Clobazam
Clobazam Uses, Dosage, Side Effects, Food Interaction and all others data.
Clobazam binds to one or more specific GABA receptors at several sites within the CNS including the limbic system and reticular formation. Increased permeability of neuronal membrane to chloride ions results in GABA's inhibitory effect leading to hyperpolarisation and stabilisation.
Similar to other benzodiazepines, clobazam binds to the interface of the α and γ2-subunit of the GABA-A receptor. However, it is considered a partial agonist to GABA-A receptors which sets clobazam apart from 1,4-benzodiazepines which are full agonist. The significance of this difference is that one may experience less sedation with clobazam than with other benzodiazepines. Unlike the endogenous GABA ligand, clobazam binds allosterically to the GABA receptor to increase the frequency of the chloride channel opening and membrane permeability to chloride ions. Pharmacodynamic tolerance has been demonstrated in animal models.
| Trade Name | Clobazam |
| Availability | Prescription only |
| Generic | Clobazam |
| Clobazam Other Names | Clobazam, Clobazamum |
| Related Drugs | Onfi, Banzel, Sympazan, gabapentin, clonazepam, lamotrigine, pregabalin, Lyrica, topiramate, Topamax |
| Weight | 10mg, 20mg, 5mg, 2.5mg/ml |
| Type | Tablet, Oral Film, Oral Suspension, Oral Tablet |
| Formula | C16H13ClN2O2 |
| Weight | Average: 300.74 Monoisotopic: 300.066555377 |
| Protein binding | Clobazam is the primary circulating entity in the serum and is highly protein-bound (80-90%). |
| Groups | Approved, Illicit |
| Therapeutic Class | Benzodiazepine hypnotics |
| Manufacturer | Essential Drugs Company Ltd, Pt Dexa Medica, Etercon Pharma, Mersifarma Tirmaku Mercusana |
| Available Country | Bangladesh, United States, Indonesia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Clobazam is used for anxiety, tension, irritability, restlessness, epilepsy and response in the treatment of fear, depressive mood, sleep disturbances.
Clobazam is also used to associated treatment for these conditions: Epilepsies
How Clobazam works
Clobazam binds at distinct binding sites associated with the chloride ionopore at the post-synaptic GABA receptor. These GABA receptors are in various locations in the CNS (limbic, reticular formation) and clobazam increases the duration of time for which the chloride ionopore is open. As a result, hyper polarization and stabilization of the membrane occur as the post-synaptic inhibitory effect of GABA is enhanced.
Dosage
Clobazam dosage
Adults: 20-30 mg daily in divided dosage or as a single dosage at bed time, may increase up to 60 mg daily in divided dosage in severe anxiety and dosage of 20 mg daily for elderly, debilitated patients.
Children: Over 3 years up to ½ of the adult dose. Clobazam is not recommended for children under 3 years of age.
Elderly: Doses of 20 mg daily may be used in the elderly patients with anxiety.
Side Effects
The most frequently observed adverse reactions, particularly during the initial phase of therapy include drowsiness, ataxia, fatigue, confusion, vertigo and these may diminish with continued therapy. Occasionally dry mouth, headache, hypersensitivity reactions and respiratory depression may occur.
Toxicity
The most common adverse effects include somnolence, pyrexia, upper respiratory tract infection, and lethargy.
Precaution
Clobazam should be administered with caution to patients with hepatic or renal disease. The ability to operate machinery or drive a car may be impaired for patients taking high doses.
Interaction
The administration of alcohol results in significantly higher serum concentrations of clobazam. The concurrent administration of hypnotic or antidepressants with sedative activity may cause an increase in side effects, particularly tiredness or drowsiness.
Food Interaction
- Avoid alcohol. Alcohol increases clobazam absorption by 50%.
- Take with or without food. The absorption is unaffected by food.
[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.
Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.
Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.
Clobazam Drug Interaction
Moderate: lorazepam, rufinamide, diphenhydramine, diazepam, cannabidiol, perampanel, levetiracetam, lamotrigine, phenytoin, quetiapine, carbamazepine, topiramate, valproic acid, sertralineUnknown: polyethylene glycol 3350, acetaminophen, acetaminophen, lacosamide, cyanocobalamin, cholecalciferol
Clobazam Disease Interaction
Major: acute alcohol intoxication, drug dependenceModerate: depression
Volume of Distribution
Vdss = 100 L. This high volume of distribution suggests extensive distribution to body tissues.
Elimination Route
After oral administration of clobazam, it is almost completely absorbed (87% of dose). Bioavailability relative to solution was almost at 100%. Food does not affect absorption. Tmax = 1-3 hours.
Half Life
The mean elimination half life of an oral dose of clobazam 40 mg is 32 hours. It's main metabolite, norclobazam, as a half life of 57 hours. The half life in adult patients with epilepsy are higher than those that are healthy.
Clearance
Median estimated clearance = 2.49 L/h
Elimination Route
Clobazam is eliminated via the urine (~94%) as metabolites.
Pregnancy & Breastfeeding use
Pregnancy: There is little information on the use of Clobazam in early pregnancy but no untoward effects have been found in animal studies. However, there are reports of a possible malformations in infants due to the administration of other benzodiazepines in early pregnancy.
