OPIOID AND NONOPIOID ANALGESICS

PharmacologyKendi Lyles, Verna Meadows, Janet Olbert, Brooke Robinson and Olethea TennysonJuly 18, 2009

ACTIONS AND USES OF MEDICATION

OPIOID CATEGORIES Natural

Morphine Codeine Thebaine

Video http://youtube.com/watch?v=9nQQzH4rH7

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OPIOID CATEGORIES Semi-synthetic

Hydromorphone Hydrocodone Oxycodone Oxymorphone Desmorphine Heroin Nicomorphine Dipropanoylmorphine Benzylmorphine Ethylmorphine

OPIOID CATEGORIES Fully synthetic

Fentanyl Pethidine Methadone Tramadol Propoxyphene

Video http://www.youtube.com/watch?v=RCjIwHi

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OPIOID CATEGORIES Endogenous Opioid Peptides

naturally produced by the body endorphins enkephalins dynophins endomorphins

OPIOID ACTIONS Opioids work in two ways

Attach to opioid receptors specific proteins on the surface of cells in the

brain, spine and GI tract Work in the brain to alter the sensation of

pain

OPIOID USES Post-operative pain Cancer pain Non-malignant chronic pain Cough Diarrhea

Loperamide does not cross the blood-brain barrier and only acts on smooth muscle (the digestive tract)

OPIOID USES Painful wounds

Topical morphine Detoxification

Methadone and buprenorphine only Back, neck or joint pain Dental pain Painful diabetic neuropathy Migraines

NONOPIOID CATEGORIES There are several different types of

nonopioids they include acetaminophen, NSAIDS which are aspirin, Motrin and Advil and also naproxen. They are less potent than opioids.

They are used to treat mild to moderate pain.

Nonopioids are usually purchased over-the-counter, but (Cox-2 inhibitors require a prescription.

NONOPIOID USES Nonopioids are effective for the dull,

throbbing pain of headaches,dysmenorrhea which is menstrual pain, inflammation, minor abrasion, muscular aches and pain, and mild to moderate arthritis. Most analgesics also have an antipyretic effect and will lower an elevated body temperature. Some, such as aspirin, have anti-inflammatory and antiplaelet effects as well.

NSAID’S All nonsterioial anti-inflammatory drugs

have an analgesic effect as well as an antipyretic and anti-inflammatory action. Some examples of NSAIDS are aspirin, ibuprofen which include (Motrin IB, nuprin, Advil, medipren) and naproxen(aleve) all of them can be purchased as OTC drugs.

ASPIRIN

ASPIRIN Aspirin, a salicylate NSAID, is the oldest nonopioid

analgesic still in use. Aspirin is a analgesic, antipyretic, and anti-inflammatory Aspirin decreases platelet aggregation. Aspirin is in a group of drugs called salicylates.

It works by reducing substances in the body that cause pain, fever, and inflammation.

Aspirin is used to treat mild to moderate pain, and also to reduce fever or inflammation.

It is sometimes used to treat or prevent heart attacks, strokes, and angina.

NAPROXEN

NAPROXEN Naproxen is rapidly and completely absorbed from the gastrointestinal tract with

an in vivo bioavailability of 95%. The elimination half-life of Naproxen ranges from 12 to 17 hours. Steady-state levels of Naproxen are reached in 4 to 5 days, and the degree of Naproxen accumulation is consistent with this half-life.

Absorption Peak plasma levels of Naproxen given as Naproxen suspension are attained in 1

to 4 hours. Distribution

Naproxen has a volume of distribution of 0.16 L/kg. At therapeutic levels Naproxen is greater than 99% albumin-bound. At doses of Naproxen greater than 500 mg/day there is less than proportional increase in plasma levels due to an increase in clearance caused by saturation of plasma protein binding at higher doses (average trough Css 36.5 mg/L, 49.2 mg/L and 56.4 mg/L with 500 mg, 1000 mg and 1500 mg daily doses of Naproxen, respectively). The Naproxen anion has been found in the milk of lactating women at a concentration equivalent to approximately 1% of maximum Naproxen concentration in plasma

NAPROXEN Metabolism

Naproxen is extensively metabolized to 6-0-desmethyl Naproxen, and both parent and metabolites do not induce metabolizing enzymes. Both Naproxen and 6-0-desmethyl Naproxen are further metabolized to their respective acylglucuronide conjugated metabolites.

