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Details

Stereochemistry RACEMIC
Molecular Formula C14H22N2O3
Molecular Weight 266.3361
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ATENOLOL

SMILES

CC(C)NCC(O)COC1=CC=C(CC(N)=O)C=C1

InChI

InChIKey=METKIMKYRPQLGS-UHFFFAOYSA-N
InChI=1S/C14H22N2O3/c1-10(2)16-8-12(17)9-19-13-5-3-11(4-6-13)7-14(15)18/h3-6,10,12,16-17H,7-9H2,1-2H3,(H2,15,18)

HIDE SMILES / InChI

Molecular Formula C14H22N2O3
Molecular Weight 266.3361
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description
Curator's Comment: description was created based on several sources, including http://www.world-medicinehistory.com/2014/08/discovery-of-atenolol.html https://www.ncbi.nlm.nih.gov/pubmed/3730023

Atenolol is a Beta-1 cardio-selective adreno-receptor blocking agent discovered and developed by ICI in 1976. Atenolol was launched in the market under the trade name Tenormin in 1976, and became the best-selling Beta-blocker in the world in the 1980s and 1990s. TENORMIN is indicated for the treatment of hypertension, to lower blood pressure; also for the long-term management of patients with angina pectoris and also is indicated in the management of hemodynamically stable patients with definite or suspected acute myocardial infarction to reduce cardiovascular mortality. 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. Hypotensive mechanism of atenolol is very complex. Decrease in CO and inhibition of renin-angiotensin-aldosterone system may mainly be responsible for hypotension. It is likely that potassium retaining action of atenolol partly contributes to its hypotensive action. It is also hypothetized that renal kallikrein-kinin system may play a role in modulating the hypotensive action of atenolol.

CNS Activity

Curator's Comment: Known to be CNS non penetrant in dog. Human data not available.

Approval Year

Targets

Targets

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
TENORMIN

Approved Use

Hypertension Atenolol tablets are indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure lowers the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacologic classes including atenolol tablets. Control of high blood pressure should be part of comprehensive cardiovascular risk management, including, as appropriate, lipid control, diabetes management, antithrombotic therapy, smoking cessation, exercise and limited sodium intake. Many patients will require more than one drug to achieve blood pressure goals. For specific advice on goals and management, see published guidelines, such as those of the National High Blood Pressure Education Program’s Joint National Committee on Prevention, Detection, Evaluation and Treatment of High Blood Pressure (JNC). Numerous antihypertensive drugs, from a variety of pharmacologic classes and with different mechanisms of action, have been shown in randomized controlled trials to reduce cardiovascular morbidity and mortality, and it can be concluded that it is blood pressure reduction, and not some other pharmacologic property of the drugs, that is largely responsible for those benefits. The largest and most consistent cardiovascular outcome benefit has been a reduction in the risk of stroke, but reductions in myocardial infarction and cardiovascular mortality also have been seen regularly. Elevated systolic or diastolic pressure causes increased cardiovascular risk, and the absolute risk increase per mmHg is greater at higher blood pressures, so that even modest reductions of severe hypertension can provide substantial benefit. Relative risk reduction from blood pressure reduction is similar across populations with varying absolute risk, so the absolute benefit is greater in patients who are at higher risk independent of their hypertension (for example, patients with diabetes or hyperlipidemia), and such patients would be expected to benefit from more aggressive treatment to a lower blood pressure goal. Some antihypertensive drugs have smaller blood pressure effects (as monotherapy) in black patients, and many antihypertensive drugs have additional approved indications and effects (e.g., on angina, heart failure or diabetic kidney disease). These considerations may guide selection of therapy. Atenolol tablets may be administered with other antihypertensive agents. Angina Pectoris Due to Coronary Atherosclerosis Atenolol tablets are indicated for the long-term management of patients with angina pectoris. Acute Myocardial Infarction Atenolol tablets are indicated in the management of hemodynamically stable patients with definite or suspected acute myocardial infarction to reduce cardiovascular mortality. Treatment can be initiated as soon as the patient's clinical condition allows. (See DOSAGE AND ADMINISTRATION, CONTRAINDICATIONS, and WARNINGS.) In general, there is no basis for treating patients like those who were excluded from the ISIS-1 trial (blood pressure less than 100 mm Hg systolic, heart rate less than 50 bpm) or have other reasons to avoid beta blockade. As noted above, some subgroups (e.g., elderly patients with systolic blood pressure below 120 mm Hg) seemed less likely to benefit.

