Tadalafil-NW
Tadalafil-SZ: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Tadalafil-SZ
ATX code: G04BE08
Active ingredient: tadalafil (Tadalafil)
Manufacturer: Severnaya Zvezda, CJSC (Russia)
Description and photo updated: 30.11.2018
Prices in pharmacies: from 52 rubles.
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Tadalafil-SZ is a drug for the treatment of erectile dysfunction, phosphodiesterase type 5 inhibitor (PDE-5).
Release form and composition
Tadalafil-SZ is available in the form of film-coated tablets: round, biconvex; dosage 5 mg - yellow, with a dividing line on one side, dosage 20 mg - pinkish-orange; the core of the tablet is almost white or white (dosage 5 mg: in blisters - 10 pcs., in a cardboard box 2, 3 or 6 packages, 14 pcs., in a cardboard box 1 or 2 packages; 20 pcs. in a polymer can / bottle, in a cardboard box 1 can / bottle; dosage 20 mg: in blisters - 4, 7 or 8 pcs., in a cardboard box 1 package, 10 pcs., in a cardboard box 1 or 2 packages; 20 pcs. in a polymer can / bottle, in a cardboard box 1 can / bottle. Each pack also contains instructions for the use of Tadalafil-SZ).
1 tablet contains:
- active substance: tadalafil - 5 or 20 mg;
- auxiliary components: lactopress (lactose monohydrate) (milk sugar), lactose monohydrate (milk sugar), croscarmellose sodium (primellose), microcrystalline cellulose, crospovidone (Kollidon CL), crospovidone (Kollidon CL-M), hyprolose (hydroxypropyl cellulose) (hydroxypropyl cellulose), sodium lauryl sulfate, sodium stearyl fumarate.
Film casing composition:
- dosage 5 mg: Opadry II 85F22048 yellow - polyvinyl alcohol (partially hydrolyzed), macrogol [PEG (polyethylene glycol) 3350], titanium dioxide (E171), aluminum varnish based on the dye "Sunset" yellow, aluminum varnish based on the dye quinoline yellow, aluminum varnish based on indigo carmine dye, iron dye oxide (II) yellow (E172), talc;
- dosage 20 mg: Opadry II 85F240037 pink - polyvinyl alcohol (partially hydrolyzed), iron dye oxide (II) yellow (E172), iron dye oxide (II) red (E172), macrogol (PEG 3350), titanium dioxide (E171), talc.
Pharmacological properties
Pharmacodynamics
Tadalafil-SZ - a drug designed to stimulate erectile function, improves erection and increases the ability to have a full sexual intercourse. Its active ingredient - tadalafil - is a reversible selective inhibitor of cyclic guanosine monophosphate (cGMP) of specific PDE-5, which is active only during the period of sexual arousal, accompanied by local release of nitric oxide. Tadalafil, inhibiting PDE-5, increases the concentration of cGMP in the cavernous body of the penis and relaxes the smooth muscles of the arteries. This allows blood to flow to the tissues of the penis and induces an erection.
PDE-5 is an enzyme found in the smooth muscles of the vessels of the internal organs and the corpus cavernosum, platelets, kidneys, lungs, cerebellum, skeletal muscles. Compared to the effect of tadalafil on PDE-5, the degree of its activity towards other PDEs is low. The results of in vitro studies demonstrate that the inhibition of PDE-1, PDE-2, PDE-4 and PDE-7 by tadalafil, which are predominantly located in the brain, heart, blood vessels, leukocytes, liver, skeletal muscles, is 10,000 times lower, than PDE-5. Selective activity in relation to PDE-5 is of great importance. So, tadalafil does not have a blocking effect on PDE-3 (an enzyme found in the heart and blood vessels), which is involved in the contraction of the heart muscle. In addition, the activity of tadalafil is about 700 times lower in relation to PDE-6 - an enzyme thatfound in the retina and responsible for photographic transmission. The effect of the drug on PDE-8, PDE-9, PDE-10 is 9000 times and on PDE-11 is 14 times less than PDE-5. The distribution of PDE-8-PDE-11 enzymes in tissues and the physiology of their inhibition effects have not been established.
In healthy men, tadalafil does not cause significant changes in systolic and diastolic blood pressure (BP) in the supine and standing position, does not change the heart rate (HR).
Low affinity for PDE-6 determines the absence of changes in color recognition (blue or green) and the effect of tadalafil on visual acuity, pupil size, electroretinogram, intraocular pressure.
With daily intake of Tadalafil-SZ, the undesirable effect of tadalafil on the morphology of spermatozoa and their motility has not been established. A decrease in the average sperm concentration can be caused by a high frequency of ejaculation. In addition, there was no negative effect on the average concentration of sex hormones, including testosterone, luteinizing and follicle-stimulating hormones.
