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Ocular Pharm > Wk 12 - Analgesic Intro / NSAIDs > Flashcards

Wk 12 - Analgesic Intro / NSAIDs Flashcards

1
Q

Local anesthetic agents

A
  • Proparacaine
  • Lidocaine
  • Benoxinate
  • Lidocaine/Prilocaine (EMLA)
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2
Q

EMLA cream / patch

A

Lidocraine / prilocaine mixture
Uses:
-Pre-­‐op for removing skin lesions
-Post-­‐herpetic neuralgia

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3
Q

Local anesthetic MOA

A

Sodium channel blockers

-Block Na channels on nociceptor axons to block the transmission of the pain signal

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4
Q

Local anesthetic Adverse Effects

A

Long term use slows wound healing and can degrade the cornea, so we never Rx these
-Use in-office only

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5
Q

Peripherally Acting Analgesics

A
  • NSAIDs

- Aspirin

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6
Q

NSAID & Aspirin MOA

A

COX inhibitors
-Inhibit the enzyme cyclooxygenase to prevent the production of prostaglandins from arachidonic acid
Prostaglandins sensitize nociceptors, so preventing their production helps to prevent pain signal
-NO EFFECT on leukotriene production
-DO NOT prevent the formation of subepithelial infiltrates in the cornea since white blood cell migration is controlled by leukotrienes
- comparison: Remember that steroids inhibit phospholipase to prevent the production of arachidonic acid, prostaglandins, and leukotrienes

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7
Q

Centrally Acting Analgesics

A
  • Opiods

- Acetaminophen

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8
Q

Opiod & Acetaminophen MOA

A

Block pain signal to the brain (opioid mu agonists, SNRIs, etc.)

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9
Q

Clinical uses of Topical NSAIDs

A
  • Anterior segment
    GOOD:
    o Pain control
    • Abrasions, peri-operative (esp cataract surgery), betadine treatment for EKC
    • Topicals are better than oral NSAIDs for A-Seg pain
    POOR:
    o Anti-inflammatory effects are poorer than oral NSAIDs or topical steroids
    o Limited value in treatment of allergy

-Posterior segment
o Treatment of cystoid macular edema
• Caused by inflammation in the retina
• Topical NSAIDs penetrate to the retina well to inhibit prostaglandin synthesis

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10
Q

Adverse effects of Topical NSAIDs

A

1) May allow formation of subepithelial infiltrates after corneal surgery
2) May delay wound healing
o Not as much as steroids
o Reported more with long term use
3) Corneal melt syndrome
o May cause extreme corneal damage
o More likely in unhealthy eyes and with overdosing
o Generic diclofenac is most likely drug to cause CMS
o Watch patients carefully and stick to FDA recommended dosing
4) Burning, stinging, SPK, and conjunctival hyperemia
o More common with the classic/older NSAIDs
5) Contraindicated in soft CL wearers
o Corneal toxicity and decreased immunity can leave patient more susceptible to bacterial infections

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11
Q

Diclofenac 0.1% (Voltaren)

A

Topical NSAID

•Older formulation, rarely used today

Indications:

  • Post-op inflammation after cataract extraction
  • Pain and photophobia in patients undergoing corneal refractive surgery

Dosing: 1 gt qid

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12
Q

Ketorolac 0.5% (Acular)

A

Topical NSAID

-Ketorolac is an older NSAID, used occasionally today.

Indications:
• Ocular itching due to SAC
• Post-op inflammation after cataract extraction

Dosing: 1 gt qid

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13
Q

Ketorolac 0.4% (Acular LS)

A

Topical NSAID

Slightly lower concentration reduces stinging

Indication: reduction of pain following refractive surgery

Dosing: 1 gt qid

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14
Q

Ketorolac 0.45% (Acuvail)

A

Topical NSAID

Preservative free

Indication: treatment of pain and inflammation after cataract extraction

Dosing: 1 gt bid

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15
Q

Bromfenac 0.7% (Prolensa)

A

Topical NSAID

Newer formulation used commonly.
Comfortable and well tolerated.
Earlier 0.9% formulations (Xibrom and Bromday) have been discontinued.

Indication: Treatment of post-op inflammation and reduction of ocular pain in patients who have undergone cataract surgery

Dosage: 1 gt qday
= 1 gt the day before surgery, 1 gt the day of survery, and 1 gt qday for 14 days after surgery

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16
Q

Nepafenac 0.1% suspension (Nevanac)

A

Nepafenac is a newer formulation used commonly.

