|Composition||Cilnidipine ,10 ,Olmesartan 20mg and Chlorthalidone 12.5mg Tablets.|
|Mechanism of Action||
Cilnidipine is a dihydropyridine calcium-channel blocker. It inhibits cellular influx of calcium, thus causing vasodilatation. It has greater selectivity for vascular smooth muscle. It has little or no action at the SA or AV nodes and -ve inotropic activity is rarely seen at therapeutic doses.
Chlortalidone is an oral, long acting antihypertensive/diuretic. It is a monosulfamyl diuretic that acts by enhancing the excretion of sodium and chloride ions, and water by interfering with the transport of sodium ions across the renal tubular epithelium.
Their primary site of action appears to be at the cortical diluting segment in the nephron of the loop of Henle.Olmesartan :Volume- or salt-depleted patients including patients on prolonged diuretic therapy. Patients w/ renal artery stenosis, aortic or mitral stenosis, obstructive biliary disease. Renal and mild to moderate hepatic impairment. Lactation. Monitoring Parameters Monitor BP, electrolytes and serum creatinine levels.
Rapid absorption. Cmax within 2 h. Highest level in the liver and also distribution in the kidneys, plasma, and other tissues. No tissue showed a particularly high accumulation of the drug following repeated oral administrations. Protein binding 98% The percentage urinary excretion of Cilnidipine following an oral dose is about 36%
Chlortalidone :Onset: 2 hr.
Duration: 48-72 hr
Absorption: Erratic absorption from the GI tract (oral).
Distribution: Binds to red blood cells; crosses the placenta and enters breast milk. Protein-binding: Weak.
Excretion: Urine (as unchanged drug); 40-60 hr (elimination half-life).
Olmesartan is a selective and competitive angiotensin II Type 1 (AT1) receptor antagonist that blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II. As a result, olmesartan relaxes blood vessels, hence lowering BP and increases blood supply and oxygen to the heart.
Absorption: Bioavailability: Approx 26%. Time to peak plasma concentration: Approx 1-2 hr. Distribution: Volume of distribution: 17 L. Plasma protein binding: ≤99%.
Metabolism: Olmesartan medoxomil undergoes ester hydrolysis in the GI tract to active form olmesartan.
Excretion: Via faeces (50-65%) and urine (35-50%) both as olmesartan. Terminal half-life: Approx 10-15 hr.
Dizziness; flushing; headache; hypotension; peripheral oedema; tachycardia; palpitations; GI disturbances; increased micturition frequency; lethargy; eye pain; depression; ischaemic chest pain; cerebral or myocardial ischaemia; transient blindness; rashes; fever; abnormal liver function; gingival hyperplasia; myalgia; tremor; impotence.
Hypotension, poor cardiac reserve, heart failure. Sudden withdrawal may exacerbate angina. Discontinue in patients who experience ischemic pain following administration. Pregnancy, lactation.
Chlortalidone:Adult: PO HTN 25 mg/day, up to 50 mg/day. Oedema Initial: 25-50 mg/day up to 100-200 mg/day in severe cases. Maintenance: 25-50 mg/day or on alternate days. Diabetes insipidus Initial: 100 mg twice daily. Maintenance: 50 mg/day.
Adult: 5-10 mg once daily, increase to 20 mg once daily if necessary.
Adult: Initial: 10-20 mg once daily may then be increased up to max 40 mg once daily if needed.
Child: 6-16 yr 35 kg: 10 mg once daily; ≥35 kg: 20 mg once daily. Doses may be doubled once if necessary after 2 wk.Elderly: No dosage adjustment needed.Renal impairment: Mild to moderate (CrCl: 20-60 mL/min): Max: 20 mg once daily.
Hepatic impairment: Moderate: Initial: 10 mg once daily may increase up to max 20 mg once daily.