Wikipedia intranasally

Posted on by admin

Intranasal method of drug administration

To date, medical science has come up with many ways to introduce drugs into the human body. Each of them has advantages and disadvantages.

Table of contents:

Each should be applied promptly and correctly.

When a person reads the instructions for use of a pharmacological drug and comes across a new formulation, he may become confused, not knowing what to do. Thus, the phrase “use intranasally” can be confusing.

In fact, there is nothing complicated about it. Let's figure out what this means. Let's consider the existing forms of drugs for intranasal administration. Let's understand what their pros and cons are. Let's find out which medications do not make sense to use intranasally.

What does it mean to use intranasally?

With the intranasal route of administration, the medication is introduced into the body through the nasal cavity. Simply put, if you see the word “intranasal” in the instructions for use of a medicine, then it should be administered through the nose.

We deliberately do not use the word “drip”, since intranasal drugs are not only available in the form of drops, which means that using this term in this context is not entirely correct. But this will be discussed in the next section of our article.

Also, you should now understand the word “nasal”. It is usually used in conjunction with the release form of the drug. For example, nasal drops. That is, in this case, it should be clear to us that such drops should be instilled into the nose.

Dosage forms of intranasal drugs

Currently, the pharmacological industry produces three forms of intranasally administered drugs:

Now we understand why the word “drip” cannot be applied to all nasal medications. So, the nasal cavity should be irrigated with sprays, and the ointment should be placed in the nasal passages.

But which dosage form is best to use?

When answering this question, you first need to focus on the recommendations of your doctor. Then carefully read the instructions for use of the product. And only after that apply the knowledge acquired on the Internet on medical portals.

The most preferred form of intranasal medications is sprays. Their advantages:

  • ease of use;
  • accuracy of medication dosage;
  • maximum coverage of the nasal mucosa;
  • rapid absorption of the active substance.

In the case of sprays, we should not talk about the disadvantages, but about one limitation. They cannot be used to treat newborns and infants. In the annotations of different sprays, the children's age at which they can be used varies. Usually it is within 1 to 2 years. Check the instructions for the medicine you choose for details.

The main disadvantage of nasal ointments is that no matter how hard you try to distribute them over the surface of the nasal mucosa, it is almost impossible to do this. Additionally, read the article “Nasal ointment for a runny nose.”

Intranasal nasal drops have even greater problems with covering a significant area of ​​the nasal mucosa. As soon as you tilt your head a little at the wrong angle, they completely flow into the nasopharynx. In this case, the effect of treatment is largely lost.

In addition, both ointments and intranasal drops have serious problems with the accuracy of dosages. As you understand, you won’t be able to measure them by eye. And in their case, built-in dispensers, as is the case with aerosol sprays, are most often not provided.

What types of intranasal medications are there?

Currently, a fairly wide range of pharmacological agents for intranasal use is produced. These include the following drugs:

  • vasoconstrictors;
  • antihistamines;
  • glucocorticosteroids;
  • antiviral;
  • immunomodulators;
  • antibiotic.

Of course, the most commonly used medications are nasal medications for nasal congestion.

What medications should not be taken intranasally?

Remember not to use nasal medications with antibiotics. There are three main points that explain why this statement of ours is true.

Firstly, an antibiotic will only act on a bacterial infection when a sufficient concentration has accumulated in the tissues of our body. The intranasal route of taking antibiotic drugs does not allow this to be achieved.

Secondly, this method of using antibiotics leads to the appearance of bacteria in the human nasal cavity that are immune to antibacterial therapy. If they cause any complications, it will be unclear how to treat them.

Thirdly, intranasal administration of an antibiotic into the nose contributes to the appearance and development of allergic reactions to its repeated use.

All materials are for informational purposes only.

Before using the information received, consult your doctor.

Questions and suggestions:

Copying of materials is permitted only with an active link to the source.

Source: http://rinitanet.ru/nazalnye-kapli-i-sprei/intranazalno.html

Intranasal - how is it?

It’s clear that through the nose, HOW? just bury it?

Questions on the topic

You can view the value in the official source here http://www.gripp.ru/dict.aspx

By Addendum #1

Administration can be a drip or a spray. Depends on the drug. You can also read here http://www.antibiotic.ru/index.php?article\u003d703

nose spray

Well, if it drops, then drip, obviously. instructions for whom?

Well, yes, just into the nasal cavity. How exactly depends on the dosage form: a spray is injected, drops are instilled, an ointment is applied, the powder is inhaled.

Just on the nose. what other options are there?

The company http://webrega.ru/ - “WEBREGA.RU” (professional website promotion) is a guarantor of your success!

You can see the full list of tariffs on our website.

advertising on the Internet search engine promotion of websites optimization and

Source: http://medicina.moi-vopros.ru/answer/478119/intranazalno—eto-kak

Intranasally

Intranasally - drugs enter the body through the mucous membrane of the nasopharynx, having first passed through the nasal openings.

