Telgio

TELGIO 40 mg: Each tablet contains: Telmisartan 40 mg.
TELGIO 80 mg: Each tablet contains: Telmisartan 80 mg.

Pharmacology: Pharmacodynamics: 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 characterized 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.
Pharmacokinetics: Telmisartan is well absorbed following oral administration. Telmisartan tablet has been studied in a randomized, open-label, three-period, three-sequence partial replicate design study under fasting conditions which included 30 healthy adult male and female subjects.
After oral administration of 80 mg telmisartan tablet, the mean of AUC_0-72h was 5,089.1 ng.hour/mL. The mean of maximum plasma concentration (C_max) was 1,018.44 ng/mL and reached within 0.88 hours (0.50-2.00 hours). The mean elimination half-life (t_½) of telmisartan tablet was 24.36 hours. The geometric mean ratios (90% confidence intervals) of telmisartan tablet were 101.65% (96.33-107.27%) for AUC_0-72h and 84.17% (73.01-97.03%) for C_max. The result of this study showed that the pharmacokinetic parameters of telmisartan tablet were within the acceptance range for bioequivalence, therefore, telmisartan tablet were similar or bioequivalent to the reference drug.
Elderly patients: The pharmacokinetics of telmisartan do not differ in younger and elderly patients.
Patients with renal impairment: Lower plasma concentrations were observed in patients with renal insufficiency undergoing dialysis. Telmisartan is highly bound to plasma protein in renal-insufficient patients and cannot be removed by dialysis. The elimination half-life is not changed in patients with renal impairment.
Patients with hepatic impairment: Pharmacokinetic profile of telmisartan in patients with hepatic impairment showed an increase in absolute bioavailability up to nearly 100%. The elimination half-life is not changed in patients with hepatic impairment.
Pediatric population: The pharmacokinetics assessment are generally consistent with the findings in adults and confirm the nonlinearity of telmisartan, particularly for C_max.

Treatment of essential hypertension.
Prevention of cardiovascular morbidity and mortality in patients 55 years or older at high risk of cardiovascular disease.

Adults: Treatment of essential hypertension: The recommended dose is 40 mg once daily. In cases where the target blood pressure is not achieved, telmisartan dose 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.
In patients with severe hypertension treatment with telmisartan at doses up to 160 mg alone and in combination with hydrochlorothiazide 12.5-25 mg daily was well tolerated and effective.
Prevention of cardiovascular morbidity and mortality: The recommended dose is 80 mg once daily. It is not known whether doses lower than 80 mg of telmisartan are effective in preventing cardiovascular morbidity and mortality. When initiating telmisartan therapy for the prevention of cardiovascular morbidity and mortality, monitoring of blood pressure is recommended, and if appropriate, adjustment of medications that lower blood pressure may be necessary.
Telmisartan may be administered with or without food.
Renal impairment: No posology adjustment is required for patients with renal impairment, including those whose hemodialysis. Telmisartan is not removed from blood by hemofiltration.
Hepatic impairment: In patients with mild to moderate hepatic impairment, the posology should not exceed 40 mg once daily.
Elderly: No dosing adjustment is necessary.
Children and adolescents: Safety and efficacy of telmisartan for use in children below 18 years have not been established.

Limited information is available for telmisartan with regard to overdose in humans. The most prominent manifestations of telmisartan overdose were hypotension and tachycardia, bradycardia also occurred. If symptomatic hypotension should occur, supportive treatment should be instituted. Telmisartan is not removed by hemodialysis.

Hypersensitivity to the active ingredient or any of the excipients.
Second and third trimesters of pregnancy.
Lactation.
Biliary obstructive disorders.
Severe hepatic impairment.
The concomitant use of telmisartan with aliskiren is contraindicated in patients with diabetes mellitus or renal impairment (GFR <60 mL/minute/1.73 m²).
In case of rare hereditary conditions that may be incompatible with an excipient of the product, the use of the product is contraindicated.

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, a periodic monitoring of potassium and creatinine serum levels is recommended. There is no experience regarding the administration of telmisartan in patients with a recent kidney transplant.
Intravascular volume depletion: 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, diarrhea, or vomiting. Such conditions, especially volume and/or sodium depletion, should be corrected before administration of telmisartan.
Dual blockade of the renin-angiotensin-aldosterone system: As a consequence of inhibiting the renin-angiotensin-aldosterone system, changes in renal function (including acute renal failure) have been reported in susceptible individuals, especially if combining medicinal products that affect this system.
Dual blockade of the renin-angiotensin-aldosterone system (e.g. by adding an ACE-inhibitor or the direct renin-inhibitor aliskiren to an angiotensin II receptor antagonist) should therefore be limited to individually defined cases with close monitoring of renal function (see Contraindications).
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, hyperazotemia, 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.
Hyperkalemia: During treatment with medicinal products that affect the renin-angiotensin-aldosterone system, hyperkalemia may occur, especially in the presence of renal impairment and/or heart failure. Monitoring of serum potassium levels in patients at risk is recommended.
Based on experience with the use of 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 (e.g. heparin, etc.) may lead to an increase in serum potassium and should therefore be coadministered cautiously with telmisartan.
Hepatic impairment: Telmisartan is mostly eliminated in the bile. Patients with biliary obstructive disorders or severe hepatic insufficiency can be expected to have reduced clearance. Telmisartan is, therefore, contraindicated for use in these patients. Telmisartan should only be used with caution in patients with mild to moderate hepatic impairment (see Dosage & Administration).
Diabetes mellitus: In diabetic patients with an additional cardiovascular risk, i.e. patients with diabetes mellitus and coexistent coronary artery disease (CAD), the risk of fatal myocardial infarction and unexpected cardiovascular death may be increased when treated with blood pressure lowering agents such as ARBs or ACE-inhibitors. In patients with diabetes mellitus CAD may be asymptomatic and therefore undiagnosed. Patients with diabetes mellitus should undergo appropriate diagnostic evaluation, e.g. exercise stress testing, to detect and to treat CAD accordingly before initiating treatment with telmisartan.
Other: As observed for angiotensin converting enzyme inhibitors, angiotensin receptor antagonists including telmisartan are apparently less effective in lowering blood pressure in black people than in nonblacks, 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 ischemic cardiopathy or ischemic cardiovascular disease could result in a myocardial infarction or stroke.
Effects on ability to drive and use machine: No studies on the effect on the ability to drive and use machines have been performed. However, when driving vehicles or operating machinery, it should be taken into account that dizziness or drowsiness may occasionally occur when taking antihypertensive therapy.
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.

