JINOFIL [Sildenafil] 100 mg Film-coated tablets
JINOFIL
instructions for medical use of the medicinal product
Tradename
Ginofil, Jinofil
International non-proprietary name
Sildenafil, Sildenafil
Compound
Ginophil 25 mg
Each film-coated tablet contains:
Sildenafil citrate 35.12 mg
equiv. Sildenafil 25 mg
Ginophil 50 mg
Each film-coated tablet contains:
Sildenafil citrate 70 mg
equiv. Sildenafil 50 mg
Ginophil 100 mg
Each film-coated tablet contains:
Sildenafil citrate 140 mg
equiv. Sildenafil 100 mg
Excipients: lactose monohydrate, microcrystalline cellulose PH 102, croscarmellose sodium, magnesium stearate, colloidal silicon dioxide (Aerosil 200), purified talc, hydroxypropyl methylcellulose 2910, hydroxypropyl methylcellulose L.F. cellulose, dibutyl phthalate, titanium dioxide, patent blue, Siko indigotine lake ) E132 ( methylene chloride, methanol.
Dosage form
Tablets.
Pharmacotherapeutic group
Preparations for the treatment of erectile dysfunction.
Pharmacological properties
Sildenafil is an oral therapy for erectile dysfunction. Under natural conditions, that is, with sexual stimulation, it restores impaired erectile function by increasing blood flow to the penis.
The physiological mechanism responsible for penile erection involves the release of nitric oxide in the cavernous body during sexual simulation. Nitric oxide then activates the enzyme guanylate cyclase, which leads to an increase in cyclic guanosine monophosphate (cGMP), causing smooth muscle relaxation in the corpus cavernosum and allowing blood flow. Sildenafil is an apotent and selective inhibitor of cGmp -specific phosphodiesterase type 5 in the cavernous body, where PDE 5 is responsible for the degradation of cGMP . Sildenafil has a peripheral site of action on erection.
Sildenafil does not have a direct relaxing effect on isolated human corpora cavernosa, but greatly enhances the relaxant effect. When the No / GMP pathway is activated, as occurs with sexual stimulation, PDE5 inhibition by sildenafil results in an increase in GMP levels in the corpus cavernosum. Therefore, sexual modeling is necessary for sildenafil to produce its intended beneficial pharmacological effects.
Pharmacodynamics
Research in
vitro have shown that sildenafil is selective for PDE 5, which is involved in the erection process. Its action is stronger on PDE 5 than on other known phosphodiesterases. There is a 10-fold selectivity for PDE 6, which is involved in the phototransduction pathway in the retina. At the maximum recommended doses, there is an 80-fold selectivity for PDE 1 and more than 700-fold for PDE 2, 3, 4, 7, 8, 9, 10 and 11. In particular, sildenafil has more than 4000-fold selectivity for PDE 5 for compared to PDE 3, the cAMP-specific phosphodiesterase isoform is involved in the control of cardiac contractility.
Pharmacokinetics
Sildenafil is rapidly absorbed. The maximum observed plasma concentrations are reached within 30-120 minutes after oral administration. The mean absolute oral bioavailability is 41%.
After oral administration of sildenafil, AUC and C max increase in proportion to the dose in the recommended dose range (25-100 mg).
When sildenafil is taken with food, the absorption rate decreases with an average delay tmax of 60 minutes and an average decrease in Cmax of 29%.
The mean volume of sustained distribution for sildenafil is 105 L, indicating tissue distribution. After a single oral dose of 100 mg, the mean maximum total plasma concentration of sildenafil is approximately 440 ng/mL. Since sildenafil is 96% bound to plasma proteins, this results in an average maximum free plasma concentration for sildenafil of 18 ng/mL. Protein binding is independent of the total drug concentration.
In healthy volunteers treated with sildenafil, less than 0.0002% of the administered dose was present in the ejaculate 90 minutes after the dose.
Sildenafil is predominantly cleared by liver isoenzymes CYP 3 A 4 and CYP 2 C 9. The main circulating metabolite is the result of N -dernetylation of sildenafil. This metabolite has a phosphodiesterase selectivity profile similar to sildenafil and potency in in vitro for PDE 5 approximately 50% higher than the parent drug. The plasma concentration of this metabolite is approximately 40% of the concentrations observed for sildenafil. The N -desmethyl metabolite is further metabolized with a terminal half-life of approximately 4 hours.
The total clearance of sildenafil is 41 l / h with a terminal half-life of 35 hours. After oral administration, sildenafil is excreted as metabolites, predominantly in the feces (approximately 80% of the administered oral dose) and to a lesser extent in the urine (approximately 13% of the administered oral dose).
Indications for use
Erectile dysfunction, characterized by the inability to achieve or maintain an erection of the penis sufficient for satisfactory intercourse.
Dosage and administration
For oral use.
Dosage: The recommended dose is 50 mg taken as needed approximately one hour before sexual activity. When taking the drug with food, the onset of activity may be delayed compared to the fasting state. Based on efficacy and tolerability, the dose may be increased to 100 mg or reduced to 25 mg. The maximum recommended dose is 100 mg.
