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152 Cards in this Set

  • Front
  • Back
What are some symptoms of depression?
unhappiness, weight loss, weight gain, insomnia, hypersomnia, indecisiveness, motor retardation, fatigue, feelings of worthlessness, suicidal ideation
what is the most common symptom of depression?
insomnia.
What is anhedonia?
inability to have fun.
What depression symptom are we most concerned about?
suicidal ideation.
What is a concern clinicians should have when they start a suicidal patient on antidepressants?
make sure the patient is not going to fulfill their ideation when they get the energy to do so.
What percentage of our population is diagnosed with major depression?
10 to 15%.
What percentage of patients with major depression commit suicide successfully?
10%.
What percentage of patients with major depression responds to treatment?
70 to 80%.
What are the three major treatments available for depression?
therapy, ECT, drug therapy.
If drug funded studies show 80% of patients responding to grud treatment for depression, what to government-funded studies show?
more like 50%.
In order to have replication studies for research done that have high placebo effect, what you need in the next study?
a larger sample size.
Name some drugs that can cause depression:
respirine, methyldopa, propanolol, birth control,benzos, steroids, alcohol, opioids.
What is respirine?
an old anti-hypertensive
what is methyldopa?
an old anti-hypertensive. Is pregnancy category a. Can use in pregnant women with high blood pressure (immediately post.)
How else can propanolol be used?
anxiety symptoms like, say for example, before a test, or posttraumatic stress disorder.
Do steroids commonly cause depression with acute or chronic use?
more commonly cause depression with chronic use.
What are the for major antidepressants categories?
MAO inhibitors, tricyclic antidepressants, selective serotonin reuptake inhibitors, or other agents.
How do MAO inhibitors work?
they block the enzyme MAO
what do MAOI's do in the synaptic cleft?
increase amounts of all three neurotransmitters, dopamine, serotonin, norepinephrine
can propanolol cloud your thoughts if you use it before test?
no, it only blunts your nervousness.
Why do not use maoi's on everyone?
so many drugs interact with them. Plus a lot of foods interact with them (cheese, wine, beer.).
What do antipsychotics do in the synaptic cleft?
they block dopamine.
What does dopamine cause in the body?
it depends on where it is working. In the gi, nausea and diarrhea. In the brain, increased dopamine. In the peripheral blood vessels, vasodilation.
What does MAO do to dopamine in the body?
it degrads it to an inactive product.
What do antipsychotics block in the brain?
dopamine.
How do beer cheese and wine interact with MAOi's?
they bind to receptors causing high blood pressure.
Can you give an MAOi with another antidepressant?
no.
Do we use a lot of MAOi's today?
no. Safer alternatives are available.
Which contraindication do we need to worry about the most with MAOi's?
make sure that we don't give them with other sympathomimetic drugs. Plus we need to know about the food interactions.
Are MAOi's very effective?
yes. They increase the amounts of all three neuro transmitters in the cleft.
What is the name of the MAOi patch?
selegiline.
What is the problem with the MAOi patch?
It is good because it is selected for MAO b, thus avoiding food interactions. However, it avoids first pass, and therefore can increase to toxic serum concentrations. When this happens, you lose selectivity.
How do TCAs work?
inhibit the reuptake of norepinephrine in the presynaptic neuron. They do this by binding to receptors of the presynaptic cleft. The presynaptic neuron will respond by sending out lots of norepinephrine. When you have lots of norepinephrine in the cleft, you get down regulation of receptors in the post-synaptic cleft. This makes the post-synaptic neuron less sensitive to norepinephrine, thus decreasing the symptoms of depression.
Name some TCAs:
Elavil, doxepin, nortriptyline, norpramiin
what is the most common side effect of TCAs?
dry mouth.
What are some common side effects of TCAs?
constipation, urinary retention, blurred vision. This is due to the antihistamine/anticholinergic effect. They also caused EKG changes and sexual dysfunction.
What is the EKG change that occurs with TCAs?
QRS prolongation.
How do you treat QRS prolongation in TCA overdose?
HCO3. It decreases the amount of free TCA in the circulation.
Why are anticholinergic side effects, so troublesome and the elderly?
because they decrease cognition. This is a concern in Alzheimer's disease. Patients can become more confused. It has to do with their effect on the parasympathetic nervous system (anticholinergic.).
