Buy Emoxypine solution 10 mg/ml 1 ml ampoule 10 pcs
  • Buy Emoxypine solution 10 mg/ml 1 ml ampoule 10 pcs

Emoxypine

Moscow Endocrine Plant
1240 Items
2019-09-19
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Clinical Pharmacology

Angioprotector, reduces the permeability of the vascular wall, is an inhibitor of free radical processes, antihypoxant and antioxidant.

Reduces blood viscosity and platelet aggregation, increases the content of cyclic nucleotides (cAMP and cGMP) in platelets and brain tissue, has fibrinolytic activity, reduces the permeability of the vascular wall and the risk of hemorrhages, contributes to their resorption. Expands coronary vessels, in the acute period of myocardial infarction limits the size of the source of necrosis, improves the contractility of the heart and the function of its conduction system. With increased blood pressure has a hypotensive effect. In acute ischemic disorders of cerebral circulation reduces the severity of neurological symptoms, increases the resistance of tissue to hypoxia and ischemia.

Possesses retinoprotective properties, protects the retina from the damaging effects of high-intensity light, promotes the resorption of intraocular hemorrhages, improves microcirculation of the eye.

Indications

Subconjunctival and intraocular hemorrhage, angioretinopathy (including diabetic), chorioretinal dystrophy (including atherosclerotic genesis), dystrophic keratitis, retinal vascular thrombosis, complications of myopia, protection of the cornea (when wearing contact lenses) and retina of the eye of the eye of the eye, retina, complications of myopia, protection of the cornea (when wearing contact lenses) and retina of the eye of the eye of the eye, retina, complications of myopia, protection of the cornea (when wearing contact lenses) and retina of the eye of the eye) high intensity light (laser and sunburns, with laser coagulation), trauma, inflammation and cornea burns, cataracts (including prevention in people over 40 years old), eye surgery, condition after surgery for laucoma with choroidal detachment.

Composition

1 ml of solution contain

Active ingredient: methylethylpyridinol hydrochloride (Emoxypine) 10 mg

Emoxypine is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Emoxypine Moscow Endocrine Plant Russia solution
Vixipin eye drops
Emoxy-Optic Synthesis AKOMP Russia eye drops
Emoxibel Belmedpreparaty Belarus ampoules
Emoxypine Enzyme Russia eye drops

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Emoxypine

Dosage and Administration

Subconjunctival or parabulbary, 1 time per day or every other day. Subconjunctival - 0.2-0.5 ml of 1% solution (2-5 mg), parabulbarno - 0.5-1 ml of 1% solution (5-1 mg). The duration of treatment is 10-30 days; The course can be repeated 2-3 times a year.

Adverse reactions

Short-term excitement, drowsiness, increased blood pressure, allergic reactions (skin rashes, etc.), local reactions - pain, burning, itching, hyperemia, hardening of paraorbital tissues (resolves independently).

Contraindications

Hypersensitivity, pregnancy.

Drug interactions

Pharmaceutical is not compatible with other drugs.

Pregnancy and Lactation

Contraindicated in pregnancy.

Special instructions

Treatment should be under the control of blood pressure and blood clotting.

Dexamethasone

12 mg orally 30 minutes before the start of chemotherapy

8 mg orally (in the morning)

8 mg orally (in the morning)

8 mg orally (in the morning)

Serotonin 5-HT Antagonists3 receptors

see relevant instructions for medical use.

-

-

-

Mild chemotherapy

A drug

Day 1

Day 2

Day 3

Emend®

125 mg orally for 1 h before the start of chemotherapy

80 mg (in the morning)

80 mg (in the morning)

Dexamethasone

12 mg orally 30 minutes before the start of chemotherapy

-

-

Serotonin 5-HT Antagonists3 receptors

see relevant instructions for medical use.

-

-

In patients with mild or moderate liver failure (from 5 to 9 points on the Child-Pugh scale) dose adjustment is not required. Clinical data on the use of the drug in patients with severe liver failure (> 9 points on the Child-Pugh scale) are not available.

