Adrenergic Drugs Flashcards
Epinephrine (Adrenalin)
Catecholamine. High affinity for Beta-2 receptors.
Norepinephrine (Levophed)
Catecholamine. Less effect on Beta-2 and more effect on Beta-3.
Isoproterenol (Isuprel)
Catecholamine. Equal affinity for all beta receptors.
Phenylephrine (Neofrin; neosynephrine)
Alpha-1 agonist
Pseudoephedrine (Sudafed)
Alpha-1 agonist
Xylometazoline (Otrivin)
Alpha-1 agonist
Oxymetazoline (Afrin)
Alpha-1 agonist
Midodrine (ProAmatine)
Alpha-1 agonist
Clonidine (Catapress)
Alpha-2 agonist
Methyldopa (Aldomet)
Alpha-2 agonist
Apraclonidine (Iopidine)
Alpha-2 agonist
Dobutamine (Dobutrex)
Beta-1 agonist
Albuterol (Ventolin)
Beta-2 agonist
Ritodrine (Yutopar)
Beta-2 agonist
Mirabegron (Myrbetriq)
Beta-3 agonist
Ephedrine
“other” adrenergic stimulant
Amphetamine
“other” adrenergic stimulant
Methylphenidate (Ritalin)
“other” adrenergic stimulant
Methamphetamine
“other” adrenergic stimulant. Increases the release of NE from the presynaptic terminal so there must be an intact innervation
Cocaine
“other” adrenergic stimulant. inhibits reuptake of NE.
Tyramine
“other” adrenergic stimulant. Increases the release of NE from the presynaptic terminal so there must be an intact innervation
Dopamine (Intropin)
Dopamine agonist
Fenoldopam (Corlopam)
Dopamine agonist
VMA/HVA test
Measures the metabolism of NE and Epi.
Alpha-1 agonist effects
Vasoconstriction of peripheral vessels, nasal mucosa. Mydriasis. Contraction of the prostate and GU smooth muslce. Erection of hair (pilomotor).
Alpha-2 agonist effects
Act presynaptically to inhibit transmitter release. Cause aggregation of platelets and contraction of vascular smooth muscle. Decreases insulin release.
Beta-1 agonist effects
Increases force of contraction and AV conduction. Increases renin secretion from the kidney.
Beta-2 agonist effects
Relax respiratory, uterine and GI smooth muscle. Vasodilate vessels supplying skeletal muscles. Increase potassium uptake into muscle. Increase glycogenolysis and gluconeogenesis.
Beta-3 agonist effects
Increase lipolysis in fat cells
Alpha receptor effects on the heart
Increased arterial resistance in small blood vessels. Increased BP leads to baroreceptor reflex that slows the HR.
Alpha receptor effects on the eye
Mydriasis. No accommodation. Decreases intraocular presure.
Alpha receptor effects on the respiratory system
vasoconstricts the vessels in the nasal mucosa. Act as a decongestant.
Alpha receptor effects on the GU
Constrict the sphincters to promote continence. Promotes ejaculation.
Beta receptor effects on the Heart
Increased contractility and conduction through the AV node. Increases automaticity. Increased coronary and skeletal muscle blood flow (decreased diastolic BP)
Beta receptor effects on the eye
increased intraocular pressure.
Beta receptor effects on the respiratory tract
relax bronchial smooth muscle
Beta receptor effects GU
Relaxes the uterus
Beta receptor effects on metabolism
Increased renin secretion. Glycogenolysis. Increased uptake of potassium. Increased insulin secretio. Lipolysis.
Norepinephrine MOA
Stimulates alpha (vasoconstriction) and beta 1 receptors with little effect on beta 2. Must be injected.
Norepinephrine effects
Increases BP with a slight decrease in HR (vagal reflex). Atropine can inhibit the vagal reflex if given prior to NE and the HR will increase. Used rarely during severe hypotensive crisis.
Norepinephrine adverse side effects
Vasoconstriction at the infusion site can cause necrosis.
Epinephrine MOA
Must be injected. Stimulates alpha (Vasoconstriction) , beta 1 (Inotropy/chronotropy) and beta 2 (Vasodilation in skeletal muscle) receptors. Short duration of action.
