Inhouse product
Indications
For the improvement of
neurological outcome by reducing the incidence and severity of ischemic
deficits in patients with subarachnoid hemorrhage from ruptured intracranial
berry aneurysms regardless of their post ictus neurological condition.
* রেজিস্টার্ড চিকিৎসকের পরামর্শ মোতাবেক ঔষধ সেবন করুন'
Pharmacology
Nimodipine is a
calcium channel blocker. The contractile processes of smooth muscle cells are
dependent upon calcium ions, which enter these cells during depolarization as
slow ionic transmembrane currents. Nimodipine inhibits calcium ion transfer
into these cells and thus inhibits contractions of vascular smooth muscle.
Nimodipine had a greater effect on cerebral arteries than on arteries elsewhere
in the body, perhaps because it is highly lipophilic, allowing it to cross the
blood-brain barrier; concentrations of Nimodipine as high as 12.5 ng/mL have
been detected in the cerebrospinal fluid of Nimodipine-treated subarachnoid
hemorrhage (SAH) patients. The precise mechanism of action of Nimodipine in SAH
in humans is unknown. Clinical studies demonstrates a favorable effect of
Nimodipine on the severity of neurological deficits caused by cerebral
vasospasm following SAH, there is no arteriographic evidence that the drug
either prevents or relieves the spasm of these arteries.
Nimodipine is rapidly absorbed after oral administration, and peak
concentrations are generally attained within one hour. The terminal elimination
half-life is approximately 8 to 9 hours but earlier elimination rates are much
more rapid, equivalent to a half-life of 1-2 hours; a consequence is the need
for frequent (every 4 hours) dosing. Nimodipine is over 95% bound to plasma
proteins. Nimodipine is eliminated almost exclusively in the form of
metabolites and less than 1% is recovered in the urine as unchanged drug.
Because of a high first-pass metabolism, the bioavailability of Nimodipine
averages 13% after oral administration. The bioavailability is significantly
increased in patients with hepatic cirrhosis, with Cmax approximately double
that in normals which necessitates lowering the dose in this group of patients.
Dosage & Administration
Adult: Initial dose is 60 mg in every four
hours interval for 21 consecutive days, preferably not less than one hour
before or two hours after meals. Oral Nimodipine therapy should be commence
within 96 hours of the subarachnoid hemorrhage.
Use in Pediatric Patients: While there is no specific information
on use of this medication in pediatric patients.
* রেজিস্টার্ড চিকিৎসকের পরামর্শ মোতাবেক ঔষধ সেবন করুন'
Interaction
Plasma concentration
and efficacy may be significantly reduced when administered with strong CYP3A4
inducers (e.g. rifampicin, carbamazepine, phenobarbital, phenytoin). May
increase serum levels and toxicity of phenytoin. Increased plasma concentrations
with cimetidine or sodium valproate.
Contraindications
Use within 1 mth of MI
or an episode of unstable angina. Concomitant use with potent CYP3A4 inhibitors
(e.g. clarithromycin, ritonavir, ketoconazole, nefazodone).
Side Effects
Although side effects
from Nimocal are not common, the following can occur: headache, dizziness,
flushing (feeling of warmth), heartburn, fast heartbeat, slow heartbeat, upset
stomach, stomach pain, constipation, depression etc.
Pregnancy & Lactation
Large doses of nimodipine
have been shown to cause birth defects in animals. Human studies have not been
done. Before you take nimodipine, tell your doctor if you are pregnant or plan
to become pregnant. Nimodipine may pass into breast milk but has not been
reported to cause problems; caution is advised. Consult your doctor for advice.
Precautions & Warnings
Blood pressure: Nimocal has the hemodynamic effects expected
of a calcium channel blocker, although they are generally not marked. Blood
pressure should be carefully monitored during treatment with Nimocal based on
its known pharmacology and the known effects of calcium channel blockers.
Hepatic disease: The metabolism of Nimocal is decreased in
patients with impaired hepatic function. Such patients should have their blood
pressure and pulse rate monitored closely and should be given a lower dose.
Therapeutic Class
Calcium-channel
blockers
Storage Conditions
Store between 15-30°
C. Protect from light.
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