SEGUREX, MALE ERECTILE DYSFUNTION ED

SEGUREX COMPR.
Division: MEDICAL
Active Ingredient: Sildenafil Citrate
Coated tablets. ORAL THERAPY FOR MALE ERECTILE DYSFUNCTION
Formula: Each tablet contains SEGUREX:
Sildenafil (as citrate From 35.11 to 70.22 and 140.45 mg (equivalent to Sildenafil 25 mg 50 mg 100 mg..........................
Excipients ........................................................................................ Cs.

Therapeutic Action:
The administration of sildenafil increases the effectiveness of the physiological mechanisms involved in penile erection in the presence of sexual stimulation.
In patients with organic or psychogenic erectile dysfunction, sildenafil administration
improves the quality of erection after sexual stimulation. The increased efficiency is observed
about 1 hour after drug administration. The effect of sildenafil
occurs in patients with a wide variety of diseases, including cardiovascular diseases,
bypass graft surgery, diabetes mellitus, prostatectomy or transurethral prostate resection,
spinal cord injuries, mental depression and in the presence of drugs such as antidepressants or psychotic.

Indications:
Oral treatment of male erectile dysfunction.

Dosage:
Sildenafil is a Potent selective inhibitor of Phosphodiesterase type 5 (PDE-5), Guanosinamonofosfato cyclic (cGMP) specific. The response of penile erectile tissue is mediated by nitric oxide (NO) released by action of neurons and endothelial cells of the penis during sexual stimulation. The NO through enzymatic activation of guanylate cyclase, stimulates the synthesis of messenger Cyclic GMP, which in turn results in a cascade of events ending with relaxation
smooth muscle of the corpora cavernosa and more blood to them, that begins the process of penile tumescence. This reaches its maximum when a compression occurs venous occlusion. The inhibition of PDE-5 as a result of sildenafil prevents the hydrolysis of cyclic GMP and thus get a higher concentration this intracellular messenger and more lasting erection. Dose levels
recommended, the effects of sildenafil have been observed only in the presence of stimulation
sexual. The importance of high selectivity of action of PDE-5 in relation to other
FDE, is the absence of effects of sildenafil in healthy volunteers, on contraction
heart in vitro and electrocardiogram. Their lower selectivity with respect to the PDE-
6, which is found mainly in retina, explains some visual disturbances observed
with higher doses, patients described as sensitivity to light and tinted vision color.

Pharmacokinetics:
Sildenafil absorption is rapid following oral administration in fasting, reaching
peak concentrations in blood at 60 minutes (30-120). If ingested during
a high-fat meal, the peak may be delayed about 60 minutes. Sildenafil
is widely distributed in tissues (volume of distribution at steady state:
105 L). Circle, with its major metabolite N-desmethyl sildenafil, most
part attached to plasma proteins (> 95%). Metabolite concentrations
reach 40% of those achieved in the sildenafil. Only a tiny proportion of the dose
given (1 / 10000) appears in the semen 90 minutes after the shot. The half-life
terminal is about 4 hours. Sildenafil is eliminated by the liver microsomal system
mainly by CYP3A4 and a small proportion by isozyme
CYP2C9. The N-desmethyl sildenafil is an activity profile similar to that of the parent drug
with power equal to 50%. Both are excreted predominantly in faeces
and to a lesser extent in urine (80% and 13% of the oral dose, respectively).
Plasma concentrations may be higher than in control volunteers
in over 65 healthy subjects (> 40%) in patients with severe renal failure
creatinine clearance <30 ml / min (100%) and in patients with liver cirrhosis (80%).

Cautions and warnings:
The usual average dose for most patients is 50 mg given appropriate Segurex 25-50-100
SILDENAFIL 25-50-100 mg ® mately 1 hour before sexual activity. In some cases it may be taken between 4 hours and 1 / 2 hour before intercourse. Based on the efficacy and tolerability the dose may be increased to a maximum of 100 mg or decreased to 25 mg depending on individual response of each patient. The maximum frequency is recommended to take one a day. In patients 65 and older or those with severe renal insufficiency (clearance
<30 ml / mim) or with cirrhosis should be started at a dose of 25 mg.

