Duodart caps 0.5mg + 0.4mg #90

Instruction for use of Duodart

You can buy Duodart here

Duodart is a two-component drug designed to treat and control the symptoms of benign prostatic hyperplasia.

Release form and composition

Dosage form of release of Duodart - hard capsules from hypromellose: oblong, size No. 00; body - brown, lid - orange with marking in black ink "GS 7CZ"; contents of capsules - soft gelatin capsule and pellets; soft gelatin capsules - opaque, oblong, dull yellow; pellets - from almost white to white (30 or 90 pcs. in high density polyethylene bottles, 1 bottle in a cardboard box).
Composition of the shell of a hard capsule (for 1 capsule):
    body: carrageenan - 0-1.3 mg; potassium chloride - 0-0.8 mg; titanium dioxide ~ 1 mg; red dye iron oxide ~ 5 mg; purified water ~ 5 mg; hypromellose-2910 - up to 100 mg;
    cap: carrageenan - 0-1.3 mg; potassium chloride - 0-0.8 mg; titanium dioxide ~ 6 mg; sunset yellow dye ~ 0.1 mg; black ink ~ 0.05 mg; purified water ~ 5 mg; hypromellose-2910 - up to 100 mg.
Composition of 1 soft capsule:
    active substance: dutasteride - 0.5 mg;
    additional components: butylhydroxytoluene - 0.03 mg; mono- and diglycerides of capric / caprylic acid - 299.47 mg;
    shell: gelatin - 116.11 mg; titanium dioxide - 1.29 mg; glycerol - 66.32 mg; dye yellow iron oxide - 0.13 mg.
Pellet composition in 1 capsule:
    active substance: tamsulosin hydrochloride - 0.4 mg;
    additional components: talc - 8.25 mg; microcrystalline cellulose - 138.25 mg; 30% dispersion copolymer (1: 1) ethyl acrylate: methacrylic acid - 8.25 mg; triethyl citrate - 0.825 mg;
    shell: triethyl citrate - 1.04 mg; talc - 4.16 mg; 30% dispersion copolymer (1: 1) ethyl acrylate: methacrylic acid - 10.4 mg.

Pharmacological properties

Duodart is a combined drug, the components of which complement each other's action to eliminate the symptoms of benign prostatic hyperplasia (BPH):
    dutasteride: dual 5α-reductase inhibitor; inhibits the activity of 5α-reductase isoenzymes of types I and II, under the action of which testosterone is converted into 5α-dihydrotestosterone (DHT) - the main androgen responsible for hyperplasia of the glandular tissue of the prostate gland;
    tamsulosin: an α1a-adrenergic receptor blocker; inhibits α1a-adrenergic receptors in the bladder neck and smooth muscles of the prostate stroma.

Pharmacodynamics

    dutasteride: helps to lower the level of DHT, reduce the size of the prostate gland, reduce the severity of symptoms of diseases of the lower urinary tract and increase the rate of urination, as well as reduce the likelihood of acute urinary retention and the need for surgery. The maximum effect is dose-dependent, it develops within 7-14 days. After 1–2 weeks of administration at a dose of 0.5 mg, the average serum DHT concentrations in the blood decrease by 85% and 90%, respectively;
    tamsulosin: helps to increase the maximum urinary flow rate by decreasing the smooth muscle tone of the urethra and prostate gland and therefore reduces obstruction. Also, the substance reduces the symptom complex of filling and emptying. Alpha1-blockers can lower blood pressure (blood pressure) by decreasing peripheral resistance.

