Atenolol

(BAN, USAN, rINN)
Atenolol Chemical formula
Synonyms: Aténolol; Atenololi; Atenololis; Atenololum; ICI-66082. 2-{p-[2Hydroxy-3-(isopropylamino)propoxy]phenyl}acetamide.
Cyrillic synonym: Атенолол.

💊 Chemical information

Chemical formula: C14H22N2O3 = 266.3.
CAS — 29122-68-7; 60966-51-0.
ATC — C07AB03.
ATC Vet — QC07AB03.

Pharmacopoeias.

In Chin., Eur., Int., Jpn, and US.

Ph. Eur. 6.2

(Atenolol). A white or almost white powder. Sparingly soluble in water; soluble in dehydrated alcohol; slightly soluble in dichloromethane.

USP 31

(Atenolol). White or practically white, odourless powder. Slightly soluble in water and in isopropyl alcohol; sparingly soluble in alcohol; freely soluble in methyl alcohol.

💊 Adverse Effects, Treatment, and Precautions

As for Beta Blockers.

Breast feeding.

Atenolol is distributed into breast milk and there has been a report of cyanosis and bradycardia in a breastfed neonate whose mother had been taking atenolol (see under Pharmacokinetics, below). The American Academy of Pediatrics therefore considers1 that it should be given with caution to breast-feeding mothers.
1. American Academy of Pediatrics. The transfer of drugs and other chemicals into human milk. Pediatrics 2001; 108: 776–89. Correction. ibid.; 1029. Also available at: http://aappolicy.aappublications.org/cgi/content/full/ pediatrics%3b108/3/776 (accessed 10/01/08)

Effects on the eyes.

Visual symptoms without headache were associated with atenolol for migraine prophylaxis in a patient who had experienced a similar reaction with nadolol.1
1. Kumar KL, Cooney TG. Visual symptoms after atenolol therapy for migraine. Ann Intern Med 1990; 112: 712–13. Correction. ibid.; 113: 257.

Effects on the heart.

Beta blockers are used in the management of cardiac arrhythmias. However, atenolol 2.5 mg by intravenous injection induced atrial fibrillation in 6 of 12 predisposed patients.1
1. Rassmussen K, et al. Atrial fibrillation induced by atenolol. Eur Heart J 1982; 3: 276–81.

Effects on lipid metabolism.

For a report of acute pancreatitis due to hypertriglyceridaemia in a patient taking atenolol and metoprolol.

Effects on the liver.

Adverse hepatic reactions in patients receiving atenolol have included reversible cholestatic hepatitis in one1 and hepatic dysfunction in another.2
1. Schwartz MS, et al. Atenolol-associated cholestasis. Am J Gastroenterol 1989; 84: 1084–6
2. Yusuf SW, Mishra RM. Hepatic dysfunction associated with atenolol. Lancet 1995; 346: 192.

Overdosage.

Atenolol appears to lack membrane-stabilising activity and may have fewer adverse cardiac effects than some other beta blockers. However, cardiovascular toxicity has been noted after massive overdosage: ventricular asystole1 and hypotension with ECG abnormalities2 have been reported. Severe cardiovascular effects also occurred3 in a patient with mixed overdosage including atenolol and diltiazem, and were attributed to additive toxicity.
1. Stinson J, et al. Ventricular asystole and overdose with atenolol. BMJ 1992; 305: 693
2. Love JN, Elshami J. Cardiovascular depression resulting from atenolol intoxication. Eur J Emerg Med 2002; 9: 111–14
3. Snook CP, et al. Severe atenolol and diltiazem overdose. J Toxicol Clin Toxicol 2000; 38: 661–5.

💊 Pharmacokinetics

About 50% of an oral dose of atenolol is absorbed. Peak plasma concentrations are reached in 2 to 4 hours. Atenolol has low lipid solubility. It crosses the placenta and is distributed into breast milk where concentrations higher than those in maternal plasma have been achieved. Only small amounts are reported to cross the blood-brain barrier, and plasma-protein binding is minimal. The plasma half-life is about 6 to 7 hours. Atenolol undergoes little or no hepatic metabolism and is excreted mainly in the urine. It is removed by haemodialysis.

Breast feeding.

