Analgesics

Algesia (pain)

It is an ill defined, unpleasant sensation, usually evoked by an external or internal noxious stimulus.

Analgesics

A drug that selectively relieves pain by acting in the CNS or on peripheral pain mechanisms, without
significantly altering consciousness.

Analgesics are divided into two groups.

1. Narcotic (opioid) analgesics

2. Non-opioid analgesics

Analgesics

analgesics (also known as a painkillers) are a group of drugs used to relieve pain (achieve analgesia).

DRUGS FOR THE CONTROL OF PAIN

 Pain is a physiological and emotional experience characterized by unpleasant feelings, usually

associated with trauma or disease.

 Pain may be viewed as a defense mechanism that helps people to avoid potentially damaging
situations and encourages them to seek medical help.

 Anxiety, fatigue, and depression can increase the perception of pain.

 Pain is a normal manifestation of everyday life and is an essential defense mechanism

Types of Pain

• ___________- is short term generally lasting only for the duration of tissue damage and can be
relieved once the trauma or injury is addressed and the chemical
mediators of pain are removed.

• ____________- is long lasting and can persist in the absence of pathology. Pain of at least 6
months in duration. Example is, neuropathic pain, caused by damage in
CNS.

• ____________ – occurs because visceral nerve fibers synapse at a level in the spinal cord
close to fibers supplying certain subcutaneous tissues of the body.
Examples are, pain associated with cholecystitis is referred to the back and the
scapula. Pleural pain from the diaphragm is referred to the shoulder, and
myocardial ischemia is often felt in the left arm, shoulder or jaw.

• ____________- is believed to be originated from a pathologic condition of vascular or

petivascular tissues. Distention, displacement, or pulling of cranial vessels may
account for a large portion of migraine headaches and tumors. Blood vessel
responses are thought to be associated with pain induced by cold.

• _____________- is associated with the traumatic or surgical amputation of a body part.

Patients describe the pain as residing in the missing part, with the
sensations described as itching, tingling, stabbing or burning.
 Types of Pain: accdng to location

A. ____________– pain originates in the cutaneous tissues such as skin and superficial tissues.
Pain in these structures is well defined and localized. Although the pain is of low to
moderate intensity, it stimulates the sympathetic nervous system to increase BP, PR,
and RR, dilate pupils, and increase in the tension of the skeletal muscles.

B. _____________ - arises from body organs and the pain is diffused and localized. Deep pain
originates in bone, nerves, muscles, blood vessels, and other supporting tissues of the
abdominal or thoracic cavities. It produces dull, aching sensation that is hard to
localized. Deep pain stimulates the parasympathetic nervous system, reducing the BP,
PR, but often causing N/V, weakness, syncope, and possibly loss of consciousness.

Pain Transmission Gate Theory

• Most common and well-described

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

Tissue injury causes the release of:

• _____________

• ______________

• ______________

• _____________

• ______________

These substances stimulate nerve endings,

starting the pain process

 There are two types of nerves stimulated:

• “A” fibers

and

• “C” fibers

“A” Fibers “C” Fibers

• _____________ ____________

• _____________ ____________

• _____________ _____________

• _____________ _____________
 • Sharp and Dull and
well-localized nonlocalized

 Types of pain related to proportion of “A” to “C” fibers in the damaged areas
 These pain fibers enter the spinal cord and travel up to the brain.
 The point of spinal cord entry is the DORSAL HORN.
 The______________ is the location of the “GATE.”
 This gate regulates the flow of sensory impulses to the brain.
 Closing the gate stops the impulses.
 If no impulses are transmitted to higher centers in the brain, there is ____ pain perception.
 Activation of large “A” fibers _________ gate
 Inhibits transmission to brain

o Limits perception of pain

 Activation of small “B” fibers _______ gate

 Allows impulse transmission to brain

o Pain perception

 Gate innervated by nerve fibers from brain, allowing the brain some control over gate

 Allows brain to:

o Evaluate, identify, and localize the pain

o Control the gate before the gate is open

T” cells

• Cells that control the gate have a threshold

• Impulses must overcome threshold to be sent

to the brain

• Body has endogenous neurotransmitters

• __________

• ___________

• Produced by body to fight pain

• Bind to opioid receptors

• Inhibit transmission of pain by closing gate

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

• Result:

