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Molecules react only with those receptors in the body that are shaped similarly,
like a lock and key.
A drug’s activity can be predicted by examining its molecular shape and functional
groups.
Stereoisomers – isomers of the same molecule that are mirror images of each other.
A drug that contains a mixture of stereoisomers can have more drug activity and/or
cause more side effects.
Lipids – molecules that form long chains of covalently bonded carbon and hydrogen
atoms; soluble in fat or oil; used to create hormones and other active biochemical.
Ionization affects drug activity. Ionic molecules cannot easily cross membranes and
enter the bloodstream.
Ionization can affect excretion; ionized drugs cannot easily cross membranes to
exit the bloodstream.
Acid molecules donate protons; basic molecules accept protons.
A basic drug in the acidic stomach environment facilitates the exchange of many
protons, creating ionic molecules that are difficult to absorb into the
bloodstream. An acidic drug in the acidic stomach environment, more of the drug
will get absorbed because few molecules will shed protons and most will remain
neutrally charged.
Pharmacodynamics – the study of drug receptor theory at the molecular level and how
that interaction translates to drug activity on the entire body.
Agonist – drugs whose activity stimulate a specific response when binding to
receptors.
Antagonist – drugs that block a response when binding to receptors.
Antagonists block in two ways:
directly by inactivating the receptor, blocking its ability to trigger a response;
binding to the receptor in a competitive fashion, keeping agonist molecules from
binding and then triggering a response.
Potency – power to affect body or mind. A drug that achieves the same response as
another drug but at a lower dose is more potent. Timing of dosing is very
important, when desired is a constant concentration in the therapeutic range.
Active transport – use energy to bring drug molecules across the membrane.
Age
The very young and old pose the greatest risks to safe drug therapy.
Pediatric practice – infants and children
infants being of greatest concern because of body makeup and liver function
higher body water content, drugs that are highly water-soluble will distribute
well, toxicity is an issue
good blood circulation
liver function is not fully mature at birth – affecting absorption, distribution,
and metabolism