Norilafin

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

Norilafin is a non-steroidal antirheumatic agent possessing anti-inflammatory, analgesic and anti-pyretic properties. Prostaglandin synthetase inhibition is probably the basis of the mechanism of action of non-steroidal anti-inflammatory agents. Following absorption, Norilafin undergoes two major transformations. It is oxidised to the sulphone and then reversibly reduced to the sulphide. The sulphide metabolite is the biologically active form which is an inhibitor of prostaglandin synthesis.

Norilafin is a non-steroidal anti-inflammatory indene derivative, also possessing analgesic and antipyretic activities.

Trade Name Norilafin
Availability Prescription only
Generic Sulindac
Sulindac Other Names Sulindac, Sulindaco, Sulindacum
Related Drugs Humira, Buprenex, aspirin, prednisone, ibuprofen, acetaminophen, tramadol, meloxicam, naproxen, Tylenol
Type
Formula C20H17FO3S
Weight Average: 356.411
Monoisotopic: 356.088243305
Protein binding

At 1 mcg/ml concentrations, approximately 93% sulindac and 98% of its sulfide metabolite are bound to human serum albumin.

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

Uses

Norilafin is used for the symptomatic treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, periarticular inflammatory disorders, acute painful shoulder (acute subacromial bursitis/ supraspinatus tendinitis), acute gouty arthritis.

Norilafin is also used to associated treatment for these conditions: Ankylosing Spondylitis (AS), Colorectal Polyps, Gouty Arthritis, Osteoarthritis (OA), Rheumatoid Arthritis, Tendonitis exacerbated, Acute Subacromial bursitis, Acute supraspinatus tendinitis

How Norilafin works

Norilafin's exact mechanism of action is unknown. Its antiinflammatory effects are believed to be due to inhibition of both COX-1 and COX-2 which leads to the inhibition of prostaglandin synthesis. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.

Dosage

Norilafin dosage

The usual dosage is 100 mg to 200 mg twice a day, although dosages should be optimized for each individual. The maximal daily dose is 400 mg. Therapy for seven days in acute gouty arthritis and for seven to fourteen days in acute painful shoulder is usually sufficient. After a satisfactory response has been achieved, the dosage may be reduced according to the response. Norilafin should be taken with food

Side Effects

Gastrointestinal side effects are the most common and consist of abdominal pain, nausea and constipation. Gastrointestinal ulceration and bleeding may also occur. The most frequently reported central nervous system side effects are drowsiness, dizziness, headache and nervousness. Other adverse effects include depression, tinnitus, confusion, light-headedness, insomnia, psychiatric disturbances, syncope, convulsions, coma, peripheral neuropathy, blurred vision and other ocular effects, oedema and mass gain, hypertension, hematuria, skin rashes, pruritus, urticaria, stomatitis, alopecia and hypersensitivity reactions. A hypersensitivity syndrome consisting of fever and chills, skin rashes or other cutaneous manifestations, hepatotoxicity, renal toxicity (including renal failure), leukopenia, thrombocytopenia, eosinophilia, inflammed glands or lymph nodes, and arthralgia have been reported. Leucopenia, purpura, thrombocytopenia, aplastic anaemia, haemolytic anaemia, agranulocytosis, epitaxis, hyperglycaemia, hyperkalaemia and vaginal bleeding have been reported. There have also been reports of hepatitis and jaundice or renal failure.

Toxicity

Acute oral toxicity (LD50) in rats is 264 mg/kg. Cases of overdose have been reported and rarely, deaths have occurred. The following signs and symptoms may be observed following overdose: stupor, coma, diminished urine output and hypotension.

Precaution

Patients intolerant of one of the non-steroidal anti-inflammatory analgesics, including Aspirin, may be intolerant of Norilafin.

Interaction

Norilafin and its sulphide metabolite are highly protein bound. Patients should be monitored carefully until it is certain that no change in their anticoagulant or hypoglycaemic dosage is required. Aspirin has been shown to decrease the bioavailability of the active sulfide metabolite of Norilafin. The combination showed an increase in the incidence of gastrointestinal side-effects, without providing additional symptomatic relief, and is therefore not recommended. Prolonged concurrent use of Paracetamol with Norilafin may increase the risk of adverse renal effects. It is recommended that patients be under close medical supervision while receiving such combined therapy. Probenecid may increase the plasma concentration of Norilafin and its sulfone metabolite, and slightly decrease the plasma concentration of the active sulfide metabolite.

Food Interaction

  • Avoid alcohol. Ingesting alcohol may increase the risk of gastrointestinal bleeding.
  • Take with food.

Norilafin 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.

Norilafin Hypertension interaction

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

Therapy with NSAIDs should be administered cautiously in patients with preexisting fluid retention, hypertension, or a history of heart failure.

Blood pressure and cardiovascular status should be monitored closely during the initiation of NSAID treatment and throughout the course of therapy.

Hypertension interaction

[Moderate] Nonsteroidal anti-inflammatory drugs (NSAIDs), including topicals, can lead to new onset of hypertension or worsening of preexisting hypertension, either of which can contribute to the increased incidence of cardiovascular events.

