Content on this page requires a newer version of Adobe Flash Player.

Get Adobe Flash player

 
 
 
 
 
 
 
 
 
 

EXILAR 10

Quick Overview

Our aim is to reach out to the globe within shortest possible time frame.


To promote this objective, not only we distribute and market our Male Health range of products globally through our distribution channels but we also undertake ‘contract manufacturing’& ‘formulation development ’of our wide range of generic products such as Exilar 10 mg tablet which contains Tadalafil 10 mg .

EXILAR 10

Double click on above image to view full picture

Zoom Out
Zoom In

Details

COMPOSITION:

EXILAR 10

Each film coated tablet contains:

Tadalafil                                      10 mg

Excipients                                    q.s.

Colour:  Titanium Dioxide BP

CHEMISTRY: Pyrazino [1’,2’:1,6] pyrido[3,4-b]indole-1,4-dione,6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-, (6R,12aR)

CATEGORY: Drug used in erectile dysfunction

PHARMACOLOGY

PHARMACODYNAMICS:

Tadalafil is a selective, reversible inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). When sexual stimulation causes the local release of nitric oxide, inhibition of PDE5 by Tadalafil produces increased levels of cGMP in the corpus cavernosum. This results in smooth muscle relaxation and inflow of blood into the penile tissues, thereby producing an erection. Tadalafil has no effect in the absence of sexual stimulation.

Tadalafil is a selective inhibitor of PDE5. PDE5 is an enzyme found in corpus cavernosum smooth muscle, vascular and visceral smooth muscle, skeletal muscle, platelets, kidney, lung and cerebellum. The effect of Tadalafil is more potent on PDE5 than on other phosphodiesterases. Tadalafil is >10,000-fold more potent for PDE5 than for PDE1, PDE2 and PDE4, enzymes which are found in the heart, brain, blood vessels, liver and other organs. Tadalafil is >10,000-fold more potent for PDE5 than for PDE3, an enzyme found in the heart and blood vessels. This selectivity for PDE5 over PDE3 is important because PDE3 is an enzyme involved in cardiac contractility. Additionally, Tadalafil is approximately 700-fold more potent for PDE5 than for PDE6, an enzyme which is found in the retina and is responsible for phototransduction. Tadalafil is also >10,000-fold more potent for PDE5 than for PDE7 through PDE10.

PHARMACOKINETICS:

Absorption:

Tadalafil is readily absorbed after oral administration and the mean maximum observed plasma concentration (C ) is achieved at a median time of max 2 hours after dosing. Absolute bioavailability of Tadalafil following oral dosing has not been determined. The rate and extent of absorption of Tadalafil are not influenced by food, thus Tadalafil may be taken with or without food. The time of dosing (morning versus evening) had no clinically relevant effects on the rate and extent of absorption.

Distribution:

The mean volume of distribution is approximately 63 liters, indicating that Tadalafil is distributed into tissues. At therapeutic concentrations, 94% of Tadalafil in plasma is bound to proteins. Protein binding is not affected by impaired renal function

Metabolism:

Tadalafil is predominantly metabolized by the cytochrome P450 (CYP) 3A4 isoform. The major circulating metabolite is the methylcatechol glucuronide. This metabolite is at least 13,000-fold less potent than Tadalafil for PDE5.

Elimination:

The mean oral clearance for Tadalafil is 2.5 l/h and the mean halflife is 17.5 hours in healthy subjects. Tadalafil is excreted predominantly as inactive metabolites, mainly in the faeces (approximately 61% of the dose) and to a lesser extent in the urine (approximately 36% of the dose).

 

INDICATIONS:

Tadalafil Tablets are indicated in the treatment of erectile dysfunction in adult males. In order for Tadalafil Tablets to be effective, sexual stimulation is required. Tadalafil Tablets are not indicated for use by women.

 

DOSAGE AND ADMINISTRATION:

Use in Adult Men: In general, the recommended dose is 10 mg taken prior to anticipated sexual activity with or without food. In those patients in whom Tadalafil Tablets 10 mg does not produce an adequate effect, 20 mg might be tried. It may be taken at least 30 minutes prior to sexual activity.

