‫قسم تقنيات التخدير‬

‫المرحلة الثانية‬

‫التخدير‬
‫‪LEC 2‬‬

‫م‪.‬د‪ .‬دعاء سالم‬ ‫‪2023 – 2024‬‬

 GENERAL PHARMACOLOGY

Part: 1
Pharmacokinetic

Dr. Duaa Salam

PHARMACOLOGY

Pharmacology:
is the study of drugs and their actions on the
body.

Science of drugs:
dealing with the study of Desirable and
Undesirable effects.
 What is PHARMACOLOGY ?
Pharmacokinetics Pharmacodynamics
What the body does to drug Pharmacology What the drug does to body

Pharmacology

Pharmacotherapeutics Pharmacy
The study of the use of drugs Preparing suitable dosage forms

Toxicology

Drug

“ Drug is any substance or product that is

(used or is intended to be used) to modify
physiological systems or pathological states for
the benefit of the recipient .”
 DOSE Vs DOSAGE
•Dose: The quantity of drug administered at one time

•500mg of Paracetamol

•Dosage: The amount of the drug that should be given over

time

•500 mg Paracetamol TID for 3 days

PHARMACOKINETICS
•The study of what the body does to the drug

•It is the study of absorption, distribution, metabolism

and excretion (ADME) of drugs

•“Fate of drug”
 PHARMACOKINETICS

•Absorption
#How the drug is moved into blood stream from the site of administration ?

•Distribution
#How much drug is moved to various body tissues / organs ? Depends on
blood flow through tissue

•Metabolism
#How the drug is altered – broken down ?

•Excretion
#How much of the drug is removed from the body ?

Absorption
•Absorption is the movement of a drug from its site of
administration into the blood.

• The rate of absorption determines how soon effects will

begin.

•The amount of absorption helps determine how intense

effects will be.
 Absorption

•Factors Affecting Drug Absorption

Rate of Dissolution

Surface Area

Blood Flow

Lipid Solubility

PH Partitioning
 BIOAVAILABILITY

•Bioavailability is a fraction of administered dose of

a drug that reaches the systemic circulation in the
unchanged form.

•What is the bioavailability of IV route?

 BIOAVAILABILITY
Factors influencing bioavailability

• Dosage forms
• Chemical form
• Dissolution & Absorption of drug
• Route of administration
• Presence of food/drugs in GI tract
• First pass effect
• Extent of drug metabolism before reaching systemic
circulation .

DISTRIBUTION

Distribution is a branch of pharmacokinetics

which describes the the movement of drugs
throughout the body.
 DISTRIBUTION

•Drug distribution is determined by three major

factors:

•Blood flow to tissues

•The ability of a drug to exit the vascular system

•The ability of a drug to enter cells.

Plasma- Protein Binding

•Many drugs bound to circulating plasma proteins such as

albumin, lipoproteins, glycoprotein, globulins etc.

¾Free form: Pharmacologically active

¾Bound form: Pharmacologically inactive

 Effects of Protein Binding

•Acts as temporary store of drug

•Prolongs it’s action
•Cause prolonged low level of drugs
•Slowly released from bound reservoir
•Delays metabolism
•Delays excretion
•Decreases its entry into CNS

•Factors affect protein binding:

•Renal failure

•Inflammation

•Fasting or malnutrition

•Competition from other drugs can also affect % bound.

 An Example

•Warfarin (anticoagulant) protein bound ~98%

•Therefore, for a 5 mg dose, only 0.1 mg of drug is free in the

body to work!

•If patient takes normal dose of aspirin at same time

(normally occupies 50% of binding sites), the aspirin displaces
warfarin so that 96% of the warfarin dose is protein-bound;
thus, 0.2 mg warfarin free; thus, doubles the injested dose

Dosing

•Dosing Interval - How often the drug should be given

•Loading dose – Which puts the plasma concentration

in the therapeutic range

•Maintenance dose - Routine smaller doses to

maintain the steady state (Plateau)
 METABOLISM

™Metabolism = biotransformation
™The conversion from one chemical form to another

™Site of drug biotransformation

•Liver - cytochrome P450 (microsomal P450) pathways are used to
metabolize most agents
•In w enzymatic alteration of drug structure occure

™Drugs may induce (activate) or inhibit these enzymes

Drug – Drug interactions

Drug Metabolism Therapeutic

Consequences of Drug
•Drug metabolism has six possible consequences of
therapeutic significance:

1.Accelerated renal excretion of drugs

2.Drug inactivation
3.Increased therapeutic action
4.Activation of "pro-drugs"
5.Increased toxicity
6.Decreased toxicity
 First Pass Metabolism
™Effect of first pass metabolism
¾Part of administered dose made
inactive
™↓ bioavailability
¾Drug converted into its active form

•Nitroglycerin when given orally

•Totally inactivated in the liver
•100% first pass effect
•Always given sublingually

Factors affecting metabolism

1.Age : Children / Elderly
2.Disease condition e.g. Liver disease
3.Induction of drug metabolizing enzymes
4.First-pass effect: Nitroglycerin
5.Competition between drugs
6.Genetics
7.Environment e.g. Smoking
 Excretion
Drugs &/or its metabolites are irreversibly eliminated
from the body

•Elimination of the drug

•Unchanged (Parent form)

•Metabolites
•Routes of excretion
•Kidneys – Urine
•GIT – Stools
•Skin - Perspiration
•Eyes – Tears
•Lung - expiration