Cardiovascular Medicine Book

Hypotension

Hypertension

Coronary Artery Disease

Electrocardiogram

Hyperlipidemia

Pericardial Disorders

Congestive Heart Failure

Examination

Inotrope

Obstetrics Chapter related topics

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Beta Blocker

Aka: Beta Blocker, Beta-Blocker, Beta Adrenergic Antagonist, Beta Adrenoceptor Blocking Drug, Atenolol, Timolol, Nadolol
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  1. See Also
    1. Carvedilol
    2. Esmolol
    3. Metoprolol
    4. Propranolol
    5. Beta Blocker Overdose
    6. Perioperative Beta Blocker
  2. History: Sir James Black and Propranolol
    1. Sir James Black won 1988 Nobel Prize for Propranolol
    2. Synthesized Propranolol first in the 1960's
    3. Revolutionized cardiovascular medicine
  3. Indications
    1. Hypertension
    2. Atrial Fibrillation Rate Control
    3. Coronary Artery Disease without prior Myocardial Infarction
      1. Consider to reduce Anginal symptoms and improve Exercise tolerance
    4. Myocardial Infarction without Congestive Heart Failure
      1. Continue for at least 2-3 years after Myocardial Infarction
    5. Stable Congestive Heart Failure (Carvedilol, Metoprolol, Bisoprolol)
      1. Continue Beta Blocker indefinately
    6. Arrhythmia refractory to other modality
      1. Recurrent Ventricular Tachycardia
      2. Recurrent Ventricular Fibrillation
    7. Migraine Prophylaxis
  4. Contraindications
    1. Reactive Airway Disease (Asthma, COPD)
      1. Cardioselective Beta Blockers are not contraindicated
      2. See Bronchospasm under adverse effects below
    2. Acute Congestive Heart Failure exascerbation
    3. Concurrent Calcium Channel Blocker use
  5. Precautions
    1. Abrupt discontinuation is associated with exacerbation of Angina and risk of MI (FDA black box warning)
    2. Taper over one to two weeks
  6. Mechanism
    1. Beta Adrenergic Receptor Antagonist
      1. Blocks Beta Adrenergic Receptors
      2. Inhibits effects of circulating Catecholamines
    2. General Cardiac Effects
      1. Negative Inotrope
        1. Reduces Myocardial Contractility
      2. Negative Chronotrope
        1. Reduces Heart Rate
      3. Reduces Blood Pressure
      4. Reduces Myocardial Oxygen Demand
    3. Antiarrhythmic effects
      1. Seen with non-selective Beta Blockers (Propranolol)
      2. Controls Catecholamine stimulated arrhythmias
        1. Recurrent Ventricular Tachycardia
        2. Recurrent Ventricular Fibrillation
      3. Controls Myocardial Ischemia related arrhythmias
      4. Reduces AV Nodal Conduction
        1. Slows ventricular response
          1. Atrial Fibrillation
          2. Atrial Flutter
          3. Paroxysmal Supraventricular Tachycardia
        2. Quinidine-like effect on action potential
          1. Seen with Propranolol
    4. Myocardial protection
      1. Reduces Myocardial Infarction size
      2. Prevents re-infarction after Thrombolytic
    5. Non-Selective effects (Beta 2 Adrenergic Receptor)
      1. Results in bronchoconstriction
      2. Non-Selective Beta Blockers (e.g. Propranolol)
      3. Selective Beta Blockers lose selectivity at high dose
        1. High dose Metoprolol (over 200 mg/day)
        2. High dose Esmolol (over 300 ug/kg/min)
  7. Adverse Effects
    1. SA and AV nodal blockade
      1. Avoid in over age 75 unless secondary indication
      2. Do not use with Calcium Channel Blockers
    2. Hypotension or Orthostasis
    3. Congestive Heart Failure
      1. Treat with vasodilators and Diuretics with inotropes
    4. Bradycardia
      1. Treat with Atropine, Transcutaneous pacing, Dopamine
    5. Bronchospasm
      1. Treat with Sympathomimetics and Aminophylline
      2. Unlikely to occur in cardioselective Beta Blockers
        1. Study looked at Atenolol, Metoprolol, bisoprolol
        2. First dose may lower FEV1 (responds to Albuterol)
