Identification

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Name
Clonidine
Accession Number
DB00575  (APRD00174, DB07566)
Type
Small Molecule
Groups
Approved
Description

Clonidine is an imidazole derivate that acts as an agonist of alpha-2 adrenoceptors.2 This activity is useful for the treatment of hypertension, severe pain, and ADHD.8,9,10,11

Clonidine was granted FDA approval on 3 September 1974.8

Structure
Thumb
Synonyms
  • 2-((2,6-Dichlorophenyl)imino)imidazolidine
  • 2,6-Dichloro-N-2-imidazolidinylidenebenzenamine
  • Chlofazoline
  • Clonidin
  • Clonidina
  • Clonidine
  • Clonidinum
External IDs
M-5041T / SKF 34427 / ST 155 / ST 155-BS
Product Ingredients
IngredientUNIICASInChI Key
Clonidine hydrochlorideW76I6XXF064205-91-8ZNIFSRGNXRYGHF-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CatapresTablet.300 mg/1OralBoehringer Ingelheim Promeco s.a. De c.v.1999-05-012013-03-25Us
CatapresTablet0.200 mg/1OralPhysicians Total Care, Inc.1974-09-032011-06-30Us
CatapresTablet0.200 mg/1OralBoehringer Ingelheim Promeco s.a. De c.v.1999-05-012013-03-25Us
CatapresTablet0.300 mg/1OralBoehringer Ingelheim1999-05-01Not applicableUs
CatapresPatch, extended release0.2 mg/24hTransdermalPhysicians Total Care, Inc.1994-10-112011-06-30Us
CatapresTablet0.100 mg/1OralBoehringer Ingelheim Promeco s.a. De c.v.1999-05-012013-03-25Us
CatapresTablet0.200 mg/1OralBoehringer Ingelheim1999-05-01Not applicableUs
CatapresPatch, extended release0.1 mg/24hTransdermalPhysicians Total Care, Inc.1994-12-092012-06-30Us
CatapresTablet0.100 mg/1OralBoehringer Ingelheim1999-05-01Not applicableUs
CatapresPatch, extended release0.1 mg/24hTransdermalRebel Distributors1985-10-01Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-clonidineTabletOralApotex Corporation2004-07-13Not applicableCanada
Apo-clonidine Tab 0.1mgTabletOralApotex Corporation1990-12-31Not applicableCanada
Apo-clonidine Tab 0.2mgTabletOralApotex Corporation1990-12-31Not applicableCanada
ClonidinePatch0.2 mg/1dTransdermalMylan Pharmaceuticals Inc.2013-02-08Not applicableUs
ClonidineTablet, extended release0.1 mg/1OralIngenus Pharmaceuticals, LLC2019-03-05Not applicableUs
ClonidinePatch0.1 mg/1dTransdermalPar Pharmaceutical2009-08-202012-06-30Us
ClonidineTablet0.1 mg/1OralStat Rx USA1986-12-16Not applicableUs00228 2127 10 nlmimage10 5321a9ed
ClonidineInjection, solution100 ug/1mLEpiduralX Gen Pharmaceuticals, Inc.2013-10-29Not applicableUs
ClonidinePatch0.1 mg/1dTransdermalMylan Pharmaceuticals Inc.2013-02-08Not applicableUs
ClonidinePatch, extended release0.3 mg/24hTransdermalCorium International, Inc.2016-08-03Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
ClorpresClonidine hydrochloride (0.1 mg/1) + Chlorthalidone (15 mg/1)TabletOralPhysicians Total Care, Inc.2005-01-262011-06-30Us
ClorpresClonidine hydrochloride (0.1 mg/1) + Chlorthalidone (15 mg/1)TabletOralMylan Bertek Pharmaceuticals2015-11-012015-11-19Us
ClorpresClonidine hydrochloride (0.3 mg/1) + Chlorthalidone (15 mg/1)TabletOralMylan Bertek Pharmaceuticals2015-11-012015-11-19Us
ClorpresClonidine hydrochloride (0.3 mg/1) + Chlorthalidone (15 mg/1)TabletOralMylan Pharmaceuticals1998-03-132018-02-28Us
ClorpresClonidine hydrochloride (0.2 mg/1) + Chlorthalidone (15 mg/1)TabletOralMylan Pharmaceuticals1998-03-132018-02-28Us
ClorpresClonidine hydrochloride (0.2 mg/1) + Chlorthalidone (15 mg/1)TabletOralPhysicians Total Care, Inc.2005-04-152011-06-30Us
ClorpresClonidine hydrochloride (0.2 mg/1) + Chlorthalidone (15 mg/1)TabletOralMylan Bertek Pharmaceuticals2015-11-012015-11-19Us
ClorpresClonidine hydrochloride (0.1 mg/1) + Chlorthalidone (15 mg/1)TabletOralMylan Pharmaceuticals1998-03-132018-02-28Us
Combipres 0.1/15 TabClonidine hydrochloride (.1 mg) + Chlorthalidone (15 mg)TabletOralBoehringer Ingelheim (Canada) Ltd Ltee1974-12-311997-08-14Canada
KapvayClonidine hydrochloride (0.1 mg/1) + Clonidine hydrochloride (0.2 mg/1)KitOralShionogi2010-12-092014-08-31Us
International/Other Brands
Catapresan (Boehringer Ingelheim) / Catapressan (Boehringer Ingelheim) / Catarpres-TTS / Dixarit (Boehringer Ingelheim) / Isoglaucon (Agepha) / Run Rui (Bausch & Lomb) / Velaril (Roemmers) / Winpress (Winston)
Categories
UNII
MN3L5RMN02
CAS number
4205-90-7
Weight
Average: 230.094
Monoisotopic: 229.017352717
Chemical Formula
C9H9Cl2N3
InChI Key
GJSURZIOUXUGAL-UHFFFAOYSA-N
InChI
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)
IUPAC Name
N-(2,6-dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine
SMILES
ClC1=CC=CC(Cl)=C1NC1=NCCN1

