Sedatives (Analgesia, Anesthesia) Flashcards
tranquilizer (neuroleptic, anxiolytic)
- induces state of behavioral change wherein anxiety is relieved and patient is relaxed although aware of surroundings
- NO ANALGESIA or ANESTHESIA
sedative
induces state characterized by CNS depression and drowsiness, decreased awareness of surroundings
hypnotic
induces sleep
analgesic
- attenuate nociceptive input leading to reduction in pain sensation
- STOP TRANSDUCTION AND TRANSMISSION
antihyperalgesics
- decrease central sensitization to pain
- DO NOT BLOCK TRANSMISSION OF STIMULUS
antinociception
diminished ability to perceive pain
narcotic
induces analgesia and stupor bordering on general anesthesia
neuroleptanalgesia
- ANALGESIA and AMNESIC state produced by administration of a neuroleptic + narcotic
- deep sedation achievable, unconciousness may occur
premedication
drug(s) given before a medical, surgical, or invasive procedure to induce sedation, analgesia, and relieve anxiety
blood-brain barrier
- tight capillary endothelial junctions
- sealed off by glial cells
- active transport mechanism for removal of organic acids or bases (i.e. p-glycoprotein efflux pump)
- constant flow of CSF into venous drainage
excitatory NTs
- glutamate (NMDA receptor)
- acetylcholine
inhibitory NTs
- GABA
- glycine (spinal cord)
what are the main effects of neuroleptics (tranquilizers)?
- sedation and hypnosis
- emotional quietness
- dissociation from surroundings
what class of tranquilizers have analgesic effects?
alpha-2 agonists
what is the most common phenothiazine?
acepromazine
why might you want to be careful in using a phenothiazine with a nursing or late-term pregnant animal?
- phenothiazines increase prolactin release which is normally inhibited by dopamine
- dopamine is necessary for pregnant animals, at normal concentrations there is no milk letdown
what is the chemoreceptor trigger zone (CRTZ)?
= vomiting center
are there reversal agents for phenothiazines?
no because they act in a lot of places, you just have to ride out the clinical effects (2-4 hrs)
what breeds are more sensitive to CNS effects of phenothiazines?
-boxers, brachycephalics, MDR1 mutants, large breed dogs, sighthounds
what would you be care using phenothiazines on patients in need of a splenectomy?
they reduce hematocrit leading to splenomegaly
what can a phenothiazine mask in a patient?
a hypersensitivity reaction
what animals would you practice caution in using acepromazine with?
- boxers, large breed dogs, sighthounds, MDR1 gene mutations (increased CNS effects)
- stallions (w/ possibility of seeing mare, penile prolapse and injury)
- cattle (rumenal regurg, not approved in food)
- aggressive dogs (startle more easily, increased)
- excited patients
what other drug would you take precaution in using with acepromazine?
epinephrine, stimulates a1, a2, b1, and b2 so if a1 is blocked then b2 vasodilation is unopposed
what are phenothiazines typically combine with?
analgesics
what is the number one adverse cardiovascular/respiratory effect of phenothiazines?
hypotension
what drug antagonizes benzodiazepine agonists such as diazepam, midazolam, and alprazolam?
flumazenil
full agonist
full effect triggered when bound
partial agonist
less effect triggered when bound, may be saturable (“ceiling effect”)
antagonist
- binds to a receptor and blocks effects of any agonists
- may reverse the effect of previously given agonist
inverse agonist
- binds to receptor and causes an effect that is opposite of an agonist
- reverse of what is seen w/ the agonist
competitive binding
REVERSIBLE effect
non-competitive binding
IRREVERSIBLE binding
what receptor are benzodiazepine binding sites on and what do benzodiazepines binding there cause?
- GABAa receptors
- cause hyperpolarization of neurons leading to a higher threshold (less likely to fire)
- agonize GABA leads to suppressing the CNS
between diazepam and midazolam which route of administration, IV or IM, would you give which drug?
- diazepam give IV, slowly (hypotension w/ rapid inj)
- midazolam give IM
what can diazepam cause in cats if given orally?
hepatic necrosis
what benzodiazepine works well for thunder storm anxiety?
alprazolam
what is the most reliable sedative for ruminants?
benzodiazepines
what class of drugs can have paradoxical excitation?
benzodiazepines, NOT reliable on its own
what drug is a specific reversal for benzodiazepines?
flumazenil = competitive antagonist
what class of drug is often the MOST reliable as sedatives for very young, very old, or very sick patients?
benzodiazepines
what are some contraindications of diazepam injections?
- IM = painful
- IV given fast shows hypotension
- large IV doses can cause hemolysis
T/F: benzodiazepines can serve as an anticonvulsant
TRUE! great for emergency treatment of seizures (i.e. diazepam given rectally) and status epilepticus