Dynamico Long, 5 mg 14 pcs

Indications

Active ingredient

Composition

Associates:

Lactose monohydrate (spray-dried) – 88.25 mg,

sodium lauryl sulfate – 0.75 mg,

povidone K-12 – 12.5 mg,

crospovidone – 12.5 mg,

sodium stearyl fumarate – 1 mg.

Composition of the film coating:

Opadray II 85F32782 yellow – 4 mg (partially hydrolyzed polyvinyl alcohol – 1.6 mg, macrogol-3350 – 0.808 mg, titanium dioxide (E171) – 0.688 mg, talc – 0.592 mg, iron oxide yellow dye (E172) – 0.312 mg.

How to take, the dosage

For oral administration.

Application of DYNAMIKO LONG for the indication of erectile dysfunction (ED).

For patients with frequent sexual activity (more than twice a week): Recommended frequency of administration is daily, once daily, 5 mg, at the same time, regardless of meal times. The daily dose can be reduced to 2.5 mg, depending on individual sensitivity.

For patients with infrequent sexual activity (less than twice a week):

The recommended dose is 10 mg before anticipated sexual activity, regardless of food intake. In patients in whom a dose of 10 mg is not effective enough, a dose of 20 mg is used. The drug should be taken at least 16 minutes before intended sexual activity. Patients may attempt sexual intercourse at any time within 36 hours of taking the drug in order to establish the optimal response time to the drug.

The recommended maximum daily dose of DYNAMIKO LONG is 20 mg.

The maximum recommended frequency of administration is once daily.

Doses of 10 mg and 20 mg are used immediately before sexual activity and are not recommended for daily use.

Application of DYNAMIKO LONG for the indication of benign prostatic hyperplasia (BPH) or ED/DPH.

The recommended dose of DYNAMIKO LONG 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 doctor individually.

In patients with mild renal insufficiency (creatinine clearance of 51 to 80 ml/min) and moderate renal insufficiency (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 the drug DYNAMIKO LONG is contraindicated.

Interaction

Influence of other drugs on tadalafil

Tadalafil is mainly metabolized with the isoenzyme CYP3A4. The selective CYP3A4 isoenzyme inhibitor ketoconazole (at a dose of 400 mg daily) increases the AUC of tadalafil by 312% and Cmax tadalafil by 22%, and ketoconazole (at a dose of 200 mg daily) increases the AUC of tadalafil by 107% and the Cmax of tadalafil by 15%.

Ritonavir (at a dose of 200 mg twice daily), an inhibitor of the CYP3A4, 2C9, 2C19 and 2D6 isoenzymes, increases the AUC of tadalafil by 124% without changing Cmax. Although 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, itraconazole and grapefruit juice, may increase plasma concentrations of tadalafil.

The role of transporters (e.g., P-glycoprotein) in the distribution of tadalafil is unknown. There is a possibility of drug interactions mediated by inhibition of transporters.

The selective CYP3A4 isoenzyme inducer, rifampicin (at a dose of 600 mg daily), reduces the AUC of tadalafil by 88% and the Cmax of tadalafil by 46%. It can be assumed that concomitant use of other CYP3A4 isoenzyme inducers (such as phenobarbital, phenytoin or carbamazepine) may also reduce plasma concentrations of tadalafil.

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

The increase in gastric pH due to intake of H2-histamine receptor blockers 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.

Influence 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 (NO) and cGMP metabolism, so the use of tadalafil with nitrates is contraindicated.

Tadalafil has no clinically significant effect on clearance of drugs metabolized by cytochrome P450 isoenzymes.

The studies 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 has no effect on 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 agents in whom blood pressure was poorly controlled. In most patients, the blood pressure decrease was not accompanied by symptoms of hypotension. Patients treated with hypotensive medications and taking tadalafil should be given appropriate clinical advice.

Two clinical studies showed no significant reduction in blood pressure when tadalafil and the selective alpha1A adrenoblocker tamsulosin were used concomitantly in healthy volunteers.

The concomitant use of tadalafil with doxazosin is contraindicated. When tadalafil was used by healthy volunteers who were taking the alpha1-adrenoblocker doxazosin (4-8 mg per day), an increase in the hypotensive effect of doxazosin was observed. Some patients experienced symptoms associated with decreased blood pressure, including fainting.

In clinical studies it has been shown that ryociguat enhances the hypotensive effect of FDE-5 inhibitors. Concomitant use of riociguat with FDE-5 inhibitors, including tadalafil, is contraindicated.

Tadalafil and 5-alpha reductase inhibitors have not been studied for drug interaction, so 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 oral terbutaline, but clinical implications have not been established.

Tadalafil had no effect on ethanol concentrations, and ethanol had no effect on tadalafil concentrations. At high doses of ethanol (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 ethanol (0.6 g/kg), no decrease in blood pressure was observed, and dizziness occurred with the same frequency as with ethanol alone.

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 erectile dysfunction treatment, including with DYNAMIKO LONG, should not be performed in men with such 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 effectiveness of combining tadalafil with other FDE-5 inhibitors and erectile dysfunction treatments have not been studied, so the use of such combinations is not recommended.

