Quinoctal Uses

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What is Quinoctal?

Quinoctal is used to treat malaria, a disease caused by parasites. Parasites that cause malaria typically enter the body through the bite of a mosquito. Malaria is common in areas such as Africa, South America, and Southern Asia.

Quinoctal will not treat severe forms of malaria, and it should not be taken to prevent malaria. Quinoctal also should not be taken to treat or prevent night-time leg cramps.

Using this medication improperly or without the advice of a doctor can result in serious side effects or death. Quinoctal is approved for use only in treating malaria. Some people have used Quinoctal to treat leg cramps, but this is not an FDA-approved use.

The U.S. Food and Drug Administration has banned the sale of all non-approved brands of Quinoctal. As of December 2006, Quinoctal is the only brand of Quinoctal that is approved by the FDA.

Quinoctal may also be used for purposes not listed in this medication guide.

Quinoctal indications

An indication is a term used for the list of condition or symptom or illness for which the medicine is prescribed or used by the patient. For example, acetaminophen or paracetamol is used for fever by the patient, or the doctor prescribes it for a headache or body pains. Now fever, headache and body pains are the indications of paracetamol. A patient should be aware of the indications of medications used for common conditions because they can be taken over the counter in the pharmacy meaning without prescription by the Physician.
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Oral

Malaria

Adult: As sulfate: 648 mg 8 hrly for 7 days.

Child: As sulfate: ≥8 yr10 mg/kg 8 hrly for 7 days.

Renal impairment: Severe: Initially, 648 mg followed after 12 hr by maintenance doses of 324 mg 12 hrly.

Hepatic impairment: Mild to moderate (Child-Pugh class A and B): No dosage adjustment needed.

Reconstitution: Dilute in NaCl 0.9% to a concentration of diHCl 60-100 mg/mL.

Intravenous

Malaria

Adult: As diHCl: Initially, 20 mg/kg to max 1.4 g over 4 hr w/ 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 received Quinoctal, quinidine, halofantrine or mefloquine during the previous 12 hr.

Child: ≤5 mg/kg/hr by slow IV infusion.

Renal impairment: Severe: Reduce maintenance dose to 5-7 mg/kg of Quinoctal salt 8 hrly.

Hepatic impairment: Mild to moderate (Child-Pugh class A and B): No dosage adjustment needed. Severe: Reduce maintenance dose to 5-7 mg/kg of Quinoctal salt 8 hrly.

Reconstitution: Dilute in NaCl 0.9% to a concentration of diHCl 60-100 mg/mL.

How should I use Quinoctal?

Use Quinoctal capsules as directed by your doctor. Check the label on the medicine for exact dosing instructions.

Ask your health care provider any questions you may have about how to use Quinoctal capsules.

Uses of Quinoctal in details

There are specific as well as general uses of a drug or medicine. A medicine can be used to prevent a disease, treat a disease over a period or cure a disease. It can also be used to treat the particular symptom of the disease. The drug use depends on the form the patient takes it. It may be more useful in injection form or sometimes in tablet form. The drug can be used for a single troubling symptom or a life-threatening condition. While some medications can be stopped after few days, some drugs need to be continued for prolonged period to get the benefit from it.
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Use: Labeled Indications

Malaria, uncomplicated, due to Plasmodium falciparum (treatment): Treatment of uncomplicated chloroquine-resistant P. falciparum malaria, in combination with other antimalarial agents

Off Label Uses

Babesiosis

Clinical experience suggests the utility of Quinoctal (in combination with clindamycin) for the treatment of Babesia microti infection.

Based on the Infectious Diseases Society of America (IDSA) guidelines for the Clinical Assessment, Treatment, and Prevention of Lyme Disease, Human Granulocytic Anaplasmosis, and Babesiosis, Quinoctal (in combination with clindamycin) is an effective and recommended initial therapy in the treatment of babesiosis.

Malaria, uncomplicated, due to Plasmodium vivax (treatment)

Based on the Centers for Disease Control and Prevention (CDC) Guidelines for Treatment of Malaria in the United States, Quinoctal (in combination with other antimalarial agents) is effective and recommended in the treatment of uncomplicated chloroquine-resistant P. vivax malaria.

