Helogaphen - General Information
An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal. [PubChem]
Pharmacology of Helogaphen
Helogaphen has antianxiety, sedative, appetite-stimulating and weak analgesic actions. The precise mechanism of action is not known. The drug blocks EEG arousal from stimulation of the brain stem reticular formation. The drug has been studied extensively in many species of animals and these studies are suggestive of action on the limbic system of the brain, which recent evidence indicates is involved in emotional responses. Hostile monkeys were made tame by oral drug doses which did not cause sedation. Helogaphen revealed a "taming" action with the elimination of fear and aggression. The taming effect of chlordiazepoxide was further demonstrated in rats made vicious by lesions in the septal area of the brain. The drug dosage which effectively blocked the vicious reaction was well below the dose which caused sedation in these animals.
Helogaphen 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 the drug.
Although clinical studies have not established a cause and effect relationship, physicians should be aware that variable effects an blood coagulation have been reported very rarely in patients receiving oral anticoagulants and chlordiazepoxide.
The concomitant use of alcohol or other central nervous system depressants may have an additive effect.
Chlordiazepoxide HCl Capsules are contraindicated in patients with known hypersensitivity to the drug.
Additional information about Helogaphen
Helogaphen Indication: For the management of anxiety disorders or for the short-term relief of symptoms of anxiety, withdrawal symptoms of acute alcoholism, and preoperative apprehension and anxiety.
Mechanism Of Action: Helogaphen binds to stereospecific benzodiazepine (BZD) binding sites on GABA (A) receptor complexes at several sites within the central nervous system, including the limbic system and reticular formation. BZDs enhance GABA-mediated chloride influx through GABA receptor channels, causing membrane hyperpolarization. The net neuro-inhibitory effects result in the observed sedative, hypnotic, anxiolytic, and muscle relaxant properties.
Drug Interactions: Cimetidine Cimetidine increases the effect of the benzodiazepine
Clozapine Increased risk of toxicity
Ethotoin Possible increased levels of the hydantoin, decrease of 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
Fluconazole Fluconazole increases the effect of the benzodiazepine
Indinavir 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
Voriconazole The imidazole increases the effect of the benzodiazepine
Kava Kava increases the effect of the benzodiazepine
Nelfinavir The protease inhibitor increases the effect of the benzodiazepine
Omeprazole Omeprazole increases the effect of benzodiazepine
Food Interactions: Take without regard to meals.
Generic Name: Chlordiazepoxide
Synonyms: Not Available
Drug Category: Anti-anxiety Agents; Hypnotics and Sedatives; Adjuvants, Anesthesia; Benzodiazepines; GABA Modulators
Drug Type: Small Molecule; Illicit; Approved
Other Brand Names containing Chlordiazepoxide: A-Poxide; Abboxide; Apo-Chlordiazepoxide; Balance; CD 2; CDO; CDP; Chloradiazepoxide; Chlordiazachel; Chlordiazepoxid; Chlordiazepoxide Base; Chlordiazepoxide Hcl; Chlordiazepoxidum; Chloridazepoxide; Chloridiazepide; Chloridiazepoxide; Chlorodiazepoxide; Chlozepid; Clopoxide; Clordiazepossido; Contol; Control; Decacil; Eden; Elenium; Helogaphen; Ifibrium; Kalmocaps; Librax; Librelease; Librinin; Libritabs; Librium; Limbitrol; Limbitrol Ds; Lygen; Menrium; Mesural; Methaminodiazepoxide; Mildmen; Multum; Napoton; Napton; Novo-Poxide; Psicosan; Radepur; Risolid; Silibrin; Tropium; Viopsicol;
Absorption: Not Available
Toxicity (Overdose): LD50=537 mg/kg (Orally in rats). Signs of overdose include respiratory depression, muscle weakness, somnolence (general depressed activity).
Protein Binding: Not Available
Half Life: 24-48 hours
Dosage Forms of Helogaphen: Capsule Oral
Chemical IUPAC Name: 7-chloro-4-hydroxy-N-methyl-5-phenyl-3H-1,4-benzodiazepin-2-imine
Chemical Formula: C16H14ClN3O
Chlordiazepoxide on Wikipedia: https://en.wikipedia.org/wiki/Chlordiazepoxide
Organisms Affected: Humans and other mammals