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Pharm 1 - Adrenergics

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isabellepjk's version from 2017-05-06 02:57

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 synaptically?
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 (S=sleepy)
(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 & ↓ Ca++ influx (K and Ca both end up with more OUTSIDE the 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
β1actionsheart (stimulate= positive inotropy; Increase contractions) & ↑ cardiac output
β2 actionsvasodilation, 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. (gotta get through the gate to get cigarettes)
MUSCARINIC = G-Protein (G-dawg's wearing his musk)
What are the Reversible cholinesterase inhibitors?
Uses of reversible cholinesterase inhibitors? 6
Contraindications?2
(PPEN) Physostigmine; Pyridostigmine, Neostigmine, Edrophonium

Antidote of atropine (Physo), anti-curare, Impaction in cattle, Glaucoma, Myasthenia gravis, NMM blockage

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
memorize

Adrenergic Agonsits α 1

Question Answer
What are the three α1 agonists direct drugs?Methoxamine, Phenylephrine, Phenylpropanolamine (Directly stare at A Massive Purple Pee)
(Remember α1=Gq=sm. mm. contraction. remember α1 POSTsynaptically)
What is Methoxamine?
What does it do?
Adverse effects?
α1 agonist direct.
Vasoconstriction increases peripheral resistance, BP & reflex bradycardia. (Vasopressor)
Tx hypotension during sx (meth & oxys will make you tense)
Adverse: Headache and vomiting
What is Phenylephrine? What does it do?α1 agonist direct. Nasal decongestant (phenylePHLEGM)
What is phenylpropanolamine? What does it do?α1 agonist direct. Treat urinary incontinence.
What is the α1 agonists MIXED drug?Metaraminol
(I have mixed feelings about Tara)
(Remember α1=Gq=sm.mm. contraction. remember α1 POSTsynaptically)
What is Metaraminol? What does it do?α1 mixed agonist. VASOPRESSOR treat hypotension during spinal anesthesia. (Does vasoconstriction) (Tara makes me tense)
memorize

Adrenergic Agonsits α 2

Question Answer
What are the α2 agonists?Clonidine, Apraclonidine, Methyl-dopa, Xylazine, Detomidine, Medetomidine, Romifidine
(Remember, α2=Gi=sm.mm. contraction. but remember α2 works PREsynaptically)
What is Medetomidine? What does it do?α2 agonist.
Anesthetic premed for horses and small animals. Treat emergence delirium following anesthesia (MEDelirious, also horses are always fucking delirious after anesthesia) (cytochrome p450 (enzyme) is inhibited by Medetomidine)
What is Romifidine?
What does it do?
α2 agonist.
IV premed use in horses
What is Clonidine?
What does it do?
Adverse effects?
α2 agonist.
Increase sedation (without change in renal BF), pre-anesthetic/analgesic, treats hypertension (want to vasodilate) (Clowns push your BV open)
Adverse: Dry mouth, rebound hypertension, sexual dysfunction (clowns shouldn't have sex), bradycardia
What is Apraclonidine? What does it do?α2 agonist.
Treats glaucoma by reducing Aq humor production
What is Methyl-dopa? What does it do?
Adverse:
α2 agonist.
Treats hypertension (vasodilates). (especially in pregs (Moms and Dads))
Makes you sleepy (meth and dope make you sleepy)
What is Xylazine?
What does it do?
Adverse effects?
α2 agonist.
Muscle relaxation, sedation/pre-med for large animals (Xtra Large)
Adverse: Bradyc, conduction disturbances, myocardial depression
(Reversed by Yohimbine)
What is Detomidine?
What does it do?
α2 agonist.
Sedation/anesthetic premedication for large animals
memorize

Adrenergic Agonsits β1 & β2

Question Answer
What are the β1 agonists?Dobutamine
What is Dobutamine?
What does it do?
β1 agonist.
Synthetic catecholamine
Used for CHF (ionotropic, but does not change HR or rhythm, only contractility)
What are the β2 agonists categories?Selective (Bronchodilators, uterine relaxants), non-selective
("THE -OLs”)
What are the β2 agonists bronchodilators? (6)Metaproterenol, Terbutaline, Albuterol, Salbutamol, Clenbuterol, Salmeterol
(SAL & MET ALl agonize over CLEN TER a SALMon open)
What is Metaproterenol?
What does it do?
β2 agonist,
bronchodilator
(the mets are a team that cheat w/ bronchodilators)
What is Terbutaline?
What does it do?
Contraindications?
β2 agonist
bronchodilator
DO NOT USE IN ANIMALS WITH HEART DZ; induces tachycardia
(tear butt if you couldn't breathe & your heart rate increased)
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
(RAC of ribs; makes meat more lean)
What is Clenbuterol?
What does it do?
β2 agonist
COPD horses (bronchodilator)
* banned in food producing animals
What is Salmeterol?
What does it do?
β2 agonist
Bronchodilator, slow onset and long acting
What is Isoxuprine?
What does it do?
β2 agonist
vasodilator in skel mm (good for navicular Dz/laminitis)
What is Ritodrine?
What does it do?
β2 agonist,
Uterine relaxant ( --> arrests premature labor)
(RELAX don't get RIT of that baby yet!)
What is the nonselective β agonist?Isoproterenol
What is Isoproterenol?
What does it do?
β nonselective.
Synth catecholamine, vasodilation, uterine relaxation
(In Search Of Catecholamines), (ALL Betas do sm mm RELAX so uterus relaxes and vasodilation)
Adverse effects of Dobutamine?Arrhythmias (↑ AV conduction), Tolerance (tachyphylaxis)
memorize