Why do we not used TCAs that much anymore?
because they have a narrow therapeutic index. It is very easy to overdose on these drugs. Never give more than a one-month supply.
What, in essence, do MAOi's due in the synaptic cleft?
they prevent degradation of dopamine norepinephrine in serotonin, thus promoting down regulation of postsynaptic receptors.
Explain synaptic receptors response to serotonin in a depressed patient?
it is overly sensitive. This brings about depressive symptoms. But you can treat this: if you make a lot of neurotransmitter available, you can promote down regulation and shut down the oversensitivity.
A synaptic receptors in depressed patients more or less sensitive to neurotransmitters?
more sensitive. We want to promote more neurotransmitters in the cleft. So that those receptors get down regulated and become less sensitive.
Why are the synaptic receptors in depressed patients so sensitive?
there is a little neurotransmitter to begin with, they have an exaggerated response. When they come into contact with a neurotransmitter. This causes a depressed mood.
Which neurotransmitters do MAOi's increase in the cleft?
all three.
What is the main enzyme that breaks down all three neurotransmitters?
MAO.
Is there a test to tell which neurotransmitters deficient in the cleft?
no, there is no specific way to tell. It is unclear what exactly is happening in depressed patients.
In a depressed patient, wat is the overly sensitive postsynaptic neuron not usually seen enough of?
neurotransmitter.
How long does it take for down regulation of post-synaptic receptors to occur in treatment with depression?
weeks.
Should you induce vomiting in TCA overdose?
no.
What happens clinically with the TCA overdose?
rapid neurological and hemodynamic deterioration. Loss of gag reflex.
Why do not want to induce vomiting with TCA overdose?
because gag reflexes impaired.
What is one reason we do not used TCAs as much anymore?
because they are difficult to manage.
What can you give beside HCO3 with the TCA overdose?
activated charcoal/gastric lavage.
What else can he use, besides HCO3, to increase pH in TCA overdose?
intubation and hyperventilation.
How do SSRI's is work?
they block presynaptic reuptake of serotonin.
What is the best antidepressant for suicidal patient?
SSRI's. They are safer Re: overdose.
Why are SSRI's more commonly used than other antidepressants?
because they are easier to manage and safer to use.
What is a risk for SSRI's and suicidal patients?
the drug can give the patient the energy to actually commit the act.
With the SSRI's, what is happening in the synaptic cleft?
reuptake of serotonin is blocked. Ultimately, there is more serotonin in the cleft. This causes postsynaptic down regulation.
What side effects do we need to know for SSRI's?
nausea, headache, sexual dysfunction, insomnia, somnolence.
What percentage of people suffer sexual dysfunction from SSRI's?
10 to 20%.
What other side effects can SSRI's have?
anxiety, restlessness, tremor, akathesia (inability to sit still).
What is a rare side effect of SSRI's that has to do with breasts?
galacrorrhea - dopamine inhibits pituitary, specific for prolactin. Blocks dopamine, prolactin increases. Can cause males to have breasts, and women to lactate. Very rare.
How much data is available on the use of SSRI's and kids?
not a lot. Only prescribe them if you really need to.
What is a rare side effect of SSRI's regarding platelets?
platelets also release, like thromboxane, serotonin. Can activate if you block serotonin. There could be an increased potential for bleeding. But this is very rare.
Explain why EPS occur with antipsychotics?
because they are dopamine blockers. However, the new ones don't block dopamine as much.
What was the first SSRI to be approved?
Prozac.
Which SSRI is the most "activating?"
Prozac. It also causes more insomnia and tremor.
Where is Prozac cleared?
liver.
What is the half-life for Prozac and its metabolites?
one to three days for drug, four to 16 days for active metabolites.
His Luvox indicated for depression?
no it is indicated for OCD.
Which SSRI has the highest incidence of GI effects?
Zoloft. You should take it with food.
We're a Zoloft cleared?
in the liver. Extensively.
What is the difference between select celexa and Lexapro?
nothing really. Lexapro is an S isomer. Lexapro is more potent. Lexapro is the active part of the molecule.
Which SSRI has the longest half-life?
Prozac.
Which SSRI has the shortest half-life?
Paxil. It is 22 hours, almost the day.
Which SSRI is most likely to cause withdrawal symptoms with abrupt cessation?
Paxil. It has the shortest half-life.
