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PHARMACOLOGY- Pharmacokinectics & Pharmacodynamis Flashcards

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1
Q

In pharmacology, Which are the Enzyme Kinetics?

A

Michaelis Menten kinetics
Lineweaver Burk plot
Enzyme inhibition

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2
Q

What is the Michaelis Menten kinetics?

A

Equation describing the rate of enzymatic reactions, by relating reaction rate v to [S], the concentration of a substrate S.

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3
Q

In Michaelis Menten kinetics what is equivalent to Km?

A

Km is irreversely related to the affinity of the enzyme for its substrate

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4
Q

What is the meaning of Km in Michaelis Menten kinetics?

A

The Michaelis constant Km is the substrate concentration at which the reaction rate is half of V\max

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5
Q

What does the Vmax represents in Michaelis Menten kinetics?

A

Vmax is directly proportional to the enzyme concentration

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6
Q

In graphics which is the form of enzymatic reactions in Michaelis Menten kinetics?

A

Most enzymatic reactions follow a hyperbolic curve

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7
Q

What does a sigmoid curve indicates in Michaelis Menten kinetics?

A

Cooperative kinetics (eg. Hemoglobin)

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8
Q

This is the alternative name for Lineweaver–Burk plot

A

Double reciprocal plot

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9
Q

Which is the proportion of Lineweaver–Burk plot

A

↑ y intercept, ↓ Vmax

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10
Q

How is Lineweaver–Burk plot interpreted

A

The further to the right the x intercept (closer to zero), the greater the Km and the lower the affinity

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11
Q

Which are the characters of Enzyme inhibition?

A

Noncompetitive inhibitor
Competitive inhibitor
Uninhibited

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12
Q

In enzyme inhibition which is the difference between Noncompetitive inhibitor and Competitive inhibitor?

A

Competitive inhibitor cross each other competitively, whereas Noncompetitive inhibitor do not

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13
Q

How are Competitive inhibitor classifed?

A

Reversible

Irreversible

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14
Q

What is pharmacokinetics?

A

The effect of the body on the drug

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15
Q

What is pharmacodynamics?

A

The effect of the drug on the body

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16
Q

This is the mnemonic of Pharmacokinetics

A 
ADME
Absorption
Distribution
Metabolism
Excretion
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17
Q

Which are the characteristics of Pharmacodynamics?

A

Receptor binding
Drug efficacy
Drug potency
Toxicity

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18
Q

These are the main points of Pharmacokinetics

A

Bioavailability
Volume distribution
Half life
Clearance

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19
Q

How is bioavailability abbreviated?

A

F

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20
Q

What is bioavailability?

A

Fraction of administered drug that reaches systemic circulation unchaged

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21
Q

If a drug is administer IV, which is the percentage of Bioavailability?

A

100%

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22
Q

If a drug is administer oraly, which is the percentage of Bioavailability? Why?

A

F typically < 100% due to imcomplete absorption and first-pass metabolism

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23
Q

What is Vd?

A

Volume of distribution

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24
Q

What is Volume of distribution?

A

Theoretical volume occupied by the total absorbed drug amount at the plasma concetration

