Original name: Tadalafil
International (nonproprietary) name: Tadalafil
Dosage form: film-coated tablets
Active ingredients: Tadalafil. Each tablet contains 20 mg tadalafil.
Excipients: lactose monohydrate, croscarmellose sodium, hydroxypropylcellulose, microcrystalline cellulose, sodium lauryl sulfate, magnesium stearate, a mixture of yellow dye Opadri II.
Pharmacotherapeutic group: a treatment for erectile dysfunction, PDE5 inhibitor.
Code ATX :G04BE08.
Tadalafil is an effective reversible selective inhibitor of phosphodiesterase type 5 (PDE5) which break down cyclic guanosine monophosphate (cGMP). When a sexual stimulation causes a local release of nitric oxide, the inhibition of PDE5 by tadalafil leads to increase of cGMP levels in the cavernous body of the penis. This results is relaxation of smooth muscles of arteries and increased blood flow to the tissues of the penis. Ultimately this causes erections. Tadalafil 20mg is ineffective without sexual excitement.
Studies in vitro have shown that tadalafil is a selective inhibitor of PDE5. PDE5 is an enzyme found in in the smooth muscle of the corpus cavernosum, smooth muscle of the internal organs, skeletal muscle, platelets, kidney, lung and cerebellum. Tadalafil is 10 000 times more selective for PDE5 than for FDE1, FDE2, FDE4 and FDE7, which are located in the heart, brain, blood vessels, liver, leukocytes, skeletal muscle and other organs. Original Tadalafil is 10 000 times more actively blocks PDE5 than PDE3 - an enzyme that is found in the heart tissue and blood vessels. This selectivity for PDE5 compared with PDE3 is important, because PDE3 an enzyme involved in contractility of the heart muscle. In addition, Tadalafil original about 700 times is more active against PDE5 than FDE6 discovered in the retina and is responsible for the vision.
Calis original improves erection and the possibility of successful sexual intercourse. The drug acts for a period 36 hours. The effect is manifested even after 16 minutes after taking the medication.
Tadalafil does not cause significant changes in systolic and diastolic blood pressure in healthy individuals compared with placebo. Tadalafil does not affect heart rate. Tadalafil does not cause changes in recognition colors (blue / green), due to its low affinity to PDE6. In addition, there were no observed any affects on the ECG, intraocular pressure and vision. Tadalafil does not change testosterone, luteinizing and follicle-stimulating hormone blood levels. Tadalafil does not have any affects on the sperm characteristics. .
After oral administration, Tadalafil 20mg is rapidly absorbed. An average maximum concentration (Vmax) in plasma is reached in 2 hours after and therefore, Tadalafil 20mg can be taken without regard to meals. Tada can be taken in the morning or evening without changes in the therapeutic activity.The pharmacokinetics of tadalafil in patients with erectile dysfunction is similar pharmacokinetics in patients without erectile dysfunction.
The average volume of distribution is about 63 liters, indicating that tadalafil is distributed in the tissues of the body. In therapeutic concentrations, 94% of tadalafil binds to plasma proteins. Protein binding is not altered in patients with impaired renal function. In healthy persons the amount of tadalafil in the sperm was less than 0.0005%.
Tadalafil is metabolized in the liver with the participation of cytochrome P450 isoenzyme CYP3A4. The main circulating metabolite is methylcatechol glucuronide. This metabolite, is13 000 times less active than tadalafil. Consequently, the concentration of this metabolite is not clinically significant.
In healthy individuals the average clearance of tadalafil ingestion of 2,5 l / h, and the average half-life - 17.5 hours. Tadalafil is excreted as inactive metabolites, mainly in the faeces (about 61% of the dose) and the urine (about 36% of the dose).
Healthy elderly (65 years and over) had a lower clearance of tadalafil when taken orally, which was reflected in the increase in area under the curve "concentration-time" by 25% compared with healthy people aged 19 to 45 years. This distinction is not clinically significant and does not require the correction of the Tadalafil original dose.
Patients with renal insufficiency
In people with renal insufficiency, including patients on hemodialysis, the area under the curve "concentration-time" was higher than in healthy individuals.
Patients with liver failure
The pharmacokinetics of tadalafil in patients with low and mederate hepatic insufficiency is comparable to that in healthy individuals. For patients with severe hepatic impairment (according to the classification of Child-Pugh Class C) data are not available.
