Module 1

Chpt 11 - Anesthetics

General Anesthetics

  • Alters CNS nerve impulses to reduce pain and other sensations

  • Complete loss of consciousness and respiratory drive depression

  • Types

    • Inhalation (Ex: Laughing gas in dental procedures)

    • Parenteral

    • Adjunct - Enhances clinical therapy when used simultaneously with another drug


Overton-Meyer Theory

  • Potency of anesthetics varies with lipid solubility

  • Fat-soluble drugs are more potent than water-soluble drugs because they easily cross the blood-brain barrier

  • Progression reduction of cerebral and spinal sensory function


Indications

  • Used during surgical procedures to produce:

    • Unconsciousness

    • Skeletal muscular relaxation

    • Visceral smooth muscle relaxation

Contraindications

  • Known drug allergy

  • Depending on drug type

    • Pregnancy

    • Narrow-angle glaucoma (causes increased intraocular pressure)

    • Acute porphyria (Metabolic disorder; triggers severe attacks)

    • Known history of malignant hyperthermia


Effects of Inhaled and IV General Anesthetics

Organ/System

Reaction

Respiratory system

Impaired o2, depressed airway-protective mechanisms, airway irritation and possible laryngospasm

Cardiovascular system

Depressed myocardium, hypotension and tachycardia, bradycardia in response to vagal stimulation

Cerebrovascular system

Increased intracranial pressure

Gastrointestinal system

Reduced hepatic blood flow and thus reduced hepatic clearance

Renal system

Decreased glomerular filtration rate

Skeletal Muscles

Skeletal muscle relaxation

Cutaneous circulation

Vasodilation

CNS

CNS depression; blurred vision; nystagmus; progression of CNS depression to decreased alertness, sensorium, and decreased consciousness


Adverse Effects

  • Vary according to dosage and drug used

  • Sites primarily affected

    • Heart, peripheral circulation, liver, kidneys, respiratory tract

  • Myocardial depression is commonly seen

  • Malignant Hyperthermia

    • Occurs during or after volatile inhaled general anesthesia or use of th neuromuscular blocking drug (NMBD) succinylcholine

    • Sudden elevation in body temp (greater than 104 F)

    • Tachypnea, tachycardia, muscle rigidity

    • Life-threatening emergency

    • Treated with cardiorespiratory supportive care and dantrolene (skeletal muscle relaxant - administered via IV and looks like a bright orange tang juice)

  • Toxicity and management of overdose

    • In large doses, anesthetics are potentially life threatening

    • Cardiac and respiratory arrest ultimate causes of death in an overdose

    • Administered in a controlled environments

  • General anesthetics: interactions

    • Antihypertensives: increased hypotensive effecfts

    • Beta blockers: increased myocardial depression


Anesthetics

Drug Name

Classification and Schedule

Key Notes

Dexmedetomidine (Precedex)

Alpha 2-adrenergic receptor agonist

Sedation, reduced anxiety, analgesia without respiratory depression. Short duration, quick awakening

Ketamine

General anesthetic

General anesthesia, moderate sedation. Rapid onset, lower cardiovascular impact. May cause hallucinations

Nitrous Oxide (aka laughing gas

Inhaled general anesthetic

Weakest anesthetic, mainly used for dental procedures or as a supplement

Propofol (Diprivan)

Parenteral general anesthetic

Indication/maintenance of anesthesia. Sedation in ICU. Monitor triglycerides if used with TPN

Sevoflurane (Ultane)

Inhaled general anesthetic

Rapid onset/elimination. Nonirritating, useful in outpatient and pediatric surgeries


Moderate Sedation

  • Also called conscious sedation or procedural sedation

  • Does not cause complete loss of consciousness and does no normally cause respiratory arrest

  • Combination of an IV benzodiazepine (e.g., midazolam) or propofol and an opiate analgesic (e.g., fentanyl or morphine)


Local Anesthetics

  • Topical

    • Applied directly to skin or mucous membranes

    • Creams (ex: Emla to numb the skin), solutions, ointments, gels, ophthalmic drops, powders, suppositories

