"Sildenafil" for women: application features, reviews

• May 12, 2021
• Other drugs
• Vitalina Bronovitskaya

The drug Sildenafil works by increasing blood flow to the genitals, which in men leads to an erection. First released in 1998, it was designed to improve men's sex lives. Unsurprisingly, this has piqued the curiosity of many women too: if it works so well for their male partners, couldn't it "work" for them too? It’s worth figuring out whether women can take male Sildenafil?

When did women decide to try the drug on themselves?

This issue was first raised in the United States, in the New York Times, in an article entitled “Women See Sildenafil Work Miracles for Them.” And this happened just a few months after the drug became available. This research was also included in an episode of the TV series Sex and the City, in which the heroine with a huge number of sexual relationships, Samantha, uses a remedy to get rid of her inhibitions as much as possible.

Natural pathogen

Sildenafil is an artificial substance created in a laboratory. To obtain it, a special technology was used that cannot be repeated at home.

Many people still prefer natural ones to any chemical substances and try to use in their diet products that are natural pathogens (aphrodisiacs). Aphrodisiacs are products that affect the body in such a way that, with their constant use, a person’s libido increases, sexual function and sensitivity improve.

Natural pathogens are chocolate, honey, olive oil, coffee, mushrooms, bananas, strawberries, seaweed, dates, coconuts, pine nuts, horseradish, onions, garlic, carrots, herbs (dill, parsley, celery), asparagus, eggs, caviar , seafood (shrimp, mussels, oysters, snails), seasonings (saffron, vanilla, anise, ginger, cinnamon, ginseng), aloe, avocado, artichoke.

Mental vs. Physical Arousal

So why is Sildenafil not available to women and what happens to those who take it anyway (contrary to generally accepted medical recommendations)? Gynecologists say that the drug cannot be used as a simple libido enhancer.

The real reason men take the drug is because they want to have sex and are unable to get or maintain an erection. It can be seen how the drugs can cause a huge increase in blood supply and therefore inflation of the blood vessels that cause an erection. However, this has nothing to do with desire.

But few women are concerned about something like this. While women experience increased penile blood flow during sex, it does not follow that female arousal problems are related to these problems.

In fact, low libido in women is a complex problem with a wide range of possible causes. These can range from relationship issues to hormonal conditions and must be addressed on a case-by-case basis. Simply put, mental and physical arousal are two different things.

Both men and women can be aroused without any mental interest. This is a separate mechanism that allows the release of a certain secretion in women or blood flow to the penis in men.

Safety and effectiveness

Therefore, this means that a woman can take Sildenafil without seeing any real impact on her sexual functioning (depending on how it is defined). All this said, there have been some studies in which women using this drug reported increased sexual pleasure.

The most famous of these, conducted by the UCLA Center for Women's Sexual Medicine in 2003, followed 202 postmenopausal women with female sexual arousal disorder. It is important to note that none of these women reported emotional difficulties or problems in their relationships.

During the 12-week trial, participants took either sildenafil or a placebo before becoming sexually active. Overall, the first group experienced greater sexual pleasure, and most side effects were minor.

However, subsequent studies have failed to reproduce these results, and no large clinical trials have been conducted in this area. The evidence base is too limited to draw any real conclusions.

Based on this, it is impossible to say unequivocally how safe the drug is for women. Although it was well tolerated in studies, there is not much information about its long-term effects. What is known for sure is that it should not be combined with certain other drugs.

It is generally a very safe drug, but if you dilate your blood vessels, it means your blood pressure drops. If you are taking certain other medications that may cause your blood pressure to drop further, this may be dangerous because you may lose consciousness or reduce blood flow to your heart or brain.

Sildenafil can be especially dangerous when combined with amyl nitrate, another drug often used for recreational purposes and to enhance sexual sensations. In rare cases, combining these two drugs has proven fatal.

Sildenafil-SZ

Registration number

LP-002313

Dosage form

Film-coated tablets

Compound

1 film-coated tablet contains:

Dosage 25 mg:

active substance: sildenafil citrate in terms of sildenafil – 25 mg; excipients (core): microcrystalline cellulose – 50.0 mg; lactose monohydrate (milk sugar) – 61.5 mg; croscarmellose sodium (primellose) – 7.5 mg; povidone (medium molecular weight polyvinylpyrrolidone) – 4.5 mg; magnesium stearate – 1.5 mg; excipients (shell): Opadry II (polyvinyl alcohol, partially hydrolyzed - 2.0 mg; titanium dioxide E 171 - 1.145 mg; macrogol (polyethylene glycol 3350) - 1.01 mg; talc - 0.74 mg; aluminum varnish based brilliant blue – 0.096 mg; iron oxide (II) yellow E 172 – 0.0085 mg; iron oxide (II) black E 172 – 0.0005 mg).

