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Identification
NameClonidine
Accession NumberDB00575  (APRD00174, DB07566)
TypeSmall Molecule
GroupsApproved
Description

Clonidine, an imidazoline-derivative hypotensive agent is a centrally-acting α2-adrenergic agonist. It crosses the blood-brain barrier and acts in the hypothalamus to induce a decrease in blood pressure. It may also be administered as an epidural infusion as an adjunct treatment in the management of severe cancer pain that is not relieved by opiate analgesics alone. Clonidine may be used for differential diagnosis of pheochromocytoma in hypertensive patients. Other uses for clonidine include prophylaxis of vascular migraine headaches, treatment of severe dysmenorrhea, management of vasomotor symptoms associated with menopause, rapid detoxification in the management of opiate withdrawal, treatment of alcohol withdrawal used in conjunction with benzodiazepines, management of nicotine dependence, topical use to reduce intraocular pressure in the treatment of open-angle and secondary glaucoma and hemorrhagic glaucoma associated with hypertension, and in the treatment of attention-deficit hyperactivity disorder (ADHD). Clonidine also exhibits some peripheral activity.

Structure
Thumb
Synonyms
2-[(2,6-Dichlorophenyl)imino]imidazoline
2,6-Dichloro-N-2-imidazolidinylidenebenzenamine
Chlofazoline
Clonidin
Clonidina
Clonidinum
External Identifiers
  • ST 155
  • ST 155-BS
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cataprestablet.1 mg/1oralBoehringer Ingelheim Pharmaceuticals Inc.1999-05-01Not applicableUs
Cataprespatch, extended release.1 mg/24htransdermalRebel Distributors Corp1985-10-01Not applicableUs
Cataprespatch, extended release.3 mg/24htransdermalBoehringer Ingelheim Pharmaceuticals Inc.1985-10-01Not applicableUs
Cataprespatch, extended release.2 mg/24htransdermalBoehringer Ingelheim Pharmaceuticals Inc.1985-10-01Not applicableUs
Cataprespatch, extended release.1 mg/24htransdermalBoehringer Ingelheim Pharmaceuticals Inc.1985-10-01Not applicableUs
Cataprestablet.3 mg/1oralBoehringer Ingelheim Pharmaceuticals Inc.1999-05-01Not applicableUs
Cataprestablet.2 mg/1oralBoehringer Ingelheim Pharmaceuticals Inc.1999-05-01Not applicableUs
Catapres Tab 0.1mgtablet0.1 mgoralBoehringer Ingelheim (Canada) Ltd Ltee1973-12-31Not applicableCanada
Catapres Tab 0.2mgtablet0.2 mgoralBoehringer Ingelheim (Canada) Ltd Ltee1974-12-312015-03-30Canada
Clonidinetablet0.025 mgoralSanis Health Inc2011-02-082012-08-03Canada
Clonidinetablet0.2 mgoralSanis Health Inc2011-02-082012-08-03Canada
Clonidinetablet0.1 mgoralSanis Health Inc2011-02-082012-08-03Canada
Clonidine 0.1tablet0.1 mgoralPro Doc Limitee1991-12-312014-07-24Canada
Clonidine HCl Tab 0.2mgtablet.2 mgoralPro Doc Limitee1991-12-312014-07-24Canada
Clonidine Hydrochloridetablet.3 mg/1oralState of Florida DOH Central Pharmacy2009-06-20Not applicableUs
Clonidine Hydrochloride Extended-releasetablet, extended release.1 mg/1oralConcordia Pharmaceuticals Inc.2010-12-09Not applicableUs
Dixarit Tab 0.025mgtablet0.025 mgoralBoehringer Ingelheim (Canada) Ltd Ltee1981-12-31Not applicableCanada
Dom-clonidinetablet.2 mgoralDominion Pharmacal2003-05-22Not applicableCanada
Dom-clonidinetablet.1 mgoralDominion Pharmacal2003-05-22Not applicableCanada
Duracloninjection, solution.5 mg/mLepiduralMylan Institutional LLC1996-10-02Not applicableUs
Duracloninjection, solution.1 mg/mLepiduralMylan Institutional LLC1996-10-02Not applicableUs
Kapvaytablet, extended release.2 mg/1oralConcordia Pharmaceuticals Inc.2010-12-09Not applicableUs
Kapvaytablet, extended release.1 mg/1oralConcordia Pharmaceuticals Inc.2010-12-09Not applicableUs
Nexiclontablet, extended release.17 mg/1oralTris Pharma, Inc.2010-12-17Not applicableUs
Nexiclon XRtablet, extended release.26 mg/1oralTris Pharma, Inc.2010-12-17Not applicableUs
Nexiclon XRfor suspension, extended release.09 mg/mLoralTris Pharma, Inc.2010-12-17Not applicableUs
Ntp-clonidinetablet0.2 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-clonidinetablet0.1 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-clonidinetablet0.025 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Nu-clonidine Tab 0.1mgtablet.1 mgoralNu Pharm Inc1992-12-312012-09-04Canada
Nu-clonidine Tab 0.2mgtablet.2 mgoralNu Pharm Inc1992-12-312012-09-04Canada
Teva-clonidinetablet0.1 mgoralTeva Canada Limited1993-12-31Not applicableCanada
Teva-clonidinetablet0.2 mgoralTeva Canada Limited1993-12-31Not applicableCanada
