Nitrazepam (Alodorm, Mogadon) is a benzodiazepine drug that has strong sedative, amnestic, anticonvulsant, and anxiolytic properties. When used for the treatment of insomnia, its effects last for 6 to 8 hours.
Nitrazepam (Alodorm) Uses:
Note:
- Not approved in the US
-
Insomnia:
- Insomnia, which is characterised by frequent nocturnal awakenings, trouble settling asleep, and early morning awakenings, can be treated and relieved temporarily.
-
Limitations of use:
- Restrict use to insomnia that impairs normal daytime functioning.
- Treatment should typically not exceed 7-10 consecutive days.
- If treatment continues for >2 to 3 consecutive weeks, reevaluation of the patient is required.
- Only a month's worth of medication should be prescribed for short-term (7 to 10 day) use.
-
Seizures:
- Managing myoclonic seizures
Nitrazepam (Alodorm) Dose in Adults
Nitrazepam (Alodorm) Dose in the treatment of Insomnia:
- P/O:
- 5-10 milligram at bedtime.
- Therapy shouldn't go longer than 7 to 10 days straight.
- Usage for more than 2 to 3 weeks in a row necessitates a thorough reevaluation of the patient.
Nitrazepam (Alodorm) Dose in Children
Nitrazepam (Alodrom) Dose in the treatment of Myoclonic seizures:
-
Infants and Children ≤30 kg:
- P/O:
- Usual dosage:
- 0.3 to 1 milligram/kilogram/day in 3 equally divided doses.
- Administer larger dose at bedtime, If doses are not divided equally,
Note:
- Therapy should be started and cautiously titrated based on response below the standard dosage range.
- Gradually increase the dose further if there is an inadequate response to the usual dosage.
- Manufacturer labeling does not specify a max dosage.
Nitrazepam Pregnancy Risk Category: D
- It is not recommended to use during pregnancy.
- Nitrazepam crosses over the human placenta.
- Certain benzodiazepines have teratogenic side effects. Nonetheless, more study is required.
- Low birth weights and premature births can be more common after maternal use of benzodiazepines.
- After exposure late in pregnancy, hypoglycemia and respiratory problems may develop in the neonate.
- Some benzodiazepines have been linked to neonatal withdrawal symptoms, which can occur as soon as days or weeks after birth.
Use of Nitrazepam while breastfeeding
- Breast milk contains Nitrazepam.
- There have been cases in which nursing infants experienced drowsiness, lethargy or weight loss after maternal use of some benzodiazepines.
- According to the manufacturer, breastfeeding should not be done.
Nitrazepam Dose in Kidney Disease:
- There are no dosage adjustments in the manufacturer's labeling.
- Use caution.
Nitrazepam Dose in Liver disease:
-
Mild to moderate impairment
- There are no dosage adjustments in the manufacturer's labeling.
- Use caution.
-
Severe impairment
- Contraindicated.
Side effects of Nitrazepam (Alodorm):
-
Cardiovascular:
- Hypotension
- Palpitations
-
Central Nervous System:
- Aggressive Behavior
- Agitation
- Amnesia
- Ataxia
- Confusion
- Delusions
- Depression
- Disorientation
- Dizziness
- Excitement
- Falling
- Fatigue
- Hallucination
- Hangover Effect
- Headache
- Hyperactivity
- Irritability
- Lethargy
- Myasthenia
- Nervousness
- Nightmares
- Outbursts Of Anger
- Psychosis
- Restlessness
- Sedation
- Staggering
- Withdrawal Syndromer
-
Dermatologic:
- Dermatological Reaction
-
Endocrine & Metabolic:
- Change In Libido
-
Gastrointestinal:
- Constipation
- Diarrhea
- Heartburn
- Nausea
- Sialorrhea
- Vomiting
-
Hematologic & Oncologic:
- Granulocytopenia
- Leukopenia
-
Hepatic:
- Abnormal Hepatic Function Tests
-
Hypersensitivity:
- Anaphylaxis
-
Neuromuscular & Skeletal:
- Muscle Spasticity
-
Ophthalmic:
- Blurred Vision
-
Respiratory:
- Aspiration
- Dyspnea
- Increased Bronchial Secretions
Contraindications to Nitrazepam:
- Hypersensitivity
- Myasthenia gravis.
- Severe respiratory impairment (eg, severe sleep apnea syndrome).
- Severe hepatic impairment.
- Use with children to hypnotize
Warnings and precautions
-
Anaphylaxis, anaphylactoid reactions
- Rarely reported as a result of use.
- Patients who have angioedema should not be given nitrazepam.
-
Anterograde amnesia
- Anterograde amnesia has been linked to benzodiazepines (Nelson 1999).
- If taken to induce sleep while on the road, may also cause transient global amnesia and traveler's amnesia.
