Qualaquin (Page 5 of 5)

12.4 Microbiology

Mechanism of Action

Quinine inhibits nucleic acid synthesis, protein synthesis, and glycolysis in Plasmodium falciparum and can bind with hemazoin in parasitized erythrocytes. However, the precise mechanism of the antimalarial activity of quinine sulfate is not completely understood.

Activity In Vitro and In Vivo

Quinine sulfate acts primarily on the blood schizont form of P. falciparum. It is not gametocidal and has little effect on the sporozoite or pre-erythrocytic forms.

Drug Resistance

Strains of P. falciparum with decreased susceptibility to quinine can be selected in vivo. P. falciparum malaria that is clinically resistant to quinine has been reported in some areas of South America, Southeast Asia, and Bangladesh.

13 NONCLINICAL TOXICOLOGY

13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenesis

Carcinogenicity studies of quinine have not been conducted.

Mutagenesis

Genotoxicity studies of quinine were positive in the Ames bacterial mutation assay with metabolic activation and in the sister chromatid exchange assay in mice. The sex-linked recessive lethal test performed in Drosophila , the in vivo mouse micronucleus assay, and the chromosomal aberration assay in mice and Chinese hamsters were negative.

Impairment of Fertility

Published studies indicate that quinine produces testicular toxicity in mice at a single intraperitoneal dose of 300 mg/kg corresponding to a dose of approximately 0.75 times the maximum recommended human dose (MRHD; 32 mg/kg/day) and in rats at an intramuscular dose of 10 mg/kg/day, 5 days/week, for 8 weeks corresponding to a daily dose of approximately 0.05 times the MRHD based on body surface area (BSA) comparisons. The findings include atrophy or degeneration of the seminiferous tubules, decreased sperm count and motility, and decreased testosterone levels in the serum and testes. There was no effect on testes weight in studies of oral doses of up to 500 mg/kg/day in mice and 700 mg/kg/day in rats (approximately 1.2 and 3.5 times the MRHD respectively based on BSA comparisons). In a published study in 5 men receiving 600 mg of quinine TID for one week, sperm motility was decreased and percent sperm with abnormal morphology was increased; sperm count and serum testosterone were unaffected.

14 CLINICAL STUDIES

Quinine has been used worldwide for hundreds of years in the treatment of malaria. Thorough searches of the published literature identified over 1300 references to the treatment of malaria with quinine, and from these, 21 randomized, active-controlled studies were identified which evaluated oral quinine monotherapy or combination therapy for treatment of uncomplicated P. falciparum malaria. Over 2900 patients from malaria-endemic areas were enrolled in these studies, and more than 1400 patients received oral quinine. The following conclusions were drawn from review of these studies:

In areas where multi-drug resistance of P. falciparum is increasing, such as Southeast Asia, cure rates with 7 days of oral quinine monotherapy were at least 80%; while cure rates for 7 days of oral quinine combined with an antimicrobial agent (tetracycline or clindamycin) were greater than 90%. In areas where multi-drug resistance of the parasite was not as widespread, cure rates with 7 days of quinine monotherapy ranged from 86 to 100%. Cure was defined as initial clearing of parasitemia within 7 days without recrudescence by day 28 after treatment initiation. P. falciparum malaria that is clinically resistant to quinine has been reported in some areas of South America, Southeast Asia, and Bangladesh, and quinine may not be as effective in those areas.

Completion of a 7-day oral quinine treatment regimen may be limited by drug intolerance, and shorter courses (3 days) of quinine combination therapy have been used. However, the published data from randomized, controlled clinical trials for shorter regimens of oral quinine in conjunction with tetracycline, doxycycline, or clindamycin for treatment of uncomplicated P. falciparum malaria is limited, and these shorter course combination regimens may not be as effective as the longer regimens.

16 HOW SUPPLIED / STORAGE AND HANDLING

16.1 How Supplied

QUALAQUIN capsules USP, 324 mg are available as clear/clear capsules imprinted AR 102:

Bottles of 30 NDC 13310-153-07
Bottles of 100 NDC 13310-153-01
Bottles of 500 NDC 13310-153-05
Bottles of 1000 NDC 13310-153-10

16.2 Storage

Store at 20° to 25°C (68° to 77°F).

[See USP Controlled Room Temperature]

Dispense in a tight container as defined in the USP.

