Papaverine: instructions for use, indications during pregnancy, dosage. Detailed instructions for use "Papaverine

Article content: classList.toggle()">expand

Papaverine is a fairly well-studied and effective drug that has proven itself in the pharmaceutical market. High efficiency and democratic cost allows this medicine to remain popular for many years.

Release form and mechanism of action

The drug is produced in the form of ampoules of 1 ml, which contain 20 mg of papaverine hydrochloride and in the form of tablets of 10 mg No. 10.

Papaverine is a remedy that relaxes muscles, relieves spasm and lowers blood pressure. In fact, it is an alkaloid found in opium.

The drug has a relaxing effect on the vessels and smooth muscles of the internal organs, and also reduces their tone.

Papaverine dilates arteries and increases blood flow. It has very little effect on the central nervous system. In large quantities, Papaverine can cause a sedative effect.

Indications for use

• Papaverine is used to relieve spasms in diseases of the pancreas;
• It is also used for spasms of the bladder, including renal colic;
• With spasms of blood vessels;
• With spasms of smooth muscles of organs that are in the abdominal cavity (,).

Method of application and dosage

The introduction of papaverine is carried out intramuscularly, intravenously, subcutaneously. For adults and children who are already 14 years old, the drug is prescribed in the following dosage: from 0.5 to 2 ml of solution. At a time, you can enter no more than 100 mg (5 ml of solution). The maximum dose per day is 300 mg (15 ml of Papaverine).

The drug is most effective when administered intravenously. Previously, 1 ml of 20% Papaverine is dissolved in 10 or 20 ml of Sodium chloride 0.9%. Papaverine must be administered very slowly (up to 5 minutes). The maximum dose that is used at a time for intravenous administration is 20 mg (1 ml of solution). No more than 120 mg (6 ml of solution) can be administered intravenously per day.

For children whose age is from 1 to 14 years, the drug is used at the rate of 0.7 - 1 mg / kg of body weight at a time. 2-3 doses are possible per day. Maximum daily dose for children:

• Up to 3 years 20 mg solution;
• From 3 to 4 years 30 mg;
• From 5 to 6 years 40 mg;
• From 7 to 9 years 60 mg;
• From 10 to 14 years 100 mg.

Also, children are prescribed Papaverine in tablets, in a dosage corresponding to the solution. The tablet can be crushed and mixed with a teaspoon of boiled, chilled water.

The doctor prescribes the duration of use individually, depending on the disease and the severity of the symptoms.

Side effects

When using Papaverine, the following side effects may occur:

• From the nervous system: drowsiness, dizziness, sweating, impaired consciousness, headache, weakness;
• From the digestive system: increased activity of hepatic transaminases, anorexia;
• From the side of the heart and blood vessels: tachycardia, arrhythmia, low blood pressure, collapse, apnea;
• From the immune system: hypersensitivity reactions, itching, rash, urticaria, hyperemia of the skin of the upper body;
• Other reactions: swelling may occur at the injection site.

Contraindications

The drug is not prescribed in the following cases:

• Glaucoma;
• Liver failure;
• Children's age up to 6 months;
• Violation of atrioventricular conduction;
• Hypersensitivity to components.

Interaction with other drugs

The antispasmodic effect of Papaverine is enhanced by its simultaneous use with brabiturates.

If the drug is used simultaneously with procainamide, reserpine, tricyclic antidepressants, the antihypertensive (lowering pressure) effect of the drug is enhanced.

special instructions

A drug such as Papaverine or Papaverine belongs to myotropic antispasmodics and vasodilators. The drug Papaverine is often used for problems with the functioning of the gastrointestinal tract, namely, it is used for severe pain in the abdomen, which is accompanied by cramps and, most importantly, with nausea and vomiting.

Candles papaverine - what are they used for, what is the effectiveness?

Papaverine for nausea and vomiting is used in three forms: the first of which is papaverine ampoules, the second papaverine tablets and the third, papaverine rectal suppositories. The latter, that is, papaverine suppositories, are very effective, because. very quickly, the drug papaverine enters the bloodstream and begins its therapeutic effect. For all three forms of using the papaverine preparation, the same contraindications for use are provided. Also, the drug papaverine is used in gynecology, namely in cases where assistance is needed in obstetric practice. Papaverine is used in this case for women with increased uterine tone during pregnancy.

