Betaxolol

Chemical name

1-[4-[2-(Циклопропилмето��си)этил]фенокси]-3-[(1-м��тилэтил)амино)-2-пропа нол (as hydrochloride)

Gross

C18-H29-N-O3

Characteristics

Betaxolola hydrochloride, a white crystalline powder. Rat in the water, ethanol, methanol and chloroform.

Of drugs

The drugs-protivoglaucomnoe, gipotenzivne, antianginalnoe, antiaritmicescoe. Does beta_1-adrainoretseptora, his own simpatomimeticescoy activity is a minor мембраностабилизирую щую activity. Impact sensitivity of peripheral tissues to kateholaminam hampered central sympathetic impulsaciu, suppressing the renin secretion. Has negative chrono, foreign, and dromo- batmotroponoe effect. Decreases Patient reduces airway and the need heart of oxygen (antianginalny effect), oppressing automaticity sinoatrialnogo hub and the emergence of hotbeds ectopiceskih in predserdiah, AV connections. The effect is two to three hours after admission, reaches a maximum 3-4 h continues p 12-24, stabilizing with regular admission within 1-2 weeks. Warn the AD in response to the physical strain or Stress.effegus gipotensus therapy by lower mass attack left heart and improvement of a number of indicators of its contractile ability. 75% of patients with mild or moderate hypertension reacted positively to Aciclovir. With long-term use reliably does not alter the lipid exchange sodium excretion. In patients with concomitant asthma and chronic bronchitis little reduces the external device. Use in the form of eye drops accompanied by a decline vnutriglaznogo pressure (as normal, and high) at the expense of products vnutriglazna liquid. It is mioza, ccomodation diseases, blindness and the effect of the veil in front of you (as miotiki). The effect is 30 minutes after application, reaches its maximum two hour lasts 12 hours Impact inner pressure by 25%, effective in 94% Sluchaev.bystro and completely (95%) of the skin glands (regardless of the meal). Bioavailability - 80-95%. C_max plasma states in 3-4 h, using eye drops, after 2 hours Connectivity plasma protein does not exceed 50%. Equilibrium concentration in the blood is achieved in 5-7 days regular admission. T_1/2 - 14-22 h. Metabolised in the liver with the formation of active metabolites (85%), presented with urine (more than 80%, of which 15% in unmodified form). If any liver T_1/2 grew by 33% (dose adjustment is not required); if there is a violation of the kidney-T_1/2 twice (to be reduced dose), in older patients is 30 hours Passes through GEB, placental barrier (to development gipoglikemii, bradikardii, hypotension, respiratory problems in the foetus and newborn). Penetrates into parent Moloko.v doses, in the 72 times (rats) and 90-fold (mouse) exceeding the maximum recommended for humans (MRDC) no carcinogenic action. There is mutagenic properties of the cells of mammals and bacteria. In imposing krolikam and rats has embriotoksicescoe effects (increase in postimplantatini deaths and cases rezorbtion) in doses, respectively 54 and 300 times higher than MRDC. When the input rats doses (600 MRDC) is not only embriotoksicskie, and teratogenic properties (an increase in the frequency of skeletal anomalies and internal organs).

Indications

Arterial hypertension, stenocardia voltage; Akatizia due neiroleptikami; Eye drops : otkratougolnaya chronic glaucoma, vnutriglaznaya hypertension, the state of the laser trabekuloplastiki, gipotensus prolonged therapy after rapid eye intervention.

Restrictions on the use of

Chronic obstructive lung diseases, unstable stenocardia, the propensity to bradikardii, AV blockade I extent of peripheral blood circulation, diabetes under decompensation, hypoglycaemia, feohromotsytoma, violations of the liver and kidneys, Ray, muscle weakness, old age, Children age (safety and efficiency to be determined).

Pregnancy and lactation

Perhaps if the effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, sinusova aetiology (less than 45-50 u. / min), the weakness syndrome sinusnogo hub, AV blockade II extent Arterial gipotenzia (Sad below 100 mm Hg), cardiogenny shock, a severe and refrakternaya to treat severe heart failure, severe obstructive respiratory distress.

