Pharmacodynamics and pharmacokinetics
The active component of Olfen-75, diclofenac sodium, belongs to non-steroidal drugs with pronounced antirheumatic , analgesic , anti-inflammatory and antipyretic properties. Its action is based on preventing the biosynthesis of prostaglandins , which affect inflammatory processes, fever and pain.
For rheumatic diseases, the drug helps get rid of the signs and symptoms of the disease, it relieves pain, normalizes the functioning of joints and eliminates stiffness. In case of inflammation after injuries and operations, Olfen-75 promotes the rapid disappearance of pain, relieves the severity of swelling due to wounds and inflammation. In addition, it greatly reduces the need for opioid . This drug also acts as an analgesic for diseases of non-rheumatic origin. It reduces pain 15-30 minutes after internal administration.
This remedy is well suited for starting the treatment of many inflammatory diseases.
The degree of its binding to plasma proteins is almost 100%. It penetrates into the synovial fluid . The maximum concentration of the drug is achieved 2-4 hours after the peak concentration. The half-life of synovial fluid is approximately 4-5 hours. High concentrations of diclofenac sodium in synovial fluid are observed even after 12 hours.
The drug is metabolized in part by glucuronidation and methoxylation to form active phenolic metabolites .
The half-life of the drug is approximately 1.5 hours. About 60% is excreted through the kidneys in the form of metabolites and less than 1% unchanged. The remaining amount is excreted in metabolized form with bile and feces.
Analogs
All drugs containing diclofenac can be called analogues of the drug. These include Dicloran, Dicloberl, Diclak, Voltaren, Ortofen, Vurdon, Clodifen, Dolex, Naklofen.
Dicloran
Diklak
Vourdon
Clodifene
All non-steroidal anti-inflammatory drugs can also be called analogues. For problems with joints or tendons, aceclofenac, ketoprofen, and naproxen are most often prescribed.
Indications for use
The medicine is used for:
- exacerbations of rheumatism : rheumatoid arthritis , osteoarthritis , vertebral pain syndromes, ankylosing spondylitis , spondyloarthritis , extra-articular rheumatism ;
- renal and hepatic colic ;
- acute attacks of gout ;
- pain, swelling and inflammation after injuries and operations.
Reviews
Anna, practices Pole-dance “At first, when I became interested in pole dancing, there were a lot of injuries. There were also sprains and back problems, since beginners do not really understand what non-professional dancers can and cannot do. All pain in the legs and back was treated with the Olfen patch. Once, when I sprained my leg, I even gave injections: my leg went away quickly.”
Victor “I treated my back for a long time; I had a hernia. Now the pain only appears when I put pressure on my back. Olfen gel and a little rest help.”
Contraindications
Olfen injections should not be used for:
- hypersensitivity to the components of the drug;
- history of seizures due to lidocaine;
- a history of bronchospasm , nasal polyps , acute rhinitis , urticaria (and other allergic reactions that may be caused by acetylsalicylic acid or other NSAIDs ) ;
- bleeding in the gastrointestinal tract or perforation ;
- peptic ulcer of the stomach and/or duodenum during exacerbation;
- inflammatory bowel diseases;
- severe liver failure ;
- hypovolemia or hypohydria ;
- renal failure in moderate and severe stages;
- atrioventricular block II and III degrees;
- Adams-Stokes syndrome;
- bradycardia;
- complete transverse heart block ;
- severe heart failure ;
- sick sinus syndrome;
- severe arterial hypotension ;
- cardiogenic shock;
- treatment of pain after coronary bypass surgery or use of a heart-lung machine;
- hematopoiesis , bleeding, and incomplete hemostasis occurring after surgery ;
- porphyria;
- myasthenia gravis.
Side effects
If any undesirable reactions occur when using Olfen-75 ampoules, you should immediately contact a specialist.
abscesses may develop at the injection site . In addition, the following side effects are known to occur when using this medication:
- CNS - headaches , dizziness ;
- sense organs – vertigo ;
- Gastrointestinal tract - pain in the abdominal area, vomiting, cramps , flatulence , nausea , diarrhea, dyspepsia , anorexia ;
- hepatobiliary system - increased levels of transaminases ;
- kidneys and urinary tract - fluid retention in the body, swelling;
- skin and skin – rash;
- general disorders - reactions at the injection site.