Papaverine injections - what are they used for, what is the effectiveness?

The drug papaverine in the form of injections is designed to relieve spasm of smooth muscle fibers. Most often, papaverine injections are used for the following health problems: cholecystitis, endarteritis, papaverine injections are also given for pylorospasm and severe pain in the kidney area, with the appearance of renal colic. Papaverine injections should be carried out under the supervision of a doctor, because. When a health problem occurs, the drug is administered slowly, while the doctor must monitor the patient's blood pressure.

Papaverine tablets - dosage, how to use, instructions

Papaverine in the form of a tablet contains the following components: 30 mg papaverine hydrochloride, potato starch and calcium stearate. As for bendazole, which is also part of the drug, its medicinal effect is characterized by the appearance of an effect on the smooth muscles of blood vessels, and also affects the smooth muscle fibers in the abdominal cavity. Also, the function of papaverine includes such a function as stimulation of the spinal cord. The action of the drug with prolonged use is aimed at an immunomodulatory effect. Under the immunomodulatory effect is meant an increase in the production of interferon, a gradual activation of the process of production of phagocytes by the body.

What does papaverine do, how does it work?

The substance papaverine is designed to quickly reduce the calcium content in muscle cells, which means that the spasm will gradually go away. Also, the substance papaverine contributes to the process of reducing vascular resistance, which in turn acts as a decrease in blood pressure in the body. In the event that a doctor diagnoses angina pectoris in a patient, then the use of a drug such as papaverine is usually used together with other drugs. Here, a preliminary consultation with a doctor is simply necessary before you start using papaverine for treatment.

When is papaverine used in treatment?

The use of papaverine is usually used to eliminate abdominal pain that is caused by cramps. In turn, cramps can be formed due to both severe pain in the abdomen and due to frequent vomiting, due to severe nausea, which leads to vomiting. Papaverine effectively copes with the elimination of spasms in smooth muscles, which means it eliminates and relieves pain in the abdomen. Do not know how to reduce pain in the abdomen, in the lower abdomen, do not know how to reduce pain, consult a doctor who can prescribe an effective drug to relieve abdominal pain, including papaverine. Papaverine medicine has a very wide range of applications, so when using it in anesthesiology, it acts as a premedication agent. The most common cases when papaverine is used are with increased uterine tone during a woman's pregnancy, with intestinal diseases (functional), as a way to relieve spasm of the muscles of the gastrointestinal tract. Also, the drug papaverine is used if it is necessary to relieve inflammation of the gallbladder, which usually occurs with a disease such as cholecystitis. Papaverine is used to relieve spasm of the kidneys, to relieve spasms of the bronchi, to relieve spasms of smooth muscle fibers of the coronary, peripheral and cerebral vessels. Papaverine is also used if the patient has an exacerbation of gallstone disease.

Papaverine instructions for use

Each form of papaverine has its own specific instructions for the use of the drug. So, if we consider the use of papaverine in tablets, then it is usually used in a dosage of 40-60 mg. The daily dose of papaverine is 2 or 3 tablets. If the drug papaverine is administered into the body by injection, that is, when papaverine is administered intravenously or intramuscularly, then the bioavailability of papaverine is usually several times greater. And this means that the dose, dosage of papaverine for intramuscular or intravenous use is usually reduced to 10-20 mg. If papaverine is prescribed to people who are in old age, then the dose of papaverine is still reduced and usually does not exceed 10 mg. If you use papaverine suppositories, then the dose of the drug is from 20 to 40 mg. Papaverine suppositories are usually not used more than 2 times a day.

Who is contraindicated for papaverine? When should papaverine not be used?

The instructions for use of papaverine indicate that it cannot be used to treat children under the age of 12 years. Also contraindications for the use of papaverine include the following diseases and health problems: papaverine cannot be used for bronchial obstruction syndrome, papaverine is not allowed to be used for traumatic brain injury, with the appearance of a disease such as convulsive readiness or convulsive syndrome, with other neuralgic disorders. Papaverine is also contraindicated in the event of such a problem as the development of a hypertrophic process in the prostate region. Contraindications to taking papaverine include problems such as liver failure, low blood pressure, or hypotonic bleeding.

