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.

Dimecrotic acid is a choleretic agent with spasmolytic properties. It is obtained by reaction of resorcinol with acetoacetate to give 4-methyl-7-hydroxycoumarin. It is indicated for the treatment of hepato-digestive insufficiency and its manifestations. It shouldn’t be used in case of blockage of bile ducts, severe liver failure and severe renal impairment. Diarrhea may be associated with high doses of dimecrotic acid.

Citicoline (CDP-choline; cytidine 5'-diphosphocholine) is a novel nutrient with a broad spectrum of benefits for conditions associated with symptoms of neurological dysfunction shows promise of clinical efficacy in elderly patients with cognitive deficits, inefficient memory, and early-stage Alzheimer's disease. Citicoline has also been investigated as a therapy in stroke patient. Despite it was approved in some countries for treatment Traumatic Brain Injury (TBI), the use of this drug for acute TBI seems to have no field of support anymore, whereas it may have some benefits in improving the neuro-cognitive state in chronic TBI patients. It's also recommended to keep in mind acute interventions like Psychological First Aid (PFA) during acute TBI management. Citicoline plays several important roles in human physiology, including enhancement of structural integrity and signaling for cell membranes, support of acetylcholine synthesis, and synthesis of betaine, a methyl donor. The precise mechanism of action of Citicoline to treat disease is unknown, but was confirmed, that drug might increase phosphatidylcholine (PtdCho) synthesis and might reverse PtdCho loss. In addition, was shown, that citicoline modulates phospholipids metabolism and neurotransmitter levels and appears to improve cognition in some central nervous system disorders such as bipolar disorder and cocaine dependence. Bipolar disorder is associated with the highest rates of substance abuse of any psychiatric disorder. Cocaine use is particularly common in patients with bipolar disorder.

Flotufolastat F 18 (POSLUMA®) is an 18F-labelled radiohybrid (rh) prostate-specific membrane antigen (PSMA)-targeted imaging agent being developed by Blue Earth Diagnostics, a subsidiary of Bracco Imaging, for prostate cancer imaging. In May 2023, flotufolastat F 18 received its first approval in the USA as a radioactive diagnostic agent for positron emission tomography (PET) of PSMA positive lesions in men with prostate cancer with suspected metastasis who are candidates for initial definitive therapy or with suspected recurrence based on elevated serum prostate-specific antigen (PSA) level. Flotufolastat F 18 binds to PSMA (IC50 = 4.4 nM) expressed on cells, including prostate cancer cells, and is internalized. Prostate cancer cells usually overexpress PSMA. Fluorine-18 is a beta emitting radionuclide that can be detected using positron emission tomography.

Menatetrenone (INN), also known as MK4, is a vitamin K compound used as a hemostatic agent, and also as adjunctive therapy for the pain of osteoporosis. MK4 is marketed for the osteoporosis indication in Japan by Eisai Co., under the trade name Glakay. Has several mechanism of actions: (1) Acceleration of osteogenesis. In human osteoblast cultures, calcification was accelerated by administration of menatetrenone at a concentration of 2.25 × 10-6 mol/L alone or when it was coadministered with 1,25(OH)2D3. The osteocalcin content in the cell layers was increased by coadministration with 1,25(OH)2D3. 2. Inhibition of bone resorption. In organ cultures of mouse calvaria, at concentrations of 3 × 10-6 to 3 × 10-5 mol/L, menatetrenone inhibited bone resorption induced by IL-1α, PGE2, PTH and 1,25(OH)2D3. In mouse bone marrow cell cultures, at concentrations of 3 × 10-6 to 1 × 10-5 mol/L, menatetrenone inhibited the induction of osteoclast release by 1,25(OH)2D3. 3. Effect on serum level of osteocalcin. Menatetrenone was administered to patients with osteoporosis at a dose of 45 mg/day for 2 years. Menatetrenone increased the serum level of osteocalcin and decreased the serum level of Glu-osteocalcin.

