Pharm Ch 12- 15
REM sleep
a stage of sleep characterized by rapid eye movements (REM) and dreaming
Consists of CNS stimulation and autonomic changes that are predominantly sympathomimetic in nature.
Somatic Phase
Tardive dyskinesia (TD)
drug-induced involuntary movements of the lips, jaw, tongue & extremities
A condition characterized by muscular rigidity, tremors, and disturbances of movement.
parkinsonism
The drug that possesses anesthetic properties and that acts by blocking glutamate receptors is
phencyclidine
Phenothiazines
Chlorpromazine (Thorazine) Fluphenazine (Prolixin) Thioridazine (Mellaril) Trifluoperazine (Stelazin
MAOIs
monoamine oxidase inhibitors, antidepressants drugs that inhibit MAO
Bipolar mood disorder
mood disorder where episodes of mania and depression occur alternately
Dependency
requirement of repeated drug consumption in order to prevent onset of withdrawal symptoms
Hashish
resin from the marijuana plant that contains higher levels of THC
Thioxanthenes
Thiothixene (Navane)
Flumazenil (Romazicon) is used to reverse the depressant effects of
alprazolam
Psychomotor stimulant
amphetamine or related drug that increases mental and physical activity
The pharmacologic effects of TCAs include
A.alpha-adrenergic blockade B. antihistaminic C. anticholinergic D. sedation E. ALL OF THESE
Alcohol has pharmacological effects on which body systems?
A.central nervous system B. gastrointestinal system C. renal system D. vascular system E. ALL OF THESE
What are the adverse effects of the selective serotonin reuptake inhibitors
All the SSRIs gastrointestinal disturbances involve nausea, diarrhea, dry mouth, and anorexia. The most common symptoms of overdosage include confusion, fever, nervousness, tremor agitation, restlessness, and other signs of CNS excitation; seizures also have been reported. Sudden discontinuation of SSRI treatment has been associated with a discontinuation syndrome. Symptoms include dizziness, nausea, insomnia, and anxiety.
atypical antipsychotics
Aripiprazole (Abilify) Clozapine (Clozaril) Iloperidone (Fanapt) Olanzapine (Zyprexa) Quetiapine (Seroquel) Risperidone(Risperdal) Asenapine (Saphris) Ziprasidone (Geodon)
Explain the meaning of automatism.
Automatism is a drug-induced confusion that can cause increased drug consumption.
Caller A says he has no particular reason to feel down, but he's feeling really depressed anyway. He says he gets down-and-out a lot, but it doesn't usually get quite this bad. He wonders if there's any kind of treatment or drug for how he feels.
Caller A appears to have major depressive disorder (MDD) and may need both drug treatment and psychotherapy to cope effectively with the problem.
Caller B says she's usually a happy-go-lucky sort of person, but she's been feeling depressed since her mother died last month. She thinks she should be over the worst of her grief by now and wonders if she should get counseling.
Caller B appears to have EXOGENOUS depression, for which the support of friends and family may be sufficient to alleviate the symptoms.
Adverse effects of MAO
Common adverse effects include dry mouth, urinary retention, constipation, blurred vision, hypotension, weight gain, and sexual dysfunction
Describe a few of the more serious neurological adverse effects of the phenothiazine drugs. (LO 13.2)
Dystonia, akathisia, and Parkinsonism are neurological conditions caused by excessive dosage of phenothiazine drugs. These conditions are characterized by movement disorders such as muscle spasms, restlessness, rigidity, and tremors. Tardive dyskinesia is a condition involving involuntary movements of the lips, jaw, tongue, and extremities. It usually occurs after long-term antipsychotic drug use when drug treatment is stopped. The symptoms can be suppressed by reinstituting the drug or by increasing the dose of the antipsychotic drug.
Hallucinogenic effect of LSD relived long after the use of LSD.
Flashback
How does GABA normally function?
GABA is a neurotransmitter in the CNS that normally decreases neuronal excitability and produces varying degrees of CNS depression.
What is GABA an abbreviation for?
GABA is the abbreviation for gamma-aminobutyric acid.
Patient A has been brought to the emergency room (ER) exhibiting extremely agitated and manic behavior.
Haldol
Patient D just presented at the ER with tonic-clonic epileptic convulsions in progress.
Haldol
Tardive dyskinesia
Is a more serious condition that may develop after long-term antipsychotic therapy. This condition involves INVOLUNTARY movements of the lips, jaw, tongue, and extremities. The symptoms of tardive dyskinesia often appear when antipsychotic drug treatment is stopped. The symptoms can be suppressed by reinstituting the drug or by increasing the dose of the antipsychotic drug. However, the condition of tardive dyskinesia continues to progress and will be worse when the drug is stopped.
List the common pharmacological effects produced by marijuana.
Marijuana produces conjunctival reddening and increases in heart rate. After one marijuana cigarette, the user usually experiences feelings of euphoria. With moderate intoxication, there may be drowsiness, lapses of attention, and impairment of short-term memory. At high levels of intoxication, reflexes are slowed, muscle coordination decreases, and the ability to concentrate become more difficult.
Tricyclic Drugs ( Patient instruction)
Monitor vital signs when drugs are administered parenterally with particular attention to blood pressure and heart rate. Explain to patient the common side effects due to anti- cholinergic, alpha-blocking, and antihistaminic actions: dry mouth, constipation, low blood pressure, drowsiness. Instruct patient to report increased pulse rate, excessive difficulties with urination or defecation, excessive CNS stimulation (tremors, restlessness, seizures) Remember that these drugs may be contraindicated in patients with glaucoma and prostatic hypertrophy, and that the ELDERLY are more sensitive to anticholinergic drugs. Instruct patient not to take other drugs unless this is checked with the physician or pharmacist.
