Papaverine: instructions for use, indicationsduring pregnancy, dosage

Update: October 2018

Papaverine – an antispasmodic drug that
actively used to reduce the contractile function of smooth
muscle fibers and reduced muscle tone, which leads to
rapid relaxation of smooth muscles. Is a derivative of opioid
alkaloids and produced by the method of synthesis.

Appointed to eliminate spasms of the biliary tract,
ureters, gastrointestinal tract, reducing the tone of the uterus.
Used as a vasodilator for the coronary system.
circulation in hemorrhages of the subarachnoid type and
coronary artery bypass surgery, as well as in a number of other cases.

Фармгруппа: миотропные спазмолитики.

Composition, physico-chemical properties, price

Available in three forms: rectal suppositories (suppositories),
tablets, injection.

Pills A solution of 2% (papaverine in ampoules) Suppositories
Main substance 10 or 40 mg of papaverine hydrochloride in 1 tab. On 20 mg of papaverine hydrochloride in 1 ml of p-ra – 2 ml of p-ra in 1
ampoule
20 mg papaverine hydrochloride
Excipients Sugar, starch, stearic acid, talc Edetate disodium, L-methionine, water d / i Semi-synthetic glycerides up to 2 grams
Physicochemical properties White tablets with two perpendicular risks located
divide the tablet into 4 equal parts

Clear solution, colorless or slightly yellow

Torpedo-shaped suppositories, solid. White color. Without
smell.
Packaging 10 pcs. in blister cell blisters. In carton packs
1-3 blisters

5 or 10 ampoules in cartons

5 suppositories in polyethylene blisters. 2 blisters each
carton package
Price 40 mg № 10 – 10-40 rubles. № 10 – 35-50 rubles. № 10 – 35-70 rubles.

pharmachologic effect

папаверин инструкцияPapaverine hydrochloride is
inhibitor (inhibitory) of the enzyme phosphodiesterase and
leads to accumulation of cyclic 3,5-adenosine monophosphate,
decrease the level of calcium inside the cells, which causes a violation
contractility of muscle fibers and relaxation of smooth muscle
structures of internal organs and blood vessels. In medium therapeutic doses on
affects the central nervous system. In high doses leads to a decrease in
excitability of muscle tissue of the heart and slows down the speed
intracardiac conduction. A feature of the drug is
lack of paralytic effect – the muscles only relax,
while their movements and functions are fully preserved.

In addition to the antispasmodic effect, the drug has a moderate
local anesthetic effect, characterized by minor
antihypertensive and sedative properties.

Pharmacokinetics

Fully and quickly absorbed, comes into contact with plasma
proteins by 90%. It penetrates the blood-brain barrier and during
all fabrics. Undergoes biotransformation in the liver. Period
The half-life ranges from 0.5 to 2 hours. Excreted by the kidneys in
form of metabolites.

Indications

  • smooth muscle spasms;
  • gastrointestinal spasms on the background of cholecystitis, spastic colitis;
  • pylorospasm;
  • renal colic;
  • spasms of peripheral vessels;
  • vascular spasms of the central nervous system;
  • spasms of heart vessels against the background of angina and hypertensive
    crisis (as part of complex treatment);
  • urinary retention on the background of urinary tract spasm;
  • bronchospasm.

Assigned as an auxiliary drug for premedication.
before surgery on the gastrointestinal tract, proctologic and
urological procedures.

Contraindications

  • Glaucoma
  • AV blockade
  • Severe liver failure
  • Older age over 75 years
  • Children age up to six months (up to 12 months – on other
    sources)
  • Hypersensitivity to the main or auxiliary
    components.

Papaverine during pregnancy

Candles with Papaverine during pregnancy are quite often prescribed
by doctors. The main reason for prescribing the drug is
hypertonicity of the uterus, which is known to be one of the reasons
miscarriage of the fetus (especially often papaverine is prescribed in the early
pregnancy), as well as preeclampsia. Because the uterus is
a muscular organ, to relax it and prescribe a drug that is very
often in combination with hormonal drugs.

In combination with No-Shpa, Papaverine is prescribed at a later date.
carrying to prepare the cervix for labor.
However, many obstetrician-gynecologists are against such training because
this leads to artificial inhibition of uterine contractility and
weak labor activity.

The instructions to Papaverine noted that the effect of the drug in
the period of pregnancy and lactation has not been studied, therefore, to assert
its security is impossible. This means that the appointment can
carry out only a doctor, weighing the possible benefits and risks. How much and
How to take papaverine, should tell the attending physician, self-treatment
is unacceptable.

Papaverine children

In children under one year, the main indication for treatment is spastic.
GI pain and intestinal colic. Older children are assigned to withdraw
bronchospasm, in the treatment of pancreatitis, urethral spasms, hepatic
colic.

Another application is withdrawal. peripheral spasms
hyperthermia: papaverine is given 20 minutes before
antipyretic.

