Heptral

Heptral is a hepatoprotective medication that also has an antidepressant effect.

Demonstrates cholekenetic and choleretic activity, and in addition, it has a regenerating, antifibrinolytic, detoxifying, neuroprotective and antioxidant effect. The medicine allows not only to replenish the deficiency of ademetionine inside the body, but in addition stimulates the production of this element within various organs (this primarily concerns the spinal cord with the brain, as well as the liver). 

Indications Heptral

It is used for the following disorders:

• intrahepatic cholestasis;
• hepatic pathologies, including cholangitis and chronic ulcerative cholecystitis;
• pre-cirrhotic as well as cirrhotic conditions;
• hepatic intoxication, having an alcoholic, viral or drug (antiviral or anti-tuberculosis substances, antibiotics, contraception and chemotherapy drugs) nature;
• chronic hepatitis or fatty hepatic dystrophy;
• a state of depression;
• withdrawal symptoms (also of alcoholic origin).

Release form

The release of a therapeutic substance is realized in tablets - 10 or 20 pieces inside a pack.

In addition, it is produced in the form of an injection lyophilisate - inside 5 ml vials. The box contains 5 of these bottles and a solvent.

Pharmacodynamics

Ademetionine is a component found inside almost all physiological fluids along with body tissues. The chemical structure of the drug makes it a donor of the methyl subcategory in transmethylation processes. The substance is the basis of many biochemical thiol ligaments (taurine with cysteine, coenzyme A, etc.) during the development of transsulfonation, and in addition, it is a polyamine precursor (spermidine and putrescine with spermine, which are included in the ribosomal structure). It also stimulates cellular repair.

Transmethylation carried out by ademetionine with respect to various components within the body (neurotransmitters, hormones, phospholipids and proteins) is a very important metabolic process. [1]

Long-term use of drugs causes an increase in hepatic glutamine levels, as well as plasma taurine with cysteine; in addition, the amount of serum methionine decreases, from which it can be concluded regarding the stabilization of intrahepatic metabolic processes and the improvement of liver function. [2]

The drug has a choleretic effect through the stimulation of the binding of phosphatidylcholine within the hepatocyte membranes, as well as polarization and an increase in their elasticity. As a result, the transport activity of bile acids is improved, which allows them to be excreted into the biliary system. In addition, the medication helps to relieve bile acids from toxicity - in the process of their sulfation. This improves their renal elimination and facilitates their passage through the hepatocyte walls and excretion in bile.

The use of Heptral leads to the development of positive dynamics in the values of direct bilirubin, and in addition to the activity of aminotransferases and alkaline phosphatase. The hepatoprotective and choleretic properties of drugs continue to persist for a period of 3 months from the date of drug withdrawal.

The level of ademetionine in a child or adolescent is much higher than in an elderly person, because its values decrease with age. At the same time, the values of ademetionine are lower in persons with depression. With high levels of the substance inside the brain tissues, the processes of metabolism of catecholamines (norepinephrine with adrenaline), histamine and indolamines (melatonin with serotonin) are stimulated.

The use of drugs stabilizes phospholipid methylation inside the walls of neuronal cells, normalizing the movement of neuronal impulses and increasing the period of activity of nerve cells.

Experiments have established the effectiveness of Heptral in the treatment of depression. Its antidepressant effect develops at a high rate, reaching peak rates by the 5th-7th day of drug use. During the use of drugs, ademetionine overcomes transformation phases similar to the endogenous component.

Pharmacokinetics

Suction.

When using drugs, the pharmacokinetics of ademetionine has a biexponential character with a stage of pronounced and having a high rate of tissue distribution, as well as with the final stage of elimination with a half-life of approximately 90 minutes.

The absorption of the drug after application is almost complete (96%), and the Cmax values are recorded after 45 minutes. When taken orally, an ademetionine tablet, its Cmax values are tied to the portion size and equal to 0.5-1 mg / l; to achieve this indicator with the introduction of a 1-fold portion in the range of 0.4-1 g, 3-5 hours are required. The intraplasmic level decreases to the initial levels over a period of 24 hours.

