Nervous System Drugs - Classes Flashcards
Cyclobenzaprine
Centrally acting skeletal muscle relaxant
Structurally related to TCAs, similar anticholinergic side effects
Propofol
IV anesthetic
Potentiates GABAa
Benztropine
Antimuscarinic: Improves tremor and rigidity but has little effect on bradykinesia in Parkinson disease
Rocuronium
Non-depolarizing NM blocking drug:
Competitive antagonists (compete with ACh for receptors)
Reversal: Neostigmine, edrophonium, other AChE inhibitors (must be given with atropine to prevent muscarinic effects such as bradycardia)
Secobarbital
Bariturate: Faciliate GABAa action by increasing duration of Cl channel opening, thus decreasing neuron firing
Tacrine
AChE inhibitor
Alzheimer disease drug
Dantrolene
Prevents release of Ca2+ from SR of skeletal muscle by binding to the ryanodine receptor
Uses:
Malignant hyperthermia
Neuroleptic malignant syndrome (NMS)
Amantadine
Increases DA release and decreases DA reuptake
Parkinson drug
Loperamide
Act as agonists at opioid receptors to modulate synaptic transmission - open K+ channels, close Ca2+ channels → decrease synaptic transmission
Inhibit release of:
- ACh
- NE
- 5-HT
- Glutamate
- Substance P
Butorphanol
k-opioid receptor agonist
mu-opioid receptor partial agonist
Produces analgesia
Isoflurane
Inhaled anesthetic
Cocaine
Local anesthetic
Ester (one eyed ester)
Thiopental
Bariturate: Faciliate GABAa action by increasing duration of Cl channel opening, thus decreasing neuron firing
IV anesthetic (induction of anesthesia)
Eszopiclone
Non-BDZ hypnotic:
Act via BZ1 subtype of the GABA receptor
Effects reversed by flumazenil
Sleep cycle less affected as compared with BDZs
Sumatriptan
5-HT1B/1D agonist:
Inhibits trigeminal nerve activation
Prevent vasoactive peptide release
Induce vasoconstriction
Zaleplon
Non-BDZ hypnotic:
Act via BZ1 subtype of the GABA receptor
Effects reversed by flumazenil
Sleep cycle less affected as compared with BDZs
Tetracaine
Local anesthetic
Ester (one eyed ester)
Riluzole
Decreases glutamate excitotoxicity via an unclear mechanism
Treatment for ALS (modestly improves survival)
Chlordiazepoxide
Benzodiazepine: Facilitate GABAa action by increasing frequency of Cl channel opening
Desflurane
Inhaled anesthetic
Tubocurarine
Non-depolarizing NM blocking drug:
Competitive antagonists (compete with ACh for receptors)
Reversal: Neostigmine, edrophonium, other AChE inhibitors (must be given with atropine to prevent muscarinic effects such as bradycardia)
Rivastigmine
AChE inhibitor
Alzheimer disease drug
Morphine
Act as agonists at opioid receptors to modulate synaptic transmission - open K+ channels, close Ca2+ channels → decrease synaptic transmission
Inhibit release of:
- ACh
- NE
- 5-HT
- Glutamate
- Substance P
Fentanyl
Opioid: Used with other CNS depressants during general anesthesia
Zolpidem
Non-BDZ hypnotic:
Act via BZ1 subtype of the GABA receptor
Effects reversed by flumazenil
Sleep cycle less affected as compared with BDZs
Codeine
Act as agonists at opioid receptors to modulate synaptic transmission - open K+ channels, close Ca2+ channels → decrease synaptic transmission
Inhibit release of:
- ACh
- NE
- 5-HT
- Glutamate
- Substance P
Galantamine
AChE inhibitor
Alzheimer disease drug
Methadone
Act as agonists at opioid receptors to modulate synaptic transmission - open K+ channels, close Ca2+ channels → decrease synaptic transmission
Inhibit release of:
- ACh
- NE
- 5-HT
- Glutamate
- Substance P
Donepezil
AChE inhibitor
Alzheimer disease drug
Trihexyphenidyl
Antimuscarinic: Improves tremor and rigidity but has little effect on bradykinesia in Parkinson disease
Arylcyclohexylamines: Ketamine
IV anesthetic: PCP analog that acts as a dissociative anesthetic
Block NMDA receptors
CV stimulant
Diazepam
Benzodiazepine: Facilitate GABAa action by increasing frequency of Cl channel opening
Name the benzodiazepines that are
metabolized outside the liver
(no active metabolites; better in elderly patients)
Oxazepam
Temazepam
Lorazepam
Clonazepam
Oxycodone
Act as agonists at opioid receptors to modulate synaptic transmission - open K+ channels, close Ca2+ channels → decrease synaptic transmission
Inhibit release of:
- ACh
- NE
- 5-HT
- Glutamate
- Substance P
Entacapone
COMA inhibitor: Prevents peripheral L-DOPA degradation to 3-O-methyldopa (3-OMD) by inhibiting COMT
Parkinson drug
Meperidine
Act as agonists at opioid receptors to modulate synaptic transmission - open K+ channels, close Ca2+ channels → decrease synaptic transmission
Inhibit release of:
- ACh
- NE
- 5-HT
- Glutamate
- Substance P
Benzocaine
