Piperaquine is a bisquinoline antimalarial drug that was first synthesized in the 1960s and used extensively in China and Indochina as prophylaxis and treatment during the next 20 years. Usage declined in the 1980s as piperaquine-resistant strains of P. falciparum arose and artemisinin-based antimalarials became available. However, during the next decade, piperaquine was rediscovered by Chinese scientists as one of a number of compounds suitable for combination with an artemisinin derivative. The rationale for such artemisinin combination therapies (ACTs) was to provide an inexpensive, short-course treatment regimen with a high cure rate and good tolerability that would reduce transmission and protect against the development of parasite resistance. Piperaquine is characterized by slow absorption and a long biological half-life, making it a good partner drug with artemisinin derivatives which are fast acting but have a short biological half-life.

Aminopropyl racementhyl phosphate is a prodrug of menthol patented by Pacific Corporation (Korea). Upon administration, it is enzymatically decomposed into menthol and 3-aminopropylphosphoric acid, a component used for anti-aging cosmetic composition. Aminopropyl racementhyl phosphate was found to reduce the irritation of menthol while maintaining its useful effects.

Isaxonine (N-isopropyl-amino-2-pyrimidine orthophosphate) is able to accelerate nerve regeneration and functional recovery. Isaxonine has specific affinity for peripheral nerves. It acts directly on the neuron or indirectly by stimulating the production of a growth factor remains unknown. It demonstrates activity in the treatment of neuropathies of various etiology. Isaxonine treatment may be associated with hepatotoxicity.

Naphthoquine is an antimalarial drug first synthesized in China in 1986 but which was not developed for clinical use until the late 1990s. This drug now is used in combination for treatment of Plasmodium Falciparum and Malaria. The use of anti-malarial drug combinations with artemisinin or with one of its derivatives is now widely recommended to overcome drug resistance in falciparum as well as vivax malaria. The fixed oral dose artemisinin-naphthoquine combination (ANQ, ARCO™) is a newer artemisinin-based combination (ACT) therapy undergoing clinical assessment.

Ligustrazine (tetramethylpyrazine) is a bioactive ingredient extracted from the widely-used Chinese herb, Chuanxiong. It inhibits of platelet aggregation, enhances of vessel dilation, increases cerebral blood flow and possesses neuroprotective properties. The injection solution of ligustrazine has been used especially in China to treat ischemic stroke, coronary heart disease, diabetic nephropathy, and knee osteoarthritis. Ligustrazine was also evaluated in clinical as a remedy for pressure sores, as a salvage agent for patients with non-Hodgkin's lymphoma, as a treatment for bronchial asthma and vertebrobasilar insufficiency.

Antihistamine agent

Paramethasone is a glucocorticoid. It exerts anti-inflammatory and immunosuppressant actions. Paramethasone stimulates the synthesis of enzymes needed to decrease anti-inflammatory response. It suppresses the immune system by reducing activity and volume of the lymphatic system, thus producing lymphocytopenia decreasing passage of immune complexes and possibly by depressing reactivity of tissue to antigen-antibody interactions.

Piperaquine is a bisquinoline antimalarial drug that was first synthesized in the 1960s and used extensively in China and Indochina as prophylaxis and treatment during the next 20 years. Usage declined in the 1980s as piperaquine-resistant strains of P. falciparum arose and artemisinin-based antimalarials became available. However, during the next decade, piperaquine was rediscovered by Chinese scientists as one of a number of compounds suitable for combination with an artemisinin derivative. The rationale for such artemisinin combination therapies (ACTs) was to provide an inexpensive, short-course treatment regimen with a high cure rate and good tolerability that would reduce transmission and protect against the development of parasite resistance. Piperaquine is characterized by slow absorption and a long biological half-life, making it a good partner drug with artemisinin derivatives which are fast acting but have a short biological half-life.

TAT-59 (Miproxifene Phosphate) is a triphenylethylene analog of tamoxifen. TAT-59 is the phosphate ester prodrug of the practically insoluble parent drug DP-TAT-59. It is an antiestrogen developed in Japan for breast cancer. It is a potent antitumor agent for hormone-dependent tumors. Most of TAT-59 metabolites possessed remarkable binding affinity toward estrogenic receptors as well as fairly good antiuterotrophic activity.

Rilmenidine (brand names Albarel, Hyperium, Iterium and Tenaxum) is an imidazoline derivative used for the treatment of hypertension. Rilmenidine, an oxazoline compound with antihypertensive properties, acts on both medullary and peripheral vasomotor structures. Rilmenidine shows greater selectivity for imidazoline receptors than for cerebral alpha2-adrenergic receptors, distinguishing it from reference alpha2-agonists. Rilmenidine is as effective in monotherapy as all other first line classes of drugs, including diuretics, beta-blockers, angiotensin converting enzyme (ACE) inhibitors, and calcium antagonists. It is well tolerated and can be taken in combination for greater efficacy. Sedation and dry mouth are not prominent side effects and withdrawal hypertension is not seen when treatment is stopped abruptly. In addition to a reduction in blood pressure, Rilmenidine has been shown to improve glucose tolerance, lipid risk factors, and insulin sensitivity.