Drug Monograph

Dofetilide

US brand: Tikosyn (Pfizer); FDA-approved October 1, 1999. Generics available since 2011. Not marketed in Europe, Canada, or Australia.
Class III antiarrhythmic (selective IKr blocker) · Oral capsule
Pharmacokinetic Profile
Half-Life
~10 h (range 4.8–13.5 h)
Metabolism
Minor hepatic via CYP3A4 (low affinity)
Protein Binding
60–70%
Bioavailability
>90%; unaffected by food/antacid
Volume of Distribution
~3 L/kg
Clinical Information
Drug Class
Class III antiarrhythmic (selective IKr blocker)
Available Doses
125, 250, 500 mcg capsules
Route
Oral only (no IV form approved in US)
Renal Adjustment
Mandatory by CrCl; contraindicated <20 mL/min
Hepatic Adjustment
Mild–moderate: none required; severe: limited data, use with caution
Pregnancy
Use only if benefit clearly justifies fetal risk; animal teratogenicity
Lactation
Not recommended — milk excretion unknown
Boxed Warning
Yes — torsades; mandatory inpatient initiation ≥3 days
Generic Available
Yes
Rx

Indications

IndicationApproved PopulationTherapy TypeStatus
Conversion of atrial fibrillation/atrial flutter to normal sinus rhythmAdults with highly symptomatic AF/AFL of >1 week durationPharmacologic cardioversionFDA Approved
Maintenance of normal sinus rhythm after conversion of AF/AFL of >1 week durationAdults with highly symptomatic AF/AFL who have been converted to NSRChronic monotherapyFDA Approved

Dofetilide is a selective blocker of the rapidly activating delayed rectifier potassium current (IKr). It is one of the few oral antiarrhythmics that can be used in patients with structural heart disease, including reduced left ventricular ejection fraction, because the DIAMOND-CHF and DIAMOND-MI mortality studies showed that dofetilide is mortality-neutral in heart failure and post-MI populations. This distinguishes it from Class IC agents (flecainide, propafenone), which increase mortality in these settings. The 2023 ACC/AHA/ACCP/HRS atrial fibrillation guideline lists dofetilide as one option for rhythm control in patients with structural heart disease where Class IC agents are unsafe.

Two important boundaries on the FDA-approved indication should be noted explicitly: dofetilide is approved only for AF/AFL of greater than one week duration, and the prescribing information states that dofetilide has not been shown to be effective in patients with paroxysmal atrial fibrillation. Because of its torsades risk, dofetilide must be initiated in a hospital setting with at least three days of continuous ECG monitoring per the boxed warning, even though the FDA-mandated REMS program for the brand-name product was rescinded in 2016.

Off-Label Uses (with Evidence Quality)

Maintenance of sinus rhythm in paroxysmal AF (low-quality evidence): the FDA prescribing information explicitly states dofetilide has not been shown to be effective in paroxysmal AF; observational data suggest substantially lower long-term success rates compared with persistent AF, and proarrhythmia risk persists. Reserved for patients who have failed multiple alternative agents.

Suppression of recurrent atrial tachycardia (low-quality evidence): occasionally used in specialized electrophysiology practice when other agents have failed.

Bridging in patients awaiting catheter ablation (moderate-quality evidence): observational cohorts have reported acceptable safety and partial symptomatic benefit when used as a second-line agent in patients refractory to other antiarrhythmics.

Ventricular arrhythmias (low-quality evidence): limited published experience; not a recommended first-line indication.

Dose

Dosing

Dofetilide is unique among commonly prescribed antiarrhythmics in that the dose must be selected from a matrix of two variables — calculated creatinine clearance (Cockcroft–Gault using actual body weight) and corrected QT interval — and re-checked at every dose for the first three days of therapy. The doses below organize the regimen by clinical scenario rather than by capsule strength.

