Active Substance: Aliskiren (as hemifumarate).
Overview
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This medicine contains an important and useful components, as it consists of
Aliskiren (as hemifumarate)is available in the market in concentration
Aliskiren
- Aliskiren should be used with caution in patients with a history of hypotension, as it can cause a further reduction in blood pressure, especially when starting treatment or when combined with other antihypertensive medications. - It should be monitored in patients with kidney dysfunction, as aliskiren has the potential to worsen renal function, especially in those with pre-existing conditions. - Use with caution in patients who are elderly or frail, as they may be more prone to experiencing adverse effects, particularly hypotension or renal dysfunction. - Aliskiren may cause hyperkalemia (high potassium levels), and potassium levels should be monitored regularly, especially in patients with diabetes, kidney disease, or those on other medications that raise potassium levels (e.g., ACE inhibitors, ARBs, potassium-sparing diuretics). - Caution should be exercised in patients with a history of angioedema (swelling of the deeper layers of the skin), as there is an increased risk of this condition with the use of aliskiren. - Aliskiren is not recommended for use during pregnancy, as it can harm the fetus, particularly during the second and third trimesters. It should be discontinued if pregnancy is confirmed. - Patients taking aliskiren should avoid using it concurrently with ACE inhibitors or angiotensin receptor blockers (ARBs) in patients with diabetes, as this combination increases the risk of kidney impairment, low blood pressure, and elevated potassium levels.
- Aliskiren is primarily indicated for the treatment of hypertension (high blood pressure). It works by inhibiting renin, a key enzyme in the renin-angiotensin-aldosterone system (RAAS), which helps to regulate blood pressure. - It is used either alone or in combination with other antihypertensive medications for better blood pressure control. - Aliskiren may also be considered in the management of patients with cardiovascular diseases that require blood pressure control to prevent complications, although it is not typically used as a first-line treatment. - It is used in patients with essential hypertension who need more effective blood pressure management when lifestyle changes alone do not suffice. - Aliskiren may have potential off-label use in conditions where controlling blood pressure is essential, but its primary indication remains for hypertension.
- Aliskiren is contraindicated in patients with a known hypersensitivity or allergy to the drug or any of its components. - It is contraindicated in patients who are pregnant, particularly in the second and third trimesters, due to the risk of harm to the fetus. - Aliskiren should not be used in combination with ACE inhibitors or ARBs in patients with diabetes, as this combination has been associated with an increased risk of kidney problems, hyperkalemia, and hypotension. - The drug is contraindicated in patients with a history of angioedema, especially if it was induced by an ACE inhibitor, ARB, or similar medication. - Aliskiren is contraindicated in patients with severe renal impairment (creatinine clearance <30 mL/min) or those with a history of significant renal disease, as it may further compromise kidney function. - It is also contraindicated in patients with moderate to severe hepatic impairment due to the limited data on the safety and efficacy in this population.
- Common side effects of aliskiren include dizziness, fatigue, and headache, which are typically mild and may improve over time. - A frequent side effect is hyperkalemia (elevated potassium levels), which can lead to dangerous heart arrhythmias if not addressed. Potassium levels should be regularly monitored. - Renal dysfunction or worsening kidney function can occur, especially in patients with pre-existing kidney disease or those taking other medications that affect renal function. - Aliskiren may cause hypotension, especially when initiating therapy or in combination with other antihypertensive drugs. Symptoms of low blood pressure can include lightheadedness, fainting, or dizziness. - Angioedema (swelling, usually in the face or throat) is a rare but serious side effect that requires immediate medical attention. - Gastrointestinal side effects, such as diarrhea, nausea, and abdominal pain, may occur but are generally less common. - Some individuals may experience fatigue, back pain, or respiratory symptoms such as cough. - Allergic reactions, including rash or itching, may also occur, though they are not common. - In rare cases, aliskiren can cause liver enzyme abnormalities or other liver-related issues, though this is infrequent.
4
- Aliskiren works by directly inhibiting renin, a key enzyme in the renin-angiotensin-aldosterone system (RAAS). Renin plays a central role in regulating blood pressure and fluid balance by converting angiotensinogen into angiotensin I. - By inhibiting renin, aliskiren reduces the formation of angiotensin I, which in turn leads to a decrease in the production of angiotensin II, a potent vasoconstrictor. This results in dilation of blood vessels and a reduction in blood pressure. - In addition to its vasodilatory effects, aliskiren also reduces aldosterone secretion, which helps prevent fluid retention and further lowers blood pressure. - Since aliskiren blocks the very first step in the RAAS pathway, its effect is more comprehensive than that of ACE inhibitors or angiotensin receptor blockers (ARBs), which target later steps in the pathway. - The result is an overall reduction in blood pressure, particularly effective in patients with essential hypertension. - Aliskiren's actions are dose-dependent, with higher doses providing greater antihypertensive effects, although the risk of side effects may also increase with higher doses.
- Aliskiren can interact with other antihypertensive drugs, such as ACE inhibitors, ARBs, and diuretics, leading to an increased risk of hypotension, hyperkalemia, and renal dysfunction, especially in patients with diabetes or kidney problems. - Concurrent use of aliskiren with potassium-sparing diuretics, potassium supplements, or salt substitutes containing potassium can increase the risk of hyperkalemia. - The combination of aliskiren with non-steroidal anti-inflammatory drugs (NSAIDs) may reduce its antihypertensive effect and increase the risk of kidney dysfunction. - Aliskiren may increase the blood levels of other medications metabolized by the cytochrome P450 system, potentially altering their efficacy. Close monitoring is required when combining aliskiren with drugs like ciclosporin, ketoconazole, or other CYP450 inhibitors. - Drugs that affect the renin-angiotensin-aldosterone system (RAAS), such as ACE inhibitors and ARBs, should not be used together with aliskiren in patients with diabetes due to an increased risk of renal impairment and hyperkalemia. - Aliskiren may interact with certain blood pressure-lowering agents like beta-blockers, calcium channel blockers, or alpha-blockers, and while the combination may be effective, close monitoring for side effects such as hypotension is recommended.
C (1st trimester), D (2nd & 3rd trimesters)
- The recommended starting dose of aliskiren for the treatment of hypertension is 150 mg once daily. - If blood pressure is not adequately controlled after 2-4 weeks, the dose may be increased to 300 mg once daily. - Aliskiren should be taken at the same time each day, with or without food, to maintain a consistent therapeutic level. - The maximum recommended dose is 300 mg once daily. - Dose adjustments may be required in patients with renal or hepatic impairment, and it should be prescribed cautiously in these populations.
- Aliskiren is not approved for use in pediatric patients (under the age of 18) and its safety and efficacy in children have not been established. - Therefore, no pediatric dosage recommendations are available, and aliskiren should not be used in children.
- For patients with mild renal impairment (creatinine clearance ≥60 mL/min), the usual dose of aliskiren (150-300 mg daily) is typically considered safe. - In patients with moderate renal impairment (creatinine clearance 30-60 mL/min), aliskiren can still be used, but it should be started at the lowest dose and adjusted based on blood pressure and renal function. - Aliskiren is contraindicated in patients with severe renal impairment (creatinine clearance <30 mL/min) due to the increased risk of adverse effects, including worsening kidney function. - Renal function should be monitored regularly in patients with any degree of renal impairment during aliskiren therapy.
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