Dosage 50 mg:

active substance: sildenafil citrate in terms of sildenafil – 50 mg; excipients (core): microcrystalline cellulose – 54.0 mg; lactose monohydrate (milk sugar) – 74.0 mg; croscarmellose sodium (primellose) – 10.0 mg; povidone (medium molecular weight polyvinylpyrrolidone) – 10.0 mg; magnesium stearate – 2.0 mg; excipients (shell): Opadry II (polyvinyl alcohol, partially hydrolyzed - 2.4 mg; titanium dioxide E 171 - 1.374 mg; macrogol (polyethylene glycol 3350) - 1.212 mg; talc - 0.888 mg; aluminum varnish based on brilliant blue - 0 ,1152 mg; iron oxide (II) yellow E 172 – 0.0102 mg; iron oxide (II) black E 172 – 0.0006 mg).

Dosage 100 mg:

active substance: sildenafil citrate in terms of sildenafil – 100 mg excipients (core): microcrystalline cellulose – 83.5 mg; lactose monohydrate (milk sugar) – 83.5 mg; croscarmellose sodium (primellose) – 15.0 mg; povidone (medium molecular weight polyvinylpyrrolidone) – 15.0 mg; magnesium stearate – 3.0 mg; excipients (shell): Opadry II (polyvinyl alcohol, partially hydrolyzed - 3.6 mg; titanium dioxide E 171 - 2.061 mg; macrogol (polyethylene glycol 3350) - 1.818 mg; talc - 1.332 mg; aluminum varnish based on brilliant blue – 0.1728 mg; iron oxide (II) yellow E 172 – 0.0153 mg; iron oxide (II) black E 172 – 0.0009 mg).

Description

Blue film-coated tablets, round, biconvex. The tablets are white or almost white when broken.

ATX code

[G04BE03]

Pharmacological properties

Pharmacodynamics

Sildenafil is a powerful selective inhibitor of cycloguanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5).
Mechanism of action
The physiological mechanism of erection is associated with the release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation.
This, in turn, leads to an increase in cGMP levels, subsequent relaxation of the smooth muscle tissue of the corpus cavernosum and increased blood flow. Sildenafil does not have a direct relaxant effect on the isolated human corpus cavernosum, but enhances the effect of nitric oxide (NO) by inhibiting PDE5, which is responsible for the breakdown of cGMP. Sildenafil is selective against PDE5 in vitro
, its activity against PDE5 exceeds that against other known phosphodiesterase isoenzymes: PDE6 – 10 times; PDE1 – more than 80 times; PDE2, PDE4, PDE7-PDE11 – more than 700 times. Sildenafil is 4000 times more selective for PDE5 compared to PDE3, which is of utmost importance since PDE3 is one of the key enzymes in the regulation of myocardial contractility.

A prerequisite for the effectiveness of sildenafil is sexual
stimulation. Clinical data Cardiac studies
The use of sildenafil in doses up to 100 mg did not lead to clinically significant ECG changes in healthy volunteers.
The maximum decrease in systolic pressure in the supine position after taking sildenafil at a dose of 100 mg was 8.3 mmHg. Art., and diastolic pressure – 5.3 mm Hg. Art. A more pronounced, but also transient effect on blood pressure (BP) was observed in patients taking nitrates (see sections “Contraindications” and “Interaction with other drugs”). In a study of the hemodynamic effect of sildenafil at a single dose of 100 mg in 14 patients with severe coronary artery disease (CAD) (more than 70% of patients had stenosis of at least one coronary artery), resting systolic and diastolic blood pressure decreased by 7 % and 6%, respectively, and pulmonary systolic pressure decreased by 9%. Sildenafil did not affect cardiac output or impair blood flow in stenotic coronary arteries, and also resulted in an increase (by approximately 13%) in adenosine-induced coronary flow in both stenotic and intact coronary arteries. In a double-blind, placebo-controlled study, 144 patients with erectile dysfunction and stable angina taking antianginal drugs (except nitrates) exercised until their angina symptoms improved. The duration of the exercise was significantly longer (19.9 seconds; 0.9 - 38.9 seconds) in patients taking sildenafil in a single dose of 100 mg compared to patients receiving placebo. A randomized, double-blind, placebo-controlled study examined the effect of varying the dose of sildenafil (up to 100 mg) in men (n = 568) with erectile dysfunction and hypertension taking more than two antihypertensive medications. Sildenafil improved erections in 71% of men compared to 18% in the placebo group. The incidence of adverse effects was comparable to that in other patient groups, as well as in individuals taking more than three antihypertensive drugs. Studies of visual impairment
In some patients, 1 hour after taking sildenafil at a dose of 100 mg, the Farnsworth-Munsell 100 test revealed a mild and transient impairment in the ability to distinguish shades of color (blue/green).
2 hours after taking the drug, these changes were absent. Color vision impairment is thought to be caused by inhibition of PDE6, which is involved in light transmission in the retina. Sildenafil had no effect on visual acuity, contrast perception, electroretinogram, intraocular pressure, or pupil diameter. In a placebo-controlled crossover study of patients with proven early-onset macular degeneration (n = 9), sildenafil in a single dose of 100 mg was well tolerated. There were no clinically significant changes in vision assessed by specific visual tests (visual acuity, Amsler grating, color perception, color transmission simulation, Humphrey perimeter, and photostress). Efficacy
The effectiveness and safety of sildenafil were assessed in 21 randomized, double-blind, placebo-controlled studies lasting up to 6 months in 3,000 patients aged 19 to 87, with erectile dysfunction of various etiologies (organic, psychogenic or mixed). The effectiveness of the drug was assessed globally using an erection diary, the International Index of Erectile Function (a validated questionnaire about the state of sexual function) and a partner interview. The effectiveness of sildenafil, defined as the ability to achieve and maintain an erection sufficient for satisfactory sexual intercourse, has been demonstrated in all studies conducted and was confirmed in long-term studies lasting 1 year. In fixed-dose studies, the proportion of patients who reported that therapy improved their erections was: 62% (sildenafil 25 mg dose), 74% (sildenafil 50 mg dose), and 82% (sildenafil 100 mg dose) compared with 25%. in the placebo group. Analysis of the International Index of Erectile Function showed that in addition to improving erection, treatment with sildenafil also increased the quality of orgasm, achieved satisfaction from sexual intercourse and overall satisfaction. According to the pooled data, among patients who reported improved erections with sildenafil treatment, 59% of patients with diabetes, 43% of patients who had undergone radical prostatectomy and 83% of patients with spinal cord injury (versus 16%, 15% and 12% in the placebo group, respectively) ).

