Papaverine

Papaverine is an opiate-type alkaloid. The medicine affects smooth muscles, helping to relax it. Due to these properties, the drug is included in the category of antispasmodic myotropic type.

[1], [2], [3], [4], [5], [6]

Indications of the papaverina

It is used to eliminate such disorders:

• smooth-muscle spasms in the peritoneum (often develop with colitis of a spastic character, pilorospasm or cholecystitis);
• hypertensive crisis (for complex conservative treatment);
• endarteritis;
• colic in the kidney area;
• spasms in the peripheral vasculature;
• narrowing of the lumen of the cerebrospinal vessels due to the reduction of arterial muscles;
• spasms of bronchi and angina pectoris;
• reduction of the arterial inflow through the kidneys, which is of vascular origin;
• delayed urination caused by spasm in the urinary tract.

In addition, papaverine is prescribed at the premedication stage before performing surgical operations in the abdominal area, and in addition, with urological and proctologic procedures, in order to relax the smooth musculature.

[7]

Release form

The release occurs in tablets, injection solution, as well as rectal suppositories.

Tablets have a volume of 0.01 or 0.04 g (application is determined by the age category of patients - for example, the first appoint babies from six months). They are contained in an amount of 10 pieces inside the blister pack.

Injection treatment solution (2%) - in ampoules with a volume of 2 ml. The pack usually contains 10 such ampoules.

Suppositories for rectal administration have a volume of 0.02 g. Inside the blister contains 10 suppositories. Inside the box there is 1 blister plate.

[8], [9]

Pharmacodynamics

The mechanism of the medicinal effect of the active component is due to the effect on the secondary mediators that transmit the excitation of the muscles. The drug slows the element of PDE, which contributes to cumulation of cAMP inside cells and reduces the amount of calcium ions. As a result of these biochemical changes, the tone of the smooth muscles of the internal organs (vascular bed, urogenital and respiratory system, as well as the digestive tube) decreases and it relaxes.

[10], [11], [12], [13], [14], [15], [16], [17], [18], [19]

Pharmacokinetics

The active element is rapidly and almost completely absorbed in any method of administration.

Once inside the circulatory system, the substance is synthesized with a plasma protein (90%), which allows it to penetrate through the histohematological barriers. The process of biotransformation occurs in the liver.

The half-life lasts within 30-120 minutes (the more accurate figure is determined by the type of the auxiliary elements of the drug). Excretion mostly occurs through the kidneys - under the guise of decay products.

[20], [21], [22], [23], [24],

Dosing and administration

Use of drugs in tablets.

Tablets can be given to both children and adults, with the same frequency of use - 3-4 times / day. The sizes of portions of the drug for oral administration are determined by the age of the patient and are assigned according to the following scheme:

• infants from six months to 2 years - 0,005 g per 1 use;
• children within the age of 3-4 years - intake of 0,005-0,01 g;
• children in the age group of 5-6 years - use 0.01 g;
• children in the period of 7-9 years of age - application of 0.01-0.015 g;
• children and adolescents aged 10-14 years - use of 0.015-0.02 g;
• for adult patients - application for 0,04-0,08 g.

Scheme of the drug in the form of suppositories.

Papaverine in suppositories helps to weaken manifestations of hemorrhoids. At the beginning of the course of therapy, a dosage of 0.02 g should be used, eventually gradually increasing it to a size of 0.04 g (in the absence of medication from a lower dose). It is forbidden to introduce more than 3 suppositories per day, because exceeding this limit leads to the appearance of negative symptoms and the development of intoxication, due to the fact that the medicinal components inside the rectal region are absorbed faster and fuller.

Scheme of use of a solution for injection.

The active element of the drug solution has high bioavailability, which allows for both intramuscular and subcutaneous injections - both methods provide a powerful and effective effect. But it must be taken into account that the injections of the SC are required to be performed not in the distal region of the forearm, but in the external part of the thigh or shoulder, because the frequency of injection can provoke the development of the hematoma. The injections of the solution in the / m method are performed in a standard way - the buttocks, their upper lateral part, are used for the introduction.

Before performing IV injections, dilute the dosage prescribed by the doctor with 10-20 ml of sodium chloride solution. It must also be taken into account that the solution must be administered at a very slow rate so as not to cause discomfort in the patient.

Subcutaneous method usually injected 2 ml of the drug (1 ampoule).

• Dose sizes (in ampoules) when administered to a patient in / m or IV injection:
• for an adult: a single - 0.1 g, a total daily - 0.3;
• infants 6-12 months: single - 0.005 g, total daily is 0.01 g;
• children 2 years: a single is 0.01 g, and the total daily - 0.02 g;
• age category 3-4 years: one-off portion - 0.015 g, total daily allowance - 0.03 g;
• within 5-6 years of age: a one-time dose of 0.02 g, a total daily dose of 0.04 g;
• group at the age of 7-9 years: size of a single serving - 0.03 g, total daily - 0.06 g;
• children and adolescents within 10-14 years: single dose - 0.06 g, total daily - 0.1-0.2 g.

