Eufillin, 24 mg/ml, solution for intravenous administration, 10 ml, 10 pcs.

Pharmacodynamics and pharmacokinetics

The mechanism of action of aminophylline (in Latin - aminophylline) is associated with its ability to block purine (adenosine) A2-type receptors of bronchial smooth muscle cells, increase the accumulation of cyclic AMP in tissues, suppress PDE, reduce the flow of Ca ions through plasma membrane channels (cell membranes), reduce contractile activity smooth muscle activity.

The effects of the drug manifest themselves as:

• relaxation of the bronchial muscles;
• stimulation of diaphragm contractions;
• increasing mucociliary clearance;
• improving the function of intercostal and respiratory muscles;
• stimulation of the respiratory center and increasing its sensitivity to CO2;
• improving alveolar ventilation.

All this helps to reduce the severity and frequency of episodes of respiratory arrest ( apnea ).

By normalizing breathing, it ensures better oxygen saturation of the blood and helps reduce CO2 concentration. Stimulates the activity of the heart muscle, increases the number and strength of its contractions, improves blood circulation through the blood vessels of the heart and increases the myocardial need for oxygen.

Reduces tension in the vascular walls, promotes dilation of peripheral vessels, reduces vascular resistance in the lungs, and reduces pressure in the pulmonary circulation.

It is a diuretic of moderate strength, increases the volume of blood flow in the kidneys, promotes the dilation of the bile ducts, suppresses platelet aggregation, increases the resistance of red blood cells to deformation (improves blood rheology), normalizes microcirculation and reduces thrombus formation.

Reduces the excitability and contractility of the myometrium (tocolytic effect), in high doses it has an epileptogenic effect .

Absorption from the gastrointestinal tract when taken orally is rapid. Food does not change its magnitude, but reduces its speed. The degree of absorption also depends on the dose: the higher it is, the slower aminophylline .

In a healthy adult, about 60% of the dose of aminophylline is bound to plasma proteins, in a patient with liver cirrhosis - about 35%, in infants during the newborn period - 36%.

TSmax for regular tablets is 60-120 minutes.

In the liver, part of the administered dose of aminophylline is biotransformed into caffeine . T1/2 of caffeine in children under 3 years of age is longer than in adults. The concentration of the substance in a child can reach 30% of the concentration of aminophylline .

In patients older than three years of age, the phenomenon of caffeine is not observed.

The T1/2 indicator is influenced by concomitant diseases and the patient’s age. In children under six months of age, as well as in adult patients with heart failure , COPD and cor pulmonale, it is more than 24 hours, in children over six months of age - 3.7, in non-asthmatic adults - 8.7, in people who smoke more than 20 cigarettes a day - 4-5 hours. After quitting smoking, it takes at least 3 months for the pharmacokinetics of the drug to normalize.

Eliminated by the kidneys, about 10% is excreted in pure form in adults, and about half of the taken dose of aminophylline is excreted in children.

Indications for use of Eufillin

Eufillin - what are these pills for?

Indications for use of Eufillin tablets:

• bronchial asthma (BA);
• Pickwick's syndrome (paroxysmal sleep apnea);
• chronic obstructive bronchitis (COB);
• chronic “pulmonary heart”;
• emphysema.

Eufillin is the drug of choice for exercise-induced asthma; for other forms of the disease it is used in combination with other drugs.

When is Euphyllin in ampoules prescribed?

Indications for Eufillin in ampoules are:

• broncho-obstructive syndrome due to bronchitis , asthma, cardiac asthma (mainly to relieve attacks) or emphysema ;
• cerebrovascular insufficiency of the brain (the solution is used in combination with other drugs to reduce intracranial pressure);
• hypertension in the pulmonary circulation;
• migraine;
• left ventricular failure , accompanied by periodic breathing of the Cheyne-Stokes type and bronchospasm (in combination with other drugs).

Composition and release form

The composition of the drug depends on the form of release of the drug. Eufillin is produced in the following versions:

• Pills. One piece contains the active substance - aminophylline (150 milligrams), as well as auxiliary components. The latter include calcium, stearic acid and potato starch.
• Ampoules (solution for injection). Aminophylline is also the main substance. Each ampoule contains 24 milligrams of the active ingredient. In addition to it, the composition also contains water for injection.

Contraindications for Eufillin solution and tablets

Contraindications to the use of tablets:

• intolerance to aminophylline or any other xanthine ;
• myocardial infarction (MI) in the acute stage;
• hypertrophic cardiomyopathy with obstruction;
• tachyarrhythmia;
• exacerbation of symptoms of stomach/duodenal ulcer ;
• severe functional impairment of the kidneys/liver;
• epilepsy;
• hyperthyroidism.

In pediatrics, it is not prescribed to children under six years of age, or in combination with Phedrine .

Injection of the drug is contraindicated in the following cases:

• hypersensitivity to aminophylline and other xanthine ;
• MI in the acute stage;
• angina pectoris;
• OSN;
• extrasystoles;
• paroxysmal tachycardia;
• severe arterial hypotension/hypertension;
• pulmonary edema;
• vascular atherosclerosis;
• hemorrhagic stroke;
• there is an indication of any spontaneous bleeding in the anamnesis;
• hemorrhage into the retinal tissue;
• peptic ulcer in the acute stage;
• epilepsy;
• increased threshold of convulsive readiness;
• gastroesophageal reflux (GER);
• uncontrolled hypothyroidism ;
• thyrotoxicosis;
• hyperthyroidism;
• porphyria;
• sepsis;
• kidney and/or liver dysfunction.

