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47 Cards in this Set

  • Front
  • Back
-useful for managing urinary retention
-used to decrease esophageal tone in patients with GERD and reflux esophagitis
-May be useful as an agent to test for and aid in the diagnosis of asthma (methacholine challenge)
-Also useful for chronic myasthenia gravis
-Treatment of glaucoma, decreases intraocular pressure
-Treatment of glaucoma, decreases intraocular pressure
-induces salvation for the treatment of dry-mouth due to Sjogren's Syndrome
-Use in smoking cesssation by indirectly stimulating the mesolimbic dopamine system in the CNS impt. to reward experience of smoking.
-Useful for treatment of Alzheimer's disease
-Well known drug-induced hepatotoxicity
-Useful for patient's with Alzheimer's disease
-Useful in the diagnosis of myasthenia gravis
-Useful for patient's with Alzheimer's disease
-Useful for urinary retention
-Useful for chronic myasthenia gravis
-Useful for chronic myasthenia gravis
-Useful for patient's with Alzheimer's disease
Which cholinergic drugs are useful for patient's with Alzheimer's disease?
Galantamine, Rivastigmine, Donepezil, Tacrine
Which cholinergic drugs are useful for myasthenia gravis?
Edrophonium, Pyridostigmine, Rivastigmine
Which 2 cholinergic drugs are useful for treatment of glaucoma?
Carbachol, pilocarpine
Which 2 cholinergic drugs are useful for urinary retention?
Bethanechol, Neostigmine
Which two drugs are completely resistant to acetylcholinesterase?
Bethanechol and Carbachol
Which drug is less suspectible to acetylcholinesterase degradation?
Name two types of chemical modifications that have been made to acetylcholine?
1. Addition of a methyl side-chain and
2. Modification of the ester moiety of ACh to a carbamic ester
Name the two cholinergic drugs which are carbamic acid moiety?
Carbachol and Bethanechol
Name the two cholinergic drugs which have more selectivity for muscarinic receptors and why?
Methacholine and Bethanechol have significant muscarinic selectivity because they are the ACh to which a methyl side chain has been added to the beta-carbon.
Which 2 alkaloids are found in nature?
Pilocarpine and muscarine
Pilocarpine is a tertiary amine, why is this important?
Muscarine, due to it's permanently charge quaternary amine moiety, has limited absorption relative to pilocarpine, which is a tertiary amine.
Which cholinergic drug has selectivity for neuronal nicotinic receptors?
Which 2 cholinergic drugs are reversible ACh inhibitors which bind competetively in a non-covalent manner, acts like ACh by binding to the active site of AChE in a noncovalent manner?
Edrophonium and Galantamine
Which 2 cholinergic drugs are Reversible noncompetitive (non-classic) AChE inhibitors?
Tacrine and Donepezil
Name 3 cholinergic drugs which are slow reverisble and noncompetitive AChE inhibitors?
Neostigmine, pyridostigmine, and rivastigmine
What are irreversible AChE inhibitors called?
How do cholinergic drugs affect cardiac contractility?
Negative inotropic effect (decreases contractile strength) due to M2 stimulation in cardiac contractile cells
How do cholinergic drugs affect heart rate?
Negative chronotropic effect (decrease in HR) due to M2 stimulation at SA node
How do cholinergic drugs affect the lower respiratory tract?
Contraction of bronchial smooth muscle and increased mucous secretion due to M3 stimulation
How do cholinergic drugs affect the GI tract?
Increased peristalsis due to M3 stimulation
How do cholinergic drugs affect the Genitourinary tract?
Contraction of bladder wall muscle and relaxation of urinary sphincter resulting in increased ease of urination (M3 receptors)
How do cholinergic drugs affect the eye?
Contraction of pupillary constrictor muscle (miosis); contraction of ciliary muscle leading to outflow of aqueous humor and decrease in IOP (M3 receptors)
What is a short-acting AChE inhibitor?
Which 2 cholinergic drugs are used for chronic management of myasthenia gravis and why?
Pyridostigmine, Rivastigmine, and neostigmine because they are longer acting AChE inhbitors
Why is Varenicline useful for treatment of smoking?
It decreases craving by replacing the reward/pleasure experience secondary to cigarette smoking.
Symptoms of acute nicotine toxicity include:
convulsions, respiratory paralysis, hypertension, and cardiac arrythmias.
Toxicity of the direct-acting muscarinic cholinergic drugs are simply excess of usual pharmacological effects. These include:
excess salvation, miosis, sweating, nausea, vomiting, diarrhea, and bronchial constriction
Name the AChE inhibitor toxicities.
They are a combination of the toxicities seen from nicotine and the direct-acting muscarinic cholinergic drugs.
What is the most common cause of AChE inhibitor toxicity?
Accidental exposure to insecticides (many insecticides are organophosphates AChE inhibitors)
What can be used if there is acute poisoning of AChE inhibtors exposure to insecticides?
An Antidote such as pralidoxime (2-PAM), which may aid in the regeneration of AChE if the patient is treated quickly enough
What are the toxicities that Alzheimer's patients will experience when taking AChE inhibitors?
significant nausea and vomiting especially with Tacrine and rivastigmine
What happens if a patient is taking a anticholinergic drug with a cholinergic drug?
Drugs with anticholinergic effects may decrease the efficacy of cholinergic agents.
Name the 4 muscarinic ACh Receptor Agonist.
Bethanechol, Carbachol, Methacholine, Pilocarpine
Name the nicotinic ACh receptor Agonist.
Name the 7 AChE Inhibitors.
Donepezil, Tacrine, Edrophonium, Galantamine, Neostigmine, Pyridostigmine, and Rivastigmine