Negative symptoms caused by spasms are well known to everyone – this is a headache, pain in the abdomen, and even such a dangerous condition as arterial hypertension. Especially bad when blood vessels are spasmed. Naturally, physicians have long sought to obtain a drug that effectively protects the human body from spasms. And such a drug actually exists – it is familiar to many papaverine. Of course, the description of the drug can be found in the instructions, but many readers would certainly like to know what Papaverin is from, and what its principle of action is.
- Release form
- Storage Conditions
- Comparative characteristics of papaverine and drotaverine
- Features of suppository use
- Papaverine Use in Pregnancy
- Pediatric Papaverine Use
- Side Effects
- Papaverine, instructions for use
- Papaverin tablets, instructions for use
- Parenteral Drug Administration
- Intramuscular and subcutaneous injections of papaverine hydrochloride, instructions for use
- The combined use of Papaverine with Dibazol
- Instructions for use of papaverine in the form of rectal suppositories
- Interaction with other drugs and substances
The drug is among the oldest drugs used in medicine. Its discovery is due to the efforts of the German chemist Georg Merck in the mid-19th century.
The name “papaverine” comes from the Latin word papaver – “poppy”. And this is not by chance, since for the first time the drug was actually obtained from opium, which is contained in considerable quantities in poppy seeds. According to its structure, the drug is an opium alkaloid derived from isoquinoline. However, unlike other alkaloids, the drug has virtually no effect on the central nervous system. At least as long as it comes to therapeutic doses.
The main course of action of papaverine is antispasmodic. It is caused by complex chemical transformations in the body. First of all, the drug inhibits the synthesis of phosphodiesterase, which, in turn, leads to the accumulation of cyclic adenosine monophosphate in the cell. Ultimately, there is a decrease in the amount of calcium ions in the muscle tissue, which the muscles need for contractile activity. Thus, the drug contributes to the fact that the tone of muscle fibers goes down and the phase of their relaxation begins. But the pathological contraction of muscle fibers is the main cause of spasm.
It is worth paying attention to the fact that the tool is active only in relation to smooth muscles. This is a very important circumstance. After all, smooth muscle is the musculature that manages the contractions of the internal organs (first of all, these are the respiratory organs, the gastrointestinal tract, the urogenital system), as well as the blood vessels. The skeletal muscles, as well as the heart muscle, have a completely different type of structure. These muscles are called striated. And this type of muscle drug does not work. Thus, the drug can be safely used without any risk that it will affect the contractility of the myocardium. Although the drug still has a definite influence on the work of the heart, it is not connected with the effect on the heart muscle. In large doses, the drug reduces the conductivity of nerve signals in the myocardium and reduces the excitability of the heart muscle.
In addition, the effect of Papaverine is only relaxing. It does not cause muscle paralysis, and they can respond to signals from the nervous system. What are dangerous spasms of internal organs? When spasms disrupt their normal functioning. For example, intestinal spasm retards the movement of food masses through it, ureteral spasm leads to urinary retention and overflow of the bladder, spasm of the biliary tract and gall bladder – to delay bile and indigestion. But the most dangerous spasm of blood vessels. When this phenomenon increases pressure, the blood can not normally circulate through the tissues. As a result, their hypoxia occurs. No less dangerous is bronchospasm, in which the body also suffers from a lack of oxygen, which cannot penetrate the lungs.
However, in itself, the malfunction of the internal organs – this is not the only negative consequence of spasm. A common companion of spasm is pain. It occurs due to the squeezing of various tissues, nerves, as well as difficulties in the circulation of various substances in the body. For example, the accumulation of gas in it caused by spasm of the intestines can lead to strong pressure on the intestinal walls and cause unbearable pain in the patient. It should be borne in mind that the use of analgesics in many cases is dangerous, as it hides the pain itself, but does not affect its immediate cause – the spasm. As a result, a person’s condition may worsen, and after the effect of the analgesic passes, the pain will return with a new force.
In addition to antispasmodic, the drug shows a number of other effects:
In principle, most of these effects are derived from the antispasmodic action of Papaverine. The hypotonic action is associated with relaxation of the vascular smooth muscle, due to which the lumen of the vessels expands. And, as a result, the blood flow in the arteries, including those located in the brain, increases. With regard to the analgesic effect, it should be remembered that the pain is often caused by a spasm of certain muscles. Removing this spasm, the drug relieves and pain. However, these effects are secondary. Papaverine is not among the drugs with a pronounced hypotonic effect, which means that it is usually used in combination with antihypertensive drugs in the treatment of hypertension.
The same can be said about the anesthetic properties of Papaverine. Although its advantage in this regard is that it can remove the cause of the pain itself, and not just pain, however, unlike anesthetics, papaverine can help only in case of pain caused by muscle spasm of smooth muscles or blood vessels, and in others In cases of its use will be meaningless. Thus, the analgesic effect of Papaverine cannot be considered universal.
