Lokren - a drug for the treatment of hypertension

width = Lokren - a drug related to cardioselective beta-blockers, gives a weak membrane-stabilizing effect, has a selective beta-adrenergic blocking effect, partial agonist activity in the drug absent.

Lokren has proven himself in the therapy of hypertension and cardiovascular pathologies. However, it has its own contraindications and indications, so you need to understand how to take the pill correctly? What do doctors say, what are the analogues of this tool?

Clinical and pharmacological group

Beta1-adrenoblocker.

Conditions of leave from pharmacies

It is released on prescription.

Price list

How much does Lokren cost? The average price in pharmacies is at the level of800 rubles.

Form of issue and composition

Lokren is manufactured in the form of tablets coated with a film sheath: round, biconvex, white, with a risk on one side and the inscription "KE 20" on the other (14 pcs. in blisters, 2 blisters in a cardboard bundle).

The composition of 1 tablet includes:

Active substance: betaxolol - 20 mg (in the form of hydrochloride);

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Auxiliary components: colloidal silicon dioxide -, mg; lactose monohydrate - 100 mg; sodium carboxymethyl starch (type A) - 4 mg; microcrystalline cellulose - 113 mg; magnesium stearate, mg.

Composition of the film coat: Macrogol 400 -, 3 mg; hypromellose -, mg; titanium dioxide (E171) -, 7 mg.

Pharmacological effect

Lokren has a selective beta-adrenoblocking and membrane-stabilizing action, while not possessing its own sympathomimetic action.

The use of the drug leads to a decrease in heart rate, a decrease in cardiac output, diastolic and systolic arterial pressure at rest and under physical exertion, and also to a decrease in the orthostatic reflex tachycardia. These effects help reduce the load on the heart at rest and in motion.

Indications for use

What helps? Lokren is prescribed for arterial hypertension. With its help, prevent the attack of angina pectoris.

Contraindications

The agent is considered to be banned under such conditions:

Monotherapy of angina of Prinzmetal;
Severe form of obliterating pathologies of peripheral arteries and Raynaud's disease;
Severe form of chronic obstructive pulmonary disease and bronchial asthma;
Metabolic acidosis;
Pheochromocytoma in the absence of simultaneous use of alpha-blockers;
Simultaneous use with sultopride, floktaphenin, monoamine oxidase inhibitors;
Lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
Cardiogenic shock;
Acute congestive heart failure;
Cardiomegaly (in the absence of symptoms of heart failure);
Age to 18 years;
The period of breastfeeding;
Anaphylactic reactions in the anamnesis;
Chronic heart failure in the stage of decompensation (with ineffective therapy with inotropes, diuretics, angiotensin-converting enzyme inhibitors and other vasodilators);
Atrioventricular (AV) blockade of II and III degree (without artificial pacemaker);
Syndrome of weakness of the sinus node (SSSU), including sinoatrial block;
Arterial hypotension (systolic blood pressure (BP) less than 100 mm Hg);
Severe form of bradycardia (heart rate (heart rate) is less than 45-50 beats per minute);
Hypersensitivity to the components of the drug.

With caution, it is recommended to appoint Lokren to patients with chronic heart failure in the stage of compensation, AV-blockade of I degree, non-severe forms of obliterating diseases peripheral arteries and Reynaud's syndrome, prinzmetal angina (only in combination with vasodilators), bronchial asthma and chronic obstructive pulmonary disease with moderate severity the course of the disease, patients with treated pheochromocytoma, hepatic and / or renal insufficiency, diabetes mellitus, psoriasis, during desensitizing treatment and in patient therapy the elderly.

Use in pregnancy and lactation

The use of a drug during pregnancy is possible, but only in situations where the benefit to the mother exceeds the risk to the fetus. It is recommended to stop lactation for the entire period of treatment, tk. beta-blockers are absorbed into breast milk.

Dosage and route of administration

The instructions for use indicate that Lokren is taken orally and washed down with a sufficient amount of liquid. Do not chew the tablet.

The initial dose of the drug Lokren for both indications for the use of the drug is usually 10 mg (1/2 table. 20 mg). If the target values of blood pressure are not achieved within 7-14 days of treatment, the dose is doubled to 20 mg / day.
Usually, do not use doses of the drug Lokren, exceeding 20 mg (due to the fact that with increasing doses more than 20 mg there is no statistically significant increase in the antihypertensive effect of the drug).
The maximum daily dose of Lokren is 40 mg.

In patients with hepatic insufficiencydose adjustment is usually not required. However, at the beginning of therapy, a more thorough clinical observation of the patient is recommended.