Due to the likelihood of side effects, it is not recommended to use the solution in children under 14 years of age. Children under three years of age are contraindicated to administer Eufillin intravenously; in children over three years of age, the medicine can be used for health reasons and for no more than 14 days.

Side effects

Side effects of using Eufillin tablets:

• sleep disturbances, anxiety, dizziness, convulsions, tremor;
• irregular heart rhythm, palpitations;
• hematuria , albuminuria ;
• hypoglycemia (rare).

Against the background of injection therapy, the following are possible:

• headache, anxiety, dizziness, agitation, irritability, tremor, insomnia ;
• arrhythmias , tachycardia (including in the fetus, if the woman took the drug in the 3rd trimester of pregnancy), palpitations, cardialgia , decreased blood pressure, unstable angina ;
• nausea, diarrhea , heartburn, gastralgia , vomiting, exacerbation of symptoms of peptic ulcer , GER, with long-term use - loss of appetite;
• itching of the skin, skin rashes, fever;
• tachypnea , chest pain, hypoglycemia , albuminuria , increased diuresis, hematuria , increased sweating, feeling of heat in the face.

Side effects are dose-dependent, that is, to relieve them, it is often enough to reduce the dose of the drug.

Local reactions to the injection of the solution manifest themselves in the form of skin hyperemia, pain and the formation of a seal at the injection site.

Side effects

When taking Eufillin, in addition to the main pharmacological action, side effects may also occur. Most often, patients develop insomnia, dizziness, weakness, tachycardia, arrhythmia, dyspeptic syndrome, allergic reactions, hypoglycemia, hypotension, increased sweating, pain in the head, chest and abdomen.

Against the background of a drug overdose, muscle cramps, increased body temperature, polyuria, hematuria, albuminuria and even disturbances of consciousness may occur.

To eliminate adverse symptoms, it may be necessary to reduce the dosage or stop taking the drug.

If the rules of asepsis and antisepsis are violated during injections of Eufillin, infectious complications sometimes develop.

Instructions for use of Eufillin

Eufillin tablets: instructions for use

The Vidal reference book states that the tablets should be taken orally after meals with plenty of liquid. The dosage of the drug is selected individually, taking into account the different rates of elimination of aminophylline in different patients.

If necessary, the dose is increased every three days until the desired effect is achieved.

Patients weighing more than 50 kg (including teenagers) are prescribed Eufillin for bronchitis and other conditions accompanied by bronchial obstruction at 450-900 mg/day, if necessary, the dose can be increased to 1.2 g with a frequency of use of 4 times ./day with an interval of 6 hours.

For patients weighing less than 50 kg and adolescents whose weight is in the range of 45-55 kg, Eufillin tablets are prescribed to take 450-600 mg/day.

For children 6-17 years old with bronchitis and other broncho-obstructive conditions, tablets are given at the rate of 13 mg/kg, usually 1 tablet 3 times a day.

For COPD in the acute phase, treatment begins with a dose of 5-6 mg/kg (for adults) with further increases. Serum concentration should not exceed 0.02 mg/ml. An increase in the dose for every 0.5 mg/kg leads to an increase in the concentration of the drug in the blood by 0.001 mg/ml.

Outside of an exacerbation, the initial dose of Eufillin for an adult with COPD is 6-8 mg/kg/day, the highest (in the initial stages of treatment) is 400 mg/day. It is recommended to divide it into 3-4 doses.

If used during pregnancy, the dosage (as well as the method of administration) is determined by the doctor. It should be borne in mind that for the mother, an overdose is associated with the risk of cardiac dysfunction (and sometimes cardiac arrest), and for the fetus, high doses of Eufillin are dangerous due to the likelihood of hypoxia and antenatal death.

Eufillin ampoules: instructions for use

For conditions that require emergency care, adult patients are advised to use an infusion with a loading dose of the drug: Eufillin is administered intravenously over half an hour at a dose of 5.6 mg/kg. To prepare a dropper, 10-20 ml of solution is combined with a similar volume of 0.9% aqueous NaCl solution and then the medicine is diluted in 0.25-0.5 liters of physiological solution.

During maintenance therapy, Eufillin is infused into the patient intravenously for 1-3.5 times at a dose of 0.9 mg/kg.

If the patient has previously taken theophylline , the dose of aminophylline should be reduced by at least half.

For status asthmaticus, 720 to 750 mg of aminophylline .

The permissible upper limit of the daily dose for an adult is 0.4-0.5 ml/kg.

Children under 3 months are administered intravenously from 30 to 60 mg of aminophylline per day; for older children and adolescents, the dose varies from 60 to 500 mg/day.

Intravenous injections of Eufillin in emergency conditions are performed for at least five minutes. A single dose for an adult is 6 mg/kg. Before giving the injection, the drug is diluted in 10-20 ml of a 0.9% aqueous solution of NaCl.

The daily dose for intramuscular administration is from 0.1 to 0.5 mg.

For children with COPD, Eufillin is administered at a dose of 5-6 mg/kg (initial dose); during maintenance therapy for children under six months of age, the drug is administered every 8 hours at a dose calculated by the formula: child’s age in weeks * 0.07 + 1, 7.