        3. Continuous use does not impair lung function
        4. Salpeter (2002) Ann Intern Med 137:715-25
    6. Major Depression exacerbation
    7. Fatigue
  8. Drug Interactions: Decreased Heart Rate and AV Conduction
    1. Amiodarone
    2. Diltiazem
    3. Verapamil
    4. Propafenone (Rythmol)
    5. Sotalol (Betapace)
  9. Preparations: Cardioselective
    1. Atenolol (Tenormin)
      1. Despite daily dosing, duration of activity is not a a full 24 hours
        1. Consider dividing dosing into twice daily (e.g. 50 mg twice daily)
      2. Not as effective as other Beta Blockers in cardiovascular disease prevention (especially with Hypertension present)
        1. Consider Metoprolol, Bisoprolol, Carvedilol or Nadolol instead
        2. Carlberg (2004) Lancet 364:1684-9
      3. Dosing
        1. Regular: 50 mg PO daily (MAX: 100 mg/day)
        2. IV (Acute MI): 5 mg IV over 5 min, repeat in 10 min
    2. Bisoprolol
      1. Most cardioselective of Beta Blockers
    3. Metoprolol (Lopressor)
    4. Esmolol Hydrochloride (Brevibloc)
    5. Nebivolol (Bystolic)
      1. Third generation Beta Blocker with vasodilatory properties (nitric oxide release)
  10. Preparations: Nonselective
    1. Propranolol (Inderal)
    2. Carvedilol (Coreg)
      1. Third generation Beta Blocker with vasodilatory properties (alpha blocker)
    3. Timolol (Blocadren)
      1. Dose: 10 mg PO bid (MAX 60 mg/day)
    4. Nadolol (Corgard)
      1. Dose: 40 mg PO qd (MAX 320 mg/day)
  11. References
    1. (2012) Presc Lett 19(12): 67-8
Medication Costs
ATENOLOL (on 2/10/2012 at Target.com)
ATENOLOL 25 MG Tablet #30 for $4.00 ($0.13/unit)
ATENOLOL 50 MG Tablet #30 for $4.00 ($0.13/unit)
ATENOLOL 100 MG Tablet #30 for $4.00 ($0.13/unit)
ATENOLOL/CHLORTHAL (on 2/10/2012 at Target.com)
ATENOLOL/CHLORTHAL 50/25 MG Tablet #30 for $4.00 ($0.13/unit)
ATENOLOL/CHLORTHAL 100/25 MG Tablet #30 for $4.00 ($0.13/unit)
TIMOLOL MALEATE (on 2/10/2012 at Target.com)
TIMOLOL MALEATE 0.25% OphthalmicSolution #30 for $4.00 ($0.13/unit)
TIMOLOL MALEATE 0.5% OphthalmicSolution #30 for $4.00 ($0.13/unit)
NADOLOL (on 2/10/2012 at Target.com)
NADOLOL 20 MG Tablet #30 for $4.00 ($0.13/unit)
NADOLOL 40 MG* Tablet #30 for $4.00 ($0.13/unit)
Atenolol-Chlorthalidone (on 2/9/2012 at DrugStore.com)
Atenolol-Chlorthalidone 50-25mg Tablets #30 for $13.99 ($0.47/unit)
Atenolol-Chlorthalidone 100-25mg Tablets #90 for $30.99 ($0.34/unit)
Atenolol (on 2/9/2012 at DrugStore.com)
Atenolol 50mg Tablets #90 for $17.99 ($0.20/unit)
Atenolol 100mg Tablets #90 for $18.99 ($0.21/unit)
Atenolol 25mg Tablets #90 for $14.99 ($0.17/unit)
Timolol Maleate (on 2/9/2012 at DrugStore.com)
Timolol Maleate 5mg Tablets #60 for $34.99 ($0.58/unit)
Timolol Maleate 10mg Tablets #60 for $39.99 ($0.67/unit)
Timolol Maleate 20mg Tablets #60 for $65.99 ($1.10/unit)
Timolol Maleate 0.25% Solution #15 for $19.99 ($1.33/unit)
Timolol Maleate 0.25% Gel Forming Solution 5ml Bottle #1 for $59.71 ($59.71/unit)
Timolol Maleate 0.5% Gel Forming Solution 5ml Bottle #1 for $55.99 ($55.99/unit)
Timolol Maleate 0.25% Solution 5ml Bottle #1 for $12.99 ($12.99/unit)
Timolol Maleate 0.25% Solution 10ml Bottle #1 for $16.99 ($16.99/unit)
Timolol Maleate 0.5% Solution 5ml Bottle #1 for $15.99 ($15.99/unit)
Timolol Maleate 0.5% Solution 10ml Bottle #1 for $19.99 ($19.99/unit)
Timolol Maleate 0.5% Solution 15ml Bottle #1 for $20.99 ($20.99/unit)
Dorzolamide-Timolol (on 2/9/2012 at DrugStore.com)
Dorzolamide-Timolol 2-0.5% Solution 10ml Bottle #1 for $99.99 ($99.99/unit)
Nadolol-Bendroflumethiazide (on 2/9/2012 at DrugStore.com)
Nadolol-Bendroflumethiazide 40-5mg Tablets #100 for $219.99 ($2.20/unit)
Nadolol (on 2/9/2012 at DrugStore.com)
Nadolol 20mg Tablets #30 for $14.99 ($0.50/unit)
Nadolol 80mg Tablets #30 for $22.99 ($0.77/unit)
Nadolol 40mg Tablets #30 for $16.99 ($0.57/unit)
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

