ACUDOL 30 INJ

Indications

• Moderate to severe pain
• Postoperative pain management
• Short-term management of pain

Dosage

Children: Refer to the BNF for Children for dosing information in paediatric patients.

Adults: Refer to the BNF for specific dosing recommendations in adults.

Mechanism of action

Ketorolac exerts its effects primarily through the inhibition of cyclooxygenase (COX) enzymes, particularly COX-1 and COX-2, which are crucial for the conversion of arachidonic acid to prostaglandins. By inhibiting these enzymes, ketorolac decreases the production of prostaglandins, which play a significant role in the mediation of pain, inflammation, and fever.

Pharmacodynamics

Ketorolac produces analgesic effects by blocking the formation of prostaglandins, which are responsible for the sensation of pain and the inflammatory response. Unlike other NSAIDs, ketorolac is known for its ability to provide pain relief rapidly, making it suitable for acute pain management. It has a higher potency in analgesic effects compared to other traditional NSAIDs, although it carries a risk of gastrointestinal and renal side effects.

Pharmacokinetics

After administration, ketorolac is rapidly absorbed, with peak plasma concentrations typically occurring within 1 to 2 hours. It has a high protein binding rate, approximately 99%, primarily to albumin. The elimination half-life ranges from 5 to 6 hours in healthy adults, and it is primarily metabolized in the liver via glucuronidation, with renal excretion of metabolites. The pharmacokinetics can be affected by age, renal function, and the presence of other comorbid conditions.

Contra-indications

• Hypersensitivity to ketorolac or any component of the formulation
• Active or history of peptic ulcer disease
• Recent gastrointestinal bleeding or perforation
• Severe renal impairment
• Concurrent use of other NSAIDs or aspirin
• Labor and delivery
• Hypovolemia
• Patients at high risk for bleeding

Adverse effects

• Gastrointestinal bleeding
• Peptic ulcer
• Renal impairment
• Dizziness
• Headache
• Nausea
• Vomiting
• Rash
• Anaphylactic reactions
• Increased blood pressure

Interactions

• Increased risk of gastrointestinal toxicity with other NSAIDs or anticoagulants
• May enhance the effects of other medications that affect renal function
• Caution with diuretics and ACE inhibitors due to potential for renal impairment
• May increase the risk of bleeding when used with antiplatelet agents or anticoagulants

Precautions

• Monitor renal function, especially in patients with pre-existing renal disease
• Use with caution in patients with cardiovascular disease or hypertension
• Assess for signs of gastrointestinal bleeding
• Use the lowest effective dose for the shortest duration necessary
• Evaluate the risk of anaphylaxis in patients with a history of asthma or allergic reactions

Pregnancy

Use is contraindicated in the third trimester due to potential effects on fetal cardiovascular system and risk of prolonged labor.

Breast-feeding

Limited data available; use with caution and evaluate the risks versus benefits.

Storage

Store at room temperature, away from moisture and heat. Protect from light.

Formulations

• Oral tablets
• Injectable solution

Indications

• pH stabilization in intravenous solutions
• buffering agent in pharmaceutical preparations

Dosage

Children: Refer to specific formulations for appropriate use and concentrations as clinical dosing is not standardized for this compound.

Adults: Refer to specific formulations for appropriate use and concentrations as clinical dosing is not standardized for this compound.

Mechanism of action

Tromethamane acts as a proton acceptor, stabilizing the pH of solutions by maintaining a balance between hydrogen ions and hydroxyl ions. When added to a solution, it can neutralize excess acid or base, thus preventing significant alterations in pH levels.

Pharmacodynamics

The pharmacodynamic properties of tromethamane are primarily related to its buffering capacity. It is designed to resist changes in pH, which is crucial in maintaining homeostasis in biological systems. Its ability to stabilize pH can enhance the efficacy and safety of drug formulations, particularly those administered intravenously.

Pharmacokinetics

Tromethamane is not extensively absorbed into the systemic circulation when used as a buffering agent. Its pharmacokinetics are less characterized as it remains mainly in the local environment of the solution it is added to. The elimination and metabolism pathways are not well defined, given its function is predominantly as a stabilizing agent rather than a therapeutic drug.

Pregnancy

Tromethamine is generally considered safe in pregnancy; however, clinical use should be guided by a risk-benefit assessment.

Breast-feeding

Tromethamine is expected to be safe during breastfeeding, but caution is advised and clinical judgment should be applied.

Storage

Store at room temperature, away from light and moisture.