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23 Cards in this Set

  • Front
  • Back

GRADED DOSE-RESPONSE RELATIONSHIP

- Response increases with increasing dose


- Commonly used to assessing safety and efficiacy


- E.g: Psychomotor (relationship between cognitive functions and movement) effects of alcohol

QUANTAL DOSE-RESPONSE RELATIONSHIP

- All or none dose-response


- Commonly used for assessing safety


- E.g: effectiveness of an oral contraceptive, percentage of rodant death at particular dose of sedatives.

DRUG-RESPONSE CURVE FOR GRADED RESPONSE

- Hyperbolic curve which makes it difficult to extrapolate information from

- Hyperbolic curve which makes it difficult to extrapolate information from

SEMI-LOG DRUG-RESPONSE CURVE FOR GRADED RESPONSE

- Log one axis (drug conc) which allows you to extrapolate from big linear part

- Log one axis (drug conc) which allows you to extrapolate from big linear part

DOSE-RESPONSE CURVE FOR QUANTAL RESPONSE

- Hyperbolic curve, difficult to extrapolate information

- Hyperbolic curve, difficult to extrapolate information

SEMI-LOG DOSE-RESPONSE CURVE FOR QUANTAL RESPONSE

- Log one axis (drug conc) which allows you to extrapolate information easier

- Log one axis (drug conc) which allows you to extrapolate information easier

Emax

Maximum response of drug. No more increase in response when dose is continued to be increased.

THRESHOLD DOSE

First dose of the drug that will give you a response.

CEILING DOSE

The maximum biological effect that can be induced in a tissue by a given drug, regardless of how large a dose is administered.

EFFECTIVE CONCENTRATION

The dose at 50% of the maximum response.

THERAPEUTIC INDEX

Therapeutic index (TI) = LD50 (lethal dose that would kill 50% of population) or TD50 (toxic dose that would effect 50% of population)/ ED50 (effective dose of 50% of population)

THERAPEUTIC INDEX CURVES

FACTORS INFLUENCING AN INDIVIDUALS RESPONSE TO DRUGS

- Age


- Gender


- Body weight


- Liver function


- Kidney function


- Ethnic origin


- Genetic make up (pharmacogenetics)


- Interactions: drug-drug, drug-nutrients, drug-disease

LOCK AND KEY HYPOTHESIS

AGONIST

- A drug that binds to an activates a receptor


- Intrinsic activity = 1

ANTAGONIST

- A drug that attenuates(reduces) the effect of an agonist


- Intrinsic activity = 0


- Competitive antagonist: binds to the same receptor site as the agonist does, blocking the action of the agonist


- Non-competitive antagonist: binds to allosteric (non-agonist) site of the receptor preventing activation of receptor

DRUG-DOSE RELATIONSHIP WITH AGONISTS AND ANTAGONISTS

AFFINITY (Ka)

Affinity (Ka) = association constant (K1)/dissociation constant (K-1)



How tightly a drug bounds to the receptor

POTENCY

- The amount of response a drug causes at specific concentrations


- A highly potent drug will cause a great response at a small dose

EFFICIACY

A drugs capacity to produce an effect.

TYPES OF RECEPTORS

- Type 1: Ionotropic receptors (ligand gated ion channels)


- Type 2: Metabotropic receptors (G-protein coupled receptors)


- Type 3: Enzyme-linked receptors (


- Type 4: Intracellular receptors

SWITCHING OFF: DRUG DESENSITISATION

When an agonist is administered continuously or receptors are being activated constantly, desensitisation of receptors takes place until the agonist falls below a certain threshold and the system can become sensitive again.

5 TYPES OF DRUG DESENSITISATION

- Receptor sequestration


- Receptor down regulation


- Receptor inactivation


- Inactivation of signalling proteins


- Production of inhibitory protein