cocculin

cocculin Uses, Dosage, Side Effects, Food Interaction and all others data.

A noncompetitive antagonist at GABA-A receptors and thus a convulsant. cocculin 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]

cocculin 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. cocculin 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.

Table Of contents

• cocculin
• Uses
• Dosage
• Side Effect
• Precautions
• Interactions
• Uses during Pregnancy
• Uses during Breastfeeding
• Accute Overdose
• Food Interaction
• Half Life
• Volume of Distribution
• Clearance
• Interaction With other Medicine
• Contradiction
• Storage

Trade Name	cocculin
Generic	Picrotoxin
Picrotoxin Other Names	cocculin
Type
Formula	C30H34O13
Weight	Average: 602.5832 Monoisotopic: 602.199941174
Groups	Experimental
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Used internally for relieving respiratory distress. Also for use as an antidote in poisoning by CNS depressants, especially barbiturates.

How cocculin works

cocculin antagonizes the GABA_A 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. cocculin reduces conductance through the channel by reducing not only the opening frequency but also the mean open time. cocculin also antagonizes GABA_C receptors (also called GABA_A-rho receptors) but the result of this action is not known. The GABA_C receptor is also linked to chloride channels, with distinct physiological and pharmacological properties. In contrast to the fast and transient responses elicited from GABA_A receptors, GABA_C receptors mediate slow and sustained responses.

Toxicity

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.

Innovators Monograph

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