Drugs Details

Drugs Info of Tekturna
Drugs Details
  • Drugs Type  : FDA
  • Date : 19th Jun 2015 02:51 am
  • Brand Name : Tekturna
  • Generic Name : aliskiren (Pronunciation: a LIS ke rin)
Descriptions

Tekturna contains aliskiren hemifumarate, a renin inhibitor, that is provided as tablets for oral administration. Aliskiren hemifumarate is chemically described as (2S,4S,5S,7S)-N-(2-carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7diisopropyl-8-[4-methoxy-3-(3-methoxypropoxy)phenyl]-octanamide hemifumarate and its structural formula is

 

Tekturna® (aliskiren) Structural Formula Illustration

Molecular formula: C30H53N3O6 •0.5 C4H4O4

Aliskiren hemifumarate is a white to slightly yellowish crystalline powder with a molecular weight of 609.8 (free base- 551.8). It is soluble in phosphate buffer, n-octanol, and highly soluble in water.

What are the possible side effects of aliskiren (Tekturna)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; severe stomach pain; difficult breathing; swelling of your face, lips, tongue, or throat.

If you have an allergic reaction to aliskiren you should not take it again.

Call your doctor at once if you have a serious side effect such as:

  • feeling light-headed, fainting;
  • nausea with slow uneven heart rate and a weak pulse;
  • swelling around your eyes; or
  • severe skin reaction -- fever, sore throat, swelling in your face or tongue, burning in your eyes,...

Read All Potential Side Effects and See Pictures of Tekturna »

What are the precautions when taking aliskiren tablets (Tekturna)?

Before taking aliskiren, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: diabetes, gout, heart problems, kidney disease (including kidney stones), loss of too much body water (dehydration), untreated mineral imbalance (such as low sodium, high potassium).

This drug may make you dizzy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Limit alcoholic beverages.

This medication may increase your potassium...

This monograph has been modified to include the generic and brand name in many instances.

Indications

Hypertension

Tekturna is indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacologic classes. There are no controlled trials demonstrating risk reduction with Tekturna.

Control of high blood pressure should be part of comprehensive cardiovascular risk management, including, as appropriate, lipid control, diabetes management, antithrombotic therapy, smoking cessation, exercise, and limited sodium intake. Many patients will require more than one drug to achieve blood pressure goals. For specific advice on goals and management, see published guidelines, such as those of the National High Blood Pressure Education Program's Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC).

Numerous antihypertensive drugs, from a variety of pharmacologic classes and with different mechanisms of action, have been shown in randomized controlled trials to reduce cardiovascular morbidity and mortality, and it can be concluded that it is blood pressure reduction, and not some other pharmacologic property of the drugs, that is largely responsible for those benefits. The largest and most consistent cardiovascular outcome benefit has been a reduction in the risk of stroke, but reductions in myocardial infarction and cardiovascular mortality also have been seen regularly.

Elevated systolic or diastolic pressure causes increased cardiovascular risk, and the absolute risk increase per mmHg is greater at higher blood pressures, so that even modest reductions of severe hypertension can provide substantial benefit. Relative risk reduction from blood pressure reduction is similar across populations with varying absolute risk, so the absolute benefit is greater in patients who are at higher risk independent of their hypertension (for example, patients with diabetes or hyperlipidemia), and such patients would be expected to benefit from more aggressive treatment to a lower blood pressure goal.

Some antihypertensive drugs have smaller blood pressure effects (as monotherapy) in black patients, and many antihypertensive drugs have additional approved indications and effects (e.g., on angina, heart failure, or diabetic kidney disease). These considerations may guide selection of therapy.

Dosage Administration

Hypertension

The usual recommended starting dose of Tekturna 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 (85-90%) by 2 weeks.

Use With Other Antihypertensives

Tekturna may be administered with some other antihypertensive agents. In diabetics, do not use in combination with angiotensin receptor blockers (ARBs) or angiotensin converting enzyme inhibitors (ACEIs) [see CONTRAINDICATIONS Concomitant use of aliskiren with an ARB or ACEI is not recommended in patients with GFR < 60 ml/min [see WARNINGS AND PRECAUTIONS]. Most exposure to date is with diuretics, an angiotensin receptor blocker (valsartan) or a calcium channel blocker (amlodipine). Aliskiren used together with these drugs has a greater effect at their maximum recommended doses than either drug alone. It is not known whether additive effects are present when Tekturna is used with angiotensin-converting enzyme inhibitors (ACEIs) or beta blockers (BB).

Relationship To Meals

Patients should establish a routine pattern for taking Tekturna with regard to meals. High fat meals decrease absorption substantially [see CLINICAL PHARMACOLOGY].

How Supplied

Dosage Forms And Strengths

150 mg light pink biconvex round tablet, imprinted NVR/IL (Side 1/Side 2)

300 mg light red biconvex ovaloid round tablet, imprinted NVR/IU (Side 1/Side 2)

Storage And Handling

Tekturna is supplied as a light-pink, biconvex round tablet containing 150 mg of aliskiren, and as a light-red biconvex ovaloid tablet containing 300 mg of aliskiren. Tablets are imprinted with NVR on one side and IL, IU, on the other side of the 150, and 300 mg tablets, respectively.

All strengths are packaged in bottles and unit-dose blister packages (10 strips or 10 tablets) as described below in Table 6.

Table 6: Tekturna Tablets Supply

Tablet Color Imprint Imprint NDC 0078-XXXX-XX
Side 1 Side 2 Bottle of 30 Bottle of 90 Blister Packages of 100
150 mg Light-Pink NVR IL 0485-15 0485-34 0485-35
300 mg Light-Red NVR IU 0486-15 0486-34 0486-35

Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F) [See USP Controlled Room Temperature]. Protect from moisture.

Dispense in original container.

Manufactured by: Novartis Pharma AG, Stein, Switzerland Novartis Pharma Produktions GmbH, Wehr, Germany. Distributed by: Novartis Pharmaceuticals Corporation East Hanover, NJ 07936. Revised: March 2014


This monograph has been modified to include the generic and brand name in many instances.

Side Effects

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in clinical trials of another drug and may not reflect the rates observed in practice.