For children aged six months to one year, the maintenance dose is calculated using the formula: child’s age in weeks * 0.05 + 1.25. The interval between injections is 6 hours.

Children from one to 9 years old are administered 5 mg/kg, children 9-12 years old - 4 mg/kg, children 12-16 years old - 3 mg/kg every 6 hours.

Outside of exacerbation, the initial dose for a child is 16 mg/kg/day, the highest dose is 400 mg/day. It should be divided into 3-4 injections.

If necessary and if Eufillin is well tolerated, the dose is increased every couple of days by 25% to the highest daily dose, which for children under one year old is calculated using the formula “age in weeks * 0.3 +8”, for children under 9 years old it is 22, for children up to 12 years old - 20, for adolescents under 16 years old - 18, for patients over 16 years old - 13 mg/kg.

Eufillin is administered intramuscularly to children at a dose of 15 mg/kg/day. The maximum duration of parenteral use in children is 14 days.

For apnea in children of the first year of life (accompanied by bradycardia and cyanosis , in which the child does not breathe for periods of 15 seconds), the starting dose is 5 mg/kg (the medicine is administered through a nasogastric tube). When carrying out maintenance therapy, the child is recommended to use 2 mg/kg in two doses.

Treatment can last up to several months (usually several weeks).

Electrophoresis with Eufillin

Euphylline for electrophoresis in adults is used to treat arthrosis and osteochondrosis . For electrophoresis, it is prescribed to children for dysplasia , as well as when it is necessary to relieve muscle hypertonicity or reduce intracranial pressure .

In case of cerebrovascular insufficiency or intracranial hypertension , it is performed on the cervical vertebrae; in case of hypertonicity of the child’s legs, it is performed in the lumbar region.

Electrophoresis with Eufillin is a procedure that allows you to create the desired concentration of the active substance directly in the affected tissues. Acting locally, the medicine does not cause systemic side effects, so it can be used in infants older than one month.

The doctor places a gauze cloth soaked in Eufillin solution on the sore spot and secures the electrodes. Exposure time is 15 minutes. This is enough for the drug to penetrate deep into the tissue. The course of treatment is designed for ten sessions.

To restore organ function after birth injuries in newborns, cerebral circulation in pathologies of the cervical spine , as well as in cerebral palsy , electrophoresis according to Ratner is recommended.

The essence of this method is that the patient is placed on two pads impregnated with different drugs: the first (with Eufillin solution 0.5%) - on the cervical vertebrae, the second (with papaverine 1%) - on the ribs, to the right of the sternum. Exposure time is 15 minutes. Current strength is 1-2 mA.

It should be noted that both children and adults tolerate the procedure equally well, so in the absence of contraindications, it can be performed without any fear.

Electrophoresis is contraindicated for any skin diseases, arterial hypertension , arrhythmia , heart failure , or the presence of neoplasms in the patient (any location).

Inhalations with Eufillin for children - effective or inappropriate?

Prescription of Eufillin for children with cough and bronchial obstruction allows them to expand the bronchi, relieve spasm and facilitate the discharge of sputum. However, the drug has these effects only when it enters the systemic circulation.

The use of Eufillin for inhalation belongs to the “off-label” prescribing category. Despite the lack of instructions in the manufacturer's instructions regarding the possibility of using the drug in this way, many people often prescribe this treatment for themselves and, moreover, treat their children in this way.

Most doctors unanimously believe that the effectiveness of inhalations with Eufillin is extremely low, since when inhaling vapors, the drug settles on the mucous membrane and, therefore, does not enter the systemic bloodstream in a therapeutically effective concentration.

The positive effect on the bronchi (their relaxation and improvement of sputum discharge) is due to the fact that during inhalation water vapor enters them. This means that the effectiveness of the drug when used in inhalation is comparable to the effectiveness of ordinary water.

Eufillin for cellulite

One of the properties of aminophylline is the ability to dilate peripheral vessels and restore the functioning of the circulatory system, which in turn cannot. Cellulite, as is known, occurs when blood circulation is impaired and cells begin to suffer from a lack of oxygen. The use of Eufillin allows you to tighten the upper layers of the skin, remove excess fluid and reduce swelling.

For weight loss and getting rid of orange peel, the product is used in the form of creams, masks and wraps. Massage with Eufillin also gives a good effect.

To prepare the composition, the medicine should be mixed with any massage cream, and then add a small amount of Dimexide , which in this case will act as a transporter (thanks to it, aminophylline will be able to penetrate very deeply into the tissues).

For wraps, you can use a mixture of regular baby cream, Dimexide , Euphyllin and tangerine or lemon essential oil (6-8 drops). The composition is applied to the skin cleansed with a scrub and covered with cling film. While it “works” (impact time is usually about 30 minutes), it is recommended to move intensively to enhance the effect.

To prepare anti-cellulite cream based on Eufillin, use the following recipe:

• petrolatum;
• moisturizing cream;
• 1 powdered tablet or the contents of 1 ampoule (5 ml) of Eufillin (this dose of the drug is suitable for women weighing less than 75 kg);
• Dimexide (for one five-milliliter ampoule of solution, take 2 ml of Dimexide concentrate).

You can also add the drug to a ready-made pharmaceutical anti-cellulite product. The optimal proportion of ingredients is 1:5.