– ________ closed, recognition of pain REDUCED

– Same pathway used by opiates

Non-pharmacologic Techniques for Pain Management

 • Acupuncture
• Biofeedback therapy
• Massage
• Heat or cold packs
• Meditation
• Relaxation therapy
• Art or music therapy
• Imagery
• Chiropractic manipulation
• Hypnosis
• Therapeutic touch
• Transcutaneous electrical nerve stimulations (TENS)
• Energy therapies (Reiki and Qi gong)

Analgesics
–are medication used to relieve pain.
–The two main categories of analgesics
• Opioids - is a natural or synthetic morphine-like substance responsible for
reducing severe pain. Opioids are narcotics substances, meaning that
they produce numbness or stupor like symptoms.
• Non Opioids.
  OPIOID (NARCOTIC) ANALGICIC

CLASSIFICATION
Strong Agonists – used to treat severe pain
Morphine (Duramorph, epimorph, Roxanol, Statex)
Fentanyl (Sunlimaze)
Hydromorphone (dilaudid)
Meperidine (Demerol)
Methadone (Dolophine, Methadose)
 
Mild-to-moderate Agonists – treating moderate pain
Codeine
Hydrocodone (Dicodid, Hycodan)
Oxycodone (Percodan, Supeudol)
Propoxyphene (Darvon, Dolene, Novopropoxyn)
 
Mixed Agonists-Antagonists – appear to have the advantage of producing adequate analgesia with less
risk of tolerance and dependence, produce less respiratory depression, and they are safer in terms of a
reduced risk of fatal overdose.
Nalbuphine (Nubain)
Butorphanol (Stadol)
Pentazocine (Talwin)
 
Antagonists – these drugs are used primarily in the treatment of opioid overdose and addiction.
Naloxone (Narcan)
Naltrexone (Trexan)
 Opioid Analgesics
• Pain relievers that contain opium, derived from the opium poppy or
• chemically related to opium
Narcotics: very strong pain relievers
EXAMPLE:
• codeine sulfate
• meperidine HCl (Demerol)
• methadone HCl (Dolophine)
• morphine sulfate
• propoxyphene HCl

Three classifications based on their actions:

• Agonist
• Agonist-antagonist
• Partial agonist

Opioid Analgesics: Site of action

• ________________
• ________________

Opioid Analgesics: Mechanism of Action

• Bind to receptors on inhibitory fibers, stimulating them
• Prevent stimulation of the GATE
• Prevent pain impulse transmission
to the brain
Three types of opioid receptors:
• _______
• ________
• _________

Opioid Analgesics: Therapeutic Uses

Main use: to alleviate moderate to severe pain

• Opioids are also used for:
– Cough center suppression
– Treatment of constipation
Opioid Analgesics: Side Effects
• Euphoria
• Nausea and vomiting
• Respiratory depression
• Urinary retention
• Diaphoresis and flushing
• Pupil constriction (________)
• Constipation

Opiate Antagonists
naloxone (Narcan)
naltrexone (Revia)
• Opiate antagonists
• Bind to opiate receptors and prevent a response
 • Used for complete or partial reversal of opioid-induced respiratory depression

Opiates: Opioid Tolerance

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

Opiates: Physical Dependence

• The physiologic adaptation of the body to
the presence of an opioid

Opiates: Psychological Dependence (addiction)

• 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 tolerance and physical dependence are expected with long-term opioid treatment and
should not be confused with psychological dependence (addiction).
 Physical dependence on opioids is seen when the opioid is abruptly discontinued or when an opioid
antagonist is administered.
• Narcotic withdrawal
• Opioid abstinence syndrome
 Narcotic Withdrawal Opioid Abstinence Syndrome
• Manifested as:
• anxiety, irritability, chills and hot flashes, joint pain, lacrimation, rhinorrhea,
diaphoresis, nausea, vomiting, abdominal cramps, diarrhea