Atenolol diffuses into breast milk in concentrations similar1 to or higher2 than those in maternal blood. Cyanosis and bradycardia associated with ingestion of atenolol in breast milk has been reported in a 5-day-old term infant. The baby improved when breast feeding was stopped.3
1. Thorley KJ, McAinsh J. Levels of the beta-blockers atenolol and propranolol in the breast milk of women treated for hypertension in pregnancy. Biopharm Drug Dispos 1983; 4: 299–301
2. White WB, et al. Atenolol in human plasma and breast milk. Obstet Gynecol 1984; 63: 42S–44S
3. Schimmel MS, et al. Toxic effects of atenolol consumed during breast feeding. J Pediatr 1989; 114: 476–8.

Pregnancy.

Creatinine clearance increases during pregnancy, and a study in 17 pregnant patients found that the elimination half-life was shorter and renal clearance of atenolol faster during the second and third trimesters compared with three months post partum.1 In another study,2 postpartum samples were taken from the maternal and umbilical serum of 6 women who had been taking atenolol for at least 6 days before delivery; atenolol was detected in both maternal and cord blood in about equal concentrations. Atenolol was not detected in the maternal or cord blood of another patient who had stopped taking atenolol one day before delivery; the authors concluded that atenolol levels in the mother and fetus are equal at steady state, and that fetal accumulation does not occur. Atenolol concentrations in 35 term neonates whose mothers had received atenolol were examined.3 It was found that the elimination rate for the neonates was 4 times slower than in adults, possibly because of immaturity of renal function. Transient bradycardia developed in 14 neonates.
1. Hebert MF, et al. Pharmacokinetics and pharmacodynamics of atenolol during pregnancy and postpartum. J Clin Pharmacol 2005; 45: 25–33
2. Melander A, et al. Transplacental passage of atenolol in man. Eur J Clin Pharmacol 1978; 14: 93–4
3. Rubin PC, et al. Atenolol elimination in the neonate. Br J Clin Pharmacol 1983; 16: 659–62.

💊 Uses and Administration

Atenolol is a cardioselective beta blocker. It is reported to lack intrinsic sympathomimetic activity and membrane-stabilising properties. Atenolol is used in the management of hypertension, angina pectoris, cardiac arrhythmias, and myocardial infarction. It may also be used for the prophylaxis of migraine. In hypertension atenolol is given orally in a dose of 50 to 100 mg daily, as a single dose, although 50 mg daily is generally adequate. The full effect is usually evident within 1 to 2 weeks. The usual dose for angina pectoris is 50 to 100 mg daily orally, given as a single dose or in divided doses. Additional benefit is not usually obtained from higher doses of atenolol although up to 200 mg daily has been given. For the emergency treatment of cardiac arrhythmias atenolol may be given by intravenous injection in a dose of 2.5 mg injected at a rate of 1 mg/minute, repeated if necessary every 5 minutes to a maximum total dosage of 10 mg. Alternatively atenolol may be given by intravenous infusion over 20 minutes in a dose of 150 micrograms/kg. The injection or infusion procedure may be repeated every 12 hours if necessary. When control is achieved maintenance oral doses of 50 to 100 mg daily may be given. Atenolol is also used in the early management of acute myocardial infarction. Treatment should be given within 12 hours of the onset of chest pain; atenolol 5 to 10 mg should be given by slow intravenous injection at a rate of 1 mg/minute, followed after 15 minutes with 50 mg orally, provided no adverse effects result from the injection; alternatively an intravenous dose of 5 mg may be repeated after 10 minutes followed by an oral dose of 50 mg after a further 10 minutes. A further 50 mg may be given orally after 12 hours, and subsequent dosage maintained, after a further 12 hours, with 100 mg daily. In the prophylaxis of migraine an oral dose of 50 to 100 mg daily has been used. Reduced doses may be required in patients with impaired renal function (see below).

Administration in renal impairment.

The dose of atenolol should be reduced in patients with renal impairment, depending on the creatinine clearance (CC) as follows:
CC 15 to 35 mL/minute per 1.73 m2: 50 mg daily orally or 10 mg once every two days intravenously
CC less than 15 mL/minute per 1.73 m2: 25 mg daily or 50 mg on alternate days orally or 10 mg once every four days intravenously
dialysis patients: 25 to 50 mg orally after each dialysis.

