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8/7/2019 Drug table for Neuroscience 11-23-2010
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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 arenot 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
gated sodium channels
(VGSC)
Systemic doses can
result in death due to the
blockade of respiration,cardiovascular problems
and depress smoothmuscle 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
duration of action.
As above
Benzocaine As above lacks
efficacy
As above
Cocaine As above, in addition to
VGSC blockadedue
to its ability to block
reuptake of NE can also
result in local
vasoconstriction
As above ..can also
lead to addiction due to
its ability to block
reuptake of dopamine
Neuromuscular Blockers
Category Drug Mechanism of action Side effects
Competitive agents Tubocurarine Skeletal muscle
nicotinic channel
antagonist
Ganglionic blockade
causing decrease in
blood pressure andtachycardia. Release of
histamine. Respiratory
paralysis.
Pancuronium As above long
duration of action
As above yet side
effects decreased with
the rest of the agents
listed
Rocuronium As above As above
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.intermediate duration
of action
Atracurium As above
.intermediate duration
of action
As above
Vecuronium As above
.intermediate durationof action
As above
Mivacurium As above shorter
duration of action
As above
Depolarizing agent Succinylcholine
(Acectine, Scoline)
Skeletal muscle
nicotinic channel
agonist
Ganglionic effects,
decrease in blood
pressure and
tachycardia. Release of
histamine. Respiratory
paralysis.
Spasmolytics (muscle relaxants)
Category Drug Mechanism of action Side effects
Dantrolene (Dantrium)
used for malignant
hyperthermia and ALS
Blocks calcium release
from the sarcoplasmic
reticulum by blocking
the ryanodine receptor.
Dizziness, Drowsiness,
weakness, fatigue, GI
disturbances, respiratory
depression
Diazepam (Valium) Potentiate GABAs
ability to open the
GABAA chloridechannel (increase
channel openingfrequency)
Sedation,
Ataxia,
Dependence
Baclofen (Kemstro,Lioresal)
GABAB agonist (GPCRinhibitory coupling)
Dizziness, Drowsiness,weakness, fatigue,
seizures, hallucinations
Botulinum Toxin
(Botox, Dysport)
Inhibits release of
acetylcholine at he NMJ
Anxiety, Dizziness,
Drowsiness, dry eyes &
mouth, back & neck
pain
Drugs used for Pain
Category Drug Mechanism of action Side effects
Opioids (used for acute
and chronic pain)
Morphine Acts at mu GPCR to
cause opening of K+
channels and blocks
VGCC
Nausea/emesis,
constipation, sedation,
somnolence, pruritis,
respiratory depression,
abuse potential
Codeine As above yet less potent As above
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than morphine, better
bioavailability
Oxycodone (in
Percocet, Percodan)
As above As above
Hydrocodone (inVicodin)
As above As above
Hydromorphone
(Dilaudid)
As above yet 10 fold
more potent than
morphine
As above
Fentanyl (Actiq,
Duragesic, Fentora,
etc)
As above yet Mu
agonist, 100 times more
potent than morphine
As above
Sufentanil (Sufenta) As above yet 1000 fold
more potent than
morphine
As above
Alfentanil (Alfenta) As above yet 80 fold
more potent than
morphine
As above
Remifentanil (Ultiva) As above yet 100 fold
more potent than
morphine
As above
Methadone
(Dolophine)
Orally available mu
opioid agonist
As above
Meperidine (Demerol) As above yet 5 to 10
fold less potent than
morphine
As above, also large
doses can cause the
accumulation of
normeperidine, seizures,
hallucinations;
contraindicated in
patients with renal
insufficiency
Loperamide
(Imodium)
Weak mu agonists that
does not cross the bloodbrain barrier, used for
diarrhea
Can cause severe
constipation.
Tramadol (Ultram) Weak mu agonist, also
inhibits uptake of NE
and 5HT
As above like other mu
opioid agonists that
penetrate the CNS but
thought to have less
abuse potential
NSAIDs
Aspirin Irreversible COX
inhibition
All COX inhibitors can
result in GI irritation,
GERD and GI ulcers
Ibuprofen (Advil,
Motrin, Nuprin)
Reversible COX
inhibition
As above
Indomethacin(Indocin)
As above As above
Ketorolac (Lodine) As above As above
Ketoprofen (Orudis,
Oruvail)
As above As above
Naproxen (Aleve) As above As above
Celecoxib (Celebrex) Irreversible COX2 Lacks GI effects, Can
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inhibition cause cardiovascular
problems including
stroke and myocardial
infarction, can decrease
kidney function
Steroids
Dexamethasone Increase levels oflipocortin that inhibits
phospholipase A2,
decreasing inflammatory
mediators
(oral admin)
Prolonged use can leadto immunosuppression
and cushingoid (central
obesity, moon face,
hyperglycemia,
osteoporosis, etc.)
