Adrenergic beta-Antagonists

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.
DrugDrug NameDrug Indication
DB00187EsmololFor the rapid control of ventricular rate in patients with atrial fibrillation or atrial flutter in perioperative, postoperative, or other emergent circumstances where short term control of ventricular rate with a short-acting agent is desirable. Also used in noncompensatory sinus tachycardia where the rapid heart rate requires specific intervention.
DB00195BetaxololFor the management of hypertension.
DB00264MetoprololMetoprolol is indicated for the treatment of angina, heart failure, myocardial infarction, atrial fibrillation, atrial flutter and hypertension.[A175141] Some off-label uses of metoprolol include supraventricular tachycardia and thyroid storm.[A175141] All the indications of metoprolol are part of cardiovascular diseases. These conditions correspond to a number of diseases that involve the function of the heart and blood vessels. The underlying causes of these conditions are variable and can be due to genetic disposition, lifestyle decisions such as smoking, obesity, diet, and lack of exercise, and comorbidity with other conditions such as diabetes. The cardiovascular diseases are the leading cause of death on a global scale.[L5533]
DB00335Atenolol**Indicated** for:[label] 1) Management of hypertension alone and in combination with other antihypertensives. 2) Management of angina pectoris associated with coronary atherosclerosis. 3) Management of acute myocardial infarction in hemodynamically stable patients with a heart rate greater than 50 beats per minutes and a systolic blood pressure above 100 mmHg. **Off-label** uses include: 1) Secondary prevention of myocardial infarction.[A178156] 2) Management of heart failure.[A178153] 3) Management of atrial fibrillation.[A178141] 4) Management of supraventricular tachycardia.[A178162] 5) Management of ventricular arrythmias such as congenital long-QT and arrhythmogenic right ventricular cardiomyopathy.[A178168] 6) Management of symptomatic thyrotoxicosis in combination with [methimazole].[A178147] 7) Prophylaxis of migraine headaches.[A178171] 8) Management of alcohol withdrawal.[A178174,A178177]
DB00373TimololThe oral form is used to treat high blood pressure and prevent heart attacks, and occasionally to prevent migraine headaches. Ophthalmic timolol is indicated for the treamtnet of open-angle and occasionally secondary glaucoma.
DB00521CarteololFor the treatment of intraocular hypertension and chronic open-angle glaucoma
DB00571PropranololFor the prophylaxis of migraine.
DB00598LabetalolFor the management of hypertension (alone or in combination with other classes of antihypertensive agents), as well as chronic stable angina pectoris and sympathetic overactivity syndrome associated with severe tetanus. Labetalol is used parenterally for immediate reduction in blood pressure in severe hypertension or in hypertensive crises when considered an emergency, for the control of blood pressure in patients with pheochromocytoma and pregnant women with preeclampsia, and to produce controlled hypotension during anesthesia to reduce bleeding resulting from surgical procedures.
DB00612BisoprololFor management of heart failure, angina pectoris, and mild to moderate hypertension and for secondary prevention of myocardial infarction (MI).
DB00960PindololFor the management of hypertension, edema, ventricular tachycardias, and atrial fibrillation.
DB01136CarvedilolFor the treatment of mild or moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin.
DB01193AcebutololFor the management of hypertension and ventricular premature beats in adults.
DB01203NadololUsed in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension.
DB01210LevobunololFor lowering intraocular pressure (IOP) and may be used in patients with chronic open-angle glaucoma or ocular hypertension.
DB01214MetipranololIndicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open angle glaucoma.
DB00489SotalolSotalol is indicated to treat life threatening ventricular arrhytmias and maintain normal sinus rhythm in patients with atrial fibrillation or flutter.[Label] There are also oral solutions and intravenous injections indicated for patients requiring sotalol, but for whom a tablet would not be appropriate.[Label,L6373,L6376]
DB04861NebivololFor the treatment of essential hypertension.
DB00866AlprenololFor the treatment of hypertension, angina, and arrhythmia
DB01295BevantololFor the treatment of angina pectoris and hypertension.
DB01297PractololUsed in the emergency treatment of cardiac arrhythmias.
DB01359PenbutololPenbutolol is indicated in the treatment of mild to moderate arterial hypertension. It may be used alone or in combination with other antihypertensive agents, especially thiazide-type diuretics.Penbutolol is contraindicated in patients with cardiogenic shock, sinus bradycardia, second and third degree atrioventricular conduction block, bronchial asthma, and those with known hypersensitivity.
