How Does Ketorolac Work? Mechanism of Action Explained in Plain English

Updated:

February 17, 2026

Author:

Peter Daggett

Summarize this blog with AI:

How does Ketorolac (Toradol) work? A plain-English explanation of its mechanism of action, how fast it works, and what makes it different from other NSAIDs.

How Does Ketorolac Work?

Ketorolac works by blocking the enzymes in your body that produce pain-causing chemicals called prostaglandins, providing powerful short-term pain relief comparable to opioid medications.

If you've been prescribed Ketorolac (brand name Toradol) — or you're curious about how this potent NSAID actually reduces pain — this article breaks it down in plain language. No medical degree required.

What Ketorolac Does in Your Body

To understand how Ketorolac works, it helps to understand what causes pain and inflammation in the first place.

The Pain Signal Chain

When you're injured or have surgery, your body kicks off a chain reaction:

  1. Damaged cells release a fatty acid called arachidonic acid
  2. Enzymes called COX-1 and COX-2 (cyclooxygenase) convert that acid into chemicals called prostaglandins
  3. Prostaglandins cause pain, swelling, inflammation, and fever at the injury site

Think of it like a fire alarm system: the injury is the smoke, COX enzymes are the alarm sensors, and prostaglandins are the blaring alarms that make you feel pain.

How Ketorolac Turns Down the Alarm

Ketorolac is a non-selective COX inhibitor — meaning it blocks both COX-1 and COX-2 enzymes. By shutting down these enzymes, Ketorolac stops your body from making prostaglandins at the site of injury.

The result: less pain, less inflammation, and less swelling.

Here's the analogy: if prostaglandins are fire alarms, Ketorolac is like disconnecting the alarm sensors. The smoke (injury) is still there, but the blaring alarm (pain signal) is significantly quieter.

Why Ketorolac Is Stronger Than Other NSAIDs

All NSAIDs — Ibuprofen, Naproxen, Diclofenac — work by blocking COX enzymes. So what makes Ketorolac special?

Ketorolac has an unusually high analgesic (pain-relieving) potency compared to its anti-inflammatory effect. In simple terms, while other NSAIDs are balanced between reducing pain and reducing inflammation, Ketorolac is tilted heavily toward pain relief. That's why it's described as providing "opioid-level analgesia" — it relieves pain as effectively as some narcotic medications, without the addiction risk.

How Long Does Ketorolac Take to Work?

The onset depends on how it's given:

  • IV injection: Pain relief begins within minutes. Peak effect in about 1-2 hours.
  • IM injection: Works within 10-30 minutes. Peak effect in 1-2 hours.
  • Oral tablets: Takes about 30-60 minutes to start working. Peak effect in 2-3 hours.
  • Nasal spray (Sprix): Onset in about 20-30 minutes.

This rapid onset — especially with injection — is one reason Ketorolac is so popular in emergency rooms and post-surgical settings.

How Long Does Ketorolac Last?

A single dose of Ketorolac provides pain relief for approximately 4 to 6 hours. The medication's half-life is about 5-6 hours in healthy adults, meaning half the drug is cleared from your system in that time.

In elderly patients, the half-life can be longer (6-7 hours), which is one reason lower doses are recommended for patients 65 and older.

The total treatment duration must not exceed 5 days across all forms (oral, injection, nasal spray) combined. For details on why this limit exists and what happens if you take it longer, see our article on Ketorolac side effects.

What Makes Ketorolac Different From Similar Medications?

Here's how Ketorolac compares to other common pain relievers:

Ketorolac vs. Ibuprofen

Both are NSAIDs, but Ketorolac is significantly more potent. Ibuprofen is available over the counter and safe for longer-term use. Ketorolac requires a prescription and is limited to 5 days. If you need ongoing pain relief, your doctor will likely switch you to an alternative like Ibuprofen or Naproxen.

Ketorolac vs. Diclofenac

Diclofenac is another prescription NSAID with similar anti-inflammatory potency. It's available in oral, topical, and injectable forms (Dyloject IV) and can be used for longer periods. Ketorolac has a stronger analgesic effect but more restrictions on duration.

Ketorolac vs. Celecoxib (Celebrex)

Celecoxib is a COX-2 selective inhibitor — it blocks only COX-2, leaving COX-1 mostly alone. This means fewer GI side effects (less stomach bleeding risk), but it's less potent for acute pain relief. Celecoxib is a better choice for patients at high risk of stomach problems.

Ketorolac vs. Opioids

This is the comparison that matters most. Ketorolac provides pain relief comparable to moderate-dose opioids like Morphine — but without the risks of addiction, respiratory depression, or sedation. This makes it a valuable tool in the ongoing effort to reduce opioid use in acute care settings.

Final Thoughts

Ketorolac is a uniquely powerful NSAID that works by blocking the COX enzymes responsible for producing pain-causing prostaglandins. Its high analgesic potency, rapid onset, and non-addictive profile make it an important option for short-term acute pain management.

Just remember: its strength comes with strict rules. Five days maximum, never with other NSAIDs, and always under medical supervision.

Want to learn more? Read our comprehensive guide on what Ketorolac is, its uses, and dosage information, or find out about drug interactions to watch for.

Is Ketorolac as strong as an opioid?

Ketorolac provides analgesic (pain-relieving) potency comparable to moderate-dose opioids like Morphine, but it works through a completely different mechanism. Unlike opioids, Ketorolac is not addictive and doesn't cause respiratory depression or sedation.

How quickly does a Ketorolac injection work?

An IV Ketorolac injection begins working within minutes, with peak pain relief occurring in about 1-2 hours. An IM (intramuscular) injection typically works within 10-30 minutes. This fast onset is why it's commonly used in emergency departments.

What is the difference between COX-1 and COX-2?

COX-1 and COX-2 are enzymes that produce prostaglandins. COX-1 is active all the time and helps protect the stomach lining and support kidney function. COX-2 is mainly activated during injury and inflammation. Ketorolac blocks both, which is why it's so effective but also why it can cause stomach and kidney side effects.

Why can't I take Ketorolac for more than 5 days?

The 5-day limit exists because Ketorolac's potent blocking of COX enzymes, while great for short-term pain relief, significantly increases the risk of serious GI bleeding, kidney damage, and cardiovascular events when used longer. Other NSAIDs like Ibuprofen or Naproxen are safer for extended use.

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