CNS Drugs Flashcards
List the class and mechanism of Levodopa (L-DOPA) (Dopar)
Class: Dopamine precursor;
Mechanism: Oral, absorbed in small bowel, rapidly converted to DA by peripheral AAD
List the class and mechanism of Carbidopa (Lodosyn)
Class: AAD (aromatic amino acid decarboxylase) inhibitor;
Mechanism: Inhibits peripheral conversion of L-DOPA to dopamine; does not cross BBB
List the class and mechanism of Pergolide (Permax)
Class: Ergot derivative;
Mechanism: —
List the class and mechanism of Bromocriptine (Parlodel)
Class: Ergot derivative;
Mechanism: D2 agonist, D1 antagonist
List the class and mechanism of Pramipexole (Mirapex)
Class: Non-ergot DA receptor agonist;
Mechanism: D2 agonist
List the class and mechanism of Ropinorole (Requip)
Class: Non-ergot DA receptor agonist;
Mechanism: D2 agonist
List the class and mechanism of Rotigotine (Neupro)
Class: Non-ergot DA receptor agonist;
Mechanism: D2 agonist
List the class and mechanism of Apomorphine (Apokyn)
Class: Non-ergot DA receptor agonist;
Mechanism: D2 agonist
List the class and mechanism of Entacapone (Comtan)
Class: COMT inhibitor;
Mechanism: Prevents breakdown of DA, prolongs half-life of levodopa
List the class and mechanism of Tolcapone (Tasmar)
Class: COMT inhibitor;
Mechanism: Prevents breakdown of DA, prolongs half-life of levodopa
List the class and mechanism of Selegiline (Eldepryl)
Class: MAO-B inhibitor;
Mechanism: Prevents breakdown of DA
List the class and mechanism of Rasagiline (Azilect)
Class: ;
Mechanism:
List the class and mechanism of Benztropine (Cogentin)
Class: Anticholinergics;
Mechanism: —
List the class and mechanism of Biperiden (Akineton)
Class: Anticholinergics;
Mechanism: —
List the class and mechanism of Trihexyphenidyl (Artane)
Class: Anticholinergics;
Mechanism: —
List the class and mechanism of Procyclidine (Kemadrin)
Class: Anticholinergics;
Mechanism: —
List the class and mechanism of Ethopropazine (Parsidol)
Class: Anticholinergics;
Mechanism: —
List the class and mechanism of Amantadine (Symmetrel)
Class: Influenza A anti-viral;
Mechanism: Dopaminergic, anticholinergic, anti-NMDA
List the class and mechanism of Deep brain stimulation
Class: Surgery;
Mechanism: Hits subthalamic nucleus
List the class and mechanism of Tetrabenazine (Xenazine)
Class: —;
Mechanism: Dopamine depletion, VMAT2 inhibitor
List the class and mechanism of Dantrolene (Dantrium)
Class: —;
Mechanism: Muscle relaxant
List the class and mechanism of Riluzole (Rilutek)
Class: ;
Mechanism: Kaninate and NDMA (Glu receptors) antagonist; may inhibit Na channels and GPCRs
List the class and mechanism of Baclofen (Lioresal)
Class: ;
Mechanism: GABA-B agonist
List the class and mechanism of Tizanidine (Zanaflex)
Class: ;
Mechanism: α2 agonist
List the class and mechanism of Chlorpromazine (Thorazine)
Class: First Generation Antipsychotic;
Mechanism: Catalepsy (trance, muscle rigidity, lack of voluntary movement)
List the class and mechanism of Haloperidol (Haldol)
Class: First Generation Antipsychotic;
Mechanism: Catalepsy (trance, muscle rigidity, lack of voluntary movement)
List the class and mechanism of Fluphenazine (Prolixin)
Class: First Generation Antipsychotic;
Mechanism: Catalepsy (trance, muscle rigidity, lack of voluntary movement)
List the class and mechanism of Perphenazine (Trilafon)
Class: First Generation Antipsychotic;
Mechanism: Catalepsy (trance, muscle rigidity, lack of voluntary movement)
List the class and mechanism of Loxapine (Loxitane)
Class: First Generation Antipsychotic;
Mechanism: Catalepsy (trance, muscle rigidity, lack of voluntary movement)
List the class and mechanism of Trifluoperazine (Stelazine)
Class: First Generation Antipsychotic;