Reviews about Eufillin for cellulite can be found very different - some are completely dissatisfied with the result, others claim that the result exceeded all expectations. Based on this, we can draw the following conclusion - if the remedy works, then definitely not from the first procedure.

Overdose

The annotation states that overdose symptoms develop when the plasma concentration of aminophylline exceeds 0.02 mg/ml. Characteristics are:

• diarrhea;
• prolonged vomiting;
• facial hyperemia;
• excitation;
• arrhythmia;
• tremor;
• photophobia;
• convulsions.

When the blood concentration exceeds 0.04 mg/ml, the patient falls into a coma.

Helpful measures include stopping the administration of Eufillin to the patient and enhancing natural detoxification by stimulating kidney function (forced diuresis).

If the aminophylline exceeds 0.05 mg/ml, plasmapheresis , hemosorption , peritoneal dialysis or hemodialysis , respiratory support (ventilation and oxygen supply), and monitoring of hemodynamic parameters are indicated.

To relieve convulsive syndrome, the patient is administered diazepam (intramuscularly). The use of barbiturates is contraindicated!

Interaction

The effect of aminophylline is enhanced by use in combination with furosemide , ephedrine, caffeine , and β-adrenergic stimulants .

When used simultaneously with phenytoin , phenobarbital , isoniazid , rifampicin , sulfinpyrazone , carbamazepine of aminophylline is observed , which is accompanied by a decrease in its therapeutic effectiveness and may require an increase in the dose used.

Acceleration of aminophylline is also observed in heavy smokers (at least 20 cigarettes per day).

Use in combination with drugs from the macrolide group, allopurine , isoprenaline , COCs , cimetidine , lincomycin , viloxazine , fluvoxamine , disulfiram , β-blockers , influenza vaccines leads to a slower elimination of aminophylline , an increase in its plasma concentration and, consequently, a reduction in the dose of Euphyllin.

If the drug is prescribed in combination with drugs of the fluoroquinolone group, the dose of Eufillin is reduced to 25% of the usually recommended one.

Aminophylline weakens the therapeutic effect of Li drugs and β-blockers. β-blockers, in turn, weaken the bronchodilator effect of aminophylline .

When taking Eufillin together with corticosteroids (for example, with dexamethasone ), diuretics and β-adrenergic agonists, hypoglycemia increases .

Aminophylline may cause side effects of fluorinated derivatives of general anesthesia ( ventricular arrhythmias ), mineralocorticosteroids (hypernatremia), and drugs that excite the central nervous system ( neurotoxicity ).

May enhance the effect of anticoagulants .

The solution is incompatible with solutions of acids, fructose, glucose and levulose. When preparing for intravenous infusion of an infusion solution, it is necessary to take into account the pH of the solutions used.

Should be used with caution in combination with purine derivatives , theophylline derivatives , and anticoagulants . During the treatment period, it is prohibited to take substances that contain xanthines (including tea and coffee).

In one syringe, Eufillin solution can only be mixed with isotonic NaCl solution.

Practical recommendations for the treatment of shortness of breath

Definition

Shortness of breath (dyspnea) is a subjective feeling of lack of air. Like pain, it is caused by both an objective condition and the patient’s individual reaction to this symptom. Dyspnea limits general daily and social activities, leading to loss of independence, loss of social role, and later, as it progresses, to anxiety, fear, sleep disturbance, depression and hopelessness. In some patients, shortness of breath and associated anxiety do not clearly correlate with the feeling of shortness of breath. So, in the presence of severe shortness of breath and visual signs of anxiety, the patient may not feel that he is short of air. On the contrary, with a normal breathing rate, patients sometimes complain of a pronounced feeling of lack of air. It is anxiety about the lack of air that is the only trait that significantly correlates with shortness of breath.

Prevalence

COPD ‒ 90–95%, oncology ‒ 50–77%, CHF ‒ 60–90%.

Prognostically, shortness of breath is divided into the following three groups:

• shortness of breath on exertion (prognosis = months to years);
• shortness of breath at rest (prognosis = weeks to months);
• terminal dyspnea (prognosis = days to weeks).

Causes

Obstructive:

• narrowing of the lumen of small bronchi, especially bronchioles of spastic origin (bronchial asthma, asthmatic bronchitis);
• narrowing of the airway lumen due to thickening of the walls of the bronchi (inflammatory, allergic, bacterial edema, edema due to hyperemia, heart failure);
• the presence of a viscous secretion on the bronchial mucosa, with an increase in its production by goblet cells of the bronchial epithelium, or mucopurulent sputum, or blood;
• narrowing of the airways due to cicatricial deformation of the bronchi;
• development of endobronchial tumor;
• compression of the bronchi from the outside, including by a tumor replacing the lung parenchyma, spread of lymphangitis to the interalveolar septa;
• presence of bronchiolitis.

Restrictive (arise as a result of impaired alveolar ventilation due to limited stretching of the lungs, impossibility of straightening the lungs):

• pulmonary fibrosis (interstitial fibrosis, scleroderma, pneumoconiosis, etc.);
• large pleural and pleuro-phrenic adhesions;
• exudative pleurisy, hydrothorax, hemothorax;
• pneumothorax;
• extensive inflammation of the alveoli, pneumonia;
• large tumors of the lung parenchyma;
• surgical removal of part of the lung.

