Norfludiazepam is a designer benzodiazepine that shares structural similarities with the drug diazepam . It is the active metabolite of flurazepam and fludiazepam but has a longer half-life than flurazepam. Producers and researchers often use it to make midazolam — either as an intermediate or as the starting material itself .
Neither the 1961 Single Convention on Narcotic Drugs nor the 1971 United Nations Convention on Psychotropic Substances regulates norfludiazepam.
First identified in Stockholm, Sweden, by Swedish customs in 2016, norflurazepam appeared on the scene as a white powder. Since 2016, the reputation surrounding it has marketed it as a designer drug.
Status | Research chemical 💊 |
Common Dosage | 5-10 mg |
PubChem ID | 4540 |
CAS# | 2886-65-9 |
IUPAC Name | 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-1,4-benzodiazepin-2-one |
Other Names | Norfludiazepam, N-Desalkylflurazepam, Norflutoprazepam, Descarbethoxyloflazepate |
Norflurazepam is largely metabolized into inactive metabolites by the cytochrome P450 enzymes, including the CYP3A4 enzyme that takes place in the liver.
Intermediate-acting (10-16 hours). Onset is within 45-120 minutes, and after-effects may last for 1-12 hours.
A light dose of norflurazepam is 2 to 5 mg, and the common dose is 5 to 10 mg. Most people consider 10 to 20 mg and over to be a strong dose.
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**Caution:** Benzodiazepines have a narrow therapeutic window. Dose equivalents may not be accurate in higher doses.
This calculator does not substitute for clinical experience and is meant to serve only as a reference for determining oral benzodiazepine equivalence.
Please consult a medical practitioner before taking benzodiazepines.
The γ-aminobutyric acid type A (GABA-A) receptor — expressed on both the presynaptic and postsynaptic terminal of neurons — is the main target of benzodiazepines.
These GABA channels primarily function through ligand-gated ion channels. The membrane becomes hyperpolarized when these ligand-gated ion channels open, inhibiting neurotransmission. GABA is one of the body’s primary inhibitory neurotransmitters.
The GABA receptor complex is made up of five different protein subunits that are broadly distributed throughout the nervous system; 2 subunits, 2 subunits, and 1 subunit constitute it. Additionally, every one of these subunits comes in several isoforms.
Between the α and γ subunits is the location of benzodiazepines’ binding site [5]. The GABA-A receptors transform chemical inputs into electrical signals in a fraction of a millisecond. Due to this interaction, the GABA-A receptor undergoes a conformational change, and subsequent responses follow.
Since even small variations in just one subtype may radically change properties like potency, various benzodiazepines have diverse effects. This means that even molecules with a similar structural makeup might vary significantly. Norflurazepam binds unselectively to the numerous benzodiazepine receptor subtypes.
GABA-A receptors quickly inhibit the whole basal ganglia network. Norflurazepam is a benzodiazepine capable of various physical and mental effects by binding to various subtypes of GABA-A.
Norflurazepam is a research chemical with very little research on it. Since it’s a research chemical, it has an unknown safety profile.
Based on a few reports, the drug has addictive potential, just like other benzodiazepines do. In the event of abrupt cessation, the user may experience unpleasant withdrawal symptoms such as tremors, stomach pain, and perspiration.
Moreover, respiratory issues or coma are a serious risk for users combining the drug with other depressants like alcohol.
Common side effects of norflurazepam include:
Serious side effects of norflurazepam include:
If you suffer any of the above, seek immediate medical attention.
Norflurazepam, like many other drugs in its class, has a chance of becoming addictive and may cause withdrawal symptoms. Here are some words of advice to minimize the harm associated with this drug.
Drug dependency is the state of feeling compelled to use a substance. Consult your doctor if you feel you can’t go without the drug, and never buy from a source that’s not reputable.
This applies to any drug you are taking, not only norflurazepam. It is dangerous to use this substance with any others, especially benzodiazepines, sedatives, antihistamines, or depressants like alcohol.
