Vigrande

Vigrande is a medication used in cases of erectile dysfunction. It helps restore weakened erectile activity by potentiating blood flow to the penis.

The principle of therapeutic influence develops when nitrous oxide is released inside the corpora cavernosa (provided there is a sexual stimulus). Free nitrous oxide stimulates the activation of the enzyme guanylate cyclase, causing an increase in the volume of cGMP, during which the fibers of the smooth muscle elements of the cavernous bodies relax and the blood flow is potentiated. [1]

Indications Vigrande

It is used in the case of male erectile dysfunction (inability to maintain or achieve an erection of the penis required for successful sexual intercourse).

Release form

The drug is released in the form of tablets (25, 50 or 100 mg) - 1 or 4 pieces inside a separate package. The box contains 1 such plate.

Pharmacodynamics

Sildenafil is a component that selectively slows down the cGMP-specific component of PDE-5 (its activity causes the decay of cGMP in the region of the corpus cavernosum), which has a powerful therapeutic effect. The substance does not have a direct relaxing effect on the corpus cavernosum, but potentiates the relaxing effect that nitrous oxide has on this tissue. During sexual arousal, the local release of the element NO under the action of sildenafil causes a suppression of PDE-5 activity and an increase in cGMP values inside the corpus cavernosum, which leads to relaxation of smooth muscles and potentiation of blood circulation inside the corpus cavernosum. [2]

Sildenafil can cause temporary mild color discrimination (green-blue). It is assumed that this disorder develops in connection with the suppression of the action of PDE-6, which is involved in the processes of light transmission inside the retina. In vitro tests revealed that the effect of sildenafil on PDE-6 is ten times weaker than its effect on PDE-5.

In vitro tests also show that the effect of sildenafil in relation to PDE-5 is 10-10000 times stronger than in relation to other PDE isoforms (PDE-1, -2, -3, as well as -4 and -6). For example, the effect on PDE-5 is 4000 times stronger than the effect on PDE-3, a cAMP-specific component of PDE that participates in heart contractions.

Pharmacokinetics

After oral administration, sildenafil is absorbed at a high rate. The average level of absolute bioavailability is 40% (range 25-63%). With a single oral dose of 0.1 g, the Cmax is 18 ng / ml and, if consumed on an empty stomach, is reached in 0.5-2 hours. In the case of the introduction of sildenafil together with fatty products, the rate of absorption is reduced; Tmax indicators increase by 1 hour, and the Cmax level falls on average by 29%.

The equilibrium Vd values of sildenafil are 105 liters. The active element, together with the main circulating N-desmethyl metabolic component, is approximately 96% synthesized with intraplasmic proteins. Sildenafil total values do not affect protein binding.

Less than 0.0002% of the drug portion (average value - 188 ng) is recorded after 1.5 hours inside the semen.

Dosing and administration

Vigrande must be taken orally. For a drug to have its maximum effect, a sexual stimulus is required. Therefore, the tablet should be applied approximately 60 minutes before sexual intercourse.

Usually, 50 mg of the drug is used for a 1-time serving (it is recommended to use it on an empty stomach). In general, for 1 dose, it is allowed to take no more than 0.1 g of the medication.

• Application for children

The medication is not prescribed in pediatrics (until the age of 18).

Use Vigrande during pregnancy

Vigrande is not used to treat women.

Contraindications

The main contraindications:

• the presence of an allergy to sildenafil;
• hypersensitivity associated with auxiliary elements of drugs;
• combination with nitrous oxide donor substances (for example, amyl nitrite) or nitrates;
• conditions in which sexual intercourse is prohibited (angina pectoris, which has an unstable form, or severe HF);
• loss of vision, affecting one eye, due to the development of ischemic neuropathy (anterior non-arterial type) that affects the optic nerve;
• severe hepatic dysfunction;
• reduced blood pressure values (indicators less than 90/50 mm Hg);
• recent myocardial infarction or stroke;
• having a degenerative nature of the retinal changes (hereditary nature) (among them, for example, retinitis of the pigmentary type).

Side effects Vigrande

Among the side effects:

• neurological disorders: neuralgia, depression, headaches, tremor and hypesthesia, and in addition, flushing of the face, fainting, paresthesia, migraine, dizziness, deterioration of reflexes, ataxia and drowsiness or insomnia;
• problems of an ophthalmic nature: visual disturbances (blurred vision, photophobia and changes in color perception), mydriasis, pain in the eyeball area or hemorrhage in them, conjunctivitis, xerophthalmia and cataract;
• otolaryngological lesions: ear ringing or deafness;
• respiratory disorders: pharyngitis, asthma, dyspnea, laryngitis and nasal congestion, increased sputum volume, sinusitis, cough potentiation and bronchitis;
• cardiovascular disorders: angina pectoris, heart failure, changes in ECG readings, tachycardia, cerebral thrombosis and a decrease in blood pressure, and in addition, palpitations, orthostatic collapse, cardiomyopathy, AV block, myocardial ischemia and cardiac arrest;
• problems associated with hematological lesions: leukopenia or anemia;
• gastrointestinal signs: gastritis, dysphagia, glossitis, gastroenteritis with stomatitis, nausea and colitis, and in addition, gingivitis, rectal bleeding, esophagitis and xerostomia;
• metabolic disorders: gout, thirst, hypernatremia or -uricemia, and in addition, labile type diabetes and hypo / hyperglycemia;
• problems with urogenital function: cystitis, gynecomastia, urinary tract infections, ejaculation disorder, increased urination, nocturia, genital swelling and urinary incontinence;
• ODE lesions: arthritis, myasthenia gravis, tendosynovitis, ossalgia, arthrosis, as well as rupture in the tendon area, myalgia and synovitis;
• dermatological manifestations: common herpes, exfoliative or contact dermatitis, epidermal ulceration, photosensitivity, urticaria, rashes and itching;
• others: pain, shock, peripheral edema, chills, allergy symptoms and sweating.

Overdose

Possible manifestations of intoxication include headaches, nasal congestion, visual disturbances, dyspepsia, flushing, and dizziness.

In case of poisoning, standard supportive actions are taken.

Interactions with other drugs

The introduction of the drug together with agents that slow down the action of the CYP3A4 element (cimetidine or erythromycin) reduces the level of sildenafil clearance and increases its plasma values.

The combination of the drug with ritonavir, indinavir or saquinavir increases the intraplasmic Cmax, as well as the AUC of sildenafil - due to the slowdown in the activity of the CYP3A4 isoenzyme under the influence of these drugs.

There is a possibility that more powerful substances that slow down the activity of the CYP3A4 isoenzyme, among which itraconazole or ketoconazole, will increase the plasma values of sildenafil.

The combination of Vigrande and nitrates leads to the potentiation of the antihypertensive effect of the latter.

There is a description of one case with the appearance of signs of rhabdomyolysis with 1-time use of a portion of sildenafil in a person who used simvastatin.

Storage conditions

Vigrande must be stored at temperatures not exceeding the + 30 ° C mark.

Shelf life

Vigrande can be used for a 24-month term from the date of sale of the drug substance.

Analogs

The analogues of the medicine are the preparations Silagra, Ergos, Adamax with Zidena, and in addition Novigra, Erosil and Vekta with Kamshila. In addition, Viafil, Philap, Confido with Superwiga, Erektra and Potential are on the list.

Reviews

Vigrande receives good reviews from patients - they are satisfied with the effect of the drug, as well as the lower, in comparison with popular analogues, the cost of drugs.