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25
What is the Apparent Vd of plasma protein?
Bound drugs can be altered by liver and kidney disease
26
What is the proportion of Protein binding and Volume of distribution?
↓ Protein binding ↑ Vd
27
How are drugs distibuted?
In more than one compartment
28
This is the formula for Volume distribution
Vd= Amount of drug in the body/ plasma drug concentration
29
These are the characteristics of Low of Vd
The drug is found in Blood (4-8 L)
30
Which are the characteristics of the drug in orger to have Low Vd?
Large charged molecules; plasma protein bound
31
Where are located the drugs with medium Vd?
ECF
32
Medium Vd drugs characteristics
Small hydrophilic molecules
33
This is how High Vd drugs are distributed
All tissues including fat
34
These are the characteristics of High Vd drugs
Small lipophilic molecules, especially if bound to tissue protein
35
In pharmacokinetics, what is Hlaf life (t1/2)?
The time required to change the amount of drug in the body by 1/2 during elimination (or constant infusion)
36
Porperty of first order elimination
Half life
37
How many half lives does it takes for Drug infused at a constant rate to reach a steady state?
4-5 half lives
38
How many half lives does it takes to reach 90% of the steady state level?
3.3 half lives
39
Which is the Half life formula?
t1/2 = 0.693 X Vd / CL
40
What is Clearance?
The volume of plasma cleared of drug per unit time
41
When is Clearance impaired?
With defects in Cardiac, hepatic, or renal function
42
This is Clearance formula
CL= rate of elimination of drug/ plasma drug concetration
43
This is an equivalent to clearance
Vd X Ke (elimination constant)
44
For Dosage calculation this is the loading dose
Cp X Vd ------------- F Cp= target plasma concentration at steady state
45
In doseage calculation, How is Maintenance dose calculated?
Cp X CL X τ ------------------ F τ= dosage interval (time between doses), if not administer continuously
46
In Which situation are Maintenance dose decreased and loading dose unchaged?
In renal or liver disease
47
How are we specting to see loading dose and Maintenance dose in renal or liver disease?
Maintenance dose decreased and loading dose unchaged
48
In Which factor does time to steady state depends primarily?
T 1/2
49
From Which factor does time to steady state is independent?
Dose and dosing frequency
50
How are Eliminations of drugs classified?
Zero order elimination | First order elimination
51
What is the purpose of Zero order elimination?
Rate of elimination is constatn regardless of Cp (Constant amount of drug eliminated per unit of time)
52
Which drugs have Zero order elimination?
Phenytoin Ethanol Aspirin (at high or toxic concetrations)
53
This is a characteristic of Zero order elimination
Capacity limited elimination
54
This is the main point of First order elimination
Rate of elimination is directly proportional to the drug concentration (constant fraction of drug eliminated per unit of time)
55
How is CP affected in first order elimination?
Cp exponentially ↓ with time
56
For Zero order elimination this is the way Cp is affected
Cp ↓ linearly with time
57
What is Cp in elimination of drugs?
target plasma concentration at steady state
58
In first order elimination of drugs which is th dendant?
Flow dependent elimination
59
Which species are trapped in urine and cleared quickly?
Ionized species
60
Which forms can be reabsorbed in drug elimination?
Neutral forms
61
These drugs are consider weak acids
Phenobarbital, methotrexate, aspirin
62
In which environments are weak acids trapped?
Basic environments
63
How do you treat weak acids overdose?
Bicarbonate
64
This is an example of weak bases drugs
Amphetamines
65
This is the enviroment where amphetamines (weak bases) are trapped
Acidic environments
66
How do you treat amphetamines (weak bases) overdose?
Ammonium chloride
67
Which are the phases for Drug elimination?
Phase I | Phase II
68
These are phase I drug metabolism of Drugs
Reduction, oxidationm hydrolysis with cytochrome P-450 ussually yield slightly polar, water soluble metabolites (often still actives)
69
Which phase of Drug metabolism is first lost in Geriatric patients?
Phase I
70
Which patients lose phase I first?
Geriatric patients
71
Which process are included in Phase II drug metabolism?
Conjugation (Glucuronidation, Acetylation, Sulfation) ussually yields very polar, inactive metabolites (renal excreted)
72
These are conjugation processs
Glucuronidation, Acetylation, Sulfation
73
Which patients have greater side effects from certain drugs (related to Phase II drug metabolism)?
Patients who are low acetylators
74
Why Patients who are low acetylators have greater side effects from certain drugs?
Because of ↓ rate of metabolism
75
What is the efficacy of a drug?
Maximal effect a drug can produce
76
Which drugs have high efficacy?
Analgesic, antibiotics, antihistamines and decongestant
77
Which medications have less afficacy between partial agonits and full agonist?
Partial agonist have less efficacy
78
What is the potency of a drug?
Amount of drug needed for a given effect
79
What is proportional to potency of drug?
↑ Potency, ↑Affinity
80
These are examples of Highly potetn drug classes
Chemotherapeutic Antihipertensive Lipid lowering drugs
81
How are Receptor binding classified?
Competitive antagonist Noncompetitive antagonist Irrevesible competitive antagonist Partial agonist
82
Which is the effect of a Competitive antagonist?
Shifts curve to the right (↓ potency), no change in efficacy
83
In case of competitive antagonist how can it can be overcome?
Can be overcome by ↑ the concetration of agonist substrate
84
Name an example of Competitive antagonist. Where do they act?
Diazepam+ Flumazenil on GABA receptor (Competitive antagonist)W
85
In receptor binding graphic, what does a shift the curve to the right means?
Decreased in potency
86
This is the effect of Noncompetitive antagonist and Irreversible competitive antagonist
Shift curve down (↓ efficacy)
87
Which receptor bindings Shift curve down (↓ efficacy)?
Noncompetitive antagonist and Irreversible competitive antagonist
88
In receptor binding graphic, what does a shift the curve down means?
↓ efficacy
89
Its an example of Noncompetitive antagonist. Where do they work?
Glutamate + ketamine on NMDA recetors (Noncompetitive antagonist)
90
Irreversible competitive antagonist. Where do they work?
Norepinephrine+ phenoxybenzamine (Irreversible competitive antagonist) on α receptors
91
What is the effect of Partial agonist?
Acts at same site as full agonist, but with lower maximal effect (↓ efficacy)
92
How is the potency in partial agonist?
Potency is an independent Variable
93
Consider a partial agonist. Where does is acts?
Morphine vs buprenorphine (partial agonist) at opioid µ-receptors
94
Measurement of drug safety
Therapeutic index
95
Which formula is used for Therapeutic index?
TD50 median toxic dose --------- = --------------------------- ED50 median effective dose TD- Toxic Dose ED- Effective dose
96
What is the therapeutic window?
Measure of clinical drug effectiveness for a patient
97
Which are safer drugs?
Safer drugs have higher Terapeutic index values
98
These drugs have low Therapeutic index
Digoxin, lithium, theophylline and warfarin
99
What is LD50? and what is it for?
Lethal median dose. Often replaces TD50 in animal studies

PHARMACOLOGY (4 decks)

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