Clinical ScenarioStarting DoseMaintenance DoseMaximum DoseNotes
Atrial fibrillation/flutter — inpatient initiation, CrCl >60 mL/min500 mcg PO BID500 mcg BID, modified by post-dose QTc500 mcg BIDRecheck QTc 2–3 h after each dose for the first 5 doses; halve dose if QTc rises >15% above baseline OR >500 ms after dose 1.
Discontinue if QTc >500 ms (550 ms with VCA) after the second dose or any subsequent dose.
CrCl 40–60 mL/min250 mcg PO BID250 mcg BID, modified by post-dose QTc250 mcg BIDHalve to 125 mcg BID if early QTc criteria met after dose 1.
Recheck CrCl every 3 months as outpatient.
CrCl 20–39 mL/min125 mcg PO BID125 mcg BID, modified by post-dose QTc125 mcg BIDIf QTc criteria met after first dose, reduce to 125 mcg once daily.
High-vigilance group — consider alternative antiarrhythmic.
CrCl <20 mL/minContraindicated — do not initiateHemodialysis effect on dofetilide is unknown.
Same prohibition applies if CrCl declines below 20 mL/min during therapy.
Reinitiation after a treatment gapSame starting dose as initial CrCl/QTc-based regimenPer QTc response over the inpatient course500 mcg BIDHospital readmission for monitoring is required even when restarting at a previously tolerated dose.
Reload data show TdP risk is higher when reloading at a higher than previously tolerated dose.

QTc-Based Dose Adjustment During Initiation

Trigger (after dose 1, before dose 2)ActionTrigger (after dose 2 or any later dose)Action
QTc rises >15% above baseline OR QTc >500 ms (550 ms with VCA)Halve the next dose:
500 mcg → 250 mcg BID
250 mcg → 125 mcg BID
125 mcg → 125 mcg once daily
QTc >500 ms (550 ms with VCA)Discontinue dofetilide and observe until QTc returns to baseline.

Population-Specific Adjustments

PopulationAdjustmentRationale
Older adultsInitiate at the lower end of the matrix; verify CrCl using actual body weightAge-related decline in renal function may not be reflected in serum creatinine alone; risk of TdP rises with female sex and advanced age.
Female patientsNo formal dose change; heightened TdP vigilanceFemale sex was an independent risk factor for TdP in DIAMOND-CHF analyses (odds ratio approximately 3).
NYHA III–IV heart failureNo formal dose change; heightened TdP vigilanceNYHA III–IV class was an independent TdP risk factor in DIAMOND-CHF analyses (odds ratio approximately 4).
Hepatic impairmentMild–moderate: no adjustment. Severe: limited data; use cautiouslyHepatic metabolism contributes minimally; PK is not significantly altered in mild–moderate dysfunction.
Pediatric (<18 y)Safety and efficacy not establishedExcluded from pivotal trials.
Clinical Pearl — The Initiation Protocol Is the Drug

The boxed-warning protocol — baseline ECG and CrCl, dosing matrix, QTc check at 2–3 hours after each of the first five doses, dose halving for early QTc rise, discontinuation for sustained QTc >500 ms after dose 2, and three full days of telemetry — is what makes dofetilide safe enough to use. Outside this structure, the drug carries a torsades risk substantially higher than other Class III agents. Most TdP events occur within the first 72 hours, which is exactly when the patient is on telemetry; this design intentionally surfaces the risk where it can be managed.

PK

Pharmacology

Mechanism of Action

Dofetilide is a methanesulfonamide derivative that selectively blocks the rapidly activating component of the delayed rectifier potassium current (IKr) without affecting other ion channels at therapeutic concentrations. Per the FDA prescribing information, dofetilide blocks only IKr at concentrations covering several orders of magnitude, with no relevant effect on other repolarizing potassium currents (IKs, IK1), sodium channels, or alpha- or beta-adrenergic receptors. This action prolongs the cardiac action potential duration and effective refractory period in both atrial and ventricular myocardium, terminating reentry circuits responsible for atrial fibrillation and atrial flutter. Unlike amiodarone or sotalol, dofetilide has no clinically meaningful effect on heart rate, blood pressure, AV nodal conduction, or cardiac contractility, and lacks beta-adrenergic blocking activity. This selectivity allows safer use in patients with sinus node disease, AV block, hypotension, or systolic dysfunction — but it also means dofetilide does not slow the ventricular response in atrial fibrillation and may be used together with rate-controlling agents.

The drug exhibits “reverse use-dependence” — QT prolongation is greatest at slow heart rates and after conversion to sinus rhythm, which explains why torsades de pointes most often appears shortly after restoration of sinus rhythm rather than during the initial atrial fibrillation.

