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Pharmacology (Topics A) > A12. Beta-receptor antagonists > Flashcards

A12. Beta-receptor antagonists Flashcards

1
Q

What do beta blockers do?

A
  1. Beta blocking decreases cardiac output (decreases inotropy, chronotropy, dromotropy)
  2. Beta 1 also is in kidney for renin secretion, so inhibits RAAS → BP ↓ , decreased remodeling of the heart
  3. Non-selective β blockers: propranolol, nadolol, timolol, sotalol, pindolol
  4. selective β1 blockers: metoprolol, atenolol, esmolol, bisoprolol, betaxolol, acebutolol, nebivolol (+ NO effect)
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2
Q

What are the Cardiovascular indications for Beta blockers?

A
  1. Hypertension: main indication. better in younger people (more likely to have hypertension as a result of increased sympathetic tone). Cardiovascular effects of β blockers: decrease CO, BP, and renin secretion
  2. Angina, IHD, post-MI: decrease the O2 demand. longer diastolic time → longer time for coronary filling. (remember that they don’t dilate the coronaries, just allows better filling time)
  3. Arrhythmia: part of class II anti-arrhythmics. Decreasing sympathetic tone, AV conduction, etc. Help supraventricular tachyarrhythmias.
  4. Chronic Heart Failure (CHF): maybe not intuitive to slow down the heart when it’s failing, but have been shown to prolong lifetime. decrease remodeling of the heart. Only given until signs of CHF (edema), which indicates the dose is too. Strong and acute heart failure has started.
  5. Obstructive hypertrophic cardiomyopathy, low EF.
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3
Q

List the nNon cardivascular indications?

A

o hyperthyroidism: propranolol
o glaucoma: timolol, betaxolol (must not have Na channel blocking effect) o migraine: propranolol, metoprolol
o anxiety: esp. pindolol, propranolol
o essential tremor: propranolol, metoprolol
o possibly local anesthesia: many inhibit Na channels

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4
Q

What are the general side effects of Beta blockers?

A
  1. Bradycardia, AV block
  2. Hypotension
  3. from β2 effects: Bronchoconstriction. Even with beta 1 selective drugs, if the dose is high then beta 2 blocked effects will still occur.
  4. Lethargy, depression
  5. Worse lipid profile
  6. Maybe impotence
  7. Peripheral vasoconstriction: cold hands, cold legs. worsening of peripheral vascular disease.
  8. In diabetic patient, there may be more tendency to develop hypoglycemia. The symptoms of hypoglycemia are not visible bc many of those are related to sympathetic response (pale skin, anxiety..)
  9. Sleep disturbances (nightmares) in the CNS-penetrating β blockers.
  10. Uterine contractions during pregnancy
  11. If a patient suddenly discontinues β blockers that they’ve been taking for a long time, they will get tachycardias/tachyarrhythmias. Have to discontinue slowly!!
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5
Q

What are the Contraindications of Beta Blockers?

A
  1. Severe bradycardia, second degree AV block
  2. Severe hypotension
  3. Vasospastic disorders: Prinzmetal angina, Raynaud
  4. Psoriasis (worsens)
  5. Unstable diabetes
  6. During pregnancy (might worsen placental perfusion)
  7. Severe bronchial asthma, COPD.. be very careful with them here. β1 blockers must be used cautiously.
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6
Q

List the Non-selective beta blockers.

A
  1. Propanolol
  2. Nadolol
  3. Timolol
  4. Sotalol
  5. Pindolol
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7
Q

What is the MOA of Non- selective beta blockers?

A

Non-selective beta blockers work on both β1 and β2, and β2 blockade → some bronchoconstriction. May be a problem in asthmatics or COPD patients.

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8
Q

What are the indications for Propranolol?

A
  1. Propranolol is the most important and strongest β antagonist.
  2. Also inhibits T4 → T3 transformation (indicated in hyperthyroidism) so it’s useful to lower the risk of tachycardia from thyrotoxicosis.
  3. Local anesthetic effect, inhibits Na channels.
  4. Penetrates CNS: used for migraine prophylaxis, some anti-anxiety effects, essential tremor.
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9
Q

What are the indications for Nadolol?

A

Nadolol is one of the longest acting β blockers, duration of 24-hours. It doesn’t enter CNS, hydrophilic. It is used for Hypertension.

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10
Q

What are the indications for Timolol?

A

Timolol is not Na channel and has local anesthetic effect but used topically as eyedrop for glaucoma. Inhibit secretion of aqueous humour.

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11
Q

What are the indications and adverse effects of Sotalol?

A
  1. Sotalol inhibits not Na+ but K+ channels.
  2. Used as a class III antiarrhythmic (PSVT)
  3. All K+ channel blockers can cause long QT, with a risk of Torsades.
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12
Q

What are the indications for Pindolol?

A
  1. Pindolol has ISA effect (intrinsic sympathomimetic activity), meaning it has partial agonist of β receptors. Will antagonize effect of full agonist, that being endogenous epinephrine.
  2. This makes it better for patients that have bradycardia.Won’t worsen the bradycardia, might even improve it.
  3. Also partial agonist on serotonin 1A receptor (good for anxiety, especially situational anxiety).
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13
Q

List the β1 selective aka cardiac selective beta blockers.

A
  1. Metoprolol
  2. Atenolol
  3. Esmolol
  4. Bisoprolol
  5. Betaxolol
  6. Acebutolol
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14
Q

What are the indications for Metoprolol?

A
  1. Metoprolol is used for Hypertension.
  2. Also indicated for prophylaxis of migraine (penetrates CNS).
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15
Q

What are the indications for Atenolol?

A
  1. Atenolol is used for hypertension.
  2. Doesn’t penetrate CNS, maybe won’t have nightmares?
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16
Q

What are the indications for Esmolol?

A
  1. Esmolol has a very short duration of action (10 minutes).
  2. Not used for chronic treatment.
  3. Only emergencies, maybe for PSVT
17
Q

What is the DOA of action of Bisoprolol?

A
  1. Bisoprolol has a long duration of action (18-22 hours).
  2. Can give 1 x day.
18
Q

What are the indications for Betaxolol?

A
  1. Betaxolol is used for glaucoma as eyedrop too.
  2. But also can be used for cardiovascular reasons.
19
Q

What is the MOA and indication for Acebutolol?

A

Acebutolol is a partial agonist of β1 receptor (ISA), similar to pindolol but it’s cardiac-selective.

20
Q

List the Beta 1 selective (+ NO release) Beta Blockers.

A
  1. Nebivolol
21
Q

What are the indications for Nebivolol?

A
  1. Nebivolol has a direct vasodilator effect + systemic effect.
  2. (Racemic mixture: one isomer is β1 blocker, other isomer induces NO release)
  3. Used for hypertension mainly
22
Q

Give examples of beta blockers with shortest to longest DOA?

A
  1. Very short: esmolol
  2. Very long (> 10 hours): Nadolol, Betaxolol, Bisoprolol, Nebivolol
23
Q

What are the differences in lipid solubilty of the beta blockers?

A
  1. High lipid solubility: Propranolol, Nebivolol, Metoprolol. These drugs have more CNS effects, so are better for migraine or essential tremor, but also have CNS side effects (e.g. nightmares)
  2. Low lipid solubility: Atenolol, Sotalol, Acebutolol. These drugs will be useful if patients complain of nightmares from taking propranolol. May be more of a problem if patients have kidney disease (difficulty excreting hydrophilic drugs).
24
Q

List the Alpha and Beta blockers.

A
  1. Urapidil
  2. Carvedilol
  3. Labetalol

Pharmacology (Topics A) (39 decks)

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