Intro To Adrenergic Drugs - More Detailed Flashcards
Phenylephrine CLASS: MOA: SE: CI:
Phenylephrine
CLASS: a1 agonist (a1>a2»B)
MOA: Causes a decrease in Bronchial Mucous Secretion, an Increase in Blood Pressure, and Mydriasis
SE: Bradycardia (BR Reflex), Severe Vasoconstriction w/ elevated BP
CI: HTN
Clonidine
CLASS:
MOA:
SE:
Clonidine
CLASS: Selective a2 agonist (a2>a1»B)
MOA: Decreases release of NE at synaptic terminals where a2 receptors are found in the Brainstem -> decreasing Sympathetic Outflow -> Decreased BP and Bradycardia.
Local (peripheral) Application causes Vasoconstriction.
Isoproterenol
CLASS:
MOA:
SE:
Isoproterenol
CLASS: Non-Selective B agonist (B1 and B2)
MOA: Increased HR/CO (B1) and Bronchodilation & Vasodilation (B2)
SE: Slight decrease in BP, BUT substantial Tachycardia
Albuterol
CLASS:
MOA:
Albuterol
CLASS: Selective B2 agonist
MOA: Increases Bronchodilation and Uterine Relaxation
Dobutamine
CLASS:
MOA:
Dobutamine
CLASS: Selective B1 Agonist
MOA: Increase in Heart Contractility -> Increased CO
Epinephrine
CLASS:
MOA:
Epinephrine
CLASS: Endogenous NT, Mixed a & B Agonist
MOA: Increase in CO/HR, Vasodilation -> Slight Increase in BP & Tachycardia; Bronchodilation and Decreased Mucous Secretion; enhances glycogenolysis and gluconeogenesis; increases Renin levels; increases K+ reuptake
Norepinephrine
CLASS:
MOA:
Norepinephrine
CLASS: Endogenous NT, Mixed a & B Agonist (except B2)
MOA: Potent Cardiac stimulant; Increases HR and BP, BUT BR corrects this -> Bradycardia;
Dopamine
CLASS:
MOA:
Dopamine
CLASS: Endogenous NT, Dopamine Receptor Agonist
MOA: D1 Receptors cause vasodilation and D2 Receptors suppress NE release (at physiological levels) -> decreased BP
At higher levels DA activates B1 receptors -> Increased CO/HR
At even higher levels DA activates a1 receptors -> Vasoconstriction and Increased BP
Cocaine
CLASS:
MOA:
SE:
Cocaine
CLASS: Indirect AR Agonist (Sympathomimetic)
MOA: Cocaine inhibits the reuptake of DA and NE into the presynaptic terminal via NET, thus enhancing their activity
SE: Has the potential to induce Hemorrhagic stroke and/or death
Phenelzine, Selegiline
CLASS:
MOA:
Phenelzine, Selegiline
CLASS: Indirect AR Agonist (Sympathomimetic)
MOA: inhibits MOA (Monamine Oxidase) from breaking down E, NE, and DA, increasing their stores in the CNS
Amphetamines, Methylphenidate
CLASS:
MOA:
SE:
Amphetamine, Methylphenidate
CLASS: Indirect AR Agonist (Sympathomimetic) may have a small direct effect as well
MOA: Stimulates the release of NE and DA, and inhibits their reuptake, increasing their overall activity. Creates a stimulant effect.
SE: Decreased appetite
Ephedrine
CLASS:
MOA:
Ephedrine
CLASS: Indirect AR Agonist (Sympathomimetic) but has some direct activity
MOA: Non-selectively releases stored catecholamines with a long duration of action. Increases BP. Mildly Stimulating.
Tyramine CLASS: MOA: Rx: Other:
Tyramine
CLASS: Indirect AR Agonist (Sympathomimetic)
MOA: Releases NE stored in Pre-Synaptic Terminals if administered Parenterally.