Side effects

  • General: hyperthermia (especially in the elderly).
  • Immune system: allergic phenomena, skin flushing and rash,
    itchiness
  • CNS: excessive sweating, drowsiness, dizziness,
    weakness, migraine.
  • Organs of vision: decreased vision, diplopia.
  • Gastrointestinal tract: nausea, diarrhea, constipation, dry mouth.
  • CVS: asystolia, arrhythmia, ventricular premature beats,
    tachycardia, ventricular fibrillation, arterial hypotension,
    collapse.
  • Respiratory system: apnea.

The treatment is likely to increase the activity of the liver.
transaminase and development of jaundice. In general, a blood test is possible.
eosinophilia.

For rapid intravenous administration or when administered at high
Doses can develop AV blockade. At the injection site
possible thrombosis.

Dosage

Dosage Папаверина отличается для различных лекарственных форм
and different age groups.

Pills:

  • Adults and children from 15 liters: 40-60 mg three to five times a
    days
  • Children 6-24 m: 5 mg (half a tablet of 10 mg)
    трех-четырехкратно в days
  • Дети 2-4 года: 5 – 10 мг трех-четырехкратно в days
  • Дети 5-6 лет: по 10 мг трех-четырехкратно в days
  • Дети 7 лет: по 10-15 мг трех-четырехкратно в days
  • Дети 10-14 лет: по 15-20 мг трех-четырехкратно в days

The use of Papaverine tablets for children younger age
groups should be carried out after preliminary dissolution in
water.

Candles:

Enter rectally. The suppository can be cut.

  • Взрослые: по 20-40 мг (1-2 свечи) двух-трехкратно в days
  • Дети от 10 лет: по 20 мг (1 свече) 2 р в days
  • Дети 5-10 лет: по 10 мг (полсвечи) 2 р в days
  • Дети до 4 л: 5 мг (четвертина свечи) 2 р в days

Solution (papaverine injections):

  • Single dose for adults and children from 14 years with intramuscular
    and subcutaneous injection (injections) is 10-40 mg, and the maximum
    single – 100 mg (or 5 ml of solution). Between introductions should
    observe the 4 hour interval. The maximum dose per day – 300 mg
    (15 ml of solution).
  • For intravenous administration, which is considered the most
    effective, 1 ml of 2% p-ra (20 mg) dissolved in 10-20 ml p-ra NaCl
    0.9%, which is a single dose. Maximum Daily Dose –
    120 mg (or 6 ml of solution). In / in the introduction is justified in severe
    patient’s condition, after 3-4 days it is recommended to switch to tablets
    or candles.
  • For children 1-14 years old, the maximum single dose is calculated
    individually and is 0.7-1 mg per 1 kg of weight. amount
    введений: 2 р в days
  • The maximum daily dose depends on age and is the same for
    all method of administration:

    • 1-2 years – 1 ml of p-ra (20 mg);
    • 3-4 years – 1.5 ml of the p-ra (30 mg);
    • 5-6 years – 2 ml of p-ra (40 mg);
    • 7-9 years – 3 ml of p-ra (60 mg);
    • 10-14 years – 5 ml (100 mg).

Features of the solution

The drug can be administered subcutaneously, intravenously and intramuscularly.
IV administration is carried out slowly, controlling performance
heart, especially in patients with stenotic
coronary sclerosis.

Overdose

Visual impairment, weakness, redness of the skin, dry mouth,
arterial hypotension, constipation, ataxia, asystole, tachycardia,
трепетание желудочков, collapse.

The specific antidote does not exist, therefore it is organized
symptomatic treatment, and in severe cases – hemodialysis.

Features of treatment

Since smoking decreases the effectiveness of papaverine,
give up the habit at least for the duration of treatment. Also impossible
drink alcohol with papaverine (potentiates the action
alcohol).

During therapy, you should abandon work and activities where
important reaction rate.

For elderly patients, patients with head injury, chronic renal failure, supraventricular
tachycardia, decompensated heart failure,
diseases of the endocrine system, with shock conditions initial
the dose is set below the average therapeutic, most often not
more than 10 mg (or 0.5 ml of 2% p-ra).

Drug interactions

  • Compatible with Dibazol without developing negative reactions (for
    cupping hypertensive crisis).
  • Combination with anticholinergic agents – enhancement
    anticholinergic action;
  • Use with Alprostadil for its intracavernous administration
    possible development of priapism;
  • Combined use with Levodopa leads to a decrease in
    the effectiveness of the latter;
  • In combination with methyldopa decreases hypotensive
    Effect;
  • With the appointment of cardiac glycosides increases
    myocardial contractile function;
  • When used together with antihypertensive drugs,
    Procainamide tricyclic antidepressants, Reserpine,
    Хинидином, Новокаинамидом усиливается гипотензивный Effect;
  • There is evidence of the development of hepatitis in combination with
    Furadonin.
  • Barbiturates, Metamizole (Analgin), Diphenhydramine
    (Димедрол), Диклофенак усиливают спазмолитический эффект
    Papaverine.

Analogs

Papaverine bufus, Papaverine hydrochloride MS, Papavin.

Автор: врач-гигиенист, эпидемиолог

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