Norflurazepam: A Look At the Effects & Risks of This Designer Benzo
Norfludiazepam is a designer benzodiazepine that shares structural similarities with the drug diazepam [1]. 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 [2].
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 [3].
Norflurazepam Specs
| 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 |
Metabolism
Norflurazepam is largely metabolized into inactive metabolites by the cytochrome P450 enzymes, including the CYP3A4 enzyme that takes place in the liver.
Duration of Effects
Intermediate-acting (10-16 hours). Onset is within 45-120 minutes, and after-effects may last for 1-12 hours.
What is the Dose of Norflurazepam?
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.
Benzodiazepine Dosage Equivalency Calculator
**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.
How Does Norflurazepam Work?
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 [4].
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 [6]. 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 [7].
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.
Is Norflurazepam Safe? Risks & Side Effects
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.
Side Effects Of Norflurazepam
Common side effects of norflurazepam include:
- Blurred vision
- Dizziness
- Decreased desire for sexual activity
- Drowsiness
- Increased frequency of urination
- Increased salivation
- Mood disturbances like low mood or even depression
- Muscle weakness or fatigue
- Memory or cognitive impairment
- Sleep disturbances
- Unsteadiness or gait problems
Serious side effects of norflurazepam include:
- Anaphylaxis symptoms include swelling of the lips, tongue, or face, hives, itching, trouble swallowing or speaking, hoarseness of voice, and disorientation
- Bleeding from the gums or nose
- Confusion
- Hallucinations or delusions
- Heart-involvement symptoms such as limb edema, breathing difficulties, and palpitations
- Memory loss
- Respiratory issues, such as difficulty breathing or short, shallow breaths
- Suicidal ideation
- Yellowing of the skin or eyes, which indicate liver dysfunction
If you suffer any of the above, seek immediate medical attention.
Harm Reduction: Norflurazepam
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.
1. Know the Signs of Addiction
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.
2. Avoid Drug Interactions
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.
3. Do Not Take The Drug If You Have Certain Conditions
Using norflurazepam when you have certain medical issues may harm your health. This is especially true for anyone experiencing:
- Kidney issues
- Liver issues
- Pregnancy or breastfeeding children
Similar Benzodiazepines
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 vs. Other Intermediate to Long-Acting Benzodiazepines:
| 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 |
Alternatives to Benzodiazepines
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.
1. Kava
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 [8].
2. Gotu Kola
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].
3. Valerian Root
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 [10].
4. St. John’s Wort
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 [11].
5. Passionflower
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) [11].
Norflurazepam FAQs
This section answers some of the most frequently asked questions about norflurazepam.
Can I get a prescription for norflurazepam?
Norflurazepam is not a prescription medication because it lacks adequate study and evidence. There are plenty of other, safer options than this substance.
How long will it take for norflurazepam to be legally available?
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.
Will I become addicted to norflurazepam?
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.
Can I mix norflurazepam with other drugs?
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.
Can I buy norflurazepam from online vendors?
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.
References
- Orsolini, L., Corkery, J. M., Chiappini, S., Guirguis, A., Vento, A., Berardis, D. D., Papanti, D., & Schifano, F. (2020). ‘New/Designer Benzodiazepines’: An Analysis of the Literature and Psychonauts’ Trip Reports. Current Neuropharmacology, 18(9), 809-837.
- Sternbach, L. H., Fryer, R. I., Metlesics, W., Sach, G., & Stempel, A. (1962). Quinazolines and 1, 4-benzodiazepines. V. o-aminobenzophenones1a, b. The Journal of Organic Chemistry, 27(11), 3781-3788.
- Riva, R., de Anna, M., Albani, F., & Baruzzi, A. (1981). Rapid quantitation of flurazepam and its major metabolite, N-desalkylflurazepam, in human plasma by gas—liquid chromatography with electron-capture detection. Journal of Chromatography B: Biomedical Sciences and Applications, 222(3), 491-495.
- Moosmann, B., & Auwärter, V. (2018). Designer benzodiazepines: another class of new psychoactive substances. In New psychoactive substances (pp. 383-410). Springer, Cham.
- Olsen, R. W., & Sieghart, W. (2008). International Union of Pharmacology. LXX. Subtypes of γ-aminobutyric acidA receptors: classification on the basis of subunit composition, pharmacology, and function. Update. Pharmacological reviews, 60(3), 243-260.
- Goetz, T., Arslan, A., Wisden, W., & Wulff, P. (2007). GABAA receptors: structure and function in the basal ganglia. Progress in brain research, 160, 21-41.
- Manchester, K. R., Maskell, P. D., & Waters, L. (2018). Experimental versus theoretical log D7. 4, pKa and plasma protein binding values for benzodiazepines appearing as new psychoactive substances. Drug Testing and Analysis, 10(8), 1258-1269.
- Pittler, M. H., & Ernst, E. (2003). Kava extract versus placebo for treating anxiety. Cochrane Database of Systematic Reviews, (1)
- Bradwejn, J., Zhou, Y., Koszycki, D., & Shlik, J. (2000). A double-blind, placebo-controlled study on the effects of Gotu Kola (Centella asiatica) on acoustic startle response in healthy subjects. Journal of clinical psychopharmacology, 20(6), 680-684.
- Shahinfar, J., Zeraati, H., Masrorniya, M., & Shojaei, S. (2016). Comparison of valerian extract and diazepam on anxiety before orthopedic surgery. Journal of Patient Safety & Quality Improvement, 4(4), 434-440.
- Lakhan, S. E., & Vieira, K. F. (2010). Nutritional and herbal supplements for anxiety and anxiety-related disorders: systematic review. Nutrition journal, 9(1), 1-14.
