Details
Stereochemistry | ACHIRAL |
Molecular Formula | C9H9Cl2N3 |
Molecular Weight | 230.0941 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
c1cc(c(c(c1)Cl)NC2=NCCN2)Cl
InChI
InChIKey=GJSURZIOUXUGAL-UHFFFAOYSA-N
InChI=1S/C9H9Cl2N3/c10-6-2-1-3-7(11)8(6)14-9-12-4-5-13-9/h1-3H,4-5H2,(H2,12,13,14)
Molecular Formula | C9H9Cl2N3 |
Molecular Weight | 230.0941 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment:: description was created based on several sources, including
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/017407s037lbl.pdf | https://clinicaltrials.gov/ct2/show/NCT02177461 | https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022331lbl.pdf | https://clinicaltrials.gov/ct2/show/NCT00556959
Curator's Comment:: description was created based on several sources, including
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/017407s037lbl.pdf | https://clinicaltrials.gov/ct2/show/NCT02177461 | https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022331lbl.pdf | https://clinicaltrials.gov/ct2/show/NCT00556959
Clonidine is a centrally acting α2 adrenergic agonist and imidazoline receptor agonist used to treat high blood pressure, attention deficit hyperactivity disorder, anxiety disorders, tic disorders, withdrawal (from either alcohol, opioids, or smoking), migraine, menopausal flushing, diarrhea, and certain pain conditions. Clonidine treats high blood pressure by stimulating α2 receptors in the brain, which decreases peripheral vascular resistance, lowering blood pressure. It has specificity towards the presynaptic α2 receptors in the vasomotor center in the brainstem. This binding decreases presynaptic calcium levels, thus inhibiting the release of norepinephrine (NE). It has also been proposed that the antihypertensive effect of clonidine is due to agonism on the I1 receptor (imidazoline receptor), which mediates the sympatho-inhibitory actions of imidazolines to lower blood pressure. Clonidines mechanism of action in the treatment of ADHD is to increase noradrenergic tone in the prefrontal cortex (PFC) directly by binding to postsynaptic α2A adrenergic receptors and indirectly by increasing norepinephrine input from the locus coeruleus. Clonidine indicated in the treatment of hypertension. Clonidine hydrochloride tablets may be employed alone or concomitantly with other antihypertensive agents. The US Food and Drug Administration (FDA) has approved clonidine for the treatment of attention deficit hyperactivity disorder (ADHD), under the trade name of Kapvay alone or with stimulants in 2010, for pediatric patients aged 6–17 years.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1867 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27265687 |
30.2 nM [EC50] | ||
Target ID: CHEMBL2095158 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25521963 |
3.8 nM [Ki] | ||
Target ID: CHEMBL1942 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22750139 |
31.6 nM [Ki] | ||
Target ID: CHEMBL1916 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22750139 |
9.3 nM [Ki] | ||
Target ID: CHEMBL2094251 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8784451 |
290.0 nM [EC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | CATAPRES-TTS-1 Approved UseINDICATIONS & USAGE Clonidine hydrochloride tablets, USP are indicated in the treatment of hypertension. Clonidine hydrochloride tablets, USP may be employed alone or concomitantly with other antihypertensive agents. Launch Date4.66214388E11 |
|||
Primary | KAPVAY Approved UseINDICATIONS AND USAGE. KAPVAY® is a centrally acting alpha2-adrenergic agonist indicated for the treatment of attention deficit hyperactivity disorder (ADHD) as monotherapy or as adjunctive therapy to stimulant medications Launch Date1.25418235E12 |
|||
Primary | CATAPRES-TTS-1 Approved UseINDICATIONS & USAGE Clonidine hydrochloride tablets, USP are indicated in the treatment of hypertension. Clonidine hydrochloride tablets, USP may be employed alone or concomitantly with other antihypertensive agents. Launch Date4.66214388E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
443 pg/mL |
0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered: |
CLONIDINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
7313 pg × h/mL |
0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered: |
CLONIDINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
12.57 h |
0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered: |
CLONIDINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
0.25 mg 2 times / day multiple, oral Studied dose Dose: 0.25 mg, 2 times / day Route: oral Route: multiple Dose: 0.25 mg, 2 times / day Co-administed with:: Methylphenidate(54 mg/day) Sources: Page: nda/2010/022331Orig1s001.pdf - p.139 |
unhealthy, 13 years n = 1 Health Status: unhealthy Condition: attention deficit hyperactivity disorder Age Group: 13 years Sex: M Population Size: 1 Sources: Page: nda/2010/022331Orig1s001.pdf - p.139 |
Other AEs: Suicide attempt... Other AEs: Suicide attempt Sources: Page: nda/2010/022331Orig1s001.pdf - p.139 |
2 mg 3 times / day multiple, oral Highest studied dose Dose: 2 mg, 3 times / day Route: oral Route: multiple Dose: 2 mg, 3 times / day Sources: |
unhealthy, adult n = 1 Health Status: unhealthy Condition: hypertension Age Group: adult Population Size: 1 Sources: |
|
0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Co-administed with:: Amphetamine Sources: Page: nda/2010/022331Orig1s001.pdf - p.108Methylphenidate(54 mg/day) |
unhealthy, median age 10 years n = 102 Health Status: unhealthy Condition: attention deficit hyperactivity disorder Age Group: median age 10 years Sex: M+F Population Size: 102 Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