DB01580OxprenololUsed in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety.
DB04846CeliprololCeliprolol is indicated for the management of mild to moderate hypertension and effort-induced angina pectoris.
DB06726BufuralolNot Available
DB08807BopindololFor the management of hypertension, edema, ventricular tachycardias, and atrial fibrillation.
DB08808BupranololUsed to manage hypertension and tachycardia. Also used to treat glaucoma.
DB08952IndenololNot Available
DB09013BefunololUsed in the management of open angle glaucoma. PMID: 12480285.
DB09204ArotinololArtinolol was introduced to be used as an antihypertensive agent since 1986.[T88] It has been studied for other functions like tremor control for patients with Parkinson disease and it is currently in clinical trials for its use in the control of blood pressure and heart rate.[L1168]
DB11770TalinololNot Available
DB12212LandiololNot Available
DB12752BucindololNot Available
DB13508CloranololNot Available
DB13530MepindololNot Available
DB13757EpanololNot Available
DB13775TertatololNot Available
DB13443EsatenololNot Available
DB01182PropafenoneUsed to prolong the time to recurrence of paroxysmal atrial fibrillation/flutter (PAF) associated with disabling symptoms in patients without structural heart disease. Also used for the treatment of life-threatening documented ventricular arrhythmias, such as sustained ventricular tachycardia.
DB09351LevobetaxololUsed in the treatment of open-angle glaucoma and ocular hypertension [FDA Label].
DB11785AnisodamineNot Available
DB03322DexpropranololNot Available
DB01023FelodipineFor the treatment of mild to moderate essential hypertension.
DB01115NifedipineFor the management of vasospastic angina, chronic stable angina, hypertension, and Raynaud's phenomenon. May be used as a first line agent for left ventricular hypertrophy and isolated systolic hypertension (long-acting agents).
DB09083IvabradineIvabradine is indicated by the FDA to reduce the risk of hospitalization for worsening heart failure in adult patients with stable, symptomatic chronic heart failure with left ventricular ejection fraction ≤35%, who are in sinus rhythm with resting heart rate ≥70 beats per minute and either are on maximally tolerated doses of beta-blockers or have a contraindication to beta-blocker use. It is also indicated for treatment of stable symptomatic heart failure as a result of dilated cardiomyopathy for pediatric patients 6 months of age or more[FDA Label].
DrugDrug NameTargetType
DB00187EsmololBeta-1 adrenergic receptortarget
DB00187EsmololCytochrome P450 2D6enzyme
DB00195BetaxololBeta-1 adrenergic receptortarget
DB00195BetaxololBeta-2 adrenergic receptortarget
DB00195BetaxololCytochrome P450 1A2enzyme
DB00195BetaxololCytochrome P450 2D6enzyme
DB00264MetoprololBeta-1 adrenergic receptortarget
DB00264MetoprololCytochrome P450 2D6enzyme
DB00264MetoprololBeta-2 adrenergic receptortarget
DB00264MetoprololSolute carrier family 22 member 2transporter
DB00264MetoprololMultidrug resistance protein 1transporter
DB00264MetoprololSerum albumincarrier
DB00264MetoprololCytochrome P450 3A4enzyme
DB00335AtenololBeta-1 adrenergic receptortarget
DB00335AtenololBeta-2 adrenergic receptortarget
DB00335AtenololCytochrome P450 2D6enzyme
DB00335AtenololBile salt export pumptransporter
DB00335AtenololSerum albumincarrier
DB00373TimololBeta-1 adrenergic receptortarget
DB00373TimololBeta-2 adrenergic receptortarget
DB00373TimololCytochrome P450 2D6enzyme
DB00373TimololMultidrug resistance protein 1transporter
