Pharm Flashcards
name 3 typical antipsychotic agents
haloperidol
chlorpromazine
fluphenazine
(haloperidol + “-azines”)
typical antipsychotics
mechanism of action:
block dopamine D2 post-synaptic receptors»_space; incr [cAMP]
what are the 3 main side effects of low potency typical agents?
give 2 examples of low potency typical agents.
low potency typical agents cause:
- sedation
- hypotension
- seizure-threshold reduction (i.e., incr likelihood for seizures)
chlorpromazine and thioridazine
(“CHeating THieves are LOW”)
high potency typical agents cause what kind of side effects?
movement disorders (EPS symptoms)
give 3 examples of high potency typical agents.
trifluoperazine
fluphenazine
haloperidol
(“Try to Fly HIGH”)
what percent of D2 receptors should be occupied to provide efficacious treatment?
at what percent would you begin to see EPS side effects?
60-75% D2 receptor occupancy = efficacy
≥80% = EPS
what 3 other receptors give non-neurologic side effects assoc w/ low potency typical agents?
- anticholinergic (antimuscarinic) effects: dry mouth, constipation, urinary retention, blurred vision, sedation
- antihistamine effects: sedation
- alpha-adrenergic effects: orthostatic hypoT, impotency/ejac interference
what 2 side effects are assoc w/ anti-dopamine effects?
- dopamine receptor antagonism»_space; hyperprolactinemia
- extrapyramidal system SEs (EPS) / tardive dyskinesia (TD)
how would you treat the EPS / tardive dyskinesia assoc w/ the anti-dopamine effects of typical antipsychotic agents?
give 3 options for treatment.
anticholinergic agents:
- diphenhydramine
- benztropine
- trihexyphenidyl
which atypical antipsychotic drug causes agranulocytosis?
therefore, what must be monitored while on this drug?
clozapine
-must monitor WBCs
neuroleptic malignant syndrome (NMS) is another toxicity of typical antipsychotic agents and is fatal in 10-20% of cases. what drug is given to treat NMS?
dantrolene
give the 4 main side effects assoc w/ atypical antipsychotic agents.
weight gain
metabolic effects (hyperglycemia, hyperlipidemia)
QT prolongation / ECG changes (only a few)
stroke
which agents, typical or atypical, are more commonly used for first line therapy?
ATYPICAL = first line therapy
adherence (compliance) is critical in treatment of psychotic disorders. how can non-adherence be managed?
long-acting injectable agents (LAIAs)
what typical (2) and atypical (4) antipsychotics are used as long-acting injectable agents to manage non-adherence?
typical: -haloperidol decanoate -fluphenazine decanoate ------------------------- atypical: -risperidone -olanzapine pamoate -aripiprazole -paliperidone palmitate
how long does it take to evaluate response to therapy?
2–3 weeks
what would you give as an adjunctive therapy in pts that are acutely agitated bc the therapeutic drug hasn’t kicked in yet?
benzodiazepines (e.g., diazepam / alprazolam / lorazepam)
what antipsychotic drug is used in pts with suicidal thoughts/behaviors?
clozapine
Question: A 35‐year‐old homeless man has been taking thioridazine for many years to control his schizophrenia and has experienced numerous typical adverse effects of treatment, including blurred vision, dry mouth, mydriasis, nausea, urinary retention, and constipation. These effects are caused by blockade of which of the following receptors? A. Alpha adrenergic B. Dopamine C. Nicotinic D. Serotonin E. Muscarinic
E. Muscarinic
which 2 typical antipsychotics have the most antimuscarinic effects?
thioridazine
mesoridazine
which 2 atypical antipsychotics have the most antimuscarinic effects?
clozapine
olanzapine
Question: A 63‐year‐old man presents with social withdrawal, blunted affect and poor hygiene. After taking an antipsychotic medication prescribed for these symptoms, he developed blurry vision, weight gain and excessive salivary secretions. Laboratory results show fasting hyperglycemia. Which of the following drugs is he most likely taking? A. Olanzapine B. Haloperidol C. Lithium D. Asenapine E. Valproic acid
A. Olanzaprine
weight gain and metabolic effects are side effects from which class of antipsychotics – typical or atypical?
