CNS FINAL Flashcards
What is the class/MOA of Acetylcholine?
Direct-Acting Cholinergic Agonist; acts on muscarinic and nicotinic receptors
What are the indications for Acetylcholine?
Limited clinical userapidly eliminated; used in eye surgery
What are the side effects of Acetylcholine?
Decreases HR, lowers BP, increases gastric acid secretion
What is the class of Bethanechol?
Direct-Acting Cholinergic Agonist
What is the mechanism of action of Bethanechol?
Stimulates smooth muscle in bladder and GI tract
What are the indications for Bethanechol?
Atonic bladder, GI atony
What are the side effects of Bethanechol?
Diaphoresis, salivation, nausea, bronchospasm
What are important notes about Bethanechol?
Contraindicated in bladder/GI obstruction
What is the class of Pilocarpine?
Direct-Acting Cholinergic Agonist
What is the mechanism of action of Pilocarpine?
Stimulates secretions (sweat, tears, saliva); used in glaucoma
What are the indications for Pilocarpine?
Glaucoma, dry mouth
What are the side effects of Pilocarpine?
Sweating, excessive salivation, risk of systemic effects
What are important notes about Pilocarpine?
First-line for acute glaucoma attacks
What is the class of Cevimeline?
Direct-Acting Cholinergic Agonist
What is the mechanism of action of Cevimeline?
Selective for muscarinic receptors; used for dry mouth
Sjorgrens
What are the indications for Cevimeline?
Xerostomia due to radiation or Sjogren’s syndrome
What are the side effects of Cevimeline?
Fewer systemic effects than pilocarpine (preferred over Pilocarpine)
Sweating, salivating, possible systemic effects
What is the class of Physostigmine?
Reversible Acetylcholinesterase Inhibitor
What is the mechanism of action of Physostigmine?
Reverses CNS effects of anticholinergic toxicity
Acetylcholinesterase inhibitor
What are the indications for Physostigmine?
Reversal of anticholinergic overdose
What are the side effects of Physostigmine?
Bradycardia, seizures, salivation, bronchospasm
What are important notes about Physostigmine?
Used for atropine overdose
What is the class of Neostigmine?
Reversible Acetylcholinesterase Inhibitor
What is the mechanism of action of Neostigmine?
Enhances skeletal muscle contraction
What are the indications for Neostigmine?
Myasthenia gravis, neuromuscular blockade reversal
What are the side effects of Neostigmine?
GI distress, salivation, bronchospasm
myasthenia gravis. It can also reverse the effects of anesthesia
What is the class of Pyridostigmine?
Reversible Acetylcholinesterase Inhibitor
What is the mechanism of action of Pyridostigmine?
Long-acting acetylcholinesterase inhibitor for myasthenia gravis
What are the indications for Pyridostigmine?
Chronic myasthenia gravis management
What are the side effects of Pyridostigmine?
Similar to neostigmine, but longer duration
What is the class of Donepezil?
Acetylcholinesterase Inhibitor
What is the mechanism of action of Donepezil?
Prevents breakdown of acetylcholine to slow Alzheimer’s progression
What are the indications for Donepezil?
Mild to moderate Alzheimer’s disease
What are the side effects of Donepezil?
Nausea, diarrhea, syncope, bradycardia
What are important notes about Donepezil?
Take at bedtime; caution with bradycardia
What is the class of Rivastigmine?
Acetylcholinesterase Inhibitor
What is the mechanism of action of Rivastigmine?
Prevents breakdown of acetylcholine, available as patch or oral
What are the indications for Rivastigmine?
Mild to moderate Alzheimer’s disease
What are the side effects of Rivastigmine?
GI distress, weight loss, muscle wasting
What is the class of Galantamine?
Acetylcholinesterase Inhibitor
What is the mechanism of action of Galantamine?
Prevents breakdown of acetylcholine to slow Alzheimer’s progression
What are the indications for Galantamine?
Mild to moderate Alzheimer’s disease
What are the side effects of Galantamine?
GI distress, weight loss, dizziness
What are important notes about Galantamine?
Derived from plants; marketed as natural
What is the class of Memantine?
NMDA Receptor Antagonist
Alzheimer’s
What is the mechanism of action of Memantine?
Blocks excitotoxic effects of glutamate to slow cognitive decline
What are the indications for Memantine?
Moderate to severe Alzheimer’s disease
What are the side effects of Memantine?
Dizziness, headache, rare seizures
What are important notes about Memantine?
Often combined with acetylcholinesterase inhibitors
What is the class of Lecanemab?
