Tadalafil-SZ, 20 mg 4 pcs

How to take, the dosage

For oral administration.

The use of Tadalafil-SZ for the indication erectile dysfunction (ED)
For patients with frequent sexual activity (more than twice a week): the recommended frequency of administration is daily, once daily, 5 mg, at the same time, regardless of meals. The daily dose may be reduced to 2.5 mg (1/2 tablet 5 mg) depending on individual sensitivity.

In patients with infrequent sexual activity (less than twice a week), a dose of 20 mg of Tadalafil-SZ is recommended immediately before sexual activity according to the instructions for medical use of the drug.

The maximum daily dose of Tadalafil-SZ is 20 mg.

The use of Tadalafil-SZ for the indication of BPH or ED/DPH.

The recommended dose of Tadalafil-SZ when used once daily is 5 mg; the drug should be taken at approximately the same time of the day, regardless of the time of sexual activity. The duration of treatment is determined by the physician individually.

In patients with mild renal failure (creatinine clearance of 51 to 80 ml/min) and moderate renal failure (creatinine clearance of 31 to 50 ml/min), no dose adjustment is required. In patients with severe renal insufficiency (creatinine clearance < 30 ml/min and on hemodialysis): the use of Tadalafil-SZ is contraindicated.

Interaction

The effect of other drugs on tadalafil

Tadalafil is mainly metabolized with participation of the CYP3A4 isoenzyme. The selective CYP3A4 isoenzyme inhibitor ketoconazole (400 mg per day) increases tadalafil single dose exposure (AUC) by 312% and Stah values by 22%, and ketoconazole (200 mg per day) increases tadalafil single dose exposure (AUC) by 107% and Stah values by 15% relative to AUC and Stah values for tadalafil alone.

Ritonavir (200 mg twice daily), an inhibitor of the CYP3A4, 2C9, 2C19, and 2D6 isoenzymes, increases single-dose tadalafil exposure (AUC) by 124% with no change in Stache.

While specific interactions have not been studied, it can be assumed that other HIV protease inhibitors, such as saquinavir, as well as CYP3A4 isoenzyme inhibitors such as erythromycin, clarithromycin, and itraconazole and grapefruit juice, may increase tadalafil plasma concentrations. The role of transporters (e.g., P-glycoprotein) in the distribution of tadalafil is unknown.

There is a possibility of a drug interaction mediated by inhibition of transporters. The selective CYP3A4 isoenzyme inducer, rifampicin (at a dose of 600 mg daily), reduces single-dose tadalafil exposure (AUC) by 88% and Stach by 46%, relative to the AUC and Stach values for tadalafil alone.

The concomitant use of other CYP3A4 isoenzyme inducers (such as phenobarbital, phenytoin or carbamazepine) may also be expected to reduce plasma concentrations of tadalafil.

Concomitant administration of antacid (magnesium hydroxide/aluminum hydroxide) and tadalafil reduces the rate of absorption of tadalafil without changing the AUC for tadalafil.

The increase in gastric pH due to ingestion of the H2-histamine receptor blocker nizatidine had no effect on the pharmacokinetics of tadalafil.

The safety and efficacy of combining tadalafil with other erectile dysfunction treatments or other FDE-5 inhibitors have not been studied, so such combinations are not recommended.

The effect of tadalafil on other drugs

Tadalafil is known to increase the hypotensive effect of nitrates. This is due to the additive effect of nitrates and tadalafil on nitric oxide II (N0) and cGMP metabolism. Therefore, the use of tadalafil with nitrates is contraindicated.

Tadalafil has no clinically significant effect on the clearance of drugs whose metabolism involves cytochrome P450. Studies have confirmed that tadalafil neither inhibits nor induces CYP1A2, CYP3A4, CYP2C9, CYP2C19, CYP2D6, CYP2E1 isoenzymes. Tadalafil has no clinically significant effect on the AUC of S-warfarin or R-warfarin. Tadalafil does not affect the effect of warfarin on prothrombin time.

Tadalafil does not potentiate an increase in the duration of bleeding caused by taking acetylsalicylic acid.

Tadalafil has systemic vasodilator properties and may increase the effect of hypotensive drugs to reduce blood pressure. Additionally, a slightly greater reduction in blood pressure was observed in patients taking multiple hypotensive drugs in whom blood pressure was poorly controlled.

