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Composition:


active ingredient: sildenafil;


1 tablet contains 50 mg of sildenafil;


excipients: lactose monohydrate, magnesium gluconate, powdered sugar, calcium stearate, lemon flavor, tartrazine dye (E 102).


Dosage form. Pills.


Basic physical and chemical properties: biconvex tablets of yellow color interspersed with a dividing line on one side and the company logo on the other.


Pharmacotherapeutic group. Remedies used for erectile dysfunction. Sildenafil. ATX code G04B E03.

Clinical characteristics.


Indications.


Sildenafil is recommended for men with erectile dysfunction, which is defined as the inability to achieve or maintain the penile erection necessary for successful sexual intercourse.


The effective action of Sildenafil requires sexual arousal.


Contraindications.


- Hypersensitivity to the active substance or to any of the excipients of the drug.


- Concomitant use with nitric oxide donors (such as amyl nitrite) or nitrates in any form, since sildenafil is known to affect the metabolic pathways of nitric oxide (no)/cyclic guanosine monophosphate (cGMP) and potentiates the hypotensive effect of nitrates.


- Concomitant use of PDE-5 inhibitors (including sildenafil) with guanylate cyclase stimulants such as riociguate, as this may lead to symptomatic hypotension (see Section "interactions with other drugs and other types of interactions").


- Conditions for which sexual activity is not recommended (for example, severe cardiovascular disorders, such as unstable angina or severe heart failure).


- Loss of vision in one eye due to non-arterial anterior ischemic neuropathy of the optic nerve, regardless of whether this pathology is associated with previous use of PDE-5 inhibitors or not.


- The presence of diseases such as severe liver function disorders, hypotension (blood pressure below 90/50 mm Hg). recent stroke or myocardial infarction, and known hereditary degenerative retinal diseases such as retinitis pigmentosa (a small number of such patients have genetic disorders of retinal phosphodiesterases), since the safety of sildenafil has not been studied in such subgroups of patients.


Interactions with other drugs and other types of interactions.


Effect of other drugs on sildenafil.


In vitro studies. Sildenafil metabolism occurs mainly with the participation of isoform 3A4 (main pathway) and isoform 2c9 (secondary pathway) of cytochrome P450 (CYP). Therefore, inhibitors of these isoenzymes can reduce the clearance of sildenafil, and inducers of these isoenzymes can increase the clearance of sildenafil.


In vivo studies. Population pharmacokinetic analysis of clinical trial data showed a decrease in sildenafil clearance when co-administered with CYP3A4 inhibitors (such as ketoconazole, erythromycin, cimetidine). Although no increase in the frequency of side effects was observed with concomitant use of sildenafil and CYP3A4 inhibitors, the possibility of using an initial dose of sildenafil 25 mg should be considered.


Concomitant use of the HIV protease inhibitor ritonavir, a very powerful P450 inhibitor, at steady state concentrations (500 mg 1 time per day) and sildenafil (a single dose of 100 mg) resulted in an increase in the CMAX of sildenafil by 300 % (4 times) and an increase in the plasma AUC of sildenafil by 1000 % (11 times). After 24 hours, the plasma level of sildenafil was still approximately 200 ng/ml compared to the level of approximately 5 ng/mL characteristic of sildenafil alone, which is consistent with the significant effect of ritonavir on a wide range of P450 substrates. Sildenafil does not affect the pharmacokinetics of ritonavir. Given these pharmacokinetic data, concomitant use of sildenafil and ritonavir is not recommended (see the section "special instructions for use"); in any case, the maximum dose of sildenafil should never exceed 25 mg within 48 hours. 


Concomitant use of the HIV protease inhibitor saquinavir, a CYP3A4 inhibitor, at a dose that provides an equilibrium concentration (1200 mg 3 times a day), and sildenafil (100 mg once) resulted in an increase in the CMAX of sildenafil by 140% and an increase in the AUC of sildenafil by 210 %. There was no effect of sildenafil on the pharmacokinetics of saquinavir (see the section "dosage and administration"). More potent CYP3A4 inhibitors, such as ketoconazole and Itraconazole, are expected to have a more pronounced effect.