  • Parenteral

    • Injected IV or into the CNS by various spinal injection techniques

Types

  • Spinal or intraspinal

  • Infiltration

  • Nerve block

  • Topical

  • Peripheral nerve catheter attached to a pump containing the local anesthetic: Pain Buster and On-Q pump

Medications

  • Lidocaine

  • Bupivacaine

  • Chloroprocaine

  • Mepivacaine

  • Prilocaine

  • Procaine

  • Propoxycaine

  • Ropivacaine

  • Tetracaine


Drug Effects: Paralysis

  • First, autonomic activity is lost

  • Then pain and other sensory functions are lost

  • Last, motor activity is lost.

  • As local drugs wear off, recovery occurs in reverse order (motor, sensory, then autonomic activity are restored)


Indications for Local Anesthesia

  • Used for:

    • Surgical, dental, and diagnostic procedures

    • Treatment of certain types of chronic pain

    • Spinal anesthesia: to control pain during surgical procedures and childbirth

  • Local anesthetics are given by:

    • Infiltration anesthesia

    • Nerve block anesthesia

Adverse Effects

  • Usually limited

  • Adverse effects results if:

    • Inadvertent IV injection

    • Excessive dose or rate of injection

    • Slow metabolic breakdown

    • Injection into highly vascular tissue

    • Allergy

      • Generally limited

      • Most common with “ester type” anesthetics

  • Spinal headache

    • 70% of patients who either experience inadvertent dural puncture during epidural anesthesia or undergo intrathecal anesthesia

      • Causes severe, postural headache (specifically when sitting up)

    • Usually self-limiting

    • Treatment: bed rest, analgesics, caffeine

      • Blood patch for severe cases (small amount of pt’s blood and injected into pt’s injection hole)


Neuromuscular Blocking Drugs

  • Also known as NMBDs

  • Prevent nerve transmission in muscle, resulting in muscle paralysis including those required to breathe

  • Used with anesthetics (as adjuncts for things like intubation) during surgery

  • Respiratory muscle paralysis occurs with these drugs

  • Does not cause an sedation (sedative needed)

  • Emergency ventilation equipment must be immediately available

  • Indications

    • Main use: facilitating controlled ventilation during surgical procedures

    • Endotracheal intubation (short acting)

    • To reduce muscle contraction in an area that need surgery

  • Contraindications

    • Malignant hyperthermia

      • Antidotes: anitcholinesterase

  • Two Categories

    • Depolarizing (Succinylcholine): Works similarly to neurotransmitter acetylcholine (ACh), causing depolarization

      • Succinylcholine isn’t broken down quickly, causing prolonged depolarization and preventing further muscle contractions

      • Used for rapid sequence intubation and short surgical procedures

    • Rocuronium: Rapid-to-intermediate acting

      • Rocuronium blocked ACh at the neuromuscular junction; can also lead to paralysis


Nursing Implications

  • Preop

    • Assess past surgeries and anesthesia response

    • Review allergies, medications, and medical history

    • Evaluate alcohol, illicit drug, and opioid use

  • Intraoperative

    • Vital signs

    • perform baseline lab tests and ECG

    • Ensure ABCs

    • Monitor all body systems

  • Postop

    • Watch for cardiovascular and respiratory depression

    • Identify anesthesia-related complications

    • Implement safety measures if motor/sensory loss occurs


Chpt 10 - Analgesics

Analgesics

  • Medications the relieve pain without causing loss of consciousness

  • “Painkillers”

  • Opioid analgesics

  • Adjuvant analgesic drugs


Pain

  • An unpleasant sensory and emotional experience associated with actual or potential tissue damage

  • A person and individual experience

  • Pain involved:

    • Physical factors

    • Psychologic factors

    • Cultural factors


Key Terms

  • Pain Tolerance: Amount of pain a person can endure without it interfering with normal function

  • Pain Threshold: Level of stimulus needed to produce the perception of pain

  • Nociception: Pain results from stimulation of sensory nerve fibers called nociceptors


