Telmisartan STELLA

Telmisartan STELLA

telmisartan

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Stellapharm J.V.
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Contents
Telmisartan.
Description
Each Telmisartan STADA 40 mg tablet contains: Telmisartan 40 mg.
Each Telmisartan STADA 80 mg tablet contains: Telmisartan 80 mg.
Excipients/Inactive Ingredients: Sorbitol, sodium hydroxide, meglumine, povidone K25, magnesium stearate.
Action
Pharmacology: Pharmacodynamics: Telmisartan is an orally active 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 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.
In human, 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 4-8 weeks after the start of treatment and is sustained during long-term therapy.
Pharmacokinetics: Telmisartan is rapidly absorbed from the gastrointestinal tract. The absolute oral bioavailability is dose dependent and is about 42% after a 40 mg dose and 58% after a 160 mg dose. Peak plasma concentrations of telmisartan are reached about 0.5 to 1 hour after an oral dose. Telmisartan is over 99% bound to plasma proteins. It is excreted almost entirely in the faeces via bile, mainly as unchanged drug. The terminal elimination half-life of telmisartan is about 24 hours.
Indications/Uses
Hypertension: Treatment of essential hypertension in adults.
Cardiovascular prevention: Reduction of cardiovascular morbidity in adults with: Manifest atherothrombotic cardiovascular disease (history of coronary heart disease, stroke, or peripheral arterial disease); or Type 2 diabetes mellitus with documented target organ damage.
Dosage/Direction for Use
Hypertension: 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, the dose of telmisartan can be increased to a maximum of 80 mg once daily. Alternatively, telmisartan may be used in combination with thiazide-type diuretics such as hydrochlorothiazide, which has been shown to have an additive blood pressure lowering effect with telmisartan. When considering raising the dose, it must be borne in mind that the maximum antihypertensive effect is generally attained four to eight weeks after the start of treatment.
Cardiovascular prevention: The recommended dose is 80 mg once daily. It is not known whether doses lower than 80 mg of telmisartan are effective in reducing cardiovascular morbidity. When initiating telmisartan therapy for the reduction of cardiovascular morbidity, close monitoring of blood pressure is recommended, and if appropriate adjustment of medications that lower blood pressure may be necessary.
Renal impairment: Limited experience is available in patients with severe renal impairment or haemodialysis. A lower starting dose of 20 mg is recommended in these patients. No posology adjustment is required for patients with mild to moderate renal impairment.
Hepatic impairment: In patients with mild to moderate hepatic impairment, a daily dose should not exceed 40 mg once daily in monotherapy and combination therapy with hydroclorothiazide. The combination with thiazide diuretics is contraindicated in patients with severe hepatic impairment.
Elderly patients: No dose adjustment is necessary.
Adolescents aged below 18 years: The safety and efficacy of telmisartan have not been established.
Use of suitable dosage forms is recommended when using telmisartan with dose of 20 mg.
Administration: Telmisartan STADA is administered orally, taken without regard to meals. Tablets should be taken out of the blister shortly before administration.
Overdosage
There is limited information with regard to overdose in humans.
Symptoms: The most prominent manifestations of telmisartan overdose were hypotension and tachycardia; bradycardia, dizziness, increase in serum creatinine, and acute renal failure have also been reported.
Treatment: Telmisartan is not removed by haemodialysis. The patient should be closely monitored, and the treatment should be symptomatic and supportive. Management depends on the time since ingestion and the severity of the symptoms. Suggested measures include induction of emesis and/or gastric lavage. Activated charcoal may be useful in the treatment of overdosage. Serum electrolytes and creatinine should be monitored frequently. If hypotension occurs, the patient should be placed in a supine position, with salt and volume replacement given quickly.
Contraindications
Known hypersensitivity to any ingredient in the formulation; Second and third trimesters of pregnancy and lactation; Biliary obstructive disorders; Severe hepatic impairment; The concomitant use of telmisartan with aliskiren-containing products is contraindicated in patients with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73 m2).
Special Precautions
Hepatic impairment: Telmisartan is not to be given to patients with cholestasis, biliary obstructive disorders or severe hepatic impairment since telmisartan is mostly eliminated with the bile. These patients can be expected to have reduced hepatic clearance for telmisartan. Telmisartan should be used only with caution in patients with mild to moderate hepatic impairment.
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.
Renal impairment and kidney transplant: When telmisartan is used in patients with impaired renal function, periodic monitoring of potassium and creatinine serum levels is recommended. There is no experience regarding the administration of telmisartan in patients with recent kidney transplantation.
Intravascular hypovolaemia: Symptomatic hypotension, especially after the first dose, may occur in patients who are volume and/or sodium depleted by vigorous diuretic therapy, dietary salt restriction, diarrhoea or vomiting. Such conditions should be corrected before the administration of telmisartan.
