General Pharmacology: Pharmacokinetics Pharmacodynamics Drug-Drug Interactions

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General Pharmacology

➢Pharmacokinetics
➢Pharmacodynamics
➢Drug-drug interactions
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1. Pharmacokinetics: Describe what the body does to the drug. This
includes: absorption, distribution, biotransformation and excretion of durg.
2. Pharmacodynamics: Describe what the drug does to the body. This
includes the mechanism of action, pharmacological action, adverse effects,
and the pharmadodynamic drug-drug interaction.
3. Pharmacotherapeutics: Describe uses of drug for prevention, diagnosis
and treatment of diseases.
Drug: Chemical substance that affects biologic systems of living
organism.
Drug nomenclature:
3 1.Chemical name: Describe chemistry of the drug e.g. acetyl salicylic acid.
2.Generic (Non-proprietary or approved) name: This is the
abbreviated and approved name of the drug. It is the official medical
name assigned by the producer in collaboration with the food & Drug
Board and Nomeneclature committee. Each drug has only one name all
over the world and it is not capitalizes e.g. aspirin, atenolol, amlodipine,
and captopril. Very few drug have two generic names e.g (“paracetmol-
acetaminophen”, “neostigmine-prostigmine”, “epinephrine-
adrenaline”, “norepinephrine-noradrenaline”, “meperidine-
pethidine”).
3.Brand (Proprietary or Trade) name: These are names given to the
drug by the manufacturing and marketing company, and they are
copyrighted terms selected by the manufacturer e.g. Aspocid, Inderal,
Tonormin, Myodura, and Capoten.
PHARMACOKINETICS
4 ABSORPTION
Definition: Passage of drugs from site of administration
to systemic circulation.
the mechanisms of drug absorption follow the
mechanisms of drug movement across the biological
membranes, which include:
1. Passive diffusion: The most common and most
important mechanism, it includes:
A. Rapid movement of lipid-soluble drug across
the cell membrane.
B. Movement of water-soluble drugs across the
aqueous channels (water pores).
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2. Facilitated diffusion:
No energy is required as the drugs are carried to inside of the cell according
to the concentration gradient by :
a. Carrier protein.
b. Drug transporter.
3. Active transport:
Energy is required because the drug movement may be against the
concentration gradient by :
a. Drug transporter.
b. P-glycoprotein drug transporter extrudes drug outside the cells, and it is
responsible for drug resistance.
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4. Endocytosis and exocvtosis:
Usually occur by drugs of high molecular
weight. The drug binds to the cell membrance,
dips in and enveloped by the cell membrane,
a tear in the cell membrane allow the drug to
move inside/ outside the cell.
The tear is healed immediately.
2. Factors affecting absorption:
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A) Factors related to the patient:
1.Route of administration: I.V. and inhalation > I.M. > S.C. > Oral >
Topical.
2.Absorbing surface:
 Vascularity (Alveoli > Skeletal muscle > S.C.tissue).
 Surface area (Alveoli > Intestine > Stomach).
 Pathological conditions: Diarrhea & malabsorption oral
absorption.
3. Systemic circulation :
H.F. & shock absorption oral and I.M. routes are not suitable.
4. Specific factors: Intrinsic factor is essential for vitamin B12
absorption.
B) Factor related to the drug:
8 1. Water and lipid solubility:
Both are needed for absorption
Completely water-insoluble compounds are not absorbed (e.g. barium
chloride).
 Lipid solubility absorption ( lipid /water partition coefficient)
2. Ionization:
Non-ionized (uncharged) better absorption
Depends on pKa of the drug and pH of the medium
Quaternary ammonium compounds ionized poor absorption
Streptomycin has high pKa always ionized not absorbed
orally
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3. Valency : Ferrous iron (Fe+2) is absorbed better than ferric iron (Fe+3)
4. Nature: Inorganic compounds (small particles) > organic compounds
( large particles)
5. Pharmaceutical preparation:
Dosage form: Solution > Suspension> tablet
Shape, size of particles and rate of disintegration and dissolution of
tablets
Excepient (filler): Ca+2 salts oral absorption of tetracyclines

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