Ch19 – Antiseizure
Drug classes: hydantoins, barbiturates, succinimide, benzodiazepines, iminostilbene, valproate
Patients should not operate heavy machinery when starting on antiseizure therapy because of
drowsiness side effect
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Hydantoins: inhibit sodium influx, stabilize cell membrane, reduces repetitive neuronal
firing, and limit seizures
o Side effects: gingival hyperplasia, bradycardia, tachycardia, ventricular
fibrillation, etc. (most important side effects)
o Do not use when pregnant, has teratogenic effects
o Highly protein bound drugs (don’t use with anticoagulants and aspirin, can cause
more free-drug availability and increase their activity)
o Phenytoin: reduces motor cortex activity and alters ion transport by acting on
sodium channels on neuronal cell membranes
 side effects: headache, confusion, tinnitus, insomnia, etc.
 adverse effects: agranulocytosis, leukopenia, thrombocytopenia, StevensJohnson syndrome, ventricular fibrillation, etc.
 therapeutic serum range level: 10 to 20 mcg/mL
Barbiturates: enhance GABA activity (GABA is an inhibitory neurotransmitter
o Phenobarbital
o Used for tonic-clonic, partial, myoclonic seizures, and status epilepticus
o Therapeutic serum range: 15 to 40 mcg/mL
o Side effects: sedation and tolerance – high doses can lead to respiratory
depression and coma
o Gradual discontinuation avoids seizure recurrence
o Can be taken with food to minimize GI irritation
Succinimides: decrease calcium influx
o Ethosuximide
o Used to treat absence seizures
o Therapeutic serum range: 40 to 100 mcg/mL
o Adverse effects: blood dyscrasias, psychosis, SLE, and suicidal ideation
Benzodiazepines
o Clonazepam: controls absence and myoclonic seizures
 Tolerance may occur after 6 months
o Clorazepate: treats partial seizures
o Diazepam: treats status epilepticus
 Used to treat medical emergency
 Administered through IV
 Short-term effect – other antiseizure drugs must be given during or
immediately after administration
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Iminostilbenes
o Carbamazepine: used for tonic-clonic and partial seizures; also used for
psychiatric disorders (bipolar disorder) and trigeminal neuralgia
 Therapeutic serum range: 4 to 12 mcg/mL
 Toxic interaction with grapefruit juice
 Monitor drug concentration closely
 Linked to fetal abnormalities – cardiac defects and cleft lip and palate
Valproic acid: used for tonic-clonic, absence, and partial seizures
o Therapeutic serum range: 50 to 100 mcg/mL
o Not safe for children under 2 years old
o Hepatoxicity is an adverse reaction – can occur in young children and patients
with liver disease
o May be taken with food to avoid GI distress
o Side effects: suicidal ideation, GI distress, thrombocytopenia, insomnia, etc.
CH15 - Adrenergic Agonists and Antagonists
Function of adrenergics: stimulate sympathetic nervous system; mimic neurotransmitters
norepinephrine and epinephrine
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Act on adrenergic receptor sites: heart, bronchi, GI tract, urinary bladder, ciliary eye
muscles
Effects of Alpha Agonist Receptors
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Alpha1 Receptors: increases force of heart contraction; vasoconstriction increases;
mydriasis; secretion of salivary glands decreases; urinary bladder relaxation and sphincter
contraction increases
o Too much stimulation can lead to decreased blood flow to the vital organs
Alpha2: inhibits release of norepinephrine; dilates blood vessels; produces hypotension;
decreases GI motility and tone
Effects of Beta Agonist Receptors
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Beta1: increases HR and force of contraction; increases renin secretion which increases
BP
Beta2: dilates bronchioles; promotes gastrointestinal and uterine relaxation; promotes
increase in blood glucose through glycogenolysis in the liver; increases blood flow in
skeletal muscles
Classifications of Sympathomimetics
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Direct-acting: Epinephrine, Norepinephrine
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o Directly stimulates adrenergic receptor
Indirect-acting: Amphetamine
o Stimulates the release of norepinephrine from terminal nerve endings
Mixed-acting: Ephedrine, Pseudoepinephrine
o Stimulates adrenergic receptor sites and stimulate the release of norepinephrine
from the terminal nerve endings
Direct Acting:
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Epinephrine
o Action: acts on alpha and beta receptors
o Uses: used to treat anaphylaxis, anaphylactic shock, bronchospasms, status
asthmaticus
o Rapid onset
o Side effects: cardiac dysrhythmias, palpitations, tachycardia, hypertension,
dizziness, headache, paresthesias, agitation, tremors, restlessness, hyperglycemia,
oliguria
o Drug interactions: don’t take with digoxin; beta blockers decrease onset
Central Acting Alpha Agonists
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Action: work by decreasing the release of norepinephrine from sympathetic nerves and
by decreasing peripheral adrenergic receptor activation
o Clonidine
 Selective alpha2 adrenergic agonist
 Used to treat hypertension
 Side effects: bradycardia, hypotension, sedation, and dry mouth
o Methyldopa
 Alpha-adrenergic agonist that acts within the CNS
 Alpha2 activation leads to vasodilation and decreased BP
