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A cardioselective beta-adrenergic blocker possessing properties and potency similar to propranolol, but without a negative inotropic effect. [PubChem]

• Able laboratories inc
• Apothecon sub bristol myers squibb co
• Astrazeneca lp
• Astrazeneca pharmaceuticals lp
• Aurobindo pharma ltd
• Caraco pharmaceutical laboratories ltd
• Dava pharmaceuticals inc
• Genpharm pharmaceuticals inc
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• Mutual pharmaceutical co inc
• Mylan pharmaceuticals inc
• Northstar healthcare holdings ltd
• Nostrum laboratories inc
• Pliva inc
• Sandoz inc
• Scs pharmaceuticals
• Teva pharmaceuticals usa
• Teva pharmaceuticals usa inc
• Unique pharmaceutical laboratories
• Watson laboratories inc
• Zydus pharmaceuticals usa inc

• Advanced Pharmaceutical Services Inc.
• Amerisource Health Services Corp.
• Apotheca Inc.
• AQ Pharmaceuticals Inc.
• A-S Medication Solutions LLC
• AstraZeneca Inc.
• Aurobindo Pharma Ltd.
• Bryant Ranch Prepack
• Cadila Healthcare Ltd.
• Caraco Pharmaceutical Labs
• Cardinal Health
• Comprehensive Consultant Services Inc.
• Corepharma LLC
• Darby Dental Supply Co. Inc.
• DAVA Pharmaceuticals
• Dept Health Central Pharmacy
• DHHS Program Support Center Supply Service Center
• Direct Dispensing Inc.
• Dispensing Solutions
• Diversified Healthcare Services Inc.
• Genpharm LP
• Golden State Medical Supply Inc.
• Group Health Cooperative
• H.J. Harkins Co. Inc.
• Heartland Repack Services LLC
• Innovative Manufacturing and Distribution Services Inc.
• Ipca Laboratories Ltd.
• Ivax Pharmaceuticals
• Kaiser Foundation Hospital
• Lake Erie Medical and Surgical Supply
• Liberty Pharmaceuticals
• Major Pharmaceuticals
• Mallinckrodt Inc.
• Medisca Inc.
• Medvantx Inc.
• Merckle GmbH
• Murfreesboro Pharmaceutical Nursing Supply
• Mutual Pharmaceutical Co.
• Mylan
• Neighborcare Repackaging Inc.
• Northstar Rx LLC
• Norwich Pharmaceuticals Inc.
• Novopharm Ltd.
• Nucare Pharmaceuticals Inc.
• Ohm Laboratories Inc.
• Pack Pharmaceuticals
• Palmetto Pharmaceuticals Inc.
• Par Pharmaceuticals
• PCA LLC
• PD-Rx Pharmaceuticals Inc.
• Pharmaceutical Utilization Management Program VA Inc.
• Pharmpak Inc.
• Physicians Total Care Inc.
• Piramal Healthcare
• Preferred Pharmaceuticals Inc.
• Prepackage Specialists
• Prepak Systems Inc.
• Qualitest
• Ranbaxy Laboratories
• Rebel Distributors Corp.
• Remedy Repack
• Sandhills Packaging Inc.
• Sandoz
• Southwood Pharmaceuticals
• Stat Scripts LLC
• Talbert Medical Management Corp.
• Teva Pharmaceutical Industries Ltd.
• Tya Pharmaceuticals
• UDL Laboratories
• United Research Laboratories Inc.
• Va Cmop Dallas
• Vangard Labs Inc.
• Watson Pharmaceuticals
• Zydus Pharmaceuticals

Synthesis Reference	Not Available
General Reference	Not Available

Type	small molecule

Classes

Phenols and Derivatives Ethers Phenethylamines Anisoles

Substructures

Hydroxy Compounds Aliphatic and Aryl Amines Phenols and Derivatives Amino Ketones Ethers Benzene and Derivatives Carbamates and Derivatives Amino Alcohols Phenethylamines Aromatic compounds Anisoles Carboxamides and Derivatives Carboxylic Acids and Derivatives Alcohols and Polyols Phenyl Esters

ANTIHYPERTENSIVES 降血压;

