Adrenergic agonist – a1 selective (a1 >> a2) Long acting (no OH) B1/A1 receptor stimulant - vasoconstriction, mydriasis, piloerection, increased cardiac output, inhibit GI motility Hyperactive sympathetic symptoms Vasopressor (hypotension – not shock)

Adrenergic agonist – a1 selective Vasoconstriction, mydriasis, piloerection, increased cardiac output, inhibit GI motility Hyperactive sympathetic symptoms

Adrenergic agonist – a1 selective (a1 = a2) Long acting (no OH) - vasoconstriction, mydriasis, piloerection, increased cardiac output, inhibit GI motility Hyperactive sympathetic symptoms Nasal decongestant, vasopressor, mydriatic, overcome hypotension, local vasoconstrictor

- a-methyldopa - Clonidine - Guanabenz

Adrenergic agonist – a2 selective Inhibit NE release by nerve terminal - decreased total peripheral resistance, HR, and cardiac output) Sedation, xerostomia, anorexia, fluid retention, vivid dreams, CNS stimulation Can be used for hypertension

Adrenrgic agonist – mixed a/b Hyperactive sympathetic symptoms Open angle glaucoma

Adrenergic agonist – mixed a/b – a1 = a2, B1>>B2 Vasoconstriction to increase peripheral resistance (a1 receptors) and increase cardiac output (B1 receptors) Hyperactive sympathetic symptoms Vasopressor (shock) (IV only)

Adrenergic agonist – B1 selective Increase force cardiac contraction, increase cardiac output Hyperactive sympathetic symptoms Congestive heart failure, cardiogenic shock following MI

Adrenergic agonist – B non-selective Very potent B agonist with very little a activity - relax bronchial smooth muscle (B2 stimulation), cardiac stimulant (B1), vasodilator Hyperactive sympathetic symptoms AV block, asthma – increase in cardiac output and decreased MAP with vasodilation

Adrenergic agonist – B2 selective Skeletal muscle vasodilation, smooth muscle relaxation Hyperactive sympathetic symptoms Bronchial asthma

Adrenergic agonist – B2 selective Skeletal muscle vasodilation, smooth muscle relaxation Hyperactive sympathetic symptoms Vasopressor (hypotension – not shock), bronchial asthma

Adrenergic agonist – B2 selective Relax bronchial smooth muscle Hyperactive sympathetic symptoms Asthma, relax pregnant uterus

Adrenergic agonist – dopamine (D2) Decreases neurotransmitter release Postural hypotension, cardiac arrhythmias Anti-parkinson agent with CNS effects

Adrenergic agonist – dopamine, D1 = D2 Vasoconstriction (a1), increase cardiac output (B1), dilate renal blood vessels (DA1) Hyperactive sympathetic symptoms Vasopressor, very effective for shock, cardiogenic shock following MI

Andrenergics Flashcards by Greg Esparza

Metaraminol

Adrenergic agonist – a1 selective (a1&raquo_space; a2)
Long acting (no OH) B1/A1 receptor stimulant - vasoconstriction, mydriasis, piloerection, increased cardiac output, inhibit GI motility
Hyperactive sympathetic symptoms
Vasopressor (hypotension – not shock)

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Methoxamine

Adrenergic agonist – a1 selective
Vasoconstriction, mydriasis, piloerection, increased cardiac output, inhibit GI motility
Hyperactive sympathetic symptoms

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Phenylephrine

Adrenergic agonist – a1 selective (a1 = a2)
Long acting (no OH) - vasoconstriction, mydriasis, piloerection, increased cardiac output, inhibit GI motility
Hyperactive sympathetic symptoms
Nasal decongestant, vasopressor, mydriatic, overcome hypotension, local vasoconstrictor

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a-methyldopa
Clonidine
Guanabenz

Adrenergic agonist – a2 selective
Inhibit NE release by nerve terminal - decreased total peripheral resistance, HR, and cardiac output)
Sedation, xerostomia, anorexia, fluid retention, vivid dreams, CNS stimulation
Can be used for hypertension

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Amphetamine

*Adrenergic agonist – mixed a/b, 
NE releasing agent
*Block NE reuptake and reverse transport to release intraneuronal NE (a1 and B1 receptors)
*Hyperactive sympathetic symptoms
*Vasopressor