Teva-clonidinetablet0.025 mgoralTeva Canada Limited2008-06-26Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-clonidinetablet0.025 mgoralApotex Inc2004-07-13Not applicableCanada
Apo-clonidine Tab 0.1mgtablet.1 mgoralApotex Inc1990-12-31Not applicableCanada
Apo-clonidine Tab 0.2mgtablet.2 mgoralApotex Inc1990-12-31Not applicableCanada
Clonidinepatch.1 mg/dtransdermalMylan Pharmaceuticals Inc.2013-02-08Not applicableUs
Clonidineinjection, solution500 ug/mLepiduralX Gen Pharmaceuticals, Inc.2013-10-29Not applicableUs
Clonidinepatch.3 mg/dtransdermalMylan Pharmaceuticals Inc.2013-02-08Not applicableUs
Clonidinepatch.3 mg/dtransdermalPhysicians Total Care, Inc.2011-05-10Not applicableUs
Clonidinepatch.2 mg/dtransdermalPhysicians Total Care, Inc.2010-12-14Not applicableUs
Clonidinepatch, extended release.3 mg/24htransdermalBarr Laboratories Inc.2010-08-25Not applicableUs
Clonidinepatch, extended release.2 mg/24htransdermalLake Erie Medical DBA Quality Care Products LLC2010-08-25Not applicableUs
Clonidinepatch, extended release.2 mg/24htransdermalBarr Laboratories Inc.2010-08-25Not applicableUs
Clonidinetablet.1 mg/1oralSTAT Rx USA LLC1986-12-16Not applicableUs
Clonidinepatch.2 mg/dtransdermalLake Erie Medical DBA Quality Care Products LLC2013-02-08Not applicableUs
Clonidinepatch, extended release.1 mg/24htransdermalBarr Laboratories Inc.2010-08-25Not applicableUs
Clonidineinjection, solution500 ug/mLepiduralFresenius Kabi USA, LLC2011-07-08Not applicableUs
Clonidineinjection, solution100 ug/mLepiduralX Gen Pharmaceuticals, Inc.2013-10-29Not applicableUs
Clonidinepatch.2 mg/dtransdermalMylan Pharmaceuticals Inc.2013-02-08Not applicableUs
Clonidinepatch.1 mg/dtransdermalPhysicians Total Care, Inc.2011-09-24Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralNorth Star Rx Llc2013-02-04Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralLake Erie Medical DBA Quality Care Products LLC2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralA S Medication Solutions Llc2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralREMEDYREPACK INC.2014-07-18Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralA S Medication Solutions Llc2013-02-04Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralCardinal Health2009-09-03Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralSt Marys Medical Park Pharmacy2010-03-01Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralREMEDYREPACK INC.2015-12-09Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation1995-01-03Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralPreferred Pharmaceuticals, Inc.2015-04-13Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1986-12-16Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralMajor Pharmaceuticals2006-11-20Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralRebel Distributors Corp1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralUnit Dose Services1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralMutual Pharmaceutical Company, Inc.1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralRichmond Pharmaceuticals, Inc.1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralCardinal Health2013-06-17Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralSt Marys Medical Park Pharmacy2014-01-23Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralDIRECT RX2015-01-01Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralTYA Pharmaceuticals2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralMc Kesson Contract Packaging2012-01-10Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralGlobal Pharmaceuticals, Division of Impax Laboratories Inc.2009-12-01Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralBlenheim Pharmacal, Inc.2010-04-08Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralUnichem Pharmaceuticals (USA), Inc.2009-09-21Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralREMEDYREPACK INC.2011-07-29Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralMed Health Pharma, LLC2011-01-10Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralClinical Solutions Wholesale2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralREMEDYREPACK INC.2015-03-07Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralProficient Rx LP1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralBlue Point Laboratories2014-03-03Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralActavis Elizabeth LLC1995-01-03Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralNorth Star Rx Llc2013-02-04Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralLake Erie Medical DBA Quality Care