Cialis

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Cialis: 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. Drug interactions
14. Analogs
15. Terms and conditions of storage
16. Terms of dispensing from pharmacies
17. Reviews
18. Price in pharmacies

Latin name: Cialis

ATX code: G04BE08

Active ingredient: Tadalafil (Tadalafil)

Producer: Eli Lilly and Company, Great Britain, Eli Lilly Vostok SA, Switzerland, Eli Lilly Nederland B. V., The Netherlands

Description and photo update: 2019-12-08

Prices in pharmacies: from 1006 rubles.

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Cialis is a drug that helps to relax the smooth muscles of the arteries, thereby increasing the blood flow to the tissues of the penis and increasing the likelihood of achieving and maintaining an erection sufficient for sexual intercourse; ineffective in the absence of sexual arousal.

Release form and composition

Dosage form of Cialis - film-coated tablets:

2.5 mg: almond-shaped, light yellow-orange film shell; on one side of engraving - "C 2 ¹ / ₂ " (14 pieces in the blister, Al foil laminated and PVC / PE / PCTFE film;. 1 or 2 in the blister cardboard pack);
5 mg: almond-shaped, light yellow film coat; engraving "С 5" on one side (14 pcs. in a blister; 1 or 2 blisters in a cardboard box);
20 mg: almond-shaped, yellow film coat; engraving on one side - "C 20" (1 pc. in a blister, 1 blister in a cardboard box; 2 pcs. in a blister, 1, 2 or 4 blisters in a cardboard box).

Composition of 1 tablet:

active substance: tadalafil - 2.5 / 5/20 mg;
auxiliary components: hyprolose (hydroxypropyl cellulose), lactose monohydrate, MCC (microcrystalline cellulose), croscarmellose sodium, sodium lauryl sulfate, magnesium stearate;
film shell: yellow opadry [triacetin, hypromellose, lactose monohydrate, titanium dioxide, iron dye red oxide (for tablets 2.5 mg), iron dye yellow oxide].

Pharmacological properties

Pharmacodynamics

Tadalafil is a reversible selective inhibitor of the specific PDE-5 (phosphodiesterase type 5) cGMP (cyclic guanosine monophosphate). With sexual arousal, a local release of nitric oxide occurs, which leads to the suppression of PDE-5 by tadalafil and an increase in the level of cGMP in the corpus cavernosum. As a result of this action, the smooth muscles of the arteries relax, and blood flows to the tissues of the penis, which leads to an erection. In the absence of sexual arousal, tadalafil does not show its effect.

PDE-5 is present not only in the smooth muscles of the corpus cavernosum, but also in skeletal muscles, in the walls of the vessels of internal organs, lungs, kidneys, platelets and cerebellum. On phosphodiesterases of other types, tadalafil acts much less actively. Its effect on PDE-5 is 10,000 times stronger than on PDE-1, PDE-2, PDE-4 and PDE-7, localized in the brain, heart, liver, skeletal muscles, blood vessels, leukocytes and other organs. This selectivity of tadalafil is very important, since other phosphodiesterases (except PDE-5) are involved in vital processes in the body. The activity of tadalafil is 700 times higher in relation to PDE-5 than to PDE-6, and 9000 times more potent in relation to PDE-5 compared to the effect on PDE-8, PDE-9 and PDE-10. In comparison with PDE-11, the activity is 14 times higher.

Cialis improves erection and increases the likelihood of full intercourse.

In healthy individuals, there was no significant change in blood pressure compared with placebo in the standing and lying positions, as well as in heart rate. Tadalafil does not affect visual acuity, color recognition, pupil size, intraocular pressure and electroretinogram.

The drug does not affect the morphology and motility of spermatozoa. Only one study reported a decrease in mean sperm concentration compared with placebo, which was associated with increased ejaculation. Cialis also does not affect the average concentrations of sex hormones, follicle-stimulating hormone, luteinizing hormone and testosterone.

In the course of clinical studies, when using the drug once a day, an improvement in erection was observed with all degrees of severity of erectile dysfunction.

Pharmacokinetics

Tadalafil is rapidly absorbed after oral administration of the tablets. The degree and speed of absorption does not depend on food intake, as well as the time of taking the drug (morning or evening). The maximum plasma concentration of tadalafil is reached after about 2 hours.