 Side effects: drowsiness, headache, nasal congestion, nightmares, edema,
constipation, ejaculation dysfunction, elevated hepatic enzymes
Nursing actions: report tachycardia, palpitations, tremors, dizziness, hypertension,
increased BP, and dysrhythmias
Adrenergic Antagonists
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Block effects of adrenergic neurotransmitter by blocking alpha and beta receptor sits
Alpha-adrenergic antagonists can be selective or non-selective
o Selective block alpha1
o Nonselective block alpha2 and alpha1
o Not prescribed often due to side effects of orthostatic hypotension and reflex
tachycardia
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o Promote vasodilation, causing decrease in BP
Beta-adrenergic antagonists (beta blockers) decrease the heart rate and decrease BP
o Nonselective block both beta1 and beta2
 Use with caution in those with COPD or asthma – due to
bronchoconstriction side effect
o ISA – term used to describe the ability of certain beta blockers to bind with a beta
receptor to prevent strong agonists from binding to that receptor – produce
complete activation
 Nonselective: carvedilol, penbutolol, pindolol
 Selective (beta1 only): acebutolol (has ISA)
 Non-ISA beta blockers: metoprolol, atenolol
o Atenolol
 Action: selectively blocks beta1-adrenergric receptor sites, decreases
sympathetic outflow to the periphery, suppresses RAAS
 Used to treat hypertension, angina, prophylaxis, and treatment of acute
myocardial infarction
 Side effects: dizziness, drowsiness, headache, depression, fatigue, nausea,
diarrhea, erectile dysfunction
Drug interactions: decreased effects with NSAIDs, increased hypotension with other
antihypertensives
Nursing actions: monitor vitals – report significant decrease in blood pressure and heart
rate; assist with ambulation to avoid falls from orthostatic hypotension
Therapeutic effects may not occur for 2-3 weeks after initiation of therapy
CH17 – Stimulants
Drug categories: amphetamines, analeptics, anorexiants
Amphetamines and related anorexiants are greatly abused – long-term usage can lead to
dependence or tolerance; recommended for short-term use only (12 weeks)
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Amphetamines: stimulate the release of neurotransmitters norepinephrine and dopamine
from the bran and sympathetic nervous system
o Cause euphoria and increased alertness
 Also cause dry mouth, insomnia, restlessness, tremors, irritability, and
weight loss
o Methylphenidate and dexmethylphenidate
 used to increase a child’s attention span and cognitive performance
 decrease impulsiveness, hyperactivity and restlessness
 Methylphenidate is used to treat ADHD and narcolepsy
 Main drug for ADHD treatment
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Should be given upon waking up or 30-45 minutes before meals
o Should be monitoring child’s weight – drug can cause
weight loss
o Do not take with sympathomimetics or psychostimulants
because it increases stimulatory effects – irritability,
nervousness, tremors, and insomnia
o Modafinil
 Amphetamine-like stimulant that increases wakefulness in patients with
sleep disorders (narcolepsy)
Anorexiants
o Cause a stimulant effect of the hypothalamic and limbic regions of the brain to
suppress appetite
 Most do not have serious side effects
o Put an emphasis on using nonpharmacologic methods before moving onto
medications
 Nutritious diet, exercise, and behavior modifications
o Contraindicated: hypertension, hyperthyroidism, glaucoma, and within 14 days of
MAOI therapy
 Caution in those with DM, seizures, Tourette’s, and bipolar disorder
o Side effects: euphoria, restlessness, insomnia, tachycardia, hypertension, and
erectile dysfunction
Analeptics (Caffeine)
o Affect the brain stem and the spinal cord but also affect the cerebral cortex
o Primary use is to stimulate respiration, mental alertness, neonatal apnea
o Side effects: headache, withdrawal, palpitations, tachycardia, insomnia, GI
irritation, urinary frequency
CH18 – Depressants
Consider nonpharmacological methods first before moving on to medication
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Waking up at the same time every day, little/no daytime naps, avoid caffeinated drinks,
avoid nicotine 6 hours before bedtime, avoid eating heavy meals before bedtime, take
warm bath, listen to soothing music, decrease loud noise
Drug classes: Sedative-Hypnotics & Anesthetics
Sedative-hypnotics
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Used to treat sleep disorders
Barbiturates, benzodiazepines, nonbenzodiazepines, melatonin agonists
o Barbiturates not as commonly prescribed due to mental and physical dependency
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Can be short or intermediate acting
Barbiturates
o Long, intermediate, short, and ultrashort acting
 Phenobarbital – long acting; used to control seizures in epilepsy
 Butabarbital – intermediate acting; maintain long periods of sleep; vital
signs should be closely monitored
 Secobarbital – short acting; used for procedure sedation; vital signs should
be monitored
o Restricted to short term use (2 weeks or less)
 Due to side effects – drug tolerance
o Drug interactions: alcohol, opioids, and other sedatives can further depress the
CNS; hepatoxicity
Benzodiazepines
o Used to treat insomnia and reduce anxiety
o Action: increase the action of inhibitory neurotransmitter GABA to the GABA
