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CNS DRUGS EXAM 1

CNS EXAM 1

CLASSDRUGMOA(s)USE(s)ADR(s)NOTES
NSAIDS Ibuprofen (OTC), Naproxen (OTC), Diclofenac, Aspirin (OTC) COX 1/2 inhibitions (aspirin and naproxen more cox 1) (diclofenac more cox 2) acute migraines GI (cox 1) and CV (cox 2) goof for tension headaches and mild to moderate migraines
Triptans (5-HT agonists) Almotriptan, Naratriptan, Eletriptan, Frovatriptan Partial, Selective 5HT-1B/1D agonist decrease acute migraine pain via vasoconstriction, decrease CGRP release, postpartum bleeding (ergots) paresthesia (skin sensations), dizziness, coronary vasoconstriction, serotonis syndrome from combined used of triptans and ergots, MAOIs, SSRIs, SNRIs
Triptans (5-HT agonists) Rizatriptan, Sumatriptan, Zolmitriptan Partial, Selective 5HT-1B/1D agonist decrease acute migraine pain via vasoconstriction, decrease CGRP release, postpartum bleeding (ergots) paresthesia (skin sensations), dizziness, coronary vasoconstriction, serotonis syndrome from combined used of triptans and ergots, MAOIs, SSRIs, SNRIs caution use in CV disease, CI in ischemic heart disease and coronary artery vasospasm, increase in preterm births, sumatriptan available with naproxen
Ergotamines (5-HT agonists) Ergotamine tartrate, Dihydroergotamine Nonselective, 5-HT receptor partial agonists ​ Alpha-adrenergic receptor agonists decrease acute migraine pain via vasoconstriction, decrease CGRP release, postpartum bleeding (ergots) N/V, vasospasm, rebound headache with over use, hepatotoxicity, ergot toxicity (seizures, fingertip necrosis) ergots can block DA/adrenergic receptors, CI in pregnacy, serotonin syndrome
Ditans (5-HT agonsits) Lasmiditan Selective 5HT-1F agonist acute migraine pain, trigeminal activation without vasoconstriction dizziness, vertigo, nausea, paresthesia fewer adverse effects (no vasoconstriction) compared to triptans
Neurotoxin Onabotlinumtoxin A SNARE protein cleavage​ Inhibits vesicular release (ACh, CGRP) Migraine prophylaxis​ Muscle spasms​ Cosmetic, skin rejuvenation muscle weakness, flaccid paralysis, death Respiratory tract infections, muscle weakness, urinary incontinence, falls, fever
CGRP Receptor antibodies Erenumab Monoclonal antibodies for CGRP receptor​ Reversible Migraine prophylaxis Nausea, diarrhea, antibody development, hypersensitivity Rapid association , Slow dissociation, long t1/2 Avoid with other monoclonal antibodies
CGRP ligand antibodies Fremanezumab, Eptinezumab-jjmr, Galcanezumab Monoclonal antibodies for CGRP ligand​ Migraine prophylaxis Nausea, diarrhea, antibody development, hypersensitivity Cluster headaches (galcanezumab), Avoid with other monoclonal antibodies
CGRP antagonists Atogepant Small molecule CGRP receptor blockers​ Migraine prophylaxis
CGRP antagonists Rimegepant, Ubrogepant, Zavegepant (nasal) Competitive reversible blockade of CGRP receptor Acute migraines (rimegepant and ubrogepant are also prophylactic) nausea, skin rash, hypersensitivity shorter half life than mAbs
DA receptor antagonist Metoclopramide Dopamine-2 (D2) receptor antagonist​ Adjunct therapy to increase triptans/NSAIDs oral absorption, antinausea, GERD drowsiness, fatigue, restlessness, insomnia, anxiety, hyperrolactinemia, dyskinesias BOXED WARNING: tardive dyskinesia
Mild narcotic Butorphanol Mixed opioid, MOR partial agonist/KOR agonist​ analgesia constipation, sedation, abuse
Beta blockers Metoprolol, propranolol, timolol Nonselective β-AR antagonists​ Blocks β2 induced-vasodilation Vasoconstriction​ Antihypertensive migraine prophylaxis
Tricyclic antidepressants Amitriptyline Blocks NET/SERT reuptake ​ ↑ [NE/5HT] Analgesia​ Antidepressant migraine prophylaxis
Calcium channel blockers Verapamil Inhibits slow voltage Ca2+ channels Anti-inflammatory​ Antihypertensive migraine prophylaxis
Anticonvulsants Valproate, topiramate Na+ channel inactivation​ & other mechanisms Anti-inflammatory​ Anticonvulsants migraine prophylaxis , valproate is CI in pregnancy
Created by: beezy41
 

 



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