A database of FDA approved therapeutic peptides and proteins
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1651 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 | Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): Increased risk of renal impairment and loss of antihypertensive effect, Simvastatin: Avoid doses greater than 20 mg daily. Â |
| Target | Renin |
| Information of corresponding available drug in the market | |
| Brand Name | Tekamlo |
| Company | Novartis Pharmaceuticals Corporation |
| Brand Discription | Aliskiren: Renin inhibitor; blocks effect of increased renin levels, thereby decreasing feedback loop and reducing plasma renin activity, angiotensin I, and angiotensin II. Amlodipine: Calcium channel blocker; inhibits extracellular Ca ions across the membranes of myocardial cells and vascular smooth muscle cells, resulting in inhibition of cardiac and vascular smooth muscle contraction; this action causes dilation of the main coronary and systemic arteries. |
| Prescribed for | Tekamlo is a combination of aliskiren, a renin inhibitor, and amlodipine, a dihydropyridine calcium channel blocker, indicated for the treatment of hypertension, alone or with other antihypertensive agents, 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): 150 mg/5 mg, 150 mg/10 mg, 300 mg/5 mg, 300 mg/10 mg |
| Physcial Appearnce | 150 mg aliskiren/5 mg amlodipine tablets: Non-scored light yellow, ovaloid convex shaped film-coated tablet with a beveled edge with debossing “T2†on one side and “NVR†on the reverse side of the tablet, 150 mg aliskiren/10 mg amlodipine tablets: Non-scored yellow, ovaloid convex shaped f |
| Route of Administration | Oral route |
| Recommended Dosage | The recommended initial once-daily dose of Tekamlo is 150 mg/5 mg. Titrate as needed to a maximum of 300 mg/10 mg. The blood pressure lowering effects are largely attained within 1 to 2 weeks. If blood pressure remains uncontrolled after 2 to 4 weeks of therapy, titrate the dose to a maximum of Tekamlo 300 mg/10 mg once daily. |
| Contraindication | Do not use with angiotensin receptor blockers (ARBs) or angiotensin-converting enzyme inhibitors (ACEIs) in patients with diabetes. Known hypersensitivity to any of the components. |
| Side Effects | Swelling of lower legs, diarrhea,dizziness, cough, flu-like symptoms, tiredness, high levels of potassium in the blood (hyperkalemia) |
| Useful Link | http://www.drugbank.ca/drugs/DB09026 |
| PubMed ID | 12927775 |
| 3-D Structure | N.A. |