A benzodiazepine used as an anticonvulsant for epilepsy and as a sedative for sleep disorders.
[C(H)LO(RO)– + (PHE)N(YL) + (DI)AZEPAM.]
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Results for clonazepam
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A benzodiazepine used as an anticonvulsant for epilepsy and as a sedative for sleep disorders.
[C(H)LO(RO)– + (PHE)N(YL) + (DI)AZEPAM.]
trade names: Klonopin, Rivotril; drug class: anti-convulsant, benzodiazepine derivative, controlled substance schedule IV; action: inhibits spike-wave formation; uses: akinetic myoclonic seizures.
Brand names: Ceberclon, Klonopin®
Chemical formula:

Clonazepam tablets
What are clonazepam tablets?
CLONAZEPAM (Klonopin®) is a benzodiazepine. Benzodiazepines belong to a group of medicines that slow down the central nervous system. Clonazepam is effective in treating certain types of seizures (convulsions) and is also used for a mental health condition called Panic Disorder. Federal law prohibits the transfer of clonazepam to any person other than the patient for whom it was prescribed. Do not share this medicine with anyone else. Generic clonazepam tablets are available.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
an alcohol or drug abuse problem
bipolar disorder, depression, psychosis or other mental health condition
glaucoma
kidney disease
liver disease
lung disease, such as chronic obstructive pulmonary disease (COPD), sleep apnea or other breathing difficulties
myasthenia gravis
Parkinson's disease
seizures or a history of seizures
shortness of breath
snoring
suicidal thoughts
an unusual or allergic reaction to clonazepam, other benzodiazepines, foods, dyes, or preservatives
pregnant or trying to get pregnant
breast-feeding
How should I take this medicine?
Take clonazepam tablets by mouth. Follow the directions on the prescription label. Swallow the tablets with a drink of water. If clonazepam upsets your stomach, take it with food or milk. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking or change the dose except on your prescriber's advice.
Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.
What if I miss a dose?
If you miss a dose and remember within an hour, take it as soon as you can. If it is more than an hour since you missed a dose, skip that dose and go back to your regular schedule. Do not take double or extra doses.What drug(s) may interact with clonazepam?
alcohol
bosentan
caffeine
cimetidine
disulfiram
female hormones, including contraceptive or birth control pills
herbal or dietary supplements such as kava kava, melatonin, St. John's Wort or valerian
imatinib, STI-571
isoniazid
medicines for anxiety or sleeping problems, such as alprazolam, diazepam, lorazepam or triazolam
medicines for depression, mental problems or psychiatric disturbances
medicines for fungal infections (fluconazole, itraconazole, ketoconazole, voriconazole)
medicines for HIV infection or AIDS
nicardipine
prescription pain medicines
probenecid
rifampin, rifapentine, or rifabutin
sevelamer
some antibiotics (clarithromycin, erythromycin, troleandomycin)
some medicines for colds, hay fever or other allergies
some medicines for high blood pressure or heart-rhythm problems (amiodarone, diltiazem, verapamil)
some medicines for seizures (carbamazepine, phenobarbital, phenytoin, primidone)
theophylline
zafirlukast
zileuton
Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.
What should I watch for while taking clonazepam?
Visit your prescriber or health care professional for regular checks on your progress. Your body may become dependent on clonazepam. If you have been taking clonazepam regularly for some time, do not suddenly stop taking it. You must gradually reduce the dose or you may get severe side effects. Ask your prescriber or health care professional for advice before increasing or decreasing the dose. Even after you stop taking clonazepam it can still affect your body for several days.
If you suffer from several types of seizures, clonazepam may increase the chance of grand mal seizures (epilepsy). Let your prescriber or health care professional know, he or she may want to prescribe an additional medicine.
You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how clonazepam affects you. To reduce the risk of dizzy and fainting spells, do not stand or sit up quickly, especially if you are an older patient. Alcohol may increase dizziness and drowsiness. Avoid alcoholic drinks.
If you are a female patient with a newborn, it is not recommended that you breast-feed your infant while receiving clonazepam. Ask your health care professional for additional advice.
Do not treat yourself for coughs, colds or allergies without asking your prescriber or health care professional for advice. Some ingredients can increase possible side effects.
If you are going to have surgery, tell your prescriber or health care professional that you are taking clonazepam.
What side effects may I notice from taking clonazepam?
Side effects that you should report to your prescriber or health care professional as soon as possible:
confusion
depression
double vision or abnormal eye movements
hallucinations (seeing and hearing things that are not really there)
lightheadedness or fainting spells
mood changes, excitability or aggressive behavior
movement difficulty, staggering or jerky movements
muscle cramps
restlessness
tremors
weakness or tiredness
Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
constipation or diarrhea
difficulty sleeping, nightmares
dizziness, drowsiness, clumsiness, or unsteadiness; a 'hangover' effect
headache
increased secretions or saliva from your mouth
nausea, vomiting
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.
Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Protect from light. Keep container tightly closed. Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
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Clonazepam
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| Systematic (IUPAC) name | |
| 6-(2-chlorophenyl)-9-nitro- 2,5-diazabicyclo[5.4.0]undeca- 5,8,10,12-tetraen-3-one |
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| Identifiers | |
| CAS number | |
| ATC code | N03 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C15H10ClN3O3 |
| Mol. mass | 315.715 |
| Pharmacokinetic data | |
| Bioavailability | 90% |
| Metabolism | Hepatic CYP3A4 |
| Half life | 18–50 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status | |
| Routes | Oral, I.M., I.V, sublingual |
Clonazepam (marketed by Roche under the trade-names Klonopin in the United States and Rivotril in Europe, South America, Canada, India, and Australia) is a drug which is a benzodiazepine derivative. It is a highly potent anticonvulsant, amnestic, anxiolytic and muscle relaxant. Clonazepam is also used in cases of amphetamine overdose as to reverse some of the adverse effects.
Clonazepam is a chlorinated derivative of nitrazepam.[1] Clonazepam is classed as a nitrobenzodiazepine along with nitrazepam and flunitrazepam.[2] Aromatic nitro-containing compounds such as clonazepam produce superoxide free radicals during cellular metabolism by endothelial cells. The nitro anion radical produced during clonazepam metabolism rapidly reacts with oxygen to form the free radical superoxide.[3][4]
Clonazepam is chemically related to quinazolines and is a hapten.[5] Like other benzodiazepines, clonazepam acts on benzodiazepine receptors which enhance the binding of GABA to the GABAA receptor which results in inhibitory effects on the central nervous system.[6] Because of its powerful anxiolytic properties, it is said to be among the class of "highly potent" benzodiazepines. Although benzodiazepines are valuable in the treatment of anxiety disorders, they carry a high potential for physical and psychological dependence with profound withdrawal symptoms, especially if discontinued abruptly or overrapidly in certain individuals. Caution is advised when taking this or any benzodiazepine medication longer than a few weeks.
One milligram of clonazepam is approximately equivalent to twenty milligrams of diazepam.[7]
Clonazepam appears to also have a secondary effect on the neurotransmitter serotonin.[8] It has shown itself to be highly effective as a short-term (3 weeks) adjunct to SSRI treatment in obsessive-compulsive disorder and clinical depression in reducing SSRI side effects with the combination being superior to SSRI treatment alone in a study funded by the manufacturers of clonazepam, Hoffman LaRoche Inc.[9] Similar results have been found with some other anxiety disorders, but the role of the serotonergic effects enhancing the action of the SSRI treatment remains unclear in these cases due to clonazepam's primary anxiolytic mechanism of action.
The anticonvulsant properties of clonazepam and other benzodiazepines may be in part or entirely due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors. Sustained repetitive firing seems to be limited by benzodiazepines effect of slowing recovery of sodium channels from inactivation.[10]
Peak blood concentrations of 6.5–13.5 ng/mL were usually reached within 1–2 hours following a single 2 mg oral dose of micronized clonazepam in healthy adults. In some individuals, however, peak blood concentrations were reached at 4–8 hours.[11]
Clonazepam is sometimes used for refractory epilepsies; however, long-term prophylactic treatment of epilepsy has considerable limitations, most notably the loss of antiepileptic effects due to tolerance, which renders the drug useless with long-term use, and also side effects such as sedation, which is why clonazepam and benzodiazepines as a class should generally only be prescribed for the acute management of epilepsies.[12] Clonazepam is less effective and potent as an anticonvulsant in bringing infantile seizures under control compared with nitrazepam in the treatment of West syndrome, which is an age-dependent epilepsy affecting the very young. However, as with other epilepies treated with benzodiazepines, long-term therapy becomes ineffective with prolonged therapy, and the side effects of hypotonia and drowsiness are troublesome with clonazepam therapy; other antiepileptic agents are therefore recommended for long-term therapy, possibly Corticotropin (ACTH) or vigabatrin. Clonazepam is therefore not recommended for widespread use in the management of seizures related to West syndrome.[13] Also with long-term use, abrupt or overrapid withdrawal from clonazepam can precipitate withdrawal-related seizures if tolerance and physical dependence have developed.
Clonazepam has been used in the management of seizure disorders in children and also for infantile spasms. However, usefulness of clonazepam is limited due to its deleterious effect on neurological function, especially its negative effect on cognition. Clobazam, a 1,5-benzodiazepine, has shown to be less neurotoxic than 1,4-benzodiazepines such as clonazepam.[14][15]
Clonazepam may be prescribed for:
Clonazepam is rarely used as a treatment for insomnia due to its relatively weak hypnotic effects. It has not been marketed for the treatment of insomnia mainly because its long half life makes it unsuitable for this application.
Clonazepam was approved in the United States as a generic drug in 1997 and is now manufactured and marketed by several companies.