Mechanism: Catalepsy (trance, muscle rigidity, lack of voluntary movement)
List the class and mechanism of Thioridazine (Mellaril)
Class: First Generation Antipsychotic;
Mechanism: Catalepsy (trance, muscle rigidity, lack of voluntary movement)
List the class and mechanism of Thiothixene (Navane)
Class: First Generation Antipsychotic;
Mechanism: Catalepsy (trance, muscle rigidity, lack of voluntary movement)
List the class and mechanism of Clozapine (Clozaril)
Class: Second Gen Antipsychotic (tricyclic);
Mechanism: D2 receptor antagonist, 5HT2 receptor antagonist
List the class and mechanism of Olanzapine (Zyprexa)
Class: Second Gen Antipsychotic (tricyclic);
Mechanism: D2 receptor antagonist, 5HT2 receptor antagonist
List the class and mechanism of Quetiapine (Seroquel)
Class: Second Gen Antipsychotic (tricyclic);
Mechanism: D2 receptor antagonist, 5HT2 receptor antagonist
List the class and mechanism of Risperidone (Risperdal)
Class: Second Gen Antipsychotic (non-tricyclic);
Mechanism: D2 receptor antagonist, 5HT2 receptor antagonist
List the class and mechanism of Paliperidone (Invega)
Class: Second Gen Antipsychotic (non-tricyclic);
Mechanism: D2 receptor antagonist, 5HT2 receptor antagonist
List the class and mechanism of Ziprazidone (Geodon)
Class: Second Gen Antipsychotic (non-tricyclic);
Mechanism: D2 receptor antagonist, 5HT2 receptor antagonist
List the class and mechanism of Aripiprazole (Abilify)
Class: Second Gen Antipsychotic (non-tricyclic);
Mechanism: Partial D2 and D3 receptor agonist, partial 5HT1a agonist, 5HT2a antagonist
List the class and mechanism of Asenapine
Class: Atypical Antipsychotic;
Mechanism: complicated, but involves D2 antagonism and 5HT partial agonism
List the class and mechanism of Lurazidone
Class: Atypical Antipsychotic;
Mechanism: complicated, but involves D2 antagonism and 5HT partial agonism
List the class and mechanism of Iloperidone
Class: Atypical Antipsychotic;
Mechanism: complicated, but involves D2 antagonism and 5HT partial agonism
List the class and mechanism of Tranylcypromine (Parnate)
Class: MAOI;
Mechanism: Irreversibly inhibit both MAO-A and MAO-B
List the class and mechanism of Phenelzine (Nardil)
Class: MAOI;
Mechanism: Irreversibly inhibit both MAO-A and MAO-B
List the class and mechanism of Desipramine (Norpramin)
Class: Tricyclic;
Mechanism: Block reuptake of NE or 5-HT at varying potencies and selectivity; also variably block muscarinic, a-adrenergic, dopamine, and histamine receptors
List the class and mechanism of Imipramine (Tofranil)
Class: Tricyclic;
Mechanism: Block reuptake of NE or 5-HT at varying potencies and selectivity; also variably block muscarinic, a-adrenergic, dopamine, and histamine receptors
List the class and mechanism of Amitriptyline (Elavil)
Class: Tricyclic;
Mechanism: Block reuptake of NE or 5-HT at varying potencies and selectivity; also variably block muscarinic, a-adrenergic, dopamine, and histamine receptors
List the class and mechanism of Nortriptyline (Pamelor)
Class: Tricyclic;
Mechanism: Block reuptake of NE or 5-HT at varying potencies and selectivity; also variably block muscarinic, a-adrenergic, dopamine, and histamine receptors
List the class and mechanism of Fluoxetine (Prozac)
Class: SSRI;
Mechanism: Inhibit reuptake of 5-HT (and NE to lesser extent)
List the class and mechanism of Paroxetine (Paxil)
Class: SSRI;
Mechanism: Inhibit reuptake of 5-HT (and NE to lesser extent)
List the class and mechanism of Sertraline (Zoloft)
Class: SSRI;
Mechanism: Inhibit reuptake of 5-HT (and NE to lesser extent)
List the class and mechanism of Escitalopram (Lexapro)
Class: SSRI;
Mechanism: Inhibit reuptake of 5-HT (and NE to lesser extent)
