Clonazepam (Rivotril)

Introduction to clonazepam (Rivotril)

Clonazepam, better known in Brazil as Rivotril and in the United States as Klonopin, is a benzodiazepine that inhibits the central nervous system, acting as an anxiolytic, anticonvulsant, sedative, tranquilizer and muscle relaxant.

It is very important to remember that this medicine is a black label, that is, it is a controlled medicine that must be prescribed using a special prescription and by a doctor.

Brazil is the largest consumer of clonazepam (Rivotril) in the world, being the 2nd most sold medicine in Brazil, second only to a contraceptive distributed by the government. But is its use being correct?

The problem with using this medicine in Brazil is that people take the medicine from acquaintances and relatives without going to the doctor, buy it in pharmacies and the internet without a prescription, use the calming effect, erroneously, to get rid of the pressure of day-to-day work, without any medical follow-up. This practice usually leads to worsening of the person’s condition in the future.

This medicine is indicated in cases of seizures and some cases of emotional disorders (panic disorder, anxiety disorders, mood disorders, treatment of sleep disorders…).

The main adverse effects were drowsiness, impaired attention, and memory problems. In addition to being able to cause dependence in some cases.

Patients using this medicine should not consume alcohol.

Clonazepam interacts with opioid analgesics, barbiturates, some muscle relaxants; therefore, the concomitant use of these drugs must be monitored.

It should not be used during pregnancy or lactation, unless there is no other option, in which case breastfeeding should be discontinued.

The use of this medicine cannot be stopped abruptly, as there is a risk of withdrawal crises.

Clonazepam chemical structure

Name (IUPAC) 5-(2-Chlorophenyl)-7-nitro-2,3-di-hidro-1H-1,4-benzodiazepine-2-ona.

Molecule names: clonazepam (PT-Bra); clonazepam (ING)

Check out the clonazepam interview with psychiatrist Dr. José Carlos Ramos

Dose

Adult use

The treatment of epilepsy is chronic and only the doctor knows the ideal dose of clonazepam for your case;

– Panic Syndrome:

  Initial – recommended oral dose of 0.25 mg twice daily for 3 days, then 0.5 mg twice daily.

  Maintenance – oral dosage can be increased from 0.125 to 0.25 mg twice daily every 3 days to a maximum daily dosage of 1 to 4 mg (divided into 2 or 3 daily doses).

– Convulsions:

Initial – 0.5mg 3 times a day, oral dose.

– Maintenance: the daily oral dose can be increased from 0.5 to 1.0mg every 3 days for a maximum dosage of 20mg (divided into up to 3 daily doses).

Child use (Over 10 years or over 30 kg)

– Panic Syndrome:

There are no studies that prove its effectiveness for panic syndrome in children.

– Convulsions

Initial – 0.01 to 0.03 mg/kg/day orally divided into 2 to 3 daily doses

Maintenance – daily oral dose may be increased by 0.25 to 0.5 mg every 3 days for a total daily dose of 0.1 to 0.2 mg/kg/day (divided into up to 3 daily doses).

dose adjustment

– Discontinuation dose— decrease dose by 0.125 mg twice daily every 3 days.

– Elderly — decrease 50% of the usual dose (adult use)

– Liver disorders — decrease the usual dose by 50% (adult use)

Only the doctor knows the ideal dose of clonazepam for your case;

Indications

– panic disorder

– seizures

– anxiety disorders (such as anxiolytic in general or panic disorder with or without agoraphobia, social phobia)

– mood disorders (bipolar effective disorder, treatment of mania, major depression)

– psychotic syndromes

– restless legs syndrome

– vertigo and symptoms related to loss of balance

– treatment of sleep disorders (REM sleep disorders, sleepwalking and insomnia).

It can be used as an adjunct to antidepressants in the treatment of major depression, as well as in the treatment of epileptic seizures of various types.

Effects

Anxiolytic, sedative, muscle relaxant, traquilizer, anticonvulsant .

It is not known exactly how this drug works, it is believed that its action is related to its ability to increase GABA activity, which is the main inhibitory neurotransmitter in the central nervous system. It has the ability to suppress the wave and peak discharges of absence seizures (a type of seizure) and decreases the frequency, duration, amplitude, and spread of discharge in minor motor seizures.

The elimination of the drug is slow, as the active metabolites can remain in the blood for several days and even weeks, with persistent effects. Clonazepam has an intermediate half-life, with an average action of 18 hours in the body, from the beginning of relaxation, the peak of the effect, and the exit from the body. Its binding to proteins is high, metabolized in the liver and excreted by the kidneys.

