Peringatan Keamanan

Intravenous LD50 in rats is 150-200 mg/kg in males and 200 to 250 mg/kg in females. Acute oral toxicity is low: no deaths and no changes occurred in rats or dogs at 2000 mg/kg, the highest dose tested.L44662 Limited data are available with regard to overdosage in humans. The most likely manifestations of overdosage with telmisartan would be hypotension, dizziness and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation. Supportive treatment should be instituted if symptomatic hypotension occurs. Telmisartan is not removed by hemofiltration and is not dialyzable.L44652

Telmisartan

DB00966

small molecule approved investigational

Deskripsi

Telmisartan is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. Generally, angiotensin II receptor blockers (ARBs) such as telmisartan bind to the angiotensin II type 1 (AT1) receptors with high affinity, causing inhibition of the action of angiotensin II on vascular smooth muscle, ultimately leading to a reduction in arterial blood pressure.A1489,A1490 Recent studies suggest that telmisartan may also have PPAR-gamma agonistic properties that could potentially confer beneficial metabolic effects.A1492

Struktur Molekul 2D

Berat 514.6169
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Telmisartan displays bi-exponential decay kinetics with a terminal elimination half-life of approximately 24 hours.[L44652]
Volume Distribusi Telmisartan has a volume of distribution of approximately 500 liters.[L44652]
Klirens (Clearance) Telmisartan has a total plasma clearance of >800 mL/min.[L44652]

Absorpsi

Oral telmisartan follows nonlinear pharmacokinetics over the dose range of 20 mg to 160 mg. Both Cmax and AUC present greater than proportional increases at higher doses. With once-daily dosing, telmisartan has trough plasma concentrations of about 10% to 25% of peak plasma concentrations. The absolute bioavailability of telmisartan depends on the dosage. At 40 mg and 160 mg, the bioavailability was 42% and 58%, respectively. Food slightly decreases bioavailability. For instance, when the 40 mg dose is administered with food, a decrease of about 6% is seen, and with the 160 mg dose, there is a decrease of about 20%.L44652

Metabolisme

Minimally metabolized by conjugation to form a pharmacologically inactive acyl-glucuronide, the glucuronide of the parent compound is the only metabolite that has been identified in human plasma and urine. The cytochrome P450 isoenzymes are not involved in the metabolism of telmisartan.L44652

Rute Eliminasi

Following either intravenous or oral administration of 14C-labeled telmisartan, most of the administered dose (>97%) was eliminated unchanged in feces via biliary excretion; only minute amounts were found in the urine (0.91% and 0.49% of total radioactivity, respectively).L44652

