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Cardiovascular Drugs
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: Aliskiren is contraindicated during the 2nd and 3rd Trimesters because the animal reproduction studies showed a profound potentiality of teratogenicity and severe fetal toxicity associated with its use during this period.
2018 ESC/ESH Guidelines for the Management of Arterial Hypertension
Published in Giuseppe Mancia, Guido Grassi, Konstantinos P. Tsioufis, Anna F. Dominiczak, Enrico Agabiti Rosei, Manual of Hypertension of the European Society of Hypertension, 2019
Bryan Williams, Giuseppe Mancia, Wilko Spiering, Enrico Agabiti Rosei, Michel Azizi, Michel Burnier, Denis L. Clement, Antonio Coca, Giovanni de Simone, Anna F. Dominiczak, Thomas Kahan, Felix Mahfoud, Josep Redon, Luis M. Ruilope, Alberto Zanchetti, Mary Kerins, Sverre E. Kjeldsen, Reinhold Kreutz, Stéphane Laurent, Gregory Y.H. Lip, Richard McManus, Krzysztof Narkiewicz, Frank Ruschitzka, Roland E. Schmieder, Evgeny Shlyakhto, Konstantinos P. Tsioufis, Victor Aboyans, Ileana Desormais
Both ACE inhibitors and ARBs are among the most widely used classes of antihypertensive drugs. They have similar effectiveness [295,296] as each other and other major drug classes on major cardiovascular events and mortality outcomes [2,292]. ARBs are associated with significantly lower treatment discontinuation rates for adverse events than those of all other antihypertensive therapies [297], and similar rates to placebo [294]. ACE inhibitors and ARBs should not be combined for the treatment of hypertension because there is no added benefit on outcomes and an excess of renal adverse events [298,299]. Dual combination of RAS blockers also led to the premature cessation of another trial due to adverse events [291], when a renin inhibitor, aliskiren, was combined with either an ACE inhibitor or an ARB in people with diabetes. This result halted further research into the clinical utility of aliskiren for BP treatment.
Cardiovascular drug therapy in the elderly
Published in Wilbert S. Aronow, Jerome L. Fleg, Michael W. Rich, Tresch and Aronow’s Cardiovascular Disease in the Elderly, 2019
William H. Frishman, Wilbert S. Aronow, Angela Cheng-Lai
Aliskiren is a non-peptide direct renin inhibitor, and is the first drug of this class to be approved for clinical use in systemic hypertension (see also Chap Systemic Hypertension in the Elderly) (105). The drug is approved for once daily use as a monotherapy and for combination use with other antihypertensive drugs.
Asymmetric organocatalysis in drug discovery and development for active pharmaceutical ingredients
Published in Expert Opinion on Drug Discovery, 2023
Aliskiren (Rasilez®) is an anti-hypertensive drug that was developed by Novartis, in 2007. An asymmetric organocatalytic method was reported by this company [34]. The Jørgensen-Hayashi diphenylprolinol silyl ether 3 was used at a reasonably low loading of 8 mol% in a key Michael reaction between isovaleraldehyde 1 and nitroethene (generated in situ from the benzoate ester nitro precursor 2) (Figure 2 a). The procedure mentioned in this patent was run on a multi-gram scale. This was followed by a sodium borohydride reduction to give the key nitroalcohol adduct 4 as the (S)-enantiomer with an ee of 93% (no yield was given). This adduct was then transformed into the API target in several steps (Figure 2, a). This synthetic pathway involves a key Boc-protected lactone-lactam intermediate 5. The prolinol catalyst 3 formed a reactive enamine nucleophile which combined with the in situ generated Michael acceptor to form the adduct 4. A very recent report by Hayashi clearly illustrates the main advantages of the use of the Jørgensen-Hayashi diphenylprolinol silyl ether catalyst for targeting many API molecules [35] (also see below).
Interactions of antiepileptic drugs with drugs approved for the treatment of indications other than epilepsy
Published in Expert Review of Clinical Pharmacology, 2020
Kinga K. Borowicz-Reutt, Stanisław J. Czuczwar, Marta Rusek
In addition, Łukawski et al. found that aliskiren, a piperidine derivative used in unresponsive to, or intolerant of other antihypertensives patients [147], can affect the anticonvulsant activity of AEDs [153]. Specifically, it enhanced the anticonvulsant action of clonazepam and valproate against MES-induced seizures; however, the reaction was pharmacokinetic. Moreover, the co-administration of aliskiren with clonazepam resulted in motor impairment. Combinations of this antihypertensive drug with several additional AEDs (carbamazepine, phenobarbital, oxcarbazepine, lamotrigine, topiramate, and pregabalin) remained neutral regarding the seizure activity. However, a combined treatment of aliskiren with phenobarbital induced impairment of long-term memory [153]. Moreover, the anticonvulsant activity of clonazepam, phenobarbital, or valproate was potentiated against PTZ-induced convulsions in mice [175], but the adverse effects were not associated in terms of motor coordination and long-term memory [175].
Immunomodulatory properties of antihypertensive drugs and digitalis glycosides
Published in Expert Review of Cardiovascular Therapy, 2022
Paweł Bryniarski, Katarzyna Nazimek, Janusz Marcinkiewicz
Aliskiren is a renin inhibitor. It is used for the triple blockade of the renin-angiotensin-aldosterone system (RAA) in combination with drugs from a group of angiotensin converting enzyme inhibitors and angiotensin receptor inhibitors. The potency of the antihypertensive effect of aliskiren is comparable to that of angiotensin converting enzyme inhibitors [121]. Aliskiren has side effects similar to all drugs that affect the RAA system, i.e. facial swelling, elevated uric acid levels, gout attacks, hyperkalemia, diarrhea, and shortness of breath. Aliskiren reduces TNF-alpha expression in cultured endothelial cells [122]. In patients with chronic kidney disease, aliskiren reduces TGF-β1 concentrations [123].