When using sildenafil (100 mg once) and erythromycin, a moderate CYP3A4 inhibitor, at steady state (500 mg 2 times a day for 5 days), an increase in the AUC of sildenafil was observed by 182 %. In healthy male volunteers, no effect of azithromycin (500 mg per day for 3 days) on AUC, Cmax, Tmax, elimination rate constant, and subsequent Half-Life of sildenafil or its main circulating metabolite was observed. Cimetidine (cytochrome P450 inhibitor and non-specific CYP3A4 inhibitor) at a dose of 800 mg when co-administered with sildenafil at a dose of 50 mg in healthy volunteers resulted in a 56% increase in the plasma concentration of sildenafil.


Grapefruit juice is a weak inhibitor of CYP3A4 in the intestinal wall and can cause a moderate increase in plasma sildenafil levels.


A single dose of antacids (magnesium hydroxide/aluminum hydroxide) did not affect the bioavailability of sildenafil.


Although studies of specific interaction with all drugs have not been conducted (according to population pharmacokinetic analysis), the pharmacokinetics of sildenafil did not change when it was co-administered with drugs belonging to the group of CYP2C9 inhibitors (tolbutamide, warfarin, phenytoin), the group of CYP2D6 inhibitors (such as selective serotonin reuptake inhibitors, tricyclic antidepressants), the group of thiazide and thiazide-like diuretics, loop and potassium-sparing diuretics, angiotensin-converting enzyme inhibitors, calcium antagonists, beta-adrenergic antagonists or inducers of CYP450 metabolism (such as rifampicin, barbiturates).


In a study involving healthy male volunteers, concomitant use of the endothelin antagonist bosentan (a moderate inducer of CYP3A4, CYP2C9, and possibly CYP2C19) at steady state (125 mg 2 times a day) and sildenafil at steady state (80 mg 3 times a day) resulted in a decrease in the AUC and Cmax of sildenafil by 62.6% and 55.4%, respectively. Therefore, the simultaneous use of such powerful CYP3A4 inducers as rifampin may lead to a more pronounced decrease in the concentration of sildenafil in blood plasma.


Nicorandil is a hybrid of calcium channel activator and nitrate. The nitrate component determines the possibility of its serious interaction with sildenafil.


Effect of sildenafil on other medications.


In vitro studies. Sildenafil is a weak inhibitor of cytochrome P450 isoforms 1A2, 2c9, 2c19, 2d6, 2e1, and 3A4 (IC50 >150 mmol). Since the peak plasma concentrations of sildenafil are approximately 1 mmol, the effect of the drug on the clearance of substrates of these isoenzymes is unlikely.


There are no data on the interaction of sildenafil and non-specific phosphodiesterase inhibitors such as theophylline and Dipyridamole.


In vivo studies. Since sildenafil is known to affect the metabolism of no/cGMP, it was found that sildenafil potentiates the hypotensive effect of nitrates, so its simultaneous use with nitric oxide donors or with nitrates in any form is contraindicated (see the section "contraindications").


Riociguat. Preclinical studies have demonstrated an additive systemic effect of lowering blood pressure when PDE-5 inhibitors are co-administered with riociguate. Clinical studies have shown that riociguate enhances the hypotensive effect of PDE-5 inhibitors. in patients who participated in the study, no positive clinical effect was observed when PDE-5 inhibitors were co-administered with riociguate. Concomitant use of riociguate with PDE-5 inhibitors, including sildenafil, is contraindicated (see the section "contraindications").


Concomitant use of sildenafil and alpha-adrenergic blockers may lead to the development of symptomatic hypotension in some predisposed patients. This reaction most often occurred within 4 hours after the use of sildenafil (see the sections "features of Use" and "dosage and administration"). In 3 studies of the specific interaction of alpha-adrenergic blockers, Doxazosin (4 mg and 8 mg) and sildenafil (25 mg, 50 mg and 100 mg) were used simultaneously in patients with Benign Prostatic Hyperplasia, whose condition was stabilized with Doxazosin. In these populations, an average additional reduction in blood pressure was observed in the patient's supine position by 7/7 mmHg. St., 9/5 mm Hg. St. and 8/4 mmHg. and the average decrease in blood pressure in the patient's standing position by 6/6 mm Hg. St., 11/4 mm Hg. St., 4/5 mm Hg. Art. respectively. With the simultaneous use of sildenafil and Doxazosin in patients whose stabilization was achieved with the use of Doxazosin, the development of symptomatic orthostatic hypotension has sometimes been reported. These reports reported cases of dizziness and pre-fainting, but no syncope.