Epinephrine effects
Increased pulse pressure. Increased BP and increased HR. Increases blood glucose and FFA concentrations. Increased renin secretion.
Epinephrine infused slowly
Beta 1 increases HR and contractility. Increases coronary blood flow. Alpha receptors increase systolic and diastolic BP. Beta 2 decreases diastolic pressure therefore increasing the pulse pressure. No change in mean BP shows little vagal reflex so HR is increased.
Epinephrine rapid infusion
Increases blood pressure with a slight increase in HR.
Epinephrine uses
anaphylactic shock, cardiac arrest, complete heart block, vasoconstictor to decrease diffusion of local anesthetics, glaucoma, asthma (bronchodilation).
Epinephrine side effects
Tremor, throbbing HA, increased BP, tachycardia, angina
Epinephrine contraindications
Beta blocker use. Can cause severe hypertension.
Epinephrine Dose dependence
Vasodilation dominates at low doses while vasoconstriction at high doses.
Ephedrine MOA
Stimulates alpha and beta receptors. Long duration of effect.
Ephedrine effects
Increases HR and BP. Causes bronchodilation.
Ephedrine adverse effects
hemorrhagic stroke and death due to severe hypertension.
Phenylephrine MOA
Alpha 1 agonist.
Phenylephrine effects
Vasoconstriction increases BP with a reflex decrease in HR.
Phenylephrine uses
Hypotensive emergency, decongestant, mydriasis.
Pseudophedrine uses
decongestant. Use caution in those with HTN.
Xylometazoline MOA
Alpha receptor stimulant
Xylometazoline and Oxymetazoline uses
topically as nasal sprays to decrease congestion.
Oxymetazoline MOA
Alpha receptor stimulant. Also acts on alpha 2 receptors and can cause hypotension is a large amount is absorbed.
Xylometazoline and Oxymetazoline contraindications
narrow-angle glaucoma
Clonidine MOA
Acts on alpha 2 receptors in the brain to decrease release of NE and overall SNS output. Used as a transdermal patch.
Clonidine uses
treatment of HTN, reduces addictive cravings, decreases hot flashes, used pre-anesthetically to cause sedation.
Clonidine adverse side effects
dry mouth, sedation, sexual dysfunction. Avoid getting the patch hot because it causes a large release of clonidine leading to hypotension. Abrupt withdrawal can cause rebound HTN.
Methyladopa uses
similar to clonidine.
Apraclonidine uses
Used in the eye to decrease intraocular pressure
Tizanidine uses
Less effective on lowering BP but effective at reducing muscle spasticity.
Isoproterenol MOA
Beta 1 and Beta 2 agonists
Isoproterenol effects
Increases HR and force of contraction. Causes vasodilationand decreases BP.
Isoproterenol uses
Cardiac arrest and complete heart block
Isoproterenol adverse side effects
tachycardia, palpitations and arrhythmias.
Dobutamine MOA
Beta 1 agonist with some effect on alpha receptors
Dobutamine effects
Positive inotrope that increases CO. Increases BP and HR
Dobutamine uses
cardiac stress tests, cardiogenic shock and CHF.
Albuterol MOA
Beta 2 agonist. With little effect on Beta 1 receptors.
Albuterol uses
asthma
Albuterol adverse effects
HA, tachycardia, tremor.
Mirabegron MOA
Beta 3 receptor agonist
Mirabegron uses
treatment of overactive bladder.
Mirabegron adverse effects
nausea, HA, HTN, diarrhea, constipation, dizziness and tachycardia.
Low dose dopamine MOA
D1 receptors that cause vasodilation and increases renal blood flow.
High dose dopamine MOA
Stimulates Beta 1 receptors and produce a positive ionotropic and chronotropic effect.
Dopamine uses
Cardiogenic shock
Dopamine adverse effects
Nausea, vomiting, tachycardia, angina, arrhythmias, HA, and peripheral vasoconstriction.
Fenoldopam MOA
D1 agonsit
Fenoldopam effects
dilation of vascular beds which decrease BP.
Fenoldopam uses
Treatment of a hypertensive crisis.
