Losartan

Abstract

Losartan (Cozaar) is an angiotensin AT1 receptor antagonist. It is approved in numerous countries for the treatment of hypertension and has been approved in the UK, the US and several European countries for stroke risk reduction in patients with hypertension and left ventricular hypertrophy (LVH). Losartan is recommended for use alone or with hydrochlorothiazide, but it can also be administered with other antihypertensive medications. In patients with hypertension, losartan effectively lowers blood pressure and also leads to regression of LVH. In the large, well designed LIFE (Losartan Intervention For Endpoint reduction in hypertension) study in patients with hypertension and LVH, losartan was more effective than atenolol in reducing the composite primary endpoint of cardiovascular (CV) mortality, stroke or myocardial infarction (MI). This was mainly due to a significant 25% reduction in the risk of stroke in the losartan group. Losartan recipients also had a significantly lower incidence of new-onset diabetes mellitus compared with atenolol recipients. Similar benefits were observed in several patient subgroups from the LIFE study, but not in the subgroup of Black patients. Losartan is well tolerated and is a cost effective alternative to atenolol in the setting of stroke reduction. Comparative data on clinical outcomes in hypertensive patients for losartan versus other antihypertensive agents would be of interest. Nonetheless, in addition to its established antihypertensive and end organ effects, the LIFE study indicates that, with the possible exception of Black patients, losartan can reduce the risk of stroke in patients with hypertension and LVH.

Coronavirus Pandemic—Therapy and Vaccines

“…It is therefore necessary to develop mAbs with specific binding affinity to the SARS-CoV-2 receptor-binding domain. Another tentative approach comprises the evaluation of existing angiotensin receptor 1 (ATR1) blockers such as losartan, commonly used for the treatment of hypertension [108], for a reduction in aggressiveness and mortality from SARS-CoV-2 infections [115]. The approach is based on the finding that ACE2 most likely represents the binding site for both SARS-CoV and SARS-CoV-2, thereby providing a sensible target for therapeutic interventions for coronavirus infections.…”

Coronavirus Pandemic: Treatment and Future Prevention

“…Another approach, which also could be described as a repurposing drug relates to existing AT1R blockers such as losartan, successfully used for hypertension treatment [ 51 ]. AT1R is a valid target as ACE2, which activates AT1R by cleavage of angiotensin I, serves as the binding site for both SARS-CoV and SARS-CoV-2 [ 72 ].…”

Design and Evaluation of Losartan Potassium Effervescent Floating Matrix Tablets: In Vivo X-ray Imaging and Pharmacokinetic Studies in Albino Rabbits

“…Several approaches/mechanisms have been attempted to attain controlled GRT in GRDDS, such as flotation [ 7 ], super-porous hydrogels [ 8 ], mucoadhesion [ 9 ], swellable and expansion systems [ 10 ], ion exchange resins [ 11 ], bioadhesive systems [ 12 ], low-density systems [ 13 ], erosion systems [ 14 ], modified shape systems [ 15 ], in situ gelling systems [ 16 ], and raft-forming systems [ 16 , 17 ]. Losartan potassium (LP) is the primary member of the new category of non-peptide angiotensin 2 receptor antagonists [ 18 ]. It significantly lowers the blood pressure through blocking the rennin–angiotensin pathway by reducing the angiotensin II receptor site.…”

“…It has a short biological half-life of 2 h and its bioavailability is just 32% [ 19 ]. It undergoes a quick first-pass metabolism [ 18 , 19 ]. It was therefore chosen as the model drug for the FDDS.…”