Taking Tadalafil-SZ once a day provides an improvement in erection in case of erectile dysfunction of all severity.
Inhibition of PDE-5 by tadalafil leads to an increase in the concentration of cGMP not only in the cavernous body of the penis, but also in the smooth muscles of the prostate gland, urinary bladder and blood vessels that supply them with blood. Taking the drug for benign prostatic hyperplasia (BPH) promotes relaxation of vascular smooth muscles, leads to an increase in blood perfusion in these organs and a decrease in the severity of BPH symptoms. Relaxation of the smooth muscles of the bladder and prostate gland can further enhance vascular effects.
Pharmacokinetics
After taking Tadalafil-SZ inside, tadalafil is rapidly absorbed, its average maximum concentration (C max) in plasma is reached after 2 hours. The speed and degree of absorption is not affected by simultaneous food intake or time of day (morning or evening). With respect to time and dose, the pharmacokinetics of the drug in healthy men is linear. In the range of 2.5–20 mg of tadalafil, AUC (total plasma concentration) increases in proportion to the dose. When the drug is taken once a day, the equilibrium plasma concentration is reached within 5 days. The pharmacokinetics of tadalafil is similar both with and without erectile dysfunction.
The volume of distribution averages 63 liters.
Plasma protein binding - 94%, with impaired renal function, it does not change. Tadalafil is well distributed in body tissues, up to 0.000 5% of the dose taken is found in semen.
Tadalafil is metabolized with the participation of the CYP3A4 isoenzyme. The main circulating metabolite, methylcatecholglucuronide, has no clinical significance, its activity against PDE-5 is 13,000 times lower than that of tadalafil.
In healthy men, the half-life (T 1/2) averages 17.5 hours, the average clearance is 2.5 l / h.
The drug is excreted in the form of inactive metabolites: through the intestines - about 61%, through the kidneys - about 36% of the dose.
Men aged 65 and over do not need to change the dosage regimen.
With mild renal failure with creatinine clearance (CC) 51–80 ml / min and moderate renal failure with CC 31–50 ml / min, the exposure of tadalafil (AUC) increases approximately 2 times. In patients with end-stage renal failure who are on hemodialysis, C max is increased by 41% compared to healthy volunteers. With hemodialysis, tadalafil is excreted to a small extent.
With mild to moderate hepatic impairment (classes A and B according to the Child-Pugh classification), the pharmacokinetics of tadalafil does not change. In severe hepatic impairment (class C according to the Child-Pugh classification), it is recommended to start taking the drug after a preliminary assessment of the risk-benefit ratio of therapy.
In patients with diabetes mellitus, the dose selection of tadalafil is not required.
Indications for use
The use of Tadalafil-SZ is indicated for the treatment of erectile dysfunction.
In addition, taking tablets at a dose of 5 mg is prescribed to patients with lower urinary tract symptoms with benign prostatic hyperplasia, including with concomitant erectile dysfunction.
Contraindications
Absolute:
- diseases of the cardiovascular system: uncontrolled arrhythmias, unstable angina pectoris, chronic heart failure of class II and higher according to the NYHA classification (New York Heart Association) in the last six months, attacks of angina pectoris during intercourse, arterial hypotension (BP below 90/50 mm Hg), uncontrolled arterial hypertension, myocardial infarction within the last three months, ischemic stroke within the last six months;
- the simultaneous use of funds that contain any organic nitrates;
- concomitant therapy with other PDE-5 inhibitors or erectile dysfunction therapy agents, doxazosin, guanylate cyclase stimulants (including riociguat);
- chronic renal failure with CC less than 30 ml / min;
- loss of vision as a result of non-arterial anterior ischemic optic neuropathy (NAPION), including while taking PDE-5 inhibitors;
- lactose intolerance, glucose-galactose malabsorption syndrome, lactase deficiency;
- age up to 18 years;
- hypersensitivity to the components of the drug.
Care should be taken when prescribing Tadalafil-SZ to patients with severe hepatic impairment (class C according to the Child-Pugh classification), a predisposition to priapism (sickle cell anemia, leukemia, multiple myeloma), anatomical deformity of the penis (Peyronie's disease, angular curvature, cavernous fibrosis), with concomitant therapy with alpha 1- adrenergic blockers, antihypertensive drugs, ritonavir, saquinavir, ketoconazole, itraconazole, clarithromycin, erythromycin and other inhibitors of the CYP3A4 isoenzyme (including the use of grapefruit juice), 5-alpha reductase inhibitors.
Tadalafil-SZ, instructions for use: method and dosage
Tadalafil-SZ tablets are taken orally, regardless of food intake.
