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

Effect Regions Age Groups Incidences Evidence Type
Hypotension/Postural Hypotension US
  • Kind: experimental
    • Percent: 47
  • Clinical Trial
    Hypotension US
  • Kind: experimental
    • Percent: 44.8
  • Kind: placebo
    • Percent: 10.6
  • Clinical Trial
    Anxiety/Confusion US
  • Kind: experimental
    • Percent: 38
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 38
  • Kind: placebo
    • Percent: 4
  • Clinical Trial
    Postural Hypotension US
  • Kind: experimental
    • Percent: 31.6
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 31
  • Kind: placebo
    • Percent: 4
  • Clinical Trial
    Excessive Sleepiness US
  • Kind: experimental
    • Percent: 25
  • Clinical Trial
    Urinary Tract Infections (UTIs) US
  • Kind: experimental
    • Percent: 22
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 13.2
  • Kind: placebo
    • Percent: 21.3
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 13.2
  • Kind: placebo
    • Percent: 21.3
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 20
  • Kind: placebo
    • Percent: 16
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 19
  • Kind: placebo
    • Percent: 7
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 16
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 13
  • Kind: placebo
    • Percent: 16
  • Clinical Trial
    Upper Abdominal Pain US
  • Kind: experimental
    • Percent: 15
  • Kind: placebo
    • Percent: 12
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 10.5
  • Kind: placebo
    • Percent: 14.9
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 14
  • Kind: placebo
    • Percent: 4
  • Clinical Trial
    Confusion US
  • Kind: experimental
    • Percent: 13.2
  • Kind: placebo
    • Percent: 10.6
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 13.2
  • Kind: placebo
    • Percent: 4.3
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 13.2
  • Kind: placebo
    • Percent: 8.5
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 13
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 13
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 7
  • Kind: placebo
    • Percent: 12
  • Clinical Trial
    Upper Abdominal Pain US
  • Kind: experimental
    • Percent: 10
  • Kind: placebo
    • Percent: 12
  • Clinical Trial
    Weakness US
  • Kind: experimental
    • Percent: 10
  • Varying Reports
    Irritability US
  • Kind: experimental
    • Percent: 9
  • Kind: placebo
    • Percent: 4
  • Clinical Trial
    Nightmare US
  • Kind: experimental
    • Percent: 9
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Nausea/Vomiting US
  • Kind: experimental
    • Percent: 7.9
  • Kind: placebo
    • Percent: 2.1
  • Clinical Trial
    Upper Abdominal Pain US
  • Kind: experimental
    • Percent: 7
  • Kind: placebo
    • Percent: 4
  • Clinical Trial
    Irritability US
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 7
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 7
  • Kind: placebo
    • Percent: 5
  • Clinical Trial
    Infection NOS US
  • Kind: experimental
    • Percent: 6
  • Clinical Trial
    Fevers US
  • Kind: experimental
    • Percent: 6
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: 6
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 6
  • Clinical Trial
    Decreased appetite US
  • Kind: experimental
    • Percent: 6
  • Kind: placebo
    • Percent: 3
  • Clinical Trial
    Abdominal Pain Upper US
  • Kind: experimental
    • Percent: 6
  • Kind: placebo
    • Percent: 3
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 6
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 6
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Tinnitus US
  • Kind: experimental
    • Percent: 5.3
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Hallucination US
  • Kind: experimental
    • Percent: 5.3
  • Kind: placebo
    • Percent: 2.1
  • Clinical Trial
    Chest Pain US
  • Kind: experimental
    • Percent: 5.3
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Sweating US
  • Kind: experimental
    • Percent: 5.3
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 5
  • Clinical Trial
    Skin Ulcers US
  • Kind: experimental
    • Percent: 5
  • Clinical Trial
    Pain US
  • Kind: experimental
    • Percent: 5
  • Clinical Trial
    Hyperesthesia US
  • Kind: experimental
    • Percent: 5
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: 5
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 5
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Gastrointestinal viral US
  • Kind: experimental
    • Percent: 5
  • Kind: placebo
    • Percent: 0
  • Clinical Trial

    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.