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Pharm Block 1 > Adrenergic II > Flashcards

Adrenergic II Flashcards

1
Q

What are sympatholytic drugs?

A

Sympatholytic drugs are adrenergic receptor antagonists and they act by blocking the postganglionic function of the sympathetic nervous system.

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2
Q

How do sympatholytic drugs block sympathetic action?

A

3 mechanisms to block:

1) Decrease sympathetic outflow from the brain
2) Suppress nerve terminal NE:
a) Inhibit synthesis
b) Deplete NE granules
c) Suppress the release of NE
3) Block postsynaptic receptors

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3
Q

Describe the qualities of irreversible receptor antagonists.

A

Irreversible antagonists:

1) Do not dissociate => phenoxybenzamine
2) Their antagonism outlasts the presence of the compound
3) The block is insurmountable/not overcome by NE

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4
Q

Describe the characteristics of reversible receptor antagonists.

A

Reversible antagonists:

1) Dissociate from the receptor and produce an equilibrium blockade
2) The block disappears as free drug is metabolized
* Examples => phentolamine and prazosin

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5
Q

What is the function of α-adrenergic receptor blockers?

A

Vasodilation and lowering BP

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6
Q

What type of α-adrenergic receptor blocker is used clinically?

A

α1-AR selective blockers are used clinically.

They are used for vasodilation and reduction in arterial pressure => clinically used for HTN and BPH

- There is no reflex tachycardia in these drugs are decrease in cardiac function    - Prototype drug: Prazosin
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7
Q

What are the uses of nonselective α-adrenergic receptor blockers?

A

Non-selective α-adrenergic receptor blockers:

1) Phentolamine = reversible and rarely used
2) Phenoxybenzamine (Dibenzyline) => irreversible, used in peripheral vasospasm
* Adverse reactions: hypotension and tachycardia

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8
Q

What are the cardiovascular effects of β1 blockers?

A

1) Reduce heart rate
2) Delay AV conduction
3) Decrease rate of depolarization
4) Decrease force of contraction
5) Decrease oxygen consumption
6) Decrease BP
7) Inhibit renin release

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9
Q

What are the cardiovascular effects of β2 blockers?

A

1) Vasoconstriction in arterioles
2) Increased airway resistance
3) Decreased glycogenolysis and gluconeogenesis
4) Inhibit insulin release

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10
Q

What are the properties of β-AR blockers?

A

1) Selectivity => peripheral vascular disease and diabetes
2) Partial agonist activity
3) Action as a local anesthetic
4) Lipid solubility

Pharmacokinetic properties

1) Metabolism in the liver and kidney
2) Elimination half life, bioavailability
3) Well absorbed after oral administration=> peak concentration at 1-3 hours
4) Extensive hepatic metabolism => half lives from 3-10 hours
- Gradually taper doses if discontinuing as receptor up regulation with blockade

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11
Q

What considerations need to be made with β-AR blockers?

A

1) Drug interactions with anti-hypertensives => verapmil, digoxin
2) Caution with airway disease, diabetes and heart failure

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12
Q

What are the primary indications for β-AR blockers?

A

Primary indications for β-AR blockers:

1) Hypertension
2) Arrythmias
3) Ischemic heart disease

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13
Q

What are secondary indications for β-AR blockers?

A

Secondary indications for β-AR blockers?

1) Hyperthyroidism
2) Glaucoma
3) Migraine
4) Anxiety

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14
Q

What is Prazosin (Minipress)?

A

Prazosin is a sympatholytic drug used to treat high blood pressure, anxiety, PTSD, and panic disorder.

Costs range from $4-$2 per month

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15
Q

What is the drug class for Prazosin?

A

Pharmacologic class => selective alpha-1 adrenoceptor blocker
Therapeutic class => antihypertensive, treatment of BPH (benign prostatic hyperplasia), treatment of Raynaud’s syndrome, treatment for kidney stones

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16
Q

Describe the pharmacodynamics of Prazosin.

