Drugs for Headache

Question 1

Describe the mechanism of action of propanolol.

Answer 1

It is a beta blocker that may be related to decreasing adrenergic tone

Question 2

Describe the side effects associated with propanolol.

Answer 2

Cardiovascular side effects (e.g. SOB, fatigue, exercise intolerance), GI disturbance

Question 3

What are the contraindications to prescribing propanolol?

Answer 3

Ca++ channel blockers and asthma

Question 4

What is the clinical use of propanolol in the management of migraines?

Answer 4

Prophylaxis

Question 5

Describe the mechanism of action of valproate?

Answer 5

It is an anticonvulsant that increases GABA-mediated neurotransmission thus suppressing inflammation and also modulates 5-HT.

Question 6

What percentage of patients generally benefit from valproate?

Answer 6

About 50%

Question 7

Describe the side effects associated with valproate.

Answer 7

There are a lot- nausea, weight gain, fatigue, tremor, hair loss

Question 8

What are the contraindications to prescribing valproate for migraines?

Answer 8

Pregnancy

Question 9

Describe the role of valproate in the management of migraines.

Answer 9

Prophylaxis

Question 10

Describe the mechanism of action of topiramate.

Answer 10

It is a newer anticonvulsant that enhances GABA activity and blocks Na+ & Ca++ channels. It also inhibits glutamate receptors and the activation of TNC, which activates the pain centers in the thalamus.

Question 11

Name the side effects associated with topiramate.

Answer 11

Weight loss, paresthesias, fatigue, cognitive impairment, abnormal taste.

Question 12

Describe the use of topiramate in the management of migraines.

Answer 12

Prophylaxis

Question 13

Describe the mechanism of action of NSAIDs (e.g. naproxen)

Answer 13

Analgesic and anti-inflammatory

Question 14

Describe the side effects associated with NSAIDs.

Answer 14

Withdrawal and precipitation of migraines

Question 15

What is the clinical use of NSAIDs in the management of migraines?

Answer 15

They are useful as prophylaxis for predictable onset migraines and are good because they do not cause rebound headaches.

Question 16

Describe the mechanism of action of caffeine.

Answer 16

Causes vasoconstriction and can potentiate analgesics

Question 17

Describe the clinical use of caffeine in the management of migraines.

Answer 17

A common adjuvant with other anti-migraine medications, useful in mild to moderate migraines.

Question 18

Name the medications commonly used in the treatment of migraines.

Answer 18

Propanolol, valproate, topiramate, NSAIDs, caffeine, metaclopromide, ergotamine, dihydroergotamine, sumatriptan

Question 19

Describe the mechanism of action of metaclopromide.

Answer 19

It is an antagonist at 5-HT(3) and D2 receptors.

Question 20

Discuss the drawback of using metaclopromide.

Answer 20

It has little significant analgesic effect so it typically has to be used as an adjuvant.

Question 21

What is one unique benefit of metaclopromide?

Answer 21

It can keep you from throwing up.

Question 22

Describe the administration and pharmacokinetics involved with metaclopromide.

Answer 22

It has the highest response as an injectable, but can also be given nasally (spray), parenterally, or sublingually

Question 23

Name the medications used for prophylaxis in migraine management.

Answer 23

Propanolol, valproate, topiramate, and NSAIDs.

Question 24

Name the medications used for mild to moderate migraine treatment.

Answer 24

NSAIDs, caffeine, and metaclopromide.

Question 25

Describe the mechanism of action of ergotamine.

Answer 25

It is a cerebral vasoconstrictor and non-selective 5-HT agonist at the trigeminal nerve

Question 26

What are the common side effects associated with ergotamine?

Answer 26

Cramps, n/v, vertigo, can become dependent if taken >3 weeks; less commonly- ischemia, cold extremities, gangrene, and diarrhea

Question 27

What is the least effect form of administration for ergotamine?

Answer 27

Oral administration

Question 28

What is the clinical indication for ergotamine?

Answer 28

Acute migraines; best for moderate to severe migraines and works 80% of the time but most people have side effects.

Question 29

What side effects are associated with dihydroergotamine?

Answer 29

Nausea

Question 30

How do you administer dihydroergotamine?

Answer 30

Parenteral or nasal

Question 31

Describe the mechanism of action of sumatriptan.

Answer 31

It is a selective agonist at 5-HT receptors.

Question 32

What is unique about sumatriptans?

Answer 32

They can be effective when taken later in the course of a migraine (unlike ergots)

Question 33

Name the side effects associated with sumatriptan.

Answer 33

Much decreased side effects but can have injection site rxn if injected.

Question 34

What is a significant contraindication for sumatriptan?

Answer 34

Ischemic heart disease

Question 35

How can sumatriptan be administered?

Answer 35

PO, IM, sublingual, or nasal. The injectable is the fastest acting version.

Question 36

Name the medications used to manage moderate to severe migraines.

Answer 36

Ergotamine, dihydroergotamine, and sumatriptan

Question 37

How does migraine prophylaxis work?

Answer 37

It raises the threshold for cortical spreading depression (CSD) and work best with the classic presentation (with aura)

Question 38

What causes migraines?

Answer 38

Cortical spreading depression causes neuronal firing that spreads changing blood flow in the brain and activating the trigeminovascular system. The TGVS releases peptides (e.g. CGRP) and other vasoactive substances that cause neuroinflammation and result in pain.

Question 39

What is the role of serotonin in migraines?

Answer 39

We aren’t sure exactly, but it stimulates some pain afferents and causes cerebral vasoconstriction.