receptors; neuron excitability is reduced
o Alprazolam, estazolam, lorazepam, temazepam, triazolam
 Lorazepam and diazepam are also used for anxiety relief
o Avoid alcohol and antidepressant, antipsychotic, and opioid drugs
 Respiratory depression can occur when taking in combination
o Do not operate heavy machinery
o Don’t take with kava kava – can cause a sedative effect
o Should not be used longer than 3-4 weeks
Nonbenzodiazepines
o Zolpidem
 Used for short term treatment of insomnia – <10 days
Melatonin agonists
o Ramelteon
 Not a controlled substance
 Action: selectively targets melatonin receptors to regulate circadian
rhythms in the treatment of insomnia
 Adverse effects: drowsiness, dizziness, fatigue, headache, nausea, and
suicidal ideation
Older adult considerations
o Consider nonpharmacologic methods
o Hypnotic usage can cause a variety of side effects
 Barbiturates can increase CNS depression and confusion in older adults
 Should not be taken for sleep
 Short to intermediate acting benzos are considered the safer option
 Long acting benzos should be avoided
Anesthetics
Classified as general or local
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General: depress the CNS, alleviate pain, and cause a loss of consciousness
Balanced anesthesia
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Combination of drugs frequently used in general anesthesia
o Include: hypnotic, premedication with opioid analgesic or benzo +
anticholinergic, short acting barbiturate, inhaled gas, muscle relaxant
o Minimizes cardiovascular problems, decreases the amount of general anesthetic
needed, reduces possible nausea and vomiting, minimizes the disturbance of
organ function, and decreases pain
Inhalation Anesthetics
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Provide smooth induction
Halothane, enflurane, isoflurane, desflurane, sevoflurane
o Full recovery approx. 1 hour
o Desflurane and sevoflurane recovery can be within minutes
Usually combined with nonbarbiturate, a strong analgesic, and a muscle relaxant
Adverse effects: respiratory depression, hypotension, dysrhythmias, and hepatic
dysfunction
o Can trigger malignant hyperthermia
IV Anesthetics
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Can be used for general anesthesia or induction stage
Propofol, droperidol, etomidate, ketamine
o Have rapid onset and short duration of action
Adverse effects: respiratory and cardiovascular depression
Local Anesthetics
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Action: block pain at the site where the drug is administered by preventing conduction of
nerve impulses
Used in dental procedures, suturing skin lacerations, short-term surgery at localized area,
blocking nerve impulses, and diagnostic procedures
Lidocaine, procaine
o Lidocaine has rapid onset and longer duration of action
CH20 – Parkinsonism and Alzheimer's
Parkinson disease: chronic, progressive neurological disorder that effects the extrapyramidal
motor tract – controls posture, balance, and locomotion
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Rigidity, bradykinesia, gait disturbances, and tremors
o Rigidity increases with movement, shuffling gait, absence of arm swing, pillrolling motions, involuntary tremors of head and neck
Patho: imbalance of neurotransmitters dopamine and acetylcholine
o Degeneration of dopaminergic neurons leads to a lack of dopamine
o Less dopamine = unopposed acetylcholine – causes excitation and stimulation of
neurons that release GABA
Treatment: anticholinergics, dopaminergics, dopamine agonists, MAO-B inhibitors
Anticholinergics
o Action: inhibit release of acetylcholine – reduces rigidity and some tremors
o Trihexyphenidyl and benztropine
o Side effects: dizziness, anxiety, photophobia, blurred vision, ocular hypertension,
weakness, tachycardia, GI distress, constipation, anhidrosis, dry mouth, urinary
retention
o Contraindicated in people with glaucoma
o Monitor urine output for urinary retention
o Increase fluid intake, fiber, and exercise to avoid constipation
Dopaminergics
o Levodopa
 When first introduced, was effective in diminishing symptoms of PD and
increasing mobility
 Needs large doses to achieve pharmacologic response
 High doses cause side effects – nausea, vomiting, dyskinesia,
orthostatic hypotension, cardia dysrhythmias, and psychosis
o Carbidopa-Levodopa
 Action: converts to dopamine and increases mobility
 Drug of choice
 Carbidopa inhibits enzyme in peripheral nervous system allowing more
levodopa to reach the brain
 Smaller doses of levodopa are needed to reach desired effect
 More side effects occur due to more available levodopa: nausea,
vomiting, dystonic movement, and psychotic behavior
Dopamine Agonist
o Bromocriptine
 Action: acts directly on DA receptors in the CNS, cardiovascular system,
and GI tract
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Taken alone or in combination with carbidopa-levodopa
Side effects: headache, fatigue, hypotension, rhinitis, sinusitis, GI
bleeding, nausea, constipation, hypoglycemia
Monoamine Oxidase B Inhibitors
o Selegiline
 Action: enzyme MAO-B causes catabolism of DA
 Inhibits MAO-B and prolongs the action of levodopa
 Side effects: dizziness, headache, confusion, hallucinations, depression,
insomnia, ataxia, nausea, constipation, orthostatic hypotension
 Interactions: foods high in tyramine can cause hypertensive crisis
 Aged cheese, bananas, red wine, etc.