The following medication options are also possible:

Oral - taking medication by mouth by swallowing the medication. The main dosage forms for oral administration are solutions, powders, tablets, capsules and pills. The method has many disadvantages and a number of features that reduce efficiency.

Parenteral - infusion, injection, inhalation - without entering the stomach

intramuscularly. One of the most common methods of administering small volumes of drugs. Muscles have an extensive network of blood and lymphatic vessels, which creates good conditions for the absorption of drugs. Intravenous - the introduction of liquids, drugs or blood preparations/components into a venous vessel.

Source: http://pro-gaimorit.ru/intranazalno/

What does "intranasal" mean? Where is this term used? What are some examples?

Intranasal - "intra" - inside, "nasal" - nasal. Refers to the passage of a drug or solution through the nasal cavity. The term is usually used in medicine. An example is ordinary nasal drops, for example, Nazivin, which are used intranasally.

But besides them, you can instill into the nose not only drugs to treat the nose, but also for other organs. Sometimes they even give vaccinations through the nose.

Intranasal administration is one of the many ways to introduce a drug into the body. Intranasal means that the medicine, which can be a spray (aerosol), ointment or drops, is injected into the nasal cavity. The big advantage of this method is that the active substance is rapidly absorbed, but it should be used with caution when treating young children. The intranasal route of drug administration is used to treat many diseases.

Intrasally. This term is used most often in medicine. In fact, this is a method of delivering the active drug substance to the human body to obtain a real therapeutic effect. As an example, we can cite nasal drops.

Source: http://www.bolshoyvopros.ru/questions/chto-znachit-intranazalno-gde-primenjaetsja-etot-termin-kakie-primery.html

intranasal

Universal Russian-English dictionary. Akademik.ru. 2011.

See what “intranasal” is in other dictionaries:

Semax - Active ingredient ›› Semax (Semax) Latin name Semax ATX: ›› N06BX Other psychostimulants and nootropics Pharmacological group: Nootropics Nosological classification (ICD 10) ›› I64 Stroke, not specified as hemorrhage or heart attack... ... Dictionary of medical drugs

Thymogen - (inter. Glutamyl Tryptophan, lat. Glutamyl Triptophan) is a peptide immunomodulator, which is a chemically synthesized dipeptide Glu Trp (glutamyl tryptophan), identical to the natural compound isolated by chromatography ... ... Wikipedia

Dysfunctional uterine bleeding - uterine bleeding in the puberty, reproductive and premenopausal periods, caused by a violation of the functional state of the hypothalamus-pituitary-ovarian-adrenal system. Depending on the presence or absence of ovulation (see... ... Medical Encyclopedia

Immunization - I Immunization (lat. immunis free, free from anything; synonym: immunoprophylaxis, protective vaccinations, preventive vaccinations) specific prevention of infectious diseases of people and animals. Immunoprophylaxis of a number of ... ... Medical encyclopedia

Afrin - Active ingredient ›› Oxymetazoline* (Oxymetazoline*) Latin name Afrin ATX: ›› S01GA04 Oxymetazoline Pharmacological groups: Alpha adrenergic agonists ›› Anticongestants Composition and dosage form 1 ml solution for intranasal use... ... Dictionary of medications

Buserelin - Active ingredient ›› Buserelin* (Buserelin*) Latin name Buserelin ATX: ›› L02AE01 Buserelin Pharmacological groups: Hormones of the hypothalamus, pituitary gland, gonadotropins and their antagonists ›› Antitumor hormonal agents and... ... Dictionary of medications

Minisem - Latin name Minicem ATX: ›› N06BX Psychostimulants and other nootropics Pharmacological group: Nootropics Nosological classification (ICD 10) ›› F81 Specific disorders of the development of learning skills ›› G46 Brain vascular syndromes... ... Dictionary of medications

Semax solution 0.1% - Active ingredient ›› Semax (Semax) Latin name Solutio Semaxi 0.1% ATX: ›› N06BX Other psychostimulants and nootropics Pharmacological group: Nootropics Nosological classification (ICD 10) ›› F07.2 Post-concussion syndrome › › F43.9… … Dictionary of medications

Parenteral administration of drugs is a route of introducing drugs into the body in which they bypass the gastrointestinal tract, in contrast to the oral route of drug administration. These are primarily injections and inhalations. There are other, rarer ones... ... Wikipedia

DACRYOCYSTORHINOSTOMIA - DACRYOCYSTORHINOSTOMIA, dacryocy storhinostomia, operation, with the help of a cut, a direct connection between the lacrimal sac cavity and the nasal cavity is established, bypassing the nasolacrimal canal. Proposed instead of enucleation of the lacrimal sac in cases ... ... Great Medical Encyclopedia

Share link to highlight

Direct link:

We use cookies to give you the best experience on our website. By continuing to use this site, you agree to this. Fine

Source: http://universal_ru_en.academic.ru//%D0%B8%D0%BD%D1%82%D1%80%D0%B0%D0%BD%D0%B0%D0%B7%D0%B0% D0%BB%D1%8C%D0%BD%D1%8B%D0%B9

How to administer drugs intranasally?

