Active substanceButylamine hydroxypropoxyphenoxymethyl methyl oxadiazoleButylamine hydroxypropoxyphenoxymethyl methyl oxadiazole
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Dosage form: & nbsp
solution for intravenous administration
Composition:
Active substance:
Butylamine hydroxyiropoxyphenoxymethyl methyloxadiazole hydrochloride 10 mg
Excipients:
Citric acid 0.048 mg
Sodium citrate for injection 0.526 mg
Water for injection up to 1 ml
Description:Transparent colorless or slightly colored liquid.
Pharmacotherapeutic group:Alpha- and beta-blocker
ATX: & nbsp

S.01.E.X   Other antiglaucoma drugs

C.07.A.G.   Alpha-, beta-blockers

Pharmacodynamics:Butylamine hydroxypropoxyphenoxymethyl methyl oxadiazole - Beta1 and beta2-adrenoblocker with alpha1-adrenergic blocking activity, has antihypertensive, anti-anginal and antiarrhythmic effects. The drug interacts with alpha1 and beta-adrenoreceptors and does not interact with angiotensin II receptors and vasopressin.
Antihypertensive effect is provided by a decrease in cardiac output, stroke volume and a decrease in the total peripheral vascular resistance.The antianginal effect of the drug is due to a decrease in myocardial oxygen demand (due to a decrease in the heart rate (heart rate)), as well as redistribution of regional (coronary) myocardial blood flow in favor of ischemic foci due to diastole lengthening and improvement of myocardial perfusion. The mechanism of antiarrhythmic action is associated with the elimination of arrhythmogenic sympathetic influences on the conduction system of the heart, inhibition of heterogeneous automatism and the speed of propagation of excitation through the atrioventricular (AV) node, an increase in the refractory period, and a decrease in heart rate.
The tone of the bronchi in connection with the blockade of beta2-adrenoreceptors is increased.
Results of clinical study of the drug in patients with hypertensive crisis showed that systolic blood pressure (BP) decreases on average by 15% of the initial, diastolic blood pressure decreases on average by 12.8% of the initial.
Pharmacokinetics:After intravenous administration at a dose of 40 mg in the first 15 minutes in the blood plasma, high concentrations of unchanged active substance are determined (mean concentration is 29.04 μg / ml).30 minutes after the administration, the average concentration of active substance in the blood plasma is 3.31 μg / ml / - The average volume of distribution is 1.1 liters. Half-life (T1/2) - 4.2 hours, clearance - 0.8 l / h.
Indications:Hypertensive crisis (cupping).
Contraindications:Increased sensitivity to the drug, bradycardia, atrio-ventricular (AV) block II - III degree, chronic heart failure (decompensated), cardiogenic shock, hypotension, chronic obstructive pulmonary disease, bronchial asthma, simultaneous monoamine oxidase inhibitors pregnancy, lactation, age under 18 years (efficacy and safety not established).
Carefully:Atrioventricular blockade of the 1st degree, chronic heart failure, type 1 diabetes (insulin-dependent), peptic ulcer of the stomach and duodenum.
Dosing and Administration:
Only for intravenous administration!
Enter intravenously struino or drip.
Intravenously streamwise injected for 1-2 minutes at a dose of 10-20 mg (1-2 ml solution, (10 mg / ml)), previously diluted in 20 ml of 0.9% sodium chloride solution.In the absence of therapeutic effect, subsequent administrations are carried out at a dose of 20 mg (2 ml) no earlier than 30 minutes from the previous administration of the drug.
Intravenously drip 50 mg (10 mg / ml) of a 0.9% solution of sodium chloride previously dissolved in 200 ml or a 5% solution of dextrose (glucose) at a rate of 0.5 mg (2 ml infusion solution) per minute, before the therapeutic effect is achieved.
The maximum daily dose of the drug Albertor® is 50-100 mg (5-10 ml).
Side effects:

From the cardiovascular system: excessive decrease in blood pressure, incl. orthostatic hypotension, pronounced bradycardia, blockade of the legs of the bundle of His, AV blockade.

