Psychopharmacology Flashcards
This is the thought that the lack of 5-HT and NE results in depression, so replacement of these NT’s will reduce depression
Amine hypothesis
All major anti-depressants except for which drug will work on the amine hypothesis?
Buproprion
True or False: all anti-depressants have a LONG latency, so they typically dont work right away.
True
What % of patients fail to respond to treatment with antidepressants?
1/3-1/2
Fluoxetine, Paroxetine, Sertraline, Citalopram, Fuvoxamine, and Excitalopram belogn to which drug class?
SSRI
What is the advantage of SSRI’s over other AD classes (like MAOI’s) as far as toxicities?
They do not have the toxicities like TCA’s or MAOI’s (anti-muscarinic, antihistaminic, and a-adrenroreceptor blocking actions) so theyre better tolerated
This is the metabolite of Fluoxetine, has a half life of 7-9 days, and thus extends the time fluoxetine is effective.
Norfluoxetine
Sertraline and Paroxetine have pharmacokinetics similar to what other drug class?
TCA’s
What was the trial that looked at pts with major depression who did not respond to or could not tolerate therapy with 1 SSRI?
STAR*D
According to the STAR*D trials, what % of patients had a remission rate using an SSRI?
25%
What is the major adverse effect of citalopram, making it contraindicated with cardiac or eating disorders?
prolonged QT itnerval
Case: pt presents to the ER with a recent diagnosis of depression and complains of hyperthermia. The patient soon slips into a coma and experiences muscle rigidity, myoclonus, and rapid changes in mental status. What condition is he experiencing?
Serotonin syndrome
Giving SSRI’s with what other drug class can precipitate Serotonin syndrome?
MAOi’s
What is the DOC for serotonin syndrome to reverse the Sx?
Cyproheptadine
5-HT2 antagonist
What is the only SSRI apporved for the use in pediatrics?
Fluoxetine (prozac)
What must you monitor in kids taking prozac, because of the increased risk of suicide during the first weeks of Tx?
Mood
Case: a patient presents to you with depression and you consider starting him on pharmacotherapy. What other condition might be an indicator to use Bupropion?
A. Bulemia B. Concurrent CAD C. 20-pack year smoking Hx D. Insomnia E. Migrane
C. Smoking Hx
Bupropion slaps both depression and smoking in the face. The other answers are contraindications to use Bupropion.
True or False: Unfortunately, as with other antidepressants, Bupropion has a side effect of sexual dysfunction.
FALSE
There is NO sex side effects with buproprion
Which of the SSRI has the following antagonism to the receptors?
Sedative- + Antimuscarinic- + Serotonin- +++ NE- 0,+ DA- 0,+
Fluoxetine
Which of the SSRI’s has the following antagonism to the receptors?
Sedative- + Antimuscarinic- 0 Serotonin- +++ NE- 0 DA- 0
Sertraline
Which of the TCA’s (Protriptyline, imipramine, Amtryptyline, Desipramine) has the following antagonism to the receptors?
Sedative- +++ Antimuscarinic- +++ Serotonin- +++ NE- + DA- 0
Amitriptyline
Which of the TCA’s (Protriptyline, imipramine, Amtryptyline, Desipramine) has the following antagonism to the receptors?
Sedative- + Antimuscarinic- + Serotonin- 0 NE- +++ DA- 0
Desipramine
Which of the TCA’s (Protriptyline, imipramine, Amtryptyline, Desipramine) has the following antagonism to the receptors?
Sedative- ++ Antimuscarinic- ++ Serotonin- +++ NE- ++ DA- 0
Impiramine
Which of the TCA’s (Protriptyline, imipramine, Amtryptyline, Desipramine) has the following antagonism to the receptors?
Sedative- 0 Antimuscarinic- ++ Serotonin- ? NE- +++ DA- ?
Protriptyline
What does Bupropion do the antagonism to the receptors?
Sedative Antimuscarinic Serotonin NE DA
Sedative- 0 Antimuscarinic- 0 Serotonin- +,0 NE- +,0 DA- ?
What is the drug class that has a lot of side effects, like antimuscarinic, anti-a-adrenergic, and antihistaminergic (drowsiness)?
TCAs
What is the typical STARTING dose for TCAs?
Low doses (~100mg/day for inpatient and 10-75mg/day for outpatient)
How much do you increase the TCA’s dose every 2-3 weeks?
25mg
All TCA’s end in what 2 suffixes, except for doxpin and amoxapine?