Disc. AE: Bradyphrenia... AEs leading to discontinuation/dose reduction: Bradyphrenia (1%) Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
0.1 mg 2 times / day multiple, oral Recommended Dose: 0.1 mg, 2 times / day Route: oral Route: multiple Dose: 0.1 mg, 2 times / day Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
unhealthy, median age 9 years n = 76 Health Status: unhealthy Condition: attention deficit hyperactivity disorder Age Group: median age 9 years Sex: M+F Population Size: 76 Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
Disc. AE: Somnolence, Fatigue... AEs leading to discontinuation/dose reduction: Somnolence (3.9%) Sources: Page: nda/2010/022331Orig1s001.pdf - p.108Fatigue (2.6%) |
0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
unhealthy, median age 9 years n = 78 Health Status: unhealthy Condition: attention deficit hyperactivity disorder Age Group: median age 9 years Sex: M+F Population Size: 78 Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
Disc. AE: Somnolence, Fatigue... AEs leading to discontinuation/dose reduction: Somnolence (6.4%) Sources: Page: nda/2010/022331Orig1s001.pdf - p.108Fatigue (5.1%) Constipation (1.3%) Vomiting (1.3%) Electrocardiogram QT prolonged (1.3%) Rash (1.3%) |
0.1 mg 2 times / day steady, oral Dose: 0.1 mg, 2 times / day Route: oral Route: steady Dose: 0.1 mg, 2 times / day Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Fecal Incontinence Population Size: 22 Sources: |
Other AEs: Dry mouth, Drowsiness... Other AEs: Dry mouth (below serious, 16 patients) Sources: Drowsiness (below serious, 5 patients) Lightheadedness (below serious, 6 patients) Fatigue (below serious, 8 patients) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Suicide attempt | 0.25 mg 2 times / day multiple, oral Studied dose Dose: 0.25 mg, 2 times / day Route: oral Route: multiple Dose: 0.25 mg, 2 times / day Co-administed with:: Methylphenidate(54 mg/day) Sources: Page: nda/2010/022331Orig1s001.pdf - p.139 |
unhealthy, 13 years n = 1 Health Status: unhealthy Condition: attention deficit hyperactivity disorder Age Group: 13 years Sex: M Population Size: 1 Sources: Page: nda/2010/022331Orig1s001.pdf - p.139 |
|
Bradyphrenia | 1% Disc. AE |
0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Co-administed with:: Amphetamine Sources: Page: nda/2010/022331Orig1s001.pdf - p.108Methylphenidate(54 mg/day) |
unhealthy, median age 10 years n = 102 Health Status: unhealthy Condition: attention deficit hyperactivity disorder Age Group: median age 10 years Sex: M+F Population Size: 102 Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
Fatigue | 2.6% Disc. AE |
0.1 mg 2 times / day multiple, oral Recommended Dose: 0.1 mg, 2 times / day Route: oral Route: multiple Dose: 0.1 mg, 2 times / day Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
unhealthy, median age 9 years n = 76 Health Status: unhealthy Condition: attention deficit hyperactivity disorder Age Group: median age 9 years Sex: M+F Population Size: 76 Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
Somnolence | 3.9% Disc. AE |
0.1 mg 2 times / day multiple, oral Recommended Dose: 0.1 mg, 2 times / day Route: oral Route: multiple Dose: 0.1 mg, 2 times / day Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
unhealthy, median age 9 years n = 76 Health Status: unhealthy Condition: attention deficit hyperactivity disorder Age Group: median age 9 years Sex: M+F Population Size: 76 Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
Constipation | 1.3% Disc. AE |
0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
unhealthy, median age 9 years n = 78 Health Status: unhealthy Condition: attention deficit hyperactivity disorder Age Group: median age 9 years Sex: M+F Population Size: 78 Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
Electrocardiogram QT prolonged | 1.3% Disc. AE |
0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
unhealthy, median age 9 years n = 78 Health Status: unhealthy Condition: attention deficit hyperactivity disorder Age Group: median age 9 years Sex: M+F Population Size: 78 Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
Rash | 1.3% Disc. AE |
0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
unhealthy, median age 9 years n = 78 Health Status: unhealthy Condition: attention deficit hyperactivity disorder Age Group: median age 9 years Sex: M+F Population Size: 78 Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
Vomiting | 1.3% Disc. AE |
0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
unhealthy, median age 9 years n = 78 Health Status: unhealthy Condition: attention deficit hyperactivity disorder Age Group: median age 9 years Sex: M+F Population Size: 78 Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
Fatigue | 5.1% Disc. AE |
0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
unhealthy, median age 9 years n = 78 Health Status: unhealthy Condition: attention deficit hyperactivity disorder Age Group: median age 9 years Sex: M+F Population Size: 78 Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
Somnolence | 6.4% Disc. AE |
0.2 mg 2 times / day multiple, oral Recommended Dose: 0.2 mg, 2 times / day Route: oral Route: multiple Dose: 0.2 mg, 2 times / day Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
unhealthy, median age 9 years n = 78 Health Status: unhealthy Condition: attention deficit hyperactivity disorder Age Group: median age 9 years Sex: M+F Population Size: 78 Sources: Page: nda/2010/022331Orig1s001.pdf - p.108 |
Dry mouth | below serious, 16 patients | 0.1 mg 2 times / day steady, oral Dose: 0.1 mg, 2 times / day Route: oral Route: steady Dose: 0.1 mg, 2 times / day Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Fecal Incontinence Population Size: 22 Sources: |
