drug table for neuroscience 11-23-2010

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


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


2/16

.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)


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


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


3/16

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


4/16

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


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


5/16

hours)

Opioids (are used for

migraine)

See above in acute pain

meds


meds


meds

NSAIDs See above in acute pain

meds


meds


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


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),


6/16

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)


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_mouth


7/16

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


channels



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/Paresthesia


8/16

Gabapentin

(Neurontin)

Unknown mechanism

but thought to inhibit

voltage-sensitive

calcium channels

Sedation, somnolence,

dizziness, ataxia, peripheral

edema

Trimethadione

(Tridione)

Reducing current


channels




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


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,


9/16

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


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


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


VMAT inhibitor Tetrabenazine

(Xenazine)

Inhibition of dopamine

uptake into vesicles, results

in the degradation ofdopamine

Akathisia, dizziness,

depression,

Parkinsonism


10/16

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


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



Oxazepam (Serax) Sedation,

Ataxia,


11/16

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,

Dizziness

Zaleplon (Sonata) Potentiate GABAs ability



Sedation,

Dizziness

Eszopiclone (Lunesta) Potentiate GABAs ability



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


12/16

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


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,


beta receptors

Nausea,diarrhea, ,

bradycardia,


dizziness, abnormalvision, hallucinations

Timolol (Timoptic) Antagonists at betaadrenergic receptors,


beta receptors

Nausea,diarrhea, ,bradycardia,


dizziness, abnormal

vision, hallucinations

Drugs used for ADHD


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/Dizziness


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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 +,


14/16

Strong sexual & GI


Inhibits CYP2D6

Fluvoxamine (Luvox) Sexual & GI


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


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


15/16

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)


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


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/Dyskinesia


16/16

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



synapse

Nausea,

Diarrhea,

Vomiting,

Insomia

Galantamine (Reminyl) Inhibits the breakdown



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


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

drug table for neuroscience 11-23-2010

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