Introduction
No-Spa Injection 40 mg/2 ml is an antispasmodic drug that works by inhibiting phosphodiesterase-4 (PDE4). It is a benzylisoquinoline derivative that is structurally related to papaverine, although it displays more potent antispasmodic activities than papaverine. No-Spa Injection 40 mg/2 ml has been used in the symptomatic treatment of various spastic conditions, such as gastrointestinal diseases, biliary dyskinesia, and vasomotor diseases associated with smooth muscle spasms. It also has been investigated in dysmenorrhea, abortion, and augmentation of labour. More recently, drotaverine gained attention in the treatment of benign prostatic hyperplasia, parainfluenza, and avian influenza viruses.
No-Spa Injection 40 mg/2 ml is not approved by the FDA, European Medicines Agency, or Health Canada. It is approved for use in Thailand as oral tablets or intramuscular injections.
Uses
No-Spa Injection 40 mg/2 ml is a phosphodiesterase-4 inhibitor used to alleviate gastrointestinal and genitourinary smooth muscle spasms.
No-Spa Injection 40 mg/2 ml is used to alleviate gastrointestinal and genitourinary smooth muscle spasms, such as cholecystitis and gallbladder disorders.
Associated Conditions
Pharmacodynamics
No-Spa Injection 40 mg/2 ml 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. No-Spa Injection 40 mg/2 ml may have minor allosteric calcium channel blocking properties: in vitro, drotaverine behaves like voltage-dependent L-type calcium channel blockers.[A231624]
Mechanism of Action
No-Spa Injection 40 mg/2 ml 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.
Absorption
No-Spa Injection 40 mg/2 ml 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 Cmax was 292 ± 88 ng/mL. Mean AUC was 3251 ± 950 ng*h/mL. Mean Tmax was 1.9 ± 0.54 hours.
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.
Protein Binding
There is no information available.
Route of Elimination
No-Spa Injection 40 mg/2 ml is mainly eliminated via hepatic metabolism. About 67% of the drug is found in feces and 20% of the drug was eliminated with urine.
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.
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.
Toxicity
Oral LD50 is 540 mg/kg in rats and 350 mg/kg in mice. There is limited information on drotaverine overdose and toxicity.
Food Interactions
No interactions found.
