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Intro to Pharmacology > Week 2 Lectures > Flashcards

Week 2 Lectures Flashcards

1
Q

Metabolism is a ______ mechanism against adverse effects of ________ ________.

A

defense, lipophilic xenobiotics

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2
Q

What would happen in biological systems without drug metabolism?

  • ________ compounds would stay in the body for a much longer period of time.
  • Drugs would have a _______ activity
  • There would be a tissue drug _______
  • Potential ______.
A

Absorbed, prolonged, accumulation, toxicity

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3
Q

The _____ is the major organ for drug metabolism in the body

A

liver

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4
Q

Drug metabolism in the liver depend on factors such as?
• _________ properties of the liver (existence of major drug metabolism ______)
• Hepatic _____/______ rate
• Drug ________ to and _______ by hepatic metabolic sites
• ________ properties of the drug (______, _______ ______, _______ _____)

A

Biological, enzymes, volume, perfusion, accessibility, extraction, Physicochemical, pKa, lipid solubility, molecular weight

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5
Q

Most drugs are eliminated by ______ metabolism, ______ excretion, or ____.

A

hepatic, renal, both

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6
Q

Lipid-soluble drugs require conversion to a _____-
soluble form before they can be eliminated by the _______

A

water, kidney

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7
Q

Hepatic metabolism can be divided into phase I and
phase II. Explain this process.

A

The main goal of phase 1 and 2 is to increase water solubility

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8
Q

The majority of drug metabolism occurs in ______ but the _____ is not the only site. Other organs with substantial metabolic capacity include?

A

liver, liver, kidney, lungs, skin, GI tract.

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9
Q

The ______ is also capable of metabolizing some drugs, although this capacity is only occasionally of clinical importance

A

kidney

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10
Q

Most metabolizing enzymes are located in the _______ ________ _______ (___) of the
hepatocyte, others are located in the ______ of the cell.

A

smooth endoplasmatic reticulum, SER, cytosol

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11
Q

The enzymes located in the SER consist of a protein (________) with an ____ central core (______) that absorbs light at ___ nm when bound to _______ _______.

A

cytochrome, iron, pigmented, 450, carbon monoxide

Cytochrome 450 is the most important family of enzymes.

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12
Q

The enzymes in the SER are actually an enzyme _______ that can be genetically classified as a ________ containing several ______ of enzymes.

A

system, superfamily, subfamilies

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13
Q

All CYP-mediated drug metabolic reactions involve the addition of a _______ atom of _______ onto the substrate.

A

single, oxygen

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14
Q

Examples of cytochrome P450 enzymes and
substrates in the dog. DO WE HAVE TO KNOW THIS?

A

did she say we have to know this chart? could not understand

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15
Q

The major phase I drug-metabolizing reactions include?

A

Oxidation, hydrolysis, reduction.

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16
Q

In Phase 1 metabolism, oxidation is the addition of _______ across a ______ double bond, addition of _______ to a carbon chain, and the loss of an ______.

A

oxygen, carbon, oxygen, electron

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17
Q

In Phase 1 metabolism, hydrolysis is the ________ of the drug molecule and addition of a _____ molecule to each of the _____ portion.

A

splitting, water, split

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18
Q

In Phase 1 metabolism, reduction is the addition of ______ and an _____.

A

hydrogen, electron

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19
Q

Most ______ drugs can be deactivated to inactive
metabolites. In contrast, some drugs can also be
activated from an inactive form, ______ to an
active drug, or from an active form to an ______ _______.

A

parent, prodrug, active metabolite

By first phase of metabolism, not everyone will be destroyed or activated.

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20
Q

There are considerable differences among the species in the _______ of the oxidative enzymes

A

activity

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21
Q

List these species in order from highest to lowest in regards to oxidation: cattle, dogs, cats, horses

A

Oxidation is higher in horses > cattle > dogs > cats

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22
Q

The duration of pentobarbital anesthesia in horses is _______ than in dogs.

