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PHARM 2-EXAM 1 (kinetics/dynamics/renal) > Dynamics > Flashcards

Dynamics Flashcards

1
Q

Pharmacodynamics is the study of

A

what a drug does to the body

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2
Q

What is pharmacokinetics?

A

The study of what the body does to a drug

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3
Q

Pharmacokinetics is the relationship between

A

Dose & plasma concentrations

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4
Q

Pharmacodynamics is the relationship between

A

Effect site concentration & clinical effects

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5
Q

What is the movement of ions in the Na+/K+ pump?

A

3 Na+ out

2 K+ in

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6
Q

The endoplasmic reticulum makes ______, lipids, & metabolizes_________. The sarcoplasmic reticulum in the muscle stores & releases what important 2nd messenger?

A

Protein

Carbs

Calcium

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7
Q

The resting membrane potential is slightly polarized at

A

-70mV

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8
Q

ICF is relatively______ compared to ECF

A

Negative

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9
Q

Neuronal action potential threshold is

A

-55mV & is when Na+ channels open

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10
Q

What is it called when Na+ channels open?

A

Depolarization

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11
Q

When do Na+ channels close?

A

When membrane potential is at +30mV (inactivation)

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12
Q

When do K+ channels open?

A

At +30mV ( a delay)

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13
Q

What is it called when K+ channels open?

A

Repolarization

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14
Q

When K+ channels start to close, this is called…

A

Hyper-repolarization

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15
Q

What abnormality occurs when hypocalcemia is present?

A

Na+ channels are prevented from closing, causing a sustained depolarization (repetitive fire; tetany)

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16
Q

What abnormality occurs when hypercalcemia is present?

A

There is a decrease in cell membrane permeability to Na+, causing a decrease in membrane excitability

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17
Q

What abnormality occurs when hypokalemia is present?

A

There is a more negative resting membrane potential, causing hyperpolarization. This decreases membrane excitability

(skeletal muscle weakness)

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18
Q

Sodium can cause what action potential abnormality?

A

Sodium channel blockade & prevents threshold potential for action potential generation

There will be a decrease in contractility & altered cardiac conduction

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19
Q

The pre-synaptic membrane receives what type of action potential?

A

Afferent

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20
Q

The post-synaptic membrane receives what type of action potential?

A

Efferent

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21
Q

What is modulation?

A

A change in synaptic function, which influence depolarization & response

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22
Q

What causes synaptic fatigue?

A

Repetative stimulation of excitatory synapses

Reduced post-synaptic response

Depletion of NT stores

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23
Q

Explain Post-Tetanic Facilitation?

A

Repetitive stimulation of Pre-synaptic terminal

Short rest period

Synapse is more responsive than normal to subsequent stimulation

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24
Q

Alkalosis will cause this synaptic response

A

Increased excitability (H+ will want to leave the cell, causing K+ to shift inward)

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25
Q

Acidosis will cause this synaptic response

A

Decrease excitability (H+ into the cell & K+ leaves)

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26
Q

Hypoxia will cause this

A

Decreased excitability

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27
Q

Receptor Sensitivity

A

Concentration required for cellular response

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28
Q

Receptor Selectivity

A

Structurally compatible & similar chemically

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29
Q

Receptor Specificity

A

Cellularly-determined response

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30
Q

Receptors have this type of bonding

A

Hydrophobic

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31
Q

Receptors acceptors include

A

Albumin, Alpha1-acid GP, & beta-globulin, which will reduce the amount of free drug available & they act as an alternative binding site

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32
Q

Which dipole-dipole interaction requires considerable energy to break & helps hold globular proteins together?

A

Hydrogen bonds (most common)

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33
Q

Which dipole interaction is the weakest type of intermolecular force?

A

Van der Waals (London) forces

most common

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34
Q

Nonpolar tails are

A

Hydrophobic, which is important for lipid soluble drugs

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35
Q

Which molecular bond is the strongest?

A

Covalent Bonds

least common & irreversible

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36
Q

Chirality is

A

Asymmetric 3-D molecules

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37
Q

Enantiomers are

A

Mirror images molecules which cannot be superimposed

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38
Q

2 enantiomers that are equal in proportion are

A

50/50

Racemic mixture

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39
Q

Receptor states can be

A

Active, Inactive or Open

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40
Q

Signal replay involves a

A

chemical messenger that causes cellular/tissue response

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41
Q

Signal amplification will

A

Increase the cellular response to ligand binding

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42
Q

Signal integration is when

A

A signal merges with another biochemical pathway

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43
Q

What are the 3 common receptor sites

A

G-protein coupled

Ligand-gated

Voltage-gated

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44
Q

G-protein coupled receptors are a series of

A

Intracellular signaling & functions

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45
Q

Ligand-gated ion channels are activated by

A

Binding of chemical messenger, causing ions to move across the membranes

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46
Q

Voltage-gated ion channels are activated by

A

changes in electrical membrane potential, causing ion movement

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47
Q

G protein coupled receptors involve the formation of

A

GDP–> GTP, involving a 2nd messenger activation & interaction with other intracellular proteins

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48
Q

G protein coupled receptors involve these 2 types of responses

A

Activation/stimulation

Inhibition/depression

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49
Q

Na+, Ca+ & Cl- like to flow

A

Into the cell

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50
Q

K+ likes to flow

A

Out of the cell

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51
Q

Na+ and Ca+ channels are ________

A

Depolarizing/Excitatory

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52
Q

Cl- and K+ channels are

A

Hyperpolarizing/ Inhibitory

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53
Q

Activation of ion channels involve activation, membrane________, ligand binding______ & ___________

A

Depolarization

GPRO activation

Conformational change

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54
Q

Which ligand-gated ion channels are excitatory?

