Disalicylsäure

Disalicylsäure Uses, Dosage, Side Effects, Food Interaction and all others data.

The mode of anti-inflammatory action of salsalate and other nonsteroidal anti-inflammatory drugs is not fully defined, but appears to be primarily associated with inhibition of prostaglandin synthesis. This inhibition of prostaglandin synthesis is done through the inactivation of cyclooxygenase-1 (COX-1) and COX-2, which are reponsible for catalyzing the formation of prostaglandins in the arachidonic acid pathway. Although salicylic acid (the primary metabolite of salsalate) is a weak inhibitor of prostaglandin synthesis in vitro, salsalate appears to selectively inhibit prostaglandin synthesis in vivo, providing anti-inflammatory activity equivalent to aspirin and indomethacin. Unlike aspirin, salsalate does not inhibit platelet aggregation.

Disalicylsäure is a nonsteroidal anti-inflammatory agent for oral administration. Disalicylsäure's mode of action as an anti-inflammatory and antirheumatic agent may be due to inhibition of synthesis and release of prostaglandins. The usefulness of salicylic acid, the active in vivo product of salsalate, in the treatment of arthritic disorders has been established. In contrast to aspirin, salsalate causes no greater fecal gastrointestinal blood loss than placebo.

Trade Name Disalicylsäure
Availability Prescription only
Generic Salsalate
Salsalate Other Names Disalicylic acid, Disalicylsäure, O-Salicylcylsalicylsäure, o-Salicylsalicylic acid, Salicylic acid bimolecular ester, Salicyloxysalicylic acid, Salicyloylsalicylic acid, Salicylsalicylic acid, Salsalate, Salsalato, Salsalatum, Sasapyrin, Sasapyrine, Sasapyrinum
Related Drugs Humira, aspirin, prednisone, ibuprofen, meloxicam, naproxen, Cymbalta, hydroxychloroquine, Enbrel, Remicade
Type
Formula C14H10O5
Weight Average: 258.2262
Monoisotopic: 258.05282343
Protein binding

Salicylate: 90-95% bound at plasma salicylate concentrations 400 mcg/mL.

Groups Approved
Therapeutic Class Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs)
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Disalicylsäure
Disalicylsäure

Uses

Disalicylsäure is used for relief of the signs and symptoms of rheumatoid arthritis, osteoarthritis and related rheumatic disorders, pain, fever and inflammation.

How Disalicylsäure works

The mode of anti-inflammatory action of salsalate and other nonsteroidal anti-inflammatory drugs is not fully defined, but appears to be primarily associated with inhibition of prostaglandin synthesis. This inhibition of prostaglandin synthesis is done through the inactivation of cyclooxygenase-1 (COX-1) and COX-2, which are reponsible for catalyzing the formation of prostaglandins in the arachidonic acid pathway. Although salicylic acid (the primary metabolite of salsalate) is a weak inhibitor of prostaglandin synthesis in vitro, salsalate appears to selectively inhibit prostaglandin synthesis in vivo, providing anti-inflammatory activity equivalent to aspirin and indomethacin. Unlike aspirin, salsalate does not inhibit platelet aggregation.

Dosage

Disalicylsäure dosage

Adults: The usual dosage is 3000 mg daily, given in divided doses as follows:

  • Two doses of two 750 mg tablets
  • Two doses of three 500 mg tablets/capsules
  • Three doses of two 500 mg tablets/capsules

Some patients, e.g., the elderly, may require a lower dosage to achieve therapeutic blood concentrations and to avoid the more common side effects such as auditory.

Alleviation of symptoms is gradual, and full benefit may not be evident for 3 to 4 days, whenplasmasalicylate levels have achieved steady state. There is no evidence for development of tissue tolerance (tachyphylaxis) but salicylate therapy may induce increased activity of metabolizing liver enzymes, causing a greater rate of salicyluric acid production and excretion, with a resultant increase in dosage requirement for maintenance of therapeuticserumsalicylate levels.

