      Document 0108
 DOCN  DRG0108
 UNIQUE IDENTIFIER        DRG-0139
 NAME OF SUBSTANCE        Nimodipine [USAN 1996]
 REGISTRY NUMBER          66085-59-4
 STANDARD CHEMICAL NAME   Isopropyl(2-methoxyethyl)1,4-dihydro
                          -2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridine--
                          dicarboxylate [PDR 1995]
 SYNONYMS                 Nimotop [PDR 1995]
 SYNONYMS                 Bay e 9736 [USAN 1996]
 SYNONYMS                 Periplum [Merck Index 1989]
 PROTOCOL ID NUMBERS      NIAID ACTG 162
 SECONDARY SOURCE ID      DRG
 PHARMACOLOGICAL ACTION   A calcium channel blocker with preferential
                          cerebrovascular activity. Nimodipine has
                          marked cerebrovascular dilating effects and
                          lowers blood pressure. The drug inhibits
                          calcium ion transfer into smooth muscle cells
                          and thus inhibits contractions of vascular
                          smooth muscle. Nimodipine is rapidly absorbed
                          after oral administration, and peak
                          concentrations are generally attained within
                          1 hour. It is over 95 percent bound to plasma
                          proteins. The terminal elimination half-life
                          is 8-9 hours, but earlier elimination rates
                          are much more rapid, equivalent to 1-2 hours.
                          Nimodipine is eliminated almost exclusively
                          in the form of metabolites, and less than one
                          percent is recovered in the urine as
                          unchanged drug. The metabolism of nimodipine
                          is decreased in patients with impaired
                          hepatic function. [PDR 1993] [MeSH]
 DISEASES STUDIED/TREATED Under investigation for the treatment of AIDS
                          dementia complex [AmFAR Tx Dir 1995;7(4)]
 CLASSIFICATION CODE      Calcium Channel Blocker [PDR 1995]
 CLASSIFICATION CODE      Vasodilator [USAN 1996]
 OTHER MAJOR USES         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 (eg. Hunt
                          and Hess Grades, I-III) [PDR 1995]
 SUBSTANCE INTERACTIONS   Possibly enhances the cardiovascular action
                          of other calcium channel blockers. In
                          European trials, nimodipine occasionally
                          intensified the effect of antihypertensive
                          compounds taken concomitantly by patients
                          with hypertension. [PDR 1995]
 ADVERSE EFFECTS          The most frequently reported adverse effects
                          include decreased blood pressure, edema, and
                          headache. [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: A 1,4-dihydropyridine
                          structurally related to nifedipine [AHFS Drug
                          Information 1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C21H26N2O7 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 418.45 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Practically insoluble in water,
                          soluble in glycerin and PEG 400 [AHFS Drug
                          Information 1995]
 CHEMICAL/PHYSICAL DATA   ELEMENTAL COMPOSITION: C60.28% H6.26% N6.69%
                          O26.76% [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   MELTING POINT: 125 C [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: Yellow crystalline
                          substance [PDR 1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: 30 mg capsules. [PDR 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral. [PDR 1995]
 SUBSTANCE DELIVERY DATA  STORAGE: Store between 15 and 30 C (59 and 86
                          F). Protect from light and freezing. [PDR
                          1995]
 MANUFACTURERS            Miles Incorporated Pharmaceutical Division
 REFERENCES               Galgani S, Narciso P, Balestra P, Pigorini F,
                          Pau F, Sette P, Tozzi V, Alba L, Grisetti S,
                          Visco G. Nimodipine+ZDV vs ZDV in patients
                          with ADC. Int Conf AIDS. 1994 Aug
                          7-12;10(1):205 (abstract no. PBO248).
 REFERENCES               Grobe-Einsler R. Clinical aspects of
                          nimodipine. Clin Neuropharmacol. 1993; 16
                          Suppl 1:S39-45.
 REFERENCES               Gallo JM, Swagler AR, Mehta M, Qian M.
                          Pharmacokinetic evaluation of drug
                          interactions with anti-human immunodeficiency
                          virus drugs. VI. Effects of the calcium
                          channel blocker nimodipine on zidovudine
                          kinetics in monkeys. J Pharmacol Exp Ther
                          1993 Jan;264(1):315-20.
 REFERENCES               Lipton SA. Calcium channel antagonists and
                          human immunodeficiency virus coat
                          protein-mediated neuronal injury. Ann Neurol.
                          1991 Jul;30(1):110-4.
 ENTRY MONTH              9203
 LAST REVISION DATE       951213
 

SOURCE: National Library of Medicine, Bethesda, MD.  Distributed by AEGIS.
