Nucleospermate sodium (Solution) Instructions for Use

Marketing Authorization Holder

Nucleopharm, LLC (Russia)

Manufactured By

Pharmazashchita SPC, FSUE FMBA of Russia (Russia)

ATC Code

L03A (Immunostimulants)

Active Substance

Sodium nucleospermate (Grouping name)

Dosage Forms

	Nucleospermate sodium	Solution for intramuscular and subcutaneous administration 15 mg/1 ml: amp. 5 ml 1, 2, 4, 5, 10 or 20 pcs.; fl. 5 ml 1, 2, 4, 5, 10 or 20 pcs.
		Solution for intramuscular and subcutaneous administration 15 mg/1 ml: amp. 10 ml 1, 2, 4, 5, 10 or 20 pcs.; fl. 10 ml 1, 2, 4, 5, 10 or 20 pcs.

Dosage Form, Packaging, and Composition

Solution for intramuscular and subcutaneous administration colorless, transparent or slightly opalescent.

Excipients: sodium chloride – 1 ml, water for injection – up to 1 ml.

5 ml – ampoules of colorless glass (1) – contour cell packaging (1) – cardboard packs.
5 ml – ampoules of colorless glass (1) – contour cell packaging (2) – cardboard packs.
5 ml – ampoules of colorless glass (2) – contour cell packaging (1) – cardboard packs.
5 ml – ampoules of colorless glass (2) – contour cell packaging (2) – cardboard packs.
5 ml – ampoules of colorless glass (5) – contour cell packaging (1) – cardboard packs.
5 ml – ampoules of colorless glass (5) – contour cell packaging (2) – cardboard packs.
5 ml – ampoules of colorless glass (10) – contour cell packaging (1) – cardboard packs.
5 ml – ampoules of colorless glass (10) – contour cell packaging (2) – cardboard packs.
5 ml – vials of colorless glass (1) – contour cell packaging (1) – cardboard packs.
5 ml – vials of colorless glass (1) – contour cell packaging (2) – cardboard packs.
5 ml – vials of colorless glass (2) – contour cell packaging (1) – cardboard packs.
5 ml – vials of colorless glass (2) – contour cell packaging (2) – cardboard packs.
5 ml – vials of colorless glass (5) – contour cell packaging (1) – cardboard packs.
5 ml – vials of colorless glass (5) – contour cell packaging (2) – cardboard packs.
5 ml – vials of colorless glass (10) – contour cell packaging (1) – cardboard packs.
5 ml – vials of colorless glass (10) – contour cell packaging (2) – cardboard packs.

Solution for intramuscular and subcutaneous administration colorless, transparent or slightly opalescent.

Excipients: sodium chloride – 1 ml, water for injection – up to 1 ml.

10 ml – ampoules of colorless glass (1) – contour cell packaging (1) – cardboard packs.
10 ml – ampoules of colorless glass (1) – contour cell packaging (2) – cardboard packs.
10 ml – ampoules of colorless glass (2) – contour cell packaging (1) – cardboard packs.
10 ml – ampoules of colorless glass (2) – contour cell packaging (2) – cardboard packs.
10 ml – ampoules of colorless glass (5) – contour cell packaging (1) – cardboard packs.
10 ml – ampoules of colorless glass (5) – contour cell packaging (2) – cardboard packs.
10 ml – ampoules of colorless glass (10) – contour cell packaging (1) – cardboard packs.
10 ml – ampoules of colorless glass (10) – contour cell packaging (2) – cardboard packs.
10 ml – vials of colorless glass (1) – contour cell packaging (1) – cardboard packs.
10 ml – vials of colorless glass (1) – contour cell packaging (2) – cardboard packs.
10 ml – vials of colorless glass (2) – contour cell packaging (1) – cardboard packs.
10 ml – vials of colorless glass (2) – contour cell packaging (2) – cardboard packs.
10 ml – vials of colorless glass (5) – contour cell packaging (1) – cardboard packs.
10 ml – vials of colorless glass (5) – contour cell packaging (2) – cardboard packs.
10 ml – vials of colorless glass (10) – contour cell packaging (1) – cardboard packs.
10 ml – vials of colorless glass (10) – contour cell packaging (2) – cardboard packs.