Amphetamine MOA
increases the release of NE and DA
Amphetamine effects
alertness, insomnia, decreased appetite, euphoria, increases motor activity.
Amphetamine adverse effects
Psychosis, HA, chills, pallor, arrhythmias, HTN, cerebral hemmorhage, convulsions
Amphetamine uses
enuresis. Causes contraction of the bladder sphincter.
Methamphetamine uses
Recreational drug
Methylphenidate uses
(ritalin) ADHD
Cocaine MOA
inhibits re-uptake of DA and NE.
Cocaine effect
Vasoconstrictor. Can cause severe HTN.
Cocaine adverse effects
Stroke, arrhythmias, MI, tachycardia. Long-term use can causes psychosis.
Tyramine MOA
Increases the release of catecholamines from the nerve terminals. Usually hydrolyzed by MOA. Those treated for depression with MOA inhibitors that ingest large amounts of tyramine can have a HTN crisis.
Phentolamine (Regitine)
Alpha-receptor blocker. Reversible antagonist.
Phenoxybenzamine (Dibenzyline)
Alpha-receptor blocker. non competitive, irreversible antagonist.
Prazosin (minipress)
Alpha 1 blocker. Reversible antagonist.
Terazosin (Hytrin)
Alpha 1 blocker. Reversible antagonist.
Doxazosin (cardura)
Alpha 1 blocker. Reversible antagonist.
Alfuzosin (Uroxatral)
Alpha 1 blocker
Tamsulosin (Flomax)
Alpha 1 blocker
Yohimbine
Alpha 2 blocker
Propranolol (inderal)
Beta blocker
Timolol (timoptic)
Beta blocker
Nadolol (corgard)
Beta blocker
Metoprolol (Lopressor)
Cardiospecific/Beta1 blocker
Atenolol (Tenormin)
Cardiospecific/Beta1 blocker
Bisoprolol (zebeta)
Cardiospecific/Beta1 blocker
acebutolol (sectral)
Cardiospecific/Beta1 blocker with intrinsic sympathetic activity.
Esmolol (brevibloc)
Cardiospecific/Beta1 blocker
Betaxolol (betoptic)
Cardiospecific/Beta1 blocker
Nebivolol (bystolic)
Cardiospecific/Beta1 blocker
Pindolol (visken)
beta blocker with intrinsic sympathetic activity
Carteolol (Cartol)
beta blocker with intrinsic sympathetic activity
Carvedilol (Coreg)
Combo beta and alpha blocker
Labetalol (Normodyne)
Combo beta and alpha blocker
Guanethidine (ismelin)
Affects neurotransmitter release
Reserpine
Affects neurotransmitter release
Metryrosine (demsar)
synthesis inhibitor
Alpha 1 blockers effects
decrease BP, orthostatic hypotension, miosis, esier to urinate, inhibit ejaculation.
Alpha 2 blockers effects
increased NE and insulin release.
Beta blockers effects
Decreased HR and contraction, decreased renin secretion, bronchoconstriction, decreased glycogenolysis and lipolysis, decreased intraocular pressure.
Alpha blockade effects on the heart
Lowers peripheral resistance (postural hypotension). Reflex tachycardia. Used for epinephrine reversal to block it’s alpha effects and decrease BP.
Alpha blockade effects on the eye
Miosis
Alpha blockade effect on the nose
congestion due to vasoconstriction
Alpha blockade effect on the GU system
decreases resistance to urine flow (BPH) and inhibits ejaculation.
Phentolamine MOA
Competitive antagonist of alpha 1 and alpha 2 receptors.
Phentolamine effects
Decreases peripheral resistance with cardiac stimulation (reflex and increased NE due to alpha 2 block). Also causes gastric stimulation due to blockade of serotonin receptors.
Phentolamine uses
hypertensive crisis of to prevent necrosis of tissue where a vasoconstrictor has been injected.
Phentolamine adverse effects
tachycardia, arrhythmia, MI, Hypotension, abdominal pain, peptic ulcers.
Phenoxybenzamine MOA
irreversible alpha blocker that bind covalently to the receptor. Also inhibits reuptake of NE
Phenoxybenzamine effects
Decreases peripheral resistance.
