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Twynsta

Composition
1 tablet contains:

[1,1'-biphenyl]-2-carboxylic acid, 4'-[(1,4'dimethyl-2'-propyl[2,6-bi-1H-benzimidazole]-1'-yl)methyl] (= telmisartan) 40 or 80 mg 3-ethyl-5-methyl(4RS)-2-[-(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3.5-dicarboxylate (= amlodipine besilate) 5 or 10 mg, as besilate

Excipients: colloidal anhydrous silica, FD&C blue No 1 aluminium lake (E 133), ferric oxide black (E172), ferric oxide yellow (E172), magnesium stearate, maize starch, meglumine, microcrystalline cellulose, povidone K25, pregelatinized starch, sodium hydroxide, sorbitol

Description
Telmisartan / amlodipine layered tablets 40/5 mg are layered tablets of oval, biconvex shape. The two layers have different colours with the telmisartan layer being white to off- white, the amlodipine layer is blue. The white layer is debossed with the Boehringer Ingelheim company symbol and the code A1. The tablets are for oral administration.

Telmisartan / amlodipine layered tablets 40/10 mg are layered tablets of oval, biconvex shape. The two layers have different colours with the telmisartan layer being white to off- white, the amlodipine layer is blue. The white layer is debossed with the Boehringer Ingelheim company symbol and the code A2. The tablets are for oral administration.

Telmisartan / amlodipine layered tablets 80/5 mg are layered tablets of oval, biconvex shape. The two layers have different colours with the telmisartan layer being white to off- white, the amlodipine layer is blue. The white layer is debossed with the Boehringer Ingelheim company symbol and the code A3. The tablets are for oral administration.

Telmisartan / amlodipine layered tablets 80/10 mg are layered tablets of oval, biconvex shape. The two layers have different colours with the telmisartan layer being white to off- white, the amlodipine layer is blue. The white layer is debossed with the Boehringer Ingelheim company symbol and the code A4. The tablets are for oral administration.

Properties
Pharmacotherapeutic group: angiotensin II antagonists, plain (telmisartan), combinations with dihydropyridine derivatives (amlodipine), ATC Code: C09DB04.

TWYNSTA combines two antihypertensive compounds with complementary mechanisms to control blood pressure in patients with essential hypertension: an angiotensin II receptor antagonist, telmisartan, and a dihydropyridinic calcium channel blocker, amlodipine.

The combination of these substances has an additive antihypertensive effect, reducing blood pressure to a greater degree than either component alone.

Telmisartan:

Telmisartan is an orally effective and specific angiotensin II receptor (type AT1) antagonist. Telmisartan displaces angiotensin II with very high affinity from its binding site at the AT1 receptor subtype, which is responsible for the known actions of angiotensin II. Telmisartan does not exhibit any partial agonist activity at the AT1 receptor. Telmisartan selectively binds the AT1 receptor. The binding is long lasting. Telmisartan does not show affinity for other receptors, including AT2 and other less characterised AT receptors. The functional role of these receptors is knot known, nor is the effect of their possible over-stimulation by angiotensin II, whose levels are increased by telmisartan. Plasma aldosterone levels are decreased by telmisartan. Telmisartan does not inhibit human plasma renin or block ion channels.


Telmisartan does not inhibit angiotensin converting enzyme (kininase II), the enzyme which also degrades bradykinin. Therefore it is not expected to potentiate bradykinin-mediated adverse effects.


In man, an 80 mg dose of telmisartan almost completely inhibits the angiotensin II evoked blood pressure increase. The inhibitory effect is maintained over 24 hours and still measurable up to 48 hours.


After the first dose of telmisartan, the antihypertensive activity gradually becomes evident within 3 hours. The maximum reduction in blood pressure is generally attained 4 weeks after the start of treatment and is sustained during long-term therapy.


The anti hypertensive effect persists constantly over 24 hours after dosing and includes the last 4 hours before the next dose as shown by ambulatory blood pressure measurements. This is confirmed by trough to peak ratios consistently above 80% seen after doses of 40 and 80 mg of telmisartan in placebo controlled clinical studies.


There is an apparent trend to a dose relationship to a time to recovery of baseline SBP. In this respect data concerning DBP are inconsistent.


In patients with hypertension telmisartan reduces both systolic and diastolic blood pressure without affecting pulse rate.


The antihypertensive efficacy of telmisartan is comparable to that of agents representative of other classes of antihypertensive drugs (demonstrated in clinical trials comparing telmisartan to amlodipine , atenolol, enalapriI , hydrochlorothiazide , losartan, lisinopril, ramipril and valsartan). Upon abrupt cessation of treatment with telmisartan, blood pressure gradually returns to pre-treatment values over a period of several days without evidence of rebound hypertension.


Telmisartan treatment has been shown in clinical trials to be associated with statistically significant reductions in Left Ventricular Mass and Left Ventricular Mass Index in patients with hypertension and Left Ventricular Hypertrophy.


Telmisartan treatment has been shown in clinical trials (including comparators like losartan, ramipril and valsartan) to be associated with statistically significant reductions in proteinuria (including microalbuminuria and macroalbuminuria) in patients with hypertension and diabetic nephropathy.


