Papaverine forte instructions for use. What does papaverine help with?
Instructions
on medical use of the drug
PAPAVERINE
Tradename
Papaverine
International nonproprietary name
Dosage form
Tablets 0.04 g
Compound
One tablet contains
active substance- papaverine hydrochloride 0.040 g,
Excipients: potato starch, sucrose, stearic acid.
Description
Tablets are white, flat-cylindrical with a score and a chamfer.
Farmacotherapy group
Drugs for the treatment of functional gastrointestinal disorders. Papaverine and its derivatives.
ATS code A03AD01
Pharmacological properties
Pharmacokinetics
After oral administration, it is quickly absorbed from the gastrointestinal tract. Bioavailability is 29-57%. Therapeutically effective concentrations of the drug in blood plasma are 0.2-2.0 mcg/ml. With repeated use of the drug, its pharmacokinetics do not change.
Binds to plasma proteins by 90%. Easily passes through histohematic barriers. Forms a depot in the liver and adipose tissue. Subject to biotransformation in the liver. The half-life of papaverine (T ½) is 0.5-2.0 hours. It is excreted in the form of phenolic metabolites conjugated with glucuronic acid in the urine; small amounts of papaverine (less than 0.5%) are excreted unchanged.
Pharmacodynamics
Papaverine has a hypotensive and myotropic antispasmodic effect.
The mechanism of action is associated with the ability of papaverine to block the activity of phosphodiesterase type IV. Blockade of the enzyme leads to the cessation of cAMP hydrolysis and an increase in its concentration in the smooth muscle cells of blood vessels and internal organs. cAMP limits the flow of calcium ions into the muscle cell and inactivates the kinase of myosin light chains, a contractile protein that ensures muscle contraction.
Papaverine reduces the tone and relaxes the smooth muscles of internal organs (gastrointestinal tract, respiratory tract, genitourinary system) and blood vessels. Papaverine dilates mainly arterial vessels and helps increase blood flow, including cerebral. Has a hypotensive effect. In high doses, it reduces the excitability of the heart muscle and slows down intracardiac conduction.
When used in average therapeutic doses, papaverine has virtually no effect on the central nervous system.
Indications for use
- spasms of smooth muscles of internal organs with cholecystitis, spastic colitis, pylorospasm (prevention and relief)
- encephalopathy of vascular origin (as part of complex therapy)
Directions for use and doses
Use internally on an empty stomach. Adults are prescribed 0.04-0.06 g (1-1½ tablets) 3-5 times a day. The highest single dose is 0.4 g (10 tablets), the maximum daily dose is 0.60 g (15 tablets). The duration of the course of treatment is 10-14 days; if necessary, repeated courses of use of the drug are possible at intervals of 7-10 days.
For persons over 70 years of age, the initial single dose is no more than 0.01 g (¼ tablet).
Children over 10 years of age are prescribed a dose of 0.3-0.5 mg/kg body weight 2-3 times a day.
Side effects
- nausea, constipation
- drowsiness
- increased sweating
- increased transaminase levels, eosinophilia
- hypotension, atrioventricular block, ventricular extrasystole
Contraindications
- hypersensitivity to papaverine and other components
drug
- respiratory depression or coma
- atrioventricular block
- glaucoma
- children under 10 years old
- age over 75 years (risk of hyperthermia)
Drug interactions
Reduces the antiparkinsonian effect of levodopa and the hypotensive effect of methyldopa. In combination with barbiturates, the antispasmodic effect of papaverine hydrochloride is enhanced. When used together with tricyclic antidepressants, procainamide, reserpine, quinidine sulfate, the hypotensive effect may be enhanced.
special instructions
Caution should be exercised and only small doses of papaverine should be used in persons with traumatic brain injury, impaired liver and kidney function, hypothyroidism, and adrenal insufficiency, since the hypotensive effect of papaverine is enhanced in them. In persons with benign prostatic hyperplasia, high doses of papaverine can provoke the development of acute urinary retention.
When using papaverine hydrochloride, you should avoid drinking alcohol-containing drinks, as well as medicines containing ethyl alcohol.