Pharmacokinetics

The pharmacokinetics of sildenafil in the recommended dose range is linear.
Absorption
After oral administration, sildenafil is rapidly absorbed.
Absolute bioavailability averages about 40% (from 25% to 63%). In vitro,
sildenafil at a concentration of about 1.7 ng/ml (3.5 nM) inhibits human PDE5 activity by 50%.
After a single dose of sildenafil 100 mg, the average maximum concentration of free sildenafil in blood plasma (Cmax) in men is about 18 ng/ml (38 nM). Cmax when taking sildenafil orally on an empty stomach is achieved on average within 60 minutes (from 30 minutes to 120 minutes). When taken in combination with fatty foods, the rate of absorption decreases: Cmax decreases by an average of 29%, and the time to reach maximum concentration (Tmax) increases by 60 minutes, but the degree of absorption does not significantly change (the area under the concentration-time pharmacokinetic curve (AUC) decreases by 11%). Distribution
The volume of distribution of sildenafil at steady state averages 105 liters.
The binding of sildenafil and its main circulating N-demethyl metabolite to plasma proteins is about 96% and does not depend on the total concentration of the drug. Less than 0.0002% of the sildenafil dose (average 188 ng) was found in semen 90 minutes after dosing. Metabolism
Sildenafil is metabolized mainly in the liver under the influence of the cytochrome CYP3A4 isoenzyme (major pathway) and the cytochrome CYP2C9 isoenzyme (minor pathway).
The main circulating active metabolite, formed as a result of N-demethylation of sildenafil, undergoes further metabolism. The selectivity of this metabolite for PDE is comparable to that of sildenafil, and its activity against PDE5 in vitro is about 50% of the activity of sildenafil. The concentration of the metabolite in the blood plasma of healthy volunteers was about 40% of the concentration of sildenafil. The N-demethyl metabolite undergoes further metabolism; its half-life (T1/2) is about 4 hours. Elimination
The total clearance of sildenafil is 41 l/hour, and the final T1/2 is 3-5 hours.
After oral administration, as after intravenous administration, sildenafil is excreted in the form of metabolites, mainly by the intestines (about 80% of the oral dose) and, to a lesser extent, by the kidneys (about 13% of the oral dose). Pharmacokinetics in special groups of patients Elderly patients
In healthy elderly patients (over 65 years of age), the clearance of sildenafil is reduced, and the concentration of free sildenafil in the blood plasma is approximately 40% higher than in young patients (18-45 years of age).
Age does not have a clinically significant effect on the incidence of side effects. Impaired renal function
With mild (creatinine clearance (CL) 50-80 ml/min) and moderate (CL 30-49 ml/min) degrees of renal failure, the pharmacokinetics of sildenafil after a single oral dose of 50 mg does not change.
In severe renal failure (creatinine clearance ≤ 30 ml/min), the clearance of sildenafil is reduced, which leads to an approximately twofold increase in AUC (100%) and Cmax (88%) compared to those with normal renal function in patients of the same age group. Liver dysfunction
In patients with liver cirrhosis (stages A and B according to the Child-Pugh classification), the clearance of sildenafil is reduced, which leads to an increase in AUC (84%) and Cmax (47%) compared to those with normal liver function in patients the same age group. The pharmacokinetics of sildenafil in patients with severe liver dysfunction (Child-Pugh stage C) has not been studied.

Indications for use

Treatment of erectile dysfunction, characterized by the inability to achieve or maintain a penile erection sufficient for satisfactory sexual intercourse. Sildenafil is only effective during sexual stimulation.