Monoclonal Antibody for Alzheimer’s
What is the mechanism of action of Lecanemab?
Monoclonal antibody that reduces amyloid plaque in Alzheimer’s
What are the indications for Lecanemab?
Early-stage Alzheimer’s disease with amyloid plaques
What are the side effects of Lecanemab?
Brain microhemorrhages, infusion reactions
What is the mechanism of action of Diazepam?
Binds to GABA receptors, enhancing inhibitory effects to reduce neuron firing
What are the indications for Diazepam?
Seizures, anxiety, muscle spasms, status epilepticus
What are the side effects of Diazepam?
Drowsiness, dizziness, respiratory depression, tolerance development
What are important notes about Diazepam?
Used mainly for acute seizure management; tolerance can develop
What is the class of Levetiracetam?
SV2A Binding Anticonvulsant
What is the mechanism of action of Levetiracetam?
Binds synaptic vesicle protein 2A, reducing neurotransmitter release
What are the indications for Levetiracetam?
Focal seizures, generalized tonic-clonic seizures, myoclonic seizures
What are the side effects of Levetiracetam?
Mood alterations, dizziness, fatigue
What are important notes about Levetiracetam?
Well absorbed orally; primarily excreted unchanged in urine
What is the class of Carbamazepine?
Sodium Channel Blocker
What is the mechanism of action of Carbamazepine?
Blocks Na+ channels, reducing neuronal excitability
What are the indications for Carbamazepine?
Partial seizures, generalized tonic-clonic seizures, trigeminal neuralgia, bipolar disorder
What are the side effects of Carbamazepine?
Hyponatremia, dizziness, drowsiness, aplastic anemia, Stevens-Johnson Syndrome
What are important notes about Carbamazepine?
Induces its own metabolism; avoid in HLA-B1505 positive Asians due to SJS risk
What is the class of Phenytoin?
Hydantoin
What is the mechanism of action of Phenytoin?
Stabilizes hyper-excitable neurons by selectively inhibiting Na+ channels
What are the indications for Phenytoin?
Generalized tonic-clonic seizures, partial seizures, status epilepticus
What are the side effects of Phenytoin?
Gingival hyperplasia, sedation, dizziness, ataxia, Stevens-Johnson Syndrome
What are important notes about Phenytoin?
Highly protein-bound; many drug interactions; nonlinear kinetics require careful dosing
What is the class of Ethosuximide?
Calcium Channel Blocker
What is the mechanism of action of Ethosuximide?
Blocks T-type Ca++ channels to suppress nerve transmission in motor cortex
What are the indications for Ethosuximide?
Generalized absence seizures
What are the side effects of Ethosuximide?
GI distress, dizziness, rash, weight loss
What is the class of Perampanel?
AMPA Receptor Antagonist
What is the mechanism of action of Perampanel?
Selective AMPA receptor antagonist that reduces excitatory neurotransmission
What are the indications for Perampanel?
Focal seizures, adjunct for generalized tonic-clonic seizures
What are the side effects of Perampanel?
Aggression, hostility, irritability, homicidal ideation
What are important notes about Perampanel?
Long half-life allows once-daily dosing; psychiatric side effects require monitoring
What is the mechanism of action of Phenobarbital?
Increases seizure threshold by enhancing GABA-mediated inhibition
What are the indications for Phenobarbital?
Seizures, sedation, status epilepticus
What are the side effects of Phenobarbital?
Sedation, drowsiness, confusion, CNS depression
What are important notes about Phenobarbital?
Long half-life; tolerance may develop; gradual taper needed when discontinuing
What is the class of Cenobamate?
Sodium Channel Blocker & GABA Modulator
What is the mechanism of action of Cenobamate?
Blocks voltage-gated Na+ channels and modulates GABAA receptors
What are the indications for Cenobamate?
Focal seizures
What are the side effects of Cenobamate?
Fatigue, headache, dizziness, diplopia
What is the class of Valproic Acid (VPA)?
Multiple MOA Anticonvulsant
What are the indications for Valproic Acid (VPA)?
All seizure types, bipolar disorder, migraine prophylaxis
What are the side effects of Valproic Acid (VPA)?
Tremors, GI distress, weight gain, hepatotoxicity, alopecia, sedation
What are important notes about Valproic Acid (VPA)?
Avoid in pregnancy due to teratogenicity; interacts with multiple drugs; monitor LFTs
What is the class of Lamotrigine?
Sodium Channel Blocker
What is the mechanism of action of Lamotrigine?
