Tadalafil tablets

During sexual stimulation, the penis becomes erect due to the relaxation of the smooth muscles of the penis arteries and corpus cavernosum, which increases the blood flow to the penis. This reaction is mediated by nitric oxide (NO) released by nerve endings and endothelial cells. NO stimulates smooth muscle cells to synthesize cyclic guanosine monophosphate (cGMP), which causes smooth muscle relaxation and increases blood flow to the corpus cavernosum. Inhibition of phosphodiesterase 5 (PDE5) enhances erectile function by increasing cGMP. PDE5 is present in the smooth muscles of the corpus cavernosum, blood vessels and visceral smooth muscles, skeletal muscles, platelets, kidneys, lungs, cerebellum and pancreas. In vitro studies have shown that tadalafil is a selective inhibitor of PDE5. Since sexual stimulation is required to stimulate the local release of NO, the inhibition of PDE5 by tadalafil is meaningless without sexual stimulation. PDE5 inhibition can affect the concentration of cGMP in the corpus cavernosum and pulmonary arteries. The same situation has been observed in the smooth muscles and blood vessels of the prostate and bladder. The mechanism of action for alleviating BPH symptoms is not yet clear. In vitro studies have shown that tadalafil has a stronger effect on PDE5 than on other phosphodiesterases. These studies showed that tadalafil's effect on PDE5 is more than 10,000 times stronger than on PDE1, PDE2, PDE4, and PDE7 in the heart, brain, blood vessels, liver, leukocytes, skeletal muscle, and other organs; more than 10,000 times stronger than on PDE3 in the heart and blood vessels; about 700 times stronger than on PDE6 involved in phototransduction in the retina; more than 9,000 times stronger than on PDE8, PDE9, and PDE10; 14 times stronger than on PDE11A1, and 40 times stronger than on PDE11A4. PDE11 is found in the human prostate, testes, skeletal muscle, and other tissues. In vitro, tadalafil can inhibit recombinant PDE11A1, and at therapeutic concentrations, the degree of inhibition of PDE11A4 activity is low. The physiological effects and clinical impact of PDE11 inhibition in humans are not yet clear.

The main ingredient of this product is tadalafil.

This product is a film-coated tablet, which is white or off-white after removing the coating. Chemical name: (6R,12aR)-6-(1,3-benzodioxolan-5-yl)-2-methyl 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione

Treatment of erectile dysfunction (ED). Treatment of symptoms and signs of erectile dysfunction (ED) combined with benign prostatic hyperplasia (BPH).

Taking tadalafil tablets is not affected by food, and sexual stimulation is required for tadalafil tablets to be effective. Erectile dysfunction Take tadalafil tablets as needed • For most patients, the recommended starting dose of tadalafil tablets as needed is 10 mg, taken before sexual intercourse. • Depending on individual efficacy and tolerability, the dose can be increased to 20 mg or reduced to 5 mg. The maximum recommended frequency of medication for most patients is once a day. • Compared with placebo, taking tadalafil tablets as needed can improve erectile function for up to 36 hours. Therefore, this factor should be considered when recommending patients to take tadalafil tablets in the best way. Take tadalafil tablets once a day • The recommended starting dose of tadalafil tablets once a day is 2.5 mg, taken at approximately the same time every day, regardless of when sexual intercourse occurs. • Depending on individual efficacy and tolerability, the dose of tadalafil tablets once a day can be increased to 5 mg. The risk-benefit balance should be based on the patient's specific situation to select an appropriate treatment plan. Use in Special PopulationsTadalafil tablets are taken as needed for renal impairment•Mild (creatinine clearance 51~80mL/min): No dose adjustment is required. •Moderate (creatinine clearance 31~50mL/min): The recommended starting dose is 5mg, not more than once a day, and the maximum dose limit is not more than 10mg every 48 hours. •Severe (creatinine clearance <30mL/min and hemodialysis): The maximum recommended dose is 5mg, not more than once every 72 hours (see [Precautions]). Take tadalafil tablets once a day•Mild (creatinine clearance 51~80mL/min): No dose adjustment is required. •Moderate (creatinine clearance 31~50mL/min): No dose adjustment is required. •Severe (creatinine clearance <30mL/min and hemodialysis): Once-daily tadalafil tablets are not recommended (see [Precautions]). Take tadalafil tablets as needed • Mild or moderate (Child Pugh grade A or B): The dose of tadalafil tablets should not exceed 10 mg once daily. Once-daily tadalafil tablets have not been extensively evaluated in patients with hepatic impairment, so they should be used with caution. • Severe (Child Pugh grade C): Tadalafil tablets are not recommended (see [Precautions]). Take tadalafil tablets once daily • Mild or moderate (Child Pugh grade A or B): Once-daily tadalafil tablets have not been extensively evaluated in patients with hepatic impairment. Therefore, caution is advised if once-daily tadalafil tablets are prescribed to these patients. • Severe (Child Pugh grade C): Tadalafil tablets are not recommended (see [Precautions]). Elderly No dose adjustment is required for patients over 65 years of age. Concomitant use of nitrates Concomitant use of nitrates in any form is strictly prohibited (see [Contraindications]). α-blockers When tadalafil tablets are used in combination with α-blockers, patients receiving α-blocker therapy should be stabilized before starting tadalafil tablets and starting at the lowest recommended dose (see [Precautions]). CYP3A4 inhibitors Take tadalafil tablets as needed For patients who are taking strong CYP3A4 inhibitors, such as ketoconazole or ritonavir, the maximum recommended dose of tadalafil tablets is 10 mg, not to exceed once every 72 hours (see [Precautions] and [Drug Interactions]). Take tadalafil tablets once a day For patients who are taking strong CYP3A4 inhibitors, such as ketoconazole or ritonavir, the recommended dose is not more than 2.5 mg (see [Precautions] and [Drug Interactions]).