Side effects when taking papaverine

Side effects that may occur if papaverine is taken incorrectly or for other reasons include: an allergic reaction on the skin in the form of a rash, such an allergic reaction can be compared with urticaria by the nature of its skin lesion. When using papaverine, increased sweating, increased sweating, and pain in the head may occur. So, in addition to a headache when taking papaverine, the following side effects may appear: nausea and vomiting, the appearance of abdominal pain. Some people have side effects from the use of papaverine, this is the appearance of low blood pressure, arrhythmia and other disorders that are associated with the work of the cardiovascular system of organs. Taking high doses of papaverine can be very dangerous, because. such a problem can lead to excitability of the heart muscle. It should also be noted that the use of medium therapeutic doses of papaverine should not lead to any side effects from papaverine.

If we talk about the interaction of papaverine according to the type of stimulation, according to the type of process of reducing the effect, then doctors usually use papaverine with tranquilizers, antispasmodics and antidepressants.

When else should papaverine be used?

It is highly not recommended to use expired papaverine. Regarding the dosage in each case, it is necessary to consult with the attending physician specialist, because. for each person, the dosage of papaverine can be individual. Particular attention is given to the use of the drug papaverine by those people who have ever had a brain injury. It is also dangerous to use papaverine for people with acute renal failure, supraventricular tachycardia, prostatic hyperplasia and chronic renal failure, adrenal insufficiency. It is also not always possible to use papaverine if a person has a severe state of shock.

The drug papaverine during pregnancy - what is it used for, how to use it?

Women often ask about what papaverine is used for during pregnancy. The most common reason for the use of papaverine during pregnancy is uterine hypertonicity. Why is papaverine used during pregnancy to reduce uterine hypertonicity? Because the hypertonicity of the uterus is a certain threat of miscarriage by a woman. Papaverine during pregnancy can reduce such a threat by reducing unpleasant disorders, improving well-being, which is achieved by reducing uterine hypertonicity.

In some cases, papaverine during pregnancy can also be used during childbirth. In this case, papaverine is used to relieve spasms, but during this period of pregnancy, not ordinary papaverine is used, but papaverine with drotaverine, that is, papaverine with noshpa.

Dibazol with papaverine

Such a combination of a drug, like dibazol with papaverine, is one of the most common in medical practice. One of the main purposes of such a drug as dibazol with papaverine is the use of such a solution as a way to stop a hypertensive crisis, so dibazol with papaverine is used in emergency care. What else is dibazol with papaverine used for? In order to reduce pressure, which, in terms of its indicators, approaches a mark dangerous for life and health. Also, the therapeutic effect of dibazol with papaverine is aimed not only at reducing nausea, feelings of nausea, but also helps to get rid of pain. After a certain time after using dibazol with papaverine in the form of an injection, a gradual decrease in pressure occurs until it returns to normal. For many years of using dibazol with papaverine, this drug has proven itself well as one of the effective ways to deal with a hypertensive crisis.

papaverine hydrochloride- this is one of the few drugs that gynecologists have been trusting for the health of future mothers and their babies for several decades. It is included in the standard of care for some common pathological conditions in pregnant women.

The action of papaverine in the body

Papaverine hydrochloride belongs to the group of drugs with antispasmodic action. Due to the effect on the rate of penetration of calcium ions through the cell membrane of smooth muscle myocytes, it leads to their relaxation. As a result, the universal effect of papaverine can be observed in all organs without exception, where there are smooth muscle elements. In addition, calcium affects the rate of passage of an electrical impulse through the conduction system of the heart.

The main clinical effects of papaverine in the body:

1. Relaxes the smooth muscles of the blood vessels. Due to this, blood delivery through them to the organs improves, both systolic and diastolic blood pressure decreases. The drug acts on blood vessels that are both in normal tone and in increased tone.
2. Relieves spasm of smooth muscles of the excretory ducts (bile, renal, ureters), intestines and pyloric stomach with pylorospasm, intestinal colic or spastic colitis.
3. Relaxes the muscles of the bronchi.
4. Reduces the rate of conduction of the heart impulse through the conduction system of the myocardium and reduces the heart rate. In high doses, it increases the excitability of ectopic rhythmogenic foci in the heart, causing tachycardia and increasing the risk of extrasystole.
5. Causes general mild inhibition and drowsiness.

