Tiaprofenic Acid

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Czech Republic: Surgam, Thialgin; Denmark: Surgamyl; France: Acide Tiaprofenique, Flanid, Surgam; Germany: Surgam; Hungary: Surgam; Italy: Surgamyl; Luxembourg: Artiflam, Surgam; Malta: Surgam; Netherlands: Surgam; Poland: Apo-Tiapro, Surgam; Portugal: Surgam; Slovakia: Surgam; UK: Surgam.

North America

Canada: Tiaprofenic.

Latin America

Mexico: Surgam.

Asia

Japan: Samnant, Sulimen, Surgam, Surugafen, Tiogam.

Drug combinations

Chemistry

Tiaprofenic Acid: C~14~H~12~O~3~S. Mw: 260.31. 5-Benzoyl-α-methyl-2-thiopheneacetic acid. CAS-33005-95-7.

Pharmacologic Category

Analgesics and Antipyretics; Nonsteroidal Anti-inflammatory Agents; Cyclooxygenase-2 (COX-2) Inhibitors. Disease-modifying Antirheumatic Drugs. (ATC-Code: M01AE11).

Mechanism of action

Reversibly inhibits cyclooxygenase-1 and 2 (COX-1/PTGS1 and COX-2/PTGS2) enzymes, which results in decreased formation of prostaglandin precursors. Has antipyretic, analgesic, and anti-inflammatory properties.

Therapeutic use

Relief of signs and symptoms of rheumatoid arthritis and osteoarthritis.

Pregnancy and lactiation implications

Fetal exposure to NSAIDs late in pregnancy associated with premature closure of ductus arteriosus. 1^st^ trimester miscarriages reported. Enters breast milk; not recommended in lactation.

Unlabeled use

Contraindications

Hypersensitivity to tiaprofenic acid, any component of the formulation, aspirin, or other NSAIDs. Asthma or nasal polyps. Active hepatic disease, renal insufficiency (CrCl <30 mL/minute). Active peptic ulcer or active inflammatory disease of gut (diverticulosis, ulcerative colitis, Crohn’s disease). Pregnancy (3^rd^ trimester).

Warnings and precautions

Fatal asthmatic and anaphylactoid reactions have occurred in «aspirin triad». NSAIDs are associated with increased risk of adverse cardiovascular events, including MI, stroke, and new onset or worsening of pre-existing hypertension (risk may be increased with duration of use or pre-existing cardiovascular risk factors or disease). Use caution with fluid retention, heart failure, or hypertension. Severe cases of cystitis (bladder pain, dysuria, urinary frequency, hematuria) reported. Avoid use in prior history of urinary symptoms. GI bleeding may occur without prior symptoms of GI irritation. Use with caution in history of GI disease. When used concomitantly with ≤325 mg of aspirin, substantial increase in risk of GI complications occurs. Do not administer with asthma (severe bronchospasm may occur). Patients with autoimmune disorders may be at greater risk of developing aseptic meningitis, as rare adverse reaction associated with some NSAIDs. Use with caution in decreased hepatic function. NSAID use may compromise existing renal function. Dose-dependent decreases in prostaglandin synthesis may result from NSAID use, reducing renal blood flow which may cause renal decompensation. Patients with impaired renal function, dehydration, heart failure, liver dysfunction, those taking diuretics, and ACEIs, and the elderly are at greater risk of renal toxicity. Contraindicated in deteriorating function or severe impairment (CrCl <30 mL/minute). Long-term NSAID use may result in renal papillary necrosis. Withhold for at least 4-6 half-lives prior to surgical or dental procedures.

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