From the gastrointestinal tract: dryness of the oral mucosa, gastralgia, nausea.

From the nervous system: headache, dizziness, asthenia, fatigue, fainting.

From the immune system: allergic reactions (local or generalized exanthema, urticaria).

Other: bronchospasm, increased contractility of myometrium, increased sweating, chills.

Overdose:Symptoms: marked decrease in blood pressure, bradycardia (passes through 10-20 minutes after discontinuation of administration), acute heart failure, ventricular extrasystole, bronchospasm.

Treatment: give the patient a horizontal position with raised legs; oxygen therapy.

Symptomatic therapy:

with bradycardia - introduction of atropine, epinephrine, dobutamine, temporary pacing;

with a pronounced decrease in blood pressure - administration of vasoconstrictors (epinephrine, norepinephrine, dopamine or dobutamine), intravenous injection of plasma-substituting solutions (in the absence of signs of left ventricular failure) under the control of heart rate and blood pressure; with acute heart failure - intravenous introduction of cardiac glycosides and / or diuretics;

with ventricular extrasystole - lidocaine or phenytoin;

with bronchospasm - intravenous administration of beta2-adrenomimetics and theophylline.

Interaction:
Simultaneous use with cardiac glycosides, methyldopa, reserpine and guanfacin, blockers of "slow" calcium channels (faith-pamil, diltiazem), amiodarone and other antiarrhythmic drugs increases the risk of developing or worsening bradycardia, atrioventricular blockade, can cause heart failure.

Nifedipine, diuretics, clonidine, sympatholytics, hydralazine and other antihypertensives can lead to excessive blood pressure lowering. Lengthens the effect of nondepolarizing muscle relaxants and anticoagulant effect of coumarins.

At simultaneous appointment with tri- and tetracyclic antidepressants, antipsychotic drugs (antipsychotics), ethanol, sedatives and hypnotics, an intensification of central nervous system depression.

It is not recommended simultaneous use with MAO inhibitors due to a significant increase in antihypertensive effect.
Special instructions:
With intravenous administration of the drug, it is necessary to monitor heart rate and blood pressure, ECG monitoring. The effectiveness of the drug is assessed every 10 minutes for 30 minutes after each administration (before deciding on the need for subsequent administration).

With a decrease in heart rate, less than 60 beats per minute. subsequent administration of the drug is not carried out (risk of severe bradycardia).

In the absence of the effect of the fourth introduction, it is necessary to consider the possibility of switching to therapy with other antihypertensive drugs that are used to stop the hypertensive crisis.
Effect on the ability to drive transp. cf. and fur:Use with caution in the performance of potentially hazardous activities requiring special attention and quick reactions (driving and other vehicles, working with moving mechanisms, dispatcher and operator work, etc.).
Form release / dosage:
Solution for intravenous administration 10 mg / ml.
Packaging:
5 ml into neutral glass ampoules.
For 5 or 10 ampoules are placed in a contoured cell pack of a polyvinylchloride film or polyethylene terephthalate tape and aluminum foil or paper with a polyethylene coating, or without a foil, or without paper.
For 1 or 2 contour packs with instructions for use and a knife for opening ampoules or a scarifier ampullum is placed in a pack of cardboard.
When you pack the ampoules with a break ring or break point, the ampoule opener or ampoule scapper is not put in.
Storage conditions:
Store in a dark place at a temperature of 5 to 25 ° C.
Keep out of the reach of children.
Shelf life:2 years. Do not use after expiry date.
Terms of leave from pharmacies:On prescription
Registration number:LSR-002179/07
Date of registration:15.08.2007 / 16.12.2015
Expiration Date:Unlimited
The owner of the registration certificate:OBNINSKAYA CHEMICAL - PHARMACEUTICAL COMPANY, CJSC OBNINSKAYA CHEMICAL - PHARMACEUTICAL COMPANY, CJSC Russia
Manufacturer: & nbsp
Information update date: & nbsp14.07.2017
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