(P2) Lab 8 Q&A Set 2 Flashcards
A 37-year-old man complained to his physician of persistent, intolerable pain in his left leg that started about 2 days earlier. He reported that he had tried several over-the-counter pain medications without success. One month earlier, the patient underwent the amputation of his left leg following an accident at work. Physical examination revealed that pain could be elicited by a no noxious stimulus applied to the region of amputation. The physician made a preliminary diagnosis and prescribed a drug for pain. Which of the following drugs would be appropriate for this patient?
Venlafaxine
Venlafaxine
Define
Antidepressant Medication of Serotinin-norepinephrine reuptake inhibitor class. (SNRI’s)
USE: to tx major depressive disorder, generalized anxiety disorder, panic disorder and Social Phobia
ALSO may be used for CHRONIC PAIN
Phenobarbital
define class:
BARBITURATES
Give four examples of barbiturates
and
their duration of action
- Phenobarbital* (Luminal)—long- acting/1–2 days.
- Pentobarbital* (Nembutal)—short- acting/2–8 hours.
- Amobarbital* (Amytal)—short-acting
- Thiopental* (Pentothal)—ultra–short-acting/10–20 minutes.
Phenobarbital
(Barbiturates)
MOA:
Like benzodiazepines, barbiturates increase the duration of GABA action on Cl– entry into the cell, which results in membrane hyperpolarization and a decrease in neuron excitability.
Barbiturates do not bind to benzodiazepine receptors.
phenobarbital
(Barbiturates)
What are the therapeutic indications
for
barbiturate administration?
Induction of anesthesia—thiopental Anticonvulsants—phenobarbital Anxiety—rarely
- Decrease the activity of Brain and NS
- Prevent and Treat Seizures
- also short term sedation
- anxiolytic- CNS depressant
BARBITURATES
Phenobarbital
ROA:
IV, PO, or IM
Phenobarbital
What are the pharmacokinetic properties of barbiturates?
They are metabolized in the liver and excreted in the urine.
Does barbiturate dependency occur?
Yes.
Abrupt cessation can lead to severe withdrawal symptoms (tremor, restlessness, nausea, seizures, and cardiac arrest).
For whom are
barbiturates contraindicated?
For patients who have acute intermittent porphyria, because they increase porphyrin synthesis
phenobarbital (Barbiturates)
What are the adverse effects of these drugs?
-Drowsiness and decreased motor control Induction of the P-450 system, which can
therefore decrease the effect of other
drugs metabolized by these enzymes
- Addiction
- In high doses, respiratory depression and coma
- Allergic reactions, especially in patients with asthma
What is acetaminophen
and
Clinical indications
also known as Tylenol
Acetaminophen is an over-the-counter antipyretic and analgesic medication that is routinely administered.
-Fever and mild-to-moderate pain
How does acetaminophen work
This drug acts by inhibiting cyclooxygenase and thus prostaglandin synthesis in the CNS.
It has much less of an effect on cyclooxygenase in peripheral tissues, which accounts for its weak anti- inflammatory effects.
What are antipsychotic drugs
Antipsychotics, also known as neuroleptics, are drugs used primarily to treat psychotic states such as schizophrenia, delusional disorder, and other hallucinatory states
Antipsychotics
MOA:
Antipsychotics block various receptors including cholinergic, adrenergic, serotoninergic, muscarinic, and histamine receptors.
However, their antipsychotic actions are primarily thought to be due to blocking of dopamine receptors in the central nervous system, particularly the D2 receptors in the mesocortical and mesolimbal systems of the brain.
Do antipsychotic agents differ in potency?
Yes—a drug’s potency parallels its affinity for D2 receptors.
Haloperidol and thiothixene
are high-potency drugs because they have high affinity for the D2
receptors, whereas chlorpromazine and thioridazine are low-potency drugs because they have low affinity for D2 receptors.
How are antipsychotics usually administered?
these drugs are given orally;
or
intramuscularly if the patient is noncompliant.
Describe the absorption and metabolism of the traditional antipsychotics.
They are variably absorbed orally but they pass into the brain easily and have a large volume of distribution. Metabolism occurs by the cytochrome P-450 system in the liver.