Prednisone As above (oral admin) As above
Budesonide (Entocort)
(Symbocort +
formoterol)
As above (Inhaled
admin)
As above
Hydrocortisone As above (Topical
admin)
As above
Additional drugs used
for chronic pain Gabapentin
(Neurontin)
Unknown mechanism
but thought to inhibit
voltage-sensitive
calcium channels
Sedation, somnolence,
dizziness, ataxia,
peripheral edema
Pregabalin (Lyrica) Sedation, somnolence,
dizziness, ataxia,
peripheral edema, visual
disturbances
Tricyclic antidepressants
(TCAs)
Norepinephrine and
serotonin uptake
inhibitors
Sedative,
Antimuscarinic action
Selective serotonin
reuptake inhibitors(SSRIs)
Serotonin uptake
inhibitors
Sedative, Insomia,
Antimuscarinic action ,Sexual & GI
disturbances
Lidocaine (lidoderm
patch)
Blocks voltage gated
sodium channels
If high systemic doses
are reached can causecardiovascular
arrhythmia, seizures
Migraine Medications
Category Drug Mechanism of action Side effects
Triptans Sumatriptan (Imitrex) 5HT1B and 5HT1Dagonists
Cardiovascular ,
coronary artery
vasospasm,Contraindicated in
individuals with
previous MI
Rizatriptan (Maxalt) As above As above
Zolmitriptan (Zomig) As above As above
Naratriptan (Amerge) As above, longest acting
of the triptans (1/2 life 6
As above
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hours)
Opioids (are used for
migraine)
See above in acute pain
meds
See above in acute pain
meds
See above in acute pain
meds
NSAIDs See above in acute pain
meds
See above in acute pain
meds
See above in acute pain
meds
Topiramate
(Topamax)
Reduces voltage gated
sodium channel activity,increase activity at
GABAA CL- channels,
some inhibition of
glutamate AMPA-
kainate channels and
carbonic anhydrase
inhibitor
Somnolence, fatigue,
nervousness, weightloss, Psychomotor
slowing
Stroke
Category Drug Mechanism of action Side effects
Clot busters tPA A serine protease andcatalyzes the conversion
of plasminogen to
plasmin
Risk of hemorrhage
Antiplatelet Aspirin Irreversible inhibition of
COX decreasing platelet
production of
thromboxane (TXA2)
GI disturbances
Antiplatelet Clopidogrel (Plavix) Blocks irreversibly the
ADP receptor P2Y12
inhibiting platelet
aggregation by
inhibiting activation ofthe glycoprotein IIb/IIIa
pathway
Risk of bleeding,
bleeding risk increases
dramatically when in
combination with drugs
like aspirin
Ocular PharmacologyCategory Drug Mechanism of action Side effects
Ocular Hypertension
Decrease synthesis
Timolol (Timoptic)
Betaxolol (Betagan)
Beta-2 receptor
antagonist (Inhibit
aqueous humor
secretion)
Bronchospasm,
bradycardia
Brimonidine
(Alphagan)Apraclonidine
(Iopidine)
Alpha-2 receptor agonist
(Inhibit aqueous humorsecretion)
Ocular allergy
Dorzolamide
(Trusopt)
Acetazolamide
Carbonic anhydrase
inhibitor (Inhibit
aqueous humor
secretion)
Malaise, fatigue, weight
loss, anorexia,
depression
Pilocarpine, carbachol Cholinergic agonist
(Stimulates contractionof ciliary muscle which
Accommodation
(reduced visual acuity),miosis (dimmed vision),
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Increase outflow
stretches open trabecular
outflow pathway
(pressure-dependent))
brow ache (muscle
spasm)
Echothiophate,
(Phospholine Iodide),
Physostigmine (Isoptoserine)
Acetylcholinesterase
inhibitor (Promotes
contraction of ciliary
muscle which stretchesopen trabecular outflow
pathway)
Accommodation
(reduced visual acuity),
miosis (dimmed vision),
brow ache (musclespasm)
Latanoprost (Xalatan),
Bimatoprost
Prostaglandin FP
receptor agonist
(Increases uveoscleral
(pressure-independent)outflow)
Eyelash growth, iridial
pigmentation,
conjunctival hyperemia
Mydriasis Atropine (Atriposol),Scopolamine (Isopto
Hyoscine)
Muscarinic antagonist(Inhibit contraction of
circular muscle)
Photosensitivity, blurredvision
Phenylephrine (AK-
Dilate)
Alpha-1 adrenergic
agonist (Stimulatecontraction of radial