Use in pediatrics
The use of papaverine hydrochloride tablets in children under 10 years of age is not recommended.
Pregnancy and lactation
During pregnancy and lactation, the safety and effectiveness of papaverine hydrochloride have not been established.
Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms
Considering the side effects of the drug, you must be careful when driving vehicles or other mechanisms.
Overdose
Symptoms: diplopia, weakness, drowsiness, hypotension.
Treatment: there is no specific antidote. Helpful measures include discontinuation of the drug, gastric lavage with milk and activated carbon, and symptomatic therapy aimed at eliminating the resulting disorders and increased blood pressure.
Papaverine is a popular drug that is widely used as an antispasmodic. This remedy is even used in the treatment of impotence. How it works and what it helps with can be found in the detailed instructions for using Papaverine.
Release form and composition
Papaverine is available in three forms. These can be tablets - papaverine hydrochloride, injection solution, as well as suppositories that are administered rectally. The composition includes papaverine hydrochloride in different concentrations, depending on the form of release. The tablets also contain talc, refined sugar and potato starch. Additional components in the injections are disodium edetate, D, L - methionine. And in rectal suppositories you can find cosmetic stearin and hard fat.
Indications for use
Antispasmodic Papaverine is used for a wide variety of diseases and pathologies. Among them:
- Renal colic.
- Angina pectoris.
- Spasm of smooth muscles in various diseases.
- Endarteritis.
- Bronchospasm.
- Urinary retention due to spasm of the urinary tract.
- Spasms of the vascular bed.
- Constriction of blood vessels in the brain.
- Hypertensive crisis.
In addition, the drug is used in medicinal preparation for operations, to relax muscle tissue.
Contraindications
Like any drug, Papaverine has its own number of contraindications for which the doctor should not prescribe this drug.
The main contraindications include:
- Glaucoma.
- Severe renal failure.
- Intracardiac conduction disorders.
- Intolerance to at least one of the components of the drug.
- Elderly age.
- Young age (up to six months).
In addition to direct contraindications, there are several restrictions that require consultation with a specialist.
Such restrictions include:
- The patient has recently suffered a traumatic brain injury.
- Hypothyroidism.
- Supraventricular tachycardia.
In any case, like any medicine, Papaverine should be taken only after consultation with a specialist. The doctor will carefully evaluate your medical history, look at your medical history, the medications used, and, after assessing all possible side effects and contraindications, prescribe the dose and duration of the course.
Side effects of Papaverine and overdose
Side effects can occur from many body systems. This happens due to the fact that almost everywhere in our body there is smooth muscle, which is affected by the drug. From the gastrointestinal tract, nausea, bloating, constipation, as well as excessive activity of liver transaminases are observed. From the blood and cardiovascular system, low blood pressure may occur, as well as tachycardia and atrioventricular block.
If side effects occur, you should contact a specialist to adjust the dosage or replace the drug with a similar one.
In case of an overdose, several symptoms appear, including double vision, weakness, drowsiness, decreased blood pressure, as well as fatigue, loss of strength and performance.
There is no special drug to neutralize the effects. Treatment is exclusively symptomatic. Gastric lavage with milk and activated carbon has a positive effect. The most important thing is to prevent blood pressure from falling to a critical level. If necessary, it is worth increasing it with the help of medications.
Interaction with other drugs
When prescribing complex treatment of Papaverine with other drugs, their interactions must be taken into account. For example, it is effective to use Papaverine in combination with Platyphylline, which has a similar effect. Positive results have been noticed when combining Papaverine with No-shpa, especially in gynecology.
If a patient suffers from Parkinson's disease and takes Levodopa, then Papaverine is contraindicated for him; it is better to replace it with another antispasmodic. The price may be similar or slightly different.
Papaverine and erection
Papaverine is used for potency. Thanks to the administration of this medicine, the blood vessels dilate, which improves the flow of blood to the penis. This promotes erection. The procedure can be performed by a doctor or the patient himself. The process is performed with a small needle, which is inserted a centimeter into the penis. After the injection, an erection occurs within 5-15 minutes and lasts about an hour.