The incidence of dry cough was significantly lower in patients treated with telmisartan than in those given angiotensin converting enzyme inhibitors in clinical trials directly comparing the two antihypertensive treatments.


Amlodipine:
Amlodipine is a calcium ion influx inhibitor of the dihydropyridine group (slow channel blocker or calcium ion antagonist) and inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle.

 

The mechanism of the antihypertensive action of amlodipine is due to a direct relaxant effect on vascular smooth muscle, leading to reductions in peripheral vascular resistance and in blood pressure. Experimental data indicate that amlodipine binds to both dihydropyridine and non-dihydropyridine binding sites. Amlodipine is relatively vessel-selective, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells.

 

In patients with hypertension, once daily dosing provides clinically significant reductions of blood pressure in both the supine and standing positions throughout the 24 hour interval. Due to the slow onset of action, acute hypotension is not a feature of amlodipine administrations.

 

In hypertensive patients with normal renal function, therapeutic doses of amlodipine resulted in a decrease in renal vascular resistance and an increase in glomerular filtration rate and effective renal plasma flow, without change in filtration fraction or proteinuria.

 

Amlodipine has not been associated with any adverse metabolic effects or changes in plasma lipids and is suitable for use in patients with
asthma, diabetes, and gout.

Use in Patients with Heart Failure:
Haemodynamic studies and exercise based controlled clinical trials in NYHA Class II-IV heart failure patients have shown that amlodipine did not lead to clinical deterioration as measured by exercise tolerance, left ventricular ejection fraction and clinical symptomatology.

A placebo controlled study (PRAISE) designed to evaluate patients in NYHA Class III-IV heart failure receiving digoxin, diuretics and ACE inhibitors has shown that amlodipine did not lead to an increase in risk of mortality or combined mortality and morbidity with heart failure.

In a follow-up, long term, placebo controlled study (PRAISE-2) of amlodipine in patients with NYHA III and IV heart failure without clinical symptoms or objective findings suggestive or underlying ischaemic disease, on stable doses of ACE inhibitors, digitalis, and diuretics, amlodipine had no effect on total cardiovascular mortality. In this same population amlodipine was associated with increased reports of pulmonary oedema despite no significant difference in the incidence of worsening heart failure as compared to placebo.

TWYNSTA
In an 8-week multicenter, randomised, double-blind, placebo-controlled, parallel group factorial study 1461 patients with mild to severe hypertension (mean seated diastolic blood pressure >95 and <110 mmHg) underwent a 3-4 week placebo run-in period in order to wash out all antihypertensive medications before they were randomised to a double-blind active treatment. Treatment with each combination dose of TWYNSTA resulted in significantly greater diastolic and systolic blood pressure reductions and higher control rates
compared to the respective monotherapy components.

The telmisartan/amlodipine combinations showed dose-related reductions in systolic/diastolic blood pressure across the therapeutic dose range:
-21.8/-16.5 mmHg with 40/5 mg,
-22.1/-18.2 mmHg with 80/5 mg,
-24.7/-20.2 mmHg with 40/10 mg, and
-26.4/-20.1 mmHg with 80/10 mg.

The proportions of patients reaching a diastolic blood pressure <90 mmHg with a telmisartan/amlodipine combination were:
71.6% with 40/5 mg,
74.8% with 80/5 mg,
82.1% with 40/10 mg, and
85.3% with 80/10 mg.

A subset of 1050 patients in the factorial design study had moderate to severe hypertension (DBP≥100 mmHg). In these patients who are likely to need more than one antihypertensive agent to achieve blood pressure goal, the observed mean changes in systolic/diastolic blood pressure with a combination therapy containing amlodipine 5 mg (-22.2/-17.2 mmHg with 40/5 mg; -22.5/-19.1 mmHg with 80/5 mg) were comparable to or greater than those seen with amlodipine 10 mg (-21.0/-17.6 mmHg). Additionally, combination therapy showed notably lower oedema rates (1.4% with 40/5 mg; 0.5% with 80/5 mg; 17.6% with amlodipine 10 mg).

 

The majority of the antihypertensive effect was attained within 2 weeks after initiation of therapy.

 

Automated ambulatory blood pressure monitoring (ABPM) performed in a subset of 562 patients confirmed the results seen with in-clinic systolic and diastolic blood pressure reductions consistently over the entire 24-hours dosing period.

 

In a further multicentre, double-blind, active-controlled study, a total of 1097 patients with mild to severe hypertension who were not adequately controlled on amlodipine 5 mg received TWYNSTA (40/5 mg or 80/5 mg) or amlodpine alone (5 mg or 10 mg). After 8 weeks of treatment, each of the combination was statistically significantly superior to both amlodipine monotherapy doses in reducing systolic and diastolic blood pressures:
-13.6/-9.4 mmHg with TWYNSTA 40/5 mg,
-15.0/-10.6 mmHg with TWYNSTA 80/5 mg,
-6.2/-5.7 mmHg with amlodipine 5 mg, and
-11.1/-8.0 mmHg with amlodipine 10 mg.

 

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