⚠Discount 10%. ✌
Cialis tablets contain 5 mg of tadalafilum, lactose (in the form of monohydrate) and spray dried lactose monohydrate, giprolose and extra thin giprolose, sodium lauryl sulfate, Mcc, croscarmellose Na, plant stearate Mg.
the composition of the p / o: Opadry yellow (hypromellose, triacetin, ti dioxide, lactose monohydrate, dye E172 (yellow)).
Form of issue
Tablets in p / o.5 mg. Packing No. 14 and No. 28.
the tablets are almond-shaped, covered with a light yellow film membrane. On one side is engraved “c 5”.
Improves erectile function.
Pharmacodynamics and pharmacokinetics What is Cialis?
Cialis (tadalafilum) is a drug that reversibly and selectively suppresses specific PDE-5 cGMP (cyclic guanosine monophosphate).
Wikipedia says that the drug is designed to treat disorders in which a man is not able to achieve and maintain the necessary erection for sexual intercourse.
With sexual excitement, local release of nitric oxide occurs, and due to the suppression of PDE-5, the concentration of cyclic guanosine monophosphate in the cavernous body of the penis increases.
As a result, the smooth muscles of the arteries relax, the blood flow to the tissues of the penis increases and an erection occurs. In the absence of sexual arousal, there is no such effect.
Elevated concentrations of cGMP are also observed in the smooth muscles of the bladder, the prostate and supplying them with blood vessels.
Relaxation of the musculature of the vessels promotes an increase in perfusion (passage) of blood in these organs and a reduction in the manifestation of BPH symptoms, and relaxation of the smooth muscles of the bladder and prostate further enhances vascular effects.
Improving the erection, tadalafilum thus increases the possibility of carrying out PA (sexual intercourse).
In healthy men, compared with placebo, there is no significant change in the change in DAD, SAD, and heart rate, does not affect the electroretinogram, visual acuity, IOP and pupil size, does not violate the ability to recognize colors (green / blue).
After taking the pill tadalafilum well absorbed in the body. the concentration of the substance in the blood plasma reaches peak values 2 hours after ingestion. Food and time of taking the drug do not have a clinically significant effect on the rate of absorption of tadalafilum and its bioavailability.
About 94% of the substance is in the state associated with plasma proteins. It is metabolized in the liver with the participation of the cYP3A4 isoenzyme. the main circulating metabolite in comparison with tadalafilum shows at least 13 thousand times less activity in relation to PDE-5.
the average half-elimination period in healthy men is 17.5 hours. the drug is excreted mainly in the form of pharmacologically inactive metabolites. About 61% of the accepted dose is excreted with feces, about 36% – with urine.
Indications for use
The drug is used for ED (erectile dysfunction); With MRSA (symptoms of the lower urinary tract) in patients with BPH; With ED in patients with LUtS with BPH.
Cialis is not prescribed for:
♂Hypersensitivity to tadalafilum or auxiliary components of tablets;
♂Simultaneous use of any organic nitrate-containing preparation;
♂Simultaneous use of doxazosin or preparations for the treatment of ED;
♂The presence of contraindications to sexual activity in men with cardiac and vascular pathologies (unstable angina, suffered during the last three months of MI, angina pectoris, cHF II-IV classes according to the NYHA classification, AH, uncontrolled arrhythmias, transferred during the last six months ischemic stroke);
♂Associated or unrelated to the use of PDION-5 inhibitors NAION (anterior ischemic optic nerve neuropathy);
♂Lactose intolerance, lactase deficiency, glucose / galactose malabsorption.
♂In addition, the drug is contraindicated to persons under the age of eighteen, and can not be used more than 2 rubles a week. In men with renal damage, in which clcr is below 30 ml / min.
Because of the lack of data on patients with hepatic insufficiency, which is classified in the child-Pugh c-class classification, caution should be exercised when using tadalafilum in this group of patients.
With caution, Cialis is prescribed to persons who are on treatment with α1-adrenoreceptor blockers. this is due to the fact that with the simultaneous use of tadalafilum with these drugs has a risk of symptomatic arterial hypotension (SAG).
