Periplum
Periplum - General Information
A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure. [PubChem]
Pharmacology of Periplum
Periplum belongs to the class of pharmacological agents known as calcium channel blockers. Periplum is indicated for the improvement of neurological outcome by reducing the incidence and severity of ischemic deficits in patients with subarachnoid hemorrhage from ruptured congenital aneurysms who are in good neurological condition post-ictus (e.g., Hunt and Hess Grades I-III). The contractile processes of smooth muscle cells are dependent upon calcium ions, which enter these cells during depolarization as slow ionic transmembrane currents. Periplum inhibits calcium ion transfer into these cells and thus inhibits contractions of vascular smooth muscle. In animal experiments, 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.
Periplum for patients
Periplum Interactions
It is possible that the cardiovascular action of other calcium channel blockers could be enhanced by the addition of NimotopÒ.
In Europe, NimotopÒ was observed to occasionally intensify the effect of antihypertensive compounds taken concomitantly by patients suffering from hypertension; this phenomenon was not observed in North American clinical trials.
A study in eight healthy volunteers has shown a 50% increase in mean peak nimodipine plasma concentrations and a 90% increase in mean area under the curve, after a one week course of cimetidine at 1,000 mg/day and nimodipine at 90 mg/day. This effect may be mediated by the known inhibition of hepatic cytochrome P- 450 by cimetidine, which could decrease first pass metabolism of nimodipine.
Periplum Contraindications
None known.
Additional information about Periplum
Periplum Indication: For the treatment of subarachnoid bleeding.
Mechanism Of Action: Although the precise mechanism of action is not known, nimodipine blocks intracellular influx of calcium that is thought to be a central to ischaemic neuronal damage. Periplum binds specifically to L-type voltage-gated calcium channels.
Drug Interactions: Cimetidine Cimetidine increases the effect of the calcium channel blocker
Divalproex sodium Valproic acid increases the effect of nimodipine
Valproic Acid Valproic acid increases the effect of nimodipine
Quinupristin This combination presents an increased risk of toxicity
Food Interactions: Not Available
Generic Name: Nimodipine
Synonyms: Nimodipino [Inn-Spanish]; Nimodipinum [Inn-Latin]
Drug Category: Antihypertensive Agents; Vasodilator Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Nimodipine: Nimotop; Periplum;
Absorption: Bioavailability is 100% following intravenous administration and 13% following oral administration.
Toxicity (Overdose): Symptoms of overdosage would be expected to be related to cardiovascular effects such as excessive peripheral vasodilation with marked systemic hypotension.
Protein Binding: 95%
Biotransformation: Hepatic.
Half Life: 8-9 hours
Dosage Forms of Periplum: Capsule Oral
Chemical IUPAC Name: O5-(2-methoxyethyl) O3-propan-2-yl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Chemical Formula: C21H26N2O7
Nimodipine on Wikipedia: https://en.wikipedia.org/wiki/Nimodipine
Organisms Affected: Humans and other mammals