Pharmacokinetics

Dutasteride:
    absorption: Cmax in serum after taking 0.5 mg of dutasteride is achieved within 1-3 hours. The absolute bioavailability in men is about 60% in relation to a two-hour intravenous infusion. Bioavailability does not depend on food intake;
    distribution: large Vd (300–500 l); high (> 99.5%) degree of binding to blood plasma proteins; the serum concentration of dutasteride in the blood with daily intake reaches 65% of the stable concentration after 1 month, approximately 90% of the stable concentration level after 3 months. Css in serum and semen, equal to approximately 40 ng / ml, is reached after 6 months. After 52 weeks of therapy, the concentration of dutasteride in the semen averages 3.4 ng / ml. About 11.5% of dutasteride gets into semen from blood serum;
    metabolism: metabolized by the CYP3A4 isoenzyme of the cytochrome P450 system to two small monohydroxylated metabolites; it is also influenced by isoenzymes CYP2D6, CYP2A6, CYP1A2, CYP2C8, CYP2E1, CYP2C19, CYP2C9, CYP2B6 of this system. After reaching a stable concentration of dutasteride in the blood serum, unchanged dutasteride, 3 major and 2 minor metabolites are found;
    excretion: dutasteride in the body undergoes intensive metabolism. After oral administration of a daily dose of 0.5 mg to achieve a stable concentration through the intestine, 1–15.4% is excreted unchanged, the rest is excreted through the intestine in the form of 4 major and 6 minor metabolites. Only trace amounts of unchanged dutasteride are found in the urine. At a low serum concentration in the blood (less than 3 ng / ml), the substance is rapidly excreted in two ways. At high concentrations (from 3 ng / ml), the elimination of the substance is slow, mostly linear, with a half-life of 3-5 weeks.
Tamsulosin:
    absorption: occurs in the intestine, the bioavailability of tamsulosin is almost 100%. It is characterized by linear pharmacokinetics after single / repeated use with the achievement of stable concentrations on the fifth day when taken once a day. After a meal, a slowdown in the rate of absorption is observed. The same level of absorption can be achieved when the patient takes tamsulosin every day after the same meal after about 30 minutes;
    Distribution: Tamsulosin is distributed in the extracellular fluid of the body. For the most part (from 94 to 99%) it binds to human blood plasma proteins, mainly to α1-acid glycoprotein. Binding is linear over a wide concentration range (20 to 600 ng / ml);
    metabolism: no enantiomeric bioconversion of tamsulosin from the R (-) isomer to the S (+) isomer is observed. Tamsulosin is extensively metabolized by isoenzymes of the cytochrome P450 system in the liver, and less than 10% of the dose is excreted by the kidneys unchanged. The pharmacokinetic profile of metabolites has not been determined. According to available data, CYP3A4 and CYP2D6 isoenzymes are involved in the metabolism of tamsulosin, and there is also a small participation of other cytochrome P450 isoenzymes. Inhibition of the activity of liver enzymes that are involved in the metabolism of tamsulosin can lead to an increase in its exposure. Before excretion by the kidneys, tamsulosin metabolites undergo intensive conjugation with sulfates or glucuronides;
    Elimination: the half-life of tamsulosin varies from 5 to 7 hours. Approximately 10% of tamsulosin is excreted unchanged by the kidneys.

Indications for use

Duodart is prescribed for the treatment and prevention of BPH progression, which is achieved by reducing its size, eliminating symptoms, increasing urination rate, reducing the likelihood of acute urinary retention and the need for surgery.

Contraindications

Absolute:
    severe liver failure;
    orthostatic hypotension (including a burdened history);
    age under 18;
    individual intolerance to the components of the drug, as well as other 5α-reductase inhibitors.
In addition, the drug is not prescribed to female patients.
Relative (diseases / conditions in which the appointment of Duodart requires caution):
    chronic renal failure (with creatinine clearance below 10 ml / min);
    planned cataract surgery;
    arterial hypotension;
    combined use with powerful / moderately active inhibitors of the isoenzyme CYP3A4 - ketoconazole, voriconazole and others.

Instructions for the use of Duodart: method and dosage

Duodart is taken orally, preferably 30 minutes after the same meal.
The capsules must be taken whole with water, without opening or chewing. When the contents of a soft gelatin capsule inside the hard shell come into contact with the oral mucosa, inflammation from the mucous membrane may develop.
The recommended dosing regimen of Duodart for adult men (including elderly patients): 1 capsule 1 time per day.

Side effects

Estimation of the incidence of side effects:> 10% - very often; > 1% and <10% - often; > 0.1% and <1% - infrequently; > 0.01% and <0.1% - rarely; <0.01% - very rare.
Disorders observed with the use of dutasteride as monotherapy:
    rarely: hypertrichosis, alopecia (manifests itself mainly in the form of hair loss on the body);
    very rare: swelling / pain in the testicular area, depression.
Violations observed with the use of tamsulosin hydrochloride as monotherapy:
    often: ejaculation disorder, dizziness;
    infrequently: constipation, vomiting, diarrhea, heart palpitations, asthenia, urticaria, rhinitis, pruritus, rash, postural hypotension;
    rarely: angioedema, loss of consciousness;
    very rare: Stevens-Johnson syndrome, priapism.
When carrying out combination therapy, in very rare cases, the development of the following disorders is observed: dizziness, breast tenderness, impotence, ejaculation disorders, decreased libido, gynecomastia.
Sexual disorders are caused by dutasteride and may persist after discontinuation.
According to the results of post-registration observations, in some patients who received alpha1-blockers, including tamsulosin hydrochloride, intraoperative atonic iris syndrome is observed during cataract surgeries.
Also, while taking tamsulosin, cases of atrial fibrillation, arrhythmias, dyspnea and tachycardia were identified. It is impossible to estimate the frequency of occurrence of these disorders; the connection with the drug intake has not been established.

