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Pharmacology > Exam 1: PharmacoKinetics > Flashcards

Exam 1: PharmacoKinetics Flashcards

1
Q

_________ is the study of how a drug enters the body, circulates within the body, is changed by the body, and leaves the body.

A

Pharmacokinetics

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2
Q

What are the 4 major steps of drug movement in the body?

A

1.Absorption 2.Distribution 3.Metabolism 4.Excretion

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3
Q

Determing a drugs ability to exert an effect: The ______ of drug that is able to pass through a cell membrane…. The ____ at which a drug moves through the body

A

amount…rate

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4
Q

________ = the more, the easier that the drug will cross

A

Lipid Solubility

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5
Q

Degree of ionization (charge) = charged molecules cannot cross (must use _____/_____).

A

pores/channels

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6
Q

______ sized molecules cross more easily.

A

Smaller

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7
Q

_____ of the drug molecule = molecules can “contort” to fit through the membrane

A

Shape

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8
Q

_______ = small molecules that are water- soluble pass through membrane pores by the bulk flow of water

A

Filtration

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9
Q

_______ transport = large, ionized water-soluble drugs require a more complex mechanism than simple diffusion

A

Specialized

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10
Q

________ = drug forms a complex with a component of cell membrane on one side; complex is carried through membrane; drug is released on inside

A

Facilitated diffusion

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11
Q

_______ are engulfed by cell membrane and are released unchanged in cytoplasm (endocytosis)

A

vitamins!

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12
Q

Movement of glucose across cell membranes is _______ by insulin

A

facilitated

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13
Q

__________ = movement of drug molecules across biologic membranes against both a concentration and an electrochemical gradient…Requires _____

A

Active transport….ATP

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14
Q

What are the 3 influences on the RATE a drug is moved across the membrane?

A

1.Physiochemical factors (size, charge, etc) 2.Solubility 3.Route of administration

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15
Q

_______ = drugs given by this route are placed directly into the gastrointestinal tract…THERE ARE ONLY 2 WAYS: ______ & ______

A

Enteral….Oral & Rectal

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16
Q

________= administration that bypasses the gastrointestinal tract and includes various injection routes, inhalation and topical drug administration.

A

Par-enteral

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17
Q

Which route of drug administration is the cheapest, easiest, and most conveneient?

A

Enteral-Oral route

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18
Q

Liquid pills are absorbed more ______ then regular tablets.

A

quickly

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19
Q

A down side to recall route drugs are poorly or irregularly _______ from rectum. Poor patient _______, so its mainly used on ______.

A

absorbed…compliance…babies

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20
Q

Inhalation is a _____ way to access the circulation and it can be both ______ and systemic.

A

rapid…local

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21
Q

What is the MOST RAPID route for drug response, and it produces a _______ response.

A

IntraVenous… Predictable

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22
Q

IntraMuscular route allows for a _______ effect of the drug (absorbed more slowly)

A

sustained

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23
Q

Topical Route: can be either _____ or ______ in effect, depending on dose.

A

local or systemic

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24
Q

What is the newest route of drug administration in dentistry?

A

subgingival! (in pocket)

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25
Q

What is the official title for the route we use to give a IA block?

A

Subcutaneous

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26
Q

In a sublingual route the drug is _____ absorbed.

A

rapidly

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27
Q

What is the most concentrated drug delivery vehicle?

A

Transdermal (pouch)

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28
Q

The _______ route is an injection of solutions into the spinal sub-arachnoid space?

A

IntraTheCal

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29
Q

The _______ route places fluid into the peritoneal cavity for exchange of substances.

A

IntraPeritoneal Route (form of dialysis)

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30
Q

Drug _______ is the movement of the drug from its site of administration into the plasma.

A

absorption

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31
Q

Many drugs are weak ________ (either weak acids or weak bases)

A

elecrtolyes

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32
Q

As weak electrolytes, drugs can exist in either ionized or non-ionized state, depending on the ______ of the environment, the ________ form can diffuse across membranes.

A

pH…Non-ionized

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33
Q

A weak acid in an ______ environment = lipid soluble

A

acidic

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34
Q

A weak acid in a ______ environment = water soluble (dissociates)

A

basic

35
Q

A weak base in ______ environment = water soluble (dissociates)

A

acidic

36
Q

Weak base in a _____ environment = lipid soluble

A

basic

37
Q

Aspirin is a weak _____; pKa for aspirin = 4.4….Therefore, In acid environment of stomach, aspirin dissociates to 1000 uncharged molecules (lipid soluble) to 1 charged molecule (polar, water soluble) = acid gets absorbed across wall of stomach (membrane) into plasma because most of drug is in lipid soluble form

A

acid…

38
Q

Aspirin’s story: However, once in the plasma (pH = 7.4), ratio of _______ aspirin molecules changes: 1000 charged (polar, water soluble) to 1 uncharged (lipid soluble) = aspirin cannot pass back through blood vessel wall membrane into stomach

A

dissociated

39
Q

_______ is the fraction of the administered drug that becomes available in the plasma…only _____ administration gives 100% of this.

A

Bioavailability…IV

40
Q

FDA mandates that generics must have ___% of the bioavailability of the parent compound.

A

90%

41
Q

_________ = drug movement from the site of absorption to the site of action

A

drug distribution

42
Q

What are the two ways drug distribution occurs in the blood?

A

1.bound to plasma proteins 2. free (unbound)

43
Q

Of the 2 ways a drug can be distributed, only the ______ form can pass across cell membranes.