Hemodynamic:

• obstruction of the superior vena cava;
• heart failure;
• pulmonary embolism.

Neuromuscular:

• weakness of the respiratory muscles (neurological disease, infection (poliomyelitis));
• asthenia;
• paralytic drugs, etc.

Other organs : anemia.

Psychogenic : anxiety, fear, family problems, spiritual and other problems. Often there is a combination of reasons, which allows us to talk about the symptom of “total shortness of breath” by analogy with the symptom of “total pain”.

Condition assessment:

• determination of the degree of severity (intensity) of shortness of breath - according to the patient, you can use the N merological Rating Scale ( NSS ) (Fig. 1) or the Visual Tax Scale ( VAS ) ; this is important both for the initial assessment and for assessing the effectiveness of treatment;

• identifying factors that alleviate or increase shortness of breath, determining blood oxygen saturation in the presence of a pulse oximeter;
• identification of psycho-emotional (fears, anxiety, etc.) and social unfavorable factors;
• degree of physical activity;
• Determination of overall quality of life, prognosis and planning (for example, assistance in organizing the receipt of an oxygen concentrator or, in the case of increasing shortness of breath against the background of a sharp deterioration in general condition, planning the management of shortness of breath in the last days of life with the patient and family).

General principles of assistance

Elimination of reversible causes, if possible (Fig. 2):

• obstruction of the superior vena cava - urgent transfer to a specialized department (for patients with a life prognosis of more than 2-3 months); prescribing large doses of corticosteroids (Dexamethasone 16 mg orally or subcutaneously or Prednisolone 60 mg orally; at the same time provide protection to the gastric mucosa);
• treatment of bronchospasm;
• treatment of pulmonary edema;
• treatment of pneumonia;
• treatment of pleural effusion (thoracentesis);
• treatment of severe anemia (blood transfusion);
• palliative interventions: radiotherapy, laser treatment, stenting (for patients with a life prognosis of more than 2–3 months).

Non-drug interventions involving an interdisciplinary team:

• presence of relatives and medical staff; important: explain and reassure, help with social problems;
• comfortable position in bed with the head end raised;
• cool air (open window, fan, hand fan at a distance of 20–30 cm from the face);
• relaxation practice, breathing exercises;
• planning physical activity in accordance with the condition;
• oxygen (not indicated for all patients): prescribed for hypoxemia (decrease in blood oxygen saturation less than 90%) and for those who feel relief when using it (given through a mask, nasal catheters 1-3 l/min can be titrated to 6 l/min) . Check every 20–30 minutes. When normoxemia is reached (94–98%) - cancel. Remember that incorrect administration of oxygen can have serious, even fatal, effects. For example, in patients with ventilatory hypercapnic insufficiency (COPD, etc.), whose activity of the respiratory center depends on hypoxia, a lower target level of blood oxygen saturation should be used: 88–92%.

Drug treatment

Bronchodilators, mucolytics

Even with seemingly absent clinical signs of bronchospasm during shortness of breath, a positive effect can be achieved from their use.

• Salbutamol/Ventolin 2.5–5 mg 4 times a day by nebulizer or 2 puffs/pressures 4 times a day through a spacer.
• Ipratropium/Atrovent 250–500 mcg 3 times a day by nebulizer or 2 puffs/pressures 3–4 times a day through a spacer.
• Saline solution 5 ml via nebulizer can help in thinning sticky sputum.
• Ambroxol/Lazolvan through a nebulizer for viscous sputum.

Important
Attention! Salbutamol can cause tachycardia, tremor and agitation with prolonged use!

Corticosteroids

They reduce peritumoral edema, reduce shortness of breath with multiple pulmonary metastases and with carcinomatous lymphangitis. The positive effect should appear within 7 days of their use. Try 4 to 8 mg orally daily for 1 week. For lymphangitis or airway obstruction - 8–16 mg per day. Prescribe in the morning to ensure protection of the gastric mucosa. Discontinue gradually if there is no effect after one week of treatment.

Opioids

Reduce respiratory effort and perception of shortness of breath; effective for refractory shortness of breath, shortness of breath at rest and in the terminal stage; improvement is noticeable with low doses that do not cause respiratory depression, so titration of opioids is necessary. At the same time, laxatives should be prescribed to prevent constipation, and antiemetics to prevent nausea and vomiting.

For patients not taking morphine, the following dosages are used:

IF THE PATIENT CAN SWALLOW*

The initial dose is 2.5–10 mg orally as needed, titrated in 5 mg increments.

If more than 2 doses per day: prescribe on a regular basis (3-6 times a day) with a further transition to modified-release morphine.

IF THE PATIENT CANNOT SWALLOW

The initial dose is 2.5–5 mg subcutaneously, the titration step is 5 mg.

If more than 2 administrations per day: prescribe on a regular basis 3-6 times a day with a further transition to prolonged infusions.

The following dosages are used for patients taking morphine:

• Severe dyspnea: 100–150% of breakthrough morphine dosage**
• Moderate dyspnea: 50–100% of breakthrough morphine dosage
• Mild shortness of breath: 25–50% of breakthrough morphine dosage

A maximum of 6 additional doses can be used in 24 hours for all indications - breakthrough pain, shortness of breath and cough. Dosages must be titrated. If the patient cannot tolerate morphine due to side effects, then a second line of opioids for dyspnea or rotation of opioids should be considered.