Clinical studies of the pharmacological properties of tadalafilum in a group of healthy men have shown that a single dose of a standard dose of Cialis does not lead to SAG with simultaneous application of α1A-adrenoblocker tamsulosin. the study involved 18 people.
Other restrictions apply:
☞Predisposition to priapism;
☞Anatomical deformation of the penis;
☞Simultaneous administration of antihypertensive drugs, as well as drugs that suppress the isoenzyme cYP3A4 (Erythromycin, Saquinavir, Itraconazole, Ritonavir, Ketoconazole).
Diagnosis of ED should include identifying the main cause of impotence, conducting an appropriate examination and determining adequate therapy.
With dysfunction of erection, the use of Cialis is most often accompanied by pain in the muscles or back, headache, flushing of the face, dyspepsia, nasal congestion.
In patients with ED / BPH, pain in the extremities and / or muscles, headache, gastroesophageal reflux (GER), dyspepsia were most often recorded.
Other possible adverse reactions:
☞Often – dizziness;
☞Infrequently, hypersensitivity reactions, blurred perception of visual images, pain in the eyeball, tachycardia, palpitations, increased or decreased blood pressure (the latter is possible in people who have already taken antihypertensive drugs), shortness of breath, nasal congestion, GER, abdominal pain, hyperhidrosis, rash ;
☞Rarely – a stroke (including acute damage to the blood circulation of the brain with a rupture of the vessel and hemorrhage (HMNc through hemorrhagic type)), transient amnesia, epileptic seizure, eyelid swelling, visual field disturbance, injection of the vessels of the sclera of the eyeball, myocardial infarction, nosebleeds, Urticaria, a prolonged erection.
In patients with previously existing risk factors for cVD, there were:
☞Infrequently – chest pain;
☞In rare cases – fainting, migraines, transient ischemic attacks, sudden cardiac death.
However, to be precise, these phenomena are associated with the use of tadalafilum, risk factors for cVD, sexual arousal, other factors or a combination of factors, or not, can not.
there are also reports of isolated cases of sudden hearing loss when using PDE-5 inhibitors (including tadalafilum) during clinical and post-marketing studies.
Side effects that occurred during postmarketing studies, but were not found in clinical placebo-controlled studies:
☞Swelling of the face;
☞Occlusion of the vessels of the retina;
☞Sudden cardiac death.
Instructions for use Cialis How to take Cialis with ED?
♂Patients with frequent sexual activity, when PA occurs more than 2 rub / week, 5 mg tablets are recommended to be taken daily, one at a time, at the same time.
♂Depending on the individual tolerance, it is possible to reduce the dosage of tadalafilum up to 2.5 mg.
♂If PA occurs less often than 2 p. / Week, it is recommended to take tablets immediately before coition at a dose of 20 mg.
the permissible upper limit of the daily dose of Cialis 20 mg.
♂Instructions for the use of Cialis according to ED / BPH or BPH
With these pathologies, the patient is prescribed a drug of 1 r./day for one tablet at the same time (any, regardless of the time of ingestion and the time of sexual activity).
♂The duration of the course of treatment Cialis 5 mg is determined individually.
♂When the kidneys are affected, when the clcr score is 31-80 ml / min, there is no need for correction of the dose. Patients with severe renal lesions, in which clcr does not exceed 30 ml / min, daily use of the drug is contraindicated.
Single administration of up to 0.5 g of tadalafilum by a healthy person and repeated application up to 100 mg / day. ♂Tadalafilum in patients with erectile dysfunction is accompanied by side effects similar to those that occur with the use of a lower drug.
♂In case of an overdose, standard symptomatic therapy is performed. Cialis is practically not excreted in hemodialysis.
Interaction of other drugs on tadalafilum
♂Biotransformation of Cialis is carried out with the participation of the isoenzyme cYP3A, and therefore drugs inhibiting this isoenzyme increase the value of cmax and AUc of tadalafilum.
