Why can painkillers make a headache worse? And what exactly is “medication overuse”?
“MY HEAD HURTS ALMOST EVERY DAY, AND NOTHING HELPS!”
But when you start asking questions, it turns out that the pills do help — but only for a couple of hours, and then the pain returns again.
This is a classic medication-overuse headache (MOH).
It develops because of taking painkillers too often.
📌 Numbers and facts
You’re at risk if you take:
• NSAIDs (ibuprofen, ketorolac, nimesulide, etc.) more than 10–15 doses per month
• Triptans more than 8–10 doses per month
• Combined analgesics (Citramon, Pentalgin, Sedalgin) are especially dangerous — even fewer than 8 doses may be enough:
✖️ They provide quick relief → you develop the habit of reaching for them immediately
✖️ They contain caffeine/phenobarbital/codeine → dependence
✖️ Their effect is short → pain returns faster → another dose is needed
✖️ Multiple active ingredients → extra risk for liver, stomach and vessels
❓ How medication overuse develops
- initially, pills really help
- their effect becomes shorter
- eventually the head hurts almost daily
- the person assumes the illness is “getting worse”, but they’re actually stuck in a loop
❓ Next common question:
“ But how is it possible that pills make the pain worse?”
There are several hypotheses:
🔵 Brain sensitization
Frequent analgesic use changes pain thresholds:
➡️ The antinociceptive (pain-inhibiting) systems become less active. The trigeminal system becomes more excitable
➡️ As a result, the brain reacts with pain to minimal stimuli
🔵 Neurotransmitter imbalance
➡️ Evidence shows that medication overuse disrupts serotonin and dopamine balance:
Serotonin decreases (normally it suppresses migraine), dopamine increases
➡️ Sensitivity to triggers grows
🔵 CGRP and inflammation
➡️ Uncontrolled painkiller use increases CGRP release (a key protein in migraine pathways)
➡️ Chronic pain develops. This is why anti-CGRP drugs work so well in MOH patients
🔵 Dependence factor
Especially with combined analgesics: caffeine, codeine, barbiturates shape a behavioral habit
➡️ slightest pain = pill
➡️ the cycle becomes reinforced: the more often you take them, the faster the pain returns
What to do if you suspect medication overuse?
- Keep a headache diary
- Do NOT stop painkillers abruptly
- Discuss with a doctor a structured plan to taper and prevent frequent attacks
The problem isn’t “bad pills” — it’s how the brain adapts when they’re taken too often. Painkillers are allowed — but within reason and with clear boundaries