Vitalis (Tadalafil)

Vitalis (Tadalafil)

Vitalis (Tadalafil)

Vitalis (Tadalafil)

$55.00

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$55.00

Vitalis (Tadalafil)

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Description

Minister of Health of the Republic of Moldova
Directions for use

VITALIS 5 mg/dose
Oral spray, suspension

Registration Certificate
Moldova
COMMERCIAL NAME
Vitalis 5 mg/dose

ICN ACTIVE INGREDIENTS

Tadalafilum
COMPOSITION

   Active ingredient: tadalafilum 5 mg/dose

   Other ingredients: Glycerol, macrogol 400, xanthan gum, benzoic acid, acesulfate potassium, polysorbate 80, flavor orange, vanillin, potassium sorbate, saccharin sodium, purifiend wather.
PHARMACEUTICAL FORM

Oral spray, suspension

Product description

White suspension with specific smell and taste of orange and vanilla, homogeneous after strirring.
Pharmacotherapeutic group and ATC code

Drugs used in erectile dysfunction, G04BE08
Pharmacological properties

Pharmacodynamic  properties

Tadalafil is a selective inhibitor, reversible to phosphodiesterase type 5 (PDE5), specific to cyclic guanosine monophosphate (cGMP). When the sexual stimulation causes local release of nitric oxide, inhibitor of PDE5 by tadalafil produces increased levels of cGMP in the corpus cavernosum , resulting 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.

Pharmacokinetic properties
   Absorbation

Tadalafil is readily absorbed after oral administration and the mean maximum observed plasma concentration (Cmax ) is achieved at a median time of 10 minutes after administration. Absolute bioavailability of tadalafil following oral dosing has not been determined. The rate and extent of absorption of tadalafil are not influenced by food , so that preparation can be with or without food . Time of dosing (morning or evening ) had co clinically relevant effects on the rate and extend of absorption.

   Dristribution

At therapeutic concentration 94% of the tadalafil in plasma is bound to protein. Protein binding is not affected by renal dysfunction . Less than 0.0005% of the administered dose appears in the semen of healthy subjects .
   Biotransformation

Tadalafil is predominantly metabolized by cytochrome P450 (CYP) 3A4 isoenzyme . The major circulating metabolite is the methylcatechol glucoronide . This metabolite is at least 13,000 times less than tadalafil for PDE5. Consequently , it is not expented to be clinically active at observed metabolite concentrations.

   Elimination

The mean oral clearance for tadalafil is 2.5 l/h and the mean terminal half-life is 17.5 hours in healthy subjects. Tadalafil is excreted predominantly as inactive metabolites .

   Linearity/not – linearity

Tadalafil pharmacokinetics in healthy subjects are linear with respect to time and dose. Over a dose range from 5 mg to 20 mg , exposure(AUC) increases proportionally with dose. Steady state plasma concentrations are attained within 5 days of oncedaily administration. Pharmacokinetics determined with a population approach in patients with erectile dysfunction  are similar to the pharmacokinetics in subjects without erectile dysfunction.

Therapeutic Indications

Treatment of erectile dysfunction in adult males . For tadalafil to be effective, sexual stimulation is required .
DOSAGE AND METHOD OF ADMINISTRATION

Shake the bottle before use. Before  the first use, press few times the spray device until the appearance of a dispersed flow. Administer spray sublingual or on lingual surface and mentain it in the oral cavity till the full absorbtion.

Use of adult men

Generally, the recommended dose is 10 mg, that is 2 sprayings (5 mg/spraying),taken prior to anticipated sexual activity with or without food. To the patients  , to whom tadalafil 10 mg did not produce an adequate effect , 20 mg/4 sprayings might be tried. The drug can be administered at least 10 minutes before sexual activity . The maximum recommended dosing frequency is once per day and not more then  20 mg. Tadalafil 10 and 20 mg is intended for use prior to anticipated sexual activity and is not recommended for continuous daily use. To patients , whom Tadalafil is prescribed by the doctor for a continuous daily administration, the recommended dose is 5 mg per dey approximately at the same time of the day. Opportunity of continuous daily regimen should be reassessed  periodically .

Use for elderly men
Dosage adjustments are not required in elderly patients .

 

Use in men with impaired renal function

No dosage adjustment is necessary for patients with mild to moderate impired renal function . For patients with severe renal impairment  the maximum recommended dose in 10 mg. Daily dosing of tadalafil is not recommended in patients with severe renal impairment .

