Clobazam: Uses, Interactions, Mechanism Of Action
Clobazam is a drug classified under the benzodiazepine group of medications. It is mainly used for the treatment of epilepsy mostly when other medications for epilepsy prove futile in handling complex partial seizures and other hard to manage seizures. It is also used for the purpose of treating the alleviation of symptoms associated with anxiety but is not to be utilised for anxiety for a long span of time due to issues related with tolerance and dependence.
USES
Lennox-Gastaut Syndrome (LGS): Clobazam is approved for use as an add-on therapy for Lennox-Gastaut syndrome, a severe epilepsy that affects children and is manifested by different types of seizures like atonic, tonic, and absence seizures. Clobazam will also minimise the possibility of these seizures, hence it is used in conjunction with other antiepileptic drugs.
Seizure Disorders: Apart from LGS, clobazam is prescribed for other types of epilepsy especially when other forms of treatment have failed. It is useful in controlling the number and intensity of the seizures when other means of managing seizures have failed.
Anxiety Disorders: Clobazam is sometimes employed for anxiety disorders even when it is a less frequent choice in this category because of the newer sedative anxiolytics. Its sedative properties make it useful for short-term relief of anxiety, but long-term use can lead to dependence and tolerance.
Mechanism Of Action
The mechanism of action of clobazam is quite different since it increases the efficacy of a neurotransmitter called gamma aminobutyric acid (GABA) in the brain. GABA helps balance the activity of nerve cells in the brain and decrease the exaggeration of their activity that could lead to seizure or anxiety. Clobazam is not typical of many other benzodiazepines as it belongs to 1,5−benzodiazepine instead of 1,4−benzodiazepine. This structural variation means that clobazam binds more selectively to GABA-A receptors which increases the effect of the drug compared to other benzodiazepines. This makes it more suitable for long-term treatment of epilepsy.
Interaction
Clobazam is one of those antiepileptic agents that may be administered in combination with other antiepileptic drugs. While these combinations can be effective in reducing seizures, there is a potential for drug interactions:
Valproate: Clobazam when given together with valproate, the plasma levels of its active metabolite, N-desmethyl clobazam are raised, causing high sedation and other CNS side effects.
Inhibitors: Fluconazole, ketoconazole, or clarithromycin are likely to raise clobazam level in the blood stream and increase the sedation effect, along with the likelihood of its side effects as well.
Inducers: Rifampin or phenobarbital may decrease clobazam levels by cutting down the time it takes for the body to process the drug.
Opioids: Co-administration with opioids can increase the risk of profound sedation, respiratory depression, coma, and even death. This combination requires careful monitoring.
Alcohol: Alcohol can amplify the sedative and respiratory depressant effects of clobazam, increasing the risk of accidents or overdose.
Oral Contraceptives: Clobazam can reduce the efficacy of oral contraceptives by inducing the metabolism of their active components. Women taking both medications should use alternative or additional non-hormonal birth control methods to prevent unintended pregnancy.
While clobazam is generally well-tolerated, it carries the risk of side effects, especially when used long-term. Some common side effects include:
Drowsiness and Fatigue: Due to its sedative properties, clobazam can cause significant drowsiness, which may impair cognitive and motor function.
Dizziness: Dizziness and light-headedness are also common, particularly when initiating therapy or increasing doses.
Ataxia: Loss of coordination and balance can occur, especially at higher doses. Behavioural Changes: Clobazam can lead to irritability, agitation, or even aggression, more commonly in children or elderly patients.
Tolerance and Dependence: With prolonged use, patients can develop tolerance to clobazam’s effects, requiring higher doses to achieve the same therapeutic benefit. Additionally, there is a risk of physical dependence, and abrupt discontinuation can lead to withdrawal symptoms.
Respiratory Depression: At high doses or in combination with other CNS depressants, clobazam can cause respiratory depression, which is life-threatening.
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