Vuvuzela

Description

Vuvuzela (Tadalafil) is a selective, potent, reversible inhibitor of Cyclic Guanosine Monophosphate (GMPc) -specific phosphodiesterase type 5 (PDE5), used for the treatment of erectile dysfunction. Inhibition of PDE5 causes an increase in cGMP levels in the corpora cavernosa and in the smooth muscle of the prostate, bladder and its vascular contributions. Vascular relaxation results in increased blood perfusion and can reduce symptoms of benign prostatic hypertrophy. Relaxation of the stroma of the smooth muscle of the prostate can complement said vascular effects, with which a relaxation of the smooth muscle is obtained, thus allowing the influx of blood, producing an erection. The erection disappears after sexual intercourse. You cannot get an erection just by taking Tadalafil, the drug works with sexual stimulation.

Absorption

Vuvuzela (Tadalafil) is rapidly absorbed orally, produces a rapid effect (from 16 minutes), the mean plasma concentration (Cmax) is reached in an average time of 2 hours after dosing, lasting 36 hours. Neither the speed nor the degree of absorption of Tadalafil is influenced by food intake, so it can be taken with or without food.

Distribution

Tadalafil is widely distributed in tissues and 94% is bound to plasma proteins and this binding is not affected by impaired renal function.

Metabolism

Tadalafil is mainly metabolized by the 3A4 isoform of cytochrome P-450 (CYP), the main circulating metabolite is methylcatechol glucuronide.

Elimination

The average clearance of Tadalafil is 2.5 liters and its half-life is 17.5 hours in healthy individuals, it is excreted predominantly as inactive metabolites.

Indications

Vuvuzela is indicated in the treatment of erectile dysfunction and impotence; as well as in the treatment of low urinary symptoms associated with benign prostatic hypertrophy in patients with or without erectile dysfunction.

Posology

 

Adults: the recommended dose is 10mg taken before sexual activity regardless of meals. If the 10mg dose does not produce an adequate effect, 20mg can be administered. It can be taken from 30 minutes to 12 hours before sexual activity. The effect of Vuvuzela can last up to 36 hours after administration. The maximum recommended dose is 20mg once a day. For those patients who have responded to demand and who foresee frequent use of Tadalafil, that is, twice a week, daily use of lower doses may be appropriate, taking into account both the patient’s choice and the physician’s clinical judgment. In these patients the recommended dose is 5mg once a day, at approximately the same time. The dose can be reduced to 2.5mg once a day, depending on the tolerability of the patient. The suitability of continued use of this daily administration regimen should be periodically reevaluated.

Treatment of low urinary symptoms associated with benign prostatic hypertrophy in patients with or without erectile dysfunction: The recommended dose of Vuvuzela is 5mg once a day, administered at approximately the same time of day.

Children and adolescents: Vuvuzela is not indicated in people under 18 years of age, its efficacy and safety in them have not been established. No dosage adjustment is required in elderly patients, in patients with mild to moderate hepatic impairment, in diabetic patients, or in patients with mild renal impairment.


Side effects

 

The most common adverse effects associated with the use of Tadalafil are: back pain, muscle pain, redness, congestion or runny nose. They generally disappear after 48 hours. Cardiovascular events, including myocardial infarction, sudden death, cerebral vascular event, chest pain, palpitations and tachycardia, have been reported in temporal association with the use of Tadalafil. Most of the patients had pre-existing cardiovascular risk factors.

Gastrointestinal: Abdominal pain and gastroesophageal reflux.

Skin and subcutaneous tissue: Hyperhidrosis (sweating).

Urogenital: Priapism and prolonged erection.

Nervous System: Migraine.

Respiratory system: Epistaxis.

Special Senses: Blurred vision, retinal vein occlusion, visual field defect.

Drug interactions

Tadalafil is metabolized by CYP3A4 isoenzymes of cytochrome P450 and therefore, can cause interactions with drugs that inhibit or induce or are metabolized by this enzyme system, such as: Ketoconazole, rifampicin, phenobarbital, phenytoin and carbamazepine, which can reduce the efficacy and plasma concentration of Tadalafil.

Although specific interactions have not been studied, some protease inhibitors such as ritonavir and saquinavir and other cytochrome CYP3A4 inhibitors such as erythromycin, clarithromycin, or itraconazole should be administered with caution as plasma concentrations of Tadalafil may be increased.

Tadalafil causes an increase in the hypotensive effect of nitrates. There are no clinically significant interactions of Tadalafil with first-line antihypertensive drugs. Decreased blood pressure, which is generally small and probably without clinical relevance, has been observed with some antihypertensive drugs. However, patients should be appropriately informed of the possible decrease in blood pressure when receiving treatment with antihypertensive medication, especially in the case of alpha-blockers (prazosin, doxazosin).

Cautions

The concomitant use of Vuvuzela with alpha adrenergic blockers can produce a significant decrease in blood pressure that can determine symptomatic hypotension (for example, fainting).

In patients with severe renal failure or end-stage renal disease, the dose of Vuvuzela should be limited to 5mg no more than 1 time per day and in patients with severe liver failure, its use is not recommended.

The use of Vuvuzela is not recommended in patients who have not passed 90 days after suffering an acute myocardial infarction, in patients with unstable angina or those in whom angina occurs during sexual intercourse, in patients with uncontrolled arrhythmia, hypotension or patients who suffered a stroke in the last 6 months. The use of Vuvuzela is also not recommended in patients with inherited degenerative disorders of the retina, including retinitis pigmentosa.

Composition

Vuvuzela 5:

Each coated tablet contains:

Tadalafil     5mg

C.S.P. excipients     1 coated tablet

Vuvuzela 10:

Each coated tablet contains:

Tadalafil     10mg

C.S.P. excipients     1 coated tablet

Vuvuzela 20:

Each coated tablet contains:

Tadalafil     20mg

C.S.P. excipients     1 coated tablet


Administration route

Oral


Presentation

Vuvuzela 5: Box containing 25 blisters with one 5mg coated tablet.

Vuvuzela 10: Box containing 25 blisters with one 10mg coated tablet.

Vuvuzela 20: Box containing 25 blisters with one 20mg coated tablet.


Storage

Keep in a dry place at a temperature below 30 °C.


Contraindications

Vuvuzela is contraindicated in patients suffering from serious liver or kidney problems, in patients taking medications containing nitrates; since, the joint use of Tadalafil together with nitrates can cause sudden drops in blood pressure, resulting in critical complications, in patients with heart problems or chest pain or who suffer from high or low blood pressure.

Vuvuzela (Tadalafil) should not be administered to patients with hypersensitivity to Tadalafil and in patients with Ischemic Optic Neuropathy. Its use in women is not recommended.


Warnings

Sale by prescription, keep out of the reach of children.