Excretion The clearance of Naproxen is 0.13 mL/min/kg. Approximately 95% of the

Naproxen from any dose is excreted in the urine, primarily as Naproxen (<1%), 6-0-desmethyl Naproxen (<1%) or their conjugates (66% to 92%). The plasma half-life of the Naproxen anion in humans ranges from 12 to 17 hours. The corresponding half-lives of both Naproxen’s metabolites and conjugates are shorter than 12 hours, and their rates of excretion have been found to coincide closely with the rate of Naproxen disappearance from the plasma. Small amounts, 3% or less of the administered dose, are excreted in the feces. In patients with renal failure metabolites may accumulate. http://www.drugs.com/pro/naproxen.html

NAPROXEN Naproxen Oral Suspension is indicated: For the relief of the signs and symptoms of rheumatoid arthritis For the relief of the signs and symptoms of osteoarthritis For the relief of the signs and symptoms of ankylosing spondylitis For the relief of the signs and symptoms of juvenile arthritis Naproxen Oral Suspension is recommended for juvenile rheumatoid

arthritis in order to obtain the maximum dosage flexibility based on the patient’s weight.

Naproxen Oral Suspension is also indicated: For relief of the signs and symptoms of tendonitis For relief of the signs and symptoms of bursitis For relief of the signs and symptoms of acute gout For the management of pain For the management of primary dysmenorrhea

http://www.drugs.com/pro/naproxen.html

IBUPROFEN

IBUPROFEN Generic name Brand names include:

Advil, Advil Childrens, Advil Junior Strength, Advil Liquigel, Advil Migraine, Childrens Ibuprofen Berry, Genpril, IBU-200, Midol IB, Midol Maximum Strength Cramp Formula, Motrin, Motrin Childrens, Motrin IB, Motrin Infant Drops, Motrin Junior Strength, Motrin Migraine Pain, Nuprin.

IBUPROFEN Indicated for relief of the signs and symptoms of

rheumatoid arthritis and osteoarthritis. Indicated for relief of mild to moderate pain. Indicated for the treatment of primary dysmenorrhea. In patients with primary dysmenorrhea, Ibuprofen

tablets have been shown to reduce elevated levels of prostaglandin activity in the menstrual fluid and to reduce resting and active intrauterine pressure, as well as the frequency of uterine contractions. The probable mechanism of action is to inhibit prostaglandin synthesis rather than simply to provide analgesia.

IBUPROFEN Ibuprofen tablets are rapidly absorbed.

Peak serum Ibuprofen levels are generally attained one to two hours after administration. With single doses up to 800 mg, a linear relationship exists between amount of drug administered and the integrated area under the serum drug concentration vs. time curve.

Ibuprofen is rapidly metabolized and eliminated in the urine. The excretion of Ibuprofen is virtually complete 24

hours after the last dose. The serum half-life is 1.8 to 2.0 hours.

ACETAMINOPHEN The analgesic acetaminophen is a

popular nonprescription drug for the relief of pain, discomfort, and fever in infants, children, adults, and older adults.

Acetaminophen, unlike aspirin, does not have an anti-inflammatory process.

ACETAMINOPHEN Acetaminophen is well absorbed fro the

gastrointestinal tract. Rectal absorption may be erratic

because of the presence of fecal material or a decrease in blood flow to the colon.

Because of its short half-life it cam be administered every four hours as needed with a maximum dose of 4g a day.

ACETAMINOPHEN Acetaminophen weakly inhibits

prostaglandin synthesis, which decrease pain sensation.

It is effective in eliminating mild to moderate pain and headaches and is useful for its antipyretic effect.

