Genitourinary System / Increase Potency

Maxigra 1’s 100 mg coated tablets

Brands: Polpharma (Poland)

$22.90

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Maxigra 1's 100 mg coated tablets quantity

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Brands:: Polpharma (Poland)

Description

The instruction for medical use

of Maxigra medicine

the Trade name

of Maksigr Mezhdunarodnoye the unlicensed

name Sildenafil Lekarstvennaya
the Tablet form, coated 50 mg, 100 mg

Structure
One tablet contains
active agent – sildenafit citrate of 70.24 mg or 140.48 mg (it is equivalent to a sildenafil) 50.00 mg or 100.00 mg respectively,
excipients: Mannitolum, krospovidon (type A), povidone (To 25), silicon dioxide colloidal, starch corn, magnesium stearate, sodium lauryl sulfate,
structure of a cover: gipromelloza (15 mPas), macrogoal 6000, titan E171 dioxide, talc, E132 indigo carmine.

The description
of the Tablet of round shape, with a biconvex surface, coated blue color.

Pharmacotherapeutic group
Drugs for treatment of disturbances of an erection.
The ATX G04BE03 code
the Pharmacological

Sildenafil Pharmacokinetics Absorption properties is quickly soaked up. The maximum concentration in blood plasma after oral administration of drug are on an empty stomach reached within from 30 to 120 minutes. The average absolute bioavailability at oral administration is 41% (range of 2563%). After oral administration of a sildenafil of AUC and Cmax increase in proportion to a dose at reception in the recommended range of doses (50-100 mg).
At reception of a sildenafil together with food the speed of absorption decreases, at the same time the average delay of Tmax makes 60 minutes and average decrease in Cmax – 29%.
Distribution
the Average volume of distribution of a sildenafil in a condition of equilibrium concentration (Vd) makes 105 l that demonstrates its distribution in fabrics. After single oral administration in a dose of 100 mg the average maximum general concentration of a sildenafil in plasma makes about 440 ng/ml. As sildenafit (and its main circulating N-dezmetil metabolite) for 96% contacts proteins of plasma, average maximum concentration of a free sildenafil in plasma makes 18 ng/ml (38 nanometers). Linking with proteins does not affect the general concentration of drug.
At the healthy volunteers receiving sildenafit (single dose in a dose of 100 mg), in 90 minutes after introduction in semen less than 0.0002% (on average 188 ng) the entered dose were defined.
Metabolism
Sildenafil is metabolized by mainly microsomal isoenzymes of a liver of CYP3A4 (main way) and CYP2C9 (minor way). The main tsirkulirushchy metabolite is formed of a sildenafil by N-demethylation. This metabolite possesses a selectivity profile concerning phosphodiesterases, similar to that sildenafit, and its activity concerning FDE5 in vitro is about 50% of activity of initial drug. Concentration of this metabolite in plasma makes about 40% of concentration of a sildenafil. Further the metabolite of N-dezmetil is metabolized, at the same time its elimination half-life makes about 4 h.
Removal
the General clearance of a sildenafil makes 41 l/h, at the same time terminal elimination half-life makes 3-5 h. After oral or intravenous administration sildenafit it is removed in the form of metabolites mainly with a stake (about 80% of the dose entered orally) and in smaller quantity with urine (about 13% of the dose entered orally).
Drug pharmacokinetics in separate groups of patients
Elderly
At healthy volunteers of advanced age (65 years are more senior) the decrease in clearance of a sildenafil was noted that led to increase in concentration of a sildenafil and active metabolite of N-dezmetila in plasma up to 90% in comparison with healthy volunteers of younger age (18-45 years). Owing to age differences in linking with proteins of plasma, the corresponding increase in concentration of a free sildenafil in plasma was about 40%.