A

shorter

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23
Q

Phase II, also known as ______, occurs when a _______ _____-soluble molecule is chemically added to either the ______ drug or its phase ____ metabolite

A

conjugation, large, water, parent, I

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24
Q

Glucuronidation is the ______ ______ phase II reaction. Glucuronide conjugates are eliminated in the _____ and ____.

A

most common, urine, bile

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25
Q

______ and ______ are also phase II reactions.

A

Sulfation, acetylation

the most important reaction is the glucorindation

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26
Q

Which of the following statements regarding phase I and II metabolic reactions is true?

A. Phase II acts only on phase I metabolites

B. Phase I acts on parents drugs and/or phase I metabolites

C. Phase II acts on parent drugs and/or phase I metabolites

D. Phase II acts only on parents drugs.

A

C. Phase II acts on parent drugs and/or phase I metabolites

B can not be true because there are no metabolites? in this phase.

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27
Q

What are the enzymes involved in phase II metabolism?

A

glucuronosyltransferase, sulfotransferase, N-acetyltransferase and methyltransferase

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28
Q

Most of ____________ is eliminated by glucoronidation and sulfation.

A

acetaminophen

Many drugs can be metabolized via different types of reactions.

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29
Q

As in humans, ________ in drug-metabolizing enzymes has been reported in dogs but it is
not as well described.

A

polymorphism

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30
Q

Polymorphisms in CYP metabolic enzymes have been associated with ________ ______.

A

therapeutic failure

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31
Q

Polymorphisms in CYP metabolic enzyme results in?

A
  • Extremely rapid metabolism of a drug
  • Toxic effects caused by decreased metabolism
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32
Q

Cytochrome-mediated clearance of anesthetic agents is less in _________ compared with other (______ _____) dogs. Documented drugs include?

A

Greyhounds, nonsight hound
Thiopental, thiamylal and methohexital

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33
Q

Clearance of ________ by Greyhounds is three time less than by Beagles

A

propofol

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34
Q

Cats have very low activity of _______, but activity of ______ and _____ approximates that of dogs
or humans.

A

CYP2C, CYP2D, CYP3A

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35
Q

Notice which isoforms are associated with isoforms and which ones have a very low association

A
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36
Q

CYP2D15
In a study of 242 Beagles receiving celecoxib, approximately ___% were considered efficient metabolizers and ____% poor metabolizers. The PM group showed a ______ and maximum ___ almost twofold higher.

A

50, 50, bioavailability, PDC

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37
Q

Deficiencies in phase II metabolism have long been recognized in ____. This is because they have extremely low concentrations of some _______ _______.

A

cats, glucoronyl tranferases

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38
Q

Many drugs excreted as glucuronide conjugates in species other than cats are characterized by a ________ clearance and ______ pharmacologic responses. ____ levels may accumulate much more quickly.

A

prolonged, exaggerated, Toxic

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39
Q

Deficiencies in phase I demethylation and hydroxylation as well as phase II glucuronidation lead to a much ________ elimination of ______ and _____ ____ and _______ in the cat compared with other species

A

slower, phenols, aromatic acids, amines

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40
Q

Aspirin half-life approximates ___ hours in cats
compared with __ hours in dogs. To prevent
toxicity in the cat, aspirin is dosed every ___ to ___
hours, compared with twice daily in dogs.

A

36 , 8, 48, 72

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41
Q

Because cats are deficient in __________, excessive acetaminophen is shunted more aggressively back into phase __ metabolism, which produces toxic ______ ______. More _______ are produced than can be handled causing
destruction of _____ (____ and ____)

A

glucuronidation, I , oxygen radicals, metabolites, tissues, liver, RBCs

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42
Q

Not all drugs that are conjugated with ________ are predisposed to toxicity in the cat.

A

glucuronide

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43
Q

The cat is deficient only in certain families of ________ ________.

A

glucuronyl transferase

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44
Q

Cats can _______ and ______ endogenous substrates such as ______, ______ hormones as
well as other species.

A

conjugate, excrete, bilirrubin, steroid

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45
Q

The degree of _______ and potential ______ depend on the drug substrate: level of ______, wide _______ margin (If accumulation occurs).

A

deficiency, toxicity, conjugation, safety

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46
Q

Drugs may be sufficiently metabolized by an alternative pathway: ?

