Aliskiren

What is Aliskiren?

• Aliskiren (Tekturna and Rasilez) is a renin inhibitor (RI) used for the treatment of hypertension in adults to lower blood pressure.

Aliskiren

Aliskiren Structural Formulae V.1

What are the uses of this medicine?

• Aliskiren (Tekturna and Rasilez) is a prescription medicine used to treat high blood pressure (hypertension) in adults to lower blood pressure.

How does this medicine work?

• Aliskiren (al' is key' ren) is a direct inhibitor of renin and acts to inhibit its ability to convert angiotensinogen to angiotensin 1, an early step in the renin-angiotensin system pathway.
• By inhibiting renin and the subsequent production of angiotensin II and aldosterone release, aliskiren results in a decrease in peripheral vasoconstriction and increase in sodium excretion.
• Aliskiren is effective in lowering blood pressure and can be used alone or in combination with other antihypertensive medications, including other inhibitors of the renin-angiotensin system such as the angiotensin converting enzyme (ACE) inhibitors and the angiotensin receptor blockers (ARBs).

Who Should Not Use this medicine ?

This medicine cannot be used if:

• you have diabetes and are taking a kind of medicine called an angiotensin receptor blocker (ARB) or angiotensin-converting enzyme inhibitor (ACEI).
• you are allergic to any of the ingredients in aliskiren tablets.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention the medications listed below:

• certain antifungals such as itraconazole (Sporanox)
• aspirin and other nonsteroidal anti-inflammatory medications (NSAIDs, such as ibuprofen (Advil, Motrin) and naproxen (Aleve, Naprosyn)
• atorvastatin (Lipitor, in Caduet, Liptruzet)
• celecoxib (Celebrex)
• cyclosporine (Gengraf, Neoral, Sandimmune)
• diuretics ('water pills')
• potassium supplements or potassium-containing medications
• any other medications for heart disease or high blood pressure.
• angiotensin receptor blocker (ARB) such as azilsartan (Edarbi, Edarbyclor)
• candesartan (Atacand, in Atacand HCT), eprosartan (Teveten, in Teveten HCT), irbesartan (Avapro, in Avalide), losartan (Cozaar, in Hyzaar), olmesartan (Benicar, in Azor, Benicar HCT), telmisartan (Micardis, in Micardis HCT), and valsartan (Diovan, in Diovan HCT, Exforge)
• or an ACE inhibitor
• an angiotensin-converting enzyme (ACE) inhibitor such as benazepril (Lotensin, in Lotrel), captopril (Capoten), enalapril (Vasotec, in Vaseretic), fosinopril, lisinopril (in Prinzide, in Zestoretic), moexipril (Univasc, in Uniretic), perindopril (Aceon), quinapril (Accupril, in Accuretic, in Quinaretic), ramipril (Altace), and trandolapril (Mavik, in Tarka)
• any other medications, or any of the ingredients in aliskiren tablets

Is this medicine FDA approved?

• In 2007, aliskiren became the first in the class of direct renin inhibitors to be approved for use in the United States.
• Aliskiren is available in under the brand name of Tekturna in tablets of 150 and 300 mg.
• Fixed combinations of aliskiren with hydrochlorthiazide (Tekturna HCT), valasartan (Valturna) and amlodipine (Amturnide) are also available.

How should this medicine be used?

Recommended dosage: Adult Hypertension:

• The usual recommended starting dose of aliskiren tablets is 150 mg once daily.
• In patients whose blood pressure is not adequately controlled, the daily dose may be increased to 300 mg.
• Doses above 300 mg did not give an increased blood pressure response but resulted in an increased rate of diarrhea.
• The antihypertensive effect of a given dose is substantially attained (85% to 90%) by 2 weeks.

Administration:

• Aliskiren comes as a tablet to take by mouth.
• It is usually taken once a day.
• Aliskiren should be taken either always with food or always without food.
• Take aliskiren at around the same time every day.
• Your doctor will probably start you on an low dose of aliskiren and may increase your dose after you have been taking this medication for at least 2 weeks.
• Patients should establish a routine pattern for taking aliskiren tablets with regard to meals.
• High-fat meals decrease absorption substantially.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 150 mg, 300 mg

This medicine is available in fallowing brand namesː

• Tekturna and Rasilez

What side effects can this medication cause?

The most common side effects of this medicine include:

• diarrhea
• headaches
• fatigue
• dizziness
• nasopharyngitis

Some side effects can be serious which may include:

• Hypersensitivity
• Urticaria
• Peripheral edema
• Hepatic enzyme increase with clinical symptoms of hepatic dysfunction
• Severe cutaneous adverse reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis
• hypotension
• Kidney problems, including kidney failure
• hyperkalemia

What special precautions should I follow?

• Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death.
• Aliskiren tablets are contraindicated in patients with diabetes who are receiving ARBs or ACEIs because of the increased risk of renal impairment, hyperkalemia, and hypotension. In general, avoid combined use of aliskiren with ACE inhibitors or ARBs, particularly in patients with creatinine clearance (CrCl) less than 60 mL/min.
• Hypersensitivity reactions such as anaphylactic reactions and angioedema of the face, extremities, lips, tongue, glottis and/or larynx have been reported in patients treated with aliskiren tablets. Discontinue aliskiren tablets immediately in patients who develop anaphylactic reactions or angioedema, and do not readminister.
• Symptomatic hypotension may occur after initiation of treatment with aliskiren tablets. Correct imbalances in volume and/or salt depleted patients.
• Monitor renal function periodically in patients treated with aliskiren tablets. Changes in renal function, including acute renal failure, can be caused by drugs that affect the RAAS. Consider withholding or discontinuing therapy in patients who develop a clinically significant decrease in renal function.
• Monitor serum potassium periodically in patients receiving aliskiren tablets. Drugs that affect the RAAS can cause hyperkalemia.
• When aliskiren was given with cyclosporine or itraconazole, the blood concentrations of aliskiren were significantly increased. Avoid concomitant use of aliskiren with cyclosporine or itraconazole.
• Aliskiren has been linked to rare instances of serum aminotransferase elevations during therapy and rare cases of idiosyncratic, clinically apparent liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• hypotension

Management of overdosage:

• If symptomatic hypotension occurs, supportive treatment should be initiated.
• Aliskiren is poorly dialyzed.
• Therefore, hemodialysis is not adequate to treat aliskiren overexposure

Can this medicine be used in pregnancy?

• Aliskiren can cause fetal harm when administered to a pregnant woman.
• Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death.

Can this medicine be used in children?

• Safety and effectiveness have not been established in pediatric patients younger than 18 years old.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• aliskiren hemifumarate

Inactive ingredients:

• calcium stearate, colloidal silicon dioxide, crospovidone, hypromellose, iron oxide red, microcrystalline cellulose, polyethylene glycol, talc and titanium dioxide. In addition, the 150 mg strength contains iron oxide black.

Who manufactures and distributes this medicine?

Dist. by:

• Par Pharmaceutical
• Chestnut Ridge, NY U.S.A.

Mfg. by:

• Par Formulations Private Limited,
• 9/215, Pudupakkam, Kelambakkam

What should I know about storage and disposal of this medication?

• Store aliskiren tablets at room temperature between 68° to 77°F (20° to 25°C).
• Keep aliskiren tablets in the original container it comes in. Do not remove the desiccant (drying agent) from the bottle.
• Protect aliskiren tablets from moisture.

• Dailymed label info on Aliskiren
• FDA Aliskiren

Antihypertensive agents