Drugs To Treat Pain

NURSING PHARMACOLOGY
DRUGS TO PREVENT AND TREAT PAIN

PAIN
Is an unpleasant sensation of physical discomfort
Highly subjective and difficult to define
It is whatever the person says it is and exists whenever the person says it does
An acute pain is useful because it signals pathologic situations
Regardless of etiology, pain has both sensory (perception) and affective (interpretation)
components
Relatively constant pain threshold exists in all person
Pain tolerance is the point beyond which pain becomes unbearable, varies among
individuals
Assessment of Pain
Check pain prior to medicating and 1 hour after medicating
Pain is subjective but affected by factors:
culture
patients expectations
influences
associated diseases
psychologic factors
Ask For:
Location of pain
Type of pain
GRACE ANN L. LAGURA, RN MAN Page 1
TYPES OF PAIN
Acute Pain
Short term
Has an immediate onset
Relieved once the trauma is addressed
Visceral Pain
Arises from body organs
Pain sensations are diffused and poorly localized
Visceral nociceptors transmit referred pain
Referred Pain
Peculiar and intense although there is little or no pain at the point of the noxious stimuli
Vascular Pain
Pain is believed to originate from a pathologic condition of vascular or perivascular

origin
Chronic Pain
Pain at least with 6 months in duration
May occur with or without tissue damage
Often unresponsive to conventional treatment
Phantom Pain
Pain is associated with traumatic or surgical amputation of a body part
Central Pain
Pain is associated with lesions, tumors, inflammation in the brain
Manifested as high frequency or bursts of impulses that patients describe as severe,

spontaneous and often unyielding
Thalamic Pain
Describe as hyperthesia (abnormally increased sensitivity to stimuli) in one half of the

body
Psychogenic Pain
Pain is caused by psychologic factors rather than physiologic dysfunction
Real to the patient
OPIOID
Derived from opium
OPIATE compounds present in opium
NARCOTICS means analgesia, CNS depressants, or any drug that produce dependence
This may include cocaine, marijuana, LSD
Endogenous Opioid Peptides:
Enkephalins
Endorphins
Dynorphins
These are found in the CNS and peripheral tissues; they contain opioid-like properties; they
serve as neurotransmitters, neuorohormones or neuromodulators
Physical Dependence:
Taking the drug for prolonged period of time
state of abstinence syndrome will occur if the dependence-producing drug is withdrawn

abruptly
Adaptive cellular changes occur in response to continued presence of the drug
2 FACTORS:
Half life morphine has short half life; methadone has long half life
Degree of physical dependence parallels with withdrawal syndrome
WITHDRAWAL SYNDROME
- Yawning
- sneezing & weakness
- Rhinorrhea
- nausea/vomiting
- Sweating
- abdominal cramps
- Anorexia
- diarrhea
- Irritability
- muscle spasms
- Gooseflesh (cold turkey)
- kicking movements
In Acute Pain:
Even 2-3 grams TID is no cause for physical dependence and withdrawal syndrome
should drug be discontinued abruptly
In Utero:
Babies are born drug dependent
Abstinence syndrome may occur opium tincture is given in smaller doses
Abuse
Drug use inconsistent with medical or social norms
TOLERANCE
A larger dose is required to produce the same response that is formerly elicited by a
small dose
Produces little effect than when treatment started
Prolonged Use of Morphine Develop TOLERANCE to:
Analgesia
Euphoria
Sedation
Respiratory depression
Little tolerance to constipation and miosis
Cross tolerance among opioid agonists
Addiction:
Continued use of psychoactive substances despite physical, psychologic or social harm
PHYSICAL DEPENDENCE, ABUSE AND ADDICITION
The excessive and unrealistic concern about the damages of addiction in the
3 TYPES OF OPIOIDS
Opioid Agonists
Agonist/Antagonist Opioids
Opioid Antagonists
OPIOID AGONISTS:
Activate Mu and Kappa receptors
Produces analgesia, euphoria, respiratory depression, sedation, decrease GI motility,

