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RCS > Andrenergic Agonist and Antagonist > Flashcards

Andrenergic Agonist and Antagonist Flashcards

1
Q

Isoproterenol

A

M: non-selective beta agonist

CA: emergency arrythmias and bronchospasm

AE: HTN, palpitations, tremor

TCo:

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2
Q

Dobutamine

A

M: B1 agonist with potent inotrope but mild chronotropic effects

CA: management of acute heart failure and cardiogenic shock; dobutamine stress echocardiogram

AE:

TCo: short half life due to COMT metabolism

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3
Q

Albuterol

A

M: B2 agonist causing bronchodilation

CA: asthma and COPD

AE: tachycardia, tremors, restlessness, apprehencion, anxiety

TCo: short acting (15min)

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4
Q

Salmeterol & Formoterol

A

M: B2 agonist to prevent bronchoconstriction

CA: asthma and COPD

AE: tachycardia and tremors

TCo: long acting 12-24 hours

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5
Q

Phenylephrine

A

M: selective A1 agonist causing vasoconstriction

CA: nasal decongestant, mydriatic, increase BP in hypotension from septic shock, anesthesia, or episodes of supraventricular tachycardia

AE: bradycardia when given parenterally

TCo: HTN

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6
Q

What are the A2-selective adrenergic agonist?

A

Clonidine, Methyldopa, Brimonidine

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7
Q

Clonidine

A

M: partial A2 agonist

CA: centrally acting antihypertensive (reduces sympathetic outflow)

AE: lethargy, sedation, xerostomia

TCo:

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8
Q

Methyldopa

A

M: converted to alpha-methylnorepinephrine which activates central A2-receptors

CA: DOC for HTN during pregnancy

AE: sedation, impaired mental concentration, xerostomia

TCo:

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9
Q

Brimonidine

A

M: highly selective A2 agonist

CA: lower intraocular pressue in glaucoma (reduces aqueous humor production and increased outflow)

AE:

TCo:

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10
Q

What are the indirect-acting adrenergic agonists that act as releasing agents?

A

Amphetamine, Methylphenydate, Tyramine

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11
Q

Amphetamine

A

M: cause relase of norepinephrine from presynaptic terminals

CA: ADHD, and narcolepsy

AE:

TCo: centrally stimulatory action, can increase blood pressure by A-agonist action on vasculature as well as B-stimulatory effects on heart

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12
Q

Methylphenydate

A

M: causes release of norepinephrine from presynaptic terminals

CA: ADHD

AE:

TCo: structural analogue of amphetamine

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13
Q

Tyramine

A

M: causes relase of norepinephrine from presynaptic terminals

CA:

AE: normally oxidized by MAO but if pt is taking MAO inhibitors it can precipitate as serious vasopressor episodes causing headache

TCo: found in fermented foods (cheese, wine)

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14
Q

What are the uptake inhibitors?

A

Cocaine, Atomoxetine, Modafinil

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15
Q

Cocaine

A

M: blocks monoamine reuptake causing monoamines to accumulate in synaptic space

CA: potentiation and prolongation of their central and peripheral actions

AE:

TCo:

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16
Q

Atomoxetine

A

M: selective inhibitor of the norepinephrine reuptake transporter

CA: ADHD

AE:

TCo:

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17
Q

Modafinil

A

M: not fully known but inhibits norepinephrine and dopamine transporters

CA: treats narcolepsy

AE:

TCo: increase synaptic concentrations of norepinephrine, dopamine, serotonin, and glutamate; decrease in GABA levels

18
Q

What are the mixed-acting adrenergic agonists?

A

Ephedrine and Pseudoephedrine

19
Q

Ephedrine

A

M: activate andrenergic receptors to induce relase or norepinephrine

CA: myasthenia gravis and used as a pressor (during spinal anesthesia)

AE:

TCo:

20
Q

Pseudoephedrine

A

M: activate adrenergic receptors to induce release of norepinephrine

CA: decongestant

AE:

TCo: one of four enantiomers

21
Q

What are the non-selective alpha-andrenergic blockers?

A

Phenoxybenzamine and Phentolamine

22
Q

Phenoxybenzamine

A

M: irreversible non-selctive alpha-adrenergic blocker

CA: DOC for pheochromocytoma prior to surgical removal of tumor and for chronic management of inoperable tumors

AE: postural hypotension, nasal stuffiness, nausea, vomiting, inhibit ejaculation

TCo: contraindicated in pts with decrease coronary perfusion because of reflex tachycardia

23
Q

Phentolamine

A

M: reversibly blocks alpha receptors

CA: HTN crisis due to stimulant drug overdose, control HTN during surgery of Pheochromocytoma, diagnoses of pheochromocytoma (phentolamine blocking test), pevent dermal necrosis

AE: postural hypotension, arrythmias, angina

TCo: contraindicated in pts with decrease coronary perfusion due to reflex tachycardia

24
Q

Explain epinephrine reversal?

