Professional Documents
Culture Documents
body. So we have two parts of this science: the body and drugs
1- Pharmacodynamics: (quality…effect) simply how the drug
affects the body (tissue function, cells or biological
medium), so it’s related to drug ACTION. Most drugs acts
by affecting specific receptors either by stimulating or
inhibiting them(agonist and antagonist are discussed later)
2- Pharmacokinetics:(quantity….level) how the body reacts to
the drug…. This involves drug absorption, distribution,
metabolism and excretion(ADME).
Pharmacokinetics include:
- Free drug: drugs are found in blood in two forms(free and bound
to plasma proteins … mainly albumin), only the free portion can
exert a pharmacological effect( because it’s the part that can
interact with receptors, while the bound is trapped)… so free
portion is the one that really works and and excreted or
metabolized. So what happens when the free portion is
consumed? Ok, there’s a balance between bound and free
portion, so some of the bound drug is released and become free.
- Bioavailability: is the ratio between drug level in blood when given
in extravenous route and when given. Assuming when the drug
given I.V. has 100% bioavailability, so it’s given as percentage.
- Bioequivalence: comparison of related drugs bioavailabilities ( e.g.
two hypoglycemic agents with bioavailability of 60% are said to be
bioequivalent)
- Therapeutic equivalence: comparison of therapeutic or toxic effect
of related drugs(e.g. amount of blood pressure drop for two
antihypertensive agents)
- Receptors: macromolecules-usually proteins- found on cell
surface, in the nucleus or in the cytoplasm, and most of drugs
exert their actions through binding to their specific receptor.
a- Affinity: how tight is the drug bound to it’s receptor.
b- Intrinsic activity: ability of the drug to induce specific
changes upon binding to it’s receptor
c- Agonist: a drug that induces a response upon binding to
it’s receptor
d- Antagonist: a drug that binds to a receptor without
inducing it. So it acts by inhibiting the agonist from
exerting their actions.
e- Agonist and antagonist can be competitive or non-
competitive
f- When we said its competitive agonist it means that the
number of drug bound to the receptor is proportional to
relative concentration to other substances trying to bind
to the same receptor(i.e. its binding is reversible), same
concept for antagonist.
g- Non competitive is irreversible binding, so once the drug
is bound it can’t be displaced.
- Potency: relative doses of drugs needed to produce specific effect.
(two hypoglycemic agents with different doses to cause glucose
drop by 20% with different doses)
- Efficacy: maximal effect an agonist can achieve-at the highest
practical concentration-.
- Therapeutic index: toxic dose/therapeutic dose, higher value
means safer drug.
- Minimal dose: lowest therapeutic dose.
- Maximal dose: highest therapeutic dose without toxicity.
- Average dose: dose needed in most patients for a desired effect.
- Therapeutic dose: range from minimal to maximal dose.
- Half life of a drug (t1/2): time needed to eliminate 50% of the
drug.
- Loading dose: Large doses given initially to reach the therapeutic
range fast, then we give regular lower doses (maintenance dose)
to maintain therapeutic level.
- Median lethal dose (LD50): the dose that kills 50% of experimental
animals.
- Effective dose 50%: dose causing therapeutic response in 50% of
subjects.
- Phamacogenetics: difference in drug response among people due
to different genetics(e.g. some has fast metabolism of certain
drugs)
- Teratogenicity : to cause harm to the fetus in a pregnant woman
due to drugs given in pregnancy(e.g. warfarin).
- Chemotherapy: treatment of inflammatory diseases caused by
micro-organisms with drugs, also used for drug for cancer
treatment.
Drugs interactions:
Two types: