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Pharm 1 - Adrenergics

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hpaul2's version from 2017-03-09 00:24

Intro Basics

Question Answer
What are the adrenergic receptors?α1, α2, β1, β2, (β3)
Which G proteins match up w/ α1, α2, & β receptors?α1= Gq. α2= Gi. β1/2= Gs (QIS!!)
Which is long/short neuron for adrenergic system? Cholinergic system?ADRENERGIC is short preganglionic & long postganglionic. CHOLINERGIC is long preganglionic & short postganglionic [ganglion is close to parasymp bc it can just go do it's own thing while we don't pay attention]
Which adrenergic receptor works post synoptically? Which works pre?POSTsynaptically is α1 (aka Gq)...PREsynaptically is α2 (aka Gi) [α -2-year-old-preteen is Immature]
Which adrenergic receptors (α1, α2, β) have what effect on sm. mm. (what are their G proteins?)α1=Gq=sm.mm. Contraction...α2=Gi=sm.mm. Contraction...β=Gs=sm.mm. Relaxation (β is only relaxation one, even w/ M receptors, βs the only one)
What is the path of inhibition of Gi?Inhibit adenylate cyclase would ↓ CAMP, which would ↑ K+ out flux (more K out of cell) & ↓ Ca++ influx (more Ca++ out of cell)
What do sympatholytics do the same thing as?Parasympathomimetics
What are the two types of cholinergic receptors?Nicotinic, Muscarinic
What are the two types of nicotinic receptors?Nm (nicotinic muscular) & Nn (nicotinic neuronal)
What are the types of muscarinic receptors? What G-protein do they correlate w/? What does the G-protein mean (in relation to sm. mm. action)Q=queer=odd. M1=Gq. M2=Gi. M3=Gq. M4=Gi. M5=Gq. (Gq=sm mm contraction) (Gi=sm mm contraction) (So, M receptors all activate sm mm)
Describe how sympathetic (adrenergic) system affects kidneys?The post ganglionic NT is DOPAMINE! (Those are some dope kidneys)
Describe how the symp. system affects sweat glands?ACh is the NT POSTganglionically!
What is NANC? Ex? Where?Noradrenergic noncholinergic neurons. These release NITRIC OXIDE at the POSTganglionic terminal. NO does penile erection, also has GI effects (inhibit motility & vascular effect (vasoDILATE)
What are two ways a receptor is able to cause a response in the cell?(1) The receptor is connected to a G-protein which is inside the cell
(2) Receptor is connected to a ligand-gated ion channel
α1 effectsVasoconstriction & sphincter constrictor (1=constriction...on outside so pushes in)
α2 effectsInhibits norepi = sedative & analgesic & mm relax
β1heart (stimulate= positive inotropy) & ↑ cardiac output
β2vasodilation, sm mm relax (β 2= relax gaiz)
How is the mechanism which makes the receptor work different between nicotinic & muscarinic receptor?NICOTINIC = ligand gated ion channel. MUSCARINIC = G-Protein (G-dawg's wearing his musk)
Uses of reversible cholinesterase inhibitors? Contraindications?Impaction in cattle, anti-curare, etc. CONTRA = impaction w/ obstruction, pregnancy
Ganglionic blockers antagonize what?Nn receptor
Neuromuscular blockers antagonize what?Nm receptor
Where is the only post synaptic α2?Pancreas
Epi works on what receptors?α1 & β1
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Adrenergic Agonsits α 1

Question Answer
What are the three α1 agonists direct drugs?Methoxamine, Phenylephrine, Phenylpropanolamine
What is Methoxamine? What does it do?α1 agonist direct. VASOPRESSOR Tx hypotension during sx. (Does vasoconstriction) (meth & oxys will make you tense)
What is Phenylephrine? What does it do?α1 agonist direct. Nasal decongestant (sounds like ephedrine, another nasal decongestant), glaucoma
What is phenylpropanolamine? What does it do?α1 agonist direct. Treat urinary incontinence (sphincter constriction)
What is the α1 agonists MIXED drug?Metaraminol
What is Metaraminol? What does it do?α1 agonist mixed. VASOPRESSOR treat hypotension. (Does vasoconstriction)
What is Oxymetaxoline used fornasal decongestant, eye redness
Name all the α 1 agonists Methoxamine, Phenylephrine, Phenylpropanolamine, Metaraminol, Oxymetaxoline
What are the adverse effects of methoxamineReflex bradycardia, hypertension headache, vomiting (stay away from meth and oxys)
How is phenylpropanolamine administeredPO
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Adrenergic Agonsits α 2

