Note – all drugs will produce side effects (must warn patients that most drugs could cause

nausea and vomiting). There is always a possibility that drugs will produce an allergic
reaction and that they should report any type of allergic reaction immediately. Always
warn patients about taking alcohol with drugs and the possibilities of severe central
nervous system depression.
These drug tables are only partial tables for learning material. The listed side effects are
not a complete list. For complete lists of drugs and side effects see the latest version of the
Physician Desk Reference (PDR).

Local Anesthetics

Category Drug Mechanism of action Side effects

Lidocaine Blockade of Voltage Systemic doses can
gated sodium channels result in death due to the
(VGSC) blockade of respiration,
cardiovascular problems
and depress smooth
muscle contraction.
Seizures.
Bupivicaine As above As above

Procaine As above As above

Mepivacaine As above As above..…more toxic

in infants
Tetracaine As above ……longer As above
duration of action.
Benzocaine As above …lacks As above
efficacy
Cocaine As above, in addition to As above …..can also
VGSC blockade…due lead to addiction due to
to its ability to block its ability to block
reuptake of NE can also reuptake of dopamine
result in local
vasoconstriction

Neuromuscular Blockers

Category Drug Mechanism of action Side effects

Competitive agents Tubocurarine Skeletal muscle Ganglionic blockade
nicotinic channel causing decrease in
antagonist blood pressure and
tachycardia. Release of
histamine. Respiratory
paralysis.
Pancuronium As above …long As above …yet side
duration of action effects decreased with
the rest of the agents
listed
Rocuronium As above As above
 ….intermediate duration
of action
Atracurium As above As above
….intermediate duration
of action
Vecuronium As above As above
….intermediate duration
of action
Mivacurium As above …shorter As above
duration of action
Depolarizing agent Succinylcholine Skeletal muscle Ganglionic effects,
(Acectine®, Scoline®) nicotinic channel decrease in blood
agonist pressure and
tachycardia. Release of
histamine. Respiratory
paralysis.

Spasmolytics (muscle relaxants)

Category Drug Mechanism of action Side effects

Dantrolene (Dantrium®) Blocks calcium release Dizziness, Drowsiness,
– used for malignant from the sarcoplasmic weakness, fatigue, GI
hyperthermia and ALS reticulum by blocking disturbances, respiratory
the ryanodine receptor. depression
Diazepam (Valium®) Potentiate GABAs Sedation,
ability to open the Ataxia,
GABAA chloride Dependence
channel (increase
channel opening
frequency)
Baclofen (Kemstro®, GABAB agonist (GPCR Dizziness, Drowsiness,
Lioresal®) inhibitory coupling) weakness, fatigue,
seizures, hallucinations
Botulinum Toxin Inhibits release of Anxiety, Dizziness,
(Botox®, Dysport®) acetylcholine at he NMJ Drowsiness, dry eyes &
mouth, back & neck
pain

Drugs used for Pain

Category Drug Mechanism of action Side effects

Opioids (used for acute Morphine Acts at mu GPCR to Nausea/emesis,
and chronic pain) cause opening of K+ constipation, sedation,
channels and blocks somnolence, pruritis,
VGCC respiratory depression,
abuse potential
Codeine As above yet less potent As above
 than morphine, better
bioavailability
Oxycodone (in As above As above
Percocet®, Percodan®)
Hydrocodone (in As above As above
Vicodin®)

Hydromorphone As above yet 10 fold As above

(Dilaudid®) more potent than
morphine
Fentanyl (Actiq®, As above yet Mu As above
Duragesic®, Fentora®, agonist, 100 times more
etc) potent than morphine