In patients with renal insufficiencya dose adjustment is recommended depending on the functional state of the patient's kidneys. With QC more than 20 ml / min dose adjustment is not required. However, at the beginning of treatment, it is recommended to conduct clinical observation until the equilibrium concentration of the drug in the blood is reached, (which is achieved on the average by 4-7 days of treatment). At the expressed renal insufficiency (KK less than 20 ml / mines) the recommended initial dose of a preparation makes 5 mg / sut (without dependence from frequency and days carrying out the procedure of hemodialysis in patients on hemodialysis), which, if insufficiently effective, can increase 2 times every 1-2 of the week. The maximum daily dose is 20 mg.

Side effects

Lokren can cause various side effects:

On the part of the digestive system: gastralgia, nausea, diarrhea, vomiting.
From the side of metabolism: in rare cases - hyperglycemia, hypoglycemia.
On the part of the organs of vision: decreased intraocular pressure, dry eyes, impaired vision.
On the part of the genitals: impotence. Allergic reactions: skin rash, hives, itching, exacerbation of psoriasis or the appearance of psoriasis-like rashes.
From the nervous system: insomnia, headaches, asthenia, dizziness; rarely - confusion, depression, nightmares, hallucinations, paresthesia.
From the respiratory system: in rare cases - bronchospasm. Influence on the fetus: bradycardia, hypoglycemia, intrauterine growth retardation.
From the cardiovascular system: a marked decrease in blood pressure, bradycardia, symptoms of heart failure, a decrease in the temperature of the skin lower and upper extremities, slowing of AV conduction and development of angiospasm manifestations (increased peripheral circulatory disturbances, syndrome Reynaud).

Lokren can cause the "withdrawal" syndrome (increased blood pressure, increased / increased angina attacks), arthralgia, back pain, decreased potency and decreased libido.

Overdose

When taking high doses of medicament there are:

fainting condition;
cyanosis of the palms, nails;
difficulty breathing;
dizziness;
heart failure;
bradycardia;
arrhythmias;
decreased blood pressure;
atrioventricular block;
ventricular extrasystole;
convulsions.

It is recommended to take enterosorbents and emergency gastric lavage. At registration of a bradycardia or fast falling of a BP appoint or nominate 1 mg of a glucagon. If necessary, additionally, a slow infusion of isoprenaline - 25 μg or dobutamine - 10 μg / kg. If a heart failure is found in a newborn, due to taking betaxolol by the mother during pregnancy, immediate hospitalization with long-term administration of isoprenaline and dobutamine in large doses under the supervision of specialists (pediatrician, pediatric cardiologist, resuscitator).

special instructions

Do not interrupt Lokren's treatment abruptly and change the recommended dose without first consulting a physician, since this can lead to a temporary worsening of the heart. Treatment should not be interrupted suddenly, especially in patients with ischemic heart disease. sudden cancellation can lead to severe heart rhythm disturbances, myocardial infarction or cardiac arrest. The dose should be reduced gradually, that is, within 2 weeks, and if necessary, it is possible to simultaneously To start substitution therapy with another antianginal drug in order to avoid more frequent attacks angina pectoris.

Patients taking Lokren should monitor heart rate and blood pressure (at the beginning of treatment daily, then once every 3-4 months), the concentration of glucose in the blood in patients with diabetes mellitus (1 every 4-5 months), the function of the kidneys in elderly patients (1 every 4-5 months).

The patient should be taught how to calculate heart rate, and the patient should be instructed to consult a doctor if the heart rate is less than 50 beats per minute.

Approximately in 20% of patients with angina pectoris beta-blockers are ineffective. The main causes are severe coronary atherosclerosis with a low threshold of ischemia (heart rate at the time of an anginal attack less than 100 bpm) and increased end-diastolic pressure of the left ventricle, which violates the subendocardial blood flow.

With the simultaneous administration of clonidine, his reception may be discontinued only a few days after the withdrawal of the drug Lokren.

Lokren should be discontinued before the study of the concentration of catecholamines, normetanephrine and vanillin-mandelic acid in blood and urine; as well as titers of antinuclear antibodies in the blood.

Heart failure

In patients with heart failure controlled therapeutically, if necessary, betaxolol can be used under strict medical supervision in a very low initial doses with a gradual increase if necessary and in case of good tolerability (preservation of the compensated state of chronic cardiac insufficiency).

Bronchial asthma and chronic obstructive pulmonary disease

Beta-blockers may be prescribed only to patients with moderate disease severity, with the choice of a selective beta-blocker in a low initial dose. Before the start of treatment it is recommended to perform an evaluation of the function of breathing.
With the development of seizures during treatment, bronchodilators - beta2-adrenomimetics - can be used.

AV-blockade of the I degree

Given the negative dromotropic effect of beta-blockers, with blockade of the I degree the drug should be used with caution.

Bradycardia

If the heart rate at rest becomes less than 50-55 bpm, the dose of Lokren should be reduced.

