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75 Cards in this Set

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What are characteristics of Major Endogenous Depression
Recurrent, Cyclic, Seasonal.
Degree of depression is not adequate for precipitating event.
Automaton (unresponsive).
Mania Core Symptoms
It is characterized by an elevated “high” mood.
Talkative, go on-and-on about the things they will do.
Increased self-esteem.
Auditory hallucinations.
Decrease need to sleep.
Lack judgement, indiscrete.
Biological Correlates of Depression
1. Hypersecretion of cortisol.
2. Escape from dexamethasone suppression.
3. Blunted TSH response to TRH.
4. Blunted GH response to hypoglycemia.
5. Altered 24hr rhythm of prolactin secretion.
6. Decreased 5-HT metabolites in plasma.
7. Decreased REM latency.
Biological Basis for Depression
. Has a genetic component.
2. Depression can be drug-induced.
3. Depression can be drug-repressed.
4. Depression can be treated with drugs.
5. Depression can be treated with
Electroconvulsive Therapy (ECT).
Biogenic Theory of Depression
The precise cause of affective disorders remains elusive.
Evidence implicates alterations in the firing patterns of a subset of biogenic amines in the CNS, Norepinephrine (NE) and Serotonin (5-HT).

 Activity of NE and 5 -HT systems?.
How does the NE System effect depression
Mood: -- higher functions performed by the cortex.
Cognitive function: -- function of cortex.
Drive and motivation: -- function of brainstem
Memory and emotion: -- function of the hippocampus and amygdala.
Endocrine response: -- function of hypothalamus.

alph and Beta-adrenergic receptors.
Serotonin System is involved in what?
Sexual behavior.
Rhythms (Suprachiasmatic nucleus).
Temperature regulation.
CSF production.
Name the 4 Types of Antipressants.
1. Tricyclic anti-depressants (TCAs).
Imipramine, desipramine, nortriptyline,
protryptyline, amytriptiline, doxepin.
2. Monoamine oxidase inhibitors (MAOIs).
Isocarboxacid, phenelzine, tranylcypromine.
3. Selective serotonin reuptake inhibitors (SSRIs)
Fluoxetine, sertraline, paroxetine, trazodone.
4. Atypical anti-depressants (Others)
New TCAs, amoxapine, bupropion,
alprazolam, maprotiline, nomifensine, mianserin
Name the 5 Mechanism of Antipressants.
Inhibition of NE and 5-HT reuptake.
(TCAs, SSRIs, Newer TCAs).
2. Inhibition of MAO enzymes.
3. 5-HT2A and 5-HT2C antagonists.
(Nefazodone, trazodone, mirtazapine)
4. Alteration of NE output .
5. Alpha 2–AR antagonists.
Name some Tricyclic Antidepressants (TCAs)
Characteristics of TCA
Characteristic three ring nucleus.
Most are incompletely absorbed, all are metabolized in liver => High first pass effect:
1) Transformation of the tricyclic nucleus => hydroxylation => conjugation => glucoronides.
2) Alteration of aliphatic side chain => demethylation of the nitrogen => active metabolites.
High protein binding, high lipid solubility.
Amine structure os TCA
/ CH3 / H
\ CH3 \ CH3

tertiary amine secondary amine
3o => 2o
Tertiary amine TCA
3°Amines: Imipramine, Amitriptyline
Secondary Amine TCA
2°Amines: Desipramine, Nortriptyline
TCA Selectivity
Selectivity 2o Amines -- NE > 5-HT
3o Amines -- 5-HT > NE
Mechanism of action of TCA
Mechanism of Action:
- Inhibition of NT reuptake.
- Immediate action = > NE and 5-HT in synapse.
- After chronic treatment (2 - 4 weeks) = >
  NE-R and 5-HT2R.
 NE release and turnover.
 NE-stimulated cAMP in brain.
 Sensitization of 5-HT receptors.
* Adaptive Responses *
- Takes up to 4 weeks for all TCA antidepressants to have an effect.
TCA Side effects
Atropine-like side effects: dry mouth, paradoxical excessive perspiration, constipation, blurred vision, mydriasis, metallic taste, urine retention => muscarinic blockade.
Orthostatic hypotension => 1-AR and possibly 2-AR blockade.
Drowsiness, sedation and weight gain => Histamine-Receptor blockade.
TCA Side effect cont..
Most serious side effect is cardiac toxicity => Palpitations, tachycardia, dizziness => excessive CNS stimulation => NE in Heart.