muscle)
Photosensitivity,
conjunctival hyperemia
Corneal Anesthesia Proparacaine
(Alcaine)
Sodium channel blocker
(Decrease excitability of
sensory nerves in
corneal)
Corneal irritation
Epilepsy drugs (Anticonvulsants)
Category Drug Mechanism of action Side effects
Inactivation of Na+
channelsCarbamazepine
(Tegretol)
Prolong fast inactivationof voltage gated sodium
channels
Induces CYP3A4,lifethreatening skin reactions
(Stevens-Johnson SyndromeandToxicEpidermal
Necrolysis ), Teratogen,
drowsiness, headaches, motor
coordination impairment, GI
disturbances
Phenytoin(Phenytek) See above Teratogen, horizontal gazenystagmus, sedation, cerebellar
ataxia, paradoxical seizures
Topiramate (Topamax) in addition increase
activity at GABAA CL-
channels, some
inhibition of glutamate
AMPA-kainatechannels and carbonic
anhydrase inhibitor
Somnolence, fatigue,
nervousness, weight loss
Psychomotor slowing
Lamotrigine(Lamictal) See above life threatening skin reactions(Stevens-Johnson Syndrome
andToxic Epidermal
Necrolysis), headaches,dizziness, insomnia, nightmares,
muscle aches, dry mouth,
http://en.wikipedia.org/wiki/Stevens-Johnson_Syndromehttp://en.wikipedia.org/wiki/Stevens-Johnson_Syndromehttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Motor_coordinationhttp://en.wikipedia.org/wiki/Motor_coordinationhttp://en.wikipedia.org/wiki/Teratogenesishttp://en.wikipedia.org/wiki/Physiologic_nystagmushttp://en.wikipedia.org/wiki/Sedationhttp://en.wikipedia.org/wiki/Ataxiahttp://en.wikipedia.org/wiki/Seizureshttp://en.wikipedia.org/wiki/Seizureshttp://en.wikipedia.org/wiki/Stevens-Johnson_Syndromehttp://en.wikipedia.org/wiki/Stevens-Johnson_Syndromehttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Headachehttp://en.wikipedia.org/wiki/Dizzinesshttp://en.wikipedia.org/wiki/Insomniahttp://en.wikipedia.org/wiki/Nightmarehttp://en.wikipedia.org/wiki/Myalgiahttp://en.wikipedia.org/wiki/Dry_mouthhttp://en.wikipedia.org/wiki/Stevens-Johnson_Syndromehttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Motor_coordinationhttp://en.wikipedia.org/wiki/Motor_coordinationhttp://en.wikipedia.org/wiki/Teratogenesishttp://en.wikipedia.org/wiki/Physiologic_nystagmushttp://en.wikipedia.org/wiki/Sedationhttp://en.wikipedia.org/wiki/Ataxiahttp://en.wikipedia.org/wiki/Seizureshttp://en.wikipedia.org/wiki/Stevens-Johnson_Syndromehttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Headachehttp://en.wikipedia.org/wiki/Dizzinesshttp://en.wikipedia.org/wiki/Insomniahttp://en.wikipedia.org/wiki/Nightmarehttp://en.wikipedia.org/wiki/Myalgiahttp://en.wikipedia.org/wiki/Dry_mouth8/7/2019 Drug table for Neuroscience 11-23-2010
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fatigue, cognitive problems,
weight changes, hairloss,
changes in libido, frequent
urination, nausea,
Rufinamide (Banzel) See above.seizures
associated with Lennox-
Gastaut syndrome
Somnolence, headache, loss of
coordination, uncontrollable
movements, loss of appetite,nausea
Lacosamide (Vimpat) Prolong slow
inactivation of voltage
gated sodium channels
GI disturbances, nausea
vomiting headaches, blurredor
double vision, headache,
drowsiness, loss ofcoordination,
Valproic acid
(Depakene),Divalproex or Valproate
(Depakote)
Teratogen,hepatotoxicityfatigue, GI disturbances,
peripheral edema, dizziness,
drowsiness, hairloss,
headaches, tremors,
hyperammonemia & ensuing
encephalopathy
Zonisamide
(Zonegran)
in addition increase
activity at GABAA CL-
channels, reduce T-type
Ca+2 channel activity
and carbonic anhydrase
inhibitor
Somnolence, drowsiness, loss of
appetite, dizziness, headache,
nausea, and agitation/irritability
Enhanced GABA
synaptic transmission
Benzodiazepines
*Diazepam (Valium) Potentiate GABAs
ability to open the
GABAA CL- channel
(increase channel
opening frequency)
Sedation,