* In January 2021, Morphine solution for oral administration was registered in the Russian Federation in dosages of 2 mg/ml, 6 mg/ml, 20 mg/ml (5 ml in a plastic ampoule), which allows for more accurate and safe titration.

** Dosage for “breakthrough” pain / “breakthrough” - 1/5–1/6 of the daily dosage of morphine.

Benzodiazepines

Relieves restlessness and anxiety associated with severe shortness of breath, but is less effective for shortness of breath than opioids and should be the third line of treatment for patients who do not respond to non-pharmacologic approaches and opioids:

• Lorazepam sublingually 0.5 mg every 4–6 hours as needed;
• Diazepam/Relanium orally 2–5 mg at night if there is prolonged anxiety
• Midazolam/Dormicum subcutaneously 2–5 mg every 4–6 hours as needed if it is not possible to give the medication orally or sublingually.

For shortness of breath, accompanied by severe restlessness, anxiety, and insomnia, use the entire range of measures and medications listed above, with an emphasis on selecting (increasing) the dose of available benzodiazepines and opioids. Antipsychotics (Haloperidol) are indicated for patients who are anxious and delirious.

Psycho-emotional support and the constant presence of someone caring next to the patient is necessary to reassure and be able to assess changes in the patient’s condition. Make changes to ongoing activities as necessary.

Diuretics

Prescribed for severe congestion in the lungs is 20–40 mg Furosemide subcutaneously. It should not be prescribed on an ongoing basis for shortness of breath due to hypoalbuminemic edema.

Shortness of breath in the last days and hours of life, refractory shortness of breath

Diazepam can be used on an outpatient basis or at home. In a hospital setting - Midazolam, depending on the severity of anxiety, shortness of breath, age and condition:

• initial dose 2.5–5 mg, subcutaneously with a gradual increase if necessary to 10–30 mg (initial dose can reach 0.4–0.8 mg/kg). Assess every 10–20 minutes and can be maintained with low levels of sedation if dyspnea is controlled satisfactorily;
• maintenance therapy: continuous subcutaneous infusion (still quite rarely used in Russian practice), intravenous infusion (maintenance dose is determined individually, maximum 0.2 mg/kg/hour), usually 10–60 mg/24 hours are sufficient (average values) with constant monitoring of the level of shortness of breath and consciousness;
• hyoscine butyl bromide (Neoscapan, Spanil, Buscopan) subcutaneously 20 mg every hour for wheezing, noisy breathing and secretions in the respiratory tract; if necessary, up to 120 mg/24 hours, or atropine subcutaneously 200–300 mcg (0.2–0.3 ml of 0.1% solution) every 4–6 hours.

Practical points

• Non-pharmacological measures to relieve shortness of breath are important. As the disease progresses, drug treatment to relieve shortness of breath becomes increasingly necessary.
• Prescribing opioids in low doses and carefully titrating the dose is safe and does not lead to respiratory depression in patients with cancer, airway obstruction, and patients with heart failure.
• Plan interventions to relieve dyspnea in the last days of life with the patient and family:

* discuss the possibility of sedation in case of uncontrollable anxiety;

* medications to relieve symptoms;

* resolve the issue of consultations at night.

Talk to the patient

Tell the patient and caregivers that shortness of breath in itself is not life-threatening. Explain: “You will not suffocate or die.” Agree on realistic goals; Help the patient and his family get used to the idea that gradual deterioration is inevitable.

Help the patient cope with loss of social role, abilities, etc.

Help the patient improve functionality: Encourage physical effort during shortness of breath to maintain or improve physical fitness. Use walking aids. Adequate exercise should be encouraged. The required physical activity is determined individually, in accordance with the patient’s goals, his disease, somatic status and prognosis.

Explain to the patient and his family

How to breathe more efficiently

Shallow, rapid breathing is ineffective - this type of breathing leads to the development of anxiety and panic. During controlled breathing, patients are advised to take full inhalations and exhalations, relaxing the neck, shoulder girdle, and upper chest to promote calm and relaxed breathing. It is advisable to minimize the work of breathing and create a sense of control in the patient's breathing. The goal is to engage the diaphragm, not the accessory muscles. Patients should breathe through their nose and perform passive exhalation 1.5–2 times longer than inhalation.

How to breathe better with COPD

Breath control techniques can be combined with pursed lip breathing in patients with severe COPD who suffer from dynamic hyperextension. The technique involves inhaling through the nose and exhaling through partially closed lips. Some patients do this intuitively. This technique is not suitable for patients with severe hyperextension of the lung tissue and a flattened diaphragm, since breathing at rest depends on the work of the accessory muscles.

How does body position affect breathing efficiency?

Specific positions may help with shortness of breath in certain circumstances. They can be recommended to patients if they have not yet intuitively mastered these techniques. For example:

• for COPD: while sitting, lean forward, place your hands/elbows on your knees or on the table, this will increase the pressure in the abdominal cavity, increasing the efficiency of the flattened diaphragm. The position of the hands fixes the shoulder girdle, which increases the efficiency of contraction of auxiliary muscles and breathing in general;
• in case of unilateral bronchopulmonary disease (for example: collapse, compaction, pleural effusion), you should lie on the side of the healthy lung; this will maximize the ventilation-perfusion ratio. Unfortunately, this advantage is lost in cases of severe pleural effusion.