ADME Profile

ParameterValueClinical Implication
AbsorptionBioavailability >90%; Tmax 2–3 h fasted; food and antacids do not affect total exposureMay be administered without regard to meals; rapid absorption explains the timing of post-dose QTc checks at 2–3 hours.
DistributionVd ~3 L/kg (per FDA label); protein binding 60–70%, independent of plasma concentration and renal functionModest tissue distribution and stable protein binding mean dofetilide does not accumulate in fat or organs the way amiodarone does.
MetabolismMinor hepatic metabolism via CYP3A4 (low affinity), N-dealkylation, and N-oxidation; no quantifiable circulating metabolitesStrong CYP3A4 inhibitors (e.g., ketoconazole) can raise levels and trigger TdP; dofetilide does not inhibit CYP enzymes itself.
Elimination~80% renal excretion (~80% as unchanged drug); cleared by glomerular filtration plus active tubular secretion via the cation transport system; terminal half-life ~10 hRenal-dose adjustment is mandatory and contraindicated below CrCl 20 mL/min. Drugs that inhibit organic cation transport (cimetidine, trimethoprim, ketoconazole, megestrol, prochlorperazine, dolutegravir) are contraindicated.
SE

Side Effects

Dofetilide is generally well tolerated, with a non-cardiac adverse-event profile dominated by mild, self-limited symptoms. The dominant safety signal is torsades de pointes, which is dose-dependent and almost always emerges during the first 72 hours of therapy under telemetry — the rationale for the inpatient initiation protocol. Incidence rates below are drawn primarily from the supraventricular arrhythmia trials in the Tikosyn FDA label and from the DIAMOND mortality studies, with the source population indicated where rates differ meaningfully between settings.

≥10% Very Common Adverse Effects
Adverse EffectIncidenceClinical Note
Headache~11%Most frequently reported adverse event in pivotal trials; usually mild and self-limited.
Chest pain~10%Often non-cardiac; investigate for ischemia or arrhythmia recurrence first.
Ventricular arrhythmias (DIAMOND population — heart failure / post-MI)Up to ~14.5%Higher rate reflects the high baseline arrhythmia burden in patients with structural heart disease enrolled in DIAMOND, not the rate expected in the SVT/AF population.
1–10% Common Adverse Effects
Adverse EffectIncidenceClinical Note
Dizziness~8%Distinguish orthostatic light-headedness from arrhythmia-related presyncope.
Respiratory tract infection~7%Rate similar to placebo; no mechanistic link to dofetilide.
Dyspnea~6%Often related to underlying heart failure; reassess for decompensation.
Nausea~5%Usually mild; rarely requires intervention.
Insomnia~4%Reported numerically more often than placebo.
Flu syndrome / asthenia~4%Generally mild and not therapy-limiting.
Diarrhea, back pain, abdominal pain, rash~3% eachRates similar to placebo for several of these.
Serious Serious Adverse Effects (regardless of frequency)
Adverse EffectEstimated FrequencyTypical OnsetRequired Action
Torsades de pointes — supraventricular arrhythmia population (FDA label)0.8% (with recommended renal-adjusted dosing)Majority within first 3 daysIV magnesium sulfate, correct electrolytes, withhold drug, pace if bradycardic; permanent discontinuation usually required.
Torsades de pointes — heart failure (DIAMOND-CHF)3.3% (25/762 patients)Most within first 3 daysAs above; female sex and NYHA III–IV are independent risk factors.
Torsades de pointes — post-MI (DIAMOND-MI, with renal-adjusted dose)~0.9% (per Jaiswal 2014 review of DIAMOND data)Most within first 3 daysCorrect electrolytes; verify CrCl and concomitant medications.
Sustained ventricular tachycardia~2.0% (FDA label, SVT studies)Days to weeksMost common cause for trial discontinuation; manage per ACLS.
Sudden cardiac deathRare in published seriesAny timeOutpatient deaths reported when protocol breaches occur (drug interactions, electrolyte loss, missed CrCl re-check).
QTc prolongation requiring interventionApproximately 23% of patients required dose reduction for renal function during initiation; ~3% required additional reduction or discontinuation for excessive QT/QTc prolongation (FDA label, SAFIRE-D and EMERALD)Within 2–3 h of any doseHalve dose if criteria met after dose 1; discontinue if criteria met after dose 2 or any later dose.
Stroke / cerebral ischemiaReported, frequency not quantified in labelVariableConfirm therapeutic anticoagulation before electrical or pharmacologic cardioversion.
Discontinuation Treatment Discontinuation
Adults — supraventricular arrhythmia trials
8.7% vs 8.0% placebo
Top reason: ventricular tachycardia (2.0% vs 1.3% placebo). QTc prolongation and intolerable adverse effects accounted for the remainder.
Pediatric
not established
Safety and efficacy in patients younger than 18 years have not been established.
Reason for DiscontinuationApprox. IncidenceContext
Ventricular tachycardia (sustained or non-sustained)2.0%Most common reason for trial discontinuation per FDA label.
Excessive QTc prolongation during initiation~3% require down-titration or discontinuation in pivotal trials; ~30% require dose adjustment in reload admissionsMost occur after dose 1 or 2.
Symptomatic non-cardiac adverse effects<2%Most non-cardiac adverse events do not require discontinuation.
Decline in renal function below CrCl 20 mL/minPopulation-dependentDiscontinue if CrCl falls below contraindication threshold during therapy.
Management of Suspected Torsades de Pointes

