Receptor blocker-Several orally active non-peptide ...



Telmisartan Use in Hypertension Abstract: Telmisartan is used alone or in combination with other medications to treat high blood pressure. Telmisartan is also used to decrease the chance of heart attack, stroke, or death in people 55 years of age or older who are at high risk for cardiovascular disease. Telmisartan is in a class of medications called angiotensin II receptor antagonists. It works by blocking the action of certain natural substances that tighten the blood vessels, allowing the blood to flow more smoothly and the heart to pump more efficiently.Telmisartan is an angiotensin II receptor antagonist that is highly selective for type 1 angiotensin II receptors. It was significantly more effective than placebo in large (n >100), double-blind, randomised, multicentre clinical trials in patients with mild to moderate hypertension. Telmisartan 20 to 160mg once daily produced mean reductions in supine trough systolic blood pressure and diastolic blood pressure of up to 15.5 and 10.5mm Hg, respectively. Maximum blood pressure reduction occurred with a dosage of 40 to 80 mg/day.Telmisartan 40 to 120 mg/day was as effective as amlodipine 5 to 10 mg/day or atenolol 50 to 100 mg/day in dose-titration studies. Telmisartan 20 to 160 mg/day was generally similar in efficacy to enalapril 5 to 20 mg/day or lisinopril 10 to 40 mg/day in both titration-to-response and other studies. Hydrochlorothiazide was coadministered in most of the titration-to-response studies if patients remained hypertensive.Telmisartan 80 mg/day was more effective than submaximal dosages of losartan (50 mg/day) or valsartan (80 mg/day) and was as effective as a fixed-dose combination of losartan 50mg plus hydrochlorothiazide 12.5mg over the last 6 hours of the dosage interval and the whole 24-hour postdose interval. In patients with severe hypertension, telmisartan 80 to 160 mg/day was as effective as enalapril 20 to 40 mg/day (both agents could be titrated and combined sequentially with hydrochlorothiazide 25mg and amlodipine 5mg).The addition of hydrochlorothiazide to telmisartan was more effective than each agent alone at lowering blood pressure in patients with hypertension.Conclusion: Telmisartan is an effective antihypertensive agent with a tolerability profile similar to that of placebo. Comparative data have shown telmisartan to be as effective as other major classes of antihypertensive agents at lowering blood pressure. Compared with lisinopril, telmisartan is associated with a significantly lower incidence of dry, persistent cough. Therefore, telmisartan is a useful therapeutic option in the management of patients with hypertension.Receptor blocker-Several orally active non-peptide angiotensin II subtype 1 (AT1) receptor antagonists are now available for the treatment of hypertension. These agents have a common mechanism of action-blockade of the binding of angiotensin II to the subtype 1 receptor - and their binding to this receptor is generally insurmountable. There are some pharmacokinetic and pharmacodynamic differences between these antagonists, which may reflect in their clinical efficacy, especially at the end of the dosing interval. Losartan has an active metabolite that prolongs its duration of action, and candesartan cilexetil requires conversion to an active form after administration. Telmisartan has the longest duration of action, with a terminal elimination half-life of around 24 h in comparison with 11-15 h for irbesartan, the agent with the next longest half-life. The long duration of action and insurmountable binding to the receptor may be related to the slow dissociation kinetics of the antagonists from the AT1 receptor. Comparative clinical studies suggest that at the recommended dose losartan, the original drug in this class, has a lower efficacy than the newer agents, such as telmisartan. It is possible that these differences between angiotensin II receptor antagonists are due to variations in the degree and duration of receptor blockade, and may be of clinical significance with regard to the cardioprotective and renoprotective effects of this class of antihypertensive agents.Pharmacokinetics and Pharmacodynamics-As toxicology is a continuum of pharmacokinetics and pharmacodynamics, this is a review of recent advances on pharmacokinetics and physiologically-based pharmacokinetic (PBPK) modeling involving nanoparticles. We provide a synopsis of the state-of-the-science on the absorption, distribution, metabolism, and excretionangiotensin II mediates its haemodynamic effects by binding to specific cell-surface receptors. In humans, two receptor subtypes have been identified, designated AT1 and AT2. Because all major deleterious effects of angiotensin II are produced via binding to AT1-receptors, selective