Catecholamines

Question Answer
Where are catecholamines made and what makes them?Your body makes them already from Tyrosine
Catecholamines in order of least metabolized to mostDopamine, Norepi, Epi, Isoproterenol
(Littlest Dogs Need Everyone's Ice)
What are the effects of Dopamine?Depends on the dose...
Low concentrations: activates D1 receptors, receptors of renal vasculature; vasoDilation
Increase renal BF, Increase GFR, increase Na excretion --> Cardiogenic and hypovolumic shock
(down amount, D1 receptors, vasoDilation)
Higher doses B1 receptors; positive inotropic action
Max doses : a1 receptors; vasoconstriction
(mAX; vAsoconstriXon)
↓ dose of Dopamine - what receptor, does what?D1 receptor, vasodilation (↑ GFR!)
↑ dose of Dopamine - what receptor, does what?β1 receptor; positive inotropic action
heart & kidney stuff
Max dose of Dopamine - what receptor, does what?α1 receptor,
(mAx; constriXon)
vasoconstrictor
What does epi/norepi do? (5)↑ HR for cardiac arrest,
treat hypotension, topical hemostasis and prolongs action of local anesthetics via vasoconstriction
treat allergies/hypersensivity
treat bronchospasm (does bronchodilation)
What does Isoprotenerol do on its receptors?Nonselective β agonist
B1 for cardiac arrest;
B2 for vasodilation and uterine relaxation
What are the two synthetic Dopamines?
Which is selective, & for what?
Dopexamine,
Fenoldopam (D1 SELECTIVE)
(Old pam has dope pexes )
What is Fenoldopam? What does it do?Synthetic Dopamine, D1 selective means it does VASODILATION
Affinity for catecholamines at alpha receptors?Epi > (or equal to) norepi > Isoproterenol
Synth of Dopamine? Include rate limiting step.Tyrosine - (hydroxylase=RLS) → Dopa → Dopamine
When is epinephrine contraindicated?
Why?
DURING PREGNANCY!
↑ uterine sm. mm contractions.
What would you give to pt in shock/oliguric?
How much?
MAX dose of Dopamine (vasoconstriction)
Precaution w/ using Dopamine?If it gets into the tissues, can cause necrosis. Make sure pt isnt hypovolemic
What does Fenoldopam usually treat?
Contraindications?
Treats hypertensive crisis
(Old Pam is hyper during her crisis)
DON'T use in CATS (cats dont have as many D1 receptors-results unpredictable & messy)
(FEline --> NO)
Drug that can interfere w/ synth of catecholamine?Methyl dopa (indirect)
(Making Meth and Dope will interfere with making Catecholamines)
What interferes w/ storage of epi?Reserpine (indirect) (a snake is storing my epi pen)
What prevents release of norepi?(Indirect) guanethidine (Guanor, trogdors son)
What drug ↓ central sympathetic outflow?(Indirect) Clonidine (Clonidine Central)
What blocks the high-affinity transport of choline?Hemicholinium (block so only get half the choline)
How is ACh blocked from being transported into vesicles by vesicular xporter? (Drug)Vesamicol (ves - ves Ach= AVV)
memorize

Adrenergic Antagonists

Question Answer
How many/what categories of adrenergic antagonists?5
Non selective alpha
Selective a1
Selective a2
Non selective b
selective b1
What do indirect adrenergic antagonists do? (4)Interfere w/storage of norepi,
↓ symp outflow,
prevent norepi release,
inhibit catecholamines synth
What are the α1 antagonistic selective drugs?Terazosin, Doxazosin, Prazosin
What is Terazosin? What does it do?α1 selective, lower BP
What is Doxazosin? What does it do?α1 selective, lower BP (via vasodilation)
What is Prazosin? What does it do?α1 selective antagonist, lower BP (α1 BLOCKER so α one would constrict so now DILATE. also PRESSURE is a sin so fix it) without reflex tachycardia
What are the α2 selective antagonistic drugs?Yohimbine, Atipamezzole
What is Yohimbine? What does it do?Reversal agent of Xylazine & Detomidine (beans do double duty)
What is Atipamezole?
What does it do?
α2 selective antagonist
Reverses Detomidine (Medetomidine) Small animals
What are the α nonselective drugs?Phenoxybenzamine, Phentolamine, Tolazoline
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.
Stimulates GI sm mm, pseudo-obstruction relief, Treat hypertension (does vasodilation), dermal necrosis
(phantom is a dead pseudo being?)
What is Tolazoline?
What does it do?
Nonselective α antagonist.
To reverse the effects of Xylazine in large animals
What are the β antagonist nonselective drugs?Propranolol, Timolol, Sotalol
(Tim can't select Between sota and propane)
What is Propranolol? What does it do?β nonselective,
Negative inotropic & chronotropic effect, bronchoconstrictor, decrease glucose
(anyBody can buy propane)
(constrict bronchioles around propane)
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 (via vasodilation), cardiac arrhythmias, & ischemic heart Dz
What is Acebutolol,
what does it do?
Selective β1 blocker.
Treat hypertension, cardiac arrhythmias, & ischemic heart Dz, thryotoxicosis, pheochromocytoma, glaucoma
What is Metoprolol, what does it do?Selective β1 blocker.
Treat hypertension, cardiac arrhythmias, & ischemic heart Dz, pheochromocytoma, thyrotoxicosis, glaucoma
What is esomolol,
what does it do?
What can be said about its duration of action?
Selective β1 blocker.
Treat hypertension, cardiac arrhythmias, & ischemic heart Dz, phechromocytoma, thyrotoxicosis, glaucoma
very short acting
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
memorize