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Drotaverine

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2019-09-19
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Clinical Pharmacology

ATC code: A03A D02

Pharmacological properties:

Pharmacodynamics

Drotaverine is an isoquinoline derivative that has a potent antispasmodic effect on smooth muscle by inhibiting the enzyme phosphodiesterase (PDE). The enzyme phosphodiesterase is necessary for the hydrolysis of cyclic adenosine monophosphate (cAMP) to adenosine monophosphate (AMP). Inhibition of the phosphodiesterase enzyme leads to an increase in the concentration of cAMP; which triggers the following cascade reaction: high concentrations of cAMP activate cAMP dependent phosphorylation of myosin light chain kinase (MLCK). Phosphorylation of MLCC leads to a decrease in its affinity to the Ca2 + -calmodulin complex, as a result of which the inactivated form of MLCC supports muscle relaxation. cAMP also affects the cytosolic concentration of the Ca2 + ion, thanks to the stimulation of Ca2 + transport to the extracellular space and the sarcoplasmic reticulum. This drotaverine effect of decreasing the Ca2 + ion through cAMP explains the antagonistic effect of drotaverinate with respect to Ca2 +.

In vitro, Drotaverine inhibits the PDE IV isoenzyme without inhibiting the PDE III and PDE isoenzymes. Therefore, the effectiveness of drotaverine depends on the concentration of PDE IV in the tissues, the content of which varies in different tissues. PDE IV is most important for suppressing the contractile activity of smooth muscles, and therefore selective inhibition of PDE IV may be useful for treating hyperkinetic dyskinesias and various diseases involving the spastic state of the gastrointestinal tract.

Hydrolysis of cAMP in the myocardium and vascular smooth muscle occurs mainly with the help of PDE III isoenzyme, which explains the fact that with high spasmolytic activity in Drotaverine there are no serious side effects from the heart and vessels and pronounced effects on the cardiovascular system.

Drotaverine is effective in spasms of smooth muscles of both neurogenic and muscular origin. Regardless of the type of vegetative innervation, drotaverine relaxes the smooth muscles of the gastrointestinal tract, biliary tract, urinary system.

Pharmacokinetics

Absorption:

After oral administration, drotaverine is rapidly and completely absorbed. After the presystemic metabolism, 65% of the dose of drotaverine injected into the systemic circulation The maximum plasma concentration (Сmax) is reached in 45-60 minutes.

Distribution

In vitro, drotaverine has a high correlation in plasma transactions (95–98%), especially γ-albumin and β-globumin.

Drotaverin is evenly distributed in the tissues, penetrates into the smooth muscle cells. Does not penetrate the blood-brain barrier. Drotaverine and / or its metabolites may slightly penetrate the placental barrier.

Metabolism

In humans, drotaverine is almost completely stabilized in the liver by O-de-ethylation. Its metabolites are rapidly conjugated with glucuronic acid. The main metabolite is 4'-deethyldrotaverine, in addition to which 6-deethyldrotaverin and 4'-deethyldrotaveraldine have been identified.

Removal

In humans, a two-chamber mathematical model was used to assess the pharmacokinetics of drotaverine. The final half-life of plasma radioactivity was 16 hours.

Within 72 hours, drotaverine is almost completely excreted from the body. More than 50% of drotaverine is excreted by the kidneys and about 30% through the gastrointestinal tract (excretion into the bile). Drotaverine is mainly excreted as metabolites, unchanged drotaverine is not detected in the urine.

Indications

As an adjuvant therapy:

  • Spasms of smooth muscles of the gastrointestinal tract: gastric ulcer and duodenal ulcer, gastritis, cardia and pylorus spasms, enteritis, colitis, spasticity, colitis with constipation, and irritable bowel syndrome with meteorism after excluding diseases that manifest as acute stomach syndrome (appendix syndrome and acute stomach) , peritonitis, ulcer perforation, acute pancreatitis, etc.).
  • With tension headaches.
  • With dysmenorrhea.