Data described below reflect the evaluation of the safety of Tekturna in more than 6,460 patients, including over 1,740 treated for longer than 6 months, and more than 1,250 patients for longer than 1 year. In placebo controlled clinical trials, discontinuation of therapy due to a clinical adverse event, including uncontrolled hypertension occurred in 2.2% of patients treated with Tekturna vs. 3.5% of patients given placebo. These data do not include information from the ALTITUDE study which evaluated the use of aliskiren in combination with ARBs or ACEIs [see CONTRAINDICATIONS, WARNINGS AND PRECAUTIONS, and Clinical Studies].

Angioedema: Two cases of angioedema with respiratory symptoms were reported with Tekturna use in the clinical studies. Two other cases of periorbital edema without respiratory symptoms were reported as possible angioedema and resulted in discontinuation. The rate of these angioedema cases in the completed studies was 0.06%. In addition, 26 other cases of edema involving the face, hands, or whole body were reported with Tekturna use including 4 leading to discontinuation. In the placebo controlled studies, however, the incidence of edema involving the face, hands or whole body was 0.4% with Tekturna compared with 0.5% with placebo. In a long term active control study with Tekturna and HCTZ arms, the incidence of edema involving the face, hand or whole body was 0.4% in both treatment arms [see WARNINGS AND PRECAUTIONS].

Gastrointestinal: Tekturna produces dose-related gastrointestinal (GI) adverse reactions. Diarrhea was reported by 2.3% of patients at 300 mg, compared to 1.2% in placebo patients. In women and the elderly (age ≥ 65) increases in diarrhea rates were evident starting at a dose of 150 mg daily, with rates for these subgroups at 150 mg comparable to those seen at 300 mg for men or younger patients (all rates about 2.0-2.3%). Other GI symptoms included abdominal pain, dyspepsia, and gastroesophageal reflux, although increased rates for abdominal pain and dyspepsia were distinguished from placebo only at 600 mg daily. Diarrhea and other GI symptoms were typically mild and rarely led to discontinuation.

Cough: Tekturna was associated with a slight increase in cough in the placebo-controlled studies (1.1% for any Tekturna use vs. 0.6% for placebo). In active-controlled trials with ACE inhibitor (ramipril, lisinopril) arms, the rates of cough for the Tekturna arms were about one-third to one-half the rates in the ACE inhibitor arms.

Seizures: Single episodes of tonic-clonic seizures with loss of consciousness were reported in two patients treated with Tekturna in the clinical trials. One of these patients did have predisposing causes for seizures and had a negative electroencephalogram (EEG) and cerebral imaging following the seizures (for the other patient EEG and imaging results were not reported). Tekturna was discontinued and there was no re-challenge.

Other adverse effects with increased rates for Tekturna compared to placebo included rash (1% vs. 0.3%), elevated uric acid (0.4% vs. 0.1%), gout (0.2% vs. 0.1%) and renal stones (0.2% vs. 0%).

Aliskiren's effect on ECG intervals was studied in a randomized, double-blind, placebo and active-controlled (moxifloxacin), 7-day repeat dosing study with Holter-monitoring and 12 lead ECGs throughout the interdosing interval. No effect of aliskiren on QT interval was seen.

Clinical Laboratory Findings

In controlled clinical trials, clinically relevant changes in standard laboratory parameters were rarely associated with the administration of Tekturna in patients with hypertension not concomitantly treated with an ARB or ACEI. In multiple-dose studies in hypertensive patients, Tekturna had no clinically important effects on total cholesterol, HDL, fasting triglycerides, or fasting glucose.

Blood Urea Nitrogen, Creatinine: In patients with hypertension not concomitantly treated with an ARB or ACEI, minor increases in blood urea nitrogen (BUN) or serum creatinine were observed in less than 7% of patients treated with Tekturna alone vs. 6% on placebo [see WARNINGS AND PRECAUTIONS].

Hemoglobin and Hematocrit: Small decreases in hemoglobin and hematocrit (mean decreases of approximately 0.08 g/dL and 0.16 volume percent, respectively, for all aliskiren monotherapy) were observed. The decreases were dose-related and were 0.24 g/dL and 0.79 volume percent for 600 mg daily. This effect is also seen with other agents acting on the renin angiotensin system, such as angiotensin inhibitors and angiotensin receptor blockers and may be mediated by reduction of angiotensin II which stimulates erythropoietin production via the AT1 receptor. These decreases led to slight increases in rates of anemia with aliskiren compared to placebo were observed (0.1% for any aliskiren use, 0.3% for aliskiren 600 mg daily, vs 0% for placebo). No patients discontinued therapy due to anemia.

Serum Potassium: In patients with hypertension not concomitantly treated with an ARB or ACEI, increases in serum potassium > 5.5 mEq/L were infrequent (0.9% compared to 0.6% with placebo) [See CONTRAINDICATIONS and WARNINGS AND PRECAUTIONS].

Serum Uric Acid: Aliskiren monotherapy produced small median increases in serum uric acid levels (about 6 μmol/L) while HCTZ produced larger increases (about 30 μmol/L). The combination of aliskiren with HCTZ appears to be additive (about 40 μmol/L increase). The increases in uric acid appear to lead to slight increases in uric acid-related AEs: elevated uric acid (0.4% vs 0.1%), gout (0.2% vs. 0.1%), and renal stones (0.2% vs 0%).

Creatine Kinase: Increases in creatine kinase of > 300% were recorded in about 1% of aliskiren monotherapy patients vs. 0.5% of placebo patients. Five cases of creatine kinase rises, three leading to discontinuation and one diagnosed as subclinical rhabdomyolysis, and another as myositis, were reported as adverse events with aliskiren use in the clinical trials. No cases were associated with renal dysfunction.

Postmarketing Experience

The following adverse reactions have been reported in aliskiren post-marketing experience. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to estimate their frequency or establish a causal relationship to drug exposure.

Hypersensitivity: anaphylactic reactions and angioedema requiring airway management and hospitalization
Urticaria

Peripheral edema

Hepatic enzyme increase with clinical symptoms of hepatic dysfunction

Severe cutaneous adverse reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis

Pruritus

Erythema

Read the Tekturna (aliskiren tablets) Side Effects Center for a complete guide to possible side effects

Interactions

Cyclosporine

Avoid co-administration of cyclosporine with aliskiren.

Itraconazole

Avoid co-administration of itraconazole with aliskiren [See CLINICAL PHARMACOLOGY].

