Definition
An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses.
Description
An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of gamma-aminobutyric acid receptor responses. [PubChem]
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Hepatic (cytochrome P450, including CYP3A). Biotransformation occurs mainly by reduction of the 7-nitro group to the 4-amino derivative. This derivative can be acetylated, hydroxylated, and glucuronidated. Route of Elimination: Clonazepam is highly metabolized, with less than 2% unchanged clonazepam being excreted in the urine. Metabolites of Klonopin are excreted by the kidneys. Clonazepam also undergoes acetylation via NAT2. Half Life: 30-40 hours
- Uses/Sources: Clonazepam is used as an anticonvulsant in the treatment of the Lennox-Gastaut syndrome (petit mal variant), akinetic and myoclonic seizures. It can also be used for the treatment of panic disorders.
- Health Effects: May cause a potentially dangerous rash that may develop into Stevens Johnson syndrome, an extremely rare but potentially fatal skin disease.
- Symptoms: Somnolence, confusion, coma, and diminished reflexes. The most commonly reported adverse event when clonazepam is used for seizure disorders is CNS depression.
- Treatment: Treatment includes monitoring of respiration, pulse and blood pressure, general supportive measures and immediate gastric lavage. Intravenous fluids should be administered and an adequate airway maintained. Hypotension may be combated by the use of levarterenol or metaraminol. Flumazenil, a specific benzodiazepine-receptor antagonist, is indicated for the complete or partial reversal of the sedative effects of benzodiazepines and may be used in situations when an overdose with a benzodiazepine is known or suspected. (L1712)
- Route of Exposure: Clonazepam is rapidly and completely absorbed after oral administration. The absolute bioavailability of clonazepam is about 90%. Cmax, oral administration = 1 -4 hours.
Toxicity
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: LD50, oral, rats = >15000 mg/kg.
Mechanism of Action
Clonazepam Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Barrett's esophagus | 7.97 |
|
Mesothelioma, Malignant | 7.75 |
|
Esophageal Neoplasms | 7.33 |
|
Intestinal Neoplasms | 5.99 |
|
Chronic obstructive pulmonary disease | 5.76 |
|
Adenocarcinoma | 5.35 |
|
Multiple myeloma | 4.96 |
|
Lymphoma, Non-Hodgkin | 4.93 |
|
Eye Infections, Bacterial | 4.81 |
|
Intracerebral hemorrhage | 4.77 |
|
Male infertility | 4.72 |
|
AIDS-related Kaposi sarcoma | 4.67 | |
Jaundice, Neonatal | 4.66 |
|
Prostatic Neoplasms | 4.46 |
|
Polycystic ovary syndrome | 4.43 |
|
Pancreatic carcinoma | 4.41 |
|
Adenocarcinoma, Clear Cell | 4.32 |
|
Alzheimer's Disease | 4.24 |
|
Chondrosarcoma, Mesenchymal | 4.21 |
|
Pulmonary Emphysema | 4.21 |
|