TIONA [Thioctic acid] Tablets
instructions for the medical use of
the medicinal product
TIONA
Tradename: Tiona
International non-proprietary name
or generic name: thioctic acid
Dosage form: film-coated tablets.
Composition
for 1 tablet:
active
substance: thioctic acid 600 mg.
excipients: starch, microcrystalline cellulose, dextrin, sodium
starch glycolate, PVP-K30, silicon dioxide, talc, magnesium stearate.
Pharmacotherapeutic
group: Metabolic agent.
ATX
code: A16AX01
Pharmacological properties
Pharmacodynamics
It
is an endogenous antioxidant that binds free radicals. Thioctic acid is
involved in the mitochondrial metabolism of the cell; it functions as a
coenzyme in the complex of transformation of substances that have a pronounced
antitoxic effect. They protect the cell from reactive radicals arising during
intermediate metabolism or during the breakdown of exogenous foreign
substances, and from heavy metals. Thioctic acid exhibits synergism with
insulin, which is associated with increased glucose utilization. In patients
with diabetes mellitus, thioctic acid leads to a change in the concentration of
pyruvic acid in the blood.
Pharmacokinetics
When
taken orally, it is quickly and completely absorbed from the gastrointestinal
tract. Cmax is reached 30 minutes after administration and is 4 mcg/ml.
With
intravenous administration of thioctic acid at a dose of 600 mg, Cmax in blood
plasma after 30 minutes is about 20 mcg/ml.
Thioctic
acid has a “first pass” effect through the liver. The formation of metabolites
occurs as a result of side chain oxidation and conjugation. Vd - about 450
ml/kg.
Thioctic
acid and its metabolites are excreted by the kidneys mainly in the form of
metabolites (80-90%), in small quantities - unchanged. T1/2 is 25 min. Total
plasma clearance is 10-15 ml/min/kg.
Indications for use
• Diabetic
polyneuropathy.
• Alcoholic
polyneuropathy.
Contraindications
• Hypersensitivity to
thioctic acid or to any other component of the drug.
• Pregnancy.
• Breastfeeding
period.
• Children and
adolescents up to 18 years of age.
Method of administration
and dosage
Orally,
without chewing, with a sufficient amount of water, 30 minutes before the first
meal (on an empty stomach), 1 tablet 1 time per day. The recommended dose is
600 mg/day.
The
duration of treatment is determined individually, depending on the severity of
the disease.
Side effect
From the nervous system: dizziness, change or
disturbance of taste, hot flashes, convulsions.
From the digestive system: nausea, vomiting,
abdominal pain, diarrhea.
From the organ of vision: diplopia.
From the immune system: allergic reactions
(skin rash, eczema, urticaria, itching), anaphylactic shock, autoimmune insulin
syndrome in patients with diabetes, which is characterized by frequent
hypoglycemia in the presence of autoantibodies to insulin.
Metabolic: hypoglycemia (due to
improved absorption of glucose), symptoms of which include dizziness, increased
sweating, headache and blurred vision.
If any of the side effects indicated in the
instructions get worse, or you notice any other side effects not listed in the
instructions, tell your doctor.
Interaction with
other medicinal products
With
simultaneous use of thioctic acid and cisplatin, a decrease in the
effectiveness of cisplatin is observed.
Thioctic
acid is capable of forming chelate complexes with metals; co-administration
with iron, magnesium, and calcium preparations should be avoided. Keep in mind
that dairy products contain calcium. Therefore, it is also necessary to avoid
using thioctic acid simultaneously with dairy products (due to their calcium
content).
With
simultaneous use of thioctic acid and insulin or oral hypoglycemic drugs, their
effect may be enhanced, therefore regular monitoring of blood glucose levels is
recommended, especially at the beginning of therapy with thioctic acid. In some
cases, it is permissible to reduce the dose of hypoglycemic drugs to avoid the
development of symptoms of hypoglycemia.
Thioctic
acid enhances the anti-inflammatory effect of GCS.
Ethanol
and its metabolites weaken the effect of thioctic acid.
Thioctic
acid forms poorly soluble complex compounds with sugar molecules. Thioctic acid
is incompatible with solutions of dextrose (glucose), fructose, Ringer, as well
as with solutions that react with disulfide or SH groups.
Special instructions and precautions
Before using the drug,
consult your doctor.
For severe diabetic polyneuropathy, it is
recommended to begin treatment with parenteral administration of thioctic acid
for 2-4 weeks, then use oral forms of thioctic acid.
During the period of use of thioctic acid in
patients with diabetes mellitus, constant monitoring of the concentration of
glucose in the blood plasma is necessary, especially at the initial stage of
therapy. In some cases, it may be necessary to reduce the dose of insulin or
oral hypoglycemic drugs to avoid the development of hypoglycemia. If symptoms
of hypoglycemia occur (dizziness, increased sweating, headache, blurred vision,
nausea), you should immediately stop using thioctic acid.
Alcohol intake reduces the effectiveness of
treatment. During therapy, patients should refrain from drinking alcohol during
the entire course of treatment, and, if possible, in between courses. Alcohol
consumption during treatment with thioctic acid is also a risk factor for the
development and progression of neuropathy.
It is possible to develop autoimmune insulin
syndrome in patients with diabetes mellitus during treatment with thioctic
acid, which is characterized by frequent hypoglycemia in the presence of
autoantibodies to insulin.
Influence
on the ability to drive vehicles and mechanisms
During
the period of use of the drug, care should be taken when driving vehicles and
machinery, as well as when engaging in other potentially hazardous activities
that require increased concentration and speed of psychomotor reactions.
Symptoms:
when using very high doses of thioctic acid from 10
to 40 g, serious signs of intoxication may be observed (generalized convulsive
seizures, severe acid-base imbalance leading to lactic acidosis, hypoglycemic
coma, severe blood clotting disorders, sometimes leading to death).
If a significant overdose of the drug is suspected
(doses equivalent to more than 10 tablets for an adult or more than 50 mg/kg
body weight for children), immediate hospitalization is necessary.
Treatment:
symptomatic. If necessary, anticonvulsant therapy,
measures to maintain the functions of vital organs.
Release form
10 tablets in an aluminum foil blister. 3 blisters along with
instructions for use in a cardboard box.
Storage conditions
Store in a place
protected from light, at a temperature not exceeding 25°C.
Keep out of the reach
of children!
Shelf life
3 years. Do not use
after the expiration date stated on the package.
Vacation
conditions
Dispensed by prescription.