Cocculus - General Information:

A noncompetitive antagonist at GABA-A receptors and thus a convulsant. Cocculus blocks the gamma-aminobutyric acid-activated chloride ionophore. Although it is most often used as a research tool, it has been used as a CNS stimulant and an antidote in poisoning by CNS depressants, especially the barbiturates. [PubChem]

Pharmacology:

Cocculus is a toxin obtained from the seeds of the shrub Anamirta cocculus. It is used as a central nervous system stimulant, antidote, convulsant, and GABA (gamma aminobutyric acid) antagonist. It is a noncompetitive antagonist at GABAA receptors and thus a convulsant. Cocculus blocks the GABAActivated chloride ionophore. Although it is most often used as a research tool, it has been used as a CNS stimulant and an antidote in poisoning by CNS depressants, especially barbiturates.

Additional information about Cocculus

Cocculus Indication: Used internally for relieving respiratory distress. Also for use as an antidote in poisoning by CNS depressants, especially barbiturates.
Mechanism Of Action: Cocculus antagonizes the GABAA receptor channel directly, which is a ligand-gated ion channel concerned chiefly with the passing of chloride ions across the cell membrane. Therefore picrotoxin prevents Cl- channel permeability and thus promtes an inhibitory influence on the target neuron. Cocculus reduces conductance through the channel by reducing not only the opening frequency but also the mean open time. Cocculus also antagonizes GABAC receptors (also called GABAA-rho receptors) but the result of this action is not known. The GABAC receptor is also linked to chloride channels, with distinct physiological and pharmacological properties. In contrast to the fast and transient responses elicited from GABAA receptors, GABAC receptors mediate slow and sustained responses.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Picrotoxin
Synonyms: Not Available
Drug Category: Anti-barbituates; Stimulants; GABA receptor antagonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Picrotoxin: Cocculin; Cocculine; Cocculus; Coques du levant; Fish berry; Indian berry; Oriental berry;
Absorption: Not Available
Toxicity (Overdose): Oral, mouse: LD50 = 15 mg/kg. In large doses it is a powerful poison, causing unconsciousness, delirium, convulsions, gastro-enteritis and stimulation of the respiratory centre followed by paralysis, from which death sometimes results.
Protein Binding: Not Available
Biotransformation: Not Available
Half Life: Not Available
Dosage Forms of Cocculus: Solution / drops Oral
Liquid Oral
Chemical IUPAC Name: Not Available
Chemical Formula: C30H34O13
Picrotoxin on Wikipedia: http://en.wikipedia.org/wiki/Picrotoxin
Organisms Affected: Humans and other mammals

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