyl-transferase

87
Q

All conjugation reactions except for conjugation of glucuronic acid are catalyzed by:

A

Non-CYP450 enzymes
eg. esterases in liver, plasma, GI tract

88
Q

Glucuronidation metabolizes what drugs:

A

Propofol, opioids, midazolam

89
Q

What is Glucuronidation

A

A metabolic pathway that uses glucose to conjugate and metabolize compounds into glucuronides

90
Q

Glucuronidation is catalyzed by:

A

UDP-glucuronosyltransferases (UGTs)

91
Q

UDP-glucuronosyltransferases (UGTs) are found where?

A

found in many cells, tissues, and organs, but are especially concentrated in the liver, kidneys, and intestines

92
Q

Conjugation of glucuronic acid (glucuronidation) DOES involve:

A

CYP450 enzymes

93
Q

CYP2C8:

A

allows potential drug binding to glucuronides, which then allows the drug to become ionized and excreted

94
Q

CYP450 are found:

A

in most body tissues, concentrated in liver, intestines, and kidneys

95
Q

Majority if anesthesia related CYP activity is generated by:

A

CYP3A4, CYP2E1 and CYP2D6

96
Q

CYP3A4

A

metabolizes majority of all drugs

97
Q

CYP2D6 and CYP2E1

A

second most important to anesthesia

98
Q

CYP2D6

A

responsible for Phase 1 reaction in 25% of drugs - analgesics, antidysrhythmics, amide LAs, ketamine, propofol, antiemetics, beta-blockers

99
Q

CYP2E1

A

Metabolizes inhaled anesthetics

100
Q

Hepatic extraction ratio of 0

A

no drug elimination during single pass through the liver

101
Q

Hepatic extraction ration of 1

A

all drug is eliminated during a single pass thought the liver

102
Q

Drugs with a HIGH hepatic extraction ratio =

A

more sensitive to a reduction in hepatic blood flow

103
Q

Drugs with a LOW hepatic extraction ratio =

A

more sensitive to a decline in hepatocellular function (i.e. enzymatic activity)

104
Q

Drugs with HIGH Hepatic extraction ratio examples:

A

Propanolol, morphine, ketamine, propofol

105
Q

Drugs with LOW hepatic extraction ratio examples:

A

Benzos, methadone, naproxen, alfentanyl, warfarin, rocuronium

106
Q

Half life is estimated by knowing you need ___ to ___ half times to mostly eliminate the medication

A

4 to 5 halftimes to mostly eliminate the medication

107
Q

First order Metabolism:

A

Constant fraction, certain % is metabolized (most drugs) (curved line)

108
Q

Zero Order Metabolism:

A

Contant amount (strait line)
example: alcohol

109
Q

First order metabolism can be turned into zero order how?

A

by overwhelming the receptors

110
Q

(increase) Lipid Solubility
(increase) Ionization
(increase) Protein Binding

A

**(increase) Lipid Solubility -
(increase) Potency
**(increase) Ionization -
(decrease) Onset
***(increase) Protein Binding - (increase) Duration

Pharmacology 1 (12 decks)

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