Classification by Onset and Duration

  • Acute:

    • Sudden onset

    • Usually subsides once treated

  • Chronic:

    • Persistent or recurring

    • Lasts 3 to 6 months

    • Often difficult to treat

    • Tolerance of meds

    • Physical dependence of meds


Gate Theory of Pain Transmission

  • Most common and well-described theory

  • Uses the analogy of a gate to describe how impulses from damaged tissues are sensed in the brain

  • Many current pain management strategies are aimed at altering this system


Pain Transmission

  • Tissue injury causes the release of the following (all cause inflammatory response and pain):

    • Bradykinin

    • Histamine

    • Potassium

    • Prostaglandins

    • Serotonin

  • Body has endogenous neurotransmitters (that we make in our body to fight pain)

    • Enkephalins

    • Endorphins


Stopping Pain Transmission

  • Rubbing a painful area with massage or liniment stimulates large sensory fibers

  • Result

    • Closes gate

    • Reduces transmission


Adjuvant Drugs

  • Assist primary drugs in relieving pain

    • NSAIDS

    • Antidepressants

    • Anticonvulsants

    • Corticosteroids

  • Example: Adjuvant drugs for neuropathic pain

    • Amitriptyline (antidepressant)

    • Gabapentin or pregabalin (anticonvulsants)


World Health Organization: Three-Step Analgesic Ladder

  • Step 1: Nonopioids (with or without adjuvant medications) after the pain has been identified and assessed. If pain persists or increases, treatment moves to…

  • Step 2: Opioids with or without nonopioids and with or without adjuvants. If pain persists or increases, management then rises to

  • Step 3: Opioids indicated for moderate to severe pain, administered with or without nonopioids or adjuvant medications


Opioid Analgesics: Mechanism of Action

  • Three classification based on their actions

    • Agonists (Morphine, fentanyl): Activate opioid receptors and produce strong analgesic effect for pain management

    • Agonists-antagonists (Pentazocine, nalbuphine): Partially activate opioid receptors while blocking others for moderate pain relief and lower risk of respiratory depression or addiction

    • Antagonists (Naloxone, Naltrexone): Block opioid receptors to reverse overdoses of opioids (not for actual pain relief)


Opioid Drugs

  • Mild Agonists (moderate pain relief) (found in prescription pain meds and cough syrups)

    • Codeine

    • Hydrocodone

  • Strong Agonists (severe pain relief)

    • Morphine

    • Hydromorphone

    • Oxycodone

    • Meperidine

    • Fentanyl

    • Methadone


Equianalgesia

  • Ability to provide equivalent pain relief by calculating dosages of different drugs or routes of administration that provide comparable analgesia

  • Hydromorphone (Dilaudid): 7x more potent than morphine


Opioid Analgesics

  • Indications

    • Alleviate moderate to severe pain

    • Often given with adjuvant analgesics drugs to assist primary drugs with pain relief

  • Also used for:

    • Cough center supression

    • Treatment of diarrhea

    • Balanced anesthesia

  • Contraindications

    • Known drug allergy

    • Severe asthma

  • Use with extreme caution in patients with:

    • Respiratory insufficiency

    • Elevated intracranial pressure

    • Morbid obesity or sleep apnea

    • Paralytic ileus

    • Pregnancy

  • Adverse Effects

    • CNS depression

      • Leads to respiratory depression

      • Most serious adverse effect

    • Nausea and vomiting

    • Urinary retention

    • Diaphoresis and flushing

    • Pupil constriction (miosis)

    • Constipation

    • Itching


Opioid Tolerance

  • A common physiologic result of chronic opioid treatment

  • Result: Larger dose to maintain same level of analgesia


Physical Dependence (not psychologic)

  • Physiologic adaptation of the body to the presence of an opioid

  • Opioid tolerance and physical dependence are expected with long-term opioid treatment and should not be confused with psychologic dependence (addiction)


Psychologic Dependence

  • Pattern of compulsive drug use characterized by a continued craving for an opioid and the need to use the opioid for effects other than pain relief