List the class and mechanism of Citalopram (Celexa)
Class: SSRI;
Mechanism: Inhibit reuptake of 5-HT (and NE to lesser extent)
List the class and mechanism of Duloxetine (Cymbalta)
Class: SNRI;
Mechanism: Inhibits reuptake of 5-HT and NE
List the class and mechanism of Venlafaxine (Effexor)
Class: SNRI;
Mechanism: Inhibits reuptake of 5-HT and NE
List the class and mechanism of Bupropion (Wellbutrin)
Class: Atypical;
Mechanism: Blocks DA and NE reuptake
List the class and mechanism of Mirtazapine (Remeron)
Class: Atypical;
Mechanism: 5HT2a antagonists; also inhibit 5HT reuptake
List the class and mechanism of Lithium
Class: —;
Mechanism: Unknown; lithium depletes secondary messengers IP3 and DAG, important in a-adrenergic and muscarinic-cholinergic transmission
List the class and mechanism of alcohol / ethanol
Class: ;
Mechanism: GABA-A agonist; binds to α subunit
List the class and mechanism of methyl alochol
Class: poison;
Mechanism: metabolized to formaldehyde and formic acid
List the class and mechanism of ethylene glycol
Class: poison;
Mechanism: metabolized to oxalic acid
List the class and mechanism of isopropyl alcohol
Class: poison;
Mechanism:
List the class and mechanism of barbiturates
Class: ;
Mechanism: GABA-A agonist
List the class and mechanism of benzos
Class: ;
Mechanism: GABA-A agonist
List the class and mechanism of Flunitrazepam
Class: benzodiazepine;
Mechanism: GABA-A agonist
List the class and mechanism of anesthetics
Class: ;
Mechanism:
List the class and mechanism of inhalants
Class: ;
Mechanism: GABA-A agonist
List the class and mechanism of Aliphatic nitrites
Class: inhalant;
Mechanism:
List the class and mechanism of Disulfiram (Antabuse)
Class: ;
Mechanism: Inhibits aldehyde dehydrogenase, causing acetaldehyde accumulation
List the class and mechanism of Fomepizole (Antizol)
Class: —;
Mechanism: Blocks alcohol dehydrogenase
List the class and mechanism of N-acetylcysteine (Mucomyst)
Class: Antioxidant;
Mechanism: Supplies sulfhydryl groups to glutathione; improves microcirculation, provides anti-inflammatory effect
List the class and mechanism of Cocaine
Class: CNS stimulant;
Mechanism: Blocks reuptake of dopamine, norepinephrine, and serotonin
List the class and mechanism of Amphetamines (Benzadrine)
Class: ;
Mechanism: Indirect sympathomimetic (release biologic amines from nerve terminals in periphery and in CNS); dopamine most important
List the class and mechanism of Methyxanthines
Class: ;
Mechanism: Antagonist at adenosine “purinergic” receptors
List the class and mechanism of Theophylline
Class: methyxanthine;
Mechanism: Antagonist at adenosine “purinergic” receptors
List the class and mechanism of Nicotine
Class: ;
Mechanism: activates nAChRs on VTA dopamine neurons leading to increased DA release in nucleus accumbens and prefrontal cortex
List the class and mechanism of Heroin
Class: opioid;
Mechanism: Mu-opioid receptor agonist
List the class and mechanism of Nalmefene (Revex)
Class: Opiod antagonist;
Mechanism: —
List the class and mechanism of LSD
Class: Schedule I Hallucinogen, indole alkyl amine;
Mechanism: Agonist at 5HT2A receptors on Raphe cell body –> inhibition of Raphe Nuclei firing –> increased sensory input; partial dopamine agonist
List the class and mechanism of Mescaline
Class: Schedule I Hallucinogen, phenyethylamine ;
Mechanism: Agonist at 5HT2A receptors on Raphe cell body –> inhibition of Raphe Nuclei firing –> increased sensory input; partial dopamine agonist
List the class and mechanism of Psilocybin
Class: Schedule I Hallucinogen, indole alkyl amine;
Mechanism: Agonist at 5HT2A receptors on Raphe cell body –> inhibition of Raphe Nuclei firing –> increased sensory input; partial dopamine agonist
