Cupid 36 (Cupid 36)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceTadalafilTadalafil
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    • Dosage form: & nbsptfilm-covered laths
    Composition:

    Each tablet, covered with a film jacket contains:

    Active substance: tadalafil 20.00 mg;

    Excipients: lactose monohydrate 249.00 mg, microcrystalline cellulose 66.00 mg, giprolose 3.50 mg, sodium lauryl sulfate 1.00, croscarmellose sodium 7.00 mg, magnesium stearate 3.50 mg;

    Film sheath: opadrai II 32K520009 yellow 8.00 mg (lactose monohydrate 36%, hypromellose 26%, titanium dioxide 15.5%, iron oxide yellow 8.5%, triacetin 8.0%, talc 6.0%).

    Description:

    Almond-shaped tablets covered with a film shell, yellow, engraved "20" on one side.

    Pharmacotherapeutic group:Erectile dysfunction remedy - PDE5-inhibitor
    ATX: & nbsp

    G.04.B.E.08   Tadalafil

    Pharmacodynamics:

    Tadalafil is a reversible selective inhibitor of specific phosphodiesterase type 5 (PDE-5) cyclic guanosine monophosphate (cGMP). When sexual stimulation causes local release of nitric oxide, inhibition of PDE-5 with tadalafil leads to an increase in the concentration of cGMP in the cavernous body of the penis.The consequence of this is the relaxation of the smooth muscles of the arteries and the flow of blood to the tissues of the penis, which causes an erection. Tadalafil does not have an effect in the absence of sexual arousal.

    Research in vitro showed that tadalafil is a selective PDE-5. PDE-5 is an enzyme found in the smooth muscles of the cavernous body, in the smooth muscles of the vessels of internal organs, in skeletal muscles, platelets, kidneys, lungs and the cerebellum. The effect of tadalafil on PDE-5 is more active than on other phosphodiesterases. Tadalafil is 10,000 times more potent for PDE-5 than for PDE-1, PDE-2, PDE-4 and PDE-7, which are located in the heart, brain, blood vessels, liver, leukocytes, skeletal muscles and in other organs. Tadalafil 10,000 times more actively blocks PDE-5 than PDE-3 - an enzyme that is found in the heart and blood vessels. This selectivity for PDE-5 in comparison with PDE-3 is important, since PDE-3 is an enzyme involved in contraction of the heart muscle. Besides, tadalafil approximately 700 times more active against PDE-5 than with PDE-6, found in the retina and responsible for photo transmission. Tadalafil also exhibits an effect of 9000 times more potent on PDE-5 than its effect on PDE-8, PDE-9 and PDE-10, and 14-fold more potent for PDE-5 compared with PDE-11. The distribution in tissues and the physiological effects of the inhibition of PDE-8-PDE-11 have not yet been elucidated.

    Tadalafil improves an erection and increases the possibility of a full sexual intercourse.

    The drug is valid for 36 hours. The effect is manifested the same after 16 minutes after taking the drug in the presence of sexual arousal.

    Tadalafil in healthy individuals does not cause a significant change in systolic arterial and diastolic blood pressure compared to placebo in the supine position (the mean maximum decrease is 1.6 / 0.8 mm Hg, respectively) and in the standing position (the mean maximum decrease is 0 , 2 / 4.6 mm Hg, respectively). Tadalafil does not cause a significant change in heart rate. Tadalafil does not cause changes in color recognition (blue / green), which is explained by its low affinity for PDE-6. In addition, there is no effect of tadalafil on visual acuity, electroretinogram, intraocular pressure and pupil size.

    To assess the effect of daily administration of tadalafil on spermatogenesis, several studies have been carried out. None of the studies showed an undesirable effect on the morphology of spermatozoa and their mobility. In one study, a decrease in the average concentration of spermatozoa was found compared with placebo. Reducing the concentration of spermatozoa was associated with a higher incidence of ejaculation. In addition, there was no adverse effect on the average concentration of sex hormones, testosterone, luteinizing hormone and follicle-stimulating hormone when taking tadalafil.