Interaksi Makanan

1 Data
  • 1. Take with or without food. Bioavailability may be slightly reduced by taking telmisartan with food.

Interaksi Obat

1017 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Telmisartan is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Telmisartan is combined with Levodopa.
Risperidone Telmisartan may increase the hypotensive activities of Risperidone.
Troglitazone Troglitazone may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Reserpine Reserpine may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Progesterone Progesterone may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Chlorpromazine Chlorpromazine may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Cimetidine Cimetidine may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Bosentan Bosentan may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Tipranavir Tipranavir may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Ethinylestradiol Ethinylestradiol may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Glyburide Glyburide may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Ketoconazole Ketoconazole may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Fusidic acid Fusidic acid may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Simeprevir Simeprevir may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Lenvatinib Lenvatinib may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Valinomycin Valinomycin may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Erythromycin Erythromycin may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Quinidine Quinidine may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Nifedipine Telmisartan may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Telmisartan.
Alfuzosin Alfuzosin may increase the hypotensive activities of Telmisartan.
Aliskiren The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Telmisartan.
Amifostine Telmisartan may increase the hypotensive activities of Amifostine.
Canagliflozin The risk or severity of hypotension, hyperkalemia, and reduced intravascular volume can be increased when Canagliflozin is combined with Telmisartan.
Diazoxide Diazoxide may increase the hypotensive activities of Telmisartan.
Drospirenone The risk or severity of hyperkalemia can be increased when Telmisartan is combined with Drospirenone.
Eplerenone The risk or severity of hyperkalemia can be increased when Eplerenone is combined with Telmisartan.
Semuloparin The risk or severity of hyperkalemia can be increased when Semuloparin is combined with Telmisartan.
Lithium citrate The serum concentration of Lithium citrate can be increased when it is combined with Telmisartan.
Lithium carbonate The serum concentration of Lithium carbonate can be increased when it is combined with Telmisartan.
Lithium hydroxide The serum concentration of Lithium hydroxide can be increased when it is combined with Telmisartan.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Telmisartan.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Telmisartan.
Obinutuzumab Telmisartan may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Telmisartan.
Rituximab Telmisartan may increase the hypotensive activities of Rituximab.
Tolvaptan The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Telmisartan.
Trimethoprim The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Telmisartan.
Desmopressin Desmopressin may decrease the antihypertensive activities of Telmisartan.
Phentermine Phentermine may decrease the antihypertensive activities of Telmisartan.
Midodrine Midodrine may decrease the antihypertensive activities of Telmisartan.
Isoetharine Isoetharine may decrease the antihypertensive activities of Telmisartan.
Methysergide Methysergide may decrease the antihypertensive activities of Telmisartan.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Telmisartan.
Etomidate Etomidate may decrease the antihypertensive activities of Telmisartan.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Telmisartan.
Dihydroergotamine Dihydroergotamine may decrease the antihypertensive activities of Telmisartan.
Protriptyline Protriptyline may decrease the antihypertensive activities of Telmisartan.
Methylergometrine Methylergometrine may decrease the antihypertensive activities of Telmisartan.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Telmisartan.
Mirtazapine Mirtazapine may decrease the antihypertensive activities of Telmisartan.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Telmisartan.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Telmisartan.
Promazine Promazine may decrease the antihypertensive activities of Telmisartan.
Droperidol Droperidol may decrease the antihypertensive activities of Telmisartan.
Buspirone Buspirone may decrease the antihypertensive activities of Telmisartan.
Nortriptyline Nortriptyline may decrease the antihypertensive activities of Telmisartan.
Amoxapine Amoxapine may decrease the antihypertensive activities of Telmisartan.
Doxapram Doxapram may decrease the antihypertensive activities of Telmisartan.
Lisuride Lisuride may decrease the antihypertensive activities of Telmisartan.
Metaraminol Metaraminol may decrease the antihypertensive activities of Telmisartan.
Trazodone Trazodone may decrease the antihypertensive activities of Telmisartan.
Epinephrine Epinephrine may decrease the antihypertensive activities of Telmisartan.
Ergotamine Ergotamine may decrease the antihypertensive activities of Telmisartan.
Nicergoline Nicergoline may decrease the antihypertensive activities of Telmisartan.
Methoxamine Methoxamine may decrease the antihypertensive activities of Telmisartan.
Propiomazine Propiomazine may decrease the antihypertensive activities of Telmisartan.
Alfentanil Alfentanil may decrease the antihypertensive activities of Telmisartan.
Fentanyl Fentanyl may decrease the antihypertensive activities of Telmisartan.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Telmisartan.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Telmisartan.
Dobutamine Dobutamine may decrease the antihypertensive activities of Telmisartan.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Telmisartan.
Benzphetamine Benzphetamine may decrease the antihypertensive activities of Telmisartan.
Ritodrine Ritodrine may decrease the antihypertensive activities of Telmisartan.
Terbutaline Terbutaline may decrease the antihypertensive activities of Telmisartan.
Bitolterol Bitolterol may decrease the antihypertensive activities of Telmisartan.
Almotriptan Almotriptan may decrease the antihypertensive activities of Telmisartan.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Telmisartan.
Salmeterol Salmeterol may decrease the antihypertensive activities of Telmisartan.
Naratriptan Naratriptan may decrease the antihypertensive activities of Telmisartan.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Telmisartan.
Dopamine Dopamine may decrease the antihypertensive activities of Telmisartan.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Telmisartan.
Albuterol Salbutamol may decrease the antihypertensive activities of Telmisartan.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Telmisartan.
Ergoloid mesylate Ergoloid mesylate may decrease the antihypertensive activities of Telmisartan.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Telmisartan.
Arbutamine Arbutamine may decrease the antihypertensive activities of Telmisartan.
Dutasteride Dutasteride may decrease the antihypertensive activities of Telmisartan.
Desipramine Desipramine may decrease the antihypertensive activities of Telmisartan.
Pergolide Pergolide may decrease the antihypertensive activities of Telmisartan.
Finasteride Finasteride may decrease the antihypertensive activities of Telmisartan.
Ergometrine Ergometrine may decrease the antihypertensive activities of Telmisartan.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Telmisartan.
Arformoterol Arformoterol may decrease the antihypertensive activities of Telmisartan.

Target Protein

Peroxisome proliferator-activated receptor gamma PPARG
Type-1 angiotensin II receptor AGTR1

Referensi & Sumber

Synthesis reference: Kumar AS, Ghosh S, Mehta GN: Efficient and improved synthesis of Telmisartan. Beilstein J Org Chem. 2010 Mar 11;6:25. Pubmed(http://www.ncbi.nlm.nih.gov/pubmed/20502601).
Artikel (PubMed)
  • PMID: 11558835
    Sharpe M, Jarvis B, Goa KL: Telmisartan: a review of its use in hypertension. Drugs. 2001;61(10):1501-29.
  • PMID: 12462282
    Smith DH: Treatment of hypertension with an angiotensin II-receptor antagonist compared with an angiotensin-converting enzyme inhibitor: a review of clinical studies of telmisartan and enalapril. Clin Ther. 2002 Oct;24(10):1484-501.
  • PMID: 20448797
    Galzerano D, Capogrosso C, Di Michele S, Galzerano A, Paparello P, Lama D, Gaudio C: New standards in hypertension and cardiovascular risk management: focus on telmisartan. Vasc Health Risk Manag. 2010 Mar 24;6:113-33.
  • PMID: 22429010
    Balakumar P, Bishnoi HK, Mahadevan N: Telmisartan in the management of diabetic nephropathy: a contemporary view. Curr Diabetes Rev. 2012 May;8(3):183-90. doi: 10.2174/157339912800563972.

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