Adrenergic beta-Antagonists (C0001645)

Definition (NCI) Natural or synthetic beta adrenergic antagonists selectively blocking or diminishing physiologic beta-adrenergic agonist actions on the sympathetic system. This group of antagonists are generally used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.
Definition (CHV) a type of drug used for hypertension, migrane, cardiac infarction, etc
Definition (CHV) a type of drug used for hypertension, migrane, cardiac infarction, etc
Definition (CHV) a type of drug used for hypertension, migrane, cardiac infarction, etc
Definition (CHV) a type of drug used for hypertension, migrane, cardiac infarction, etc
Definition (CHV) a type of drug used for hypertension, migrane, cardiac infarction, etc
Definition (CHV) a type of drug used for hypertension, migrane, cardiac infarction, etc
Definition (CHV) a type of drug used for hypertension, migrane, cardiac infarction, etc
Definition (CHV) a type of drug used for hypertension, migrane, cardiac infarction, etc
Definition (CHV) a type of drug used for hypertension, migrane, cardiac infarction, etc
Definition (CHV) a type of drug used for hypertension, migrane, cardiac infarction, etc
Definition (CHV) a type of drug used for hypertension, migrane, cardiac infarction, etc
Definition (MSH) Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.
Concepts Pharmacologic Substance (T121)
MSH D000319
SnomedCT 318350007, 33252009, 373254001
English beta Adrenergic Blocking Agents, beta Adrenergic Receptor Blockaders, beta Blockers, Adrenergic, Adrenergic beta Antagonists, Adrenergic beta Receptor Blockaders, Adrenergic beta-Blockers, Adrenergic beta-Receptor Blockaders, Agents, beta-Adrenergic Blocking, Blockaders, Adrenergic beta-Receptor, Blockaders, beta-Adrenergic Receptor, Blockers, beta-Adrenergic, Blocking Agents, beta-Adrenergic, Receptor Blockaders, beta-Adrenergic, beta Adrenergic Blockers, beta-Adrenergic Blockers, beta-Adrenergic Blocking Agents, beta-Adrenergic Receptor Blockaders, beta-Antagonists, Adrenergic, beta-Blockers, Adrenergic, beta-Receptor Blockaders, Adrenergic, Beta-adrenoceptor blocker, beta-Adrenergic blocking agent, NOS, beta-Blocking agent, NOS, BETA BLOCKERS ADREN, ADREN BETA RECEPT BLOCK, BETA ADREN RECEPT BLOCK, BETA ADREN BLOCK, ADREN BETA ANTAG, ADRENERGIC ANTAGONISTS BETA, ADRENERGIC RECEPTOR BLOCKADERS BETA, BETA ADREN BLOCK AGENTS, beta blocker, beta adrenergic blocking agents (medication), adrenergic beta receptor blockaders, beta adrenergic blocking agents, Beta-adrenoceptor blocking drug (substance), Adrenergic beta-Antagonists, Beta-Blockers, Beta Blocker, beta-Adrenergic Blocker [EPC], beta-Adrenergic Receptor Inhibitor, beta-Adrenergic Blocker, beta-adrenergic receptor blockaders, Beta blockers, beta-adrenergic blocking agents, beta adrenergic blockers, beta blockers, beta-adrenergic blocking agent, beta-blocking agent, beta adrenergic antagonist, beta adrenergic blocker, beta-blocker, beta-adrenergic blockers, Beta-adrenoceptor blocking drug, Beta-blocker, beta-Adrenergic blocking agent, beta-Blocking agent (product), beta-Blocking agent (substance), beta-Blocking agent, Beta-adrenoceptor blocking agent, Beta Blockers, Beta-Adrenergic Antagonist, Beta-Adrenergic Blocking Agent, Beta-adrenergic Blocking Agents
French Bêta-bloquants adrénergiques, Bêta-adrénolytiques, Bêta-bloquants, Adrénolytiques bêta, Antagonistes bêta-adrénergiques, Antagonistes des récepteurs adrénergiques bêta, Bêta-bloqueurs
Swedish Adrenerga betablockerare
Spanish bloqueantes beta, Beta-adrenoceptor blocking drug, beta-Antagonistas Adrenérgicos, beta-Bloqueadores Adrenérgicos, beta-Antagonistas Adrenergicos, Bloqueadores de los Receptores beta-Adrenergicos, Agentes Bloqueadores beta-Adrenergicos, Agentes Bloqueadores beta-Adrenérgicos, Bloqueadores de los beta-Receptores Adrenergicos, beta-Bloqueadores Adrenergicos, Bloqueadores de los beta-Receptores Adrenérgicos, Bloqueadores de los Receptores beta-Adrenérgicos, agente betabloqueante (producto), agente betabloqueante (sustancia), agente betabloqueante, antiadrenérgicos beta, betabloqueantes, bloqueantes beta (producto), bloqueantes beta (sustancia)
Czech receptory adrenergní beta - blokátory, beta-adrenergní blokátory, betablokátory
Finnish Beetasalpaajat
Italian Bloccanti dei recettori adrenergici, Agenti bloccanti beta-adrenergici, Bloccanti beta-adrenergici, Beta-antagonisti adrenergici
Russian ADRENERGICHESKIE BETA-ANTAGONISTY, ADRENERGICHESKIKH BETA-RETSEPTOROV BLOKATORY, BETA-ADRENERGICHESKIKH RETSEPTOROV BLOKATORY, BETA-ADRENOLITICHESKIE SREDSTVA, BETA-ADRENOLITIKI, BETA-BLOKATORY ADRENERGICHESKIE, АДРЕНЕРГИЧЕСКИЕ БЕТА-АНТАГОНИСТЫ, АДРЕНЕРГИЧЕСКИХ БЕТА-РЕЦЕПТОРОВ БЛОКАТОРЫ, БЕТА-АДРЕНЕРГИЧЕСКИХ РЕЦЕПТОРОВ БЛОКАТОРЫ, БЕТА-АДРЕНОЛИТИКИ, БЕТА-АДРЕНОЛИТИЧЕСКИЕ СРЕДСТВА, БЕТА-БЛОКАТОРЫ АДРЕНЕРГИЧЕСКИЕ
German ADRENERGE REZEPTORENBLOCKER BETA, ADRENERGE ANTAGONISTEN BETA, Adrenerge Beta-Antagonisten, Adrenerge Beta-Rezeptorenblocker, Beta-Blocker, adrenerge, Beta-adrenerge Blocker, Beta-adrenerge Rezeptorenblocker
Croatian ADRENERGIČKI BETA-ANTAGONISTI
Polish Środki blokujące receptory adrenergiczne beta, Leki blokujące receptory beta-adrenergiczne, Beta-adrenolityki, Blokery beta, Antagoniści adrenergiczni beta
Japanese β-アドレナリン作動性受容体遮断薬, β-遮断剤, β-ブロッカー, β-受容体遮断薬, β-遮断薬, アドレナリンベータきっ抗剤, アドレナリン作用性ベータ受容体遮断剤, アドレナリン作用性ベータ受容体遮断薬, アドレナリン作用性ベータ拮抗薬, アドレナリン作用性ベータ遮断薬, ベータアドレナリン作用性受容体遮断薬, ベータアドレナリン作用性遮断薬, β-アドレナリン受容体遮断薬, β-アドレナリン遮断薬, β受容体遮断薬, β遮断薬, アドレナリンベータアンタゴニスト, アドレナリンベータブロッカー, アドレナリン作用性ベータ受容器遮断薬, ベータ遮断剤
Portuguese Agentes Bloqueadores beta-Adrenérgicos, Antagonistas Adrenérgicos beta, beta-Antagonistas Adrenérgicos, beta-Bloqueadores Adrenérgicos, Bloqueadores dos beta-Receptores Adrenérgicos, Bloqueadores dos Receptores beta-Adrenérgicos
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Atenolol (C0004147)

