A database of FDA approved therapeutic peptides and proteins
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1652 details |
| Primary information | |
|---|---|
| ThPP ID | Th1148 |
| Therapeutic Peptide/Protein Name | Aliskiren |
| Sequence | N.A. view full sequnce in fasta |
| Functional Classification | IIa |
| Molecular Weight | 551.75832 |
| Chemical Formula | C30H53N3O6 |
| Isoelectric Point | N.A. |
| Hydrophobicity | N.A. |
| Melting Point (℃) | N.A. |
| Half Life | 24 hours |
| Description | Aliskiren is an anti-hypertensive (blood pressure lowering) medicine. It works by decreasing substances in the body that narrow blood vessels and raise blood pressure. It is chemically, (2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-2-propan-2-ylnonanamide. |
| Indication/Disease | It is used to treat hypertension, renal impairment and hepatic impairment |
| Pharmacodynamics | Aliskiren shows high specificity for human renin, with almost no inhibitory effect against other aspartic peptidases such as cathepsin D and pepsin. Although aliskiren also exhibits high affinity for primate renin, it is significantly less active against renin from dog, rat, rabbit, pig and cat. This high potency for human renin compensates for the relatively low oral bioavailability of the drug. |
| Mechanism of Action | Renin inhibitor that inhibits the conversion of angiotensinogen to angiotensin I. The decrease in antiotensin I causes a decrease in angiotensin II, a potent blood pressure elevating peptide. |
| Toxicity | It can cause injury and death to the developing fetus |
| Metabolism | Metabolized by CYP3A4 |
| Absorption | Poorly absorbed; oral bioavailability is about 2.5%. |
| Volume of Distribution | N.A. |
| Clearance | Urine (25% as parent compound in urine)Â |
| Categories | Renin inhibitor |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| Drug Interaction | Antidiabetic Drugs: Antidiabetic dosage adjustment may be required |
| Target | Renin |
| Information of corresponding available drug in the market | |
| Brand Name | Amturnide |
| Company | Novartis Pharmaceuticals Corporation |
| Brand Discription | Amturnide is a combination of aliskiren, a renin inhibitor, amlodipine besylate, a dihydropyridine calcium channel blocker, and hydrochlorothiazide (HCTZ), a thiazide diuretic. |
| Prescribed for | Amturnide 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. |
| Chemical Name | N.A. |
| Formulation | Tablets (aliskiren/ amlodipine/ HCTZ): 150/5/12.5, 300/5/12.5, 300/5/25, 300/10/12.5, 300/10/25 mg. |
| Physcial Appearnce | Tablets are convex ovaloid with a beveled edge, film-coated, and unscored. |
| Route of Administration | Oral route |
| Recommended Dosage | Dose once-daily. The dosage may be increased after 2 weeks of therapy. The maximum recommended dose of Amturnide is 300/10/25 mg. High-fat meals decrease absorption of aliskiren substantially. |
| Contraindication | Do not use with angiotensin receptor blockers (ARBs) or angiotensin-converting enzyme inhibitors (ACEIs) in patients with diabetes, Anuria, Hypersensitivity to sulfonamide derived drugs or to any of the components. |
| Side Effects | Dizziness or lightheadedness as your body adjusts to the medication. Swelling hands/ankles/feet, flushing, headache, or diarrhea may also occur. |
| Useful Link | http://pubchem.ncbi.nlm.nih.gov/compound/Aliskiren#section=FDA-Pharmacological-Classification |
| PubMed ID | 12927775 |
| 3-D Structure | N.A. |