Dynamics Flashcards
1
Q
Pharmacodynamics is the study of
A
what a drug does to the body
2
Q
What is pharmacokinetics?
A
The study of what the body does to a drug
3
Q
Pharmacokinetics is the relationship between
A
Dose & plasma concentrations
4
Q
Pharmacodynamics is the relationship between
A
Effect site concentration & clinical effects
5
Q
What is the movement of ions in the Na+/K+ pump?
A
3 Na+ out
2 K+ in
6
Q
The endoplasmic reticulum makes ______, lipids, & metabolizes_________. The sarcoplasmic reticulum in the muscle stores & releases what important 2nd messenger?
A
Protein
Carbs
Calcium
7
Q
The resting membrane potential is slightly polarized at
A
-70mV
8
Q
ICF is relatively______ compared to ECF
A
Negative
9
Q
Neuronal action potential threshold is
A
-55mV & is when Na+ channels open
10
Q
What is it called when Na+ channels open?
A
Depolarization
11
Q
When do Na+ channels close?
A
When membrane potential is at +30mV (inactivation)
12
Q
When do K+ channels open?
A
At +30mV ( a delay)
13
Q
What is it called when K+ channels open?
A
Repolarization
14
Q
When K+ channels start to close, this is called…
A
Hyper-repolarization
15
Q
What abnormality occurs when hypocalcemia is present?
A
Na+ channels are prevented from closing, causing a sustained depolarization (repetitive fire; tetany)
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
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)
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
19
Q
The pre-synaptic membrane receives what type of action potential?
A
Afferent
20
Q
The post-synaptic membrane receives what type of action potential?
A
Efferent
21
Q
What is modulation?
A
A change in synaptic function, which influence depolarization & response
22
Q
What causes synaptic fatigue?
A
Repetative stimulation of excitatory synapses
Reduced post-synaptic response
Depletion of NT stores
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
24
Q
Alkalosis will cause this synaptic response
A
Increased excitability (H+ will want to leave the cell, causing K+ to shift inward)
25
Acidosis will cause this synaptic response
Decrease excitability (H+ into the cell & K+ leaves)
26
Hypoxia will cause this
Decreased excitability
27
Receptor Sensitivity
Concentration required for cellular response
28
Receptor Selectivity
Structurally compatible & similar chemically
29
Receptor Specificity
Cellularly-determined response
30
Receptors have this type of bonding
Hydrophobic
31
Receptors acceptors include
Albumin, Alpha1-acid GP, & beta-globulin, which will reduce the amount of free drug available & they act as an alternative binding site
32
Which dipole-dipole interaction requires considerable energy to break & helps hold globular proteins together?
Hydrogen bonds (most common)
33
Which dipole interaction is the weakest type of intermolecular force?
Van der Waals (London) forces
most common
34
Nonpolar tails are
Hydrophobic, which is important for lipid soluble drugs
35
Which molecular bond is the strongest?
Covalent Bonds
least common & irreversible
36
Chirality is
Asymmetric 3-D molecules
37
Enantiomers are
Mirror images molecules which cannot be superimposed
38
2 enantiomers that are equal in proportion are
50/50
Racemic mixture
39
Receptor states can be
Active, Inactive or Open
40
Signal replay involves a
chemical messenger that causes cellular/tissue response
41
Signal amplification will
Increase the cellular response to ligand binding
42
Signal integration is when
A signal merges with another biochemical pathway
43
What are the 3 common receptor sites
G-protein coupled
Ligand-gated
Voltage-gated
44
G-protein coupled receptors are a series of
Intracellular signaling & functions
45
Ligand-gated ion channels are activated by
Binding of chemical messenger, causing ions to move across the membranes
46
Voltage-gated ion channels are activated by
changes in electrical membrane potential, causing ion movement
47
G protein coupled receptors involve the formation of
GDP--> GTP, involving a 2nd messenger activation & interaction with other intracellular proteins
48
G protein coupled receptors involve these 2 types of responses
Activation/stimulation
Inhibition/depression
49
Na+, Ca+ & Cl- like to flow
Into the cell
50
K+ likes to flow
Out of the cell
51
Na+ and Ca+ channels are ________
Depolarizing/Excitatory
52
Cl- and K+ channels are
Hyperpolarizing/ Inhibitory
53
Activation of ion channels involve activation, membrane________, ligand binding______ & ___________
Depolarization
GPRO activation
Conformational change
54
Which ligand-gated ion channels are excitatory?
