JESTO-100 Tablet

For the treatment of erectile dysfunction. Little is known about the effects of sildenafil on neural control of the circulation or about the effects of sildenafil on neurocirculatory stress responses.

Dosage

Use in adults

The recommended dose is 50mg, taken as needed approximately 1 hour before sexual activity. Based on efficacy and toleration, the dose may be increased to 100mg or decreased 25mg. The maximum recommended dose is 100mg. The maximum recommended dosing frequency is once per day.

Use in the Elderly and in Patients with Impaired Renal or Hepatic Function

See the package insert about the details.

Use in Children

JESTO is not dictated for use in children.

Consistent with its known effects on the nitric oxide/cGMP pathway, sildenafil was shown to potentiate the hypotensive effects of nitrates, and its administration to patients who are using organic nitrates, either regularly and/or intermittently in any form is therefore contraindicated.

Sildenafil citrate is contraindicated in patients with a known hypersensitivity to any component of the tablet. A thorough medical history and physical examination should be undertaken to diagnose erectile dysfunction, determine potential underlying causes, and identify appropriate treatment.

Ocular: abnormal vision (mild and transient. Predominately colour tinge to vision, but also increased perception of light or blurred vision). Diplopia, temporary vision loss/decreased vision, ocular redness or bloodshot appearance, ocular burning, ocular swelling/pressure, increased intraocular pressure, retinal vascular disease or bleeding, vitreous detachment/traction and paramacular edema. Conjunctivitis, photophobia, eve haemorrhage, cataract, dry eyes and eye pain.

Urogenital: cases or priapism (prolonged erection) have been reported. Cystitis, nocturia, urinary frequency, breast enlargement, urinary incontinence, abnormal ejaculation, genital edema, anorgasmia and haematuria have also been reported.

Body as a whole: face edema, photosensitivity reaction, shock, asthenia, pain, chills, accidental fall, abdominal pain, allergic reaction, chest pain, accidental injury.

Digestive: dyspepsia, vomiting, glossitis, colitis, dysphagia, gastritis, gastroenteritis, esophagitis, stomatitis, dry mouth, liver function tests abnormal, rectal hemorrhage, gingivitis.

Hemic and Lymphatic: anemia and leukopenia.

Metabolic and Nutritional: thirst, edema, gout unstable diabetes, hyperglycemia, peripheral edema, hyperuricemia, hypoglycemic reaction and hypernatremia.

Musculoskeletal: arthritis, arthroses, myalgia, tendon rupture, and tenosynovitis, bone pain, myasthenia, synovitis, paresthesia, tremor, vertigo, depression, insomnia, somnolence, abnormal dreams, reflexes decreased, and hypoesthesia.

Respiratory: nasal congestion, asthma, dyspnea, laryngitis, pharyngitis, sinusitis, bronchitis, sputum increased, cough increased.

Skin and Appendages: urticaria, herpes simplex, pruritus, sweating, skin ulcer, contact dermatitis, exfoliative dermatitis.

Special Senses: tinnitus, deafness, ear pain.

Sildenafil is a weak inhibitor of the CYP450 isoforms 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4.

No significant interactions were shown with tolbutamide or warfarin, both of which are metabolised by CYP2C9.

Single doses of antacid (magnesium Hydroxide/ aluminium Hydroxide) did not affect the bioavailability of sildenafil citrate.

It can be expected that concomitant administration of CYP3A4 inducers, such as rifampicin, will decrease plasma levels of sildenafil citrate.

Contraindicated

There is a potential for cardiac risk of sexual activity in patients with pre-existing cardiovascular disease. Therefore treatments for erectile dysfunction, including sildenafil citrate should not be generally used in men for whom sexual activity is inadvisable because of their underlying cardiovascular status. A thorough medical history and physical examination should be undertaken to diagnose erectile dysfunction determine potential underlying causes and identify appropriate treatment JESTO has systemic vasodilatory properties that resulted in transient decreases in supine blood pressure in healthy volunteers.

In the event of an erection that persists longer than 4 hours, the patient should seek immediate medical assistance. If priapism is not treated immediately penile tissue damage and permanent loss of potency could result. Agents for the treatment of erectile dysfunction should be used with caution in patients with anatomical deformation of the penis (such as angulation, cavernosal fibrosis of Peyronie’s disease), or in patients who have conditions which may predispose them to priapism (such as sickle cell anaemia, multiple myeloma or leukaemia). Agents for the treatment of erectile dysfunction inadvisable. The safety and efficacy of Combinations of JESTO with other treatments for erectile dysfunction have not been studied. Therefore the use of such combinations is not recommended. Controlled studies of drug interactions between JESTO and other antihypertensive medications have not been performed. JESTO has no effect on bleeding time, including during co-administration with aspirin. In vitro studies with aggregatory effect of sodium nitroprusside (a nitric oxide donor). There is no safety information on the administration of ulceration. Therefore sildenafil Citrate should be administered with caution to these patients.

JESTO restores impaired erectile function by increasing blood flow to the penis, in response to sexual stimulation. Sildenafil is a selective inhibitor of cGMP specific phosphodiesterase type 5 (PDF5) which is responsible for degradation of cGMP in the corpus cavernosum. Sildenafil has no direct relaxant effect on isolated human corpus cavernosum but enhances the relaxant effect of NO on this tissue. When the NO/cGMP pathway is activated, during sexual stimulation, inhibition of PDE5 by sildenafil results in increased corpus cavernosum levels of cGMP, producing smooth muscle relaxation in the corpus cavernosum allowing the inflow of blood.