The doctor prescribes the drug and determines the treatment tactics based on the results of an appropriate medical examination, including identifying the main potential cause of erectile dysfunction.
Recommended dosage of Tadalafil-SZ:
- erectile dysfunction: men with sexual activity more than 2 times within 7 days - 5 mg once a day, every day, always at the same time. Taking into account individual sensitivity, the daily dose can be reduced to 2.5 mg. Men with sexual activity less than 2 times within 7 days - 20 mg immediately before intercourse. The maximum daily dose is 20 mg;
- benign prostatic hyperplasia, including with erectile dysfunction: 5 mg once a day, always at the same time, regardless of the time of sexual activity. The doctor sets the duration of the course of treatment individually.
With mild to moderate renal failure (CC from 31 to 80 ml / min), dose adjustment of Tadalafil-SZ is not required.
Side effects
Adverse events from systems and organs (classified as follows: very often - ≥ 1/10, often - ≥ 1/100 and <1/10, infrequently - ≥ 1/1000 and <1/100, rarely - ≥ 1/10 000 and <1/1000, very rarely - <1/10 000, including isolated cases):
- from the gastrointestinal tract: often - dyspepsia; infrequently - nausea, abdominal pain, vomiting, gastroesophageal reflux, over the age of 65 - diarrhea;
- from the nervous system: often - headache; infrequently - dizziness; rarely - migraine, fainting, transient ischemic attacks, transient amnesia, epileptic seizures, stroke (including acute hemorrhagic impairment of cerebral circulation);
- from the heart: infrequently - tachycardia, palpitations; rarely - unstable angina, ventricular arrhythmias, myocardial infarction;
- from the side of the vessels: often - flushing of the face; infrequently - lowering blood pressure (more often against the background of simultaneous administration of antihypertensive drugs), increased blood pressure;
- on the part of the organ of vision: infrequently - a feeling of pain in the eyeball, blurred visual perception; rarely - swelling of the eyelids, impaired visual fields, conjunctival hyperemia, occlusion of retinal vessels, NAPION;
- from the organ of hearing and labyrinthine disorders: infrequently - ringing in the ears; rarely - sudden hearing loss;
- from the respiratory system, chest and mediastinal organs: often - nasal congestion; infrequently - nosebleeds, shortness of breath;
- dermatological reactions: infrequently - rash; rarely - hyperhidrosis (excessive sweating), urticaria, exfoliative dermatitis, Stevens-Johnson syndrome;
- from the immune system: infrequently - hypersensitivity reactions; rarely - angioedema;
- from the musculoskeletal system and connective tissue: often - myalgia, pain in the back and / or extremities;
- from the genitals and mammary gland: infrequently - prolonged erection; rarely - hematospermia, bleeding from the penis, priapism;
- from the urinary system: infrequently - hematuria;
- general disorders: infrequently - fatigue, peripheral edema, chest pain; rarely - facial edema, sudden cardiac death.
Overdose
Symptoms: the occurrence of undesirable effects characteristic of the use of Tadalafil-SZ in usual doses.
Treatment: the appointment of symptomatic therapy. Hemodialysis is ineffective.
special instructions
Against the background of the use of Tadalafil-SZ, such undesirable phenomena as headache, dyspepsia, back pain and myalgia most often occur.
You should not treat erectile dysfunction in men with cardiovascular disease, in which sexual activity is associated with a potential risk.
When treating with tadalafil, priapism may occur. Therefore, the patient should be informed that if an erection continues for 4 hours or more, it is necessary to urgently seek medical help in order to avoid damage to the tissues of the penis and the onset of irreversible impotence.
When prescribing Tadalafil-SZ to patients with cardiovascular diseases, the physician should carefully assess the expected degree of transient lowering of blood pressure resulting from the systemic vasodilatory effect of the drug.
The effectiveness of Tadalafil-SZ in men who have undergone radical neuro-sparing prostatectomy or surgery on the pelvic organs has not been established.
To confirm the diagnosis of benign prostatic hyperplasia, the patient needs to undergo an examination that excludes prostate cancer.
Patients should be informed about the possible sudden loss of vision and the need to stop taking Tadalafil-SZ and consult a doctor in this case. It should be borne in mind that patients who have undergone NAPION have an increased risk of its recurrence.
Influence on the ability to drive vehicles and complex mechanisms
During the period of application of Tadalafil-SZ, it is recommended to be careful when driving vehicles and performing potentially hazardous activities that require increased attention and high speed of psychomotor reactions.
Application during pregnancy and lactation
Tadalafil-SZ is not intended for use in women.
Pediatric use
Tadalafil-SZ is contraindicated in patients under the age of 18.
With impaired renal function
With severe renal failure (CC less than 30 ml / min) and patients on hemodialysis, the use of Tadalafil-SZ is contraindicated.