Patients with a renal failure
At volunteers with a renal failure of light and moderate severity (clearance of creatinine = 30-80 ml/min.) after single oral introduction of a sildenafil in a dose of 50 mg its pharmacokinetic parameters did not change. Average AUC and Cmax values of a metabolite N-dezmetila increased up to 126% and 73% respectively in comparison with volunteers of the same age without renal failure. However owing to high interindividual variability these distinctions were not significant. At volunteers with a heavy renal failure (clearance of creatinine & lt, 30 ml/min.) the clearance of a sildenafil decreased that led to increase in average AUC and Cmax values to 100% and 88% respectively in comparison with volunteers of the same age without renal failure. Besides, AUC and Cmax values for a metabolite of N-dezmetila were considerably increased to 79% and 200% respectively.
Patients with a liver failure
At volunteers with easy and moderate degree of cirrhosis (And yes In a class on classification of Chayld-Pyyu) decrease in clearance of a sildenafil was noted that led to increase in AUC values (84%) and Cmax (47%) in comparison with volunteers of the same age without disturbance of hepatic function. Pharmacokinetic parameters of a sildenafil at patients with a heavy abnormal liver function were not studied.
The pharmacodynamics
Sildenafil is oral drug for treatment of erectile dysfunction. Under natural conditions, for example at sexual stimulation, drug restores the broken erectile function by strengthening of inflow of blood to a penis.
The physiological mechanism by means of which there is a penis erection includes release of nitrogen oxide (NO) in a cavernous body during sexual stimulation. Further nitrogen oxide activates enzyme guanylate cyclase that leads to increase in level of the cyclic guanozinmonofosfat (tsGMF) which causes relaxation of unstriated muscles in a cavernous body and promotes blood inflow. Sildenafil is selection inhibitor of tsGMF-specific phosphodiesterase of the 5th type (FDE5) in a cavernous body where FDE5 is responsible for disintegration of tsGMF. Sildenafil possesses peripheral type of action on an erection. Sildenafil has no direct weakening effect on the isolated cavernous human body, but actively enhances the weakening effect NO on cavernous fabric. At activation of a way NO/tsGMF as in case of sexual stimulation, FDE5 inhibition under the influence of a sildenafil leads to increase in the tsGMF level in a cavernous body. Therefore in order that sildenafit had the expected effective pharmacological effect, sexual stimulation is necessary. Sildenafil selektiven concerning FDE5 which participates in process of an erection. Its activity concerning FDE5 exceeds activity concerning other known phosphodiesterases. This activity by 10 times exceeds activity concerning FDE6 which participates in the course of transfer of light in a retina. Sildenafil causes an insignificant and passing lowering of arterial pressure which in most cases is not shown clinically. Average maximum decrease in systolic arterial blood pressure in a dorsal decubitus after oral administration of a sildenafil in a dose of 100 mg was 8.4 mm Hg. Corresponding change of diastolic arterial blood pressure in a dorsal decubitus made 5.5 mm Hg. Such lowering of arterial pressure will be coordinated with the vazodilatiruyushchy action of a sildenafil which is possibly connected with increase in the tsGMF level in unstriated muscles of vessels. Single oral introduction of a sildenafil in a dose up to 100 mg had no clinically significant impact on the ECG parameters.
After single dose of a sildenafil in a dose of 100 mg of impact on mobility or morphology of spermatozoa it was not noted.