Products LLC1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralA S Medication Solutions Llc2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralREMEDYREPACK INC.2013-08-28Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralA S Medication Solutions Llc2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralCardinal Health2011-07-08Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralAmerican Health Packaging2015-10-01Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralREMEDYREPACK INC.2015-11-12Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralbryant ranch prepack2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralPreferred Pharmaceuticals, Inc.2011-11-10Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralMylan Pharmaceuticals Inc.1987-06-09Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1986-12-16Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralBlenheim Pharmacal, Inc.2011-04-01Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralUnichem Pharmaceuticals (USA), Inc.2009-09-21Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralREMEDYREPACK INC.2011-03-28Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralMed Health Pharma, LLC2011-01-10Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralClinical Solutions Wholesale, Llc2009-09-21Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralREMEDYREPACK INC.2015-06-16Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralAmerican Health Packaging2013-05-20Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralContract Pharmacy Services Pa2010-07-29Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralAvera Mc Kennan Hospital2015-03-05Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralActavis Elizabeth LLC1995-01-03Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralSTAT Rx USA LLC2009-09-03Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralA S Medication Solutions Llc2013-06-17Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralREMEDYREPACK INC.2013-06-09Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralA S Medication Solutions Llc2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralCardinal Health2011-07-08Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralAmerican Health Packaging2015-10-01Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralREMEDYREPACK INC.2015-09-17Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralbryant ranch prepack1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralPreferred Pharmaceuticals, Inc2011-11-10Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralMylan Pharmaceuticals Inc.1987-06-09Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralQualitest Pharmaceuticals2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralREMEDYREPACK INC.2013-02-26Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralPd Rx Pharmaceuticals, Inc.1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralMed Health Pharma, LLC2011-01-10Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralPhysicians Total Care, Inc.2004-11-30Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralClinical Solutions Wholesale, Llc2009-09-21Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralREMEDYREPACK INC.2014-11-03Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralAmerican Health Packaging2013-05-20Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralContract Pharmacy Services Pa2010-08-18Not applicableUs
Clonidine Hydrochlorideinjection, solution100 ug/mLintravenousWest ward Pharmaceutical Corp2011-01-01Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralA S Medication Solutions Llc2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralREMEDYREPACK INC.2013-03-18Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralCardinal Health2011-07-08Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralAmerican Health Packaging2015-10-01Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralREMEDYREPACK INC.2015-08-31Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralbryant ranch prepack1995-01-03Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralPreferred Pharmaceuticals, Inc2011-11-10Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralMylan Pharmaceuticals Inc.1987-06-09Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralQualitest Pharmaceuticals2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralREMEDYREPACK INC.2011-04-04Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralPd Rx Pharmaceuticals, Inc.2009-09-03Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralMylan Institutional Inc.1995-06-12Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralPhysicians Total Care, Inc.1995-01-09Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralCarlsbad Technology, Inc2013-06-17Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralAmerican Health Packaging2013-05-20Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralDispensing Solutions, Inc.2007-03-09Not applicableUs
