Paxane - General Information
A benzodiazepine derivative used mainly as a hypnotic. [PubChem]
Pharmacology of Paxane
Paxane, a benzodiazepine derivative, is a hypnotic agent which does not appear to decrease dream time as measured by rapid eye movements (REM). Furthermore, it decreases sleep latency and number of awakenings for a consequent increase in total sleep time.
Paxane for patients
To assure the safe and effective use of benzodiazepines, patients should be informed that, since benzodiazepines may produce psychological and physical dependence, it is advisable that they consult with their physician before either increasing the dose or abruptly discontinuing this drug.
No information provided.
Flurazepam hydrochloride is contraindicated in patients with known hypersensitivity to the drug.
Usage in Pregnancy: Benzodiazepines may cause fetal damage when administered during pregnancy. An increased risk of congenital malformations associated with the use of diazepam and chlordiazepoxide during the first trimester of pregnancy has been suggested in several studies.
Flurazepam hydrochloride is contraindicated in pregnant women. Symptoms of neonatal depression have been reported; a neonate whose mother received 30 mg of flurazepam hydrochloride nightly for insomnia during the 10 days prior to delivery appeared hypotonic and inactive during the first four days of life. Serum levels of N1-desalkyl-flurazepam in the infant indicated transplacental circulation and implicate this long-acting metabolite in this case. If there is a likelihood of the patient becoming pregnant while receiving flurazepam, she would be warned of the potential risks to the fetus. Patients should be instructed to discontinue the drug prior to becoming pregnant. The possibility that a woman of childbearing potential may be pregnant at the time of institution of therapy should be considered.
Additional information about Paxane
Paxane Indication: For short-term and intermittent use in patients with recurring insomnia and poor sleeping habits
Mechanism Of Action: Benzodiazepines bind nonspecifically to bezodiazepine receptors BNZ1, which mediates sleep, and BNZ2, 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 of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Drug Interactions: Amprenavir Amprenavir increases the effect and toxicity of benzodiazepine
Cimetidine Cimetidine increases the effect of the benzodiazepine
Clozapine Increased risk of toxicity
Ethotoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Fluconazole Fluconazole increases the effect of the benzodiazepine
Fosphenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Mephenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Phenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Fosamprenavir Amprenavir increases the effect and toxicity of benzodiazepine
Indinavir The protease inhibitor increases the effect of the benzodiazepine
Nelfinavir The protease inhibitor increases the effect of the benzodiazepine
Ritonavir The protease inhibitor increases the effect of the benzodiazepine
Saquinavir The protease inhibitor increases the effect of the benzodiazepine
Itraconazole The imidazole increases the effect of the benzodiazepine
Ketoconazole The imidazole increases the effect of the benzodiazepine
Kava Kava increases the effect of the benzodiazepine
Omeprazole Omeprazole increases the effect of benzodiazepine
Voriconazole The imidazole increases the effect of the benzodiazepine
Food Interactions: Take without regard to meals.
Generic Name: Flurazepam
Synonyms: Flurazepam HCL
Drug Category: Anti-anxiety Agents; GABA Modulators; Hypnotics and Sedatives
Drug Type: Small Molecule; Illicit; Approved
Absorption: Flurazepam hydrochloride is rapidly (30 minutes) absorbed from the gastrointestinal tract
Toxicity (Overdose): Coma, confusion, low blood pressure, sleepiness
Protein Binding: 83%
Biotransformation: Flurazepam is rapidly metabolized and is excreted primarily in the urine. Both hydroxyethyl flurazepam (the major metabolite) and N-desalkyl flurazepam are active. The N-desalkyl metabolite is slowly excreted in the urine as the conjugated form
Half Life: The mean apparent half-life of flurazepam is 2.3 hours. The half life of elimination of N1-des-alkyl- flurazepam ranged from 47 to 100 hours
Dosage Forms of Paxane: Tablet Oral
Chemical IUPAC Name: 7-chloro-1-(2-diethylaminoethyl)-5-(2-fluorophenyl)-3H-1,4-benzodiazepin-2-one
Chemical Formula: C21H23ClFN3O
Flurazepam on Wikipedia: https://en.wikipedia.org/wiki/Flurazepam
Organisms Affected: Humans and other mammals