Adrenergic Agonists/Antagonists

What category is/are

Epinephrine, Norepinephrine, Dopamine?

Direct, Non-selective adrenergics

What category is/are
PHENYLEPHRINE (Pseudoephedrine Oxymetazoline, Tetrahydrozoline, Midodrine, Naphazoline, Xylometazoline)

Direct, Alpha 1 adrenergics

What category is/are
Apraclonidine, Clonidine, Methyldopa (Guanfacine, Guanabenz, Dexmedetomidine,Tizanidine)

Direct, Alpha 2 adrenergics

What category is/are

Dobutamine

Direct, Beta 1 adrenergics

What category is/are

Salbutamol, Albuterol, terbutaline, Isoxuprine, Ritodrine

Direct, Beta 2 Adrenergics

What category is/are

Phenylpropanolamine

Indirect, releasers

Two types of Indirect adrenergics

Releasers, Reuptake inhibitors

What category is/are

Phenoxybenzamine

Alpha, Non-selective, Irreversible antagonists

What category is/are

Phentolamine (Tolazoline)

Alpha, non-selective, reversible antagonist

What category is/are
Prazosin (Doxazosin, Terazosin, Tamsulosin, Silodosin, Alfuzosin)

Alpha 1 antagonist

What category is/are

Propranolol (Pindolol, Timolol, Labetalol, Carvedilol, Nadolol, Levobunolol, Metipranolol, Carteolol)

Non-selective, Beta antagonist

What category is/are

Atenolol (Betaxolol, Bisoprolol, Esmolol, Acebutolol,Alprenolol, Metoprolol, Nebivolol)

Beta 1 antagonist

Uses: Cardiac arrest, Anaphylaxis (DOC), Asthma, COPD, Hemostasis

SE: Hypertension, Tachycardia, Ischemia, Hyperglycemia

Notes: Inactive PO: do not enter CNS significantly; short DOA; can cross placenta (may cause fetal anoxia)

Epinephrine

Uses: Neurogenic shock, Cardiogenic shock (last resort)

SE: Extreme vasospalsm, Tissue necrosis, Excessive BP increase, Arrythmias, infarction, Reflex Bradycardia

Notes: Compensatory vagal reflexes tend to overcoe the direct positive airect posilive chronotropic effects; Alpha>Beta; Inactive PO; do not enter CNS significantly; short DOA

Norepinephrine

D1: vasodilation in splanchnic & renal blood vessels

Uses: Cardiogenic shock, heart failure

SE: CVS disturbance, arrhytmias

Notes: Inactive PO; do not enter CNS significantly; short DOA; very effective in renal failure associated with shock

Dopamine

Uses: Nasal congestin, mydriatic, drug-induced hypotension, orthostatic hypotension, spinal shock

SE: Rebound nasal congestion (Rhinitis medicamentosa);supine HPN, stroke, MI, piloerection, urinary retention

PHENYLEPHRINE (Pseudoephedrine Oxymetazoline, Tetrahydrozoline. reanydrozom Midodrine, Naphazoline, Xylometazoline)

Avoid ___ in 1st term, may cause Gastroschisis

Pseudoephedrine

Uses: HPN, Cancer pain, Opioid withdrawal

SE: Sedation, rebound HPN, dry mouth

Taper use prior to d/c to avoid rebound HPN;

When taken PO, there is initial increase in BP then will go down once the drug enters the CNS

Clonidine

Treat rebound HPN caused by clonidine with ___

Phentolamine

Uses: Preecmplasia, GHPN, sedative (Dexmedetomidine), muscle relaxant (Tizanidine)

SE: Sedation, Hemolytic Anemia (+) Coomb's test

Metyldopa

What Alpha 2 adrenergic is a sedative

Dexmedetomidine

What Alpha 2 adrenergic is a muscle relaxant

Tizanidine

Drug of choice for gestational hypertension

Methyldopa

Drug of choice for hypertensive urgency

Clonidine

MOA: decreases secretion of aqueous humor

Uses: Glaucoma

SE: Blurring of vision, dry mouth, hyperemia, pruritus, eye discomfort

Apraclonidine (Brimonidine)

MOA: B1: increase HR & contractility

Uses: Acute heart failure, Cardiogenic shock

SE: Tachycardia, arrhythmias, tachyphylaxis, HPN, eosinophilic myocarditis, premature ventricular beats, angina, dysnea, fever, HA, nausea

Dobutamine

Use is for acute asthma attack

Salbutamol

Use is for Tocolysis for preterm labor

Terbutaline, Ritodrine, Isoxuprine

SE: tachycardia, tremors,nervousness,restlessness, arrhythmias when used excessively,loss of responsiveness (tolerance)

May precipiate arrhythmias in COPD and heart disease

Beta 2 adrenergics

used as vasodilator in Reynaud's phenomenon; may causematernal pulmonary edema

Isoxuprine

MOA: Act mainly by causing release of NE, but also has direct agonist activity at some adrenegic receptors; activates A & B adrenegic receptors in respi mucosa

Uses: nasal vasoconstrictor, appetite supressant

May preciptate Hemorrhagic stroke esp in women

Phenylpropanolamine

MOA: blocks A1>A2 irrerversibly

Uses: Pheochromocytoma (presurgical)

SE: Orthostatic hypotension, Reflex tachycardia, GI irritation, MI

Forms covalent bond w alpha receptors (effects last for several days)

Phenoxybenzamine

MOA: blocks A1>A2 rerversibly

Uses: Pheochromocytoma (presurgical), Antidote to A1 agonist overdose, Rebound HPN

SE: Orthostatic hypotension, Reflex tachycardia, GI irritation

Phentolamine (Tolazoline)

MOA: Blocks A1 adrenergic receptors

Uses: BPH, HPN

SE: First dose orthostatic hypotension, Reflex tachycardia (less chance), dizziness, drowsiness, headache, weakness, asthenia, nausea, edema

Alpha 1 antagonists (-zosin)

most selective for prostatic smooth muscle

Tamsulosin

not indicated in females for tx of HPN

Doxazosin, Tamsulosin, Silodosin & Alduzosin

MOA:blocks B1 & B2 receptors. Blocks sympathetic effects on heart & BP. Reduces renin release

Uses: Angina prophylaxis, HPN, Arrythmias, migraine, performance anxiety, hyperthyroidism, glaucoma

SE: bronchospasm, AV block, heart failure, CNS sedation, erectile dysfunction

Notes: May mask symptoms of hypoglycemia in DM

Non-selective Beta antagonists

combined A & B blockade (may used in pheochromocytoma)

Carvedilol & Labetalol

IUGR, small placenta & congenital abnormalities have been reported with use, but no adequate & well-contracted studies conducted

Propranolol

used as ophthalmic drops for Glaucoma

METIPRANOLOL

MOA: selectively blocks B1 receptors. Blocks sympathetic effects on heart & BP

Uses: Angina, HPN, heart failure, SVT (Esmolol only)

SE: Bronchospasm (less chance), AV block, heart failure, CNS sedation, erectile dysfunction

Notes: Masks symptoms of hypoglycemia in DM

Beta 1 antagonists

shortest half life of Beta 1 antagonists

Esmolol

may also be used as ophthalmic solution for glaucoma

Betaxolol

use of this cardioselective BB during pregnancy has been shown to lower birthweights & impair fetal growth

Atenolol