OLESTA PLUS®– Amlodipine and Olmesartan BP
COMPOSITION
20 Tablet: Each film coated tablet contains Amlodipine Besilate BP equivalent to Amlodipine 5 mg and Olmesartan Medoxomil BP 20 mg.
PHARMACOLOGY
This product is a combination of two antihypertensive drugs: Amlodipine is a dihydropyridine calcium antagonist and Olmesartan Medoxomil is an angiotensin-II receptor blocker.The Amlodipine component inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle and the Olmesartan Medoxomil component blocks the vasoconstrictor effects of angiotensin-II.
Pharmacokinetics:
Absorption
Amlodipine after oral administration of therapeutic doses of amlodipine, absorption produces peak plasma concentrations between 6 and 12 hours. Absolute bioavailability is estimated at between 64% and 90%. Olmesartan medoxomil Olmesartan medoxomil is rapidly and completely bioactivated by ester hydrolysis to olmesartan during absorption from the gastrointestinal tract. The absolute bioavailability of olmesartan medoxomil is approximately 26%. After oral administration, the peak plasma concentration (Cmax) of olmesartan is reached after 1 to 2 hours. Food does not affect the bioavailability of olmesartan medoxomil.
Distribution
Amlodipine Ex vivo studies have shown that approximately 93% of the circulating drug is bound to plasma proteins in hypertensive patients. Steady-state plasma levels of amlodipine are reached after 7 to 8 days of consecutive daily dosing. Olmesartan medoxomil The volume of distribution of olmesartan is approximately 17 L. Olmesartan is highly bound to plasma proteins (99%) and does not penetrate red blood cells. The protein binding is constant at plasma olmesartan concentrations well above the range achieved with recommended doses.
Metabolism
Amlodipine is extensively (about 90%) converted to inactive metabolites via hepatic metabolism. Olmesartan medoxomil following the rapid and complete conversion of olmesartan medoxomil to olmesartan during absorption, there is virtually no further metabolism of olmesartan.
Elimination
Elimination from the plasma is biphasic with a terminal elimination half-life of about 30 to 50 hours. Ten percent of the parent compound and 60% of the metabolites are excreted in the urine. Olmesartan appears to be eliminated in a biphasic manner with a terminal elimination half-life of approximately 13 hours.
INDICATION
Amlodipine Besilate & Olmesartan Medoxomil is indicated for the treatment of hypertension alone or with other antihypertensive agents. Amlodipine Besilate & Olmesartan Medoxomil may also be used as initial therapy in patients who are likely to need multiple antihypertensive agents to achieve their blood pressure goals.
DOSAGE & ADMINISTRATION
Initial therapy: The usual recommended dosage of Amlodipine Besilate & Olmesartan Medoxomil one tablet once daily. Amlodipine Besilate & Olmesartan Medoxomil 5/20 tablet may be administrated in patients whose blood pressure is not adequately controlled by Amlodipine Besilate & Olmesartan Medoxomil tablet. The dosage can be increased after 1 to 2 weeks of therapy to a maximum dose of 10/40 mg once daily as needed to control blood pressure. It may be taken with or without food. Initial therapy with this combination product is not recommended in patients 75 years old or with hepatic impairment.
Replacement therapy: Amlodipine Besilate & Olmesartan may be substituted for its individually titrated components. When substituting for individual components, the dose of one or both of the components can be increased if blood pressure control has not satisfactory.
SIDE EFFECTS
The most common side effects include peripheral oedema, dizziness, flushing, pruritus, vomiting, diarrhea, alopecia, etc. face oedema, hypersensitivity syncope urticaria etc.
PRECAUTION
When pregnancy is detected, this combination drug should be discontinued as soon as possible. Symptomatic hypotension may occur after initiation of therapy. Amlodipine Besilate & Olmesartan Medoxomil should be used with caution in patients with congestive heart failure, impaired renal function/ hepatic Impairment, patients with severe aortic stenosis, severe obstructive coronary artery disease. Patients may develop increased frequency, duration or severity of angina or acute MI on starting Calcium channel Blocker therapy or at the time of dosage increase.
CONTRAINDICATION
Aliskiren is contraindicated with Amlodipine Besilate & Olmesartan Medoxomil in patients with diabetes. It is also contraindicated in patients with anuria or hypersensitivity to either sulfonamide derived drug.
DRUG INTERACTION
With medicine: Based on experience with the use of other drugs that affect the renin-angiotensin system concomitant use of potassium-sparing diuretics, potassium supplements, salt substitutes containing potassium or other drugs that may increase serum potassium levels (e.g. heparin may lead to increases in serum potassium. Such concomitant use is therefore not recommended.
With food & others: Administration of Amlodipine with grapefruit or grapefruit juice is not recommended as bioavailability may be increased in some patients resulting in increased blood pressure lowering effects.
USE IN PREGNANCY AND LACTATION
Pregnancy: When pregnancy is detected, discontinue this combination product as soon as possible. When used in pregnancy during the second and third trimesters drugs that act directly on the rennin angiotensin system can cause injury and even death to the developing fetus.
Nursing Mothers: Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue the drug to the mother.
STORAGE
Store in a cool, dry place & below 30°C. Protected from light. Keep out of reach of children.
PACKAGING
Olesta Plus®: Tablet 20 mg: Each box contains 3 x 10’s film coated tablets in Alu-Alu blister pack.