Pharmacology

Indication

Clonidine tablets and transdermal systems are indicated for the treatment of hypertension alone or in combination with other medications.8,9 A clonidine injection is indicated for use with opiates in the treatment of severe cancer pain where opiates alone are insufficient.10 An extended release tablet of clonidine is indicated for the treatment of ADHD either alone or in combination with other medications.11

Clonidine is also used for the diagnosis of pheochromocytoma,3 treatment of nicotine dependance,4 and opiate withdrawal.5

Associated Conditions
Associated Therapies
Pharmacodynamics

Clonidine functions through agonism of alpha-2 adrenoceptors which have effects such as lowering blood pressure, sedation, and hyperpolarization of nerves.2 It has a long duration of action as it is given twice daily and the therapeutic window is between 0.1mg and 2.4mg daily.8,9,10,11

Mechanism of action

Clonidine is primarily an alpha-2 adrenoceptor agonist which causes central hypotensive and anti-arrhythmogenic effects.2 The alpha-2 adrenoceptor is coupled to the G-proteins Go and Gi.2 Gi inhibits adenylyl cyclase and activates opening of a potassium channel that causes hyperpolarization.2 Clonidine binding to the alpha-2 adrenoceptor causes structural changes in the alpha subunit of the G-protein, reducing its affinity for GDP.2 Magnesium catalyzes the replacement of GDP with GTP.2 The alpha subunit dissociates from the other subunits and associates with an effector.2

The stimulation of alpha-2 adrenoceptors in the locus coeruleus may be responsible for the hypnotic effects of clonidine as this region of the brain helps regulate wakefulness.2 Clonidine can also decrease transmission of pain signals at the spine.2 Finally clonidine can affect regulators of blood pressure in the ventromedial and rostral-ventrolateral areas of the medulla.2

TargetActionsOrganism
AAlpha-2A adrenergic receptor
agonist
Humans
AAlpha-2B adrenergic receptor
agonist
Humans
AAlpha-2C adrenergic receptor
agonist
Humans
UAlpha-1A adrenergic receptor
agonist
Humans
UAlpha-1B adrenergic receptor
agonist
Humans
UAlpha-1D adrenergic receptor
agonist
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

Clonidine reaches maximum concentration in 60-90 minutes after oral administration.2,6 Race and fasting status do not influence pharmacokinetics of clonidine.8

A 100µg oral clonidine tablet reaches a Cmax of 400.72pg/mL with an AUC of 5606.78h*pg/mL and a bioavailability of 55-87%.6

Volume of distribution

The volume of distribution of clonidine has been reported as 1.7-2.5L/kg2, 2.9L/kg9, or 2.1±0.4L/kg10 depending on the source.

Protein binding

Clonidine is 20-40% bound to plasma proteins, especially albumin.2,10

Metabolism

The metabolism of clonidine is poorly understood.7 The main reaction in clonidine metabolism is the 4-hydroxylation of clonidine by CYP2D6, CYP1A2, CYP3A4, CYP1A1, and CYP3A5.7

Clonidine is <50% metabolized in the liver to inactive metabolites.2,8,9,10,11

Route of elimination

Approximately 50% of a clonidine dose is excreted in the urine as the unchanged drug and 20% is eliminated in the feces.2,8

Half life

The elimination half life after epidural administration is 30 minutes but otherwise can range from 6-23h.2

Clearance

The clearance of clonidine is 1.9-4.3mL/min/kg.2

Toxicity

Oral LD50 is 126 mg/kg in rats.12 The TDLO is 70µg/kg in children, 126µg/kg in women, and 69µg/kg in men.12

Symptoms of overdose include hypertension followed by hypotension, bradycardia, respiratory depression, hypothermia, drowsiness, decreased reflexes, weakness, irritability, and miosis.8,9,10,11 Severe overdoses can cause reversible cardiac conduction defects or dysrhythmias, apnea, coma, and seizures.8,9,10,11 Induction of vomiting is not recommended due to CNS depression but gastric lavage or activated charcoal may be useful in recent ingestion.8,9,10,11 Dialysis is also unlikely to be beneficial.8,9,10,11 Overdose can be treated with supportive measures such as atropine sulfate for bradycardia, intravenous fluids or vasopressors for hypotension, vasodilators for hypertension, naloxone for respiratory depression, and blood pressure monitoring.8,9,10,11

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidineThe metabolism of Clonidine can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid may decrease the antihypertensive activities of Clonidine.
1-benzylimidazoleThe risk or severity of hypertension can be increased when Clonidine is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of hypertension can be increased when Clonidine is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of sedation can be increased when Clonidine is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of sedation can be increased when Clonidine is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-MethoxyamphetamineThe risk or severity of sedation can be increased when Clonidine is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of sedation can be increased when Clonidine is combined with 5-methoxy-N,N-dimethyltryptamine.
6-Deoxyerythronolide BThe metabolism of Clonidine can be decreased when combined with 6-Deoxyerythronolide B.
7-ethyl-10-hydroxycamptothecinThe metabolism of Clonidine can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.

References

Synthesis Reference

David R. Pierce, William D. Dean, Michael E. Deason, "Process for preparation of clonidine derivatives." U.S. Patent US5684156, issued October, 1968.