-iptyline or -ipramine
What are the Sx of TCA OD?
Coma with acidosis, respiratory depression, agitation, seizures, bowel-bladder paralysis, cardiac arrhythmias
(Tri-C’s = Convulsions, Coma, Cardiotoxicity)
What is the DOC for TCA OD?
NaHCO3
If a patient tries to commit suicide with TCA’s, what 2 things must u do to avoid OD again?
- Prescription for < 1.25g or 50 dose units with no refill
2. Entrust drug to relative
What are the 3 adjunctive therapies to antidepressants?
Li
Thyroid H’s
Atypical anti-psychotics
What are the 5 “D’s” of AD treatment?
Diagnosis (is the pt actually depressed?) Drug (would a different AD work better?) Dose Duration Different Tx (should we try ECT?)
What is the condition to which Clomipramine is used for?
OCD
To which class of drugs does Clomipramine belong?
TCA
Which drug class acts on the the GABA(A) receptors, and increases the frequency of GABA receptor openings?
Benzo’s
What is the primary indication for Alprazolam?
Panic disorders
What is the primary indication for lorazepam?
Generalized Anxiety Disorder
What is the primary indication for Meprobamate?
Short-term anxiety and sedative hyponosis
What % must you taper off a benzo per week until the dose is 50% of the original?
25%
Once the dose reaches 50% of the original dose while you taper a benzo, what amount do you decrease the dose?
↓ 1/8 dose every 4-7 days
Which type of patient is Meprobamate a contraindication?
Pregnant ladies cuz it’s a teratogen
What receptors does Azapirones act on, which inhibits serotonin release?
5HT1A
What is the main indication for Buspirone?
Generalized anxiety disorder
“I’m always anxious if the BUS will be ON time, so I take BUSpirONe.”
In terms of side effects, what is the advantage of Buspirone over Benzos?
No sedation, addiction, tolerance, or interaction with alcohol.
What is the site of Z-hyponotics action?
GABA(A) typ`e 1 receptors
Sedative actions, anterograde amnesia, exhaustion, and intoxication are all Sx of intoxication to what drug class?
Benzo’s
During which trimester is the fetus at risk of congenital malformations if mom uses a benzo?
1st trimester
After what time of prolonged use does dependence become a big problem with benzo use?
2-3 weeks
Which benzo can cause seizures with abrupt discontinuance, especially 24-72 hours after the discontinuance?
Alprazolam (xanax)
What is the dose of Alprazolam that is given to treat panic disorder but also causes withdrawal Sx?
4 mg daily
What is the deal with the demonstrated efficacy of chlordiazepoxide for long term use (> 4 mo)?
The efficacy has not been established, so u gotta keep reassessing to make sure it’s working
This is the drug u give for preop sedation, anxiolysis, and anterograde amnesia.
Midazolam
What are the 2 routes of administration for Midazolam?
IM or IV
What is the receptor that Buspirone stimulates?
5-HT1A
True or False: Buspirone is effective in panic disorder just like it is for Generalized Anxiety Disorder.
FALSE
It has a gradual onset of action and therefore is not effective in Panic disorder.
How long does it take to see the effects of Buspirone?
2-4 weeks
2013 first aid says 1-2
Which receptor does Serotonin bind to induce B-endorphin secretion, which allows the antidepressant effects?
5-HT1A
same one Buspirone binds
Which form of Zelpidem tartrate had the adverse effects of drowsiness, dizziness, diarrhea, headache, amnesia, vertigo, falls, nausea, and vomiting?
conventional Tablet
Which form of Zelpidem tartrate caused just headache, somnolence, and dizziness?
Extended release tablet
What class of drugs does Zolpidem belong to?
ZopiDEM = Ambien, which is a nonbenzodiazepine hypontoics
What are the main indications for ZOLEPLON use?
Sleep-driving, making phone calls, or preparing and eating food while asleep.
What is the mg of Midazolam that is given 30-60min before surgery in adults < 60 y/o?
5mg
What are the 3 conditions where the dose of midazolam is adjusted before surgery?
- COPD pts
- High risk pts
- Pts who take opiate agonists or other CNS depressants.
What is the mg of Midazolam that is given to adults > 60 y/o?
2-3mg
There is a hypothesis that psychosis is caused by a relative excess of what NT in the dorsal and/or ventral striatum?
Dopamine
There is also a hypothesis that states that an excess of what NT causes + and - symptoms of schizophrenia?
Serotonin
Where is the majority of Serotonin made in the CNS?
