Gallopamil is a L-type calcium channel blocker designed for the treatment of coronary heart diseases: angina pectoris, prinzmetal angina and hypertonia.

Deptropine citrate is a well-known H1-histamine receptor antagonist and muscarinic receptor antagonist. It is prescribed frequently for treatment of asthma, although there has been a sharp decrease in prescriptions since 1994. Deptropine is gradually being replaced by inhaled beta 2 adrenergic agonists and glucocorticosteroids as the preferred clinical prescription. Recently deptropine has garnered interest as a potential treatment for breast cancer. In vitro studies have shown deptropine citrate has inhibitory effects on cell viability and mammosphere formation in Breast Cancer Stem Cells (BCSCs). However, it does not seem to inhibit the self-renewal capacity of the breast cancer cell line MDA-MB-231 when it is enriched with Cancer Stem Cells.

Tulobuterol is a long-acting beta2-adrenergic receptor agonist. Tulobuterol has almost no effects on blood pressure and heart rate and is highly selective for the tracheal muscle. It is indicated to improve symptoms such as respiratory distress caused by airway obstruction of bronchial asthma, bronchitis, chronic obstructive pulmonary disease (COPD) and emphysema. Serious side effects detected were: tremor, palpitations and serum potassium level decrease.

Subarachnoid haemorrhage (SAH) following cerebral aneurysm rupture or trauma can result in the induction of secondary ischaemic brain damage via a decrease in microvascular perfusion, a disruption of the blood-brain barrier and consequent vasogenic oedema, and the delayed spasm of the major cerebral arteries (i.e. vasospasm). It is increasingly apparent that oxygen radical-induced, iron-catalyzed lipid peroxidation (LP) within the subarachnoid blood and vascular wall plays a key role in the occurrence of these secondary events. Tirilazad mesylate, is a nonglucocorticoid, 21-aminosteroid, is a potent cytoprotective inhibitor of LP that works by a combination of radical scavenging and membrane stabilizing properties. It has been demonstrated to attenuate the acute and delayed vascular consequences of SAH and to protect the brain against ischaemic insults. Tirilazad mesylate has been proposed to treat acute ischaemic stroke. When tested on animal models, tirilazad protects brain tissue, and reduces brain damage. However, the drug fails to treat, and even worsens a stroke when studied on a human being.

Fentonium is an anticholinergic, antispasmodic and anti-ulcerogenic agent. It is quaternary analog of hyoscyamine, is a blocker of muscarinic activity and an allosteric blocker of α12βγε nicotinic receptors. It increases the spontaneous release of acetylcholine at the motor endplate without depolarizing the muscle or inhibiting cholinesterase activity. Fentonium inhibited transmitter release and depressed twitch without changing the responsiveness to noradrenaline or ATP. It is a K(+)-channel opener. Administration of fentonium bromide in rats receiving naloxone after chronic morphine treatment reduced the intensity of withdrawal signs such as increased defecation or micturition, salivation and wet-dog shakes, and elevated the nociceptive threshold values.

Methylnaltrexone bromide, (17s)- (methylnaltrexone bromide), a quaternary amine of the pure narcotic antagonist naltrexone, is a peripherally-acting selective mu-opioid antagonist. Methylnaltrexone antagonizes opioid binding at mu-opioid receptors, half-maximal inhibitory concentration (IC50) of 70 nM. It has a relatively lower affinity for κ-opioid receptors (IC50 575 nM), and it does not interact with δ-receptors or orphanin FQ receptors. Approved by FDA in the United States under the trade name Relistor, methylnaltrexone bromide is indicated for the treatment of opioid-induced constipation in patients with advanced illness who are receiving palliative care, when the response to laxative therapy has not been sufficient. Restricted ability to cross the blood-brain barrier allows methylnaltrexone bromide to function in tissues such as the gastrointestinal tract, decreasing the constipating effects of opioids without impacting opioid-mediated analgesic effects on the central nervous system.

trans-Sobrerol is a mucolytic known due its emplyment in therapy for respiratory diseases. In preclinical studies sobrerol, administered daily at the oral dose of 400 mg/rat, markedly decreased the monocrotaline-induced alterations and regulate the development of pulmonary hypertension. Treatment with sobrerol was well tolerated and significantly reduced frontal headache and rhinorrhoea, efficacy being confirmed by rhinomanometry.

Oxyfedrine, an amino ketone derivative and partial agonist at beta receptors, has been shown to have potent antianginal properties and to increase coronary blood flow in normal and ischemic myocardial regions.

Mitiglinide is a drug for the treatment of type 2 diabetes currently marked under tradename Glufast. Glufast® is available as the tablet for oral use, containing 5 mg or 10 mg of Mitiglinide calcium hydrate. The recommended dose is 10 mg three times daily just before each meal (within 5 minutes). Mitiglinide was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on January 29, 2004, and is currently co-marketed in Japan by Kissei and Takeda. Mitiglinide is a rapid-acting insulin secretion-stimulating agent, its belongs to the meglitinide (glinide) class of blood glucose-lowering drugs. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) (K(ATP)) channels in pancreatic beta-cells.

Indobufen inhibits platelet aggregation by reversibly inhibiting the platelet cyclooxygenase enzyme thereby suppressing thromboxane synthesis. Indobufen under brand name ibustrin is used in Italy for the following conditions: cerebrovascular insufficiency, atherosclerosis of peripheral and cerebral vessels, thrombophlebitis, deep vein thrombosis, and diabetes mellitus. In addition, this drug has been investigated in the phase II clinical trial for the prevention of thromboembolic events in patients with nonrheumatic atrial fibrillation. After oral administration, it is quickly and completely absorbed.