Product Name: Tadacip
Common Brand Names: Cialis
Pharmaceutical Category: Men's Health
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There is an additional general information about this medication active ingredient tadalafil:
Tadacip is a medication for the treatment of erectile dysfunction. This drug is a selective inhibitor of PDE5-specific cGMP. When sexual stimulation causes local release of nitric oxide, inhibition of PDE5 tadalafil leads to increased levels of cGMP in the cavernous body of penis. The result is relaxation of smooth muscles of arteries and blood flow to the tissues of the penis, causing erection. Tadalafil is ineffective in the absence of sexual stimulation.
Studies in vitro have shown that tadalafil is a selective inhibitor of PDE5. PDE5 is an enzyme found in smooth muscles of cavernous bodies in vascular smooth muscle of the internal organs, skeletal muscle, platelets, kidney, lung cerebellum.
Effect of tadalafil on PDE5 is more active than other phosphodiesterase. Tadalafil in 10,000 times more potent for PDE5 than for FDE1, FDE2, PDE4, which are located in the heart, brain, blood vessels, liver and other organs. This medication in 10,000 times more active blocks PDE5 than FDE3 - an enzyme that is found in the heart and blood vessels. This selectivity for PDE5 compared with FDE3 is important because FDE3 is an enzyme participating in the reduction of the heart muscle. In addition, tadalafil is about 700 times more potent for PDE5 than for FDE6, found in the retina and is responsible for photo transfer.
Tadacip acts within 36 hours. The effect is already apparent 16 minutes after ingestion in the presence of sexual arousal.
Tadalafil in healthy individuals does not cause significant changes in systolic and diastolic blood pressure compared with placebo in the prone position (mean maximum decrease of 1.6/0.8 mm Hg, respectively) and standing (mean maximum decrease of 0.2/4.6 mm Hg, respectively). Tadalafil does not cause significant changes in heart rate.
This medicine does not cause changes in the recognition of colors (blue / green), due to its low affinity for PDE6. In addition, no marked effect of tadalafil on visual acuity, electroretinogram, intraocular pressure and pupil size.
Clinically significant effect on the characteristics of sperm in men taking Tadacip in daily doses for 6 months has not been identified.
After oral administration Tadacip is rapidly absorbed. Cmax achieved in average of 2 hours. The rate and extent of absorption do not depend on the meal. The pharmacokinetics of tadalafil in healthy individuals is linear with respect to time and dose. At doses ranging from 2.5 to 20 mg AUC it increases proportionally to dose. Css in plasma are attained within 5 days while taking the drug 1 time / day.
The pharmacokinetics of this medication in patients with impaired erectile function is similar to the pharmacokinetics in individuals without erection dysfunction.
Vd is about 63 liters, indicating that tadalafil is distributed into body tissues. At therapeutic concentrations, 94% of tadalafil bound to plasma proteins. In healthy persons less than 0.0005% of the dose found in the semen.
This medicine metabolized with the participation of isoenzyme CYP3A4.
The main circulating metabolite is methylcatechol glucuronide, which is 13,000 times less potent for PDE5 than tadalafil, so unlikely that this metabolite is clinically significant.
In healthy individuals the average clearance of tadalafil ingestion of 2.5 l / h, and the median T1/2 is 17.5 hours. Tadalafil appears mainly as inactive metabolites mainly in the faeces (61%) and to a lesser extent in the urine (about 36%).
In patients with mild renal insufficiency (creatinine clearance from 51 to 80 ml / min) or moderate (creatinine clearance of 31 to 50 ml / min) AUC is more than in healthy individuals.
Why is Tadacip prescribed?
Dosage and administration
Middle-aged men are prescribed to take Tadacip in dose of 20 mg at least 16 minutes prior to anticipated sexual activity, regardless of the meal. Patients may attempt to carry out sexual intercourse at any time within 36 hours after admission in order to establish the optimal response time to receive this medication.
The maximum frequency of admission is 1 time / day.
Tadacip side effects, adverse reactions
The most frequently: headache, indigestion.
Perhaps: back pain, myalgia, nasal congestion, flushing.
Rarely: edema of the eyelids, eye pain, conjunctival hyperemia, dizziness.
Simultaneous administration of drugs containing any organic nitrates, childhood and adolescence to 18 years; hypersensitivity to tadalafil.
With extreme caution and only when absolutely necessary, you can use Tadacip in patients with severe renal insufficiency (creatinine clearance less than 30 mL / min) and severe hepatic impairment.
The treatment with Tadacip in patients with moderately renal insufficiency (QC from 31 to 50 ml / min) were more common back pain compared to patients with mild renal insufficiency (creatinine clearance from 51 to 80 ml / min) or healthy volunteers. In patients with CC less than 50 mL / min this drug should be used with caution. Therefore, a treatment of erectile dysfunction (including with this medication) there should not been in men with heart disease, in whom sexual activity is not recommended.
Keep in mind the potential risk of complications in sexual activity in patients with cardio-vascular system: myocardial infarction within the last 90 days; unstable angina or angina occurring during sexual intercourse; chronic heart failure (II functional class and higher classification of NYHA), which developed over the last 6 months; uncontrolled cardiac arrhythmia; arterial hypotension (BP less than 90/50 mm Hg) or uncontrolled hypertension; stroke in the last 6 months.
Use Tadacip with precautions in patients with predisposition to priapism (eg sickle cell anemia, multiple myeloma or leukemia) or patients with anatomical deformation of the penis (such as angulation, cavernous fibrosis or Peyronie's disease).
A patient should be informed of the need for immediate treatment to the doctor in the event of an erection, lasting 4 hours or more. Delays in treatment for priapism causes damage to penile tissue, as a result can occur long-term loss of potency.
Whilre taking tadalafil there were no reported about cases of priapism.
It not recommended to use this medicine in combination with other drugs for erectile dysfunction.
Tadacip drug interactions
Tadalafil is mainly metabolized with the participation of the enzyme CYP3A4. A selective inhibitor of CYP3A4 ketoconazole increases AUC by 107%, and rifampicin reduces it by 88%.
Despite the fact that the specific interactions were not investigated, in can be suggested that protease inhibitors such as ritonavir and saquinavir, as well as inhibitors of CYP3A4, such as erythromycin and itraconazole increase the activity of Tadacip.
At the same time taking an antacid (magnesium hydroxide / aluminum hydroxide) and tadalafil the rate of absorption of the latter reduces without changing the AUC.
This medication enhances the hypotensive effect of nitrates. This is due to additive effect of nitrates and tadalafil on the metabolism of nitric oxide and cGMP. Therefore, using of Tadacip in patients treated with nitrates is contraindicated.
Tadacip in case of emergency / overdose
Symptoms: a prescription for healthy volunteers of single doses of 500 mg and patients with erectile dysfunction multiple doses up to 1000 mg adverse effects were the same as receiving lower doses.
Treatment: standard supportive care. Hemodialysis contributes little to elimination of tadalafil.