Pharmacology WHAT ARE AUTACOIDS produced in one organ and are transported via the lymph system All occur made naturally in the body OCCUR NATURALLY IN THE BODY Terms amp Definitions Autacoids Examples ID: 215369
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Slide1
Dentalelle Tutoring
PharmacologySlide2
WHAT ARE AUTACOIDS?Slide3
produced
in one organ and are transported via the lymph system
All
occur (made) naturally in the body.
OCCUR NATURALLY IN THE BODYSlide4
Terms & Definitions
Autacoids - Examples:
Prostaglandins
– lipids that are synthesized locally by inflammatory stimuli –↑↑
PAIN receptors
Thromboxanes
(
a vasoconstrictor and a potent hypertensive agent, and facilitates platelet aggregation [clotting]).
Leukotrienes
(
I
nflammatory molecules;
precursor of prostaglandins
)
“-kinins”
- messengersSlide5
IS PAIN DIFFERENT FOR EVERYONE?Slide6
YESSlide7
Perception
Reaction
PAIN
The Psychological component:
The patient
’
s emotional response;
Differs from person to person;
Several factors will affect reaction
The Physical component of pain:
The Message that is carried from the
Injured tissue to the brain;
It is the ability to realize you are hurtSlide8
WHAT ARE PLACEBOS?Slide9
For some people, pain can also be effectively treated with inactive pills (placebos)
‘’FAKE’ DRUGSSlide10
WHAT ARE ANTIPYRETICS ALSO CALLED?Slide11
Non opioid
analgesics are also called:
nonnarcotic,
peripheral, mild, and Antipyretic (agents that reduce
fever)
Opioid analgesics are also called:
narcotic,
central, or
strong analgesics.
NON-OPIODSSlide12
Nonopioids
(
nonnarcotics
)
Act primarily at the:
peripheral nerve endings
Inhibit prostaglandin synthesis
(regulating the contraction and relaxation of smooth muscle tissue)
Not
effective for
severe
pain
3 subgroups:
Salicylates (aspirin-like group)NSAIDs Acetaminophen
2. Opioids
(
narcotics
)
Act primarily within the:
central nervous system
Depress
the central
nervous
system
Effective
for
severe
painExamples: Morphine, Codeine, Agents in cough suppressantsWe will discuss this area more in the next chapter
Difference is in their site of action
Classification of Analgesic Agents
Difference in their mode of actionSlide13
WHAT CATEGORY IS ASPIRIN UNDER?Slide14
ASPIRIN
is the most useful and common salicylate to reduce pain (analgesic action
)
acetyl salicylic acid (ASA) – THE CHEMICAL NAME FOR ASPIRIN
SALICYLATESSlide15
WHAT DOES
NSAIDS
STAND FOR AND WHAT DOES IT MEEAN?Slide16
NONSTEROIDAL ANTI-INFLAMMATORY DRUGSSlide17
Salicylates
Aspirin
belongs to a class of medications called nonsteroidal antiinflammatory drugs (
NSAIDs
).
Aspirin and other NSAIDs, for example, ibuprofen (eg. Motrin, Advil) and naproxen (eg. Aleve), are widely used to treat fever (
antipyretic action
), pain (
analgesic action
), and inflammatory (
anti-inflammatory action
) conditions such as arthritisAspirin is also known for its anti-platelet actionSlide18
ASA
Aspirin
have:
a
nti-inflammatory
,
antipyretic
,
analgesic
,
and
antiplatelet actions.These actions are related to the ability to inhibit prostaglandin synthesis
Salicylates:
MECHANISM OF ACTION
Whereas,
Acetaminophen
drugs have only
antipyretic
&
analgesic
actions
. Slide19
ASA
Aspirin inhibits cyclo-oxy-genase (COX) to block production of prostaglandins
Prostaglandins can sensitize pain receptors to substances such as BRADY
KININ
(SEE NOTE)
A reduction in prostaglandins results in a reduction in pain
Salicylates:
MECHANISM OF ACTIONSlide20
HOW LONG BEFORE ASPIRINS PEAK EFFECT?Slide21
REMEMBER NOT TO APPLY TOPICALLY TO ORAL MUCOSA!!!!
