Apaurin - General Information
A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of gamma-aminobutyric acid activity. It is used in the treatment of severe anxiety disorders, as a hypnotic in the short-term management of insomnia, as a sedative and premedicant, as an anticonvulsant, and in the management of alcohol withdrawal syndrome. (From Martindale, The Extra Pharmacopoeia, 30th ed, p589)
Pharmacology of Apaurin
Apaurin, a benzodiazepine, generates the same active metabolite as chlordiazepoxide and clorazepate. In animals, diazepam appears to act on parts of the limbic system, the thalamus and hypothalamus, and induces calming effects. Apaurin, unlike chlorpromazine and reserpine, has no demonstrable peripheral autonomic blocking action, nor does it produce extrapyramidal side effects; however, animals treated with diazepam do have a transient ataxia at higher doses. Apaurin was found to have transient cardiovascular depressor effects in dogs. Long-term experiments in rats revealed no disturbances of endocrine function. Injections into animals have produced localized irritation of tissue surrounding injection sites and some thickening of veins after intravenous use.
Apaurin for patients
This medicine is used to treat anxiety. This medicine is used to calm you.
It may be prescribed for patients who have trouble sleeping, Take this
medicine exactly as directed. It may be taken with food or milk if stomach
upset occurs, this medicine may cause drowsiness, possible drug interactions
may occur with other sedating medications or pain medications. Talk to your
doctor if you are taking any medications for depression, pain, or seizures.
Other sedative medications including over-the-counter antihistimines can
increase the side effects of this medicine and should be used cautiously.
No information provided.
Additional information about Apaurin
Apaurin Indication: Used in the treatment of severe anxiety disorders, as a hypnotic in the short-term management of insomnia, as a sedative and premedicant, as an anticonvulsant, and in the management of alcohol withdrawal syndrome.
Mechanism Of Action: Benzodiazepines bind nonspecifically to benzodiazepine receptors which mediate sleep, 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
Clarithromycin The macrolide increases the effect of the benzodiazepine
Clozapine Increased risk of toxicity
Digoxin The benzodiazepine increases the effect of digoxin
Erythromycin The macrolide increases the effect of the benzodiazepine
Ethotoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Fluconazole Fluconazole increases the effect of the benzodiazepine
Fosamprenavir Amprenavir increases the effect and toxicity of benzodiazepine
Fosphenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Indinavir The protease inhibitor increases the effect of the benzodiazepine
Itraconazole The imidazole increases the effect of the benzodiazepine
Josamycin The macrolide increases the effect of the benzodiazepine
Kava Kava increases the effect of the benzodiazepine
Ketoconazole The imidazole increases the effect of the benzodiazepine
Mephenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Nelfinavir The protease inhibitor increases the effect of the benzodiazepine
Omeprazole Omeprazole increases the effect of benzodiazepine
Phenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Quinupristin This combination presents an increased risk of toxicity
Rifampin Rifampin decreases the effect of benzodiazepine
Ritonavir The protease inhibitor increases the effect of the benzodiazepine
Saquinavir The protease inhibitor increases the effect of the benzodiazepine
St. John's Wort St. John's Wort could reduce the benzodiazepine effect
Voriconazole The imidazole increases the effect of the benzodiazepine
Food Interactions: Avoid alcohol.
Take with food.
Avoid excessive quantities of coffee or tea (caffeine).
Avoid taking with grapefruit or grapefruit juice as grapefruit can significantly increase serum levels of this product.
Generic Name: Diazepam
Synonyms: DAP; Methyldiazepinone
Drug Category: Adjuvants, Anesthesia; Anesthetics, Intravenous; Anti-anxiety Agents; Anticonvulsants; Antiemetics; GABA Modulators; Hypnotics and Sedatives; Muscle Relaxants, Central
Drug Type: Small Molecule; Illicit; Approved
Other Brand Names containing Diazepam: Alboral; Aliseum; Alupram; Amiprol; An-Ding; Ansiolin; Ansiolisina; Apaurin; Apo-Diazepam; Apozepam; Armonil; Assival; Atensine; Atilen; Bensedin; Bialzepam; Calmocitene; Calmpose; Cercine; Ceregulart; Condition; Diacepan; Dialag; Dialar; Diapam; Diastat; Diazemuls; Diazemulus; Diazepam Intensol; Diazepan; Diazetard; Dienpax; Dipam; Dipezona; Dizac; Domalium; Duksen; Duxen; E-Pam; Eridan; Eurosan; Evacalm; Faustan; Faustan,; Freudal; Frustan; Gewacalm; Gihitan; Kabivitrum; Kiatrium; LA III; La-Iii; Lamra; Lembrol; Levium; Liberetas; Mandrozep; Morosan; Neurolytril; Noan; Novazam; Novo-Dipam; Paceum; Pacitran; Paranten; Paxate; Paxel; Plidan; Pms-Diazepam; Pro-Pam; Q-Pam; Q-Pam Relanium; Quetinil; Quiatril; Quievita; Relaminal; Relanium; Renborin; Ruhsitus; Saromet; Sedapam; Sedipam; Seduksen; Seduxen; Serenack; Serenamin; Serenzin; Servizepam; Setonil; Sibazon; Sibazone; Solis; Sonacon; Stesolid; Stesolin; Tensopam; Tranimul; Tranqdyn; Tranquase; Tranquirit; Tranquo-Puren; Tranquo-Tablinen; Umbrium; Unisedil; Usempax Ap; Valaxona; Valeo; Valiquid; Valitran; Valium; Valrelease; Vatran; Velium; Vival; Vivol; Zetran; Zipan; Apaurin.
Absorption: Essentially complete, with a bioavailability of 93%.
Toxicity (Overdose): Symptoms of overdose include somnolence, confusion, coma, and diminished reflexes. Respiration, pulse and blood pressure should be monitored.
Protein Binding: 98.5%
Biotransformation: Hepatic via the Cytochrome P450 enzyme system. The main active metabolite is desmethyldiazepam, in addition to minor active metabolites including temazepam and oxazepam.
Half Life: Biphasic 1-2 days and 2-5 days, active metabolites with long half lives.
Dosage Forms of Apaurin: Emulsion Intramuscular
Chemical IUPAC Name: 7-chloro-1-methyl-5-phenyl-3H-1,4-benzodiazepin-2-one
Chemical Formula: C16H13ClN2O
Diazepam on Wikipedia: http://en.wikipedia.org/wiki/Diazepam
Organisms Affected: Humans and other mammals