Alphascar

Finasteride.

Each film-coated tablet contains 5 mg of finasteride.
Excipients/Inactive Ingredients: Cellactose 80, microcrystalline cellulose, pregelatinized starch, sodium starch glycolate, sodium lauryl sulfate, magnesium stearate, Opadry03F40519*, purified water.
* Opadry03F40519: HPMC 2910 / hypromellose, titanium dioxide, macrogol / PEG, FD&C Blue #2 / indigo carmine aluminum lake, FD&C Blue #1 / brilliant blue FCF aluminum lake, FD&C Yellow #6 / sunset yellow FCF aluminum lake.

Alphascar Tablets 5mg is indicated for the treatment and control of benign prostatic hyperplasia (BPH) in patients with an enlarged prostate to: cause regression of the enlarged prostate, improve urinary flow and improve the symptoms associated with BPH; reduce the incidence of acute urinary retention and the need for surgery including transurethral resection of the prostate (TURP) and prostatectomy.

Posology: The recommended adult dose is one 5 mg tablet daily, with or without food.
Finasteride can be administered alone or in combination with the alpha-blocker doxazosin.
Although early improvement in symptoms may be seen, treatment for at least six months may be necessary to assess whether a beneficial response has been achieved. The risk of acute urinary retention is reduced within four months of treatment.
Dosage in the elderly: Dosage adjustments are not necessary although pharmacokinetic studies have shown that the elimination rate of finasteride is slightly decreased in patients over the age of 70.
Dosage in hepatic insufficiency: The effect of hepatic insufficiency on the pharmacokinetics of finasteride has not been studied.
Dosage in renal insufficiency: No adjustment in dosage is required in patients with varying degrees of renal insufficiency (creatinine clearances as low as 9 mL/min), as pharmacokinetic studies did not indicate any change in the disposition of finasteride.
Paediatric population: Finasteride is contraindicated in children.
Method of administration: Finasteride is for oral use only.

Patients have received single doses of finasteride up to 400 mg and multiple doses of finasteride up to 80 mg/day for up to three months without any adverse effects.
No specific treatment of overdosage with finasteride is recommended.

Finasteride is not indicated for use in women or children.
Finasteride is contraindicated in the following: Hypersensitivity to the active substance or to any of the excipients; Pregnancy (use in women when they are or may potentially be pregnant).