30 MINUTESSlide22
ASPIRIN’S EFFECTS BY DOSE
LOW
HIGHSlide23
ASA
Reye
’
s Syndrome
Associated with use of aspirin in children & adolescents who took it when they had the chickenpox or influenza
Fatal disease that causes numerous detrimental effects to many organs, especially the brain and liver.
ACETAMINOPHEN
and
NSAIDs
are now used for fever (
antipyretic action)
or pain (
analgesic action) in pediatric and adolescents to reduce the chances of Reye’s Syndrome
Salicylates:
ADVERSE REACTIONSSlide24
WHAT DRUG SHOULD YOU NOT TAKE WITH ASPIRIN?Slide25
A drug interaction between aspirin and Warfarin can result in significant bleeding
WARFARINSlide26
NSAIDs
A rapidly growing group with important application in dentistry
Mechanism of action
and many of their
pharmacologic effects
and
adverse reactions
resemble aspirin
Many
authors agree that the NSAIDs are the
most useful
drug group for the treatment of dental pain
.Most are available without a prescription.Slide27
WHEN IS THE PEAK PERIOD FOR MOST NSAIDS?Slide28
1-2 hoursSlide29
NSAIDs
Most NSAIDs peak in about 1-2 hours
Well absorbed orally and food reduces the rate but
not
the extent of absorption
Metabolized in liver, excreted in kidneys
PHARMACOKINETICSSlide30
NSAIDs
have a significant
anti-inflammatory
effect
Similar as aspirin:
analgesic
antipyretic
anti-inflammatory
They
inhibit prostaglandin synthesis
PHARMACOLOGIC EFFECTSSlide31
ARE NSAIDS ADDICTING?Slide32
NSAIDs are not addicting, tolerance does NOT develop, and
no withdrawal syndrome can be induced
.
NO!Slide33
NSAIDs
7
. Pregnancy and Nursing
Contraindicated
in pregnancy;
Like aspirin, NSAIDs given late in pregnancy can prolong gestation
IBUPROFEN
is drug of choice for nursing
ADVERSE REACTIONSSlide34
DENTAL PAIN IS BEST MANAGED BY HOW MUCH MG OF IBUPROFEN?Slide35
In usual prescription doses, NSAIDs can be shown to be statistically significantly better than codeine alone, aspirin, acetaminophen, or placebo.
400MGSlide36
NSAIDs
NSAIDs should be used with
caution
in patients with:
asthma
cardiovascular disease
Renal diseases with fluid retention
coagulation problems
peptic ulcer disease
ulcerative colitis
CONTRAINDICATIONS & CAUTIONS
Contraindicated in pregnancySlide37
WHAT IS THE MOST COMMONLY USED NSAID?Slide38
IBUPROFENSlide39
WHAT HAS
NO
ANTI-INFLAMMATORY EFFECT?Slide40
ACETAMINOPHENSlide41
Acetaminophen
Used as an
analgesic
and
antipyretic
in children and adults when aspirin is contraindicated
Has no anti-inflammatory action Slide42
Acetaminophen
Rapidly
and
completely
absorbed from the GI tract
Peak plasma level in 1 – 3 hours
Half life of 1 to 4 hours
Metabolized by the liver
Excreted by the kidneys in 24 hours
When
large
doses
are ingested, an intermediate metabolite is produced that is thought to be
hepatotoxic and possibly nephrotoxic..
PHARMACOKINETICSSlide43
AN ACUTE OVERDOSE OF ACETAMINOPHEN CAN CAUSE WHAT?Slide44
LIVER DAMAGESlide45
Acetaminophen
Acetaminophen is used as an:
A
nalgesic agent (
↓
pain)
Antipyretic agent (
↓
fever)
USESSlide46
Acetaminophen
Used when
hypersensitivity to aspirin
or for patients experiencing
aspirin-gastric induced irritation.
Used as an
antipyretic instead of aspirin for young children
;
due to aspirin
’
s association with Reye
’
s syndrome.Can be used in all stages of pregnancy (always ask doctor)
USESSlide47
WHAT DRUGS ARE USED TO TREAT GOUT?Slide48
Allopurinol AND ProbenecidSlide49
Drugs Used to Treat Gout
Allopurinol (Zyloprim)
used in
PREVENTION
of a gout attack.
