Pharmacology Flashcards

Analgesic Drugs

• Pain management is an important aspect of nursing care.
• Pain is a common reason for seeking healthcare.
• Pain can lead to suffering and economic burden.

Pain

• Pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage.
• It's a personal and individual experience.
• Pain is whatever the patient says it is and exists when the patient says it exists.
• Pain involves physical, psychological, and cultural factors.

The Patient Experiencing Pain

• Culture influences beliefs, thoughts, and ways of managing pain.
• Attitudes, meanings, and perceptions of pain vary with culture, race, and ethnicity.
• African Americans may believe in healers who use religious faith, prayer, and laying on of hands.
• Hispanic Americans may use prayer, amulets, herbs, and spices.
• Chinese traditional methods include acupuncture, herbal remedies, yin and yang balancing, and cold treatment (moxibustion).
• Asian and Pacific Islander patients may be reluctant to express pain, believing it's God's will or punishment.
• Native Americans may use massage, heat, sweat baths, herbal remedies, and harmony with nature.
• In Arab culture, patients may openly express pain and expect immediate relief through injections or intravenous drugs.
• Awareness of cultural influences is important for effective and individualized nursing care.

Pain Management Approach

• No single approach is effective for all patients.
• Tailored to each patient's needs considering:
  • Cause of pain
  • Concurrent medical conditions
  • Characteristics of pain
  • Psychological and cultural characteristics
• Requires ongoing reassessment of pain and treatment effectiveness.

Classification of Pain by Onset and Duration

• Acute pain:
  • Sudden onset
  • Usually subsides once treated
• Chronic pain:
  • Persistent or recurring
  • Often difficult to treat
• Tolerance
• Physical dependence
• Length beyond 3 months

Classification of Pain

• Somatic
• Visceral
• Superficial
• Deep
• Vascular
• Referred
• Neuropathic
• Phantom
• Cancer
• Central

Key Concepts (Definitions)

