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Clonazepam information from DrugsUpdate  

See Available Brands of Clonazepam in India

P - Caution when used during pregnancy
L - Caution when used during lactation

Clonazepam is a benzodiazepine derivative with highly potent anticonvulsant, muscle relaxant, and anxiolytic properties. It is marketed by Roche under the trade-names Klonopin in the United States, and Ravotril in Chile. Other names like Rivotril or Rivatril are known throughout the large majority of the rest of the world. Clonazepam is a chlorinated derivative of nitrazepam and therefore a nitrobenzodiazepine.

Pharmacodynamics

The precise mechanism by which Clonazepam exerts its antiseizure and antipanic effects is unknown, although it is believed to be related to its ability to enhance the activity of gamma aminobutyric acid, the major inhibitory neurotransmitter in the central nervous system. Convulsions produced in rodents by pentylenetetrazol or, to a lesser extent, electrical stimulation are antagonized, as are convulsions produced by photic stimulation in susceptible baboons.


A taming effect in aggressive primates, muscle weakness and hypnosis are also produced. In humans, Clonazepam is capable of suppressing the spike and wave discharge in absence seizures (petit mal) and decreasing the frequency, amplitude, duration and spread of discharge in minor motor seizures.

Pharmacokinetics

Clonazepam is an effective anticonvulsant. It raises the threshold for propagation of seizure activity and prevents generalisation of focal or local activity. Clinically, it improves focal epilepsy and generalised seizures. It is also believed to enhance the activity of GABA, and acts as anxiolytic.


Absorption:
Well absorbed from the GI tract (oral); peak plasma concentrations after 4 hours.

Distribution:
Crosses the placenta; enters breast milk. Protein-binding: 86%.

Metabolism:
Extensively hepatic; converted to 7-aminoclonazepam.

Excretion:
Urine (as free or conjugated metabolites); 20-40 hours (elimination half-life).

Clonazepam Indications / Clonazepam Uses

Information is not available

Clonazepam Adverse Reactions / Clonazepam Side Effects

Drowsiness, fatigue, muscular hypotonia, coordination disturbances, dizziness, vertigo, anorexia, visual disturbances, libido changes.


Potentially Fatal: Salivary or bronchial hypersecretion leading to respiratory problems (children). May produce diminished reflexes or coma. Rarely, blood dyscrasias.

Precautions

General


Worsening of Seizures
When used in patients in whom several different types of seizure disorders coexist, Clonazepam may increase the incidence or precipitate the onset of generalized tonic-clonic seizures (grand mal). This may require the addition of appropriate anticonvulsants or an increase in their dosages. The concomitant use of valproic acid and Clonazepam may produce absence status.


Laboratory Testing During Long-Term Therapy Periodic blood counts and liver function tests are advisable during long-term therapy with Clonazepam.


Risks of Abrupt Withdrawal
The abrupt withdrawal of Clonazepam, particularly in those patients on long-term, high-dose therapy, may precipitate status epilepticus. Therefore, when discontinuing Clonazepam, gradual withdrawal is essential. While Clonazepam is being gradually withdrawn, the simultaneous substitution of another anticonvulsant may be indicated.


Caution in Renally Impaired Patients
Metabolites of Clonazepam are excreted by the kidneys; to avoid their excess accumulation, caution should be exercised in the administration of the drug to patients with impaired renal function.


Hypersalivation
Clonazepam may produce an increase in salivation. This should be considered before giving the drug to patients who have difficulty handling secretions. Because of this and the possibility of respiratory depression, Clonazepam should be used with caution in patients with chronic respiratory diseases.

Special Precautions

Neonates, chronic pulmonary insufficiency, hepatic/renal dysfunction, porphyria, elderly; pregnancy and lactation.

Other Drug Interactions

Carbamazepine, phenobarbitone or phenytoin may accelerate clonazepam metabolism.


Potentially Fatal: Increased sedative effect with alcohol, general anaesthetics and TCAs.

Other Interactions

Information Not Available

Dosage

Oral
Epilepsy
Adult: Initially, 1 mg given at night for 4 nights, gradually increased over 2-4 weeks. Maintenance: 4-8 mg daily. Max: 20 mg/day
Child: 1-5 years: 250 mcg daily; 5-12 years: 500 mcg daily. Maintenance (given in 2-4 divided doses):
Infants: 0.5-1 mg daily; 1-5 years: 1-3 mg daily; 5-12 years: 3-6 mg daily. Max: 200 mcg/kg/day
Elderly: Initially, 500 mcg at night for 4 nights, may gradually increase over 2-4 weeks.

Hepatic impairment: Dose reduction may be needed.

Oral
Panic disorder
Adult: Initially, 250 mcg bid, increased after 3 days up to 1 mg daily. Max: 4 mg daily.


Hepatic impairment: Dose reduction may be needed.

Intravenous
Emergency management of status epilepticus
Adult: 1 mg as injection or infusion given over at least 2 minutes, repeated if necessary.
Child: and infants: 500 mcg as injection or infusion given over at least 2 minutes, repeated if necessary.


Hepatic impairment: Dose reduction may be needed.

Food(before/after)

May be taken with or without food

List of Contraindications

Clonazepam and Pregnancy

Caution when used during pregnancy.


Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Clonazepam and Lactation

Caution when used during lactation

Clonazepam and Children

Panic disorder
Safety and efficacy not established.

Seizure disorders
Initial dose should be small and gradually increased. Long-term use may cause adverse effects such as possibly delayed mental or physical development.

Clonazepam and Geriatic

Initial dose should be small and gradually increased. Give drug with extreme care to elderly or very ill patients with limited respiratory reserve.

Clonazepam and Other Contraindications

Hypersensitivity to benzodiazepines, acute pulmonary insufficiency, acute narrow angle glaucoma.

Storage

Intravenous
Store at 25°C.


Oral
Store at 25°C.

Lab interference

Intravenous
Store at 25°C.


Oral
Store at 25°C.

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