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Nimodipine



Nimodipine
Systematic (IUPAC) name
2-methoxyethyl1-methylethyl2,6-dimethyl-4-(3-nitrophenyl) -1,4-dihydropyridine-3,5- dicarboxylate
Identifiers
CAS number 66085-59-4
ATC code C08CA06
PubChem 4497
DrugBank APRD00612
Chemical data
Formula C21H26N2O7 
Mol. mass 418.44 g/mol
Physical data
Melt. point 7 °C (45 °F)
Pharmacokinetic data
Bioavailability 100% (Intravenous) 13% (Oral)
Protein binding 95%
Metabolism Hepatic
Half life 8-9 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

C: (USA)

Legal status
Routes Intravenous, Oral

Nimodipine (marketed by Bayer as Nimotop®) is a dihydropyridine calcium channel blocker originally developed for the treatment of 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.

Additional recommended knowledge

Contents

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),[1] 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 vasospasm and resultant ischemia, a complication of subarachnoid hemorrhage (a form of 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.[2][1]

A 2003 trial (Belfort et al) found nimodipine was inferior to magnesium sulfate in preventing seizures in women with severe preeclampsia.[3]

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.[4]

Contraindications & side-effects

Nimodipine is associated with low blood pressure, flushing and sweating, edema, nausea and other gastrointestinal problems. It is 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.[5]

References

  1. ^ a b Janjua N, Mayer SA (2003). "Cerebral vasospasm after subarachnoid hemorrhage". Current opinion in critical care 9 (2): 113–9. PMID 12657973.
  2. ^ Allen GS, Ahn HS, Preziosi TJ, et al (1983). "Cerebral arterial spasm--a controlled trial of nimodipine in patients with subarachnoid hemorrhage". N. Engl. J. Med. 308 (11): 619–24. PMID 6338383.
  3. ^ Belfort MA, Anthony J, Saade GR, Allen JC (2003). "A comparison of magnesium sulfate and nimodipine for the prevention of eclampsia". N. Engl. J. Med. 348 (4): 304–11. doi:10.1056/NEJMoa021180. PMID 12540643.
  4. ^ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-44307-145-4. 
  5. ^ Information for Healthcare Professionals: Nimodipine (marketed as Nimotop). Retrieved on 2007-10-10.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Nimodipine". A list of authors is available in Wikipedia.
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