Currently, doctors have begun to use a new method of administering the drug - intranasal (through the nose).

Previously, this method was also used, but only for the administration of anti-inflammatory drugs and exclusively for local treatment of rhinitis. At this stage of development in medicine, they began to more actively use the intranasal method of administering medications to treat many diseases, including osteoporosis, migraines, conjunctivitis, as well as inflammatory processes occurring in the nasopharynx. In addition, intranasal vaccination is currently used.

Release form

Intranasal administration is carried out using sprays, which can be produced in the form of a can with a dispenser containing compressed air. The latest innovation was the release of a can equipped with an active spray pump. This form of release of the drug is very convenient, because in this way you can control the dosage with extreme precision. In addition, the medicine completely irrigates the nasal mucosa, which allows it to achieve its maximum pharmacological effect. All of the above arguments determine the fact that the spray is the most preferred form of intranasal drugs.

The restriction on the use of such sprays is age up to 2 years.

The form of release of drugs administered intranasally is not limited to sprays and includes ointments and drops.

The choice of drug release form depends directly on the disease. In any case, this issue should be discussed with your doctor.

Advantages and disadvantages

Among the advantages, it can be noted that using this method of administration, the drug does not participate directly in the primary metabolism of the liver. This happens because the drug is administered through the nasal cavity, which is enriched with blood vessels, due to which the required dose of the drug quickly enters the blood. It is also worth noting that this is a fairly safe method, because intranasal administration does not damage the mucous membrane in the nasal cavity.

The ease of use of a pharmaceutical drug is another undoubted advantage of the intranasal route of administration, which is especially important for the category of patients undergoing treatment at home.

Flaws

  1. As for the disadvantages of this method, it is necessary to note the bioavailability factor. The physiology of the nasal cavity is complex and has its own individual characteristics. This creates a need for different bioavailability of the active substance in each individual patient.
  2. The second disadvantage is such side effects as the development of local reactions: the appearance of irritation on the nasal mucosa, the occurrence of sinusitis, rhinitis, or complete loss of smell. However, this largely depends not on the method of administration as such, but on the drug (its composition, dosage, course duration).
  3. It is also worth noting that if the drug is administered intranasally, it is quickly absorbed into the mucous membrane. This fact makes it impossible to use this method long-term for therapeutic purposes.

Drugs that can be administered intranasally

The intranasal route of administration is possible when using the following groups of drugs:

  • antiallergic;
  • vasoconstrictors;
  • antibiotic;
  • hormonal;
  • antihormonal;
  • antiviral;
  • narcotic analgesics;
  • psychostimulants;
  • nootropics;
  • correctors of metabolism of bone and cartilage tissue;
  • immunostimulants.

Features of intranasal vaccination

One method of administering vaccines is intranasal, or aerosol. The technique of such vaccination involves spraying the vaccine into the nasal passages using a special device. Drops can also be used for these purposes. Doctors believe that this method makes it possible to create an immunological barrier on the mucous membranes, increasing the body’s resistance to airborne infections.

However, this method also has disadvantages. In particular, this is the insufficiency of immunity to fight infections that have already penetrated the mucous membranes of the upper respiratory tract. Disadvantages also include significant spillage of the drug during direct vaccination.

Precautionary measures

Despite the fact that drugs with the intranasal route of administration do not require special skills or additional drugs, one must remember that the drug itself may be intolerable to certain patients. For example, many drugs with this release form are recommended to be used with extreme caution by those individuals who are predisposed to allergic reactions.

It goes without saying that the dosage and duration of use of these drugs should be prescribed and monitored by a doctor.

Another important indicator is the compatibility of drugs. Situations often arise when the simultaneous use of pharmaceutical products of different nature is indicated. In this case, it is necessary to consult with a specialist and find out whether such a method will have an adverse effect on the body, affecting the functioning of the organs and systems of the body.

Source: http://gaimoritstop.ru/intranasalnoe-vvedenie.html

Intranasal use

Intranasal use - section Medicine, Methods of using medicines In the nose (Intranasal) Medicines are used in the form of powders, vapors (amyl nitrite.

Medicines are used in the nose (intranasally) in the form of powders, vapors (amyl nitrite, ammonia vapor), solutions and ointments. They have local, resorptive and reflex effects. Absorption through the nasal mucosa occurs very quickly. Powders are drawn into the nose by a stream of inhaled air: closing one nostril, the powder is inhaled through the other. The drops are administered with a pipette, while the patient's head should be tilted back. Apply the ointment with a glass spatula. Lubrication is carried out by the doctor with a cotton swab wound onto the probe. After lubrication, the swab is discarded and the probe is sterilized in a disinfectant solution. Recently, special dispenser sprays have been used for intranasal administration, in which medicinal substances are in the form of solutions or suspensions with the addition of substances that increase viscosity to slow down the evacuation of the drug from the nasal cavity.