Blocks Na+ channels, stabilizes membranes, prevents glutamate & aspartate release
What are the indications for Lamotrigine?
Partial seizures, generalized tonic-clonic seizures, bipolar disorder maintenance
What are the side effects of Lamotrigine?
Dizziness, headache, double vision, ataxia
What are important notes about Lamotrigine?
Risk of Stevens-Johnson Syndrome; titrate dose slowly; avoid rechallenge if rash develops
Anti epileptic
What is the class of Topiramate?
Multiple MOA Anticonvulsant
What is the mechanism of action of Topiramate?
Blocks Na+ channels, augments GABA activity, inhibits glutamate
What are the indications for Topiramate?
Adjunct therapy for seizures, migraine prophylaxis
What are the side effects of Topiramate?
Fatigue, difficulty concentrating, speech problems, weight loss, kidney stones
What are important notes about Topiramate?
Increase hydration (kidney stones); interacts with CYP
What is the class of Cannabidiol (Epidolex)?
Unknown MOA Anticonvulsant
What are the indications for Cannabidiol (Epidolex)?
Seizures from Lennox-Gastaut, Dravet, or tuberous sclerosis syndromes
What are the side effects of Cannabidiol (Epidolex)?
Drowsiness, diarrhea, vomiting, decreased appetite, increased LFTs (with VPA)
What are important notes about Cannabidiol (Epidolex)?
No psychoactive effects; only available as a liquid; interacts with multiple drugs
What is the class of Fenfluramine (Fentepla)?
5-HT2 Receptor Agonist
Dravet syndrome seizure
What is the mechanism of action of Fenfluramine (Fentepla)?
Exact MOA unknown for seizures; originally used for obesity
What are the indications for Fenfluramine (Fentepla)?
Seizures from Dravet syndrome
What are the side effects of Fenfluramine (Fentepla)?
Drowsiness, lethargy, reduced appetite, weight loss
Possibly valvular heart disease, or pulmonary htn
What are important notes about Fenfluramine (Fentepla)?
Requires bi-annual echocardiograms due to risk of valvular heart disease
What is the class of Gabapentin (Neurontin)?
Unknown MOA Anticonvulsant
What is the mechanism of action of Gabapentin (Neurontin)?
Increases GABA release, inhibits seizure discharges, inhibits pain transmission
What are the indications for Gabapentin (Neurontin)?
Adjunct for partial seizures, RLS, neurogenic pain
What are the side effects of Gabapentin (Neurontin)?
Sedation, dizziness, ataxia, fatigue, weight gain
What are important notes about Gabapentin (Neurontin)?
No major drug interactions; requires slow titration to avoid sedation
What is the class of Rufinamide (Banzel)?
Sodium Channel Blocker
What is the mechanism of action of Rufinamide (Banzel)?
Acts on Na+ channels to reduce excitability
What are the indications for Rufinamide (Banzel)?
Add-on therapy for Lennox-Gastaut syndrome
What are the side effects of Rufinamide (Banzel)?
Shortened QT intervals, dizziness, fatigue
What is the class of Carbidopa/Levodopa (Sinemet)?
Dopamine Precursor
What is the mechanism of action of Carbidopa/Levodopa (Sinemet)?
Levodopa is converted to dopamine in the CNS; Carbidopa prevents peripheral metabolism
What are the indications for Carbidopa/Levodopa (Sinemet)?
Parkinson’s disease
What are the side effects of Carbidopa/Levodopa (Sinemet)?
Nausea, vomiting, hypotension, arrhythmias, anxiety, hallucinations
What are important notes about Carbidopa/Levodopa (Sinemet)?
Gold standard treatment; effects diminish over time; contraindicated in malignant melanoma
What is the class of Selegiline (Eldepryl)?
MAO-B Inhibitor
What is the mechanism of action of Selegiline (Eldepryl)?
Prevents dopamine metabolism in the brain
What are the indications for Selegiline (Eldepryl)?
Adjunct therapy in Parkinson’s disease
What are the side effects of Selegiline (Eldepryl)?
Hypertension (if over 10 mg/day), insomnia, nausea
What is the class of Rasagiline (Azilect)?
MAO-B Inhibitor
What is the mechanism of action of Rasagiline (Azilect)?
Blocks metabolism of dopamine, improving quality of life and slowing disease progression
What are the indications for Rasagiline (Azilect)?
Parkinson’s disease
What are the side effects of Rasagiline (Azilect)?
Orthostatic hypotension, headache, dyskinesia
What are important notes about Rasagiline (Azilect)?