In the vast majority of patients, this decrease was not associated with hypotensive symptoms. Patients treated with hypotensive medications and taking tadalafil should be given appropriate clinical advice. No significant reduction in blood pressure was observed with concomitant use of tadalafil and the selective alpha1A-adrenoblocker tamsulosin in healthy volunteers.

The concomitant use of tadalafil with doxazosin is contraindicated. When tadalafil was used by healthy volunteers who were taking doxazosin (4-8 mg per day), alpha]-adrenoblocker, an increase in the hypotensive effect of doxazosin was observed. Some patients experienced symptoms associated with decreased blood pressure, including fainting.

The concomitant use of riociguat with FDE-5 inhibitors, including tadalafil, is contraindicated because riociguat increases the hypotensive effect of FDE-5 inhibitors.
No studies of drug interaction between tadalafil and 5-alpha reductase inhibitors have been conducted, caution should be exercised when taking them concomitantly.

Tadalafil causes an increase in bioavailability of ethinylestradiol when taken orally.
A similar increase in bioavailability can be expected with terbutaline, but no clinical effects have been established.

Tadalafil had no effect on alcohol concentration, nor did alcohol affect tadalafil concentration. At high doses of alcohol (0.7 g/kg), tadalafil administration did not cause a statistically significant decrease in mean blood pressure. Postural dizziness and orthostatic hypotension were observed in some patients.

When tadalafil was taken in combination with lower doses of alcohol (0.6 g/kg), no decrease in blood pressure was observed, and dizziness occurred with the same frequency as when alcohol alone was taken.

Tadalafil has no clinically significant effect on the pharmacokinetics or pharmacodynamics of theophylline.

Special Instructions

Sexual activity has potential risks for patients with cardiovascular disease. Therefore, treatment of erectile dysfunction, including with Tadalafil-SZ, should not be performed in men with heart disease in which sexual activity is not recommended.

There have been reports of the occurrence of priapism when using FDE-5 inhibitors, including tadalafil. Patients should be informed to seek immediate medical attention if an erection lasts 4 hours or more. Failure to treat priapism in a timely manner leads to penile tissue damage, which may result in irreversible impotence.

The safety and efficacy of combination of Tadalafil-SZ with other FDE-5 inhibitors and treatments for erectile dysfunction have not been studied. Therefore, the use of such combinations is not recommended. Like other FDE-5 inhibitors, tadalafil has systemic vasodilator properties, which may lead to a transient decrease in blood pressure.

Before prescribing tadalafil-SZ, physicians should carefully consider whether patients with cardiovascular disease would be adversely affected by such vasodilatory effects. Nonarterial anterior ischemic optical neuropathy (NAPION) causes visual impairment, including total vision loss.

There have been rare post-marketing reports of cases of NAPION development temporally associated with the intake of FDE-5 inhibitors. At

it is not currently possible to determine whether there is a direct link between the development of NAPION and the intake of FDE-5 inhibitors or other factors. Physicians should advise patients to discontinue tadalafil and seek medical attention in the event of sudden vision loss.

Doctors should also inform patients that people who have had NAPION have an increased risk of developing NAPION again. Patients with a suspected diagnosis of BPH should be screened to rule out prostate cancer.

The efficacy of Tadalafil-SZ in patients who have undergone pelvic surgery or radical neurosurgical prostatectomy is unknown.

When treating with Tadalafil-SZ, caution should be exercised when driving motor vehicle and engaging in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

• High sensitivity to tadalafil or any drug ingredient;
• taking drugs containing any organic nitrates;
• possible contraindications to sexual activity in patients with cardiovascular disease: myocardial infarction within the last 90 days, unstable angina, occurrence of an angina attack during sexual intercourse, chronic heart failure NYHA class II or higher within the last 6 months, uncontrolled arrhythmias, arterial hypotension (BP <90/50 mm Hg.Hg.), uncontrolled arterial hypertension, ischemic stroke within last 6 months;
• loss of vision due to nonarterial anterior ischemic optical neuropathy (NAPION) (regardless of association with FDE-5 inhibitors);
• concomitant use with doxazosin, other FDE-5 inhibitors, other erectile dysfunction therapies, with guanylate cyclase stimulators such as riociguat;
• lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
• the age below 18 years.