Sufentanil (Sufenta®) As above yet 1000 fold As above

more potent than
morphine
Alfentanil (Alfenta®) As above yet 80 fold As above
more potent than
morphine
Remifentanil (Ultiva®) As above yet 100 fold As above
more potent than
morphine
Methadone Orally available mu As above
(Dolophine®) opioid agonist
Meperidine (Demerol®) As above yet 5 to 10 As above, also large
fold less potent than doses can cause the
morphine accumulation of
normeperidine, seizures,
hallucinations;
contraindicated in
patients with renal
insufficiency
Loperamide Weak mu agonists that Can cause severe
(Imodium®) does not cross the blood constipation.
brain barrier, used for
diarrhea
Tramadol (Ultram®) Weak mu agonist, also As above like other mu
inhibits uptake of NE opioid agonists that
and 5HT penetrate the CNS but
thought to have less
abuse potential
NSAIDs
Aspirin Irreversible COX All COX inhibitors can
inhibition result in GI irritation,
GERD and GI ulcers
Ibuprofen (Advil®, Reversible COX As above
Motrin®, Nuprin®) inhibition
Indomethacin As above As above
(Indocin®)
Ketorolac (Lodine®) As above As above
Ketoprofen (Orudis®, As above As above
Oruvail®)
Naproxen (Aleve®) As above As above
Celecoxib (Celebrex®) Irreversible COX2 Lacks GI effects, Can
 inhibition
Steroids
Dexamethasone Increase levels of
lipocortin that inhibits
phospholipase A2,
decreasing inflammatory
mediators
(oral admin)
Prednisone As above (oral admin)
Budesonide (Entocort®) As above (Inhaled
(Symbocort® + admin)
formoterol)
Hydrocortisone As above (Topical
admin)
Additional drugs used
for chronic pain
Gabapentin Unknown mechanism
(Neurontin®) but thought to inhibit
voltage-sensitive
calcium channels
Pregabalin (Lyrica®)
Tricyclic antidepressants Norepinephrine and
(TCAs) serotonin uptake
inhibitors
Selective serotonin Serotonin uptake
reuptake inhibitors inhibitors
(SSRIs)
Lidocaine (lidoderm Blocks voltage gated
patch) sodium channels
Migraine Medications
Category Drug Mechanism of action
Triptans Sumatriptan (Imitrex®) 5HT1B and 5HT1D
agonists
Rizatriptan (Maxalt®) As above
Zolmitriptan (Zomig®) As above
Naratriptan (Amerge®) As above, longest acting
of the triptans (1/2 life 6
cause cardiovascular
problems including
stroke and myocardial
infarction, can decrease
kidney function
Prolonged use can lead
to immunosuppression
and cushingoid (central
obesity, moon face,
hyperglycemia,
osteoporosis, etc.)
As above
As above
As above
Sedation, somnolence,
dizziness, ataxia,
peripheral edema
Sedation, somnolence,
dizziness, ataxia,
peripheral edema, visual
disturbances
Sedative,
Antimuscarinic action
Sedative, Insomia,
Antimuscarinic action ,
Sexual & GI
disturbances
If high systemic doses
are reached can cause
cardiovascular
arrhythmia, seizures
Side effects
Cardiovascular ,
coronary artery
vasospasm,
Contraindicated in
individuals with
previous MI
As above
As above
As above
 hours)
Opioids (are used for See above in acute pain See above in acute pain See above in acute pain
migraine) meds meds meds
NSAIDs See above in acute pain See above in acute pain See above in acute pain
meds meds meds
Topiramate Reduces voltage gated Somnolence, fatigue,
(Topamax®) sodium channel activity, nervousness, weight
increase activity at loss, Psychomotor
GABAA CL- channels, slowing
some inhibition of
glutamate AMPA-
kainate channels and
carbonic anhydrase
inhibitor

Stroke

Category Drug Mechanism of action Side effects

Clot busters tPA A serine protease and Risk of hemorrhage
catalyzes the conversion
of plasminogen to
plasmin
Antiplatelet Aspirin Irreversible inhibition of GI disturbances
COX decreasing platelet
production of
thromboxane (TXA2)
Antiplatelet Clopidogrel (Plavix®) Blocks irreversibly the Risk of bleeding,
ADP receptor P2Y12 bleeding risk increases
inhibiting platelet dramatically when in
aggregation by combination with drugs
inhibiting activation of like aspirin
the glycoprotein IIb/IIIa
pathway

