Mifamurtide (liposomal muramyl tripeptide phosphatidylethanolamine; trade name Mepact) is an immunomodulator with antitumor effects that appear to be mediated via activation of monocytes and macrophages. After intravenous administration, mifamurtide is selectively phagocytosed by monocytes and macrophages. Cytosolic Mifamurtide specifically interacts with nucleotide-binding oligomerization domain 2 (NOD2) receptor that induces nuclear factor (NF)-kB activation and is implicated in innate immune defense. Activation of monocyte-mediated tumoricidal function was observed following in vivo treatment with mifamurtide in phase I/II clinical trials. Intravenous administration of mifamurtide inhibited tumor growth and increased survival in rodent models of lung and liver metastasis. In a large, randomized, open-label, multicenter, phase III trial, the addition of adjuvant (postoperative) mifamurtide to three- or four-drug combination chemotherapy (doxorubicin, cisplatin, and high-dose methotrexate with, or without, ifosfamide) was associated with a statistically significant improvement in overall survival in patients with newly diagnosed, high-grade, non-metastatic, resectable osteosarcoma. The pattern of outcome was generally similar in a small cohort of patients with metastatic disease who were enrolled in this trial. Mifamurtide is generally well tolerated; adverse events attributed to administration of the drug include chills, fever, headache, nausea, and myalgias. In the EU, mifamurtide is indicated in children, adolescents, and young adults for the treatment of high-grade, resectable, non-metastatic osteosarcoma after macroscopically complete surgical resection; it is administered by intravenous infusion in conjunction with postoperative multiagent chemotherapy. In the US, mifamurtide is currently an investigational agent that holds orphan drug status for the treatment of osteosarcoma.

Mefenorex or (+/-)N-(3-chloropropyl)-1-methyl-2-phenylethylamine is an N-alkylated analogue of amphetamine. The therapeutic efficacy of mefenorex as an adjunctive support in the treatment of obesity for limited periods of time, as well as its ability to be well tolerated, has been amply demonstrated. Mefenorex is considered to be racemic mixture, no available data regarding enantiospecific pharmacological activity of the compound.

Zimeldine was one of the first selective serotonin reuptake inhibitors to be marketed as an antidepressant under the brand names Zimeldine, Normud, and Zelmid. Zimelidine was developed in the late 1970s and early 1980s by Arvid Carlsson, who was then working for the Swedish company Astra AB. While zimelidine had a very favorable safety profile, within a year and a half of its introduction, rare case reports of Guillain–Barré syndrome emerged that appeared to be caused by the drug, prompting its withdrawl from the market.

Ethamsylate (2,5-dihydroxy-benzene-sulfonate diethylammonium salt) is a synthetic hemostatic drug indicated in cases of capillary bleeding. Ethamsylate acts on the first step of hemostasis by improving platelet adhesiveness and restoring capillary resistance. In addition it inhibits prostaglandin biosynthesis. Well-controlled clinical trials clearly showed the therapeutic efficacy of ethamsylate in dysfunctional uterine bleeding, with the magnitude of blood-loss reduction being directly proportional to the severity of the menorrhagia. Other well-controlled clinical trials showed therapeutic efficacy of ethamsylate in periventricular hemorrhage in very low birth weight babies and surgical or postsurgical capillary bleeding.

Dipyrone, also known as Metamizole (INN), is an ampyrone sulfonate analgesic, antispasmodic and antipyretic. It was withdrawn from US market in 1977 on the basis of reports of agranulocytosis. Depyrone is still used to treat severe and diffucult for relieving pains of different origin; headache, tooth-ache, pains in the joints, muscles, following traumas and operations, gall and kidney colics, neurites, neuralgias, traumatic cerebrasthenia; inflammation of upper respiratory ways of microbial or virus origin; chorea; febrile states. Mechanism of action of dipyrone is complex. It is believed that dipyrone exerts its action by inhibiting COX-3, and activates opioid and cannabioid systems either itself, or by products of its metabolic degradation.

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

Medifoxamine, an antidepressive drug, preferentially inhibits dopamine reuptake. It was marketed in France, but because of the hepatotoxicity, then was withdrawn.

Pyritinol is a semi natural analogue of water soluble vitamin B6. Pyritinol was synthetized way back in 1961 by Merck Laboratories. After years of research, it entered the market in the 1970s, where it was used for clinical applications – including treating stroke patients and those with Alzheimer’s. Since the 1990s, it has been sold as a nootropic dietary supplement in the United States and many other parts of the world. Pyritinol, unlike many other nootropics, has been approved for use as a medical treatment in countries around the world. Doctors in many European countries use Pyritinol to treat patients with chronic degenerative brain disorders – like dementia. Countries where Pyritinol is an approved treatment include Austria, Germany, France, Greece, Italy, and Portugal. France has approved the use of Pyritinol – but only as a treatment for rheumatoid arthritis. Pyritinol is not currently licensed for use in the United Kingdom, but in most other countries, it’s available online or through drug stores as an over the counter substance. Pyritinol is marketed under the brand names Encephabol, Encefabol and Cerbon 6. One of the known mechanisms of action of Pyritinol involves increasing choline uptake into your neurons and thereby increasing acetylcholine levels. Pyritinol is also a great effective precursor to dopamine, which is one of the neurotransmitter mood-boosters in the brain. Pyritinol has better conversion into the neurochemical. This drug increases dopamine, which can keep the brain from anxiety because a lower dopamine level is connected to mood disorders and depression.

Propiverine is a well established antimuscarinic agent. It’s indicated in adults for the symptomatic treatment of urinary incontinence and/or increased urinary frequency and urgency in patients with overactive bladder syndrome or neurogenic detrusor overactivity (detrusor hyperreflexia) from spinal cord injuries, e.g. transverse legion paraplegia. As well as blocking muscarinic receptors in the detrusor muscle, the drug also inhibits cellular calcium influx, thereby diminishing muscle spasm. Overdose with the muscarinic receptor antagonist propiverine hydrochloride can potentially result in central anticholinergic effects, e.g. restlessness, dizziness, vertigo, disorders in speech and vision and muscular weakness. Moreover, severe dryness of mucosa, tachycardia and urinary retention may occur.

Amezinium is a sympathomimetic used for its vasopressor effects in the treatment of hypotensive states. Amezinium inhibited monoamine oxidase (MAO) activity. Amezinium antagonized the response to tyramine and blocked neuronal uptake of noradrenaline. Side effects revealed are: palpitation, headache, nausea/vomiting, hot flashes, high blood pressure.