Indications
– treatment of disturbances of an erection (for maintenance of an erection of a penis
sufficient for carrying out sexual intercourse)

the Route of administration and doses
For use inside
Adults
the Recommended initial dose is 1 tablet of 50 mg of a sildenafil. The maximum daily recommended dose – 100 mg.
The drug Maxigra should be taken approximately in 60 minutes prior to the beginning of sexual activity.
Patients of advanced age
Selection of a dose is carried out by individually attending physician.
Use for patients with renal failures
At patients with a heavy renal failure (clearance of creatinine & lt, 30 ml/min.) is recommended a dose decline up to 25 mg. The dose can be raised to 50 mg and 100 mg, depending on efficiency and tolerance of medicine.
Use for patients with abnormal liver functions
At patients from the liver broken by function (for example, in cirrhosis) metabolism of a sildenafil is reduced. Therefore at patients with the slight and moderated abnormal liver functions it is recommended to lower a dose to 25 mg, taking into account efficiency and shipping the dose can be raised to 50 mg and 100 mg.

Side effects
Very often ≥1/10
– a headache
– “inflows”
Often ≥1/100 to & lt, 1/10
– disorders of vision (photosensitization, disturbance of visual acuity)
– a tranzitorny chromatopsia, weak intensity
– feeling of heartbeat
– feeling of congestion of a nose
– dyspepsia
Seldom ≥1/10000 to & lt, 1/1000
– hypersensitivity reactions
– skin rash
– eye pain and reddening of eyes
– tachycardia, ventricular arrhythmia, a myocardial infarction, unstable
stenocardia
– nasal bleeding
– intracerebral bleeding
– the tranzitorny ischemic attack
– arterial hypertension or hypotension, a faint
– vomiting
– a priapism, a long erection
of the Contraindication
– hypersensitivity to a sildenafil or any of
drug components
– diseases of a cardiovascular system (for example, unstable stenocardia, heavy heart failure)
– it is not necessary to use drug at the patients undergoing treatment
by the nitrates and other medicines releasing
nitrogen oxide
– a heavy liver failure
– arterial hypotension (the ABP is lower than 90/50 mm Hg)
– recently had myocardial infarction or a stroke of a brain
– hereditary degenerative diseases of a retina (for example,
retinitis pigmentoza)
– loss of sight in one eye owing to the front ischemic neuropathy of an optic nerve which is not connected with inflammation of an artery regardless of whether this episode was connected with the previous use of FDE5 inhibitor or not
– children’s and teenage age up to 18 years

Medicinal interactions
Sildenafil exponentiates hypotensive effect of the medicines releasing nitrogen oxide (for example, nitrates, Molsidominum, Natrium nitroprussicum).
Simultaneous use of a sildenafil (once in a dose of 100 mg) and inhibitor of HIV protease of the sakvinavir which is CYP3A4 inhibitor in the conditions of equilibrium concentration (in a dose of 1200 mg 3 times a day) led to increase in Cmax of a sildenafil for 140%, and AUC of a sildenafil – for 210%. Sildenafil did not influence pharmacokinetics of a sakvinavir. Stronger inhibitors of an isoenzyme CYP3A4, such as ketokonazol and itrakonazol, can have more significant impact.
Grapefruit juice is weak inhibitor of metabolism of an isoenzyme CYP3A4 in a wall of digestive tract and can cause moderate increase in level of a sildenafil in blood plasma.
Single dose of an antacid (hydroxide aluminum hydroxide magnesium) does not affect bioavailability of a sildenafil.
Though researches of specific interaction for all medicines were not conducted, the population pharmacokinetic analysis showed that simultaneous use of the accompanying drugs, such as CYP2C9 inhibitors (for example, tolbutamide, warfarin, Phenytoinum), CYP2D inhibitors (for example, selective serotonin reuptake inhibitors, tricyclic antidepressants), tiazida and tiazidopodobny diuretics, loopback and kaliysberegayushchy diuretics, angiotensin-converting enzyme inhibitors, blockers of calcium channels, antagonists the beta of adrenoceptors, or inductors of metabolism CYP450 (for example, rifampicin, barbiturates) do not influence pharmacokinetic parameters of a sildenafil.
Nikorandil represents the activator of potassium channels and nitrate. Interaction with sildenafily because of existence of a nitrate component is possible.
Interaction of a sildenafil (50 mg) at combined use with tolbutamide (250 mg) or warfarin (40 mg) which are metabolized by CYP2C9 is not revealed.
Sildenafil (50 mg) did not cause additional increase in the bleeding time caused by intake of acetylsalicylic acid (150 mg).
Sildenafil (50 mg) did not strengthen hypotensive effect of alcohol at healthy volunteers at the maximum level of alcohol in blood on average of 80 mg/dl.
At the combined use of a sildenafil with medicines, the oppressing CYP3A4 (for example, ketokonazol, erythromycin, Cimetidinum), metabolism of a sildenafil decreases. In case of simultaneous use of a sildenafil and CYP3A4 inhibitors the decrease in an initial dose of a sildenafil to 25 mg is recommended.
Simultaneous use of a sildenafil with ritonaviry (HIV protease inhibitor) is not recommended as metabolism of a sildenafil at the same time considerably decreases.
Simultaneous use of a sildenafil and inhibitor of HIV protease of a sakvinavir causes increase in concentration of a sildenafil in blood plasma.
Sildenafil it is necessary to apply with care at the patients taking α-adrenolytic medicines (especially in a dose & gt, 25 mg), within 4 hours after reception of a sildenafil there can come symptomatic hypotension.
At simultaneous use of an amlodipin and sildenafil in a dose of 100 mg the hypotensive action of an amlodipin (decrease in systolic and diastolic pressure respectively by 8 mm Hg and 7 mm Hg) increases.

