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Dosage in the Elderly:
No dosage adjustments are required even though the elimination of FINCAR 5 is decreased in patients older
than 70 years.
SCHEDULING STATUS: S4
PROPRIETARY NAME (AND DOSAGE FORM):
FINCAR 5 (Tablets)
SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Side-effects:
Reproductive system and breast disorders:
COMPOSITION:
Each film-coated tablet contains 5 mg finasteride.
Less Frequent:
PHARMACOLOGICAL CLASSIFICATION:
A 21.12 Hormone inhibitors.
Impotence, decrease in libido, decrease in volume of ejaculate and ejaculation disorder
are the most reported adverse experiences related to sexual function. Breast
tenderness and breast enlargement.
The following side effects have been reported and frequencies
Testicular pain.
are unknown:
PHARMACOLOGICAL ACTION:
Finasteride is a synthetic 4-azasteroid compound. Finasteride inhibits an intracellular enzyme, Type II 5alpha-reductase, which metabolises testosterone into the more potent androgen dihydrotestosterone (DHT).
Finasteride does not bind to the androgen receptor.
The enlargement of the prostate gland and subsequent benign prostate hyperplasia (BPH) is dependent upon
the conversion of testosterone to DHT within the prostate.
Finasteride reduces both circulating and intraprostatic DHT concentrations. Within 24 hours after oral
administration of finasteride, there is a significant reduction in circulating DHT levels as a result of the
inhibition of 5-alpha-reductase.
Pharmacokinetics:
Following an oral dose of 14C-finasteride in humans, the bioavailability is approximately 80 % (relative to an
intravenous reference dose). This is not affected by food.
Finasteride reaches maximum plasma concentrations within approximately 2 hours. Absorption is complete
after 6 – 8 hours. Protein binding is approximately 93 %, the volume of distribution 76 litres and plasma
clearance about 165 ml/min.
In subjects aged 46-60 years, finasteride displays a mean plasma elimination half-life of about 6 hours (4-12
hours) and of approximately 8 hours in men 70 years of age or older.
Two finasteride metabolites with only a small fraction of the 5-alpha-reductase inhibitory activity have been
identified. Thirty six percent of a total finasteride dose is excreted in the urine in the form of metabolites while
57 % of the total dose is excreted in the faeces.
INDICATIONS:
FINCAR 5 is used for the treatment of symptomatic benign prostatic hyperplasia (BPH) in males with an
enlarged prostate to:
• Improve urinary flow
• Improve the symptoms associated with BPH by causing regression of the enlarged prostate.
• Decrease the incidence of acute urinary retention.
• Improve the symptoms associated with BPH.
• Decrease the incidence of surgery including prostatectomy and transurethral resection of the prostate
(TURP).
CONTRA-INDICATIONS:
Hypersensitivity to any of the ingredients of FINCAR 5.
Pregnancy – (see “WARNINGS” and “PREGNANCY AND LACTATION”).
FINCAR 5 is not indicated for use in females.
FINCAR 5 is not indicated for use in children.
WARNINGS:
FINCAR 5 is contra-indicated for use in females when they are or may potentially be pregnant as it may result
in abnormalities of the external genitalia of a male foetus when administered to a pregnant woman (see
“PREGNANCY AND LACTATION”).
It is not known whether FINCAR 5 is excreted in breast milk.
Serum Prostate Specific Antigen (S-PSA) levels are decreased in patients treated with FINCAR 5.
INTERACTIONS:
No interactions of clinical importance have been identified.
FINCAR 5 does not appear to significantly affect the cytochrome P450 enzyme system.
No clinically meaningful interactions were found with the following compounds tested in men: digoxin,
propranolol, warfarin, glibenclamide and theophylline.
Other Concomitant Therapy:
FINCAR 5 has been used concomitantly with, non-steroidal anti-inflammatory drugs (NSAIDs), paracetamol,
acetylsalicylic acid, ACE-inhibitors, alpha-blockers, beta-blockers, calcium channel blockers, cardiac nitrates,
diuretics, HMG-CoA reductase inhibitors, H2-antagonists, quinolones and benzodiazepines without evidence
of clinically significant adverse interactions.
PREGNANCY AND LACTATION:
Pregnancy:
FINCAR 5 is contra-indicated in pregnancy (see “WARNINGS” and “CONTRA-INDICATIONS”).
FINCAR 5, through its inhibitory activities on Type II 5-alpha-reductase, inhibits the conversion of testosterone
to dihydrotesterone. This may cause abnormalities of the external genitalia of a male foetus when administered
to a pregnant woman.
Skin Disorders:
Less frequent:
Rash, hypersensitivity reactions, including pruritus, urticaria, swelling of the lips
and face.
Special Precautions:
General:
The beneficial response of FINCAR 5 may not be manifested immediately and thus patients with large
residual urine volume and/or severely diminished urinary flow should be monitored carefully for obstructive
uropathy.
