Classification of Neuropsychiatric Medications Based On Their Principle Mechanisms Of Action
Acetylcholine
| Cholinesterase Inhibition |
| donepezil (Aricept) | rivastigmine (Exelon) |
| galantamine (Reminyl) | |
| Muscarinic Acetylcholine Receptor Antagonism |
| atropine | orphenadrine (eg, Norflex) |
| belladonna | oxybutynin (eg, Ditropan) |
| benztropine (Cogentin) | procyclidine (Kemadrin) |
| biperiden (Akineton) | propanthethine (eg, Pro-Banthine) |
| clidinium (Quarzan) | scopolamine (eg, Sopace) |
| dicyclomine (eg, Bentyl) | solifenacin (Vesicare) |
| glycopyrrolate (eg, Robinul) | trospium (Sanctum) |
| hyoscyamine (eg, Anaspaz) | tolterodine (Detrol) |
| mepenzolate (Cantil) | trihexyphenidyl (Artane) |
| methscopolamine (Pamine) | |
| Also includes: A number of low-potency phenothiazines (See the class below labeled: “5-HT2A, D2 and multiple other receptor antagonism”), a number of tertiary amine TCAs and related antidepressants (See the class below labeled: “Dual norepinephrineand serotonin uptake pump inhibition plus other actions”). |
| Nicotinic (alpha-4 beta-2 subtype) Receptor Agonism |
| varenicline (Chantix) | |
Biogenic Amines (dopamine. norepinephrine. and serotonin)
| Catechol-O-Methyltransferase Inhibition |
| entacapone (Comtan) | tolcapone (Tasmar) |
| Monoamine Oxidase Inhibition |
| isocarboxazid (Marplan) | selegiline (Eldepryl/EMSAM) |
| phenelzine (Nardil) | tranylcypromine (Parnate) |
| Biogenic Amine Release |
| Release: Classically NE>DA>SE but rank order of effects on these neurotransmitters may vary amongst the different drugs in this class. |
| amphetamines (eg, Desoxyn) | methamphetamine |
| benzphetamine (Didrex) | methylphenidate (eg, Ritalin) |
| dextroamphetamine (eg, Dexedrine) | phendimetrazine (eg, Prelu-2) |
| diethylpropion (eg, Tenuate) | phentermine (eg, lonamin) |
Dopamine
| Dopaminem Agonism (general) |
| levodopa (dopamine precursor, dopamine agonism [general] component of Sine met). |
| Dopamine-2 (D2) Agonism |
| bromocriptine [+partial D1 agonism]: (Parlodel) | pramipexole [+ D3 agonism but no D1 activity]: (Mirapex) |
| pergolide [+D1 agonism]: (Permax) | ropinirole [+ D3 agonism but no D1 activity]: (Requip) |
| Dopamine Uptake Inhibition |
| amantadine (Symmetrel) | cocaine |
| benzphetamine (Didrex) | methamphetamine (eg, Desoxyn) |
| bupropion (Wellbutrin, Zyban) | |
| Dopa Decarboxylase Inhibitor |
| carbidopa (Component of Sinemet) | |
| Selective D2 Receptor Antagonism |
| fluphenazine (eg, Prolixin) | piperazine (Entacyl) |
| haloperidol (eg, Haldol) | trifluoperazine (eg, Stelazine) |
| perphenazine (eg, Trilafon) | triflupromazine (eg,Vesprin) |
| pimozide(Orap) | |
| D2 Receptor Partial Agonism |
| aripiprazole (Ability) | |
| D2 Receptor Antagonism Plus Multiple Other Effects |
| See 5-HT2A, D2 and multiple other effects below. |
Ethanol
| Solubilizes electrically excitable membranes. |
GAM
| Barbiturates |
| (enhance the binding of GABA to GABAA receptors and promote rather than displace the binding of benzodiazepines) |
| amobarbital (Amytal) | phenobarbital (eg, Nembutal) |
| butabital (eg, Butisol) | phenobarbital |
| mephobarbital (Mebaral) | primidone (Mysoline) |
| metharbital | secobarbital (Seconal) |
