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Auto Pharm Meds

ANS Pharmacology Drugs

QuestionAnswer
What drugs are Direct Acting Muscarinic Agonist Choline Esters? Betanechol, Carbachol, Methacholine
What drugs are Direct Acting Muscarinic Agonists? Muscarine, Pilocarpine
What drug is a Muscarinic Antagonist that treats diarrhea? Atropine
What drug is a Muscarinic Antagonist that treats nausea? Scopolamine
What are the differences between Atropine & Scopolamine? Atropine stimulates the heart, has minor CNS effects, and the L-isomer is Hyoscyamine. Scopolamine has strong CNS effects b/c it crosses the BBB & causes drowsiness, L-isomer is hyoscine.
What Direct Acting Muscarinic Agonist is the best to treat urinary retention? Betanechol b/c it doesn't stimulate Nicotinic Receptors
What Direct Acting Muscarinic Agonists treat glaucoma? Carbachol, Pilocarpine
What are the natural alkaloids of Direct Acting Muscarinic Agonists? Muscarine, Pilocarpine
What are 2 drugs that are Muscarinic Antagonists that treat COPD? Ipratropium, Tiotropium
Why can Tiotropium be used to treat asthma along with COPD? Tiotropium is M3-R selective. M3 specifically bronchodilates.
What do Methscopolamine Br & Homatropine Methylbromide treat? GI spasms & IBS
What is Glycopyrrolate used for? Anesthesia - anti-Vagal
What does Pirenzepine treat? Acid-peptic disorders, ulcers. M1&M4 selective
What drugs are Muscarinic Antagonists that treat urinary incontinence? Darifenacin, Oxybutynin, Tolterodine
What are the differences between the urinary incontinence Muscarinic Antagonists? Darifenacin is M3 selective & also treats fecal incontinence. Oxybutynin & Tolterodine aren't selective, relax the detrusor mm.
What Muscarinic Antagonists treat Parkinson's? How are they able to do this? Benztropine, Trihexyphenidyl, Biperiden, Procyclidine. They are able to cross the BBB.
What Muscarinic Antagonists are receptor selective? Tiotropium, Pirenzepine, Darifenacin
What are the side effects of stimulating Muscarinic Receptors? Parasympathetic effects: SLUDGE, bradycardia, bronchoconstriction, hypotension, miosis
What are the side effects of blocking Muscarinic Receptors? Sympathetic effects: tachycardia, hypertension, bronchodilation, constipation, urinary retention, mydriasis, cyclopegia, dry mouth
What is the SNS exception for NT & Receptor? Sweat glands. ACh-R are stimulated.
What Muscarinic Receptors stimulate? M1, 3, 5. Use Phospholipase C (PLC) as a 2nd messenger.
What Muscarinic Receptors inhibit? M2, 4. Inhibit adenylate cyclase, open K+ & close Ca2+ channels.
What drugs are Cholinesterase Inhibitors (Indirect Cholinergic Agonists) that treat glaucoma? Echothiophate, DFP
What Cholinesterase Inhibitors (Indirect Cholinergic Agonists) treat Myasthenia Gravis? Neostigmine, Pyridostigmine, Ambenonium, Edrophonium
How is Edrophonium used? If administered to patient & they feel better, diagnosis of MG. If already diagnosed: if administered & feel better pt is underdosed; if administered & feel worse pt is overdosed.