Since serum markers of prostate cancer may be reduced in patients taking FINCAR 5, such malignancies
should be excluded before treatment of benign prostatic hyperplasia is initiated.
Effects on PSA and prostate cancer detection:
The clinical benefit of FINCAR 5 in the treatment of patients with prostate cancer has not been demonstrated.
Prostate cancer evaluations including digital rectal examinations and others are recommended prior to
initiating therapy with FINCAR 5 and should be repeated periodically thereafter. Serum prostate-specific
antigen (S-PSA) is also used for the detection of prostate cancer. A baseline S-PSA level above 10 ng/ml
(Hybritech) generally prompts further evaluation and consideration of a biopsy. Further evaluation is advisable
for S-PSA levels between 4 - 10 ng/ml. The medical practitioner should be aware that a baseline S-PSA level
lower than 4 ng/ml does not exclude prostate cancer.
FINCAR 5 causes a decrease in S-PSA concentrations even in the presence of prostate cancer (see
“Drug/Laboratory Test Interactions”). The reduction of S-PSA levels in patients with BPH treated
with FINCAR 5, should be considered when evaluating S-PSA levels and does not rule out
concomitant prostate cancer.
Careful evaluation of patients with a sustained increase in S-PSA levels while treated with FINCAR 5 is
required.
Drug/ Laboratory Test Interactions:
Prostatic volume is correlated with patient’s age whereas serum prostate specific antigen (S-PSA)
concentration is correlated with patient’s age and prostatic volume. Consideration should be given to the fact
that S-PSA levels decrease in patients treated with FINCAR 5 when S-PSA laboratory determinations are
evaluated (see “Special Precautions”). S-PSA levels decrease rapidly within the first months of therapy,
whereafter it stabilises to a new baseline. The post-treatment baseline is approximately half of the pretreatment value. Although it may vary in individual patients, the decrease is predictable over the entire range
of S-PSA values. Therefore, in typical patients treated with FINCAR 5 for six months or longer, S-PSA values
should be doubled for comparison to normal S-PSA ranges in untreated men. There is considerable overlap
in S-PSA concentrations among men with and those without prostate cancer. Therefore, in men with BPH,
S-PSA values within the normal reference range do not rule out prostate cancer, regardless of treatment with
FINCAR 5. The ability of S-PSA to distinguish between BPH and cancer is not adversely affected by treatment
with FINCAR 5.
Laboratory Test Findings:
The fact that S-PSA levels are decreased in patients treated with FINCAR 5 should be considered when SPSA laboratory test determinations are evaluated (see “Special Precautions”).
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
There is no specific treatment for overdosage with FINCAR 5.
Treatment should be symptomatic and supportive.
IDENTIFICATION:
Light blue, circular, biconvex, film-coated tablets plain on both sides.
PRESENTATION:
Aluminium foil blister strips of 10 tablets each, packed in 30’s.
STORAGE INSTRUCTIONS:
Store below 25°C. Protect from light.
Keep blisters in the outer carton until required for use.
KEEP OUT OF REACH OF CHILDREN.
REGISTRATION NUMBER:
41/21.12/0422
Lactation:
The safety of FINCAR 5 during breastfeeding is not known.
Exposure of pregnant women to FINCAR 5 - Risk To Male Foetus:
FINCAR 5 tablets are coated which prevents contamination with the active ingredient during normal handling,
provided that the tablets are intact; i.e. not crushed or broken.
Because of the possibility of absorption of FINCAR 5 and the subsequent potential risk to the male foetus (see
“PREGNANCY AND LACTATION”), pregnant women should not handle crushed or broken FINCAR 5
tablets.
Additionally, since FINCAR 5 is present in semen, condoms should be used by male patients or otherwise
female sexual partners at risk of becoming pregnant should be avoided to prevent exposure.
NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION:
CIPLA MEDPRO (PTY) LTD.
Rosen Heights,Pasita Street,
Rosen Park, Bellville 7530 RSA
DATE OF PUBLICATION OF THIS PACKAGE INSERT:
August 2007
© CIPLA MEDPRO (PTY) LTD.
Dosage in Renal Insufficiency:
Adjustments in dosage are not required in patients with varying degrees of renal insufficiency (creatinine
clearance as low as 9 ml/min) as there are no changes in the disposition of FINCAR 5 in these patients when
compared to healthy subjects.
Size: 200x260 mm
AE36 A
DOSAGE AND DIRECTIONS FOR USE:
The recommended daily dose is one 5 mg tablet, taken with or without food.
Despite a possible early improvement in symptoms, a therapeutic trial of 6 - 12 months may be necessary to
assess achievement of a beneficial response.
E:\Patil\Medpro\Fincar.p65 Dt.: 21-09-07