QUINAGLUTE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for QUINAGLUTE (QUINAGLUTE).

How it works

Class Ia antiarrhythmic agent; binds to sodium channels and inhibits the fast inward sodium current, slowing phase 0 depolarization and prolonging the action potential duration. Also exhibits anticholinergic and negative inotropic effects.

What the body does with it

Metabolism	Primarily hepatic via CYP3A4; also undergoes renal excretion (20% unchanged).
Excretion	Renal elimination of unchanged drug and metabolites accounts for approximately 60-70% of total clearance. Biliary/fecal excretion contributes about 20-30%. Acidic urine increases renal clearance.
Half-life	Terminal elimination half-life is 5-7 hours in adults with normal renal function. In hepatic impairment, half-life may increase to 12-24 hours; in severe renal impairment (CrCl <10 mL/min), half-life may exceed 24 hours.
Protein binding	85-95% bound primarily to alpha-1-acid glycoprotein (AAG) and albumin. Binding saturable and concentration-dependent.
Volume of Distribution	2-4 L/kg, indicating extensive tissue distribution. Higher in heart, liver, lungs, and skeletal muscle.
Bioavailability	Oral: 70-85% for sustained-release; immediate-release: 70-90%. First-pass metabolism is minimal (less than 10%).
Onset of Action	Oral: 1-3 hours for conversion of atrial fibrillation/flutter. Intravenous: 5-10 minutes.
Duration of Action	Oral: 6-8 hours for sustained-release formulations; 4-6 hours for immediate-release. Intravenous: 4-6 hours. Note: Duration is dose-dependent and may be prolonged in renal impairment.

Classification & Brands

Dosing & administration

324-648 mg orally every 8-12 hours; extended-release formulation (quinidine gluconate).

Dosage form	TABLET, EXTENDED RELEASE
Renal impairment	GFR 10-50 mL/min: administer 75% of normal dose every 8-12 hours; GFR <10 mL/min: administer 50% of normal dose every 8-12 hours.
Liver impairment	Child-Pugh Class A: no adjustment; Class B: reduce dose by 25%; Class C: reduce dose by 50%.
Pediatric use	15-60 mg/kg/day orally divided every 6 hours; maximum 4 g/day.
Geriatric use	Initiate at lower end of dosing range (324-648 mg/day); monitor for QT prolongation and hypoglycemia.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for QUINAGLUTE (QUINAGLUTE).

Breastfeeding	Quinidine is excreted into human breast milk. The milk-to-plasma (M/P) ratio is approximately 0.5–0.8. Estimated infant dose is about 2–4% of maternal weight-adjusted dose. Although generally considered compatible with breastfeeding, monitor infant for arrhythmias, thrombocytopenia, and other adverse effects.
Teratogenic Risk	Quinidine (active ingredient in QUINAGLUTE) has demonstrated fetal toxicity in animal studies. In humans, use during pregnancy is associated with a low risk of teratogenicity in the first trimester. Reports of thrombocytopenia, eighth cranial nerve damage, and fetal QT prolongation have been noted. Risk is considered low but should be used only if clearly needed.

Warnings & precautions

■ FDA Black Box Warning

May cause fatal arrhythmias including torsade de pointes; quinidine can increase mortality in treatment of atrial fibrillation/flutter; monitor ECG and serum potassium; avoid if QT prolongation.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to quinidine, complete AV block, severe intraventricular conduction defects, history of drug-induced torsade de pointes, myasthenia gravis, and concurrent use with other QT-prolonging agents.

Clinical Precautions

Precautions

May cause cinchonism, thrombocytopenia, hepatotoxicity, and arrhythmogenic effects; caution in hepatic/renal impairment, myasthenia gravis, and concurrent QT-prolonging drugs.

Clinical Tips & Counseling

Drug interactions

Loading safety data…

QUINAGLUTE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for QUINAGLUTE (QUINAGLUTE).

How it works

What the body does with it

Metabolism	Primarily hepatic via CYP3A4; also undergoes renal excretion (20% unchanged).
Excretion	Renal elimination of unchanged drug and metabolites accounts for approximately 60-70% of total clearance. Biliary/fecal excretion contributes about 20-30%. Acidic urine increases renal clearance.
Half-life	Terminal elimination half-life is 5-7 hours in adults with normal renal function. In hepatic impairment, half-life may increase to 12-24 hours; in severe renal impairment (CrCl <10 mL/min), half-life may exceed 24 hours.
Protein binding	85-95% bound primarily to alpha-1-acid glycoprotein (AAG) and albumin. Binding saturable and concentration-dependent.
Volume of Distribution	2-4 L/kg, indicating extensive tissue distribution. Higher in heart, liver, lungs, and skeletal muscle.
Bioavailability	Oral: 70-85% for sustained-release; immediate-release: 70-90%. First-pass metabolism is minimal (less than 10%).
Onset of Action	Oral: 1-3 hours for conversion of atrial fibrillation/flutter. Intravenous: 5-10 minutes.
Duration of Action	Oral: 6-8 hours for sustained-release formulations; 4-6 hours for immediate-release. Intravenous: 4-6 hours. Note: Duration is dose-dependent and may be prolonged in renal impairment.

Classification & Brands

Dosing & administration

324-648 mg orally every 8-12 hours; extended-release formulation (quinidine gluconate).

Dosage form	TABLET, EXTENDED RELEASE
Renal impairment	GFR 10-50 mL/min: administer 75% of normal dose every 8-12 hours; GFR <10 mL/min: administer 50% of normal dose every 8-12 hours.
Liver impairment	Child-Pugh Class A: no adjustment; Class B: reduce dose by 25%; Class C: reduce dose by 50%.
Pediatric use	15-60 mg/kg/day orally divided every 6 hours; maximum 4 g/day.
Geriatric use	Initiate at lower end of dosing range (324-648 mg/day); monitor for QT prolongation and hypoglycemia.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for QUINAGLUTE (QUINAGLUTE).

Breastfeeding	Quinidine is excreted into human breast milk. The milk-to-plasma (M/P) ratio is approximately 0.5–0.8. Estimated infant dose is about 2–4% of maternal weight-adjusted dose. Although generally considered compatible with breastfeeding, monitor infant for arrhythmias, thrombocytopenia, and other adverse effects.
Teratogenic Risk	Quinidine (active ingredient in QUINAGLUTE) has demonstrated fetal toxicity in animal studies. In humans, use during pregnancy is associated with a low risk of teratogenicity in the first trimester. Reports of thrombocytopenia, eighth cranial nerve damage, and fetal QT prolongation have been noted. Risk is considered low but should be used only if clearly needed.

Warnings & precautions

■ FDA Black Box Warning

May cause fatal arrhythmias including torsade de pointes; quinidine can increase mortality in treatment of atrial fibrillation/flutter; monitor ECG and serum potassium; avoid if QT prolongation.

Side Effect Profile

Serious Effects

Absolute Contraindications

Clinical Precautions

Precautions

May cause cinchonism, thrombocytopenia, hepatotoxicity, and arrhythmogenic effects; caution in hepatic/renal impairment, myasthenia gravis, and concurrent QT-prolonging drugs.

Clinical Tips & Counseling

Drug interactions

Loading safety data…