Difference between revisions of "Alpha-2 Agonists"
| (14 intermediate revisions by 6 users not shown) | |||
| Line 1: | Line 1: | ||
| − | |||
Alpha-2 agonists have sedative, anxiolytic and analgesic effects. | Alpha-2 agonists have sedative, anxiolytic and analgesic effects. | ||
| Line 12: | Line 11: | ||
==Actions== | ==Actions== | ||
| − | Alpha-2 agonists have a wide range of actions, due to the presence of alpha-2 receptors throughout the body. The most useful | + | 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: | ||
* <u>Cardiovascular System</u> | * <u>Cardiovascular System</u> | ||
** 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. | ||
| − | ** Pre-synaptic inhibition of noradrenaline release gives a reduced sympathetic outflow. This | + | ** Pre-synaptic inhibition of noradrenaline release gives a reduced sympathetic outflow. This dexreases heart rate and offsets vasoconstriction. |
* <u>Respiratory System</u> | * <u>Respiratory System</u> | ||
| − | ** The drugs cause mild depression of the respiratory | + | ** The drugs cause mild depression of the respiratory systsem. |
| − | ** The response to | + | ** The response to hypercapnoea is reduced. |
* <u>Gastrointestinal Tract</u> | * <u>Gastrointestinal Tract</u> | ||
| − | ** Alpha-2 agonists cause extreme | + | ** 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. | ||
* <u>Endocrine System</u> | * <u>Endocrine System</u> | ||
| Line 39: | Line 38: | ||
===Xylazine=== | ===Xylazine=== | ||
| − | 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 [[ | + | 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 [[NMDA Antagonists|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. |
Xylazine must not be used in the last month of pregnancy, since it causes uterine contractions. The drug is also arrhythmogenic. | Xylazine must not be used in the last month of pregnancy, since it causes uterine contractions. The drug is also arrhythmogenic. | ||
| Line 49: | Line 48: | ||
===Medetomidine=== | ===Medetomidine=== | ||
| − | Medetomidine is available as a 1mg/ml solution for use in dogs and cats. | + | Medetomidine is available as a 1mg/ml solution for use in dogs and cats. |
| − | |||
===Romifidine=== | ===Romifidine=== | ||
| − | |||
| − | |||
| − | |||
| − | |||
| − | |||
| − | |||
| − | |||
| − | |||
| − | |||
| − | |||
| − | |||
| − | |||
| − | |||
| − | |||
| − | |||
| − | |||
Revision as of 14:53, 14 April 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.
Pharmacokinetic Considerations
There is great variation between species sensitivity to alpha-2 agonists. Cattle are ten times as sensitive to the drugs as horses.
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 above, causes excessive urination.
- Growth hormone release is triggered by alpha-2 agonists.
- Urogenital Tract
- Uterine contraction occurs with alpha-2 agonist administration.
Side Effects and Contraindications
Side effects relate to the wide range of action of the drugs. These particularly include vomitting, hypertension and uterine contraction.
Drugs in this Group
Xylazine
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 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.
Xylazine must not be used in the last month of pregnancy, since it causes uterine contractions. The drug is also arrhythmogenic.
Detomidine
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 is available as a 1mg/ml solution for use in dogs and cats.