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Ministry of Health of the Republic of Moldova
Directions for use
Penfix 6,25 mg/dose
Oral spray, suspension
Number of registration certificate In Republic of Moldova.
TRADE NAME: Penfix 6,25/dose
ICN ACTIVE INGRIDIENT: Sildenafilum
Active ingredient: Sildenafil citrate equivalent to 6,25 mg sildenafil base/dose
Other ingredients: Glycerol, macrogol 400, xanthan gum, benzoic acid, acesulfame potassium, polysorbate 80, flavor raspberries, potassium sorbate, saccharin sodium, purified water.
Oral spray, suspension.
It’s a white suspension, raspberries’ taste and specific smell, after agitation became homogeneous.
PHARMACEUTICAL GROUP AND ATC CODE
Drugs use in erectile dysfunction, G04BE03.
Sildenafil is a powerful and selective inhibitor of cGMP-spe-cific phosphodiesterase type 5 (PDE5) which is responsible for the breakdown of cGMP in the cavernous body. Increasing the concentration of cGMP, reduces intracellular calcium concentration and relaxation of the corpus cavernously smooth muscle cells, followed by an overflow sinus blood flow by background amplification penile compression and efferent veins. The drug increases and prologs an erection due to sexual simulation. PDE5 inhibition with sildenafil in these tissues may increase the antiplatelet activity of nitric oxide platelets in vitro, inhibition of platelet aggregates formation and peripheral arteriovenous dilatation in vivo. High-dose promotes a significant increase in bleeding time (but did not have an effect on the clotting time). It dilates the blood vessels, of both arterial and venous, which leads to a reduction in systolic and diastolic blood pressure and increased heart rate. The drug has no effect on fertility, and has ejaculate volume and viscosity. It has no teratogenic, mutagenic, clastogenic and carcinogenic proprieties.
Sildenafil is rapidly absorbed. The concentration of sildenafil in plasma is reached in maximum 10 minutes, after oral dosing of sildenafil. The absolutely internal bioavailability is 50%.
Sildenafil and its major circulating N-desmetilovy methabolite is bound approximately 96% in plasma proteins. In healthy volunteers receiving drug less than 0.0002% (average 188ng) of the dose was found semen at 90 min after administration.
Sildenafil is metabolized primarily by the action of CYP3A4 (major route) and CYP2C9 (option path) of the liver microsomal isoenzymes. The main circulating metabolite is formed by the N-desmetilirovaniya sildenafil. The concentrations of metabolite in plasma is approximately 40% of sildenafil. N-desmetilmetabolite exposed further metabolism, the final period of its half-life is about 4 hours.
Total body clearance of sildenafil is 41 l/h, and the terminal half-life – 5.3 hours after oral administration, sildenafil apprears as metabolites in the urine lesser extent (approximately 13% of the administered dose).
Pharmacokinetics in special patient groups
For healthy elderly volunteers (65 year and older) sildenafil clearance is reduced, and the concentration of free drug in plasma and N-demethyl metabolite is approximately 90% higher than its level in healthy young volunteers (18-45 years).
For volunteers with light (creatinine clearance 50-80 ml/min) or moderate (creatinine clearance 30-49 ml/min) renal insufficiency pharmacokinetics, after a single dose of sildenafil (25mg), has not changed. The volunteers with critical(creatinine clearance of 30 ml/min) of renal insufficiency sildenafil clearance is reduced, resulting of increase in AUC (100%) and Cmax (88%), compared with those from volunteers agematched, is not suffering from renal dysfunction.
Volunteers with cirrhosis (Child-Pugh A and B) sildenafil clearance degreased, thereby increasing performance AUC (84%) and Cmax (47%) compared with those of the volunteers of the same age who do not have liver failure. In patient with severe hepatic insufficiency pharmacokinetics of sildenafil has not been studied.
Erectile dysfunction characterized by the inability to achieve or maintain a penile erection sufficient for satisfactory sexual activity.
For making the drug effective, sexual stimulation is required.
DOSAGE AND METHOD OF ADMINISTRATION
Shake before use contents of the vial.
Before the first use, you must fill dosing pump by removing the protective cap and pressing the metering valve several times until the spray. By clicking on the metering valve is applied to the drug or under the tongue, and kept in the mouth until complete absorption.
Use in adult
Recommended dose of PENFIKS is 25 mg or 4 sprays (6.25 mg/1 spray). PENFIKS is taken 10 minutes before anticipated sexual activity.
Depending on tolerance and efficacy, the dose may be increased to maximum of 50 mg (8 spray), but can be reduced to 12.5 mg (2 spray).
Patient may attempt to carry out sexual intercourse at any time within 36 hours after taking the drug in order to establish the optimal response time to receive the drug.
The maximum recommended frequency of admission – once.
Dosage adjustments are not required in elderly patients.
Patients with renal impairment
For patients with light (creatinine clearance 50-80 ml/min) or moderate (creatinine clearance 30-49 ml/min) renal impairment requires selection of doses.
Patients with severe (creatininamenee clearance 30 ml/min) renal impairment where sildenafil clearance is reduced, recommended dose is 12.5 mg.