Alzheimer's disease: irreversible neurodegenerative disorder characterized by a decline in a
patient’s ADL, cognitive abilities, and changes in behavior
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Patho: degeneration of the cholinergic neuron and deficiency in Ach, neuritic plaques that
form
Acetylcholinesterase/Cholinesterase Inhibitors
o Rivastigmine
 Uses: improve cognitive function for patients with mild to moderate AD
 Action” “allow more acetylcholine in neuron receptors
 Increase cognitive function, slows disease process
 Contraindicated in people with liver disease
 Side effects: dizziness, headache, confusion, depression, dry mouth,
dehydration, GI distress, weight loss, peripheral edema, orthostatic
hypotension
 Don’t take with food
CH21 – Neuromuscular Disorders and Muscle Spasms
Myasthenia gravis: autoimmune neuromuscular disease
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Patho: antibodies attack ACh receptors – results in a decreased amount of AChR sites at
the neuromuscular junction
o Prevents ACh molecules from attaching to receptors and stimulating normal
muscular contraction
 Results in ineffective muscle contraction and muscle weakness
Characterized by weakness and fatigue of the skeletal muscles – eyelid or extraocular
muscles are involved – ptosis and diplopia
o Other: dysphagia, dysarthria, and respiratory muscle weakness
Myasthenic crisis: severe, generalized muscle weakness that involves the muscles of
respiration (diaphragm and intercostal muscles)
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o Triggers – inadequate dosing of AChE inhibitors, infection, emotional stress,
menses, pregnancy, surgery, trauma, hypokalemia, temperature extremes, and
alcohol intake
o Can lead to death from paralysis of respiratory muscles – if muscle weakness
remains untreated
o Treated with neostigmine – fast acting AChE inhibitor
Acetylcholinesterase inhibitors
o Neostigmine
 First drug used to manage MG – parasympathomimetic agent
 All other AChE drugs should be discontinued 8 hours before
administration of neostigmine
 Short-acting – treats Myasthenic Crisis
o Pyridostigmine
 Reversable AChE inhibitor, preventing the destruction of acetylcholine by
cholinesterase and thereby allowing free transmission of nerve impulses
across the neuromuscular junction
 Intermediate acting
o Side effects: GI disturbances, increased salivation and tearing, miosis, blurred
vision, and brady cardia
 Overdosing and underdosing cause: muscle weakness, dyspnea, and
dysphagia
 Underdosing = myasthenia crisis
 Overdosing = cholinergic crisis
When unresponsive to AChE inhibitors: prednisone, plasma exchange, IV immune
globulin, immunosuppressive drugs
Multiple Sclerosis: autoimmune disorder that attacks the myelin sheath of nerve fibers in the
brain and spinal cord – results in lesions (plaques)
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Onset is usually slow with remissions and exacerbations of multiple symptoms
Common manifestations: motor, sensory, neurologic, cerebellar, and emotional problems
o Motor: weakness or paralysis of the limbs, muscle spasticity, and diplopia
o Sensory: numbness, tingling, blurred vision, vertigo, and tinnitus
Classification: relapsing-remitting, primary progressive, secondary progressive,
progressive relapsing, clinically isolated syndrome
Immunomodulators
o Disease modifying drugs – first line treatment for MS
o Slow the progression of the disease and prevent relapses
o Interferon beta-1a, peginterferon beta-1a
Skeletal Muscle Relaxants
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Used to relieve muscular spasms and pain associated with traumatic injuries and
spasticity from chronic debilitating disorders
Central acting
o Used in cases of spasticity to suppress hyperactive reflex and for muscle spasms
that do not respond to anti-inflammatory agents, physical therapy, or other forms
of therapy
o Have sedative effect
o Side effects: drowsiness, dizziness, lightheadedness, headaches, and occasional
GI sensitivity
Direct-acting
o Decreases muscle spasm pain and increases ROM
o Suppresses hyperactive reflex
CH8 – Drugs in Substance Abuse Disorder
Reward circuit – drugs increase availability of dopamine and other neurotransmitters (GABA,
serotonin) in the limbic system (regulates pleasure & other emotions)
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Patient will start wanting more drugs and create tolerance
Alcohol use disorder
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Alcohol inhibits GABA – leads to reduction of neurotransmitters
Disulfiram
o Action: inhibits aldehyde dehydrogenase (enzyme involved in metabolizing
alcohol)
o Best used in people who are newly abstinent
o Contraindicated: people who are intoxicated; should not be taken within 12 hours