In addition, a certain sedative effect was found associated with the use of Papaverine. However, it also appears mainly in high doses.
The absorption of papaverine varies depending on the dosage form and averages just over 54%. The drug is well distributed in all tissues of the body. The half-life is from half an hour to 2 hours. Metabolized in the liver and excreted through the kidneys. It can be removed from the body through hemodialysis.
The drug can be purchased in pharmacies without a prescription, it is produced by various pharmaceutical companies. The drug from Russian and Belarusian manufacturers is available in Russian pharmacies.
You can find three dosage forms of Papaverine on sale. Each of them has differences in its purpose. This is:
- rectal suppositories.
Papaverine tablets have a bitter taste and are available in two dosages – 10 and 40 mg. The first one is designed to treat children, the second is more suitable for adults.
Excipients included in tablets may vary depending on the manufacturer. These are usually the following:
- stearic acid.
Suppositories, in addition to the active ingredient, contain solid fats and stearins that melt at the temperature of the human body, as well as emulsifiers.
Rectal suppositories (suppositories) have a dosage of 40 mg of active ingredient.
The solution for injection is available in 2 ml ampoules and has an active substance concentration of 2%. This means that 1 ml of solution contains 20 mg of papaverine, and 40 mg in the ampoule. In general, the liquid in the ampoules is a solution of sodium chloride. Methionine and disodium edetate may also be present in the solution.
The price of the drug depends on the form of release. A pack of 10 tablets can be purchased for as little as 20 p. A pack of 10 ampoules costs 50 p.
The drug in tablets and solution should be stored at room temperature (not higher than +25 ° C) and in a dark place. But suppositories should be stored in the refrigerator (at a temperature of + 5-8 ° C), because otherwise they can melt.
The drug is popular, and it is produced by many companies. There are a number of drugs containing as the main component of papaverine. Such drugs are called structural analogues. There are drugs containing papaverine, however, in addition, having in the composition and other active ingredients, such as Papazol, Andipal, Teodibaverin.
There is a number of other drugs based on other substances with antispasmodic action. Among these compounds, drotaverine is a papaverine derivative.
Comparative characteristics of papaverine and drotaverine
In many ways, experts prefer Drotaverinum. This is a more modern substance, which also has antispasmodic activity. Drotaverinum has a spectrum of indications almost similar to papaverine. But the number of side effects of drotaverine is less, more and the effectiveness of the drug. That is why doctors most often prescribed drotaverin as an antispasmodic.
However, papaverine is still still used in clinical practice, and quite widely. The reason for this is a few things. First, it is a more tried and tested drug. It is worth mentioning that it has been used for almost a century and a half – few of which drugs can boast such a long service life. Therefore, it seems to many doctors that it is more familiar and reliable drug that is difficult to refuse. In addition, you can not discount the slightly lower price of papaverine compared with peers.
But there is a slightly more important reason. It is believed that the effect of papaverine is somewhat faster than that of drotaverine. Therefore, it is more suitable for the relief of acute spasms. At the same time, the drug is much less suitable for long-term administration. If there is a need to take a spasmolytic for weeks or months, then in this case it is better to choose Drotaverine.
In the classification of drugs, the drug is usually classified into two categories – vasodilators and antispasmodics.
The drug can be administered with various spasms of the internal organs related to the gastrointestinal tract, urinary and circulatory system. First of all, it is spasms of smooth muscles of internal organs. Similar organs include:
- gall bladder,
- respiratory organs.
Also, the drug can relieve spasms of peripheral vessels, brain vessels and the heart.
Areas of medicine where the drug is used:
Main indications for papaverine use:
- cholecystitis (inflammation of the gallbladder);
- colitis (inflammation of the large intestine);
- cholangitis (inflammation of the bile ducts);
- menstrual pain;
- renal colic;
- biliary tract spasms;
- ureteral spasms leading to urinary retention;
- cerebral vascular spasms;
- stomach and intestinal colic;
- uterine hypertonus.
The drug can be used as the only means to relieve certain symptoms, and be used as one of the components of complex therapy.
Also, often the drug is used as a means for sedation before various surgical procedures and operations on the organs of the gastrointestinal tract, in the field of proctology and urology. The use of papaverine relaxes the muscles of the internal organs and thus facilitates surgical manipulations.
For subarachnoid hemorrhage, the drug is used as a vasodilator for the coronary arteries. Also, the drug can be used with the same purpose when bypassing the coronary arteries.
The drug, like other antispasmodics, can be used as one of the means for the complex therapy of erectile dysfunction.
If there is no improvement after the course of Papaverine use, consult a doctor.
