Quinine Bisulphate Kent
Quinine Bisulphate Kent Uses, Dosage, Side Effects, Food Interaction and all others data.
Quinine Bisulphate Kent is a cinchona alkaloid and a 4-methanolquinoline. It rapidly acts on blood schizontocide by interfering with lysosomal function or nucleic acid synthesis in the Plasmodia spp. It has no activity against exoerythrocytic forms.
Quinine Bisulphate Kent is used parenterally to treat life-threatening infections caused by chloroquine-resistant Plasmodium falciparum malaria. Quinine Bisulphate Kent 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.
| Trade Name | Quinine Bisulphate Kent |
| Availability | Prescription only |
| Generic | Quinine |
| Quinine Other Names | (8S,9R)-quinine, 6'-Methoxycinchonidine, Chinin, Chinine, Chininum, Quinina, Quinine |
| Related Drugs | doxycycline, clindamycin, hydroxychloroquine, Plaquenil, Cleocin |
| Type | |
| Formula | C20H24N2O2 |
| Weight | Average: 324.4168 Monoisotopic: 324.183778022 |
| Protein binding | Approximately 70% |
| Groups | Approved |
| Therapeutic Class | Anti-malarial drugs |
| Manufacturer | |
| Available Country | United Kingdom |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Quinine Bisulphate Kent Sulfate, is an antimalarial drug used only for treatment of uncomplicated Plasmodium falciparum malaria. Quinine Bisulphate Kent sulfate has been shown to be effective in geographical regions where resistance to chloroquine has been documented
Quinine Bisulphate Kent Sulfate oral capsules are not approved for:
- Treatment of severe or complicated P. falciparum malaria.
- Prevention of malaria.
- Treatment or prevention of nocturnal leg cramps
Quinine Bisulphate Kent Dihydrochloride is used for the acute treatment of malaria. It may also be used in the treatment of Babesiosis in conjunction with clindamycin.
Quinine Bisulphate Kent is also used to associated treatment for these conditions: Malaria caused by Plasmodium falciparum
How Quinine Bisulphate Kent works
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.
Dosage
Quinine Bisulphate Kent dosage
Intravenous:
- Adult: Initially, 20 mg/kg to max 1.4 g over 4 hr with maintenance infusion started after 8 hr. Maintenance infusions: 10 mg/kg to max 700 mg over 4 hr 8 hrly. Loading dose should not be given if patient has received quinine, quinidine, halofantrine or mefloquine during the previous 24 hr.
- Child:≤5 mg/kg/hr by slow IV infusion.
Oral:
- Adult: 648 mg given every 8 hr for 7 days.
- Child: ≥8 yr10 mg/kg 8 hrly for 7 days.
Should be taken with food. Take with food to minimise GI discomfort.
Reconstitutions
Dilute in NaCl 0.9% to a concentration of diHCl 60-100 mg/mL.
Side Effects
Headache, nausea, disturbed vision, impaired hearing, tinnitus, abdominal pain, vomiting, diarrhoea, vertigo; flushing skin with intense pruritus, urticaria; fever, dyspnoea, agranulocytosis, palpitations, rashes; myalgia, muscle weakness, asthma, asthenia, disorientation, angioedema; haemoglobinuria; hypoprothrombinaemia, hypoglycaemia, hypotension, renal failure.
Toxicity
Quinine Bisulphate Kent is a documented causative agent of drug induced thrombocytopenia (DIT). Thrombocytopenia is a low amount of platelets in the blood. Quinine Bisulphate Kent induces production of antibodies against glycoprotein (GP) Ib-IX complex in the majority of cases of DIT, or more rarely, the platelet-glycoprotein complex GPIIb-IIIa. Increased antibodies against these complexes increases platelet clearance, leading to the observed thrombocytopenia.
Precaution
Patients with cardiac conduction defects, heart block or AF. Pregnancy and lactation.
Interaction
Reduced renal clearance of amantadine. Reduced clearance with cimetidine. Increased anticoagulant effect of warfarin and other anticoagulants. Reduced plasma levels of ciclosporin. Increased plasma levels of digoxin. Increased risk of myopathy and rhabdomyolysis with atorvastatin. May enhance hypoglycaemic effects of oral antidiabetics.
Food Interaction
- Take with food. Food reduces irritation.
[Minor] Coadministration with grapefruit juice does not appear to affect the pharmacokinetics of quinine in a clinically relevant manner.