The AUC (area under the concentration-time curve) of tadalafil in the dose range of 2.5–20 mg increases in proportion to the dose. After 5 days of a single daily intake of Cialis, equilibrium plasma concentrations of tadalafil are achieved.

Pharmacokinetic parameters of the drug in patients with erectile dysfunction are similar to those in healthy individuals without erectile dysfunction.

Tadalafil is distributed into body tissues. The average volume of distribution is about 63 liters. Tadalafil is 94% bound to plasma proteins (with impaired renal function, this indicator does not change). Less than 0.0005% of the dose taken is found in semen in healthy individuals.

As a result of the metabolism of tadalafil, methylcatecholglucuronide (the main circulating metabolite) is formed. Its activity is 13,000 times lower than that of tadalafil, so the concentration of this metabolite is of no clinical significance.

The half-life is 17.5 hours on average. About 61% of the dose taken is excreted in the feces and about 36% in the urine (the drug is mainly excreted in the form of inactive metabolites).

Indications for use

Cialis is indicated for the treatment of erectile dysfunction in adult men.

Contraindications

Absolute:

concomitant use with doxazosin and other drugs for the treatment of erectile dysfunction;
simultaneous reception with drugs containing any organic nitrates;
pathologies of the cardiovascular system in which sexual activity of patients is undesirable [unstable angina, myocardial infarction within the last 3 months, ischemic stroke during the last 6 months, attacks of angina pectoris during intercourse, CHF (chronic heart failure) according to NYHA classification - II- IV classes, arterial hypotension with a decrease in blood pressure (BP) ≤90/50 mm Hg. Art., uncontrolled arterial hypertension, uncontrolled arrhythmias];
atrophy of the optic nerve and loss of vision due to acute ischemia of the anterior segment of the optic nerve (regardless of whether the condition has been identified with the intake of PDE-5 inhibitors);
chronic renal failure with CC (creatinine clearance) ≤30 ml / min with frequent (more than 2 times a week) use;
lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
children and adolescents up to 18 years old;
hypersensitivity to tadalafil or other substances that make up the drug.

Relative (Cialis is taken with caution, due to the increased likelihood of complications):

severe hepatic impairment of class C on the Child-Pugh scale (there is not enough research data on the use of the drug in this category of patients);
simultaneous reception with α ₁ -adrenergic blockers (in some cases, it can cause symptomatic arterial hypotension);
simultaneous administration with antihypertensive drugs and strong inhibitors of the isoenzyme CYP3A4 (saquinavir, ritonavir, ketoconazole, erythromycin, itraconazole);
predisposition to priapism, which develops as a result of sickle cell anemia, leukemia, multiple myeloma;
anatomical deformity of the penis (cavernous fibrosis, Peyronie's disease, angular curvature).

When diagnosing erectile dysfunction, it is necessary to identify the main potential cause of the pathology in order to conduct an appropriate examination of the patient and determine the tactics of treatment and the most likely contraindications.

Instructions for the use of Cialis: method and dosage

Cialis tablets are taken orally, regardless of food intake, but no later than 16 minutes before the planned sexual activity.

Recommended dosage regimen:

frequent sexual activity (> 2 times a week): 5 mg per day for 1 dose, at the same time; depending on the individual tolerance of the drug, it is possible to reduce the daily dose to 2.5 mg;
infrequent sexual activity (<2 times a week): 20 mg per dose, immediately before the intended sexual activity.

The maximum dose of tadalafil per day is 20 mg.

During 36 hours from the use of Cialis at any convenient time, you can attempt intercourse in order to determine the optimal response time to taking the pill.

Side effects

Side effects manifested more often than in single episodes (according to the following gradation: ≥10% - very often; ≥1% - <10% - often; ≥0.1– <1% - infrequently; ≥0.01– <0, 1% - rarely; <0.01% - very rare; frequency unknown - according to the available data, it is impossible to estimate the frequency of reactions):

