Naclofen solution for injections ampoules 75 mg/3 ml. №5

Description

Naclofen composition
active substance: diclofenac;
3 ml of solution (1 ampoule) contain diclofenac sodium – 75 mg;
Excipients: benzyl alcohol, propylene glycol, sodium metabisulfite (E 223), sodium hydroxide, water for injections.

Dosage form
Solution for injection.

Pharmacological properties
Naclofen is a non-steroidal drug with pronounced analgesic / anti-inflammatory properties. It is an inhibitor of prostaglandin synthetase (cyclooxygenase). Diclofenac sodium in vitro at concentrations equivalent to those achieved in humans does not inhibit the biosynthesis of proteoglycans in cartilage. When used concomitantly with opioids to relieve postoperative pain, Naclofen significantly reduces the need for opioids.
In rheumatic diseases, the anti-inflammatory and analgesic properties of the drug cause a clinical response, which is characterized by a marked decrease in signs and symptoms: pain at rest and during movement, morning stiffness and swelling of the joints and improvement of their functions. In post-traumatic and postoperative conditions with inflammation, Naclofen also relieves pain and swelling.

Indication
Naclofen when administered intramuscularly is intended for the treatment of:

• inflammatory and degenerative forms of rheumatism, rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, spondyloarthritis, vertebral pain, non-articular rheumatism;
• acute gout attacks;
• renal and biliary colic;
• pain and swelling after injuries and operations;
• severe migraine attacks.

The drug when administered as an intravenous infusion is intended for the treatment or prevention of postoperative pain.

Contraindication:

• Known hypersensitivity to the active substance, sodium metabisulfite or to any other components of the drug.
• History of bleeding or perforation of the gastrointestinal tract associated with previous treatment with nonsteroidal anti-inflammatory drugs (NSAIDs).
• Active form of peptic ulcer / bleeding or recurrent peptic ulcer / bleeding history (two or more separate episodes of established ulcer or bleeding).
• Hepatic failure.
• Congestive heart failure (NYHA II-IV).
• III trimester of pregnancy.
• Like other NSAIDs, diclofenac is contraindicated in patients in whom the use of ibuprofen, acetylsalicylic acid or other NSAIDs provokes asthma attacks, angioneurotic edema, urticaria or acute rhinitis / nasal polyps, or allergy-like symptoms.
• Inflammatory bowel disease (such as Crohn’s disease or ulcerative colitis).
• Acute gastric or intestinal ulcer; gastrointestinal bleeding or perforation.
• High risk of postoperative bleeding, blood clotting, hemostasis disorders, hematopoietic disorders or cerebrovascular bleeding.
• Treatment of perioperative pain during coronary artery bypass grafting (or use of an artificial circulation device).
• Ischemic heart disease in patients with angina, myocardial infarction.
• Cerebrovascular disease in patients who have suffered a stroke or have episodes of transient ischemic attacks.
• Diseases of peripheral arteries.

Children
It is not used in pediatrics.

Application during pregnancy and lactation
Use with great caution during pregnancy. In the third trimester, this drug is contraindicated.
You should stop breastfeeding while taking this drug.

Method of application and dosage
The drug should be used in the lowest effective doses for the shortest period of time, taking into account the goals of treatment of each individual patient.
Naclofen, solution for injection, do not use for more than 2 days; if necessary, treatment can be continued with the drug Naclofen in another dosage form (tablets or suppositories).

• Intramuscular injection
  The following rules should be followed to prevent damage to nerve or other tissues at the site of intramuscular injection.
  The dose is usually 75 mg (1 ampoule) per day, which should be given by deep injection into the upper outer sector of the gluteus maximus. In severe cases (such as colic), the daily dose can be increased to two injections of 75 mg, with an interval of several hours (1 injection in each buttock). Alternatively, 75 mg of solution for injection can be combined with other Naclofen formulations (such as tablets or suppositories) up to a maximum total daily dose of 150 mg of diclofenac.
  In migraine attacks, clinical experience is limited to cases with the initial use of 1 ampoule of 75 mg, the dose should be administered if possible immediately after the use of suppositories of 100 mg on the same day (if necessary). The total daily dose should not exceed 175 mg on the first day.
  No data are available on the use of Naclofen for the treatment of migraine attacks for more than 1 day.
• Intravenous infusions
  Immediately before the start of the intravenous infusion, Naclofen should be diluted in 100-500 ml of 0.9% sodium chloride solution or 5% glucose solution. Both solutions should be buffered with sodium bicarbonate solution (0.5 ml of 8.4% solution or 1 ml of 4.2%). Only clear solutions can be used.
  Naclofen, a solution for injection, should not be given as an intravenous painful injection.
  Two alternative dosage regimens of Naclofen, solution for injection are recommended:
  for the treatment of moderate and severe postoperative pain, it is necessary to enter a solution of 75 mg continuously from 30 minutes to 2 hours; if necessary, treatment can be repeated in 4-6 hours, but the dose should not exceed 150 mg per day;
  to prevent postoperative pain 15 minutes to 1 hour after surgery, a loading dose of 25-50 mg should be administered, followed by a continuous infusion of approximately 5 mg / hour up to a maximum daily dose of 150 mg.

Overdose
Symptoms. There is no typical clinical picture of diclofenac overdose. Overdose may cause symptoms such as headache, nausea, vomiting, epigastric pain, gastrointestinal bleeding, diarrhea, dizziness, disorientation, agitation, coma, drowsiness, ringing in the ears, loss of consciousness or convulsions. In case of severe poisoning, acute renal failure and liver damage are possible.
Treatment. Treatment is symptomatic. Supportive measures and symptomatic treatment should be prescribed for complications such as hypotension, renal failure, convulsions, gastrointestinal disorders and respiratory depression.
Specific measures such as forced diuresis, dialysis or hemoperfusion are unlikely to be effective in the elimination of NSAIDs, including diclofenac, due to high protein binding and extensive metabolism.
Activated charcoal should be considered within 1 hour after administration of a potentially toxic amount of the drug orally. In addition, adults should consider gastric lavage within 1 hour after administration of a potentially toxic amount of the drug. In case of frequent or prolonged convulsions, diazepam should be administered intravenously. Depending on the patient’s clinical condition, other measures may be indicated.

Side effects
Taking this drug can cause side effects in the form of:

• pain in the epigastrium;
• nausea, vomiting, diarrhea, abdominal cramps;
• dyspepsia, gastrointestinal bleeding;
• ulcers of the stomach and intestines;
• glossitis, stomatitis, lesions of the esophageal mucosa;
• intestinal adhesions;
• constipation, pancreatitis;
• headaches, drowsiness, anxiety, nightmares, hair loss;
• skin rashes, urticaria, eczema, erythema multiforme;
• edema, renal failure, hematuria, nephrotic syndrome, papillary necrosis;
• hepatitis, agranulocytosis, thrombocytopenia, leukopenia, anemia;
• tachycardia, chest pain, lowering blood pressure.

Storage conditions and periods
Naclofen is stored for up to 3 years at temperatures up to 25 ° C.