Description

Simple

A medication used to lower blood pressure, to treat severe pain, to prevent migraines, and to treat addiction as well as other conditions.

Clinical

An alpha-2 adrenergic agonist used to treat hypertension and severe cancer pain, among other conditions, and to treat withdrawal symptoms from various substances. It is also used to aid in the diagnosis of pheochromocytoma and to prevent migraines.

Overview

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]

Pharmacology

Indication

Clonidine tablets and transdermal systems are indicated for the treatment of hypertension alone or in combination with other medications.[8, Read more

Pharmacodynamic

Clonidine functions through agonism of alpha-2 adrenoceptors which have effects such as lowering blood pressure, sedation, and hyperpolarization of nerves.[ Read more

Mechanism of action

Clonidine is primarily an alpha-2 adrenoceptor agonist which causes central hypotensive and anti-arrhythmogenic effects.[ Read more

Absorption

Clonidine reaches maximum concentration in 60-90 minutes after oral administration.[ Read more

Protein binding

Clonidine is 20-40% bound to plasma proteins, especially albumin.[ Read more

Volume of distribution

The volume of distribution of clonidine has been reported as 1.7-2.5L/kg[ Read more

Clearance

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

Half life

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

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.[ Read more

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.[ Read more

Adverse Effects

Contraindications

  • Hypersensitivity:
    • true
  • Regions: US
  • Route:
    • Epidural
  • Regions: US
  • With Categories Coadmin:
      • Name: Anticoagulants
      • Drugbank Id: DBCAT000007
      • Mesh Id: D000925
  • Route:
    • Epidural
  • Regions: US
  • Patient Conditions:
      • Name: Administration above the C4 dermatome
      • Drugbank Id: DBCOND0107843
  • Route:
    • Epidural
  • Regions: US
  • Patient Conditions:
      • Name: Bleeding diathesis
      • Drugbank Id: DBCOND0099556
  • Route:
    • Epidural
  • Regions: US
  • Patient Conditions:
      • Name: Injection site infection
      • Drugbank Id: DBCOND0012701

Food Interactions

  • Avoid alcohol.
  • Take with or without food. The absorption is unaffected by food.

Interactions

Type in a drug name to check for interaction with Clonidine
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Clonidine.
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Clonidine can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
1-benzylimidazole
The risk or severity of hypertension can be increased when Clonidine is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of hypertension can be increased when Clonidine is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of sedation can be increased when Clonidine is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of sedation can be increased when Clonidine is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-Methoxyamphetamine
The risk or severity of sedation can be increased when Clonidine is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of sedation can be increased when Clonidine is combined with 5-methoxy-N,N-dimethyltryptamine.
6-Deoxyerythronolide B
The metabolism of Clonidine can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanine
The metabolism of 6-O-benzylguanine can be decreased when combined with Clonidine.
7-ethyl-10-hydroxycamptothecin
The metabolism of Clonidine can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
7-Nitroindazole
The risk or severity of sedation can be increased when Clonidine is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of sedation can be increased when Clonidine is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
8-azaguanine
The metabolism of 8-azaguanine can be decreased when combined with Clonidine.
8-chlorotheophylline
The metabolism of 8-chlorotheophylline can be decreased when combined with Clonidine.
9-aminocamptothecin
The metabolism of Clonidine can be decreased when combined with 9-aminocamptothecin.
9-Deazaguanine
The metabolism of 9-Deazaguanine can be decreased when combined with Clonidine.
9-Methylguanine
The metabolism of 9-Methylguanine can be decreased when combined with Clonidine.
Abatacept
The metabolism of Clonidine can be increased when combined with Abatacept.
Abediterol
The risk or severity of hypertension can be increased when Clonidine is combined with Abediterol.
12 References
  1. 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. 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. 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. 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. 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. 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. 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. 8 . FDA Approved Drug Products: Catapres Clonidine Hydrochloride Oral Tablets Link
  9. 9 . FDA Approved Drug Products: Catapres Clonidine Transdermal System Link
  10. 10 . FDA Approved Drug Products: Duraclon Clonidine Hydrochloride Injection Solution Link
  11. 11 . FDA Approved Drug Products: Kapvay Clonidine Hydrochloride Oral Extended Release Tablets Link
  12. 12 . Cayman Chemicals: Clonidine MSDS Link