Tenormin Tablets Composition :
Tablets containing 25 mg, 50 mg or 100 mg of Atenolol Ph. Eur.
Injection for intravenous use presenled as an isotonic, citrate buffered, aqueous solution, oontaining 5 mg 01 Atenolol Ph.
Eur. in 10 ml.
Tenormin Tablets Therapeutic Indications :
i) Hypertension.
ii) Angina pectoris.
iii) Cardiac arrhythmias.
iv) Myocardial infarction. Early and late intervention.
Tenormin Tablets Posology and method of administration :
The dose must always be adjusted to individual requirements of the patients, with the lowest possible starting dosage. The following are guidelines.
Adults :
Hypertension
One tablet daily. Most patients respond to 100 mg daily given orally as a single dose. Some patients, however, will respond to 50 mg given as a single daily dose. The effect will be fully established after one to two weeks. A further reduction in blood pressure may be achieved by combining Tenormin with other antihypertensive agents. For example, administration of Tenormin with a diuretic, provides a highly effective and convenient antihypertensive therapy.
Angina
Most patients with angina pectoris will respond to 100 mg given orally once or 50 mg given twice daily. It is unlikely that additional benefit will be gained by increasing the dose.
Cardiac Arrhythmias
A suitable initial dose of Tenormin is 2.5 mg (5 ml) injected intravenously over a 2.5 minute period (i.e. 1 mg/minute). This may be repeated at 5 minute intervals until a response is observed, up to a maximum dosage of 10 mg. If Tenormin ts given by infusion, 0.15 mg/kg bodyweight may be administered over a 20 minute period. If required, the injection or infusion may be repeated every 12 hours. Having controlled the arrhythmias with intravenous Tenormin, a suitable oral maintenance dosage is 50- 100 mg daily, given as a single dose.
Myocardial Infarction
Early intervention after acute myocardial infarction: For patients suitable for treatment with intravenous beta-blockade and presenting within 12 hours of the onset of chest pain, Tenormin 5-10 mg should be given by slow intravenous injection (1 mg/minute) followed by Tenormin 50 mg orally about 15 minutes later, provided no untoward effects have occurred from the intravenous dose. This should be followed by a further 50 mg orally 12 hours after the intravenous dose and then 12 hours later by 100 mg orally, once daily. If bradycardia and/or hypotension requiring treatment, or any other untoward effects occur, Tenormin should be discontinued.
late intervention after acute myocardial infarction: For patients who present some days alter suffering an acute myocardial infarction an oral dose of Tenormin (100 mg daily) is recommended for long-term prophylaxis of myocardial infarction.
Elderty
Dosage requirements may be reduced, especially in patients with impaired renal function.
Children
There is no paediatric experience with Tenormin and for this reason it is not recommended for use in children.
Renal Failure Since Tenormin is excreted via the kidneys the dosage should be reduced in cases of severe impairment of renal function
Patients on haemodialysis should be given 50 mg orally after each dialysis; this should be done under hospital supervision as marked falls in blood pressure can occur.
Tenormin Tablets Contraindications :
Tenormin, as with other beta·blockers, should not be used in patients wrth any of the following: known hypersensitivity to the active substance, or any of the excipients; bradycardia «45bpm); cardiogenic shock; hypotension; metabolic acidosis; severe peripheral arterial Circulatory disturbances; second or third degree heart block; sick sinus syndrome; untreated phaeochromocytoma uncontrolled heart failure.
Tenormin Tablets Special warnings and precautions for use :
Tenormin as with other beta-blockers:
– should not be withdrawn abruptly. The dosage should be withdrawn gradually over a period of 7-14 days, to facilitate a reduction in beta-blocker dosage. Patients should be followed during withdrawal, especially those with ischaemic heart disease.
– when a patient is scheduled for surgery, and a decision is made to discontinue beta-blocker therapy, this should be done at least 24 hours prior to the procedure. The risk-benefit assessment of stopping beta-blockade should be made for each patient. if treatment is continued, an anaesthetic with little negative inotropic activity should be selected to minimise the risk of myocardial depression. The patient may be protected against vagal reactions by intravenous administration of atropine.
– although contraindications in uncontrolled heart failure may be used in patients whose signs of heart failure have been controlled. Caution must be exercised in patients whose cardiac reserve is poor.
– may increase the number and duration of angina attacks in patients with Prinzmetal’s angina due to unopposed alpha receptor mediated coronary artery vasoconstriction.
– although contraindicated in severe peripheral arterial circulatory disturbances (see Conlraindicalions), may also aggravate less severe peripheral arterial circulatory disturbances.
– due to M negative effect on conduction time, caution must be exercised if it is given to patients with first degree heart block.
– may mask the symptoms of hypoglycaemia, in particular, tachycardia.
– may mask the signs of thyrotoxicosis.
– will reduce heart rate, as a result of its pharmacological action. In the rare instances when a treated patient develop symptoms which may be attributable to a slow heart rate and the pulse rate drops to less than 50-55 bpm at rest, the dose should be reduced.
