Tekturna

aliskiren

Tekturna

Pharmacologic class: Direct renin inhibitor

Pregnancy risk category C (first trimester), D (second and third trimesters)

Pregnancy risk category C (first trimester), D (second and third trimesters)

FDA Box Warning

• Drugs that act directly on the reninangiotensin system can cause injury and death to a developing fetus.

• Discontinue drug as soon as possible when pregnancy is detected.

Action

Decreases plasma renin activity and inhibits conversion of angiotensinogen to angiotensin

Availability

Tablets: 150 mg, 300 mg

Indications and dosages

Hypertension (alone or in combination with other antihypertensives)

Adults: Initially, 150 mg P.O. once daily; may increase to 300 mg if blood pressure isn't adequately controlled

Contraindications

• Concurrent use of angiotensin receptor blockers (ARBs) or ACE inhibitors in patients with diabetes

Precautions

Use cautiously in:
• patients with severe renal dysfunction, nephrotic syndrome, renovascular hypertension, or history of dialysis
• angioedema (laryngeal edema)
• concurrent use of ACE inhibitors or ARBs in patients with renal impairment (GFR less than 60 ml/minute; avoid use)
• concurrent use of NSAIDs including selective COX-2 inhibitors, potassium-sparing diuretics, potassium supplements, salt substitutes containing potassium, or other drugs that increase potassium levels
• females of childbearing age
• pregnant or breastfeeding patients
• children (safety and efficacy not established).

Administration

• Give consistently with or without food, but not with high-fat foods.

Adverse reactions

CNS: headache, fatigue

CV: dizziness, hypotension

EENT: nasopharyngitis

GI: diarrhea, gastroesophageal reflux

Musculoskeletal: back pain

Respiratory: upper respiratory tract infection, cough

Skin: rash

Other: edema, angioedema

Interactions

Drug-drug.ACE inhibitors, ARBs: increased risk of renal impairment, hypotension, and hyperkalemia

Cyclosporine, itraconazole: significantly increased aliskiren level

NSAIDs (including selective COX-2 inhibitors): increased risk of deterioration of renal function, including possible acute renal failure, and increased aliskiren antihypertensive effect

Drug-diagnostic tests.BUN, creatine kinase, potassium, serum creatinine, serum uric acid: increased values

Hematocrit, hemoglobin: decreased values

Drug-food.High-fat meals: decreased drug absorption

Patient monitoring

• Stay alert for signs and symptoms of renal dysfunction, especially in patients receiving NSAIDs.

Monitor patient for signs and symptoms of angioedema; discontinue drug if signs and symptoms are present.

Patient teaching

• Instruct patient to take drug consistently with or without food, but not with high-fat foods.
• Instruct patient not to stop drug suddenly because doing so could result in uncontrolled high blood pressure.
• Advise female to tell prescriber if she's pregnant or breastfeeding before taking drug.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, tests, and foods mentioned above.

aliskiren

(a-lis-ki-ren) ,

Rasilez

(trade name),

Tekturna

(trade name)

Classification

Therapeutic: antihypertensives
Pharmacologic: renin inhibitors
Pregnancy Category: D

Indications

Treatment of hypertension (alone or with other agents).

Action

Inhibition of renin results in decreased formation of angiotensin II, a powerful vasoconstrictor.

Therapeutic effects

Decreased BP.

Pharmacokinetics

Absorption: Poorly absorbed (bioavailability 2.5%).
Distribution: Unknown.
Metabolism and Excretion: 2% excreted unchanged in urine, remainder is probably metabolized (CYP3A4 enzyme system).
Half-life: 24 hr.

Time/action profile (antihypertensive effect)

ROUTEONSETPEAKDURATION
POunknown2 wk24 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity;Concurrent use with cyclosporine or itraconazole;Concurrent use with ACE inhibitors or ARBs in patients with diabetes or moderate-to-severe renal impairment (CCr <60 mL/min); Obstetric: May cause fetal injury or death—if pregnancy occurs, discontinue immediately; Lactation: Discontinue drug or use formula.
Use Cautiously in: Salt or volume depletion (correct before use);Severe renal impairment; Pediatric: Safety and efficacy not established.

Adverse Reactions/Side Effects

Respiratory

  • cough

Cardiovascular

  • hypotension

Gastrointestinal

  • abdominal pain
  • diarrhea (↑ in females and elderly)
  • dyspepsia
  • reflux

Miscellaneous

  • angioedema (life-threatening)

Interactions

Drug-Drug interaction

↑ risk of hyperkalemia, renal impairment, and hypotension with concurrent use of ACE inhibitors or angiotensin II receptor blockers in patients with diabetes or moderate-to-severe renal impairment (CCr <60 mL/min); concurrent use contraindicated.Blood levels are ↑ by atorvastatin, itraconazole, ketoconazole, verapamil, and cyclosporine ; avoid concurrent use with cyclosporine or itraconazole.May ↓ effects of furosemide.Antihypertensive effects may be ↑ by other antihypertensives, diuretics, and nitrates.↑ risk of hyperkalemia with concurrent use of ACE inhibitors, angiotensin II receptor blockerspotassium supplements, potassium-sparing diuretics, or potassium-containing salt substitutes.NSAIDs and selective COX-2 inhibitors may blunt the antihypertensive effect and ↑ the risk of renal dysfunction.High fat meals significantly ↓ absorption.

