Quinine | apollo +9191 46 950 950

Quinine | apollo +9191 46 950 950

Quinine

CAS Number : 130-95-0

Molecular Formula : C20H24N2O2

Molecular Weight : 324.41 g/mol

Systematic (IUPAC) : (R)-[(1S,2S,4S,5R)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl](6-methoxyquinolin-4-

yl)methanol

Type : small molecule

Description

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. Quinine 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. Quinine 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.

Categories

Antimalarials

Analgesics, Non-Narcotic

Muscle Relaxants, Central

Pharmacology

Indication : For the treatment of malaria and leg

cramps

Pharmacodynamics : 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.

Mechanism of action : 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.

Absorption : 76 - 88%

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]

Protein binding : Approximately 70%

Metabolism : Hepatic, over 80% metabolized by the

liver.

Route of elimination : Quinine is eliminated

primarily via hepatic biotransformation. Approximately 20% of quinine is excreted unchanged in urine.

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]

Toxicity : Quinine is a documented causative agent of

drug induced thrombocytopenia (DIT). Thrombocytopenia is a low amount of platelets in the

blood. Quinine 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.

Affected organisms : Humans and other mammals

Uses

This medication is used alone or with other medication to treat malaria caused by mosquito bites in countries where malaria is common. Malaria parasites can enter the body through these mosquito bites, and then live in body tissues such as red blood cells or the liver. This medication is used to kill the malaria parasites living inside red blood cells. In some cases, you may need to take a different medication (such as primaquine) to kill

the malaria parasites living in other body tissues. Both drugs may be needed for a complete cure and to prevent the return of infection (relapse). Quinine belongs to a class of drugs known as antimalarials. It is not used for the prevention of malaria.The United States Centers for Disease Control provide updated guidelines and travel recommendations for the prevention and treatment of malaria in different parts of the world. Discuss the most recent information with your doctor before traveling to areas where malaria occurs.The US Food and Drug

Administration (FDA) warns that quinine should not be used to treat leg cramps. It has not been shown to work

for this use and may cause serious side effects.

How To Use?

Read the Medication Guide and, if available, the Patient Information Leaflet provided by your pharmacist before you start taking quinine and each time you get a refill. If

you have any questions, ask your doctor or pharmacist.Take this medication by mouth, with food to decrease upset stomach, exactly as prescribed by your doctor. This medication is usually taken every 8 hours for 3 to 7 days or as directed by your doctor.Take this medication 2 to 3 hours before or after taking antacids containing aluminum or magnesium. These products bind with quinine, preventing your body from fully

absorbing the drug.Dosage and length of treatment are based on your medical condition, country where you

were infected, other medications you may be taking for malaria, and your response to treatment.The dosage in children is also based on weight.It is very important to continue taking this medication (and other malaria

medications) exactly as prescribed by your doctor. Do

not take more or less of this drug than prescribed. Do not skip any doses. Continue to take this medication until the full prescribed amount is finished, even if

symptoms disappear after a few days. Skipping doses or stopping the medication too early may make the

infection more difficult to treat and result in a return of the infection.This medication works best when the

amount of drug in your body is kept at a constant level. Therefore, take this drug at evenly spaced intervals. To help you remember, take it at the same times each day.Tell your doctor if your condition persists or

worsens after 1-2 days of taking this medication. If your fever returns after completing this prescription, contact your doctor so that he/she can determine whether the

malaria has returned.