Non-Steroidal Anti-Inflammatory Agents (NSAIDs) including selective Cyclooxygenase-2 inhibitors (COX-2 inhibitors)

In patients who are elderly, volume-depleted (including those on diuretic therapy), or with compromised renal function, co-administration of NSAIDs, including selective COX-2 inhibitors with agents that affect the renin-angiotensinaldosterone system, including aliskiren, may result in deterioration of renal function, including possible acute renal failure. These effects are usually reversible. Monitor renal function periodically in patients receiving aliskiren and NSAID therapy.

The antihypertensive effect of aliskiren may be attenuated by NSAIDs.

Dual Blockade of the renin-angiotensin-aldosterone system

The concomitant use of aliskiren with other agents acting on the renin-angiotensin-aldosterone system such as ACEIs or ARBs is associated with an increased risk of hypotension, hyperkalemia, and changes in renal function (including acute renal failure) compared to monotherapy. Monitor blood pressure, renal function, and electrolytes in patients on aliskiren and other agents that affect the renin-angiotensinaldosterone system [see WARNINGS AND PRECAUTIONS].

The concomitant use of aliskiren with an ARB or an ACEI in diabetic patients is contraindicated and should be avoided in patients with moderate renal impairment [see CONTRAINDICATIONS and WARNINGS AND PRECAUTIONS].

Furosemide

Oral co-administration of aliskiren and furosemide reduced exposure to furosemide. Monitor diuretic effects when furosemide is co-administered with aliskiren.

Read the Tekturna Drug Interactions Center for a complete guide to possible interactions


This monograph has been modified to include the generic and brand name in many instances.

Warnings

Included as part of the PRECAUTIONS section.

Precautions

Fetal Toxicity

Pregnancy Category D

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. Resulting oligohydramnios can be associated with fetal lung hypoplasia and skeletal deformations. Potential neonatal adverse effects include skull hypoplasia, anuria, hypotension, renal failure, and death. When pregnancy is detected, discontinue Tekturna as soon as possible [see Use In Specific Populations].

Renal Impairment/Hyperkalemia/Hypotension When Tekturna Is Given In Combination With ARBs Or ACEIs

Tekturna is contraindicated in patients with diabetes who are receiving ARBs or ACEIs because of the increased risk of renal impairment, hyperkalemia, and hypotension [see CONTRAINDICATIONS and Clinical Studies].

Avoid use of Tekturna with ARBs or ACEIs in patients with moderate renal impairment (GFR < 60 ml/min).

Anaphylactic Reactions And Head And Neck Angioedema

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 Tekturna and has necessitated hospitalization and intubation. This may occur at any time during treatment and has occurred in patients with and without a history of angioedema with ACE inhibitors or angiotensin receptor antagonists. Anaphylactic reactions have been reported from post-marketing experience with unknown frequency. If angioedema involves the throat, tongue, glottis or larynx, or if the patient has a history of upper respiratory surgery, airway obstruction may occur and be fatal. Patients who experience these effects, even without respiratory distress, require prolonged observation and appropriate monitoring measures since treatment with antihistamines and corticosteroids may not be sufficient to prevent respiratory involvement. Prompt administration of subcutaneous epinephrine solution 1:1000 (0.3 to 0.5 ml) and measures to ensure a patent airway may be necessary.

Discontinue Tekturna immediately in patients who develop anaphylactic reactions or angioedema, and do not readminister.

Hypotension

Symptomatic hypotension may occur after initiation of treatment with Tekturna in patients with marked volume depletion, patients with salt depletion, or with combined use of aliskiren and other agents acting on the renin-angiotensin-aldosterone system. The volume or salt depletion should be corrected prior to administration of Tekturna, or the treatment should start under close medical supervision.

A transient hypotensive response is not a contraindication to further treatment, which usually can be continued without difficulty once the blood pressure has stabilized.

Impaired Renal Function

Monitor renal function periodically in patients treated with Tekturna. Changes in renal function, including acute renal failure, can be caused by drugs that affect the renin-angiotensin-aldosterone system. Patients whose renal function may depend in part on the activity of the renin-angiotensin-aldosterone system (e.g., patients with renal artery stenosis, severe heart failure, post-myocardial infarction or volume depletion) or patients receiving ARB, ACEI or non-steroidal anti-inflammatory (NSAID) therapy may be at particular risk for developing acute renal failure on Tekturna [see CONTRAINDICATIONS, Clinical Studies]. Consider withholding or discontinuing therapy in patients who develop a clinically significant decrease in renal function.

Hyperkalemia

Monitor serum potassium periodically in patients receiving Tekturna. Drugs that affect the renin-angiotensin-aldosterone system can cause hyperkalemia. Risk factors for the development of hyperkalemia include renal insufficiency, diabetes, combination use with ARBs or ACEIs [see CONTRAINDICATIONS, and Clinical Studies], NSAIDs, or potassium supplements or potassium sparing diuretics.

Cyclosporine Or Itraconazole

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 [see DRUG INTERACTIONS].

Patient Counseling Information

See FDA-approved patient labeling (PATIENT INFORMATION)

Information for Patients

Pregnancy: Female patients of child bearing age should be told about the consequences of exposure to Tekturna during pregnancy. Discuss treatment options with women planning to become pregnant. Patients should be asked to report pregnancies to their physicians as soon as possible.

Anaphylactic Reactions and Angioedema: Patients should be advised and told to report immediately any signs or symptoms suggesting a severe allergic reaction (difficulty breathing or swallowing, tightness of the chest, hives, general rash, swelling, itching, dizziness, vomiting, or abdominal pain) or angioedema (swelling of face, extremities, eyes, lips, tongue, difficulty in swallowing or breathing) and to take no more drug until they have consulted with the prescribing physicians. Angioedema, including laryngeal edema, may occur at any time during treatment with Tekturna.

Symptomatic Hypotension: A patient receiving Tekturna should be cautioned that lightheadedness can occur, especially during the first days of therapy, and that it should be reported to the prescribing physician. The patients should be told that if syncope occurs, Tekturna should be discontinued until the physician has been consulted.

All patients should be cautioned that inadequate fluid intake, excessive perspiration, diarrhea, or vomiting can lead to an excessive fall in blood pressure, with the same consequences of lightheadedness and possible syncope.