This topic belongs to the section:

Methods of using medicines

External use of drugs is designed mainly for their local action. They are absorbed only through intact skin. Injecting medications into the ears. Medicines are instilled into the ears with a pipette, see the Ear Care section in the Chapter Oil solutions of medicinal substances.

If you need additional material on this topic, or you did not find what you were looking for, we recommend using the search in our database of works: Intranasal use

What will we do with the received material:

If this material was useful to you, you can save it to your page on social networks:

All topics in this section:

In modern practical medicine there is not a single area in which it has not been successfully used

A nurse, without the knowledge of a doctor, has no right to prescribe or replace one medication with another. If the drug is given to the patient by mistake or its dose is exceeded, the nurse will

Medicines are applied to the skin in the form of ointments, emulsions, solutions, tinctures, mash, powders, pastes. There are several ways to apply the drug to the skin. • Lubrication (shir

When treating eye lesions, solutions of various medicinal substances and ointments are used (see the “Eye Care” section in Chapter 6). The purpose of application is local effect. It is necessary to be careful under

For various diseases of the respiratory tract and lungs, drugs are administered directly into the respiratory tract. In this case, the medicinal substance is administered by inhalation - inhalation (lat.

In the treatment of catarrhal inflammation of the upper respiratory tract and sore throats, steam inhalations using a simple inhaler have long been used. A jet of steam generated in a heated water tank

Parenteral (Greek para - near, near, entern - intestines) is the method of introducing medicinal substances into the body, bypassing the digestive tract (Fig. 11-3). I distinguish

Intradermal injection is used for diagnostic purposes (Burnet, Mantoux, Casoni, etc. allergy tests) and for local anesthesia (needling). For diagnostic purposes, 0.1-1 ml of substance is administered

Subcutaneous injection is performed to a depth of 15 mm. The maximum effect of a subcutaneously administered drug is achieved on average 30 minutes after injection. The most convenient site

Intramuscular injections should be carried out in certain places of the body where there is a significant layer of muscle tissue and large vessels and nerve trunks do not pass close to the injection site. Most n

Venipuncture (Latin vena - vein, punctio - injection, puncture) - percutaneous insertion of a hollow needle into the lumen of a vein for the purpose of intravenous administration of drugs, blood transfusions and blood

Infusion, or infusion (Latin infusio - infusion), is the parenteral introduction of a large volume of liquid into the body. Intravenous drip infusion is performed to restore blood volume, detoxifier

The procedure for prescribing and receiving medications by departments of a medical institution consists of the following stages. A selection of doctor's orders from medical records.

The head of the department is responsible for the storage and consumption of medicines, as well as for order at storage sites, compliance with the rules for issuing and prescribing medicines. Principle of storage of medicinal media

Poisonous and narcotic medicines are stored in safes or iron cabinets. On the inside of the cabinet (safe) doors, the inscription “Group A” is written and a list of poisonous and narcotic drugs is placed.

Want to receive the latest news by email?
Subscribe to Our Newsletter
News and information for students
Advertising
Related material
  • Similar
  • Popular
  • Tag Cloud
  • Here
  • Temporarily
  • Empty
About the site

Information in the form of abstracts, notes, lectures, coursework and dissertations have their own author, who owns the rights. Therefore, before using any information from this site, make sure that you are not violating anyone else's rights.

Source: http://allrefs.net/c49/47ye5/p5/

Intranasal administration is a promising route of drug administration

Intranasal use of drugs is a long-known and currently quite widely used route of administration for a number of drugs. It is used for vaccination, treatment of migraines, osteoporosis, sexual dysfunction, and even for insulin replacement therapy. The benefits of this route of administration are most obvious when using drugs that are not intended for oral administration and are usually administered by injection. The advantages of intranasal administration are ease of implementation, convenience for the patient and relatively low cost.

At the same time, there are some problems with intranasal administration of drugs. These include differences in physiological processes in the nasal cavity in different people, the presence of pronounced protective mechanisms, the development of local complications and low bioavailability of drugs, leading to the need to use special “absorption enhancers”, which in turn can damage the mucous membranes of the nasal cavity.

Therefore, when developing an intranasal method of administering a particular drug, a detailed study of its mechanisms of action, as well as the physicochemical characteristics of the drug itself, is extremely important. For example, the safety of intranasal use of local anti-inflammatory drugs has been confirmed by research and experience in their clinical use, while at the same time, too little data is available on the local effects of systemic drugs administered intranasally.

The low bioavailability of drugs when administered intranasally is associated with the functioning of a special family of 25 proteins that make up the nasal mucosa and control the transport of all molecular and cellular objects that penetrate the mucosa.

To increase intranasal absorption of drugs, Nastech proposed the use of recently discovered non-toxic substances that bind to mucosal proteins according to the principle of receptor interaction and open transport channels. At the same time, the bioavailability of drugs increases by 30-50%, which is 3-6 times higher than the effectiveness of using traditional “absorption enhancers”. The second way to solve the problem of low bioavailability is the development of new formulations of drugs and technical means for intranasal administration.

The most important feature of intranasal administration of drugs is the possibility of their penetration directly into the central nervous system. Scientists believe that the transport of drugs from the nasal cavity to the central nervous system occurs without the participation of the mucous membrane, through the extracellular route along the trigeminal and olfactory nerves. Within minutes, chemical agents administered intranasally are detected in the brain. This fact attracts everyone's attention because it provides revolutionary new opportunities in the treatment of diseases of the central nervous system. Theoretically, drugs penetrate the brain only from the olfactory region, where there is the possibility of extra- and intracellular penetration of drugs through the epithelial barrier and entering not into the bloodstream, but directly to the membranes of the brain.

Previous animal experiments have yielded encouraging results, but extrapolation of these data to intranasal use of drugs in humans should be done with great caution, since there are marked differences in the distribution of mucous secretions carrying the drug within the nasal cavity in humans and animals. In particular, in humans, too little of the drug substance is delivered directly to the olfactory area and the required concentrations are not achieved. Moreover, the possibility of direct transport of a drug into the central nervous system can only be assessed in an experiment using drugs that do not penetrate into the bloodstream and with it into the brain structures. However, even with the proven possibility of a direct effect on the central nervous system when drugs are administered intranasally in humans, special endoscopic equipment will have to be used to deliver them to the olfactory area, since conventional sprays do not allow achieving a sufficiently high concentration of the drug in this area.

Thus, intranasal administration of drugs is fraught with great opportunities. Already, there are twice as many dosage forms in development for intranasal use as for intravenous administration.

Sniffing out profit

Scrip Magazine July/August, 2003.

intranasal administration, absorption enhancer, intranasal, extracellular intracellular pathway, trigeminal olfactory nerve

Source: http://www.antibiotic.ru/index.php?article=703

Interferon (Intranasal administration)

Interferon administered intranasally causes an effect only on the surface of the mucous membrane of the nasopharynx, since it is not absorbed into the blood. The effect is short-lived, as the drug is quickly inactivated. It is used for the prevention and treatment of acute respiratory viral infections, influenza, viral eye diseases, and herpes zoster.

At the same time, the severity and duration of the disease in patients are reduced, various complications arise less, and the healing of tissues damaged by the pathological process is accelerated. Complications with this use of interferon are usually not noted. Highly purified (!) interferon preparations can be administered by injection intravenously, intramuscularly, subcutaneously, intraosseously, intralumbarally. However, from the bloodstream it penetrates poorly into tissues, and in the blood it quickly undergoes inactivation.

Therefore, its high concentrations are not created in the plasma and especially in the lymph. Thus, after intravenous administration, the half-life of β-interferon is 2 hours, after intramuscular administration - 2.3 hours, after subcutaneous administration - 1.7 hours. In this case, the ratio of interferon concentration in blood plasma to concentration in lymph ranges from 1 to 5 (after intravenous administration ) or from 1 to 2 (after intramuscular injection).

It should be noted that β-interferon is quickly captured and inactivated by the liver, and α-interferon more slowly (Bocci V., 1982). N. Yoshikawa et al. (1983) developed a method that facilitates the absorption of interferon from the colon (using special surfactants or lipid solutions obtained in the form of micelles). At the same time, significantly higher concentrations are created in the blood plasma and especially in the lymph, which persist for 5 or more hours.

“Pediatric pharmacology”, I.V.Markova

Sulfanilamide drugs - derivatives of sulfanilic acid - are active chemotherapeutic agents that are effective in the treatment of diseases caused by resistant strains of pathogens to antibiotics, as well as in the treatment of children who have severe allergic reactions to them. All sulfonamides are characterized by a fundamentally similar mechanism of bacteriostatic action. Their structure is similar to para-aminobenzoic acid, and microorganisms (which do not synthesize it...

Nalidixic acid can cause a number of serious complications. The most dangerous effect is hepatotoxicity. Therefore, in case of liver dysfunction, the drug is not recommended. In addition, when using this drug, dyspeptic and allergic reactions may occur; sometimes dysfunction of the central nervous system, accompanied by headache, dizziness, etc. As already mentioned, nalidixic acid cannot be prescribed simultaneously with nitrofurans. Oxolinic acid (gramurin),…

Most sulfonamides penetrate well into all tissues, cerebrospinal fluid (CSF). Therefore, they can be used in the treatment of diseases of various localizations, including inflammation of the meninges. The only exceptions are drugs that are poorly absorbed from the gastrointestinal tract. Sulfadimethoxine also penetrates poorly into the CSF, so it is not suitable for the treatment of meningitis. Sulfapyridazine readily penetrates into the CSF. With prolonged administration, its concentration...

Metronidazole (Flagyl, Trichopolum) - a derivative of nitroimidazole - has long been used to suppress Trichomonas, Giardia and intestinal amoebae. Since 1962, information began to appear about its ability to suppress anaerobic infection. It is currently believed that 90% of known anaerobic microorganisms are sensitive to it. It inhibits antibiotic-resistant strains of Bacteroides fragilis, CI. perfringens, as well as spirochete pallidum….

An increased concentration of acetylated derivatives in the urine can lead to crystalluria and sedimentation in the urinary tract, blockage of the kidney tubules. To accelerate the excretion of sulfonamide metabolites in the urine and prevent nephrolithiasis, it is necessary to prescribe the child plenty of fluids and alkaline medications. These conditions of administration must be observed when using sulfadimezine, sulfazine, streptocide, nor sulfazole, sulfacyl. These drugs are ineffective in…

The information on the site is for informational purposes only and is not a guide for self-medication.

Source: http://www.medkursor.ru/deti/farmokol/inf/1891.html

Development of intranasal drug delivery systems

Published in the magazine:

Department of Pathophysiology, Faculty of Medicine, Moscow State Medical Dental University

Until recently, drugs with predominantly local effects were used intranasally, mainly to relieve the symptoms of rhinitis. In recent years, it has been shown that active absorption of a number of medicinal substances can occur in the nasal cavity, which are also broken down in the gastrointestinal tract, in particular, this applies to hormones and substances of protein-peptide nature. Due to the convenience and ease of use, the speed of achieving maximum concentration in the blood, there is an active development of the pharmaceutical market for drugs for intranasal use that have systemic effects.

One of the specific ways of administering drugs is to spray them in the nasal cavity. It is based on the ability of a number of medicinal substances (DS) to be absorbed in the mucous membrane of the nasal cavity and enter the systemic bloodstream. Despite the fact that until recently, intranasal administration of drugs was predominantly used as local therapy (for example, for rhinitis), in recent years, the administration of those drugs that subsequently have a systemic effect has become of greatest importance [2] (see table).

Table 1 Some drugs for intranasal use that have a predominantly systemic effect [3]

The main advantages of intranasal use of drugs are:

  • the presence of a central action of the drug (due to the fact that the sheaths of the olfactory nerves lack a blood-brain barrier, drugs from the nasal cavity can immediately enter the brain)
  • high bioavailability
  • lack of first pass effect through the liver and associated adverse reactions
  • convenience and ease of use, which leads to improved patient compliance
  • speed of development of the systemic effect

Restrictions on the use of intranasal agents:

  • possible irritation or contact sensitization of the nasal mucosa, the cause of which is the unfavorable interaction of active or inactive components with the mucous membrane
  • only a small percentage of the drug can enter the systemic circulation. This means that an excess amount of the drug must be manufactured and put into the aerosol can, which ultimately leads to an increase in the cost of the drug.
  • intranasal drug delivery system can be used for drugs; possessing certain physicochemical properties to penetrate the systemic circulation in a therapeutically effective amount
  • the impossibility of ensuring a constant, without fluctuations, concentration of the drug in the blood and associated adverse reactions

Researchers pay special attention to the possibility of intranasal use of drugs that are not absorbed orally or are destroyed in the gastrointestinal tract, in particular drugs of a peptide or protein nature. To date, more than 30 protein-peptide hormones are known that are absorbed when administered intranasally. In particular, it was found that cholecystokinin has a long-term effect on the functional activity of the central nervous system when administered intranasally, while with other routes of its administration, its complete destruction in the gastrointestinal tract or rapid degradation under the influence of blood plasma enzymes is noted [25].

When administered orally, many protein-peptide hormones and drugs are inactivated by enzymes of the gastrointestinal tract. Even when using liposomes that protect drugs from destruction by digestive enzymes, the problem of chemical modification of drugs during their passage through the liver remains (the phenomenon of “first passage through the liver” or first passage). Since the portal vein receives blood from the entire intestine, except the lower part of the rectum, the phenomenon of the first passage of drugs through the liver can be avoided when they are administered rectally. However, the processes of drug absorption in the lower part of the rectum are not intensive, in particular, most substances of a protein-peptide nature are practically not absorbed. Therefore, currently the main route of administration of protein-peptide drugs is injection. This route is invasive and often requires the participation of medical personnel. Unlike injection administration, intranasal use of drugs is non-invasive and, as a rule, does not require the special participation of medical personnel. Moreover, due to the rapid absorption of the drug in the nasal cavity, the rate of development of the therapeutic effect with intranasal administration is comparable to the injection route. Typically, the systemic effect of intranasal use of drugs develops within 5-10 minutes after their use [24].

However, intranasal use of drugs has a number of limitations. In particular, the beating speed of epithelial cilia is 5 mm/min, so if drugs are administered simply in the form of liquid or powder, they are not quickly absorbed and are easily excreted from the body with mucus. An attempt to overcome this problem has been the inclusion of surfactants in finished dosage forms, but they have the potential to lead to irritation and inflammation of the nasal mucosa and increase the potential allergenicity of the drug. Currently, for intranasal administration of drugs, special dispenser sprays (meter-dose nebulizer) are most often used, while at the same time the issue of drug dosage is resolved, since with each press a strictly defined amount of the active substance is released. Typically, drugs in nebulizers are in the form of solutions or suspensions with the addition of special substances that increase the viscosity of the dosage form in order to slow down the evacuation of the active substance from the nasal cavity. In metering aerosols, drugs are under pressure (approximately 3 atm), which prevents bacterial contamination [2].

