TELMIZ 40 mg: A white to off-white, biconvex round shaped tablet with breakline on one side and plain on the other side.
Each tablet TELMIZ 40 contains: Telmisartan 40 mg.
TELMIZ 80 mg: A white to off-white, biconvex round-shaped tablet with breakline on both sides.
Each tablet TELMIZ 80 contains: Telmisartan 80 mg.
Excipients/Inactive Ingredients: Mannitol, Meglumine, Polyvinylpyrrolidone, Sodium Starch Glycolate, Sodium Stearyl Fumarate, Sodium Hydroxide.
Pharmacology: 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 selectivity binds the AT1 receptor. The binding is long lasting. Telmisartan does not show affinity for other receptor, including AT2 and other less characterized AT receptors. The functional role of these receptors is unknown, 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 patients with hypertension telmisartan reduces both systolic and diastolic blood pressure without affecting pulse rate. The antihypertensive efficacy of telmisartan has been compared to antihypertensive drugs such as amlodipine, atenolol, enalapril, 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 to be associated with reductions in left ventricular mass index in patients with hypertension and left ventricular hypertrophy.
Telmisartan treatment has been shown to be associated with 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.
Pharmacokinetics: Telmisartan is well absorbed following oral administration. TELMIZ tablet has been studied in a randomized, open-label, three-period, three-sequence, partial replicate design study under fasting conditions which included 33 healthy adult male subjects.
After oral administration of 80 mg TELMIZ tablet, the mean of AUC0-72h was 5916.94 ng·h·mL-1. The mean of maximum plasma concentration (Cmax) was 1147.19 ng·mL-1 and reached within 1.00 hour (0.50-4.00 hours). The mean elimination half-life (t½) of TELMIZ tablet was 18.76 hours. The geometric mean ratios (90% confidence intervals) of TELMIZ tablet were 97.51% (92.73-102.54%) for AUC0-72h and 88.90% (78.37-100.84%) for Cmax. The result of this study showed that the pharmacokinetic parameters of TELMIZ tablet were within the acceptance range for bioequivalence, therefore, TELMIZ tablet were similar or bioequivalent to the reference drug.
Treatment of essential hypertension.
Adults: 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 4-8 weeks after the start of treatment. Telmisartan may be taken with or without food.
Renal impairment: No posology adjustment is required for patients with renal impairment, including those on haemodialysis.
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: Telmisartan is not recommended for use in children below 18 years due to limited data on safety and efficacy.
Limited information is available 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 haemodialysis.
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/min/1.73 m2).
In case of rare hereditary conditions that may be incompatible with an excipient of the product (refer to PRECAUTIONS) the use of the product is contraindicated.
Renovascular hypertension: There is an increased risk of severe hypotension and renal insufficiency when patient 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, diarrhoea or vomiting. Such conditions, especially volume and/or sodium depletion, should be corrected before the 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) is therefore not recommended in patients with already controlled blood pressure and should 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 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.
Hyperkalaemia: During treatment with medicinal products that affect the renin-angiotensin-aldosterone system hyperkalaemia may occur, especially in the presence of renal impairment and/or heart failure. Monitoring of serum potassium 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 (heparin, etc.) may lead to an increase in serum potassium and should therefore be co-administered cautiously with telmisartan.
Hepatic impairment: Telmisartan is mostly eliminated in the bile. Patients with biliary obstructive disorders or hepatic insufficiency can be expected to have reduced clearance. telmisartan should be used with caution in these patients.
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.
Others: As observed for angiotensin converting enzyme inhibitors, angiotensin receptor blockers including telmisartan 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 cardiopathy or ischaemic cardiovascular disease could result in a myocardial infarction or stroke.
Effect on the ability to drive and use machines: 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: See Use in Pregnancy & Lactation section for further information.
Fertility, pregnancy and lactation: 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.
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.
Telmisartan do not indicate teratogenic effects but have shown fetotoxicity.
When used in pregnancy during the second and third trimesters, drug that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus. When pregnancy is detected, telmisartan tablets should be discontinued as soon as possible.
Drug that acts directly on the renin-angiotensin system can cause fetal and neonatal morbidity and death when administered to pregnant women. When pregnancy is detected, telmisartan tablets should be discontinued as soon as possible.
The use of drug that act directly on the renin-angiotensin system during second and third trimesters of pregnancy has been associated with fetal and neonatal injury, including hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure, and death.
Oligohydramnios has also been reported, presumably resulting from decreased fetal renal fiction: Oligohydramnios in this setting has been associated with fetal limb contractures, craniofacial deformation, and hypoplastic lung development. Prematurity, intrauterine growth retardation, and patent ductus arteriosus have also been reported, although it is not clear whether these occurrences were due to exposure to the drug.
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, hyperkalaemia).
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.
Telmisartan is contraindicated during lactation since it is not known whether it is excreted in human milk. Non-clinical studies have shown excretion of telmisartan in breast milk.
Fertility: No studies on fertility in humans have been performed. An effect of telmisartan on male and female fertility was not observed.
The incidence of adverse events was not dose related and showed no correlation with gender, age or race of the patients.
The adverse drug reactions listed as follows have been, accumulated from patients treated with telmisartan: Infections and infestations: Urinary tract infections (including cystitis), upper respiratory tract infections, sepsis including fatal outcome.
Blood and lymphatic system disorders: Anaemia, eosinophilia, thrombocytopenia.
Immune system disorders: Anaphylactic reaction, hypersensitivity.
Metabolism and nutrition disorders: Hyperkalemia, hypoglycemia (in diabetic patients).
Psychiatric disorders: Insomnia, depression, anxiety.
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: Dyspnoea.
Gastro-intestinal disorders: Abdominal pain, diarrhoea, dry mouth, dyspepsia, flatulence, vomiting, stomach discomfort.
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 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 legs), myalgia, arthralgia, pain in extremity (leg pain), tendon pain (tendinitis like symptoms).
Renal and urinary disorders: Renal impairment including acute renal failure (see also under PRECAUTIONS).
General disorders and administration site conditions: Chest pain, asthenia (weakness), influenza-like illness.
Investigations: Blood creatinine increased, haemoglobin decreased, blood uric acid 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.
Co-administration of telmisartan did not result in a clinically significant interaction with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin, and amlodipine. For digoxin, an increase in median concentration of digoxin in plasma has been observed, therefore monitoring of plasma digoxin levels should be considered.
The co-administration of telmisartan and ramipril led to an increase in the AUC0-24 and Cmax 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., 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 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.
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.
The occurrence of hyperkalaemia depends on associated risk factors. The risk is increased in case of the previously-mentioned treatment combinations. The risk is particularly high in combination with potassium sparing-diuretics, and when combined with salt substitutes containing potassium. A combination with ACE inhibitors or NSAIDs, for example, presents as lesser risk provided that precautions for use are strictly followed.
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.
Potassium sparing diuretics or potassium supplements: Angiotensin II receptor antagonists such as telmisartan, attenuate diuretic induced potassium loss. Potassium sparing diuretics e.g., spironolactone, 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 hypokalaemia, they should be used with caution and with frequent monitoring of serum potassium.
Corticosteroids (systemic route): Reduction of the antihypertensive effect.
Store at temperature below 30°C.
C09CA07 - telmisartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.
Telmiz tab 40 mg
3 × 10's (Rp240,000/boks)
Telmiz tab 80 mg
3 × 10's (Rp300,000/boks)
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