17 PATIENT COUNSELING INFORMATION

See FDA-approved Medication Guide (17.2)

17.1 Dosing Instructions

Patients should be instructed to:

  • Take all of the medication as directed.
  • Take no more of the medication than the amount prescribed.
  • Take with food to minimize possible gastrointestinal irritation.

If a dose is missed, patients should also be instructed not to double the next dose. If more than 4 hours has elapsed since the missed dose, the patient should wait and take the next dose as previously scheduled.

17.2 FDA-Approved Medication Guide

MEDICATION GUIDE

QUALAQUIN® (kwol -a-kwin)

(Quinine sulfate) Capsules

Read the Medication Guide that comes with QUALAQUIN ® before you start taking it and each time you get a refill. There may be new information. This Medication Guide does not take the place of talking to your healthcare provider about your medical condition or treatment. You and your healthcare provider should talk about QUALAQUIN ® when you start taking it and at regular checkups. QUALAQUIN ® is not approved for the treatment of night-time leg cramps.

What is the most important information I should know about QUALAQUIN® ?

QUALAQUIN® used to treat or prevent leg cramps may cause serious side effects or even death.

  • QUALAQUIN ® may cause your blood cell (platelet) count to drop causing serious bleeding problems. In some people, serious kidney problems can happen.
  • QUALAQUIN® may cause problems with your heart rhythm that can lead to death.
  • QUALAQUIN® may cause serious allergic reactions.

Call your healthcare provider right away if you have:

  • easy bruising
  • severe nose bleed
  • blood in urine or stool
  • bleeding gums
  • appearance of unusual purple, brown or red spots on your skin (bleeding under your skin)
  • rash
  • hives
  • severe itching
  • severe flushing
  • swelling of your face
  • trouble breathing
  • chest pain
  • rapid heartbeat
  • irregular heart rhythm
  • weakness
  • sweating
  • nervousness

Taking QUALAQUIN® with some other medicines can increase the chance of serious side effects. Tell your healthcare provider if you take any other medicines.

Certain medicines can cause the blood levels of QUALAQUIN ® to be too high or too low in your body. It is important for you to tell your healthcare provider about all the medicines you take, including prescription and non-prescription medicines, vitamins and herbal supplements.

QUALAQUIN® and other medicines may affect each other causing serious side effects or death. Even medicines that you may take for a short period of time, such as antibiotics, can mix in your blood with QUALAQUIN® and cause serious side effects or death. Do not start taking a new medicine without telling your healthcare provider or pharmacist.

What is QUALAQUIN® ?

QUALAQUIN ® is a prescription medication used to treat malaria (uncomplicated) caused by the parasite Plasmodium falciparum.

QUALAQUIN® is Not approved to:

  • Prevent malaria
  • Treat severe or complicated malaria
  • Prevent or treat night-time leg cramps

It is not known if QUALAQUIN® is safe and works in children younger than 16 years old.

Who should not take QUALAQUIN® ?

Do not take QUALAQUIN® if you have:

  • certain heart rhythm problems (atrial fibrillation) or abnormal electrocardiogram (ECG) (QT prolongation).
  • low levels of an enzyme called Glucose-6-phosphate dehydrogenase (G6PD).
  • an autoimmune disease (myasthenia gravis) that leads to muscle weakness.
  • had allergic reactions to quinine, quinidine, or mefloquine (Lariam®).
  • had serious side effects to quinine (QUALAQUIN®), such as low platelets, which are necessary for your blood to clot.
  • an inflammation of the nerve important for vision (optic neuritis).

What should I tell my healthcare provider before starting QUALAQUIN® ?

Before you take QUALAQUIN® , tell your healthcare provider if you:

  • Have heart problems.
  • Have kidney problems.
  • Have liver problems.
  • Have any other medical condition.
  • Are pregnant or could be pregnant. Treatment of malaria is important because it can be a serious disease for a pregnant woman and her unborn baby. Your healthcare provider can tell you more about the benefits and risks of taking this medication during pregnancy. Low blood sugar (hypoglycemia) can be seen in pregnant women while taking QUALAQUIN®. This can include sweating, weakness, nausea, vomiting, or confusion. You and your healthcare provider can decide if QUALAQUIN ® is right for you.
  • Are breast-feeding. Small amounts of QUALAQUIN ® can pass into your breast milk. You and your healthcare provider can decide if you should breastfeed while taking QUALAQUIN ® .

Tell your healthcare provider about all the medicines you take, including prescription medicines, vitamins and herbal supplements.

How should I take QUALAQUIN® ?

