Finasteride apollo

Transcription

1 Finasteride apollo Finasteride apollo Finasteride CAS Number : Molecular Weight : g/mol Molecular Formula : C23H36N2O2 Systematic (IUPAC) : (1S,2R,7R,10S,11S,14S,15S)-N- tert-butyl-2,15-dimethyl-5-oxo-6- azatetracyclo[ ^{2,7}.0^{11,15}]heptadec-3-ene- 14-carboxamide

2 DRUG DESCRIPTION This medication is used to treat male pattern hair loss and is to be used only by adult men. Finasteride is a white crystalline powder with a melting point near 250 C. It is freely soluble in chloroform and in lower alcohol solvents, but is practically insoluble in water. Finasteride tablets for oral administration are filmcoated tablets that contain 5 mg of Finasteride and the following inactive ingredients: lactose monohydrate, microcrystalline cellulose, sodium starch glycolate, pregelatinised starch, docusate sodium, magnesium stearate, hypromellose, hydroxypropyl cellulose, titanium dioxide, talc, iron oxide yellow Finasterideis used alone or in combination with another medicationto treat benign prostatic hypertrophy (BPH, enlargement of the prostate gland). Finasteride improves symptoms of BPH such as frequent and difficult urination and may reduce the chance of acute urinary retention (suddenly being unable to pass urine). It also may decrease the chance of needing prostate surgery. Finasterideis also used to treat male pattern hair loss (a common condition in which men have gradual thinning of the hair on the scalp, leading to a receding hairline or balding on the top of the head.) Finasteridehas not been shown to treat thinning hair at the temples and is not used to treat hair loss in women or children. Finasteride is in a class of medications called 5-alpha reductase inhibitors. Finasteride treats BPH by blocking the body's production of a male hormone that causes the prostate to enlarge. Finasteride treats male pattern hair loss by blocking the body's production of a male hormone in the scalp that stops hair growth.

3 DOSAGE Finasteride comes as a tablet to take by mouth. It is usually taken once a day with or without food. Take finasteride at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take finasteride exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor. If you are taking finasteride to treat BPH, you should know that finasteride controls your condition, but does not cure it. It may take at least 6 months before your symptoms improve. Continue to take finasteride even if you feel well. Do not stop taking finasteride without talking to your doctor. If you are taking finasteride to treat male pattern hair loss, you should know that finasteride controls hair loss, but does not cure it. It may take at least 3 months before you see any benefit. Continue to take finasteride even if you have already seen an effect. Do not stop taking finasteride without talking to your doctor. If you stop taking finasteride, you will probably lose the hair you have regrown within 12 months of stopping your treatment. If you are taking finasteride to treat male pattern hair loss and have not seen any improvement within 12 months, further treatment will probably not help. Talk to your doctor about whether you should continue your treatment. SIDE EFFECTS

4 Unlikely to occur but the possible side effects include impotence, decreased sex drive or decrease in amount of ejaculate. Finasteride may cause side effects. * inability to have or maintain an erection * decreased sexual desire * decreased volume of ejaculate (amount of semen) * pain in the testicles Some side effects can be serious. If you experience any of these symptoms, call your doctor immediately: * changes in the breasts such as increased size, lumps, pain, or nipple discharge * rash * itching * hives * swelling of the lips and face INTERACTION 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 have included antipyrine, digoxin, propranolol, theophylline, and warfarin and no clinically meaningful interactions were found. Other Concomitant Therapy: Although specific interaction studies were not performed, Finasteride was concomitantly used in clinical studies with acetaminophen, acetylsalicylic acid, α-blockers, angiotensin-converting enzyme (ACE) inhibitors, analgesics, anti-convulsants, beta-adrenergic blocking agents, diuretics, calcium channel blockers, cardiac nitrates, HMG-CoA reductase inhibitors, nonsteroidal

5 anti-inflammatory drugs (NSAIDs), benzodiazepines, H2 antagonists and quinolone anti-infectives without evidence of clinically significant adverse interactions. PHARMALOGY The development and enlargement of the prostate gland is dependent on the potent androgen, 5αdihydrotestosterone (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. Finasteride 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. Finasteride has no affinity for the androgen receptor. In man, the 5αreduced steroid metabolites in blood and urine are decreased after administration of Finasteride. In man, a single 5 mg oral dose of Finasteride produces a rapid reduction in serum DHT concentration, with the maximum effect observed 8 hours after the first dose. The suppression of DHT is maintained throughout the 24-hour dosing interval and with continued treatment. Daily dosing of Finasteride at 5 mg/day for up to 4 years has been shown to reduce the serum DHT concentration by approximately 70%. The median circulating level of testosterone increased by approximately 10 to 20% but remained within the physiologic range. Adult males with genetically inherited Type II 5αreductase deficiency also have decreased levels of DHT. Except for the associated urogenital defects present at

