Ch 4 Pharmacokinetics / Dynamics Flashcards

1
Q

The study of drug movement through the body

A

Pharmacokinetics

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2
Q

Name the four Basic processes of pharmacokinetics

A

Absorption

distribution

metabolism

excretion

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3
Q

The drugs movement from the site of administration into the blood

A

Absorption

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4
Q

The movement of the drug from the blood to the interstitial space of tissues and from there into the cells

A

Distribution

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5
Q

The enzymatically mediated alteration of drug structure. This is also known as biotransformation

A

Metabolism

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6
Q

The movement of drugs and their metabolites out of the body

A

Excretion

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7
Q

True or false: the combination of metabolism and excretion is called elimination

A

True

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8
Q

The goal of applying knowledge of pharmacokinetics to drug therapy is to maximize beneficial effects and minimize harm

A

True

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9
Q

True or false: distribution is the only phase of pharmacokinetics that involves drug movement across membranes

A

False: To move through the body in all four phases of pharmacokinetics drugs must cross membranes

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10
Q

Name the three ways drugs can cross cell membranes

A

Channels or pores

passage with the aid of a transport system

direct penetration of the membrane (most common)

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11
Q

True or false: membranes are composed primarily of lipids therefore to directly penetrate a membrane - a drug must be lipid soluble.

A

True

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12
Q

True or False: potassium and sodium are too large to cross membranes through channels or pores

A

False: K+ and Na+ are examples of the smallest of compounds that can pass through these channels if the channel is the right one.

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13
Q

Name two kinds of molecules that are not lipid soluble and cannot penetrate membranes

A

Polar molecules

ions

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14
Q

True or false: water is an example of an ion with a positive charge

A

False: water is an example of a polar molecule that has no net charge

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15
Q

True or False: Ions are an example of molecules that have a net positive charge

A

False: ions are molecules that have a net electrical charge that can be either positive or negative

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16
Q

___________ Is the process whereby a drug accumulates on the side of a membrane where the pH most favors it’s ionization

A

Ion trapping

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17
Q

Acidic drugs accumulate on the ___________ side

A

Alkaline

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18
Q

Basic drugs accumulate on the __________ side

A

Acidic

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19
Q

What five factors affect drug absorption

A

Rate of dissolution

surface area

blood flow

lipid solubility

PH partitioning

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20
Q

True or false: the rate of absorption determines how soon effects will begin where is the amount of absorption helps determine how intense effects will be

A

True

21
Q

True or false: drug preparations are considered chemically equivalent if the drug they contain is absorbed at the same rate in to the same extent

A

False: Drug preparations are considered chemically equivalent if they contain the same amount of the identical chemical compound / drug

Preparations are considered equal in bio availability if the drug they contain is absorbed at the same rate in to the same extent

22
Q

What three processes affect drug distribution ?

A

Blood flow to the tissues,

the ability of a drug to exit the vascular system,

the ability of a drug to enter cells

23
Q

Why must abscesses usually be surgically drained for drug therapy to be effective?

A

Abscesses have no internal blood vessels so they have no blood supply therefore antibiotics cannot reach the bacteria within

24
Q

___________ Is a transporter known as a multi drug transporter protein that transports a wide variety of drugs out of cells

A

P - glycoproteins (PGP)

25
Q

Most drug metabolism takes place in the _________

A

Liver

26
Q

What is another name for the hepatic microsomal enzyme system that takes place in the liver?

A

P450 or cytochrome P450 which is made of 12 closely related enzyme families

27
Q

Name the three P450 families that metabolize drugs

A

CYP1

CYP2

CYP3

28
Q

The other 9 P450 enzyme families metabolize __________ compounds like ______ &________.

A

Endogenous

Steroids and fatty acids

29
Q

What is the most important consequence of drug metabolism and why

A

Promotion of renal drug excretion is the most important consequence because the kidneys are the major organ of drug excretion. They cannot excrete drugs that are highly lipid soluble. If drugs can be converted into more hydrophilic forms metabolic conversion can accelerate renal excretion of many agents

30
Q

Name six consequences of drug metabolism of therapeutic significance

A

Accelerated renal excretion of drugs,

drug and activation,

increased therapeutic action,

activation of pro drugs,

increased toxicity,

decreased toxicity

31
Q

Metabolism converting codeine and some morphine is an example of what

A

Increased therapeutic action

32
Q

This is a compound that is pharmacologically an active as administered and undergoes conversion to it’s active form through metabolism

A

Prodrug

33
Q

This refers to the rapid hepatic an activation of certain oral drugs

A

First pass effect

34
Q

This is the time required for the amount of drug in the body to decrease by 50% and determines dosing interval

A

Drug half life

35
Q

The study of the bio chemical and physiologic effects of drugs on the body and the molecular mechanisms by which those effects are produced

A

Pharmacodynamics

36
Q

The largest defect that he drug can produce

A

Maximal efficacy

37
Q

The amount of drug we must give to elicit an effect it’s indicated by the relative position of the dose response curve

A

Potency

38
Q

This is any functional macromolecule any cell to which a drug binds to produce it’s effects

A

Receptor

39
Q

This refers to the strength of the attraction between a drug and it’s receptor

A

Affinity

Drugs with higher Affinity are very potent

40
Q

The ability of a drug to activate a receptor up on binding

A

Intrinsic activity

Drugs with high intrinsic activity have high maximal efficacy

41
Q

True or false: agonist are molecules that deactivate receptors

A

FALSE

Agonists - ACTIVATE

42
Q

True or false: antagonists produce their effects by preventing receptor activation by endogenous regulatory molecules and drugs

A

TRUE

43
Q

The average effective dose - this is also defined as the dose required to produce a defined therapeutic response in 50% of the population

A

ED50

44
Q

This is a measure of a drugs safety it is defined as the ratio of a drugs lethal dose (LD50) to its effective dose (ED50). The larger this is the safer the drug is

A

Therapeutic index

45
Q

When another substance alters a drug efficacy effects or safety

A

Drug interaction

46
Q

True or false: albuterol and propanolol should not be taken together

A

True : Propanolol reduce his albuterol therapeutic effects

47
Q

Which isoenzyme does grapefruit juice effect by inhibiting metabolism metabolism

A

CYP3A4

48
Q

Name some examples of food on drug

A

MAO inhibitor combined with foods rich in tyramine like aged cheeses yeast extract and she Chianti wine. This combination causes life-threatening elevation and blood pressure

Theophylline combined with caffeine can cause excessive CNS excitation

Potassium sparing diuretics like spironolactone plus salt substitute can result in dangerously high potassium levels

Aluminum containing antacids plus citrus beverages can result in excessive absorption of aluminum

49
Q

How does vitamin K reduce the effects of warfarin?

A

Warfare and inhibits vitamin K dependent clotting factors so in vitamin K is more abundant warfarin and is less able to inhibit the clotting factors and therapeutic effects decline