Chemical: Drug
clonidine

PharmGKB contains no dosing guidelines for this . To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.



PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all variant annotations for clonidine

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA
rs11269124 NC_000004.11:g.3769789_3769790insGGGAGCTTTCCCAGAGACCC, NC_000004.11:g.3769789_3769790insGGGGAGCTTTCCCAGAGACCC, NC_000004.12:g.3768062_3768063insGGGAGCTTTCCCAGAGACCC, NC_000004.12:g.3768062_3768063insGGGGAGCTTTCCCAGAGACCC, NG_012640.1:g.6494_6495insGGGAGCTTTCCCAGAGACCC, NG_012640.1:g.6494_6495insGGGGAGCTTTCCCAGAGACCC, NM_000683.3:c.*67_*68insGGGAGCTTTCCCAGAGACCC, NM_000683.3:c.*67_*68insGGGGAGCTTTCCCAGAGACCC, rs147319738
- > GGGAGCTTTCCCAGAGACCC
- > GGGGAGCTTTCCCAGAGACCC
indel
No VIP available No Clinical Annotations available VA
rs1800544 NC_000010.10:g.112836503G>C, NC_000010.11:g.111076745G>C, NG_012020.1:g.4714G>C, NM_000681.3:c.-1252G>C
G > C
SNP
No VIP available No Clinical Annotations available VA
rs29000568 NC_000002.11:g.96780995_96780996insTCCTCCTCT, NC_000002.12:g.96115256_96115257insTCCTCCTCT, NG_032950.1:g.5893_5894insAGAGGAGGA, NM_000682.6:c.893_894insAGAGGAGGA, NP_000673.2:p.Glu309_Cys310insGluGluGlu, XM_005263890.1:c.893_894insAGAGGAGGA, XM_005263891.1:c.646+247_646+248insAGAGGAGGA, XP_005263947.1:p.Glu306_Cys307insGluGluGlu
- > TCCTCCTCT
indel
No VIP available CA VA
rs5443 NC_000012.11:g.6954875C>T, NC_000012.12:g.6845711C>T, NG_009100.1:g.10501C>T, NM_001297571.1:c.822C>T, NM_002075.3:c.825C>T, NP_001284500.1:p.Ser274=, NP_002066.1:p.Ser275=, NW_003871083.2:g.47295C>T, XM_005253679.1:c.825C>T, XM_005253680.1:c.822C>T, XM_005253681.1:c.702-6C>T, XM_005277751.1:c.825C>T, XM_005277752.1:c.822C>T, XM_005277753.1:c.702-6C>T, XM_011520953.1:c.825C>T, XM_011520954.1:c.822C>T, XM_011521027.1:c.*1818G>A, XM_011521028.1:c.*1818G>A, XM_011521029.1:c.*2036G>A, XM_011521030.1:c.*1969G>A, XP_005253736.1:p.Ser275=, XP_005253737.1:p.Ser274=, XP_005277808.1:p.Ser275=, XP_005277809.1:p.Ser274=, XP_011519255.1:p.Ser275=, XP_011519256.1:p.Ser274=, rs2230334, rs3138516, rs57419337, rs6489738
C > T
SNP
S274S
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

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 Mixture Names
  • Combipres 0.1/15 Tab (Chlorthalidone + Clonidine Hydrochloride)

PharmGKB Accession Id

PA449051

Type(s):

Drug

Description

Clonidine, an imidazoline-derivative hypotensive agent is a centrally-acting alpha 2-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.

Source: Drug Bank

Indication

May 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).

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

See Pharmacology section above.

Source: Drug Bank

Pharmacology

Clonidine is an alpha-adrenergic agent that acts specifically on alpha 2-receptors. alpha 2-receptors regulate a number of signaling pathways mediated by multiple G i proteins, Galpha i1, Galpha i2, and G&alpha i3. Stimulation of alpha 2-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 Ca 2+ currents. Three G-protein coupled alpha 2-receptor subtypes have been identified: alpha 2A, alpha 2B, and alpha 2C. Each subtype has a unique pattern of tissue distribution in the central nervous system and peripheral tissues. The alpha 2A-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. alpha 2A-receptors are also expressed in the kidneys, spleen, thymus, lung and salivary glands. The alpha 2C-receptor is primarily expressed in the central nervous system, including the striatum, olfactory tubercle, hippocampus and cerebral cortex. Low levels of the alpha 2C-subtype are also found in the kidneys. The alpha 2Breceptor 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 alpha 2A and alpha 2C-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 alpha 2A-receptors, while peripheral alpha 2B-receptors mediate constriction of vascular smooth muscle. alpha 2A-Receptors also mediate essential components of the analgesic effect of nitrous oxide in the spinal cord. Clonidine stimulates all three alpha 2-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.

