TARKA MV PILLS 180/2MG
TARKA MV PILLS 180/2MG - 28 tabs
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2 mg / 180 mg: Tablets, film-coated, oval pink in color, embossed with the trademark Knoll „182" on one side, length from 17.5 to 17.8 mm, width from 8.8 to 9.0 mm and height from 6.1 to 6.6 mm;
2 mg / 240 mg: Film-coated tablets, oval-colored ocher (light yellow with a brownish tinge), embossed with the Knoll trademark “242" on one side, from 18.6 to 19.0 mm long, from 9.3 to 9.6 mm wide and a height of 6.7 to 7.3 mm;
4 mg / 240 mg: Film-coated tablets, oval-shaped, red-brown in color, with an embossed Knoll trademark “244" on one side, from 18.6 to 19.0 mm long, from 9.3 to 9.6 mm wide, and from 6.7 to 7.3 high mm
Slow Calcium channel blockers. Slow calcium channel blockers, selective, with direct effect on cardiomyocytes. Phenylalkylamine derivatives. Verapamil in combination with other drugs
Tarka bilayer tablets: one layer is designed for the slow release of verapamil hydrochloride, the other for the immediate release of trandolapril.
More than 90% of orally administered verapamil is absorbed. The average bioavailability is 22%, after repeated administration may increase up to 30%.
Eating does not affect the bioavailability of verapamil.
The average time to reach peak plasma concentration is 4 hours. The peak concentration of norverapamil in the blood plasma is reached approximately 6 hours after taking the dose.
Equilibrium concentration after repeated dosing with a regimen of 1 time per day is achieved in 3-4 days.
Binding of verapamil to plasma proteins is approximately 90%.
The half-life after repeated administration is 8 hours. 3-4% of the administered dose is excreted by the kidneys in an unchanged condition. The metabolite is excreted in the urine (70%) and feces (16%).
Bioavailability and the half-life of verapamil are increased in patients with cirrhosis of the liver. However, the kinetics of verapamil does not change in patients with compensated liver dysfunction.
Kidney function does not affect verapamil excretion.
Trandolapril is rapidly absorbed. Absorption is 30 - 60% and does not depend on food intake.
The time to reach peak plasma concentration is about 30 minutes.
Trandolapril is very rapidly excreted from blood plasma, its half-life is less than 1 hour. Trandolapril is hydrolyzed in plasma to trandolaprilat, a specific ACE inhibitor. Absolute bioavailability of trandolaprilat is 13%. The amount of trandolaprilat formed does not depend on food intake. The time to reach average values of peak concentration of trandolaprilat in the blood plasma is 3-8 hours.
The binding of trandolaprilat to plasma proteins is approximately 80%. Binding to ACE is saturated, with high affinity. Most of the circulating trandolaprilat also binds (unsaturated bond) with albumin. The state of equilibrium concentrations of trandolaprilat is reached after approximately 4 days of regular dose once a day. The effective half-life of trandolaprilat is in the range of 15–23 h.
9 - 14% of the administered dose of trandolapril is excreted in the urine as unchanged trandolaprilat.
Kidney clearance of trandolaprilat demonstrates a linear correlation with creatinine clearance and varies within 0.15–4 l / h, depending on the dose. The concentration of trandolaprilat in the blood plasma is significantly higher in patients with creatinine clearance ≤ 30 ml / min. In patients with chronic impaired renal function, an equilibrium state is reached after 4 days, regardless of the degree of impaired renal function.
The concentration of trandolapril in the blood plasma of patients with liver cirrhosis can be 10 times higher. Plasma concentrations and excretion of trandolaprilat also increase in patients with cirrhosis, although to a slightly lesser extent.
In patients with compensated liver dysfunction, the tradolapril / trandolaprilat kinetics does not change.
Since the kinetic interaction between verapamil and trandolapril or trandolaprilat has not been established, the individual kinetic parameters of these two drugs are generally applied to this combination drug.
Tarka is a fixed combination of the calcium antagonist verapamil and the ACE inhibitor trandolapril.
The pharmacological action of verapamil is due to the inhibition of calcium ion current through the slow calcium channels of the cell membrane of vascular smooth muscle and myocardial cells.
The mechanism of action of verapamil provides the following effects.
