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sumatriptan (Imitrex, migratriptan, Arcoiran, Sumavel DosePro)
Tradename: Imitrex.
Indications:
- treatment of migraine with or without aura
- may be less effective for migraine with aura [9]
Contraindications:
1) ischemic heart disease
2) Prinzmetal's angina
3) uncontrolled hypertension
4) seizures
5) liver or kidney disease
6) concurrent use of ergotamine derivatives
7) concurrent use of MAO inhibitors [5]
8) use for:
a) migraine prophylaxis
b) hemiplegic migraines
c) basilar migraines
d) cluster migraines
Dosage:
1) sumatriptan succinate:
- 6 mg SC, may repeat after 1 hour, max 12 mg/day
- do NOT administer IV
- 25 mg PO, may repeat up to 100 mg after 2 hours, max 200 mg/day
2) sumatriptan nasal spray
- do NOT prime the pump
- do not tilt head back or inhale while spraying
- 20 mg, 1 spray (10 mg) in each nostril
- may repeat in 2 hours if needed
- may 40 mg/day
Tabs: 25, 50 & 100 mg (sumatriptan succinate). {triangular shape}
Injection: 12 mg/mL (0.5 mL syringe, vial)
Sumavel DosePro delivers 6 mg of sumatriptan subcutaneously with a high-pressure burst of nitrogen gas instead of a needle [7]
Nasal spray: 5 mg, 20 mg.
Pharmacokinetics:
1) well absorbed orally
2) time to peak concentration is 5-20 minutes (10-30 minutes) [6]
3) terminal 1/2life is 1.5-2.6 hours
4) 22% eliminated unchanged in the urine
Adverse effects:
=== Nasal ===
1) common (> 10%)
- bad/unusual taste, nausea/vomiting
2) less common (1-10%)
- throat discomfort, nasal cavity/sinus discomfort, dizziness
3) uncommon (< 1%)
- atypical or burning sensation
=== Injection ===
1) common (> 10%)
- injection site reaction, tingling, hot flashes, dizziness
2) less common (1-10%)
- weakness, myalgia, burning sensation, chest tightness, drowsiness, headache, numbness, neck pain & stiffness, abdominal discomfort, mouth discomfort, jaw discomfort, sweating
2) uncommon (< 1%)
- thirst, polydipsia, dehydration, dyspnea, hiccups, rash, dysuria, dysmenorrhea, renal calculus
4) other
a) coronary vasospasm
b) ventricular arrhythmias
c) frequent use can exarcerbate migraines [4]
d) jet injector (Sumavel DosePro) causes more redness, swelling, bleeding, & bruising than a needle injection [7]
Drug interactions:
1) MAO inhibitors: may decrease clearance of sumatriptan; allow 2 weeks after discontinuaton of MAO inhibitor
2) ergot alkaloids: in combination increase level of vasoconstriction
3) selective serotonin reuptake inhibitors (SSRI): in combination may result in weakness, hyper-reflexia & problems with coordination
Laboratory:
- sumatriptan in blood
- sumatriptan in serum/plasma
- sumatriptan in urine Mechanism or action:
1) selective agonist of vascular serotonin receptor 1D
Interactions
drug interactions
drug adverse effects (more general classes)
Specific
Sumatriptan Topical (Zecuity)
General
amine
serotonin agonist (5-HT receptor agonist, triptan)
sulfonamide
Properties
SIZE: MW = 295.4 G/M
MISC-INFO: elimination route KIDNEY
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional
Drug Formulary, 1998 (removed 3/2000)
- Prescriber's Letter 9(2):2 2002
- Prescriber's Letter 10(3):14-15 2003
- Features of Available Triptans
Prescriber's Letter 11(2):10 2004
Detail-Document#: 200206
(subscription needed) http://www.prescribersletter.com
- Prescriber's Letter 17(1): 2010
Comparison of Available Triptans
Detail-Document#: 260103
(subscription needed) http://www.prescribersletter.com
- Deprecated Reference
- Hansen JM et al.
Reduced efficacy of sumatriptan in migraine with aura vs
without aura.
Neurology 2015 May 5; 84:1880
PMID: 25841032
http://www.neurology.org/content/84/18/1880
Component-of
naproxen/sumatriptan (Treximet)