Ocular Pharmacology
Category Drug Mechanism of action Side effects
Ocular Hypertension Timolol (Timoptic®) Beta-2 receptor Bronchospasm,
Betaxolol (Betagan®) antagonist (Inhibit bradycardia
aqueous humor
Decrease synthesis secretion)
Brimonidine Alpha-2 receptor agonist Ocular allergy
(Alphagan®) (Inhibit aqueous humor
Apraclonidine secretion)
(Iopidine®)
Dorzolamide Carbonic anhydrase Malaise, fatigue, weight
(Trusopt®) inhibitor (Inhibit loss, anorexia,
Acetazolamide aqueous humor depression
secretion)
Pilocarpine, carbachol Cholinergic agonist Accommodation
(Stimulates contraction (reduced visual acuity),
of ciliary muscle which miosis (dimmed vision),
 stretches open trabecular brow ache (muscle
Increase outflow outflow pathway spasm)
(pressure-dependent))
Acetylcholinesterase Accommodation
Echothiophate, inhibitor (Promotes (reduced visual acuity),
(Phospholine Iodide®), contraction of ciliary miosis (dimmed vision),
Physostigmine (Isopto muscle which stretches brow ache (muscle
serine®) open trabecular outflow spasm)
pathway)
Latanoprost (Xalatan®), Prostaglandin FP Eyelash growth, iridial
Bimatoprost receptor agonist pigmentation,
(Increases uveoscleral conjunctival hyperemia
(pressure-independent)
outflow)
Mydriasis Atropine (Atriposol®), Muscarinic antagonist Photosensitivity, blurred
Scopolamine (Isopto (Inhibit contraction of vision
Hyoscine®) circular muscle)
Phenylephrine (AK- Alpha-1 adrenergic Photosensitivity,
Dilate®) agonist (Stimulate conjunctival hyperemia
contraction of radial
muscle)
Corneal Anesthesia Proparacaine Sodium channel blocker Corneal irritation
(Alcaine®) (Decrease excitability of
sensory nerves in
corneal)

Epilepsy drugs (Anticonvulsants)

Category Drug Mechanism of action Side effects

Inactivation of Na+ Carbamazepine Prolong fast inactivation Induces CYP3A4, life
channels (Tegretol) of voltage gated sodium threatening skin reactions
channels (Stevens-Johnson Syndrome
and Toxic Epidermal
Necrolysis), Teratogen,
drowsiness, headaches, motor
coordination impairment, GI
disturbances
Phenytoin (Phenytek) See above Teratogen, horizontal gaze
nystagmus, sedation, cerebellar
ataxia, paradoxical seizures
Topiramate (Topamax) …in addition increase Somnolence, fatigue,
activity at GABAA CL- nervousness, weight loss
channels, some Psychomotor slowing
inhibition of glutamate
AMPA-kainate
channels and carbonic
anhydrase inhibitor
Lamotrigine (Lamictal) See above life threatening skin reactions
(Stevens-Johnson Syndrome
and Toxic Epidermal
Necrolysis), headaches,
dizziness, insomnia, nightmares,
muscle aches, dry mouth,
 fatigue, cognitive problems,
weight changes, hair loss,
changes in libido, frequent
urination, nausea,
Rufinamide (Banzel) See above…….seizures Somnolence, headache, loss of
associated with Lennox- coordination, uncontrollable
Gastaut syndrome movements, loss of appetite,
nausea

