Adrenergic and Cholinergic Drugs: Mechanisms, Indications and Nursing Assessment

Adrenergic Drugs:
Dopamine – Alpha and Beta Agonists

- Mechanism of Action
o Produces positive chronotropic and inotropic effects on the myocardium by indirect stimulation of beta receptors causes
release of norepinephrine. This causes increased HR and contractility
- Indications
o Correction of hemodynamic instability in shock syndrome due to MI, trauma, sepsis, and heart failure
o Adjunct to standard measures to improve:
 BP
 Cardiac output
 Urine output treatment in shock unresponsive to fluid replacement
 Increase renal perfusion
- Contraindications
o Drug allergy, phenpchrompcytoma, tachyarrhythmias, hypersensitivity
- Use Cautiously In
o Hypovolemia, MI, occlusive vascular diseases
- Adverse Effects
o CNS: headache
o EENT: mydriasis (high dose)
o Resp: dyspnea
o CV: arrhythmias, hypotension, angina, ECG change, palpitations, vasoconstriction
o GI: nausea, vomiting
- Interactions
o Increased effect with other adrenergic agonists
- Dosages
o Low dose to dilate blood vessels, increased dose improves cardiac output, high doses causes vasoconstriction to increase
blood pressure
- Therapeutic Effects
o Increase cardiac output, increase BP, improved renal blood flow, increase air exchange
- Toxicity and Overdose
o If excessive hypertension occurs, rate infusion should be decreased or temporarily discontinued until BP is decreased
- Nursing Assessment
o Monitor BP, HR, pulse pressure, ECG, cardiac output, respiratory, CVP, urinary output during administration
o Palpate peripheral pulses and assess appearance of extremities
o If hypotension occurs, increase the rate
Epinephrine – Alpha and Beta Agonist
o Nonselective adrenergic agonist (works on alpha and beta receptors)
o Produces bronchodilation, vasoconstriction, inhibit release of mediators of immediate hypersensitivity
- Indications
o Emergency situations like ACLS, anaphylaxis, acute asthma, COPD, croup, management of cardiac arrest
- Contraindications
o Drug allergy, severe hypertension, hypersensitivity to adrenergic amines
o Use cautiously in cardiac disease; hypertension; hyperthyroidism; Parkinson’s disease; phenpchrompcytoma; diabetes;
glaucoma
- Adverse effects
o CNS stimulation, tremor, tachycardia
o CNS: nervousness, restlessness, tremor, headache, insomnia
o Resp: paradoxical, bronchospasm
o CV: angina, arrhythmias, hypertension, tachycardia
o GI: nausea, vomiting
- Interactions
o Other adrenergic agonists
o Bronchodilation, maintenance of HR and BP
o Symptoms of overdose include persistent agitation, chest pain, or discomfort, decreased BP, dizziness, hyperglycemia,
hypokalemia, seizures, tachyarrhythmias, trembling, vomiting
o Assess lung sounds, respiratory pattern, pulse, BP, observe for bronchospasm
Phenylephrine (Neo-Synephrine) – Alpha Specific Agonist
o Works almost exclusively on the alpha-adrenergic receptors
- Indications
o Used primarily for short-term treatment to increase BP in patients in shock
o Control of supraventricular tachycardias
o Vasoconstriction in regional anesthesia
o Topical ophthalmic drug
o Nasal decongestant
- Contraindications
o Hypersensitivity to bisulfites, HF, coronary artery disease or peripheral arterial disease
- Adverse Effects
o Tachycardia, arrythmias, hypertension, ischemic injury
o CNS: blurred vision, headache, insomnia, nervousness, tremor
o Resp: dyspnea
o CV: arrythmias, bradycardia, chest pain, hypertension, ischemia, tachycardia
o GI: nausea and vomiting
- Interactions
o General anesthetics, MAOIs, alpha-adrenergic blockers
o Increase BP
o Monitor BP, ECD+G continuously for arrythmias, assess IV site
Doxazosin – Alpha Blocker
o Cause both arterial and venous dilation, reducing peripheral vascular resistance and BP
- Indication