Launch Date

3.67027192E11
Primary
TENORMIN

Approved Use

Hypertension Atenolol tablets are indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure lowers the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacologic classes including atenolol tablets. Control of high blood pressure should be part of comprehensive cardiovascular risk management, including, as appropriate, lipid control, diabetes management, antithrombotic therapy, smoking cessation, exercise and limited sodium intake. Many patients will require more than one drug to achieve blood pressure goals. For specific advice on goals and management, see published guidelines, such as those of the National High Blood Pressure Education Program’s Joint National Committee on Prevention, Detection, Evaluation and Treatment of High Blood Pressure (JNC). Numerous antihypertensive drugs, from a variety of pharmacologic classes and with different mechanisms of action, have been shown in randomized controlled trials to reduce cardiovascular morbidity and mortality, and it can be concluded that it is blood pressure reduction, and not some other pharmacologic property of the drugs, that is largely responsible for those benefits. The largest and most consistent cardiovascular outcome benefit has been a reduction in the risk of stroke, but reductions in myocardial infarction and cardiovascular mortality also have been seen regularly. Elevated systolic or diastolic pressure causes increased cardiovascular risk, and the absolute risk increase per mmHg is greater at higher blood pressures, so that even modest reductions of severe hypertension can provide substantial benefit. Relative risk reduction from blood pressure reduction is similar across populations with varying absolute risk, so the absolute benefit is greater in patients who are at higher risk independent of their hypertension (for example, patients with diabetes or hyperlipidemia), and such patients would be expected to benefit from more aggressive treatment to a lower blood pressure goal. Some antihypertensive drugs have smaller blood pressure effects (as monotherapy) in black patients, and many antihypertensive drugs have additional approved indications and effects (e.g., on angina, heart failure or diabetic kidney disease). These considerations may guide selection of therapy. Atenolol tablets may be administered with other antihypertensive agents. Angina Pectoris Due to Coronary Atherosclerosis Atenolol tablets are indicated for the long-term management of patients with angina pectoris. Acute Myocardial Infarction Atenolol tablets are indicated in the management of hemodynamically stable patients with definite or suspected acute myocardial infarction to reduce cardiovascular mortality. Treatment can be initiated as soon as the patient's clinical condition allows. (See DOSAGE AND ADMINISTRATION, CONTRAINDICATIONS, and WARNINGS.) In general, there is no basis for treating patients like those who were excluded from the ISIS-1 trial (blood pressure less than 100 mm Hg systolic, heart rate less than 50 bpm) or have other reasons to avoid beta blockade. As noted above, some subgroups (e.g., elderly patients with systolic blood pressure below 120 mm Hg) seemed less likely to benefit.

