?1
Eye
GI
Vasoconstriction
Bladder
Penis
?2
Vasoconstriction
?1
Heart
?2
Lung
Liver
GI
Vasodilation
Bladder
Uterus
?3
Bladder
Sympathetic Stimulation of Eye
Mydriasis
Sympathetic Stimulation of Lung
Bronchodilation
Sympathetic Stimulation of HEart
^ rate, contractility, and impulse conduction
Sympathetic Stimulation of Liver
^ glc release
Sympathetic Stimulation of GI Tract
Inhibit peristalsis
Sympathetic Stimulation of BV
Vasoconstrition and vasodilation
Sympathetic Stimulation of Urinary Bladder
Dec urination
Sympathetic Stimulation of Uterus
Relax
Sympathetic Stimulation of Penis
Ejaculation
?1 - Direct Acting Agonist
Epinephrine
Norepinephrine
Phenylephrine
?2 - Direct Acting Agonist
Epinephrine
Norepinephrine
Oxymetazoline
Brimonidine
Clonidine
Guanfacine
?1 - Direct Acting Agonist
Epinephrine
Norepinephrine
Isopreterenol
Dobutamine
?2 - Direct Acting Agonist
Epinephrine
Isoproterenol
Albuterol
Terbutaline
Salmeterol
Epinephrine
Endogenous hormone, not orally active. Rapidly metabolized by monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT).
From chromaffin cells in the Adrenal Gland; Only last a few minutes = not very clinically useful; Short duration of action, only
Norephinephrine
Endogenous neurotransmitter, not orally active. Rapidly metabolized by MAO and COMT.
From chromaffin cells in the Adrenal Gland; Only last a few minutes = not very clinically useful; Also short duration of action. Very low affinity at ?2, so won't work fo
Isoproterenol
Synthetic drug, other drugs = nylidrin, isoxsuprine.
B1 and B2. Used in asthma, but can cause palpitations, increase HR, etc d/t ?1 receptor
Phenylephrine
Synthetic drug, other drug = methoxamine.
Used for vasoconstriction
a1
Oxymetazoline
Synthetic drug, applied locally, peripheral acting, other drugs = brimonidine, naphazoline, tetrahydrozoline
Concentrated in the brain (Inhibit sympathetic nerve outflow from the brain)
Outside the brain
A2
Clonidine
Synthetic drug, acts in the CNS as an inhibitor, other drugs = guanfacine, lofexidine, methyldopa.
Gets into brain really well, along with Guanfacine.
A2
Dobutamine
Synthetic drug, other drug = dopamine. Dopamine is an endogenous neurotransmitter found in the brain. Dopamine stimulates dopamine receptors, b1-adrenergic receptors, a-adrenergic receptors and causes release of norepinephrine.
Catecholamine; NT in CNS; I
Albuterol
Synthetic drug, other drugs = terbutaline, salmeterol, formoterol, levalbuterol, pirbuterol.
Used to treat asthma by dilating the bronchioles. Used via inhalation
Mirabegron
Synthetic drug, new.
Selectively stimulates B3
Dextroamphetamine (Focalin)
Indirect Acting Agonist
R isomer, CNS active.
Commonly used to treat ADHD. Has the same effects and use as amphetamines
Long duration (12 hours): 1 x per day - Ritalin LA, Focalin XR
Amphetamine Mixture (Adderall)
Indirect Acting Agonist
CNS active (R) and less active (L) isomer.
Lisadexamfetamine (Vyvanse)
Indirect Acting Agonist
A prodrug of dextroamphetamine.
Methylphenidate (Ritalin)
Indirect Acting Agonist
Commonly used to treat ADHD. Has the same effects and use as amphetamines.
Short duration (4 hours): 2-3 x per day - Ritalin
Intermediate duration (8 hours): 2 x per day - Ritalin SR
Long duration (12 hours): 1 x per day - Ritalin
Pseudoephedrine
Mixed Acting Sympathomimetic Drugs
Act like both direct acting (stimulate receptors) and like indirect acting (release NE) drugs.
Used to treat nasal congestion
Can be converted to methamphetamine (potential abuse)
DOC Cardiac Arrest
Epinephrine (B1)
Ventricular fibrillation --> Normal cardiac rhythm
DOC Circulatory Shock
Treat with Dobutamine (B1) to increase the force, rate and conduction. Could use Dopamine, but this also dilates the renal vasculature to maintain renal profusion.