Using norflurazepam when you have certain medical issues may harm your health. This is especially true for anyone experiencing:
Norflurazepam is an intermediate-acting 1,4-benzodiazepine with a half-life averaging 24-74 hours. It’s time for the onset of action is about 45 to 120 minutes.
Other benzodiazepines having similar properties as those of norflurazepam are:
Norflurazepam | Diazepam | Chlordiazepoxide | Pinazepam | Bromazepam | |
Chemical composition | 1,4-benzodiazepine | 1,4-benzodiazepine | 1,4-benzodiazepine | 1,4-benzodiazepine | 1,4-benzodiazepine |
Route of administration | Oral | IV, IM | Oral, IV | Oral | Oral |
Onset of action | 45 to 120 minutes | 15 to 60 minutes | 1 to 2 hours (oral) | 45 to 60 minutes | 60 minutes |
Peak concentration | 2 to 4 hours | 1 to 1.5 hours | 2 hours | 2 to 3 hours | 1 to 4 hours |
Duration of effects | Intermediate-acting (10 to 16 hours) | Long-acting (20 to 80 hours) | Long-acting (36 to 200 hours) | Long-acting ( > 48 hours) | Intermediate-acting (8 to 19 hours) |
Mechanism of action | GABA-A receptor agonist | GABA-A receptor agonist | GABA-A receptor agonist | GABA-A receptor agonist | GABA-A receptor agonist |
Medical Uses | Strong sedation | Seizures, alcohol withdrawal, insomnia, muscle spasms, panic disorder, anxiety disorders | Panic disorders, alcohol withdrawal, anxiety disorders | Anxiety disorder, insomnia, muscle relaxant | Anxiety disorder, alcohol withdrawal |
Here are a few natural alternatives to norflurazepam. Many reports claim these compounds have benzodiazepine-like effects.
However, there is a lack of clinical evidence to support their effectiveness. Therefore, approach these alternatives with caution.
An alternative option to manage anxiety is kava extract (Piper methysticum). Compared to a placebo in a double-blind, randomized trial to treat anxiety, kava showed a substantial reduction in anxiety. However, it also stated that while the extract is generally safe for short-term use, additional research is needed to determine its safety for long-term usage.
Centella asiatica, often known as gotu kola, has long been a part of traditional Chinese and Ayurvedic medicine. Research indicates that gotu kola has calming benefits on people, as seen by a reduction in acoustic startle response (ASR). This measures a muscle’s response to sudden noise and suggests it is an alternative worthy of consideration [9].
A well-liked sleep aid, Valerian root comes in a variety of forms, including dried roots, tinctures, and extracts. Valerian can also be a viable substitute due to its beneficial effects on anxiety.
A perennial shrub called St. John’s wort (Hypericum perforatum) is widely popular for its anxiolytic properties. Numerous locations in the body are where the substance binds to GABA-A, which has proven effective in treating anxiety and depression in patients.
Another natural ingredient, passion flower (Passiflora incarnata Linn), has long been a successful treatment modality. While there is a need for further research, some studies suggest using it reduces anxiety, particularly for those who have a generalized anxiety disorder (GAD).
This section answers some of the most frequently asked questions about norflurazepam.
Norflurazepam is not a prescription medication because it lacks adequate study and evidence. There are plenty of other, safer options than this substance.
Norflurazepam is not yet approved for human use, and it is unclear when — or if — this will happen. All pharmaceuticals must undergo significant testing and study before being available to the general population.
Norflurazepam is strongly sedating and has the risk of developing a dependence on it. Make sure not to take it without consulting a physician. Contact your physician if you develop an addiction and feel like you can’t go a day without it.
It is incredibly risky to combine benzodiazepines with other medicines, especially other benzodiazepines, sedatives, or alcohol. This risk only increases when dealing with these newer substances.
A severe danger exists of developing respiratory issues or perhaps collapsing or going into a coma.
As a research chemical, norflurazepam is available online, but the reputability of these sources is uncertain. It’s best not to gamble on it since this is not yet something a doctor can prescribe for regulated use.
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