Quinoctal description

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An alkaloid derived from the bark of the cinchona tree. It is used as an antimalarial drug, and is the active ingredient in extracts of the cinchona that have been used for that purpose since before 1633. Coco-Quinoctal is also a mild antipyretic and analgesic and has been used in common cold preparations for that purpose. It was used commonly and as a bitter and flavoring agent, and is still useful for the treatment of babesiosis. Coco-Quinoctal is also useful in some muscular disorders, especially nocturnal leg cramps and myotonia congenita, because of its direct effects on muscle membrane and sodium channels. The mechanisms of its antimalarial effects are not well understood.

Quinoctal dosage

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule,

Oral, as sulfate:

Quinoctal: 324 mg

Generic: 324 mg

Dosing: Adult

Note: Dosage expressed in terms of the salt; 1 capsule Quinoctal = 324 mg of Quinoctal = 269 mg of base; Canadian products contain 200 mg of Quinoctal = 167 mg of base or 300 mg of Quinoctal = 250 mg of base.

Malaria, uncomplicated, due to chloroquine-resistant P. falciparum (treatment):

Oral:

CDC guidelines: 648 mg every 8 hours, in combination with doxycycline, tetracycline, or clindamycin (preferred in pregnancy). Note: Administer Quinoctal for 3 days unless the infection was acquired in Southeast Asia, in which case Quinoctal duration of therapy is 7 days. Duration of concomitant agent is 7 days, regardless of geographic region (CDC 2013).

Canadian product: 600 mg every 8 hours for 3 to 7 days. Note: Use in combination with tetracycline, doxycycline, or clindamycin.

Malaria, uncomplicated, due to chloroquine-resistant P. vivax (treatment) (off-label use):

Oral: 648 mg every 8 hours, in combination with doxycycline or tetracycline plus primaquine. Note: Quinoctal in combination with clindamycin is an alternative regimen for pregnant patients. Administer Quinoctal for 3 days unless the infection was acquired in Southeast Asia, in which case Quinoctal duration of therapy is 7 days. Duration of concomitant agent is 7 days (doxycycline, tetracycline, clindamycin) or 14 days (primaquine), regardless of geographic region (CDC 2013).

Babesiosis (off-label use):

Oral: 650 mg every 6 to 8 hours for at least 7 to 10 days with clindamycin (Vannier 2012; Wormser 2006). Relapsing infection may require at least 6 weeks of therapy (Vannier 2012). Note: US manufactured Quinoctal capsule is 324 mg; 2 capsules (648 mg Quinoctal) should be sufficient for adult dosing.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Note: Dosage expressed in terms of the Quinoctal salt; 324 mg capsule Quinoctal = 269 mg of base. Canadian products: 200 mg capsule of Quinoctal = 167 mg of base or 300 mg capsule of Quinoctal = 250 mg of base.

Malaria: Children and Adolescents; regardless of HIV status (HHS [OI pediatric 2013]): Limited data available in ages <16 years: Note: Duration of Quinoctal treatment for malaria dependent upon the geographic region or pathogen. Lack of an appropriate Quinoctal dosage form may restrict use in some smaller patients.

P. falciparum (chloroquine resistant), uncomplicated; treatment:

Oral: 10 mg/kg/dose Quinoctal every 8 hours for 3 to 7 days depending on region; maximum dose: 650 mg/dose; use in combination with tetracycline, doxycycline, or clindamycin (dependent upon patient age) (CDC 2013)

P. vivax (chloroquine resistant), uncomplicated; treatment:

Oral: 10 mg/kg/dose Quinoctal every 8 hours for 3 to 7 days depending on region; maximum dose: 650 mg/dose; use in combination with primaquine and tetracycline or doxycycline (dependent upon patient age) (CDC 2013)

Severe malaria:

Oral Quinoctal, using the regimens previously described (dose and duration), may be used following IV quinidine including antimicrobial regimen once parasite density is <1% and patient is able to tolerate oral medications (CDC 2013)

Babesiosis: Limited data available: Children and Adolescents:

Oral: 10 mg/kg/dose Quinoctal every 8 hours for 7 to 10 days; maximum dose: 650 mg/dose (Red Book [AAP 2015]; Wittner 1982); use in combination with clindamycin as a first-line treatment option (IDSA [Wormser 2006])

Quinoctal interactions

See also:
What other drugs will affect Quinoctal?

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Effects Of Drugs And Other Substances On Quinoctal Pharmacokinetics

Quinoctal is a P-gp substrate and is primarily metabolized by CYP3A4. Other enzymes, including CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP2E1 may contribute to the metabolism of Quinoctal.