Acute management is identical regardless of the triggering antiarrhythmic: discontinue dofetilide immediately, give intravenous magnesium sulfate 1–2 g (regardless of measured serum magnesium), correct hypokalemia aggressively to a target potassium ≥4 mEq/L, and consider isoproterenol or transvenous pacing for bradycardia-dependent TdP. Defibrillation is required for hemodynamic collapse. Investigate every modifiable contributor — concomitant QT-prolonging drug, missed CrCl re-check, hypomagnesemia, recent diuretic dose, or breach of the contraindicated drug list — before any consideration of restarting therapy.

Int

Drug Interactions

Dofetilide has the most extensive list of contraindicated drug combinations of any oral antiarrhythmic. Two pharmacokinetic mechanisms drive nearly every major interaction: inhibition of the renal organic cation transport system, which delays dofetilide elimination, and CYP3A4 inhibition, which raises plasma exposure modestly. Either pathway can push QTc into the danger zone. Concurrent use of any QT-prolonging drug additionally raises the risk of torsades through pharmacodynamic addition. Medication reconciliation before admission for dofetilide initiation is therefore as important as the ECG and CrCl checks.

Contraindicated Cimetidine
MechanismInhibits renal organic cation transport.
EffectPer FDA label, cimetidine 400 mg BID coadministered with dofetilide 500 mcg BID for 7 days increased dofetilide plasma levels by 58%.
ManagementSwitch to famotidine or a proton pump inhibitor; coadministration is contraindicated, including with OTC cimetidine.
FDA PI
Contraindicated Verapamil
MechanismIncreases dofetilide peak plasma exposure (rapid increase reported in coadministration studies).
EffectHigher incidence of torsades de pointes in pooled SVT and DIAMOND analyses.
ManagementUse diltiazem or a beta-blocker for rate control instead.
FDA PI
Contraindicated Ketoconazole
MechanismStrong CYP3A4 inhibition and competition for cation transport.
EffectPer FDA label, ketoconazole 400 mg/day for 7 days increased dofetilide AUC by 41% in men / 69% in women and Cmax by 53% in men / 97% in women.
ManagementAvoid; if antifungal therapy is essential, choose an alternative class such as terbinafine after specialist review.
FDA PI
Contraindicated Trimethoprim (alone or with sulfamethoxazole)
MechanismInhibits renal cation transport.
EffectPer FDA label, TMP/SMX 160/800 mg BID with dofetilide 500 mcg BID for 4 days increased dofetilide AUC by 103% and Cmax by 93%.
ManagementChoose an alternative antibiotic (e.g., nitrofurantoin, fosfomycin, or a beta-lactam) for the indication.
FDA PI
Contraindicated Hydrochlorothiazide (alone or in combination)
MechanismCombined effect: increases dofetilide plasma concentrations AND induces hypokalemia/hypomagnesemia (lowers TdP threshold).
EffectFDA label states HCTZ significantly increases dofetilide plasma concentrations and QT interval prolongation.
ManagementSwitch to a non-thiazide diuretic (e.g., loop diuretic with potassium replacement); also applies to combinations such as HCTZ/triamterene.
FDA PI
Contraindicated Prochlorperazine
MechanismInhibits renal cation transport; also has intrinsic QT-prolonging effect.
EffectIncreased dofetilide exposure plus additive QT prolongation.
ManagementAvoid; non-pharmacologic antiemetic measures or alternative agents (with awareness that ondansetron is also QT-prolonging).
FDA PI
Contraindicated Megestrol
MechanismInhibits renal cation transport.
EffectIncreased dofetilide exposure raising TdP risk.
ManagementAvoid; alternative appetite stimulants (e.g., mirtazapine) may be considered.
FDA PI
Contraindicated Dolutegravir
MechanismInhibits OCT2 (renal organic cation transporter 2).
EffectIncreased dofetilide plasma concentration; potential for life-threatening QT prolongation and TdP.
ManagementAvoid combination; use an alternative integrase inhibitor or non-INSTI regimen in consultation with HIV specialist.
FDA PI
Major Other QT-prolonging drugs (Class IA/III antiarrhythmics, methadone, citalopram, certain fluoroquinolones, ondansetron, haloperidol, azithromycin, etc.)
MechanismAdditive QT prolongation through IKr blockade and other repolarization effects.
EffectIncreased risk of torsades de pointes.
ManagementDiscontinue all other Class I or III antiarrhythmics for at least three half-lives before initiating dofetilide; for amiodarone, a long washout (typically several months) is required given its very long half-life. Avoid other QT-prolonging agents whenever possible.
FDA PI / CredibleMeds
Moderate Other CYP3A4 inhibitors (macrolides, protease inhibitors, diltiazem, grapefruit juice, nefazodone, norfloxacin, quinine, zafirlukast, amiodarone, SSRIs)
MechanismInhibits CYP3A4-mediated minor metabolic pathway, modestly increasing dofetilide exposure.
EffectVariable rises in plasma concentration; potentially clinically significant given the narrow therapeutic window.
ManagementUse cautiously; recheck QTc when starting or stopping; avoid strong CYP3A4 inhibitors when alternatives exist.
FDA PI / Lexicomp
Moderate Potassium-depleting diuretics (loop diuretics)
MechanismHypokalemia and hypomagnesemia lower the threshold for TdP.
EffectIncreased TdP risk even at therapeutic dofetilide concentrations.
ManagementMaintain potassium ≥4 mEq/L and magnesium within normal range throughout therapy; supplement proactively. Note thiazides are separately contraindicated.
FDA PI
Minor Digoxin
MechanismNo significant pharmacokinetic interaction.
EffectCombined use was associated with a higher TdP rate in pooled analyses, likely reflecting underlying heart disease rather than a direct DDI.
ManagementCoadministration is permitted; maintain therapeutic digoxin trough and serum potassium.
FDA PI
Mon

