isradipine


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Related to isradipine: Calcium channel blockers

isradipine

 [is-rad´ĭ-pēn]
a calcium channel blocking agent used alone or with a thiazide diuretic for the treatment of hypertension.

isradipine

DynaCirc CR, Prescal (UK)

Pharmacologic class: Calcium channel blocker

Therapeutic class: Antihypertensive

Pregnancy risk category C

Action

Inhibits calcium ion movement across cell membranes of cardiac and arterial muscles, relaxing coronary and peripheral vascular smooth muscle. This action reduces diastolic blood pressure, enhances left ventricular function, and improves ejection rates; it also reduces mean vascular and systemic vascular resistance, increasing cardiac output and improving stroke volume.

Availability

Capsules: 2.5 mg, 5 mg

Tablets (controlled-release): 5 mg, 10 mg

Indications and dosages

Hypertension

Adults: Initially, 2.5 mg P.O. b.i.d. as monotherapy or combined with a thiazide diuretic (regular-release capsules); may increase in increments of 5 mg/day at 2- to 4-week intervals, to a maximum of 20 mg/day. Or, 5 to 10 mg P.O. (controlled-release) daily as monotherapy or combined with a thiazide diuretic.

Contraindications

• Hypersensitivity to drug or other calcium channel blockers

Precautions

Use cautiously in:

• heart disease, hypotension, hepatic or renal disease, GI hypermotility or obstruction (controlled-release form)

• concurrent use of beta-adrenergic blockers

• elderly patients

• pregnant or breastfeeding patients

• children.

Administration

• Give with or without food.

• Don't give with grapefruit juice.

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

Adverse reactions

CNS: dizziness, headache, fatigue, syncope, sleep disturbances

CV: peripheral edema, tachycardia, hypotension, chest pain, arrhythmias

GI: nausea, vomiting, constipation, abdominal pain or distention, dry mouth

GU: nocturia, urinary frequency

Hematologic: leukopenia

Hepatic: hepatitis

Skin: rash, pruritus, urticaria

Other: flushing

Interactions

Drug-drug. Atracurium, gallamine, pancuronium, tubocurarine, vecuronium: increased respiratory depression

Beta-adrenergic blockers: increased cardiac depression

Carbamazepine, digoxin, prazosin, quinidine: increased blood levels of these drugs

Drug-food. Grapefruit juice: increased drug absorption

Patient monitoring

• Monitor vital signs closely, especially blood pressure.

• Assess liver function test results.

• Monitor for arrhythmias and peripheral edema.

Patient teaching

• Tell patient he may take with or without food, but not with grapefruit juice.

• Instruct patient to move slowly when sitting up or standing, to avoid dizziness or light-headedness from sudden blood pressure decrease.

• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.

• Teach patient with heart, kidney, or liver disease to watch for and promptly report adverse reactions.

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

isradipine

A calcium channel blocking drug used to treat high blood pressure (HYPERTENSION). A brand name is Prescal.
References in periodicals archive ?
As presented (Table 4, according to [129]), for diltiazem (poor lipid solubility), no AO was detected, whereas the other CA and a-tocopherol have demonstrated AOA at least at concentrations of 10 and 50 [micro]M: [alpha]-tocopherol > lacidipine > nifedipine > isradipine, verapamil, and amlodipine.
Similar results were obtained in studies by Mielcarek and Daczkowska (1999), where the methyl derivative of [beta]-cyclodextrin doubled the photostability of isradipine. Other studies revealed that [beta]-cyclodextrin not only increased the photostability of the encapsulated substance but also the thermal stability of the host (TAKAHASHI et al., 2011).
Isradipine * 0.15-0.45 Adverse effects mg/kg/d up to are flushing, 20 mg/d nausea/ (tid-qid) vomiting, headache, and Nifedipine XR 0.2-0.50 edema.
Alomrani, Effect of formulation, chemical enhancer and ultrasound on the percuteous absorption of isradipine through rabbit skin [M.S.
Some commonly prescribed drugs in this class include nifedipine (Adalat, Procardia and others), nicardipine (Cardene), isradipine (DynaCirc), amlodipine (Norvasc) and felodipine (Plendil).
Al-Olyan, "Spectrofluorometric determination of nicardipine, nifedipine and isradipine in pharmaceutical preparations and biological fluids," Central European Journal of Chemistry, vol.
Indeed, administration of L-type [Ca.sup.2+] channel antagonists, including isradipine [59] and nimodipine [60], exerts neuroprotective effects in MPTP mouse models.
isradipine, efonidipine, felodipine, fluspirilene, gallopamil,
And because the drug, called isradipine, has already been approved for human use, it could soon be available for Parkinson's patients, the lead researcher said.
Furthermore, after 24 hours, calcium antagonists (verapamil, nifedipine, darodipine, isradipine, diltiazem, etc.) reduced cholesterol level in cultured cells, whereas beta-blockers (propranolol, alprenolol, metoprolol, atenolol, pindolol, and timolol) caused a 1.5- to twofold rise of cholesterol content in the cells, cultured from an atherosclerotic plaque (5).