A

Sulfate-conjugating system.

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47
Q

_________ is not a common route of elimination for xenobiotics, but it is an enzyme system whose deficiency in the ______ (____ and other ____ species) is clinically relevant.

A

Acetylation, canine, dog, canine

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48
Q

The antiarrhythmic procainamide is _________ in humans to an active metabolite. This ________ metabolite is more potent than the _____ drug. Because of this the canine dose for _______ is considerably ______ than that in humans in order to
achieve an equivalent pharmacologic response.

A

acetylated, acetylated, parent, procainamide, higher

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49
Q

Sulfonamides are detoxified by __-______ in humans. The dog lacks the ability to acetylate ______ ______, relying on alternative metabolic pathways to convert sulfonamides to ____ ____ forms (________ conjugation and aromatic __________)

A

N-acetylation, aromatic amines, less active, glucuronide, hydroxylation

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50
Q

Factors that can affect hepatic drug metabolism include

A
  • The amount and activity of drug- metabolizing enzymes
  • Hepatic blood flow
  • A flow-limited drug
  • Species, age, nutritional status, tissue storage, health status
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51
Q

Some diets may inhibit or induce the _______ enzyme system. Flavonoids found in ______ _____
inhibit CYP3A4 in the _____ ________. Ginkgo biloba induces _______.

A

CYP450, grapefruit juice, small intestine, SYP219A

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52
Q

The level of oxidative enzymes is lower in ____ ______ animals. Liver enzymes systems are not fully
developed until ___ _______ of age

A

very young, 3 months

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53
Q

The ability to synthesize liver enzymes may be impaired in _____ animals thus decrease the capacity to _______.

A

old, metabolize

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54
Q

Malnourished animals cannot synthesize enough ______ enzymes needed for metabolism

A

liver

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55
Q

Many liver diseases such as ________, ______ ______, and ______ inhibit the CYP450s

A

hepatitis, liver cirrhosis, cancer

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56
Q

Hyperthyroidism may increase the _____ of metabolism of drugs while hypothyroidism does the _______

A

rate, opposite

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57
Q

When administering a drug metabolized by the liver, it is wise to anticipate a drug _______ if a second drug also metabolized by the liver is added to therapy.

A

interaction

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58
Q

Induction of drug-metabolizing enzymes should be considered as a ________ mechanism that
facilitates excretion of potentially ______ compounds

A

protective, toxic

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59
Q

Inducers generally act as _______ for the induced enzymes and the induction is ____ dependent

A

substrates, dose

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60
Q

Inducers often induce more than ____ ______.

A

one CYP

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61
Q

Maximal induction generally requires ___ to ___ hours of exposure to a drug. It can return to baseline
___ to ___ hours (depending on dose) after the inducer is discontinued.

A

10, 12, 18, 24

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62
Q

Barbiturates are recognized inducers of ____. _______ is one of the most potent microsomal
enzyme inducers known and can enhance the _________ of other ________ drugs.

A

CYP, Phenobarbital, hepatotoxicity, hepatotoxic

Metabolites can be toxic; if they accumulate in the liver; metabolites go back through first pass metabolism?

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63
Q

Drug interactions that reflect ________ of _____ may be at greater risk of causing serious
adverse events

A

inhibition, enzymes

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64
Q

As with inducers, the extent of inhibition is ?

A

dose dependent

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65
Q

Inhibitors often act as _______ at the inhibited enzyme

A

substrates

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66
Q

Currently, three types of inhibitors have been described: ?

A

reversible, quasireversible and irreversible

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67
Q

________, ______ and ______ _____ drugs are examples of potent enzyme inhibitors

A

Chloramphenicol, cimetidine, imidazole, antifungal

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68
Q

__________ inhibits CYP enzymes including CYP3A4 in dogs

A

Ketoconazole

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69
Q

Drug-induced inhibition of drug metabolism can be used for ?

A

therapeutic benefit

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70
Q

Ketoconazole interferes with the ________ of drugs that are metabolized via _______. It has
been used to ______ blood drug concentrations of _______ in dogs and cats (reduce
dosage/cost).

