Velnacrine (9-amino-1,2,3,4-tetrahydroacridin-1-ol) is an inhibitor of acetylcholinesterase. It was studied for the treatment of Alzheimer's disease however development was discontinued. There has been no research into the use of velnacrine as a cognitive enhancer in the treatment of Alzheimer's disease since 1994. The FDA peripheral and CNS drug advisory board voted unanimously against recommending approval. This review shows the toxic nature of velnacrine, and provides no evidence of efficacy.

Phosphocreatine (creatine phosphate, PCr, PC) is the phosphorylated form of endogenous creatine that serves as a rapidly mobilizable reserve of high-energy phosphates in skeletal muscle and the brain of vertebrates. Phosphocreatine is a key component in the intracellular system of energy buffering and transports from the site of energy production to the site of energy utilization to ensure that supply meets the high and dynamic demands of the heart. Phosphocreatine can anaerobically donate a phosphate group to ADP to form ATP during the first two to seven seconds following an intense muscular or neuronal effort. Conversely, excess ATP can be used during a period of low effort to convert creatine to phosphocreatine. The reversible phosphorylation of creatine is catalyzed by several creatine kinases. Particularly, PCr makes the energy of phosphoryl bonds of adenosine triphosphate (ATP) available at the myofibrillar creatine kinase that allows myocardium contraction. Supplementation with PCr was, therefore, suggested as potentially beneficial in patients with acute and chronic myocardial ischaemic injury. Phosphocreatine has been tried in the treatment of cardiac disorders and has been added to cardioplegic solutions. Phosphocreatine is used intravenously in hospitals in some parts of the world for cardiovascular problems under the name Neoton and also used by some professional athletes, as it is not a controlled substance.

Dipipanone are indicated for the management of moderate to severe pain in medical and surgical conditions in which morphine may be indicated. Dipipanone is related to methadone and can be substituted for assorted opioids. The severe or irreversible adverse effects of Dipipanone, which give rise to further complications, include hypotension, hypotension, hependence, agranulocytosis, ischemic colitis, generalized chorea, hypersensitivity hepatitis. It may interact badly with monoamine oxidase inhibitors, which are substances found in some antidepressants and other medication.

Zafuleptine is an antidepressant drug developed in the 1970s by Science Union & Cie. The compound was reported to have anti-aggressive activity without having other effects on the central nervous system. The mode of action of the compound is similar to that found with the Thyrotropin-Releasing Hormone.

Zafuleptine is an antidepressant drug developed in the 1970s by Science Union & Cie. The compound was reported to have anti-aggressive activity without having other effects on the central nervous system. The mode of action of the compound is similar to that found with the Thyrotropin-Releasing Hormone.

Proxibarbal is a non-sedative barbiturate with a specific anti-serotonin and anti-histamine effect, due to enzyme induction of serotoninase and histaminase. Its lack of unpleasant side-effects. Proxibarbal exists in ring-chain tautomeric equilibrium with the two diastereomers of valofan. Proxibarbal is metabolized to a five-membered lactone. Its only barbituric property is its ability to induce enzymes that destroy a surplus of neurohormones and rid people of their neurovegetative sufferings, including migraine and other types of vascular headache. Side effects are: dizziness, drowsiness, dyspepsia, allergic reactions. Proxibarbal enhances the effects of other depriving agents, including alcohol.

Levorphanol Sulfate (brand name Levo-Dromoran) is an opioid medication used to treat moderate to severe pain. It is one of two enantiomers of the compound racemorphan and was first described in Germany in 1948 and approved for use in the United States in 1953 as an orally active, morphine-like analgesic. Levorphanol is approved for use in moderate to severe pain where an opioid analgesic is appropriate. Levorphanol has a wide range of activities including mu-opioid agonism, delta agonism, kappa1 and kappa3 receptor agonism, N-methyl-D-aspartate receptor antagonism and reuptake inhibition of both norepinephrine and serotonin. This multimodal profile might prove effective for pain syndromes that are refractory to other opioid analgesics, such as central and neuropathic pain and opioid-induced hyperalgesia. Levorphanol is well suited as a first-line opioid and can also be used during opioid rotation. It has no known effect on the cardiac QT interval or drug-drug interactions involving hepatic cytochrome P450s enzymes. In these regards, levorphanol may offer a superior safety profile over methadone and other long-acting opioids. Despite its prospective value of multiple mechanisms of action and the potential for treating various types of pain, levorphanol use has been largely supplanted by other recently approved opioids. Its waning use over the years has caused it to be referred to as the “Forgotten Opioid” and resulted in what some consider its underutilization. In fact, levorphanol is relatively unfamiliar to most prescribers.

Dihydromorphine is a semi-synthetic opioid derived from morphine. dihydromorphine is a moderately strong analgesic and is used clinically in the treatment of pain and is also the active metabolite of dihydrocodeine. Dihydromorphine acts as an agonist at the μ-opioid (mu), δ-opioid (delta) and κ-opioid (kappa) receptors. Dihydromorphone is approved for clinical use in the United States, Europe, and Japan; and sold under the brand name Dilaudid. Similar to morphine, and other morphine derivatives, hydromorphone has a high potential for addiction and abuse and is listed as a Schedule II drug in the United States Controlled Substances Act of 1970 (and similarly regulated in other countries).

Normethadone is a derivate of opioid analgetic methadone, used as component of antitussive drops in Canada. Illicit drug.

Stibogluconic acid (Sodium stibogluconate) is the pentavalent antimonial compound used to treat leishmaniasis and is only available for administration by injection. Sodium stibogluconate is sold in the UK as Pentostam (manufactured by GlaxoSmithKline). Sodium stibogluconate was granted orphan drug designation for the treatment of cutaneous leishmaniasis by the US FDA in January 2007. It is available in the United States only through the Centers for Disease Control. Sodium stibogluconate is indicated for the treatment of various types of a protozoal infection called leishmaniasis, which may result from sandfly bites in tropical and temperate parts of the world. It is also investigated for use/treatment in cancer. The mode of action of sodium stibogluconate is not clearly understood. In vitro exposure of amastigotes to 500 mg pentavalent antimony/ml results in a greater than 50% decrease in parasite DNA, RNA protein and purine nucleoside triphosphate levels. It has been postulated that the reduction in ATP (adenosine triphosphate) and GTP (guanosine triphosphate) synthesis contributes to decreased macromolecular synthesis. Sodium stibogluconate was shown to specifically inhibit type I DNA topoisomerase from Leishmania donovani through the inhibition of the unwinding and cleavage of the supercoiled plasmid pBR322, and to stabilize topoisomerase and DNA covalent complexes but not calf-thymus topoisomerase I and Escherichia coli DNA gyrase. Sodium stibogluconate is also a potent inhibitor of PTPases Src homology PTPase1 (SHP-1), SHP-2, and PTP1B but not the dual-specificity phosphatase mitogen-activated protein kinase phosphatase 1. Sodium stibogluconate combined with IFN-alpha-2b (IFN-α) inhibited solid tumor cell line growth in vitro, in vivo it was well tolerated and augmented cellular immune parameters.