Human neuropharmacology

Aducanumab

monoclonal antibody against Aβ oligomers and aggregates, promising trials in treatment of AD.

Agomelatine

antidepressant: melatonin receptor agonist.

Weak antagonist of 5-HT_2C.

Amantadine

anti-viral, may enhance DA release, used in PD

Amitriptyline

Antidepressant: TCA, inhibits NET/SERT, additional polypharmacology.

Amphetamine

can be used to treat ADHD: competitive NET/DAT inhibitor, enters vesicles to displace NA/DA.

Aripiprazole

Antipsychotic (atypical): D2 partial agonist, 5-HT1A partial agonist.

Bromocriptine

ergot derived DA receptor agonist, can be used in PD

Bupropion

Antidepressant: – inhibits NET/DAT, also used to treat nicotine dependence

Buspirone

anxiolytic: partial 5-HT1A agonist, used in generalised anxiety disorder.

Caffeine

PDE inhibitor, adenosine receptor antagonist, CNS stimulant

Carbamazepine

Antiepileptic: NaV blocker, antiepileptic

Carbidopa

peripherally acting DOPA decarboxylase inhibitor, used with levodopa in PD

Chlorpromazine

Antipsychotic (typical): Broad spectrum of action – pan DA and 5-HT receptor antagonist, antihistamine, antimuscarinic.

Citalopram

Antidepressant: SERT inhibitor, also used to treat panic attacks.

Clobazam

benzodiazepine, enhances GABAA response to GABA, used as an add on treatment for tonic-clonic seizures.

Clozapine

Antipsychotic (atypical): weak D2 antagonist, 5-HT2 antagonist, antihistamine, antimuscarinic.

Desipramine

Antidepressant: TCA, inhibits NET/SERT, additional polypharmacology. Imipramine metabolite

Diazepam

benzodiazepine, enhances GABAA response to GABA, used to treat anxiety and status epilepticus.

Diphenhydramine

Antihistamine: H1 receptor antagonist, has sedative effects.

Domperidone

Antiemetic: D2/3 receptor antagonist, used to limit levodopa-induced nausea.

Donepezil

Anticholinesterase inhibitor: used to treat AD.

Duloxetine

Antidepressant: SNRI, inhibits NET/SERT

Entacapone

COMT inhibitor (peripherally restricted) used in the treatment of PD.

Ethosuximide

Antiepileptic: T-type CaV blocker, efficacious in treating absence seizures.

Fluoxetine

Antidepressant: SSRI, inhibits SERT (also 5-HT2C antagonist).

Gabapentin

Antiepileptic: binds α2δ1 subunits thereby reducing CaV plasma membrane expression, efficacious in treating absence seizures.

Galantamine

Anticholinesterase inhibitor: used to treat AD.

Haloperidol

Antipsychotic (typical): D1/2 and 5-HT2A receptor antagonist

Imipramine

Antidepressant: TCA, inhibits NET/SERT, additional polypharmacology

Ketamine

NMDA receptor channel blocker. Anaesthetic, possible antidepressant.

Lacosamide

Antiepileptic: inhibits NaV by enhancing slow inactivation.

Lamotrigine

Antiepileptic: NaV blocker, also used in bipolar disorder.

Levetiracetam

Antiepileptic binds SV2A (synaptic vesicle protein 2A). Used for partial/generalised seizures

Levodopa/L-DOPA

substrate for DOPA decarboxylase, used to treat PD.

Lithium

mood stabiliser: treatment for bipolar disorder.

Lorazepam

benzodiazepine, enhances GABAA response to GABA, used as sedative and also status epilepticus

Memantine

Alzheimer’s treatment: non-competitive NMDA receptor channel blocker

Methylphenidate (Ritalin)

DAT inhibitor. Elevated DA levels used in the treatment of ADHD.

Midazolam

benzodiazepine, enhances GABAA response to GABA, used in the treatment of status epilepticus.

Mirtazapine

Antidepressant: NASSA, α2 adrenoceptor and 5-HT2A/C and 5-HT3 antagonist.

Moclobemide

antidepressant: reversible MAO-A inhibitor.

Modafinil

weak DAT inhibitor + enhances 5-HT, glutamate, histamine release + inhibits GABA release. Used to treat narcolepsy

Nortriptyline

Antidepressant: TCA, inhibits NET/SERT, additional polypharmacology. Amitriptyline metabolite.

Olanzapine

Antipsychotic (atypical): D2 and 5-HT2A antagonist, also used to treat bipolar disorder.

Orphenadrine

muscarinic receptor antagonist, used to treat drug-induced parkinsonism

Perampanel

Antiepileptic: non-competitive AMPA receptor antagonist.

Phenelzine

antidepressant: irreversible non-selective MAO inhibitor.

Phenobarbital

long acting barbiturate, enhances the magnitude of GABAA currents, rarely used anticonvulsant.

Phenytoin

Antiepileptic: NaV blocker, antiepileptic.

Pitolisant

Histamine H3 receptor inverse agonist used in the treatment of narcolepsy

Propranolol

beta blocker, non-selective β adrenoceptor antagonist, reduces the physical symptoms of anxiety.

Ramelteon

melatonin agonist used in the treatment of insomnia.

Ranitidine

Histamine H2 receptor antagonist. Reduced stomach acid production used to treat peptic ulcers and reflux disease.

Retigabine

KV7.2 opener used to treat partial seizures (withdrawn 2017)

Rivastigmine

Anticholinesterase inhibitor: used to treat AD

Ropinirole

non-ergot derived D2/3 receptor agonist, used in PD.

Safinamide

MAO-B and DAT inhibitor, used in PD.

Selegiline

MAO-B inhibitor, used in PD.

Sertraline

Antidepressant: SSRI, inhibits SERT, also used to treat panic attacks and post traumatic stress disorder (PTSD).

Suvorexant

Orexin (OX1 and OX2) receptor antagonist, used to treat insomnia

Talcapone

COMT inhibitor (centrally penetrant) used in the treatment of PD.

Tiagabine

Antiepileptic: inhibits GAT1, add-on therapy for partial seizures.

Topiramate

Antiepileptic: inhibits NaV, CaV, AMPA receptors and facilitates GABAA function.

Trazodone

Antidepressant: pan 5-HT2 antagonist used to treat insomnia

Valproate (sodium)

Antiepileptic: T-type CaV blocker, weak GABA transaminase inhibitor and may enhance GABA function and block NaV, efficacious in treating absence seizures.

Venlafaxine

Antidepressant: SNRI, inhibits NET/SERT

Vigabatrin

Antiepileptic: irreversible GABA transaminase inhibitor

Vortioxetine

Antidepressant: SSRI, 5-HT1A agonist, 5-HT1B partial agonist & 5-HT3 antagonist

Zolpidem

“Z” drug acts at GABAA benzodiazepine site, short acting, hypnotic used in the treatment of insomnia.

Zonisamide

Antiepileptic: inhibits NaV/CaV, may enhance GABAA function