US5684156
General References
  1. Hossmann V, Maling TJ, Hamilton CA, Reid JL, Dollery CT: Sedative and cardiovascular effects of clonidine and nitrazepam. Clin Pharmacol Ther. 1980 Aug;28(2):167-76. [PubMed:7398184]
  2. Khan ZP, Ferguson CN, Jones RM: alpha-2 and imidazoline receptor agonists. Their pharmacology and therapeutic role. Anaesthesia. 1999 Feb;54(2):146-65. doi: 10.1046/j.1365-2044.1999.00659.x. [PubMed:10215710]
  3. Sjoberg RJ, Simcic KJ, Kidd GS: The clonidine suppression test for pheochromocytoma. A review of its utility and pitfalls. Arch Intern Med. 1992 Jun;152(6):1193-7. [PubMed:1599347]
  4. Sliwinska-Mosson M, Zielen I, Milnerowicz H: New trends in the treatment of nicotine addiction. Acta Pol Pharm. 2014 Jul-Aug;71(4):525-30. [PubMed:25272878]
  5. Fresquez-Chavez KR, Fogger S: Reduction of opiate withdrawal symptoms with use of clonidine in a county jail. J Correct Health Care. 2015 Jan;21(1):27-34. doi: 10.1177/1078345814557630. Epub 2014 Nov 26. [PubMed:25431436]
  6. Vasseur B, Dufour A, Houdas L, Goodwin H, Harries K, Emul NY, Hutchings S: Comparison of the Systemic and Local Pharmacokinetics of Clonidine Mucoadhesive Buccal Tablets with Reference Clonidine Oral Tablets in Healthy Volunteers: An Open-Label Randomised Cross-Over Trial. Adv Ther. 2017 Aug;34(8):2022-2032. doi: 10.1007/s12325-017-0585-9. Epub 2017 Jul 19. [PubMed:28726169]
  7. Claessens AJ, Risler LJ, Eyal S, Shen DD, Easterling TR, Hebert MF: CYP2D6 mediates 4-hydroxylation of clonidine in vitro: implication for pregnancy-induced changes in clonidine clearance. Drug Metab Dispos. 2010 Sep;38(9):1393-6. doi: 10.1124/dmd.110.033878. Epub 2010 Jun 22. [PubMed:20570945]
  8. FDA Approved Drug Products: Catapres Clonidine Hydrochloride Oral Tablets [Link]
  9. FDA Approved Drug Products: Catapres Clonidine Transdermal System [Link]
  10. FDA Approved Drug Products: Duraclon Clonidine Hydrochloride Injection Solution [Link]
  11. FDA Approved Drug Products: Kapvay Clonidine Hydrochloride Oral Extended Release Tablets [Link]
  12. Cayman Chemicals: Clonidine MSDS [Link]
External Links
Human Metabolome Database
HMDB0014714
KEGG Drug
D00281
PubChem Compound
2803
PubChem Substance
46508119
ChemSpider
2701
BindingDB
14062
ChEBI
46632
ChEMBL
CHEMBL134
Therapeutic Targets Database
DAP000231
PharmGKB
PA449051
Guide to Pharmacology
GtP Drug Page
HET
CLU
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Clonidine
ATC Codes
S01EA04 — ClonidineC02LC01 — Clonidine and diureticsC02AC01 — ClonidineN02CX02 — ClonidineC02LC51 — Clonidine and diuretics, combinations with other drugs
AHFS Codes
  • 24:08.16 — Central Alpha-agonists
PDB Entries
2pnc
MSDS
Download (73.8 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Not Yet RecruitingBasic ScienceHealthy Volunteers1
0Not Yet RecruitingBasic ScienceMalignancies / Neuro-Degenerative Disease1
0Not Yet RecruitingTreatmentBlood Pressures / High Blood Pressure (Hypertension)1
1Active Not RecruitingScreeningAutonomic Nervous System Diseases / Dopamine Beta-Hydroxylase Deficiency / Orthostatic Hypotension / Orthostatic Intolerance1
1CompletedBasic ScienceAmphetamine-Related Disorders / Moods Disorders / Substance-Related Disorders1
1CompletedTreatmentCocaine Abuse / Heroin Abuse1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentHigh Blood Pressure (Hypertension)1
1CompletedTreatmentOpioid-Related Disorders1
1Not Yet RecruitingBasic ScienceHealthy Controls1
1RecruitingTreatmentCutaneous Nerves CNS Itch1
1RecruitingTreatmentHypoxic Ischemic Encephalopathy (HIE)1
1, 2Active Not RecruitingTreatmentChronic Orthostatic Intolerance / Tachycardia1
1, 2CompletedPreventionPost Operative Pain1
1, 2CompletedTreatmentHypoxic-Ischaemic Encephalopathy1
1, 2CompletedTreatmentOpioid Addiction / Opioid Dependence / Opioid Related Disorders1
1, 2CompletedTreatmentPain, Acute / Respiration stimulated / Sedation1
1, 2CompletedTreatmentPostoperative pain1
1, 2RecruitingTreatmentMechanical Ventilation Complication1
1, 2TerminatedTreatmentPain1
1, 2WithdrawnTreatmentHigh Blood Pressure (Hypertension) / Pregnancy Toxemias / Proteinuria1
1, 2WithdrawnTreatmentTreatment-Related Cancer1
2Active Not RecruitingSupportive CareBreast Cancer / Hot Flushes1
2CompletedSupportive CareCholesteatoma / Cochlear Implants / Mastoidectomy / Tympanomastoid Surgery1
2CompletedSupportive CarePostoperative pain1
2CompletedTreatmentAnaesthesia therapy2
2CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)1
2CompletedTreatmentBrain Injury / Craniocerebral Trauma / Trauma, Nervous System / Traumatic Brain Injury (TBI)1
2CompletedTreatmentDiabetes Mellitus (DM) / Painful Diabetic Neuropathy (PDN)1
2CompletedTreatmentDiabetic Neuropathies / Neuropathy / Painful Diabetic Neuropathy (PDN)2
2CompletedTreatmentDrug withdrawal syndrome neonatal1
2CompletedTreatmentFascicular Block / Latency Period / Motor Activities / Postoperative pain1
2CompletedTreatmentFecal Incontinence1
2CompletedTreatmentHealthy Volunteers1
2CompletedTreatmentCaudal epidural block therapy / Herniorrhaphy / Regional Anesthesia1
2CompletedTreatmentHigh Blood Pressure (Hypertension)1
2CompletedTreatmentHydrocele / Inguinal Hernias1
2CompletedTreatmentIndication for Surgery of the Posterior Segment Under Locoregional Anaesthesia1
2CompletedTreatmentMyalgic Encephalomyelitis (ME)1
2CompletedTreatmentOpioid-Related Disorders / Substance-Related Disorders1
2CompletedTreatmentOral Mucositis1
2CompletedTreatmentPain2
2CompletedTreatmentPainful Diabetic Neuropathy (PDN)1
2RecruitingTreatmentBMI >30 kg/m2 / High Blood Pressure (Hypertension) / Prehypertension1
2RecruitingTreatmentDrug withdrawal syndrome neonatal1
2RecruitingTreatmentMpulse Control Disorders / Parkinson's Disease (PD)1
2TerminatedTreatmentDelirium1
2TerminatedTreatmentVasospasm1
2Unknown StatusTreatmentAnxiety1
2Unknown StatusTreatmentArrhythmia / Pain1
2WithdrawnTreatmentAutism Spectrum Conditions/Disorders1
2WithdrawnTreatmentOther Reconstructive Surgery1
2, 3CompletedPreventionTransversus Abdominis Plane Block / Transversus Abdominis Plane Block, Pediatric Laparoscopy1
2, 3CompletedTreatmentPre- and Postoperative Analgesia / Renal Cell Adenocarcinoma / Spinal Anaesthesia1
2, 3CompletedTreatmentMinor burns1
2, 3RecruitingTreatmentSubstance, Addiction1
2, 3TerminatedDiagnosticShock, Septic1
2, 3TerminatedTreatmentCannabis Dependence / Marijuana Dependence1
2, 3TerminatedTreatmentDrug withdrawal syndrome neonatal1
3CompletedPreventionCardiovascular Disease (CVD)1
3CompletedPreventionIs an Only Child1
3CompletedPreventionNegative Behaviour Change1
3CompletedPreventionNormal Pregnancies1
3CompletedTreatmentAttention Deficit Disorder With Hyperactivity2
3CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)2
3CompletedTreatmentBiceps Tendonitis1
3CompletedTreatmentCritical Illness / Delirium1
3CompletedTreatmentHyperemesis Gravidarum1
3CompletedTreatmentPostoperative pain1
3CompletedTreatmentLumbar epidural anesthesia therapy1
3Not Yet RecruitingTreatmentChild Preschool1
3Not Yet RecruitingTreatmentDelirium1
3RecruitingSupportive CareIntraoperative Neurophysiological Monitoring / Pain Management1
3RecruitingSupportive CareMalignant Neoplasms of Male Genital Organs1
3RecruitingTreatmentBile Acid Malabsorption / Fecal Incontinence1
3RecruitingTreatmentCritical Illness / Sedation in Critically Ill Patients1
3RecruitingTreatmentDrug withdrawal syndrome neonatal1
3RecruitingTreatmentLocoregional Analgesia / Locoregional Analgesia in Breast Surgery / Neoplasms, Breast1
3RecruitingTreatmentLumbosacral Radiculopathy1
3RecruitingTreatmentPain1
3RecruitingTreatmentScoliosis1
3TerminatedTreatmentPain1
3TerminatedTreatmentSedation in Intensive Care1
3Unknown StatusTreatmentDiabetic Neuropathies / Pain1
3WithdrawnTreatmentPostoperative Hyperalgesia1
4Active Not RecruitingBasic ScienceAnxiety / High Blood Pressure (Hypertension)1
4Active Not RecruitingTreatmentAnterior Cruciate Ligament Injury1
4Active Not RecruitingTreatmentInguinal Hernias / Spinal Anaesthesia1
4Active Not RecruitingTreatmentOpiate withdrawal symptoms1
4CompletedBasic ScienceHeart Failure1
4CompletedPreventionCardiovascular Disease (CVD)1
4CompletedPreventionHigh Blood Pressure (Hypertension)1
4CompletedPreventionPsychomotor Agitation1
4CompletedPreventionShivering1
4CompletedSupportive CareFemoracetabular Impingement / Postoperative pain1
4CompletedTreatmentAcetabular Labrum Tear / Femoroacetabular Impingement / Hip Dysplasia1
4CompletedTreatmentAnalgesia / Pain / Systemic Inflammatory Stress Response1
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)1
4CompletedTreatmentBimalleolar Fractures of the Ankle / Post Operative Analgesia Duration / Saphenous Nerve Block / Sciatic Nerve Block1
4CompletedTreatmentCritical Illness / Deep Sedation / Respiration, Artificial / Sedation, Conscious1
4CompletedTreatmentDelirium1