Patients with hepatic impairment
Sildenafil clearance is reduced for patients with hepatic impairment (e.g. cirrhosis), so 12.5 mg should be considered.
Use in patients taking other medicinal products
Because of interaction of sildenafil with their ritonavir at combined use, is not recommended to increase the dose more than 12.5 mg within 48 hours.
The use of sildenafil initial doses of 12.5 mg is recommended for patients receiving concurrent of CYP3A4 (for example, erythromycin, saquinavir, ketoconazole, itraconazole). To minimize the possibility of developing postural hypotension, patients should be hemodynamically stabilized at treating alpha-blocker, before you start the treatment with sildenafil. Thereby in such cases it is advisable to start the treatment with sildenafil at lower doses.
MedDRA frequency convention
Very frequent (>1/10)
Infrequent (>1/1000 and <1/100)
Rare (>1/10000 and <1/1000)
Very rare (<1/10000)
With unknown frequency (can not be estimated from available data).
The most common adverse reactions in clinical trials in patients receiving sildenafil were: headache, flushing, dyspepsia, visual disturbances, nasal congestion, dizziness and distortion of color.
Fouls of the immune system Rare:
Disorders of the nervous system
Very common: headache
Uncommon: somnolence, hypoesthesia
Rare: stroke, fainting
Unclear frequency: convulsions, transient ischemic attack
Violations by the authority of Common: blurred vision, distorsion of color perception
Uncommon: conjunctivitis, xerophtalmia, and other violations
Unclear frequency: violation of view fields, anterior ischemic optic neuropathy, non-arteritic (NAION), retinal vascular occlusion
Violations by the organ of hearing and labyrinthine disorders
Uncommon: tinnitus, vertigo
Violation of the heart
Uncommon: tachycardia, palpitations
Rare: myocardial infarction, ventricular fibrillation
Unclear frequency: ventricular arrhythmia, unstable angina, sudden carciac death
Violations by vessels often: hyperemia of the person
Rare: hypotension, hypertension
Violations of the respiratory system, chest and mediastinum
Often: nasal congestion
Violations by the gastrointestinal tract
Uncommon: nausea, vomiting, dry mouth
Violations of the skin and subcutaneous tissue
Violations by musculoskeletal and connective tissue
Violations by the genital and breast Obscure frequency: prolonged erection.
General disorders and administration
Uncommon: chest pain, tiredness
Impact on the results of laboratory and instrumental investigations
In case of other effects mentioned above, than those specified in this manual, you need to see a doctor.
Preparations for the treatment of erectile dysfunction should not be given to men for whom sexual activity is undesirable (eg. Patients with severe cardiovascular disorders such as unstable angina or severe heart failure).
Sildenafil is contraindicated for patients who have loss of vision in one eye due to anterior ischemic optic neuropathy. Has not been studied the safety of using sildenafil for those patient subgroups, like: people with severe hepatic impairment, hypotension (blood pressure <90/50 mmHg), stroke, or myocardial infarction, hereditary degenerative retinal disorders, such as retinitis pigment’s.
Symptoms: hot flashes, dizziness, flushing of the face, headache, blurred vision, indigestion, blood pressure reduction.
Treatment: symptomatic therapy.
WARNING AND SPECIAL PRECAUTIONS FOR USE
Before taking Sildenafil the patient should undertake a medical checking of the cardiovascular system.
It has to use Sildenafil with caution the patients with anatomical deformation of the penis (such as angulations, cavernous fibrosis or Peyronie’s disease), also people with medical conditions that predispose to the development of priapism (such as sickle cell anemia, multiple myeloma, or leukemia).
It has to be use with caution also for patients with tendency to bleeding, gastric ulcer and duodenal ulcer in acute phase, with hereditary retinitis pigments.
In experimental studies found no evidence of carcinogenicity of sildenafil. Bacterial and in vivo mutagenicity test for the study were negative.
Sildenafil is not used in patients under age of 18 years.
Effects on ability to drive vechicles and management mecanisms.
Sildenafil has no effect on the ability to drive vehicles and management mechanisms.
Interctions with other medicaments and other types of interactions
With simultaneous application of inhibitors of CYP3A4 (erythromycin, cimetidine) degreased clearance of sildenafil, sildenafil increases the concentration in blood of plasma.
With Simultaneous use of indinavir, saquinavir, ritonavir increases the plasma Cmax and AUC values of sildenafil, which is due to inhibition of CYP3A4 isoenzyme under the influence of indinavir, saquinavir, ritonavir.
It can be expected that stronger inhibitors isoenzyme CYP3A4, such as: itraconazole and ketoconazole, will increase the concentration of sildenafil in blood plasma.
With simultaneous use of nitrates its increase hypertensive effect of nitrates.
There is a case of the development the symptoms of rhabdomyolysis after a single dose of sildenafil, dose in patients receiving simvastatin.
Oral spray, suspension 6.25 mg/dose, 12 ml/48 doses in vial. 1 vial together with instruction for administration in the carton box.
Store below 25°C.
Store in the original package, in order to protect from moisture and light.
Keep away from children.
Do not use it after expiration date shown on the pack.
With medical description
DATE OF LAST TEXT REVIEW
NAME AND ADRESS
Republic of Moldova