Name

Brand Name Clinical Indications

Potent naturally occurring analgesic (10mg IM = 4-5

hours of analgesia)

Morphine

Most commonly used drug for treatment of opiate

withdrawal

Methadone
Etorphine

Mixed opiate agonist antagonist. Used in opiate

addiction

Buprenorphine
Naloxone

Narcan

Acute opiod overdose

Diprenorphine

Acute opiod overdose

Nalorphine

analgesic

Pentazocine

analgesic

Oxycodone

roxicodone

Codeine

synthetic form of morphine

Opiate analgesic and antitussive

Oxycontin
Diphenoxylate

Lomotil

antidiarrheal

Percodan

analgesic

Percocet

analgesic

Merperidine

Demerol

L-acetyl-alpha-methadol

LAAM

Synthetic opiate analgesic

Used for treatment of opiate withdrawal

Subutex
Suboxone
Naltrexone

Acute opiod overdose

Fentanyl
Nalbuphine

Endogenous Peptides
Met, Leu-Enkephalin
Beta-endorphin
Dynorphin-A
Dynorphin-B
alpha-Neoendorphin

Mechanism

Binds to mu, K, and delta receptors in spinal cord to block transmission between cfibers and STh neurons. Disinhibits descending pain inhibitors. Decreases substance
P. Modulates affect to make you not care about pain.

Normal opiate effects with less euphoria, mental clouding, and a much longer
duration of action. Withdrawal symptoms less severe, but longer in duration

High mu affinity, partial agonist. Suppresses opiate withdrawal. Less withdrawal

effects.
pure antagonist at mu receptors, reversing the effects of opiod agonists within
minutes
pure antagonist at mu, del, kappa receptors, reversing the effects of opiod agonists
within minutes
antagonist at mu receptors, but agonist at kappa receptors
Partial agonist at u reveptors, agonist at kappa receptors
Decreases the cough reflex in brainstem. Blocks pain by targetting mu, K and delta
receptors. Less analgesia, more antitussive than morphine
long acting oxycodone
acts on mu receptors to abolisj peristalic reflex.
Oxycodone with acetaminophen
Oxycodone with aspirin

Especially targets K receptors in spinal cord and best for acute pain

Long acting version of methadone, used over the weekend in addicts

slower onset long agonist activity than buprenorphine
Subutex with Naloxone, naloxone will not block opiate effects until metabolized
pure antagonist at mu receptors, reversing the effects of opiod agonists within
minutes
Very potent
Strong kappa agonist, mu antagonist

eptides
mu < delta agonist
mu = delta agonist
mu < kappa agonist
mu = delta < kappa agonist
mu = delta < kappa agonist

Side Effects
Constapation and miosis (occor every time with no tolerance).
Nausea, vomitting, sedation, mental clouding, decreased
brainstem response to CO2, thus decreased resp. Smooth
muscle constriction: thus cant use in pregnancy, gall bladder
pain, renal colic pain, and athma.

Can be injected and have the same effect as morphine. Must

be taken orally

can precipitate withdrawls

Less addictive but can induce nausea and vomitting.

little to no morphine-like euphoria

Less constipation, miosis, and less smooth muscle effects. But

highly addictive. CONTRAINDICATED with MAOI and
amphetimines

can precipitate withdrawls

Drug interactions Metabolism Notes

Name

Brand Name Class

Clinical Indications

Topiramate

Topamax

Na channel blocker

Partial Seizures, Generalized tonicclonic Seizures, Prophylaxis against

migraines

Carbamazepine

Tegretol

Na channel blocker

Partial seizures, tonic clonic

seizures, trigeminal nueralgia, bipolar
disorder, neuropathic pain

Phenytoin

Dilantin

Na channel blocker

First line tonic clonic seizures,

partial seizures, treatment of status
epilepticus after BZs

Phenobarbital

Luminal

Barbiturate

tonic-clonic and partial seizures in

children, Antiepileptic choice in
pregnant women, sedative

Primidone

Mysoline

Potentiation of GABA

tonic-clonic, partial, complex partial,

recurrent fibrile convulsions in
children; convulsions associated with
withdrawal

Diazepam

BZ

Status Epilipticus, anxiolytic,

anticonvulsant, sedative, muscle
relaxant, alcohol withdrawl

Benzodiazepines

BZ

Lorazepam (Longer duration);

Clonazepam (absence seizures),
Chlorazepate (Complex partial
seizures

Valproic Acid

Valproate

Ca channel Blockers

Myoclonic seizures (drug of choice);

partial and generalized tonic-clonic
seizures, absence seizures

Ethosuximide

Zarontin

Ca channel Blockers

First line for absence seizures

Lamotrigine

Lamictal

Partial with 2nd generalization seizure

Felbamate

Felbatol

Partial seizure

Topiramate

Topamax

vigabatrin

Sabril

partial seizures

Tiagabine

Gabitril

partial seizures

Gabapentin

Neurontin

partial seizure

Pregabalin

Lyrica

partial seizure

SEE Topiramate
Above

levetiracetam

Keppra

refractory partial seizures

Mechanism

Side Effects
Na channel Blockers

Drug interactions

inhibits excitatory neuro transmission by blocking

the action of glutamate at AMPA/kainate receptors;
weight loss, word finding difficulties,
inhibition of Na channels and potentiation of GABA paresthesias, kidney stones; anti folate
neuro transmission

inhinbits generation of repetative APs by binding to

Na channels; binds to Na channels in inactive
state and prolongs refractory period. Does not
interfere with normal neuronal depolarizations

