Kamagra (tablets, 100 mg)
International non-proprietary name
Tablets, film coated, 50 and 100 mg
One tablet contains
active ingredient - sildenafil citrate 70,250 / 140,500 mg equivalent
Sildenafil 50/100 mg
excipients: sodium starch glycolate (type A),
Povidone (PVPK 30), microcrystalline cellulose, purified talc,
shell: hypromellose, Instacoat Sol IC-S-3788 (green) 1, titanium
dioxide (E 171)
1 - The composition includes: hypromellose (USP *), polyethylene glycol (NFSHA *),
talc (USP *), brilliant blue E 133 (USP *), quinoline
yellow E 104 (USP *), titanium dioxide E 171 (USP *)
Tablets are green, diamond-shaped, film-coated, engraved with “ap” on one side and “KGR 50” on the other, from 11.4 to 11.6 mm long, 8.3 to 8.5 mm wide (for 50 mg dosage).
Tablets are green, diamond-shaped, film-coated, engraved with “ap” on one side and “KGR 100” on the other, 14.2 to 14.4 mm long, 10.2 to 10.4 mm wide (for a dosage of 100 mg).
Drugs for the treatment of erectile dysfunction. Sildenafil
ATX code G04BE03
The pharmacokinetics of sildenafil are dose dependent. After taking the drug inside the sildenafil is rapidly absorbed. Absolute bioavailability, on average, is 41%. After taking the drug on an empty stomach Cmax is achieved within 30 minutes. When taking sildenafil in combination with fatty foods, the absorption rate decreases; Tmax increases by 60 minutes, and Cmax decreases on average by 29%. 96% Sildenafil is bound to plasma proteins. Protein binding does not depend on the total concentration of sildenafil. Sildenafil is metabolized in the liver. The major circulating metabolite undergoes further metabolism. According to the selectivity of action, the metabolite is comparable to sildenafil, and its in vitro activity is about 50% of the activity of sildenafil itself. The concentration of the metabolite in plasma is approximately 40% of the concentration of sildenafil. Terminal T1 \ 2 is about 4 hours.
After ingestion or administration of intravenous administration, sildenafil is excreted as metabolites, mainly with feces (approximately 80%) and to a lesser extent with urine (approximately 13%).
Kamagra is a drug for the treatment of erectile dysfunction. Sildenafil citrate is a potent and selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE5). The physiological mechanism of penile erection involves the release of nitric oxide (NO) in the cavernous body during sexual stimulation.
Nitric oxide activates the enzyme guanylate cyclase, which leads to an increase in the level of cyclic guanosine monophosphate (cGMP), relaxation of the smooth muscles of the cavernous body and increased blood flow in the penis. When sexually aroused, the local release of NO under the influence of sildenafil leads to inhibition of PDE5 and an increase in cGMP level in the cavernous body, resulting in relaxation of smooth muscles and increased blood flow in the cavernous body. The use of sildenafil in the recommended doses is ineffective in the absence of sexual stimulation.
Kamagra does not affect visual acuity, sensitivity to contrast, intraocular pressure, or pupil diameter.
The drug at a dose of 100 mg does not affect the locomotor activity or morphology of spermatozoa when it is taken once.
Toxicological characteristics of the drug
The drug belongs to virtually non-toxic substances. Does not have irritant effects. It does not have a teratogenic and embryotoxic action, does not possess an immunotoxic and sensitizing effect.
Indications for use
- erectile dysfunction characterized by inability to achieving or maintaining an erection of the penis, sufficient for satisfactory sexual intercourse.
Kamagra is effective only in the presence of sexual stimulation.
Dosage and administration
In order to avoid complications, apply strictly as prescribed by a doctor!
Kamagra should be taken as needed approximately one hour before sexual intercourse. The recommended dose of the drug is 50 mg and taken before meals.
Based on the effectiveness and tolerability of the drug, its dose can be increased to 100 mg or reduced to 25 mg.
The maximum recommended dose of the drug is 100 mg.
The maximum recommended frequency of taking the drug is 1 time per day.
With mild and moderate degree of kidney failure (creatinine clearance 30-80 ml / min), the recommended dose adjustment is not required.
Due to the fact that in patients with severe impaired renal function (creatinine clearance <30 ml / min), the clearance of sildenafil is reduced, it is necessary in such cases to reduce the dose to 25 mg.