• Chronic pain: Persistent or recurring pain lasting longer than 3-6 months, or 1 month after acute injury healing, or with non-healing tissue injury.
• Deep pain: Pain in tissues below skin level, opposite of superficial pain.
• Gate theory: Explains pain transmission and relief using a gate model.
• Narcotics: Legal term for drugs producing insensibility or stupor, especially opioids (but term is falling out of use).
• Neuropathic pain: Pain from a disturbance of nerve function.
• Nociception: Processing of pain signals in the brain.
• Nociceptors: Sensory nerves (A and C fibers) transmitting pain signals to the CNS.
• Nonopioid analgesics: Analgesics not classified as opioids.
• Pain threshold: The level of a stimulus that results in the sensation of pain.
• Pain tolerance: The amount of pain a patient can endure without it interfering with normal function.
• Partial agonist: Drug that binds to a receptor and causes a response that is less than that caused by a full agonist (same as agonist-antagonist).
• Phantom pain: Pain experienced in an amputated body part.
• Physical dependence: Unpleasant physical symptoms (withdrawal) occur if a drug is stopped abruptly.
• Psychologic dependence: Compulsive use of opioids or other addictive substance characterized by a continuous craving for the substance and the need to use it for effects other than pain relief (also called addiction).
• Referred pain: Pain occurring in an area away from the organ of origin.
• Somatic pain: Pain originating from skeletal muscles, ligaments, or joints.
• Acute pain: Pain that is sudden in onset, usually subsides when treated, and typically occurs over less than a 6-week period.
• Addiction: A chronic, neurobiologic disease whose development is influenced by genetic, psychosocial, and environmental factors (same as psychologic dependence).
• Adjuvant analgesic drugs: Drugs that are added for combined therapy with a primary drug and may have additive or independent analgesic properties, or both.
• Agonist: A substance that binds to a receptor and causes a response.
• Agonists-antagonists: Substances that bind to a receptor and cause a partial response that is not as strong as that caused by an agonist (also known as a partial agonist).
• Analgesic ceiling effect: Occurs when a given pain drug no longer effectively controls pain despite the administration of the highest safe dosages.
• Analgesics: Medications that relieve pain without causing loss of consciousness (sometimes referred to as painkillers).
• Antagonist: A drug that binds to a receptor and prevents (blocks) a response.
• Breakthrough pain: Pain that occurs between doses of pain medication.
• Cancer pain: Pain resulting from any of a variety of causes related to cancer and/or the metastasis of cancer.
• Central pain: Pain resulting from any disorder that causes central nervous system damage.
• Nonsteroidal antiinflammatory drugs (NSAIDS): A large, chemically diverse group of drugs that are analgesics and also possess antiinflammatory and antipyretic activity.
• Opioid analgesics: Synthetic drugs that bind to opiate receptors to relieve pain.
• Opioid naive: Describes patients who are receiving opioid analgesics for the first time and who therefore are not accustomed to their effects.
• Opioid tolerance: A normal physiologic condition that results from long-term opioid use, in which larger doses of opioids are required to maintain the same level of analgesia and in which abrupt discontinuation of the drug results in withdrawal symptoms (same as physical dependence).
• Opioid tolerant: The opposite of opioid naïve; describes patients who have been receiving opioid analgesics (legally or otherwise) for a period of time (1 week or longer).
• Opioid withdrawal: The signs and symptoms associated with abstinence from or withdrawal of an opioid analgesic when the body has become physically dependent on the substance.
• Opioids: A class of drugs used to treat pain. This term is often used interchangeably with the term narcotic.
• Pain: An unpleasant sensory and emotional experience associated with actual or potential tissue damage.
• Special pain situations: The general term for pain control situations that are complex and whose treatment typically involves multiple medications, and nonpharmacologic therapeutic modalities (e.g., massage, chiropractic care, surgery).
• Superficial pain: Pain that originates from the skin or mucous membranes; opposite of deep pain.
• Synergistic effects: Drug interactions in which the effect of a combination of two or more drugs with similar actions is
  greater than the sum of the individual effects of the same drugs given alone. For example, 1+1 is greater than 2.
• Tolerance: The general term for a state in which repetitive exposure to a given drug, over time, induces changes in drug
  receptors that reduce the drug's effects (same as physical dependence).
• Vascular pain: Pain that results from pathology of the vascular or perivascular tissues.
• Visceral pain: Pain that originates from organs or smooth muscles.
• World Health Organization (WHO): An international body of
  health care professionals that studies and responds to health needs and trends worldwide.

Analgesics

• Medications that relieve pain without causing loss of consciousness
• "Painkillers"
• Opioid analgesics
• Adjuvant analgesic drugs

Adjuvant Drugs

• Assist primary drugs in relieving pain
• Examples:
  • NSAIDs
  • Antidepressants
  • Anticonvulsants
  • Corticosteroids
• Example: adjuvant drugs for neuropathic pain
  • Amitriptyline (antidepressant)
  • Gabapentin or pregabalin (anticonvulsants)

Opioid Drugs

• Synthetic drugs that bind to opiate receptors to relieve pain
• Mild agonists: codeine, hydrocodone
• Strong agonists: morphine, hydromorphone, oxycodone, meperidine, fentanyl, and methadone
• Meperidine: not recommended for long-term use because of the accumulation of a neurotoxic metabolite, normeperidine, which can cause seizures

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 classifications based on their actions
  • Agonists
  • Agonists-antagonists
  • Antagonists (nonanalgesic)

Opioid Analgesics: Indications

• Main use: to alleviate moderate to severe pain
• Often given with adjuvant analgesic drugs to assist primary drugs with pain relief
• Opioids are also used for:
  • Cough center suppression
  • Treatment of diarrhea
  • Balanced anesthesia

Opioid Analgesics: 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

Opioid Analgesics: 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

Opioids: Opioid Tolerance

• A common physiologic result of chronic opioid treatment
• Result: larger dose is required to maintain the same level of analgesia

Opioids: Physical Dependence

• 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).