Potassium Supplements: A patient receiving Tekturna should be told not to use potassium supplements or salt substitutes containing potassium without consulting the prescribing physician.

Relationship to Meals: Patients should establish a routine pattern for taking Tekturna with regard to meals. High-fat meals decrease absorption substantially.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment Of Fertility

Carcinogenic potential was assessed in a 2-year rat study and a 6-month transgenic (rasH2) mouse study with aliskiren hemifumarate at oral doses of up to 1500 mg aliskiren/kg/day. Although there were no statistically significant increases in tumor incidence associated with exposure to aliskiren, mucosal epithelial hyperplasia (with or without erosion/ulceration) was observed in the lower gastrointestinal tract at doses of ≥ 750 mg/kg/day in both species, with a colonic adenoma identified in one rat and a cecal adenocarcinoma identified in another, rare tumors in the strain of rat studied. On a systemic exposure (AUC0-24hr) basis, 1500 mg/kg/day in the rat is about 4 times and in the mouse about 1.5 times the maximum recommended human dose (300 mg aliskiren/day). Mucosal hyperplasia in the cecum or colon of rats was also observed at doses of 250 mg/kg/day (the lowest tested dose) as well as at higher doses in 4- and 13-week studies.

Aliskiren hemifumarate was devoid of genotoxic potential in the Ames reverse mutation assay with S. typhimurium and E. coli, the in vitro Chinese hamster ovary cell chromosomal aberration assay, the in vitro Chinese hamster V79 cell gene mutation test and the in vivo mouse bone marrow micronucleus assay.

Fertility of male and female rats was unaffected at doses of up to 250 mg aliskiren/kg/day (8 times the maximum recommended human dose of 300 mg Tekturna/60 kg on a mg/m² basis.)

Use In Specific Populations

Pregnancy

Pregnancy Category D

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. Resulting oligohydramnios can be associated with fetal lung hypoplasia and skeletal deformations. Potential neonatal adverse effects include skull hypoplasia, anuria, hypotension, renal failure, and death. When pregnancy is detected, discontinue Tekturna as soon as possible. These adverse outcomes are usually associated with use of these drugs in the second and third trimester of pregnancy. Most epidemiologic studies examining fetal abnormalities after exposure to antihypertensive use in the first trimester have not distinguished drugs affecting the renin-angiotensin system from other antihypertensive agents. Appropriate management of maternal hypertension during pregnancy is important to optimize outcomes for both mother and fetus.

In the unusual case that there is no appropriate alternative to therapy with drugs affecting the renin-angiotensin system for a particular patient, apprise the mother of the potential risk to the fetus. Perform serial ultrasound examinations to assess the intra-amniotic environment. If oligohydramnios is observed, discontinue Tekturna, unless it is considered lifesaving for the mother. Fetal testing may be appropriate, based on the week of pregnancy. Patients and physicians should be aware, however, that oligohydramnios may not appear until after the fetus has sustained irreversible injury. Closely observe infants with histories of in utero exposure to Tekturna for hypotension, oliguria, and hyperkalemia. [see Use in Specific Populations]

Nursing Mothers

It is not known whether aliskiren is excreted in human breast milk. Aliskiren was secreted in the milk of lactating rats. Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use

Safety and effectiveness of aliskiren in pediatric patients < 18 years have not been established.

Neonates with a history of in utero exposure to Tekturna

If oliguria or hypotension occurs, direct attention toward support of blood pressure and renal perfusion. Exchange transfusions or dialysis may be required as a means of reversing hypotension and/or substituting for disordered renal function.

Geriatric Use

Of the total number of patients receiving aliskiren in clinical studies, 1,275 (19%) were 65 years or older and 231 (3.4%) were 75 years or older. No overall differences in safety or effectiveness were observed between these subjects and younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.

Renal Impairment

Safety and effectiveness of Tekturna in patients with severe renal impairment (CrCL < 30 ml/min) have not been established as patients with eGFR < 30ml/min were excluded in clinical trials [see Clinical Studies].

 

OverDose

Limited data are available related to overdosage in humans. The most likely manifestation of overdosage would be hypotension. If symptomatic hypotension occurs, supportive treatment should be initiated.

Aliskiren is poorly dialyzed. Therefore, hemodialysis is not adequate to treat aliskiren overexposure [see CLINICAL PHARMACOLOGY].

ContrainDications

Do not use aliskiren with ARBs or ACEIs in patients with diabetes [see WARNINGS AND PRECAUTIONS, Clinical Studies].


This monograph has been modified to include the generic and brand name in many instances.

Clinical Pharamacology

Mechanism Of Action

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). Aliskiren 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.

Pharmacodynamics

In placebo controlled clinical trials, plasma renin activity (PRA) was decreased in a range of 50- 80%. This reduction in PRA was not dose-related and did not correlate with blood pressure reductions. The clinical implications of the differences in effect on PRA are not known.

Pharmacokinetics

Aliskiren is poorly absorbed (bioavailability about 2.5%) with an approximate accumulation half life of 24 hours. Steady state blood levels are reached in about 7-8 days.

Absorption and Distribution

Following oral administration, peak plasma concentrations of aliskiren are reached within 1 – 3 hours. When taken with a high fat meal, mean AUC and Cmax of aliskiren are decreased by 71% and 85% respectively. In the clinical trials of aliskiren, it was administered without requiring a fixed relation of administration to meals.

Metabolism and Elimination

About one fourth of the absorbed dose appears in the urine as parent drug. How much of the absorbed dose is metabolized is unknown. Based on the in vitro studies, the major enzyme responsible for aliskiren metabolism appears to be CYP 3A4. Aliskiren does not inhibit the CYP450 isoenzymes (CYP 1A2, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A) or induce CYP 3A4.

Transporters: Pgp (MDR1/Mdr1a/1b) was found to be the major efflux system involved in absorption and disposition of aliskiren in preclinical studies. The potential for drug interactions at the Pgp site will likely depend on the degree of inhibition of this transporter.

Drug Interactions

The effect of co-administered drugs on the pharmacokinetics of aliskiren and vice versa, were studied in several single and multiple dose studies. Pharmacokinetic measures indicating the magnitude of these interactions are presented in Figure 1 (impact of co-administered drugs on aliskiren) and Figure 2 (impact of aliskiren on co-administered drugs).

