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Pharmacology > Stimulatns&treatment of Headache > Flashcards

Stimulatns&treatment of Headache Flashcards

1
Q

amphetamine like drugs

A
  • amphetamine found to produce weight loss in early studies of pts with narcolepsy
  • rate of weight loss is increased by ~ 0.5 pound per week
  • efficacy is similar btwn drugs
  • no long -term weight loss unless the drugs are taken continuously
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2
Q

SE of amphetamine like drugs

A
  • potential for drug abuse and habituation
  • exacerbation of HTN
  • sleep disturbances
  • palpitations
  • dry mouth
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3
Q

MOA of methamphetamine

A
  • releases dopamine, other biogenic amines
  • inhibits neuronal and vesicular monoamine transporters
  • inhibit MAO
  • CNS stimulants w/ little peripheral effects at low doses compared to amphetamine
  • high dose inc. BP and Inc. cardiac output
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4
Q

SE of methamphetamine

A 
high abuse potential
HTN
Tachycardia
Increased risk of stroke, MI
Insomnia
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5
Q

indications of methamphetamine

A
  • exogenous obesity

- short term adjunctive therapy for pts refractory to standard therapies (repeated diets and other drugs)

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6
Q

contraindications of methamphetamine

A

CV disease, HTN, hyperthyroidism, history of drug abuse

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7
Q

methamphetamine drug interactions

A
  • should not be combined w/ MAOs or other NS stimulants

- decrease effectiveness of guanethidine used to treat hypertension

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8
Q

MOA of phentermine

A
  • sympathomimetics, CNS stimulant

- increased NE release from central noradrenergic neurons

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9
Q

effectiveness of phentermine

A
  • 2-10kg loss of original wt as long as the drug is taken

- weight regained once therapy ceases- used chronically

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10
Q

AE of phentermine

A
  • dry mouth, insomnia, constipation
  • HTN, tachycardia
  • abuse liability thought to be low
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11
Q

drug interactions

A

MAOIs, guanethidine, other CNS stimulants, alcohol, sibutramine and tricyclic antidepressants

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12
Q

contraindications of phentermine

A

HTN, advanced CV disease, hyperthyroidism, glaucoma, anxiety and history of drug abuse

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13
Q

MOA of Sibutramine

A

inhibits the reuptake of NE, serotonin, dopamine

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14
Q

effectiveness of Sibutramine

A

10% loss of original wt as long as the drug is taken

-wt regained once therapy ceases-used chronically

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15
Q

AE of Sibutramine

A
  • dry mouth, insomnia, constipation and asthenia

- Hypertension and tachycardia-required monitoring

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16
Q

what are the SSRI antidepressants

A
  • fluoxetine
  • setraline
  • paroxetine
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17
Q

MOA of SSRIs

A
  • increase wt loss in combo w/ caloric restriction for up to a yr
  • wt gain associated w/ long term use
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18
Q

what is Bupropion (Wellbutrin SR)

A
  • non SSRI antidepressant

- modestly effective when added to a program of caloric restriction

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19
Q

what are the Antiepileptic drugs

A

Topiramate

Zonisamide

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20
Q

MOA of Topiramate

A
  • produce wt loss in pts w/ epilepsy
  • increased wt loss in combo w/ caloric restriction: up to 6.3% in 6 months
  • longer durations and higher doses are more effective, but can be associated w/ adverse neurological and psychiatric effects
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21
Q

MOA of Zonisamide

A
  • shown to produce wt loss when used in treating epilepsy

- significantly increased wt loss w/ caloric restrictions: 6 kg over 16 wks

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22
Q

what drugs are used for Narcolepsy

A

amphetamine
dextroampheamine
methamphetamine

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23
Q

what are the AE of narcolepsy drugs

A

development of tolerance, abuse, potential, irritability, depression, paranoia

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24
Q

what drugs can be used to treat ADHD

A

methylphenidate
dextroamphetamine
amphetamine

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25
Q

what are the AE of ADHD

A

insomnia, wt loss, growth impairment

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26
Q

see table on 19+20

A

see table on 19+20

27
Q

how many time should acute therapy migraine medications be taken

A

limit to no more than 2 times per week

28
Q

prolonged use of many acute migraine medications can lead to what

A

daily headache that doe snot respond to preventive therapy

29
Q

which NSAIDS can be used for acute migraine therapy

A
  • aspirin
  • acetaminophen
  • naproxen
  • ibuprogen
  • for mild/moderate episodes w/o nausea, disability or need for bed rest
30
Q

what combination of analgesics can be used for acute migraine therapy

A
  • aspirin, acetaminophen & caffeine

- acetaminophen, isometheptene (sympathomimetic) & dichloralphenazone (chloral hydrate)

31
Q

MAO of metoclopramide

A
  • antimetic
  • 5HT4 agonist
  • dopamine D2 receptor antagonist
  • decreases nausea and vomiting
  • increases gastric motility and absorption of oral analgesics
  • some sedation
  • used for acute therapy migraine, nonspecific
32
Q

what opioids can be used for acute migraine therapy

A

butorphanol nasal spray; tramadol & acetaminophen

33
Q

which corticosteroid can be used for acute migraine therapy

A
  • dexamethasone

- may reduce recurrence within 72 hrs

34
Q

which ergot alkaloids can be used to treat acute therapy migraine

A
  • ergotamine tartrate

- dihydroergotamine (DHE)mesylate

35
Q

MAO of ergot alkaloids

A
  • nonspecific serotonin agonists
  • alpha-adrenergic agoinst
  • vasoconstrictors
36
Q

