Chloroquine and Hydroschloroquine for Covid-19 patients

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.