Physostigmine, Tacrine, Donepezil, Galantamine are what type of drugs & what do they treat? They are Cholinesterase Inhibitors (Indirect Cholinergic Agonists) that can cross BBB, and they treat Alzheimer's
Parathion, Malathion, Sevin, Chlorpyriphos are what? Cholinesterase Inhibitors (Indirect Cholinergic Agonists) that are used as bug poisons
Sarin, Soman, VX are what? Cholinesterse Inhibitors (Indirect Cholinergic Agonists) that are used as human poisons
What is a side effect of inhibiting Acetylcholinesterase? An increase in skeletal muscle contractions (fasciculations)
How do quaternary amines inhibit AChE, and what is an example drug? They bind to AChE for a very short amount of time & just go away. Edrophonium is an example
How do carbamates inhibit AChE, and what is an example drug? They bind to AChE, and break into 2 pieces. 1 piece stays attached to the esteratic site until it's hydrolyzed by water. At this point it will go away. This is intermediate to long acting. Example drugs are neostigmine & physostigmine
How do organophosphates inhibit AChE, and what is an example drug? They bind to the esteratic site & 1 isopropyl group leaves after being hydrolyzed. This causes the OP to stay bound and this is irreversible. An example is DFP
If given an OP, how would you stop the permanent "killing" of AChE? Administer 2-PAM before the OP is hydrolyzed. 2-PAM will bind to the OP & fill the anionic site. The combined molecules can then go away
Why would you treat glaucoma with a Muscarinic Agonist? M3 stimulation promotes drainage by contracting the ciliary & iris muscles (miosis)
Why would you treat glaucoma with a B2 Antagonist? B2 promotes the production of the aqueous humor, so if it's blocked, there will be no fluid buildup
Why would you treat glaucoma with an A2 Agonist? A2 helps drainage & reduce fluid buildup
What are the drugs that are Ganglionic Blockers & used to treat acute dissecting aortic aneurysm? Hexamethonium, Mecamylamine, Tetraethylammonium
Succinylcholine, Pancuronium, Tubocurarine, Atracurium, Doxacurium are all what type of drugs & what do they do? They are Nicotinic Blockers used for paralysis that don't cross BBB
Nicotinic Blockers are typically competitive non-depolarizing. What makes Succinylcholine special? It causes many little depolarizations until the muscle can't respond anymore. At this point it becomes non-depolarizing & the muscles can't reset. Lasts about 8 mins
What are some B1 Agonists? Dopamine, Dobutamine, Isoproterenol, Epi
Dopamine is a B1 Agonist. What does it do? Stimulates NE release & improves renal blood flow
Dobutamine is a B1 Agonist. What does it do? It helps in the treatment of CHF. It increases CO by increasing contractility
Isoproterenol is a B1 Agonist. What does it do? Cardiac stimulation
Epi is a B1 Agonist in low doses. What does it do? Cardiac stimulation
What do B1 Receptors do? Most prominent effect is cardiac stimulation. It also stimulates renin release & promotes production of the aqueous humor
What effect does Isoproterenol have on B2-R? Bronchodilation & vasodilation
What B2 Agonist drugs are used to treat asthma & COPD? Albuterol, Terbutaline, Salmeterol, Formoterol
What B2 Agonist asthma/COPD drugs are short acting? Albuterol & Terbutaline
Ritodrine is a B2 Agonist. What does it do? Prevent premature labor
Epi has an effect on B2-R at low doses. What does it do? Bronchodilation & vasodilation
What effects do B2-R have? Most prominent effect is bronchodilation. It also has BPULSE effects.
You can remember what effects B2-R have by 2B's & PULSE. What do these stand for? Blood vessel dilation, Bronchodilation, Pancreas (insulin), Uterus (relaxation), Liver (glycogenolysis), Skeletal mm (inc contractility), Eye (mydriasis)
MAO & COMT degrade monoamines & catecholamines. What are their main methods of doing this? MAO - deamination, COMT - methylation
What are some things about COMT? Widely distributed, degrades circulating catecholamines
What are some things about MAO? Metabolizes monoamines, MAO-A (other places) & MAO-B (blood platelets)
A1 Agonists use G-Protein coupling. What is the sequence of events? A1-R is activated, which activates the G-protein. In turn, this activates PLC to cleave PIP2 into IP3 & DAG. IP3 stimulates the ER to release Ca2+, & the Ca2+ activates things.
What do B-R & A2-R do to adenylyl cyclase? They do opposite things. B-R stimulate cAMP & A2-R inhibit cAMP from being formed.