Which patients, genetically, will SSRIs be less effective with?
people who over express CYP 2-D 6. The exception is Prozac, which has an active metabolite. Prozac is a pro-drug.
Which SSRIs are least likely to have an interaction with another drug?
Celexa, Lexapro
which SSRI is best to use for patients who sleep too much (hypersomnia?)
Prozac. It is the most stimulating of all.
Why does Zoloft have the most G.I. Effects?
because of the local activity on the dopamine receptors in the G.I. tract. There is nausea, vomiting, diarrhea. At first when starting Zoloft.
Which SSRI is good to give the depressed patient who was having trouble sleeping?
Paxil. It has the most anticholinergic/antihistamine effects.
Name all of the SSRIs
Luvox, Prozac, Paxil, Zoloft,celexa, Lexapro.
Why did they invent Paxil CR?
so that would be released lower in the G.I. tract, maybe this will cause less nausea and vomiting.
Why do they not use Luvox for depression?
because it has too many other drug interactions. You really couldn't give it in the elderly. It is used for OCD only.
How does how Effexor work?
it blocks reuptake of norepinephrine in the synaptic cleft.
is Effexor, long or short acting?
short acting.
What are the side effects with Effexor?
those common to other SSRIs, plus high blood pressure, high pulse (especially at high doses.).
Who should we avoid using Celexa with?
patients with cardiovascular disease.
Is Effexor an SSRI?
it is an SNRI
what is antidepressant that inhibits reuptake of both serotonin and norepinephrine?
duloxetine (cymbalta.)
When would we use Duloxetine (cymbalta?)
only if other drugs are not working. This drug is more aggressive. It also costs more.
What drugs fall under "other agents?"
Wellbutrin, trazodone, serzone, Remeron.
How does Wellbutrin work?
it blocks reuptake of dopamine and to some extent, norepinephrine in the synaptic cleft.
What does Wellbutrin due to wakefulness?
it stimulates, rather than sedate.
Why do we use Wellbutrin and younger people?
because there are less sexual side effects.
What things do you have to worry about with wellbutrin when you're causing increased dopamine in the synaptic cleft?
psychosis. Haldol and Thorazine are dopamine blockers. Also have to worry about seizures.
As trazodone often used for depression?
very rarely. It is more as a sedative for a sleep aid. Dose for sedation is 25 to 100 mg, and dose for depression is up to 500 mg. For this reason we don't use it for depression very often.
Why do we not use serzone as much anymore?
is toxic on the liver.
Which antidepressant is most toxic of the liver?
cymbalta.
Which antidepressants, would we do LFT monitoring for?
cymbalta, serzone. Both are toxic of the liver.
What is Remeron classified as?
a tetracyclic agent.
What is the method of action of Remeron?
it blocks alpha receptors, resulting in enhanced norepinephrine levels.
What is unique about Remeron and its side effects?
it is very sedating. It also causes a lot of weight gain. It's not good for fat people. Otherwise it is very well tolerated.
In summary, MAOi's:
very effective, but there are limits because of the blood pressure risks in food and drug risks.
In summary, TCAs:
work by inhibiting presynaptic uptake of norepinephrine, difficult to use in the elderly, because of anticholinergic side effects, risk for overdose. Treat overdose with HCO3, do not induce vomiting.
In summary, SSRI's:
most widely used. Well tolerated. Common side effects are nausea and sexual dysfunction.
Problems with Effexor?
BP, liver.
Who do we not use Wellbutrin for?
mental illness. But it is good for sexually active people. Also not as much weight gain.
Which receptor does Remeron work on?
alpha-2 receptors.
Explain how Remeron works in the synaptic cleft:
there are alpha 2 receptors attached to the presynaptic neuron. They release all three neurotransmitters when stimulated. Remeron blocks them. So we call Remeron, a presynaptic alpha-2 receptor blocker.
What good thing happens in the cleft when you give Remeron?
you have a lot of different neurotransmitters that show up there.
What is serotonin syndrome?
It is not a spontaneous drug reaction. It is caused by excess serotonergic activity at CNS and peripheral serotonin receptors. The excess serotonin activity produces clinical symptoms that can range range from barely noticible to fatal.

Sx onset is rapid after poisening. They include:
The symptoms are often described as a clinical triad of abnormalities:

Cognitive effects: mental confusion, hypomania, hallucinations, agitation, headache, coma.
