Antihistamines and Mast Cell Stabilizers

How Well Do Antihistamines and Mast Cell
Stabilizers Help with COVID-19?

With severe COVID-19 courses there is an overreaction of the immune system with an uncontrolled over production of inflammation mediators, a so called cytokine storm.^[1] At the same time mast cells play a central role. Mast cells belong to the white blood cells and are of particular importance for non-specific immune defence.

Mast cells become active as a reaction to contact with disease-causing agents like viruses, bacteria or parasites as well as allergens. They are found distributed throughout the whole body in the connective tissue, most often in the submucosa of the intestine and respiratory tract.

The multifunctional immune cells help to fight against an infection by releasing various different materials like inflammation mediators, cytokines and histamines and coordinate the immune defence. Exactly these materials play a central role with COVID-19, COVID Pneumonia and Long-COVID. The activation of mast cells is decisively responsible for this.

It is difficult to control hyperactive mast cell reactions. In addition to vital substances like for example Vitamin C, D, K2, Quercetin or Boswellia, antihistamines promise relief with COVID-19 and Long-COVID.

The Clinical Studies

Reduction of the Need for Oxygen Therapy by 93% with Quercetin

As a natural mast cell stabilizer the plant substance quercetin is especially interesting. Quercetin stabilizes the mast cells and thus inhibits the release of histamines, cytokines and interleukins. Quercetin has been known for a long time as a highly effective plant substance, whose application clinically was so far only a little successful due to poor bioavailability.

The first clinical studies of quercetin with improved bioavailability showed impressive results against COVID-19: One study examined the influence of quercetin-phospholipid on the illness course for COVID-19. 76 patients received quercetin for 30 days in the early stages of the illness in addition to the standard therapy (2 times 200 mg per day as quercetin-phospholipid), another 76 patients were treated without quercetin. In the quercetin group the probability of hospitalization was reduced by 68%, the duration of the hospitalization by an average of 77% and the frequency of oxygen therapy by 93%. In the control group 8 patients required an intensive care treatment of which 3 passed away. In the quercetin group no intensive care treatment was necessary and there were no deaths.^[2]

Strong Reduction of Risk of Intubation and Mortality with Antihistamines

The combination of Cetirizine [Zyrtec] and Famotidine has already been proven in a cohort study sponsored by physicians themselves in the USA with patients with severe to critical pulmonary symptoms. In comparison to the average illness statistics of COVID-19 patients, the combination showed a clear reduction of the mortality and symptom progression. While the average hospitalization was normally 18 days in the hospital, 41.7% of patients had to be intubated and all intubated died. It was 11 days for the treated patients; only 16.4% had to be intubated and only 7.3% died.

It is often overestimated what intensive care medicine can still do for a patient if he is first of all intubated and artificially respirated. Therefore this is a small but substantial study because the treatment with both antihistamines had no side effects but very clear results. The evaluation of the accompanying medications showed that hydroxychloroquine still led to negative results. The authors see in cetirizine combined with famotidine a safe and effective method to moderate the progression of the symptom severity and the illness course, presumably by minimizing the histamine-produced cytokine storm.^[3]

Desloratadine [Clarinex/Aerius] is a better option than cetirizine because it not only blocks the H1 Receptor but additionally stabilizes the mast cells which disburse not only histamine but also other inflammatory materials. Moreover, desloratadine binds to the ACE2 receptor blocking with it the interaction of the spike proteins with the ACE2 and thus can prevent the penetration of the virus into the cells.^[4] Famotidine is an H2 histamine receptor blocker. Especially before the second vaccination with an mRNA vaccine desloratadine, cetirizine and famotidine are also meaningful because they can reduce the vaccine reaction. Other side-effect-rich vaccines should better be avoided or already accompanied by mast cell stabilizing with the first vaccination.

The Medical Background

Damage from Hyperactive Mast Cells

The SARS-CoV-2 Virus frequently activates the mast cells to an extent that leads to an excessive antiviral immune reaction and the development of a cytokine storm. With the cytokine storm it becomes a cascade of stronger and stronger immune reactions that exhaust the immune system which can lead finally to organ failure and fatal respiratory distress.^[5] It can already be proven that mast cells in patients with COVID-19 are increasingly activated – dependent on the severity of the disease.^[6] Autopsy of patients who died of COVID-19 identified an accumulation of mast cells in the lung.^[5]

Similar Symptoms in MCAS and COVID-19

In Mast Cell Activation Syndrome (MCAS) the mast cells are “hyperactive” and release too much histamine and other messenger materials. MCAS is a chronic multi-system illness with inflammatory and allergic components. The mast cells are activated by IgE and cytokines, but also by environmental factors (i.e. heat, cold), allergens, food, infections, certain medications, drugs and physical or psychic stress.^[7] The symptoms are non-specific and especially affect the skin, the gastrointestinal tract, the cardiovascular system, the respiratory tract and the neurological system; among other things low blood pressure, rapid pulse (tachycardia), diarrhea, abdominal cramps, nausea, redness of the skin, itching, hives, angioedema, nasal congestion and headaches.^{[8, 9]} The symptoms also let us think about a histamine intolerance (HIT). Indeed, in most cases an HIT is actually a Mast Cell Activation Syndrome with increased formation of histamine by the mast cells. Many of the symptoms with MCAS are similar to those of an acute COVID-19 infection and/or Long-COVID, as is the severe inflammatory reaction which can be released by a mast cell activation.