Lacosamide (Vimpat®) Prolong slow GI disturbances, nausea

inactivation of voltage vomiting headaches, blurredor
gated sodium channels double vision, headache,
drowsiness, loss of
coordination,
Valproic acid Teratogen, hepatotoxicity
(Depakene), fatigue, GI disturbances,
Divalproex or Valproate peripheral edema, dizziness,
(Depakote) drowsiness, hair loss,
headaches, tremors,
hyperammonemia & ensuing
encephalopathy
Zonisamide … in addition increase Somnolence, drowsiness, loss of
(Zonegran) activity at GABAA CL- appetite, dizziness, headache,
channels, reduce T-type nausea, and agitation/irritability
Ca+2 channel activity
and carbonic anhydrase
inhibitor
Enhanced GABA *Diazepam (Valium) Potentiate GABA’s Sedation,
synaptic transmission ability to open the Ataxia,
GABAA CL- channel Dependence
Benzodiazepines (increase channel
opening frequency)
*Pentobarbital Potentiate GABA’s Depression of autonomic
Barbiturates (Nembutal) ability to increase ganglia,
duration of GABAA Respiratory depression,
CL- channel openings, at Sedation,
high concentrations can Dependence,
open directly Withdrawal
Vigabatrin (Sabril) Inhibits the breakdown Somnolence, headache,
of GABA dizziness, nervousness,
depression, memory
disturbances, diplopia, ataxia,
GI disturbances
Tiagabine (Gabitril) Blocking re-uptake of Confusion, difficulty speaking
GABA clearly/stuttering, mild sedation,
tingling sensation (paresthesia)
Voltage gated Ca+2 Ethosuximide Reducing current Drowsiness, mental confusion,
channel antagonists (Emesideor Zarontin) through the T-type Ca+2 insomnia, headache, ataxia, GI
channels disturbances, hyperactive

Zonisamide (Zonegran) Reducing current Somnolence, drowsiness, loss of

through the T-type Ca+2 appetite, dizziness, headache,
channels nausea, and agitation/irritability
 Gabapentin Unknown mechanism Sedation, somnolence,
(Neurontin) but thought to inhibit dizziness, ataxia, peripheral
voltage-sensitive edema
calcium channels
Trimethadione Reducing current Somnolence, drowsiness, loss of
(Tridione) through the T-type Ca+2 appetite, dizziness, headache,
channels nausea, and agitation/irritability

Inhibits Vesicular Levetiracetam (keppra) Binds to a protein (SV2) Asthenia (weakness),

release on vesicles and inhibits hallucinations, Sedation,
their release. Overall somnolence, infections, loss of
decrease in appetite
neurotransmitter release.
Glutamate NMDA Felbamate (Felbatol) Blocks the “open state” Aplastic anemia, liver failure,
channel antagonist of the NMDA channels. inhibits CYP2C19, dizziness,
somnolence, insomnia, loss of
appetite, nausea, headache

*Note: additional Benzodiazepines and Barbiturates are in the tables for antianxiety drugs

Drugs used for Parkinson’s Disease

Category Drug Mechanism of action Side effects

Dopamine precursors Carbidopa/Levodopa Levodopa is GI disturbances,
(Sinemet) or (Atamet) decarboxylated to form Dyskinesias-excessive
dopamine in the CNS; and abnormal
Carbidopa is added to involuntary movements,
levodopa since it Hallucinations and
inhibits the breakdown confusion,
by the GI tract. Orthostatic hypotension
Dopamine agonists Bromocriptine Dopamine D2 receptor Hallucinations and
(Parlodel) ergot agonist & D1 partial confusion, GI
derivatives agonist distubances
Orthostatic hypotension,
Cardiac valve trouble,

Pergolide (Permax) Dopamine D2 receptor Hallucinations and

ergot derivatives agonist & D1 receptor confusion,
partial agonist Orthostatic hypotension,
Cardiac valve trouble,

Ropinirole (Requip) Dopamine D2 & D3 Sleep disturbances,

receptor agonist Drowsiness
Pramipexole (Mirapex) Dopamine D2 & D3 Sleep disturbances,
receptor agonist Drowsiness
COMT inhibitors Tolcapone (Tasmar) Inhibitors of catechol-O- GI disturbances,
methyltransferase, Hepatotoxicity,
inhibits dopamine Hallucinations and
breakdown confusion,
Orthostatic hypotension
Entacapone (Comtan) Inhibitors of catechol-O- GI disturbances,
 methyltransferase, Hallucinations and
inhibits dopamine confusion,
breakdown Orthostatic hypotension
MAO inhibitors Selegiline (Eldepryl) Inhibitor of monoamine Sedation,
oxidase B isoenzyme, Hypotension,
inhibits dopamine Weight gain,
breakdown in striatum Sexual disturbances