[32], [33], [34], [35],

Use of the papaverina during pregnancy

Before using Papaverine, you need to determine the appropriate dosage form - to ensure the greatest possible positive effects on the mother and fetus. Determine the most optimal form of drugs for pregnant women should be given the terms of gestation. For example, at an early stage of pregnancy it is recommended to use tablets for ingestion, and on a later one, a solution for sc or injections is considered more appropriate.

At the late gestation period, the drug in the form of a solution is considered to be the most suitable. During this period, uterine hypertension or painful cramping spastic nature can cause water leakage and premature birth.

The size of the dose for injection, as well as the frequency of their administration, are selected for each patient separately. Often it varies within 1-10 ml (2% solution). The injection should be 2-4 times / day. If complications develop during conservative therapy, you should immediately consult a doctor.

Oral tablets are prescribed only if there are indications. The criterion of admission is a subjective sensation of a woman, because of what strict sizes of accepted portions of drugs are not. Doctors do not recommend eating more than 4 papaverine tablets a day. Reception should be performed 120 minutes before eating - in order to enhance the medicinal properties of the active element.

Contraindications

The main contraindications:

• the presence of hypersensitivity to the elements of the medication;
• problems with intracardiac conduction, especially in the case of AV blockade;
• the presence of glaucoma;
• hepatocellular insufficiency in severe degree;
• elderly patients (because this increases the likelihood of fever);
• infants under the age of six months.

The use of drugs can be further limited in such cases (it is recommended to use exclusively under the regular supervision of medical specialists and subject to continuous diagnostic tests):

• a history of recent traumatic brain injury;
• kidney failure in a chronic degree;
• state of shock;
• hypothyroidism;
• supraventricular tachycardia;
• hyperplasia of the prostate benign;
• problems with the functional activity of the adrenal glands.

[25], [26], [27], [28]

Side effects of the papaverina

The use of the drug may lead to the appearance of some side effects:

• lesions in the hemopoietic system and CCC: ventricular tachycardia, AV blockade, and a decrease in blood pressure;
• reactions affecting the function of the digestive tract: constipation, flatulence and nausea, and in addition, a disorder of the passage inside the digestive tube and an increase in the activity of liver transaminases;
• other: the development of eosinophilia, the appearance of allergic symptoms and a feeling of drowsiness.

[29], [30], [31]

Overdose

When poisoning with papaverine may occur following manifestations: a decrease in blood pressure, the development of diplopia, and in addition a feeling of drowsiness, weakness or severe fatigue.

The drug does not have a specific antidote, so standard procedures for symptomatic and detoxification treatment are used to eliminate the disorders. The most effective is gastric lavage and the intake of sorbents (such as activated charcoal or milk) at the initial stage after the development of an overdose due to the taking of tablets.

In addition, with intoxication it is important to regularly monitor blood pressure indicators and artificially support them when such a need arises.

[36], [37], [38], [39],

Interactions with other drugs

The drug platyphylline has vasodilator, sedative and spasmolytic properties, that is, its medicinal effect is similar to that of Papaverin. These drugs differ only in the mechanisms of their pharmacological action, so they can be used in combination with conservative treatment of hypertensive crisis, spastic syndromes, as well as other disease states.

Good interaction with the drug demonstrates and no-shpa. The drugs have a synergistic effect on smooth muscle. Such a drug combination is often used in gynecology and obstetrics with the development of uterine tone, the threat of miscarriage, or extremely active and early-onset labor.

There is information that the properties of levodopa are greatly weakened in the case of combined conservative treatment, therefore it is forbidden to use Papaverine in the form of an injection solution or tablets during the period of drug therapy with a tremor paralysis.

Combined application of the drug with cholinolytic drugs manifests itself in the form of potentiation of the medicinal effect of the latter. Because of this, if you need to combine them, you need to consult your doctor about reducing dosages or temporarily stopping taking drugs.

[40], [41], [42]

Storage conditions

Papaverine is required to be kept in a dark place, protected from moisture, as well as access to children. The medicine should be stored at temperature values not exceeding 25 ° C.

[43], [44], [45], [46]

Special instructions

Reviews

Papaverin has a wide range of medicinal activity, therefore, reviews about it appear on medical forums of very different directions. This remedy is used to treat a variety of different diseases.

For example, a lot of positive responses about the medicine are left by proctologists, as well as people who use the drug for hemorrhoids, which nowadays occurs quite often. Rectal suppositories Papaverin contribute to facilitation of defecation processes and partially relieve pain, and besides this, they relieve hemorrhages arising in the region of enlarged hemorrhoids. All these positive effects are often mentioned in discussions on the forums.

In addition, they often mention the positive effects of suppositories during pregnancy, because their relaxing and spasmolytic effects contribute to the rapid and complete elimination of uterine hypertension, preventing the risk of premature birth. The active element of the drug helps to ease pain resembling labor pains (they are often observed on the last gestation). Along with this, the drug is often used for prophylaxis in obstetric hospitals.

[47]

Shelf life

Papaverine should be used in the period of 2 years from the date of manufacture of the medicament.

[48], [49], [50]