Procaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine. Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.

Noscapine (also known as Narcotine, Nectodon, Nospen, Anarcotine and (archaic) Opiane) is a benzylisoquinoline alkaloid from plants of the poppy family, without painkilling properties. This agent is primarily used for its antitussive (cough-suppressing) effects. Noscapine is often used as an antitussive medication. A 2012 Dutch guideline, however, does not recommend its use for coughing. Noscapine can increase the effects of centrally sedating substances such as alcohol and hypnotics. Noscapine should not be taken in conjunction with warfarin as the anticoagulant effects of warfarin may be increased. Noscapine, and its synthetic derivatives called noscapinoids, are known to interact with microtubules and inhibit cancer cell proliferation. Mechanisms for its antitussive action are unknown, although animal studies have suggested central nervous system as a site of action. Furthermore, noscapine causes apoptosis in many cell types and has potent antitumor activity against solid murine lymphoid tumors (even when the drug was administered orally) and against human breast and bladder tumors implanted in nude mice. Because noscapine is water-soluble and absorbed after oral administration, its chemotherapeutic potential in human cancer merits thorough evaluation. Antifibrotic effect of noscapine based on novel mechanism, which it shows through EP2 prostaglandin E2 receptor-mediated activation of protein kinase A.

An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. Papaverine is a vasodilating agent. Papaverine is used for the treating certain conditions that are accompanied by smooth muscle spasms (eg, blood vessel, urinary, gallbladder, or intestinal spasm). Papaverine is a nonxanthine phosphodiesterase inhibitor for the relief of cerebral and peripheral ischemia associated with arterial spasm and myocardial ischemia complicated by arrhythmias. The main actions of Papaverine are exerted on cardiac and smooth muscle. Like qathidine, Papaverine acts directly on the heart muscle to depress conduction and prolong the refractory period. Papaverine relaxes various smooth muscles. This relaxation may be prominent if spasm exists. The muscle cell is not paralyzed by Papaverine and still responds to drugs and other stimuli causing contraction. The antispasmodic effect is a direct one, and unrelated to muscle innervation. Papaverine is practically devoid of effects on the central nervous system. Papaverine relaxes the smooth musculature of the larger blood vessels, especially coronary, systemic peripheral, and pulmonary arteries. Papaverine is a potent, specific inhibitor of PDE10A. Papaverine for treatment of erectile dysfunction (ED) is excluded from coverage.

p-Chlorocresol (p-chloro-m-cresol; PCMC; brand name: Preventol CMK) possesses disinfectant and antiseptic properties. Chlorocresol is used in various preparations for skin disinfection and wounds. It also used as a preservative in creams and other preparations for external use which contain water. For use as a disinfectant such as a hand wash, it is commonly dissolved in alcohol in combination with other phenols. It is a moderate allergen for sensitive skin. Chlorocresol produces potentially life-threatening effects which include dermatitis, which are responsible for the discontinuation of chlorocresol therapy. The symptomatic adverse reactions produced by chlorocresol are more or less tolerable and if they become severe, they can be treated symptomatically, these include hypersensitivity reactions, irritation of eyes.

Azidocillin is a narrow-spectrum, semisynthetic penicillin derivative with antibacterial activity towards Grain-positive and Gram-negative microorganisms, including Haemophilus influenze, against which it is as effective as ampicillin. Azidocillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall, eventually causing cell lysis. Azidocillin can be applied in the treatment of inflammation of upper airways, middle ear, sinuses, throat, larynx and palatine tonsils. The substance is excreted with urine in 50-70% in the unchan¬ged form. It binds to the blood plasma proteins in 84%, and its half-life period is 30 min. The side effects are similar as those of benzylpenicillin but occur less frequently.

Propicillin (Baycillin Mega) is this semisynthetic penicillin, analogous to penicillin V, was introduced in the early 1960s. Although it is better absorbed from the gastrointestinal tract, overall it is inferior to phenoxymethylpenicillin and phenoxyethylpenicillin because of its lower antibacterial activity. Propicillin is used by propicillin-susceptible pathogens in adults and adolescents from 14 years to treat mild to moderate bacterial infections. These include skin infections, ear, nose and throat infections (such as otitis media, sinusitis, tonsillitis, pharyngitis) and infections of the bronchi andlung inflammation. Moreover propicillin can for prevention and treatment of scarlet fever or against rheumatic fever are used (bacterial infection of the nose and throat). Even with tooth or jaw surgery the drug is used to treat an endocarditis endocarditis prevent. Its mechanism of action could be due to binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, thus propicillin may inhibit the third and last stage of bacterial cell wall synthesis

Alcuronium (diallylnortoxiferine) is a semi-synthetic substance prepared from C-toxiferine I a bis-quaternary alkaloid obtained from Strychnos toxifera. Alcuronium is a neuromuscular blocking (NMB) agent, alternatively referred to as a skeletal muscle relaxant. Alcuronium is used for endotracheal intubation and to produce muscle relaxation in general anesthesia during surgical procedures. The pharmacological action of alcuronium is readily reversed by neostigmine, and it produced little histamine release. The major disadvantage of alcuronium is that it elicits a vagolytic effect produced by a selective atropine-like blockade of cardiac muscarinic receptors.

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.

Apalcillin is a naphthydridine derivative of ampicillin. Apalcillin has a broad spectrum of antibacterial activity that is very similar to that of piperacillin, except that apalcillin is significantly more active against Pseudomonas aeruginosa and Acinetobacter spp. Against Acinetobacter spp., apalcillin is uniquely active, compared to the other penicillins and comparison drugs. Strains producing high amounts of β-lactamases do become resistant to apalcillin. PAH (p-aminohippurate) clearance was significantly decreased during apalcillin infusion. Apalcillin appeared to compete with PAH for proximal tubular secretion but induced no further renal dysfunction.