QUINATIME

Clinical safety rating: caution

Comprehensive clinical and safety monograph for QUINATIME (QUINATIME).

How it works

Quinine acts by interfering with the parasite's ability to break down hemoglobin, leading to accumulation of toxic heme and parasite death. It also inhibits nucleic acid and protein synthesis in the parasite.

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 to 3-hydroxyquinine. Also metabolized by CYP2C19 and CYP2D6 to minor metabolites.
Excretion	Renal: ~20% unchanged; hepatic metabolism (CYP3A4) major route; biliary/fecal: ~80% as metabolites.
Half-life	Terminal elimination half-life 10-12 hours in healthy adults; prolonged in hepatic impairment.
Protein binding	80-85% bound primarily to albumin.
Volume of Distribution	2-3 L/kg; indicates extensive tissue distribution (e.g., liver, spleen, lung).
Bioavailability	Oral: ~75-85%.
Onset of Action	Oral: 1-3 hours; IV: immediate (within minutes).
Duration of Action	Oral: 6-8 hours; IV: 4-6 hours; clinical effect correlates with plasma concentration above MIC.

Classification & Brands

Dosing & administration

600 mg (base) orally every 8 hours for 7 days; or 10 mg/kg (base) intravenously loading dose over 1 hour, then 0.02 mg/kg/min continuous infusion for 3 days, then switch to oral.

Dosage form	TABLET, EXTENDED RELEASE
Renal impairment	GFR 30-60: reduce dose by 30%; GFR <30: use with caution, consider 50% dose reduction and monitor levels; hemodialysis: not removed, use 50% dose.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 25%; Child-Pugh C: contraindicated or reduce dose by 50% with close monitoring.
Pediatric use	Children: 10 mg/kg (base) orally every 8 hours for 7 days (max 600 mg/dose); IV: loading 10 mg/kg over 1 hour, then 0.02 mg/kg/min continuous (max 24-hour dose: 30 mg/kg).
Geriatric use	Initiate at lower end of dosing range (e.g., 400 mg orally every 8 hours) due to reduced renal function and increased risk of QT prolongation; monitor ECG and electrolytes.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for QUINATIME (QUINATIME).

Breastfeeding	Quinine is excreted into human breast milk in small amounts (M/P ratio ~0.1-0.3). Considered compatible with breastfeeding by the WHO; however, monitor infant for signs of hemolysis in G6PD-deficient infants. Benefit of treating maternal malaria outweighs minimal risk.
Teratogenic Risk	Quinine (active ingredient in QUINATIME) is classified as FDA Category D. First trimester: associated with congenital malformations including auditory nerve hypoplasia and limb defects; avoidance recommended unless treating life-threatening malaria. Second and third trimesters: risk of hypoglycemia and fetal distress; use only when benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Quinine may cause fatal hypersensitivity reactions including thrombocytopenia, hemolytic-uremic syndrome, and severe cutaneous adverse reactions. It is not recommended for prevention of malaria. Cardiac monitoring is required due to risk of arrhythmias.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to quinine or any of its components","G6PD deficiency (relative contraindication, use with caution)","Prolonged QT interval or known cardiac arrhythmias","Myasthenia gravis (may worsen symptoms)","Concurrent use with ritonavir or other potent CYP3A4 inhibitors (increases quinine toxicity)"]

Clinical Precautions

Precautions

["Cardiotoxicity: QT interval prolongation, torsades de pointes; avoid in patients with pre-existing cardiac conditions or concurrent QT-prolonging drugs.","Hypersensitivity: Can cause severe thrombocytopenia, hemolytic anemia, and anaphylaxis.","Hematologic effects: May induce hemolysis in G6PD-deficient patients.","Visual disturbances: Dose-related cinchonism (tinnitus, headache) and rare retinal toxicity with prolonged use.","Drug interactions: Inhibit CYP3A4 and CYP2D6; caution with warfarin, digoxin, and antimalarials."]

Clinical Tips & Counseling

Drug interactions

Loading safety data…

QUINATIME

Clinical safety rating: caution

Comprehensive clinical and safety monograph for QUINATIME (QUINATIME).

How it works

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 to 3-hydroxyquinine. Also metabolized by CYP2C19 and CYP2D6 to minor metabolites.
Excretion	Renal: ~20% unchanged; hepatic metabolism (CYP3A4) major route; biliary/fecal: ~80% as metabolites.
Half-life	Terminal elimination half-life 10-12 hours in healthy adults; prolonged in hepatic impairment.
Protein binding	80-85% bound primarily to albumin.
Volume of Distribution	2-3 L/kg; indicates extensive tissue distribution (e.g., liver, spleen, lung).
Bioavailability	Oral: ~75-85%.
Onset of Action	Oral: 1-3 hours; IV: immediate (within minutes).
Duration of Action	Oral: 6-8 hours; IV: 4-6 hours; clinical effect correlates with plasma concentration above MIC.

Classification & Brands

Dosing & administration

600 mg (base) orally every 8 hours for 7 days; or 10 mg/kg (base) intravenously loading dose over 1 hour, then 0.02 mg/kg/min continuous infusion for 3 days, then switch to oral.

Dosage form	TABLET, EXTENDED RELEASE
Renal impairment	GFR 30-60: reduce dose by 30%; GFR <30: use with caution, consider 50% dose reduction and monitor levels; hemodialysis: not removed, use 50% dose.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 25%; Child-Pugh C: contraindicated or reduce dose by 50% with close monitoring.
Pediatric use	Children: 10 mg/kg (base) orally every 8 hours for 7 days (max 600 mg/dose); IV: loading 10 mg/kg over 1 hour, then 0.02 mg/kg/min continuous (max 24-hour dose: 30 mg/kg).
Geriatric use	Initiate at lower end of dosing range (e.g., 400 mg orally every 8 hours) due to reduced renal function and increased risk of QT prolongation; monitor ECG and electrolytes.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for QUINATIME (QUINATIME).

Breastfeeding	Quinine is excreted into human breast milk in small amounts (M/P ratio ~0.1-0.3). Considered compatible with breastfeeding by the WHO; however, monitor infant for signs of hemolysis in G6PD-deficient infants. Benefit of treating maternal malaria outweighs minimal risk.
Teratogenic Risk	Quinine (active ingredient in QUINATIME) is classified as FDA Category D. First trimester: associated with congenital malformations including auditory nerve hypoplasia and limb defects; avoidance recommended unless treating life-threatening malaria. Second and third trimesters: risk of hypoglycemia and fetal distress; use only when benefit outweighs risk.