ATYPICAL»_space; weight gain, metabolic effects, stroke
Question: A highly agitated 23‐year‐old woman is admitted to a psychiatric unit complaining that “dead people” are telling her that she is going to be buried alive. She also claims that Jimmy Fallon has been reading her mind and telling everyone her intimate secrets on TV. Organic causes for the patient’s behavior are ruled out, and a thorough psychiatric evaluation indicates that her current behavior did not arise secondary to a mood disorder. The patient is treated with a drug considered to be appropriate for her condition. Two days later she complains of severe pain in the eyes and neck and is found to have a fixed upward gaze and a twisting upward torsion of the head. Treatment with which drug would most likely cause the patient’s eye and neck problem? A. Amitriptyline B. Chlorpromazine C. Fluphenazine D. Lithium E. Risperidone
C. Fluphenazine
Fluphenazine (+++) > Chlorpromazine (++)
EPS symptoms are most likely to result as a side effect from which class of antipsychotics – typical or atypical?
TYPICAL»_space; EPS
which 4 typical antipsychotic drugs are most likely to induce EPS as a side effect in a pt? (only looking at (++++) and (+++))
haloperidol (++++)
fluphenazine (+++)
trifluoperazine (+++)
pimozide (+++)
which 1 atypical antipsychotic drug may cause EPS as a side effect in a pt?
lurasidone (+++)
Question: A 38‐year‐old patient is being treated with clozapine for negative symptoms associated with schizophrenia. Which of the following laboratory tests is most important to monitor during initial therapy? A. Red blood cell count B. Platelet count C. Serum creatinine D. White blood cell count E. Serum lipase
D. White blood cell count
“Must watch CLOZapine CLOZely!”
Question: A 31‐year‐old man with schizophrenia is evaluated because of signs of tardive dyskinesia. He has been treated with several different medications to control his schizophrenia during the past several years. His physician stops treatment with his current medication and prescribes clozapine 25mg. He is currently taking no other medications. This patient is most likely to require special monitoring and surveillance due to the potential of clozapine to cause which of the following adverse effects? A. Agranulocytosis B. Seizures C. Diabetes D. Orthostatic Hypotension E. QT prolongation
A. Agranulocytosis
Question: A 22‐year‐old schizophrenic patient is unfortunately diagnosed with NMS following treatment with a high‐dose, multi‐drug regimen for his psychiatric condition. Which of the following agents is best suited for therapy of this condition? A. Alprazolam B. Dantrolene C. Phenytoin D. Aspirin E. Valproic acid
B. Dantrolene
Question: A 41‐year‐old schizophrenic patient is being treated with haloperidol and chlorpromazine and develops a drug‐induced acute dystonic reaction. Which of the following is the most appropriate acute therapy? A. Lithium B. Diphenhydramine C. Imipramine D. Tranylcypromine
B. Diphenhydramine
May also use benztropine or trihexyphenidyl
Question: In comparing neuroleptics, which of the following is more likely associated with skeletal muscle rigidity, tremor at rest, flat facies, uncontrollable restlessness, and spastic torticollis? A. Haloperidol B. Clozapine C. Olanzapine D. Ziprazidone E. Quetiapine
A. Haloperidol
Question: A 22‐year‐old, obese college student is diagnosed with schizophrenia. Which of the following medications would be most appropriate given her current weight while also effectively treating her schizophrenia? A. Aripiprazole B. Divalproex C. Clozapine D. Amitriptyline E. Olanzapine
A. Aripiprazole
-Although atypical antipsychotics (like aripiprazole) usually cause weight gain, aripiprazole (0/+) is the least likely of the atypicals. If a typical antipsychotic was an answer choice, it would be a better choice.
Question: A schizophrenic patient has a history of cardiac arrhythmias due to a prolonged QT interval. Which agent should be avoided in this patient because it can cause further QT prolongation, with an associated risk of serious ventricular arrhythmias, including torsades de pointes? A. Diazepam B. Fluoxetine C. Phenobarbital D. Phenytoin E. Thioridazine
E. Thioridazine
ECG changes are predominantly a side effect from which class of antipsychotics - typical or atypical? which typical antipsychotic drug is most likely to cause ECG changes in a pt?
TYPICAL»_space; ECG changes
thioridazine
most atypical antipsychotics do not cause ECG changes. however, if an atypical antipsychotic is used and ECG changes (QT prolongation) result, which drug was most likely used?
ziprasidone
Question: A 31‐year‐old woman is treated with an antipsychotic agent because of a recent history of spontaneously removing her clothing in public places and claiming she hears voices telling her to do so. Her BP is normally 130/70 mmHg. Since being treated, she has had several bouts of syncope. Orthostatic hypotension was noted on physical exam. Which of the following drugs most likely caused the syncope? A. Chlorpromazine B. Fluphenazine C. Haloperidol D. Olanzapine E. Ziprazidone
A. Chlorpromazine
which 2 typical and 1 atypical antipsychotics are most likely to cause hypotension as a side effect?
typical:
chlorpromazine
thioridazine
atypical:
clozapine
Question: A 36‐year‐old woman has had schizophrenia for several years, during which time she has received various types of medications. Her current treatment is with thioridazine, and she is experiencing amenorrhea and galactorrhea. Which of the following antipsychotic agents would be more appropriate for this patient to decrease the severity of her current adverse effects? A. Quetiapine B. Haloperidol C. Paliperidone D. Risperidone E. Thiothixene
A. Quetiapine
hyperprolactinemia is a side effect of which class of antipsychotic drugs – typical or atypical?
