Clinical Information
Gen. Code and Des.
64360 clonidine HCl/PF EPIDURAL VIAL 1000MCG/10
GCN and Des.
13643 clonidine HCl/PF EPIDURAL VIAL 1000MCG/10
Strength
1000MCG
Dose Form
VIAL (ML)
Product Category
RX Pharmaceuticals
Fine Line Class
850085008510 All Rx Products
DEA Class
NC
OMP Family
AHFS Class
28089200 ANALGESICS AND ANTIPYRETICS, MISC.
24081600 CENTRAL ALPHA-AGONISTS
12120400 ALPHA-ADRENERGIC AGONISTS
Active Ingredients
644 clonidine HCl 4205918
9870 preservative free
CLONIDINE HYDROCHLORIDE- clonidine hydrochloride tablet
DAVA Pharmaceuticals, Inc.
DESCRIPTION
Clonidine hydrochloride USP is a centrally acting alpha-agonist hypotensive agent available as tablets for oral administration in three dosage strengths: 0.1 mg, 0.2 mg and 0.3 mg. The 0.1 mg tablet is equivalent to 0.087 mg of the free base.
The inactive ingredients are dibasic calcium phosphate, magnesium stearate, microcrystalline cellulose and povidone. In addition, the 0.1 mg tablet also contains FD&C Blue No. 2; the 0.2 mg tablets contain Yellow #10; the 0.3 mg tablets contain FD&C Blue No. 2 and Yellow #10.
Clonidine hydrochloride is an imidazoline derivative and exists as a mesomeric compound. The chemical name is 2-(2,6-dichlorophenylamino)-2-imidazoline hydrochloride. The following is the structural formula:
CLONIDINE HYDROCHLORIDE Structural Formula
(click image for full-size original)
C9 H9 C12 N3 � HCl Mol. Wt. 266.56
Clonidine hydrochloride is an odorless, bitter, white, crystalline substance soluble in water and alcohol.
CLINICAL PHARMACOLOGY
Clonidine stimulates alpha-adrenoreceptors in the brain stem. This action results in reduced sympathetic outflow from the central nervous system and in decreases in peripheral resistance, renal vascular resistance, heart rate, and blood pressure. Clonidine HCl Tablets USP act relatively rapidly. The patient's blood pressure declines within 30 to 60 minutes after an oral dose, the maximum decrease occurring within 2 to 4 hours. Renal blood flow and glomerular filtration rate remain essentially unchanged. Normal postural reflexes are intact; therefore, orthostatic symptoms are mild and infrequent.
Acute studies with clonidine hydrochloride in humans have demonstrated a moderate reduction (15% to 20%) of cardiac output in the supine position with no change in the peripheral resistance: at a 45� tilt there is a smaller reduction in cardiac output and a decrease of peripheral resistance. During long-term therapy, cardiac output tends to return to control values, while peripheral resistance remains decreased. Slowing of the pulse rate has been observed in most patients given clonidine, but the drug does not alter normal hemodynamic response to exercise.
Tolerance to the antihypertensive effect may develop in some patients, necessitating a reevaluation of therapy.
Other studies in patients have provided evidence of a reduction in plasma renin activity and in the excretion of aldosterone and catecholamines. The exact relationship of these pharmacologic actions to the antihypertensive effect of clonidine has not been fully elucidated.
Clonidine acutely stimulates growth hormone release in both children and adults, but does not produce a chronic elevation of growth hormone with long-term use.
Pharmacokinetics: The plasma level of clonidine peaks in approximately 3 to 5 hours and the plasma half-life ranges from 12 to 16 hours. The half-life increases up to 41 hours in patients with severe impairment of renal function. Following oral administration about 40-60% of the absorbed dose is recovered in the urine as unchanged drug in 24 hours. About 50% of the absorbed dose is metabolized in the liver.
INDICATIONS AND USAGE
Clonidine HCl Tablets USP are indicated in the treatment of hypertension. Clonidine HCl Tablets may be employed alone or concomitantly with other antihypertensive agents