Tamsulosin Hydrochloride MR 0.4 mg and Dutasteride 0.5 mg Capsules
Composition of Flomax D 0.4mg/0.5mg Tablet:
Each hard gelatin capsule contains: Tamsulosin Hydrochloride BP 0.4 mg (As Modified Release Pellets)
Dutasteride BP 0.5 mg (As Pellets)
Excipients Q.S.
Approved colours used in empty capsule shells & pellets.
Pharmaceutical form:
Capsule
Therapeutic indications for Flomax D 0.4mg/0.5mg Tablet
Treatment of moderate to severe symptoms of benign prostatic hyperplasia (BPH). Reduction in the risk of acute urinary retention (AUR) and surgery in patients with moderate to severe symptoms of BPH.
Posology and method of administration:
Posology:
Adults (including elderly) – The recommended dose of Prostatin is one capsule (0.5 mg/ 0.4 mg) once daily.
Method of administration:
- Oral use.
Contraindications:
- Patients with a history of orthostatic hypotension. – Patients with severe hepatic impairment.
Special warnings and precautions for use of Flomax D 0.4mg/0.5mg Tablet:
Breast neoplasia
There have been rare reports of male breast cancer reported in men taking dutasteride in clinical trials and during the post-marketing period. However, epidemiological studies showed no increase in the risk of developing male breast cancer with the use of 5-alpha reductase inhibitors. Physicians should instruct their patients to promptly report any changes in their breast tissue such as lumps or nipple discharge.
Interaction with other medicinal products and other forms of interaction:
Effects of other drugs on the pharmacokinetics of dutasteride
Dutasteride is mainly eliminated via metabolism. In vitro studies indicate that this metabolism is catalysed by CYP3A4 and CYP3A5. No formal interaction studies have been performed with potent CYP3A4 inhibitors. However, in a population pharmacokinetic study, dutasteride serum concentrations were on average 1.6 to 1.8 times greater, respectively, in a small number of patients treated concurrently with verapatnil or diltiazem (moderate inhibitors of CYP3A4 and inhibitors of P-glycoprotein) than in other patients.
Tamsulosin
Concomitant administration of tamsulosin hydrochloride with drugs which can reduce blood pressure, including anaesthetic agents, PDE5 inhibitors and other alpha,- adrenoceptor antagonists could lead to enhanced hypotensive effects. Dutasteride-tamsulosin should not be used in combination with other alpha, – adrenoceptor antagonists.
Pregnancy and lactation:
Pregnancy
As with other 5 alpha reductase inhibitors, dutasteride inhibits the conversion of testosterone to dihydrotestosterone and may, if administered to a woman carrying a male foetus, inhibit the development of the external genitalia of the foetus.
Lactation
It is not known whether dutasteride or tamsulosin are excreted in human milk.
Fertility
Dutasteride has been reported to affect semen characteristics (reduction in sperm count, semen volume, and sperm motility) in healthy men. The possibility of reduced male fertility cannot be excluded. Effects of tamsulosin hydrochloride on sperm counts or sperm function have not been evaluated.
Undesirable effects:
Dutasteride
Not known: Allergic reactions, including rash, pruritus, urticaria, localised oedema, and angioedema.
Overdose:
No data are available with regard to overdosage of Prostatin.
Pharmacological properties:
Pharmacodynamic properties:
Pharmacotherapeutic group: Alpha-adrenoreceptor antagonists, ATC code: G04CA52 Dutasteridetamsulosin is a combination of two drugs: dutasteride, a dual 5 a-reductase inhibitor (5 ARI) and tamsulosin hydrochloride, an antagonist of ar.and adrenoreceptors. These drugs have complementary mechanisms of action that rapidly improve symptoms, urinary flow and reduce the risk of acute urinary retention (AUR) and the need for BPH related surgery.
Pharmacokinetic properties:
Absorption: Dutasteride
Following oral administration of a single 0.5 mg dutasteride dose, the time to peak serum concentrations of utasteride is 1 to 3 hours. The absolute bioavailability is approximately 60%. The bioavailability of dutasteride is not affected by food.
Tamsulosin
Tamsulosin is absorbed from the intestine and is almost completely bioavailable. Both the rate and extent of absorption of tamsulosin are reduced when taken within 30 minutes of a meal. Uniformity of absorption can be promoted by the patient always taking Prostatin after the same meal. Tamsulosin shows dose proportional plasma exposure.
Distribution: Dutasteride
Dutasteride has a large volume of distribution (300 to 500 L) and is highly bound to plasma proteins (>99.5%). Following daily dosing, dutasteride serum concentrations achieve 65% of steady state concentration after 1 month and approximately 90% after 3 months.
Tamsulosin
In man tamsulosin is about 99% bound to plasma proteins. The volume of distribution is small(about 0.21/kg). Biotransformation:
Dutasteride
Dutasteride is extensively metabolised in vivo. In vitro, dutasteride is metabolised by the cytocbrome P450 3A4 and 3A5 to three monohydroxylated metabolites and one dihydroxylated metabolite.
Tamsulosin
There is no enantiomeric bioconversion from tamsulosin hydrochloride [R(-) isomer] to the S(+) isomer in humans.
Elimination: Dutasteride
The elimination of dutasteride is dose dependent and the process appears to be described by two elimination pathways in parallel, one that is saturable at clinically relevant concentrations and one that is non saturable. Tamsulosin
Tamsulosin and its metabolites are mainly excreted in the urine.
Special precautions for storage:
Store below 30°C. Protect from light and moisture. Keep the medicine out of reach of children. Presentation: 30 Capsules
Marketed by:
PYXUS PHARMACEUTICALS PVT. LTD.
