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 accomm ...

, 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 gastrointestina ...

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 ...

during

childbirth Childbirth, also known as labour, parturition and delivery, is the completion of pregnancy, where one or more Fetus, fetuses exits the Womb, internal environment of the mother via vaginal delivery or caesarean section and becomes a newborn to ...

and to relieve

smooth muscle Smooth muscle is one of the three major types of vertebrate muscle tissue, the others being skeletal and cardiac muscle. It can also be found in invertebrates and is controlled by the autonomic nervous system. It is non- striated, so-called bec ...

spasms A spasm is a sudden involuntary contraction of a muscle, a group of muscles, or a hollow organ, such as the bladder. A spasmodic muscle contraction may be caused by many medical conditions, including dystonia. Most commonly, it is a muscle ...

in the

gastrointestinal tract The gastrointestinal tract (GI tract, digestive tract, alimentary canal) is the tract or passageway of the Digestion, digestive system that leads from the mouth to the anus. The tract is the largest of the body's systems, after the cardiovascula ...

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

, 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, althoug ...

. 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 ...

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

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

effects. It is available in

Asia Asia ( , ) is the largest continent in the world by both land area and population. It covers an area of more than 44 million square kilometres, about 30% of Earth's total land area and 8% of Earth's total surface area. The continent, which ...

Central and Eastern Europe Central and Eastern Europe is a geopolitical term encompassing the countries in Baltic region, Northeast Europe (primarily the Baltic states, Baltics), Central Europe (primarily the Visegrád Group), Eastern Europe, and Southeast Europe (primaril ...

(Poland, Hungary, Estonia, Latvia, Lithuania) under several brand names. A popular brand is ''No-Spa,'' owned by

Sanofi Sanofi S.A. is a French Multinational corporation, multinational pharmaceutical and healthcare company headquartered in Paris, France. The corporation was established in 1973 and merged with Synthélabo in 1999 to form Sanofi-Synthélabo. In 200 ...

). It is distributed by Sanofi as ''Но-Шпа'' (No-shpa) in Russia.

Pharmacodynamics

Drotaverine hydrochloride has a

spasmolytic Spasmolytic may refer to: * Antispasmodic, smooth muscle relaxant * A type of muscle relaxant A muscle relaxant is a drug that affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spa ...

, myotropic,

vasodilation Vasodilation, also known as vasorelaxation, 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. Blood vessel wa ...

hypotensive Hypotension, also known as low blood pressure, is a cardiovascular condition characterized by abnormally reduced blood pressure. Blood pressure is the force of blood pushing against the walls of the arteries as the heart pumps out blood and is ...

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

phosphodiesterase A phosphodiesterase (PDE) is an enzyme that breaks a phosphodiester bond. Usually, ''phosphodiesterase'' refers to cyclic nucleotide phosphodiesterases, which have great clinical significance and are described below. However, there are many oth ...

and intracellular accumulation of

cAMP Camp may refer to: Areas of confinement, imprisonment, or for execution * Concentration camp, an internment camp for political prisoners or politically targeted demographics, such as members of national or minority ethnic groups * Extermination ...

. 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 In cardiac physiology, cardiac output (CO), also known as heart output and often denoted by the symbols Q, \dot Q, or \dot Q_ , edited by Catherine E. Williamson, Phillip Bennett is the volumetric flow rate of the heart's pumping output: tha ...

(minute volume of heart), and has some

antiarrhythmic Antiarrhythmic agents, also known as cardiac dysrhythmia medications, are a class of drugs that are used to suppress abnormally fast rhythms (tachycardias), such as atrial fibrillation, supraventricular tachycardia and ventricular tachycardia. M ...

potential. Drotaverine decreases

vascular tone Vascular resistance is the resistance that must be overcome for blood to flow through the circulatory system. The resistance offered by the systemic circulation is known as the systemic vascular resistance or may sometimes be called by another ter ...

of cerebral blood vessels and increases blood-filling. Practically, Drotaverine does not influence the

autonomic nervous system The autonomic nervous system (ANS), sometimes called the visceral nervous system and formerly the vegetative nervous system, is a division of the nervous system that operates viscera, internal organs, smooth muscle and glands. The autonomic nervo ...

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, spinal cord and retina. The CNS is so named because the brain integrates the received information and coordinates and influences the activity o ...

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 (also known as sudden cardiac arrest CA is when the heart suddenly and unexpectedly stops beating. When the heart stops beating, blood cannot properly Circulatory system, circulate around the body and the blood flow to the ...

, paralysis of respiratory system.

Counterfeits

Israel Israel, officially the State of Israel, is a country in West Asia. It Borders of Israel, shares borders with Lebanon to the north, Syria to the north-east, Jordan to the east, Egypt to the south-west, and the Mediterranean Sea to the west. Isr ...

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 entity, Subnational entities, such as State (administrative division), states, county, counties an ...

,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 Ben Gurion International Airport , commonly known by the Hebrew language, Hebrew-language acronym (), is the main international airport of Israel. Situated on outskirts north of the city of Lod and directly south of the city of Or Yehuda, i ...

with several thousand pills. In 2011, the Israeli patent and trademark office declined the use of No-SPA.

Risks

An article from 2013 described the effects from overdose (in a 19-year-old female) 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 ...

died of a massive overdose (or poisoning) of the drug, which was initially thought to be a stroke; the 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