Diovan hct

Diovan hct

Diovan HCT -
Valsartan - Hydrochlorothiazide
Diovan HCT---Diovan HCT Side Effects - Diovan HCT-information
Pharmacology:-Diovan HCT combines action valsartan, an orally active angiotensin II AT 1 receptor blocker, and that the diuretic, hydrochlorothiazide.
Diovan hct
Valsartan: Valsartan acts electoral AT 1, receptor subtype that the mediator known cardiovascular actions of angiotensin II, the primary vasoactive hormone in the renin-angiotensin system. In 2-subtype receptors, which are in tissues such as the brain, endometrium, myometrium and fetal kidneys and adrenals, plays no known role in cardiovascular homeostasis today. Valsartan does not exhibit any partial AT 1 receptor agonist activity, and, in fact, there was no activity in AT 2 receptors. Valsartan does not bind or block other hormone receptors or ion channels known that it is important in cardiovascular regulation. The main metabolite 4 valeryl - hydroxy valsartan, mostly inactive.

Angiotensin II is a wide range of physiological effects, and many of them are directly or indirectly involved in the regulation of blood pressure. A potent vasoconstrictor, has a direct angiotensin II pressor response. In addition, it contributes to the conservation of sodium and aldosterone secretion.

The blockade of angiotensin II AT 1 receptors results in a 2 - 3 times in plasma renin and angiotensin II plasma concentration in hypertensive patients. The lingering effects of the expansion of 2-receptor stimulation in angiotensin II unknown.

Valsartan not preclude the angiotensin-converting enzyme (ACE), which is also known as kininase II, the enzyme makes angiotensin I to angiotensin II and degrades bradykinin.

Hydrochlorothiazide: Hydrochlorothiazide is a thiazide diuretic. Thiazides affect the renal tubular mechanism of electrolyte absorption, directly increasing the excretion of sodium and chloride in roughly equivalent amounts. Indirectly, the diuretic hydrochlorothiazide effect reduces the plasma volume, followed by an increase in plasma renin activity and aldosterone secretion increases, increases in urinary calcium loss, and a decline in serum potassium. In the renin-angiotensin aldosterone link brokered II, so coadministration of AT 1 angiotensin II receptor blocker trend is potassium losses associated with thiazide Diuretics.

Hydrochlorothiazide useful in the treatment of hypertension. It can be used independently or as a complement to other antihypertensive drugs. Hydrochlorothiazide does not affect normal blood pressure.
Diovan hct
Pharmacokinetics: Diovan hct Valsartan: It is a linear pharmacokinetics of 80 to 320 mg dose range, valsartan not accumulate in plasma markedly after repeated administration. Plasma concentrations similar to the men and women.

The average absolute bioavailability valsartan is about 23%, but with a high variability. Peak plasma concentration is achieved between 2 and 4 hours after dosing.

Valsartan is 94 to 97% bound to serum protein, serum albumin basically. The sustainability of the distribution volume of about 17 liters, which indicates that valsartan not spread widely in tissues.

After i.v. Administration shows valsartan biexponential kinetics of dissolution (1/2a t <1 hour, and more 1/2b ages 5 to 9 hours). Plasma cleaning relatively slow (about 2 l / h) compared with hepatic blood flow (about 30 L / h).

Following oral administration of 14C solution called valsartan, 83% is absorbed valsartan excretion in feces and 13% in urine, largely unchanged complex. Valsartan biotransformation apparently not related to cytochrome P450 system. Ferment (s) responsible for the metabolism of valsartan were not identified.

On average, patients with mild to moderate chronic liver disease twice impact valsartan healthy volunteers, as measured by AUC and C max (see Precautions, in patients with violation of the functions of the liver and dosage).

Renal clearance is only 30% of total plasma clearance. There was no apparent correlation between renal function and effects of valsartan, as measured by AUC and C max, in patients with varying degrees of renal impairment. In patients with renal insufficiency hemodialysis time, the limited information suggests that the impact of valsartan comparable to that in patients with creatinine clearance> 10 ml / min.

Valsartan is not removed from the plasma dialysis.
Diovan hct
The impact of valsartan is about 50% higher than that measured by AUC and C max and the half-life of more questions than elderly in young subjects. However, this difference was not found that any clinical significance.

Hydrochlorothiazide: absorption following oral dose hydrochlorothiazide quick to about 2 hours max. The distribution and elimination kinetics, as has been described in biexponential decay function in the terminal half life of 6 to 15 hours.

The absolute bioavailability of hydrochlorothiazide is 60 to 80% after oral administration, with> 95% of the absorbed dose unchanged excretion in the urine.

Hydrochlorothiazide crosses the placental but not the blood-brain barrier and excretion in breast milk.

Valsartan-Hydrochlorothiazide: System Availability hydrochlorothiazide reduced by about 30% when coadministered with valsartan. In kinetics valsartan not markedly affected by the coadministration of hydrochlorothiazide. This interaction has no effect on the combined use of valsartan and hydrochlorothiazide.

Pharmacodynamics: Valsartan: Valsartan prevents the pressor effect of angiotensin II infusion. An oral dose of 80 mg inhibits pressor effect by about 80% at peak about 30% inhibition occurred in 24 hours.

After one oral dose, the antihypertensive activity valsartan has begun for about 2 hours and peaks during the 4 to 6 hours in most patients.

In the antihypertensive effect of valsartan remains within 24 hours after dosing. Drain / peak ratio varies from 0.54 to 0.76. Valsartan reduces blood pressure in hypertensive patients without affecting heart rate.

In the course of repeated dosing, the maximum reduction in blood pressure in a dose is usually achieved within 4 weeks and maintained during long-term therapy. Combinations with hydrochlorothiazide produce additional reduction in blood pressure.

There was no apparent effect of a sharp rebound after the withdrawal of valsartan therapy.

Although the available data to date indicate a similar pharmacodynamic effect of valsartan in black and white hypertensive patients, it should be viewed with caution because antihypertensive drugs affecting the renin-angiotensin system, such as ACE inhibitors and angiotensin II receptor blockers AT 1, as a whole it was found that less effective in low-renin AG (often black).

Hydrochlorothiazide: Top of the diuretic action following oral administration occurs in 2 hours and peak action in about 4 hours. Diuretic activity lasts for about 6 to 12 hours.

Valsartan-Hydrochlorothiazide: Components of Diovan HCT-found that the additive effect on lowering blood pressure, lowering blood pressure, more so than any component used alone.
Diovan hct
In the antihypertensive effect of Diovan HCT-supported 24 - hour period. In clinical studies of at least 1 year duration, the antihypertensive effect is maintained at a constant therapy. Despite a significant reduction of blood pressure, administration of Diovan HCT-has no clinically significant effect on heart rate.