Solufen Application, Dosage, Side Effects, FAQ - Drug FAQ (2023)

soluble

Solufen is a non-selective inhibitor of cyclooxygenase, an enzyme involved in the synthesis of prostaglandins via the arachidonic acid pathway. Its pharmacological effects are thought to be due to inhibition of cyclooxygenase-2 (COX-2), which decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling. Antipyretic effects may be due to action on the hypothalamus, resulting in increased peripheral blood flow, vasodilation and subsequent heat dissipation. COX-1 inhibition is thought to cause some of the side effects of ibuprofen, including gastrointestinal ulcers. Solufen is administered as a racemic mixture. The R enantiomer undergoes extensive interconversion to the live S enantiomer. The S enantiomer is believed to be the more pharmacologically active enantiomer.

Solufen has multiple effects on different inflammatory pathways involved in acute and chronic inflammation. The main effects of ibuprofen are related to the control of pain, fever and acute inflammation due to the inhibition of prostanoid synthesis by COX-1 and COX-2. Pain relief is attributed to affected peripheral regions and central nervous system effects on pain transmission mediated by the dorsal horn and superior spinothalamic tract. Some reports have attempted to link pain regulation to a possible increase in endogenous cannabinoid synthesis and action at NMDA receptors. It has been shown that the effect on pain is related to cortical evoked potentials.

It is reported that the antipyretic effect is related to the effect on prostanoid synthesis, since prostanoids are the main mediator of pyresis signaling in the hypothalamus-preoptic region.

The use of ibuprofen in dental procedures has been attributed to local inhibition of prostanoid production, as well as its anti-edema effects and increase in plasma beta-endorphins. Some reports indicate a rapid local reduction in COX-2 expression in the dental pulp as a result of ibuprofen administration.

Usos

Solfen is used

• To treat signs and symptoms of rheumatoid arthritis, ankylosing spondylitis, osteoarthritis and other non-rheumatoid arthropathies,
• For the treatment of non-articular rheumatic diseases such as frozen shoulder, bursitis, tendinitis, tenosynovitis and low back pain,
• Used to treat soft tissue injuries such as sprains, strains and post-operative pain
• To treat dysmenorrhea,
• To treat toothache.
• Used to treat colds and fevers.

Solufen is also used in the concomitant treatment of the following conditions: ankylosing spondylitis (AS), common cold, cystic fibrosis (CF), fever, stomach ulcer, gouty arthritis, headache, insomnia, juvenile idiopathic arthritis (JIA), menstrual problems ( dysmenorrhea). ), migraine, mild pain, nasal congestion, osteoarthritis (OA), pain, acute pain, inflammatory pain, patent ductus arteriosus (PDA), pericarditis, primary dysmenorrhea, rheumatoid arthritis, severe pain, sinus pressure, mild to moderate pain, mild pain, moderate pain

How Solufen works

The exact mechanism of action of ibuprofen is not known. However, ibuprofen is considered an NSAID and, therefore, a non-selective inhibitor of cyclooxygenase, an enzyme involved in the synthesis of prostaglandins (mediators of pain and fever) and thromboxane (stimulators of blood clotting) via the arachidonic acid pathway.

Solufen is a non-selective COX inhibitor and therefore inhibits COX-1 and COX-2 activity. Inhibition of COX-2 activity decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling, while inhibition of COX-1 is believed to cause some of the side effects of ibuprofen, including gastrointestinal ulcers.

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Structure

Dose

Solufen can

Oral Administrations-

For kids:

• 20 mg per kg of body weight daily in divided doses. In children weighing less than 30 kg, the total daily dose should not exceed 500 mg. If gastrointestinal disturbances occur, Solufen should be taken with food or milk.
• 1-2 years: 1/2 teaspoon (2.5 ml) 3-4 times a day;
• 3-7 years: 1 teaspoon (5 ml) 3-4 times a day;
• 8-12 years: 2 teaspoons (10 ml) 3-4 times a day. Solufen is not recommended for children under 1 year of age.

for adults:

• for arthritic pain: The dosage range is 0.9 to 2.4 g per day. The usual dose is 400 mg 3-4 times a day, preferably after meals. Depending on the severity of symptoms at the time drug treatment is started, or if patients do not respond, the dose can be increased to a maximum of 2.4 g per day. After a satisfactory response has been obtained, the patient's dose should be reviewed and, if necessary, adjusted and gradually reduced.
• For mild to moderate pain: 400 mg every 6 hours or as needed.
• for dysmenorrhea: 400 mg every 4 hours or as needed.

topical administrations-

Pain and inflammation associated with musculoskeletal and joint disorders: As a 5% cream, foam, gel, spray solution or 10% gel: apply to the affected area.

