What is Clonazepam and what is it used for?
The active ingredient Clonazepam refers to long-acting benzodiazepines that stimulate inhibitory signals from the nervous system. Therefore, because of its predominantly anticonvulsant action, Clonazepam is used orally or parenterally as adjunctive therapy for epilepsy.
In addition to its anxiolytic, sedative, hypnotic, and muscle relaxant effects, Clonazepam has a pronounced anticonvulsant effect. Therefore, the active ingredient is used in the following diagnoses:
- Complementary therapy for generalized epilepsy, especially in infants, children and adolescents (e.g., West syndrome, Lennox-Gasto syndrome)
- Absent epilepsy and other myoclonic syndromes when other antiepileptic drugs are inadequate or inapplicable
- Focal seizures in adults
- Insomnia
Mechanism of action of the drug
Clonazepam belongs to the group of benzodiazepines. They affect the action of the physiologically most important inhibitory mediator GABA (Ξ³-aminobutyric acid), which provides protection against excessive spontaneous activity in the nervous system.
Clonazepam binds to the allosteric benzodiazepine binding site and thus increases the affinity of the natural GABA ligand for the receptor.
Chlorine channel opening is increased, and the influx of chlorine ions into the postsynapse and hyperpolarization are enhanced, resulting in an eventual decrease in excitability. Benzodiazepines cannot increase the maximal effect of GABA and therefore have a large therapeutic range.
Absorption and half-life of Clonazepam
Clonazepam is well absorbed from the gastrointestinal tract after oral administration. Bioavailability is 71 to 76%. Tablets and oral solutions are bioequivalent in absorption, but maximum plasma concentrations are somewhat lower for tablets and are reached somewhat later, after 2-3 hours.
Clonazepam, with a half-life of 30 to 40 hours, is one of the long-acting benzodiazepines. The drug is excreted 50-70% by the kidneys and 9-30% with the feces and is reabsorbed in the intestine. Complete excretion occurs 4-10 days after oral administration of the drops.
Clonazepam drops: dosage
How to take Clonazepam drops?
The dose of Clonazepam is adjusted according to the patient's age, clinical response and tolerability. Therapy should be started cautiously with low doses that are gradually increased over two to four weeks to the required maintenance dose. Clonazepam therapy is a long-term treatment. Any removal should be done gradually.
Adults initially receive 1 mg Clonazepam per day in the form of tablets or drops; elderly or sensitive patients receive a lower dose of 0.5 mg per day.
The first dose should be divided into two doses. The dose may be increased by 0.5 to 1 mg of Clonazepam every three to five days until the desired dose is reached. On average, this is 4 to 8 mg of Clonazepam per day and should be divided into three to four separate doses.
The maximum dose of 20 mg per day should not be exceeded.
Clonazepam drops: dosage for anxiety
Clonazepam drops for anxiety are taken 0.25 mg orally every 12 hours initially. It is possible to increase the dose to 1 mg daily after three days of treatment and to 4 mg daily for patients with high tolerance.
How many drops of Clonazepam to sleep?
Clonazepam drops for sleep are usually prescribed 0.25-2.0 mg 30 minutes before sleep. The total daily dose of the drug should not exceed 4 mg per day in the treatment of insomnia.
Clonazepam drops: dosage for narcolepsy
Low doses of Clonazepam sleeping drops starting at 0.25-0.5 mg orally before bedtime are effective in the treatment of narcolepsy. The usual range of effective doses for narcolepsy is 0.5 to 1 mg per night, depending on the prescribing physician.
Clonazepam side effects
The following side effects may often occur during therapy with Clonazepam: fatigue, drowsiness, drowsiness dizziness, increased reaction time, nystagmus, ataxia, decreased muscle tone.
If any side effects occur, it is advisable to consult a doctor.
What are the Clonazepam interactions?
When using Clonazepam, there may be interactions with the following drugs:
- Rifampicin, Phenobarbital, Carbamazepine, Lamotrigine.
- Phenytoin, Primidone: increased plasma concentrations due to Clonazepam may occur.
- Valproic acid: sometimes Peitit-Mal status is possible.
- Sleeping pills, narcotics, opioids, antiepileptics, neuroleptics, antidepressants, lithium: mutually reinforcing CNS depressant effects, increased risk of sedation, respiratory depression, coma and death.
- Alcohol: mutually reinforcing effects due to joint attack on the GABA receptor.
Clonazepam: contraindications
The following contraindications should be considered when treating with Clonazepam: hypersensitivity to the active substance or other benzodiazepines; history of drug or alcohol dependence; myasthenia gravis, coma, severe respiratory failure, severe liver failure.
Clonazepam is not recommended during pregnancy and lactation. It passes through the placental barrier and into breast milk. There is a risk of malformations and mental retardation in the child after an overdose of Clonazepam during pregnancy.
Newborns have an increased risk of physical dependence, respiratory depression, hypothermia, arterial hypotension, decreased muscle tone, and poor drinking (flaccid infant syndrome).
On the other hand, pregnancy can aggravate epilepsy. Therefore, the use of Clonazepam in pregnancy is possible only if there are strong indications and at the lowest effective dose. If possible, it should not be combined with other antiepileptic drugs.
Driving ability
Even when used as prescribed, Clonazepam can seriously impair your ability to drive and operate machinery. Therefore, such activities should be avoided for the first few days or, if possible, completely. The decision will be made by your treating physician on a case-by-case basis, taking into account the dosage and individual response.
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