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How well a drug can bind to a receptor

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The median lethal dose. The amount of toxic agent sufficient to kill 50% of a population within a certain time. e.g rat poison

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Median toxic dose. The dose required to get 50% of the population reporting this specific toxic effect.

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The study of the therapeutics uses and effects of drugs; the study of beneficial and adverse effects of drugs

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The median effective dose. The dosage required to achieve 50% of the desired response in 50% of the population

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First pass through the liver greatly reduces drug bioavailability before reaching to systemic circulation

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- concept describing subjects' reduced reaction to a drug following its repeated use. Increasing its dosage may re-amplify the drug's effects, but this may accelerate tolerance, further reducing the drug's effects.
- Is indicative of drug use but is not necessarily associated with drug dependence or addiction.

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Binding to the receptor and producing the opposite effect to the normal physiological response

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- Positively charged ion

Anion
- Negatively charged ion

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Binds to an allosteric (non-agonist site) on the receptor to prevent activation of the receptor.

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Are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist.

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Bind to receptors (active site) at the same binding site as the endogenous ligand or agonist but without activating the receptor, therefore once it binds it blocks agonist from binding.

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Binds to a receptor but only has a partial efficacy

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Is a receptor antagonist that binds to a receptor but does not activate the receptor.

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The percentage of total concentration of a drug, that reaches the blood stream in tact

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The quality of a drug having a certain action, affecting certain organisms/tissue or reacting with only certain substances.

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A constant proportion of drug is eliminated per unit time eg. alcohol

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A drug’s efficiency may be affected by how it binds to the plasma proteins.
Common blood proteins that drugs bind to, are human serum, lipoprotein, α, β & γ globulins and albumin.

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Involves enzymes changing the molecular structure of a drug 2 important ways:
1. Drug made more water soluble = easier to excrete
2. Metabolites = less pharmacologically active

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Rapid desensitisation of the body to the drug - occurs in minutes usually

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A property of a drug determined by combining its affinity at various binding sites, the knowledge of which can help predict a drug's potential for therapeutic and side effects.

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Molecules with a positive charge, attracting water molecules forming a macro-complex. Cannot cross the membrane due to low lipid solubility

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Selectivity refers to a drug's ability to preferentially produce a particular effeDct and is related to the structural specificity of drug binding to receptors.

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Amount of time taken for a drug to 1/2 relative to its initial concentration

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Measurement of Vol. of Plasma from which substance is completely removed per unit time. (mL/min)

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Movement of the drug in and alteration of the drug by the body. Often expressed as ADME
Absorption
Distribution
Metabolism
Excretion

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Physiological and biochemical effects of a drug + their mechanism of action at organ/system/subcellular/macromolecular levels

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Bringing to a receptor and not creating a physiological response

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the volume of distribution (VD) is the theoretical volume that would be necessary to contain the total amount of an administered drug at the same concentration that it is observed in the blood plasma

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Binding to a receptor and having a physiological response

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A considerable number of drugs are excreted from liver into bile  and from bile into small intestines.

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The ability to penetrate aqueous structures

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A body compartment into which a drug MIGHT be distributed e.g low Vd. (<5L) implies a drug is retained within vasculature + high Vd (>15L) drug is more lipid soluble & distributed to many parts of body compartments

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Ability to penetrate the cell membrane - like fat

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Family of isozymes responsible for the biotransformation of several drugs.

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A substance which initiates a physiological response when combined with a receptor

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Hepatic first pass metabolism
Irreversible loss of the drug from the body

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Severe adverse allergic reaction that has a rapid onset affect on the body. Does not discriminate between sexes or ages

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The effects of the drug on the body

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What the body does to the drug

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The effect of a drug on the body: action-effect sequence + dose effect relationship. Also includes how one drug may modify the actions of another.
There are 5 basic types of drug action
1. Stimulation
2. Depression
3. Irritation
4. Replacement
5. Cytotoxic Action

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<7 Acidic (the lower the number the more acidic)
>7 Alkaline/Basic (the higher the number the more alkaline)
7 Neutral

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The rate and extent of absorption of drugs reaching the systemic circulation via any route i.e oral, IV

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The pH that is 50% ionised and 50% unionised