Local anesthetic
Ester (one eyed ester)
Ramelteon
Melatonin receptor agonist:
Binds MT1 and MT2 in suprachiasmatic nucleus
Carbidopa
Peripheral DOPA decarboxylase inhibitor: Blocks peripheral conversion of L-DOPA to dopamine by inhibiting DOPA decarboxylase
Parkinson drug
Rasagiline
Selective MAO-B inhibitor: Blocks CENTRAL (post-BBB) conversion of DA to DOPAC
Parkinson drug
Pentobarbital
Bariturate: Faciliate GABAa action by increasing duration of Cl channel opening, thus decreasing neuron firing
Tramadol
Very weak opioid agonist
Also inhibits 5-HT and NE reuptake (works on multiple neurotransmitters
Midazolam
Benzodiazepine: Facilitate GABAa action by increasing frequency of Cl channel opening
IV anesthetic
Name the short-acting benzodiazepines
Less daytime side effects
Higher addictive potential
Alprazolam
Trizolam
Oxazepam
Midazolam
Sevoflurane
Inhaled anesthetic
Tolcapone
COMT inhibitor: Prevents peripheral AND CENTRAL L-DOPA degradation to 3-O-methyldopa (3-OMD) by inhibiting COMT
Parkinson drug
Lidocaine
Local anesthetic
Amide (one eyed ester)
Pentazocine
k-opioid receptor agonist
mu-opioid receptor weak antagonist/partial agonsit
Diphenoxylate
Act as agonists at opioid receptors to modulate synaptic transmission - open K+ channels, close Ca2+ channels → decrease synaptic transmission
Inhibit release of:
- ACh
- NE
- 5-HT
- Glutamate
- Substance P
Suvorexant
Orexin (hypocretin) receptor antagonist
Pramipexol
Dopamine agonist (non-ergot - preferred)
Parkinson drug
Vecuronium
Non-depolarizing NM blocking drug:
Competitive antagonists (compete with ACh for receptors)
Reversal: Neostigmine, edrophonium, other AChE inhibitors (must be given with atropine to prevent muscarinic effects such as bradycardia)
Ropinirole
Dopamine agonist (non-ergot - preferred)
Parkinson drug
Treatment and MOA for malignant hyperthermia
Dantrolene: Ryanodine receptor antagonist → decreases calcium release from SR
Bupivacaine
Local anesthetic
Amide (one eyed ester)
Reserpine
Vesicular monoamine transporter (VMAT) inhibitor: Decrease DA vesicle packaging and release
Huntington disease drug
Phenobarbital
Bariturate: Faciliate GABAa action by increasing duration of Cl channel opening, thus decreasing neuron firing
Enflurane
Inhaled anesthetic
Dextromethorphan
Act as agonists at opioid receptors to modulate synaptic transmission - open K+ channels, close Ca2+ channels → decrease synaptic transmission
Inhibit release of:
- ACh
- NE
- 5-HT
- Glutamate
- Substance P
Succinylcholine
Depolarizing NM blocking drug:
Strong ACh receptor agonist → produces sustained depolarization and prevents muscle contraction
Bromocriptine
Dopamine agonist (ergot)
Parkinson drug
Pancuronium
Non-depolarizing NM blocking drug:
Competitive antagonists (compete with ACh for receptors)
Reversal: Neostigmine, edrophonium, other AChE inhibitors (must be given with atropine to prevent muscarinic effects such as bradycardia)
Atracurium
Non-depolarizing NM blocking drug:
Competitive antagonists (compete with ACh for receptors)
Reversal: Neostigmine, edrophonium, other AChE inhibitors (must be given with atropine to prevent muscarinic effects such as bradycardia)
Methoxyflurane
Inhaled anesthetic
Mepivacaine
Local anesthetic
Amide (one eyed ester)
Tetrabenazine
Vesicular monoamine transporter (VMAT) inhibitor: Decrease DA vesicle packaging and release
Huntington disease drug
Fentanyl
Act as agonists at opioid receptors to modulate synaptic transmission - open K+ channels, close Ca2+ channels → decrease synaptic transmission
Inhibit release of:
- ACh
- NE
- 5-HT
- Glutamate
- Substance P
Mivacurium
Non-depolarizing NM blocking drug:
Competitive antagonists (compete with ACh for receptors)
Reversal: Neostigmine, edrophonium, other AChE inhibitors (must be given with atropine to prevent muscarinic effects such as bradycardia)
Memantine
NMDA receptor antagonist
Helps prevent excitotoxicity (mediated by Ca2+)
Alzheimer disease drug
Selegiline
Selective MAO-B inhibitor: Blocks conversion of DA to DOPAC
Parkinson drug
Procaine
Local anesthetic: Blocks Na+ channels by binding to specific receptors on inner portion of channel
Ester (one eyed ester)
Haloperidol
D2 receptor antagonist
Huntington disease drug
Nitrous oxide (N2O)
Inhaled anesthetic
Low blood/lipid solubility
Fast induction; Low potency
Treat BDZ OD with ___. What is the mechanism?
Flumazenil: Competitive antagonist at GABAa receptor
Baclofen
Activates GABAB receptors at spinal cord level, inducing skeletal muscle relaxation
Halothane
Inhaled anesthetic
High lipid/blood solubility
Slow induction; high potency