ETOVAC SP

Indications

• Pain and inflammation in musculoskeletal disorders
• Acute gout
• Osteoarthritis
• Rheumatoid arthritis
• Ankylosing spondylitis

Dosage

Children: For children aged 16-17 years, the recommended dose is 120 mg once daily for a maximum of 8 days.

Adults: 120 mg once daily for a maximum of 8 days.

Mechanism of action

Etoricoxib selectively inhibits isoform 2 of the cyclo-oxygenase enzyme (COX-2), preventing the conversion of arachidonic acid to prostaglandins (PGs), which are mediators of inflammation and pain. This selective inhibition results in reduced inflammatory responses without significantly affecting the COX-1 pathway, which is important for maintaining gastrointestinal mucosal integrity.

Pharmacodynamics

Etoricoxib exhibits a high selectivity for COX-2, being about 106 times more selective for COX-2 than for COX-1. This selective action minimizes the gastrointestinal side effects commonly associated with non-selective NSAIDs, as COX-1 plays a protective role in the gastric mucosa. Etoricoxib provides analgesic and anti-inflammatory effects by lowering prostaglandin levels involved in the inflammatory process.

Pharmacokinetics

Etoricoxib is well-absorbed following oral administration, with peak plasma concentrations typically occurring about 1 to 2 hours after ingestion. The drug has a half-life of approximately 22 hours, allowing for once-daily dosing. It is extensively metabolized in the liver, primarily via CYP2C9 and CYP3A4 pathways, and is excreted mainly through urine as metabolites. The presence of food does not significantly affect its absorption.

Contra-indications

• Active gastrointestinal bleeding
• Active gastrointestinal ulceration
• Severe cutaneous adverse reactions (SCARs)
• Cerebrovascular disease
• Uncontrolled hypertension (persistently above 140/90 mmHg)
• Severe renal failure
• Hypersensitivity to aspirin or other NSAIDs
• Ischaemic heart disease
• Active inflammatory bowel disease

Adverse effects

• Hypertension
• Fluid retention
• Gastrointestinal discomfort
• Nausea
• Vomiting
• Headache
• Dizziness
• Chest pain
• Heart failure
• Palpitations
• Skin reactions
• Malaise
• Nephrotoxicity
• Insomnia
• Anemia
• Visual impairment
• Aseptic meningitis
• Tinnitus

Interactions

• Increased exposure when used with combined hormonal contraceptives
• Increased exposure when used with hormone replacement therapy
• May interact with other NSAIDs

Precautions

• Caution in patients with cardiac impairment
• Caution in patients with renal impairment
• Dehydration risk
• Caution in patients with allergic disorders
• May mask symptoms of infection

Pregnancy

Avoid unless the potential benefit outweighs the risk, especially during the third trimester due to risk of closure of the fetal ductus arteriosus.

Breast-feeding

Use with caution during breastfeeding; the manufacturer advises avoiding use if possible.

Storage

Store in a cool, dry place, away from direct sunlight, and out of reach of children.

Formulations

• Modified-release tablet
• Dispersible tablet
• Oral suspension
• Oral solution

Indications

• Chronic pain conditions
• Postoperative swelling
• Traumatic injuries
• Sinusitis
• Bronchitis

Dosage

Children: Refer to the BNF for Children for appropriate dosing information.

Adults: Refer to the BNF for appropriate dosing information.

Mechanism of action

Serratiopeptidase exerts its effects primarily through the breakdown of proteins and the modulation of inflammatory processes. It acts by hydrolyzing peptide bonds in proteins, which can lead to the dissolution of dead or damaged tissue and the reduction of inflammatory mediators, thus attenuating pain and swelling. This enzymatic action helps to improve tissue repair and healing.

Pharmacodynamics

The pharmacodynamics of serratiopeptidase involve its ability to modulate inflammation and pain through its proteolytic activity. By breaking down inflammatory mediators and promoting tissue healing, serratiopeptidase can enhance recovery from various inflammatory conditions. Its analgesic properties may also be attributed to the reduction of bradykinin and other inflammatory substances that contribute to pain.

Pharmacokinetics

Serratiopeptidase is absorbed in the gastrointestinal tract, with its bioavailability influenced by the presence of food. Once in the bloodstream, it distributes to tissues where it exerts its proteolytic effects. The enzyme is metabolized primarily in the liver, and its elimination half-life is variable, depending on individual patient factors. Renal function may also play a role in the clearance of serratiopeptidase and its metabolites.

Pregnancy

There is insufficient evidence regarding the safety of serratiopeptidase during pregnancy. Consult healthcare professionals before use.

Breast-feeding

Limited data are available on the excretion of serratiopeptidase in breast milk. Caution is advised when administering to nursing mothers.

Storage

Store in a cool, dry place, away from direct sunlight and moisture. Keep out of reach of children.

Formulations

• {'name': 'Serratiopeptidase tablet', 'strength': '10 mg', 'route': 'oral'}
• {'name': 'Serratiopeptidase capsule', 'strength': '20 mg', 'route': 'oral'}

Mechanism of action

Like any other COX-2 selective inhibitor Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2), preventing production of prostaglandins (PGs) from arachidonic acid.

Pharmacodynamics

Etoricoxib is a COX-2 selective inhibitor (approximately 106 times more selective for COX-2 inhibition over COX-1).