In patients with liver failure, the dose of Kamagra can be reduced to 25 mg.
Elderly patients do not require dose adjustment.
Kamagra is not indicated for use in patients under 18 years of age.
Use in patients taking other drugs
When combined with ritonavir, the maximum single dose of the drug should be 25 mg, no more than 1 time within 48 hours.
When used together with cytochrome P450 3A4 inhibitors (such as erythromycin, saquinavir, ketoconazole, itraconazole), the initial dose of the drug is 25 mg.
In order to reduce the risk of postural arterial hypotension in patients undergoing treatment with alpha blockers, the condition of patients receiving alpha blockers should be stabilized. In addition, you should consider the possibility of using the drug, starting with a dose of 25 mg.
- color distortions of vision (chloropsia, chromatopsia, cyanopsia, erythropsia, xantopsia), visual disturbances, blurred vision
- hyperemia, hot flashes
- nasal congestion
- dyspepsia, nausea
- drowsiness, hypesthesia
- disorders associated with lacrimation (dry eyes, dysfunction of the lacrimal gland, increased lacrimation), eye pain, photophobia, photopsia, vascular hyperemia of the eyes, brightness of visual perception, conjunctivitis
- spatial disorientation (vertigo), tinnitus
- tachycardia, palpitations
- arterial hypertension, arterial hypotension
- nosebleeds, nasal sinuses congestion
- pain in the upper abdomen, gastroesophageal reflux disease, vomiting, dry mouth
- myalgia, pain in the limbs
- chest pain, fatigue, feeling of heat
- increased heart rate
- acute violation of cerebral circulation, transient ischemic attack, convulsive seizure *, relapse of convulsive seizure *, syncope
- Anterior non-arteritis ischemic neuropathy of the optic nerve *, retinal vascular occlusion *, retinal hemorrhage, arteriosclerotic retinopathy, retinal disease, glaucoma, visual field defect, diplopia, reduced visual acuity, myopia, asthenopia, floating body vitreous body organ, opacities, reduced opacities , presence of rainbow circles in the field of view, swelling of the eye, swelling of the eye, visual disturbance, conjunctival hyperemia, eye irritation, unusual sensation in the eye, eyelid edema, discoloration of the sclera
- Sudden cardiac death *, myocardial infarction, ventricular arrhythmia *, atrial fibrillation, unstable stenocardia
- feeling of tightness in the throat, swelling of the nose, dry nasal mucosa
- oral hypesthesia
- Stevens-Johnson syndrome *, toxic epidermal necrolysis *
- penis bleeding, priapism *, hematospermia, increased erection - irritability
* side effects registered only during post-registration observation.
Reporting information about suspected adverse reactions
Reporting information about suspected adverse reactions identified after registration of a drug is of great importance. This allows you to continue monitoring the ratio of the benefits and risks of the drug.
Medical professionals and patients are asked to report any adverse reactions at the address given at the end of this medical application.
- hypersensitivity to any component of the drug
- simultaneous administration of drugs that are nitric oxide donors (amyl nitrite) or nitrates in any form
- simultaneous reception with guanylate cyclase stimulants (riociguat)
- severe liver failure
- hereditary degenerative diseases of the retina (for example, hereditary retinitis pigmentosa (a small number of these patients have hereditary dysfunction of retinal phosphodiesterase))
- loss of vision in one eye due to anterior non-arteritis ischemic neuropathy of the optic nerve, regardless of whether this episode was associated with prior use of the PDE-5 inhibitor or not
- arterial hypotension (BP <90/50 mm Hg. Art.)
- severe cardiovascular diseases (for example, severe heart failure, unstable angina)
- myocardial infarction transferred in the last 6 months
- suffered a stroke in the last 6 months
- simultaneous use with CYP3A4 isoenzyme inhibitors (for example, ketoconazole, itraconazole, ritonavir, erythromycin, saquinavir, clarithromycin)
- simultaneous administration of drugs for the treatment of pulmonary arterial hypertension (bosentan, iloprost) and drugs containing sildenafil or any other PDE-5 inhibitor
- men with rare hereditary intolerance to galactose, Lapp's lactase deficiency or glucose and galactose malabsorption syndrome
- simultaneous use with other oral or topical treatments for erectile dysfunction
- anatomical deformity of the penis (including angulation, cavernous fibrosis or Peyronie’s disease)
- diseases that predispose to the development of priapism (such as sickle cell anemia (red blood cell abnormality), multiple myeloma (bone marrow cancer) or leukemia (blood cell cancer))
- problems with blood clotting (hemophilia)
- bleeding disorders
- acute gastric or duodenal ulcers
- simultaneous use with drugs of the alpha adrenergic blocking group
According to the registered indication, the drug is not intended for use in children and adolescents under the age of 18 years and in women.