What neurotransmitters are deficient in mental depression?
Norepinephrine and serotonin are the neurotransmitters that are deficient in mental depression
Define the term Parkinsonism
Parkinsonism is a disease of drug-induced condition characterized by muscular rigidity, tremors, and disturbances of movement.
What pharmacological properties do the phenothiazines possess, and how do these properties relate to clinical use and adverse effects?
Phenothiazines possess the following pharmacological properties: .Antipsychotic effect due to the blockage of dopamine; this also explains their use as antiemetics. Anticholinergic effect, which decreases the activity of the parasympathetic nervous system and causes adverse effects such as dry mouth and constipation. Antihistaminic effect due to the blocking of histamine; this is useful in allergic reactions and can also cause sedation. Alpha-adrenergic-blocking effect, which lowers blood pressure.
is the main classes of antipsychotic drugs and give an example of each.
Phenothiazines: chlorpromazine (Thorazine). Butyrophenones: haloperidol (Haldol). Thioxanthenes: thiothixene (Navane).
Differentiate between REM sleep and NREM sleep.
REM sleep is characterized by rapid eye movement. NREM is characterized by nonrapid eye movement.
Robyn's physician has just prescribed Nardil for severe depression. What foods does Robyn need to avoid and why?
Robyn needs to avoid wine, beer, herring, and certain cheeses. These contain tyramine, which may produce massive releases of norepinephrine that could result in a hypertensive crisis or cerebral stroke.
Venlafaxine (Effexor) is classified as
SNRI
The serotonin syndrome is mainly associated with overdosage of
SSRI Selective serotonin reuptake inhibitors
What are the main pharmacological differences between the secondary and tertiary amine antidepressants
Secondary amines mainly increase brain levels of norepinephrine more than serotonin, while the tertiary amines mainly increase brain levels of serotonin more than norepinephrine. Tertiary amines also cause greater sedation.
Chapter 12
Sedative- Hypnotic Drugs & Alcohol
List the different stages of sleep and the characteristics of each.
Stage 1 NREM: relaxed and drowsy Stage 2 NREM: asleep but easily awakened; occupies about 50 percent of total sleep time Stages 3 and 4 NREM: deep stages of sleep that occupy about 20 to 25 percent of total sleep time REM: characterized by rapid eye movements, increased autonomic nervous system activity, and dreaming occupies about 20 to 25 percent of total sleep time
SELECTIVE SEROTONIN REUPTAKE INHIBITORS SSRIs
The SSRIs are a group of drugs that have a very selective action to block the reuptake of serotonin (5HT) back into the serotonergic nerve endings. This action treatment of most anxiety disorders such as posttraumatic stress disorder (PTSD) and obsessive-compulsive disorder (OCD)
Which antidepressant drug classes are considered to be the preferred therapy for DEPRESSION.
The SSRIs are currently considered the preferred drugs for major depression.
Briefly describe the psychotomimetic syndrome.
The psychotomimetic syndrome consists of three phases. During the initial somatic phase, CNS stimulation and autonomic effects occur. This is followed by the sensory phase, during which sensory distortions and pseudohallucinations are experienced. The psychic phase signals a maximum drug effect. Psychotic episodes, disruption of thought processes, depersonalization, and true hallucinations may be experienced.
Explain the mechanism of action of zolpidem and zaleplon.
These drugs bind selectively to a subunit of the benzodiazepine receptor to increase the inhibitory effects of GABA.
Describe the development of tolerance to LSD. What does the term cross-tolerance refer to?
Tolerance to LSD develops rapidly, usually within a few doses of continuous use, but there's no development of physical dependency. Cross-tolerance refers to tolerance between LSD and other hallucinogens, so the effects of one hallucinogen are reduced when taken after another hallucinogen.
You receive a phone call at the doctor's office from Mr. Smith, who has a prescription for Antabuse. He complains that he feels terrible and has been vomiting. He claims to have just developed a chest cold and has taken a spoonful of Vicks cough syrup. Mr. Smith doesn't think the vomiting has anything to do with the cold. What do you think?
Vicks cough medicine and many other liquid cold medicines contain alcohol. Mr. Smith is experiencing a typical disulfiram reaction to alcohol.
Patient C has suffered severe anxiety ever since being diagnosed with a terminal illness.
Xanax
A condition causing individuals to have continuous body movement
akathisia
A young man with a history of occasional drug abuse is in the doctor's office complaining of difficulty sleeping. The physician is writing a prescription for a hypnotic with no refills. Which hypnotic agent might be the best choice for this patient?
Zolpidem (Ambien), which is not associated with development of drug dependence or withdrawal reactions, would be the best choice for this individual, who is prone to abusing drugs.
Hallucinogenic drug
a drug or plant substance that produces psychotomimetic effects and sensory distortions
Depression
a mental state characterized by depressed mood, w/ feelings or frustration & hopelessness
LSD
a powerful hallucinogenic drug; also known as acid (lysergic acid diethylamide)
Zolpidem
binds to the benzodiazepine-1 (BZD1) receptor
The main action of phenothiazines in the treatment of schizophrenia is
blockage of D 2 receptors more than 5HT2A receptors
Extrapyramidal symptoms (EPS) are caused mainly by
blockage of dopamine receptors
he antianxiety effect of buspirone (BuSpar) is associated with
blockage of serotonin receptors
Dystonic reactions
characterized by muscle spasms, twitching, facial grimacing, and torticollis (wryneck).
