(a lis kye' ren)
P / L: Contraindication for pregnancy & lactation (breast feeding)
|| See TERMINOLOGY & ABBREVIATIONS |
|Dosage & Administration||
Use with Other Antihypertensives
|Overdosage||Symptoms: Hypotension. Management: Treatment is supportive.|
|Special Precautions||Severe renal impairment, renovascular hypertension, sodium or volume depletion. Discontinue if diarrhoea is severe and persistent. Routine monitoring of electrolytes and renal function especially in patients with DM, kidney disease or heart failure. Children <18 yr.|
|Adverse Drug Reaction(s)||Diarrhoea, abdominal pain, dyspepsia, gastro-oesophageal reflux, hypotension, headache, dizziness, fatigue, back pain, cough, rashes, elevated uric acid, gout, renal calculi, hyperkalaemia and dose-related decreases in haemoglobin. Rarely, angioedema and seizures.|
|Drug Interactions||Increased risk of hypotension with other antihypertensives. Decreased aliskiren concentrations with irbesartan. Increased aliskiren concentration with atorvastatin and ketoconazole. Significant decrease in furosemideconcentrations with aliskiren. Increased risk of hyperkalaemia with potassium-sparing diuretics, potassium supplements or any substances that may increase serum potassium levels (e.g. heparin).
|Food Interaction||Possible decrease bioavailability of aliskiren with St John's Wort.|
|Pregnancy Category (FDA)||Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).|
|Storage||Oral: Store between 15-30°C (59-86°F).|
|Pharmacology||Aliskiren is an orally active, non-peptide renin inhibitor used in the management of hypertension. By inhibiting the enzyme renin, it prevents conversion of angiotensinogen into angiotensin I and therefore inhibits subsequent production of angiotensin II and aldosterone. Unlike ACE inhibitors and angiotensin II receptor antagonists which cause a compensatory rise in plasma renin activity, treatment with aliskiren decreases plasma renin activity and concentrations of angiotensin I, angiotensin II and aldosterone .
Absorption: Poorly absorbed from GI tract. Bioavailability: 2.5%. Peak plasma concentration: 1-3 hr. Absorption reduced when taken with high fat diet.
Distribution: Distributes extensively into extravascular space. Volume of distribution: 135 L. Protein binding: 50%.
Metabolism: Undergoes minimal metabolism. 1.4% of oral dose metabolised by cytochrome P450 isoenzyme CYP3A4.
Excretion: Excreted mainly in faeces and urine (25% of absorbed dose) as unchanged drug. Elimination half life: 24-40 hr. Steady state concentration: 7-8 days.
|ATC Classification||C09XA02 - aliskiren; Belongs to the class of renin-inhibitors. Used in the treatment of cardiovascular disease.|
Search Google: Aliskiren
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|Do not take aliskiren if you are pregnant. If you become pregnant while taking aliskiren, call your doctor immediately. Aliskiren may harm the fetus.|
Why is Aliskiren prescribed?
Aliskiren is used alone or in combination with some medications to treat high blood pressure. Aliskiren is in a class of medications called direct renin inhibitors. It works by decreasing certain natural chemicals that tighten the blood vessels, so blood vessels relax and the heart can pump blood more efficiently.
How should Aliskiren be used?
Aliskiren comes as a tablet to take by mouth. It is usually taken once a day. Aliskiren should be taken either always with food or always without food. Take aliskiren at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor to explain any part you do not understand. Take aliskiren exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Your doctor will probably start you on an low dose of aliskiren and may increase your dose after you have been taking Aliskiren for at least 2 weeks.
Aliskiren controls high blood pressure but does not cure it. Continue to take aliskiren even if you feel well. Do not stop taking aliskiren without talking to your doctor.
Ask your doctor for a copy of the manufacturer's information for the patient.
Other uses of Aliskiren
This medication may be prescribed for other uses; ask your doctor for more information.
What special precautions to follow?
Before taking aliskiren,
- inform your doctor if you are allergic to aliskiren, an angiotensin-converting enzyme (ACE) inhibitor such as benazepril, captopril , enalapril, fosinopril, lisinopril, moexipril, perindopril, quinapril, ramipril, and trandolapril, any other medications, or any of the ingredients in aliskiren tablets. Ask your check the patient information for a list of the ingredients.
- inform your doctor if you have diabetes (high blood sugar) and you are taking an angiotensin receptor blocker (ARB) such as azilsartan, candesartan, eprosartan, irbesartan, losartan, olmesartan, telmisartan, and valsartan (Diovan, in Diovan HCT, Exforge); or an angiotensin-converting enzyme (ACE) inhibitor. Your doctor will probably inform you not to take aliskiren if you have diabetes and you are taking one of these medications.
- inform your doctor what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: certain antifungals such as itraconazole; aspirin and other nonsteroidal anti-inflammatory medications (NSAIDS, such as ibuprofen and naproxen); atorvastatin; celecoxib; cyclosporine (Neoral, Sandimmune); diuretics ('water pills'); potassium supplements or potassium-containing medications;and any other medications for heart disease or high blood pressure. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
- inform your doctor if you have or have ever had diabetes, seizures, a heart attack or heart failure, or kidney disease.
- inform your doctor if you plan to become pregnant or if you are breast-feeding. Do not breast-feed while taking aliskiren.
- you should know that diarrhea, vomiting, not drinking enough fluids, and sweating a lot can cause a drop in blood pressure, which may cause light headedness and fainting. inform your doctor if you have any of these problems or develop them during your treatment.
What special dietary instructions to follow?
You should try to avoid eating a high fat meal (foods such as fried foods or fast foods) when taking aliskiren with a meal. You should not use salt substitutes containing potassium or take potassium supplements without first talking with your doctor.
What to do if I forget a dose?
Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.
What side effects can Aliskiren cause?
Aliskiren may cause side effects. inform your doctor if any of these symptoms are severe or do not go away:
Some side effects can be serious. If you experience any of these symptoms, stop taking aliskiren and call your doctor immediately or get emergency medical treatment:
lightheadedness and fainting
swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
blisters or peeling skin
difficulty swallowing or breathing
slow, weak, or irregular heart beat
Aliskiren may cause other side effects. Call your doctor if you have any unusual problems while taking Aliskiren.
What storage conditions are needed for Aliskiren?
Keep Aliskiren in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Do not remove the desiccant (drying agent) from the bottle, if one has been provided. Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.
In case of emergency/overdose
In case of overdose, consult your doctor. If the victim has collapsed or is not breathing, consult local medical emergency services.
Symptoms of overdose may include:
What other information to know?
Keep all appointments with your doctor and the laboratory. Your doctor may order lab tests to check your body's response to aliskiren.
Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.
It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.
Ref: MedlinePLus, U.S. National Library of Medicine.
This information is provided for reference only and not a replacement for and should only be used in conjunction with full consultation with a registered medical practitioner. It may not contain all the available information you require and cannot substitute professional medical care, nor does it take into account all individual circumstances. Although great effort has been made to ensure content accuracy, mph-bd shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise.
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