MICARDROXI 80
-
Chemical Name:
Telmisartan -
Therapeutic Category:
Cardiovascular drugs -
Pharmacologic Category:
Angiotensin II Receptor Blocker -
Pharmaceutical Form:
Tablets -
Composition:
Telmisartan 80mg
MICARD ROXI
Tablets
Telmisartan 40-80 mg
1.COMPOSITION:
MICARD ROXI 40: Each tablet contains 40 mg Telmisartan.
MICARD ROXI 80: Each tablet contains 80 mg Telmisartan.
2.PHARMACOLOGY:
PHARMACODYNAMICS AND MECHANISM OF ACTION
Telmisartan is an orally effective and specific angiotensin II receptor (type AT1) antagonist. Telmisartan displaces angiotensin II with very high affinity from its binding site at the AT1 receptor , which is responsible for the known actions of angiotensin II. The binding is long-lasting. Telmisartan does not exhibit any partial agonist activity at the AT1 receptor. Plasma aldosterons levels are decreased by telmisartan.
In man, an 80 mg dose of telmisartan almost completely inhibits the angiotensin II evoked blood pressure increase. After the first dose of telmisartan, the antihypertensive activity gradually becomes evident within 3 hours. The hypertensive effect persists constantly over 24 hours after dosing and includes the last 4 hours before the next dose. In patients with hypertension, telmisartan reduces both systolic and diastolic blood pressure without affecting pulse rate. The maximum reduction in blood pressure is generally attained 4weeks after the start of the treatment and is sustained during long-term therapy.
Upon abrupt cessation of treatment with telmisartan, blood pressure gradually returns to pretreatment values over a period of several days without evidence of rebound hypertension.
PHARMACOKINETICS:
Absorption: Following oral administration, peak concentrations (Cmax) of telmisartan are reached in 0.5 to 1 hour after dosing.
Absorption of telmisartan is rapid although the amount absorbed varies. The mean absolute bioavailability of telmisartan is dose dependent at 40---160 mg the bioavailability was 42&58 % respectively.
Distribution: Telmisartan is highly bound to plasma proteins ( > 99.5%), mainly albumin and α1 - acid glycoprotein.
Metabolism and Elimination: Most of the administered dose ( > 97%) was eliminated unchanged in feces via biliary excretion; Telmisartan is metabolized by conjugation to form a pharmacologically inactive acyl glucuronide. Telmisartan is characterized by a terminal half-life of approximately 24hours. There is no evidence of clinically relevant accumulation of telmisartan.
Patients with renal impairment: lower plasma concentrations were observed in patients with renal insufficiency undergoing dialysis. Telmisartan is highly bound to plasma protein in renal-insufficient subjects and cannot be removed by dialysis. The elimination half-life is not changed in patients with renal impairment.
Patients with hepatic impairment: Pharmacokinetics studies in patients with hepatic impairment showed an increase in absolute bioavailability up to nearly 100%. The elimination half-life is not changed in patients with hepatic impairment.
3.INDICATIONS:
MICARD ROXI is indicated for:
- Treatment of hypertension
- Reduction of the risk of myocardial infarction, stroke, or death from cardiovascular causes.
4.CONTRAINDICATIONS:
Hypersensitivity to the active ingredients or any of the excipients.
5.SIDE EFFECTS:
The following are expected adverse events for telmisartan: upper respiratory tract infection, sinusitis, pharyngitis, back pain, diarrhea , influenza-like symptoms, dyspepsia, myalgia, urinary tract infection, abdominal pain, headache, dizziness, pain, fatigue, coughing, hypertension, chest pain, nausea and peripheral edema.These undesirable effects have usually been mild and transient in nature and have only infrequently required discontinuation of therapy. The incidence of undesirable effects was not dose related. The overall incidence of adverse events reported with telmisartan was usually comparable to placebo. Casual association of these events with telmisartan could not be established.