Designer drug
chemically altered form of an approved drug that produces similar effects and that is sold illegally
Benzodiazepine
class of drugs used to treat anxiety & sleep disorders
The atypical drug associated with causing agranulocytosis and decreased WBCs is
clozapine
Mechaism of action of benzodiazepines
decrease the excitability and the functional activity of specific areas of the brain and spinal cord.
Because of this, larger and larger doses of a drug are necessary to prevent withdrawal.
dependency
Monoamine oxidase (MAO)
enzyme that inactivates norepinephrine and serotonin
Patient B appeared at the clinic suffering from a possible overdose of lithium. She appeared drowsy and complained of dizziness and ringing in her ears. What should be done to help rid her body of the excess lithium
force fluids and increase the intake of sodium to help rid the patient's body of excess lithium.
GABA
gamma-aminobutyric acid; an inhibitory neurotransmitter in the CNS
Second major type of depression
is referred to as major depressive disorder (MDD). MDD is frequently more serious and usually requires both psychotherapy and drug treatment. This type of depression originates from within the individual and may not be associated with easily recognized causes.
Flashback
phenomenon occurring long after the use of LSD in which the hallucinogenic effects are relived in some type of memory flash
List the adverse effects and drug interactions that may occur with the antianxiety drugs.
rowsiness, confusion, ataxia, minor GI disturbances, and rashes are common adverse effects. Menstrual irregularities, agranulocytosis, and changes in liver function occur less frequently but are of greater concern. Antianxiety drugs increase the effects of all other CNS depressants, such as alcohol and barbiturates. In addition, the microsomal drug cimetidine inhibits the metabolism of the antianxiety drugs and prolongs and intensifies their effects.
A major form of psychosis.
schizophrenia
SSRIs
selective serotonin reuptake inhibitors, a class of antidepressant drugs
drugs that can increase the level of norepinephrine or serotonin in the brain are useful in the treatment of mental depression
they are referred to as antidepressants, or mood elevators.
Neuroleptic Malignant Syndrome (NMS)
toxic syndrome associated with the use of antipsychotic drugs
Which drug requires a dietary restriction for foods containing tyramine?
tranylcypromine
TCAs
tricyclic antidepressants, a class of antidepressant drugs
The adverse effects of lithium include
vomiting ?
Psychosis
A form of mental illness that produces bizarre behavior & deterioration of the personality
Select the additional effects of phenothiazine drugs
A. antiemetic B. anticholinergic C. antihistaminic D. alpha-adrenergic blockade E. ALL OF THESE
Flurazepam
A. is classified as long-acting B. forms active metabolites C. may cause next-day residual effects .D. increases chloride ion influx E. ALL OF THESE
The adverse effects of barbiturates include
A. slurred speech B. ataxia C. irritability D. automatism E. ALL OF THESE
clinical uses of bupropion (Wellbutrin) include
A.) treatment of depression B. treatment of bipolar disorder C. cessation of smoking D. treatment of obesity E. ALL OF THESE
Select the statement(s) that are true concerning the use of marijuana.
A.active ingredient referred to as THC B. believed to bind to a specific receptor in the brain C. frequent use associated with development of drug tolerance D. psychic effects involve release of dopamine E. ALL STATEMENTS ARE TRUE
Disadvantages to the use of barbiturate hypnotics include
A.development of drug tolerance B. risk of drug dependency C. disruption of normal stages of sleep D. suppression of REM sleep E.ALL OF THESE STATEMENTS
intravenous administration and abuse of psychomotor stimulants, such as methamphetamine, are associated with the following:
A.increased sympathomimetic actions B. development of drug tolerance C. behavioral and psychotomimetic effects D. activation of mesolimbic dopamine E. ALL OF THESE
adverse effects of TCAs include
A.liver toxicity B. cardiac arrhythmias C. convulsions D. postural hypotension E. ALL OF THESE
What are the signs of PCP intoxication?
A.muscular rigidity B. catatonia C. convulsions D. nystagmus E. ALL OF THESE
What is the difference between akathisia and dystonia?
Akathisia is a continuous body movement, while dystonia is the twitching or spasms of the muscles.
List some of the effects that alcohol produces on the different body systems
Alcohol produces depression of the CNS, which can cause sedation, hypnosis, and coma. Alcohol dilates peripheral blood vessels, and this may contribute to rapid heat loss in cold weather. In the gastrointestinal tract, increased secretion of gastric juices can cause increased appetite, gastritis, and ulceration. In the urinary system, there is usually increased formation of urine.
Short acting
Alprazolam (Xanax) Lorazepam (Ativan) Oxazepam (Serax) Temazepam (Restoril) Triazolam (Halcion)
What mechanism of action is common to both amphetamines and cocaine?
Amphetamines and cocaine increase the levels of norepinephrine and dopamine within the brain. These increased levels affect CNS activity and behavior.
Patient B complains of a rash, nausea, drowsiness, confusion, and poor coordination (ataxia)
Antianxiety
Explain the terms antipsychotic and antianxiety.
Antianxiety drugs are used to treat anxiety, where as antipsychotic drugs are used to treat schizophrenia and other psychotic disorders.
Phenothiazines
Anticholinergic effects, CNS depression
Chapter 14
Antidepressant Psychomotor Stimulants and Lithium
Chapter 13
Antipsychotic and Anti Anxiety
The most common emotion
Anxiety
Differentiate between barbiturates and nonbarbiturates.
