Investigational Drug Details
| Drug ID: | D162 |
| Drug Name: | Clonidine |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00575 |
| DrugBank Description: | Clonidine is an imidazole derivate that acts as an agonist of alpha-2 adrenoceptors.[A180559] This activity is useful for the treatment of hypertension, severe pain, and ADHD.[L7237,L7240,L7243,L7246] Clonidine was granted FDA approval on 3 September 1974.[L7237] |
| PubChem ID: | 2803 |
| CasNo: | 4205-90-7 |
| Repositioning for NAFLD: | Yes |
| SMILES: | ClC1=CC=CC(Cl)=C1NC1=NCCN1 |
| Structure: |
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| InChiKey: | GJSURZIOUXUGAL-UHFFFAOYSA-N |
| Molecular Weight: | 230.094 |
| DrugBank Targets: | Alpha-2B adrenergic receptor; Alpha-2C adrenergic receptor; Alpha-2A adrenergic receptor; Alpha-1A adrenergic receptor; Alpha-1B adrenergic receptor; Alpha-1D adrenergic receptor |
| DrugBank MoA: | Clonidine is primarily an alpha-2 adrenoceptor agonist which causes central hypotensive and anti-arrhythmogenic effects.[A180559] The alpha-2 adrenoceptor is coupled to the G-proteins G<sub>o</sub> and G<sub>i</sub>.[A180559] G<sub>i</sub> inhibits adenylyl cyclase and activates opening of a potassium channel that causes hyperpolarization.[A180559] Clonidine binding to the alpha-2 adrenoceptor causes structural changes in the alpha subunit of the G-protein, reducing its affinity for GDP.[A180559] Magnesium catalyzes the replacement of GDP with GTP.[A180559] The alpha subunit dissociates from the other subunits and associates with an effector.[A180559] 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.[A180559] Clonidine can also decrease transmission of pain signals at the spine.[A180559] Finally clonidine can affect regulators of blood pressure in the ventromedial and rostral-ventrolateral areas of the medulla.[A180559] |
| DrugBank Pharmacology: | Clonidine functions through agonism of alpha-2 adrenoceptors which have effects such as lowering blood pressure, sedation, and hyperpolarization of nerves.[A180559] 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.[L7237,L7240,L7243,L7246] |
| DrugBank Indication: | Clonidine tablets and transdermal systems are indicated for the treatment of hypertension alone or in combination with other medications.[L7237,L7240] A clonidine injection is indicated for use with opiates in the treatment of severe cancer pain where opiates alone are insufficient.[L7243] An extended release tablet of clonidine is indicated for the treatment of ADHD either alone or in combination with other medications.[L7246] Clonidine is also used for the diagnosis of pheochromocytoma,[A180565] treatment of nicotine dependance,[A180568] and opiate withdrawal.[A180571] |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L1688 | NCT00440557 | PHASE3 | COMPLETED | YES | 2006-09 | 2014-05-07 | Details |
| L1880 | NCT00700960 | COMPLETED | NO | 2007-06 | 2017-01-31 | Details | |
| L5500 | NCT02960659 | PHASE1|PHASE2 | COMPLETED | YES | 2017-05-09 | 2023-08-01 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Article ID | PMID | Source | Title |
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