Launch Date

3.67027192E11
Primary
TENORMIN

Approved Use

Hypertension Atenolol tablets are indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure lowers the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacologic classes including atenolol tablets. Control of high blood pressure should be part of comprehensive cardiovascular risk management, including, as appropriate, lipid control, diabetes management, antithrombotic therapy, smoking cessation, exercise and limited sodium intake. Many patients will require more than one drug to achieve blood pressure goals. For specific advice on goals and management, see published guidelines, such as those of the National High Blood Pressure Education Program’s Joint National Committee on Prevention, Detection, Evaluation and Treatment of High Blood Pressure (JNC). Numerous antihypertensive drugs, from a variety of pharmacologic classes and with different mechanisms of action, have been shown in randomized controlled trials to reduce cardiovascular morbidity and mortality, and it can be concluded that it is blood pressure reduction, and not some other pharmacologic property of the drugs, that is largely responsible for those benefits. The largest and most consistent cardiovascular outcome benefit has been a reduction in the risk of stroke, but reductions in myocardial infarction and cardiovascular mortality also have been seen regularly. Elevated systolic or diastolic pressure causes increased cardiovascular risk, and the absolute risk increase per mmHg is greater at higher blood pressures, so that even modest reductions of severe hypertension can provide substantial benefit. Relative risk reduction from blood pressure reduction is similar across populations with varying absolute risk, so the absolute benefit is greater in patients who are at higher risk independent of their hypertension (for example, patients with diabetes or hyperlipidemia), and such patients would be expected to benefit from more aggressive treatment to a lower blood pressure goal. Some antihypertensive drugs have smaller blood pressure effects (as monotherapy) in black patients, and many antihypertensive drugs have additional approved indications and effects (e.g., on angina, heart failure or diabetic kidney disease). These considerations may guide selection of therapy. Atenolol tablets may be administered with other antihypertensive agents. Angina Pectoris Due to Coronary Atherosclerosis Atenolol tablets are indicated for the long-term management of patients with angina pectoris. Acute Myocardial Infarction Atenolol tablets are indicated in the management of hemodynamically stable patients with definite or suspected acute myocardial infarction to reduce cardiovascular mortality. Treatment can be initiated as soon as the patient's clinical condition allows. (See DOSAGE AND ADMINISTRATION, CONTRAINDICATIONS, and WARNINGS.) In general, there is no basis for treating patients like those who were excluded from the ISIS-1 trial (blood pressure less than 100 mm Hg systolic, heart rate less than 50 bpm) or have other reasons to avoid beta blockade. As noted above, some subgroups (e.g., elderly patients with systolic blood pressure below 120 mm Hg) seemed less likely to benefit.

Launch Date

3.67027192E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1.75 μg/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATENOLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
0.75 μg/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATENOLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
0.3 μg × h/mL
10 mg single, intravenous
dose: 10 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
ATENOLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
13.45 μg × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATENOLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
8.47 μg × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATENOLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
5.4 h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATENOLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
5.9 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ATENOLOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
7 h
unknown
ATENOLOL plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
94%
unknown
ATENOLOL plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
540 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 540 mg, 1 times / day
Route: oral
Route: multiple
Dose: 540 mg, 1 times / day
Sources:
unhealthy, 42 to 65 years
n = 16
Health Status: unhealthy
Condition: hypertension
Age Group: 42 to 65 years
Sex: M+F
Population Size: 16
Sources:
DLT: Bradycardia...
Dose limiting toxicities:
Bradycardia (31%)
Sources:
900 mg 1 times / day multiple, oral
Highest studied dose
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
unhealthy, 42 years
n = 1
Health Status: unhealthy
Condition: hypertension
Age Group: 42 years
Sex: M
Population Size: 1
Sources:
Other AEs: Somnolence, Exertional dyspnea...
Other AEs:
Somnolence
Exertional dyspnea
Sources:
150 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy, mean age 53 years
n = 9
Health Status: unhealthy
Condition: angina pectoris
Age Group: mean age 53 years
Sex: M+F
Population Size: 9
Sources:
DLT: Fatigue...
Dose limiting toxicities:
Fatigue (11%)
Sources:
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy, mean age 62 years
n = 32
Health Status: unhealthy
Condition: ventricular ectopy
Age Group: mean age 62 years
Sex: M+F
Population Size: 32
Sources:
Disc. AE: Vertigo, Bronchospasm...
AEs leading to
discontinuation/dose reduction:
Vertigo (6.2%)
Bronchospasm (3%)
Fatigue (3%)
Sources:
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, mean age 62 years
n = 32
Health Status: unhealthy
Condition: ventricular ectopy
Age Group: mean age 62 years
Sex: M+F
Population Size: 32
Sources:
Disc. AE: Ventricular tachycardia...
AEs leading to
discontinuation/dose reduction:
Ventricular tachycardia (3%)
Sources:
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
n = 18
Health Status: unhealthy
Condition: Hypertension
Population Size: 18
Sources:
Other AEs: Fatigue, Nausea...
Other AEs:
Fatigue (below serious, 2 patients)
Nausea (below serious, 2 patients)
Sources:
AEs