Although grapefruit juice is an inhibitor of CYP450 3A4 and quinine is metabolized by this pathway to its major metabolite, 3-hydroxyquinine, a study of ten healthy volunteers found no significant differences in quinine peak plasma concentration (Cmax), time to reach Cmax (Tmax), terminal elimination half-life, systemic exposure (AUC), or apparent oral clearance (Cl Relative to the control period, the apparent renal clearance of quinine was markedly increased by 81% during treatment with half-strength grapefruit juice. However, since renal clearance accounts for approximately 6% of the total clearance of quinine, this change would likely have minimal clinical impact. The lack of a significant interaction is probably due to the fact that grapefruit juice primarily inhibits intestinal rather than hepatic CYP450 3A4, and quinine is not known to undergo significant presystemic metabolism as evidenced by its relatively high oral bioavailability (76% to 88%). Nevertheless, excessive consumption of grapefruit juice and tonic water (which contains quinine) was suspected as the cause of torsade de pointes arrhythmia in a patient with a history of asymptomatic long QT syndrome. Treatment with magnesium sulfate and metoprolol had no effect, but the arrhythmia resolved spontaneously 48 hours after discontinuation of the drinks. Based on current data, moderate grapefruit juice consumption is probably safe for the majority of patients taking quinine.
Quinine Bisulphate Kent Drug Interaction
Moderate: fluticasone / salmeterol, duloxetine, budesonide / formoterolUnknown: aspirin, diphenhydramine, calcium / vitamin d, celecoxib, rosuvastatin, omega-3 polyunsaturated fatty acids, fluticasone nasal, atorvastatin, pregabalin, esomeprazole, acetaminophen, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, cetirizine
Quinine Bisulphate Kent Disease Interaction
Major: QT prolongation, G-6-PD deficiency, myasthenia gravis, ocular toxicity, thrombocytopenia, tinnitusModerate: liver impairment, renal impairment
Volume of Distribution
- 1.43 ± 0.18 L/kg [Healthy Pediatric Controls]
- 0.87 ± 0.12 L/kg [P. falciparum Malaria Pediatric Patients]
- 2.5 to 7.1 L/kg [healthy subjects who received a single oral 600 mg dose]
Elimination Route
76 - 88%
Half Life
Approximately 18 hours
Clearance
- 0.17 L/h/kg [healthy]
- 0.09 L/h/kg [patients with uncomplicated malaria]
- 18.4 L/h [healthy adult subjects with administration of multiple-dose activated charcoal]
- 11.8 L/h [healthy adult subjects without administration of multiple-dose activated charcoal]
- Oral cl=0.06 L/h/kg [elderly subjects]
Elimination Route
Quinine Bisulphate Kent is eliminated primarily via hepatic biotransformation. Approximately 20% of quinine is excreted unchanged in urine.
Pregnancy & Breastfeeding use
Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Contraindication
Hypersensitivity to quinine, mefloquine or quinidine. Patients with nocturnal leg cramps; prolonged QT interval, tinnitus or optic neuritis, myasthenia gravis, G6PD deficiency, haemolysis and who had suffered from blackwater fever. Concomitant use with ritonavir, mefloquine, rifampicin, class IA and class III antiarrhythmic agents, neuromuscular blocking agents, other drugs known to cause QT prolongation, and Al- and/or Mg-containing antacids.
Special Warning
Renal Impairment:
- Oral:Severe: Initially, 648 mg followed after 12 hr by maintenance doses of 324 mg 12 hrly.
- Intravenous: Severe: Reduce maintenance dose to 5-7 mg/kg of quinine salt 8 hrly.
Hepatic Impairment:
- Mild to moderate: No dosage adjustment needed.
- Intravenous: Severe: Reduce maintenance dose to 5-7 mg/kg of quinine salt 8 hrly.
Acute Overdose
Symptoms: GI effects, CNS disturbances, oculotoxicity, cardiotoxicity,; tinnitus, abdominal pain, diarrhoea, vertigo, pulmonary oedema, hypotension, sweating, flushing, nausea, vomiting, headache, slightly disturbed vision, deafness, vasodilatation and adult resp distress syndrome.
Management: Administer multiple dose of activated charcoal within 1 hr or perform gastric lavage. Symptomatic (e.g. maintaining BP, respiration and renal function, treating arrhythmias) and supportive treatment.
Storage Condition
Store between 20-25° C. Protect from light.
Innovators Monograph
You find simplified version here Quinine Bisulphate Kent
Quinine Bisulphate Kent contains Quinine see full prescribing information from innovator Quinine Bisulphate Kent Monograph, Quinine Bisulphate Kent MSDS, Quinine Bisulphate Kent FDA label
FAQ
What is Quinine Bisulphate Kent used for?
Quinine Bisulphate Kent is used to treat malaria caused by Plasmodium falciparum. Plasmodium falciparum is a parasite that gets into the red blood cells in the body and causes malaria.
How safe is Quinine Bisulphate Kent?
Experts consider Quinine Bisulphate Kent safe to consume in small doses.The FDA also specify that manufacturers must place Quinine Bisulphate Kent on the label for consumers to easily see.
How does Quinine Bisulphate Kent work?
Quinine Bisulphate Kent works by killing the parasite or preventing it from growing.
