Approved Date: December 26, 2006 Revision Date: September 12, 2012 Modify Date: December 1, 2013 Finasteride tablets instructions Please read the instructions carefully and use under the guidance of a physician [Drug Name] Generic name: Finasteride tablets English name: Finasteride Tablets Pinyin: Feinaxiong'an Pian Ingredient main ingredients for non-finasteride, its chemical name: 17β a (N-tert-butyl carbamoyl) a 5α- 4-aza-androst a BU a ene-3-one. Accessories for silica, pregelatinized starch, lactose, microcrystalline cellulose, povidone K30, sodium lauryl sulfate, sodium carboxymethyl starch, magnesium stearate, film coating premix (Stomach type ). Its structural formula is: Molecular formula: C23H36N2O2 Molecular Weight: 372.55 Properties Film-coated tablets, after removing the coating it has a pure white or almost white color. Indications This product is suitable for the treatment of existing symptoms of benign prostatic hyperplasia (BPH): Improve symptoms. Reduce the risk of acute urinary retention. Reduce the need for transurethral resection of the prostate (TURP) and prostatectomy risk. [Specification] 5mg. Oral Dosage. Recommended dosage: Each 5 mg (1), once a day, can be taken on an empty stomach or with food. Adverse reactions. Finasteride has good tolerability, adverse reactions are mild, short-lived. Literature: 1. The incidence of adverse reactions 1%, mainly affected sexual function (impotence, loss of libido, ejaculation disorders), breast discomfort (Mammary Fire, breast pain) and skin rash. Gai products for one year the incidence of adverse events is as follows (in brackets placebo group), use of the product two to four years, the cumulative decline of incidence.
Atrophy: 8.1% (3.7%). Libido: 6.4% (3.4 /). Reduce semen volume: 3.7% (0.8%). Ejaculation disorder: 0.8% (0.1%). Breast increase: 0.5% (0.1%). Breast pain: 0.4% (0.1%). Skin rash: 0.5%. 2. Other adverse reactions reported after the market include: itching, urticarial and other allergic reactions and lip swelling and testicular pain. 3. Laboratory test results: laboratory evaluation results should be considered in patients taking nonfinasteride prostate specific circumstances antigen (PSA) levels decreased. Taking non-patient finasteride or a placebo, there is no difference between other standard laboratory parameters. This product is not available for women and children. The product is contraindicated in the following situations: 1. Allergy to the chemicals of any person. 2. Pregnancy and women who may become pregnant. [Note] I. General Considerations 1. Should be excluded from the FDA before and benign prostatic hyperplasia (BPI) similar to other diseases, such as infection, prostate cancer, urethral stricture, bladder low tension, neurogenic disorders. 2. Finasteride is mainly metabolized in the liver, liver dysfunction, caution. 3. Patients with renal insufficiency not need to adjust the dose. Second, the impact of prostate-specific antigen (PSA) and prostate cancer check 1. Non-clinical efficacy no finasteride for prostate cancer treatment. Finasteride does not affect the incidence of prostate cancer, it does not affect the detection rate of prostate cancer. 2. Recommended accept non-regular prostate exam after when former finasteride therapy and treatment for some ask, such as digital rectal examination, prostate pain other relevant examination (including PSA). 3. Finasteride can prostatic hyperplasia (or associated with prostate cancer) in serum PSA concentrations decreased by about 50%. Evaluating PSA data and does not rule when accompanied by prostate cancer, serum PSA level should consider finasteride causes the prostate hyperplasia is reduced. 4. Caution should be evaluated using non-psa levels in patients that finasteride treatment continued to increase, including consideration of non-compliance that non-finasteride therapy.