4CompletedTreatmentFractures, Closed / Hip Arthritis / Knee Arthropathy1
4CompletedTreatmentGilles de la Tourette's Syndrome / Tic Disorders1
4CompletedTreatmentGlycemia During Coronary Artery Bypass Graft / Sedation During Pre-anesthetic Medication1
4CompletedTreatmentHigh Blood Pressure (Hypertension)2
4CompletedTreatmentLabour1
4CompletedTreatmentLabour Pain1
4CompletedTreatmentLocal Anesthesia1
4CompletedTreatmentOpiate withdrawal symptoms / Opioid-use Disorder1
4CompletedTreatmentCaudal epidural block therapy / Pain / Total Knee Arthroplasty (TKA)1
4CompletedTreatmentPatients to Benefit a Planned Femoropopliteal Bypass Through PAOD (Peripheral Arterial Occlusive Disease) Stage II or III / Peripheral Obliterative Arteriopathy1
4CompletedTreatmentPhysiology1
4CompletedTreatmentPhysiology, Ocular / Regional Blood Flow1
4CompletedTreatmentPost-Operative Pain1
4CompletedTreatmentPostoperative pain1
4CompletedTreatmentPreeclampsia1
4CompletedTreatmentTotal Hip and Knee Arthroplasty / Total Hip Arthroplasty (THA)1
4Enrolling by InvitationTreatmentAnesthesia Complication / Hemodynamics Instability / Ileus paralytic / Nausea / Postoperative pain / Vomiting1
4Enrolling by InvitationTreatmentKnee Osteoarthritis (Knee OA)1
4RecruitingPreventionPostoperative pain1
4RecruitingTreatmentDrug withdrawal syndrome neonatal1
4RecruitingTreatmentLabour Pain1
4RecruitingTreatmentPostoperative pain2
4SuspendedTreatmentDrug withdrawal syndrome neonatal1
4TerminatedTreatmentBipolar Disorder, Mania1
4TerminatedTreatmentDegenerative Joint Disease / Osteoarthritis (OA)1
4Unknown StatusDiagnosticAtaxia Telangiectasia (AT) / Growth Failure1
4Unknown StatusPreventionDiabetic Nephropathies1
4Unknown StatusPreventionHeart Diseases1
4Unknown StatusTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Gilles de la Tourette's Syndrome1
4Unknown StatusTreatmentDrug withdrawal syndrome neonatal1
4Unknown StatusTreatmentHigh Blood Pressure (Hypertension)1
4Unknown StatusTreatmentNeonates / Spinal Anaesthesia1
4WithdrawnPreventionKnee Arthroscopy / Shoulder Arthroscopy1
4WithdrawnSupportive CarePain Management / Total Knee Arthroplasty (TKA)1
4WithdrawnTreatmentKnee Osteoarthritis (Knee OA)1
4WithdrawnTreatmentLabour Pain1
Not AvailableActive Not RecruitingTreatmentDepressive Disorder, Treatment-Resistant1
Not AvailableCompletedNot AvailableKnee Osteoarthritis (Knee OA)1
Not AvailableCompletedNot AvailableLabour Pain1
Not AvailableCompletedNot AvailableMyalgic Encephalomyelitis (ME)1
Not AvailableCompletedNot AvailableRhytidoplasty1
Not AvailableCompletedNot AvailableSedation1
Not AvailableCompletedNot AvailableUpper Extremity Fractures / Upper Extremity Surgery1
Not AvailableCompletedBasic ScienceIntrusive Memories1
Not AvailableCompletedPreventionDelirium on Emergence1
Not AvailableCompletedPreventionSecondary Hyperalgesia1
Not AvailableCompletedSupportive CareAnxiety / Pain1
Not AvailableCompletedSupportive CareOsteoarthritis (OA) / Post-traumatic; Arthrosis1
Not AvailableCompletedTreatmentAscitic Cirrhosis / Hyperactivation of Sympathetic Nervous System1
Not AvailableCompletedTreatmentCerebral Hemorrhage / Cerebrovascular Accident / Intracranial Hemorrhages1
Not AvailableCompletedTreatmentKnee Osteoarthritis (Knee OA)1
Not AvailableCompletedTreatmentOpiate Addiction1
Not AvailableCompletedTreatmentPregnancy1
Not AvailableCompletedTreatmentSchizophrenic Disorders1
Not AvailableCompletedTreatmentSubstance Withdrawal Syndrome1
Not AvailableRecruitingNot AvailableAsphyxia Neonatorum1
Not AvailableRecruitingPreventionPostoperative pain1
Not AvailableRecruitingSupportive CarePain Management1
Not AvailableRecruitingTreatmentPilonidal Sinus1
Not AvailableRecruitingTreatmentRenal Dialysis1
Not AvailableTerminatedSupportive CareComplex Regional Pain Syndrome (CRPS)1
Not AvailableTerminatedTreatmentAnxiety / Pain1
Not AvailableTerminatedTreatmentBack Pain, Unspecified1
Not AvailableTerminatedTreatmentDrug withdrawal syndrome neonatal1
Not AvailableTerminatedTreatmentLumbar and Other Intervertebral Disc Disorders With Radiculopathy1
Not AvailableTerminatedTreatmentPostoperative pain1
Not AvailableWithdrawnBasic ScienceExperimental Pain Perception1
Not AvailableWithdrawnTreatmentFull Term Pregnant Patients / Undergoing Lower Segment Caesarian Section1
Not AvailableWithdrawnTreatmentHigh Blood Pressure (Hypertension)1
Not AvailableWithdrawnTreatmentVentricular Tachycardia (VT)1

Pharmacoeconomics

Manufacturers
  • Boehringer ingelheim
  • Aveva drug delivery systems inc
  • Mylan technologies inc
  • Tris pharma inc
  • Pharmaforce inc
  • Bioniche pharma usa llc
  • Actavis elizabeth llc
  • American therapeutics inc
  • Dava pharmaceuticals inc
  • Duramed pharmaceuticals inc sub barr laboratories inc
  • Impax laboratories inc
  • Interpharm inc
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Par pharmaceutical inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Unichem laboratories ltd
  • Vintage pharmaceuticals llc
  • Warner chilcott div warner lambert co
  • Watson laboratories inc
  • Shionogi pharma inc
Packagers
  • AAIPharma Inc.
  • Actavis Group
  • Advanced Pharmaceutical Services Inc.
  • Alza Corp.
  • American Regent
  • Amerisource Health Services Corp.
  • Apotheca Inc.
  • APP Pharmaceuticals
  • A-S Medication Solutions LLC
  • Bioniche Pharma
  • Blenheim Pharmacal
  • Boehringer Ingelheim Ltd.
  • Bryant Ranch Prepack
  • Cardinal Health
  • Central Texas Community Health Centers
  • Comprehensive Consultant Services Inc.
  • Coupler Enterprises Inc.
  • DAVA Pharmaceuticals
  • Dept Health Central Pharmacy
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Global Pharmaceuticals
  • Heartland Repack Services LLC
  • Innoviant Pharmacy Inc.
  • Lake Erie Medical and Surgical Supply
  • Liberty Pharmaceuticals
  • Major Pharmaceuticals
  • Mckesson Corp.
  • Medisca Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mutual Pharmaceutical Co.
  • Mylan
  • Neighborcare Repackaging Inc.
  • Neuman Distributors Inc.
  • Nucare Pharmaceuticals Inc.
  • Palmetto Pharmaceuticals Inc.
  • Par Pharmaceuticals
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Pharmaceutical Utilization Management Program VA Inc.
  • Pharmaforce Inc.
  • Pharmedix
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Qualitest
  • Rebel Distributors Corp.
  • Redpharm Drug
  • Remedy Repack
  • Richmond Pharmacy
  • Sandhills Packaging Inc.
  • Southwood Pharmaceuticals
  • Stat Rx Usa
  • Tya Pharmaceuticals
  • UDL Laboratories
  • Unichem Laboratories Ltd.
  • United Research Laboratories Inc.
  • Vangard Labs Inc.
  • Vintage Pharmaceuticals Inc.
  • West-Ward Pharmaceuticals
  • Xanodyne Pharmaceuticals Inc.
Dosage forms
FormRouteStrength
Patch, extended releaseTransdermal0.1 mg/24h
Patch, extended releaseTransdermal0.2 mg/24h
Patch, extended releaseTransdermal0.3 mg/24h
TabletOral.300 mg/1
PatchTransdermal0.1 mg/1d
PatchTransdermal0.2 mg/1d
PatchTransdermal0.3 mg/1d
TabletOral0.025 mg
TabletOral0.1 mg
TabletOral0.2 mg
Injection, solutionEpidural0.1 mg/1mL
Injection, solutionEpidural0.5 mg/1mL
Injection, solutionEpidural100 ug/1mL
Injection, solutionEpidural500 ug/1mL
Injection, solutionIntravenous100 ug/1mL
Injection, solutionIntravenous500 ug/1mL
TabletOral.1 mg/1
TabletOral.2 mg/1
TabletOral.3 mg/1
TabletOral0.1 mg/1
TabletOral0.100 mg/1
TabletOral0.2 mg/1
TabletOral0.200 mg/1
TabletOral0.3 mg/1
TabletOral0.300 mg/1
Tablet, extended releaseOral25 mg/1
TabletOral
Injection, solutionIntravenous0.1 mg/1mL
Injection, solutionIntravenous0.5 mg/1mL
KitOral
Tablet, extended releaseOral0.1 mg/1
Tablet, extended releaseOral0.2 mg/1
For suspension, extended releaseOral0.09 mg/1mL
Suspension, extended releaseOral0.09 mg/1mL
Tablet, extended releaseOral0.17 mg/1
Tablet, extended releaseOral0.26 mg/1
TabletOral
Prices
Unit descriptionCostUnit
Catapres-TTS-3 4 0.3 mg/24hr Patches Box328.42USD box
CloNIDine HCl 4 0.3 mg/24hr Patches Box279.9USD box
Catapres-TTS-2 4 0.2 mg/24hr Patches Box236.75USD box
CloNIDine HCl 4 0.2 mg/24hr Patches Box201.75USD box
Catapres-TTS-1 4 0.1 mg/24hr Patches Box141.08USD box
CloNIDine HCl 4 0.1 mg/24hr Patches Box119.84USD box
Catapres-tts 3 patch78.95USD patch
Clonidine 0.3 mg/day patch67.28USD patch
Clonidine hcl powder53.09USD g
Clonidine 0.2 mg/day patch48.5USD patch
Duraclon 500 mcg/ml vial47.4USD ml
Catapres-tts 2 patch39.23USD patch
Clonidine 0.1 mg/day patch28.81USD patch
Catapres-tts 1 patch21.18USD patch
Clonidine 5000 mcg/10 ml vial21.0USD ml
Duraclon 0.1 mg/ml vial14.4USD ml
Clonidine 1000 mcg/10 ml vial5.04USD ml
Catapres 0.3 mg tablet2.98USD tablet
Catapres 0.2 mg tablet2.35USD tablet
Catapres 0.1 mg tablet1.57USD tablet
Clonidine hcl 0.3 mg tablet0.5USD tablet
Clonidine hcl 0.2 mg tablet0.35USD tablet
Catapres 0.2 mg Tablet0.35USD tablet
Apo-Clonidine 0.2 mg Tablet0.33USD tablet
Novo-Clonidine 0.2 mg Tablet0.33USD tablet
Nu-Clonidine 0.2 mg Tablet0.33USD tablet
Dixarit 0.025 mg Tablet0.28USD tablet
Clonidine hcl 0.1 mg tablet0.24USD tablet
Catapres 0.1 mg Tablet0.19USD tablet
Apo-Clonidine 0.1 mg Tablet0.18USD tablet
Novo-Clonidine 0.1 mg Tablet0.18USD tablet
Nu-Clonidine 0.1 mg Tablet0.18USD tablet
Apo-Clonidine 0.025 mg Tablet0.16USD tablet
Novo-Clonidine 0.025 mg Tablet0.16USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5869100No1999-02-092013-10-13Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)130http://www.chemspider.com/Chemical-Structure.2701.html?rid=816613e6-a54a-46f0-8152-4a93e09e4170
logP1.59HANSCH,C & LEO,AJ (1985)
Caco2 permeability-4.59ADME Research, USCD
pKa8.05 (at 25 °C)KONTTURI,K & MURTOMAKI,L (1992)
Predicted Properties
PropertyValueSource
Water Solubility0.48 mg/mLALOGPS
logP2.55ALOGPS
logP2.49ChemAxon
logS-2.7ALOGPS
pKa (Strongest Basic)8.16ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area36.42 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity59.09 m3·mol-1ChemAxon
Polarizability21.7 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9632
Blood Brain Barrier+0.9402
Caco-2 permeable+0.8866
P-glycoprotein substrateSubstrate0.6305
P-glycoprotein inhibitor INon-inhibitor0.9061
P-glycoprotein inhibitor IINon-inhibitor0.8383
Renal organic cation transporterInhibitor0.745
CYP450 2C9 substrateNon-substrate0.8219
CYP450 2D6 substrateNon-substrate0.6984
CYP450 3A4 substrateNon-substrate0.6353
CYP450 1A2 substrateNon-inhibitor0.8998
CYP450 2C9 inhibitorNon-inhibitor0.7681
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.8732
CYP450 3A4 inhibitorNon-inhibitor0.8332
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.803
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.9303
BiodegradationNot ready biodegradable0.9949
Rat acute toxicity3.5030 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7232
hERG inhibition (predictor II)Non-inhibitor0.8905
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-003r-5970000000-33c27878b8b7ad9d5d75
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-001i-0090000000-2c051509a637beaafe73
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-001i-0090000000-f1477af875c25c537ccb
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-001i-0090000000-ccdeb1dfce0424b12c0c
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-01po-6950000000-dd68628a46215027ef29
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0006-6900000000-ce531320f1fda74d127e
LC-MS/MS Spectrum - LC-ESI-IT , positiveLC-MS/MSsplash10-03fr-2980000000-24b18e2a89a65b2b178f
MS/MS Spectrum - , positiveLC-MS/MSsplash10-001i-0190000000-7cbbf9fb244993abe922