Use in men with impaired hepatic function

Vitalis recommended dose of 5 mg/dose is 10 mg taken with or without food, prior to anticipated sexual activity. There are limited clinical data on the safety of Tadalafil in patients with severe hepatic impairment (Child- Pugh Class C), if prescribed, the doctor will need to make a careful individual assessment of the benefit / risk ratio. No information on doses higher than 10 mg of Tadalafil in patients with hepatic impairment.

The use of men with diabetes mellitus

In diabetic patients dosage adjustments are not necessary.

Children and adolescents

Vitalis should not be used by person under the age of 18.

SIDE EFFECTS

Adverse reactions are ranked by frequency, using MedDRA frequency convention:

Very common (>1/10)

Common (>1/100 and <1/10)

Uncommon (>1/1000, <1/100)

Rare (>1/10000, <1/1000)

Very rare (<1/10000)

Unknown (can not be estimated from available data).

Immune system disorders

Uncommon: hypersensitivity reactions

Rare: angioedema

Nervous System Disorders

Common: headache

Uncommon: dizziness

Rare: stroke, syncope, transient ischemic attacks, migraine, seizures, transient amnesia

Eye disorders

Uncommon: blurred vision, sensations described as eye pain

Rare: visual field defect, eyelid edema, conjunctival hyperemia, anterior ischemic optic meuropathy, non – arteritic (NAION), retinal vascular occulusion

Ear and labyrinth disorders

Uncommon: tinnitus

Rare: Sudden deafness

Cardiac disorders

Uncommon: tachycardia, palpitations

Rare: myocardial infarction, unstable angina, ventricular arrhythmia

Vascular disorders

Common: flushing

Uncommon: hypertension

Respiratory, thoracic and mediastinal disorders

Common: nasal congestion

Uncommon: dyspnea, epistaxis

Gastrointestinal disorders

Common: dyspepsia, gastro-oesophageal reflux

Uncommon: abdominal pain

Skin and subcutaneous tissue disorders

Uncommon: rash, hyperhidrosis (sweating)

Rare: urticarial, Stevens – Johnson syndrome, exfoliative dermatis

Musculoskeletal and connective tissue disorders

Common: back pain, myalgia, pain in extremity

Renal and urinary disorders

Uncommon: hematuria

Reproductive system and breast disorders

Uncommon: bleeding from the penis, hematospermia

Rare: prolonged erection, priapism

General disorders and administration site

Uncommon: chest pain

Rare: facial swelling, sudden cardiac death

CONTRAINDICATIONS

Not be used in men cardiac disease for whom sexual activity is inadvisable. Physicians should consider the potential cardiac risk of sexual activity in patients with pre-existing cardiovascular disease.

The following groups of patients with cardiovascular disease have not been included in clinical trials, and therefore the use of tadalafil is contraindicated in patients with:

·         Myocardial infarction within the last 90 days.

·         Unstable angina or angina occurring during sexual intercourse.

·         Class 2 heart failure New York Heart Association (NYHA) or greater, failure in the last 6 month

·         Uncontrolled arrhythmias, hypotension (<90/50 mmHg) or uncontrolled hypertension

·         A stroke within the last 6 months

Tadalafil is contraindicated in patients who have loss of vision due to anterior ischemic optic neuropathy, non – arteritic (NAION), even though this episode was in connection or not with previous PDE5 inhibitor exposure.

Overdose

Symptoms: Adverse reactions were similar to those seen at lower doses.

Treatment: In case of overdose, be taken, as needed, standard supportive measures.

WARNING AND SPECIAL PREAUTIONS FOE USE

Before initialing any treatment for erectile dysfunction, physicians should consider the cardiovascular status of patients, because the sexual activity is associated with degree of cardiac risk.

Tadalafil has vasodilator proprieties, resulting in mild and transient decreases in blood pressure and thus potentiate the hypotensive effects of nitrates.

It is not known if the preparation is effective in patients who have had surgery within the pelvic region or the radical prostatectomy without nerve preservation erection.

In some of the patients using concomitant alpha 1 blockers Vitalis 5 mg / dose can cause symptomatic hypotension. The combination of tadalafil and doxazosin is not recommended. Vitalis 5 mg / dose should be used caution in patients with:

·         Anatomical deformation of the penis (such as angulation, cavernosal fibrosis or Peyronie’s diseas) or in patients with conditions that predispose them to priapism (such as sickle cell anemia, multiple myeloma or leukemia).