Adverse effects

Clonazepam can cause a series of adverse effects, among the most important and most frequent are drowsiness, attention difficulties and memory problems.

Below is a list containing all possible adverse effects, it is worth remembering that many of the effects reported below rarely occur:

– Gastrointestinal: Excessive salivation

– Neurological: Abnormal eye movements, coma, respiratory depression, nystagmus, migraine, slurred speech, tremor, vertigo, loss of balance, lethargy, paresthesia, ataxia, dizziness, impaired cognition, convulsion, aggravation, drowsiness.

– Psychiatric: irritability, depression, behavior problems

– Respiratory: pulmonary congestion, respiratory depression and wheezing.

– Cardiovascular: palpitations, chest pain.

– Dermatologic: hair loss, rash, facial and ankle swelling

– Gastrointestinal: anorexia, coated tongue, constipation, diarrhea, dry mouth, gastritis, hepatomegaly, increased appetite, nausea, sore gums, abdominal discomfort or pain, gastrointestinal inflammation, toothache.

– Genitourinary: urinary retention, cystitis, urinary tract infection, dysmenorrhea.

– Musculoskeletal: muscle weakness, pain, low back pain, traumatic fracture, myalgia, nuchalgia, dislocations and tensions.

– Hematopoietic: anemia, leukopenia, thrombocytopenia, eosinophilia.

– Hepatic: temporary elevations of serum transaminases and alkaline phosphatase.

– Auditory and Vestibular Disorders: otitis, vertigo.

– Miscellaneous: dehydration, general deterioration, fever, lymphadenopathy, weight gain or loss, allergic reaction, fatigue, viral infection.

– Drug abuse and dependence.

contraindications

The use of clonazepam is contraindicated in cases of:

– acute angle-closure glaucoma

– hypersensitivity to benzodiazepines

– significant liver disease

Interactions 

Opioid analgesics, barbiturates, some muscle relaxants.

Patients undergoing treatment with clonazepam should under no circumstances consume alcohol, as it may potentiate the effect of the drug or produce undesirable and unpredictable effects.

The effect of antiepileptic drugs (hydantoins, carbamazepine,…) can become more pronounced, causing greater sedation.

Pregnancy

Pregnancy risk category: D

It can increase the risk of birth defects, particularly in the first trimester of pregnancy. However, despite the risk to the fetus, the use of this drug may be acceptable in extreme cases (life-threatening and serious illness without safer alternative treatment).

Lactation

Although clonazepam is excreted in breast milk in only small amounts, mothers undergoing treatment with this medication should not breast-feed. If there is indication for the use of the drug, breastfeeding should be discontinued.

Presentation

– 0.25 mg sub-ligual tablet

– tablets, 0.5 mg and 2 mg

– 2.5 mg/ml drops

– solution

clinical studies

Clinical studies confirmed the use and effectiveness of clonazepam in the treatment of seizures, social phobia, panic disorder. The best route of administration is oral, where the drug concentration peak is reached between 1 and 4 hours and it takes 30 to 40 hours to be eliminated (metabolization is hepatic, and renal excretion).

In cases of seizure, 30% of patients experienced loss of anticonvulsant activity within the initial three months of administration.

It has been shown that more than 1% and less than 5% of patients experience any type of adverse effect.

The drug is being successfully tested for treatments of chronic pulsatile tinnitus.

Tips

– One should not stop using clonazepam abruptly, particularly in cases of chronic use and high dose therapy, due to the potential for epilepsy.

– One should not take alcohol or valproic acid, CNS depressants, while taking clonazepam.

– Attention in cases of drug addiction history; potential abuse.*

– This medicine should be avoided by people with dangerous professions, such as machine operators or motor vehicle drivers; may interfere with motor and cognitive performance.

– Liver function and kidney function should be monitored regularly during chronic use of clonazepam.

– Attention to the increased risk of suicide attempts when used as an adjuvant in cases of depression; recommended monitoring.

– Withdrawal symptoms may occur shortly after discontinuation if not gradual.

IMPORTANT ANNOUNCEMENT

The information contained on the website www.Creates Health is for information purposes only and does not replace, under any circumstances and situation, consultation with a doctor or pharmacist.

Jeanne Kenney
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I’m a stylist trainer, a content creator, and an entrepreneur passion. Virgo sign and Pisces ascendant, I move easily between my dreams, the crazy world I want, and my feet on the ground to carry out my projects.

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