Drug/Small Molecule:
clonidine

2D structure

Overview

Generic Names: Chlornidinum; Clonidin; Clonidine HCl; Clonidinhydrochlorid; Clonidinum [INN-Latin]; ST 155BS
Trade Names: Adesipress; Catapres; Catapres-TTS; Catapresan; Catapressan; Catarpres; Catarpresan; Clonistada; Dixarit; Duraclon; Duraclont; Ipotensium; Isoglaucon; Tenso-Timelets
Brand Mixtures: Combipres 0.1/15 Tab (Chlorthalidone + Clonidine Hydrochloride)
PharmGKB Accession Id: PA449051

Description

An alpha-2 adrenergic agonist that crosses the blood-brain barrier. Clonidine acts centrally by reducing sympathetic tone, resulting in a fall in diastolic and systolic blood pressure and a reduction in heart rate. It also acts peripherally, and this peripheral activity may be responsible for the transient increase in blood pressure seen during rapid intravenous administration. (From Martindale, the Extra Pharmacopoeia, 30th ed, p350) (source: Drug Bank)

Indication

For the treatment of hypertension and maybe used in prophylaxis of migraine or recurrent vascular headache; Menopausal flushing (source: Drug Bank)

ATC Therapeutic Categories

  • C02AC:Imidazoline receptor agonists
  • N02CX:Other antimigraine preparations
  • S01EA:Sympathomimetics in glaucoma therapy

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Clonidine acts as an agonist at presynaptic alpha(2)-receptors in the nucleus tractus solitarius of the medulla oblongata. Stimulation of these receptors results in the supression of efferent sympathetic pathways and the subsequent decrease in blood pressure and vascular tone in the heart, kidneys, and peripheral vasculature. Clonidine is also a partial agonist at presynaptic alpha(2)-adrenergic receptors of peripheral nerves in vascular smooth muscle. (source: Drug Bank)

Pharmacology

Clonidine is an antihypertensive agent and an epidural agent for refractory cancer pain. Similar to guanabenz in mechanism of action, clonidine is used in the treatment of hypertension, opiate and nicotine withdrawal, vascular headaches, diabetic diarrhea, glaucoma, ulcerative colitis, Gilles de la Tourette's syndrome, menopause symptoms, severe pain in cancer patients refractory to opiate agonists, and neuropathic pain and in the diagnosis of pheochromocytoma. (source: Drug Bank)

Food Interactions

Avoid alcohol.
Take without regard to meals. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. Metabolized through minor pathways. The major metabolite, p-hydroxyclonidine, is present in concentrations less than 10% of those of unchanged clonidine in urine. (source: Drug Bank)

Protein Binding

20-40% (source: Drug Bank)

Absorption

Well absorbed following oral administration. Bioavailability following chronic administration is approximately 65%. (source: Drug Bank)

Toxicity

Oral 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. (source: Drug Bank)

Isomeric SMILES Code:

c1cc(c(c(c1)Cl)N=C2NCCN2)Cl (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
No phenotype data Genotype Data Available Literature annotations available Not annotated
ADRA2A
  •   
  • PD
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
GNB3
  •   
  • PD
  •   
  •   
  • GN
Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
ADRA2A Uncurated Annotation (source: Drug Bank)
TACR2 Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
acebutolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
amitriptyline Uncurated Annotation The tricyclic decreases the effect of clonidine (source: Drug Bank)
amoxapine Uncurated Annotation The tricyclic decreases the effect of clonidine (source: Drug Bank)
atenolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
betaxolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
bevantolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
bisoprolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
carteolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
carvedilol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
clomipramine Uncurated Annotation The tricyclic decreases the effect of clonidine (source: Drug Bank)
desipramine Uncurated Annotation The tricyclic decreases the effect of clonidine (source: Drug Bank)
doxepin Uncurated Annotation The tricyclic decreases the effect of clonidine (source: Drug Bank)
esmolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
imipramine Uncurated Annotation The tricyclic decreases the effect of clonidine (source: Drug Bank)
labetalol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
metoprolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
mirtazapine Uncurated Annotation Possible hypertensive crisis (source: Drug Bank)
nadolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
nortriptyline Uncurated Annotation The tricyclic decreases the effect of clonidine (source: Drug Bank)
oxprenolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
penbutolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
pindolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
practolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
propranolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
protriptyline Uncurated Annotation The tricyclic decreases the effect of clonidine (source: Drug Bank)
sotalol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
timolol Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
trimipramine Uncurated Annotation The tricyclic decreases the effect of clonidine (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
diabetes mellitus type 2 and obesity
  •   
  • PD
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Diabetes Mellitus, Type 2
  •   
  • PD
  •   
  • FA
  •   
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00575
KEGG Drug ID:
D00281
PubChem Compound ID:
2803
PubChem Substance ID:
163008
IUPHAR Ligand ID:
516

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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