Drotaflex
Drotaflex Uses, Dosage, Side Effects, Food Interaction and all others data.
Drotaflex 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.
Drotaflex 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. Drotaflex may have minor allosteric calcium channel blocking properties: in vitro, drotaverine behaves like voltage-dependent L-type calcium channel blockers.[A231624]
| Trade Name | Drotaflex |
| Generic | Drotaverine |
| Drotaverine Other Names | Drotaverin, Drotaverina, Drotaverine, Drotaverinum |
| Type | Tablet, Injection |
| Formula | C24H31NO4 |
| Weight | Average: 397.5072 Monoisotopic: 397.225308485 |
| Protein binding | There is no information available. |
| Groups | Approved, Investigational |
| Therapeutic Class | Anticholinergics |
| Manufacturer | Invision Medi Sciences Pvt Ltd |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
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.
Drotaflex 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 Drotaflex works
Drotaflex 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
Drotaflex 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
No interactions found.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
Drotaflex 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.
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
Drotaflex 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 Drotaflex Hydrochloride should be avoided during pregnancy and lactation unless essential.
Contraindication
Drotaflex is contraindicated in patients with known hypersensitivity to the products and its constituents.
Innovators Monograph
You find simplified version here Drotaflex
FAQ
What is Drotaflex?
Drotaflex (INN, Drotaverine also known as drotaverin) is an antispasmodic drug, used to enhance cervical dilation during childbirth. It is structurally related to papaverine, is a selective inhibitor of phosphodiesterase 4, and has no anticholinergic effects.
What is Drotaflex used for?
Drotaflex is used to treat menstrual pain and abdominal pain. It relieves pain due to smooth muscle spasms, such as menstrual pain, kidney stone pain, biliary stone pain, and gastrointestinal colic pain.
Is Drotaflex a painkiller?
It relieves pain due to smooth muscle spasm like menstrual pain, pain due to kidney stone, pain due to biliary stone and gastro-intestinal colicky pain. Drotaflex is an anti-spasmodic medicine which relieves contractions (spasms) associated with smooth muscles in the abdomen.
Is Drotaflex safe?
Drotaflex is an effective and safe pharmaceutical agent in the management of recurrent abdominal pain.
How to take Drotaflex?
Take Drotaflex in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Drotaflex Tablet may be taken with or without food, but it is better to take it at a fixed time.
Is Drotaflex safe in pregnancy?
Due to the lack of safety information, Drotaflex should not be used during pregnancy until prescribed.
What are the side effects of Drotaflex?
Drotaflex side effects are:
- Nausea
- Vomiting
- Dry mouth
- Change in pulse rate
- Dizziness
- Headache
- Difficulty in breathing
- Skin allergic
- Swelling of face, lips, eyelids and tongue
- Fall in Blood pressure
- Vertigo
- Constipation
- Sleep disorders
- Dermatitis
What is the indication of Drotaflex?
The indications to Drotaflex administration include contractions of the biliary ducts, urinary tract, and digestive smooth muscles; also dysmenorrhea and imminent abortion.
Is Drotaflex a steroid?
Drotaflex is an anti-spasmodic medicine which relieves contractions (spasms) associated with smooth muscles in the abdomen.
Is Drotaflex safe in children?
Drotaflex is an effective and safe pharmaceutical agent in the management of recurrent abdominal pain in children.
How long does Drotaflex take to work?
You should take Drotaflex for the treatment as prescribed by the doctor. However, if there is no improvement in pain after seven days, consult your doctor.
Why Drotaflex is given in pregnancy?
It was concluded that Drotaflex is highly effective in reducing the duration of active phase of labour by hastening cervical dilatation, more effective when given in more dilated cervix than with less dilatation and more effective in multigravida than in primigravida.
Why Drotaflex is given?
Drotaflex is an antispasmodic medicine. It is used in the treatment of menstrual pain and abdominal pain. It provides relief from pain due to smooth muscle spasm like menstrual pain, pain due to kidney stones, pain due to biliary stone and gastrointestinal colicky pain.