of alcohol consumption (mouthwash, cough medicine, anything containing
alcohol)
 Side effects: nausea, headache, vomiting, chest pain, and difficulty
breathing – rash, drowsiness, impotence, acne, and metallic aftertaste –
hepatoxicity, psychosis, peripheral neuropathy, and optic neuritis
Acamprosate
o Action: GABA analogue thought to work in the brain to restore the balance
between neuronal excitation and inhibition via GABA and glutamate
o Should only be used in people who are abstinent but can be continued through
relapse
o Contraindicated in people with creatinine clearance under 30
o Side effects: pain, loss of appetite, nausea, diarrhea, dizziness, anxiety, pruritus,
depression, insomnia, xerostomia, paresthesia
Opioid use disorder
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Controlled substances legally prescribed to treat moderate to severe pain
o Interact with opioid receptors in the brain – floods the brain’s reward system with
dopamine, producing a sense of euphoria and tranquility
Opioids: oxycodone, hydrocodone, morphine, methadone, fentanyl
o Short-term effects: drowsiness, mental confusion, nausea, constipation, and dosedependent respiratory depression
o Cancer treatment patients may need higher dose of opioids due to built up
tolerance
o When taken with SSRIs, can cause serotonin syndrome
 Agitation, hallucinations, coma, tachycardia, hypertension, hyperthermia,
and rigidity
Naloxone (Narcan)
o Drug of choice to treat respiratory depression
o Action: short-acting opioid antagonist that attaches to the opioid receptors in the
brain, blocking its activation
Methadone
o Action: opioid receptor agonist at the mu receptor and an antagonist at the NMDA
receptor
 Changes the way a person’s brain responds to pain
o Taken daily – blocks the sense of euphoria and tranquility cause by opioid usage
and prevents opioid withdrawal and craving
o Don’t take with rifampin, phenytoin, St. John’s wort, phenobarbital, or
carbamazepine – reduced serum methadone levels and precipitate withdrawal
o Side effects: lightheadedness, constipation, dizziness, sedation, nausea, and
vomiting
Cannabis and tobacco use disorders
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Cannabis effects: THC rapidly crosses blood brain barrier and binds with cannabinoid
receptors
o Reduces ability to respond appropriately to incoming stimuli
o Legal in some places, illegal in most
Tobacco: nicotine stimulates the release of dopamine, norepinephrine, GABA, glutamate,
and endorphins – results in stimulation and pleasure and a reduction in stress and anxiety
CH22 – Antipsychotics and Anxiolytics
Schizophrenia: chronic psychotic disorder
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Positive symptoms: “hyper” – exaggeration of normal function, incoherent speech,
hallucinations, delusions, and paranoia
o Typical antipsychotics used to manage positive symptoms of schizophrenia
Negative: “hypo” – decrease or loss in function and motivation
o Poverty/simplicity of speech, blunted affect, inertia, poor self-care, and social
withdrawal
o More chronic and persistent
o Atypical antipsychotics used to manage both positive and negative symptoms
Antipsychotics
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Action: block D2 dopamine receptors in the brain and reduce psychotic symptoms
Typical: phenothiazines and nonphenothiazines
o assess for symptoms of neuroleptic malignant syndrome (fever, pulse, BP)
Phenothiazines: aliphatic, piperazine, piperidine (differ based off of side effects)
o Action: block norepinephrine causing sedative and hypotensive effects early in
treatment
o High incidence of EPS symptoms
o Fluphenazine, perphenazine
 action: blocks dopamine receptors in the brain
 use: manages symptoms of psychosis including schizophrenia
 side effects: EPS, dizziness, headache, blurred
Nonphenothiazines
o Haloperidol
 Action: alters dopamine effect by blocking dopamine receptors
 Used: control psychosis and decreased agitation in adults and children
 Strong EPS effects – pseudoparkinsonsim, akathisia, dystonia, tardive
dyskinesia; photosensitivity, dry mouth, tachycardia, urinary retention, and
constipation
 Contraindications: narrow-angle glaucoma, dehydration, CNS depression,
CVD, hepatic damage, blood dyscrasias
Should not be given with other antipsychotic or antidepressive drugs – except those who
are refractory to drug therapy
o Don’t take alcohol or other CNS depressants
o Avoid driving until drug dosing is stabilized
Atypical Antipsychotics: Clozapine, risperidone, olanzapine, ziprasidone, aripiprazole
o Effective in treating both positive and negative symptoms of schizophrenia
o Unlikely to cause symptoms of EPS
o Action: block serotonin and dopaminergic D4 receptors