Phenoxybenzamine uses
Treatment of pheochromocytoma.
Phenoxybenzamine adverse effects
Hypotension (if hypovolemic), postural hypotension, tachycardia, nasal congestion, inhibition of ejaculation. With Epi can cause hypotension and tachycardia.
Prazosin MOA
Highly selective for alpha one receptors. Well absorbed orally. Duration of action is 7-10 hours (given twice daily). Metabolized by the liver. Half life doubles in CHF (lower dose needed).
Prazosin effects
Decreases peripheral resistance (no increases in HR due to selectivity). Cardiac output doesn’t increase. Decreases SNS outflow from the CNS. Decreases LDL/Triglycerides and increases HDL.
Prazosin uses
HTN, BPH.
Prazosin adverse effects
First does phenomenon (postural hypotension/syncope 30-90 mins after first dose). Postural hypotension, dizziness, nasal congestion, sexual dysfunction. Don’t combine with drugs like viagra.
Terazosine MOA
Selective alpha one receptor blockade. 12 hour half life (given once daily).
Terazosine uses
BPH
Terazosine adverse effects
first dose phenomenon
Doxazosin MOA
Selctive alpha one receptor blockade. 20 hour half life
Doxazosin uses
BPH
Doxazosin adverse effects
first dose phenomenon
Tamsulosin MOA
Selective blockade for alpha 1a receptors (prostate). Half life of 5-10 hours. Metabolized by P450s.
Tamsulosin effects
Relaxes the prostate (alpha 1a) with little effect on BP (alpha 1b). Also relaxes the bladder sphincter.
Tamsulosin uses
BPH
Tamsulosin adverse effects
Difficulty ejaculating.
Alfuzosin uses
BPH
Alfuzosin adverse effects
dizziness
Yohimbine MOA
Selective alpha 2 antagonist that increases NE release
Yohimbine effects
Increases BP and HR. Increase in SNS may increase libido (“natural viagra”).
Yohimbine contraindications
dangerous in men with HTN.
Beta blocker effect on the heart
Slows the HR and decreases contractility. Slowed AV conduction. Reduced automaticity. Decreases the oxygen demand of the heart. With chronic use BP will be lowered due to decreased CO. Renin release is reduced. Initially BP may increase due to beta 2 blockade but over time BP will be reduced.
Beta blocker contraindications
Pheochromocytoma without concomitant administration of an alpha blocker. Those with asthma.
Beta blocker effects on the respiratory system
Beta 2 blockers will cause bronchoconstriction.
Beta blocker effects on the eye
reduce intraocular pressure
Beta blocker effects on metabolism
Inhibits lipolysis (increases VLFL and decreases HDL). Decreased glycogenolysis (beta 2). Can impair the ability of type 1 diabetics recovery from hypoglycemia. Can also mask the symptoms of hypoglycemia. Should use extreme caution when prescribing beta blockers for type 1 diabetics.
Beta blocker use as a local anesthetic
Acebutolol, labetalol, metoprolol, pindolol, propranolol. Membrane stabilizing through blockade of sodium channels. Don’t use an an anesthetic in the eye.
Propranolol MOA
Non-selective (beta 1 and 2) competitive antagonist.
Propranolol effects
Slows the HR, decreases AV conduction, decreases contractility, decreases renin release, decreases lipolysis and glycogenolysis. Can have local anesthetic effects.
Propranolol pharmacokinetics
Oral. Sustained release. Lipid soluble (CNS penetration). Metabolized in liver with a 3-6 hour half life.
Propranolol uses
Chronic use for HTN. Decreases mortality post-MI. Angina. Arrhythmias. CHF (when stable). Hyperthyroidism. Migraines. Reduces portal vein pressure in cirrhosis. Decreases tremors (“stage-fright”).
Propranolol adverse effects
Bronchoconstriction (especially in asthmatics). Exacerbation of CHF if unstable. Bradycardia, hypotension, sedation, fatigue. Can worsen vasospastic disorders. Can mask the symptoms of hypoglycemia and hyperthyroidism. Can increase VLDL and decrease HDL. Should not be discontinued abruptly due to rebound HTN (beta receptors have been upregulated).