Toxicity and management of Overdose

  • Opioid withdrawal or opioid abstinence syndrome

  • Manifested as:

    • Anxiety, irritability, chills and hot flashes, joint pain, lacrimation, rhinorrhea, diaphoresis, nausea, vomiting, abdominal cramps, diarrhea, confusion


Interactions

  • Alcohol

  • Antihistamines

  • Barbiturates

  • Benzodiazepines

  • Monoamine oxidase inhibitors

  • Others


Naloxone Hydrochloride (Narcan)

  • Pure opioid antagonist

  • Drug of choice for the complete or partial reversal of opioid-induced respiratory depression

  • Indicated in cases of suspected acute opioid overdose

  • Failure of the drug to significantly reverse the effects of the presumed opioid overdose indicates that the condition may not be related to opioid overdose

Management of Overdose

  • Naloxone now available without a prescription and is being used by 1st responders for opioid/illegal drug overdoses

  • Naltrexone

    • Opioid antagonist

    • Oral form

    • Used for alcohol and opioid addiction

Assessment

  • Thorough H&P

  • Thorough Pain assessment

Nursing Implications

  • Be sure to medicate patients before the pain becomes severe so as to provide adequate analgesia and pain control

  • Pain management includes pharmacologic and nonpharmacologic approaches; be sure to include other interventions as indicated

  • Take with food

  • Ensure safety measures (beware of falls)

  • Withhold dose and contact physician if there is a decline in the patient’s condition

  • Check dosages carefully

  • Constipation

  • Orthostatic hypotension

  • Monitor for:

    • Adverse effects

      • Vital sings change, patient’s condition declines, or pain continues

      • Respiratory depression

    • Therapeutic Effects

      • Decreased complaints of pain

      • Decreased severity of pain

      • Increased ability to perform ADL’s


Chpt 12 - CNS Depressants and Muscle Relaxants

CNS Depressants

  • aka Sedatives

    • Drugs that have an inhibitory effect on the CNS to the degree taht they reduce:

      • Nervousness

      • Excitability

      • Irritability

  • Hypnotics

    • Cause sleep

    • Much more potent effect on CNS than sedatives

    • A sedative can become a hypnotic if it is given in large enough doses

  • Sedative-hypnotics: dose dependent

    • At low doses, calm the CNS without inducing sleep

    • At high doses, calm the CNS to the point of causing sleep

    • Classified into three main groups

      • Barbiturates

      • Benzodiazepines (many end in pam)

      • Miscellaneous drugs


Sleep

  • Transient, reversible, and periodic state of rest

    • Decrease in physical activity and consciousness

  • Normal sleep is cyclic and repetitive

    • Sleep architecture - characterized by different brainwave patterns

      • R.E.M. sleep (causes dreams and muscles are paralyzed)

        • Said that it helps emotional regulation and consolidates memories

      • Non-rem sleep (3 Stages - N1, N2, N3)

        • N1 - Transition from wakefulness to sleep

        • N2 - Light sleep

        • N3 - Deep sleep

      • Stress, alcohol, some meds can affect REM sleep

      • After a period of REM sleep deprivation, individuals often will experience REM rebound where the proportion and intensity of REM sleep increases

  • A sleeping person is unaware of sensory stimuli within the immediate environment


Benzodiazepines

  • Most commonly prescribed sedative-hypnotic drug

  • Nonbenzodiazepines are currently more frequently prescribed for people who can’t sleep

  • Favorable adverse effect profiles, efficacy, and safety when used appropriately

  • Classified as either sedative-hypnotic (calm or sedate for sleeping purposes) and anxiolytics (treats anxiety)

  • Mechanism of Action

    • Depress CNS activity

    • Affect hypothalamic, thalamic, and limbic systems of the brain

    • Benzodiazepine receptors

      • closely linked (enhance)to the activity of Gamma-aminobutyric acid (GABA)

        • GABA is the brain’s major inhibitory neurotransmitter

    • Do not suppress rapid eye movement (REM) sleep as much as barbiturates do (to prevent grogginess and poor sleep quality)

