Papaverine

Papaverine is an opium-type alkaloid. The drug affects smooth muscles, promoting their relaxation. Due to these properties, the drug is included in the category of myotropic antispasmodics.

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

Indications Papaverine

It is used to eliminate the following disorders:

• smooth muscle spasms in the peritoneum (often develop with spastic colitis, pylorospasm or cholecystitis);
• hypertensive crisis (for complex conservative treatment);
• endarteritis;
• colic in the kidney area;
• spasms in the peripheral vessels;
• narrowing of the lumen of the cerebral vessels due to contraction of the arterial muscles;
• bronchial spasms and angina pectoris;
• reduction of arterial inflow through the kidneys, which has a vascular origin;
• urinary retention 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 also during urological and proctological procedures - in order to relax smooth muscles.

[ 7 ]

Release form

It is available in tablets, injection solution, and rectal suppositories.

The tablets have a volume of 0.01 or 0.04 g (use is determined by the age category of patients - for example, the first are prescribed to infants from six months). They are contained in the amount of 10 pieces inside a blister pack.

Injection medicinal solution (2%) – in 2 ml ampoules. A pack usually contains 10 such ampoules.

Suppositories for rectal use have a volume of 0.02 g. The blister contains 10 suppositories. The box contains 1 blister plate.

[ 8 ], [ 9 ]

Pharmacodynamics

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

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

Pharmacokinetics

The active element is quickly and almost completely absorbed with any method of application of the drug.

Once inside the bloodstream, the substance is synthesized with plasma protein (90%), which allows it to penetrate histohematic barriers. The biotransformation process occurs in the liver.

The half-life is between 30 and 120 minutes (a more precise figure is determined by the type of auxiliary elements of the drug). Excretion occurs largely through the kidneys - in the form of decay products.

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

Dosing and administration

Use of drugs in tablet form.

The tablets can be prescribed to both children and adults, with the same frequency of use - 3-4 times a day. The dose sizes of the medicine for oral use are determined by the patient's age and are prescribed according to the following scheme:

• infants from six months to 2 years old – 0.005 g per 1 dose;
• children aged 3-4 years – take 0.005-0.01 g;
• children in the age category 5-6 years – consume 0.01 g;
• children aged 7-9 years – use 0.01-0.015 g;
• children and adolescents aged 10-14 years – use 0.015-0.02 g;
• for adult patients – use 0.04-0.08 g.

Scheme for using the medicine in the form of suppositories.

Papaverine in suppositories helps to relieve the symptoms of hemorrhoids. At the beginning of the course of therapy, a dosage of 0.02 g should be used, gradually increasing it over time to 0.04 g (in the absence of a medicinal effect from a lower dose). It is forbidden to administer 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 inside the rectal area, medicinal components are absorbed faster and more completely.

Scheme of use of the injection solution.

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

Before performing intravenous injections, it is necessary to dilute the dosage of the drug prescribed by the doctor with 10-20 ml of sodium chloride solution. It is also necessary to take into account that the solution must be administered at a very slow speed so as not to cause discomfort to the patient.

The subcutaneous method usually administers 2 ml of the drug (1 ampoule).

• Dose sizes (in ampoules) when administered to a patient by intramuscular or intravenous injections:
• for an adult: single dose – 0.1 g, total daily dose – 0.3;
• infants 6-12 months: single dose – 0.005 g, total daily dose is 0.01 g;
• for children 2 years old: a single dose is 0.01 g, and the total daily dose is 0.02 g;
• age category 3-4 years: single serving – 0.015 g, total daily serving – 0.03 g;
• within 5-6 years of age: single dose – 0.02 g, total daily dose – 0.04 g;
• group aged 7-9 years: single serving size – 0.03 g, total daily – 0.06 g;
• for children and adolescents aged 10-14 years: single dose – 0.06 g, total daily dose – 0.1-0.2 g.

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

Use Papaverine during pregnancy

Before using Papaverine, it is necessary to determine the appropriate dosage form - to ensure the maximum possible positive effect on the mother and fetus. The most optimal form of the drug for pregnant women should be determined taking into account the gestation period. For example, in the early stages of pregnancy, it is recommended to use tablets for oral administration, and at a later stage, a solution for subcutaneous or intramuscular injections is considered more suitable.