💊 Preparations

BP 2008: Atenolol Injection; Atenolol Oral Solution; Atenolol Tablets; Cotenidone Tablets; USP 31: Atenolol and Chlorthalidone Tablets; Atenolol Injection; Atenolol Oral Solution; Atenolol Tablets.

Proprietary Preparations

Arg.: Atel; Atenoblock; Atenovit; Cardioblock; Corpaz; Fabotenol; Felobits; Ilaten; Myocord; Plenacor; Prenormine; Telvodin; Tensilol; Tozolden; Vericordin; Austral.: Anselol; Atehexal; Noten; Tenormin; Tensig; Austria: Arcablock; Atehexal; Atenolan; Atenotyrol†; Betasyn; Tenormin; Belg.: Atenotop; Athenol†; Docateno; Tenormin; Braz.: Ablok; Angipress; Atecard; Atenegran; Ateneo; Atenobal; Atenokin; Atenol; Atenolab; Atenopress†; Atenorm; Atenuol; Atepress; Biotenor†; Ditenol†; Neotenol†; Plenacor; Sifnolol†; Canad.: Apo-Atenol; Novo-Atenol; Nu-Atenol; Tenolin†; Tenormin; Chile: Betacar; Grifotenol; Labotensil; Tenormin†; Cz.: Apo-Atenol; Ateblocor†; Atehexal; Atenobene; Catenol†; Corotenol†; Tenormin; Denm.: Atenet; Atenodan; Atenor; Tenormin; Uniloc; Fin.: Atenblock; Atenol; Tenoblock; Tenoprin; Fr.: Betatop; Tenormine; Ger.: Ate Lich; Ate†; Atebeta; Atehexal; Atendol†; Ateno; Atenogamma; Blocotenol†; Cuxanorm; duratenol†; Evitocor†; Falitonsin†; Jenatenol; Juvental; Tenormin; Gr.: Adenamin; Azectol; Blocotenol; Estanolin†; Fealin; Galol†; Hemon†; Mesonex; Mezarid†; Neocardon; Silder†; Synarome; Tenormin; Tradiver†; Umoder; Hong Kong: Adoll; Antipressan; Apo-Atenol; Ateno†; CP-Atenol; Hypernol; Lo-Ten; Martenol; Normaten; Nortelol; Oraday; Tenormin; Ternolol; Tredol; Vascoten; Velorin; Hung.: Atenobene; Atenomel; Blokium; Huma-Atenol†; Prinorm; India: Atecard†; Aten; Beta; Beten; Cadpres; Hipres; Lonol; Teno; Tenolol; Tenormin; Tensimin†; Indon.: Betablok; Farnormin; Hiblok; Internolol; Tenblok; Tenormin; Tensinorm; Zumablok; Irl.: Amolin; Atecor; Ateni; Atenogen; Atenomel; Tenormin; Trantalol; Israel: Normalol; Normiten; Ital.: Atenol; Atermin; Seles Beta; Tenomax; Tenormin; Malaysia: Apo-Atenol; Beten; Corotenol†; Loten; Normaten†; Noten; Oraday†; Ranlol; Renotol†; Tenormin; Ternolol†; Uphanormin†; Urosin; Vascoten; Mex.: Atenol; Atoken; Biofilen; Blotex; Min-T; Nosbal; Tenormin; Trebanol; Neth.: Te n o r m i n ; Norw.: Alinor†; Tenormin; Uniloc; NZ: Anselol†; Lo-Ten; Philipp.: Atestad; Cardioten; Durabeta; Tenor-Bloc; Tenormin; Tenostat; Tensimin; Therabloc; Velorin; Pol.: Normocard; Port.: Ancoren†; Atenolac†; Blokium†; Tenormin; Tessifol; Rus.: Atenolan (Атенолан); Betacard (Бетакард); Catenol (Катенол); Hypoten (Хайпотен); Tenolol (Тенолол); S.Afr.: Atenoblok; B-Vasc†; Hexa-Blok; Ten-Bloka; Tenormin; Venapulse; Singapore: Alonet†; Apo-Atenol; Hypernol; Normaten; Noten; Prenolol; Tenolol; Tenormin; Ternolol†; Vascoten; Velorin†; Spain: Blokium; Neatenol; Tanser; Tenormin; Swed.: Selinol†; Tenormin; Uniloc†; Switz.: Atenil; ateno-basan†; Atesifar†; Cardaxen; Primatenol†; Selobloc; Tenormin; Thai.: Atcard; Atenol; Coratol; Nolol; Nortelol; Oraday; Preloc; Prenolol; Tenocor; Tenol; Tenolol; Tenormin; Tetalin; Vascoten; Velorin; Turk.: Nortan; Tensidif; Tensinor; UAE: Te n s o t i n ; UK: Antipressan; Atenix; Tenormin; USA: Te n o r m i n ; Venez.: Artenolol†; Atenoval†; Beloc; Blokium; Ritmilan; Tenormin. Multi-ingredient: Arg.: Atel C†; Atel N†; Plenacor D; Prenomod†; Prenoretic; Vericordin Compuesto; Austria: Arcablock comp; Atenolan comp; Atenolol comp; Atenotyrol comp†; Beta-Adalat; Nif-Ten; Polinorm; Tenoretic; Belg.: Beta-Adalat†; Kalten†; Tenif; Tenoretic; Braz.: Ablok Plus; Angipress CD; Atenoclor†; Atenoric; Atenuol CRT; Betalor; Nifelat; Tenoretic; Canad.: Apo-Atenidone; Tenoretic; Chile: Tenoretic†; Cz.: Atedon†; Atenolol Compositum†; Tenoretic; Denm.: Tenidon; Tenoretic; Fin.: Nif-Ten; Fr.: Beta-Adalate; Tenordate; Tenoretic; Ger.: Ate Lich comp; Atehexal comp; Atel; AteNif beta; Ateno comp; Atenogamma comp; Atenolol AL comp; Atenolol comp; Blocotenol comp†; Bresben; Diu-Atenolol; duratenol comp†; Nif-Ten; Nifatenol; Sigabloc†; Teneretic; TRI-Normin; Gr.: Apress†; Chlotenor; Obosan; Tenoretic; Typofen; Hong Kong: NifTen ; Tar g e t ; Te no re t; Te n o r e t i c ; Hung.: Atenolol Comp†; Blokium Diu; India: Amdepin-AT; Amlopres AT; Amlosafe-AT†; Amlostat-AT; AtecardD†; Beta Nicardia†; Cardif Beta; Cardules Plus; Depten; Hipres-D; LerezAT†; Nifetolol; Presolar; Tenochek; Tenoclor; Tenofed; Tenolol-AM; Tenolol-D†; Tenoric; Indon.: Nif-Ten; Tenoret; Tenoretic; Irl.: Atecor CT; Atenetic; Beta-Adalat; Nif-Ten; Tenoret; Tenoretic; Ital.: Atenigron; Atinorm; Carmian; Clortanol; Diube; Eupres; Igroseles; Mixer; Nif-Ten; Nor-Pa; Normopress; Target; Tenolone†; Tenoretic; Malaysia: Apo-Atenidone; Preteno l C ; Tar ge t; Te n o r e t ; Te n or et ic ; Mex.: Plenacor; Tenoretic; Neth.: NifTen†; Tenoretic; Philipp.: Ni f-Te n; Te n ore tic ; Port.: Blokium Diu†; Tenoretic; Rus.: Atehexal Compositum (Атегексал Композитум); Tenochek (Теночек); Tenoric (Тенорик); Tenorox (Тенорокс); S.Afr.: Adco-Loten; Atenoblok Co†; Tenchlor; Tenoretic; Singapore: Beta Nicardia; Nif-Ten; Nifetex; Tenoret; Tenoretic; Spain: Blokium Diu; Kalten; Neatenol Diu; Neatenol Diuvas; Normopresil; Tenoretic; Switz.: Atedurex; ateno-basan comp†; Beta-Adalat; Cardaxen plus; Co-Atenolol†; Cotenolol-Neo; Cotesifar†; Kalten; Nif-Atenil; Nif-Ten; Primatenol Plus†; Tenoretic; Thai.: Te n oret†; Tenoretic†; Turk.: Tenoretic; UK: AtenixCo; Beta-Adalat; Kalten; Tenchlor; Tenif; Tenoret; Tenoretic; Totaretic; USA: Tenoretic; Venez.: Blokiuret; Tenoretic.
Published December 04, 2018.