A patient who uses accessory muscles for breathing can increase its efficiency by fixing the position of the arms. This can be placing your hands behind your head - in a sitting position, or resting your hands on the wall, on your hips, on your belt - in a standing position.

How to use the fan

Many patients experience relief when cool air is blown onto the face, possibly due to stimulation of facial and naso-pharyngeal cold receptors. The ventilator is mainly used to relieve shortness of breath after exercise. It is recommended to keep it at a distance of 15–20 cm from the face, pointing it towards the nose and mouth.

Why are opioids prescribed for shortness of breath?

In general, opioids are more helpful for patients who experience shortness of breath at rest rather than just with exertion. Even at maximum exertion, breathing restores itself within a few minutes, that is, much faster than required by the administration and onset of action of opioids. Therefore, non-drug options are of paramount importance for shortness of breath from exercise.

Morphine and other opioids reduce the response to hypercapnia, hypoxia, and exercise, reducing respiratory effort and dyspnea. Improvements are noticeable at dosages that do not cause respiratory depression.

Opioids are also needed for patients with severe COPD who suffer from shortness of breath that is not relieved by conventional treatments. Research supports the effectiveness of oral and parenteral opioids, but not via nebulizer.

Will oxygen help the patient with shortness of breath?

• Even a stream of fresh air from a fan or from an open window can significantly help the patient;
• recent studies have shown that morphine has a greater calming effect on shortness of breath than oxygen;
• in the last hours of life, in the absence of respiratory distress, oxygen should not be used, even with severe hypoxemia;
• In most patients receiving oxygen, it can be discontinued without worsening the condition.

Thank you for your help in preparing the materials:

Kravchenko T.V. (Chief Physician of the State Budgetary Healthcare Institution, Center for Emergency Medicine, Department of Healthcare),

Gurkin S.P. (Deputy Chief Physician for the organization of inpatient care of the State Budgetary Healthcare Institution of the Central Clinical Hospital of the Department of Healthcare),

Ibragimova A. N. (Head of the branch “First Moscow Hospice named after Vera Millionshchikova” of the State Budgetary Healthcare Institution of the Center for Emergency Medicine of the Department of Healthcare),

Brusnitsyn V.N. (Head of the 3rd department of the State Budgetary Healthcare Institution of the Center for Emergency Medicine of the Department of Healthcare),

List of sources:

1. Abuzarova G.R. Nevzorova D.V. Pain management in palliative care. Practical guide for the doctor. Moscow, 2021.
2. Chronic pain syndrome (CPS) in adult patients requiring palliative care, 2021. ICD 10: R52.1/ R52.2.
3. Introducing Palliative Care Fifth Edition. Editors Twycross R., Wilcock A., 2021.
4. Hospice and Palliative Care Training for Physicians. Unipac Self-Study Program, 2008.
5. Lanarkshire Palliative Care Guidelines, 2012.
6. ProCare HospiceCare. Hospice Medication Utilization Guidelines. Eds. S. Shah, M. Madison.

You can download the guide in pdf format here: Practical recommendations for the treatment of shortness of breath. 2021.pdf

special instructions

The bronchodilator effect of the drug occurs when the concentration of the active substance reaches 0.01-0.02 mg/ml. A concentration exceeding 0.02 mg/ml is toxic.

The stimulating effect on the respiratory center is realized when the content of aminophylline in the blood is in the range from 0.005 to 0.01 mg/ml.

In newborn infants and people over 55 years of age, the medicine is used with caution due to the insufficient activity of the liver enzymatic systems involved in the biotransformation of aminophylline .

In geriatrics, aminophylline should be used in minimal doses while monitoring the plasma concentration of aminophylline .

During the treatment period, you should not eat foods that contain xanthine derivatives: mate, chocolate, coffee, cocoa, strong tea.

The solution is heated to body temperature before administration.

What are the advantages of this drug administration regimen?

• Minimal number of side effects, because the drug enters the body bypassing the digestive tract
• Local exposure with a high concentration of the substance helps deliver the medicine directly to the pathology area without saturating the entire body
• The procedure is painless and non-invasive; during the procedure the patient does not experience pain, there is no damage to the skin and mucous membranes
• Prolonging the effect of a medicinal substance, creating a kind of “depot” with a drug in the skin, which provides a long-lasting therapeutic effect and allows you to reduce the dosage of the drug
• The effect of the drug is enhanced by direct electric current
• The effectiveness of other non-drug treatment methods used in the Prognoz clinic is increasing.

Analogs

Level 4 ATC code matches:
Aerophyllin

Theotard

Teopek

Theophylline

Aminophylline

Neophylline

Analogs of Eufillin: Aminophyllin-Eskom , Eufillin-pharm , Eufillin-Darnitsa .

Drugs with a similar mechanism of action: Diprophylline , Neo-Teofedrine , Neoteopek A , Teobiolong , Theobromine , Theotard , Teofedrine-N , Theophylline .

Eufillin during pregnancy

The manufacturer, in the instructions for Eufillin, warns that the use of solution/tablets during pregnancy may create concentrations of aminophylline and caffeine that are potentially hazardous to the health of the fetus/newborn.

Children whose mothers received the drug during pregnancy (especially in the third trimester) should be under medical supervision during the neonatal period to monitor possible symptoms of intoxication with methyl xanthine derivatives.

