Instructions for Tesalin tablets No. 20
Composition
active ingredient: native extract from the leaves of hybrid flint (P. hybridus);
1 tablet contains 17.8–40 mg of native extract from the leaves of P. hybridus (extractant — carbon dioxide), which corresponds to 8 mg of petasins;
Excipients: colloidal anhydrous silicon dioxide, microcrystalline cellulose, magnesium stearate, sodium starch glycolate (type A), stearic acid, hypromellose, titanium dioxide (E 171), macrogol 20,000.
Dosage form
Film-coated tablets.
Main physicochemical properties: round, biconvex tablets, film-coated, white to cream in color.
Pharmacotherapeutic group
Agents acting on the respiratory system. Other agents acting on the respiratory system.
ATX code R07AX.
Pharmacological properties
Pharmacodynamics.
Tesalin is an antiallergic and anti-inflammatory drug for the treatment of allergic rhinitis. Tesalin inhibits the biosynthesis of leukotrienes and the degranulation of neutrophils and eosinophil granulocytes.
In a randomized, double-blind, placebo-controlled study involving 18 patients with allergic rhinitis caused by grass pollen, the pharmacodynamic properties of Tesalin were investigated by comparing the symptoms of allergic rhinitis with changes in the amount of inflammatory mediators. During the studies, a significant reduction in the symptoms of allergic rhinitis, including a faster elimination of nasal congestion after exposure to grass pollen, was observed when treated with Tesalin compared to placebo and desloratadine. During 5 days of treatment, Tesalin showed significant inhibition of the inflammatory mediators leukotriene B4 (6-fold and 5-fold) and interleukin-8 (6-fold) in the nasal secretions of patients compared to desloratadine and placebo. There is no evidence of systemic immunosuppressive effects.
Pharmacokinetics.
Absorption
No relevant studies have been conducted.
Distribution
The data below refer to petasin, but no conclusions can be drawn regarding the distribution of the total extract.
Maximum plasma petasin concentrations (Cmax) were reached after approximately 1.6 hours (tmax) regardless of dose. Maximum plasma petasin concentrations were 25.5 ± 14.8 ng/mL after 2 tablets and 58.1 ± 26.7 ng/mL after 4 tablets.
The AUC (area under the pharmacokinetic concentration-time curve) was proportional to the dose and was 65.3 ± 35.6 ng/mL×h after the use of 2 tablets and 151.2 ± 68.2 ng/mL×h after the use of 4 tablets.
Metabolism
No relevant studies have been conducted.
Breeding
The half-life of petasin is 7.2 ± 4.6 h (2 tablets) and 7.6 ± 3.3 h (4 tablets).
Due to the half-life of approximately 7 hours, there is no accumulation. The dosage regimen (1 tablet two or three times a day) can be adapted for patients according to their needs.
Indication
For the treatment of symptoms associated with allergic rhinitis (hay fever).
Contraindication
Hypersensitivity to the active substance or to any of the excipients, as well as to any plants of the Asteraceae/Compositae family.
Liver and kidney dysfunction.
Contraindicated in patients receiving anticoagulant therapy or barbiturates.
Pregnancy and breastfeeding.
Interaction with other medicinal products and other types of interactions
Interactions with other drugs, as well as with foods or stimulants (such as coffee, tea) are not known.
In vitro pharmacological studies have shown that the use of the extract from the leaves of the hybrid flint does not cause the expression of the MDR1 and CYP3A4 genes. In addition, the activity of liver enzymes remains unchanged, i.e. is not stimulated or inhibited. The following enzymes were tested: CYP2E1, CYP1A2, CYP2D6, CYP2C19, CYP3A4 and CYP2C9. According to the results of these studies, interactions with other drugs are not expected.
Application features
In very rare cases, severe liver damage has been observed (see section "Adverse reactions") in connection with the use of medicinal products containing extract from the roots of P. hybridus. However, the possibility of liver damage due to the extract from the leaves of P. hybridus contained in the medicinal product Tesalin cannot be excluded. During treatment, doctors and patients should pay attention to early signs of liver damage (upper abdominal pain, loss of appetite, jaundice, yellowing of the sclera, etc.).
There are currently no clinical trial results in patients with reduced liver or kidney function. Therefore, the drug is contraindicated in these patients.
This medicinal product contains less than 1 mmol (23 mg) sodium per dose, i.e. essentially 'sodium-free'.
Use during pregnancy or breastfeeding
There are no clinical data on the use of the drug during pregnancy and breastfeeding.
Use during pregnancy and breastfeeding is contraindicated.
Ability to influence reaction speed when driving vehicles or other mechanisms
If dizziness and fatigue occur during treatment with the drug, you should refrain from driving or operating other mechanisms.
Method of administration and doses
For oral use.
The usual daily dose for adults is 2 film-coated tablets: take 1 tablet in the morning and 1 tablet in the evening. In case of external exposure to a large amount of pollen, the dose can be increased if necessary: 1 tablet 3 times a day. The tablet should be swallowed without chewing and washed down with water. The tablets are taken regardless of the time of day and food intake.
Duration of use
The duration of use depends on the progression of the disease or the duration of exposure to the allergen and is determined by the doctor, but should not exceed 14 days. If symptoms persist during this period, you should stop using the drug and consult a doctor.
Children.
The medicine is not used in children (under 18 years of age).
Overdose
No acute poisoning with the drug Tesalin was detected.
Side effects
The frequency of adverse reactions is defined as follows:
Very common: ≥ 1/10
Common: ≥ 1/100 to < 1/10
Uncommon: ≥ 1/1000 to < 1/100
Rare: ≥ 1/10,000 to < 1/1,000
Very rare: < 1/10,000
Unknown: cannot be estimated from the given data
From the digestive tract
Common: gastrointestinal discomfort (including nausea, abdominal pain/stomach ache, diarrhea).
Skin and subcutaneous tissue disorders
Uncommon: hypersensitivity skin reactions including erythema, oedema, pruritus, eczema, urticaria, rash.
Liver and biliary tract disorders
Very rarely, severe liver damage (liver necrosis, liver cell damage, hepatitis, liver failure, early signs of which may be fatigue, dark urine, discolouration of stools, upper abdominal pain, loss of appetite, jaundice, yellowing of the sclera) has been observed in association with the use of medicinal products containing P. hybridus root extract. The possibility of liver damage due to the action of P. hybridus leaf extract contained in Tesalin cannot be excluded.
From the nervous system
Very rare: fatigue, dizziness, headache, lethargy.
On the part of the immune system
Not known: hypersensitivity reactions.
Reporting of suspected adverse reactions
It is important to report suspected adverse reactions after the registration of a medicinal product. This allows for continuous monitoring of the benefit-risk balance associated with the use of the medicinal product. Healthcare professionals should report any suspected adverse reactions via the Automated Pharmacovigilance Information System at: https://aisf.dec.gov.ua.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 °C in the original packaging. Keep out of the reach of children.
Packaging
10 tablets in a blister; 2 or 6 blisters in a cardboard box.
Vacation category
Without a prescription.
Producer
Max Zeller Söhne AG.
Max Zeller Sohne AG.
Location of the manufacturer and address of its place of business.
Seeblickstrasse 4, 8590 Romanshorn, Switzerland.
Seeblickstrasse 4, 8590 Romanshorn, Switzerland.
Applicant
Amaxa Ltd.
Amaxa Ltd.
Location of the applicant.
31 John Islip Street, London SW1P 4FE, United Kingdom.
31 John Islip Street, London SW1P 4FE, United Kingdom.
