Omsulosin - instructions for use, dose, side effects, contraindications

Capsule shell composition: housing - gelatin, dye-yellow, dye-colored (Ponce 4 R), dye diamond blue, dye quinoline yellow, titanium dioxide; kholitechka - gelatin, iron oxide, yellow oxide, blue diamond dye, azorubin dye, titanium dioxide.

Composition of ink for inscription: Activated carbon, shellac.

Description:Hard gelatin capsules №2 with orange casing and brown lid, printed with black ink "R" on the lid and "TSN 400 "on the body, the contents of the capsules are white or almost white granules.

Pharmacotherapeutic group:alpha 1 - adrenoblocker

ATX: & nbsp

G.04.C.A.02 Tamsulosin

Pharmacodynamics:Omsulosin selectively and competitively blocks postsynaptic alpha 1_A-adrenoreceptors located in the smooth muscles of the prostate gland, the neck of the bladder and the prostate part of the urethra, as well as alpha-1D-adrenoreceptors, which are found mainly in the body of the bladder. This leads to a decrease in the tone of the smooth muscles of the prostate gland, the neck of the bladder, the prostatic part of the urethra and the improvement of the detrusor function, thereby reducing the symptoms of obstruction and irritation associated with benign prostatic hyperplasia. The therapeutic effect usually develops 2 weeks after the start of the drug, although in some patients a decrease symptoms are noted after the first dose.

The ability of tamsulosin to act alpha 1_A -adrenoceptors 20 times greater than his ability to interact with alpha 1B -adrenoceptors that located in the smooth muscles of the vessels.

Due to this high selectivity, the drug does not cause a clinically significant decrease systemic arterial pressure (BP) as in patients with arterial hypertension, and patients with normal initial BP.

Pharmacokinetics:

After taking the drug inside, on an empty stomach at a dose 400 mcg, the absorption of tamsulosin is more than 90% in the gastrointestinal tract (GIT).

Bioavailability of the drug is about 100%. After single oral intake of 0.4 mg maximum concentration of the drug in plasma is achieved after 4-5 hours when taken on an empty stomach, and through 6-7 hours after eating. Bioavailability of the drug is increased by 30%, and the maximum plasma concentration by 40-70% upon admission on an empty stomach, in comparison with the same parameters after eating. In the state of equilibrium concentration (after 5 days of the course reception) the maximum concentration of tamsulosin in plasma blood is 60-70% higher than after a single drug administration. Binding to plasma proteins is 94-99%. Volume of distribution is 0.2 l / kg. The drug is active metabolized by isozymes of the family cytochrome P450 (mainly isoenzymes CYP3A4 and CYP2D6) in the liver, and less than 10% of the drug is excreted in the urine in unchanged form. Therefore inhibition of these isoenzymes (due to intake appropriate drugs) can lead to increased concentration of tamsulosin in plasma blood. Most of tamsulosin is present in blood in unchanged form. The drug and its metabolites are mainly excreted in the urine (76%), with feces (21%). Half-life drug with a single admission drug capsules of prolonged action is 14-15 hours.

Indications:

Treatment of functional symptoms with benign prostatic hyperplasia glands.

Contraindications:

- Hypersensitivity to tamsulosin hydrochloride or to any other component of the drug.

- Severe hepatic insufficiency.

- Orthostatic hypotension.

- Children under 18 years.

Carefully:

Severe renal insufficiency (decrease clearance of creatinine below 10 ml / min), acute liver failure.

Dosing and Administration:

The drug is taken by 1 capsule (400 μg) in day after eating at the same time, with enough water. Capsule It is not recommended to chew, as it can to influence the release rate tamsulosin.

In the absence of therapeutic effect after 2-4 weeks of taking the drug at a dose of 400 mcg, The daily dose of Omsulosin can be increased up to 800 mcg.

Interrupted treatment with Omsulosin regardless of the daily dose (400 or 800 μg), should be resumed from a dose of 400 μg in day.

Side effects:

By frequency, the side effects were divided into the following categories: very frequent> = 1: 10; frequent> = 1: 100 and <1:10; infrequent> = 1: 1000 and <1: 100; rare> = 1: 10000 and <1: 1000; highly rare <1: 10000.

Disorders of general condition: rarely - asthenia, chest pain, back pain; very rarely - dental pain.

From the nervous system: often - the head pain; infrequently - dizziness; rarely - faint, sleep disturbance (drowsiness or insomnia).

