Test 2 Flashcards
all antidepressants have a potential for
lowering the threshold for seizure activity, especially when alcohol is being consumed
patients consuming this drug should avoid foods high in levels of tyramine…why?
Monoamine oxidase inhibitors…MAOis essential for the adequate breakdown of tyramine
what has been reported as a consequence of dietary intake of tyramine in patients taking MAOIs
hypertensive emergencies and fatal accelerated hypertension
chief side effects of Tricyclic antidepressants
anti-cholinergic signs and symptoms such as dry mouth, constipation, urinary hesitancy, orthostatic hypotension, and sedation
drug where high toxicity is usually due to prolongation of QT interval, leading to arrhythmias
Tricyclic antidepressants
class of Amitriptyline/ Elavil
TCA
ind. of Amitriptyline/ Elavil
major depression, bipolar disorder, migraine and tension headaches, chronic pain
MOA of Amitriptyline/ Elavil
CNS modulation of both serotonin and norepinephrine, increasing levels of each of these neurotransmitters
side effects of Amitriptyline/ Elavil
Dizziness and marked drowsiness. Anticholinergic effects such as dry mouth, constipation, urinary hesitancy and blurred vision. Stopping treatment abruptly cause withdrawal-like symptoms i.e. nausea, headache, dizziness, lethargy, and flu-like symptoms. This is referred to as discontinuation syndrome.
class of Trazodone/ Desyrel
Tetracyclic
ind. of Trazodone/ Desyrel
major depressive disorder, anxiety, panic disorder and insomnia
MOA of Trazodone/ Desyrel
Serotonin reuptake inhibitor and partial antagonist. Decreased serotonin reuptake at presynaptic cleft allows for increased serotonin levels in the synapse and increased serotonin made available at post-synaptic receptor sites.
side effects of Trazodone/ Desyrel
Sedation, orthostatic hypotension, fatigue, possible cardiac dysrhythmias, possible mania in patients with bipolar disorder. Increased risk of suicide.
most commonly prescribed category of antidepressant drugs
Selective serotonin reuptake inhibitors (SSRIs)
class of Fluoxetine/ Prozac
SSRI
ind. of Fluoxetine/ Prozac
major depressive disorder, OCD, bulimia and panic disorder
MOA of Fluoxetine/ Prozac
decreased serotonin reuptake at presynaptic cleft allows for increased serotonin levels in the synapse and increased serotonin made available at post-synaptic receptor sites
side effects of Fluoxetine/ Prozac
Side effects as noted along with potential for serotonin syndrome with symptoms of fever, agitation, diarrhea and elevated blood pressure. Sexual dysfunction is a very common side-effect with all SSRIs. Common sexual side-effects include lack of interest in sex, impotency and anorgasmia (inability to reach orgasm).
what drug category may interfere and reduce the efficiency of SSRIs and compound risk of GI bleeds caused by SSRI use
NSAIDs
drug used for major depressive disorder, general anxiety disorder, painful peripheral neuropathy and fibromyalgia
Duloxetine/ Cymbalta
Antidepressant you would give to a patient who also has insomnia
tricyclic antidepressants, tetracyclic antidepressants
“depressing” side effect of SSRIs
weight gain
class of Bupropion/ Wellbutrin
norepinephrine and dopamine reuptake inhibitors (NDRI) and nicotine receptor antagonist
ind. of Bupropion/ Wellbutrin
Major depression, bipolar disorder and attention deficit disorder. Aid in smoking cessation is another indication for Bupropion, although it is marketed under the brand name Zyban when it is used as for that purpose.
