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26 Cards in this Set
- Front
- Back
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The action of parasympathomimetic agents act through what receptor in what capacity? |
They act as cholinergic agonists. |
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Why don't we give ACh directly as a cholinergic agent? |
It breaks down too quickly and has too brief an action. Thus we give a drug that breaks down more slowly. |
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Other than giving a cholingeric agent, what other way can we affect conditions that need a cholinergic innervation? |
We can reduce the breakdown of naturally occuring ACh so that it has a greater chance of meeting the correct receptor to elicit it's action. |
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In addition to reducing the breakdown rate of ACh, what other change can we effect on ACh to in crease its efficacy. |
We can increase the rate of ACh release so that there is a greater amount of natural ACh present. |
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We reduce the breakdown rate of ACh by giving anticholinesterases. What two varieties do these drugs come in? |
They come as reversible anticholinesterases and irreversible anticholinesterases. |
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What is an example of an irreversible anticholinesterase? |
Organophosphorous compounds and nerve gases that keep ACh in high abundance. |
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What are some examples of reversible anticholinesterases? |
Edrophonium, physostigmine, neostimine, and pyridostigmine |
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What do anticholinesterase drug names normally end in? |
-stigmine |
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How are cholinergic drugs given? |
They are normally injected because they are charged compounds that don't absorb well through the intestine and they do not cross the BBB. |
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What anticholinesterase passes well through the skin? |
Organophosphates. |
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Anticholinesterase drugs cause a decrease in blood pressure but what is the initial reaction? |
An increase in BP due to the affect of there being increased cGMP which increases intracellular Ca and activates smooth muscle which causes vasoconstriction. |
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What does it mean to say that the nicotinic receptor shows escape? |
It means that when the dosage of a cholinergic drug becomes high enough that the action of the drug will stop showing. It shows inhibition of the chosen action. |
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Where do you typically see escape? |
You see it at the level of the skeletal muscle or the diaphragm. |
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What is PAM or pralidoxime used for? |
The treatment of organophosphate compounds by binding to the compound and dragging it away from being able to complex with the receptor. |
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How does the treatment with a cholinergic drug help with the treatment of open angle glaucoma? |
The contraction of the ciliary body which pulls on the canals to open up the outflow more. |
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How do we treat ED? |
We block the action of phosphodiesterase which in doing so we maintain the action of cGMP which is induced by the action of ACh. |
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What would cause the blockade of an autonomic ganglia? |
The injection of highly concentrated |
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Control at most organs is under the control of which portion of the nervous system? (Which system has the exception?) |
Parasympathetic. The exception is the blood vessels |
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At high doses of nicotine, what happens to the drug as it spills over? |
It starts to act on the muscarinic receptors causing muscle issues. |
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What is the effect of nicotine at low dose? |
Activation at the level of the ganglia and resultant NE that is released at the second neuron that causes tachycardia and increased blood pressure. |
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How can we use nicotine in clinical practice? |
Blockade of the sympathetic ganglia in order to stop the release of NE at the level of the organ so as to bring down blood pressure.
Or in the treatment of smoking and removal of nicotine addication. |
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At high enough doses, nicotine spreads not only to the NMJ but where else does it go? |
It heads to the ganglia where it can cause cross stimulation with the sympathetic nervous system. |
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If the drug has chol in it, what type of drug is it? |
Direct acting cholinergic drug. |
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What is the one naturally occuring cholinergic direct acting drug? |
Pilocarpine |
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List the reversible anticholinesterases. |
Edrophonium and drugs ending in stigmine such as physostimine, neostimine, and pyridostigmine. |
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What is trimethaphan used for the treatment of? |
It is used in the blockade of autonomic ganglia. |