Like other FDE-5 inhibitors, tadalafil has systemic vasodilator properties, which may lead to transient decrease in blood pressure. Before prescribing DYNAMIKO LONG, the physician should carefully consider whether patients with cardiovascular disease would be adversely affected by such vasodilatory effects.

NAPION is a cause of visual impairment, including total loss of vision. There have been rare post-marketing reports of cases of NAPION development that are temporally related to the intake of FDE-5 inhibitors. Analysis of 1 to 4 days of episodic use of FDE-5 inhibitors in men with erectile dysfunction suggests an increased risk of acute NAPION. The physician should advise patients in cases of sudden vision loss to stop taking tadalafil and seek medical attention. The physician should also inform patients that the risk of recurrence of NAPION is higher in patients who have previously had NAPION.

Patients with a suspected diagnosis of BPH should be screened to rule out prostate cancer.

The efficacy of DYNAMIKO LONG in patients who have undergone pelvic surgery or radical prostatectomy without preservation of nerve-vascular bundles is unknown.

Influence on the ability to drive and operate vehicles

. Although the incidence of dizziness is similar between placebo and tadalafil, caution should be exercised during treatment when driving motor vehicles and engaging in other potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Synopsis

Contraindications

Cautions

There is not enough data about patients with severe hepatic impairment (Child-Pugh class C), so caution must be exercised when DYNAMICO LONG is prescribed to this group of patients.

We should exercise caution when administering the drug to patients taking alpha1-adrenoblockers, because concomitant use may lead to symptomatic arterial hypotension in some patients. In two clinical pharmacology studies, symptomatic arterial hypotension was not observed in healthy volunteers taking tadalafil when used concomitantly with tamsulosin, a selective alpha1A-adrenoblocker (see “Interaction with Other Drugs”).

The drug should be used with caution in patients with a predisposition to priapism (in case of sickle cell anemia, multiple myeloma or leukemia) or in patients with anatomical deformity of the penis (angular curvature, cavernous fibrosis or Peyronie’s disease). Caution should also be observed when concomitant administration with CYP3A4 isoenzyme inhibitors (ritonavir, saquinavir, ketoconazole, itraconazole, clarithromycin, erythromycin, grapefruit juice), hypotensive agents, 5-alpha reductase inhibitors.

The diagnosis of erectile dysfunction should include identifying the potential underlying cause, appropriate physical examination, and determining treatment tactics.

Side effects

The most common adverse events in patients with erectile dysfunction and BPH are: headache, dyspepsia, and back pain and myalgia.

The following are the side effects that have been reported during clinical trials and during post-registration use of the drug. The reported side effects were usually mild to moderate and transient. According to WHO classification, all reactions are categorized by organ system and frequency of development: very common (≥1/10); common (≥1/100, < 1/10); infrequent (≥1/1000, < 1/100): rare (≥1/10000, < 1/1000): very rare (< 1/10000); frequency unknown (cannot be determined based on available data).

Immune system disorders: infrequent – hypersensitivity reactions; rare – angioedema2.

Nervous system disorders: frequent – headache; infrequent – dizziness; rare – stroke1 (including acute hemorrhagic cerebral circulation disorder), syncope, transient ischemic attacks1, migraine2, epileptic seizures2, transient amnesia.

Visual disturbances: infrequently – blurred vision, pain in the eyeball; rarely – visual field disturbance, eyelid swelling, conjunctival hyperemia, NAPION2, retinal vascular occlusion2.

Hearing organ and labyrinth disorders: infrequently – tinnitus;

rarely – sudden hearing loss.

Cardiac disorders1: infrequently – tachycardia, palpitations; rarely – myocardial infarction, ventricular rhythm disturbances2, unstable angina2.

vascular disorders: frequent – “rushes” of blood to the face; infrequent – reduction of blood pressure3, increase in blood pressure.

Disorders of the respiratory system, thoracic and mediastinal organs: often – nasal congestion; infrequently – shortness of breath, nasal bleeding.

Disorders of the gastrointestinal tract: frequent – dyspepsia; infrequent – abdominal pain, gastroesophageal reflux, diarrhea in patients older than 65 years, vomiting, nausea.

Skin and subcutaneous tissue disorders: infrequently – skin rash; rarely – urticaria, Stevens-Johnson syndrome2, exfoliative dermatitis2, hyperhidrosis (increased sweating).

Skeletal, muscular and connective tissue disorders: frequently – back pain, myalgia, pain in the extremities.

Recreational and urinary tract disorders: frequently – hematuria.

Renital and mammary gland disorders: frequently – prolonged erection; rarely – priapism, hematospermia, bleeding from the penis.

General disorders: infrequent – chest pain1, peripheral edema, fatigue; rare – facial edema2, sudden cardiac death1,2.

1 Observed in patients with previous cardiovascular risk factors.

But 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.

2 Adverse reactions identified with postmarketing use not observed in clinical placebo-controlled studies.

3 More commonly observed when tadalafil was used in patients already taking hypotensive agents.

Overdose

Similarities