Figure 1: The impact of co-administered drugs on the pharmacokinetics of aliskiren.

View Enlarged Table

Warfarin: There was no clinically significant effect of a single dose of warfarin 25 mg on the pharmacokinetics of aliskiren.

Figure 2: The impact of aliskiren on the pharmacokinetics of co-administered drugs

View Enlarged Table

Furosemide: In patients with heart failure, co-administration of aliskiren (300 mg/day) reduced plasma AUC and Cmax of oral furosemide (60 mg/day) by 17% and 27%, respectively, and reduced 24 hour urinary furosemide excretion by 29%. This change in exposure did not result in statistically significant difference in total urine volume and urinary sodium excretion over 24 hours. However, a transient decrease in urinary sodium excretion and urine volume effects up to 12 hours were observed when furosemide was co-administered with aliskiren 300 mg/day.

Special Populations

Renally Impaired Patients: Aliskiren was evaluated in patients with varying degrees of renal insufficiency. The rate and extent of exposure (AUC and Cmax) of aliskiren in subjects with renal impairment did not show a consistent correlation with the severity of renal impairment. Adjustment of the starting dose is not required in these patients [see WARNINGS AND PRECAUTIONS].

The pharmacokinetics of aliskiren following administration of a single oral dose of 300 mg was evaluated in patients with End Stage Renal Disease (ESRD) undergoing hemodialysis. When compared to matched healthy subjects, changes in the rate and extent of aliskiren exposure (Cmax and AUC) in ESRD patients undergoing hemodialysis was not clinically significant.

Timing of hemodialysis did not significantly alter the pharmacokinetics of aliskiren in ESRD patients. Therefore, no dose adjustment is warranted in ESRD patients receiving hemodialysis.

Hepatically Impaired Patients: The pharmacokinetics of aliskiren were not significantly affected in patients with mild to severe liver disease. Consequently, adjustment of the starting dose is not required in these patients.

Pediatric Patients: The pharmacokinetics of aliskiren have not been investigated in patients < 18 years of age.

Geriatric Patients: Exposure (measured by AUC) is increased in elderly patients ≥ 65 years. Adjustment of the starting dose is not required in these patients.

Race: The pharmacokinetic differences between Blacks, Caucasians, and the Japanese are minimal.

Animal Toxicology And/Or Pharmacology

Reproductive Toxicology Studies

Reproductive toxicity studies of aliskiren hemifumarate did not reveal any evidence of teratogenicity at oral doses up to 600 mg aliskiren/kg/day (20 times the maximum recommended human dose (MRHD) of 300 mg/day on a mg/m² basis) in pregnant rats or up to 100 mg aliskiren/kg/day (7 times the MRHD on a mg/m² basis) in pregnant rabbits. Fetal birth weight was adversely affected in rabbits at 50 mg/kg/day (3.2 times the MRHD on a mg/m² basis). Aliskiren was present in placenta, amniotic fluid and fetuses of pregnant rabbits.

Clinical Studies

Aliskiren Monotherapy

The antihypertensive effects of Tekturna have been demonstrated in six randomized, double-blind, placebo-controlled 8week clinical trials in patients with mild-to-moderate hypertension. The placebo response and placebo-subtracted changes from baseline in seated trough cuff blood pressure are shown in Table 1.

Table 1: Reductions in Seated Trough Cuff Blood Pressure in the Placebo-Controlled Studies

Study Placebo mean change Aliskiren daily dose, mg
75 150 300 600
Placebo-subtracted Placebo-subtracted Placebo-subtracted Placebo-subtracted
1 2.9/3.3 5.7/4* 5.9/4.5* 11.2/7.5* --
2 5.3/6.3 -- 6.1/2.9* 10.5/5.4* 10.4/5.2*
3 10/8.6 2.2/1.7 2.1/1.7 5.1/3.7* --
4 7.5/6.9 1.9/1.8 4.8/2* 8.3/3.3* --
5 3.8/4.9 -- 9.3/5.4* 10.9/6.2* 12.1/7.6*
6 4.6/4.1 -- -- 8.4/4.9† --
*p < 0.05 vs. placebo by ANCOVA with Dunnett's procedure for multiple comparisons
†p < 0.05 vs. placebo by ANCOVA for the pairwise comparison.

The studies included approximately 2,730 patients given doses of 75-600 mg of aliskiren and 1,231 patients given placebo. As shown in Table 1, there is some increase in response with administered dose in all studies, with reasonable effects seen at 150-300 mg, and no clear further increases at 600 mg. A substantial proportion (85%-90%) of the blood pressure lowering effect was observed within 2 weeks of treatment studies with ambulatory blood pressure monitoring showed reasonable control throughout the interdosing interval; the ratios of mean daytime to mean nighttime ambulatory BP range from 0.6 to 0.9.

Patients in the placebo-controlled trials continued open-label aliskiren for up to one year. A persistent blood pressure lowering effect was demonstrated by a randomized withdrawal study (patients randomized to continue drug or placebo), which showed a statistically significant difference between patients kept on aliskiren and those randomized to placebo. With cessation of treatment, blood pressure gradually returned toward baseline levels over a period of several weeks. There was no evidence of rebound hypertension after abrupt cessation of therapy.

Aliskiren lowered blood pressure in all demographic subgroups, although Black patients tended to have smaller reduction than Caucasians and Asians, as has been seen with ACE inhibitors and ARBs.

There are no studies of Tekturna or members of the direct renin inhibitors demonstrating reductions in cardiovascular risk in patients with hypertension.

Aliskiren In Combination With Other Antihypertensives

Hydrochlorothiazide

Aliskiren 75, 150, and 300 mg and hydrochlorothiazide 6.25, 12.5, and 25 mg were studied alone and in combination in an 8-week, 2,776-patient, randomized, double-blind, placebo-controlled, parallel-group, 15-arm factorial study. Blood pressure reductions with the combinations were greater than the reductions with the monotherapies as shown in Table 2.

Table 2: Placebo-Subtracted Reductions in Seated Trough Cuff Blood Pressure in Combination with Hydrochlorothiazide

View Enlarged Table
Valsartan

Aliskiren 150 and 300 mg and valsartan 160 and 320 mg were studied alone and in combination in an 8-week, 1,797patient, randomized, double-blind, placebo-controlled, parallel-group, 4-arm, dose-escalation study. The dosages of aliskiren and valsartan were started at 150 and 160 mg, respectively, and increased at four weeks to 300 mg and 320 mg, respectively. Seated trough cuff blood pressure was measured at baseline, 4, and 8 weeks. Blood pressure reductions with the combinations were greater than the reductions with the monotherapies as shown in Table 3.

