BERMIN GRANULES

Indications

• Pain relief
• Fever reduction
• Inflammatory conditions

Dosage

Children: Refer to specific clinical guidelines or product information for paediatric dosing.

Adults: Refer to specific clinical guidelines or product information for adult dosing.

Mechanism of action

Diaceturatephenazone exerts its therapeutic effects primarily through the inhibition of cyclooxygenase (COX) enzymes, which are responsible for converting arachidonic acid into prostaglandins. By inhibiting COX, diaceturatephenazone decreases the levels of prostaglandins, leading to reduced pain and inflammation.

Pharmacodynamics

The pharmacological effects of diaceturatephenazone include analgesia, antipyresis, and anti-inflammatory actions. These effects are due to its ability to inhibit COX enzymes, leading to decreased synthesis of pro-inflammatory mediators. Its onset of action is generally rapid, providing relief from symptoms quickly, while the duration of action may vary based on the dose and individual metabolism.

Pharmacokinetics

Diaceturatephenazone is absorbed following oral administration, with peak plasma concentrations typically occurring within a few hours. It is metabolized in the liver and excreted primarily through the kidneys. The elimination half-life can vary, but it is generally in the range of several hours, which allows for periodic dosing in clinical settings.

Contra-indications

• Hypersensitivity to diaceturatephenazone or any of its components
• Severe hepatic impairment
• Active peptic ulcer disease
• Severe renal impairment
• History of gastrointestinal bleeding

Adverse effects

• Gastrointestinal disturbances (nausea, vomiting, abdominal pain)
• Allergic reactions (rash, urticaria)
• Hepatotoxicity
• Renal impairment
• Blood dyscrasias (e.g., agranulocytosis, thrombocytopenia)
• Headache, dizziness

Interactions

• May enhance the effects of anticoagulants, increasing the risk of bleeding
• Concomitant use with other NSAIDs may increase the risk of gastrointestinal adverse effects
• May affect the metabolism of drugs metabolized by the liver, potentially altering their effectiveness

Precautions

• Use with caution in patients with a history of gastrointestinal disorders
• Monitor liver function during prolonged therapy
• Use with caution in elderly patients and those with cardiovascular disease

Pregnancy

Diaceturatephenazone is generally not recommended during pregnancy due to potential risks to the fetus. Consultation with a healthcare professional is advised.

Breast-feeding

It is advisable to avoid the use of diaceturatephenazone while breastfeeding, as it may be excreted in breast milk and could affect the nursing infant.

Storage

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

Formulations

• Oral tablets
• Oral suspension

Indications

• Trypanosomiasis (sleeping sickness)
• Nagana in livestock
• Infections caused by Trypanosoma brucei
• Infections caused by Trypanosoma congolense

Dosage

Children: Paediatric dosing of diminazene should be derived from the BNF for Children, taking into account the weight and age of the child. Refer to the BNF for Children for specific dosing recommendations.

Adults: The dosage for adults should be determined based on the specific condition and patient factors. Refer to the BNF for accurate dosing guidelines.

Mechanism of action

Diminazene acts by inhibiting the enzyme dihydrofolate reductase, which is crucial for the synthesis of folate in protozoa. This inhibition disrupts the folate metabolic pathway, leading to a decrease in nucleic acid synthesis and ultimately resulting in the death of the protozoan parasites. Additionally, it may interfere with the mitochondrial function of the parasites, further contributing to its antiparasitic effects.

Pharmacodynamics

The pharmacodynamics of diminazene involve its selective action on trypanosomes, with the drug being less toxic to host cells. It has a high affinity for the target enzyme, allowing for effective suppression of protozoan growth. The drug's therapeutic index is favorable, meaning it can effectively treat infections at doses that are relatively safe for the host.

Pharmacokinetics

Diminazene is well-absorbed following parenteral administration. It is widely distributed throughout the body, with a significant volume of distribution. The drug undergoes hepatic metabolism, and its elimination half-life can vary depending on species and individual health. Excretion is primarily via the urine, with metabolites detected in both urine and feces.

Adverse effects

• Anorexia
• Vomiting
• Diarrhoea
• Lethargy
• Neurological signs (e.g., tremors, ataxia)
• Hypersensitivity reactions

Precautions

• Use with caution in animals with hepatic or renal impairment.
• Monitor for signs of toxicity, especially in cases of overdose.

Pregnancy

Safety during pregnancy has not been established; use only if the benefits outweigh the risks.

Breast-feeding

Safety during breastfeeding has not been established; use with caution.

Storage

Store in a cool, dry place away from light. Keep out of reach of children.

Formulations

• Injection solution