Prescription of Eufillin during pregnancy and lactation is possible only for extreme health reasons and requires an assessment of possible risks for the fetus/child.

Why can Eufillin be prescribed during pregnancy?

Gynecologists recommend the use of Eufillin for edema during pregnancy, for placental insufficiency, in the complex treatment of gestosis , as well as for other conditions that require urgent use of this medicine due to a threat to the life of the mother.

There is no clear treatment regimen for Eufillin during pregnancy, since the manufacturer’s instructions list pregnancy as one of the contraindications for use. The doctor makes all appointments depending on the condition of a particular patient.

Reviews of Eufillin during pregnancy allow us to conclude that the medicine is far from harmless (some women say that after the dropper they felt a strong heartbeat, weakness and dizziness), but for many it helps them to return to normal.

Reviews about Eufillin

The drug is most often used to treat diseases accompanied by airway obstruction , therefore most of the reviews about Eufillin are reviews of its use for bronchitis and asthma .

People who have taken the medicine note that the drug effectively relieves attacks of painful coughing, accelerates the removal of mucus and makes breathing easier. Moreover, improvement occurs literally within 10 minutes after taking the tablet or administering the solution.

During pregnancy (if used correctly in accordance with the doctor's recommendations), the medicine helps to remove excess fluid, normalize the condition and avoid hospitalization in the department of pathology of pregnant women.

There are few negative reviews about the drug and they are primarily associated with individual sensitivity to its active substance.

A separate category of reviews about Eufillin are reviews about the use of tablets and solution for weight loss and against cellulite. For cellulite, the drug is used as an additive to the main anti-cellulite agent, as well as in combination with Dimexide and essential oils.

It is quite difficult to judge the effectiveness of Eufillin against cellulite, since reviews of the results of its use in cosmetology are quite contradictory. Most women claim that it is possible to achieve smooth skin with the help of the drug, but the effect usually becomes noticeable after completing the full course of procedures.

Reviews about the drug

Reviews of Euphylline, like any other medicinal drug, are very diverse on the Internet. However, most patients note its high effectiveness and rapid elimination of symptoms of the disease.

There are also negative reviews, but they are most often associated with the development of adverse reactions due to individual intolerance to a component of the drug or as a result of an incorrectly selected dosage.

Some patients use Eufillin in combination with Dimexide and a number of essential oils for weight loss and getting rid of cellulite. The effectiveness of the drug in this regard has not been proven, so it is impossible to objectively judge its effectiveness.

Attention! Before taking the medicine, consultation with a specialist is required. Only a doctor will be able to select the correct dosage of the drug, calculate the duration of the course of treatment and take into account all the indications and contraindications for taking Eufillin. Otherwise, there is a high risk of developing negative side effects.

Eufillin price

The price of Eufillin tablets (150 mg No. 30) in Russian pharmacies is 10-12 rubles, a 2.4% solution in 5 ml ampoules (package No. 10) can be bought for 35 rubles, in 10 ml ampoules (package No. 10) - for 40 rubles

In Ukraine, the cost of tablets is from 13 UAH, the price of Eufillin ampoules is from 21 UAH.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

ZdravCity

• Eufillin solution for intravenous injection.
  24 mg/ml 10 ml 10 pcs. JSC Novosibirsk Chemical Plant 110 rub. order
• Eufillin tablets 150 mg 30 pcs. Pharmstandard-Leksredstva OJSC

  34 RUR order

Pharmacy Dialogue

• Eufillin (amp. 2.4% 10ml No. 10)Novosibkhimpharm OJSC

  96 RUR order

• Eufillin (amp. 2.4% 5ml No. 10) DHF JSC

  46 RUR order

• Eufillin (tab. 150 mg No. 30 (bl.)) Usolye-Sibirsky Chemical Physics Complex

  32 RUR order

• Eufillin (tab. 150 mg No. 30 (bl.)) Ozon LLC

  34 RUR order

• Eufillin (tab. 150 mg No. 30 (bl.)) BZMP

  20 rub. order

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Pharmacy24

• Eufillin-pharm 0.4 g No. 30 capsules TOV VTF "Farmakom", Ukraine
  23 UAH. order
• Eufillin-N 200 2% 5 ml No. 10 solution PAT "Farmak", Ukraine

  22 UAH order

• Eufillin-Darnitsa 2% 5 ml No. 10 solution

  30 UAH order

• Eufillin-pharm 0.25 g No. 40 tablets TOV VTF "Farmakom", Ukraine

  17 UAH order

• Eufillin-pharm 0.25 g No. 80 tablets TOV VTF "Farmakom", Ukraine

  31 UAH order

PaniPharmacy

• Eufillin ampoule Eufillin 200 solution d/in. 2% amp. 5ml No. 10 Ukraine, Darnitsa ChAO

  33 UAH order

• Eufillin ampoule Eufillin solution d/in. 2% amp. 5ml No. 10 Ukraine, Health LLC

  30 UAH order

• Eufillin-pharm tablets 0.25g N40 Ukraine, Farmakom PTF LLC

  17 UAH order

• Eufillin-pharm tablets 0.25g N80 Ukraine, Farmakom PTF LLC

  30 UAH order

• Eufillin-pharm capsules 0.4g No. 30 Ukraine, Farmakom PTF LLC

  24 UAH order

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