o ALPHA: treat hypertension, Benign prostatic hyperplasia (BPH)
- Contraindications
o Hypersensitivity
- Adverse Effects
o Orthostatic hypotension, tachycardia, vertigo, sexual dysfunction
o CNS: dizziness, headache, depression, drowsiness, fatigue, nervousness, weakness
o Resp: dyspnea
- Interactions
o Increase risk of hypotension
o Lowering of BP, increased urine flow and decreased symptoms of BPH
o Monitor BP and pulse, assess for orthostatic hypotension and syncope, monitor I/O, assess for symptoms of BPH
Labetolol – Beta Blocker
- Mechanism of action
o Blocks stimulation of beta1 (myocardial) and beta2 (pulmonary, vascular) – adrenergic receptor sites
- Indications
o Management of hypertension
- Contraindications
o Uncompensated HF; pulmonary edema, cardiogenic shock; bradycardia or heart block
- Adverse Effects
o CNS: fatigue, weakness, anxiety, depression, dizziness, drowsiness, insomnia, memory loss, mental status changes
o Resp: bronchospasm, wheezing
o CV: arrythmias, bradycardia, CHF, pulmonary edema, orthostatic hypotension, peripheral vasoconstriction
o GI: constipation, diarrhea, nausea
o Neuro: paresthesia
- Interactions
o General anesthesia and verapamil, digoxin
o Decreased BP
o Monitor BP and pulse, assess for orthostatic hypotension, monitor I/O and daily weights
Propranolol – Beta Blocker
- Indications
o Management of hypertension, angina, arrythmias, hypertrophic cardiomyopathy, thyrotoxicosis
- Contraindications
o Hypersensitivity, uncompensated HF; pulmonary edema, cardiogenic shock; bradycardia or heart block
- Adverse Effects
o Neuro: paresthesia
- Interactions
o General anesthesia, IV phenytoin, verapamil, digoxin
o Decreased HR and BP, suppression of arrythmias, prevention of MI
o Monitor BP and pulse, assess for orthostatic hypotension, monitor I/O and daily weights
Metoprolol – Beta Blocker (most commonly used beta blocker)
- Indications
o Hypertension, angina pectoris, prevention of MI and decreased mortality in patients with recent MI
- Contraindications
o Uncompensated HF; pulmonary edema, cardiogenic shock; bradycardia or heart block
- Adverse Effects
- Interactions
o General anesthesia, IV phenytoin, verapamil, digoxin
o Decreased BP and HR, decreased frequency of attacks of angina pectoris, decreased rate of cardiovascular mortality
o Monitor BP, ECG and pulse, vital signs, monitor I/O and daily weights
Cholinergic Drugs:
Donepezil (Aricept) – Agonist
o Inhibits acetylcholinesterase thus improving cholinergic function by making more acetylcholine available
- Indications
o Cholinesterase inhibitor that works centrally in the brain to increase levels of ACh by inhibiting acetylcholinesterase
o Used in the treatment of mild to moderate dementia associated with Alzheimer’s disease
o Similar cholinesterase inhibitors include galantamine and rivastigmine
- Contraindications
o Known drug allergy
o Underlying cardiac disease, history of ulcer disease
- Adverse Effects
o GI upset (including ulcer risk caused by increased gastric secretions), drowsiness, dizziness, insomnia, and muscle cramps.
The effects on the cardiovascular system are complex and may include bradycardia, syncope, hypotension with reflex
tachycardia, or hypertension.
- Interactions
o Anticholinergics (counteract donepezil effects) and nonsteroidal anti-inflammatory drugs (NSAIDs)
o May temporarily lessen some of the dementia associated with Alzheimer’s disease. Enhances cognition
o Assess cognitive function, monitor HR
Atropine – Blocker (Anticholinergic)
o Inhibits the action of acetylcholine at postganglionic sites located in smooth muscle, secretory glands, CNS
- Indications
o Naturally occurring antimuscarinic
o Bradycardia, ventricular asystole, antidote for anticholinesterase inhibitor toxicity or poisoning, and preoperatively to
