Stimulatns&treatment of Headache Flashcards
amphetamine like drugs
- 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
SE of amphetamine like drugs
- potential for drug abuse and habituation
- exacerbation of HTN
- sleep disturbances
- palpitations
- dry mouth
MOA of methamphetamine
- 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
SE of methamphetamine
high abuse potential HTN Tachycardia Increased risk of stroke, MI Insomnia
indications of methamphetamine
- exogenous obesity
- short term adjunctive therapy for pts refractory to standard therapies (repeated diets and other drugs)
contraindications of methamphetamine
CV disease, HTN, hyperthyroidism, history of drug abuse
methamphetamine drug interactions
- should not be combined w/ MAOs or other NS stimulants
- decrease effectiveness of guanethidine used to treat hypertension
MOA of phentermine
- sympathomimetics, CNS stimulant
- increased NE release from central noradrenergic neurons
effectiveness of phentermine
- 2-10kg loss of original wt as long as the drug is taken
- weight regained once therapy ceases- used chronically
AE of phentermine
- dry mouth, insomnia, constipation
- HTN, tachycardia
- abuse liability thought to be low
drug interactions
MAOIs, guanethidine, other CNS stimulants, alcohol, sibutramine and tricyclic antidepressants
contraindications of phentermine
HTN, advanced CV disease, hyperthyroidism, glaucoma, anxiety and history of drug abuse
MOA of Sibutramine
inhibits the reuptake of NE, serotonin, dopamine
effectiveness of Sibutramine
10% loss of original wt as long as the drug is taken
-wt regained once therapy ceases-used chronically
AE of Sibutramine
- dry mouth, insomnia, constipation and asthenia
- Hypertension and tachycardia-required monitoring
what are the SSRI antidepressants
- fluoxetine
- setraline
- paroxetine
MOA of SSRIs
- increase wt loss in combo w/ caloric restriction for up to a yr
- wt gain associated w/ long term use
what is Bupropion (Wellbutrin SR)
- non SSRI antidepressant
- modestly effective when added to a program of caloric restriction
what are the Antiepileptic drugs
Topiramate
Zonisamide
MOA of Topiramate
- 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
MOA of Zonisamide
- shown to produce wt loss when used in treating epilepsy
- significantly increased wt loss w/ caloric restrictions: 6 kg over 16 wks
what drugs are used for Narcolepsy
amphetamine
dextroampheamine
methamphetamine
what are the AE of narcolepsy drugs
development of tolerance, abuse, potential, irritability, depression, paranoia
what drugs can be used to treat ADHD
methylphenidate
dextroamphetamine
amphetamine
what are the AE of ADHD
insomnia, wt loss, growth impairment
see table on 19+20
see table on 19+20
how many time should acute therapy migraine medications be taken
limit to no more than 2 times per week
prolonged use of many acute migraine medications can lead to what
daily headache that doe snot respond to preventive therapy
which NSAIDS can be used for acute migraine therapy
- aspirin
- acetaminophen
- naproxen
- ibuprogen
- for mild/moderate episodes w/o nausea, disability or need for bed rest
what combination of analgesics can be used for acute migraine therapy
- aspirin, acetaminophen & caffeine
- acetaminophen, isometheptene (sympathomimetic) & dichloralphenazone (chloral hydrate)
MAO of metoclopramide
- 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
what opioids can be used for acute migraine therapy
butorphanol nasal spray; tramadol & acetaminophen
which corticosteroid can be used for acute migraine therapy
- dexamethasone
- may reduce recurrence within 72 hrs
which ergot alkaloids can be used to treat acute therapy migraine
- ergotamine tartrate
- dihydroergotamine (DHE)mesylate
MAO of ergot alkaloids
- nonspecific serotonin agonists
- alpha-adrenergic agoinst
- vasoconstrictors
Indications of ergot alkaloids
moderate to severe migraine or many yrs
what drugs interact w/ ergot alkaloids
effects potentiated by triptans, B-blockers, dopamine, nicotine, CPY3A4 inhibitors
contraindications of ergot alkaloids
should not be taken within 24 hrs of a triptan
pharmacokinectics of ergotamine
- sublingual
- oral w/ caffeine
SE of ergotamine
- nausea and vomiting
- severe vasoconstriction
pharmacokinetics of DHE
- nasal spray
- IV
- IM
- SC
-poor oral bioavailability but less AE than ergotamine
which Triptans are used for acute migraine therapy
- sumatriptan
- almotriptan
- frovatriptan
- Rizatriptan
- Eletriptan
- Naratriptan
- Zolmitriptan
MAO of Triptans
- serotonin (5GT1) agonists
- administered early in attack for best outcome
pharmacokinetics of Triptans
- 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
SE of triptans
nausea & vomiting often associated w/ acute migraine
AE of Triptans
- flushing, tingling, feeling of fullness in head, neck, chest
- injection site discomfort
- cardiac complications - rare
contraindications of Triptans
w/ preexisting arterial disease of HTN
drug interaction with Triptans
- 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
what drugs can be used as preventative therapy for migraine
- antiepileptics
- antidepressants
- B-blockers
- CCBs
- neurotoxins
- long-acting NSAIDS
indications for preventative migraine therapy
- 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
which anti epileptics can be used as preventive migraine therapy
- valproate*, topramate
* divalproex: sodium valproate and valproic acid, 1:1 molar
MAO of Valprate and topiramate in preventing migraine
- 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
which antidepressants can be used as a preventive migraine therapy
-amitriptyline, nortriptyline (tricyclic antidepressants)
MOA of tricyclic antidepressants as preventive migraine therapy
- effective dose lower than that for treating depression
- block reuptake of NE and serotonin; SSRIs are generally not effective at preventing migraine
which B-blockers can be used as a preventive migraine therapy
- propranolol and timolol approved for migraine prevention
- metoprolol, nadolol, atenolol
which CCBs can be used as a preventative migraine therapy
-verapamil
CCBs may interact with what
- ergotamine, eletriptan (CYP3A4 inhibitor)
- do not combine with B-blocker
which neurotoxins can be used as a preventative migraine therapy
- botulinum toxin - onabotulinumtoxinA (botox)
- approved for chronic migraine
- done administered as injections across 7 head/neck muscle sites
which long acting NSAIDs can be used as a preventative migraine therapy
- naproxen sodium, flurbiprofen
- short term prevention, e.g menstrual migraine
- also for aborting acute attacks
what drugs can be used for tension type headaches
NSAIDs, including combinations w/ propoxyphene, caffeine
-caffeine-increases NE and dopamine release; some vasoconstriction, generally increases the effectiveness of NSAIDs
what preventive therapy is used for tension-type headaches
amitriptyline
what drugs are used as acute therapy for cluster headaches
O2 - vasoconstrictive action
Triptans, SC
DHE, SC or IM
instranasal lidocaine
what drugs are used as preventive therapy for cluster headaches
CCBs Lithium Antiepiletpics Ergotamine Short-term corticosteroids
