Jinge commodity introduction
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Generic name: sildenafil citrate tablets
Manufacturer: Guangzhou Baiyunshan Pharmaceutical Co., Ltd. Guangzhou Baiyunshan Pharmaceutical General Factory
Approval number: National Medicine Zhunzi H20 143255
Drug specification: 50mg*2 tablets.
Jingo instruction
Trade name Jinge
General name sildenafil citrate tablets
English name sildenafil citation film
Chinese phonetic word formation
The main component of Ginger is sildenafil citrate.
The feature is that the gold lattice is a film-coated tablet, and the appearance is white to white-like after the coating is removed.
Indications are suitable for the treatment of erectile dysfunction.
Usage and Dosage For most patients, the recommended dosage is 50 mg, which should be taken on demand about 1 hour before sexual activity. But you can take it at any time within 0.5-4 hours before sexual activity. According to the curative effect and tolerance, the dose can be increased to 100 mg (recommended dose) or decreased to 25 mg, and taken once a day.
Pharmacological Action Ginger is an oral drug for the treatment of erectile dysfunction (ED). It is the citrate of sildenafil, a selective inhibitor of phosphodiesterase type 5 (pDE5) with specificity for cyclic guanosine phosphate (cGMp). Mechanism of action: The physiological mechanism of penile erection involves the release of nitric oxide (NO) from the corpus cavernosum during sexual stimulation. NO activation of guanylate cyclase leads to the increase of cGMp level, which makes the smooth muscle in cavernous body relax and blood fill. Effect of pharmacodynamics sildenafil on penile erection: Sildenafil citrate is a highly selective phosphodiesterase 5(pDE5) inhibitor. PDE5 is highly expressed in corpus cavernosum of penis, but low expressed in other tissues (including platelets, blood vessels, visceral smooth muscle and skeletal muscle). Sildenafil can selectively inhibit pDE5, enhance nitric oxide (NO)-cGMp pathway, increase cGMp level, lead to relaxation of smooth muscle of corpus cavernosum, and make erectile dysfunction patients have natural erectile response to sexual stimulation. Erectile response generally increases with the increase of sildenafil dose and plasma concentration. Experiments show that the drug can last for 4 hours, but the reaction is weaker than 2 hours. Reaction of sildenafil to myocardium: pDE5 does not exist in normal or diseased cardiac conduction tissues, myocardial cells, endothelial cells and lymphoid tissues, so sildenafil (pDE5 inhibitor) has no positive inotropic effect and cannot directly affect myocardial contraction function. Effect of sildenafil on cardiac parameters: Normal male volunteers took a single dose of sildenafil 100mg orally, and there was no clinically significant ECG change. Under the monitoring of Swan-Ganz catheter, eight patients with stable ischemic heart disease were injected with sildenafil four times. Results: At rest, the systolic blood pressure and diastolic blood pressure decreased by 7% and 65438 00% respectively compared with the baseline. Resting right atrium, pulmonary artery pressure, pulmonary artery wedge pressure and cardiac output decreased by 28%, 28%, 20% and 7% respectively. Although this intravenous dose is 2 ~ 5 times higher than the average peak blood concentration of sildenafil 100mg taken orally by healthy male volunteers, the above hemodynamic reaction still exists during exercise. Response of sildenafil to blood pressure: A single oral dose of sildenafil 100mg in healthy male patients led to a decrease in blood pressure of bedsore (average 8.4/5.5mmHg). Blood pressure decreased significantly at 1-2 hours after taking the medicine, and there was no difference between the two groups at 8 hours after taking the medicine. The effects of 25mg, 50mg and 100mg sildenafil on blood pressure are similar, and it seems that it has nothing to do with drug dosage and blood concentration. Patients who take nitrate at the same time have a greater antihypertensive effect. Hypotension (90/50mmHg), nitrate or drugs providing nitrate are the strict contraindications for sildenafil application. The great effect of sildenafil on blood pressure occurred about 65438 0 hours after administration, which was consistent with the peak value of drug plasma. Therefore, when the blood concentration of sildenafil reaches the peak, sexual activity may induce cardiac events. Although the hypotensive reaction caused by sildenafil is light and short-lived (blood pressure generally returns to the baseline within 4 hours), the interaction between sildenafil and nitrate can produce obvious and longer-term hypotensive effect. Sildenafil has a short half-life and can be eluted within 24 hours (about 6 half-lives). The American Heart College and the American Heart Association have clearly pointed out that sildenafil is prohibited for those who use nitrate drugs within 24 hours. Effect of sildenafil on vision: Studies show that taking twice the recommended dose of Jinge has no effect on vision, electroretinogram, intraocular pressure and papilla size. There may be a transient blue/green discrimination abnormality. Whether used alone or in combination with aspirin, Ginger has no effect on bleeding time. In vitro, Gingert enhanced the anti-platelet aggregation effect of sodium nitroprusside (NO donor). In anesthetized rabbits, the combination of heparin and sildenafil has a superposition effect on prolonging bleeding time, but similar human studies have not been carried out. After a single oral dose of sildenafil 100mg in healthy volunteers, sperm motility and morphology were not affected.