MOA of Bupropion/ Wellbutrin
Blockade of norepinephrine and dopamine reuptake increases the available pool of these amines in the synaptic cleft.
side effects of Bupropion/ Wellbutrin
Headache, insomnia, dry mouth, tremors, restlessness, agitation, anxiety, sweating and dizziness.
all antidepressants are being looked at for potential of an increase in
suicidal behavior
antidepressant indicated for smoking cessation
Bupropion/Wellbutrin
depression may be associated with deficiency in this vitamin
folate
active form of folic acid
Levomefolic acid aka methyltetrahydrofolate aka 5-MTHF
nutriceutical adjunct therapy for depression
Levomefolic acid/ Deplin
adding ___ to anxiolytics and sedatives makes the sedative effect more powerful
alcohol
in general anxiolytics have this effect
sedation
are receptor sites for barbituates and benzodiazepines in the same place?
No, appear to be adjacent but not in the same location as the GABA sites on cell membrane of neurons in CNS.
block GABA can result in
seizures
at higher doses barbiturates will result in
coma and death
do barbiturates have analgesic properties
no
ultra-short acting barbiturates
Thiopental/Pentothal
short acting barbiturates
Pentobarbital/Nembutal
Intermediate-acting barbiturates
Butalbital/Fiorinal
Long-acting barbiturates
Phenobarbital/Luminal
reasons why barbiturates have largely been replaced
drug tolerance, psychological and physical dependence, severe withdrawal symptoms (can be fatal), potential for coma and respiratory failure esp when alcohol consumed
how do benzodiazepines work
Benzodiazepines act by binding to specific, high affinity sites on the cell membrane of neurons in the CNS which are adjacent to but separate from the gamma-aminobutyric acid (GABA) receptor sites.
short-acting benzodiazepines are generally used for
patients with sleep onset insomnia (difficulty falling asleep)
short-acting benzodiazepine utilized for sedation and anxiety prior to such procedures as upper and lower G.I. endoscopy as well as prior to general anesthesia and in critical care settings.
Midazolam/Versed…also for acute management of aggressive, violent or delirious patients
benzodiazepine with longer duration
Diazepam/Valium
class of Diazepam/ Valium
benzodiazepine
ind. of
Diazepam/ Valium
Anxiolytic, sedative, muscle relaxant and seizure control
MOA of
Diazepam/ Valium
Binds to benzodiazepine receptors in the C.N.S. to enhance GABA activity
side effects of
Diazepam/ Valium
Drowsiness, impaired mentation, tolerance and addiction. Rebound insomnia may occur after drug discontinuation. Withdrawal can be severe, similar to that of barbiturates, especially when patient has been on chronic therapy.
class of Eszopiclone/ Lunesta
Benzodiazepine-like hypnotic
ind. of Eszopiclone/ Lunesta
Treatment of insomnia
MOA of Eszopiclone/ Lunesta
Potentiation of GABA effect on chloride ion channels by binding to a specific receptor site not involved with the binding of benzodiazepines.
side effects of Eszopiclone/ Lunesta
Impaired mentation prior to sedation. Eszopiclone is reported as having minimal drowsiness upon awakening and minimal change in mentation relative to all other benzodizepines. As with almost every medication, the full side effect profile may not be fully appreciated until that drug has been in use for at least five years or more.
melatonin agonist
Remelteon/Rozerem
MOA of Remelteon/Rozerem
melatonin receptor agonist with high binding affinity at the melatonin MT1 and MT2 receptors
most common symptoms of benzodiazepine overdose
CNS depression and signs of intoxication with impaired balance, ataxia and slurred speech.
class/MOA of Flumazenil/ Romazicon
benzodiazepine receptor antagonist that can rapidly reverse effects of benzodiazepines
effectiveness of Flumazenil/ Romazicon
Flumazenil is very effective at reversing the CNS depression associated with benzodiazepines but is less effective at reversing respiratory depression.
main MOA of neuroleptic drugs
blockade of dopamine receptors in the brain
For neuroleptic drugs, five dopamine receptors have been identified and the chief antipsychotic effects of the neuroleptics appears related to dopamine blockade at the
D2 receptors
what pathway has been linked to psychotic experiences w/ neuroleptic drugs
Mesolimbic pathway…Excess release of dopamine in the mesolimbic pathway has been linked to psychotic experiences and it is the blockade of dopamine receptors in this pathway that is thought to control psychotic experiences.