Clonazepam is available in the U.S. as tablets (0.5, 1.0, and 2 mg), orally disintegrating tablets (wafers) (0.125, 0.25, 0.5, 1.0, and 2 mg), liquid solutions (2.5 mg/mL) and for injection (1 mg/mL)
Like all benzodiazepines, clonazepam is a benzodiazepine receptor agonist. Long-term use (more than 2–4 weeks) can lead to a number of problems, including muscle weakness and fatigue, tolerance, physical dependence and withdrawal syndromes upon discontinuation. The benzodiazepine withdrawal syndrome, which may appear during reduction or withdrawal of clonazepam treatment, can be reduced in intensity with gradual reduction of dosage. Clonazepam is sometimes used to help with Methadone withdrawal symptoms
Common:
Rare:
Withdrawal-related:
Many individuals treated on a long-term basis develop a form of dependence known as "low-dose dependence", as was shown in one
double-blind, placebo-controlled study of 34 therapeutic low-dose benzodiazepine
users—physiological dependence was demonstrated via flumazenil-precipitated withdrawal.[19] Use of alcohol or other CNS depressants while
taking clonazepam greatly intensifies the effects (and side effects) of the drug. Side effects of the drug itself are generally
benign, but sudden withdrawal after long-term use can cause severe, even fatal, symptoms.
Caution in the Elderly. Increased risk of impairments, falls and drug accumulation.[citation needed]
Caution in children. Clonazepam is not recommended for use in those under 18. Use in very young children may be especially hazardous. Clonazepam was implicated along with the drugs diphenylhydantoin and nitrazepam in the death of a 7 and a half month old girl. She developed inclusions consisting of lamellar profiles, situated in membrane-bound cytosomes which were found mainly in astrocytes, but also in neurones and in axons of peripheral nerves before dying. Lipofuscin bodies were also found to be increased in number.[20]
10–15% of individuals treated with clonazepam on a long-term basis (in excess of 30 days of continuous use) develop a protracted withdrawal syndrome. Protracted withdrawal lasts for months, years, or a lifetime after clonazepam is discontinued. Protracted withdrawal results from structural brain damage, which is often irreversible.[21] Common protracted withdrawal symptoms include:[22]
Benzodiazepines including clonazepam may inhibit the glucuronidation of morphine leading to increased levels of and prolongation of the effects of morphine. Clonazepam may inhibit morphine metabolism more than any other benzodiazepine.[23]
There is some medical evidence of various malformations eg cardiac or facial deformations when used in early pregnancy, however the data is not conclusive. The data is also inconclusive whether benzodiazepines such as clonazepam cause developmental deficits or decreases in IQ when taken during pregnancy. Clonazepam when used late in pregnancy may result in the development of a severe benzodiazepine withdrawal syndrome in the neonate and also floppy infant syndrome. Withdrawal symptoms from benzodiazepines in the neonate may include hypotonia, and reluctance to suck, to apnoeic spells, cyanosis, and impaired metabolic responses to cold stress. These symptoms may persist for hours or months after birth.[24]
An individual who has consumed too much clonazepam will display one or more of the following symptoms:
Unless combined with other drugs, deep coma or other manifestations of severe central nervous system depression are rare, and the mortality rate associated with poisoning is very low. As with other benzodiazepines, overdose symptoms of clonazepam may be reversed with flumazenil (Romazicon®).
Relatively few cases of addiction arise from legitimate use of benzodiazepines.[25] If in tablet form, they are most commonly used as a secondary drug to increase the pleasure resulting from a primary drug, or to lessen or prevent some of the primary drug's negative side effects. Clonazepam has been implicated in drug facilitated sexual assaults.[26]
| Benzodiazepines (N05BA, N05CD) |
|---|
| Adinazolam • Alprazolam • Arfendazam • Avizafone • Bentazepam • Bretazenil • Bromazepam • Brotizolam • Camazepam • Chlordiazepoxide • Cinolazepam • Clobazam • Clonazepam • Clorazepate • Clotiazepam • Cloxazolam • Cyprazepam • Delorazepam • Diazepam • Doxefazepam • Estazolam • Ethyl loflazepate • Etizolam • Fletazepam • Fludiazepam • Flumazenil • Fosazepam • Flunitrazepam • Flurazepam • Flutazolam • Flutoprazepam • Gidazepam • Halazepam • Haloxazolam • Iclazepam • Imidazenil • Ketazolam • Lofendazam • Loprazolam • Lorazepam • Lormetazepam • Medazepam • Metaclazepam • Mexazolam • Midazolam • Nimetazepam • Nitrazepam • Nordazepam • Oxazepam • Oxazolam • Phenazepam • Pinazepam • Pivoxazepam • Prazepam • Quazepam • QH-II-66 • Reclazepam • Rilmazafone • Ro15-4513 • Temazepam • Tetrazepam • Tofisopam • Triazolam • Zapizolam • Zolazepam |
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