8-24 Muscle Relaxers/Serotonin/Dopamine/Opiods/ Anesthetics Flashcards
Baclofen:
Mechanism of Action
GABA agonist
Inhibits neurotransmitter
release from skeletal muscle sensory afferent- (by inhibiting calcium influx and therefore reducing the release of excitatory transmitters)
Baclofen:
Rx
ºmuscle spasticity assoc.
with multiple sclerosis or Spinal Cord Injury
Baclofen:
Side Effects (1)
Drowsiness
Diazepam:
Mechanism of Action
Benzodiazepine receptor agonist
Diazepam:
Rx (2):
- Muscle spasm due to local injury (inflammation),
2. muscle spasticity due to loss of descending inhibitory input, (e.g.cerebral palsy)
General for benzodiazepines
(Diazepam, cloneazepam…)
Mechanism of Action (1):
Facilitate GABA mediated pre-synaptic inhibition
General for benzodiazepines
(Diazepam, cloneazepam…)
Clinical usages (2)
- Spinal Spasticity
2. Multiple Sclerosis
General for benzodiazepines
(Diazepam, cloneazepam…)
Side effects (2)
Sedation
Drowsiness
Rocuronium
Duration of Action
25 mins
Rocuronium
MOA
[Non-Depolarizing Muscular Nicotinic BLOCKER]
Rocuronium
Location of Elimination
Liver
Rocuronium
Rx (2)
- Intubation
2. Muscle relaxation during surgery or ventilation
Mivacurium
Duration of Action
15-20min
Mivacurium
MOA
[Non-Depolarizing Muscular Nicotinic BLOCKER]
Mivacurium
Elimination
Plasma cholinesterase
Mivacurium
Rx. (2)
- Intubation
2. Muscle relaxation during surgery or ventilation in pts w/ renal failure
Vecuronium
Duration of action
30-45 min
Vecuronium
MOA
[Non-Depolarizing Muscular Nicotinic BLOCKER]
Vecuronium
Elmination (2)
- Liver (metabolism and clearance)
2. Renal (elimination)
Vecuronium
Rx (2)
Adjuvant in Surgical Anesthesia for:
1) Abdominal Wall Relaxation
2) Orthopedic Procedures
Bromocriptine
Mechanism of Action
D2 Agonist
Bromocriptine
Rx
Parkinson’s Disease
Carbidopa
Mechanism of Action
Aromatic acid decarboxylase inhibitor
Carbidopa
Rx
Parkinson’s Disease
Carbidopa
Side Effects (2)
Same as L-Dopa since it increases L-Dopa –> arrhythmia, dyskinesia
Selegiline
Mechanism of Action
MAO-b inhibitor
Selegiline
Rx
Parkinson’s disease
Talcapone
Mechanism of Action
COMT inhibitor
Talcapone
Rx
Parkinson’s disease
Methylphenidate
Mechanism of Action
Dopamine reuptake inhibitor
Methylphenidate
Rx
ADHD
Methylphenidate
Side effect
Tachycardia
Mu (OP3)
Locations (6)
Brain:
- cortex (lamina III-IV)
- Thalamus
- Striosomes
- periaqueductal gray
Spinal Cord
- substantial gelatinosa
-Intestinal tract
Mu - subtype 1
Function (2)
- Supraspinal analgesia
- physical dependence
Mu - subtype 2
Function (5)
- Respiratory depression
- miosis
- euphoria
- reduced GI mobility
- physical dependence
” Mu2 was a kinda GRUMP “
Mu - subtype 3
Function
unknown
Naloxone
Receptors - antagonist/agonist (3)
mu-R: antagonist
Delta-R: antagonist
Kappa-R:antagonist
Naloxone
A: Used for:
B: Its indication helps prevent/reduce effects such as…(3)
C: Has NO _______ properties characteristic of other narcotic antagonist
Naloxone
A: antidote for opioid overdose
B: prevents or reverses effects of opioids including respiratory depression, sedation and hypotension
C: NO [agonistic or morphine-like] properties characteristics of other narcotic antagonist
Naloxone
Side Effects (4)
- Change in mood
- Trembling
- Change in heart rhythm
- Block the action of pain-lowering endorphins
MethaDone
Receptor - Antagonist/agonist (2)
mu - agonist
delta- agonist
- (M)etha(D)one *
MethaDone
Side effects
Firm occupancy of opioid receptors by MethaDone ____ (INC/DEC) desire for other opioid intake, because it is producing a _______ but ___ (INC/DEC) effect which attenuates withdrawal manifestations.
dependence
Firm occupancy of opioid receptors by MethaDone DEC desire for other opioid intake, because it is producing a LONGER but DEC EFFECT which attenuates withdrawal manifestations.
MethaDone
Function
Treats Opioid Dependence
Tizanidine
Physiological effect:
[CENTRAL a2 agonist] that acts on pre and post-synpatic nerves of Spinal Cord —> Inhibition
Tizanidine
Indication (2)
Multiple sclerosis
Spinal spasticity
Tizanidine
Toxicity (2)
Drowsiness
Hypotension
Dantrolene
Physiological Actions
Blocks calcium release from SR of skeletal muscle
Dantrolene
Indications (5)
- SPASMS 2º to Stroke
- SPASMS 2º to Spinal Cord Injury
- Malignant Hyperthermia
- Cerebral Palsy
- Multiple Sclerosis
Dantrolene
Toxicity (3)
- Muscle weakness
- Sedation
- Hepatitis
Metaclopramide
MOA:
Side effects (2) :
MOA: [D2 Blocker] with some [5HT4 agonist]
SE: [Focal dystonia], Akathisia, [Tardive Dystonia after 3 months]
M.SE.FAT
Metaclopramide:
Contraindications:
Contraindications: long-term rx (3 months
can cause tardive dyskinesia)
Haloperidol
MOA:
Indications (2):
MOA: [D2 Blocker]
Indications:
ºacute psychosis
ºlong-term depot for poorly compliant schizophrenic
patients
Haloperidol
Side Effects:
extrapyramidal motor disturbances
Trazadone MOA (2)
[5-HT2A/2C BLOCKER] + SSRI
Trazadone Indications (2)
Anxiety/depression
Trazadone
SE
Warning of suicidality in young adults at initiation of treatment
Trazadone
Contraindicaitons
MAO inhibitors
Nociceptin receptor
(OP4)
Subtypes
ORL1
Nociceptin receptor location (7)
Brain:
- Cortex
- Amygdala
- hippocampus
- septal nuclei
- habenula
- hypothalamus
Spinal cord