    Pharmacokinetics:

    Suction

    After taking the drug inside tadalafil quickly absorbed. The mean maximum concentration (CmOh) in the blood plasma is achieved on average 2 hours after ingestion. The speed and degree of absorption of tadalafil do not depend on the time of ingestion, so the drug Cupid 36 can be used regardless of the time of meal. The time of administration (morning or evening) had no clinically significant effect on the rate and degree of absorption. The pharmacokinetics of tadalafil in healthy individuals is linear in time and dose.In the dose range from 2.5 to 20 mg, the area under the concentration-time curve (AUC) increases in proportion to the dose. Equilibrium concentrations in the plasma are reached within 5 days after taking the drug once a day. The pharmacokinetics of tadalafil in patients with an erection disorder is similar to the pharmacokinetics of a drug in persons without erectile dysfunction.

    Distribution

    The average volume of distribution is about 63 liters, which indicates that tadalafil is distributed in the tissues of the body. In therapeutic concentrations, 94% of tadalafil in the plasma binds to proteins. Binding to proteins does not change with impaired renal function. In healthy subjects, less than 0.0005% of the administered dose is found in semen.

    Metabolism

    Tadalafil is mainly metabolized with the participation of isoenzyme CYP3A4 cytochrome P450. The main circulating metabolite is methylcatechol glucuronide. This metabolite is at least 13,000 times less active against PDE5 than tadalafil. Consequently, the concentration of this metabolite is not clinically significant.

    Excretion

    In healthy individuals, the average clearance of tadalafil with oral administration is 2.5 l / h, and the average T1/2 - 17.5 h. Tadalafil is excreted mostly in the form of inactive metabolites, mainly through the intestine (about 61% of the dose) and, to a lesser extent, by the kidneys (about 36% of the dose).

    Special Populations

    Elderly patients

    Healthy elderly patients (65 years and over) had a lower clearance of tadalafil for oral administration, which was expressed by an increase in the area under the concentration-time curve by 25% compared with healthy individuals aged 19 to 45 years. This difference is not clinically significant and does not require dose selection.

    Patients with renal insufficiency

    In persons with renal insufficiency, including patients on hemodialysis, the area under the concentration-time curve was larger than in other healthy individuals.

    Patients with hepatic insufficiency

    The pharmacokinetics of tadalafil in patients with mild and moderate hepatic insufficiency is comparable to that of healthy individuals. For patients with severe hepatic insufficiency (class C according to the Child-Pugh classification), no data are available.

    Patients with diabetes mellitus

    In patients with diabetes mellitus against the background of tadalafil, the area under the concentration-time curve was less by about 19% than in healthy individuals.This difference does not require a dose adjustment.

    Indications:Erectile disfunction.
    Contraindications:

    - Hypersensitivity to tadalafil or to any substance included in the preparation;

    - in the case of taking drugs containing any organic nitrates;

    - age to 18 years;

    - severe degree of renal failure;

    - simultaneous use with stimulators of guanylate cyclase, such as riotsiguat;

    - the presence of contraindications to sexual activity in patients with diseases of the cardiovascular system: myocardial infarction during the last 90 days, unstable angina, the onset of angina pectoris during intercourse, chronic heart failure II-IV Classes by classification NYHA, uncontrolled arrhythmias, arterial hypotension (BP less than 90/50 mmHg), uncontrolled hypertension, ischemic stroke during the last 6 months;

    - loss of vision due to non-arterial anterior ischemic neuropathy of the optic nerve (regardless of the connection with the intake of PDE-5 inhibitors);

    - simultaneous administration of doxazosin, as well as drugs for the treatment of erectile dysfunction;

    - often (more than 2 times a week) use in patients with chronic renal failure (creatinine clearance less than 30 ml / min);

    - deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.

