Drug information of Quinine

Mechanism of effect

The theorized mechanism of action for quinine and related anti-malarial drugs is that these drugs are toxic to the malaria parasite. Specifically, the drugs interfere with the parasite's ability to break down and digest hemoglobin. Consequently, the parasite starves and/or builds up toxic levels of partially degraded hemoglobin in itself.

Pharmacodynamic

Quinine is used parenterally to treat life-threatening infections caused by chloroquine-resistant Plasmodium falciparum malaria. Quinine acts as a blood schizonticide although it also has gametocytocidal activity against P. vivax and P. malariae. Because it is a weak base, it is concentrated in the food vacuoles of P. falciparum. It is thought to act by inhibiting heme polymerase, thereby allowing accumulation of its cytotoxic substrate, heme. As a schizonticidal drug, it is less effective and more toxic than chloroquine. However, it has a special place in the management of severe falciparum malaria in areas with known resistance to chloroquine.

Pharmacokinetics

Absorption: 76 - 88% 

Protein binding: Approximately 70%

Metabolism: Hepatic, over 80% metabolized by the liver

Half-life: Approximately 18 hours

Drug indications

malaria

malaria

Dosage

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

Drug contraindications

Hypersensitivity , ECG prolonged QT , Myasthenia gravis

Prolonged QT interval

Hypersensitivity; cross-sensitivity with mefloquine or quinidine

G6PD deficiency

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

Thrombocytopenia

Hemolytic uremic syndrome

Blackwater fever

Myasthenia gravis

Optic neuritis

Side effects

flushing

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

Interactions

Succinylcholine , Carbamazepine , ritonavir , Dolasetron , vandetanib , Succinylcholine Chloride , Atracurium , Ondansetron , Enoxaparin , Pimozide , Topotecan , Thioridazine , Bremelanotide , MICRORELIN , Fluticasone and Vilanterol , lefamulin , fondaparinux , vortioxetine , voxelotor , Venetoclax , Entrectinib , Bemiparin , Lorlatinib , glasdegib , Eliglustat , lasmiditan , Erdafitinib , Antithrombin alfa , Apalutamide , encorafenib , pexidartinib , ivosidenib , Idelalisib , Ivacaftor , Rocuronium , Lumacaftor , Antithrombin III , Rapacuronium , Afatinib , pomalidomide , vemurafenib , Chloroquine , Ribociclib , Eribulin , Vecuronium , Nefazodone , dronedarone , Phenindione , Bivalirudin , Argatroban , Dapsone , Cis atracurium , Heparin , Hydroxychloroquine , Warfarin , Colchicine , sparfloxacin , Mefloquine , Dofetilide , brigatinib , Dalteparin , Tinzaparin , lumacaftor and Ivacaftor , Halofantrine , Grepafloxacin , Terfenadine , Alfuzosin , Edoxaban , Sodium lactate , Troleandomycin , Glycerol Phenylbutyrate , riociguat , Bepridil , bedaquiline , talazoparib , vemurafenib , Fidaxomicin , secukinumab

Contraindicated (5)

• dronedarone
• eliglustat
• lefamulin
• pimozide
• thioridazine

Serious - Use Alternative (61)

• afatinib
• alfuzosin
• antithrombin alfa
• antithrombin III
• apalutamide
• argatroban
• atracurium
• bemiparin
• bivalirudin
• bremelanotide
• brigatinib
• chloroquine
• cisatracurium
• colchicine
• dalteparin
• dapsone topical
• edoxaban
• encorafenib
• enoxaparin
• entrectinib
• erdafitinib
• eribulin
• fondaparinux
• glasdegib
• heparin
• hydroxychloroquine sulfate
• idelalisib
• ivosidenib
• lasmiditan
• lorlatinib
• lumacaftor/ivacaftor
• macimorelin
• mefloquine
• nefazodone
• onabotulinumtoxinA
• ondansetron
• pancuronium
• pexidartinib
• phenindione
• pitolisant
• pomalidomide
• protamine
• rapacuronium
• ribociclib
• rimegepant
• riociguat
• ritonavir
• rocuronium
• siponimod
• succinylcholine
• topotecan
• tucatinib
• umeclidinium bromide/vilanterol inhaled
• vandetanib
• vecuronium
• vemurafenib
• venetoclax
• vilanterol/fluticasone furoate inhaled
• vortioxetine
• voxelotor
• warfarin

Alerts

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

Points of recommendation

Before using this medication, tell your doctor or pharmacist your medical history, especially of: previous serious side effects with quinine (such as blood problems), family/personal history of a certain enzyme problem (glucose-6-phosphate dehydrogenase deficiency-G6PD), a certain eye nerve problem (optic neuritis), hearing problems (such as ringing in the ears), a certain nerve/muscle disease (myasthenia gravis), heart rhythm problems (such as atrial fibrillation/flutter), kidney problems, liver problems.

This drug may make you dizzy or blur your vision. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness or clear vision until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).

Quinine may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.

The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using quinine, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).

Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using quinine safely.

Pregnancy level

No evidence that quinine causes uterine contractions at doses recommended for malaria treatment

Breast feeding warning

Low levels of quinine in breastmilk; amounts ingested by infant are small and would not be expected to cause any adverse effects

 

Related drugs

Pyrimethamine , primaquine , Chloroquine , Mefloquine , Lumefantrine / artemether , Halofantrine , Atovaquone