Sinegra® 12s 25 mg coated tablets

Composition

One tablet contains
sildenafil citrate 35.12 mg, 70.24 mg, 140.48 mg equivalent to 25 mg, 50 mg, 100 mg sildenafil, respectively

Packaging

4 contour packs with 1 tablet, together with instructions for medical use in the state and Russian languages, are placed in a cardboard box.

Description

Blue film-coated tablets, square, with arrows on one side.

Dosage

25 mg

Indications

- treatment of erectile dysfunction, characterized by the inability to achieve or maintain an erection of the penis sufficient for a satisfactory sexual intercourse.
SINEGRA® is effective only when there is sexual stimulation.

Shelf Life

2 year

Release Form

1 contour package with 1 or 4 tablets; 4 contour packs with 1 tablet or 3 contour packs with 4 tablets (for SINEGRA® 50 and SINEGRA® 100) together with instructions for medical use in the state and Russian languages ​​are placed in a cardboard box.

Overdose

Symptoms: increased side effects.
Treatment: symptomatic. Dialysis does not accelerate the clearance of sildenafil, since the latter actively binds to blood plasma proteins and is not excreted in the urine.

Pharmodynamics

The effect of SINEGRA® develops approximately 30 - 60 minutes after administration. The severity of erection, in general, increases with an increase in the dose of sildenafil and an increase in its concentration in plasma. SINEGRA® causes a decrease in systolic / diastolic blood pressure by an average of 8.4 / 5.5 mm Hg, which is most often observed within one to two hours after taking the drug. When taking SINEGRA® 25, SINEGRA® 50 and SINEGRA® 100, the same effect on blood pressure is observed and, therefore, this effect of sildenafil does not depend on the dose or the level of the drug in plasma within the dosage range from 25 mg to 100 mg.
SINEGRA® does not have a direct relaxing effect on the corpus cavernosum alone, but enhances the effect of nitric oxide by inhibiting phosphodiesterase type 5 (PDE 5), which is responsible for the breakdown of cyclic guanosine monophosphate (c-GMP) in the corpus cavernosum. When a local release of nitric oxide occurs during sexual arousal, inhibition of PDE 5 leads to an increase in the level of c-GMP in the corpus cavernosum, resulting in relaxation of smooth muscles and blood flow to the corpus cavernosum.

Interaction

SINEGRA® is a weak inhibitor of cytochrome P450 isoenzymes - 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 (IC50> 150 μmol). When CINEGRA® is taken in recommended doses, its Cmax is about 1 μmol, therefore it is unlikely that CINEGRA® can affect the clearance of substrates of these isoenzymes.
CINEGRA® enhances the hypotensive effect of nitrates both with prolonged use of the latter and with their appointment for acute indications. In this regard, the use of CINEGRA® in combination with nitrates or nitric oxide donors is contraindicated.
There were no signs of significant interaction with tolbutamide (250 mg) or warfarin (40 mg), which are metabolized by CYP2C9.
CINEGRA® (100 mg) has no effect on the pharmacokinetics of HIV protease inhibitors, saquinavir and ritonavir, which are substrates of CYP3A4, at a constant level in the blood.
CINEGRA® (50 mg) does not cause an additional increase in bleeding time when taking acetylsalicylic acid (150 mg).
CINEGRA® (50 mg) does not enhance the hypotensive effect of alcohol.
With the simultaneous use of CINEGRA® with amlodipine in patients with arterial hypertension, no significant clinical interactions were noted. The average additional decrease in blood pressure in the supine position is 8 mm Hg. Art. (systolic) and 7 mm Hg. Art. (diastolic).
With the simultaneous administration of the alpha-blocker doxazosin (4 mg) and CINEGRA® (25 mg) in patients with benign prostatic hyperplasia, both systolic and diastolic blood pressure in the supine position is further reduced by an average of 7 mm Hg. The use of higher doses of CINERA® in conjunction with doxazosin (4 mg) occasionally led to the development of orthostatic hypotension 1-4 hours after taking the drugs. In some patients receiving alpha-blockers, the simultaneous use of SINEGRA® may lead to symptomatic hypotension. SINEGRA® enhances the antiaggregatory effect of sodium nitroprusside (nitric oxide donor).

