Of the antispasmodic drugs, "Papaverine" is one of the safest means, which is used for various pathologies. For what diseases and for what purpose "Papaverine" is prescribed, it will become clear if you understand the mechanism of its action. Like all medicines, this medication is prescribed only by a doctor.
What is papaverine
Papaverine hydrochloride is a medicinal substance with a vasodilating and antispasmodic effect. Contained in poppy plants. What is papaverine, people learned in the middle of the XIX century, although even in ancient Roman sources it is told about mixing in a substance with a similar name. At the beginning of the 20th century, papaverine learned to synthesize, and now it is a drug widely used in medicine.
Papaverine action
The action of papaverine on smooth muscle cells is associated with enzymatic processes, which ultimately reduce the amount of calcium inside the cell, so that smooth muscles relax. This ability extends to the gastrointestinal tract, biliary tract, cells lining the bronchi, urinary system, cells of the vascular wall, heart muscle, and muscle layer of the uterus. It describes a weak sedative effect on the brain of patients.
Suction and removal
The drug substance is able to assimilate by 54%. The drug binds well with blood plasma proteins (90%). In the body, it quickly passes between blood and tissue fluid, penetrating into all cells of the body, including the brain. Papaverine conversion reactions occur in the liver cells. It is eliminated from the body quickly enough: the half-life is from thirty minutes to two hours, but with liver diseases a much longer elimination of the substance is possible. The medication is removed by the kidneys, therefore, it is important to know that in dialysis patients, accelerated excretion of papaverine (what you already know) with urine is possible.
Indications for use
From what papaverine helps, it becomes clear based on its mechanism of action. The drug has an antispasmodic effect and is used:
- To relieve stomach cramps caused by intoxication, inflammation (gastritis), peptic ulcer and functional disorders of the nervous system.
- Elimination of biliary tract spasms with cholecystitis, cholangitis, impaired function due to imbalance in the regulation of the nervous system, cholelithiasis.
- In the treatment of spastic processes in the intestine associated with inflammatory diseases of the small and large intestines, functional spasms.
- To reduce bronchospasm in acute and chronic bronchitis, bronchial asthma, pneumonia.
- When eliminating the causes of spasm of the walls of the urinary tract and blood vessels of the kidneys due to infectious processes, impaired relaxation function as a result of pathology of the peripheral nervous system.
- To relieve vascular spasms in inflammatory processes in the arteries, functional spasms of the brain causing headaches, arterial hypertension.
- In combination with other medicines to treat angina pectoris.
- "Papaverine" during pregnancy in the early stages is used to relieve increased uterine tone.
- To relieve cramps in the muscles of the uterus and relieve pain during menstruation in women.
- In preparation for surgical interventions to provide a light sleeping pill in conjunction with other means for sedation.
Dosage "Papaverine"
The drug is used in tablets of 40 mg, suppositories of 20 mg and in injections of 40 mg.
The dosage of Papaverine for adults is two tablets (suppositories) or one ampoule intramuscularly three times during the day. The maximum dose is possible up to 240 mg per day with severe painful spasmodic sensations. The introduction of the drug in any way should be carried out no more than four hours later.
Taking the medicine does not depend on food. The action develops quickly enough, the medication begins to relieve spasmodic pains thirty minutes after use.
The duration of taking "Papaverine" is individual and with chronic pain may be long.
Use in childhood
For infants up to six months, the drug is contraindicated. Starting from six months of age and up to two years, you can give 5 mg three times a day. Children 3-4 years old are given 5-10 mg three times a day. At five and six years of age - 10 mg, that is, 1/4 tablet three times a day. From seven to nine years, 10-15 mg three times a day is given. Children 10-14 years old - from 15 to 20 mg three times a day. From the age of 15, the dosage corresponds to that in adults, which is 40 mg three times a day.
Pregnancy
In the first trimester of pregnancy, women often have an increased tone of the uterus, that is, muscle spasm. This can lead to an early miscarriage. Pathology is often accompanied by pain in the abdomen and in the sacral region, sometimes there may even be discharge, as during menstruation. Such patients are hospitalized in the Department of Pregnancy Pathology and Papaverine is prescribed for use in injections. In this case, the drug perfectly relaxes the smooth muscles of the uterus, improves blood circulation, without exerting a harmful effect on the developing child.
Candles "Papaverine" in the early stages have the same positive effect. Apply them 3-4 times a day, depending on the condition. Such treatment should be carried out under the mandatory supervision of a doctor to avoid strong relaxation of the uterine muscles.
Use for arterial hypertension
Arterial hypertension, which is accompanied by cerebrovascular spasm and an increase in blood pressure, can be stopped with the help of Papaverine and Dibazol, administered together. "Dibazole" is an antispasmodic, eliminating spasm of peripheral vessels and muscles of internal organs. The combination of these two antispasmodics can increase the chances of lowering blood pressure and quickly improve the patient's condition. One ampoule of "Dibazole" in 2 ml contains 10 mg of the active substance.
