Holestiramin

Холестирамин Constitutional formula

The description is actual on 01.07.2015

  • Latin name: Colestyraminum
  • ATH code: C10AC01
  • Chemical formula: [C22H29NO] x
  • CAS code: 11041-12-6

Chemical name

The copolymer of styrene and divinyl benzene containing quarternary ammonium groups. Substance usually is also in the form of a hydrochloride.

Chemical properties

Colestyraminum represents copolymer of divinyl benzene and styrene, it is ion-exchange resin which possesses property to connect bile acids in intestines. Substance is insoluble in water.

Pharmacological action

Gipokholesterinemicheskoye.

Pharmacodynamics and pharmacokinetics

The mechanism of action of Colestyraminum is based on its ability to connect in intestines bile acids, thus, forming insoluble chelate complexes which then are removed in the natural way with a stake. Also substance is capable to reduce absorbing capacity of cholesterol and other fatty acids, to stimulate synthesis of bile acids in liver tissues (feedback mechanism).

Drugs on the basis of this component considerably reduce the level of cholesterol and lipoproteins of low density in blood. During enterogepatichesky circulation about 98% of bile acids are again soaked up in intestines and get into a liver, then are again allocated with bile. The liver is forced to spend cholesterol to synthesize additional bile acids. Thus, excess cholesterol and LPNP is spent.

At the patients suffering from a giperlipoproteinemiya 2 types, means considerably reduces the level of cholesterol and lipoproteins. At partial obstruction of zhelchevyvodyashchy ways substance reduces the content in blood of bile acids, interferes with their adjournment in integuments, removes an itch.

Achievement of desirable therapeutic effect usually requires prolonged systematic treatment. Medicine reception, at least, within 30 days is recommended. During therapy by medicine it is necessary to make control of content of folic acid in blood and erythrocytes, to monitor digestion, coagulability of blood.

Absorbing capacity of Colestyraminum strongly depends on a hydrogen indicator of the environment. Means possesses the greatest efficiency in a neutral rn. In this regard, medicine concedes to other modern analogs a little.

Holestiramin is not soaked up in intestines and therefore does not render system toxic effects on an organism. The elimination half-life of substance makes about one hour.

Indications to use

Means is appointed:

  • at a giperlipoproteinemiya 2 types, especially 2a type;
  • for prevention of complications at atherosclerosis, stenocardia, a myocardial infarction, a coronary disease of heart if other methods remain inefficient;
  • for removal of an itch at partial obstruction of bilious ways.

Contraindications

Colestyraminum is not appointed:

Side effects

Drugs on the basis of Holestiramin possess a number of side effects:

At prolonged treatment by means can develop:

  • disturbances of coagulability of blood, bleeding in a stomach and a duodenum;
  • giperkhloremichesky acidosis;
  • hemorrhoidal bleedings;
  • impassability of a gastrointestinal tract.

Holestiramin, application instruction (Way and dosage)

Most often substance is let out in the form of powder for preparation of suspension or tablets.

The mode of dosing and duration of treatment is defined by the attending physician.

Tablets Holestiramin and powder accept before food, inside.

Powder can be mixed with water, cream or juice. The prepared suspension needs to be mixed and drunk well 10 minutes later, after preparation.

The dosage is selected individually, depending on age of the patient and a type of a disease. As a rule, for adults the daily dosage makes from 4 to 24 grams of active ingredient distributed on 2,3 or 4 receptions.

Overdose

The most dangerous side effect which can arise at overdose – impassability of a gastrointestinal tract. In what case, it is recommended to stop administration of drug and will see a doctor.

Interaction

Means reduces diuretic effect of furosemide reception.

Colestyraminum reduces absorption of a raloksifen and sulindak (even at observance of a three-hour interval between receptions).

At drug intake with left thyroxine or other hormones of a thyroid gland their efficiency and contents in a blood plasma decreases.

The combination of this means to ferrous sulfate or phenylbutazone leads to decrease in plasma concentration of both drugs.

Colestyraminum reduces absorbing capacity of a hydrochlorothiazide and its diuretic effect.

The combined reception of this substance and Vancomycinum leads to loss of efficiency of Vancomycinum.

At a concomitant use of means and Amiodaronum, concentration of the last of blood can increase considerably.

Colestyraminum combination to tricyclic antidepressants, such as Imipraminum, desipramine, amitriptyline, nortriptilin can lead to decrease in their plasma concentration.

Substance can increase efficiency of an akarboza.

Holestiramin reduces efficiency of Valproatum of sodium, anticoagulants (warfarin, a dikumarol, a fenprokumon, an etilbiskumatsetat), a glipizid and a hydrocortisone.

At a means combination to digoxin if the interval between administrations of drugs is observed at 1,5 o'clock, Colestyraminum does not influence plasma concentration and efficiency of drug.

It is not recommended to combine medicine with an ibuprofen and diclofenac. It can lead to decrease in absorbing capacity of NPVS.

Medicine reduces efficiency of loperamide, a methotrexate, metronidazole, paracetamol.

The substance combination to piroxicam, tenoksikamy and meloksikamy accelerates removal of drugs from an organism.

The concomitant use of means and Spironolactonum can lead to development of a gipokhloremichesky alkalosis.

Storage conditions

To store far from children.

Special instructions

During treatment plentiful drink and periodic control of level of triglycerides and cholesterol in blood is necessary.

At development of disturbances of coagulability of blood administration of vitamin K is recommended.

To children

Children require correction of a dosage.

Elderly

To patients 60 years drug are aged more senior appoint with care.

At pregnancy and a lactation

Reception of this means can perniciously affect fetation therefore its inclusion in time of pregnancy is strictly forbidden. Also during therapy by medicine it is necessary to stop breastfeeding.

Section: Active ingredients
PAY ATTENTION! Information on active ingredients on the website is help generalizing, collected from public sources and can form the basis for making decision on use of these substances it is not aware of treatment. Before substance use Holestiramin surely consult with the attending physician.