Nifoxipam is a benzodiazepine that is being sold online as a research chemical (sometimes referred to as a designer drug)[1]. Though not regulated and potentially not scheduled (illegal) it carries similar effects of other benzodiazepine and can be used for anxiety, insomnia, sedation and has anxiolytic, hypnotic, sedative, anticonvulsant, muscle relaxant, and amnesic effects. As with other benzodiazepines, nifoxipam binds to specific sites on the GABAA receptor, and is in the same class of hypnotic nitrobenzodiazepines as nitrazepam, nimetazepam, flunitrazepam, and flurazepam. As with all GABAergic drugs, overdose can be lethal when mixed with other depressents like opiates and alcohol. This is particularly concerning because Nifoxipam is a research chemical and has not been approved for medicinal use: addiction and overdose are possible.[2]
Introduction to Nifoxipam
Nifoxipam is a long-lasting psychoactive drug of the benzodiazepine class which produces anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsant, anti-nausea and amnesic effects. Nifoxipam, like other benzodiazepines, binds to specific sites on the GABAA gamma-amino-butyric acid receptor.
It is classed as a 7-nitrobenzodiazepine and is therefore in the same category as other hypnotic nitrobenzodiazepines such as nitrazepam (7-nitro-1,4-benzodiazepin-2-one), nimetazepam (1-methyl-nitrazepam), flunitrazepam (2'-fluoro,1-methyl-nitrazepam) and ''flurazepam'' (1-(2-diethylamino)ethyl-2'-fluoro-nitrazepam).
Using Nifoxipam
Nifoxipam has potential use for the short-term treatment of anxiety, insomnia, acute seizures, and the sedation of hospitalized patients. However, it is currently exclusively sold by online research chemical vendors for use as a recreational psychoactive substance.Ways of Administration
Nifoxipam is administered in tablet form, ranging from 0.5mg to 2mg. It is also available in powder form.Dose
Column 1 Column 2 Threshold 0.5mg Light 1mg Medium 2mg Strong 2+mg Effects of Nifoxipam
Physical effects
The physical effects of nifoxipam can be broken down into several components which progressively intensify proportional to dosage. These are described below and generally include:
Sedation - In terms of energy level alterations, nifoxipam is moderately sedating and can potentially result in a lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit down and generally feel as if they are constantly on the verge of passing out instead of engaging in physical activities. This sense of sleep deprivation increases proportional to dosage and eventually becomes powerful enough to force a person into complete unconsciousness.
Motor control loss - Lack of coordination may result in falls and injuries, in particular, in the elderly. Another result of motor control loss is the impairment of driving skills and the increased likelihood of road traffic accidents.
Muscle relaxation
Dizziness
Respiratory depression
Cognitive effects
The cognitive effects of nifoxipam can be broken down into several components which progressively intensify proportional to dosage. The general head space of nifoxipam is described by many as one of intense sedation and decreased inhibition. It contains a large number of typical depressant cognitive effects.
The most prominent of these cognitive effects generally include:
Anxiety suppression
Thought deceleration
Disinhibition
Information processing suppression
Euphoria
Amnesia
Compulsive redosing
Delusions of sobriety - This is the false belief that one is perfectly sober despite obvious evidence to the contrary such as severe cognitive impairment and an inability to fully communicate with others.
Paradoxical effects
Paradoxical reactions such as increased seizures (in epileptics), aggression, increased anxiety, violent behavior, loss of impulse control, irritability and suicidal behavior sometimes occur (although they are rare in the general population, with an incidence rate below 1%).[4][5] These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.[6][7]Nifoxipam combinations
Recreational drug combinations with Nifoxipam
No Recreational drug combinations with Nifoxipam have been added to this wiki yet.Dangerous interactions with Nifoxipam
As with all benzodiazepines, it is dangerous to mix this drug with other Central Nervous System (CNS) depressants. This can cause slowed respiration, heart rate, and death.Medication interactions with Nifoxipam
During Serotonin Syndrome or Serotonin Toxicity benzodiazepines are often used in order to lower neurological excitability.Potentiators of Nifoxipam
It is possible that, as with other benzodiazepines, Grapefruit Juice may inhibit Nifoxipam's metabolism from the body. Below is a study regarding another benzodiazepine, Alprazolam;
The effects of repeated ingestion of grapefruit juice, an inhibitor of cytochrome P450 3A4 (CYP3A4), on the pharmacokinetics and pharmacodynamics of both single and multiple oral doses of alprazolam, a substrate of CYP3A4, were examined.
In study 1, eight healthy volunteers ingesting 600 ml/day water or grapefruit juice for 10 days took a single oral 0.8-mg dose of alprazolam on the eighth day.
Plasma drug concentrations were monitored up to 48 h after alprazolam dosing together with evaluation of psychomotor function. Grapefruit juice altered neither the plasma concentrations of alprazolam at any time points, any pharmacokinetic parameters, nor the majority of psychomotor function parameters in subjects.