– may cause a more severe reaction to a variety of allergens, when given to patients with a history of anaphylactic reaction to such allergens. Such patients may be unresponsive to the usual doses of adrenaline used to treat the allergic reactions.
– may cause a hypersensitivity reaction including angioedema and urticaria.
– should be used with caution in the elderly, starting with a lesser dose (see Posology and method of administration). Since Tenormin is excreted via the kidneys, dosage should be reduced in patients with a creatinine clearance of below 35 ml /min/1.7 m2.
– although cardio selectiive (beta,) beta-blockers may have less effect on lung function than nonselectiive beta-bIockers, as with all, beta -blockers, these should be avoided in patients with reversible obstructive airways disease, unless there are compelling clinical reasons for their use. Where such reasons exist, Tenormin may be used with caution. 0ccasionally, some increase in airways resistance may occur in asthmatic patients, however, and this may usually be reversed by commonly used dosage of bronchodilators such as salbutamol or isoprenaline. As with other beta-blockers, in patients with a phaeochromocyphae, an alpha-blocker shoufd be given concomitantly.
Tenormin Tablets Interactions :
– Combined use of beta-blockers and calcium channel blockers with negative inotropic effects e.g. verapamil, diltiazem can lead to an exaggeration of these effects particularly in patients with impaired ventricular function and/or sino-atrial or atrioventricular conduction abnormalities. This may result in severe hypotension, bradycardia and cardiac failure. Neither the beta-blocker nor the calcium channel blocker should be administered intravintravenous within 48 hours of discontinuing the other.
– Digitalis glycosides, in association with beta-blockers, may increase atria-ventricular conduction time.
– Class I antiarrhythmic drugs (e.g. disopyramide) and amiodarone may have a potentiating effect on atrial conduction time and induce negative inotropic effect.
– Concomitant use of sympathomimetic agents, e.g. adrenaline, may counteract the effect of beta-blockers.
– Concomitant use with insulin and oral antidiabetic drugs may lead to the intensification of the blood sugar lowering effects of these drugs. Symptoms at hypoglycaemia, particularly tachycardia, may be masked (see Special warnings and precautions for use).
– Concomitant use of prostaglandin synthetase inhibiting drugs (e.g. ibuprofen, indomethacin), may decrease the hypotensive effects of beta-blockers.
– Caution must be exercised when using anaesthetic agents with Tenormin. The anaesthetist should be informed and the choice of anaesthetic should be an agent with as little negative inotropic activity as possible. Use of beta-blockers with anaesthetic drugs may result in atattenuation of the reflex tachycardia and increase the risk of hypotension. Anaesthetic agents causing myocardial depression are best avoided.
Tenormin Tablets Pregnancy and lactation :
tenormin crosses the placental barrier and appears in the cord blood no studies have been performed on the use of tenormin in the first trimester and the possibility of foetal cannot be excluded tenormin has been used under close supervision for the treatment of hypertension in the third trimester. Administration of Tenoonin to pregnant women in the management of mild to moderate hypertension has been associated with intrauterine growth retardation. The use of tenormin in women who are, or may become, pregnant requires that the anticipated benefit be weighed against the possible asks, particularly in the first and second trimesters, since beta-blockers, in general, have been associated with a decrease in placental perfusion which may result in intra-utrine deaths, immature and premature deliveries. There is significant accumulation of Tenormin in breast milk.
Neonates bom to mothers who are receiving Tenormin at parturition or breast-feeding may be at risk of hypoglycemia and bradycardia.
caution should be exercised when Tenoonin is administered dunng pregnancy or to a woman who is breast-feeding.
Tenormin Tablets Effect on ability to drive and use machines :
Use is unlikely to result in any impairment of the ability of patients to dove or operate machinery. However it should be taken into account that occasionally dizziness or fatigue may occur.
Tenormin Tablets Undesirable effects :
Tenormin is well tolerated. In clinical studies, the undesired events reported are usually attributable to the pharmacological actions of atenotol.
The following undesired events, listed by body system, have been reported with the following frequencies: Very common (” 10%), common (1- 9.9%), uncommon (0.1- 0.9%), rare (0.01- 0.09%), very rare « 0.01%) including isolated reports.
cardiac disorders:
Common: Bradycardia.
Rare: Heart failure deterioration, precipitation of heart block.
Vascular disorders:
Common: Cold extremities.
Rare: Postural hypotension which may be associated with syncope, intermittent claudication may be increased if already present, in susceptible patients Raynaud’s phenomenon.
Nervous system disorders:
Rare: Dizziness, headache, paraesthesia.
Psychiatric disorders:
Uncommon: Sleep disturbances of the type noted with other beta blockers.
Rare: Mood changes, nightmares, confusion, psychoses and hallucinations.
Gastrointestinal disorders :
Common: Gastrointestinal disturtlances.
Rare: Dry mouth.
Investigations :
Uncommon: Elevations of transaminase levels.
Very rare: An increase in ANA (Anti nuclear Antibodies) has been observed, however the cliniccl relevance of this is not clear.