Opioid Analgesics: Nursing Implications

• Before beginning therapy, perform a thorough history regarding allergies, use of other
medications,health history, and medical history.
• Obtain baseline vital signs and I & O.
• Assess for potential contraindications and drug interactions.
• Perform a thorough pain assessment, including nature and type of pain, precipitating and
relieving factors, remedies, and other pain treatments.
• Assessment of pain is now being considered a “______________.”
• Be sure to medicate patients before the pain becomes severe as to provide adequate analgesia
and pain control.
• Pain management includes pharmacologic and nonpharmacologic approaches. Be sure to
include other interventions as indicated.
• 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 patient’s condition or if VS are
abnormal—especially if respiratory rate is below ____________________.
• Follow proper administration guidelines for IM injections, including site rotation.
• Follow proper guidelines for IV administration, including dilution, rate of administration, and so
forth.
CHECK DOSAGES CAREFULLY
• Constipation is a common side effect and may be prevented with adequate fluid and
fiber intake.
• Instruct patients to follow directions for administration carefully, and to keep a
record of their pain experience and response to treatments.
 • Patients should be instructed to change positions slowly to prevent possible
orthostatic hypotension.
• Patients should not take other medications or OTC preparations without checking with their
physician.
• Instruct patients to notify physician for signs of allergic reaction or adverse effects.
Monitor for side effects:
• Should VS change, patient’s condition decline,
or pain continue, contact physician immediately.
• Respiratory depression may be manifested by respiratory rate of less than 12/min, dyspnea,
diminished breath sounds, or shallow breathing.
Monitor for therapeutic effects:
• Decreased complaints of pain
• Increased periods of comfort
• With improved activities of daily living, appetite,
and sense of well-being

General Use
• Management of moderate to severe pain and adjunct to general anaesthesia.
• Codeine is an effective cough suppressant.
• Morphine is used in the management of acute pulmonary edema of its peripheral vasodilating
effect.
 Contraindications

 Hypersensitivity
 Head injury or any condition that causes increased ICP and CSF pressure.
 Respiratory depression and shock (Further depression of respiration and blood
pressure)
 ranges from slow, shallow respirations to respiratory arrest.
 Depression is noted about 7 minutes after IV administration; 30 minutes after
IM injection; and 90 minutes after subcutaneous injection of morphine.

Adverse Reaction and Side Effects

• Euphoria or sedation, lightheadedness, dizziness, impaired reasoning, and respiratory
depression.
• N/V (most common side effect; Caused by stimulation of the chemoreceptor trigger zone in the
medulla, if these occurs antemetic may be indicated))
• Constipation (common side effects because motility of GIT is decreased)
• Urinary retention, esp. after surgery (because of increased tone in urethral sphincter)
• Morphine may cause biliary colic (Gallbladder attack) because of increased sphincter spasticity.
• Narcotics are sometimes used in combination with aspirin or acetaminophen
• Cardiovascular side effects: flushing, changes in heart rate, palpitations, hypotension (d/t
blunting of the baroreceptor reflex and dilation of the peripheral arterioles and veins), and
fainting.
• Respiratory depression (most serious side effect)
• Mental slowing and drowsiness; mood changes such euphoria

Nursing Precaution
• Narcotics are used carefully in patients with undiagnosed abdominal pain; liver ort renal disease;
alcoholism; prostatic hypertrophy; and history of addiction to narcotics.
• Tolerance develops with long-term use
 • Both physical and psychological dependence may occur
• Patients taking narcotics concurrently with other CNS depressants – especially alcohol,
antipsychotics, antianxiety drugs and antidepressants – need to monitored carefully.
• Pregnant women and nursing women
• Carefully prescribed for children under the age of 12 years.

Interaction
• Use of mixed narcotics in patients physically dependent on narcotics may precipitate withdrawal
symptoms
• MAOI or procarbazine with meperidine (Cause severe reactions, which can lead to death)
• S/SX of CNS depression may be enhance by narcotics are given with other class of CNS
depressants (Alcohol, antihistamines, antidepressants, MAOI, phenothiazine antipsychotics, or
sedative/hypnotics)
 
NONOPIOID ANALGESICS
Individual Agents:
 acetaminophen (Tylenol),
 misoprostol,
 phenmazopyridine
Nonsteroidal Anti-inflammatory Drugs (NSAIDs):
o ibuprofen (Advil, Motrin),
o indomethacin (Indocin),
o naproxen (Naprosyn, Naprolen),
o piroxicam (Feldene),
o celecoxib (Celebrex),
o diclofenac (Voltaren),
o rofecoxib (Vioxx),
o ketorolac
o tromethamine (Toradol),
o MFA (Ponstan),
Salicylates:
 aspirin (Acetylsalicylic Acid, ASA),
 choline magnesium trisalicylate,
 choline salicylate (Arthrophan),
 salsalate (Disalcid)
Centrally Acting Agents:
 clonidine (Catapres),
 tramadol (Ultram)

