DRUG DISTRIBUTION
| A |
Volume of distribution |
|
| B |
Clearance |
|
| C | Rate of administration | |
| D | Half life |
| A |
Volume of distribution |
|
| B |
Clearance |
|
| C | Rate of administration | |
| D | Half life |
Volume of distribution [Ref. K.D.T. 51h/e p 16, 17]
- After the drug reaches the blood, it may be distributed to various tissues.
- This is detennined by a hypothetical parameter, volume of distribution.
- It relates to the amount of drug in the body to the concentration of drug (c) in the blood or plasma
amount of drug in the body V —
concentration of drug in the plasma
- This volume does not necessarily refer to an identifiable physiological volume but rather to the fluid volume that would he required to contain all the drug in the body at the same concentration.
- if volume of distribution is more, it means more amount of drug is in the tissues and less is in the plasma.
- Thus a drug with high volume of distribution will require higher dose to achieve a particular plasma concentration. Loading dose
- If the time required to attain a steady state concentration of a drug is long relative to the temporal demands of the condition, a loading dose is required.
- The loading dose is one or a series of dose that may be given at the onset of therapy with the aim of achieving the target concentration rapidly.
- Loading dose is given to saturate the tissue stores so it is mainly dependent on volume of distribution.
Also know
- Maintenance dose depends on the clearance.
The pharmacokinetic properties of a new antihistamine are being studied in normal volunteers during phase I clinical trials. The clearance and half-life of the drug are determined to be 4.0 L/hour and 10 hours, respectively. Which of the following values is the approximate volume of distribution for this drug?
| A |
0.06 L |
|
| B |
14 L |
|
| C |
45 L |
|
| D |
60 L |
The pharmacokinetic properties of a new antihistamine are being studied in normal volunteers during phase I clinical trials. The clearance and half-life of the drug are determined to be 4.0 L/hour and 10 hours, respectively. Which of the following values is the approximate volume of distribution for this drug?
| A |
0.06 L |
|
| B |
14 L |
|
| C |
45 L |
|
| D |
60 L |
The volume of distribution of a drug can be determined using the following equation:
Concentration of a drug in blood is 40 microgna/ml. Dose of the drug is 200mg. Volume of distribution of the drug assuming minute elimination is ‑
| A |
5 litre |
|
| B |
0.5 litre |
|
| C |
2.5 litre |
|
| D |
3 litre |
Concentration of a drug in blood is 40 microgna/ml. Dose of the drug is 200mg. Volume of distribution of the drug assuming minute elimination is ‑
| A |
5 litre |
|
| B |
0.5 litre |
|
| C |
2.5 litre |
|
| D |
3 litre |
Ans. is ‘a’ i.e., 5 It.
Apparant volume of distribution of a drug less than 5 liters implies that the drug is predominantly in which of the following compartment?
| A |
Extracellular fluid |
|
| B |
Total body water |
|
| C |
Intracellular fluid |
|
| D |
Intravascular fluid |
Apparant volume of distribution of a drug less than 5 liters implies that the drug is predominantly in which of the following compartment?
| A |
Extracellular fluid |
|
| B |
Total body water |
|
| C |
Intracellular fluid |
|
| D |
Intravascular fluid |
Ans is ‘a’ i.e., Extracellular fluid
o A drug with high volume of distribution has more concentration in tissue and less in plasma.
o A drug with low volume of distribution has concentration only in plasma (intravascular)
Relationship between volume of distribution and extent of distribution
|
Vd (L) |
% body weight |
Extent of distribution |
|
< 5 |
7 |
only in plasma |
|
5-20 |
7-28 |
In extracellular fluid |
|
20-40 |
28-56 |
In total body water |
|
>40 |
>56 |
In deep tissues; bound to peripheral tissues |
Apparent volume of distribution of a drug exceeds total body fluid volume, if a drug is –
| A |
Sequestrated in body tissues |
|
| B |
Slowly eliminated from body |
|
| C |
Poorly soluble in plasma |
|
| D |
Poorly bound to plasma protein |
Apparent volume of distribution of a drug exceeds total body fluid volume, if a drug is –
| A |
Sequestrated in body tissues |
|
| B |
Slowly eliminated from body |
|
| C |
Poorly soluble in plasma |
|
| D |
Poorly bound to plasma protein |
Ans. is ‘a’ i.e., Sequestrated in body tissues
o Drug may have volume of distribution for in excess of total body water if it is sequestered in other tissues because most of the drug is present in tissues and plasma concentration is low.
Dosage of drug is determined by following except ‑
| A |
Volume of distribution |
|
| B |
Halflife |
|
| C |
Lipid solubility |
|
| D |
None |
Dosage of drug is determined by following except ‑
| A |
Volume of distribution |
|
| B |
Halflife |
|
| C |
Lipid solubility |
|
| D |
None |
Ans. is ‘None’
o Loading dose is governed by volume of distribution and volume of distribution is affected by lipid solubility. o Maintenance dose is governed by clearance (excretion) of drug and half life.
o For one option go ahead for option b ie half life because :
“Clearance is the most important factor for maintenance dose”.
Loading dose depends on ‑
| A |
Volume of distribution |
|
| B |
Elimination rate |
|
| C |
Half life |
|
| D |
Plasma volume |
Loading dose depends on ‑
| A |
Volume of distribution |
|
| B |
Elimination rate |
|
| C |
Half life |
|
| D |
Plasma volume |
Ans. is ‘a’ i.e., Volume of distribution
Loading dose is governed by volume of distribution and volume of distribution is affected by lipid solubility.
Maintenance dose is governed by clearance (excretion) of drug and half life.
Dosage of drug is determined by following except-
| A |
Volume of distribution |
|
| B |
Half life |
|
| C |
Lipid solubility |
|
| D |
Excretion of drug |
Dosage of drug is determined by following except-
| A |
Volume of distribution |
|
| B |
Half life |
|
| C |
Lipid solubility |
|
| D |
Excretion of drug |
Ans. is’d’ Excretion of drug
- Loading dose is governed by volume of distribution and volume of distribution is affected by lipid solubility.
- Maintenance dose is governed by clearance (excretion) of drug and half life.
- For one option go ahead for option b ie half life because :
- “Clearance is the most important factor for maintenance dose”.– Katzung 10th/e – 44




