Introduction to Chloroquine

Chloroquine was discovered in 1934 by Hans Andersag [3]. It is an analogue of quinine, which is extracted from the bark of Cinchona officinalis and was the first antimalarial drug known to humans. It is on the World Health Organisation list of essential medications [4], but is considered mostly obsolete as an antimalarial due to widespread resistance. While it has been promoted by some public figures for its potential in treating coronavirus including COVID-19, research has not yet been completed to confirm its efficacy for this indication. Clinical trials are needed to establish this as effective [5]. Self administered Chloroquine phosphate from aquarium cleaning products in an attempt to self-medicate for COVID-19 have led to at least one fatality [6].

Using Chloroquine

Ways of Administration

Administration is primarily oral. Oral formulations are available as phosphate, sulfate and hydrochloride salts [7].

Effects of Chloroquine

While chloroquine might be considered psychoactive, it has no desirable effects and no recreational value. Psychoactive side effects include delirium, personality changes, paranoia, and suicidal ideation. Chloroquine's wide distribution throughout the body and tendency to accumulate in a variety of tissues contributes to its long list of side effects. Its effects on the brain also include seizures as well as extrapyramidal symptoms such as dystonia and torticollis. Chloroquine also accumulates in the eyes, where it can cause irreversible retinopathy and blindness, and in the heart, where it interferes with conduction, causing a variety of arrythmias, AV block, EKG changes, ventricular tachycardia, and ventricular fibrillation. Other particularly heinous effects include deafness, pancytopenia, hepatitis, and severe hypoglycemia resulting in coma.

Chemistry of Chloroquine

The Dangers of Chloroquine

Chloroquine is noted for having a very small therapeutic index. That is to say that the difference in dosage between what is effective for its therapeutic indications and what may cause dangerous and potentially fatal side effects is small. Because of the risk of accidental death drugs-forum strongly recommends that Chloroquine should only be administered under medical supervision.

Symptoms of overdose include headache, nausea, vomiting, seizures, and sudden respiratory and cardiac arrest and individuals experiencing overdose can expect to experience considerable discomfit.

Due to the suggestion of its potential for efficacy in treating COVID-19 users have attempted self-administration of Chloroquine, leading to several incidents of accidental overdose and at least one fatality .
[8][9].

References

1. ^Aralen Phosphate". The American Society of Health-System Pharmacists. Archived from the original on 8 December 2015. Retrieved 2 December 2015.
2. ^Wang, M., Cao, R., Zhang, L. et al. (2020) "Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro". Cell Research, 30, 269–271. Retrieved 25 March 2020. https://doi.org/10.1038/s41422-020-0282-0
3. ^Manson P, Cooke G, Zumla A, eds. (2009). Manson's tropical diseases (22nd ed.). [Edinburgh]: Saunders. p. 1240. ISBN 978-1-4160-4470-3. Archived from the original on 2 November 2018. Retrieved 9 September 2017
4. ^https://www.who.int/medicines/publications/essentialmedicines/en/
5. ^"Could an old malaria drug help fight the new coronavirus?". asbmb.org. Archived from the original on 6 February 2020. Retrieved 6 February 2020
6. ^https://www.nytimes.com/2020/03/24/us/chloroquine-poisoning-coronavirus.html
7. ^"Chloroquine". nih.gov. National Institutes of Health. Retrieved 24 March 2020
8. ^https://edition.cnn.com/2020/03/23/africa/chloroquine-trump-nigeria-intl/index.html
9. ^https://www.nytimes.com/2020/03/24/us/chloroquine-poisoning-coronavirus.html