Rx: Can cause a marked increase in BP in Patients taking a MOA Inhibitor
Other: Pdt of Tyrosine metabolism found in cheese, cured meats, & smoked and pickled fish
What Adrenergic Agonists might you use to treat CHF?
Dobutamine (B1 Agonist) - may be used short-term to treat Acute HF as it increases CO
Dopamine - may be used to treat Severe Congestive HF with reduced Renal perfusion as D1 Receptors will induce Renal A. Vasodilation
What Adrenergic Agonists might you use to treat Hypertension?
Clonidine or another a2 agonist may be used as they work in the brainstem to inhibit catecholamine release and reduced Sympathetic outflow
What Adrenergic Agonists might you use to treat a patient in Hypotensive Emergencies such as Hemorrhagic Shock, OC of Anti-Hypertensives, or CNS Depressants?
Epinephrine or Norepinephrine, both of which will increase Sympathetic activity and functions to increase CO/HR (B1) and BP (a1)
What Adrenergic Agonists might you use to treat Chronic Hypotension?
Ephedrine would be a likely drug to use due to the fact that it is plant-based, and thus not a Catecholamine, so it will have a longer duration of action as opposed to other Adrenergic Agonists we have discussed. It increases BP by stimulating Catecholamine Release
What Adrenergic Agonists might you use to treat a patient in Cardiogenic Shock due to a Massive Acute MI?
Dopamine (enough to stimulate B1 receptors) or Dobutamine (B1) could both function to increase CO
What kind of Adrenergic Agonists might you use for Emergency treatment of a complete AV Block and Cardiac Arrest?
Epinephrine or Isoproterenol could be used as both function to increase HR (B1)
What kind of Adrenergic Agonist might you use to treat Narcolepsy?
Amphetamines or Methylphenidate could be used as either function to increase sympathetic outflow by increasing Catecholamine release and inhibiting their uptake, and function as a stimulant
What kind of Adrenergic Agonist might you use to treat ADHD?
Methylphenidate could be used as it functions as a stimulant and increases sympathetic outflow by stimulating the release of catecholamines and inhibiting their reuptake
What kind of Adrenergic Agonist might you use to treat Obesity?
Amphetamines or Ephedrine may be used as both have stimulant activity (which decreases appetite) due to the fact that they increase Sympathetic Outflow by stimulating the release of catecholamines and Amphetamines also inhibit their reuptake
What kind of Adrenergic Agonist might you use to treat Bronchial Asthma?
Albuterol could be used as it functions to cause Bronchodilation as a Selective B2 agonist.
What kind of Adrenergic Agonist might you use in order to achieve de Congestion of mucous membranes?
Phenylephrine or Ephedrine could be used as they both stimulate a1 Receptors to decrease Bronchial Mucous secretions
What kind of Adrenergic Agonist might you use to treat Anaphylaxis? (Bronchospasm, Upper Airway Congestion, Severe Hypotension, Cardiac Depression)
Epinephrine functions to correct all of the symptoms via a1, B1, and B2 activity
What kind of Adrenergic Agonist might you use to induce Mydriasis (Pupil Dilation)
Phenylephrine could be used as it functions to dilate the pupil via the contraction of the Radial Muscle of the eye via a1 receptors
What kind of Adrenergic Agonist might you use to treat Glaucoma?
Clonidine or another a2 selective agonist could be used in order to decrease sympathetic outflow
What kind of Adrenergic Agonist might you use to treat stress urinary incontinence?
Ephedrine could be used as it functions to increase sympathetic outflow by stimulating the release of catecholamines and has a long duration of action (as it is not a catecholamine itself)
What kind of Adrenergic Agonist might you use to treat Depression?
Phenelzine, Selegiline could be used as they function to inhibit MOA and thus increase the concentration of NE, E, and DA in the CNS
Phentolamine
CLASS:
MOA:
Phentolamine
CLASS: Non-Selective, Competitive (Reversible) a Adrenergic Antagonist
MOA: non-covalent binds to a AR’s to suppress sympathetic activity
Phenoxybenzamine
CLASS:
MOA:
Phenoxybenzamine:
CLASS: Non-selective, Non-Competitive (Irreversible) a Adrenergic Antagonist
MOA: Covalent binds to a AR’s to suppress Sympathetic Outflow.