Opioids: Psychologic Dependence

• A 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

Opioid Analgesics: Toxicity and Management of Overdose

• Naloxone (Narcan)
• Naltrexone (ReVia)
• Regardless of withdrawal symptoms, when a patient experiences severe respiratory depression, an opioid antagonist should be given.

Opioid Analgesics: Interactions

• Alcohol
• Antihistamines
• Barbiturates
• Benzodiazepines
• Monoamine oxidase inhibitors
• Others

Codeine Sulfate

• Opioid agonist
• Natural opiate alkaloid (Schedule II) obtained from opium
• Less effective; ceiling effect
• Often combined with acetaminophen (Schedule III)
• More commonly used as an antitussive drug
• Most common adverse effect: GI disturbance

Fentanyl

• Synthetic opioid (Schedule II) used to treat moderate to severe pain
• Forms: Parenteral injections, transdermal patches (Duragesic), buccal lozenges (Fentora), buccal lozenges on a stick (Actiq)
• 0.1 mg IV fentanyl = 10 mg IV morphine
• Fentanyl patch for chronic, long-term pain management

Hydromorphone (Dilaudid)

• Very potent opioid analgesic; Schedule II drug
• 1 mg IV/IM hydromorphone = 7 mg morphine
• Exalgo:
  • Osmotic extended-release oral delivery
  • Difficult to crush/extract for injection (reducing abuse potential)

Meperidine

• Synthetic opioid analgesic (Schedule II)
• Use with caution in elderly or those with kidney dysfunction
• Active metabolite (normeperidine) can accumulate to toxic levels, causing seizures
• Rarely used; not recommended for long-term pain treatment
• Uses: Migraine treatment, post-op shivering

Morphine Sulfate

• Naturally occurring alkaloid derived from the opium poppy
• Drug prototype for all opioid drugs; Schedule II controlled substance
• Indication: severe pain
• High abuse potential
• Dosage forms: oral, injectable, rectal; also extended-release

Tramadol Hydrochloride

• Trade name: Ultram
• Centrally acting analgesic with a dual mechanism of action
  • Weak bond to mu opioid receptors
  • Inhibits the reuptake of norepinephrine and serotonin
• Indicated for moderate to moderately severe pain
• Adverse effects similar to those of opioids
• Careful use in patients taking SSRIs, MAOIs, neuroleptics

Oxycodone hydrochloride

• Analgesic agent structurally related to morphine (Class II)
• Comparable analgesic activity to morphine
• Often combined with acetaminophen (Percocet) or with aspirin (Percodan)
• IR = immediate release
• SR = sustained release
• Hydrocodone (weaker) often combined with acetaminophen (Vicodin, Norco)

Naloxone Hydrochloride (Narcan)

• Pure opioid antagonist
• Drug of choice for complete/partial reversal of opioid-induced respiratory depression
• Indicated in cases of suspected acute opioid overdose
• Failure to reverse presumed opioid overdose suggests condition may not be related to opioids

Opioid Antagonists

• Naloxone now available without a prescription; used by first responders for opioid/illegal drug overdoses
• Naltrexone
  • Opioid antagonist (oral form)
  • Used for alcohol and opioid addiction

Nonopioid Analgesics: Acetaminophen (Tylenol)

• Analgesic and antipyretic effects
• Little to no anti-inflammatory effects
• Available over-the-counter (OTC) and in combination products with opioids

Acetaminophen: Mechanism of Action

• Similar to salicylates
• Blocks pain impulses peripherally by inhibiting prostaglandin synthesis

Acetaminophen: Indications

• Mild to moderate pain, fever
• Alternative for those who cannot take aspirin products

Acetaminophen: Dosage

• Maximum daily dose for healthy adults is being lowered to 3000 mg/day
• 2000 mg for older adults and those with liver disease
• Inadvertent excessive doses may occur when different combination drug products are taken together
• Be aware of the acetaminophen content of all medications taken by the patient (OTC and prescription).