Drowsiness | below serious, 5 patients | 0.1 mg 2 times / day steady, oral Dose: 0.1 mg, 2 times / day Route: oral Route: steady Dose: 0.1 mg, 2 times / day Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Fecal Incontinence Population Size: 22 Sources: |
Lightheadedness | below serious, 6 patients | 0.1 mg 2 times / day steady, oral Dose: 0.1 mg, 2 times / day Route: oral Route: steady Dose: 0.1 mg, 2 times / day Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Fecal Incontinence Population Size: 22 Sources: |
Fatigue | below serious, 8 patients | 0.1 mg 2 times / day steady, oral Dose: 0.1 mg, 2 times / day Route: oral Route: steady Dose: 0.1 mg, 2 times / day Sources: |
unhealthy n = 22 Health Status: unhealthy Condition: Fecal Incontinence Population Size: 22 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 265.0 |
likely | |||
Page: abstract |
no | |||
yes [IC50 1.21 uM] | ||||
Page: 3.0 |
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 1.0 |
no | |||
Page: 1.0 |
no | |||
Page: 1.0 |
no | |||
Page: 1.0 |
no | |||
Page: 1.0 |
no | |||
Page: 1.0 |
no | |||
Page: 1.0 |
no | |||
Page: 1.0 |
no | |||
Page: 1.0 |
no | |||
Page: abstract |
yes | |||
Page: abstract |
yes | |||
Page: abstract |
yes | |||
Page: abstract |
yes | |||
Page: abstract |
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 102.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Letter: Dementia associated with clonidine therapy. | 1975 Mar 15 |
|
Drug treatment options for irritable bowel syndrome: managing for success. | 2001 |
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Alpha2 adrenergic agonists for the management of opioid withdrawal. | 2001 |
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[Potentiation of local anesthesia in endonasal surgery]. | 2001 |
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P75-expressing elements are necessary for anti-allodynic effects of spinal clonidine and neostigmine. | 2001 |
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Evidence for functional presynaptic alpha-2 adrenoceptors and their down-regulation in human heart failure. | 2001 Apr |
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Oops--wrong dose of epidural clonidine in children! | 2001 Apr |
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Alpha2A-adrenoceptor mediated tachypnea in awake goats. | 2001 Apr |
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Brain alpha(2)-adrenoceptors in monoamine-depleted rats: increased receptor density, G coupling proteins, receptor turnover and receptor mRNA. | 2001 Apr |
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Sodium-induced rise in blood pressure is suppressed by androgen receptor blockade. | 2001 Apr |
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Blockade by agmatine of catecholamine release from chromaffin cells is unrelated to imidazoline receptors. | 2001 Apr 6 |
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Continuous intrathecal morphine treatment for chronic pain of nonmalignant etiology: long-term benefits and efficacy. | 2001 Feb |
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The impact of glycaemic control on autoregulation of glomerular filtration rate in patients with non-insulin dependent diabetes. | 2001 Feb |
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Some behavioural effects of antidepressant drugs are time-dependent. | 2001 Feb |
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Baclofen versus clonidine in the treatment of opiates withdrawal, side-effects aspect: a double-blind randomized controlled trial. | 2001 Feb |
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Interactions of ligands at angiotensin II-receptors and imidazoline receptors. | 2001 Feb |
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Comparison of the effects of clonidine and hydroxyzine on haemodynamic and catecholamine reactions to microlaryngoscopy. | 2001 Feb |
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The use of baclofen in cluster headache. | 2001 Feb |
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Differential effects of clonidine, dopamine, dobutamine, and dopexamine on basal and acid-stimulated mucosal blood flow in the rat stomach. | 2001 Feb |
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Nitric oxide and central antihypertensive drugs: one more difference between catecholamines and imidazolines. | 2001 Feb |
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Mortality after coronary artery occlusion in different models of cardiac hypertrophy in rats. | 2001 Feb |
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Inhibition of the I(h) current in isolated peripheral nerve: a novel mode of peripheral antinociception? | 2001 Feb |
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Partial agonist clonidine mediates alpha(2)-AR subtypes specific regulation of cAMP accumulation in adenylyl cyclase II transfected DDT1-MF2 cells. | 2001 Feb |
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Effectiveness of apraclonidine 1% in preventing intraocular pressure rise following macular hole surgery. | 2001 Feb |
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Noradrenergic dysfunction in the prefrontal cortex in depression: an [15O] H2O PET study of the neuromodulatory effects of clonidine. | 2001 Feb 15 |
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[Cardiovascular stress protection following anesthesia induction. Comparison of clonidine and esmolol]. | 2001 Jan |
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Do infant rats cry? | 2001 Jan |
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Antagonistic effects of selective alpha1-adrenoceptor antagonists MDL73005EF and tamsulosin and partial agonists clonidine and tizanidine in rat thoracic aorta and rabbit iliac artery. | 2001 Jan |