Table 3: Placebo-Subtracted Reductions in Seated Trough Cuff Blood Pressure in Combination with Valsartan

Aliskiren, mg change Placebo mean Valsartan, mg
0 160 320
0 4.6/4.1* -- 5.6/3.9 8.2/5.6
150 -- 5.4/2.7 10.0/5.7 --
300 -- 8.4/4.9 -- 12.6/8.1
* The placebo change is 5.2/4.8 for week 4 endpoint which was used for the dose groups containing Aliskiren 150 mg or Valsartan 160 mg.
Amlodipine

Aliskiren 150 mg and 300 mg and amlodipine besylate 5 mg and 10 mg were studied alone and in combination in an 8week, 1,685-patient, randomized, double-blind, placebo-controlled, multifactorial study. Treatment with aliskiren and amlodipine resulted overall in significantly greater reductions in diastolic and systolic blood pressure compared to the respective monotherapy components as shown in Table 4.

Table 4: Placebo-Subtracted Reductions in Seated Trough Cuff Blood Pressure in Combination with Amlodipine

Aliskiren, mg Placebo mean change Amlodipine, mg
0 5 10
0 5.4/6.8 -- 5.6/9.0 8.5/14.3
150 -- 2.6/3.9 8.6/13.9 10.8/17.1
300 -- 4.9/8.6 9.6/15.0 11.1/16.4
ACE inhibitors

Aliskiren has not been studied when added to maximal doses of ACE inhibitors to determine whether aliskiren produces additional blood pressure reduction.

Aliskiren In Patients With Diabetes Treated With ARB Or ACEI (ALTITUDE Study)

Patients with diabetes with renal disease (defined either by the presence of albuminuria or reduced GFR) were randomized to aliskiren 300 mg daily (n=4296) or placebo (n=4310). All patients were receiving background therapy with an ARB or ACEI. The primary efficacy outcome was the time to the first event of the primary composite endpoint consisting of cardiovascular death, resuscitated sudden death, non-fatal myocardial infarction, non-fatal stroke, unplanned hospitalization for heart failure, onset of end stage renal disease, renal death, and doubling of serum creatinine concentration from baseline sustained for at least one month. After a median follow up of about 32 months, the trial was terminated early for lack of efficacy. Higher risk of renal impairment, hypotension and hyperkalemia was observed in aliskiren compared to placebo treated patients, as shown in the table below.

Table 5: Incidence of Selected Adverse Events During the Treatment Phase in ALTITUDE

  Aliskiren
N=4272
Placebo
N=4285
Serious Adverse Events* (%) Adverse Events (%) Serious Adverse Events* (%) Adverse Events (%)
Renal impairment † 5.7 14.5 4.3 12.4
Hypotension †† 2.3 19.9 1.9 16.3
Hyperkalemia ††† 1 38.9 0.5 28.8
†renal failure, renal failure acute, renal failure chronic, renal impairment
††dizziness, dizziness postural, hypotension, orthostatic hypotension, presyncope, syncope
††† Given the variable baseline potassium levels of patients with renal insufficiency on dual RAAS therapy, the reporting of adverse event of hyperkalemia was at the discretion of the investigator.
* A Serious Adverse Event (SAE) is defined as: an event which is fatal or life-threatening, results in persistent or significant disability/incapacity, constitutes a congenital anomaly/birth defect, requires inpatient hospitalization or prolongation of existing hospitalization, or is medically significant (i.e. defined as an event that jeopardizes the patient or may require medical or surgical intervention to prevent one of the outcomes previously listed).

The risk of stroke (3.4% aliskiren vs 2.7% placebo) and death (8.4% aliskiren vs. 8.0% placebo) were also numerically higher in aliskiren treated patients.


This monograph has been modified to include the generic and brand name in many instances.

Patient Information

Tekturna
(pronounced tek-turn-a)
(aliskiren) Tablets

Dosing Strengths: 150 mg tablets 300 mg tablets

Available by Prescription Only

Read the patient information that comes with Tekturna before you start taking it and each time you get a refill. There may be new information. This leaflet does not replace talking to your doctor about your condition or treatment. If you have any questions about Tekturna, ask your doctor or pharmacist.

What is the most important information I should know about Tekturna?

Tekturna can cause harm or death to an unborn baby. Talk to your doctor about other ways to lower your blood pressure if you plan to become pregnant. If you get pregnant while taking Tekturna, tell your doctor right away.

What Is Tekturna?

Tekturna can help your blood vessels relax and widen so blood pressure is lower. Tekturna is a type of prescription medicine called a direct renin inhibitor. By reducing renin, it helps to reduce blood pressure.

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. Drugs that lower blood pressure lower your risk of having a stroke or heart attack.

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.

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.
  • If you have diabetes and are taking a kind of medicine called an angiotensin-receptor-blocker or angiotensin-converting-enzyme-inhibitor.
  • Do not take Tekturna if you are allergic to any of its ingredients. See the end of this leaflet for a complete list of the ingredients in Tekturna.
  • 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:

  • have kidney problems.
  • are pregnant or planning to become pregnant, see “What is the most important information I should know about Tekturna?”
  • 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.
  • are allergic to any of the ingredients in Tekturna, see “What are the ingredients in Tekturna?”
  • have ever had a reaction called angioedema, to an ACE inhibitor medicine. Angioedema causes swelling of the face, lips, tongue, throat, arms, and legs, and may cause difficulty breathing.