    Carefully:

    Since there is no data for patients with severe hepatic impairment (Child-Pugh class C), caution should be exercised in prescribing the drug Cupid 36 this group of patients.

    Care should be taken when prescribing the drug Cupid 36 patients receiving alpha [1] -adrenoceptor blockers, for example doxazosin, because simultaneous application can lead to symptomatic hypotension in some patients. In the study of clinical pharmacology, 18 healthy volunteers taking a single dose of tadalafil did not experience symptomatic hypotension with simultaneous administration of tamsulosin, alpha [1A] -adrenoconvertor (see "Interaction with Other Drugs").

    The potential risk of complications associated with sexual activity in patients with cardiovascular disease (myocardial infarction within the last 90 days, unstable angina or angina pectoris,arising during sexual intercourse; Heart failure class 2 and higher by NYHA, developed during the last 6 months; uncontrolled disturbances of the heart rhythm; arterial hypotension (BP less than 90/50 mm Hg) or uncontrolled hypertension; stroke, lasting for the last 6 months).

    Cupid 36 should be used with caution in patients with severe renal failure (CK less than 30 ml / min), CRF (CK less than 50 ml / min), predisposition to priapism (in sickle cell anemia, multiple myeloma or leukemia) or in patients with anatomical deformity the penis (angular curvature, cavernous fibrosis or Peyronie's disease).

    Pregnancy and lactation:A drug Cupid 36 not suitable for use in women.
    Dosing and Administration:

    Inside, (at least 16 minutes before the alleged sexual activity).

    The recommended maximum dose of the drug Cupid 36 is 20 mg. The maximum recommended frequency of reception is 1 time / day.

    Patients can attempt to have intercourse at any time within 36 hours after taking the drug in order to establish the optimal response time for taking the drug.

    Side effects:

    Adverse reactions occurring more often than in single cases are listed according to the following gradation: very often (≥ 10%); often (≥ 1%, <10%); infrequently (≥ 0.1%, <1%); rarely (≥ 0.01%, <0.1%); very rarely (<0.01%), it is not known (it is impossible to estimate the frequency of occurrence of reactions according to available data).

    Immune system disorders

    Infrequently (≥0,1%, <1%): hypersensitivity reactions.

    Disturbances from the nervous system

    Very often (≥ 10%): headache

    Often (≥1%, <10%): dizziness

    Rarely (≥0,01%, <0,1%): stroke (including acute disorders of cerebral circulation by hemorrhagic type), fainting1, transient ischemic attacks1, migraine3, epileptic seizure, transient amnesia.

    Vision disorders

    Infrequently (≥0,1%, <1%): blurred vision, pain in the eyeball.

    Rarely (≥0,01%, <0,1%): violation of visual fields, eyelid swelling, injection of vessels of the sclera of the eyeball, non-arterial anterior ischemic optic neuropathy3, occlusion of the vessels of the retina3.

    Hearing disorders and labyrinthine disorders

    Rarely (≥0,01%, <0,1%): sudden hearing loss2.

    Disorders from the cardiovascular system

    Infrequent (≥ 0.1%, <1%): palpitations, tachycardia, lower blood pressure (in patients who have already taken antihypertensives), increased blood pressure.

    Rarely (≥0.01%, <0.1%): myocardial infarction, ventricular arrhythmias3, unstable angina3.

    Disturbances from the respiratory system

    Often (≥ 1%, <10%): nasal congestion.

    Infrequently (≥ 0.1%, <1%): shortness of breath.

    Rarely (≥ 0.01%, <0.1%): nasal bleeding.

    Violations from hand gastrointestinal tract

    Often (≥ 1%, <10%): indigestion.

    Infrequently (≥ 0.1%, <1%): abdominal pain, gastroesophageal reflux.

    Disturbances from the skin and subcutaneous tissues

    Infrequently (≥ 0.1%, <1%): skin rash, hyperhidrosis (increased sweating).