With caution:

severe hepatic impairment (Child-Pugh class C) (there are insufficient data for such patients); concomitant use of alpha1-adrenoblockers (concomitant use of these drugs may lead to symptomatic arterial hypotension in some patients; no symptomatic arterial hypotension is observed with a single dose of tadalafil when used concomitantly with tamsulosin, a selective alpha1A-adrenoblocker (see “Interactions “Interaction);

predisposition to priapism (in sickle cell anemia, multiple myeloma or leukemia) or anatomical deformity of the penis (angular curvature, cavernous fibrosis or Peyronie’s disease); concurrent use with CYP3A4 isoenzyme inhibitors (including Ritonavir, saquinavir, ketoconazole, itraconazole, clarithromycin, erythromycin, grapefruit juice), hypotensive agents, 5-alpha reductase inhibitors.

Diagnosis of erectile dysfunction should include identification of the potential underlying cause, appropriate medical examination and determination of treatment tactics.

Side effects

The most frequent adverse events in patients with erectile dysfunction and BPH are headache and dyspepsia, as well as back pain and myalgia.
According to the WHO classification, all reactions are categorized according to organ system and frequency of development: Very common (> 1/10); common (> 1/100, < 1/10); infrequent (> 1/1000, < 1/100); rare (> 1U0000, < 11000); very rare (< 1/10000), frequency unknown (the frequency of reactions cannot be determined from available data).

Disorders of the immune system:

Infrequent: hypersensitivity reactions. Rare: angioedema. Nervous system disorders:

Often: headache.
Infrequent: dizziness.
Rare: stroke’ (including acute hemorrhagic cerebral circulation disorder (ACAD)), syncope, transient ischemic attacks, migraine, epileptic seizures, transient amnesia.

Visual organ disorders:
Infrequent: blurred vision, pain in the eyeball.
Rarely: visual field disorders, eyelid swelling, conjunctival hyperemia, nonarterial anterior ischemic optical neuropathy, retinal vascular occlusion.

Hearing and labyrinth disorders:

Infrequent: tinnitus.
Rarely: sudden hearing loss.

Heart disorders:
Infrequent: palpitations, tachycardia.
Rare: myocardial infarction, ventricular rhythm disturbances, unstable angina pectoris.

Vascular disorders: Often: “flushes” of blood to the face.

Infrequent: decreased blood pressure, increased blood pressure.
Respiratory system disorders, thoracic and mediastinal organs:

Often: nasal congestion.
Infrequent: shortness of breath, nasal bleeding.
Gastrointestinal disorders:

Often: dyspepsia.
Infrequent: abdominal pain, gastroesophageal reflux, diarrhea in patients older than 65 years, vomiting, nausea.

Skin and subcutaneous tissue disorders:
Infrequent: rash.
Rare: urticaria, Stevens-Johnson syndrome, exfoliative dermatitis, hyperhidrosis (increased sweating).

Musculoskeletal and connective tissue disorders:

Often: back pain, myalgia, pain in the extremities. Renal and urinary tract disorders: Infrequent: hematuria.

Gender and mammary gland disorders: Infrequent: prolonged erection.
Rarely: priapism , hematospermia, bleeding from the penis.

General disorders:
Infrequent: chest pain, peripheral edema, fatigue. Rarely: facial edema, sudden cardiac death.

‘Observed in patients with previous cardiovascular risk factors. However, it is not possible to definitively determine whether these phenomena are directly related to these risk factors, to tadalafil, to sexual arousal, or to a combination of these or other factors.

The adverse reactions seen with post-marketing use not observed in clinical placebo-controlled studies.

Prevalently observed when tadalafil was used in patients already taking hypotensive medications.

Overdose

Symptoms: when tadalafil at a single dose of up to 500 mg was administered to healthy volunteers and to patients with erectile dysfunction repeatedly, up to 100 mg/day, the adverse effects were the same as those of lower doses.

Treatment: symptomatic. In hemodialysis tadalafil is practically not excreted.

Pregnancy use

Tadalafil-SZ is not intended for use in women.

Similarities

Cialis, Dynamico Long, Framitus