In study 2, 11 patients with anxiety disorders receiving alprazolam (0.8-2.4 mg/day) ingested grapefruit juice (600 ml/day) for 7 days. Blood samples were collected before and during grapefruit juice ingestion and 1 week after its discontinuation together with an assessment of clinical status.
Grapefruit juice altered neither the steady-state plasma concentration of alprazolam nor the clinical status in patients. The present study shows that grapefruit juice is unlikely to affect pharmacokinetics or pharmacodynamics of alprazolam due to its high bioavailability.Different Uses for Nifoxipam
Recreational use of Nifoxipam
Chemistry of Nifoxipam
Systematic(IUPAC) name: 5-(2-fluorophenyl)-3-hydroxy-7-nitro-1,3-dihydro-2H-1,4-benzodiazepin-2-one Synonyms: None Molecular Formula: C15H10FN3O4 Molar mass: 315.26 g/mol CAS Registry Number: 74723-10-7 Melting Point: Boiling Point: no data Flash Point: no data Solubility: Additionnal data: LogP: 10.45 Notes: Aspect: Crystalline Solid; Stability: 2 years Reagent test results of Nifoxipam
The Dangers of Nifoxipam
General Warnings
Side Effects and Interactions
Potential Side Effects
Potential Drug Interactions
Association with other depressants might lead to coma or death.Potential Food Interactions
Physical Health Risks
The risks associated with consumption of Nifoxipam are similar to other benzodiazepines. They include addiction, tolerance, potentially deadly withdrawal.Benzodiazepine addiction
Usage of Nifoxipam on a regular basis can cause typical benzodiazepine addiction, habituation, and tolerance.
If you have been prescribed Nifoxipam for more than 4 weeks, seek medical attention before ceasing use.Mental Health Risks
Benzodiazepine use long term has been linked to delayed mental function, memory problems and dementia in elderly people.Overdose
Benzodiazepines are among the most frequently prescribed drugs worldwide.
This popularity is based not only on their efficacy but also on their remarkable safety.
Pure benzodiazepine overdoses usually induce a mild to moderate central nervous system depression; deep coma requiring assisted ventilation is rare, and should prompt a search for other toxic substances.
The severity of the CNS depression is influenced by the dose, the age of the patient and his or her clinical status prior to the ingestion, and the coingestion of other CNS depressants.
In severe overdoses, benzodiazepines can occasionally induce cardiovascular and pulmonary toxicity, but deaths resulting from pure benzodiazepine overdoses are rare. Quantitative determinations of benzodiazepines are not useful in the clinical management of intoxicated patients since there is no correlation between serum concentrations and pharmacological and toxicological effects.
Benzodiazepine overdoses occurring during pregnancy rarely induce serious morbidity in mothers or fetuses, although large doses administered near delivery can induce respiratory depression in neonates. The teratogenic potential of benzodiazepines remains controversial, but is probably small if it exists at all.
There is clear evidence that the prolonged use of even therapeutic doses of benzodiazepines will lead to dependence. The risk of developing significant withdrawal symptoms is related to dosage and duration of treatment. Prevention of gastrointestinal absorption should be initiated in all intentional benzodiazepine overdoses. Forced diuresis and dialysis techniques are not indicated since they will not significantly accelerate the elimination of these agents. Intravenous administration of flumazenil, a pure benzodiazepine antagonist, effectively reverses benzodiazepine-induced CNS depression.Reported Deaths
More Nifoxipam Sections and Information
Nifoxipam image Gallery: Post and view pictures of Nifoxipam.
Addiction Calculator: Do this small test to calculate your dependency.
References
http://www.ncbi.nlm.nih.gov/entrez/q..._uids=10907671
Psychopharmacology (Berl). 2000 Jun;150(2):185-90. Related Articles,Links
Effects of repeated ingestion of grapefruit juice on the single and multiple oral-dose pharmacokinetics and pharmacodynamics of alprazolam.
Yasui N, Kondo T, Furukori H, Kaneko S, Ohkubo T, Uno T, Osanai T, Sugawara K, Otani K.
Department of Neuropsychiatry, Hirosaki University School of Medicine, Japan.
Drug Saf. 1991 Jul-Aug;6(4):247-65.
Benzodiazepine poisoning. Clinical and pharmacological considerations and treatment.
Gaudreault P1, Guay J, Thivierge RL, Verdy I.
Malanciuc C, et al. Analytical characterization of flunitrazepam. Farmacia. 57, 167-83. (2009)
Benzodiazepine interactions with GABA receptors | http://www.ncbi.nlm.nih.gov/pubmed/6147796
Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review]
Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr
Bond AJ | Drug-induced behavioural disinhibition: incidence, mechanisms and therapeutic implications | CNS Drugs
Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev
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