Rash (Steven-Johnson Syndrome);

water retention; toxic, ataxia

induces P450 enzymes

inhinbits generation of repetative Aps by binding to

Na channels; binds to Na channels in inactive
state and prolongs refractory period. Does not
interfere with normal neuronal depolarizations

nystagmus, diplopia, ataxia, sedation,

Gingival hyperplasia, teratogenic,
decrease Ca absorption, folic acid
deficiency

induces P450 enzymes

Potentiation of GABA
Potentiaties GABA by increasing Cl conduction, at
hight doses and directly activate GABA receptor

sleeping pill OD, sedation, amnesia

Potentiates GABA by increasing Cl conduction =

membrane hyperpolarization

allosteric modulator of GABAa receptor, increases

Cl conductance

induces P450 enzymes

induces P450 enzymes

Tolerance, dependance, withdrawal.

Behavioral disinhibition, psychomotor
probs., Concentration

Ca channel blockers
enhance GABA synthesis and inhibits break down,
inhibits Na channels similar to carbamazepine,
inhibits T-type Ca channels

hepatotoxicity; anti folate

inhibits low threshold T-type Ca channels

GI upsets, aplastic anemia

Hepatic

Antagonism of Glutamate
Blocks NMDA, Na channel block

anti-folate activity

Blocks NMDA, Na channel block, enhances GABA

aplastic anemia

inhibits GABA transaminase

sedation, agitation, weight gain,

psychosis

blocks neuronal and glial uptake of GABA from

difficulty concentrating, abnormal
synapses by inhibiting GAT (GABA transporter) =
thinking (not psychosis), mental lethargy
enhanced GABA inhibitory neuro transmission

hepatic

alpha2-delta modulation
Binds to GABA B and alph 2 delta Ca channel.
Binds to GABA B and alph 2 delta Ca channel.
Others

Few or no side effects, may cause

peripheral edema
Few or no side effects, may cause
peripheral edema

no hepatic metabolism; good for pts with

impaired liver function
no hepatic metabolism; good for pts with
impaired liver function

binds to SV2A; selective blockade of N-type Ca

channels

Metabolism Notes

hepatic/ active
metabolites

dose-dependent
elimination (starts 1st
order -> 0 order)

pH dependent excretion, greater in

alkaline urine

No DDIs

No DDIs
No DDIs

No effect on liver enzymes

No DDIs

Name

Brand Name

Clinical Indications

Sumatriptan
Acute Migraine Headaches
rizatriptan

NSAIDS

administer during early part (aspirin, ibuprofen, naproxen, indomethacin, diclofenac, ketoprofen, ketorolac)

Ergotamine

Dihydroergotamine DHE

Acetaminophen

See NSAID tab

Migraines

Esgic
Acute Migraine Headaches
Excedrin

Methylprednisone

Medrol

Valproate

Valproic acid

metoclopramide

Acute Migraine Headaches

Acute migrianes, Migraine

prophylaxis, bipolar disorder,
epilepsy

antiemetic

Topiramate

Migraine Prophylaxis,
Antiepileptic

Antiepileptic, Prophylaxis against

migraines

Propanolol

See anxiolytic tab

migraine prophylaxis

Amitriptyline

Gabapentin

Migraine Prophylaxis, antiepileptic

Verapamil

cluster headaches

Venlafaxine

See Antidepressants tab

Botulinum Toxin

Botox

Migraine Prophylaxis

Mechanism

A very specific 5HT agonist; constriction of

intracranial vessels (5HT-1b); peripheral and
neuronal inhibition (5HT-1D); enhancement of
descending inhibitory pain pathways

Side Effects

Contraindicated in pts with CAD or

risk factors for CAD;

Drug interactions

not to be used within 2 weeks of MAOI;

Pregnancy class C

proxen, indomethacin, diclofenac, ketoprofen, ketorolac)

Diarrhea, nausea, vommitting;
A 5HT agonist but is less specific than Sumatriptan;
Contraindicated: vascular disease, HTN, Renal
Contraindicated in pts with CAD or
a potent vasocontrictor
failure, Hepatic failure, pregnancy
risk factors for CAD

Combination of acetaminophen, butalbital, caffeine Butalbital in Esgic can be sedating

All of these can lead to rebound (medication
overuse headaches)

Combination of acetaminophen, aspirin, caffeine

Corticosteroid controls inflammation; vascular

permeability

enhances neurotransmission of GABA by inhibiting

GABA-T (gaba transaminase); blocks Na channels
and T-type Ca channels

teratogenicity, bone density, weight gain,

thrombocytopenia, hepatotoxicity, acceleration
of carotid disease, liver enzyme inhibition

controls nausea and vomitting; usually given with

DHE
inhibits excitatory neuro transmission by blocking
the action of glutamate at AMPA/kainate receptors; weight loss, word finding difficulties,
inhibition of Na channels and potentiation of GABA
paresthesias, kidney stones
neuro transmission
Beta-blocker

Binds to GABA B and alph 2 delta Ca channel.