Drugs used for Amyotrophic Lateral Sclerosis (ALS) “Lou Gehrig’s” Disease

Category Drug Mechanism of action Side effects

Diminish Riluzole (Rilutek) Inhibits glutamate Nausea,
neuroexcitotoxicity release, Antagonist at Diarrhea,
NMDA and Kainate- Weight loss,
type glutamate Dizziness,
receptors, Antagonist at Hepatic injury
voltage-dependent
sodium channels
Reduces spasticity Baclofen (Lioresal) GABAB agonist- Weakness,
produces inhibitory CNS depression
effects in the CNS

Drugs used for Myasthenia Gravis

Category Drug Mechanism of action Side effects

Cholinergic enhancers Neostigmine Acetylcholinesterase GI disturbances,
(Prostigmin) Inhibitors (reversible increased salivation &
AChE inhibitors) Tend bronchial secreations,
to not cross the BBB tearing (“SLUDGE”)
Pyridostigmine
(Mestinon)
Edrophonium
(Tensilon)

Immunosuppressive Prednisone (Deltasone) Synthetic corticosteroid Prolonged use can lead

drugs acts at several levels to to immunosuppression
inhibit the immune and cushingoid (central
system (Tcells, obesity, moon face,
cytokines, etc.) hyperglycemia,
osteoporosis, etc.)

Drugs used for Huntington’s Disease

Category Drug Mechanism of action Side effects

VMAT inhibitor Tetrabenazine Inhibition of dopamine Akathisia, dizziness,
(Xenazine) uptake into vesicles, results depression,
in the degradation of “Parkinsonism”
dopamine
Dopamine antagonist Risperidone Inhibition of dopamine D2 Drug induced
(Risperdal) receptors parkinsons-like
behavior,
Hypotension
Haloperidol (Haldol) Inhibition of dopamine D2 Drug induced
receptors parkinsons-like
behavior,
Hypotension
Clozapine (Clozaril) Inhibition of dopamine D2 Sedation,
receptors Hypotension

Olanzapine (Zyprexa) Inhibition of dopamine D2 Sedation,

receptors Hypotension,
Weight gain
Quetiapine (Seroquel) Inhibition of dopamine D2 Sedation,
receptors Hypotension
Selective serotonin Fluoxetine (Prozac) Serotonin uptake inhibitors Sedative +,
reuptake inhibitors Used to treat the Antimuscarinic
(SSRIs) depression (can include action +,
other antidepressants) Sexual & GI
disturbances,
Insomia

