Rasilez is a renin inhibitor. It was approved by the U.S. Food and Drug Administration in 2007 for the treatment of hypertension.

Rasilez - Pharmacology:

Renin is secreted by the kidney in response to decreases in blood volume and renal perfusion. Renin cleaves angiotensinogen to form the inactive decapeptide angiotensin I (Ang I). Ang I is converted to the active octapeptide angiotensin II (Ang II) by angiotensin-converting enzyme (ACE) and non-ACE pathways. Ang II is a powerful vasoconstrictor and leads to the release of catecholamines from the adrenal medulla and prejunctional nerve endings. It also promotes aldosterone secretion and sodium reabsorption. Together, these effects increase blood pressure. Ang II also inhibits renin release, thus providing a negative feedback to the system. This cycle, from renin through angiotensin to aldosterone and its associated negative feedback loop, is known as the renin-angiotensin-aldosterone system (RAAS). Rasilez is a direct renin inhibitor, decreasing plasma renin activity (PRA) and inhibiting the conversion of angiotensinogen to Ang I. Whether aliskiren affects other RAAS components, e.g., ACE or non-ACE pathways, is not known. All agents that inhibit the RAAS, including renin inhibitors, suppress the negative feedback loop, leading to a compensatory rise in plasma renin concentration. When this rise occurs during treatment with ACE inhibitors and ARBs, the result is increased levels of PRA. During treatment with aliskiren, however, the effect of increased renin levels is blocked, so that PRA, Ang I and Ang II are all reduced, whether aliskiren is used as monotherapy or in combination with other antihypertensive agents. PRA reductions in clinical trials ranged from approximately 50%-80%, were not dose-related and did not correlate with blood pressure reductions. The clinical implications of the differences in effect on PRA are not known.

Rasilez for patients

IMPORTANT WARNING: If you get pregnant, stop taking Tekturna and call your doctor right away. Tekturna may harm an unborn baby, causing injury and even death. If you plan to become pregnant, talk to your doctor about other treatment options before taking Tekturna.

What Is High Blood Pressure (Hypertension)? Blood pressure is the force that pushes the blood through your blood vessels to all the organs of your body. You have high blood pressure when the force of your blood moving through your blood vessels is too great. Renin (pronounced REE-nin) is a chemical in the body that starts a process that makes blood vessels narrow, leading to high blood pressure.

High blood pressure makes the heart work harder to pump blood throughout the body and causes damage to the blood vessels. If high blood pressure is not treated, it can lead to stroke, heart attack, heart failure, kidney failure, and vision problems.

What Is Tekturna? Tekturna is a type of prescription medicine called a direct renin inhibitor that works in the body to help lower blood pressure (hypertension).

How Does Tekturna Work? Tekturna reduces the effect of renin and the harmful process that narrows blood vessels. Tekturna helps blood vessels relax and widen so blood pressure is lowered.

Who Should Not Take Tekturna?

  • If you get pregnant, stop taking Tekturna and call your doctor right away. If you plan to become pregnant, talk to your doctor about other treatment options for your high blood pressure.
  • Do not take Tekturna if you are allergic to any of its ingredients.

Rasilez is the active ingredient in Tekturna. The inactive ingredients (the ingredients that bind the tablet together) are colloidal silicon dioxide, crospovidone, hypromellose, iron oxide colorants, magnesium stearate, microcrystalline cellulose, polyethylene glycol, povidone, talc, and titanium dioxide. These inactive ingredients are considered safe and are commonly used in many medications. Talk to your doctor if you have questions.

Tekturna has not been studied in children under 18 years of age.

What Should I Tell My Doctor Before Taking Tekturna? Tell your doctor about all your medical conditions, including whether you:

  • are pregnant or planning to become pregnant.
  • are breast-feeding. It is not known if Tekturna passes into your breast milk. You should choose either to take Tekturna or breast-feed, but not both.
  • have kidney problems.
  • are allergic to any of the ingredients in Tekturna.

