Drotaverine (

INN Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...

, also known as drotaverin) is an

antispasmodic An antispasmodic (synonym: spasmolytic) is a pharmaceutical drug or other agent that suppresses muscle spasms. Smooth muscle spasm One type of antispasmodics is used for smooth muscle relaxation, especially in tubular organs of the gastrointest ...

drug, used to enhance

cervical dilation Cervical dilation (or cervical dilatation) is the opening of the cervix, the entrance to the uterus, during childbirth, miscarriage, induced abortion, or gynecological surgery. Cervical dilation may occur naturally, or may be induced surgically o ...

during

childbirth Childbirth, also known as labour and delivery, is the ending of pregnancy where one or more babies exits the internal environment of the mother via vaginal delivery or caesarean section. In 2019, there were about 140.11 million births glob ...

and to relieve smooth muscle spasms in gastrointestinal tract,

urinary system The urinary system, also known as the urinary tract or renal system, consists of the kidneys, ureters, bladder, and the urethra. The purpose of the urinary system is to eliminate waste from the body, regulate blood volume and blood pressure, c ...

, and

gall bladder In vertebrates, the gallbladder, also known as the cholecyst, is a small hollow organ where bile is stored and concentrated before it is released into the small intestine. In humans, the pear-shaped gallbladder lies beneath the liver, although ...

. It is structurally related to

papaverine Papaverine (Latin '' papaver'', "poppy") is an opium alkaloid antispasmodic drug, used primarily in the treatment of visceral spasms and vasospasms (especially those involving the intestines, heart, or brain), occasionally in the treatment of e ...

, and is a selective inhibitor of phosphodiesterase-4, and has no

anticholinergic Anticholinergics (anticholinergic agents) are substances that block the action of the neurotransmitter called acetylcholine (ACh) at synapses in the central and peripheral nervous system. These agents inhibit the parasympathetic nervous sys ...

effects. It is available in

Asia Asia (, ) is one of the world's most notable geographical regions, which is either considered a continent in its own right or a subcontinent of Eurasia, which shares the continental landmass of Afro-Eurasia with Africa. Asia covers an are ...

, India, Central and Eastern Europe under several brand names. Most known brand is ''No-Spa'' by Hungarian plant Chinoin (owned by

Sanofi Sanofi S.A. is a French multinational pharmaceutical and healthcare company headquartered in Paris, France. Originally, the corporation was established in 1973 and merged with Synthélabo in 1999 to form Sanofi-Synthélabo. In 2004, Sanofi-Syn ...

Pharmacodynamics

Drotaverine hydrochloride has a spasmolytic, myotropic,

vasodilation Vasodilation is the widening of blood vessels. It results from relaxation of smooth muscle cells within the vessel walls, in particular in the large veins, large arteries, and smaller arterioles. The process is the opposite of vasoconstrictio ...

hypotensive Hypotension is low blood pressure. Blood pressure is the force of blood pushing against the walls of the arteries as the heart pumps out blood. Blood pressure is indicated by two numbers, the systolic blood pressure (the top number) and the dia ...

action. Drotaverine decreases active ionized calcium supply binding to smooth muscle cells due to inhibition of phosphoesterase and

cAMP Camp may refer to: Outdoor accommodation and recreation * Campsite or campground, a recreational outdoor sleeping and eating site * a temporary settlement for nomads * Camp, a term used in New England, Northern Ontario and New Brunswick to descri ...

intracellular accumulation of

adenosine monophosphate Adenosine monophosphate (AMP), also known as 5'-adenylic acid, is a nucleotide. AMP consists of a phosphate group, the sugar ribose, and the nucleobase adenine; it is an ester of phosphoric acid and the nucleoside adenosine. As a substit ...

. It has an apparent and prolonged action on smooth muscles of internal organs and blood vessels and it moderately decreases

arterial blood pressure Blood pressure (BP) is the pressure of circulating blood against the walls of blood vessels. Most of this pressure results from the heart pumping blood through the circulatory system. When used without qualification, the term "blood pressure" r ...

, increases cardiac output (minute volume of heart), and have some

antiarrhythmic Antiarrhythmic agents, also known as cardiac dysrhythmia medications, are a group of pharmaceuticals that are used to suppress abnormally fast rhythms (Tachycardia, tachycardias), such as atrial fibrillation, supraventricular tachycardia and vent ...

potential. Drotaverine decreases

vascular tone Vascular resistance is the resistance that must be overcome to push blood through the circulatory system and create flow. The resistance offered by the systemic circulation is known as the systemic vascular resistance (SVR) or may sometimes be ca ...

of cerebral blood vessels and increases blood-filling. Practically, Drotaverine does not influence the autonomic nervous system and does not penetrate into the

central nervous system The central nervous system (CNS) is the part of the nervous system consisting primarily of the brain and spinal cord. The CNS is so named because the brain integrates the received information and coordinates and influences the activity of all p ...

Side effects

Possible side effects include: heating sensation, dizziness, headache (rarely), insomnia. May be observed: arrhythmia (rarely), hypotension, tachycardia, sweating, nausea. Overdose of Drotaverine potentially can cause atrioventricular (AV) block,

cardiac arrest Cardiac arrest is when the heart suddenly and unexpectedly stops beating. It is a medical emergency that, without immediate medical intervention, will result in sudden cardiac death within minutes. Cardiopulmonary resuscitation (CPR) and poss ...

, paralysis of respiratory system.

Counterfeits

Israel Israel (; he, יִשְׂרָאֵל, ; ar, إِسْرَائِيل, ), officially the State of Israel ( he, מְדִינַת יִשְׂרָאֵל, label=none, translit=Medīnat Yīsrāʾēl; ), is a country in Western Asia. It is situated ...

the product is known under the brand name "No-Spa" by the general publicNO-SPA (also pronounced as No-SHPA) trade mark registration decision 202248
Israeli patent and trade mark office, 11 July 2007 which did not receive a permit to be distributed by the

health ministry A health department or health ministry is a part of government which focuses on issues related to the general health of the citizenry. Subnational entities, such as states, counties and cities, often also operate a health department of their o ...

,Health Ministry: Fake drug had been smuggled
''NRG'', 11 March 2009 however due to high demand local medical counterfeiters have managed to smuggle No-Spa tablets over the years. In 2008, the Israeli health organization warned consumers against counterfeit No-SPA pills after a smuggler had been arrested at the Ben Gurion Airport with several thousand pills. In 2011, Israeli patent and trademark office declined the use of the No-SPA.

Risks

An article from 2013 described the effects from overdose (in a 19-year-old woman) as including vomiting, seizures and fatal cardiac toxicity. In 2016, the young Russian chess player

Ivan Bukavshin Ivan Alexandrovich Bukavshin (; 3 May 1995 – 12 January 2016) was a Russian chess player. He was awarded the title Grandmaster by FIDE in 2011. Bukavshin was three-time European champion in his age category. Chess career Bukavshin won three g ...

died of a massive overdose (or poisoning) of the drug, which was initially thought to be a stroke; dose detected in his blood was 17 mg/kg.Silence, lack of will, indifference
(Russian, Chess-News)

References

{{Drugs for functional gastrointestinal disorders Drugs acting on the gastrointestinal system and metabolism Norsalsolinol ethers Antispasmodics PDE4 inhibitors Sanofi