A

free

44
Q

As free drug leaves the plasma, the bound drug becomes “unbound” therefore the “_____” of bound:unbound drug _________ in the blood.

A

“ratio” ….stays the same!!!

45
Q

The bound form of a drug has _____ on the body.

A

NO EFFECT

46
Q

The BLOOD BRIAIN BARRIER: drugs that can cross this barrier are ______-soluble, very _____ molecular weight/size, and exert effects on the central nervous system (CNS).

A

lipid….small

47
Q

Placenta = most drugs cross ______; ______- soluble drugs cross most easily

A

easily…lipid

48
Q

If a drug has a high binding affinity for plasma proteins: remain in the blood ______!

A

longer

49
Q

Hmmm…Cross reactions maybe?!?! When 2 or more drugs are competing for the same plasma protein binding sites for transport through the body, the drug with the highest ________ will become bound to plasma proteins..Other drug(s) will remain unbound or “free” to exert their effects by reacting with target tissue

A

binding affinity

50
Q

Most of the drugs are cleared/removed from the body in __ to ___ half-lives.

A

4 to 5 half lives

51
Q

It takes approximately __ to __ half-lives for a drug to build up to a steady state level (level amount) in the body.

A

4 to 5

52
Q

_______ is the movement of the drug from the site of action to nonspecific sites of action…if it occurs the drug’s action will be _______.

A

Redistribution…terminated

53
Q

An “induction” agent that helps knock your ass out before surgery is an example of _______ because it’s action is diminished after it moves from the CNS to muscle.

A

redistribution

54
Q

Drug metabolism is also known as _________.

A

Biotransformation

55
Q

Drug metabolism/biotransformation works by converting a drug from _____ soluble to ______ soluble metabolites that can be excreted by the kidneys.

A

lipid…water

56
Q

Which organ is the most common drug metabolizer? What are its enzymes called?

A

the LIVER!…cytochrome P450 system)

57
Q

Phase I of biotransformation: occurs in the _____ where the drug molecule is modified through _______, _______, or _______.

A

oxidation, reduction, or hydrolysis

58
Q

In Phase II of biotransformation the drug molecule is modified by conjugation to a large _____ endogenous molecule. Phase II metabolites are pharmacologically _____.

A

polar…inactive

59
Q

Since metabolism breaks down or “inactivates” drugs, then increasing the rate of metabolism would ________ the action of the drug

A

decrease

60
Q

If Drug A induces the metabolism of Drug B, then the action of Drug B would be _______.

A

reduced

61
Q

If we “_____” cytochrome P450 liver enzymes, we decrease the rate of metabolism.

A

“inhibit”

62
Q

Since metabolism breaks down or “inactivates” drugs, then _________ the rate of metabolism would _______ the action of the drug.

A

decreasing….increase

63
Q

If Drug A inhibits the metabolism of Drug B, then the action of Drug B would be ________.

A

increased

64
Q

The most common mechanism of biotransformation is ______ to inactive.

A

active

65
Q

Mechanism of biotransformation: What is the nickname for drugs that go from inactive to active?

A

“prodrugs”-the inactive parent drug is converted to an active drug after metabolism

66
Q

Mechanism of biotransformation: Active parent drug is converted to a second active drug (metabolite is active). this is called ______ to ______.

A

active to active

67
Q

Liver function declines with age, so it often requires a _____ modification.

A

dose

68
Q

The first pass effect is only for drugs that are administered ______.

A

orally

69
Q

Drugs that are given ________ bypass the first pass effect.

A

parenterally

70
Q

What is the principle organ of drug excretion/elimination out of the body?

A

the kidney

71
Q

Did you know: Salivary drug concentration mimics ______ concentration!

A

blood plasma

72
Q

If a drug is FAT SOLUBLE when it reaches the kidneys, it will be _______ by the kidneys and be placed back into the blood stream.

A

reabsorbed

73
Q

EVERYONE screws this up: _______ drug elimination: The amount of drug eliminated is dependent upon the amount of drug in the plasma at any given time.

A

First Order Drug Elimination

74
Q

IN First Order Drug Elimination: A constant _______ of the drug is eliminated per unit time.

A

FRACTION (5%ofdrug/min) ((where as zero order is 5mg/min))

75
Q

________ half-life = rapid decline in plasma drug concentration as 50% of drug distributed throughout the body

A

Distribution

76
Q

_______ half-life = time required to excrete 50% of drug from the system

A

Elimination

77
Q

_______ drug elimination: A given amount of drug is eliminated per unit time

A

ZERO order drug elimination

78
Q

In Zero Order Drug elimination a _______ amount of drug is eliminated per unit time.

A

GIVEN

79
Q

An example of Zero Order Drug Elimination is Alcohol, because it is eliminated at a rate of 1 gram per hour, the rate is ______.

A

constant!

80
Q

_______ concentration: Following administration of MULTIPLE therapeutic dosages of a drug at REGULAR time intervals, a plateau level of drug accumulates.

A

Steady-State

81
Q

A Steady-State concentration ______ represents a rate of drug administration that is EQUAL to the rate of drug elimination.

A

plateau

82
Q

Stready State Accumulation: If the drug is taken too _____ (too ______) before the preceding dose is eliminated completely, the next dose will ADD to the residual amount of drug still remaining in the body. EVENTUALLY The rate of intake _______ the rate of elimination!!

A

soon…frequently..exceeds

83
Q

At a ______ dosing frequency, the drug does not accumulate and a steady state or equilibrium is eventually reached.

A

regular

84
Q

The higher the drug concentration, the greater is the amount ________ per unit time

A

eliminated

Pharmacology (23 decks)

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