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Adrenergic Pharm Flashcards

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1
Q

List three important aspects of receptor interaction?

A
  1. Second messenger amplification
  2. Effector cell response
  3. Pre-synaptic receptors
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2
Q

Trace out the formation of and release of NE starting with what amino acid?

A
  1. Tyrosine in the circulation
  2. Tyrosine hydroxylase (convert tyrosine to DOPA)
  3. Dopa decarboxylase (make dopamine)
  4. Uptake into vesicle
  5. Conversion of dopamine to NE by dopamine beta-hydroxylase
  6. NE in the vesicle can be converted to epi in the adrenal medulla (chromaffin cells with ratio of epi to NE 4:1)
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3
Q

Epi is a ______, whereas norepi is a ______

A

Neurohormone; neurotransmitter

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4
Q

Adrenergic receptors have how many membrane-spanning helices? Beta1 channels help increase cAMP, but what else do they increase? How does D1 compare to beta 1, 2, 3?

A

7; activate voltage-sens Ca channels in heart;

uses the same mech of action (increase cAMP)

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5
Q

When NE’s done its job, list the three ways it can leave from the cleft?

A
  1. Neuron specific (re-uptake)
  2. Extraneuronal uptake in effector cells
  3. Some diffusion back into an e.g. capillary
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6
Q

For extraneuronal uptake in effector cells, what two enzymes will metabolize e.g. NE? Where can this happen?

A

MAO (mito surface) and catechol-O-methyltransferase (cytoplasm of many cells, NOTABLY LIVER);
this process is VERY PROMINENT in the LIVER

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7
Q

For synthesis of the transmitter, release of transmitter, combining with receptor, and termination step, what can be used to agonize or antagonize each step?

A
  1. Trans synthesis: alpha me tyrosine ANTAGONIZES
  2. Trans release: bretylium antagonizes, amphetamine agonizes
  3. Combine w/ receptor: isoproterenol agonizes, propranolol antagonizes
  4. Cocaine agonizes termination step
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8
Q

Beta1 receptor prominent effector organs

A

Heart: increased HR, force of contraction
Kidney: renin secretion (JGA)

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9
Q

Beta 2 prominent effector organs and response

A

Arterioles (and arteries in skeletal muscle, coronary): dilation;
Bronchial muscle, pregnant uterus: relaxation
Several sites: increased metabolic effects

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10
Q

Beta 3 prominent effector organs and response

A

Adipose tissue (lipocytes): lipolysis, thermogenesis (increased)

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11
Q

Alpha1 prominent effector organs and response (skim milk victimizes kids)

A

Arterioles in skin, mucosa, viscera, kidney (resistant vessels): constriction;
Veins: constriction;
Uterus and Spleen: contraction

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12
Q

Alpha2 prominent effector organs and response

A

Presyn nerve endings: inhibit NE release and ACh release (gut);
Postsyn in CNS: decreased peripheral symp tone

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13
Q

D1 prominent effector organs and response

A

Renal, mesenteric, and cerebral arterioles: dilation

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14
Q

Idea of autoreceptors and heteroreceptors?

A

NE can stim presyn alpha2 receptors and inhibit NE release from the nerve terminal;
NE can control e.g. release of ACh from parasymps and result in relaxation of the gut

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15
Q

For blood vessels in skeletal muscle, which receptor has the dominant tone? What’s activated in low/high NE concentrations?

A
  1. alpha1
  2. At low concentrations of NE, or physiological, you have beta2 receptors activated, promoting relaxation and vasodilation
  3. At high concentrations of NE, like in shock, alpha1 receptors DOMINATE!!
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16
Q

Difference between norepi, epi and isoproterenol in terms of selectivity?

A

Norepi: H on N, means alphas and beta ONE
Epi: CH3 on N, means alphas and BOTH BETAS
Isoproterenol: Isopropyl group on N, means BETAS

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17
Q

Some tricks for knowing agonist potencies at adrenergic receptors?