Source: Drug Bank

Food Interaction

Avoid alcohol.|Take without regard to meals.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

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.

Source: Drug Bank

Protein Binding

20-40%, primarily to albumin

Source: Drug Bank

Absorption

Well absorbed following oral administration. Bioavailability following chronic administration is approximately 65%.

Source: Drug Bank

Half-Life

6-20 hours; 40-60% is excreted in urine unchanged, 20% is excreted in feces. Less than 10% is excreted by p-hydroxyclonidine.

Source: Drug Bank

Toxicity

Oral LD 50 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

Chemical Properties

Chemical Formula

C9H9Cl2N3

Source: Drug Bank

Isomeric SMILES

c1cc(c(c(c1)Cl)N=C2NCCN2)Cl

Source: OpenEye

Canonical SMILES

ClC1=CC=CC(Cl)=C1NC1=NCCN1

Source: Drug Bank

Average Molecular Weight

230.094

Source: Drug Bank

Monoisotopic Molecular Weight

229.017352717

Source: Drug Bank

SMILES

ClC1=CC=CC(Cl)=C1NC1=NCCN1

Source: Drug Bank

InChI String

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)

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Sympathetic Nerve Pathway (Neuroeffector Junction)
    Simplified diagram of a sympathetic neuroeffector junction displaying genes which may be involved.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ADRA2A (source: Drug Bank )
ADRA2B (source: Drug Bank )
ADRA2C (source: Drug Bank )
TACR2 (source: Drug Bank )

Drug Interactions

Interaction Description
acebutolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
acebutolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
amitriptyline - clonidine The tricyclic decreases the effect of clonidine (source: Drug Bank )
amitriptyline - clonidine The tricyclic antidepressant, amitriptyline, decreases the effect of clonidine. (source: Drug Bank )
amoxapine - clonidine The tricyclic decreases the effect of clonidine (source: Drug Bank )
amoxapine - clonidine The tricyclic antidepressant, amoxapine, decreases the effect of clonidine. (source: Drug Bank )
atenolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
atenolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
bisoprolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
bisoprolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
carvedilol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
carvedilol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
clomipramine - clonidine The tricycli decreases the effect of clonidine (source: Drug Bank )
clomipramine - clonidine The tricycli decreases the effect of clonidine (source: Drug Bank )
clonidine - acebutolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - acebutolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - amitriptyline The tricyclic decreases the effect of clonidine (source: Drug Bank )
clonidine - amitriptyline The tricyclic antidepressant, amitriptyline, decreases the effect of clonidine. (source: Drug Bank )
clonidine - amoxapine The tricyclic decreases the effect of clonidine (source: Drug Bank )
clonidine - amoxapine The tricyclic antidepressant, amoxapine, decreases the effect of clonidine. (source: Drug Bank )
clonidine - atenolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - atenolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - betaxolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - betaxolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - bevantolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - bevantolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - bisoprolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - bisoprolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - carteolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - carteolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - carvedilol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - carvedilol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - clomipramine The tricyclic decreases the effect of clonidine (source: Drug Bank )
clonidine - clomipramine The tricyclic antidepressant, clomipramine, decreases the effect of clonidine. (source: Drug Bank )
clonidine - desipramine The tricyclic decreases the effect of clonidine (source: Drug Bank )
clonidine - desipramine The tricyclic antidepressant, desipramine, decreases the effect of clonidine. (source: Drug Bank )
clonidine - doxepin The tricyclic decreases the effect of clonidine (source: Drug Bank )
clonidine - doxepin The tricyclic antidepressant, doxepin, decreases the effect of clonidine. (source: Drug Bank )
clonidine - esmolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - esmolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - imipramine The tricyclic decreases the effect of clonidine (source: Drug Bank )
clonidine - imipramine The tricyclic antidepressant, imipramine, decreases the effect of clonidine. (source: Drug Bank )
clonidine - labetalol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - labetalol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - metoprolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - metoprolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - mirtazapine Possible hypertensive crisis (source: Drug Bank )
clonidine - mirtazapine Possible hypertensive crisis (source: Drug Bank )
clonidine - nadolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - nadolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - nortriptyline The tricyclic decreases the effect of clonidine (source: Drug Bank )
clonidine - nortriptyline The tricyclic antidepressant, nortriptyline, decreases the effect of clonidine. (source: Drug Bank )
clonidine - oxprenolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - oxprenolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - penbutolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - penbutolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - pindolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - pindolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - practolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - practolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - propranolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - propranolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - protriptyline The tricyclic decreases the effect of clonidine (source: Drug Bank )
clonidine - protriptyline The tricyclic antidepressant, protriptyline, decreases the effect of clonidine. (source: Drug Bank )
clonidine - sotalol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - sotalol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - timolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - timolol Increased hypertension when clonidine stopped (source: Drug Bank )
clonidine - trimipramine The tricyclic decreases the effect of clonidine (source: Drug Bank )
clonidine - trimipramine The tricyclic antidepressant, trimipramine, decreases the effect of clonidine. (source: Drug Bank )
desipramine - clonidine The tricyclic decreases the effect of clonidine (source: Drug Bank )
desipramine - clonidine The tricyclic antidepressant, desipramine, decreases the effect of clonidine. (source: Drug Bank )
doxepin - clonidine The tricyclic decreases the effect of clonidine (source: Drug Bank )
doxepin - clonidine The tricyclic antidepressant, doxepin, decreases the effect of clonidine. (source: Drug Bank )
esmolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
esmolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
imipramine - clonidine The tricyclic decreases the effect of clonidine (source: Drug Bank )
imipramine - clonidine The tricyclic antidepressant, imipramine, decreases the effect of clonidine. (source: Drug Bank )
labetalol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
metoprolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
metoprolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
mirtazapine - clonidine Possible hypertensive crisis (source: Drug Bank )
mirtazapine - clonidine Possible hypertensive crisis (source: Drug Bank )
nadolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
nadolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
nortriptyline - clonidine The tricyclic decreases the effect of clonidine (source: Drug Bank )
nortriptyline - clonidine The tricyclic antidepressant, nortriptyline, decreases the effect of clonidine. (source: Drug Bank )
oxprenolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
oxprenolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
pindolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
pindolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
propranolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
propranolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
timolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
timolol - clonidine Increased hypertension when clonidine stopped (source: Drug Bank )
treprostinil - clonidine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use. (source: Drug Bank )
trimipramine - clonidine Trimipramine may reduce the antihypertensive effect of the alpha2-agonist, Clonidine. Trimipramine may also increase the rebound hypertensive effect of Clonidine. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Clonidine if Trimipramine is initiated, discontinued or dose changed. Clonidine should be withdrawn very gradually to reduce the risk of hypertensive crisis. (source: Drug Bank )

