Drotaverine forte

Drotaverine forte Uses, Dosage, Side Effects, Food Interaction and all others data.

Drotaverine forte 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 forte 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 forte may have minor allosteric calcium channel blocking properties: in vitro, drotaverine behaves like voltage-dependent L-type calcium channel blockers.[A231624]

Trade Name Drotaverine forte
Generic Drotaverine
Drotaverine Other Names Drotaverin, Drotaverina, Drotaverine, Drotaverinum
Type
Formula C24H31NO4
Weight Average: 397.5072
Monoisotopic: 397.225308485
Protein binding

There is no information available.

Groups Approved, Investigational
Therapeutic Class Anticholinergics
Manufacturer
Available Country Russia
Last Updated: September 19, 2023 at 7:00 am
Drotaverine forte
Drotaverine forte

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.

Drotaverine forte 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 Drotaverine forte works

Drotaverine forte 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

Drotaverine forte 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

Drotaverine forte 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

Drotaverine forte 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 Drotaverine forte Hydrochloride should be avoided during pregnancy and lactation unless essential.

Contraindication

Drotaverine forte is contraindicated in patients with known hypersensitivity to the products and its constituents.

Innovators Monograph

You find simplified version here Drotaverine forte

FAQ

What is Drotaverine forte?

Drotaverine forte (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 Drotaverine forte used for?

Drotaverine forte 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 Drotaverine forte 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. Drotaverine forte is an anti-spasmodic medicine which relieves contractions (spasms) associated with smooth muscles in the abdomen.

Is Drotaverine forte safe?

Drotaverine forte is an effective and safe pharmaceutical agent in the management of recurrent abdominal pain.

How to take Drotaverine forte?

Take Drotaverine forte in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Drotaverine forte Tablet may be taken with or without food, but it is better to take it at a fixed time.

Is Drotaverine forte safe in pregnancy?

Due to the lack of safety information, Drotaverine forte should not be used during pregnancy until prescribed.

What are the side effects of Drotaverine forte?

Drotaverine forte 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 Drotaverine forte?

The indications to Drotaverine forte administration include contractions of the biliary ducts, urinary tract, and digestive smooth muscles; also dysmenorrhea and imminent abortion.

Is Drotaverine forte a steroid?

Drotaverine forte is an anti-spasmodic medicine which relieves contractions (spasms) associated with smooth muscles in the abdomen.

Is Drotaverine forte safe in children?

Drotaverine forte is an effective and safe pharmaceutical agent in the management of recurrent abdominal pain in children.

How long does Drotaverine forte take to work?

You should take Drotaverine forte for the treatment as prescribed by the doctor. However, if there is no improvement in pain after seven days, consult your doctor.

Why Drotaverine forte is given in pregnancy?

It was concluded that Drotaverine forte 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 Drotaverine forte is given?

Drotaverine forte 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.

*** Taking medicines without doctor's advice can cause long-term problems.
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