A
  • When alpha-andrenergic blockers are present there will be no effect on the alpha receptors by epinephrine so vasodilation by B2 receptors will be predominant leading to decrease in blood pressure (reflex tachycardia)
25
Q

What are the alpha-1 selective andrenergic blockers?

A
  • Prozosin
  • Terazosin
  • Doxazosin
  • Tamsulosin
26
Q

Prazosin

A

M: alpha-1 selective blocker

CA: DOC for BPH; HTN

AE: first does must be 1/3 or 1/4 normal because of exaggerated hypotensive response can cause syncope

TCo: Prazosin is the prototype and has short half-life

27
Q

Terazosin and Doxazosin

A

M: alpha-1 selective blocker

CA: DOC for benign prostatic hypertropy (BPH), HTN

AE: first does must be 1/3 or 1/4 normal because of exaggerated hypotensive response can cause syncope

TCo: prazosin analogs with longer half life

28
Q

Tamulosin

A

M: alpha-1A selective blocker (alpha-1A receptor predominant in GU smooth muscle)

CA: BPH

AE: less likely to cause orthostatic hypotension

TCo: little effect on blood pressure

29
Q

What are the nonselective beta-blockers and name there cardiovascular, respiratory, and metabolic effects?

A

Propranolol, Nadolol, Timolol

CVS: slow heart rate and decrease myocardial contractility

Respiratory: can precipitate a respiratory crisis in pts with COPD or asthma

Metabolic: decrease glycogenolysis and decrease glucagon secretion

30
Q

Atenolol and Metoprolol

A

M: beta-1 selective adrenergic antagonist

CA: tx HTN in pts with impaired pulmonary function and diabetics who are receiving insulin/oral hypoglycemic agents

AE:

TCo:

31
Q

Esmolol

A

M: B1 selective andrenergic antagonist

CA: rapid control of ventricular rate in pts with atrial fibrillation or atrial flutter

AE:

TCo: ultra-short acting, half life 10 minutes, IV

32
Q

Labetalol

A

M: alpha-1 and beta blockers

CA: HTN

AE:

TCo: more potent as a beta antagonist

33
Q

Carvedilol

A

M: alpha-1 and beta-blockers

CA: HTN and CHF

AE:

TCo: also has antioxidant properties

34
Q

Pindolol

A

M: partial beta-agonist

CA:

AE:

TCo: preferred in individuals with diminished cardiac reserve or a propensity to bradycardia

35
Q

What are the uses of beta blockers?

A
  • HTN: lower blood pressure by decreasing CO
  • Glaucoma: diminishig intraocular pressure (timolol)
  • Migraine: prophylaxis
  • Hyperthyroidism: blunt sympathetic stimulation
  • Angina Pectoris: decrease O2 requirement of heart
  • Atrial Fibrillation: contral ventricular rate
  • MI: protective effect on myocardium
  • Performance Anxiety: stage fright
  • Essential Tremor: most commonly used drug
36
Q

What are the adverse effects of beta blockers?

A
  • Hypoglycemia: blockade of beta-2 receptors in liver
  • Lipid metabolism: inhibit relase of free FA from adipose tissue, both non-selective and B1 blockers increase TG and reduce HDL, lipids unaffected by labetalol and pindolol
  • CNS: sedation, dizziness, lethargy, fatigue
37
Q

What are the warnings and precautions of beta blockers?

A
  • should not be withdrawn abruptly (especially pts with CAD) because of gradually tapered to avoid acute tachycardia, HTN, and/or ischemia due to up-regulation of beta receptors
38
Q

alpha-Methyltyrosine (Metyrosine)

A

M: competitive inhibitor of tyrosine hydroxylase

CA: management of malignant Pheochromocytoma and used preop during resection of Pheochromocytoma

AE:

TCo:

39
Q

Reserpine

A

M: irreversibly blocks VMAT so vesicles cannot store norepinephrine and dopamine (depletion of norepinephrine because of MAO in cytoplasm)

CA: HTN (used in the past)

AE:

TCo: gradual decrease in BP and slowing of cardiac rate

40
Q

Tetrabenazine

A

M: reversible inhibitor of VMAT causing presynaptic depletion of catecholamines

CA: chorea associated with Huntington’s Disease

RCS (8 decks)

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