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PROS-D

Generic Name:                    Dutasteride

Therapeutic Category:     Benign Prostatic Hyperplasia Agents

Pharmacological Class:  Type I and II 5 alpha-reductase inhibitor

Composition:                      Each film coated tablet contains Dutasteride IP 0.5 mg Tablet

Pregnancy Category:        X

Presentation:                      Available in the pack size as 14 tablets X 2 blisters

What is Pros-D and what is it used for?

Pros-D contains Dutasteride 0.5 mg in tablet form and belongs to a group of medicines called 5-alpha reductase inhibitors.

It is used to treat men with an enlarged prostate (benign prostatic hyperplasia) – a non-cancerous growth of the prostate gland, caused by producing too much of a hormone called dihydrotestosterone. As the prostate grows, it can lead to urinary problems, such as difficulty in passing urine and a need to go to the toilet frequently. It can also cause the flow of the urine to be slower and less forceful. If left untreated, there is a risk that your urine flow will be completely blocked (acute urinary retention). This requires immediate medical treatment. In some situations surgery is necessary to remove or reduce the size of the prostate gland.

It is also used to treat male pattern baldness.

How does it work?

Pros-D belongs to the group of medicines, called 5-alpha reductase inhibitors. They act by reducing the size of the prostate gland in men. It is used in the treatment and control of benign enlargement of the prostate (benign prostatic hyperplasia – BPH). It helps improve urinary flow and may also reduce your need for prostate surgery later on.

How to take Pros-D?

The recommended dose is one capsule (0.5 mg) taken once a day. Swallow the capsules whole with water. Do not chew or break open the capsule. Contact with the contents of the capsules may make your mouth or throat sore. Pros-D is a long-term treatment. Some men notice an early improvement in their symptoms. However, others may need to take this medicine for 6 months or more before it begins to have an effect. Keep taking it for as long as your doctor tells you.

What if you miss a dose?

If you have missed a dose, just take your daily tablet on the next day at the usual time. Do not take two tablets to make up for a forgotten capsule.

What to do in case of overdose?

If you take more of this medicine than you should, talk to a doctor or pharmacist straight away.

What do you need to know before you take Pros-D?

Do not take Pros-D:

·         if you are allergic to dutasteride, other 5-alpha reductase inhibitors, soya, peanut or to any of the other ingredients of this medicine

·         if you have a severe liver disease

·         if you are younger than 18 years old and a woman.

Warnings and Precautions

Talk to your doctor before taking Pros-D

·         Make sure your doctor knows about liver problems. If you have had any illness affecting your liver, you may need some additional check-ups while you are taking Pros-D

·         Women, children and adolescents must not handle leaking Pros-D, because the active ingredient can be absorbed through the skin. Wash the affected area immediately with soap and water if there is any contact with the skin.

·         Use a condom during sexual intercourse. Dutasteride has been found in the semen of men taking Pros-D. If your partner is or may be pregnant, you must avoid exposing her to your semen as dutasteride may affect the normal development of a male baby. Dutasteride has been shown to decrease sperm count, semen volume and sperm motility. This could reduce your fertility.

·         Pros-D affects a blood test for PSA (prostate-specific antigen), which is sometimes used to detect prostate cancer. Your doctor should be aware of this effect and can still use the test to detect prostate cancer. If you are having a blood test for PSA, tell your doctor that you are taking Pros-D. Men taking Pros-D should have their PSA tested regularly.

·         In a clinical study of men at increased risk of prostate cancer, men taking Pros-D had a serious form of prostate cancer more often than men who did not take Pros-D. The effect of this medicine on this serious form of prostate cancer is not clear.

·         Pros-D may cause breast enlargement and tenderness. If this becomes troublesome, or if you notice breast lumps or nipple discharge you should talk to your doctor about these changes as these may be signs of a serious condition, such as breast cancer.

Pros-D and other medications

Tell your doctor or pharmacist if you are taking, have recently taken or might take any medicines

·         to lower your blood pressure such as verapamil and diltiazem

·         Medicines to treat HIV such as ritonavir or indinavir

·         Medicines to treat a fungal infection such as ketoconazole or itraconazole

·         Other alpha-blockers such as doxazosin, indoramin, prazosin, or alfuzosin

·         Erythromycin, an antibiotic used to treat infections

Tell your doctor or dentist that you are on Pros-D before any operation or dental procedure as there is a potential that your medicine may interfere with the effects of the anaesthetic.

Pregnancy and breast-feeding

Pregnancy

Pros-D must not be administered by pregnant women.  Also, women who are pregnant (or may be) must not handle leaking capsules. Dutasteride is absorbed through the skin and can affect the normal development of a male baby. This is a particular risk in the first 16 weeks of pregnancy.

Breast-feeding

Intake of Pros-D is not recommended in lactating mothers.

Driving and using machines

Pros-D is unlikely to affect your ability to drive or operate machinery.

Pros-D and other medicines

Tell your doctor if you are taking, have recently taken, or might take any other medicines.

Some medicines can react with this medication and may make it more likely that you’ll have side-effects. These medicines include:

• verapamil or diltiazem (for high blood pressure)

• ritonavir or indinavir (for HIV)

• itraconazole or ketoconazole (for fungal infections)

• nefazodone (an antidepressant)

• alpha-blockers (for enlarged prostate or high blood pressure).

What are the possible side effects?

Common side effects are:

·         not able to achieve or maintain an erection (impotence)

·         decreased sex drive (libido), this may continue after you stop taking Avodart

·         difficulty with ejaculation, such as a decrease in the amount of semen released during sex,  breast enlargement or tenderness (gynecomastia)

·         dizziness when taken with tamsulosin(Prostam 0.4)

Mechanism of action:

Prostate growth is caused by a hormone in the blood called dihydrotestosterone (DHT). Dutasteride 0.5 mg inhibits both Type 1 and 2 5- alpha reductase enzymes. Dutasteride lowers DHT production in the body, leading to shrinkage of the enlarged prostate in most men. While some men have fewer problems and symptoms after 3 months of treatment with Dutasteride, a treatment period of at least 6 months is usually necessary to see if Dutasteride will work. Studies have shown that treatment with Dutasteride for 2 years reduces the risk of complete blockage of urine flow (acute urinary retention) and/or the need for surgery for benign prostatic hyperplasia (BPH).

Pharmacokinetic properties:

Absorption:  Following oral administration of a single dose of 0.5 mg dutasteride, the peak serum concentrations were reached within 2 to 3 hours. In healthy subjects, the absolute bioavailability was 60%, ranging from 40% to 94%. While food intake reduced the maximum serum concentrations by 10 to 15%, food intake is reported to have a negligible effect on the bioavailability of the drug.

Volume of Distribution: Dutasteride displays a large volume of distribution ranging from 300 to 500 L.

Protein Binding: Dutasteride is about 99% bound to albumin and 96.6% bound to α-1 acid glycoprotein in the serum.

Metabolism:  Dutasteride undergoes extensive hepatic metabolism mediated by CYP3A4 and CYP3A5.

Excretion: Dutasteride and its metabolites mainly undergo fecal excretion. About 1-15% of the dose is excreted as the unchanged parent compound, while 2-90% of the total dose is excreted in the form of dutasteride-related metabolites in the feces.

Elimination Half-life:  The terminal elimination half-life of dutasteride is approximately 5 weeks at steady state.

Clearance: In a study of healthy volunteers receiving single oral doses of dutasteride ranging from 0.01 to 40 mg, dutasteride displayed a low linear clearance of 0.58 L/h.

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