| Barbiturate-Like Drugs |
| chloral hydrate (eg, Aquachloral) | ethchlorvynol (Placidyl) |
| Benzodiazepine Binding Site Agonism |
| alprazolam (eg, Xanax) | lorazepam (eg, Ativan) |
| chlordiazepoxide (eg, Librium) | midazolam (eg, Versed) |
| clonazepam (eg, Klonopin) | prazepam (Centrax) |
| clorazepate (eg, Tranxene) | quazepam (Doral) |
| diazepam (eg, Valium) | temazepam (eg, Restoril) |
| estazolam (eg, ProSom) | triazolam (eg, Halcion) |
| flurazepam (eg, Dalmane) | zolpidem (Ambien) |
| halazepam (Paxipam) | |
| Benzodiazepine-Like Drug |
| meprobamate (eg, Miltown) | |
| GABA Transaminase Inhibition and Stimulation of Slutaminic Acid Decarboxylase |
| divalproex sodium (Depakote) | valproate sodium (Depacon) |
| valproic acid (Depakene) | |
| Promotion of Nonvesicular Release of SABA |
| gabapentin (Neurontin) | |
Glutamate (N-methyl-D-aspartate receptor)
Herbals
| ginkgo biloba | St. John’s Wort |
| ginseng | |
Histamine (Centrally Active) (H1) Antagonism
| chlorpheniramine | diphenhydramine (Benadryl) |
| cyclobnezaprine (Flexeril) | hydroxyzine (Atarax) |
| Also includes: a number of low potency phenothiazines (See the class below labeled: “5-HT2A, D2 and multiple other receptor antagonism”), a number of tertiary amineTCA and related antidepressants (See the class below labeled: “Dual norepinephrineand serotonin uptake pump inhibition plus other actions”). |
Ion Channel Inhibition
| carbamazepine (eg, Tegretol) slows the recovery of voltage-activated Na+ channels. |
| dantrolene (Dantrium) interferes with the release of Ca++ from sacroplasmic reticulum. |
| felbamate (Felbatol) inhibits NMDA-evoked responses and potentiates GABA-evoked responses. |
| lithium (eg, Eskalith) substitutes for multiple ions. |
| lamotrigine (Lamictal) [has the effects of carbamazapine] plus inhibition of glutamate release. |
| mephenytoin (Mesantonin) slows recovery of voltage-activated Na+ channels. |
| phentyoin (eg, Dilantin) slows recovery of voltage-activated Na+ channels. |
| topiramate (Topamax) reduces voltage-gated Na+ currents, enhances postsynap-tic GABAA receptor currents, and limits activation of AMPA-kainate subtypes of the gluta mate receptor. |
| Other CNS drugs with potentially clinically relevant effects on ion channels at usual concentrations include: a number of low potency phenothiazines (See the class below labeled: “5-HT2A, D2 and multiple other receptor antagonism”), a number of tertiary amine TCAs and related antidepressants (See the class below labeled: “Dual norepinephrine and serotonin uptake pump inhibition plus other actions”). Thioridazine has a black box warning because of such effects. |
Norepinephrine
| alpha-1 Antagonism |
| This mechanism is not known to mediate any desired CNS effect, thus no neuro-psychiatric medications were developed to have only this specific mechanism of action. Nevertheless, several neuropsychiatric medications do achieve concentrations under clinically relevant dosing conditions, which block this receptor. These medications include: amitriptyline, chlorpromazine, clozapine, quetiapine, nefazodone, risperidone, thioridazine, and trazodone. See Tables 2, 8, and 9 for relative binding affinities to this receptor by these drugs. |