DOC Septic Shock
NE or phenylephrine to activate A1, constricts to treat
DOC Hypotension
Hypotension during anesthesia (reduce BP) - Phenylephrine, etc.
Cause vasoconstriction to maintain BP during surgery
DOC Bronchoconstriction
Albuterol: Acute; Rescue inhaler
Salmeterol: B2 agonists with long durations of action; Prevent bronchoconstriction
DOC Nasal Congestion
Oxymetazoline: Spray; Afrin
Phenylephrine:
Pseudoephedrine: Oral
Overactive Bladder Tx
Active B2 receptors to reduce detrusor so don't get the urge to urinate
Mirabegron
Preterm Labor DOC
B2 receptors on the pregnant uterus; Target B2 receptors to relax; Prevent pre-term labor; Selectively stimulates B2 receptors, which can become desensitized, so need to take a higher dose, causing stimulation of B1 (cardiovascular activation), which limi
Wide Open Angle Glaucoma Tx
Stimulates a2 receptors in the ciliary body (produce aqueous humor); If make less AH reduce the pressure and treat glaucoma; Give as eye drop because need directly at the eye
Brimonidine (a2)
Analphylaxis DOC
Epinephrine: ^ BP, dilate the airways, reduce inflammatory mediators; Stabilize Mast Cells so don't get mediators; Dilates airways; Relax tissues in the throat; ^ BP to relieve hypotension
Self-administered injectable to the thigh
Obesity - Appetite Suppression Tx
Phentermine + topiramate (Qsymia�; Anti-epileptic; Reduce CNS stimulation of Phentermine alone)
Increases monoamine neurotransmitters (dopamine, norepinephrine, serotonin) in the CNS.
ADHD Tx
Block removal of norepinephrine and dopamine from the synapse and stimulate release of norepinephrine and dopamine from CNS and peripheral nerves to cause:
CNS stimulation - ? focus, attention, alertness, mood, motor activity, talking; ? appetite, weight,
1st Generation/Nonselective Adrenergic Antagonists
Propranolol
Timolol
Pindolol
Block both ?1 and ?2 -adrenergic receptors.
2nd Generation/Nonselective Adrenergic Antagonists
Metroprolol
Atenolol
Selectively block ?1 (not just in the heart, but anywhere)-adrenergic receptors.
3rd Generation/Nonselective Adrenergic Antagonists
Labetalol
Carvedilol
Block multiple adrenergic receptors and have vascular relaxation activity
Alpha 1 Blockers
Phentolamine
Phenoxybenzamine
Tamsulosin
Doxazosin
Labetalol
Carvedilol
Alpha 2 Blockers
Yohimbine
Phentolamine
Phenozybenzamine
Hypertension - Tx
Alpha and Beta Blockers
Blood pressure of 120/80 mmHg is considered normal.
Doxazosin (Cardura), Terazosin (Hytrin), etc.
Alpha 1 more prevalent than beta 1and 2s
Not primary drugs
Atenolol (Tenormin), etc.
Antihypertensive Mechanisms of ? Blockers
? Card
Benign Prostatic Hyperplasia
Alpha Blocker
Alpha 1- adrenergic receptors in bladder sphincter and prostate smooth muscle
Tamsulosin (Flomax), etc.
At base of bladder, sphincter with alpha 1 receptors and on smooth muscle in prostate gland, which surrounds urethra at the end of the bl
Impotence Tx
Alpha Blocker
Yohimbe Tree Bark; treats sexual disinterest disorder
Phentolamine
Angina Pectoris Tx
Beta Blocker
Angina Pectoris is a characteristic type of chest discomfort (pain) associated with myocardial ischemia
Metoprolol (Lopressor), etc. For prevention
Reducing the need for O2; acutely on the tongue for angina, we can use nitroglycin? BB are DOC
Arrhythmias Tx
Beta Blockers - Metoprolol, Atenolol etc
Chronic Heart Failure Tx
Beta Blockers
Carvedilol and other ? blockers can be helpful.
Heart changes structure w heart failure, can activate the sympathetic NS to pump out more blood
As heart changes even more, the sympathetic activation is not helpful bc the chronic stimulation
Migraine Tx
Propranolol (B Blocker)
Mechanism isn't very clear
People with migraine typically have myoalgesia
Used to prevent, not used for acute headache
Glaucoma Tx
Beta Blockers
Timolol and other Beta-blocker drugs reduce AH formation