dependence
Opioids
Morphine (Contin)
Codeine (Paveral)
Fentanyl
Meperidine (Demerol)
Oxycodone (Numorphan)
Methadone (Dolophine)
Levophanol (Levorphan)
Hydromorphone (Dilaudid)
ACT AS ANALGESIA
Relieve moderate to severe pain of various causes
Increases the threshhold for pain perception
Reduces anxiety and fear
Reduces pain but does not alter sensations
Indications:
Post operative pain
Labor and delivery
Cancer pain
MI
For constant and dull pain
Opioid Peptides and Morphine:
Structurally the same
Binds to the same receptors in the brain
Cross tolerance to analgesia
Blocked by the same antagonist (Naloxone)
Opioids Produce Respiratory Depression:
If given IV within 7 minutes
If given IM 30 minutes
If given SC 90 minutes
Tolerance develops in long term use
Monitor RR (if below 12bpm, withhold the drug)
Avoid cuncurrent use of other drugs that may cause respiratory depression
Cause Constipation:
Suppress propulsive intestinal contractions
Increases tone of anal sphincter
Decreases GI secretions
May require prophylactic drug (laxatives)

GIVE: Methylnatrexone (opioid anatagonist)
blocks opioid receptors in the intestines and induce laxation and increases
intestinal transit time
Not absorbed in the GI and systemic circulation
Do not block analgesia in the brain and spinal cord
Orthostatic Hypotension:
Decreases blood pressure by blocking the baroreceptor
Dilates peripheral veins and arteries
Releases histamine causing vasodilation
Urinary Retention:
Hesitancy by increasing tone of the bladder sphincter
Increases tone of the detrusor muscles
Suppresses awareness of bladder stimuli (esp. in BPH)
Releases ADH
Not given with anticholinergics
Antitussive:
Suppresses the cough center
Accumulation of secretions in the airway
Biliary Colic:
Causes spasms of the common bile duct
Morphine may intensify pain rather than relieve
MEPERIDINE - causes less smooth muscle spasms
Emesis
Stimulates the CTZ
Emesis is high during the initial treatment
Associated with vestibular causes
May give antiemetics before morphine
Increase ICP
By depressing respirations, CO2 in the blood is high which dilates cerebral vasculature
Euphoria
Exaggerated sense of well being
Can enhance pain relief but a potential for abuse
DYSPHORIA anxiety and being ill at ease; occurs when morphine is taken in the absence of pain
Sedation
Drowsiness and mental clouding
Prevention:
o Smaller doses
o Using opioids with shorter half life
o Giving doses of CNS stimulants in the morning and early afternoon
Miosis
Pupils may constrict
Impairs vision in dim lights
Morphine
Not very lipid soluble
Do not cross blood brain barrier easily
Babies require lower doses because of underdevelop barriers
High FPE
GRACE ANN L. LAGURA, RN MANPage 10
Precautions:
Decrease respiratory reserve
Pregnancy
Labor and delivery
Head injury
Drug Interactions:
CNS depressants
Anticholinergics
Hypotensive drugs
MAO inhibitors
Agonist/antagonist opioids
Antiemetics
Amphetamines
Dextromethorphan
TOXICITY TO OPIOID
Respiratory depression
Pin point pupils
Coma
DOSAGES:
Patients with low tolerance to pain increase dose
Patients with extreme pain increase dose
Elderly and children lower dose
Dose should be decreased as pain subsides
OPIOIDS SHOULD BE ADMINISTERED ON FIXED SCHEDULE