Antacids

Antacids containing aluminum and/or magnesium may delay or decrease absorption of Quinoctal. Concomitant administration of these antacids with Quinoctal should be avoided.

Antiepileptics (AEDs) (carbamazepine, phenobarbital, and phenytoin)

Carbamazepine, phenobarbital, and phenytoin are CYP3A4 inducers and may decrease Quinoctal plasma concentrations if used concurrently with Quinoctal.

Cholestyramine

In 8 healthy subjects who received Quinoctal 600 mg with or without 8 grams of cholestyramine resin, no significant difference in Quinoctal pharmacokinetic parameters was seen.

Cigarette Smoking (CYP1A2 inducer)

In healthy male heavy smokers, the mean Quinoctal AUC following a single 600 mg dose was 44% lower, the mean Cmax was 18% lower, and the elimination half-life was shorter (7.5 hours versus 12 hours) than in their non-smoking counterparts. However, in malaria patients who received the full 7-day course of Quinoctal therapy, cigarette smoking produced only a 25% decrease in median Quinoctal AUC and a 16.5% decrease in median Cmax, suggesting that the already reduced clearance of Quinoctal in acute malaria could have diminished the metabolic induction effect of smoking. Because smoking did not appear to influence the therapeutic outcome in malaria patients, it is not necessary to increase the dose of Quinoctal in the treatment of acute malaria in heavy cigarette smokers.

Grapefruit juice (P-gp/CYP3A4 inhibitor)

In a pharmacokinetic study involving 10 healthy subjects, the administration of a single 600 mg dose of Quinoctal with grapefruit juice (full-strength or half-strength) did not significantly alter the pharmacokinetic parameters of Quinoctal. Quinoctal may be taken with grapefruit juice.

Histamine H2-receptor blockers [cimetidine, ranitidine (nonspecific CYP450 inhibitors)]

In healthy subjects who were given a single oral 600 mg dose of Quinoctal after pretreatment with cimetidine (200 mg three times daily and 400 mg at bedtime for 7 days) or ranitidine (150 mg twice daily for 7 days), the apparent oral clearance of Quinoctal decreased and the mean elimination half-life increased significantly when given with cimetidine but not with ranitidine. Compared to untreated controls, the mean AUC of Quinoctal increased by 20% with ranitidine and by 42% with cimetidine (p < 0.05) without a significant change in mean Quinoctal Cmax. When Quinoctal is to be given concomitantly with a histamine H2-receptor blocker, the use of ranitidine is preferred over cimetidine. Although cimetidine and ranitidine may be used concomitantly with Quinoctal, patients should be monitored closely for adverse events associated with Quinoctal.

Isoniazid

Isoniazid 300 mg/day pretreatment for 1 week did not significantly alter the pharmacokinetic parameter values of Quinoctal. Adjustment of Quinoctal dosage is not necessary when isoniazid is given concomitantly.

Ketoconazole (CYP3A4 inhibitor)

In a crossover study, healthy subjects (N=9) who received a single oral dose of Quinoctal hydrochloride (500 mg) concomitantly with ketoconazole (100 mg twice daily for 3 days) had a mean Quinoctal AUC that was higher by 45% and a mean oral clearance of Quinoctal that was 31% lower than after receiving Quinoctal alone. Although no change in the Quinoctal dosage regimen is necessary with concomitant ketoconazole, patients should be monitored closely for adverse reactions associated with Quinoctal.

Macrolide Antibiotics (erythromycin, troleandomycin) (CYP3A4 inhibitors)

In a crossover study (N=10), healthy subjects who received a single oral 600 mg dose of Quinoctal with the macrolide antibiotic, troleandomycin (500 mg every 8 hours) exhibited a 87% higher mean Quinoctal AUC, a 45% lower mean oral clearance of Quinoctal, and a 81% lower formation clearance of the main metabolite, 3-hydroxyquinine, than when Quinoctal was given alone.

Erythromycin was shown to inhibit the in vitro metabolism of Quinoctal in human liver microsomes, an observation confirmed by an in vivo interaction study. In a crossover study (N=10), healthy subjects who received a single oral 500 mg dose of Quinoctal with erythromycin (600 mg every 8 hours for four days) showed a decrease in Quinoctal oral clearance (CL/F), an increase in half-life, and a decreased metabolite (3hydroxyquinine) to Quinoctal AUC ratio, as compared to when Quinoctal was given with placebo.

Therefore, concomitant administration of macrolide antibiotics such as erythromycin or troleandomycin with Quinoctal should be avoided.

