Butylamin hydroxypropoxyphenoxymethyl methyloxadiazole - instructions for use, dose, side effects, contraindications

Unselectively blocks alpha and beta-adrenergic receptors. Refers to Class II antiarrhythmics. Expands blood vessels, reduces the overall peripheral vascular resistance, reduces cardiac output.

When instilled into the conjunctival sac, it lowers the intraocular pressure (reduces the volume of watery moisture).

Hypotensive, anti-anginal, antiarrhythmic, anti-glaucoma.

Pharmacokinetics:The hypotensive effect on intraocular pressure occurs 15-30 minutes after instillation and reaches a maximum after 4-6 hours. The duration of the action is 24 hours. The drug does not change the diameter of the pupil and accommodation, it does not render locally irritatinghis actions.

Indications:

Inside: arterial hypertension, stenocardia (prophylaxis), arrhythmia, compensated chronic heart failure (as part of a combination therapy).

Parenteral: hypertensive crisis.

Conjunctival: glaucoma (open and closed, secondary).

ICD-10

VII.H40-H42.H40.5 Glaucoma secondary due to other eye diseases

VII.H40-H42.H40.4 Glaucoma secondary due to inflammatory disease of the eye

VII.H40-H42.H40.3 Glaucoma secondary posttraumatic

VII.H40-H42.H40.2 Primary angle-closure glaucoma

VII.H40-H42.H40.1 Primary open angle glaucoma

IX.I20-I25.I20 Angina pectoris [angina pectoris]

IX.I10-I15.I15 Secondary Hypertension

IX.I10-I15.I10 Essential [primary] hypertension

IX.I30-I52.I50.0 Congestive heart failure

IX.I30-I52.I49.9 Disorder of heart rhythm, unspecified

Contraindications:

Hypersensitivity.

In the systemic application: AV-block II-III level, decompensated heart failure, cardiogenic shock, sinus bradycardia, hypotension, chronic obstructive pulmonary disease, bronchial asthma, gastric ulcer and duodenal ulcer, diabetes Type 1, pregnancy, breastfeeding, age under 18 years (efficacy and safety of use not established).

Carefully: When instillation in the conjunctival sac: AV-blockade II-III degree, decompensatedchronic cardiac insufficiency, cardiogenic shock, sinus bradycardia, chronic obstructive pulmonary diseases, bronchial asthma, stomach ulcer

and twelve fingersoh intestines, diabetes

1-st type.

Pregnancy and lactation:Category of recommendations Food and Drug Administration (US Food and Drug Administration) not determined. Adequate and well-controlled studies on humans and animals have not been conducted. Contraindicated in pregnancy. There is no information on the penetration into breast milk.

Dosing and Administration:

Inside, intravenously, conjunctivally.

For antihypertensive, antianginal and antiarrhythmic therapy: inside, 10 mg 3-4 times a day with a gradual increase (with good tolerability) by 10-20 mg per day to 80-120 mg per day, the maximum dose is 240 mg per day; with chronic heart failure 5 mg 3 times a day, with a gradual increase of 15 mg per day to achieve a daily dose of 45-60 mg.

For relief of the hypertensive crisis: intravenously spray-10-20 mg (1-2 ml of 1% solution) for 1 minute, perhaps again every 5 minutes until the effect is achieved, no more than 50-100 mg (5-10 ml of 1% solution ).With intravenous drip administration, 50 mg (5 ml of a 1% solution) is diluted in 200 ml of a 0.9% solution of sodium chloride or in a 5% solution of dextrose and injected at a rate of 0.5 mg per minute (2 ml infusion solution) until a positive reaction .

Conjunctival: 1 to 2 drops of 1% solution are instilled into the conjunctival sac 2-3 times a day, in case of insufficient effect, 2% solution is used (can be combined with pilocarpine and / or clonidine as eye drops).

Side effects:

With systemic application (inside, parenteral): headache, dizziness, weakness, asthenia, increased fatigue, increased sweating, chills; bradycardia, excessive lowering of arterial pressure, cooling of the limbs, blockade of the legs of the bundle of the Guiss, AV blockade; bronchospasm, increased contractility of the myometrium; nausea, dry mouth, epigastric pain; allergic reactions (local or generalized exanthema, urticaria).

When instillation in the conjunctival sac: bradycardia, lowering blood pressure, bronchospasm, dizziness, weakness, nausea, allergic reactions (local or generalized exanthema, urticaria); local reactions - burning (within 15-20 seconds).

Overdose:

Symptoms: increased severity of side effects.

Treatment: symptomatic therapy.

Interaction:

Pilocarpine in the form of eye drops: increased effect (decreased intraocular pressure.

Clonidine in the form of eye drops: increased effect (decreased intraocular pressure).

Systemic alpha or beta-blockers: increased hypotensive effect.

Cardiac glycosides, methyldopa, reserpine and guanfacine, blockers of "slow" calcium channels (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs: increased risk of developing or worsening bradycardia and AV blockade, can cause heart failure.

Nifedipine, diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure. Lengthens the effect of nondepolarizing muscle relaxants and anticoagulant effect of coumarins.

Tri- and tetracyclic antidepressants, antipsychotics (antipsychotics), antipsychotics ethanol, sedatives and hypnotics: increased central nervous system depression.

Inhibitors of monoamine oxidase: a significant increase in hypotensive effect.

Special instructions:

During the application of eye drops, contact lenses should not be worn.

When intravenously, the drug requires strict control of blood pressure, heart rate, electrocardiograms.

Instructions

Butylamine hydroxypropoxyphenoxymethyl methyl oxadiazole (Butylaminohydroxypropoxyphenoxymethyli methyloxadiazolum)