Route/Dosage

Oral (Adults) 150 mg/day initially; may be ↑ to 300 mg/day.

Availability

Tablets: 150 mg, 300 mg
In combination with: hydrochlorothiazide (Tekturna HCT), amlodipine (Tekamlo), and amlodipine/hydrochlorothiazide (Amturnide); see combination drugs.

Nursing implications

Nursing assessment

  • Monitor BP and pulse frequently during initial dose adjustment and periodically during therapy. Notify health care professional of significant changes. If an excessive fall in BP occurs, place patient in a supine position and administer IV 0.9% NaCl, if necessary. A transient hypotensive response does not contraindicate further therapy.
  • Monitor frequency of prescription refills to determine adherence.
  • Lab Test Considerations: May cause minor ↑ in BUN, serum creatinine, potassium, uric acid, and creatine kinase.
    • May cause small ↓ in hemoglobin and hematocrit.

Potential Nursing Diagnoses

Noncompliance (Patient/Family Teaching)

Implementation

  • Correct volume or sodium depletion prior to initiating therapy.
  • Oral: Administer at the same time each day without regard to meals.

Patient/Family Teaching

  • Instruct patient to take aliskiren as directed at the same time each day, even if feeling better. Take missed doses as soon as remembered, but not if almost time for next dose. Do not double doses. Do not share medication with others, even with same condition; may be harmful.
  • May cause dizziness. Caution patient to lie down and notify health care professional. Also, avoid driving and other activities requiring alertness until response to aliskiren is known.
  • Advise patient to report signs and symptoms of angioedema (swelling of face, extremities, eyes, lips, tongue, difficulty swallowing, or breathing) to health care professional immediately.
  • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
  • Advise female patients to notify health care professional if pregnancy is planned or suspected or if breast feeding. If pregnancy is detected, discontinue aliskiren as soon as possible.

Evaluation/Desired Outcomes

  • Decrease in BP without appearance of side effects. Antihypertensive effect is 90% attained by 2 wk.

Tekturna

a trademark for aliskiren.
Mentioned in ?
References in periodicals archive ?
The initial growth will be due to the increased penetration of fixed-dose combination drugs (Amturnide, Exforge Tribenzor, Azor, Tekturna HCT, Edarbyclor, Twynsta, Benicar HCT, Micardis Plus, Tekamlo, Valturna), a rise in the prevalence population from 181 million to 190 million at a CAGR of 0.
21 billion net profit posted in the final three months of 2011, when the Basel-based company took a hit from ending its clinical study into wider uses of the hypertension drug Tekturna.
The group is also expected to take a one-off charge of $900 million in the fourth quarter after stopping a study of Rasilez, also known as Tekturna, to treat high-risk patients with type-2 diabetes and renal impairment.
East Hanover, NJ, announced the FDA has approved Tekamlo (aliskiren and amlodipine) tablets, a single-pill for the treatment of high blood pressure combining the only approved direct rennin inhibitor, Tekturna (aliskiren), with the widely used calcium channel blocker amlodipine.
It cited strong sales of new blood pressure drugs Exforge and Tekturna, and cancer drugs Zometa and Femara.
Wall Street sees its key growth drivers (Diovan, Tekturna, Gleevec, Tasigna, Exjade and Aclasta) as the company's "cliff protection"--when branded drugs go off patent and face competition from generics.
The FDA issued the approval for Tekturna as the first in a new class of drugs called direct renin inhibitors.
In its first research update since 2006, Novartis said it will combine the newer heart pill Tekturna with Diovan as well as other treatments, and plans to bring them to market before Diovan's 2012 patent loss.
The FDA recently announced the approval of Tekturna (aliskiren) tablets for the treatment of high blood pressure, or hypertension, which affects an estimated 25 percent of Americans and causes increased risk of stroke, heart attack, kidney failure, heart failure and death.
Novartis AG, the Swiss drugmaker that faced setbacks to three products, said it plans to buy its research partner, Swiss biotech company Speedel, for about $880 million to hasten development of potential blockbuster blood-pressure drug Tekturna.
The launch of Tekturna will mark the first introduction of a new class of antihypertensive medication in more than a decade, and the drug will achieve blockbuster status by earning $2.