BREAKTHROUGH PAIN MUST BE GIVEN SHORT ACTING PREPARATIONS
Other Strong Opioids:
Fentanyl:
More potent than morphine
For induction and maintenance of anesthesia (with Droperidol neurolept

anesthesia)
Meperidine (demerol) short half life; causes dysphoria, tremors and seizures
Methadone (dolophine) used in the treatment of addicts (detoxification)
Heroine legal in Europe to treat pain
Alfentanil/Sufentanil for induction and maintenance of anesthesia; 10 times more

potent than morphine
Ramifentanil during surgery and post operative; 100 times greater than morphine
Hydromorphone, Oxymorphone, Levorphanol
Moderate to Strong Opioids:
Produce less analgesia and respiratory depression and abuse
Codeine:
As much as 325 mg aspirin or 325 mg acetaminophen
10 mg produces antitussive effect
Oxycodone
Oral preparation
Not crushed, dissolved or injected
AGONIST/ANATAGONIST OPIOIDS
They produce analgesia and

respiratory depression at
therapeutic doses similar to
morphine.
However, there is a ceiling

effect for analgesia and
respiratory depression
Produce less analgesia
Act as Kappa agonist and Mu antagonist (all

except Buprenorphine)
Buprenorphine act as Mu partial agonist and
Pentazocine (Talwin)
Less potent than morphine
Increases cardiac workload
Precipitates abstinence syndrome in opioid dependents
Talwin NX 50 mg with 0.5 mg Naloxone to counter abuse
Nalbuphine (Nubain)
Butorphanol (Stadol)
Dezocine
Buprenorphine (Buprenex) Mu partial agonist and Kappa antagonist; naloxone cannot reverse
toxicity easily
Indications:
Relieve moderate to severe pain
Labor and delivery
Sedative before surgery
As a supplement in balance anesthesia
Little antitussive effect
Adverse Reactions & Complications:
Nausea and vomiting
Lightheadedness
Sedation & euphoria
Visual hallucinations
Disorientation
confusion
OPIOID ANTAGONISTS
NALOXONE (Narcan)
Structural analog of morphine
Reverses coma, analgesia, sedation, euphoria and respiratory depression caused

by opioids
If administered prior to opioid blocks opioid effects
If administered to an opioid-dependent, causes immediate withdrawal syndrome
Reverses toxicity caused by agonist/antagonist opioids
Reverses post operative opioid effects
Reverses neonatal respiratory depression
NALTREXONE
Reverses effects of opioid and alcohol abuse
Less successful because they do not eliminate cravings for opioids
NALMEFENE
Longer duration of action
Brings complete reversal of respiratory depression
NON OPIOID CENTRALLY ACTING ANALGESICS

TRAMADOL
Strong analgesic
Analog of codeine
Do not cause respiratory depression, dependence or abuse
Not more effective than codeine with aspirin or acetaminophen
Blocks reuptake of norepinephrine and serotonin
Less effective than morphine
Naloxone partially blocks the effects of Tramadol
CLONIDINE (Duraclon)
Clonidine (Catapres in oral or transdermal patch) treat hypertension
Given by continuous epidural infusion relieves pain
Blocks nerve traffic pathways that transmit pain sensations
Given with opioid analgesics for cancer pain (neuropathic and visceral
pain)
CYCLOOXYGENASE INHIBITORS PRODUCES:
o
Antiinflammatory action
Antipyretic
o analgesia
COX 1
COX 2
Prostaglandin
Prostacyclin
CYCLOOXYGENASE 1
Good Cox
Present in all tissues
Protect the gastrointestinal tract
Supports renal function
Promotes platelet aggregation
CYCLOOXYGENASE 2
Bad Cox
Produced at injured sites
Mediates inflammation
Sensitizes receptors to pain
Mediates fever
2 Types of COX Inhibitors:
Drugs that produce antiinflammatory effects (NSAIDs)

Drugs with no antiinflammatory effect (Acetaminophen)
FIRST GENERATION NSAIDs

Inhibit both COX 1 and COX 2
1. ASPIRIN (family of Salicylates)
Irreversible inhibitor of cyclooxygenase

