Summary

Drotaverine is a phosphodiesterase-4 inhibitor used to alleviate gastrointestinal and

genitourinary smooth muscle spasms.

Background
Drotaverine is an antispasmodic drug that works by inhibiting phosphodiesterase-4
(PDE4).5 It is a benzylisoquinoline derivative that is structurally related to papaverine,
although it displays more potent antispasmodic activities than papaverine. Drotaverine 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.1 It also has been investigated in dysmenorrhea, abortion, 3 and augmentation of
labour.4 More recently, drotaverine gained attention in the treatment of benign prostatic
hyperplasia, parainfluenza, and avian influenza viruses.5

Drotaverine 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.10

Indication
Drotaverine is used to alleviate gastrointestinal and genitourinary smooth muscle spasms,
such as cholecystitis and gallbladder disorders.

COMBIN
ED
PRODUC PATIENT
INDICATION T APPROVAL AGE CHARACTE
TYPE INDICATION DETAILS LEVEL GROUP RISTICS DOSE FORM
Treatment Spastic pain Prescription Injection, solution
of
Treatment Spastic pain caused by cholecysitis Prescription Injection, solution
of
Treatment Spastic pain of the gastrointestinal tract Prescription Tablet
of
Treatment Spastic pain caused by physical Prescription Tablet
of examination
Treatment Spastic pain caused by cystitis Prescription Tablet
of
Treatment Spastic pain caused by funicular Prescription Tablet
of nephritis
Treatment Spastic pain caused by cholecysitis Prescription Tablet
of
Treatment Spastic pain caused by gallbladder Prescription Tablet
of disorders
Treatment Muscle spasms Prescription
of
Treatment Abdominal pain caused by gall stones Prescription Tablet
of
Treatment Abdominal pain caused by kidney stones Prescription Tablet
of
Pharmacodynamics
Drotaverine 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.5 Drotaverine may have minor allosteric calcium channel blocking properties: in
vitro, drotaverine behaves like voltage-dependent L-type calcium channel blockers.8

Mechanism of action
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.5

TARGET ACTIONS ORGANISM

A3',5'-cyclic-AMP phosphodiesterase 4A inhibitor Humans
UVoltage-dependent L-type calcium channel inhibitor Humans

Route of elimination
Drotaverine is mainly eliminated via hepatic metabolism.1 About 67% of the drug is found in
feces and 20% of the drug was eliminated with urine.7

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.1
Generic Medicine Info

Indications and Dosage

Oral

Antispasmodic

Adult: 40-80 mg tid.

Child: 1-6 years 20-40 mg times aily; >6 years 40 mg tid.

Administration

May be taken with or without food.

Special Precautions

Patient with cardiac dysfunction. Renal and hepatic impairment. Children. Pregnancy and
lactation.

Adverse Reactions

Cardiac disorders: Palpitation.

Gastrointestinal disorders: Gastrointestinal disturbance, nausea, vomiting, constipation, dry

mouth.

Nervous system disorders: Vertigo, headache, dizziness.

Psychiatric disorders: Insomnia.

Vascular disorders: Orthostatic hypotension.

Patient Counseling Information

This drug may occasionally cause vertigo, if affected, do not drive or operate machinery.

Overdosage

Symptoms: Drowsiness, hypotension, and reduced gastric motility. Management:

Symptomatic and supportive treatment.

Drug Interactions

May attenuate the antiparkinsonian action of levodopa.

 Action

Description:

Mechanism of Action: Drotaverine is a musculotropic antispasmodic agent which inhibits

phosphodiesterase enzyme, causing increased cAMP levels thereby producing smooth
muscle relaxation.

Drotaverine indication
Drotaverine hydrochloride tablet has no cardiac toxic or hypotensive effects, which is why it can
be prescribed to patients in the following conditions associated with coronary insufficiency and
angina pectoris.
 Gastric spasm
 Intestinal spasm
 Pyloric spasm (spasm at the pyloric sphincter situated at the bottom of the stomach)
 Cholelithiasis (gallstones which are formed from concentrated bile)
 Spastic constipation
 Tenesmus in dysentery (Tenesmus is the feeling of passing stools, even though the
bowels are already empty)
 Dysmenorrhea (painful menstruation, typically associated with abdominal cramps)
Peripheral vascular disorders
Injection
 In adults, 2-4 ml injection may be given intramuscularly 1–3 times a day.
 No information about children's dosage.


