Exam -2 Cholinergic and Adrenergic drugs Flashcards
What is the drug that targets the antiporter enzyme for Acetylcholine? What deficit does it cause?
Vesamicol: it results in a deficit of Ach storage and subsequent release.
What does Hexamethonium do?
Selective blockade of the modulatory presynaptic cholinergic receptors by antagonism. It prevents facilitation and causes rapid tetanic fade to occur in muscles.
Atropine
Antimuscarinic agent. Can be use to block vagal slowing of the sinoatrial node, and hece in relative tachycardia occurs.
Methacholine
It is a muscarinic receptor agonist.
This drug attaches to M-1 muscarinic receptors (located in autonomic ganglia) with higer affinity than M-2 and M-3 receptors (located in parasympathetic end organs).
What’s the drug? and what’s the outcome?
Pirenzepine
The drug’s predominant effect at clinically used does is ganglionic blockae.
What drug we will use in the case of an anticholinergic overdose?
what kind of property makes it a good drug?
Physostigmine, it is a lipophilic agent which has excellent CNS penetration.
What kind of drug is Hemicholinium-3?
ACh inhibitor, this drug is used in research setting.
Blocks the high affinity transporter for choline and thus prevents the uptake of choline required for ACh sysntehsis.
This drug degraded SNAP-25and thus prevent synaptic vesicle fusion with the axon terminal (presynaptic) membrane.
Botulinum Toxin A. Made by Clostridium Botulinum.
Which AChE inhibitor has a direct action, and activates nAChRs at the neuromuscular junction?
Neostigmine
What drug is an AChE inhibitor that binds rapidly (2-10 min) , resulting in a complete rapid and reversible block?
Edrophonium. Often used clinically to diagnosed Myasthenia Gravis.
Properties of Diisopropyl Fluorophosphate , and Isoflurophate?
Possible drug administer to reverse effect?
It is an organophosphate. These irreversible bind to AChE, and act as an inhibitor (this is due to Aging) New AChE molecules need to be synthesize in order to restore activity. f
Pralidoxime is administered before aging has occurred, it is possible to recover enzymatic function from the inhibited AChE.
Tubocurare?
What can be used to improve conditions that mimic this drug?
Anticholinergic drug, cause weakness or paralysis by acting as competitive antagonist at the nAChR, preventing ACh from binding to the receptor and causing nondepolarizing blockade of cholinergic transmission.
An AChE inhibitor in order to increase ACh, that would be Physostigmine.
If we give a patient Edrophonium and muscle weakness decreases even further, what can we deduce? what drug must be in action?
It means that there is an agonist of AChR, there is a depolarizing blockade. The receptors are being stimulated so much, the go into blockade, the drug that can cause this is succinylcholine.
What are the drug indicated for the treatment of mild and moderate Alzheimer’s disease (AD)?
Don’t Take Rupaul Geerrrlll
Donepezil
Tacrine
Rivastigmine
Galantamine
These are AChE inhibitors
What drug is indicated to treat AD and Parkinson’s disease?
Rivastigmine is a pseudo-irreversible cholinesterase inhibitor.
Muscarinic recptor agonist?
Please Become My Cute Ass Muse
Pilocarpine Bethanechol Muscarine Carbachol Acetylcholine Methacholine
What drug is used for diagnosis of asthma?
Methacoline: the bronchial hyperreactivity that is characteristic of asthma causes an exaggeraed bronchoconstriciton response to parasympathomimetics.
This agent can not be used systemically because its nicotinic action at autonomic ganglia leads to unpredictable responses.
Instead it is used topically as tx of Glaucoma, what is the agent?
Carbacho (Muscarinic agonist) l. Local application of the drug to the cornea of the eye results in both pupillary constriction (miosis) and decreases intraocular pressure.
What’s the drug of choice for promoting GI and urinary tract motility, particularly for post-opertive, post partum, and drug-related urinary retention?
Bethanechol: is completely selesctive for mucarinic receptors.
What kind of drug we would use to treat Xerostomia?
A muscarinic agononist.
Pilocarpine, is a miotic agent as a sialagogue (saliva inducing agent) used to treat xerostomia.
What drug is used to induce paralysis during surgery?
A nicotinic receptor agonist, such as Succinylcholine (resistant to AChE) it causes depolarizing blockade as it is a strong nicotinic receptor agonist.
What is the Muscarinic antagonist drug of choice for its substantial CNS effects, antiemetic effects, and motion sickness?
Scopolamine, a tertiary amine.
What is the drug that is an alternative H2 receptor antagonist and can be used to treat peptic ulcer as well as decrease GI spams?
