Package Effex Sildenafil pills 100mg, 1pc

Certificate of conformity (COC) Effex Sildenafil pills 100mg, 1pc

Effex Sildenafil pills 100mg, 1pc

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Active ingredient:	Sildenafil
Dosage form:	Pills

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Categories: Genitourinary system, Medication, Tonicity of the urogenital system

Description
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Composition

Sildenafil citrate,

Auxiliary substances:

Microcrystalline cellulose,

Calcium hydrophosphate,

Pre-gelatinized corn starch,

Magnesium stearate,

Croscarmellose sodium,

Colloidal silicon dioxide

Shell composition:

Hypromellose (hydroxypropylmethylcellulose), Macrogol 4000 (polyethylene glycol 4000), Titanium Dioxide, Polysorbate-80, Talc, Iron Oxide dye red, Iron Oxide Dye Yellow

Pharmacological action

Medication for the treatment of erectile dysfunction. It starts working in 30-120 minutes.

Indications

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

Contraindications

Hypersensitivity to sildenafil or any other component of the drug.

Use in patients receiving continuous or intermittent nitric oxide donors, organic nitrates or nitrites in any form, as EFFEX® Sildenafil enhances the hypotensive effect of nitrates.

The safety and efficacy of EFFEX ® Sildenafil in combination with other treatments for erectile dysfunction have not been studied, so the use of such combinations is not recommended. Co-use with ritonavir.

Liver function disorders.

Severe chronic renal failure. Severe heart failure, unstable angina, stroke or myocardial infarction in the last 6 months, life-threatening arrhythmias, hypertension (BP > 170/100 mm Hg) or hypotension (BP > According to the registered indication, EFFEX® Sildenafil is not intended for use in children under 18 years of age. According to the registered indication, EFFEX® Sildenafil is not intended for use in women.

With caution

Anatomical deformity 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). Diseases accompanied by bleeding. Exacerbation of gastric ulcer and duodenal ulcer. Hereditary retinitis pigmentosa.

Side effects

The most common side effects were headache and hot flashes. Usually, the side effects of EFFEX® Sildenafil are mild to moderate and transient. Fixed-dose studies have shown that the frequency of some adverse events increases with increasing dose.

Classification of the frequency of side effects according to the recommendations of the World Health Organization: Very common (≥1/10), common (≥1/10 to <1/10), uncommon (≥1/1000 to <1/100), rare (≥1/10000 to <1/1000), very rare (

From the immune system: infrequently-hypersensitivity reactions (including skin rash), allergic reactions.

From the side of the visual organ: often – blurred vision, visual impairment, cyanopsia; infrequently – eye pain, photophobia, photopsia, chromatopsia, redness of the eyes/sclera injections, changes in the brightness of light perception, mydriasis, conjunctivitis, hemorrhage in the eye tissue, cataracts, disruption of the lacrimal apparatus; rarely – swelling of the eyelids and adjacent tissues, dryness in the eyes, the presence of iridescent circles in the field of vision around the light source, increased eye fatigue, vision of objects vision of objects in yellow (xanthopsia), vision of objects in red (erythropsia), conjunctival hyperemia, irritation of the eye mucosa, unpleasant sensations in the eyes; frequency unknown – non-arteriitic anterior ischemic neuropathy of the optic nerve (NPINZN), retinal vein occlusion, visual field defect, diplopia*, temporary loss of vision or decreased visual acuity, increased intraocular pressure, retinal edema, retinal vascular diseases, vitreous detachment/vitreal traction.

From the side of the organ of hearing: infrequently-sudden decrease or loss of hearing, tinnitus, pain in the ears, ringing in the ears.

From the cardiovascular system: often-hot flashes; infrequently-tachycardia, palpitation sensation, decreased blood pressure, increased blood pressure, increased heart rate, unstable angina, atrioventricular block, myocardial ischemia, cerebral thrombosis, cardiac arrest, heart failure, deviations in electrocardiogram readings, cardiomyopathy; rarely-atrial fibrillation.

From the blood and lymphatic system: infrequently-anemia, leukopenia.

From the side of metabolism and nutrition: infrequently-thirst, edema, gout, uncompensated diabetes mellitus, hyperglycemia, peripheral edema, hyperuricemia, hypoglycemia, hypernatremia.

From the respiratory system: often-nasal congestion; infrequently-nosebleeds, rhinitis, asthma, dyspnoea, laryngitis, pharyngitis, sinusitis, bronchitis, increased sputum volume, increased cough; rarely – a feeling of tightness in the throat, dryness of the nasal mucosa, swelling of the nasal mucosa.