Composition

Active ingredient: drotaverine hydrochloride - 40 mg;

excipients: magnesium stearate - 3 mg, talc - 4 mg, povidone - 6 mg,

Corn starch - 35 mg, lactose monohydrate - 52 mg.

Drotaverine is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
No-spa Hinoin Pharmaceutical and Chemical Product Plant Hungary pills
Doverin Anzhero-Sudzhensky HFZ Russia pills
Drotaverine Organica Russia pills
Drotaverine Pharmproject Russia pills
No-spa forte pills
No-spa Hinoin Pharmaceutical and Chemical Product Plant Hungary solution

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Drotaverine

Dosage and Administration

Adults

Usually the average daily dose in adults is 120-240 mg (the daily dose is divided into 2-3 doses). The maximum single dose is 80 mg. The maximum daily dose is 240 mg.

Children

no clinical studies with the use of drotaverine have been conducted with the participation of children.

In the case of the appointment of drotaverine children

- for children from 6 to 12 years, the maximum daily dose is 80 mg, divided into 2 doses.

- for children over 12 years old, the maximum daily dose is 160 mg divided into 2-4 doses. Duration of treatment without consulting a doctor

When taking the drug without consulting a doctor, the recommended duration of taking the drug is usually 1-2 days. If the pain syndrome does not diminish during this period, the patient should consult a doctor to clarify the diagnosis and, if necessary, change the therapy. In cases where drotaverine is used as an adjuvant therapy, the duration of treatment without consulting a doctor may be longer (2-3 days).

Method of performance evaluation

If a patient can easily self-diagnose the symptoms of his illness, as they are well known to him, then the effectiveness of the treatment, namely the disappearance of pain, is also easily measurable by the patient. If within a few hours after taking the maximum single dose there is a moderate decrease in pain or, the absence of a decrease in pain, or if the pain does not significantly decrease after taking the maximum daily dose, it is recommended to consult a doctor.

Adverse reactions

Below are the adverse reactions observed in clinical trials, divided by systems, organs, indicating the frequency of their occurrence in accordance with the following gradations: very frequent (≥ 10%), frequent (≥1%, <10); infrequent (≥0.1%, <1%); rare (≥0.01%, <0.1%) and very rare, including individual messages (<0.01%), unknown frequency (according to the available data, the frequency cannot be determined).

Since the cardiovascular system

Rare - increased heart rate, lower blood pressure.

The nervous system

Rare - headache, dizziness, insomnia.

From the gastrointestinal tract

Rare nausea, constipation.

The immune system

Rare - allergic reactions (angioedema, urticaria; rash, itching) (see section "Contraindications").

Contraindications

Hypersensitivity to the active substance or to any of the excipients of the drug

Severe hepatic or renal failure

Severe heart failure (low cardiac output syndrome)

Children's age up to 6 years

The period of breastfeeding (no clinical data).

Rare hereditary intolerance to galactose, lactase deficiency and glucose-galactose malabsorption syndrome (due to the presence of lactose in the formulation).

Carefully:

- With arterial hypotension.

- In children (lack of clinical experience).

- In pregnant women (see section "Pregnancy and lactation").

Drug interactions

With levodopa

Phosphodiesterase inhibitors, like papaverine, reduce the antiparkinsonian effect of levodopa. With the appointment of drotaverine simultaneously with levodopa may increase rigidity and tremor. With other antispasmodic agents, including m-anticholinergic blockers. Mutually increasing antispasmodic action.

Drugs significantly binding to plasma proteins (more than 80%)

Drotaverine significantly binds to plasma proteins, predominantly albumin,

γ and β-globulins (see Pharmacokinetics section). There is no data on the interaction of drotaverine. with drugs that significantly bind to plasma proteins, however, there is a hypothetical possibility of their interaction with drotaverine at the level of communication with the protein (displacing one of the drugs by the other because of the protein and increasing the concentration of the free fraction in the blood of the drug with a less strong connection with the protein), which is hypothetically may increase the risk of pharmacodynamic and / or toxic side effects of this drug.

