Anethetics and Analgesics etc. Flashcards
LEARN DAT SH*T
Phenothiazines MOA
- Dopamine (D2) receptor blockade within CNS
- d2 - pre and post-synaptic G-protein coupled receptor
- blockade leads to decrease in cAMP and adenylate cyclase activity, Ca conductance, and alterations in postsynaptic potassium conductance
- blockage of alpha 1 adrenergic, muscarinic, and histamine (H1) receptors
Phenothiazine example
Acepromazine
Acepromazine drug type
phenothiazine
Phenothiazine negative side effects
- dec stroke volume, CO, arterial blood pressure
- Dec blood pressure and systemic vascular resistance
- dec PCV (dt splenic engorgement ofter a1-adrenergic receptor blockade), reduction of platelet aggregation (no impact in clot formation)
Acepromazine Effects and duration
- moderate sedation and some muscle relaxation
- No analgesia
- some antiemetic and antihistamine effects
- lasts 4-6 hrs post IM or IV
- no reversal
Benzodiazepines MOA
Enhances the GABA-A receptor’s affinity for GABA resulting in inc chloride conductance and hyperpolarization of postsynaptic cell membranes, preventing propogation of action potentials (GABA is primary inhibitory neurotransmitter in CNS)
Benzodiazepines examples
midazolam, diazepam
Diazepam specifics
- Benzodiazepine
- poorly water soluble
- binds to plastics
- Metabolized by hepatic microsomal enzymes - do not use with liver dysfunction (results in delayed metabolism/clearance)
Benzodiazepines effects
- cause muscle relaxation, some narcosis, amnesia, and no analgesia.
- anticonvulsant
- wide thereputid index and overdose is difficult
- reversal is flumazenil
Benzodiazepines negative side effects
- no significant cardiovascular or respiratory depression
- may cause excitement esp in young animals due to central disinhibitory effects
Alpha2-adrenergic receptor agonists - MOA
- Cause a decrease of norepinephrine release in the central nervous system
Alpha2-adrenergic receptor agonists - examples
- Xylazine
- Medetomidine
- Dexmedetomidine
Alpha2-adrenergic receptor agonists - negative side effects
- Some activity at peripheral alpha1-receptors resulting in vasoconstriction, hypertension, arrhythmogenicity, and paradoxical excitation
- hypertension can result in reflex bradycardia which can lead to dec sympathetic output and eventually hypotension.
- hyperglycemia, diuresis, and respiratory depression
Xylazine
- Alpha2:Alpha1 receptor selectivity of 160:1
- Duration 15-20min after IV or IM
- induce vomiting in cats
- associated with 44-fold inc in cardiac arrest during anesthesia in dogs and is not indicated in this species
Alpha2-adrenergic receptor agonists effects
- produce profound sedation, analgesia, and muscle relaxation
- reversed with atipamazol
Medetomidine
- Alpha2:Alpha1 receptor selectivity of 1600:1
- Duration of effect 60-90 min
- causes hypertension and reflex bradycardia in dogs
- if used alone may result in brief periods of unexpected arousal and aggression, biting nearby personel.
- increasing dose prolongs duration of effect but does not change the degree of effect
- bradycardia and hypotension may persist after reversal
Dexmedetomidine
- dextrorotary isomer of the racemic medetomidine
- less sedation and shorter duration of action from medetomidine
Opiods MOA
Act on G protein-couples receptors to decrease release of neurotransmitters, such as substance P and glutamate, in the presynaptic cell and cause hyperpolarization of the postsynaptic cell.
- net result is a decrease in neuronal activity and transmission of pain signals
- Act on any of 3 receptors, µ, κ, and δ located throughout the CNS and peripheral tissues
- analgesia is primary systemic effects
- reversed with nalaxone
µ-receptor
- G protein-coupled receptor
- regulates the majority of clinical effects, including analgesia and side effects
κ-receptor
- G protein-coupled receptor
- plays a role of analgesia but distinguishing that role from that of the µ-receptor is challenging