Quinine

Хинин Constitutional formula

The description is actual on 07.10.2015

  • Latin name: Quinine
  • ATH code: P01BC01, M09AA
  • Chemical formula: C20H24N2O2
  • CAS code: 130-95-0

Chemical name

(8S,9R)-6 -Metoksitsinkhonan-9-ol

Chemical properties

Quinine — what is it?

This substance – one of the main alkaloids of bark of a cinchonic tree. Bark possesses characteristic bitter taste, the anesthetizing and febrifugal properties, ability to fight against a malarial plasmodium. Long means was used for treatment of malaria.

Bark of a tree was delivered on the territory of Europe in 30 years of the 17th weight. The malaria medicine made of powder of pounded Jesuit bark was known under the name "countess's powder" and soon gained distribution in all territory of Europe.

Quinine is it from numerous alkaloids of bark of a cinchonic tree, except it in raw materials found tsinkhonin, quinidine, tsinkhonidin. The molecule of substance contains quinolinic and hinuklidinovy cycles which are connected by group of atoms (CH-OH). On the structure means represents quinidine isomer.

Substance can be extracted by means of organic solvent from alkaline water a ditch. Most effectively process proceeds at a hydrogen indicator from 9 to 10. Wikipedia the molecular mass of means = 324,4 grams agree to mol. Substance melts at 177 degrees Celsius.

In medicine use sulfate, a hydrochloride or quinine dihydrochloride. The basis is well soluble in ethyl ether, diethyl ether and chloroform, will badly be dissolved in water. The hydrochloride is soluble in ethanol, water and chloroform, slaborastvory in diethyl ether. It is easy to dilute sulfate with ethyl ether.

The hydrochloride and sulfate of Quinine let out in the tableted form, dihydrochloride – solution for injections. At the moment in medical practice most often use quinidine or other medicines.

Pharmacological action

Antiarrhytmic, sedative, anesthetizing, febrifugal.

Pharmacodynamics and pharmacokinetics

What is Quinine?

Quinine – the medicine making multilateral and difficult impact on a human body.

This connection – antiarrhytmic means, possesses ability to slow down conductivity and to reduce excitability of a cardiac muscle. At the same time substance has slight antropinopodobny effect. Medicine is carried to antiarrhytmic means of the first class A. However, Quinine considerably concedes to quinidine, possesses a large number of side effects, in comparison with active isomer.

Alkaloid of a cinchonic tree possesses characteristic bitter taste, properties of bitterness. Substance stimulates development of a gastric juice and increases appetite. Means influences the center of thermal control in a hypothalamus, normalizing body temperature. Raises a uterus tone.

Substance well anesthetizes, in particular relieves of a headache, strengthens action of narcotic and non-narcotic anesthetics. Means is often used in a combination with analginum.

Quinine oppresses processes of reproduction of erythrocyte forms of the causative agent of malariaa malarial plasmodium. On the mechanism of action substance is similar to Chingaminum, however its activity is slightly lower. Substance collects in lysosomes a plasmodium, raises a hydrogen indicator of intracellular organellas, thus breaking phospholipase transport. Means does not influence fabric and sexual uniforms of the harmful agent. Presently medicine is used at especially steady forms of malaria. Means is active in relation to Plasmodium falciparum, Plasmodium vivax and Plasmodium malariae.

Also this connection has antimiotonichesky effect. It extends the refractory period of work of skeletal muscles, breaking calcium transport through a semi-impenetrable membrane. Thus, the response of a nervous system to muscular stimulation is violated, excitability of the terminations of a motorium decreases.

After intake substance is completely and quickly acquired by the alimentary system. Its biological availability makes about 80%. After reception of tablets the maximum concentration of medicine is observed in 4 hours. Means has high extent of linkng with proteins of a blood plasma. Quinine breaks a blood-brain barrier, passes through a placenta and is emitted with breast milk.

The metabolism of medicine occurs in a liver, metabolites are less active. It is removed through kidneys within 16-18 hours.

Indications to use

Medicine is appointed:

  • for stimulation of a tone of a uterus at weak patrimonial activity;
  • as a part of complex treatment of hypotonia of a uterus in an early puerperal period;
  • at the heavy and malignant course of malaria and resistance of the activator to others lek. to means;
  • within complex therapy at cardiovascular insufficiency.

Contraindications

Means is contraindicated:

  • at hemorrhagic fever;
  • to patients with diseases of an inner and middle ear and with reduced hearing;
  • at deficit of enzyme glyukozo-6-fosfatdegiidrogenazy;
  • to pregnant women (if there is no need of a call of patrimonial activity);
  • at an allergy to active ingredient;
  • during a lactation.

