Sedatives and Opioids Flashcards
describe the reasons for premedication (7)
- facilitate restraint
- anxiolysis
- muscle relaxation
- pre-emptive analgesia
- decrease required induction and maintenance anesthetics
- smooth induction
- modulate autonomic reflex activity
categorize the drugs used for premedication based on class and drug enforcement agency (DEA) scheduling
5 classes
1. phenothiazines
2. alpha-2 agonists
3. opioids
4. benzodiazepines
5. anticholinergics: now only if indicated by patient blood pressure and heart rate
describe the 5 DEA scheduling levels
Schedule 1:
-no currently accepted medical use; high potential for abuse (ILLEGAL); heroin, LSD< marijuana, ecstasy, peyote
Schedule II:
-high potential for abuse, but do have a medical reason for use
-pure mu agonists
Schedule III:
-moderate to low potential for dependence or abuse
-ketamin/buprenorphine
Schedule IV:
-low potential for abuse
-tramadol, benzodiazepines, butorphenol, alfaxolone
Schedule V:
-very low potential for abuse
-cough medicine with less then 200mg codeine
propofol and etomidate not controlled!
describe phenothiazines (acepromazine)
- sedative effect via antagonism of dopamine receptors
- label dose is 0.45mg/kg but this is hella high!
-clinical dose is 0.01-0.05mg/kg - does NOT provide analgesia
- onset of action takes up to 20 min and duration of action is 6-8 hours (long! but variable based on metabolic rate)
- there is no reversal and no way to increase clearance so if overdose = fucked until patient clears it itself
- can give IV, IM, SQ; can be mixed with other drugs
- NOT controlled by DEA
describe the effects of acepromazine on the body (pharmacodynamics)
CNS: dose dependent sedation
cardiovascular: vasodilation, unresponsive hypotension, anti-arrhythmic
respiratory: minimal
GI: anti-emetic
other:
-splenic sequestration of RBCs (can decrease PCV 20-30%)
-anti-histaminic
-paraphimosis in horses: makes it easy to clean sheath and more likely to die from anesthesia than to have its penis amputated!
-decreases platelet aggression: not super clinically relevant
give indications and contraindications (6) of acepromazine
indications: suitable for exercise tolerant adult patients
contraindications/avoid in patients that are/have:
1. neonates
2. geriatric
3. heart disease
4. anemic
5. coagulopathic
6. hypotensive or cardiovascularly unstable
what 4 alpha agonists are available?
- dexmedetomidine: 1620:1
-most frequently used in small animal, available in a gel for thunderstorm anxiety
-much safer than xylazine for small animals - romifidine: 340:1
-associated with less ataxia in horses - detomidine: 260:1
-used frequently in horses, available in a gel - zylazine: selectivity is 160 alpha 2 receptors for every alpha 1 receptors
-oldest, still frequently used in horses, produces largest increase in blood glucose
-ruminants are very sensitive! so only use 1/10 of the equine dose
difference in selectivity for alpha 2 over alpha 1 receptor = slightly different effects despite same MOA
describe alpha 2 agonists
- produce sedation and hypnosis
-activate alpha-2 receptors in locus ceruleus of brain
-decreases norepi centrally and peripherally resulting in sedation and analgesia - rapid onset, short duration
- IV, IM, SQ; can be mixed with other drugs
- reversible
- not controlled by DEA
describe the cardiovascular effects of alpha 2 agonists
phase 1: vasoconstriction causes increased blood pressure causes reflex bradycardia and decreased CO but this is appropriate bc compensation
phase 2: resolution of vasoconstriction, persistent low HR (vagal effect) causes decreased blood pressure and decreased CO- up to 50% (doesn’t really effect them bc they’re sleeping)
arrhythmias:
1. sinus bradycardia
2. AV block (1st, 2nd, 3rd)
3. ventricular arrhythmias
describe respiratory, GI, genitourinary, and metabolic effects of alpha 2 agonists
respiratory: mild respiratory depression and mild pulmonary edema in small ruminants
-all small ruminants will have some measure of pulm edema but will occasionally be life threatening so be ready always! reverse and give furosemide or lasix
GI: decreased motility and occasional vomiting (xylazine to make cats vomit)
genitourinary:
-inhibit ADH = causes patients to urinate
-causes increased uterine wall tone
metabolic: inhibition of insulin release can lead to hyperglycemia
describe indications and contraindications (7) for alpha 2 agonists
indications: suitable for exercise tolerant adult patients
contraindications:
1. neonates
2. geriatrics
3. heart disease
4. anemic
5. cardiovascularly unstable
6. diabetic
7. pregnant
describe reversal agents for alpha 2 agonists
- atipamizole: used to reverse dexmedetomidine (equal volume given even though actual reversal dose given is 10 times admin dose based on concentration)
- yohimbine: used in horses to reverse xylazine, romifidine, detomidine
- tolazoline: commonly used in food animals
what opioids are available?
- morphine
- hydromorphone
- oxymorphone
- methadone
- meperidine
- fentanyl
- buprenorphine
- butorphenol
commonly used for acute pain; animals can become biologically addicted so be careful
how are opioids classified?
based on receptor selectivity
pure mu: morphine, hydromorphone, oxymorphone, methadone, meperidine, fentanyl
-give most profound analgesia, moderate sedation
partial mu: buprenorphine; moderate analgesia (species dependent), moderate sedation
mixed agonist/antagonist: butorphernol, nalbuphine
-mild analgesia (think enough for a nail trim), moderate sedation
describe opioid receptors
- mu, kappa, delta
- present throughout body: brain, spinal cord, peripheral nociceptors, joint spaces, circulating immune cells
- endogenous ligand is endorphins