List the class and mechanism of MPTP
Class: poison, fentanyl derivative;
Mechanism: destroys substantia nigra –> Parkinson’s
List the class and mechanism of Marijuana (THC)
Class: Schedule I hallucinogen; Cannabinoid;
Mechanism: Hits cannabinoid receptors (CB1, CB2: G-protein coupled receptors)
List the class and mechanism of Anandamide
Class: Endogenous cannabinoid;
Mechanism: Hits cannabinoid receptors (CB1, CB2: G-protein coupled receptors)
List the class and mechanism of Dronabinol (Marinol)
Class: Schedule III drug; Synthetic THC;
Mechanism: Hits cannabinoid receptors (CB1, CB2: G-protein coupled receptors)
List the class and mechanism of Nabilone (Cesamet)
Class: Schedule II drug; Synthetic THC;
Mechanism: Hits cannabinoid receptors (CB1, CB2: G-protein coupled receptors)
List the class and mechanism of Phencyclidine (PCP)
Class: Dissociative anesthetic;
Mechanism: Antagonist of ion channel associated with NDMA receptor; agonist at mu opioid receptors
List the class and mechanism of MDMA (Ecstasy)
Class: Amphetamine derivative;
Mechanism:
List the class and mechanism of Bath salts
Class: Amphetamine / cathinone analog;
Mechanism:
List the class and mechanism of Morphine
Class: Opioid;
Mechanism: Mu-opioid receptor agonist
List the class and mechanism of Codeine
Class: Opioid;
Mechanism: Mu-opioid receptor agonist (low receptor affinity); demethylated to form morphine (10% of oral ingestion, via CYP2D6)
List the class and mechanism of Tramadol (Ultram)
Class: Opioid;
Mechanism: Mu opioid receptor agonist (weak); some NE/5HT uptake inhibition (leading to analgesia); synthetic codeine analog
List the class and mechanism of Fentanyl (Duragesic)
Class: Opioid;
Mechanism: Mu-opioid receptor agonist (strong); highly lipid-soluble
List the class and mechanism of Methadone (Methadose)
Class: Opioid;
Mechanism: Mu-opioid receptor agonist
List the class and mechanism of Oxycodone
Class: Opioid;
Mechanism: Mu-opioid receptor agonist
List the class and mechanism of Meperidine (Demerol)
Class: Opioid;
Mechanism: Mu-opioid receptor agonist
List the class and mechanism of Propoxyphene (Darvon)
Class: Opioid;
Mechanism: Mu-opioid receptor agonist (weak)
List the class and mechanism of Loperamide (Imodium)
Class: Opioid;
Mechanism: Slows peristalsis via opioid receptors in intestine, and possibly decreased GI secretion
List the class and mechanism of Diphenoxylate (Lomotil)
Class: Opioid;
Mechanism: Slows peristalsis via opioid receptors in intestine, and possibly decreased GI secretion
List the class and mechanism of Naloxone (Narcan)
Class: Opioid antagonist;
Mechanism: Competitive mu-, delta-, and kappa-opioid receptor antagonist
List the class and mechanism of Naltrexone (Revia)
Class: Opioid antagonist;
Mechanism: Mu-opioid receptor antagonist
List the class and mechanism of Diazepam (Valium)
Class: Benzodiazepine;
Mechanism: GABA-A agonist; binds between a1 and y2 subunits to open Cl- channel and hyperpolarize the cell
List the class and mechanism of Chlordiazepoxide (Librium)
Class: Benzodiazepine;
Mechanism: GABA-A agonist; binds between a1 and y2 subunits to open Cl- channel and hyperpolarize the cell
List the class and mechanism of Lorazepam (Ativan)
Class: Benzodiazepine;
Mechanism: GABA-A agonist; binds between a1 and y2 subunits to open Cl- channel and hyperpolarize the cell
List the class and mechanism of Flurazepam (Dalmane)
Class: Benzodiazepine;
Mechanism: GABA-A agonist; binds between a1 and y2 subunits to open Cl- channel and hyperpolarize the cell
List the class and mechanism of Alprazolam (Xanax)
Class: Benzodiazepine;
Mechanism: GABA-A agonist; binds between a1 and y2 subunits to open Cl- channel and hyperpolarize the cell