- Patients should make sure they can get at least 7-8 hours of unbroken sleep after ingesting.
-
Aspiration pneumonia
- Rarely, patients with aspiration pneumonia can experience bronchial hypersecretion and excessive salivation/drooling.
-
Depression in the CNS:
- CNS depression can lead to mental or physical impairment.
- It is important to inform patients about tasks that require mental alertness, such as driving or operating machinery.
-
Paradoxical reactions
- Benzodiazepines have been associated with paradoxical effects.
- Patients with a history of alcohol abuse or psychiatric/personality disorders may be more likely to develop an alcohol-
- related disorder in adolescence or childhood or psychiatric/personality disorders.
-
Rebound insomnia
- After the withdrawal of therapy, transient insomnia can recur. This may be accompanied by anxiety, restlessness, mood changes, and other reactions.
-
Activities that are sleep-related:
- With benzodiazepines, hazardous sleep-related activities like sleep-driving and cooking while sleeping have been identified.
-
Depression
- Patients with depression should be cautious if there is a high risk of suicide.
-
Use of drugs:
- Patients with a history or alcoholism should be cautious.
- Drug dependency is possible.
- Prolonged use can lead to tolerance, psychological reliance, and/or physical dependence.
-
Hepatic impairment
- Patients with severe hepatic impairment should be cautious.
-
Renal impairment
- Use caution in patients with impaired renal function.
-
Respiratory disease
- Patients with severe respiratory problems should be cautious.
Nitrazepam (United States: Not available): Drug Interaction
|
Risk Factor C (Monitor therapy) |
|
|
Alcohol (Ethyl) |
CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). |
|
Alizapride |
May enhance the CNS depressant effect of CNS Depressants. |
|
Brexanolone |
CNS Depressants may enhance the CNS depressant effect of Brexanolone. |
|
Brimonidine (Topical) |
May enhance the CNS depressant effect of CNS Depressants. |
|
Bromopride |
May enhance the CNS depressant effect of CNS Depressants. |
|
Cannabidiol |
May enhance the CNS depressant effect of CNS Depressants. |
|
Cannabis |
May enhance the CNS depressant effect of CNS Depressants. |
|
Chlorphenesin Carbamate |
May enhance the adverse/toxic effect of CNS Depressants. |
|
CNS Depressants |
May enhance the adverse/toxic effect of other CNS Depressants. |
|
Cosyntropin |
May enhance the hepatotoxic effect of Nitrazepam. |
|
Dimethindene (Topical) |
May enhance the CNS depressant effect of CNS Depressants. |
|
Doxylamine |
May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. |
|
Dronabinol |
May enhance the CNS depressant effect of CNS Depressants. |
|
Esketamine |
May enhance the CNS depressant effect of CNS Depressants. |
|
Fosphenytoin |
Benzodiazepines may increase the serum concentration of Fosphenytoin. Shortterm exposure to benzodiazepines may not present as much risk as chronic therapy. |
|
HydrOXYzine |
May enhance the CNS depressant effect of CNS Depressants. |
|
Kava Kava |
May enhance the adverse/toxic effect of CNS Depressants. |
|
Lofexidine |
May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
|
Magnesium Sulfate |
May enhance the CNS depressant effect of CNS Depressants. |
|
Melatonin |
May enhance the sedative effect of Benzodiazepines. |
|
MetyroSINE |
CNS Depressants may enhance the sedative effect of MetyroSINE. |
|
Minocycline |
May enhance the CNS depressant effect of CNS Depressants. |
|
Mirtazapine |
CNS Depressants may enhance the CNS depressant effect of Mirtazapine. |
|
Nabilone |
May enhance the CNS depressant effect of CNS Depressants. |
|
Phenytoin |
Benzodiazepines may increase the serum concentration of Phenytoin. Short-term exposure to benzodiazepines may not present as much risk as chronic therapy. |
|
Piribedil |
CNS Depressants may enhance the CNS depressant effect of Piribedil. |
|
Pramipexole |
CNS Depressants may enhance the sedative effect of Pramipexole. |
|
ROPINIRole |
CNS Depressants may enhance the sedative effect of ROPINIRole. |
|
Rotigotine |
CNS Depressants may enhance the sedative effect of Rotigotine. |
|
Rufinamide |
May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. |
|
Selective Serotonin Reuptake Inhibitors |
CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. |
|
Teduglutide |
May increase the serum concentration of Benzodiazepines. |
|
Tetrahydrocannabinol |
May enhance the CNS depressant effect of CNS Depressants. |
|
Tetrahydrocannabinol and Cannabidiol |
May enhance the CNS depressant effect of CNS Depressants. |
|
Trimeprazine |
May enhance the CNS depressant effect of CNS Depressants. |
|
Yohimbine |
May diminish the therapeutic effect of Antianxiety Agents. |
|
Risk Factor D (Consider therapy modification) |
|
|
Blonanserin |
