Fibromyalgia, Muscle Relaxers, Spasticity Drugs Flashcards
Duloxetine
Inhibits uptake of SER > NE.
CYP metabolism, esp. CYP2D6.
Milnacipran
Inhibits uptake of NE > SER (3x)
Side effects of duloxetine & milnacipran
↑ HR & BP
Contraindicated with uncontrolled closed-angle glaucoma & in conjunction with MAOIs.
SIADH, BBW for suicidal ideation.
Pregabalin
Inhibits the presynaptic alpha2delta subunit of L-type calcium channels → inhibit excitatory transmission by glutamate.
Side effects of pregabalin
Rebound after withdrawal, can cause dependence.
Additive sedation, worsening depression/suicidal ideation.
Dizziness, sedation, blurred vision, xerostomia, esp in elderly.
Drugs for fibromyalgia
Duloxetine, milnacipran, pregabalin
Amitriptyline (TCA) & fluoxetine (SSRI) & cyclobenzaprine (muscle relaxer)
Carisoprodol
Central CNS action in reticular activating system & spinal cord → sedation and ↓ perception of pain. No direct effect on neuronal conduction.
Side effects of Carisoprodol
CYP2C19 metabolism
Drowsiness, dizziness, agitation, insomnia, vertigo, ataxia, asthenia, mydriasis, orthostatic hypotension.
Monitoring with pregabalin
serum creatinine
Monitoring with carisoprodol
serum creatinine/BUN
Cyclobenzaprine
Similar to amitriptyline. Central action, maybe at brain stem.
For muscle spasm & fibromyalgia.
Side effects of cyclobenzaprine
CYP3A4, CYP1A2, CYP2D6 metabolism.
Significant anticholinergic action.
Additive CNS depression & anticholinergic activity. GI problems most significant.
Can prolong QT interval.
Methocarbamol
Oral, IM, or IV.
Generalized sedative action, altered pain perception.
For muscle spasm & tetanus.
Side effects of methocarbamol
Additive CNS depression. Drowsiness, dizziness, lightheadedness, blurred vision, HA, irritability.
Tizanidine
Agonist on presynaptic alpha2 receptor → decreased activation of polysynaptic spinal cord motor neurons and reduction in muscle tone.
For MS, spasticity, spinal cord trauma.