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:

  • a kind of medicine called angiotensin receptor blocker or angiotensin converting enzyme inhibitor
  • Atorvastatin (medicine to lower cholesterol in your blood).
  • water pills (also called “diuretics”).
  • medicines for treating fungus or fungal infections.
  • cyclosporine (a medicine used to suppress the immune system).
  • potassium-containing medicines, potassium supplements, or salt substitutes containing potassium.
  • nonsteroidal anti-inflammatory drugs (like ibuprofen or naproxen)

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. 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 serious side effects:

  • Injury or death to an unborn baby. See “What is the most important information I should know about Tekturna?”
  • 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.
  • Severe Allergic Reactions and Angioedema. Aliskiren may cause difficulty breathing or swallowing, tightness of the chest, hives, general rash, swelling, itching, dizziness, vomiting, or abdominal pain (signs of a severe allergic reaction). Aliskiren can also cause swelling of the face, lips, tongue, throat, arms and legs or the whole body (signs of angioedema). Get medical help right away and tell your doctor if you get any one or more of these symptoms. Angioedema can happen at any time while you are taking Tekturna.
  • Renal impairment or failure. Aliskiren may cause renal disorder with symptoms such as severely decreased urine output or decreased urine output (signs of renal impairment or failure).

Common side effects of Tekturna include:

diarrhea
cough
dizziness
headache
flu-like symptoms
back pain
tiredness
high levels of potassium in the blood (hyperkalemia)

Less common side effects include rash, severe skin reactions (signs may include severe blistering of the lips, eyes or mouth, rash with fever and skin peeling) and liver disorder (signs may include nausea, loss of appetite, dark colored urine or yellowing of skin and eyes).

Tell your doctor if you have any side effect that bothers you or that does not go away. These are not all of the possible side effects of Tekturna. For a complete list of side effects, ask your doctor or pharmacist.

How Do I Store Tekturna?

  • Store Tekturna tablets at room temperature between 59°to 86°F (15°-30°C).
  • 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

Medicines are sometimes prescribed for conditions not listed in the patient information leaflet. Do not take Tekturna for a condition for which it was not prescribed. 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. If you have more questions about Tekturna talk with your doctor. You can ask your doctor or pharmacist for information that is written for healthcare professionals.

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

What are the ingredients in Tekturna?

Active Ingredients: Aliskiren (Tekturna)

Inactive Ingredients: colloidal silicone dioxide, crospovidone, hypromellose, iron oxide colorants, magnesium stearate, microcrystalline cellulose, polyethylene glycol, talc, and titanium dioxide.


This monograph has been modified to include the generic and brand name in many instances.

Consumer Overview Uses

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

 

ALISKIREN - ORAL

 

(AL-is-KYE-ren)

 

COMMON BRAND NAME(S): Tekturna

 

WARNING: This drug can cause serious (possibly fatal) harm to an unborn baby if used during pregnancy. Therefore, it is important to prevent pregnancy while taking this medication. Consult your doctor for more details and to discuss the use of reliable forms of birth control while taking this medication. If you are planning pregnancy, become pregnant, or think you may be pregnant, contact your doctor immediately.

 

USES: This medication is used to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Aliskiren works by relaxing blood vessels so blood can flow more easily.

 

HOW TO USE: Read the Patient Information Leaflet available from your pharmacist before you start using aliskiren and each time you get a refill. If you have any questions, consult your doctor or pharmacist.

Take this medication by mouth, usually once daily or as directed by your doctor. The dosage is based on your medical condition and response to treatment. Some foods may decrease how well this drug is absorbed by your body. You may take this medication with or without food, but it is important to choose one way and take this medication the same way with every dose. If you are unclear about how to take this medication, ask your doctor or pharmacist.

Do not take with fruit juices (such as apple, grapefruit, or orange) since they may decrease the absorption of this drug.

Take this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day. It is important to continue taking this medication even if you feel well. Most people with high blood pressure do not feel sick.

For the treatment of high blood pressure, it may take 2 weeks before you get the full benefit of this drug.

Tell your doctor if your condition does not improve or if it worsens (your blood pressure readings remain high or increase).

Consumer Overview Side Effect

SIDE EFFECTS: Upset stomach, diarrhea, dizziness, lightheadedness, or cough may occur as your body adjusts to the medication. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

To lower your risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: symptoms of a high potassium blood level (such as muscle weakness, slow/irregular heartbeat), fainting, change in the amount of urine.

Get medical help right away if you have any very serious side effects, including: seizure.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

 

Read the Tekturna (aliskiren tablets) Side Effects Center for a complete guide to possible side effects

Learn More »

PRECAUTIONS: Before taking aliskiren, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: diabetes, gout, heart problems, kidney disease (including kidney stones), loss of too much body water (dehydration), untreated mineral imbalance (such as low sodium, high potassium).

This drug may make you dizzy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Limit alcoholic beverages.

This medication may increase your potassium levels. Before using potassium supplements or salt substitutes that contain potassium, consult your doctor or pharmacist.

Before having surgery, tell your doctor or dentist that you are taking this medication.

This medication is not recommended for use during pregnancy due to the risk for harm to an unborn baby. Consult your doctor for more details. (See also Warning section.)

It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

Consumer Overview Missed Dose

DRUG INTERACTIONS: See also How to Use and Precautions sections.

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.

Some products that may interact with this drug include: atorvastatin, furosemide, drugs that may increase the level of potassium in the blood (including amiloride, triamterene, ACE inhibitors such as lisinopril/fosinopril/quinapril, ARBs such as irbesartan/candesartan/telmisartan, birth control pills containing drospirenone).

Other medications can affect the removal of aliskiren from your body, which may affect how aliskiren works. Examples include azole antifungals (such as itraconazole), cyclosporine, quinidine, among others.

Check the labels on all your medicines (such as cough-and-cold products, diet aids, or NSAIDs such as ibuprofen, naproxen) because they may contain ingredients that could increase your blood pressure. Ask your pharmacist for more details.

 

OVERDOSE: If overdose is suspected, contact a poison control center or emergency room immediately. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: fainting, severe dizziness.

 

NOTES: Do not share this medication with others.

Talk with your doctor about making changes to your lifestyle that may increase the effectiveness of this medication (e.g., stress reduction programs, exercise, and dietary changes).

Laboratory and/or medical tests (such as kidney function, blood potassium/uric acid levels) may be performed regularly to monitor your progress or check for side effects. Consult your doctor for more details.

Have your blood pressure checked regularly while taking this medication. Learn how to monitor your own blood pressure at home, and share the results with your doctor.

 

MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

 

STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

 

Information last revised November 2013. Copyright(c) 2013 First Databank, Inc.