Effect of other drugs on sildenafil
In vivo studies
While taking sildenafil with CYP3A4 inhibitors (such as ketoconazole, erythromycin and cimetidine), there is a decrease in the clearance of sildenafil. In this group of patients, there is no increased frequency of side effects, however, it is necessary to begin treatment with Kamagra in the initial dose of 25 mg
The simultaneous administration of HIV protease inhibitor ritonavir, which is a strong inhibitor of cytochrome P450, in equilibrium (500 mg twice a day) with sildenafil (100 mg in a single dose) leads to an increase in the maximum concentration (Cmax) of sildenafil by 300% (4 times), and also an increase in AUC of sildenafil in the blood plasma by 1000% (11-fold). After 24 hours, plasma levels of sildenafil are approximately 200 ng / ml compared to approximately 5 ng / ml after taking sildenafil alone. These data are consistent with the pronounced effects of ritonavir on a wide range of cytochrome P450 substrates. Based on the above data, the simultaneous use of sildenafil with ritonavir is not recommended.
Kamagra does not affect ritonavir pharmacokinetics.
The maximum dose of sildenafil should under no circumstances exceed 25 mg within 48 hours.
The simultaneous administration of HIV protease inhibitor saquinavir, which is a CYP3A4 inhibitor, in an equilibrium state (1200 mg three times a day) with sildenafil (100 mg single dose) leads to an increase in Cmax of sildenafil by 140%, as well as an increase in AUC of sildenafil by 210%. Sildenafil does not affect the pharmacokinetics of saquinavir. More potent CYP3A4 inhibitors, such as ketoconazole and itraconazole, have a more pronounced effect.
With a single dose of sildenafil in a dose of 100 mg together with erythromycin, a moderate CYP3A4 inhibitor, in equilibrium (500 mg twice a day for 5 days), an increase in systemic exposure to sildenafil is observed by 182% (determined by the AUC value).
Azithromycin (at a dose of 500 mg per day for 3 days) does not affect AUC, Cmax, Tmax rates, elimination rate constant, or the subsequent half-life of sildenafil or its main circulating metabolite.
Simultaneous use of cimetidine (800 mg), which is an inhibitor of cytochrome P450 and a nonspecific CYP3A4 inhibitor with sildenafil (50 mg dose) in healthy volunteers, causes an increase in plasma concentrations of sildenafil by 56%.
Grapefruit juice is a weak inhibitor of CYP3A4-mediated metabolism in the intestinal wall and can cause a moderate increase in plasma levels of sildenafil.
A single dose of antacid (magnesium hydroxide / aluminum hydroxide) does not affect the bioavailability of sildenafil.
Uniforms of a CYP2C9 inhibitor (tolbutamide, warfarin, and phenytoin); The receptors and inducers of the metabolic activity of P450 (rifampicin, barbiturates) do not affect the pharmacokinetics of sildenafil.
The simultaneous use of endothelin antagonist bosentan (moderate inducer CYP3A4, CYP2C9 and probably CYP2C19) in an equilibrium state (125 mg twice a day) with sildenafil in an equilibrium state (80 mg three times a day) leads to a decrease in AUC and Cmax for sildenafil by 62.6% and 55.4%, respectively. Thus, it is believed that the simultaneous use of strong inducers of CYP3A4, such as rifampin, causes a more pronounced decrease in plasma concentrations of sildenafil.
Concurrent use with other PDE-5 inhibitors or other treatments for erectile dysfunction
The safety and efficacy of using sildenafil in combination with other PDE-5 inhibitors or other drugs containing sildenafil for the treatment of pulmonary arterial hypertension (PAH) or other drugs for the treatment of erectile dysfunction have not been studied. In this regard, the use of such combinations of drugs is not recommended.
Nicorandil is a hybrid of potassium channel activator and nitrate. Due to the nitrate component, it is potentially capable of entering into serious interactions with sildenafil.
Effect of sildenafil on other drugs
In vitro studies
Data on the interaction of sildenafil with non-specific phosphodiesterase inhibitors, such as theophylline or dipyridamole, are not available.
