Pharm - Psych - Depression, Anxiety, Mania

Front 1

General tx for depression

Back 1

Regular rigorous exercise
Omega-3 fatty acids
Methylphenidate (Ritalin)
Sleep deprivation
Medically-induced generalized seizures
Challenging negative self-statements
St. john’s wort
Falling in love

Front 2

Antidepressants relation to stress

Back 2

Brings down stress (cortisol)

Front 3

2 effects, based on time, of antidepressants

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Immediate - Augmentation of biogenic amines at receptors (side effects mostly)

Downstream latent effects - Second messengers for molecular expression and receptor down regulation. 1-6 weeks

* - Aside from brain, gut has the most biogenic amine receptors. So many SEs ocurr there.

Front 4

Biogenic amines (4)

Back 4

NE, serontonin, DA, epinephrine

Front 5

Mechanism of downstream latent effects

Back 5

Consistently blocking a post-synaptic receptor or blocking reuptake will increase the number of post-synaptic receptors.

Front 6

MAO inhibitors (2)

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Phenelzine (Nardil)
Tranylcypromine (Parnate)

Reasoning: In depression, certain parts of the brain have increased MAO activity.

Very effective but lots of interactions (HTN crisis)

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Tricyclics (tertiary) (5)

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Imipramine (Tofranil)
Amitriptyline (Elavil)
Clomipramine (Anafranil)
Desipramine
Nortriptyline (Pamelor)

OFten used for chronic pain and migrains. Highly toxic and easy to OD (cardiac issues)

Front 8

SSRIs (5)

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Fluoxetine (Prozac)
Sertaline (Zoloft) - Slight DA effect
Citalopram (Celexa)
Escitalopram (Lexapro)
Paroxetine (Paxil) - slight NE effect

Lexapro is a monoisomer of Celexa, but not really that much better (expected to have more ther effect and less SE)

***when orig learning about isomers, you were CITting in orgo.

Front 9

SNRIs (2)

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venlafaxine (Effexor)
duloxetine (Cymbalta)

Inhib serotonin and NE

Front 10

Herbals

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St. John's Wort

Front 11

"Other" antidepressants - Antagonizes serotonin receptors
(3)

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Nefazodone (Serzone)
Trazadone (Desyrel)
Mirtazapine (Remeron)

Front 13

Alpha 2 receptor

Back 13

Good target site for people with too much NE tone in their brains.

Agonists will stop NE release. Must worry about hypotension

Front 14

Dopaminergic drug indications

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Reward/addition.

Having a pt restore pleasure in pleasurable things (e.g. food)

Weight change - but body can bounce back over time.

Front 15

General SCZ tx

Back 15

Block D2 receptor ("too much DA in these pts")

Front 16

General DA tx in depression

Back 16

Block reuptake or digestion of DA via MAO

Wanna increase levels

Front 17

General DA tx in ADHD

Back 17

Mimic DA and also block the transporter that sucks it back in.

Can induce psychosis (bc too much DA).

Front 18

MAOI ther. effects

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Efficacy in refractory panic, mixed anxiety/depression, depression with atypical features, genrealized social phobias.

Front 19

MAOI side effects

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Hypertensive crisis with tyramine containing foods, cold preps, diet pills and Demerol (meperidine - often given in ER).

Hypotension

Weight gain.

Front 20

TCA mechanism
(tricyclic antidepressant)

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Block reuptake of NE, 5HT. Also multiple post-syn effects on NE, 5HT, ACH, histamine

Front 21

TCA ther effects

Back 21

Severe depression, anxiety, panic, helps to maintain sleep, efficacy in pain syndromes, bed wetting (enuresis), ADHD

Front 22

TCA side effects

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ACH and histamine blockade (dry mouth, orthostasis, constipation, sedation, weight gain).

Risk of cardiac conduction delay, suddent cardiac death in overdose.

Front 23

SSRI mechanism

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Potent and specific blockade of 5HT reuptake, complexity of over 14 serotonin receptor subtypes.

These are less messy than tricyclics--effect less NTs!

Front 24

SSRI ther. effects

Back 24

Efficacy in mild/mod depression, dysthymia (low mood but not quite major depressive disorder), GAD (general anxiety disorder), panic, PTSD, OCD, social phobia, school avoidance, trichotillomania (impulsive hair pulling), body dysmorphic disorder, PMMD (paramenopausal mood disorder), bulimia, recurrent abdominal pain (bowel-brain connection!), IBS, autistic rigidity, Tourette's

Front 25

SSRI side effects

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Favorable safety profile, nausea, somnolence/activation, agitation, mood swings, sexual SEs, weight gain/loss, suicidal thoughts.