Few or no side effects, may cause

peripheral edema

Ca channel blocker

dizziness, hypotension,
constipation, cardiac conduction
blocks

inhibits release of Ach; highly efficacious

Muscle paralysis

CYP3A inhibitioin

Metabolism

no hepatic
metabolism; good for
pts with impaired liver
function

Notes

Believed to bind to brainstem nuclei and the area around the vasculature near trigeminal nerve innervation; block vasoactive peptide release
from trigeminal nerve endings; promote vasocontriction of vasculature; block pain pathways in brainstem; First line of defense

Nasal Spray (migranol); IV, IM

Name

Brand Name

Class/Type

Clinical Indications

Amitriptyline

Elavil

TCA

Unipolar depression, Anti-panic & anxiolytic, Chronic

pain, insomnia, Migraine Prophylaxis

Desipramine

Norpramin

TCA

Unipolar depression, Anti-panic & anxiolytic, Chronic pain,

insomnia

Nortriptyline

Pamelor

TCA

Unipolar depression, Anti-panic & anxiolytic, Chronic pain,

insomnia

Clomipramine

Anafranil

TCA

Unipolar depression, Anti-panic & anxiolytic, Chronic pain,

insomnia

Imipramine

Tofranil

TCA

Unipolar depression, Anti-panic & anxiolytic, Chronic pain,

insomnia

Doxepin

Sinequan

TCA

Unipolar depression, Anti-panic & anxiolytic, Chronic pain,

insomnia

Amoxapine

Asendin

TCA

Unipolar depression, Anti-panic & anxiolytic, Chronic pain,

insomnia

Phenelzine

Nardil

MAOI

Depression and anxiety

Tranylcypromine

Parnate

MAOI

Depression and anxiety

Selegiline

Eldeprenyl

MAOI

Depression and anxiety

Fluoxetine

Prozac

SSRIs

Depression and anxiety

Sertaline

Zoloft

SSRIs

Depression and anxiety

Paroxetine

Paxil

SSRIs

Depression and anxiety

Fluvoxamine

Luvox

SSRIs

Depression and anxiety

Citalopram

Celexa

SSRIs

Depression and anxiety

Escitalopram

Lexapro

SSRIs

Depression and anxiety

Buproprion

Welbutrin/Zyban

NDRI (NE and DA

reptake inhibitor)

Venlafaxine

Effexor IR XR

SNRI (SE and NE

reptake inhibitor)

Desvenlafaxine

Pristiq

SNRI
SARI (SE antagonist
and RI)

Nefazodone

Mirtazapine

Remeron

NaSSA (NE and SE

specific antagonist)

Duloxetine

Cymbalta

SNRI

Depression, anxiety, diabetic neuropathy

Atamoxetine

Strattera

NRI

ADHD

Mechanism

Side Effects

Block 5HT and NE reuptake, but are also Dangerous in an OD. Sedation (H1, mACh),
antagonists for H1, Alpha1 and mACh. Also Weight Gain (H1), Hypotension (Alpha1), Blurred
good for chronic headaches
vision & constipation (mACh), Sexual Dysfunction

Drug interactions
Avoid giving with drugs that inhibit
2D6 enzyme

Block 5HT and NE reuptake, but are also

antagonists for H1, Alpha1 and mACh Drug
interaction with SSRI

Dangerous in an OD. Sedation (H1, mACh),

Weight Gain (H1), Hypotension (Alpha1), Blurred
vision & constipation (mACh), Sexual Dysfunction

Avoid giving with drugs that inhibit

2D6 enzyme

Block 5HT and NE reuptake, but are also

antagonists for H1, Alpha1 and mACh

Dangerous in an OD. Sedation (H1, mACh),

Weight Gain (H1), Hypotension (Alpha1), Blurred
vision & constipation (mACh), Sexual Dysfunction

Avoid giving with drugs that inhibit

2D6 enzyme

Block 5HT and NE reuptake, but are also

antagonists for H1, Alpha1 and mACh

Dangerous in an OD. Sedation (H1, mACh),

Weight Gain (H1), Hypotension (Alpha1), Blurred
vision & constipation (mACh), Sexual Dysfunction

Avoid giving with drugs that inhibit

2D6 enzyme

Block 5HT and NE reuptake, but are also

antagonists for H1, Alpha1 and mACh

Dangerous in an OD. Sedation (H1, mACh),

Weight Gain (H1), Hypotension (Alpha1), Blurred
vision & constipation (mACh), Sexual Dysfunction