The maximum dose frequency is once per day. Tadalafil Tablets10mg and 20mg are intended for use prior to anticipate sexual activity and it is not recommended for continuous daily use.

In patients who anticipate a frequent use of Tadalafil Tablets (i.e., at least twice weekly) a once daily regimen with the lowest doses of Tadalafil Tablets might be considered suitable, based on patient choice and the physician's judgment.

In these patients, the recommended dose is 5 mg taken once a day at approximately the same time of day. The dose may be decreased to 2.5 mg once a day based on individual tolerability.

The appropriateness of continued use of the daily regimen should be reassessed periodically.

Use in Elderly Men: Dose adjustments are not required in elderly patients.

Use in Men with Impaired Renal Function: Dose adjustments are not required in patients with mild renal impairment. For men with moderate (creatinine clearance 31 to 50 ml/min) renal impairment a starting dose of 5 mg not more than once per day is recommended and the maximum dose should be limited to 10 mg not more than once in every 48 hours. For patients with severe renal impairment, 10 mg is the maximum recommended dose. Once-a-day dosing of Tadalafil Tablets are not recommended in patients with severe renal impairment.

Use in Men with Impaired Hepatic Function: The recommended doses of Tadalafil Tablets are 10 mg taken prior to anticipated sexual activity with or without food. There is limited clinical data on the safety of Tadalafil Tablets in patients with severe hepatic impairment; if prescribed, a careful individual benefit/risk evaluation should be undertaken by the prescribing physician. There are no available data about the administration of doses higher than 10 mg of Tadalafil to patients with hepatic impairment. Once-a-day dosing has not been evaluated in patients with hepatic impairment; therefore if prescribed, a careful individual benefit/risk evaluation should be undertaken by the prescribing physician.

Use in Men with Diabetes: Dose adjustments are not required in diabetic patients.

Paediatric population: Tadalafil Tablets should not be used in individuals below 18 years of age.

CONTRAINDICATIONS:

Hypersensitivity to the active substance or to any of the excipients. Tadalafil Tablets are contraindicated in patients who have loss of vision in one eye because of non-arteritic anterior ischemic optic neuropathy (NAION), regardless of whether this episode was in connection or not with previous PDE5 inhibitor exposure.

WARNINGS AND PRECAUTIONS:

A medical history and physical examination should be undertaken to diagnose erectile dysfunction and determine potential underlying causes, before pharmacological treatment is considered. Prior to initiating any treatment for erectile dysfunction, physicians should consider the cardiovascular status of their patients, since there is a degree of cardiac risk associated with sexual activity. Tadalafil has vasodilator properties, resulting in mild and transient decreases in blood pressure and as such potentiates the hypotensive effect of nitrates.

In patients receiving concomitant antihypertensive medicines, Tadalafil may induce a blood pressure decrease. When initiating daily treatment with Tadalafil, appropriate clinical considerations should be given to a possible dose adjustment of the antihypertensive therapy. Serious cardiovascular events, including myocardial infarction, sudden cardiac death, unstable angina pectoris, ventricular arrhythmia, stroke, transient ischemic attacks, chest pain, palpitations and tachycardia, have been reported either post-marketing and/or in clinical trials.

Most of the patients in whom these events have been reported had pre-existing cardiovascular risk factors. However, it is not possible to definitively determine whether these events are related directly to these risk factors, toTadalafil, to sexual activity, or to a combination of these or other factors.

Visual defects and cases of NAION have been reported in connection with the intake of Tadalafil and other PDE5 inhibitors. The patient should be advised that in case of sudden visual defect, he should stop taking Tadalafil and consult a physician immediately.

Due to increased Tadalafil exposure (AUC), limited clinical experience and the lack of ability to influence clearance by dialysis, once-a-day dosing of Tadalafil is not recommended in patients with severe renal impairment.

There is limited clinical data on the safety of single-dose administration of Tadalafil in patients with severe hepatic insufficiency. Once-a-day administration has not been evaluated in patients with hepatic insufficiency. If Tadalafil is prescribed, a careful individual benefit/risk evaluation should be undertaken by the prescribing physician.

