Retard in medicine is an extension of the duration of something, any process: treatment, taking medications. In Russian, the term “retard” is sometimes used not only in the medical, legal and financial fields, but also in the general sense of extending something.
Recently, studies on prolonging the effects of drugs have become widespread. Prolonged forms are those that have a modified release, which increases the duration of action of the substance by reducing the rate of its release.
The benefits of such drugs
Thanks to the use of long-acting drugs (this concept is now increasingly used), it is possible not only to reduce, due to improved use, the total volume of the drug entering the body throughout the entire therapeutic course and the number of injections or doses, but also to highlight a number of other significant advantages.
In addition, their use eliminates or reduces variations in the concentration of the active component in tissues and blood, which are inevitable companions of periodically repeated doses of conventional drugs. Thanks to compounds with a prolonged action, it is possible to reduce the frequency of side effects in the patient (this also occurs due to the elimination of the irritating effect of the drug on the gastrointestinal tract), and the likelihood of negative consequences is reduced if the medicine is not taken at the prescribed time.
Also, the use of these drugs can significantly save time spent on procedures (one dose or injection instead of four or five). This is important when conducting therapy in a clinical setting. The word retard itself translated from English means “slow down”, “delay”.
Uno, OD, SR
Uno, OD and SR have a similar effect. Drugs with these abbreviations added to their names are also taken once a day (“Fromilid Uno”, “Cifran OD”, “Klacid SR”). It would seem that it is more convenient to take the drug once a day, and there is no need at all to use the same drugs that are taken several times a day. But this is far from true.
For example, when treating peptic ulcers in the presence of Helicobacter pylori, antibiotics with Uno or SR at the end of the name are not used. Gastroenterologists always pay attention to this point, so do not hesitate to transfer the prescription or doctor's notes to your pharmacist, rather than reading them yourself and risking missing such a “tiny” detail like a few letters.
Importance in pharmacology
Increasing the duration of the influence of drugs is one of the current trends in pharmaceutical technology, since in some cases it is necessary to ensure the presence of a certain level of drugs in the tissues and biological fluids of the human body for a long time. This requirement must especially be adhered to when taking sulfonamides, antibiotics, and other antibacterial agents.
When their concentration decreases, the effectiveness of therapy decreases accordingly, resistant strains of various microorganisms are produced, the elimination of which will require an even higher dosage, which means that the side effects will increase. That is why the problem of prolonging the effect of drugs remains important and relevant.
Classification and characteristics of prolonged forms
Retard are special prolonged dosage forms that must meet the following requirements:
- the concentration of the substance in accordance with the release from the drug should not fluctuate significantly and be in an optimal state in the body over a certain period of time;
- excipients that are included in the dosage form must be removed in full or deactivated;
- prolongation methods should be easy to use and easy to use and should not have a negative impact on the patient’s body.
The drug "Cortexon" (retard) is an example of this type of medical product.
Express
The word "Express" speaks for itself. These drugs have an accelerated effect. It is commonly used in painkillers, but is also found in other classes of medications.
Neo usually means that new substances have been added to a known drug or it has been completely changed. Sometimes such drugs remain with the same effect, only “better”, and sometimes they radically change their functions. For example, “Troxevasin Neo” is also applied to veins like regular “Troxevasin”, but additionally cares for the skin and contains an anticoagulant. But Codelac Neo is a remedy for dry cough, and Codelac Broncho is a remedy for wet cough.
All medications must be prescribed by a doctor! Trade names in the text are given as examples only!
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Types
Depending on how long-acting forms are administered, they are divided into the following types:
- depot dosage forms (hereinafter referred to as DF);
- LF retard.
Based on the nature of the kinetic features of the process, dosage forms with release are distinguished:
- periodic;
- continuous;
- delayed.
Periodic release
Retard is now a very common form of drugs. LF with periodic release (also multiple or intermittent release) are prolonged dosage forms, with the entry into the body of which the active substance is released in portions, which is reminiscent in its essence of plasma concentrations that are created by simply taking tablets every four hours. They also help ensure repeated action of a particular drug.
D, DSR, Insta
One drug for the stomach can have 4 varieties with the same name. “Omez” can be generic, or it can be D, DCP, Insta. The latter type differs in its dosage form - it is a powder, not capsules. The rest differ in the composition and amount of active ingredients. D stands for domperidone. DCP stands for Domperidone and its extended release.
Continuous
Retard dosage forms with continuous (long-term) release are prolonged dosage forms, upon entry into the body the substance is released in its initial dose, while the remaining doses, that is, maintenance doses, are released at a constant rate, that is, in accordance with the rate of elimination, which ensures constancy required therapeutic concentration. Thus, the drug acts as a supporting agent.
Peculiarities
Retard are dosage forms that are prolonged enteral dosage forms that ensure the creation of a supply of the drug in the human body and its subsequent gradual release. They are most often administered orally, but rectal forms are also available.
Depending on what technology was used to obtain them, there are two main types of retard dosage forms (translation presented above), such as matrix and reservoir. Matrix-type forms contain a polymer matrix with a medicinal substance distributed in it. They often look like regular pills.
The reservoir type is a core in which the drug substance is included, as well as a polymer or membrane shell that determines the rate of the release process. The reservoir can be a single form (capsule, tablet) or a microform, the combination of which forms the final form (for example, microcapsules, etc.).
The general meaning of the word “retard” interests many.
What forms are there?
Long-acting dosage forms include:
- Enteric granules.
- Retard and retard forte capsules.
- Retard dragee with enteric coating.
- Enteric-coated capsules.
- Retard solution and rapid retard.
- Enteric tablets, two-layer, frame and multi-layer.
- Retard suspension.
- Tablets retard, retard mite, rapid retard, ultraretard and retard forte.
- Tablets with multiphase and film coating.
There are also retard tablets that have other release methods - continuous, delayed and evenly extended. In addition, they have such varieties as structured and “duplex” tablets. These include the drugs “Potassium-normine”, “Dalfaz SR”, “Ketonal”, “Diclonate Pretard 100”, “Tramal Retard”, “Cordaflex”, and in veterinary medicine “Cortexon retard”.
Long-acting solid dosage forms
Long-acting solid dosage formsWe continue the series of publications of articles by young specialists studying factory technology. The future of the Russian pharmaceutical industry depends on those who will come to work tomorrow at Russian pharmaceutical production. Therefore, the training of highly qualified engineers, technologists, and quality specialists should begin at the university. We hope that the topic of releasing long-acting solid dosage forms is especially relevant for our manufacturing readers.
E.A. Chursina, 5th year student of the Faculty of Pharmacy, Department of General Pharmaceutical and Biomedical Technology, MMA named after. THEM. Sechenov
Prolonged dosage forms (from the Latin Prolongare - to extend) are dosage forms with a modified release. Due to the slower release of the drug, the duration of its action is increased.
The main advantages of these dosage forms are:
- possibility of reducing reception frequency,
- possibility of reducing the course dose,
- the ability to eliminate the irritating effect of drugs on the gastrointestinal tract,
— the ability to reduce the manifestations of major side effects.
The following requirements apply to extended dosage forms:
— The concentration of the drug as it is released from the drug should not be subject to significant fluctuations and should be optimal in the body for a certain period of time.
— Excipients introduced into the dosage form must be completely eliminated from the body or inactivated.
— Methods of prolongation should be simple and accessible to implement and should not have a negative effect on the body. The most physiologically indifferent method is prolongation by slowing drug absorption
.
Depending on the route of administration, prolonged forms are divided into retard dosage forms
and
depot dosage forms
. Taking into account the kinetics of the process, dosage forms with periodic release, continuous and delayed release are distinguished. Depot dosage forms (from the French depot - warehouse, set aside. Synonyms - deposited dosage forms) are prolonged dosage forms for injections and implantations, ensuring the creation of a supply of the drug in the body and its subsequent slow release. Depot dosage forms always enter the same environment in which they accumulate, in contrast to the changing environment of the gastrointestinal tract. The advantage is that they can be administered at longer intervals (sometimes up to a week). In these dosage forms, slowing down absorption is usually achieved by using poorly soluble drug compounds (salts, ethers, complex compounds), chemical modification - for example, microcrystallization, placing the drug in a viscous medium (oil, wax, gelatin or synthetic medium), using systems delivery – microspheres, microcapsules, liposomes.
The modern nomenclature of depot dosage forms includes:
Injection forms
– oil solution, depot suspension, oil suspension, microcrystalline suspension, micronized oil suspension, insulin suspensions, microcapsules for injection.
Implantation forms
– depot tablets, subcutaneous tablets, subcutaneous capsules (depot capsules), intraocular films, ophthalmic and intrauterine therapeutic systems. To designate parenteral application and inhalation dosage forms, the term “extended release” or more generally “modified release” is used.
Dosage forms retard
(from Latin retardo - slow down, tardus - quiet, slow; synonyms - retardets, retarded dosage forms) - these are prolonged dosage forms that provide a supply of the drug substance in the body and its subsequent slow release. These dosage forms are used primarily orally, but are sometimes used for rectal administration. Previously, this term also denoted prolonged injectable forms of heparin and trypsin.
To obtain dosage forms of retard, physical and chemical methods are used.
To physical
include methods of coating crystalline particles, granules, tablets, capsules; mixing medicinal substances with substances that slow down absorption, biotransformation and excretion; use of insoluble bases (matrices), etc.
Basic chemical
methods are adsorption on ion exchangers and the formation of complexes. Substances bound to the ion exchange resin become insoluble and their release from dosage forms in the digestive tract is based solely on ion exchange. The rate of release of the drug substance varies depending on the degree of grinding of the ion exchanger and the number of its branched chains.
Depending on the production technology, there are two main types of retard dosage forms - reservoir and matrix
.
Tank type molds
They represent a core containing the drug and a polymer (membrane) shell, which determines the release rate. The reservoir can be a single dosage form (tablet, capsule) or a dosage microform, many of which form the final form (pellets, microcapsules). Matrix-type retard forms contain a polymer matrix in which the drug is distributed, and very often takes the form of a simple tablet. Dosage forms of retard include enteric granules, retard dragees, enteric-coated dragees, retard and retard forte capsules, enteric-coated capsules, retard solution, rapid retard solution, retard suspension, two-layer tablets, enteric tablets, frame tablets, multilayer tablets, tablets retard, rapid retard, retard forte, retard mite and ultraretard; multiphase coated tablets, film coated tablets, etc.
Taking into account the kinetics of the process, dosage forms are distinguished with periodic release, continuous release and delayed release.
Periodic release dosage forms
(synonymous with intermittent-release dosage forms) are prolonged dosage forms, when administered into the body, the drug is released in portions, which essentially resembles the plasma concentrations created by normal dosing every four hours. They ensure repeated action of the drug.
In these dosage forms, one dose is separated from another by a barrier layer, which can be film, pressed or coated. Depending on its composition, the dose of the drug can be released either after a given time, regardless of the localization of the drug in the gastrointestinal tract, or at a certain time in the required part of the digestive tract.
Thus, when using acid-resistant coatings, one part of the drug substance can be released in the stomach, and the other in the intestines. In this case, the period of general action of the drug can be extended depending on the number of doses of the drug contained in it, i.e. on the number of layers of the tablet or dragee. Dosage forms with periodic release include double-layer tablets and double-layer dragees (“duplex”), multilayer tablets.
Sustained release dosage forms
– these are prolonged dosage forms, when administered into the body, an initial dose of the drug is released, and the remaining (maintenance) doses are released at a constant rate that corresponds to the rate of elimination and ensures the constancy of the desired therapeutic concentration. Dosage forms with continuous, uniformly extended release provide the maintenance effect of the drug. They are more effective than time-release forms because... ensure a constant concentration of drugs in the body at a therapeutic level without pronounced extremes, and do not overload the body with excessively high concentrations.
Continuous-release dosage forms include frame tablets, microform tablets and capsules, etc.
Delayed release dosage forms
– these are prolonged dosage forms, when administered into the body, the release of the drug substance begins later and lasts longer than from a regular dosage form.
They provide a delayed onset of action of the drug. An example of these forms are suspensions ultralong, ultralente with insulin.
Tablets are of particular interest among prolonged dosage forms.
Extended tablets
(synonyms: extended-release tablets, extended-release tablets) are tablets from which the drug substance is released slowly and evenly or in several portions. These tablets allow you to provide a therapeutically effective concentration of the drug in the body for a long period of time.
The range of extended-release tablets includes implantable tablets, or depot; retard tablets, frame, multilayer, multiphase. These include Depakin Chrono, Cardil, Nifecard HL, Trittico, Sustonit).
Implantable tablets
(syn. – implantablets, depot tablets, tablets for implantation) are sterile trituration tablets with prolonged release of highly purified medicinal substances for administration under the skin. It has the shape of a very small disk or cylinder. These tablets are made without fillers. This dosage form is very common for the administration of steroid hormones. The term “pellets” is also used in foreign literature. Examples - Disulfiram, Doltard, Esperal.
Retard tablets
are oral tablets with prolonged (mostly periodic) release of drugs.
Usually they are microgranules of a medicinal substance surrounded by a biopolymer matrix (base). They dissolve layer by layer, releasing the next portion of the drug. They are obtained by pressing microcapsules with a solid core on tablet machines. Soft fats are used as excipients, which can prevent the destruction of the microcapsule shell during the pressing process.
There are also retard tablets with other release mechanisms - delayed, continuous and evenly extended release. Varieties of retard tablets are “duplex” tablets and structural tablets. These include Dalfaz SR, Diclonate Pretard 100, Potassium-normine, Ketonal, Cordaflex, Tramal Pretard.
Repetabs
- These are multilayer coated tablets that ensure repeated action of the drug. They consist of an outer layer with a drug substance that is designed for rapid release, an inner shell with limited permeability and a core that contains another dose of the drug substance.
To produce these tablets, cyclic tablet machines with multiple pouring are used. The machines can carry out triple pouring with different granulates.
Frame tablets
(syn. Durules, Durules tablets, matrix tablets, porous tablets, skeletal tablets, tablets with an insoluble frame) are tablets with a continuous, uniformly extended release and supporting action of the drug. This dosage form is obtained by incorporating (incorporating) a drug into a network structure (matrix) of insoluble excipients, or into a matrix of hydrophilic substances that do not form a high-viscosity gel. The materials for the “skeleton” are inorganic compounds - barium sulfate, gypsum, calcium phosphate, titanium dioxide and organic compounds - polyethylene, polyvinyl chloride, aluminum soaps. Skeletal tablets can be prepared by simply compressing medicinal substances that form a skeleton. These tablets do not disintegrate in the gastrointestinal tract. Depending on the nature of the matrix, they can swell and slowly dissolve or maintain their geometric shape throughout the entire period of stay in the body and be excreted in the form of a porous mass, the pores of which are filled with liquid. Thus, the drug is released by leaching. Dosage forms can be multilayer. It is important that the medicinal substance is located predominantly in the middle layer. Its dissolution begins from the side surface of the tablet, while from the upper and lower surfaces, only excipients from the middle layer initially diffuse through the capillaries formed in the outer layers. Currently, the technology for producing frame tablets using solid dispersed systems (Kinidin Durules) is promising.
Spacestabs
- These are tablets with a medicinal substance included in a solid fat matrix, which does not disintegrate, but is slowly dispersed from the surface.
Lontabs
- These are tablets with prolonged release of drugs. The core of these tablets is a mixture of drugs with high molecular weight waxes. They do not disintegrate in the gastrointestinal tract, but slowly dissolve from the surface.
One of the modern methods of prolonging the action of tablets is to coat them with coatings, in particular Aqua Polish coatings. These coatings provide prolonged release of the substance. They have alkaliphilic properties, thanks to which the tablet is able to pass through the acidic environment of the stomach unchanged. Solubilization of the coating and release of active substances occurs in the intestine. The release time of the substance can be controlled by adjusting the viscosity of the coating. It is also possible to set the release time of various substances in combination preparations.
Examples of the compositions of these coatings:
Aqua Polish,
Methacrylic acid/Ethyl acetate
Sodium carboxymethylcellulose
Talc
Titanium dioxide.
Another coating option replaces sodium carboxymethylcellulose with polyethylene glycol.
The microencapsulation process is often used to prolong dosage forms.
Microencapsulation
- the process of enclosing microscopic particles of solid, liquid or gaseous medicinal substances. Most often, microcapsules with sizes ranging from 100 to 500 microns are used. Particles <1 µm in size are called nanocapsules. Particles with liquid and gaseous substances have a spherical shape, while solid particles have an irregular shape.
