Peringatan Keamanan

Oral LD50 is 126 mg/kg in rats.L7276 The TDLO is 70µg/kg in children, 126µg/kg in women, and 69µg/kg in men.L7276

Symptoms of overdose include hypertension followed by hypotension, bradycardia, respiratory depression, hypothermia, drowsiness, decreased reflexes, weakness, irritability, and miosis.L7237,L7240,L7243,L7246 Severe overdoses can cause reversible cardiac conduction defects or dysrhythmias, apnea, coma, and seizures.L7237,L7240,L7243,L7246 Induction of vomiting is not recommended due to CNS depression but gastric lavage or activated charcoal may be useful in recent ingestion.L7237,L7240,L7243,L7246 Dialysis is also unlikely to be beneficial.L7237,L7240,L7243,L7246 Overdose can be treated with supportive measures such as atropine sulfate for bradycardia, intravenous fluids or vasopressors for hypotension, vasodilators for hypertension, naloxone for respiratory depression, and blood pressure monitoring.L7237,L7240,L7243,L7246

Clonidine

DB00575

small molecule approved

Deskripsi

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

Struktur Molekul 2D

Berat 230.094
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half life after epidural administration is 30 minutes but otherwise can range from 6-23h.[A180559]
Volume Distribusi The volume of distribution of clonidine has been reported as 1.7-2.5L/kg[A180559], 2.9L/kg[L7240], or 2.1±0.4L/kg[L7243] depending on the source.
Klirens (Clearance) The clearance of clonidine is 1.9-4.3mL/min/kg.[A180559]

Absorpsi

Clonidine reaches maximum concentration in 60-90 minutes after oral administration.A180559,A180577 Race and fasting status do not influence pharmacokinetics of clonidine.L7237 A 100µg oral clonidine tablet reaches a Cmax of 400.72pg/mL with an AUC of 5606.78h\*pg/mL and a bioavailability of 55-87%.A180577

Metabolisme

The metabolism of clonidine is poorly understood.A14844 The main reaction in clonidine metabolism is the 4-hydroxylation of clonidine by CYP2D6, CYP1A2, CYP3A4, CYP1A1, and CYP3A5.A14844 Clonidine is <50% metabolized in the liver to inactive metabolites.A180559,L7237,L7240,L7243,L7246

Rute Eliminasi

Approximately 50% of a clonidine dose is excreted in the urine as the unchanged drug and 20% is eliminated in the feces.A180559,L7237

