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Definition
MOA: act on GABA-A receptor to incr channel opening time and thus incr Cl- influx; alters sensory cortex, cerebellar, and motor activities; produces sedation, hypnosis, and anesthesia (barbiturate) Note: Metabolism takes place in the liver via oxidation to the inactive metabolite hydroxypentobarbital. Note: pKa is 8.0 so phenobarbital (pKa=7.3) is more ionized by alkaline urine!! Uses: Anticonvulsant and sedative-hypnotic Toxicities: caution in elderly pts, caution if suicidal
caution if impaired liver fxn, caution if drug abuse hx |
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Definition
MOA:act on GABA-A receptor to incr channel opening time and thus incr Cl- influx; "Use-dependent" inhibition of voltage-sensitive sodium channels (epilepsy); alters sensory cortex, cerebellar, and motor activities; produces sedation, hypnosis, and anesthesia (barbiturate) Uses: Anticonvulsant Toxicities: hypersens. to drug/class/compon.
porphyria hx
severe liver dysfxn
respiratory dysfxn
avoid abrupt withdrawal
caution if depression
caution if suicidal
caution if uremia |
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Definition
MOA: binds to benzodiazepine receptors; enhances GABA effects Uses: benzodiazepam 1, anti-anxiety Toxicities: contraindications-laucoma, angle-closure
pregnancy, CNS depression, caution if impaired liver fxn, caution if impaired renal fxncaution in elderly, debilitated, acutely ill pts |
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Definition
MOA: binds to benzodiazepine receptors; enhances GABA effects Uses: anti-anxiety, muscle spasms, status epilepticus Class: BZD 3, long-acting; Onset of Action: Rapid!
Metabolism: liver extensively |
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Definition
MOA:exact mechanism of action unknown; binds to serotonin and dopamine D2 receptors Uses: Class: Anxiolytic/Hypnot, Non-BZD Toxicities: serotonin syndrome (rare) Cautions: hypersens. to drug/class/compon.
MAO inhibitor use w/in 14 days
caution if impaired liver fxn
caution if impaired renal fxn |
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Definition
MOA: Increaseses affinity for GABA on the GABAA receptor, incr probability of opening; interacts w/ GABA-benzodiazepine receptor complexes
Uses: Sedative; Anxiolytic/Hypnot, Non-BZD |
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Definition
MOA: GABA-B agonist used to treat spasticity, improve mobility in pts with MS and other spinal cord lesions; acts as an inhibitory NT itself or by hyperpolarizing the primary afferent nerve terminals which inhibits release of excitatory NT's (ie Glut) Uses: muscle relaxant |
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Definition
MOA:exact mechanism of action unknown (centrally-acting muscle relaxant); some of its effects are similar to the tricyclic antidepressants, including Anti-cholinergic activity, potentiation of NE and antagonism of reserpine
Uses: muscle relaxant ; cyclobenzaprine relieves muscle spasms through a central action possibly at brainstem level
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Definition
MOA:alters skeletal muscle contractility (direct muscle relaxant); decrease muscle contraction by directly interfering w/Calcium ion release from the sarcoplasmic reticulum within skeletal muscle cells-->this uncouples the excitation-contraction process
Uses: muscle relaxant, malignant hyperthermia
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Definition
MOA: exact mechanism of action unknown; binds to central alpha2-adrenergic receptors, increasing presynpatic motor neuron inhibition and reducing spasticity (centrally-acting muscle relaxant Uses: muscle relaxant; ALS pts complaining of muscle weakness, but not first line drug in SC injury pts Cautions: produces more drowsiness than baclofen |
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