Lactation: Clobazam has been detected in the breast milk of nursing mothers, but the effect on the neonate is not known.
Contraindication
Clobazam should not be used in patients known to be hypersensitive to benzodiazepines.
Acute Overdose
Symptom: Drowsiness, mental confusion, lethargy, ataxia, hypotonia, hypotension, respiratory depression, coma and very rarely death.
Management: Treatment includes emptying stomach by inducing vomiting (if within 1 hr) or gastric lavage. Activated charcoal may be used to reduce absorption. Monitor respiratory and CV functions. Flumazenil may be given if necessary. Forced diuresis or haemodialysis unlikely to be effective.
Storage Condition
Store at 15-30° C.
Innovators Monograph
You find simplified version here Clobazam
Clobazam contains Clobazam see full prescribing information from innovator Clobazam Monograph, Clobazam MSDS, Clobazam FDA label
FAQ
What is the Clobazam used for?
Clobazam is used to help control seizures that occur with Lennox-Gastaut syndrome (LGS). It works in the brain to prevent seizures. This medicine will not cure LGS and will only control seizures for as long as you continue to take it. Clobazam is a benzodiazepine.
How safe is Clobazam?
Clobazam is generally considered safe to use, with only mild side effects when compared to other AEDs. As with any benzodiazepine, there is a risk for dependence 18.
How does Clobazam work?
Clobazam increases the activity of GABA in the brain, it increases its calming effects. Clobazam is metabolized or broken down in the liver to the parent or main drug and breakdown products called metabolite. The parent or main Clobazam provides most of the activity in the brain to decrease or stop seizures.
What are the common side effects of Clobazam?
Common side effects of Clobazam may include:
- drowsiness, tiredness, trouble sleeping;
- slurred speech;
- anger, aggression;
- constipation;
- painful urination;
- fever, cough, breathing problems; or
- drooling.
Is Clobazam safe during pregnancy?
Some authorities state that use is contraindicated in the first trimester. Use is not recommended unless clearly needed in the second and third trimesters; however, other experts recommend that use is contraindicated throughout pregnancy.
Is Clobazam safe during breastfeeding?
Clobazam would not be expected to cause any adverse effects in breastfed infants, especially if the infant is >2 months.
Can I drink alcohol with Clobazam ?
Do not drink alcohol while you are on Clobazam as it will increase the likelihood that you experience this side-effect. While you are being treated for epilepsy there is a small risk that you may develop mood changes, distressing thoughts and feelings about suicide.
Does Clobazam make me sleepy?
This Clobazam may cause some people to be dizzy, drowsy.
How long does Clobazam stay in my system?
Clobazam and its main metabolite last a long time in the body. The mean half-life (or how long it takes for the body to get rid of half of the drug) for Clobazam ranges 36 to 42 hours.
Can Clobazam cause weight gain?
Weight gain has not been reported as a side effect with Clobazam.
Can Clobazam cause insomnia?
There are no currently available published reports on the effect of Clobazam on sleep.
Does Clobazam affect memory?
Clobazam did not impair memory.
When should be taken of Clobazam?
Clobazam is usually taken as a once-daily dose at bedtime, although as your dose increases you may be asked to take it divided into two smaller doses.
How do I take Clobazam?
Clobazam tablets should be swallowed whole, followed by at least a half a glass of water. They can also be split in half along the score or crushed and mixed with applesauce or another soft food. Clobazam can be taken with food or without food.
How long does Clobazam take to work?
Clobazam is absorbed quickly into the blood stream. The amount peaks or reaches its highest level within 30 minutes to 4 hours after a dose is take.
How long does Clobazam stay in my system?
The mean half-life (or how long it takes for the body to get rid of half of the drug) for Clobazam ranges 36 to 42 hours. The metabolite may last longer in the body, up to 82 hours.
Who should not take Clobazam?
You should not take Clobazam if you are allergic to it. Tell your doctor if you have ever had: breathing problems or lung disease; depression, mood problems, or suicidal thoughts or behavior; a drug or alcohol addiction; or liver or kidney disease.
What happens if I miss a dose?
Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.
What happens if I overdose?
Seek emergency medical attentio. An overdose of Clobazam can be fatal if you take it with alcohol, opioid medicine, or other drugs that cause drowsiness or slow your breathing. Overdose symptoms may include extreme drowsiness or weakness, confusion, slow breathing, or loss of consciousness.
What happen If I suddenly stop taking Clobazam?
Do NOT stop taking this Clobazam suddenly. Stopping this medicine suddenly can cause seizures that will not stop, hearing or seeing things that are not there, shaking, nervousness, or stomach and muscle cramps.
Can Clobazam affect my kidneys?
There is no significant effect of race on the clearance of Clobazam either. - Renal impairment has been evaluated and patients with severe renal impairment have not been studied extensively, but it apparently seems to be non-problematic in patients with mild or moderate renal impairment.
Can Clobazam affects my liver?
clinically apparent liver injury from Clobazam has yet to be reported and must be rare.
