Lokren
Use during pregnancy and breastfeeding
Pregnancy
Experimental studies have not revealed the teratogenic effect of betaxolol.
To date, no teratogenic effects have been reported in humans.
In general, beta blockers reduce blood flow to the placenta and may affect fetal development. Blood flow in the placenta and uterus should be monitored, as well as the growth and development of the unborn child should be monitored, and if adverse events occur in relation to pregnancy and/or the fetus, alternative therapeutic measures should be taken.
The newborn should be carefully examined after birth. In the first 3-5 days of life, symptoms of bradycardia and hypoglycemia may occur, because The effect of beta-blockers in newborns whose mothers took them before birth persists for several days after birth. During the neonatal and postnatal period, newborns have an increased risk of cardiac and respiratory complications. In case of heart failure, hospitalization of the newborn in an intensive care unit is required. The use of plasma expanders should be avoided (risk of developing acute pulmonary edema). Bradycardia, respiratory failure and hypoglycemia have also been reported. In this regard, during the first 3-5 days of life, careful monitoring of such newborns in a specialized department is required (heart rate, blood glucose concentration).
In this regard, the use of Lokren® during pregnancy is not recommended and is only possible if the benefit to the mother outweighs the potential risk to the fetus or child.
Lactation period
Beta blockers, including betaxolol, are excreted in breast milk. The risk of hypoglycemia or bradycardia in infants has not been studied, therefore, as a precaution, breastfeeding should be discontinued during treatment.
Use for liver dysfunction
Use with caution in case of liver failure (more careful clinical monitoring is required at the beginning of treatment).
Use for renal impairment
Use with caution in case of renal failure (for creatinine clearance more than 20 ml/min - careful monitoring of the patient during the first 4 days of treatment; for creatinine clearance less than 20 ml/min and/or hemodialysis, adjustment of the dosage regimen is required.
Use in children
Contraindication: children and adolescents under 18 years of age (efficacy and safety have not been established).
special instructions
You should not interrupt treatment with Lokren® abruptly and change the recommended dose without first consulting your doctor, because this may lead to a temporary deterioration in heart function. Treatment should not be interrupted suddenly, especially in patients with coronary artery disease, because Sudden withdrawal may result in severe heart rhythm disturbances, myocardial infarction, or cardiac arrest. The dose should be reduced gradually, that is, over 2 weeks, and if necessary, replacement therapy with another antianginal agent can be started at the same time to avoid an increase in angina attacks.
In patients taking Lokren®, heart rate and blood pressure should be monitored (daily at the beginning of treatment, then once every 3-4 months), blood glucose concentration in patients with diabetes mellitus (once every 4-5 months), kidney function in the elderly patients (once every 4-5 months).
The patient should be taught how to calculate heart rate, and the patient should be instructed to contact a doctor if the heart rate decreases below 50 beats/min.
In approximately 20% of patients with angina, beta blockers are ineffective. The main reasons are severe coronary atherosclerosis with a low ischemic threshold (heart rate at the time of development of an anginal attack less than 100 beats/min) and increased end-diastolic pressure of the left ventricle, disrupting subendocardial blood flow.
When taking clonidine simultaneously, it can be discontinued only a few days after stopping the drug Lokren®.
Lokren® should be discontinued before studying the concentration of catecholamines, normetanephrine and vanillinmandelic acid in the blood and urine; as well as titers of antinuclear antibodies in the blood.
Bronchial asthma and chronic obstructive pulmonary disease
Beta blockers should only be prescribed to patients with moderate disease severity, with the choice of a selective beta blocker at a low initial dose. Before starting treatment, it is recommended to assess respiratory function.
If attacks develop during treatment, bronchodilators - beta2-adrenergic agonists can be used.
Heart failure
In patients with therapeutically controlled heart failure, if necessary, betaxolol can be used under strict medical supervision in very low initial doses with a gradual increase if necessary and if well tolerated (maintaining a compensated state of chronic heart failure).
Bradycardia
If the heart rate at rest falls below 50-55 beats/min, the dose of Lokren® must be reduced.
1st degree AV block
Considering the negative dromotropic effect of beta-blockers, the drug should be used with caution during first-degree blockade.
Prinzmetal's angina
Beta blockers may increase the frequency and duration of attacks in patients with Prinzmetal's angina. The use of cardioselective beta1-blockers is possible for mild Prinzmetal angina or mixed angina, provided that treatment is carried out in combination with vasodilators.
Peripheral circulation disorders
Beta-blockers may lead to a deterioration in the condition of patients with peripheral circulatory disorders (Raynaud's disease or Raynaud's syndrome, arteritis or chronic occlusive diseases of the arteries of the lower extremities).