It does not possess anti-inflammatory action. Its onset of action is rapid, and the duration of action is 5 hours or less.

ACETAMINOPHEN Some examples of products that have

acetaminophen in it are Acephen, Actamin, Feverall, Q-Pap, Tactinal, Tempra, Tylenol, Uniserts, Vitapap.

ACETAMINOPHEN

TYLENOL

TYLENOL Tylenol is a product that has acetaminophen.

Used for the head and body pain, for colds and cough, fevers, arthritis, allergies and sinus, pain and sleepiness

For children it is the product most parents used to help in fever reducer.

Combined—to reduce fever and for the temporary relief of minor aches and pains due to:

Headache. Muscular aches. Backache. Minor pain of arthritis. The common cold. Toothache. Premenstrual and menstrual cramps . Temporarily reduces fever.

SIDE EFFECTS AND ADVERSE EFFECTS

OPIOID ANALGESICS Have many more side effects than

nonopioid drugs. Most severe side effect is constipation

Can be avoided or reduced if a stool softener/laxative is taken while using opioid analgesics.

OPIOID ANALGESICS Other possible side effects

Nausea/vomiting Confusion Decrease in blood pressure/orthostatic

hypotension Drowsiness Respiratory depression Sedation Urinary retention Antitussive effects

NONOPIOID ANALGESICS As a group, these have one major side

effect which is gastrointestinal system upset/disturbance.

Other side effects can be present with nonopioid analgesic drugs.

NSAIDs Can cause stomach ulcers and bleeding They break down the protective lining of the

stomach

NONOPIOID ANALGESICS Over use or abuse of nonopioid

analgesics can also cause kidney and/or liver damage which can ultimately result in organ failure.

NURSING IMPLICATIONS

OPIOID ANALGESICS

OPIOID ANALGESICS Nurses must increase their knowledge

about pain, take every client’s pain seriously, and implement measures for treating pain effectively. Whenever a client’s pain is not controlled to his or her satisfaction, the nurse pursues better goal achievement by collaborating with pain experts.

OPIOID IMPLICATIONS The nurse needs to monitor vital signs

at frequent intervals to detect respiratory changes. Respirations of <10/min can indicate respiratory stress.

OPIOID IMPLICATIONS Record client’s urine output because

urinary retention is a side effect of morphine. Urine output should be at least 600 ml/day.

NON-OPIOID ANALGESICS

NONOPIOID IMPLICATIONS While liver enzymes should be

monitored, nurses should be prepared to do more client teaching with nonopioid analgesics

Clients should be taught to not take acetaminophen for more than 10 days in adults or 5 days with children to prevent liver damage.

NONOPIOID IMPLICATIONS If it appears a client could have

overdosed on these medications, toxicity levels should be checked Normal serum is 5 to 20 mcg/ml Toxic level is >50mcg/ml Levels of >200 mcg/ml are an indication of

heatoxicity

OPIOID OR NONOPIOID?? Evaluate client pain

level Start with the

lowest possible pain reliever that will help the client

Monitor the client for pain relief or adverse reactions

REFERENCES http://www.udel.edu/chem/theopold/ch

em465/copland.udel.edu/~rmarcus/drug%20chart.gif

http://www.clinicaladvisor.com/Media/Images/36/feature1208-pain_fig1_35070_35073.gif

http://www.spineunivers.com/displayarticle.php/article1345.html

http://en.wikipedia.org/wiki/Opioid Kee, Hayes and McCuistion (2009),

Pharmacology, A Nursing Process, 6th Edition, Saunders Elsvier

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_does_aspirin_work http://health.yahoo.com/children-resources/acetaminop

hen-oral-rectal/healthwise--d00049a1.html http://www.drugs.com/pro/ibuprofen.html http://www.drugs.com/aspirin.html http://www.migraines.org/treatment/images/tylenol.gif http://www.pharmacy-and-drugs.com/reviews/Ibuprofen.

jpg http://www.tylenol.com/ http://www.pharmacy-and-drugs.com/reviews/Naproxen.

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