Pregnancy: The use of angiotensin II receptor antagonists is not recommended during the first trimester of pregnancy and should not be initiated during pregnancy. When pregnancy is diagnosed, treatment with angiotensin II receptor antagonists should be stopped immediately, and, if appropriate, alternative therapy should be started.
The use of angiotensin II receptor antagonists is contraindicated during the second and third trimester of pregnancy.
Nonclinical studies with telmisartan do not indicate teratogenic effect, but have shown fetotoxicity.
Angiotensin II receptor antagonists exposure during the second and third trimesters is known to induce human fetotoxicity (decreased renal function, oligohydramnios, skull ossification retardation) and neonatal toxicity (renal failure, hypotension, hyperkalemia).
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.
Should exposure to angiotensin II receptor antagonists have occurred from the second trimester of pregnancy, ultrasound check of renal function and skull is recommended.
Infants whose mothers have taken angiotensin II receptor antagonists should be closely observed for hypotension.
Lactation: Telmisartan is contraindicated during lactation since it is not known whether it is excreted in human milk. Animal studies have shown excretion of telmisartan in breast milk.
Fertility: No studies on fertility in humans have been performed.
In preclinical studies, an effect of telmisartan on male and female fertility was not observed.

Infections and infestations: Urinary tract infections (including cystitis), upper respiratory tract infections, sepsis include fatal outcome.
Blood and lymphatic system disorders: Anemia, eosinophilia, thrombocytopenia.
Immune system disorders: Anaphylactic reaction, hypersensitivity.
Metabolism and nutrition disorders: Hyperkalemia, hypoglycemia (in diabetic patients).
Psychiatric disorders: Anxiety, insomnia, depression.
Nervous system disorders: Syncope (faint).
Eye disorders: Visual disturbance.
Ear and labyrinth disorders: Vertigo.
Cardiac disorders: Bradycardia, tachycardia.
Vascular disorders: Hypotension, orthostatic hypotension.
Respiratory, thoracic, and mediastinal disorders: Dyspnea.
Gastrointestinal disorders: Abdominal pain, diarrhea, dry mouth, dyspepsia, flatulence, stomach discomfort, vomiting.
Hepatobiliary disorders: Hepatic function abnormal/liver disorder*.
*Most cases of hepatic function abnormal/liver disorder occurred in patients in Japan, who are more likely to experience these adverse drug reactions.
Skin and subcutaneous tissue disorders: Pruritus, hyperhidrosis, rash, angioedema (with fatal outcome), eczema, erythema, urticaria, drug eruption, toxic skin eruption.
Musculoskeletal, connective tissue, and bone disorders: Back pain, muscle spasms (cramps in leg), myalgia, arthralgia, pain in extremity (leg pain), tendon pain (tendinitis like symptoms).
Renal and urinary tract disorders: Renal impairment including acute renal failure (see Precautions).
General disorders and administration site conditions: Chest pain, influenza-like illness, asthenia (weakness).
Investigations: Blood creatinine increased, hemoglobin decreased, blood uric increased, hepatic enzymes increased, blood creatine phosphokinase (CPK) increased.

Telmisartan may increase the hypotensive effect of other antihypertensive agents. Other interactions of clinical significance have not been identified.
Coadministration of telmisartan did not result in a clinically significant interaction with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin, and amlodipine. For digoxin, a 20% increase in median plasma digoxin trough concentration has been observed (39% in a single case), monitoring of plasma digoxin levels should be considered.
Coadministration of telmisartan and ramipril led to an increase of up to 2.5 fold in the AUC_0-24 and C_max of ramipril and ramiprilat. The clinical relevance of this observation is not known.
Reversible increases in serum lithium concentrations and toxicity have been reported during concomitant administration of lithium with angiotensin converting enzyme inhibitors. Cases have also been reported with angiotensin II receptor antagonists including telmisartan. Therefore, serum lithium level monitoring is advisable during concomitant use.
Treatment with NSAIDs (i.e. acetylsalicylic acid (ASA) at anti-inflammatory dosage regimens, COX-2 inhibitors and nonselective NSAIDs) is associated with the potential for acute renal insufficiency in patients who are dehydrated. Compounds acting on the renin-angiotensin system like telmisartan may have synergistic effects. Patients receiving NSAIDs and telmisartan should be adequately hydrated and be monitored for renal function at the beginning of combined treatment.
A reduced effect of antihypertensive drugs like telmisartan by inhibition of vasodilating prostaglandins has been reported during combined treatment with NSAIDs.

Store at temperatures not exceeding 30°C.

Angiotensin II Antagonists

C09CA07 - telmisartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.

Rx