A

ACH & nicotinic ACH receptors (nAChRs)

Glutamate, NMDA, AMPA, kainate receptors

Serotonin/5-HT receptors

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55
Q

Which ligand-gated ion channels are inhibitory?

A

Gamma-aminobutyric acid & GABA receptors

Glycine & glycine receptors

56
Q

Voltage gated ion channels are located in the

A

Neurons, skeletal muscles & endocrine cells

57
Q

What is receptor UP regulation?

A

Increase in the number of receptors & sensitivity to agonists

Response to too little agonist

58
Q

What is the goal of UP regulation?

A

Increase cellular response

59
Q

Receptor DOWN regulation is…

A

The decrease in the number & sensitivity of receptors

Response to excess catecholamines

60
Q

What is the goal of DOWN regulation?

A

To decrease cellular response

61
Q

Receptors are created & expressed

A

When DNA gives the cell instructions

62
Q

When are receptors increased or decreased

A

Receptors are increased when signals are weak

Receptors are decreased when signals are strong

63
Q

What happens when there is chronic exposure to a receptor?

A

Can cause down regulation & desensitization of the existing receptors

64
Q

What is the graded dose response?

A

A change in response with increased dosage

Determination of dose which achieves maximal response

65
Q

What is the quantal dose response?

A

Frequency with which a given drug dose produces a desired therapeutic response in a population

66
Q

Quantal dose response is

A

All or nothing response

67
Q

What is potency?

A

Concentration or amount of drug to cause a specific clinical response

68
Q

What is efficacy?

A

The ability of a drug to cause a maximum response or clinical effect

69
Q

What is C50?

A

The concentration associated with 50% peak drug effect

70
Q

What is ED50?

A

The effective dose to produce a desired response in 50% of the population

71
Q

What is LD50?

A

The lethal dose to produce death in 50% of the population

72
Q

What is the therapeutic index equation?

A

LD50/ED50

73
Q

What are the 4 receptor types

A

Agonist
Antagonist
Partial Agonist
Inverse Agonist

74
Q

Antagonist have

A

NO activation (blocking action of NT)

75
Q

Agonists have ______bonding & receptors have______

A

Reversible; Activation

76
Q

Agonists effect is related to

A

The total number of receptors it occupies

77
Q

Agonists have a maximal response from receptors, having ____

A

Full efficacy

78
Q

What happens when there is a continuous administration of an agonists?

A

May cause DOWN-regulation of target receptors

79
Q

Partial agonists are also known as

A

Agonist-antagonists

Mixed agonists-antagonist

80
Q

What type of activation do partial agonists have?

A

Limited receptor activation, leading to reduced efficacy & have a ceiling effect

81
Q

Partial agonist may

A

Block the effects of a full agonist by competing for binding sites

82
Q

Antagonist block

A

Agonist binding

83
Q

Antagonist can be _____ or _____

A

Competitive or Non-competitive

84
Q

What is a competitive antagonist?

A

An increased level of agonist will reverse the antagonism

85
Q

What is a non-competitive antagonist?

A

Irreversible and increased levels if the agonist will NOT overcome antagonism (strong bond)

86
Q

Antagonists have _____ receptor activation

A

NO receptor activation

87
Q

Antagonists have ______ response & ______efficacy

A

NO clinical response

No efficacy

88
Q

What happens when there is a continuous administration of antagonists?

A

May cause UP regulation of target receptors

89
Q

Receptors must have

A

Constitutive or an intrinsic (basal) level of activity without any ligand bound to it

90
Q

Inverse agonists turn off what?

A

Basal activity of receptors

91
Q

Inverse agonist bind same receptors as

A

Agonists, but may be blocked by antagonists

92
Q

inverse agonists have the ________ effect of_______

A

Opposite effect of agonist, having a negative efficacy

93
Q

What is an allosteric modulator?

A

Binding to a specific allosteric site on the receptor; binding to a site other than the activating site

DO NOT bind to the normal agonist site

Modify the effect of the agonist

94
Q

What is an additive effect?

A

A clinical response that results from the sum effect of 2 different drugs

95
Q

What is a synergistic effect?

A

A clinical response that is greater than the sum effect of 2 different drugs given together

96
Q

What is potentiation?

A

the effect of one drug is enhanced by a different drug (usually working on different receptors or sites)

97
Q

What is an antagonistic effect?