DB00373TimololCytochrome P450 2C19enzyme
DB00373TimololLysozymetarget
DB00521CarteololBeta-2 adrenergic receptortarget
DB00521CarteololBeta-1 adrenergic receptortarget
DB00521CarteololCytochrome P450 2D6enzyme
DB00571PropranololBeta-1 adrenergic receptortarget
DB00571PropranololBeta-2 adrenergic receptortarget
DB00571PropranololBeta-3 adrenergic receptortarget
DB00571Propranolol5-hydroxytryptamine receptor 1Atarget
DB00571Propranolol5-hydroxytryptamine receptor 1Btarget
DB00571PropranololCytochrome P450 1A2enzyme
DB00571PropranololCytochrome P450 2D6enzyme
DB00571PropranololAlpha-1-acid glycoprotein 1carrier
DB00571PropranololCytochrome P450 2C19enzyme
DB00571PropranololCytochrome P450 3A4enzyme
DB00571PropranololCytochrome P450 3A5enzyme
DB00571PropranololCytochrome P450 3A7enzyme
DB00571PropranololSolute carrier family 22 member 2transporter
DB00571PropranololMultidrug resistance protein 1transporter
DB00571PropranololCytochrome P450 1A1enzyme
DB00571PropranololAmine oxidase [flavin-containing] Aenzyme
DB00598LabetalolAlpha-1 adrenergic receptorstarget
DB00598LabetalolBeta-1 adrenergic receptortarget
DB00598LabetalolBeta-2 adrenergic receptortarget
DB00598LabetalolCytochrome P450 2D6enzyme
DB00598LabetalolCytochrome P450 2C19enzyme
DB00612BisoprololBeta-1 adrenergic receptortarget
DB00612BisoprololBeta-2 adrenergic receptortarget
DB00612BisoprololCytochrome P450 2D6enzyme
DB00612BisoprololCytochrome P450 3A4enzyme
DB00960PindololBeta-1 adrenergic receptortarget
DB00960PindololBeta-2 adrenergic receptortarget
DB00960Pindolol5-hydroxytryptamine receptor 1Atarget
DB00960Pindolol5-hydroxytryptamine receptor 1Btarget
DB00960PindololCytochrome P450 2D6enzyme
DB00960PindololBeta-3 adrenergic receptortarget
DB01136CarvedilolAlpha-1A adrenergic receptortarget
DB01136CarvedilolBeta-1 adrenergic receptortarget
DB01136CarvedilolNADH dehydrogenase [ubiquinone] 1 subunit C2target
DB01136CarvedilolBeta-2 adrenergic receptortarget
DB01136CarvedilolVascular endothelial growth factor Atarget
DB01136CarvedilolNatriuretic peptides Btarget
DB01136CarvedilolGap junction alpha-1 proteintarget
DB01136CarvedilolPotassium voltage-gated channel subfamily H member 2target
DB01136CarvedilolVascular cell adhesion protein 1target
DB01136CarvedilolCytochrome P450 2C9enzyme
DB01136CarvedilolCytochrome P450 2D6enzyme
DB01136CarvedilolXanthine dehydrogenase/oxidaseenzyme
DB01136CarvedilolMultidrug resistance protein 1transporter
DB01136CarvedilolCytochrome P450 1A2enzyme
DB01136CarvedilolCytochrome P450 3A4enzyme
DB01136CarvedilolCytochrome P450 1A1enzyme
DB01136CarvedilolCytochrome P450 2E1enzyme
DB01136CarvedilolProstaglandin G/H synthase 1enzyme
DB01136CarvedilolAlpha-1D adrenergic receptortarget
DB01136CarvedilolAlpha-1B adrenergic receptortarget
DB01136CarvedilolAlpha-2C adrenergic receptortarget
DB01136CarvedilolAlpha-2B adrenergic receptortarget
DB01136CarvedilolAlpha-2A adrenergic receptortarget
DB01136CarvedilolE-selectintarget
DB01136CarvedilolHypoxia-inducible factor 1-alphatarget
DB01136CarvedilolInward rectifier potassium channel 4target
DB01136CarvedilolUDP-glucuronosyltransferase 1-1enzyme
DB01193AcebutololBeta-1 adrenergic receptortarget
DB01193AcebutololCytochrome P450 2D6enzyme
DB01193AcebutololBeta-2 adrenergic receptortarget
DB01193AcebutololMultidrug resistance protein 1transporter
DB01203NadololBeta-1 adrenergic receptortarget
DB01203NadololBeta-2 adrenergic receptortarget
DB01203NadololMultidrug resistance protein 1transporter
DB01203NadololCytochrome P450 2D6enzyme