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Dose adjustment based on gender, age, race or body mass index is not required.

Adverse reactions

The safety of aprepitant was evaluated in approximately 6500 patients.

Prevention of nausea and vomiting caused by chemotherapy

High Effective Therapy

The clinical study involved 544 patients who received highly emethogenic therapy and aprepitant in the first cycle. 413 patients from this group continued therapy (the maximum number of chemotherapy courses was 6). The three-day regimen of the drug Emend® in combination with ondansetron and dexamethasone was well tolerated by patients. Most of the adverse reactions reported in clinical trials have been identified as mild to moderate.

The most frequent adverse reactions on the background of high-efficacy chemotherapy in patients who received aprepitant in combination with serotonin 5-HT3 receptor antagonists and dexamethasone (were observed with greater frequency than during therapy with serotonin 5-HT antagonists3receptors and dexamethasone): hiccups (4.6%), increased ALT activity (2.8%), dyspepsia (2.6%), constipation (2.4%), headache (2%), and decreased appetite ( 2%).

In an additional clinical study in 1169 patients who received various types of high-efficacy chemotherapy and regimens for the prevention of nausea and vomiting with the use of aprepitant and serotonin antagonists 5-HT3receptors and dexamethasone or serotonin 5-HT antagonists only3receptor and dexamethasone, the profile of adverse reactions was the same.

Mild Effective Therapy

In a clinical trial involving 868 patients, the most frequent adverse reaction against moderate emethogenic chemotherapy in patients who received aprepitant in combination with 5-HT antagonists3-receptors and dexamethasone (was observed with greater frequency than during therapy with 5-HT antagonists3 receptor and dexamethasone), was fatigue (1.4%).

In the combined analysis of high-emittogenic and moderate emethogenic chemotherapy in patients treated with aprepitant, the following side effects were observed with the use of the drug, and more often than with standard therapy:

  • often (≥1 / 100 to <1/10);
  • infrequently (from ≥1 / 1000 to <1/100);
  • rarely (from ≥1 / 10,000 to <1/1000).

Infectious and parasitic diseases: rarely - candidiasis, a staph infection.

From the hemopoietic system: infrequently - anemia, febrile neutropenia.

Metabolism and nutrition: often - loss of appetite; rarely polydipsia.

Mental Disorders: infrequently - anxiety; rarely - disorientation, euphoria.

From the nervous system: infrequently - dizziness, drowsiness; rarely - cognitive impairment, lethargy, taste perversion.

From the senses: rarely - conjunctivitis, tinnitus.

Since the cardiovascular system: infrequently - heart palpitations, hot flashes ("hot flashes"); rarely - bradycardia, cardiovascular disorders.

On the part of the respiratory system: often - hiccups; rarely - sore throat, sneezing, cough, post-nasal syndrome, pharyngeal irritation.

From the digestive system: often - dyspepsia; rarely — belching, nausea, gastroesophageal reflux, vomiting, abdominal pain, dry mouth, flatulence; rarely - solid feces, perforated duodenal ulcer, neutropenic colitis, stomatitis, bloating.

On the part of the skin and subcutaneous fat: infrequently - rash, acne; rarely - photosensitization, excessive sweating, seborrhea, increased oily skin, itchy rash.

From the musculoskeletal system: rarely, muscle spasms, muscle weakness.

From the urinary system: infrequently - dysuria; rarely - pollakiuria.

Changes from laboratory indicators: often - increased activity of ALT; infrequently - increased AST activity, increased alkaline phosphatase activity; rarely - an increase in diuresis, the presence of red blood cells in the urine, hyponatremia, weight loss, glycosuria, neutropenia.

Common disorders: often - fatigue; infrequently - asthenia, malaise; rarely - swelling, discomfort in the chest, gait disturbance.

The side effect profile of patients receiving highly emittogenic and moderate emethogenic chemotherapy during the repeated courses (the maximum number of courses was 6) using aprepitant was comparable to that during the 1st cycle of chemotherapy.