Patients who experience erections lasting 4 hours or more should be instructed to seek immediate medical assistance. If priapism is not treated immediately, penile tissue damage and permanent loss of potency may result.

Agents for the treatment of erectile dysfunction, including Tadalafil, should be used with caution in patients with anatomical deformation of the penis (such as angulation, cavernosal fibrosis or Peyronie's disease) or in patients who have conditions which may predispose them to priapism (such as sickle cell

anaemia, multiple myeloma or leukemia).The evaluation of erectile dysfunction should include a determination of potential underlying causes and the identification of appropriate treatment, following an appropriate medical assessment. It is not known if Tadalafil is effective in patients who have undergone pelvic surgery or radical non-nerve sparing prostatectomy. In patients who are taking alpha1-blockers concomitant administration of Tadalafil may lead to symptomatic hypotension in some patient. The combination of Tadalafil and doxazosin is not recommended.

Caution should be exercised when prescribing Tadalafil to patients using potent CYP3A4 inhibitors (Ritonavir, Saquinavir, Ketoconazole, Itraconazole, and Erythromycin), as increased Tadalafil exposure (AUC) has been observed if the medicines are combined.

The safety and efficacy of combinations of Tadalafil and other PDE5 inhibitors or other treatments for erectile dysfunction have not been studied. The patients should be informed not to take Tadalafil with such combinations. Tadalafil contains lactose monohydrate. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product.

INTERACTIONS:

Effects of Other Substances on Tadalafil

Although specific max interactions have not been studied, other protease inhibitors, such as Saquinavir, and other CYP3A4 Inhibitors, such as Erythromycin, Clarithromycin, Itraconazole, and Grapefruit juice, should be co-administered with caution, as they would be expected to increase plasma concentrations of Tadalafil.

Effects of Tadalafil on Other Medicinal Products

Administration of Tadalafil to patients who are using any form of organic nitrate is contraindicated.

The co-administration of doxazosin (4 mg and 8 mg daily) and Tadalafil (5 mg daily dose and 20 mg as a single dose) increases the blood pressure-lowering effect of this alpha-blocker in a significant manner. This effect lasts at least twelve hours and may be symptomatic, including syncope. Therefore this combination is not recommended.

Tadalafil has been demonstrated to produce an increase in the oral bioavailability of Ethinyl estradiol; a similar increase may be expected with oral administration of Terbutaline, although the clinical consequence of this is uncertain.

Tadalafil (10 mg and 20 mg) did not potentiate the increase in bleeding time caused by acetylsalicylic acid. Specific interaction studies with anti-diabetic agents were not conducted.

PREGNANCY AND LACTATION:

Pregnancy

Tadalafil Tablets are not indicated for use by women. There are limited data from the use of Tadalafil in pregnant women. As a precautionary measure, it is preferable to avoid the use of Tadalafil during pregnancy.

Lactation

Tadalafil should not be used during breast feeding. Available pharmacodynamics/toxicological data in animals have shown excretion of Tadalafil in milk. A risk to the suckling child cannot be excluded.

 

Effect to Drive & Use the Machine:

No studies of the effect on the ability to drive and use machines have been performed. Patients should be aware of how they react to Tadalafil should not be used before driving or operating machinery.

 

ADVERSE DRUG REACTIONS:

The most commonly reported adverse reactions were headache and dyspepsia. The adverse reactions reported were transient and generally mild or moderate. Adverse reaction data are limited in patients over 75 years of age.

OVERDOSAGE:

Single doses of up to 500 mg have been given to healthy subjects and multiple daily doses up to 100 mg have been given to patients. Adverse events were similar to those seen at lower doses. In cases of overdose, standard supportive measures should be adopted, as required. Hemodialysis contributes negligibly to Tadalafil elimination.

PRESENTATION: Blister of 10 Tablets/Blister of 4 Tablets.

STORAGE: Store in a cool and dry place below 30o C. Protect from light.

Keep out of reach of Children.

 
OUR PRESENCE:
FIND US ON: