Atenolol Tablets Bp 100mg
Out of date information, search anotherSUMMARY OF PRODUCT CHARACTERISTICS
1 NAME OF THE MEDICINAL PRODUCT
Atenolol Tablets BP 100mg.
2. QUALITATIVE AND QUANTITATIVE COMPOSITION
Each tablet contains atenolol BP 100mg.
3. PHARMACEUTICAL FORM
Film-coated tablet.
4. CLINICAL PARTICULARS
4.1 Therapeutic indications
i) Management of hypertension.
ii) Management of angina pectoris.
iii) Oral maintenance management of cardiac dysrhythmias.
iv) Early intervention in the acute phase of myocardial infarction.
4.2 Posology and method of administration
The lowest possible dosage should be given at the start of treatment in case of cardiac decompensation or bronchial phenomena. This is especially important when treating elderly patients. If the dose needs to be increased, this should be done slowly (eg once a week) under control or on the basis of clinical effect.
Adults:
Hypertension: 1 tablet daily. Most patients respond to 100mg daily given orally as a single dose. Some patients, however, will respond to 50mg given as a single daily dose. The effect will be fully established after 1 or 2 weeks. A further reduction in blood pressure may be achieved by combining atenolol with other anti-hypertensive agents.
Angina: Most patients with angina pectoris will respond to 100mg given orally once daily or 50mg given twice daily. It is unlikely that additional benefit will be gained by increasing the dose.
Dysrhythmias: Following control of the dysrhythmias with intravenous atenolol a single daily oral maintenance dose of 50mg or 100mg may be given.
Myocardial infarction: For patients suitable for treatment with intravenous beta-blockade and presenting within 12 hours of the onset of the chest pain, atenolol 5mg to 10mg should be given by slow intravenous injection (1mg/minute) followed by atenolol 50mg orally about 15 minutes later provided no untoward effects occur from the intravenous dose. This should be followed by a further 50mg orally 12 hours after the intravenous dose and then 12 hours later by 100mg orally to be given once daily. If bradycardia and/or hypotension requiring treatment, or any other untoward effects occur, atenolol should be discontinued.
Elderly patients or patients with impaired renal function:
Dosage requirements may be reduced, especially in patients with impaired renal function.
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For patients with a creatinine clearance of 15ml to 35ml/minute/1.73m (equivalent to serum creatinine of 300 to 600 micromol/litre) the oral dose should be 50mg daily. For patients with a creatinine clearance of less than 15ml/minute/1.73m (equivalent to serum creatinine of greater than 600 micromol/litre) the oral dose should be 50mg on alternate days. Patients on haemodialysis should be given 50mg orally after each dialysis, this should be given under hospital supervision as marked falls in blood pressure can occur.
Children:
There is no paediatric experience with atenolol and for this reason it is not recommended for use in children.
Method of administration: Oral.
4.3 Contraindications
Atenolol is contra-indicated in patients with:
• hypersensitivity to atenolol or any of the other ingredients
• a history of bronchospasm or asthma
• bradycardia
• second or third degree heart block
• sick sinus syndrome
• cardiogenic shock
• uncontrolled heart failure
• hypotension
• severe peripheral arterial disease
• Prinzmetal’s angina
• untreated phaeochromocytoma
• prolonged fasting, or prone to hypoglycaemia
• metabolic acidosis.
4.4 Special warnings and precautions for use
Especially in patients with ischaemic heart disease, treatment should not be discontinued suddenly. The dosage should gradually be reduced, i.e. over 1 to 2 weeks, if necessary at the same time initiating replacement therapy, to prevent exacerbation of angina pectoris.
In addition, hypertension and arrhythmias may develop. When it has been decided to interrupt a beta-blockade in preparation for surgery, therapy should be discontinued for at least 24 hours. Continuation of beta-blockade reduces the risk of arrhythmias during induction and intubation, however the risk of hypotension may be increased as well. If treatment is continued, caution should be observed with the use of certain anaesthetic drugs. The patient may be protected against vagal reactions by intravenous administration of atropine.
In patients with peripheral circulatory disorders (Raynaud’s disease or syndrome, intermittent claudication), beta-blockers should be used with great caution as aggravation of these disorders may occur.
Special care should be taken in patients whose cardiac reserve is poor.
Beta-blockers should not be used in patients with untreated congestive heart failure. This condition should first be stabilised.
Patients with a history of wheezing or asthma should not take atenolol, unless it is considered essential. The label will carry the following warning: “Do not take this medicine if you have a history of wheezing or asthma.”. The Patient Information Leaflet will state “Do not take this medicine if you have a history of wheezing or asthma. Consult your doctor or pharmacist first.”.
The side effects of Beta-blockers may induce bradycardia. If the pulse rate decreases to less than 50 to 55 beats per minute at rest and the patient experiences symptoms related to the bradycardia, the dosage should be reduced.
In patients with chronic obstructive pulmonary disorders, airway obstructions may be aggravated. Beta1 selective blockers such as atenolol should be
administered only with utmost care.