Another problem that arises with intranasal use of drugs is inflammatory and degenerative diseases of the nasal cavity. In particular, banal rhinitis can significantly accelerate the evacuation of a number of drugs and their bioavailability when administered intranasally [1]. To date, the influence of inflammatory and degenerative diseases of the nasal mucosa on the bioavailability of drugs and the rate of their absorption, and, consequently, on the effectiveness of their therapeutic use, has been practically not studied. This limits the possibility of widespread therapeutic intranasal use of drugs. Only for some drugs have studies been conducted on comparative bioavailability and pharmacokinetics for different routes of administration. These data are given below.

The main developers of intranasal forms of drugs are Nastech (USA) and California Biotechnology Inc. (USA). Nastech has more than 20 forms of intranasal medications approved by the FDA. California Biotechnology Inc. developed a special intranasal drug delivery system, Nazdel, containing tauro-24,25-dihydrofusidate to increase the permeability of the mucous membranes of the nasal cavity. In addition, California Biotechnology Inc. is the owner of a patent protecting a method for transmucosal delivery of peptides. Researchers at the Royal Danish School of Pharmacy have developed a new form of intranasal drug delivery - bioadhesive microspheres, which ensures long-term contact of the drug with the nasal mucosa, thereby prolonging the form of the drug. Microspheres have a size of microns, otherwise they are easily removed. Drugs contained in microspheres are also protected from enzymatic destruction in the nasal cavity [21].

Let us consider in more detail the features of the pharmacokinetics of a number of drugs with intranasal administration.

When 2 mg of lorazepam was administered intranasally to healthy volunteers, the bioavailability of the drug was shown to be similar to that of intramuscular administration (77.7+/-11.1%). In this case, intranasal administration of the drug leads to a faster entry of the drug into the systemic circulation and the achievement of maximum concentration [29].

When studying the comparative pharmacokinetics of midazolam, a hypnotic from the group of benzodiazepines (intravenous and intranasal administration), it was revealed that in both cases the drug elimination time is the same. The sedative and anxiolytic effect during intravenous administration developed 3-4 minutes after administration, while increasing the dose of midazolam from 0.2 to 0.4 mg/kg was accompanied by a pronounced increase in sedation. With intranasal administration, the sedative effect developed within 5 minutes. Despite the fact that the bioavailability of midazolam with intranasal administration was 64%, the sedative effect of a dose of 0.2 mg/kg was comparable to that with intravenous administration of 0.4 mg/kg midazolam. With intranasal administration of 0.4 mg/kg midazolam, the development of drowsiness was observed [21].

With intranasal administration of 2 mg of diazepam to 9 healthy volunteers, it was shown that the bioavailability of the drug was 50.4%, the time to reach maximum concentration in the blood was 5 minutes. The therapeutic effect was comparable to that of intravenous administration [16]. A similar result is described in the works of Bjorkmanetal. (1997), Bursteinetal. (1997) [8, 10].

Intranasal administration of narcotic analgesics and their analogues ensures high bioavailability and rapid achievement of maximum concentration. In particular, the biavailability of buprenorphine is about 50% [22], apomorphine% [17], and oxymorphine - 43% [20]. Intranasal administration of heroin leads to the same rapid development of mental effects as intramuscular administration, however, with this method of administration of the drug no side development of local reactions is observed [20].

Leo (Sweden) has developed an intranasal form of nicotine used for smoking cessation. Peak concentrations of nicotine in the blood are reached after 7.5 minutes, whereas when chewing gum it occurs after 30 minutes. In addition, when administered intranasally, dyspepsia and nausea do not develop [2].

Of particular importance is the absorption of interferons in the nasal cavity. Through the membranes of the first pair of cranial nerves, interferons enter the brain [28], where they have not only immune [30], but also regulatory significance [9]. In the absence of inflammation of the meninges, no other routes for the entry of interferons into the central nervous system have been found [26]. Unlike other routes of interferon administration, intranasal use of the drug provides the greatest effectiveness with the least number of adverse reactions [6, 11].

As a means of preventing ARVI, interferons are considered emergency measures. Thus, it takes time for the effects of vaccination or immunomodulation to manifest; Interferon preparations can be used immediately after contact with a patient with ARVI or at the first symptoms of the disease. Even if the first symptoms of ARVI appear, intranasal use of interferons allows one to avoid the manifestation of the disease in more than 80% of cases [11]. Recombinant a2-interferon when administered intranasally is more effective than human one [6].

IRS19, which is an aerosol for intranasal use, contains antigenic determinants of 19 strains of bacteria that are the most common causative agents of respiratory tract infections. The drug has a specific and nonspecific effect on the immune system. The nonspecific effect is to increase the phagocytic activity of macrophages, increase the content of endogenous lysozyme and interferon. Extensive clinical trials have shown the high effectiveness of the drug in respiratory diseases, including those of a sluggish or chronic nature [4].

It was revealed that intranasal administration of corticosteroids makes it possible to reduce the dose of drugs required for administration to patients with allergic diseases and, accordingly, reduce the number of adverse reactions during therapy. In particular, with long-term use of beclomethasone propionate. administered in the traditional way, children are stunted. Meanwhile, with intranasal use of beclomethasone propionate aerosol for one year, no significant changes in the growth and development of children were found [27]. Similar data were obtained when studying the intranasal form of triamcinolone. In addition, it has been proven that only with intranasal administration, long-term use of triamcinolone does not affect the functioning of the hypothalamus-pituitary-adrenal cortex axis. Based on these data, intranasal corticosteroids were recommended as the first choice in the treatment of allergic rhinitis [15].

With oral, intravenous, intranasal and inhalation administration of beclomethasone dipropionate to healthy volunteers, it was found that with oral and intranasal administration of the drug its bioavailability is 95%, and with inhalation it is 62%. Compared with other routes of administration, intranasal administration resulted in the highest concentration in the blood of its active metabolite, beclomethasone-17-monopropionate [13].

In the estrogen pulse therapy study, 36 women with postmenopausal disorders were randomly assigned to receive 17b-estradiol intranasally at 100, 300, 450 mcg/day or orally at 2 mg/day. In contrast to oral administration, a maximum concentration of 17b-estradiol is observed in the blood within a minute after intranasal administration. At a dose of 300 mcg/day intranasally, other pharmacokinetic parameters are indistinguishable from a dose of 2 mg/day orally [14].

Randomized administration of 17b-estradiol intranasally at a dose of 300 mcg/day, orally at a dose of 2 mg/day, or placebo was used to treat 659 women during menopause. The duration of therapy was one year. All women also received oral dihydroesterone at a dose of 10 mg/day for 14 days of a 28-day cycle. In the groups receiving 17b-estradiol, the change in the Kupperman index, which characterizes the severity of menopausal disorders, was significantly more significant than in the group receiving placebo. The decrease in blood triglyceride levels was more pronounced in the group receiving oral hormone replacement therapy (compared to intranasal hormone replacement therapy). The incidence of mastopathy in the group receiving 17b-estradiol intranasally was 1%, orally - 6%. Thus, intranasal administration of 17b-estradiol as hormone replacement therapy turned out to be slightly less effective, but also associated with a lower incidence of adverse reactions than oral therapy [23].

There are conflicting data regarding intranasal insulin use. Jacobs et al. (1993) on healthy volunteers showed that intranasal administration of insulin is comparable in pharmacokinetic parameters to subcutaneous administration. Since intranasal administration does not cause pain, inflammation at the injection site, lipodystrophy, and this route of administration is non-invasive, it is preferable for the treatment of type 1 diabetes mellitus [18]. A different result was described by Hilsted et al. (1995). Intranasal administration of insulin to patients with type 1 diabetes mellitus ensures the same rapid release of the hormone into the blood as subcutaneous administration. However, the bioavailability of insulin when administered intranasally is significantly lower: to achieve the same effective concentration in the blood, it is necessary to increase the dosage by approximately 20 times compared to subcutaneous administration [19].

Based on the Nazdel system, Eli Lilly (USA) developed an intranasal form of insulin. It is believed that the drug is better tolerated by patients with type 1 diabetes mellitus, and will also be effective in a number of patients with type 2 diabetes mellitus. According to analysts, within 5 years, revenues from the sale of intranasal forms of insulin may exceed $10 million [2].

GlaxoSmithKline has developed an intranasal form of inactivated influenza vaccine. It not only contributes to the formation of systemic immunity, but also stimulates the local immunity of the nasal cavity, which is usually the entry point for infection [5]. For emergency prevention and treatment of colds, Merck Co. (USA) has developed a drug sprayed into the nasal cavity and containing monoclonal antibodies that block the introduction and spread of the rhinovirus. Unlike other drugs containing monoclonal antibodies, this drug does not affect systemic immunity [1].

Thus, the intranasal use of drugs with not only local but also systemic action is a promising area of ​​medicine. In many cases, it allows one to avoid the injection route of administration and reduce the number of adverse reactions to the therapy. In addition, with intranasal use of drugs, a change in their pharmacological effects is sometimes observed, which can later be used in clinical medicine.

Recently a lot of intranasal drugs with local effect are used to relieve the symptoms of rhinitis. It was found that there is an active absorption in the nasal cavity of some medicines, which can disintegrate in gastro-intestinal tracts, eg hormones and proteins. There is an active development of intranasal medicines with systemic effects because of their facility, simple usage and celerity of maximum drug concentration. These new drugs allow to avoid injections and advers events during therapy.

Source: http://medi.ru/info/12291/