In addition to treating impotence, papaverine is used for its diagnosis. If the patient, in principle, is unable to achieve an erection, then with the introduction of Papaverine it will not occur.
When using the drug as an erection aid, you should be careful about the dosage, since an injection of a large dose can lead to an abnormal erection, which will be accompanied by pain. In any case, consultation with a specialist is required who can calculate the dose and advise how long to use this drug for this purpose.
Instructions for use
To take Papaverine, you need a doctor's prescription. It is sold in pharmacies only by prescription.
In order to avoid side effects, the dosage should be strictly observed. It depends on the form in which papaverine is used:
- Pills. Take 3-4 times a day. The dose depends on age: up to 2 years 0.005 g, 3-4 years - 0.01 g, 5-6 years - 0.01 g, 10-14 years - 0.02 g, adults - up to 0.08 gram per appointment.
- Papaverine suppositories - suppositories are used that have a dosage of 0.02 g. substances. Gradually the dosage increases to 0.04 g. Use up to 3 suppositories per day.
- Papaverine injections. The single and daily dose is calculated by the doctor. The ampoules contain 2 ml. For adults, the daily dose is 0.3 grams.
The dosage is calculated depending on the presence of chronic diseases, as well as age and severity of the pathology. Reviews are mostly positive, especially from those who used Papaverine for impotence.
Analogues of the drug
Among the analogues of Papaverine, Caverject is known. Used to treat sexual impotence. An excellent analogue of antispasmodics is No-spa, which also successfully relieves spasms of smooth muscles.
Conclusion
Papaverine tablets and what they are used for are known to many. But they must be prescribed by a doctor, since, like all medications, Papaverine must be dosed correctly. The price of the medicine depends on the form of release. Tablets, on average, cost 10 rubles, injections 35 rubles, and suppositories - 62 rubles. At some points of sale the price may vary slightly.
Description of the dosage form
Papaverine
Papaverine hydrochloride
Composition and release form
Rectal suppositories:
1 suppository contains papaverine hydrochloride 20 mg;
Excipients: hard fat, type A or vitepsol - a sufficient amount to obtain a suppository weighing from 1.19 to 1.31 g;
in a blister pack 5 pcs., in a cardboard pack 2 packs.
Solution for injection 2%:
1 mg of solution contains 20 mg of papaverine hydrochloride;
in ampoules of 2 ml, 10 ampoules per box.
Pills:
1 tablet contains 40 mg of papaverine hydrochloride;
10 tablets per package.
pharmachologic effect
Myotropic antispasmodic agent. Has a hypotensive effect. Inhibits phosphodiesterase, causes accumulation of cyclic 3`,5`-AMP in the cell and a decrease in calcium levels; reduces tone and relaxes smooth muscles of internal organs (gastrointestinal tract, respiratory and genitourinary systems) and blood vessels. Causes dilation of arteries, increases blood flow, incl. cerebral. In large doses, it reduces the excitability of the heart muscle and slows down intracardiac conduction. The effect on the central nervous system is weak, but in large doses it has a sedative effect.
Myotropic antispasmodic agent. Reduces the tone of smooth muscles of internal organs and blood vessels. Causes dilation of arteries, increases blood flow, incl. cerebral. When used in average therapeutic doses, papaverine has virtually no effect on the central nervous system.
Pharmacokinetics
Absorption is high. Penetrates histohematic barriers. Excreted by the kidneys (in the form of metabolites).
Indications
Spasm of smooth muscles of the abdominal organs (cholecystitis, pylorospasm, spastic colitis, renal colic);
spasm of peripheral vessels (endarteritis);
spasm of cerebral vessels;
angina pectoris (as part of complex therapy);
bronchospasm.
Contraindications
Hypersensitivity, AV block, glaucoma, liver dysfunction, old age (risk of hyperthermia), childhood (up to 6 months).