Inhibits the synthesis of uric acid
Also used in patients receiving either chemotherapy or irradiation
If a pruritic rash should occur, the drug should be promptly discontinued
Probenecid (Benemid)
used in
PREVENTION
of a gout attack.
Is an uricosuric drug that increases uric acid excretion in the urineSlide50
CHAPTER 6Slide51
WHAT ARE OPIODS USED TO TREAT?Slide52
At first referred to drugs that are derivatives of
opium
poppy
Opioid or narcotic analgesics are used to manage dental pain in patients in whom NSAIDs are contraindicated
MODERATE TO SEVERE PAINSlide53
Mechanism
of action at the receptor site
:
53
CLASSIFICATION
-THREE GROUPS-
GROUP
SUBGROUP
EXAMPLE
OPIOID
AGONISTS
morphine, codeine
MIXED OPIOIDS
AGONIST-ANTAGONISTSPARTIAL AGONISTpentazocinebuprenorphineANTAGONISTSNaloxoneSlide54
54
CLASSIFICATION:
CHEMICAL STRUCTURE
BOX 6-1 OPIOD ANALGESIC AGENTS BY STRUCTURE GROUP
MORPHINE AND CODEINE
(Largest Group)
hydromorphone
(Dilaudid)
agonist
hydrocodone
(in Vicodin) agonist
dihydrocodeine (in Synalgos-DC)oxycodone (in Percodan, Percocet, Tylox) agonistMETHADONEmethadone (Dolophine) agonist
propoxyphene (Darvon) agonistMORPHINAN
butorphanol (Stadol)
agonist-antagonist
pentazocine (in Talwin-NX) agonist-antagonist
MEPERIDINE
meperidine
(Demerol)
agonist
fentanyl
(Sublimaze)
agonist
diphenoxylate
(in Lomotil)
OTHER
buprenorphine (Buprenex, Subutex) partial agonistDo not give any of these drugs if the patient has an allergy to morphine or codeineSlide55
WHAT ARE WEAKER FORMS OF OPIODS?Slide56
Codeine (in Tylenol#3) and Hydrocodone (in Vicodin) are some of the weakestSlide57
57
DRUG NAME (SOME EXAMPLES)
COMMENTS
SCHEDULE FOR CONTROLLED SUBSTANCE
STRONGEST
MORPHINE
Standard agent; prototype
II
MERPERIDENE
(Demerol)
Abused by professionals
IIINTERMEDIATE
OXYCODONE (in Percocet)Popular with addicts ‘shopping’ for opioidsIIWEAKEST
HYDROCODONE (in Vicodin)
IIICODEINE
(in Tylenol#3)#2=15mg; #3-30mg; #4=60mg
IIISlide58
WHERE DO NONOPIODS ACT?Slide59
Opioids bind to receptors in both the central nervous system (CNS) and the spinal cord, producing an altered perception of reaction to pain
PERIPHERAL NERVE ENDINGSSlide60
WHAT ARE NATURAL OPIODS?Slide61
Natural opioids (also called endogenous opioids), include:
Enkephalins
Endorphins
Dynorphins
These
are the chemicals that make sure we can function during accidents, like after breaking our leg…
RELIEVE PAIN AND RELAXATIONSlide62
Enkephalins
Endorphins
Dynorphins
All 3 have opioid-like action and are found in the body.
They are naturally occurring peptides that possess analgesic
action and addiction potential
62
The Discovery of 3 Groups of Endogenous Substances
Probably function as
neurotransmitters
, although their exact function has
not
been elucidated.
reduces pain & positively affects mood.
stimulates delta(
)
receptor
stimulates the kappa (
)
-receptor
MECHANISM OF ACTIONSlide63
WHEN DO OPIODS START WORKING?Slide64
The dosing intervals of most opioids are between 4-6 hours; the usual dose depends on the
drug.
Duration
– necessitates dosing every 4-6 hours
WITHIN 1 HOURSlide65
WHAT IS THE FIRST PASS EFFECT?Slide66
Undergoes first pass metabolism in the liver and intestine, reducing its bioavailability.