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to clonidine: 6

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genetics and pharmacogenetics of aminergic transmitter pathways in functional gastrointestinal disorders. Pharmacogenomics. 2015. Martinucci Irene, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association of the G-protein and alpha2-adrenergic receptor gene and plasma norepinephrine level with clonidine improvement of the effects of diuretics in patients with cirrhosis with refractory ascites: a randomised clinical trial. Gut. 2010. Yang Y Y, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Overexpression of alpha2A-adrenergic receptors contributes to type 2 diabetes. Science (New York, N.Y.). 2010. Rosengren Anders H, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Norepinephrine attenuates hypoxia-inhibited thyrotropin-releasing hormone release in median eminence and paraventricular nucleus of rat hypothalamus. Neuro endocrinology letters. 2005. Hou Tian-De, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics of antihypertensive drug responses. American journal of pharmacogenomics : genomics-related research in drug development and clinical practice. 2004. Schwartz Gary L, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Effect of the C825T polymorphism of the G protein beta 3 subunit on the systolic blood pressure-lowering effect of clonidine in young, healthy male subjects. Clinical pharmacology and therapeutics. 2003. NĂ¼rnberger Jens, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
49884-774-86
DrugBank:
DB00575
PDB:
CLU
ChEBI:
46631
KEGG Drug:
D00281
PubChem Compound:
2803
PubChem Substance:
163008
46508119
IUPHAR Ligand:
516
Drugs Product Database (DPD):
2247608
ChemSpider:
2701
HET:
CLU
Therapeutic Targets Database:
DAP000231
FDA Drug Label at DailyMed:
d08d5bb4-3039-405c-843e-63a41a14a324

Clinical Trials

These are trials that mention clonidine and are related to either pharmacogenetics or pharmacogenomics.

No trials loaded.

NURSA Datasets

provided by nursa.org

No NURSA datasets available.

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

Sources for PharmGKB drug information: DrugBank, PubChem.