Potentiated by CYP1A2 inhibitors; avoid tyramine-rich foods
What is the class of Pramipexole (Mirapex)?
Dopamine Agonist
What is the mechanism of action of Pramipexole (Mirapex)?
Selective D2 receptor agonist
What are the indications for Pramipexole (Mirapex)?
Parkinson’s disease, restless leg syndrome
What are the side effects of Pramipexole (Mirapex)?
Nausea, dizziness, hallucinations, somnolence, hypotension
What are important notes about Pramipexole (Mirapex)?
Used as monotherapy in early disease; combined with levodopa in later stages
What is the class of Ropinirole (Requip)?
Dopamine Agonist
What is the mechanism of action of Ropinirole (Requip)?
D2/D3 receptor agonist
What are the indications for Ropinirole (Requip)?
Parkinson’s disease, restless leg syndrome
What are the side effects of Ropinirole (Requip)?
Nausea, dizziness, daytime somnolence, hypotension
What are important notes about Ropinirole (Requip)?
Used as monotherapy in young patients or with Sinemet to reduce levodopa needs
What is the class of Apomorphine (Apokyn)?
Dopamine Agonist
What is the mechanism of action of Apomorphine (Apokyn)?
Non-ergot D1/D2 dopamine agonist
What are the indications for Apomorphine (Apokyn)?
Treatment of ‘off’ episodes in Parkinson’s disease
What are the side effects of Apomorphine (Apokyn)?
Hypotension, nausea, hallucinations
What are important notes about Apomorphine (Apokyn)?
Requires antiemetic (Tigan); administered subcutaneously
What is the class of Tolcapone (Tasmar)?
COMT Inhibitor
What is the mechanism of action of Tolcapone (Tasmar)?
Blocks peripheral levodopa metabolism, increasing CNS dopamine levels
What are the indications for Tolcapone (Tasmar)?
Parkinson’s disease (adjunct to levodopa)
What are the side effects of Tolcapone (Tasmar)?
Liver toxicity, diarrhea, dyskinesia
What are important notes about Tolcapone (Tasmar)?
Black box warning for hepatotoxicity; requires liver function monitoring
What is the class of Entacapone (Comtan)?
COMT Inhibitor
What is the mechanism of action of Entacapone (Comtan)?
Prevents breakdown of levodopa in the periphery
What are the indications for Entacapone (Comtan)?
Parkinson’s disease (adjunct to levodopa)
What are the side effects of Entacapone (Comtan)?
Dyskinesia, nausea, diarrhea
What are important notes about Entacapone (Comtan)?
Often combined with carbidopa/levodopa to extend its duration
What is the class of Istradefylline (Nourianz)?
Adenosine A2A Receptor Antagonist
What is the mechanism of action of Istradefylline (Nourianz)?
Reduces frequency of ‘off’ episodes by blocking adenosine receptors
What are the indications for Istradefylline (Nourianz)?
Adjunct to Sinemet in Parkinson’s disease
What are the side effects of Istradefylline (Nourianz)?
Dyskinesia, nausea, hallucinations, impulse control issues
What is the class of Amantadine (Symmetrel)?
Glutamate Agonist
What is the mechanism of action of Amantadine (Symmetrel)?
Promotes dopamine release and inhibits reuptake
What are the indications for Amantadine (Symmetrel)?
Parkinson’s disease, rigidity, akinesia
What are the side effects of Amantadine (Symmetrel)?
Insomnia, dizziness, hallucinations, livedo reticularis
What are important notes about Amantadine (Symmetrel)?
Used as an add-on therapy for Parkinson’s symptoms (last ditch)
Which medication could interfere with the effectiveness of Sinemet in a Parkinson’s patient?
Metoclopramide
Which combination of drugs is appropriate for a 75-year-old with moderate Parkinson’s disease?
Levodopa, Carbidopa, Entacapone
What common side effect should you caution about when prescribing Bethanechol?
Diaphoresis, bronchospasm, nausea
Which agent is a first-line treatment for a 79-year-old patient with Alzheimer’s dementia?
Donepezil
Which drug is most appropriate for a child with absence seizures affecting school performance?
Ethosuximide (Zarontin)
For a 28-year-old woman with generalized seizures planning pregnancy, what should be done?
Consider switching to Lamotrigine (Lamictal)
Which AED is least likely to have a drug interaction with Carbamazepine in a focal seizure patient?
Levetiracetam (Keppra)
Which AED increases the risk of hyponatremia in a 62-year-old with HTN on HCTZ?
Carbamazepine (Tegretol)