What do A1-R do? Predominately vasoconstriction, which causes an increase in BP; urinary retention, prostate contraction, mydriasis, stimulate ejaculation
What does an A2-R do? It lowers BP by inhibiting ACh from being released by presynaptic cells in the SNS
What receptors inhibit NE from being released by presynaptic cells in the PSNS? M2- & M4-R
What effect does NE have on A1-R? Vasoconstriction
What effect does NE have on B1-R? Cardiac stimulation at high doses. Body will initiate reflex bradycardia via baroreceptors so the HR & heart work will be lowered. This is dangerous b/c there is already vasoconstriction with A1-R & stimulation of B1-R can also cause vasoconstriction
What kind of effect does Epi have on A1-R at high doses? Vasoconstriction
Pseudophedrine, Phenylephrine, Oxymetazoline, Tetrahydrozaline are decongestants. What type of drugs are they? A1 Agonists b/c A1-R inhibit respiratory tract secretions
Methoxamine & Mephenteramine are A1 Agonists. What would they treat? Hypotension
Metaraminol is a A1 Agonist. What does it treat? Paroxysmal supraventricular tachycardia
What A1 Agonist is used to treat postural/orthostatic hypotension? Midodrine
Amphetamine, Methamphetamine, Phentermine aren't really A1 Agonists, but they have Alpha effects for what? Weight loss
A2 Agonists are used to treat what? Hypertension, mm spasms, glaucoma
What A2 Agonist drugs are used to treat hypertension? Clonidine, Guanabenz, Guanfacine
Tizanidine is an A2 Agonist. What does it treat? Muscle spasms
What A2 Agonists are used to treat glaucoma? Apraclonidine & Brimonidine
There are 2 A1 Antagonist drugs used to treat pheochromocytoma. What are they? Phenoxybenzamine & Phentolamine
What is the difference between Phenoxybenzamine & Phentolamine? Phentolamine has a bigger reflex tachycardia b/c it binds to both A1- & A2-R
Prazosin & Doxazosin are what type of drugs & what do they treat? A1 Antagonists, hypertension
Terazosin & Tamsulosin are A1 Antagonists. What do they treat? BPH, they cause vasodilation
Yohimbine is an A2 Antagonist. What is it used for? Sexual dysfunction
B1 Blockers are good for a lot of things. Name some. Antihypertensive, prophylaxis for migraines, tx of glaucoma, reduce sense of situational stress
Why can't you just stop taking Beta Blockers cold turkey? There is serious risk of rebound hypertension & receptor up-regulation on the heart which can cause a MI
Exposure to agonists cause... Receptor down-regulation (there is a lot of NT or whatever around, there's no need for extra receptors)
Exposure to antagonists cause... Receptor up-regulation (there isn't a lot of NT or whatever around, & all the receptors scramble to pick up what little is there)
What are the Selective B1 Antagonists? Acebutolol, Atenolol, Esmolol, Metoprolol
What are the Non-Selective Beta Blockers? Labetalol, Nadolol, Pindolol, Propranolol, Timolol
What drugs exhibit Intrinsic Sympathomimetic Activity (ISA)? Acebutolol, Labetalol, Pindolol
Why wouldn't you give someone with asthma Propranolol as a Beta Blocker? Propranolol is non-selective, so it'll antagonize B2-R which causes bronchoconstriction.
Why is Metoprolol special? It is B1-R selective (cardioselective)
What Beta Blocker is the prototype? Propranolol
What Beta Blocker blocks B-R & A1-R? Labetalol
Why would giving someone Esmolol orally be a bad idea? It has a half-life of 10 minutes
What is the half-life of Propranolol? 3.5-6H b/c of high lipid solubility
Pindolol has ISA. What does this do? Pindolol is a partial agonist. It will stimulate B-R a little while also inhibiting the B-R so HR won't drop too low
What are the main effects of the Beta Blockade? Decreases HR & contractility, inhibits gluconeogenesis & glycogenlysis, inhibits renin release, decreases intraocular pressure
Created by: Naychan07