Due to its negative effect on conduction time, beta-blockers should only be given with caution to patients with first degree heart block.
Patients with kidney insufficiency need a lower dosage, please refer to section
4.2 Posology and method of administration.
The elderly should be treated cautiously, starting with a lower dosage but tolerance is usually good.
Beta-blockers may increase the number and the duration of anginal attacks in patients with Prinzmetal’s angina due to unopposed alpha-receptor mediated coronary artery vasoconstriction. Atenolol should only be used with the utmost care.
Patients with a history of psoriasis should take beta-blockers only after careful consideration.
Beta-blockers may increase both the sensitivity towards allergens and the seriousness of anaphylactic reactions, they also may make patients less responsive to doses of adrenaline used to treat the allergic reactions.
Atenolol should be used with caution in those with, or a history of, myasthenia gravis.
4.5 Interactions with other medicinal products and other forms of interaction Not recommended association:
It is not recommended that atenolol be taken with:
- Calcium antagonists: verapamil and to a lesser extent diltiazem: negative influence on cardiac contractility and auriculo-ventricular conduction.
- Digitalis glycosides: association with beta-blockers may increase auriculo-ventricular conduction time.
- Monoamine oxidase (MAO) inhibitors: atenolol should not be taken with MAO inhibitors with the exception of MAO-B inhibitors.
- Sympathomimics - Adrenaline (ephedrine) / Noraderenaline (norepinephrine): may cause sever hypotersion. Xamoterol: reduction in beta-blockade.
- Moxisylyte (thymoxamine): Possible sever postural hypotension
- Analgesics: NSAIDS antagonise hypotensive effect.
Precautions for use:
Care should be taken if atenolol is taken with:
- Clonidine: caution should be exercised when transferring patients from clonidine to beta-adrenoceptor blocking drugs. If beta-adrenoceptor blocking drugs and clonidine are given concurrently, clonidine should not be discontinued until several days after the withdrawal of the beta-adrenoceptor blocking drug.
- Verapamil: beta-adrenoceptor blocking drugs should be used with caution in combination with verapamil in patients with impaired ventricular function. The combination should not be given to patients with conduction abnormalities. Neither drug should be administered intravenously within 48 hours of discontinuing the other.
- Class 1 anti-arrhythmic drugs such as disopyramide, quinidine or amiodarone: may have potentiating effect on atrial-conduction time and induce negative inotropic effect. This means there is an increased risk of myocardial depression and bradycardia
- Insulin and oral anti-diabetic drugs: may intensify the blood sugar lowering effect. Use of beta-blockers may mask the signs of hypoglycaemia e.g. tachycardia. It may even cause hypoglycaemia in non-diabetic patients e.g. neonates, infants, children, elderly patients, patients on haemodialysis or patients suffering from chronic liver disease and patients suffering from overdose. It has rarely caused seizures and/or coma in isolated patients. Caution should be exercised in the concurrent use of atenolol therapy in diabetic patients as it may prolong the hypoglycaemic response to insulin.
- Anaesthetic agents: may attenuate reflex tachycardia and increase the risk of hypotension. However, continuation of beta-blockades reduces the risk of arrhythmia during induction and intubation. The anaesthetist should be informed that the patient is taking atenolol. Anaesthetic agents causing myocardial depression, such as cyclopropane and trichlorethylene should be avoided.
- Cimetidine, hydralazine or alcohol: induce increased plasma levels of hepatically metabolised beta-blockers.
- ACE inhibitors and Angiotensin-II Antagonists: taken at the same time as propranolol may result in enhanced hypotensive effects. Aldesleukin andAlprostadil: also have this effect.
- Anti-arrhythmics: Increased risk of myocardial depression and
bradycardia.
- Antimalarials: increased risk of bradycardia with mefloquine.
- Tropisetron: risk of ventricular arrhythmias - manufacturer of tropisteron advises caution.
Take into account:
- Calcium antagonists: dihydropyridine derivates such as nifedipine: the risk of hypotension may be increased. In patients with latent cardiac insufficiency, treatment with beta-blocking agents may lead to cardiac failure.
- Prostaglandin synthetase inhibiting drugs: may decrease the hypotensive effects of beta-blockers.
- Sympathicomimetic agents: may counteract the effect of beta-adrenergic blocking agents.
- Tricyclic antidepressants, barbiturates, phenothiazides or other antihypertensive agents: taken at the same time as atenolol may increase the blood pressure lowering effect.
- Parasympathomimetics: risk of arrhythmias possibly increased by
pilocarpine.
- Anxiolytics and Hypnotics: enhanced hypotensive effect.
- Corticosteroids: antagonism of hypotensive effect.
- Diuretics: enhanced hypotensive effect.
- Ergotamine and Ergometrine: increased perhiperal vasoconstriction.
- Oestrogen and Progestrogens: oestrogen and combined oral contraceptives antagonise hypotensive effect.
