Finasteride | apollo | +9191 46 950 950

Finasteride | apollo | +9191 46 950 950

Finasteride

CAS Number : 98319-26-7

Molecular Weight : 372.549g/mol

Molecular Formula : C23H36N2O2

Systematic (IUPAC) : (1S,2R,7R,10S,11S,14S,15S)-N-tert-butyl-2,15-dimethyl-5-oxo-6-

azatetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-3-ene-14-carboxamide

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 film-coated 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.

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

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

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, 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.

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 5α-

reduced 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 5α-reductase deficiency also have decreased levels of DHT. Except for the associated urogenital defects present at

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

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

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

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 5a-

reductase, 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 two-thirds of circulating DHT. Although finasteride is 100-fold more selective for type II 5a-reductase than for the

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%

(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

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