ATENOLOL

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 Search

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

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/018240s032lbl.pdf
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

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Beta-2 adrenergic receptor 203 Target ID: CHEMBL210 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12795776	Antagonist 2778
Beta-1 adrenergic receptor 158 Target ID: CHEMBL213 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1979509	Antagonist 2778

Conditions

Condition	Modality	Highest Phase	Product
Hypertension 567 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/018240s032lbl.pdf	Primary	Approved 8429	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 1981
Angina pectoris 106 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/018240s032lbl.pdf	Primary	Approved 8429	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 1981
Acute myocardial infarction 37 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/018240s032lbl.pdf	Primary	Approved 8429	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 1981

C_max

Value	Dose	Co-administered	Analyte	Population
1.75 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/658112/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/658112/	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

Value	Dose	Analyte	Population
0.3 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/658112/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/658112/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/658112/	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

T_1/2

Value	Dose	Analyte	Population
5.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/658112/	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/658112/	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/018240s032lbl.pdf	unknown	ATENOLOL plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
94% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/018240s032lbl.pdf	unknown		ATENOLOL plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse 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: https://pubmed.ncbi.nlm.nih.gov/776487/	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: https://pubmed.ncbi.nlm.nih.gov/776487/	DLT: Bradycardia... Dose limiting toxicities: Bradycardia (31%) Sources: https://pubmed.ncbi.nlm.nih.gov/776487/
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: https://pubmed.ncbi.nlm.nih.gov/776487/	unhealthy, 42 years n = 1 Health Status: unhealthy Condition: hypertension Age Group: 42 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/776487/	Other AEs: Somnolence, Exertional dyspnea... Other AEs: Somnolence Exertional dyspnea Sources: https://pubmed.ncbi.nlm.nih.gov/776487/
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: https://pubmed.ncbi.nlm.nih.gov/6111212/	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: https://pubmed.ncbi.nlm.nih.gov/6111212/	DLT: Fatigue... Dose limiting toxicities: Fatigue (11%) Sources: https://pubmed.ncbi.nlm.nih.gov/6111212/
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: https://pubmed.ncbi.nlm.nih.gov/3802701/	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: https://pubmed.ncbi.nlm.nih.gov/3802701/	Disc. AE: Vertigo, Bronchospasm... AEs leading to discontinuation/dose reduction: Vertigo (6.2%) Bronchospasm (3%) Fatigue (3%) Sources: https://pubmed.ncbi.nlm.nih.gov/3802701/
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: https://pubmed.ncbi.nlm.nih.gov/3802701/	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: https://pubmed.ncbi.nlm.nih.gov/3802701/	Disc. AE: Ventricular tachycardia... AEs leading to discontinuation/dose reduction: Ventricular tachycardia (3%) Sources: https://pubmed.ncbi.nlm.nih.gov/3802701/
50 mg 1 times / day steady, oral Dose: 50 mg, 1 times / day Route: oral Route: steady Dose: 50 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01522950	unhealthy n = 18 Health Status: unhealthy Condition: Hypertension Population Size: 18 Sources: https://clinicaltrials.gov/ct2/show/NCT01522950	Other AEs: Fatigue, Nausea... Other AEs: Fatigue (below serious, 2 patients) Nausea (below serious, 2 patients) Sources: https://clinicaltrials.gov/ct2/show/NCT01522950