- Xamoterol: antagonism of effect of xamoterol and reduction of beta-
blockade.
4.6 Pregnancy and lactation
The use of atenolol is not recommended during pregnancy or lactation.
Beta-blockers reduce placental perfusion, which may result in intrauterine foetal death, immature and premature deliveries. In addition, adverse effects (especially hypoglycaemia and bradycardia) may occur in foetus and neonate. There is an increased risk of cardiac and pulmonary complications in the neonate in the postnatal period.
Most beta-blockers, particularly lipophilic compounds, will pass into breast milk although to a variable extent.
4.7 Effects on ability to drive and use machines
There are no studies on the effect of this medicine on the ability to drive. When driving vehicles or operating machines it should be taken into account that occasionally dizziness or fatigue may occur.
4.8 Undesirable effects
The following undesirable effects may occur:
- Bradycardia, a slowed AV-conduction or increase of an existing AV-block, hypotension, heart failure, cold and cyanotic extremities, Raynaud’s phenomenon, paraesthesia of the extremities, increase of an existing intermittent claudication.
- Fatigue, headaches, impaired vision, hallucinations, psychoses, confusion, impotence, dizziness, sleep disturbances, depression, nightmares.
- Gastro-intestinal problems, nausea, vomiting, diarrhoea.
- Bronchospasm in patients with bronchial asthma or a history of asthmatic complaints. Disorder of the skin, especially rash. Dry eyes.
- Beta-blockers may mask the symptoms of thyrotoxicosis or
hypoglycaemia.
- An increase in anti nuclear antibodies (ANA) has been seen; its clinical relevance is not clear.
4.9 Overdose
Symptoms of overdosage are: bradycardia, hypotension, bronchospasm and acute cardiac insufficiency.
After ingestion of an overdose or in case of hypersensitivity, the patient should be kept under close supervision and be treated in an intensive-care ward. Absorption of any drug material still present in the gastro-intestinal tract can be prevented by gastric lavage, administration of activated charcoal and a laxative. Artificial respiration may be required. Bradycardia or extensive vagal reactions should be treated by administering atropine or methylatropine. Hypotension and shock should be treated with plasma/plasma substitutes and, if necessary, catecholamines. The beta-blocking effect can be counteracted by slow intravenous administration of isoprenaline hydrochloride, starting with a dose of approximately 5 micrograms/minute, or dobutamine, starting with a dose of approximately 2.5 micrograms/minute, until the required effect has been obtained. In refractory cases isoprenaline can be combined with dopamine. If this does not produce the desired effect either, intravenous administration of 8 to 10mg glucagon may be considered. If required the injection should be repeated within one hour, to be followed, if required, by an intravenous infusion of glucagon at an administration rate of 1mg to 3mg/hour. Administration of calcium ions, or the use of a cardiac pacemaker may also be considered. In patients intoxicated with hydrophilic beta-blocking agents haemodialysis or haemoperfusion may be considered.
5. PHARMACOLOGICAL PROPERTIES
5.1 Pharmacodynamic properties
Atenolol is a ^-selective adrenergic receptor antagonist. The betai receptor selectivity is likely to cause fewer side-effects due to bronchial beta2 receptor blockade. It should be taken into account that selectivity decreases with increasing dosages.
5.2 Pharmacokinetic properties
After oral administration, only approximately 50% atenolol is absorbed from the gastro-intestinal tract due to low lipid solubility. Plasma protein binding is less than 5%. Peak plasma concentrations occur in 2 to 4 hours. Small amounts cross the blood-brain barrier and atenolol crosses the placenta and is present in breast-milk. The plasma half life is between 6 and 8 hours. No significant hepatic metabolism of atenolol occurs. It is excreted via the kidneys in the urine.
5.3 Preclinical safety data
There are no preclinical safety data of relevance to the prescriber.
6. PHARMACEUTICAL PARTICULARS
6.1 List of excipients
Microcrystalline cellulose, lactose, sodium starch glycollate, magnesium stearate, sodium lauryl sulphate, colloidal silicon dioxide, hydroxypropyl methylcellulose, ethylcellulose 45, diethylphthalate and Opaspray orange K-1-2433 which contains E171 and E110.
6.2 Incompatibilities
Not known.
6.3 Shelf life
24 months.
6.4 Special precautions for storage
Store in a cool, dry place and protect from light.
6.5 Nature and contents of container
i) Securitainer with polyethylene closures.
Pack sizes: 50, 100, 250, 500 and 1,000.
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ii) Blister packs with the following composition: 250pm PVC coated with 60g/m PVDC 20pm aluminium foil.
Pack sizes: 28, 30, 56 and 60.
6.6 Instructions for use/handling
Not applicable.
7 MARKETING AUTHORISATION HOLDER
Sandoz Ltd Woolmer Way Bordon Hampshire GU35 9QE
8 MARKETING AUTHORISATION NUMBER(S)
PL 04416/0163
9. DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
14 October 1993
10. DATE OF REVISION OF TEXT
January 2004