Oral Contraceptives (estrogen, progestin)

In 7 healthy females who were using single-ingredient progestin or combination estrogen-containing oral contraceptives, the pharmacokinetic parameters of a single 600 mg dose of Quinoctal were not altered in comparison to those observed in 7 age-matched female control subjects not using oral contraceptives.

Rifampin (CYP3A4 inducer)

In patients with uncomplicated P. falciparum malaria who received Quinoctal 10 mg/kg concomitantly with rifampin 15 mg/kg/day for 7 days (N=29), the median AUC of Quinoctal between days 3 and 7 of therapy was 75% lower as compared to those who received Quinoctal monotherapy. In healthy subjects (N=9) who received a single oral 600 mg dose of Quinoctal after 2 weeks of pretreatment with rifampin 600 mg/day, the mean Quinoctal AUC and Cmax decreased by 85% and 55%, respectively. Therefore, the concomitant administration of rifampin with Quinoctal should be avoided.

Ritonavir

In healthy subjects who received a single oral 600 mg dose of Quinoctal with the 15 dose of ritonavir (200 mg every 12 hours for 9 days), the mean ritonavir AUC, Cmax, and elimination half-life were slightly but not significantly increased compared to when ritonavir was given alone. However, due to the significant effect of ritonavir on Quinoctal pharmacokinetics, the concomitant administration of Quinoctal capsules with ritonavir should be avoided.

Theophylline Or Aminophylline (CYP1A2 substrate)

In 19 healthy subjects who received multiple doses of Quinoctal 648 mg every 8 hours x 7 days with a single 300 mg oral dose of theophylline, the mean theophylline AUC was 10% lower than when theophylline was given alone. There was no significant effect on mean theophylline Cmax. Therefore, if Quinoctal is co-administered to patients receiving theophylline or aminophylline, plasma theophylline concentrations should be monitored frequently to ensure therapeutic concentrations.

Warfarin And

Oral Anticoagulants

Cinchona alkaloids, including Quinoctal, may have the potential to depress hepatic enzyme synthesis of vitamin K-dependent coagulation pathway proteins and may enhance the action of warfarin and other oral anticoagulants. Quinoctal may also interfere with the anticoagulant effect of heparin. Thus, in patients receiving these anticoagulants, the prothrombin time (PT), partial thromboplastin time (PTT), or international normalization ratio (INR) should be closely monitored as appropriate, during concurrent therapy with Quinoctal.

Drug/Laboratory Interactions

Quinoctal may produce an elevated value for urinary 17-ketogenic steroids when the Zimmerman method is used.

Quinoctal may interfere with urine qualitative dipstick protein assays as well as quantitative methods (e.g., pyrogallol red-molybdate).

Quinoctal side effects

See also:
What are the possible side effects of Quinoctal?

Applies to Quinoctal: oral capsule, oral tablet, oral tablet extended release

As well as its needed effects, Quinoctal (the active ingredient contained in Quinoctal) may cause unwanted side effects that require medical attention.

Major Side Effects

If any of the following side effects occur while taking Quinoctal, check with your doctor immediately:

More common:

Less common: Rare

If any of the following symptoms of overdose occur while taking Quinoctal, get emergency help immediately:

Symptoms of an overdose

Quinoctal contraindications

See also:
What is the most important information I should know about Quinoctal?

Quinoctal Capsules are contraindicated in patients with the following:

Prolonged QT interval. One case of a fatal ventricular arrhythmia was reported in an elderly patient with a prolonged QT interval at baseline, who received Quinoctal intravenously for P. falciparum malaria.
Glucose-6-phosphate dehydrogenase (G6PD) deficiency.
Hemolysis can occur in patients with G6PD deficiency receiving Quinoctal.
Known hypersensitivity reactions to Quinoctal.
These include, but are not limited to, the following :
Thrombocytopenia
Idiopathic thrombocytopenia purpura (ITP) and Thrombotic thrombocytopenic purpura (TTP)
Hemolytic uremic syndrome (HUS)
Blackwater fever (acute intravascular hemolysis, hemoglobinuria, and hemoglobinemia)
Known hypersensitivity to mefloquine or quinidine: cross-sensitivity to Quinoctal has been documented.
Myasthenia gravis. Quinoctal has neuromuscular blocking activity, and may exacerbate muscle weakness.
Optic neuritis. Quinoctal may exacerbate active optic neuritis.



