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Pharmacology and Toxicology > Drug properties > Flashcards

Drug properties Flashcards

1
Q

What must happen in order for a drug to reach its target

A

It will need to be absorbed and distributed

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2
Q

What must happen for the effect of the drug to be stopped?

A

Metabolized and Excreted

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3
Q

Fill in the blanks.
In order for a drug to have a biological effect, it must be soluble in _______ and cross the ______

A

bodily fluids and cell membranes

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4
Q

What determines if a drug will be able to cross the cell barrier?

A
  1. The physiochemical properties
  2. molecular size
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5
Q

What is the ideal size of a drug for it to be able to cross barrier, if taken PO?

A

200-500 DA

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6
Q

Why do proteins such as insulin need to be ingested to express its desired effect

A

Due to the molecular size being so large, it won’t be able to reach its target size as easily due to the likelihood of being digested.

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7
Q

What types of compounds would dissolve in lipid solutions?

A

Hydrophobic/lipophilic compounds

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8
Q

T/F. Ionic/ Polar compounds are lipophilic.

A

False they are not
- to be lipophilic means to be able to pass the cell membranes and only uncharged/unionized compounds will be able to pass.
- They are hydrophilic, this hydrogen casing makes it easy for them to dissolve in water due to H bonds

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9
Q

Bioaccumulations

A

This is when the drug get stuck to reservoirs/ lipid compartments

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10
Q

Are drugs either hydrophilic or lipophilic

A

They are both, making them amphipathic because they not only need to be able to pass through body fluids they also need to make it through cell membranes to get to their target site

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11
Q

What is significant about drugs having non-polar and polar groups in connection to its solubility?

A

The combination of the two properties will determine its solubility

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12
Q

How do you measure solubility?

A

The partition co-efficient (Pow/Kow)

con. drug dissolved in octane/ con.drug dissolved in water

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13
Q

What does a high Pow level signify?

A

this means that the drug has good permeability across the membrane

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14
Q

What is the log P range for drug-like properties

A

0.5-5

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15
Q

Why is solubility reduced for molecules with a log P value bigger than 5?

A

Because there is less ability for solubility across water and a drug must first cross the aqueous membrane before reaching the lipid membrane

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16
Q

What is Lipinski’s Rule of 5?

A
  • mol. size between 200-500
  • log p value of <5
  • hydrogen acceptor <10
  • hydrogen donors <5
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17
Q

What is another way to determine whether a drug is permeable?

A

The TPSA (topical polar surface area)
a TPSA of >140 is usually poor at permeability

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18
Q

T/F. Drugs are usually weak acids or bases.

A

True

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19
Q

Why does a drug’s ionization depend on the pH of the surrounding medium?

A

The protonization/deprotonization of compound

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20
Q

Which form of a drug will readily diffuse?

A

unionized

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21
Q

What determines if a drug is more likely to be ionized or not?

A
  1. pH of compartment
  2. pka of the drug
  3. acid/base
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22
Q

When will an acid drug ionze

A

at a high pH and low [H] by losing a proton

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23
Q

At a high pH will the reaction shift left or right for an acid?

A

shift to the right to produce more [H] because in this state more of the drug is deprotonated and ionized

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24
Q

What happens if a compartment has a high pH and low [H] for a base?

A

it will be unionized and become more soluble

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25
Q

What happens if a compartment has a low pH and high [H] for both acids and bases?

A

Acids:
unionized/more soluble

Bases:
ionized/less soluble

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26
Q

T/F. For a high pH, low[H], the drug will be deprotonated.

A

True

27
Q

State the rules for an acid and base to be more or less lipid soluble and its pka and compartment’s pH

A

Acids:

pH> pka, less lipid soluble (the compound will be charged)

Bases:
pH>pka, more lipid soluble (the molecule is neutral)

28
Q

What is the significance of pka for a drug’s solubility?

A

pka is the point at which the protonated and deprotonated fractions are equal

29
Q

How can you use protonation to see if a drug will be soluble?

A

the protonated form of a weak acid is neutral and
will be more lipid soluble

The unprotonated form of a weak base is neutral and will be more lipid soluble

30
Q

What different things do ionization effect when it comes to drug action in the body?

A

solubility and absorption
elimination of the drug
the binding

31
Q

pH of blood

A

7.4

32
Q

pH urine

A

5-8

33
Q

pH of intestines

A

7.5-8

34
Q

pH of stomach

A

1.92-2.59

35
Q

pH of prostatic secretion

A

6.45-7.4

36
Q

pH of vaginal secretion

A

3.4-4.2

37
Q

What are barriers to drug movement in the body

A

1.cell membranes
2. transport systems that carry drugs around the body but cause the drug con to decrease

38
Q

Partition Coefficient

A

measures drug solubility so very useful for determining permeation

39
Q

T/F. a higher partition coefficient means higher permeability

A

true

40
Q

Fill in the blank.
Epithelial cells are joined by ____

A

tight junctions/occluding zonulae

41
Q

Endothelial Cells

A

These are cells that line blood vessels and capillaries with occluding zonula, aka blood brain barriers

42
Q

Blood brain barrier

A

brain capillaries that are joined by endothelial cells with tight junctions . There are few passages but there are some exceptions

43
Q

What are the exceptions to the blood brain barrier transient passages?

A

There are drug passages to the brain such as pineal, pituitary, median eminence

44
Q

Median eminence

A

This is where we measure toxins

45
Q

Why is the blood brain barrier an issue in drug targeting?

A

because most compounds do not have entry to the CNS due to the BBB

46
Q

Basolateral Enterocyte Transport location

A

This means that drug will move from the intestine to the blood

47
Q

Apical Enterocyte Transport location

A

proceed to lumen from the intestine

48
Q

Hepatocyte sinusoidal transport

A

liver to blood

49
Q

Hepatocyte canicular transport

A

liver to lumen/bile

50
Q

basolateral renal tubular transport

A

kidney to blood

51
Q

apical renal tubular transport

A

kidney to lumen

52
Q

abluminal brain capillary endothelial cells

A

goes to the brain

53
Q

luminal brain capillary endothelial cells

A

goes to brain capillary

54
Q

Organic anion transporters substrates

A

cAMP, cGMP, folate, urate

55
Q

Organic cation transporters

A

mainlyion basolateral membrane

56
Q

Organic cation transporters

A

dopamine serotonin, histamine

57
Q

novel organic cation transporter location

A

cell apical membrane

58
Q

Organic anion transporting polypeptides substrates

A

bile salts, thyroid hormones, estrogen

59
Q

ATP binding cassette

A

substrates undergo primary active transport

60
Q

Why are ABC transporters important?

A

They limit cellular exposure to drugs and toxins

61
Q

Multidrug resistance binding and structure

A
  1. the substrate will bind to the p-qp drug binding key
  2. two ATP will hydrolysis to ADP creating a conformation change
  3. The substrate will be released into extracellular environment
62
Q

P-gp direction

A

It will favour taking things to the blood, feces mucus, or urine

63
Q

What leads to multi drug resistance

A

ABC transporters with broad substrate specificity affect multi drug resistance because they pump these drugs out of the body.

64
Q
A

Pharmacology and Toxicology (18 decks)

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