Side-Effects

From the nervous system and sensory organs : fatigue (7.1%), headache (6.5%), dizziness (4.5%), drowsiness (2.8%), insomnia (1.2%), concern (0.8%), depression (0.8%), the concentration, nightmares, sinkope, stalemate, hallucinations, amnesia, emotional lability, disorders sensitivity, paresthesia, nevralgia, neiropatia; pain and noise in the ears, vestibular violations partial hearing loss, Tremor.so the urogenital system : impotence (1.2%), dizuria, oliguria, proteinurija, oedema, anesthetic, renal kolica, reduced libido, the menstrual cycle, pain and changes fibrosno-kistosnye breast (women), prostate, disease Peyroni.so part of the intestine : neuralgia (4.7%), diarrhea (2%), nausea (1.6%), dry mouth, anorexia, disfagia, vomiting, constipation, pain in Zivote.so the respiratory system : infection upper respiratory tract infection (2.6%), despnoe (2.4%), pain in the chest (2.4%), pharyngitis (2%), myalgia (1.4%), sinusit, cough, shortness of breath, bronhospazm, respiratory Nedostaternsti.so the circulatory system and blood (blood, gemostaz) : aetiology (8.1%); symptomatic 0.8%, heart, AV blockade gipotenzia, hypertension, the trophic attack, myocardial infarction, heart failure, exacerbation peremejateisa hromota, thrombosis, anaemia, leucocytosis, thrombocytopenia, Purpura.so the musculoskeletal system : artralgia (3.1%), tendonitis Mialgia.so the Skin : rash (1.2%), alopecia, eczema, erythema, worsening psoriasis, gipertrihoz, Prurigo.prochie : allergic reactions, the concentration of LDG, liver enzymes (AST, ALT), acidosis, giperholesterinemia, giperglikemia, giperlipidemia, giperuriquemia, gipokaliemia, hypothermia, the change in mass body syndrome Otmena.pri use eye drops : slezotechenie (immediately after instillation) feeling discomfort or inogodny body in the eye, dry eyes, the fog, pain, refers, anizokoria, reducing sensitivity or spotted sensitive cornea keratit, erythema, itching, systemic reaction.

Specific guidance

The treatment may change the results of laboratory studies (lozhnopolojitelnaya reaction in the analysis of doping, titra growth antinuclearnah antibodies, etc.).

Patient interaction

Increases (mutually), the likelihood of violations of automaticity, and conduction sokratimosti hearts in the face of evidence, diltiazema, verapamila, hinidinovykh preparations the risk of hypotension and cardiac decompensation activities, in the face of digidropiridinovh calcium antagonists, especially in patients with latent heart failure. NPVS, glukokortikoida, estrogena, obwolakiwate and antatsidnye to weaken gipotenzivny effect; Tricyclic antidepressants (imipramin) increase (perhaps the Orthostatic hypotension). Potenziruet the nedepoliarizuth miorelaksantov hampered lidocaine metabolism in the liver. Zimetidin fenotiazina and to the concentration of plasma. If you are systemic and local (in the form of eye drops) of бета-адреноблокаторо�� The evolution of additive effects (on the inner pressure or systemic).

Overdosing

Symptoms : dizziness, aetiology, incredible, gipotenzia, acute cardiac insufficiency, bronhospazm, hypoglycaemia, convulsions, in the most severe cases - Kollaps.lechenie : wash stomach, and the appointment of absorbent; symptomatic treatment : atropine (in / with 1-2 mg), beta-adrainomimetiki (izoprenalin), sedation (diazepam, lorazepam), cardiac (dobutamin, dopamine, epinephrine, norapinefrin) preparations glukagon and other means. The blockade heart can transvenoznaya stimulation. Haemodialysis weak.

Precautions

Treatment is carried out at regular doctor control. Can mask of tireotoxicoza and gipoglikemii (in patients with diabetes receiving antidiabetic drugs). Impact compensatory cardiovascular reactions in response to the use of general anaesthetics and yodsoderjath contrasting substances. Before operational interference with the use of general anesthesia should be lifted product or select anestetik with the least negative effect inotrope. Older patients increased the risk of hypothermia, mental disorders, the side effects of the cardiovascular system. In human liver and kidneys recommended clinical monitoring for the first 4 days. Against the backdrop of aggravated allergologicaki history may increase symptoms reaction гиперчувствительност и and the lack of therapeutic effect of the usual dose adrenaline. Recommended that the use of alcohol at the time of treatment. Be wary of during the drivers of vehicles and people skills relate to the high concentration of attention. Termination treatment should be phased in over about two weeks.

Dosing and Administration

Inside morning. When hypertension and 10 mg once. If after 14 days the effect is insufficient, dose can be increased to 20 mg and in 1-2 weeks to 40 mg in a time. For patients with compromised renal function in dialysis, and elderly patients, the initial dose of 5 mg, once, if necessary, be increased by 5 mg every 14 days to 20 mg (not more). In glaucome : instillation in kongungualny bag on one drop twice a day (during the first month under the supervision vnutriglaznogo pressure).

Literature

DV Preobrazhensky, A. Sidorenko, Romanov NE, Shatunov IM Clinical pharmacology major classes of drugs antigipertenziveh / / Consilium Medicum-2000. T.-2-N 3-S. 99-127.

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