In case of hypertensive crisis, 1-2 ampoules of each substance are administered intramuscularly or slowly intravenously in one syringe. Papaverine and Dibazole tend to mutually reinforce each other. It is undesirable to use this combination for older people who have heart problems. "Dibazol" is contraindicated in case of epilepsy and convulsive seizures of another etiology, as well as hypersensitivity to this drug.
Contraindications
Studying what Papaverine is, you should understand who should not take this drug:
- Babies up to six months of age.
- Elderly people over 70 who have a sick heart that is less capable of pumping blood through the body.
- Persons having myocardial infarction.
- Patients with atrioventricular block, slowing down the pulse between the ventricle and the atrium, which leads to a decrease in heart rate and a decrease in the discharge of blood into the aorta.
- With increased eye pressure.
- Severe liver failure.
- In case of respiratory failure, obstructive pulmonary processes.
- In patients with impaired consciousness (in a coma and soporous state).
- With increased individual sensitivity.
special instructions
"Papaverine" for the most part is well tolerated, but it should be used with caution in the following cases:
- Propensity for low blood pressure and bradycardia.
- Decreased thyroid function.
- Inadequate production of adrenal hormones.
- Chronic kidney disease with insufficiency.
- Dyshormonal prostatic hyperplasia in men.
- Brain injuries.
- Shock states.
- ECG signs of supraventricular tachycardia.
- When driving vehicles and high-altitude work, the effect of Papaverine on the body should be taken into account.
Side effects
What is Papaverine used for, we described above, but it does not always bring only positive results. Undesirable consequences are sometimes possible:
- Nausea, discomfort in the abdomen, dry mouth, constipation, diarrhea, bloating, instability of appetite.
- Decrease in blood pressure up to collapse, extrasystoles, arrhythmias, tachycardia, bradycardia, blockade, dizziness.
- Drowsiness, lethargy, impaired vision, headache, sensitivity to light.
- Increased eosinophils in peripheral blood.
- An increase in body temperature above 37 degrees (more often in young children and the elderly).
- Increased sweating.
- Yellowness of the skin and sclera.
- Allergic rashes, Quincke's edema.
- Burning sensation in the place where the injection was made.
- Vein thrombosis with a tendency to thrombosis.
Overdose
Exceeding the dose of Papaverine can lead to a general deterioration. The patient will complain of double vision, painful sensitivity to light, fatigue, drowsiness, discomfort in the heart, a decrease in heart rate, dizziness. Perhaps the development of respiratory arrest.
Assistance should be provided immediately. When breathing stops, cardiopulmonary resuscitation is indicated. In milder cases, when taking the tablets, gastric lavage and sorbent intake (activated charcoal) are performed. With an intravenous overdose, dialysis can be used to quickly cleanse the body.
Drug interactions
It should be clarified whether Papaverine can be used with other medicinal substances.
The use of alcohol during treatment with this drug is contraindicated due to increased toxic effects on liver cells. Nicotine reduces the effect of Papaverine, so smoking should be stopped or reduced so as not to reduce the effectiveness of the treatment.
Anticholinergic drugs (Atropine, Cyclodolum, Ipratropium bromide) may be more potent when used together with Papaverine, so their dosage should be adjusted.
Reducing the effect of "Levodopa" (a drug for parkinsonism), "Methyldopa" and "Dopegita".
It may be more likely to cause a heart rhythm failure when used simultaneously with 3-adrenergic drugs (Reserpine, Octadine).
The sedative effect when combined with sleeping pills, narcotic, anti-anxiety, antidepressant, antipsychotic and pain medication is enhanced.
Taking drugs to lower blood pressure, you should adjust their dose due to the high probability of hypotension.
Release form and trade names
In tablet form, the drug is available in the following names only by domestic manufacturers:
- Papaverine is a pharmaceutical product manufactured by Pharmstandard-Tomskkhimfarm OJSC.
- "Papaverine" in tablets of 40 mg, manufactured by JSC "Irbitsky HFZ".
- "Papaverine" company PJSC "Biosynthesis."
- "Papaverine hydrochloride MS" manufactured at the company ZAO Medisorb.
In the form of rectal suppositories, the drug in Russia is represented by domestic medicines:
- "Papaverine" suppositories of 20 mg produced by JSC "Biochemist".
- “Papaverine” rectal suppositories made by Nizhpharm JSC.
- "Papaverine" rectal suppositories manufactured by the Tula Pharmaceutical Factory.
- "Papaverine hydrochloride" candles PJSC "Biosynthesis."
- "Papaverine hydrochloride" suppositories of OJSC "Dalkhimpharm."
The drug for injection of 2 ml is available at Russian enterprises under the names:
- Papaverin, manufacturers: OJSC Novosibkhimpharm, LLC Grotex, JSC Veropharm, OJSC Biochemist, PJSC Biosynthesis, LLC Ellara.
- Papaverine Bufus, manufactured by PFK Update.
- "Papaverine hydrochloride" enterprises: OJSC "Moskhimpharmpreparat them. N. A. Semashko, Atoll LLC, Slavic Pharmacy LLC, Dalkhimpharm OJSC, Armavir Biofactory FKP.
As well as the imported “Papaverine” in solution from the Republic of Belarus, made at OJSC “Borisov Plant of Medical Preparations”.