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44 Cards in this Set

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Which drugs activate the cholinergic system?
All drugs activate cholinergic system
How can we classify drugs that act on the cholinergic system based on their method of action?
Can be classified as drugs that act directly and indirectly on the the cholinergic system
What kind of cholinergic system direct acting drugs are there? and how do they work?
manmade and natural drugs. These drugs affect the cholinereceptor directly
How do drugs that act indirectly affect the cholinergic system?
By interfering with a catabolic enzyme which would have broken down ACH therefore the ACH (cholinergic) receptors are stimulated
What kind of drugs are there that indirectly act on the cholinergic system?
Reversible (non-covalent binding) and Irreversible (covalente binding)
ACETYLCHOLINE
Non-specific drug - fast acting - affects all cholinergic receptors
What kind of drug is MIOCHOL?
It is a cholinergic drug it is acetylcholine chloride.
Hos is MIOCHOL used?
It is used before ocular surgery to cause the ciliary muscle to constrict pupils
Are all direct acting cholinergic drugs reversible or irreversible?
They are reversible.
CARBACHOL - kind of drug, method of action, structure and significance of structure
direct acting synthetic cholinergic drug, causes pupillary constriction, has a carbonic acid derivaty at the end of acetylcholine - which makes it more resistant to acetylcholesterase degradation.
What is Isopto-carbachol and how is it used?
It is a derivative of Carbachol, Used for open angle glaucoma.
What are the ADRs for "ALL" cholinergic drugs?
Flushing, Sweating, GI, Urinary urgency, headache, salivation, ciliary spasms
What is one important ADR of carbachol?
Bronchial constriction. Asthma not a contraindication, however, caution with asthma patients.
What are nicotinic acetylcholine receptors?
receptors activated by both acetylcholine and nicotine (an alkaloid)
A cholinergic drug could have a sympathomimetic or parasympathomimetic effect?
Parasympoathomimetic
>------ ACH ------<ACH [Parasympathetic fibers]
Parasympathetic fibers
BETHANECOL , type of cholinergic drug, structure, ADRs, contraindications, use
Cholinergic synthetic drug, It has a carbonic acid and methyl group on acetylcholine, same ADRs as carbechol, contraindicated in asthma, use in NONOBSTRUCTIVE urinary retention.
PILOCARPINE, type of cholinergic drug, structure, use
Cholinergic natural drug (from plant), not too similar to acetylcholine, used for open-angle glaucoma (pilocarpine occular therapeutic system)
What two drugs are used in open-angle glaucoma?
Isopto-carbachol and pilocarpine
One is a derivative of another cholinergic drug and the other used to be used in ordeal trials.
NICOTINE , mechanism, use,
Natural cholinergic drug, It activates the following cholinergic receptors: autonomica gnaglia, muscular junctions, brain, adrenal medulla, It is used to stop smoking habit (no otc nicotine medication)
How does nicotine stimulate the cerebral cortex?
via the locus coruleus
What effect does nicotine have on the limbic system?
It stimulates the pleasure/reward action via dopamine release (direct and indirect stimulation)
Nicotine stimulates CV ganglia, what are some of the symptoms of this stimulation?
peripheral vasoconstriction, tachycardia and increased BP
What kind of drug is physostigmine?
It is an indirect rversible cholinergic drug
In what two forms can physostigmine be found?
Topical = ESERINE
Systemic = ANTILIRIUM
ESERINE , type of drug, use,
Topical form of physostigmine - an indirect reversible cholinergic drug, reverses cycloplegia / mydriasis and it's an alternate treatment for open-angle glaucoma.
ANTILIRIUM type of drug, use, adverse effects
Systemic form of physostigmine an indirect cholinergic drug. Antidote to toxic neurologic effects of caused by drugs with central anticholinergic activity. Highly lipid soluble - penetrates CNS. Adverse effects: sweating, n/v, urinary urgency, cramping, salivation, diarrhea, muscle weakness, hypotension, bradychardia, convulsions,bronchospasms, resp. paralysis.
DEMECARIUM: use
Indirect reversible cholinergic drug. Topical use only, used for glaucoma
What are the signs of a cholinergic crisis?
Nausea, diarrhea, sweating, increased bronchial and salivary secretions, bradychardia, muscle weakness,
What is the acetylcholinesterase inhibitor antidote?
Pralidoxime
What are some signs of CNS toxicity from indirect cholinergic drugs?
Jitterness, confusion, dizziness
What drug do we use to counteract cholinergic CNS toxicity?
atropine (a classis anti-cholinergic drug)
AMBENONIUM use, mechanism, ADRs
A systemic indirect reversible acetylcholynesterase inhibitor. Used for diagnosis/treatment of myasthenia gravis, it works by increasing cholinergic transmission at the neuromuscular junction. ADRs = possible cholinergic crisis with overdose and typical cholinergic CV adverse effects.
EDROPHONIUM use, mechamism, ADRs
A systemic indirect reversible acetylcholinesterase inhibitor. Used for treatment/diagnosis of myasthenia gravis and to underdose/oversode of cholinergic drugs in myasthenia gravis patients. It works by increasing cholinergic transmission at the neuromuscular junction. ADRs = possible cholinergic crisis with overdose and typical cholinergic CV adverse effects.
NEOSTIGMINE - use, mechanism
A systemic indirect reversible acetylcholynesterase inhibitor. Used for diagnosis/treatment of myasthenia gravis, it works by increasing cholinergic transmission at the neuromuscular junction IT DOES NOT CROSS THE BBB and it exhibits ACH-like stimulating effect at the neuromuscular junction, therefore it can reverse skeletal muscle blockade. ADRs = possible cholinergic crisis with overdose and typical cholinergic CV adverse effects.
Which direct cholinergic drug does not cross the blood brain barrier?
NEOSTIGMINE
Which direct cholinergic drug exhibits direct ACH-like stimulating effect at the neuromuscular junction?
NEOSTIGMINE
PYRIDOSTIGMINE use, mechanism ADRs
A systemic indirect reversible
cholinergic drug (acetylcholynesterase inhibitor). Used for diagnosis/treatment of myasthenia gravis and as prophylaxis by the military to prevent nerve gases from binding, it works by increasing cholinergic transmission at the neuromuscular junction. ADRs = possible cholinergic crisis with overdose and typical cholinergic CV adverse effects.
Which indirect cholinergic drug is used by the army as prophylaxis to lessen nerve gas from binding to ACH receptor upon exposure?
PYRIDOSTIGMINE
Name three general features of irreversible acetylcholinestarase inhibitors
Highly lipid soluble - organo-phosphorous compounds - used widely as pesticides and insecticides
ECOTHIOPHATE use
An irreversible acetylcholinesterase inhibitor drug. Used for glaucoma both open-angle and angle-closure GLAUCOMA
Which cholinergic drug is used for angle-closure glaucoma? and what type of cholinergic drug is it?
ECOTHIOPHATE . It is an indirect cholinergic drug - irreversible acetylcholinesterase inhibitor.
ISOFLUROPATHE
This irreversible acetylcholinergic drug belongs to the fluoride group which makes the molecule more active and lasts longer.
SARIN use
Nerve gas, irreversible acetylcholinesterase inhibitor.
PRALIDOXIME use, mechanism
Antidote for acetylcholinesterase. It acts by hydrolyzing the phosphorylated enzyme, if the complex has not "aged"