(P2) Practice Q's Set 1 Flashcards
A drug with pronounced
anticholinergic properties ?
Name:
Amitriptyline
Amitriptyline
Define:
Use:
Amitriptyline belongs to a class of drugs called tricyclic antidepressants
treat a number of mental illnesses:
include major depressive disorder
anxiety disorders
less commonly attention deficit hyperactivity disorder (ADHD) and bipolar disorder.
Other: include prevention of migraines, treatment of neuropathic pain such as fibromyalgia and postherpetic neuralgia, and less commonly insomnia
SE: signs of an allergic reaction to amitriptyline: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Amitriptyline
- SE:*
- mild/seriuous*
side effects: blurred vision
dry mouth,
low blood pressure on standing,
sleepiness,
constipation.
Serious side effects may include seizures, an increased risk of suicide in those less than 25 years of age, urinary retention, glaucoma, and a number of heart issues.
Amitriptyline
Contraindications:
- It should not be taken with MAO inhibitors or the medication cisapride.*
- Amitriptyline may cause problems if taken during pregnancy.*
- Use during breastfeeding appears to be relatively safe.*
Bupropion
- Define:*
- Use:*
Bupropion is an atypical antidepressant.
It acts as a norepinephrine–dopamine reuptake inhibitor (NDRI) and a nicotinic receptor antagonist
USE:
to treat major depressive disorder
and
to support smoking cessation.
It is an effective antidepressant on its own,
also
used as an add-on medication* in cases of *incomplete response to first-line SSRI antidepressants
- Bupropion*
- SE:*
side effects of bupropion include:
a dry mouth, difficulty sleeping, agitation, and headaches.
Serious side effects increased risk for epileptic seizures and suicide.
In comparison to some other antidepressants, bupropion may have a lower rate of sexual dysfunction* or *sleepiness* and *may result* in *weight loss.
bupropion
Contraindications:
should not be prescribed to individuals with epilepsy
or
other conditions that lower the seizure threshold: anorexia nervosa,
bulimia nervosa,
benzodiazepine abuse
or withdrawal alcohol abuse or withdrawal.
Avoid in individuals who are also taking monoamine oxidase inhibitors (MAOIs).
NOTE: When switching from MAOIs to bupropion, it is important to include a washout period of about two weeks between the medications
Citalopram
- Define:*
- Use:*
Is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class.
USE: used to treat major depressive disorder, obsessive compulsive disorder,
panic disorder,
social phobia.
- The antidepressant effects may take one to four weeks to occur.*
- It is taken by mouth*
Fluoxetine
- Also known as:*
- define:*
- Use:*
Prozac
an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class.
USE: for the treatment of major depressive disorder, obsessive–compulsive disorder (OCD), bulimia nervosa, panic disorder, and premenstrual dysphoric disorder.
- It may decrease the risk of suicide in those over the age of 65.*
- It has also been used to treat premature ejaculation.*
- Fluoxetine is taken by mouth.*
Citalopram
SE:
Common side effects :
nausea, trouble sleeping, sexual dysfunction, shakiness, feeling tired, and sweating
Serious side effects:
include an increased risk of suicide in those under the age of 25, serotonin syndrome, glaucoma, and QT prolongation.
- Citalopram*
- Contraindications:*
It should not be used in someone on a MAO inhibitor.
Antidepressant discontinuation syndrome may occur when stopped.
Citalopram should not be taken with St John’s wort, tryptophan, 5-HTP, MAOI’s as the resulting drug interaction could lead to serotonin syndrome.
(SSRIs) Citalopram, can increase the risk* of *bleeding, especially when coupled with aspirin, NSAIDs, warfarin, or other anticoagulants.
NOTE:citalopramwithomeprazolemay cause higher blood levels ofcitalopram.
- Fluoxetine*
- SE:*
- If stopped suddenly:*
Common side effects include indigestion, trouble sleeping, sexual dysfunction, loss of appetite, dry mouth, rash, and abnormal dreams
Serious side effects include serotonin syndrome, mania, seizures, an increased risk of suicidal behavior in people under 25 years old, and an increased risk of bleeding.
If stopped suddenly, a withdrawal syndrome* may occur with *anxiety, dizziness, and changes in sensation.
It is unclear if it is safe in pregnancy.
- Fluoxetine*
- Is it effective for Social anxiety disorder?*
ineffective for social anxiety disorder.
- Mirtazapine*
- Define:*
- Use:*
has antihistamine, α2-blocker, and antiserotonergic activity.
It is specifically a potent antagonist or inverse agonist of the α2A-, α2B-, and α2C-adrenergic receptors, the serotonin 5-HT2A, 5-HT2C, and the histamine H1receptor.