Barbiturates are CNS depressant drugs possessing the barbituric acid ring structure. Nonbarbiturates are hypnotic drugs that do not possess the barbituric acid ring structure.
How do barbiturates alter the normal sleep cycle?
Barbiturates usually increase stage 2 NREM but decrease stages 3 and 4 NREM and suppress REM sleep.
Explain the mechanism of action of benzodiazepine hypnotics. What is the main site of action to produce this effect
Benzodiazepines bind to their drug receptor sites (BZD receptors) that are in close relationship to the GABA receptors. The combined action of GABA and the benzodiazepine drug increases the frequency of chloride ion channel opening, resulting in hyper polarization of the nerve membrane and reduced neuronal activity. In the reticular activating system, this depression produces sedation or hypnosis.
The correct statement concerning the use of hypnotic drugs is
Benzodiazepines increase chloride channel opening
How do benzodiazepine hypnotics alter the sleep cycle?
Benzodiazepines increase stage 2 NREM and usually decrease stage 4 NREM. They do not suppress REM sleep as the barbiturates do.
Buspirone (BuSpar)
Buspirone is a drug that is used primarily as an antianxiety drug. It does NOT demonstrate useful sedative, hypnotic, anticonvulsant, or skeletal muscle relaxant actions like the benzodiazepines. The usual dosage for anxiety is 5-10 mg administered 2-3 times daily.
Barbiturate
CNS depressant drug possessing the barbituric acid ring structure
Pharmacologically active substance found in the marijuana plant.
Cannabinoid
Long acting
Chlordiazepoxide (Librium) Clonazepam (Klonopin) Clorazepate (Tranxene) Diazepam (Valium) Flurazepam (Dalmane
What adverse effects are associated with the chronic use of marijuana
Chronic abuse of marijuana has been associated with precancerous changes in the respiratory epithelium, bronchitis, hoarseness and cough. Marijuana alters the plasms levels resulting in decreased sperm count among males and menstrual irregularities among females. Reduced birth weights have been recorded in women who smoked marijuana during pregnancy.
Explain how disulfiram (Antabuse) is used in the treatment of alcoholism, and describe the disulfiram reaction.
Disulfiram is a drug used to treat CHRONIC alcoholism. It interferes with the metabolism of alcohol. Alcohol is metabolized through a series of steps to acetaldehyde, which is then converted into acetyl coenzyme A (CoA). 1st. alcohol 2nd. acetaldehyde 3rd acetyl coenzyme A isulfiram causes the accumulation of acetaldehyde, which produces a very disagreeable reaction characterized by nausea, vomiting, headache, and hypotension. Individuals who want to stop drinking must voluntarily take disulfiram and not ingest alcohol. The ingestion of any alcohol will trigger the disulfiram reaction. In this manner, disulfiram acts as a deterrent to alcohol consumption.
What adverse effects are caused by barbiturates?
Drowsiness, dry mouth, lethargy, incoordination, and impaired judgment are the adverse effects caused by barbiturates. Elderly patients are particularly sensitive to loss of memory. Overdosage or intoxication can result in coma, cardiovascular and CNS depression, and death.
Neuroleptic Malignant Syndrome (BAD GUY)
Drug allergy is an infrequent but potentially dan-gerous complication of phenothiazine therapy. Allergic symptoms usually involve skin rashes and photosensi tivity, blood disorders, and liver toxicity (cholestatic jaundice). Other miscellaneous adverse effects include skin pigmentation, ocular deposits (lens and cornea), and various endocrine disturbances.
Caller B says he thinks he needs to get medical help with his cocaine problem. He's been using cocaine for months now, and he needs larger and larger doses just to keep from feeling sick and strung out. He can't imagine going without the cocaine, but he knows things can't go on this way, either.
Drug dependency
Caller A says he needs help quitting cocaine. His main reason for wanting to quit is that he can no longer afford to buy the amount of cocaine he needs to get high. He says it seems that he uses more every day, and he still doesn't get as high as he did when he first started using the drug.
Drug tolerance
Anticholinergics, antihistamines
Dry mouth, constipation, urinary retention, blurred vision
What is the importance of enzyme induction caused by barbiturate drugs?
Enzyme induction increases the amount of drug metabolizing enzymes in the liver, increasing metabolism of barbiturates and other drugs. This reduces the duration of drug effect.
Describe the areas of the brain and neurotransmitters that are involved in psychosis.
Excessive activity of certain brain neurotransmitters, especially dopamine and serotonin, in the cerebral cortex and limbic system appear to be responsible for the psychotic behavior.
List the two main types of depression and define each.
Exogenous—or reactive, depression is caused by external factors or life events (death or unemployment). Major depressive disorder (MDD)—depression that arises from within an individual and requires psychotherapy and drug treatment.
SSRI (Selective Serotonin Reuptake Inhibitor) Drugs ( Patient instruction)
Explain to patient the common side effects: headache, nerv- ousness, insomnia, nausea, loss of appetite, diarrhea. Instruct patient to report excessive GI and CNS stimulation (agitation, seizures). Instruct patient not to suddenly stop taking these drugs on his or her own.
What is the main difference between flurazepam (Dalmane) and triazolam (Halcion)?