Indications of ergot alkaloids

A

moderate to severe migraine or many yrs

37
Q

what drugs interact w/ ergot alkaloids

A

effects potentiated by triptans, B-blockers, dopamine, nicotine, CPY3A4 inhibitors

38
Q

contraindications of ergot alkaloids

A

should not be taken within 24 hrs of a triptan

39
Q

pharmacokinectics of ergotamine

A
  • sublingual

- oral w/ caffeine

40
Q

SE of ergotamine

A
  • nausea and vomiting

- severe vasoconstriction

41
Q

pharmacokinetics of DHE

A
  • nasal spray
  • IV
  • IM
  • SC

-poor oral bioavailability but less AE than ergotamine

42
Q

which Triptans are used for acute migraine therapy

A
  • sumatriptan
  • almotriptan
  • frovatriptan
  • Rizatriptan
  • Eletriptan
  • Naratriptan
  • Zolmitriptan
43
Q

MAO of Triptans

A
  • serotonin (5GT1) agonists

- administered early in attack for best outcome

44
Q

pharmacokinetics of Triptans

A
  • oral, SC, nasal spray
  • onset of action more rapid w/ SC or nasal administration
  • 2-3 hour half life
  • exception: naratriptan, frovatriptan - slower onset, longer action
45
Q

SE of triptans

A

nausea & vomiting often associated w/ acute migraine

46
Q

AE of Triptans

A
  • flushing, tingling, feeling of fullness in head, neck, chest
  • injection site discomfort
  • cardiac complications - rare
47
Q

contraindications of Triptans

A

w/ preexisting arterial disease of HTN

48
Q

drug interaction with Triptans

A
  • not to be taken within 24hrs of initial dose or within 24 hrs of an ergotamine - to avoid additive vasoconstriction
  • not to be taken with MAOI (or within 2 weeks of stopping one)- Sumatriptan, rizatriptan or zolmitriptan
  • serum [ ] of some increased by propranolol
  • eletriptan concentration increased by CYP3A4 inhib
49
Q

what drugs can be used as preventative therapy for migraine

A
  • antiepileptics
  • antidepressants
  • B-blockers
  • CCBs
  • neurotoxins
  • long-acting NSAIDS
50
Q

indications for preventative migraine therapy

A
  • 2 or more attacks/month that produce disability lasting > 3 days/month
  • contraindication to, or failure of, acute treatments
  • use of abortive medications more than twice/week
  • presence of uncommon migraine conditions
51
Q

which anti epileptics can be used as preventive migraine therapy

A
  • valproate*, topramate

* divalproex: sodium valproate and valproic acid, 1:1 molar

52
Q

MAO of Valprate and topiramate in preventing migraine

A
  • reduce firing rate of midbrain serotonergic neurone
  • enhanced peripheral GABAa activity; reduced neuronal inflammation
  • enhanced central GABAa activity; increased central antiociception
  • decrease headache frequency
  • efficacy similar to propranolol
53
Q

which antidepressants can be used as a preventive migraine therapy

A

-amitriptyline, nortriptyline (tricyclic antidepressants)

54
Q

MOA of tricyclic antidepressants as preventive migraine therapy

A
  • effective dose lower than that for treating depression

- block reuptake of NE and serotonin; SSRIs are generally not effective at preventing migraine

55
Q

which B-blockers can be used as a preventive migraine therapy

A
  • propranolol and timolol approved for migraine prevention

- metoprolol, nadolol, atenolol

56
Q

which CCBs can be used as a preventative migraine therapy

A

-verapamil

57
Q

CCBs may interact with what

A
  • ergotamine, eletriptan (CYP3A4 inhibitor)

- do not combine with B-blocker

58
Q

which neurotoxins can be used as a preventative migraine therapy

A
  • botulinum toxin - onabotulinumtoxinA (botox)
  • approved for chronic migraine
  • done administered as injections across 7 head/neck muscle sites
59
Q

which long acting NSAIDs can be used as a preventative migraine therapy

A
  • naproxen sodium, flurbiprofen
  • short term prevention, e.g menstrual migraine
  • also for aborting acute attacks
60
Q

what drugs can be used for tension type headaches

A

NSAIDs, including combinations w/ propoxyphene, caffeine

-caffeine-increases NE and dopamine release; some vasoconstriction, generally increases the effectiveness of NSAIDs

61
Q

what preventive therapy is used for tension-type headaches

A

amitriptyline

62
Q

what drugs are used as acute therapy for cluster headaches

A

O2 - vasoconstrictive action
Triptans, SC
DHE, SC or IM
instranasal lidocaine

63
Q

what drugs are used as preventive therapy for cluster headaches

A 
CCBs
Lithium
Antiepiletpics
Ergotamine
Short-term corticosteroids

Pharmacology (23 decks)

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