Duodart
Duodart: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Duodart
ATX code: G04CA52
Active ingredient: Tamsulosin (Tamsulosin), Dutasteride (Dutasteride)
Producer: GlaxoSmithKline Trading CJSC (Russia)
Description and photo update: 2018-27-07
Prices in pharmacies: from 1207 rubles.
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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 Duodart - hard capsules from hypromellose: oblong, size No. 00; body - brown, lid - orange with black ink marking "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 reduce DHT levels, reduce the size of the prostate gland, reduce the severity of symptoms of lower urinary tract diseases 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 mean serum DHT concentrations in the blood decrease by 85% and 90%, respectively;
- tamsulosin: helps to increase the maximum urinary flow rate by decreasing the tone of the smooth muscles 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: C max in serum after taking 0.5 mg of dutasteride is achieved within 1-3 hours. The absolute bioavailability in men is about 60% relative 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. C ss in serum and semen, equal to approximately 40 ng / ml, are 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 isoenzyme CYP3A4 of the cytochrome P 450 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 an 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 excretion 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 eating, there is a slowdown in the rate of absorption. 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. Most (from 94 to 99%) 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 P 450 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, the isoenzymes CYP3A4 and CYP2D6 are involved in the metabolism of tamsulosin, there is also a small participation of other cytochrome P 450 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 are intensively conjugated 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 up to 18 years;
- 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, located inside the hard shell, come into contact with the mucous membrane of the oral cavity, inflammatory phenomena 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 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare.
Violations observed when using 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 when using 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 withdrawal.
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 when taking Duodart.
Dutasteride:
- main symptoms: disorders 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 affected 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 prescribed with caution in patients who are taking medium-strength inhibitors of the isoenzyme CYP3A4 (erythromycin), strong / medium-strength inhibitors of the isoenzyme CYP2D6, a combination of inhibitors of isoenzyme CYP3D6, or known low metabolic rate of CYP2D6.
Patients with prostatic hyperplasia, before the appointment of Duodart and periodically during the period of therapy, need a digital rectal examination and 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 indicate non-adherence to the therapy regimen or the development of prostate cancer (in particular, prostate cancer with a high degree of differentiation on the Gleason scale).
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 should 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 discontinued 1–2 weeks before cataract surgery, 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.
Pediatric use
Duodart is contraindicated for 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 P 450 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 C max 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).
Analogs
There is no information about the analogues of Duodart.
Terms and conditions of storage
Store at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
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.
Price for Duodart in pharmacies
The price for Duodart (1 bottle) is approximately: 30 capsules - 1570 rubles, 90 capsules - 3500 rubles.
Duodart: prices in online pharmacies
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Drug name Price Pharmacy |
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Duodart 0.5 mg + 0.4 mg modified release capsules 30 pcs. 1207 RUB Buy |
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Duodart capsules with modif. release 0.5mg + 0.4mg 30 pcs. 1658 RUB Buy |
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Duodart 0.5 mg + 0.4 mg modified release capsules 90 pcs. RUB 2599 Buy |
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Duodart capsules with modif. release 0.5mg + 0.4mg 90 pcs. 3619 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
