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Lect 2 Pharmacokinetics (Absorp + Distribution) - Sphinx - Absorption

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8 views

Lect 2 Pharmacokinetics (Absorp + Distribution) - Sphinx - Absorption

Uploaded by

www.moks.mahmoud123
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Lecture 2

Basic pharmacology
Pharmacokinetics
Absorption
Pharmacokinetics
Pharmacokinetics: is the branch of pharmacology which studies the
effect of the body on the drug

 For an administered drug to exert a pharmacological effect at the site of


action, it must pass four essential pathways of drug movement and
modification in the body (ADME)

Absorption  drug enters the body and 1


reaches the bloodstream.
Distribution  drug transfers to different 3
body tissues 2

Metabolism  How drug is changed by the


body

Excretion  The route by which drug, or its


metabolites, leave the body
4
1) Absorption
Absorption is the process which means the transfer of the
drug from site of administration to blood.

Drug absorption requires passage of the drug through


various cell membranes
Transmembranal
Linear glycoprotein protein

Peripheral protein

Hydrophilic Surface
phosphate protein
head Oily non-
polar core
 Types of drug passage through cell membrane
 Rate of drug transport through cell membranes depends on
Drug lipophilicity and Drug concentration
 The rate of passage of the drug is directly proportional to the
concentration gradient of the drug across cell membrane.

 Transfer of drug occurs till equilibrium

a- Passive diffusion:

 Is the most common mode of


drug transport.

 Drug is lipophilic
 Drug transports according to
gradient of concentration from
 to  conc.
b- Carrier-mediated transport (Facilitated) :
 Drug transports according to gradient of concentration
from  to  conc.
 Drug is not lipid soluble
 This type of transport needs Carrier but does not need
energy
C- Active transport :
 Transport of substance across the phospholipid
layers of the cell membrane goes against
concentration gradient.

 Energy is required.
d- Para cellular transport :
 This is diffusion and transport of the drug molecules and
accompanying water across narrow junctions between cells
or trans-endothelial channels.
e- Vesicular transport:
 This is the process of engulfing particles or dissolved
materials by a cell. This includes:
1. Phagocytosis: which is the engulfment of large particles or
macromolecules, usually by phagocytes

2. Pinocytosis: which is the engulfment of small solutes or fluids.

3. Endocytosis: which is the movement of macromolecules into of


the cell.
4. Exocytosis: which is the movement of macromolecules out of the
cell.
Factors affecting drug absorption

Drug Body (host)


1. Drug molecular weight 1. Blood supply
2. Drug formulation 2. Gastric emptying rate (GER)
3. Drug combination: 3. Intestinal motility (peristalsis)
ex: Vit C  absorption of Iron
4. Diseases:
4. Drug route of administration

5. Drug polarity and lipophilicity


6. Drug acid base nature
 Factors due to body 
1. Blood supply:
 The  in blood supply to the site of administration   drug absorption
and vice versa
 Local anesthetics is preferred to be applied together with a vasoconstrictor
like adrenaline?????????
2. Gastric Emptying Rate (GER)
 Natural process meaning ejecting the stomach's contents, normally, this
occurs a few hours after eating.
 It can be delayed or accelerated by certain conditions, such as diabetes,
gastric ulcers, or neurological disorders.

3. Intestinal motility
 Factors due to drug 
1. Drug molecular weight:

2. Drug formulation

3. Route of administration
 Different routes of drug administration differ in drug bioavailability
(rate and extent of drug absorption)

 This may dramatically modify drug effects, drug onset and duration
of action

 There is a difference between the route of drug administration which may


be (enteral, parenteral or topical) and the obtained action which may be
(local or systemic).
4. Drug Polarity and lipophilicity
 Drug Polarity (lipid/water partition coefficient)

 Drug polarity is the ratio of the lipid-soluble portion to the water-soluble


portion of the drug when distributed between water and an immiscible
lipid.

Non polar drugs Polar drugs


Lipophilic Lipophobic
Hydrophobic Hydrophilic

Highly absorbed Poorly absorbed

- Drug absorption from GIT - Weak GIT absorption


- Blood brain barrier (BBB) - Cannot pass BBB
- Placental barrier (PB) - Cannot pass PB
- Reabsorption in the kidneys - Easily excreted
Water or lipid solubility is a
physical character which can
affect drug kinetics (Absorption –
Distribution – Metabolism –
Excretion) but it has no effect on
drug activity
5. Drug acid/base nature (effect of pH)
 Most drugs are weak acids, weak bases or salts of either of them.

 They become ionized or nonionized according to the pH of the medium


around them

weak acids drugs weak bases drugs


example Morphine /
acetylsalicylic acid amphetamine

Acid media less ionized highly ionized


more lipid soluble less lipid soluble

Basic media highly ionized less ionized


less lipid soluble more lipid soluble
 pKa of drug 
 pKa: is the pH at which drug (50% ionized) and (50% non
ionized).

pKa of aspirin=3.5 pKa of


amphetamine=10

- Drugs with low pKa is (acidic) and drugs with high pKa is
(basic)
 pKa is a constant value but it helps to illustrate drug
dissolution in different pH media
• Aspirin in acid media (stomach) present highly in non-ionized
form  highly absorbed
• Aspirin in alkaline media (intestine) present highly in ionized
form  poorly absorbed

• Amphetamine in acid media (stomach) present highly in


ionized form  poorly absorbed
• Amphetamine in alkaline media (intestine) present highly in
ionized form  highly absorbed
 Bioavailability 
 The of rate and extent (amount) of drug reached the systemic circulation
after administration (Biological available for action).

 Bioavailability affected by routes of administration and drug absorption.

 Bioavailability calculated on time conc curve.


 Selected dose of a drug injected iv (red curve)

 Then you inject the same drug with same


dose but with other route (blue curve)

(AUC) oral
= --------------
(AUC) iv
 Oral bioavailability of drug 70% what does
it mean????

 Is it possible that oral bioavailability of drug >100% ??????

 Why oral conc of a drug differ than iv conc of the same drug
?????

 Doses of the same drug may differ according to dosage form


????

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