Nisoldipine

Nisoldipine is a pharmaceutical drug used for the treatment of chronic angina pectoris and hypertension. It is a calcium channel blocker of the dihydropyridine class. It is sold in the United States under the proprietary name Sular. Nisoldipine has tropism for cardiac blood vessels.[1]

Nisoldipine
Clinical data
Trade namesSular, Baymycard, Syscor
AHFS/Drugs.comMonograph
MedlinePlusa696009
Pregnancy
category
  • US: C (Risk not ruled out)
    Routes of
    administration    		Oral
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Bioavailability4–8%
    Protein binding>99%
    MetabolismCYP3A4
    Elimination half-life7–12 hours
    Excretion70–80% via urine
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard100.058.534
    Chemical and physical data
    FormulaC20H24N2O6
    Molar mass388.414 g·mol−1
    3D model (JSmol)
     NY (what is this?)  (verify)

    It was patented in 1975 and approved for medical use in 1990.[2]

    Contraindications

    Nisoldipine is contraindicated in people with cardiogenic shock, unstable angina, myocardial infarction, and during pregnancy and lactation.[3]

    Adverse effects

    Common side effects are headache, confusion, fast heartbeat, and edema. Hypersensitivity reactions are rare and include angioedema.[3]

    Interactions

    The substance is metabolized by the liver enzyme CYP3A4. Consequently, CYP3A4 inducers such as rifampicin or carbamazepine could reduce the effectiveness of nisoldipine, while CYP3A4 inhibitors such as ketoconazole increase the amount of nisoldipine in the body more than 20-fold. Grapefruit juice also increases nisoldipine concentrations by inhibiting CYP3A4.[3]

    Pharmacology

    Mechanism of action
    Further information: Calcium channel blocker § Mechanism of action

    Nisoldipine is a calcium channel blocker that selectively inhibits L-type calcium channels.[3]

    gollark: I mean, insects are waaay more effective at that than us.
    gollark: It doesn't have a "purpose".
    gollark: If you do actually *have* goals beyond "maximum amount of humans", and even if your goal is "maximum amount of humans in the long term" I guess, they're NOT best served by just having the maximum amount of children NOW.
    gollark: Some species, like ours, do better by having smaller amounts of children and taking care of each one better.
    gollark: I mean, in some cases having maximum amount of children isn't actually advantageous.

    References
    1. Knorr, Andreas M. (1995). "Why is nisoldipine a specific agent in ischemic left ventricular dysfunction?". The American Journal of Cardiology. 75 (13): E36–E40. doi:10.1016/S0002-9149(99)80446-9.
    2. Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 464. ISBN 9783527607495.
    3. Haberfeld, H, ed. (2019). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag. Syscor 5 mg-Filmtabletten.
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