NON- STEROIDAL ANTI-INFLAMMATORY DRUGS (NSAIDS)

• NSAIDS: non steroidal anti-inflammatory drugs

• They have the important property of inhibiting prostaglandins biosynthesis
• Principal actions of NSAIDS are:
1. Analgesic action
2. Anti-inflammatory action
3. Antipyretic action

• Although there are many components to inflammation, only the prostaglandin component is
substantially reduced by the action of an NSAIDS.
 • The process of PG synthesis begins with arachidonic acid, this acid is converted by the enzyme
cycloxygenase to synthesize different prostaglandins.
• NSAIDS drugs work by interfering with cycloxygenase pathway.
• There are two types of cycloxygenase denoted COX-1 and COX-2 .

Classification of NSAIDS:

A. Nonselective COX inhibitors

1.Salicylates: Aspirin, Diflunasil
2.Pyrazolone derivatives: Phenylbutazone, Oxyphenbutazone
3.Indole derivatives: Indomethacin
4.Propionic acid derivatives: Ibuprofen, Naproxen, Ketoprofen
5.Anthranilic acid derivatives: Mephenamic acid
6.Aryl-acetic acid derivatives: Diclofenac
7.Oxicam derivatives: Piroxicam
8.Pyrrolo-pyrrole derivatives: Ketorolac

B.Preferential COX-2 inhibitors

• Nimesulide, Meloxicam, Nabumetone

C.Selective COX-2 inhibitors

• Celecoxib, Rofecoxib, Valdecoxib

D.Analgesic-antipyretics with poor anti-inflammatory action

1.Paraaminophenol derivatives: Paracetamol (Acetaminophen)
2.Pyrazolone derivatives: Metamizol
3.Benzoxazocine derivatives: Nefopam

Common adverse effects of NSAIDS:

1. GIT
• Gastric ulceration
• Nausea
• Vomiting
2. Hypersensitivity
• Rashes
• Rhinitis
• Asthma
3. Liver
• Liver damage
4. Kidney
• Chronic intestinal nephritis
• Renal tubular necrosis
• Reversible acute renal failure
5. Blood
• Thrombocytopenia
• Decreased platelet aggregation
• Impaired clotting
6. CVS
• Hypertension
• Congestive heart failureUI
7. CNS
 • Headache
• Confusion
• Hallucinations
• Depression
• Tremor
ASPIRIN (ACETYLSALICYLIC ACID)
• Source: __________________________
• Chemical nature: weak organic acid
• Non-opioid analgesics
• Aspirin is the initial drug of choice for treating the majority of articular (arrthritis) and
musculoskeletal disorders

The principal effects of aspirin are:

1. ____________________
2. ____________________
3. ____________________
4. ____________________

Pharmacokinetics of aspirin:
1. Routes of administration: oral, parenteral
2. Absorption: well absorbed from stomach
3. Distribution: highly protein bound
4. Metabolism: hydrolysis
5. Excretion: renal

Indication of aspirin:
1. To relieve mild to moderate pain:
• Headache
• Myalgia
• Arthralgia
• Osteoarrthritis
2. Acute rheumatic fever
3. Rheumatoid arrthritis
4. Arterial thromboembolism
5. Myocardial infarction
6. Treatment of migraine

Contraindication of aspirin:
1. Pre-existing ulceration in the GIT
2. Coagulation disorders
3. Hepatic and renal disease
4. Any hypersensitivity to aspirin
5. Pregnancy (last trimester)
• Causes prolongation of labor
• Chance of intra-cranial hemorrhage
• Causes premature closure of __________________

Adverse effects of aspirin:

1. Gastric and duodenal ulceration
2. Impaired clotting
3. Hepatic and renal damage
 4. Deafness (overdose)
5. Allergic manifestations

PARACETAMOL (ACETAMINOPHEN)
• Popular domestic antipyretic and analgesic drug
• Normally a safe drug, acute overdose causes hepatotoxicity
• Useful in patients who should avoid aspirin
( because of gut intolerance, bleeding tendency, allergy)