    • Do not increase metabolism of other drugs

  • Drug Effects

    • Calming effect on the CNS

    • Useful in controlling agitation and anxiety

    • Reduce excessive sensory stimulation, inducing sleep

    • Induce skeletal muscle relaxation (for muscle spasms and muscle tension)

  • Indications

    • Sedation

    • Sleep innduction

    • 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

    • Drug allergy

    • Narrow-angle glaucoma

    • Pregnancy

  • Adverse Effects (Mild and Infrequent)

    • Headache

    • Drowsiness

    • Dizziness

    • Cognitive Impairment

    • Vertigo

    • Lethargy

    • Fall hazard for older adults

    • “Hangover” effect or day time sleepiness

  • Toxicity, Overdose and Interactions

    • Somnolence, Confusion, Coma, Diminished reflexes

    • Do not cause hypotension and respiratory depression unless taken with other CNS depressants

    • Treatment symptomatic and supportive

      • Flumazenil as an antidote

    • Interactions: things metabolized by the liver, opioids, Etoh, azoles, herbals, high protein

  • Common Benzodiazepines

    • Diazepam (Valium): first clinically available benzo used for anxiety, anesthesia adjunct, anticonvulsant and muscle relaxer (PO, IM, PR)

    • Midazolam (Versed): used for sedation, causes amnesia (IV, Liquid peds)

    • Temazepam (Restoril): intermediate acting, metabolite of diazepam, sleep inducted 20-40 min

    • Eszopiclone (Lunesta): First hynotic to be FDA approved

    • Ramelteon (Rozerem): Structurally similar to the hormone melatonin: works as an agonist at melatonin receptors in the CNS

    • Zolpidem (Ambien): Lower incidence of daytime sleepiness compared with benzodiazepine hypnotics


Barbiturates

  • First introduced in 1903; were the standard drugs for insomnia and sedation

  • Habit forming; low therapeutic index

  • Only a few are commonly used today partly because of the safety and efficacy of benzodiazepines

  • Indications

    • Ultrashort acting

      • Anesthesia for short surgical procedures

      • Anesthesia induction

      • Control of convulsions

      • Reduction of intracranial pressure in neurologic patients

    • Short acting

      • Sedation and control of convulsive conditions

    • Intermediate acting

      • Sedation and control of convulsive conditions

    • Long acting

      • Epileptic seizure prophylaxis

  • Contraindications

    • Drug Allergy

    • Pregnancy

    • Significant respiratory difficulties

    • Sever kidney or liver disease

    • Caution in older adults

  • Toxicity and Overdose

    • Overdose frequently leads to respiratory depression and subsequent respiratory arrest

    • Overdose produces CNS depression (sleep to coma and death)

    • Can be therapeutic

      • Anesthesia induction

      • Uncontrollable seizures or severe head injury: “phenobarbital coma”

    • Treatment of overdose

      • Symptomatic and supportive

      • Maintain adequate airway

      • Assisted ventilation and oxygen therapy

      • Fluids

      • Pressor support

      • Urine alkalization (raising urine pH) to hasten elimination

  • Interactions

    • Additive effects

      • Alcohol, antihistamines, benzodiazepines, opioids, tranquilizers

    • Inhibited metabolism

      • MAOIs prolong the effects of barbiturates

    • Increased metabolism (enzyme inducers)

      • Reduces anticoagulant response, leading to possible clot formation

  • Drugs

    • Pentobarbital (Nembutal)

      • Long acting drug

      • Uses:

        • Preoperatively to relieve anxiety and provide sedation

        • occasionally to control status epilepticus

        • No longer used as a sedative hypnotic drug for insomnia

    • Phenobarbital

      • Prototypical barbiturate

      • Long acting

      • Uses

        • Prevention of generalized tonic-clinic seizures

        • Hyperbilirubinemia in neonates

        • Rarely used as a sedative

        • No longer recommended as a hypnotic


OTC Hypnotics

  • Nonprescription sleeping aids often contain antihistamines, which have CNS depressant effect