DB01210LevobunololBeta-1 adrenergic receptortarget
DB01210LevobunololBeta-2 adrenergic receptortarget
DB01210LevobunololCytochrome P450 2D6enzyme
DB01214MetipranololBeta-1 adrenergic receptortarget
DB01214MetipranololBeta-2 adrenergic receptortarget
DB01214MetipranololCytochrome P450 2D6enzyme
DB00489SotalolPotassium voltage-gated channel subfamily H member 2target
DB00489SotalolBeta-1 adrenergic receptortarget
DB00489SotalolBeta-2 adrenergic receptortarget
DB00489SotalolCytochrome P450 2D6enzyme
DB04861NebivololBeta-1 adrenergic receptortarget
DB04861NebivololCytochrome P450 2D6enzyme
DB04861NebivololBeta-2 adrenergic receptortarget
DB04861NebivololCytochrome P450 3A4enzyme
DB00866AlprenololBeta-1 adrenergic receptortarget
DB00866AlprenololBeta-2 adrenergic receptortarget
DB00866Alprenolol5-hydroxytryptamine receptor 1Atarget
DB00866AlprenololCytochrome P450 2D6enzyme
DB00866AlprenololBeta-3 adrenergic receptortarget
DB01295BevantololBeta-1 adrenergic receptortarget
DB01295BevantololBeta-2 adrenergic receptortarget
DB01295BevantololAlpha-1A adrenergic receptortarget
DB01295BevantololCytochrome P450 2D6enzyme
DB01297PractololBeta-1 adrenergic receptortarget
DB01297PractololCytochrome P450 2D6enzyme
DB01359PenbutololAlpha-1-acid glycoprotein 1carrier
DB01359PenbutololBeta-1 adrenergic receptortarget
DB01359PenbutololBeta-2 adrenergic receptortarget
DB01359Penbutolol5-hydroxytryptamine receptor 1Atarget
DB01359Penbutolol5-hydroxytryptamine receptor 1Btarget
DB01359PenbutololCytochrome P450 2D6enzyme
DB01580OxprenololBeta-1 adrenergic receptortarget
DB01580OxprenololBeta-2 adrenergic receptortarget
DB01580OxprenololSolute carrier family 22 member 2transporter
DB01580OxprenololCytochrome P450 2D6enzyme
DB01580OxprenololBeta-3 adrenergic receptortarget
DB04846CeliprololBeta-1 adrenergic receptortarget
DB04846CeliprololBeta-2 adrenergic receptortarget
DB04846CeliprololBeta-3 adrenergic receptortarget
DB04846CeliprololAlpha-2A adrenergic receptortarget
DB04846CeliprololAlpha-2B adrenergic receptortarget
DB04846CeliprololAlpha-2C adrenergic receptortarget
DB04846CeliprololCytochrome P450 2D6enzyme
DB06726BufuralolCytochrome P450 2D6enzyme
DB06726BufuralolBeta adrenergic receptortarget
DB08807BopindololBeta-1 adrenergic receptortarget
DB08807BopindololBeta-2 adrenergic receptortarget
DB08807Bopindolol5-hydroxytryptamine receptor 1Atarget
DB08807Bopindolol5-hydroxytryptamine receptor 1Btarget
DB08807BopindololBeta-3 adrenergic receptortarget
DB08807BopindololCytochrome P450 2D6enzyme
DB08808BupranololBeta-1 adrenergic receptortarget
DB08808BupranololBeta-2 adrenergic receptortarget
DB08808BupranololBeta-3 adrenergic receptortarget
DB08808BupranololCytochrome P450 2D6enzyme
DB08952IndenololCytochrome P450 2D6enzyme
DB09013BefunololBeta-1 adrenergic receptortarget
DB09013BefunololBeta-2 adrenergic receptortarget
DB09013BefunololCytochrome P450 2D6enzyme
DB09204ArotinololBeta-1 adrenergic receptortarget
DB09204ArotinololBeta-2 adrenergic receptortarget
DB09204ArotinololAlpha-1 adrenergic receptorstarget
DB09204ArotinololSerum albumincarrier
DB09204ArotinololAlpha-1-acid glycoprotein 1carrier
DB09204ArotinololCytochrome P450 2D6enzyme
DB11770TalinololCytochrome P450 2D6enzyme
DB12212LandiololCytochrome P450 2D6enzyme
DB12752BucindololCytochrome P450 2D6enzyme
DB13508CloranololCytochrome P450 2D6enzyme
DB13530MepindololCytochrome P450 2D6enzyme
DB13757EpanololCytochrome P450 2D6enzyme
DB13775TertatololCytochrome P450 2D6enzyme
DB13443EsatenololCytochrome P450 2D6enzyme
