Muscle Relaxants Masserano Flashcards
Antispasmodic
Benzos, tiazanidine, Flexeril, Soma, Robaxin
Antispasticity
Benzos, Tizanidine, Baclofen, Dantrolene
Cyclobenzaprine, Tizanidine, Carisoprodol side effect profile
More sedating
Carisoprodol, Meprobamate, opioids, benzos side effect profile
Abuse potential
Ways to relax the muscle
Inhibit Ca uptake and inhibit glutamate release
Diazepam MOA
Potentiates GABA hyperpolarization (chloride channel) by action on GABAa receptor. Acts on CNS and spinal cord
Baclofen MOA
Presynaptic GABAb receptors decrease Ca influx and glutamate release
Postsynaptic GABAb increase K+ efflux (hyperpolarize)
Tizanadine MOA
Centrally acting alpha2 agonist that decreases Ca flow into the presynaptic neuron = decrease in glutamate release
Dantrolene MOA
Binds to RyR1 channel in skeletal muscle which inhibits Ca release thus inhibiting contractions.
Dantrolene BBW
Hepatotoxicity
If no benefit after 45 days D/C
Cyclobenzaprine warnings
QT prolongation
Carisoprodol MOA
Metabolized to meprobomate and mechanism related to sedative properties
Male r value
0.68
Female r value
0.55
Alcohol Metabolism
Follows zero order kinetics so everyone metabolized at about the same rate.
One drink in 1 to 2 hours
Consequences of increase in NADH
- Increase in blood lactate
- Mg++ excretion increases = potential convulsions
- Uric acid excretion decreases = increase in nausea and vomiting
Consequences of increased Fatty acid synthesis
Increased triglyceride and lipid accumulation in liver
Cirrhosis
Consequences of Decreased gluconeogenesis
Synthesis of glucose from amino acids is impaired
Liver glycogen being low = hypoglycemia
Headaches, lethargy, confusion
Wernicke-Korsakoff syndrome
Due to malabsoprtion of thiamine
Ophthalmic difficulties and ataxia of gait
If not treated with thiamine (B1) mental state may deteriorate
Ethanol as a drug
Can be used to treat methanol and ethylene glycol poisoning which will competitively block alcohol dehydrogenase
Fomepizole
Injection used to competitively inhibit alcohol dehydrogenase
Ethanol potentiates CNS depressants with these drugs:
Opioids, benzos, sedatives, antidepressants, antipsychotics, antihistamines
Disulfiram MOA
Blocks the conversion of acetaldehyde to acetic acid. Cause lots of toxicity if alcohol is taken
Naltrexone MOA
Long lasting opioid antagonist and lowered rates of heavy drinking
Acamprostate MOA
Blocks glutamatergic aspartate receptors while activating GABAa