Indication	For the management of hypertention and long-term management of patients with angina pectoris
Pharmacodynamics	Atenolol, a competitive beta(1)-selective adrenergic antagonist, has the lowest lipid solubility of this drug class. Although it is similar to metoprolol, atenolol differs from pindolol and propranolol in that it does not have intrinsic sympathomimetic properties or membrane-stabilizing activity. Atenolol is used alone or with chlorthalidone in the management of hypertension and edema.
Mechanism of action	Like metoprolol, atenolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart and vascular smooth muscle, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension. Higher doses of atenolol also competitively block beta(2)-adrenergic responses in the bronchial and vascular smooth muscles.
Absorption	Approximately 50% of an oral dose is absorbed from the gastrointestinal tract, the remainder being excreted unchanged in the feces.
Volume of distribution	Not Available
Protein binding	Plasma protein binding is 6-16%
Metabolism	Hepatic (minimal)
Route of elimination	Approximately 50% of an oral dose is absorbed from the gastrointestinal tract, the remainder being excreted unchanged in the feces. Unlike propranolol or metoprolol, but like nadolol, atenolol undergoes little or no metabolism by the liver, and the absorbed portion is eliminated primarily by renal excretion.
Half life	6-7 hours
Clearance	Not Available
Toxicity	LD50=2000-3000 mg/kg(orally in mice). Symptoms of an atenolol overdose include a slow heart beat, shortness of breath, fainting, dizziness, weakness, confusion, nausea, and vomiting.
Affected organisms	Humans and other mammals
Pathways	Pathway Name SMPDB ID Atenolol Pathway SMP00298

Properties
State	solid
Experimental Properties	Property Value Source melting point 147 °C PhysProp water solubility 1.33E+004 mg/L (at 25 °C) MCFARLAND,JW ET AL. (2001) logP 0.16 HANSCH,C ET AL. (1995) Caco2 permeability -6.44 ADME Research, USCD pKa 9.6 MERCK INDEX (2001)
Predicted Properties	Property Value Source water solubility 4.29e-01 g/l ALOGPS logP 0.57 ALOGPS logP 0.43 ChemAxon logS -2.8 ALOGPS pKa (strongest acidic) 14.08 ChemAxon pKa (strongest basic) 9.67 ChemAxon physiological charge 1 ChemAxon hydrogen acceptor count 4 ChemAxon hydrogen donor count 3 ChemAxon polar surface area 84.58 ChemAxon rotatable bond count 8 ChemAxon refractivity 73.51 ChemAxon polarizability 29.98 ChemAxon

Drug	Interaction
Acetohexamide	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Ampicillin	Ampicillin decreases bioavailability of atenolol
Chlorpropamide	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Clonidine	Increased hypertension when clonidine stopped
Dihydroergotamine	Ischemia with risk of gangrene
Dihydroergotoxine	Ischemia with risk of gangrene
Diltiazem	Increased risk of bradycardia
Disopyramide	The beta-blocker, atenolol, may increase the toxicity of disopyramide.
Epinephrine	Hypertension, then bradycardia
Ergonovine	Ischmeia with risk of gangrene
Ergotamine	Ischemia with risk of gangrene
Fenoterol	Antagonism
Formoterol	Antagonism
Gliclazide	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Glipizide	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Glisoxepide	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Glyburide	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Glycodiazine	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Ibuprofen	Risk of inhibition of renal prostaglandins
Indacaterol	Beta-adrenergic antagonists, especially those that are not cardioselective, may interfere with the effect of indacaterol when administered concurrently. Beta-blockers may exacerbate bronchospasms in patients with COPD.
Indomethacin	Risk of inhibition of renal prostaglandins
Insulin Aspart	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Insulin Detemir	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Insulin Glargine	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Insulin Glulisine	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Insulin Lispro	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Isoproterenol	Antagonism
Lidocaine	The beta-blocker, atenolol, may increase the effect and toxicity of lidocaine.
Methysergide	Ischemia with risk of gangrene
Orciprenaline	Antagonism
Pipobroman	Antagonism
Pirbuterol	Antagonism
Piroxicam	Risk of inhibition of renal prostaglandins
Prazosin	Risk of hypotension at the beginning of therapy
Procaterol	Antagonism
Repaglinide	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Salbutamol	Antagonism
Salmeterol	Antagonism
Terazosin	Increased risk of hypotension. Initiate concomitant therapy cautiously.
Terbutaline	Antagonism
Tolazamide	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Tolbutamide	The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
Treprostinil	Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Verapamil	Increased effect of both drugs

• Consult your doctor before taking large amounts of Vitamin K (Green leafy vegetables).
• Take 30-60 minutes before meals, take at the same time each day.