When is papaverine indicated during pregnancy

Papaverine hydrochloride is the drug of choice for the treatment of increased uterine tone. Moreover, it is effective at any stage of pregnancy. The useful quality of the drug, for which gynecologists love it, is its ability not only to relax the muscles of the uterus, but also to increase the delivery of nutrients and oxygen to it. Therefore, the main indication for the appointment of papaverine is uterine hypertonicity.

The antihypertensive effect of the drug is also not forgotten.: papaverine is included in the treatment regimen for arterial hypertension and even all degrees of severity.

In addition, it is prescribed as one of the first, if necessary, to treat such extragenital pathologies as urolithiasis and complicating it with renal colic, cholelithiasis and hepatic colic, exacerbation of chronic cholecystitis, intestinal colic, endarteritis, vegetative-vascular dystonia, angina pectoris, obstructive or asthmatic bronchitis . It is also used as a component of a lytic mixture for high temperature, pain syndrome and for premedication.

How is papaverine used during pregnancy

An important advantage of the drug is the variety of its forms of release: solution 2% for injection(intramuscular, subcutaneous, intravenous) tablets and rectal suppositories. There are also combined tablet preparations, in which papaverine hydrochloride is included as one of the active ingredients.

During pregnancy, the drug is prescribed mainly in the form of suppositories. Depending on the condition of the woman, it is injected into the rectum one at a time from 2 to 4 times a day at approximately equal intervals. Tablets are taken in the same way. They need to be washed down with a small amount of water. The course of treatment is selected by the doctor individually and can range from several days to several weeks.

Since papaverine is well tolerated in most cases, it is used both in a hospital and independently administered at home. But due to the risk of lowering blood pressure, intramuscular and, moreover, intravenous slow or drip injections are recommended to be done under the supervision of a doctor (that is, in a hospital or clinic).

Contraindications and side effects of papaverine

Side effects of papaverine hydrochloride associated with the mechanism of its action, individual hypersensitivity to it or improper dose selection. Due to the pronounced expansion of blood vessels, there may be:

• decrease to undesirable limits of arterial pressure;
• headache;
• double vision;
• drowsiness;
• tachycardia;
• redness of the skin.

Relaxation of the intestinal muscles in some cases provokes atonic constipation. In addition, a blood test reveals eosinophilia, an increase in liver transaminases. An allergic reaction, impaired conduction and excitability of the heart in the form of AV blockade or ventricular extrasystole are possible.

Contraindications to the appointment of papaverine are:

• glaucoma;
• AV blockade and cardiac arrhythmias, manifested by tachycardia;
• a previous allergic reaction to this drug;
• severe liver or kidney failure.

In addition, the introduction of the drug is prohibited at low blood pressure due to hypothyroidism, shock of any origin, adrenal insufficiency. Due to the unpredictability of the response to vasodilation, papaverine is not indicated in the acute period after a traumatic brain injury and an episode of severe circulatory disorders in the brain.

Special large-scale studies to study the effect of papaverine on the body of a pregnant woman and fetus have not been conducted. Its safety is confirmed only by the lack of information on cases of a proven connection of the drug with the occurrence of any serious pathology over the entire long-term period of drug use. But nevertheless, only the gynecologist or therapist who is observing her should prescribe the treatment of the expectant mother.

Papaverine during pregnancy: reviews

• Irina. During my first pregnancy from 5 to 24 weeks, I often had pulling pains in my abdomen. Papaverine was a real lifesaver for me: I injected a candle, and literally after 15 minutes there was no trace of pain left. If I took the drug in the evening, I fell asleep much faster and slept peacefully. I didn't even have to go to the hospital.
• Natalia. Even before pregnancy, I had a severe headache when the weather changed. When I realized that I was expecting a baby, I forbade myself to even think about migraine medications. She saved herself with papaverine tablets and suppositories. Let not so quickly, but he helped, and I was calm about the health of the baby.
• Alexandra. I was prescribed papaverine in injections to treat the threat of miscarriage, when I had to go to the hospital at 7 weeks. The injections are a little painful, but only twice a day, so it was possible to be patient. After 5 days, the doctor allowed me to replace the injections with candles. After being discharged at home, on the advice of a gynecologist, she herself introduced suppositories as soon as discomfort appeared in the uterus. It's better to be safe than to end up in the hospital again. The child was born full-term and healthy.