reduce salivation and GI secretions
- Contraindications
o Angle-closure glaucoma, advanced hepatic and renal dysfunction, hiatal hernia associated with reflux esophagitis,
intestinal atony, obstructive GI or GU conditions, and severe ulcerative colitis
- Adverse Effects
o ABCDS: agitation, blurred vision, constipation/confusion, dry mouth, stasis of urine/sweating
o CNS: drowsiness, confusion, hyperpyrexia
o EENT: blurred vision, dry eyes, mydriasis
o CV: tachycardia, palpitations, arrythmias
o GI: dry mouth, constipation, impaired GI motility
- Interactions
o Anticholinergics, antihistamines, tricyclic antidepressants
o Increased HR, decreased GI and respiratory secretions, reversal of muscarinic effects
o If overdose occurs, physostigmine is the antidote
o Assess vital signs and ECG tracings, monitor I/O, assess abdominal distention and auscultate for bowel sounds
Opioid Analgesics:
Morphine – Agonist
o Bind to opioid receptors in the CNS and alters the perception of and response to pain stimuli while producing generalized
CNS depression
- Indications
o Severe pain, pain severe enough to require daily, around the clock long term opioid treatment for which alternative
treatment options are inadequate
- Contraindications
o Hypersensitivity; alcohol should be avoided; acute, mild, intermittent or postoperative pain
- Adverse Effects
o Constipation > 9%, N/V > 10%, pruritis 80%, dyspnea 3-10%, respiratory depression
- Safety
o Monitor respiratory status, many black box warnings,
- Developmental concerns
o Elders at greater risk for adverse effects, pregnancy category C, peds intermittent
- Interactions
o MAO inhibitors, antipsychotics, benzodiazepines, muscle relaxants, anxiolytics, alcohol
o Decrease in severity of pain
o If an opioid antagonist is required to reverse respiratory depression or coma, naloxone is the antidote
o Use pain scale, check RR, O2 sat, determine dose based on response to last dose
- Nursing Implementation
o IV – give slowly 2-4 min/mg, look up information for unfamiliar routes, patient teaching (orthostatic precautions)
- Nursing Evaluation
o Pain scale after peak, respiratory assessment, assess GI status and other side effects
Fentanyl (Transmucosal) – Agonist
o Bind to opioid receptors in the CNS and alters the perception of and response to pain stimuli while producing generalized
CNS depression
- Indications
o Management of breakthrough pain in cancer patients already receiving opioids and tolerant to around the clock opioids for
persistent cancer pain
- Contraindications
o Known tolerance or hypersensitivity
- Adverse Effects
o Usual opiate, high incidence, muscle rigidity
o CNS: dizziness, drowsiness, headache
o Resp: respiratory depression
o GI: nausea, vomiting, constipation
o CV: hypotension
- Safety
o High risk for respiratory depression, transdermal patches, after removal, still have med present – cautious disposal
o Remove old patches when applying new ones
o Too fast of IV administration increase risk for muscle rigidity
- Developmental Concerns
o Elders: high risk of confusion; Peds: safe disposal of transdermal patches
- Interactions
o MAO inhibitors, CYP3A4 inhibitors, CYP3A4 inducers
o Decrease in severity of breakthrough pain
o If an opioid antagonist is required to reverse respiratory depression or coma, naloxone is the antidote
o Breakthrough dosage should be 1-hour equivalent; Use pain scale, check RR, O2 sat, determine dose based on response to
last dose
o IV intermittent dose – give over 1-2 min; transdermal: upper back preferred, intact skin, don’t share hair, no heat; patient
teaching (orthostatic precautions) and safety issues
o Pain scale after peak, respiratory assessment, assess GI status and other side effects
Oxycodone – Agonist
- Everything same as morphine
Methadone – Synthetic Opioid Analgesic

