Each Atehexal 25, 50, 100 film-coated tablet contains atenolol 25mg, 50mg
and 100mg respectively.
Atehexal is a β1-selective (cardioselective) adrenoceptor
blocking drug and acts by competitively blocking the adrenergic stimulation
within the myocardium and within vascular smooth muscle. At high doses (e.g.
greater than 100mg daily), the selectivity of Atehexal for
β1-adrenoceptors usually diminishes, resulting in competitive blocking
of β1- and β2-adrenoceptors. Peak plasma concentrations are reached in 2
to 4 hours.
Atehexal is preferred to non-selective β-blockers in patients with asthma or
diabetes mellitus. Because of low lipid solubility and limited penetration
into the brain, Atehexal has a lower incidence of CNS effects than seen with
propranolol. Atehexal crosses the placenta and is distributed into breast
milk where concentrations higher than those in maternal plasma have been
achieved. The plasma half-life is about 6 to 7 hours. Atehexal is eliminated
virtually entirely as unchanged drug in the urine and dosage needs to be
reduced in patients with moderate to severely impaired renal function (glomerular
filtration rate less then 30ml/min.).
Atehexal is indicated in the treatment of hypertension or chronic stable
Atehexal is contraindicated in patients:
• who are hypersensitive to any of its ingredients.
• with second or third degree heart block or uncontrolled heart failure.
• with metabolic acidosis
• with untreated phaeochromocytoma.
Side Effects / Adverse Reactions
The most common side effects are cold extremities, fatigue and diarrhoea.
Muscle fatigue may be marked during the first few weeks of treatment with
Atehexal, particularly in physically active patients; but after several
weeks it often improves or disappears. Vivid dreams or insomnia have
occasionally been reported.
Minor side effects may include gastrointestinal disturbances and dry mouth.
Elevations of transaminase levels have been seen infrequently while hepatic
toxicity including intrahepatic cholestasis has rarely been reported.
Despite Atehexal's high cardioselectivity, bronchospasm has been reported in
some patients and is more likely to occur when dosage of the drug exceeds
Rashes, visual disturbances and dryness of the eyes, though rare, have been
reported. Haematological reactions may include purpura and thrombocytopenia.
Neurological effect such as paraesthesia has been seen infrequently.
Precautions / Warnings
Atehexal should be used with caution in patients with inadequate cardiac
function, since congestive heart failure may be precipitated by blockage of
β-adrenergic stimulation when Atehexal therapy is administered. In addition
in patients with latent cardiac insufficiency, prolonged β-adrenergic
blockade may lead to cardiac failure. Although β-adrenergic blocking agents
should be avoided in patients with overt congestive heart failure, Atehexal
may be administered cautiously, if necessary, to patients with
well-compensated heart failure (e.g. those with cardiac glycosides and/or
diuretics). Patients receiving Atehexal therapy should be instructed to
consult their physician at the first sign or symptom of impending cardiac
and should be adequately treated (e.g. with a cardiac glycoside and/or
diuretic) and observed closely; if cardiac failure continues, Atehexal
should be discontinued gradually if possible.
Because of its high cardioselectivity, Atehexal may be used with caution in
patients with bronchospastic disease who do not respond to or cannot
tolerate other hypotensive agents. If Atehexal is used in such patients, the
initial dosage should be 50mg daily and the lowest dosage should be used. In
patients who develop symptoms of bronchospasm, Atehexal dosage should be
reduced or the drug discontinued (gradually if possible), and supportive
treatment administered. In patients with bronchospastic disease, concomitant
administration of a beta2-adrenergic agonist and/or twice daily dosing of
25mg may minimise the risk of bronchospasm.
Abrupt withdrawal of Atehexal may exacerbate angina symptoms and/or
precipitate myocardial infarction and ventricular arrhythmias in patients
with coronary artery disease, or may precipitate thyroid storm in patients
with thyrotoxicosis. Therefore, patients receiving Atehexal (especially
those with ischemic heart disease) should be warned not to interrupt or
discontinue therapy without consulting their physician. If exacerbation of
angina occurs or acute coronary insufficiency develops after Atehexal
therapy is interrupted or discontinued, treatment with the drug should be
reinstituted, at least temporarily.
Atehexal should be used with caution in patients with diabetes mellitus or
hyperthyroidism. The drug may mask the tachycardia associated with
hyperthyroidism or hypoglycaemia, but usually will not mask the dizziness
and sweating seen with hypoglycaemia.
Atehexal should be used with caution in patients undergoing major surgery
involving general anaesthesia. If Atehexal is discontinued, this should be
done two days before surgery. If patients continue to receive Atehexal prior
to surgery in which anaesthetics with negative inotropic activity are used,
the patients should be observed for signs and symptoms of heart failure. In
patients with impaired renal function, individualised dosage adjustment
should be based on renal function tests.
Patients receiving Atehexal after haemodialysis may develop severe
The safety and efficacy of atenolol in children have not been established.
There are no adequate and controlled studies to date using atenolol in
pregnant women and therefore, Atehexal should be used during pregnancy only
when the potential benefits justify the possible risks to the foetus.
Atenolol is distributed into breast milk, hence, caution should be exercised
when Atehexal is administered to a nursing woman.
Some reduction in dosage may be appropriate for the elderly since decreased
kidney function is a physiologic consequence of aging. Atenolol excretion
would be expected to decrease with advancing age.
Atehexal should be used with caution in patients with impaired renal
function since atenolol is excreted via the kidneys. Therefore, the dosage
should be adjusted in cases of severe impairment of renal function.
Treatment with Atehexal should not be discontinued abruptly. If treatment is
to be discontinued, dosage
of the drug should be reduced gradually over a period of about two weeks.