Clonidine Hydrochlorideinjection, solution500 ug/mLintravenousWest ward Pharmaceutical Corp2011-01-01Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralApotheca, Inc1996-12-21Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralAidarex Pharmaceuticals LLC2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-05-19Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralREMEDYREPACK INC.2012-08-20Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralCardinal Health2006-11-20Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralREMEDYREPACK INC.2015-07-30Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralREMEDYREPACK INC.2016-04-11Not applicableUs
Clonidine Hydrochloridetablet, extended release.2 mg/1oralActavis Pharma, Inc.2015-06-17Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralQualitest Pharmaceuticals2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralMajor Pharmaceuticals2006-11-20Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralRebel Distributors Corp1987-09-04Not applicableUs
Clonidine Hydrochlorideinjection, solution500 ug/mLepiduralPharma Force, Inc.2009-10-16Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralMylan Institutional Inc.1995-06-12Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralMutual Pharmaceutical Company, Inc.1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralPhysicians Total Care, Inc.2001-10-03Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralPd Rx Pharmaceuticals, Inc.2009-09-03Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralCarlsbad Technology, Inc2013-06-17Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralDIRECT RX2015-01-01Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralMed Vantx, Inc.2011-12-13Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralGlobal Pharmaceuticals, Division of Impax Laboratories Inc.2009-12-01Not applicableUs
Clonidine Hydrochlorideinjection, solution500 ug/mLepiduralAmerican Regent, Inc.2010-04-15Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralAidarex Pharmaceuticals LLC1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralREMEDYREPACK INC.2011-08-05Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralNorthwind Pharmaceuticals, LLC2014-09-24Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralState of Florida DOH Central Pharmacy2014-01-01Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralDispensing Solutions, Inc.2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralClinical Solutions Wholesale2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralREMEDYREPACK INC.2015-07-17Not applicableUs
Clonidine Hydrochlorideinjection, solution100 ug/mLepiduralFresenius Kabi USA, LLC2011-07-08Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralBlue Point Laboratories2014-03-03Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralPd Rx Pharmaceuticals, Inc.2009-09-03Not applicableUs
Clonidine Hydrochloridetablet, extended release.1 mg/1oralActavis Pharma, Inc.2015-06-17Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralNorth Star Rx Llc2013-02-04Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralUnit Dose Services2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralGeneral Injectables & Vaccines, Inc2010-03-01Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralRichmond Pharmaceuticals, Inc.1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralCardinal Health2009-09-03Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralSt Marys Medical Park Pharmacy2014-01-23Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralDIRECT RX2014-01-01Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralTYA Pharmaceuticals1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralPreferred Pharmaceuticals, Inc.2014-10-22Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1986-12-16Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralMajor Pharmaceuticals2006-11-20Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralRebel Distributors Corp1987-09-04Not applicableUs