A

metabolism, CYP3A, increase, cyclosporine

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71
Q

________ has been used to prevent metabolism of acetaminophen in ______ and ______ into potentially lethal toxic metabolites.

A

Cimetidine, humans, cats

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72
Q

Cilastatin inhibits the metabolism of _______ by ________ __ on the brush border of _____ _____ cells.

A

imipenem, dehydropeptidase, I, renal tubular

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73
Q

Renal excretion is the most important route of drug ________ for both ______ (especially _____
soluble) drugs and their ______.

A

elimination, parent, water, metabolittes

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74
Q

The kidney has been the most widely studied excretory organ because of the accessibility of ____
to collection and analysis.

A

urine

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75
Q

Host factors that determine renal excretion include

A
  • Renal blood flow (glomerular filtration)
  • Active tubular secretion
  • Tubular (generally passive) reabsorption
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76
Q

Total renal excretion of a drug = ?

A

𝑹𝒂𝒕𝒆 𝒐𝒇 𝒇𝒊𝒍𝒕𝒓𝒂𝒕𝒊𝒐𝒏
+ Secretion - reabsorption

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77
Q
A
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78
Q

The glomerular filtration is a ______ process. Drugs enter the glomerulus from the _____ by ____ flow. Too large drugs (> ______ MW) are excluded as occurs for _____-bound drug if the glomerulus is _______.

A

passive, blood, bulk, 60,000, protein, healthy

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79
Q
A
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80
Q

Active transport of drugs in the ______ tubules is a very efficient and rapid process. It is susceptible
to _______ between drugs. Separate ______ transport systems exist for acid, basic, and neutral
drugs (________,________,_______). It is not limited by _____ binding.

A

proximal, competition, active, p-glycoprotein, OATPs, POTs, protein

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81
Q

The transport systems across tubule cells involves _____ _________ _____ of transport proteins. One set is located in the _____ _____ and the other is located in the ________ _______.

A

two, separate, pairs, brush, border, basolateral membrane

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82
Q

There are two distinct secretory pathways in the later sections of the _______ renal tubule: one for _______ (?) and one for ____ compounds (?)

A

proximal, acidic, organic anion transporter/OAT, basic, organic cation transporter/OCT

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83
Q

The primary orientation of this system is from _____ to tubular _____, ______ drugs and/or metabolite _______ from the _____.

A

blood, filtrate, removing, conjugates, blood

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84
Q
A
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85
Q

Many drugs compete for the same ______ _______ sites, leading to drug interactions. This interaction has been studied with the ______ ____ transport system.

A

tubular transport, organic acid

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86
Q

Weak acids such as ________ or __________ will inhibit secretion of the _____ ______ penicillin, thereby prolonging the ______ concentration of penicillin.

A

probenecid, phenylbutazone, weak acid, blood

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87
Q

Do we need to know this slide?

A
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88
Q

Reabsorption of drugs from renal _____ into ______ capillaries slows renal ______.

A

tubules, peritubular, excretion

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89
Q

The drug reabsorption depends on its ?

A

lipid solubility and its ionization

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90
Q

______ _____ drugs are more likely to be reabsorbed in _____ urine but are trapped and
excreted in ______ urine

A

Weakly acidic, acidic, alkaline

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91
Q

A brisk, alkaline diuresis is induced to decrease ________ _______ into the blood and ________ excretion into the ____

A

salicylate reabsorption, accelerate, urine

92
Q

Difference in pH can have a major influence on the ____ of renal excretion

A

rate

93
Q

Carnivores tend to have a more _____ urine (pH ?) than herbivores (pH ?).

A

acidic, 5.5-7.0, 7.0-8.0

94
Q

A weakly acidic drug will have a _______ renal excretion

A

higher, Herbivores > carnivores

95
Q

A weakly basic drug will have a _______ renal excretion

A

higher, Carnivores > herbivores

96
Q

In healthy animals, small changes in urinary pH or urinary flow rate do not significantly contribute
to ?.

A

altered drug clearance

97
Q

Urinary pH can be therapeutically altered such that the renal _______ ___ of a drug can be modified ( _______ or _____).

