Pharmacology Adrenergics Flashcards

Terms Definitions
β1 antagonists
Esmolol
Atenolol
Albuterol
Asthma reliever
α1 antagonists
Prazosin
Tamsulosin
Inhibitors of storage
Reserpine
Tyramine
Amphetamines
Methylpenidate
Pseudoephidrine
Imipramine
Treatment of mild depression
Carreditol
α1 receptor block --> vasodilation
β1 receptor block --> prevents sympathetic increase in heart rate
Treatment of heart failure
Reduces blood pressure
Dobutamine
Acute management of heart failure
Name the class: Phenoxybenzmine, phentolamine
alpha-adrenergic Antagonist
Selegiline
MAO B inhibitor used for Parkinson's
Timolol
Treatment of glaucoma through reduced production of aqueous humour
 
 
 
Nonselective alpha blockers  
Phentolamine = competitive inhibitor
 
Phenoxybenamine = noncompetitive inhibitor (irreversibly binds) 
Name the class: Reserpine
Inhibitor of catecholamine storage
Name the general class: Propranolol, labetalol, metoprolol, atenolol
Beta-adrenergic antagonist
Esmolol
emergency β receptor blocker in a thyroid storm
Phenylephrine
is an a1 selective agonist; produces vasocontriction and an increase in peripheral resistance therefore increasing diastolic blood pressure with little direct effect on the heart; the primary cardiac effect seen following phenylephrine administration is t
 
 
Adrenergic junction (catecholamine synthesis)
Tyrosine --> Dopa (via tyrosine hydroxylase) --> Dopamine --> NE (via dopamine beta hydroxylase) --> NE placed in storage vesicle --> released into junction to act on alpha and beta receptors  
Name the specific class of Metoprolol and atenolol
B1-selective antagonist
Name the class: Phenelzine, iproniazid
Monoamine oxidase (MAO) Inhibitor
On what receptors does NE act?
a1, a2, b1
List other effects of isoproterernol.
decreased intestinal motitlity; increased renin secretion; bronchodilation
 
 
 
Beta 1 receptor
Heart
SA node -- increase HR (positive chronotropy)
AV node -- increase conduction velocity
Atrial and ventricular muscle -- increase force of contraction (positive ionotropy), CV, CO, O2 consumption
His-Pukinje -- increase automaticity and CV
Kidney -- increase renin release
 
 
 
Beta blocker drugs (+general uses) 
Acebutolol, Atenolol, Metoprolol (1st half of the alphabet is beta 1 selective) so safer in asthmatics, diabetics, and peripheral vascular dz
 
Pindolol, Propranolol, Timolol (2nd half is nonselective)
 
Acebutolol and Pindolol both have intrisic sympathomimetic activity and act as partial agonists causing slight vasodilation and minimal change in lipids 
 
Used for angina, HTN, post-MI
Antiarrhythmics (propranolol, acebutolol, esmolol)
Glaucoma (timolol)
Migraine, thyrotoxicosis, performance anxiety, essential tremor (propranolol b/c overstimulation of beta 2 on skeletal mm) 
 
List the serious adverse effects of: Guanethidine, Guanadrel
Kidney disease, apnea
List hte serious adverse effects of Clonidine
Bradycardia, heart failure
_____ inhibits hepatic enzymes while ____ induces hepatic enzymes. Taking these two drugs together can cause ____and ____.
Propanolol (non-specific beta blocker); alcohol. nausea, vomiting
What drug is a structural analog to tyrosine. How does it effect catecholamine synthesis and in particular what enzyme does it inhibit. ? When would such a compound be used?
alpha-methyl-para-tyrosine (metyrosine); It is a competitive inhibitor of tyrosine hydroxylase (the rate limiting step in catecholamine synthesis); therefore it decreases the synthesis of catecholamines, reducing the amount that is available for release;
Enter your front text here.
Enter your back text here.
 
 
 
Closed angle glaucoma (+ treatment) 
Acute, painful condition w/ increased IOP d/t the blockade of the canal of Schlemm
 
Emergency treatment involving a cholinomimetic, carbonic anhydrase inhibitor, and/or mannitol
 
Pilocarpine, Acetazolamide, Mannitol 
1st = muscarinic agonist causes contraction of ciliary muscle which increases flow through canal
2nd = decreases aqueous humor formation
3rd = osmotic diuretic 
 
 
 
Uses of NE and Epi (5)
 
Cardiac arrest
Adjunct to local anesthetic
Hypotension
Anaphylaxis (epi only)
Asthma (epi only) 
Describe the mechanism of: Phenelzine, iproniazid
Inhibits MAO, increases catecholamine levels by blocking catecholamine degradation
List the serious adverse effects of: Pseudoephedrine
Atrial fibrillation, ventricular premature beats, Myocardial ischemia
Affinity of epinephrine to receptors
β: higher affinity
α1: affinity at higher concentrations
Alpha-methyl-DOPA is a sympatholytic compound. Briefly describe its mechanism of action.
Alpha-methyl dopa is a competitive inhibitor of dopa-decarboxylase. It inhibits the conversion of L-Dopa to DA, thereby reducing the levels of DA and NE; methyl-dopa is itself decarboxylated to form alpha-methyl dopamine which is then hydroxylated to for
What two drugs have been approved by the FDA for continuous prophylaxis in migraine?
Propranolol and timolol
 