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Treatment of chronic hypertension with intravenous enalaprilat and transdermal clonidine. | 2001 Jan |
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Chronic treatment with desipramine facilitates its effect on extracellular noradrenaline in the rat hippocampus: studies on the role of presynaptic alpha2-adrenoceptors. | 2001 Jan |
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Apical uptake of organic cations by human intestinal Caco-2 cells: putative involvement of ASF transporters. | 2001 Jan |
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Effect of chronic morphine treatment on alpha(2)-adrenoceptor mediated autoinhibition of transmitter release from sympathetic varicosities of the mouse vas deferens. | 2001 Jan |
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Chronic treatment with reboxetine by osmotic pumps facilitates its effect on extracellular noradrenaline and may desensitize alpha(2)-adrenoceptors in the prefrontal cortex. | 2001 Jan |
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[Low sensitivity of IGF-I, IGFBP-3 and urinary GH in the diagnosis of growth hormone insufficiency in slowly-growing short-statured boys. Grupo Español de Estudio de la Talla Baja]. | 2001 Jan 13 |
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Effects of antisense to the (alpha)2A-adrenoceptors administered into the region of the locus ceruleus on behaviors in plus-maze and sexual behavior tests in sham-operated and castrated male rats. | 2001 Jan 15 |
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Galanin/alpha2-adrenoceptor interactions in telencephalic and diencephalic regions of the rat. | 2001 Jan 22 |
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Frequency dependent alpha(2)-adrenoceptor mediated modulation of excitatory junction potentials in guinea-pig mesenteric artery. | 2001 Jan 5 |
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Clonidine in preterm-infant caudal anesthesia may be responsible for postoperative apnea. | 2001 Jan-Feb |
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Premedication modifies the quality of sedation with propofol during regional anesthesia. | 2001 Mar |
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Clonidine-induced antinociception and locomotor hypoactivity are reduced by dexamethasone in mice. | 2001 Mar |
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Noradrenergic modulation of calcium currents and synaptic transmission in the olfactory bulb of Xenopus laevis tadpoles. | 2001 Mar |
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Ultrasonic vocalizations of preweanling rats: involvement of both alpha(2)-adrenoceptor and kappa-opioid receptor systems. | 2001 Mar |
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Effects of N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine (DSP4) on alpha2-adrenoceptors which regulate the synthesis and release of noradrenaline in the rat brain. | 2001 Mar |
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The antinociceptive effect of intrathecal administration of epibatidine with clonidine or neostigmine in the formalin test in rats. | 2001 Mar |
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The analgesic interaction between intrathecal clonidine and glutamate receptor antagonists on thermal and formalin-induced pain in rats. | 2001 Mar |
|
Neural circuits regulating pulsatile luteinizing hormone release in the female guinea-pig: opioid, adrenergic and serotonergic interactions. | 2001 Mar |
|
Prevention of ischemic ventricular tachycardia of Purkinje origin: role for alpha(2)-adrenoceptors in Purkinje? | 2001 Mar |
|
Gelatin microspheres crosslinked with D,L-glyceraldehyde as a potential drug delivery system: preparation, characterisation, in vitro and in vivo studies. | 2001 Mar 14 |
|
Alpha-adrenergic agonists inhibit the dipsogenic effect of angiotensin II by their stimulation of atrial natriuretic peptide release. | 2001 Mar 23 |
|
Linkage study of the alpha2A adrenergic receptor in attention-deficit hyperactivity disorder families. | 2001 Mar 8 |
Sample Use Guides
In Vivo Use Guide
Curator's Comment:: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/018891s028lbl.pdf
Oral
Initial Dose 0.1 mg tablet twice daily (morning and bedtime). Elderly patients may benefit from a lower initial dose
Maintenance Dose Further increments of 0.1 mg per day may be made at weekly intervals if necessary until the desired response is achieved. Taking the larger portion of the oral daily dose at bedtime may minimize transient adjustment effects of dry mouth and drowsiness. The therapeutic doses most commonly employed have ranged from 0.2 mg to 0.6 mg per day given in divided doses. Studies have indicated that 2.4 mg is the maximum effective daily dose, but doses as high as this have rarely been employed.
Transdermal: once every 7 days to a hairless area of intact skin on the upper outer arm or chest.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17691718
Neural membranes (P2 fractions) were prepared from the prefrontal cortex of human brains obtained at autopsy. Specific Clonidine binding was measured in 0.55 mL aliquots (50 mM Tris HCl, pH 7.5) of the neural membranes, which were incubated with [3H]RX821002 (1 nM) for 30 min at 25 °C in the absence or presence of the Clonidine (10^-12 M to 10^-3 M, 10 concentrations). Specific binding was determined and plotted as a function of the compound concentration. Incubations were terminated by diluting the samples with 5 mL of ice-cold Tris incubation buffer (4 °C). Membrane-bound [3H]RX821002 was separated by vacuum filtration through Whatman GF/C glass fiber filters. Then the filters were rinsed twice with 5 mL of incubation buffer and transferred to minivials containing 3 mL of OptiPhase “HiSafe” II cocktail and counted for radioactivity by liquid scintillation spectrometry.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Jun 25 20:54:07 UTC 2021
