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Adrenergic drugs

Kaplan medical

QuestionAnswer
What is Epinephrine reversal? - To test if Epinephrine or NE is given If you give an α₁-blocker and then epinephrine, you get hypotension — that’s epinephrine reversal. If you give an α₁-blocker and then norepinephrine, you do not get hypotension because NE lacks β₂ activity Bloc
Describe the synthesis of NE Tyrosine gets taken up (presynaptic neuron) converted to DOPA —> Dopamine —> NE Enzymes: 1) Tyrosine hydroxylase 2) DOPA decarboxylase/ L- aromatic among acid decarboxylase 3) DA beta decarboxylase
What is the rate limiting step in NE synthesis? Tyrosine hydroxylase
When NE gets released from te presynaptic neuron it has different fates (4), what are they? 1) Reuptake (by NaCl NE co-transporter) this is why NE has such a short half life 2) Act on the adrenergic receptors (alpha or beta) 3) broken down 4) signal a negative feedback loop via a receptor on the presynaptic neuron (alpha 2)
NE gets broken down by 2 enzymes, what are they? (in the synaptic space and mobile pool in presynaptic neuron) Synaptic space: by COMT Presynaptic neuron: by MAO-A
Alpha 1 receptor agonists? Phenylephrine
Alpha 2 agonists? 1. Clonidine 2. Methyldopa
Non selective beta receptor agonists?(2) 1. Isoproterenol ( beta 1= beta 2) iso= the same/equal 2. Dobutamine (beta 1> beta2)
Beta 2 selective agonists (3)? 1. Albuterol 2. Terbutaline 3. Salmeterol
Beta 3 selective agonists (1)? Mirabegron (used for overactive bladder but only oerscribes after M3 antagonist haven’t work, Oxybutynin)
What is the difference between NE and Epi (based on the receptor they do/donot work on)? Beta 2 receptors (NE does not but Epi does)
Which adrenergic receptors are more sensitive to activators? (Alpha or Beta) Beta receptors followed by alpha receptors
Dopamine works on which receptors? (Based n what) Dopamine works on D1, B1 and A1 depending on the dose. From low to high dose follow this sequence.
Cathecolamines effect is first on which organ, blood vessels or cardiac muscle (heart)? Blood vessels gets work upon first.
Epi can increase (alpha1) or decrease (beta 2) the BP, what determine what it will do? The DOSE.
High dose Epi acts as which drug? NE
Low dose Epi acts as which drug? Isoproterenol (beta1=beta2)
What drugs “increase” the RELEASE of NE from the presynaptic neuron (3)? 1. Tyramine ( this occurs when a MAO-A inhibitor is given b/c it gets to accumulate) 2. Amphetamines (increase release of DA, NE, 5HT) 3. Pseudoephedrine (not really used anymore but Phenylephrine)
What drugs inhibits the NE reuptake (2) ? 1. cocaine 2. TCAs (Tricyclic antidDepressants)
What are the forms of MAO and where are they found? MAO-A (anywhere) and MAO-B (brain mostly) - MAO-A metabolizes tyramine, NE, 5HT) - MAO-B metabolized DA. Blocker is Selgiline
Non-selective alpha blockers (2)? 1. Phentolamine 2. Phenoxybenzamine (noncompetitive inhibitor used in Pheochromocytoma)
alpha 1 selective blocker? All the “-zosin” - Prazosin - Doxazosin Terazosin Tamsulosin (treat BPH only) All of the -zosin act on alpha 1 and are good for BHP but the last one is isolated BHP)
Alpha 2 selective blocker? Mirtazapine
Beta 1 blockers vs Non-selective beta 1 blocker? (Names Beta 1 blockers: A-M w/ suffix -o lol Beta 1 non selective blockers: N-Z w/ suffix -o lol
What are the effects of glucagon on the heart? It’s a Positive inotropic and chronotropic via its own Gs receptor (not via beta 1). That is why it is used in beta-blocker overdose.
What are the partial Beta blocker agonist (Intrinsic sympathomimetic activity) ? 1. Acebutolol 2. Pindolol. Alone they acts as a agonists (not the case in the human body) but in the prescience of NE or Epithey acts as a n antagonist.
Which beta blocker does not enter the CNS? Atenolol *they can’t pay “aten”tion
what are the (2) Beta blockers w/ alpha blocker properties? 1. Labetalol 2. Carvediol
Which beta blocker also has K channel blockage properties? Sotalol
What is Open angle Glaucoma? A chronic condition with increased intraocluar pressure d/t decreased reabsorption of aqueous humor. Lead to progressive, painless vision loss, if untreated.
What is intraocular pressure and how is it maintained. A balance between fluid formation and its drainage from the globe.
Which structure makes the aqueous humore and what helps with the drainage? -Fluid formation; Ciliary epithelial cells makes the fluid ( a beta agonist aids in this recess too that is why a beta blocker is used in glaucoma to stop this fluid formation) drainage: PGF2a aids in drainage (a prostaglandin)
What is a closed angle glaucoma? Acute condition w/ increased IOP dt blockade of the canal of Schlemm.
Which class of drugs are contraindicated in closed angle glaucoma? Anti-muscarinic drugs and alpha 1 agonists b/c both increase the IOP.
What is a PGF2a agonist and MOA? Latanoprost. Increases aqueous humor drainage through the uveoscleral pathway
What other two drugs decrease aqueous humor formation? Acetazolamide and Apraclonidine
What is a Dopamine agonist? Fenoldepam
Where are a1 receptors found? (7) 1. Arterioles (constriction) 2. Veins 3.Radial muscle of the eye (mydriasis) 4. Bladder trigone/ sphincter and prosthetic urethra 5. Liver ( increase glycogenolysis) 6. Kidney (decrease renin release) 7. Male sex organ (vas deferens : ejaculation)
Where are a2 receptors found? (3) 1. Presynaptic neuron ( decrease release of neurotransmitters) 2. Platelets (aggregation) 3. Pancreas (decrease insulin release)
Where are b1 receptors found? (2) 1. Heart (increase chrono-, dromo- and inotrophy) 2. Kidneys (increase renin release: JGCs)
Where are b2 receptors found? (6) 1. Bronchioles (dilate) 2. Uterus (dilate) 3. Blood vessels (all: vasodilation) 4. Skeletal muscle (glycogenolysis/ contrct) 5. Liver (glycogenolysis) 6. Pancreas (incr insulin)
Where are b3 receptors found? (1) 1. Detrusor muscle of the bladder (relaxation)
Where are d1 receptors found? 1. Renal (vasodilation : increase RBF, GFR, Na secretion) 2. Mesenteric 3. Coronary vasculature
Created by: DVD27
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