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Encyclopedia > Clonidine
Clonidine
Systematic (IUPAC) name
N-(2,6-dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine
Identifiers
CAS number 4205-90-7
ATC code C02AC01 N02CX02, S01EA04
PubChem 2803
DrugBank APRD00174
Chemical data
Formula C9H9Cl2N3 
Mol. mass 230.093 g/mol
Pharmacokinetic data
Bioavailability 75-95%
Protein binding 20-40%
Metabolism Hepatic to inactive metabolites
Half life 12-33 hours
Excretion urine (40-50%)
Therapeutic considerations
Pregnancy cat.

C(US) Image File history File links No higher resolution available. ... IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... A section of the Anatomical Therapeutic Chemical Classification System. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... This article or section does not cite any references or sources. ... General Name, Symbol, Number carbon, C, 6 Chemical series nonmetals Group, Period, Block 14, 2, p Appearance black (graphite) colorless (diamond) Standard atomic weight 12. ... General Name, Symbol, Number hydrogen, H, 1 Chemical series nonmetals Group, Period, Block 1, 1, s Appearance colorless Atomic mass 1. ... General Name, Symbol, Number chlorine, Cl, 17 Chemical series halogens Group, Period, Block 17, 3, p Appearance yellowish green Standard atomic weight 35. ... General Name, Symbol, Number nitrogen, N, 7 Chemical series nonmetals Group, Period, Block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... A drugs efficacy may be affected by the degree to which it binds to the proteins within blood plasma. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... The liver is an organ in vertebrates including humans. ... A metabolite is the product of metabolism. ... It has been suggested that Effective half-life be merged into this article or section. ... Excretion is the process of eliminating waste products of metabolism and other materials that are of no use. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ... Motto: (Out Of Many, One) (traditional) In God We Trust (1956 to date) Anthem: The Star-Spangled Banner Capital Washington D.C. Largest city New York City None at federal level (English de facto) Government Federal constitutional republic  - President George Walker Bush (R)  - Vice President Dick Cheney (R) Independence from...

Legal status

Prescription only The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ...

Routes oral, transdermal

Clonidine is a direct-acting adrenergic agonist prescribed historically as an anti-hypertensive agent. It has found new uses, including treatment of some types of neuropathic pain, opioid detoxification, sleep hyperhydrosis, and, off-label, to counter the side effects of stimulant medications such as methylphenidate or amphetamine. It is becoming a more accepted treatment for insomnia, as well as for relief of menopausal symptoms. Clonidine is increasingly used in conjunction with stimulants to treat attention-deficit hyperactivity disorder (ADHD), where it's given in late afternoon and/or evening for sleep, and because it sometimes helps moderate ADHD-associated impulsive and oppositional behavior, and may reduce tics.[1] Clonidine can also be used in the treatment of Tourette syndrome.[2] In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... A transdermal patch is a medicated adhesive patch that is placed on the skin to deliver a time released dose of medication through the skin and into the bloodstream. ... An adrenergic is a drug, or other substance, which has effects similar to, or the same as, epinephrine (adrenaline). ... In medicine, hypertension refers to the problem of abnormally high blood pressure. ... Neuropathy is usually short for peripheral neuropathy, meaning a disease of the peripheral nervous system. ... An opioid is a chemical substance that has a morphine-like action in the body. ... Detox, short for detoxification, in general is the removal of toxic substances. ... Sleep hyperhidrosis is the occurrence of excessive sweating during sleep. ... The term off-label refers to the use of a drug for a medical condition other than for which it was officially approved and marketed. ... Stimulants are drugs that temporarily increase alertness and wakefulness. ... Vitamin R redirects here. ... Amphetamine or Amfetamine (Alpha-Methyl-PHenEThylAMINE), also known as, beta-phenyl-isopropylamine, and benzedrine, is a prescription stimulant commonly used to treat Attention-deficit hyperactivity disorder (ADHD) in adults and children. ... This article is about the sleeping disorder. ... DISCLAIMER Please remember that Wikipedia is offered for informational use only. ... Tic may also refer to Tenancy in Common. ... Tourette syndrome (also called Tourettes syndrome, Tourettes disorder, Gilles de la Tourette syndrome, GTS or, more commonly, simply Tourettes or TS) is an inherited neurological disorder with onset in childhood, characterized by the presence of multiple physical (motor) tics and at least one vocal (phonic) tic; these...

Contents

Indications

The main use for this medication is used to treat high blood pressure. It works by stimulating certain brain receptors (alpha adrenergic type) which results in the relaxing of blood vessels in other parts of the body, causing them to widen.

Clonidine tablets and transdermal patch
Clonidine tablets and transdermal patch


ImageMetadata File history File links Clonidine_pills_and_patch. ... ImageMetadata File history File links Clonidine_pills_and_patch. ...


Clonidine is typically available as tablets (Catapres, Dixarit), as a transdermal patch (Catapres-TTS), or as an injectable form to be given epidurally, directly to the central nervous system. This article or section does not adequately cite its references or sources. ... A 21mg dose Nicoderm CQ patch applied to the right arm A transdermal patch or skin patch is a medicated adhesive patch that is placed on the skin to deliver a time released dose of medication through the skin and into the bloodstream. ... An injection is a method of putting liquid into the body with a hollow needle and a syringe which is pierced through the skin long enough for the material to be forced into the body. ... An epidural catheter after insertion. ... A diagram showing the CNS: 1. ...


