Metampicillin is the approved name for the penicillin resulting from the reaction of ampicillin with formaldehyde. Metampicillin is hydrolysed in aqueous solution with the formation of ampicillin. Metampicillin has broad spectrum of activity coupled with a marked degree of stability to bacterial penicillinase. Furthermore, metampicillin is reported to be absorbed to a greater extent than ampicillin, resulting in superior blood levels in human subjects, and also giving high levels of antibiotic in bile following parenteral administration. Metampicillin showed a spectrum and level of activity similar to that of ampicillin in vitro, and both compounds were inactive against penicillinase-producing strains of bacteria. The activity of metampicillin was markedly reduced by human serum, and the compound was less active than ampicillin in the presence of human serum. Following the oral administration of metampicillin to man, metampicillin was not detected in the blood stream nor in urine, and ampicillin alone was demonstrated in these subjects. The serum concentrations of ampicillin that were produced following the oral administration of metampicillin were somewhat lower than those obtained with equivalent doses of ampicillin. Adminstration of metampicillin by the intramuscular (i.m.) route to volunteers resulted in the appearance of both ampicillin and metampicillin in the blood, and of ampicillin alone in the urine of these subjects. When parenteraly administered, metampicillin appeared to be a particularly suitable penicillin for the treatment of biliary tract infections. Metampicillin is a cell wall biosynthesis inhibitor.

Bumecaine (Pyromecaine) is a local anesthetic and anti-arrhythmic drug. It is indicated as an agent for superficial anesthesia during medical and diagnostic procedures in dentistry, ophthalmology, otorhinolaryngology, surgery, bronchology, gastroenterology, urology. The experiments on the isolated neurons in the rat spinal ganglions have shown that interaction of pyromecaine with inactivated Na+ channels makes a considerable contribution to the blocking effect of anesthesia. Oral administration of pyromecaine pills considerably depresses platelet aggregation and even causes platelet disaggregation. Possible side effects are: general weakness, nausea, vomiting, headache, dizziness, fainting, a drop in blood pressure. Quinidine increases the risk of side effects.

NELTENEXINE, an amide derivative of ambroxol and thiophenecarboxylic acid, is a mucolytic agent. It is an elastase inhibitor used in the treatment of human lung diseases.

Nepinalone is a new alchilaminate derivative of β-tetralone, which possess a non-opioid antitussive activity. Nepinalone racemus exerted a significant antitussive activity and both L- and D-isomers confirmed to possess a significant dose-correlated antitussive effect with better trend of activity for D-isomer, but not statistically significant. It was predicted to act via sigma receptors. Occasionally, episodes of gastric intolerance have been reported and rapidly receded when treatment was stopped. The use of doses higher than those recommended could cause drowsiness.

Picloxydine is a heterocyclic biguanide with antibacterial and antiplaque activity. 0.4% Picloxydine produces a highly significant drop in the number of aerobic organisms. 0.4% Picloxydine is far more effective than 0.2% Picloxydine or chlorhexidine in reducing the total viable count of oral aerobic and anaerobic organisms. It is used to treat superficial eye infections. Picloxydine is also used in eye drops in the topical therapy of trachoma. This drug can cause side effects - local intolerance reactions (temporary irritation, allergic reactions).

Epirizole (also known as Mepirizole) is a nonsteroidal anti-inflammatory drug developed for the treatment of such conditions as chronic rheumatoid arthritis. Although the drug was tested in a clinical trial, its current status is unknown and is supposed to be discontinued. Epirizole is known to be a duodenal ulcerogen, and its effect is mediated by generation of ROS.

Bumadizone is a non-steroidal anti-inflammatory drug exerting analgesic, antipyretic and anti-inflammatory properties. It has been studied in the treatment of rheumatoid diseases.

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.

Etodroxizine is a first-generation antihistamine of the diphenylmethane and piperazine classes. It is a sleep-inducing agent. Etodroxizine in combination with methaqualone had a somewhat stronger surpressive effect upon REM-sleep than methaqualone alone.

Etodroxizine is a first-generation antihistamine of the diphenylmethane and piperazine classes. It is a sleep-inducing agent. Etodroxizine in combination with methaqualone had a somewhat stronger surpressive effect upon REM-sleep than methaqualone alone.