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Drotaverine | CAS No: 14009-24-6 | GMP-certified suppliers
A medication that relieves gastrointestinal and genitourinary smooth muscle spasms, aiding conditions like cholecystitis and biliary dyskinesia by promoting muscle relaxation.
Therapeutic categories
Primary indications
- Drotaverine is used to alleviate gastrointestinal and genitourinary smooth muscle spasms, such as cholecystitis and gallbladder disorders
Product Snapshot
- Drotaverine is available as oral tablets and injectable solutions
- It is primarily indicated for the relief of gastrointestinal and genitourinary smooth muscle spasms
- The product is approved in some markets and remains investigational in others
Clinical Overview
Pharmacologically, drotaverine functions as a selective inhibitor of phosphodiesterase-4 (PDE4). PDE4 catalyzes the breakdown of cyclic adenosine monophosphate (cAMP), a secondary messenger involved in smooth muscle tone regulation. Inhibition of PDE4 by drotaverine elevates intracellular cAMP levels, leading to smooth muscle relaxation and alleviation of spasms. In vitro data also suggest minor allosteric effects on voltage-dependent L-type calcium channels, which may contribute to its pharmacodynamic profile. Additionally, drotaverine has demonstrated cytostatic effects against various human tumor cell lines, warranting further investigation into its potential anticancer properties.
Key ADME characteristics include oral and intramuscular administration routes, reflecting its use in clinical contexts such as Thailand where it has regulatory approval. Detailed pharmacokinetic parameters such as absorption rate, bioavailability, metabolism pathways, and elimination half-life are not extensively characterized in the public domain.
Safety considerations underscore the absence of regulatory approval by the FDA, EMA, or Health Canada, highlighting the necessity for cautious use guided by local regulatory frameworks. Reported safety profiles emphasize its tolerability; however, comprehensive toxicity data remain limited. Potential interactions related to its PDE4 inhibitory mechanism should be carefully evaluated, particularly in polypharmacy scenarios.
Notable marketed preparations of drotaverine are predominantly available as oral tablets and intramuscular injections within select Asian markets.
From an API sourcing perspective, quality assurance should focus on stringent control of impurities, consistent crystal form, and reproducible dissolution characteristics due to drotaverine’s influence on clinical efficacy. Suppliers must comply with relevant pharmacopeial standards and demonstrate robust manufacturing practice adherence to ensure reliable supply for pharmaceutical formulation and development.
Identification & chemistry
| Generic name | Drotaverine |
|---|---|
| Molecule type | Small molecule |
| CAS | 14009-24-6 |
| UNII | 98QS4N58TW |
| DrugBank ID | DB06751 |
Pharmacology
| Summary | Drotaverine selectively inhibits phosphodiesterase 4 (PDE4), increasing intracellular cAMP levels and promoting smooth muscle relaxation. It primarily targets PDE4A and exhibits additional activity as a voltage-dependent L-type calcium channel blocker. These pharmacodynamic effects underlie its use in relieving gastrointestinal and genitourinary smooth muscle spasms. |
|---|---|
| Mechanism of action | Drotaverine is a selective inhibitor of phosphodiesterase 4 (PDE4), which is an enzyme responsible for the degradation of cyclic adenosine monophosphate (cAMP). Inhibition of PDE4 leads to elevated levels of cAMP, leading to smooth muscle relaxation. Recent research showed that low levels of cAMP have been associated with brain tumorigenesis, leading to the investigation of PDE4 inhibitors as potential anticancer agents. |
| Pharmacodynamics | Drotaverine is an e spasmolytic agent with a relaxing effect on smooth muscles. It works to relieve visceral spasms and improve cervical dilation. _In vitro_, drotaverine mediated cytostatic effects on several human tumor cell lines and nonmalignant mouse fibroblasts. Drotaverine may have minor allosteric calcium channel blocking properties: _in vitro_, drotaverine behaves like voltage-dependent L-type calcium channel blockers. |
Targets
| Target | Organism | Actions |
|---|---|---|
| cAMP-specific 3',5'-cyclic phosphodiesterase 4A | Humans | inhibitor |
| Voltage-dependent L-type calcium channel | Humans | inhibitor |
ADME / PK
| Absorption | Drotaverine is not completely absorbed following oral administration and its bioavailability is highly variable. Following oral administration of a single 80 mg dose, the absolute bioavailability ranged between 24.5 and 91 % with a mean of 58.2 ± 18.2%. Mean C<sub>max</sub> was 292 ± 88 ng/mL. Mean AUC was 3251 ± 950 ng*h/mL. Mean T<sub>max</sub> was 1.9 ± 0.54 hours. |
|---|---|
| Half-life | Following oral administration of a single 80 mg dose, the mean half-life was 9.11 ± 1.29 hours. Following an intravenous dose of 80 mg, the mean half-life 9.33 ± 1.02 hours. |
| Protein binding | There is no information available. |
| Metabolism | Drotaverine is reported to undergo extensive hepatic metabolism, which is its main route of elimination. It may also undergo biliary excretion to form conjugated metabolites. Proposed metabolic pathways and metabolites are based on limited animal studies: in rats, the major identified metabolites of drotaverine are 4'-desethyl-drotaverine, 6-desethyl-drotaverine, drotaveraldine, and 4'-desethyl-drotaveraldine, all of which are glucuronidated in the bile. 4'-desethyl-drotaveraldine was the most predominant metabolite eliminated into the bile. |
| Route of elimination | Drotaverine is mainly eliminated via hepatic metabolism. About 67% of the drug is found in feces and 20% of the drug was eliminated with urine. |
| Volume of distribution | Following oral administration of a single 80 mg dose, the mean volume of distribution was 193 ± 48 L. Following an intravenous dose of 80 mg, the mean volume of distribution was 195 ± 48 L. |
| Clearance | Following oral administration of a single 80 mg dose, the mean renal clearance was 0.59 ± 0.18 mL/min. Following an intravenous dose of 80 mg, the mean renal clearance was 0.73 ± 0.29 mL/min. |
Formulation & handling
- Drotaverine is a small molecule with low water solubility and moderate lipophilicity, suitable for oral and injectable formulations.
