Neuro pharmacology

Chapters 10,11, 12,16

Opioid Analgesics
Pain relievers that contain opium, derived
from the opium poppy or chemically related

to opium
Narcotics: strong pain relievers

Terminology
Analgesics: medication that relieves pain without causing a loss of conciousness Pain: whatever the patient says it is Pain threshold:level of stimulus that results in the perception of pain Pain tolerance: the amount of pain an individual can endure without interferinf with normal functionning

Terminology cont
Acute pain: sudden onset

Chronic pain: persistent of recurring

Opioid Analgesics (contd)

codeine sulfate meperidine HCl methadone HCl morphine sulfate propoxyphene HCl

Opioid Analgesics: Indications

Main use: to alleviate moderate to severe pain
Often given with adjuvant analgesic agents to assist the primary agents with pain relief NSAIDs Antidepressants Anticonvulsants Corticosteroids

Opioid Analgesics: Indications (contd)

Opioids are also used for:
Cough centre suppression

Treatment of diarrhea
Balanced anaesthesia

Opioid Analgesics: Contraindications

Known drug allergy
Severe asthma or other respiratory

insufficiency
Elevated intracranial pressure

Pregnancy

Opioid Analgesics: Side Effects

Euphoria CNS depression Nausea and vomiting Respiratory depression Urinary retention Diaphoresis and flushing Pupil constriction (miosis) Constipation Itching

Opiate Antagonists
Naloxone, Narcan
Opiate antagonists Bind to opiate receptors and prevent a response
Used for complete or partial reversal of opioid-induced respiratory depression

Opiates
Opoid tolerance: a common physiological result of chronic opioid treatment. Larger dose of opioids is required to maintain the same level of analgesia Opoid physical dependance:The physiological adaptation of the body to the presence of an opioid Opoid phsychological dependance: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

Opiates
Opioid tolerance and physical dependence are expected with long-term opioid treatment and should not be confused with psychological dependence (addiction) *Misunderstanding of these terms leads to ineffective pain management and contributes to the problem of under treatment

Opioid Analgesics: Nursing Implications

Oral forms should be taken with food to minimize gastric upset Ensure safety measures, such as keeping side rails up, to prevent injury Withhold dose and contact physician if there is a decline in the clients condition or if VS are abnormal, especially if respiratory rate is less than 12 breaths/minute

Opioid Analgesics: Nursing Implications (contd)

CHECK DOSAGES CAREFULLY
Follow proper administration guidelines for IM injections, including site rotation Follow proper guidelines for IV administration, including dilution, rate of administration, institutions IV drug manual

Opioid Analgesics: Nursing Implications (contd)

Constipation is a common side effect and may be prevented with adequate fluid and fibre intake Instruct clients to follow directions for administration carefully, and to keep a record of their pain experience and response to treatments Clients should be instructed to change positions slowly to prevent possible orthostatic hypotension

Monitor for Side Effects

Should VS change, clients condition decline, or pain continue, contact physician immediately Respiratory depression may be manifested by respiratory rate of less than 12/minute, dyspnea, diminished breath sounds, or shallow breathing

Nonopioid Analgesics
Acetaminophen
Analgesic and antipyretic effects
little anti-inflammatory effects Available OTC and in combination products

with opioids

Mechanism of Action
Similar to salicylates Blocks pain impulses peripherally by inhibiting prostaglandin synthesis
Indications: Mild to moderate pain fever Alternative for those who cannot take aspirin products

Acetaminophen Contraindications
Drug allergy Severe liver disease Genetic disease (G6PD)

Toxicity and Managing Overdose

Even though available OTC, lethal when overdosed Overdose, whether intentional or due to chronic unintentional misuse, causes hepatic necrosis Long-term ingestion of large doses also causes nephropathy Recommended antidote: acetylcysteine

Dosage
Maximum daily dose for healthy adults is 4000 mg per day Inadvertent excessive doses may occur when different combination drug products are taken together Be aware of the acetaminophen content of the medications taken by the client

Interactions
Dangerous interactions may occur if taken with alcohol Should not be taken in the presence of:
Liver dysfunction

Possible liver failure When taking other hepatotoxic drugs

Analgesics: Nursing Implications (contd)

Perform a thorough pain assessment, including pain intensity and character, onset, location, description, precipitating and relieving factors, type, remedies, and other pain treatments
Assessment of pain is now being considered a fifth vital sign

Analgesics: Nursing Implications (contd)

Be sure to medicate clients before the pain becomes severe in order to provide adequate analgesia and pain control Pain management includes pharmacological and nonpharmacological approaches; be sure to include other interventions as indicated

Analgesics Case Study

Mr. Jones is admitted with Renal Colic. He rings his bell stating he cant take in anymore? What are your assessments?

