Aliskiren

Aliskiren Brand Name– Tekturna

What is Aliskiren

Aliskiren (SPP 100) is the first drug of the class of non-peptide, orally active renin inhibitors. It is approved for the treatment of hypertension, either alone or in combination with other antihypertensive agents.

When used in combination, most clinical experience available is with diuretics or valsartan. The clinical effects of combination therapy with aliskiren and angiotensin-converting enzyme inhibitors or beta blockers has not been established; specifically, its use in combination with maximum doses of ACE inhibitors has not been adequately studied.

Aliskiren is unique in the way it interupts the generation of angiotensin II by inhibiting renin within the renin-angiotesnin system (RAS) cascade. The ability of aliskiren to act on this highly specific rate-limiting step may present an advantage over ACE inhibitors and ARBs.

Futhermore, inhibition of angiotensin-converting enzymes causes an increase in angiotensin I (Ang I), which is then available for conversion to angiotensin II (Ang II) through pathways not blocked by ACE inhibitors. Given that renin inhibitors prevent the formation of both Ang I and Ang II, they may offer a therapeutic profile distinct from those of both ACE inhibitors and ARBs.

Renin inhibitors do not affect kinin metabolism and therefore would be expected to cause less dry cough or angioedema, which are characteristic side effects of ACE inhibitors. In addition, ARBs increase levels of Ang II, a biologically active vasoconstrictor, an effect that does not occur with renin inhibitors, resulting in major potential benefits in blood pressure control.

Use of drugs that inhibit the RAS is an effective way to interfere in the pathogenesis of cardiovascular and renal disorders. Aliskiren is also in phase III clinical trials for its potential use in the treatment of left ventricular hypertrophy and heart failure.

Aliskiren was approved by the FDA on March 5, 2007.

Indications

  • hypertension

For the treatment of hypertension either as monotherapy or in combination with other antihypertensive agents

Side Effects

  1. anemia
  2. angioedema
  3. back pain
  4. cough
  5. diarrhea
  6. dizziness
  7. fatigue
  8. gout
  9. headache
  10. hyperkalemia
  11. hyperuricemia
  12. hypotension
  13. infection
  14. nephrolithiasis
  15. peripheral edema
  16. pharyngitis
  17. rash
  18. renal failure (unspecified)
  19. seizures
  20. Stevens-Johnson syndrome
  21. teratogenesis
  22. toxic epidermal necrolysis

Monitoring Parameters

  • serum creatinine/BUN
  • serum potassium

Contraindications

  • ACE-inhibitor induced angioedema
  • angioedema
  • aortic stenosis
  • biliary cirrhosis
  • Black patients
  • breast-feeding
  • cardiomyopathy
  • cerebrovascular disease
  • children
  • coronary artery disease
  • diabetes mellitus
  • geriatric
  • heart failure
  • hepatic disease
  • hereditary angioedema
  • hyperkalemia
  • hypokalemia
  • hyponatremia
  • hypotension
  • hypovolemia
  • infants
  • myocardial infarction
  • neonates
  • pregnancy
  • renal artery stenosis
  • renal failure
  • renal impairment
  • surgery

