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| Primary information |
|---|
| ID | 10676 |
| Therapeutic ID | Th1148 |
| Protein Name | Aliskiren |
| Sequence | NA
|
| Molecular Weight | 551.7583 |
| Chemical Formula | C30H53N3O6 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | >95°C |
| 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 | NA |
| Metabolism | NA |
| Absorption | NA |
| NA |
| Clearance | NA |
| Categories | Renin inhibitor |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | Cyclosporine, Itraconazole: Avoid concomitant use |
| Target | Renin |
| Brand Name | Tekturna |
| Company | Physicians Total Care, Inc. |
| Brand Description | Physicians Total Care, Inc. |
| Prescribed For | This medication is used to treat high blood pressure (hypertension). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Aliskiren works by relaxing blood vessels so blood can flow more easily. It belongs to a class of drugs known as direct renin inhibitors. |
| Chemical Name | (2S,4S,5S,7S)-N-(2-carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3-methoxypropoxy)phenyl]-octanamide hemifumarate |
| Formulation | Tekturna is supplied as a light-pink, biconvex round tablet containing 150 mg of aliskiren, and as a light-red biconvex ovaloid tablet containing 300 mg of aliskiren. |
| Physical Appearance | 150 mg light pink biconvex round tablet, imprinted NVR/IL, 300 mg light red biconvex ovaloid round tablet, imprinted NVR/IU |
| Route of Administration | Oral route |
| Recommended Dosage | The usual recommended starting dose of Tekturna is 150 mg once daily. In patients whose blood pressure is not adequately controlled, the daily dose may be increased to 300 mg. The antihypertensive effect of a given dose is substantially attained (85-90%) by 2 weeks. |
| Contraindication | None |
| Side Effects | Hives; vomiting, severe stomach pain; dizziness, diarrhea, difficult breathing; swelling of your face, lips, tongue, or throat. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |