Temocapril is a prodrug-type angiotensin-I converting enzyme (ACE) inhibitor not approved for use in the United States but is approved in Japan and South Korea. Temocapril can also be used in hemodialysis patients without risk of serious accumulation.

Bamifylline (or bamiphylline), a selective antagonist of the A1 adenosine receptor, was studied in the therapy of asthmatic syndromes.

PHENOPERIDINE is an opioid analgesic partly metabolized to meperidine in the liver. It is derived from pethidine by replacing the N methyl by a phenyl propanol chain. It is reputed to be a typical morphine-like analgesic characterized by its high potency, rapid onset of action, the intensity of its peak effect and the short duration of its pharmacological effects. It is used in general anesthesia.

Benapryzine is a dialkylaminoethanol ester of diphenylacetic acid. It is a muscarinic cholinoceptor antagonist with negligible peripheral effects. Benapryzine in addition to its anti-acetylcholine action antagonizes both maximal electroshock and metrazol-induced convulsions in mice. This feature is not generally shown by anti-acetylcholine agents but is seen with orphenadrine. Side effects of benapryzine were rare. They are: drowsiness, dry mouth, confusion, disorientation, hallucinations and postural syncope with measurable postural hypotension. Benapryzine has been used as an antiparkinsonian agent.

Naftidrofuryl (INN), also known as nafronyl or as the oxalate salt naftidrofuryl oxalate or nafronyl oxalate, is a vasodilator used in the management of peripheral and cerebral vascular disorders. The drug act as a selective antagonist of 5-HT2 receptors. Naftidrofuryl is marketed under a variety of trade names, including Artocoron, Azunaftil, Di-Actane, Dusodril, Enelbin, Frilix, Gevatran, Iridus, Iridux, Luctor, Nafti, Naftoling, Naftodril, Nafoxal, Praxilene, Sodipryl retard, and Vascuprax. Praxilene belongs to a group of medicines known as ‘metabolic activators’. These are used to treat different types of blood circulation problems. Praxilene allows the body to make better use of the oxygen in your blood. Praxilene is used to treat the following symptoms: cramp-like pains; cramps in legs at night; severe pain in r legs when people are resting (rest pain); pale or blue fingers or toes which get worse when it is cold; numbness, tingling or burning feelings in the fingers or toes (Raynaud’s syndrome or acrocyanosis); open sores on the legs or feet (trophic ulcers); poor circulation caused by diabetes (diabetic arteriopathy).

Landiolol (Onoact) is an intravenously administered, ultra short-acting β1-blocker with an elimination half-life of 3-4 min and ≈8-fold greater cardioselectivity than esmolol in vitro. It is approved in Japan for the treatment of intraoperative and postoperative tachyarrhythmias, but in clinical practice is also used to prevent postoperative tachyarrhythmias, such as atrial fibrillation after coronary artery bypass grafting. Randomized controlled trials in patients undergoing open-heart surgery demonstrated that various dosages of landiolol (0.0005-0.04 mg/kg/min) [0.5-40 μg/kg/min] were more effective than diltiazem in converting postoperative atrial fibrillation to normal sinus rhythm during the first 8 h after surgery, and were more effective than placebo (or no landiolol) in preventing the development of atrial fibrillation during the first week after surgery (primary efficacy endpoints). Landiolol was generally well tolerated in clinical trials, with a relatively low risk of hypotension and bradycardia, although routine monitoring of cardiac function during landiolol administration is important. In general, adverse events such as reduced blood pressure resolve quickly after discontinuation of landiolol. Thus, as an ultra short-acting β1-blocker with a rapid onset of action and readily titratable and rapidly reversible effects, landiolol represents an important agent for the management of intraoperative and postoperative tachyarrhythmias.

Alphacetylmethadol (INN), aka α-acetylmethadol (AAM), is a synthetic opioid analgesic. Its levorotary enantiomer, levacetylmethadol, is an FDA-approved treatment for opioid addiction. Alphacetylmethadol is very similar in structure to methadone, a widely-prescribed treatment for opioid addiction. In the United States, it is a Schedule I controlled substance under the Controlled Substances Act with an ACSCN of 9603 and a 2013 annual manufacturing quota of 2 grams. Studies in rats indicate that alphacetylmethadol also evokes the heroin-like discriminative stimulus effects.

METHOPHOLINE, an isoquinoline derivative, is an opioid analgesic drug. Its (R)-enatiomer is approximately six times more potent than codeine, and (S)-enantiomer is inactive. METHOPHOLINE was withdrawn from the market for reasons of safety.