In vivo studies
In accordance with the known effect of sildenafil on the NO / cGMP signaling pathway, sildenafil is capable of enhancing the hypotensive effect of nitrates, namely, a significant decrease in blood pressure. Therefore, its simultaneous use with nitric oxide donors (amyl nitrite) or nitrates in any form is contraindicated.
In clinical studies, riociguat increased the hypotensive effect of PDE-5 inhibitors. There was no evidence of a favorable clinical effect when using such a combination in the studied population. Simultaneous use of riociguat with PDE-5 inhibitors, including with sildenafil, is contraindicated.
Simultaneous reception with alpha-blockers
It is recommended that sildenafil be used with caution in patients taking the drug of the alpha-blocker group, since their simultaneous use can lead to symptomatic arterial hypotension in some sensitive patients. This is most likely to occur within 4 hours after taking a dose of sildenafil. To reduce the risk of postural hypotension, the hemodynamic stability of patients receiving treatment with alpha-blockers should be achieved before starting treatment with sildenafil. The possibility of using sildenafil, starting with a dose of 25 mg should be considered. In addition, physicians should instruct patients about the actions in case of symptoms of postural hypotension.
With simultaneous use of sildenafil and doxazosin in patients stabilized with doxazosin therapy, rare cases of symptomatic arterial hypotension, dizziness, and a faint state, but not fainting, have been reported.
With simultaneous use of sildenafil (50 mg dose) with tolbutamide (250 mg dose) or warfarin (40 mg dose), both of which are metabolized by CYP2C9, no significant interactions were detected.
Sildenafil (at a dose of 50 mg) does not contribute to an increase in bleeding time caused by the administration of acetylsalicylic acid (at a dose of 150 mg).
Sildenafil (at a dose of 50 mg) does not contribute to enhancing the hypotensive effect of alcohol in healthy volunteers with an average maximum blood alcohol level of 80 mg / dl.
Combination of the following classes of antihypertensive drugs: diuretics, beta-blockers, ACE inhibitors, angiotensin II antagonists, antihypertensive drugs (vasodilators and central action), adrenergic neuroblocking agents, calcium channel blockers and alpha-adrenoreceptor blockers - did not reveal differences taking sildenafil compared with patients receiving placebo. In special studies of drug interactions, during which sildenafil (at a dose of 100 mg) was used simultaneously with amlodipine in patients with arterial hypertension, an additional decrease in systolic blood pressure in the supine position was 8 mm. Hg Art. The corresponding additional decrease in diastolic blood pressure in the supine position was 7 mm. Hg Art. These additional reductions in blood pressure were similar in magnitude to those seen with sildenafil in healthy volunteers as monotherapy.
Sildenafil (at a dose of 100 mg) does not affect the pharmacokinetics in the equilibrium state of HIV protease inhibitors, saquinavir and ritonavir, both of which are substrates of CYP3A4.
When applied simultaneously with bosentan, sildenafil in equilibrium (80 mg three times a day) causes an increase in the AUC and Cmax of bosentan (125 mg twice a day) by 49.8% and 42%, respectively, in healthy male volunteers.
To diagnose erectile dysfunction, determine its possible causes and select an adequate treatment, it is necessary to collect a complete medical history and conduct a thorough physical examination.
Sexual activity poses a certain risk in the presence of heart disease, so before starting any therapy for erectile dysfunction, the doctor should conduct an examination of the cardiovascular system.
Preparations for the treatment of erectile dysfunction should not be given to men for whom sexual activity is undesirable.
During the post-registration period, cases of serious cardiovascular complications, including myocardial infarction, sudden cardiac death, ventricular arrhythmia, cerebrovascular bleeding and transient ischemic attack, during the use of sildenafil for the treatment of erectile dysfunction, have been reported. Most, but not all, of these patients had prior cardiovascular risk factors. Many of these phenomena were recorded during or shortly after the completion of sexual intercourse, and several phenomena were recorded shortly after taking sildenafil without sexual activity. Others took place a few hours or days after the application of sildenafil and sexual activity. It is not possible to determine whether these phenomena were directly related to the administration of sildenafil, to sexual activity, to an existing cardiovascular disease, to a combination of these factors, or to other factors.