AEs

AESignificanceDosePopulation
Bradycardia 31%
DLT
540 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 540 mg, 1 times / day
Route: oral
Route: multiple
Dose: 540 mg, 1 times / day
Sources:
unhealthy, 42 to 65 years
n = 16
Health Status: unhealthy
Condition: hypertension
Age Group: 42 to 65 years
Sex: M+F
Population Size: 16
Sources:
Exertional dyspnea
900 mg 1 times / day multiple, oral
Highest studied dose
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
unhealthy, 42 years
n = 1
Health Status: unhealthy
Condition: hypertension
Age Group: 42 years
Sex: M
Population Size: 1
Sources:
Somnolence
900 mg 1 times / day multiple, oral
Highest studied dose
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
unhealthy, 42 years
n = 1
Health Status: unhealthy
Condition: hypertension
Age Group: 42 years
Sex: M
Population Size: 1
Sources:
Fatigue 11%
DLT
150 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy, mean age 53 years
n = 9
Health Status: unhealthy
Condition: angina pectoris
Age Group: mean age 53 years
Sex: M+F
Population Size: 9
Sources:
Bronchospasm 3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy, mean age 62 years
n = 32
Health Status: unhealthy
Condition: ventricular ectopy
Age Group: mean age 62 years
Sex: M+F
Population Size: 32
Sources:
Fatigue 3%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy, mean age 62 years
n = 32
Health Status: unhealthy
Condition: ventricular ectopy
Age Group: mean age 62 years
Sex: M+F
Population Size: 32
Sources:
Vertigo 6.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy, mean age 62 years
n = 32
Health Status: unhealthy
Condition: ventricular ectopy
Age Group: mean age 62 years
Sex: M+F
Population Size: 32
Sources:
Ventricular tachycardia 3%
Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, mean age 62 years
n = 32
Health Status: unhealthy
Condition: ventricular ectopy
Age Group: mean age 62 years
Sex: M+F
Population Size: 32
Sources:
Fatigue below serious, 2 patients
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
n = 18
Health Status: unhealthy
Condition: Hypertension
Population Size: 18
Sources:
Nausea below serious, 2 patients
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
n = 18
Health Status: unhealthy
Condition: Hypertension
Population Size: 18
Sources:
PubMed