Contraindications:
Hypersensitivity to sildenafil or any component of the product. Pregnant Patients treated with organic nitrates or nitric oxide donors.

Warnings:
Patients who require treatment with nitrates should avoid concomitant use as sildenafil may potentiate the hypotensive effect of these (See Interactions). Segurex does not protect against sexually transmitted diseases, including human immunodeficiency virus (HIV)

Precautions:
Before indicating Segurex treatment the PATIENT Should be fully evaluated to determine the etiology of erectile dysfunction.
Segurex should be administered with caution in patients with anatomic abnormalities
penile angulation, cavernosal fibrosis (Peyronie disease) and those Likely to have priapism or other disorders such as sickle cell anemia, multiple myeloma multiple or leukemia.
While sildenafil given alone or in combination with aspirin did not affect bleeding time,
In vitro studies indicate that potentiates the antiaggregatory effect of sodium nitroprusside
(Nitric oxide donor). Segurex should be administered with caution in patients risk of bleeding or active ulcer.
Because sexual activity can increase the risk of some heart disorders Should assess cardiovascular function prior to initiation of treatment.
Sildenafil should be administered with caution in patients with retinitis pigmentosa due
that in some individuals with this condition there is a genetic disorder phosphodiesterases in the retina.
The efficacy and safety of sildenafil administered in combination with other treatments
male erectile dysfunction has not been evaluated. Therefore, the association is not recommended until it has carried out appropriate research with Drug Interactions.
In vitro studies: Inhibition of CYP3A4 and CYP2C9 isoenzymes may reduce the elimination capacity of sildenafil. Since it is a weak inhibitor of CYP1A2, CYP2E9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4 No changes are expected in the elimination of substrates metabolized by these isoenzymes.
Live studies: The co-administration of 50 mg of sildenafil in healthy volunteers with cimetidine may increase sildenafil plasma concentrations by about 56%. The administration of a single 100 mg dose of sildenafil in patients receiving with an inhibitor of CYP3A4 such as erythromycin (500 mg twice daily for 5 days) produced a 182% increase in area under the curve (AUC) of sildenafil. Furthermore, inhibitors more potent CYP3A4 such as erythromycin, ketoconazole, itraconazole or mibefradil have the ability to reduce sildenafil clearance. In patients treated with these drugs should be considered to reduce the dose of sildenafil to 25 mg.
By contrast, the administration of sildenafil with CYP3A4 inducers such as rifampicin may reduce plasma levels of it.
The single dose administration of antacids containing aluminum hydroxide or
magnesium does not affect the bioavailability of sildenafil.
Inhibitors of CYP2C9 (tolbutamide, warfarin) or CYP2D6 (selective inhibitors
serotonin reuptake, tricyclic antidepressants), thiazide diuretics, angiotensin
of angiotensin converting enzyme blockers or calcium channels affect the pharmacokinetics of sildenafil.
The area under the curve (AUC) of its active metabolite N-desmethyl-sildenafil, increases
62% with the use of potassium-sparing diuretics or loop diuretics and 102%
with administration of nonselective beta blockers. However, it is not anticipated that these
effects on the active metabolite of sildenafil have significant clinical consequences.
No significant interactions were found with tolbutamide or warfarin.
Sildenafil at recommended doses does not potentiate the effect of 150 mg of aspirin on
coagulation. Nor hypotensive effects of alcohol in healthy volunteers. No
have found significant differences in adverse effect profile presented by patients
with or without antihypertensive medication on treatment with sildenafil.
Carcinogenesis and tumorigenesis: Sildenafil has not demonstrated carcinogenicity in two rodent species studied.
Mutagenesis: Sildenafil has not demonstrated mutagenicity in vitro tests with bacteria and cells Chinese hamster ovary or clastogenesis in vitro studies on human lymphocytes and
live mouse micronucleus test.
Pregnancy and Reproduction: In rats and rabbits at doses between 20 and 40 times the maximum recommended in humans based on mg/m2 no evidence of teratogenicity or toxicity
the embryo or fetus. No problems were observed on fertility of female rats
or male. Since there is insufficient information on pregnant women, sildenafil
should not be administered during pregnancy.
No abnormalities were observed morphological or functional sperm
healthy volunteers receiving single doses of 100 mg of sildenafil orally.
Breastfeeding It is unknown whether sildenafil appears in breast milk.
Segurex is not indicated in children.
In people over 65 is recommended to adjust the dose (see Dosage and Body).

