2.6 PharmofMigraineHeadacheMedications Flashcards
What is Calcitonin Gene related peptide (CGRP)?
- Potent vasodilator
- action at peripheral receptors
MOA of Sumatriptan
- vasoconstriction of painful intracranial extra cerebral vessels
- inhibition of vasoactive neuropeptide
- inhibition of nociceptive neurotransmission
Therapeutic use of -triptans
- Migraine Pain
- Migraine Symptoms:
- nausea
- vomiting
- photophobia
- phonophobia
The 3Fs that triptans can be used
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
- Formulation (oral, injection, nasal)
- Formulary tier and availability (sumatriptan =generic)
Pharmokinetics of -triptans
- triptan: oral, nasal, subcutaneous (Sumatriptan)
- rapid onset of action
Adverse effects of -triptans
- fatigue
- dizziness
- paresthesia
- warm sensations
- tightness (neck, chest, and throat)
triptans: Contraindications
•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
How are ergot alkoids produced?
•Produced by Claviceps pururea a fungus
•Poisoning effects of Ergot Alkoids
•hallucination•vasospasm (gangrene)•abortifacient (in pregnancy)
MOA of Ergot alkaloids:
- Dihydroergotamine (DHE)
- Ergotamine
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
Therapeutic use of Ergotamine
Ergotamine
•migraine pain
•effective at beginning of attack
Therapeutic use of DHE
- DHE
- intractable migraine (favored by some clinicians)
Pharmakinetics of Ergotamine
Ergotamine
•routes of admin: oral and suppository
•high first pass effect
•combined with caffeine (helps bioavailability)
•excreted by liver
Pharmokinetics of DHE
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
Adverse effects of Ergot Alkaloids
Decreased blood flow: brain, heart, extremities
Adverse effects of Ergotamine
Ergotamine
- Adverse Effects
- diarrhea
- nausea
- vomiting
Contraindications of of Ergotamine
- Contraindications
- obstructive vascular disease
- collagen disease
Ergot alkaloids: Contraindications
- 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
MOA of Beta blockers
Unknown
What is the first line drug for preventation of migraines?
Beta blockers
B-1 do what?
increase heart rate
increase contractility
increase nerve conduction
B2 receptors do what?
bronchodialation
relaxation
vasodilation
B3 receptors do what?
Relax bladder
Propranolol Pharmokinetics
- route of administration: oral
- hepatic first pass effect
- lipophilic
- metabolized by liver
Adverse effects of Propanlol
- bradycardia
- sedation
- vivid dreams
β-Blockers Drug Interactions with? and what occurs with this drug interaction?
- Calcium blockers i.e. verapamil
- severe hypotension
- bradycardia
- heart failure
- cardiac conductance abnormalities
ANS drug rule?
•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
Prochlorperazine MOA
Mechanism of Action: D2-antagonist in chemoreceptor trigger receptor zone”
Prochlorperazine: Therapeutic Use
•Therapeutic Use Associated with Migraines
- vomiting
- nausea
- pain
Prochlorperazine: Adverse Effects
- Adverse Effects
- extrapyramidal (acute dystonic effects)
- akathisia (restlessness)
What is normally given with Prochlorperazine in order to prevent what?
Prochlorperazine often given with diphenhydramine prevents akathisia
Which is better for pain Prochlorperazine (I.V.) or Sumatriptan (subcutaneous)?
Prochlorperazine (I.V.) reduces pain more than Sumatriptan (subcutaneous)
Botox MOA
Mechanism of Action:
Enzymatic removal of amino acids in fusion proteins critical to the release of acetylcholine