At a later stage of pregnancy, the most suitable medicine is considered to be in the form of a solution. During this period, uterine hypertonicity or pain of a cramping, spasmodic nature can cause the waters to break and premature birth.

The injection dose size and frequency of administration are selected for each patient individually. Often it varies within 1-10 ml (2% solution). The injection should be administered 2-4 times a day. If complications develop during conservative therapy, it is necessary to immediately consult a doctor.

Oral tablets are prescribed only if there are indications. The criterion for taking is the subjective sensations of a woman, which is why there are no strict sizes of the doses of the drug. Doctors do not recommend taking more than 4 Papaverine tablets per day. The intake should be carried out 120 minutes before eating - to enhance the medicinal properties of the active element.

Contraindications

Main contraindications:

• the presence of hypersensitivity to the components of the drug;
• problems with intracardiac conduction, especially AV block;
• presence of glaucoma;
• severe hepatocellular insufficiency;
• elderly patients (because this increases the likelihood of developing fever);
• infants under six months of age.

The use of the drug may be further restricted in the following cases (it is recommended to use it only under regular supervision of medical specialists and subject to constant diagnostic tests):

• history of recent TBI;
• chronic renal failure;
• state of shock;
• hypothyroidism;
• supraventricular tachycardia;
• benign prostatic hyperplasia;
• problems with the functional activity of the adrenal glands.

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

Side effects Papaverine

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

• lesions in the hematopoietic system and cardiovascular system: ventricular tachycardia, AV block, as well as a decrease in blood pressure values;
• reactions affecting the function of the gastrointestinal tract: constipation, flatulence and nausea, as well as disturbance of passage within the digestive tract and increased activity of liver transaminases;
• Others: development of eosinophilia, appearance of allergic symptoms and a feeling of drowsiness.

[ 29 ], [ 30 ], [ 31 ]

Overdose

In case of poisoning with Papaverine, the following symptoms may occur: a decrease in blood pressure, the development of diplopia, and also a feeling of drowsiness, weakness or severe fatigue.

The drug has no specific antidote, so standard symptomatic and detoxification treatment procedures are used to eliminate disorders. The most effective is gastric lavage and intake of sorbents (such as activated carbon or milk) at the initial stage after the development of an overdose due to taking pills.

In addition, in case of intoxication, it is important to regularly monitor blood pressure levels and artificially maintain them if necessary.

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

Interactions with other drugs

The drug platifillin has vasodilatory, sedative and antispasmodic properties, that is, its medicinal effect is similar to the action of Papaverine. These drugs differ only in the mechanisms of their pharmacological action, so they are allowed to be used in combination in the conservative treatment of hypertensive crisis, spastic syndromes, and other painful conditions.

No-shpa also demonstrates good interaction with the drug. The drugs have a synergistic effect on smooth muscles. Such a drug combination is often used in gynecology and obstetrics in 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, the use of Papaverine in the form of an injection solution or tablets during drug therapy for shaking palsy is prohibited.

The combined use of the drug with anticholinergic drugs manifests itself in the form of potentiation of the medicinal effect of the latter. Because of this, if it is necessary to combine them, it is necessary to consult with your doctor about reducing the dosage or temporarily stopping taking the drug.

[ 40 ], [ 41 ], [ 42 ]

Storage conditions

Papaverine should be kept in a dark place, protected from moisture and out of reach of children. The medicine should be stored at a temperature of no more than 25°C.

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

Special instructions

Reviews

Papaverine has a wide range of medicinal activity, so reviews of it appear on medical forums of various specializations. This remedy is used to treat many different diseases.

For example, many positive reviews of the drug are left by proctologists, as well as people who use the drug to treat hemorrhoids, which are quite common these days. Rectal suppositories Papaverine help to facilitate the process of defecation and partially relieve pain, and in addition, eliminate bleeding that occurs in the area of enlarged hemorrhoids. All these positive effects are often mentioned in discussions on forums.

In addition, the positive effect of suppositories during pregnancy is often mentioned, because their relaxing and antispasmodic effect promotes rapid and complete elimination of uterine hypertonicity, preventing the risk of premature birth. The active element of the drug helps to relieve pain resembling labor contractions (they are often observed in the last stages of gestation). At the same time, the drug is often used for prevention in obstetric hospitals.

[ 47 ]

Shelf life

Papaverine must be used within 2 years from the date of manufacture of the drug.

[ 48 ], [ 49 ], [ 50 ]