REDUCES THE BIOAVAILABILITYSlide67
D
istribution:
Oral bioavailability of opioids is
primarily
limited
by
first pass metabolism.
Undergoes
first pass metabolism in the liver and intestine, reducing its
bioavailability.
Degree
of first pass differs among
individuals.May
cause respiratory depression in fetus when mother is given opioids near term.67PHARMACOKINETICSSlide68
E
xcretion:
Most
opioids are excreted through the kidneys, but this action does
not
selectively affect their availability after oral administration
.
Metabolized
opioids and the unchanged drug are excreted in the urine.
68
A.
D.
M.
EPHARMACOKINETICSSlide69
True or false?
severity
of side effects is proportional to the efficacy (strength
)?Slide70
A pharmacologic effect may also be an adverse reaction, depending on the clinical use of the agent.
TRUESlide71
IS MORPHINE THE STRONGEST OR WEAKEST OPIOD?Slide72
Morphine is the opioid agonist by which all others are measured
.
Strongest can relieve severe pain while weaker agents mixed with
non-opioids
are equivalent to NSAIDs.
THE STRONGESTSlide73
Aspirin
(ASA)
and
ibuprofen
(NSAID)
are
analgesic
, antipyretic, and antiinflammatory
, and they inhibit platelet aggregation
.
Acetaminophen is analgesic
and antipyretic. Codeine is analgesic.73
AnalgesiaPHARMACOLOGIC EFFECTSWhat do aspirin, acetaminophen, ibuprofen, and codeine have in common?Slide74
WHAT IS AN ANTITUSSIVE?Slide75
dextromethorphan
SUPRESSES A COUGHSlide76
Opioid
analgesics ↑
smooth muscle tone and ↓
propulsive contractions and
motility
(some opioids have constipation as a side effect).
Useful
for treating diarrhea
.
Example: diphenoxylate (in Lomotil)
76
Gastrointestinal EffectsOpioids are not used for depression, infections, or hypertension
PHARMACOLOGIC EFFECTSSlide77
Combining an opioid with a nonopioid analgesic produces an additive analgesic effect with fewer adverse reactions.
77
ADVERSE
REACTIONS
TRUE
or
FALSE
TRUE
These agents work at two different levels on pain and produce an additive analgesic effect. In combination products, lower doses of each analgesic may be used, and a
potential
exists for a reduction in adverse reactions.Slide78
DO OPIODS INCREASE OR DEPRESS THE RESPIRATORY CENTRE?Slide79
The rate and depth of breathing are reduced
.
The depression is related to a decrease in the sensitivity of the brainstem to carbon dioxide.
DEPRESS
THE RESPIRATORY CENTER IN A
DOSE RELATED
MANNERSlide80
80
Respiratory Depression (RP)
Not
a problem with usual doses in normal
patients
RP is usually
the cause of death with an
overdose
ADVERSE REACTIONSSlide81
81
Nausea
and Emesis
Analgesic doses of opioids often produce
nausea and
vomiting.
Result
of their direct stimulation of the chemoreceptor trigger zone
(CTZ) located
in the
medulla.
Repeated administration of regular doses can prevent
vomiting at the vomiting center (VC).
ADVERSE REACTIONSSlide82
WHAT IS A VERY COMMON SIDE EFFECT OF OPIOD USE?Slide83
Their duration outlasts their analgesic effect
CONSTIPATIONSlide84
WHAT IS A SIGN IN RECOGNIZING AN OPIOD ADDICT?Slide85
MIOSIS – ‘PINPOINT PUPILS’. RESPIRATORY DEPRESSIONSlide86
HOW DO YOU TREAT AN OVERDOSE TO OPIODS?Slide87
an antagonist such as naloxone (in
Narcan
)
AN ANTAGONISTSlide88
88
Biliary
Tract Constriction
Opioids
may constrict the biliary duct, causing
biliary colic
(bile duct obstruction leading to gall
stones).
ADVERSE REACTIONS
Importance in patients passing gallstones who are being treated with opioids.Slide89
A MOTHER ON OPIODS – WHAT CAN HAPPEN TO THE BABY?Slide90
Not teratogenic, but may prolong labor or depress fetal respiration if given near term.
.