A
  1. Epi is always greater than or equal to NE EXCEPT for beta2 receptors, since NE shouldn’t have selectivity for that
  2. Isoproterenol is best for beta2 and beta1 because of the isopropyl group; but obviously worst at ALPHAS!!
  3. CLON is best at alpha2 since it’s selective for it
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18
Q

Tyramine is a(n)

A

indirect agent that causes release of NE to allow it to interact with postsynaptic receptor

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19
Q

Norepinephrine (Levophed)

A

Class: Non-selective agonist
Mech: Agonist: α1, α2, β1
Thera: Acute Hypotension
Important SE’s: Hypertension; arrythmias; headache

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20
Q

Epinephrine

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A

Class: Non-selective agonist
Mech: Agonist: α1, (α2), β1, β2
Thera: Anaphylactic shock; combined with local anesthetics; glaucoma
Important SE’s: Palpitation; arrhythmias; headache

21
Q

Amphetamine

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A

Class: Indirect acting
Mech: Increases release of NE
Thera: ADHD, narcolepsy, recreation
Important SE’s: Hypertension, insomnia, anxiety, arrhythmias

22
Q

Isoproterenol (Isuprel)

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A

Class: Non-selective β agonist
Mech: Agonist: β1, β2
Thera: shock; heart block
Important SE’s: Palpitation; tachyarrhythmia; headache

23
Q

Dobutamine

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A

Class: β1-selective β agonist
Mech: Agonist: β1
Thera: Cardiac decompensation; shock; heart block
Important SE’s: Tachyarrythmias; hypertension

24
Q

Albuterol (Proventil)

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A

Class: β2-selective β agonist
Mech: Agonist: β2
Thera: Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD
Important SE’s: Can mask progressively severe inflammation
Other SE’s: Tachycardia, muscle tremor
Misc: 10-15 minutes to take action, 6-12 hours (max) of duration; nebulizer delivers more, but greater side effects; oral is least effective (requires more dose –> side effects); can be used night symptoms, but not ideal

