Chapter 5 Nonopioid Analgesics THIS ONE

7/27/2019 Chapter 5 Nonopioid Analgesics THIS ONE

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Premedication Regimen

No allergy to Penicillin

2g or 2000mg Amoxicillin one hr prior to

appt time

RX:

Amoxicillin 500mg caps

Dispense 4

Take four capsules 1 hour before appointment

time.

Refills Zero


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Premedication Regimen

Allergy to Penicillin

600mg Clindamycin

Available in 150 mg or 300mg capsules RX:

Clindamycin 150 mg capsules

Take 4 caps 1 h before appointment time. Refills Zero


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Nonopioid (Non Narcotic)

AnalgesicsChapter 5


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Pain

Pain is the means by which the body ismade urgently aware of the presence oftissue damage. Suffering or distress of

the body and or mind.

Protective reflex for self-preservation

Diagnostic symptom of an underlyingpathologic condition


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Pain

Pain Control is of great importance in the

dental office

Pain brings patient to the dental office

Conversely, pain will keep patient away from the

dental office

Provider needs to recognize and evaluate

a patients need for medication


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Two components of pain

Perceptionphys ical componentof pain

Involves the message of pain that is

carried through the nerves eventually tothe cortex.

Reaction psycho logical component

of pain, involves the patients emotionalresponse to the pain.


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Pain Threshold

Individuals perceive pain but reactdifferently to it.

Decrease in pain threshold-greater

reaction to pain. Decrease in PT associated with emotional

instability, anxiety, youth, fatigue, certain

nationalities, women, fear, andapprehension.


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Raise Pain Threshold

Getting adequate sleep

Sympathy-understanding

Activities-hold a pts hand, talk with thepatient, stay busy, swim, hot shower,

meditation, etc..

Analgesics- Tylenol, Advil, Motrin, Aspirin


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Pain Threshold

Analgesic therapy must be selected for the

individual

A level of discomfort that may not require

drug treatment in one person may demand

extreme therapy in another


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Classification of Analgesic Agents

Divided into 2 groups

1-Nonopiods-aka: nonnarcotic,

peripheral, mild, and antipyretic,

analgesics.

Site of action-peripheral nerve endings,

mediated centrally

2-Opiods-aka: narcotic central, or strong

group.

Site of action-act primarily on the central

nervous system


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More Actions

Action of non-opioid analgesics related to

theirability to inhibit prostaglandin

synthesis

Opioids affect the response to pain by

depressing the CNS


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Non-Opioids

Non-opioids are divided into:

salicylates (aspirin-like) i.e Anacin,

Diflunisal

acetylsalicylic acid (ASA)

acetic acid and salicylic acid

acetic acid imparts the vinegar odor to a

bottle of aspirin when it gets old

-


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Non-Opioids

acetaminophen (Tylenol)

NSAIDs (nonsteroidal anti-inflammatory

drugs/agents) i.e. Advil, ibuprofen,

Naproxen, Etodolac, Ketoprofen


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Salicylates

From extracts of willow bark and containsalicin that have been used to reduce

fever

Chemical name: acetylsalicylicacid=ASA=aspirin

ASA HA(acetic acid) + SA(salicytic acid)

Acetic acid has characteristic of vinegarodor = ifyour bottle of aspirin STINKS,

then it is time for a new one

Metabolized via zero order kinetics


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Acetylsalicylic Acid

Mechanism of Action

Analgesic - pain reliever

Better to give before pain begins, effectiveagainst throbbing pain vs. a stabbing pain.

Inhibits prostaglandin synthesis Inhibits enzyme cyclo-oxygenase (COX or COX II)

What types of procedures or dental problemscome to mind when you hear a patient saythrobbing pain? Stabbing pain?

A t l li li A id


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Mechanism of Action

What are prostaglandins?

From arachidonic acid

Are lipids that are synthesized locally by

inflammatory stimuli

Sensitize pain receptors to bradykinin

Bradykinin has two receptors

B1 involved with tissue injury, chronic pain andplays a role with inflammation

A t l li li A id


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Mechanism of Action

aspirin blocks the synthesis of

prostaglandins

Effective if given before painful stimuli are

experienced

More effective against throbbing pain

Due to inflammation


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Acetylsalicyclic Acid

Mechanism of Action Antipyretic - fever reducer-induces

peripheral vasodilation and sweating

Reduces prostaglandin synthesis in the

hypothalamus The higher the prostaglandin synthesis the higher

the body temp

Anti-inflammatory- inflammation reducer

(by inhibiting prostaglandin synthesis) Prostaglandins strong vasodilators-capillary

permeability

aspirin decreases erythema and swelling


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Acetylsalicyclic Acid

Mechanism of Action

Anti-platelet effects blood thinner

Irreversibly binds to platelets and reduces

platelet adhesivenessAll platelets affected (will not normally clot)

New platelets will need to form (4-7 days)

After 20% of platelets replaced normal clotting

returns (about 36 hours)