Side effects

Solufen generally has a low incidence of side effects. The most common side effects are gastrointestinal problems. Gastric ulcers and gastrointestinal bleeding have been reported infrequently. Other side effects include headache, dizziness, nervousness, rash, itching, drowsiness, insomnia, blurred vision and other ocular reactions, hypersensitivity reactions, abnormal liver function tests, impaired kidney function, agranulocytosis, and thrombocytopenia.

toxicity

Overdose symptoms occur in persons who have ingested more than 99 mg/kg. The most common symptoms of overdose are abdominal pain, nausea, vomiting, lethargy, dizziness, drowsiness (tiredness), dizziness and sleeplessness. Other overdose symptoms include headache, loss of consciousness, tinnitus, CNS depression, seizures and convulsions. Rarely, metabolic acidosis, hepatic dysfunction, hyperkalemia, renal failure, dyspnoea, respiratory depression, coma, acute renal failure, and apnoea (mainly in very young pediatric patients) may occur.

The reported LD50 of ibuprofen is 636 mg/kg in the rat, 740 mg/kg in the mouse and 495 mg/kg in the guinea pig.

Careful

Solufen should be used with caution in patients with bleeding disorders, cardiovascular disease or a history of peptic ulcer disease, in patients receiving coumarin anticoagulants, and in patients with renal or hepatic impairment.

interaction

Increased risk of GI bleeding with warfarin, corticosteroids, SSRIs, and aspirin. May decrease the natriuretic effects of diuretics. Reduction of the antihypertensive effects of ACE inhibitors and angiotensin II receptor antagonists. May increase the toxicity of lithium and methotrexate. Increased nephrotoxicity with cyclosporine and tacrolimus.

food interaction

• Avoid alcohol.
• Take with food. Eating reduces irritation.

Solufen alcohol interaction

[Moderate] GENERALLY AVOID:

Concomitant use of aspirin or nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol may result in gastrointestinal (GI) blood loss.

The mechanism may be due to a combined local effect and prostaglandin inhibition, resulting in reduced integrity of the GI lining.

Patients should be informed of this potential interaction and instructed to avoid alcohol while taking aspirin or NSAIDs.

Interaction of solufen hypertension

[Major] Fluid retention and edema have been reported in association with the use of non-steroidal anti-inflammatory drugs (NSAIDs).

Therapy with NSAIDs should be used with caution in patients with a history of fluid retention, hypertension, or heart failure.

Blood pressure and cardiovascular status should be carefully monitored at the start of treatment with NSAIDs and during treatment.

Hypertension Interaction

[Moderate] Nonsteroidal anti-inflammatory drugs (NSAIDs), including topical medications, can cause the return of hypertension or worsen pre-existing hypertension, both of which can contribute to an increased incidence of cardiovascular events.

NSAIDs should be used with caution in patients with hypertension.

Blood pressure should be carefully monitored at the start of NSAID therapy and during therapy.

Solufen drug interaction

Moderate: Duloxetine, duloxetine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids

Not known: diphenhydramine, diphenhydramine, pregabalin, pregabalin, paracetamol, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, alprazolam, alprazolam, cetirizine, cetirizine

Interaction with Solufen disease

Major: asthma, fluid retention, gastrointestinal toxicity, rash, kidney toxicity, thrombosis

Moderate: PKU, anemia, heart failure, hepatotoxicity, hyperkalemia, hypertension, inhibition of platelet aggregation

volume of distribution

The apparent volume of distribution of ibuprofen is 0.1 l/kg.

distance path

It is very well absorbed orally and the maximum serum concentration can be reached in 1 to 2 hours after extravascular administration. When ibuprofen is given immediately after a meal, there is a slight reduction in the rate of absorption but no change in the degree of absorption.

When administered orally, absorption of ibuprofen in adults is very rapid from the upper gastrointestinal tract. Mean Cmax, Tmax, and AUC range from 20 µg/mL, 2 h to 70 µg.h/mL. These parameters may vary depending on the form of the enantiomer, the route of administration and the dose of administration.

half life

The serum half-life of ibuprofen is 1.2 to 2 hours. In patients with hepatic impairment, the half-life may increase to 3.1 to 3.4 hours.

to allow

The elimination rate is between 3 and 13 l/h depending on the route of administration, type of enantiomer and dose.

distance path

Solufen is rapidly metabolized and excreted in the urine, accounting for more than 90% of the dose administered by this route. It is completely eliminated 24 hours after the last dose and almost the entire administered dose is metabolized, representing about 99% of the eliminated dose. Biliary excretion of unchanged drug and phase II active metabolites accounts for 1% of the administered dose.

Briefly, ibuprofen is excreted as metabolites or their conjugates. The elimination of ibuprofen is not affected by advanced age or the presence of renal impairment.

Use during pregnancy and lactation

Solufen is not recommended during pregnancy or for use by nursing mothers.

contraindication

Solufen should not be administered to patients with hypersensitivity to ibuprofen or to individuals with nasal polyps, angioedema, bronchospastic reactivity to aspirin or other non-steroidal anti-inflammatory drugs. Solufen is contraindicated in patients with active or previous peptic ulcer and gastrointestinal ulceration or bleeding.

acute overdose

Gastric lavage, electrolyte correction of blood (if necessary). There is no specific antidote for Solufen.

storage condition

Store in a cool, dry place. Keep away from children.

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