♂Despite the fact that specific studies were conducted only on the interaction of tadalafilum with ketoconazole and ritonavir, it can be assumed that such drugs as Itraconazole and Erythromycin are also capable of increasing the activity of tadalafilum.
♂Rifampicin, which is an inducer of cYP3A, reduces the exposure of a single dose of the drug and the value of cmax. Most likely, the simultaneous use of other drugs from the group of cYP3A inducers should help reduce the plasma concentration of tadalafilum.
♂The use of Cialis in combination with antacids (hydroxide Al / Mg hydroxide) helps to reduce the rate of absorption of the active substance of the drug without changing the AUc for tadalafilum.
✌Drugs that increase the index of the acidity of the stomach (pH), and, in particular, the H2-blocker nizatidine, do not affect the pharmacokinetic parameters of tadalafilum.
✌A study of the safety and efficacy of Cialis combination with other methods of treating erectile ✌dysfunction (including in combination with other PDE5 inhibitors) has not been carried out, and it is therefore recommended that such combinations be avoided.
Tadalafilum does not contribute to an increase in bleeding time caused by ASA.
✌Effect of tadalafilum on other drugs
Tadalafilum able to enhance the hypotensive effect of nitrates, because of what these drugs are not prescribed in combination.
✌The substance has no significant effect on the clearance of drugs that are metabolized with the participation of the cytochrome P450 system.
In the course of the studies it was found that tadalafilum:
☞Does not suppress or induce isoenzymes cYP3A4, cYP1A2, cYP2c19, cYP2c9, cYP2t1 and cYP2D6;
☞Does not have a significant effect on the pharmacokinetics of S- or R-warfarin, as well as on the effect of warfarin on PtV (prothrombin time);
☞Does not increase the duration of bleeding caused by ASA;
☞causing a systemic vasodilator effect, is able to intensify the hypotensive effect of the funds intended for lowering blood pressure (in patients taking several antihypertensive drugs in poorly controlled hypertension, the blood pressure decreased more pronounced, and in most patients this phenomenon was not associated with hypotensive symptoms);
☞Does not have a significant effect on the pharmacodynamics and pharmacokinetic profile of teofillin.
✌The results of two studies show that the use of the drug in healthy men in combination with tamsulosin (α1A-adrenoblocker) does not cause a significant decrease in blood pressure.
✌The use of a drug with α1-adrenoblocker Doxazosin (provided that the latter is taken at a dose of 4 to 8 mg / day) was accompanied by augmentation of the hypotensive effect of doxazosin.
✌Individual patients experienced pressure-related symptoms, including fainting.
☞tablets should be stored at temperatures below 30° c.
Sexual activity can be dangerous in a number of pathologies of the heart and blood vessels. In connection with this, men with diseases that require restriction of sexual activity, treatment of erectile dysfunction, including tadalafilum, is contraindicated.
☑There are reports of cases of priapism (long, unrelated to sexual arousal, involuntary erection) against treatment with PDE-5 inhibitors.
Patients should be informed of the urgent need to see a doctor if the erection persists for four (or more) hours.
☑In the absence of timely assistance, such conditions lead to irreversible impotence.
☑Like other inhibitors of PDE-5, the drug causes systemic vasodilation, which can trigger a transient decrease in blood pressure. Before appointing tadalafilum, the physician should make sure that the patient with cardiac / vascular pathology does not undergo undesirable effects due to this effect.
☑Non-arterial AION is one of the causes of visual impairment (in some cases, before its complete loss). In the course of postmarketing observations, reports were recorded of rare cases of development of this pathology (cases were time-related with the use of PDE-5 inhibitors).
☑Determine exactly whether there is a direct link between tadalafilum and NAION treatment, to date it is impossible.
☑In case of sudden loss of vision, tadalafilum should be discontinued and seek medical attention.
☑The patient should also be warned that the people who have undergone NAION have a high risk of re-development of optical neuropathy.
☑If a patient is suspected of having BPH, he should undergo an additional examination to rule out prostate cancer.
☑Despite the fact that dizziness with the admission of tadalafilum occurred with the same frequency as when taking placebo, during the treatment should be careful when driving and machinery.