Week 2 Flashcards

1
Q

Drugs are biologic active substances that can modify

A

Cell function

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2
Q

Terms used to measure drug response or ACTION

A

Dose response curve
Potency
Efficacy

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3
Q

Describe dose effect curve

A

Dose of a drug (amount) given with a measured effect (response)

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4
Q

On a dose effect curve graph what does x axis represent and what does h axis represent

A

X axis - increasing dose
Y axis - increasing effect of the drug

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5
Q

Describe what the therapeutic effect looks like on a graph

A

As dose (x axis) increases the effect is 0 at first then a quick increase effect

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6
Q

What does EC50

A

Effective concentration of drug is needed to get half of maximum effect

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7
Q

What is potency

A

The amount of drug to provide an effect

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8
Q

Potency is shown by the location along the

A

Log dose axis (x axis )

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9
Q

10mg of morpheme has the same effect as 100mg of meperidine therefore which is more potent?

A

Morphine

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10
Q

More potent drugs can reach _____ levels at lower doses

A

Toxic

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11
Q

What is the maximum intensity of effect (response) that can be produced by a drug no matter the dose

A

Maximal effect

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12
Q

If drug dose is increased after maximal effect it may increase chance for an?

A

Adverse reaction

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13
Q

Efficacy indicates?

A

Drug action

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14
Q

What is the therapeutic index (TI)

A

Ratio of median lethal dose (LD50) to the median effective dose (ED50)
* TI = LD50/ED50

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15
Q

What is LD50

A

Death dose in 50% of test animals

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16
Q

What is ED50

A

Dose required to produce desirable effect on 50% of tested animals

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17
Q

The higher the therapeutic index (TI)

A

The safer the drug

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18
Q

Drugs do not perform a new function on the organism, either the drug produces the same ____ or ____

A

The same action as an endogenous agent or block the action of the endogenous agent

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19
Q

Endogenous agents are

A

Any chemicals produced in your body (ex hormones)

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20
Q

Drug must bind to a ____ on the cell membrane to exert an effect

A

Receptor

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21
Q

What are drug receptors

A

Many large molecules (proteins) either on the cell membrane or within the cell

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22
Q

Usually specific drug binds with a specific receptor, what action is happening?

A

Lock and key

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23
Q

Drug receptor interactions are

A

Weak chemical bonds

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24
Q

Different drugs compete for same receptor sites, stronger ____(more potent) binds with more receptors than weaker _____ (less potent) drugs

A

Affinity for both blanks

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25
Q

Describe agonist drugs

A

Naturally occurring neurotransmitters (NTs)

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26
Q

Describe process of agonist drugs

A

Affinity for a receptor
Combines with receptor
Produces an effect

27
Q

Antagonist drugs do what?

A

Counteracts agonist drugs

28
Q

What are the 3 types of antagonist drugs

A

Competitive antagonist
Non competitive antagonist
Physiologic antagonist

29
Q

Describe the mechanism for competitive antagonist

A

Affinity for receptor
Combines with receptor
Produces no effect

30
Q

Describe the mechanism of a noncompetitive antagonist

A

Binds to a different receptor site than antagonist
Reduces maximal response of agonist

31
Q

Describe mechanism of physiologic antagonist

A

Affinity for a different receptor than agonist
Decreases maximal response of the agonist by producing an opposite effect via different receptors

32
Q

Amount and rate of drug passing through cell membrane are important in what 2 things

A

Time course of action
Individual response

33
Q

Membranes are composed of (3)

A

Lipids
Proteins
Carbohydrates

34
Q

Lipid soluble substance moves across the lipoprotein membrane by passive transfer called

A

Simple diffusion using a concentration gradient (from high to low concentration)

35
Q

Water soluble substances have difficulty passing through

A

A lipoprotein membrane

36
Q

In active transport substances are transported

A

Against a concentration gradient
Blocked by metabolic inhibitors
Mediated by transport “carriers” with energy

37
Q

Facilitated diffusion does not

A

Move against a concentration gradient

38
Q

Factors that influence the movement of drugs are in 4 major steps (ADME)

A

Absorption
Distribution
Metabolism
Excretion

39
Q

Absorption refers to the process where drug molecules are transferred from where to what?

A

From administration site to circulating blood, passing through biologic membranes

40
Q

What 3 things influence rate of absorption

A

Physiochemical factors
Site of absorption
Solubility

41
Q

Weak electrolyte drugs dissociate (separate) in solution (pKa) and break into?

A

Un-ionized and ionized forms

42
Q

Describe un ionized

A

Uncharged non polar lipid soluble
EASILY crosses cell membrane

43
Q

Describe ionized

A

Charged polarized less lipid soluble
DIFFICULT to cross cell membrane

44
Q

What 2 things will determine the amount of drug present in ionized and un ionized states

A

pH of site of administration and dissociation characteristics

45
Q

Weak acids are better absorbed when

A

pH is less than pKa

46
Q

Weak bases are better absorbed when

A

The pH is greater than the pKa

47
Q

Release of dose from a tablet or capsule follows what 4 steps in oral absorption

A

Disruption (of coating)
Disintegration
Dispersion
Dissolution (dissolved in GI fluid)

48
Q

Drug in solution skips the oral absorption steps and usually a quicker

A

Onset of action

49
Q

Absorption from injection site; if the drug has low solubility then it has a ____ duration

A

Longer

50
Q

Drugs occur in 2 forms in the blood

A

Bound to plasma proteins (reservoir for the drug)
Free drug (pharmacological effect b/c it only passes through cell membrane)

51
Q

Distribution is the passage of drugs into various body fluid compartments for an

A

Action

52
Q

What are some factors of distribution

A

Size of the organ
Blood flow of the organ
Solubility of the drug
Plasma protein binding capacity
Barriers

53
Q

Biologic activity of a drug is related to

A

Concentration of the free or unbound drug in the plasma
(This is the biologically active drug)

54
Q

drug interaction happens when one drug is bounded and another highly bounded drug displaces the first drug from plasma protein binding sites increasing what?

A

The effect of the first drug

55
Q

Blood brain barrier; to penetrate the CNS depends on the (2)

A

Drugs lipid solubility and degree of ionization

56
Q

What is a highly lipid soluble un ionized drug easily penetrates the blood brain barrier to access CF and induce sleep seconds after IV

A

Thiopental

57
Q

In what kind of circulation are metabolites secreted via bile into intestine and continue with some drug being excreted in the cycle

A

Enterohepatic circulation

58
Q

Enterohepatic circulation allows for ?

A

Prolonged effect of the drug

59
Q

Drugs get ____ if it goes to a non specific site

A

Terminated

60
Q

Metabolism (bio transformation): produces compounds that are more

A

Polar and more easily excreted
(Mostly in the LIVER)

61
Q

Metabolite is more ____ and ____ soluble therefore renal reabsorption with be _____ b/c reabsorption favours lipid soluble metabolites

A

Polar and lipid soluble
Reduced

62
Q

Metabolism is what kind of process

A

Enzyme dependent process

63
Q

What are the 3 ways drugs metabolize

A

Active to inactive
Inactive to active
Active to active