 
 
Beta vs alpha receptors  
Beta receptors are usu more sensitive to activators than alpha receptors so drugs that exert both effects like (Epi) the beta responses are dominant at low doses and alpha at high doses
List all the b2 selective drugs used for treatment of asthma along with +/- of each drug.
1. Metaproterenol--prototype; administered orally 2. salmeterol--long lasting; inhalation; it is specific for lungs and therefore the side effects are minimal. The problem with long lasting agents is that if difficulties arise, it can be hard to rever
What is levadopa?
It is a dopamine like compound used to treat parkinson's disease, it is a sympathomimetic because it has similar functions to dopamine.
What are the cardioselective b1 blockers? What makes these agents so great?
Pindolol and acebutolol because they have a much lower effect on serum TAGs or HDL. Remember sserum TAGs could produce long-term complications such as angina associated with coronary artery disease and chronic treatment of hypertension. It is therefore
Summarize the GI effects of EPI.
Intestinal sommoth muscle is inhibited by EPI, resulting in decreased motility. This is due to b2 effects on the intestinal wall, but also due to an inhibitory effect of a2 stimulation in the gut to reduce Ach most likely contributes as well.
 
 
 
Beta blockade (general effects) 
Beta 1 blockade = decrease HR, SV, CO, renin release, aqueous humor production
 
Beta 2 blockade = precipitate bronchospams, and vasospasm in pts w/ these disorders
Also blocks glycogenolysis and gluconeogenesis (problem in diabetics)
Can increase LDL's and TG's 
Describe the mechanism of action of reserpine.
Reserpine binds to VMAT-2 and IRREVERSIBLY damages the vesicular ability to concentrate NE and DA (sometimes serotonin). Reserpine causes a massive efflux of catecholamine and this causes only a transient sympathomimetic effect because reserpine ultimate
Tyramine is decarboxylated form of what amino acid? Where is one likely to encounter tyramine? What could this potentially be a problem?
Tyrosine; Tyramine is found in many fermented foods (wine, cheese, sausage). Although it is well absorbed, it does not have effects under normal physiological conditons, because it is rapidly metabolized to in inactive form by MAO in the gut and liver.
Summarize the Respiratory effects of EPI.
Epi produces a potent b2 mediated relaxation of bronchial smooth muscle and bronchodilation. There is also an alpha mediated decrease in mucosal congestion and b2 mediated inhibition of antigen-induced histamine release. All of these features enhance ai
List as many side effects of amphetamine use as you can.
Increased HR may result in reflex bradycarida. The cardiovascular effects give rise to major acute toxicities, including arrhythmias, dissecting aneurysms and hypertension, all of which can be fatal.
What reflex actions could one expect to see in a patient taking phenoxybenzamine?
In the heart, a reflex tachycardia occurs following the sympathetic response; this response probably becomes exaggerated, probably due to the blockage of the inhibitory alpha-2A recpetors in the sympathetic nerve terminals in the heart leading to excessiv
On tissues or organs that have both alpha and beta receptors, which effects predominate and when?
at low concentrations beta effects predominate; at high concentrations alpha effects predominate
What is a major side effect associated with the -zosins (alpha 1 antagonists)?
Fainting (aka syncope) with inital treatment/dose.
Once again (because I'm pretty sure I asked this earlier)...What types of patients are beta blockers contraindicated in?
Both selective and non-selective beta blockers are contraindicated in asthmatics or individuals with airway problems, since life-threatening brochoconstriction may result (even with a topical application). Beta-2 blockade consistently increases airway re
What is the main draw for using atenolol?
It has features similar to metoprolol, but it has LESS CNS effects, it has a long half-life and is a popular agent to treat hypertension WITHOUT bronchoconstriction
What could one do to a cathecholamine to increase its Beta activity? What does this do for beta selectivity.
move the OH substiution from the 3,4 position to the 3,5 position; it increases beta-2 selectivity with a loss of alpha and beta-1 selectivity
What is the optimal length for the side chain on a phenylethylamine compound? What does hydroxylation of the B carbon do? How can you convert a phenylethylamine into a catecholamine? What are the effects of this conversion? Give examples of such compo
2 carbons; it increase the alpha and beta activity; hydroxylation of the 3,4 carbons on the benzene ring; it enhances the alpha and beta activity; NE, EPI, DA are all catecholamines
What is the effect of epi on vascular resistance?
There is no net effect on vascular resistance because resistance increases markedly in some vascular beds, while decreasing in others, reflecting the local distribution of alpha and beta2 receptors.
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