ACH & nicotinic ACH receptors (nAChRs)
Glutamate, NMDA, AMPA, kainate receptors
Serotonin/5-HT receptors
55
Which ligand-gated ion channels are inhibitory?
Gamma-aminobutyric acid & GABA receptors
Glycine & glycine receptors
56
Voltage gated ion channels are located in the
Neurons, skeletal muscles & endocrine cells
57
What is receptor UP regulation?
Increase in the number of receptors & sensitivity to agonists
Response to too little agonist
58
What is the goal of UP regulation?
Increase cellular response
59
Receptor DOWN regulation is...
The decrease in the number & sensitivity of receptors
Response to excess catecholamines
60
What is the goal of DOWN regulation?
To decrease cellular response
61
Receptors are created & expressed
When DNA gives the cell instructions
62
When are receptors increased or decreased
Receptors are increased when signals are weak
Receptors are decreased when signals are strong
63
What happens when there is chronic exposure to a receptor?
Can cause down regulation & desensitization of the existing receptors
64
What is the graded dose response?
A change in response with increased dosage
Determination of dose which achieves maximal response
65
What is the quantal dose response?
Frequency with which a given drug dose produces a desired therapeutic response in a population
66
Quantal dose response is
All or nothing response
67
What is potency?
Concentration or amount of drug to cause a specific clinical response
68
What is efficacy?
The ability of a drug to cause a maximum response or clinical effect
69
What is C50?
The concentration associated with 50% peak drug effect
70
What is ED50?
The effective dose to produce a desired response in 50% of the population
71
What is LD50?
The lethal dose to produce death in 50% of the population
72
What is the therapeutic index equation?
LD50/ED50
73
What are the 4 receptor types
Agonist
Antagonist
Partial Agonist
Inverse Agonist
74
Antagonist have
NO activation (blocking action of NT)
75
Agonists have ______bonding & receptors have______
Reversible; Activation
76
Agonists effect is related to
The total number of receptors it occupies
77
Agonists have a maximal response from receptors, having ____
Full efficacy
78
What happens when there is a continuous administration of an agonists?
May cause DOWN-regulation of target receptors
79
Partial agonists are also known as
Agonist-antagonists
Mixed agonists-antagonist
80
What type of activation do partial agonists have?
Limited receptor activation, leading to reduced efficacy & have a ceiling effect
81
Partial agonist may
Block the effects of a full agonist by competing for binding sites
82
Antagonist block
Agonist binding
83
Antagonist can be _____ or _____
Competitive or Non-competitive
84
What is a competitive antagonist?
An increased level of agonist will reverse the antagonism
85
What is a non-competitive antagonist?
Irreversible and increased levels if the agonist will NOT overcome antagonism (strong bond)
86
Antagonists have _____ receptor activation
NO receptor activation
87
Antagonists have ______ response & ______efficacy
NO clinical response
No efficacy
88
What happens when there is a continuous administration of antagonists?
May cause UP regulation of target receptors
89
Receptors must have
Constitutive or an intrinsic (basal) level of activity without any ligand bound to it
90
Inverse agonists turn off what?
Basal activity of receptors
91
Inverse agonist bind same receptors as
Agonists, but may be blocked by antagonists
92
inverse agonists have the ________ effect of_______
Opposite effect of agonist, having a negative efficacy
93
What is an allosteric modulator?
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
What is an additive effect?
A clinical response that results from the sum effect of 2 different drugs
95
What is a synergistic effect?
A clinical response that is greater than the sum effect of 2 different drugs given together
96
What is potentiation?
the effect of one drug is enhanced by a different drug (usually working on different receptors or sites)
97
What is an antagonistic effect?
