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Chloroquine and Hydroschloroquine for Covid-19 patients

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Oleh
The mechanism of action of chloroquine in the Covid-19 treatment :
  • Inhibits the entry of the virus into host cells by increasing endosomal PH.
  • Disrupting virus particles to bind to their receptors on the cell surface.
  • Reducing the expression of ACE2 receptors (ACE2 receptors are the place of viruses when they enter the body).
  • Chloroquine has been shown to inhibit in vitro replication of several Corona viruses.
  • Chloroquine can improve the clinical picture of patients infected with SARS-Cov-2.

So, China recommends patients diagnosed with Covid-19 to be treated with chloroquine phosphate.

Expert consensus published in February 2020 from Guangdong province, China :
recommend chloroquine phosphate tablets 500 mg, 2 × daily, for 10 days (for patients diagnosed with mild, moderate, or severe SARS-Cov-2 pneumonia) provided there are no contraindications to the drug.

Suggest the use of chloroquine for Covid-19 patients who require hospital treatment with a base dose of chloroquine :
The first day 600 mg ➡ after the first dose, the patient was again given 300 mg base chloroquine (12 hours after the first dose).
The second to fifth days were given basic chloroquine at a dose of 2 × 300 mg/day.

Chloroquine side effects :
  • Cardio Toxicity.
  • Arrhythmia.
  • Vision loss.
  • Death of the patient after being given chloroquine.
Patients receiving chloroquine therapy need to be monitored :
  • Investigations to monitor for anemia, thrombocytopenia, disruption of serum electrolytes, liver and kidney dysfunction.
  • ECG examination to monitor the extension of the QT interval (bradycardia).
  • Perform a thorough history to analyze the potential for visual retinopathy disorders.
  • In patients with G6PD (Glucose-6-phosphate-dehydrogenase) deficiency, chloroquine can cause erythrocyte hemolysis, causing hemolytic anemia.
Hydroschloroquine.
A study was conducted to look at the potential of hydroschloroquine as an alternative to chloroquine for the treatment of Covid-19 or as an anti-virus SARS-Cov-2. Hydroschloroquine is an analogue of chloroquine with a better safety profile.

In vitro research ➡
  • Hydroschloroquine can inhibit the virus from entering the host cell and is more potent (EC50 = 0.72% μm) than chloroquine (EC50 = 5.47% μm) as anti SARS-Cov-2 by using the effective parameter concentration 50.
  • Human studies have shown that hydroschloroquine is three times more potent than chloroquine, so that the effective dose needed is also less.
Hydroschlorokuin is given to Covid-19 patients with : initial dose 400 mg, 2 × daily ➡ followed by 200 mg, 2 × daily for 4 days.

Preliminary (open label, non-randomized) clinical trial in France for Covid-19 patients : comparing Hydrosychlorokuin Sulfate therapy with a dose of 3 × 200 mg given for 10 days, with supportive therapy. The result is a different group of viruses in patients receiving Hydroschlorokuin therapy.

Parameters :
  • PCR examination of the virus from the airway swab (negative on the 6th day) compared with a group of patients who only received supportive therapy.
  • The mechanism of action of Hydroschlorokuin in Covid-19 patients is thought to be similar to Chloroquine.
Hydroschlorokuin side effects :

  • Retinal damage.
  • Heart disorders (prolongation of the QT interval).
  • Hemolytic anemia in patients with G6PD deficiency.
  • Patients who experience hepatoctocic or nephrotoxic symptoms need evaluation for administration of Hydroschlorokuin.
Conclusion.

  • The characteristics of chloroquine and hydroschloroquine are already known as anti-malaria, but evidence of the efficacy and safety of the use of these two drugs is still limited.
  • Various clinical trials for Hydroschlorokuin for the treatment of Covid-19 are still ongoing throughout the world.
  • There is no effective drug (definitive therapy) for Covid-19. The therapy currently given to patients is only based on observations and experiences in other countries.
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