Avoid giving with drugs that inhibit

2D6 enzyme

Block 5HT and NE reuptake, but are also

antagonists for H1, Alpha1 and mACh

Dangerous in an OD. Sedation (H1, mACh),

Weight Gain (H1), Hypotension (Alpha1), Blurred
vision & constipation (mACh), Sexual Dysfunction

Avoid giving with drugs that inhibit

2D6 enzyme

Block 5HT and NE reuptake, but are also

antagonists for H1, Alpha1 and mACh

Dangerous in an OD. Sedation (H1, mACh),

Weight Gain (H1), Hypotension (Alpha1), Blurred
vision & constipation (mACh), Sexual Dysfunction

Avoid giving with drugs that inhibit

2D6 enzyme

Block MAOI and increase NE, DA, 5HT in

neuron. Excess NT in cleft causes
modulation

Orthostatic hypotension, impotence, hyperreflexia, Dangerous in an OD, Tyramine

hallucinations, hyeperthermia, Poor tolerabilty, interaction, several drug interactions
Toxic in OD
(Demerol, decongestants

Block MAOI and increase NE, DA, 5HT in

neuron. Excess NT in cleft causes
modulation

Orthostatic hypotension, impotence, hyperreflexia, Dangerous in an OD, Tyramine

hallucinations, hyeperthermia, Poor tolerabilty, interaction, several drug interactions
Toxic in OD
(Demerol, decongestants

Block MAOI and increase NE, DA, 5HT in

neuron. Excess NT in cleft causes
modulation

Orthostatic hypotension, impotence, hyperreflexia, Dangerous in an OD, Tyramine

hallucinations, hyeperthermia, Poor tolerabilty, interaction, several drug interactions
Toxic in OD
(Demerol, decongestants

Block 5HT reuptake, modulate neurons.

Prozac - most commonly prescribed for
depression

Less side effects, but: sexual disfunction, GI

problems, nervousness, (5HT RI). Inhibit CYP 2D6
and CYP 3A4 enzymes (problems with drug
metabolisim: desipramine, seldane)

Block 5HT reuptake, modulate neurons.

Used in panic disorders, OCD, PTSD, and
obviously depression

Less side effects, but: sexual disfunction, GI

problems, nervousness, headaches (5HT RI).
Inhibit CYP 2D6 and CYP 3A4 enzymes (problems
with drug metabolisim: desipramine, seldane)

Block 5HT reuptake, modulate neurons.

Paxil - also sedative b/c of M1
antagonism.

Less side effects, but: sexual disfunction, GI

problems, nervousness, (5HT RI). Inhibit CYP 2D6
and CYP 3A4 enzymes (problems with drug
Fluvoaxamine, paroxetine,
metabolisim: desipramine, seldane)
fluoxetine inhibit CYP450 enzymes

Fluvoaxamine, paroxetine,
fluoxetine inhibit CYP450 enzymes

Block 5HT reuptake, modulate neurons

Less side effects, but: sexual disfunction, GI

problems, nervousness, (5HT RI). Inhibit CYP 2D6
and CYP 3A4 enzymes (problems with drug
metabolisim: desipramine, seldane)

Block 5HT reuptake, modulate neurons

Least side effects of SSRI's

Less side effects, but: sexual disfunction, GI

problems, nervousness, (5HT RI). Inhibit CYP 2D6
and CYP 3A4 enzymes (problems with drug
metabolisim: desipramine, seldane)

Block 5HT reuptake, modulate neurons

Less side effects, but: sexual disfunction, GI

problems, nervousness, (5HT RI). Inhibit CYP 2D6
and CYP 3A4 enzymes (problems with drug
metabolisim: desipramine, seldane)

DA RI does most of the work

Can augment anxiety (due to NE), increase risk of

seizure (especially those with bulimia)

Seretonin and NE reuptake inhibitor, Rapid

onset, short half life; Good efficacy in
elderly

HTN in dose response; early side effects;

discontinuation syndrome; more toxic in OD than
SSRIs; nausea, dizziness, sweating, insomnia

Seretonin and NE reuptake inhibitor, Rapid

onset, short half life

Nausea, dizziness, sweating, insomnia;

discontinuation syndrome

5HT antagonist and RI. Good in elderly

(sedative, little weight gain)

Alpha effects (dizziness, HT), Drug interactions

NE and 5HT specific antagonist. Potent H1

antagonist (sedative, induces hunger,
antiemetic), good cancer drug

Weight gain, sedation, dry mouth, Constipation

considered to be a selective reuptake

inhibitor at the 5-HT and NE transporters

DDIs, Dual agent tolerability, nausea, dizziness,

insomnia, sexual dysfunction

no liver metabolism

Metabolism

Notes

Tyramine increases NE release; increase in NE can

lead to hypertension; Avoid a diet in aged cheese,
sausage, beer, red wine, soy sauce
Lethal DDI w/ decongestants, stimulants,
narcotics (Demerol) and anesthetics

