Analgesics and Migraine Medications

Recommended Texts for Further Reading

• Katzung, B.G., Basic and Clinical Pharmacology. Available in Access Pharmacy and Medicine databases at MWU Library.
• Pharmacology and Therapeutics for Dentistry, 7th Edition (2016).
• Lexicomp Dental, available at MWU Library website.
• Acute treatment of migraine in adults, available in the UpToDate database at MWU Library website.
• The Medical Letter, New drugs for migraine prevention, Issue 1559 (11/5/2018).

Analgesics

• Aspirin
• Acetaminophen (Tylenol)
• Excedrin (acetaminophen, aspirin, caffeine)
• Ibuprofen (Advil, Motrin)
• Naproxen sodium (Aleve, Anaprox); Treximet (naproxen + sumatriptan)
• Butorphanol (Stadol NS) (nasal spray)
• Ketorolac (Sprix, nasal spray), (Toradol)
• Midrin (isometheptene + dichloralphenazone + acetaminophen)
• Prodrin (isometheptene + caffeine + acetaminophen)

Ergot Alkaloids and 5-HT Receptors

• Ergotamine tartrate (Ergomar) (oral, sublingual, rectal)
• Ergotamine tartrate/caffeine/l-belladonna alkaloids/sodium pentobarbital (30mg) (Ercaf, Wigraine)
• Ergotamine/caffeine (Cafergot suppository)
• Dihydroergotamine (D.H.E.45) (IV, IM, SC, nasal)
• Dihydroergotamine mesylate nasal spray (Migranal)
• Sumatriptan (Imitrex) – first generation (SC, nasal spray, oral, transdermal patch)
• Zolmitriptan (Zomig, Zomig ZMT) – second generation (nasal or oral)
• Rizatriptan (Maxalt, Maxalt MLT) – second generation (oral)
• Eletriptan (Relpax) – second generation (oral)

Dopamine Antagonists - Antiemetics

• Metoclopramide (Reglan)
• Prochlorperazine (Compazine)
• Chlorpromazine (Thorazine)

Calcitonin Gene-Related Peptide (CGRP) Blockers

• Erenumab-aooe (Aimovig)
• Fremanezumab-vfrm (Ajovy)
• Galcanezumab-gnlm (Emgality)

Miscellaneous Drugs for Prophylaxis or Preventive Therapy

• Antihypertensive β-Blockers (e.g. metropolol, propranolol, timolol, atenolol, nadolol)
• Calcium Channel Blockers (verapamil, nimodipine, nifedipine)
• Antidepressants (amitriptyline, etc.)
• Anticonvulsant Drugs (valproate, topiramate, gabapentin)
• Lithium carbonate (Eskalith)
• Dexamethasone
• Feverfew
• Monoamine Oxidase Inhibitors – phenelzine (Nardil), isocarboxazid
• Botulinum toxin type A (Botox)
• Riboflavin - Vitamin B2

Migraine Phases and Aura

• Migraine attacks have 4 phases: prodrome, aura, headache, and postdrome.
• Common triggers include emotional stress, hormone changes (in women), and lack of food.
• Prodrome symptoms include euphoria, depression, irritability, cravings etc. (24-48 hours before head pain).
• Aura (visible in 25% of migraine sufferers) can be visual, sensory, verbal, or motor disturbances.
• Migraine headache pain is often one-sided, throbbing, and pulsating, often increasing in intensity, with nausea and vomiting, photophobia, and phonophobia.
• Postdrome symptoms can include tiredness or being refreshed/euphoric.

Migraine Visual Aura (information and YouTube link)

Proposed Etiology of Migraine Headaches (diagram)

Abortive vs. Prophylactic Migraine Therapy (diagram)

Migraine Diagnosis and Treatment (link)

Abortive or Pain-Relieving Medications

• Analgesics are effective for mild or moderate migraine pain (e.g., NSAIDs and acetaminophen).
• NSAIDs, like ibuprofen and naproxen, work by inhibiting prostaglandin synthesis, thereby lowering inflammation/pain in the trigeminal system.
• Acetaminophen (effective for migraine symptoms including photophobia and phonophobia) works in combination with other NSAIDs (e.g., Excedrin, which also includes caffeine).

Ergotamine Tartrate

• Used to treat moderate to severe migraines.
• Ergot alkaloids occur naturally in rye.
• Ergotamine is available in oral, sublingual, and suppository forms.
• Dihydroergotamine (D.H.E. 45) is equally effective in treating moderate to severe migraines (nasal spray is available).

5-HT Agonists

• Sumatriptan (Imitrex) and other triptans are first-line treatments for moderate to severe migraines.
• Triptans work by constricting inflamed/dilated intracranial arteries and inhibiting the release of vasodilators/inflammatory mediators from the trigeminal nerve endings.
• Second-generation triptans (e.g., Zolmitriptan) offer greater bioavailability relative to sumatriptan due to greater lipid-solubility.

Anti-emetics

• Metoclopramide (Reglan), Prochlorperazine (Compazine), and Chlorpromazine (Thorazine) are effective against migraine-related nausea/vomiting.
• These drugs also have anti-emetic properties.

Prophylaxis or Preventive Medications

• Prophylactic treatment for migraines is considered if a patient experiences 3 or more migraines per week, doesn't respond to acute therapies, or needs acute therapies over twice a week.
• Therapy should be continued for at least 3 to 6 months to check for remission

Cardiovascular Drugs

• Beta-blockers (e.g., propranolol) may help with migraine prophylaxis.
• Mechanism of action isn't fully understood.
• They can increase vasoconstriction.

Antidepressants

• Amitriptyline (Elavil) helps with migraine prophylaxis.
• Mechanism of action is independent from its antidepressant functions; it may increase serotonin/norepinephrine concentrations in the CNS via inhibiting reuptake.

Antiseizure or Anticonvulsant Drugs

• Valproic acid (Depakote) and topiramate (Topamax) are effective for migraine prophylaxis.
• Their mechanism involves blocking voltage-dependent sodium channels and increasing GABA levels.

Botulinum Toxin Type A (Botox)

• Botox is effective for migraine prophylaxis (primarily chronic migraines) in cases where acute therapies fail.
• Mechanism for pain relief isn't completely understood.

Calcitonin Gene-Related Peptide (CGRP) Blockers

• Erenumab-aooe (Aimovig), Fremanezumab-vfrm (Ajovy), and Galcanezumab-gnlm (Emgality) prevent migraines by blocking CGRP, a potent vasodilator and pain-signaling neurotransmitter.

Migraine in Children

• Migraines in children are generally shorter than in adults (symptoms typically lasting 30 minutes to 72 hours).
• Triggers, like diet, may differ compared to adults.
• Treatments like acetaminophen and ibuprofen are recommended for migraine, but metoclopramide should not.

This lesson covers analgesics like aspirin, acetaminophen, ibuprofen, and naproxen. It also discusses migraine treatments, including ergot alkaloids and 5-HT receptor agonists. Key medications and resources for further reading are mentioned.