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21 Cards in this Set

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What are the four levels of drug action described in class?
Molecular, cellular, tissue, and system.
Do drugs only stimulate receptors, or can they block them too?
They can also block them.
Where do histamine H2 receptor antagonists work?
At the H2 receptors in the stomach wall.
How can antibodies be involved with pharmacology?
They can be used as receptor blockers.
What are two ways that agonist effects are potentiated (what a dumb word)?
1. By allosteric mechanisms which enhance receptor affinity.
2. By inhibition of agonist inactivation (ie. inhibition of removal of neurotransmitter from synapse).
What effects do calcium ion channel blockers have?
They reduce the contractility of the heart muscle, and also dilate the blood vessels, reducing the load that the heart pumps against. This helps with dysrhthmias, hypertension, etc.
What is the effect of inhibiting sodium entry?
Action potentials are blocked (can't reach threshold voltage).
What is the effect of inhibiting the Na+/K+ pump?
Ca2+ builds up, yielding a positive inotropic effect.
What are 5 ways that drugs can act on enzyme targets?
1. Can mimic enzyme product.
2. Can serve as enzyme substrate.
3. May be changed to altered product.
4. May inhibit enzyme.
5. May alter enzyme abundance.
What is an antimetabolite?
An antimetabolite is a chemical with a similar structure to a substance (a metabolite) required for normal biochemical reactions, yet different enough to interfere with the normal functions of cells, including cell division.
What 4 classes of enzyme-inhibiting drugs were discussed in the notes?
Cholinesterase inhibitors, cyclo-oxygenase (COX) inhibtors, and phosphodiesterase inhibitors, and angiotensin-converting enzyme (ACE) inhibitors.
What do cholinesterase (AChase-1) inhibitors do on a micro and macro level?
On a micro level, they prevent the breakdown of acetylcholine. On a macro level, they mimic an increase in parasympathetic activity.
What does inhibition of the COX enzymes do?
It reduces inflammation and pain.
What is the generalized name for COX inhibitors?
NSAIDs (non-steroidal anti-inflammatory drugs).
What are a couple of non-selective NSAIDs?
Aspirin and ibuprofen.
What is an example of a COX-II inhibitor?
Celebrex.
In general, what do phosphodiesterase inhibitors do?
They preserve cAMP & cGMP.
What are the results of preserving cAMP?
Positive inotropic effects, vasodilation, bronchodilation.
What are the results of preserving cGMP?
Enhances NO vasodilation, anti-anginal, treats erectile dysfunction.
What do ACE inhibitors do on the micro scale?
They prevent formation of angiotensin II, and reduce breakdown of bradykinin.
What do ACE inhibitors do on the macro scale?
They lead to vasodilation, which can treat hypertension and heart failure.