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Although aliskiren is not the first drug in this class, it is a newcomer in the world of heart failure therapy. Unlike its ancestors, aliskiren is evidence-based and is not considered a substitute for ACE inhibitors. It will likely find a niche as an addition to ACE inhibitors, especially in patients who cannot tolerate or are uncontrolled by conventional treatment. In addition, its guideline is simple, as the results are easily interpreted as low plasma renin.
Among its major characteristics, aliskiren has a low bioavailability and a 24 hour accumulation half-life. Therefore, the drug reaches its steady state blood levels within seven to eight days. In addition, peak plasma concentrations of aliskiren are reached within one to three hours of administration. When aliskiren is taken with high-fat meals, the drug concentrations decrease by up to 71% or 85%. The drug is best administered without regard to meals.
In clinical trials, aliskiren has a low to moderate effect on blood pressure. However, it may also cause other side effects, including lightheadedness and fainting. Hence, it is advisable to consult a doctor before using aliskiren. Although it is a very effective blood pressure-lowering drug, it should not be taken if you are taking an angiotensin-converting enzyme inhibitor. The medication should be stored tightly, out of the reach of children. Moreover, it should not be taken while pregnant or breastfeeding.
Compared to other blood pressure-lowering drugs, aliskiren reduces both systolic and diastolic blood pressures. One study even showed a significant reduction in sitting systolic blood pressure after discontinuing aliskiren treatment. In addition, the drug's antihypertensive effect was also observed in patients with mild-to-moderate hypertension. Thus, aliskiren is a useful treatment option for hypertension patients, and it is gaining popularity among a variety of patient populations.
This treatment option was initially approved in 2004 for the treatment of high blood pressure. In recent years, it has been widely used to reduce the risk of heart attacks and strokes. In fact, it is one of the first drugs on the market that can reduce blood pressure levels in patients with hypertension. But there is a major downside to aliskiren, too. It has a low rate of side effects and is safe to use.
Another issue that limits aliskiren's effectiveness is the fact that it increases PRC (prorenin concentration) more than any other drug in the anti-renin system class. Because of this, aliskiren's low bioavailability has led to limited efficacy in previous trials. But aliskiren's subnanomolar affinity for the renin enzyme compensates for the low plasma concentration.
Patients with congestive heart failure who failed to respond to enalapril or a placebo were excluded from the study. However, aliskiren was not superior to enalapril in terms of time to first cardiovascular event, the composite endpoint of which included cardiovascular death, nonfatal myocardial infarction, or unplanned hospitalization for heart failure. However, the presence of a greater incidence of adverse reactions in elderly patients cannot be excluded.
Other side effects of aliskiren include low sodium levels, headache, confusion, and severe weakness. The drug is also known to cause fetal oligohydramnios, although fetal testing may be required for this condition. Some cases of oligohydramnios in infants may not be detected until irreversible damage has occurred. Regardless of the time of exposure, infants exposed to aliskiren should be monitored closely for signs of hypotension, hyperkalemia, and oliguria. Dialysis may be required for the child's disordered renal function.
Another important side effect of aliskiren is diarrhea. In a study, aliskiren monotherapy was associated with a normalized daytime ambulatory BP in six out of 17 patients. However, this increased BP in a fifth of patients, and a significant proportion of patients were considered uncontrolled. The drug should be taken as prescribed by a healthcare provider. Moreover, it should be stored at a room temperature of 59 to 86 degF (15-30 degC).
However, there are still many important caveats to be considered before prescribing aliskiren for hypertension. For example, aliskiren induces large reactive increases in renin secretion, far greater than that of other antihypertensive drugs. Researchers will need to clarify the nature of these responses in order to identify ways to control aliskiren's effect, or eliminate them altogether. But the long-term benefits of aliskiren are still a matter of debate.
The renin inhibitors also reduce the negative feedback effect on ANG II by decreasing the activity of secreted renin. In some cases, aliskiren can even reduce the negative effects of ang II on blood pressure. Because it occupies the active cleft of secreted renin, aliskiren is considered a renin inhibitor that inhibits the activity of renin. For this reason, aliskiren is an effective treatment for hypertension and has numerous potential benefits.