Drug interactions

See also How to Use section.The effects of some drugs can change if you take other drugs or herbal products at the same time. This can increase your risk for serious side effects or may cause your medications not to work correctly. These drug interactions are possible, but do not always occur. Your doctor or pharmacist can often

prevent or manage interactions by changing how you use your medications or by close monitoring.To help your doctor and pharmacist give you the best care, be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products) before starting treatment

with this product. While using this product, do not start, stop, or change the dosage of any other medicines you are using without your doctor's approval.Some products

that may interact with this drug include: "blood

thinners" (such as warfarin), mefloquine, penicillamine.Other medications can affect the removal

of quinine from your body, which may affect how quinine works. Examples include cimetidine,

erythromycin, ketoconazole, troleandomycin, phenytoin, rifampin, urinary alkalinizers such as

acetazolamide/sodium bicarbonate, among others.This medication can slow down the removal of other

medications from your body, which may affect how they work. Examples of affected drugs include desipramine, digoxin, certain "statin" drugs (atorvastatin, lovastatin, simvastatin), certain anticonvulsants (carbamazepine, phenobarbital), among others.Many drugs besides

quinine may affect the heart rhythm (QT prolongation), including amiodarone, dofetilide, mefloquine, pimozide, procainamide, quinidine, sotalol, macrolide antibiotics (such as erythromycin), among others. Therefore, before using quinine, report all medications you are currently using to your doctor or pharmacist.Cimetidine is a nonprescription drug that is commonly used to treat

extra stomach acid (such as heartburn, ulcers). Because cimetidine and aluminum/magnesium antacids may interact with quinine, ask your pharmacist about other products to treat extra stomach acid.This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications

with you, and share the list with your doctor and pharmacist.

Why is this medication prescribed?

Quinine is used alone or with other medications to treat malaria (a serious or life-threatening illness that is

spread by mosquitos in certain parts of the world). Quinine should not be used to prevent malaria. Quinine is in a class of medications called antimalarials. It works

by killing the organisms that cause malaria.

How should this medicine be used?

Quinine comes as a capsule to take by mouth. It usually is taken with food three times a day (every 8 hours) for 3-7 days. Take quinine at around the same times every day. Follow the directions on your prescription label

carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take quinine exactly as directed. Do not take more or less of it or take it more

often than prescribed by your doctor.

Swallow the capsules whole; do not open, chew, or crush them. Quinine has a bitter taste.

You should begin to feel better during the first 1-2 days of your treatment. Call your doctor if your symptoms do not improve or if they get worse. Also call your doctor if you have a fever soon after you finish your treatment. This could be a sign that you are experiencing a second

episode of malaria.

Take quinine until you finish the prescription, even if you feel better. If you stop taking quinine too soon or if you skip doses, your infection may not be completely treated and the organisms may become resistant to

antimalarials.

Other uses for this medicine

Quinine is also sometimes used to treat babesiosis (a serious or life-threatening illness that is transmitted from animals to humans by ticks). Talk to your doctor

about the risks of using this medication for your condition.

This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.

What special precautions should I follow?

Before taking quinine,

tell your doctor and pharmacist if you are allergic to quinine, quinidine, mefloquine (Lariam), any other medications, or any of the ingredients in quinine

capsules. Ask your doctor or pharmacist for a list of the ingredients.

tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan

to take. Be sure to mention any of the following: acetazolamide (Diamox); aminophylline; anticoagulants

('blood thinners') such as warfarin (Coumadin) and heparin; antidepressants ('mood elevators') such as desipramine; certain antifungals such as fluconazole (Diflucan), ketoconazole (Nizoral), and itraconazole (Sporanox); cholesterol-lowering medications such as atorvastatin (Lipitor), lovastatin (Mevacor), simvastatin (Zocor); cisapride (Propulsid); dextromethorphan (a medication in many cough products); fluoroquinolone antibiotics such as ciprofloxacin (Cipro), gatifloxacin

(Tequin) (not available in the U.S.), levofloxacin (Levaquin), lomefloxacin (Maxaquin), moxifloxacin

(Avelox), norfloxacin (Noroxin), ofloxacin (Floxin), and sparfloxacin (Zagam) (not available in the U.S.);

macrolide antibiotics such as erythromycin (E.E.S., E-Mycin, Erythrocin) and troleandomycin (not available in the U.S.); medications for diabetes such as repaglinide