Contraindications

Hypersensitivity to sildenafil or to any other component of the drug Use in patients receiving continuous or intermittent nitric oxide donors, organic nitrates or nitrites in any form, since sildenafil enhances the hypotensive effect of nitrates (see section “Interaction with other drugs”) Safety and the effectiveness of the drug Sildenafil when used together with other drugs for the treatment of erectile dysfunction have not been studied, therefore the use of such combinations is not recommended (see section “Special instructions”) According to the registered indication, the drug Sildenafil is not intended for use in children under 18 years of age. According to the registered indication, the drug Sildenafil not intended for use in women Lactase deficiency, lactose intolerance, glucose-galactose malabsorption. Concomitant use of sildenafil with ritonavir is not recommended.\ With caution

Anatomical deformation of the penis (angulation, cavernous fibrosis or Peyronie's disease) (see section "Special instructions").
Diseases predisposing to the development of priapism (sickle cell anemia, multiple myeloma, leukemia, thrombocythemia) (see section “Special instructions”). Diseases accompanied by bleeding. Exacerbation of peptic ulcer of the stomach and duodenum. Hereditary retinitis pigmentosa (see section “Special instructions”). Heart failure, unstable angina, myocardial infarction, stroke or life-threatening arrhythmias in the last 6 months, arterial hypertension (BP > 170/100 mm Hg) or hypotension (BP < 90/50 mm Hg) (see. section "Special instructions"). In patients with episodes of anterior non-arteritic ischemic optic neuropathy (history). Use during pregnancy and breastfeeding
According to the registered indication, the drug is not intended for use in women.

Directions for use and doses

Inside. The recommended dose for most adult patients is 50 mg approximately 1 hour before sexual activity. Taking into account effectiveness and tolerability, the dose can be increased to 100 mg or reduced to 25 mg. The maximum recommended dose is 100 mg. The maximum recommended frequency of use is once a day. Renal dysfunction

For mild to moderate renal failure (creatinine clearance 30-80 ml/min), no dose adjustment is required; for severe renal failure (creatinine clearance <30 ml/min), the dose of sildenafil should be reduced to 25 mg.
Liver dysfunction
Since the elimination of sildenafil is impaired in patients with liver damage (particularly cirrhosis), the dose of Sildenafil should be reduced to 25 mg.
Combined use with other drugs
When used together with ritonavir, the maximum single dose of Sildenafil should not exceed 25 mg, and the frequency of use should be 1 time per 48 hours (see section “Interaction with other drugs”).
When used together with inhibitors of the cytochrome CYP3A4 isoenzyme (erythromycin, saquinavir, ketoconazole, itraconazole), the initial dose of Sildenafil should be 25 mg (see section “Interaction with other drugs”). To minimize the risk of postural hypotension in patients taking α-blockers, Sildenafil should be started only after hemodynamic stabilization has been achieved in these patients. You should also consider the advisability of reducing the initial dose of sildenafil (see sections “Special instructions” and “Interaction with other drugs”). Elderly patients
No dose adjustment of Sildenafil is required.

Side effect

Typically, the side effects of Sildenafil are mild or moderate and transient. Fixed-dose studies have shown that the incidence of some adverse events increases with increasing dose.

When using the drug Sildenafil in doses exceeding the recommended ones, adverse events were similar to those noted above, but usually occurred more often. General condition disorders:

facial swelling, photosensitivity reactions, shock, asthenia, pain, chills, abdominal pain, chest pain.
Allergic reactions:
hypersensitivity reactions (including skin rash), Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).
Disorders of the central and peripheral nervous system:
drowsiness, insomnia, hypoesthesia, paresthesia, ataxia, neuralgia, neuropathy, tremor, depression, unusual dreams, decreased reflexes, stroke, transient ischemic attack, convulsions, incl.
recurrent. Cardiovascular system disorders:
tachycardia, increased or decreased blood pressure, myocardial infarction, atrial fibrillation, ventricular arrhythmia, unstable angina, AV block, cerebral thrombosis, heart failure, ECG abnormalities, cardiomyopathy, sudden death, syncope.
Respiratory disorders:
nosebleeds, asthma, shortness of breath, laryngitis, pharyngitis, sinusitis, bronchitis, increased sputum production, increased cough.
Gastrointestinal disorders: vomiting, nausea, dry oral mucosa, glossitis, colitis, dysphagia, gastritis, gastroenteritis, esophagitis, stomatitis, rectal bleeding, gingivitis. Visual disorders:
eye pain, eye redness/scleral injections, conjunctival damage, lacrimation disorders, anterior ischemic optic neuropathy, retinal vascular occlusion, visual field defects, mydriasis, cataracts, eye pain.
Hearing disorders:
vertigo, tinnitus, ear pain, deafness.
Blood and lymphatic system disorders:
anemia, leukopenia.
Metabolic and nutritional disorders:
thirst, gout, unstable diabetes, hyperglycemia, peripheral edema, hyperuricemia, hypoglycemic reaction, hypernatremia.
Musculoskeletal disorders:
arthritis, arthrosis, myalgia, tendon rupture, tendovaginitis, bone pain, myasthenia gravis, synovitis.
Skin and subcutaneous tissue disorders:
urticaria, herpes simplex, itching, sweating, skin ulcers, contact dermatitis, exfoliative dermatitis.
Disorders of the genitourinary system:
cystitis, nocturia, frequent urination, gynecomastia, urinary incontinence, ejaculation disorders, genital swelling, anorgasmia.
Reproductive system disorders:
prolonged erection and/or priapism.