Extra care is recommended to be observed:

  • on late durations of gestation;
  • at sharp decrease in pumping function of a cardiac muscle.

Side effects

Medicine often causes the following side effects:

At hypersensitivity to substance body temperature increases, there are uterine bleedings, complication of a course of malaria which arises because of an erythrocytolysis. Lethal outcomes are known.

Quinine, application instruction (Way and dosage)

Medicine is taken, as a rule, inside, Quinine the hydrochloride is entered intravenously or subcutaneously.

The instruction on drug at malaria

The adult appoint 1-1,2 grams a day inside. At heavy disease – on 1,5 grams a day distributed on 2-3 receptions within 5-7 days.

At the malignant course of a disease medicine is entered subcutaneously deeply on 2 grams, 4 times a day. Slow intravenous administration of substance is also shown. Before procedure of 1 ml of 50% of solution of Quinine part in Dextrosum or sodium chloride, previously having warmed up solution to 35 degrees. In a critical condition it is intravenously possible to enter 0,5 grams of the received solution and 0,5 more grams subcutaneously. Frequency rate of injections – from 3 to 4 times a day. The maximum daily dosage – 3 grams of substance.

Quinine, application instruction

At heart failure which symptoms are a cardiopalmus the sunk-down veins, etc., use means in combination with other drugs (ephedrine, camphor, caffeine). Medicine is entered subcutaneously. After the condition of the patient was stabilized, recommended to be passed to the tableted form.

For children till 12 months the daily dosage is distributed from a ratio of 10 mg of drug for one month of life of the child. Aged till 10 flyings – for 1 year, till 15 flyings no more than 1 gram of means a day are recommended to give 100 mg to the patient. To avoid development of necroses in a drug injection site children till 15 flyings cannot make medicine injections.

For stimulation of patrimonial activity and increase of a tone of a uterus drug is combined with other stimulators (Oxytocin, estrogen, serotonin, Pachycarpinum). Medicine is appointed inside, on 100-150 mg, by everyone half of hour, to 6 times.

For increase of a tone of a uterus after the delivery intravenously enter from 1 to 3 ml of solution of the Quinine (50%) dissolved by a dextrose or sodium chloride.

Overdose

At overdose the frequency and force manifestation of side reactions most often increases, there are painful feelings in a stomach, the general weakness, decreases arterial pressure, the patient suddenly loses sight, cardiac arrhythmia, disorders of work of respiratory system is observed, convulsive activity increases, heart can stop.

As therapy wash out a stomach, give to the victim enterosorbents, introduction of the drugs understanding rn urine is shown (for example, ammonium chloride), carry out reanimation of the patient and a symptomatic treatment.

Interaction

Means breaks processes of synthesis of a prothrombin and other factors of coagulability of blood, strengthens effect of indirect anticoagulants.

The combined reception of Quinine with digoxin can lead to increase of plasma concentration of the last and strengthening of its efficiency.

Inductors of a microsomal oxidation reduce efficiency of drug. Inhibitors of a microsomal oxidation increase probability of development of side effects and efficiency of means.

Terms of sale

The recipe is necessary.

Storage conditions

Tablets are recommended to be stored in original packaging, in well corked container, without influence of sunshine.

Special instructions

Before administration of drug it is intravenously necessary to make sure that the patient normally transfers this substance to avoid development of an idiosyncrasy and sudden death.

It is necessary to consider that at administration of drug the probability of development of abscess, a necrosis of soft tissues and sharp pain in the place of an injection is intramusculary high. Whenever possible it is desirable to use means in the form of tablets.

During therapy it is recommended to make periodic control of a peripheral picture of blood and urine.

To children

For children it is necessary to correct a dosage, as directed in the instruction. Extremely parenteral administration is not recommended.

At pregnancy and a lactation

In general means is contraindicated to use during treatment to pregnant women and feeding women. Except cases when Quinine is applied in obstetric practice as a part of complex therapy or in an early puerperal period.

Drugs in which contains (Analogues)

Substance is a part of tablets from a headache Analginum-quinine, Quinine the Hydrochloride, Quinine Sulphate in tablets.

Also this means can be met as a part of some products food and drinks, for example Quinine in Shvepsa as synthetic fragrance: Schweppes Bitter Lemon, Schweppes Indian Tonic Water, Jumbo Gin-tonic, Evervess.

Quinine also is a part of cosmetics (shampoo Kloral with Quinine).

What is Quinine in Shvepsa?

The chemical compound was initially added to water as a prophylactic from malaria. There is an opinion that the lemon to drink was added to take away the taste of bitterness. It is at the moment replaced with the fragrance identical to natural.

Section: Active ingredients
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