Children: Dosage recommendations and indications for Disalicylsäure use in children have not been established.

Should be taken with food. Take with food or milk.

Side Effects

GI symptoms, hypersensitivity reactions, skin eruptions, angioedema, weakness, rhinitis and dyspnoea, hypoprothrombinaemia. Hepatotoxicity, renal impairment, iron-deficiency anaemia, occult bleeding. Local irritation (rectally); Reye's syndrome.

Toxicity

Death has followed ingestion of 10 to 30 g of salicylates in adults, but much larger amounts have been ingested without fatal outcome.

Precaution

Peptic ulcers; asthma, allergic disorders. Impaired hepatic or renal function. Dehydrated patients; uncontrolled hypertension. May cause acute haemolytic anaemia in patients with G6PD deficiency.

Interaction

May increase risk of liver damage when used with gold compounds. GI effects may be enhanced with alcohol or concurrent use with corticosteroids. May increase activity of coumarin anticoagulants, sulfonylureas, zafirlukast, methotrexate, phenytoin and valproate. May decrease the activity of probenecid and sulfinpyrazone.

Food Interaction

  • Avoid excessive or chronic alcohol consumption. Ingesting alcohol may increase the risk of developing a gastrointestinal bleed.
  • Take with or without food. Taking salsalate with food may slow the absorption of salsalate but does not significantly impact the Cmax or AUC.

Disalicylsäure Alcohol interaction

[Moderate] GENERALLY AVOID:

The concurrent use of aspirin or nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol may lead to gastrointestinal (GI) blood loss.

The mechanism may be due to a combined local effect as well as inhibition of prostaglandins leading to decreased integrity of the GI lining.



Patients should be counseled on this potential interaction and advised to refrain from alcohol consumption while taking aspirin or NSAIDs.

Elimination Route

Disalicylsäure is insoluble in acid gastric fluids (< 0.1 mg/ml at pH 1.0), but readily soluble in the small intestine where it is partially hydrolyzed to two molecules of salicylic acid. A significant portion of the parent compound is absorbed unchanged. The amount of salicylic acid available from salsalate is about 15% less than from aspirin, when the two drugs are administered on a salicylic acid molar equivalent basis (3.6 g salsalate/5 g aspirin). Food slows the absorption of all salicylates including salsalate.

Half Life

The parent compound has an elimination half-life of about 1 hour. Salicylic acid (the active metabolite) biotransformation is saturated at anti-inflammatory doses of salsalate. Such capacity limited biotransformation results in an increase in the half-life of salicylic acid from 3.5 to 16 or more hours.

Pregnancy & Breastfeeding use

Pregnancy Category C. Disalicylsäure and salicylic acid have been shown to be teratogenic and embryocidal in rats when given in doses 4 to 5 times the usual human dose. The effects were not observed at doses twice as great as the usual human dose. There are no adequate and well-controlled studies in pregnantwomen. Disalicylsäure should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers: It is not known whether salsalate per se is excreted in human milk; salicylic acid, the primary metabolite of Disalicylsäure , has been shown to appear in human milk in concentrations approximating the maternal blood level. Thus, the infant of a mother on Disalicylsäure therapy might ingest in mother†s milk 30 to 80% as much salicylate per kg body weight as the mother is taking. Accordingly, caution should be exercised when Disalicylsäure is administered to a nursing woman.

Contraindication

Haemophilia, haemorrhagic disorders, gout, hypersensitivity to aspirin or NSAIDs. Children <12 yr. Pregnancy (3rd trimester) and lactation. Severe renal or hepatic impairment.

Acute Overdose

Symptoms: Tinnitus, vertigo, headache, confusion, drowsiness, sweating, hyperventilation, vomiting and diarrhea will occur. More severe intoxication will lead to disruption of electrolyte balance and blood pH, and hyperthermia and dehydration.

