Quiz Flashcards

1
Q

What breed of dog is particularly sensitive to the cardiovascular effects of the phenothiazine sedative, acepromazine?

A

Boxers

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2
Q

A dog with GI disease is on antiacid therapy which raises his stomach pH. This dog is inadvertenly exposed to a toxin that requires a very acidic environment to be absorbed, but because of the antacid the dog absorbs very little of the toxin. What is the best description of this drug-drug interaction?

A

Pharmacokinetic antagonism- because it is affected the absorption

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3
Q

The antibiotic chloramphenicol is known to cause aplastic anemia(complete shutdown of RBC production) that has a 50% mortality rate. This reaction occurs in about 1:524,000 people. It is an unpredictable response and does not require previous exposure to the drug. What best describes this type of reaction

A

Idiosyncratic reaction

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4
Q

Which form of cellular transport directly utilizes ATP?

A

Primary active transport

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5
Q

Define Drug disposition

A

the study of the movement of drugs across biological membranes in the body from the time of absorption until elimination. Can be broken down into four stages called the ADME process. The time in the body until the time it leaves

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6
Q

Passive Diffussion

A

Movement with a concentration gradient; can be paracelluar or via specialized intercellular junctions

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7
Q

Ionization

A

The pka of a weak acid or base determines in what pH the substance will be ionized

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8
Q

When the pKa= pH

A

the drug is 50% ionized and 50% non-ionized

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9
Q

Acidic drugs are ionized in _______, while basic drugs are ionized in_____

A

Acidic drugs are ionized in basic environments, while basic drugs are ionized in acidic environments

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10
Q

What determines ionization?

A
  1. Acid or base 2. pKa 3. environment of drug
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11
Q

Formula for pKa of an acidic drug

A

pka= pH + log [AH- non-ionized]/ [A-ionized]

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12
Q

Formula for pKa of a basic drug

A

pka= pH + log [BH+ionized]/ [B non-ionized]

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13
Q

Ion-trapping

A

Because of the properties of ionization a drug will be more likely to cross membranes from a certain pH environment, but it then may ionize and be unable to cross back over the membrane

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14
Q

Weak acids are absorbed from an acidic environment and will become trapped in a ______ environment.

A

basic

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15
Q

Weak bases are absorbed from a basic environment and will become trapped in a more _______ enviroment.

A

Acidic

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16
Q

Faciliatated diffusion

A

This is a carrier mediated form of transport to move substances across lipid membranes. THIS IS SATURABLE!
This moves with passive diffusion and does NOT require energy to work.

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17
Q

Active Transport

A

Carrier mediated(like facilitated diffusion) and it can also be saturated. It is also selective, meaning that only certain molecules can be moved by a specific transporter) Substances are being moved AGAINST the concentration gradient, thus it REQUIRES ENGERY

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18
Q

Primary active transport

A

A form of active transport that requires that energy is supplied directly i.e. Na/ K ATPase

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19
Q

secondary active transport

A

A form of active transport where the energy is supplied indirectly i.e. ATP is used to make an electrochemical gradient and this is used to move substances

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20
Q

antiporter

A

A type of transport where one substance is exchanged for another

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21
Q

symporter

A

A type of transport where two substances are brought into the cell together

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22
Q

P-glycoprotein system

A

This is a specific form of active transport in which the transporter is an efflux pump. This protein expresses ABCB-1(MDR 1 gene) and will remove substances from specific cells.

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23
Q

Efflux Pump

A

before the drugs can move through the cell, it moves to the other side of the membrane. This is a form of ACTIVE TRANSPORT. i.e. BBB- keeps drugs out- however, ivermectin in collies messes with this

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24
Q

pinocytosis

A

A specific type of endocytosis. Drugs bind to the surface of the cell, then the cell membrane invaginates and interiorizes the drug. REQUIRES ENGERY
i.e. aminoglycosides being taken up this way by renal tubular cells

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25
Q

Absorption

A

Movement of the drug from the site of admin. into the blood- Remember, there is no absorption for IV drugs!

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26
Q

Dissolution

A

the first part of absorption and can actually be the rate limiting step. Once dissolution has occurred, then the real absorption can start to take place

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27
Q

Solubility of a drug

A

Determined by it’s molecular structure, ionization, and preparation.

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28
Q

Fastest-slowest routes of administration

A

IV> sublingual/inhaled/IP>IM>SC>PO

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29
Q

What are some factors related to the drug that can influence absorption?

A
  • Molecular size of the drug
  • rate of dissolution
  • degree of ionization
  • concentration at absorptive site( higher concentration= more absorption)
  • Route of adminstration
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30
Q

What are some factors related to the animal that can influence absorption?

A
  • blood flow ( more blood flow= more absorption)
  • Absorbing surface area( more surface area= more absorption)
  • presence of connective/scar tissue
  • species
  • fasted vs fed
  • indiviudal variation
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31
Q

Bioavailability

A

The fraction of a given dose that ends up in systemic circulation. IV administration is considered to represent 100% bioavailability (F=1). Topical drugs generally mean that they do not enter systemic circulation

32
Q

enteral

A

anything that goes into the alimentary canal- usually oral

33
Q

Enterohepatic Recycling

A

Where a drug is absorbed into portal circulation, metabolized and excreted into bile, then reabsorbed into the SI again- Drugs that do this generally have longer half lives

34
Q

First-Pass Metabolism

A

where an oral drug(also rectal) is absorbed into portal circulation and a portion of that drug is metabolized by the liver before it reaches systemic circulation. A drug that undergoes first pass metabolism will have lower bioavailability

35
Q

Most absorption takes place in ___________

A

in the small intestine- where there is large SA, rich blood supply, and presence of microorganism

36
Q

Parenteral

A

IV, IM, SC, and IP; Generally the barrier to absorption via these routes is less than with oral and topical use and so drug levels are expected to get into systemic circulation faster.

