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Pharmacology: the study of drugs and how it interacts with the body. -…
Pharmacology:
the study of drugs and how it interacts with the body.
Pharmacodynamics:
What the drug does to the body.
What the drug targets
What the drug
blocks/activates
What the
effects
it
produces
Agonist:
activates the Receptor.
Full:
Maximum possible outcome
Partial:
Partial outcome
Selective:
Binds to specific chemical signals, but not all of it.
Inverse:
Binds to a specific receptor but does the opposite effect of the agonist. Lowers the baseline activity.
Antagonist:
Blocks the receptor. Prevents/reduces agonist activity.
Competitive:
Competes with agonist to the same binding sites. Can be overcome/overpowered by more agonist.
Non-competitive:
Binds to a different binding site (allosteric site) to change how the receptor functions. Cannot be overpowered by more agonists.
Inverse agonist VS. antagonist
: Inverse agonist reduces the baseline activity. Antagonist simple blocks the activity from increasing, the baseline activity stays the same.
Therapeutic effect:
desired effect
of the medication
Dose-response relationship:
How changing the amount of a drug affect the response produced in the body.
Side effects:
an
unintended
effect. an additional effect that is
not
the
intended
therapeutic/desired effect.
not necessarily dangerous.
toxicity:
Harmful effects that occur when drug exposure becomes excessive or the drug causes toxic injury.
Dose increase ➡️ Therapeutic effect ➡️ unwanted effects may increase ➡️ excessive exposure ➡️
toxicity
More drug ➡️ generally produces a greater response,
up to a point.
Potency VS. Efficacy
Efficacy:
The maximum effect a drug can produce. how well a drug works at its best.
Potency:
How much a drug is needed to produce a particular effect. how strong/potent the dose is.
amount needed for an effect
But just because a drug is more potent doesn't mean it "works better". More potent ≠ greater efficacy
maximum effect it can produce
Example: -
Pill A
needs Just
5 mg
to completely stop pain.
Pill B
needs
50 mg
to stop pain. Both pills stop 100% pain,
same efficacy
. But
Pill A
is
more potent
(smaller mg) because it stopped the pain at a
smaller amount
.
affinity:
is how strongly a drug binds to its receptor
therapeutic window:
The safe and range of a drug's dosage without causing dangerous side effects. The "sweet spot"
Journey of the drug: once absorbed through the bloodstream and distributed.
Drug reaches the target tissues/organs
Receptor binding. Affinity
Activates Agonist
Receptor response
Mechanism of action
Cell/Physiological resonse
Therapeutic effect
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Blocks. Antagonist
Pharmacokinetics:
What the body does to the drug.
ADME
Absorption:
How the drug gets
into
the bloodstream.
Distribution:
How the drug
travels
through your bloodstream to
reach
target cells molecules.
once distributed and drugs are in target tissues/organs, the effect happens
Metabolism:
How the body (mostly the liver) chemically changes the drug.
Excretion:
How the body gets rid of the drug.
several exit routes
Lungs/Exhalation:
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enzymes:
a special protein that helps speed up the chemical reactions in the body.
Vocabs & definitions
metabolite:
When the body chemically changes a drug into another substance
The body modifies the drug so the drug can be
processed
and eventually
eliminated
(excretion).
First-pass metabolism:
Some orally absorbed drug is metabolized by the liver before reaching systemic circulation.
drug goes to the
Liver
(Major site of drug metabolism)
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Lipid-soluble:
a substance capable of dissolving in fats, oils, or waxy natural molecules that does not dissolve in water.
water-soluble:
capable of dissolving in water.
CYP450:
a large family of enzymes (mostly found in the liver), that breaks down drugs, natural body chemicals, and toxins.
But the drug doesn't automatically renders as inactive.
active
drug ➡️
inactive
metabolite
active
drug ➡️
active
metabolite
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The drug works ➡️ the body metabolizes it ➡️ it no longer has the same pharmacological activity
drug moves from blood to tissues
anatomical barriers
found in certain organs can hinder the way the drug travels through the body. Some drugs can pass, some cannot.
Blood-brain barrier:
Blood-placental barrier:
Blood-testicular barrier:
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Free VS. Bound drug
Protein-Bound drug:
Attached to proteins like
albumin
It is not necessarily inactive or useless, just less immediately available to leave the bloodstream. It can
reversibly detach and become
free.
Free/unbound drug:
moves much more freely in the bloodstream. They can: leave the bloodstream & distribute into tissues, reach its target, be metabolized, be excreted.
Half-life:
How long it takes for the amount of drug in your body to decrease by half.
Bioavailability:
a part/portion of the drug that is successfully absorbed into the
systemic circulation (bloodstream)
Not all of the administered drug reaches the target point with 100%
But if the drug is
injected directly
into
the bloodstream
, then the bioavailability is 100%
reasons why it won't be 100%
A drug can be:
incompletely absorbed.
broken down in the GI tract
metabolized by the intestinal wall
metabolized by the liver before reaching systemic circulation
metabolism can decrease the half-life of a drug
Pharmacodynamics & pharmacokinetics time line
Absorption
Bloodstream
First-pass metabolism
systemic circulation
Distribution
Free/unbound Drug
target site
pharmacodynamic
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Protein-bound