Maxigra
Maxigra: 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. Use in childhood
- 10. In case of impaired renal function
- 11. For violations of liver function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Maxigra
ATX code: G04BE03
Active ingredient: sildenafil (sildenafil)
Producer: Polfarma S. A., Poland Pharmaceutical plant (Poland)
Description and photo update: 2018-26-10
Prices in pharmacies: from 226 rubles.
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Maxigra is a drug used in the treatment of erectile dysfunction.
Release form and composition
The dosage form of Maxigra is film-coated tablets: blue, round biconvex (1 blister in a cardboard box containing 1 or 4 tablets).
Composition of 1 tablet:
- active substance: sildenafil - 25, 50 or 100 mg (in the form of sildenafil citrate - 35.12; 70.24 or 140.48 mg);
- auxiliary components (25/50/100 mg): sodium lauryl sulfate - 1/2/4 mg; colloidal silicon dioxide - 1/2/4 mg; magnesium stearate - 1.5 / 3/6 mg; mannitol - 35.38 / 70.76 / 141.52 mg; corn starch - 5/10/20 mg; crospovidone - 3/6/12 mg; povidone - 3/6/12 mg;
- shell: talc - 0.24 / 0.43 / 0.6 mg; titanium dioxide - 0.52 / 0.9 / 1.3 mg; hypromellose - 2.36 / 4.13 / 5.9 mg; indigo carmine (E132) - 0.14 / 0.24 / 0.35 mg; macrogol 6000 - 0.74 / 1.3 / 1.85 mg.
Pharmacological properties
Pharmacodynamics
Maxigra is one of the drugs used to treat erectile dysfunction.
Sildenafil is a potent selective inhibitor of cyclic guanosine monophosphate (cGMP) -specific phosphodiesterase type 5 (PDE5). By increasing blood flow to the penis during sexual stimulation, it helps to restore impaired erectile function. Sildenafil does not have a direct relaxing effect on the isolated corpora cavernosa, but by inhibiting PDE5, it actively enhances the relaxing effect of nitric oxide (NO). As a result of the use of the drug in the corpus cavernosum, blood flow increases and smooth muscle tissue relaxes. In relation to PDE5, the activity of sildenafil is 10–10,000 times higher than the activity in relation to other PDE isoenzymes (1–11).
The pharmacological action of the drug is observed only in the presence of sexual stimulation.
According to clinical studies, the average time to achieve an erection sufficient for sexual intercourse (resistance - 60%) is in the range of 12–37 minutes (average - 25 minutes).
In some patients, 60 minutes after taking 100 mg of Maxigra using the Farnsworth-Munsell 100 test, a slight and transient violation of the ability to distinguish colors (blue / green) was recorded, after 120 minutes these changes were absent. Sildenafil does not affect the perception of contrast, visual acuity, electroretinogram, pupil diameter or intraocular pressure.
Pharmacokinetics
Sildenafil is rapidly absorbed after oral administration. The average absolute bioavailability is 41% (from 25 to 63%). After a single dose of 100 mg Maxigra inside on an empty stomach, Cmax (maximum concentration of the substance) is 18 ng / ml, the average time to reach it is 60 minutes (from 30 to 120 minutes).
Cmax is reduced by 20–40% when taking Maxigra in combination with fatty foods, the time to reach Cmax is 90–180 minutes.
The Vd (volume of distribution) of sildenafil at equilibrium is approximately 105 liters. Plasma protein binding of the substance and its main circulating N-desmethyl metabolite is about 96% (it does not depend on the total concentration of sildenafil).
In healthy volunteers, after a single dose of 100 mg of Maxigra after 90 minutes, less than 0.000 2% of the administered dose was determined in the semen.
Metabolism occurs mainly in the liver. Microsomal isoenzymes CYP3A4 (main pathway) and CYP2C9 (sub pathway) are involved in the process. The main circulating metabolite is formed by N-desmethylation. The metabolite in terms of selectivity of action on PDE is comparable to sildenafil, its activity in relation to PDE5 is approximately 50% of the activity of the substance, plasma concentration is about 40% of the concentration of sildenafil. The N-desmethyl metabolite undergoes further metabolism, T 1/2 (half-life) is approximately 4 hours.
The total clearance of sildenafil is 41 l / h, the final T 1/2 is from 3 to 5 hours. After oral administration, the substance is excreted in the form of metabolites, mainly through the intestines (about 80% of the dose), by the kidneys - to a lesser extent (about 13% of the dose).