Sexual dysfunction, including loss of libido, impaired erection and ejaculation and anorgasmia
List 4 MAOI
What is the Therapeutic use of MAOI?
Developed for the treatment of tuberculosis (iproniazid derivatives) - 1951.
These drugs are not widely used today, although a small number of patients appear to do better in MAOIs than TCAs or the newer drugs.
Are readily absorbed from GI tract and widely distributed throughout the body.
May have active metabolites, inactivated by acetylation.
Effects persist even after these drugs are no longer detectable in plasma (1-3 weeks).
What is the Mechanism of Action of MAOIs?
Mechanism of action:
Inhibit MAO enzymes (non-selective):
1) Irreversible MAO inhibitors
Phenelzine and isocarboxazid => hydrazides.
2) Reversible MAO Inhibitors.
Tranylcypromine => non-hydrazide,
prolonged blockade, but reversible within 4hr.

Decrease metabolism of most biogenic amines (NE, 5HT, DA, tyramine, octopamine).
MAO Inhibitors- Acute Administration causes what?
high NE and 5-HT in synaptic terminals in brain but low NE in PNS. low NE synthesis.
Acute euphoria
Suppressed REM sleep.
MAO Inhibitors- Chronic Administration causes what?
low NE-stimulated cAMP in brain.
Down regulation of Beta receptors.
Down regulation of 5-HT2 receptors.
What do MAO-A aned MAO-B inhibit?
MAO-A -->NE, 5-HT, Tyramine
Name some Selective MAOI's?
Inhibitors MAO-A
Moclobemide, Clorgyline
Inhibitors of MAO-B.
Selegiline (most useful for treating Parkinson’s)
What some dietary restrictions on MAOI and why?
Vegetables: Avocados, fermented bean curd, soy bean, soy bean paste.
Fruits: Figs, bananas.
Meats: fermented (bologna, peperoni, salami) or smoked, liver.
Fish: Dried or cured fish; fish that is fermented, aged, or smoked; spoiled fish.
Milk, milk products: All cheeses.
Foods with yeast: chianti wine, some imported beer; yeast extracts (Marmite, Bovril).
Others: protein dietary supplements, soups (with protein extract); shrimp paste; soy sauce.
What some reactions with Wine and Cheese
Fatal interaction with tyramine-containing foods (fermented foods in particular, such as wine and cheese).
- low MAO-A => high Tyramine in the body =>increase NE in circulation => induces hypertensive crisis => can lead to intracranial bleeding and other organ damage.
Increase in NE will lead to what type on reaction on the arteries?
Vasoconstriction and stimulation of the heart.
What are negative drug interaction with MAOI?
Any drug metabolized by MAOs including SSRIs, TCAs and meperidine, alcohol, CNS depressants, sympathomimetics, phenylephrine (O/C nasal decongestants), ampetamines, and other indirect-acting adrenergic drugs.
What are the effect of negative drug interaction action with MAOI?
Interaction with drugs metabolized by MAOs (e.g. Meperidine (opioid analgesics) => hyperpyrexia or “hyperexcitation syndrome” involving high fever, delirium and hypertension).
Side effects of MAOI?
Other side effects:
Hypotension (NE)
Hot flashes

