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Pharma > Lec 7 > Flashcards

Lec 7 Flashcards

1
Q

The process by which a drug reversibly leaves the bloodstream and enters the interstitium (extracellular fluid) and the tissues know as ?

A

Drug distribution

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2
Q

For drugs administered IV, absorption is not a factor, and the initial phase (from immediately after administration through the rapid fall in concentration) represents the distribution phase . (T/F) ?

A

True

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3
Q

during distribution phase , the drug slowly leaves the circulation and enters the tissues . (T/F) ?

A

F—>(rapidly) ?

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4
Q

Mention the factors that affecting distribution :

A

1- Blood flow
2- Capillary permeability
3- Binding of drugs to plasma proteins and tissues
4- Lipophilicity

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5
Q

Give me the descending order of the organelles in terms of the availability of blood and blood vessels in them :

A

(brain, liver, and kidney) > skeletal muscles > Adipose tissue, skin and viscera

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6
Q

Capillary permeability is determined by ?

A
  1. Capillary Structure
  2. Chemical nature of the drug .
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7
Q

Capillary structure varies in terms of the …………… exposed by …………. between endothelial cells.

A
  1. fraction of the basement membrane
  2. slit junctions
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8
Q

significant portion of the basement membrane is exposed due to ……….. through which ( large / small ) plasma proteins can pass .

A

A. large discontinuous capillaries
B. Large

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9
Q

In the brain, the capillary structure is discontinuous , and there are slit junctions . (T/F) ?

A

F —> ( The capillary structure is continuous, and there are no slit junctions )

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10
Q

The capillary structure is continuous, and there are no slit junctions .
So how drugs will passes ?

A

Drugs must pass through the endothelial cells of the CNS capillaries or be actively transported .

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11
Q

Give me example about drug can pass into the brain by specific transporter carries :

A

Levodopa

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12
Q

Reversible binding to ………….. sequesters drugs in a non-diffusible form and slows their transfer out of the vascular compartment

A

Plasma proteins
——————————
sequesters—> (يعزل)

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13
Q

The major drug-binding protein and may act as a drug reservoir is called ?

A

Albumin

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14
Q

lipid-soluble drugs readily penetrate the CNS because they dissolve in the endothelial cell membrane.
(T/F) ?

A

True

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15
Q

Ionized or polar drugs generally success to enter the CNS because they can pass through the endothelial cells that have no slit junctions . (T/F) ?

A

F—> (Ionized or polar drugs generally fail to enter the CNS because they cannot pass through the endothelial cells that have no slit junctions)

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16
Q

The albumin act as ?

A

drug reservoir

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17
Q

How the albumin act as drug reservoir ?

A

As the concentration of free drug decreases due to elimination, the bound drug dissociates from the protein .

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18
Q

When albumin act as a drug reservoir it lead to ?

A

maintains the free drug concentration as a constant fraction of the total drug in the plasma

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19
Q

All drugs accumulate in tissues , leading to higher concentrations in tissues than in the extracellular fluid and blood . (T/F) ?

A

F—> ( many not all )

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20
Q

Many drugs accumulate in tissues, leading to ?

A

Higher concentrations in tissues than in the extracellular fluid and blood .

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21
Q

Drugs may accumulate as a result of binding to ?

A

lipids, proteins, or nucleic acids .

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22
Q

Drugs may also be actively transported into tissues. (T/F) .

A

True

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23
Q

Tissue reservoirs may serve at two function, mention them

A
  1. As a major source of the drug .
  2. prolong its actions or cause local drug toxicity .
24
Q

Acrolein, the metabolite of cyclophosphamide , can cause ?

A

hemorrhagic cystitis

25
Q

Acrolein, the metabolite of cyclophosphamide, can cause hemorrhagic cystitis because ?

A

It accumulates in the bladder.

26
Q

The metabolite of cyclophosphamide is called ?

A

Acrolein

27
Q

The chemical nature of a drug weakly influences its ability to cross cell membranes ? (T/F)

A

F—>[The chemical nature of a drug strongly
influences its ability to cross cell membranes]

28
Q

Lipophilic drugs can’t move across most biologic membranes ? (T/F) ?

A

F—> (Lipophilic drugs “ readily “ move across most
biologic membranes)

29
Q

The features of Lipophilic drugs are ?