  • Comfortable and well tolerated.
  • Minimized potential for toxicity
  • Pentrates vitreous much better than older NSAIDs like ketorolac

Indication: treatment of pain and inflammation after cataract surgery

Major Off-label use:
Prevention of cystoid macular edema

Dosing: 1 gt tid

17
Q

Nepafenac 0.4% suspension (Ilevro)

A

Nepafenac is a newer formulation used commonly.

  • Comfortable and well tolerated.
  • Minimized potential for toxicity
  • Pentrates vitreous much better than older NSAIDs like ketorolac

•Similar performance compared to Nevanac
Indication: post-op cataract surgery

Major Off-label use:
prophylactic for CME

Dosing: 1 gt qday

18
Q

General info on Topical NSAIDs

A

-Diclofenac is FDA Category D ; All the rest are Category C

Dosing:
Diclo and Ketoro (older) = QID
Brom and Ilevro (newer) = Qday
Nevanac (low concentration) = TID

Minimum Age:
Ketoro = 3
Nepa = 10
Brom = 18

19
Q

Oral NSAIDs MOA

A

Inhibit COX-1 and -2 enzymes to prevent the production of prostaglandins, which sensitize nociceptors

Notes:
1) Ceiling effect
o Beyond a certain dose there is no further analgesic effect
o No ceiling effect in opioids

2) No risk of tolerance or addiction with repeated or chronic use.
o Not the case with opioids

3) Patients vary in response to different NSAIDs.
o If max dose is not effective, switch to an alternate

20
Q

Oral NSAID Side Effects and Possible Complications

A

1) Renal and liver excretion
o Use caution in patients with history of renal or liver problems, diabetes, or significant use of diuretics
2) Highly protein bound
o Can cause interactions by displacing other drugs from plasma proteins
3) GI upset, ulcers, etc.
o COX-2 is involved in production of prostaglandins that cause pain
o COX-1 produces prostaglandins that have a protective function in the stomach
o Most NSAIDs are COX nonspecific, so they inhibit the production of good prostaglandins in the stomach
4) Bleeding disorders
o Effects on platelets causes blood thinning
o Can worsen bleeding/clotting disorders
o Increased risk of re-bleed in problems like hyphema and vitreous heme
5) CAUTION IN:
o Asthma, aspirin hypersensitivity, after invasive surgery, 3rd trimester pregnancy

21
Q

Aspirin

A

Oral NSAID

Prototype NSAID
o Analgesic, anti-inflammatory, anti-pyretic, and anti-platelet effects

Clinical uses
o Corneal abrasion
o Conjunctival discomfort from viral infection
o Can be combined with Tylenol, codeine, or other narcotics for an additive pain relieving effect

Toxic reaction
o Tinnitus – ringing in the ears

Formulations
o Buffered aspirin has increased dissolution rate
o Enteric coating can reduce GI problems
o **Avoid either of these in acute pain

Contraindication:
children under 18
o Can cause Reyes syndrome

22
Q

Dosing for Aspirin

A

Anti-inflammatory dosing
o 3-4 grams/day or 8-16 OTC tabs/day

Adult dose for ocular pain
o Two 325 mg or one 650 mg tab q4h
o Do not exceed 4 gm/day

23
Q

Ibuprofen (Motrin, Advil, Nuprin, Medipren)

A

Oral NSAID
non-selective COX inhibitor

More effective analgesic than aspirin. 
Half-life is 2 hours. 
Peak levels reached in 1-2 hours.  
Formulations
o	200 mg tabs OTC
o	300-800 mg tabs Rx

Dosing
Adult analgesic dose = 400 mg q4h
2400 mg is anti-inflammatory level
3200 mg is max daily dose

24
Q

Naproxen (Anaprox, Naprosyn, Aleve)

A

Oral NSAID
non-selective COX inhibitor

May be the safest NSAID
For relief of mild to moderate pain

Adult Rx dose
- 550 mg initially followed by 275 mg q6-8h
OTC dose
- 220 mg q8-12h

25
Q

Ketoprofen (Orudis, Oruvail)

A

Oral NSAID
• 2 hour half life
• 50 mg q4h may be as effective as Tylenol+Codeine for analgesia

