ORFENAK solution for injection
ORFENAK
International non-patented name: Diclofenac sodium + Orphenadrine citrate
Composition
Active substance: 3 ml (1st ampoule) of the solution contains 75 mg of diclofenac sodium.
2 ml (2nd ampoule) of the solution contains 60 mg of orphenadrine citrate.
Diclofenac
Excipients: sodium metabisulfite, benzyl alcohol, disodium edetate, propylene glycol, water for injection.
Orphenadrine
Excipients: sodium metabisulfite, sodium chloride, sodium hydroxide, water for injection.
Composition
- Diclofenac
- Colorless solution.
- Orphenadrine
- Colorless solution.
Pharmacotherapeutic group
Analgesic, Non-steroidal anti-inflammatory drug, Muscle relaxant.
ATC kodu: M03BC51.
Pharmacological properties
Pharmacodynamics
Diclofenac is a non-steroidal anti-inflammatory drug (NSAID). Non-steroidal anti-inflammatory drugs inhibit the activity of the cyclooxygenase enzyme and reduce the formation of prostaglandins and thromboxane precursors. Diclofenac prevents the generation of pain impulses and has a peripheral effect on tissues. Reversible inhibition of platelet aggregation.
Orphenadrine acts through the central nervous system rather than directly into skeletal muscle. This can weaken polysynaptic reflexes. Its muscle relaxant effect is related to its depressant effect on the CNS. It has an analgesic effect that enhances the myorelaxant effect on skeletal muscles, in addition, it has an anticholinergic effect and reduces the symptoms of parkinsonism.
Pharmacokinetics
Diclofenac is 99% bound to proteins. It undergoes biotransformation in the liver. The half-life is 1.2-2 hours. 40-65% is excreted by the kidneys, 35% by bile and feces.
Protein binding of orphenadrine is low. Its effect begins 5 minutes after intramuscular injection, and the duration of effect in intravenous administration is 12 hours. It undergoes biotransformation in the liver. The half-life is 14 hours, and its metabolites are 2-25 hours. It is excreted through the kidneys and intestines.
Instructions for use
ORFENAK is used in the treatment of rheumatic diseases accompanied by muscle contracture (rheumatoid arthritis, arthrosis, spondylitis, bursitis), trauma (tendon strain, fractures) or bone-muscle pain caused during surgery.
Contraindications
Diclofenac
Hypersensitivity to any substance contained in the preparation.
Active gastritis, intestinal erosion, bleeding or perforation.
History of gastrointestinal bleeding or perforation due to NSAID use.
Severe liver, kidney and heart failure.
3rd trimester of pregnancy.
Under 18 years of age.
Hemostasis disorders or anticoagulant treatment.
Heart failure (NYHA II-IV), ischemic heart disease, peripheral arterial diseases, cerebrovascular diseases.
Hypovolemia, dehydration.
History of severe allergic reactions such as anaphylaxis or angioedema after taking aspirin or other NSAIDs. Nasal polyps accompanied by bronchospasm due to aspirin use (high risk of severe allergic reactions). Active pathological changes in the anamnesis or currently present in the blood or bone marrow depression (may increase or aggravate pathologies).
It should be used with caution
History of mild allergic reactions such as allergic rhinitis, urticaria or rash caused by aspirin or other NSAIDs, anemia or asthma, conditions causing or related to fluid accumulation in the body: congestive heart disease, edema, hypertension, renal dysfunction or kidney failure, conditions that increase the toxic effect of the drug on the gastrointestinal system: alcoholism or cancer, inflammatory or ulcerative diseases of the gastrointestinal system, including Crohn’s disease, diverticulitis, history or current peptic ulcer or active erosive colitis, tobacco use (if NSAID use is necessary, antiulcer therapy should be prescribed, misoprostol or sucralfate can be used to reduce the risk of gastrointestinal toxicity), heart failure, diabetes, edema, sepsis (risk of renal failure)
Haemophilia, coagulation or platelet dysfunction (increased risk of bleeding)
Liver cirrhosis or impaired liver function (increased risk of kidney failure)
Elderly (higher risk of serious events resulting in death such as adverse effects on the liver or kidneys, gastrointestinal bleeding)
Conditions such as dysuria, cystitis, hematuria, nephritis or nephrotic syndrome during treatment with other NSAIDs
For patients who need to limit their sodium intake, the amount of sodium in the drug should be taken into account when choosing an NSAID.
Orphenadrine
Achalasia, urinary tract obstruction, glaucoma or predisposition to it, myasthenia gravis, muscle hypotonia, cardiospasm, arrhythmia, tachycardia, peptic ulcer, prostatic hyperplasia, pyloric or duodenal obstruction.
It should be used with caution
History of hypersensitivity to orphenadrine, heart disease, arrhythmia or tachycardia (may cause tachycardia), depression, impaired liver and kidney function.
Special instructions and precautions
Diclofenac
Diclofenac should not be used in patients with serious cardiovascular diseases such as heart failure, ischemic heart disease, and peripheral arterial or cerebrovascular diseases.
It should be used with caution in patients with cardiovascular risk factors (diabetes, hypertension, hypercholesterolemia, smoking), and then the balance between the expected benefit and risk should be considered for each patient individually.
