MICARDROXI-EXTRA 5/40
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Chemical Name:
Telmisartan - Amlodipine -
Therapeutic Category:
Cardiovascular drugs -
Pharmacologic Category:
Angiotensin II Receptor Blocker/ Calcium Channel Blocker -
Pharmaceutical Form:
Tablets -
Composition:
Telmisartan 40mg + Amlodipine 5mg
MICARD ROXI – EXTRA
Tablets
Telmisartan & Amlodipine (Besylate)
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WARNING: FETAL TOXICITY
When pregnancy is detected, discontinue telmisartan and amlodipine as soon as possible.
Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus.
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1-COMPOSITION:
MICARD ROXI-EXTRA 5/40- Tablets: Each tablet contains Amlodipine (Besylate) 5 mg+ Telmisartan 40 mg.
MICARD ROXI-EXTRA 10/40- Tablets: Each tablet contains Amlodipine (Besylate) 10 mg+ Telmisartan 40 mg.
MICARD ROXI-EXTRA 5/80- Tablets: Each tablet contains Amlodipine (Besylate) 5 mg+ Telmisartan 80 mg.
MICARD ROXI-EXTRA 10/80- Tablets: Each tablet contains Amlodipine (Besylate) 10 mg+ Telmisartan 80 mg
EXCIPIENT:
MICARD ROXI -EXTRA 5/40-10/40:
Sodium hydroxide, Povidone, Meglumine, Sorbitol, Magnesium stearate, Microcrystalline cellulose, Maize starch, Silicon Dioxide colloidal, Brilliant blue.
MICARD ROXI –EXTRA 5/80-10/80:
Sodium hydroxide, Povidone, Meglumine, Sorbitol, Magnesium stearate, Microcrystalline cellulose, Maize starch, Silicon Dioxide colloidal, Red Iron Oxide.
2-PHARMACOKINETICS:
Absorption:
telmisartan: peak concentrations are reached in 0.5 to 1 hour after dosing. Food slightly reduces the bioavailability of telmisartan. The absolute bioavailability of telmisartan is dose dependent.
Amlodipine: Peak plasma concentrations of amlodipine are reached 6 to 12 hours after administration of amlodipine alone. Absolute bioavailability has been estimated to be between 64% and 90%. The bioavailability of amlodipine is not altered by the presence of food.
Distribution:
Telmisartan: Telmisartan is highly bound to plasma proteins (> 99.5%).
Amlodipine: Approximately 93% of circulating amlodipine is bound to plasma proteins.
Metabolism and Elimination:
Telmisartan: (> 97%) was eliminated unchanged in feces.
Amlodipine: Amlodipine is extensively (about 90%) converted to inactive metabolites via hepatic metabolism with 10% of the parent compound and 60% of the metabolites excreted in the urine.
3-MECHANISM of ACTION:
Telmisartan: ACE inhibitor the biosynthesis of angiotensin II from angiotensin I. Telmisartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal glandIts action is therefore independent of the pathways for angiotensin II synthesis.
Amlodipine: is a dihydropyridine calcium channel blocker that inhibits selectively the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle . Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause areduction in peripheral vascular resistance and reduction in blood pressure.
4-INDICATIONS:
The treatment of hypertension, alone or with other antihypertensive agents which reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions reduce cardiovascular morbidity.
Telmisartan and Amlodipine tablets are indicated as initial therapy in patients likely to need multiple antihypertensive agents to achieve their blood pressure goals.
5-CONTRAINDICATIONS:
Telmisartan and Amlodipine tablets are contraindicated in patients with known hypersensitivity (e.g., anaphylaxis or angioedema) to Telmisartan, Amlodipine, or any other component of this product.
Do not co-administer aliskiren with Telmisartan and Amlodipine tablets in patients with diabetes.
6-ADVERSE REACTION:
Adverse reactions have generally been mild and transient in nature and have only infrequently required discontinuation of therapy.
The most common reasons for discontinuation of therapy with Telmisartan and Amlodipine were peripheral edema, dizziness, and hypotension (each ≤0.5%).
