Nitrapan

Nitrapan Uses, Dosage, Side Effects, Food Interaction and all others data.

Nitrapan 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.

Nitrapan is a type of benzodiazepine drug. It is a powerful hypnotic drug which possesses strong sedative, anxiolytic, amnestic, anticonvulsant, and skeletal muscle relaxant properties. Nitrapan 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 Nitrapan
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 Brazil
Last Updated: September 19, 2023 at 7:00 am
Nitrapan
Nitrapan

Uses

Short-term management of insomnia, Infantile spasms

Nitrapan is also used to associated treatment for these conditions: Insomnia, Myoclonic seizures

How Nitrapan works

Nitrapan 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. Nitrapan 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

Nitrapan 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 Nitrapan

FAQ

What is Nitrapan used for?

Nitrapan 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 Nitrapan?

A double-blind trial in patients in general medical wards established that Nitrapan was as effective as butobarbitone as a hypnotic. It is concluded that Nitrapan is a safe and effective hypnotic.

How does Nitrapan work?

Nitrapan 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 Nitrapan?

Common side effects include drowsiness during the day, numbed emotions, reduced alertness, confusion, fatigue, headache, dizziness, muscle weakness, ataxia and double vision.

Is Nitrapan safe during pregnancy?

Nitrapan 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 Nitrapan safe during breastfeeding?

Your baby may develop dependency to this medicine and may be at risk of developing withdrawal symptoms. Nitrapan passes into breast-milk; therefore, do not breast-feed if you are taking this medicine.

Can I take Nitrapan with alcohol?

Do not drink alcohol while you are taking Nitrapan tablets. Alcohol will increase the sedative effect of this medicine and can be dangerous.

Can I drive after taking Nitrapan?

The effects of Nitrapan 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 Nitrapan?

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 Nitrapan on an empty stomach?

Nitrapan 10mg tablet may be taken with or without food, but it is better to take it at a fixed time.

How much Nitrapan should I take to sleep?

The recommended adult dose of Nitrapan 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 Nitrapan take to work?

Nitrapan acts in 30 to 60 minutes to produce sleep lasting six to eight hours. Nitrapan is well absorbed with peak blood levels being achieved within two hours after administration.

How long does Nitrapan stay in my system?

The half-life of Nitrapan is on average 24 hours. Steady-state levels are achieved within five days. Nitrapan undergoes biotransformation to a number of metabolites none of which possesses significant clinical activity.

Can I take Nitrapan for a long time?

Nitrapan 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 Nitrapan?

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 Nitrapan?

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 Nitrapan make me depressed?

Nitrapan may causes Depression.

Can Nitrapan 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 Nitrapan 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.

*** Taking medicines without doctor's advice can cause long-term problems.
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