Oral bioavailability values increase when drugs are used between meals. After oral administration, the tablets are absorbed inside the gastrointestinal tract and significantly increase the values of plasma ademetionine.

Animal testing using isotopic processes has confirmed that oral administration of ademetionine stimulates the formation of methylated intrahepatic ligaments. In addition, it has been proven that the substance is assimilated through typical metabolic pathways that are characteristic of endogenous ligaments (transsulfonation with transmethylation, decarboxylation, etc.).

Distribution processes.

The indicators of the distribution volume are equal to 0.41, as well as 0.44 l / kg with portions of 0.1 and 0.5 g. Protein synthesis is rather weak - equal to ≤5%.

Exchange processes.

The processes by which ademetionine is produced, regenerated and absorbed are called the ademetionine cycle. During the 1st phase of this cycle, ademetionine-dependent methylase uses ademetionine as a substrate for the production of S-adenosyl-homocysteine, and this element is further hydrolyzed to form adenosine with homocysteine (with the participation of S-adenosyl-homocysteine hydrolase).

In this case, homocysteine is converted back to methionine - through the transfer of the methyl subcategory from 5-methyltetrahydrofolate. At the end, methionine is transformed into ademetionine, which ends the cycle.

Excretion.

During radioisotope tests with the participation of volunteers - ingestion of radioactively labeled (such as methyl 14C) ademetionine demonstrated excretion of a radioactive element in the urine, amounting to 15.5 ± 1.5% after 48 hours; with feces in 72 hours, 23.5 ± 3.5% were excreted. At the same time, approximately 60% of drugs remained incorporated within the stable pools.

Dosing and administration

The medication is used orally (in tablets) or injected intravenously / intramuscularly (lyophilisate dissolved in the supplied L-lysine solvent before the injection procedure). The intravenous procedure is performed at a very low speed.

During intensive therapy, Heptral is administered through injections (a daily portion is equal to 1-2 vials (0.4-0.8 g) for the first 14-21 days of treatment).

With maintenance treatment, the medication is taken orally in a daily dosage of 800-1600 mg (corresponds to 2-4 tablets).

The medicine must be taken between meals. It is recommended to do this during the first half of the day, because with the introduction of drugs, slight nervous excitement can be observed. The tablets are swallowed without chewing and washed down with plain water.

The duration of the supporting treatment cycle is selected by the attending doctor (on average, it is 0.5-2 months).

• Application for children

There is no information regarding the drug efficacy and safety of its use in pediatrics.

Use Heptral during pregnancy

You can not prescribe medication in the 1st and 2nd trimesters; in the 3rd trimester, its use is possible, but only in situations where the likely benefit is more expected than the possible risks of complications.

If the use of Heptral is required for hepatitis B, the issue of canceling breastfeeding must first be resolved.

Contraindications

It is contraindicated to prescribe to people with personal intolerance to the elements of the medication.

Side effects Heptral

The main side signs:

• disorders associated with the work of the gastrointestinal tract: dyspepsia, nausea, heartburn or gastralgia;
• problems with the work of the central nervous system: the rhythm of sleep may change (to correct it, you can take sedatives at night);
• allergy symptoms.

Interactions with other drugs

There is information regarding the appearance of serotonin intoxication in people who used ademetionine together with clomipramine. Therefore, although the likelihood of interaction is only theoretical, you need to be very careful when using the drug in combination with SSRIs, plant elements that contain tryptophan, as well as tricyclics (including clomipramine).

Storage conditions

Heptral must be stored in a place protected from moisture penetration, at temperatures within the 25 ° C mark.

Shelf life

Heptral can be used for a period of 36 months from the date of manufacture of the drug element.

Analogs

Analogues of drugs are Heptor and Ademetionine.

Reviews

Many patients call Heptral one of the most effective or even the only really helping hepatoprotective drug. Many reviews indicate that the drug helps very well in the treatment of the liver. Although there are also opinions of those for whom the medication did not fit at all. Of the shortcomings, only the very high cost of drugs is noted.