Question Answer
Name the α2 agonistsClonidine, Apraclonidine, Detomidine, Medetomidine, Dexmedetomidine, Romifidine, Xylazine, Methyl-dopa (6 dines, a zine, and a dope)
What is Medetomidine? What does it do?α2 agonist. Anesthetic premed. Treat emergence delirium
What is Romifidine? What does it do?α2 agonist. Anaesthetic premed/sedative (horses)
How is Romifidine administered, what species?IV use in horses
What is Clonidine? What does it do?α2 agonist. Treats hypertension (vasodilator), analgesia (pre-ansesthetic)
What are the adverse effects of ClonidineDry mouth/sedation (good or bad), rebound hypertension, sexual dysfunction, bradycardia
What is Apraclonidine? What does it do?α2 agonist. Treats glaucoma (↓ intraocular pressure, ↓ aqueous humor production)
What is Methyl-dopa? What does it do?α2 agonist. Treats hypertension. (↓ BP)
What is Xylazine? What does it do?α2 agonist. Sedative-anesthetic premedication (Large animal)
What is the reversal agent for Xylazine Yohimbine
What are the adverse effects of XylazineBradycardia, conduction disturbance, myocardia depression
What is Detomidine? What does it do?α2 agonist. Sedation/anesthetic premedication (large animal)
memorize

Adrenergic Agonsits β1 & β2

Question Answer
What is the β1 agonist?Dobutamine
What is Dobutamine? What does it do?β1 agonist. Treats congestive heart failure ***↑ isotropy but NOT heart rate or rhythm which is awesome.
What are the β2 agonists categories?selective (Bronchodilators, uterine relaxants), non-selective
What are the β2 agonists bronchodilators? (5)Metaproterenol, Terbutaline, Albuterol/Salbutamol, Clenbuterol, Salmeterol (1 terb + 4 ols)
What is Metaproterenol? What does it do?β2 agonist, bronchodilator (the mets are a team that cheat w/ bronchodilators) (THIS IS NOT METARAMINOL, THE A-1 MIXED AGONIST)
What is Terbutaline? What does it do?β2 agonist, bronchodilator for **animals w/ heart Dz (tear your heart out)
What is Salbutamol? What does it do?β2 agonist, bronchodilator AKA albuterol
What is Ractopamine? What does it do?β2 agonist, repartitioning agent for cattle & swine, no withdrawal period (lean, fast growing meat - what a rack)
What is Clenbuterol? What does it do?β2 agonist, COPD horses (bronchodilator)
What is Salmeterol? What does it do?β2 agonist, bronchodilator, slow onset long acting **so can be used prophylactically
What is Isoxsuprine? What does it do?β2 agonist, vasodilator in sk. mm, navicular Dz/laminitis (supreme laminitis)
What is Ritodrine? What does it do?β2 agonist, uterine relaxant (Rito Suave-open your uteruses, ladies!)
What is the nonselective β agonist?Isoproterenol
What is Isoproterenol? What does it do?β nonselective (does it all) Synth catecholamine, inotropic, vasodilation, uterine relaxation
Adverse effects of Dobutamine?Arrhythmias (↑ AV conduction), Tolerance (tachyphylaxis)
What β2 agonist is banned in food animals?Clenbuterol
Which bronchodilator is potent & fast acting and which is slow onset & long acting?potent/fast - Albuterol/Salbutamol; slow/long - Salmeterol
memorize

Catecholamines

Question Answer
What are catecholamines?Your body makes them already from Tyrosine
Catecholamines in order of least metabolized to mostDopamine, Norepi, Epi, Isoproterenol
How do the effects of Dopamine change?DOSE DEPENDENT
↓ dose of Dopamine - what receptor, does what?D1 receptor, vasodilation (↑ GFR!)
↑ dose of Dopamine - what receptor, does what?β1 receptor, heart & kidney stuff
Max dose of Dopamine - what receptor, does what?α1 receptor, vasoconstrictor
What does epi/norepi do? (5)↑ HR for cardiac arrest, treat hypotension (vasoconstriction), topical hemostasis, allergies, bronchospasm (bronchodilation)
What receptor does Isoproterenol work on? Do?Nonselective β agonist for cardiac arrest (inotropy) & asthma
What are the two synthetic Dopamines? Which is selective, & for what?Dopexamine, Fenoldopam (D1 SELECTIVE)
What is Fenoldopam? What does it do?Synthetic Dopamine, D1 selective means it does VASODILATION
Affinity for catecholamines at receptors most to leastEpi > (or equal to) norepi > Isoproterenol
Synth of Dopamine? Include rate limiting step.Tyrosine - (hydroxylase=RLS) → Dopa → Dopamine
When is epinephrine contraindicated? Why?NOT DURING PREGNANCY! ↑ uterine sm. mm contractions.
What would you give to pt in shock/oliguric?MAX dose of Dopamine (vasoconstriction)
Precaution w/ using Dopamine?If it gets into the tissues, can cause necrosis. Make sure pt isn't hypovolemic
What does Fenoldopam usually treat? Contraindications?↑ urination, hypertensive crisis - DON'T use in CATS (cats don't have as many D1 receptors)
Drug that can interfere w/ synth of catecholamine?Methyl dopa (indirect)
What interferes w/ storage of epi?Reserpine (indirect) (a snake stole my epi pen)
What prevents release of norepi?(Indirect) guanethidine (guano stops the excitement)
What ↓ central sympathetic outflow?(Indirect) Clonidine (Clonidine Central)
What blocks the high-affinity transport of choline?Hemicholinium (half the choline)
How is ACh blocked from being transported into vesicles by vesicular xporter? (Drug)Vesamicol
memorize