nervous system: very often - headache; often - dizziness; rarely - stroke, including stroke (acute cerebrovascular accident) of hemorrhagic type, TIA (transient ischemic attacks) ¹, transient amnesia, fainting ¹, migraine ³, epileptic seizures;
organ of vision: infrequently - pain in the eyeball, blurred vision; rarely - swelling of the eyelids, impaired visual fields, non-arterial anterior ischemic optic neuropathy ³, injection of the vessels of the sclera of the eyeball, impaired patency (occlusion) of the retinal vessels ³;
immune system: infrequently - allergic reactions;
organ of hearing and labyrinthine disorders: rarely - sudden deafness ²;
CVS (cardiovascular system): infrequently - tachycardia, sudden palpitations, increased blood pressure, decreased blood pressure (in patients taking antihypertensive drugs); rarely - ventricular rhythm disturbances ³, myocardial infarction, unstable angina pectoris ³;
respiratory system: often - dry nasal congestion; infrequently - shortness of breath; rarely - epistaxis (nosebleed);
Gastrointestinal tract (gastrointestinal tract): often - indigestion; infrequently - gastroesophageal reflux, abdominal pain;
skin and subcutaneous tissue: infrequently - hyperhidrosis, rash; rarely - Stevens-Johnson syndrome ³, exfoliative dermatitis ³, urticaria;
musculoskeletal and connective tissue: often - myalgia, back pain;
genitals and mammary gland: rarely - priapism ³, prolonged erection;
general disorders: infrequently - chest pain ¹; rarely - facial edema ³, sudden cardiac death ^1.3.

Notes

1 - were recorded in patients with a history of cardiovascular risk factors. But it is not possible to determine reliably whether these reactions are directly related to previously observed risk factors, to the patient's sexual arousal, to taking tadalafil, or to a combination of existing or other factors.

2 - sudden hearing loss was recorded in several cases during post-marketing and clinical studies of the use of all PDE-5 inhibitors, including tadalafil.

3 - adverse reactions recorded during post-marketing studies, but not observed in clinical placebo-controlled studies.

Overdose

When taking tadalafil in doses up to 500 mg per day once (in healthy individuals) and in doses up to 100 mg per day multiple times (in persons with erectile dysfunction), the undesirable effects of Cialis were similar to those that occur when taking lower doses.

In case of an overdose of the drug, standard symptomatic therapy is prescribed. Hemodialysis is practically ineffective.

special instructions

There is evidence of cases of priapism due to the use of PDE-5 inhibitors, including tadalafil. It is required to notify patients of the need to immediately seek medical attention for an erection lasting more than 4 hours. Failure to treat priapism can damage the tissues of the penis, resulting in irreversible impotence.

NAPION (non-arterial anterior ischemic optic neuropathy) is the cause of visual impairment, up to and including its complete loss. There are rare data of post-marketing observations about the episodes of the development of NAPION, associated in time with therapy with PDE-5 inhibitors. Today it is impossible to determine whether the development of NAPION and the intake of PDE-5 inhibitors directly depends, or other factors affect. Patients with sudden loss of vision are required to immediately stop taking tadalafil and seek help from specialists. It should be borne in mind that if there is a history of NAPION data, the risk of re-development is increased.

There is no data on the effectiveness of the use of Cialis in patients after surgery on the pelvic organs and / or radical neurosaving prostatectomy.

The incidence of dizziness during therapy with tadalafil and when taking placebo is the same. Despite this, during treatment, care should be taken when driving vehicles and engaging in other potentially hazardous activities that require quick psychomotor reactions and increased concentration of attention.

Application during pregnancy and lactation

Cialis is used only in men. The drug is not intended for use in women.

Pediatric use

According to the instructions, Cialis is prohibited from prescribing to children and adolescents under 18 years of age.

With impaired renal function

In case of severe renal failure, the use of Cialis is possible only in cases of extreme necessity and with special care.

In moderate renal failure (with creatinine clearance of 31-50 ml / min), back pain was observed more often than in patients with mild renal insufficiency (creatinine clearance 51-80 ml / min) or healthy volunteers.

With a creatinine clearance of 50 ml / min or less, Cialis is prescribed with caution.

For violations of liver function

In case of severe hepatic failure, Cialis tablets are used with extreme caution and only in cases of extreme necessity.

Drug interactions

Cialis is metabolized mainly with the participation of the CYP3A4 enzyme, which results in an effect on tadalafil when the following substances / drugs are used together:

ketoconazole: enhances the effects of tadalafil;
ritonavir and, presumably, other HIV protease inhibitors (saquinavir) and CYP3A4 inhibitors (erythromycin and itraconazole): increase the activity of tadalafil;
rifampin (rifampicin): reduces the concentration of tadalafil in plasma;
antacids (magnesium hydroxide, aluminum hydroxide): reduce the rate of its absorption without changing the AUC;
nizatidine (H ₂ antagonist that increases the pH of gastric juice): has no effect on the pharmacokinetics of tadalafil;
other drugs for the treatment of erectile dysfunction: interaction with Cialis has not been studied, but the use of such combinations is not recommended.

