Drotaverine

Drotaverine (also known under the trade name No-Spa) is a drug used to relieve cramps and contractions of smooth muscles of the organs of the human internal systems. Its main active ingredient is drotaverine hydrochloride.

Drotaverine has the ability to relax the smooth muscles of the abdominal organs, blood vessels and urinary tract. It is often used to relieve symptoms of various conditions such as:

Drotaverine is usually taken orally in tablet or capsule form. Dosage and administration may vary depending on the individual patient's needs and the doctor's recommendations.

Indications Drotaverine

1. Abdominal pain: Drotaverine may be used to relieve pain associated with cramps and spasms in the stomach or intestines, such as colic.
2. Gallbladder and Bile Duct Pain: The drug can be used to relieve pain associated with spasms in the gallbladder or bile ducts.
3. Menstrual cramps: Drotaverine helps relieve menstrual cramps in women, which may reduce the intensity and duration of pain during menstruation.
4. Bladder symptoms: The drug can be used to relieve symptoms of cramps and discomfort in the bladder.
5. Symptoms of vascular spasms: Drotaverine can help relieve vascular spasms and improve blood circulation in cases where they cause painful symptoms.

Release form

1. Tablets: This is the most common form of drotaverine. Tablets are taken orally, usually with water, and come in a variety of dosages, allowing the optimal dose to be selected based on the individual needs of the patient.
2. Injection solution: For cases requiring a more rapid onset of action or when oral administration is not possible, drotaverine can be presented as an injection solution. The solution is usually administered intravenously or intramuscularly by medical personnel.

Pharmacodynamics

Drotaverine is a drug that belongs to the class of myotropic antispasmodics. Its pharmacodynamics is associated with its ability to relax the smooth muscles of blood vessels and internal organs, especially the intestines, urinary tract and uterus.

The drug acts by blocking phosphodiesterase, which leads to an increase in the level of cyclic adenosine monophosphate (cAMP) in smooth muscle cells. This, in turn, leads to relaxation of blood vessels and a decrease in the tone of the smooth muscles of internal organs, thereby improving blood supply and alleviating spasm symptoms.

Drotaverine also has an antispasmodic effect on blood vessels, which can lead to dilation of peripheral arteries and veins, improving blood circulation and reducing peripheral resistance.

Pharmacokinetics

1. Absorption: Drotaverine is absorbed in the gastrointestinal tract. After oral administration, maximum blood concentrations are usually reached within 1-2 hours.
2. Distribution: Drotaverine is widely distributed throughout the body tissues, including the central nervous system and organs where spasms occur. It can penetrate the blood-brain barrier.
3. Metabolism: Drotaverine is metabolized in the liver to form inactive metabolites. The main metabolites are N-oxide and N-demethylated drotaverine.
4. Excretion: Drotaverine and its metabolites are excreted from the body primarily via the kidneys. Excreted metabolites are usually in conjugated form.
5. Half-terminal time (t½): The half-terminal time of drotaverine is about 4 hours. In elderly patients it may be slightly prolonged.
6. Protein binding: Drotaverine binds to plasma proteins to a small extent (about 80%).

Dosing and administration

1. Tablets or capsules: Drotaverine is usually taken 40-80 mg (1-2 tablets or capsules) up to three times a day. However, the exact dosage may be adjusted by the doctor depending on the severity of symptoms and the individual needs of the patient. Tablets or capsules are usually taken before meals, with a small amount of water if desired.
2. Injection solution: In cases where oral administration is impossible or ineffective, drotaverine can be administered intravenously or intramuscularly by medical personnel. The dosage of the solution is usually 40-80 mg (1-2 ampoules) up to three times a day.

Use Drotaverine during pregnancy

Before using drotaverine (No-Spa) during pregnancy, you should always discuss it with your doctor. He or she should evaluate the benefits of the drug for the mother and the potential risks to the fetus.

There is limited safety data on the use of drotaverine during pregnancy. Although animal studies have not shown toxic effects on fetal development, there is limited data on the use of the drug in pregnant women, and recommendations for its use vary.

A doctor may prescribe drotaverine to pregnant women only if the benefits of treatment outweigh the potential risks. He or she may also consider alternative treatments or the use of other drugs with more extensive clinical experience during pregnancy.

Contraindications

1. Known individual intolerance to the drug.
2. Severe liver or kidney dysfunction.
3. Hypotension (low blood pressure).
4. Heart failure.
5. Acute bleeding in the gastrointestinal tract.
6. Tachyarrhythmia (rapid heart rate).
7. Closed-angle glaucoma.
8. Myasthenia gravis (a disease characterized by weakness and fatigue of skeletal muscles).
9. Atony (weakening) of the bladder or intestines.
10. Past myocardial infarction (especially in the acute stage).
11. Pregnancy (especially in the first trimester) and the period of breastfeeding (lactation).

Side effects Drotaverine

1. Drowsiness and dizziness: These symptoms may be the most common when taking drotaverine. They may affect the ability to concentrate and perform certain activities, such as driving.
2. Headache and weakness: Some patients may experience headaches or a feeling of weakness after taking drotaverine.
3. Gastrointestinal disorders: Include symptoms such as nausea, vomiting, diarrhea, or constipation.
4. Allergic reactions: In rare cases, drotaverine may cause allergic reactions such as skin rash, itching, or angioedema.
5. Decreased blood pressure: In some patients, drotaverine may cause a decrease in blood pressure, which may manifest as hypotension and may worsen existing cardiovascular problems.
6. Dry mouth: This can also be a common side effect when taking drotaverine.
7. Tachycardia: Some patients may experience rapid heartbeat or a feeling of palpitations after taking the drug.

Overdose

1. Increased side effects such as dizziness, weakness, headache, drowsiness, nausea, vomiting, decreased blood pressure.
2. Heart rhythm disorders such as tachycardia or arrhythmia.
3. Gastrointestinal disorders such as diarrhea or constipation.

Interactions with other drugs

1. Anticholinergic drugs: Concomitant use of drotaverine with other anticholinergic drugs, such as atropine or scopolamine, may enhance their effects and increase the risk of side effects such as dry mouth or constipation.
2. Centrally acting drugs: Drotaverine may enhance the effects of centrally acting drugs such as sedatives or analgesics. This may result in increased drowsiness or decreased reaction speed.
3. Blood pressure lowering drugs: Concomitant use of drotaverine with antihypertensive drugs such as beta-blockers or angiotensin-converting enzyme inhibitors (ACEIs) may enhance their hypotensive effect and lead to a decrease in blood pressure.
4. Drugs that prolong the QT interval: Drotaverine may increase the prolonging effect of drugs that affect the QT interval, such as antiarrhythmic drugs or macrolide antibiotics. This may increase the risk of developing cardiac arrhythmias.
5. Drugs metabolized via cytochrome P450: Drotaverine may affect the metabolism of other drugs metabolized via the liver enzyme cytochrome P450, which may lead to an increase or decrease in their concentration in the blood.