Dot (Drotaverine)

Uses

Spastic conditions of the gastrointestinal tract, irritable bowel syndrome-

• Biliary colics and spastic conditions of the biliary tract: Cholecystolithiasis, cholecystitis, cholangitis.
• Renal colics and spastic conditions of the urogenital tract: Nephrolithiasis, ureterolithiasis, pyelitis, cystitis.
• Spastic conditions of the uterus: Dysmenorrhea, imminent abortion, uterine tetanus.

Dot (Drotaverine) is also used to associated treatment for these conditions: Abdominal Pain caused by Gall Stones, Abdominal Pain caused by Kidney Stones, Muscle Spasms, Spastic Pain, Spastic Pain caused by Cystitis, Spastic Pain caused by Funicular Nephritis, Spastic Pain caused by Gallbladder disorders, Spastic Pain caused by Physical Examination, Spastic Pain caused by cholecysitis, Spastic Pain of the Gastrointestinal Tract

How Dot (Drotaverine) works

Dot (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.

Dosage

Dot (Drotaverine) dosage

Oral-

• Adults: 1 to 2 tablets, 3 times daily
• Children (over 6 years): 1/2 to 1 tablet, 1-2 times daily.
• Children (1-6 years): 1/4 to 1/2 tablet, 1-2 times daily.

Injection-

• Adults: 1 to 2 ampoules, intramuscularly or subcutaneously, 1-3 times daily.
• For the management of acute stone colics: 1 or 2 ampoules by slow intravenous injection.

Side Effects

The common side effects are headache, dizziness, rhinitis, sinusitis, gastrointestinal upset, nausea, pharyngitis, edema and fatigue.

Toxicity

Oral LD₅₀ is 540 mg/kg in rats and 350 mg/kg in mice. There is limited information on drotaverine overdose and toxicity.

Precaution

Caution should be taken for patients suffering from liver and kidney disease.

Interaction

May attenuate the action of levodopa. Concurrent use of analgesics, antimuscarinics or benzodiazepines. Additive beneficial effect with concurrent use of analgesics, antimuscarinics or benzodiazepines.

Food Interaction

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.

Elimination Route

Dot (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_max was 292 ± 88 ng/mL. Mean AUC was 3251 ± 950 ng*h/mL. Mean T_max 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.

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.

Elimination Route

Dot (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.

Pregnancy & Breastfeeding use

As with most drugs, the use of Dot (Drotaverine) Hydrochloride should be avoided during pregnancy and lactation unless essential.

Contraindication

Dot (Drotaverine) is contraindicated in patients with known hypersensitivity to the products and its constituents.

Innovators Monograph

You find simplified version here Dot (Drotaverine)