The clearance of sildenafil in elderly patients (over 65 years old) is reduced, the plasma concentration of the free active substance is about 40% higher than that in young patients (18–45 years old).
Changes in the pharmacokinetic parameters of sildenafil after a single oral dose of 50 mg in renal insufficiency of mild and moderate severity (with creatinine clearance of 30–80 ml / min) does not occur. With creatinine clearance ≤ 30 ml / min (severe renal failure), sildenafil clearance decreases, which leads to a significant increase in AUC (area under the concentration-time curve) and Cmax (by 100 and 88%, respectively) in comparison with those in no impaired renal function.
In patients with mild / moderate liver cirrhosis (on the Child - Pugh scale - class A and B), the clearance of sildenafil decreases, which leads to an increase in AUC and Cmax (84 and 47%, respectively) in comparison with indicators in the absence of impaired hepatic function. The pharmacokinetic processes of sildenafil in severe liver dysfunction have not been studied.
Indications for use
According to the instructions, Maxigra is prescribed for the treatment of organic, psychogenic, mixed erectile dysfunction, which are characterized by an inability to achieve / maintain an erection of the penis sufficient for satisfactory intercourse.
The drug is effective only for sexual stimulation.
Contraindications
Absolute:
- combined use with donors of nitric oxide or nitrates in any form;
- age up to 18 years;
- individual intolerance to any component of the drug.
Relative (Maxigra is prescribed under medical supervision):
- diseases that predispose to the occurrence of priapism, including sickle cell anemia, multiple myeloma, leukemia, thrombocytopenia;
- anatomical deformity of the penis (including with Peyronie's disease, angulation or cavernous fibrosis);
- peptic ulcer of the stomach and duodenum in the acute stage;
- diseases accompanied by bleeding;
- some disorders of the cardiovascular system, including heart failure, unstable angina pectoris, myocardial infarction, stroke, severe, life-threatening arrhythmias, arterial hypertension or hypotension with blood pressure (arterial pressure) more than 170/100 or less than 90/50 mm in the last 6 months rt. Art.;
- hereditary retinitis pigmentosa.
Instructions for use of Maxigra: method and dosage
Maxigra tablets are taken orally, preferably on an empty stomach, since the onset of action of the drug when taken simultaneously with fatty foods may be delayed.
The recommended time for taking the drug is approximately 60 minutes before the planned sexual activity.
The average single dose is 50 mg once a day. Depending on the efficacy / tolerability, the dose can be reduced to 25 mg or doubled (maximum).
The initial dose for creatinine clearance <30 ml / min and / or impaired hepatic function is 25 mg. If necessary, it can be increased to 50 or 100 mg.
Maxigra at a reduced dose of 25 mg is prescribed in case of combined use with CYP3A4 inhibitors (except for ritonavir, the combination with this drug is not recommended).
To reduce the likelihood of orthostatic hypotension in patients who use alpha-blockers, Maxigra should be taken after hemodynamic stabilization at an initial dose of 25 mg.
Side effects
Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01%, including individual messages - very rare; with an unknown frequency - violations registered during the post-marketing observation period):
- sense organs: often - a change in color perception, visual impairment; sometimes - ringing in the ears, tearing disorders, conjunctival diseases, other eye disorders; rarely - deafness; with an unknown frequency - retinal vascular occlusion, anterior ischemic neuropathy of the optic nerve of non-inflammatory etiology, visual field defect;
- skin / subcutaneous tissue: sometimes - skin rash;
- nervous system: very often - headache; often - dizziness; sometimes - hypesthesia, drowsiness; rarely - fainting, acute disorders of cerebral circulation; with an unknown frequency - convulsions, transient ischemic attack, repeated convulsions;
- respiratory system: often - nasal congestion; rarely - nosebleeds;
- cardiovascular system: often - flushing of the face; sometimes - tachycardia, palpitations; rarely - atrial fibrillation, arterial hypotension / hypertension, myocardial infarction; with an unknown frequency - unstable angina pectoris, ventricular arrhythmia, sudden cardiac death;
- reproductive system: with an unknown frequency - prolonged erection, priapism;
- digestive system: often - dyspeptic disorders; sometimes - nausea, vomiting, xerostomia;
- immune system: rarely - hypersensitivity reactions;
- musculoskeletal system: sometimes - myalgia;
- others: rarely - fatigue, chest pain.
Overdose
When conducting studies, it was found that as a result of a single dose of Maxigra in a dose of 800 mg, adverse reactions are comparable to those when taking lower doses of the drug, but their severity and frequency increase.