Taxonomy

Description
This compound belongs to the class of organic compounds known as dichlorobenzenes. These are compounds containing a benzene with exactly two chlorine atoms attached to it.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Halobenzenes
Direct Parent
Dichlorobenzenes
Alternative Parents
Aniline and substituted anilines / Aryl chlorides / Imidazolines / Guanidines / Propargyl-type 1,3-dipolar organic compounds / Carboximidamides / Azacyclic compounds / Organopnictogen compounds / Organochlorides / Hydrocarbon derivatives
Substituents
1,3-dichlorobenzene / Aniline or substituted anilines / Aryl chloride / Aryl halide / 2-imidazoline / Guanidine / Organic 1,3-dipolar compound / Propargyl-type 1,3-dipolar organic compound / Carboximidamide / Azacycle
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
clonidine (CHEBI:3757)

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. Fairbanks CA, Stone LS, Kitto KF, Nguyen HO, Posthumus IJ, Wilcox GL: alpha(2C)-Adrenergic receptors mediate spinal analgesia and adrenergic-opioid synergy. J Pharmacol Exp Ther. 2002 Jan;300(1):282-90. [PubMed:11752127]
  2. Lavand'homme PM, Ma W, De Kock M, Eisenach JC: Perineural alpha(2A)-adrenoceptor activation inhibits spinal cord neuroplasticity and tactile allodynia after nerve injury. Anesthesiology. 2002 Oct;97(4):972-80. [PubMed:12357167]
  3. Ozdogan UK, Lahdesmaki J, Hakala K, Scheinin M: The involvement of alpha 2A-adrenoceptors in morphine analgesia, tolerance and withdrawal in mice. Eur J Pharmacol. 2004 Aug 23;497(2):161-71. [PubMed:15306201]
  4. Ozdogan UK, Lahdesmaki J, Mansikka H, Scheinin M: Loss of amitriptyline analgesia in alpha 2A-adrenoceptor deficient mice. Eur J Pharmacol. 2004 Feb 6;485(1-3):193-6. [PubMed:14757140]
  5. Wang XM, Zhang ZJ, Bains R, Mokha SS: Effect of antisense knock-down of alpha(2a)- and alpha(2c)-adrenoceptors on the antinociceptive action of clonidine on trigeminal nociception in the rat. Pain. 2002 Jul;98(1-2):27-35. [PubMed:12098614]
  6. Millan MJ, Dekeyne A, Newman-Tancredi A, Cussac D, Audinot V, Milligan G, Duqueyroix D, Girardon S, Mullot J, Boutin JA, Nicolas JP, Renouard-Try A, Lacoste JM, Cordi A: S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine. J Pharmacol Exp Ther. 2000 Dec;295(3):1192-205. [PubMed:11082457]
  7. Hein, L. (2004). alpha-Adrenergic system. In Encyclopedic reference of molecular pharmacology (pp. 27-30). Berlin: Springer. [ISBN:9783540298328]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Epinephrine binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
Molecular Weight
49565.8 Da
References
  1. Millan MJ, Dekeyne A, Newman-Tancredi A, Cussac D, Audinot V, Milligan G, Duqueyroix D, Girardon S, Mullot J, Boutin JA, Nicolas JP, Renouard-Try A, Lacoste JM, Cordi A: S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine. J Pharmacol Exp Ther. 2000 Dec;295(3):1192-205. [PubMed:11082457]
  2. Hein, L. (2004). alpha-Adrenergic system. In Encyclopedic reference of molecular pharmacology (pp. 27-30). Berlin: Springer. [ISBN:9783540298328]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Protein homodimerization activity
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name
ADRA2C
Uniprot ID
P18825
Uniprot Name
Alpha-2C adrenergic receptor
Molecular Weight
49521.585 Da
References
  1. Millan MJ, Dekeyne A, Newman-Tancredi A, Cussac D, Audinot V, Milligan G, Duqueyroix D, Girardon S, Mullot J, Boutin JA, Nicolas JP, Renouard-Try A, Lacoste JM, Cordi A: S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine. J Pharmacol Exp Ther. 2000 Dec;295(3):1192-205. [PubMed:11082457]
  2. Hein, L. (2004). alpha-Adrenergic system. In Encyclopedic reference of molecular pharmacology (pp. 27-30). Berlin: Springer. [ISBN:9783540298328]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. Millan MJ, Dekeyne A, Newman-Tancredi A, Cussac D, Audinot V, Milligan G, Duqueyroix D, Girardon S, Mullot J, Boutin JA, Nicolas JP, Renouard-Try A, Lacoste JM, Cordi A: S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine. J Pharmacol Exp Ther. 2000 Dec;295(3):1192-205. [PubMed:11082457]
  2. PDSP Ki Database [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
Molecular Weight
56835.375 Da
References
  1. Millan MJ, Dekeyne A, Newman-Tancredi A, Cussac D, Audinot V, Milligan G, Duqueyroix D, Girardon S, Mullot J, Boutin JA, Nicolas JP, Renouard-Try A, Lacoste JM, Cordi A: S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine. J Pharmacol Exp Ther. 2000 Dec;295(3):1192-205. [PubMed:11082457]
  2. PDSP Ki Database [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Alpha1-adrenergic receptor activity
Specific Function
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name
ADRA1D
Uniprot ID
P25100
Uniprot Name
Alpha-1D adrenergic receptor
Molecular Weight
60462.205 Da
References