Taken orally absorbed in small intestine

ASA (cont)


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ASA (cont) Reaches peak effect

on empty stomach in

30 minutes Buffered tablet in 20

minutes- buffer will

help the aspirin be

dispersed, and

dissolved quicker, it

has higher blood

levels Buffer = slower

absorption but that is

offset by the faster

rate of dissolution


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ASA (cont) Given orally or rectally

Never apply directly to tooth or mucosa =painful ulceration

Take when MI is suspected

GI effects (most frequent effect)-nausea,vomiting, gastric irritation, may exacerbatepreexisting ulcers, gastritis, or hernia

Antacids reduce absorption with diflunisal Metabolized in the liver

Excreted by the kidney


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ASA common drug reactions warfarin (Coumadin)=bleeding

Methotrexate (cancer drug)

probenecid (gout medicine)

Interferes with ACE inhibitors, beta blockers,

reducing antihypertensive effects Dosage for aspirin

Fever = 325 to 650mg every 4 hours

Arthritis = between 3-6gm a day

LD for pediatrics 4 gm, adults 10-30 gm

Enteric-Coated Aspirin-coat dissolves in the

intestine rather than the stomach

Aspirin with caffeine is more effective


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ASA common drug reactions and

contraindications

Inhibits prothrombin production resulting inhypoprothrombinemia

In children and adolescentsassociated withReyes Syndrome when taken for chicken poxand influenza. (use Tylenol instead)

No use during pregnancy

Allergy=usually occurs in asthmatics Nasal polyps, asthma, and aspirin

hypersensitivity

Triad usually occurs


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ASA common drug reactions

and contraindications

True allergy to aspirin is uncommon

Toxic levels taken=salicylismtinnitus,

headache, dizziness, dimness of vision,electrolyte imbalance, hyperthermia

All meds should be in childproofcontainers


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ASA common drug

combinations

Can add to a sedative, but preferred to

prescribe separately for more control

Mix with another opioid can allow a

decrease in the amount of opioid in the

product and reduce side effects


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diflunisal (Dolobid)

Advantages-thought to have no effect onplatelets and no cross-hypersensitivity withaspirin

Fewer GI side effects (not much proof of) Contain magnesium, contraindicated in

renal disease

This is a salicylate classified as anNSAID

Premed with this to delay post op pain

Given 2-3x/day; no useful antipyretic effect


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diflunisal (Dolobid)

Classified as an NSAID

Peak action 2-3 hrs after ingestion

Not recommended for acute dental pain

May take before dental pain
http://www.drugs.com/pdr/images/P05323C5.jpg


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NSAIAs or NSAIDs

Brand Names

Generic


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Nonsteroidal Antiinflammatory

Agents

Kissin cousins of aspirin ??Most useful drug group for tx of dental

pain

Classified by chemical make-up/Name(pg. 57)

Common Rx for pain = propionic acid

derivitives-naproxen sodium (Anaprox)

-naproxen (Naprosyn)

-ibu rofen Advil, Motrin


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NSAIDs

Some other commonly used derivatives:

Acetic acid derivatives

indomethacin (Indocin)

etodolac (Lodine)

diclofenac (Voltaren)

Salicylates (but classified as a NSAID)

diflunisal (Dolobid) Oxicams

proxicam (Feldene)


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Mechanism of Action

Inhibit prostaglandin synthesis by inhibiting

the enzyme COX COX I and II

ibuprofen (Advil)

naproxen (Naprosyn, Aleve)

meclofenamate (Meclomen)

COX I specific

indomethacin

COX II

celecoxib (Celebrex)

Most peak in 1-2 hours


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Mechanism of Action

Take with food to reduce the rate of

absorption

Antacids have no effect on absorption except

diflunisal

Used as an analgesic, anti-inflammatory,

antipyretic, especially rec. for menstrual

cramps (dysmenorrhea)

Metabolized in the liver

Excreted via kidneys


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Mechanism of Action

Tissue Injury TriggersCOXII in periphery

tissue

COXII will convertarachidonic acid toprostaglandin E2

(PGE2)

Results in stimulationof the nociceptor inperipheral nerve to

send a signal for painin the CNS

A nociceptor is a sensory receptor that sends

signals that cause the perception of pain in

response to potentially damaging stimulus


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Adverse Reactions

GI irritation, pain, bleeding, increase acid

secretion

CNS-vertigo, headache, depression,

convulsions

These are not addicting, no tolerance, no

withdrawal


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Adverse Reactions

Reversibly inhibit platelet aggregation:

Effect lasts as long as med in blood

No need to wait for new platelets to form

ibuprofen in the blood 1 day

naproxen 4 days

oxaprozin 2 weeks

Adverse reactions (cont)


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Adverse reactions (cont)

Cause Lithium toxicity, increase effect of

digoxin ( used for heart failure), reduceseffects forB-blockers, ACE inhibitors

and diuretics

Hypersensitivity-hives, itching, chills, fever Dry mouth, gingival ulcerations

Renal effects

Contraindicated for pregnancyprolongsgestation (Category C)

Use with caution in pt.s with renal and

hepatic conditions, sens. to aspirin

Therapeutic Uses


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Therapeutic Uses

Osteoarthritis, pain, fever, dysmenorrhea

Manage dental pain Take with full glass of water, and food

Use caution when driving

Do not use with aspirin Do not take OTC analgesics with Rx

NSAIAs

If pain does not subside call DDS


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Specifics on NSAIDs - ibuprofen Ibuprofen (Advil, Motrin)

-onset 30 mins, duration2-4 hrs.