Antipsychotics
What is the onset of action?
Antipsychotics may not become effective for several weeks to months.
-sedation and other side effects can occur rapidly.
Can these drugs cure illnesses such as schizophrenia?
No!
Antipsychotics only reduce the symptoms of the illness; they cannot cure the illness.
Name 6 examples of
atypical antipsychotic drugs
- Clozapine (Clozaril)
- Risperidone (Risperdal)
- Olanzapine (Zyprexa)
- Aripiprazole (Abilify)
- Quetiapine (Seroquel)
- Ziprasidone (Geodon)
Why are these drugs considered “atypical”?
They are newer drugs and in addition to blocking dopamine receptors, atypical antipsychotics also produce significant therapeutic effects through the blockade of serotonin (5-HT2) receptors.
They are also rarely associated with extrapyramidal side effects.
Describe the actions of
clozapine
This agent is a dibenzodiazepine derivative.
It differs from traditional antipsychotics in its potent blockade of serotonin (5-HT2) receptors*, along *with
the usual dopamine blockade.
Clozapine
What is it used for?
Clozapine has been effective in treating cases of schizophrenia that are refractory to other neuroleptic drugs.
It is especially effective in treating the negative symptoms of schizophrenia (blunted emotion, withdrawal, reduced ability to form relationships)
Clozapine
SE :
causes fewer extrapyramidal side effects than traditional neuroleptics.
Clozapine does cause seizures and a very dangerous agranulocytosis in 1% to 2% of patients ( common board question).
Weekly blood tests are required for patients receiving clozapine therapy.
-weight gain can occur with extended treatment of most antipsychotics, it is especially prominent with clozapine. This can lead to hypertension and other diseases.
Diazepam
also known as:
and
Class of drugs:
Duration of action:
(Valium)
BENZODIAZEPINES
Long-Acting (1 to 3 days)
How do benzodiazepines work?
When benzodiazepines bind to specific receptors that are separate from but adjacent to the GABAA receptor, they potentiate the binding of GABA to its own receptor.
The binding of GABA to its own receptor results in increased chloride ion conductance, cell membrane hyperpolarization, and decreased initiation of action potentials.
NOTE: that benzodiazepines do not bind to GABA receptors—they bind adjacent to them
What is GABA?
GABA (γ-aminobutyric acid) is the major inhibitory neurotransmitter of the CNS.
What are the therapeutic indications for benzodiazepines?
These drugs are used clinically as muscle relaxants and in the treatment of the following:
- Anxiety disorders*
- Panic disorders*—alprazolam is the drug of choice.
- Status epilepticus*—diazepam is the drug of choice.
- Sleep disorders*—flurazepam or temazepam.
- Alcohol withdrawal*—diazepam is most commonly used.
Are benzodiazepines effective
for
controlling pain as well as anxiety?
No.
They have little analgesic effect.
What is their route of administration
PO, IV, or IM
Where are benzodiazepines metabolized?
They are metabolized in the liver and excreted in the urine.
Many of the benzodiazepines have active metabolites.
What types of symptoms may a patient taking benzodiazepines experience?
Drowsiness and confusion
—
the most common side effects Ataxia Dizziness
Respiratory depression and death if taken
with other CNS depressants such as ethanol
Diazepam
Class:
USE:
Benzodiazepines
anxiety , seizures, alcohol withdrawl, restless leg syndrome
Sedative, hypnotic, sleep inducing, muscle relaxant, minor trangualizer
A 41-year-old man recently diagnosed with major depressive disorder complained to his psychiatrist that he felt drowsy for most of the day. The patient had started a treatment with paroxetine 2 months earlier, but his depressive symptoms were minimally improved. One week ago, his psychiatrist decided to shift to another antidepressant and prescribed 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?
Amitriptyline
A 43-year-old man went to his physician complaining of difficulty in maintaining an erection during intercourse. Past history of the patient was significant for an episode of ventricular tachycardia 1 year earlier. He was recently diagnosed with major depressive disorder and started a drug treatment 2 weeks ago. Which of the following drugs most likely caused the symptom reported by the patient?