Overdose

With a single dose of Sildenafil in doses up to 800 mg, adverse events were comparable to those when taking the drug in lower doses, but were more common. Treatment is symptomatic. Hemodialysis does not accelerate the clearance of sildenafil, since the latter actively binds to plasma proteins and is not excreted by the kidneys.

Interaction with other drugs

The influence of other drugs on the pharmacokinetics of sildenafil

The metabolism of sildenafil occurs mainly under the influence of the cytochrome CYP3A4 (main pathway) and CYP2C9 isoenzymes, therefore inhibitors of these isoenzymes can reduce the clearance of sildenafil, and inducers, accordingly, increase the clearance of sildenafil.
A decrease in the clearance of sildenafil was noted with simultaneous use of inhibitors of the cytochrome CYP3A4 isoenzyme (ketoconazole, erythromycin, cimetidine). Cimetidine (800 mg), a nonspecific inhibitor of the cytochrome CYP3A4 isoenzyme, when taken together with sildenafil (50 mg), causes an increase in plasma sildenafil concentrations by 56%. A single dose of 100 mg of sildenafil together with erythromycin (500 mg/day 2 times a day for 5 days), a specific inhibitor of the cytochrome CYP3A4 isoenzyme, against the background of achieving a constant concentration of erythromycin in the blood, leads to an increase in the AUC of sildenafil by 182%. When taking sildenafil (single 100 mg) and saquinavir (1200 mg/day 3 times a day), an inhibitor of HIV protease and cytochrome CYP3A4 isoenzyme, while achieving a constant concentration of saquinavir in the blood, the Cmax of sildenafil increased by 140%, and the AUC increased by 210%. Sildenafil has no effect on the pharmacokinetics of saquinavir. Stronger inhibitors of the cytochrome CYP3A4 isoenzyme, such as ketoconazole and itraconazole, may cause more severe changes in the pharmacokinetics of sildenafil. The simultaneous use of sildenafil (100 mg once) and ritonavir (500 mg 2 times a day), an HIV protease inhibitor and a strong inhibitor of cytochrome P450, while achieving a constant concentration of ritonavir in the blood leads to an increase in Cmax of sildenafil by 300% (4 times ), and AUC by 1000% (11 times). After 24 hours, the concentration of sildenafil in the blood plasma is about 200 ng/ml (after a single dose of sildenafil alone - 5 ng/ml), which is consistent with information about the pronounced effect of ritonavir on the pharmacokinetics of various cytochrome P450 substrates. Sildenafil has no effect on the pharmacokinetics of ritonavir. The combined use of sildenafil with ritonavir is not recommended. If sildenafil is taken in recommended doses by patients simultaneously receiving strong inhibitors of the cytochrome CYP3A4 isoenzyme, then the Cmax of free sildenafil does not exceed 200 nM, and the drug is well tolerated. A single dose of an antacid (magnesium hydroxide/aluminum hydroxide) does not affect the bioavailability of sildenafil. Inhibitors of the cytochrome CYP2C9 isoenzyme (tolbutamide, warfarin), the cytochrome CYP2D6 isoenzyme (selective serotonin reuptake inhibitors, tricyclic antidepressants), thiazide and thiazide-like diuretics, ACE inhibitors and calcium antagonists do not affect the pharmacokinetics of sildenafil. Azithromycin (500 mg/day for 3 days) has no effect on the AUC, Cmax, Tmax, elimination rate constant and T1/2 of sildenafil or its main circulating metabolite. Effect of sildenafil on other drugs
Sildenafil is a weak inhibitor of cytochrome P450 isoenzymes - 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 (IC50>150 µmol).
When sildenafil is taken at recommended doses, its Cmax is approximately 1 µmol, so it is unlikely that sildenafil could affect the clearance of substrates of these isoenzymes. Sildenafil enhances the hypotensive effect of nitrates both with long-term use of the latter and when they are prescribed for acute indications. In this regard, the use of sildenafil in combination with nitrates or nitric oxide donors is contraindicated. When taking the α-blocker doxazosin (4 mg and 8 mg) and sildenafil (25 mg, 50 mg and 100 mg) simultaneously in patients with benign prostatic hyperplasia with stable hemodynamics, the average additional reduction in systolic/diastolic blood pressure in the supine position was 7/ 7 mmHg art., 9/5 mm Hg. and 8/4 mm Hg, respectively, and in a standing position – 6/6 mm Hg, 11/4 mm Hg. and 4/5 mmHg, respectively. Rare cases of symptomatic postural hypotension, manifested in the form of dizziness (without fainting), have been reported in such patients. In selected sensitive patients receiving α-blockers, concomitant use of sildenafil may lead to symptomatic hypotension. signs of significant interaction with tolbutamide (250 mg) or warfarin (40 mg), which are metabolized by the cytochrome CYP2C9 isoenzyme.
Sildenafil (100 mg) does not affect the pharmacokinetics of HIV protease inhibitors, saquinavir and ritonavir, which are substrates of the cytochrome CYP3A4 isoenzyme, at their constant blood levels. Sildenafil (50 mg) does not cause an additional increase in bleeding time when taking acetylsalicylic acid (150 mg). Sildenafil (50 mg) does not enhance the hypotensive effect of alcohol in healthy volunteers with a maximum blood alcohol concentration of 0.08% (80 mg/dL) on average. In patients with arterial hypertension, no signs of interaction between sildenafil (100 mg) and amlodipine were detected. The average additional reduction in blood pressure in the supine position is 8 mm Hg. (systolic) and 7 mm Hg. (diastolic). The use of sildenafil in combination with antihypertensive drugs does not lead to additional side effects.