Monitoring

Monitoring during the inpatient initiation period is intensive — every dose, every two to three hours, on telemetry. After discharge, monitoring shifts to a quarterly check of renal function and ECG with prompt re-evaluation whenever clinical context changes (intercurrent illness, new medications, electrolyte loss).

  • Continuous telemetry Minimum 3 days at initiation; or 12 h after conversion to NSR (whichever is longer)
    Routine
    Required by the boxed warning regardless of indication; same requirement applies to reinitiation. Most TdP events occur during this window.
  • 12-lead ECG (QTc) Baseline; 2–3 h after each of the first 5 doses; then every 3 months as outpatient
    Routine
    QTc >440 ms (or >500 ms with VCA) at baseline contraindicates initiation. After dose 1, halve dose if QTc rises >15% above baseline OR exceeds 500 ms. After dose 2 or any later dose, QTc >500 ms (or >550 ms with VCA) requires discontinuation.
  • CrCl (Cockcroft–Gault, actual body weight) Baseline, then every 3 months
    Routine
    Recalculate any time renal function may have changed (intercurrent illness, dehydration, new nephrotoxic drug). Reduce dose or stop if CrCl crosses a threshold.
  • Serum potassium and magnesium Baseline, before each dose during initiation, then periodically
    Routine
    Maintain potassium within normal range (FDA label notes potassium levels were generally maintained above 3.6–4.0 mEq/L in clinical trials) and magnesium within normal range throughout therapy. Replete and recheck before any dose is given if values fall below target.
  • Heart rate / rhythm Continuous during initiation; periodic outpatient
    Routine
    Heart rate <50 bpm has not been studied; use uncorrected QT (not QTc) when heart rate is <60 bpm.
  • Anticoagulation status Before any cardioversion attempt
    Routine
    Patients with AF should be anticoagulated according to standard practice (CHA₂DS₂-VASc, prior TEE or therapeutic anticoagulation per current guideline) prior to electrical or pharmacologic cardioversion.
  • Medication reconciliation Before every dose during initiation; at every outpatient visit
    Trigger-based
    Verify absence of contraindicated drugs and any new QT-prolonging agent. The contraindicated list includes cimetidine, dolutegravir, hydrochlorothiazide, ketoconazole, megestrol, prochlorperazine, trimethoprim, and verapamil.
  • Symptom assessment Each visit
    Routine
    Ask about palpitations, syncope, presyncope, chest pain, and new-onset diarrhea, vomiting, or excess sweating (electrolyte loss).
Outpatient Visit Template (every 3 months)

