DUPLAX

DUPLAX tablets

DUPLAX

International nonproprietary name: telmisartan and amlodipine.

Compound:

Active ingredient: 1 tablet contains amlodipine besylate, which is equivalent to 5 or 10 mg of amlodipine and contains 80 mg of telmisartan.

Excipients: mannitol, meglumine, potassium hydroxide, purified talc, magnesium stearate, croxamellose sodium, 
colloidal anhydrous silicon dioxide, sodium methylhydroxybenzoate, sodium propylhydroxybenzoate, lactose monohydrate, microcrystalline cellulose, corn starch.

Description:

White/pink, round, biconvex and smooth uncoated bilayer tablets.

Pharmacotherapeutic group:

Substances affecting the renin-angiotensin system, angiotensin II antagonists and calcium channel blockers.

ATS code: C09DB04.

Pharmacological properties:

Pharmacodynamics

The drug Duplax contains two antihypertensive substances that regulate blood pressure in patients with arterial hypertension: 
telmisartan, an angiotensin II receptor antagonist, and calcium from the dihydropyridine group.

The combination of these substances has an additional antihypertensive effect and reduces blood
 pressure to a greater extent than each component used separately.

Telmisartan and amlodipine effectively and consistently reduce blood pressure when administered
 in therapeutic doses once daily at 24-hour intervals.

Telmisartan

The functional role of these receptors or the consequences of overstimulation
 by increased angiotensin II levels resulting from
telmisartan are unknown. Telmisartan reduces plasma aldosterone levels.

Amlodipine

Amlodipine is a calcium ion flux inhibitor (slow channel blocker or calcium ion antagonist), belonging to the dihydropyridine 
group and suppressing the transmembrane flux of calcium ions into the smooth muscles of the heart and blood vessels.

The mechanism of the antihypertensive effect of amlodipine is a direct relaxing effect on vascular smooth muscle, 
leading to a decrease in peripheral vascular resistance and blood pressure. Research data shows that amlodipine, as

binds to both dihydropyridine and non-dihydropyridine binding sites. Amlodipine has a selective effect on blood vessels 
and has a greater effect on vascular smooth muscle cells than on cardiac muscle cells.

Absorption

After oral administration of therapeutic doses, amlodipine is well absorbed and reaches maximum concentration 
in the blood after 6-12 hours. Absolute bioavailability is about 64-80%. The bioavailability of amlodipine is independent of food intake.

Distribution

Telmisartan is bound to plasma proteins (>99.5%), mainly to albumin and alpha-1 acid glycoprotein. 
The average apparent volume of distribution
 at steady state (Vdss) is approximately 500 liters. The volume of distribution of amlodipine is approximately 21 L/kg. In vitro

Studies have shown that in patients with arterial hypertension, approximately 97.5% of circulating amlodipine is bound to plasma proteins.

Biotransformation

Telmisartan is metabolized by binding to a glucuronide. The pharmacological activity of the conjugate has not been proven.

The rate and rate of absorption of telmisartan and amlodipine are equivalent to the bioabsorption
of telmisartan and amlodipine when taken as separate tablets.

Telmisartan is rapidly absorbed, although the amount absorbed varies. The absolute bioavailability of
telmisartan is approximately 50%. Plasma concentration versus time curve (AUC0-∞) of telmisartan when taking telmisartan with food

the area under reduction ranges from approximately 6% (40 mg dose) to approximately 19% (160 mg dose). 
Plasma concentrations of telmisartan 3 hours after dosing, regardless 
of whether telmisartan is taken on an empty stomach or with food it was the same.

Removal

Telmisartan has biexponential dissociation pharmacokinetics with a half-life of >20 hours. The maximum plasma concentration (Cmax) and,
to a lesser extent, the concentration under the plasma concentration-time curve.

The elimination of amlodipine from plasma is biphasic, with a half-life of approximately 30-50 hours, which corresponds to the daily dose.
 Stable plasma levels are achieved after 7-8 days of continuous use. Amlodipine 10% and 60% of its metabolites are excreted in the urine.

After oral (and intravenous) administration, telmisartan is almost completely excreted unchanged in the feces. Cumulative urinary excretion 
is ± 1% of the dose. Total plasma clearance (Cltot) (about 1000 ml/min) is high compared to hepatic blood flow (about 1500 ml/min).

indications for use:

Telmisartan and amlodipine are indicated for the treatment of hypertension alone or in combination with other antihypertensive agents.

Telmisartan and amlodipine can be used as initial therapy in patients who require more than one drug to achieve target blood pressure levels.

Contraindications:

Hypersensitivity to any of the components contained in DUPLAX and dihydropyridine derivatives,
 obstructive diseases of the biliary tract, impaired liver function, cardiogenic shock, diabetes mellitus or renal failure, 
concomitant use with aliskeren, pregnancy and lactation, childhood and children under 18 years of age . teenage years.

Directions for use and dosage:

Telmisartan provides effective treatment of arterial hypertension at a daily dose of 20-80 mg,
 while amlodipine is effective at a dose of 2.5-10 mg.

The dose should be individualized and the dose may be increased after at least 2 weeks.
 The antihypertensive effect is detected within 2 weeks. The maximum reduction in blood pressure usually occurs after 4 weeks. 
The maximum recommended dose of telmisartan and amlodipine tablets is 80/10 mg once daily.

Release form:

30 tablets, in a blister. 1 blister is packed in a cardboard box along with an insert.

Storage method:

Store at temperatures below 30°C, in a dry place, protected from light and out of reach of children.

Manufacturer:

Rivpra Formulation Pvt. Ltd. India.

Licensee:

Claus Marsh Ltd., UK.