Features of suppository use
Rectal suppositories with papaverine are used to treat hemorrhoids. With hemorrhoids suppositories demonstrate the following effects:
- facilitate the act of defecation,
- relieve pain,
- reduce the intensity of bleeding.
It is also preferable to use suppositories for diseases of the genitourinary system. In such cases, suppositories are more effective than tablets.
Papaverine Use in Pregnancy
Although the instructions indicate that the drug has not been tested for safety during pregnancy, nevertheless, it is often used by gynecologists to treat such a dangerous condition as uterine hypertonus. This condition can occur in a woman during pregnancy and is fraught with premature birth. Especially often the appointment of Papaverine occurs in early pregnancy. In most cases, it is used not as a single drug, but as part of complex therapy, for example, together with hormonal drugs. Often, the combination of Papaverine and Drotaverine is also prescribed. However, such an appointment usually takes place in late pregnancy. Its purpose is to prepare the cervix for labor.
However, the appointment of this kind carries a certain amount of risk, because too high a dose of an antispasmodic can lead to the opposite effect and cause the uterus to relax too much and the woman cannot give birth on her own. Thus, the dosage of papaverine should be selected extremely carefully. But this fact suggests that self-treatment in such cases is completely unacceptable.
Treatment of gynecological pathologies in future mothers is carried out exclusively in the hospital. In this case, the doctor can use as a pill form of papaverine, and injections. In many cases, rectal suppositories with papaverine are also effective. As a rule, they operate with high speed and efficiency. They are usually prescribed in the first trimester of pregnancy.
Pediatric Papaverine Use
About the high security of papaverine says the fact that it is allowed to give children from 6 months. In some cases, a pediatrician may prescribe a drug at a younger age, but this practice is not encouraged by most doctors.
In most cases, Papaverine is prescribed for children to relieve spastic abdominal pain, intestinal colic and bronchospasms, hepatic colic, spasms, urethra, in the treatment of pancreatitis. Another option for the use of papaverine in children is the elimination of peripheral vascular spasm on the background of hyperthermia. At the same time, an antispasmodic is given to the child for 20 minutes. to febrifuge.
The drug has a high degree of safety and it has a relatively small number of contraindications.
In some cases, the drug is not recommended:
- 6 months old
- heart attack,
- advanced age (over 75)
- severe renal failure,
- atrioventricular block 2-3 degrees,
- tendency to low blood pressure,
- Hypersensitivity to the components of the drug,
The drug is used with caution when:
- adrenal insufficiency,
- chronic renal failure,
- prostatic hyperplasia
- supraventricular tachycardia,
- brain injuries.
At the age of over 65 years, the drug is used under strict medical supervision.
Some drugs are incompatible with papaverine, so before you start taking the drug is best to consult a doctor.
The drug is usually well tolerated by patients and the occurrence of adverse reactions is an infrequent phenomenon. As a rule, this occurs with a slight excess of the dosage of the drug. In most cases, side effects are transient and disappear either with papaverine withdrawal or with a lower dosage.
The following types of side effects may occur while taking Papaverine:
- drop in blood pressure;
- ventricular premature beats;
- impaired cardiac conduction (atrioventricular block);
- arrhythmias (ventricular premature beats, tachycardia);
- hyperthermia (most commonly seen in older people);
- decreased vision, diplopia;
- thrombosis at the injection site;
From the side of the gastrointestinal tract can be observed:
- dry mouth,
- abdominal pain,
Allergic reactions when using the drug:
If there are signs of allergy, the drug should be stopped immediately.
Since among the side effects of Papaverine include possible dizziness and pressure drop, for the time of therapy should be abandoned driving and carrying out work requiring attention and concentration.
In clinical practice, overdose of papaverine occurs infrequently. Most often, the drug is taken in large doses by children.
For overdose, the main symptoms are the side effects described above, but in an enhanced version. The most common symptoms include:
- double vision,
- low blood pressure.
Treatment of symptomatic overdose. The patient must be taken to the hospital. It is shown gastric lavage, intake of enterosorbents, the use of pressure-enhancing agents. In severe cases, hemodialysis is possible.
Papaverine, instructions for use
The dosage of papaverine depends on the dosage form, dosage, age of the patient and his illness. Therefore, it is best to ask the doctor about the desired dosage. It should be borne in mind that in some cases, for example, in the treatment of uterine tone in pregnant women, self-treatment is strictly prohibited.
Papaverin tablets, instructions for use
40 mg tablets are taken by adults three times a day on a tablet. The highest single dose – 200 mg daily – 600 mg. Children are given smaller doses:
- 6 months-2 years – 5 mg,
- 2-4 years – 5-10 mg,
- 5-6 years old – 10 mg,
- 7-9 years old – 10-15 mg,
- 10-14 years old – 15-20 mg.
