Description
Composition Kamagra 100
active ingredient: sildenafil;
1 tablet contains sildenafil citrate in terms of sildenafil 50 mg or 100 mg
Auxiliary substances: microcrystalline cellulose, magnesium stearate, sodium starch (type A), povidone, talc, hypromellose, coating Instacoat Sol IC-S-3788 (green) *, titanium dioxide (E 171)
* Instacoat Sol IC-S-3788 (green): talcum, hypromellose, polyethylene glycol, titanium dioxide
(E 171), quinoline yellow (E 104), brilliant blue (E 133).
Dosage form
The tablets covered with a cover.
Basic physical and chemical properties:
diamond coated tablets, green, embossed “ar” on one side and “KGR 50” on the other;
diamond coated tablets, green, embossed “ar” on one side and “KGR 100” on the other.
Pharmacological group
Means used for erectile dysfunction. Sildenafil. ATX Code G04B E03.
Pharmacological properties
Pharmacodynamics .
Kamagra 100 is a drug for oral administration, intended for the treatment of erectile dysfunction. With sexual stimulation, the drug restores reduced erectile function by increasing the flow of blood to the penis.
A physiological mechanism that leads to an erection, including the release of nitric oxide (NO) in cavernous bodies during sexual arousal. The released nitric oxide activates the enzyme guanylate cyclase, which stimulates the increase in the level of cyclic guanosine monophosphate (cGMP), which, in turn, causes relaxation of the smooth muscles of the cavernous bodies, contributing to the influx of blood.
Kamagra 100 Sildenafil is a potent and selective inhibitor of cGMP-specific phosphodiesterase
5 (PDE-5) in cavernous bodies, where PDE-5 is responsible for the decay of cGMP. Effects of sildenafil on erection are peripheral. Sildenafil does not have a direct relaxing effect on isolated cavernous bodies of a person, but powerfully enhances the relaxing effect of NO on this tissue. When the metabolic pathway of NO / cGMP is activated, which occurs during sexual stimulation, sildenafil inhibition of PDE5 leads to an increase in the level of cGMP in cavernous bodies. Thus, in order for sildenafil to cause a necessary pharmacological effect, sexual arousal is necessary.
Studies in vitro have shown selective effects of sildenafil on PDE-5, which is actively involved in the process of erection. The effect of sildenafil on PDE-5 is more powerful than other known phosphodiesterases. This effect is 10 times more powerful than the effect on PDE6, involved in the processes of phototransformation in the retina. When the maximum recommended doses are used, the selectivity of sildenafil in PDE-5 is 80 times greater than its selectivity to PDE1, in
700 times higher than in FDE2, FDEZ, FDE4, FDE7, FDE8, FDE9, PDE10 and FDE11. In particular, the selectivity of sildenafil in PDE-5 is 4000 times greater than its selectivity to FDEZ-cGMP-specific isoform PDE, involved in the regulation of cardiac contractility.
Pharmacokinetics.
Absorption. Kamagra 100 (Sildenafil) is rapidly absorbed. The maximum plasma concentrations of the drug is achieved within 30-120 minutes (with a median of 60 min) after its oral application on an empty stomach. Average bioavailability after oral administration is 41% (with a range of values from 25% to 63%). In the recommended dose range (from 25 to 100 mg), the area under the concentration-time curve (AUC) and the maximum concentration ( max ) of sildenafil after its oral administration increase in proportion to the dose.
When Kamagra 100 is used during food intake, the degree of absorption decreases with an average elongation of T max to 60 minutes and an average decrease of C max by 29%.
Distribution. The average equilibrium volume of distribution (V d ) is 105 liters, which indicates the distribution of the drug in the tissues of the body. After a single oral intake of sildenafil at a dose of 100 mg, the average maximum total plasma concentration of sildenafil is approximately 440 ng / ml (the coefficient of variation is 40%). Since binding of sildenafil and its main N-desmethyl metabolite to plasma proteins is 96%, the average maximum plasma concentration of free sildenafil reaches 18 ng / ml (38 nmol). The degree of binding to plasma proteins does not depend on the total concentrations of sildenafil.
In healthy volunteers taking sildenafil once in a dose of 100 mg, after 90 minutes, less than 0.0002% (an average of 188 ng) of the dose was determined in the ejaculate.