Tyramine increases NE release; increase in NE can

lead to hypertension; Avoid a diet in aged cheese,
sausage, beer, red wine, soy sauce
Tyramine increases NE release; increase in NE can
lead to hypertension; Avoid a diet in aged cheese,
sausage, beer, red wine, soy sauce

No sexual dysfunction; mood stabilizer; no

weight gain

expensive medication

liver toxicity

CI: alcohol and BZ withdrawl,

anorexia, Bulimia

Name

Brand Name Clinical Indications

Ibuprofen

Analgesic and Antipyretic, antiinflammatory, antithrombotic

Naproxen

Analgesic and Antipyretic, antiinflammatory, antithrombotic

meclofenamate

Analgesic and Antipyretic, antiinflammatory, antithrombotic

paroxicam

Analgesic and Antipyretic, antiinflammatory, antithrombotic

Sulindac

Analgesic and Antipyretic, antiinflammatory, antithrombotic

indomethacin

Analgesic and Antipyretic, antiinflammatory, antithrombotic

nabumetone

Analgesic and Antipyretic, antiinflammatory, antithrombotic

celecoxib

Celebrex

Analgesic and Antipyretic, antiinflammatory, antithrombotic

refecoxib

Analgesic and Antipyretic, antiinflammatory, antithrombotic

Aspirin

Analgesic and Antipyretic, antiinflammatory, antithrombotic

Acetaminophen

Analgesic and Antipyretic (NOT

and NSAID)

Mechanism

Side Effects

Blocks COX 1 &2: in tissues this decreases PG synth and thus

decreases neural sensitization and inflammation cascade. In
hypothalamus, block of PG reduces fever. In blood blocks TXA.

Gastric upset, bleeding, gastritis,

intolerance, ulceration probably
due to inhibition of COX1

Blocks COX 1 &2: in tissues this decreases PG synth and thus

decreases neural sensitization and inflammation cascade. In
hypothalamus, block of PG reduces fever. In blood blocks TXA.

Gastric upset, bleeding, gastritis,

intolerance, ulceration probably
due to inhibition of COX1

Blocks COX 1 &2: in tissues this decreases PG synth and thus

decreases neural sensitization and inflammation cascade. In
hypothalamus, block of PG reduces fever. In blood blocks TXA.

Gastric upset, bleeding, gastritis,

intolerance, ulceration probably
due to inhibition of COX1

Blocks COX 1 > COX2: in tissues this decreases PG synth and thus
decreases neural sensitization and inflammation cascade. In
hypothalamus, block of PG reduces fever. In blood blocks TXA.

Gastric upset, bleeding, gastritis,

intolerance, ulceration probably
due to inhibition of COX1

Blocks COX 1 > COX2: in tissues this decreases PG synth and thus
decreases neural sensitization and inflammation cascade. In
hypothalamus, block of PG reduces fever. In blood blocks TXA.

Gastric upset, bleeding, gastritis,

intolerance, ulceration probably
due to inhibition of COX1

Blocks COX 1 >COX 2: in tissues this decreases PG synth and thus

decreases neural sensitization and inflammation cascade. In
hypothalamus, block of PG reduces fever. In blood blocks TXA.

Gastric upset, bleeding, gastritis,

intolerance, ulceration probably
due to inhibition of COX1

Blocks COX 1 < COX 2: in tissues this decreases PG synth and thus
decreases neural sensitization and inflammation cascade. In
hypothalamus, block of PG reduces fever. In blood blocks TXA.

Gastric upset, bleeding, gastritis,

intolerance, ulceration probably
due to inhibition of COX1

Blocks COX 1 <<COX 2: in tissues this decreases PG synth and thus

decreases neural sensitization and inflammation cascade. In
hypothalamus, block of PG reduces fever. In blood blocks TXA.

Gastric upset, bleeding, gastritis,

intolerance, ulceration probably
due to inhibition of COX1

Blocks COX 1 << COX2: in tissues this decreases PG synth and thus
decreases neural sensitization and inflammation cascade. In
hypothalamus, block of PG reduces fever. In blood blocks TXA.

Gastric upset, bleeding, gastritis,

intolerance, ulceration probably
due to inhibition of COX1

Blocks COX 1 &2: in tissues this decreases PG synth and thus

decreases neural sensitization and inflammation cascade. In
hypothalamus, block of PG reduces fever. In blood blocks TXA.

COX effects also cause blood

thinning, gastritis, ulcers, bleeding.
Reyes syndrome in children.
Alkalosis and then acidosis.

Analgesic properties thought to be due to COX 3 inhibition

Less side effects than NSAIDS.