TYPICAL»_space; prolactin
which atypical antipsychotic drug is most likely to give hyperprolactinemia?
risperidone
which 2 atypical antipsychotics are most likely to cause weight gain, metabolic effects, and seizures?
clozapine
olanzapine
which 3 atypical antipsychotics are most likely to cause stroke?
olanzapine
paliperidone
risperidone
which 3 typical antipsychotics are most likely to cause sedation (may be used with atypical at night to induce sleep)?
chlorpromazine (+++)
mesoridazine (+++)
thioridazine (++/+++)
What are the 2 categories for ADHD meds?
Stimulants and non-stimulants
What are the stimulant drugs for ADHD?
- Amphetamine (d,l), Dextroamphetamine (d) (Methamphetamine)
- Lisdexamfetamine (pro‐drug)
- Methylphenidate (d/d,l) & Dexmethylphenidate (d)
What are the non-stimulant drugs for ADHD?
Atomoxetine
Guanfacine
Clonidine
What are the MOA of stimulants (ADHD)?
Main effect of stimulants is to enhance neurotransmitter transmission via:
- Inhibition of neurotransmitter pre‐synaptic reuptake (DA & NE)
- Increase neurotransmitter release (amphetamines only)
- Amphetamines greater impact on dopamine synthesis, storage/release, and reuptake
- Methylphenidate’s main focus of activity is on inhibition of dopamine reuptake
TQ What are the Amphetamine salts* drugs for ADHD?
- Adderall (IR/XR): *Amphetamine (2 different salt forms) and *Dextroamphetamine (2 different salt forms)
- Dextroamphetamine: Dexedrine/Dextrostat
- Methamphetamine: Desoxyn
TQ What are the Methylphenidate drugs for ADHD?
- Ritalin (IR/SR/LA)
- Concerta
- Methylin
- Metadate (IR/ER/CD)
- **Quillivant XR (oral suspension)
- **Daytrana (patch)
- Dexmethylphenidate (Focalin (IR/XR))
What is Lisdexamfetamine a pro-drug of?
dextroamphetamine (vyvanse)
less risk of drug abuse because no initial high
TQ The onset of activity for stimulants is what?
Less than 24 hours
works immediately! versus non-stimulant…3 days before the school year and the kid is focused
TQ Are stimulants controlled substances?
Yes (1 month supply only, no refills, no samples)
Adderall is made of 2 amphetamine salts and comes in an IR and ER forms. What proportion of the long acting product is immediate release versus long acting release?
XR = 50% IR beads and 50% XR beads
XR Duration = 8‐12 hours (shorter for IR form) for most indiv
T/F: Dexedrine/dextroamphetamine doesn’t last as long as other agents
True
TQ: Vyvanse (lisdexamfetamine; pro‐drug of _______________)
Long acting!
dextroamphetamine
Longest DOA for all methylphenidate derivatives
Concerta (d,l‐methylphenidate)
10-12 hours
What separates concerta from other agents?
-methylphenidate (not amph.)
-not 50%/50% ratio b/c different delivery system: “Biphasic” release property (OROS)
• Phase 1: 22% IR
• Phase 2: 78% ER
Ritalin (d,l‐methylphenidate)
SR and LA DOA and ratio of IR to LA
- SR DOA = 4‐8 hours (shorter for IR form)
- LA DOA = 8‐10 hours
- LA = 50% IR beads and 50% LA bead
TQ!!
- Only extended‐release oral solution available (liquid)
- Lowest IR highest ER ratio
- Distributed as a powder requiring reconstitution prior to dispensing…comes in liquid
- No need to refrigerate, yet do need to shake well
Quillivant XR (d‐methylphenidate)
20% immediate‐release and 80% extended‐release methylphenidate formulation
Metadate (IR/ER/CD) (d,l‐methylphenidate)
ER and CD DOA, and ratio
- ER DOA = 6‐8 hours (shorter for IR form)
- CD DOA = 8‐10 hours
- CD = 30% IR beads and 70% CD beads
TQ Which stimulant drug is the patch?