Interaksi Makanan

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

Interaksi Obat

1870 Data
Modafinil The metabolism of Clonidine can be increased when combined with Modafinil.
Armodafinil The metabolism of Clonidine can be increased when combined with Armodafinil.
Ceritinib Clonidine may increase the bradycardic activities of Ceritinib.
Ivabradine Clonidine may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Clonidine.
Deferasirox The serum concentration of Clonidine can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Clonidine can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Clonidine can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Clonidine can be decreased when it is combined with Teriflunomide.
Alfuzosin Alfuzosin may increase the hypotensive activities of Clonidine.
Amifostine Clonidine may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Clonidine.
Obinutuzumab Clonidine may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Clonidine.
Rituximab Clonidine may increase the hypotensive activities of Rituximab.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Clonidine.
Isoxsuprine Isoxsuprine may decrease the antihypertensive activities of Clonidine.
Midodrine Midodrine may decrease the antihypertensive activities of Clonidine.
Albuterol Salbutamol may decrease the antihypertensive activities of Clonidine.
Vilanterol Vilanterol may decrease the antihypertensive activities of Clonidine.
Acetylsalicylic acid Acetylsalicylic acid may decrease the antihypertensive activities of Clonidine.
Indacaterol Indacaterol may decrease the antihypertensive activities of Clonidine.
Selpercatinib Selpercatinib may decrease the antihypertensive activities of Clonidine.
Naxitamab Naxitamab may decrease the antihypertensive activities of Clonidine.
Phentermine Phentermine may decrease the antihypertensive activities of Clonidine.
Levosalbutamol Levosalbutamol may decrease the antihypertensive activities of Clonidine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Clonidine.
Pramipexole Clonidine may increase the sedative activities of Pramipexole.
Ropinirole Clonidine may increase the sedative activities of Ropinirole.
Thalidomide Clonidine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Benzylpenicilloyl polylysine Clonidine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Desmopressin Desmopressin may decrease the antihypertensive activities of Clonidine.
Isoetharine Isoetharine may decrease the antihypertensive activities of Clonidine.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Clonidine.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Clonidine.
Doxapram Doxapram may decrease the antihypertensive activities of Clonidine.
Metaraminol Metaraminol may decrease the antihypertensive activities of Clonidine.
Methoxamine Methoxamine may decrease the antihypertensive activities of Clonidine.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Clonidine.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Clonidine.
Dobutamine Dobutamine may decrease the antihypertensive activities of Clonidine.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Clonidine.
Ritodrine Ritodrine may decrease the antihypertensive activities of Clonidine.
Terbutaline Terbutaline may decrease the antihypertensive activities of Clonidine.
Bitolterol Bitolterol may decrease the antihypertensive activities of Clonidine.
Dopamine Dopamine may decrease the antihypertensive activities of Clonidine.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Clonidine.
Arbutamine Arbutamine may decrease the antihypertensive activities of Clonidine.
Fenoterol Fenoterol may decrease the antihypertensive activities of Clonidine.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Clonidine.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Clonidine.
Ephedrine Ephedrine may decrease the antihypertensive activities of Clonidine.
Mephentermine Mephentermine may decrease the antihypertensive activities of Clonidine.
Procaterol Procaterol may decrease the antihypertensive activities of Clonidine.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Clonidine.
Bambuterol Bambuterol may decrease the antihypertensive activities of Clonidine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Clonidine.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Clonidine.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Clonidine.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Clonidine.
Amibegron Amibegron may decrease the antihypertensive activities of Clonidine.
Solabegron Solabegron may decrease the antihypertensive activities of Clonidine.
Droxidopa Droxidopa may decrease the antihypertensive activities of Clonidine.
Isometheptene Isometheptene may decrease the antihypertensive activities of Clonidine.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Clonidine.
Naphazoline Naphazoline may decrease the antihypertensive activities of Clonidine.
Saralasin Saralasin may decrease the antihypertensive activities of Clonidine.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Clonidine.
Tyramine Tyramine may decrease the antihypertensive activities of Clonidine.
Adrafinil Adrafinil may decrease the antihypertensive activities of Clonidine.
Hexoprenaline Hexoprenaline may decrease the antihypertensive activities of Clonidine.
Etilefrine Etilefrine may decrease the antihypertensive activities of Clonidine.
Olodaterol Olodaterol may decrease the antihypertensive activities of Clonidine.
Cirazoline Cirazoline may decrease the antihypertensive activities of Clonidine.
Synephrine Synephrine may decrease the antihypertensive activities of Clonidine.
Moxisylyte Moxisylyte may decrease the antihypertensive activities of Clonidine.
Iofetamine I-123 Iofetamine I-123 may decrease the antihypertensive activities of Clonidine.
Racepinephrine Racepinephrine may decrease the antihypertensive activities of Clonidine.
DL-Methylephedrine DL-Methylephedrine may decrease the antihypertensive activities of Clonidine.
Amitraz Amitraz may decrease the antihypertensive activities of Clonidine.
Atipamezole Atipamezole may decrease the antihypertensive activities of Clonidine.
Ractopamine Ractopamine may decrease the antihypertensive activities of Clonidine.
Etafedrine Etafedrine may decrease the antihypertensive activities of Clonidine.
PF-00610355 PF-00610355 may decrease the antihypertensive activities of Clonidine.
Ritobegron Ritobegron may decrease the antihypertensive activities of Clonidine.
Abediterol Abediterol may decrease the antihypertensive activities of Clonidine.
Tulobuterol Tulobuterol may decrease the antihypertensive activities of Clonidine.
Dopexamine Dopexamine may decrease the antihypertensive activities of Clonidine.
Idazoxan Idazoxan may decrease the antihypertensive activities of Clonidine.
Higenamine Higenamine may decrease the antihypertensive activities of Clonidine.
Reproterol Reproterol may decrease the antihypertensive activities of Clonidine.
Tramazoline Tramazoline may decrease the antihypertensive activities of Clonidine.
Mephedrone Mephedrone may decrease the antihypertensive activities of Clonidine.
Octopamine Octopamine may decrease the antihypertensive activities of Clonidine.
Fenozolone Fenozolone may decrease the antihypertensive activities of Clonidine.
Norfenefrine Norfenefrine may decrease the antihypertensive activities of Clonidine.
Oxyfedrine Oxyfedrine may decrease the antihypertensive activities of Clonidine.
Buflomedil Buflomedil may decrease the antihypertensive activities of Clonidine.
Rimiterol Rimiterol may decrease the antihypertensive activities of Clonidine.
Methoxyphenamine Methoxyphenamine may decrease the antihypertensive activities of Clonidine.

Target Protein

Amine oxidase [copper-containing] 3 AOC3
Alpha-2B adrenergic receptor ADRA2B
Alpha-2C adrenergic receptor ADRA2C
Alpha-2A adrenergic receptor ADRA2A
Alpha-1A adrenergic receptor ADRA1A
Alpha-1B adrenergic receptor ADRA1B
Alpha-1D adrenergic receptor ADRA1D

Referensi & Sumber

Synthesis reference: David R. Pierce, William D. Dean, Michael E. Deason, "Process for preparation of clonidine derivatives." U.S. Patent US5684156, issued October, 1968.
Artikel (PubMed)
  • PMID: 7398184
    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.
  • PMID: 10215710
    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.
  • PMID: 1599347
    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.
  • PMID: 25272878
    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.
  • PMID: 25431436
    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.
  • PMID: 28726169
    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.
  • PMID: 20570945
    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.

Contoh Produk & Brand

Produk: 513 • International brands: 8
Produk
  • Apo-clonidine
    Tablet • 0.025 mg • Oral • Canada • Generic • Approved
  • Apo-clonidine Tab 0.1mg
    Tablet • 0.1 mg • Oral • Canada • Generic • Approved
  • Apo-clonidine Tab 0.2mg
    Tablet • 0.2 mg • Oral • Canada • Generic • Approved
  • Catapres
    Patch, extended release • 0.1 mg/24h • Transdermal • US • Approved
  • Catapres
    Tablet • 0.100 mg/1 • Oral • US • Approved
  • Catapres
    Tablet • 0.200 mg/1 • Oral • US • Approved
  • Catapres
    Tablet • 0.100 mg/1 • Oral • US • Approved
  • Catapres
    Tablet • 0.200 mg/1 • Oral • US • Approved
Menampilkan 8 dari 513 produk.
International Brands
  • Catapresan — Boehringer Ingelheim
  • Catapressan — Boehringer Ingelheim
  • Catarpres-TTS
  • Dixarit — Boehringer Ingelheim
  • Isoglaucon — Agepha
  • Run Rui — Bausch & Lomb
  • Velaril — Roemmers
  • Winpress — Winston

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