    Rarely (≥ 0.01%, <0.1%): hives, Stevens-Johnson syndrome3, exfoliative dermatitis3.

    Disturbances from musculoskeletal and connective tissue

    Often (≥ 1%, <10%): back pain, myalgia.

    Violations of the genitals and mammary gland

    Rarely (≥ 0.01%, <0.1%): prolonged erection, priapism3.

    General disorders

    Infrequently (≥ 0.1%, <1%): chest pain1.

    Rarely (≥ 0.01%, <0.1%): swelling of the face3 , sudden cardiac death1,3.

    (1) They were observed in patients who previously had cardiovascular risk factors.However, it is impossible to determine precisely whether these phenomena are directly related to these risk factors, with tadalafil, with sexual arousal, or with a combination of these or other factors.

    (2) On sudden hearing loss has been reported in a small number of cases of post-marketing and clinical studies with the use of PDE5 inhibitors, including tadalafil.

    (3) Adverse reactions found during post-marketing research are not observed in a clinical placebo-controlled study.

    Overdose:

    With single assignment healthy persons tadalafil at a dose of 500 mg and patients with erectile dysfunction - repeatedly to 100 mg / day undesirable effects were the same as in the application of lower doses. In case of an overdose, standard symptomatic treatment should be performed. With hemodialysis tadalafil almost not output.

    Interaction:

    The effect of other drugs on tadalafil

    Tadalafil is mainly metabolized with the enzyme CYP3A4. Selective inhibitor CYP3A4, ketoconazole in a dose of 400 mg / day increases the exposure of a single dose of tadalafil (AUC) by 312% and CmOh - by 22%, and ketoconazole (200 mg / day) increases the exposure of a single dose of tadalafil (AUC) by 107% and CmOh by 15% relative to AUC and the quantities CmOh only for one tadalafil.

    Ritonavir (200 mg twice daily), inhibitor of isoenzymes CYP3A4, 2C9, 2C19 and 2D6 increases the exposure of a single dose of tadalafil (AUC) by 124% without change Cmax. Although specific interactions have not been studied, it can be assumed that other HIV protease inhibitors, such as, for example, saquinavir, as well as inhibitors of isoenzyme CYP3A4, such as erythromycin and intraconazole, increase the activity of tadalafil.

    Selective inductor of isoenzyme CYP3A4, rifampicin (600 mg per day), reduces the exposure of a single dose of tadalafil (AUC) by 88% and CmOh by 46%, relatively AUC and the quantities CmOh only for one tadalafil. It can be assumed that the simultaneous introduction of other isoenzyme inducers CYP3A4 should also reduce the concentration of tadalafil in plasma.

    Simultaneous intake of antacid (magnesium hydroxide / aluminum hydroxide) and tadalafil reduces the rate of absorption of the latter without changing the area under the pharmacokinetic curve for tadalafil.

    Increase in the pH of the contents of the stomach as a result of taking a blocker of histamine H2-nizatidine receptors do not influence the pharmacokinetics of tadalafil.

    The safety and efficacy of the combination of tadalafil with other treatments for erectile dysfunction have not been studied, so the use of such combinations is not recommended.

    Effect of tadalafil on other drugs

    Tadalafil enhances the hypotensive effect of nitrates. This is due to the additive effect of nitrates and tadalafil on the metabolism of nitric oxide and cGMP. Therefore, the drug administration Cupid 36 against the background of the use of nitrates is contraindicated.

    Tadalafil does not have a clinically significant effect on the clearance of drugs whose metabolism occurs with the participation of cytochrome P450. The studies confirmed that tadalafil Does not inhibit or induce isoenzymes CYP3A4, CYP1A2, CYP2D6, CYP2E1,CYP2C9, CYP2C19.