blockade of this receptor subtype should confer haemodynamic benefits, while allowing stimulation of the potentially beneficial effects mediated by AT2-receptors. Experimental studies using various models have consistently revealed marked differences in the receptor binding properties of different AT1-receptor blockers. The relative receptor binding affinities of currently available AT1-receptor blockers is candesartan > irbesartan > valsartan/EXP-3174/telmisartan > tasosartan > losartan > eprosartan. Candesartan is also released from the receptor more slowly than other available AT1-receptor blockers, with a half-life of approximately 152 min for the receptor-blocker complex, compared with 31 min for EXP-3174, 17 min for irbesartan and 5 min for losartan. Candesartan therefore binds to the AT1-receptor more tightly and more persistently than other AT1-receptor blockers.Active Pharma Ingredients (API) TELSARTAN ?TELMISARTAN Cardiac TELSARTAN-AM ?AMLODIPINE + OTHERS Cardiac TELSARTAN-H ?TELMISARTAN + HCT Cardiac TELSARTAN-R ?TELMISARTAN+RAMIPRIL CardiacDose response and safety of telmisartan in patients with mild to moderate hypertensionThis randomized, double-blind, double-dummy, placebo-controlled, parallel-group study evaluated the dose-response relationship of telmisartan in 207 patients with mild to moderate hypertension (diastolic blood pressure [DBP] 100 to 114 mmHg). After a 28-day placebo run-in period, patients were randomized to 28 days of once-daily, double-blind, double-dummy treatment with telmisartan 40, 80, or 120 mg; enalapril 20 mg; or placebo. Blood pressure (BP) was manually recorded for 12 hours after the first dose and after 24 hours at baseline (Day 0), Day 1, and Day 28 of double-blind treatment. Pharmacokinetic and pharmacodynamic parameters were assessed from telmisartan plasma concentrations. All doses of telmisartan and enalapril significantly reduced BP compared with placeboBP reductions after 4 weeks of treatment with telmisartan were no different from those achieved with enalapril. No significant linear trend in BP reduction was evident among telmisartan doses. Reductions in SBP and DBP were maintained over the 24-hour period at Day 28. Treatment did not affect supine heart rate.Dosage Adult: PO Initial: 40 mg once daily. Max: 80 mg/day.Administration May be taken with or without food.Medial Serve for TELMISARTAN molecule Products on KARVE road medicals dated 22nov2011. Dr. LIST ON KARVE ROADDr.Nilesh KulkarniDr.Sudhir Mundle Dr.Anand Siya (MBBS)Dr.AgrawalDr.RaneDr. PhatakeDr. ShendgekarDr.Prathiba PhadkeDr.A. BapatDr.JavdekarDr. BhattSTOKIST-Nitin AnandKundanTapdiaPrasad RaviMaharashtraAmar agenciesArun ShahaMEDICAL ON KARVE ROADSai Shradha MedicalMahesh MedicalPulse MedicalAshwini MedicalSanjay medicalShriram MedicalNew Bharti MedicalReliff medicalSwami Vivekanand Medical Varad MedicalMedicine Point Pooja medicalsMaharashtra MedicalChaitali MedicalJeevanJyoti MedicalArihant chemistNiaa aushadh BazzarMayur MedicalAnish MedicalMedicare ChemistChintamani MedicoRegal ChemistMetro MedicalRelif medicalSwaroop MedicalReligare MedicalAnand MedicalVarad MedicalMedi-Plus Pooja drugsShankar MedicalMAIN COMPETATORS FOR TELSARTAN BRANDSTELVAS - ABBOTTTELMIKIND - MANKINDTELMA - GLENMARKTELISTA - LUPINPRICE LIST TELSRTAN PRODUCT telsarTAN tab Telmisartan 20mg DR. REDDY'S LABS 1551.75telsarTAN tab Telmisartan 40mg DR. REDDY'S LABS 15109.50TELSARTAN tab Telmisartan 80mg DR. REDDY'S LABS 10 119.00telsarTAN-am tab Telmisartan 40mg, amlodipine 5mg DR. REDDY'S LABS 10 85.50telsarTAN-ATR tab Telmisartan 20mg, atorvastatin 10mg DR. REDDY'S LABS 10 90.00TELSARTAN-H tab Telmisartan 80mg, hydrochlorothiazide 12.5mg DR. REDDY'S LABS 15137.70TELSARTAN-H tab Telmisartan 40mg, hydrochlorothiazide 12.5mg DR. REDDY'S LABS 10 124.80TELSARTAN-R tab Telmisartan 40mg, ramipril 2.5mg DR. REDDY'S LABS 10 77.00TELSARTAN-R tab Telmisartan 40mg, ramipril 5mg DR. REDDY'S LABS 10 102.00Telma - Glenmark (Zoltan) [Telmisartan] StrengthVolumePresentationPrice* ??Telma 20mg10Telma TAB38.90???Telma 40mg10Telma TAB71.00???Telma 80mg10Telma TAB119.40????Telma- H - Glenmark (Zoltan) [Telmisartan] CombinationVolumePresentationPrice* ??Telma- H Telmisartan 40mg,Hydrochlorothiazide12.5mg10Telma- H TAB???Telma- R - Glenmark (Zoltan) [Telmisartan] CombinationVolumePresentationPrice* ??Telma- R Telmisartan 40mg,Ramiroil 5mg10Telma- R TAB???Telma- R Telmisartan 40mg,Ramiroil 5mg10Telma- R TAB???MONTHLY SALE TELMISARTAN MOLECULE STRIP PER MONTH(approximately)TELSARTAN Dr.Reddys220TELMA Glenmark303TELVAS ABBOTT58 Note- Blue - Telma Orange – Telsartan Green - TelvasCONCLUSION-Rx status outsideResidential Dr. Not availableNo scheme for productPrice is much more comparative to other main competators ................
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