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Analgesics
Dr. Wael M. Talaat
Objectives





Knowledge of different types of analgesics
How to manage the side effects of these
analgesics
How to write a prescription
Topics to be discussed





Acetaminophen
Salicylates
Nonsteroidal anti-inflammatory agents
Opiates
Acetaminophen
Background



Common in OTC
products (Tylenol,
Paracetamol)



Found in combination
with other products
Acetaminophen
Pharmacokinetics






Rapidly absorbed from GI tract
Peak concentrations w/in 1-2 hrs (tabs)
10% bound to plasma proteins
Half-life is 2-3 hrs


In overdose can be 12 hours
Acetaminophen
Metabolism

Acetaminophen
5%
urine

80-90%
Glucuronic Acid
or sulfate

Non Toxic
Acetaminophen

Clinical Presentation (Stages)


Stage 1 (0-24 hours)
Often no symptoms
 Nausea, vomiting, anorexia may occur

Acetaminophen

Clinical Presentation (Stages)


Stage 2 (24-48 hours)




bilirubin , PT prolonged

Stage 3 (3-4 days)
Coagulation defects, jaundice, renal failure, hepatic
complications may be present
 Death is usually due to hepatic failure

Acetaminophen

Clinical Presentation (Stages)


Stage 4 (Recovery)


Liver returns to
normal within 3
months
Acetaminophen

Rumack-Matthew Nomogram

Acetaminophen (mcg/ml)

1000

Probable
toxicity
100

10

Toxicity
unlikely
1
4

8

12

18

Hours from ingestion

24
Acetaminophen
N-acetylcysteine cont.



Administration Overview
It comes in 10% and 20% solutions
 Must be diluted to a 5% solution prior to
administration

Acetaminophen
N-acetylcysteine cont



Oral Administration
Load: 140mg/kg
 Maintenance: 70mg/kg Q 4 hours X 17 doses
 If pt vomits w/in 1 hour, repeat dose and consider
increasing dilution

Acetaminophen
N-acetylcysteine cont



IV administration (not FDA approved)
Dilute 1:5, administer over 1 hour through 0.22
micron filter
 Load: 140mg/kg
 Maintenance: 70mg/kg Q 4 hours X 11 doses

Acetaminophen
Management cont.



Supportive care






Vitamin K considered if PT> 1.5X control

For extended relief product, repeat level 6-8
hours after ingestion
Hemoperfusion or hemodialysis have no
conventional role
Salicylates


Sources


Acetylsalicylic acid
(Aspirin)




Methyl salicylate




regular, buffered,
enteric coated
oil of wintergreen

Bismuth
subsalicylate


PeptoBismol
Salicylates
Pharmacokinetics







Absorbed rapidly
Peak of 2-5 hours
Highly protein bound
Mainly metabolized by conjugation in liver
Renal excretion
Salicylates
Dosing



Toxic dose
< 150mg/kg
 150-300mg/kg
 300-500mg/kg
 >500mg/kg


no symptoms expected
mild to mod. symptoms
serious symptoms
potentially lethal
Salicylates

Mechanisms of toxicity



Stimulates the CNS respiratory center
Alters glucose metabolism
Salicylates

Clinical Presentation


Respiratory




Electrolytes




Tachypnea, pulmonary edema
Sodium, potassium, and bicarbonate excretion

CNS


coma, seizures
Salicylates

Clinical Presentation


GI




CV




Nausea, vomiting
Hypotension, tachycardia

Other


Fever, glucose abnormalities, PT prolongation,
tinnitus
Salicylates
Treatment





ABC’s
Hemodialysis
Replace electrolytes
Salicylates

Hemodialysis Indications







Coma
Seizures
Pulmonary edema
Acute level >100mg/dl
Refractory acidosis
Renal failure
Nonsteroidal Anti-inflammatory
Agents
NSAID’s

Pharmacokinetics






In general, rapidly absorbed
Highly protein bound
Time to peak between 1-4 hours
Half-lives vary from 1-86 hours
Undergo hepatic metabolism and are mainly
renally eliminated (some thru feces also)
NSAID’s
Toxic dose



Generally, significant symptoms occur after the
ingestion of more than 5-10 times the usual
therapeutic dose
NSAID’s

Clinical presentation


GI




CNS




Nausea, vomiting, abdominal pain
Drowsiness, headache, tinnitus, dizziness, coma and
seizures (severe ingestions)

CV


Hypotension (severe ingestions), tachycardia
NSAID’s

Clinical presentation


Renal




Hematologic




Acute renal failure
Aplastic anemia, prolonged PT

Acid-Base


Metabolic acidosis is seen rarely (usually due to
seizures)
NSAID’s

Clinical presentation


In piroxicam and massive ibuprofen
overdoses….seizures, coma, renal failure, and
cardiorespiratory arrest may occur
NSAID’s
Treatment