Pharmacological actions of paracetamol

1. Weak analgesic potency
2. Antipyretic
3. Little or no anti-inflammatory action
4. No anti-platelet action
Pharmacokinetics of paracetamol
1. R/A: orally administered
2. Absorption: rapidly from the GIT
3. Metabolism: liver
4. Excretion: kidney
Indication of paracetamol
1. ______________
2. ______________
3. ______________
4. ______________
5. _______________
Adverse effects:
1. Skin rash, allergy
2. Chronic renal disease (long term use)
3. Hepatotoxicity in acute overdose

INDOMETHACIN
Pharmacological actions
1. Strong anti-inflammatory agent than aspirin
2. Antipyretic
3. Analgesic
4. Rapid absorption from the GIT
5. Safe in patient with gout
6. Does not modify the action of oral anticoagulants
Indications:
1. Rheumatoid arthritis
2. Ankylosing spondylitis
3. Osteoarthritis
4. Acute Gout
5. Treatment of patent _______________in premature infant
6. Pericarditis

Contraindications
1. Pre-existing gastric ulcer
2. Pregnancy, nursing mother
 3. Renal disorders
4. Psychiatric disorders
5. Epilepsy
6. Parkinsonism

Adverse effects of indomethacin:

1. GIT: nausea, vomiting, ulceration
2. CNS: dizziness, vertigo, confusion
3. Hypersensitivity: rash, itching
4. Hematological: neutropenia, thrombocytopenia

IBUPROFEN
Pharmacological actions of ibuprofen:
1. Potent analgesic than aspirin or paracetamol
2. Anti-inflammatory action
3. Antiplatelet action
Indications:
1. _______________
2. _______________
(adverse effects, contraindication same as aspirin)
Advantage over aspirin: less incidence of GIT ulceration with low dose

DICLOFENAC
Pharmacological action of diclofenac:
1. Potent anti-inflammatory action
2. Potent analgesic action
3. Potent antipyretic action
Pharmacokinetics of diclofenac:
1. R/A: oral, injectable
2. Absorption: rapid from the GIT
3. Plasma half life: 12hrs
4. Distribution: highly protein bound
Indications:
1. Rheumatoid arthritis
2. Osteoarhtritis
3. Ankylosing spondylitis
4. Post-operative patient
5. Dysmenorrhoea
(adverse effects, contraindication same as aspirin)

Contraindications
• All NSAIDs are CIx if the patient is hypersensitive to aspirin
• Acetaminophen is the only nonnarcotic analgesic safe for use in pregnancy, provided it is used
only occasionally.
• All salicylates are CIx in persons under the age of 12 years (Risk of Reye’s syndrome, a
potentially fatal disease involving brain and liver dysfunction)
• Bleeding disorders (Hemophilia, von Willebrands disease, and Talangiectasia)
• Favism (genetic G6PD enzyme deficiency)
 
Adverse Reactions and Side Effects
 • GI discomfort and irritation (diarrhea, N/V: d/t to an effect on the vomiting center in the
medulla, abdominal pain, flatulence and even GI bleeding and ulceration: d/t antiprostaglandin
action increases gastric acid secretion and decreasing the protective mucus secretion in the
stomach and intestine)
• Tinnitus and hearing loss (common on large doses of salicylates, esp. ASA; d/t increased
pressure in the labyrinth of the inner ear or by an effect on the hair cells of the cochlea)
• Weakness, profuse sweating, and slowed respiration and heart rate (d/t toxic doses of
salicylates)
Nursing Precautions
• Should be taken with full glass of water and with meals
• Monitored close for clients with history of GI bleeding or bleeding disorders
• Cautiously given to clients with severe cardiovascular (NSAIDs may cause fluid retention and
further decrease cardiac function), liver or kidney disease (serum levels of the drugs may
become elevated, increasing the risk of toxicity)
• Asthma or nasal polyps and those allergic to ASA (High risk of developing hypersensitivity).
• Monitor for nephrotoxicity (dysuria, hematuria, oliguria: BUN, creatinine, ASL, ALT, hemoglobin)
• Monitor for blood dyscrasias, hepatitis, and allergic response (rash and urticaria)