Name some SSRI
What are SSRI's mostly used for?
Most widely prescribed drugs for depression.
SSRI's side effects?
They have few side effects and seem to be rather safe. More rational prescribing and better patient compliance.
SSRI's Adverse Effects?
Adverse effects include: nausea, decreased libido, decrease sexual function.
What is the mechanism of action os SSRIs?
Specific serotonin uptake inhibitors increase 5-HT by inhibiting reuptake.
Enhance serotonergic receptor responses.
What is the protoype drug for SSRI?
Approximately 70% of depressed patients will respond to an SSRI therapy at the end of 6 weeks (4 to 6 weeks before effects are evident to patient).
T1/2 of 16 – 24 hrs except for fluoxetine’s metabolite, norfluoxetine (T1/2 = 8 days).
Fluoxetine and paroxetine inhibit liver enzymes, particularly P450-2D6.
Paroxetine and Sertraline have PK parameters similar to TCAs.
What is some effects of Drug interaction with SSRIs?
Drug-drug interactions:
SSRIs are dangerous with other anti-depressant drugs, MAOIs in particular because of accumulation of high levels of 5-HT.

”Serotonin Syndrome”:
hyperthermia, muscle rigidity, myoclonus, rapid changes in mental status and vital signs.
Thus it is important to wait up to 6 weeks after medication is stopped, before starting with another drug.
Name some second generation heterocyclic drugs?
Name some Third Generation Heterocyclic drugs?
What two heterocyclic drugs have the shortest plasam half lives?
Trazodone and Venlafaxine have the shortest plasma half-lives, which mandates divided doses during the day.
What two heterocyclic drugs cause inhibition of CYP3A4?
Nefazodone and fluvoxamine cause inhibition of CY3A4
Nefazodone and fluvoxamine inhibit which enzyme?
Explain the mechanism of action of Heterocyclics
1) NT reuptake inhibition.
2) 5-HT receptor antagonism (for 5-HT2A and 5-HT2C receptors).
nefazodone, mirtazapine, and trazodone
3) Alteration of NE Output.
bupropion, amoxapine, and trazodone.
What is the mechanism of action of Amoxapine?
Enhances NE output. Metabolite of Loxapine (an anti-psychotic) -- retains some antipsychotic activity and DA receptor antagonism => parkinson's-like symptoms. May be useful if psychosis is present.
What is the mechanism of action of Maprotiline?
Blocks NE reuptake. A tetracyclic drug, resembles desipramine with less sedative and antimuscarinic side effects. Evokes seizures at high doses. Blocks NT reuptake.
What is the mechanism of action of Trazodone?
Antagonist of 5-HT2A or 5-HT2C receptors. Unpredictable efficacy. Highly sedative (hypnotic), but minimal antimuscarinic action.
What is the mechanism of action of Buspropion?
Resembles amphetamine. Increases NE output. Blocks DA reuptake (not important in depression). Causes CNS stimulation. Inhibits appetite. Aggravates psychosis.

Second Generation Heterocyclic
What is the mechanism of action of Mirtazapine?
A derivative of mianserin. Antagonist of 5-HT2A or 5-HT2C receptors. Also antagonizes 2-adrenergic receptors. Increases NE and 5-HT release. Very sedating (antihistaminic).
What is the mechanism of action of Venlafaxine?
Short plasma half-live, thus needs to be given in divided doses. Potent inhibitor of 5-HT uptake and weaker at NE uptake (at low concentrations it acts like an SSRI).
What is the mechanism of action of Nefazodone?
Antagonist of 5-HT2A or 5-HT2C receptors. Moderately sedating. Potent inhibitor of CYP3A4, so it cannot be given with cisapride terfenadine or astemizole (“torsade de pointes”).
What drug would you use to treat Bulimia?
Fluoxetine (SSRI)
What drug would you use to treat Insomnia/Agitation?
Nefazodone (enhances-sleep), mirtazapine (sedative)
What drug would you use to treat Anorexia?
Mirtazapine (enhances apetite)
What drug would you use to treat Sexual active, overweight, sedation?
What drug would you use to treat Obsessive-Compulsive disorder?
Fluvoxamine (SSRIs)
What drug would you use to treat Generalized Anxiety Disorder?
List some alternative ways to treat depression.
Light Therapy
Psychological Treatment
St. John’s Wort*
What is the drug of choice for treating Mania?
List some anti-Manic Drugs.
1) Antipsychotics (carbamazepine, similar in structure to TCAs but not effective in depression).
2) Valproic acid
3) Calcium-channel blockers (nifendipine, diltiazem, verapamil).
4) Lithium
List some characteristics of Li+
Small monovalent cation (between H+ and Na+).
Distributed in total body water, similar to sodium.
May partially inhibit Na+-K+ ATPase.
Inhibits ADH => diuresis.
May decrease thyroid function.
Teratogenic (tricuspid valve malformation).
Excreted by kidney.
What drugs do lithium interact with?
Not to be taken with thiazide diuretics (e.g. chlorthiazide).
Lithium clearance is reduced by 25%.