  • Take QUALAQUIN ® exactly as your healthcare provider tells you to take it.
  • Your healthcare provider will tell you how many QUALAQUIN® capsules to take and when to take them.
  • To lower the chance of stomach upset, take QUALAQUIN® with food.
  • Finish all the QUALAQUIN ® that is prescribed even if you feel better. Do not stop taking the medication without talking to your healthcare provider.
  • Do not take more than the amount prescribed. Do not take more than 2 capsules at one time or more than 3 doses in one day. If you take more than the prescribed dose, call your healthcare provider right away.
  • If you forget to take QUALAQUIN® , do not double the next dose. If it has been more than 4 hours since the missed dose, just wait and take the regular dose at the next scheduled time. Call your healthcare provider if you are not sure what to do.
  • If you take too much QUALAQUIN® , call your healthcare provider or go to the nearest emergency room right away.

Call your healthcare provider right away if:

  • If you feel worse, or if you do not start feeling better within 1 or 2 days of starting to take QUALAQUIN®.
  • If your fever comes back after finishing treatment with QUALAQUIN®.

What are the possible side effects of QUALAQUIN® ?

QUALAQUIN® may cause serious side effects.

Common side effects with QUALAQUIN ® include:

  • headache
  • sweating
  • flushing
  • nausea
  • ringing in your ears
  • diarrhea
  • deafness
  • hearing loss
  • dizziness (vertigo)
  • blurred vision
  • changes in how you see color
  • vomiting
  • stomach pain
  • blindness

Tell your healthcare provider if you have any side effect that bothers you or that does not go away.

These are not all of the possible side effects of QUALAQUIN ® . For more information, ask your healthcare provider or pharmacist.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

How should I store QUALAQUIN® ?

  • Keep the capsules in a tightly closed container.
  • Do not refrigerate or freeze.
  • Store at 20°C to 25°C (68ºF to 77°F).

Keep QUALAQUIN® and all medicines out of the reach of children.

General Information about QUALAQUIN®

Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use QUALAQUIN ® for a condition for which it was not prescribed. Do not give QUALAQUIN ® to other people, even if they have the same symptoms that you have. It may harm them.

This Medication Guide summarizes the most important information about QUALAQUIN ® . If you would like more information, talk with your healthcare provider. You can ask your healthcare provider or pharmacist for information about QUALAQUIN ® that is written for healthcare professionals.

For more information, go to www.QUALAQUIN.com or call 1-888-351-3786.

What are the ingredients in QUALAQUIN® ?

Active Ingredients: Quinine Sulfate, USP
Inactive Ingredients: Corn starch, magnesium stearate, talc

This Medication Guide has been approved by the U.S. Food and Drug Administration.

Manufactured for:
AR SCIENTIFIC, INC.
Philadelphia, PA 19124 USA
by:
MUTUAL PHARMACEUTICAL COMPANY, INC.
Philadelphia, PA 19124 USA

Rev 23, April 2013

PRINCIPAL DISPLAY PANEL — 324 mg Capsule Bottle Label

100 CAPSULES
NDC 13310-153-01

QUALAQUIN ®
quinine sulfate
capsules USP

324 mg

DISPENSE THE ACCOMPANYING
MEDICATION GUIDE TO EACH PATIENT

AR SCIENTIFIC

Rx only

PRINCIPAL DISPLAY PANEL -- 324 mg Capsule Bottle Label
(click image for full-size original)
QUALAQUIN quinine sulfate capsule
Product Information
Product Type HUMAN PRESCRIPTION DRUG Item Code (Source) NDC:13310-153
Route of Administration ORAL DEA Schedule
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
Quinine Sulfate (Quinine) Quinine Sulfate 324 mg
Inactive Ingredients
Ingredient Name Strength
starch, corn
magnesium stearate
talc
Product Characteristics
Color WHITE (clear) Score no score
Shape CAPSULE Size 22mm
Flavor Imprint Code AR;102
Contains
Packaging
# Item Code Package Description Multilevel Packaging
1 NDC:13310-153-07 30 CAPSULE in 1 BOTTLE, PLASTIC None
2 NDC:13310-153-01 100 CAPSULE in 1 BOTTLE, PLASTIC None
3 NDC:13310-153-05 500 CAPSULE in 1 BOTTLE, PLASTIC None
4 NDC:13310-153-10 1000 CAPSULE in 1 BOTTLE, PLASTIC None
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA021799 08/12/2005
Labeler — AR Scientific Inc. (606563521)

Revised: 04/2013 AR Scientific Inc.

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