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Serotonin and Ergot Alkaloids
Pharm Interval II - Robert Wood Johnson
24
Pharmacology
Graduate
01/12/2011

Additional Pharmacology Flashcards

 


 

Cards

Term
Three primary headache types
Definition

Migraine

 

Cluster

 

Tension-type

 

 

Term
Where do secondary headaches come from?
Definition

Head Trauma

Vascular disorders

CNS infections

Metabolic disorders

Brain tumors

Term
Description of a migraine
Definition

Women more than men in 20s-40s, unilateral or bilateral, mod-severe, pulsating, aggravated by activity, nausea/vomiting, light, sound, and smell sensitive, familial, and alleviated by sleep

 

Post-migraine: tired, dull, neck pain

Term
Types of migraine
Definition

With aura (classic): less common type of migraine

Visual auras are most common, lasting minutes to 24 hours

Aura may be visual, sensory, or somatic

 

Without aura (common)

Term
Pathophysiology of migraines
Definition

1. Problems with bloodflow to parts of brain

2.  Trigeminal gets over excited

3.  Trigeminal releases vasodilators: sub P, neurokinin A, calcitonin gene-related peptide

4.  Vasodilation displaces brain things

5.  Diminished serotonin, a vasoconstrictor play a role

Term
Risk factors and triggers of migraines
Definition
Stress, allergies, pressure changes, changes in sleep, alcohol, lights/sounds/smells, use or withdrawal of caffeine, smoke, hypoglycemia, OCPs, tyramine, MSG, nitrates, phenylethylamine, aspartame
Term
Diagnosis of migraines
Definition

1. Lack of physical findings

2.  Not connected to trauma and do not cause neurological damage

3.  MRI/CT rules out sinus infection or other causes

Term
Migraine treatment
Definition

Avoid triggers: make diary to identify triggers

 

Abortive therapy: Analgesics, serotonin receptor agonists, anti-emetics

Term
Facts about Serotonin
Definition

Tryptophan + hydroxylation + decarboxylation

 

7 classes with subclasses

 

G-protein or ligand gated channels

 

Vasoconstricts everywhere but skeletal muscle and heart

 

Contracts GI smooth muscle/starts peristalsis

Term

Triptans

 

(Sumatriptan, Zolmatriptan, Naratriptan, Rizatriptan, Almotriptain, Frovatriptan, Eletriptan)

Definition

Initial therapy for moderate to severe migraines

 

Work on head pain and nausea, etc.

Effective 4+ hours after onset of headache

Onset of drug 1-2 hours

Stimulates serotonergic
5‐HT1B/1D

receptors

Well tolerated with only tingliness, dizziness, chest tightness

Expensive

 

Term
Triptans mechanism
Definition

Reduce excitability of trigeminal and therefore release of vasodilators

Vasoconstrict by stimulation of serotonin receptors

 

Term
Triptans contraindications
Definition

1.  Serotonin receptors on cardiac as well - not for heart disease/OD = cardiac ischemia

2.  Heart or peripheral vascular disease

3.  Cerbrovascular disease

4.  Use with ergots, triptans, or MAOIs because of serotonin syndrome

Term
Sumatriptan
Definition

Analog of serotonin

First triptan approved

Prototype

Oral, SQ (fast acting), or nasal spray

1-2 hour half life

Term
2nd generation triptans
Definition

zolmitriptan,
naratriptan,

rizatriptan,
almotriptan,
frovatriptan,
and
eletriptan

 

Improved bioavailability

Zolmitriptan can be nasal spray

Try switching if patient doesn't respond

Frovatriptan takes 3-5 hours to work and has a 27 hour half life

CYP3A4
inhibitors reduce eletriptan and almotriptan clearance

Term
Ergots
Definition

Ergotamine tartrate and dihydroergotamine

 

Derivatives of lysergic acid - old gold standard

Must be taken ASAP to be effective

Stimulate
serotonergic
(5‐HT1A,
5‐HT1B,
5‐HT1D,

5‐HT1F,
5‐HT2) dopaminergic,
and
noradrenergic
receptors
(many
side
effects).

Use no more than 2x per week:

nausea, vomiting, anorexia, cardiac ischemia, lower extremity circulation problems, rebound headache

Term
Ergots
Definition

Ergotamine is oral, rectal, inhaled, or sublingual

Dihydroergotamine is oral, rectal, inhaled, sublingal, subcutaneous, or intramusclar.

 

Cheap

Term
Ergots mechanisms
Definition

Inhibition of release of neuropeptides

 

Vasoconstriction in brain

 

Sometimes given with caffeine to potentiate vasoconstriction

Term
Ergots contraindication
Definition
Heart disease, peripheral and cerebral vascular disease, hypertension, anemia, malnutrition, kidney and liver disease, sepsis, pregnancy, breast feeding, with
triacetyloleandomycin
or
erythromycin
(inhibitors
of
ergotamine metabolism)
or
with
triptans
Term
Intractable migraine
Definition

Do not respond to conventional therapy and need parenteral treatment:

Dihydroergotamine subQ, IM, or IV with antiemetic

 

Sumatriptan subQ

Term
Prophylactic migraine treatment
Definition

Criteria - impact life despite abortive treatment

more frequent than abortive treatment can be used

disabling

abortive treatment contraindicated

significant risk for future comorbidity

Term
Propanolol
Definition

Prophylactic migraine treatment

 

Beta blocker

First line due to safety and efficacy

Relief in 4-6 weeks

Dizziness, weakness, drowsiness, restlessness, tremor, nausea, bradycardia, bronchospasm

 

Contraindications: shock, valve disease, asthma

Term
Amitryptiline
Definition

Prophylactic migraine medication

 

Tricyclic antidepressant

First line due to safety and efficacy

Blocks serotonin reuptake

4-6 weeks for response

SSRIs don't work

Dry mouth, blurred vision, difficulty thinking, weight gain

Not for seizure disorders, pregnancy, children

 

 

Term
Verapamil and
Flunarizine
Definition

Migraine prophylaxis

 

Calcium channel blocker

Second line

Modest effect in 3 to 8 weeks

Vertigo, hypotension, nausea, muscle fatigue, constipation

Not for: severe hypotension, shock, CHF

Term
Methysergide
Definition

Migraine prophylaxis

 

semi-synthetic ergot alkaloid

third line

1-2 days to kick in

adverse effects serious: GI, fibrotic changes, CAD, angina

Not for: CAD, peripheral or cerebral vascular disease, hypertension, hepatic disease, PUD, pulmonary disease, RA, pregnancy, breastfeeding

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