Percorten V

Generic name: desoxycorticosterone pivalatae
Dosage form: FOR ANIMAL USE ONLY

CAUTION:

Federal (U.S.A.) law restricts this drug to use by or on the order of a licensed veterinarian.

DESCRIPTION:

The active ingredient in PERCORTEN-V is desoxycorticosterone pivalate (DOCP). It is a mineralocorticoid hormone and an analog of desoxycorticosterone. It is white, odorless, and stable in air. It is practically insoluble in water, sparingly soluble in acetone, slightly soluble in methanol, ether and vegetable oils. The molecular weight is 414.58. It is designated chemically as 21 (2,2-dimethyl-1-oxopropoxy)-pregn-4-ene-3,20-dione. The empirical formula is C26H38O4 and the structural formula is:

PERCORTEN-V is a white aqueous suspension. Each ml contains 25mg desoxycorticosterone pivalate, 10.5mg methylcellulose, 3mg sodium carboxymethylcellulose, 1mg polysorbate 80 and 8mg sodium chloride with 0.002% thimerosal as preservative in water for injection.

CLINICAL PHARMACOLOGY:

Desoxycorticosterone pivalate (DOCP), like other adrenocorticoid hormones, is thought to act by controlling the rate of synthesis of proteins. It reacts with receptor proteins in the cytoplasm to form a steroid-receptor complex. This complex moves into the nucleus, where it binds to chromatin that results in genetic transcription of cellular DNA to messenger RNA. The steroid hormones appear to induce transcription and synthesis of specific proteins which produce the physiologic effects seen after administration.

DOCP is a long-acting ester of desoxycorticosterone acetate (DOCA) which is recognized as having the same qualitative effects as the natural mineralocorticoid hormone aldosterone.

The most important effect of DOCP is to increase the rate of renal tubular absorption of sodium. This effect is seen most intensely in the thick portion of the ascending limb of the loop of Henle. It also increases sodium absorption in the proximal convoluted tubule but this effect is less important in sodium retention. Chloride follows the sodium out of the renal tubule.

Another important effect of DOCP is enhanced renal excretion of potassium. This effect is driven by the resorption of sodium that pulls potassium from the extracellular fluid into the renal tubules, thus promoting potassium excretion.

DOCP also acts to increase extracellular fluid volume. The enhanced retention of sodium, chloride and bicarbonate, creates an osmotic gradient that promotes water absorption from the renal tubules. The extracellular fluid volume is supported. This expands the blood volume and improves the venous return to the heart and cardiac output. The expanded blood volume and increased cardiac o...