Not usually a problem with mother’s milk with therapeutic doses.
THE INFANT MAY HAVE DEPRESSED RESPIRATION AND WITHDRAWL SYMPTOMSSlide91
Use of opioids is
NOT
contraindicated in hypertensive
patients.Slide92
92
ADVERSE
REACTIONS
Addiction
The degree of addiction
potential
is proportional to analgesic
strength.
An addict will develop
tolerance
to the effects of opioids,
EXCEPT
for miosis and constipation.Slide93
93
Addiction
Since the duration of use in dentistry is usually short – addiction for dentistry does not pose a problem
NSAIDs should be used to control dental pain in the addict.
AN ADVANTAGE OF NSAIDs OVER OPIOIDS:
NSAIDs are not addictive, tolerance does not develop, and no withdrawal syndrome can be induced.
ADVERSE REACTIONSSlide94
IF A CLIENT CLAIMS ALLERGIES TO NSAIDS, WHAT COULD THIS MEAN?Slide95
TERMED ‘SHOPPERS’ THE CLIENT IS LOOKING FOR A SPECIFIC OPIOD.
KEEP IN MIND – THIS ISNT ALWAYS THE CASE…LOOK FOR OTHER SIGNS NOT JUST ONE
OPIOD ADDICTSlide96
96
Addiction:
Identification
of an Addict
The “shoppers” - What to look for:
Asks
for the opioid analgesic by name and says that this is the only drug that works for
them.
Claims
allergies to NSAIDs
.
Cancels
dental appointment but still requests the opioid analgesic even though they will be
“out of town on business”.Experiences pain for days after scaling and root planingMoves from office to office because “others don’
t understand”.
Claims a “
low pain threshold”.
Needs refills several days after a procedure without
complications.
Calls
with a request for an opioid analgesic just as the office is closing or after
hours.
ADVERSE REACTIONSSlide97
WHAT IS METHADONE?Slide98
Maintaining
patients on high doses of methadone (methadone maintenance
).
USED TO TREAT OPIOD ADDICTION AND WITHDRAWLSlide99
99
Addiction: 4 Treatment Options
Addiction, overdose, and withdrawal can be treated with opioid antagonists
Substituting
addict with oral opioid
(
methadone
).
Going cold turkey
and using medication such as phenothiazines, clonidine or benzodiazepines (to alleviate symptoms of withdrawal
).
Maintaining patients on high doses of methadone (methadone maintenance
).Administering an orally effective, long-acting antagonist Naltrexone (Trexan).
ADVERSE REACTIONSSlide100
100
Addiction: Treatment Options
Example: The Heroin Addict
T
he
following drugs can be used to treat heroin
addiction
ADVERSE REACTIONS
METHADONE
, is used by substituting methadone for heroin and then tapering off or maintaining the addict on oral methadone.
NALTREXONE
,
a long-acting opioid antagonist, is used to block the action of usual doses of opioid administered illegallySlide101
IS TRUE OPIOD ALLERGY COMMON?Slide102
Most common types of true allergic reactions to opioids is
dermatologic
in nature
.Due to the histamine-releasing properties of opioid analgesics.
Includes skin rashes and urticaria.
GI side effects are often reported.
NOSlide103
103
A patient with a true allergy to codeine should
NOT
be given an analgesic in that group
This includes:
oxycodone
hydromorphone,
hydrocodone, and
dihydrocodone
Because they are all members of the same
morphine and codeine group
.Slide104Slide105
WHAT IS THE PROTOTYPE OPIOD AGONIST WHICH OTHER OPIODS ARE MEASURED?Slide106
MORPHINESlide107
The
prototype opioid agonist which other opioids are
measured
107
Agonists:
Morphine
SPECIFIC OPIODS
Parenterally:
used
to control postoperative
pain
Orally:
used primarily
in the treatment of cancerSlide108
U
sed
alone or combined with aspirin (in Percodan) or acetaminophen (in Percocet, Tylox
) with fewer adverse reactions.
For moderate
to severe
pain.
It is located in the middle of the chart for strength value.
108
Agonists:
Oxycodone
SPECIFIC OPIODSSlide109
Weak opioid analgesic with fewer adverse
reactions.
Less potential for
abuse.