General: Patients with large residual urine and/or severely diminished urinary flow should be carefully monitored for obstruction uropathy.
Consultation of a urologist should be considered in patients treated with finasteride.
Obstruction due to trilobular growth pattern of the prostate should be excluded before starting treatment with finasteride.
To avoid obstructive complications, it is important that patients with large residual urine and/or heavily decreased urinary flow are carefully controlled.
The possibility of surgery should be an option.
Erectile dysfunction, male infertility and decreased libido: Erectile dysfunction (ED) that continued after discontinuation of treatment, reported rarely in men taking finasteride for the treatment of BPH. Most men were older and were taking concomitant medications and/or had co-morbid conditions with a known association to ED. The independent role of Alphascar in these events is unknown.
Male infertility and/or poor seminal quality have been reported rarely in men taking finasteride for the treatment of BPH. The independent role of Alphascar in these events is unknown. Normalization or improvement of seminal quality has been reported after discontinuation of finasteride.
Decreased libido that continued after discontinuation of treatment.
Effects on prostate-specific antigen (PSA) and prostate cancer detection: No clinical benefit has yet been demonstrated in patients with prostate cancer treated with finasteride. Patients with BPH and elevated PSA were monitored in controlled clinical studies with serial PSAs and prostate biopsies. In these BPH studies, finasteride did not appear to alter the rate of prostate cancer detection and the overall incidence of prostate cancer was not significantly different in patients treated with finasteride or placebo.
Digital rectal examination, as well as other evaluations for prostate cancer, should be performed on patients with BPH prior to initiating therapy with finasteride and periodically thereafter. Serum PSA is also used for prostate cancer detection. Generally, a baseline PSA >10 ng/mL (Hybritech) prompts further evaluation and consideration of biopsy; for PSA levels between 4 and 10 ng/mL, further evaluation is advisable. There is considerable overlap in PSA levels among men with and without prostate cancer. Therefore, in men with BPH, PSA values within the normal reference range do not rule out prostate cancer regardless of treatment with finasteride. A baseline PSA <4 ng/mL does not exclude prostate cancer.
Finasteride causes a decrease in serum PSA concentrations by approximately 50% in patients with BPH, even in the presence of prostate cancer. This decrease in serum PSA levels in patients with BPH treated with finasteride should be considered when evaluating PSA data and does not rule out concomitant prostate cancer. This decrease is predictable over the entire range of PSA values, although it may vary in individual patients. In patients treated with finasteride for six months or more, PSA values should be doubled for comparison with normal ranges in untreated men. This adjustment preserves the sensitivity and specificity of the PSA assay and maintains its ability to detect prostate cancer.
Any sustained increase in PSA levels of patients treated with finasteride should be carefully evaluated, including consideration of non-compliance to therapy with finasteride.
Percent free PSA (free to total PSA ratio) is not significantly decreased by finasteride and remains constant even under the influence of finasteride. When percent free PSA is used as an aid in the detection of prostate cancer, no adjustment to its value is necessary.
Prostate cancer: Use of the product may increase the risk of high-grade prostate cancer. The product is not approved for the prevention of prostate cancer.
Drug/laboratory test interactions: Effect on levels of PSA: Serum PSA concentration is correlated with patient age and prostatic volume, and prostatic volume is correlated with patient age. When PSA laboratory determinations are evaluated, consideration should be given to the fact that PSA levels decrease in patients treated with finasteride. In most patients, a rapid decrease in PSA is seen within the first months of therapy, after which time PSA levels stabilize to a new baseline. The post-treatment baseline approximates half of the pre-treatment value. Therefore, in typical patients treated with finasteride for six months or more, PSA values should be doubled for comparison to normal ranges in untreated men.
Percent free PSA (free to total PSA ratio) is not significantly decreased by finasteride. The ratio of free to total PSA remains constant even under the influence of finasteride. When percent free PSA is used as an aid in the detection of prostate cancer, no adjustment to its value is necessary.
Breast cancer in men: Breast cancer has been reported in men taking finasteride 5 mg during clinical trials. Post-marketing cases of male breast cancer have been reported with the use of finasteride. Physicians should instruct their patients to promptly report any changes in their breast tissue such as lumps, pain, gynaecomastia or nipple discharge.
Mood alterations and depression: Mood alterations including depressed mood, depression and, less frequently, suicidal ideation have been reported in patients treated with finasteride 5 mg. Patients should be monitored for psychiatric symptoms and if these occur, the patient should be advised to seek medical advice.
Lactose: The tablet contains lactose monohydrate. Patients with any of the following genetic deficiencies should not take this medicine: galactose intolerance, total lactase deficiency or glucose-galactose malabsorption.
Hepatic insufficiency: The effect of hepatic insufficiency on the pharmacokinetics of finasteride has not been studied.
Effects on ability to drive and use machines: There are no data to suggest that finasteride affects the ability to drive or use machines.
Use in Pregnancy: Women who are pregnant or may become pregnant should not handle crushed or broken finasteride tablets because of the possibility of absorption of finasteride and the subsequent potential risk to a male foetus. Finasteride tablets have a film-coating which prevents contact with the active ingredient provided that the tablets have not been broken or crushed.
Use in Children: Finasteride is not indicated for use in children. Safety and effectiveness in children have not been established.

Pregnancy: Finasteride is contraindicated for use in women when they are or may potentially be pregnant (see Contraindications).
Because of the ability of Type II 5α-reductase inhibitors to inhibit conversion of testosterone to dihydrotestosterone, these medicinal products, including finasteride, may cause abnormalities of the external genitalia of a male foetus when administered to a pregnant woman.
In animal developmental studies, dose-dependent development of hypospadias were observed in the male offspring of pregnant rats given finasteride at doses ranging from 100 μg/kg/day to 100 mg/kg/day, at an incidence of 3.6% to 100%. Additionally, pregnant rats produced male offspring with decreased prostatic and seminal vesicular weights, delayed preputial separation, transient nipple development and decreased anogenital distance, when given finasteride at doses below the recommended human dose. The critical period during which these effects can be induced has been defined in rats as days 16-17 of gestation.
The changes previously described are expected pharmacological effects of Type II 5α-reductase inhibitors. Many of the changes, such as hypospadias, observed in male rats exposed in utero to finasteride are similar to those reported in male infants with a genetic deficiency of Type II 5α-reductase. It is for these reasons that finasteride is contraindicated in women who are or may potentially be pregnant.
No effects were seen in female offspring exposed in utero to any dose of finasteride.
Exposure to finasteride - risk to male foetus: Women should not handle crushed or broken tablets of finasteride when they are or may potentially be pregnant because of the possibility of absorption of finasteride and the subsequent potential risk to a male foetus (see Pregnancy as previously mentioned). Finasteride tablets are coated and will prevent contact with the active ingredient during normal handling, provided that the tablets have not been broken or crushed.
Small amounts of finasteride have been recovered from the semen in subjects receiving finasteride 5 mg/day. It is not known whether a male foetus may be adversely affected if his mother is exposed to the semen of a patient being treated with finasteride. When the patient's sexual partner is or may potentially be pregnant, the patient is recommended to minimise exposure of his partner to semen.
Breast-feeding: Finasteride is not indicated for use in women. It is not known whether finasteride is excreted in human milk.