Flurazepam is classified as a long-acting benzodi- azepine. It forms several active metabolites, some of which have long half-lives. For this reason, the sedative and antianxiety effects of flurazepam are usually evi- dent the day following a hypnotic dose. This prolonged action can be useful in anxious patients when sedating drug effects are desired during the following day. On the other hand, daytime sedation and drowsiness may inter- fere with employment or other activities. Temazepam is an intermediate-acting hypnotic that does not form any important active metabolites. The duration of hypnotic action is 8 to 10 hours, and there are usually little or no drug effects evident the following day. One preparation of temazepam is marketed in a hard gelatin capsule that gives a delayed onset of action. This drug dosage form should be taken 1 to 2 hours before sleep is desired. Also Flurazepam is a long-acting hypnotic that forms several active metabolites . Triazolam is a short-acting hypnotic that does not form active metabolites.
An inhibitory neurotransmitter in the CNS.
GABA
Butyrophenones
Haloperidol (Haldol)
Patient A presents with LSD toxicity, experiencing anxiety, paranoia, and real hallucinations (as opposed to pseudohallucinations, which the individual knows are not real)
I should reassure the patient that everything will be all right and use benzodiazepine antianxiety agents or barbiturates for sedation.
List the pharmacological effects produced by LSD. What is synesthesia?
In addition to the psychotomimetic effects, there are piloerection, pupillary dilation, increased reflexes, tachycardia, and increased blood pressure. Synesthesia refers to the confusion of hearing and visual perception, in which "sounds are seen" and "sights are heard."
Barbiturate and benzodiazepine hypnotics both
Increase NREM stage 2 sleep
Amphetamines
Increased CNS Stimulation
MAO inhibitors
Increased CNS stimulation, hyperpyrexia, seizures
SSRIs, SNRIs
Increased CNS stimulation, serotonin syndrome
Alcohol
Increased Sedation
Barbiturates
Increased metabolism of tricyclics (decreased effectiveness), increased sedation
Anticonvulsants
Increased possibility of seizures
A serious and potentially fatal condition, neuroleptic malignant syndrome (NMS)
Is also associated with the use of antipsychotic drugs. This syndrome is characterized by hyperthermia, muscular rigidity, catatonia (patient appears frozen in position), and autonomic nervous system instability. Treatment is immediately required and involves stopping antipsychotic drug administration and symptomatic treatment of the symptoms.
Janet has just been prescribed lithium for her manic states. What should be included in her medication counseling?
It may take one to two weeks of treatment before noticing any difference. Common side effects include nausea and tremors, but they should diminish with continued treatment. Also, she will have increased thirst and frequency of urination. It is important to have adequate fluid and sodium intake. She should immediately report any excessive nausea, vomiting, CNS stimulation, dizziness, abnormal muscle movements, low blood pressure, or ringing in the ears. It is important to have her blood levels checked as required by her physician.
June is a 36-year-old alcoholic. She has unsuccessfully attempted to quit drinking multiple times. Her physician has decided to initiate disulfiram therapy. What should June be told before taking this medication?
June should be told NOT to take disulfiram for at least 12 hours after drinking alcohol. Avoid alcohol in any form: beverages, vinegars, some sauces (wine or others containing alcohol), many liquid medications containing alcohol, and topical products such as lotions, colognes, and so on. Always read product labels or ask your pharmacist before choosing a liquid medication. The disulfiram-alcohol reaction can have serious effects on the heart and respiratory systems. Use caution while driving or performing tasks requiring alertness.
Patient F is in alcohol withdrawal in the local Veterans Administration (VA) hospital detoxification unit.
Librium
List the major sites of action of the benzodiazepines and the clinical effects produced at each site.
Limbic system: antianxiety effect. Reticular formation: sedation and hypnosis. Cerebral cortex: anticonvulsant effect. Spinal cord: skeletal muscle relaxant.
Explain the mechanism of action and major adverse effects of lithium.
Lithium interferes with nerve conduction. As a result, there is a decrease in the excitability of nerve tissue. Most patients experience some nausea or tremors. With overdose, vomiting, diarrhea, drowsiness, loss of equilibrium, ringing in the ears, and frequent urination are common . At toxic levels, the heart and kidneys may be damaged, leading to the development of cardiac arrhythmias or nephritis. Lithium occasionally produces disturbances of the thyroid gland. In acute overdoses, muscle fasciculations, convulsions, and circulatory collapse leading to death are possible.
Lithium Mechanism of Action
Lithium is an element similar in chemical properties to sodium. The body utilizes lithium as if it were sodium. Both lithium (Li+) and sodium (Na+) exist in body flu- ids as charged particles, or ions. However, whereas Na+ is normally required for conduction of nerve impulse
How do the MAO inhibitors increase the levels of norepinephrine and serotonin in the brain?
MAO inhibitors suppress the enzyme MAO, which normally breaks down norepinephrine and serotonin into metabolites that are then excreted by the kidneys. Drugs that inhibit, or block, MAO are called appropriately MAO inhibitors (MAOIs). By inhibiting MAO, these drugs decrease the amounts of norepinephrine and serotonin that are destroyed. Consequently, the amounts of these neurotransmitters increase after MAO inhibition.
Differentiate between mania and depression.
Mania is a mental state of excitement, hyperactivity, and excessive elevation of mood. Depression is characterized by depressed mood, with feelings of frustration and hopelessness.
What do the terms marijuana, cannabinoid, tetrahydrocannabinol (THC), and hashish refer to?
Marijuana refers to the plant Cannabis sativa, which is dried, chopped, and smoked like tobacco. Cannabinoids are specific, pharmacologically active chemicals found in the marijuana plant. Tetrahydrocannabinol (THC) is the major active cannabinoid found in the plant. Hashish is the resin that is extracted from the flower pod of the plant, which contains high percentages of THC.
