Finasteride propecia drug information

Finasteride is a competitive and specific inhibitor of Type II 5a-reductase, an intracellular enzyme that converts the androgen testosterone into DHT. Two distinct isozymes are found in mice, rats, monkeys, and humans: Type I and II. Each of these isozymes is differentially expressed in tissues and developmental stages. In humans, Type I 5a-reductase is predominant in the sebaceous glands of most regions of skin, including scalp, and liver. Type I 5a-reductase is responsible for approximately one-third of circulating DHT. The Type II 5a-reductase isozyme is primarily found in prostate, seminal vesicles, epididymides, and hair follicles as well as liver, and is responsible for two-thirds of circulating DHT.

In humans, the mechanism of action of finasteride is based on its preferential inhibition of the Type II isozyme. Using native tissues (scalp and prostate), in vitro binding studies examining the potential of finasteride to inhibit either isozyme revealed a 100-fold selectivity for the human Type II 5a-reductase over Type I isozyme (IC50=500 and 4.2 nM for Type I and II, respectively). For both isozymes, the inhibition by finasteride is accompanied by reduction of the inhibitor to dihydrofinasteride and adduct formation with NADP+. The turnover for the enzyme complex is slow (t ½ approximately 30 days for the Type II enzyme complex and 14 days for the Type I complex).

Finasteride has no affinity for the androgen receptor and has no androgenic, antiandrogenic, estrogenic, antiestrogenic, or progestational effects. Inhibition of Type II 5a-reductase blocks the peripheral conversion of testosterone to DHT, resulting in significant decreases in serum and tissue DHT concentrations. Finasteride produces a rapid reduction in serum DHT concentration, reaching 65% suppression within 24 hours of oral dosing with a 1-mg tablet. Mean circulating levels of testosterone and estradiol were increased by approximately 15% as compared to baseline, but these remained within the physiologic range.

In men with male pattern hair loss (androgenetic alopecia), the balding scalp contains miniaturized hair follicles and increased amounts of DHT compared with hairy scalp. Administration of finasteride decreases scalp and serum DHT concentrations in these men. The relative contributions of these reductions to the treatment effect of finasteride have not been defined. By this mechanism, finasteride appears to interrupt a key factor in the development of androgenetic alopecia in those patients genetically predisposed.

DOSAGE AND ADMINISTRATION

The recommended dosage is 1 mg orally once a day.

PROPECIA may be administered with or without meals.

In general, daily use for three months or more is necessary before benefit is observed. Continued use is recommended to sustain benefit, which should be re-evaluated periodically. Withdrawal of treatment leads to reversal of effect within 12 months.

DRUG INTERACTIONS

No drug interactions of clinical importance have been identified. Finasteride does not appear to affect the cytochrome P450-linked drug-metabolizing enzyme system. Compounds that have been tested in man include antipyrine, digoxin, propranolol, theophylline, and warfarin and no clinically meaningful interactions were found.

WARNINGS

PROPECIA is not indicated for use in pediatric patients (see INDICATIONS AND USAGE; and PRECAUTIONS, Pediatric Use) or women (see also WARNINGS, EXPOSURE OF WOMEN - RISK TO MALE FETUS; PRECAUTIONS, Information for Patients and Pregnancy; and HOW SUPPLIED, Storage and Handling).

GENERIC NAME: finasteride
BRAND NAME: Proscar

DRUG CLASS AND MECHANISM: 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). Finasteride inhibits the enzyme necessary for the conversion of testosterone to DHT in the prostate. Therefore, administration of finasteride 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 finasteride, only 50% will experience improvement in the symptoms of BPH. Patients generally respond to finasteride in several weeks, but it often takes 6 months for the patient to receive the full effect of the drug.
PREPARATIONS: Tablet (5mg).

STORAGE: Finasteride should be stored at room temperature in a tight light resistant container.

PRESCRIBED FOR: Finasteride is used to treat symptoms of BPH. Finasteride is approved for use with the alpha-blocker, doxazosin, to reduce the progression of symptoms of BPH.

DOSING: Finasteride is metabolized mainly by the liver, and caution should be used in patients with liver dysfunction. Finasteride may be taken with or without food.

DRUG INTERACTIONS: Drug interactions are generally not a problem.

PREGNANCY: Finasteride causes abnormal development of the sexual organs of the male fetus. Therefore, women who are pregnant or are likely to be pregnant should not handle crushed or broken finasteride tablets in order to prevent absorption through the skin.

NURSING MOTHERS: Finasteride is not prescribed for women.
SIDE EFFECTS: Side effects are rare but can include impotence and decreased sex drive. Finasteride should not be used by women, children, or male partners of women trying to become pregnant. Finasteride should not be used until a thorough prostate examination has been done to exclude cancer, stricture, or infection in the gland.