1. Arterial vasodilation.
Verapamil lowers blood pressure, both at rest and during physical activity due to the expansion of peripheral arterioles.
Reducing the total resistance of peripheral vessels (afterload) leads to a decrease in myocardial oxygen demand and energy.
2. Reduction of myocardial contractility.
The negative inotropic effect of verapamil is compensated by a decrease in total peripheral resistance. Cardiac index does not decrease, except for patients with left ventricular dysfunction.
Verapamil does not affect the sympathetic regulation of the heart, because it does not block beta-adrenergic receptors. Therefore, bronchospasm and similar conditions are not a contraindication for the use of verapamil.
Trandolapril blocks the plasma renin-angiotensin-aldosterone system (RAS), which causes a decrease in plasma angiotensin II levels and leads to a decrease in vasopressor activity and a decrease in aldosterone secretion. Although the latter decrease is not significant, a slight increase in serum potassium concentration may occur along with loss of sodium and fluid. Trandolapril also contributes to peripheral vasodilation by activating the prostaglandin system. In patients with arterial hypertension, the use of ACE inhibitors leads to a decrease in blood pressure both in the prone position and in the standing position, about the same, without a compensatory increase in heart rate. Peripheral arterial resistance decreases without change or with an increase in cardiac output.
An increase in renal blood flow is observed, but the glomerular filtration rate remains unchanged. Achieving optimal reduction in blood pressure may require several weeks of therapy in some patients. Antihypertensive effects persist during long-term therapy. Abrupt cancellation of therapy is not accompanied by a rapid increase in blood pressure.
The antihypertensive effect of trandolapril is established 1 hour after the dose has been taken and lasts for 24 hours, without affecting the circadian rhythm of the arterial pressure.
Not detected pharmacokinetic or RAS interactions between verapamil and trandolapril. Therefore, the observed synergistic activity of these two active ingredients is due to their complementary pharmacological actions.
In clinical studies, Tarka was more effective in reducing high blood pressure than each of her active ingredients separately.
Indications for use
- Essential arterial hypertension in patients in whom blood pressure is normalized with trandolapril and verapamil separately in the same doses, or with inadequate control of blood pressure when using only one of the active components of the drug.
Dosage and administration
For oral administration
Adults use 1 pill 1 time per day.
Special patient groups
in children and adolescents is still not installed. Therefore, use in this age group is not recommended. ÒChildren: safety and efficacy of Tarka
Elderly people: some elderly patients may have a more pronounced effect of lowering blood pressure due to higher systemic bioavailability compared with younger patients suffering from arterial hypertension.
Mode of application
The pill should be swallowed whole, washed down with water, ideally in the morning after eating.
Adverse reactions are classified by message frequency: frequent (> 1/100, <1/10), infrequent (> 1/1000, <1/100), rare (> 1/10 000, <1/1000), very rare (<1/10 000), including isolated cases.
- dizziness, headache
- AV block I degree
Reports from post-marketing observations and phase IV clinical trials
- leukopenia, thrombocytopenia
- anxiety, insomnia
- balance disorders, paresthesia, drowsiness, syncope
- blurred vision, blurred image
- complete AV block, angina pectoris, bradycardia, palpitations, tachycardia
- hypotension, hyperemia, hot flashes
- shortness of breath, nasal congestion
- nausea, diarrhea, dry mouth
- Stevens-Johnson syndrome, angioedema, pruritus, rash
- arthralgia, myalgia
- polakiuria, polyuria
- erectile disfunction
- chest pain, swelling, fatigue
- an increase in the level of lactate dehydrogenase, an increase in the level of alkaline phosphatase, an increase in the content of urea and creatinine in the blood plasma, an increase in aspartate aminotransferase and alanine aminotransferase
Reports of adverse events associated with the use of verapamil hydrochloride
- increased sensitivity
- tremor, extrapyramidal disorders, paralysis (tetraparesis) 1, convulsions
- ringing in the ears
- AV-blockade (2º, 3º), heart failure , stop of the sinus node, sinus bradycardia, asystole
- abdominal pain, vomiting, abdominal discomfort, gingival hyperplasia, intestinal obstruction
- hyperhidrosis, erythema multiforme, alopecia, pruritus, purpura, urticaria
- muscle weakness
- galactorrhea, gynecomastia