A

A. These drugs dissolve in the lipid membranes
B. It penetrate the entire cell surface.

30
Q

The major factor influencing the distribution of lipophilic drugs is ?

A

blood flow

31
Q

hydrophilic drugs do not readily penetrate cell membranes and must pass through slit junctions . (T/F) ?

A

True

32
Q

The fluid volume that is required to contain the entire drug in the body at the same concentration measured in the plasma.
This statement describe ?

A

The apparent volume of distribution

33
Q

How we can calculated the apparent volume of distribution ( Vd ) ?

A

It is calculated by dividing the dose that ultimately gets into the systemic circulation by the plasma concentration at time zero (C0).

34
Q

Slides from 18 - 22 are ?

A

Examples about the apparent volume of distribution (Vd) .

35
Q

Vd has physiologic and physical basis . (T/F) ?

A

F —[Vd has no physiologic or physical basis]

36
Q

Although Vd has no physiologic or physical basis, it can be useful to ?

A

Compare the distribution of a drug with the volumes of the water compartments in the body .

37
Q

The pecture in slide num.24 is ?

A

Ktheeeer Mohm 🥳

38
Q

The drug effectively trapped within the plasma (vascular) compartment. This case happen if the drug ?

A

• Has a high molecular weight
• Extensively protein bound,
• Too large to pass through the slit junctions of the capillaries

39
Q

The result from the previous case is ?

A

The drug has a low Vd that approximates the plasma volume (4 L in a 70-kg individual) .

40
Q

Give me example about drug trapped within the plasma .

A

Heparin

41
Q

The drug can pass through the endothelial slit junctions of the capillaries into the interstitial fluid if it ?

A

• Has a low molecular weight
• Hydrophilic

42
Q

Hydrophilic drugs cannot move across the lipid membranes of cells to enter the intracellular fluid. (T/F) ?

A

True

43
Q

In the previous case ,the drugs distribute into a volume that is the sum of the ?

A

plasma volume and the interstitial fluid

44
Q

plasma volume and the interstitial fluid together constitute the ?

A

extracellular fluid (about 20% of body weight or 14 L in a 70- kg individual).

45
Q

The drug can move into the interstitium through the slit junctions and also pass through the cell membranes into the intracellular fluid if it ?

A

• Has a low molecular weight
• Lipophilic

46
Q

The drug in the previous case distribute into a volume of about ……….
and the example about it is ………..

A

A. 60% of body weight or about 42 L in a 70-kg individual.
B. Ethanol

47
Q

A drug commonly associates exclusively with only one of the water compartments of the body.(T/F) ?

A

F—> ( rarely)

48
Q

the vast majority of drugs distribute into several compartments, often avidly binding cellular components, such as:

A
  1. Lipids : (abundant in adipocytes and cell membranes)
  2. Proteins : (abundant in plasma and cells)
  3. Nucleic acids : (abundant in cell nuclei)
49
Q

The volume into which drugs distribute is called ?

A

The apparent volume of distribution, Vd .

50
Q

Vd is useful pharmacokinetic parameter for ?

A

Calculating the loading dose of a drug .

51
Q

This process can be most easily analyzed by plotting the ……. of the plasma drug concentration (Cp) versus time

A

Log

52
Q

The concentration of drug in the plasma can be extrapolated back to time zero (the time of IV bolus) on the Y axis to determine C0. (T/F) ?

A

T

53
Q

The concentration of drug that would have been achieved if the distribution phase had occurred instantly . This statement describe ?

A

C0

54
Q

Why Vd has an important influence on the half-life of a drug ?

A

Because drug elimination depends on the amount of drug delivered to the liver or kidney (or other organs where metabolism occurs) per unit of time.

55
Q

Delivery of drug to the organs of elimination depends only on blood flow . (T/F) ?

A

F—(Delivery of drug to the organs of elimination depends not only on blood flow but also on the fraction of the drug in the plasma) .

56
Q

a drug has a large Vd, most of the drug is in the ?

A

extravascular space and is unavailable to the excretory organs.

57
Q

Any factor that increases Vd can decrease the half-life and extend the duration of action of the drug .(T/F) ?

A

F—(increase)

Pharma (8 decks)

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