Patient B presents with cocaine intoxication, following a prolonged binge on the drug. She has had a mild seizure and shows psychotic behavior, hyperthermia, and exhaustion.
Mark should give diazepam to control seizures and for sedation and should give an antipsychotic drug, such as chlorpromazine or haloperidol, to antagonize the psychoactive effects of the cocaine.
Describe the pharmacological effects produced by phencyclidine (PCP)
Phencyclidine (PCP), at low doses, produces CNS stimulation, euphoria, and sympathetic stimulation, With increasing dosage, thought processes become disoriented and speech is slurred. In acute toxicity, individuals exhibit anxiety, agitation, hallucinations, and occasionally violent behavior. This may progress to convulsions, coma, and death.
Patient A has been experiencing dry mouth, constipation, and EPS.
Phenothiazine
Patient C presents with high fever and muscular rigidity and appears unable to move.
Phenothiazine
What is the mechanism of action of the phenothiazine antipsychotic drugs?
Phenothiazines block the D2 receptors to a greater degree than the 5HT2A receptors, which decreases psychotic behaviors.
MAO inhibitors (patient instruction)
Provide patient with a list of tyramine-containing foods and over-the-counter drugs that must be avoided while taking MAO inhibitors. Explain to patient the common side effects: dizziness, low blood pressure, dry mouth, constipation and other GI dis- turbances, blurred vision, impotency in males. Instruct patient to report excessive dizziness or feelings of faintness, difficulty with urination, CNS stimulation or agita- tion, yellowing of skin (liver jaundice).
A "bad trip."
Psychic Phase
Characteristic of a maximum drug effect.
Psychic Phase
Produces disruption of thought, depersonalization, hallucinations, and psychotic episodes.
Psychic Phase
What are some of the clinical uses of psychomotor stimulants?
Psychomotor stimulants are used to treat narcolepsy (uncontrolled tendency to fall asleep) and hyperkinesis in children.
Chapter 15
Psychotomimetic Drugs of Abuse
Adverse effects of SSRI
SSRIs have little action to block cholinergic, adrenergic, or histamine receptors. All the SSRIs listed cause GI disturbances including nausea, diarrhea, dry mouth, and anorexia.
Mary's husband John occasionally takes Dalmane when he has trouble sleeping. He came home late last night after a banquet and a few too many drinks; he took a Dalmane capsule because he wasn't tired and he had to get up early for an important meeting. At 8 a.m., John was sound asleep and Mary couldn't seem to wake him up. What do you think may have happened?
Sedative-hypnotic drugs and alcohol together can cause a synergistic effect that produces a much greater degree of CNS depression than expected. These drugs should not be used together.
What is the major indication for the use of sedatives and hypnotics?
Sedatives are used to decrease the desire for physical activity. Hypnotics are used to induce sleep in individuals experiencing insomnia.
What is the difference between a sedative and a hypnotic?
Sedatives are used to produce mental relaxation and to reduce the desire for physical activity. (Fast to Slow) Hypnotic drugs are used to induce and maintain sleep. (Slow keep Slow)
Produces the effects desired by the user
Sensory Phase
produces sensory distortions and pseudohallucinations
Sensory Phase
Occurs right after absorption of the hallucinogen.
Somatic Phase
A distortion of sensory perception that occurs with the use of LSD
Synesthesia
Drug-induced involuntary movements of the lips, jaw, tongue, and extremities.
Tardive dyskinesia
An 82-year-old woman has been taking a sleeping pill for the past 6 months to help her fall asleep. What can you tell her about the use of hypnotic drugs
Tell her that regular use of hypnotic drugs causes tolerance and that she may have developed a psychological dependence to the sleeping pill. She should use the hypnotic only on the nights that she really has difficulty sleeping.
Explain the Monoamine Theory of Mental Depression
The Monoamine Theory of Mental Depression states that mental depression is caused by low brain levels of norepinephrine and serotonin (monoamines).
What adverse effects are associated with the tricyclic antidepressants?
The anticholinergic effects of tricyclics may cause dry mouth, constipation, urinary retention, and rapid heartbeat. Alpha-blocking actions may cause postural hypotension, blurred vision, and drowsiness. In addition, they may cause CNS stimulation, seizures, and cardiac arrhythmias.
Which stage of the sleep cycle is most important for physical rest and restoration?
The beginning stage 1 NREM
What are the advantages of the benzodiazepines over the barbiturate hypnotics?
The benzodiazepines generally do NOT interfere with REM sleep. They produce less tolerance and therefore are effective for a few weeks longer than are the barbiturates when taken on a nightly basis. They also do not induce microsomal metabolizing enzymes significantly. When abused, the benzodiazepines generally cause less physical dependence than do barbiturates. These factors, along with a lower incidence of adverse effects, give the benzodiazepines a number of advantages over the barbi- turates for both sedation and hypnosis Also Benzodiazepines have a low incidence of adverse effects. In addition, they produce less tolerance, little if any enzyme induction, and no REM suppression.
A coworker confides in you that working full time, going to school, and taking care of a child and husband are exhausting, so occasionally she takes amphetamines to help her get through it all. She doesn't feel it is a problem because she only uses them when she needs to. What do you do?
The instructor should make certain that the discussion includes ethics, laws, risks, safety, to whom and how to report situations, and methods for reducing stress.
You are over at a coworker's house and she brings out some marijuana. What do you do?
The instructor should make certain that the discussion includes ethics, laws, risks, safety, to whom and how to report situations, and methods for reducing stress.