Adrenergic Antagonists

Question Answer
How many/what categories of adrenergic antagonists?Indirect (1), Direct → α (nonslective=3, selective → α 1=3, α 2=2), β (nonselective=2, β 1=4)
What do indirect adrenergic antagonists do? (4)Interfere w/storage of norepi, ↓ symp outflow, prevent norepi release, inhibit catecholamines synth
What are the α1 selective drugs?Terazosin, Doxazosin, Prazosin (vasodilate...made you sleepy 3 ZZZ's)
What is Terazosin? What does it do?α1 selective, lower BP, vasodilation (α1 BLOCKER so α one would constrict so now DILATE)
What is Doxazosin? What does it do?α1 selective, lower BP, vasodilation (α1 BLOCKER so α one would constrict so now DILATE)
What is Prazosin? What does it do?α1 selective, lower BP (α1 BLOCKER so α one would constrict so now DILATE)
What are the α2 selective antagonistic drugs?Yohimbine, Atipamezzole
What is Yohimbine? What does it do?Reversal agent of Xylazine & Detomidine
What is Atipamezole? What does it do?α2 selective antagonist reverse Detomidine (Medetomidine) (Tip over one person named Pam)
What are the α nonselective drugs?Phenoxybenzamine, Phentolamine, Tolazoline (nonselective-- a phantom takes oxys to be LAZy)
What is Phenoxybenzamine? What does it do?Nonselective α antagonist. Irreversible inhibition of α-receptors. (Both αs, irreversible) treat adrenal tumor (pheochromacytoma)...also hypertrophy of prostate. (pheno for pheo- & prostates - triple p PPP)
What is Phentolamine? What does it do?Nonselective α antagonist. Non-selective blocker of α-receptors. Treat hypertension (does vasodilation) (phantom pushing your vessels open)
What is Tolazoline? What does it do?Nonselective α antagonist. To reverse the effects of Xylazine in large animals (both have a z in them. it doesn't draw a "line", its not picky)
What are the β antagonist nonselective drugs?Propranolol, Timolol (TIM ANTAGONIZES us nonselectively by lighting a Β tape on fire w/ PROPANe)
What is Propranolol? What does it do?β nonselective, Negative inotropic & chronotropic effect, bronchoconstrictor (Hank/Tim will sell propane to anyone)
What is Timolol? What does it do?(β blocker) β nonselective. Treat glaucoma. (Tim has eye problems)
What are the β1 antagonists?Atenolol, Acebutolol, Metoprolol, Esomolol (β1 antagonists are Bullies, they LOL at you)
What is Atenolol, what does it do?Selective β1 blocker. Treat hypertension, cardiac arrhythmias, & ischemic heart Dz
What is Acebutolol, what does it do?Selective β1 blocker. Treat hypertension, cardiac arrhythmias, & ischemic heart Dz
What is Metoprolol, what does it do?Selective β1 blocker. Treat hypertension, cardiac arrhythmias, & ischemic heart Dz (makes your heart chill out)
What is esomolol, what does it do?Selective β1 blocker. Treat hypertension, cardiac arrhythmias, & ischemic heart Dz
What is reserpine, what does it do?Indirectly acting adrenergic antagonist. Interferes w storage of epi.
Therapeutic uses of α-adrnergic blockers (5)Hypertension associated w/ pheochromocytoma, Essential hypertension, Migraine, Benign prostate hyperplasia, Reversal agent of Xylazine & Detomidine
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