Urototal tablets (Propecia) is a drug used to treat male pattern baldness. Side effects, drug interactions, dosage, storage, and safety information should be reviewed prior to taking this medication.
What is Urototal (Proscar)? How does it work (mechanism of action)?
The prostate gland is located around the tube which empties urine from the bladder (urethra). As the prostate gland enlarges, usually after 50 years of age, it can obstruct or partially block the urine flow. This leads to symptoms which include dribbling of urine, narrow stream, problems starting urine flow, interruption while urinating, and a feeling of incomplete emptying. Other symptoms include wetting and staining of clothes, urinary burning, and urgency.
Prostate gland enlargement (benign prostatic hyperplasia or BPH), is directly dependent on DHT (a hormone converted from the male hormone testosterone). Urototal inhibits the enzyme necessary for the conversion of testosterone to DHT in the prostate. Therefore, administration of Urototal lowers blood and tissue DHT levels and helps reduce the size of the prostate gland.
Although reductions in the size of the prostate gland can occur in virtually all the patients who take Urototal, only 50% will experience improvement in the symptoms of BPH. Patients generally respond to Urototal in several weeks, but it often takes 6 months for the patient to receive the full effect of the drug.
What are the side effects of Urototal-oral (hair growth)?
The most common side effects associated with Urototal are:
Serious side effects include increased risk of high-grade prostate cancer, and increased risk for male breast cancer.
Propecia (1 mg Urototal) was approved by the FDA for the treatment of male pattern baldness in December 1997. Another Urototal oral dosage form, Proscar or 5 mg Urototal tablets are FDA approved only for the treatment of benign prostatic hyperplasia (BPH) and should not be used for androgenetic alopecia. Do not confuse these Urototal tablets.
Urototal hides higher-grade cancer
The trouble with Urototal dates back to 2003 when the original article was published in the New England Journal of Medicine. The authors of that article studied 18,000 men who randomly were assigned to receive either 5 mg of Urototal (then used mainly to treat benign enlargement of the prostate) or a placebo.
The men in the Urototal group had a 25 percent lower risk of being diagnosed with prostate cancer, but a 68 percent higher risk of being diagnosed with a high-grade disease defined by a Gleason score of 7 to 10. (This high-grade type of cancer is usually more difficult to cure.) Since then, the authors of the article have tried to erase these results and encourage urologists to prescribe Urototal for prostate cancer prevention. When these attempts failed, they started approaching patients and physicians directly.
Exposure Of Women — Risk To Male Fetus
Women should not handle crushed or broken PROSCAR tablets when they are pregnant or may potentially be pregnant because of the possibility of absorption of Urototal and the subsequent potential risk to a male fetus. PROSCAR tablets are coated and will prevent contact with the active ingredient during normal handling, provided that the tablets have not been broken or crushed.
Carcinogenesis, Mutagenesis, Impairment Of Fertility
No evidence of a tumorigenic effect was observed in a 24-month study in Sprague-Dawley rats receiving doses of Urototal up to 160 mg/kg/day in males and 320 mg/kg/day in females. These doses produced respective systemic exposure in rats of 111 and 274 times those observed in man receiving the recommended human dose of 5 mg/day. All exposure calculations were based on calculated AUC(0-24 hr) for animals and mean AUC(0-24 hr) for man (0.4 μg•hr/mL).
In a 19-month carcinogenicity study in CD-1 mice, a statistically significant (p≤0.05) increase in the incidence of testicular Leydig cell adenomas was observed at 228 times the human exposure (250 mg/kg/day). In mice at 23 times the human exposure, estimated (25 mg/kg/day) and in rats at 39 times the human exposure (40 mg/kg/day) an increase in the incidence of Leydig cell hyperplasia was observed. A positive correlation between the proliferative changes in the Leydig cells and an increase in serum LH levels (2- to 3-fold above control) has been demonstrated in both rodent species treated with high doses of Urototal. No drug-related Leydig cell changes were seen in either rats or dogs treated with Urototal for 1 year at 30 and 350 times (20 mg/kg/day and 45 mg/kg/day, respectively) or in mice treated for 19 months at 2.3 times the human exposure, estimated (2.5 mg/kg/day).