special instructions

To diagnose erectile dysfunction, determine its possible causes and select adequate treatment, it is necessary to obtain a complete medical history and conduct a thorough physical examination. Erectile dysfunction treatments should be used with caution in patients with anatomical deformation of the penis (angulation, cavernous fibrosis, Peyronie's disease), or in patients with risk factors for priapism (sickle cell anemia, multiple myeloma, leukemia) (see section C caution"). Medicines intended to treat 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, so before starting any therapy for erectile dysfunction, the doctor should refer the patient for an examination of the condition of the cardiovascular system. Sexual activity is not advisable in patients with heart failure, unstable angina, myocardial infarction or stroke in the last 6 months, life-threatening arrhythmias, arterial hypertension (BP > 170/100 mm Hg) or hypotension (BP < 90/50 mm Hg. Art.) (see section “With caution”). Clinical studies have shown no difference in the incidence of myocardial infarction (1.1 per 100 people per year) or the incidence of cardiovascular death (0.3 per 100 people per year) in patients treated with Sildenafil compared with patients who received placebo. Cardiovascular complications

During post-marketing use of sildenafil for the treatment of erectile dysfunction, adverse events such as serious cardiovascular events (including myocardial infarction, unstable angina, sudden cardiac death, ventricular arrhythmia, hemorrhagic stroke, transient ischemic attack, hypertension and hypotension) have been reported. ), which had a temporary association with the use of sildenafil.
Most of these patients, but not all of them, had risk factors for cardiovascular complications. Many of these adverse events occurred shortly after sexual activity, and some of them occurred after taking sildenafil without subsequent sexual activity. It is not possible to establish a direct connection between the observed adverse events and these or other factors. Hypotension
Sildenafil has a systemic vasodilating effect, leading to a transient decrease in blood pressure, which is not a clinically significant phenomenon and does not lead to any consequences in most patients.
However, before prescribing Sildenafil, the physician should carefully assess the risk of possible undesirable manifestations of the vasodilating effect in patients with relevant diseases, especially against the background of sexual activity. Increased susceptibility to vasodilators is observed in patients with obstruction of the left ventricular outflow tract (aortic stenosis, hypertrophic obstructive cardiomyopathy), as well as with the rare syndrome of multiple system atrophy, manifested by severe dysregulation of blood pressure from the autonomic nervous system. Since the combined use of sildenafil and α-blockers can lead to symptomatic hypotension in some sensitive patients, Sildenafil should be administered with caution to patients taking α-blockers (see section "Interaction with other drugs"). To minimize the risk of developing postural hypotension in patients taking α-blockers, Sildenafil should be started only after hemodynamic stability has been achieved in these patients. You should also consider the advisability of reducing the initial dose of Sildenafil (see section “Dosage and Administration”). The physician should inform patients about what actions to take if symptoms of postural hypotension occur. Visual disturbances
Rare cases of anterior non-arteritic ischemic optic neuropathy as a cause of deterioration or loss of vision have been reported with the use of all PDE5 inhibitors, including sildenafil.
Most of these patients had risk factors such as optic disc excavation, age over 50 years, diabetes mellitus, hypertension, coronary artery disease, hyperlipidemia, and smoking. A cause-and-effect relationship between the use of PDE5 inhibitors and the development of anterior non-arteritic ischemic optic neuropathy has not been identified. The physician should inform the patient about the increased risk of developing anterior non-arteritic ischemic optic neuropathy if this condition has already been noted. In case of sudden loss of vision, patients should receive the necessary medical attention immediately. A small number of patients with hereditary retinitis pigmentosa have genetically determined dysfunction of retinal phosphodiesterases. There is no information on the safety of using Sildenafil in patients with retinitis pigmentosa, so sildenafil should be used with caution (see section "With caution"). Hearing Impairment
Some post-marketing and clinical studies have reported cases of sudden deterioration or loss of hearing associated with the use of all PDE5 inhibitors, including sildenafil.
Most of these patients had risk factors for sudden deterioration or loss of hearing. A cause-and-effect relationship between the use of PDE5 inhibitors and sudden hearing loss or deterioration has not been established. If there is a sudden deterioration in hearing or hearing loss while taking sildenafil, you should consult your doctor immediately. Bleeding
Sildenafil enhances the antiplatelet effect of sodium nitroprusside, a nitric oxide donor, on human platelets in vitro.
There are no data on the safety of sildenafil in patients with a tendency to bleeding or exacerbation of gastric and duodenal ulcers, therefore Sildenafil should be used with caution in these patients (see section "With caution"). The incidence of epistaxis in patients with PH associated with diffuse connective tissue diseases was higher (sildenafil 12.9%, placebo 0%) than in patients with primary pulmonary hypertension (sildenafil 3.0%, placebo 2.4%). Patients receiving sildenafil in combination with a vitamin K antagonist had a higher incidence of epistaxis (8.8%) than patients not receiving a vitamin K antagonist (1.7%). Use in conjunction with other means of treating erectile dysfunction.
The safety and effectiveness of Sildenafil in combination with other drugs for the treatment of erectile dysfunction have not been studied, therefore the use of such combinations is not recommended (see section “Contraindications”).