Not yet clear

Patients who are allergic to any of the ingredients in this product are prohibited from taking tadalafil tablets. Nitrates Patients who are taking any form of nitrates, whether regularly and/or intermittently, are strictly prohibited from taking tadalafil tablets. Clinical pharmacology studies have shown that tadalafil tablets can enhance the antihypertensive effect of nitrates (see [Pharmacology and Toxicology]). Hypersensitivity Patients with known severe allergies to tadalafil should not take tadalafil tablets. There have been reports of hypersensitivity reactions, including Stevens-Johnson syndrome and exfoliative dermatitis (see [Adverse Reactions]). Guanylate Cyclase (GC) stimulators Patients who are taking GC stimulators (such as riociguat) should not take tadalafil tablets. PDE5 inhibitors, including tadalafil tablets, may enhance the antihypertensive effect of GC stimulators.

Precautions for children: Not yet clear Precautions for pregnancy and lactation: Summary of risks for pregnant women Tadalafil is not for use in women. There are currently no data on the use of tadalafil in pregnant women, and no risk of adverse developmental outcomes associated with the drug is known. In animal reproduction studies, oral administration of tadalafil during the period of organogenesis at doses up to 11 times the maximum recommended human dose (MRHD, Maximum Recommended Human Dose, 20 mg/day) did not produce adverse developmental effects in pregnant rats or mice (see data below). Animal data Animal reproduction studies have shown that oral administration of tadalafil to pregnant rats or mice during the period of organogenesis, with exposure levels reaching 11 times the maximum recommended human dose (MRHD, 20 mg/day), did not produce evidence of teratogenicity, embryotoxicity, or fetotoxicity. In a prenatal/postnatal development study, the survival of pups after birth was reduced when the mother was given tadalafil at doses greater than 10 times the MRHD based on AUC. Based on AUC, symptoms of maternal toxicity occurred at doses exceeding 16 times the MRHD. Surviving fetuses had normal development and reproductive performance (see [Pharmacology and Toxicology]). Reduced survival of postnatal pups was observed in another rat prenatal and postnatal development study at dose levels of 60, 200, and 1000 mg/kg. The no observed effect level (NOEL) for maternal toxicity was 200 mg/kg per day, while the no observed effect level for developmental toxicity was 30 mg/kg per day. The exposure levels at these doses were approximately 16 times and 10 times the human AUC at MRHD20 mg, respectively. Tadalafil and/or its metabolites can cross the rat placenta, resulting in fetal exposure. Risk summary for lactating women Tadalafil tablets cannot be used in women. There is no information on the secretion of tadalafil and/or its metabolites in human milk, the effects on breastfed children, or the effects on the amount of breast milk produced. Tadalafil and/or its metabolites can be detected in the milk of lactating rats at concentrations approximately 2.4 times the plasma concentration. Infertility in males and females of reproductive age Based on data from three studies in adult males, tadalafil reduced sperm concentrations in a study where 10 mg tadalafil was administered for 6 months and in a study where 20 mg tadalafil was administered for 9 months. This effect was not observed in another study where 20 mg tadalafil was administered for 6 months. Neither 10 mg nor 20 mg of tadalafil had an adverse effect on mean concentrations of testosterone, luteinizing hormone, or follicle-stimulating hormone. The clinical significance of the reduction in sperm concentration in the first two studies is unclear, and no studies have evaluated the effects of tadalafil on male fertility. In animal studies, decreased spermatogenesis was observed in dogs, but not in rats. Precautions for the elderly: Not yet clear

Not yet clear

Store at room temperature.

5 mg

Chongqing Huapont Pharmaceutical Co., Ltd.

• Founded in:

  2012-06-26

• Address:

  No. 69, Renhe Xingguang Avenue, Yubei District, Chongqing

• Tax NO.:

  915000005992299001

• Registered Funds:

  450 million yuan

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