Anti-anxiety (Anxiolytic) Drugs

(Sedative-Hypnotics)
Category Drug Mechanism of action Side effects
Long-acting Potentiate GABAs ability
benzodiazepines to open the GABAA
chloride channel (increase
channel opening
frequency)
Diazepam (valium) Sedation,
Ataxia,
Dependence
Chlordiazepoxide Sedation,
(Librium) Ataxia,
Dependence
Clorazepate Sedation,
(Tranxene) Ataxia,
Dependence
Clonazepam Sedation,
(Klonopin) Ataxia,
Dependence
Flurazepam Sedation,
(Dalmane) Ataxia,
Dependence
Short-acting Potentiate GABAs ability
benzodiazepines to open the GABAA
chloride channel (increase
channel opening
frequency)
Oxazepam (Serax) Sedation,
Ataxia,
 Dependence,
Withdrawal
Lorazepam (Ativan) Sedation,
Ataxia,
Dependence,
Withdrawal
Alprazolam (Xanax) Sedation,
Ataxia,
Dependence,
Withdrawal
Temazepam (Restoril) Sedation,
Ataxia,
Dependence,
Withdrawal
Triazolam (Halcion) Sedation,
Ataxia,
Dependence,
Withdrawal
Midazolam (Versed) Sedation,
Ataxia,
Dependence,
Withdrawal
Non-
benzodiazepam
Sedative/hypnotics
Zolpidem (Ambien) Potentiate GABAs ability Sedation,
to open the GABAA Dizziness
chloride channel (increase
channel opening
frequency)
Zaleplon (Sonata) Potentiate GABAs ability Sedation,
to open the GABAA Dizziness
chloride channel (increase
channel opening
frequency)
Eszopiclone (Lunesta) Potentiate GABAs ability Sedation,
to open the GABAA Dizziness,
chloride channel (increase Somnolence
channel opening
frequency)
Chloral hydrate Increase duration of Sudden acute
GABAA chloride channel intoxication-death,
openings, at high Dependence,
concentrations can open Severe withdrawal,
directly Liver damage
Buspirone (BuSpar) 5-HT1A receptor partial Sedation, Ataxia,
agonist Should not be taken
with MAOIs,
Withdrawal
Barbiturates Increase duration of Depression of
GABAA chloride channel autonomic ganglia,
openings, at high Respiratory depression,
concentrations can open Sedation,
directly Dependence,
Withdrawal
 Pentobarbital
(Nembutal)
Secobarbital
(Seconal)
Phenobarbital
(Luminal)
Thiopental
(Pentothal)
Thiopental
(Pentothal)

Note: All Anxiolytics (sedative-hypnotics) cross the placenta and enter into the breast milk. Benzodiazepines have
been known to produce anterograde amnesia (inability to remember events occurring during the drug’s duration of
action). All drugs except Zaleplon will decrease REM sleep. CNS depressants combined with alcohol or other CNS
depressants can cause death.

Drugs used for PTSD

Category Drug Mechanism of action Side effects

Drugs that decrease NE Clonidine (Catapres) Agonist at NE Hypotension,
actions autoreceptors (alpha2), drowsiness,
Inhibits the release of lightheadedness, dry
more NE mouth, dizziness,
constipation
Propanolol (Inderal) Antagonists at beta Nausea,diarrhea, ,
adrenergic receptors, bradycardia,
blocks NE activity at hypotension,fatigue,
beta receptors dizziness, abnormal
vision, hallucinations
Atenolol (Tenormin) Antagonists at beta Nausea,diarrhea, ,
adrenergic receptors, bradycardia,
blocks NE activity at hypotension,fatigue,
beta receptors dizziness, abnormal
vision, hallucinations
Timolol (Timoptic) Antagonists at beta Nausea,diarrhea, ,
adrenergic receptors, bradycardia,
blocks NE activity at hypotension,fatigue,
beta receptors dizziness, abnormal
vision, hallucinations

