Lisinopril 2.5mg, 5mg, 10mg

Category:- Cardiology | Type:- Tablet

COMPOSITION
Each tablet contains:
Lisinopril USP 10 mg
Hydrochlorothiazide USP 12.5 mg
 

PHARMACOLOGICAL CLASSIFICATION:
A 7.1.3 Other hypotensives.
 

PHARMACOLOGICAL ACTION:
Lisinopril/HCT is a combination of an angiotensin converting enzyme inhibitor, lisinopril and a diuretic, hydrochlorothiazide. Both these components have been widely used alone and in combination for
the treatment of hypertension due to additive effects. Lisinopril is a peptidyl dipeptidase inhibitor and inhibits the angiotensin converting enzyme (ACE) that catalyses the conversion of angiotensin I to
angiotensin II. Angiotensin II is a vasoconstrictor peptide which also stimulates aldosterone secretion by the adrenal cortex.
Inhibition of ACE results in decreased concentrations of angiotensin II which results in decreased vasopressor activity and reduced aldosterone secretion. Reduced aldosterone secretion may result in an
increase in serum potassium concentration.
The mechanism of action through which lisinopril lowers blood pressure is mainly via suppression of the renin-angiotensin-aldosterone system; however lisinopril also has antihypertensive effects in
patients with low-renin hypertension.
ACE is identical to kininase II, an enzyme that degrades bradykinin. It could be possible that increased levels of bradykinin, a potent vasodilatory peptide, play a role in the therapeutic effects of lisinopril.
However, this remains to be elucidated.
Hydrochlorothiazide is a thiazide diuretic and an antihypertensive agent. It affects the distal renal tubular mechanism of electrolyte re-absorption and increases excretion of sodium and chloride in
approximately equivalent amounts. Natriuresis may be accompanied by some loss of potassium and bicarbonate. The mechanism of the antihypertensive effects of the thiazides is unknown. Thiazides do
not usually affect normal blood pressure.
 

Pharmacokinetics
The concomitant administration of lisinopril and hydrochlorothiazide has no clinical significant effect on the pharmacokinetics of either drug.
Lisinopril
Approximately 60% of lisinopril is absorbed after oral administration. The absorption varies between individuals (6 to 60%).
Following oral administration of lisinopril, peak serum concentrations occur within about 7 hours. Lisinopril has an effective half-life of 12 hours. Lisinopril does not bind to other serum proteins.
The absorption of lisinopril is not affected by the presence of food in the gastrointestinal tract.
Lisinopril does not undergo metabolism and absorbed drug is excreted unchanged entirely in the urine. Impaired renal function decreases elimination of lisinopril. This decrease only becomes clinically
important when the glomerular filtration rate is below 30 mL/min. Lisinopril can be removed by dialysis.
Older patients have higher blood levels and higher values for the area under the plasma concentration time curve than younger patients.
Hydrochlorothiazide
The plasma half-life of hydrochlorothiazide can vary between 5 and 15 hours. Approximately 60% of the dose is eliminated unchanged within 24 hours.
After oral administration of hydrochlorothiazide, diuresis begins within 2 hours, peaks in about 4 hours and lasts 6 to 12 hours.
 

INDICATIONS:
Mild to moderate hypertension in patients who have been stabilized on their individual components given in the same proportions.