Cefsulodin is a third-generation of cephalosporin antibiotic with a narrow spectrum of activity. It has a specific activity against Pseudomonas aeruginosa. Cefsulodin’s targets are bacterial penicillin binding proteins. Drug is indicated for the treatment of infections of lower respiratory tract, skin and skin structures, urinary tract, bone and joint; treatment of gynecological infections; treatment of intra-abdominal infections; treatment of septicemia and CNS infections including meningitis caused by susceptible strains of specific microorganisms. Cefsulodin appears to be well tolerated and relatively free of any significant toxicity except for nausea and vomiting.

Etilefrine is a cardiac stimulant used as an antihypotensive. Intravenous infusion of this compound increases cardiac output, stroke volume, venous return and blood pressure in man and experimental animals, suggesting stimulation of both α and β adrenergic receptors. However, in vitro studies indicate that etilefrine has a much higher affinity for β1 (cardiac) than for β2 adrenoreceptors. Intravenous etilefrine increases the pulse rate, cardiac output, stroke volume, central venous pressure and mean arterial pressure of healthy individuals. Marked falls in pulse rate, cardiac output, stroke volume and peripheral bloodflow, accompanied by rises in mean arterial pressure, occur when etilefrine is infused after administration of intravenous propranolol 2,5 mg. These findings indicate that etilefrine has both β1 and α1 adrenergic effects in man. The French Health Products Agency concluded that etilefrine and heptaminol have an unfavourable harm-benefit balance, and also placed restrictions on the use of midodrine.

Bisantrene was classed as an anthracycline chemotherapeutic agent. It inhibits replication, kills tumor cells in clonogenic assays, and intercalates with DNA, where it inhibits both DNA and RNA synthesis. Bisantrene preferentially binds to A-T rich regions of DNA, where it effects changes to supercoiling and initiates strand breaks in association with DNA-associated proteins. This results from the inhibition of the enzyme topoisomerase II, which relaxes DNA coiling during replication and transcription. Toxicity studies in dogs and monkeys revealed that leukopenia, anorexia, diarrhea injection site necrosis, enterocolitis, muscle degeneration, and pulmonary edema were observed with high doses. Bisantrene was found to have less associated cardiotoxicity than other anthracenes. The existing data for bisantrene clearly demonstrated activity in acute myeloid leukemia, and in other indications including lymphoma, refractory breast cancer, and ovarian cancer.

Naftidrofuryl (INN), also known as nafronyl or as the oxalate salt naftidrofuryl oxalate or nafronyl oxalate, is a vasodilator used in the management of peripheral and cerebral vascular disorders. The drug act as a selective antagonist of 5-HT2 receptors. Naftidrofuryl is marketed under a variety of trade names, including Artocoron, Azunaftil, Di-Actane, Dusodril, Enelbin, Frilix, Gevatran, Iridus, Iridux, Luctor, Nafti, Naftoling, Naftodril, Nafoxal, Praxilene, Sodipryl retard, and Vascuprax. Praxilene belongs to a group of medicines known as ‘metabolic activators’. These are used to treat different types of blood circulation problems. Praxilene allows the body to make better use of the oxygen in your blood. Praxilene is used to treat the following symptoms: cramp-like pains; cramps in legs at night; severe pain in r legs when people are resting (rest pain); pale or blue fingers or toes which get worse when it is cold; numbness, tingling or burning feelings in the fingers or toes (Raynaud’s syndrome or acrocyanosis); open sores on the legs or feet (trophic ulcers); poor circulation caused by diabetes (diabetic arteriopathy).

Benapryzine is a dialkylaminoethanol ester of diphenylacetic acid. It is a muscarinic cholinoceptor antagonist with negligible peripheral effects. Benapryzine in addition to its anti-acetylcholine action antagonizes both maximal electroshock and metrazol-induced convulsions in mice. This feature is not generally shown by anti-acetylcholine agents but is seen with orphenadrine. Side effects of benapryzine were rare. They are: drowsiness, dry mouth, confusion, disorientation, hallucinations and postural syncope with measurable postural hypotension. Benapryzine has been used as an antiparkinsonian agent.

Debrisoquin is an antihypertensive drug having guanethidine-like properties, which inhibits monoamine oxidase (MAO) and does not enter the brain. Debrisoquine was used for the treatment of hypertension. Debrisoquine hydroxylation phenotype has been the most used test in humans to evaluate CYP2D6 activity. Two debrisoquine hydroxylation phenotypes have been described: poor and extensive metabolizers. A group with a very low debrisoquine metabolic ratio within the extensive metabolizers, named ultrarapid metabolizers, has also been distinguished. This CYP2D6 variability can be for a large part alternatively determined by genotyping, which appears to be of clinical importance given CYP2D6 involvement in the metabolism of a large number of commonly prescribed drugs.

Dequalinium is a quaternary ammonium cation commonly available as the dichloride salt. Dequalinium chloride has an antiseptic effect against a wide range of bacteria, yeasts, and some fungi and viruses. It kills the micro-organisms associated with various mild infections of the mouth and throat. Also, Dequalinium chloride is active against the bacteria which cause bacterial vaginosis. Dequalinium Chloride (DECA) is a PKC inhibitor and high-affinity blocker CNGA1 channel, and nearly as effective on heteromeric CNGA1+CNGB1 channels. Common side effects are: vaginal discharge; vaginal itching or vaginal burning; vaginal yeast infection (thrush); tender tongue.

Astromicin is an aminoglycoside antibiotic produced by Micromonospora spp. It is effective against major gram-negative bacterias such as Proteus, Serratia, Citrobacter, Enterobacter spp., Klebsiella, Escherichia coli and Staphylococcus aureus. Astromicin sulfate has been given by intramuscular injection or intravenous infusion. Side effects are: rash, urticaria, itch, erythema, fever, nausea, vomiting, and diarrhea. Combination with strong diuretics can cause nephrotoxicity and ototoxicity.

Anagestone acetate is a progestin medication, used in the 1960s in combination with the estrogen mestranol as a combined birth control pill. Toxicological study of chronic administration in dogs and monkeys showed the increased risk of developing malignant tumors in the mammary glands and a dose-dependent, nonprogressive decrease in hemoglobin and hematocrits. The drug was voluntarily withdrawn from the market in 1969.

In the US, Ethaverine is a member of the drug class peripheral vasodilators. It’s an alkaloid prepared synthetically from opium with no narcotic properties. Directly relaxes all smooth muscles, especially when they have been spasmodically contracted. Action is especially pronounced when spasm is present on coronary, cerebral, pulmonary, and peripheral arteries. Acts directly on myocardium like quinidine; depresses conduction and irritability, and prolongs refractory period. Primarily for peripheral and cerebral vascular insufficiency associated with arterial spasm; also a smooth muscle spasmolytic in spastic conditions of the GI and GU tracts. Adverse Effects ( 1%) CNS: Vertigo, headache, drowsiness. CV: Hypotension, arrhythmias. GI: Nausea, anorexia, abdominal distress, dry throat. Other: Malaise, flushing, sweating, lassitude, respiratory depression. Ethaverine may decrease levodopa effectiveness; morphine may antagonize smooth muscle relaxation effect of ethaverine.