Patients suffering from diabetes
Patients with diabetes the area under the curve "concentration-time" was less on 19% than in healthy individuals. This difference does not require the dose correction
Tadalafil original indications
The medication is used for the treatment of erectile dysfunction in men over 18 years of age. Erectile dysfunction is usually classified as inability to achieve and maintain erection sufficient for the sexual intercourse.
Tadalafil is contraindicated in the following health conditions:
- Known hypersensitivity to any compounds of the preparation
- Patients taking organic nitrates and nitrogen oxide donors (like nitroglycerin)
- Patients under 18 years of age
- Severe blood diseases
- Severe liver of kidney diseases
Since there is no data on patients with severe hepatic insufficiency (according to the classification of Child-Pugh Class C), Tadalafil should be used with caution in this group of patients. Tadalafil original should be taken with caution in patients which take alpha-blockers such as doxazosin (simultaneous use may result in symptomatic hypotension)
Sexual activity is a potential risk for patients with cardiovascular diseases. Therefore, treatment of erectile dysfunction, including the use of Tadalafil brand, should not be undertaken in men with heart diseases, in which sexual activity is not recommended. Keep in mind the potential risk of complications during the sexual activity in patients with the following cardiovascular diseases:
- Myocardial infarction
- Unstable angina or angina occurring during sexual intercourse
- Heart failure class
- Uncontrolled cardiac arrhythmia,
- Hypotension (blood pressure of <90/50 mm Hg. Art.)
- Uncontrolled hypertension
Tadalafil 20mg should be used with caution in patients with predisposition to priapism (eg sickle-cell anemia, multiple myeloma, leukemia FPI) or patients with anatomical deformation of the penis (eg, angular distortion, cavernous fibrosis or Peyronie's disease). Some clinical data report the possible occurrence of priapism in patients using PDE5 inhibitors, including tadalafil. Patients should necessarily inform their health care providers if the erection lasts more than 4 hours. Uncontrolled priapism may lead to tissue damage of the penis, resulting in a long-term potency.
Safety and effectiveness of the combination of Tadalafil 20mg original with other erectile dysfunction preparations were not studied. Therefore, the use of such combinations is not recommended.
As with other PDE5 inhibitors, tadalafil has a systemic vasodilating properties, which can lead to a transient decrease in blood pressure. Before the application of Tadalafil brand, physicians should carefully weigh the risk of possible Tadalafil 20mg side effects.
Application of Tadalafil during pregnancy and lactation
Tadalafil is not intended for use in women.
Tadalafil Dosing and Administration
For oral administration the recommended maximum dose of Tadalafil is 20 mg. Tadalafil should be taken before anticipated sexual activity, regardless of meal. Drug should take at least 16 minutes prior to the sexual intercourse. Patients may have the following sexual intercourses for a period of 36 hours after beginning the application. The maximum recommended frequency of admission - once a day.
Tadalafil brand Side effects
The most frequently reported Tadalafil side effects were headache and dyspepsia (11 and 7% of cases, respectively). Side effects associated with taking tadalafil were generally unsignificant and didn't require the cessation of therapy.
Other common Tadalafil side effects included back pain, myalgia, nasal congestion and hot flashes.
In very rare cases Tadalafil brand side effects included: swelling of the eyelids, eye pain, hyperemia of the conjunctiva and dizziness.
In very rare cases Tadalafil side effects included hypersensitivity reactions (including rash, urticaria and swelling of the face, Stevens-Johnson syndrome and exfoliative dermatitis), hypotension (in patients who have already received antihypertensive agents); hypertension and syncope, abdominal pain and gastroesophageal reflux, hyperhydrosis (increased sweating), and the delay erection - priapism, blurred vision, anterior ischemic optic neuropathy, retinal vein occlusion;
Myocardial infarction, cardiogenic sudden death, stroke, chest pain, palpitations and tachycardia were observed in patients who previously had cardiovascular risk factors. However, it is rather difficult to determine whether these complication have any casual relationship with Tadalafil brand.
Tadalafil 20mg overdose
Patients taking Tadalafil original 500mg experienced the same side effects with those observed in healthy patients. However the rate of the side effects was significantly high. In case of overdose it is necessary to perform symptomatic treatment.