DB01182PropafenoneSodium channel protein type 5 subunit alphatarget
DB01182PropafenonePotassium voltage-gated channel subfamily H member 2target
DB01182PropafenoneCytochrome P450 1A2enzyme
DB01182PropafenoneCytochrome P450 2D6enzyme
DB01182PropafenoneCytochrome P450 2C8enzyme
DB01182PropafenoneCytochrome P450 3A4enzyme
DB01182PropafenoneMultidrug resistance protein 1transporter
DB01182PropafenoneBeta-1 adrenergic receptortarget
DB01182PropafenoneBeta-2 adrenergic receptortarget
DB09351LevobetaxololBeta-1 adrenergic receptortarget
DB09351LevobetaxololCytochrome P450 2D6enzyme
DB11785AnisodamineCytochrome P450 2D6enzyme
DB01023FelodipineVoltage-dependent calcium channel subunit alpha-2/delta-1target
DB01023FelodipineCalmodulintarget
DB01023FelodipineCytochrome P450 3A4enzyme
DB01023FelodipineVoltage-dependent L-type calcium channel subunit alpha-1Ctarget
DB01023FelodipineVoltage-dependent L-type calcium channel subunit beta-2target
DB01023FelodipineCytochrome P450 2C8enzyme
DB01023FelodipineCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1Btarget
DB01023FelodipineCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1Atarget
DB01023FelodipineVoltage-dependent T-type calcium channel subunit alpha-1Htarget
DB01023FelodipineVoltage-dependent calcium channel subunit alpha-2/delta-2target
DB01023FelodipineTroponin C, skeletal muscletarget
DB01023FelodipineTroponin C, slow skeletal and cardiac musclestarget
DB01023FelodipineMineralocorticoid receptortarget
DB01023FelodipineVoltage-dependent L-type calcium channel subunit alpha-1Dtarget
DB01023FelodipineVoltage-dependent L-type calcium channel subunit alpha-1Starget
DB01023FelodipineCytochrome P450 3A5enzyme
DB01023FelodipineCytochrome P450 3A7enzyme
DB01023FelodipineMultidrug resistance protein 1transporter
DB01023FelodipineCytochrome P450 2C9enzyme
DB01023FelodipineCytochrome P450 2D6enzyme
DB01023FelodipineBile salt export pumptransporter
DB01115NifedipineVoltage-dependent calcium channel subunit alpha-2/delta-1target
DB01115NifedipineCytochrome P450 3A4enzyme
DB01115NifedipineCytochrome P450 2E1enzyme
DB01115NifedipineCytochrome P450 2D6enzyme
DB01115NifedipineCalmodulintarget
DB01115NifedipineVoltage-dependent L-type calcium channel subunit alpha-1Dtarget
DB01115NifedipineVoltage-dependent L-type calcium channel subunit alpha-1Starget
DB01115NifedipineVoltage-dependent L-type calcium channel subunit alpha-1Ctarget
DB01115NifedipineVoltage-dependent L-type calcium channel subunit beta-2target
DB01115NifedipinePotassium voltage-gated channel subfamily A member 1target
DB01115NifedipineVoltage-dependent T-type calcium channel subunit alpha-1Htarget
DB01115NifedipineCytochrome P450 1A2enzyme
DB01115NifedipineCytochrome P450 2A6enzyme
DB01115NifedipineCytochrome P450 2C8enzyme
DB01115NifedipineCytochrome P450 3A5enzyme
DB01115NifedipineCytochrome P450 3A7enzyme
DB01115NifedipineCanalicular multispecific organic anion transporter 2transporter
DB01115NifedipineMultidrug resistance protein 1transporter
DB01115NifedipineCanalicular multispecific organic anion transporter 1transporter
DB01115NifedipineCytochrome P450 1A1enzyme
DB01115NifedipineCytochrome P450 2B6enzyme
DB01115NifedipineNuclear receptor subfamily 1 group I member 2target
DB01115NifedipineSolute carrier organic anion transporter family member 1B1transporter
DB01115NifedipineBile salt export pumptransporter
DB09083IvabradineCytochrome P450 3A4enzyme
DB09083IvabradinePotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2target