AEs

AE	Significance	Dose	Population
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: https://pubmed.ncbi.nlm.nih.gov/776487/	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: https://pubmed.ncbi.nlm.nih.gov/776487/
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: https://pubmed.ncbi.nlm.nih.gov/776487/	unhealthy, 42 years n = 1 Health Status: unhealthy Condition: hypertension Age Group: 42 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/776487/
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: https://pubmed.ncbi.nlm.nih.gov/776487/	unhealthy, 42 years n = 1 Health Status: unhealthy Condition: hypertension Age Group: 42 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/776487/
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: https://pubmed.ncbi.nlm.nih.gov/6111212/	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: https://pubmed.ncbi.nlm.nih.gov/6111212/
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: https://pubmed.ncbi.nlm.nih.gov/3802701/	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: https://pubmed.ncbi.nlm.nih.gov/3802701/
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: https://pubmed.ncbi.nlm.nih.gov/3802701/	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: https://pubmed.ncbi.nlm.nih.gov/3802701/
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: https://pubmed.ncbi.nlm.nih.gov/3802701/	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: https://pubmed.ncbi.nlm.nih.gov/3802701/
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: https://pubmed.ncbi.nlm.nih.gov/3802701/	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: https://pubmed.ncbi.nlm.nih.gov/3802701/
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: https://clinicaltrials.gov/ct2/show/NCT01522950	unhealthy n = 18 Health Status: unhealthy Condition: Hypertension Population Size: 18 Sources: https://clinicaltrials.gov/ct2/show/NCT01522950
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: https://clinicaltrials.gov/ct2/show/NCT01522950	unhealthy n = 18 Health Status: unhealthy Condition: Hypertension Population Size: 18 Sources: https://clinicaltrials.gov/ct2/show/NCT01522950

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
			inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
BSEP 402	OCT1 327 OCT2 355 MATE1 135 MATE2 96 OCT3 80 OAT1 326 OAT3 339

Drug as perpetrator

Target	Modality	Activity	Metabolite	Clinical evidence
BSEP 403	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/24014644/	weak

Drug as victim

Target	Modality	Activity
OAT1 326	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/26374172/	no
OAT3 339	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/26374172/	no
OCT3 80	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/26374172/	no
MATE1 135	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/26374172/\|https://pubmed.ncbi.nlm.nih.gov/27758931/	yes
MATE2 96	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/26374172/\|https://pubmed.ncbi.nlm.nih.gov/27758931/	yes
OCT1 327	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/26374172/\|https://pubmed.ncbi.nlm.nih.gov/29124159/	yes
OCT2 355	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/26374172/\|https://pubmed.ncbi.nlm.nih.gov/27758931/	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://pubmed.ncbi.nlm.nih.gov/16314852/

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:2904	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:2904
ChemicalBook	CB3753116	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB3753116
MolPort	MolPort-001-792-717	https://www.molport.com/shop/molecule-link/MolPort-001-792-717
eMolecules	27677625	https://www.emolecules.com/cgi-bin/more?vid=27677625
eMolecules	533825	https://www.emolecules.com/cgi-bin/more?vid=533825

