CNS Pharm EC Flashcards
Phenytoin (MOA, Use)
Inactivate Na channels
1st line for tonic clonic seizures
1st line for status epilepticus prophylaxis
Simple partial seizures
Complex partial seizures
Phenytoin toxicity
Nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsutism, megaloblastic anemia, teratogen, SLE-like syndrome, induction of P450s, lymphadenopathy, Steven’s Johnson syndrome, osteopenia
Carbamazepine (MOA, Use)
Inactivate Na channels
1st line for simple partial seizures
1st line for complex partial seizures
1st line for tonic clonic seizures
1st line for trigeminal neuralgia
Carbamazepine toxicity
Diplopia, ataxia, blood dyscrasias, liver toxicity, induce P450s, teratogen, SIADH, Stevens-Johnson syndrome
Lamotrigine (MOA, Use)
Blocks voltage gated Na channels
Simple partial seizures
Complex partial seizures
Tonic clonic seizures
Lamotrigine toxicity
Stevens-Johnson syndrome
Gabapentin (MOA, Use)
Inhibits voltage activated Ca channels
Simple partial seizures Complex partial seizures Tonic clonic seizures Peripheral neuropathy Migraine prophylaxis Bipolar disorder
Gabapentin toxicity
Sedation, ataxia
Topiramate (MOA, Use)
Blocks Na channels
Potentiates GABA
Simple partial seizures
Complex partial seizures
Tonic clonic seizures
Migraine prevention
Topiramate toxicity
Sedation, mental dulling, kidney stones, weight loss
Phenobarbital (MOA, Use)
Potentiate GABAa
1st line in children
Simple partial seizures
Complex partial seizures
Tonic clonic seizures
Phenobarbital toxicity
Sedation
Tolerance
Dependence
Induction of P450s
Valproic acid (MOA, Use)
Inactivate Na channels
Increase GABA concentration
1st line for tonic clonic seizures Simple partial seizures Complex partial seizures Absence seizures Myoclonic seizures
Valproic acid toxicity
GI distress Fatal hepatotoxicity Neural tube defects (contraindicated in pregnancy) Tremor Weight gain
Ethosuximide (MOA, Use)
Blocks thalamic T-type Ca channels
1st line for absence seizures
Ethosuximide toxicity
GI distress Fatigue Headache Urticaria Stevens-Johnson syndrome
Diazepam or Lorazepam (MOA, Use in seizures)
Potentiate GABAa
1st line for acute status epilepticus
Seizures of eclampsia
Tiagabine (MOA, Use)
Inhibits GABA reuptake
Simple partial seizures
Complex partial seizures
Vigabatrin (MOA, Use)
Irreversibly inhibits GABA transaminase (increases [GABA])
Simple partial seizures
Complex partial seizures
Levetiracetam (MOA, Use)
Modulate GABA and glutamate release
Simple partial seizures
Complex partial seizures
Tonic clonic seizures
Zolpidem, Zaleplon, Eszopiclone (MOA, Use, Tox)
Act on BDZ1 GABA receptor (effects reversed by flumazenil)
Treats insomnia
Can cause ataxia, headaches, confusion.
Halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, nitrous oxide (Use, Effects, Tox)
Inhaled anesthetics
Myocardial depression, respiratory depression, N/V, Increase cerebral blood flow
Malignant hyperthermia (all but NO)
Halothane toxicity
Hepatotoxicity
Methoxyflurane toxicity
Nephrotoxicity
Enflurane toxicity
Proconvulsant
NO toxicity
Expansion of trapped gas in a body cavity
Thiopental (Class, Use, Effects)
High potency barbiturates used as IV anesthetic
Induction of anesthesia
Rapid redistribution
Decrease cerebral blood flow
Midazolam (Class, Use, Effects)
Benzodiazepine used as IV anesthetic
Choice for endoscopy
Adjunct with gaseous anesthetics and narcotics
Severe postoperative respiratory depression
Decrease in BP
Amnesia
Ketamine (MOA, Use, Effects)
Block NMDA receptor (PCP analog) used as IV anesthetic
Cardiovascular stimulant
Disorientation
Hallucination/bad dreams
Increase cerebral blood flow
Morphine and Fentanyl as IV anesthetics
Adjunct in general anesthesia
Propofol (MOA, Use, Effects)
Potentiates GABAa
IV anesthetic
Used for sedation in ICU
Rapid anesthesia, induction and short procedures
Little postoperative nausea
Procaine, Cocaine, Tetracaine (Class, MOA, Use, Tox)
