Description overdue on 06/10/2014
- Latin name: Lokren
- ATC code: C07AB05
- Active substance: Betaxolol (Betaxolol)
- Manufacturer: Sanofi-Winthrop Industrie (France)
- Composition
- Product form
- Pharmacological action
- Pharmacodynamics and pharmacokinetics
- Indications
- Contraindications
- Side effects
- Instructions for use (method and dosage)
- Overdose
- Cooperation
- Storage conditions
- Terms of sale
- Shelf life
- Cautions
- Analogs
- During pregnancy (and lactation)
- Reviews
- Price, where to buy
Composition
One tablet contains the active ingredient betaxolol - 20 mg. Additional material: sodium amylopectin glycolate, magnesium stearate, MCC, hypromellose, colloidal anhydrous silicon dioxide, macrogol, lactose monohydrate.
Product form
The drug release in a tablet form. The aluminum blister pack contains 14 tablets. Carton boxes are 2 blisters (28 tablets).
Pharmacological action
Lokren is Beta-blockers . The mechanism of action of the drug is in the blockade beta1-adrenergic receptors. Additionally Lokren has membrane stabilizing activity, without causing simpatomimicheskogo impact. The pharmacological effects of the drug:
- antianginal;
- hypotensive;
- antiarrhythmic.
The drug is able to reduce the sensitivity of tissues to catecholamines , Decrease in heart rate and indicators of myocardial contractility, inhibits secretion Renin . Also, the medication prevents increased blood pressure during stress and physical activity.
Pharmacodynamics and pharmacokinetics
After receiving the medication quickly, completely absorbed from the gastrointestinal tract. The maximum blood concentration is achieved in two hours (an indicator of the bioavailability of about 85%). Poor passes through the blood-brain barrier and the placental, sparingly soluble in fats. With blood proteins binds slightly above 50% betaxolol. Betaxolol is metabolized in the liver, as metabolites (over 80%) excreted by the kidneys. The half-life is about 20 hours. With hemodialysis betaxolol is not removed from the bloodstream. The drug is not addictive.
Indications
Means prescribed for primary and secondary hypertension ; for prophylaxis angina .
Contraindications
- Prinzmetal angina;
- heart failure;
- expressed bradycardia ;
- Individual hypersensitivity to betaxolol;
- cardiogenic shock;
- Combination therapy with sultopride;
- atrioventricular block ;
- a one-time admission monoamine oxidase inhibitors ;
- cardiomegaly .
Antihypertensives contain galactose , And the drug is contraindicated in:
- galactose malabsorption syndrome at / or glucose deficiency laktozy;
- congenital galactosemia .
Such diseases and conditions such as:
- pheochromocytoma;
- bronchial asthma;
- metabolic acidosis ;
- hepatic impairment;
- myasthenia gravis;
- old age;
- hemodialysis;
- psoriasis;
- atrioventricular block (I degree);
- hyperthyroidism;
- depression;
- diabetes;
- CRF
is a relative contraindication for appointment of betaxolol.
Side effects
From the nervous system:
- insomnia ;
- drowsiness;
- muscle weakness;
- anxiety;
- nightmares;
- confusion;
- asthenic syndrome;
- headache;
- hallucinations;
- weakness;
- dizziness ;
- fatigue.
Cardio-vascular system:
- bradycardia (sinus shape);
- orthostatic hypotension;
- reduction blood pressure ;
- palpitations;
- AV block;
- myocardial dysfunction;
- chest pain;
- manifestation Angiospasm .
From the digestive system:
- changes in taste;
- dry mouth;
- abdominal pain;
- vomiting;
- constipation;
- nausea;
- diarrhea .
The respiratory system:
- nasal congestion;
- and broncho laryngism .
In the appointment of high doses of difficulty breathing logged in predisposed patients.
From endocrine system:
- hyperglycemia;
- hypothyroid state;
- hypoglycaemia.
From the senses:
- soreness, dryness of the eyes;
- violation of visual perception.
There are allergic responses.
Rarely are recorded:
- arthralgia;
- the weakening of the libido;
- back pain;
- erectile dysfunction.
As a result of laboratory tests are sometimes found Antinuclear antibodies Which can masquerade as symptoms of lupus. In such cases, removal of the drug Lokren.