Ataxia,
Dependence
Barbiturates*Pentobarbital(Nembutal)
Potentiate GABAsability to increase
duration of GABAACL- channel openings, at
high concentrations can
open directly
Depression of autonomicganglia,
Respiratory depression,Sedation,
Dependence,
Withdrawal
Vigabatrin (Sabril) Inhibits the breakdownof GABA
Somnolence, headache,dizziness, nervousness,
depression, memory
disturbances, diplopia, ataxia,
GI disturbances
Tiagabine (Gabitril) Blocking re-uptake of
GABA
Confusion, difficulty speaking
clearly/stuttering, mild sedation,
tingling sensation (paresthesia)Voltage gated Ca+2
channel antagonists
Ethosuximide
(Emesideor Zarontin)Reducing current
through the T-type Ca+2
channels
Drowsiness, mental confusion,
insomnia, headache, ataxia, GI
disturbances, hyperactive
Zonisamide (Zonegran) Reducing current
through the T-type Ca+2
channels
Somnolence, drowsiness, loss of
appetite, dizziness, headache,
nausea, and agitation/irritability
http://en.wikipedia.org/wiki/Fatigue_(medical)http://en.wikipedia.org/wiki/Hair_losshttp://en.wikipedia.org/wiki/Hair_losshttp://en.wikipedia.org/wiki/Libidohttp://en.wikipedia.org/wiki/Frequent_urinationhttp://en.wikipedia.org/wiki/Frequent_urinationhttp://en.wikipedia.org/wiki/Frequent_urinationhttp://en.wikipedia.org/wiki/Nauseahttp://en.wikipedia.org/wiki/Fatigue_(medical)http://en.wikipedia.org/wiki/Peripheral_edemahttp://en.wikipedia.org/wiki/Dizzinesshttp://en.wikipedia.org/wiki/Dizzinesshttp://en.wikipedia.org/wiki/Hair_losshttp://en.wikipedia.org/wiki/Hair_losshttp://en.wikipedia.org/wiki/Hair_losshttp://en.wikipedia.org/wiki/Tremorhttp://en.wikipedia.org/wiki/Hyperammonemiahttp://en.wikipedia.org/wiki/Encephalopathyhttp://en.wikipedia.org/wiki/Somnolencehttp://en.wikipedia.org/wiki/Headachehttp://en.wikipedia.org/wiki/Clinical_depressionhttp://en.wikipedia.org/wiki/Diplopiahttp://en.wikipedia.org/wiki/Ataxiahttp://en.wikipedia.org/wiki/Paresthesiahttp://en.wikipedia.org/wiki/Fatigue_(medical)http://en.wikipedia.org/wiki/Hair_losshttp://en.wikipedia.org/wiki/Libidohttp://en.wikipedia.org/wiki/Frequent_urinationhttp://en.wikipedia.org/wiki/Frequent_urinationhttp://en.wikipedia.org/wiki/Nauseahttp://en.wikipedia.org/wiki/Fatigue_(medical)http://en.wikipedia.org/wiki/Peripheral_edemahttp://en.wikipedia.org/wiki/Dizzinesshttp://en.wikipedia.org/wiki/Hair_losshttp://en.wikipedia.org/wiki/Tremorhttp://en.wikipedia.org/wiki/Hyperammonemiahttp://en.wikipedia.org/wiki/Encephalopathyhttp://en.wikipedia.org/wiki/Somnolencehttp://en.wikipedia.org/wiki/Headachehttp://en.wikipedia.org/wiki/Clinical_depressionhttp://en.wikipedia.org/wiki/Diplopiahttp://en.wikipedia.org/wiki/Ataxiahttp://en.wikipedia.org/wiki/Paresthesia8/7/2019 Drug table for Neuroscience 11-23-2010
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Gabapentin
(Neurontin)
Unknown mechanism
but thought to inhibit
voltage-sensitive
calcium channels
Sedation, somnolence,
dizziness, ataxia, peripheral
edema
Trimethadione
(Tridione)
Reducing current
through the T-type Ca+2
channels
Somnolence, drowsiness, loss of
appetite, dizziness, headache,
nausea, and agitation/irritability
Inhibits Vesicular
releaseLevetiracetam (keppra) Binds to a protein (SV2)
on vesicles and inhibits
their release. Overall
decrease in
neurotransmitter release.
Asthenia (weakness),
hallucinations, Sedation,
somnolence, infections, loss of
appetite
Glutamate NMDA
channel antagonistFelbamate (Felbatol) Blocks the open state
of the NMDA channels.
Aplastic anemia, liver failure,
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 Parkinsons Disease
Category Drug Mechanism of action Side effects
Dopamine precursors Carbidopa/Levodopa
(Sinemet) or (Atamet)
Levodopa is
decarboxylated to form
dopamine in the CNS;
Carbidopa is added to
levodopa since it
inhibits the breakdownby the GI tract.