• Synthetic opioid analgesic (Schedule II)
• Opioid of choice for the detoxification treatment of opioid addicts in methadone maintenance programs
• Renewed interest in the use of methadone for chronic (e.g., neuropathic) and cancer-related pain
• Prolonged half-life of the drug: cause of unintentional overdoses and deaths
• Cardiac dysrhythmias
Naloxone (Narcan) – Antagonist
o Opioid receptor antagonist that completely blocks the effects of opioids, including CNS and respiratory depression without
producing any agonist effects
o Blocks the effects of opioids on the brain and restores breathing within 2-8 minutes to prevent death
- Indications
o Reversal of CNS depression and respiratory depression because of suspected opioid overdose
- Contraindications
o Hypersensitivity; use cautiously in cardiovascular disease and patients who are physically dependent on opioids
- Adverse Effects
o Headache, hypertension, immediate and reversal of opioids: pain, seizures, death
o CV: ventricular arrhythmias
o GI: nausea and vomiting
- Safety
o Abrupt opioid withdrawal dangerous
- Legal and Ethical Issues
o Used in terminally ill patients
o Reversal of signs of opioid excess
o Naloxone is a pure antagonist with no agonist properties and minimal toxicity
o Respiratory assessment, determine dose based on desired outcomes
o IV: may give undiluted or dilute with NS and given over 30 sec; patient teaching: intranasal, adverse effects, should be
taken supine, don’t prime sprayer, call 911
o Pain scales Respiratory
Non-Opioid Analgesics:
Acetaminophen (Tylenol)
o Reduces prostaglandin synthesis that may serve as mediators of pain and fever, primarily in the CNS
- Indications
o PO, Rect: treatment of mild pain, fever; IV: treatment of mild to moderate pain, moderate to severe pain with opioid
analgesics
- Contraindications
o Previous hypersensitivity, products containing alcohol should be avoided
- Adverse Effects
o Low incidence EXCEPT if overdose
o Maximum dose 4000 mg/24 hr, liver failure, acetylcysteine for overdose
- Safety
o Common ingredient in OTC meds, PO opioid combinations
- Genetics and Meds
o Possible genetic variability affects excretion, not due to ethnicity
o Analgesia, antipyresis
o If overdose occurs, acetylcysteine (acetadote) is the antidote
o Use pain scales, how much acetaminophen have they received in past 24 hours
o Patient teaching: maximum 24-hour dose, beware of acetaminophen in OTC meds
o Pain scales, temperature if given for fever
Anesthetics:
Propofol
o Short-acting hypnotic and produces amnesia (mechanism of action is unknown)
- Indications
o Conscious sedation?
- Contraindications
o Hypersensitivity to propofol, soybean oil, egg lecithin, or glycerol
- Adverse Effects
o Site pain 28%, involuntary muscle movement 17%, HF 10%, apnea, other cardiopulmonary effects, sepsis, propofol
infusion syndrome – mimics septic shock
- Safety
o Cardiovascular monitoring, respiratory monitoring, carful sterile technique
o RN’s cannot give anesthetics
o Induction and maintenance of anesthesia
o If overdose occurs, monitor pulse, respiration, and BP continuously. Maintain patient airway and assist ventilation as
needed. If hypotension occurs, treatment includes IV fluids, repositioning and vasopressors
o Assess respiratory status, pulse, BP, maintain patient airway and adequate ventilation, monitor propofol infusion syndrome
Lidocaine/Prilocaine
o Blocks conduction by decreasing ionic flux and produces local anesthesia by inhibiting transport of ions across neuronal
membranes, thereby preventing initiation and conduction of normal nerve impulses
- Indications
o Produces local anesthesia prior to minor painful procedures including insertion of needles etc
- Contraindications
o Hypersensitivity to lidocaine, prilocaine and any other amide-type local anesthetic
- Adverse Effects
o Low incidence except if absorbed systemically in large doses, irritation where used
o Local: blanching, redness, alteration in temperature sensation, edema, itching, rash
o Misc: anaphylaxis
- Safety
o Assure proper route, prevent injury to area anesthetized, aspiration prevention after oral use
- Genetics and Meds
o Red hair = resistance to lidocaine
