Neuro Pharm Flashcards
Triptans
sumatriptan
What is the MOA of triptans?
5-HT agonists, inhibit trigeminal nerve activation; induce vasoconstriction
What is the clinical use of the triptans?
acute migraine, cluster headache attacks
What are the adverse effects of the triptans?
coronary vasospasm (C/I in patients with CAD or prinzmetal angina), mild paresthesia, serotonin syndrome, relative C/I in pregnancy
Side effects of phenytoin
Phenytoin Has Given MDs Frustration:
- Peripheral neuropathy
- Hirsutism
- Gingival hyperplasia
- Megaloblastic anemia (d/t decreased folate absorption)
- Drug-induced lupus
- Stevens-Johnson syndrome
- Fetal hydantoin syndrome
Which seizure drugs block Na+ channels?
phenytoin, carbamazepine, lamotrigine, topiramate, valproic acid
Which seizure drugs increase GABA activity?
gabapentin, phenobarbital, valproic acid, benzodiazepines, tigabine, vigabatrin, levetiracetam
Which seizure drugs block T-type Ca2+ channels?
gabapentin, ethosuximide, phenytoin (high doses)
Which antiepileptics are teratogens?
phenytoin, carbamazepine, valproic acid (spina bifida)
What drugs cause Stevens-Johnson syndrome?
Steve Jobs made APPLE PCs
- Allopurinol
- Phenytoin
- Phenobarbital
- Lamotrigine
- Ethosuximide
- Penicillin
- Carbamazepine
- Sulfonamide
What drugs are known to cause agranulocytosis?
“C’s”
- carbamazepine
- clozapine
- colchicine
- PTU & methimazole
What antiepileptics are hepatotoxic?
valproic acid & carbamazepine
What drugs induce the P450 system?
Coronas, Guinness, & PBRs induce chronic alcoholism
- Carbamazepine
- Griseofulvin
- Phenytoin
- Barbiturates
- Rifampin
- St. John’s wort
- chronic alcoholism
Parkinson Disease drugs
(BALSA)
- Bromocriptine
- Amantadine
- Levodopa/Carbidopa
- Selegiline/Rasagiline
- Antimuscarinics
Bromocriptine
Dopamine agonist - ergot (peripheral vasoconstrictor, so increases BP)
Pramipexole, ropinirole
Dopamine agonists, non ergots
Amantadine
increases dopamine availability (increases dopamine release and decreases dopamine reuptake)
Carbidopa
given with levodopa; blocks peripheral conversion of L-DOPA into dopamine by inhibiting DOPA decarboxylase
Entacapone, tolcapone
prevent peripheral conversion of L-DOPA into 3-OMD by inhibiting COMT
(tolcapone acts both peripherally with L-DOPA and centrally with dopamine)
Selegiline, Rasagiline
blocks conversion of dopamine into DOPAC by selectively inhibiting MAO-B
Benztropine
antimuscarinic that improves some of the symptoms of Parkinsons (improves tremor and rigidity, but has little effect on bradykinesia)
Medications that are common Tx for insomnia
melatonin, antihistamines, antidepressants, benzodiazepines, zolpidem & zaleplon, eszopiclone, ramelteon, orexin rector antagonists
melatonin tx for insomnia
nonaddictive, OTC, good safety profile, questionable efficacy
antihistamines tx for insomnia
commonly used OTC by patients first line; anticholinergic side effects (avoid in the elderly), next-day fatigue
antidepressant tx for insomnia
(amitriptyline, trazodone, doxepin); anticholinergic effects, dry mouth
benzodiazepines tx for insomnia
(triazolam, temazepam, lorazepam); increases GABA, addictive, short term only
zolpidem, zaleplon tx for insomnia
act at the benzo receptor; short term only (<35 days), rebound insomnia when discontinued
Eszopiclone tx for insomnia
longer half life than zolpidem, may be used long term
Ramelteon tx for insomnia
nonaddictive, works at melatonin receptors, avoid if hepatic insufficiency
Orexin receptor antagonists tx for insomnia
block effects of orexin A and B, which promote wakefulness
Inhaled anesthetics: Nitrous oxide
low blood solubility, low lipid solubility
Inhaled anesthetics: Halothane
high blood solubility, hepatotoxicity
Inhaled anesthetics: sevoflurane, desflurane
low blood solubility, high lipid solubility
Inhaled anesthetics: isoflurane
moderate blood and lipid solubility
IV anesthetics: propofol
increases GABA, rapid onset, rapid recovery, high triglyceride content (can cause pancreatitis long term)
IV anesthetics: ketamine
dissociative anesthetic, hallucinations, increases cerebral blood flow; PCP analog, blocks NMDA receptors
IV anesthetics: barbiturates (phenobarbital, pentobarbital, secobarbital)
decreases cerebral blood flow, increase duration of chloride channel opening on GABA receptors
thiopental - good for brain surgery
IV anesthetics: benzodiazepines (diazepam, lorazepam, alprazolam)
Increase frequency of chloride channel opening on GABA receptors, reverse with fumazenil
midazolam - used for endoscopy
may cause severe post op respiratory depression
AE - decrease BP
IV anesthetics: opioids (morphine, fentanyl, remifentanil, sufentanil)
analgesia; mu (beta-endorphins), delta (enkephalin), and kappa receptors (dynorphin)
reverses with opioid receptor antagonists (naloxone, naltrexone)
butorphanol (opioid):
partial opioid, causes less respiratory depression
dextromethorphan (opioid):
weak opioid used for cough suppression
tramadol (opioid)
less-addictive opioid used for analgesia
loperamide and diphenoxylate (opioids)
treatment of diarrhea
neuromuscular blocking agents: non-depolarizing
tubocurarine, atracurium, mivacurium, vecuronium, rocuronium, pancuronium
competitive inhibitors of postsynaptic nicotinic acetylcholine receptors at NMJ
can reverse with acetylcholinesterase inhibitor
neuromuscular blocking agents: depolarizing
succinylcholine
Phase I: rapid onset and recovery, cannot be reversed
Phase II: larger dose, longer recovery, can be reversed with acetylcholinesterase inhibitor
What is the dangerous side effect of succinylcholine?
succinylcholine + inhaled anesthetics in patient with RYR1 gene mutation -> possible malignant hyperthermia
Local anesthetics
esters - procaine, cocaine, tetracaine, benzocaine
amides - lidocaine, mepivacaine, bupivacaine (amides have 2 I’s)
- block Na+ channels
- can be given with vasoconstrictors (epinephrine) to enhance local action (only in tissues with collateral circulation)
- in infected (acidic) tissues, you need more drugs
What is the order of activity of local anesthetics on different fiber types?
small-diameter > large-diameter myelinated > unmyelinated (but size predominates)
sensory fibers = small
SNS = medium myelinated
motor = large myelinated