Pregnancy and Lactation

Animal fertility experiments and retrospective studies of clinical data have shown that the use of drotaverine during pregnancy does not lead to either teratogenic or embryotoxic effects. However, the use of the drug is recommended only after carefully weighing the ratio of benefits and risks.

In the absence of the necessary clinical data in the period of lactation is not recommended.

Special instructions

No-spa® 40 mg pills contain 52 mg of lactose. This may cause gastrointestinal complaints in persons suffering from lactose intolerance. This form is unacceptable for patients suffering from a deficiency of lactose, galactosemia, or impaired glucose / galactose absorption syndrome (see the “Contraindications” section).

Influence on ability to steer the car and other mechanisms

When ingested in therapeutic doses, Drotaverine does not affect the ability to drive and perform work requiring increased attention. When any side effects are manifested, the question of driving a vehicle and working with mechanisms requires individual consideration. In the case of dizziness after taking the drug, you should avoid engaging in potentially hazardous activities, such as driving and working with mechanisms.

Overdosage

Data overdose of the drug is not available.

In case of overdose, patients should be under medical supervision and, if necessary, they should undergo symptomatic treatment aimed at maintaining the main body functions, including artificial induction of vomiting or gastric lavage.

  • Brand name: No-spa
  • Active ingredient: Drotaverine
  • Manufacturer: Hinoin Pharmaceutical and Chemical Product Plant

Studies and clinical trials of Drotaverine (Click to expand)

  1. Annelation of Drotaverine by p-Quinones to Form Hydroxyindolo- and Hydroxybenzindoloisoquinoline Derivatives.
  2. High-performance liquid chromatographic method for the determination of drotaverine in human plasma and urine
  3. Cathodic adsorptive stripping voltammetry of drotaverine hydrochloride and its determination in tablets and human urine by differential pulse voltammetry
  4. Modified high-performance liquid chromatographic method for analysis of drotaverine in human plasma
  5. Voltammetric behaviour of drotaverine hydrochloride in surfactant media and its enhancement determination in Tween-20
  6. Application of new membrane selective electrodes for the determination of drotaverine hydrochloride in tablets and plasma
  7. Spectrophotometric and spectrodensitometric determination of paracetamol and drotaverine HCl in combination
  8. Spectrophotometric determination of pipazethate HCl, dextromethorphan HBr and drotaverine HCl in their pharmaceutical preparations
  9. Simultaneous determination of Nifuroxazide and Drotaverine hydrochloride in pharmaceutical preparations by bivariate and multivariate spectral analysis
  10. The effect of drotaverine hydrochloride in acute colicky pain caused by renal and ureteric stones
  11. Transport properties and electroanalytical response characteristics of drotaverine ion-selective sensors
  12. A randomised controlled study comparing Drotaverine hydrochloride and Valethamate bromide in the augmentation of labour
  13. Carbon Paste Electrode for the Potentiometric Flow Injection Analysis of Drotaverine Hydrochloride in Serum and Urine
  14. Optimization of the Composition and Wet Granulation Technology of Drotaverine Hydrochloride Tablets
  15. Synthesis and blood coagulation properties of drotaverine derivatives
  16. Annelation of drotaverine byp-quinones to form hydroxyindolo- and hydroxybenzindoloisoquinoline derivatives
  17. Membrane drotaverine-selective electrodes based on tetraphenylborate derivatives: Electrochemical, adsorption, and transport properties and analytical application
  18. Voltammetric determination of papaverine and drotaverine
  19. Comparing hyoscine and drotaverine effects on colon in CT colonography
  20. Effects of Drotaverine Hydrochloride on Viability of Rat Cultured Cerebellar Granulocytes
  21. Qualitative and quantitative determination of drotaverine metabolites in rat bile
  22. The fate of Drotaverine — Acephyllinate+in rat and man I. Absorption, distribution and excretion in the rat
  23. The fate of Drotaverine-Acephyllinate in rat and man II. Human pharmacokinetics of Drotaverine-14C-Acephyllinate
  24. Pharmacokinetics and bioavailability of drotaverine in humans

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