Tilorone

Overview

Brand names: Amixin IC, Amiksin IC (alternate machine-generated English translation), Lavomax

Tilorone is an over-the-counter drug that is widely used in Russia and Ukraine. It is included in the list of vital and essential medicines of the Russian Federation. While invented in the USA, it is not FDA approved and is not used in the Western world.

Tilorone has a track record of safe use in children and adults for ~20 years as both a prophylaxis and treatment for viral diseases. It has broad antiviral activity due to one or both of the following mechanisms:

• Inhibition of translation of virus-specific proteins in infected cells, thus inhibiting the reproduction of viruses.
• Induces the generation of Type I interferons.

Tilorone is water soluble, highly permeable, and is able to penetrate the blood-brain barrier. This suggests that it could access sites of the body where viruses might hide out. For a scientific review of this drug, please see the paper Tilorone: a Broad-Spectrum Antiviral Invented in the USA and Commercialized in Russia and beyond (https://www.ncbi.nlm.nih.gov/labs/pmc/articles/PMC7100484/).

Animal experiments suggest that tilorone can have antiviral effects without inducing interferon production (https://doi.org/10.3390/ph15050617).

Interferon overview

Interferons are part of the body's innate immune system. Whereas the adaptive immune system can retain a 'memory' of previous antigens that the body has seen (allowing for vaccines to 'train' the immune system), the innate immune system has broad anti-pathogenic action and has no memory mechanisms. Interferons (type I and II) are molecules produced by the body that seem to have an "interfering" effect with infectious pathogens, as demonstrated by in vitro studies where cells are grown without a functional adaptive immune system.

Western countries use interferon beta-1a based drugs such as Rebif (and the pegylated drug Plegridy) to treat multiple sclerosis. Pegylated interferon alpha-2a is used to hepatitis B and C. Pegylated interferon alpha-2b is used to treat melanoma (skin cancer) and was formerly used to treat hepatitis C.

Former Soviet bloc countries use low-cost interferon alpha-2a for cancer and a number of different infectious diseases. They also use interferon-inducing drugs such as tilorone and umifenovir (Arbidol) for many different conditions including infectious viral diseases.

Antibacterial action

In vitro, tilorone has an antibacterial effect against Borrelia Burgdorferi (https://doi.org/10.3390/antibiotics4030397).

Tilorone usages

According to a manufacturer's website (Interchem):

• Viral hepatitis A, B, C
• Herpes
• Cytomegalovirus infection
• Urogenital and respiratory chlamydia
• Treatment and prevention of influenza and acute respiratory viral infections.
• Neuroviral infections: infectious-allergic and viral encephalomyelitis (multiple sclerosis, panencephalitis, uveoencephalitis and meningoencephalitis).
• To counteract (or compensate for) the degree of immunosuppression in the 'complex therapy' of diseases that are accompanied by secondary induced immunodeficiencies and require immunocorrection

Potential other uses:

• HPV - "The experience of the drug in the treatment of this viral infection exists, but you should consult your doctor on this issue."
• Herpes - "Such experience exists and to determine the possibility of using the drug for the prevention of herpes you need to consult a doctor dermatovenereologist."
• Potential use for SARS-CoV-2 prophylaxis and treatment

Scientific papers

• Synergistic Suppression of the Hyperacute Form of Experimental Allergic Encephalomyelitis by Tilorone and Cycloleucine. - https://sci-hub.ru/10.3181/00379727-156-39956 - Tilorone and Cycloleucine had synergistic effects in delaying paralysis in rats with Experimental Allergic Encephalomyelitis (EAE), a model of autoimmunity and multiple sclerosis.
• Necrotic myelopathy (myelomalacia) in rats with allergic encephalomyelitis treated with tilorone - https://pubmed.ncbi.nlm.nih.gov/1082719 - Under selected conditions of dose and timing, tilorone delayed onset of clinical signs of encephalomyelitis, though the condition ultimately progressed to paralysis.
• Accelerated Mortality in Young NZB/NZW Mice Treated with the Interferon Inducer Tilorone Hydrochloride - https://deepblue.lib.umich.edu/bitstream/handle/2027.42/22849/0000410.pdf;sequence=1 - Tilorone accelerated mortality in young mice prone to developing autoimmunity as they age. However, the same effect was not seen in older mice.
• Effects of two pediatric vaccines on autoimmune diabetes in NOD female mice - https://sci-hub.ru/10.1016/j.toxlet.2003.09.005 - Tilorone hydrochloride and the DTaP-IPV vaccine both reduced the incidence of autoimmune diabetes. However, the study was underpowered to show statistical significance for the DTaP-IPV vaccine.

Side effects and safety information

• X Not for pregnant mothers and women who may become pregnant
• X Not for children under 7 years

In some cases are possible dyspeptic phenomena, short-term fever; in rare cases - allergic reactions such as skin rash, pruritus, urticaria. Contraindications for use of Amixin® ІC - is increased individual sensitivity to the drug, pregnancy and lactation, age under 7 years.

https://interchem.ua/en/faq#drug_26

• This medicine contains dyes that may cause allergic reactions.
• There is no experience with the use of the drug during pregnancy and breastfeeding, so it is contraindicated in these periods.
• Ability to influence the speed of reaction when driving a car or other machinery: Does not affect.

Adverse reactions

• From the skin and subcutaneous tissue: allergic reactions, including angioneurotic edema, rash (including urticaria), redness of the skin, dry skin, itching.
• From the gastrointestinal tract: bitterness in the mouth, dyspepsia (including epigastric pain, nausea, heartburn), diarrhea.
  • Dyspepsia = indigestion; refers to discomfort or pain that occurs in the upper abdomen (epigastric)
• General disorders: general weakness, lethargy, loss of appetite, short-term fever.

Other safety information

The inactive Twitter account __ice9 states:

Tilorone has also produced rare reports of progressive dose-dependent retinal and corneal toxicity in long-term use at ≥500mg/day in cancer patients, and similar findings in experimental animals at high doses. A mechanism similar to chloroquine retinopathy has been proposed. I was unable to locate further case reports of Tilorone retinopathy or corneal damage. Effects reversed on dose reduction. Indomethacin has a few similarly chloroquine-like reversible case reports as well. Some sources claim UV-exposure-triggered fluorescence may be involved.

Interchem instructions

Instructions: https://web.archive.org/web/20220530093137/https://interchem.ua/uploads/drugs/am%D1%96ksin_R_IC_%D1%96nstr_sait.pdf (archive.org)

Machine translated version: https://docs.google.com/document/d/1cwvkh0GPbPsL_r1_6sb9Ie2WEMuTxLmu1z2uSyvcJwc/edit?usp=sharing

PDF version of machine translation: https://www.longhaulwiki.com/resources/assets/am%D1%96ksin_translated.pdf

Method of application and dosage

Take orally after a meal.

Adults

• In the treatment of influenza and acute respiratory viral infections: in the first 2 days of treatment - 125 mg, then - 125 mg in 48 hours. Course dose - 750 mg. (Editor's note: the instructions imply that the dose should be repeated every 2 days until the cumulative dose is 750mg)
• For the prevention of influenza and acute respiratory viral infections: 125 mg once a week for 6 weeks.
• Treatment of viral hepatitis A: on the 1st day of treatment - 125 mg 2 times, then - 125 mg after 48 hours. Course dose - 1.25 g.
• Prevention of hepatitis A: 125 mg once a week for 6 weeks.

For a full list of application instructions, see the Interchem instructions.

Storage

Store in the original package at a temperature not exceeding 25 ° C. Keep out of reach of children.

Expiration date. 4 years.