All neuroleptics (with the exception of clozapine), produce more severe extrapyramidal syndromes when combined with lithium.
What are some therapeutic used os Li+?
Helps alleviate the depressive phase of bipolar illness.

Useful in refractory depression when added to SSRIs or TCAs, but not a good antidepressant alone.
What is the Mechanism of action of Li+?
Does not alter receptor numbers but alters the coupling of the receptors with their second messengers by reducing coupling of G-proteins.
Regulation of -AR and DAR.
Can reduce release of NTs (5-HT) and affinity of binding to receptor.
Inhibits breakdown of IP2 to IP1 (during PIP hydrolysis) and IP1 to Inositol=> depletion of DAG and IP3 and  [Ca2+] in response to receptor activation (i.e. from 5-HT2R, 1-AR, muscarinic receptors and others).
Alterations in adenylate cyclase and phospholipase C.
What are symptoms of Li+ toxicity (Mild to Moderate (1.5-2 mEq/L)in GI?
Abdominal pain
Dryness of mouth
What are symptoms of Li+ toxicity (Mild to Moderate (1.5-2 mEq/L)in Neurological?
Slurred speech
Lethargy or excitement
Muscle weakness
What are symptoms of Li+ toxicity (Moderate to Severe Intoxication >2.0-2.5mEq/L)in GI?
Anorexia nervosa
Persistent nausea and vomiting
What are symptoms of Li+ toxicity (Moderate to Severe Intoxication >2.0-2.5mEq/L)in Neurological?
Blurred vision
Muscle fasciculations
Clonic limb movements
Hyperactive deep tendon reflexes
Electroencephalographiic changes
What are some symptoms of Severe Li+ Intoxication (>2.5 mEq/L)?
Circulatory Failure (lowered blood pressure, cardiac arrhythmias, and conduction abnormalities).
Generalized convulsions
Oliguria (decreased urine output) and renal failure
What are uses of Valproic Acid?
A well known antiepileptic has been found to have antimanic effects. Shows efficacy equivalent to that of lithium during the early weeks of treatment and is being evaluated for maintenance treatment. Titrated well, the sedation can be controlled. Nausea being the only limiting factor in some patients.
May be used as first line treatment for mania, although it may not be as effective in maintenance treatment as lithium for some patients.
What are some symptom of Valproic acid toxicity?
Elevated liver enzymes including own.
Nausea and vomiting.
Abdominal pain and heartburn.
Tremor, hair loss,
Weight gain.
Negative interactions with other antiepileptics.
Teratogen: spina bifida
What is the use and mechanism of action of carbamazepine?
Effective as an antimania medication

Mechanism of action (Con’t):
May be due to decrease over-excitability of neurons (anticonvulsive effect).
What is the mechanism of action of Valproic acid?
Fully ionized at body pH, thus active form is valproate ion.
carboxylic acid.
 levels of GABA in brain.
May facilitate Glutamic acid decarboxylase (GAD).
Inhibits GAT-1.  [aspartate]Brain?
May increase membrane potassium conductance.
Decreases overexcitabitity/
hyperactivity (anti-convulsive effect).
What is the mechanism of action of Carbamazepine/
Tricyclic, antidepressant (bipolar)
Inhibits high frequency repetitive firing.
Decreases synaptic activity presynaptically.
Binds to adenosine receptors (?).
Inh. uptake and release of NE.
Potentiates postsynaptic effects of GABA.
Metabolite is active.
Which two antidepressants are Ca2+ blockers? And what is their mechanism of action?
Ca2+ Channel blockers

Mechanism of action (Con’t):
Block NT Release?