The effect of tadalafil on other substances / drugs in combined use:

nitrates: their hypotensive effect is enhanced; Cialis therapy is contraindicated against the background of the use of nitrates;
drugs metabolized with the participation of cytochrome P450 isoenzymes: tadalafil does not induce or inhibit cytochrome isoenzymes, as a result of which it does not have a clinically significant effect on the clearance of these drugs;
warfarin: tadalafil has no effect on its effectiveness;
acetylsalicylic acid: the duration of bleeding does not increase;
antihypertensive drugs: due to the systemic vasodilating properties of tadalafil, it is possible to enhance the effect of antihypertensive drugs, aimed at lowering blood pressure; with this combination, patients should be given appropriate recommendations for joint therapy;
tamsulosin (selective α ₁ A-blocker): no significant decrease in blood pressure (when using tadalafil in healthy individuals) was not observed;
doxazosin (α ₁ -adrenergic blocker): the hypotensive effect of doxazosin increases, manifested by a decrease in blood pressure, up to fainting;
theophylline: there is no clinically significant effect on pharmacokinetics and pharmacodynamics;
ethanol: no mutual influence of alcohol (at a dose of up to 0.6 g / kg) with tadalafil was observed; high doses of alcohol (> 0.7 g / kg) did not produce a significant decrease in the mean blood pressure, but some patients had orthostatic hypotension and postural dizziness.

Analogs

Analogues of Cialis are: Afalaza, Viagra, Verona, Vizarsin, Viasan-LF, Zydena, Impaza, Yohimbine hydrochloride, Dynamico, Maxigra, Tornetis, Sirbida, Silafil, Sildenafil, Cialis Forte, Cialis Soft, Cialis Capsules, Raylis

Terms and conditions of storage

Store at a temperature not exceeding 30 ° C. Keep out of the reach of children.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Cialis

Positive reviews about Cialis on the forums are confirmed by the results of clinical studies. So, when taking the drug at a dose of 20 mg, 81% of patients with varying degrees of severity of erectile dysfunction showed an improvement in potency.

Despite the good tolerance of Cialis, some reviews mentioned side effects such as headache, dizziness, heartburn, back pain and muscle pain. In some reports, there was information that the morning after taking the pills, there was a sensation similar to an alcoholic hangover.

Before using the drug, you must carefully read the instructions, and also remember that in the absence of sexual arousal, Cialis is ineffective, since it only provides blood flow to the genitals, but does not cause arousal.

Price for Cialis in pharmacies

The drug is quite expensive. In pharmacies, prices for Cialis fluctuate in the following ranges:

film-coated tablets, 5 mg (14 pcs. in a package) - 2,800-4,000 rubles;
film-coated tablets, 5 mg (28 pcs. in a package) - 5420-6990 rubles;
film-coated tablets, 20 mg (1 pc. in a package) - 955-1300 rubles;
film-coated tablets, 20 mg (2 pcs. in a package) - 1840–2590 rubles.
film-coated tablets 20 mg (4 pcs. in a package) - 3035-3990 rubles;
film-coated tablets 20 mg (8 pcs. in a package) - 5670–7140 rubles.

Cialis: prices in online pharmacies

Drug name

Price

Pharmacy

Cialis tablets 20mg 1 pc.

RUB 1006

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Cialis 20 mg film-coated tablets 1 pc.

RUB 1006

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Cialis 20 mg film-coated tablets 2 pcs.

1600 RUB

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Cialis tablets 20mg 2 pcs.

2141 RUB

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Cialis 5 mg film-coated tablets 14 pcs.

RUB 3092

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Cialis tablets 5mg 14 pcs.

3320 RUB

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Cialis 20 mg film-coated tablets 4 pcs.

3337 RUB

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Cialis tablets 20mg 4 pcs.

3510 RUB

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Cialis 5 mg film-coated tablets 28 pcs.

RUB 5657

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Cialis 20 mg film-coated tablets 8 pcs.

5698 RUB

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Cialis tablets 20mg 8 pcs.

RUB 6167

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Cialis tablets 5mg 28 pcs.

RUB 6259

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Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, 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!