12-lead ECG with QTc; serum creatinine and electrolytes; medication reconciliation against the contraindicated list; symptom-focused review for syncope, palpitations, and gastrointestinal losses; review of all new prescriptions and over-the-counter products since the last visit. Discontinue dofetilide and refer back to telemetry if QTc exceeds 500 ms (or 550 ms with VCA), if CrCl falls below 20 mL/min, or if any contraindicated drug has been started.

CI

Contraindications & Cautions

FDA Boxed Warning To Minimize the Risk of Induced Arrhythmia

To minimize the risk of induced arrhythmia, patients initiated or re-initiated on TIKOSYN should be placed for a minimum of 3 days in a facility that can provide calculations of creatinine clearance, continuous electrocardiographic monitoring, and cardiac resuscitation. For detailed instructions regarding dose selection, see the prescribing information.

The risk of torsades de pointes is dose-related and is highest in the first 72 hours after initiation. Although the formal Risk Evaluation and Mitigation Strategy (REMS) program for Tikosyn was rescinded by the FDA in January 2016, the inpatient initiation requirement remains in the prescribing information and is the standard of care.

Absolute Contraindications

  • Congenital or acquired long QT syndrome
  • Baseline QT or QTc >440 ms (or >500 ms in patients with ventricular conduction abnormalities)
  • Severe renal impairment — calculated CrCl <20 mL/min
  • Concomitant cation transport inhibitors: cimetidine, dolutegravir, hydrochlorothiazide (alone or in any combination), ketoconazole, megestrol, prochlorperazine, trimethoprim (alone or with sulfamethoxazole), verapamil
  • Known hypersensitivity to dofetilide or any component

Relative Contraindications (Specialist Input Recommended)

  • Heart rate <50 beats per minute at baseline — not studied in clinical trials; consider pacemaker support
  • NYHA class III–IV heart failure with female sex — independent risk factors for TdP in DIAMOND-CHF; specialist co-management advised
  • Severe hepatic impairment (Child-Pugh C) — limited PK data; cautious use only
  • Concurrent QT-prolonging drugs that cannot be stopped — joint cardiology and prescribing-specialty decision; sustained telemetry required
  • Pregnancy — animal studies show teratogenicity; use only when potential benefit clearly outweighs fetal risk in the absence of safer alternatives

Use with Caution

  • Older adults — confirm CrCl is calculated using actual body weight; age-related decline in renal function may not be reflected in serum creatinine
  • Female sex — heightened TdP vigilance even within the standard dosing matrix
  • Concurrent CYP3A4 inhibitors — modest pharmacokinetic interaction can be clinically meaningful
  • Concurrent loop diuretics — proactively maintain potassium ≥4 mEq/L and magnesium within normal range
  • Lactation — dofetilide excretion in human milk is unknown; not recommended
  • Pediatric patients — safety and efficacy not established
  • Paroxysmal atrial fibrillation — FDA prescribing information notes dofetilide has not been shown to be effective in paroxysmal AF; observational data show lower long-term success rates
Pt

Patient Counselling

Purpose of Therapy

Explain that dofetilide is used to convert atrial fibrillation or atrial flutter to a normal heart rhythm and to keep it normal once converted. Frame it as an effective option that requires careful initial monitoring: the first three days in hospital are essential for establishing the safe dose and identifying the small minority of patients who develop a dangerous rhythm called torsades de pointes during this window.

How to Take

Take dofetilide twice daily, roughly twelve hours apart, at the same times each day. It can be taken with or without food. If a dose is missed, do not double up — skip the missed dose and take the next dose at the usual time. Avoid grapefruit juice, which can increase blood levels of dofetilide. The medication must not be stopped or restarted without the cardiologist’s involvement; restarting requires a return to hospital for monitoring, even at the same dose previously tolerated.

