Vigrande

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

The principle of therapeutic influence develops with the release of nitrous oxide inside the cavernous bodies (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 cases 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. There is 1 such plate in a box.

Pharmacodynamics

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

Sildenafil can cause temporary mild color blindness (green vs. blue). It is believed that this disorder develops due to the suppression of PDE-6, which is involved in light transmission processes within the retina. In vitro testing has shown that sildenafil's effect on PDE-6 is ten times weaker than its effect on PDE-5.

In vitro tests also show that sildenafil's effect on PDE5 is 10-10,000 times stronger than on other PDE isoforms (PDE1, -2, -3, as well as -4 and -6). For example, the effect on PDE5 is 4,000 times stronger than the effect on PDE3, the cAMP-specific PDE component involved in cardiac contractions.

Pharmacokinetics

After oral administration, sildenafil is absorbed at a high rate. The average absolute bioavailability is 40% (in the range of 25-63%). With a single oral dose of 0.1 g, the Cmax value is 18 ng / ml and in the case of taking on an empty stomach is achieved in 0.5-2 hours. In the case of taking sildenafil together with fatty foods, the rate of absorption decreases; Tmax values u200bu200bincrease by 1 hour, and the Cmax level drops by an average of 29%.

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

Less than 0.0002% of the LS portion (average value – 188 ng) is recorded after 1.5 hours inside the sperm.

Dosing and administration

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

Usually 50 mg of the drug is used for a single dose (it is recommended to take it on an empty stomach). In general, no more than 0.1 g of the drug is allowed to be taken at a time.

• Application for children

The medication is not prescribed in pediatrics (under 18 years of age).

Use Vigrande during pregnancy

Vigrande is not used to treat women.

Contraindications

Main contraindications:

• presence of allergy to sildenafil;
• hypersensitivity associated with excipients of the drug;
• combination with nitrous oxide donor substances (for example, amyl nitrite) or nitrates;
• conditions in which sexual contact is prohibited (angina pectoris, which is unstable, or heart failure in a severe degree of severity);
• loss of vision affecting one eye due to the development of ischemic neuropathy (anterior non-arteritic type) affecting the optic nerve;
• severe liver dysfunction;
• decreased blood pressure values (indicators less than 90/50 mmHg);
• a recent history of myocardial infarction or stroke;
• degenerative changes in the retina (hereditary in nature) (among these, for example, retinitis pigmentosa).

Side effects Vigrande

Side effects include:

• neurological disorders: neuralgia, depression, headaches, tremors and hypoesthesia, as well as flushing of the face, fainting, paresthesia, migraine, dizziness, impaired reflexes, ataxia and drowsiness or insomnia;
• problems of ophthalmological origin: visual disturbances (visual blurring, photophobia and changes in color perception), mydriasis, pain in the eyeballs or hemorrhage in them, conjunctivitis, xerophthalmia and cataracts;
• otolaryngological lesions: tinnitus or deafness;
• respiratory disorders: pharyngitis, bronchial asthma, dyspnea, laryngitis and nasal congestion, increased sputum volume, sinusitis, increased cough and bronchitis;
• cardiovascular disorders: angina pectoris, heart failure, changes in ECG readings, tachycardia, thrombosis of cerebral vessels and decreased blood pressure, as well as palpitations, orthostatic collapse, cardiomyopathy, AV block, myocardial ischemia and cardiac arrest;
• problems associated with hematological lesions: leukopenia or anemia;
• gastrointestinal symptoms: gastritis, dysphagia, glossitis, gastroenteritis with stomatitis, nausea and colitis, as well as gingivitis, rectal bleeding, esophagitis and xerostomia;
• metabolic disorders: gout, thirst, hypernatremia or -uricemia, as well as labile diabetes and hypo-/hyperglycemia;
• problems with urogenital function: cystitis, gynecomastia, urinary tract infections, ejaculation disorder, increased urination, nocturia, genital swelling and urinary incontinence;
• lesions of the musculoskeletal system: arthritis, myasthenia, tendosynovitis, ossalgia, arthrosis, as well as ruptures in the area of tendons, 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, hot flashes, and dizziness.

In case of poisoning, standard supportive measures are carried out.

Interactions with other drugs

Administration of the drug together with agents that inhibit the action of the CYP3A4 element (cimetidine or erythromycin) reduces the clearance rate of sildenafil and increases its plasma values.

Combination of the drug with ritonavir, indinavir or saquinavir increases intraplasmic Cmax, as well as AUC of sildenafil - due to the slowing down of the activity of the isoenzyme CYP3A4 under the influence of these drugs.

It is possible that more potent substances that inhibit the activity of the CYP3A4 isoenzyme, including itraconazole or ketoconazole, will increase plasma levels of sildenafil.

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

There is a description of one case of the development of signs of rhabdomyolysis with a single dose of sildenafil in a person who was using simvastatin.

Storage conditions

Vigrande must be stored at temperatures no higher than +30°C.

Shelf life

Vigrande can be used for a period of 24 months from the date of sale of the medicinal substance.

Analogues

Analogues of the drug are Silagra, Ergos, Adamax with Zidena, and also Novigra, Erosil and Vekta with Kamshila. In addition, the list includes Viafil, Filap, Confido with Superviga, Erectra and Potenciale.

Reviews

Vigrande receives good feedback from patients - they are satisfied with the effect the drug provides, as well as the lower cost of the drug compared to popular analogues.