In another study of the use of aprepitant for the prevention of nausea and vomiting induced by chemotherapy, a report was received about serious side effects - Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

Post-registration data

Due to the fact that reports were received from volunteers from groups of the population with an undetermined number, it is impossible to reliably determine the expected frequency or causal relationship with taking the drug.

From the skin and skin appendages: itching, rash, urticaria, rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

On the part of the immune system: hypersensitivity reactions, including anaphylactic reactions.

With caution: Emend® should be used in patients simultaneously receiving medications that are metabolized mainly with the participation of the CYP3A4 isoenzyme. The simultaneous appointment of the drug Emend® with warfarin can lead to a clinically significant reduction in INR. In patients receiving long-term warfarin therapy, the INR value should be carefully monitored for 2 weeks with each cycle of chemotherapy and especially 7-10 days after starting Emend® on a 3-day regimen. The effectiveness of hormonal contraceptives may decrease during and within 28 days after treatment with Emend®. During treatment with Emend® and within 1 month after taking the last dose of Emend®, alternative and backup methods of contraception should be used.

Drug interactions

Aprepitant is a substrate, a moderate inhibitor and inducer of the isoenzyme CYP3A4, as well as an inducer of the isoenzyme CYP2C9.

With the simultaneous appointment of aprepitant can increase the plasma concentration of drugs, the metabolism of which occurs with the participation of the isoenzyme CYP3A4.Emend® should not be used simultaneously with pimozide, terfenadine, astemizole, cisapride, ergot alkaloid derivatives. Inhibition of CYP3A4 isoenzyme under the influence of aprepitant can lead to increased plasma concentrations of these drugs and to potentially serious and life-threatening reactions.

Aprepitant induces the metabolism of warfarin and tolbutamide. The simultaneous administration of Emend® with these or other drugs that are metabolized with the participation of the CYP2C9 isoenzyme (for example, phenytoin) can lead to a decrease in their plasma concentration. No effect of Emend® on AUC R (+) - or S (-) - warfarin was noted, but when used together, a decrease in the minimum concentration of S (-) - warfarin was observed, which was accompanied by a decrease in INR by 14% 5 days after the end of the drug Emend®.

In patients receiving warfarin therapy for a long time, the level of INR should be carefully monitored for 2 weeks, and especially for 7–10 days after the start of Emend® administration on a 3-day regimen, during each cycle of chemotherapy.

Emend® reduces the AUC of tolbutamide, a substrate of the CYP2C9 isoenzyme, by 23% on the 4th day, by 28% on the 8th day, and by 15% on the 15th day. At the same time, tolbutamide in a single dose of 500 mg was administered before the start of the 3-day regimen with Emend® on the 4th, 8th, and 15th days.

The interaction of the drug Emend® with drugs that are substrates of the P-glycoprotein transporter is unlikely (no interaction of the drug Emend®® with digoxin). Aprepitant does not cause clinically significant changes in the pharmacokinetics of serotonin 5HT antagonists3-receptors - ondansetron, granisetron and hydrodolasetron (the active metabolite of dolasetron).

With simultaneous administration of Emend® and GCS, there was an increase in AUC of dexamethasone (by ingestion) 2.2 times, methylprednisolone administered IV, 1.3 times, and methylprednisolone orally, 2.5 times. In this regard, to achieve the desired effect, the standard dose of dexamethasone, when taken orally, in combination with aprepitant, is reduced by 50%, methylprednisolone is reduced by approximately 25% when administered intravenously, and if administered orally, by 50%.

When using the drug Emend® together with chemotherapeutic drugs, the metabolism of which mainly or partially occurs with the participation of the CYP3A4 isoenzyme (etoposide, vinorelbine, docetaxel and paclitaxel), the doses of these drugs can not be adjusted. However, caution is advised when applying to patients receiving these drugs, and to provide additional monitoring. In post-registration studies, there have been cases of neurotoxicity, which can be considered as a possible side effect of ifosfamide, used in conjunction with aprepitant.

The effect of Emend® on the pharmacokinetics of docetaxel was not detected.