  • Doxylamine (Unisom) and diphenhydramine (Sominex / Benadryl), acetaminophen/diphenhydramine (Extra Strength Tylenol PM); melatonin

  • As with other CNS depressants, concurrent use of alcohol can cause respiratory depression or arrest


Muscle Relaxants MOA

  • Act to relieve pain associated with skeletal muscle spasms

  • Resemble GABA

    • Binds to GABA receptors and enhance sedation

  • Indications

    • Relief of painful musculoskeletal conditions

    • Work best when used along with physical therapy

  • Adverse Effects

    • Extension of effects on CNS and skeletal muscles

      • Euphoria

      • Lightheadedness

      • Dizziness

      • Drowsiness

      • Fatigue

      • Muscle weakness

  • Toxicity and Management of Overdose

    • Primarily involve the CNS

    • No specific antidote or reversal

    • If taken along with other CNS depressants

      • Adequate airway must be maintained

      • EKG monitoring

      • Administer fluids to avoid crystalluria

    • Caution with other CNS depressants

      • Benzodiaepines

      • Alcohol

  • Common Muscle Relaxants

    • Baclofen (Lioresal)*

    • Cyclobenzaprine (Flexeril)*

    • Dantrolene (Dantrium)*

    • Metaxalone (Skelaxin)

    • Tizanidine (Zanaflex)

    • Carisoprodol (Soma)

    • Chlorzoxazone (Paraflex)

    • Methocarbamol (Robaxin)


Nursing Implications

  • Before beginning therapy, obtain a thorough history regarding allergies, use of other medications, health history, and medical history

  • Obtain baseline vital signs and I&O, including supine and erect blood pressure

  • Assess for potential disorders and conditions that may be contraindications and for potential drug interactions

  • Give hypnotics 30 to 60 min before bedtime

  • Most benzodiazepines cause REM rebound

  • Instruct patients to avoid alcohol and other CNS depressants

  • Check with the prescriber before taking any other medications, including over-the-counter medications

  • Rebound insomnia may occur for a few nights after a 3 to 4 week regimen has been discontinued

  • Safety is important:

    • Keep side rails up or use bed alarms

    • Do not permit smoking

    • Assist patient with ambulation

    • Keep call light within reach

  • Monitor adverse effects

  • Age appropriate considerations

  • Monitor for therapeutic effects

    • Increased ability to sleep at night

    • Fewer awakenings

    • Shorter time for falling asleep

    • Few adverse effects, such as “hangover” effects

    • Improved sense of well-being because of improved sleep

    • For muscle relaxants: decrease spasticity, decreased rigidity


Chpt 13 - CNS Stimulants, and Related Drugs

CNS Stimulants

  • Drugs that stimulate a specific area of the brain or spinal cord

  • Neurons contain receptors for excitatory neurotransmitters, including dopamine (dopaminergic drugs), norepinephrine (adrenergic drugs), and serotonin (serotonergic)

  • “Sympathomimetic drugs”


Classification

  • Classified according to

    • Chemical structural similarities, amphetamines, serotonin agonists, sympathomimetics, and xanthines

    • Site of therapeutic action in the CNS

    • Major therapeutic uses: attention deficit hyperactivity disorder, antinarcoleptic, anorexiant, antimigraine, and analeptic drugs


Indications

  • ADHD

  • Narcolepsy

  • Obesity

  • Migraine

  • Analeptic Responsive type Syndromes


ADHD

  • Most common psychiatric disorder in children, affection 10.8% of school-age children

  • Boys are affected more often than girls (but girls may be underdiagnosed)

  • Primary symptoms of ADHD are inappropriate ability to maintain attention span (when things are boring to the person) or the presence of hyperactivity and impulsivity

  • Drug therapy for both childhood and adult ADHD is the same


Narcolepsy

  • Incurable neurologic condition in which patients unexpectedly fall asleep in the middle of normal daily activities. These “sleep attacks” are reported to cause car accidents or near-misses in 70% or more of patients