Clinical-Pharmacological Group

Leukopoiesis stimulant

Pharmacotherapeutic Group

Leukopoiesis stimulator, immunomodulatory agent

Pharmacological Action

It is a hemopoiesis stimulator, has the ability to stimulate hemopoiesis by influencing the processes of proliferation, migration and differentiation of colony-forming units and acting at all levels of hematopoiesis. It actively participates in cellular metabolism, integrating into cellular structures and especially in proliferating tissues.

It accelerates granulocytopoiesis at the promyelocyte and myelocyte stage, increases the neutrophil maturation index.

The therapeutic effect occurs within 3-10 days (depending on the severity of leukopenia). It restores hematological parameters reduced as a result of chemotherapy with cytostatic drugs. It does not have local irritant, embryotoxic, immunotoxic, mutagenic or teratogenic effects.

It has an immunomodulatory effect at the cellular and humoral levels (activates killer cells, stimulates antibody formation). It activates antiviral, antifungal and antimicrobial immunity. It suppresses the reproduction of the HIV virus, effectively reduces the viral load of HIV-infected patients.

Pharmacokinetics

With subcutaneous, intramuscular and rectal administration at the recommended dose, it quickly enters the blood. The concentration in the blood increases in a direct linear dependence. T_Cmax with a single subcutaneous and intramuscular administration is 0.5 hours, with rectal administration – 5 hours.

After 24 hours, a rapid decrease in the concentration of the drug in the blood begins, associated with its distribution in organs and tissues. The redistribution of the drug between plasma and blood cells occurs in parallel with its metabolism and excretion. The gradual elimination of the drug from the blood occurs in the time interval from 2 to 8 days from the moment of administration.

With repeated administration of the drug every 24 hours for 5 days, the process of its accumulation in the blood and bone marrow is observed only from the first 4 doses. In other proliferating tissues, the total concentration increases even after the 5th administered dose. After 8 days after the 5th administration, its concentration significantly decreases in all organs and tissues, but at the same time exceeds the concentration achieved with a single administration and sufficient for the therapeutic effect of the drug.

The main route of transport of sodium nucleospermate for all routes of administration is the endolymphatic pathway. The greatest tropism to the drug is shown by the bone marrow, lymph nodes, spleen, thymus, and kidneys. It penetrates the blood-brain barrier.

It is excreted (including in the form of metabolites) mainly with urine and partially with feces. T_1/2 with subcutaneous and intramuscular administration is 63-69 hours.

With intramuscular administration during the first day, about 50% is excreted in the urine and 12.5% in the feces, with subcutaneous administration – 37% and 3%, with rectal administration – 2.5% and 61.5%, respectively.

Indications

Leukopenia (against the background of cytostatic use and radiation therapy) – treatment and prevention.

Additionally: HIV infection at different stages of the disease (as part of combination therapy).

ICD codes

Dosage Regimen

A single dose is 0.075 g, maximum doses: daily – 10 ml, course – 150 ml.

Prevention of neutropenia: adults – 5 ml once a day for 3-5 days. Children – 5 ml once a day for 1-2 days. The first administration of the drug is carried out 24 hours before the start of the chemotherapy course.

Treatment of neutropenia: adults – 5-10 ml once a day for 5-10 days. Children – 5 ml once a day for 1-4 days.

Maximum single dose for adults is 150 mg (10 ml of 1.5% solution), for children – 75 mg.

Treatment of HIV infection in adults: rectally, after bowel movement, using a 14 cm catheter attached to a syringe. The catheter is inserted into the rectum for the entire length up to the syringe tip.

The recommended dose is 25 ml of 1-1.5% solution (250-375 mg) 2 times a day (morning and evening) 2 times a week.

Depending on the indications, the course of treatment is from 1 to 6 months.

Adverse Reactions

Hyperemia, pain (at the injection site), increase in body temperature to subfebrile values.

With rectal administration, no side effects were identified.

Contraindications

Hypersensitivity, pregnancy, lactation period, children under 3 years of age. Acute diseases of the liver, kidneys, pancreas, gastrointestinal tract; decompensated chronic heart failure, cerebrovascular accident.

With caution any myeloid preneoplastic disease.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and lactation.

Use in Hepatic Impairment

Contraindicated in acute liver diseases.

Use in Renal Impairment

Contraindicated in acute kidney diseases.

Pediatric Use

Contraindicated in children under 3 years of age.

Special Precautions

The effectiveness of use for leukopenia below 2 thousand/µl has not been proven.

Storage Conditions

Store at 2°C (36°F) to 8°C (46°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.