Pentolinium

Betamethasone Benzoate 538.6 Pentolinium Tartrate 605.6 Butaperazine Phosphate... 

Diquat Dibromide Distigmine Bromide Ethyl Nicotinate Gallamine Triethiodide Hexamethonium Bromide Hydrastinine Mebezonium Iodide Neomycin Noradrenaline Paraquat Dichloride Pentolinium Tartrate Quinuronium Sulphate Streptomycin Tubocurarine Chloride... 

Pentolinium, however, had certain disadvantages which made it impractical for the treatment of mild or moderate hypertension. The disturbing side effects associated with blockade of the sympathetic and parasympathetic nervous system were still present constipation, dry mouth, impotence, chilling in a cold environment, and blockade of the reflex adjustment of blood pressure which normally occurs when the patient assumes the erect position. Occasionally, the postural hypotension was so severe that there was insufficient blood flow to the brain and the patient fainted. 

Quaternary ammonium bases are poorly absorbed from the gastrointestinal tract. In the case of hexamethonium and pentolinium less than 10% of the ingested dose is actually absorbed. Further development of effective ganglionblocking agents, therefore, was directed toward improving absorption. It was hoped that the fluctuations in blood pressure and the severity of the side effects... 

Such ganglionic blocking agents that interfere with the nervous transmission of sympathetic as well as para-sympathetic ganglia may include hexa-methonium bromide mecamylamine hydrochloride pempidine pentolinium tartrate, trimetaphan camsylate, etc. 

Pentolinium tartrate is mainly used in the treatment of severe essential and malignant hypertensions and employed to produce controlled hypotension in patients undergoing surgical procedures. 

The inactin (lOOmg/kg, i.p. sodium ethyl-(1-methyl-propyl)-malonylthio-urea) anesthetized rats are treated with atropine (2.4mg/kg, s.c.), and their ganglions are blockaded with pentolinium (19.2mg/kg, s.c.). Overall, 10-mg/kg captopril is administered i.v. acutely to the rats in the captopril group, and it inhibits fully the pressor effect of 60-ng/kg angiotensin I. 

Responses, in terms of the increases in systolic (SBP) and diastolic (DBP) blood pressures, to test peptide and bradykinin are determined. After ganglion blockade with pentolinium (group GB) without or with added captopril (group GB+Cap), heart rate and plasma adrenaline and noradrenaline concentrations are determined. In some cases, the rats are not subjected to ganglion blockade and served as controls for animals in the GB group (control group). 

New Compounds (Ganglion Blockers) - KY6 (XVI) produced hypotensive activity in anesthetized cats via blockade of sympathetic ganglia, and is as effective eis pentolinium bitartrate.25 Examination of a series of related N-alkyl and N,N,-dialkyl-aininopropion droxamic acids failed to provide a conpound with more potent activlty.So... 

Injection of Pentolinium Tartrate, A sterile solution in water for injection, adjusted to pH 6-5 with sodium hydroxide. 

This preparation can be assayed as reineckate similarly to hexamethonium tartrate injection above. Pentolinium reineckate solution for washing the precipitate is prepared similarly using pentolinium tartrate. 1 g residue -- 0-6140 g C23H420i2N2. 

For assay an amount of powdered tablets equivalent to about 0 12 g of pentolinium tartrate should be extracted with warm water, filtered and the insoluble matter washed before evaporating the total filtrate and washings to about 10 ml and then continuing as for the injection. 

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