Papaverine

Pharmacological properties

papaverine is an alkaloid found in opium. Papaverine is a myotropic antispasmodic. it reduces tone, reduces contractile activity of smooth muscles and, in connection with this, has a vasodilating and antispasmodic effect. Papaverine is an inhibitor of the PDE enzyme; it causes intracellular accumulation of cyclic 3 ’, 5’-adenosine monophosphate (cAMP). accumulation of cAMP leads to impaired contractility of smooth muscles and their relaxation in spastic conditions. the effect of the drug on the central nervous system is weakly expressed, only in high doses does it have a slight sedative effect.

Pharmacokinetics With parenteral administration, the drug quickly forms stable complexes with plasma albumin. It easily penetrates the histohematological barriers. Metabolized in the liver. About 60% is excreted in the form of compounds, mainly phenolic, with glucuronic acid and only in a small amount - unchanged. T_½ - 0.5–2 hours

Indications

Spasms of the smooth muscles of the abdominal organs (pylorospasm, irritable bowel syndrome, cholecystitis, attacks of gallstone disease);

• urinary tract spasms, renal colic;
• cerebrovascular spasm;
• peripheral vascular spasms (endarteritis).

Application

The drug is used s / c, v / m and / v.

P / to and in / m to enter to adults and children over the age of 14 years on 0,5–2 ml (10–40 mg) of 2% solution, and to / in to enter very slowly, with a speed of 3-5 ml / min, dissolving 1 ml of 2% solution of papaverine hydrochloride (20 mg) in 10-20 ml of 0.9% solution of sodium chloride. Most effective in / in the introduction.

For elderly patients, a single dose at the beginning of treatment should not exceed 10 mg (0.5 ml of 2% solution).

The maximum doses for adults with sc or intramuscular administration: a single dose - 100 mg (5 ml 2% solution), a daily dose of 300 mg (15 ml 2% solution); with the on / in the introduction: single - 20 mg (1 ml 2% solution), daily - 120 mg (6 ml 2% solution).

For children aged 1 year to 14 years, use the drug 2-3 times a day. A single dose is 0.7–1 mg / kg body weight.

The maximum daily dose for children is (regardless of the method of administration):

at the age of 1-2 years - 20 mg (1 ml of 2% solution);

3-4 years - 30 mg (1.5 ml of 2% solution);

5-6 years - 40 mg (2 ml of 2% solution)

7–9 years old - 60 mg (3 ml of 2% solution);

10-14 years - 100 mg (5 ml of 2% solution).

Contraindications

Hypersensitivity to the components of the drug, arterial hypotension, impaired av-conduction, coma, respiratory depression, simultaneous use of MAO inhibitors, glaucoma, liver failure, bronchial obstruction syndrome, age over 75 years (risk of hyperthermia).

Side effects

From the central and peripheral nervous system: drowsiness, increased sweating, weakness, headache, dizziness.

From the sensory organs: impaired vision, diplopia.

From the gastrointestinal tract: anorexia, nausea, constipation, dry mouth, diarrhea.

From the liver and biliary tract: jaundice, impaired liver function, increased activity of hepatic transaminases.

From the cardiovascular system: arrhythmias, tachycardia, arterial hypotension, partial or complete block, asystole, ventricular extrasystole, ventricular fibrillation / flutter, collapse.

Blood side: eosinophilia.

On the part of the respiratory system: apnea.

From the skin, subcutaneous tissue and immune system: hypersensitivity reactions, including from the respiratory system, anaphylactic shock, itching, skin rash, urticaria, flushing of the upper body, face and hands.

Other: reactions at the injection site, including thrombosis at the injection site.

special instructions

With caution and in doses below the average therapeutic, it should be prescribed:

• elderly patients and debilitated patients;
• patients with traumatic brain injury;
• patients with chronic renal failure;
• patients with supraventricular tachycardia, severe heart failure with decompensation;
• with adrenal insufficiency, hypothyroidism, prostatic hyperplasia, shock conditions.

In / in the drug should be administered very slowly and under the control of blood pressure, heart rate, ECG.

With caution, iv injection of the drug should be prescribed for stenotic coronary sclerosis.

In the elderly, hyperthermia may occur.

Smoking worsens the effectiveness of the drug.

During the period of use of the drug, it is necessary to stop drinking alcohol.

Use during pregnancy and lactation. Safety and effectiveness of the drug during pregnancy and lactation have not been established. For the period of treatment should stop breast-feeding.

Children. The drug is used in children aged 1 year.

The ability to influence the reaction rate when driving vehicles or other mechanisms. During treatment should refrain from driving vehicles or working with mechanisms.

Interactions

The antispasmodic effect of papaverine is enhanced by barbiturates, diphenhydramine, metamizole, diclofenac. the hypotensive effect is enhanced with the simultaneous use with antihypertensive drugs of other groups, as well as with tricyclic antidepressants, procainamide, reserpine, quinidine. papaverine may reduce the antiparkinsonian effect of levodopa and the hypotensive effect of methyldopa. with simultaneous use with alprostadil for intracavernous administration, there is a risk of priapism. phentolamine potentiates the effect of papaverine on the cavernous bodies of the penis with combined use.

With simultaneous use with cardiac glycosides, a marked increase in myocardial contractile function is observed due to a decrease in OPSS. When used with Novocaineamide, an increase in the hypotensive effect is possible.

It is possible to reduce the severity of the tonic effect of anticholinesterase drugs on smooth muscles under the influence of papaverine hydrochloride.

It is possible to reduce the antispasmodic activity of papaverine hydrochloride under the influence of morphine. However, papaverine hydrochloride is used simultaneously with morphine hydrochloride to reduce the severity of the spasmogenic effect of the latter and with promedol in case of pain associated with smooth muscle spasms.

There is evidence of the development of hepatitis with combined use with furadonin.

With the combined use of reserpine with papaverine hydrochloride, the antihypertensive effect is enhanced.

When combined with antidepressants, an increase in the hypotensive effect is possible.

Pharmaceutically compatible with dibazole.

With the simultaneous use of papaverine hydrochloride potentiates the effect of alcohol.

Smoking. In patients who smoke, papaverine metabolism is accelerated, and its plasma concentration and pharmacokinetic effects are reduced.

Incompatibility. Pharmaceutically compatible with dibazole, chemically incompatible with sodium caffeine benzoate. Use only recommended solvent.

Overdose

Symptoms: impaired vision, diplopia, weakness, dry mouth, constipation, redness of the skin of the upper body, hyperventilation, nystagmus, ataxia, tachycardia, arterial hypotension, asystole, ventricular flutter, collapse. with the use of high doses of the drug and its rapid introduction into the vein, the development of arrhythmias or complete av-blockade is possible. when used in very high doses, papaverine has a moderate sedative effect.

Treatment: stop using the drug. The treatment is symptomatic. It is completely removed from the blood during hemodialysis. There is no specific antidote.

Storage conditions

In the original packaging at a temperature not exceeding 25 ° C. do not freeze.