o Anesthetic action localized to area of the application
o Assess application site for open wounds, apply only to intact skin, assess application site for anesthesia following removal
of system and prior to procedure
o Administration: don’t dilute, ID or SC – aspirate before injection
Nitrous Oxide (Laughing Gas)
o Inhaled anesthetic
o Weakest of the anesthetic drugs
o Used primarily for dental procedures or in addition to stronger inhaled agents.
o Increased postoperative nausea and vomiting
o Only inhaled gas currently used as a general anesthetic
o Very good analgesic properties and is used primarily for dental procedures or as a supplement to other, more potent
anesthetics
Dantrolene (Dantrium, Ryanodex) – for malignant hyperthermia
o Acts directly on skeletal muscle, causing relaxation by decreasing calcium release from sarcoplasmic reticulum in muscle
cells. Prevents intense catabolic process associated with malignant hyperthermia
- Indications
o PO: treatment of spasticity associated with spinal cord injury, stroke, cerebral palsy, MS
o IV: emergency treatment of malignant hyperthermia
- Contraindications
o None for IV
- Adverse Effects
o CNS: drowsiness, muscle weakness, confusion, dizziness, headache, insomnia, malaise, nervousness
o EENT: visual disturbances
o Resp: dyspnea, pleural effusions, respiratory depression
o CV: changes in BP, HF, tachycardia
o GI: hepatoxicity, diarrhea, anorexia, cramps, dysphagia
o Reduction of muscle spasticity, treatment and prevention of malignant hyperthermia
o Assess bowel function, assess neuromuscular status and muscle spasticity, assess previous anesthesia history, monitor
ECG, vital signs, electrolytes and urine output, monitor difficulty swallowing and choking during meals, monitor liver
function
Muscle Relaxants:
Baclofen (Lioresal)
o Inhibits reflexes at the spinal level
- Indications
o Relief of painful musculoskeletal conditions: muscle spasms, management of spasticity of severe chronic disorders
 Types of spasms: extensor spasms, flexor spasms, clonus, stiffness
o Work best when used along with physical therapy
o PO: treatment of reversible spasticity due to multiple sclerosis or spinal cord lesions
o IT: treatment of severe spasticity of cerebral or spinal cord origin
- Contraindications
o Hypersensitivity
- Adverse Effects
o Euphoria, lightheadedness, dizziness, drowsiness, fatigue, muscle weakness
o PO: confusion, nausea, weakness tiredness
o IT: unwanted movement of catheter or pump, skin over pump breaks down, infection or spinal fluid leak caused by
surgery, mechanical fail overdose or withdrawal symptoms from mech failure (seizures, difficulty breathing, organ failure)
o CNS: seizures, dizziness, drowsiness, fatigue
o EENT: nasal congestion, tinnitus
o Decreased muscle spasticity, bowel and bladder function may also be improved
- Interactions
o Other CNS depressions including alcohol, antihistamines, opioid analgesics and sedatives/hypnotics
o Assess muscle spasticity, observe patient for drowsiness, dizziness or ataxia, monitor during test dose
o Assess for pain and mobility
o Patient teaching: taking extended release at same time daily, report serious CNS symptoms
o Efficacy and adverse effects
Cyclobenzaprine (Amrix)
o Decreases motor nerve transmission in brain stem and reduces tonic somatic muscle activity at the level of the brainstem
- Indications
o Management of acute painful musculoskeletal conditions associated with muscle spasms
o Relief of painful musculoskeletal conditions: muscle spasms, management of spasticity of severe chronic disorders
o Work best when used along with physical therapy
- Contraindications
o Hypersensitivity; should not be used with MAO inhibitor therapy
- Adverse Effects
o CNS effects high incidence, some serious
o Euphoria, lightheadedness, dizziness, drowsiness, fatigue, muscle weakness
o EENT: dry mouth, blurred vision
o CV: arrhythmias
o Reduction in muscle spasm and hyperactivity without loss of function
- Interactions
o Additive CNS depression with other CNS depressants including alcohol, antihistamines, opioid analgesics and
sedatives/hypnotics
- Nursing assessment
o Assess for pain and mobility
CNS Depressants (Benzodiazepines, Barbiturates):