Fluoxetine
Phantom limb pain
Define :
Nerves in parts of your spinal cord and brain “rewire” when they lose signals from the missing arm or leg. As a result, they send pain signals, a typical response when your body senses something is wrong.
Dulotexine
Define;
medication used to treat major depressive disorder, generalized anxiety disorder, fibromyalgia, and neuropathic pain.
-It is taken by mouth-
Dulotexine:
SE:
Common side effects include dry mouth, nausea, feeling tired, dizziness, agitation, sexual problems, and increased sweating.
Severe side effects include an increased risk of suicide, serotonin syndrome, mania, and liver problems.
Antidepressant withdrawal syndrome may occur if stopped.
Duloxetine
Contraindications
1. Duloxetine and thioridazine* should *not be
co-administered.
- Monoamine oxidase inhibitors (MAOIs): concomitant use in patients taking MAOIs is contraindicated.
Duloxetine
MOA:
Duloxetine inhibits the reuptake of serotonin and increases dopamine (DA) specifically in the prefrontal cortex, where there are few DA reuptake pumps, via the inhibition of NE reuptake pumps (NET), which is believed to mediate reuptake of DA and NE.
Duloxetine has no significant affinity for dopaminergic, cholinergic, histaminergic, opioid, glutamate, and GABA reuptake transporters, however, and can therefore be considered to be a selective reuptake inhibitor at the 5-HT and NE transporters.
Amitriptyline
Quick review Define
primarily used to treat a number of mental illnesses:
major depressive disorder
anxiety disorders
less commonly attention deficit hyperactivity disorder
bipolar disorder.
-Tricyclic antidepressant (TCA) drug calssification and acts by blocking the reuptake of both Serotonin and Norepinephrine neurotransmitters
Trazodone
Quick review
define
antidepressant med.
used to tx: major depressive disorder, anxiety disorders and WITH other medications ALCOHOL DEPENDENCE
A 53-year-old woman with along history of depression was admitted to the hospital because of agitation, insomnia, and tremors. She had been taking fluoxetine, lorazepam, and mirtazapine for several months. The doses of fluoxetine and mirtazapine had just been increased. Physical examination showed a confused patient with hyperhidrosis, hyperlexia, and myoclonus but without focal neurologic deficits. Vital signs were blood pressure 105/60
mm Hg, heart rate 130 bpm, respirations 32/min,, body temperature 39.8°C. Qualitative plasma tests for alcohol, opioids, benzodiazepines, and tricyclic antidepressants were negative. An electrocardiogram indicated sinus tachycardia. A brain computed tomography scan was normal. Which of the following disorders most likely caused the patient’s signs and symptoms?
Serotonin Syndrome
A 48-year-old woman visited a psychiatrist because for the past 2 months she had been depressed and was not interested in any of her usual activities, nor did she find anything enjoyable. She was also worried and anxious and felt very sleepy nearly every day. Her medical history was significant for exertional angina for the past 5 years. The psychiatrist made a preliminary diagnosis of major depressive disorder and prescribed cognitive behavioral therapy and a drug treatment. Which of the following drugs would be appropriate for this patient?
Fluoxetine
A 34-year-old m an suffering from a major depressive disorder had started a therapy with paroxetine, but 1 month later his symptoms were minimally improved, and his psychia- trist decided to add a drug to the treatment. The prescribed drug has a complex molecular mechanism of action that in- cludes a blockade of presynaptic α2 receptors. Which of the
following drugs was most likely given?
Mirtazapine
A 61-year-old woman came to her psychiatrist’s office for a routine visit. She stated that the drug she was taking im- proved her depressed mood, but that she was still suffering from sadness and fatigue from time to time and from heavy drowsiness, nearly every day. The woman, recently diagnosed with major depressive disorder, had started fluoxetine 1 month earlier. After further questioning, the psychiatrist decided to add to the therapy a drug that is thought to act by decreasing reuptake of both norepinephrine and dopamine by brain neurons. Which of the following drugs was most likely prescribed?