Treatment: Further absorption of Disalicylsäure from the G.I. tract should be prevented by emesis (syrup of ipecac) and if necessary, by gastric lavage. Fluid and electrolyte imbalance should be corrected by the administration of appropriate I.V. therapy. Adequate renal function should be maintained. Hemodialysis or peritoneal dialysis may be required in extreme cases.

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FAQ

What is Disalicylsäure used for?

Disalicylsäure is used to relieve pain, tenderness, swelling, and stiffness caused by rheumatoid arthritis arthritis caused by swelling of the lining of the joints, osteoarthritis arthritis caused by a breakdown of the lining of the joints, and other conditions that cause swelling.

How safe is Disalicylsäure?

Disalicylsäure can increase your risk of fatal heart attack or stroke, even if you don't have any risk factors. Do not use Disalicylsäure just before or after heart bypass surgery. Disalicylsäure may also cause stomach or intestinal bleeding, which can be fatal.

What are the common side effects of Disalicylsäure?

Common side effects of Disalicylsäure include: 

  • upset stomach,
  • heartburn, or
  • mild dizziness.

How does Disalicylsäure work?

It works by stopping the body's production of a substance that causes pain, fever, and swelling.

Does Disalicylsäure reduce inflammation?

As a consequence, inflammation, pain and fever are reduced.Disalicylsäure is as strong as aspirin in reducing inflammation but has less effect on blood clotting than aspirin.

Is Disalicylsäure a salicylate?

Disalicylsäure is an orally available salicylate and non-steroidal anti-inflammatory drug, with anti-inflammatory, analgesic and antipyretic activities.

Is Disalicylsäure hard on the kidneys?

Disalicylsäure can cause a hemodynamically mediated acute renal failure in patients at risk for this nephropathy.

Does Disalicylsäure raise blood pressure?

Disalicylsäure is considered to have little or no effect on blood pressure.

Is Disalicylsäure safe during pregnancy?

Use should be avoided during the third trimester of pregnancy.Use only if potential benefit justifies the potential risk to the fetus. Comments: Avoid use in late pregnancy as it may cause premature closure of the ductus arteriosus.

Is Disalicylsäure safe during breastfeeding?

Disalicylsäure appears in breast milk at levels close to maternal blood levels. This may cause adverse effects in the infant. Nursing women should avoid nursing while taking Disalicylsäure or use alternate drugs.

Can I drink alcohol with Disalicylsäure?

Avoid drinking alcohol. Heavy drinking can increase your risk of stomach bleeding.

Can I drive after taking Disalicylsäure?

Do not drive, use machinery, or do anything that needs alertness until you can do it safely.

Does Disalicylsäure make me sleepy?

Disalicylsäure may causes tiredness also with other side effects.

How long does Disalicylsäure take to work?

Disalicylsäure may take three to four days until you feel the full benefit of the medication.

Is Disalicylsäure a narcotic?

Disalicylsäure is a nonsteroidal anti-inflammatory drug  in a group of drugs called salicylates used to reduce pain, swelling, and joint stiffness caused by arthritis.

Can Disalicylsäure be crushed?

Do not crush them or break them up before taking. The tablets must be swallowed whole.

How long does Disalicylsäure stay in my system?

It may take three to four days until you feel the full benefit of the medication.

Who should not take Disalicylsäure?

You should not use Disalicylsäure if you have severe kidney disease, or if you have ever had a severe allergic reaction after taking aspirin, an nonsteroidal anti-inflammatory drug or other salicylates.

What happens if I miss a dose of Disalicylsäure?

Since Disalicylsäure is used when needed, you may not be on a dosing schedule. Skip any missed dose if it's almost time for your next dose. Do not use two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include ringing in your ears, headache, confusion, severe dizziness or drowsiness, sweating, fast breathing, severe vomiting or diarrhea.

*** Taking medicines without doctor's advice can cause long-term problems.
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