What is the mechanism of action for celecoxib?
The mechanism of action of celecoxib is due to selective inhibition of cyclooxygenase-2 (COX-2), which is responsible for prostaglandin synthesis, an integral part of the pain and inflammation pathway. [4] This pharmacologic activity gives celecoxib its analgesic, anti-inflammatory, and antipyretic effects.
How is Celebrex processed?
Mechanism of action. Celecoxib prevents the synthesis of a chemical called prostaglandin by inhibiting an enzyme called cyclooxygenase 2 (COX-2). Prostaglandins are important mediators of pain and inflammation in the body.
Is celecoxib a synthetic?
24 Celecoxib Interestingly, its synthetic derivatives show potent activity with reduced toxicity profile and inhibited intracellular proliferation of Francisella in macrophages [126]. Celecoxib has also exhibited a modest activity against S.
What is celecoxib made from?
Celecoxib is hydrophobic (log P is 3.5) and is practically insoluble in aqueous media at physiological pH range. The inactive ingredients in CELEBREX include: croscarmellose sodium, edible inks, gelatin, lactose monohydrate, magnesium stearate, povidone and sodium lauryl sulfate.
What are the pharmacokinetics of celecoxib?
After oral administration, celecoxib is rapidly absorbed and achieves peak serum concentration in approximately 3 h. It is extensively metabolized in the liver, with very little drug (< 3%) being eliminated unchanged [17]. The major routes of excretion for celecoxib are feces and urine [18].
How is celecoxib metabolized?
It is extensively metabolized in the liver, with very little drug (< 3%) being eliminated unchanged [17]. The major routes of excretion for celecoxib are feces and urine [18]. Celecoxib is metabolized primarily through methyl hydroxylation to form hydroxycelecoxib.
How prostaglandins are synthesized?
Prostaglandins and thromboxane A2 (TXA2), collectively termed prostanoids, are formed when arachidonic acid (AA), a 20-carbon unsaturated fatty acid, is released from the plasma membrane by phospholipases (PLAs) and metabolized by the sequential actions of prostaglandin G/H synthase, or cyclooxygenase (COX), and …
Is celecoxib a prodrug?
N-succinylaspart-1-yl celecoxib is a potential colon-specific prodrug of celecoxib with improved therapeutic properties. J Pharm Sci. 2012 May;101(5):1831-42. doi: 10.1002/jps.
What is the chemical formula of celecoxib?
C17H14F3N3O2SCelecoxib / Formula
What is prostaglandin synthesis?
Prostaglandin synthesis is initiated by the interaction of various hormones (e.g. bradykinin, angiotensin II, thrombin) with their cognate cell surface receptors (Figs. 2 and 3). Hormonal stimulation results in the activation of one or more cellular lipases.
How NSAIDs inhibit the prostaglandin synthesis?
Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used for their anti-inflammatory, analgesic, and antipyretic effects. NSAIDs generally work by blocking the production of prostaglandins (PGs) through the inhibition of two cyclooxygenase enzymes.
Which drugs inhibit synthesis of prostaglandins?
Aspirin and a large number of nonsteroidal anti-inflammatory drugs act primarily through the inhibition of prostaglandin synthesis by inhibiting the enzyme cyclooxygenase.
What is the pH of celecoxib?
The solubility of celecoxib was not influenced by the physiological pH condition (1.0–7.5) since the pKa of celecoxib is 11.1.
Is Celebrex water soluble?
On the basis of biopharmaceutics classification system (BCS), celecoxib is a type 2 drug (low water solubility (<5 μg·mL−1) and high permeability), where dissolution is the rate limiting step for the absorption of a drug.
How do COX inhibitors work?
What are COX-2 inhibitors, and how do they work? COX-2 inhibitors are a subclass of nonsteroidal antiinflammatory drugs (NSAIDs). NSAIDs work by reducing the production of prostaglandins, chemicals that promote inflammation, pain, and fever.
What is the mechanism of action of celecoxib?
The mechanism of action of celecoxib is due to selective inhibition of cyclooxygenase-2 (COX-2), which is responsible for prostaglandin synthesis, an integral part of the pain and inflammation pathway.[4] This pharmacologic activity gives celecoxib its analgesic, anti-inflammatory, and antipyretic effects.
How does celecoxib affect prostaglandin?
This is an enzyme, something that speeds up biochemical reactions. Celecoxib decreases the activity of this enzyme. The activity of this enzyme is, in the end, responsible for the formation of prostaglandins. In other words, celecoxib inhibits prostaglandin synthesis. But what is prostaglandin and why is its inhibition important?
Is celecoxib an anti-inflammatory?
A highly selective reversible inhibitor of the COX-2 isoform of cyclooxygenase, celecoxib inhibits the transformation of arachidonic acid to prostaglandin precursors. Therefore, it has antipyretic, analgesic and anti-inflammatory properties.
Is celecoxib a COX-2 inhibitor?
Specifically, celecoxib is a COX-2 selective NSAID at therapeutic concentrations. Put another way, it is a COX-2 inhibitor. By decreasing the activity of this enzyme, COX-2 (cyclooxygenase-2), fewer prostaglandins are made.