Non-FDA approved uses

This medication may also be used to ease withdrawal symptoms associated with the long-term use of narcotics, alcohol and nicotine (smoking). In addition, clonidine has also be used for migraine headaches, hot flashes associated with menopause, attention deficit hyperactivity disorder.[3][4]


Clonidine is regularly prescribed to opiate addicts to help alleviate their withdrawal symptomology. It is mainly used to combat the sympathetic nervous system response to opiate withdrawal, namely tachycardia and hypertension, in the first couple days of withdrawals.[citation needed] It helps take away the sweating, hot/cold flashes, and general restlessness.[citation needed] The sedation effect is also useful. Scoring the poppy pod. ... Grays FIG. 838– The right sympathetic chain and its connections with the thoracic, abdominal, and pelvic plexuses. ... This article or section does not cite any references or sources. ... This article does not cite any references or sources. ...


Adverse effects

This drug may cause drowsiness, lightheadedness, dry mouth, dizziness, or constipation. Sucking on sugarless hard candy or ice chips, chewing sugarless gum, drinking water, and using a saliva substitute may help relieve dry mouth.


Pharmacodynamics

Clonidine is a centrally-acting alpha-2 agonist. It selectively stimulates receptors in the brain that monitor catecholamine levels in the blood. These receptors close a negative feedback loop that begins with descending sympathetic nerves from the brain that control the production of catecholamines (epinephrine, also known as adrenaline, and norepinephrine) in the adrenal medulla. By fooling the brain into believing that catecholamine levels are higher than they really are, clonidine causes the brain to reduce its signals to the adrenal medulla, which in turn lowers catecholamine production and blood levels. The result is a lowered heart rate and blood pressure, with side effects of dry mouth and fatigue. If clonidine is suddenly withdrawn the sympathetic nervous system will revert to producing high levels of epinephrine and norepinephrine, higher even than before treatment, causing rebound hypertension. Rebound hypertension can be avoided by slowly withdrawing treatment. The adrenergic receptors (or adrenoceptors) are a class of G_protein coupled receptors that is the target of catecholamines. ... Agonists An agonist is a substance that binds to a receptor and triggers a response in the cell. ... tyrosine is the precursor of catecholamines epinephrine norepinephrine dopamine Synthesis Catecholamines are chemical compounds derived from the amino acid tyrosine containing catechol and amine groups. ... Adrenaline redirects here. ... Norepinephrine (INN)(abbr. ... In mammals, the adrenal glands (also known as suprarenal glands) are the triangle-shaped endocrine glands that sit on top of the kidneys; their name indicates that position (ad-, near or at + -renes, kidneys). They are chiefly responsible for regulating the stress response through the synthesis of corticosteroids and catecholamines... Rebound hypertension is high blood pressure associated with sudden withdrawal of various antihypertensive medications. ...


Clonidine suppression test

Clonidine's effect on reducing circulating epinephrine by a central mechanism was used in the past as an investigatory test for pheochromocytomae, which are catecholamine-synthesizing tumors, usually of the adrenal medulla. In a Clonidine suppression test plasma catecholamines levels are measured before and 3 hours after a 0.3 ug/kg oral test dose has been given to a patient. A positive test occurs if there is no decrease in plasma levels. A phaeochromocytoma (pheochromocytoma in the US) is a neuroendocrine tumor of the medulla of the adrenal glands originating in the chromaffin cells, which secretes excessive amounts of catecholamines, usually adrenaline and noradrenaline (epinephrine and norepinephrine in the US). ...


Footnotes

  1. ^ National Institute of Neurological Disorders and Stroke (2002). "Methylphenidate and Clonidine Help Children With ADHD and Tics".
  2. ^ Schapiro NA. "Dude, you don't have Tourette's": Tourette's syndrome, beyond the tics. Pediatr Nurs. 2002 May-Jun;28(3):243-6, 249-53. PMID 12087644
  3. ^ Clonidine Oral Uses. Web MD.
  4. ^ Clonidine. Drugs.com.

  Results from FactBites:
 
Catapres Online, Description, Chemistry, Ingredients, Blackbox - Clonidine - RxList Monographs (361 words)
Clonidine hydrochloride USP is a centrally acting antihypertensive agent available as tablets for oral administration in three dosage strengths: 0.1 mg, 0.2 mg and 0.3 mg.
Clonidine hydrochloride is an imidazoline derivative and exists as a mesomeric compound.
Clonidine hydrochloride is an odorless, bitter, white, crystalline substance soluble in water and alcohol.
Clonidine - RxList Monographs (5364 words)
Clonidine stimulates alpha-adrenoreceptors in the brain stem, resulting in reduced sympathetic outflow from the central nervous system and a decrease in peripheral resistance: at a 45° tilt there is a smaller reduction in cardiac output and a decrease of peripheral resistance.
Clonidine is thought to produce analgesia at presynaptic and postjunctional alpha-2-adrenoceptors in the spinal cord by preventing pain signal transmission to the brain.
of clonidine in rats was 465 mg/kg, and in mice 206 mg/kg.
  More results at FactBites »


 
 

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