Microencapsulation capabilities:
a) protection of unstable drugs from exposure to the external environment (vitamins, antibiotics, enzymes, vaccines, serums, etc.);
b) masking the taste of bitter and nauseating drugs;
c) release of medicinal substances in the desired area of the gastrointestinal tract (enteric-soluble microcapsules);
d) prolonged action. A mixture of microcapsules differing in size, thickness and nature of the shell, placed in one capsule, ensures the maintenance of a certain level of the drug in the body and an effective therapeutic effect for a long time;
e) combining in one place drugs that are incompatible with each other in their pure form (use of release coatings);
f) “transformation” of liquids and gases into a pseudo-solid state, i.e. into a granular mass consisting of microcapsules with a hard shell filled with liquid or gaseous medicinal substances.
Application of microcapsules
A number of medicinal substances are produced in the form of microcapsules: vitamins, antibiotics, anti-inflammatory, diuretic, cardiovascular, anti-asthmatic, antitussive, sleeping pills, anti-tuberculosis, etc.
Microencapsulation opens up interesting possibilities for the use of a number of medicinal substances that cannot be realized in conventional dosage forms. An example is the use of nitroglycerin in microcapsules. Regular nitroglycerin in sublingual tablets or drops (on a sugar cube) has a short period of action. Microencapsulated nitroglycerin has the ability to be released in the body for a long time.
Microencapsulation technology
Existing microencapsulation methods: physical; physico-chemical; chemical.
Physical methods.
Physical methods for microencapsulation are numerous. These include methods of panning, spraying, spraying in a fluidized bed, dispersion in immiscible liquids, extrusion methods, electrostatic method, etc. The essence of all these methods is the mechanical application of a shell to solid or liquid particles of medicinal substances. The use of one or another method depends on whether the “core” (the contents of the microcapsule) is a solid or liquid substance.
Spray method.
For microencapsulation of solids, which must first be converted into fine suspensions. The size of the resulting microcapsules is 30 – 50 microns.
Method of dispersion in immiscible liquids
. For microencapsulation of liquid substances. The size of the resulting microcapsules is 100 – 150 microns. The drip method can be used here. A heated emulsion of an oil solution of a medicinal substance stabilized with gelatin (O/W emulsion) is dispersed in cooled liquid paraffin using a stirrer. As a result of cooling, the smallest droplets are covered with a quickly hardening gelatin shell. The frozen balls are separated from the liquid paraffin, washed with an organic solvent and dried.
“Spraying” method in a fluidized bed.
In devices such as SP-30 and SG-30. The method is applicable for solid medicinal substances. Solid kernels are liquefied by a stream of air and a solution of a film-forming substance is “sprayed” onto them using a nozzle. Solidification of liquid shells occurs as a result of evaporation of the solvent.
Extrusion method.
Under the influence of centrifugal force, particles of medicinal substances (solid or liquid), passing through the film of the film-forming solution, are coated with it, forming a microcapsule.
Solutions of substances with significant surface tension (gelatin, sodium alginate, polyvinyl alcohol, etc.) are used as film formers.
Physico-chemical methods.
Based on phase separation, they allow you to enclose a substance in any state of aggregation in a shell and obtain microcapsules of different sizes and film properties. Physicochemical methods use the phenomenon of coacervation.
Coacervation
– the formation in a solution of high-molecular compounds of droplets enriched with the dissolved substance.
As a result of coacervation, a two-phase system is formed due to stratification. One phase is a solution of a high molecular weight compound in a solvent, the other is a solution of a solvent in a high molecular weight substance.
The solution, which is richer in high molecular weight material, is often released in the form of coacervate droplets - coacervate droplets, which is associated with a transition from complete mixing to limited solubility. A decrease in solubility is facilitated by changes in system parameters such as temperature, pH, concentration, etc.
Coacervation during the interaction of a polymer solution and a low molecular weight substance is called simple. It is based on the physicochemical mechanism of adhesion, “raking into a heap” of dissolved molecules and separating water from them using water-removing agents. Coacervation during the interaction of two polymers is called complex, and the formation of complex coacervates is accompanied by the interaction between the (+) and (-) charges of the molecules.
Coacervation method
is as follows. First, the cores of future microcapsules are obtained by dispersion in a dispersion medium (polymer solution). The continuous phase is, as a rule, an aqueous solution of a polymer (gelatin, carboxymethylcellulose, polyvinyl alcohol, etc.), but sometimes it can also be a non-aqueous solution. When conditions are created under which the solubility of the polymer decreases, coacervate droplets of this polymer are released from the solution, which settle around the nuclei, forming an initial liquid layer, the so-called embryonic membrane. Next, the shell gradually hardens, achieved using various physical and chemical techniques.
Solid shells allow microcapsules to be separated from the dispersion medium and prevent the core substance from penetrating outward.
Chemical methods.
These methods are based on polymerization and polycondensation reactions at the interface of two immiscible liquids (water - oil). To obtain microcapsules by this method, first the drug substance is dissolved in oil, and then the monomer (for example, methyl methacrylate) and the appropriate polymerization reaction catalyst (for example, benzoyl peroxide). The resulting solution is heated for 15–20 minutes at t=55 °C and poured into an aqueous solution of the emulsifier. An O/W emulsion is formed, which is left to complete polymerization for 4 hours. The resulting polymethyl methacrylate, insoluble in oil, forms a shell around the droplets of the latter. The resulting microcapsules are separated by filtration or centrifugation, washed and dried.
Apparatus for drying tablet mixtures in a fluidized bed SP-30
Designed for drying powdered materials and tablet granules that do not contain organic solvents and pyrophoric impurities in the pharmaceutical, food, and chemical industries.
When drying multicomponent mixtures, mixing is carried out directly in the apparatus. In SP type dryers it is possible to powder tablet mixtures before tableting.
Specifications
Operating principle:
The air flow sucked into the dryer by the fan is heated in the heating unit, passes through the air filter and is directed under the mesh bottom of the product tank. Passing through the holes in the bottom, the air causes the granulate to be suspended. Humidified air is removed from the working area of the dryer through a bag filter, the dry product remains in the tank. Upon completion of drying, the product is transported in a trolley for further processing.
List of used literature
1.V.I. Chueshov, Industrial technology of drugs: textbook. – Kharkov, NFAU, 2002. 715 p.
2.material from lectures of the Department of General Pharmaceutical and Biomedical Technology, MMA named after. THEM. Sechenov
3. Concise Medical Encyclopedia
4. www.pharm.witec.com.
5.www.golkom.ru
6.www.gmpua.com
7.http:|//protabletki.ru
8.www.rosapteki.ru
What methods can be used to prolong the effect of drugs?
It has now been established that it is possible to ensure a prolonged effect (this means long-term) of therapeutic agents by reducing the rate of their release from the dosage form, reducing the rate and degree of deactivation of substances by enzymes, excretion from the body, and deposition of the drug in tissues and organs. It is a known fact that a drug reaches its maximum concentration when its content in the blood is directly proportional to the dose administered to the body and the rate of absorption, and is also inversely proportional to the rate at which the substance is excreted from the body.
To achieve a prolonged effect of drugs, you can use various methods, including chemical, physiological and technological.
We became familiar with the concept of “retard”; it is now known that it is used in medicines.
Who is retard
Gamers can call their friend a retard. This is part of slang, a generally accepted, widespread statement in this environment. Judging by the reaction of the gamer who was called a retard, one can understand that the fact of such treatment can outrage and anger. A person may begin to explain something for a long time, as if making excuses. It also happens that an address makes people laugh and forces everyone to unanimously change the topic of conversation. It always evokes a lively, chaotic reaction from the participants in the conversation.
They call it that when they want to touch a nerve. This word is used to give an impartial description. A retard is a slow-reacting gamer who thinks for a long time. The address is used, however, often as a joke, it conveys emotions and makes you think.
In the game, reflexes must work well, otherwise you can lose, and in a team game you can set your friends down. At the same time, no one will teach the rules. Each participant in the game has his own tactics and strategy. Retard often can only smile embarrassedly, because he is wrong. It can make you angry that the situation is out of control. In fact, nothing depended on him; his friends’ accusations were groundless. The reputation of a strong competitor is nevertheless spoiled, and the word retard may become a second nickname.
Can a professional gamer really be called a retard? Mistakes are familiar to all people. Once you become a retard, it’s easy to fix everything. New tactics and strategy will bring success. It will no longer be possible to call other players who made a mistake that way, but I still want to discuss the game. Emotions are overwhelming. Accordingly, there is really nothing to worry about. The nickname will remain the one the gamer chose when registering in the game.