Autonomic effects: shivering, sweating, fever, hypertension, tachycardia, nausea, diarrhea.
Somatic effects: myoclonus/clonus, hyperreflexia, tremor.

Hard to pinpoint, because it can be so many other things.
In what pregnancy category to most antidepressants fall?
category C. Paxil is recently bumped to category D, because an increased risk was noted.
With SNRI's like effexor, what happens when you keep going up on the dose?
that inhibits the receptor for both norepinephrine and serotonin. As you go up in the dose, blood pressure goes up.
With all antidepressants, how long does it take see the full effects?
4 to six weeks. Vegetative symptoms will respond first.
When should we think about discontinuing antidepressants?
failure to respond, and after six to 12 months if good response.
How do you does a patient with an antidepressant when you first start them on it?
small doses, then gradually titrate upwards.
How do you take a patient off of antidepressants?
slowly to prevent withdrawal.
What are some withdrawal symptoms with antidepressants?
headache, nausea, dizziness, insomnia, nervousness.
What if you get a poor response from an antidepressant?
consider changing the drug to one with a different method of action, or maybe add on another for augmentation.
Mr. Smith is a 65-year-old man with a history of hypertension, heart disease, GERD and seizure disorder. He is newly diagnosed with depression that feature suicidal ideation's, somnolence, and lack of interest in most activities. What medication might be of use?
(hint: Figure out which ones to rule out first, then figure out which one is appropriate for his type of depression.)
avoid tricyclics because of the risk. No Wellbutrin because of the seizure disorder. Maybe try Prozac, because it is more stimulating (for his somnolence).
what are the 4 antianxiety drugs we are going to study?
ativan, xanax, libruim, valium
what benzos do to the sleep process?
the appropriate sleep distribution between all of the stages of sleep.
Why are benzos controlled?
because they're physically and psychologically addictive.
What will happen if we stop a benzo abruptly?
there will be withdrawal symptoms, and a rebound of whatever you were treating (anxiety, seizure, etc.).
Do antidepressants work for anxiety?
yes. They all work for anxiety.
What do benzos produce in the body?
sedation, antianxiety activity, muscle relaxation, anticonvulsant activity.
Can you develop a tolerance with benzos?
yes. Tolerance builds to sedation, but not tothe antianxiety effect.
What is the method of action of benzos?
they enhance the activity of GABA receptors.
What are some low to medium potency benzos?
Librium and Valium.
What are some high potency of benzos?
Ativan and Xanax.
What is benzo 1 GABA receptor a selective for?
sedation and sleep.
What is benzo 2 GABA receptor b selective for?
antianxiety, muscle relaxation and anticonvulsant.
What is sonata?
it is like Ambien. It is a benzo like drug.
Describe selectivity with sonata and Ambien:
they bind preferentially to benzo 1 GABA receptor a.
When prescribing sleep medication, what would you give to someone who is having early awakenings?
a longer acting benzo. Not Xanax.
Who in the population uses more sleep aids and anyone?
20 to 44-year-olds.
Name three new insomnia drugs:
lunesta, Ambien CR, rozerem.
What is rozerem?
souped up melatonin. It helps reset the biological clock. It has a short half-life.
Which sleep aids are best for induction?
the ones with a short half-life. (rozerem).
Which sleep aids are best for maintenance of sleep?
the one longer half-life. (lunesta.)
What is romazicon?
generic: flumazenil. It is a benzo antagonists. It reverses benzos.
Why must we be careful with romazicon?
if the patient is suffering from a mixed TCA/benzo overdose, you can induce the TCA seizures by removing the benzo.
Does buspar act on GABA receptors?
no, it is a serotonin modulator.
When does BuSpar begin to work?
in a few weeks, like antidepressants. It does not give an immediate effect like benzos do.
What are some advantages to BuSpar?
low cost, low abuse, easy to give.
How do antihistamines work is sleep aids?
the anticholinergic effect is sleep promoting.
Which barbiturate can be used as a sleep aid?
phenobarbital.
What is the method of action of phenobarbital?
it enhances GABA activity and more widespread CNS depression.
What makes barbiturate sleep aids, dangerously unique?
they are extremely potent. There is huge CNS depression. You can really overdose and die. They are also inducers of CYP.