| alpha-2 Agonism |
| clonidine (eg, Catapres) | |
| Norepinephrine Uptake Pump Inhibition |
| atomoxetine (Strattera) | nortriptyline (eg, Pamelor) |
| cocaine | phentermine (eg, lonamine) |
| desipramine (eg, Norpramin) | protriptyline (eg, Vivactil) |
| maprotiline (eg, Ludiomil) | reboxetine (Vespar) |
| Dual Norepinephrine and Serotonin (NE>SE) Uptake Pump Inhibition Plus Other Actions |
| amitriptyline (eg, Elavil) | doxepin (eg, Sinequan) |
| amoxapine (eg, Ascendin) | imipramine (eg, Tofranil) |
| clomipramine (eg, Anafril) | trimipramine (eg, Surmontil) |
Opiate Receptors
| alfentanil (Alfental) | nalbuphine (eg, Nubain) |
| buprenorphine(Buprenex) | opium (eg, Paregoric) |
| codeine | oxycodone (Roxicodone) |
| fentanyl (eg, Sublimaze) | pentazocine (eg, Talwin) |
| hydrocodone (eg, Vicodin) | prophyphene (eg, Darvon) |
| hydromorphine (eg, Dilaudid) | sufenatil (eg, Sufenta) |
| meperidine (eg, Demerol) | tramadol (Ultram) |
| methadone (eg, Dolophine) | |
Serotonin
| 5-HT1A Partial Agonism |
| buspirone (eg, Buspar) | |
| 5-HT1B/D Agonism |
| ergotamine (eg, Ergomar) | dihyrdoergotamine (D.H. E. 45) |
| naratriptan (Amerge) | sumitriptan (Imitrex) |
| rizatriptan (Maxalt) | zolmitriptan (Zomig) |
| 5-HT2 Receptor Antagonism |
| cyproheptadine (Periactin) | nefazodone (Serzone)* |
| methysergide (Sansert) | trazodone (eg, Desyrel)* |
| mirtazapine (Remeron)* | |
| * See Table 8 for relative effects on neuroreceptors. |
| 5-HT2A, D2 and Multiple Other Receptor Antagonism – Newer Antipsychotics** |
| asenapine(Saphris) | quetiapine (Seroquel) |
| iloperidone (Fanapt) | risperidone (Risperdal) |
| olanzapine (Zyprexa) | ziprasidone (Geodon) |
| paliperidone (Invega) | |
| ** See Table 9 for relative effects on neuroreceptors for all of these drugs. |
| 5-HT2A, D2 and Multiple Other Receptor Antagonism – Older Antipsychotics |
| chlorpromazine (eg, Thorazine)*** | prochlorperazine (eg, Compazine) |
| clozapine (eg, Clozaril)*** | promethazine (eg, Phenergan) |
| loxapine (eg, Loxitane)*** | promazine (eg, Sparine) |
| mesoridazine (eg, Serentil) | thiethylperazine (Torecan) |
| propiomazine (Largon) | thioridazine (eg, Mellaril)*** |
| *** See Tables 2 and 9 for relative effects on neuroreceptors. |
| Serotonin Uptake Inhibition |
| dexfenfluramine (Redux) | Fenfluramine(Pondimin) |
| Selective Serotonin Uptake Inhibition |
| citalopram (Celexa) | fluvoxamine (eg, Luvox) |
| escitalopram (Lexapro) | paroxetine (Paxil) |
| fluoxetine (eg, Prozac) | sertraline (Zoloft) |
| Dual Serotonin and Norepinephrine (5-HT≥NE) Uptake Pump Inhibition |
| desvenlafaxine (Pristiq) | sibutramine (Meridia) |
| duloxetine (Cymbalta) | venlafaxine (Effexor) |
| milnacipran (Savella) | |
5-HT = serotonin; D2 = dopamine-2; TCAs = tricyclic antidepressants; NE = norepinephrine; DA = dopamine; SE = serotonin; GABA = Ύ-aminobutyric acid; NMDA = N-methyl-D-aspartate AMPA = α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid; CNS = central nervous system.
Psychotherapeutic Drugs:
- Antidepressants
- Antipsychotics/Antimanics
- Antianxiety Drugs
- Stimulants and Non-stimulants for ADHD
- Smoking Cessation Drugs, Drug Addiction Treatments and Other Psychotherapeutics