What does this word mean
In English-speaking countries, the word retard can often be heard in pharmacies and on the street. The context can be anything. This word is found in literary works, movies, and the lyrics of popular songs. This is indeed the name, but not of an art gallery, a pub, but of medical supplies. Using an online translator, you can find out that it is used in the following senses:
- delay;
- slowdown;
- being late;
- delay;
- puff;
- guy
- lag;
- delay.
It can be used to talk about being late for work or the train, and other situations with appropriate meaning. But among gamers it once acquired a special secret meaning. A newcomer will not immediately understand what is being said; he will not know that he is being scolded or insulted. When you first ask how this expression is translated, you may be very surprised. Yesterday's friends will turn out to be opponents.
Physiological methods
Physiological methods include methods that ensure changes in the rate of absorption or excretion of a medicinal substance due to the influence of various factors (chemical, physical) on the body.
This is mainly achieved by the following methods:
- cooling the tissue in the place where the drug injection was administered;
- the use of a blood-sucking cup;
- introduction of hypertonic solutions into the body;
- the use of vasoconstrictors, that is, agents that promote vasoconstriction;
- inhibition of the excretory function of the kidneys (for example, etamide is used for this purpose to slow down the excretion of penicillin from the body), etc.
But it is worth noting that these methods can become unsafe for the patient, which is why they are very rarely used. For example, in dentistry, vasoconstrictors and local anesthetics are used together to prolong the local anesthetic effect of the latter by reducing the lumen of blood vessels. In this case, a side reaction such as tissue ischemia develops, due to which the supply of oxygen is reduced, and this leads to hypoxia, which can ultimately cause tissue necrosis.
Arifon® retard
UNDESIRABLE DRUG COMBINATION
— Lithium preparations:
With the simultaneous use of indapamide and lithium preparations, as well as when following a salt-free diet, an increase in the concentration of lithium in the blood plasma may be observed due to a decrease in its excretion, accompanied by the appearance of signs of overdose. If necessary, diuretics can be used in combination with lithium preparations, and the lithium content in the blood plasma should be carefully monitored and the dose of the drug should be adjusted accordingly.
COMBINATION OF DRUGS REQUIRING SPECIAL ATTENTION
— Drugs that can cause pirouette-type arrhythmia:
- class IA antiarrhythmic drugs
(quinidine, hydroquinidine, disopyramide); - class III antiarrhythmic drugs
(amiodarone, sotalol, dofetilide, ibutilide); - some neuroleptics:
phenothiazines (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoroperazine), benzamides (amisulpride, sulpiride, sultopride, tiapride), butyrophenones (droperidol, haloperidol); - others
: bepridil, cisapride, diphemanil, erythromycin (iv), halofantrine, mizolastine, pentamidine, sparfloxacin, moxifloxacin, astemizole, vincamine (iv).
Increased risk of ventricular arrhythmias, especially pirouette-type arrhythmias (risk factor - hypokalemia).
The concentration of potassium in the blood plasma should be determined and, if necessary, adjusted before starting combination therapy with indapamide and the above drugs. It is necessary to monitor the patient’s clinical condition, monitor the level of electrolytes in the blood plasma, and ECG indicators.
In patients with hypokalemia, drugs that do not cause ari should be used.
- Non-steroidal anti-inflammatory drugs (when administered systemically), including selective COX-2 inhibitors, high doses of acetylsalicylic acid (≥ 3 g/day):
The antihypertensive effect of indapamide may be reduced.
There is a risk of developing acute renal failure due to decreased glomerular filtration. Patients need to compensate for fluid loss and carefully monitor renal function at the beginning of treatment.
— Angiotensin-converting enzyme (ACE) inhibitors:
Prescribing ACE inhibitors to patients with an initially reduced concentration of sodium ions in the blood (especially patients with renal artery stenosis) is accompanied by a risk of sudden arterial hypotension and/or acute renal failure.
Patients with arterial hypertension and possibly reduced levels of sodium ions in the blood plasma due to diuretics should:
- 3 days before starting treatment with an ACE inhibitor, stop taking the diuretic. In the future, if necessary, the use of a non-potassium-sparing diuretic can be resumed;
- or begin ACE inhibitor therapy with low doses, followed by a gradual increase in dose if necessary.
For chronic heart failure
Treatment with ACE inhibitors should be started with the lowest doses, with a possible preliminary reduction in diuretic doses.
In all cases
In the first weeks of taking ACE inhibitors in patients, it is necessary to monitor renal function (plasma creatinine content).
