procainamide hydrochloride.txt

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 &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :271.8

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :15–20

%Excreted unchanged in urine &nbsp &nbsp : 30–70

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :1.48–4.3

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :2.5–5/9.6–11.3

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function

10 to 20 &nbsp &nbsp : Dose as in normal renal function

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : 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 &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Dialysed. Dose as in GFR

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Dialysed. Dose as in GFR

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min

HDF/high flux &nbsp :Dialysed. Dose as in GFR

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min

CAV/VVHD &nbsp &nbsp &nbsp: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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