From the gastrointestinal tract: often-nausea, dyspepsia; infrequently-gastroesophageal reflux disease, vomiting, abdominal pain, dry oral mucosa, glossitis, gingivitis, colitis, dysphagia, gastritis, gastroenteritis, esophagitis, stomatitis, deviation of “liver” functional tests from the norm, rectal bleeding; rarely – hypesthesia of the oral mucosa.

From the musculoskeletal system:

often-back pain; infrequently-myalgia, limb pain, arthritis, osteoarthritis, tendon rupture, tenosynovitis, bone pain, myasthenia gravis, synovitis.

From the genitourinary system: infrequently – cystitis, nocturia, breast enlargement, urinary incontinence, hematuria, ejaculation disorders, genital edema, anorgasmia, hematospermia, penile tissue damage; rarely-prolonged erection and / or priapism.

From the central and peripheral nervous system: very often – headache; often-dizziness; infrequently-drowsiness, migraine, ataxia, hypertonia, neuralgia, neuropathy, paresthesia, tremor, vertigo, symptoms of depression, insomnia, unusual dreams, increased reflexes, hypesthesia; rarely-convulsions*, repeated convulsions*, fainting, impaired cerebral circulation, transient ischemic attack.

From the skin and subcutaneous tissues: infrequently-skin rash, urticaria, herpes simplex, pruritus, increased sweating, skin ulceration, contact dermatitis, exfoliative dermatitis; frequency unknown-Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the reproductive system: rarely-bleeding from the penis.

Others: infrequently-a feeling of heat, swelling of the face, photosensitivity reaction, shock, asthenia, increased fatigue, pain of various localization, chills, accidental falls, chest pain, accidental injuries; rarely-irritability.

* Side effects identified during post-marketing studies.

Cardiovascular complications

Adverse events such as severe cardiovascular events (including myocardial infarction, unstable angina, sudden cardiac death, ventricular arrhythmia, hemorrhagic stroke, transient ischemic attack, hypertension, and hypotension) that were temporarily associated with the use of sildenafil have been reported during post-marketing use of sildenafil for the treatment of erectile dysfunction. Most of these patients, but not all of them, had risk factors for cardiovascular complications. Many of these adverse events were observed shortly after sexual activity, and some of them were observed after taking sildenafil without subsequent sexual activity. It is not possible to establish a direct link between the observed adverse events and these or other factors.

Visual impairments

In rare cases, post-marketing use of all PDE5 inhibitors, including sildenafil, reported non-arteriitic anterior ischemic optic neuropathy – NPINZN), a rare disease and cause of reduced or lost vision. Most of these patients had risk factors, such as a decrease in the ratio of excavation diameters to the optic disc (“congestive disc”), age over 50 years, diabetes mellitus, hypertension, coronary heart disease, hyperlipidemia, and smoking. An observational study evaluated whether the recent use of drugs of the PDE5 inhibitor class is associated with acute onset of NSAID. The results indicate an approximately 2-fold increase in the risk of NSAIDs within 5 half-lives after the use of a PDE5 inhibitor. According to published data for 5 days), a moderate inhibitor and literature-based data, the annual incidence of NSAID is 2.5-11.8 cases per 100,000 men aged ≥ 50 years in the general population. Patients with sudden vision loss should be advised to discontinue sildenafil therapy and consult their doctor immediately.Individuals who have already had a case of NSAIDs have an increased risk of recurrence of NSAIDs. Therefore, the doctor should discuss this risk with these patients, as well as discuss with them the potential for adverse effects of PDE5 inhibitors. PDE5 inhibitors, including sildenafil, should be used with caution in such patients and only in situations where the expected benefit outweighs the risk.

Interaction

Effect of other drugs on the pharmacokinetics of sildenafil

The metabolism of sildenafil occurs mainly under the action of cytochrome CYP3A4 (main pathway) and CYP2C9 isoenzymes, so inhibitors of these isoenzymes can reduce the clearance of sildenafil, and inducers, respectively, increase the clearance of sildenafil.

A decrease in the clearance of sildenafil was observed with the simultaneous use of inhibitors of the cytochrome CYP3A4 isoenzyme (ketoconazole, erythromycin, cimetidine).

Cimetidine (800 mg), a non-specific inhibitor of the cytochrome CYP3A4 isoenzyme, when co-administered with sildenafil (50 mg) causes an increase in the concentration of sildenafil in plasma by 56%.

A single dose of 100 mg of sildenafil together with erythromycin (500 mg / day 2 times a day) of cytochrome CYP3A4, while achieving a constant concentration of erythromycin in the blood, leads to an increase in the AUC of sildenafil by 182%.

When co-administered with sildenafil (a single 100 mg dose) and saquinavir (1200 mg / day 3 times a day), an inhibitor of HIV protease and cytochrome CYP3A4, while achieving a constant concentration of saquinavir in the blood, the Cmax of sildenafil increased by 140%, and the AUC increased by 210%. Sildenafil does not affect the pharmacokinetics of saquinavir.

