Hexamethonium is a nicotinic cholinergic antagonist. It was used to treat hypertension, but has never been approved and was discontinued because of the non-specified treatment. When this drug tried to use in medical study via inhalation, one of the volunteer died, the death has been described as “particularly disturbing ”because it was a healthy volunteer who had no thing to gain by taking part in the study. This volunteer participated in a study designed to provoke a mild asthma attack in order to help doctors discover the reflex that protects the lungs of healthy people against asthma attacks. Hexamethonium is poorly absorbed from the gastrointestinal tract and does not cross the blood-brain barrier. Now it is widely used a research tool.

Thiphenamil, an antispasmodic drug with a local anesthetic activity, inhibits contraction. The clinical trials have shown that thiphenamil could suppress upper urinary tract contractility, and was suggested to use the drug for renal colic and stone management. In addition, this drug was studied for the treatment of detrusor incontinence in patients with detrusor instability. The results showed, that the drug caused a significant decrease in problems due to loss of urine when the patient was taking the drug compared to the placebo.

Methoxamine is an alpha-adrenergic agonist that induces prolonged peripheral vasoconstriction, and can also stimulate the release of arginine vasopressin in humans. In clinical trials, methoxamine was found to improve fecal incontinence. It had been marketed by Glaxo-Smith-Kline under the brand name Vasoxyl but has been discontinued. Methoxamine was also found to stimulate the induction of hiPSC-derived hepatoblasts to ALBUMIN+ cells.

Piperoxan is the first antihistamine was discovered. Piperoxan protected guinea pigs against histamine-induced bronchospasm. The piperoxan has been used to provoke anxiety behaviors in the monkey. Piperoxan is an alpha-adrenergic antagonist. Piperoxan has been claimed to preferentially block presynaptic alpha-adrenoreceptors leading to an increase in noradrenaline release and by this way the postsynaptic alpha-adrenoreceptors blockade may be overcome. There was clear evidence that piperoxan enhanced myocardial performance. Piperoxan is a diagnostic aid used in studies of hypertension.

Piridocaine is a piperidyl propanol ester of orthoaminobenzoic acid. The toxicity of this drug resembles that of procaine. It differs from procaine in that the minimum anesthetic dose is smaller, the minimal lethal dose larger, and duration of anesthesia longer. Subarachnoid piridocaine with and without epinephrine or ephedrine offers a simple and dependable means of obtaining any degree or extent of analgesia up to the third thoracic nerves without profound or widespread motor paralysis. The most promising clinical field of usefulness for piridocaine is obstetrics.

Methoxyphenamine also known as 2-methoxy-N-methylamphetamine (OMMA), is a beta adrenergic receptor agonist nd is used as a bronchodilator to treat asthma, chronic obstructive pulmonary disease (COPD) and postinfectious cough. In addition, methoxyphenamine using is prohibited in sports according to the regulations of the World Anti-Doping Agency (WADA).

ALPHAPRODINE is an opioid analgesic. It was used in obstetrics, as pre-operative medication, and for minor surgical procedures. In addition, this drug was used in the dentistry setting to help effectively manage pain associated with dental procedures.

Caramiphen is a muscarinic M1 acetylcholine receptor antagonist, which was used for the treatment of Parkinson Disease and cough, but then there using were discontinued. Caramiphen is also used in local anesthesia, and effect could be achieved through the suppression of voltage-gated Na⁺ currents.

Cyclomethycaine (also known as Surfacaine) is a local anesthetic.

Cyclomethycaine (also known as Surfacaine) is a local anesthetic.