Mechanism of Action of tricyclics
The main action of the tricyclics and related antidepressant drugs is to block the reuptake of norepinephrine and serotonin back into the neuronal nerve ending
Antipsychotic effects
The main effects of the phenothiazines are to reduce the bizarre behavior, hallucinations, and irrational thought disorders of psychosis without significantly depressing other intellectual functions. The antipsychotic effects usually require several weeks to fully develop. With drug therapy, patients usually demonstrate decreased interest in the surroundings and less behavioral activa- tion. However, routine daily activities can be carried out, and patients are able to communicate more rationally. Although the psychosis is not cured, it is possible to control it adequately with the proper medication. In addition, patients are usually more amenable to psycho- therapy and other treatment measures.
Adverse effects of butyrophenones
They are similar to those of the phenothiazines. However, the butyro- phenones,haloperidol in particular, produce the highest blocking D2 receptors more than 5HT2A receptors. The most important thioxanthene is thiothixene (Navane).
How do the selective serotonin reuptake inhibitors produce their antidepressant effect?
The selective serotonin reuptake inhibitors (SSRI) are a group of drugs that have a very selective action to block the reuptake of serotonin (5HT) back into the serotonergic nerve endings. This action increases the concentration of 5HT in the synaptic cleft, which results in increased stimulation of serotonin receptors. The increase in 5HT activity in the limbic and cerebral cortical areas of the brain is believed to contribute to the antidepressant effect.
LSD and similar hallucinogens produce a sequence of dose-related effects that have been divided into three phases
The somatic phase occurs initially after absorption, and it consists of CNS stimula- tion and autonomic changes that are pre- dominantly sympathomimetic in nature. The sensory phase is characterized by sen- sory distortions and pseudohallucinations (the user knows the hallucinations are not real), which are the effects desired by the drug user. The psychic phase signals a maximum drug effect. Disruption of thought processes, depersonalization, and true hallucinations (the user believes the hallucinations are real) and psychotic episodes may occur. Experiencing this phase would be considered a "bad trip."
Adverse effects of Toxic effects
The tricyclics possess significant anticholinergic activ- ity, which is responsible for many of the adverse effects. Anticholinergic effects include dry mouth, constipation, urinary retention, and rapid heartbeat. Alpha-blocking actions may cause postural hypotension, blurred vision, and drowsiness. Like the MAO inhibitors, the tricyclics stimulate the CNS and may produce restlessness, tremors, convulsions, or mania.
John is a healthy 29-year-old who has recently had trouble sleeping. His physician has prescribed Dalmane 30 mg. While talking with John, he tells you how happy he is to know that he is going to get a good night's sleep. He works in a high-energy office and was concerned that he might be in danger of losing his job due to his recent lack of energy. Do you think this should be brought to the physician's attention? Why? Would you expect the drug therapy to change? If so, which medication do you think it might be changed to? (LO 12.4)
This should be brought to the attention of his physician because Dalmane is a long-acting sedative and may interfere with employment. Expect therapy to change. A possibility would be Restoril, as there are usually little or no drug effects evident the following day.
Patient B is in intensive care following an episode of bizarre delusions and hallucinations
Thorazine
Characterize the development of tolerance and dependency with the psychomotor stimulants. (LO 15.2)
Tolerance develops fairly rapidly with the psychomotor stimulants, especially when large amounts are ingested. Although some physical dependency develops, the major withdrawal effects are psychological in nature.
Explain the mechanism of action of the tricyclic antidepressants.
Tricyclic antidepressants block the reuptake of norepinephrine and serotonin back into the neuronal nerve endings of the brain. As a result there is an accumulation of these neurotransmitters in the synaptic clefts. This action increases the level of neuronal activity of norepinephrine and serotonin and alleviates the symptoms and dysfunction of depression.
What is the usual treatment for LSD and other hallucinogenic drug intoxication?
Usually, individuals are placed in a quiet, nonthreatening room and given reassurance that everything will be all right. Benzodiazepines or other sedatives are used when individuals are excessively agitated or hyperactive.
Patient E has open-heart surgery scheduled for tomorrow and is experiencing presurgical anxiety
Valium
Describe the clinical uses of diazepam (Valium).
Valium is used to reduce excessive nervousness and anxiety, to relax patients before surgery, to treat alcohol withdrawal, and to stop convulsive seizures, itching, muscle spasms, and spasticity.
Julie has never had trouble sleeping until the past month. She is going through a stressful period and is having difficulty falling asleep. Once asleep, she usually sleeps through the night. Her care provider had prescribed Ambien 5 mg in a quantity to last 2 weeks. Do you feel this is appropriate? Why?
Yes, this is appropriate therapy. Ambien has a short half-life, does not interfere with the normal sleep cycle, and is not associated with withdrawal reactions.
Anxiety
a state of anxiousness & hyper-emotionalism that occurs with uncertainty, stress & fearful situations
What are the main areas at which benzodiazepines exert their effects?
a.)limbic system B. cerebral cortex C. reticular formation D. spinal cord E. ALL OF THESE
Tetrahydrocannabinol (THC)
active ingredient of the marijuana plant
Lithium
an element similar to sodium that is used in the treatment of mania & bipolar mood disorder
Drugs used to calm and reduce excessive nervousness
anti anxiety drugs
Drugs used to treat schizophrenia.
antipsychotic drugs
tricyclic antidepressant drugs
are so named because of the characteristic triple-ring structure that they possess. Recently, some new antidepressants, which produce pharmacological effects similar to those of the tricyclics, have been introduced with two rings (bicyclics), four rings (tetracyclics), and others with quite different chemical structures (nontricyclics). The chemistry of these antidepressants is beyond the scope of this book.