Drugs that inhibit metabolism of Propranolol
cimetidine and chlorpromazine.
Drugs that increase metabolism of Propranolol
barbituates, phenytoin, rifampin and smoking. Calcium channel blockers can have an additive effect.
Timolol uses
Glaucoma. Can be used systemically like Propranolol.
Timolol contraindications
asthma
Nadolol uses
similar to Propranolol but has a longer half life. Doesn’t penetrate the CNS so less likely to cause sedation.
Sotalol uses
Blocks potassium channels and has class three antiarrythmic activity.
The beta 1 selective antagonists
Metroprolol, Atenolol and bisoprolol
beta 1 selective antagonists effects
Decreases HR and contractility. Does not block beta 2 receptors in the skeletal muscle vessels (better exercise tolerance) and is less likely to inhibit glycogenolysis (decreased risk of hypoglycemia).
beta 1 selective antagonists uses
HTN, post-MI, migraine prophylaxis.
beta 1 selective antagonists adverse effects
dizziness, fatigue, bradycardia and hypotension.
Atenolol and diabetes
Reduces the risk for type 2 diabetes.
beta 1 selective antagonists contraindications
Use caution in patients with COPD and asthma because the selectivity is not absolute and at high doses can effect beta 2 receptors.
Betaxolol MOA
selective beta 1 blocker. Less likely to cause bronchoconstriction than timolol.
Betaxolol uses
glaucoma
Nebivolol MOA
Selective beta 1 blocker that increases the release of Nitric oxide. Lowers BP without depressing LV function.
Nebivolol effects
Lowers BP (nitric oxide) and decreases cholesterol, triglycerides and BGL.
Esmolol MOA
selective beta 1 blocker with a very short duration of action (8 mins). Must be administered IV.
Esmolol Uses
Used when short blockade is needed or when necessary to rapidly remove the beta blocker effect.
Intrinsic Sympathetic activity
Means the drug is a partial agonist
Beta blockers with ISA uses
treatment of HTN and angina. Risk of bradycardia is lower than with other beta blockers.
Carteolol uses
Glaucoma
Beta blockers with ISA
Pindolol, carteolol, penbutolol. Acebutolol (selective Beta 1)
Labetalol MOA
Blocks Beta 1, Beta 2 and alpha 1 receptors.
Labetalol effects
Decreased BP without the compensatory increase in HR.
Labetalol uses
HTN emergencies
Carvedilol MOA
Non-selective beta blocker that also blocks alpha 1 receptors.
Carvedilol effects
Reduces BP without a compensatory increase in HR. Reduces the effects of free radicals on vascular smooth muscle.
Carvedilol uses
Decreases morbidity/mortality in CHF. Treatment of HTN.
Clinical uses of beta blockers
HTN, Ischemic heart disease, arrhythmias, obstructive cardiomyopathy, dissecting aortic aneurysm, hyperthyroidism, migraines.
Beta blockers that improve survival after an MI
Timolol, propranolol and metoprolol
Beta blockers that can be used in early CHF
Metoprolol, carvedilol and bisprolol.
Beta blockers to treat hyperthyroidism
propranolol
Beta blockers for migraine prophylaxis
propranolol, metoprolol and atenolol.
DOC for glaucoma
Prostaglandin analogues (latanoprost)
Beta blockers for glaucoma
Timolol, carteolol and betaxolol (beta 1 selective). Second line treatment. Decreases production of aqueous humor.
alpha 2 agonists for glaucoma
apraclonidine. Decreases production of aqueous humor and increases outflow.
Cholinergic agonist for glaucoma
Pilocarpine, carbachol, phyostigme and echothiophate. Rarely used because they effect vision.
Guanethidine MOA
Inhibits the release of NE. No longer used.
Reserpine MOA
Causes the depletion of NE, DA and serotonin by inhibitng uptake of biogenic amines.
Reserpine adverse effects
No longer used. Diarrhea, depression, sedation and parkinson’s like symptoms.
Metyrosine MOA
Tyrosine analogue that blocks tyrosine hydroxylase. Decreases the amount of DA, NE and Epi.
Metyrosine uses
Pre-surgical treatment of pheochromocytoma.
