Penicillin G, also known as benzylpenicillin, is a penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It is administered intravenously or intramuscularly due to poor oral absorption. Penicillin G may also be used in some cases as prophylaxis against susceptible organisms. Microbiology Penicillin G is bactericidal against penicillin-susceptible microorganisms during the stage of active multiplication. It acts by inhibiting biosynthesis of cell-wall mucopeptide. It is not active against the penicillinase-producing bacteria, which include many strains of staphylococci. Penicillin G is highly active in vitro against staphylococci (except penicillinase-producing strains), streptococci (groups A, B, C, G, H, L and M), pneumococci and Neisseria meningitidis. Other organisms susceptible in vitro to penicillin G are Neisseria gonorrhoeae, Corynebacterium diphtheriae, Bacillus anthracis, clostridia, Actinomyces species, Spirillum minus, Streptobacillus monillformis, Listeria monocytogenes, and leptospira; Treponema pallidum is extremely susceptible. Adverse effects can include hypersensitivity reactions including urticaria, fever, joint pains, rashes, angioedema, anaphylaxis, serum sickness-like reaction.

Epinephrine is a sympathomimetic catecholamine. It acts as a naturally occurring agonist at both alpha and beta-adrenergic receptors. Three pharmacologic types have been identified: alpha 1-, alpha 2-, and beta-adrenergic receptors. Each of these has three subtypes, characterized by both structural and functional differences. The alpha 2 and beta receptors are coupled negatively and positively, respectively, to adenylyl cyclase via Gi or Gs regulatory proteins, and the alpha 1 receptors modulate phospholipase C via the Go protein. Subtype expression is regulated at the level of the gene, the mRNA, and the protein through various transcriptional and postsynthetic mechanisms. Through its action on alpha-adrenergic receptors, epinephrine lessens the vasodilation and increased vascular permeability that occurs during anaphylaxis, which can lead to loss of intravascular fluid volume and hypotension. Through its action on beta-adrenergic receptors, epinephrine causes bronchial smooth muscle relaxation and helps alleviate bronchospasm, wheezing and dyspnea that may occur during anaphylaxis. Epinephrine also alleviates pruritus, urticaria, and angioedema and may relieve gastrointestinal and genitourinary symptoms associated with anaphylaxis because of its relaxer effects on the smooth muscle of the stomach, intestine, uterus and urinary bladder. Epinephrine increases glycogenolysis, reduces glucose up take by tissues, and inhibits insulin release in the pancreas, resulting in hyperglycemia and increased blood lactic acid.

Aspirin is a nonsteroidal anti-inflammatory drug. Aspirin is unique in this class of drugs because it irreversibly inhibits both COX-1 and COX-2 activity by acetylating a serine residue (Ser529 and Ser516, respectively) positioned in the arachidonic acid-binding channel, thus inhibiting the synthesis of prostaglandins and reducing the inflammatory response. The drug is used either alone or in combination with other compounds for the treatment of pain, headache, as well as for reducing the risk of stroke and heart attacks in patients with brain ischemia and cardiovascular diseases.

Moprolol is a beta-adrenergic antagonist, or beta blocker, typically prescribed to treat hypertension, high blood pressure, angina pectoris, arrhythmias, anxiety, and glaucoma. Moprolol has been the subject for many clinical trials to study the effect moprolol has on both blood pressure and glaucoma. In clinical trials, Moprolol shows some effect on lowering blood pressure with no effects on the heart rate. Moprolol is currently off the market, most likely due to the manufacturer being in violation of US good manufacturing practices.

Broxaterol is a β2 adrenoreceptor agonist used for the treatment of respiratory disease. Broxaterol produced a significant clinical improvement, an increase in FEV1 and a decrease in supplemental anti-asthmatic drugs used in patients with reversible airflow obstruction and in asthmatic children. The increases in FEV1 versus baseline were significantly maintained after the end of the treatment. Prompt disappearance of the asthmatic attack with significant improvement in lung function was observed in children. In two long-term controlled trials, the respiratory effects of broxaterol nebulizer solution were significantly greater than placebo. Moreover, broxaterol by metered dose inhaler was more effective than salbutamol after 3 months follow-up, showing the absence of tachyphylaxis. In long-term clinical evaluation, broxaterol has been shown to be well tolerated, with an incidence of adverse reactions equal to or less than that reported in the literature for other beta 2-agonists. The side effects most frequently associated with broxaterol were tremor, nervousness, and palpitations.

Abediterol, a fast and long-acting β2-adrenoceptor agonist (LABA), is being developed by AstraZeneca, for the treatment of asthma and chronic obstructive pulmonary disease. The investigational drug is a long-acting beta2-agonist (LABA) that has a bronchodilator effect, relaxing the muscles around the airways. It is currently under development and is in Phase II clinical trials.

Solabegron (GW427353), a beta-3 adrenoceptor agonist, is in development with AltheRx (now Velicept Therapeutics) for the treatment of irritable bowel syndrome (IBS) and overactive bladder (OAB). Solabegron was discovered and first developed by GlaxoSmithKline. It was acquired by AltheRx, which merged with Velicept in 2015 to continue development of the program. Solabegron has been tested in over 800 study subjects in a twice-a-day formulation and demonstrated efficacy in the treatment of OAB as well as IBS. A once daily formulation designed to optimize patient convenience as well as efficacy has been developed and is currently being evaluated in a phase 2b dose ranging clinical trial. A Phase 2b dose ranging study with the twice daily formulation also began enrollment in Q1 2018.

Norbudrine (KWD2109) is a sympathomimetic drug. It is an active bronchospasmolytic agent. KWD2109 shows an in vitro bronchospasmolytic acitivity which is about 14 times better than that of KWD2025. In the in vivo tests or guinea pig bronchospasmolytic activity KWD2109 has an effect which is about 3 times that of KWD2025 after intraperitoneal and oral administration

Tigemonam is a dialkylazetidinone derivative patented by E. R. Squibb and Sons, Inc. as a beta-lactam agent useful for the treatment of bacterial infections. Of the orally active beta-lactams, tigemonam is one of the most potent, with a spectrum of activity similar to that of aztreonam and highly resistant to hydrolysis by the beta-lactamase enzymes. Tigemonam inhibits 90% of Escherichia coli, Klebsiella spp., Proteus spp., Salmonella spp., Haemophilus influenzae and Branhamella catarrhalis tested. In localized infections, tigemonam also demonstrated excellent in vivo activity. In acute pyelonephritis in mice caused by Escherichia coli or Proteus sp., tigemonam was very effective. In a rat lung model with Klebsiella pneumoniae, tigemonam was active with a median effective dose of 46 mg/kg compared with 160 mg/kg for cefaclor and over 200 mg/kg for amoxicillin.