by
admin
on
Fri Jun 25 20:54:07 UTC 2021
|
Record UNII |
MN3L5RMN02
|
Record Status |
Validated (UNII)
|
Record Version |
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-
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Classification Tree | Code System | Code | ||
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WHO-ATC |
C02LC51
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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WHO-ATC |
S01EA04
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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NDF-RT |
N0000009918
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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WHO-VATC |
QC02LC01
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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WHO-ATC |
N02CX02
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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WHO-VATC |
QC02LC51
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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WHO-VATC |
QN02CX02
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
|
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NCI_THESAURUS |
C29709
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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FDA ORPHAN DRUG |
425614
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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NDF-RT |
N0000175554
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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FDA ORPHAN DRUG |
34388
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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WHO-VATC |
QC02AC01
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
|
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WHO-VATC |
QS01EA04
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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LIVERTOX |
225
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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|
WHO-ATC |
C02AC01
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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WHO-ATC |
C02LC01
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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Code System | Code | Type | Description | ||
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C380
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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4205-90-7
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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DB00575
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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2599
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | RxNorm | ||
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MN3L5RMN02
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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4205-90-7
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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224-119-4
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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D003000
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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516
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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2803
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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Clonidine
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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1140393
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | USP-RS | ||
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2624
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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CLONIDINE
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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CHEMBL134
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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704
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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M3650
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | Merck Index | ||
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3040
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY | |||
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SUB06730MIG
Created by
admin on Fri Jun 25 20:54:07 UTC 2021 , Edited by admin on Fri Jun 25 20:54:07 UTC 2021
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PRIMARY |
Related Record | Type | Details | ||
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TRANSPORTER -> INHIBITOR | |||
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TARGET -> AGONIST | |||
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TARGET -> AGONIST |
SHORT-ACTING
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TRANSPORTER -> INHIBITOR | |||
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TARGET -> AGONIST | |||
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TRANSPORTER -> INHIBITOR | |||
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SALT/SOLVATE -> PARENT |
Related Record | Type | Details | ||
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT |
Related Record | Type | Details | ||
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ACTIVE MOIETY |