Impact on the ability to drive vehicles and operate machinery

While taking sildenafil, no negative effects on the ability to drive a car or use other technical equipment were observed. However, since taking sildenafil may reduce blood pressure, develop chromatopsia, blurred vision, etc. 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 dosage regimen.

Release form

Film-coated tablets, 25 mg, 50 mg and 100 mg 1, 2, 4 or 10 tablets per blister pack. 20 tablets in polymer jars or polymer bottles. Each jar, bottle, 1 blister pack of 1, 2, 4 or 10 tablets along with instructions for use are placed in a cardboard box.

Best before date

3 years. Do not use after the expiration date stated on the packaging.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Vacation conditions

On prescription.

Prescription drug

Prescription drug

Quest for women

So, for women who have problems with arousal, are there other drugs that can help where Sildenafil cannot? The answer to this question will depend on the nature of the problem.

There are many gynecological conditions to consider, so it is important to seek advice from a specialist. Most postmenopausal women almost certainly need to use estrogen in the vagina, as well as a good lubricant if they experience vaginal dryness or painful sex.

Research suggests that topical estrogen is generally fairly safe, at least in the short term, but some doctors may be cautious about prescribing such a medication if a woman has a history of estrogen-positive breast cancer. In these cases, there are many hormone-free vaginal moisturizers and lubricants available that can help.

Some postmenopausal women may receive small amounts of testosterone in addition to hormone replacement therapy (HRT). Although it is not generally recommended due to limited evidence of its effectiveness and concerns about side effects, some doctors will prescribe it "off-license".

Another interesting candidate is Addyi (flibanserin). It is supposed to be for women with hypoactive sexual desire disorder and targets certain chemicals in the brain (serotonin, dopamine and norepinephrine) to increase sexual motivation.

These stimulant pills were popularly known as "Female Viagra" when they hit the market in 2015. However, it was something of a commercial failure, with critics citing the drug's frequent side effects and unconvincing effect.

Features of the drug use

The positive effect of Sildenafil on women is possible only during sexual intimacy, when active stimulation occurs. If taking the drug is accompanied by deterioration in hearing or vision (fogging, color vision disturbances), then it is best to abandon it and find a more suitable drug from your doctor.

Also, Sildenafil tablets are not recommended to be combined with other drugs of the same spectrum of action. There are no special recommendations for the use of the medicine while driving a vehicle. A physician will be needed if the patient has active hypotension.

Sildenafil has a whole list of side effects that will increase if the dosage is exceeded for some reason.

Impact on the female body

It is important to know how Sildenafil affects women, because this drug is intended to increase male potency.

Due to chemical reactions that affect the pelvic organs, the vessels dilate and the blood flow increases. And all thanks to the drug “Sildenafil”. Feedback from women about him is only positive. Representatives of the gentle sex note the following effects after taking this stimulant:

1. Increased sensitivity during sexual intercourse.
2. Sensitivity to touch increases.
3. The production of lubricant is stimulated.
4. Pain during sex is eliminated.
5. Sexual desire increases.
6. The time of orgasm accelerates.
7. Sexual intercourse is prolonged.

It is also very important that Sildenafil allows women during menopause and after surgery on the female organs to feel a man, have a sufficient amount of natural lubrication and increases excitability.

In addition, this drug acts as an antidepressant, relieves fatigue, irritation and stress. It is because of this that a woman can completely relax and surrender to a man.

What will happen if a woman takes Sildenafil, intended for men? Experts advise using exactly the type of drug that is made specifically for the female body. Only in this case will it be possible to achieve the desired effect. This should be done an hour before intimacy. The drug must dissolve inside and completely spread throughout the body.

Composition of the drug

Sildenafil for women is an aphrodisiac. The drug is available in tablet form for oral use. The pills are coated with a special coating to protect the stomach. Pharmacies offer the following types of dosages: twenty-five, fifty and one hundred milligrams.

The main active ingredient is sildenafil citrate. Excipients include lactose monohydrate, microcrystalline cellulose, magnesium stearate, indigo carmine, titanium dioxide, polyvinylpyrrolidone.