It is recommended to use the lowest possible dose and duration of treatment for all patients.
Periodic review of the need for continued treatment is recommended.
The antipyretic, analgesic and anti-inflammatory effects of NSAIDs can mask the signs of the onset or exacerbation of infection. NSAIDs may cause bronchospasm or anaphylaxis in aspirin-sensitive asthmatic patients.
The use of the drug with alcohol can increase the risk of ulcers.
Taking two or more NSAIDs, including ketorolac, or taking acetaminophen, aspirin, or other salicylates for more than a few days while taking NSAIDs is not recommended unless prescribed by a doctor.
Due to the increased risk of bleeding, it is recommended to use the drug with caution before surgical operations.
Caution should be exercised in case of contusion, dizziness, drowsiness or vision problems.
Flu-like symptoms (chills, muscle aches, or other pains) along with a rash may be signs of a serious drug reaction. When such symptoms appear, the doctor must be informed.
In case of side effects such as blood in the sputum, nosebleeds, chest pain, fainting, convulsions, it is recommended to immediately stop the medicine and consult a doctor.
Symptoms of anaphylaxis, angioedema or bronchospasm (discoloration of the face, rash, hives and/or bruising, shortness of breath, swelling of the eyelids or around the eyes, swelling of the mouth, lips and/or tongue, shortness of breath, difficulty breathing, chest tightness tightness and/or wheezing), drop in blood pressure and collapse, the drug should be stopped immediately and the doctor should be consulted urgently.
Cross-sensitivity: Patients sensitive to aspirin, ketorolac, and other obsolete NSAIDs (such as oxyphenbutazone, suprofen, and zomepirac) may be sensitive to other NSAIDs.
Orphenadrine
Alcohol or other central nervous system depressants should not be used during therapy unless prescribed and approved by a physician.
Be careful if any of the following symptoms occur: blurred vision or other vision problems, dizziness, drowsiness, muscle weakness.
It can cause dry mouth, if this symptom lasts more than 2 weeks, you should consult a dentist.
Do not stop treatment abruptly.
This drug is prone to abuse (may have a euphoric effect).
It can affect the ability to drive a vehicle and other potentially dangerous machinery.
Children
There is no information on the use of the drug in children. Its safety is unknown. Injections contain benzyl alcohol as a preservative, so they should not be used in newborns and premature babies. The use of benzyl alcohol in newborns has been associated with a fatal toxic syndrome. During this syndrome, in addition to metabolic acidosis, central nervous, respiratory, blood-vascular systems and kidney functions are disturbed.
The elderly
Diclofenac has not been identified as having a higher risk of toxicity. However, in the elderly with gastrointestinal infections, the use of NSAIDs can cause ulcers and/or gastrointestinal bleeding.
Dentistry
NSAIDs can cause pain or irritation and damage to the lining of the mouth.
Surgical operations
The drug can prolong the duration of intraoperative and postoperative bleeding. Platelet function is restored on the first day of discontinuation of diclofenac. It should be discontinued before surgery.
Interaction with other drugs
Diclofenac
Any NSAID hypoprothrombinemia. Concomitant use with drugs that can cause thrombocytopenia, ulcers, or gastrointestinal bleeding may result in changes in blood coagulation or an increased risk of bleeding.
Taking it at the same time as acetaminophen increases its negative effect on the kidneys.
Alcohol, corticosteroids, glucocorticoids, corticotropin (chronic use) or potassium supplements, coumarin anticoagulants, thrombolytic agents such as heparin, anistreplase, streptokinase, or urokinase, two or more concurrent NSAIDs, aspirin, colchicine, and other platelet aggregation inhibitors, ulcers or increases the risk of gastrointestinal bleeding.
Diclofenac enhances the effect of oral antidiabetic agents and insulin.
Antihypertensives or diuretics, especially when triamterene is used simultaneously with diclofenac, antihypertensive effects may decrease, the risk of renal failure increases.
Potassium-sparing diuretics increase the risk of hyperkalemia.
Use with bone marrow depressants can cause leukopenia and thrombocytopenia.
Use of cefamandol with cefaperazone causes hypoprothrombinemia, inhibits platelet aggregation and increases the risk of bleeding.
Increases the concentration and nephrotoxicity of cyclosporine.
Increases the concentration and toxicity of digoxin.
It increases the concentration of lithium.
Increases methotrexate toxicity by reducing protein binding and/or renal excretion. It is recommended that diclofenac be discontinued 12 to 24 hours before high-dose methotrexate infusions, and NSAID therapy should not be restarted until at least 12 hours after the infusion.
Probenecid increases the serum concentration and toxicity of diclofenac.
Orphenadrine
Enhances the effect of alcohol or CNS depressants (the dose of one or both drugs should be reduced).
May enhance the effect of anticholinergic drugs.
Use during pregnancy and lactation
Studies on the use of diclofenac in the first trimester of pregnancy have not been conducted. It is not recommended to use in the second trimester. It is contraindicated in the third trimester. Orphenadrine can be used by pregnant women only when strictly indicated. During lactation, dicofenac penetrates into breast milk and should not be used during lactation. Orphenadrine should not be used during lactation.