Special instructions
It is necessary to use with care drug at patients with the accompanying anatomic pathology of a penis (for example, fibrosis of cavernous bodies, Peyroni’s disease), at patients with diseases of a cardiovascular system (drug has vasodilating property that can cause, a short-term lowering of arterial pressure) and also at patients who have factors contributing to approach of a priapism (for example, drepanocytic anemia, leukoses, a multiple myeloma).
It is not recommended to apply sildenafit along with other methods of treatment of disturbances of an erection because of lack of the researches confirming safety and efficiency of such therapy.
Preliminary sexual stimulation is necessary for approach of therapeutic action of a sildenafil.
Considering lack of the data concerning safety of use of a sildenafil for patients with disturbances of a hemostasis and also at patients with exacerbation of a peptic ulcer of a stomach and duodenum, at these patients the drug Maxigra should be used only when the advantage of treatment of disturbances of an erection exceeds potential risk of approach of bleeding.
As the sexual activity represents a certain risk in heart diseases, before any therapy concerning disturbance of an erection the doctor should perform examination of a condition of a cardiovascular system of patients. Sildenafil has properties of a vazodilatator that leads to an insignificant and passing lowering of arterial pressure. The increased susceptibility to vazodilatator is observed at patients with obstruction of an output path of a left ventricle (for example, an aortal stenosis, a hypertrophic subaortic stenosis) and also seldom found syndrome of the multiple system atrophy which is shown heavy disturbance of autonomous regulation of arterial blood pressure.
Sildenafil strengthens hypotensive effect of nitrates.
The post-marketing phenomena from a cardiovascular system included a myocardial infarction, unstable stenocardia, a sudden cardiac death, ventricular arrhythmia, hemorrhage in a brain, the tranzitorny ischemic attack, hypertensia and hypotension and had communication on time using a sildenafil. The majority, but not all from these patients had earlier existing risk factors from a cardiovascular system. It was reported that many phenomena arose in time or right after sexual intercourse whereas some were noted right after reception of a sildenafil without sexual activity. It is impossible to establish whether these phenomena directly are connected with these factors, or they are connected with other factors.
There are messages about exceptional cases of development of not arterial front ischemic optical neuropathy which leads to a disorder of vision, when sharing Maxigra and other FDE5 inhibitors. In case of a sudden disorder of vision the patient should recommend to stop reception of a sildenafil and to consult immediately with the doctor.
Sildenafil the patients accepting alpha blockers as their combined use can lead to clinically apparent hypotension at certain sensitive patients should appoint with care. Development of this effect within 4 hours after reception of a sildenafil is the most probable. To minimize a possibility of development of orthostatic hypotension in the patients accepting alpha blockers, treatment sildenafily it is necessary to begin after stabilization of a hemodynamics at these patients. The attending physician has to inform patients what actions should be taken in case of symptoms of orthostatic hypotension.
Researches show that sildenafit enhances antiagregantny effect of Natrium nitroprussicum on thrombocytes of the person of in vitro.
Pregnancy and the period of a lactation
the Drug Maxigra is not intended for use for women.
The feature of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms
After administration of drug of Maksigr should be careful at control of vehicles and potentially dangerous mechanisms, in connection with a possibility of development of side effects – dizziness, a disorder of vision.
Overdose
Symptoms: strengthening of symptoms of side effects.
Treatment: symptomatic. Specific antidote for a sildenafil is unknown. Dialysis does not accelerate removal of a sildenafil.

Form of release and packing
of the Tablet, coated 50 mg and 100 mg.
On 1 or 4 tablets place in blister strip packaging from a film of polyvinylchloride and aluminum foil.
On 1 planimetric packing together with the instruction for medical use in the state and Russian languages place in a pack from cardboard.

To Store storage conditions in the dry, protected from light place, at a temperature not above 25 °C.
To store out of children’s reach!

A period of storage
4 years
not to use drug after expiry date.

Prescription status
According to the prescription

the Producer
the Pharmaceutical plant JSC Polfarm
of st. Pelplinsk 19, 83-200 Starogard Gdanski, Poland

the Owner of the registration certificate
of JSC Khimfarm, Kazakhstan

the Address of the organization accepting claims from consumers on quality of products, goods in the territory of the Republic of Kazakhstan
JSC Khimfarm,
Shymkent, REPUBLIC OF KAZAKHSTAN, Rashidov St.,/N, ph.: 560882
Phone number 7252 (561342)
Fax number 7252 (561342)

to Develop the E-mail address of standart@santo.kz

Additional information