·         Using potent CYP3A4 inhibitors (ritonavir, saquinavir, ketoconazole, itraconazole, and erythromycin) as increased tadalafil exposure (AUC) for these drug combinations.

Use in pregnancy lactation

It is not indicated for use by women.

 

Influence on ability to drive and use machines.

Preparation effect on ability to drive and use machines is considered negligible. Although the frequency of reports of dizziness in tadalafil and placebo – treated groups in clinical trials was similar, before driving or operating machinery patients should know they react to Vitalis 5 mg/dose.

Effects of tadalafil on other drugs

Nitrate

In clinical studies, tadalafil (5 mg, 10 mg and 20 mg) was shown to augment the hypotensive effects. Therefore Vitalis administration in patients who are using any form of organic nitrate is contraindicated. In such circumstances, nitrates should only be administered under close medical supervision with apropiate hemodynamic monitoring.

Antihypertensive drugs (including calcium channel blockers)

Concomitant administration of doxazosin ( 4 and 8 mg daily) and tadalafil ( 5 mg daily dose and 20 mg single dose) significantly increase the hypotensive effect of this alpha – blocker. This effect lasts at least twelve hours and may symptomatic, including syncope. Therefore, such use is not recommended. In interaction studies to a limited number of healthy volunteers, these effects were not relative to administration of alfuzosin or tamsulosin. However, caution is needed when using tadalafil to patients who are taking any alpha –blocker therapy, and especially to the elder ones. Treatment should be initiated at the lowest dose and gradually adjusted.

Inhibitors of 5.allpha.-reductase

However, because it wasn’t conducted a formal drug-drug interaction to assess the effects of administration tadalafil with 5 alpha- reductase inhibitors (5-IAR) caution is needed in concomitant administration of tadalafil with 5 – IAR.

Substrates of CYP1A2 ( for example, theophylline )

When tadalafil 10 mg was administered with theophylline (non-selective phosphodiesterase inhibitor) in a clinical pharmacology study, there was no pharmacokinetic interaction manifested. The only pharmacodynamics effect was a small increase in heart rate ( 3.5 bpm). Although this effect is minor and had no clinical significance in this study, it should be considered when administering these drugs concomitantly.

Ethinykestradiol and terbutaline

Tadalafil has been desomnstrated to produce an increase in the oral bioavailability of ethinylestradiol; asimilar increase may be expected with oral administration of terbutaline, although the clinical consequence of this is uncertain.

Ethyl alcohol

Alcohol concentrations ( mean maximum blood alcohol levels of 0.08% ) were not affected by concomitant administration of tadalafil ( 10 mg or 20 mg ). In addition, no changes were found in tadalafil concentrations 3 hours after co-administration of alcohol. Effects of alcohol on cognitive function was not increased by tadalafil ( 10 mg ).

Drugs methabolized by cytochrome P450

Tadalafil os not expected to cause clinically significant inhibition or induction of the clearance of drugs metabolized by CYP450 isoenzymes. Studies have confirmed that tadalafil does not inhibit or induce CYP450 isoenzymes, including  CYP3A4, CYP1A2, CYP2D6, CYYP2E1, CYP2C9 and CYP2C19.                                                        CYP2C9 substrates ( e.g., R – warfarin )

Tadalafil ( 10 mg and 20 mg ) had no clinically significant effect on exposure (AUC) to S – warfarin or    R – warfarin ( CYP2C9 substrate ) and did not affect changes in prothrombin time induced by warfarin.

Acetylsalicylic Acid

Tadalafil ( 10 mg and 20 mg ) did not potentiate the increase of bleeding time caused by acetylic acid.

Antidiabetic

No specific interaction studies with andiabetic drugs.

Appearance, packaging

Oral spray suspension, 5 mg/dose, 12 ml/48 doses in vial. 1 vial together with instructions for administration in cadboard box.

STORAGE

Store below 25°C.

Store in original package to protect from light and moisture.

Keep out of reach and sight of children!

SHELF LIFE

3 years.

Do not use after the expiry data shown on the pack.

LEGAL STATUS

With prescription.

Date of last revision of text March 2014.

NAME AND ADRESS

“Flumed – Farm” Ltd

Republic of Moldova

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