Also in rare cases, the following may appear: thrombocytopenia , anemia , leukopenia , agranulocytosis , hypersensitivity reactions, angioedema , numbness of the extremities, sensations of heat/cold, disorientation, insomnia, irritability , depression , nightmares, mental disorders.
Drowsiness , paresthesia , convulsions, aseptic meningitis , stroke , memory, vision, hearing and taste disorders, anxiety, tremor , diplopia , and tinnitus have been reported infrequently
In addition, there are reports of side effects from the cardiovascular system such as increased heart rate, heart attack , arterial hypertension , arrhythmia , chest pain, heart failure , vasculitis , bradycardia . From the respiratory system, the appearance of asthma , bronchospasm , pneumonitis and respiratory depression is noted. There are also rare reports of gastritis , vomiting with blood, melena , bleeding in the gastrointestinal tract, gastric or intestinal ulcers, colitis , stomatitis , esophageal lesions, pancreatitis , constipation , glossitis , diaphragm-like intestinal strictures .
Rare side effects after taking Olfen-75 include hepatitis liver dysfunction and necrosis jaundice , liver failure , urticaria , erythema , Stevens-Johnson syndrome , exfoliative dermatitis , photosensitivity , allergic purpura , itching , eczema , toxic epidermal necrolysis , alopecia , acute renal failure , proteinuria , nephrotic syndrome , hematuria , interstitial nephritis , renal papillary necrosis .
Patch
Olfen is a patch that is applied externally. Needed for local therapy for inflammation of ligaments and tendons, as well as inflammatory processes in muscles and joints. Also used to treat muscles and ligaments after injuries, for example, after tendon ruptures, bruises and dislocations.
A patch is needed for the treatment of localized forms of joint rheumatism.
The patch is used only externally and on intact areas of the skin. Before using the patch, remove the film from it and apply a little pressure to the skin.
The patch must not come into contact with mucous membranes. Don't forget to wash your hands well. Only a doctor can determine the dosage and duration of the course. Treatment lasts up to 14 days. Change the patch twice a day.
Side effects are rare. Peeling, itching and rashes are possible. With prolonged use, photosensitivity, bronchospasms, and angioedema may develop. Contraindicated for skin lesions, eczema, wounds, as well as hypersensitivity to diclofenac, lidocaine and non-steroidal anti-inflammatory drugs in general.
Instructions for use Olfen (Method and dosage)
The dosage in which Olfen-75 ampoules are used is selected for each patient individually . The minimum dose is taken for the shortest possible period of time.
The instructions for Olfen also recommend that you first conduct a skin test for hypersensitivity to the components of the drug. In the absence of negative reactions, the drug continues to be used in the form of intramuscular infusions .
As a rule, the dosage is administered in a single dose of 75 mg Olfen in ampoules, applied once a day. Injections are given into the upper outer quadrant of the gluteal muscle. Immediately after the ampoule is opened, the solution should be used. If there is any unused solution left in an open ampoule, it must be discarded.
For severe pain, if Olfen injections are used, the instructions for use recommend injections 2 times a day with a break of several hours between them. The location of the infusion should be different. Combination with other dosage forms of Olfen is acceptable, but the maximum daily dosage should not exceed 150 mg.
The duration of parenteral use of the drug should not exceed 2 days. If it is necessary to continue therapy, Olfen-75 is replaced by other forms of the drug. In addition, this drug cannot be used for intravenous administration.
Candles
Otherwise called rectal capsules Olfen Rektocaps. It is recommended to wet the candle before use. The suppository contains 100 mg of diclofenac sodium. Available in boxes of five capsules in one blister.
The candle is inserted with a blunt part. After administration, you need to lie down for a third of an hour. Olfen is usually prescribed one suppository once a day. Sometimes it is acceptable to use two candles a day, but not for very long. Only the doctor will determine the course.