Tell your doctor about all the medicines you take including prescription and nonprescription medicines, vitamins and herbal supplements. Especially tell your doctor if you are taking:

  • other medicines for high blood pressure or a heart problem.
  • water pills (also called “diuretics”).
  • medicines for treating fungus or fungal infections. Your doctor or pharmacist will know what medicines are safe to take together.

How Should I Take Tekturna?

  • Take Tekturna once a day, at the same time each day. As with any blood pressure medication, it is important to take Tekturna on a regular daily basis exactly as prescribed by your doctor.
  • Tekturna can be taken by itself or safely in combination with other medicines to lower high blood pressure. It can also be safely taken in combination with medications for other conditions such as high cholesterol or diabetes. Your doctor may change your dose if needed.
  • Tekturna can be taken with or without food.

If you miss a dose, take it as soon as you remember. If it is close to your next dose, do not take the missed dose. Just take the next dose at your regular time. If you take too much Tekturna, call your doctor or Poison Control Center, or go to the nearest hospital emergency room.

What Are Possible Side Effects Of Tekturna? Tekturna may cause the following serious side effect:

  • Low blood pressure (hypotension). Your blood pressure may get too low if you also take water pills, are on a low-salt diet, get dialysis treatments, have heart problems, or get sick with vomiting or diarrhea. Lie down if you feel faint or dizzy. Call your doctor right away.

Side effects were usually mild and brief. Few patients decided to stop taking Tekturna because of side effects. In clinical studies, the most common side effect experienced by more patients taking Tekturna than patients taking a sugar pill (placebo) was diarrhea. Other less common reactions to Tekturna include cough, and rash.

If you develop an allergic reaction involving swelling of the face, lips, throat and/or tongue which may cause difficulty in breathing and swallowing, stop taking Tekturna and contact your doctor immediately.

For a complete list of side effects, ask your doctor or pharmacist. Tell your doctor if you get any side effect that bothers you or will not go away.

How Do I Store Tekturna?

  • Store Tekturna tablets at room temperature between 59o to 86oF.
  • Keep Tekturna in the original prescription bottle in a dry place. Do not remove the desiccant (drying agent) from the bottle.
  • Keep Tekturna and all medicines out of the reach of children.

General Information About Tekturna Do not give Tekturna to other people, even if they have the same condition or symptoms you have. It may harm them.

This leaflet summarizes the most important information about Tekturna.

For more information about Tekturna, ask your doctor or pharmacist, visit www.Tekturna.com, or call 1-888-Tekturna (1-888-835-8876).

Rasilez Interactions

Effects of Other Drugs on Rasilez

Based on in-vitro studies, aliskiren is metabolized by CYP 3A4. Co-administration of lovastatin, atenolol, warfarin, furosemide, digoxin, celecoxib, hydrochlorothiazide, ramapril, valsartan, metformin and amlodipine did not result in clinically significant increases in aliskiren exposure. Co-administration of irbesartan reduced aliskiren Cmax up to 50% after multiple dosing. Co-administration of atorvastatin resulted in about a 50% increase in aliskiren Cmax and AUC after multiple dosing.

Ketoconazole Co-administration of 200 mg twice-daily ketoconazole with aliskiren resulted in an approximate 80% increase in plasma levels of aliskiren. A 400 mg once-daily dose was not studied but would be expected to increase aliskiren blood levels further.

Effects of Rasilez on Other Drugs Rasilez does not inhibit the CYP450 isoenzymes (CYP1A2, 2C8, 2C9, 2C19, 2D6, 2E1, and CYP 3A) or induce CYP 3A4. Co-administration of aliskiren did not significantly affect the pharmacokinetics of lovastatin, digoxin, valsartan, amlodipine, metformin, celecoxib, atenolol, atorvastatin, ramipril or hydrochlorothiazide.

Warfarin The effects of aliskiren on warfarin pharmacokinetics have not been evaluated in a well-controlled clinical trial.

Furosemide When aliskiren was co-administered with furosemide, the AUC and Cmax of furosemide were reduced by about 30% and 50%, respectively.

Generic name, Overdose, Half Life Rasilez, Food Interactions, Chemical, etc..

Rasilez see also

Brand Names containing Aliskiren