Tadalafil drug interaction
Tadalafil is mainly metabolized with the participation of the enzyme CYP3A4. A selective inhibitor of CYP3A4, ketoconazole (400 mg / day) increases the activity of the Tadalafil 20mg brand single dose (AUC) on 312% and 22% Cmax and ketoconazole (200 mg / day) increases the activity of the Tadalafil 20mg brand single dose (AUC) on 107% and Cmax at 15% compared with AUC.
Ritonavir (200 mg twice a day), an inhibitor of CYP3A4, 2C9, 2S1E and 2D6, increases the activity of the tadalafil brand single dose (AUC) on 24% without changing Cmax. Despite the fact that the specific interactions have not been studied, we can assume that other HIV protease inhibitors such as saquinavir, as well as SURZA4 inhibitors such as erythromycin and intraconazol, increase the activity of tadalafil.
Selective inducer of CYP3A4, rifampin (rifampicin, 600 mg / day), reduces the activity of the Tadalafil brand single dose (AUC) on 88% and 46% of Cmax. We can assume that the simultaneous administration of other inducers of CYP3A4 should also reduce the concentration of tadalafil in plasma.
Simultaneous treatment with an antacid (magnesium hydroxide / aluminum hydroxide) and tadalafil reduce the rate of absorption of tadalafil without altering the area under the pharmacokinetic curve of Tadalafil brand.
Effect of Tadalafil on other drugs
Tadalafil significantly enhances the hypotensive effect of nitrates. This is a result of the additive action of nitrates and tadalafil on the metabolism of nitric oxide and cGMP. Therefore, use of tadalafil on nitrates is strictly contraindicated.
Tadalafil has no clinically significant effect on clearance of drug metabolism that takes place with the participation of enzyme cytochrome P450. Studies have confirmed that tadalafil does not inhibit or induce isozymes CYP1A2, CYP3A4, CYP2C9, CYP2C19, CYP2D6, CYP2E1.
Tadalafil has no clinically significant effect on the pharmacokinetics of 5-warfarin or R-warfarin.
Tadalafil 20mg brand does not increase the duration of bleeding caused by acetylsalicylic acid.
Additionally, patients taking multiple antihypertensive agents, in which hypertension poorly controlled, observed several large reduction in blood pressure.. Patients treated with antihypertensive drugs and receiving tadalafil, should be given appropriate clinical care.
There were not observed a significant reduction in blood pressure, when using Tadalafil original with alpha-blocker and tamsulosin.
In the simultaneous application of tadalafil and doxazosin (8 mg / day) an alpha-blocker there were observed dizziness in healthy patients. Lower doses of doxazosin were not studying. Tadalafil did not affect the concentration of alcohol, as well as alcohol does not affect the concentration of tadalafil. At high doses of alcohol (0.7 g / kg), receiving tadalafil caused no statistically significant reduction in average blood pressure. Some patients experienced postural dizziness and orthostatic hypotension.
Tadalafil has no clinically significant effect on the pharmacokinetics or pharmacodynamics of theophylline.
Store at temperature below 30 ° C in the original packaging. Keep out of reach of children.
Tadalafil shelf life
3 years. Do not use later than the date specified on the package.
The most common Tadalafil brand questions
How long does Tadalafil work?
Tadalafil brand usually works for a period of 36 hours. It does not mean that you will have an erection for 36 means. It means that you can have 2 or 3 and even more erection during this period. More than 67% of patients Tadalafil had a strong erection enough for the sexual intercourse. Tadalafil is more effective than Tadalafil 10mg h(only 56% of successful sexual intercourse)
What is herbal Tadalafil?
Herbal Tadalafilis usually related to certain herbal compounds that work by increasing the blood flow to the penis. The effectiveness of these medications was not studied. They are not working like other PDE5 inhibitors.
Can Tadalafil original cause blindness?
In more than 2% of patients Tadalafil brand may cause the following vision side effects:
- See a blue tinge to objects
- Blurred vision
- Hard recognition the difference between blue and green
- Pain in the eyes
Can I become addicted to Tadalafil 20mg?
Clinical studies showed that brand Tadalafil does not cause the addiction. Tadalafil 20mg tablets is not a habit-forming preparation.
Where can I buy Tadalafil?
You can buy Tadalafil at our online drugstore. We offer reasonable and affordable prices and original medication from the manufacture.
How can I buy Tadalafil?
You can Tadalafil tablets made by Eli Lilly using your Visa or Visa Electron Card