PubMed

TitleDatePubMed
Cardiovascular and adrenergic effects of cigarette smoking during immediate non-selective and selective beta adrenoceptor blockade in humans.
1979 Jun
Atenolol induced high grade AV block.
1998 Aug
Sleep attacks and Parkinson's disease treatment.
2000 Apr 15
Carvedilol prevents epinephrine-induced apoptosis in human coronary artery endothelial cells: modulation of Fas/Fas ligand and caspase-3 pathway.
2000 Feb
Bupivacaine inhibits baroreflex control of heart rate in conscious rats.
2000 Jan
L-Dopa uptake and dopamine production in proximal tubular cells are regulated by beta(2)-adrenergic receptors.
2000 Jul
Mechanism of action of noradrenaline on secretion of progesterone and oxytocin by the bovine corpus luteum in vitro.
2001
Effect of strict blood pressure control on proteinuria in renal patients treated with different antihypertensive drugs.
2001
Treating hypertension in women of child-bearing age and during pregnancy.
2001
[In vitro permeability studies as a substitute for in vivo studies--which requirements have to be met?].
2001
[The comparison of the efficacy of atenolol and isosorbide dinitrate therapy in chronic hypotension patients with stable angina pectoris].
2001
[Comparison of carvedilol and atenolol efficacy in patients with stable effort angina].
2001
Beta-blockade with nebivolol enhances the acetylcholine-induced cutaneous vasodilation.
2001 Apr
Testing the effectiveness of converting patients to long-acting antianginal medications: The Quality of Life in Angina Research Trial (QUART).
2001 Apr
The effects of opioids on isolated human pregnant uterine muscles.
2001 Apr
Small blood volumes from children for quantitative sotalol determination using high-performance liquid chromatography.
2001 Apr 5
Quantitative structure-retention and retention-activity relationships of beta-blocking agents by micellar liquid chromatography.
2001 Apr 6
LIFE study--still-blinded results show promise.
2001 Apr-May
A 39-year-old man with an overdose of beta-blockers.
2001 Aug
Antihypertensive therapy and the risk of malignancies.
2001 Aug
Can we assess the efficacy of therapy in neurocardiogenic syncope?
2001 Feb
Lack of efficacy of atenolol for the prevention of neurally mediated syncope in a highly symptomatic population: a prospective, double-blind, randomized and placebo-controlled study.
2001 Feb
[Intense muscle fatigue: an undesirable effect of beta blockers use in morbid obesity].
2001 Feb 24
Enhancer aided in vitro permeation of atenolol and prazosin hydrochloride through mice skin.
2001 Jan
Long-term stability characterization of a controlled release gastrointestinal therapeutic system coated with a cellulose acetate pseudolatex.
2001 Jan
Reversal of deteriorated fractal behavior of heart rate variability by beta-blocker therapy in patients with advanced congestive heart failure.
2001 Jan
Evidence for the binding of beta-adrenoceptor blockers to microsomal Na+/K+-ATPase in guinea pig heart preparations.
2001 Jan
Denopamine, a beta(1)-adrenergic agonist, increases alveolar fluid clearance in ex vivo rat and guinea pig lungs.
2001 Jan
Buccal iontophoretic delivery of atenolol.HCl employing a new in vitro three-chamber permeation cell.
2001 Jan 29
Influence of atenolol on the kinetics of RT interval rate adaptation in conscious dogs.
2001 Jul
A new aspect of view in synthesizing new type beta-adrenoceptor blockers with ancillary antioxidant activities.
2001 Jul
Ouabain-induced coronary vasoconstriction in cats is not neurally mediated.
2001 Jul
An economic evaluation of atenolol vs. captopril in patients with Type 2 diabetes (UKPDS 54).
2001 Jun
Pharmacoutilization of antihypertensive drugs: a model of analysis.
2001 Jun
Pharmacological investigation on nigrescigenin-a cardenolide from Parquetina nigrescens (Afzel.) Bullock: comparative studies on cardiotonic effects of Parquetina nigrescens, g-strophanthin and noradrenaline in guinea-pig isolated atria.
2001 Jun
Usefulness of the head-upright tilt test for distinguishing syncope and epilepsy in children.
2001 Jun
Beta-blockers, diabetes, and hypoglycemia: risky business?
2001 Mar
By the way, doctor...I have hypertension, and I take a beta blocker called atenolol and an ACE inhibitor every morning. But I find that my blood pressure is high when I first get up. As the day goes on, my pressure falls. It seems like it's always pretty good by the time I see my doctor, so she thinks everything is fine. But the high numbers worry me. Should I be on another drug?
2001 Mar
Development and validation of an automated method for the liquid chromatographic determination of sotalol in plasma using dialysis and trace enrichment on a cation-exchange pre-column as on-line sample preparation.
2001 Mar
Efficacy and safety of losartan/hydrochlorothiazide in patients with severe hypertension.
2001 Mar 15
Smoothed pseudo Wigner-Ville distribution as an alternative to Fourier transform in rats.
2001 Mar 23
Nebivolol and airway responsiveness in the rabbit.
2001 Mar 23
beta(1)- and beta(2)-Adrenoceptor-mediated thermogenesis and lipid utilization in obese and lean men.
2001 May
Stereospecific pharmacokinetics and pharmacodynamics of beta-adrenergic blockers in humans.
2001 May-Aug
A prospective comparison of four antihypertensive agents in daily clinical practice.
2001 May-Jun
Patents