Dual blockade of the renin-angiotensin-aldosterone system (RAAS): There is evidence that the concomitant use of ACE inhibitors, angiotensin II receptor blockers or aliskiren increases the risk of hypotension, hyperkalaemia and decreased renal function (including acute renal failure). Dual blockade of RAAS through the combined use of ACE inhibitors, angiotensin II receptor blockers or aliskiren is therefore not recommended. If dual blockade therapy is considered absolutely necessary, this should only occur under specialist supervision and subject to frequent close monitoring of renal function, electrolytes and blood pressure. ACE inhibitors and angiotensin II receptor blockers should not be used concomitantly in patients with diabetic nephropathy.
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 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: As with other vasodilators, special caution is indicated in patients suffering from aortic or mitral stenosis, or obstructive hypertrophic cardiomyopathy.
Diabetic patients treated with insulin or antidiabetics: In these patients hypoglycaemia may occur under telmisartan treatment. Therefore, in these patients an appropriate blood glucose monitoring should be considered; a dose adjustment of insulin or antidiabetics may be required, when indicated.
Telmisartan may cause porphyria, it should be used only when there are no safer alternative therapies and caution should be exercised in patients with severe hypertension.
Hyperkalaemia: The use of medicinal products that affect the renin-angiotensin-aldosterone system may cause hyperkalaemia.
In the elderly, in patients with renal insufficiency, in diabetic patients, in patients concomitantly treated with other medicinal products that may increase potassium levels, and/or in patients with intercurrent events, hyperkalaemia may be fatal.
Before considering the concomitant use of medicinal products that affect the renin-angiotensin-aldosterone system, the benefit risk ratio should be evaluated.
The main risk factors for hyperkalaemia to be considered are: Diabetes mellitus, renal impairment, age (>70 years).
Combination with one or more other medicinal products that affect the renin-angiotensin-aldosterone system and/or potassium supplements. Medicinal products or therapeutic classes of medicinal products that may provoke hyperkalaemia are salt substitutes containing potassium, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor antagonists, non steroidal anti-inflammatory medicinal products (NSAIDs, including selective COX-2 inhibitors), heparin, immunosuppressives (cyclosporin or tacrolimus), and trimethoprim.
Intercurrent events, in particular dehydratation, acute cardiac decompensation, metabolic acidosis, worsening of renal function, sudden worsening of the renal condition (e.g. infectious diseases), cellular lysis (e.g. acute limb ischemia, rhabdomyolysis, extend trauma). Close monitoring of serum potassium in at risk patients is recommended.
Sorbitol: Telmisartan STADA contains sorbitol. Patients with rare hereditary problems of fructose intolerance should not take this drug.
Sodium ion: The maximum recommended daily dose (80 mg) of this medicinal product contains 3.864 mg sodium (found in NaOH). This is equivalent to approximately 0.2% of the recommended maximum daily intake of sodium for an adult.
Gastroduodenal ulcer can work or other stomach problems (increased risk of gastrointestinal bleeding) can occur.
Mild or moderate renal function impairment.
Others: As observed for angiotensin converting enzyme inhibitors, telmisartan and the other angiotensin II receptor antagonists are apparently less effective in lowering blood pressure in black people than in non-blacks, possibly because of higher prevalence of low-renin states in the black hypertensive population.
As with any antihypertensive agent, excessive reduction of blood pressure in patients with ischaemic cardiovascular disease could result in a myocardial infarction or stroke.
Effects on ability to drive and use machines: When driving vehicles or operating machinery it should be taken into account that vertigo or dizziness may occasionally occur when taking antihypertensive therapy such as telmisartan.
Use in Pregnancy: Angiotensin II receptor antagonists should not be initiated during pregnancy. Unless continued angiotensin II receptor antagonist therapy is considered essential, patients planning pregnancy should be changed to alternative antihypertensive treatments which have an established safety profile for use in pregnancy. When pregnancy is diagnosed, treatment with angiotensin II receptor antagonists should be stopped immediately, and, if appropriate, alternative therapy should be started.
Use In Pregnancy & Lactation
Pregnancy: When used in pregnancy during the second and third trimesters, drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus. When pregnancy is detected, telmisartan should be discontinued as soon as possible.
Angiotensin II receptor antagonists should not be initiated during pregnancy. Unless continued angiotensin II receptor antagonist therapy is considered essential, patients planning pregnancy should be changed to alternative antihypertensive treatments which have an established safety profile for use in pregnancy. When pregnancy is diagnosed, treatment with angiotensin II receptor antagonists should be stopped immediately, and, if appropriate, alternative therapy should be started.
Lactation: It is not known whether telmisartan is excreted in human milk, but telmisartan was shown to be present in the milk of lactating rats. Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Adverse Reactions
Very common (ADR ≥1/10); common (1/100 ≤ADR <1/10); uncommon (1/1000 ≤ADR <1/100); rare (1/10000 ≤ADR <1/1000); very rare (ADR <1/10,000).
Infections and infestations: Uncommon: Upper respiratory tract infection including pharyngitis and sinusitis, urinary tract infection including cystitis. Rare: Sepsis including fatal outcome.
Blood and the lymphatic: Uncommon: Anaemia. Rare: Eosinophilia, thrombocytopenia.
Immune system: Rare: Anaphylactic reaction, hypersensitivity.
Metabolism and nutrition: Uncommon: Hyperkalaemia. Rare: Hypoglycaemia (in diabetic patients).