Pharmacokinetics Sildenafil is absorbed rapidly after oral administration, and its absolute bioavailability is about 40%. Its pharmacokinetic parameters are directly proportional to the dose within the recommended dose range. Eliminate liver metabolism (cytochrome p450 isoenzyme 3A4 pathway) and generate an active metabolite, whose properties are similar to sildenafil. When powerful inhibitors of cytochrome p450 isoenzyme 3A4(CYp4503A4) (such as erythromycin, ketoconazole and itraconazole) and nonspecific inhibitors of cytochrome p450 (such as cimetidine and sildenafil) are used at the same time, the elimination half-life of sildenafil and its metabolites is about 4 hours. When 25 ~ 100 mg was given on an empty stomach, the plasma concentration (Cmax) of about 1 hour reached 127 ~ 560 ng/ml. The selectivity of sildenafil or its main metabolite N- demethylation to pDE5 is about 50%, and the protein binding rate is 96%. At a higher total plasma concentration of sildenafil, the Cmax of free sildenafil is 22ng/ml. After oral or intravenous administration, sildenafil is mainly excreted from feces in the form of metabolites (about 80% of the oral dose), and a small part is excreted from urine (about 13% of the oral dose). Pharmacokinetics of special population: elderly: healthy elderly volunteers (? The clearance rate of sildenafil in 65-year-old volunteers decreased, and the free blood concentration was about 40% higher than that in young healthy volunteers (18-45 years old). Renal Insufficiency: The pharmacokinetics of 50 mg sildenafil in volunteers with mild (creatinine clearance is equal to 50-80 ml/min) and moderate (creatinine clearance is equal to 30-49 ml/min) renal impairment did not change. Severe renal damage (creatinine clearance is equal to? 30ml/ min), the clearance rate of sildenafil decreased, and the area under the drug-time curve (AUC) and Cmax almost doubled compared with the volunteers without renal damage in the same age group. Hepatic insufficiency: The clearance rate of sildenafil in patients with liver cirrhosis (Child-pugh Grade A and B) decreased, while AUC and Cmax increased by 84% and 47% respectively compared with those without liver injury in the same age group. Therefore, the age over 65, liver function damage and severe renal function damage will lead to the increase of plasma sildenafil level. The initial dose for such patients is 25 mg.
Adverse reactions are not clear.
Note: The interaction between sildenafil and nitrate which affects blood pressure can last from the time of administration to the whole 6-hour observation period. Therefore, in any case, sildenafil combined with organic nitrate or not providing any medicine (such as sodium nitroprusside) is taboo. Sildenafil should be used with caution in the following patients: anatomical deformity of penis (such as penile deviation, cavernous fibrosis, Peroni's disease) and diseases that easily cause abnormal erection of penis (such as sickle cell anemia, multiple myeloma, leukemia). The safety and effectiveness of other methods combined with Ginger in the treatment of erectile dysfunction have not been studied, so it is not recommended to use them together. When there are cardiovascular risk factors, there is a risk of non-fatal/fatal cardiac events after medication. If angina pectoris, dizziness, nausea and other symptoms appear at the beginning of sexual activity, sexual activity must be terminated. After Jinge was approved to be listed abroad, there were a few reports of prolonged erection time (more than 4 hours) and abnormal erection (erectile pain more than 6 hours). If the erection lasts more than 4 hours, the patient should seek medical attention immediately. If abnormal erection is not treated immediately, penis tissue may be damaged and permanent erection function may be lost. Sildenafil has no protective effect on sexually transmitted diseases.