Diazepam (Valium) – Long Acting
o Depress CNS activity
o Benzodiazepine receptors GABA is an inhibitory neurotransmitter that inhibits overstimulation
o Produces skeletal muscle relaxation by inhibiting spinal polysynaptic afferent ways
- Indications
o Sedation, sleep induction, skeletal muscle relaxation, anxiety relief, anxiety-related depression, treatment of acute seizure
disorders, treatment of alcohol withdrawal, agitation relief, balanced anesthesia, moderate or conscious sedation
o Calming effect on the CNS, useful in controlling agitation and anxiety, reduce excessive sensory stimulation, inducing
sleep, induce skeletal muscle relaxation
- Contraindications
o Hypersensitivity, cross-sensitivity with other benzodiazepines may occur
- Adverse Effects
o CNS depression usually with alcohol or other CNS depressant drugs, hypotension, addiction  withdrawal syndrome, fall
risk especially in elderly
o Relief of anxiety, sedation, amnesia, skeletal relaxation, decreased seizure activity
o Flumazenil is an adjunct in the management in toxicity or overdose
- Interactions
o Use with opioids other CNS depression including alcohol, antihistamines, opioid analgesics and sedatives/hypnotics may
cause profound sedation
o Pain and mobility
Lorazepam (Ativan) – Intermediate Acting Benzodiazepine
o Depresses the CNS, probably by potentiating GABA, an inhibitory neurotransmitter
o Depress CNS activity
o Benzodiazepine receptors GABA is an inhibitory neurotransmitter that inhibits overstimulation
- Indications
o Sedation, sleep induction, skeletal muscle relaxation, anxiety relief, anxiety-related depression, treatment of acute seizure
disorders, treatment of alcohol withdrawal, agitation relief, balanced anesthesia, moderate or conscious sedation
- Contraindications
o Hypersensitivity, cross-sensitivity with other benzodiazepines may occur
- Adverse Effects
o CNS depression usually with alcohol or other CNS depressant drugs, hypotension, addiction  withdrawal syndrome, fall
risk especially in elderly
o CNS: dizziness, drowsiness, lethargy
o EENT: blurred vision
o CV: apnea, cardiac arrest
o Sedation, decreased anxiety, decreased seizures
o If overdose occurs, flumazenil is the antidote
- Interactions
o Use with other CNS depression including alcohol, antihistamines, opioid analgesics and sedatives/hypnotics may cause
profound sedation
o Pain and mobility
Phenobarbital – Long Acting Prototypical Barbiturate
o CNS depression
o Site of action: brainstem (reticular formation)
o By potentiating the action of GABA, nerve impulses traveling in the cerebral cortex are inhibited
- Indications
o Treat anxiety, seizures, migraines and alcohol poisoning
o Can be highly addictive and extremely dangerous if mismanaged
o Prevention of generalized tonic-clonic seizures and febrile convulsions, hyperbilirubinemia in neonates, rarely used as
sedative, no longer recommended as a hypnotic
o Long acting
 Seizure prophylaxis
- Contraindications
o Hypersensitivity; comatose patients or those with pre-existing CNS depression
- Adverse Effects
o Lethargy, confusion, lack of coordination, vomiting, reduced REM sleep, respiratory arrest, tolerance and dependence
o Anticonvulsant activity, sedation
o Slurred speech, shallow breathing, kidney failure, coma, death
o Serum phenobarbital levels may be monitored when used as ab anticonvulsant
- Tolerance and Withdrawal
o Similar w/d to alcohol, do not stop abruptly
o Panic attacks, uncontrollable shakiness, seizures
- Interactions
o Use with other CNS depression including alcohol, antihistamines, opioid analgesics and sedatives/hypnotics may cause
profound sedation
o Pain and mobility
Flumazenil – Antidote (Reversal Agent)
o Flumazenil is a benzodiazepine derivative that antagonizes the CNS depressant effects of benzodiazepine compounds
- Indications
o Complete/partial reversal effects of benzodiazepines used as general anesthetics, during diagnostic or therapeutic
procedures
- Contraindications
o Hypersensitivity to flumazenil or benzodiazepines
- Adverse Effects
o CNS: seizures, dizziness, agitation, confusion, drowsiness, fatigue, headache, sleep disorders
o EENT: abnormal hearing, abnormal vision
o Reversal of benzodiazepine effects
o Assess level of consciousness and respiratory status before and during therapy, observe patient for at least 2 hours after
administration for the appearance of resedation (hypoventilation may occur)
Antianxiety:
Buspirone (Miscellaneous Anxiolytic)
o Binds to serotonin and dopamine receptors in the brain and increases norepinephrine metabolism in the brain
- Indications
o Management of anxiety
- Contraindications
- Interactions
o Do not give with MAO inhibitors
o Grapefruit juice increases serum levels
- Adverse Effects
o Paradoxical anxiety, dizziness, blurred vision, headache, nausea
o Relief of anxiety
o Assess degree of manifestation of anxiety before and periodically during therapy
o Do not give with MAO inhibitors
Diazepam, Lorazepam (benzodiazepines)
(In CNS depressant section)
Antidepressants:
Amitriptyline – Tricyclic Antidepressant (TCA)
o Blocks serotonin and norepinephrine reuptake and potentiates the effect of these two in the CNS
- Indications
o Depression
- Contraindications
o Angle-closure glaucoma
- Adverse Effects (greater incidence in higher doses)
o QT prolongation
o Confusion
o Sedation
o NMS
o Fractures
o Antidepressant action
- Safety
o Black box warning – all antidepressants
 Suicide risk increased with patients < 24 years old
o Elders at greater risk for ARDs, especially CV
o QT interval, especially with higher doses, elders
o Patient and family teaching: alert to suicide risk – all antidepressants
o Suicide risk
Fluoxetine (Prozac) – Selective Serotonin Reuptake Inhibitor (SSRI)
o Inhibits serotonin reuptake in brain
- Indications
o Major depressive disorder, OCD, bulimia nervosa, panic disorders
- Contraindications
- Adverse Effects
o Anxiety, dizziness, drowsiness, headache, insomnia
o Antidepressant action, decreased behavior associated with panic disorders and bulimia
- Safety
o Black box warning
o Mood changes, assess for suicidal tendencies, monitor appetite
o Patient teaching – similar to other antidepressant medications
o Suicide risk, serotonin syndrome
Venlafaxine (Effexor XR) – Selective Serotonin/Norepinephrine Reuptake Inhibitor (SNRI)
o Inhibits serotonin and norepinephrine reuptake in the CNS
- Indications
o Major depressive disorder, generalized anxiety disorder, social anxiety disorder, panic disorders
- Contraindications
o Hypersensitivity; concurrent use of MAO inhibitors
- Adverse Effects
o CNS: abnormal dreams, anxiety, dizziness, headache, insomnia, nervousness, weakness, abnormal thinking
o GI: abdominal pain, altered taste, anorexia, constipation, diarrhea, dry mouth
o Decrease depressive symptomatology, with fewer relapses/recurrences, decreased anxiety, decrease in panic attacks
o Assess suicidal tendencies, assess for serotonin syndrome, assess mental status and mood changes
Phenalzine – Nonselective Monoamine Oxidase Inhibitors (MAOIs)

