Nelurolen
Nelurolen Uses, Dosage, Side Effects, Food Interaction and all others data.
Nelurolen is a benzodiazepine with a pronounced sleep-inducing activity. It depresses the reticular-activating system in the brainstem by enhancing the inhibitory effect of GABA on brain cells, thus preventing excessive brain activity.
Nelurolen is a type of benzodiazepine drug. It is a powerful hypnotic drug which possesses strong sedative, anxiolytic, amnestic, anticonvulsant, and skeletal muscle relaxant properties. Nelurolen shortens the time required to fall asleep and lengthens the duration of sleep. It is also useful for the management of myoclonic seizures.
| Trade Name | Nelurolen |
| Generic | Nitrazepam |
| Nitrazepam Other Names | N-desmethylnimetazepam, Nitrazepam, Nitrazépam, Nitrazepamum |
| Type | |
| Formula | C15H11N3O3 |
| Weight | Average: 281.2661 Monoisotopic: 281.080041233 |
| Groups | Approved |
| Therapeutic Class | Benzodiazepine hypnotics |
| Manufacturer | |
| Available Country | Japan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Short-term management of insomnia, Infantile spasms
Nelurolen is also used to associated treatment for these conditions: Insomnia, Myoclonic seizures
How Nelurolen works
Nelurolen belongs to a group of medicines called benzodiazepines. This drug affects central benzodiazepine receptors, which are associated with inhibitory GABA (gamma amino butyric acid)receptors, leading to enhanced GABA binding activity. GABA is a major neurotransmitter in the brain, which causes somnolence, relaxation of muscles, a decrease in anxiety and general central nervous system depression. Nelurolen has anticonvulsant properties that may be attributed to its ability to bind to voltage-dependent sodium channels. Sustained repetitive firing seems to be limited by benzodiazepines effect of slowing recovery of sodium channels from inactivation.
Dosage
Nelurolen dosage
Short-term management of insomnia:
- Adult: 5 mg at night; increase to 10 mg if necessary.
- Elderly: and debilitated patients: ≤normal adult dose.
Infantile spasms:
- Child: Infants: 125 mcg/kg bid; gradually increase to 250-500 mcg/kg bid.
May be taken with or without food
Side Effects
Hypotension, palpitation; agitation, aggressiveness, amnesia, ataxia, confusion, delusions, disorientation, dizziness, fatigue, hallucination, hangover, headache, irritability, nightmares, psychoses, rage, restlessness, sedation; rash; changes in libido; constipation, diarrhoea, excessive salivation, heartburn, nausea, vomiting; granulocytopenia, leukopenia; falling, muscle weakness; blurred or double vision; tinnitus (associated with withdrawal); aspiration, increased bronchial secretion, dyspnoea.
Toxicity
An overdose of nitrazepam may lead to impaired breathing, dizziness, decreased cognition and balance, bluish nails and lips, slurred speech, and extreme somnolence, among others. In severe overdose, these symptoms may progress to a coma with a possibility of death.
Precaution
May induce anterograde amnesia; caution patients to have uninterrupted sleep of 7-8 hr after ingestion of dose. May impair ability to drive or operate machinery. Depression, especially if suicidal risk may be present. History of drug abuse or acute alcoholism. Hepatic and renal impairment. Respiratory disease. Debilitated patients. Patients who are at risk of falls. Children, elderly. Pregnancy and lactation.
Interaction
CNS depressant effect increased with alcohol, barbiturates, TCAs, phenothiazines, morphine derivatives. Effects may be antagonised by theophylline. Increased levels/effects with probenecid. Reduced levels/effects with rifampicin. May reduce effects of levodopa.
Food Interaction
- Avoid alcohol.
- Limit caffeine intake.
- Take with food.
Elimination Route
Bioavailability is 53-94% following oral administration.
Half Life
15-38 hours (mean elimination half life 26 hours).
Pregnancy & Breastfeeding use
Category not classified
Contraindication
Myasthenia gravis, narrow-angle glaucoma, severe respiratory insufficiency, sleep apnoea syndrome, severe hepatic impairment, porphyria.