Sample Use Guides

Hypertension: The initial dose of TENORMIN (atenolol) is 50 mg given as one tablet a day either alone or added to diuretic therapy. The full effect of this dose will usually be seen within one to two weeks. Angina Pectoris: The initial dose of TENORMIN is 50 mg given as one tablet a day. If an optimal response is not achieved within one week, the dosage should be increased to TENORMIN 100 mg given as one tablet a day. In patients with definite or suspected acute myocardial infarction, treatment with TENORMIN I.V. Treatment should begin with the intravenous administration of 5 mg TENORMIN over 5 minutes followed by another 5 mg intravenous injection 10 minutes later. TENORMIN I.V. Injection should be administered under carefully controlled conditions including monitoring of blood pressure, heart rate, and electrocardiogram.
Route of Administration: Other
The aim of the study was to assess the effects of the beta-blocker atenolol and the high energy demand in an ischaemia-reperfusion model free of neurohormonal and vascular factors. There was exposed Langendorff-perfused isolated rat hearts to low-flow ischaemia (30 min) and reflow (20 min). Three groups of hearts were used: control hearts (n =11), hearts that were perfused with 2.5 micrograms l-1atenolol (n =9), and hearts electrically paced during ischaemia to distinguish the effect of heart rate from that of the drug (n =9). During ischaemia, the pressure-rate product was 2.3+/-0.2, 5.2+/-1.1, and 3.3+/-0.3 mm Hg 10(3) min in the control, atenolol and paced hearts, respectively. In addition, the ATP turnover rate, calculated from venous (lactate), oxygen uptake and flow, was higher in atenolol (11.2+/-1.7 micromol min-1) and paced (8.1+/-0.8 micromol min-1) hearts than in control (6.2+/-0.8 micromol min-1). At the end of reflow, the pressurexrate product recovered 75.1+/-6.4% of baseline in control vs 54.1+/-9.1 and 48.8+/-4.4% in atenolol and paced hearts (P<0.05).
Substance Class Chemical
Created
by admin
on Sat Dec 16 18:03:17 UTC 2023
Edited
by admin
on Sat Dec 16 18:03:17 UTC 2023
Record UNII
50VV3VW0TI
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ATENOLOL
EP   HSDB   INN   MART.   MI   ORANGE BOOK   USAN   USP   USP-RS   VANDF   WHO-DD   WHO-IP  
INN   USAN  
Official Name English
ATENOLOL [USAN]
Common Name English
DURAATENOLOL
Common Name English
Atenolol [WHO-DD]
Common Name English
ATENOLOL [USP MONOGRAPH]
Common Name English
C07AB03
Code English
ATENOLOL [JAN]
Common Name English
ICI 66082
Code English
ATENOLOL [HSDB]
Common Name English
BENZENEACETAMIDE, 4-(2-HYDROXY-3-((1-METHYLETHYL)AMINO)PROPOXY)-
Systematic Name English
UROSIN
Common Name English
ATENOLOL [VANDF]
Common Name English
COROTENOL
Common Name English
TENORETIC COMPONENT ATENOLOL
Common Name English
ATENOLOL [MART.]
Common Name English
ATENOLOL [ORANGE BOOK]
Common Name English
ATENOLOL [EP MONOGRAPH]
Common Name English
ATENOLOL [USP IMPURITY]
Common Name English
JUVENTAL
Common Name English
ATENOLOL [MI]
Common Name English
BETACARD
Common Name English
ATENOLOLUM [WHO-IP LATIN]
Common Name English
ATENOLOL COMPONENT OF TENORETIC
Common Name English
NOVATEN
Common Name English
ATENOLOL [WHO-IP]
Common Name English
ICI-66082
Code English
2-(P-(HYDROXY-3-(ISOPROPYLAMINO)PROPOXY)PHENYL)ACETAMIDE
Systematic Name English
MYOCORD
Common Name English
ICI 66,082
Code English
POLYCAP COMPONENT ATENOLOL
Brand Name English
NSC-757832
Code English
ATENOLOL [USP-RS]
Common Name English
PRENORMINE
Common Name English
2-(P-(2-HYDROXY-3-(ISOPROPYLAMINO)PROPOXY)PHENYL)ACETAMIDE (RACEMATE)
Systematic Name English
atenolol [INN]
Common Name English
TENORMIN
Brand Name English
Classification Tree Code System Code
WHO-VATC QC07CB53
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
LIVERTOX NBK548379
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
WHO-ATC C07CB53
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
WHO-VATC QC07CB03
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