Directions for use and doses
Pills
: inside adults
40-60 mg 3-4 times a day. Children aged 6 months and older. up to 2 years -
5 mg, 3-4 years
- 5-10 mg, 5-6 years
-10 mg, 7-9 years
- 10-15 mg, 10-14 years
- 15-20 mg 3-4 times a day.
Solution for injection:
SC, IM - 1-2 ml of 2% solution (20-40 mg) 2-4 times a day; IV, slowly 20 mg with preliminary dilution in 10-20 ml of 0.9% sodium chloride solution.
For elderly patients
the initial single dose is no more than 10 mg.
Suppositories: rectally, 20-40 mg 2-3 times a day (adults).
Side effect
Allergic reactions; AV block, ventricular extrasystole, decreased blood pressure, constipation, drowsiness, increased activity of liver transaminases, eosinophilia.
Overdose
Diplopia, weakness, drowsiness.
special instructions
It should be used with caution and in small doses in elderly and debilitated patients, as well as in patients with traumatic brain injury, impaired liver and kidney function, hypothyroidism, adrenal insufficiency, prostatic hypertrophy, supraventricular tachycardia and shock.
IV should be administered slowly and under the supervision of a physician.
During pregnancy and lactation, the safety and effectiveness of papaverine hydrochloride have not been established.
During the treatment period, alcohol consumption should be avoided.
Drug interactions
Reduces the effect of dopegyt. When smoking, the effectiveness decreases.
Storage conditions
Store in a place protected from light.
Formula: C20H21NO4, chemical name: 1-[(3,4-Dimethoxyphenyl)methyl]-6,7-dimethoxyisoquinoline (as hydrochloride).
Pharmacological group: organotropic drugs / cardiovascular drugs / vasodilators; organotropic agents/myotropic antispasmodics.
Pharmachologic effect: hypotensive, antispasmodic.
Pharmacological properties
Papaverine inhibits the enzyme phosphodiesterase and in the cell reduces the content of calcium ions and increases the content of cyclic 3,5"-AMP. Papaverine relaxes and reduces the tone of smooth muscles of blood vessels and internal organs (genitourinary, respiratory system, gastrointestinal tract). In large doses, papaverine slows down intracardiac conduction and reduces the excitability of the heart muscle. Papaverine is absorbed completely and quickly through any route of administration. In plasma, it is 90% protein bound. Papaverine passes through histohematic barriers easily and is biotransformed in the liver. The half-life of papaverine is 0.5–2 hours. Papaverine is excreted mainly in the form of metabolites by the kidneys.
Indications
Spasms of smooth muscles: cerebral vessels, heart vessels (in the complex treatment of angina pectoris), peripheral vessels (with endarteritis), bronchospasm, abdominal organs (pylorospasm, cholecystitis, renal colic, spastic colitis); for premedication as an additional drug.
Method of use of papaverine and dose
Orally (regardless of food intake), adults - 3–4 times a day, 40–60 mg. The highest single dose is 0.2 g; the maximum daily value is 0.6 g. Children from 6 months to 14 years - depending on age, 5–20 mg. Rectally for adults, 2-3 times a day, 1-2 suppositories (20-40 mg). Subcutaneously, intramuscularly: 2–4 times a day, 1–2 ml of a 2% solution (20–40 mg); intravenously, slowly - pre-dilute a 2% solution in 10–20 ml of isotonic sodium chloride solution, 1 ml (20 mg).
The effectiveness of papaverine decreases when smoking. During treatment with papaverine, it is necessary to avoid drinking alcohol.
Contraindications for use
Hypersensitivity, glaucoma, AV block, severe liver failure, age up to 6 months, old age (possible development of hyperthermia).
Restrictions on use
Shock conditions, conditions after traumatic brain injury, adrenal insufficiency, chronic renal failure, hypothyroidism, supraventricular tachycardia, prostatic hyperplasia.
Use during pregnancy and breastfeeding
The safety of using papaverine during pregnancy and breastfeeding has not been established.
Side effects of papaverine
Digestive system: increased activity of liver transaminases, constipation;
the cardiovascular system: ventricular extrasystole, AV block, decreased blood pressure;
others: eosinophilia, drowsiness, allergic reactions.