Acute Overdose
Symptoms: Somnolence, drowsiness, confusion, ataxia, impaired reflexes, coma, dyspnoea, hypotension, respiratory and cardiovascular depression.
Management: Supportive. Gastric lavage may be beneficial if performed soon after ingestion. Flumazenil may reverse benzodiazepine-induced CNS depression.
Storage Condition
Store at room temperature. Protect from light and moisture.
Innovators Monograph
You find simplified version here Nelurolen
FAQ
What is Nelurolen used for?
Nelurolen is a hypnotic drug of the benzodiazepine class used for short-term relief from severe, disabling anxiety and insomnia. It also has sedative properties, as well as amnestic, anticonvulsant, and skeletal muscle relaxant effects.
How safe is Nelurolen?
A double-blind trial in patients in general medical wards established that Nelurolen was as effective as butobarbitone as a hypnotic. It is concluded that Nelurolen is a safe and effective hypnotic.
How does Nelurolen work?
Nelurolen works by affecting the way certain brain chemicals (neurotransmitters) transmit messages. This has a calming effect which helps you to sleep. It works well in the short term, with one week's treatment normally being sufficient, although up to three weeks of treatment are sometimes required.
What are the common side effects of Nelurolen?
Common side effects include drowsiness during the day, numbed emotions, reduced alertness, confusion, fatigue, headache, dizziness, muscle weakness, ataxia and double vision.
Is Nelurolen safe during pregnancy?
Nelurolen is not recommended during pregnancy as it is associated with causing a neonatal withdrawal syndrome and is not generally recommended in alcohol- or drug-dependent individuals or people with comorbid psychiatric disorders.
Is Nelurolen safe during breastfeeding?
Your baby may develop dependency to this medicine and may be at risk of developing withdrawal symptoms. Nelurolen passes into breast-milk; therefore, do not breast-feed if you are taking this medicine.
Can I take Nelurolen with alcohol?
Do not drink alcohol while you are taking Nelurolen tablets. Alcohol will increase the sedative effect of this medicine and can be dangerous.
Can I drive after taking Nelurolen?
The effects of Nelurolen can last into the following day; it is likely to impair your reactions and your ability to drive. Do not drive and do not use tools or machines while affected.
How does I take Nelurolen?
Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it.
Can I take Nelurolen on an empty stomach?
Nelurolen 10mg tablet may be taken with or without food, but it is better to take it at a fixed time.
How much Nelurolen should I take to sleep?
The recommended adult dose of Nelurolen when taken for insomnia is 5 mg to 10 mg taken at bedtime. Seniors may be more likely to experience unwanted effects of this medication and should start with 2.5 mg taken at bedtime.
How long does Nelurolen take to work?
Nelurolen acts in 30 to 60 minutes to produce sleep lasting six to eight hours. Nelurolen is well absorbed with peak blood levels being achieved within two hours after administration.
How long does Nelurolen stay in my system?
The half-life of Nelurolen is on average 24 hours. Steady-state levels are achieved within five days. Nelurolen undergoes biotransformation to a number of metabolites none of which possesses significant clinical activity.
Can I take Nelurolen for a long time?
Nelurolen tablets can only be used for short-term insomnia treatment when it is serious, disabling, or causing intense pain, and when daytime sedation is appropriate. Treatment should be as brief as possible, with the lowest effective dose being used to begin.
How long can I take Nelurolen?
Generally the duration of treatment varies from a few days to two weeks, with a maximum of four weeks; including the tapering off process.
Who should not take Nelurolen?
Children below the age of 12 years: Do not use. Elderly and debilitated patients: 2.5 – 5 mg before retiring, doses should not exceed half those normally recommended for adults. In patients with chronic pulmonary insufficiency, and in patients with chronic renal or hepatic disease, dosage may need to be reduced.
Can Nelurolen make me depressed?
Nelurolen may causes Depression.
Can Nelurolen affect my kidneys?
If you have reduced kidney function or kidney disease, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
Can Nelurolen affects my liver?
People with reduced liver function or liver disease may experience a stronger effect from the medication than would normally occur. If you have reduced liver function or liver disease, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
