Atebrine - General Information
An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2.
Pharmacology of Atebrine
Atebrine has been used as an antimalarial drug and as an antibiotic. It is used to treat giardiasis, a protozoal infection of the intestinal tract, and certain types of lupus erythematosus, an inflammatory disease that affects the joints, tendons, and other connective tissues and organs. Atebrine may be injected into the space surrounding the lungs to prevent reoccurrence of pneumothorax. The exact way in which quinacrine works is unknown. It appears to interfere with the parasite's metabolism.
Atebrine for patients
This medication is best taken after meals with a full glass of water, fruit juice, or tea, unless your doctor instructs otherwise. Tablets may be crushed and mixed with chocolate syrup, honey, or jam for persons who cannot stand the bitter taste or have difficulty swallowing tablets. If you miss a dose, take it as soon as you remember. If it is near the time for the next dose, skip the missed dose and resume your regular dosage schedule. Do not double the next dose. Take it as prescribed for the full treatment period, even if you feel better before the scheduled end of therapy.
Alcohol (this combination may make you very sick) and primaquine
A history of mental illness or alcoholism, porphyria, or psoriasis.
Additional information about Atebrine
Atebrine Indication: For the treatment of giardiasis and cutaneous leishmaniasis and the management of malignant effusions.
Mechanism Of Action: The exact mechanism of antiparasitic action is unknown; however, quinacrine binds to deoxyribonucleic acid (DNA) in vitro by intercalation between adjacent base pairs, inhibiting transcription and translation to ribonucleic acid (RNA). Atebrine does not appear to localize to the nucleus of Giaridia trophozoites, suggesting that DNA binding may not be the primary mechanism of its antimicrobial action. Fluorescence studies using Giardia suggest that the outer membranes may be involved. Atebrine inhibits succinate oxidation and interferes with electron transport. In addition, by binding to nucleoproteins, quinacrine suppress the lupus erythematous cell factor and acts as a strong inhibitor of cholinesterase.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Quinacrine
Synonyms: Quinacrine Dihydrochloride
Drug Category: Antihelmintics; Antiprotozoals; Antineoplastic Agents; Antinematodal Agents; Antimalarials; Anticestodal Agents; Enzyme Inhibitors
Drug Type: Small Molecule; Approved
Absorption: Absorbed rapidly from the gastrointestinal tract following oral administration.
Toxicity (Overdose): Oral, rat: LD50 = 900 mg/kg; Oral, mouse: LD50 = 1000 mg/kg. Symptoms of overdose include seizures, hypotension, cardiac arrhythmias, and cardiovascular collapse.
Protein Binding: 80-90%
Biotransformation: Not Available
Half Life: 5 to 14 days
Dosage Forms of Atebrine: Not Available
Chemical IUPAC Name: N'-(6-chloro-2-methoxyacridin-9-yl)-N,N-diethylpentane-1,4-diamine
Chemical Formula: C23H30ClN3O
Quinacrine on Wikipedia: https://en.wikipedia.org/wiki/Quinacrine
Organisms Affected: Parasitic protozoa and helminths