-metabolized in liver,

excreted by kidneys

-Drug of choice for dental

pain

-400-800mg every 4-6

hrs.-do not exceed 3200mg

in a 24 hour period

- dose = anti-inflam.

-200mg capsules,

tablet = OTC

-400, 600, 800mg = Rx-more effective than

ace. with codeine,

-double doses of ace.

C I hibit


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Cox Inhibitors

Specific Cox II inhibitors block the enzyme

that is synthesized when inflammationoccurs

-Celebra, Celebrex (lowest dose

possible)(higher GI upset), refecoxib(Vioxx) and valdecoxib (Bextra) (off the

market) (arthritis)

Cox I-widely distributed, always presentenzyme

-responsible for adverse effects of

NSAIDs.

N d N


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Naproxen and Naproxen

Sodium Proprionic acid derivative NSAID

Slightly longer half lives

Dosed on an 8-12 hour schedule Longer acting

Need loading dose

naproxen 500 mg stat; 250 mg q 6-8; max

daily = 1500mg (peaks in 2-4h)

naproxen sodium 550mg stat;275 mg q6-8h

daily max = 1375 (peaks in 1-2h)

Will cause lithium levels to rise


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ACETAMINOPHEN

USES


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USESANALGESIC AND ANTIPYRETIC

PT WITH ASPIRIN SENSITIVITY PT WITH GI UPSET FROM ASPIRIN

YOUNG CHILDREN

Dose 1-2 tabs/caps (325 to 650mg) every4 -6 hours OR 1000mg -3-4 X/day

FDA does not recommend more than 650mg every 4-6 hours, 3-4X/day

4000mg/day

New recommended single dose

Must include a box warning mostdangerous type for liver failure

USES


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USES

Dose 1-2 tabs/caps (325 to 650mg) every4 -6 hours OR 1000mg -3-4 X/dayDo notgive to children


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Ph l i Eff t


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Pharmacologic Effects Rapidly absorbed form GI

Peaks in 1-3 hours Large doses produce a metabolite in liver

that can be hepatotoxic and nephrotoxic

Equally efficacious as aspirin (pain) andjust as potent for fever and pain.

Alcoholics avoid acetominophen

No effect on resp. or CV. No GI bleeding Does not produce or affect platelet

adhesiveness, or uric acid excretion

Ph l i Eff t


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Pharmacologic Effects

Acetaminophen and AlcoholAlcohol stimulates oxidizing enzymes that

metabolize acetaminophen to its TOXICMETABOLITE

Normal maximum dose for people who DONOT drink = 325 per pill x2 = 650 mgevery 4 - 6 hours

For moderate drinkers (< 3 drinks a day),do not exceed 2gm of acetaminophen

For people who exceed 3 drinks a day orsomeone is an alcoholic AVOID

ACETAMINOPHEN


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DRUGS USED TO TREATGOUT URICOSURIC EFFECT


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GOUT

Inherited disease

Primarily in men

Involves one joint

Often big toe or knee Hyperuricemia and urate crystals are found at

joints (amount of uric acid)

Uric acid must be excreted because it cannot be

destroyed within the body Excess acid caused by excessive production

or reduced ability to excrete adequate amount ofuric acid


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GOUT

Colchicine

Treatment of an acute

case of gout

Taken hourly at theonset

Interferes with

inflammatory response

Side effects Vomiting

Diarrhea

Nausea

allopurinol (Zyloprim)

Inhibits synthesis of

uric acid

Prevent excess fromforming

Used with patients in

chemotherapy

Death of cells release

uric acid

D U d t T t G t


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Drugs Used to Treat Gout

Gout-inherited disease, mostly men,

involves 1 joint (big toe, knee, elbow) probenecid (Benemid) and allopurinol

used to prevent gout but have no pain

relief Due to an excess or uric acid (produce too

much or do not excrete enough)

Colchicine - on ly usedto tx attack of gout-taken hourly at the onset of attack

-most common side effect = GI


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Gout (cont)

allopurinol (Zyloprim)-

inhibits the synthesis

of uric acid

Also used to tx. pts

receiving chemo,

death of cells cause a

release of uric acid


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Gout (cont)

probenecid (Benemid)

increase excretion of

uric acid

GI effects, sore

gums,

Increases levels of

NSAIDs and penicillin

Natural remedy

believed by some are

natural cherries

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Chapter 5 Nonopioid Analgesics THIS ONE