  • Cataplexy: sudden acute skeletal muscle weakness. Associated symptoms in at least 70% of narcolepsy cases. It involves sudden acute skeletal muscle weakness


Obesity

  • According to the National Institutes of Health and the Centers for Disease Control and Prevention, approximately 42.2% of Americans are obese

    • Higher incidence in women and minorities

  • Many associated health risks


Migraine

  • Common type of recurring headache, usually lasting from 4 to 72 hours

  • Typical features: pulsatile quality with pain that worsens with each pulse

  • Most commonly unilateral but may occur on both sides of the head

  • Associated symptoms: nausea, vomiting, photophobia (avoidance of light), and phonophobia (avoidance of sounds)

  • Aura


Analeptic-Responsive Respiratory Depression Syndromes

  • Neonatal apnea

    • Common in 70% of premature infants born before 34 weeks’ gestation

  • Bronchopulmonary dysplasia

  • Postanesthetic respiratory depression

  • Treated with analeptic drugs such as theophylline, aminophylline, caffeine, doxapram


Drugs for ADHD and Narcolepsy

  • CNS stimulants are first line drugs

  • Amphetamines: methylphenidate (Ritalin)

  • Nonamphetamine stimulants

    • Modafinil (Provigil)

    • Atomoxetine (Strattera): nonstimulant drug that is also used to treated ADHD

    • Lisdexamfetamine (Vyvanse) prodrug for dextroamphetamine


Mechanisms of Action and Drug Effects

  • Amphetamines

    • Stimulate areas of the brain associated with mental alertness

  • CNS Effects

    • Mood elevation or euphoria

    • Increased mental alertness and capacity for work

    • Decreased fatigue and drowsiness

    • Prolonged wakefulness

  • Respiratory effects

    • Relaxation of bronchial smooth muscle

    • Increased respiration

    • Dilation of pulmonary arteries


Contraindications

  • Known drug allergy

  • Cardiac structural abnormalities

  • Recent MAOI usage


Adverse Effects

  • Wide range; dose related

  • Tend to “speed up” body systems

  • Common adverse effects:

    • Palpitation, tachycardia, HTN, angina, dysrhythmias, nervousness, restlessness, anxiety, insomnia, nausea, vomiting, diarrhea, dry mouth, increased urinary frequency, others


Anorexiants

  • Any substance that suppresses appetite

  • Used to treat obesity

  • Anoxrexiants

    • Phentermine (Ionamin)

    • Benzphetamine (Regimex)*

    • Methamphetamine (Desoxyn)*

    • Diethylpropion (Tenuate)

            

            *Only ones approved for treatment of obesity


Mechanism of Action

  • Suppress appetite control centers in the brain

  • Increase the body’s basal metabolic rate

  • Mobilization of adipose tissue stores

  • Enhanced cellular glucose uptake

  • Reduce dietary fat absorption


Other Drugs to Treat Obesity

  • Qysmia (phentermine and topiramate)

  • Orlistat (Xenical): related nonstimulant drug used to treat obesity

    • Works locally in the small and large intestines, where it inhibits absorption of caloric intake from fatty foods

    • Inhibits enzyme lipase

  • Contrave ER (naltrexone and bupropion)

  • Saxenda (liraglutide)

    • Liraglutide, when marketed as Victoza, is used to treat type II diabetes


Indications/Contraindication of Anorexiants

  • Indications

    • used to treat obesity along with behavior medications (diet exercise)

    • Most often used in higher-risk patients

  • Contraindications

    • Drug allergy

    • Sever cardiovascular disease

    • Uncontrolled HTN

    • Hyperthyroidism

    • Eating disorders

    • MAOI usage


Adverse Effects of Anorexiants

  • Possible elevated blood pressure and heart palpitations

  • Anxiety Agitation

  • Dizziness

  • Headache

  • Orlistat: fecal incontinence with oily stools (reduces body’s ability to absorb fat)


Antimigraine Drugs

  • Antimigraine (serotonin agonists; also called triptans)

    • Sumatriptan (Imitrex)

    • Others but all end in triptan

  • Ergot alkaloids (largely replaced by triptans for first line therapy)

