Products name : Esculap
Manufacturer : Balkan Pharmaceuticals
Price per with 20 tablets 20mg
Active chemicals Tadalafil Citrate
The Balkan Esculap (Tadalafil) is a selective, efficient and reversible inhibitor of type 5 phosphodiesterase (PDE5), cyclic guanosine monophosphate (cGMP).
When sexual arousal causes local release of nitric oxide, inhibition of tadalafil PDE5 leads to an increase in cGMP levels in the cavernous body of the penis.
The consequence is the relaxation of the smooth muscles of the arteries and the flow of blood into the tissues of the penis, which causes an erection. Tadalafil does not work in the absence of sexual stimulation.
In vitro studies have shown that tadalafil is a selective PDE5 inhibitor. PDE5 is an enzyme found in the smooth muscles of the corpus cavernosum, the smooth muscles of internal organ vessels, skeletal muscles, platelets, kidneys, lungs and cerebellum.
The action of the Balkan Esculap (Tadalafil) on PDE5 is more active than other phosphodiesterases. Tadalafil is 10,000 times more potent for PDE5 than for PDE1, PDE2 and PDE4, which are in the heart, brain, blood vessels, liver and other organs. Tadalafil 10,000 times more actively blocks PDE5 than PDE3 - an enzyme found in the heart and blood vessels.
This selectivity for PDE5 compared to FDHD is important because FDEZ is an enzyme involved in the contraction of the heart muscle. In addition, tadalafil is approximately 700 times more active than PDE5 than PDE6, which is found in the retina and is responsible for photo transmission. Tadalafil also has a 10,000-fold stronger effect on PDE5 than its effect on PDE7-PDE10.
Tadalafil improves erection and the possibility of successful sex. The medicine is valid for 36 hours. The effect is still 16 minutes after drug administration in the presence of sexual arousal.
Tadalafil in healthy individuals did not cause significant changes in systolic and diastolic blood pressure compared to placebo in the posterior lying position (maximum mean decrease of 1 6/0, 8 mm HgV, respectively) and standing (mean mean decrease in 0, 2/4 and 6 mm Hg, respectively).
Tadalafil does not cause a significant change in heart rate.
Tadalafil does not cause changes in color recognition (blue / green), which is explained by the low affinity for PDEB. In addition, there is no effect of tadalafil on visual acuity, electroretinogram, intraocular pressure, and pupil size.
In the male tadalafil study at a daily dose of 10 mg, there was no clinically significant effect of the drug on sperm count, sperm motility and sperm count and concentration.
Balkan Esculap Pharmacokinetics (Tadalafil)
After taking tadalafil in, tadalafil is rapidly absorbed. The maximum mean plasma concentration (C max) is reached on average 2 hours after ingestion.
The rate and extent of absorption of tadalafil do not depend on food intake, so that tadalafil can be given regardless of food intake. Receiving time (morning or evening) had no clinically significant effect on the rate and extent of absorption.
Indications
Tadalafil is indicated for erectile dysfunction.
METHOD OF USE AND DOSE The Balkan Esculap
Tadalafil is administered internally.
Use in middle-aged men.
Tadalafil is used indoors irrespective of food intake at an initial dose of 20 mg. Patients may attempt to intervene within 36 hours of admission to determine an optimal response time for the drug.
The recommended maximum reception frequency is once a day. In advanced aged men (65 years of age and older), dose adjustments are not necessary.
The renal failure of the Balkan Esculap
In patients with minor renal dysfunction no change in dosage regimen is required. At moderate renal insufficiency (creatinine Cl 31-50 ml / min), the recommended starting dose - not more than 5 mg per day, the maximum dose. Dose not more than 10 mg every 48 hours In severe severe renal insufficiency, hemodialysis is recommended - no more than 5 mg per day.
Liver disorders in the function of Esculap in the Balkans
With a low and moderate degree of hepatic impairment, the maximum dose is 10 mg once daily. In severe hepatic insufficiency, the use of the medicine is not recommended because there are no data from controlled clinical trials on safety
Concomitant therapy:
in patients taking strong CYP3A4 inhibitors (eg ketoconazole, ritonavir, etc.), the recommended maximum dose is 10 mg, not more than once every 72 hours.
The use of tadalafil with concomitant nitrate treatment (up to 48 hours) or with alpha-blockers (with the exception of 0.4 mg tamsulosin once daily) is contraindicated.
Tadalafil in children
Tadalafil is not used in people under 18 years of age.