Drugs used for ADHD

Category Drug Mechanism of action Side effects

Atomoxetine Inhibits the reuptake of Sexual & GI
(Straterra) NE disturbances
Methylphenidate Inhibits the reuptake of Psychosis, difficulty
(Ritalin) dopamine and NE sleeping, mood swings,
nervousness, GI and sex
drive disturbances,
headaches, tachycardia
 Antidepressant Agents
Category Drug Mechanism of action Side effects
Tricyclic Norepinephrine and
Antidepressants serotonin reuptake
(TCAs) inhibitors
Imipramine (Tofranil) Sedative ++,
Antimuscarinic ++
Amitriptyline (Elavil) Sedative +++,
Antimuscarinic +++
Doxepin (Adapin) Sedative +++,
Antimuscarinic +++
Desipramine mainly inhibits NE Sedative +,
(Norpramin) reuptake Antimuscarinic +
Clomipramine Sedative +++,
(Anafranil) Antimuscarinic ++
Protriptyline (Vivactil) Antimuscarinic ++,
Sedative ++
Second generation Nortriptyline (Aventy, Sedative ++,
TCAs Pamelor) Antimuscarinic ++
Amoxapine (Asendin) also inhibits some Sedative ++,
dopamine reuptake Antimuscarinic ++,
Akathisia
Maprotiline (Ludiomil) mainly inhibits NE Sedative ++,
reuptake Antimuscarinic ++
*Trazodone (Desyrel) mainly inhibits 5-HT2 Sedative +++,
receptors Dizziness, Insomia
***Bupropion also inhibits some Dizziness, Tremor,
(Wellbutrin) dopamine reuptake Seizures at high doses
Third generation TCAs **Mirtazapine Alpha2 antagonism Sedative +++,
(Remeron) Weight gain, Dizziness
*Nefazodone (Serzone) Mainly inhibits 5-HT2 Sedative ++,
receptors Antimuscarinic +++,
Dizziness, Insomia,
Inhibits CYP3A4
Selective Serotonin & Venlafaxine (Effexor) Selectively inhibits NE Hypertension, anxiety,
Norepinephrine & 5-HT uptake Dizziness,
reuptake inhbitors Strong sexual & GI
(SSNRIs) disturbances,
Duloxetine (Cymbalta) Selectively inhibits NE Hypertension, anxiety,
& 5-HT uptake Dizziness,
Urinary disturbances
Selective Serotonin Serotonin uptake
Reuptake Inhibitors inhibitors
(SSRIs)
Fluoxetine (Prozac) Sedative +,
Antimuscarinic action +,
Sexual & GI
disturbances, Insomia
Paroxetine (Paxil) Sedative +,
Strong sexual & GI
disturbances, Insomia,
Inhibits CYP2D6
Sertaline (Zoloft) Sedative +,
 Strong sexual & GI
disturbances, Insomia,
Inhibits CYP2D6
Fluvoxamine (Luvox) Sexual & GI
disturbances, Insomia,
Inhibits CYP3A4
Citalopram (Celexa) Sexual & GI
disturbances, Insomia
Escitalopram Sexual & GI
(Lexapro) disturbances, Insomia
Monoamine Oxidase Inhibit the breakdown of
Inhibitors (MAOIs) norepinephrine,
serotonin &dopamine
Phenelzine (Nardil) Sedation,
Hypotension,
Weight gain,
Strong sexual
disturbances,
Dietary Restrictions
(tyramine)
Tranylcypromine Agitation,
(Parnate) Hypotension,
Weight gain,
Sexual disturbances,
Dietary Restrictions
(tyramine)
Selegiline (Eldepryl) & also inhibits dopamine Mild sexual disturbances
(Emsam) breakdown (MAO-B)

*Trazodone, nefazodone and mirtazapine are unique in that they also antagonize the 5-HT2A or 5-HT2C .
**Mirtazapine is unique as it also antagonizes the α2 NE receptors.
***Bupropion is unique in that it will inhibit approx. 25% of dopamine uptake.
Note: all antidepressants result in the increase in serotonin levels at the synapse. Several of the antidepressants also
result in increased synaptic levels of norepinephrine.
Note: SSRIs and TCAs should not be given with MAOIs for 2 to 3 weeks after MAOIs discontinuation since the
combination can result in a sometimes fatal serotonin syndrome.
Note: MAOIs have long lasting effects (7 days to 3 wks) after discontinuation.
All TCAs at higher doses can produce cardiac problems including orthostatic hypotension, conduction defects and
arrhythmias as well as seizures, weight gain and sexual disturbances.