Angina pectoris

Beta-adrenoblockers can increase the frequency and duration of seizures in patients with Prinzmetal angina pectoris. The use of cardioselective beta 1-blockers is possible with mild angina Prinzmetal or mixed-type angina pectoris, provided that the treatment is carried out in conjunction with vasodilators.

Pheochromocytoma

In the case of using beta-adrenoblockers in the treatment of arterial hypertension caused by pheochromocytoma, careful monitoring of blood pressure is required. The purpose of the drug Lokren is possible only against the background of the use of alpha-blockers.

Violations of peripheral circulation

Beta-blockers can lead to worsening of patients with impaired peripheral circulation (Raynaud's disease or Raynaud's syndrome, arteritis or chronic obliterating diseases of lower limb arteries).

Patients with renal insufficiency

The dose should be adjusted depending on the concentration of creatinine in the blood or QC.

Elderly patients

Treatment of elderly patients should start with a small dose and under strict supervision.

Psoriasis

It requires a careful assessment of the need for the drug, there are reports of weighting the course of psoriasis during treatment with beta-blockers.

Patients with diabetes mellitus

It is necessary to warn the patient about the need to strengthen the control of blood glucose concentration, including active self-control by the patient, at the beginning of treatment. The patient should be aware that the initial symptoms of hypoglycemia (especially tachycardia, palpitation and sweating) can be masked with betaxolol.

Allergic reactions

Beta-blockers, including Lokren, may increase sensitivity to allergens and severity anaphylactic reactions due to the weakening of adrenergic compensatory regulation under the action of beta-blockers. Therapy of anaphylactic reactions with epinephrine (adrenaline) does not always produce the expected therapeutic effect.
In patients prone to severe anaphylactic reactions, especially those associated with the use of floktaphenin or carrying out desensitization, therapy with beta-blockers can lead to further intensification of reactions and decrease effectiveness of treatment.

General anesthesia

When conducting general anesthesia, the risk of blockade of β-adrenergic receptors (reduction in heart rate, reduction in cardiac output, and a decrease in systolic and diastolic blood pressure) should be considered.

Beta-adrenoblockers mask reflex tachycardia and increase the risk of developing arterial hypotension. Continuation of beta-blocker therapy reduces the risk of arrhythmia, myocardial ischemia and hypertensive crises. An anesthesiologist should be informed that the patient is receiving treatment with beta-blockers.

If it is necessary to stop Lokren before the surgery, it should be done gradually and completed 48 hours before general anesthesia; it is considered that stopping therapy for 48 h allows to restore receptors sensitivity to catecholamines.

Therapy with beta-blockers in some cases may not be interrupted:

In patients with coronary insufficiency it is desirable to continue treatment until surgery, taking into account the risk associated with the sudden abolition of beta-blockers;
In the case of emergency surgical interventions or in cases where discontinuation of treatment is not possible, the patient should protect from the effects of excitation of the vagus nerve by appropriate premedication with atropine, with repetition in the case necessity.

In such patients, for general anesthesia, it is necessary to use substances that are least depressing myocardium, and blood loss should be replenished.

The risk of developing anaphylactic reactions should be considered.

Thyrotoxicosis

Symptoms of thyrotoxicosis can be masked by therapy with beta-blockers.

For the duration of treatment should be excluded from drinking alcohol.

Patients who use contact lenses should take into account that against the background of treatment with beta-blockers may reduce the production of tear fluid.

Athletes

Athletes should consider that the drug contains an active substance, which can give a positive reaction when performing doping tests.

In smoking patients, the effectiveness of beta-blockers is lower.

Impact on ability to drive vehicles and engage in other potentially hazardous activities

When driving a vehicle or engaging in other potentially hazardous activities when taking Lokren, caution (due to the risk of developing dizziness, weakness, which can reduce the attention and speed of psychomotor reactions required for these types of activities).

Drug Interactions

Non-recommended combinations with Lokren include combinations with such drugs:

Amiodarone - leads to a violation of automatism, contractility and conductivity;
Cardiac glycosides - increase the risk of developing or enhancing AV blockade, bradycardia, cardiac arrest;
Blockers of slow calcium channels (diltiazem, bepridil, verapamil) - cause disorders automatism (stopping the sinus node, pronounced bradycardia), AV-conduction, cardiac failure;
Yodsoderzhaschie contrast substances - can lead to the development of a sharp decline in blood pressure or shock, beta-adrenoblockers - reduce the compensatory cardiovascular reactions.