Why the Hospital Stay Is Required
Tell patient The first three days in hospital are when this medicine is most likely to cause an abnormal rhythm. Continuous heart monitoring during this time lets the team detect any problem immediately and treat it before it causes harm. The dose may be reduced or the medicine stopped during these three days based on the heart-rhythm tracings.
Call prescriber This is an inpatient process — direct concerns to the bedside team during admission.
Watch for Symptoms of Heart Rhythm Problems
Tell patient After discharge, watch for new fast or pounding heartbeats, fainting, near-fainting, dizziness, severe shortness of breath, or chest pain. These can be early signs that the heart rhythm has become abnormal again.
Call prescriber For any of these symptoms; call emergency services for fainting, severe dizziness, or chest pain that does not resolve within minutes.
The Forbidden Drug List
Tell patient Several common medicines must never be combined with dofetilide because they push blood levels into a dangerous range. These include cimetidine (Tagamet), the heart medicine verapamil, the antifungal ketoconazole, the antibiotic trimethoprim (sometimes combined with sulfa as Bactrim or Septra), the diuretic hydrochlorothiazide, the antinausea medicine prochlorperazine (Compazine), the appetite stimulant megestrol (Megace), and the HIV medicine dolutegravir. Always carry an up-to-date medication list and show it to every healthcare provider, including dentists and pharmacists.
Call prescriber Before starting any new prescription, over-the-counter product, herbal supplement, or antibiotic — even a short course. Do not stop dofetilide on your own, but do call the prescribing cardiologist before adding anything new.
Diarrhea, Vomiting, Sweating, or Loss of Appetite
Tell patient Significant fluid or electrolyte losses — from a stomach virus, food poisoning, prolonged sweating, or being unable to eat or drink — can lower potassium and raise the risk of dangerous heart rhythms while on dofetilide. Stay well hydrated and keep a potassium-rich diet (bananas, potatoes, citrus, beans).
Call prescriber For diarrhea or vomiting lasting more than a day, marked weakness, or any episode of feeling about to faint while taking the medication.
Anticoagulation Around Cardioversion
Tell patient If atrial fibrillation has been present, anticoagulation (warfarin or a direct oral anticoagulant) should be on board before and after rhythm conversion to prevent stroke. Do not stop blood thinners on your own, even after the heart rhythm normalizes.
Call prescriber Before stopping any anticoagulant or before any planned procedure or surgery.
Pregnancy and Breastfeeding
Tell patient Dofetilide should be used during pregnancy only when the potential benefit clearly outweighs the risk to the fetus, since animal studies have shown harm. It is not known whether dofetilide passes into breast milk; breastfeeding is not recommended while taking the medication. Patients who could become pregnant should discuss reliable contraception with the prescriber.
Call prescriber For confirmed or suspected pregnancy, or before stopping contraception.
Restarting After a Missed Period of Therapy
Tell patient If you stop dofetilide for any reason — running out of medication, hospitalization for another problem, missing several doses — restarting requires another hospital admission for at least three days of telemetry, even at the dose that was previously tolerated. Do not resume the medication on your own.
Call prescriber As soon as possible if doses have been missed or the medication has been temporarily stopped.
Ref