Sodium gualenate (Azunol ST Tablets) is a water-soluble derivative of azulene, a natural product which is an antiinflammatory component of chamomile of the family of Asteraceae. Sodium gualenate was originally studied as an antiulcer agent, is primary indicated in conditions like Duodenal ulcer, Gastric ulcer, Gastritis, but it is also clinically used as a therapeutic agent in the treatment of inflammation of the mouth and throat, for example, pharyngitis as well as other inflammatory diseases such as tonsillitis, stomatitis and conjunctivitis. Although the mechanism by which sodium azulene sulfonate inhibited the capsaicin-induced pharyngitis is not yet unraveled, antioxidative effect, but not inhibitory effect on cyclooxygenase pathway, might be involved.

Amosulalol is a beta- and alpha-1 adrenoceptor-blocking agent developed for the treatment of hypertension. Amosulalol does not cross blood brain barrier and does not have adverse affect on CNS system.The drug is marketed under the name Lowgan in Japan and Korea.

Imepitoin (AWD 131–138 or ELB 138; 1-(4-chlorophenyl)-4-morpholino-imidazolin-2-one) is a new anti-epileptic drug recently approved in the European Union for the treatment of canine idiopathic epilepsy. It was developed from a series of imidazolinones due to its pronounced ant seizure activity in a large variety of rodent models of epileptic seizures, combined with a high tolerability in these models. Imepitoin is a centrally acting antiepileptic substance, which crosses the blood brain barrier without involvement of active transport or active clearance, resulting in immediate equilibrium between plasma and brain. Imepitoin acts as low-affinity partial agonists at the benzodiazepine (BZD) site of the GABAA receptor. Hopefully, that the favorable profile of imepitoin for the treatment of epilepsy in dogs will reactivate the interest in partial BZD site agonists as new treatments for human epilepsy.

Azaperone (Stresnil, Fluoperidol) is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects. It is mainly as a tranquilizer in veterinary medicine. Azaperone is officially indicated for the “control of aggressiveness when mixing or regrouping weanling or feeder pigs weighing up to 36.4 kg”. It is also used clinically as a general tranquilizer for swine, in particular with aggressive sows to allow piglets to be accepted, and as a preoperative agent prior to general anesthesia or cesarian section with local anesthesia. Azaperone has also been used as a neuroleptic in horses, but some horses develop adverse reactions (sweating, muscle tremors, panic reaction, CNS excitement) and IV administration has resulted in significant arterial hypotension in the horse; because of these effects, most clinicians avoid the use of this drug in equines. Azaperone appears to have minimal effects on respiration and may inhibit some of the respiratory depressant actions of general anesthetics. A slight reduction of arterial blood pressure has been measured in pigs after IM injections of azaperone, which is apparently due to slight alpha-adrenergic blockade. Azaperone has been demonstrated to prevent the development of halothane-induced malignant hyperthermia in susceptible pigs. Preliminary studies have suggested that the effects of butyrephenones may be antagonized by 4-aminopyridine. Azaperone acts primarily as a dopamine antagonist but also has some antihistaminic and anticholinergic properties as seen with similar drugs such as haloperidol. Azaperone may cause hypotension and while it has minimal effects on respiration in pigs, high doses in humans can cause respiratory depression which may be why it is rarely used in humans. Higher doses are used for anesthesia in combination with other drugs such as xylazine, tiletamine and zolazepam. Azaperone is also used in combination with strong narcotics such as etorphine or carfentanil for tranquilizing large animals such as elephants.

Tocotrienols are a group of chemicals that are part of the vitamin E family. Tocotrienol is any of the four forms, alpha, beta, gamma and delta, of a member of the vitamin E family. It has potential hypocholesterolemic, antithrombotic, antioxidant, immunomodulating and antineoplastic activities. Tocotrienol inhibits the activity of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, thereby lowering cholesterol levels. In addition, tocotrienol acts through multiple signal transduction pathways to induce cell cycle arrest and caspase-mediated apoptosis, and to decrease tumor cell proliferation. In addition, this agent may inhibit angiogenesis through the blockage of vascular endothelial growth factor receptor (VEGFR) and the subsequent inhibition of tumor cell-induced vessel formation. Also, this agent prevents free radical formation and inhibits lipid peroxidation, thereby preventing DNA cell damage. Tocotrienols are scare in nature. They are found most abundantly in crude palm oil extracted from palm fruits. Other sources are rice bran, wheat germ, oat and barley. These substances are available in supplement form as capsules or pills.