2.1 General Dosing Information
Nicardipine hydrochloride injection is intended for intravenous use. DOSAGE MUST BE INDIVIDUALIZED depending upon the severity of hypertension and the response of the patient during dosing. Blood pressure and heart rate should be monitored both during and after the infusion to avoid tachycardia or too rapid or excessive reduction in either systolic or diastolic blood pressure.
2.2 Preparation
Warning: Dilute vials before infusion.
Dilution
Nicardipine hydrochloride injection is administered by slow continuous infusion at a CONCENTRATION OF 0.1 MG/ML. Each vial (25 mg) should be diluted with 240 mL of compatible intravenous fluid (see below), resulting in 250 mL of solution at a concentration of 0.1 mg/mL.
Nicardipine hydrochloride injection has been found compatible and stable in polyvinyl chloride containers for 24 hours at controlled room temperature with:
Dextrose (5%) Injection, USP
Dextrose (5%) and Sodium Chloride (0.45%) Injection, USP
Dextrose (5%) and Sodium Chloride (0.9%) Injection, USP
Dextrose (5%) with 40 mEq Potassium, USP
Sodium Chloride (0.45%) Injection, USP
Sodium Chloride (0.9%) Injection, USP
Nicardipine hydrochloride injection is not compatible with Sodium Bicarbonate (5%) Injection, USP or Lactated Ringer’s Injection, USP.
The diluted solution is stable for 24 hours at room temperature.
Inspection
Visually inspect nicardipine hydrochloride injection for particulate matter and discoloration prior to administration, whenever solution and container permit. Nicardipine hydrochloride injection is normally light yellow in color.
Do not use the solution if particulate matter, precipitate or crystallization is present, or if the container appears damaged.
2.3 Dosage as a Substitute for Oral Nicardipine Therapy
The intravenous infusion rate required to produce an average plasma concentration equivalent to a given oral dose at steady state is shown in the following table:
Oral Nicardipine Dose
Equivalent Intravenous Infusion Rate
20 mg q8h
0.5 mg/hr
30 mg q8h
1.2 mg/hr
40 mg q8h
2.2 mg/hr
2.4 Dosage for Initiation of Therapy in a Drug-Free Patient
The time course of blood pressure decrease is dependent on the initial rate of infusion and the frequency of dosage adjustment. Nicardipine hydrochloride injection is administered by slow continuous infusion at a concentration of 0.1 mg/mL. With constant infusion, blood pressure begins to fall within minutes. It reaches about 50% of its ultimate decrease in about 45 minutes.
When treating acute hypertensive episodes in patients with chronic hypertension, discontinuation of infusion is followed by a 50% offset of action in 30 minutes ± 7 minutes but plasma levels of drug and gradually decreasing antihypertensive effects exist for many hours.
Titration
For a gradual reduction in blood pressure, initiate therapy at a rate of 50 mL/hr (5 mg/hr). If desired blood pressure reduction is not achieved at this dose, increase the infusion rate by 25 mL/hr (2.5 mg/hr) every 15 minutes up to a maximum of 150 mL/hr (15 mg/hr), until desired blood pressure reduction is achieved. For more rapid blood pressure reduction, titrate every 5 minutes.
Maintenance
Adjust the rate of infusion as needed to maintain desired response.
2.5 Conditions Requiring Infusion Adjustment
Hypotension or Tachycardia: In case of hypotension or tachycardia, discontinue infusion. When blood pressure and heart rate stabilize, restart infusion at low doses such as 30 mL/hr to 50 mL/hr (3 mg/hr to 5 mg/hr) and titrate to maintain desired blood pressure.
Infusion Site Changes: Change infusion site every 12 hours if administered via peripheral vein.
Impaired Cardiac, Hepatic, or Renal Function: Monitor closely when titrating nicardipine hydrochloride injection in patients with congestive heart failure or impaired hepatic or renal function [see Warnings and Precautions (5.4, 5.5 and 5.6)].
2.6 Transfer to Oral Antihypertensive Agents
If treatment includes transfer to an oral antihypertensive agent other than nicardipine capsules, initiate oral therapy upon discontinuation of nicardipine hydrochloride injection.
When switching to a TID regimen of nicardipine capsules, administer the first dose 1 hour prior to discontinuation of the infusion.