GI disturbances,
Dyskinesias-excessive
and abnormal
involuntary movements,
Hallucinations and
confusion,Orthostatic hypotension
Dopamine agonists Bromocriptine
(Parlodel) ergot
derivatives
Dopamine D2 receptor
agonist & D1 partial
agonist
Hallucinations and
confusion, GI
distubances
Orthostatic hypotension,Cardiac valve trouble,
Pergolide (Permax)ergot derivatives
Dopamine D2 receptor
agonist & D1 receptor
partial agonist
Hallucinations and
confusion,
Orthostatic hypotension,
Cardiac valve trouble,
Ropinirole (Requip) Dopamine D
2
& D3
receptor agonist Sleep disturbances,Drowsiness
Pramipexole (Mirapex) Dopamine D2 & D3receptor agonist
Sleep disturbances,
Drowsiness
COMT inhibitors Tolcapone (Tasmar) Inhibitors of catechol-O-
methyltransferase,
inhibits dopamine
breakdown
GI disturbances,
Hepatotoxicity,
Hallucinations and
confusion,
Orthostatic hypotension
Entacapone (Comtan) Inhibitors of catechol-O- GI disturbances,
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methyltransferase,
inhibits dopamine
breakdown
Hallucinations and
confusion,
Orthostatic hypotension
MAO inhibitors Selegiline (Eldepryl) Inhibitor of monoamine
oxidase B isoenzyme,
inhibits dopamine
breakdown in striatum
Sedation,
Hypotension,
Weight gain,
Sexual disturbances
Drugs used for Amyotrophic Lateral Sclerosis (ALS) Lou Gehrigs Disease
Category Drug Mechanism of action Side effects
Diminish
neuroexcitotoxicityRiluzole (Rilutek) Inhibits glutamate
release, Antagonist at
NMDA and Kainate-
type glutamate
receptors, Antagonist at
voltage-dependent
sodium channels
Nausea,
Diarrhea,
Weight loss,
Dizziness,
Hepatic injury
Reduces spasticity Baclofen (Lioresal) GABAB agonist-produces inhibitory
effects in the CNS
Weakness,CNS depression
Drugs used for Myasthenia Gravis
Category Drug Mechanism of action Side effects
Cholinergic enhancers Neostigmine
(Prostigmin)
AcetylcholinesteraseInhibitors (reversible
AChE inhibitors) Tend
to not cross the BBB
GI disturbances,increased salivation &
bronchial secreations,
tearing (SLUDGE)
Pyridostigmine
(Mestinon)
Edrophonium
(Tensilon)
Immunosuppressive
drugsPrednisone (Deltasone) Synthetic corticosteroid
acts at several levels to
inhibit the immune
system (Tcells,
cytokines, etc.)
Prolonged use can lead
to immunosuppression
and cushingoid (central
obesity, moon face,
hyperglycemia,
osteoporosis, etc.)
Drugs used for Huntingtons Disease
Category Drug Mechanism of action Side effects
VMAT inhibitor Tetrabenazine
(Xenazine)
Inhibition of dopamine
uptake into vesicles, results
in the degradation ofdopamine
Akathisia, dizziness,
depression,
Parkinsonism
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Dopamine antagonist Risperidone
(Risperdal)
Inhibition of dopamine D2receptors
Drug induced
parkinsons-like
behavior,
Hypotension
Haloperidol (Haldol) Inhibition of dopamine D2receptors
Drug induced
parkinsons-like
behavior,Hypotension
Clozapine (Clozaril) Inhibition of dopamine D2receptors
Sedation,
Hypotension
Olanzapine (Zyprexa) Inhibition of dopamine D2receptors
Sedation,
Hypotension,
Weight gain
Quetiapine (Seroquel) Inhibition of dopamine D2receptors
Sedation,
Hypotension
Selective serotonin
reuptake inhibitors
(SSRIs)
Fluoxetine (Prozac)
Used to treat the
depression (can include
other antidepressants)
Serotonin uptake inhibitors Sedative +,
Antimuscarinic
action +,
Sexual & GIdisturbances,Insomia
Anti-anxiety (Anxiolytic) Drugs
(Sedative-Hypnotics)Category Drug Mechanism of action Side effects
Long-acting
benzodiazepines
Potentiate GABAs ability
to open the GABAAchloride channel (increase
channel openingfrequency)
Diazepam (valium) Sedation,Ataxia,
Dependence
Chlordiazepoxide
(Librium)
Sedation,
Ataxia,
Dependence
Clorazepate
(Tranxene)
Sedation,
Ataxia,
Dependence
Clonazepam