A

excretion rate, overdose, toxicity

98
Q

Because phenobarbital is ______, ________ the
urine increases clearance about _____ fold.

A

acidic, alkalinizing, five

99
Q
A
100
Q

Drugs excreted in the urine that do not undergo _______ reabsorption will be _________
concentrated in the renal tubule

A

passive, progressively

101
Q

_______ cells may be exposed to higher concentrations of drugs, which may increase the risk of ________.

A

Tubular, nephrotoxicity

102
Q

Drug concentration in the urine can be of therapeutic benefit in some situations such _______ ______.

A

bacterial cystitis

103
Q

At ____ urine flow rates, there is greater opportunity for ______ of drug from the _____ tubular fluid back into the _____.

A

low, diffusion, distal, blood

104
Q

Diffusion is facilitated by the _____ concentration of drug in the ______ fluid

A

high, tubular

105
Q

Polar compounds having ____ _____ solubility (such as many drug _______) are not ______ since they cannot cross the ____ ______.

A

low lipid, metabolites, reabsorbed, lipid membrane

106
Q

Active reabsorption systems are also present in order to act on a drug already present in the _______ load and recover ______ _____ (e.g., _______)

A

filtered, essential nutrients, glucose

107
Q

Some drugs reach their target sites by the mechanism of active reabsorption, making their ____ more important for predicting ______ than their _____ concentration. Example: ?

A

TFC, activity, blood, the diuretic
furosemide

TFC = tubular fluid concentration

108
Q

Furosemide is first secreted by the _______ into tubular ____ and than is actively _____
back into _____ cells to gain access to its receptors for activity.

A

tubules, fluid, reabsorbed, tubular

109
Q
A
110
Q

Most of the Phase I and Phase II enzymatic systems present in the liver also exist in the ______.
Oxidative processes generally occur within the _____ _____ cells.

A

kidney, proximal tubule

111
Q

In the case of renal drug biotransformation, what two scenarios might occur?

A
  • A drug is solely metabolized by the kidney and not the liver
  • The kidney metabolizes a drug already biotransformed by the liver, relay metabolism
112
Q

Morphine and acetaminophen are also metabolized by the _____

A

kidney

113
Q

The ultimate route for drug elimination from the body is the _______.

A

kidney

114
Q

Drugs can also be eliminated in ? (7)
What is the significance, if any, of these elimination sites?

A

bile, milk, saliva, expired air, feces, sweat, and tears

For most therapeutic drugs these routes are generally not quantitatively important for reducing total body burden of drug.

115
Q

Biliary excretion is very _____ and much ____ clinically important

A

slow, less

116
Q

What factors determine biliary excretion?

A

Chemical structure, polarity, and MW of drugs (drugs > 600 MW in size) determine this excretion.

117
Q

Drugs excreted in the bile are in big contact with the ?

A

intestine and its flora

118
Q

The contact with intestine is more likely to cause ?

A

adverse reactions in the GI-tract

119
Q

Conjugated (Phase II) drugs excreted by ______ excretion may undergo enterohepatic circulation

A

biliary

120
Q

Intestinal bacteria ________ the drug or metabolite, allowing _______ absorption to occur

A

unconjugate, intestinal

121
Q

Enterohepatic circulation can prolong the _________ ____-_____ of a drug

A

elimination half-life

122
Q

After ______ or ______ administration the drug is
conjugated in the liver and eliminated in the bile

A

oral, parenteral

123
Q

Degradation results in ________ of drug, which can then be ________.

A

deconjugation, reabsorbed

124
Q
A
125
Q

Drugs enter the saliva by ______ diffusion from the ______.

A

passive, blood

126
Q

Salivary excretion is important in _______ receiving ______ antimicrobial drugs.

A

herbivores, parenteral

127
Q

Copious salivation by _____ and _____ and the swallowing of antimicrobial-drug-laden saliva
may upset the _______ process in the rumen.

A

cattle, sheep, digestive

128
Q

The expired air route of excretion is primarily important for ______ drugs including ____ ______ drugs

A

volatile, gas anesthetic

129
Q

True or False: Excretion via milk IS a major route of drug excretion.

A

False. Excretion via milk is not a major route of drug excretion.

130
Q

Drug excretion via milk is important if the milk is to be used for human ________ (requiring a _______ period).

A

consumption, withdrawal

131
Q

_______ ____ drugs will tend not to distribute into the milk after systemic distribution.
(e.g., penicillin), while weakly basic drugs will (e.g., erythromycin)

A

Weakly acidic

132
Q

Plasma pH = ___; Milk pH = ______

A

7.4, 6.5-6.8

133
Q

Drugs that are _____ absorbed after ____ administration or drugs that are secreted _______ into the intestine or into ___ are excreted in the ______

A

not, oral, directly, bile, feces

134
Q

What are the minor routes of excretion?

A

Tears and sweat

135
Q
A
136
Q

The combined effects of hepatic _______ and ______ and ______ excretion, as well as other routes of elimination irreversibly clear the drug from the body.

A

metabolism, renal, biliary,

137
Q

Pediatric generally refers to the first __ weeks of life.

A

12

138
Q

Drug disposition in the pediatric animal: At what age is an animal considered to be a neonate?

A

0-2 weeks

139
Q

Drug disposition in the pediatric animal:

What age range is an animal considered to be an Infant?

A

(> 2 to 6 weeks)

140
Q

Drug disposition in the pediatric animal:

What age range is an animal considered to be Pediatric?

A

> 6-12 weeks

141
Q

Pediatric patients exhibit:

  1. Decreased hepatic ______ capacity
  2. Immature ______ function
  3. Decreased _____ and renal _______
A

metabolic, biliary, GFR, clearance

142
Q

Drug _________ , including both ____ metabolism and ______ excretion is limited in _______ and ______ patients

A

elimination, hepatic, renal, neonatal, pediatric

143
Q

Many drugs administered to the young animal are characterized by _______ _____ clearance (until __ to _____), and _____ half-life

A

decreased renal, 2, 3, months, longer

144
Q

In pediatric patients, hepatic metabolism of drugs is ______. Both phase I and II reactions are _______.

A

deficient, reduced

145
Q

Although glomerular filtration and renal tubular function progressively _________ , adult values may not be reached until approximately ___ _____ of age

A

increase, 2.5, months

146
Q

Renal tubular reabsorption in ______ appears to be similar to that in _____ as long as body ______ and _______ are maintained

A

puppies, adults, fluids, electrolytes

147
Q

Clearance is a pharmacokinetic parameter describing drug ________

A

elimination

148
Q

Clearance is defined as the volume of _____ which contains the ____ amount of drug that is _______ from the body in ____ time

A

plasma, total, removed, unit

149
Q

Clearance is expressed as ?

A

volume per unit time, e. g., mL/min or L/h

150
Q

Cleareance is often used to assess the ?

A

excretory capacity of an organ (kidney)

151
Q

Renal clearance (Clrenal)is defined as the volume of ______ containing the amount of drug that is _______ from the body by the ______ in ____ time

A

plasma, removed, kidneys, unit

152
Q

What is the CLrenal formula?

A
153
Q

Usually ____ and ____ clearance are the most important.

A

renal, hepatic

154
Q

The _______ clearance of a drug or ____ ____ clearance (CLtotal) is the ____ of clearance ____ for each mechanism involved in ______ the drug

A

overall, total body, sum, rates, eliminating

155
Q

Cl other means what?

A

Other forms of excretion

156
Q

Clearance is used to determine the rate of ?

A

drug elimination

157
Q

Clearance is the _________ ______ to determine the rate of drug elimination

A

proportionality factor

Why? B/c if clearance is high rate of elimination is high.