Absorbed in the SI
Half life of 15-20 minutes
Distributed in all body tissues
Excreted in the kidneys (must raise ph)
Action of 1st Generation NSAIDs:
Antiinflammation
Analgesia
Antipyretic
Dysmenorrhea
platelet aggregation
Cancer prevention
Protection against Alzheimers disease
Adverse Effects: (often when giving as antiinflammatory)
Gastric distress, heartburn, nausea

Bleeding
Renal impairment
Salicylism
Reyes syndrome
Cautious Use In:
Pregnancy
Hypersensitivity reactions (may also be present in traditional NSAIDs)
Drug Interactions:
Warfarin
Glucocorticoids
Alcohol
ibuprofen
ACUTE POISONING OF ASPIRIN

20 25 grams lethal dose for adults
4 grams lethal dose for children
Results in compensated respiratory alkalosis and respiratory depression
Treatment is symptomatic
OTHER FIRST GENERATION NSAIDs:
Reversible inhibition of COX

Produce cross sensitivity to aspirin
Offers no protection against MI
2.
NONACETYLATED SALICYLATES causes little or no suppression of platelet

aggregation
choline salicylate
Mg salicylates
Na salicylate
salsalate
3.
Ibuprofen (Advil, Motrin) good inhibition of COX in the uterus
4.
Naproxen and Naprocen Na compromises renal function
5.
Diclofenac and Diclofenac with Misoprostol (Arthrotec)
6.
Indomethacin for gouty arthritis; may cause headache
7.
Ketorolac (Toradol) minimum antiinflammatory effect
8.
Piroxicam (Feldene) approved only for RA and osteoarthritis
9.
Meloxicam (Mobic) some COX 2 selectivity; for osteoarthritis
2ND GENERATION NSAIDs
COX 2 inhibitors; Coxibs
Good for chronic inflammatory disorders

Causes little adverse effects
No cardiovascular effects
Drugs:
CELECOXIB (Celebrex) may cause premature closure of Ductus Arteriosus

Rofecoxib (Vioxx)
Valdecoxib (Bextra)
ACETAMINOPHEN
Selective inhibition of Prostaglandin (limited to the CNS)
analgesic
antipyretic
Action:
Minimal inhibition of Prostaglandin in the periphery
no anti-inflammatory
no antirheumatic
no GI ulceration
no renal impairment
no platelet aggregation
METABOLISM OF ACETAMINOPHEN
MAJOR PATHWAY:
Conjugation of Glucoronic
acid
Non toxic metabolites are

excreted in the urine
MINOR PATHWAY:
Oxidized by P450 enzyme
Converted to toxic compounds
Converted to Glucothione (nontoxic)
TREATMENT FOR TOXICITY:

Acetylcysteine converts toxic substances to nontoxic forms and excreted
GOUT
A metabolic disease which pools uric acid (end product of purine metabolism)
Oversecretion of uric acid
Renal impairment which resulted to decreased excretion of uric acid
Acute Gout occurs as a result of inflammatory reaction to deposits of sodium urate crystals
in joints, tendons and bursae
Uric acid causes local infiltration of tissues by granulocytes which phagocytize urate
crystals (tophi)
ANTIGOUT DRUGS:
NSAIDs to lessen inflammation
COLCHICINE
non analgesic and non uricosuric
Inhibits the migration of granulocytes
the inhibition reduces the release of lactic acid and proinflammatory enzymes
during phagocytosis
inhibits the release of histamine from mast cells
inhibits secretion of insulin from beta cells of pancreas
effective as prophylaxis for long term use
Overdose may cause alopecia
ALLOPURINOL (Zyloprim)
Nonanalgesic
no antiinflammatory properties
non uricosuric drug
decreases production of uric acid by inhibiting the xanthine oxidase (the enzyme
that converts hypoxanthine to xanthine to uric acid)
for prophylaxis of hyperuricemia
for overproducers of uric acid and
patients with renal uric acid calculi
for patients with gout resulting
from drug therapy (anticancer drugs)
hypersensitivity may occur even after years of allopurinol therapy
URICOSURIC DRUGS
Increases the rate of uric acid secretion and reducing plasma concentration
Inhibits tubular reabsorption of urate
1.
Increases elimination of uric acid
Decreases serum uric acid level
Retards urate deposits
PROBENECID (Benemid)
inhibits the reabsorption of urate at the proximal renal tubules
inhibits excretion of penicillins and cephalosporins
2. SULFINPYRAZONE (Anturane)
similar to Probenecid
not given to patients with allergies to phenylbutazone or other pyrazoles, blood