Bupropion
A 36-year-old woman presented at an outpatient psychiatric clinic complaining of extreme lethargy and depressed mood more days than not, for the past 5 weeks. On interview she also reported an intense fear of being in confined spaces, and she carefully avoided elevators and traveling by airplane. Her psychiatric history indicated two similar episodes in the past, treated, respectively, with fluoxetine and venlafaxine, but with negligible results. After further questioning, a diagnosis of depression with atypical features was made. A drug was prescribed that acts by inactivating enzymes involved in neurotransmitter metabolism. Which of the following drugs was most likely prescribed?
Phenelzine
A 22-year-old man was sent by his physician to a psychiatrist because of the onset of a distressing and embarrassing behavior. For the previous 3 months, the man had being experiencing an irresistible urge to disinfect any object in his room and to wash his hands again and again. He was disturbed by the unreasonable amount of time spent on such activities, and he acknowledged that his behavior was totally inappropriate, but he felt he could not stop it. He denied any substance abuse or use of medications. The psychiatrist made a preliminary diagnosis and prescribed cognitive behavioral therapy and a drug treatment. Which of the following drugs would be most appropriate for this patient?
Fluoxetine
A 56-year-old man complained to his physician that he felt like he had the u. He was dizzy, shivering, very irritable, anxious,andnauseated.Themanwassu eringfromamajor depressive disorder and had taken paroxetine for 4 months, but 3 days ago he decided to stop the drug, as his depression had been in full remission for the past month. Medical his- tory of the patient was significant for hypertension, presently treated with losartan and hydrochlorothiazide. Which of the following disorders best explains the syndrome re- ported by the patient?
Selective serotonin reuptake inhibitor discontinuation syndrome
A 54-year-old man was admitted to the hospital because of generalized shaking, jerking movements of the limbs, twitching of the jaw, and clenching of the teeth. The patient had been suffering from gastrointestinal reflux disease for 2 years. Four months ago, he was diagnosed with an obsessive-compulsive disorder and started cognitive behavioral therapy and a pharmacological treatment. Three hours before admission, he took a tablet of metoclopramide given to him by a friend to decrease his heartburn. Which of the following drugs most likely interacted with metoclopramide, thus triggering the adverse effects reported by the patient?
Paroxetine
A 25-year-old woman was admitted to the emergency department because of sudden onset of chest pain, difficulty in breathing, dizziness, and nausea. She described feeling “as if my head is going off in space and I am outside my body.” She stated that she had been under extreme stress lately, working too much, and that a similar episode had occurred, “out of the blue,” 1 month ago. Physical examination and laboratory analyses revealed no abnormalities. A preliminary diagnosis was made, and an appropriate therapy was prescribed. Which of the following drugs would be appropriate for this patient?
Sertraline
A 17-year-old girl was admitted to an eating disorder clinic with a 3-month history of binge eating and vomiting and purging episodes occurring from twice per week to four times a day. After physical examination and lab tests, psychotherapy and a drug treatment were prescribed. Which of the following drugs would be appropriate for this patient?
Fluoxetine
A 38-year-old man complained to his physician that the drug he was taking was effective in relieving his anxiety but caused a disturbing adverse effect. The patient had been recently diagnosed with a social anxiety disorder and started treatment with venlafaxine 2 weeks ago. Which of the following adverse effects did the patient most likely experience?
Negligible orgasm during intercourse
A 54-year-old man was admitted to the hospital with severe lower abdominal discomfort and complete inability to urinate for the past 6 hours. The man reported that he needed to urinate 5 to 7 times during the previous night. Past history of the patient was significant for hypertension, insomnia, and chronic lower back pain, as well as for recently diagnosed depression. Present medications included lovastatin, losartan, hydrochlorothiazide, amitriptyline, and lorazepam. Which of the drugs most likely triggered the patient’s anuria?
Amitriptyline
A 67-year-old woman complained to her psychiatrist that the drug she was taking did not improve her depressed mood at all. Three months earlier, the woman had suffered a
myocardial infarction, and she had been suffering from a second-degree atrioventricular block since then. Eight days ago, she was diagnosed with a depressive disorder and started an appropriate treatment. The psychiatrist advised the patient to continue the treatment, explaining that the therapeutic effects of the prescribed drug usually take 2 to 3 weeks or more to become evident. Which of the following drugs was the patient most likely taking?
Paroxetine