With mild to moderate renal failure (CC from 31 to 80 ml / min), dose adjustment is not required.
For violations of liver function
Tadalafil-SZ tablets should be used with caution in patients with severe hepatic impairment (class C according to Child-Pugh classification).
Use in the elderly
No dose adjustment is required for men over the age of 65.
Drug interactions
- ketoconazole (a selective inhibitor of the isoenzyme CYP3A4): in a daily dose of 400 or 200 mg causes an increase in the exposure of a single dose of tadalafil by 312 or 107% and C max by 22 or 15%, respectively, compared with the AUC and C max of tadalafil with monotherapy;
- ritonavir (an inhibitor of isoenzymes CYP3A4, CYP2C9, CYP2C19 and CYP2D6): in a daily dose of 400 mg increases the AUC of a single dose of tadalafil by 124%;
- clarithromycin, erythromycin, itraconazole, grapefruit juice (inhibitors of the isoenzyme CYP3A4), HIV (human immunodeficiency virus) protease inhibitors (including saquinavir): may increase the concentration of tadalafil in blood plasma;
- rifampicin, phenobarbital, phenytoin, carbamazepine (inducers of the CYP3A4 isoenzyme): may cause a decrease in the concentration of tadalafil in blood plasma;
- magnesium hydroxide, aluminum hydroxide: reduce the rate of absorption of tadalafil, without affecting the AUC of the drug;
- nizatidine (blocker of H 2 -histamine receptors): an increase in gastric acidity while taking it does not affect the pharmacokinetics of tadalafil;
- nitrate preparations: the hypotensive effect of nitrates increases;
- drugs, the metabolism of which occurs with the participation of cytochrome P 450: tadalafil does not have a clinically significant effect on their clearance;
- warfarin: when taken simultaneously with tadalafil, clinically significant changes in the action of warfarin on prothrombin time are not observed, there is no effect on the AUC of the R- or S-isomers of warfarin;
- acetylsalicylic acid: tadalafil has no effect on the duration of bleeding caused by taking acetylsalicylic acid;
- antihypertensive drugs: it is possible to enhance their action;
- riociguat: causes a clinically significant increase in the hypotensive effect of PDE-5 inhibitors;
- doxazosin (in a daily dose of 4–8 mg): enhances its hypotensive effect;
- tamsulosin (selective alpha 1A- adrenergic blocker): a significant decrease in blood pressure is not expected;
- ethinylestradiol, terbutaline: their bioavailability increases;
- ethanol: changes in the concentrations of tadalafil and alcohol do not occur, in some cases, the development of orthostatic hypotension, postural dizziness is possible;
- theophylline: there are no clinically significant changes in its pharmacokinetics or pharmacodynamics.
In addition, according to research results, tadalafil does not induce or inhibit isoenzymes CYP1A2, CYP3A4, CYP2C19, CYP2C9, CYP2D6, CYP2E1.
Analogs
Analogs of Tadalafil-SZ are: Cialis, Viagra, Cialis Forte, Cialis Soft, Viasan-LF, Yohimbine hydrochloride, Vizarsin, Tornetis, Verona, Dynamico, Zydena, Railis, Impaza, Sirbida, Maxigra, Silafil, Sildena Strong and Olmax Strong.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C in a dark place.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tadalafil-SZ
Reviews about Tadalafil-SZ are positive. Patients indicate the effectiveness of the drug. In addition, in comparison with similar products, the drug has a reasonable price, which is its significant advantage.
Price for Tadalafil-SZ in pharmacies
The price of Tadalafil-SZ for a package containing 8 tablets of 20 mg each can range from 1,347 rubles.
Tadalafil-SZ: prices in online pharmacies
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Drug name Price Pharmacy |
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Tadalafil-SZ 20 mg film-coated tablets 1 pc. 52 RUB Buy |
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Tadalafil-SZ 20 mg film-coated tablets 4 pcs. 259 r Buy |
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Tadalafil-SZ tablets p.o. 20mg 4 pcs. 348 r Buy |
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Tadalafil-SZ 20 mg film-coated tablets 8 pcs. 442 r Buy |
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Tadalafil-SZ tablets p.o. 20mg 8 pcs. 555 RUB Buy |
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Tadalafil-SZ 5 mg film-coated tablets 30 pcs. 588 r Buy |
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Tadalafil-SZ 5 mg film-coated tablets 28 pcs. 601 RUB Buy |
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Tadalafil-SZ tablets p.o. 5mg 28 pcs. RUB 609 Buy |
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Tadalafil-SZ tablets p.o. 5mg 30 pcs. 645 RUB Buy |
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Tadalafil-SZ 20 mg film-coated tablets 10 pcs. 787 r Buy |
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Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