- Ingestion of foods or drinks with tyramine leads to hypertensive crisis, which may lead to cerebral hemorrhage, stroke, coma, or death
- Avoid foods that contain tyramine!
- Aged, mature cheeses (cheddar, bleu, Swiss)
- Smoked, pickled, or aged meats, fish, poultry (herring, sausage, corned beef, salami, pepperoni, pâté)
- Yeast extracts
- Red wines (Chianti, burgundy, sherry, vermouth)
- Italian broad beans (fava beans)
- Potential to cause hypertensive crisis
Bupropion – Miscellaneous Anxiolytic NDRI
o Decreases neuronal reuptake of dopamine in the CNS
- Indications
o Treatment of depression (with psychotherapy)
- Contraindicated
o Hypersensitivity; concurrent use of MAO inhibitors
- Adverse Effects
o CNS: homicidal thoughts/behaviors, seizures, suicidal thoughts and behaviors, agitation, headache
o CV: hypertension
o GI: dry mouth, nausea, vomiting
o Diminished depression, decreased craving of cigarettes
o Monitor mood changes, asses mental status and mood changes
- Originally indicated for treatment of depression; now also indicated as an aid in smoking cessation
- Sometimes added as an adjunct antidepressant for patients experiencing sexual adverse effects secondary to SSRI therapy
- Sustained Release Bupropion (zyban): approved for smoking cessation treatment and was the first nicotine-free prescription medicine
used to treat nicotine dependence
Mood Stabilizing:
Lithium
o Alters cation transport in nerve and muscle and may also influence reuptake of neurotransmitters
- Indications
o Drug of choice for the treatment of mania
 Narrow therapeutic range: acute mania—lithium serum level of 1 to 1.5 mEq/L; maintenance serum levels
should range between 0.6 and 1.2 mEq/L
 Levels exceeding 1.5 to 2.5 mEq/L begin to produce toxicity, including gastrointestinal (GI) discomfort, tremor,
confusion, somnolence, seizures, and possibly death.
 Keeping the sodium level in the normal range (135 to 145 mEq/L) helps to maintain therapeutic lithium levels.
o Manic episodes of bipolar I disorder
- Contraindications
o Dehydration, known sodium imbalance, cardiovascular disease, renal dysfunction
- Adverse Effects
o Cardiac dysrhythmia, hyponatremia
o GI discomfort, tremor, somnolence, seizures
o CNS: seizures, fatigue, headache, impaired memory
o CV: ECG changes
o Prevents/decreases incidence of acute manic episodes
o Monitor serum lithium levels twice daily during initiation of therapy
o Assess mental status, monitor I/O ratios, evaluate renal and thyroid function, assess patient for signs and symptoms of
lithium toxicity
Antipsychotics:
Haloperidol – Typical Antipsychotic, Butyrophenones
o Blocks impulse transmission of dopaminergic neurons and alters the effect of dopamine in the CNS
- Indications
o Acute and chronic psychotic disorders including: schizophrenia, manic states, drug-induced psychoses
- Contraindications
o Hypersensitivity; angle-closure glaucoma
- Adverse Effects
o Higher incidence of extrapyramidal effects
o Lower incidence of CV effects
o High incidence of QT prolongation with IV administration
o Neuroleptic malignant syndrome (NMS)
o Neuroleptic malignant syndrome-high fever, unstable vitals
o Extrapyramidal effects-involuntary movements similar to Parkinson’s disease
o Tardive dyskinesia-involuntary contractions of the face and mouth and dancing movements of the extremities
o Diminished signs and symptoms of psychoses, improved behavior in children with Tourette’s syndrome or other
behavioral problems
- Safety
o Black Box Warning-increased death in older adult with dementia, increased suicide in young
o FDA withdrew approval of IV use
o Elders – decrease dosage
o Cognitive functioning, ECG, CBC, monitor for effects
 Therapeutic window
 Extrapyramidal effects
 May occur in first few days, then resolve
 May be dose related
 May be controlled by Parkinson drugs
 NMS
 Discontinue immediately
Risperidone – Atypical Antipsychotic, Benzisoxazoles
o May act by antagonizing dopamine and serotonin in the CNS
- Indications
o Schizophrenia, bipolar mania, autistic disorder
- Contraindications
o Hypersensitivity to risperidone or paliperidone
- Adverse Effects
o Prolonged QT interval, sudden cardiac death, extrapyramidal effects, dizziness, tiredness, fatigue, GI disturbance
o Neuroleptic malignant syndrome-high fever, unstable vitals
o Extrapyramidal effects-involuntary movements similar to Parkinson’s disease
o Tardive dyskinesia-involuntary contractions of the face and mouth and dancing movements of the extremities
o Decreased symptoms of psychoses, bipolar mania, or autism
- Safety
o Increased risk of death for elderly being treated with antipsychotics, not approved for use in dementia-related psychosis
Antiepileptic:
Phenobarbital – Barbiturate
o Produces all levels of CNS depression. Depresses the sensory cortex, decreases motor activity, and alters cerebellar
function
- Indications
o Anticonvulsant in tonic-clonic (grand mal), partial, and febrile seizures in children
- Contraindications
o Hypersensitivity; comatose patients or those with pre-existing CNS depression
- Adverse Effects
o CNS: hangover, delirium, depression, drowsiness, excitation, lethargy, vertigo
o Resp: respiratory depression, laryngospasm, bronchospasm
o CV: hypotension
o Anticonvulsant activity, sedation
o Serum phenobarbital levels may be monitored when used as an anticonvulsant
o Monitor respiratory status, pulse, and BP and signs and symptoms of angioedema
o Prolonged therapy may lead to psychological or physical dependence, monitor serum folate concentrations
Phenytoin (Dilantin) – Hydantoin Anti-Convulsant

