Chemical formula: C₃₃H₃₀N₄O₂ Molecular mass: 514.617 g/mol PubChem compound: 65999
Telmisartan interacts in the following cases:
Orthostatic hypotension may be aggravated by alcohol, barbiturates, narcotics, or antidepressants during therapy with telmisartan.
Limited experience is available in patients with severe renal impairment or haemodialysis. A lower starting dose of 20 mg is recommended in these patients.
Periodic monitoring of potassium and creatinine serum levels is recommended.
In patients with mild to moderate hepatic impairment, the posology should not exceed 40 mg once daily.
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 hypokalaemia, they should be used with caution and with frequent monitoring of serum potassium.
The blood pressure lowering effect of telmisartan can be increased by concomitant use of other antihypertensive medicinal products.
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.
Clinical trial data has shown that dual blockade of the renin-angiotensin-aldosterone-system (RAAS) through the combined use of ACE-inhibitors, angiotensin II receptor blockers or aliskiren is associated with a higher frequency of adverse events such as hypotension, hyperkalaemia and decreased renal function (including acute renal failure) compared to the use of a single RAAS-acting agent.
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.
Co-administration of telmisartan with corticosteroids (systemic route) results in a decrease in the antihypertensive effect of telmisartan.
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.
Based on their pharmacological properties it can be expected that baclofen and amifostine may potentiate the hypotensive effects of all antihypertensives including telmisartan: baclofen, amifostine.
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.
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.
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.
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.
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:
Close monitoring of serum potassium in at risk patients is recommended.
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.
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.
As with other vasodilators, special caution is indicated in patients suffering from aortic or mitral stenosis, or obstructive hypertrophic cardiomyopathy.
In diabetic patients treated with insulin or antidiabetics, 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.
Symptomatic hypotension, especially after the first dose of telmisartan, 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. Volume and/or sodium depletion should be corrected prior to administration of telmisartan.
The use of angiotensin II receptor antagonists is not recommended during the first trimester of pregnancy. The use of angiotensin II receptor antagonists is contraindicated during the second and third trimesters of pregnancy.
There are no adequate data from the use of telmisartan in pregnant women. Studies in animals have shown reproductive toxicity.
Epidemiological evidence regarding the risk of teratogenicity following exposure to ACE inhibitors during the first trimester of pregnancy has not been conclusive; however a small increase in risk cannot be excluded. Whilst there is no controlled epidemiological data on the risk with angiotensin II receptor antagonists, similar risks may exist for this class of drugs. 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.
Exposure to angiotensin II receptor antagonist therapy 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). 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.
Because no information is available regarding the use of telmisartan during breast-feeding, telmisartan is not recommended and alternative treatments with better established safety profiles during breastfeeding are preferable, especially while nursing a newborn or preterm infant.
In preclinical studies, no effects of telmisartan on male and female fertility were observed.
When driving vehicles or operating machinery it should be taken into account that dizziness or drowsiness may occasionally occur when taking antihypertensive therapy such as telmisartan.
Serious adverse drug reactions include anaphylactic reaction and angioedema which may occur rarely (≥1/10,000 to <1/1,000), and acute renal failure.
The overall incidence of adverse reactions reported with telmisartan was usually comparable to placebo (41,4% vs 43.9%) in controlled trials in patients treated for hypertension. The incidence of adverse reactions was not dose related and showed no correlation with gender, age or race of the patients. The safety profile of telmisartan in patients treated for the reduction of cardiovascular morbidity was consistent with that obtained in hypertensive patients.
The adverse reactions listed below have been accumulated from controlled clinical trials in patients treated for hypertension and from post-marketing reports. The listing also takes into account serious adverse reactions and adverse reactions leading to discontinuation reported in three clinical long-term studies including 21,642 patients treated with telmisartan for the reduction of cardiovascular morbidity for up to six years.
Adverse reactions have been ranked under headings of frequency using the following convention: very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000). Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness.
Uncommon: Urinary tract infection including cystitis, upper respiratory tract infection including pharyngitis and sinusitis
Rare: Sepsis including fatal outcome1
Uncommon: Anaemia
Rare: Eosinophilia, thrombocytopenia
Rare: Anaphylactic reaction, hypersensitivity
Uncommon: Hyperkalaemia
Rare: Hypoglycaemia (in diabetic patients)
Uncommon: Insomnia, depression
Rare: Anxiety
Uncommon: Syncope
Rare: Somnolence
Rare: Visual disturbance
Uncommon: Vertigo
Uncommon: Bradycardia
Rare: Tachycardia
Uncommon: Hypotension2, orthostatic hypotension
Uncommon: Dyspnoea, cough
Very rare: Interstitial lung disease4
Uncommon: Abdominal pain, diarrhoea, dyspepsia, flatulence, vomiting
Rare: Dry mouth, stomach discomfort, dysgeusia
Rare: Hepatic function abnormal/liver disorder3
Uncommon: Pruritus, hyperhidrosis, rash
Rare: Angioedema (also with fatal outcome), eczema, erythema, urticaria, drug eruption, toxic skin eruption
Uncommon: Back pain (e.g. sciatica), muscle spasms, myalgia
Rare: Arthralgia, pain in extremity, tendon pain (tendinitis like symptoms)
Uncommon: Renal impairment including acute renal failure
Uncommon: Chest pain, asthenia (weakness)
Rare: Influenza-like illness
Uncommon: Blood creatinine increased
Rare: Haemoglobin decreased, blood uric acid increased, hepatic enzyme increased, blood creatine phosphokinase increased
1,2,3,4 for further descriptions, please see sub-section "Description of selected adverse reactions"
In the PRoFESS trial, an increased incidence of sepsis was observed with telmisartan compared with placebo. The event may be a chance finding or related to a mechanism currently not known.
This adverse reaction was reported as common in patients with controlled blood pressure who were treated with telmisartan for the reduction of cardiovascular morbidity on top of standard care.
Most cases of hepatic function abnormal/liver disorder from post-marketing experience occurred in Japanese patients. Japanese patients are more likely to experience these adverse reactions.
Cases of interstitial lung disease have been reported from post-marketing experience in temporal association with the intake of telmisartan. However, a causal relationship has not been established.
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