Caution should be used combination Lokrena with the following drugs:

Propafenone - a violation of automatism, conduction and contractility;
Baclofen - increases the antihypertensive effect;
Insulin and oral derivatives of sulfonylureas - masking with beta-adrenoblokatorami symptoms of hypoglycemia (palpitation, tachycardia);
Inhaled halogen-containing anesthetics - reduced by beta-adrenoblockers compensatory cardiovascular reactions. It is required to continue therapy and to abandon the sudden abolition of beta-blockers, informing about the treatment of an anesthesiologist;
Cholinesterase inhibitors (donepezil, ambenonium, galantamine, pyridostigmine, neostigmine, tacrine, rivastigmine) - the risk of bradycardia increases;
Antihypertensive agents of central action (alpha-methyldopa, clonidine, guanfacine, rilmenidine, moxonidine) - there is a risk development of AV-conduction disorder, bradycardia, a significant increase in BP with a sharp reversal of antihypertensive drug of the central actions;
Antiarrhythmics of class I A (hydroquinidine, quinidine, disopyramide) and class III (ibutilide, dofetilide, amiodarone, sotalol), benzamides (sulpiride, amisulpride, tiaprid), some neuroleptics from the phenothiazine group (ciammazin, thioridazine, chlorpromazine, levomepromazine), butyrophenones (haloperidol, droperidol), other antipsychotics (pimozide) and other drugs (difemanyl, cisapride, misolastine, halofantrine, pentamidine, moxifloxacin, injected intravenously (iv) erythromycin, vincamine and spiramycin) - the risk of ventricular arrhythmias increases (in particular, ventricular tachycardia type "pirouette");
Lidocaine (IV) - increases the concentration of lidocaine in the blood plasma, which can be accompanied by an increase in unwanted neurological signs and phenomena from the cardiovascular system.

Changes in the medicinal properties of other drugs and / or Lokren, which must be taken into account in the course of therapy:

Non-steroidal anti-inflammatory drugs (systemic action), including selective inhibitors of cyclooxygenase-2 (COX-2) - reduce hypotensive effect;
Mefloquine - increases the threat of bradycardia;
Allergens used for immunotherapy or allergen extracts used for skin tests - increase the risk of anaphylaxis or severe systemic allergic reactions;
Phenytoin (IV) - increases the likelihood of lowering blood pressure and severity of cardiodepressive action;
Estrogens, tetracosactide, glucocorticosteroids (GCS) - reduce the hypotensive effect;
Diuretics, sympatholytics, hydralazine and other antihypertensive drugs - contribute to an excessive decrease in blood pressure;
Ethanol, hypnotics and sedatives - exacerbate the depression of the central nervous system;
Blockers of slow calcium channels (from the group dihydropyridines) - cause arterial hypotension, circulatory insufficiency patients with uncontrolled or latent heart failure, beta-adrenoblockers are able to minimize reflex sympathetic mechanisms;
Dipiridamole (iv administration), antipsychotics, tricyclic antidepressants (such as imipramine), amifostine, alpha-adrenoblockers, incl. Used in urology (prazosin, doxazosin, tamsulosin, alfuzosin, terazosin) - increase the antihypertensive effect of betaxolol, increase the risk of orthostatic hypotension;
Unhydrated ergot alkaloids - increase the risk of peripheral circulatory disorders.

Betaxolol enhances the anticoagulant effect of coumarins and prolongs the effect of nondepolarizing muscle relaxants, as well as increases the concentration of xanthines (except for diphylline) in the blood.

Reviews

We picked up some feedback from people who took Lokren:

Vladimir. I took 0.5 mg of the drug and my heart rate dropped to 42 beats per minute. He reduced the dose to 0.2, the SS was up to 50 beats per minute. When taking the drug, watch for heart rate. Lokren with Lercamen completely reduces blood pressure.
Irina. Lokren once appointed my best surgeon in the city for tachycardia. I had such a tachycardia, the pulse at rest was never less than 90 beats per minute, and in waking, usually 130. A long-acting Lokren drank one tablet a day or half a tablet, depending, as the doctor appoints, I appointed a half. Saw it and the pulse did reduce for a long time. The only drawback of this medication is that it can not be abruptly dropped. It is necessary to gradually reduce the dose. Just getting used to the drug, and then without it, there may be no desirable consequences. But I already do without him.
Alexander. The medication is good for reducing the pulse rate with atrial fibrillation. When used for this purpose, the drug is a means of choice in the domestic market. To stop attacks of atrial fibrillation, it is not practical to use it (it is ineffective).

In general, reviews about Lockren on the forums are only positive. In general, the drug is recognized as quite effective. It is believed that the drug is more suitable for patients of middle and young age, because in this category of patients, hypertension is less associated with heart failure.

Analogues

A lot of Lokren's analogs are produced, which have an antihypertensive effect: Atenolol-Teva, Betak, Betakor and others. Some of them are used to treat glaucoma and are available in other dosages.

In addition to direct analogues of Lokren, drugs are produced that have an antihypertensive effect, but contain another active substance in their composition. Therefore, before using other medications, you should consult a specialist.

Before using analogues, consult your doctor.