NSAIDs should be used with caution in patients with hypertension.

Blood pressure should be monitored closely during the initiation of NSAID therapy and throughout the course of therapy.

Elimination Route

Approximately 90% absorbed in humans following oral administration.

Half Life

The mean half-life of sulindac is 7.8 hours while the mean half-life of the sulfide metabolite is 16.4 hours.

Clearance

  • Renal cl=68.12 +/- 27.56 mL/min [NORMAL (19-41 yrs)]

Elimination Route

Norilafin is excreted in rat milk; concentrations in milk were 10 to 20% of those levels in plasma. It is not known if sulindac is excreted in human milk. Approximately 50% of the administered dose of sulindac is excreted in the urine with the conjugated sulfone metabolite accounting for the major portion. Hepatic metabolism is an important elimination pathway.

Pregnancy & Breastfeeding use

Use in pregnancy: Norilafin should be used during the first two trimesters of pregnancy only if the potential benefit justifies the potential risk to the foetus. Use of Norilafin during the third trimester of pregnancy is not recommended.

Use in lactation: It is not known whether Norilafin is excreted in human milk. So a decision should be made whether to discontinue nursing or discontinue the medicine taking into account the importance of the medicine to the mother.

Contraindication

Patients known to be allergic to Norilafin and those in whom acute asthmatic attacks, urticaria or rhinitis have been precipitated by Aspirin or other non-steroidal anti-inflammatory agents. Norilafin is also contraindicated in patients with a history of active gastro-intestinal bleeding or peptic ulceration. It should not be given to children, pregnant or lactating women.

Special Warning

Patient with renal impairment: Norilafin should be administered with caution to patients with impaired renal function and to those with bleeding disorders, epilepsy, parkinsonism or psychiatric disorders.

Patient with hepatic impairment: In the presence of liver function impairment the half life of Norilafin is prolonged and a reduction of daily dosage may be required.

Acute Overdose

Reported symptoms have generally reflected the gastro-intestinal, renal and central nervous system toxicities of Norilafin. Treatment is symptomatic and supportive.

Storage Condition

Store in a cool and dry place protected from light. Keep out of reach of children.

Innovators Monograph

You find simplified version here Norilafin

Norilafin contains Sulindac see full prescribing information from innovator Norilafin Monograph, Norilafin MSDS, Norilafin FDA label

FAQ

What is Norilafin used for?

Norilafin is used to relieve pain, tenderness, swelling, and stiffness caused by osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.

How safe is Norilafin?

Dangerous stomach problems warning,Taking Norilafin increases your risk of stomach bleeding, ulcers, or small holes in the lining of your digestive system, which can be fatal. These events may occur at any time and without any symptoms.

How does Norilafin work?

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

What are the common side effects of Norilafin?

The more common side effects of Norilafin are include:

  • stomach pain.
  • heartburn.
  • nausea.
  • diarrhea.
  • constipation.
  • rash.
  • dizziness.
  • headache.


Is Norilafin safe during pregnancy?

Norilafin during pregnancy only in life-threatening emergencies when no safer drug is available.If you are pregnant, you should not take  Norilafin unless your doctor tells you to.

Is Norilafin safe during breastfeeding?

Norilafin is considered safe for use while breastfeeding.

Can I drink alcohol with Norilafin?

Do not drink alcohol while taking Norilafin. Alcohol can increase your risk of stomach bleeding caused by Norilafin.

Can I drive after taking Norilafin?

If affected, patients should not drive or operate machinery.

How quickly does Norilafin work?

Norilafin usually begins to work within one week, but in severe cases up to two weeks or even longer may pass before you begin to feel better.

Can I take Norilafin for a long time?

Norilafin oral tablet is used for short-term treatment when used for shoulder pain or gouty arthritis. It may be a long-term treatment when used for osteoarthritis, rheumatoid arthritis, or ankylosing spondylitis.

When is the best time to take Norilafin?

Norilafin should always be taken with fluids either with food or immediately after food and is normally taken twice a day.

Can I take Norilafin on an empty stomach?

It is best to take this medicine with food. Also drink extra fluids so you will pass more urine while you are using this medicine.

Does sulindac make you sleepy?

Norilafin oral tablet doesn't cause drowsiness, but it can cause other side effects.

Can Norilafin cause weight gain?

Norilafin can causes weight gain also with other side effects.

Is Norilafin hard on the kidneys?

Norilafin has been hypothesized to have decreased adverse renal effects because of its decreased inhibition and rapid renal metabolism.

Does Norilafin cause hair loss?

Some anti-inflammatory drugs that can cause hair lossas as like Norilafin.

Can Norilafin cause liver damage?

Norilafin can also cause acute liver injury with a more delayed latency with few or no features of hypersensitivity.

Can I overdose on Norilafin?

Norilafin is for information only and not for use in the treatment or management of an actual overdose . do not use it to treat or manage an actual overdose.

Who should not take Norilafin?

Norilafin can increase your risk of fatal heart attack or stroke. Do not use Norilafin just before or after heart bypass surgery. Norilafin may also cause stomach or intestinal bleeding, which can be fatal.

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

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