Hepatobiliary disorders:
Rare: Hepatic toxicity including intrahepatic cholestasis
Blood and Iymphatic system disorders:
Rare: Purpura, thrombocytopenia.
Skin and subcutaneous tissue disorders:
Rare: Alopecia, psonasnonn skin reactions, exacertlation of psoriasis, skin rashes.
Not Known: hypersensitivity reactions, including angioedema and urtcaria,
Eye disorders:
Rare: Dry eyes, visual disturbances.
Reoroductive system and breast disorders:
Rare: Impotence.
Respiratory thoracic and mediastinal disorders:
Rare: Bronchospasm may occur in patients with bronchial asthma or a history of asthmatic complaints.
Tenormin Tablets Overdose :
The symptoms of over dosage may include bradycardia, hypotension, acute cardiac insufficiency and bronchospasm General treatment should include: close supervision, treatment in an intensive care ward, the use of gastric lavage, activated charcoal and a laxative to prevent absorption of any drug still present in the gastrointestinal tract, the use of plasma or plasma substitutes to treat hypotension and shock. The use of haemodialysis or haemoperfusion may be
considered. Excessive bradycardia can be countered with atropine 1-2 mg intravenously and/or a cardiac pacemaker. If necessary, this may be followed by a bolus dose of glucagon 10 mg intravenously. If required, this may be repeated or followed by an intravenous infusion of glucagon depending on response. If no response to glucagon occurs or it glucagon is unavailable, a beta-adrenoreceptor stimulant such as dobutamine 2.5 to 10 micrograms/kg/minute by intravenous infusion may be given. Dobutamine, because of its positive inotropic effect could also be used to treat hypotension and acute cardiac insufficiency. It is likely that these doses would be inadequate to reverse the cardiac effects of beta-blocker blockade it a large overdose has been taken. Bronchospasm can usually be reversed by bronchodilators.
Tenormin Tablets Pharmacodynamic properties :
Beta blocking agents, plain selective, C07A 803
Atenolol is a beta-blocker which is beta,-selective (i.e. acts preferentially on beta,-adrenergic receptors in the heart). Selectivity decreases with increasing dose. Atenolol is without intrinsic sympathomimetic and membrane stabilising activities and as with other beta-blockers, has negative inotropic effects (and is therefore contraindicated in uncontrolled heart failure). As with other beta-blockers, the mode of action of atenolol in the treatment of hypertension is unclear. It is probably the action of atenolol in reducing cardiac rate and contractility which makes it effective in eliminating or reducing the symptoms of patients with angina.
It is unlikely that any additional ancillary properties possessed by S (-) atenolol, in comparison with the racemic mixture, will give nse to different therapeutic effects. Tenormin is effective and well-tolerated in most ethnic populations although the response may be less in black patients. Tenormin is effective for at least 24 hours after a single oral dose. The drug facilitates compliance by its acceptability to patients and simplicity of dosing. The narrow dose range and early patient response ensure that the effect of the drug in individual patients is quickly demonstrated. Tenoonin is compatible with diuretics, other hypotensive agents and antianginal agents (see Interactions) Since it acts preferentially on beta-reoeprece in the heart, Tenormin may, with care, be used successfully in the treatment of patients with respiratory disease, who cannot tolerate non-selective beta-blockers. Early intervention with Tenormin in acute myocardial infarction reduces infarct size and decreases morbidity and mortality. Fewer patients with a threatened infarction progress to frank infarction; the incidence of ventricular arrhythmias is decreased and marked pain relief may result in reduced need of opiate analgesics. Early mortality is decreased. Tenormin is an additional treatment to standard coronary care.
Tenormin Tablets Pharmacokinetic properties :
Following intravenous administration, the blood levels of atenolol decay its exponentially with an elimination half-life of about 6 hours. Throughout the intravenous dose range of 5 – 1 0 mg the blood level profile obeys linear pharmacokinetics and beta-adrenoceptor blockade is still measurable 24 hours after a 10 mg intravenous dose. Absorption of atenotol following oral dosing is consistent but incomplete (approximately 40 – 50%) with peak plasma
concentrations occurring 2- 4 hours after dosing. The atenolol blood levels are consistent and subject to little variability. There is no significant hepatic metabolism of atenolol and more than 90% of that absorbed reaches the systemic circulation unaltered. The plasma half-life is about 6 hours but this may use in severe renal impairment since the kidney is the major route of elimination. Atenolol penetrates tissues poorly due to its low lipid solubility and its concentration in brain tissue is low. Plasma protein binding is low (approximately 3%).
Tenormin Tablets Incompatibillities :
Compatibility with intravenous infusion fluids
Tenormin Injection is compatible with sodium chloride intravenous infusion (0.9%w/v) and Glucose Intravenous Infusion BP (5%w/v).
Tenormin Tablets Special precautions for storage :
Tenormin Tablets: Do not store above 25’C. Protect from light and moisture.
Tenoonin Injection: Do not store above 25’C. Protect from light.
Tenormin Tablets Pack Size :
Please refer to the outer carton for pack size.
Tenormin Tablets PRODUCED BY :
AstraZeneca – Egypt
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Tenormin Tablets