Third, the drug / test channeling interaction check Impact on PSA levels. Serum PSA concentration and patient age and prostate volume, whereas the volume of the prostate with age-related justice. When evaluating PSA laboratory measurement results, should consider accepting that PSA levels in patients with non-finasteride treatment reduced the facts. Most patients in the first month of treatment PSA decreases rapidly PSA levels subsequently stabilized at a new baseline. Treatment baseline values after treatment is about half the previous baseline values. Thus, a typical patient treatment with finasteride for six months or longer, in comparison with treatment without the normal PSA value in men when PSA values should be doubled. Pregnant women and lactating women drug] This product is contraindicated in pregnant or may become pregnant women. Because it includes finasteride, including a type II 5α-reductase inhibitors class of drugs inhibit the conversion of testosterone to dihydrotestosterone effect, when pregnant women taking, can cause abnormal genitalia of male fetuses. Pregnant or women who may become pregnant should not touch the product debris and lobes. This product is not for lactating women. It is not known whether finasteride from non-human milk excretion. Pediatric Use of this product is not for children. Safety and effectiveness in pediatric data has not been determined. [Geriatric drug use in elderly patients do not need to adjust the dose. Drug interactions drugs have not been established clinically important interactions. 1. Finasteride cytochrome P450 a related drug-metabolizing enzyme system is not significantly affected. The compound has been detected in men are propranolol, digoxin, glyburide, warfarin, theophylline and antipyrine, they were not found with finasteride had clinically significant interaction. 2. Other combination therapies. Although there is no specific drug interaction studies, but in clinical studies finasteride and angiotensin converting enzyme inhibitors, acetaminophen, acetylsalicylic acid, α receptor A blocker, β receptor a blockers, calcium channel blockers, cardiac nitrates, diuretics, H2 receptor antagonists, HMG-CoA reductase inhibitors, non-steroidal anti-inflammatory drugs (NSAIDs), quinolones and benzodiazepines class simultaneously, there is no obvious clinical adverse interactions. Over dosage Documentation: taking finasteride A single dose up to 400 mg, and taking multiple doses of finasteride 80 mg / day, a total of three months in patients with no adverse reactions. For finasteride overdose did not recommend specific treatment. Pharmacological effects This product is a 4-nitrogen steroid hormone compound as a specific type II 5α-reductase competitive inhibitor, the outer peripheral conversion of testosterone to dihydrotestosterone, reduces blood and prostate, skin and other tissue DHT levels. Growth and benign prostate hyperplasia is dependent on dihydrotestosterone, finasteride by reducing blood and prostate tissue DHT levels and inhibit prostate hyperplasia, improve the relevance of benign prostatic hyperplasia Clinical symptoms.
Toxicology Genetic Toxicity: In vitro bacterial, mammalian cell mutagenicity tests and in vitro alkaline elution test results did not show mutagenic effects in vitro chromosome aberration study in CHO cells, finasteride at 450 ~ 550μmol concentration, CHO cell chromosome aberration of light increases, the concentration corresponding to the human after oral administration of 5mg peak plasma concentrations of 4,000 to 5,000 times. In vivo chromosomal aberration assay, mice were given finasteride 250mg / kg / day (by AUC dollars, equivalent to the recommended daily human clinical dose of 5mg of 228 times, the same as all of the following toxicology dose calculation method), chromosome distortion rate did not rise. Reproductive toxicity: Finasteride 80mg / kg / day (ibid., Equivalent to 543 times the dose for human use), continuous administration of 12 weeks had no effect on sexual maturation of male fertility in male rabbits and rats. When more than 24 weeks duration in rats given finasteride 80mg / kg / day, resulting in the seminal vesicles and prostate weight was also significantly reduced, refined mating plug is formed so that the failure decreased fertility in rats; however, rats and rabbits testis and mating behavior has no effect; Toxic effects of the above-mentioned six weeks after stopping resume. Urethra dose dependent teratogenic sensitive period when rats given finasteride for male offspring has obvious teratogenic effects, 100μg ~ 100mg / kg / day (ibid., Equivalent to the clinical dose of 5mg daily 1-1000 times) hypospadias, the rate was 3.6% to 100%, dose 30μg / kg / day (ibid., equivalent to 30 percent of people daily dose), the male offspring of the prostate and seminal vesicle weight, foreskin separation delay and transient breast development, etc., when the dose 3μg / kg / day (ibid., equivalent to 3 percent of people daily dose), the male offspring urogenital pitch shortened. Research that led to the above toxicity rat male offspring critical time of pregnancy 16-17 days. Results pregnant rats were given a