Leaflet

Biocardis

Tablets

Composition :

   Each tablet contains:  20 mg or 40 mg or 80 mg of telmisartan

Mechanism of Action:   

Telmisartan is an orally effective and specific angiotensin II receptor (type AT₁) antagonist , 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 not known, nor is the effect of their possible overstimulation 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.

After the first dose of telmisartan, the antihypertensive activity gradually becomes evident within 3 hours. The maximum reduction in blood pressure is generally attained 4-8 weeks after the start of treatment and is sustained during long-term therapy. The antihypertensive effect persists constantly over 24 hours after dosing and includes the last 4 hours before the next dose.

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

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.

Pharmacokinetics :

Following oral administration, peak concentrations (C _max ) of telmisartan are reached in 0.5-1 hour after dosing. The mean absolute bioavailability for telmisartan is about 50% .

Telmisartan is characterised by biexponential decay pharmacokinetics with a terminal elimination half-life of approximately 24 hours,The most of the administered dose (>97%) was eliminated unchanged in feces via biliary excretion; only minute amounts were found in the urine .

 Telmisartan is highly bound to plasmaprotein(>99.5%).

Elderly patients:

The pharmacokinetics of telmisartan do not differ between the elderly and those younger than 65 years.

 Patients with renal impairment:

Renal excretion does not contribute to the clearance of telmisartan. No dosage adjustment is necessary in patients with mild to moderate renal impairment. Telmisartan is not removed from blood by hemofiltration  .  

Patients with hepatic impairment:

Pharmacokinetic studies in patients with hepatic impairment showed an increase in absolute bioavailability up to nearly 100%.

 

Indications:

Biocardis is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents .

Contraindications:

Biocardis is Contraindicated in :

• patients who are hypersensitive to any component of this product.
• pregnancy and lactation  .
• Biliary obstructive disorders.
• Severe hepatic impairment.
• Severe renal impairment .

Side effects :

Side effects have generally been mild and transient in nature and have only infrequently required discontinuation of therapy . The incidence of adverse events was not dose related and showed no correlation with gender, age or race of the patients .

The following adverse events may occur :  bronchitis , headache, dizziness ,insomnia , depression , anxiety,  dyspepsia, palpitation , arthralgia , cramps ( legs) , rash , sweating increased , abdominal pain, diarrhea, dyspepsia, gastrointestinal disorders.

As with other angiotensin II antagonists isolated cases of angioedema, urticaria and other related events have been reported.

when driving vehicles or operating machinery it must be borne in mind that dizziness or drowsiness may occasionally occur when taking antihypertensive therapy.

Laboratory findings

Infrequently, a decrease in haemoglobin or an increase in uric acid,  Increases in creatinine or liver enzymes have been observed during treatment with telmisartan .

Warnings and Precautions :

Hepatic impairment:

Telmisartan should be used with caution in patients with biliary obstructive disorders or hepatic insufficiency.

Renal impairment:

When telmisartan is used in patients with impaired renal function, a periodic monitoring of potassium and creatinine serum levels is recommended.

Renovascular hypertension:

There is an increased risk of severe hypotension and renal insufficiency when patients with bilateral renal artery stenosis or stenosis of the artery to a single functioning kidney are treated with medicinal products that affect the renin-angiotensin-aldosterone system.

Intravascular volume depletion:

In patients who are volume and/or sodium depleted (e.g., those being treated with high doses of diuretics), symptomatic hypotension may occur after initiation of therapy with telmisartan  . Such conditions should be corrected prior to administration of telmisartan .

Other conditions with stimulation of the renin-angiotensin-aldosterone system:

In patients whose vascular tone and renal function depend predominantly on the activity of the renin-angiotensin-aldosterone system (e.g. patients with severe congestive heart failure or underlying renal disease, including renal artery stenosis), treatment with other medicinal products that affect this system has been associated with acute hypotension, hyperazotaemia, oliguria, or rarely acute renal failure.

Primary aldosteronism:

Patients with primary aldosteronism generally will not respond to antihypertensive medicinal products acting through inhibition of the renin-angiotensin system. Therefore, the use of telmisartan is not recommended.

Aortic and mitral valve stenosis, obstructive hypertrophic cardiomyopathy:

Special caution is indicated in patients suffering from aortic or mitral stenosis, or obstructive hypertrophic cardiomyopathy.

Hyperkalaemia:

During treatment with other medicinal products that affect the renin-angiotensin-aldosterone system hyperkalaemia may occur, especially in the presence of renal impairment and/or heart failure. Adequate monitoring of serum potassium in patients at risk is recommended.

Based on experience with the use of other medicinal products that affect the renin-angiotensin system, concomitant use with potassium-sparing diuretics, potassium supplements, salt substitutes containing potassium or other medicinal products that may increase the potassium level (heparin, etc.) may lead to an increase in serum potassium and should therefore be co-administered cautiously with Telmisartan .

Drug Interactions

Telmisartan may increase the hypotensive effect of other antihypertensive agents. Other interactions of clinical significance have not been identified.

Compounds, which have been studied in pharmacokinetic trials include digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol and amlodipine. For digoxin a 20% increase in median plasma digoxin trough concentration has been observed , monitoring of plasma digoxin levels should be considered

Reversible increases in serum lithium concentrations and toxicity have been reported during concomitant administration of lithium with angiotensin converting enzyme inhibitors. Very rare cases have also been reported with angiotensin II receptor antagonists. Co-administration of lithium and Telmisartan should be done with caution. If this combination proves essential, serum lithium level monitoring is recommended during concomitant use.

Pregnancy and lactation

telmisartan should preferably not be used during the first trimester of pregnancy. A switch to a suitable alternative treatment should be carried out in advance of a planned pregnancy. The use of drugs that act directly on the renin-angiotensin system during the second and third trimesters of pregnancy can cause injury and even death in the developing foetus . If pregnancy is diagnosed telmisartan should be discontinued as soon as possible.

Telmisartan is contraindicated during lactation since it is not known whether it is excreted in human milk.

Dosage and Administration  :

Adults

The usually effective dose is 40 mg once daily. Some patients may already benefit at a daily dose of 20 mg. In cases where the target blood pressure is not achieved, telmisartan dose can be increased to a maximum of 80 mg once daily.

Renal impairment:

No dosage adjustment is necessary in patients with mild to moderate Renal impairment. Telmisartan is not removed from blood by hemofiltration  .  

Hepatic impairment:

In patients with hepatic impairment the posology should not exceed 40 mg once daily.

Elderly

No dosing adjustment is necessary.

Overdose

Limited data are available with regard to overdosage in humans. The most likely manifestation of overdosage with telmisartan would be hypotension, dizziness and tachycardia.

Management of overdosage :

If symptomatic hypotension should occur, supportive treatment should be instituted. Telmisartan is not removed by hemodialysis

Presentation :

Box of 15 or 20 or 30 tablets of telmisartan  20 mg.

Box of 15 or 20 or 30 tablets of telmisartan  40 mg.

Box of 15 or 20 or 30 tablets of telmisartan  80 mg.

Storage

Store between 15°- 30°C.