A

The effect of one drug that prevents or blocks the clinical response of a difference drug

98
Q

Polymorphism involves a variation in

A

Absorption

Distribution

Metabolism

Excretion

99
Q

The older adult population may have changes in

A

Renal/Liver impairment

Decreased muscle mass, albumin, blood flow & TBW

Increased adipose tissue

Polypharmacy

100
Q

Pediatrics/Neonates have a change in

A

Increased TBW, body fat, glomerular filtration, renal clearance, & hepatic enzyme capacity

Decreased albumin, binding capacity, & alteration in pharmacodynamics

101
Q

The obstetric population has changes in

A

Increased adipose, TBW, blood volume, & CO (35-50%)

Decrease in plasma protein

Delayed gastric emptying & GI motility

Altered hepatic enzyme activity

102
Q

Sex dependent changes include

A

Hormones

Muscle mass

Body composition

Organ blood flow & function

Enzymatic differences

103
Q

Homeostasis is altered in which population?

A

Older Adult/Geriatric

104
Q

Which population has a reduced risk of PONV?

A

Older Adult/Geriatric

105
Q

What does it mean when there is a decrease in albumin?

A

A decrease in albumin means there is more FREE drug floating around in the body

106
Q

What are some renal impairments older adults often face?

A

Decreased renal mass & GFR

Metabolism & Elimination are altered, risking the potential for drug accumulation

107
Q

What are some neuro changes the older adult/geriatric population can face?

A

BBB changes

Increased CNS sensitivity & risk for post-op cognitive decline & delirium

Risk for neuroinflammatory response with surgical trauma

NT-receptor alterations

108
Q

What are some respiratory changes the Pediatric/Neonatal population face?

A

Increased oxygen demand

They have double the adult alveolar minute ventilation

109
Q

In the Pediatric/Neonatal population, the cardiac output is dependent on

A

The HR

110
Q

What can be detrimental in the Pediatric/Neonatal population?

A

Drug induced myocardial depression & bradycardia

111
Q

Which age group has less compliant myocardium & maturing contractile elements?

A

Pediatric/Neonatal

112
Q

What are the characteristics of the neonates nerve conduction?

A

They have incomplete myelination & diminished nerve conduction (speed)

113
Q

What are the characteristics of a neonates pain input?

A

rapid transmission of nociceptive input (short distances)

114
Q

What is often used for pain management in the neonate?

A

Sucrose & suckling as analgesia

115
Q

When you have increased adipose tissue and give a highly lipophilic drug, what happens to the Vd?

A

It increases

116
Q

What population has an increase in blood volume?

A

Obstetric

117
Q

A decrease in plasma protein will cause what change in Vd?

A

An increase

118
Q

What receptor down regulates in the older adult?

A

Catecholamine receptor down regulation with increased age

119
Q

Older adults have what cardiac changes?

A

Arrhythmias

Decreased cardiac function, affecting distribution & response to cardiac drugs

120
Q

What blood vessel change occurs in the older adult?

A

Endothelial dysfunction, which reduces the response to vasoactive drugs, requiring a higher dose

121
Q

Volatile anesthetics in the older adult can cause…

A

Myocardial depression

122
Q

The older adults have this chest wall change & a decline in…

A

Increased stiffness in chest wall

Decline in gas exchange efficiency

123
Q

How is the older adults airway reflex change?

A

They have diminished sensitivity to protect their airway

124
Q

The older adults are more sensitive to drug induced…

A

Respiratory depression

125
Q

The pediatric/neonates have free drug floating around due to…

A

Decreased albumin & binding capacity

126
Q

What gradually increases int he pediatric/neonate population?

A

GFR

Renal Clearance

Hepatic Enzyme Capacity

127
Q

The pediatric/neonatal population have a possible alteration in…

A

Pharmacodynamics (receptor binding & homeostatic function)

128
Q

In the pediatric/neonatal population, thermoregulation affects

A

Distribution & Elimination

129
Q

In the pediatric/neonatal population, they tend to have a larger _______ _______, which limits ________

A

Surface Area

Thermogenesis

130
Q

This can happen to the pediatric/neonate population under general anesthesia

A

Accelerated heat loss

131
Q

Thermoregulation int he pediatric/neonatal population may delay…

A

Anesthesia emergence & affect metabolism of some drugs

132
Q

Which population has a delayed gastric emptying & GI motility?

A

Obstetric

133
Q

What may be altered in the Obstetric population?

A

Hepatic enzyme activity

Nerve sensitivity

134
Q

What is increased in the Obstetric population?

A

Increased RBF, GFR (adjust dose)

Increased sensitivity to general anesthetics (greater risk for awareness)

Increased sensitivity to local anesthetics

135
Q

What can affect distribution in the Obstetric population?

A

Distended epidural veins & decreased CSF volume

136
Q

What can possibly harm the fetus?

A

Systemic opioids

PHARM 2-EXAM 1 (kinetics/dynamics/renal) (4 decks)

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