Lokren is a drug with hypotensive, antianginal action.
Release form and composition
Lokren is produced in the form of film-coated tablets: round, biconvex, white in color, with a risk on one side and the inscription “KE 20” on the other (14 pieces in blisters, 2 blisters in a cardboard box).
The composition of 1 tablet includes:
- Active substance: betaxolol - 20 mg (in the form of hydrochloride);
- Auxiliary components: colloidal silicon dioxide - 1.6 mg; lactose monohydrate - 100 mg; sodium carboxymethyl starch (type A) - 4 mg; microcrystalline cellulose - 113 mg; magnesium stearate - 1.4 mg.
The composition of the film shell: macrogol 400 - 0.43 mg; hypromellose - 3.9 mg; Titanium dioxide (E171) - 0.67 mg.
Indications for use
Lokren is used as monotherapy or simultaneously with other drugs for the following diseases:
- Arterial hypertension;
- Attacks of angina pectoris (prevention).
- Acute heart failure, chronic heart failure in the stage of decompensation, not compensated for by treatment with inotropic drugs, diuretics, angiotensin-converting enzyme inhibitors and other vasodilators;
- Printsmetal angina (use as monotherapy is contraindicated);
- Chronic obstructive pulmonary disease and bronchial asthma (in severe forms);
- Sick sinus syndrome, including sinoatrial blockade;
- Metabolic acidosis;
- Cardiogenic shock;
- Phaeochromocytoma without simultaneous administration with alpha-blockers;
- AV block II and III degree (without an installed artificial pacemaker);
- History of anaphylactic reactions;
- Severe forms of Raynaud's disease and peripheral arterial disease obliterans;
- Severe bradycardia (heart rate less than 45-50 beats per minute);
- Arterial hypotension (systolic pressure less than 100 mm Hg. Art.);
- Cardiomegaly (without signs of heart failure);
- Lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
- Simultaneous use with flaktafenin, a sultoprid, monoamine oxidase inhibitors;
- Age up to 18 years (the efficacy and safety of Lokren in this age group of patients have not been established);
- Hypersensitivity to the drug.
Pregnant women can receive Locrien only in cases when the health benefits of the mother are higher than the potential risk to the fetus. During lactation at the time of use of the drug, breastfeeding should be interrupted.
Lokren should be taken with caution in the presence of the following diseases:
- Chronic heart failure in the stage of compensation (the drug is prescribed in very small initial doses with their gradual increase, only under strict medical supervision);
- Chronic obstructive pulmonary disease and moderate-course bronchial asthma (therapy begins with small doses, preferably by monitoring indicators of respiratory function);
- AV degree I blockade (careful monitoring is necessary, including ECG control);
- Prinzmetal angina pectoris (due to a possible increase in angina pectoris attacks; Locri can be used only simultaneously with vasodilators);
- Raynaud's syndrome (except for the severe form), obliterating diseases of the peripheral arteries (due to a possible increase in peripheral circulatory disorders);
- Treated pheochromocytoma (careful monitoring of blood pressure indicators is necessary);
- Hepatic insufficiency (at the beginning of therapy requires more careful clinical observation);
- Renal failure (when creatinine clearance is more than 20 ml per minute - during the first 4 days of treatment, careful monitoring of the patient is necessary; when creatinine clearance is less than 20 ml per minute and / or during hemodialysis, correction of the dosage regimen is necessary);
- Psoriasis (during therapy, the weighting of the course of psoriasis is possible);
- Diabetes mellitus (at the beginning of treatment it is necessary to regularly monitor the concentration of glucose in the blood, including active self-control by the patient; it is possible to reduce the severity of precursors of hypoglycemia, including tachycardia, increased sweating and a feeling of heartbeat).
Also, caution must be exercised when conducting desensitizing therapy and elderly patients (reception of Locrien should be started under close medical supervision with small doses).