Daytrana (patch) (d,l methylphenidate)
- Onset of activity within 2 hours (1‐2 hours)!!
- good for kids in the morning before school
- benefit: removable, not re-applicable, easy application
Focalin (dexmethylphenidate)
IR DOA, ER DOA, and ratio
Focalin (dexmethylphenidate)
- IR DOA = 4‐6 hours hours
- XR DOA = 10‐12 hours hours
- XR = 50% IR beads and 50% XR beads
MOA of non-stimulant agents for ADHD?
Main effect of non‐stimulants is to enhance neurotransmitter transmission via:
- Inhibition of neurotransmitter pre‐synaptic reuptake (only NE) (atomoxetine)…Also has down‐stream impact on DA system due to overlap
- Activation of centrally‐located (CNS) alpha‐2 adrenergic receptors (guanfacine/clonidine)…Post‐synaptic alpha‐2 inhibition in prefrontal areas
TQ What is the onset of activity for non-stimulant agents?
2-4 weeks! or longer… (much slower than stimulants)
Which pt groups is non-stimulant agents for ADHD good for?
- Useful for patients intolerant of stimulant effects or parents resistant to stimulant class
- Non‐scheduled, refills without visit, samples
Atomoxetine (straterra) and Guanfacine (Intuniv) are both….
long acting and once a day
18-24 hours
Clonidine is available in IR and ER but IR has to be taken up to 3x a day. ER duration of action is…
18-24 hours
What are some SE of stimulants?
- Decreased appetite (Weight loss)
- Insomnia
- Headache/Stomach‐ache
- Irritability/Aggression: (Tics, Psychoses)
- Elevated BP/HR
- Sudden cardiac death (rare): Cardiac structural abnormalities
What are some SE of non-stimulants?
- Decreased appetite (Weight loss)
- Insomnia (atomoxetine)
- Sedation/Somnolence (guanfacine/clonidine)
- Headache/Stomach‐ache
- Dizziness
- Suicidal ideation (rare; atomoxetine)
- Liver injury (rare; atomoxetine)
- Hypotension (guanfacine/clonidine)
T/F: Can be in remission in psychiatry
True!
- ___-_______: 25-50% reduction in symptoms
- Remission: Symptom-free or near symptom-free
- Recovery: sustained remission for at least 8 wks w/o worsening symptoms
- Relapse: return of symptoms 6 mo after response (depressive breakthrough)
Non-response
Response
T/F: Antipsychotics can be used to treat depression
True!
T/F: Antidepressants can be used to treat other issues, such as anxiety, PTSD, panic disorder, OCD, etc
True!
What are the SNRI’s used as antidepressants? (5)
Serotonin-Norepi Reuptake Inhibitors
- TCAs
- Desvenlafaxine
- Duloxetine
- Venlafaxine
-Amoxapine (SNRI + DRA)
What are the SSRI’s used as antidepressants? (7)
Serotonin-Selective Reuptake inhibitors
- Citalopram
- Escitalopram
- Fluoxetine
- Paroxetine
- Sertraline
- Vilazodone
- Vortioxetine
What is the NDRI used as an antidepressant? (1)
Noradrenergic-Dopamine Reuptake Inhibitors
Bupropion
What are the SARA’s used as antidepressants? (3)
Serotonin-Adrenergic Receptor Antagonists
- Mirtazapine (+H1 blockade)
- Nefazodone
- Trazodone
What are the MAOI’s used as antidepressants? (3)
Monoamine Oxidase Inhibitors
- Phenelzine
- Selegiline
- Tranylcypromine
What is the MOA of TCAs?
-inhibit the reuptake of NE and serotonin (5HT)
TQ: What are the 3 key side effects of TCAs?
- Cardiovascular (alpha): orthostatic hypotension
- Anticholinergic (muscarinic): dry mouth, constip
- CNS (histamine): **sedation
What are some additional SE’s of TCAs?
- Weight gain
- Sexual dys
- SIADH
- Altered glucose metab
TQ What are the 3 things you see with TCA overdose?
“Quinidine-like” effects (Na channel blockers)
- Coma
- Cardiotoxicity (conduction abnormalities)
- Convulsions
What is the MOA of SSRIs?
-Selectively inhibit the reuptake of serotonin eventually resulting in down-regulation of post-synaptic receptors
(differences are kinetic and indication)
What are some SE of SSRI’s?
- sexual dys
- GI: N/V/D/C
- CNS: sedation
- weight gain
What is the most serious SE of SSRI’s?
Serotonin syndrome