Ester local anesthetic
Block activated Na channels (most effective in rapidly firing neurons)
Minor surgical procedures, spinal anesthesia
Causes CNS excitation, Hypertension/Hypotension
Lidocaine, Mepivacaine, Bupivacaine (Class, MOA, Use, Tox)
Amide local anesthetic (2 I’s in name)
Block activated Na channels (most effective in rapidly firing neurons)
Minor surgical procedures, spinal anesthesia
Causes CNS excitation, Hypertension/Hypotension
CV toxicity (Bupivacaine)
Arrhythmias (Cocaine)
Succinylcholine (MOA, Use, Tox, Reversal of blockade)
Depolarizing neuromuscular blocker
ACh receptor agonist (sustained depolarization and prevents muscle contraction)
Muscle paralysis in surgery or mechanical ventilation
Hypercalcemia, Hyperkalemia, malignant hyperthermia
Phase I (prolonged depolarization) - no antidote Phase II (repolarization, ACh desensitized) - Cholinesterase inhibitors (Neostigmine)
Tubocurarine, Atracurium, Mivacurium, Pancuronium, Vecuronium, Rocuronium (MOA, Use, Reversal of blockade)
Competitive antagonists at ACh receptors
Nondepolarizing neuromuscular blocker
Cholinesterase inhibitors (Neostigmine, edrophonium)
Dantrolene (MOA, Use)
Prevents Ca release from SR of skeletal muscle
Treatment of MALIGNANT HYPERTHERMIA
Treats neuroleptic malignant syndrome (antipsychotic toxicity)
Bromocriptine, Pramipexole, Ropinirole (MOA, Use)
Dopamine agonists
Used to treat Parkinson’s
Amantadine (MOA, Use, Tox)
Increases dopamine levels
Used in Parkinson’s
Used as antiviral against Influenza A and Rubella
Can cause ataxia
L-DOPA/Carbidopa (MOA, Use, Tox)
L-DOPA can cross BBB and is converted to dopamine
*given with Carbidopa which inhibits PERIPHERAL dopa decarboxylase to isolate effect to CNS
Used in Parkinson’s
Arrhythmias
Dyskinesia with long term use
Selegiline (MOA, Use)
MOA-B blocker (prevent dopamine breakdown)
Adjunct to L-DOPA in Parkinson’s
Entacapone, Tolcapone (MOA, Use)
COMT inhibitors (prevent L-DOPA breakdown)
Used in parkinson
Benztropine (MOA, Use)
Antimuscarinic
Improves tremor and rigidity in Parkinson’s
Memantine (MOA, Use, Tox)
NMDA antagonist (prevents Ca-mediated excitotoxicity)
Used in Alzheimer’s
Dizziness, confusion, hallucinations
Donepezil, Galantamine, Rivastigmine (MOA, Use, Tox)
Acetylcholinesterase inhibitors
Used in Alzheimer’s
Nausea, dizziness, insomnia
Tetrabenazine, Reserpine (MOA, Use)
Inhibit VMAT (limiting dopamine vesicle packaging and release)
Used in Huntington’s
Haloperidol (MOA, Use in Huntington’s)
Dopamine receptor antagonist
Sumatriptan (MOA, Use, Tox)
5-HT1B/1D agonist
(inhibits trigeminal nerve activation, prevents vasoactive peptide release, induces vasoconstriction)
Used in acute migraines and cluster headache
Coronary vasospasm (contraindicated in CAD or Prinzmetal’s angina)
Epinephrine, Brimonidine (MOA, Use, Tox)
alpha-agonists -decrease aqueous humor synthesis
Open angle glaucoma
Mydriasis, blurry, vision, ocular hyperemia, foreign body sensation, allergic reaction/pruritus
Timolol, Betaxolol, Carteolol (MOA, Use, Tox)
Beta-blockers - decrease aqueous humor synthesis
Glaucoma
No pupillary or vision changes
Acetazolamide in eye (MOA, Use, Tox)
Decrease aqueous humor synthesis via inhibition of carbonic anhydrase
Glaucoma
No pupillary or vision changes
Pilocarpine, Carbachol (MOA, Use Tox)
Direct Cholinomimetics - Increase aqueous humor outflow via contraction of ciliary muscle and opening of trabecular meshwork
Glaucoma (USE PILOCARPINE FOR EMERGENCIES)
Miosis and cyclospasm (contraction of ciliary muscle)
Physostigmine, Echothiophate (MOA, Use, Tox)
Indirect Cholinomimetics - Increase aqueous humor outflow via contraction of ciliary muscle and opening of trabecular meshwork
Glaucoma
Miosis and cyclospasm (contraction of ciliary muscle)
Latanoprost (MOA, Use, Tox)
Prostaglandin - PGF2a (increase aqueous humor outflow)
Glaucoma
Darkens color of iris