Effect of drotaverine tablets on pregnancy, breastfeeding and driving

Drotaverine in pregnancy - Caution is to be advised when taking this drotaverine
hydrochloride during pregnancy. The patient is supposed to inform the prescribing doctor about
pregnancy or planning for one before using this drug.
Drotaverine in breastfeeding - Drotaverine hydrochloride use is not recommended while
breastfeeding.
 ‫ما هو دواء دروتافيرين‬
‫دروتافيرين هو دواء مضاد ولتشنج ‪ ،‬يستخدم وتعزيز تمدد عنق اورحم أثناء اوولدة ‪.‬هو مثبط انتقائي لنزيم فسفودايستراز‬
‫‪4-‬‬

‫العراض الجانبية لدروتافيرين‬

‫هذه الثار اوجانبية محتملة‪ ،‬ووكن قد ل تحدث دائما ‪.‬قد يكون بعض من الثار اوجانبية نادرة ووكنها خطيرة ‪.‬استشر طبيبك‬
‫إذا لحظت أي من الثار اوجانبية اوتاوية‪ ،‬ل سيما إذا كانت ل تزول ‪ :‬جفاف اوفم ‪ ،‬دوخة ‪ ،‬غثيان ‪ ،‬انتفاخ في اووجه ‪،‬‬
‫صعوبة في اوتنفس ‪ ،‬نزول اوشديد في ضغط اودم‪.‬‬

‫ما هي استخدامات دروتافيرين؟‬

‫يشار إويه وعلج تشنجات اوعضلت اوملساء في اومعدة واوقلب ‪.‬يتم استخدامه وتخفيف الوم اوناجم عن متلزمة اوقووون‬
‫اوعصبي واوصداع وفترات اوحيض ‪ ،‬ويستخدم أيضا وتخفيف تشنج عنق اورحم أثناء اومخاض‪.‬‬

‫ما هي موانع استخدام دروتافيرين؟‬

‫اوحساسية اومفرطة لحد مكونات اودواء‬

‫ما هي العراض الجانبية لدروتافيرين؟‬

‫هذه الثار اوجانبية محتملة‪ ،‬ووكن قد ل تحدث دائما ‪.‬قد يكون بعض من الثار اوجانبية نادرة ووكنها خطيرة ‪.‬استشر طبيبك‬
‫إذا لحظت أي من الثار اوجانبية اوتاوية‪ ،‬ل سيما إذا كانت ل تزول ‪ :‬جفاف اوفم ‪ ،‬دوخة ‪ ،‬غثيان ‪ ،‬انتفاخ في اووجه ‪،‬‬
‫صعوبة في اوتنفس ‪ ،‬نزول اوشديد في ضغط اودم‪.‬‬

‫ما هي احتياطات استخدام دروتافيرين؟‬

‫أخبر طبيبك قبل استخدام اودواء بوضعك اوصحي وضمان سلمتك اذا كنت تعاني من ‪ :‬أمراض اوقلب ‪ ،‬اوكلى اوكبد ‪،‬‬
‫اوحمل واورضاعة‪.‬‬

‫ما هي التداالت الدوائية لدروتافيرين؟‬

‫بعض الدوية يمكن أن تسبب تأثيرات غير مرغوبة أو خطيرة عند استخدامها مع اودواء أخبر طبيبك أو اوصيدلني قبل‬
‫بدء اوعلج اذا كنت تستخدم أي من ‪ :‬اتروبين ‪ ،‬ديكلوفيناك ‪ ،‬ويفودوبا ‪ ،‬ديازيبام‪.‬‬

‫ما هي جرعات دروتافيرين وطرق الستعمال؟‬

‫حسب إرشادات اوطبيب أو تناول قرص كل ‪ 8‬ساعات‪.‬‬

‫ما هي الشكال الدوائية لدروتافيرين؟‬

‫يأتي على شكل أقراص ‪ 40‬ملغم ‪ 80 ،‬ملغم ‪،‬أو على شكل محلول معلق ‪ ،‬أو على شكل إبر في اووريد أو عضلية‪.‬‬