Acetaminophen: Contraindications and Interactions

• Should not be taken in the presence of:
  • Drug allergy
  • Liver dysfunction / possible liver failure
  • G6PD deficiency
• Dangerous interactions with alcohol or other hepatotoxic drugs

Lidocaine, transdermal

• Topical anesthetic
• Indications: postherpetic neuralgia
• Left in place no longer than 12 hours
• Minimal adverse effects; skin irritation may occur

Analgesics: Nursing Process: Assessment

• Thorough history regarding allergies and use of other medications, including alcohol, health history, and medical history.
• Obtain baseline vital signs and I&O.
• Assess for potential contraindications and drug interactions.

Analgesics: Nursing Process: Assessment (Cont.)

• Thorough pain assessment: intensity, character, onset, location, description, precipitating/relieving factors, type, remedies, other treatments.
• Pain is now considered a “fifth vital sign.”
• Rate pain on a 0 to 10 or similar scale
• Use appropriate scale for age, cognition

Analgesics: Nursing Implications

• Medicate patients before pain becomes severe for adequate analgesia and pain control.
• Pain management includes pharmacologic and nonpharmacologic approaches; include other interventions as indicated.

Analgesics: Nursing Implications (Cont.)

• Patients should not take other medications or OTC preparations without checking with their physicians.
• Instruct patients to notify physician about signs of allergic reaction or adverse effects.

Herbal Products: Feverfew

• Related to the marigold family
• Anti-inflammatory properties
• Used to treat migraine headaches, menstrual cramps, inflammation, and fever
• May cause GI distress, altered taste, muscle stiffness
• May interact with aspirin and other NSAIDs, as well as anticoagulants

Anesthesia

• A state of reduced neurologic function
• Three types
  • General anesthesia: complete loss of consciousness and loss of body reflexes, including paralysis of respiratory muscles
  • Local anesthesia: no paralysis of respiratory function; elimination of pain sensation in the tissues innervated by anesthetized nerves
  • Monitored anesthesia care (MAC): local anesthesia along with sedation and analgesia

Anesthetics

• Drugs that reduce or eliminate pain by depressing nerve function in the central nervous system (CNS) and peripheral nervous system

General Anesthetics

• Administered by anesthesia providers
  • Anesthesiologist
  • Nurse anesthetist (CRNA)
  • Anesthesia assistant
• Drugs that induce a state in which the CNS is altered to produce varying degrees of:
  • Pain relief
  • Depression of consciousness
  • Skeletal muscle relaxation
  • Reflex reduction

General Anesthetics (Cont.)

• Inhalational anesthetics
  • Volatile liquids or gases that are vaporized in oxygen and inhaled
• Parenteral anesthetics
  • Administered intravenously
• Adjunct anesthetics
  • Drug that enhances clinical therapy when used simultaneously with another drug

General Anesthetics: Indications

• Used during surgical procedures to produce:
  • Unconsciousness
  • Skeletal muscular relaxation
  • Visceral smooth muscle relaxation
• Rapid onset; quickly metabolized
• Also used in electroconvulsive therapy treatments for depression

General Anesthetics: Contraindications

• Known drug allergy
• Depending on drug type:
  • Pregnancy
  • Narrow-angle glaucoma
  • Acute porphyria
  • Known history of malignant hyperthermia

General Anesthetics: Adverse Effects

• Vary according to dosage and drug used
• Sites primarily affected
  • Heart, peripheral circulation, liver, kidneys, respiratory tract
• Myocardial depression is commonly seen.

General Anesthetics: Adverse Effects (Cont.)

