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PHARMACOLOGY > PHARMACOLOGY- Pharmacokinectics & Pharmacodynamis > Flashcards

PHARMACOLOGY- Pharmacokinectics & Pharmacodynamis Flashcards

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
Q

What is the Apparent Vd of plasma protein?

A

Bound drugs can be altered by liver and kidney disease

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26
Q

What is the proportion of Protein binding and Volume of distribution?

A

↓ Protein binding ↑ Vd

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27
Q

How are drugs distibuted?

A

In more than one compartment

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28
Q

This is the formula for Volume distribution

A

Vd= Amount of drug in the body/ plasma drug concentration

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29
Q

These are the characteristics of Low of Vd

A

The drug is found in Blood (4-8 L)

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30
Q

Which are the characteristics of the drug in orger to have Low Vd?

A

Large charged molecules; plasma protein bound

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31
Q

Where are located the drugs with medium Vd?

A

ECF

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32
Q

Medium Vd drugs characteristics

A

Small hydrophilic molecules

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33
Q

This is how High Vd drugs are distributed

A

All tissues including fat

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34
Q

These are the characteristics of High Vd drugs

A

Small lipophilic molecules, especially if bound to tissue protein

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35
Q

In pharmacokinetics, what is Hlaf life (t1/2)?

A

The time required to change the amount of drug in the body by 1/2 during elimination (or constant infusion)

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36
Q

Porperty of first order elimination

A

Half life

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37
Q

How many half lives does it takes for Drug infused at a constant rate to reach a steady state?

A

4-5 half lives

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38
Q

How many half lives does it takes to reach 90% of the steady state level?

A

3.3 half lives

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39
Q

Which is the Half life formula?

A

t1/2 = 0.693 X Vd / CL

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40
Q

What is Clearance?

A

The volume of plasma cleared of drug per unit time

41
Q

When is Clearance impaired?

A

With defects in Cardiac, hepatic, or renal function

42
Q

This is Clearance formula

A

CL= rate of elimination of drug/ plasma drug concetration

43
Q

This is an equivalent to clearance

A

Vd X Ke (elimination constant)

44
Q

For Dosage calculation this is the loading dose

A 
  F

Cp= target plasma concentration at steady state

45
Q

In doseage calculation, How is Maintenance dose calculated?

A 
      F

τ= dosage interval (time between doses), if not administer continuously

46
Q

In Which situation are Maintenance dose decreased and loading dose unchaged?

A

In renal or liver disease

47
Q

How are we specting to see loading dose and Maintenance dose in renal or liver disease?

A

Maintenance dose decreased and loading dose unchaged

48
Q

In Which factor does time to steady state depends primarily?

A

T 1/2

49
Q

From Which factor does time to steady state is independent?

A

Dose and dosing frequency

50
Q

How are Eliminations of drugs classified?

A

Zero order elimination

First order elimination

51
Q

What is the purpose of Zero order elimination?

A

Rate of elimination is constatn regardless of Cp (Constant amount of drug eliminated per unit of time)

52
Q

Which drugs have Zero order elimination?

A

Phenytoin
Ethanol
Aspirin (at high or toxic concetrations)

53
Q

This is a characteristic of Zero order elimination

A

Capacity limited elimination

54
Q

This is the main point of First order elimination

A

Rate of elimination is directly proportional to the drug concentration (constant fraction of drug eliminated per unit of time)

55
Q

How is CP affected in first order elimination?

A

Cp exponentially ↓ with time

56
Q

For Zero order elimination this is the way Cp is affected

A

Cp ↓ linearly with time

57
Q

What is Cp in elimination of drugs?

A

target plasma concentration at steady state

58
Q

In first order elimination of drugs which is th dendant?

A

Flow dependent elimination

59
Q

Which species are trapped in urine and cleared quickly?

A

Ionized species

60
Q

Which forms can be reabsorbed in drug elimination?

A

Neutral forms

61
Q

These drugs are consider weak acids

A

Phenobarbital, methotrexate, aspirin

62
Q

In which environments are weak acids trapped?

A

Basic environments

63
Q

How do you treat weak acids overdose?

