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quinine (Qualaquin)

 

Classes: Antimalarials

Dosing and uses of Qualaquin (quinine)

 

Adult dosage forms and strengths

capsule

  • 324mg

 

Malaria

Uncomplicated (P. falciparum)

  • 648 mg PO q8hr x 7 days

Chloroquine -Resistant (P. falciparum)

  • 648 mg PO q8hr x 3-7 days with concomitant tetracycline, doxycycline, or clindamycin

Chloroquine-Resistant (P. vivax)

  • 648 mg PO q8hr x 3-7 days with concomitant doxycycline (or tetracycline) and PO primaquine

 

Babesiosis

648 mg PO q8hr x 7 days, with concomitant PO or IV clindamycin

 

Dosage modifications

Severe, chronic renal impairment: 648 mg PO once, then 324 mg PO q12hr

Hepatic impairment

  • Mild or moderate (Child-Pugh A or B): No dosage adjustment required; monitor closely
  • Severe (Child-Pugh C): Do not administer

 

Pediatric dosage forms and strengths

capsule

  • 324mg

 

Malaria

Uncomplicated (P. falciparum)

  • 30 mg/kg/day PO divided TID x 3–7 days
  • Should not exceed the usual adult PO dosage.

Chloroquine-Resistant (P. falciparum)

  • 30 mg/kg/day PO divided TID x3-7 days, with concomitant doxycycline, tetracycline or clindamycin
  • Should not exceed the usual adult PO dosage.

Chloroquine-Resistant (P. vivax)

  • 30 mg/kg/day PO TID x 3–7 days, with concomitant doxycyline & PO primaquine
  • Should not exceed the usual adult PO dosage.

 

Babesiosis (Off-label)

25 mg/kg/day PO divided TID x7 days, with concomitant oral clindamycin

 

Qualaquin (quinine) adverse (side) effects

<1%

Flushing of the skin

Anginal symptoms

Fever

Rash

Pruritus

Hypoglycemia

Epigastric pain

Hemolysis in G6PD deficiency

Thrombocytopenia

Hepatitis

Nightblindness

Diplopia

Optic atrophy

Impaired hearing

Hypersensitivity reaction

 

Frequency not defined

Severe headache

Nausea

Vomiting

Diarrhea

Blurred vision

Tinnituscinchonism (risk of cinchonism is directly related to dose and duration of therapy)

 

Warnings

Black box warnings

Limited or no benefit for treatment/prevention of nocturnal leg cramps

May cause serious and life-threatening hematologic reactions, including thrombocytopenia and hemolytic uremic syndrome/thrombotic thrombocytopenic purpura (HUS/TTP)

Chronic renal impairment associated with the development of TTP has been reported

 

Contraindications

Hypersensitivity

G6PD deficiency

Optic neuritis, tinnitus, history of quinine-associated blackwater fever and thrombocytopenic purpura

Pregnancy

 

Cautions

Reduce parenteral dose by half if >48 hr parenteral treatment required; monitor EKG, BP, glucose with parenteral treatment

FDA warns against unapproved use for leg cramps because of unpredictable serious and life-threatening hematologic reactions including thrombocytopenia and hemolytic-uremic syndrome/thrombotic thrombocytopenic purpura (HUS/TTP)

QT prolongation

  • Concentration-dependent prolongation of the PR and QRS interval observed
  • At particular risk are patients with underlying structural heart disease and preexisting conduction system abnormalities, elderly patients with sick sinus syndrome, patients with atrial fibrillation with slow ventricular response, patients with myocardial ischemia or patients receiving drugs known to prolong the PR interval (eg, verapamil) or QRS interval (eg, flecainide or quinidine)

 

Pregnancy and lactation

Pregnancy category: X (first trimester)

Lactation: enters breast milk

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Qualaquin (quinine)

Absorption: readily, mainly from upper small intestine

Protein Bound: 70-95%

Metabolism: primarily hepatic

Half-life elimination: children: 6-12 hr; adults: 8-14 hr

Peak Plasma Time: 1-3 hr

Excretion: feces & saliva; urine (<5% as unchanged drug)

 

Mechanism of action

Unknown; may disrupt Plasmodium DNA transcription/replication

 

Administration

IV Administration

Was administered by slow IV infusion as the dihydrochloride; however, a parenteral dosage form of the drug no longer is available in the Us