The effectiveness of hormonal contraceptives during the period of administration and within 28 days after the end of the administration of the drug Emend® can be reduced (during treatment with the drug Emend® and for 1 month after the last dose of the drug Emend®, alternative or reserve methods of contraception should be used).

With simultaneous oral administration of midazolam and Emend®, an increase in the AUC of midazolam was noted. A possible increase in plasma concentration of midazolam or other benzodiazepines, the metabolism of which is carried out with the participation of CYP3A4 isoenzyme (alprazolam, triazolam), should be taken into account when co-prescribing these drugs with Emend®.

Simultaneous administration of Emend® with drugs that inhibit the activity of CYP3A4 isoenzyme may lead to an increase in the concentration of aprepitant in the blood plasma. Therefore, it is necessary to prescribe Emend® with caution in combination with strong inhibitors of the CYP3A4 isoenzyme (for example, with ketoconazole).However, simultaneous administration of Emend® with moderate inhibitors of the CYP3A4 isoenzyme (for example, with diltiazem, itraconazole, voriconazole, posonazol, clarithromycin, telithromycin and protease inhibitors) does not cause clinically significant changes in the concentration of aprepitant in blood plasma.

Simultaneous administration of Emend® with drugs that are strong inducers of CYP3A4 isoenzyme (for example, with rifampicin, phenytoin, carbamazepine, phenobarbital) can lead to a decrease in plasma aprepitant concentration and, thus, to a decrease in the effectiveness of Emend®. Also, the simultaneous use of aprepitant with preparations of Hypericum perforatum is not recommended.

In patients with mild and moderate arterial hypertension, taking an aprepitant tablet containing a dose comparable to 230 mg of the drug in capsules in combination with diltiazem at a dose of 120 mg 3 times / day for 5 days resulted in a 2-fold increase in AUC of aprepitant and simultaneous increase AUC diltiazem 1.7 times. These pharmacokinetic effects did not lead to clinically significant changes in the ECG, heart rate or blood pressure compared with changes in these indicators when taking only diltiazem.

Simultaneous administration of aprepitant 1 time / day in the form of tablets at a dose comparable to 85 mg or 170 mg of the drug in capsules, and paroxetine at a dose of 20 mg 1 time / day resulted in a decrease in AUC by approximately 25% and Cmax approximately 20% for aprepitant and for paroxetine.

Pregnancy and Lactation

Adequate and strictly controlled clinical studies of the safety of the drug during pregnancy have not been conducted, so the use of the drug Emend® during pregnancy is not recommended.

It is not known whether aprepitant is excreted in human breast milk. If necessary, the use of the drug during lactation should decide on the termination of breastfeeding due to the risk of undesirable effects on the infant.

Special instructions

Inhibition of CYP3A4 by an aprepitant can lead to an increase in plasma concentrations of drugs that are metabolized mainly with the participation of the CYP3A4 isoenzyme (including some chemotherapeutic drugs).

Use in Pediatrics

Safety and efficacy of the drug Emend® in children have not been established.

Impact on the ability to drive vehicles and other mechanisms that require high concentration of attention

Studies on the effect of Emend® on the ability to drive or work with mechanisms have not been conducted. However, you should consider the profile of side effects of the drug, which may affect the ability of patients to control mechanisms. Patients may have different reactions to Emend®.

Overdosage

Symptoms: available data on the use of aprepitant in high doses without chemotherapy (once up to 600 mg or 375 mg daily for 42 days) indicate good tolerability of the drug. In 1 patient, who took 1440 mg of aprepitant, drowsiness and headache were observed.

Treatment: Emend® therapy should be stopped and the patient’s condition should be monitored. If necessary, carry out symptomatic therapy. In connection with the anti-emetic effect of aprepitant, drugs that induce vomiting are not likely to be effective. Antidote to the drug is unknown. Hemodialysis is not effective.

  • Brand name: Emend
  • Active ingredient: Aprepitant
  • Dosage form: Capsules
  • Manufacturer: Merck Sharp & Dohme
  • Country of Origin: USA

Studies and clinical trials of Emoxypine (Click to expand)

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