PubMed

Title	Date	PubMed
Cardiovascular and adrenergic effects of cigarette smoking during immediate non-selective and selective beta adrenoceptor blockade in humans.	1979 Jun	113217
Perindopril/indapamide 2/0.625 mg/day: a review of its place in the management of hypertension.	2001	11465878
[Two complex suicidal poisonings with drugs and their medicolegal aspects].	2001	11450365
Barnidipine.	2001	11434453
Mechanism of action of noradrenaline on secretion of progesterone and oxytocin by the bovine corpus luteum in vitro.	2001	11402689
[A possible adverse effect from the association of losartan-mefenamic acid in hemodialysis].	2001	11385903
Effect of strict blood pressure control on proteinuria in renal patients treated with different antihypertensive drugs.	2001	11369828
Treating hypertension in women of child-bearing age and during pregnancy.	2001	11368252
[Postinfarction remodeling of the left atrium and left ventricle: effects of long-term treatment with beta adrenergic blockers and angiotensin converting enzyme inhibitors].	2001	11338850
[Efficacy of oncologic surgery. Does anesthesia influence the postoperative outcome?].	2001 Apr	11370395
Beta-blockade with nebivolol enhances the acetylcholine-induced cutaneous vasodilation.	2001 Apr	11309552
['Licorice hypertension' also caused by licorice tea].	2001 Apr 14	11332259
Mass spectrometric quantitation of chiral drugs by the kinetic method.	2001 Apr 15	11338581
Small blood volumes from children for quantitative sotalol determination using high-performance liquid chromatography.	2001 Apr 5	11334359
Quantitative structure-retention and retention-activity relationships of beta-blocking agents by micellar liquid chromatography.	2001 Apr 6	11330791
LIFE study--still-blinded results show promise.	2001 Apr-May	11474698
A 39-year-old man with an overdose of beta-blockers.	2001 Aug	11468625
Antihypertensive therapy and the risk of malignancies.	2001 Aug	11465967
Beta2-adrenoceptor-mediated prejunctional facilitation and postjunctional inhibition of sympathetic neuroeffector transmission in the guinea pig vas deferens.	2001 Aug	11454924
Differential role of adrenoceptors in control of plasma glucose and fatty acids in carp, Cyprinus carpio (L.).	2001 Aug	11448867
[Intense muscle fatigue: an undesirable effect of beta blockers use in morbid obesity].	2001 Feb 24	11333741
Enhancer aided in vitro permeation of atenolol and prazosin hydrochloride through mice skin.	2001 Jan	11349525
Antihypertensive effect of alpha- and beta-adrenergic blockade in obese and lean hypertensive subjects.	2001 Jul	11465655
Effects of drug therapy on cardiac arrhythmias and ischemia in hypertensives with LVH.	2001 Jul	11465647
Role of alpha1-blockade in congenital long QT syndrome: investigation by exercise stress test.	2001 Jul	11446501
Influence of atenolol on the kinetics of RT interval rate adaptation in conscious dogs.	2001 Jul	11444492
A new aspect of view in synthesizing new type beta-adrenoceptor blockers with ancillary antioxidant activities.	2001 Jul	11425575
Ouabain-induced coronary vasoconstriction in cats is not neurally mediated.	2001 Jul	11422216
Permanent cardiac pacing versus medical treatment for the prevention of recurrent vasovagal syncope: a multicenter, randomized, controlled trial.	2001 Jul 3	11435337
An economic evaluation of atenolol vs. captopril in patients with Type 2 diabetes (UKPDS 54).	2001 Jun	11472461
Relative efficacy of an angiotensin II antagonist compared with other antihypertensive agents. Olmesartan medoxomil versus antihypertensives.	2001 Jun	11451215
Pharmacoutilization of antihypertensive drugs: a model of analysis.	2001 Jun	11430633
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	11428662
Usefulness of the head-upright tilt test for distinguishing syncope and epilepsy in children.	2001 Jun	11422323
Cardioprotective effect of propranolol from alcohol-induced heart muscle damage as assessed by plasma cardiac troponin-t.	2001 Jun	11410725
Regression of left ventricular hypertrophy in human hypertension with irbesartan.	2001 Jun	11403367
Rationale, design, methods and baseline demography of participants of the Anglo-Scandinavian Cardiac Outcomes Trial. ASCOT investigators.	2001 Jun	11403364
Differential effects of nifedipine and co-amilozide on the progression of early carotid wall changes.	2001 Jun 19	11413085
[Panniculitis induced by MINE chemotherapy].	2001 Jun-Jul	11460041
The release of the substrate for xanthine oxidase in hypertensive patients was suppressed by angiotensin converting enzyme inhibitors and alpha1-blockers.	2001 Mar	11327632
Progressive intracranial vascular disease with strokes and seizures in a boy with progeria.	2001 Mar	11305689
Partition coefficients of beta-blockers in bile salt/lecithin micelles as a tool to assess the role of mixed micelles in gastrointestinal absorption.	2001 Mar 15	11321673
Smoothed pseudo Wigner-Ville distribution as an alternative to Fourier transform in rats.	2001 Mar 23	11476287
Nebivolol and airway responsiveness in the rabbit.	2001 Mar 23	11324721
[Concurrent long QT and Brugada syndrome in a single patient].	2001 May	11412758
Blood pressure, heart rate, and behavioral responses to psychological "novelty" stress in freely moving rats.	2001 May	11352138
beta(1)- and beta(2)-Adrenoceptor-mediated thermogenesis and lipid utilization in obese and lean men.	2001 May	11344226
Determination of the beta-blocker atenolol in plasma by capillary zone electrophoresis.	2001 May 4	11382304
Stereospecific pharmacokinetics and pharmacodynamics of beta-adrenergic blockers in humans.	2001 May-Aug	11466176
A prospective comparison of four antihypertensive agents in daily clinical practice.	2001 May-Jun	11430394

Patents

Sample Use Guides

In Vivo Use Guide

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

In Vitro Use Guide

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).

Name

Type

Language

ATENOLOL

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