2.6 PharmofMigraineHeadacheMedications

Question 1

What is Calcitonin Gene related peptide (CGRP)?

Answer 1

• Potent vasodilator
• action at peripheral receptors

Question 2

MOA of Sumatriptan

Answer 2

• vasoconstriction of painful intracranial extra cerebral vessels
• inhibition of vasoactive neuropeptide
• inhibition of nociceptive neurotransmission

Question 3

Therapeutic use of -triptans

Answer 3

• Migraine Pain
• Migraine Symptoms:
• nausea
• vomiting
• photophobia
• phonophobia

Question 4

The 3Fs that triptans can be used

Answer 4

Selecting the Right Triptan

Triptans can be chosen via the 3 F’s:

1.Fast versus slow onset of activity; duration of

  action can be important for some patients

2. Formulation (oral, injection, nasal)
3. Formulary tier and availability (sumatriptan =generic)

Question 5

Pharmokinetics of -triptans

Answer 5

• triptan: oral, nasal, subcutaneous (Sumatriptan)
• rapid onset of action

Question 6

Adverse effects of -triptans

Answer 6

• fatigue
• dizziness
• paresthesia
• warm sensations
• tightness (neck, chest, and throat)

Question 7

triptans: Contraindications

Answer 7

•hepatic/renal function impairment
•
•monoamine Oxidase Inhibitor therapy•hemiplegic migraine (associated with paralysis of one side of the face)
•
•basilar migraine (associated with loss of vision, double vision, loss of balance)
•
•hypersensitivity to -triptans•peripheral vascular disease or uncontrolled blood pressure

Question 8

How are ergot alkoids produced?

Answer 8

•Produced by Claviceps pururea a fungus

Question 9

•Poisoning effects of Ergot Alkoids

Answer 9

•hallucination•vasospasm (gangrene)•abortifacient (in pregnancy)

Question 10

MOA of Ergot alkaloids:

• Dihydroergotamine (DHE)
• Ergotamine

Answer 10

Mechanism of Action:

Agonist/antagonist at α1-adrenergic, at serotonin receptors (5-HT1A and 5-HT1D )

Partial or full agonist at dopamine receptors

DHE and Ergotamine constrict cranial vascular bed

Question 11

Therapeutic use of Ergotamine

Answer 11

Ergotamine
•migraine pain
•effective at beginning of attack

Question 12

Therapeutic use of DHE

Answer 12

• DHE
• intractable migraine (favored by some clinicians)

Question 13

Pharmakinetics of Ergotamine

Answer 13

Ergotamine
•routes of admin: oral and suppository
•high first pass effect
•combined with caffeine (helps bioavailability)
•excreted by liver

Question 14

Pharmokinetics of DHE

Answer 14

DHE
•routes of admin: SC, IV, IN, and oral
•metabolized by liver, excretion by feces
•metabolites similar to parent compound
•effects last longer than expected

Question 15

Adverse effects of Ergot Alkaloids

Answer 15

Decreased blood flow: brain, heart, extremities

Question 16

Adverse effects of Ergotamine

Answer 16

Ergotamine

• Adverse Effects
• diarrhea
• nausea
• vomiting

Question 17

Contraindications of of Ergotamine

Answer 17

• Contraindications
• obstructive vascular disease
• collagen disease

Question 18

Ergot alkaloids: Contraindications

Answer 18

• peripheral vascular disease or poor circulation
• arteriosclerosis
• hypertension
• angina
• history of heart attack/ silent ischemia
• liver/kidney disease
• serious infection
• 24 hr. separation from triptans

Question 19

MOA of Beta blockers

Answer 19

Unknown

Question 20

What is the first line drug for preventation of migraines?

Answer 20

Beta blockers

Question 21

B-1 do what?

Answer 21

increase heart rate

increase contractility

increase nerve conduction

Question 22

B2 receptors do what?

Answer 22

bronchodialation

relaxation

vasodilation

Question 23

B3 receptors do what?

Answer 23

Relax bladder

Question 24

Propranolol Pharmokinetics

Answer 24

• route of administration: oral
• hepatic first pass effect
• lipophilic
• metabolized by liver

Question 25

Adverse effects of Propanlol

Answer 25

• bradycardia
• sedation
• vivid dreams

Question 26

β-Blockers Drug Interactions with? and what occurs with this drug interaction?

Answer 26

• Calcium blockers i.e. verapamil
• severe hypotension
• bradycardia
• heart failure
• cardiac conductance abnormalities

Question 27

ANS drug rule?

Answer 27

•Receptor selectivity can be “relative” or “semi-selective” in that other receptor sub-types can be affected depending on the patient and drug dose/level

Example: A patient receiving albuterol (a beta-2 agonist, inhaled bronchodilator) experiences an increased heart rate

Question 28

Prochlorperazine MOA

Answer 28

Mechanism of Action: D2-antagonist in chemoreceptor trigger receptor zone”

Question 29

Prochlorperazine: Therapeutic Use

Answer 29

•Therapeutic Use Associated with Migraines

• vomiting
• nausea
• pain

Question 30

Prochlorperazine: Adverse Effects

Answer 30

• Adverse Effects
• extrapyramidal (acute dystonic effects)
• akathisia (restlessness)

Question 31

What is normally given with Prochlorperazine in order to prevent what?

Answer 31

Prochlorperazine often given with diphenhydramine prevents akathisia

Question 32

Which is better for pain Prochlorperazine (I.V.) or Sumatriptan (subcutaneous)?

Answer 32

Prochlorperazine (I.V.) reduces pain more than Sumatriptan (subcutaneous)

Question 33

Botox MOA

Answer 33

Mechanism of Action:

Enzymatic removal of amino acids in fusion proteins critical to the release of acetylcholine