The use of Maxigra at a dose of 200 mg does not lead to an increase in efficiency, while the frequency of undesirable phenomena manifests itself in the form of headache, flushing, dizziness, dyspepsia, nasal congestion, and visual impairment.
In case of an overdose, symptomatic therapy is prescribed. Sildenafil is not excreted during hemodialysis.
special instructions
To diagnose erectile dysfunction and determine the possible causes of its occurrence, before the appointment of Maxigra, a medical history should be collected and a physical examination of the patient should be performed.
Since sexual activity is a certain risk in heart disease, it is necessary to examine the state of the patient's cardiovascular system before starting therapy.
As a result of the action of sildenafil, which has the properties of a vasodilator, a transient decrease in blood pressure is observed during its use. For certain concomitant diseases, especially in combination with sexual activity, before using Maxigra, it is necessary to assess the risk of undesirable effects of vasodilatory action. Increased susceptibility is observed with obstruction of the left ventricular outflow tract (for example, with aortic stenosis, hypertrophic obstructive cardiomyopathy), as well as in patients with the rare syndrome of multiple systemic atrophy, which is manifested by severe violations of blood pressure regulation by the autonomic nervous system.
In rare cases, with the combined use of sildenafil and other PDE5 inhibitors, the development of visual impairments and anterior ischemic neuropathy of the optic nerve of non-inflammatory etiology was noted. In case of sudden visual impairment, you need to stop taking Maxigra and seek the advice of a specialist.
Caution is required with the combined use of Maxigra with alpha-blockers, since in some sensitive patients in this case, clinically pronounced hypotension may develop. The appearance of this effect is most likely within four hours after taking the drug. To reduce the likelihood of this disorder, Maxigra in this group of patients should be prescribed after hemodynamic stabilization. It is necessary to consider the advisability of prescribing the drug at an initial dose of 25 mg
Prescribing Maxigra to patients for whom sexual activity is undesirable should not be.
Influence on the ability to drive vehicles and complex mechanisms
Due to the likelihood of developing some adverse reactions, in particular dizziness and visual impairment, patients should be careful when driving vehicles.
Pediatric use
Patients under 18 years of age are not prescribed Maxigra tablets.
With impaired renal function
When creatinine clearance is <30 ml / min, the initial dose of Maxigra should not exceed 25 mg.
For violations of liver function
In case of impaired hepatic function, therapy is recommended to start at a dose of 25 mg.
Drug interactions
Sildenafil metabolism occurs mainly in the liver under the influence of isoenzymes CYP3A4 and CYP2C9 (major and minor pathways), therefore inhibitors of these isoenzymes can reduce its clearance.
With simultaneous use with CYP3A4 inhibitors (erythromycin, ketoconazole, cimetidine), a decrease in the clearance of sildenafil is observed.
Inhibitors of CYP2C9 (warfarin, tolbutamide, phenytoin), CYP2D inhibitors (tricyclic antidepressants, selective serotonin reuptake inhibitors), beta-blockers, angiotensin-converting enzyme inhibitors, thiazides and thiazide diuretics, diuretic acid-like and diuretase-like diuretase barbiturates, rifampicin) have no effect on the pharmacokinetic processes of sildenafil.
Effect of Maxigra on other drugs:
- nitrates: increased hypotensive effect; combined use with nitric oxide donors or any form of nitrate is contraindicated;
- alpha-blockers: development of symptomatic hypotension in selected sensitive patients.
Analogs
The analogues of Maxigra are Tornetis, Dinamiko, VIVAIRA, Revazio, Vildegra, Viatail, Viagra, Silafil, Taxier, Silden, Vizarsin, Erexesil, Sildenafil, Viasan-LF and others.
Terms and conditions of storage
Store at temperatures up to 30 ° C. Keep out of the reach of children.
Shelf life (depending on dosage): 25 mg - 3 years; 50 and 100 mg - 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Maxigra
According to reviews, Maxigra is a safe and effective drug used to treat erectile dysfunction. In some cases, they indicate its high cost in comparison with analogues, as well as an insufficient therapeutic effect. The development of adverse reactions is rarely reported.
Price for Maxigra in pharmacies
The approximate price for Maxigra is:
- 50 mg (in a package of 1 or 4 pcs.): 297-317 or 592-601 rubles;
- 100 mg (in a package of 1 or 4 pcs.): 336–359 or 763–774 rubles.
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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!