Adult dose
o Orudis: 50 or 75 mg q6-8h
o Oruvail: 200 mg q?h (Sustained release, Rx only)

26
Q

Ketorolac

A

Oral NSAID
Very potent with a much higher risk of side effects.
Used short term only – 5 day max

Dosing: 10 mg q4-6h, max 40 mg/day

27
Q

Indomethacin

A

Oral NSAID
Very cheap
Dosing: 25-50 mg bid-tid

28
Q

Meloxicam (Mobic)

A

Oral NSAID
• We don’t Rx this much, but common to see patients taking it in clinic
• Easier on stomach

Dosing: 7.5-15 mg qd

29
Q

Celecoxib (Celebrex)

A

Oral NSAID
MOA: COX-2 selective inhibitor
o Fewer gastric side effects

Adverse effects:
Increased risk of heart attack and stroke

Dosing: 100 or 200 mg qday-bid

30
Q

Acetaminophen (Tylenol)

A

MOA: Centrally acting COX inhibitor
o Exact MOA not fully understood
o Analgesic and antipyretic
o NOT anti-inflammatory or anti-platelet

Use:
For mild-moderate pain
o Often combined with narcotic analgesics

Adverse Effects:
o Risk of liver, renal tubule, and myocardium toxicity
• Contraindicated with liver impairment
• Acetaminophen OD is #1 cause of liver failure
o Limit of 325 mg added to narcotic agents or other meds to prevent overdose
o Known for its safety, except in the case of overdose

Comparison to aspirin:
o Less GI upset
o Greater safety during breastfeeding
o Does not affect platelet clotting factors (No bleeding risk)

31
Q

Dosing for Acetaminophen (Tylenol)

A

Adult dose: 325-1000 mg q4h

Max = 4000 mg/day

32
Q

Synergistic Analgesic Combinations and Adjuvants

A

Alternate central acting acetaminophen + peripheral acting ibuprofen
o Analgesic effect approximates Tylenol #3 (Tylenol+Codeine) in dental and post-op pain studies
o 650-1000 mg acetaminophen q4h and 400 mg ibuprofen q4h
• Ex. acetaminophen at noon, ibuprofen at 2 pm, acetaminophen at 4 pm, ibupofen at 6 pm

Adujvants
o Added substances like caffeine can enhance the effect of NSAIDs or narcotic agents

33
Q

NSAID Safety Overview

A

-Aspirin, Ibuprofen, Meloxicam are all FDA Category D ; Celebrex is C early / D late ; All the rest are Category C.

Minimum Age:
Ibuprofen = 2 mos
Naprox, Melox, Indometh, Aceta = 2 yr
Ketoro = 17 yr
Aspirin, Ketopro = 18 yr
Max Dose Per Day
Meloxicam has lowest at 15 mg. 
Ketorolac is just behind at 40 mg.  
Indomethacin next at 150-200 mg.
Ketoprofen at 300 mg. 
Celebrex at 400 mg. 
Naproxen at 1000 mg. 
Ibuprofen at 3200 mg. 
Aspirin and Acetaminophen are highest at 4000 mg.
34
Q

Points To Remember

A

Ocular pain is usually acute and short lived, best treated with an opioid + NSAID, aspirin, or acetaminophen

Schedule III is usually a safe bet and can be Rx’d by ODs in most states

Avoid combining aspirin and codeine with barbiturates
o Watch out for polypharmacy!

Children
o	Note dosage recommendations, stick to FDA guidelines, and consult with patient’s pediatrician
o	Avoid aspirin combinations – Reye’s syndrome
o	Good choices
•	Acetaminophen 10-15 mg/kg q4h
•	Ibuprofen 4-10 mg/kg q6h
•	Naproxen 5-7 mg/kg q8h
•	Codeine 0.5-1 mg/kg q4-6h

Elderly patients
o Usually have poorer renal/liver clearance
o Increased risk of side effects
• Sedation, constipation, CNS effects
o More likely to be on multiple drugs
• Interactions, polypharmacy
• Opioid allergies are rare
o If present, use tramadol or an NSAID as an alternative
• Use precautions when writing an Rx to avoid tampering

Remember that just because a pain med contains an opioid, it isn’t necessarily the best pain killer
• Ibuprofen 400 mg was shown in this study to give better ocular pain relief than Tylenol #4

Ocular Pharm (10 decks)

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