Young children are best to take the drug in the form of tablets, previously dissolved in water.
In most cases, papaverine pills do not depend on food intake. Many patients take pills when cramps and pains make themselves felt. However, with a tendency to gastric and intestinal colic, the papaverine pill is best taken half an hour before meals. A pill is swallowed whole, without chewing. However, chew pills, given the bitter taste of papaverine, very few people come to mind. Tablets need to drink plenty of water.
The duration of treatment with papaverine depends on the type of pathology. In acute manifestations of the disease, the duration of treatment is usually 5 days, in chronic diseases it can be extended to a week.
Parenteral Drug Administration
In the case of parenteral (subcutaneous, intravenous or intramuscular) administration, a dose of 20–40 mg is applied two to three times a day. With intravenous administration, 20 mg (1 ml) of the drug is pre-diluted in 20 ml of isotonic sodium chloride solution (0.9%).
The interval between injections should be at least 4 hours. For elderly patients, the initial single dose should not exceed 10 mg. The same applies to patients with decompensated heart failure, supraventricular tachycardia, endocrine diseases, patients in shock.
The maximum single dose for subcutaneous and intramuscular administration is 100 mg, for intravenous administration the maximum daily dose is 120 mg.
Intramuscular and subcutaneous administration is preferred over intravenous. However, intravenous administration is considered more effective, although the likelihood of side effects with it is higher. Therefore, intravenous administration is justified only in case of severe condition of the patient. Intravenous drug should be administered slowly, controlling the patient’s heart parameters. This applies particularly to patients suffering from sclerotic lesions of the coronary arteries. It is best that intravenous injections be given by qualified medical personnel. In addition, at the earliest opportunity should transfer the patient to the drug in pill form or use rectal suppositories.
For children, a single dosage for parenteral administration is also less than for adults. It is calculated based on the body weight of the child – 0.7 mg per kg of body weight. The number of injections per day – 2.
Maximum daily dose for different age groups:
- 1-2 g – 1 ml (20 mg),
- 3-4 g – 1.5 ml (30 mg),
- 5-6 years old – 2 ml (40 mg),
- 7-9 years – 3 ml (60 mg),
- 10-14 years old – 5 ml (100 mg).
Intramuscular and subcutaneous injections of papaverine hydrochloride, instructions for use
Before you enter the drug intramuscularly, you must first select the injection site. For this purpose, more suitable upper outer surface of the thigh or shoulder. For subcutaneous administration, the navel area is more suitable. The skin at the injection site is wiped with an antiseptic. For intramuscular injections, the needle should be directed perpendicular to the skin surface. With subcutaneous injections, it is necessary to grasp approximately 1 cm of skin with your fingers, making it a fold. The needle should be directed at an angle of 45 ° to the skin, then it must be inserted into this fold. After the introduction of the drug, the skin should again be wiped with antiseptic. The place of each new injection should be at least 1 cm from previous injection sites. If a person has mastered the technique of intramuscular and subcutaneous injections, then he can conduct them at home on their own.
The combined use of Papaverine with Dibazol
This combination has become widespread in clinical practice as a means to combat hypertensive crises. Medicines are administered intravenously or intramuscularly with an increased pressure in a patient using a papaverine solution with a volume of 2 ml and 3-5 ml of 1% solution of Dibazol.
Instructions for use of papaverine in the form of rectal suppositories
Suppositories with papaverine are intended for rectal input. If necessary, the suppository can be cut into pieces.
Recommended doses for different age groups:
- adults – 1-2 suppositories 2-3 times a day,
- children 10-18 years old – 20 mg 2 times a day,
- children 5-10 years old – 10 mg (half a suppository) 2 times a day,
- Children under 5 years old – 5 mg (quarter of a suppository) 2 times a day.
Interaction with other drugs and substances
It is recommended to eliminate the use of ethanol for the duration of treatment with papaverine, since this may lead to an increase in the hypotensive effect and an increased risk of loss of consciousness. When smoking, the effectiveness of the drug is also reduced.
Reduces the effectiveness of Levodopa and Methyldopa. Combined use with barbiturates, Analginom, Diclofenac, Dimedrolum increases the antispasmodic effect. The antihypertensive effect is also enhanced while taking it with some drugs, for example, tricyclic antidepressants, Procainamide, Reserpine, Quinidine.
Combined use with furadonin increases the risk of developing hepatitis. Combined use with anticholinergic drugs increases their effect. The combination with Alprostadil can cause the development of priapism. Cardiac glycosides increase myocardial contractility with simultaneous use with papaverine.
Compatible with Dibazol. In practice, the combination of Dibazol and Papaverine is used to combat hypertensive crises.