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Oral Meds:  Analgesics


There are occasionally clinical settings where cycloplegia and diclofenac (Voltaren) aren’t sufficient to keep the patient tolerably comfortable. The factors of patient pain threshold and the severity of the disease often dictate the need for adjunctive orally administered pain relief.

Although not commonly needed, oral analgesics can be essential for the successful management of certain clinical conditions. The single best resource we have found on this subject is, “Drugs For Pain,” The Medical Letter, Vol. 42 (Issue 1085), August 2000. (The Medical Letter Web site is www.medletter.com, and their telephone number is 1-800-211-2769.) This is the closest thing we know of to a Consumer Reports on drugs that covers the spectrum of medical therapeutics.

There are three main categories of analgesics:
1. Over-the-counter (OTC)
2. Non-narcotic prescription
3. Narcotic prescription

Although there are dozens and dozens of such drugs, we are going to make it simple by highlighting our favorite drugs in this class.

• Acetyl para aminophenol (APAP, acetaminophen or Tylenol)
• Acetylsalicylic acid (ASA or aspirin)
• Ibuprofen (Motrin, Nuprin, Advil and generics)

Acetaminophen is the clear leader in OTC pain control. (As an aside, aspirin in low dose—81mg qd—plays a huge role in anti-platelet aggregation in stroke and heart disease management.) Acetaminophen is not platelet-active, nor is it an anti-inflammatory. APAP has two arms; one is analgesic, the other is anti-pyretic.

ASA has the triple effect of reducing pain, inflammation and fever. However, the risk of GI bleeding largely precludes its long-term use at dosages sufficient to render a clinically significant anti-inflammatory effect. Additionally, the FDA warning on ASA states: “Children and teenagers should not use salicylates for chicken pox or flu symptoms before a doctor is consulted about Reye’s syndrome, a rare but serious side effect.” Additionally, APAP is rated pregnancy category B, whereas ASA is category D.

Most people we encounter use APAP as their pain reliever of choice, and we simply advise them to use whatever works for them if there is a need for oral analgesia. The usual dosage of APAP is 325-650mg every 4-6 hours prn.

Ibuprofen enjoys popularity akin to acetaminophen. It comes in 200mg brown tablets. The usual dose is two 200mg tablets qid. From The Medical Letter: “Ibuprofen in doses no higher than 1600mg/day may be less likely to cause serious gastrointestinal toxicity than aspirin or other non-selective NSAIDs.”

It is interesting to note that ibuprofen, at 400mg qid, is comparable to acetaminophen/codeine combination drugs, such as the legendary Tylenol #3 narcotic analgesic.

NSAIDs like ibuprofen are non-selective, meaning they non-selectively inhibit the prostaglandin synthesis enzymes, cyclo-oxygenase-1 (i.e., COX-1) and cyclo-oxygenase-2 (i.e., COX-2). The release of celecoxib (Celebrex, Searle/Pfizer), and most recently, valdecoxib (Bextra, Pharmacia) are breakthroughs in clinical pharmacology. It has been found that cyclo-oxygenase, an enzyme that is essential in the formulation of prostaglandins, has two key subtypes known as cyclo-oxygenase-1 (COX-1) and cyclo-oxygenase-2 (COX-2). Prostaglandins therefore are likewise subdivided into two main subtypes.

“Normal” (physiologic) prostaglandins are constantly being produced and are found in most tissues. They participate in the physiological maintenance of gastric mucosa, renal function and coagulation.

“Inducible” (pathological) prostaglandins are synthesized as a result of inflammatory stimuli. This latter category, when induced, causes pain and inflammation. The “normal” prostaglandins are enzymatically catalyzed by cyclo-oxygenase-1 (COX-1), whereas the “pathological” prostaglandins are enzymatically catalyzed by cyclogenase-2 (COX-2).

So, the aforementioned COX-2 inhibiting drugs are relatively sparing of the physiologic (maintenance/protective) prostaglandins.

It is important to note that COX-2 inhibitors do provide a level of safety over the non-selective NSAIDs, however, their ability to relieve pain is quite similar. Therefore, we tend to prefer the OTC acetaminophen or ibuprofen over the more expensive prescription COX-2 drugs. It should be noted, however, that use of any other NSAIDs is contraindicated in patients who are taking a COX-2 inhibitor long-term.

Beyond the COX-2 inhibitors, there is one additional prescription drug worthy of discussion. Tramadol HCl (Ultram, Ortho-McNeil) is a non-narcotic prescription drug whose clinical effectiveness is equivalent to acetaminophen with codeine (Tylenol #3). Tramadol HCl offers control of moderate to moderately severe pain without the disadvantages of narcotics. Ultram possesses a dual synergistic mechanism: weak opioid receptor binding, and weak inhibition of norepinephrine and serotonin re-uptake.

This drug can be taken without regard to meals and has minimal side effects, such as dizziness, nausea, constipation, headaches and somnolence. However, patients with a history of seizures should not use Ultram. The dosage is one to two 50mg tablets q4-6 hours prn, not to exceed 400mg per day.