Nimodipine
1269912
214420344
2008-05-23T13:58:25Z
DOI bot
6652755
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{{drugbox
| IUPAC_name = 2-methoxyethyl1-methylethyl2,6-dimethyl-4-(3-nitrophenyl) -1,4-dihydropyridine-3,5- dicarboxylate
| image = Nimodipine.png
| image2 = Nimodipine.gif
| width = 194
| CAS_number = 66085-59-4
| ATC_prefix = C08
| ATC_suffix = CA06
| ATC_supplemental =
| PubChem = 4497
| DrugBank = APRD00612
| C=21 | H=26 | N=2 | O=7
| molecular_weight = 418.44 g/mol
| smiles =
| melting_point = 7
| bioavailability = 100% (Intravenous) 13% (Oral)
| protein_bound = 95%
| metabolism = Hepatic
| elimination_half-life = 8-9 hours
| pregnancy_category = C: (USA)
| legal_status =
| routes_of_administration = Intravenous, Oral }}
<!-- FAIR USE of Nimodipine.gif: see image description page at http://en.wikipedia.org/wiki/Image:Nimodipine.gif for rationale -->
'''Nimodipine''' (marketed by [[Bayer]] as '''Nimotop''') is a [[dihydropyridine]] [[calcium channel blocker]] originally developed for the treatment of [[arterial hypertension|high blood pressure]]. It is not frequently used for this indication, but has shown good results in preventing a major complication of [[subarachnoid hemorrhage]] (a form of [[cerebral hemorrhage]]) termed [[vasospasm]]; this is now the main use of nimodipine.
==Dosage==
The regular dosage is 60 mg tablets every four hours. If the patient is unable to take tablets orally, it was previously given via [[intravenous infusion]] at a rate of 1-2 mg/hour (lower dosage if the body weight is <70 kg or blood pressure is too low),<ref name=Janjua>{{cite journal |author=Janjua N, Mayer SA |title=Cerebral vasospasm after subarachnoid hemorrhage |journal=Current opinion in critical care |volume=9 |issue=2 |pages=113–9 |year=2003 |pmid=12657973 |doi=10.1097/00075198-200304000-00006}}</ref> but since the withdrawal of the IV preparation, administration by [[nasogastric tube]] is an alternative.
==Usage==
Because it has some selectivity for cerebral vasculature, nimodipine's main use is in the prevention of [[cerebral cortex|cerebral]] [[vasospasm]] and resultant [[ischemia]], a complication of [[subarachnoid hemorrhage]] (a form of [[cerebral hemorrhage|cerebral bleed]]). Its administration begins within 4 days of a subarachnoid hemorrhage and is continued for three weeks. If [[blood pressure]] drops by over 5%, dosage is adjusted. There is still controversy regarding the use of intravenous nimodipine on a routine basis.<ref>{{cite journal |author=Allen GS, Ahn HS, Preziosi TJ, ''et al'' |title=Cerebral arterial spasm--a controlled trial of nimodipine in patients with subarachnoid hemorrhage |journal=N. Engl. J. Med. |volume=308 |issue=11 |pages=619–24 |year=1983 |pmid=6338383 |doi=}}</ref><ref name=Janjua/>
A 2003 trial (Belfort ''et al'') found nimodipine was inferior to [[magnesium sulfate]] in preventing seizures in women with severe [[preeclampsia]].<ref>{{cite journal |author=Belfort MA, Anthony J, Saade GR, Allen JC |title=A comparison of magnesium sulfate and nimodipine for the prevention of eclampsia |journal=N. Engl. J. Med. |volume=348 |issue=4 |pages=304–11 |year=2003 |pmid=12540643 |doi=10.1056/NEJMoa021180}}</ref>
==Mode of action==
Nimodipine binds specifically to L-type voltage-gated calcium channels. There are numerous theories about its mechanism in preventing vasospasm, but none are conclusive.<ref name=Rang>{{cite book |author=Rang, H. P. |title=Pharmacology |publisher=Churchill Livingstone |location=Edinburgh |year=2003 |pages= |isbn=0-44307-145-4 |oclc= |doi=}}</ref>
==Contraindications & side-effects==
Nimodipine is associated with [[hypotension|low blood pressure]], flushing and sweating, edema, nausea and other gastrointestinal problems. It is [[contraindication|contraindicated]] in [[unstable angina]] or an episode of [[myocardial infarction]] more recently than one month.
While nimodipine was occasionally administered intravenously in the past, the FDA released an alert in January 2006 warning that it had received reports of the approved oral preparation being used intravenously, leading to severe complications; this was despite warnings on the box that this should not be done.<ref>{{cite web |url=http://www.fda.gov/CDER/drug/InfoSheets/HCP/nimodipineHCP.htm |title=Information for Healthcare Professionals: Nimodipine (marketed as Nimotop) |accessdate=2007-10-10 |format= |work=}}</ref>
==References==
<references/>
== External links ==
* [http://www.univgraph.com/bayer/inserts/nimotop.pdf Nimotop] (manufacturer's website)
* [http://www.meds-help.com/nimodipine/ Nimodipine] (patient information)
{{Calcium channel blockers}}
[[Category:Calcium channel blockers]]
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