Interactions

  • Aliskiren; Valsartan
  • Amiloride
  • Amiloride; Hydrochlorothiazide, HCTZ
  • Amlodipine; Atorvastatin
  • Amlodipine; Benazepril
  • Amlodipine; Celecoxib
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Amobarbital
  • Angiotensin II receptor antagonists
  • Angiotensin-converting enzyme inhibitors
  • Apomorphine
  • Apraclonidine
  • Aprepitant, Fosaprepitant
  • Asenapine
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atorvastatin
  • Atorvastatin; Ezetimibe
  • Azilsartan
  • Azilsartan; Chlorthalidone
  • Benazepril
  • Benazepril; Hydrochlorothiazide, HCTZ
  • Boceprevir
  • Bumetanide
  • Cabergoline
  • Candesartan
  • Candesartan; Hydrochlorothiazide, HCTZ
  • Captopril
  • Captopril; Hydrochlorothiazide, HCTZ
  • Cariprazine
  • Celecoxib
  • Ciprofloxacin
  • Citric Acid; Potassium Citrate
  • Citric Acid; Potassium Citrate; Sodium Citrate
  • Co-Enzyme Q10, Ubiquinone
  • Cobicistat
  • Conivaptan
  • Cyclosporine
  • Daclatasvir
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Dexmethylphenidate
  • Dextromethorphan; Guaifenesin; Potassium Guaiacolsulfonate
  • Diazoxide
  • Diclofenac
  • Diclofenac; Misoprostol
  • Diflunisal
  • Diphenhydramine; Ibuprofen
  • Diphenhydramine; Naproxen
  • Dronedarone
  • Drospirenone
  • Drospirenone; Estradiol
  • Drospirenone; Ethinyl Estradiol
  • Drospirenone; Ethinyl Estradiol; Levomefolate
  • Duloxetine
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Enalapril, Enalaprilat
  • Enalapril; Felodipine
  • Enalapril; Hydrochlorothiazide, HCTZ
  • Enflurane
  • Epoprostenol
  • Eprosartan
  • Eprosartan; Hydrochlorothiazide, HCTZ
  • Esomeprazole; Naproxen
  • Ethacrynic Acid
  • Etodolac
  • Etomidate
  • Famotidine; Ibuprofen
  • Fenoldopam
  • Fenoprofen
  • Flurbiprofen
  • Fosamprenavir
  • Fosinopril
  • Fosinopril; Hydrochlorothiazide, HCTZ
  • Fospropofol
  • Fostamatinib
  • Furosemide
  • General anesthetics
  • Glecaprevir; Pibrentasvir
  • Guaifenesin; Potassium Guaiacolsulfonate
  • Halothane
  • Hetastarch; Dextrose; Electrolytes
  • Hydralazine
  • Hydralazine; Hydrochlorothiazide, HCTZ
  • Hydralazine; Isosorbide Dinitrate, ISDN
  • Hydrochlorothiazide, HCTZ; Irbesartan
  • Hydrochlorothiazide, HCTZ; Lisinopril
  • Hydrochlorothiazide, HCTZ; Losartan
  • Hydrochlorothiazide, HCTZ; Moexipril
  • Hydrochlorothiazide, HCTZ; Olmesartan
  • Hydrochlorothiazide, HCTZ; Quinapril
  • Hydrochlorothiazide, HCTZ; Spironolactone
  • Hydrochlorothiazide, HCTZ; Telmisartan
  • Hydrochlorothiazide, HCTZ; Triamterene
  • Hydrochlorothiazide, HCTZ; Valsartan
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Ibritumomab Tiuxetan
  • Ibuprofen
  • Ibuprofen; Oxycodone
  • Ibuprofen; Pseudoephedrine
  • Idelalisib
  • Iloperidone
  • Iloprost
  • Indapamide
  • Indomethacin
  • Iodine; Potassium Iodide, KI
  • Irbesartan
  • Isavuconazonium
  • Isoflurane
  • Itraconazole
  • Ketamine
  • Ketoconazole
  • Ketoprofen
  • Ketorolac
  • Lansoprazole; Naproxen
  • Lesinurad
  • Lesinurad; Allopurinol
  • Lisdexamfetamine
  • Lisinopril
  • Lithium
  • Lomitapide
  • Loop diuretics
  • Lopinavir; Ritonavir
  • Losartan
  • Lumacaftor; Ivacaftor
  • Lurasidone
  • Meclofenamate Sodium
  • Mefenamic Acid
  • Meloxicam
  • Mepivacaine
  • Mepivacaine; Levonordefrin
  • Mestranol; Norethindrone
  • Minoxidil
  • Mitotane
  • Moexipril
  • Nabumetone
  • Naproxen
  • Naproxen; Pseudoephedrine
  • Naproxen; Sumatriptan
  • Nebivolol; Valsartan
  • Nefazodone
  • Nitroprusside
  • Nonsteroidal antiinflammatory drugs
  • Olmesartan
  • Ombitasvir; Paritaprevir; Ritonavir
  • Oxaprozin
  • Pazopanib
  • Pentoxifylline
  • Perindopril
  • Perindopril; Amlodipine
  • Piroxicam
  • Ponatinib
  • Posaconazole
  • Potassium
  • Potassium Acetate
  • Potassium Bicarbonate
  • Potassium Chloride
  • Potassium Citrate
  • Potassium Gluconate
  • Potassium Iodide, KI
  • Potassium-sparing diuretics
  • Prazosin
  • Propofol
  • Quinapril
  • Ramipril
  • Rasagiline
  • Ritonavir
  • Rofecoxib
  • Sacubitril; Valsartan
  • Sapropterin
  • Selegiline
  • Sevoflurane
  • Sildenafil
  • Silodosin
  • Sofosbuvir; Velpatasvir; Voxilaprevir
  • Spironolactone
  • Sulindac
  • Telaprevir
  • Telmisartan
  • Telotristat Ethyl
  • Thiothixene
  • Tizanidine
  • Tolmetin
  • Torsemide
  • Trandolapril
  • Trandolapril; Verapamil
  • Tranylcypromine
  • Triamterene
  • Valdecoxib
  • Valsartan
  • Vasodilators
  • Verapamil
  • Warfarin
  • Zonisamide
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