Adverse reactions that occurred at ≥2% higher incidence on Telmisartan and Amlodipine tablets than placebo were peripheral edema, dizziness, and back pain.
Adverse reactions of Telmisartan is upper respiratory tract infection ,back pain, sinusitis, diarrhea, pharyngitis.
It may occur elevations of liver chemistries. and amlodipine may cause Flushing, Palpitations, headache, Fatigue, Nausea, Abdominal pain ,Somnolence.
7-PRECAUTIONS:
Hypotension:
In patients with an activated renin-angiotensin system, such as volume- or salt-depleted patients (e.g.,those being treated with high doses of diuretics), symptomatic hypotension may occur after initiation of therapy Either correct this condition prior to administration of Telmisartan and Amlodipine, or start treatment under close medical supervision with a reduced dose.
If hypotension does occur, place the patient in the supine position and, if necessary, give an intravenous.
Hyperkalemia:
Hyperkalemia may occur particularly in patients with advanced renal impairment, heart failure, on renal replacement therapy, or on potassium supplements, potassium-sparing diuretics, potassium-containing salt substitutes or other drugs that increase potassium levels. Consider periodic determinations of serum electrolytes to detect possible electrolyte imbalances, particularly in patients at risk.
Patients with Impaired Hepatic Function:
Telmisartan:
Initiate Telmisartan at low doses and titrate slowly in these patients with biliary obstructive disorders or hepatic insufficiency.
Amlodipine:
The lowest dose of Telmisartan and Amlodipine tablet is 40/5 mg; therefore, initial therapy with Telmisartan and Amlodipine tablet is not recommended in hepatically impaired patients.
Renal Function Impairment:
In patients whose renal function may depend on the activity of the renin-angiotensin-aldosterone system (e.g., patients with severe congestive heart failure or renal dysfunction), treatment with angiotensin-converting enzyme (ACE) inhibitors and angiotensin receptor antagonists has been associated with oliguria and/or progressive azotemia and (rarely) with acute renal failure and/or death. Similar results may be anticipated in patients treated with Telmisartan.
In most patients no benefit has been associated with using two RAS inhibitors concomitantly. In general, avoid combined use of RAS inhibitors. Closely monitor blood pressure, renal function and electrolytes in patients on Telmisartan and Amlodipine and other agents that affect the RAS.
Risk of Myocardial Infarction or Increased Angina:
Amlodipine:
Worsening angina and acute myocardial infarction can develop after starting or increasing the dose of Telmisartan and Amlodipine, particularly in patients with severe obstructive coronary artery disease.
Heart Failure:
Closely monitor patients with heart failure.
8-DRUG INTERACTIONS:
A. Telmisartan:
Do not co-administer aliskiren with Telmisartan and Amlodipine in patients with diabetes. Avoid use of aliskiren with telmisartan and amlodipine tablets in patients with renal impairment (GFR <60 mL/min).
Digoxin :monitor Digoxin levels when initiating, adjusting, and discontinuing Telmisartan for the purpose of keeping the Digoxin level within the therapeutic range.
Lithium: Reversible increases in serum Lithium concentrations and toxicity have been reported during concomitant administration of Lithium ,monitor serum Lithium levels during concomitant use.
Non-Steroidal Anti-Inflammatory Agents including Selective Cyclooxygenase-2 Inhibitors (COX-2 Inhibitors): patients who are elderly, volume-depleted (including those on diuretic therapy), or with compromised renal function, co-administration of NSAIDs may result in deterioration of renal function, including possible acute renal failure. These effects are usually reversible. Monitor renal function periodically in patients receiving Telmisartan and NSAID therapy.
The antihypertensive effect of angiotensin II receptor antagonists, including Telmisartan may be attenuated by NSAIDs including selective COX-2 inhibitors.
Ramipril and Ramiprilat:
When co-administering Telmisartan and Ramipril, the response may be greater because of the possibly additive pharmacodynamic effects of the combined drugs, and also because of the increased exposure to Ramipril and Ramiprilat in the presence of Telmisartan. Co-administration of Telmisartan and Ramipril is not recommended.