158
Q

Clearance does not describe the ______ of drug being eliminated

A

amount

159
Q
A
160
Q

Rate of drug elimination is the _______ of drug being _____ per ____ time

A

amount, eliminated, unit

How much drug is being eliminated in the body

161
Q

The overall clearance CLtotal can also be estimated by measuring _____ concentrations at ______ following a ____ _____ bolus dose (Q mg)

A

plasma, intervals, single, intravenous

162
Q
A
163
Q

AUC0 −∞ is the area under the full curve relating Cp to time following a bolus dose given at time t = 0

A
164
Q

AUC0 −∞ provides an integrated measure of _______ exposure to the drug in units of time _______ by drug concentration

A

tissue, multiplied

165
Q

Drug clearance can also be determined in an individual subject by measuring the ______ concentration of the drug ( mg/L) at intervals during a _____-rate ______ infusion (X mg of drug per hour)

A

plasma, constant, intravenous

166
Q
A
167
Q
A
168
Q

Css is the plasma drug concentration at a _____ ____.

A

steady state

169
Q

Knowing the clearance enables one to calculate the _____ ____ needed to achieve a desired _____-_____ (“target”) _____ concentration.

A

dose rate, steady-state, plasma

170
Q

During a constant intravenous infusion at rate X mg/h, the plasma concentration _______ from ____ to a _____-state value (____); when the infusion is _____, ___ declines to zero

A

increases, zero, steady, Css, stopped, C

171
Q
A

Constant intravenous infusion

172
Q

Following an intravenous bolus dose (Q mg), the plasma concentration rises _____ and then declines towards _____

A

abruptly, zero

173
Q
A

IV bolus

174
Q
A

Data from panel (B) plotted with plasma concentration on a logarithminc scale. The straight line shows that concentration declines exponentially

175
Q

Elimination T½ refers to the _______ of drug from plasma.

A

disappearance

176
Q

Elimination half-life (T½) is _____ relevant and the most often reported _______ parameter

A

clinically, pharmacokinetic

177
Q

Elimination T½ is defined as the _____ necessary for _____ or ____ concentrations to ______ by 50%

A

time, plasma, blood, decline

178
Q

For example, at one drug half-life, 50% of the dose has been eliminated; after five T ½s (half-lives) 97% of the drug has been eliminated

A
179
Q

The more rapidly a drug is cleared by an organ, the ______ the drug half-life

A

shorter

180
Q

The longer the half-life, the _____ the drug will persist in the body

A

longer

181
Q

Any factor that changes the ___ of a drug will affect its half-life

A

Vd

182
Q

An increases of ___ can increase the half-life and _____ the duration of action of the drug

A

Vd, extend

If the Vd is low? the plasma concentration is high.

Vd means?

High Vd = ?

183
Q

Elimination half-life along with the dosing interval also determines the _____ of drug that _____ with each dose as _____-state equilibrium is reached

A

amount, accumulates, steady

184
Q

Along with the ______ range, the ____-___ should be the basis for an appropriate dosing interval

A

therapeutic, half-life

185
Q

Half-life (T½) of a drug is increased by:

A
  • Decreased renal or hepatic blood flow: Hemorrhage, heart failure, cardiogenic shock
  • Decreased renal function
  • Decreased metabolism: Another drug inhibits its biotransformation, hepatic insufficiency; How?
186
Q

Half-life (T½) of a drug is decreased by:

A
  • Increased hepatic blood flow
  • Decreased protein binding. Why? Protein binding stops capacity of drugs to go to the tissues.
  • Increased metabolism
187
Q

Anything that changes the _____ of ______ of a drug will affect its half-life (T½)

A

volume, distribution

188
Q

Many drugs exhibit ___-order kinetics

A

first

189
Q

The most common, note if elimination mechanisms become ______, elimination becomes ___-order

A

saturated, zero

190
Q

If a drug half life is 2h, how long does it take the body to completely eliminate the drug?

A

After first half life, 50%, second = 25, after 5 = 97%

Ever 2 hours, 50% of the drug is eliminated.

191
Q

The volume of blood cleared per unit time by an organ is _______ of PDC

A

independent

192
Q

In first order elimination, the ____ volume of blood will be irreversibly cleared of drug by an organ regardless of how much drug is in the blood.