• Malignant hyperthermia
  • Occurs during or after volatile inhaled general anesthesia or use of the neuromuscular blocking drug (NMBD) succinylcholine
  • Sudden elevation in body temperature (greater than 104° F)
  • Tachypnea, tachycardia, muscle rigidity
  • Life-threatening emergency
  • Treated with cardiorespiratory supportive care and dantrolene (skeletal muscle relaxant)

Dexmedetomidine (Precedex)

• Alpha2-adrenergic receptor agonist
• Dose-dependent sedation, decreased anxiety, and analgesia without respiratory depression
• Use: procedural sedation, surgeries of short duration
• Short half-life, and the patient awakens quickly upon withdrawal of the drug
• Sedation of mechanically ventilated patients in the intensive care unit (ICU)

Ketamine

• Intravenous administration use for both general anesthesia and moderate sedation
• Can be given IM or subcutaneously
• Rapid onset of action
• Low incidence of reduction of cardiovascular, respiratory, and bowel function
• Adverse effects: disturbing psychomimetic effects, including hallucinations

Nitrous Oxide

• “Laughing gas”
• Only inhaled gas currently used as a general anesthetic
• Weakest of the general anesthetic drugs
• Used primarily for dental procedures or as a supplement to other, more potent anesthetics

Propofol (Diprivan)

• Parenteral general anesthetic
• Used for the induction and maintenance of general anesthesia
• Sedation for mechanical ventilation in ICU settings
• Lower doses: sedative-hypnotic for moderate sedation
• Monitor triglycerides if administered with total parenteral nutrition
• Some states prohibit administration by nurses.

Sevoflurane (Ultane)

• Fluorinated ether
• Widely used
• Rapid onset and rapid elimination
• Especially useful in outpatient surgery settings
• Nonirritating to the airway
• Greatly facilitates induction of an unconscious state, especially in pediatric patients

Local Anesthetics

• Also called regional anesthetics
• Used to render a specific portion of the body insensitive to pain
• Interfere with nerve impulse transmission to specific areas of the body
• Do not cause loss of consciousness

Local Anesthetics (Cont.)

• Topical
  • Applied directly to skin or mucous membranes
  • Creams, solutions, ointments, gels, ophthalmic drops, powders, suppositories
• Parenteral
  • Injected intravenously or into the CNS by various spinal injection techniques

Types of Local Anesthesia

• Spinal or intraspinal
  • Intrathecal
  • Epidural
• Infiltration
• Nerve block
• Topical
• Peripheral nerve catheter attached to a pump containing the local anesthetic: Pain Buster and On-Q pump

Types of Local Anesthesia (Cont.)

• 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

• Local anesthetics are 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

Local Anesthetic: Adverse Effects

• Usually limited
• Adverse effects result if:
  • Inadvertent intravascular injection
  • Excessive dose or rate of injection
  • Slow metabolic breakdown
  • Injection into highly vascular tissue
  • Allergy (generally limited; most common with “ester type” anesthetics)

Local Anesthetic: Adverse Effects (Cont.)

• “Spinal headache”
  • 70% of patients who either experience inadvertent dural puncture during epidural anesthesia or undergo intrathecal anesthesia.
  • Usually self-limiting
  • Treatment: bed rest, analgesics, caffeine,
• Blood patch for severe cases

Neuromuscular Blocking Drugs

• Also known as NMBDs
• Prevent nerve transmission in skeletal and smooth muscle, resulting in muscle paralysis
• Also paralyze the skeletal muscles required for breathing: the intercostal muscles and the diaphragm
• Used with anesthetics during surgery

Neuromuscular Blocking Drugs: Indications

• Main use: facilitating controlled ventilation during surgical procedures
• Endotracheal intubation (short acting)
• To reduce muscle contraction in an area that needs surgery
• Diagnostic drugs for myasthenia gravis
• Other uses

Neuromuscular Blocking Drugs: Contraindications

• Contraindications
  • Malignant hyperthermia
• Adverse effects
• Drug interactions
• Toxicity and management of overdose
• Antidotes: anticholinesterase drugs such as neostigmine, pyridostigmine

Neuromuscular Blocking Drugs: Safety

• Respiratory muscle paralysis occurs with these drugs.
• Emergency ventilation equipment must be immediately available.