Methscopolamine and Glycopyrrolate
These are quaternary amine antimuscarinics with low CNS penetration that are used for their peripheral effects to decrease oral secretions, treat peptic ulcers, decrease GI spams, and in the case of glycopyrrolate, prevent bradycardia during surgical procedures.
What are the drugs used to treat over-reactive bladder?
Muscarinic antagonist.
Oxybutynin Propantheline Terodiline Tolterodine Fesoterodine Trospium Darifenacin Solifenacin
Ipratropium
(muscarinic antagonist) a synthetic quaternary ammonium compound, is more effective than beta-adrenergic agaonists in the treatment of chronic obstructive pulmonary disease, but less effective in treating asthma.
Tiotropium
(muscarinic antagonist) has recently been shown to have similar, and possibly superior efficacy to ipratropium as a bronchodilator in the treatment of COPD.
What are direct muscarinic agonist? which one of those is specific for relieving intraocular pressure from glaucoma?
Bethanechol
Methacholine
Pilocarpine
*Carbachol : constricts pupil and relieves intraocular pressure in glaucoma. Carbon copy of acetylcholine.
Indirect muscarinic agonist, they act as AChE inhibitors?
Donepezil, galantamine, rivastigmine Edrophonium Neostigminine Physostigmine Pyridostigmine
What would be the symptoms of a patient with organophosphate overdose?
They inhibit acetylcholinerterase, thus we will have an increase activity of Acetylcholine, we will see DUMBBELSS:
Defication (diarrhea) Urination Myosis Increase bowel activity Bradychardia Excitation Lacrimation Sweating Salivation
List some of the muscarinic antagonist?
Atropine, homotropine, tropicamide Benztropine (Park my Benz) -CNS Glycopyrrolate Hyoscyamine, dicyclomine Ipratropium(I pray can breathe)COPD/asthma Tiotropium Oxybutynin, solifenancin, tolterodine Scopolamine - CNS, motion sickness
What drug can cause acute angle-closure glaucoma in elderly (due to mydriasis)?
Atropine : side effects Hot as hare Dry as a bone Red as beat Blind as a bat Mad as a hatter
Direct sympathomimetics agonist?
Albuterol , salmeterol (B2>B1) Dobutamine Dopamine Epinephrine Isoproterenol Norepinephrine Phenylephrine
Indirect sympathomimetics?
Amphetamine
Cocaine
Ephedrine
If suspected cocaine intoxication, what is contraindicative and why?
Beta blockers, because it leads to unopposed alpha-1 activation and extreme HTN.
This drug is more effective in alpha 1>alpha2 >beta 1 receptors.
Norepinephrine: Hypotension (but decrease renal perfusion)
What does Clonidine do?
Given for hypertensive urgency (limited situations); does not decrease renal flow. (alpha 2 agonist). ADHD, Tourette syndrome.
Toxicity can cause CNS depression, bradycardia, hypotension, respiratory depression, miosis.
what does alpha-methyldopa do?
Apply in HTN in pregnancy. (alpha-2 agonist)
what are some of the nonselective alpha blockers?
AMINE : orthostatic hypotension, reflex tachy
Phenoxybenzamine : used for pheochromocytoma and preoperative to prevent hypertensive crisis.
Phentolamine: given to patients who are on MAO-I and have eaten food with tyramine
What are the selective alpha-1 blockers
ZOSIN and OSIN
Prazosin, terazosin, doxazosin, tamsulosin.
-urinary symptoms of BPH, PTSD (prazosin); hypertension (except tamsulosin).
What’s the alpha-2 blocker used to treat depression?
Mirtazapine: sedation, increase serum cholesterol, increase appetite.
What drug is indicative to block production of aqueous humor?
Beta-2 blocker.
How you we identified B-1 blockers from nonselective ones?
How about alpha and Beta antagonist?
A-M selective antagonist. B1:
Acebutolol (partial agonist), atenolol, betaxolol, esmolol, metoprolol.
Nonselective antagonist:
Nadalol, pindolo (partial agonist), propranolol, timolol.
Nonselective alpha.beta antagonist are Carvedilol, labetalol. Suffix ends in “alol -ilol”
What is tropicamide?
An antimuscarinic drug
What is the effects of Aminoglycoside antibiotics?
It has been found that aminoglycosides block the voltage activated Ca+ channels. These are needed in order for the vesicles filled with AChE to release its contents. If this doesn’t occur, no AChE will be found in the synaptic cleft. The patient was being treated for a bacteria infection, that causes weakness. But this weakness is even worse than expected because on top of that she also has Myasthenia Gravis. So her receptors are not working and then, ACh is not being released.