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Ephedrine

*Adrenergic agonist – mixed a/b,
NE releasing agent
*Long acting (no OH), directly stimulates a1 and B1 receptors - relax bronchial smooth muscle (B2), elevation of cardiac output and arterial pressure
*Hyperactive sympathetic symptoms
*Vasopressor, mydriatic, nasal decongestant, CNS stimulant, chronic orthostatic hypotension, stress incontinence

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Dipivefrin

Adrenrgic agonist – mixed a/b
Hyperactive sympathetic symptoms
Open angle glaucoma

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Epinephrine

*Adrenergic agonist – mixed a/b – a1 = a2, B1 = B2
*B receptors are 10x more sensitive than A – low dose will see only B effects
Relax bronchial smooth muscle, very potent vasoconstrictor and cardiac stimulant, decreased total peripheral resistance (B2)
*Hyperactive sympathetic symptoms
*Anaphylactic shock, severe allergic reactions, open glaucoma, slow profuse bleeding, increase systolic BP (B1/A1 effects), heart block/cardiac arrest

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Norepinephrine

Adrenergic agonist – mixed a/b – a1 = a2, B1»B2
Vasoconstriction to increase peripheral resistance (a1 receptors) and increase cardiac output (B1 receptors)
Hyperactive sympathetic symptoms
Vasopressor (shock) (IV only)

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Dobutamine

Adrenergic agonist – B1 selective
Increase force cardiac contraction, increase cardiac output
Hyperactive sympathetic symptoms
Congestive heart failure, cardiogenic shock following MI

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Isoproterenol

Adrenergic agonist – B non-selective
Very potent B agonist with very little a activity - relax bronchial smooth muscle (B2 stimulation), cardiac stimulant (B1), vasodilator
Hyperactive sympathetic symptoms
AV block, asthma – increase in cardiac output and decreased MAP with vasodilation

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Albuterol

Adrenergic agonist – B2 selective
Skeletal muscle vasodilation, smooth muscle relaxation
Hyperactive sympathetic symptoms
Bronchial asthma

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Metaproterenol

Adrenergic agonist – B2 selective
Skeletal muscle vasodilation, smooth muscle relaxation
Hyperactive sympathetic symptoms
Vasopressor (hypotension – not shock), bronchial asthma

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Terbutaline

Adrenergic agonist – B2 selective
Relax bronchial smooth muscle
Hyperactive sympathetic symptoms
Asthma, relax pregnant uterus

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Bromocriptine

Adrenergic agonist – dopamine (D2)
Decreases neurotransmitter release
Postural hypotension, cardiac arrhythmias
Anti-parkinson agent with CNS effects

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Dopamine

Adrenergic agonist – dopamine, D1 = D2
Vasoconstriction (a1), increase cardiac output (B1), dilate renal blood vessels (DA1)
Hyperactive sympathetic symptoms
Vasopressor, very effective for shock, cardiogenic shock following MI

Doxazosin

Adrenergic antagonist – a1 selective&raquo_space;» a2
Vasodilation
Excessive dilation
Urinary obstruction

Prazosin

Adrenergic antagonist – a1 selective&raquo_space;» a2
Competitive reversible - little or no tachycardia due to a1 selectivity, vasodilation
Hypotension
Hypertension – oral – 12 hours – urinary obstruction

Tamsulosin

- Terazosin

Adrenergic antagonist – a1 selective&raquo_space;» a2
Vasodilation
Excessive dilation
Urinary obstruction

Phenoxy-benzamine

Adrenergic antagonist – a non-selective a1 > a2
Noncompetitive irreversible – alkylates a1 and a2 (can’t bind NE) and inhibits NET (NE can’t reuptake) - postural hypotension and tachycardia (reflex activation of adrenergic nervous system)
Hypotension
Lasts about 24 hours – oral or IV – pheochromocytoma (management of hypertension post-op)

Phentolamine

Adrenergic antagonist – a non-selective a1 = a2
Competitive reversible – inhibits both a1 and a2 - vasodilation, but increased NE release (increased cardiac output and tachycardia)
Dirty drug – activity with muscarinic receptors and histamine
Pheochromocytoma – preoperative management of hypertension/ inoperative or metastatic tumors