Overdose

There is no information regarding an overdose while taking Duodart.
Dutasteride:
    main symptoms: violations in case of an overdose of a substance, other than the described adverse reactions, do not develop;
    therapy: there is no specific antidote, in cases of suspicion of an overdose, symptomatic / supportive treatment is recommended.
Tamsulosin:
    the main symptom: acute arterial hypotension;
    therapy: symptomatic treatment is shown, including the adoption by patients of a horizontal position, if necessary, the use of drugs that increase the volume of circulating blood, and drugs with a vasoconstrictor effect. Monitoring and, if necessary, maintenance of renal function is required. Dialysis is unlikely to be effective.

Special instructions

Dutasteride can be absorbed through the skin, therefore, women and children are advised to avoid contact with damaged capsules, if necessary, wash the corresponding area of ​​the skin with soap and water.
With the combined use of Duodart with strong inhibitors of the CYP3A4 isoenzyme (ketoconazole) or, to a lesser extent, with strong inhibitors of the CYP2D6 isoenzyme (paroxetine), an increase in tamsulosin exposure may be observed. In this regard, tamsulosin is not recommended for patients taking strong inhibitors of the isoenzyme CYP3A4, and should be used with caution in patients who are taking moderate-strength inhibitors of the isoenzyme CYP3A4 (erythromycin), strong / medium-strength inhibitors of the isoenzyme CYP2D6, a combination of inhibitors of CYP3D6 isoenzymes, or known low metabolic rate of CYP2D6.
Patients with prostatic hyperplasia, before the appointment of Duodart and periodically during the period of therapy, need to undergo a digital rectal examination and use other methods for diagnosing prostate cancer (prostate cancer).
Serum PSA (prostate specific antigen) levels are an important component of screening for prostate cancer. After 6 months of therapy, the mean serum PSA level usually decreases by 50%.
After 6 months of therapy, the patient should have a new baseline PSA level. After that, it was recommended to conduct regular monitoring of its level. Any confirmed increase in this indicator relative to its lowest value during treatment with Duodart may be evidence of non-compliance with the therapy regimen or the development of prostate cancer (in particular, prostate cancer with a high degree of Gleason differentiation).
During the use of Duodart, orthostatic hypotension may develop, which in rare cases can lead to fainting. At the beginning of treatment, patients should be warned about this and know what measures should be taken (sit or lie down when the first signs appear - dizziness and imbalance). It must be borne in mind that combined use with phosphodiesterase type 5 inhibitors can potentially lead to symptomatic hypotension.
According to the instructions, Duodart should be canceled 1–2 weeks before surgery for cataract, however, the benefits, as well as the time period for discontinuation of therapy before surgery, have not been established.
A causal relationship between Duodart's intake and the development of high grade PCa has not been established. During the period of therapy, it is necessary to regularly conduct examinations to assess the likelihood of prostate cancer, including the PSA level.
There is information about the occurrence of breast cancer in men taking dutasteride (the connection with taking the drug has not been confirmed). For any changes in the mammary glands - lumps in the gland or discharge from the nipple, you should consult a specialist.

Influence on the ability to drive vehicles and complex mechanisms

When driving, take into account the likelihood of orthostatic hypotension and associated symptoms, including dizziness.

Application during pregnancy and lactation

It is contraindicated for women to take Duodart.

Childhood use

Duodart is contraindicated in pediatric patients.

With impaired renal function

The use of Duodart with creatinine clearance below 10 ml / min requires caution.

For violations of liver function

Severe liver failure is a contraindication to the use of Duodart.

Drug interactions

Studies to study the interaction of Duodart with other drugs have not been conducted. The information below reflects the information available for its components.

Possible interactions of dutasteride

Dutasteride is metabolized by the CYP3A4 isoenzyme of the cytochrome P450 enzyme system, and therefore the concentration of dutasteride in the blood in the presence of inhibitors of the CYP3A4 isoenzyme may increase.
When combined with verapamil and diltiazem, a significant decrease in the clearance of dutasteride was noted. In this case, amlodipine has no effect on the clearance of dutasteride.
Such changes have no clinical significance and do not require dose adjustment.

Possible interactions of tamsulosin

    drugs leading to a decrease in blood pressure, including type 5 phosphodiesterase inhibitors, anesthetics and other alpha1-blockers: the likelihood of an increase in the hypotensive effect of tamsulosin; the combination with other alpha1-blockers is not recommended;
    ketoconazole, paroxetine: significant increase in Cmax and AUC of tamsulosin;
    cimetidine: decrease in clearance and increase in AUC of tamsulosin (combination requires caution);
    warfarin: no data on interaction (combination requires caution).

Terms and conditions of storage

Store at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life is 2 years.

Reviews about Duodart

There are few reviews about Duodart, testifying to its effectiveness. It is also noted that the drug is relatively new, so it often raises questions from patients regarding possible side effects and the time when the full effect of therapy can be noted.

Terms of sell

You can buy Duodart without a prescription from a doctor.