Safer, Less Expensive, Than Aspirin? -- And Actually Therapeutic Against Covid-19? August 31, 2021

I've mentioned this drug on the blog some time ago but I've avoided the subject because I never understood how an anti-parasitic could "fight" a virus.

We're talking about Ivermectin.

So, after a year of avoiding talking about it, I finally looked up its "proposed" mechanism of action that allows it to fight the Covid-19 virus. 

Link here. This comes from our own NIH.gov. Published 2020.

Intro:

Ivermectin ... is a macrocyclic lactone with a broad-spectrum antiparasitic pharmacological activity.

It is the safest and most effective semi-synthetic derivative of the entire class of avermectins, discovered in 1975 by Professor Satoshi Ōmura as fermentation products of the actinomycete bacterium Streptomyces avermitilis ... 

Its main pharmacodynamics is to bind some channel proteins for chlorine controlled by glutamate, typical of specific classes of invertebrates, causing a greater permeability to this electrolyte: all this causes a hyperpolarization of the cell membrane, blocking inhibitory neurotransmission in neurons and myocytes, resulting in paralysis and death. 

Commercialized since 1981, its low cost, its high efficacy and safety, and the marked tropism for helminths (therefore with an almost zero impact on the biochemistry of human beings) have led to its inclusion in the twenty-first World Health Organization's List of Essential Medicines (World Health Organization 2019).

Then this:

Regarding its role as an antiviral agent, its efficacy has been demonstrated on several viruses, both in vitro and in vivo. 

Among the many mechanisms by which it performs its function, the most consolidated one sees ivermectin as an inhibitor of nuclear transport mediated by the importin α/β1 heterodimer, responsible for the translocation of various viral species proteins (HIV-1, SV40), indispensable for their replication. 

This inhibition appears to affect a considerable number of RNA viruses, such as Dengue Virus 1-4, West Nile Virus, Venezuelan Equine Encephalitis Virus, and Influenza. 

In addition, ivermectin has been shown to be effective against the Pseudorabies virus (PRV, with a DNA-based genome), both in vitro and in vivo, using the same mechanism. 

Caly [has] recently shown that the drug also inhibits the replication of the SARS-CoV-2 virus in vitro, however not clarifying how it occurs. 

Since the causative agent of COVID-19 is an RNA virus, it can be reasonably expected an interference with the same proteins and the same molecular processes described above. 

And, then:

However, ivermectin could prove to be a powerful antiviral, therefore also useful for a possible treatment of the new coronavirus associated syndrome, even from a new perspective. 

This could happen assuming its role as an ionophore agent, only hinted in the recent past but never fully described. 

Ionophores are molecules that typically have a hydrophilic pocket which constitutes a specific binding site for one or more ions (usually cations), while its external surface is hydrophobic, allowing the complex thus formed to cross the cell membranes, affecting the hydro-electrolyte balance. 

These chemical species have historically been used to study the mitochondrial respiratory chain and ATP synthesis in eukaryotes (in this case also known as decoupling agents, such as 2, 4-dinitrophenol), and their antibiotic activity has long been appreciated. It is also hypothesized their role as antiviral drugs and anticancer chemotherapeutic agents. Thinking of the structure of two of the most important ionophores, monensin A and valinomycin, respectively a polyether and a depsipeptide antibiotic, it is clear that they internally present many oxygen atoms (with related free electron doublets), indispensable for binding cations and transporting them through phospholipidic bilayers.

In Africa, this drug is given -- liberally -- to treat river blindness. 

From a reader:

So, here's why the case numbers are so low in that belt of Africa.  Guess what is widely distributed to treat river blindness.  And this chart is from the World Health Organization.

Numbers are from Johns Hopkins.

The audacity of "regulators" to force vaccination using EUA vaccines with less than one year's experience, while refusing to allow physicians to prescribe one of the safest drugs ever. And cheapest. To actually treat a deadly virus. 

How about a controlled study? Allow use of ivermectin in Florida but not in California.