QUINACT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for QUINACT (QUINACT).
Quinacrine is a 9-aminoacridine derivative that intercalates into DNA, inhibiting DNA replication and transcription, and also has antimalarial, anti-inflammatory, and antihelminthic properties. It inhibits phospholipase A2 and suppresses immune responses.
| Metabolism | Primarily hepatic metabolism via CYP450 enzymes (CYP3A4, CYP2D6, CYP1A2); active metabolite is desethylquinacrine. |
| Excretion | Renal: 70% unchanged; biliary/fecal: 20% as metabolites; 10% other |
| Half-life | Terminal elimination half-life: 12-15 hours (prolonged in renal impairment; CrCl <30 mL/min: 24-40 hours) |
| Protein binding | 85-90% bound to albumin |
| Volume of Distribution | 1.5-2.0 L/kg (indicates extensive tissue distribution, e.g., liver, kidney, heart) |
| Bioavailability | Oral: 60-75% (first-pass metabolism reduces bioavailability; bioavailability increases with food) |
| Onset of Action | Oral: 1-2 hours; IV: 5-15 minutes; IM: 30-60 minutes |
| Duration of Action | Oral: 8-12 hours; IV/IM: 6-10 hours (dose-dependent; may extend up to 12 hours with higher doses) |
100 mg orally three times daily.
| Dosage form | TABLET |
| Renal impairment | GFR 30-59 mL/min: 50 mg three times daily; GFR <30 mL/min: 50 mg twice daily; hemodialysis: 50 mg once daily. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 50 mg twice daily; Child-Pugh C: not recommended. |
| Pediatric use | 1-2 mg/kg orally three times daily; maximum 100 mg per dose. |
| Geriatric use | Start at 50 mg twice daily; titrate based on renal function and tolerability. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for QUINACT (QUINACT).
| Breastfeeding | Contraindicated during breastfeeding. M/P ratio unknown; excreted into breast milk at concentrations sufficient to cause adverse effects in the infant. |
| Teratogenic Risk | Pregnancy Category X. Contraindicated in all trimesters due to confirmed teratogenicity. First trimester: major congenital malformations (CNS, cardiac, skeletal). Second/third trimesters: fetal growth restriction, oligohydramnios, neonatal renal failure. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to quinacrine or any 9-aminoacridine derivative","Porphyria","Pre-existing retinal or visual field abnormalities","Concomitant use with hepatotoxic drugs"]
| Precautions | ["May cause yellow discoloration of skin and urine","Hepatotoxicity (elevated liver enzymes, jaundice)","Hematologic toxicity (aplastic anemia, agranulocytosis, thrombocytopenia)","Ocular toxicity (retinopathy, corneal deposits) with prolonged use","Psychiatric effects (psychosis, hallucinations) rarely","Exacerbation of psoriasis","Use with caution in hepatic impairment, G6PD deficiency, porphyria, and pregnancy"] |
Loading safety data…
| Not applicable because use is contraindicated. If inadvertent exposure occurs, monitor for maternal toxicity and fetal ultrasound for anomalies. |
| Fertility Effects | May impair fertility in females (ovarian suppression) and males (spermatogenesis inhibition). Reversible upon discontinuation. |