From the side of the organs of vision: very rarely - blurred vision; single cases - intraoperative instability Iris (narrow pupil syndrome) in the operation for cataracts in patients, which increases the risk of complications during and after operation.

From the cardiovascular system: infrequent - a feeling of palpitations, orthostatic-hypotension, tachycardia.

From the respiratory system: infectious diseases diseases, influenza and influenza-like symptoms), pharyngitis, coughing; very rarely - sinusitis, rhinitis.

From the digestive system: rarely - nausea, vomiting, constipation, diarrhea.

From the side of the reproductive system: infrequently - violation of ejaculation; very rarely - decrease libido, priapism.

Allergic reactions: infrequent - skin rash, itching; rarely - angioedema, incl. edema Quincke.

Overdose:

Cases of acute drug overdose was not noted.

Symptoms: the emergence of orthostatic hypotension.

Treatment: cardiotropic therapy. If symptoms remain, it is necessary to introduce volume-substituting solutions or vasoconstrictors. For preventing further absorption a possible gastric lavage, reception activated carbon or osmotic laxative.

To restore blood pressure and heart rate (heart rate) It is necessary to transfer the patient to a horizontal position. Hemodialysis is ineffective, because tamsulosin actively binds to proteins plasma.

Interaction:

Joint use of the drug with strong and mean inhibitors of cytochromes P450 (especially with isoenzymes CYP3A4 and CYP2D6) (ketoconazole, erythromycin, paroxetine, terbinafine, etc.) leads to some increase level of tamsulosin in blood plasma.

In vitro at the level of hepatic metabolism of interaction with salbutamol was not detected. When combined with alpha₁adrenoblockers (including tamsulosin) and PDE-5 inhibitors, it is possible to lower blood pressure, and there is a potential risk of symptomatic hypotension, because both drugs have vasodilating action.

Dose adjustment is not required when using the drug with nifedipine, atenolol, enalapril, digoxin and theophylline.

With simultaneous application with cimetidine, a slight increase in the concentration of tamsulosin in the blood plasma was noted.

Co-administration with furosemide results in a slight decrease in tamsulosin absorption, which does not require dose adjustment. There is a risk of increasing the hypotensive effect when used together with anesthetics and other alpha 1 - adrenoblockers.

Diclofenac and warfarin can slightly increase the rate of elimination of tamsulosin.

Special instructions:

The drug is not intended for the treatment of hypertension.

With the simultaneous administration of Omsulosin with alpha-adrenoblockers, orthostatic hypotension (postural hypotension, dizziness), leading to fainting, is rare in rare cases. At the first signs of orthostatic hypotension (dizziness, weakness), the patient must sit or lie down and remain in this position until the above signs disappear.

Before starting to use Omsulosin, it is necessary to clarify the diagnosis and exclude diseases with similar symptoms. Patients also need to undergo regular examinations (including determining the concentration of a specific prostatic antigen (PSA), if necessary) and after treatment.

When surgical interventions for cataracts, against the background of taking the drug may develop the syndrome of intraoperative instability of the iris (narrow pupil syndrome), which must be taken into account by the surgeon for preoperative preparation of the patient and during the operation. Patients with mild to moderate liver function impairment, as well as patients with renal insufficiency, do not need to adjust the dose.

In elderly patients, there may be increased sensitivity to the action of the drug. Before taking the drug, the patient should be notified of the possibility of priapism, since this condition can lead to impotence without proper treatment.

Effect on the ability to drive transp. cf. and fur:During drug treatment, care must be taken when driving vehicles and other potentially hazardous activities.

Form release / dosage:

Capsules of prolonged action 400 mcg. 10 capsules in a blister of aluminum foil and PVC / PVDNH: 1, 3, 10 blisters in a cardboard bundle with instructions for use.

Packaging:(10) - packings, cellular, outline (1) - packs, cardboard
(10) - packings cellular planimetric (10) - packs cardboard
(10) - packings, cellular, outline (3) - packs, cardboard

Storage conditions:

Store in a dry place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001955/07

Date of registration:07.08.2007

The owner of the registration certificate:Ranbaxy Laboratories LimitedRanbaxy Laboratories Limited India

Manufacturer: & nbsp

RANBAXY LABORATORIES, Ltd. India

Representation: & nbspRABBAYS LABORATORY LIMITEDRABBAYS LABORATORY LIMITED

Information update date: & nbsp31.08.2015

Illustrated instructions

Instructions

Omsulosin (Omsulosin)