Raphe nucleus
Where does the dosal and rostral raphe nuclei connect in the brain, which is throught to be associated with schizophrenia?
Dorsal raphe nuclei –> substantia nigra
Rostral raphe nuclei –> cerebral cortex
Which DA pathway gives + symptoms, increased in schizophrenics, and causes hallucinations/delusions?
Mesolimbic pathway
Which DA pathway gives negative Sx, is decreased in schizophrenics, and cuases the slowing, avolition, and confusion characteristics?
Mesocortical pathway
Which DA pathway gives extrapyramidal Sx and tardive diskinesia, and is decrased in schizophrenics?
Nigrostriatal pathway
Which DA pathway is normal in schizophrenics, but can cause hyperprolactinemia if anypsychotics block it?
Tuberoinfundibular pathway
All “typical” antipsychotics block what receptor?
D2
What are the typical antipsychotics?
doll’s like magazines
Haloperidol, droperidol, fluphenazine, thorazine, chlorpromazine
DOLls like magaZINEs
Which 3 typical antipsychotics have a high potency (2-20mg/day) and can therefore cause extrapyramidal Sx?
Trifluoperazine, Fluphenazine, and Haloperidol
Try to Fly High
Which 2 typical antipsychotics have a low potency (300-800 mg/day) and can therefore cause non-neurological SE like anticholinergic, antihistamine, and a1-blockade?
Chlorpromazine, Thioridazine
Cheating Thieves are LOW
Which 2 typical antipsychotics have a medium potency (10-100mg/day) and are neuroleptics?
Loxapine, Perphenazine
What class of antipsychotics are 5-HT2, D2, alpha, and H1 blockers?
Atypicals
To remember the atypical antipsychotics, what does the following sentence mean?
“It’s atypical for old closets to quietly risper from A to Z”
Olanzapine, clozapine, qutiapine, risperidone, aripipazole, ziprasidone
(also, “I am DONE with OLE PINE trees” is another mnemonic)
Though 1st generation antipsychotics improve + Sx, they have a lot of what SE?
EPS
But yay! 2nd gen antipsychotics improve Sx with less EPS… HOWEVER, what is their main SE?
They make u fat
You need to check weight, BP, fasting glucose, and fasting lipid panels at what checkpoints in antipsychotic therapy?
Baseline, 1 mo, 3 mo.
So you got through the 3 months of checkpoints all good, now what 3 things must u check every year while a pt is on antipsychotics?
Weight, BP, fasting glucose.
And what must u check every 3 years while a pt is on antipsychotics?
Fasting lipid panel
Other than making u fat, having deposits in the cornea/lens are SE of clorpromazine, what other SE is specific for this drug?
Photosensitivity
Chlorpromazine = Cornea
Which typical antipsychotic is associated with retinal deposits, resembling retinitis pigmentosa and causes browning of the vision?
Thioridazine
Thioridazine = reTina
Which antipsychotics is used for emisis becuase it blocks DA centrally in the CTZ and peripherlally in the stomach?
Prochlorperazine
Which antipsychotics is used for perioperative sedation cuz it blocks H1?
Promethazine
Which antipsychotics is used for neuroleptanesthesia cuz it blocks H1?
Droperidol (+ fentanyl)
What is the most effective antipsychotic, but has a SEVERE side effect of agranulocytosis?
Clozapine
Watch CLOZapine CLOZely!
Which antipsychotic is first line for acute psychosis but can cause weight gain, sedation, dry mouth, and constipation?
Olanzapine
Which antipsychotic is used for the psychosis in parkinsons pts because it has a low D2 effect?
Quetiapine
Parkisons are Quiet
Which atypical antipsychotic has a big risk for QT interval prolongation and is metabolized by aldehyde oxidase?
Ziprasidone
Which receptor in the body is inhibited if you have SE like EPS and ↑ PRL?
D2
Which receptor in the body is inhibited if you have SE like cognitive deficits, dryu mouth, constipation, tachycardia, urinary retention, and blurred vision?
M1
Which receptor in the body is inhibited if you have SE like sedation, weight gain, and dizziness?
H1
Which receptor in the body is inhibited if you have SE like hypoTN?
a1
Which receptor in the body is inhibited if you have SE like anti-EPS?
5-HT2A
Which receptor in the body is inhibited if you have SE like satiety blockade?
5-HT2C
In summary, what drugs cause SE like EPS?
High potency
Try to Fly High
In summary, what drugs cause SE like weight gain?