Analgesics Case Study cont

Your MAR indicates that Mr Jones may have IV Morphine 2mg q 10 minutes for pain.
What will you do before administering this medication?

Analgesics Case Study cont

He settles after 4 doses. What will you do now?
What teaching will you provide about pain management? What teaching will you provide about narcotic analgesics?

Morphine

is an highly potent opiat analgesic PO, S/C, IM, IV Indications:

post op pain Chronic pain Kidney stone pain Adjunct to General anesthesia intrathecal analgesia Palliative Antitussive Diarrhea

Analgesics Case Study cont

On the next shift Mr Jones has a reoccurence of pain. The nurse gives in 5 doses of IV morphine, (total fo 10 mg). He finally settles. While checking in on him, he his unconctious, responding to painful stimuli only and his respirations are 6/minutes.

Codeine
Opiate analgesic Routes: PO, IM, SC Indications:
post op pain Chronic pain Palliative Antitussive Diarrhea

Codeine
Present in numerous combination drugs Tylenol #1 acetaminophen 300 mg caffeine 15 mg, in combination with codeine 8 mg Tylenol #2 acetaminophen 300 mg caffeine 15 mg, in combination with codeine 15 mg Tylenol#3 acetaminophen 300mg, caffeine 15mg, Codeine 30mg Codeine Contin

Others
Percocet: oxycodone and acetaminophen Percodan: oxycodone/Aspirin

Anaesthetics
Agents that depress the central nervous system (CNS)
Depression of consciousness Loss of responsiveness to sensory stimulation (including pain) Muscle relaxation

Anaesthesia: the state of depressed CNS activity

Anaesthesia
A state of depressed CNS activity Two types
General anaesthesia Local anaesthesia

Balanced anaesthesia

Types of anesthetics
General anesthetic: agents that induce global anesthesia with loss of conciousness Local anesthesia; agents that cause a specific area of the body to be insensitive to pain without affecting consciousness Topical anesthetic: local anesthetics directly applied to skin and mucous membranes.

General Anaesthetics
Agents 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

Local Anaesthetics
Also called regional anaesthetics 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

Types of Local Anaesthesia

Epidural Infiltration Nerve block Spinal Topical

Moderate Sedation Neurolept anesthesia

Combination of an IV benzodiazepine and an opiate analgesic used Anxiety and sensitivity to pain are reduced, and client cannot recall the procedure Preserves the clients ability to maintain own airway and to respond to verbal commands

Moderate Sedation (contd)

Used for diagnostic procedures and minor surgical procedures that do not require deep anaesthesia. (ie endoscopy) Topical anaesthetic may be applied also Rapid recovery time and greater safety profile than general anaesthesia

Nursing Implications
Always assess past history of surgeries and response to anaesthesia. Any known problems such as difficult intubation, N&V, malignant hyperthermia?
Assess past history, allergies, medications Assess use of alcohol, illicit drugs, opioids

Nursing Implications (contd)

Assessment is vital during pre-, intra-, and postoperative phases
Vital signs Baseline labwork, ECG Pulse oximeter (PO2) ABCs (airway, breathing, circulation) Monitor all body systems

Nursing Implications (contd)

Nursing considerations during the perioperative phase include the:
Preoperative phase Intraoperative phase Postoperative phase

Each phase has its own complex and specific nursing actions

Nursing Implications (contd)

Close and frequent observation of the client and all body systems During a procedure, monitor vital signs, ABCs Watch for sudden elevations in body temperature, which may indicate malignant hyperthermia

Nursing Implications (contd)

During recovery, monitor for cardiovascular
depression, respiratory depression, and complications of anaesthesia Monitor for S&S of bleeding Implement safety measures during recovery,

especially if motor/sensory loss occurs due to

local anaesthesia

Nursing Implications (contd)

Reorient client to surroundings
Provide preoperative teaching about the

surgical procedure and anaesthesia

Teach the client about postoperative

turning, coughing, deep breathing

CNS Depressants
Sedatives or Hypnotics
Sedatives: reduce nervousness, excitability and irritability without causing sleep

Hypnotic: causes sleep

CNS Depressants (contd)

