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isotope – same number of protons different number of neutrons; often radioactive.

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.

An example of active transport is the sodium/potassium exchange pump, which


requires ATP for energy. These proteins use energy to pump potassium into the cell,
and sodium out.

Overall absorption can be limited because active transport are limited by


availability of energy sources, can become saturated, or maxed out.
Diffusion is a passive transport mechanism where many drugs are absorbed because
molecules move along a concentration gradient. Blood flow and surface area can
affect absorption; surface areas that are large, thin, and have good blood supply,
can easily affect systemic absorption.
Highly-water soluble drug stays in the bloodstream.
Highly fat- or lipid-soluble, accumulates in fatty tissue and then slowly released
over time back into the bloodstream – two-compartment model
Cytochrome P450 enzyme system – frequently deactivates drugs; liver enzyme involved
in metabolism.
Half-life (t 1/2) – the time it takes half of a drug to be cleared from the blood.
It takes approximately eight half-lives for a drug to be completely eliminated from
the body.

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

Geriatric practice – elderly patients


Stomach acidity is decreased – higher pH, affecting drugs that need a highly acidic
(low pH) environment for absorption
Higher body fat content, drugs that are highly fat-soluble may distribute well and
accumulate
Decreased kidney and liver function, affecting elimination dramatically
Decreased doses, increased dosing frequency to accommodate altered absorption,
distribution, and elimination

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