What suffix do all Selective a1 Antagonists end in? What are the 3 examples we discussed in class?
All Selective a1 Agonists end in “-osin”
Prazosin
Tamsulosin
Doxazosin
What kind of Adrenergic Antagonists might you use to treat a Pheochromocytoma?
Phentolamine or Phenoxybenzamine could be used as they are both Non-Selective a AR Antagonists
What kind of Adrenergic Antagonists might you use to treat Chronic (Essential) HTN?
Prazosin or Doxazosin could be used as both are Selective a1 Antagonists and can thus both stimulate a decrease in TPR and subsequent BP. They are both well tolerated in work well in treating Moderate HTN
What kind of Adrenergic Antagonists might you use to treat Erectile Dysfunction?
A combination of Phentolamine (Non-specific a Antagonist) and a non-specific Vasodilator, Papaverine (which is injected directly into the penis)
What kind of Adrenergic Antagonists might you use to treat Chronic Urinary Obstruction resulting from BPH?
Tamsulosin could be used as it is more selective specifically for a1A Receptors than a1B Receptors, and a1A Receptors are the type primarily found in Prostatic Smooth Muscle. This allows Tamsulosin to relax Prostatic Smooth Muscle to treat Urinary Obstruction and the pain caused by it without causing a significant drop in the patient’s BP (which Prazosin and Doxazosin would).
What type of Adverse Effects might one see with a Adrenergic Antagonists, more specifically non-selective ones?
Postural Hypotension Tachycardia (via the BR) Fluid and Salt retention Impaired Ejaculation Nasal Stuffiness
What are the 2 Mixed (B & a1) Adrenergic Antagonists we discussed? Are they Full Antagonists, Partial Antagonists, or Inverse Antagonists?
Labetolol - Partial Antagonists
Carvedilol - Inverse Antagonist
Labetolol
CLASS:
Labetolol
CLASS: Mixed (B & a1) Partial Agonist
Carvedilol
CLASS:
Carvedilol
CLASS: Mixed (B & a1) Inverse Agonist
Propanolol
CLASS:
Propanolol
CLASS: Non-Selective B Full Antagonist
Pindolol
CLASS:
Pindolol
CLASS: Non-Selective B Partial Agonist
Nadolol
CLASS:
Nadolol
CLASS: Non-Selective B Full Antagonist
Metoprolol
CLASS:
Metoprolol
CLASS: Selective B1 Inverse Agonist
Betaxolol
CLASS:
Betaxolol
CLASS: Selective B1 Full Antagonist
Acebutolol
CLASS:
Acebutolol
CLASS: Selective B1 Partial Agonist
Atenolol
CLASS:
Atenolol
CLASS: Selective B1 Full Antagonist
Do Antagonists have Intrinsic Activity?
Antagonists do not have Intrinsic Activity, but Partial Agonists and Inverse Agonists do
What is the advantage of using Partial Agonist Beta Blockers?
Partial Agonist Beta Blockers (Acebutolol, Labetolol, Pindolol) have ISA (Intrinsic Sympathomimetic Activity) and thus are capable of producing a blunted sympathetic response, or a sympathetic response which is less that maximal but not completely absent. This creates less risk for Bradycardia, VLDL/HDL increase, and other effects of Beta Receptor Blockades caused by Full Antagonists
What Beta Blocker Drug may be used to Treat Hyperthyroidism, especially the severe form?
Propanolol may be used to treat Severe Hyperthyroidism’s effects on the heart as it is a Selective B1 Full Antagonist
What Beta Blocker Drug may be used to treat Glaucoma?
Betaxolol, a Selective B1 Full Antagonist (w/o local anesthetic Properties), may be used to treat Glaucoma by decreasing the intraocular pressure by reducing the production of aqueous humor. (Propanolol is not used)
