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Neuroscience II > Pharmacology - Agents for headaches and migraines > Flashcards

Pharmacology - Agents for headaches and migraines Flashcards

1
Q

Butalbital

A

Combination with other drugs for common headaches
Barbiturate
Incr GABAa channel opening–>CNS depressant

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2
Q

Almotriptan

A

Triptan
Migraine treatment
Metab by cyto P450 and MAO-A

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3
Q

Eletriptan, frovatriptan, naratriptan

A

Triptans
Migraine treatment
Metab by cyto P450, thus contraind with hepatic/renal impairment

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4
Q

Rizatriptan, sumatriptan, zolmitriptan

A

Triptans
Migraine treatment
Metab by MAO-A, thus contraind when taking MAO inhibitors

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5
Q

Triptans

A

Migraine treatment
Selective agonists of 5HT1b and 5HT1d
Inhib release of vasodilators–>vasoconstriction–>prevent abnormal dilation of intracranial blood vessels

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6
Q

Sumatriptan adverse effect

A

Injection site reactions

Nasal preparation–>bitter taste

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7
Q

Triptan adverse effects

A 
Parasthesias
Asthenia and fatigue
Flushing
Feelings of pressure
Tightness
Pain in chest, neck, jaw
Drowsiness
Dizziness
Nausea
Sweating
coronary vasospasm-->contraind in pts with CAD
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8
Q

Ergot and ergot alkaloids

A

Migraine treatment
Act on alpha and serotonin recep (5HT1b/5HT1d recep)
Agonist and partial agonist at CNS dopamine recep
Low bioavailability
Constrict most blood vessels
Contract uterus

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9
Q

Ergotamine

A 
Ergot and ergot alkaloid
Migraine treatment
Longer half life and longer acting than dihydroergotamine
Sublingual, oral, inhaler, suppository
IM or IV for severe attacks
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10
Q

Dihydroergotamine

A 
Ergot and ergot alkaloid
Migraine treatment
Shorter half life and shorter acting than ergotamine
Nasal spray
IM or IV for severe attacks
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11
Q

Ergot and ergot alkaloid adverse reactions

A

Nausea, vomiting, leg weakness, muscle pain, numbness and tingling of fingers and toes
Toxic doses–>prolonged vasospasm–>limb gangrene and bowel infarction
Contraind in pregnancy, PVD, CAD, htn, impaired hepatic/renal function
Rebound headache with abrupt discontinuation

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12
Q

Common headache treatment

A

OTC

Combination

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13
Q

Migraine treatment

A

Triptans

Ergot and ergot alkaloids

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14
Q

Migraine prevention

A

Antihypertensives - b blockers, CCBs
Antidepressants - TCAs, MAOIs, serotonin recep antagonists
Antiepileptic - topiramate, gabapentin, valproic acid
Methysergide

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15
Q

B blockers

A

Migraine prevention
Only antihypertensive drug indicated for migraine prophylaxis
Several weeks for onset

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16
Q

CCBs

A 
Migraine prevention
Inhib Ca entry-->relaxation of vasc smooth muscle and vasodilation
Efficacy for migraine prophylaxis weak
Off label
May dev tolerance
17
Q

Propranolol, timolol, metoprolol, nadolol, atenolol

A

B blockers

Migraine prevention

18
Q

Verapamil

A

CCB

Migraine prevention

19
Q

Tricyclic antidepressants (TCAs)

A

Migraine prevention
Off label
Sedating

20
Q

Amitriptyline, nortriptyline, imipramine, doxepin, protriptyline

A

TCAs
Migraine prevention
Amitriptyline most common and efficacious

21
Q

Monoamine oxidase inhibitors (MAOIs)

A

Migraine prevention

Off label

22
Q

Phenelzine

A

MAOI
Migraine prevention
Substantial side effects
Questionable efficacy

23
Q

Serotonin receptor antagonists

A

Migraine prevention
Block 5HT2 and 5HT3 recep
Off label

24
Q

Mirtazapine

A

Serotonin recep antagonist

Migraine prevention

25
Q

Topiramate

A 
Migraine prevention
Blocks voltage Na channels
Activates hyperpol K current
Enhances GABAa
Blocks AMPA
26
Q

Topiramate adverse effects

A

Somnolence, fatigue, wt loss, nervousness

27
Q

Gabapentin

A

Migraine prevention

No biotransformation

28
Q

Gabapentin side effects

A

Somnolence, dizziness, ataxia, fatigue

Usually subsides after 2wks of use

29
Q

Valproic acid

A

Migraine prevention
Interfere with NMDA and GABA signaling
Extensive metab by liver

30
Q

Valproic acid adverse effects

A

GI symptoms, sedation, ataxia, tremor

Serious rare ones are pancreatitis, hyperammonemia, teratogenic, fulminant hepatitis

31
Q

Methysergide

A 
Migraine prevention
Ergot derivative
Mixed agonist/antagonist on serotonin recep
No benefit during acute attack
Not available in US
32
Q

Methysergide side effects

A

Inflammatory fibrosis and dependence (req tx interruption)

33
Q

Tension headache treatment

A

Amitriptyline

34
Q

Cluster headache treatment

A

Abortive: sumatriptan
Preventive: verapamil, lithium, prednisone, indomethacin, topiramate, frovatriptan

Neuroscience II (4 decks)

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