Olanzapine and Clozapine
In summary, what drugs cause SE like hyperPRL?
all typicals and risperidone + paliperidone
In summary, what drugs are cheaper (typicals or atypicals)?
Typicals
Increased sensitivity of the DA receptors can cause what condition?
Tardive dyskinesia
What is the condition characterized by autonomic instability, muscle rigidity, diaphoresis, profound hyperthermic, and myoglonemia?
Neuroleptic malignant syndrome
What is the mortality rate in NMS?
20%
What are the drugs for the treatment of NMS?
Bromocriptine- for the D2 blockade
Dantroline- for the rigidity
Benzo- for the muscle relaxant.
What is the medicaiton that can be used as monotherapy for less severe manic of mixed episodes?
Li
What 2 conditions that Li can be used prophylactically for?
Mania and Depression
Polyuria, polydipsia, tremor, mental confusion, withdrawal, and bizarre movements are all SE of what medication?
Li
What condtion is Li a contraindication for, as it depresses the SA node?
Sick sinus syndrome
What condition often coexists with bipolar disorder, but is treated when you use Li because of the additional actions?
Alcoholism
What is the metabolism and excretion mechanism for Li?
It;s not metabolized and renally excreted
What are the Sx in infants if mom took Li whilst breastfeeding?
Lethargo, cyanosis, poor suck response and Moro relfexes.
In addtion to the CBC, urinalysis, and blood tests, what other test must u get in older patietns before starting Li due to side effects?
EKG
What substance in the Gq pathway is inhibited to form by Li?
IP3
inhibits IP2 –> IP3
Li is used with what other drug class in acute manic episodes?
Anti-psychotics or Anti-convulsives (carbamazepine)
What is the dose of carbamazepine that is given with Li in acute manic episodes?
200mg
What is the term for continuing Li therapy after the relief of manic Sx?
Maintenance or prophylactic therapy
keep them on it if theyve had a lot
What is the antiseizure drug that is contraindicated in pregnant ladies due to teratogenic effects?
Valproic acid
Which class of antipsychotics (typical or atypical) give the following changes in the dopamine pathways?
Mesolimbic- normal
Mesocortical - ↓↓
Nigrostriatal- ↓
TUberoinfundicular- ↓
1st generation
remember the ↑ risk of EPS/TD and they worsen the negative Sx of psychosis
Which of the following atypical antipsychotics have a better maintenance control?
Quetiapine, Risperidone, Ziprasidone, Aripiprazole, Olanzapine
Quetiapine
Aripiprazole
Olanzapine
Which of the following atypical antipsychotics have a better induction control?
Quetiapine, Risperidone, Ziprasidone, Aripiprazole, Olanzapine
Risperidone
Ziprasidone
Which of the following antiepileptics have a better effect on mixed episodes?
Valproate/divalproex sodium, Carbamazepine, Lamotrigine
Valproate/divalproex sodium
Which of the following antiepileptics have a better effect on depressed episodes?
Valproate/divalproex sodium, Carbamazepine, Lamotrigine
Lamotrigine
sad Lamb
Which of the following antiepileptics have a better effect on manic episodes?
Valproate/divalproex sodium, Carbamazepine, Lamotrigine
Carbamazepine
What is the most effective mood stabilizer and also prevents suicidal thoughts?
Li carbonate
Which class of antidepressants is just as effective as TCAs but way safer?
SSRIs
Which class of antidepressants are just as effective as SSRIs and TCA’s, but their action is similar to TCAs but have a lower SE than TCAs?
SNRIs
Which class of antidepressants is less effective than MAOi’s but are good for pain, headaches, and insomnia?
TCAs
TCAs carry a huge risk for what event due to their narrow therapeutic index?
Overdose
Case: pt presents to the ER with a BP of 190/120 after eating at a pizza parlor. His friend stated he just got placced on a medication for depression. What class of drugs is the pt on?
MAOi’s
Tyramine causing hypertensive crisis
Which drugs are best for panic disorders and acute anxiety, but carry a risk for addiciton, dependence, and withdrawal Sx (szrs)?
Benzos
Antihistamines, Benzos, Barbs, and “Z” drugs (zolpidem, eszopiclone, zaleplon) and Trazodone all can be used for what condition?
Sleep disorders
What is the class of drugs for ADHD that causes fast arousable and produce a “high”?
Amphetamines
What is the ADHD drugs that are arousable but dont produce the same rush, and are slower release?
Mehtylphenidates