Clinical data | |
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Trade names | No-Spa, Doverin |
AHFS/Drugs.com | International Drug Names |
Routes of administration | Oral, intravenous, intramuscular |
ATC code | |
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Legal status | |
Pharmacokinetic data | |
Bioavailability | Highly variable (~65%), peak at 45–60 min |
Protein binding | 95–98% |
Metabolism | Hepatic |
Elimination half-life | 7–16 hours |
Excretion | >50% in urine and ~30% in bile [1] |
Identifiers | |
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CAS Number | |
PubChem CID | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.110.916 |
Chemical and physical data | |
Formula | C24H31NO4 |
Molar mass | 397.515 g·mol−1 |
3D model (JSmol) | |
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Drotaverine (INN, also known as drotaverin) is an antispasmodic drug, used to enhance cervical dilation during childbirth and to relieve smooth muscle spasms in the gastrointestinal tract, urinary system, and gall bladder. [2] [3] [4] [5]
It is structurally related to papaverine, and is a selective inhibitor of phosphodiesterase-4, and has no anticholinergic effects. [6]
It is available in Asia,[ specify ] Central and Eastern Europe (Poland, [7] Hungary, [8] Estonia, [9] Latvia, [10] Lithuania [11] ) under several brand names. [12] A popular brand is No-Spa, distributed by the Hungarian plant Chinoin (owned by Sanofi). It is distributed by Sanofi as Но-Шпа (No-shpa) in Russia. [13]
Drotaverine hydrochloride has a spasmolytic, myotropic, vasodilation, hypotensive action. [5]
Drotaverine decreases active ionized calcium supply binding to smooth muscle cells due to inhibition of phosphodiesterase and intracellular accumulation of cAMP. It has an apparent and prolonged action on smooth muscles of internal organs and blood vessels and it moderately decreases arterial blood pressure, increases cardiac output (minute volume of heart), and has some antiarrhythmic potential. [5]
Drotaverine decreases vascular tone 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. [5]
Possible side effects include: heating sensation, dizziness, headache (rarely), insomnia. May be observed: arrhythmia (rarely), hypotension, tachycardia, sweating, nausea. [5]
Overdose of Drotaverine potentially can cause atrioventricular (AV) block, cardiac arrest, paralysis of respiratory system. [5]
In Israel the product is known under the brand name "No-Spa" by the general public [14] which did not receive a permit to be distributed by the health ministry, [15] however due to high demand local medical counterfeiters have managed to smuggle No-Spa tablets over the years. [15]
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. [16] [17]
In 2011, the Israeli patent and trademark office declined the use of No-SPA. [14]
An article from 2013 described the effects from overdose (in a 19-year-old female) as including vomiting, seizures and fatal cardiac toxicity. [18]
In 2016, the young Russian chess player Ivan Bukavshin 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. [19]
Pseudoephedrine (PSE) is a sympathomimetic drug of the phenethylamine and amphetamine chemical classes. It may be used as a nasal/sinus decongestant, as a stimulant, or as a wakefulness-promoting agent in higher doses.
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Losartan, sold under the brand name Cozaar among others, is a medication used to treat high blood pressure (hypertension). It is in the angiotensin receptor blocker (ARB) family of medication, and is considered protective of the kidneys. Besides hypertension, it is also used in diabetic kidney disease, heart failure, and left ventricular enlargement. It comes as a tablet that is taken by mouth. It may be used alone or in addition to other blood pressure medication. Up to six weeks may be required for the full effects to occur.
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Lofepramine, sold under the brand names Gamanil, Lomont, and Tymelyt among others, is a tricyclic antidepressant (TCA) which is used to treat depression. The TCAs are so named as they share the common property of having three rings in their chemical structure. Like most TCAs lofepramine is believed to work in relieving depression by increasing concentrations of the neurotransmitters norepinephrine and serotonin in the synapse, by inhibiting their reuptake. It is usually considered a third-generation TCA, as unlike the first- and second-generation TCAs it is relatively safe in overdose and has milder and less frequent side effects.
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Amrinone, also known as inamrinone, and sold as Inocor, is a pyridine phosphodiesterase 3 inhibitor. It is a drug that may improve the prognosis in patients with congestive heart failure. Amrinone has been shown to increase the contractions initiated in the heart by high-gain calcium induced calcium release (CICR). The positive inotropic effect of amrinone is mediated by the selective enhancement of high-gain CICR, which contributes to the contraction of myocytes by phosphorylation through cAMP dependent protein kinase A (PKA) and Ca2+ calmodulin kinase pathways.
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