Dosing and Administration
Lokren should be taken orally without chewing and drinking plenty of fluids.
As a rule, Lokren is prescribed in the initial dose of 10 mg. If the target blood pressure values are not reached within 1-2 weeks of the drug use, double the dose (higher doses are usually not prescribed, since this does not lead to an increase in the antihypertensive effect).
The maximum daily dose is 40 mg.
Patients with renal insufficiency, depending on the functional state of the kidneys, are advised to adjust the dose. When creatinine clearance is more than 20 ml per minute, dose adjustment is not performed, however, clinical observation is recommended at the beginning of therapy (equilibrium concentration of Locri in the blood is usually reached by 4–7 days of therapy). With severe renal failure (creatinine clearance less than 20 ml per minute), the drug should be taken at 5 mg per day. With a lack of effectiveness every 1-2 weeks, an increase in the dose of 2 times is possible. The maximum dose is 20 mg per day.
Patients with hepatic impairment usually do not need dose adjustment, but at the beginning of treatment more careful monitoring of the patient’s condition is recommended.
With the use of Lokren may develop allergic reactions, manifested in the form of itching and urticaria.
Also during therapy, the development of disorders on the part of certain body systems, which manifest themselves with different frequency:
- Cardiovascular system: often - decrease in skin temperature of the lower and upper extremities, bradycardia (sometimes severe); rarely, aggravation or development of symptoms of heart failure (swelling of the feet, ankles, and legs), slowing of AV conduction, marked reduction in blood pressure, manifestations of angiospasm in the form of Raynaud's syndrome, and an increase in peripheral circulatory disorders;
- Nervous system: often - headache, dizziness, insomnia, asthenia; rarely, depression; very rarely - confusion, hallucinations, paresthesia, nightmares;
- The digestive system: often - diarrhea, gastralgia, vomiting, nausea;
- Respiratory system: rarely - bronchospasm;
- Body of vision: rarely - reduction of intraocular pressure, dry eyes; very rarely - visual impairment;
- Metabolism: very rarely - hyperglycemia, hypoglycemia;
- Sex organs: often - impotence;
- Laboratory indicators: rarely - the appearance of antinuclear antibodies, which in exceptional cases are combined with the clinical manifestations of lupus-like syndrome (disappears after cessation of therapy);
- Effect on the fetus: hypoglycemia, bradycardia, intrauterine growth retardation;
- Dermatological reactions: rarely - various skin reactions, including itching, urticaria, exacerbation of the course of psoriasis or psoriasis-like rashes;
- Other: withdrawal syndrome (increased or increased angina attacks, increased blood pressure).
Without prior consultation with a physician, you should not abruptly interrupt therapy and change the recommended dose, as this may lead to a temporary deterioration of the heart. Sudden cessation of treatment is not particularly recommended for patients with coronary heart disease, because This can lead to cardiac arrest, severe cardiac arrhythmias, or myocardial infarction. The dose should be reduced gradually, within 14 days. To avoid more frequent attacks of angina pectoris, simultaneously with a reduction in the dose of Locri, one can begin replacement therapy with another antianginal agent.
During therapy, it is necessary to control the concentration of glucose in the blood of diabetic patients (once every 4-5 months), heart rate and blood pressure (at the beginning of the drug - every day, then once every 3-4 months; with heart rate cuts less than 50 beats per minute need to see a doctor), elderly patients - kidney function (once every 4-5 months).
When taken simultaneously with clonidine, its reception can be stopped only a few days after the cessation of the use of Locrien.
Therapy should be canceled before conducting a study on the concentration of catecholamines, vanillin-humic acid and normetanephrine in the urine and blood; as well as titers of antinuclear antibodies in the blood.
Before starting treatment, it is recommended that patients with bronchial asthma and chronic obstructive pulmonary disease be evaluated for respiratory function.
In patients with therapeutically controlled heart failure, Lokren can be used under strict medical supervision, starting treatment in very low doses, which, with good tolerance, gradually increase.