Labetalol

Adrenergic antagonist – mixed a/b – B1 = B2 > a1 > a2
Inhibit cardiac output, causes vasodilation
Cardiac failure
Anti-hypertensive

Atenolol

Adrenergic antagonist – B1 selective&raquo_space;» B2
Cardiac specificity - 6-9 hours – inhibit cardiac output
Fewer CNS effects – inability to cross BBB – caution with asthma and COPD – cardiac failure
Effective anti-hypertensive w/o constriction of bronchial smooth muscle (asthma)

Betaxolol

Adrenergic antagonist – B1 selective&raquo_space;» B2
Cardiac specificity - 14-22 hours – inhibit cardiac output
Caution use with asthma/COPD – cardiac failure
Effective anti-hypertensive w/o constriction of bronchial smooth muscle (asthma), open glaucoma

Metoprolol

* Adrenergic antagonist – B1 selective >>>> B2 * Cardiac specificity – effective prophylactic agent to prevent recurrence of MI - 3-4 hours – inhibit cardiac output * Caution use with asthma/COPD, ataxia and dizziness – cardiac failure * Effective anti-hypertensive w/o constriction of bronchial smooth muscle (asthma)

Nadolol

* Adrenergic antagonist – B nonselective B1 = B2 * 14-24 hours – inhibits cardiac output * Fewer CNS effects – inability to cross BBB – cardiac failure * Antihypertensive

- Carteolol - Levobunolol - Metipranolol

* Adrenergic antagonist – B nonselective * Reduce aqueous humor production – block B1 on ciliary body * Open angle glaucoma

Pindolol

* Adrenergic antagonist – B nonselective B1 = B2 * 3-4 hours – inhibits cardiac output * Cardiac failure * Antihypertensive

Propranolol

* Adrenergic antagonist – B nonselective B1 = B2 * 3-6 hours – inhibits cardiac output * Ataxia and dizziness, cardiac failure * Antihypertensive, anti-arrhythmic, angina pectoris, migraines, prophylactics to prevent MI

Timolol

* Adrenergic antagonist – B nonselective B1 = B2 * 4-5 hours – inhibits cardiac output * Cardiac failure * Prophylactics to prevent MI, antihypertensive, angina pectoris, decrease IOP (glaucoma)

a-methyldopa

* False transmitter * Enters both PNS and CNS – replaces DOPA in synthetic pathway (a-methyl NE is made) - Potent stimulation within brainstem affecting vasomotor center - hypotension * Sedation, dizziness, sleep disturbances, impotence, dry mouth, nasal congestion, postural hypotension * Antihypertensive agent

Guanethidine

* Synaptic vesicle depletion and membrane depolarization * Transported into adrenergic neurons via NET – reduces NE release * Minimal adverse side effects – doesn’t cross BBB * Orally effective hypertensive agent

Reserpine

* Synaptic vesicle depletion (pre-junctional) * Depletes stores of NE in both CNS and PNS by blocking transport into vesicles * Primarily in CNS (sedation, depression), increased GI motility (ulcers) * Very potent, orally effective, long duration

- Cocaine | - DMI (desmethyl-imipramine)

* Amine I transport inhibitor * Synaptic levels of NE rise and allow further sympathetic simulation * Hyperactive sympathetic stimulation * Hemostasis during surgery

Tyramine

* NE releasing agent * Increases NE release into synapse – increased sympathetic effects * Potentially dangerous for individuals on MAO inhibitors (elevates arterial pressure) * Vasopressor (shock or hypotension)

Pseudoephedrine

* NE releasing agent * Increases NE release into synapse * Nasal congestion

- Acetazolamide - Dichlorphenamide - Dorzolamide

* Carbonic anhydrase inhibitor * Reduce HCO3 production (required for aqueous humor production) * Decrease aqueous humor production – open angle glaucoma

Botulinum Toxin A

* Misc. ophthalmology * Blocks ability of ACh vesicles to move to nerve terminal surface and fuse – leads to relaxation in skeletal muscle * Blepharospasm (eyelid problem) and squinting (extraocular muscles)