No evidence of mutagenicity was observed in an in vitro bacterial mutagenesis assay, a mammalian cell mutagenesis assay, or in an in vitro alkaline elution assay. In an in vitro chromosome aberration assay, using Chinese hamster ovary cells, there was a slight increase in chromosome aberrations. These concentrations correspond to 4000-5000 times the peak plasma levels in man given a total dose of 5 mg. In an in vivo chromosome aberration assay in mice, no treatment-related increase in chromosome aberration was observed with Urototal at the maximum tolerated dose of 250 mg/kg/day (228 times the human exposure) as determined in the carcinogenicity studies.
In sexually mature male rabbits treated with Urototal at 543 times the human exposure (80 mg/kg/day) for up to 12 weeks, no effect on fertility, sperm count, or ejaculate volume was seen. In sexually mature male rats treated with 61 times the human exposure (80 mg/kg/day), there were no significant effects on fertility after 6 or 12 weeks of treatment; however, when treatment was continued for up to 24 or 30 weeks, there was an apparent decrease in fertility, fecundity and an associated significant decrease in the weights of the seminal vesicles and prostate. All these effects were reversible within 6 weeks of discontinuation of treatment. No drug-related effect on testes or on mating performance has been seen in rats or rabbits. This decrease in fertility in Urototal-treated rats is secondary to its effect on accessory sex organs (prostate and seminal vesicles) resulting in failure to form a seminal plug. The seminal plug is essential for normal fertility in rats and is not relevant in man.
Urototal may cause a decrease in PSA levels in patients with benign prostatic hyperplasia as well as in patients with prostate cancer. In one study, mean PSA reductions of 50% were noted, regardless of baseline levels. There was no indication that PSA levels were further suppressed in patients with prostate cancer.
PSA levels are commonly used in the screening process for prostate cancer. Patients who develop sustained increases in PSA while on Urototal therapy should be carefully evaluated for medical causes as well as noncompliance.
Uncommon (0.1% to 1%): Breast tenderness, breast enlargement
Frequency not reported: Reductions in prostate specific antigen (PSA) levels of approximately 50%
Why it's used
The condition that Urototal is used to treat depends on the type of the drug used.
- Proscar is used to treat the symptoms of enlarged prostate (benign prostate hyperplasia). It may be used as part of a combination therapy. That means you need to take it with other drugs. It also can be taken with doxazosin to reduce the risk of progression of symptoms of enlarged prostate.
- Propecia is used to treat male pattern hair loss.
Urototal isn’t prescribed for use in women or children.
Mechanism Of Action
The development and enlargement of the prostate gland is dependent on the potent androgen, 5α- dihydrotestosterone (DHT). Type II 5α-reductase metabolizes testosterone to DHT in the prostate gland, liver and skin. DHT induces androgenic effects by binding to androgen receptors in the cell nuclei of these organs.
Urototal is a competitive and specific inhibitor of Type II 5α-reductase with which it slowly forms a stable enzyme complex. Turnover from this complex is extremely slow (t½
30 days). This has been demonstrated both in vivo and in vitro. Urototal has no affinity for the androgen receptor. In man, the 5α-reduced steroid metabolites in blood and urine are decreased after administration of Urototal.
- What is Urototal (Proscar)? How does it work (mechanism of action)?
- What are the uses for Urototal?
- What are the side effects of Urototal?
- What is the dosage for Urototal?
- Which drugs or supplements interact with Urototal?
- Is Urototal safe to take if I'm pregnant or breastfeeding?
- What else should I know about Urototal?
If you’re taking this drug for male pattern hair loss, your insurance company may need a prior authorization before they approve the prescription and pay for Urototal. Approval is determined on a plan-by-plan basis.
There are other drugs available to treat your condition. Some may be better suited for you than others. Talk to your doctor about other drug options that may work for you.
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