o Side effects: weight gain, drowsiness, unsteady gait, headache, insomnia,
depression, diabetes mellitus, dyslipidemia
o Clozapine
 first atypical antipsychotic used
 serious adverse effects: seizures and agranulocytosis
 used for severely ill schizophrenic patients who have not responded to
traditional antipsychotic drugs
 monitor WBC count closely
o Risperidone
 Used to treat the positive and negative symptoms
 Does not cause agranulocytosis
 Common adverse effects: EPS, insomnia, headache, akathisia
Anxiolytics
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Used to treat excessive anxiety
Major group: Benzos
Benzodiazepines
o Enhance GABA action
o Diazepam, lorazepam, alprazolam
o Side effects: sedation, dizziness, headaches, dry mouth, blurred vision, rare
urinary incontinence, and constipation
 Adverse reactions: leukopenia
 Withdrawal symptoms from long-term use: paranoia, delirium, panic,
hypertension, and status epilepticus
o Should not be abruptly discontinued – causes withdrawal symptoms
Buspirone
o Miscellaneous anxiolytic
o Not effective until 1-2 weeks after use
o Fewer side effects of sedation and physical and psychological dependency
o Side effects: drowsiness, dizziness, headache, nausea, nervousness, and
excitement
o Limit intake of grapefruit juice – 8oz/daily; half a grapefruit
CH23 – Antidepressants and Mood Stabilizers
Complementary and alternative therapies: St. John’s wort and ginkgo biloba
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Should not be used concurrently with antidepressants – can lead to serotonin syndrome
Major antidepressants: Tricyclic, selective serotonin reuptake inhibitors, serotonin
norepinephrine inhibitors, atypical antidepressants, monoamine oxidase inhibitors
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Tricyclic antidepressants
o Amitriptyline, imipramine, trimipramine, doxepin, desipramine,
nortriptyline, protriptyline
o Action: block the uptake of neurotransmitters norepinephrine and serotonin in the
brain
o Clinical response seen after 2-4 weeks of therapy
o Elevates mood, increases interest in daily living and activity, and decreases
insomnia
o Given at night – due to sedative properties
o Don’t abruptly discontinue – can lead to vomiting, nausea, anxiety, and akathisia
o Side effects: orthostatic hypotension, sedation, anticholinergic effects,
cardiotoxicity, and seizures
 Tachycardia, urinary retention, constipation, dry mouth, blurred vision
o Don’t take alcohol, hypnotics, sedatives, and barbiturates – potentiate CNS
depression
SSRIs
o Most commonly prescribed
o Action: block the reuptake of serotonin in the nerve terminal of the CNS
o Used for major depressive disorders
 Can also be used for anxiety disorders – OCD, panic disorders, phobias,
etc.
 Fluoxetine, fluvoxamine, sertraline, paroxetine, citalopram,
escitalopram
o Therapeutic effects seen in 3-4 weeks; not immediate
o Don’t take with grapefruit juice – can lead to toxicity
o Side effects: dry mouth, blurred vision, insomnia, headache, anorexia, nausea,
diarrhea, sexual dysfunction, and suicidal ideation
 Decrease over 1-4 weeks
SNRIs
o Action: inhibit the reuptake of serotonin and norepinephrine
o Used for major depression
 Can also be used for anxiety disorder and social anxiety disorder
o Duloxetine, levomilnacipran, desvenlafaxine
o Side effects: drowsiness, dizziness, insomnia, headache, amnesia, blurred vision,
erectile/ejaculation dysfunction
 Adverse effects: hypertension, orthostatic hypotension, tachycardia,
seizures, NMS, and suicidal ideation
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MAOIs
o Action: block MAO enzyme
 MAO enzyme inactivates norepinephrine, dopamine, epinephrine, and
serotonin – by blocking it, the levels of neurotransmitters will rise
o Used for depression not controlled by TCAs and second-generation
antidepressants
o Not often prescribed due to fatal food and drug interactions
 Hypertensive crisis with medications containing phenylephrine and
pseudoephedrine
 Hypertensive crisis when eating foods with tyramine
 Aged cheese, cream, yogurt, coffee, chocolate, bananas, raisins,
Italian green beans, liver, pickled foods, sausage, soy sauce, yeast,
beer, and red wines
o Side effects: insomnia, orthostatic hypotension, anticholinergic effects
Mood stabilizers
o Lithium
 Has calming effect but may cause memory loss and confusion
 Action: alteration of ion transport in muscle and nerve cells’ increased
receptor sensitivity to serotonin
 Narrow therapeutic serum range: 0.8-1.2 mEq/L
 Over 1.5 leads to toxicity
 Check levels every 1-2 months
 Used for bipolar disorder and manic episodes
 Side effects: headache, memory impairment, blurred vision, metallic taste,
thirst, dry mouth, dental caries, drowsiness, dizziness, fatigue, ataxia,
tremor, anorexia, etc.