    Tadalafil does not have a clinically significant effect on the pharmacokinetics S-and R/ RTI & gt; Tadalafil does not affect the effect of warfarin on prothrombin time.

    Tadalafil does not increase the duration of bleeding against the background of the action of acetylsalicylic acid.

    Tadalafil has systemic vasodilating properties and can enhance the effect of antihypertensive drugs aimed at lowering blood pressure.In addition, for patients taking several antihypertensive drugs, in which hypertension was poorly controlled, there was a slightly greater decrease in blood pressure. In the vast majority of patients, this decrease was not associated with hypotensive symptoms. Patients receiving treatment with antihypertensive drugs and taking tadalafil, appropriate clinical recommendations should be given.

    There was no significant decrease in blood pressure when tadalafil was used by persons who took selective alpha [1A] -adrenoblocker tamsulosin.

    When using tadalafil by healthy volunteers who took doxazosin (4-8 mg per day), alpha [1] -adrenoceptor, increased antihypertensive effect of doxazosin. Some patients experienced symptoms associated with lowering blood pressure including fainting.

    Tadalafil did not affect the concentration of alcohol, nor did alcohol influence the concentration of tadalafil. At high doses of alcohol (0.7 g / kg), admission tadalafil not caused a statistically significant decrease in the average blood pressure.

    In some patients, postural dizziness and orthostatic hypotension were observed.

    When taking tadalafil in combination with lower doses of alcohol (0.6 g / kg), the reduction in blood pressure was not observed, and dizziness occurred with the same frequency as with the intake of alcohol alone.

    Tadalafil does not have a clinically significant effect on the pharmacokinetics and pharmacodynamics of theophylline.

    Special instructions:

    Sexual activity has a potential risk for patients with cardiovascular disease. Therefore, the treatment of erectile dysfunction, including with the drug Cupid 36, It should not be done in men with heart diseases in which sexual activity is not recommended.

    There are reports of the occurrence of priapism in the use of PDE-5 inhibitors, including tadalafil. Patients should be informed of the need to seek immediate medical attention in the event of an erection lasting 4 hours or more. Untimely treatment of priapism leads to damage to the tissues of the penis, resulting in a long-term loss of potency.

    Safety and efficacy of the drug combination Cupid 36 with other types of treatment, violations have not been studied. Therefore, the use of such combinations is not recommended. Like other PDE-5 inhibitors, tadalafil has systemic vasodilator properties, which can lead to a transient decrease in blood pressure. Before prescribing the drug Cupid 36 physicians should carefully consider whether patients with cardiovascular disease will be exposed to undesirable effects due to such vasodilating effects.

    Non-arterial anterior ischemic optic neuropathy (NAPION) is the cause of visual impairment, including complete loss of vision. There are rare post-marketing reports on cases of development of NAPION, in time associated with the intake of PDE-5 inhibitors. It is currently impossible to determine whether there is a direct link between the development of NAPION and the intake of PDE5 inhibitors or other factors. Doctors should recommend patients in case of sudden loss of vision stop taking tadalafil and seek medical help. Doctors should also tell patients that people who have undergone NAPION have a higher risk of re-developing NAPION.

    Effect on the ability to drive transp. cf.and fur:Despite the fact that the incidence of dizziness against the background of placebo and tadalafil is the same, during the treatment period it is necessary to be cautious when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:Tablets, film-coated, 20 mg.
    Packaging:

    For 1 or 2 tablets in a blister of PVC / PVDC / Al.

    For 1 or 2 or 4 blisters together with instructions for use in a cardboard box.

    Storage conditions:

    In a dry, the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.
    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-003944
    Date of registration:08.11.2016
    Expiration Date:08.11.2021
    The owner of the registration certificate:Cadil Pharmaceuticals Co., Ltd.Cadil Pharmaceuticals Co., Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspCADILA PHARMACEUTICALS LTD. CADILA PHARMACEUTICALS LTD. India
    Information update date: & nbsp07.02.2018
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