Drugs used as Mood Stabilizers

Category Drug Mechanism of action Side effects

Lithium Inhibits neuronal PI Hypothyroidism,
turnover inhibiting Polyuria & polydipsia,
second messenger Edema,
activity, ECG changes ↓T-waves
Valproic Acid Increases GABA levels, GI disturbances,
(Depakene), Valproate May block Na+ currents Weight gain,
or Divalproex similar to Hepatotoxic
(Depakote) Carbamazepine Teratogen
 Carbamazepine Prolong inactivation of Dipolpia,
(Tegretol) sodium channels Ataxia,
(slows rate of Na+ GI disturbances,
channel recovery from Drowsiness
inactivation) Teratogen

Drugs used for Psychosis (antipsychotics)

Category Drug Mechanism of action Side effects

Typical Fluphenazine (Permitil, Antagonist at dopamine Extrapyramidal
Prolixin) D2, D4, D1, adrenergic α1, reactions+++,
serotonin 5-HT2, Sedation +,
histamine H1, muscarinic Hypotensive +,
receptors Anticholinergics +
Haloperidol (Haldol) Antagonist at dopamine Extrapyramidal reactions
D2, D4, D1, adrenergic α1, +++,
serotonin 5-HT2, Sedation +,
histamine H1 receptors Hypotensive +
Atypical Risperidone (Risperdal) Antagonist at serotonin Extrapyramidal reactions
(reduced extrapyramidal 5-HT2, dopamine D2, D4, +,
side effects) adrenergic α1, histamine Sedation ++,
H1 receptors Hypotensive ++
Olanzepine (Zyprexa) Antagonist at serotonin Sedation +
5-HT2, dopamine D2, D4, Hypotensive +,
muscarinic, histamine Anticholinergics +,
H1, adrenergic α1, Weight gain +
receptors
Aripiprazole (Abilify) Partial agonist at Sedation 0/+,
dopamine D2 and Hypotensive 0/+
serotonin 5-HT1a
Clozapine (Clozaril) Antagonist at serotonin Sedation++,
5-HT2, dopamine D4, D1, Hypotensive ++,
D2, histamine H1, Anticholinergics +,
muscarinic, adrenergic Weight gain +,
α1, receptors Hematologic disturbance

Quetiapine (Seroquel) Antagonist at serotonin Sedation++,

5-HT2, 5-HT1A, Hypotensive ++,
dopamine D1, D2, Headaches +,
histamine H1, adrenergic Weight gain +,
α1, α2, receptors Tachycardia

Note: extrapyramidal reactions include motor movements that do not involve the direct activity of the “pyramids”
(i.e., corticospinal and corticobulbar tracts) these would include akinesia (inability to initiate movement) and
akathisia (restlessness) dyskinesia (involuntary movements) bradykinesia (slow movement).
Note: the inhibition of dopamine receptors can cause an increase in prolactin synthesis and secretion

Drugs used for Alzheimer’s Disease

Category Drug Mechanism of action Side effects

Acetylcholinesterase
Inhibitors (AChE
inhibitors) cross the
BBB
Donepezil (Aricept) Inhibits the breakdown Nausea,
of acetylcholine, hence Diarrhea,
more Ach remains in the Vomiting,
synapse Insomia
Rivastigmine Inhibits the breakdown Nausea,
(Excelon) of acetylcholine, hence Diarrhea,
more Ach remains in the Vomiting,
synapse Insomia
Galantamine (Reminyl) Inhibits the breakdown Nausea,
of acetylcholine, hence Diarrhea,
more Ach remains in the Vomiting,
synapse Insomia
Glutamate NMDA Memantine (Namenda) Blocks the “open-state” Confusion, dizziness,
receptor antagonist of NMDA glutamate drowsiness, headache,
channels causing a insomnia, agitation,
decrease in the influx of and/or hallucinations
calcium.

Drugs used for Narcolepsy & Sleep Apnea

Category Drug Mechanism of action Side effects

Increase the release of Modafinil (Provigil) Increase the release of Drug-induced rash, life
catecholamines & norepinephrine, threatening skin
histamine dopamine and histamine reactions (Stevens-
by possibly increasing Johnson Syndrome and
orexin (hypocretin) Toxic Epidermal
neuron activity Necrolysis), erythema
multiforme,
induces CYP3A4,
CYP2B6, CYP1A2
Armodafinil (Nuvigil)