List the class and mechanism of Triazolam (Halcion)
Class: Benzodiazepine;
Mechanism: GABA-A agonist; binds between a1 and y2 subunits to open Cl- channel and hyperpolarize the cell
List the class and mechanism of Midazolam (Versed)
Class: Benzodiazepine;
Mechanism: GABA-A agonist; binds between a1 and y2 subunits to open Cl- channel and hyperpolarize the cell
List the class and mechanism of Clonazepam
Class: Benzodiazepine;
Mechanism: GABA-A agonist; binds between a1 and y2 subunits to open Cl- channel and hyperpolarize the cell
List the class and mechanism of Zolpidem (Ambien)
Class: Non-benzodiazepine receptor agonist;
Mechanism: BDZ-1 selective agonist
List the class and mechanism of Flumazenil (Romazicon)
Class: Benzodiazepine antagonist;
Mechanism: Competitive non-selective antagonist
List the class and mechanism of Thiopental (Pentothal)
Class: Barbiturate;
Mechanism: GABA-A agonist; binds a or b subunit; highly lipid soluble, fast-on, fast-off
List the class and mechanism of Phenobarbitol
Class: Barbiturate;
Mechanism: GABA-A agonist (binds a or b subunit)
List the class and mechanism of Buspirone (Buspar)
Class: Non-benzo anxiolytic;
Mechanism: Partial agonist at 5HT1A (not GABA-A)
List the class and mechanism of Propanolol
Class: β-blocker;
Mechanism: β-adrenergic receptor antagonist
List the class and mechanism of Nitrous Oxide
Class: —;
Mechanism: NMDA receptor antagonist
List the class and mechanism of Isoflurane (Forane)
Class: Volatile anesthetic;
Mechanism: Most potent
List the class and mechanism of Desflurane (Suprane)
Class: Volatile anesthetic;
Mechanism: Least soluble, least potent (allows for rapid emergence from anesthesia)
List the class and mechanism of Sevoflurane (Ultane)
Class: Volatile anesthetic;
Mechanism: Less soluble, less potent (but not irritating)
List the class and mechanism of Methohexital (Brevital)
Class: Barbiturates;
Mechanism: GABA-A receptor binding; produce hypnosis and sedation, but are anti-analgesics
List the class and mechanism of Propofol (Diprivan)
Class: Alkylphenol (a fatty acid);
Mechanism: GABA-A receptor agonist, antagonist of NMDA-glutamate receptor; some a2 receptor activity; rapid onset and offset
List the class and mechanism of Etomidate (Amidate)
Class: Carboxylated imidazole;
Mechanism: GABA-A receptor agonist (only D-isomer)
List the class and mechanism of Ketamine (Ketalar)
Class: Phencyclidine;
Mechanism: NMDA receptor antagonist, kappa opiate agonist; leads to dose-dependent unconsciousness, amnesia, analgesia
List the class and mechanism of Dexmedetomidine (Precedex)
Class: a2 adrenergic agonist;
Mechanism: Binds a2a and a2b in locus coeruleus and spinal cord (produces sedation, sympatholysis, and analgesia)
List the class and mechanism of Succinylcholine (Anectine)
Class: Depolarizing NMB;
Mechanism: Divalent ACh molecule; attaches to all ACh receptors, overstimulating them (first seen as disorganized muscular contractions (fasiculations), then paralysis)
List the class and mechanism of Pancuronium (Pavulon)
Class: Amino steroid non-depolarizing NMB;
Mechanism: Competitive blockade of ACh (no depolarization); vagolytic
List the class and mechanism of Vecuronium (Norcuron)
Class: Amino steroid non-depolarizing NMB;
Mechanism: Competitive blockade of ACh (no depolarization)
List the class and mechanism of Rocuronium (Zemuron)
Class: Amino steroid non-depolarizing NMB;
Mechanism: Competitive blockade of ACh (no depolarization)
List the class and mechanism of Atracurium (Tracrium)
Class: Isoquinoline non-depolarizing NMB;
Mechanism: Competitive blockade of ACh (no depolarization)
List the class and mechanism of Cis-atracurium (Nimbex)
Class: Isoquinoline non-depolarizing NMB;