Active ingredient matches for Quinoctal:

Quinine in Australia.

Quinine sulfate in Australia.


List of Quinoctal substitutes (brand and generic names)

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Unit description / dosage (Manufacturer)Price, USD
Injectable; Injection; Quinine Formate Basic 500 mg (Sanofi synthelabo)
QUINOLOD 300MG INJECTION 1 vial / 2 ML injection each (Wockhardt Ltd)$ 0.23
QUINOLOD 300MG TABLET 1 strip / 10 tablets each (Wockhardt Ltd)$ 0.59
Quinolod 300mg Tablet (Wockhardt Ltd)$ 0.06
QUINOMAC 100MG SUSPENSION 1 bottle / 60 ML suspension each (Macleods Pharmaceuticals Pvt Ltd)$ 0.71
QUINOMAC 100MG TABLET 1 strip / 10 tablets each (Macleods Pharmaceuticals Pvt Ltd)$ 0.35
QUINOMAC 300MG INJECTION 1 vial / 2 ML injection each (Macleods Pharmaceuticals Pvt Ltd)$ 0.30
QUINOMAC 300MG TABLET 1 strip / 10 tablets each (Macleods Pharmaceuticals Pvt Ltd)$ 0.83
Quinomac 100mg Tablet (Macleods Pharmaceuticals Pvt Ltd)$ 0.04
Quinomac 300mg Injection (Macleods Pharmaceuticals Pvt Ltd)$ 0.15
Quinomac 300mg Tablet (Macleods Pharmaceuticals Pvt Ltd)$ 0.08
QUINONIR SYRUP 1 bottle / 60 ML syrup each (Nirlife Healthcare)$ 0.47
QUINOQUIN EC 300MG TABLET 1 strip / 10 tablets each (Leo Pharmaceuticals)$ 0.94
QUINOQUIN EC 600MG TABLET 1 strip / 6 tablets each (Leo Pharmaceuticals)$ 0.98
Quinoquin EC 600mg Tablet (Leo Pharmaceuticals)$ 0.16
QUINOQUIN P TABLET 1 strip / 10 tablets each (Leo Pharmaceuticals)$ 0.48
QUINOQUIN P EC TABLET 1 strip / 10 tablets each (Leo Pharmaceuticals)$ 0.48
Tablet; Oral; Quinine Sulfate 300 mg (Bombay Tablet Mfg Co)
300 mg x 6's (Bombay Tablet Mfg Co)$ 0.61
Quinsul 300 mg Tablet (Bombay Tablet Mfg Co)$ 0.10
Quinsul 300mg FC-TAB / 6 (Bombay Tablet Mfg Co)$ 0.61
QUINSUL 300MG TABLET 1 strip / 6 tablets each (Bombay Tablet Mfg Co)$ 0.61
QUINSUL film-coated tab 300 mg x 6's (Bombay Tablet Mfg Co)$ 0.61
Quinsul 300mg Tablet (Bombay Tablet Mfg Co)$ 0.10
QUNIMAX 300MG TABLET 1 strip / 10 tablets each (Troikaa Pharmaceuticals Ltd)$ 0.54
Quomori Inj 600 mg Injection (Aamorb Pharmaceuticals Pvt Ltd)$ 0.14
Qutil EC 300 mg Tablet (Little Greave Pharmaceuticals Ltd.)$ 0.10
Qutil-EC 300mg EC-TAB / 10 (Little Greave)$ 1.04
300 mg x 10's (Little Greave)$ 1.04
QUTIL-EC enteric-coated tab 300 mg x 10's (Little Greave)$ 1.27
100 mg x 10's (Almet)$ 0.35
300 mg x 10's (Almet)$ 0.78
600 mg x 10's (Almet)$ 1.52
150 mg x 5 mL x 60ml (Almet)$ 0.68
300 mg x 1 mL x 2ml (Almet)$ 0.28
Qutomal 100mg TAB / 10 (Almet)$ 0.35
Qutomal 300mg TAB / 10 (Almet)$ 0.78
Qutomal 600mg TAB / 10 (Almet)$ 1.52
Qutomal 150mg x 5mL SUSP / 60ml (Almet)$ 0.68

References

  1. DailyMed. "QUININE SULFATE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. PubChem. "Quinine". https://pubchem.ncbi.nlm.nih.gov/com... (accessed September 17, 2018).
  3. DrugBank. "Quinine". http://www.drugbank.ca/drugs/DB00468 (accessed September 17, 2018).

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