Instructions for use (method and dosage)
The drug is taken orally, with water without chewing. Observe the receive mode makes it easier to package instructions calendar days of the week. The daily dose of the medicament is 20 mg. Treatment is recommended to discontinue gradually, gradually reducing the dose of medication to a minimum performance. Otherwise, developing withdrawal .
Instructions for use Locri for patients with abnormal renal system It is somewhat different. For patients with renal failure is prescribed initial dose - 5 mg / day. In hepatic insufficiency the daily dose does not require correction. The first 100 hours of therapy with betaxolol require increased attention from doctors.
Overdose
At higher doses of medication occur:
- dizziness;
- heart failure;
- bradycardia;
- arrhythmia;
- lowering blood pressure;
- fainting;
- cyanosis of hands and nails ;
- difficulty breathing;
- atrioventricular block;
- ventricular premature beats;
- convulsions .
Recommended intake enterosorbents and emergency gastric lavage . When you register bradycardia or rapid fall in blood pressure administered 1 mg glucagon . If necessary, carry out further slow infusion isoprenaline - 25 micrograms or dobutamine - 10 mg / kg. Upon detection of heart failure in the newborn due to receiving betaxolol mother during gestation pregnancy requires immediate hospitalization with chronic administration of isoprenaline and dobutamine in large doses under the supervision of specialists (pediatrician, pediatric cardiologist, resuscitation).
Cooperation
In a joint application with Locri antiarrhythmics (diltiazem, verapamil . amiodarone . quinidine ) Dramatically increases the risk of myocardial dysfunction . When combined with the use of the drug increases the risk of floctafenine hypotension . In response to the use of halogenated anesthetics Lokren can weaken the compensatory ability of the heart. NSAIDs, steroids, antacids, enveloping means reduce the effectiveness of Locri.
The combined application tricyclic antidepressants blood pressure drops sharply and formed orthostatic hypotension. In the application of Locri with dihydropyridine derivatives in patients with heart failure (latentnoprotekayuschaya form), it increases the likelihood of hypotension and formed decompensation of heart . Do not take with Lokren MAO inhibitors .
Storage conditions
Store at temperature 15 - 25 degrees, in a dark and dry place.
Terms of sale
Requires a doctor's prescription.
Shelf life
The drug can be stored in the package 5 years.
Cautions
Patients with hepatic insufficiency and in patients with impaired renal function (creatinine clearance is 20 ml / min or greater) do not need a dose adjustment of medication. On the first day it recommended clinical observation.
In a joint application with hypoglycemic agents Lokren able to mask the symptoms of hypoglycemia in patients with diabetes. The attending doctor should warn patients about the need to control blood sugar. Lokren should be used with caution in people with diabetes, BOS syndrome , Atrioventricular block (I cent.), Heart failure, pheochromocytoma, blood circulation disorders, psoriasis. In the case of planned surgery Lokren need to cancel 48 hours prior to performing general anesthesia.
The preparation is not used in pediatrics, because No clinical data on the safety, efficiency of its use in these patients.
Analogs of Locri
Nebivolol
Biprol
Bisoprol
Concor Cor
Concor
Niperten
Betaloc ZOK
Betalok
Coronal
Egilok
Nebilet
Atenolol
Metoprolol
Pharmaceutical companies make a lot of substitutes Locri. Structural analogues:
- Betacam;
- Betalmik;
- Betakor;
- Betaxolol.
Analogs of Locri differ in cost and quality. Warn your doctor about wanting to buy a replacement, you may need correction of the treatment regimen.
During pregnancy (and lactation)
The use of medicines pregnancy possible, but only in those situations where the benefit to the mother outweighs the risk to the fetus. Recommended stop lactation for the entire period of treatment, as beta-blockers are absorbed into the breast milk.
Reviews on Lokren (overview)
Specialized forums for patients contain a lot of information about the antihypertensive drugs. Reviews Lokrene forums only positive. In general, the drug found effective enough. It is believed that the drug is more suited to patients young and middle age, because these patients rarely hypertension associated with heart failure.
In addition, there is convenience in use of the drug because it has a long action. Multiplicity of reception - once a day. Also, most patients sufficient preparata- minimum dose of 5 mg. Lokren is an effective tool that has in its arsenal of modern cardiologists and internists.
Price Locri, where to buy
The cost of the drug depends on the region of sale. The average price of Locri in Russia is 560 rubles, Ukraine - 80 hryvnia for 14 tablets. In any pharmacy of your city, you can Pricing and purchase the drug.