WHO-ATC C07BB03
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
WHO-ATC C07DB01
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
WHO-ATC C07CB03
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
NDF-RT N0000000161
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
NCI_THESAURUS C29576
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
NDF-RT N0000175556
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
WHO-VATC QC07AB03
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
WHO-VATC QC07BB03
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
WHO-ATC C07FB03
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
WHO-VATC QC07DB01
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
WHO-VATC QC07FB03
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
WHO-ATC C07AB03
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
Code System Code Type Description
ChEMBL
CHEMBL24
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
CHEBI
55352
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
WIKIPEDIA
ATENOLOL
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
NSC
757832
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
DAILYMED
50VV3VW0TI
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
INN
3801
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
CHEBI
2904
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
ECHA (EC/EINECS)
249-451-7
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
IUPHAR
548
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
RS_ITEM_NUM
1044403
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
CAS
29122-68-7
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
FDA UNII
50VV3VW0TI
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
MESH
D001262
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
DRUG BANK
DB00335
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
RXCUI
1202
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY RxNorm
MERCK INDEX
m2120
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY Merck Index
EVMPD
SUB05590MIG
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
NCI_THESAURUS
C28836
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
LACTMED
Atenolol
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
PUBCHEM
2249
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
HSDB
6526
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
SMS_ID
100000091183
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
DRUG CENTRAL
255
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
EPA CompTox
DTXSID2022628
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY
WHO INTERNATIONAL PHARMACOPEIA
ATENOLOL
Created by admin on Sat Dec 16 18:03:20 UTC 2023 , Edited by admin on Sat Dec 16 18:03:20 UTC 2023
PRIMARY Description: A white or almost white powder. Solubility: Sparingly soluble in water; soluble in ethanol (~750 g/l) TS; slightly soluble in dichloromethane R. Category: Cardiovascular agent; &#946;-adrenoreceptor blocking agent. Storage: Atenolol should be kept in a tightly closed container. Requirement: Atenolol contains not less than 99.0% and not more than 101.0% of C14H22N2O3, calculated with reference to the dried substance.
Related Record Type Details
TARGET -> AGONIST
SHORT-ACTING
SALT/SOLVATE -> PARENT
ENANTIOMER -> RACEMATE
ENANTIOMER -> RACEMATE
SALT/SOLVATE -> PARENT
TARGET -> INHIBITOR
BINDING
IC50
Related Record Type Details
METABOLITE LESS ACTIVE -> PARENT
found to have only one tenth of the activity of atenolol
MINOR
Related Record Type Details
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
IMPURITY -> PARENT
IMPURITY -> PARENT
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
IMPURITY -> PARENT
IMPURITY -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC RENAL IMPAIRMENT: CREATINE CLEARANCE LESS THAN 15 mL/min/1.73 m(2

RENAL IMPAIRMENT: CREATININE CLEARANCE 15 mL/min/1.73 m(2) to 35 mL/min/1.73 m(2)

MAXIMUM TOLERATED DOSE TOXICITY
Tmax PHARMACOKINETIC
ORAL BIOAVAILABILITY PHARMACOKINETIC