Papaverine (lat. Papaverinum) is a drug from the group of myotropic antispasmodics. Currently, it is used only in the form of hydrochloric acid salt (papaverine hydrochloride).

Reduces the tone and contractile activity of the smooth muscles of blood vessels and internal organs.

It is prescribed for spastic conditions of the gastrointestinal tract, urinary tract, bronchi, disorders of cerebral and peripheral circulation.

Due to the long experience of use, it is one of the most studied drugs. Produced by various pharmaceutical manufacturers.

Papaverine was discovered by chemist student Heinrich Merck in 1848. The German isolated a new substance from opium, the milky juice of the sleeping poppy (lat. Papaver Somniferum).

According to the chemical structure, the agent was assigned to the class of alkaloids.
In 1910, A. Pictet was the first to synthesize papaverine artificially from verataldehyde and hypuric acid. Around the same time, the alkaloid showed antispasmodic and vasodilating properties.

In 1913, the German physician J. Pahl introduced the drug into clinical practice, starting to use it in patients with angina pectoris and bronchial asthma. Later, papaverine was used for spasms of the intestines, ureters and as an antihypertensive agent.

In 1930, the Hungarian corporation Chinon was the first in the world to start producing a drug on an industrial scale. By the middle of the XX century. the total number of manufacturers of papaverine has grown to several dozen.
In the 50s. the drug has a competitor - drotaverine ("No-Shpa"). In terms of antispasmodic properties, it turned out to be several times more active than its predecessor, therefore it has found wider application. However, in many countries, papaverine is still a fairly popular medicine, both due to established traditions and due to its low cost.

Properties

International non-proprietary name: papaverine (English papaverine).
IUPAC chemical name: 1-(3,4-dimethoxybenzyl)-6,7-dimethoxyisoquinoline hydrochloride.
Gross formula: C20H21NO4 *HCl
Molar mass: 375,85.

Papaverine hydrochloride is a white crystalline powder with a slightly bitter taste, odorless. Melting point - 225ºС. It dissolves well in water, poorly - in ethyl alcohol, chloroform, diethyl ether. The drug is isolated from opium or obtained synthetically.

Research results

The first studies devoted to the study of the pharmacological activity of papaverine were carried out by J. Pal in the 1910s. The scientist found that the agent has a toxic effect on lower organisms (amoebae, trypanosomes), comparable to morphine.

In higher animals, papaverine, on the contrary, exhibits much lower toxicity than morphine. So, for example, in rabbits, mild symptoms of poisoning occur only with subcutaneous administration of the drug at a dose of 0.25-0.30 mg per 1 kg of body weight.

In the treatment of patients with angina pectoris, Pal noted that papaverine has practically no narcotic properties. In rare cases, the drug caused drowsiness, and usually on the second day after application. Overdose phenomena occurred only after oral administration of an alkaloid in an amount of more than 400 mg.

In placebo-controlled clinical trials conducted in the second half of the 20th century, papaverine showed good efficacy in the treatment of three groups of diseases:

• renal colic,
• gastrointestinal spasms,
• pathologies of the biliary tract.

According to tests, pronounced antispasmodic properties of the drug were noted on average by about 60% of patients. 23% described its effect as moderate or weak. In 17%, no improvement was observed.

In separate clinical trials, the rationality of using papaverine in patients with peptic ulcer of the digestive tract was studied. It was found that taking the drug at a dose of 80 mg 3 times a day leads to a noticeable weakening of the pain syndrome in 78% of patients.

Double-blind, placebo-controlled trials in the 1990s confirmed the effectiveness of papaverine in intestinal disorders.

One Russian study involved 62 patients with irritable bowel syndrome. Volunteers of the experimental group took the drug 80 mg 3 times a day for 2 months.

The control group received a placebo. At the end of therapy, all subjects from the first population noted a decrease in the strength and frequency of pain. Whereas in the control group, patients complained of increased pain.

