CLINICAL USE

Anti-arrhythmic agent:Treatment of ventricular arrhythmias, especially after myocardial infarctionAtrial tachycardia

DOSE IN NORMAL RENAL FUNCTION

Slow IV injection: 50 mg/min (100 mg with ECG monitoring), repeated at 5-minute intervals until arrhythmia is controlled; max dose 1 gInfusion: 500–600 mg over 25–30 minutes with ECG monitoring, then maintenance of 2–6 mg/minute. If required start oral anti-arrhythmics 3–4 hours after infusion

PHARMACOKINETICS

  • Molecular weight                           :271.8
  • %Protein binding                           :15–20
  • %Excreted unchanged in urine     : 30–70
  • Volume of distribution (L/kg)       :1.48–4.3
  • half-life – normal/ESRD (hrs)      :2.5–5/9.6–11.3

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function
  • 10 to 20     : Dose as in normal renal function
  • <10           : Normal loading dose. Maintenance dose according to response, lower doses or longer dosage intervals may be required

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Dialysed. Dose as in GFR
  • <10           : mL/min
  • HD                     :Dialysed. Dose as in GFR
  • <10           : mL/min
  • HDF/high flux   :Dialysed. Dose as in GFR
  • <10           : mL/min
  • CAV/VVHD      :Dialysed. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Anti-arrhythmics: amiodarone increases procainamide levels, increased risk of ventricular arrhythmias – avoid concomitant use; increased myocardial depression with other anti-arrhythmics
  • Antibacterials: increased risk of ventricular arrhythmias with moxifloxacin – avoid concomitant use; concentration increased by trimethoprim
  • Antidepressants: increased risk of ventricular arrhythmias with tricyclicsAntihistamines: increased risk of ventricular arrhythmias with mizolastine– avoid concomitant use
  • Antimalarials: increased risk of ventricular arrhythmias with artemether/lumefantrine – avoid concomitant use
  • Antipsychotics: increased risk of ventricular arrhythmias with phenothiazines and any antipsychotics that prolong the QT interval; avoid with amisulpride, pimozide and sertindole
  • Atomoxetine: increased risk of ventricular arrhythmias
  • Beta-blockers: increased myocardial depression; increased risk of ventricular arrhythmias with sotalol – avoid concomitant use5HT 3 antagonists: increased risk of ventricular arrhythmias with dolasetron – avoid concomitant use; avoid with tropisetronMuscle relaxants: enhanced effect of muscle relaxants
  • Ulcer-healing drugs: levels increased by cimetidine

    ADMINISTRATION

    Reconstition

    –

    Route

    IV bolus,

    IV infusion

    , IM

    Rate of Administration

    Bolus: 50–100 mg/minute Infusion: 2–6 mg/minute

    Comments

    Stable in glucose 5% Dilute to a concentration of 2 mg/mL and give at a rate of 1–3 mL/minute, or to a Procainamide hydrochloride.PROCAINAMIDe HYDROCHLORIDe 607concentration of 4 mg/mL and give at a rate of 0.5–1.5 mL/minuteStability of solution can be improved by adding sodium bicarbonate to glucose solution

    OTHER INFORMATION

    For optimum response, plasma concentration should be 3–10 mg/L; severe toxicity has been noted at concentrations above 12 mg/LActive metabolite is N-acetyl- procainamide (NAPA) which is 80% renally excretedHaemofiltration can be used in cases of procainamide poisoningHalf-life depends on acetylator status of patientCan cause systemic lupus erythematosus in up to 30% of patients with long-term use CAPD removes 19% of procainamide and 24% of NAPA.

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