A

same

193
Q

In first order elimination, a _____ _____ is eliminated per unit time. ___% of drug per hour. The half-life (T½) of a drug will be constant regardless of ___ ______

A

constant, fraction, 50, drug concentration

194
Q

The first half life is the same as the second in time in the case of first order elimination

A
195
Q

______-order elimination is less common.

A

Zero

196
Q

Zero-order elimination only occurs when so much drug is present in the blood that the organ of clearance becomes ______

A

saturated

197
Q

Zero-order elimination occurs when there is ______ amount of enzyme and ____ ____ of the drug.

A

limited, too much

198
Q

The rate of elimination of a drug from the plasma is _____ regardless of the _____ _____ of the drug.

A

constant, plasma concentration

199
Q

In zero-order elimination, the ___-__ is not meaningful. It is ___ constant and varies with the amount of the _____ ______.

A

half-life, not, drug concentration

200
Q
A

Half life is always constant in first order elimination

201
Q

In the case of ethanol, the time course of disappearance of drug from the _____ is eliminated by ____-order elimination.

A

plasma, zero

202
Q

The rate of elimination of ethanol from the plasma is ______, regardless of ___ or of _____ concentration of ethanol

A

constant, dose, plasma

203
Q
A

Half life is not constant in zero order elimination

Rate of elimination is constant

204
Q

Pharmacokinetics provides a framework for understanding _____ ______ ____ when given to an animal or human, ___ ____ ___ ___ ___, and how quickly, that enables one to understand the effects that it produces

A

what happens to a drug, where it goes in the body

205
Q

In practice, pharmacokinetics usually focuses on ?

A

concentration of drug in blood plasma

206
Q

Plasma concentrations are used in routine clinical practice to ?

A

individualize dosages

207
Q

To achieve the desired therapeutic effect while minimizing adverse effects in each individual patient- an approach that known as ? can be used

A

therapeutic drug monitoring, TDM

208
Q

___-_________ is used to predict the behavior of a drug in the body

A

PK-modeling

209
Q

Generally the drug of interest is given at the desire route of administration as a ____ dose

A

single

210
Q

Drug concentrations (samples) are collected _____ _____, preferably for at least ______ elimination half-lifes to ensure that all phases of drug _______ are identified

A

over time, three, movement

211
Q

For bioavailability studies, the drug should be given ______ (100%) as well as by the route of ____

A

intravenously, interest

212
Q

The most common described in the veterinary literature are either ?

A

compartmental or noncompartmental analysis

213
Q

The body is considered as consisting of a _____ ______ compartment. That is, the entire dose X of drug is assumed to move ___ of the body at a ____ rate

A

single homogenous, out, single

214
Q

The Single- or one compartment model is applicable if the _____ concentration falls ________ after drug administration.

A

plasma, exponentially

215
Q
A

After drug administration, drug is absorbed, and then in one single compartment our whole drug. After that there is constant excretions and metabolism

216
Q

The two-compartment model introduces a ______ _____ compartment to represent the _____, in communication with the _____ _____ compartment.

A

separate, peripheral, tissues, central plasma

217
Q

The two compartment model more closely resembles?

A

The real life process

218
Q

The two compartment model is a widely used approximation in which the _____ are lumped together as a _____ compartment

A

tissues, peripheral

219
Q

In the two-compartment model, drug molecules can ____ and ____ the peripheral compartment only via the ____ compartment

A

enter, leave, central

220
Q

Distribution rate constant (____) out of the ____ compartment

A

K12, central

Goes to the peripheral compartment

221
Q

Redistribution rate constant (____) from the _____ back into the ____ compartment

A

K21, peripheral, central

We need to it to goto central compartment again to be excreted and metabolised.

222
Q
A
223
Q

The multi-compartmental model is generally employed when experiments are conducted over ____ times frames.

A

long

224
Q

The multi-compartmental model may be used if the goal of a study is to to describe the tissue _____ of a drug in a ____ _____ animal

A

residue, food producing

225
Q

These compartments have specific equations to calculate clearance

A
226
Q
A
227
Q

Protein-bound drugs can be secreted by _____ tubular secretion, but can not be eliminated by _____ _____.

Passive reabsorption- ___ solubility matters

____ is not a root of excretion

A

active, renal glomerulus, lipid, fat

Intro to Pharmacology (31 decks)

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