Difference between revisions of "Alpha-2 Agonists"

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Alpha-2 agonists have sedative, anxiolytic and analgesic effects.
 
Alpha-2 agonists have sedative, anxiolytic and analgesic effects.
  
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Alpha-2 agonists act on alpha-2 adrenoreceptors, and mimic the effects of the actual ligand binding. The sedative and anxiolytic effects arise from this process leading to pre-synaptic inhibition of noradrenaline release.
 
Alpha-2 agonists act on alpha-2 adrenoreceptors, and mimic the effects of the actual ligand binding. The sedative and anxiolytic effects arise from this process leading to pre-synaptic inhibition of noradrenaline release.
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==Pharmacokinetic Considerations==
 
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There is great variation between species sensitivity to alpha-2 agonists. Cattle are ten times as sensitive to the drugs as horses.
 
  
 
==Actions==
 
==Actions==
  
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Alpha-2 agonists have a wide range of actions, due to the presence of alpha-2 receptors throughout the body. The most useful pharmacological actions are '''sedation''', '''anxiolysis''' and '''analgesia'''. The drugs also have a huge '''anaesthetic sparing effect''', reducing MAC by 50-95%. They also give '''muscle relaxation'''.
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Alpha-2 agonists have a wide range of actions, due to the presence of alpha-2 receptors throughout the body. The actions most useful pharmacologically are '''sedation''', '''anxiolysis''' and '''analgesia'''. The drugs also have a huge '''anaesthetic sparing effect''', reducing MAC by 50-95%. They also give '''muscle relaxtion'''.
  
 
Other systems affected by alpha-2 agonists include:
 
Other systems affected by alpha-2 agonists include:
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* <u>Cardiovascular System</u>
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* Cardiovascular System
 
** Post synaptic alpha-2 effects and non-selective action on alpha-1 receptors cause vasoconstriction, hypertension and reflex bradycardia.
 
** Post synaptic alpha-2 effects and non-selective action on alpha-1 receptors cause vasoconstriction, hypertension and reflex bradycardia.
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** Pre-synaptic inhibition of noradrenaline release gives a reduced sympathetic outflow. This decreases heart rate and offsets vasoconstriction.  
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** Pre-synaptic inhibition of noradrenaline release gives a reduced sympathetic outflow. This dexreases heart rate and offsets vasoconstriction.  
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* <u>Respiratory System</u>
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* Respiratory System
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** The drugs cause mild depression of the respiratory system.
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** The drugs cause mild depression of the respiratory systsem.
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** The response to hypercapnia is reduced.
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** The response to hypercapnoea is reduced.
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* <u>Gastrointestinal Tract</u>
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* Gastrointestinal Tract
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** Alpha-2 agonists cause extreme vomiting in dogs and cats. [[#Xylazine|Xylazine]] is the worst culprit for this.
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** Alpha-2 agonists cause extreme vomitting in dogs and cats. [[#Xylazine|Xylazine]] is the worst culprit for this.
 
** Huge reductions in gut motility occur following drug administration, as well as decreased salivation and secretion.
 
** Huge reductions in gut motility occur following drug administration, as well as decreased salivation and secretion.
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* <u>Endocrine System</u>
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* Endocrine System
 
** Alpha-2 agonists inhibit ADH, leading to diuresis.
 
** Alpha-2 agonists inhibit ADH, leading to diuresis.
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** Insulin is also inhibited, causing hyperglycaemia which leads to osmotic diuresis. This, along with the above, causes excessive urination.
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** Insulin is also inhibited, causing hyperglycaemia which leads to osmotic diuresis. This, along with the aboce, causes excessive urination.
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** Growth hormone release is triggered by alpha-2 agonists.
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** Growth hormone release is triggered by alhpa-2 agonists.
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* <u>Urogenital Tract</u>
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* Urogenital Tract
 
** Uterine contraction occurs with alpha-2 agonist administration.
 
** Uterine contraction occurs with alpha-2 agonist administration.
  
 
==Side Effects and Contraindications==
 
==Side Effects and Contraindications==
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Side effects relate to the wide range of action of the drugs. These particularly include vomitting, hypertension and uterine contraction.
 
  
 
==Drugs in this Group==
 
==Drugs in this Group==
  
 
===Xylazine===
 
===Xylazine===
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Xylazine is available as a 2% solution for use in cattle, horses, cats and dogs. A 10% solution for horses may be used for pre-medication prior to [[Dissociative Agents#Ketamine|ketamine]] anaesthesia or analgesia in, for example, colic cases. A powdered form is also licensed in horses. Intramuscular and intravenous administration both have a short onset time of 5 minutes. The peak effect occurs 10 minutes after intramuscular injection, and the duration of the drug's actions is 20 mins following intravenous administration. Intravenous use is only licensed in dogs and cats.
 
