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44 Cards in this Set
- Front
- Back
- 3rd side (hint)
Which drugs activate the cholinergic system?
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All drugs activate cholinergic system
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How can we classify drugs that act on the cholinergic system based on their method of action?
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Can be classified as drugs that act directly and indirectly on the the cholinergic system
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What kind of cholinergic system direct acting drugs are there? and how do they work?
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manmade and natural drugs. These drugs affect the cholinereceptor directly
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How do drugs that act indirectly affect the cholinergic system?
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By interfering with a catabolic enzyme which would have broken down ACH therefore the ACH (cholinergic) receptors are stimulated
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What kind of drugs are there that indirectly act on the cholinergic system?
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Reversible (non-covalent binding) and Irreversible (covalente binding)
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ACETYLCHOLINE
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Non-specific drug - fast acting - affects all cholinergic receptors
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What kind of drug is MIOCHOL?
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It is a cholinergic drug it is acetylcholine chloride.
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Hos is MIOCHOL used?
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It is used before ocular surgery to cause the ciliary muscle to constrict pupils
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Are all direct acting cholinergic drugs reversible or irreversible?
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They are reversible.
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CARBACHOL - kind of drug, method of action, structure and significance of structure
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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.
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What is Isopto-carbachol and how is it used?
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It is a derivative of Carbachol, Used for open angle glaucoma.
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What are the ADRs for "ALL" cholinergic drugs?
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Flushing, Sweating, GI, Urinary urgency, headache, salivation, ciliary spasms
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What is one important ADR of carbachol?
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Bronchial constriction. Asthma not a contraindication, however, caution with asthma patients.
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What are nicotinic acetylcholine receptors?
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receptors activated by both acetylcholine and nicotine (an alkaloid)
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A cholinergic drug could have a sympathomimetic or parasympathomimetic effect?
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Parasympoathomimetic
>------ ACH ------<ACH [Parasympathetic fibers] |
Parasympathetic fibers
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BETHANECOL , type of cholinergic drug, structure, ADRs, contraindications, use
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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.
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PILOCARPINE, type of cholinergic drug, structure, use
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Cholinergic natural drug (from plant), not too similar to acetylcholine, used for open-angle glaucoma (pilocarpine occular therapeutic system)
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What two drugs are used in open-angle glaucoma?
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Isopto-carbachol and pilocarpine
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One is a derivative of another cholinergic drug and the other used to be used in ordeal trials.
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NICOTINE , mechanism, use,
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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)
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How does nicotine stimulate the cerebral cortex?
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via the locus coruleus
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What effect does nicotine have on the limbic system?
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It stimulates the pleasure/reward action via dopamine release (direct and indirect stimulation)
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Nicotine stimulates CV ganglia, what are some of the symptoms of this stimulation?
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peripheral vasoconstriction, tachycardia and increased BP
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What kind of drug is physostigmine?
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It is an indirect rversible cholinergic drug
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In what two forms can physostigmine be found?
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Topical = ESERINE
Systemic = ANTILIRIUM |
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ESERINE , type of drug, use,
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Topical form of physostigmine - an indirect reversible cholinergic drug, reverses cycloplegia / mydriasis and it's an alternate treatment for open-angle glaucoma.
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ANTILIRIUM type of drug, use, adverse effects
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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.
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DEMECARIUM: use
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Indirect reversible cholinergic drug. Topical use only, used for glaucoma
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What are the signs of a cholinergic crisis?
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Nausea, diarrhea, sweating, increased bronchial and salivary secretions, bradychardia, muscle weakness,
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What is the acetylcholinesterase inhibitor antidote?
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Pralidoxime
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What are some signs of CNS toxicity from indirect cholinergic drugs?
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Jitterness, confusion, dizziness
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What drug do we use to counteract cholinergic CNS toxicity?
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atropine (a classis anti-cholinergic drug)
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AMBENONIUM use, mechanism, ADRs
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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.
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EDROPHONIUM use, mechamism, ADRs
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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.
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NEOSTIGMINE - use, mechanism
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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.
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Which direct cholinergic drug does not cross the blood brain barrier?
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NEOSTIGMINE
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Which direct cholinergic drug exhibits direct ACH-like stimulating effect at the neuromuscular junction?
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NEOSTIGMINE
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PYRIDOSTIGMINE use, mechanism ADRs
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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. |
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Which indirect cholinergic drug is used by the army as prophylaxis to lessen nerve gas from binding to ACH receptor upon exposure?
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PYRIDOSTIGMINE
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Name three general features of irreversible acetylcholinestarase inhibitors
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Highly lipid soluble - organo-phosphorous compounds - used widely as pesticides and insecticides
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ECOTHIOPHATE use
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An irreversible acetylcholinesterase inhibitor drug. Used for glaucoma both open-angle and angle-closure GLAUCOMA
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Which cholinergic drug is used for angle-closure glaucoma? and what type of cholinergic drug is it?
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ECOTHIOPHATE . It is an indirect cholinergic drug - irreversible acetylcholinesterase inhibitor.
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ISOFLUROPATHE
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This irreversible acetylcholinergic drug belongs to the fluoride group which makes the molecule more active and lasts longer.
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SARIN use
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Nerve gas, irreversible acetylcholinesterase inhibitor.
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PRALIDOXIME use, mechanism
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Antidote for acetylcholinesterase. It acts by hydrolyzing the phosphorylated enzyme, if the complex has not "aged"
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