NEO-GRA (sildenafile)100mg №2 caps


DRUG FORM: Capsules.
COMPOSITION: Active substance: Sildenafil citrate – 50mg; 100mg (calculated as sildenafil). Aiding substances: lactosa, starch, calcium stearate.
PHARMACOLOGICAL GROUP: Drug for erectile dysfunction treatment.
Pharmacodynamics: Sildenafil citrate restores erectile function disorder and ensures natural response on the sexual arousal. Physiological mechanism of erection implies nitrogen oxide release at time of sexual stimulation in the cavernous body. Nitrogen oxide activates enzyme Guanulate cyclase, which causes cyclic guanosine monophosphate (cGMP) level increase, relaxation of cavernous body smooth muscle and blood circulation strengthening in the genital organ. Sildenafil is a powerful and selective inhibitor of (cGMP) specific phosphodiesterase 5 type (5 PDE), which is responsible for degradation of cGMP in the cavernous body. Sildenafil has no direct weakening impact on the cavernous body, but actively strengthens weakening effect of nitrogen oxide on this tissue. At time of sexual arousal, nitrogen oxide releases in the cavernous body under the influence of Sildenafil, which suppresses 5 PDE and causes increase of cGMP level. Finally, smooth muscles of cavernous body relax and blood flow strengthened in the cavernous body.
Sexual stimulation is necessary for desired pharmacological effect reveal of “Neo-Gra”. At one-time intake up to 100 mg dose, in healthy volunteers the preparation doesn’t cause considerable clinical changes on the electrocardiogram. In condition of confinement to bed, maximum reduction of systolic arterial pressure makes up 8,4 mm Hg. at time of Sildenafil citrate 100mg intake. But diastolic pressure appropriate reduction – on average 5,5 mm Hg. Decrease of arterial pressure is conditioned by vasodilation effect, that can be related to cGMP level increase in the blood-vessel smooth muscles. Sildenafil doesn’t influence on sight and prescription contrast. In some patients, after 1 hour from 100mg dose intake is revealed slight and transitive disorders of colour distinguish (blue/green); these changes disappear after 2 hours.
Pharmacokinetics: Sildenafil citrate is quickly absorbed. After peroral intake on an empty stomach, preparation concentration in plasma reaches to peak during 30-120 minutes (on average in 60 min) bioavailability 41%.
In case of intake together with fatty foods, its absorption speed lowers. Tmax increases by 60 minutes and Cmax lowers by 29%. 96% of absorbed Sildenafil citrate relates to plasma proteins. Sildenafil mostly metabolizes by the influence of liver microsomal isoenzyme CYP 3A4 and CYP 2C9. Main metabolite formatted by Sildenafil M-desmethylation further metabolizes and eliminated from the organism together with excrement (approximately 80%), less together with urine (approximately 13%).
· Hypersensitivity towards any compounding components in the preparation.
· Because the influence on nitrogen oxide and cGMP change, Sildenafil citrate strengthens hypotensive action of nitrates, so its use is contraindicated in those patients who take nitrogen oxide donator or nitrates in any form.
ADMINISTRATION AND DOSAGE RULE: Capsules of “Neo-Gra” is taken perorally.
Recommended dose – 50mg intake one hour before planned sexual activity. Dose can be increased up to 100mg or decrease to 25mg, considering preparation resistance and efficiency. Maximum recommended dose 100mg. Maximum recommended usage frequency – one time intake in a day. Elderly people and patients who have liver and kidney functional disorder are recommended the same scheme of usage. “Neo-Gra” isn’t used in children.
SIDE EFFECTS: Side effects caused by Sildenafil citrate is moderate or light character. There may develop: dizziness, headache, vasodilation, hypotension, asthenia, nasal breathing difficulty, lacrimation, light and colour perception, exact sight disorder, dyspepsia, diarrhea, nausea, abdominalgiya, lumbodynia, arthralgia, myalgia. Muscle hypertonicity, insomnia, dyspnea, rash on the skin, prolonged and painful erection.
SAFETY MEASURES: For erection disorder diagnostic, determining its possible reasons and adequate treatment, it is necessary to collect full medical anamnesis and make comprehensive physical research. Sexual activity is a risk at time of heart disease. Before beginning any therapy at time of erection disorder, a doctor should research cardiovascular system.
Safety and efficiency of “Neo-Gra” in combination with other therapeutic agents that are used for erection disorder treatment isn’t learned, that’s why similar combinations aren’t recommended.
Erection disorder treating preparations is used safely for patients who have genital organ anatomic deformation (angulation, Cavernous fibrosis or peyronie’s disease) or patients who have multiple myeloma, drepancytic anemia or leukemia.
Small proportions of patients with innate pigmented retinitis have retina phosphodiesterase activity hereditary disorders. Sildenafil is used safely in such patient, because there aren’t data about preparation.
INTERACTION WITH OTHER PREPARATIONS: Cimetidine (800mg) represents nonspecific inhibitor of CYP3A4, taking together with “Neo-Gra” causes increase of Sildenafil concentration in plasma by 56%. Populate pharmacokinetic analysis of clinical studies results showed reduction of Sildenafil clearance at simultaneous use of “Neo-Gra” CYP3A4 inhibitor (such as Ketoconazole, Erythromycin, Cimetidine). Though, frequency of adverse events in these patients did not increase.
Take Antacids once (magnesium hydroxide/aluminum hydroxide) doesn’t influence on Sildenafil bioavailability. According to the data of populate pharmacokinetic analysis CYP2C9 inhibitors (such as Tolbutamide, Warfarin), CYP2D6 inhibitors (such as selective serotonin re-uptake inhibitors, tricyclic antidepressant), thiazide and thiazide diuretics, ansiform and potassium-sparing diuretic, calcium antagonist, beta blockers and CYP450 inhibitors (such as Rifampicin, barbiturates) don’t influence on Sildenafil pharmacokinetics.
PREGNANCY AND LACTATION PERIOD: “Neo-Gra” isn’t used in women. Reproductive researches implemented in rats and rabbits showed that peroral usage of Sildenafil doesn’t cause teratogenic action, doesn’t impact on reproductive function and doesn’t cause fetus postnatal and new born development disorder. Single intake of 100 mg Neo-Gra in healthy people doesn’t change sperm mobility and morphology.
INFLUENCE ON VEHICLE AND MECHANISMS MANAGEMENT: Management of vehicles and mechanisms doesn’t require protecting special security measures.
OVERDOSE: Overdose of Sildenafil (up to 800 mg) reveals the same side effects, as small dose intake of preparation, but overdose increases frequency of side effects reveal. In case of need there is carried out symptomatic treatment.
PRODUCTION FORM: Primary package: 2 capsules on pvc/alu blister;
Secondary package: One blister in a carton box with instruction..
SHELF-LIFE: 2 years.
STORAGE CONDITIONS: Store at dry, protected from light and inaccessible for children place, at room temperature.
ISSUE: Pharmaceutical product group III, issued without doctor’s prescription.
PRODUSER: ,,Neopharmi” Ltd.

12th km, David Agmashenebeli alley, Tbilisi, Georgia
Tel/Fax: +995 (032) 259-64-46; 259-57-90.