CNS Depressants may enhance the CNS depressant effect of Blonanserin. |
|
Buprenorphine |
CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. |
|
Chlormethiazole |
May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. |
|
CloZAPine |
Benzodiazepines may enhance the adverse/toxic effect of CloZAPine. Management: Consider decreasing the dose of (or possibly discontinuing) benzodiazepines prior to initiating clozapine. |
|
Droperidol |
May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
|
Flunitrazepam |
CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. |
|
HYDROcodone |
CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Avoid concomitant use of hydrocodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
|
Methadone |
Benzodiazepines may enhance the CNS depressant effect of Methadone. Management: Clinicians should generally avoid concurrent use of methadone and benzodiazepines when possible; any combined use should be undertaken with extra caution. |
|
Methotrimeprazine |
CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. |
|
Opioid Agonists |
CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
|
OxyCODONE |
CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
|
Perampanel |
May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. |
|
RifAMPin |
May decrease the serum concentration of Nitrazepam. Management: Monitor closely for reduced effects of nitrazepam. When possible, consider alternatives to one of these drugs, or increases in initial nitrazepam doses. |
|
Suvorexant |
CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. |
|
Tapentadol |
May enhance the CNS depressant effect of CNS Depressants. Management: Avoid concomitant use of tapentadol and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
|
Theophylline Derivatives |
May diminish the therapeutic effect of Benzodiazepines. |
|
Zolpidem |
CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. |
|
Risk Factor X (Avoid combination) |
|
|
Azelastine (Nasal) |
CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). |
|
Bromperidol |
May enhance the CNS depressant effect of CNS Depressants. |
|
OLANZapine |
May enhance the adverse/toxic effect of Benzodiazepines. Management: Avoid concomitant use of parenteral benzodiazepines and IM olanzapine due to risks of additive adverse events (e.g., cardiorespiratory depression). Olanzapine prescribing information provides no specific recommendations regarding oral administration. |
|
Orphenadrine |
CNS Depressants may enhance the CNS depressant effect of Orphenadrine. |
|
Oxomemazine |
May enhance the CNS depressant effect of CNS Depressants. |
|
Paraldehyde |
CNS Depressants may enhance the CNS depressant effect of Paraldehyde. |
|
Sodium Oxybate |
Benzodiazepines may enhance the CNS depressant effect of Sodium Oxybate. |
|
Thalidomide |
CNS Depressants may enhance the CNS depressant effect of Thalidomide. |
Monitoring parameters:
- Respiratory, cardiovascular, and mental status
How to administer Nitrazepam (Alodorm)?
P/O:
- Tablets can be dissolved, crumbled, or eaten whole when mixed with fluids.
For insomnia, take before bed. - Provide a higher dose at bedtime if doses are not evenly divided, or give 3 equally spaced doses to treat myoclonic seizures.
Mechanism of action of Nitrazepam (Alodorm):
- There are numerous locations in the Brain where nitrazepam can bind to stereospecific benzodiazepine receptors on postsynaptic GABA neurons, including the limbic system and the reticular formation.
- Increased neuronal membrane permeability for chloride ions results in an increase in neuronal excitability, which enhances the inhibitory effects of GABA.
- This is a shift in the chloride ions that results in hyperpolarization (a state less excitable) and stabilization.
- The GABA-A receptors appear to be responsible for benzodiazepine effects and receptors.
- Benzodiazepines don't bind to GABAB receptors.
The onset of action:
- 20-50 minutes
Absorption:
- Rapid
Distribution:
- Distributes into CSF, saliva (Kangas, 1979)
Protein binding:
- 87 percent
Metabolism:
- Hepatic: Nitroreduction, acetylation.
- no active metabolites
Bioavailability:
- ~80 percent
Half-life elimination:
- 30 hours (range: 18-57 hours),
- Elderly/ill patients: 40 hours
Time to peak, plasma:
- ~3 hours
Excretion:
- Urine (65 percent to 71 percent, ~1 percent as unchanged drug).
- Feces (14 percent to 20 percent)
International Brands of Nitrazepam:
- APO-Nitrazepam
- Mogadon
- SANDOZ Nitrazepam
- Alodorm
- Apodorm
- Arem
- Cerson
- Dumolid
- Epam
- Eunoctin
- Hypnol
- Hypnotex
- Imeson
- Insomin
- Mogadan
- Mogadon
- Mozepam
- Nitavan
- Nitrados
- Nitrapan
- Nitravet
- Nitredon
- Nitrom
- Nitrosun
- Noctin
- Novanox
- Octon
- Ormodon
- Pacisyn
- Paxadorm
- Radedorm
- Sleepin
Nitrazepam Brand Names in Pakistan:
Nitrazepam Tablets 5 mg |
|
| Mogadon | Roche Pakistan Ltd. |