Sedative-hypnoticsdose dependent
At low doses, calm or soothe the CNS without inducing sleep At high doses, calm or soothe the CNS to the point of causing sleep

Sedative-Hypnotics
3 main categories:
1. Barbtuates

2. Benzodiazepine
3. Miscellaneous agents

Sedative-Hypnotics: Barbiturates
First introduced in 1903; standard agents for insomnia and sedation Habit forming Only a handful commonly used today due in part to the safety and efficacy of benzodiazepines Barbiturates have a narrow therapeutic index

Barbiturates: Indications
pentobarbital phenobarbital

Hypnotic

Sedative Anticonvulsant Anaesthesia for surgical procedures

Barbiturates: Side Effects

Body System CNS Effects Drowsiness, lethargy, vertigo, mental depression, coma
Respiratory depression, apnea, bronchospasms, cough

Respiratory

Barbiturates: Toxicity and Overdose

Overdose frequently leads to respiratory depression, and subsequently, respiratory arrest Overdose produces CNS depression (sleep to coma and death) Can be therapeutic
Anaesthesia induction Uncontrollable seizures: phenobarbital coma

CNS Depressants: Benzodiazepines

Most frequently prescribed sedative-hypnotics
Most commonly prescribed drug classes

Favourable side effect profiles

Efficacy Safety

Benzodiazepines: Classification
Classified as either:
Sedative-hypnotic

Anxiolytic (medication that relieves anxiety)

Benzodiazepines: Sedative-Hypnotic Types

Long acting
chlordiazepoxide, clorazepate, flurazepam

Intermediate acting
alprazolam, clonazepam, lorazepam, oxazepam

Short acting
midazolam (IV), triazolam

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 Treatment of alcohol withdrawal Agitation Depression Epilepsy Balanced anaesthesia

Benzodiazepines: Side Effects

Mild and infrequent
Headache Drowsiness Dizziness Vertigo Lethargy Paradoxical excitement (nervousness) Hangover effect

Nursing Implications
Give 15 to 30 minutes before bedtime for maximum effectiveness in inducing sleep Most benzodiazepines (except flurazepam) cause REM rebound and a tired feeling the next day; use with caution in the elderly Clients should be instructed to avoid alcohol and other CNS depressants

Nursing Implications (contd)

It may take 2 to 3 weeks to notice improved sleep when taking barbiturates Rebound insomnia may occur for a few nights after a 3- to 4-week regimen has been discontinued

Nursing Implications (contd)

Safety is important
Keep side rails up or use bed alarms Do not permit smoking Assist client with ambulation (especially the elderly) Keep call light within reach

Monitor for side effects

Nursing Implications (contd)

Monitor for therapeutic effects
Increased ability to sleep at night Fewer awakenings Shorter sleep-induction time Few side effects, such as hangover effects Improved sense of well-being because of improved sleep

Muscle Relaxants
Baclofen, Flexeril, Dantrolene

Act to relieve pain associated with skeletal muscle spasms Majority are central acting
CNS is the site of action Similar in structure and action to other CNS depressants

Direct acting
Acts directly on skeletal muscle Closely resembles GABA

Muscle Relaxants: Indications

Relief of painful musculoskeletal conditions
Muscle spasms Management of spasticity of severe chronic disorders Multiple sclerosis, cerebral palsy

Work best when used along with physical therapy

Muscle Relaxants: Side Effects

Extension of effects on CNS and skeletal muscles
Euphoria Lightheadedness Dizziness Drowsiness Fatigue Muscle weakness

treatment of convulsions and status epilepticus

CNS Stimulants
Drugs that stimulate a specific area of the brain or spinal cord. Analeptics (CNS stimulants) Appetite suppressants Treatment of
Attention-deficit/hyperactivity disorder (ADHD) Narcolepsy Migraine headache

Indications
Analeptics (CNS stimulants) Reversal of anaesthesia-

induced respiratory depression

Anorexiants Thought to suppress the appetite control

centre in the brain

ADHDStimulate the areas in the brain responsible for

mental alertness and attentiveness

NarcolepsyIncrease mental alertness
Migraine headaches

Caffeine, co-administered with other drugs, used to

Side Effects
Wide range, dose related Tend to speed up body systems Common adverse effects include:
Palpitations, tachycardia, hypertension, angina, dysrhythmias, nervousness, restlessness, anxiety, insomnia, nausea, vomiting, diarrhea, increased urinary frequency