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ATC Group: G04B Other urologicals, incl. antispasmodics

Anatomical Therapeutic Chemical Classification System

Translations

Language
Translation
  English
Other urologicals, incl. antispasmodics

Hierarchical Position

Level
Code
Title
3
G04B
Other urologicals, incl. antispasmodics

Contents

Active Ingredients

Chemical substance
Description

Alprostadil is chemically identical to prostaglandin E1, the actions of which include vasodilatation of blood vessels in the erectile tissues of the corpora cavernosa and increase in cavernosal artery blood flow, causing penile rigidity.

Apomorphine is a direct stimulant of dopamine receptors and while possessing both D1 and D2 receptor agonist properties does not share transport or metabolic pathways with levodopa. Its actions on parkinsonian motor disability are likely to be mediated at post-synaptic receptor sites.

Avanafil is a highly selective and potent, reversible inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5. When sexual stimulation causes the local release of nitric oxide, inhibition of PDE5 by avanafil produces increased levels of cGMP in the corpus cavernosum of the penis. This results in smooth muscle relaxation and inflow of blood into the penile tissues, thereby producing an erection.

Calcium is the most abundant mineral in the body, and is an essential body electrolyte. Homeostasis is mainly regulated by the parathyroid hormone, by calcitonin, and by the activated form of vitamin D. Calcium is a structural component of bones and teeth. It is also required for blood clotting, neurotransmitter release, muscle contraction and normal heartbeat.

Dapoxetine is a potent selective serotonin reuptake inhibitor (SSRI) with an IC50 of 1.12 nM, while its major human metabolites, desmethyldapoxetine (IC50<1.0 nM) and didesmethyldapoxetine (IC50=2.0 nM) are equivalent or less potent (dapoxetine-N-oxide (IC50=282 nM)).

Darifenacin is a selective muscarinic M3 receptor antagonist (M3 SRA) in vitro. The M3 receptor is the major subtype that controls urinary bladder muscle contraction. It is not known whether this selectivity for the M3 receptor translates into any clinical advantage when treating symptoms of overactive bladder syndrome.

Desfesoterodine is a competitive, specific muscarinic receptor antagonist. It is the primary active metabolite of fesoterodine, and regarded as main active pharmacological principle of fesoterodine; fesoterodine is considered as prodrug of desfesoterodine. The affinity of desfesoterodine for the muscarinic receptors is 2 orders of magnitude greater than that of fesoterodine.

Fesoterodine is a competitive, specific muscarinic receptor antagonist.

Flavoxate is an antispasmodic selective to the urinary tract. Flavoxate has been shown to have a direct antispasmodic action on smooth muscle fibres.

Magnesium hydroxide is practically insoluble in water and solution is not effected until the hydroxide reacts with hydrochloric acid in the stomach to form magnesium chloride. Its neutralising action is almost equal to that of sodium bicarbonate. When the dose is in excess of that required to neutralise the acid the intragastric pH may reach pH 8 or 9. Acid rebound following magnesium hydroxide is clinically insignificant. Magnesium hydroxide has an indirect cathartic effect resulting from water retention in the intestinal lumen.

Mirabegron is a potent and selective beta3-adrenoceptor agonist. Mirabegron enhances urine storage function by stimulating beta3-adrenoceptors in the bladder.

Oxybutynin acts as a competitive antagonist of acetylcholine at post-ganglionic muscarinic receptors, resulting in relaxation of bladder smooth muscle.

The hypothetic mechanism of action of pentosan polysulfate sodium includes a local effect in the bladder after systemic administration and excretion into the urine by binding of glycosaminoglycans to the deficient mucous of the bladder. It is hypothesized, that a potential barrier function of pentosan polysulfate sodium instead of the damaged urothelial mucus might play a role as well the antiinflammatory activity of pentosan polysulfate sodium.

Propiverine inhibits calcium influx and modulates intracellular calcium in urinary bladder smooth muscle cells causing musculotropic spasmolysis. Also, it inhibits the efferent connection of the nervus pelvicus due to anticholinergic action.

Sildenafil is a potent and selective inhibitor of cyclic guanosine monophosphate (cGMP) specific phosphodiesterase type 5 (PDE5), the enzyme that is responsible for degradation of cGMP. Apart from the presence of this enzyme in the corpus cavernosum of the penis, PDE5 is also present in the pulmonary vasculature. Sildenafil, therefore, increases cGMP within pulmonary vascular smooth muscle cells resulting in relaxation.

Solifenacin is a competitive, specific cholinergic-receptor antagonist. In vitro and in vivo pharmacological studies indicate that solifenacin is a competitive inhibitor of the muscarinic M3 subtype receptor.

Tadalafil is a selective, reversible inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). When sexual stimulation causes the local release of nitric oxide, inhibition of PDE5 by tadalafil produces increased levels of cGMP in the corpus cavernosum. This results in smooth muscle relaxation and inflow of blood into the penile tissues, thereby producing an erection. Tadalafil has no effect in the absence of sexual stimulation.

Tolterodine is a competitive, specific muscarinic receptor antagonist with a selectivity for the urinary bladder over salivary glands in vivo.

Trospium is an antispasmodic, antimuscarinic agent indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. Receptor assays showed that trospium has negligible affinity for nicotinic receptors as compared to muscarinic receptors at concentrations obtained from therapeutic doses. Trospium antagonizes the effect of acetylcholine on muscarinic receptors in cholinergically innervated organs. Its parasympatholytic action reduces the tonus of smooth muscle in the bladder.

Vardenafil is a potent and selective inhibitor of the cGMP specific phosphodiesterase type 5 (PDE5), the most prominent PDE in the human corpus cavernosum. Vardenafil is an oral therapy for the improvement of erectile function in men with erectile dysfunction. In the natural setting, i.e. with sexual stimulation it restores impaired erectile function by increasing blood flow to the penis.

Monographs