B .Amlodipine:
Simvastatin:Limit the dose of simvastatin in patients on amlodipine.
Immunosuppressant :Amlodipine may increase the systemic exposure of cyclosporine or tacrolimus when co-administered. Frequent monitoring of trough blood levels of cyclosporine and tacrolimus is recommended and adjust the dose when appropriate.
Strong inhibitors of CYP3A4 (e.g., ketoconazole, itraconazole, ritonavir) may increase the plasma concentrations of amlodipine to a greater extent. Monitor for symptoms of hypotension and edema when amlodipine is co-administered with CYP3A4 inhibitors.
CYP3A4 Inducers :No information is available on the quantitative effects of CYP3A4 inducers (e.g., Carbamazepine, Phenobarbital, Phenytoin, Fosphenytoin, Primidone, Rifampicin, St. John's Wort) on Amlodipine. Patients should be monitored for adequate clinical effect when Amlodipine is co-administered with CYP3A4 inducers.
9-PREGNANCY: Category D
Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death.
10-NURSING MOTHERS:
It is not known whether Telmisartan is excreted in human milk, Decide whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
11-DOSAGE and ADMINISTRATION:
Telmisartan is an effective treatment of hypertension in once daily doses of 20 to 80 mg while amlodipine is effective in doses of 2.5 to 10 mg.
Dosage must be individualized and may be increased after at least 2 weeks. Most of the antihypertensive effect is apparent within 2 weeks and maximal reduction is generally attained after 4 weeks. The maximum recommended dose of Telmisartan and Amlodipine is 80/10 mg once daily.
Telmisartan and Amlodipine may be taken with or without food.
Telmisartan and Amlodipine may be used to provide additional blood pressure lowering for patients not adequately controlled with Amlodipine alone or with Telmisartan alone.
Patients treated with 10 mg Amlodipine who experience any dose-limiting adverse reactions such as edema, may be switched to Telmisartan and Amlodipine 40/5 mg once daily, reducing the dose of amlodipine without reducing the overall expected antihypertensive response.
Initial Therapy:
A patient may be initiated on Telmisartan and Amlodipine if it is unlikely that control of blood pressure would be achieved with a single agent. The usual starting dose of Telmisartan and Amlodipine is 40/5 mg once daily. Patients requiring larger blood pressure reductions may be started on Telmisartan and Amlodipine 80/5 mg once daily.
Initial therapy with Telmisartan and Amlodipine is not recommended in patients ≥75 years old or with hepatic impairment.
Correct imbalances of intravascular volume- or salt-depletion, before initiating therapy with Telmisartan and amlodipine tablets.
-DOSING in SPECIFIC POPULATIONS:
Renal impairment:
No initial dosage adjustment is required for patients with mild or moderate renal impairment. Titrate slowly in patients with severe renal impairment.
Hepatic Impairment:
In most patients, initiate amlodipine therapy at 2.5 mg. Titrate slowly in patients with hepatic impairment.
Patients 75 Years of Age and Older:
In most patients, initiate amlodipine therapy at 2.5 mg. Titrate slowly in patients 75 years of age and older.
12-OVER DOSAGE:
Telmisartan:
The most likely manifestations of over dosage with Telmisartan would be hypotension, dizziness, and tachycardia, supportive treatment should be instituted. Telmisartan is not removed by hemodialysis.
Amlodipine:
Over dosage cause excessive peripheral vasodilation with marked hypotension and a reflex tachycardia.
supportive treatment should be instituted .As amlodipine is highly protein bound, hemodialysis is not likely to be of benefit.
13-PACKAGING:
MICARD ROXI-EXTRA 5/40- Tablets: Carton package of 20 tablets in blister.
MICARD ROXI-EXTRA 10/40- Tablets: Carton package of 20 tablets in blister.
MICARD ROXI-EXTRA 5/80- Tablets: Carton package of 20 tablets in blister.
MICARD ROXI-EXTRA 10/80- Tablets: Carton package of 20 tablets in blister.
14-STORAGE:
Store MICARD ROXI-EXTRA- Tablets at 25ºC, excursion permitted to (15-30)ºC, Protect from light & moisture.
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