    • Ergotamine tartrate with caffeine (Cafergot): tablet form


Mechanism of Action and Drug Effects

  • Triptans

    • Stimulate 5-HT receptors in cerebral arteries, causing vasocontriction and reducing headache symptoms

    • Reduce the production of inflammatory neuropeptides

    • Abortive therapy for migraines

  • Ergot alkaloids

    • Narrow or constrict blood vessels in the brain


Adverse Effects of Antimigraine Drugs

  • Triptans

    • Vasoconstriction

    • Irritation at injection site

    • Tingling, flushing

  • Ergot alkaloids

    • Nausea and vomiting

    • Cold or clammy hands and feet

    • Muscle pain

    • Dizziness

    • Others


Drug for Specific Respiratory Depression Syndrome: Analeptics

  • Used less frequently

  • Still used for neonatal apnea

  • Examples

    • Doxapram (Dopram)

    • Methylxanthines, such as aminophylline, theophylline, and caffeine


Mechanism of Action of Analeptics

  • Stimulate areas of CNS that control respiration

  • Methylxanthines

    • Inhibit phospodiesterase, leading to buildup of cyclic adenosine monophosphate (cAMP)

  • Caffeine

    • Antagonizes adenosine receptors


Analeptics

  • Caffeine

    • Found in:

      • Over-the-counter drugs: NoDoz

      • Combination prescription drugs: Fioricet, Fiorinal

      • Food and beverages

    • Use with caution in patients with a history of:

      • Peptic ulcer

      • Recent myocardial infarction

      • Dysrhythmias

    • Intravenous: caffeine citrate and caffeine sodium benzoate

  • Doxapram (Dopram)

    • Treatment of respiratory depression associated with anesthetic drugs an drugs of abuse, COPD-induced hypercapnia

    • Monitor deep tendon reflexes, in addition to vital signs and heart rhythm, to prevent overdosage of this drug


Adverse Effects of Analeptics

  • Vagal

    • Stimulation of gastric secretions, diarrhea, and reflex tachycardia

  • Vasomotor

    • Flushing, sweating

  • Respiratory

    • Elevated respiratory rate (usually the desired effect)

  • Musculoskeletal

    • Muscular tension and tremors


Nursing Implications of Analeptics

  • Assess for:

    • Potential contraindications

    • Potential interactions, including herbal therapies

    • Condition such as abnormal cardiac rhythms, seizures palpitations, liver problems

    • For children, assess baseline height and weight


Nursing Implications of ADHD Drugs

  • Last daily dose should be given 4 to 6 hours before bedtime to reduce insomnia

  • Take on an empty stomach 30 to 45 minutes before meals (except for Strattera = nonstimulant for ADHD)

  • Needs to be taken with protein or else nausea or vomiting happens

  • Drug “holidays” may be ordered

    • Take breaks from stimulants if they don’t have to be at work or school (if they don’t need it)

  • Instruct parents to keep a journal to monitor the child’s response to therapy

  • Monitor the child for continued physical growth, including height and weight (can decrease appetite)


Nursing Implications of Anorexiants

  • Follow instructions for diet and exercise

  • Take in the morning

  • Avoid caffeine

  • Fat-soluble vitamin supplementation may be needed


Nursing Implications (Cont.)

  • Selective serotonin receptor agonists (SSRAs)

    • Dissolvable wafers, nasal spray, and self-injectable forms

    • Provide specific teaching about correct administration

    • Instruct patients to keep a journal to monitor response to therapy

  • Ergot alkaloids

    • Chest pain, confusion, slurred speech, and vision changes need immediate medical attention

  • Analeptics

    • Pay close attention to the ABCs because of the patient’s diminished sensorium

  • Monitory for therapeutic responses

    • ADHD, decrease hyperactivity, increased attention span and concentration

    • Anorexiant: appetite control and weight loss

    • Narcolepsy: decrease in sleepiness

    • Serotonin agonist: decrease in frequency, duration, and severity of migraines

  • Monitor for adverse effects