Contraindicated for bleeding in the intestines, ulcers of the stomach and intestines, ulcerative colitis and Crohn's disease, and other inflammatory bowel diseases. Rectal capsules are an excellent option for those who have stomach and liver ailments.
Olfen is a non-steroidal anti-inflammatory drug for the treatment of a variety of diseases of the ligaments, muscles, tendons and joints. Can also be used for other diseases accompanied by inflammation.
The active ingredient is diclofenac sodium. It has many side effects, so you should not prescribe the remedy yourself. Watch the dosage! Remember that any remedy can become hazardous to health if you take it incorrectly.
Overdose
Typical symptoms of diclofenac sodium have not been established. When using the drug in high doses, vomiting , diarrhea , as well as tinnitus , bleeding in the gastrointestinal tract , dizziness , and convulsions . renal failure and liver damage may develop .
Lidocaine hydrochloride in high doses can lead to numbness of the tongue and lips, euphoria, blurred vision, depression, difficulty breathing, cardiac conduction , coma , agitation, anxiety, tremor , drowsiness , bradycardia , transverse heart block .
Therapy is symptomatic. Forced diuresis , hemoperfusion or dialysis are ineffective in most cases.
Olfen™ overdose, symptoms and treatment
Typical clinical symptoms of diclofenac overdose are not known. If any side effects occur due to improper use or possible overdose, the usual general therapeutic methods for treating NSAID toxicity should be used. Treatment of acute NSAID poisoning consists of supportive and symptomatic therapy: gastric lavage and activated charcoal. With the development of hypotension, renal failure, convulsions, gastrointestinal irritation and respiratory depression, symptomatic therapy is carried out. The effectiveness of forced diuresis, dialysis or hemoperfusion is negligible due to the high degree of binding of the drug to plasma proteins.
Interaction
Olfen-75 increases the content of lithium and digoxin in the blood plasma, so control of their dosages is recommended.
Combination with diuretics or antihypertensive drugs may lead to a decrease in the antihypertensive effect . Olfen-75 should be prescribed with caution while monitoring the patient's condition. During the course of taking these drugs, you need to drink enough fluids and monitor your kidney function. When combined with potassium-sparing diuretics, hyperkalemia may develop , so serum potassium levels should be periodically determined.
When interacting with systemic NSAIDs or corticosteroids , diclofenac may contribute to the occurrence of adverse reactions from the gastrointestinal tract. In addition, it should be used with caution along with anticoagulants , SSRIs and antiplatelet agents , as this may cause bleeding. Combination with anticoagulants may also increase the risk of hemorrhagic complications . So the condition of patients must be carefully monitored.
Olfen-75 should be taken with caution with hypoglycemic agents intended for oral use. It is recommended to monitor your blood sugar levels.
This drug may also increase the toxicity and blood of Methotrexate nephrotoxicity of Tacrolimus or Cyclosporine . Therefore, dosage adjustments are required.
Olfen-75 in combination with quinolones can lead to the development of seizures. Phenytoin increases its cardiodepressive effect. Ethanol enhances the inhibitory effect on the respiratory system.
The degree of absorption of diclofenac is reduced by approximately 30% when used simultaneously with Colestipol and by 60% with cholestyramine . It is necessary to take them with a break of several hours.
Medicines that stimulate enzymes that metabolize drugs may reduce the concentration of diclofenac in the blood plasma.
Beta-blockers , Cimetidine , Bupivacaine , Disopyramide , Nortriptyline , Imipramine , Propranolol , Peptidine , Quinidine , Amitriptyline , Chlorpromazine increase the content of lidocaine in the serum, reducing its hepatic metabolism . In cardiac glycoside , it may also worsen the severity of AV block . In addition, lidocaine reduces the cardiotonic effect of cardiac glycosides , increases the cardiodepressive effect of antiarrhythmic and anticonvulsants , enhances the depression of the central nervous system by sedatives and hypnotics , as well as the effect of drugs that affect the blockade of neuromuscular transmission . May lead to delusions and hallucinations together with Procainamide .