NOTE: Unlike many other antidepressants, it does not inhibitthe reuptake of serotonin, norepinephrine, dopamine, monoamine oxidase
USE: antidepressant of the atypical antidepressants class primarily used to treat depression.
-full effect may take more than four weeks to occur, with some benefit possibly as early as one to two weeks.
Often it is used in depression complicated by anxiety or trouble sleeping.
- Mirtazapine*
- SE:*
Common side effects
include increased weight,
- sleepiness*
- dizziness*
Serious side effects may include mania, l_ow white blood cell count_, and i_ncreased suicide among children_.
Withdrawal symptoms may occur with stopping
- Mirtazapine*
- Contraindications:*
not recommended together with an MAO inhibitor It -is unclear if use during pregnancy is safe
mirtazapine
- Indications:*
- What main enzymes are responsible for its metabolism and altered concentrations:*
Concurrent use with inhibitors* or *inducers of the cytochrome (CYP) P450 isoenzymes CYP1A2, CYP2D6, and/or CYP3A4 can result in altered concentrations of mirtazapine.
As examples: fluoxetine and paroxetine, inhibitors of these enzymes, are known to modestly increase mirtazapine levels, while carbamazepine, an inducer, considerably decreases them.
Liver impairment and moderate chronic kidney disease have been reported to decrease the oral clearance of mirtazapine by about 30%; severe kidney disease decreases it by 50%.
mirtazapine
As examples, fluoxetine and paroxetine, inhibitors of these enzymes, are known to modestly increase mirtazapine levels, while carbamazepine, an inducer, considerably decreases them.[4] Liver impairment and moderate chronic kidney disease have been reported to decrease the oral clearance of mirtazapine by about 30%; severe kidney disease decreases it by 50%.
- A nonselective monoamine oxidase*
- inhibitor :*
Phenelzine
phenelzine
- Define:*
- Use:*
is a non-selective and irreversible monoamine oxidase inhibitor (MAOI) of the hydrazine class
which is used as
an antidepressant and anxiolytic.
USE: major depressive disorder, dysthymia, bipolar depression (BD), panic disorder (PD), social anxiety disorder, bulimia, post-traumatic stress disorder (PTSD), and obsessive-compulsive disorder (OCD)
NOTE: Along with tranylcypromine and isocarboxazid, phenelzine is one of the few non-selective and irreversible MAO
phenelzine
Pharmacodynamics:
is a non-selective and irreversible inhibitor of (MAO).
It inhibits both of the respective isoforms of MAO, MAO-A and MAO-B
By inhibiting MAO, phenelzine prevents the breakdown of the monoamine neurotransmitters serotonin, melatonin, norepinephrine, epinephrine, and dopamine, as well as the trace amine neuromodulators such as phenethylamine, tyramine, octopamine, and tryptamine.
This leads to an increase in the extracellular concentrations of these neurochemicals and therefore an alteration in neurochemistry and neurotransmission.
phenelzine
Pharmacokinetics
administered orally in the form of phenelzine sulfate* and is *rapidly absorbed from the gastrointestinal tract.
Time to peak plasma concentration is 43 minutes
and
half-life is 11.6 hours.
phenelzine
SE:
Common side effects of phenelzine
include dizziness, blurry vision, dry mouth, headache, lethargy, sedation, somnolence, insomnia, anorexia, weight gain or loss, nausea and vomiting, diarrhea, constipation, urinary retention, mydriasis, muscle tremors, hyperthermia, sweating, hypertension or hypotension, orthostatic hypotension, paresthesia, hepatitis, and sexual dysfunction
phenelzine
Interactions:
The MAOIs have certain dietary restrictions* and *interactions.
Hypertensive crisis is generally a rare occurrence while taking MAOIs-may result from the overconsumption of tyramine-containing foods* *such as aged cheeses and cured meats
Anyone taking phenelzine should inform their dentist before proceeding with dental surgery, and surgeon in any other contexts.
Phenelzine has also been linked to vitamin B6 deficiency
An active metabolite of this drug has a half-life of about 10 days.
A. Amitriptyline
- B. Bupropion
- C.** Citalopram
D. Fluoxetine
E. Mirtazapine
Fluoxetine
This drug can prolong the electrocardiogram QT interval
A. Amitriptyline
B. Bupropion
C. Citalopram
- D. Fluoxetine*
- E. Mirtazapine*
Amitriptyline
A serotonin 5-HT2A
presynaptic receptor blocker :
A. Trazodone
B. Bupropion
C. Selegiline
D. Fluoxetine
E. Citalopram
Trazodone
What actions are anticholinergic Drugs
known for:
Drugs that block the action of a neurotransmitter called Acetylcholine.