Clonidine Hydrochlorideinjection, solution100 ug/mLepiduralPharma Force, Inc.2009-10-16Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralMylan Institutional Inc.1997-02-14Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralMutual Pharmaceutical Company, Inc.1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralRichmond Pharmaceuticals, Inc.1987-09-04Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralPd Rx Pharmaceuticals, Inc.2009-09-03Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralCarlsbad Technology, Inc2013-06-17Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralDIRECT RX2015-12-29Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralMed Vantx, Inc.1995-01-03Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralMc Kesson Contract Packaging2011-10-03Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralGlobal Pharmaceuticals, Division of Impax Laboratories Inc.2009-12-01Not applicableUs
Clonidine Hydrochlorideinjection, solution100 ug/mLepiduralAmerican Regent, Inc.2010-04-15Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralUnichem Pharmaceuticals (USA), Inc.2009-09-21Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralREMEDYREPACK INC.2011-08-01Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralNorthwind Pharmaceuticals, LLC2015-02-25Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralClinical Solutions Wholesale2007-03-09Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralREMEDYREPACK INC.2015-03-20Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralProficient Rx LP2009-09-21Not applicableUs
Clonidine Hydrochloridetablet.2 mg/1oralBlue Point Laboratories2014-03-03Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralUnit Dose Services1995-01-03Not applicableUs
Clonidine Hydrochloridetablet.3 mg/1oralActavis Elizabeth LLC1995-01-03Not applicableUs
Clonidine Hydrochloridetablet.1 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Clonidine Hydrochloride Extended-releasetablet, extended release.2 mg/1oralPar Pharmaceutical2013-09-30Not applicableUs
Clonidine Hydrochloride Extended-releasetablet, extended release.1 mg/1oralPar Pharmaceutical2013-09-30Not applicableUs
Clonidine Hydrochloride Extended-releasetablet, extended release.1 mg/1oralGolden State Medical Supply, Inc.2015-09-30Not applicableUs
Clonidine Hydrochloride Extended-releasetablet, extended release.1 mg/1oralAmerican Health Packaging2014-10-27Not applicableUs
Clonidine Transdermal Systempatch.1 mg/dtransdermalActavis Pharma, Inc.2014-05-06Not applicableUs
Clonidine Transdermal Systempatch.3 mg/dtransdermalActavis Pharma, Inc.2014-05-06Not applicableUs
Clonidine Transdermal Systempatch.2 mg/dtransdermalActavis Pharma, Inc.2014-05-06Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
Catapres-TTSBoehringer Ingelheim
CatapresanBoehringer Ingelheim
CatapressanBoehringer Ingelheim
DixaritBoehringer Ingelheim
IsoglauconAgepha
Run RuiBausch & Lomb
VelarilRoemmers
WinpressWinston
Brand mixtures
NameLabellerIngredients
ClorpresMylan Pharmaceuticals Inc.
Combipres 0.1/15 TabBoehringer Ingelheim (Canada) Ltd Ltee
Salts
Name/CASStructureProperties
Clonidine Hydrochloride
4205-91-8
Thumb
  • InChI Key: ZNIFSRGNXRYGHF-UHFFFAOYSA-N
  • Monoisotopic Mass: 264.994030456
  • Average Mass: 266.555
DBSALT000538
Categories
UNIIMN3L5RMN02
CAS number4205-90-7
WeightAverage: 230.094
Monoisotopic: 229.017352717
Chemical FormulaC9H9Cl2N3
InChI KeyInChIKey=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
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassHalobenzenes
Direct ParentDichlorobenzenes
Alternative Parents
Substituents
  • 1,3-dichlorobenzene
  • Aryl halide
  • Aryl chloride
  • 2-imidazoline
  • Guanidine
  • Azacycle
  • Organoheterocyclic compound
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Carboximidamide
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationMay be used as an adjunct in the treatment of hypertension, as an epidural infusion as an adjunct treatment in the management of severe cancer pain that is not relieved by opiate analgesics alone, for differential diagnosis of pheochromocytoma in hypertensive patients, prophylaxis of vascular migraine headaches, treatment of severe dysmenorrhea, management of vasomotor symptoms associated with menopause, rapid detoxification in the management of opiate withdrawal, treatment of alcohol withdrawal used in conjunction with benzodiazepines, management of nicotine dependence, topical use to reduce intraocular pressure in the treatment of open-angle and secondary glaucoma and hemorrhagic glaucoma associated with hypertension, and in the treatment of attention-deficit hyperactivity disorder (ADHD).