CH24 – Antiinflammatories
5 stages of inflammation – swelling, redness, heat, pain, loss of function
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COX1: protects the stomach lining and regulates blood pressure
COX2: triggers inflammation and pain
Drug groups: NSAIDs, corticosteroids, disease-modifying antirheumatic drugs, antigout drugs
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NSAIDs
o Include aspirin and aspirin-like drugs that inhibit the enzyme COX
o Relieve inflammation and pain
o 6 groups: salicylates, para-chlorobenzoic acid derivatives, selective COX-2
inhibitors, etc.
o Salicylates
 Aspirin
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Action: prostaglandin inhibitor that decreases the inflammatory
process – inhibits COX enzyme
 Considered an antiplatelet drug also
 Should not be taken with other NSAIDs – decreases blood level
and effectiveness
 Should be taken with water, milk, or food to avoid GI distress
 Should not be taken when pregnant, given to children, or taken
with anticoagulants
 Toxic serum level: >300 mcg/mL
 Do not administer for flu symptoms in children – can lead to Reye
syndrome
o Call poison control if child ingested large/unknown amount
o Older adult considerations
 Drug interactions more common – due to polypharmacy
 GI distress 4x more common – can lead to hospitalization
 Renal function should be monitored – due to decreased renal function in
older adults
 NSAID dosage should be lowered to reduce the risk of possible
complications
Para-chlorobenzoic acid
o Indomethacin
 Not OTC
 Action: highly protein bound; potent prostaglandin inhibitor
 Use: RA, gouty arthritis, and osteoarthritis
 Should be taken with food to avoid stomach irritation
Propionic acid derivatives
o Ibuprofen
 Action: inhibits COX-1 and COX-2
 Highly protein bound – don’t give with other highly protein-bound drugs
 Use: reduce inflammatory process, relieve pain, reduce fever
 Don’t cause as much GI upset – should still be taken with food
 Don’t take with aspirin or acetaminophen, don’t taken if pregnant
Selective COX-2 inhibitors
o Celecoxib
 Action: selectively inhibits COX-2 enzyme without inhibition of COX-1
 Used to decrease inflammation and pain – drugs of choice for patients
with severe arthritic conditions who need high doses of anti-inflammatory
drugs
Corticosteroids
o Prednisone, prednisolone, and dexamethasone
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o Actions: control inflammation by suppressing or preventing the inflammatory
process at the injured site
o Prescribed for arthritic conditions
 Not drug of choice due to numerous side effects but are frequently used to
control flare-ups
DMARDs
o Immunosuppressive agents
 Used to treat refractory RA that does not respond to anti-inflammatory
drugs
CH25 – Analgesics
Analgesics: nonopioid or opioid
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Nonopioid
o NSAIDs and COX-2 inhibitors
o Used to treat mild to moderate pain
o Effective for: dull, throbbing pain of headaches; dysmenorrhea; inflammation;
minor abrasions; muscular aches and pain; mild to moderate arthritis
o NSAIDs: aspirin, ibuprofen, naproxen
 Have analgesic, antipyretic, and anti-inflammatory action
 Aspirin should not be given to those under 19 – Reye syndrome
 Side effects: gastric distress
 Should be taken with food, at mealtime, or with full glass of liquid
o Acetaminophen
 Action: inhibits prostaglandin synthesis
 Used for muscular aches and pain
 Has antipyretic properties but not anti-inflammatory ones
 Max dose – 4g/day
 Assess pain 30 minutes after administration
 Check AST and ALT levels – it is metabolized in the liver
 Side effects: anxiety, headache, insomnia, constipation, peripheral edema,
low incidence of GI distress
Opioids
o Used for moderate to severe pain
o Act mostly on CNS – contraindicated for patients with head injuries
o Suppress respiration and coughing
o Side effects: constipation, orthostatic hypotension, respiratory depression
o Morphine
 Effective for acute pain, dyspnea, and relieve preoperative anxiety

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Side effects: drowsiness, hypotension, respiratory depression, dizziness,
miosis, dependence
 Naloxone – antidote
o Meperidine
 Shorter duration of action than morphine
 Not indicated for patients for chronic pain, severe liver dysfunction, sickle
cell disease, seizures, etc.
 Not for long-term use
 Major side effect: decrease in BP
o Hydromorphone
 6x more potent than morphine with fewer hypnotic effects and less GI
distress
 Faster onset and shorter duration of action
 Respirations should be monitored and adequate hydration should be given
o Patient controlled analgesia
 Morphine, fentanyl, hydromorphone used
 Alternative route for opioid administration for self-administered pain relief
as needed
 Lockout mechanism in place with predetermined safety limits
 Prevents overdose
Adjuvant therapies
o Gabapentin
 Anticonvulsant
 Given to diabetic patients with neuropathic pain
 Also, for patients with phantom leg pain
Upper Respiratory Disorders
Antihistamines: block H1 receptor, decreasing nasal secretions
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First-generation: usually cause drowsiness, disturbed coordination, dizziness, etc.
