Omexta

OMEXTA (20 MG TABLET): Each tablet contains Olmesartan medoxomil 20 mg.
OMEXTA (40 MG TABLET): Each tablet contains Olmesartan medoxomil 40 mg.

Pharmacology: Pharmacodynamics: Olmesartan medoxomil is a selective angiotensin II receptor (type AT1) antagonist. It is expected to block all actions of angiotensin II mediated by the AT1 receptor, regardless of the source or route of synthesis of angiotensin II.
Angiotensin II is the primary vasoactive hormone of the renin-angiotensin-aldosterone system and plays a significant role in the pathophysiology of hypertension. Olmesartan medoxomil blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II and interacts reversibly at the AT1 and AT2 receptors of many tissues. Olmesartan medoxomil does not affect the response to bradykinin.
Pharmacokinetics: Olmesartan medoxomil is an ester prodrug that is hydrolyzed during absorption from the gastrointestinal tract to the active form Olmesartan. No further metabolism occurs. The absolute bioavailability is about 26%. Peak plasma concentrations of Olmesartan occur about 1 to 2 hours after oral doses. Olmesartan is at least 99% bound to plasma proteins. It is excreted in the urine and the bile as Olmesartan; about 35 to 50% of the absorbed dose is excreted in the urine and the remainder in feces via the bile. The terminal elimination half-life is 13 hours.

Treatment of essential hypertension.

Adults: Initial 20 mg once daily. After 2 weeks the dose may be increased to 40 mg once daily if required or hydrochlorothiazide may be added.
For patients with possible depletion of intravascular volume, particularly those with impaired renal function, Olmesartan medoxomil should be initiated in such patients under close medical supervision and consideration should be given to administering a lower initial dose of drug.
The antihypertensive effect of Olmesartan medoxomil generally is evident within 2 weeks, with a maximum reduction observed about by 8 weeks after initiating therapy.
Children and adolescents: The safety and efficacy of Olmesartan medoxomil have not been established in children and adolescents up to 18 years of age.
Geriatric: No initial dosage adjustment is required and the daily dose should not exceed 20 mg/day.
Renal impairment: The maximum dose is 20 mg once daily in mild to moderate impairment (creatinine clearance 20-60 mL/min) and not recommended in severe impairment (creatinine clearance less than 20 mL/min).
Hepatic impairment: Not recommended in patients with hepatic impairment.
Mode of administration: Olmesartan medoxomil is administered orally with or without food. It is recommended to be taken at about the same time each day.

Overdose and treatment: The most likely effect of overdosage is hypotension. In the event of overdosage, the patient should be carefully monitored and treatment should be symptomatic and supportive.

1. Hypersensitivity to Olmesartan medoxomil or any component of the formulation.
2. Second and third trimesters of pregnancy or lactation.
3. Patients with biliary obstruction.
4. Concomitant use with aliskiren in patients with diabetes mellitus.

In patients who are intravascular volume or salt depleted (e.g., those treated with diuretics, dietary salt restriction, diarrhea or vomiting), symptomatic hypotension may occur, especially after the first dose. Such conditions should be corrected before starting therapy.
Because the renin-angiotensin-aldosterone system appears to contribute substantially to maintenance of glomerular filtration in patients with heart failure in whom renal perfusion is severely compromised, renal function may deteriorate markedly (e.g., oliguria, progressive azotemia, renal failure) in these patients during therapy with an ACE inhibitor or an angiotensin II receptor antagonist (e.g., Olmesartan medoxomil). Renal artery stenosis also is a risk factor for renal impairment during therapy with drugs that inhibit the RAA system.
Use with caution in patients with unilateral/bilateral renal artery stenosis due to the elevated risk of deterioration in renal function and severe hypotension.
When Olmesartan medoxomil is used in patients with impaired renal function, periodic monitoring of serum potassium and creatinine levels is recommended. Use of Olmesartan medoxomil is not recommended in patients with severe renal impairment (CrCl < 20 mL/min).
Sprue-like enteropathy, an intestinal condition characterized by severe chronic diarrhea with substantial weight loss, has been reported during postmarketing experience in patients receiving Olmesartan medoxomil; may develop months to years after initiation of Olmesartan medoxomil therapy. If symptoms of sprue-like enteropathy develop during Olmesartan medoxomil therapy, if no other causative factor can be identified, discontinuance of the drug and consider other antihypertensive treatment.
Olmesartan inhibits renin-angiotensin system (RAS). Drugs that inhibit the RAS can cause hyperkalaemia. Monitor serum electrolytes periodically.
Use of Olmesartan medoxomil in patient with hepatic impairment is not recommended.
Hyperkalemia may occur, risk factors include renal dysfunction, heart failure. Use cautiously and monitor potassium closely.
The combination of lithium and Olmesartan medoxomil is not recommended.
Use caution in patients with significant aortic/mitral stenosis or obstructive hypertropic cardiomyopathy.
Patients with primary aldosteronism generally will not respond to antihypertensive drugs acting through inhibition of the renin-angiotensin system. Therefore, the use of Olmesartan medoxomil is not recommended in such patients.
As with all other angiotensin II antagonists, the blood pressure lowering effect of Olmesartan medoxomil is somewhat less in black patients than in non-black patients, possibly because of a higher prevalence of low-renin status in the black hypertensive population.
As with any antihypertensive agent, excessive blood pressure decrease in patients with ischemic heart disease or ischemic cerebrovascular disease could result in myocardial infarction or stroke.