Neuromuscular Blocking Drugs: Depolarizing Drugs

• Succinylcholine
• Works similarly to neurotransmitter acetylcholine (ACh), causing depolarization
• Metabolism is slower than Ach; therefore, as long as succinylcholine is present, repolarization cannot occur.
• Result: flaccid muscle paralysis

Nondepolarizing Neuromuscular Blocking Drugs: Rocuronium (Zemuron)

• Rapid-to-intermediate acting
• Adjunct to general anesthesia
• Facilitates tracheal intubation
• Provides skeletal muscle relaxation

Nursing Implications

• Always assess past history of surgeries and response to anesthesia.
• Assess past history, allergies, and medications.
• Assess use of alcohol, illicit drugs, and opioids.

Nursing Implications (Cont.)

• Assessment is vital during preoperative, intraoperative, and postoperative phases.
• Vital signs
• Baseline lab work, ECG
• Oxygen saturation
• ABCs (airway, breathing, circulation)
• Monitor all body systems

Nursing Implications (Cont.)

• Each perioperative phase has its own complex and very specific nursing actions.
• Provide preoperative teaching about the surgical procedure and anesthesia plan.

Nursing Implications (Cont.)

• Perform close and frequent observation of the patient and all body systems.
• During a procedure, monitor vital signs and ABCs.
• Watch for sudden elevations in body temperature, which may indicate malignant hyperthermia.

CNS Depressants

• Sedatives
  • Drugs that have an inhibitory effect on the CNS to the degree that they reduce:
    • Nervousness
    • Excitability
    • Irritability

CNS Depressants (Cont.)

• 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 vs. Hypnotics

• Sedatives are CNS depressants that induce a sense of calm and decrease anxiety.
• Hypnotics are CNS depressants that induce sleep. The three types of sedative-hypnotics are:
  • Benzodiazepines
  • Barbiturates
  • benzodiazepine-like medications

CNS Depressants: Benzodiazepines

• Formerly the most commonly prescribed sedative-hypnotic drugs
• Nonbenzodiazepines are currently more frequently prescribed.
• Favorable adverse effect profiles, efficacy, and safety when used appropriately

CNS Depressants: Benzodiazepines (Cont.)

• Classified as either:
  • Sedative-hypnotic
  • Anxiolytic (medication that relieves anxiety)
• Benzodiazepines commonly used as sedative-hypnotic drugs

Benzodiazepines: Drug Effects

• Calming effect on the CNS
• Useful in controlling agitation and anxiety
• Reduce excessive sensory stimulation, inducing sleep
• Induce skeletal muscle relaxation

Benzodiazepines: Indications

• Sedation
• Sleep induction
• Skeletal muscle relaxation
• Anxiety relief
• Anxiety-related depression

Benzodiazepines: Indications (Cont.)

• Treatment of acute seizure disorders
• Treatment of alcohol withdrawal
• Agitation relief
• Balanced anesthesia
• Moderate or conscious sedation

Benzodiazepines: Contraindications

• Drug allergy
• Narrow-angle glaucoma
• Pregnancy

Benzodiazepines: Adverse Effects

• Mild and infrequent:
  • Headache
  • Drowsiness
  • Dizziness
  • Cognitive impairment
  • Vertigo
  • Lethargy
  • Fall hazard for older adults
  • “Hangover” effect or daytime sleepiness

Benzodiazepines Medication: Diazepam (Valium)

• Diazepam has a long half life
  • Other Medications:
    • Midazolam (conscious sedation) (Versed)
    • Lorazepam (Ativan)
    • Chlordiazepoxide (Librium)
    • Temazepam (Restoril)
    • Alprazolam (Xanax)
• Expected Pharmacological Action:
  • Enhance the action of gamma-amino butyric acid (GABA) in the CNS.
• Therapeutic Uses:
  • Anxiety disorders
  • Seizure disorders: DOC for status epilepticus
  • Insomnia
  • Muscle spasm
  • Alcohol withdrawal: chlordiazepoxide
  • Induction of anesthesia