6.SPECIAL PRECAUTIONS:
- Hypotension: Symptomatic hypotension (especially after the first dose), may occur in patients who are volume and/or sodium depleted by vigorous diuretic therapy, dietary salt restriction, diarrhea or vomiting. Such conditions should be corrected before the administration of telmisartan. Volume and/or sodium depletion should be corrected prior to administration of telmisartan.
- 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.
- Impaired Hepatic Function: As the majority of telmisartan is eliminated by biliary excretion, patients with biliary obstructive disorders or hepatic insufficiency can be expected to have reduced clearance. Initiate telmisartan at low doses and titrate slowly in these patients.
- Impaired Renal Function: In patients whose renal function may depend on the activity of rennin-angiotensin-aldosterone system (e.g., patients with severe congestive heart failure or renal dysfunction), treatment with angiotensin receptor antagonists has been associated with oliguria and/or progressive azotemia and (rarely) with acute renal failure.
7.DRUG INTERACTIONS:
- Aliskiren: Do not co-administer aliskiren with MICARD ROXI in patients with diabetes. Avoid use of aliskiren with MICARD ROXI in patients with renal impairment.
- Digoxin: A 20% increase in median plasma digoxin through concentration has been observed; monitoring of plasma digoxin levels should be considered.
- Lithium: Reversible increases in serum lithium concentrations and toxicity have been reported during concomitant administration of lithium with angiotensin II receptor antagonists including telmisartan. Careful monitoring of serum lithium levels is recommended during concomitant use.
- Non-Steroidal Anti-Inflammatory Agents: In patients who are elderly, or with compromised renal function, co-administration of NSAIDs, with angiotensin II receptor antagonists, may result in deterioration of renal function, including possible acute renal failure.
- Ramipril and Ramiprilat: When co-administering telmisartan and ramipril, the response may be greater because of possibly additive pharmacodynamic effects of the combined drugs, and also because of the increased exposure to ramipril and ramiprilat in the presence of telmisartan. Concominant use of MICARD ROXI and ramipril is not recommended.
8.PREGNANCY AND LACTATION:
- Pregnancy : Category D. When pregnancy is detected, MICARD ROXI tablets should be discontinued as soon as possible.
- Lactation: It is not known whether telmisartan is excreted in human milk. Decide whether to discontinue the drug, taking into account the importance of the drug to the mother.
9.DOSAGE AND ADMINISTRATION:
- Adults: The recommended dose is 40 mg once daily. Some patients may already benefit at a daily dose of 20 mg. In cases where the target blood pressure is not achieved, telmisartan dose can be increased to a maximum of 80 mg once daily. When considering raising the dose, it must be borne in mind that the maximum antihypertensive effect is generally attained four-eight weeks after the start of the treatment.
- Cardiovascular Risk Reduction:the recommended dose of MICARD ROXI tablets is 80mg once aday and can be administered with or without food. It is not known whether doses lower than 80mg of telmisartan are effective in reducing the risk of cardiovascular morbidity and mortality.
When initiating MICARD ROXI thereby for cardiovascular risk reduction monitoring of blood pressure is recommended and if appropriate adjustment of medication that lower blood pressure may be necessary.
Renal impairment: No dosage adjustment is required for patients with mild to moderate renal impairment. Telmisartan is not removed from the blood by hemofiltration.
- Hepatic impairment: In patients with mild to moderate hepatic impairment the dosage should not exceed 40 mg once daily.
- Elderly: No dosage adjustment is necessary.
- Children: There are no data on the safety and efficacy of MICARD ROXI in children.
10.OVERDOSAGE:
No data are available with regard to overdose in humans. If symptomatic hypotension should occur, supportive treatment should be instituted. Telmisartan is not removed by hemodialysis.
11.PACKAGING:
MICARD ROXI 40: 20 tablets package.
MICARD ROXI 80: 20 tablets package.
12.STORAGE:
Store at temperature between (15-30)˚C away from light and moisture.
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