No significant interactions were observed with concomitant administration of sildenafil (50 mg) and tolbutamide (250 mg) or warfarin (40 mg) metabolized by CYP2C9.


Sildenafil (50 mg) did not prolong the bleeding time caused by the use of acetylsalicylic acid (150 mg).


Sildenafil (50 mg) did not potentiate the hypotensive effect of alcohol in healthy volunteers with an average maximum blood ethanol level of 80 mg/dL.

In patients treated with sildenafil, there were no differences in the side-effect profile compared to placebo with concomitant use of such classes of antihypertensive drugs as diuretics, beta-adrenergic blockers, ACE inhibitors, angiotensin II antagonists, antihypertensive drugs (vasodilators and central action), adrenergic neuron blockers, calcium channel blockers and alpha-adrenergic blockers. In a special interaction study, concomitant use of sildenafil (100 mg) and amlodipine in patients with arterial hypertension showed an additional decrease in systolic blood pressure in the supine position by 8 mm Hg. the corresponding decrease in diastolic blood pressure was 7 mm Hg. in terms of magnitude, these additional reductions in blood pressure were comparable to those observed with sildenafil alone in healthy volunteers (see the section "pharmacological properties").


Sildenafil at a dose of 100 mg did not affect the pharmacokinetic parameters of HIV protease inhibitors, saquinavir and ritonavir, which are substrates of CYP3A4.


In healthy male volunteers, the use of sildenafil at steady state (80 mg 3 times a day) resulted in an increase in the AUC and Cmax of bosentan (125 mg 2 times a day) by 49.8% and 42%, respectively.


Application features.


Before starting therapy, the patient's medical history should be collected and a physical examination should be performed to diagnose erectile dysfunction and determine its possible causes.


Risk factors for cardiovascular diseases. Since sexual activity is accompanied by a certain risk from the heart, before starting any treatment for erectile dysfunction, the doctor should assess the condition of the patient's cardiovascular system. Sildenafil has a vasodilating effect, which is manifested by a slight and short-term decrease in blood pressure (see the section "pharmacodynamics"). Before prescribing sildenafil, the doctor should carefully weigh whether this effect can adversely affect patients with certain underlying diseases, especially in combination with sexual activity. Patients with hypersensitivity to vasodilators include patients with obstruction of the left ventricular excretory tract (for example, aortic stenosis, Hypertrophic Obstructive Cardiomyopathy) and patients with rare multisystem atrophy syndrome, one of the manifestations of which is a severe violation of blood pressure regulation by the autonomic nervous system.


Sildenafil potentiates the hypotensive effect of nitrates (see the section "contraindications").


In the post-marketing period, severe cardiovascular adverse reactions were reported, including myocardial infarction, unstable angina, sudden cardiac death, ventricular arrhythmia, cerebrovascular hemorrhage, transient ischemic attack, arterial hypertension and hypotension, which coincided with the use of sildenafil. Most patients, but not all, had Risk Factors for cardiovascular disease. Many of these adverse reactions were observed during or immediately after sexual intercourse, and only a few occurred shortly after using sildenafil without sexual activity. Therefore, it is impossible to determine whether the development of such adverse reactions is directly related to risk factors, or their development is due to other factors.


Priapism. Medications for the treatment of erectile dysfunction, including sildenafil, should be used with caution in patients with anatomical deformity of the penis (angulation, cavernous fibrosis, or Peyronie's disease) or in patients with conditions that cause the development of priapism (sickle cell anemia, multiple myeloma, or leukemia).


Cases of prolonged erections and priapism have been reported since sildenafil entered the market. If an erection lasts longer than 4 hours, patients should seek immediate medical attention. If left untreated immediately, priapism can lead to penile tissue damage and permanent loss of potency.


