Membrane transport

**Passive diffusion**

Pharmacology for dummies

 • PK is the quantitative study of
drug movement in, through and out
of the body

During these movements a drug has

to cross various biological membranes

Study of membrane transport

explains how drugs cross biological
membranes
Pharmacology for dummies
 Types of membrane transport

1. Passive diffusion and Filtration

2. Specialized transport
a. Carrier transport

Facilitated diffusion

Active transport
* Primary active
* Secondary active
b. Pinocytosis
Pharmacology for dummies
 Passive diffusion

Higher Lower
Concentration Concentration
Passive diffusion
•Down a concentration
or
electrochemical
Passive diffusion of gradient
drug •Not saturable
{Higher to lower} •No energy required
•Lipid soluble & non-
ionized diffuse better
•Ionized drugs pass
Membrane poorly
•Governed by Fick’s law
Pharmacology for dummies •Ion trapping concept
 Passive diffusion and influence of pH
• Most drugs are weak electrolytes which
partially ionize in aqueous solutions
• Unionized drugs diffuse [Absorbed] better
• Ionization is pH dependent. Hence absorption is
pH dependent
• Weakly acidic drugs ionize more in alkaline
medium. Hence poorly absorbed in alkaline
medium [Eg.Penicillin V, aspirin]
• Weakly alkaline drugs ionize more in acidic
medium. Hence poorly absorbed in acidic
medium [Chloroquine, atropine]
• These considerations lead to three
implications -On Absorption,Ion trapping and
Excretion

Pharmacology for dummies

 pH and absorption

Acidic
Absorbed better
Drugs
Unionized

Acidic

Alkaline

Alkaline
Drugs-Unionized Absorbed better

Note: Irrespective of ionization most of the absorption

takes place in the small intestine because of the large surface area
Pharmacology for dummies
 pH and ion trapping
Gastric cell
Acidic
[Alkaline]
Drugs
Absorbed
Unionized
Eg.Aspirin
Ionized

Acidic
Medium Can not
diffuse
further

Trapped

Cell damage
Pharmacology for dummies
 pH and excretion in urine
Overdose of
Aspirin
[Acidic drug]

Alkalanize urine
[With Na Hco3]

Drug ionized

Poorly absorbed

Excreted
Urine is alkalanized[Na Hco3] or acidified [NH4Cl] to increase excretion
of acidic or basic drugs respectively, in overdosage.

Pharmacology for dummies

 Questions
• 1. Discuss with examples implications of pH
on drug transport across biological
membranes
• 2. What are the factors which determine
passive diffusion across membranes?

• Most important determinant of ion-

trapping is
a. pH across membranes
b. Lipid solubility of a drug
c. Aqueous solubility of the drug
d. None of the above
Answer: ‘ a’
Pharmacology for dummies
 Questions
• In a patient who presented with barbiturate
poisoning following drug can be administered to
facilitate excretion of barbiturate in urine

a. Ammonium chloride
b. Ascorbic acid
c. Sodium bicarbonate
d. Sodium chloride

Answer: ‘ c ‘. To alkalanize urine which increases

ionization and increases excretion.

Pharmacology for dummies