Overdose depletes liver of GSH
and can kill if untreated for 10
hours

Drug interactions

Metabolism Notes

Positive effect in
treatment of
Paroxysmal
Hemicrania

Pregnancy
Class B

Name

Brand Name

Class

Clinical Indications

First line of treatments

Alprazolam

Xanax

BZ

anxiolytic, anticonvulsant, sedative,

muscle relaxant, alcohol withdrawl

Lorazepam

Ativan

BZ

anxiolytic, anticonvulsant, sedative,

muscle relaxant, alcohol withdrawl

Chloridazepoxide

Librium

BZ

anxiolytic, anticonvulsant, sedative,

muscle relaxant, alcohol withdrawl

Diazepam

Valium

BZ

anxiolytic, anticonvulsant, sedative,

muscle relaxant, alcohol withdrawl

Oxazepam

Serax

BZ

anxiolytic, anticonvulsant, sedative,

muscle relaxant, alcohol withdrawl

Clonazepam

Klonopin

BZ

anxiolytic, anticonvulsant, sedative,

muscle relaxant, alcohol withdrawl

Buspirone

Buspar

Antinxiolytic, good in alcoholics, GAD

Propranol

Best for social phobias and PTSD

Clonidine

Best for social phobias and PTSD

Prazosin

Best for social phobias and PTSD

Tiagabine
Neurleptics

Antipychotic (ex. Olazapine (Zyprexa))

Mechanism

Side Effects

First line of treatments for anxiety is SSRIs

allosteric modulator of GABAa receptor,
increases Cl conductance
allosteric modulator of GABAa receptor,
increases Cl conductance
allosteric modulator of GABAa receptor,
increases Cl conductance
allosteric modulator of GABAa receptor,
increases Cl conductance
allosteric modulator of GABAa receptor,
increases Cl conductance
allosteric modulator of GABAa receptor,
increases Cl conductance

Antianxiolytic: 5HT 1A partial agonist (5HT 1A

is an autoreceptor on presynapse). "Puts
breaks on 5HT projections" Modulates
hippocampal projections to reduce panic
Beta Blocker
Alpha Agonist, decreases sympathetic activity
Alpha Antagonist; decreases sympathetic
activity
Modulation of Na and Ca channels

Tolerance, dependance, withdrawal.

Behavioral disinhibition, psychomotor
probs., Concentration
Tolerance, dependance, withdrawal.
Behavioral disinhibition, psychomotor
probs., Concentration
Tolerance, dependance, withdrawal.
Behavioral disinhibition, psychomotor
probs., Concentration
Tolerance, dependance, withdrawal.
Behavioral disinhibition, psychomotor
probs., Concentration
Tolerance, dependance, withdrawal.
Behavioral disinhibition, psychomotor
probs., Concentration
Tolerance, dependance, withdrawal.
Behavioral disinhibition, psychomotor
probs., Concentration

Drug interactions

Metabolism Notes

Good for PTSD, social Phobia

Name

Brand Na Clinical In Mechanis Side EffecDrug interMetabolis Notes

Nolte 2009 Figure 8-26

Receptor

Coupling Protein

Effector

2nd messenger

M1, M3, alpha1

Gq

increases
PLC

IP3 and DAG

Gs

increases
adenyl
cyclase

Gi

decrease Ca
influx, increase
decreases
enzyme
adenyl
decreases camp
activity,
cyclase
increase K
efflux

beta, D1

alpha 2, M2

camp

Result
increase in Ca,
increase
protein kinase
activity
increase Ca
influx, increase
enzyme activity

Notes

Name

Brand Name

Class

Clinical Indications

Lithium

Mood Stabilizer

Indicated for acute mania and bipolar

disorder; most effectivein pure mania and nonrapid cycling bipolar; Shown to reduce suicide
risk

Chlorpromazine

First Generation
Antipsychotic
(typical
antipsychotic)

schizophrenia, acute mania, agitation

Perphenazine

First Generation
Antipsychotic
(typical
antipsychotic)

schizophrenia, acute mania, agitation

Fluphenazine

First Generation
Antipsychotic
(typical
antipsychotic)

schizophrenia, acute mania, agitation

Thiothixene

First Generation
Antipsychotic
(typical
antipsychotic)

schizophrenia, acute mania, agitation

Haloperidol

First Generation
Antipsychotic
(typical
antipsychotic)

schizophrenia, acute mania, agitation

Clozapine

Second generation
Schizophrenia, acute mania, agitation associated
Antipsychotic
with demetia, anxiety disorder, and obsessive
(atypical
compulsive disorder
antipsychotic)

Olanzapine

Second generation Schizophrenia, acute mania, agitation associated

Antipsychotic
with demetia, anxiety disorder, and obsessive
(atypical
compulsive disorder; Very effective in treating
antipsychotic)
bipolar disorder

Quetiapine

Second generation
Schizophrenia, acute mania, agitation associated
Antipsychotic
with demetia, anxiety disorder, and obsessive
(atypical
compulsive disorder
antipsychotic)

Asenapine

Second generation
Schizophrenia, acute mania, agitation associated
Antipsychotic
with demetia, anxiety disorder, and obsessive
(atypical
compulsive disorder
antipsychotic)

Risperidone

Second generation
Schizophrenia, acute mania, agitation associated
Antipsychotic
with demetia, anxiety disorder, and obsessive
(atypical
compulsive disorder
antipsychotic)

