Pharmacology 2: Block 1 CNS Drugs

Levodopa (L-Dopa)

MOA: Taken up by dopamine neurons and converted to dopamine, Use: Treatment for Parkinson's disease, SE: Movement disorders from excess dopamine

Haloperidol

MOA: Dopamine antagonist on postsynaptic receptors, Use: Treatment for schizophrenia/psychosis, SE: Extrapyramidal side effects

Methylphenidate

MOA: Blocks dopamine and norepinephrine transporters (increases both DA and NE), Use: Treatment for ADHD (Ritalin is immediate release, Concerta is extended-release), SE: Anxiety, irritability, insomnia, increase in blood pressure and heart rate

Amphetamine

MOA: Blocks dopamine and norepinephrine transporters and increases DA availability, Use: Treatment for ADHD (Adderall is immediate-release, Vyvanse is extended-release pro-drug), SE: Anxiety, irritability, insomnia, increase in blood pressure and heart rate

Botulism toxin

MOA: Decreases release of acetylcholine at neuromuscular junction and parasympathetic nervous system, Use: Treatment for spasticity, overactive bladder, excessive drooling, SE: Effect of local injection typically lasts 3-6 months

Fluoxetine

MOA: Serotonin reuptake inhibitor, Use: Treatment for depression

Amitriptyline

MOA: Tricyclic antidepressant; blocks reuptake of both Serotonin and Norepinephrine, Use: Treatment for anxiety/depression

Diltiazem

MOA: Calcium channel blocker, Use: Hypertension

Methadone

MOA: Opioid agonist, Use: Long-term agonist as treatment for opioid use disorder, SE: Monitor QTc

Disulfiram

MOA: Inhibits acetaldehyde dehydrogenase causing build-up of acetaldehyde with alcohol, Use: Alcohol use disorder, SE: Patients may not want to take this daily as a preventative medication

Acamprosate

MOA: Interacts with glutamate and GABA transmission centrally to reduce cravings for alcohol, Use: Alcohol use disorder, SE: Renally excreted; contraindicated in low GFR

Naltrexone

MOA: Directly blocks opioid receptors and prevents euphoria, Use: Alcohol use disorder/Opioid use disorder, SE: Metabolized in the liver; need to check liver function tests prior to starting

Buprenorphine

MOA: Partial opioid agonist, Use: Opioid use disorder

Bupropion (Wellbutrin)

MOA: Blocks reuptake of norepinephrine and dopamine; non-competitive antagonist of nicotinic acetylcholine receptors, Use: Nicotine dependence; depression, SE: Lower sexual side effects than SSRI or SNRI because it has minimal activity on serotonin receptors

Varenicline (Chantix)

MOA: Partial agonist at α4β2 nicotinic acetylcholine receptors, Use: Nicotine dependence, SE: Monitor for neuropsychiatric side effects

Guanfacine

MOA: Alpha 2A adrenoreceptor agonist; decreases sympathetic nerve impulses and increases connectivity in dorsolateral prefrontal cortex, Use: Treatment of ADHD, SE: Mild sedative properties; can be useful with insomnia

Modafinil

MOA: Multiple mechanisms (Dopamine and NE reuptake inhibitor, histamine stimulator), Use: Primary indication is treatment of narcolepsy; off label treatment of ADHD

Adderall

Immediate-release amphetamine for ADHD

Vyvanse

Extended-release pro-drug of amphetamine for ADHD

Concerta

Extended-release form of methylphenidate

Ritalin

Immediate release form of methylphenidate