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 ?
M2 EQUITYBITES-November 16, 2017-Noden Pharma awarded US FDA's approval for Tekturna (aliskiren) Oral Pellets for the treatment of hypertension
M2 PHARMA-November 16, 2017-Noden Pharma awarded US FDA's approval for Tekturna (aliskiren) Oral Pellets for the treatment of hypertension
Noden Pharma DAC is a new privately held company (Noden) that has executed a purchase agreement with Novartis AG (Novartis) to acquire exclusive worldwide rights to manufacture, market, and sell the branded prescription medicine product sold under the name Tekturna and Tekturna HCT in the United States and Rasilez and Rasilez HCT in the rest of the world.
RENIN INHIBITORS: Diarrhea, headache, Tekturna Renin is an enzyme dizziness, and (aliskiren).
But the hypertension market growth will be countered by significant drug patent expirations both prior to and during the forecast period, including those of Cozaar in 2010, Diovan, Avapro and Atacand in 2012, Exforge in 2014, Benicar in 2016, and Tekturna and Tekturna HCT in 2018.
Tekturna works by inhibiting renin, a kidney enzyme that helps regulate blood pressure.
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.
5; 5/160/25; 10/160/25; 10/320/25 Central a-Agonist + Thiazide Diuretic Methyldopa/HCTZ Aldoril 250/15; 250/25 Mod D 500/30; 500/50 Direct Renin Inhibitor + Angiotensin II Receptor Blocker Aliskiren/valsartan Valturna 150/160; 300/320 Direct Renin Inhibitor + Calcium Channel Blocker Aliskiren + amiodipine Tekamlo 150/5; 150/10; 300/5; 300/10 Direct Renin Inhibitor + Thiazide Diuretic Aliskiren/HCTZ Tekturna HCT 150/12.
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.