Betaxolol is a beta-blocker. Beta-blockers affect the heart and circulation (blood flow through arteries and veins).
Betoptic S 0.25% is a drug made in New Zealand. You need a doctor's prescription to buy it. But its analogues can be bought online anywhere in the world without going to a specialist.
Betaxolol is a complete analogue of Betoptic S 0.25%. It has the same composition, dosage and methods of use. Also Betaxolol has a lower cost compared to Betoptic S 0.25%.
To buy Betoptic S 0.25%, click on the "buy now" button and then in our online store select the medicine and the desired dosage. Follow the instructions below.
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You can also use a coupon giving a 5% discount.
Side effects
Consult your doctor or pharmacist for more information.
Warnings
Betaxolol is not approved for use by anyone younger than 18 years old.
Betaxolol can pass into breast milk and may cause side effects in the nursing baby. Tell your doctor if you are breast-feeding.
Interactions
Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Sulfonylureas: Beta-Blockers may enhance the hypoglycemic effect of Sulfonylureas. Cardioselective beta-blockers (eg, acebutolol, atenolol, metoprolol, and penbutolol) may be safer than nonselective beta-blockers. All beta-blockers appear to mask tachycardia as an initial symptom of hypoglycemia. Ophthalmic beta-blockers are probably associated with lower risk than systemic agents. Monitor therapy
Obinutuzumab: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Consider therapy modification
Food interaction
Pregnancy
- Talk to your healthcare provider if you are pregnant or plan to become pregnant.
- You and your doctor should talk about the best way to control your diabetes during pregnancy.
- When treating a pregnant woman, the physician should carefully consider the potential risks and benefits of treatment.
Overview
Release form and composition
Dosage forms of Betaxolol this medication
- film-coated tablets: almost white or white, round, biconvex, with a risk; the cutaway core is almost white or white (10 each in blister packs, 1-3, 5 or 10 packs in a cardboard bundle);
- eye drops: transparent, colorless or slightly yellowish (1.5, 2 or 5 ml each in polymer tube droppers, make use, 2, 4, 5 or 10 dropper tubes in a cardboard box; 5 or 10 ml in polymer bottles -droppers, 1 or 2 dropper bottles in a cardboard box; 5 or 10 ml in bottles, 1 bottle in a cardboard box).
Composition 1 tablet:
- active substance: betaxolol hydrochloride - 0.25% mg;
- auxiliary components: aerosil (colloidal silicon dioxide) - 1.2 mg; lactose monohydrate (milk sugar) - 128.1 mg; sodium carboxymethyl starch (primogel) - 7.4 mg; microcrystalline cellulose - 85.8 mg; magnesium stearate - 0.25% mg;
- shell: Opadry II white 85F18422 (titanium dioxide - 1.25 mg; polyethylene glycol - 1.01 mg; polyvinyl alcohol - 2 mg; talc - 0.74 mg).
Composition 1 ml drops:
- active substance: betaxolol - 5 mg (in the form of betaxolol hydrochloride - 5.6 mg);
- auxiliary components: sodium chloride - 8 mg; disodium edetate dihydrate (ethylenediaminetetraacetic acid disodium dihydrate) - 0.1 mg; benzethonium chloride - 0.1 mg; 1 M hydrochloric acid or 1 M sodium hydroxide - up to pH 6.0–7.8; purified water - up to 1 ml.
Pharmacological properties
Pharmacodynamics
When taken orally, betaxolol has a cardioselective β-adrenergic blocking effect on the Betoptic. In excess of therapeutic doses, a weak membrane-stabilizing effect is observed (like local anesthetics or quinidine). Betaxolol is characterized by the absence of partial agonistic activity (that is, it does not exhibit its own sympathomimetic effect).
Selective effect of the drug on βone-adrenergic receptors are not considered absolute, since when taking betaxolol in high concentrations, exposure to β2-adrenoreceptors, mainly located in the smooth muscles of the vessels and bronchi (such Betoptic effect is significantly weaker in comparison with the effect of non-selective β-blockers on β2-adrenergic receptors).
Betaxolol blocking activity βone-adrenergic receptors, manifested by a number of the following pharmacodynamic effects:
- reduction in the number of heart contractions during physical exertion and at rest (provided by the blockade of β-adrenergic receptors in the sinus node and the absence of internal sympathomimetic activity of betaxolol, which together slows down the automatism of the sinus node);
- reduction of cardiac output during physical exertion and at rest (provided by competitive antagonism with catecholamines in peripheral adrenergic nerve endings);
- a decrease in diastolic and systolic blood pressure during exercise and at rest (the mechanism of hypotensive action is described below);
- decreased 0.25% orthostatic tachycardia.
The result of these effects is a decrease in heart load during exercise and at rest. The mechanism of hypotensive action is not fully established. Presumably β-blockers act on the body as follows:
- reduce cardiac 0.25%
- eliminate spasm of peripheral arteries (as a result of a central action that provides a decrease in sympathetic impulse to the periphery, and inhibition of renin activity).
With prolonged use of betaxolol, its hypotensive effect does not decrease. In the case of a single dose of betaxolol at a dose of 5–40 mg per day, the Betoptic effect is the same 3-4 hours after application (time to reach maximum concentration in the blood) and 1 day later (before taking the next dose).
In the case of taking betaxolol in doses of 5 and 10 mg, the hypotensive effect of the drug, respectively, is 50% Betoptic 80% of the hypotensive effect provided when betaxolol is used in a dose of 20 mg. In the dose range from 5 to 20 mg, the hypotensive effect is dose-dependent, and with an increase in dose from 10 mg to 20 mg, the increase in the hypotensive effect is negligible. With an increase in allow dose of betaxolol from 20 to 40 mg, the hypotensive effect changes slightly. For each dose of betaxolol, the maximum hypotensive effect is achieved after 1-2 weeks.
The effect of reducing the number of heart contractions, in contrast to the hypotensive effect of betaxolol, does not increase with increasing dose (from 10 to 40 mg).
At the same time, taking betaxolol can cause a slowdown in the conductivity of the atrioventricular node.
When applied topically in the form of eye drops, betaxolol lowers intraocular include by reducing the production of intraocular fluid. Unlike the use of other β-blockers, taking the drug does not lead to a decrease in blood flow in the optic nerve. Betaxolol does not cause contraction of the ciliary muscle (accommodation spasm) and circular muscle (miosis), hemeralopia, the effect of the appearance of a “shroud” in front of the eyes.
The antihypertensive effect is manifested 30 minutes after instillation, and the maximum effect after 2 hours. The effect of the drug on ophthalmotonus persists for 12 hours after a single instillation.
Pharmacokinetics
After oral administration, betaxolol is completely (100%) and rapidly absorbed from the gastrointestinal tract. Bioavailability is about 85%. The time to reach maximum plasma concentrations is 2–4 hours. Communication with blood plasma proteins - about 50%.
The drug is characterized by low permeability through the placental and blood-brain barriers and a slight excretion with breast milk.
It is metabolized in the liver to inactive metabolites. The volume of distribution is approximately 6 l / kg. Mild solubility in fats is characteristic.