Drug ID: 1d00000052
Drug Name: Aliskiren and Amlodipine
Generic Names: Tekamlo
Category: Anti- Hypertensives
Legal Status: Non Opioid Prescription only drug
Indication for Mother: Category D
There is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience or studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.
Recommended Dose: The recommended initial once-daily dose is 150mg/5 mg. Titrate as needed to a maximum of 300-mg/10 mg.
Recommended In: This combination medication contains renin inhibitor and calcium channel blocker, prescribed for high blood pressure. Amlodipine relaxes (widens) blood vessels where as Aliskiren inhibits renin and increase the blood flow.
Directions For Use: It comes as a tablet to take by mouth, with or without food.
Storage: Store at 25°C. Protect from heat and moisture.
Dosage Forms: Tablet
Side Effects: Gastroenterology- Diarrhea, abdominal pain, indigestion, and gastroesophageal reflux.
Heart - Abnormal heart rhythm, slow heart rate, chest pain, fainting, low blood pressure, inflammation of blood vessels.
Central Nervous System - Sensory loss, tingling, tremor, sexual dysfunction, sleeplessness, nervousness, depression, abnormal dreams, anxiety, and depersonalization.
Gastrointestinal - Loss of appetite, constipation, difficulty in swallowing, flatulence, inflammation of pancreas, vomiting, gum swelling.
General - Allergic reaction, weakness, back pain, hot flushes, uneasiness, pain, rigors, weight gain, weight decrease.
Musculoskeletal - Joint pain, muscle pain, degenerative disease of a joint, muscle cramps.
Respiratory - Difficulty in breathing, nosebleed.
Skin - Angioedema, itching, rash.
In Case of Overdose: Aliskiren
Limited data are available related to overdosage in humans. The most likely manifestation of overdosage would be hypotension. If symptomatic hypotension should occur, provide supportive treatment.
Aliskiren is poorly dialyzed. Therefore, hemodialysis is not adequate to treat aliskiren overexposure.
Overdosage might be expected to cause excessive peripheral vasodilation with marked hypotension and possibly a reflex tachycardia. Marked and potentially prolonged systemic hypotension up to and including shock with fatal outcome have been reported.
If massive overdose should occur, initiate active cardiac and respiratory monitoring. Frequent blood pressure measurements are essential. Should hypotension occur, provide cardiovascular support including elevation of the extremities and the judicious administration of fluids. If hypotension remains unresponsive to these conservative measures, consider administration of vasopressors (such as phenylephrine) with attention to circulating volume and urine output. As amlodipine is highly protein bound, hemodialysis is not likely to be of benefit. Administration of activated charcoal to healthy volunteers immediately or up to two hours after ingestion of amlodipine has been shown to significantly decrease amlodipine absorption.
Avoid If: Contraindicated in patients with diabetes, and hypersensitivity.
Do not use aliskiren with angiotensin receptor blockers (ARBs) and the angiotensin converting enzyme inhibitors (ACEIs)in patients with diabetes.
Caution should be exercised in patients with history of angioedema, dehydration, low blood volume, high blood potassium, low-salt (sodium) diet, gout, heart, liver or kidney disease, low blood pressure, blood vessel problems, diabetes, any allergy, who are taking other medications, elderly, children, during pregnancy and breastfeeding.
It may cause dizziness, lightheadedness, or fainting, do not drive a car or operate machinery and get up slowly from bed while taking this medication.
It may cause a serious side effect called angioedema, with the following symptoms: swelling of the hands, face, lips, eyes, throat, or tongue; difficulty in swallowing or breathing or hoarseness. If it is so consult with your healthcare provider.
Monitor blood pressure, kidney function, and blood electrolyte levels.
Drug Interaction: No drug interaction studies have been conducted with aliskiren and amlodipine besylate, although studies with the individual aliskiren and amlodipine besylate components are described below.
Cyclosporine: Avoid co-administration of cyclosporine with aliskiren.
Itraconazole: Avoid co-administration of itraconazole with aliskiren.
Non-Steroidal Anti-Inflammatory Agents(NSAIDs) including selective Cyclooxygenase-2 inhibitors (COX-2 inhibitors): In patients who are elderly, volume-depleted (including those on diuretic therapy), or with compromised renal function, co-administration of NSAIDs, including selective COX-2 inhibitors with agents that affect the renin-angiotensin-aldosterone system, including aliskiren, may result in deterioration of renal function, including possible acute renal failure. These effects are usually reversible. Monitor renal function periodically in patients receiving aliskiren and NSAID therapy.
Dual Blockade of the renin-angiotensin-aldosterone system: The concomitant use of aliskiren with other agents acting on the renin-angiotensin-aldosterone system such as ACEIs or ARBs is associated with an increased risk of hypotension, hyperkalemia, and changes in renal function (including acute renal failure) compared to monotherapy. Monitor blood pressure, renal function, and electrolytes in patients on aliskiren and other agents that affect the renin-angiotensin-aldosterone system.
Furosemide: Oral co-administration of aliskiren and furosemide reduced exposure to furosemide. Monitor diuretic effects when furosemide is co-administered with aliskiren.
Simvastatin: Co-administration of simvastatin with amlodipine increases the systemic exposure of simvastatin. Limit the dose of simvastatin in patients on amlodipine to 20 mg daily.
CYP3A4 Inhibitors: Co-administration with CYP3A inhibitors (moderate and strong) result in increased systemic exposure to amlodipine warranting dose reduction. Monitor for symptoms of hypotension and edema when amlodipine is co-administered with CYP3A4 inhibitors to determine the need for dose adjustment.
CYP3A4 Inducers: No information is available on the quantitative effects of CYP3A4 inducers on amlodipine. Blood pressure should be monitored when amlodipine is co-administered with CYP3A4 inducers.