  1. Millan MJ, Dekeyne A, Newman-Tancredi A, Cussac D, Audinot V, Milligan G, Duqueyroix D, Girardon S, Mullot J, Boutin JA, Nicolas JP, Renouard-Try A, Lacoste JM, Cordi A: S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine. J Pharmacol Exp Ther. 2000 Dec;295(3):1192-205. [PubMed:11082457]
  2. PDSP Ki Database [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Claessens AJ, Risler LJ, Eyal S, Shen DD, Easterling TR, Hebert MF: CYP2D6 mediates 4-hydroxylation of clonidine in vitro: implication for pregnancy-induced changes in clonidine clearance. Drug Metab Dispos. 2010 Sep;38(9):1393-6. doi: 10.1124/dmd.110.033878. Epub 2010 Jun 22. [PubMed:20570945]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
Data is limited to an in vitro study.
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Claessens AJ, Risler LJ, Eyal S, Shen DD, Easterling TR, Hebert MF: CYP2D6 mediates 4-hydroxylation of clonidine in vitro: implication for pregnancy-induced changes in clonidine clearance. Drug Metab Dispos. 2010 Sep;38(9):1393-6. doi: 10.1124/dmd.110.033878. Epub 2010 Jun 22. [PubMed:20570945]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Claessens AJ, Risler LJ, Eyal S, Shen DD, Easterling TR, Hebert MF: CYP2D6 mediates 4-hydroxylation of clonidine in vitro: implication for pregnancy-induced changes in clonidine clearance. Drug Metab Dispos. 2010 Sep;38(9):1393-6. doi: 10.1124/dmd.110.033878. Epub 2010 Jun 22. [PubMed:20570945]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d 24-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. Claessens AJ, Risler LJ, Eyal S, Shen DD, Easterling TR, Hebert MF: CYP2D6 mediates 4-hydroxylation of clonidine in vitro: implication for pregnancy-induced changes in clonidine clearance. Drug Metab Dispos. 2010 Sep;38(9):1393-6. doi: 10.1124/dmd.110.033878. Epub 2010 Jun 22. [PubMed:20570945]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Claessens AJ, Risler LJ, Eyal S, Shen DD, Easterling TR, Hebert MF: CYP2D6 mediates 4-hydroxylation of clonidine in vitro: implication for pregnancy-induced changes in clonidine clearance. Drug Metab Dispos. 2010 Sep;38(9):1393-6. doi: 10.1124/dmd.110.033878. Epub 2010 Jun 22. [PubMed:20570945]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Khan ZP, Ferguson CN, Jones RM: alpha-2 and imidazoline receptor agonists. Their pharmacology and therapeutic role. Anaesthesia. 1999 Feb;54(2):146-65. doi: 10.1046/j.1365-2044.1999.00659.x. [PubMed:10215710]
  2. FDA Approved Drug Products: Duraclon Clonidine Hydrochloride Injection Solution [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Toxin transporter activity
Specific Function
Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
Gene Name
SLC22A3
Uniprot ID
O75751
Uniprot Name
Solute carrier family 22 member 3
Molecular Weight
61279.485 Da
References
  1. Wu X, Huang W, Ganapathy ME, Wang H, Kekuda R, Conway SJ, Leibach FH, Ganapathy V: Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney. Am J Physiol Renal Physiol. 2000 Sep;279(3):F449-58. [PubMed:10966924]
  2. Martel F, Grundemann D, Calhau C, Schomig E: Apical uptake of organic cations by human intestinal Caco-2 cells: putative involvement of ASF transporters. Naunyn Schmiedebergs Arch Pharmacol. 2001 Jan;363(1):40-9. [PubMed:11191835]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Symporter activity
Specific Function
Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cat...
Gene Name
SLC22A5
Uniprot ID
O76082
Uniprot Name
Solute carrier family 22 member 5
Molecular Weight
62751.08 Da
References
  1. Ohashi R, Tamai I, Yabuuchi H, Nezu JI, Oku A, Sai Y, Shimane M, Tsuji A: Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance. J Pharmacol Exp Ther. 1999 Nov;291(2):778-84. [PubMed:10525100]
  2. Wu X, Huang W, Prasad PD, Seth P, Rajan DP, Leibach FH, Chen J, Conway SJ, Ganapathy V: Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter. J Pharmacol Exp Ther. 1999 Sep;290(3):1482-92. [PubMed:10454528]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Symporter activity
Specific Function
Sodium-ion dependent, low affinity carnitine transporter. Probably transports one sodium ion with one molecule of carnitine. Also transports organic cations such as tetraethylammonium (TEA) without...
Gene Name
SLC22A4
Uniprot ID
Q9H015
Uniprot Name
Solute carrier family 22 member 4
Molecular Weight
62154.48 Da
References
  1. Yabuuchi H, Tamai I, Nezu J, Sakamoto K, Oku A, Shimane M, Sai Y, Tsuji A: Novel membrane transporter OCTN1 mediates multispecific, bidirectional, and pH-dependent transport of organic cations. J Pharmacol Exp Ther. 1999 May;289(2):768-73. [PubMed:10215651]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Faassen F, Vogel G, Spanings H, Vromans H: Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. Int J Pharm. 2003 Sep 16;263(1-2):113-22. [PubMed:12954186]

Drug created on June 13, 2005 07:24 / Updated on November 19, 2019 16:25