The effect of one drug that prevents or blocks the clinical response of a difference drug
98
Polymorphism involves a variation in
Absorption
Distribution
Metabolism
Excretion
99
The older adult population may have changes in
Renal/Liver impairment
Decreased muscle mass, albumin, blood flow & TBW
Increased adipose tissue
Polypharmacy
100
Pediatrics/Neonates have a change in
Increased TBW, body fat, glomerular filtration, renal clearance, & hepatic enzyme capacity
Decreased albumin, binding capacity, & alteration in pharmacodynamics
101
The obstetric population has changes in
Increased adipose, TBW, blood volume, & CO (35-50%)
Decrease in plasma protein
Delayed gastric emptying & GI motility
Altered hepatic enzyme activity
102
Sex dependent changes include
Hormones
Muscle mass
Body composition
Organ blood flow & function
Enzymatic differences
103
Homeostasis is altered in which population?
Older Adult/Geriatric
104
Which population has a reduced risk of PONV?
Older Adult/Geriatric
105
What does it mean when there is a decrease in albumin?
A decrease in albumin means there is more FREE drug floating around in the body
106
What are some renal impairments older adults often face?
Decreased renal mass & GFR
Metabolism & Elimination are altered, risking the potential for drug accumulation
107
What are some neuro changes the older adult/geriatric population can face?
BBB changes
Increased CNS sensitivity & risk for post-op cognitive decline & delirium
Risk for neuroinflammatory response with surgical trauma
NT-receptor alterations
108
What are some respiratory changes the Pediatric/Neonatal population face?
Increased oxygen demand
They have double the adult alveolar minute ventilation
109
In the Pediatric/Neonatal population, the cardiac output is dependent on
The HR
110
What can be detrimental in the Pediatric/Neonatal population?
Drug induced myocardial depression & bradycardia
111
Which age group has less compliant myocardium & maturing contractile elements?
Pediatric/Neonatal
112
What are the characteristics of the neonates nerve conduction?
They have incomplete myelination & diminished nerve conduction (speed)
113
What are the characteristics of a neonates pain input?
rapid transmission of nociceptive input (short distances)
114
What is often used for pain management in the neonate?
Sucrose & suckling as analgesia
115
When you have increased adipose tissue and give a highly lipophilic drug, what happens to the Vd?
It increases
116
What population has an increase in blood volume?
Obstetric
117
A decrease in plasma protein will cause what change in Vd?
An increase
118
What receptor down regulates in the older adult?
Catecholamine receptor down regulation with increased age
119
Older adults have what cardiac changes?
Arrhythmias
Decreased cardiac function, affecting distribution & response to cardiac drugs
120
What blood vessel change occurs in the older adult?
Endothelial dysfunction, which reduces the response to vasoactive drugs, requiring a higher dose
121
Volatile anesthetics in the older adult can cause...
Myocardial depression
122
The older adults have this chest wall change & a decline in...
Increased stiffness in chest wall
Decline in gas exchange efficiency
123
How is the older adults airway reflex change?
They have diminished sensitivity to protect their airway
124
The older adults are more sensitive to drug induced...
Respiratory depression
125
The pediatric/neonates have free drug floating around due to...
Decreased albumin & binding capacity
126
What gradually increases int he pediatric/neonate population?
GFR
Renal Clearance
Hepatic Enzyme Capacity
127
The pediatric/neonatal population have a possible alteration in...
Pharmacodynamics (receptor binding & homeostatic function)
128
In the pediatric/neonatal population, thermoregulation affects
Distribution & Elimination
129
In the pediatric/neonatal population, they tend to have a larger _______ _______, which limits ________
Surface Area
Thermogenesis
130
This can happen to the pediatric/neonate population under general anesthesia
Accelerated heat loss
131
Thermoregulation int he pediatric/neonatal population may delay...
Anesthesia emergence & affect metabolism of some drugs
132
Which population has a delayed gastric emptying & GI motility?
Obstetric
133
What may be altered in the Obstetric population?
Hepatic enzyme activity
Nerve sensitivity
134
What is increased in the Obstetric population?
Increased RBF, GFR (adjust dose)
Increased sensitivity to general anesthetics (greater risk for awareness)
Increased sensitivity to local anesthetics
135
What can affect distribution in the Obstetric population?
Distended epidural veins & decreased CSF volume
136
What can possibly harm the fetus?
Systemic opioids