Sources

Regulatory (Prescribing Information)
  1. Tikosyn (dofetilide) capsules — full prescribing information. Pfizer Inc. Available via DailyMed at dailymed.nlm.nih.gov Primary US prescribing information; source of the dosing matrix, contraindicated drug list, drug-interaction PK data (cimetidine, ketoconazole, TMP/SMX), and adverse-event incidence rates cited in this monograph.
  2. FDA Supplement Approval / Release of REMS Requirement for Tikosyn (dofetilide) Capsules. January–March 2016. accessdata.fda.gov Documents the FDA’s release of the formal REMS program while retaining the inpatient initiation requirement in the boxed warning.
  3. FDA Supplement Approval Letter for Tikosyn (dofetilide). 2019. accessdata.fda.gov Source for the current FDA-labeled QTc thresholds, dosing algorithm steps, and monitoring schedule.
Key Clinical Trials
  1. Torp-Pedersen C, Møller M, Bloch-Thomsen PE, et al. Dofetilide in patients with congestive heart failure and left ventricular dysfunction. Danish Investigations of Arrhythmia and Mortality on Dofetilide (DIAMOND) Study Group. N Engl J Med. 1999;341(12):857–865. doi:10.1056/NEJM199909163411201 DIAMOND-CHF — established mortality neutrality and the 3.3% TdP rate (25/762 patients) in heart failure that informs current risk stratification.
  2. Køber L, Bloch Thomsen PE, Møller M, et al. Effect of dofetilide in patients with recent myocardial infarction and left-ventricular dysfunction: a randomised trial. Lancet. 2000;356(9247):2052–2058. DIAMOND-MI — confirmed mortality neutrality post-MI and informed the renal-adjusted dosing protocol that lowered TdP rates compared with earlier non-adjusted regimens.
  3. Singh S, Zoble RG, Yellen L, et al. Efficacy and safety of oral dofetilide in converting to and maintaining sinus rhythm in patients with chronic atrial fibrillation or atrial flutter: the Symptomatic Atrial Fibrillation Investigative Research on Dofetilide (SAFIRE-D) Study. Circulation. 2000;102(19):2385–2390. doi:10.1161/01.CIR.102.19.2385 Pivotal trial supporting FDA approval; defined the 500 mcg BID dose as the most effective regimen modified by the dosing algorithm.
  4. Pedersen HS, Elming H, Seibaek M, et al. Risk factors and predictors of torsade de pointes ventricular tachycardia in patients with left ventricular systolic dysfunction receiving dofetilide. Am J Cardiol. 2007;100(5):876–880. doi:10.1016/j.amjcard.2007.04.020 DIAMOND substudy quantifying female sex and NYHA class III–IV as independent TdP predictors.
Guidelines
  1. Joglar JA, Chung MK, Armbruster AL, et al. 2023 ACC/AHA/ACCP/HRS guideline for the diagnosis and management of atrial fibrillation. Circulation. 2024;149(1):e1–e156. doi:10.1161/CIR.0000000000001193 Defines the role of dofetilide in atrial fibrillation rhythm control, including recommendations for use in heart failure and structural heart disease.
  2. Al-Khatib SM, Stevenson WG, Ackerman MJ, et al. 2017 AHA/ACC/HRS guideline for management of patients with ventricular arrhythmias and the prevention of sudden cardiac death. Circulation. 2018;138(13):e272–e391. doi:10.1161/CIR.0000000000000549 Provides framework for managing acquired QT prolongation and torsades de pointes during antiarrhythmic therapy.
Mechanistic / Clinical Reviews
  1. Mounsey JP, DiMarco JP. Cardiovascular drugs. Dofetilide. Circulation. 2000;102(21):2665–2670. doi:10.1161/01.CIR.102.21.2665 Authoritative review of dofetilide pharmacology, electrophysiology, and clinical role.
  2. Lenz TL, Hilleman DE. Dofetilide, a new class III antiarrhythmic agent. Pharmacotherapy. 2000;20(7):776–786. Practical clinical pharmacology review covering dosing, monitoring, and interactions.
  3. Jaiswal A, Goldbarg S. Dofetilide induced torsade de pointes: mechanism, risk factors and management strategies. Indian Heart J. 2014;66(6):640–648. doi:10.1016/j.ihj.2013.12.021 Comprehensive review of the mechanism, modifiable risk factors, and acute management of dofetilide-induced TdP; source for the timing distribution of TdP events within DIAMOND populations.
  4. Wolbrette DL, Hussain S, Maraj I, Naccarelli GV. A quarter of a century later: what is dofetilide’s clinical role today? J Cardiovasc Pharmacol Ther. 2019;24(1):3–10. Contemporary review of dofetilide’s place in current AF rhythm-control practice, off-label uses, and real-world conversion data.
Pharmacokinetics / Special Populations
  1. Tham TC, MacLennan BA, Burke MT, et al. Pharmacodynamics and pharmacokinetics of the class III antiarrhythmic agent dofetilide (UK-68,798) in humans. J Cardiovasc Pharmacol. 1993;21(3):507–512. Original human pharmacokinetic characterization establishing the ~10-hour half-life and renal-dependent clearance.
  2. Allen MJ, Nichols DJ, Oliver SD. The pharmacokinetics and pharmacodynamics of oral dofetilide after twice daily and three times daily dosing. Br J Clin Pharmacol. 2000;50(3):247–253. Defines steady-state pharmacokinetics relevant to the twice-daily dosing schedule used clinically.
  3. Naksuk N, Sugrue AM, Padmanabhan D, et al. Potentially modifiable factors of dofetilide-associated risk of torsades de pointes among hospitalized patients with atrial fibrillation. J Interv Card Electrophysiol. 2019;54(2):189–196. doi:10.1007/s10840-018-0476-2 Modern observational study quantifying the contemporary TdP rate (~0.8%) and identifying modifiable contributors in hospitalized AF patients.