indication

Used to produce controlled hypotension during surgical procedures and in hypertensive crises.

pharmacology

Pentolinium acts as a ganglionic blocking agent. Pentolinium inhibits release of adrenaline and noradrenaline from adrenergic nerves. It is used as an antihypertensive, and can be administered orally, intramuscularly, and subcutaneously.

mechanism of action

Pentolinium binds to the nicotinic (ganglion) acetylcholine receptor. This receptor/channel is permeable to a range of divalent cations including calcium, the influx of which may activate a potassium current which hyperpolarizes the cell membrane. Blockage of the receptor leads to smooth muscle relaxation and vasodilaton.

toxicity

Oral, mouse: LD₅₀ = 512 mg/kg; Oral, rat: LD₅₀ = 890 mg/kg.