A

Blocks alpha-1 receptors on arterioles and veins, thereby inhibiting NE-mediated vasoconstriction and venoconstriction

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17
Q

Describe the pharmacokinetics of Prazosin.

A

Available po (Per Os => by mouth) or transdermal

  • Variable oral bioavailability (~60%)
  • Onset 2 h => duration 12-24 h
  • Extensively metabolized in liver
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18
Q

What toxicity is associated with Prazosin?

A

Prazosin toxicity:

Excessive hypotension with passing out => especially orthostatic and patients on diuretics

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19
Q

What are the pertinent Prazosin interactions?

A

Prazosin interactions: additive effects with most other antihypertensives, especially diuretics

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20
Q

What special considerations should be made with Prazosin?

A

Considerations:

  • Start gradually and at bedtime => to avoid first-time passing out
  • Male patients with BPH?
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21
Q

What dose/route should Prazosin be given?

A

Prazosin route/dose:

-As mono therapy => begin with1 mg tid, advance to 20 mg per day divided tid (ter in die => 3 times/day)

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22
Q

What should be monitored in patients on Prazosin?

A

BP, weight, edema

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23
Q

What is Tamsulosin/Flomax?

A

Tamsulosin is an alpha blocker, which works by relaxing bladder neck muscles and muscle fibers in the prostate itself to make it easier to urinate.

Costs range from $5-$70 per month

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24
Q

What drug class is Tamsulosin?

A

Pharmacologic class => selective alpha-1 adrenoceptor blocker
Therapeutic class => treatment of obstructive symptoms of BPH

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25
Q

Describe the pharmacodynamics of Tamsulosin.

A

Pharmacodynamics:

  • Selectively blocks alpha-1 receptors, but preferentially in the prostate
    • This leads to relaxation of smooth muscles in the bladder neck and prostate, improving urine flow, and reducing obstructive symptoms of BPH venoconstriction
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26
Q

Describe the pharmacokinetics of Tamsulosin.

A

Pharmacokinetics:

  • Completely absorbed after oral ingestion
  • > 90% metabolized by CYP 450 enzymes
  • Half-life about 6 hours, but duration of action up to 15 hours due to slow absorption
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27
Q

What toxicity is associated with Tamsulosin?

A

Toxicity:

  • Excessive hypotension with syncope => especially orthostatic and especially in patients on diuretics
  • Allergic reactions
  • Decreased libido
28
Q

What are pertinent Tamsulosin interactions?

A

Interactions:

-Additive effects with most other antihypertensives, especially diuretics

29
Q

What special considerations should be made for patients on Tamsulosin?

A

Considerations:

  • Rule out carcinoma of prostate before beginning treatment
  • Do not crush or chew tablets, as that will speed up absorption
  • Can also be used to treat spasm of ureter in patients with kidney stones
30
Q

What is the appropriate dose/route for Tamsulosin?

A

Dose/route:

- For symptoms of BPH, 0.4 mg po (by mouth) qd (1/day) or bid (2/day); similar doses for renal colic

31
Q

What should be monitored in patients on Tamsulosin?

A

BP

32
Q

What is Phentolamine/Regitine?

A

Phentolamine is a reversible nonselective alpha-adrenergic antagonist used primarily for the control of hypertensive emergencies, most notably due to pheochromocytoma.

33
Q

What drug class is Phentolamine?

A

Pharmacologic class => non-selective, competitive alpha-adrenergic receptor blocker
Therapeutic class => antihypertensive drug for patients with pheochromocytoma

34
Q

Describe the pharmacodynamics of Phentolamine.

A

Pharmacodynamics:
- Blocks alpha-1 and alpha-2 adrenergic receptors at presynaptic and postsynaptic alpha receptors, decreasing preload and afterload

35
Q

Describe the pharmacokinetics of Phentolamine.