o Diphenhydramine: competes with histamine for binding at H1-receptor sites and
antagonizes histamine effects
 Treats rhinitis, common colds
 Contraindication: closed angle glaucoma, urinary retention, severe liver
disease
 Interactions: increases CNS depression with alcohol and other CNS
depressants
 Do not operate heavy machinery after administration
 Take at night
Second-generation: fewer anticholinergic effects and lower incidence of drowsiness;
nonsedatives
o Loratadine, cetirizine, fexofenadine
o Nonsedative
o Can be taken in the morning
Nasal decongestants: stimulate the alpha-adrenergic receptors, producing
vasoconstriction of the capillaries within the nasal mucosa
o Can be administered in sprays, drops, tablet, capsule, or liquid form
o Used for allergic rhinitis and acute coryza (acute nasal discharge)
o Over-usage can lead to rebound nasal congestion
o Phenylephrine hydrochloride and pseudoephedrine
 Pseudoephedrine is frequently combined with an antihistamine, analgesic,
or antitussive in oral cold remedies
o Short-term medications
o Cause fewer side effects than systemic decongestants
o Side effects: nervousness, restlessness, rebound nasal congestion
o Limit the use of nasal sprays and drops
o Contraindicated in patients with HTN, cardiac disease, hyperthyroidism, and DM
o Interactions with MAOIs (possible increase of HTN), caffeine (increase
restlessness and palpitations)
Intranasal glucocorticoids: anti-inflammatory action that decreases rhinitis symptoms
(sneezing and congestion)
o Commonly used
o Side effects: headache, blurred vision, irritated/dry mucosa, pharyngitis,
hoarseness, nausea, vomiting, candidiasis, insomnia
o Can be used alone or with an H1 antihistamine
o Spray should be sprayed away from septum and sniffed gently
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Antitussives: act on cough control center in the medulla to suppress the cough reflex
o Used on cough that is nonproductive and irritating
o Dextromethorphan is widely used in OTC cold remedies
 Rapidly absorbed and works after 15-30 minutes
Expectorants: loosen bronchial secretions so they can be eliminated by coughing
o Used with or without other pharmacological agents
o Guaifenesin is the most commonly used expectorant
o Water is the best natural expectorant
o When taking, patient should increase fluid intake to at least 8 glasses per day to
help loosen mucus
Lower Respiratory Disorders
Sympathomimetics increase cAMP, causing dilation of the bronchioles
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-
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Epinephrine is administered in emergency situations to restore circulation and increase
airway patency
Albuterol: stimulates beta2-afrenergic receptors in the lungs – relaxes the bronchial
smooth muscle – causing bronchodilation
o Used to treat asthma, for prophylaxis and treatment of bronchospasms
o Side effects: tremors and tachycardia (over-usage); rhinitis, headache, excitability,
etc.
o High doses may stimulate beta1 responses- nervousness, tremor, and increased
pulse rate
Metaproterenol: has some beta1 effect but primarily used as beta2 agent
o Used for long-term treatment of asthma through an inhaler
 Administration route delivers more of the drug directly to the constricted
bronchial site
Tiotropium: anticholinergic drug used for maintenance treatment of bronchospasms
associated with COPD
o Administered with HaniHaler device (must be washed with warm water and
dried)
o Adverse effects: dry mouth, constipation, vomiting, dyspepsia, abdominal pain,
depression, insomnia, headache, joint pain, and peripheral edema
o Combination of ipratropium bromide with albuterol sulfate is used to treat COPD;
have synergistic effect
Methylxanthines: relaxes smooth muscle of bronchi and bronchioles increasing cAMP
promoting bronchodilation
o Used for asthma
o Low therapeutic index: 5-15 mcg/mL; greater than 20 becomes toxic
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Leukotriene modifiers are effective in reducing the inflammatory symptoms of asthma
triggered by allergic and environmental stimuli
o Decrease bronchoconstriction
o Montelukast: used for treatment of exercise-induced asthma
o Side effects: dizziness, headache, confusion, GI distress, depression, weakness,
infection
Glucocorticoids: anti-inflammatory action and are indicated if asthma is unresponsive to
bronchodilator therapy or if the patient has an asthmatic attack while on maximum doses
of theophylline or an adrenergic drug
o Have a synergistic effect when given a beta2 agonist
o MDI inhaler: Beclomethasone
o Tablet: Dexamethasone, prednisone
o IV: Dexamethasone
o Not helpful for acute attacks because of longer onset
o Increase risk of immunosuppression
o Side effects: candida albicans, dry mouth, superinfections, hyperglycemia,
headache, euphoria, etc
o Management of moderate to severe asthma exacerbations
o Weaning or tapering off the dose may be necessary when using prolonged
glucocorticoid therapy
o Should be taken with food to avoid ulceration
o Combination of fluticasone propionate and salmeterol is effecting in controlling
asthma symptoms
Cromolyn: used for prophylactic treatment if bronchial asthma, and it must be taken
daily
o Not used for acute asthma attacks
o Acts by inhibiting release of histamine and other inflammatory mediators from
mast cells to prevent an asthma attack; does not have bronchodilator properties
o Side effects: postnasal drip, cough, irritation of nose and throat
o Rebound bronchospasm is a serious side effect
o Used to treat asthma in children