Drotaverin

Drotaverine (also known under the trade name No-Spa) is a drug that is used to relieve spasms and contractions of the smooth muscles of human internal organs. Its main active ingredient is drotaverinium 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 the form of tablets or capsules. Dosage and regimen may vary depending on the individual needs of the patient and the doctor's recommendations.

Indications Drotaverina

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: This drug may be used to relieve pain associated with cramps in the gallbladder or bile ducts.
3. Menstrual cramps: Drotaverine helps soothe 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 bladder discomfort.
5. Symptoms of vascular spasms: Drotaverine may 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. The tablets are taken orally, usually with water, and come in a variety of strengths, allowing the optimal dose to be selected depending on the patient's individual needs.
2. Injection solution: For cases requiring a faster onset of action or when oral administration is not possible, drotaverine can be presented in the form of 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 are 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 the internal organs, thereby improving blood circulation and alleviating the symptoms of spasm.

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 from the gastrointestinal tract. After oral administration, maximum blood concentration is usually achieved within 1-2 hours.
2. Distribution: Drotaverine is widely distributed throughout the tissues of the body, including the central nervous system and organs in which 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 through the kidneys. The excreted metabolites are usually in conjugated form.
5. Half-terminal time (t½): The half-terminal time of drotaverine is about 4 hours. In older 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: Typically, drotaverine is taken 40-80 mg (1-2 tablets or capsules) up to three times a day. However, the exact dosage can 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 and can be taken with a small amount of water if desired.
2. Solution for injection: 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 Drotaverina during pregnancy

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

Data on the safety of drotaverine during pregnancy is limited. Although animal studies have shown no toxic effects on fetal development, data on the drug's use in pregnant women are limited and recommendations for its use vary.

A doctor can prescribe drotaverine to pregnant women only if the benefits of treatment outweigh the potential risks. He may also consider alternative treatments or other medications 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. Tachyarrhythmias (fast heart rate).
7. Angle-closure 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 Drotaverina

1. Drowsiness and dizziness: These symptoms may be most common when taking drotaverine. They may affect the ability to concentrate and carry out 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: Includes 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. Lower blood pressure: In some patients, drotaverine may cause a decrease in blood pressure, which may manifest as hypotension and possibly worsen existing problems with the cardiovascular system.
6. Dry mouth: This can also be a common side effect when taking drotaverine.
7. Tachycardia: Some patients may experience a rapid heartbeat or 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 arrhythmias.
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 increase their effect and increase the risk of side effects such as dry mouth or constipation.
2. Central-acting drugs: Drotaverine may enhance the effect of centrally acting drugs such as sedatives or analgesics. This may cause you to become more drowsy or slower to react.
3. Drugs that lower blood pressure: 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 enhance 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 through cytochrome P450: Drotaverine may affect the metabolism of other drugs metabolized through the hepatic enzyme cytochrome P450, which may lead to an increase or decrease in their concentration in the blood.