Concomitant use with other PDE5 inhibitors or other medications for the treatment of erectile dysfunction. The safety and efficacy of concomitant use of sildenafil with other PDE-5 inhibitors or other drugs for the treatment of pulmonary hypertension containing sildenafil, or with other drugs for the treatment of erectile dysfunction, have not been studied. Therefore, the use of such combinations is not recommended.


Effects on vision. Spontaneous reports of visual defects have been associated with the use of sildenafil and other PDE-5 inhibitors (see Section "adverse reactions"). Cases of non-arterial anterior ischemic optic neuropathy, which is a rare condition, have been reported spontaneously and have been reported in an observational study associated with the use of sildenafil and other PDE-5 inhibitors (see Section "adverse reactions"). Patients should be warned that in case of sudden visual impairment, the use of ergos® should be discontinued and immediately consult a doctor (see below). Section "contraindications").


Concomitant use with ritonavir. Concomitant use of sildenafil and ritonavir is not recommended (see the section "interactions with other drugs and other types of interactions").


Concomitant use with alpha-adrenergic blockers. Patients who use alpha-adrenergic blockers should use sildenafil with caution, as this combination may lead to symptomatic hypotension in some predisposed patients. Symptomatic hypotension usually occurs within 4 hours of sildenafil administration. In order to minimize the possible development of postural hypotension in patients using alpha-adrenergic blockers, their condition should be stabilized with alpha-adrenergic blockers before starting sildenafil. An initial dose of 25 mg should also be considered (see "dosage and administration"). In addition, patients should be informed how to proceed in case of symptoms of orthostatic hypotension.


Effect on Bleeding. Human platelet studies have shown that sildenafil potentiates the antiplatelet effects of sodium nitroprusside in vitro. There is no information on the safety of sildenafil in patients with blood clotting disorders or acute peptic ulcer disease. Thus, the use of sildenafil in patients in this group is possible only after careful assessment of the benefit-risk ratio.


After administration of a dose of 100 mg in healthy volunteers, no effect on sperm morphology or motility was observed (see the section "pharmacodynamics").


Hearing loss. Doctors should advise patients to stop using ergos® and seek immediate medical attention in case of sudden hearing loss or loss. These events, which may also be accompanied by tinnitus and dizziness, have been reported to be associated over time with the use of PDE-5 inhibitors, including ergos®. It is impossible to determine whether these phenomena are directly related to the use of PDE-5 inhibitors or other factors.


Concomitant use with antihypertensive drugs. Sildenafil has a systemic vasodilating effect and can further reduce blood pressure in patients using antihypertensive drugs. In a separate drug interaction study, concomitant oral administration of amlodipine (5 mg or 10 mg) and sildenafil (100 mg) showed an average additional decrease in systolic pressure by 8 mm Hg. St., diastolic-by 7 mm Hg. art.


Sexually transmitted diseases. The use of ergos® does not protect against sexually transmitted diseases. Consideration should be given to informing patients about the necessary precautions to protect against sexually transmitted diseases, including human immunodeficiency virus.


The drug contains lactose. It should not be used in men with rare hereditary disorders such as galactose intolerance, Lappa lactase deficiency, or glucose-galactose malabsorption.


The composition of the drug includes powdered sugar. If you are found to be intolerant to certain sugars, you should consult your doctor before using this medicine.


The composition of the drug includes the dye E 102, which can cause allergic reactions when using it.

Dosage and administration.


The drug is used orally.


Adults. The recommended dose of ergos® is 50 mg, used if necessary approximately one hour before sexual activity. Depending on the effectiveness and tolerability of the drug, the dose can be increased to 100 mg or reduced to 25 mg in tablets. The maximum recommended dose is 100 mg. The frequency of use of the maximum recommended dose of the drug is 1 time per day. When using the drug during food intake, its effect may occur later than when used on an empty stomach.


Elderly patients. There is no need for dose adjustment in elderly patients (≥ 65 years).


Patients with renal insufficiency. For patients with mild to moderate renal insufficiency (creatinine clearance 30-80 mL/min), the recommended dose of the drug is the same as indicated above in the section "adults".