Mechanism: Competitive blockade of ACh (no depolarization)
List the class and mechanism of Sugammadex (Bridion)
Class: Selective relaxant binding agent;
Mechanism: Complexes with rocuronium, rendering it inactive; no effect on AChesterase
List the class and mechanism of Edrophonium (Enlon)
Class: AChE-I;
Mechanism: —
List the class and mechanism of Neostigmine (Prostigmin)
Class: AChE-I;
Mechanism: —
List the class and mechanism of Pyridostigmine (Mestinon)
Class: AChE-I;
Mechanism: —
List the class and mechanism of Glycopyrrolate (Robinul)
Class: Anti-muscarinic;
Mechanism: —
List the class and mechanism of Ester anesthetic
Class: Ester;
Mechanism: Nonionized form crosses axonal membrane; ionized form (active form) blocks intracellular portion of inactive (refractory) voltage-gated sodium channel
List the class and mechanism of Amide anesthetic
Class: Amide;
Mechanism: Nonionized form crosses axonal membrane; ionized form (active form) blocks intracellular portion of inactive (refractory) voltage-gated sodium channel
List the class and mechanism of Avonex
Class: IFNβ-1a;
Mechanism: Many, potentially: inhibit T-cell activation, shift from Th1 to Th2, inhibit lymphocyte movement into CNS, anti-proliferative effect, apoptosis of T-cells, anti-viral, IFN-g antagonism
List the class and mechanism of Rebif
Class: IFNβ-1a;
Mechanism: Many, potentially: inhibit T-cell activation, shift from Th1 to Th2, inhibit lymphocyte movement into CNS, anti-proliferative effect, apoptosis of T-cells, anti-viral, IFN-g antagonism
List the class and mechanism of Betaseron / Betaferon
Class: IFNβ-1b;
Mechanism: Many, potentially: inhibit T-cell activation, shift from Th1 to Th2, inhibit lymphocyte movement into CNS, anti-proliferative effect, apoptosis of T-cells, anti-viral, IFN-g antagonism
List the class and mechanism of Extavia
Class: IFNβ-1b;
Mechanism: Many, potentially: inhibit T-cell activation, shift from Th1 to Th2, inhibit lymphocyte movement into CNS, anti-proliferative effect, apoptosis of T-cells, anti-viral, IFN-g antagonism
List the class and mechanism of Glatiramer acetate (Copaxone)
Class: Myelin basic protein analog;
Mechanism: Mixture of 4 AAs in myelin basic protein; causes T-cell apoptosis (looks like MBP), induces anti-inflammatory Th2 cells (cytokine shift from Th1), induces Treg with induction of anergy
List the class and mechanism of Natalizumab (Tysabri)
Class: Monoclonal antibody;
Mechanism: Binds VLA4 (integrin subunit), inhibiting leukocyte migration across BBB
List the class and mechanism of Fingolimod (Gilenya)
Class: Sphingosine-1-phosphate analog;
Mechanism: Prodrug; sequesters circulating lymphocytes in secondary lymphoid organs via induction of intracellular internalization of receptors on lymphocytes (no effect on lymphocyte induction, proliferation, or memory function)
List the class and mechanism of Teriflunomide (Aubagio)
Class: Immunosuppressants;
Mechanism: Selective dihydro-orotate dehydrogenase (DHODH) inhibitor: blocks de novo pyramidine synthesis which reduces T- and B-cell proliferation and function; preserves replication and function of cells living on salvage pathway (e.g., hematopoietic cells, memory cells)
List the class and mechanism of Dimethyl fumarate / BG12 (Tecfidera)
Class: —;
Mechanism: Enhances Nrf2 pathway; some Th1 -> Th2 shift
List the class and mechanism of Mitoxantrone (Novantrone)
Class: Anthracenedione;
Mechanism: Broad immune suppression and modulation of B cells, T cells and macrophages
List the class and mechanism of Azathioprine (Imuran)
Class: Immunosuppressants;
Mechanism: Immunosuppressive
List the class and mechanism of Methotrexate (Trexall)
Class: Immunosuppressants;
Mechanism: Immunosuppressive