(Klonopin)
Sedation,
Ataxia,
Dependence
Flurazepam
(Dalmane)
Sedation,
Ataxia,Dependence
Short-acting
benzodiazepines
Potentiate GABAs ability
to open the GABAAchloride channel (increase
channel openingfrequency)
Oxazepam (Serax) Sedation,
Ataxia,
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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
to open the GABAAchloride channel (increase
channel openingfrequency)
Sedation,
Dizziness
Zaleplon (Sonata) Potentiate GABAs ability
to open the GABAAchloride channel (increase
channel openingfrequency)
Sedation,
Dizziness
Eszopiclone (Lunesta) Potentiate GABAs ability
to open the GABAAchloride channel (increase
channel openingfrequency)
Sedation,
Dizziness,
Somnolence
Chloral hydrate Increase duration of
GABAA chloride channel
openings, at highconcentrations can open
directly
Sudden acute
intoxication-death,
Dependence,Severe withdrawal,
Liver damage
Buspirone (BuSpar) 5-HT1A receptor partial
agonist
Sedation, Ataxia,
Should not be takenwith MAOIs,
Withdrawal
Barbiturates Increase duration of
GABAA chloride channel
openings, at high
concentrations can open
directly
Depression of
autonomic ganglia,
Respiratory depression,
Sedation,
Dependence,
Withdrawal
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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 drugs 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
actionsClonidine (Catapres) Agonist at NE
autoreceptors (alpha2),
Inhibits the release of
more NE
Hypotension,
drowsiness,
lightheadedness, dry
mouth, dizziness,
constipation
Propanolol (Inderal) Antagonists at beta
adrenergic receptors,
blocks NE activity at
beta receptors
Nausea,diarrhea, ,
bradycardia,
hypotension,fatigue,
dizziness, abnormal
vision, hallucinations
Atenolol (Tenormin) Antagonists at beta
adrenergic receptors,
blocks NE activity at
beta receptors
Nausea,diarrhea, ,
bradycardia,
hypotension,fatigue,
dizziness, abnormalvision, hallucinations
Timolol (Timoptic) Antagonists at betaadrenergic receptors,
blocks NE activity at
beta receptors
Nausea,diarrhea, ,bradycardia,
hypotension,fatigue,
dizziness, abnormal
vision, hallucinations
Drugs used for ADHD
Category Drug Mechanism of action Side effects
Atomoxetine(Straterra)
Inhibits the reuptake ofNE Sexual & GIdisturbances
Methylphenidate
(Ritalin)
Inhibits the reuptake of
dopamine and NE
Psychosis, difficulty
sleeping, mood swings,
nervousness, GI and sex
drive disturbances,
headaches, tachycardia
http://en.wikipedia.org/wiki/Nauseahttp://en.wikipedia.org/wiki/Diarrheahttp://en.wikipedia.org/wiki/Bronchospasmhttp://en.wikipedia.org/wiki/Bradycardiahttp://en.wikipedia.org/wiki/Bradycardiahttp://en.wikipedia.org/wiki/Hypotensionhttp://en.wikipedia.org/wiki/Hypotensionhttp://en.wikipedia.org/wiki/Fatigue_(medical)http://en.wikipedia.org/wiki/Dizzinesshttp://en.wikipedia.org/wiki/Nauseahttp://en.wikipedia.org/wiki/Diarrheahttp://en.wikipedia.org/wiki/Bronchospasmhttp://en.wikipedia.org/wiki/Bradycardiahttp://en.wikipedia.org/wiki/Bradycardiahttp://en.wikipedia.org/wiki/Hypotensionhttp://en.wikipedia.org/wiki/Hypotensionhttp://en.wikipedia.org/wiki/Fatigue_(medical)http://en.wikipedia.org/wiki/Dizzinesshttp://en.wikipedia.org/wiki/Nauseahttp://en.wikipedia.org/wiki/Diarrheahttp://en.wikipedia.org/wiki/Bronchospasmhttp://en.wikipedia.org/wiki/Bradycardiahttp://en.wikipedia.org/wiki/Bradycardiahttp://en.wikipedia.org/wiki/Hypotensionhttp://en.wikipedia.org/wiki/Hypotensionhttp://en.wikipedia.org/wiki/Fatigue_(medical)http://en.wikipedia.org/wiki/Dizzinesshttp://en.wikipedia.org/wiki/Nauseahttp://en.wikipedia.org/wiki/Diarrheahttp://en.wikipedia.org/wiki/Bronchospasmhttp://en.wikipedia.org/wiki/Bradycardiahttp://en.wikipedia.org/wiki/Hypotensionhttp://en.wikipedia.org/wiki/Fatigue_(medical)http://en.wikipedia.org/wiki/Dizzinesshttp://en.wikipedia.org/wiki/Nauseahttp://en.wikipedia.org/wiki/Diarrheahttp://en.wikipedia.org/wiki/Bronchospasmhttp://en.wikipedia.org/wiki/Bradycardiahttp://en.wikipedia.org/wiki/Hypotensionhttp://en.wikipedia.org/wiki/Fatigue_(medical)http://en.wikipedia.org/wiki/Dizzinesshttp://en.wikipedia.org/wiki/Nauseahttp://en.wikipedia.org/wiki/Diarrheahttp://en.wikipedia.org/wiki/Bronchospasmhttp://en.wikipedia.org/wiki/Bradycardiahttp://en.wikipedia.org/wiki/Hypotensionhttp://en.wikipedia.org/wiki/Fatigue_(medical)http://en.wikipedia.org/wiki/Dizziness8/7/2019 Drug table for Neuroscience 11-23-2010
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Antidepressant AgentsCategory Drug Mechanism of action Side effects
Tricyclic
Antidepressants
(TCAs)
Norepinephrine and
serotonin reuptake
inhibitors
Imipramine (Tofranil) Sedative ++,Antimuscarinic ++
Amitriptyline (Elavil) Sedative +++,
Antimuscarinic +++
Doxepin (Adapin) Sedative +++,
Antimuscarinic +++
Desipramine
(Norpramin)
mainly inhibits NE
reuptake
Sedative +,
Antimuscarinic +
Clomipramine
(Anafranil)
Sedative +++,
Antimuscarinic ++
Protriptyline (Vivactil) Antimuscarinic ++,Sedative ++
Second generation
TCAs
Nortriptyline (Aventy,
Pamelor)
Sedative ++,
Antimuscarinic ++
Amoxapine (Asendin) also inhibits somedopamine reuptake
Sedative ++,Antimuscarinic ++,
Akathisia
Maprotiline (Ludiomil) mainly inhibits NE
reuptake
Sedative ++,
Antimuscarinic ++
*Trazodone (Desyrel) mainly inhibits 5-HT2
receptors
Sedative +++,
Dizziness, Insomia
***Bupropion
(Wellbutrin)
also inhibits some
dopamine reuptake
Dizziness, Tremor,
Seizures at high doses
Third generation TCAs **Mirtazapine
(Remeron)
Alpha2 antagonism Sedative +++,
Weight gain, Dizziness
*Nefazodone (Serzone) Mainly inhibits 5-HT2receptors Sedative ++,Antimuscarinic +++,
Dizziness, Insomia,
Inhibits CYP3A4
Selective Serotonin &
Norepinephrine
reuptake inhbitors
(SSNRIs)
Venlafaxine (Effexor) Selectively inhibits NE
& 5-HT uptake
Hypertension, anxiety,
Dizziness,
Strong sexual & GI
disturbances,
Duloxetine (Cymbalta) Selectively inhibits NE
& 5-HT uptake
Hypertension, anxiety,
Dizziness,Urinary disturbances
Selective Serotonin
Reuptake Inhibitors
(SSRIs)
Serotonin uptakeinhibitors
Fluoxetine (Prozac) Sedative +,
Antimuscarinic action +,Sexual & GI
disturbances, Insomia
Paroxetine (Paxil) Sedative +,
Strong sexual & GI
disturbances, Insomia,
Inhibits CYP2D6
Sertaline (Zoloft) Sedative +,
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Strong sexual & GI
disturbances, Insomia,
Inhibits CYP2D6
Fluvoxamine (Luvox) Sexual & GI
disturbances, Insomia,
Inhibits CYP3A4
Citalopram (Celexa) Sexual & GIdisturbances, Insomia
Escitalopram
(Lexapro)
Sexual & GI
disturbances, Insomia
Monoamine Oxidase
Inhibitors (MAOIs)
Inhibit the breakdown of
norepinephrine,
serotonin &dopamine
Phenelzine (Nardil) Sedation,
Hypotension,
Weight gain,
Strong sexual
disturbances,
Dietary Restrictions
(tyramine)Tranylcypromine
(Parnate)
Agitation,
Hypotension,
Weight gain,
Sexual disturbances,Dietary Restrictions
(tyramine)
Selegiline (Eldepryl) &
(Emsam)
also inhibits dopamine
breakdown (MAO-B)
Mild sexual disturbances
*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 2 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 alsoresult 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 thecombination 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
turnover inhibiting
second messenger
activity,
Hypothyroidism,
Polyuria & polydipsia,
Edema,
ECG changes T-waves
Valproic Acid
(Depakene), Valproate
orDivalproex
(Depakote)
Increases GABA levels,
May block Na+ currents
similar to
Carbamazepine
GI disturbances,
Weight gain,
Hepatotoxic
Teratogen
