Nimodipine
Drug Info:
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Nimodipine
Brand names: Nimotop®
Chemical formula:
- Espa�ol:
- Nimodipina, Cápsula oral
Nimodipine Oral capsule
What is this medicine?
NIMODIPINE (nye MOE di peen) is a calcium-channel blocker. This medicine is used to treat subarachnoid hemorrhage. This is a condition in which there is bleeding into the space around the brain that causes severe headaches and stiff neck.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•liver disease
•an unusual or allergic reaction to nimodipine, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. It is best to take this medicine at least one hour before or two hours after meals. Take your doses at regular intervals. Do not take your medicine more often than directed. Continue to take your medicine even if you feel better. Do not stop taking except on the advice of your doctor or health care professional.
Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What may interact with this medicine?
•cimetidine
•grapefruit juice
•medicines for high blood pressure
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Visit your doctor or health care professional for regular checks on your progress.
Alcohol can increase the chance of getting low blood pressure. Avoid alcoholic drinks while you are taking this medicine.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•difficulty breathing
•dizziness or drowsiness
•irregular or fast heartbeats (palpitations)
•lightheadedness or fainting
•slow heartbeat
•swelling of the legs or ankles
•unusual bleeding or bruising, red spots on skin
•unusually weak or tired
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•flushing
•headache
•nausea
•sweating
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
Keep out of reach of children.
Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Do not freeze. Protect from light. Keep foil packaged capsules in their original foil until needed. Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
Oxford A-Z of Medicinal Drugs:
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nimodipine
A class II calcium antagonist that relaxes the cerebral arteries, which supply blood to the brain. It is used to prevent spasm of these arteries following a subarachnoid haemorrhage (bleeding into the spaces around the brain caused by a rupture of one of the cerebral arteries), and thus prevents further interruption of the blood supply to the brain. Nimodipine is available, as tablets or a solution for infusion, on prescription only.
Side effects:
include low blood pressure, flushing, headache, and gastrointestinal upset (including nausea).
Precautions:
nimodipine should not be taken by people with unstable angina or within one month of a heart attack. It should be used with caution in patients with swelling of the brain, raised pressure within the brain, or poor kidney function. See also calcium antagonists.
Interactions with other drugs:
Rifampicin reduces the plasma concentration of nimedipine.
See also calcium antagonists.
Proprietary preparation:
Nimotop.
| nilotinib, nifedipine, nicotinic acid | |
| nitisinone, nitrates, nitrazepam |
Wikipedia on Answers.com:
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Nimodipine
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|
|---|---|
| Systematic (IUPAC) name | |
| 3-(2-methoxyethyl) 5-propan-2-yl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate | |
| Clinical data | |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a689010 |
| Pregnancy cat. | C: (USA) |
| Legal status | ? |
| Routes | Intravenous, Oral |
| Pharmacokinetic data | |
| Bioavailability | 100% (Intravenous) 13% (Oral) |
| Protein binding | 95% |
| Metabolism | Hepatic |
| Half-life | 8–9 hours |
| Excretion | Feces and Urine |
| Identifiers | |
| CAS number | 66085-59-4  |
| ATC code | C08CA06 |
| PubChem | CID 4497 |
| IUPHAR ligand | 2523 |
| DrugBank | DB00393 |
| ChemSpider | 4341 |
| UNII | 57WA9QZ5WH |
| KEGG | D00438 |
| ChEMBL | CHEMBL1428 |
| Chemical data | |
| Formula | C21H26N2O7 |
| Mol. mass | 418.44 g/mol |
| SMILES | eMolecules & PubChem |
|
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| Physical data | |
| Melt. point | 7 °C (45 °F) |
 (what is this?) (verify) |
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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.
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Contents
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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), specifically from ruptured intracranial berry aneurysms irrespective of the patient's post-ictus neurological condition.[2] 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.[1][3]
A 2003 trial (Belfort et al.) found nimodipine was inferior to magnesium sulfate in preventing seizures in women with severe preeclampsia.[4]
While nimodipine is not used in head injury currently, it has shown promise in clinical studies. A 2009 study found that patients with severe head trauma who were given nimodipine, via peripheral vein injection, along with the standard procedures had significantly higher cerebral perfusion pressure and jugular venous oxygen saturation, while intracranial pressure, jugular lactate and jugular glucose were lower. The study concluded that Glasgow outcome score values were higher, and that the cerebral metabolism was improved.[5]
Pharmacokinetics
Absorption
In humans, it is administered primarily orally and reaches peak plasma concentrations within one and a half hours. Patients taking enzyme-inducing anticonvulsants have lower plasma concentrations, while patients taking sodium valproate were markedly higher.[6]
Metabolism
Nimodipine is metabolized in the first pass metabolism. The dihydropyridine ring of the nimodipine is dehydrogenated in the hepatic cells of the liver, a process governed by Cytochrome P-4503A (CYP3A). This can be completely inhibited however, by troleandomycin (an antibiotic) or ketoconazole (an antifungal drug).[7]
Excretion
Studies in non-human mammals using radioactive labeling have found that 40-50% of the dose is excreted via urine. The residue level in the body was never more than 1.5% in monkeys. There were some metabolites of the drug found in the milk of lactating rat subjects.[8]
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.[9]
Contraindications
Nimodipine is associated with low blood pressure, flushing and sweating, edema, nausea and other gastrointestinal problems, most of which are known characteristics of calcium channel blockers. 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.[10]
Side-effects
The FDA has classified the side effects into groups based on dosages levels at q4h. For the high dosage group (90 mg) less than 1% of the group experienced adverse conditions including itching, gastrointestinal hemorrhage, thrombocytopenia, neurological deterioration, vomiting, diaphoresis, congestive heart failure, hyponatremia, decreasing platelet count, disseminated intravascular coagulation, deep vein thrombosis.[2]
References
- ^ a b Janjua N, Mayer SA (2003). "Cerebral vasospasm after subarachnoid hemorrhage". Current opinion in critical care 9 (2): 113–9. doi:10.1097/00075198-200304000-00006. PMID 12657973.
- ^ a b "FDA approved Labeling text. NIMOTOP (nimodipine) CAPSULES For Oral Use" (PDF). Food and Drug Administration. 12/2005. http://www.accessdata.fda.gov/drugsatfda_docs/label/2006/018869s014lbl.pdf. Retrieved 2009-07-21.
- ^ 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. doi:10.1056/NEJM198303173081103. PMID 6338383.
- ^ 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.
- ^ Aslan A, Gurelik M, Cemek M, Goksel HM, Buyukokuroglu ME (February 2009). "Nimodipine can improve cerebral metabolism and outcome in patients with severe head trauma". Pharmacol. Res. 59 (2): 120–4. doi:10.1016/j.phrs.2008.10.003. PMID 18996202.
- ^ http://www.pubmedcentral.nih.gov/picrender.fcgi?artid=1368527&blobtype=pdf
- ^ http://www.chinaphar.com/1671-4083/21/690.pdf
- ^ http://www.ionchannels.org/showabstract.php?pmid=4096729
- ^ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.
- ^ "Information for Healthcare Professionals: Nimodipine (marketed as Nimotop)". Postmarket Drug Safety Information for Patients and Providers. Food and Drug Administration. http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm129297.htm. Retrieved 2009-07-21.
External links
- Nimotop (manufacturer's website)
- Nimodipine (patient information)
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Oxford A-Z of Medicinal Drugs
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