This inhibits nerve impulses responsible for involuntary muscle movements and various bodily functions.
Can treat variety of conditions-overactive bladder to obstructive pulmonary disoreder
Define:
MAOI’s
Monoamine oxidase inhibitors are a class of drugs that inhibit the activity* of one or both *monoamine oxidase enzymes:
Monoamine oxidase A and B.
Known for Highly efficacious anti-depressants, as well as effective thereapeutic agents for
panic disorder and social disorder
Amitriptyline
- Type of drug called :*
- if given in low dose it can do what:*
- -it increases which Neurotransmitter:*
Tricyclic antidepressant
(tx: anxiety and depression)
Low doses: can reduce or stop pain
Increases: the amount of Serotonin
Provide 4 examples
of
Non-selective Monoamine Oxidae Inhibitor
- Isocarboxazid
- Phenelzine
- Selegiline
- Tranylcypromine
- A 43-year-old man recently diagnosed with major depressive disorder started a pharmacotherapy with an antidepressant drug.*
- Name the most common mechanism underlying the therapeutic effectiveness of long-term therapy with most antidepressants drugs*
C. Increased expression
of
brain-derived neurotrophic factor
A 55-year-old man suffering from severe depression was brought to the emergency department after an overdose of an unknown medication. Physical examination showed a lethargic patient with dilated pupils. Vital signs were blood pressure 95/55 mm Hg, heart rate 130 bpm, respirations 10/min. An electrocardiogram (ECG) showed tachycardia with wide QRS complex. Which of the following drugs most likely caused the patient’s signs and symptoms?
E. Amitriptyline
A 45-year-old woman complained of dizziness to the point of fainting upon standing. She also felt drowsy for most of the day. The patient had been admitted to a hospital psychiatric unit 2 weeks earlier because of her third episode of major de- pressive disorder. She had been receiving an antidepressant therapy for the past 10 days. Which of the following drugs most likely caused the patient’s symptoms
C. Amitriptyline
A 48-year-old man recently diagnosed with generalized anxiety disorder started an appropriate therapy with a drug that acts by increasing the availability of both norepinephrine and serotonin in the synaptic cleft of central nervous system neurons. Which of the following drugs was most likely prescribed?
C. Venlafaxine
A 33-year-old woman visited a psychiatrist for what she described as a very disturbing problem. The woman, who delivered a healthy boy 1 month earlier, was distraught by recurrent intrusive thoughts about stabbing her baby. After further questioning, the psychiatrist made a preliminary diagnosis and prescribed cognitive behavioral therapy and a pharmacotherapy. A drug with which of the following molecular mechanisms of action would be appropriate for this patient?
C. Inhibition of serotonin transporter
A 75-year-old woman recently diagnosed with pancreatic cancer was sent by her family physician to a psychiatrist because she complained of significant weight loss, forgetfulness, initial insomnia, and sadness. She also reported that she was discouraged, fearful, and very anxious and that sometimes she experienced sweating with a racing heart. The woman had been suffering from paroxysmal atrial tachycardia for 5 years. Considering the clinical picture and side effect pro les, which of the following would be an appropriate therapeutic regimen for addressing these complaints?
C. Paroxetine and zaleplon
A 54-year-old woman complained to her physician of dizziness and vertigo when standing up rapidly. She had a long history of recurrent major depressive disorder and had taken various antidepressant drugs over the past several years. Recently, her psychiatrist decided to prescribe imipramine. Which of the following receptors most likely mediated the adverse effects of the drug in this patient?
Alpha-1 adrenergic
A 25-year-old woman visited a psychiatrist because she felt very anxious when she had to eat or drink in public. She acknowledged that her ideas of being watched by others were irrational, but she could not get beyond them. She also realized that alcohol helped her cope with her anxiety, and she had started drinking two or three glasses of brandy every day. After further questioning, a preliminary diagnosis was made, and cognitive behavioral therapy was prescribed, together with a pharmacological treatment. Which of the following drugs would be appropriate for this patient?
Paroxetine
A 56-year-old woman with a long history of major depressive disorder was brought unconscious to the emergency department after her husband discovered she had taken several pills of amitriptyline in a suicide attempt. Which of the following symptoms did the patient most likely show?
Mydriasis
A 52-year-old woman complained to her physician that the drug she was taking caused diarrhea. The woman, recently diagnosed with social anxiety disorder, had started a therapy with paroxetine 2 week earlier. Which of the following molecular actions in the enteric nervous system most likely mediated the adverse effect of this drug?
Increased serotonergic activity