- Oral forms are available as tablets and coated tablets, while injectable forms require solution preparation due to solubility constraints.
- Formulation should consider stability in both solid and aqueous solution states to maintain potency and ensure efficacy.
Regulatory status
Safety
| Toxicity | Oral LD<sub>50</sub> is 540 mg/kg in rats and 350 mg/kg in mice. There is limited information on drotaverine overdose and toxicity. |
|---|
- Oral LD50 values are 540 mg/kg in rats and 350 mg/kg in mice, indicating moderate acute toxicity
- Limited data are available regarding overdose and systemic toxicity profiles
- Standard industrial hygiene practices are recommended to minimize exposure during handling
Drotaverine is a type of Musculotropic spasmolytics
Musculotropic spasmolytics are a subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) used to alleviate muscle spasms and related conditions. These medications primarily target smooth muscles, such as those found in the gastrointestinal tract, urinary bladder, and blood vessels.
Musculotropic spasmolytics exert their therapeutic effects by acting on the muscarinic receptors in smooth muscle cells. By blocking the binding of acetylcholine to these receptors, they inhibit the excessive contractions that cause muscle spasms. This leads to muscle relaxation, pain relief, and improved functionality.
These APIs are commonly prescribed for various conditions characterized by muscle spasms, such as irritable bowel syndrome, urinary incontinence, and peripheral vascular diseases. They can also be employed as premedication for certain diagnostic procedures, such as endoscopies or cystoscopies, to reduce discomfort and facilitate examination.
Musculotropic spasmolytics encompass several well-known drugs, including butylscopolamine, hyoscine, and dicyclomine. These medications are available in different formulations, such as tablets, capsules, or injectables, allowing for convenient administration.
As with any pharmaceutical treatment, musculotropic spasmolytics may have potential side effects. These can include dry mouth, blurred vision, dizziness, constipation, and urinary retention. It is essential for healthcare professionals to carefully evaluate each patient's medical history and prescribe the appropriate dosage to minimize adverse effects.
In conclusion, musculotropic spasmolytics are a vital subclass of pharmaceutical APIs that effectively address muscle spasms. By selectively targeting smooth muscle cells and inhibiting excessive contractions, these medications provide relief and enhance the quality of life for individuals suffering from various conditions involving muscle spasms.
Drotaverine (Musculotropic spasmolytics), classified under Autonomic Nervous System Agents
Autonomic Nervous System Agents are a crucial category of pharmaceutical active ingredients (APIs) that target the autonomic nervous system (ANS). The ANS plays a vital role in regulating essential bodily functions such as heart rate, blood pressure, digestion, and respiratory rate. This category of pharmaceutical APIs encompasses a wide range of drugs designed to modulate the activity of the ANS.
One subcategory within Autonomic Nervous System Agents is the Sympathomimetic agents, which mimic the effects of the sympathetic nervous system. These drugs are often used to treat conditions such as asthma, nasal congestion, and hypotension by stimulating specific adrenergic receptors.
Conversely, Sympatholytic agents act to inhibit or block the sympathetic nervous system. They are employed to treat hypertension, anxiety, and certain cardiac conditions by reducing sympathetic activity.
Another subcategory is Parasympathomimetic agents, which mimic the effects of the parasympathetic nervous system. These drugs are commonly used to treat glaucoma, urinary retention, and certain gastrointestinal disorders by stimulating cholinergic receptors.
Parasympatholytic agents, on the other hand, act to block the parasympathetic nervous system. They find applications in the treatment of conditions such as overactive bladder and irritable bowel syndrome by inhibiting cholinergic receptors.
The Autonomic Nervous System Agents API category includes various drugs with distinct mechanisms of action that enable healthcare professionals to fine-tune the balance of the autonomic nervous system. By targeting specific receptors and pathways, these pharmaceutical APIs provide valuable therapeutic options for managing a wide range of medical conditions related to autonomic dysfunction.
Drotaverine API manufacturers & distributors
Compare qualified Drotaverine API suppliers worldwide. We currently have 4 companies offering Drotaverine API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Punjab Chemicals & Crop | Producer | India | India | CoA, GMP, WC | 5 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Suryakala Laboratories Pv... | Producer | India | India | CoA, ISO9001 | 6 products |
| Synthokem Labs | Producer | India | India | CoA, GMP, WC | 9 products |
When sending a request, specify which Drotaverine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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