According to the results of the entire volume of clinical studies, papaverine showed the greatest antispasmodic activity in the treatment of renal colic, gastrointestinal pain, cholelithiasis, dysmenorrhea. The least effective use of the drug was in patients with cerebrovascular disorders.

In all trials, the drug was well tolerated. Side effects occurred in no more than 0.5-3% of patients.

Application in different countries

Papaverine is approved for use in more than 50 countries, including Russia, Germany, France, Great Britain, the USA and Japan. Various factories produce the drug under the trade names "Papaverine", "Papaverine hydrochloride" or under their own brand names (for example, Paparin is produced in Taiwan, Atroveran in Venezuela, Mezotin in Argentina).

• to eliminate spasms of the digestive tract, biliary and urinary tract,
• in the complex therapy of disorders of cerebral and coronary circulation.

In the US and Canada, papaverine was also approved in 1986 as a treatment for erectile dysfunction in men*. However, after the invention of phosphodiesterase-5 inhibitors (Viagra, Cialis, etc.), the drug is practically not used for this purpose.

In Russia, papaverine is included in the List of vital and essential medicines, approved by Decree of the Government of the Russian Federation No. 2135-r dated December 30, 2009.

* In case of erectile dysfunction, papaverine solution is administered intracavernously (into the cavernous body of the penis). The positive effect is associated with the relaxation of the trabeculae of the cavernous bodies and increased blood flow.

Composition and forms of release

In Russia, the drug is available in the form:

• 2% (20 mg / ml) injection solution in 2 ml ampoules,
• suppositories containing papaverine hydrochloride 20 mg,
• tablets containing papaverine hydrochloride 40 mg (for adults) and 10 mg (for children).

In some European countries (Switzerland, Great Britain), you can also find powders with papaverine, packaged in 150 mg sachets, and 3% injection solutions in pharmacies.

Mechanism of action

Papaverine acts directly on the smooth muscles of the internal organs and blood vessels, causing it to relax. Vasodilation leads to an improvement in blood flow, including cerebral, and a decrease in blood pressure.

According to modern concepts, the antispasmodic effects of the drug are due to the blockade of the phosphodiesterase enzyme in the muscles, due to which cyclic 3,5-adenosine monophosphate (cAMP) begins to accumulate in the cells. This leads to the release of calcium ions from the cells and a decrease in the contractile activity of the muscles.

The relaxing properties of papaverine in relation to different organs are expressed differently. The large intestine undergoes the greatest relaxation, then, in order of decreasing effect:

• 12 duodenal ulcer,
• stomach, uterus,
• biliary and urinary tract, sphincter of Oddi,
• bronchi,
• vessels.

In high doses, papaverine reduces myocardial excitability and slows down intracardiac conduction.

The drug has practically no effect on the central nervous system. The sedative effect is manifested only when papaverine is used in doses above the average therapeutic ones.

The effectiveness of the drug is reduced against the background of smoking.

Metabolism and excretion

When administered orally and rectally, papaverine is rapidly absorbed from the digestive tract. On average, up to 54% of the dose taken enters the bloodstream. In plasma, the drug is 90% protein bound.

The agent is well distributed throughout the body. Passes through the blood-brain barrier. Biotransformed in the liver to inactive metabolites, which are excreted by renal filtration. The half-life is 0.5-2 hours (with kidney pathologies, this time can increase up to 24 hours).

Indications for use

The grounds for the appointment of papaverine are:

• spastic conditions of the abdominal organs (spastic colitis, cholecystitis, pylorospasm),
• renal colic,
• bronchospasm,
• spasm of peripheral (endarteritis) or cerebral vessels.

As an aid, papaverine is used to prepare patients for surgery.

Previously, the drug was widely used to prevent angina attacks, but today more modern antianginal drugs are recommended for this purpose.

Contraindications

Papaverine is contraindicated in the following conditions:

• disorders of atrioventricular conduction,
• coma,
• respiratory depression,
• glaucoma,
• age up to 6 months. (for injection forms - up to 1 year),
• bronchial obstruction,
• severe liver dysfunction,
• inflammatory processes of the rectum (the restriction applies only to suppositories).