Psychiatric: Uncommon: Depression, insomnia. Rare: Anxiety.
Nervous system: Uncommon: Syncope. Rare: Somnolence.
Eye: Rare: Visual disturbance.
Ear and labyrinth: Uncommon: Vertigo.
Cardiac: Uncommon: Bradycardia. Rare: Tachycardia.
Vascular: Uncommon: Hypotension, orthostatic hypotension.
Respiratory, thoracic and mediastinal: Uncommon: Dyspnoea, cough. Very rare: Interstitial lung disease.
Gastrointestinal: Uncommon: Abdominal pain, diarrhoea, dyspepsia, flatulence, vomiting. Rare: Stomach discomfort, dry mouth.
Hepato-biliary: Rare: Hepatic function abnormal/liver disorder.
Skin and subcutaneous tissue: Uncommon: Hyperhidrosis, pruritus, rash. Rare: Angioedema (also with fatal outcome), eczema, erythema, urticaria, drug eruption, toxic skin eruption.
Muscoloskeletal and connective tissue: Uncommon: Myalgia, back pain (e.g. sciatica), muscle spasms. Rare: Arthralgia, pain in extremity, tendon pain (tendonitis like symptoms).
Renal and urinary: Uncommon: Renal impairment including acute renal failure.
General: Uncommon: Chest pain, asthenia (weakness). Rare: Influenza-like illness.
Investigations: Uncommon: Blood creatinine increased. Rare: Blood uric acid increased, hepatic enzyme increased, blood creatine phosphokinase increased, haemoglobin decreased.
Drug Interactions
Digoxin: When telmisartan was co-administered with digoxin, median increases in digoxin peak plasma concentration (49%) and in trough concentration (20%) were observed. When initiating, adjusting, and discontinuing telmisartan, monitor digoxin levels in order to maintain levels within the therapeutic range.
As with other medicinal products acting on the renin-angiotensin-aldosterone system, telmisartan may provoke hyperkalaemia. The risk may increase in case of treatment combination with other medicinal products that may also provoke hyperkalaemia (salt substitutes containing potassium, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor antagonists, non steroidal anti-inflammatory medicinal products (NSAIDs, including selective COX-2 inhibitors), heparin, immunosuppressives (cyclosporin or tacrolimus), and trimethoprim).
Concomitant use not recommended: Potassium sparing diuretics or potassium supplements: Angiotensin II receptor antagonists such as telmisartan, attenuate diuretic induced potassium loss. Potassium sparing diuretics e.g. spirinolactone, eplerenone, triamterene, or amiloride, potassium supplements, or potassium-containing salt substitutes may lead to a significant increase in serum potassium. If concomitant use is indicated because of documented hypokalemia they should be used with caution and with frequent monitoring of serum potassium.
Lithium: Reversible increases in serum lithium concentrations and toxicity have been reported during concomitant administration of lithium with angiotensin converting enzyme inhibitors, and with angiotensin II receptor antagonists, including telmisartan. If use of the combination proves necessary, careful monitoring of serum lithium levels is recommended.
Concomitant use requiring caution: Non-steroidal anti-inflammatory medicinal products: NSAIDs (i.e. acetylsalicylic acid at anti-inflammatory dosage regimens, COX-2 inhibitors and non-selective NSAIDs) may reduce the antihypertensive effect of angiotensin II receptor antagonists. In some patients with compromised renal function (e.g. dehydrated patients or elderly patients with compromised renal function), the co-administration of angiotensin II receptor antagonists and agents that inhibit cyclo-oxygenase may result in further deterioration of renal function, including possible acute renal failure, which is usually reversible. Therefore, the combination should be administered with caution, especially in the elderly. Patients should be adequately hydrated and consideration should be given to monitoring of renal function after initiation of concomitant therapy and periodically thereafter.
In one study the co-administration of telmisartan and ramipril led to an increase of up to 2.5 fold in the AUC0-24 and Cmax of ramipril and ramiprilat. The clinical relevance of this observation is not known.
Diuretics (thiazide or loop diuretics): Prior treatment with high dose diuretics such as furosemide (loop diuretic) and hydrochlorothiazide (thiazide diuretic) may result in volume depletion and in a risk of hypotension when initiating therapy with telmisartan.
To be taken into account with concomitant use: Other antihypertensive agents: The blood pressure lowering effect of telmisartan can be increased by concomitant use of other antihypertensive medicinal products. The following medicinal products may potentiate the hypotensive effects of all antihypertensives including telmisartan: Baclofen, amifostine. Furthermore, orthostatic hypotension may be aggravated by alcohol, barbiturates, narcotics or antidepressants.
Corticosteroids (systemic route): Reduction of the antihypertensive effect.
Storage
Store in a well-closed container, in a dry place, protect from moisture. Do not store above 30°C.
Shelf-Life: 24 months from the date of manufacturing.
ATC Classification
C09CA07 - telmisartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.
Presentation/Packing
Tab 40 mg (white caplet, biconvex and plain on two sides) x 4 x 7's. 80 mg (white caplet, biconvex and plain on two sides) x 4 x 7's.
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