MICRODOSING: PREPARATION, MECHANISMS OF ACTION, SOME CLINICAL TRIALS - MEDICINE - 2025

The microdose is a way to administer drugs using a dilution concentrations are obtained 1000 15000 times less than those supplied with the "allopathic" normal dose. Once the dilution has been made, two or three drops are administered on the back of the tongue with the same periodicity as the dose normally indicated for said medicine.

Also considered “microdoses” are the doses of those drugs such as hormones, some poisons or toxins whose effects are achieved with doses in the range of micrograms or less. This article refers to the use of microdosing as an alternative treatment.

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Microdoses are used to administer drugs of various origins and thereby obtain the same therapeutic effect as with the full dose. Being such a low concentration, it apparently produces fewer side effects and less toxicity.

The microdosing technique was described and promoted by Eugenio Martínez Bravo (1922-2002), a Mexican doctor who cared for inmates in a prison. In one of his consultations, three inmates took him because they had trouble sleeping for several days.

While attending to his patients, he realized that he only had a mild sedative for pediatric use that would not even serve to treat one of the inmates. As Dr. Martínez came from a family of homeopathic doctors, it occurred to him to dilute the medicine with water and administer two drops on the tongue to each inmate.

To their surprise, the three inmates were able to fall asleep and slept peacefully until the next day. As a result of this experience, Dr. Martínez began to investigate and carry out various trials and promote the use of microdoses.

Currently, microdose treatment has attracted the attention of many researchers in the world due to its apparent effectiveness in treating acute and chronic diseases, due to the low incidence of collateral and toxic effects, and due to the low costs in terms of public health.

Preparation of the microdose

The preparation of a microdose is based on an alcoholic solution to preserve the drug. This is done as long as there is no known interaction between alcohol and the drug, or the patient is alcoholic or does not want to drink alcohol for any reason. In these cases it can be replaced by a sugary solution or a dilution with honey.

Two amber containers are used to protect it from light. The containers must have a capacity of 20 ml, fill two-thirds of each container with an alcoholic beverage (drinkable alcohol or cane alcohol, pomace, etc.) or with high-grade drinkable alcohol and complete with water.

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The dose of the medicine corresponding to 24 hours is diluted in one of the bottles, if it is a tablet it must be crushed first. It mixes really well. Then twelve drops of this mixture are taken, placed in the second bottle and mixed well. The two jars are labeled and stored in a cool, dry place, protected from light.

The first bottle corresponds to the stock solution. The second bottle corresponds to the therapeutic solution.

Two drops are taken from the second bottle, placed on the back of the tongue and administered as often as prescribed by the doctor for treatment with the normal dose or more frequently if necessary. It should always be administered under medical supervision.

Action mechanisms

The mechanisms of action proposed by Dr. Martínez, in the opinion of some experts, have no scientific basis.

According to Dr. Martínez, the medicine contained in the drops stimulates local sensory endings that send information to the hypothalamus and from there to the cerebral cortex, to then exert its effect on the drug's sites of action.

An effect of this nature would be similar for all drugs and what has been observed is that the drugs tested have the expected pharmacological effect, what cannot be explained is why such an effect is achieved with such a low dose.

Microdose treatments do not have new routes of administration, they use those described by pharmacology for different drugs, the interesting thing is that the effect is somehow enhanced, but how it occurs is not yet explained.

Some clinical trials

Some clinical trials have been published for the use of microdoses of some known drugs for specific pathologies. A summary of some of them is presented below as examples of the effect of microdosing in the treatment of certain diseases.

- Microdosing of “captopril” for hypertensive patients

Santana Téllez et al. Published in 2012 a clinical trial conducted with 268 patients with a diagnosis of essential arterial hypertension and who had been treated with an angiotensin-converting enzyme (ACE) inhibitor, captopril.

The trial was done replacing the usual treatment of patients by microdosing captopril. These microdoses were prepared and controlled by the pharmacy laboratory of the "Manuel Ascunce Domenech" University Hospital, Camagüey, Cuba.

The patients were classified and dosed according to the age group, the degree of arterial hypertension and the cardiovascular risk group.

The results of the trial showed a clinical control of the blood pressure levels of the patients treated with captopril microdose of 84.7%, while in those who were treated with oral tablets (control group) it was 64.2%.

In this case, the clinical response with microdosing was better than that of conventional treatment, regardless of the age of the patients.

- Microdose of "dipyrone"

In 2008, Bello et al. Published a clinical trial with 55 patients suffering from pain (pain) of different etiologies. These authors microdosed dipyrone (an analgesic) at the rate of 3 drops on the tongue, 3 times a day, for four days.

The authors reported "satisfactory" responses to treatment, but they were not quantified.

- Microdose of "phenobarbital"

Guilarte and Zúñiga did a trial with 40 healthy volunteers: 10 treated with water, 10 treated with the hydroalcoholic vehicle, 10 with ampoule phenobarbital, and 10 with phenobarbital microdoses.

The investigators found that patients who received phenobarbital microdoses experienced drowsiness within 5 minutes of placement of the tongue doses and the EEG variations were more noticeable than in the other groups.

Although there are some controlled clinical trials, many of the existing reports in the literature are qualitative trials without rigorous controls, so more studies are necessary to rate the efficacy of this technique of pharmacological administration.

References

1. Aleksandrovich, TA, & Ivanovna, GM (2015). Protective action of essential oils in case of animal irradiation and possible appliance for human. Бюллетень Государственного Никитского ботанического сада, (114 (англ.)).
2. Bello, ET, Rodríguez, AV, Morillo, EC, & Sotolongo, ZG (2008). Dipyrone microdose. A new pharmaceutical proposal. Electronic Medical Journal, 30 (1), 53-59.
3. Gonzáles Delgado, JB (2002). Experiences and results with the use of steroid microdoses in the treatment of bronchial asthma. Mexico: Herbal.
4. Santana Téllez, TN (2013). Microdosing: reflections on a mechanism of action. Camagüey Medical Archive Magazine, 17 (3), 261-263.
5. Santana Téllez, TN, Monteagudo Canto, A., Del Águila Grandez, AY, & Vázquez Gamboa, A. (2012). Efficacy of captopril microdosing in the treatment of essential arterial hypertension. Cuban Journal of Medicine, 51 (3), 247-257.
6. Suárez Rodríguez, B., Rivas Suárez, S., & Oramas, O. (2001). Results of treatment with microdoses of naproxen in rheumatic patients. Cuban Journal of Rheumatology, 3 (2).