37
Q

Drug that has a high first pass metabolism

A

Propanoal if given orally. Thus, the oral dose will be much higher than the injectable

38
Q

Distribution of drugs

A

The transfer of drugs from the bloodstream to tissues around the body

39
Q

Compartments

A

Groups of tissues/fluids for which the rate of update/clearance of drugs are simliar

40
Q

Volume of distribution

A

what compartments a drug is being distributed.

41
Q

Tissue Barriers

A

Specialized barriers exist between the blood stream and certain organs, these often make use of tight junctions between cells and selective transport mechanisms to regulate movements of substances into and out of the organ/tissue

42
Q

Blood Brain Barrier

A
  1. tight junctions between the capilaries endothelial cells and glial cells
  2. Active Transport Mechanisms
  3. Constant CSF production/drainage
    Remember if it crosses the BBB, then it also crosses the placenta.
43
Q

Acidic drugs bind to________

A

albumin

44
Q

Basic drugs bind to________

A

several proteins (B-globulins and glycoprotein and sometimes a little bit to albumin)

45
Q

Free drugs( non-bound)

A

are ACTIVE

46
Q

Metabolism

A

the chemical alteration of the drug by different body tissues aka biotransformation

47
Q

Bioinactivation

A

the process of making a drug inactive and easier to excrete

48
Q

Bioactivation

A

when an inactive substance (prodrug) is converted to an active metabolite i.e. cefpodoximine proxayil to cefpodoximine

49
Q

Lethal Synthesis

A

non-toxic substance can be converted to a toxic

metabolite i.e. acetaminophen to n acetol benzaoquinoimine

50
Q

Main site of metabolism

A

LIVER

51
Q

Why do we see Tyenol toxicity in cats?

A

cats are deficient in glycuroyl transferase which alters their metabolism of some drugs

52
Q

Boxers are senisitve to…

A

phenothiamzines(acepromazine)

53
Q

Collies are sensitive to

A

Ivermectin- causes CNS depression

54
Q

Australian terriers respond differently

A

to droperidol/fentanylp they exhibit little sedation

55
Q

Young animals have

A

lower metabolism, lower rate of excretion, increased permeabiity of the BBB

56
Q

Specific Effects to young animals

A
  1. tetracylines affecting tooth enamel
  2. Fluroquinolones affecting cartilage
  3. Glucocorticoids affecting bone physes
57
Q

Geriatric Animals will have….

A

decreased metabolism, decreased excretion,

58
Q

Hypersentivity VS Idosyncratic

A

Idiosyncratic reactions- NOT DOSE DEPENDENT and can occur on the first exposure where as hypersentivity occurs on second exposure

59
Q

Tolerance

A

diminished response over time to a drug

60
Q

tachyphylaxis

A

acute tolerance

61
Q

Phase 1

A

includes oxidative( most common), reductive, and hydrolytic reactions( rare). Most of these take place in hepatocytes and are catalyzed by enzymes attached to the Smooth ER- most imporant cytochrome P450

62
Q

Phase 2

A

a molecule with a reactive group conjugates with a substiutent group rendering a final metabolite that is typically inactive and water soluble (polar)

63
Q

Glucuronidation

A

most common reaction and IS the ONLY microsomal- cats are deficent in this- PHASE 2 rxn

64
Q

Enzyme Induction

A

drugs that increase the capacity of microsomal enzymes
can lead to tolerance. drugs are metabolized quicker, but prodrugs might stay around longer This can enhance toxin reactions. Examples Pheno, phenylbutazone, griseofulvin, and rifampin; enhances bioactivation

65
Q

Enzyme inhibition

A

will result in a longer half life of the drug, slows down bioactivation

66
Q

excretion

A

removal of the drug from the body; KIDNEY

67
Q

Renal excretion

A
  1. glomerular filtration
  2. active tubular secretion
  3. tubular reabsorption
68
Q

Acidification of urine will cause

A

Acidification of urine with ammonium chloride or methionine will cause weak basic drugs to be ionized and enhance their excretion.

69
Q

Alkaliniziation of urine

A

Alkalinization of urine with sodium bicarb or potassium citrate will cause weak acids to be ionized and enhance their excretion.

70
Q

Hepatic Excrection

A

typically an active transport of drugs and conjugates from the hepatic sinusoids to the bile canaliculi

71
Q

Summation

A

Two drugs with additive effects

72
Q

synergism

A

two drugs have greater efficacy when combined

73
Q

Anatagonism

A

decreased effects occur when one or both drug reduces the action of the other

74
Q

chemical anatgonism

A

drugs chemically react to each other causing inactivation of one or the other

75
Q

physiologic antagonism

A

the drugs work differently and have OPPOSING physiological effects that cancel each other out

76
Q

Pharmacokinetic antagonism

A

one drug reduces the concentration of the other drug at its site of action by interfering with its ADME processes