Stronger inhibitors of the cytochrome CYP3A4 isoenzyme, such as ketoconazole and itraconazole, can also cause stronger changes in the pharmacokinetics of sildenafil.

Simultaneous use of sildenafil (100 mg once) and ritonavir (500 mg twice daily), an HIV protease inhibitor and a strong cytochrome P450 inhibitor, while achieving a constant concentration of ritonavir in the blood leads to an increase in sildenafil Cmax 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 application of sildenafil alone-5 ng/ml).

If sildenafil is used at the recommended doses in patients receiving simultaneously strong inhibitors of the cytochrome CYP3A4 isoenzyme, the Cmax of free sildenafil does not exceed 200 nM, and the drug is well tolerated.

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

In studies involving healthy volunteers, concomitant use of an endothelin receptor antagonist, bosentan (an inducer of the CYP3A4 isoenzyme (moderate), CYP2C9, and possibly CYP2C19) at steady-state concentrations (125 mg twice daily), and sildenafil at steady-state concentrations (80 mg three times daily) decreased the AUC and Cmax of sildenafil by 62.6% and 52.4%, respectively. Sildenafil increased the AUC and Cmax of bosentan by 49.8% and 42%, respectively. It is suggested that the concomitant use of sildenafil with potent inducers of the CYP3A4 isoenzyme, such as rifampicin, may lead to a large decrease in the concentration of sildenafil in blood plasma.

Inhibitors of the cytochrome CYP2C9 isoenzyme (tolbutamide, warfarin), 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 half-life of sildenafil or its main circulating metabolite. funds

Sildenafil is a weak inhibitor of cytochrome P450 isoenzymes-1A2,2C9,2C19,2D6,2E1 and 3A4 (IR 50 > 150 mmol). When taking sildenafil at the recommended doses, its Cmax is about

1 mmol, so it is unlikely that sildenafil can affect the clearance of substrates of these isoenzymes.

Sildenafil enhances the hypotensive effect of nitrates both with prolonged 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.

While taking α-adrenoblocker doxazosin (4 mg and 8 mg) and sildenafil (50 mg and 100 mg) in patients with benign prostate hyperplasia with stable hemodynamics, the average additional reduction in systolic/diastolic blood pressure in the supine position were 9/5 mmHg. art and 8/4 mm Hg. article, respectively, while in the standing position – 11/4 mmHg. art and

4/5 mm Hg. article, respectively. Rare cases of symptomatic postural hypotension, which manifested itself in the form of dizziness (without fainting), have been reported in such patients. In some sensitive patients receiving alpha-adrenergic blockers, concomitant use of sildenafil may lead to symptomatic hypotension.

There were no 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 constant blood levels.

Concomitant use of sildenafil at steady state (80 mg three times a day) leads to an increase in the AUC and Cmax of bosentan (125 mg twice a day) by 49.8% and 42%, respectively.

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, there were no signs of interaction between sildenafil (100 mg) and amlodipine. 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 agents does not lead to additional side effects.

How to take, course of use and dosage

Inside.

The recommended dose for most adult patients is 50 mg of sildenafil approximately 1 hour before sexual activity.

Depending on the effectiveness and tolerability, the dose can be increased to 100 mg. The maximum recommended dose is 100 mg. The maximum recommended frequency of application is 1 time per day.

Elderly patients

No dose adjustment of EFFEX Sildenafil is required.

Impaired renal function

No dose adjustment is required in patients with mild to moderate renal impairment (creatinine clearance 30-80 ml / min).

Concomitant use with other medications

To minimize the risk of postural hypotension in patients taking alpha-adreno blockers, sildenafil should be started only after hemodynamic stabilization has been achieved in these patients. Consideration should also be given to reducing the initial dose of sildenafil.

Overdose

When using EFFEX® Sildenafil in doses higher than recommended, adverse events were similar to those noted above, but usually occurred more frequently.

Treatment is symptomatic. Hemodialysis does not accelerate the elimination of the drug, since sildenafil is strongly bound to plasma proteins and is not excreted by the kidneys.

Special instructions

Effect of other drugs on the pharmacokinetics of sildenafil

A decrease in the clearance of sildenafil was observed with the simultaneous use of inhibitors of the cytochrome CYP3A4 isoenzyme (ketoconazole, erythromycin, cimetidine).

Cimetidine (800 mg), a non-specific inhibitor of the cytochrome CYP3A4 isoenzyme, when co-administered with sildenafil (50 mg) causes an increase in the concentration of sildenafil in plasma by 56%.

When co-administered with sildenafil (100 mg once) and saquinavir (1200 mg / day 3 times a day), an HIV protease inhibitor 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 does not affect the pharmacokinetics of saquinavir.