Finosteride 5 mg
Each film-coated Finastura tablet contains finasteride 5 mg.
Inactive ingredients: Lactose monohydrate, microcrystalline cellulose PH 10 I and PH 102. pregelatinized starch, sodium starch glycolate. sodium docusate, magnesium stearate. Opadry Blue 57U30634.
Finastura. finasteride, is a competitive inhibitor of human 5 a-reductase. an intracellular enzyme which metabolises testosterone into the more potent androgen, dihydrotestosterone (DHT). In benign prostatic hyperplasia (BPH). enlargement of the prostate gland is dependent upon the conversion of testosterone to DHT
within the prostate. Finasteride is highly effective in reducing circulating and intra-prostatic DHT. Finasteride has no affinity for the androgen receptor.
– After an oral dose ofl4C-fmasteride in man, 39010 of the dose was excreted in the urine in the form of metabolites (virtually no unchanged drug was excreted in the urine). and 57% of total dose was excreted in the faeces. Two metabolites have been identified which possess only a small fraction of the Type 115 a-reductase activity of finasteride.
– The oral bioavailability of finasteride is approximately 80%, relative to an intravenous reference dose, and is unaffected by food. Maximum plasma concentrations are reached approximately two hours after dosing and the absorption is complete within 6-8 hours. Protein binding is approximately 93%. Plasma clearance and the volume of distribution are approximately 165 mVmin and 761.
– In the elderly, the elimination rate offinasteride is somewhat decreased. Half-life is prolonged from a mean half-life of approximately six hours in men aged 18-60 years to eight hours in men aged more than 70 years. This is of no clinical significance and does not warrant a reduction in dosage.
– In patients with chronic renal impairment, whose creatinine clearance ranged from 9-55 mVmin, the disposition of a single dose of 14C_finasteride was not different from that in healthy volunteers. Protein binding also did not differ in patients with renal impairment. A portion of the metabolites which normally is excreted
renally was excreted in the faeces. It therefore appears that faecal excretion increases commensurate to the decrease in urinary excretion of metabolites.
– Dosage adjustment in non-dialysed patients with renal impairment is not necessary.
– There are no data available in patients with hepatic insufficiency. Finasteride has been found to cross the blood-brain harrier. Small amounts offinasteride have been recovered in the seminal fluid of treated patients.
Finastura 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.
Side Effects :
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.
Frequency of adverse reactions is determined as follows:
Very common ~ 1110). Common ~ 11100 to <1/10).
Uncommon ~ 111.000 to <1/100). Rare >1110.000 to
<1/1.000). Very rare «1/10.000). not known (cannot be
estimated from the available data).
System Organ Class
Frequency: adverse reaction
Common: decreased volume of ejaculate
Skin and subcutaneous tissue disorders
Unknown: pruritus, urticaria
Immune system disorders
Unknown: hypersensitivity reactions including swelling of the lips and face
Unknown: increased hepatic enzymes
Reproductive system and breast disorders
Uncommon: ejaculation disorder, breast tenderness, breast enlargement
Unknown: testicular pain
Common: decreased libido
Einasteride is contraindicated in the following:
– Hypersensitivity to any component of this product
– Pregnancy – Use in women when they are or may potentially be pregnant.
– Finasteride is not indicated for use in women or children.
Special warnings and precautions for use General :
– 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.
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 serum prostate specific antigen (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 were not significantly different in patients treated with finasteride or placebo.
– Digital rectal examination, as well as other evaluations for prostate cancer, are recommended prior to initiating therapy with finasteride and periodically thereafter. Serum PSA is also used for prostate cancer detection. Generally, a baseline PSA > 1 0 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 fmasteride. 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 estate cancer. This decrease is predictable over the entire ‘range of PSA values, although ilJllay 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.
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 stabilise to a new baseline. The post-treatment baseline approximates half of the pre- treatment value. Therefore, in typical patients treated with flnasteride 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 it} 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 and the post- marketing period. Physicians should instruct their patients to promptly report any changes in their breast tissue such as lumps, pain, gynaecomastia or nipple
Finasteride is not indicated for use in children. Safety and effectiveness in children have not been established.
The tablet contains lactose monohydrate. Patients with any of the following genetic deficiencies should not take this drug: galactose intolerance, total lactase deficiency or glucose-galactose malabsorption.
The effect of hepatic insufficiency on the pharmacokinetics of fmasteride has not been studied.
Finasteride is contraindicated in women when they are or may potentially be pregnant. Because of the ability of Type IT 5 a-reductase inhibitors to inhibit conversion of testosterone to dihydrotestosterone, these drugs, 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 J 00 ug/kg/day to 100 day, at an incidence of3.6% to 100%.
Additionally pregnant rats produced male offspring with decreased seminal vesicular weights, delayed preputial separation, transient nipple development and decreased anogenital distance, when given flnesteride 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 described above are expected pharmacological effects of Type II 5 a-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 5 a-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 offinasteride and the subsequent potential risk to a male foetus.
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.
finasteride is not indicated for use in women. It is not known whether finasteride is excreted in human milk.
Effects on the ability to drive and use machines :
There are no data to suggest that finasteride affects the bility to drive or use machines.
Drug-drug interactions :
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 effect the pharmacokinetics of other drugs 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, glyburide, warfarin, theophylline, and antipyrine and no clinically meaningful interactions were found.
No specific treatment of overdosage with finasteride is recommcnded. Patients have received single doses of finasteride up to 400 mg and multiple doses of finasteride up to 80 mglday for up to three months without any adverse effects.
Dosage & administration :
Fhe recommended adult dose is one 5 mg tablet daily, With or without food. Flnastura 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 nrecessary to assess whether a beneficial response has been achieved. Thereafter, treatment should be continued long term. No dosage adjustment is required in the elderly or in patients with varying degrees of renal insufficiency (creatinine clearances as low as 9 mUmin). there are no data available in patients with hepatic insufficiency. Einasteride is contraindicated in children.
Carton box contains 3 (AlIOpaque PVCIPElPVDC) strip, each contain 10 film coated tablets.
Store at a temperature not exceeding 30°C, in a dry place.
Keep out of reach of children I
Produced by :
GLOBAL NAPI PHARMACEUTICALS
Industrial Zone, 6″ of October City – Egypt