No-Shpa: instructions for use

No-Spa: instructions for use

No-shpa is, perhaps, the first most popular medicine for spasms of smooth muscles of quick action. The range of application of this antispasmodic is extremely wide and includes:

  • Symptomatic therapy in which the use of No-shpa is carried out to eliminate spasm as a symptom that does not carry changes in the clinical picture of the disease;
  • Etiotropic treatment is therapy aimed at eliminating the cause of the disease. In this case, the cause is directly a spasm of smooth muscle tissue;
  • Pre-medication as a procedure prior to some medical procedures.

The indisputable advantage of No-shpa, which has provided the drug with extreme demand, is a relatively small number of side effects compared to, for example, anticholinergic antispasmodics.

Drotaverinum or No-Shpa, what is the difference?

Sooner or later, most people are faced with the need to take a small yellow pill in order to quickly alleviate the unpleasant state of spasm. The active ingredient in No-Shpa is drotaverine. This name many have heard more than once, it is the most common analogue of No-shpa found in pharmacies. What are the differences between these two drugs and are they available?

A person buys one drug, then buys another. After careful familiarization with the instructions for the drugs, it becomes clear that there are no differences in pharmacological action, active substances and effects on the body. Then for what reason, No-shpa is more expensive and is there any point in buying it, and not Drotaverine, which is more affordable?

No-shpa is the registered trade name of the drug based on drotaverine. To obtain a patent for the production of a medicine, it is necessary to carry out many pharmacological tests, including the quality of the materials used in production and the complete safety of the drug in therapy. With all the costs of clinical trials, inspections and various certifications, patent a drug is very expensive for the manufacturer. Therefore, in the production of a patented drug in its value lies the percentage of the patent.

Drotaverine is a generic. This is an international name, it can be used for the production of drotaverine-containing drugs by any pharmaceutical company, without buying an expensive patent. Therefore, of course, the cost of drotaverine will be lower. But before going to the pharmacy, it is worth bearing in mind that less stringent control and safety requirements are imposed on generics.

As a result, when buying a generic, the consumer hopes for the good faith of the manufacturer. However, this does not mean that generics have more pronounced side effects or in any way harm health.

Physico-chemical properties, composition, cost

No-shpa has two forms of release: tablets for oral administration and vials for injection intravenously and intramuscularly.

Release form Main substance Excipients Physico-chemical characteristics
Tablets:
6, 20, 24 pcs. – in aluminum blisters.
60, 100 pcs. – in polypilene bottles.
Packs made of cardboard.
Drotaverine hydrochloride in an amount of 40 mg / tablet Magnesium stearate – 3 mg,
corn starch – 35 mg,
Talc – 4 mg,
Povidone – 6 mg,
lactose monohydrate – 52 mg
Round yellow tablets with a green tinge. Biconvex shape, labeled “spa” on one side
Solution for injection:
In dark glass ampoules with a notch to indicate the place of the ampoule break – 2 ml.
In a package of 5/25 ampoules. Bundles of cardboard.
Drotaverine hydrochloride in an amount of 40 mg / vial or 20 mg / ml Sodium bisulfite – 2 mg,
96% ethanol – 132 mg,
water for injection – up to 2 ml
Clear yellowish green solution

Pharmacological action

Drotaverine hydrochloride is an isoquinoline derivative. This substance is a very potent antispasmodic, targeting smooth muscles.

Drotaverine has a therapeutic effect due to its ability to inhibit the activity of the phosphodiesterase type 4 enzyme (FDA4). This enzyme catalyzes the decomposition reaction of cAMP (cyclic adenosine monophosphate) to its non-cyclic AMP derivative. As a result of the deactivation of the enzyme, an increase in the concentration of cAMP occurs. In the cell, this substance is a signaling molecule, its accumulation leads to the launch of a cascade of chemical reactions. Phosphorylation of myosin light chain kinase (MLCM), an enzyme responsible for the activation of the contractile cycle in smooth muscle cells, occurs. Along the way, cAMP stimulates the release of Ca2 + ions from the cell to the extracellular space. As a result, the phosphorylated form of CLPC becomes less affinity for the calcium-calmodulin complex, which is the triggering point for muscle relaxation.

The content of different types of phosphodiesterase varies in different types of tissues, therefore, the effect of drotaverine on different tissues has variable efficacy. The effect solely on type 4 PDE provides the drug with a minimal amount of side effects from the heart muscle. In the muscle cells of the blood vessels and the heart, PDE type 3 is localized.

Reducing the activity of PDE 4 type also contributes to the change in the susceptibility of uterine cells to the hormonal effects of oxytocin. Because of this, drotaverin can reduce the tone of the uterus, preventing a premature generic process.

Drotaverin stimulates the dehydration of muscle tissue, reduces the appearance of inflammation. The relaxation of the smooth muscles of the blood vessels contributes to a better blood supply to the internal organs. The substance provides restoration of the natural peristalsis of the digestive organs and can relieve pain.
With its pronounced effects on the body, drotaverine does not lubricate the clinical picture of the disease and does not affect the mechanisms of the body’s sensitivity to pain as it occurs as a result of taking analgesics, for example.