o Affects ion movement in neurons, stabilizing the seizure threshold
- Indications
o Treatment/prevention of tonic-clonic (grand mal) seizures and complex partial seizures
- Contraindications
o Hypersensitivity; hypersensitivity to propylene glycol
- Adverse Effects
o Rash, gingival hyperplasia, CNS disturbances – lethargy, confusion
o More adverse effects with long term use
 Acne, hirsutism, osteoporosis
o IV site necrosis – use fosphenytoin
o Diminished seizure activity, termination of ventricular arrhythmias
o Monitor serum phenytoin levels routinely
- Safety
o Black box warning IV administration – severe hypotension if given too fast
o Neonates at risk for bleeding
o Pregnant mother needs to be seizure free during pregnancy
o Phenytoin levels
o Good oral hygiene, PO – shake suspension well, IV – very irritating to veins, IV Fosphenytoin – dilute to less than 25
mg/mL and maximum infusion rate 150 mg/mL
o Patient teaching: oral hygiene, take around the clock, do not stop suddenly
o Seizures, drug levels
Antiparkinson:
Carbidopa–Levodopa (Sinemet) – Dopaminergic Agonist
o Levodopa converted to dopamine in brain, replaces depletion. Carbidopa inhibits initial breakdown of levodopa and allows
for much lower doses of levodopa to be used
- Adverse Effects
o Palpitations, hypotension, urinary retention, dyskinesia
- Safety
o Orthostatic hypotension precautions
o Symptoms – worsening or change in motor symptoms may indicate toxicity
o Don’t give with high protein meals
o Patient teaching: increase fluid intake, don’t suddenly stop taking, dosing needs may/will change
o Symptoms, kidney and liver function labs

Adrenergic and Cholinergic Drugs: Mechanisms, Indications and Nursing Assessment

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Adrenergic and Cholinergic Drugs: Mechanisms, Indications and Nursing Assessment

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Adrenergic Drugs:

Dopamine – Alpha and Beta Agonists

Methadone – Synthetic Opioid Analgesic

CNS Depressants (Benzodiazepines, Barbiturates):

Phenalzine – Nonselective Monoamine Oxidase Inhibitors (MAOIs)

Phenytoin (Dilantin) – Hydantoin Anti-Convulsant

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