Muscle relaxants Flashcards
Increased tension in skeletal muscle, often after musculoskeletal injuries and inflammation
Muscle spasm
Does muscle spasm or spasticity often occur after injury or inflammation?
Spasm
Does muscle spasm or spasticity involve central pathology?
Spasticity
Diazepam is this type of drug
Benzodiazepine
MOA of diazepam
Enhancement of GABA inhibitory actions
Drug for spasms that enhances GABA inhibitory actions
Diazepam
Drug that potentiates GABA activity at alpha motor neuron in spinal cord, and causes supraspinal sedation
Diazepam
What effect does diazepam have on GABA action?
Potentiates GABA activity at alpha motor neuron in spinal cord
What is the half life of diazepam?
30-60 hours
(extensive biotransformation)
Metabolite is 30-100 hours (may be greatly increased in elderly)
Benzodiazepine should not be used with these drugs, due to risk of profound sedation, respiratory depression, coma, and death
Opiates
Drug for muscle spasms with these adverse effects:
Unsafe during pregnancy and lactation
Tolerance and physical dependence with long-term use
Increased risk of suicidality
Diazepam
Is diazepam safe to use during pregnancy and breastfeeding?
No
Drug that is an antidote to benzodiazepine overdose
Flumazenil
Flumazenil is an antidote to this
Benzodiazepine overdose
Drug that specifically binds benzodiazepine binding site and displaces benzodiazepine
Flumazenil
Dose low or high dose diazepam treat muscle spasms?
Low dose
Dose low or high dose diazepam treat spasticity?
High dose
Activation of this increases chloride entry into postsynaptic cells
Action is inhibitory - results in hyperpolarization
GABA receptor complex
Type of drugs for muscle spasm that appear to interrupt neuronal communication within the reticular formation and spinal cord to decrease polysynaptic reflex activity
Most cause sedation that contributes to muscle relaxation
Polysynaptic inhibitors
Polysynaptic inhibitor that is an absolute contraindication for porphyria
Carisoprodol
Polysynaptic inhibitor that has anticholinergic activity noted (dry mouth, blurred vision, constipation, urinary retention, sedation, confusion)
Cyclobenzaprine
Polysynaptic inhibitor that is an absolute contraindication for heart problems, concurrent use of monoamine oxidase inhibitors, and hyperthyroidism
Cyclobenzaprine
Cyclobenzaprine should not be used concurrently with this type of drugs
Monoamine oxidase inhibitors
Polysynaptic inhibitor that is an absolute contraindication in anemia, liver or renal disease
Metaxalone