aliskiren

medtigo

aliskiren

Brand Name :

Tekturna

Synonyms :

aliskiren

Class :

Renin- inhibitors

Action and Spectrum

Actions and Spectrum:

aliskiren is a direct renin inhibitor that acts by selectively inhibiting the activity of renin, the enzyme responsible for the conversion of angiotensinogen to angiotensin I in the renin-angiotensin-aldosterone system (RAAS).

The spectrum of aliskiren’s action is primarily focused on the management of hypertension. As a renin inhibitor, aliskiren effectively lowers the BP of individual.

Dosing & Uses

Drug Interaction

Adverse Reaction

Frequency defined

Adults

1-10%

Rash (1%)

Increase in serum creatinine (<7%)

Diarrhea (2.3%)

Cough (1.1%)

Hyperkalemia (<1%)

<1%

Severe hypotension

Rhabdomyolysis

Toxic epidermal necrolysis

Increase in uric acid

Angina

Angioedema

Headache

Gout

Renal stones

Seizure

Black Box Warning

Black Box Warning:

Fetal Toxicity: aliskiren should not be used during pregnancy. Use of aliskiren during pregnancy can cause fetal harm or death.

Renal Impairment: aliskiren is contraindicated in patients with severe renal impairment (estimated glomerular filtration rate [eGFR] <30 mL/min/1.73 m²) and should be used with caution in patients with moderate renal impairment (eGFR <60 mL/min/1.73 m²).

Dual Renin-Angiotensin-Aldosterone System (RAAS) Blockade: Concomitant use of aliskiren with other drugs that block the RAAS, such as angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor blockers (ARBs), or direct renin inhibitors.

Angioedema: aliskiren has been associated with the occurrence of angioedema, a potentially life-threatening condition arises.

Hypotension: aliskiren can cause hypotension, particularly in patients with volume or salt depletion. Blood pressure should be monitored regularly, and caution should be exercised when initiating or adjusting the dose of aliskiren in patients at risk of hypotension.

Contraindication / Caution

Contraindication/Caution:

Pregnancy: aliskiren is contraindicated in pregnant women due to the risk of fetal harm or death. Use of aliskiren during pregnancy, especially during the second and third trimesters, can cause fetal toxicity, including fetal renal impairment, oligohydramnios (reduced amniotic fluid), and developmental abnormalities.

Severe Renal Impairment: Use of aliskiren in patients with severe renal impairment may result in further deterioration of renal function, including acute renal failure. Therefore, aliskiren should not be used in patients with severe renal impairment.

History of Angioedema: aliskiren is contraindicated in patients with a history of angioedema, a severe condition characterized by sudden swelling of the face, lips, tongue, or throat.

Pregnancy / Lactation

Pregnancy warnings:   

Pregnancy category: N/A

Lactation: Excreted into human milk is unknown

Pregnancy Categories:        

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in the first or second trimester.

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.  

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.  

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.   

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:

aliskiren is a medication used to treat hypertension (high blood pressure). Renin is an enzyme that plays a crucial role in regulating blood pressure by initiating the production of angiotensin II, a potent vasoconstrictor that can raise blood pressure.

Pharmacodynamics:

aliskiren exerts its pharmacodynamic effects through direct inhibition of renin, leading to reduced production of angiotensin II and subsequent vasodilation. Its unique mechanism of action as a renin inhibitor makes it a valuable option in managing hypertension, providing an alternative approach to controlling blood pressure by targeting the RAAS at its earliest step.

MOA:

The mechanism of action of aliskiren involves its ability to bind directly to renin, a protein secreted by the kidneys.

Pharmacokinetics:

Absorption

aliskiren is rapidly absorbed from the gastrointestinal tract after oral administration. The absolute bioavailability of aliskiren is low, ranging from approximately 2.5% to 3.7%.

Distribution

aliskiren has a high plasma protein binding capacity, primarily binding to albumin. The volume of distribution of aliskiren is relatively small, estimated to be around 50 liters, indicating limited tissue distribution.

Metabolism

aliskiren undergoes minimal metabolism in the liver, with less than 1% of the drug being metabolized. The main metabolic pathway involves oxidative metabolism mediated by cytochrome P450 (CYP) 3A4, forming inactive metabolites.

Elimination and Excretion

Mostly aliskiren is excreted unchanged in the feces (approximately 91%) via biliary excretion, with minimal renal elimination (less than 2%). The elimination half-life of aliskiren ranges from 24 to 40 hours, with no significant accumulation observed with repeated dosing.

Adminstartion

Administration: 

Route of Administration:

aliskiren is administered orally, typically once daily, with or without food.

Dosage Instructions:

The recommended starting dose of aliskiren for most adult patients with hypertension is 150 mg once daily. The dosage may be increased to 300 mg once daily if further blood pressure lowering is needed.

Special Populations:

For patients with impaired renal function (creatinine clearance less than 60 mL/min), the starting dose of aliskiren should be 150 mg once daily.

Patient Information Leaflet

Patient information leaflet

Generic Name: aliskiren

Why do we use aliskiren ?

aliskiren is a medication that belongs to the class of direct renin inhibitors. It is commonly used in the management of hypertension, also known as high blood pressure.

One of the primary reasons for using aliskiren is its ability to effectively lower blood pressure. It exerts its antihypertensive effects by blocking the activity of renin, which ultimately reduces the production of angiotensin II, a potent vasoconstrictor.

aliskiren may be used in combination with other antihypertensive agents to achieve optimal blood pressure control. It can be co-administered with diuretics, calcium channel blockers, or other antihypertensive drugs to achieve a synergistic effect, leading to greater blood pressure reduction compared to monotherapy.

aliskiren

No data available for drug.

DRUG INTERACTION

aliskiren

&

aliskiren +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

aliskiren

No data available for drug.

DRUG INTERACTION

aliskiren

&

aliskiren +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

medtigo

aliskiren

Brand Name :

Synonyms :

Class :

Action and Spectrum

Dosing & Uses

Drug Interaction

Adverse Reaction

Black Box Warning

Contraindication / Caution

Pregnancy / Lactation

Pharmacology

Adminstartion

Patient Information Leaflet

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