Front 26

Steroisomerism definition

Back 26

2 molecules with same atoms but diff spatial arrangement.

Front 27

Chirality definition

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Type of stereoisomerism

Molecule whose mirror image in not superimposable on the original.

Front 28

Celexa, Lexapro and stereoisomerism

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Lexapro is the R isomer of Celexa

Front 29

Buproprion (Wellbutrin)

Back 29

Part of the "other" antidepressants

DA and NE augmentation, for depression WITHOUT anxiety, ADHD, nicotine, and other drug cravings.

SEs activation, restless, weight neutral, ok for sex, bad rare rash

Front 30

Nefazodone and trazodone

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Antidepressants.

5HT-2 antagonism, for sleep enhancement to augment other treatments.

SE: sedation, weight neutral, ok for sex.

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Venlafaxine and duloxetine

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True SNRIs, both 5HT and NE reuptake blockade; anxiety and depression, refractive cases.

SEs: like SSRIs, beware of withdrawal

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Mirtazapine

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(Remeron)

5HT2, NE alpha 2 presynaptic, histamine post synaptic effects. Mostly sleep enhancement

Front 33

Old sedatives

Back 33

Ethanol, Chloral hydrate, barbituates

Front 34

Benzodiazepine drugs (6)

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Diazepam (Valium)
Chlordiazepoxide (Librium)
Lorazepam (Ativan)
Alprazolam (Xanax)
Clonazepam (Klonipin)
Temazepam (Restoril) - marketed as a hypnotic

Front 35

Benzo general characteristics

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First was Librium.
Anticonvulsant, muscle relaxant, hypnotic, anxiolytic.

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New benzodiazepine receptor agonist hypnotics (3)

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Not benzos technically.



Zolpidem (Ambien)
Zalaplon (Sonata)
Eszopiclone (Lunesta)

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Busipirone (Buspar) mech of action

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5HT-1 autoreceptor partial agonist.
No action on GABA or benzo receptors.
Partial agonist postsynaptic (cortex, hippocampus)
Full agonist pre-synaptic (raphe)

Front 38

Worred about addiction with...

Back 38

Older sedatives, benzos, benzo receptor agonists.

Front 39

Benzo mechanism

Back 39

Binding/enhancing GABA receptor.
There is also a unique benzodiazepine receptor

Binds to gamma subunit of GABAa to increase alpha affininity to GABA. Increases FREQUENCY (not duration) of Cl- channel opening

Front 40

Benzo ther. actions

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CNS depression with incremental effects, anxiolysis, hypnotic, muscle relaxant, anti-convulsant.
Wide range in terms of duration of action based on half-life of parent compound and metabolites and lipid solubility.

Front 41

Benzo SEs

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Wider safety threshold than older sedative hypnotics. Relative safety in OD. Risk of impairment in high doses, risk for physical dependence with chronic use.

Front 42

How brain quickly modulates excitatory/inhib behavior

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GABA and glutamate are metabolites of the same product. So they balance each other very quickly and effectively.

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Busipirone (Buspar) clinical effects

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Indic for GAD. No sedation, muscle relaxation or anticonvulsant effects.

Delayed onset of action, more subtle clinical effects.

Not a CNS depressant and does not carry risk of dependency!!!!!!!

Front 44

Mood stabilizers (5)

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Lithium

Now the AEDs...
Valproate (Divalproex)
Tegretol (Carbamazepine)
Lamictal (Lamotrigine)
Trileptal (Oxcarbazepine)

Front 45

Lithium mechanism

Back 45

Acutely enhances serotonin (5HT), multiple interactions with second messenger proteins, and actions at cell membrane.

Front 46

Lithium ther effects

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T and prophylaxis of mania and depression, anti-suicide, augments antidepressants.

Anti suicide is especially important here.

(note - it effects ion channels for serotonin)

Front 47

Lithium SEs

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Narrow ther range, possible CNS/thyroid/renal/liver toxicity.

Front 48

AED mechanism

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Augments GABA or antag glutamate. Act as membrane stabilizers. Or have effects on ion channels

Front 49

AED ther effects (Psychiatric)

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Acute tx of mania, advantage for mixed states and rapidly cycling, synergistic with lithium.

LAMOTRIGINE ESPECIALLY GOOD FOR BIPOLAR DEPRESSION!!!

(they decrease sz potential too...)

Front 50

AED SEs

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Blood dyscrasia (white count elev or depressed)

Hepto-cellular damage, rash, drug interactions, risks during pregnancy.