Ziprasidone

Second generation
Schizophrenia, acute mania, agitation associated
Antipsychotic
with demetia, anxiety disorder, and obsessive
(atypical
compulsive disorder
antipsychotic)

Paliperidone

Second generation
Schizophrenia, acute mania, agitation associated
Antipsychotic
with demetia, anxiety disorder, and obsessive
(atypical
compulsive disorder
antipsychotic)

Iloperidone

Second generation
Schizophrenia, acute mania, agitation associated
Antipsychotic
with demetia, anxiety disorder, and obsessive
(atypical
compulsive disorder
antipsychotic)

Lurasidone

Second generation
Schizophrenia, acute mania, agitation associated
Antipsychotic
with demetia, anxiety disorder, and obsessive
(atypical
compulsive disorder
antipsychotic)

Aripiprazole

Second generation
Schizophrenia, acute mania, agitation associated
Antipsychotic
with demetia, anxiety disorder, and obsessive
(atypical
compulsive disorder
antipsychotic)

Carbamazepine
Lamotrigine
Topiramate
Valproic Acid

Traditional Antipscychotics Notes:

Low Potency
High Potency

fewer Extra Pyramidal Symptoms but more H1, alpha1, and muscarinic bloc
more extrapyramidal side effects and fewer H1, alpha1, and anticholiner

Extrapyramidal side effects include:

Dystonia
muscular spasmsof neck (torticollis), tongue, jaw
Akathisia
a feeling of motor restlessness
Pseudoparkinsonism
bradykinesia, akinesia, resting tremor
involuntary asymmetrical movements of the muscles/ longterm chron
Tardive Dyskinesia
with long term antipsychotic use

Mechanism

Side Effects

Precise mechanism unknown; known to decrease cellular

response to neurotransmitters including serotonin

Hypothyroidism (reversible afer discontinuation); long term

use can cause irreversible decrease in GFR; can cause
nephrogenic diabetes insipidus; can cause arrythmias and
death; can cause T wave changes at normal levels;
parkinson sypmtoms (tremors); Nausea, diarrhea; weight
gain; acne; cognitive dulling; leukocytosis

First Generation Antipsychotics

D2 receptor antagonist that effects these dopaminergic
pathways: Mesocortical, Mesolimbic, Nigrostriatal,
Tuberoinfundibular

Psuedoparkinsonism, Dystonias, Akathisia, NMS

D2 receptor antagonist that effects these dopaminergic

pathways: Mesocortical, Mesolimbic, Nigrostriatal,
Tuberoinfundibular

Psuedoparkinsonism, Dystonias, Akathisia, NMS

D2 receptor antagonist that effects these dopaminergic

pathways: Mesocortical, Mesolimbic, Nigrostriatal,
Tuberoinfundibular

Psuedoparkinsonism, Dystonias, Akathisia, NMS

D2 receptor antagonist that effects these dopaminergic

pathways: Mesocortical, Mesolimbic, Nigrostriatal,
Tuberoinfundibular

Psuedoparkinsonism, Dystonias, Akathisia, NMS

D2 receptor antagonist that effects these dopaminergic

pathways: Mesocortical, Mesolimbic, Nigrostriatal,
Tuberoinfundibular

Psuedoparkinsonism, Dystonias, Akathisia, NMS

Second Generation Antipsychotics

mild D2 receptor antagonist and a 5-HT-2a receptor
antagonist in these doparminergic pathways:Mesocortical,
Mesolimbic, Nigrostriatal, Tuberoinfundibular

agrunlocytosis, weight gain, metabolic syndrome

mild D2 receptor antagonist and a 5-HT-2a receptor

antagonist in these doparminergic pathways:Mesocortical,
Mesolimbic, Nigrostriatal, Tuberoinfundibular

weight gain, metabolic syndrome, diabetes, dyslipidemias,

lethargy; very sedating

mild D2 receptor antagonist (lowest affinity out of all) and

a 5-HT-2a receptor antagonist in these doparminergic
pathways:Mesocortical, Mesolimbic, Nigrostriatal,
Tuberoinfundibular

weight gain, metabolic syndrome, diabetes, dyslipidemias,

lethargy, very sedating

mild D2 receptor antagonist and a 5-HT-2a receptor

antagonist in these doparminergic pathways:Mesocortical,
Mesolimbic, Nigrostriatal, Tuberoinfundibular

weight gain, metabolic syndrome, diabetes, dyslipidemias,

lethargy

mild D2 receptor antagonist and a 5-HT-2a receptor

antagonist in these doparminergic pathways:Mesocortical,
Mesolimbic, Nigrostriatal, Tuberoinfundibular

less likely to cause weight gain, metabolic syndrome,

diabetes, dyslipidemias, lethargy; More incidence of EPS
and mor potential for TD than other agents

mild D2 receptor antagonist and a 5-HT-2a receptor

antagonist in these doparminergic pathways:Mesocortical,
Mesolimbic, Nigrostriatal, Tuberoinfundibular

