Allopathy
Prescription Required
DCGI (Drugs Controller General of India)
Schedule H
Drotaverine is a Phosphodiesterase-4 inhibitor belonging to Antispasmodic drug.
The Mean Cmax was found to be 292 ± 88 ng/mL with Mean AUC of 3251 ± 950 ng*h/mL. Mean Tmax of Drotaverine was found to be 1.9 ± 0.54 hours. 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. 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.
Drotaverine shows common side effects like Fainting, nausea, vomiting and dry mouth.
Drotaverine is available in the form of tablet, capsule, syrup, suspension, and injection.
Drotaverine is available in India, China, Philippines, Malaysia, Australia, Singapore, France, and Spain.
Drotaverine is an Antispasmodic agent belonging to the class Phosphodiesterase-4 inhibitor.
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.
The Onset and Duration of action of Drotaverine is not clinically established.
The time to reach peak plasma concentrations was 1.9 ± 0.54 hours.
Drotaverine is available in the form of oral tablet, capsule, syrup, suspension, and injection.
Drotaverine is a pain-relieving medicine. It is used to relieve pain due to various conditions like muscle spasms, menstruation, kidney stones, gall stones, irritable bowel syndrome, and headaches. It is also used to reduce labor pains. It works by reducing the contraction of smooth muscles.
Drotaverine is a Phosphodiesterase-4 inhibitor belonging to Antispasmodic drug.
Drotaverine has antispasmodic effect mediated via inhibition of phosphodiesterase-IV, specific for smooth muscle. It has a rapid and direct action on the smooth muscle. It acts to correct cyclic AMP and Ca imbalance at the spastic site, thereby relieving smooth muscle spasm and pain.
Drotaverine is approved for use in the following clinical indications
- Antispasmodic
- Drotaverine is used to alleviate gastrointestinal and genitourinary smooth muscle spasms, such as cholecystitis and gallbladder disorders.
- Antispasmodic
Adult: 40-80 mg three times a day.
Child: 1-6 years: 20 mg 3-4 times daily; >6 year: 40 mg three times a day.
Drotaverine is available in various strengths as 40mg and 80mg.
Drotaverine is available in the form of tablet, capsule, syrup, suspension, and injection.
Drotaverine is contraindicated in patients with
- Allergy
Avoid taking Drotaverine if you are allergic to it. Serious allergic reactions to this medicine are rare. However, seek immediate medical attention if you notice any symptoms such as skin rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, breathing difficulty, etc.
- Sever liver/kidney diseases
Drotaverine is not recommended for use if you have severe liver or kidney problems as this medicine may worsen your condition.
- Heart Failure
Drotaverine is not recommended for use if you have heart problems characterized by insufficient blood flow.
- Liver disease
Use Drotaverine with caution if you have liver problems as it may lead to undesirable effects. Your doctor may suggest tests to closely monitor your liver function if necessary while taking this medicine.
- Kidney disease
Use Drotaverine with caution if you have kidney problems as it may lead to undesirable effects due to the accumulation of this medicine.
- Heart disease
Drotaverine can cause a fall in blood pressure levels. Hence, use this medicine with caution if you have disorders of the heart and blood vessels.
Breast Feeding Warning
Drotaverine is not recommended for use if you are breastfeeding.
Pregnancy Warning
Drotaverine is not recommended for use in your pregnancy.
Common
- Nausea and vomiting, Dry mouth, Change in pulse rate, Dizziness, Headache, Difficulty in breathing, Allergic skin reaction, Swelling of face, lips, eyelids, tongue, hands and feet, Fall in blood pressure, Hypoesthesia (Decreased sense of touch or sensation), Anaemia, Gastroesophageal reflux disease (Frequent acid reflexes from stomach), Decreased urine output.
Levodopa: May attenuate the action of levodopa.
The common side effects of Drotaverine include the following
Common side effects
- Nausea and vomiting, Dry mouth, change in pulse rate, Dizziness, Headache, Difficulty in breathing, Allergic skin reaction, swelling of face, lips, eyelids, tongue, hands and feet, fall in blood pressure, Hypoesthesia (Decreased sense of touch or sensation), Anaemia, Gastroesophageal reflux disease (Frequent acid reflexes from stomach), Decreased urine output.
- Pregnancy
Pregnancy Category
Drotaverine is not recommended for use in your pregnancy.
- Nursing Mothers
Drotaverine is not recommended for use if you are breastfeeding.
- Pediatric Use
Drotaverine hydrochloride is an effective and safe pharmaceutical agent in the management of recurrent abdominal pain in children.
- Pharmacodynamic
Drotaverine is an 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.
- Pharmacokinetics
Absorption
Following oral administration of a single 80 mg dose, the absolute bioavailability of Drotaverine ranged between 24.5 and 91 % with a mean of 58.2 ± 18.2%. Mean Cmax was found to be 292 ± 88 ng/mL with Mean AUC of 3251 ± 950 ng*h/mL. Mean Tmax of Drotaverine was found to be 1.9 ± 0.54 hours.
Distribution
Mean volume of distribution of Drotaverine was found to be 193 ± 48 L. Following an intravenous dose of 80 mg, the mean volume of distribution was 195 ± 48 L.
Metabolism and Excretion
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. 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.
- Romics I, Molnar DL, Timberg G, Mrklic B, Jelakovic B, Köszegi G, Blaskó G. The effect of drotaverine hydrochloride in acute colicky pain caused by renal and ureteric stones. BJU international. 2003 Jul;92(1):92-6.
- Dash A, Maiti R, Akantappa Bandakkanavar TK, Arora P. Intramuscular drotaverine and diclofenac in acute renal colic: a comparative study of analgesic efficacy and safety. Pain Medicine. 2012 Mar 1;13(3):466-71.
- Narang M, Shah D, Akhtar H. Efficacy and safety of drotaverine hydrochloride in children with recurrent abdominal pain: a randomized placebo controlled trial. Indian pediatrics. 2015 Oct;52:847-51.
- https://www.medindia.net/doctors/drug_information/drotaverine.htm#Sideeffects
- https://go.drugbank.com/drugs/DB06751
- https://www.medindia.net/doctors/drug_information/drotaverine.htm
- https://www.drugs.com/international/drotaverine.html