Given the negative dromotropic effect of beta-blockers, in blockade of the I degree, the drug should be used with caution.
With a heart rate at rest below 50-55 beats per minute, the dose of Locri must be reduced.
When AV degree I blockade, the drug should be used with caution.
With the use of beta-blockers may increase the frequency and duration of attacks in patients with Prinzmetal angina.
Lokren can lead to a deterioration of patients with peripheral circulatory disorders (Raynaud's disease or syndrome, chronic obliterating diseases of lower limb arteries or arteritis).
When pheochromocytoma Lokren should be taken only simultaneously with alpha-blockers.
Treatment of elderly patients should be started with a small dose and under strict supervision.
At the beginning of treatment in patients with diabetes, it is necessary to strengthen the control of the concentration of glucose in the blood, including the conduct of active self-control.
In case of psoriasis, a careful assessment of the need to use Locri should be carried out, which is associated with the possibility of weighting the course of the disease.
Lokren can increase the sensitivity to allergens and the severity of anaphylactic reactions, while the use of epinephrine (adrenaline) in anaphylactic reactions does not always give the expected effect.
When conducting general anesthesia, one must take into account the risk of developing a blockade of beta-adrenergic receptors, manifested in the form of a decrease in heart rate, a decrease in cardiac output, and systolic and diastolic pressure. The anesthesiologist should be informed that the patient is taking Lokren.
During therapy with beta-blockers, the symptoms of thyrotoxicosis may be masked.
Athletes need to consider that when using the drug during the doping control tests, a positive reaction is possible.
Alcohol should be excluded at the time of therapy.
In smoking patients, the efficacy of Lokren is lower.
Patients who use contact lenses, should be aware that during treatment may reduce the production of tear fluid.
Due to the risk of developing weakness and dizziness, which can reduce the speed of psychomotor reactions and attention, it is recommended to use caution when driving or when performing potentially dangerous types of work.
With the simultaneous use of Lokren with some drugs, unwanted effects may occur:
- Contraindications: with sultoprid, floctafenin;
- Not recommended combinations: with amiodarone, iodine-containing contrast agents, blockers of slow calcium channels (bepridil, verapamil and diltiazem), monoamine oxidase inhibitors, cardiac glycosides;
- Combinations that should be used with caution: with propafenone, inhaled halogen-containing anesthetics, drugs that can cause ventricular arrhythmias, including ventricular tachycardia such as pirouette, baclofen, insulin, and hypoglycemic inhalations, which are derived from the body, which are derived from the body, are derived from the body, and are used to get into the body, and are used to get into the body, I’ll get into the body, I’m used to get into the body, I’m used to get into the body, I’m used to get into the body, I’m used to get into the body, I’m used to get into the body. pyridostigmine, donepezil, ambenonium, rivastigmine, neostigmine, galantamine, takrin), centrally acting hypotensive drugs (alpha-m tildopa, clonidine, apraclonidine, moxonidine, guanfacine, rilmenidine), with 10% lidocaine (intravenously as an antiarrhythmic agents);
- Combinations to be taken into account: with blockers slow calcium channels of the group of dihydropyridines, nonsteroidal anti-inflammatory drugs, antipsychotics, tricyclic antidepressants (such as imipramine), mefloquine, alpha-blockers, including used in urology (tamsulosin, alfuzosin, prazosin, doxazosin, terazosin ), dipyridamole (intravenous administration), amifostine, phenytoin (intravenous administration), estrogens, xanthines, diuretics, glucocorticosteroids, tetracosactides, not epolyarizuyuschimi relaxants, coumarins, unhydrogenated ergot alkaloids, alcohol (ethanol), hypnotic and sedative drugs.
Terms and conditions of storage
Store in a dark, dry place inaccessible to children at temperature up to 25 ° C.
Shelf life - 5 years.