Effects on the ability to drive vehicles and other potentially dangerous mechanisms
During treatment, caution should be exercised when driving vehicles and engaging in other dangerous activities that require high attention and quick psychomotor reaction.
Method of use and dosage
Intramuscular use:
One dose of the drug consists of 2 ampoules (No. 1 and No. 2). One dose (the content of 2 ampoules) is injected intramuscularly every 12 hours during the day. The duration of treatment is not recommended to exceed 2 days.
Intravenous use:
If the pain does not go away, it can definitely be used intravenously in hospital conditions and under the supervision of a doctor for post-operative pain.
Immediately before starting intravenous infusion, 2 ampoules should be dissolved in 100-500 ml of sodium chloride solution (0.9%) or glucose solution (5%). For the treatment of moderate to severe postoperative pain, it should be infused continuously for 1.5 to 2 hours. If necessary, the treatment can be repeated after 4-6 hours, within any 24 hours. Maximum daily use should not exceed 2 doses.Əlavə təsirləri
Orfenadrin
Often: anuresis, increased intraocular pressure, tachycardia, fainting, nausea, vomiting, pain and difficulty urinating, dry mouth.
Rarely: hallucinations, aplastic anemia, difficulty breathing, chest tightness, sores or white spots on the lips or mouth, swollen or painful lymph nodes, bleeding, fatigue or weakness.
Other: insomnia, agitation, euphoria, memory changes.
Diclofenac
Hypersensitivity reactions: rhinosinusitis, asthma, angioedema or urticaria.
Very common: Delayed urination, rash, rash, headache, cramping, abdominal discomfort, constipation, diarrhea, indigestion, nausea.
Frequent: angina pectoris or its exacerbation, cardiac arrhythmia, allergic dermatitis, abdominal foam, gastrointestinal ulcer, including erosive esophagitis, peptic ulcer, multiple gastrointestinal ulcers, gastric ulcer, diverticulitis, vertigo, transaminase elevation, injection irritation and pain in the area, dizziness.
Sometimes: chest pain, heart failure, myocardial infarction
Rarely: increased blood pressure, convulsions, memory impairment, aseptic meningitis, depression, peripheral neuropathy, erythema multiforme, colitis or its complications, bleeding, gastrointestinal bleeding, vaginal bleeding or unusual menstrual bleeding, hepatitis, jaundice, anaphylaxis, angioedema, bronchospasm, laryngeal oedema, toxic amblyopia, vision change, aphthous stomatitis, hearing loss or change, pancreatitis, interstitial nephritis, nephrotic syndrome, oliguria, anuria, renal failure, dyspnoea or respiratory failure, sweating, tremor, nervousness , weakness, bitterness or taste changes in the mouth, decreased or lost appetite, restlessness, dry mouth, weight loss.
Other: insomnia, alveolitis, eosinophilia, impotence, Stevens-Johnson syndrome, eczema, hair loss, photosensitivity, toxic epidermal necrolysis, fulminant hepatitis, liver failure, ischemic colitis, deafness, optic neuritis, thrombocytopenia, leukopenia, anemia, agranulocytosis, injection site reactions.
Overdose
Diclofenac
Symptoms: renal and gastrointestinal toxicity, moderate effects may occur from the CNS (drowsiness, drowsiness) or gastrointestinal system (abdominal pain, nausea, vomiting). Occasionally, more serious reactions such as gastrointestinal bleeding, acute renal failure, convulsions, coma, and hypoprothrombinemia may occur.
Treatment: symptomatic and supportive treatment is carried out and bed rest is prescribed. To reduce absorption, the stomach is washed, activated charcoal is prescribed. For the treatment of kidney failure, hemodialysis is performed, diclofenac is removed by dialysis. In case of severe hypotension, volume expanders are used. Diazepam or other benzodiazepines are used during seizures, and vitamin K is used when hypoprothrombinemia occurs. It is possible to prevent early signs of kidney failure by using dopamine and intravenous debutamine. Nephritis or nephrotic syndrome, thrombocytopenia, hemolytic anemia, severe skin reactions, or hypersensitivity are treated with glucocorticoids. Gastrointestinal ulcers or bleeding may occur a few days after an overdose. Patients should be advised to seek medical attention immediately if this occurs.
Orphenadrine
Symptomatic and supportive treatment is carried out. Intravenous fluids are prescribed to increase excretion. Diuresis, hemodialysis or peritoneal dialysis are not effective. Patients who have overdosed on orphenadrine should receive psychiatric consultation.
Packing form:
3 ml diclofenac sodium in an amber ampoule with a blue dot. 2 ml orphenadrine citrate in an amber glass ampoule. 1 ampoule of diclofenac sodium and 1 ampoule of orphenadrine citrate are packed in a cardboard box with an insert.
Store condition
It should be stored at a temperature of 30°C and out of the reach of children.
Shelf life
2 years.
By presciption
Manufacturer
Radiant Parenterals Ltd., India.
242/5-6, G.I.D.C Dist, Estate, Waghodia, Vadodara, Gujarat 391760.