DOLOACT PLUS TABLETS

Indications

• Osteoarthritis
• Rheumatoid arthritis
• Ankylosing spondylitis
• Pain management in musculoskeletal disorders
• Postoperative pain

Dosage

Children: Refer to the BNF for Children for specific paediatric dosing guidelines.

Adults: Refer to the BNF for specific dosing guidelines as they vary based on the condition being treated.

Mechanism of action

Aceclofenac exerts its effects by inhibiting the cyclooxygenase (COX) enzymes, particularly COX-2, which play a crucial role in the conversion of arachidonic acid to prostaglandins. Prostaglandins are mediators of inflammation and pain. By reducing the synthesis of these inflammatory mediators, aceclofenac decreases inflammation, pain, and fever.

Pharmacodynamics

The pharmacodynamic effects of aceclofenac include its ability to reduce inflammation, alleviate pain, and improve joint function. The drug also has antipyretic properties. The onset of action is typically seen within a few hours after administration, with peak effects occurring within 1 to 2 days. The anti-inflammatory effects are attributed to the inhibition of prostaglandin synthesis, which is crucial in the inflammatory response.

Pharmacokinetics

Aceclofenac is rapidly absorbed from the gastrointestinal tract, with peak plasma concentrations occurring approximately 1 to 2 hours after oral administration. It has a bioavailability of about 50% due to first-pass metabolism. The drug is extensively metabolized in the liver, mainly through glucuronidation, and is eliminated primarily via the urine. The elimination half-life of aceclofenac is approximately 4 hours, but this can be affected by hepatic function. Dose adjustments may be necessary in patients with liver impairment.

Contra-indications

• Active peptic ulcer disease
• Severe heart failure
• Hypersensitivity to aceclofenac or any excipients
• History of gastrointestinal bleeding or perforation related to previous NSAID therapy
• Severe liver or renal impairment

Adverse effects

• Gastrointestinal disturbances (nausea, vomiting, diarrhea, dyspepsia)
• Increased risk of cardiovascular events
• Renal impairment
• Hepatic dysfunction
• Allergic reactions (rash, urticaria)
• Headache
• Dizziness

Interactions

• Increased risk of gastrointestinal bleeding with other NSAIDs or anticoagulants
• Potentially reduced antihypertensive effect when used with ACE inhibitors or diuretics
• May enhance the effects of anticoagulants
• Caution with methotrexate, as it may enhance toxicity

Precautions

• Use with caution in patients with a history of gastrointestinal disease
• Monitor renal function in long-term use
• Caution in elderly patients due to increased risk of adverse effects
• Assess cardiovascular risk before use in patients with pre-existing conditions

Pregnancy

Use in pregnancy should be avoided, especially in the third trimester, due to potential effects on fetal cardiovascular system and risk of premature closure of the ductus arteriosus.

Breast-feeding

Use with caution, as it is not known if aceclofenac is excreted in human milk.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Tablets (100 mg)
• Suppositories (100 mg)

Indications

• Pancreatitis
• Surgical procedures requiring protein digestion
• Post-operative recovery
• Inflammatory conditions

Dosage

Children: Refer to established clinical guidelines for dosing recommendations.

Adults: Refer to established clinical guidelines for dosing recommendations.

Mechanism of action

Chymotrypsin functions by cleaving peptide bonds at the carboxyl side of aromatic amino acids, such as tryptophan, phenylalanine, and tyrosine. This proteolytic activity reduces the size of protein molecules, facilitating their absorption and utilization in the body. The enzyme's action is highly specific and efficient, contributing to the overall digestive process.

Pharmacodynamics

Chymotrypsin exhibits its effects primarily through its enzymatic activity, enhancing the digestion of dietary proteins and facilitating nutrient absorption. Additionally, it may exert anti-inflammatory effects by modulating the immune response and reducing edema in tissues. Its activity is influenced by factors such as pH, temperature, and the presence of other ions or molecules in the digestive system.

Pharmacokinetics

Chymotrypsin is administered orally or via injection, where it is absorbed through the gastrointestinal tract or directly into the bloodstream. Once in circulation, it is distributed to tissues where it exerts its enzymatic effects. The enzyme is subject to degradation by proteolytic enzymes in the body, and its activity can be influenced by the physiological state of the patient, including factors such as age, health status, and concurrent medications. The half-life of chymotrypsin varies based on the route of administration and individual patient factors.

Contra-indications

• Hypersensitivity to chymotrypsin or any component of the formulation
• Active bleeding disorders
• History of gastrointestinal ulcers
• Severe renal impairment

Adverse effects

• Allergic reactions including rash, itching, and anaphylaxis
• Gastrointestinal disturbances such as nausea, vomiting, and diarrhea
• Local irritation at the injection site
• Increased risk of bleeding due to its proteolytic activity

Interactions

• May enhance the effects of anticoagulants due to increased proteolytic activity
• Use with caution in patients taking other medications that affect hemostasis
• No significant drug-drug interactions are well documented

Precautions

• Use with caution in patients with a history of allergic reactions
• Monitor for signs of bleeding in patients with compromised hemostasis
• Assess renal function before administration in patients with renal impairment

Pregnancy

Chymotrypsin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus, as studies on its safety in pregnant women are lacking.

Breast-feeding

It is not known whether chymotrypsin is excreted in human milk. Caution should be exercised when administering to nursing women.

Storage

Store at room temperature, away from light and moisture. Keep out of reach of children.

Formulations

• Chymotrypsin injection solution
• Chymotrypsin enteric-coated tablets