Combination of Hydrocodone (5mg) with acetaminophen (500mg)
is recommended for the majority of dental patients with
pain
109
Agonists:
Hydrocodone
SPECIFIC OPIODS
In Vicodin, it has been reported as being safe to use when breastfeedingSlide110
WHAT IS THE MOST COMMON OPIOD IN DENTISTRY?Slide111
Most commonly used opioid in dentistry and is
often combined with acetaminophen (Tylenol #3) for oral administration
CODEINESlide112
Favorite
drug of abuse for medical personnel;
100mg
meperidine
=10mg
morphine.
For
acute
management of moderate to severe pain.
Poor
choice for oral use
because it has a high first pass effect; short duration of
action.Less constipating, and without miosis or cough suppression.EXAMPLE: meperidine HCl (Demerol)
112Agonists: Meperidine
SPECIFIC OPIODSSlide113
WHAT IS HYDROMORPHINE USED FOR?Slide114
MANAGEMENT OF SEVERE PAIN, MORE POTENT THEN MORPHINESlide115
An
orally effective opioid,
reserved for management of severe
pain.
More
potent than
morphine
Similar
adverse reactions to
morphine.
Favourite of the addicts because of its high strength;
requires careful
monitoring.EXAMPLE: Dilaudid115
Agonists: HydromorphoneSPECIFIC OPIODSSlide116
116
Agonists:
Methadone
SPECIFIC OPIODS
Methadone is used either to withdraw the patient gradually or for methadone maintenance. Because it has a longer duration of action, withdrawal from methadone is easier than from heroin. Because it is an opioid analgesic, however, the risk for dependence still exists.
Used
primarily
to treat any opioid addicts
(eg. Heroin addicts)
Similar to morphine.
Slower onset and longer duration of action.
EXAMPLE:
DolophineSlide117
117
Antagonists
SPECIFIC OPIODS
Naloxone
will
block the therapeutic and toxic actions of
opioids
Methadone is an opioid used in treatment of addiction, but will exacerbate symptoms of an opioid overdose.
An pure
opioid antagonist that is active
parenterally
.
Drug of choice
for treating agonist or mixed opioid overdoses.naloxone
(Narcan)Slide118
WHAT IS TRAMADOL?Slide119
An orally administered
non-opioid
with weak analgesic
activity(ULTRAM) Slide120
Few
studies have confirmed its
efficacy:
Binds with
mu (
μ
)
opioid
receptors;
inhibits reuptake of serotonin and norepinephrine, and modifies ascending pain pathways.
Its
analgesic efficacy is equivalent to that of codeine.Side effects can include: miosis and CNS effects, such as dizziness, headache and stimulation and GI tract effects include nausea, diarrhea, constipation and vomiting.Is moving up the top 200 most prescribed drugs.
120SPECIFIC OPIODSTramadol (Ultram)Slide121
Most dental pain can be managed with
NSAIDs.
If
NSAIDs are
contraindicated -
the DDS has a wide variety of opioids to choose from.
Eg
. Beginning with
codeine
or
hydrocodone
combinations, and progressing to
oxycodone combinations.Only in rare cases and for short periods of time (approx. 1-2 days) should stronger opioids be prescribed for outpatient dental pain.121DENTAL USE OF OPIODSSlide122
ARE OPIODS USED FOR CHRONIC OR ACUTE PAIN?Slide123
ACUTE IS PREFERRED* BUT CAN BE USED FOR CHRONIC PAINSlide124
Opioids are considered first-line therapy for:
Pain associated with procedures (bone marrow biopsy)
Pain due to trauma or cancer (burns)
Visceral pain (appendicitis)
Majority used to relieve
acute
or
chronic
pain.
Few, such as fentanyl (Sublimaze, Duragesic), alfentanil (Alfenta), and sufentanil (Sufenta), are primarily indicated for
preoperative sedation
to reduce patient apprehension.
Also used to suppress cough and treat diarrhea124REVIEW: USE
OF OPIODSSlide125
#1. Hydrocodone
#32. Tramadol
#105. Oxycodone
#133. OxyContin
#156. Fentanyl transdermal
#175. Methadone HCl noninjectable
125
Some of the Opioids found in the TOP 200