Indications
The drug is recommended for men with erectile dysfunction, which is defined as the inability to achieve or support an erection of the penis necessary for a successful sexual intercourse.
For effective action of the drug, sexual arousal is necessary.
Contraindications Kamagra 100
- Hypersensitivity to the active substance or to any of the excipients of the drug.
- Simultaneous use of nitric oxide (such as amyl nitrite) or nitrates in any form with donors is contraindicated, since it is known that sildenafil affects the pathways of nitric oxide / cyclic guanosine monophosphate (cGMP) metabolism and potentiates the hypotensive effect of nitrates.
- Conditions in which sexual activity is not recommended (for example, severe cardiovascular disorders, such as unstable angina or severe heart failure).
- Loss of vision of one eye due to non-arterial anterior ischemic neuropathy of the optic nerve, regardless of whether this pathology is associated with previous use of PDE-5 inhibitors or not.
- The presence of such diseases as severe liver dysfunction, arterial hypotension (arterial pressure below 90/50 mm Pg.t.), recent stroke or myocardial infarction and known hereditary degenerative diseases of the retina, such as retinitis pigmentosa (a small number of such patients has genetic disorders of PDE of the retina), since the safety of sildenafil has not been studied in such subgroups of patients.
Overdose Kamagra 100
Using a single dose of sildenafil up to 800 mg, adverse reactions were similar to those observed with sildenafil at lower doses, but were more frequent and more severe. The use of sildenafil in a dose of 200 mg resulted in increased efficacy, but caused an increase in the incidence of adverse reactions (headache, hot flashes, dizziness, dyspepsia, nasal congestion, visual impairment).
In case of an overdose, if necessary, regular supportive measures should be taken. Acceleration of the clearance of sildenafil during hemodialysis is unlikely due to the high degree of binding of the drug to plasma proteins and the absence of elimination of sildenafil with urine.
Adverse Reactions
The most common reported adverse reactions such as headache, flushing, indigestion, nasal congestion, back pain, dizziness, nausea, hot flashes, blurred vision, cyanopsy and blurred vision.
Infections and infestations: rhinitis.
From the immune system: hypersensitivity reactions, including anaphylactic shock, angioedema, fever.
From the side of the nervous system: headache, dizziness, sleep disturbance, insomnia, drowsiness, tremor, ataxia, neuralgia, neuropathy, paresthesia, hypesthesia, decreased reflexes, sensitization, stroke, syncope, cerebral vascular thrombosis, transient ischemic attack, dysphasia, convulsions , relapses by court, fainting.
From the side of the organ of vision: impairment of color perception (chloropsy, chromatopsy, cyanopsy, erythropsy, xanthopsia), visual disturbances, blurred vision, lacrimation disorders (dry eyes, tearing and tearing), eye pain, photophobia, photopsy, eye hyperemia, brightness of vision, conjunctivitis , non-arterial anterior ischemic optic nerve neuropathy, retinal vascular occlusion, retinal hemorrhage, arteriosclerotic retinopathy, retinal disorders, glaucoma, visual field defects, diplopia, decreased o Trot vision, myopia, asthenopia floating vitreous opacities, disorders of the iris mydriasis, appearance luminous circles around the light source (halo) in the field of view, eye edema, swelling of the eye, disorders of the eye, hyperemia of conjunctiva, ocular irritation,
From the organs of hearing: vertigo, ringing in the ears, deafness.
From the cardiovascular system: hot flashes, arterial hypertension, arterial / postural hypotension, palpitations, tachycardia, myocardial ischemia / myocardial infarction, atrial fibrillation, AV blockade, ventricular arrhythmia, angina / unstable angina, sudden cardiac arrest, heart failure.
On the part of the respiratory system: nasal congestion, nosebleeds, laryngitis, pharyngitis, sinusitis, bronchitis, productive cough, congestion of the paranasal sinuses, a feeling of compression in the throat, swelling of the nasal mucosa, dryness in the nose.
On the part of the digestive tract: dyspepsia, nausea, vomiting, dry mouth, gingivitis, stomatitis, glossitis, esophagitis, gastritis, gastroenterocolitis, colitis, diarrhea, impaired liver function, hemorrhoidal bleeding, gastroesophageal reflux disease, upper abdominal pain, cavity hypoesthesia cavity.
Shelf life
3 years.
Storage conditions
Store at a temperature of no higher than 30 ° C in the original packaging.
Keep out of the reach of children.