less likely to cause weight gain, metabolic syndrome,

diabetes, dyslipidemias, lethargy; More incidence of EPS
and mor potential for TD than other agents

mild D2 receptor antagonist and a 5-HT-2a receptor

antagonist in these doparminergic pathways:Mesocortical,
Mesolimbic, Nigrostriatal, Tuberoinfundibular

weight gain, metabolic syndrome, diabetes, dyslipidemias,

lethargy

mild D2 receptor antagonist and a 5-HT-2a receptor

antagonist in these doparminergic pathways:Mesocortical,
Mesolimbic, Nigrostriatal, Tuberoinfundibular

weight gain, metabolic syndrome, diabetes, dyslipidemias,

lethargy

mild D2 receptor antagonist and a 5-HT-2a receptor

antagonist in these doparminergic pathways:Mesocortical,
Mesolimbic, Nigrostriatal, Tuberoinfundibular

weight gain, metabolic syndrome, diabetes, dyslipidemias,

lethargy

mild D2 receptor antagonist and a 5-HT-2a receptor

antagonist in these doparminergic pathways:Mesocortical,
Mesolimbic, Nigrostriatal, Tuberoinfundibular

weight gain, metabolic syndrome, diabetes, dyslipidemias,

lethargy; Requires higher doses to be effective in
sicker patients

Anticonvulsants

See antiepileptics tab

1, alpha1, and muscarinic blocking effects

H1, alpha1, and anticholinergic effects

neck (torticollis), tongue, jaw,

of motor restlessness
akinesia, resting tremor
the muscles/ longterm chronic condition associated
erm antipsychotic use

Drug interactions

Diuretics and NSAIDS can

cause increase in lithium
levels to toxic range

Metabolism

Notes

Almost exclusively renal; no

hepatic metabolism

Contraindicated: Pregnancyebstein anomaly (tricuspid valve

atresia); breastfeeding; renal
disease; acute MI, Myasthenia
gravis; less risk in (diabetes,
ulcerative colitis, psoriasis)

Low potency

Medium Potency

High potency

Medium Potency

High potency

Lower risk for EPS, NMS, TD

Name

Brand Name Class/Type

Clinical Indications

Methylphenidate

Concerta

Stimulant

ADHD

Amphetamine

Adderall

Stimulant

ADHD

Clonidine

Catapres

Alpha2 agonist

ADHD; PTSD

Guanfacine

Tenex

Alpha2 agonist

ADHD; PTSD

Imipramine

Tofranil

TCA

Unipolar depression, Anti-panic &

anxiolytic, Chronic pain, insomnia

Burproprion

Welbutrin/Zyban

NDRI (NE and DA

reptake inhibitor)

ADHD

NRI

ADHD

Atomoxetine

Mechanism

Side Effects

blocks dopamine uptake by blocking dopamine

decreased appetite; decreased sleep; tics; stunted
transport; alteration of serotonergic pathways via
growth
changes in dopamine transport may result
stimulates the release of NE; at higher doses
stimulates release of DA from mesocorticolimbic
decreased appetite; decreased sleep; tics; stunted
system and nigrostriatal DA systems; acts as
growth
direct agonist on 5-HT receptors and may inhibit
MAO

treats high blood pressure by stimulating 2 receptors in

the brain, which decreases cardiac output and peripheral
vascular resistance, lowering blood pressure. It has
specificity towards the presynaptic 2 receptors in
the vasomotor center in the brainstem. This binding
decreases presynaptic calcium levels, and inhibits the
release of norepinephrine (NE). The net effect is a
decrease in sympathetic tone

dizziness, dry mouth; dizziness; constipation;

hypotension

selectively stimulates central alpha(2)-adrenergic

receptors, resulting in inhibition of sympathetic
vasomotor centers, which contributes predominantly to
the hypotensive effects of the drug

dizziness, dry mouth; dizziness; constipation;

hypotension

Dangerous in an OD. Sedation (H1, mACh), Weight Gain

Block 5HT and NE reuptake, but are also antagonists for
(H1), Hypotension (Alpha1), Blurred vision & constipation
H1, Alpha1 and mACh
(mACh), Sexual Dysfunction

DA RI does most of the work

Selective inhibition of norepinephrine transporter

Can augment anxiety (due to NE), increase risk of

seizure (especially those with bulimia)
alopecia (hair loss); dry mouth; tiredness,
irritability; nausea, decreased appetite,
constipation, dizziness, sweating, dysuria, sexual
dysfunction, tachycardia, hypertension;
palpitations

Drug interactions

Metabolism

Notes

MAOIs, SSRIs, NRIs, SNRIs,

Pregnancy class C

MAOIs, SSRIs, NRIs, SNRIs,

CI in pregnancy

CYP3A5 inducers and inhibitors; valproic acid; CNS

depressant

hepatic

hepatic

Avoid giving with drugs that inhibit 2D6 enzyme

No sexual dysfunction;
mood stabilizer; no weight
gain
less abuse potential than
stimulants