6 birth, no other clinical abnormalities related to Type II 5α-reductase deficiency have been observed in these individuals. These individuals have a small prostate gland throughout life and do not develop BPH. In patients with BPH treated with Finasteride (1 to 100 mg/day) for 7 to 10 days prior to prostatectomy, an approximate 80% lower DHT content was measured in prostatic tissue removed at surgery, compared to placebo; testosterone tissue concentration was increased up to 10 times over pretreatment levels, relative to placebo. Intraprostatic content of prostate-specific antigen (PSA) was also decreased. In healthy male volunteers treated with Finasteride for 14 days, discontinuation of therapy resulted in a return of DHT levels to pretreatment levels in approximately 2 weeks. In patients treated for three months, prostate volume, which declined by approximately 20%, returned to close to baseline value after approximately three months of discontinuation of therapy. CONSUMER INFORMATION USES Finasteride is used to shrink an enlarged prostate (benign prostatic hyperplasia or BPH) in adult men. It may be used alone or taken in combination with other medications to reduce symptoms of BPH and may also reduce the need for surgery. HOW TO USE Read the Patient Information Leaflet provided by your pharmacist before you start taking finasteride and each time you get a refill. If you have any questions regarding

7 the information, consult your doctor or pharmacist. SIDE EFFECTS Decreased sexual ability/desire may occur. In some men, this medication can decrease the amount of semen released during sex. This is harmless. Finasteride may also increase hair growth. If any of these effects persist or worsen, notify your doctor or pharmacist promptly. PRECAUTIONS Before taking finasteride, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. MISSED DOSE If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up. STORAGE Store US product at room temperature below 86 degrees F (30 degrees C) away from light and moisture in a tightly closed container. Store Canadian product at room temperature between 59 to 86 degrees F (15 to 30 degrees C) away from light and moisture in a tightly closed container. Do not store in the bathroom. Keep all medicines away from children and pets. Type small molecule

8 Description An orally active testosterone 5-alpha-reductase inhibitor. It is used as a surgical alternative for treatment of benign prostatic hyperplasia. Synonyms Finasterida [INN-Spanish] Finasteridum [INN-Latin] Categories Enzyme Inhibitors Skin and Mucous Membrane Agents Anti-baldness Agents Antihyperplasia Agents Taxonomy Kingdom Organic Classes Steroids and Steroid Derivatives Lactams Substructures Steroids and Steroid Derivatives Alkanes and Alkenes Amino Ketones Carboxylic Acids and Derivatives Heterocyclic compounds Carboxamides and Derivatives

9 Lactams Pharmacology Indication For the treatment of symptomatic benign prostatic hyperplasia (BPH) in men with an enlarged prostate to: Improve symptoms, reduce the risk of acute urinary retention, reduce the risk of the need for surgery including transurethral resection of the prostate. Also used for the stimulation of regrowth of hair in men with mild to moderate androgenetic alopecia (male pattern alopecia, hereditary alopecia, common male baldness). Pharmacodynamics Finasteride is a synthetic 4-azasteroid compound. This drug is a competitive and specific inhibitor of Type II 5areductase, an intracellular enzyme that converts the androgen testosterone into 5α-dihydrotestosterone (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 twothirds of circulating DHT. Although finasteride is 100- fold more selective for type II 5a-reductase than for the

10 type I isoenzyme, chronic treatment with this drug may have some effect on type I 5a-reductase. Mechanism of Action The mechanism of action of Finasteride is based on its preferential inhibition of Type II 5a-reductase through the formation of a stable complex with the enzyme. Inhibition of Type II 5a-reductase blocks the peripheral conversion of testosterone to DHT, resulting in significant decreases in serum and tissue DHT concentrations, minimal to moderate increase in serum testosterone concentrations, and substantial increases in prostatic testosterone concetrations. As DHT appears to be the principal androgen responsible for stimulation of prostatic growth, a decrease in DHT concentrations will result in a decrease in prostatic volume (approximately 20-30% after 6-24 months of continued therapy). In men with androgenic alopecia, the mechanism of action has not been fully determined, but finasteride has shown to decrease scalp DHT concentration to the levels found in hairy scalp, reduce serum DHT, increase hair regrowth, and slow hair loss. Metabolism Drug is extensively metabolized, primarily in the liver via CYP3A4. Two metabolites have been identified with 20% of the activity of finasteride. Route of Elimination Following an oral dose of 14C-finasteride in man (n = 6), a mean of 39% (range, 32 to 46%) of the dose was excreted in the urine in the form of metabolites; 57%

11 (range, 51 to 64%) was excreted in the feces. Urinary excretion of metabolites was decreased in patients with renal impairment. This decrease was associated with an increase in fecal excretion of metabolites. Affected Organisms Humans and other mammals apollo asia Division apollo Pharmaceuticals INDIA [P] Ltd asia Division Mr.Vipin Saxena CEO DIRECT: Wireline Purchase HELPDESK: Wireline Sales HELPDESK: Wireless 24x7 HELPDESK: Blackberry Pin : 32E6500D 32E C58 apollo@hotmail.co.in Sales@apollopharma.in

12 Chat: MSN Hotmail:VipinrSaxena Skype NAME:VipinrSaxena Rocketmail:VipinrSaxena Google mail:vipinrsaxena BlackBerry:28415C58 Regd. Office :- 1104, Maker Chamber V, Nariman Point Mumbai, INDIA Pin: Industrial Office D-62, OIC India Oshiwara Industrial Centre, New Link Road, Goregoan West, Mumbai, INDIA Pin: Manufacturing Unit Address: Plot No. 117A, Village: Chamble Near MonaTona Limited.Wada, Maharashtra, PIN : INDIA

13

14

15

16

17