Nuctalon
Nuctalon Uses, Dosage, Side Effects, Food Interaction and all others data.
A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than diazepam or nitrazepam.
Nuctalon, a triazolobenzodiazepine derivative, is an oral hypnotic agent with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than diazepam or nitrazepam.
| Trade Name | Nuctalon |
| Availability | Prescription only |
| Generic | Estazolam |
| Estazolam Other Names | Estazolam, Estazolamum |
| Related Drugs | amitriptyline, lorazepam, melatonin, zolpidem, diphenhydramine, Ativan |
| Type | |
| Formula | C16H11ClN4 |
| Weight | Average: 294.738 Monoisotopic: 294.067224079 |
| Protein binding | 93% protein bound, independant of concentration. |
| Groups | Approved, Illicit |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Nuctalon is a benzodiazepine used for the short-term management of insomnia.
For the short-term management of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings.
Nuctalon is also used to associated treatment for these conditions: Insomnia
How Nuctalon works
Benzodiazepines bind nonspecifically to benzodiazepine receptors, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Toxicity
Symptoms of overdose include confusion, depressed breathing, drowsiness and eventually coma, lack of coordination, and slurred speech.
Food Interaction
- Avoid alcohol.
- Take with or without food. The absorption is unaffected by food.
Nuctalon Alcohol interaction
[Moderate] GENERALLY AVOID:
Acute ethanol ingestion may potentiate the CNS effects of many benzodiazepines.
Tolerance may develop with chronic ethanol use.
The mechanism may be decreased clearance of the benzodiazepines because of CYP450 hepatic enzyme inhibition.
Also, it has been suggested that the cognitive deficits induced by benzodiazepines may be increased in patients who chronically consume large amounts of alcohol.
Patients should be advised to avoid alcohol during benzodiazepine therapy.
Nuctalon Drug Interaction
Moderate: aripiprazole, aripiprazole, zolpidem, zolpidem, duloxetine, duloxetine, eszopiclone, eszopiclone, pregabalin, pregabalin, quetiapine, quetiapine, alprazolam, alprazolamUnknown: amphetamine / dextroamphetamine, amphetamine / dextroamphetamine, cholecalciferol, cholecalciferol, lisdexamfetamine, lisdexamfetamine
Nuctalon Disease Interaction
Major: acute alcohol intoxication, closed-angle glaucoma, drug dependence, renal/liver disease, respiratory depression, seizuresModerate: depression, obesity, paradoxical reactions
Elimination Route
Tablets have been found to be equivalent in absorption to an orally administered solution of estazolam. In healthy subjects who received up to three times the recommended dose, peak estazolam plasma concentrations occurred within two hours after dosing (range 0.5 to 6.0 hours) and were proportional to the administered dose, suggesting linear pharmacokinetics over the dosage range tested.
Half Life
The range of estimates for the mean elimination half-life of estazolam varies from 10 to 24 hours.
Elimination Route
Nuctalon is extensively metabolized. The elimination of the parent drug takes place via hepatic metabolism of estazolam to hydroxylated and other metabolites that are eliminated largely in the urine both free and conjugated. Less than 5% of a 2 mg dose of estazolam was excreted unchanged in the urine, with only 4% of the dose appearing in the feces. Radiolabel mass balance studies indicate that the main route of excretion is via the kidneys. After 5 days, 87% of the administered radioactivity was excreted in human urine. Less than 4% of the dose was excreted unchanged.
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