25
Terbutaline (Brethine)
Class: β2-selective β agonist Mech: Agonist: β2 Thera: Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD; early labor Important SE: Can mask progressively severe inflammation Other SE's: Tachycardia, muscle tremor Misc: 10-15 minutes to take action, 6-12 hours (max) of duration; nebulizer delivers more, but greater side effects; oral is least effective (requires more dose --> side effects); can be used night symptoms, but not ideal
26
Phenylephrine (Neo-Synephrine)
Class: α1-selective α agonist Mech: Agonist: α1 Thera: Nasal congestion; postural Hypotension Important SE's: Hypertension; reflex bradycardia
27
Clonidine (Catapres)
Class: α2-selective α agonist Mech: Agonist: CNS α2 Thera: Hypertension; shock; withdrawal from drug dependence Important SE's: Sedation
28
α-methyldopa (Aldomet)
``` Class: α2-selective α agonist Mech: Metabolite (a-methylnorepinephrine) activates CNS a2 receptors Thera: Hypertension Important SE's: Sedation Misc: Prodrug; crosses BBB ```
29
Fenoldopam (Corlopam)
Class: Selective dopamine agonist Mech: Agonist: D1 only Thera: Increase blood flow at renal, mesenteric, and cerebral arteries Misc: ~10 minute half-life
30
Dopamine
Class: Mixed acting (direct/indirect) Mech: Agonist: D1, α1, β1 Thera: Shock, renal failure, hypotension Important SE's: Vasoconstriction (@ high doses) Misc: "Low dose = Direct @ D1 Receptors Medium dose = Direct @ Beta 1, some Indirect High dose = Direct @ Alpha 1, some Indirect"
31
Phentolamine (Regitine)
Class: Non-selective α-antagonist Mech: Antagonist: α1, α2 Thera: Pheochromocytoma, Raynaud's, frostbite Important SE's: Postural hypotension; inhibit ejaculation
32
Phenoxybenzamine (Dibenzyline)
Class: Non-selective α-antagonist Mech: Antagonist: α1, α2; non-competitive blocker (covalent bond to receptor) Thera: Pheochromocytoma, Raynaud's, frostbite Important SE's: Postural hypotension; inhibit ejaculation
33
Prazosin (Minipress)
Class: α1-selective antagonist Mech: Antagonist: α1 Thera: Primary HTN, BPH Important SE's: Postural hypotension (usually 1st dose)
34
Terazosin (Hytrin)
Class: α1-selective antagonist Mech: Antagonist: α1 Thera: Primary HTN, BPH Important SE's: Postural hypotension (usually 1st dose)
35
Propranolol (Inderal)
Class: Non-selective β-antagonist (1st generation) Mech: Antagonist: β1, β2 Thera: Angina, Hypertension, Arrythmias Important SE's: Bradycardia, Bronchoconstriction, Sexual Dysfunction Misc: Workhorse by which all the rest are judged
36
Timolol (Betimol)
Class: Non-selective β-antagonist (1st generation) Mech: Antagonist: β1, β2 Thera: Glaucoma Important SE's: Bradycardia, Bronchoconstriction, Sexual Dysfunction
37
Metoprolol (Lopressor)
Class: β1-selective antagonist (2nd generation) Mech: Antagonist: β1 Thera: HTN, Angina, Arrythmias, CHF Important SE's: Bradycardia, Sexual Dysfunction
38
Atenolol (Tenormin)
Class: β1-selective antagonist (2nd generation) Mech: Antagonist: β1 Thera: HTN, Angina, Arrythmias, CHF Important SE's: Bradycardia, Sexual Dysfunction
39
Bisoprolol (Zebeta)
Class: β1-selective antagonist (2nd generation) Mech: Antagonist: β1 Thera: HTN, Angina, Arrythmias, CHF Important SE's: Bradycardia, Sexual Dysfunction
40
Carvedilol (Coreg)
Class: Non-selective β-antagonist (3rd generation "A") mech: Antagonist: β1, β2 Thera: CHF, HTN Important SE's: Bradycardia, Fatigue
41
Labetalol (Trandate)
Class: Non-selective β-antagonist (3rd generation "A") Mech: Antagonist: β1, β2 Thera: CHF, HTN Important SE's: Bradycardia, Fatigue
42
Betaxolol (Kerlone)
Class: β1-selective antagonist (3rd generation "B") Mech: Antagonist: β1 Thera; CHF, HTN Important SE's: Bradycardia
43
Tyramine
Class: Indirect acting agonist Mech: Increases cytoplasmic NE release Misc: Tyramine is involved with an exchange transporter: tyramine goes in, NE comes out
44
Cocaine
Mech: Prevents NE reuptake Thera: Local anesthetic, vasoconstrictor Important SE's: Insomnia, anxiety, arrhythmias
45
Guanethidine (Ismelin)
Class: Nerve ending blocker Mech: False neurotransmitter (vesicles become full of guanethidine rather than NE) Thera: Antihypertensive Important SE's: Many and serious Misc: Don't really use this in US; doesn't cross BBB
46
Reserpine
Class: Nerve ending blocker Mech: Release of empty vesicles (NE is not taken into vesicles b/c it binds uptake transporter and stops it) Thera: Older antihypertensive Important SE's: Many and serious (depression and suicide are major ones) Misc: Cheap! (used abroad, not here)
47
α-me-tyrosine (Metirosine)
``` Class: Nerve ending blocker Mech: Inhibit tyrosine hydroxylase (decreases NE synthesis) Thera: Pheochromocytoma Important SE's: Many and serious Misc: Still used for this ```
48
Ephedrine (Pretz-D)
Class: Mixed, direct (β2)/indirect agonist Thera: Nasal decongestion, anorexic

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