Diagnosis and Treatment of MCAS

On the basis of the varied symptoms the diagnosis of MCAS is very difficult. Often affected patients go through a many-years to decades-long doctor’s marathon until someday – hopefully – they receive the correct diagnosis. However the clinical picture is not known by many doctors at all. Only in 2016 was an ICD-10-Code assigned for Mast Cell Activation disturbances. MCAS is widespread in 17% of the population in Germany.^[10] Due to the difficult and partially restrictive diagnosis MCAS is greatly underdiagnosed. Therefore the spread and importance of MCAS in the population is also not known to most doctors. MCAS can clearly be improved and the symptoms relieved. Eliminating the triggers – the viruses, bacteria, stress, certain foods including hot or cold irritation – is the first and most important step. Additionally this occurs especially through stabilization of the mast cells (mast cell stabilizers) and inhibition of the histamine effect (antihistamines). For this there are various medications, plant materials, vitamins and other micronutrients which provide considerable improvement and clearly improve the quality of life. The prevalence numbers of MCAS of 17% correspond very closely with the estimates of the prevalence of a severe illness course of COVID-19. The hyperinflammatory cytokine storm with severe COVID cases could form the basis of a dysfunctional reaction of mast cells within the scope of an MCAS in many cases, and not the normal reaction of mast cells. MCAS is therefore a prognostic factor which makes a severe COVID-19 illness course as well as Long-COVID probable. The people who have an increased mast cell activation (allergies, intolerances, auto-immune illnesses) or histamine intolerance, must generally expect a severe COVID-19 illness course. However this is an individual and specific reaction to the spike protein of the virus. As a rule here, men react stronger than women. Surprisingly women with MCAS often do not react violently to the spike protein. The reason for this could be that the spike protein directly triggers MCAS and thus can also lead to Long-COVID courses.

Treatment of Mast Cell Reaction with (Long-)COVID and the Vaccination

Severe COVID-19 illness courses, Long-COVID and vaccination reactions are based above all on an overreaction of the mast cells. Medications against the function of the mast cells or their mediators have already proven helpful with COVID-19 and could be of great benefit for treatment.^{[5, 11]} Antiallergic medications (Ketotifen), antibiotics (Clarithromycin) and especially corticosteroids (Hydrocortisone, Dexamethasone) have studies proving them to be highly effective mast cell stabilizers.^[12] For the moment dexamethasone has been established as the most effective medication for COVID-19 but unfortunately has the strongest side effects. Just like Long-COVID, vaccination reactions are often also based on a mast cell activation syndrome. Anyone who reacts with strong side effects to the vaccination, in case of an illness with COVID-19 would have presumably suffered a very severe illness course. With the correct measures the mast cells can be kept in check and the vaccination side effects as well as Long-COVID symptoms are clearly reduced.

Treatment for Stabilization

The listed plant materials, vitamins and mineral substances can provide considerable improvement, especially with severe COVID-19 courses further mediations are added.

Mast Cell Stabilizing and Anti-Histamines

• Vitamin D3 and K2
• Quercetin(-phospholipid)
• Vitamin C

Anti-Inflammatory

• Boswellia
• Curcumin
• Dexamethasone (only on doctor’s instructions and at a later stage in severe COVID-19 cases)

Anti-Histamine

Desloratadine, famotidine, cetirizine, cinnarizine.
Especially before the second vaccination with an mRNA-vaccine desloratadine, cetirizine, famotidine and cinnarizine are meaningful because they reduce the vaccine reaction.

Result

MCAS and its under-noticed role with COVID-19 and many other chronic conditions is an important example of how necessary and helpful integrative, holistic medicine is.

Keywords: COVID-19, MCAS, prevention, vaccination, mast cells, allergy

An Exclusive Translated Article for P2P Supporters
From the Monthly Publications of P2P
Published September 2022

From an article in Der Heilpraktiker, Volume 89, Nr. January 2022
Machine Translation by SYSTRAN, Lernout & Hauspie, LogoMedia & Promt
Translation & redaction by: Carolyn L. Winsor, P2P Consulting

© Copyright 2022, Der Heilpraktiker, Dr.med. Ludwig Manfred Jacob, Ingelheim, Germany

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