Clinical studies have shown that sildenafil has a systemic vasodilating effect, leading to a transient decrease in blood pressure. In most patients, this has little or no effect. However, before prescribing sildenafil, doctors should carefully check the likelihood of undesirable effects of the vasodilator effect of this drug on the condition of patients with certain background diseases, especially in their combination with sexual activity. The group of hypersensitivity to vasodilators includes patients with narrowing of the left ventricular output (for example, aortic stenosis, hypertrophic obstructive cardiomyopathy), as well as patients with the rare syndrome of multiple systemic atrophy, manifested as a severe degree of dysregulation of blood pressure from the autonomic nervous system.
In rare cases, during post-registration use of all PDE-5 inhibitors, including sildenafil, non-arterial anterior ischemic optic neuropathy of the optic nerve (NPINZN), a rare disease and cause of loss or loss of vision have been reported. Most of these patients had risk factors such as: age over 50, optic nerve edema (congestive disc), diabetes, hypertension, coronary heart disease, hyperlipidemia, and smoking. In an observational study, it was evaluated whether the recent use of drugs of the FDE5 inhibitor class is associated with an acute onset of NPINSN. The results indicate an approximately 2-fold increase in the risk of NPINZN over a period of time equal to 5 half-lives of the PDE5 inhibitor. According to published literature data, the annual incidence of NPINSN is 2.5-11.8 cases per 100,000 men aged> 50 years in the general population. In case of unexpected deterioration or loss of vision, patients are advised to stop taking Kamagra and immediately consult with a physician. Individuals who have already had a case of an NPINZN have an increased risk of a recurrence of the NPINZN. Therefore, physicians should discuss this risk with such patients, as well as discuss the likelihood of adverse effects of PDE5 inhibitors on them. In these patients, PDE5 inhibitors, including Kamagra, are not recommended.
It is recommended that sildenafil be used with caution in patients taking the drug of the alpha-blocker group, since their simultaneous use can lead to symptomatic arterial hypotension in some sensitive patients. To reduce the risk of postural hypotension, patients who receive alpha-blockers should be stable before starting treatment with sildenafil. Consideration should be given to initiating treatment with low doses of sildenafil. In addition, physicians should advise patients what to do in case of symptoms of postural hypotension.
A small number of patients with hereditary retinitis pigmentosa have genetically determined abnormalities of retinal phosphodiesterase functions. There is no information about the safety of using sildenafil in patients with retinitis pigmentosa, so sildenafil should be used with caution.
In vitro studies using human platelets indicate that sildenafil enhances the antiaggregation effect of sodium nitroprusside (nitric oxide donor). There is no information about the safety of using sildenafil in patients with bleeding disorders or active peptic ulcer, so sildenafil should be used with caution.
Medications for the treatment of erectile dysfunction should be used with caution in patients with anatomical deformation of the penis (such as angulation, cavernous fibrosis or Peyronie's disease), as well as in patients with diseases predisposing to the development of priapism (such as sickle cell anemia, multiple myeloma or leukemia).
The safety and efficacy of using sildenafil in combination with other methods of treating erectile dysfunction has not been studied and the use of such combinations of drugs is not recommended.
Some post-marketing and clinical studies using all PDE-5 inhibitors, including sildenafil, have reported a sudden decrease or loss of hearing in patients. Most of these patients had risk factors for the development of this pathology. No causal relationship was found between the use of PDE-5 inhibitors and a sudden decrease or loss of hearing. Patients should be advised to discontinue sildenafil therapy in the event of a sudden decline or loss of hearing and consult a physician immediately.
Reproductive function, pregnancy and breastfeeding
Sildenafil is not indicated for use in women.
Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous machinery
While taking Kamagra, there was no adverse effect on the ability to drive a car or other technical equipment, however, given the side effects of the drug, caution should be exercised when driving vehicles or other potentially dangerous machinery.
When taking high doses of the drug may be increased side effects observed when taking the recommended doses. In case of overdose, general symptomatic and supportive treatment is prescribed.
Release form and packaging
On 4 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil lacquered printed.
On 1 planimetric packing together with the instruction for medical application in the state and Russian languages put in a pack from a cardboard.
Store in a dark place at a temperature not higher than 30 C.
Keep out of the reach of children!
Do not use after the expiration date!
Pharmacy sales terms
"Ajanta Pharma Limited"
Ajanta House, 98, Kandivli Cooperative Estate Limited,
Charkop, Kandivli (W), Mumbai 400067