Interaction of papaverine with other substances
When used together with barbiturates, the antispasmodic effect of papaverine is enhanced. It is possible to enhance the hypotensive effect of papaverine when used simultaneously with tricyclic antidepressants, quinidine, reserpine, procainamide.
Overdose
In case of an overdose of papaverine, the following symptoms appear: weakness, visual impairment (double vision), decreased blood pressure, drowsiness. It is necessary to lavage the stomach, take activated charcoal, and maintain blood pressure.
Composition of solution per 2 ml:
Active substance – Papaverine hydrochloride – 40 mg.
Excipients: dl-methionine, disodium ethylenediaminetetraacetic acid, water.
Release characteristics
The release form of Papaverine in ampoules is cardboard boxes with glass ampoules, the solution content is the same.
pharmachologic effect
A drug that effectively eliminates contractions of the smooth muscles of all organs without exception. Strong antispasmodic. Inhibits phosphodiesterases, stimulates the accumulation of cyclic adenosine monophosphates (CAMP) in the cell, and reduces the level of calcium contained inside the cells.
- Combats increased tone, actively and effectively normalizing the condition of the smooth muscles of internal organs, various body systems - the gastrointestinal tract (gall bladder, stomach), respiratory (bronchi), cardiovascular, reproductive and urinary systems.
- Helps dilate arteries, improve and accelerate blood flow (and cerebral).
- Helps lower blood pressure (hypotensive effect).
- Average doses of the drug have little effect on the central nervous system.
High doses, in particular the active substance of the drug itself, are likely to develop a sedative effect, slow down intracardiac conduction and reduce myocardial excitability.
Pharmacodynamics and pharmacokinetics
Bioavailability of a drug, or the ability of a drug to reach the site of its main effect on the body, is 54%. Binds to plasma proteins - up to 90%.
It is quickly and evenly distributed throughout the body and easily overcomes histohematic barriers.
The process of breakdown and metabolization occurs in the liver, which does not allow the drug to accumulate in the body.
It is excreted along with urine, kidneys in the form of metabolites, and is completely eliminated from the blood during dialysis.
Indications for use of Papaverine
In most cases, Papaverine is used in the treatment of endarteritis, bronchospasm, pylorospasm, cholecystitis, angina pectoris and spastic colitis.
Papaverine shown
- Prevention of spasms of muscle fibers of smooth structures of internal organs (inflammation of the gallbladder, irritable bowel syndrome, stomach spasms), bronchi.
- Elimination of acute pain and during attacks of biliary and renal spasms.
- Treatment of potency disorders (erectile disorder of vascular origin).
- Spasms, vascular diseases, in particular obliterating endarteritis, involuntary contractions of the vessels of the brain and lower extremities.
- Angina pectoris (in organized therapy).
- It is practiced as an additional medication to prepare the patient for general anesthesia (reduces anxiety, enhances anesthetic drugs).
Contraindications
Papaverine is prohibited
- Children up to 6 months of age.
- People in a coma.
- For depressed respiratory conditions.
- In the presence of pathologies in the form of blockade (atrioventicular, disorder of the conductive function of the nerve impulse).
- Glaucoma of different types and stages.
- Age over 75 years.
- Fibroplastic induration of the penis (Peyronie).
- Liver failure in a severe stage.
- Individual intolerance to the components of the medication.
Side effects
The response to the use of Papaverine can be represented by several deviations:
- From the digestive system, possible: nausea, vomiting, bowel disorders (in particular constipation).
- From the cardiovascular system: decreased blood pressure, development of atrioventricular (AV) block, disturbance of the rhythm of ventricular contractions.
- Drowsiness.
- Increased sweating.
- Hyperactivity of liver enzyme proteins (transaminases).
Instructions for use of Papaverine
Papaverine in ampoules, instructions for use of which must be strictly followed, are released from points of sale only according to special recipes, with the seal of the medical institution and the signature of the doctor.