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Carbamazepine
(Tegretol)
Prolong inactivation of
sodium channels
(slows rate of Na+
channel recovery from
inactivation)
Dipolpia,
Ataxia,
GI disturbances,
Drowsiness
Teratogen
Drugs used for Psychosis (antipsychotics)
Category Drug Mechanism of action Side effects
Typical Fluphenazine (Permitil,
Prolixin)
Antagonist at dopamine
D2, D4, D1, adrenergic 1,
serotonin 5-HT2,
histamine H1, muscarinic
receptors
Extrapyramidal
reactions+++,
Sedation +,
Hypotensive +,
Anticholinergics +
Haloperidol (Haldol) Antagonist at dopamine
D2, D4, D1, adrenergic 1,
serotonin 5-HT2,histamine H1 receptors
Extrapyramidal reactions
+++,
Sedation +,Hypotensive +
Atypical
(reduced extrapyramidalside effects)
Risperidone (Risperdal) Antagonist at serotonin
5-HT2, dopamine D2, D4,adrenergic 1, histamine
H1 receptors
Extrapyramidal reactions
+,Sedation ++,
Hypotensive ++
Olanzepine (Zyprexa) Antagonist at serotonin5-HT2, dopamine D2, D4,muscarinic, histamine
H1, adrenergic 1,
receptors
Sedation +Hypotensive +,
Anticholinergics +,
Weight gain +
Aripiprazole (Abilify) Partial agonist at
dopamine D2 and
serotonin 5-HT1a
Sedation 0/+,
Hypotensive 0/+
Clozapine (Clozaril) Antagonist at serotonin
5-HT2, dopamine D4, D1,
D2, histamine H1,muscarinic, adrenergic
1, receptors
Sedation++,
Hypotensive ++,
Anticholinergics +,Weight gain +,
Hematologic disturbance
Quetiapine (Seroquel) Antagonist at serotonin
5-HT2, 5-HT1A,dopamine D1, D2,
histamine H1, adrenergic
1, 2, receptors
Sedation++,
Hypotensive ++,Headaches +,
Weight gain +,
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) andakathisia (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 Alzheimers Disease
Category Drug Mechanism of action Side effects
Acetylcholinesterase
http://en.wikipedia.org/wiki/Akinesiahttp://en.wikipedia.org/wiki/Akathisiahttp://en.wikipedia.org/wiki/Dyskinesiahttp://en.wikipedia.org/wiki/Akinesiahttp://en.wikipedia.org/wiki/Akathisiahttp://en.wikipedia.org/wiki/Dyskinesia8/7/2019 Drug table for Neuroscience 11-23-2010
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Inhibitors (AChE
inhibitors) cross the
BBB
Donepezil (Aricept) Inhibits the breakdown
of acetylcholine, hence
more Ach remains in the
synapse
Nausea,
Diarrhea,
Vomiting,
InsomiaRivastigmine
(Excelon)
Inhibits the breakdown
of acetylcholine, hence
more Ach remains in the
synapse
Nausea,
Diarrhea,
Vomiting,
Insomia
Galantamine (Reminyl) Inhibits the breakdown
of acetylcholine, hence
more Ach remains in the
synapse
Nausea,
Diarrhea,
Vomiting,
Insomia
Glutamate NMDA
receptor antagonistMemantine (Namenda) Blocks the open-state
of NMDA glutamate
channels causing a
decrease in the influx ofcalcium.
Confusion, dizziness,
drowsiness, headache,
insomnia, agitation,
and/or hallucinations
Drugs used for Narcolepsy & Sleep Apnea
Category Drug Mechanism of action Side effects
Increase the release ofcatecholamines &
histamine
Modafinil (Provigil) Increase the release ofnorepinephrine,
dopamine and histamineby possibly increasing
orexin (hypocretin)neuron activity
Drug-induced rash, lifethreatening skin
reactions (Stevens-
Johnson Syndromeand
Toxic Epidermal
Necrolysis), erythema
multiforme,
induces CYP3A4,
CYP2B6, CYP1A2Armodafinil (Nuvigil)
http://en.wikipedia.org/wiki/Stevens-Johnson_Syndromehttp://en.wikipedia.org/wiki/Stevens-Johnson_Syndromehttp://en.wikipedia.org/wiki/Stevens-Johnson_Syndromehttp://en.wikipedia.org/wiki/Stevens-Johnson_Syndromehttp://en.wikipedia.org/wiki/Stevens-Johnson_Syndromehttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Stevens-Johnson_Syndromehttp://en.wikipedia.org/wiki/Stevens-Johnson_Syndromehttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysishttp://en.wikipedia.org/wiki/Toxic_Epidermal_Necrolysis