non-toxic Department said that these drugs finasteride produced (5α A reductase inhibitors) pharmacological effects, and congenital absence of 5α-reductase boy reported a similar deformity. Rhesus monkeys during pregnancy ask oral finasteride 2mg / kg / day (ibid., Equivalent to 20 times the human daily dose), male fetuses appear abnormal genitalia. All teratogenicity studies, the product of the female offspring no teratogenic effects. Giving finasteride 80mg / kg / day in male rats and female rats not administered rat offspring mating the birth was not observed in drug-related effects. Late pregnancy and lactation in rats given finasteride 3mg / kg / day (ibid., Equivalent to 30 times the human daily dose) resulting in the first generation of male offspring slightly decreased fertility, no effect on the female offspring. Carcinogenicity: SD male and female rats were administered 24 consecutive months of finasteride 320 and 160mg / kg / day (ibid., Equivalent to 274 and 11l times the recommended clinical dose, respectively), tumorigenic effect did not occur. In the 19-month carcinogenicity studies, the finasteride 250mg / kg / day (ibid., Equivalent to 228 times the recommended human daily dose) be administered so that the CD-1 male mice between the incidence of Leydig cell adenoma was significantly higher in mice given finasteride 25mg / kg / day in rats or dose exceeds 40mg / kg / day, between the two animal Leydig cell hyperplasia
significantly higher incidence; Leydig cell hyperplasia The incidence of serum LH levels were positively correlated. Rats and dogs were given the goods 20 and 45mg / kg / day (ibid., Equivalent to 30 and 350 times the human daily dose) for one year or mouse 25mg / kg / day (ibid., Equivalent to the human daily dose 2.3 times) 19 months, there was no correlation between the administration of Leydig cell hyperplasia. Pharmacokinetics] According to the version of 56 PDR Documentation: Absorption: finasteride (5mg) single-dose oral bioavailability of 63% (34-108%), its bioavailability is not affected by food. Peak plasma concentration at 1-2 hours after dosing, Cmax was 37ng / ml (range of 27 ~ 49ng / ml). Distribution: The mean steady-state volume of distribution of 76L (range 44-96L), plasma protein binding rate is approximately 90%. After multiple dose oral administration of a small amount of slow accumulation. For taking finasteride (5mg / d) 17 days, 45 to 60 age group of subjects after oral administration of multiple doses higher than plasma concentrations after a single oral dose of 47%, which in the age group 70 years and older subjects 54% higher than the single-dose oral plasma concentration; mean trough concentrations in both age groups were 6.2ng / ml and 8.1ng / ml. Another study showed that the average age of 65 years taking finasteride (5mg / d) at least one year of benign prostatic hyperplasia (BPH) patients, mean trough concentrations of 9.4ng / ml. Finasteride through the blood brain barrier. In healthy subjects using finasteride 6-24 weeks semen concentration detected 0-l0.54ng / ml. Metabolism: Finasteride is mainly in the liver by the cytochrome P450 3A4 enzyme metabolism, its two main metabolites in finasteride for 5α-reductase inhibitory activity of a play only a very small part of the role. Excretion: After finasteride plasma clearance rate of 165mL / min, mean plasma elimination half-life of six hours (range 3-16 hours), men administered a single oral dose of 14C a finasteride, 39% of the administered dose in urine It was in the form of metabolites excreted 57% of the total excretion from feces. 70 years old non-terminal half-life that finasteride was 8 hours (6-15 hours). Special Populations Pharmacokinetics: Youth under age 18 or child: No pharmacokinetic study conducted on behalf of. Gender: Female no available data about the pharmacokinetics. Elderly: Although the clearance rate reduction, but Wu actual clinical significance, older drugs without dose adjustment. Race: No racial population pharmacokinetic studies. Renal dysfunction: Renal dysfunction, without the need for dose adjustment. When associated with chronic renal dysfunction (creatinine clearance in 9-55mL / min within the range) patients, a single dose of 14C to give a non-finasteride after AUC, Cmax and t1 / 2 no difference between healthy volunteers,
part of the normal metabolites excreted by the kidneys excrete feces towel. Resulting in increased fecal excretion of metabolites, and a corresponding reduction in urinary excretion. Hepatic Insufficiency: No liver dysfunction pharmacokinetic study in patients, but finasteride is mainly metabolized by the liver, liver dysfunction, caution. [Storage] shading, sealed and stored. [Packaging] aluminum board packaging, 10 / plate 1 board / box. 10 / plate 2 plates / box. [Validity] 24 months. [Executive standard] Chinese Pharmacopoeia 2010 edition of the second supplement. [Approval No.] H20050260 Zhunzi manufacturer Company Name: Nanjing Pharmaceutical Co., Ltd. Courier Production Address: 18 Nanjing High-tech Development Zone, the new three-way division Postal Code: 210061 Telephone number: 025-84553699 5,864,612,058,646,129 Fax: 025-84553677 58646133