PharmacodynamicsClonidine is an α-adrenergic agent that acts specifically on α2-receptors. α2-receptors regulate a number of signaling pathways mediated by multiple Gi proteins, Gαi1, Gαi2, and G&alphai3. Stimulation of α2-receptors mediates effects such as inhibition of adenylyl cyclase, stimulation fo phospholipase D, stimulation of mitogen-activated protein kinases, stimulation of K+ currents and inhibition of Ca2+ currents. Three G-protein coupled α2-receptor subtypes have been identified: α2A, α2B, and α2C. Each subtype has a unique pattern of tissue distribution in the central nervous system and peripheral tissues. The α2A-receptor is widely distributed throughout the central nervous system; it is found in the locus coeruleus, brain stem nuclei, cerebral cortex, septum, hypothalamus, and hippocampus. α2A-receptors are also expressed in the kidneys, spleen, thymus, lung and salivary glands. The α2C-receptor is primarily expressed in the central nervous system, including the striatum, olfactory tubercle, hippocampus and cerebral cortex. Low levels of the α2C-subtype are also found in the kidneys. The α2B-receptor is located primarily in the periphery (kidney, liver, lung and heart) with low levels of expression in the thalamic nuclei of the central nervous system. The α2A- and α2C-receptors are located presynaptically and inhibit the released of noradrenaline from sympathetic nerves. Stimulation of these receptors decreases sympathetic tone, resulting in decreases in blood pressure and heart rate. Sedation and analgesia is mediated by centrally located α2A-receptors, while peripheral α2B-receptors mediate constriction of vascular smooth muscle. α2A-Receptors also mediate essential components of the analgesic effect of nitrous oxide in the spinal cord. Clonidine stimulates all three α2-receptor subtypes with similar potency. Its actions in the nervous system decreases blood pressure in patients with hypertension and decreases sympathetic overactivity in patients undergoing opioid withdrawal. Clonidine is also a potent sedative and analgesic and can prevent post-operative shivering in intensive and post-operative care. Its use in differential diagnosis of pheochromocytoma owes to the fact that hypertension in patients with pheochromocytoma is refractory to antihypertensive treatment with clonidine.
Mechanism of actionSee Pharmacology section above.
Related Articles
AbsorptionWell absorbed following oral administration. Bioavailability following chronic administration is approximately 65%.
Volume of distributionNot Available
Protein binding20-40%, primarily to albumin
Metabolism

Hepatic. Metabolized via minor pathways. The major metabolite, p-hydroxyclonidine, is present in concentrations less than 10% of those of unchanged clonidine in urine. Four metabolites have been detected, but only p-hydroxyclonidine has been identified.

SubstrateEnzymesProduct
Clonidine
4-HydroxyclonidineDetails
Route of eliminationNot Available
Half life6-20 hours; 40-60% is excreted in urine unchanged, 20% is excreted in feces. Less than 10% is excreted by p-hydroxyclonidine.
ClearanceNot Available
ToxicityOral LD50 is 150 mg/kg in rat and 30 mg/kg in dog. Symptoms of overdose include constriction of pupils of the eye, drowsiness, high blood pressure followed by a drop in pressure, irritability, low body temperature, slowed breathing, slowed heartbeat, slowed reflexes, and weakness.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
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
Dosage forms
FormRouteStrength
Tabletoral.1 mg
Tabletoral.2 mg
Patchtransdermal.1 mg/d
Patchtransdermal.2 mg/d
Patchtransdermal.3 mg/d
Patch, extended releasetransdermal.1 mg/24h
Patch, extended releasetransdermal.2 mg/24h
Patch, extended releasetransdermal.3 mg/24h
Injection, solutionepidural100 ug/mL
Injection, solutionepidural500 ug/mL
Injection, solutionintravenous100 ug/mL
Injection, solutionintravenous500 ug/mL
Tabletoral.1 mg/1
Tabletoral.2 mg/1
Tabletoral.3 mg/1
Tablet, extended releaseoral.1 mg/1
Tablet, extended releaseoral.2 mg/1
Tabletoral
Tabletoral0.025 mg
Injection, solutionepidural.1 mg/mL
Injection, solutionepidural.5 mg/mL
Tablet, extended releaseoral.17 mg/1
For suspension, extended releaseoral.09 mg/mL
Tablet, extended releaseoral.26 mg/1
Tabletoral0.1 mg
Tabletoral0.2 mg
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)
US5869100 No1993-10-132013-10-13Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point3053,202,660
water solubilityAppreciableNot Available
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 RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-003r-5970000000-33c27878b8b7ad9d5d75View in MoNA
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. Schapiro NA: "Dude, you don't have Tourette's:" Tourette's syndrome, beyond the tics. Pediatr Nurs. 2002 May-Jun;28(3):243-6, 249-53. [PubMed:12087644 ]
  2. 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 ]
External Links
ATC CodesC02AC01C02LC01C02LC51N02CX02S01EA04
AHFS Codes
  • 24:08.16
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (73.8 KB)
Interactions
Drug Interactions
Drug
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Clonidine.
