Migraine/Tremor/Antiepileptic Drugs Flashcards
Sumatriptan
Class: antimigraine- Serotonin 5-HT(1B/1D) Receptor agonist
Apps: acute treatment of migraine w/ or w/o aura; acute treatment of cluster headache episodes.
Mech: actions at 5-HT receptors result in constriction of meningeal blood vessels; inhibit neuropeptide release; inhibit central neural transmission in trigeminal nucleus caudalis in brain stem.
Effects: minor- paresthesia, fatigue, facial flushing, drowsiness.
Dihydroergotamine
Class: antimigraine - ergot derivative.
Apps: treat migraine w/ or w/o aura; injection for cluster headaches.
Mech: mechanism responsible for efficacy of ergots similar to triptans.
Effects: nausea, vomiting, leg weakness, muscle pain, vascular effects; nasal spray - rhinitis.
Verapamil
Class: Ca2+ channel blocker.
Apps: treatment of angina, hypertension, etc. Off-label treatment of migraine.
Mech: inhibit influx of extracellular Ca2+ across myocardial and vascular smooth muscle membranes.
Effects: GI/constipation, gingival hyperplasia, sinus bradycardia.
Topiramate
For Migraines, Tremors, and Epilepsy
Class: oral anticonvulsant; neuropathic pain medication.
Apps: monotherapy and adjunctive for partial and generalized seizures; neuropathic pain conditions. Off-label for migraine and cluster. Treat essential tremor.
Mech: modulate voltage-gated Na+ channels, potentiate GABA inhibition, block glutamate transmission, modulate voltage-gated Ca2+ channels.
Effects: Somnolence, nausea, numbness. Anorexia, weight loss.
Valproate/Valproic Acid
For Migraines and Epilepsy
Class: anticonvulsant.
Apps: Monotherapy for partial and generalized seizures. For mania associated with bipolar disorder. Migraine prophylaxis.
Mech: unclear- may increase brain concentration of GABA. May also suppress repetetive neuronal firing through inhibition of voltage-sensitive Na+ channels.
Effects: abdominal pain, diarrhea, nausea/vomiting, somnolence, alopecia, tremor, and thrombocytopenia - CYP2C inhibitor (inhibits phenobarbital, phenytoin metabolism).
Propanolol
For Migraines and Tremors
Class: nonselective beta-adrenergic blocker.
Apps: manage hypertension, angina, arrhythmia. Migraine prophylaxis. Off-label- essential tremor; ethanol withdrawal; performance anxiety.
Mech: competitively block response to beta1 and beta2-adrenergic stimulation. For tremor- binds beta-2 receptor on muscle spindle; also CNS actions.
Effects: mild. CNS- dizziness, nausea, lethargy, fatigue, cognitive dysfunction; CV dysfunction.
Primidone
Class: anticonvulsant/antiepileptic.
Apps: manage gran mal, psychomotor, and focul seizures. off-label for essential tremor.
Mech: raises seizure threshold similar to phenobarbital (increase duration of GABA channel opening > Cl- influx, hyperpolarization).
Effects: sedation, dizziness, nausea, vomiting, giddiness, ataxia, confusion, vertigo.
Phenytoin
Class: anticonvulsant.
Apps: Monotherapy for partial seizures.
Mech: Blocks voltage-sensitive Na+ channels in neurons; reduces seizure propagation. Non-sedating.
Effects: gingival hyperplasia, rash, ataxia, diplopia, nystagmus, nausea/vomiting. Birth defects (pregnancy class D). Folic acid deficiency (anemia & neuropathy). Vit D & K deficiencies. Inhibit insulin secretion & hyperglycemia. Nonlinear kinetics (changes from 1st order to 0 order elimination w/ higher doses).
Carbamazepine
Class: Anticonvulsant.
Apps: monotherapy for partial seizures. Also for trigeminal neuralgia.
Mech: block voltage-sensitive Na+ channels, inhibits sustained repetitive firing.
Effects: rash, fatigue, hepatic dysfunction, ataxia, sedation, diplopia, nausea, hyponatremia. Fetal malformations.
Phenobarbital
Class: anticonvulsant, barbiturate.
Apps: treat partial or generalized seizures; sedative.
Mech: augments GABA response by increasing length of time Cl- channels are open following GABA binding to GABA-A (distinct from benzodiazepines which increase frequency of channel openings).
Effects: CNS-depressant, drowsiness, dizziness, lethargy, headache, vertigo, anxiety.
Oxcarbazepine
Class: anticonvulsant.
Apps: monotherapy and adjunctive for partial seizures.
Mech: block voltage-sensitive Na+ channels. Increase K+ conductance and modulates activity of Ca2+ channels; reduces glutamatergic transmission.
Effects: dizziness, sedation, headache, nystagmus, nausea, rash, hyponatremia, ataxia, diplopia.
Lamotrigine
Class: anticonvulsant.
Apps: monotherapy and adjunctive fo both partial and generalized seizures.
Mech: stabilize neuron membranes by blocking voltage-sensitive Na+ channels. Decrease release of glutamate and aspartate.
Effects: Rash, dizziness, diplopia, ataxia, tremor, insomnia, drowsiness, headache, blurred vision, nausea/vision.
Levetiracetam
Class: anticonvulsant.
Apps: adjunctive for partial and generalized seizures.
Mech: Block voltage-gated K+ channels in hippocampus neurons; also blocks kainate receptors. Inhibition of voltage-dependent N-type Ca2+ channel.
Effects: fatigue, depression, somnolence, dizziness, agitation, anxiety, vomiting.
Gabapentin
Class: oral anticonvulsant; neuropathic pain med; spasmolytic.
Apps: control seizures with epilepsy, reduce pain, manage spasticity.
Mech: not related to GABA system; inhibits some classes of Ca2+ channels. High lipid solubility, devoid of drug interactions, excreted in urine.
Effects: fatigue, drowsiness.
Pregabalin
Class: oral anticonvulsant; neuropathic pain med.
Apps: adjunctive for partial seizures. Chronic pain e.g. fibromyalgia & spinal cord injury.
Mech: like gabapentin, binds to voltage-dependent Ca2+ channel.
Effects: transient dizziness, somnolencer