Pregnancy: Drugs that act on the renin-angiotensin system can reduce fetal renal function and increase fetal and neonatal morbidity and mortality when used in pregnancy during the second and third trimesters. The use of drugs that act on the renin-angiotensin system are associated with oligohydramnios. Oligohydramnios, due to decreased fetal renal function, may lead to fetal lung hypoplasia and skeletal malformations. Use is also associated with anuria, hypotension, renal failure, skull hypoplasia, and death in the fetus/neonate. ACE inhibitors also may increase the risk of major congenital malformations when administered during the first trimester of pregnancy. Olmesartan medoxomil should be discontinued as soon as possible when pregnancy is detected.
Lactation: Olmesartan medoxomil is distributed into milk in rats. It is not known whether the drug is distributed into milk in humans. Because of the potential for serious adverse reactions to Olmesartan medoxomil in nursing infants, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the mother.

Undesirable effects may be found during treatment with Olmesartan medoxomil include: Central nervous system disorders: dizziness, headache, vertigo.
Gastrointestinal disorders: nausea, vomiting, diarrhea, abdominal pain, dyspepsia, gastroenteritis, sprue-like enteropathy.
Respiratory system disorders: cough, bronchitis, pharyngitis, rhinitis.
Urinary system and renal disorders: haematuria, urinary tract infection, acute renal failure, renal insufficiency.
Musculoskeletal disorders: arthritis, back pain, muscle spasm, myalgia, bone pain.
Skin and subcutaneous tissue disorders: pruritus, rash, exanthematous rashes, allergic conditions such as allergic dermatitis, angioedema, facial edema and urticaria.
General disorders: chest pain, influenza-like symptoms, peripheral edema, pain, asthenic conditions such as asthenia, fatigue, lethargy, malaise.
Investigations: increased creatine phosphokinase, liver enzyme elevations, abnormal renal function tests such as blood creatinine increased and blood urea increased.
Metabolic and nutrition disorders: hypertriglyceridemia, hyperuricemia, hyperkalemia.
Immune system disorders: anaphylactic reaction.
Cardiovascular disorders: hypotension, angina pectoris.
Blood and lymphatic system disorders: thrombocytopenia.

Drug that block the renin-angiotensin system: Increased risk of renal impairment, hyperkalemia, and hypotension with concomitant use of other drugs that block the renin-angiotensin system (e.g., angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor antagonists, aliskiren); when Olmesartan medoxomil is used concomitantly with such drugs, blood pressure, renal function, and serum concentrations of electrolytes should be monitored closely.
Colesevelam hydrochloride: Colesevelam hydrochloride may decrease systemic exposure and peak plasma concentrations of Olmesartan medoxomil. Administration of Olmesartan medoxomil at least 4 hours prior to colesevelam decreases the extent of this interaction and should be considered.
Lithium: Olmesartan medoxomil may increase serum lithium concentrations resulting in lithium toxicity have been reported. If concomitant use is required, serum lithium concentrations should be carefully monitored.
Nonsteroidal Anti-inflammatory Agents (NSAIDs): When Olmesartan medoxomil is used concomitantly with NSAIDs, including selective COX-2 inhibitors may result in renal dysfunction. Renal function should be monitored periodically in patients receiving concomitant therapy with Olmesartan medoxomil and NSAIDs, including selective COX-2 inhibitors.

Store below 30°C.

Angiotensin II Antagonists

C09CA08 - olmesartan medoxomil ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.

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