What are the common side effects of Quinine Bisulphate Kent?
Common side effects of Quinine Bisulphate Kent are include:
- nausea.
- restlessness.
- difficulty hearing or ringing in the ears.
- confusion.
- nervousness.
Is Quinine Bisulphate Kent safe during pregnancy?
You should not avoid taking Quinine Bisulphate Kent because you are pregnant. The risk of harm to you and your baby from malaria is likely to be far greater than any possible risk from taking quinine. There is no convincing scientific evidence that Quinine Bisulphate Kent is harmful to an unborn baby.
Is Quinine Bisulphate Kent safe during breastfeeding?
Because of the low levels of Quinine Bisulphate Kent in breastmilk, amounts ingested by the infant are small and would not be expected to cause any adverse effects in breastfed infants. The dosage in milk is far below those required to treat an infant for malaria.
Can I drive after taking Quinine Bisulphate Kent?
Quinine Bisulphate Kent may cause blurred vision and may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert and able to see clearly. Do not use to treat any condition that has not been checked by your doctor.
When should be best taken of Quinine Bisulphate Kent?
Quinine Bisulphate Kent usually is taken with food three times a day (every 8 hours) for 3 to 7 days. Take Quinine Bisulphate Kent at around the same times every day.
How much Quinine Bisulphate Kent can I take daily?
Adults and children 16 years of age and older 648 milligrams (mg) (2 capsules) every 8 hours for 7 days. Children younger than 16 years of age Use and dose must be determined by your doctor.
How long does it take for Quinine Bisulphate Kent tablets to work?
A reduction in frequency of leg cramps may take up to 4 weeks to become apparent. Patients should be monitored closely during the early stages of treatment for adverse effects. After an initial trial of 4 weeks, treatment should be stopped if there is no benefit.
How long until Quinine Bisulphate Kent is out of my system?
The limit of sensitivity for quinine in urine, utilizing TLC, is approximately 0.2mg/mL. Laboratory experience indicates that Quinine Bisulphate Kent may be detected as long as 4 to 5 days after intake.
Can I take Quinine Bisulphate Kent for a long time?
Long-term off-label use of Quinine Bisulphate Kent, still prescribed to individuals with muscle cramps despite Food and Drug Administration warnings of adverse events, is associated with an increased risk of death.
When should I stop taking Quinine Bisulphate Kent?
Stop taking Quinine Bisulphate Kent and call your doctor at once if you have headache with chest pain and severe dizziness, fast or pounding heartbeats, unusual bruising or bleeding, signs of infection, severe lower back pain, or blood in your urine.
Is Quinine Bisulphate Kent bad for liver?
The hepatotoxicity of Quinine Bisulphate Kent is usually mild and resolves within 1 to 4 weeks of stopping. In many instances, jaundice and liver test abnormalities may worsen for a few days after stopping Quinine Bisulphate Kent, but fatalities have not been reported, and recovery is usually rapid.
Can I just stop taking Quinine Bisulphate Kent?
After an initial trial of 4 weeks, treatment should be stopped if there is no benefit. Treatment should be interrupted approximately every 3 months to reassess the benefit. In patients taking Quinine Bisulphate Kent long term, a trial discontinuation may be considered.
How often can I take Quinine Bisulphate Kent ?
Adults and children aged 12 years and over, 600mg every eight hours for 7 days.
Does Quinine Bisulphate Kent raise blood pressure?
This tea has been used in folk medicine to treat a variety of problems, and scientists have confirmed that it lowers blood pressure as well as cholesterol.
How does Quinine Bisulphate Kent work in the body?
brank works by killing the parasite or preventing it from growing.
Is Quinine Bisulphate Kent bad for heart?
Quinine Bisulphate Kent can cause serious side effects on your heart, kidneys, or blood cells.
Does Quinine Bisulphate Kent make me sleepy?
Quinine Bisulphate Kent may cause hypoglycemia.
What happens if I miss a dose of Quinine Bisulphate Kent?
Take the Quinine Bisulphate Kent of dose as soon as you remember. If you are more than 4 hours late for your dose, skip the missed dose and take the medicine at your next scheduled dose time. Do not take extra medicine to make up the missed dose.
Who should not take Quinine Bisulphate Kent?
You should not take Quinine Bisulphate Kent if you have a heart rhythm disorder called Long QT syndrome, a genetic enzyme deficiency called glucose-6-phosphate dehydrogenase deficiency, myasthenia gravis, optic neuritis (inflammation of the nerves in your eyes), if you have taken Quinine Bisulphate Kent in the past and it caused a blood cell disorder or severe bleeding.
What happen if I overdose on Quinine Bisulphate Kent?
Symptoms of overdose may include are sudden vision change, confusion, severe trouble hearing, fast/irregular heartbeat, fainting, slow/shallow breathing, seizures, inability to wake up (coma).