A

Pharmacokinetics:

  • Only comes in IV formulation, so F=100%
  • Plasma half-life about 20 min after IV dose
36
Q

What toxicity is associated with Phentolamine?

A

Toxicity:

  • Excessive hypotension with syncope => especially orthostatic and especially in patients on diuretics
  • Allergic reactions
  • Decreased libido
37
Q

What are pertinent Phentolamine interactions?

A

Interactions:

- Additive effects with most other antihypertensives, especially diuretics

38
Q

What special considerations should be made for patients on Phentolamine?

A

Considerations:

  • Rule out carcinoma of prostate before beginning treatment
  • Do not crush or chew tablets, as that will speed up absorption
  • Can also be used to treat spasm of ureter in patients with kidney stones
39
Q

What are the indications/route/dose for Phentolamine?

A

Indications:

  • Aid in Dx of pheo
  • Treatment of intra-op HTN during pheo removal surgery;
  • Prevention of dermal sloughing after extravasation of NE infusion
  • Hypertensive crisis from sympathomimetic amines (discuss tyramine-MAO interaction)

Dose/Route:
- Dose 5 mg IV, then titrate, repeat as needed

40
Q

What should be monitored in patients on Phentolamine?

A

BP

41
Q

What is Atenolol/Tenormin/Metoprolol/Toprol?

A

Atenolol is a Beta-1 receptor antagonist used in cardiovascular disease, primarily in the treatment of hypertension.

Class runs $4/$52 for atenolol to $100 for Toprol XL

42
Q

What drug class is atenolol?

A

Pharmacologic class => specific β1-adrenoceptor blocker Therapeutic class => antihypertensive, antiarrhythmic, primary and secondary prevention of MI, anti-anginal

43
Q

Describe the pharmacodynamics of atenolol.

A

Pharmacodynamics:

  • Binds directly to β1-receptors, with a preference for beta-1 over beta-2
    • Leading to lower blood pressure via several potential mechanisms (less cardiac output, less activation of the RAA system)
    • Recent evidence suggests less effective in preventing strokes than other drugs (reason why used less as initial mono-therapy)
44
Q

Describe the pharmacokinetics of atenolol.

A

Pharmacokinetics:

  • Available po (by mouth) or iv
  • Variable oral F
  • Onset 1-2 hours h, duration 12-24 h
  • Can be given once per day
  • Renally excreted (longer half-life)
    • Metoprolol has hepatic metabolism (and shorter half-life)
45
Q

What toxicity is associated with atenolol?

A

Toxicity:

  • Excessive hypotension
  • Bradycardia
  • Heart block can worsen severe CHF (but indicated for mild to moderate CHF)
  • Worsen bronchospasm in severe asthmatics
46
Q

What interactions should be considered for patients on atenolol?

A

Interactions:

  • Additive effects with most other antihypertensives
  • Additive AV block with CEBs
47
Q

What special considerations should be taken for patients on atenolol?

A

Considerations:

  • May be especially useful in HTN patients with exertional angina, MI, atrial fibrillation
  • Watch out for abrupt withdrawal
  • May no longer be “first line” drug for essential HTN unless other indications exist (recent data)
  • Metoprolol (needs to be taken several times per day) has more data for use in patients s/p MI
48
Q

What is the dose/route/indication for atenolol?

A

Indication:
- For treatment of hypertension
Dose/route:
- 25-100 mg per day, in one or two doses

49
Q

What should be monitored in patients on atenolol?

A

BP, HR, exercise tolerance

50
Q

What is Propranolol/Inderal?

A

Propranolol is a sympatholytic non-selective beta blocker.

  • Sympatholytics are used to treat hypertension, anxiety and panic.
  • It is on the World Health Organization’s List of Essential Medicines, a list of the most important medication needed in a basic health system.
  • $4 up to $108 for Inderal
51
Q

What is the drug class for Propranolol?