AlfuzosinAlfuzosin may increase the hypotensive activities of Clonidine.
AmifostineClonidine may increase the hypotensive activities of Amifostine.
AmitriptylineAmitriptyline may decrease the antihypertensive activities of Clonidine.
AzelastineClonidine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Clonidine.
BepridilClonidine may increase the atrioventricular blocking (AV block) activities of Bepridil.
BretyliumBretylium may increase the bradycardic activities of Clonidine.
BrimonidineBrimonidine may increase the antihypertensive activities of Clonidine.
BuprenorphineClonidine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ButabarbitalButabarbital may increase the hypotensive activities of Clonidine.
ButethalButethal may increase the hypotensive activities of Clonidine.
CeritinibClonidine may increase the bradycardic activities of Ceritinib.
DiazoxideDiazoxide may increase the hypotensive activities of Clonidine.
DigoxinClonidine may increase the atrioventricular blocking (AV block) activities of Digoxin.
DiltiazemClonidine may increase the atrioventricular blocking (AV block) activities of Diltiazem.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Clonidine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Clonidine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Clonidine.
DuloxetineClonidine may increase the orthostatic hypotensive activities of Duloxetine.
EsmololEsmolol may increase the bradycardic activities of Clonidine.
EthanolClonidine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
HeptabarbitalHeptabarbital may increase the hypotensive activities of Clonidine.
HexobarbitalHexobarbital may increase the hypotensive activities of Clonidine.
HydrocodoneClonidine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Clonidine.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Clonidine.
IvabradineClonidine may increase the bradycardic activities of Ivabradine.
LacosamideClonidine may increase the atrioventricular blocking (AV block) activities of Lacosamide.
LevodopaClonidine may increase the orthostatic hypotensive activities of Levodopa.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Clonidine.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Clonidine.
MethohexitalMethohexital may increase the hypotensive activities of Clonidine.
MethotrimeprazineClonidine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethylphenidateThe risk or severity of adverse effects can be increased when Methylphenidate is combined with Clonidine.
MetyrosineClonidine may increase the sedative activities of Metyrosine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Clonidine.
MirtazapineMirtazapine may decrease the antihypertensive activities of Clonidine.
MolsidomineMolsidomine may increase the hypotensive activities of Clonidine.
MoxonidineMoxonidine may increase the hypotensive activities of Clonidine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Clonidine.
NadololClonidine may increase the atrioventricular blocking (AV block) activities of Nadolol.
NicorandilNicorandil may increase the hypotensive activities of Clonidine.
ObinutuzumabClonidine may increase the hypotensive activities of Obinutuzumab.
OctreotideOctreotide may increase the bradycardic activities of Clonidine.
OrphenadrineClonidine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeClonidine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Clonidine is combined with Paroxetine.
PentobarbitalPentobarbital may increase the hypotensive activities of Clonidine.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Clonidine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Clonidine.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Clonidine.
PramipexoleClonidine may increase the sedative activities of Pramipexole.
PrimidonePrimidone may increase the hypotensive activities of Clonidine.
QuinineQuinine may increase the hypotensive activities of Clonidine.
