Tarka

The drug for stabilizing blood pressure Tarka refers to calcium channel blockers - drugs based on verapamil.

Indications of the tarki

Use of Tark's medication is appropriate for improving the condition of people with essential hypertension if their blood pressure is stabilized after taking trandolapril and / or verapamil.

Release form

Tarka is produced in capsular form and refers to preparations of prolonged exposure.

In one capsule, Tarka presents two active ingredients:

• trandolapril in the amount of 2 mg;
• verapamil g / x in the amount of 180 mg.

Tarka capsules are dense light-pinkish gelatinous forms, inside of which there is a granulated mass of trandolapril and a tablet of verapamil g / x.

The blister plate contains ten capsules of the medication. In the packing box of cardboard there are two blister plates and instructions for using Tark.

Pharmacodynamics

Capsules Tarka is a pharmaceutical combination of a calcium antagonist verapamil with an ACE inhibitor trandolapril.

The pharmacological effect of verapamil is due to inhibition of the calcium-ion flow through the delayed calcium tubules of the cell walls of the smooth muscle structure of the vessels and the heart muscle.

Verapamil has such abilities:

• lowers pressure indices in a quiet state or during a physical load (by vasodilation);
• reduces the degree of resistance of peripheral vessels and reduces the need for cardiac muscle in oxygen;
• reduces the contractile function of the heart muscle, without affecting the symptomatic regulation of cardiac activity.

The functional orientation of trandolapril is to block the serum renin-angiotensin-aldosterone complex, to lower the level of angiotensin II in serum, to reduce vasopressor activity and normalize aldosterone production. Trandolapril in Tarka improves peripheral vasodilation by stimulating the prostaglandin system. Probably, a similar mechanism takes place under the hypotensive effect of ACE inhibitors, and is also responsible for the appearance of certain side-effects.

In patients with high blood pressure, treatment with ACE inhibitors leads to a reduction in blood pressure, regardless of body position. Compensation acceleration of cardiac activity on this background is not observed. The resistance of the peripheral arteries decreases: the cardiac output remains unchanged or increases.

 There may be an increase in renal circulation. Nevertheless, the filtration rate does not change. In order to achieve a persistent drop in blood pressure, some people have to undergo treatment for several weeks. In this case, the effect of taking Tark is preserved even with prolonged treatment. In the future, blood pressure does not rise even with a sharp interruption in the treatment of Tark's capsules.

During the experiments, no negative interactions were found between the active ingredients of Tark. Therefore, it is assumed that the synergistic effect of verapamil and trandolapril is due to the combined pharmacological properties. This combination is considered more effective than taking each medication separately.

[1]

Pharmacokinetics

Tark's capsules contain verapamil g / x, which has a delayed release, as well as trandolapril with accelerated release.

Verapamil is absorbed by approximately 90%. The average bioavailability index is 22%, and with long-term admission it can increase to 30%.

The presence of dietary masses in the stomach does not prevent the degree of bioavailability of verapamil.

The average duration of obtaining the maximum serum concentration is 4 hours. Equilibrium with long-term admission of the drug with a frequency of once a day is detected after 3-4 days.

The association of verapamil with plasma albumins can be 90%.

The half-life after a long treatment with Tark is about eight hours. Approximately 3.5% of the used amount of the drug is excreted by renal filtration unchanged. Metabolites in 70% are excreted with urinary fluid, and in 16% - with caloric masses.

Biological availability may increase in patients with cirrhosis. In this case, the kinetic properties of verapamil remain unchanged.

Trandolapril is absorbed relatively quickly, absorption can be from 30 to 60%, regardless of the presence of food masses in the stomach.

Limit level of the drug is detected after half an hour after ingestion.

Trandolapril from Tarka capsules quickly leaves serum, with an average half-life of less than 60 minutes. The drug undergoes hydrolysis processes in plasma with the formation of trandolaprilate.

The duration of the average serum concentration can range from 3 to 8 hours. Full bioavailability is 13%.

The relationship between trandolaprilat and plasma albumin is close to 80%. The connection with the ACE is considered saturated. The bulk of the referring trandolaprilate is also linked by creating an unsaturated protein bond. Equilibrium can be achieved after 4 days of constant reception of Tark.

The half-life of trandolaprilate is estimated at 15 and 23 hours.

From 9 to 14% of the amount consumed, trandolapril leaves the body with urinary fluid in the form of unchanged trandolaprilate.

The values of clearance of trandolaprilate show a linear correlation with creatinine clearance, and are in the range of 0.15-4 L / h, which depends on the dosage. The serum trandolaprilate level is greatly increased in patients with creatinine clearance less than 30 ml per minute. After repeated admission of patients with chronic forms of renal failure, the equilibrium state is observed for four days.

The level of trandolapril in the serum in patients with cirrhosis of the liver, in comparison with healthy people, is usually about ten times higher.