The prescription describes in detail the most important nuances of prescribing the medication. Compliance with which guarantees the effectiveness and efficiency of the drug.
Method and dosage
Papaverine in ampoules is used for intramuscular, intravenous and subcutaneous administration.
An adult is prescribed a dosage by the attending physician, in accordance with his state of health, age and clinical picture of concomitant diseases.
A single injection is prescribed from 1 to 2 ml (the solution is diluted in sodium chloride 0.9%), the next injection is given no less than 4 hours later.
The duration and dosage of treatment is prescribed by the doctor.
Intravenous administration is carried out extremely slowly and under the supervision of a physician.
For patients in the older age group, the dose of the drug administered should not exceed 10 mg.
Overdose
An overdose of the drug is only possible with incorrectly administered, exceeded, uncontrolled doses. An overdose is also possible in case of existing kidney and liver diseases.
Elimination of the consequences of an overdose includes a set of procedures
The drug is immediately discontinued, followed by surgical gastric lavage with milk and activated carbon, and supportive and symptomatic therapy is prescribed to eliminate the complications and disorders that have arisen.
There is no specific antidote for Papaverine.
When a persistent pathological (not associated with sexual intercourse) erection occurs, mainly as a result of the administration of the drug through the intracavernosal route, therapy is undertaken in exactly the same way by administering adrenaline and phenylephrine.
In extremely severe situations, bypass surgery on the vessels of the genital organ may be required.
Interaction with other drugs
Simultaneous use of Papaverine with anticholinergic drugs increases the effect of the latter.
Simultaneous use of Papaverine with alprostadil (in a variation of intracavernosal administration) increases the likelihood of developing priapism (persistent pathological erection).
Concomitant use of Papaverine with an antiparkinsonian drug reduces the effectiveness of levodopa.
Simultaneous use of Papaverine with drugs that lower blood pressure reduces the effectiveness of methyldopa.
Excellent results are obtained by the combined use of Papaverine, Analgin and Diphenhydramine in the form of an urgent injection for first aid in a variety of pathologies.
Papaverine in childhood
The use of Papaverine is prohibited for therapy in children under 6 months of age, as the likelihood of hyperthermia increases.
Papaverine in old age
Prescribed with careful caution and in small doses. Monitoring by a doctor must be systematic.
Persons over 60 years of age should definitely consult a doctor and should not self-medicate under any circumstances.
Papaverine during pregnancy and lactation
The use of Papaverine during pregnancy and lactation has not been fully studied; control studies have not been carried out.
Nevertheless, the drug is used in the treatment of pregnant women only under the strict supervision of a doctor. Prescribed in serious situations when there is no other treatment option. If the expected benefit exceeds the probable threats to the child.
Papaverine injections are acceptable during breastfeeding, but strictly under the supervision of specialists. Practice has not revealed the occurrence of side effects on infants.
Under no circumstances should you self-prescribe injections.
Storage conditions
The drug must be stored in a place protected from light and out of reach of children, and the temperature limit must be observed - no higher than 25 degrees Celsius.
Best before date
Storage of the drug is 24 months from the date of manufacture. After the expiration date indicated on the package, do not use for any purpose.
special instructions
Systematic monitoring by a physician and extreme caution in using Papaverine solution are required:
- During the post-traumatic period, in the presence of craniocerebral contusions and injuries.
- In case of chronic renal failure.
- In case of insufficient functioning of the adrenal glands.
- In the presence of a persistent lack of thyroid hormones (hypothyroidism).
- For non-cancerous, benign formations of the prostate.
- Disturbances in the conduction of electrical signals, impulses and heart rate (supraventricular tachycardia).
- Weakened patients.
The consumption of alcoholic beverages during Papaverine therapy should be stopped!
Analogs
There are a lot of analogues of Papaverine, basically they are not very different, the only difference is in the grams of the active substance and auxiliary components.
Almost identical in composition and process of exposure is Drotaverine Hydrochloride (solution).
Analogs are distinguished based on therapeutic effects
- No-spa in the form of a solution.
- Papaverina Bufus in the form of a solution.