ETHAMATOL DISPERSIBLE TABLETS

Indications

• Anxiety disorders
• Insomnia
• Preoperative sedation

Dosage

Children: Refer to the BNF for Children for accurate paediatric dosing information.

Adults: Refer to specific clinical guidelines and patient factors, as dosing may vary based on individual needs and clinical judgment.

Mechanism of action

Ethamatol acts as a positive allosteric modulator of the GABA-A receptor, enhancing the inhibitory effects of gamma-aminobutyric acid (GABA). This action increases the frequency of chloride channel opening, leading to hyperpolarization of neurons, which results in a sedative and anxiolytic effect.

Pharmacodynamics

The pharmacodynamics of ethamatol are characterized by its ability to decrease neuronal excitability, thereby producing sedation, muscle relaxation, and anxiolysis. The onset of action typically occurs within a short period after administration, contributing to its efficacy in acute anxiety and panic situations. The drug's effects are dose-dependent, with higher doses leading to increased sedation and potential respiratory depression.

Pharmacokinetics

Ethamatol is absorbed rapidly following oral administration, with peak plasma concentrations typically reached within one to two hours. It undergoes hepatic metabolism, primarily through cytochrome P450 enzymes, leading to various metabolites. The elimination half-life is generally short, ranging from a few hours, which supports its use for acute interventions. The drug is excreted mainly through the urine as metabolites, with minimal unchanged drug detected.

Contra-indications

• Hypersensitivity to ethamatol or any of its components.
• Severe liver impairment.
• Acute porphyria.

Adverse effects

• Drowsiness
• Dizziness
• Nausea
• Vomiting
• Allergic reactions
• Hepatic dysfunction

Interactions

• May enhance the sedative effects of central nervous system depressants.
• Potential interaction with anticoagulants, increasing the risk of bleeding.

Precautions

• Use with caution in patients with hepatic impairment.
• Monitor for potential allergic reactions.
• Caution advised in the elderly due to increased sensitivity.

Pregnancy

Use in pregnancy only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Not recommended during breastfeeding due to potential effects on the infant.

Storage

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

Formulations

• Tablets
• Injectable solution