Pharm1 - Block3 - Gen Pharm 5

45 terms by bigjohnshea45th 

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Therapeutic range may be narrow, and in this case what is key to understand

Size of dose must be smaller to prevent exceeding therapeutic range

Therapeutic range may be wider, and in this case what is key to understand

Size of dose may be larger and still not exceed therapeutic range

Range at which drug is most beneficial to the psecific patient

Therapeutic range

Therapeutic range may be achieved quickly via the use of

Loading dose

Steady state of a drug is determined by half life of drug, and so dosage of drug that results in steady state within the therapeutic range is called

Therapeutic dosing

Macromolecular component of the cell to which a drug binds to produce it's effect

Receptor

Maximum effect of the drug may be achieved without activating

all the receptors

Ability of the drug to bind to the receptors (nothing more)

Affinity

Ability of drug to activate receptor and produce response

Intrinsic activity (of drug)

Drug which has affinity for, and intrinsic activity of, a receptor is called an

Agonist

Drug which binds to receptor and activates it, but produces receptor activity that is the opposite of what the agonist drug would produce

Inverse agonist

Prominent example of inverse angonists

Antihistamines

Drug which has affinity for the receptor, but no intrinsic activitiy or inverse agonist properties

Antagonist

Drug which activates the receptor, but has submaximal intrinsic properties by comparison

Partial agonist

When a partial agonist is given along with a pure agonist, the partial agonist will have what effect

Antagonism of the pure agonist

Greatest efficacy on a dose response curve is achieved by

Agonist

Less efficacy on a dose response curve is achieved by

Partial agonist
Invese agonist

Zero efficacy on a dose response curve is achieved by

Antagonist

If an agonist and an allosteric activator are combined, what will be the result on the dose response curve

Exceeds the agonist alone (A+C)

If an agonist and a competitive inhibitor (partial agonist) are given together, what will be the result on the dose response curve

Same efficacy as agonist alone, but the potency is lower

If an agonist and an allosteric inhibitor are given together, what will be the result on the dose response curve

Efficacy is greatly diminished, but potency is same

Receptors with the fastest physiological action

Ion channels

Receptor which results in either opening an ion channel or production of second messengers via intermediary proteins

G-protein coupled receptor

Receptor which results only in production of secondary messengers (at the membrane)

Kinase-linked receptor

Receptor that results in the production of second messengers at the nucleus

Nuclear receptor

Three important ligands that can act on nuclear receptors

Steroids
Vita D
Thyroxine

Graded dose response curves display which two properties of the drug in question

X = Potency
Y = Efficacy

Amount of drug needed to achieve EC50%

Potency

Dose required to produce 1/2 of the maximum response

EC50%
(low EC50% = high potency)

Dose required to occupy half of the receptors present

Kd
(low Kd = high affinity)

The maximum response of a drug (upper limit of drug response curve)

Efficacy

If two drugs have the same efficacy and potency, but one has a faster response to that efficacy, the slope on the drug response curve will be

Steeper

A drug which produces a steeper drug response curve is said to have a greater

Dose range

Ratio of median lethal dose (LD50), and median effective dose ED50) equals

LD50 = dose that is lethal in 50% of the population
ED50 = dose that is effective in 50% of the population

Therapeutic index/ratio

The clinical value of the Therapeutic index/ratio of a drug is essentially

Represents the safety of a drug

Therapeutic index is represented on which types of graphs

Quantal dose response curves

(Cummulative frequency distribution: is the frequency of occurance of values of a phenomenon)

Quantal dose response curves display the cummulative freuncy distribution for various doses of drugs in the population tested, and so the cummulative frequency distribution for the therpeutic effect of the drug and the lethal effect of the drug can be compared in order to establish which values

ED50% and LD50%

Drug which binds to a different receptor molecule and produces an effectt aht is opposite to that produced by the drug it antagonizes

Physiological Antagonist

Another name for an antagonist

Pharmacological antagonist

An antagonist that must compete to bind to the same receptor as the agonist

Competitive/Reversible antagonist

Competitive/Reversible antagonists have what effect on the agonists activity

Reduces the potency of the agonist, not the efficacy of the agonist

Competitive/Reversible antagonists have what effect on the position of the drug response curve of a dosage

Causes a parallel shift in the drug response curve towards a higher concentration

Antagonists that bind irreversibly to a site other than that of the agonist

Noncompetitive/Irreversible antagonists

Noncompetitive/Irreversible antagonists have what effect on the agonists activity

Reduces the efficacy of the agonist

Noncompetitive/Irreversible antagonists have what effect on the position of the drug response curve of a dosage

Causes a nonparallel shift in the drug response towards a lower efficacy

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