Patients who are forbidden to take nitrates in any dosage form, whether taking them regularly or intermittently, are contraindications. Patients who are allergic to any component of sildenafil are prohibited.
drug interaction
Effects of other drugs on sildenafil: In vitro experiment: Ginger's metabolism is mainly through cytochrome p4503A4 (primary pathway) and 2C9 (secondary pathway), so these isoenzyme inhibitors will reduce the clearance rate of sildenafil. In vivo experiment: Healthy volunteers took 50 mg of ginger and 800 mg of cimetidine (a nonspecific cytochrome p450 inhibitor) at the same time, resulting in a 56% increase in the plasma concentration of sildenafil. When a single dose of sildenafil (100mg) was combined with erythromycin (500mg, twice a day, reaching a steady state for 5 days), the AUC of sildenafil increased by 182%. A single dose of sildenafil (100mg) was used in combination with another inhibitor of CYp4503A4 HIV protease, saquinavir. When the steady state is reached (1200mg, three times a day), the Cmax and AUC of the latter increase by 140% and 2 10% respectively. Sildenafil did not affect the pharmacokinetics of the latter. More powerful CYp4503A4 inhibitors such as ketoconazole and itraconazole may have greater effects. When combined with CYp4503A4 inhibitors (such as ketoconazole, erythromycin and cimetidine), the clearance rate of sildenafil decreased. It can be predicted that taking inducer CYp4503A4 (such as rifampicin) at the same time will reduce the plasma sildenafil level. A single dose of antacid (aluminum hydroxide/magnesium hydroxide) has no effect on the bioavailability of ginger. CYp4502C9 inhibitors (such as tolbutamide and warfarin), CYp4502D6 inhibitors (such as selective serotonin reuptake inhibitors and tricyclic antidepressants), thiazide and thiazide diuretics, angiotensin converting enzyme inhibitors and calcium channel blockers have no effect on the pharmacokinetics of sildenafil. Loop diuretics and potassium-sparing diuretics can increase the AUC of the active metabolite of sildenafil (N- demethylsildenafil) by 62%, but they are not selective? -Receptor blockers increase it by 102%. These effects on sildenafil metabolites will not cause clinical changes. Effects of sildenafil on other drugs: In vitro experiment: Gingert is a cytochrome p450 1A2, 2C9, 2C 19, 2D6, 2E 1 and 3A4 (IC50 >: 150? M) is a weak inhibitor. Because the peak blood concentration of sildenafil after taking the recommended dose is about 1? So sildenafil will not change the clearance of these isoenzymes. In vivo test: When patients with hypertension take sildenafil (100mg) and amlodipine 5mg or 10mg at the same time, the average systolic blood pressure and diastolic blood pressure in supine position further decrease by 87mmHg. There is no obvious interaction between tolbutamide (250mg) and warfarin (40mg) metabolized by CYp4502C9 and sildenafil. Sildenafil (50mg) did not increase the bleeding time caused by aspirin (150mg). When the average plasma alcohol concentration of healthy volunteers was 0.08%, sildenafil (50mg) did not enhance the antihypertensive effect of alcohol. Sildenafil (100mg) did not affect the steady-state pharmacokinetics of HIV protease inhibitors, such as saquinavir and ritonavir (substrates of CYp4503A4).
Storage and shading, sealed preservation.
Validity 18 months.
Guangzhou Baiyun Mountain Pharmaceutical Co., Ltd. Guangzhou Baiyun Mountain Pharmaceutical General Factory
Frequently asked questions about Jin Ge taking medicine.
Q: There are many methods to treat impotence in clinic, among which drug therapy is the main one. Ginger is a drug for treating impotence, which can make patients with erectile dysfunction have a natural erectile response to sexual stimulation. After determining the therapeutic effect of Jinge, what are the contraindications for using Jinge?
A: Jin Ge's contraindication is that patients who take any dosage form of nitrate drugs are contraindications, whether they take it regularly or intermittently. Patients who are allergic to any component of sildenafil are prohibited. The use of ginger needs to be under the guidance of a doctor. If the patient feels uncomfortable during use, he needs to contact the patient's attending doctor. Usage and dosage of Jinge: For most patients, the recommended dosage is 50 mg, which should be taken as needed before sexual activity 1 hour; But it can be taken at any time within 0.5~4 hours before sexual activity. According to the curative effect and tolerance, the dose can be increased to 100 mg (recommended dose) or decreased to 25 mg, and taken once a day.