A

Bicarbonate

64
Q

This is an example of weak bases drugs

A

Amphetamines

65
Q

This is the enviroment where amphetamines (weak bases) are trapped

A

Acidic environments

66
Q

How do you treat amphetamines (weak bases) overdose?

A

Ammonium chloride

67
Q

Which are the phases for Drug elimination?

A

Phase I

Phase II

68
Q

These are phase I drug metabolism of Drugs

A

Reduction, oxidationm hydrolysis with cytochrome P-450 ussually yield slightly polar, water soluble metabolites (often still actives)

69
Q

Which phase of Drug metabolism is first lost in Geriatric patients?

A

Phase I

70
Q

Which patients lose phase I first?

A

Geriatric patients

71
Q

Which process are included in Phase II drug metabolism?

A

Conjugation (Glucuronidation, Acetylation, Sulfation) ussually yields very polar, inactive metabolites (renal excreted)

72
Q

These are conjugation processs

A

Glucuronidation, Acetylation, Sulfation

73
Q

Which patients have greater side effects from certain drugs (related to Phase II drug metabolism)?

A

Patients who are low acetylators

74
Q

Why Patients who are low acetylators have greater side effects from certain drugs?

A

Because of ↓ rate of metabolism

75
Q

What is the efficacy of a drug?

A

Maximal effect a drug can produce

76
Q

Which drugs have high efficacy?

A

Analgesic, antibiotics, antihistamines and decongestant

77
Q

Which medications have less afficacy between partial agonits and full agonist?

A

Partial agonist have less efficacy

78
Q

What is the potency of a drug?

A

Amount of drug needed for a given effect

79
Q

What is proportional to potency of drug?

A

↑ Potency, ↑Affinity

80
Q

These are examples of Highly potetn drug classes

A

Chemotherapeutic
Antihipertensive
Lipid lowering drugs

81
Q

How are Receptor binding classified?

A

Competitive antagonist
Noncompetitive antagonist
Irrevesible competitive antagonist
Partial agonist

82
Q

Which is the effect of a Competitive antagonist?

A

Shifts curve to the right (↓ potency), no change in efficacy

83
Q

In case of competitive antagonist how can it can be overcome?

A

Can be overcome by ↑ the concetration of agonist substrate

84
Q

Name an example of Competitive antagonist. Where do they act?

A

Diazepam+ Flumazenil on GABA receptor (Competitive antagonist)W

85
Q

In receptor binding graphic, what does a shift the curve to the right means?

A

Decreased in potency

86
Q

This is the effect of Noncompetitive antagonist and Irreversible competitive antagonist

A

Shift curve down (↓ efficacy)

87
Q

Which receptor bindings Shift curve down (↓ efficacy)?

A

Noncompetitive antagonist and Irreversible competitive antagonist

88
Q

In receptor binding graphic, what does a shift the curve down means?

A

↓ efficacy

89
Q

Its an example of Noncompetitive antagonist. Where do they work?

A

Glutamate + ketamine on NMDA recetors (Noncompetitive antagonist)

90
Q

Irreversible competitive antagonist. Where do they work?

A

Norepinephrine+ phenoxybenzamine (Irreversible competitive antagonist) on α receptors

91
Q

What is the effect of Partial agonist?

A

Acts at same site as full agonist, but with lower maximal effect (↓ efficacy)

92
Q

How is the potency in partial agonist?

A

Potency is an independent Variable

93
Q

Consider a partial agonist. Where does is acts?

A

Morphine vs buprenorphine (partial agonist) at opioid µ-receptors

94
Q

Measurement of drug safety

A

Therapeutic index

95
Q

Which formula is used for Therapeutic index?

A

TD50 median toxic dose
——— = —————————
ED50 median effective dose

TD- Toxic Dose ED- Effective dose

96
Q

What is the therapeutic window?

A

Measure of clinical drug effectiveness for a patient

97
Q

Which are safer drugs?

A

Safer drugs have higher Terapeutic index values

98
Q

These drugs have low Therapeutic index

A

Digoxin, lithium, theophylline and warfarin

99
Q

What is LD50? and what is it for?

A

Lethal median dose. Often replaces TD50 in animal studies

PHARMACOLOGY (4 decks)

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