Since in patients with severe renal insufficiency (creatinine clearance 25 mg. Depending on the effectiveness and tolerability of the drug, if necessary, the dose can be increased gradually to 50 mg and up to 100 mg.


Patients with hepatic insufficiency. Since sildenafil clearance is reduced in patients with hepatic insufficiency (e.g. cirrhosis), a dose of 25 mg should be considered. Depending on the effectiveness and tolerability of the drug, if necessary, the dose can be increased gradually to 50 mg and up to 100 mg.


Patients who use other medications. If patients are using CYP3A4 inhibitors at the same time (with the exception of ritonavir, which is not recommended to be used simultaneously with sildenafil, see the sections "interactions with other drugs and other types of interactions" and "application features", the possibility of using an initial dose of 25 mg should be considered).


In order to minimize the possible development of postural hypotension in patients using alpha-adrenergic blockers, the condition of such patients should be stabilized with alpha-adrenergic blockers before starting sildenafil. The possibility of using an initial dose of 25 mg should also be considered (see the sections "interactions with other drugs and other types of interactions" and "application specifics").


Children.


The drug is not indicated for use by persons under 18 years of age.


Overdose.


In clinical trials involving volunteers, when using a single dose of sildenafil up to 800 mg, adverse reactions were similar to those observed with sildenafil in lower doses, but occurred more often and were more severe. The use of sildenafil at a dose of 200 mg did not lead to an increase in the effectiveness, but caused an increase in the number of cases of adverse reactions (headache, hot flashes, dizziness, dyspepsia, nasal congestion, visual disorders).


In case of overdose, if necessary, resort to the usual supportive measures. Acceleration of sildenafil clearance during hemodialysis is unlikely due to the high degree of Binding of the drug to plasma proteins and the lack of elimination of sildenafil in the urine.


Adverse reactions.


The most common adverse reactions reported in clinical trials among patients taking sildenafil were headache, hot flashes, dyspepsia, nasal congestion, back pain, dizziness, nausea, visual impairment, cyanopsia, and blurred vision. Information on adverse reactions in the post-marketing follow-up of sildenafil has been collected for more than 10 years. The following are all clinically important adverse reactions that occurred in clinical trials of sildenafil with a frequency greater than that of placebo, by body system and frequency: very common (≥1/10), often (≥1/100,


Also included is the frequency of clinically important adverse reactions reported from post-marketing experience as unknown.


In each group, the frequency of side effects is indicated in descending order of manifestations.


Infectious and invasive diseases


Infrequently: rhinitis.


From the immune system


Infrequently: hypersensitivity.


From the nervous system


Very common: headache.


Often dizziness.


Infrequently: drowsiness, hypesthesia.


Rare: stroke, transient ischemic attack, seizures*, recurrent seizures*, syncope.


From the side of the visual organs


Often: impaired color perception**, visual disturbances, blurred vision.


Infrequently: lacrimation disorders***, eye pain, photophobia, photopsia, eye hyperemia, visual brightness, conjunctivitis.


Rare: non-arterial anterior ischemic neuropathy of the optic nerve*, retinal vascular occlusion*, retinal hemorrhage, arteriosclerotic retinopathy, retinal disorders, glaucoma, visual field defects, diplopia, decreased visual acuity, myopia, asthenopia, floating opacities of the vitreous body, Iris disorders, mydriasis, the appearance of shining circles around a light source (Halo) in the visual field, eye edema, eye swelling, eye disorders, conjunctival hyperemia, eye irritation, abnormal sensations in the eyes, swelling of the eyelids, discoloration of the sclera.


From the side of the hearing organs and vestibular apparatus


Infrequently dizziness, ringing in the ears.


Rare: deafness.


From the side of the heart


Infrequently: tachycardia, increased heart rate.


Rare: sudden cardiac death*, myocardial infarction, ventricular arrhythmia*, atrial fibrillation, unstable angina.


From the side of blood vessels


Often: flushes of blood to the face, hot flashes.


Infrequently: arterial hypertension, hypotension.


From the respiratory system, chest and mediastinal organs


Common: nasal congestion.


Infrequently: nosebleeds, sinus congestion.


Rare: tightness in the throat, swelling of the nasal mucosa, dryness in the nose.

Tags: Sildenafil