Since the pharmacokinetic type of interaction of individual components of verapamil and trandolapril has not been studied, the kinetic values of both the first and second drugs are applied to the Tark drug.

[2]

Dosing and administration

Adult patients should take one capsule of Tark daily, preferably in the morning, regardless of the presence of food in the stomach. The Tarka capsule is swallowed in a whole state: it is impossible to chew and pour out the contents of the capsule.

[8], [9], [10]

Use of the tarki during pregnancy

Reception of Tark by pregnant patients is prohibited.

The specialists failed to prove the safety of Tark's use during pregnancy. On the contrary, cases of intrauterine pulmonary hypoplasia, inhibition of intrauterine growth of the fetus, hypoplastic disorders of the development of the skull were documented.

Women of reproductive age, before starting treatment with Tark, should be convinced of the absence of pregnancy, and also use reliable methods of contraception.

The main ingredients of Tark are excreted in breast milk, so treatment with a medication during lactation is also contraindicated.

Contraindications

Tark's capsules are not prescribed for such painful conditions:

• propensity to allergy to this medication, or to other drugs-ACE inhibitors;
• an episode of an antrioventricular blockade of II or III degree, in the absence of a functioning IWR;
• hereditary or idiopathic form of angioedema;
• cardiogenic shock;
• acute form of myocardial infarction, accompanied by complications;
• weakness of the sinus node in patients in the absence of a functioning IWR;
• insufficiency of cardiac activity in the stage of decompensation;
• flutter and / or atrial fibrillation;
• the period of gestation and breastfeeding of the child.

Side effects of the tarki

Most often, Tark's reception is accompanied by such undesirable symptoms as coughing, headaches, difficulty with defecation, dizziness, hot flashes.

Other side effects may also occur less frequently:

• thrombocytopenia, leukopenia;
• allergy;
• change in body weight in the direction of decrease;
• sleep disorders, anxiety, apathy;
• trembling in the limbs, disturbance of the sensitivity of the limbs, vestibular disorders;
• deterioration of vision;
• atrioventricular blockade of the first degree;
• bronchitis, stagnation in the lungs;
• pain in the abdomen, diarrhea or constipation, thirst, inflammation of the pancreas;
• jaundice, hepatitis;
• edema on the face, skin rashes, hyperhidrosis, redness of the skin;
• pain in muscles, joints;
• an increase in the daily volume of urine;
• breast enlargement, erectile dysfunction;
• feeling tired.

[3], [4], [5], [6], [7]

Overdose

Acceptance of inflated dosages of Tark can be accompanied by such signs:

• excessive lowering of blood pressure;
• disturbances of electrolyte metabolism;
• slowing or increased heart rate;
• loss of consciousness;
• shock state;
• atrioventricular block;
• heart failure

There are cases of death of patients as a result of an overdose of Tark.

In case of an overdose, help should be directed to the maintenance of vital body functions. Use infusion of medicines with calcium, β-adrenergic stimulation, purification of the stomach and intestines.

Because of the prolonged properties of Tark's medication, it is necessary to establish medical control over the patient's condition for at least 2 days.

Hemodialysis in such cases is not applied.

[11]

Interactions with other drugs

Tarka + antiarrhythmics and β-blockers	Adverse effects on cardiac activity
Tarka + quinidine	Increased antihypertensive effect
Tarka + antihypertensives, diuretics and vasodilators	Increased antihypertensive effect
Tarka + prazosin, terazosin	Increased antihypertensive effect
Tarka + medicines used in HIV therapy (for example, ritonavir)	Increased concentration of verapamil in serum
Tarka + carbamazepine	An increase in the content of carbamazepine in the blood and an increase in the side effects of carbamazepine
Tarka + lithium preparations	Increased neurotoxic effects of lithium
Tarka + rifampicin	Reduction of hypotensive effect of verapamil
Tarka + sulfinpyrazone	Reduction of hypotensive effect of verapamil
Tarka + muscle relaxants	Strengthening of muscle relaxants
Tarka + aspirin	Increased likelihood of bleeding
Tarka + ethyl alcohol	Increase in the concentration of ethyl alcohol in the blood
Tarka + simvastatin and lovastatin	Increase in plasma concentrations of these drugs
Tarka + potassium preparations	Increased risk of hyperkalemia
Tarka + hypoglycemic drugs	Increased hypoglycemic effect and risk of hypoglycemia
Tarka + non-steroidal anti-inflammatory drugs	Decrease in hypotensive effect

[12], [13], [14], [15]

Storage conditions

The Tarka capsules are kept, not removed from the package, in dry and warm rooms. Optimum storage of the drug at a temperature of +18 to + 25 ° C, away from children's access.

[16]

Shelf life

Keep the capsule Tark until 3 years old.

[17]