Classifiers
ATX
0 None

INN

Sildenafil

 

Special instructions

Sildenafil has a systemic vasodilating effect, which can lead to a transient decrease in blood pressure, therefore, before prescribing CINEGRA®, the risk of adverse events in patients with cardiovascular diseases, especially against the background of sexual activity, must be carefully weighed.
An increased susceptibility to vasodilators is observed in patients with obstruction of the left ventricular outflow tract (eg, aortic stenosis, idiopathic subaortic stenosis) and in patients with severe impairment of autonomic blood pressure regulation.
In case of an erection condition, continue lasted more than 4 hours, patients should seek immediate medical attention. If priapism is not immediately healed, irreversible impotence may develop.
It is necessary to prescribe CINEGRA® with caution when used together with ritonavir, as ritonavir significantly increases the plasma concentration of sildenafil by 11 times.
To reduce the risk of side effects in patients receiving ritonavir, it is recommended that the dose of sildenafil be reduced.
Concomitant use of sildenafil and alpha-blockers may lead to hypotension in some patients. Therefore, doses of sildenafil in excess of 25 mg should not be taken within 4 hours of taking alpha-blockers. When taking higher doses of sildenafil and doxazin at a dose of 4 mg, postural hypotension may develop within 1 to 4 hours after administration.
The safety of sildenafil in patients with bleeding disorders and patients with peptic ulcers during an exacerbation is unknown.
Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms
While taking CINEGRA®, no negative effect on the ability to drive a car or other technical means was observed. However, since taking the drug may decrease blood pressure, develop chromatopsia, blurred vision, patients should be informed about the dangers associated with driving vehicles, servicing mechanical equipment and other potentially hazardous activities and are attentive to the individual action of the drug in these situations, especially at the beginning treatment and when changing the dosage regimen.

Pharmacokinetics

Sildenafil, the active ingredient of CINEGRA®, is rapidly absorbed after oral administration and the maximum plasma concentration is reached within 30 to 120 minutes (on average 60 minutes). The absolute bioavailability of the drug is about 40%. When sildenafil is taken simultaneously with fatty foods, the absorption rate decreases, and therefore the time to reach the maximum concentration (Tmax) slows down, on average, to 60 minutes and the maximum concentration (Cmax) in the blood decreases to 29%. Sildenafil and its main N-desmethyl metabolite bind to plasma proteins by about 96%. Protein binding does not depend on the total concentration of the drug.
Sildenafil is metabolized mainly by microsomal liver isoenzymes - CYP3A4 (main pathway) and CYP2C9 (minor pathway). The main metabolite, which is formed as a result of N-desmethylation of sildenafil, undergoes further metabolism. The concentration of the metabolite in plasma is approximately 40% of the concentration of sildenafil and the pharmacological effect of the metabolite is approximately 20% of the pharmacological effect of sildenafil. After oral administration, approximately 80% of the dose of the drug is excreted in the form of metabolites, mainly in the feces and about 13% in the urine

Contraindications

- hypersensitivity to any component of the drug
- Simultaneous administration of drugs that are donors of nitric oxide, organic nitrates or nitrites in any form.
Carefully:
"anatomical deformity of the penis (including angulation, cavernous fibrosis, or Peyronie's disease)
"diseases that predispose to the development of priapism (such as sickle cell anemia, multiple myeloma, leukemia, thrombocythemia)
"diseases accompanied by bleeding
"exacerbation of peptic ulcer disease
"hereditary retinitis pigmentosa
" heart failure,
"unstable angina pectoris, myocardial infarction, stroke, or life-threatening arrhythmias in the last 6 months
"arterial hypertension (blood pressure (BP)> 170/100 mm Hg) or hypotension (BP <90/50 mm Hg).
According to the registered indication, the drug is not intended for use in children under the age of 18 and in women.

Side effects

Adverse events are usually transient and mild or moderate.
The incidence of adverse events increases with dose.
Side effects%
Most common side effects (greater than or equal to 1/10)
Headache 10.8
Vasodilation ("hot flushes" of blood to the face) 10.9
Frequent side effects (greater than or equal to 1/100 and <1/10)
Dizziness 2.9
Change in vision (blurred vision, change in sensitivity to light) 2.5
Chromatopsia (mild and transient, mainly change in perception of color shades) 1.1
Rapid heartbeat 1.0
Rhinitis (nasal congestion) 2.1
Dyspepsia 3.0
The following side effects have been identified during post-marketing surveillance:
- hypersensitivity reactions (including skin rash)
- convulsions
- tachycardia, decreased blood pressure, fainting, epistaxis
- vomiting
- eye pain, eye redness / sclera injection
- prolonged erection and / or priapism.

Mode of application

To avoid complications, use strictly as directed by your doctor!
The recommended dose for most patients is 50 mg