chamberlain college of nursing nr565 week 1 lesson notes nr 565 week 1 lesson notes advanced pharmacology fundamentals latest
2020
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Chamberlain College of Nursing
NR 565 (NR565)
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NR565 Week 1 Lesson Notes
Pharmacodynamics: The study of how drugs affect the body. Places emphasis on dose
response relationships, that is, the relationship between drug concentration at the site of
action and the resulting effect, including the time course and intensity of therapeutic and
adverse effects.
Pharmacokinetics: The study of how the body affects the drug.
Together they both influence dosing, benefit and adverse effects.
Receptors: The effect of a drug present at the site of action is determined by that drug's
binding with a receptor. Receptors may be present on neurons in the central nervous
system (i.e., opiate receptors) to depress pain sensation, on cardiac muscle to affect the
intensity of contraction, or even within bacteria to disrupt maintenance of the bacterial
cell wall. For most drugs, the concentration at the site of the receptor determines the
intensity of a drug's effect. The integration of the drug at the receptor site is the main
event that initiates the action of the drug prescribed. We as providers are interested in
how drugs that we prescribe effect the body. Drugs can mirror or block normal
physiological and biochemical processes or block pathological processes in animals or
stop vital processes of endo-or ectoparasites and microbial organisms.
Drugs can have a(n):
Stimulating action through direct receptor agonism and downstream effects.
Depressing action through direct receptor agonism and downstream effects (ex.:
inverse agonist).
Antagonizing (blocking) action; (as with silent antagonists), the drug binds the
receptor but does not activate it.
Stabilizing action, the drug seems to act neither as a stimulant or as a depressant
(ex.: some drugs possess receptor activity that allows them to stabilize general receptor
activation, like buprenorphine in opioid dependent individuals or aripiprazole in
schizophrenia. All depending on the dose and the recipient).
Exchanging or replacing substances or accumulating them to form a reserve such
as: glycogen storage.
Direct beneficial chemical reaction as in free radical scavenging.
Direct harmful chemical reaction which might result in damage or destruction of
the cells, through induced toxic or lethal damage (cytotoxicity or irritation).
The desired activity of a drug is mainly due to successful targeting of one of the
following:
• Cellular membrane disruption
• Chemical reaction with downstream effects
• Interaction with enzyme proteins
• Interaction with structural proteins
• Interaction with carrier proteins
, • Interaction with ion channels
• Ligand binding to receptors:
Pharmacodynamics Video: What the drug does to the body. Involves 3 mechanisms of
action 1: Receptor, 2: Enzyme. 3 Nonselective interactions.
Receptor Interactions: Occur at the cell receptor site, usually a protein structure within
the cell membrane. Receptor sites vary as to the substances they attract and the degree to
which they attract them. Ex: Ca Channel blockers which block the flow of calcium at the
receptor site leading to a reduction in muscle contraction therefore reducing HTN. When
multiple drugs seek to interact with the receptor the one with the strongest affinity for
that receptor will have the greatest response and be absorbed in higher concentration,
leaving more of the other substance as a free drug in the circulation.
Enzyme Interactions: Mostly seen in relation to the metabolism of drugs. Enzymes act
as catalysts in nearly every chemical reaction that takes place in the cells. Dugs can
enhance or inhibit the catalytic actions of these enzymes and this affects both the drug
action and the time required for its elimination. Ex: Drug toxicity can occur when
consuming large amounts of grapefruit juice while taking Statin drugs. Constituents in
the juice interfere with a liver metabolic enzyme preventing the proper break down of
these drugs. This increases the concentration of the statin and can cause rhabdomyolysis.
Grape fruit juice can also effect nifidipine and buspirone decreases metabolism of these
drugs which cause increase in their effects.
Nonselective Interactions: Occur when drugs chemically alter or physically interfere
with cellular structures or their processes. Ex: Chemotherapy. Cancer cells proliferate
more rapidly than healthy cells, so many chemo drugs act by attacking rapidly
proliferating cells, both cancerous and noncancerous. The N/V commonly seen with
chemo is caused by the nonselective drug action on the healthy, rapidly proliferating cells
in the GI tract.
Therapeutic index: Concentration in the body at which the drug performs the desired
action without becoming toxic.
Drug-drug Interactions: Can occur during any of the four phases of pharmacokinetics,
absorption, distribution, metabolism, or excretion, but usually occur when two drugs are
in competition for the same metabolizing enzyme.
Leafy Dark Greens (Spinach): Contain vitamin K which counters the effect of warfarin.
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