Supportive care
Antacids may be used for GI upset
 Fluids if dehydrated




Hemodialysis may be effective for ketoprofen
Opiate/Opiod Toxicity


Opiates




Naturally occurring compounds

Opiods


Refers to derivatives and synthetic analogs
Opiate/Opiod Toxicity
Agents








Codeine, morphine, hydromorphone,
hydrocodone, oxycodone, levorphanol,
oxymorphone
Meperidine, diphenoxylate, fentanyl, alfentanil,
sufentanil, remifentanil
Methadone, propoxyphene
Pentazocine, butorphanol, nalbuphine
Opiates

Pharmacokinetics





Usually peak within 2-3 hours
Half-lives vary
First pass effect when adminstered orally
Variable rates of elimination
Opiate Toxicity
Clinical Presentation



CNS




Respiratory




Seizures (meperidine, propoxyphene), coma,
pinpoint pupils
Respiratory depression, apnea

GI


Decreased gut motility
Opiate Withdrawal








Anxiety, sweating
Abdominal cramps
Nausea, vomiting,
diarrhea
Insomnia, restlessness
Tachycardia
Yawning
Opiate Toxicity
Treatment





ABC’s
Supportive care
Antagonists
Naloxone
 Nalmefene




No way to enhance elimination
Opiate Toxicity
Naloxone




Administered via IV, IM, SC
Dose





0.4-2mg IV, repeated Q 2-3 minutes up to 10mg trial

Duration is 30min-2hrs
Asymptomatic for 3-4 hours since last dose
prior to discharge
Opiate Toxicity
Naloxone



Continuous infusion
To prevent resedation
 2/3rds initial reversal dose per hour administered IV
 1/2 initial reversal dose given as a bolus when
infusion started

Opiate Toxicity
Nalmefene (Revex®)




Administered IV, IM, or SC
Dose
0.5mg IV followed by
 1.0mg IV 2-5 minutes later if needed
 Unlikely any response if none by 1.5mg





Duration is 3-10 hours
Asymptomatic for 8-12 hours after last dose
Prescription


A written order or authorization directing a
pharmacist to furnish certain drugs to a patient
Writing the Prescription


Five Parts
Superscription
 Inscription
 Subscription
 Signa (Sig.)
 Signature

Writing the Prescription


Superscription


The patients name, address and symbol Rx (“take
thou”)
Inscription



The body of the prescription
Contains the official names and quantities of
drug prescribed
Subscription



The directions to the pharmacist
Indicates dosage form and quantities to be
dispensed
Signa (sig)


The instruction to the patient for use of the
preparation
Signature





The prescriber’s signature and professional
degree
DEA number for controlled substances
Refills
Some sample scenarios


During your history taking, the patient informs
you that he has been taking aspirin daily for the
last 2 years. Upon clinical examination, you find
3 badly decayed teeth indicated for extraction.
How would you manage this case ??
Some sample scenarios


A diabetic patient needs to extract his tooth. The
patient informs you that he has recently had a
prosthetic valve. How will you prepare this
patient for extraction ??
Some sample scenarios


Upon prescribing a NSAID postoperatively
following surgical extraction, you noticed that
the patient was suffering from a peptic ulcer.
How are you going to manage this case ??

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7 antibiotic-dental7 antibiotic-dental
7 antibiotic-dentalIAU Dent
 
7.b. sedative hypnotics
7.b. sedative hypnotics 7.b. sedative hypnotics
7.b. sedative hypnotics IAU Dent
 
6. peptic ulcer drugs 323
6. peptic ulcer drugs 3236. peptic ulcer drugs 323
6. peptic ulcer drugs 323IAU Dent
 
6. anti drenergic
6. anti drenergic 6. anti drenergic
6. anti drenergic IAU Dent
 
6 beta lactum drugs dental
6  beta lactum drugs dental6  beta lactum drugs dental
6 beta lactum drugs dentalIAU Dent
 
4.anti colinergic
4.anti colinergic 4.anti colinergic
4.anti colinergic IAU Dent
 
5 aminoglycosides,macrolides, anti tb dental
5 aminoglycosides,macrolides, anti tb dental5 aminoglycosides,macrolides, anti tb dental
5 aminoglycosides,macrolides, anti tb dentalIAU Dent
 
5. opioid analgesics
5. opioid analgesics5. opioid analgesics
5. opioid analgesicsIAU Dent
 

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Maxillofacial injuries
Maxillofacial injuriesMaxillofacial injuries
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Impacted teeth
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7. Adrenocorticosteriods
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7.a. histamine & antihistaminics
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