The drug effectively deals with spasms of smooth muscles of any etiology. Especially often used in medicine for painful contractions of the walls of the digestive tract, urinary and bile ducts

Pharmacokinetics of the drug

After taking drotaverine in tablet form, the substance is effectively absorbed in the gastrointestinal tract, after primary metabolism, about 65% of the consumed dose enters the systemic circulation. After 45-60 minutes, the concentration of drotaverin in the blood reaches maximum values. The substance is able to pass through the placental barrier only in small quantities. The blood-brain barrier does not cross the drug, and therefore does not affect the nervous system.

With the introduction of intravenous drotaverine, the effect occurs much faster, reaching maximum values ​​in half an hour after the injection. Metabolism occurs predominantly in the liver. Then in the form of metabolites, the drug is excreted from the body. Half of Drotaverine is excreted by the kidneys, another 30% with the help of the gastrointestinal tract. Complete elimination of the substance occurs within 72 hours.

Indications for use

According to the instructions for the drug, the administration of No-Shpa is recommended under the following conditions:

  • Spasmodic conditions accompanying gallbladder pathology of various etiologies;
  • Spasms of smooth muscle tissue in case of urinary system diseases, inflammatory and infectious;

In addition to the above situations, No-Shpa is also used as a symptomatic treatment to alleviate a person’s general condition in the following conditions:

Contraindications

Reception of No-Shpa is contraindicated for acute cardiac, renal or hepatic types of insufficiency, as well as hypersensitivity to the drug components.
The drug in the form of tablets can not be taken to children under 6 years old, injection of No-Shpa is prescribed only to persons older than 18 years.
Full or partial intolerance to lactose and / or galactose, as well as violations of the adsorption of galactose / glucose are also a contraindication to the appointment of No-Shpa in tablets. If you have a hypersensitivity to sodium bisulphite, then you should refrain from injecting this drug and treat it with drugs in the form of tablets.
Due to the low level of knowledge about the penetration of drotaverine into breast milk, No-shpa is not recommended for women who are breastfeeding.

Special Instructions

Due to the insufficient number of clinical studies, caution should be taken when taking drotaverine in children and women during pregnancy.
People with low blood pressure are advised to take this drug with caution in order to avoid a life threatening drop in blood pressure. When administered intravenously, the patient is recommended to take a horizontal position. After applying the No-Shpa solution, it is not recommended to work with mechanisms and drive a car.

No-shpa during pregnancy

No-Spa: instructions for use
Photo: Rocketclips, Inc. / Shutterstock.com

In the early stages of pregnancy, the use of No-Shpa is often recommended to reduce the level of uterine tone, helping to reduce the threat of spontaneous abortion.
Studies on animals and clinical trials of the drug indicate that drotaverin does not cause toxic and teratogenic changes in the fetus. However, it is proved that the substance is able to penetrate to a certain extent through the blood-brain barrier. Therefore, before applying No-shpa in the first trimester of pregnancy, it is imperative that you discuss this issue with your doctor and evaluate all the benefits and possible risks to the life and health of the fetus and mother.
In the later stages of childbearing and in the period of labor, taking the drug is contraindicated, since bleeding may occur due to hypotonia of the uterine tissues.

Dosage and administration

The duration of therapy is determined individually. Self-medication without a prescription is possible for no more than 3 days.

Take pills

The drug is recommended to be taken an hour after a meal, with a small amount of water.

  • Children 6-12 years old: 1 tablet 1-2 times a day. The maximum daily dose is 80 mg.
  • Children over 12 years old: 1 tablet 1-4 times a day, or 2 tablets 1-2 times a day. The maximum daily dose is 160 mg.
  • Adults: 1-2 tablets 2-3 times a day. The maximum daily dose is 240 mg.

Solution Injections

The introduction of a solution of Drotaverine is contraindicated for persons under the age of 18 years. For adults, the maximum dose of the substance in the solution is the same as in tablets – 240 mg. The introduction is carried out in 1-3 doses.
Efficacy and dosage within the maximum daily amount are determined individually based on the sensations of relieving the patient and the severity of pain symptoms.

Side Effects

Side effects on the body when taking drotaverine rarely develop (frequency of occurrence ≥0.01%, but <0.1%) and include the following reactions:

  • Headache, dizziness, insomnia;
  • Heartbeat, low blood pressure;
  • Nausea, constipation;
  • Allergic reactions of varying severity, up to anaphylactic shock;
  • Swelling of the tissues in the area of ​​the injection.
No-Spa: instructions for use
Photo: Elnur / Shutterstock.com

Overdose

Overdose with Drotaverine can lead to heart rhythm disturbances of various degrees, up to a complete cardiac arrest caused by a complete blockage of the bundle of the His bundle.
Neutralization of the effects of an overdose of the drug should be carried out under the supervision of a physician in a medical institution and include the full range of necessary symptomatic therapy.

Interaction with other drugs

The use of No-shpa can weaken the anti-Parkinsonian effect of the drug Ledopa. With the introduction of an injection of No-Shpa in combination with morphine, an increase in the antispasmodic activity of the drug was observed, when combined with antidepressants of the tricyclic series – the risk of arterial hypotension. An increase in antispasmodic activity is also observed when other antispasmodics are taken simultaneously.

Analogs

The No-shpa drug analogs include No-shpa Forte, Drotaverin, Drotaverin Forte, Spazmonet, Spasmol.

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