Pheochromocytoma
When beta-blockers are used in the treatment of arterial hypertension caused by pheochromocytoma, careful monitoring of blood pressure is required. Prescription of the drug Lokren® is possible only against the background of the use of alpha-blockers.
Elderly patients
Treatment of elderly patients should begin with a low dose and under strict supervision.
Patients with kidney failure
The dose must be adjusted depending on the concentration of creatinine in the blood or CC.
Patients with diabetes mellitus
The patient should be warned about the need to increase control of blood glucose concentrations, including active self-monitoring by the patient, at the beginning of treatment. The patient should be aware that the initial symptoms of hypoglycemia (especially tachycardia, palpitations and sweating) may be masked by betaxolol.
Psoriasis
A careful assessment of the need to use the drug is required, because There are reports of worsening psoriasis during treatment with beta-blockers.
Allergic reactions
Beta blockers, including Lokren®, may increase sensitivity to allergens and the severity of anaphylactic reactions due to weakening of adrenergic compensatory regulation under the influence of beta blockers. Treatment of anaphylactic reactions with epinephrine (adrenaline) does not always give the expected therapeutic effect.
In patients prone to severe anaphylactic reactions, especially those associated with the use of floctafenine or during desensitization, therapy with beta-blockers may lead to a further increase in reactions and a decrease in the effectiveness of treatment.
General anesthesia
When performing general anesthesia, the risk of β-adrenergic receptor blockade (decreased heart rate, decreased cardiac output, decreased systolic and diastolic blood pressure) should be taken into account.
Beta-blockers mask reflex tachycardia and increase the risk of developing arterial hypotension. Continuing therapy with beta-blockers reduces the risk of arrhythmia, myocardial ischemia and hypertensive crises. The anesthesiologist should be informed that the patient is being treated with beta-blockers.
If it is necessary to stop therapy with Lokren® before surgery, this should be done gradually and completed 48 hours before general anesthesia, because It is believed that cessation of therapy for 48 hours allows the sensitivity of receptors to catecholamines to be restored.
Therapy with beta-blockers in some cases may not be interrupted:
- in patients with coronary insufficiency, it is advisable to continue treatment until surgery, given the risk associated with sudden withdrawal of beta-blockers;
- In cases of emergency surgery or in cases where discontinuation of treatment is not possible, the patient should be protected from the effects of vagal stimulation by appropriate premedication with atropine, repeated if necessary.
In such patients, for general anesthesia it is necessary to use substances that depress the myocardium to the least extent, and blood loss should be replaced.
The risk of developing anaphylactic reactions must be taken into account.
Thyrotoxicosis
Symptoms of thyrotoxicosis may be masked by therapy with beta-blockers.
Athletes
Athletes should be aware that the drug contains an active substance that may give a positive reaction during doping control tests.
Alcohol consumption should be avoided during treatment.
Patients using contact lenses should take into account that during treatment with beta-blockers, the production of tear fluid may decrease.
In smoking patients, the effectiveness of beta-blockers is lower.
Impact on the ability to drive vehicles and engage in other potentially hazardous activities
When driving vehicles or engaging in other potentially hazardous activities, caution should be exercised while taking Lokren® (due to the risk of dizziness and weakness, which may reduce the attention and speed of psychomotor reactions required for these activities).
Contraindications to the use of the drug Lokren
History of anaphylactic reactions, hypersensitivity to betaxolol or other components of the drug, asthma and severe forms of COPD, decompensated refractory heart failure, cardiogenic shock, II-III degree AV block in patients without an implanted pacemaker, Prinzmetal's angina, sick sinus syndrome ( including sinoatrial block), bradycardia (less than 45–50 beats/min), severe forms of Raynaud's syndrome and peripheral circulatory disorders, untreated pheochromocytoma, severe arterial hypotension, concomitant therapy with floctafenine, sultopride, amiodarone, bepridil, diltiazem and verapamil (see INTERACTIONS ), congenital galactosemia, glucose/galactose malabsorption syndrome or lactase deficiency (the drug contains lactose), breastfeeding period, age up to 14 years.
Overdose of the drug Lokren, symptoms and treatment
Symptoms: bradycardia, marked decrease in blood pressure. Treatment: for bradycardia or severe arterial hypotension, 1–2 mg of atropine is administered intravenously, 1 mg of glucagon (the drug is repeated if necessary); if necessary, slow intravenous infusion of 25 mcg of isoprenaline or administration of dobutamine at a rate of 2.5–10 mcg/kg/min. For cardiac decompensation in newborns whose mothers took β-adrenergic receptor blockers during pregnancy: glucagon at a rate of 0.3 mg/kg; admission to the intensive care unit; isoprenaline and dobutamine, usually in fairly high doses and for a long time, under the supervision of a resuscitator.