RisperidoneClonidine may increase the hypotensive activities of Risperidone.
RituximabClonidine may increase the hypotensive activities of Rituximab.
RopiniroleClonidine may increase the sedative activities of Ropinirole.
RotigotineClonidine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Clonidine.
RuxolitinibRuxolitinib may increase the bradycardic activities of Clonidine.
SecobarbitalSecobarbital may increase the hypotensive activities of Clonidine.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Clonidine.
SuvorexantClonidine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TadalafilTadalafil may increase the antihypertensive activities of Clonidine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Clonidine.
ThalidomideClonidine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TofacitinibTofacitinib may increase the bradycardic activities of Clonidine.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Clonidine.
TreprostinilTreprostinil may increase the hypotensive activities of Clonidine.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Clonidine.
VardenafilVardenafil may increase the antihypertensive activities of Clonidine.
VenlafaxineVenlafaxine may decrease the antihypertensive activities of Clonidine.
VerapamilClonidine may increase the atrioventricular blocking (AV block) activities of Verapamil.
YohimbineYohimbine may decrease the antihypertensive activities of Clonidine.
ZolpidemClonidine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
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 oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
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. Hein, L. (2004). alpha-Adrenergic system. In Encyclopedic reference of molecular pharmacology (pp. 27-30). Berlin: Springer. [ISBN:9783540298328 ]
Kind
Protein
Organism
Human
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 > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 Da
References
  1. Hein, L. (2004). alpha-Adrenergic system. In Encyclopedic reference of molecular pharmacology (pp. 27-30). Berlin: Springer. [ISBN:9783540298328 ]
Kind
Protein
Organism
Human
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
Molecular Weight:
49521.585 Da
References
  1. Hein, L. (2004). alpha-Adrenergic system. In Encyclopedic reference of molecular pharmacology (pp. 27-30). Berlin: Springer. [ISBN:9783540298328 ]
Kind
Protein
Organism
Human
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) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
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) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
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
Molecular Weight:
60462.205 Da
References
  1. PDSP Ki Database [Link]

Enzymes

Kind
Protein
Organism
Human
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
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
Human
Pharmacological action
unknown
Actions
substrate
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
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
Human
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
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
Human
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
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
Human
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
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 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Secondary active organic cation transmembrane transporter activity
Specific Function:
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. Bednarczyk D, Ekins S, Wikel JH, Wright SH: Influence of molecular structure on substrate binding to the human organic cation transporter, hOCT1. Mol Pharmacol. 2003 Mar;63(3):489-98. [PubMed:12606755 ]
  2. Zhang L, Dresser MJ, Gray AT, Yost SC, Terashita S, Giacomini KM: Cloning and functional expression of a human liver organic cation transporter. Mol Pharmacol. 1997 Jun;51(6):913-21. [PubMed:9187257 ]
  3. Zhang L, Schaner ME, Giacomini KM: Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). J Pharmacol Exp Ther. 1998 Jul;286(1):354-61. [PubMed:9655880 ]
  4. Martel F, Vetter T, Russ H, Grundemann D, Azevedo I, Koepsell H, Schomig E: Transport of small organic cations in the rat liver. The role of the organic cation transporter OCT1. Naunyn Schmiedebergs Arch Pharmacol. 1996 Aug-Sep;354(3):320-6. [PubMed:8878062 ]
Kind
Protein
Organism
Human
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
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
Human
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 cations such as tetraethylammonium (TEA) without the involvement of sodium. Also relative uptake activity ratio of carnitine to TEA is 11.3.
Gene Name:
SLC22A5
Uniprot ID:
O76082
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
Human
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 the involvement of sodium. Relative uptake activity ratio of carnitine to TEA is 1.78. A key substrate of this transporter seems to be ergothioneine (ET).
Gene Name:
SLC22A4
Uniprot ID:
Q9H015
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
Human
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
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 ]
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Drug created on June 13, 2005 07:24 / Updated on April 21, 2016 13:15