Adverse Reactions:
In Controlled Clinical trials, the discontinuation rate due to adverse events secondary to sildenafil (2.5%) is not statistically significant compared to the percentage discontinuation found in the placebo group (2.3%). The incidence of some increased adverse effects related to dose.
Following is the list of adverse reactions by device and frequency.
Qualifies as common to those present with an incidence greater than 2%. Highlights
those that occur most frequently in the active treatment group than in
the placebo group. Qualifies as occasional those observed with a frequency
less than 2% and whose relationship with sildenafil has not been established.
General. Frequent: flu syndrome. Infrequent: facial edema, thirst, photosensitivity,
shock, asthenia, chills, accidental falls, accidental injury.
Cardiovascular. Uncommon: chest pain, AV block, tachycardia, palpitations, hypotension,
orthostatic hypotension, myocardial ischemia, heart failure, heart failure,
ECG changes, syncope, cardiomyopathy.
Digestive. Common: dyspepsia, diarrhea. Dyspepsia is more common with doses of
100 mg with respect to the above. Occasional abdominal pain, vomiting, glossitis, dysphagia,
gastritis, gastroenteritis, esophagitis, stomatitis, dry mouth, rectal hemorrhage, gingivitis.
Endocrine. Infrequent: gout, diabetes, peripheral edema, hyperglycemia, hypoglycemia, hypernatremia,
hyperuricemia.
Haemolymphatic. Infrequent: anemia, leukopenia.
Musculoskeletal. Common: back pain, arthralgia. Infrequent: arthritis, arthrosis, myalgia,
tenosynovitis, myasthenia, bone pain, tendon rupture.
Neurological. Common: headache, vertigo. Uncommon: migraine, ataxia, hypertonia, neuropathy,
tremor, dizziness, hyporeflexia, paresthesia, hyperesthesia, mydriasis, tinnitus.
Psychiatric. Infrequent: depression, insomnia, nightmares, drowsiness.
Respiratory. Common: upper respiratory tract infection, nasal congestion. Casual
asthma, dyspnea, pharyngitis, laryngitis, sinusitis, bronchitis, cough, increased sputum production.
Dermatological. Common: flushing, rash. Casual: herpes simplex, urticaria, pruritus,
ulcer, contact dermatitis, exfoliative dermatitis, excessive sweating.
Urogenital. Common: urinary tract infection. Infrequent: cystitis, nocturia, abnormal ejaculation, genital edema, anorgasmia, urinary incontinence, gynecomastia. Have not been reported Priapism.
Sensory. Common: visual disturbances (photophobia, blurred vision and impaired vision
color). These are more common with doses of 100 mg with respect to minors.
Infrequent: conjunctivitis, photophobia, eye pain, dry eyes, cataracts, eye hemorrhage,
deafness, otalgia.
Lab. Uncommon: changes in liver function tests. Dyspepsia and
visual disturbances were more frequent at doses of 100 mg than with lower doses.

Overdosage:
With Doses of 800 mg incidence of adverse reactions is higher than the aforementione with the usual doses.
In the event of overdosage, seek medical advice or with Poison Control Centers (With this Warnings and Instructions copy)

Conditions of Storage and Consevation:
Store at room Temperature between 15 and 30° C "This medication should be used only under medical supervision and prescription and not be repeated without a new prescription. KEEP MEDICINES OUT OF REACH OF CHILDERN