Adverse effects commonly observed with the use of neuroleptics include:
Tremors/ Parkinsonian effects, Tardive dyskinesia, Postural hypotension, Blurred vision, dry mouth, constipation and urinary retention, Sexual dysfunction, Increased prolactin release, Drowsiness
Chronic treatment w/ neuroleptic agents may lead to
Parkinsonian-like symptoms such as uncoordinated muscular movement, dystonia (abnormal muscle tone), “pill rolling”, limb rigidity and shuffling gait along with extrapyramidal signs such as akinesia (inability to initiate movement), akathisia (inability to remain motionless), and tardive dyskinesia (facial grimacing and inappropriate posturing of the tongue, neck, trunk and limbs).
Define Tardive dyskinesia
Dyskinesia refers to an involuntary movement. Facial grimacing and involuntary movements of limbs are examples of dyskinesias.
The effect of these drugs can be tardive, meaning the dyskinesia continues on or first appears after the drugs are no longer being taken.
addition side effect of neuroleptic drugs that occurs rarely
neuroleptic malignant syndrome.
neuroleptic malignant syndrome is characterized by
catatonia, fluctuating blood pressure, dysarthria and fever
neuroleptic malignant syndrome may be fatal if what doesn’t happen
This syndrome may be fatal if the antipsychotic drug is not immediately discontinued and the patient receives treatment with a dopamine agonist such as Bromocriptine.
Random effect of neuroleptic drugs
Most of the neuroleptic drugs have anti-emetic effects that are mediated by blocking D2 dopaminergic receptors in the chemoreceptor trigger zone (CTZ) of the medulla.
Several neuroleptics are useful in the treatment of the severe nausea that occurs as result of cancer chemotherapy.
class of Chlorpromazine/ Thorazine
Typical neuroleptic
ind. of Chlorpromazine/ Thorazine
psychosis, mania, schizophrenia as well as nausea and vomiting and intractable hiccoughs.
MOA of Chlorpromazine/ Thorazine
Chiefly D2 dopaminergic receptor site blockade. Also alpha-adrenergic blockade and H1 blockade (anti-histamine effects).
side effects of Chlorpromazine/ Thorazine
significant side effects include onset of Parkinsonian symptoms and extrapyramidal signs such as tardive dyskinesia. Increased release of prolactin commonly occurs as a result of dopamine blockade. Increased prolactin can result in galactorrhea and amenorrhea in women and infertility in both men and women.
Drug with increased release of prolactin commonly occurs as a result of dopamine blockade. Increased prolactin can result in galactorrhea and amenorrhea in women and infertility in both men and women.
Chlorpromazine/ Thorazine
class of Prochlorperazine/ Compazine
Typical neuroleptic
ind. of Prochlorperazine/ Compazine
Psychosis as well as vertigo and nausea and vomiting, particularly when associated with migraine headaches.
MOA of Prochlorperazine/ Compazine
Primarily H1-histamine receptor antagonist as well as alpha-adrenergic receptor antagonist and D2 dopaminergic receptor antagonist.
side effects of Prochlorperazine/ Compazine
Significant drowsiness, dry mouth, constipation and urinary retention. Lowers seizure threshold. Extrapyramidal side effects generally seen only when Prochlorperazine is given at high doses over long periods of time.
class of Haloperidol/ Haldol
Typical neuroleptic
ind. of Haloperidol/ Haldol
Psychosis, Tourette’s syndrome, Huntington’s disease, acute agitated behavior.
MOA of Haloperidol/ Haldol
Chiefly D2 dopaminergic receptor site blockade.
side effects of Haloperidol/ Haldol
Chiefly Parkinsonian-like symptoms and EXTRAPYRAMIDAL effects, which may be very dramatic. Tremors very common. Less blockade of the muscarinic and the alpha-adrenergic receptors compared to other neuroleptic agents such as Chlorpromazine. The potentially fatal NEUROLEPTIC MALIGNANT SYNDROME (NMS) is a significant possible side effect