The most frequent adverse reactions are impotence and decreased libido. These adverse reactions occur early in the course of therapy and resolve with continued treatment in the majority of patients.
The adverse reactions reported during clinical trials and/or post-marketing use with finasteride and/or finasteride at lower doses are listed in the following table. (See table.)
Frequency of adverse reactions is determined as follows: Very common (≥1/10), Common (≥1/100 to <1/10), Uncommon (≥1/1,000 to <1/100), Rare (≥1/10,000 to <1/1,000), Very rare (<1/10,000), Not known (cannot be estimated from the available data).
The frequency of adverse reactions reported during post-marketing use cannot be determined as they are derived from spontaneous reports.

Click on icon to see table/diagram/image

In addition, the following has been reported in clinical trials and post-marketing use: male breast cancer (see Precautions).
Medical Therapy of Prostatic Symptoms (MTOPS): The MTOPS study compared finasteride 5 mg/day (n=768), doxazosin 4 or 8 mg/day (n=756), combination therapy of finasteride 5 mg/day and doxazosin 4 or 8 mg/day (n=786), and placebo (n=737). In this study, the safety and tolerability profile of the combination therapy was generally consistent with the profiles of the individual components. The incidence of ejaculation disorder in patients receiving combination therapy was comparable to the sum of incidences of this adverse experience of the two monotherapies.
Other Long-Term Data: In a 7-year placebo-controlled trial that enrolled 18,882 healthy men, of whom 9060 had prostate needle biopsy data available for analysis, prostate cancer was detected in 803 (18.4%) men receiving finasteride and 1147 (24.4%) men receiving placebo. A greater number of high-grade tumours (Gleason scores of 7-10) were detected on needle biopsy in patients in the finasteride group, 280 (6.4%) vs 237 (5.1%) men in the placebo group.
Additional analyses suggest that the increase in the prevalence of high-grade prostate cancer observed in the finasteride group may be explained by a detection bias due to the effect of finasteride on prostate volume. Of the total cases of prostate cancer diagnosed in this study, approximately 98% were classified as intracapsular (stage T1 or T2). The relationship between long-term use of finasteride and tumours with Gleason scores of 7-10 is unknown.
Laboratory Test Findings: Serum PSA concentration is correlated with patient age and prostatic volume, and prostatic volume is correlated with patient age. When PSA laboratory determinations are evaluated, consideration should be given to the fact that PSA levels are decreased in patients treated with finasteride (see Precautions). In most patients, a rapid decrease in PSA is seen within the first months of therapy, after which time PSA levels stabilise to a new baseline. The post-treatment baseline approximates half of the pre-treatment value. Therefore, in typical patients treated with finasteride for six months or more, PSA values should be doubled for comparison to normal ranges in untreated men.
For clinical interpretation, see Effects on prostate-specific antigen (PSA) and prostate cancer detection under Precautions.
No other difference was observed in patients treated with placebo or finasteride in standard laboratory tests.

No drug interactions of clinical importance have been identified. Finasteride is metabolized primarily via, but does not appear to affect significantly, the cytochrome P450 3A4 system. Although the risk for finasteride to affect the pharmacokinetics of other medicinal products is estimated to be small, it is probable that inhibitors and inducers of cytochrome P450 3A4 will affect the plasma concentration of finasteride. However, based on established safety margins, any increase due to concomitant use of such inhibitors is unlikely to be of clinical significance. Compounds which have been tested in man have included propranolol, digoxin, glibenclamide, warfarin, theophylline, and phenazone and no clinically meaningful interactions were found.

Incompatibilities: Not applicable.

Shelf life: 3 years.

Drugs for Bladder & Prostate Disorders

G04CB01 - finasteride ; Belongs to the class of testosterone-5-alpha reductase inhibitors. Used in the treatment of benign prostatic hypertrophy.

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