Patient Detailed Side Effect

Brand Names: Tekturna

Generic Name: aliskiren (Pronunciation: a LIS ke rin)

  • What is aliskiren (Tekturna)?
  • What are the possible side effects of aliskiren (Tekturna)?
  • What is the most important information I should know about aliskiren (Tekturna)?
  • What should I discuss with my health care provider before taking aliskiren (Tekturna)?
  • How should I take aliskiren (Tekturna)?
  • What happens if I miss a dose (Tekturna)?
  • What happens if I overdose (Tekturna)?
  • What should I avoid while taking aliskiren (Tekturna)?
  • What other drugs will affect aliskiren (Tekturna)?
  • Where can I get more information?

What is aliskiren (Tekturna)?

Aliskiren is an anti-hypertensive (blood pressure lowering) medication. It works by decreasing substances in the body that narrow blood vessels and raise blood pressure.

Aliskiren is used to treat high blood pressure (hypertension).

Aliskiren may also be used for purposes not listed in this medication guide.

Tekturna 150 mg

round, pink, imprinted with NVR, IL

What are the possible side effects of aliskiren (Tekturna)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; severe stomach pain; difficult breathing; swelling of your face, lips, tongue, or throat.

If you have an allergic reaction to aliskiren you should not take it again.

Call your doctor at once if you have a serious side effect such as:

  • feeling light-headed, fainting;
  • nausea with slow uneven heart rate and a weak pulse;
  • swelling around your eyes; or
  • severe skin reaction -- fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.

Less serious side effects may include:

  • stomach pain or upset, diarrhea, heartburn;
  • itching or skin rash;
  • headache, dizziness, tired feeling;
  • back pain, joint pain or swelling; or
  • stuffy nose, sore throat, cough.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the Tekturna (aliskiren tablets) Side Effects Center for a complete guide to possible side effects

Learn More »

What is the most important information I should know about aliskiren (Tekturna)?

Do not use this medication if you are pregnant. Aliskiren can cause injury or death to the unborn baby if you take the medicine during your second or third trimester. Stop using this medication and tell your doctor right away if you become pregnant.

Before you take aliskiren, tell your doctor if you have kidney disease, heart disease, if you are on a low-salt diet, or if you have ever had an allergic reaction to a heart or blood pressure medication.

If you take aliskiren with meals, avoid high-fat foods. They can make it harder for your body to absorb aliskiren.

Conditions that may cause very low blood pressure include: vomiting, diarrhea, heavy sweating, heart disease, dialysis, a low-salt diet, or taking diuretics (water pills). Follow your doctor's instructions about the type and amount of liquids you should drink while taking aliskiren. Tell your doctor if you have a prolonged illness that causes diarrhea or vomiting.

 

Patient Detailed How Take

What should I discuss with my health care provider before taking aliskiren (Tekturna)?

You should not take aliskiren if you are allergic to it.

If you have diabetes or kidney disease, you may not be able to take aliskiren if you are also taking any of the following heart or blood pressure medications:

  • azilsartan (Edarbi, Edarbyclor), candesartan (Atacand), eprosartan (Teveten), irbesartan (Avapro, Avalide), losartan (Cozaar, Hyzaar), olmesartan (Benicar), valsartan (Diovan), telmisartan (Micardis); or
  • benazepril (Lotensin), captopril (Capoten), enalapril (Vasotec), fosinopril (Monopril), lisinopril (Prinivil, Zestril), moexipril (Univasc), perindopril (Aceon), quinapril (Accupril), ramipril (Altace), or trandolapril (Mavik, Tarka).

To make sure you can safely take aliskiren, tell your doctor if you have any of these other conditions:

  • kidney disease (or if you are on dialysis);
  • heart disease;
  • if you are on a low-salt diet; or
  • if you have ever had an allergic reaction to an ACE (angiotensin converting enzyme) inhibitor medication such as benazepril (Lotensin), enalapril (Vasotec), lisinopril (Prinivil, Zestril), quinapril (Accupril), ramipril (Altace), and others.

FDA pregnancy category D. Do not use this medication if you are pregnant. Aliskiren can cause injury or death to the unborn baby if you take the medicine during your second or third trimester. Stop using this medication and tell your doctor right away if you become pregnant.

It is not known whether aliskiren passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How should I take aliskiren (Tekturna)?

Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Your doctor may occasionally change your dose to make sure you get the best results.

Take aliskiren with a full glass of water.

You may take aliskiren with or without food, but take it the same way every time.

If you take aliskiren with meals, avoid high-fat foods. They can make it harder for your body to absorb aliskiren.

Conditions that may cause very low blood pressure include: vomiting, diarrhea, heavy sweating, heart disease, dialysis, a low-salt diet, or taking diuretics (water pills). Follow your doctor's instructions about the type and amount of liquids you should drink while taking aliskiren. Tell your doctor if you have a prolonged illness that causes diarrhea or vomiting.

If you are being treated for high blood pressure, keep using this medication even if you feel fine. High blood pressure often has no symptoms.

Store at room temperature away from moisture and heat.

Side Effects Centers
  • Tekturna

Patient Detailed Avoid Taking

What happens if I miss a dose (Tekturna)?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose (Tekturna)?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include feeling light-headed or fainting.

What should I avoid while taking aliskiren (Tekturna)?

Avoid drinking alcohol. It can further lower your blood pressure and may increase some of the side effects of aliskiren.

Do not use salt substitutes or potassium supplements while taking aliskiren, unless your doctor has told you to.

What other drugs will affect aliskiren (Tekturna)?

Tell your doctor about all other medicines you use, especially:

  • atorvastatin (Lipitor);
  • cyclosporine (Gengraf, Neoral, Sandimmune);
  • furosemide (Lasix);
  • antifungal medication such as fluconazole (Diflucan), itraconazole (Sporanox), or ketoconazole (Nizoral);
  • non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen (Advil, Motrin), naproxen (Aleve, Naprosyn, Naprelan, Treximet), celecoxib (Celebrex), diclofenac (Arthrotec, Cambia, Cataflam, Voltaren, Flector Patch, Pennsaid, Solareze), indomethacin (Indocin), meloxicam (Mobic), and others;
  • a potassium supplement such as K-Dur, Klor-Con;
  • salt substitutes that contain potassium; or
  • a diuretic (water pill).

This list is not complete and other drugs may interact with aliskiren. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

Where can I get more information?

Your pharmacist can provide more information about aliskiren.


Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

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