Due to the high risk of developing hyperthermia, it is not recommended to use the drug in the elderly.

Pregnancy and lactation

In Russia and Europe, special studies that would prove the safety of papaverine during pregnancy or lactation have not been conducted.

Influence on the ability to drive vehicles and complex mechanisms

After parenteral (especially intravenous) administration of the drug, driving and engaging in hazardous activities should be avoided for 1 hour.

Dosage and administration

Papaverine is administered orally, rectally, subcutaneously, intramuscularly and intravenously.

Pills .

• children from 6 months. up to 2 years, 5 mg per reception is prescribed,
• from 3 to 4 years - 5-10 mg,
• from 5 to 6 years - 10 mg,
• from 7 to 9 years - 10-15 mg,
• from 10 to 14 years - 15-20 mg.

Reception schedule: 1 dose 3-4 times a day.

Maximum allowable daily doses:

• for adults - 600 mg,
• for children from 6 months. up to a year - 10 mg, from 3 to 4 years - 20 mg, from 5 to 6 years - 40 mg, from 7 to 9 years - 60 mg, from 10 to 14 years - 200 mg.

suppositories.

Adults: enter 1-2 soup. 2-3 times a day after spontaneous bowel movements or enemas.

Injections .

Subcutaneously and intramuscularly, adults are injected with 1-2 ml of an ampoule solution (in terms of the active substance - 20-40 mg of papaverine hydrochloride).

Intravenously, adults are injected with 1 ml of the drug (or 20 mg of papaverine hydrochloride), which is first diluted with 10-20 ml of saline. The introduction is carried out slowly and under the supervision of a physician.

For elderly patients, the initial dose should not exceed 10 mg.

For children aged 1 to 12 years, the amount of the drug is calculated based on body weight: 0.3 mg of papaverine per 1 kg of weight.

The maximum daily dose for adults with parenteral use should not exceed 300 mg.

Side effects

During therapy with papaverine, the following are possible:

• lowering blood pressure,
• dizziness,
• headache,
• weakness,
• drowsiness,
• atrioventricular block or ventricular extrasystole (risks increase with rapid intravenous administration of the drug),
• dyspeptic disorders (constipation, nausea),
• increased sweating,
• allergic reactions,
• eosinophilia,
• increased levels of hepatic transaminases.

When using suppositories, local negative reactions can be observed: a burning sensation or itching in the anus.

special instructions

At the time of treatment, you must stop drinking alcohol.

Papaverine should be used with caution in the elderly, in patients with hyperthyroidism, renal or hepatic insufficiency, prostate adenoma, supraventricular tachycardia, severe heart disease, shock and traumatic brain injury.

Overdose

Papaverine poisoning manifests itself:

• general malaise,
• diplopia (double vision),
• increased sweating,
• headache,
• arrhythmia.

The condition is treated with gastric lavage and the intake of enterosorbents. If necessary, carry out symptomatic therapy (adjust blood pressure).

Interaction with other drugs

The drug inhibits the effects of levodopa and dopegyt.

The combination with barbiturates leads to a weakening of the antispasmodic properties of papaverine.

The action of the alkaloid can be enhanced by:

• drugs,
• tranquilizers,
• analgesics,
• sedatives.

The hypotensive effect of the drug is potentiated by various antihypertensive agents, tricyclic antidepressants, reserpine, quinidine, procainamide.

The activity of papaverine inhibits nicotine.

Holiday conditions

Injections are dispensed by prescription. Tablets and suppositories - without a prescription.

Storage

In a dry place protected from light. Away from children. Tablets are stored at a temperature of 8 to 25ºС, injection solution - at a temperature of 17-25ºС, suppositories - at a temperature of 8-15ºС.

In pharmacies and medical institutions, ampoules are stored according to the conditions of list B.

Best before date

Pills. 4 years.

Injection. 2 years.

Suppositories. 2-3 years (depending on the manufacturer).

Manufacturers Overview

Funds based on papaverine are produced by a number of Russian and foreign enterprises. Each company uses its own production technologies, so even identical dosage forms manufactured at different factories may differ from each other in the amount of impurities, composition of auxiliary components and physicochemical characteristics. These differences may account for small differences in the clinical performance of the products.