(Prandin); medications for high blood pressure; medications for irregular heartbeat such as amiodarone (Cordarone, Pacerone), digoxin (Lanoxin), disopyramide (Norpace), dofetilide (Tikosyn), flecainide (Tambocor), procainamide (Procanbid, Pronestyl), quinidine, and

sotalol (Betapace); certain medications for seizures such as carbamazepine (Tegretol), phenobarbital (Luminal, Solfoton), and phenytoin (Dilantin); medications for ulcers such as cimetidine (Tagamet); mefloquine

(Lariam); metoprolol (Lopressor, Toprol XL); paclitaxel (Abraxane, Taxol); pimozide (Orap); rifampin (Rifadin,

Rimactane); certain selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine (Prozac, Sarafem), fluvoxamine (Luvox), and paroxetine (Paxil); sodium

bicarbonate; tetracycline; and theophylline. Your doctor may need to change the doses of your medications or monitor you carefully for side effects. Many other

medications may also interact with quinine, so be sure to tell your doctor about all the medications you are taking,

even those that do not appear on this list.

do not take antacids that contain magnesium or aluminum (Alternagel, Amphogel, Alu-cap, Alu-tab, Basaljel, Gaviscon, Maalox, Milk of Magnesia, or

Mylanta) at the same time as you take quinine.Talk to your doctor or pharmacist about how long you should wait between taking this type of antacid and taking

quinine.

tell your doctor if you or anyone in your family has or has ever had a prolonged QT interval (a rare heart

problem that may cause fainting or irregular heartbeat), an abnormal electrocardiogram (ECG; a test that

measures the electrical activity of the heart), and if you have or have ever had G-6-PD deficiency (an inherited

blood disease), or if you have or have ever had

myasthenia gravis (MG; condition that causes weakness of certain muscles), or optic neuritis (inflammation of the optic nerve that may cause sudden changes in vision). Also tell your doctor if you have ever had a serious reaction, especially a bleeding problem or

problems with your blood after taking quinine in the past. Your doctor will probably tell you not to take

quinine.

tell your doctor if you have or have ever had a slow or irregular heartbeat; low levels of potassium in your

blood; or heart, kidney, or liver disease.

tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant

while taking quinine, call your doctor.

if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking quinine.

tell your doctor if you use tobacco products. Cigarette smoking may decrease the effectiveness of this

medication.

What special dietary instructions should I

follow?

Unless your doctor tells you otherwise, continue your normal diet.

What should I do if I forget a dose?

Take the missed dose as soon as you remember it. However, if it has been more than 4 hours since the time you should have taken the missed dose, skip the missed dose and continue your regular dosing schedule. Do not

take a double dose to make up for a missed one.

What side effects can this medication cause?

This medication may cause low blood sugar. You should know the symptoms of low blood sugar and what to do if

you develop these symptoms.

Quinine may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

nausea

restlessness

difficulty hearing or ringing in the ears

confusion

nervousness

Some side effects can be serious. If you experience any of the following symptoms, call your doctor immediately:

rash

hives

itching

flushing

hoarseness

difficulty breathing or swallowing

swelling of the face, throat, lips, eyes, hands, feet, ankles or lower legs

fever

blisters

stomach pain

vomiting

diarrhea

blurriness or changes in color vision

inability to hear or see

faintness

easy bruising

purple, brown, or red spots on the skin

unusual bleeding

blood in the urine

dark or tarry stools

nosebleeds

bleeding gums

sore throat

fast or irregular heartbeat

chest pain

weakness

sweating

dizziness

Quinine may cause other side effects. Call your doctor if you have any unusual problems while taking this

medication.

What storage conditions are needed for this

medicine?

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Do not refrigerate or freeze the

medication. Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the

proper disposal of your medication.

Symptoms of overdose may include

blurriness or changes in color vision

symptoms of low blood sugar

changes in heartbeat

headache

nausea

vomiting

stomach pain

diarrhea

ringing in the ears or difficulty hearing

seizures

slow or difficult breathing

What other information should I know?

Keep all appointments with your doctor.

Before having any laboratory test, tell your doctor and the laboratory personnel that you are taking quinine.

Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your

prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such

as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of

emergencies.

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