dyscrasias and peptic ulcers
Adverse Reactions:
GI upset
Nephrotoxic syndrome
CNS stimulation
Hypersensitivity
Depression of hematopoeisis
Management:
Given with food or antacids
Increase fluid intake
Alkalinization of urine
Avoid alcohol

Drugs To Treat Pain

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Drugs To Treat Pain

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NURSING PHARMACOLOGY

DRUGS TO PREVENT AND TREAT PAIN

Is an unpleasant sensation of physical discomfort

Highly subjective and difficult to define

An acute pain is useful because it signals pathologic situations

Relatively constant pain threshold exists in all person

Check pain prior to medicating and 1 hour after medicating

Pain is subjective but affected by factors:

GRACE ANN L. LAGURA, RN MAN Page 1

Has an immediate onset

Relieved once the trauma is addressed

Arises from body organs

Pain sensations are diffused and poorly localized

Visceral nociceptors transmit referred pain

Pain is believed to originate from a pathologic condition of vascular or perivascular

Pain at least with 6 months in duration

GRACE ANN L. LAGURA, RN MAN Page 2

May occur with or without tissue damage

Often unresponsive to conventional treatment

Pain is associated with traumatic or surgical amputation of a body part

Pain is associated with lesions, tumors, inflammation in the brain

Manifested as high frequency or bursts of impulses that patients describe as severe,

Describe as hyperthesia (abnormally increased sensitivity to stimuli) in one half of the

Pain is caused by psychologic factors rather than physiologic dysfunction

Real to the patient

Derived from opium

OPIATE compounds present in opium

GRACE ANN L. LAGURA, RN MAN Page 3

Taking the drug for prolonged period of time

state of abstinence syndrome will occur if the dependence-producing drug is withdrawn

Adaptive cellular changes occur in response to continued presence of the drug

Degree of physical dependence parallels with withdrawal syndrome

- sneezing & weakness

- Gooseflesh (cold turkey)

GRACE ANN L. LAGURA, RN MAN Page 4

Babies are born drug dependent

Abstinence syndrome may occur opium tincture is given in smaller doses

Drug use inconsistent with medical or social norms

Produces little effect than when treatment started

Prolonged Use of Morphine Develop TOLERANCE to:

Little tolerance to constipation and miosis

Cross tolerance among opioid agonists

Continued use of psychoactive substances despite physical, psychologic or social harm

PHYSICAL DEPENDENCE, ABUSE AND ADDICITION

GRACE ANN L. LAGURA, RN MAN Page 5

Activate Mu and Kappa receptors

Produces analgesia, euphoria, respiratory depression, sedation, decrease GI motility,

GRACE ANN L. LAGURA, RN MAN Page 6

Relieve moderate to severe pain of various causes

Increases the threshhold for pain perception

Reduces anxiety and fear

Reduces pain but does not alter sensations

Post operative pain

Labor and delivery

For constant and dull pain

Opioid Peptides and Morphine:

Structurally the same

Binds to the same receptors in the brain

Cross tolerance to analgesia

Blocked by the same antagonist (Naloxone)

Opioids Produce Respiratory Depression:

If given IV within 7 minutes