Benzodiazepines: Side/Adverse Effects

• CNS depression
• Anterograde amnesia
• Paradoxical response such as insomnia, excitation, euphoria, anxiety, rage
• Respiratory depression, especially with IV Administration
• Potentiation with alcohol, valerian root and other CNS depressors
• Increased in sleep apnea, organic brain disease, liver and renal diseases
• Physical dependence:
  * Withdrawal following long-term therapy manifests as delirium, paranoia, and seizures (status epilepticus)
  * Avoid abrupt discontinuation: taper
• Toxicity:
  • Decontamination: gastric lavage, activated charcoal
  • Ventilatory support
  • Flumazenil

Benzodiazepines: Toxicity and Overdose

• 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

Benzodiazepines: Interactions

• Azole antifungals, verapamil, diltiazem, protease inhibitors, macrolide antibiotics, grapefruit juice
• CNS depressants (alcohol, opioids)
• Olanzapine
• Rifampin
• Herbal Interactions
• Food-drug Interactions
• Opioids

Diazepam (Valium)

• First clinically available benzodiazepine drug. It has varied uses
• Treatment of anxiety
• Procedural sedation and anesthesia adjunct
• Anticonvulsant therapy
• Skeletal muscle relaxation
• Available in multiple forms:
  • Oral
  • Rectal
  • Injectable

Midazolam (Versed)

• Used preoperatively and for moderate sedation
• Causes amnesia and anxiolysis (reduced anxiety) as well as sedation
• Normally administered by injection in adults
• Liquid oral dosage form is also available for children.
• High-alert medication

Temazepam (Restoril)

• Intermediate-acting benzodiazepine
• One of the metabolites of diazepam
• Normally induces sleep within 20 to 40 minutes
• Long onset of action, so it is recommended that patients take it about 1 hour prior to going to bed
• Still an effective hypnotic; however, it has been replaced by newer drugs

Nonbenzodiazepines Medication: Zolpidem (Ambien)

• Enhance the action of gamma-amino butyric acid (GABA) in the CNS.
• These medications do not function as antianxiety, muscle relaxant, or antiepileptic agents.
• Short half life, rapid onset of action: take immediately going to bed
• Food inhibit absorption: empty stomach
• There is a low risk of tolerance, abuse, and dependence.
• Therapeutic Uses
  • Management of insomnia
  • Other Medications:
    • Buspirone (Buspar)
    • Trazodone (antidepressant) (Desyrel)
    • Mirtazapine (antidepressant) (Remeron)

Nonbenzodiazepines Side/Adverse Effects

• Daytime sleepiness and lightheadedness. Advise clients to take medication at bedtime, allowing for at least 8 hr of sleep.
• Contraindications/Precautions
  * Contraindicated in clients who are breastfeeding
  * Use cautiously in older adult clients and in clients with impaired kidney, liver, and/or respiratory function.
• Medication/Food Interactions
  • CNS depressants such as alcohol, barbiturates, opioids cause additive CNS depression.

Nonbenzodiazepine: Zolpidem (Ambien)

• Short-acting nonbenzodiazepine hypnotic
• Lower incidence of daytime sleepiness compared with benzodiazepine hypnotics
• Ambien CR is a longer acting form with two separate drug reservoirs.
• Concerns about somnambulation (sleep-walking)

Nonbenzodiazepine: Eszopiclone (Lunesta)

• First hypnotic to be FDA approved for long-term use
• Designed to provide a full 8 hours of sleep
• Considered a short- to intermediate-acting agent
• Patients should allot 8 hours of sleep time and should avoid taking hypnotics when they must awaken in less than 6 to 8 hours.

Nonbenzodiazepine: Ramelteon (Rozerem)

• Structurally similar to the hormone melatonin: works as an agonist at melatonin receptors in the CNS
• Technically, it is not a CNS depressant; used as hypnotic
• Not classified as a controlled substance
• Indicated for patients who have difficulty with sleep onset rather than sleep maintenance

Herbal Products: Kava

• Used to relieve anxiety, stress, and restlessness and to promote sleep
• May