Definition (NCI) A synthetic isopropylamino-propanol derivative used as an antihypertensive, hypotensive and antiarrhythmic Atenolol acts as a peripheral, cardioselective beta blocker specific for beta-1 adrenergic receptors, without intrinsic sympathomimetic effects. It reduces exercise heart rates and delays atrioventricular conduction, with overall oxygen requirements decreasing. (NCI04)
Definition (MSH) A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.
Definition (CHV) a drug that treats rapid heart rate and high blood pressure
Definition (CSP) l-p-carbamoylmethylphenoxy-3-isopropylamino -2-propanol, is a peripheral beta blocker used as an antihypertensive; propranolol, by contrast, also has CNS effects.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D001262
SnomedCT 391790005, 387506000, 87652004
English Atenolol, Benzeneacetamide, 4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)-, atenolol, ATENOLOL, atenolol (medication), Atenolol - chemical (substance), Atenolol [Chemical/Ingredient], Atenolol (product), Atenolol (substance), Atenolol - chemical
Swedish Atenolol
Czech atenolol
Spanish Atenolol - chemical, atenolol (producto), atenolol (sustancia), atenolol, Atenolol
Finnish Atenololi
Russian ATENOLOL, ICI 66082, АТЕНОЛОЛ
Japanese アテノロール
Croatian ATENOLOL
Polish Atenolol
French Aténolol
German Atenolol
Italian Atenololo
Portuguese Atenolol
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Nadolol (C0027302)