- Other drugs that can cause hypokalemia: amphotericin B (iv), gluco- and mineralocorticosteroids (for systemic use), tetracosactide, laxatives that stimulate intestinal motility:
Increased risk of hypokalemia (additive effect).
Constant monitoring of the concentration of potassium in the blood plasma is necessary, and, if necessary, its correction. Particular attention should be paid to patients concomitantly receiving cardiac glycosides. It is recommended to use laxatives that do not stimulate intestinal motility.
- Baclofen:
There is an increase in the hypotensive effect.
Patients need to compensate for fluid loss and carefully monitor renal function at the beginning of treatment.
— Cardiac glycosides:
Hypokalemia enhances the toxic effect of cardiac glycosides.
With the simultaneous use of indapamide and cardiac glycosides, the concentration of potassium in the blood plasma, ECG readings should be monitored, and, if necessary, therapy should be adjusted.
COMBINATION OF DRUGS REQUIRING ATTENTION
— Potassium-sparing diuretics (amiloride, spironolactone, triamterene):
Combination therapy with indapamide and potassium-sparing diuretics is advisable in some patients, but the possibility of developing hypokalemia or hyperkalemia cannot be excluded (especially in patients with renal failure or in patients with diabetes mellitus).
It is necessary to monitor the concentration of potassium in the blood plasma, ECG indicators and, if necessary, adjust therapy.
— Metformin:
Functional renal failure, which can occur against the background of diuretics, especially loop diuretics, with simultaneous administration of metformin increases the risk of developing lactic acidosis.
Metformin should not be used if creatinine levels exceed 15 mg/L (135 µmol/L) in men and 12 mg/L (110 µmol/L) in women.
— Iodine-containing contrast agents:
In case of dehydration while taking diuretics, the risk of developing acute renal failure increases, especially when using high doses of iodine-containing contrast agents. Before using iodinated contrast agents, patients need to compensate for fluid loss.
— Tricyclic antidepressants, antipsychotics (neuroleptics):
Drugs in these classes enhance the antihypertensive effect of indapamide and increase the risk of orthostatic hypotension (additive effect).
— Calcium salts:
With simultaneous administration, hypercalcemia may develop due to a decrease in the excretion of calcium ions by the kidneys.
- Cyclosporine, tacrolimus:
It is possible to increase the creatinine content in the blood plasma without changing the concentration of circulating cyclosporine, even with normal fluid and sodium ion levels.
— Corticosteroid drugs, tetracosactide (if administered systemically):
Reduced hypotensive effect (retention of fluid and sodium ions as a result of the action of corticosteroids).
Technological methods
Technological methods have become the most common and are most often used in practice. In this case, the effect of the drug is prolonged using the following techniques:
- increasing the viscosity of the dispersion medium: this method is based on the fact that when this indicator of solutions increases, the process of absorption of the drug from the dosage form slows down;
- In addition to the use of non-aqueous media, aqueous solutions are also used, to which substances are added that increase viscosity - semi-synthetic, natural and synthetic polymers.
In pharmaceutical practice, the placement of active substances in hydrols of high-molecular compounds and in gels has also recently become widespread. They are used as prolongators, having a soft dosage form (liniments, ointments, patches), and also serving as components, or reservoirs, of macromolecular systems, not only of the matrix type, but also of the membrane type.
We now know that this is a retard.
Forte
This means increasing the dose, usually 2 times.
But some of them are exceptions. For example, “Hilak Forte” was originally called that, that is, the drug “Hilak” simply does not exist. Vitrum Prenatal vitamins for pregnant women do not contain some vitamins and minerals that are present in Vitrum Prenatal Forte. And traditionally in the latter the dose of ingredients is higher. If we take into account the previous Vitrum drugs, then since February 2022, Vitrum Plus, almost identical to its predecessor, has appeared on pharmacy shelves. One company bought a line of these vitamins from another and switched from a drug to a dietary supplement. The appearance of the tablets also changed - the shell became white instead of orange.
In addition to the removal of coloring, some minerals are no longer included in the supplement and the dosage of some vitamins has been reduced.
When considering blood pressure medications rather than dietary supplements, Plus usually means adding a diuretic to the drug. For example, Lozap Plus contains losartan and the diuretic hydrochlorothiazide.