A

Pharmacologic class => non-specific β-adrenoceptor blocker

Therapeutic class => antihypertensive, antiarrhythmic, primary and secondary prevention of MI, anti-anginal

52
Q

Describe the pharmacodynamics of propranolol.

A

Pharmacodynamics:

  • Binds directly to β1-receptors and β2 receptors, leading to lower blood pressure via several potential mechanisms (less cardiac output, less activation of the RAA system)
  • Recent evidence suggests less effective in preventing strokes than other drugs
53
Q

Describe the pharmacokinetics of propranolol.

A

Pharmacokinetics:

  • Available po or iv; variable oral F
  • Onset 1-2 hours h, duration 12-24 h
  • Can be given once per day
  • Renally excreted (longer half-life)
    • Metoprolol has hepatic metabolism (and shorter half-life)
54
Q

What toxicity is associated with propranolol?

A

Toxicity:

  • Excessive hypotension
  • Bradycardia
  • Heart block can worsen severe CHF (but indicated for mild to moderate CHF)
  • Worsen bronchospasm in severe asthmatics
55
Q

What interactions should be considered for patients on propranolol?

A

Interactions:

  • Additive effects with most other antihypertensives
  • Additive AV block with CEB’s
56
Q

What special considerations should be considered for patients on propranolol?

A

Considerations:

- May be especially useful in HTN patients with exertional angina, MI, atrial fibrillation    - Watch out for abrupt withdrawal    - May no longer be “first line” drug for essential HTN unless other indications exist (recent data)
  - Metoprolol (needs to be taken several times per day) has more data for use in patients s/p MI
57
Q

What are the indications/dose/route for propranolol?

A

Indications:
- For treatment of hypertension
Dose/route:
- 25-100 mg per day, in one or two doses

58
Q

What should be monitored in patients on propranolol?

A

BP, HR, exercise tolerance

59
Q

What is Labetalol/Trandate/Carvedilol/Coreg?

A

Labetalol is a mixed alpha/beta adrenergic antagonist, which is used to treat high blood pressure especially in pregnancy-induced hypertension, pheochromocytoma, and hypertensive crisis

  • class cost $4 (carvedilol generic) to $26 per month
60
Q

What is the drug class of labetalol?

A

Pharmacologic class => mixed alpha- and beta-receptor blocker
Therapeutic class=> antihypertensive, treatment of CHF

61
Q

Describe the pharmacodynamics of labetalol.

A

Pharmacodynamics:

  • Reduces BP by blocking access of NE to beta-receptors and alpha-1 receptors, thereby lowering BP by several different mechanisms
  • Patients differ in degree of beta-blockade vs alpha-blockade
62
Q

Describe the pharmacokinetics of labetalol.

A

Pharmacokinetics:

  • Excellent absorption but high first-pass effect, leading to F~25%
  • Onset 1-2 hours after po, 2-5 minutes when given iv
  • Extensively metabolized in liver by IID6
63
Q

What toxicity is associated with labetalol?

A

Toxicity:

  • Avoid in patient with bradycardia, heartblock, CHF, asthma, shock
  • Use with caution in patients with cardiomyopathy, pheochromocytoma: Pregnancy Class D
64
Q

What interactions should be considered in patients on labetalol?

A

Interactions:

- Additive effects with most other antihypertensives

65
Q

What special considerations should be made for patients on labetalol?

A

Special considerations:

  • Use reduced doses in patients with impaired liver function
  • Dizziness is most troubling early side effect
  • Most often used for hypertensive crises (as with nitroprusside)
66
Q

What are the indications/route/dose for labetalol?

A

Route/Dose:

  • Most commonly given iv with initial small boluses of 20 mg, followed by continuous infusion at 2 mg/min
  • Not usually given po for chronic treatment
    • 80 mg thrice daily, or 240 mg SR once daily
67
Q

What should be monitored in patients on labetalol?

A

BP, HR

Pharm Block 1 (16 decks)

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