Definition (NCI) A non-selective beta-adrenergic antagonist with antihypertensive and antiarrhythmic activities. Nadolol competitively blocks beta-1 adrenergic receptors located in the heart and vascular smooth muscle, inhibiting the activities of the catecholamines epinephrine and norepinephrine and producing negative inotropic and chronotropic effects. This agent exhibits antiarrhythmic activity via the impairment of atrioventricular (AV) node conduction and a corresponding reduction in sinus rate. In the kidney, inhibition of the beta-2 receptor within the juxtaglomerular apparatus results in the inhibition of renin production and a subsequent reduction in angiotensin II and aldosterone levels, thus inhibiting angiotensin II-dependent vasoconstriction and aldosterone-dependent water retention.
Definition (MSH) A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for MIGRAINE DISORDERS and for tremor.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D009248
SnomedCT 387482003, 82896009
English Nadolol, 2,3-Naphthalenediol, 5-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy)-1,2,3,4-tetrahydro-, nadolol, nadolol (medication), NADOLOL, Nadolol [Chemical/Ingredient], Nadolol (product), Nadolol (substance)
Swedish Nadolol
Czech nadolol
Finnish Nadololi
Russian NADOLOL, НАДОЛОЛ
Japanese ナドロール
Polish Nadolol
Spanish nadolol (producto), nadolol (sustancia), nadolol, Nadolol
French Nadolol
German Nadolol
Italian Nadololo
Portuguese Nadolol
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Timolol (C0040233)

Definition (MSH) A beta-adrenergic antagonist similar in action to PROPRANOLOL. The levo-isomer is the more active. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. It is also used in the treatment of MIGRAINE DISORDERS and tremor.
Definition (NCI) A propanolamine derivative and a non-selective beta-adrenergic antagonist with antihypertensive property. Timolol competitively binds to beta-1-adrenergic receptors in the heart and vascular smooth muscle and beta-2-receptors in the bronchial and vascular smooth muscle, resulting in a decrease in beta-adrenergic stimulation. Beta-1-receptor blockade results in a decrease in resting and exercise heart rate and cardiac output, a decrease in both systolic and diastolic blood pressure, and, possibly, a reduction in reflex orthostatic hypotension. Beta-2-blockade results in an increase in peripheral vascular resistance. The ultimate results include vasodilation, and negative chronotropic and inotropic cardiac effects. In addition, timolol reduces intra-ocular pressure possibly by decreasing aqueous humor production by reduction of blood flow to the ciliary processes and cAMP synthesis.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D013999
SnomedCT 372880004, 85591001
English Timolol, (S)-1-((1,1-Dimethylethyl)amino)-3-((4-(4-morpholinyl)-1,2,5-thiadazol-3-yl)oxy)-2-propanol, 2-Propanol, 1-((1,1-dimethylethyl)amino)-3-((4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl)oxy)-, (S)-, 2-Propanol, 1-((1,1-dimethylethyl)amino)-3-((4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl)oxy)-,(2S)-, (S)-1-(tert-Butylamino)-3-((4-morpholino-1,2,5-thiadiazol-3-yl)oxy)propan-2-ol, timolol (ophthalmic) (medication), timolol (medication), timolol (ophthalmic), Timolol, Ophthalmic, timolol ophthalmic, timolol, Timolol [Chemical/Ingredient], Timolol (product), Timolol (substance), TIMOLOL
Swedish Timolol
Czech timolol
Finnish Timololi
Russian TIMOLOL, ТИМОЛОЛ
Japanese チモレート, チマバック, ファルチモ, ブルンネ, チモプトール, マレイン酸チモロール, リズモン, チアブート, チモロールT, チモロール
Polish Timolol
Spanish timolol (producto), timolol (sustancia), timolol, Timolol
French Timolol
German Timolol
Italian Timololo
Portuguese Timolol
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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