Detailed description page of ThPDB2
| This page displays user query in tabular form. |
Th1148 details |
| 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 |
| Primary information | |
|---|---|
| ID | 10677 |
| 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 | NA |
| Target | Renin |
| Brand Name | Tekturna |
| Company | Novartis Pharmaceuticals Corporation |
| Brand Description | Novartis Pharmaceuticals Corporation |
| 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 |
| Primary information | |
|---|---|
| ID | 10678 |
| 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 | Some products that may interact with this drug include: cisapride, dofetilide, lithium, drugs that may increase the level of potassium in the blood (including ACE inhibitors such as benazepril/lisinopril, ARBs such as candesartan/losartan, birth control pills containing drospirenone). |
| Target | Renin |
| Brand Name | Tekturna HCT |
| Company | Novartis Pharmaceuticals Corporation |
| Brand Description | Novartis Pharmaceuticals Corporation |
| Prescribed For | This product is used to treat high blood pressure (hypertension). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. This product contains 2 medications: aliskiren and hydrochlorothiazide. Aliskiren works by relaxing blood vessels so blood can flow more easily. It belongs to a class of drugs known as direct renin inhibitors. Hydrochlorothiazide causes your body to get rid of extra salt and water by making more urine. It is called a water pill or diuretic. |
| Chemical Name | NA |
| Formulation | Tekturna HCT is supplied as biconvex, ovaloid film-coated tablets. |
| Physical Appearance | 150 mg/12.5 mg tablets: white, biconvex ovaloid, film-coated tablets imprinted with NVR/LCI, 150 mg/25 mg tablets: pale yellow, biconvex ovaloid, film-coated tablets imprinted with NVR/CLL, 300 mg/12.5 mg tablets: violet white, biconvex ovaloid, film-coated tablets imprinted with NVR/CVI, 300 mg/2 |
| Route of Administration | Oral route |
| Recommended Dosage |  Initiate with 12.5 mg/150 mg PO qDay; after 2-4 weeks, may increase dose if needed; not to exceed 25 mg/300 mg |
| Contraindication | Do not use aliskiren with ARBs or ACEIs in patients with diabetes. Tekturna HCT is contraindicated in patients with anuria or hypersensitivity to sulfonamide derived drugs like HCTZ or to any of the components. Hypersensitivity reactions may range from urticaria to anaphylaxis. |
| Side Effects | Dizziness or lightheadedness may occur as your body adjusts to the medication. If either of these effects persists or worsens, tell your doctor or pharmacist promptly. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |
| Primary information | |
|---|---|
| ID | 10679 |
| 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 | Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): Increased risk of renal impairment and loss of antihypertensive effect, Simvastatin: Avoid doses greater than 20 mg daily.  |
| Target | Renin |
| Brand Name | Tekamlo |
| Company | Novartis Pharmaceuticals Corporation |
| Brand Description | Novartis Pharmaceuticals Corporation |
| 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 | NA |
| Formulation | Tablets (aliskireNAmlodipine): 150 mg/5 mg, 150 mg/10 mg, 300 mg/5 mg, 300 mg/10 mg |
| Physical Appearance | 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 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |
| Primary information | |
|---|---|
| ID | 10680 |
| 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 | Antidiabetic Drugs: Antidiabetic dosage adjustment may be required |
| Target | Renin |
| Brand Name | Amturnide |
| Company | Novartis Pharmaceuticals Corporation |
| Brand Description | Novartis Pharmaceuticals Corporation |
| 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 | NA |
| Formulation | Tablets (aliskiren/ amlodipine/ HCTZ): 150/5/12.5, 300/5/12.5, 300/5/25, 300/10/12.5, 300/10/25 mg. |
| Physical Appearance | 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 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |