nisoldipine


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nisoldipine

 [ni-sol´dĭ-pēn]
a calcium channel blocking agent used in the treatment of hypertension; administered orally.

nisoldipine

Sular, Syscor (UK)

Action

Suppresses calcium transport into vascular smooth muscle cells. This suppression inhibits vasoconstriction and dilates coronary arteries, improving myocardial oxygen uptake.

Availability

Tablets (extended-release): 8.5 mg, 17 mg, 22.5 mg, 34 mg

Indications and dosages

Hypertension

Adults: Initially, 17 mg P.O. daily; may increase by 8.5 mg per week or longer intervals to attain adequate blood pressure control. Usual maintenance dosage is 17 to 34 mg daily.

Contraindications

• Hypersensitivity to drug or dihydropyridine calcium channel blockers

Precautions

Use cautiously in:

• heart failure and left ventricular dysfunction, hepatic impairment, renal disease, coronary artery disease, hypotension

• concurrent phenytoin use

• elderly patients

• pregnant or breastfeeding patients

• children (safety not established).

Administration

• Give with meals, but not with high-fat meals, grapefruit, or grapefruit juice.

• Don't crush or break extended-release tablets. Make sure patient swallows them whole.

• Know that drug may be given alone or with other antihypertensives.

Adverse reactions

CNS: headache, dizziness

CV: peripheral edema, chest pain, vasodilation, hypotension, palpitations

EENT: pharyngitis, sinusitis

GI: nausea

Skin: rash

Interactions

Drug-drug. Cimetidine: increased nisoldipine blood level

Phenytoin, other CYP3A4 inducers: decreased nisoldipine blood level and efficacy

Drug-food. Grapefruit juice: significantly increased drug blood level and effects

High-fat meal: decreased drug blood level

Drug-herbs. Ephedra (ma huang), yohimbine: antagonism of nimodipine effects

St. John's wort: decreased nimodipine blood level

Drug-behaviors. Alcohol use: increased hypotensive effects

Patient monitoring

• Check vital signs and ECG.

• Monitor fluid intake and output. Watch for peripheral edema.

Patient teaching

• Tell patient to swallow extended-release tablets whole and not to crush or break them.

• Advise patient to take with food, but not high-fat food. Recommend small, frequent meals.

• Instruct patient to avoid high-fat meals, alcohol, grapefruit, and grapefruit juice.

• Tell patient to immediately report irregular heart beat, shortness of breath, swelling, pronounced dizziness, rash, or chest pain.

• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, foods, herbs, and behaviors mentioned above.

nisoldipine

A CALCIUM CHANNEL BLOCKER drug used to treat angina pectoris and high blood pressure (HYPERTENSION). A brand name is Syscor MR.
References in periodicals archive ?
Ganga, "Development of discriminating dissolution method for an insoluble drug: nisoldipine," International Journal of PharmTech Research, vol.
CA nisoldipine, nimodipine, nitrendipine, nifedipine, and nicardipine have AOA that correlates with their lipophilicity (modified Buege and Aust's method of TBA determination, applied in model of rat brain cortex ischemia/reperfusion) [87].
Relationship between time after intake of grapefruit juice and the effect on the pharmacokinetics and pharmacodynamics of nisoldipine in healthy subjects.
Type 2 Diarrhea Depression Diabetes Malaria Codeine Citalopram Repaglinide Atovaquone Phosphate Diphenoxylate Duloxetine Acarbose Sulfadoxine Steroid Budesonide Serotonin Metformin Pyrimethamine Reuptake Inhibitors Loperamide Repaglinide Artemether & Lumefantrine Metformin Amodiaquine Proguanil Malaron Atovaquone & Proguanil Diarrhea Diabetes Asthma Hypertension Codeine Glyburide Beclomethasone Propranolol Phosphate Dipropionate Diphenoxylate Intensive Ipratropium Angiotensin insulin Bromide Steroid Budesonide Enalapril Aminophylline Chlorthalidone Loperamide Insulin Isoprenaline Nisoldipine Repaglinide Salbutamol Hyperglycemia Angiotensin Hyperglycemia & Insulin [FIGURE 3 OMITTED]
The ABCD trial showed higher incidence of myocardial infarction in the nisoldipine arm compared with the ACE inhibitor22.
The effect of nisoldipine as compared with enalapril on cardiovascular outcomes in patients with noninsulin-dependent diabetes and hypertension.
* Blood pressure medications known as calcium channel blockers, including felodipine (Plendil), nifedipine (Adalat, Procardia), nimodipine (Nimotop) and nisoldipine (Sular)
Mylan said it's shipping its Nisoldipine ER, the first generic version of Sular in the U.S., immediately.
The effect of nisoldipine as compared with enalapril on cardiovascular outcomes in patients with non-insulin-dependent diabetes and hypertension.
Relationship between time after intake of grapefruit juice and the effect of pharmacokinetics and pharmacodynamics on nisoldipine in healthy subjects.
The following drugs have been found to interact with grapefruit juice (to be sure of your medications, ask your pharmacist): calcium channel blockers (for high blood pressure)--felodipine (Plendil), nifedipine (Procardia, Adalat), nisoldipine (Sular); immunosuppressant drugs (for organ transplants)--cyclosporine (Neoral, Sandimmune, SangCya), tacrolimus (Prograf); drugs for anxiety, insomnia or depression--diazepam (Valium), triazolam (Halcion), zaleplon (Sonata), carbamazepine (Tegretol), clomipramine (Anafranil).
The extended-release formulation of calcium channel blocker nisoldipine may be particularly effective for hypertensive African Americans, who tend to have high blood pressure levels throughout the night.