Olanzapine is classified as a(n)
atypical antipsychotic
Increased triglycerides, weight gain, and diabetes are adverse effects associated with
atypical drugs
Akathisia
continuous body movement in which an individual is restless or constantly paces about.
Because of this, doses of one drug taken shortly after another drug produce decreased effects.
cross-tolerance
Exogenous, or reactive, depression
depression caused by external factors or life events
Major Depressive Disorder (MDD)
depression that arises from within an individual and requires psychotherapy and drug treatment
Parkinsonism
disease or drug-induced condition characterized by muscular rigidity, tremors, and disturbances of movement
Synesthesia
distortion of sensory perception; usually associated with the use of LSD
Psychotomimetic drug
drug or substance that can induce psychic and behavioral patterns characteristic of a psychosis
Because of this, one consumes larger and larger doses of a drug in order to get the desired effects.
drug tolerance
Cross tolerance
drug tolerance that develops between similarly acting drugs
Hypnotic
drug used to induce and maintain sleep
Sedative
drug used to produce mental relaxation and to reduce the desire for physical activity
Automatism
drug-induced confusion that can cause increased drug consumption
Antipsychotic drug
drugs used to treat schizophrenia and other psychotic conditions
Patient A has been diagnosed with major depressive disorder. He's been taking Elavil for several weeks, but it makes him excessively drowsy, so his medication is being changed to an MAO inhibitor. The patient also is taking a prescription decongestant for allergies. What should you note on the patient's chart regarding adverse effects and drug interactions?
excessive drowsiness is a common side effect of Elavil, which is a tricyclic antidepressant. Elavil can increase the CNS stimulation of MAO inhibitors and lead to fever and seizures. This effect can last for up to two weeks after discontinuation of Elavil. MAO inhibitors are potentiated by decongestants, so the decongestant should be withheld while the patient is taking the MAO inhibitor or else the MAO inhibitor dosage should be adjusted accordingly.
There are several different types of depression
exogenous, or reactive, depression
Fluoxetine is well absorbed after oral administration. It is metabolized in the liver into an active metabolite that has a half-life that ranges from several days to a week or more
he metabolites are primarily excreted in the urine. Fluoxetine also has been shown to be an inhibitor of the metabolism of other drugs such as anti- coagulants and benzodiazepines.
SSRI most common symptoms of overdoseage
include confusion, fever, tremor agitation, restlessness, and other signs of CNS excitation; seizures also have been reported. These symptoms are referred to as the "serotonin syndrome" and may lead to coma and death if not treated. Sudden discontinuation of SSRI treatment has been associated with a discontinuation syndrome. Symptoms include dizziness, nausea, insomnia, and anxiety. The dosage of SSRIs and related drugs should be gradually reduced over time when treatment is stopped.
Other CNS effect
include headache, nervousness, insomnia, and tremors. Weight gain, especially with parox- etine, has also been reported.
he main pharmacologic effect of the SSRIs is
increase levels of serotonin
The main pharmacologic effects of TCAs on neurotransmitter activity is
increase norepinephrine and serotonin only
Eszopiclone
increases total sleep time
MAO
inhibiting MAO, these drugs decrease the amounts of norepinephrine and serotonin that are destroyed. Consequently, the MAO inhibitors permit the levels of norepinephrine and serotonin in the brain to increase
A serious and potentially fatal condition, neuroleptic malignant syndrome (NMS).
is also associated with the use of antipsychotic drugs. This syndrome is characterized by hyperthermia, muscular rigidity, catatonia (patient appears frozen in position), and autonomic nervous system instability.
In some cases of depression, there are alternate periods of hyperexcitability and elation,
known as mania Individuals who experience these alternating cycles of depression and mania are classified as manic- depressive. Another term for this condition is bipolar mood disorder.
The site of action of diazepam (Valium) to relieve anxiety is the
limbic system
Sites of action
limbic system is involved with regulation of emotional and behavioral responses. Any emotional or anxiety-producing situation increases the activity of the limbic system
Schizophrenia
major form of psychosis; behavior is inappropriate
Triazolam
may cause early morning awakenings
Mania
mental state of excitement, hyperactivity & excessive elevation of mood
Which of these represents the drug that is not correctly matched with its drug classification?
methylphenidate—MAOI
Extrapyramidal syndrome (EPS)
movement disorders such as akathisia, dystonia, and parkinsonism caused by antipsychotic drug therapy
The sympathetic and behavioral actions of cocaine in the brain are due to increases in
norepinephrine and dopamine
Cannabinoid
pharmacologically active substance obtained from the marijuana plant
which phase of dose-related effects would include true hallucinations and be classified as a "bad LSD trip"?
psychic phase
LSD is associated with the following pharmacologic effect when taken repeatedly:
rapid development of drug tolerance
Dystonic reaction
reaction characterized by muscle spasms, twitching, facial grimacing, or torticollis
Nonbarbiturate
refers to sedative-hypnotic drugs that do not possess the barbituric acid structure, such as benzodiazepines and related drugs
Drug tolerance
requirement of larger doses to be consumed in order to obtain the desired effects
SNRIs
seratonin-norepinephrine reuptake inhibitors, a class of antidepressant drugs
Select the neurotransmitter receptor interaction that explains the mechanism of action of LSD and other hallucinogens
serotonin
NREM sleep
stages of sleep characterized by nonrapid eye movement (NREM)
Monoamine Theory of Mental Depression
theory that mental depression is caused by low brain levels of norepinephrine and serotonin (monoamines)