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Xylazine must not be used in the last month of pregnancy, since it causes uterine contractions. The drug is also arrhythmogenic.
 
  
 
===Detomidine===
 
===Detomidine===
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Detomidine is available as a 10mg/ml solution in multidose vials. It is licenced for use in cattle and horses. It can be administered via an intravenous or intramuscular route. Although oral dosing is ineffective, it is readily absorbed across mucous membranes so may be adminstered sublingually. Its main indication for use is sedation in the horse for examinations, such as rectal or endoscopic, minor surgical procedures, as part of a premedication regime or before treatment, such as shoeing.
 
  
 
===Medetomidine===
 
===Medetomidine===
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Medetomidine is available as a 1mg/ml solution for use in dogs and cats.It is non irritant so therefore can be administered via an intravenous, intramuscular or subcutaneous route. Intravenous administration produces the most rapid effects, and the least amount of vomiting compared to other routes of administration. When given via an intramuscular route, maximal effects are not seen until 20 minutes after administration, although some sedation may be seen as early as 5 minutes. It is a very effective premedicant reducing the MAC of inhalation agents, and can be used in combination with [[Dissociative Agents#Ketamine|ketamine]] in cats to induce anaethesia.
 
  
 
===Romifidine===
 
===Romifidine===
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Romifidine is available as a 10mg/ml solution for use in horses. Its main indication for use is as a sedation agent and may be used in a premedication regime. It produces less ataxia and the head does not lower as much when compared to [[#xylazine|xylazine]] but the duration of action is longer.
 
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==Literature Search==
 
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[[File:CABI logo.jpg|left|90px]]
 
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Use these links to find recent scientific publications via CAB Abstracts (log in required unless accessing from a subscribing organisation).
 
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<br><br><br>
 
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[http://www.cabi.org/cabdirect/FullTextPDF/2005/20053164006.pdf ''' Medetomidine: a review.''' Read, M.; Ontario Veterinary Medical Association, Milton, Canada, Better medicine, better life. OVMA Conference Proceedings 2005, 2005, pp 31-34 - '''Full text Article''']
 
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|Vetstream = [https://www.vetstream.com/canis/Content/Generic/gen00160.asp Medetomidine]
 
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[[Category:Sedatives and Tranquilisers]]
 
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[[Category:Injectable Anaesthetic Agents]]
 

Revision as of 15:52, 3 March 2009

Alpha-2 agonists have sedative, anxiolytic and analgesic effects.

Mechanism of Action

Alpha-2 agonists act on alpha-2 adrenoreceptors, and mimic the effects of the actual ligand binding. The sedative and anxiolytic effects arise from this process leading to pre-synaptic inhibition of noradrenaline release.

Actions

Alpha-2 agonists have a wide range of actions, due to the presence of alpha-2 receptors throughout the body. The actions most useful pharmacologically are sedation, anxiolysis and analgesia. The drugs also have a huge anaesthetic sparing effect, reducing MAC by 50-95%. They also give muscle relaxtion.

Other systems affected by alpha-2 agonists include:

  • Cardiovascular System
    • Post synaptic alpha-2 effects and non-selective action on alpha-1 receptors cause vasoconstriction, hypertension and reflex bradycardia.
    • Pre-synaptic inhibition of noradrenaline release gives a reduced sympathetic outflow. This dexreases heart rate and offsets vasoconstriction.
  • Respiratory System
    • The drugs cause mild depression of the respiratory systsem.
    • The response to hypercapnoea is reduced.
  • Gastrointestinal Tract
    • Alpha-2 agonists cause extreme vomitting in dogs and cats. Xylazine is the worst culprit for this.
    • Huge reductions in gut motility occur following drug administration, as well as decreased salivation and secretion.
  • Endocrine System
    • Alpha-2 agonists inhibit ADH, leading to diuresis.
    • Insulin is also inhibited, causing hyperglycaemia which leads to osmotic diuresis. This, along with the aboce, causes excessive urination.
    • Growth hormone release is triggered by alhpa-2 agonists.
  • Urogenital Tract
    • Uterine contraction occurs with alpha-2 agonist administration.

Side Effects and Contraindications

Drugs in this Group

Xylazine

Detomidine

Medetomidine

Romifidine

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