In Russia, papaverine preparations of the following companies are registered and approved for sale:

• OJSC Pharmstandard (Russia),
• OJSC Veropharm (Russia),
• OJSC Irbit Chemical-Pharmaceutical Plant (Russia),
• OJSC Biokhimik (Russia),
• Republican Unitary Enterprise Borisov Plant of Medicinal Products (Republic of Belarus),
• OJSC Novosibkhimfarm (Russia),
• OJSC Biosintez (Russia),
• OAO Nizhpharm (Russia),
• OAO PFK Renewal (Russia),
• NPO FSUE Microgen (Russia),
• JSC Dalhimfarm (Russia),
• JSC Moskhimfarmpreparaty im. Semashko (Russia),
• FSUE Armavir biofactory (Russia),
• CJSC Medisorb (Russia).

The main production is concentrated in the Central, Siberian and Volga regions. Russian drugs enter the market under the trade names Papaverine and Papaverine Hydrochloride.

Some foreign manufacturers of papaverine:

Analogues

Other synthetic drugs and alkaloids have an antispasmodic effect similar to papaverine:

• drotaverine,
• mebeverine,
• dibazol,
• hyoscine butyl bromide,
• benziklan,
• theophylline.

Drotaverine and mebeverine are closest to papaverine in terms of chemical structure and mechanism of action. They also change the calcium content inside the muscle cells in the same way, which leads to relaxation of the internal organs. However, in comparison with their predecessor, drotaverine and mebeverine exhibit stronger pharmacological activity. In addition, the drugs differ in the range of side effects and contraindications.

Comparative characteristics of papaverine, drotaverine and mebeverine preparations:

Gross formula

Pharmacological group of the substance Papaverine

Nosological classification (ICD-10)

CAS code

Characteristics of the substance Papaverine

Papaverine hydrochloride is a white, odorless, crystalline powder with a slightly bitter taste. Slowly soluble in water (1:40), slightly soluble in ethanol, soluble in chloroform, practically insoluble in ether. Molecular weight 375.85.

Pharmacology

It inhibits phosphodiesterase and causes the accumulation of cyclic 3",5"-AMP in the cell and a decrease in the level of Ca 2+ . Reduces the tone and relaxes the smooth muscles of the internal organs (gastrointestinal tract, respiratory, genitourinary system) and blood vessels. In large doses, it reduces the excitability of the heart muscle and slows down intracardiac conduction.

Rapidly and completely absorbed by any route of administration. In plasma, it binds to proteins. Easily passes through histohematic barriers, undergoes biotransformation in the liver. T 1 / 2 - 0.5-2 hours. Excreted by the kidneys mainly in the form of metabolites.

Application of the substance Papaverine

Spasm of smooth muscles: abdominal organs (cholecystitis, pylorospasm, spastic colitis, renal colic), peripheral vessels (endarteritis), cerebral vessels, heart - angina pectoris (as part of complex therapy), bronchospasm; as an auxiliary drug for premedication.

Contraindications

Hypersensitivity, AV blockade, glaucoma, severe liver failure, old age (risk of hyperthermia), children's age (up to 6 months).

Application restrictions

Condition after TBI, shock conditions, chronic renal failure, adrenal insufficiency, hypothyroidism, prostatic hyperplasia, supraventricular tachycardia.

Use during pregnancy and lactation

The safety of use during pregnancy and during breastfeeding has not been established.

Side effects of papaverine

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): AV blockade, ventricular extrasystole, lowering blood pressure.

From the digestive tract: constipation, increased activity of hepatic transaminases.

Others: drowsiness, eosinophilia, allergic reactions.

Interaction

In combination with barbiturates, the antispasmodic effect of papaverine is enhanced. When combined with tricyclic antidepressants, procainamide, reserpine, quinidine, it is possible to increase the hypotensive effect of papaverine.

Overdose

Symptoms: blurred vision (double vision), weakness, drowsiness, decreased blood pressure.

Treatment: gastric lavage (milk, activated charcoal), maintenance of blood pressure.

Routes of administration

Inside, s / c, / m, rectally.

Papaverine Substance Precautions

It should be borne in mind that the effectiveness decreases with smoking.

Interactions with other active substances

Trade names