Naftopidil (INN, marketed under the brand name Flivas) is a drug used in benign prostatic hypertrophy which acts as a selective alpha1-adrenergic receptor antagonist, has been used for the treatment of benign prostatic obstruction and benign prostatic hyperplasia (BPH) associated lower urinary tract symptoms (LUTS). The Japanese Ministry of Health, Labor and Welfare approved naftopidil for treating men with BPH in 1996. Although well-designed, randomized studies are warranted to confirm the long-term outcomes and effector/target of naftopidil, the α1A-antagonist naftopidil, which also blocks α1D-adrenoceptor, improves voiding symptoms, and may also be useful for the management of men with storage symptoms represented by nocturia, retrieving their quality of life impaired by BPH-associated LUTS. The selective alpha1D-blocker naftopidil can significantly facilitate spontaneous passage of distal ureteral stones with few side effects, providing a new choice for medical expulsive therapy.

(R)-Timolol is the (R)-enantiomer of non-selective Beta antagonist Timolol. (R)-Timolol is a ß-adrenergic blocking agent that binds only to nonspecific sites in the particulate fraction of the heart, lungs, and brain. (R)-Timolol is an antihypertensive agent that increases ocular blood flow and reduces intraocular pressure. (R)-Timolol is one of the impurities in commercial formulation of (S)-Timolol.

Azelastine (brand names AZEP, ASTEPRO, ASTELIN etc.) a phthalazine derivative, is an antihistamine and mast cell stabilizer available as a nasal spray for hay fever and as eye drops for allergic conjunctivitis. Azelastine is a potent antiallergic compound with histamine H1-receptor antagonist activity and a rapid onset and long duration of action. The major metabolite, desmethylazelastine, also exhibits H1- receptor antagonist activity. AZEP Nasal Spray is administered as a racemic mixture. The racemate, R- and S- enantiomers were equally potent at inhibiting eyelid histamine-induced oedema in rats, however the R-enantiomer was 2-fold less active at inhibiting eyeball histamine-induced oedema.

Tiemonium (often used in a form of iodide or methylsulphate salt) is a muscarinic acetylcholine receptor antagonist, which is available in Asia (mainly Bangladesh) for the alleviation of muscle spasms of the intestine, biliary system, uterus and urinary bladder in gastrointestinal, biliary, urinary and gynecological diseases.

Zamifenacin, also known as UK-76654, a selective muscarinic M3 receptor antagonist, was studied in patients with irritable bowel syndrome (IBS). This drug participated in clinical trials for the IBS phase III in the USA and phase II in the UK, but these studies were discontinued.

Piretanide (INN, trade names Arelix, Eurelix, Tauliz) has been synthesized in 1973 at Hoechst AG (Germany) as a loop diuretic[2] compound by using a then-new method for introducing cyclic amine residues in an aromatic nucleus in the presence of other aromatically bonded functional groups. Studies of piretanide in rats and dogs in comparison with other high-ceiling diuretics such as furosemide and bumetanide found a more suitable dose/response rate (regression line) and a more favourable sodium/potassium excretion ratio. These findings led eventually to clinical studies in man and finally to the introduction as a saluretic and antihypertensive medication in Germany, France, Italy and other countries.

Xibenolol or D-32 (dl-tert-butylamino-3-(2', 3'-dimethylphenoxy)-2-propanol hydrochloride) is a beta-blocking agent. It has been developing as a hypontesive medicine by Kowa Pharmaceutical and Teikoku Hormone, however development has been discontinued.

Tymazoline (trade name Thymazen in Poland) is a nasal decongestant that can be used to treat rhinitis and nasal obstruction. Tymazoline is a drug with antihistaminic and sympathomimetic properties. It locally reduces swelling, inflammation and mucosal secretions of the nasal passages. Thymazen causes vasoconstriction of the nasal mucosa, reducing congestion and thus the swelling of the mucosa. Also reduces the secretions from the nose. Thymazen acts on alpha-adrenergic receptors, which reduces local inflammation of the nasal mucosa especially if their cause is an allergy.

Fonzine (also known as dimetotiazine) is an analgesics and anti-inflammatory agent marketed in Japan and Europe under the name Migristene and indicated for the treatment of migraine and headaches secondary to other disease. Fonzine exerts its activity by inhibiting serotonin and histamine H1 receptors.

Fimasartan is a angiotensin II receptor antagonist which was developed in Korea for the treatment of hypertension. The drug is available in different forms: Kanarb, Dukarb (in combination with Amlodipine), Tuvero (in combination with Rosuvastatin). Fimasartan was tested to be effective in Mexican and Russian population and now is being tested in the USA.