Nimodipine

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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	C08 CA06
PubChem	4497
DrugBank	APRD00612
Chemical data
Formula	C₂₁H₂₆N₂O₇
Mol. weight	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.

1 Dosage
2 Usage
3 Mode of action
4 Contraindications & side-effects
5 References
6 External links

[edit] Dosage

The regular dosage is 60 mg tablets four hourly. If the patient is unable to take tablets orally, it is 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).

[edit] 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 (Allen et al 1983, Janjua & Mayer 2003).

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

There is some indication that nimodipine, either alone or in conjunction with carbamazepine, may be an effective therapy for sufferers of ultradian and rapid-cycling bipolar disorder. (Pazzaglia et al 1993, Pazzaglia et al 1998).

[edit] 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.

[edit] 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 recent than one month.

[edit] References

Allen GS, Ahn HS, Preziosi TJ, Battye R, Boone SC, Boone SC, Chou SN, Kelly DL, Weir BK, Crabbe RA, Lavik PJ, Rosenbloom SB, Dorsey FC, Ingram CR, Mellits DE, Bertsch LA, Boisvert DP, Hundley MB, Johnson RK, Strom JA, Transou CR. Cerebral arterial spasm--a controlled trial of nimodipine in patients with subarachnoid hemorrhage. N Engl J Med 1983;308:619-24. PMID 6338383.
Belfort MA, Anthony J, Saade GR, Allen JC Jr; Nimodipine Study Group. A comparison of magnesium sulfate and nimodipine for the prevention of eclampsia. N Engl J Med 2003;348:304-11. PMID 12540643.
Janjua N, Mayer SA. Cerebral vasospasm after subarachnoid hemorrhage. Curr Opin Crit Care 2003;9:113-9. PMID 12657973.
Rang HP, Dale MM, Ritter JM, Moore PK. (2003) Pharmacology 5th edition. London, Churchill Livingstone.
Pazzaglia PJ, Post RM, Ketter TA, George MS, Marangell LB. Preliminary controlled trial of nimodipine in ultra-rapid cycling affective dysregulation. Psychiatry Res. 1993 Dec;49(3):257-72. PMID 8177920.
Pazzaglia PJ, Post RM, Ketter TA, Callahan AM, Marangell LB, Frye MA, George MS, Kimbrell TA, Leverich GS, Cora-Locatelli G, Luckenbaugh D. Nimodipine monotherapy and carbamazepine augmentation in patients with refractory recurrent affective illness. J Clin Psychopharmacol. 1998 Oct;18(5):404-13. PMID 9790159.

[edit] External links

Nimotop (manufacturer's website)
Nimodipine (patient information)

Calcium channel blockers (C08) edit
Dihydropyridines:	Amlodipine, Felodipine, Isradipine, Lacidipine, Lercanidipine, Nicardipine, Nifedipine, Nimodipine, Nisoldipine
Phenylalkylamines:	Verapamil
Benzothiazepines:	Diltiazem