Clonazepam (Rivotril): Indications and Side Effects

Clonazepam belongs to the benzodiazepine group and can cause addiction if not used properly. Its best-known trade name is Rivotril®.

Written and verified by el médico Diego Pereira.

Last update: 20 March, 2023

Clonazepam or Rivotril ® is a drug belonging to the group of benzodiazepines. It’s usually recommended for the treatment of epileptic syndromes and panic or anxiety disorders, and gives good results.

Its effects include decreased anxiety, relaxation, and even sedation. This implies that many people consume it chronically or for recreational reasons. The abusive use of benzodiazepines is considered a public health problem in many countries.

If you have questions about this medication, we have prepared the following article to answer the most frequently asked questions. Keep reading!

What is clonazepam?

It’s a drug that’s used widely throughout the world with direct effects on the central nervous system. It’s part of the benzodiazepines group, which also includes alprazolam, diazepam and lorazepam, among others.

In the mid-20th century, different laboratories of large pharmaceutical companies began to develop drugs with the aim of gradually displacing barbiturates. These were used for their sedative and anti-anxiety effects, but overdoses became a growing problem.

Benzodiazepines were the result of this set of investigations. In the specific case of clonazepam, it was patented in 1964 by the Hoffmann-La Roche company, and by 1975 it was possible to market it under the name Klonopin ® in the United States.

Due to the possibility of addiction and side effects in case of abusive use, it’s a prescription drug in most countries. It has a long half-life, at least compared to other benzodiazepines such as alprazolam. This means that, after consumption, it can remain in the body for up to 24 hours.

Depending on the type of patient and the condition, Rivotril ® is available in ampoules for intravenous administration and as tablets and drops for the oral route.

Clonazepam mechanism of action

Clonazepam is related to the effects of a very important neurotransmitter for humans: γ-aminobutyric acid or GABA. It’s the main inhibitory substance of the central nervous system.

In neurons, the term inhibition is used to refer to electrical changes capable of inducing a particular response in the brain. Of course, there are opposite changes that are the result of stimulation by other neurotransmitters.

For these changes to occur, neurotransmitters must interact with molecules known as receptors. These are located on the surface of neurons. So, to communicate, one neuron is responsible for releasing neurotransmitters, while another receives them through receptors. This process is called a chemical synapse.

When Rivotril ® reaches the nervous system, it interacts with GABA receptors in many neurons, stimulating them. That is, it acts as a simulant of γ-aminobutyric acid.

This mechanism is more or less the same in all benzodiazepines, which is why the following effects are achieved:

• Anxiolytic: This helps to reduce anxiety and all associated symptoms.
• Hypnotic or sedative: It facilitates sleep.
• Anticonvulsant: Seizures are characterized by electrical discharges in the brain.
• Muscle relaxant: Despite this effect, it’s rarely recommended for this purpose because there are more effective substances.

Clonazepam indications

Despite its effectiveness, clonazepam is generally not used as first-line therapy for many medical conditions. This is due to several reasons:

• The likelihood of developing dependence with prolonged use.
• The fact that there are more effective drugs for the control of seizures or anxiety disorders in the long term.

However, doctors may indicate Rivotril ® as part of combination therapy (i.e. accompanied by other drugs that enhance its effect). Or also as a short-term treatment in specific situations.

Epileptic seizures

It can be prescribed as a treatment for any type of epileptic disorder in adults. This includes generalized tonic-clonic seizures, partial events, absence seizures, and myoclonic disorders. In children, sources report that it can also be useful for epilepsy.

Certain factors can trigger seizures. Flashes of light, fever, the use of illicit drugs, excessive intake of alcoholic beverages, and, of course, non-compliance with antiepileptic treatment are some of the triggers.

This last aspect also involves Rivotril ®. If a patient is constantly taking a drug that alters the levels of neurotransmitters in the central nervous system, they are in danger of suffering seizures in the event of abrupt withdrawal.

The benzodiazepine withdrawal syndrome can result in the appearance of seizures, as well as episodes of anxiety and insomnia. For this reason, doctors recommend a progressive withdrawal of these drugs when it’s necessary to change them or end the treatment.

Panic and anxiety attacks

Both are related disorders, despite the fact that they have different clinical and therapeutic characteristics. Panic attacks make up one of the pathologies in which Rivotril ® is most recommended, which makes it possible to reduce the frequency of attacks and also their intensity.

It can affect around 1% of the world population with varying degrees of severity. It’s influenced by environmental and genetic factors. Women are more susceptible to both conditions and when they occur from an early age they tend to be more intense.

According to various studies, panic disorders appear in three phases:

1. At first, they are sporadic and mild crises that often have clear triggers.
2. The patient begins to develop a generalized anxiety disorder, with all the clinical elements that characterize it: avoidance behavior, tachycardia, profuse sweating, tremors, and weakness.
3. Lastly, some may develop agoraphobia.

In this last situation, the affected people tend to develop a very irrational and involuntary fear of specific situations that could potentially become an intense panic attack. It tends to greatly limit the quality of life, especially as far as social interactions are concerned.

Warnings and caution

Adverse effects of clonazepam or Rivotril ® may be the following:

• Miscellaneous gastrointestinal disorders: Nausea, vomiting, or diarrhea.
• Tiredness, drowsiness, or muscle weakness.
• Difficulty achieving concentration.
• Respiratory depression and frequent falls: especially in the elderly.

For this last reason, elderly people should be careful with the use of benzodiazepines. According to a 2015 study (in Spanish) in which 29 cases were evaluated, it was concluded that its consumption increases the risk of hip fracture in the elderly.

In turn, patients with hepatic or renal insufficiency may require a dose adjustment due to the probability of experiencing adverse effects or toxicity more easily. It’s also contraindicated if there’s a history of drug dependence or addiction.

Myasthenis gravis is a neuromuscular condition characterized by progressive loss of muscle strength. The administration of clonazepam is contraindicated in these patients, since it can worsen the symptoms.

Clonazepam interactions

Many drugs, especially those that act on the central nervous system, can interact with clonazepam. This causes a series of consequences, such as decreased effectiveness or increased risk of developing adverse effects.

Some of the drugs capable of interacting with Rivotril ® are the following:

• Phenytoin
• Carbamazepine
• Phenobarbital
• Valproic acid

Can it be administered during pregnancy and lactation?

The use of benzodiazepines in pregnancy is controversial. In principle, according to a recent review article, the risk is small when compared with other teratogenic drugs (that is, those capable of causing fetal malformations). Some conditions such as oral clefts could increase their incidence.

In fact, it’s more harmful in the last trimester, since cases of hypotonia, hypothermia, and irritability in the newborn have been reported. If a doctor decides to prescribe clonazepam during pregnancy, it must be done under strict medical instructions.

Because this drug can be released into breast milk, breastfeeding is not recommended during treatment with clonazepam.

Clonazepam, only by prescription

Clonazepam is a drug with excellent benefits, despite the fact that it should only be used in specific cases and for a short period of time. A prescription is required for its acquisition and the most appropriate specialists for its indication are psychiatrists and neurologists.