The maximum recommended dosing frequency is once a day.
Special Populations:
Elderly : Dosage adjustment is not required in elderly patients (≥65 years).
Renal failure. Since the clearance of sildenafil is reduced in patients with renal insufficiency (creatinine clearance <30 ml/min), a dose of 25 mg should be considered. Depending on efficacy and tolerability, the dose may be increased in steps from 50 mg to 100 mg as needed.
Hepatic insufficiency: Since the clearance of sildenafil is reduced in patients with hepatic insufficiency (eg, cirrhosis), a dose of 25 mg should be considered. Based on efficacy and tolerability, the dose may be increased gradually from 50 mg to 100 mg as needed.
Contraindications
In the presence of hypersensitivity to the active substance. Use in patients receiving permanently or intermittently nitric oxide donators, organic nitrates or nitrites in any form, since sildenafil enhances the hypotensive effect of nitrates.
Sildenafil should not be used in men for whom sexual activity is inappropriate (for example, in patients with severe cardiovascular disorders such as unstable angina or severe heart failure).
Contraindicated in patients with anterior ischemic optic neuropathy.
Sildenafil is not intended for use in children under 18 years of age and women.
Special instructions and precautions
To diagnose erectile dysfunction, determine their possible causes and select adequate treatment, it is necessary to collect a complete medical history and conduct a thorough physical examination.
Drugs intended for the treatment of erectile dysfunction should not be prescribed to men for whom sexual activity is undesirable. Sexual activity poses a certain risk in the presence of heart disease (heart failure, unstable angina, myocardial infarction or stroke in the last 6 months, life-threatening arrhythmia, arterial hypertension (BP> 170/100 mmHg) or hypotension (BP < 90/ 50 mm Hg), use with caution in patients with anatomical deformity of the penis (angulation, cavernous fibrosis or Peyronie's disease), in diseases predisposing to the development of priapism (sickle cell anemia, multiple myeloma, leukemia, thrombocythemia), diseases accompanied by bleeding (exacerbation of gastric ulcer and duodenal ulcer), diabetes mellitus, and shemic optic neuropathy, hereditary retinitis pigmentosa.
Interaction with other drugs
The metabolism of sildenafil occurs mainly under the action of cytochrome isoenzymes CYP3A4 (the main pathway) and CYP2C9, therefore inhibitors of these isoenzymes can reduce the clearance of sildenafil, and inducers, respectively, increase the clearance of sildenafil.
With the simultaneous use of CYP3A4 inhibitors (erythromycin, cimetidine), the clearance of sildenafil decreases, the concentration of sildenafil in the blood plasma increases.
With the simultaneous use of indinavir, saquinavir, ritonavir, plasma Cmax and AUC of sildenafil increase, which is due to inhibition of the CYP3A4 isoenzyme under the influence of indinavir, saquinavir, ritonavir.
It can be expected that stronger inhibitors of the CYP3A4 isoenzyme, such as ketoconazole or itraconazole, will increase the concentration of sildenafil in blood plasma.
With simultaneous use with nitrates, the hypotensive effect of nitrates is enhanced.
Influence on the ability to drive a car
Against the background of taking sildenafil, no negative effect on the ability to drive a car or other technical means was observed. However, since when taking sildenafil, a decrease in blood pressure, the development of chromatopsia, blurred vision, etc. is possible. side effects, you should carefully consider the individual effect of the drug in these situations, especially at the beginning of treatment and when changing the dosing regimen.
Side effect
Usually, the side effects of the drug are mild or moderate and are transient.
From the side of the central nervous system:
• headache, hot flashes, dizziness, insomnia.
From the digestive system:
• dyspepsia, asthenia, diarrhea, abdominal pain, nausea.
From the musculoskeletal system:
• arthralgia, myalgia, increased muscle tone.
From the respiratory system:
• nasal congestion, pharyngitis, rhinitis, sinusitis, respiratory infections, respiratory failure.
From the side of the organ of vision:
• vision changes (mild and transient;
• mainly change in the color of objects, as well as increased perception of light and blurred vision), conjunctivitis.
Others:
• possible flu-like syndrome, development of infectious diseases, symptoms of vasodilation, back pain, rash, urinary tract infection, prostate dysfunction;
• in isolated cases - priapism.
Overdose
With a single dose of sildenafil at a dose of up to 800 mg, adverse events were comparable to those when taking the drug at lower doses, but were more common. Treatment is symptomatic. Hemodialysis does not accelerate the clearance of sildenafil, since the latter is actively bound to plasma proteins and is not excreted by the kidneys.
Storage conditions
Store in a dry place, at a temperature not exceeding 30 0 C. Keep out of the reach of children.
Best before date
2 years. Do not use after the expiry date stated on the package.
Holiday conditions
Released by prescription.
Release form
Ginophil 25 mg
10 film-coated tablets in a strip pack together with instructions for medical use in a cardboard box.
Ginophil 50 mg
4 film-coated tablets in a strip pack together with instructions for medical use in a cardboard box.
Ginophil 100 mg
4 film-coated tablets in a strip pack together with instructions for medical use in a cardboard box.