How to use

This drug has not been used by the fairer sex for very long, and the instructions must be carefully followed. According to it, the drug is taken at a dose of 50 mg per day. This dosage is quite enough to improve sex life, in particular increase arousal. As already mentioned, the pill is taken an hour before sexual intercourse and washed down with plenty of water. And it is advisable to drink not after eating, but before eating. Otherwise, the exposure time of the drug increases.

For liver diseases, the dose of the drug per day is 25 mg.

For kidney disease, intake depends on the glomerular filtration rate. In this case, women take the drug “Sildenafil” in a dosage of no more than 25 mg.

Drug price

You can buy Sildenafil for women either at your nearest pharmacy or place an order online. In the latter case, the doctor's prescription will need to be shown to the courier at checkout. Below is the price of the drug in several pharmacies.

When is it prohibited to use the drug?

There are also prohibitions on taking the drug “Sildenafil” for women. The instructions indicate that it should not be taken together with alcoholic beverages. And this is proven by research.

Before use, consultation with a doctor is necessary. Self-appointment can lead to quite unpleasant consequences.

Here are the reasons why the drug is not allowed to be used:

1. Aortic stenosis.
2. Insufficient blood supply to the heart muscle.
3. Low pressure.
4. Heart failure.
5. Myocardial lesions.
6. Pathologies of the retina.
7. Age up to 18 years.
8. Failure of the body to accept any of the components.
9. History of stroke or heart attack.
10. Anemia.
11. Heart rhythm problems.

What analogues of the drug exist?

Generics of Sildenafil, that is, drugs created on its basis with the same chemical composition and therapeutic properties, can also be called its analogues. In the pharmacy chain you can find:

• Tornetis;
• Dynamic;
• Vizarsin;
• Taxier;
• Allmax strong;
• Caverject;
• Levitra;
• Cialis;
• Tentex forte;
• Rileys.

Dynamico

Taxier

Tentex Forte

Rileys

All of them have the same effect on the body, have a stimulating effect and improve the perception of sex.

Side effects

The main side effects after taking Sildenafil include:

• sleep problems - especially drowsiness and difficulty falling asleep;
• dry mouth;
• nausea;
• dizziness;
• low blood pressure, which may cause fainting;
• headache;
• vomiting;
• cough;
• fatigue;
• decreased heart rate.

Side effects occur only if a person does not accept any component of the drug.

How does the medication interact with other drugs?

The simultaneous use of Sildenafil with ketoconazole, erythromycin and cimetidine complicates the process of removing the drug from the body, its amount in the blood increases sharply. When taken together with sodium nitroprusside and other organic nitrates, a sharp decrease in blood pressure occurs, which is contraindicated in people with hypotension.

Sildenafil should not be used together with medications for patients with diabetes.

What to replace

But it is still better to replace the male drug “Sildenafil” with analogues. For women, the doctor may recommend the following remedies:

1. "Viagra FM".
2. "Cialis".
3. "Fliban 100 mg."
4. Femalegra 100 - female Viagra.
5. Femalefil 10 - female Cialis.
6. "Silver Fox"
7. "Spanish Fly" (GOLD FLY).

All these drugs have the same effect. But for some reason, most women prefer Sindenafil. After all, according to them, this drug produces the maximum effect.

What women say

They confirm the information specified in the instructions for the drug “Sildenafil” and reviews from women. The drug helps to resume the physiological processes of the intimate side of life without dependence and addiction. It activates the blood supply to the labia, increases the receptivity of the genitals, restores the process of secretion production, increases desire and satisfaction.

If you have problems getting pleasure from sex, taking stimulant pills for girls makes it possible to acquire maximum positive feelings. A stronger result is observed in patients who previously felt discomfort during sexual intercourse.

In addition, the drug increases the girl’s pleasure, the activity of the vaginal muscles, simplifies orgasm and improves its quality. The active element sildenafil stimulates intensive blood supply to the pelvic organs, clitoris and labia, and activates complete hydration of the internal genitalia.

Sildenafil provides girls with the opportunity to receive maximum pleasure during menopause, but also prevents soreness and vaginal dryness during intimacy.

Generics

As mentioned above, Sildenafil is used to eliminate poor blood circulation in the pelvic organs, to enhance sexual lust and receptivity of erogenous zones.

A familiar drug based on sildenafil is called Viagra. In fact, this is the “pioneer” of all medications to improve the quality of sex. Viagra is still actively sold in the pharmacy chain. At the same time, it is very expensive. Its price is two to four times higher than that of its synonyms.

To be more precise, subsequent drugs created on the basis of sildenafil are generics of Viagra. How do generics differ from a unique drug?

The technology for developing the original product is as follows:

1. Isolation of a chemical substance and analysis of its properties;
2. Conducting laboratory tests to identify the greatest number of beneficial and negative properties and determining the daily dosage;
3. Development of a method and technology for removing the main active substance on a production scale;
4. Purification of the active substance from unnecessary impurities, since their presence can provoke allergies and other third-party effects;
5. Development of a unique name for the drug and its mass release on the pharmaceutical market.

Each genuine drug has a mandatory patent, the period of which is limited. Basically, the certificate is issued for a period of five to ten years. When the patent expires, another pharmaceutical company has the right to use the original composition, but produce it as its own product.