General Principles Flashcards
The ability of a drug to produce response
Efficacy
the dose of the drug that gives 50% of the Emax
ED50 (Effective Dose)
the dose of the drug needed to cause a harmful effect in 50% of a test population of subjects.
TD50 (Toxic Dose)
the dose needed to cause death in 50% of a test group of animals
LD50 (Lethal Dose)
the ratio between the LD50 and the ED50. It is a measure of safety
Therapeutic index (TI) LD50/ED50
the ratio between the LD50 and the ED50. It is a measure of safety
Therapeutic index (TI) LD50/ED50
If the antagonist binds to the same site of the agonist on the receptor, it is called
competitive antagonist
If the antagonist binds to another site on the receptor, and prevented the action of the agonist, it is called
non-competitive antagonist
the science dealing with tailoring drug medication according to the circadian rhythm of the body to get better response and/or to avoid possible side effects.
Chronopharmacology
the science dealing with tailoring drug medication according to the circadian rhythm of the body to get better response and/or to avoid possible side effects.
Chronopharmacology
means that the combined effect of two drugs is equal to the sum
of their individual effects (i.e. 1+1=2).
Summation
means that the combined effect of two drugs is greater than the sum of their individual effects (i.e. 1+1=3).
Synergism
means that the combined effect of two drugs is greater than the sum of their individual effects (i.e. 1+1=3).
Synergism
similar to synergism but, in potentiation, the effect of one drug itself is greatly increased by intake of another drug without notable effect (i.e. 1+0=2),
Potentiation
One drug abolishes the effect of the other i.e. 1+1=0 (
Antagonism
means progressive decrease in drug response with successive administration.
Tolerance
is an acute type of tolerance that occurs very rapidly
Tachyphylaxis
is recurring of symptoms in exaggerated form when a drug is suddenly stopped after a long period of administration.
Rebound effect
is recurring of symptoms in exaggerated form plus addition of new symptoms when a drug is suddenly stopped
Withdrawal effect (syndrome)
It is the pH at which 50% of the drug is ionized and 50%is non-ionized
pKa of a drug
The apparent volume of water into which the drug is distributed in the body after distribution equilibrium.
Volume of distribution (Vd)
Some drugs are not metabolized at all and excreted unchanged.
(hard drugs)
A set of enzymes that is responsible for the majority of phase II reactions
Glucuronyl transferase
Metabolism of drugs at the site of administration before reaching systemic circulation
First-pass metabolism
(pre-systemic elimination)
The time needed to eliminate 50% of the drug from the plasma
Half-life (plasma Half-life)
the steady level of drug in plasma achieved when the rate of administration equals the rate of elimination.
Steady-state plasma concentration (Cpss)
- The Cpss is reached after 4-5 t1/2
- If we changed the dose, the new Cpss is reached after 4-5 t1/2
- If dosing stops, complete elimination of drug from plasma occurs after 4-5 t
The rule of 5
Abnormal enlargement of the thyroid gland
Goiter