Oxomemazine is a histamine H₁-receptor antagonist. Additionally, oxomemazine could be classified as a ligand for M1 receptors. It is used in the symptomatic treatment of non-productive coughs that occur specifically at night.

Proxibarbal is a non-sedative barbiturate with a specific anti-serotonin and anti-histamine effect, due to enzyme induction of serotoninase and histaminase. Its lack of unpleasant side-effects. Proxibarbal exists in ring-chain tautomeric equilibrium with the two diastereomers of valofan. Proxibarbal is metabolized to a five-membered lactone. Its only barbituric property is its ability to induce enzymes that destroy a surplus of neurohormones and rid people of their neurovegetative sufferings, including migraine and other types of vascular headache. Side effects are: dizziness, drowsiness, dyspepsia, allergic reactions. Proxibarbal enhances the effects of other depriving agents, including alcohol.

Dihydromorphine is a semi-synthetic opioid derived from morphine. dihydromorphine is a moderately strong analgesic and is used clinically in the treatment of pain and is also the active metabolite of dihydrocodeine. Dihydromorphine acts as an agonist at the μ-opioid (mu), δ-opioid (delta) and κ-opioid (kappa) receptors. Dihydromorphone is approved for clinical use in the United States, Europe, and Japan; and sold under the brand name Dilaudid. Similar to morphine, and other morphine derivatives, hydromorphone has a high potential for addiction and abuse and is listed as a Schedule II drug in the United States Controlled Substances Act of 1970 (and similarly regulated in other countries).

The phthalidyl thiazolidine carboxylic ester of ampicillin, talampicillin (Talpen, Beecham), has been introduced recently to improve absorption and to reduce these side effects. After oral administration talampicillin is rapidly absorbed and hydrolysed by tissue esterases in the intestinal wall to release into the circulation ampicillin and the ester moiety, mainly 2-hydroxymethyl-benzoic acid. No unchanged talampicillin is detectable in the peripheral blood. It is not approved by the FDA for use in the United States

Bietaserpine is a derivative of a Rauwolfia alkaloid reserpine. It was used as an antihypertensive agent and marketed in the 1960s in France and Italy. Bietaserpine is believed to act by inhibiting VMAT receptors.

Lappaconitine is an alkaloid isolated from the root of Aconltitum sinomantanum Nakai. It has a strong analgesic activity that does not involve the opioid receptor. It was shown to have class-I antiarrhythmic action and irreversibly blocks cloned human heart (hH1) channels by binding to the site 2 receptor.

(R)-3'-hydroxybutyl (R)-3'-hydroxybutyrate or D-β-hydroxybutyrate ester is a is an effective and palatable precursor to the ketone body. Ketone bodies are the most energy-efficient fuel and yield more ATP per mole of substrate than pyruvate and increase the free energy released from ATP hydrolysis. Ketone diet containing (R)-3-hydroxybutyl (R)-3-hydroxybutyrate, improved physical performance and cognitive function in rats, and its energy-sparing properties suggest that it may help to treat a range of human conditions with metabolic abnormalities. It may be used to treat a condition which is caused by, exacerbated by or associated with elevated plasma levels of free fatty acids in a human or animal subject, for instance a condition where weight loss or weight gain is implicated, or to promote alertness or improve cognitive function, or to treat, prevent or reduce the effects of, neurodegeneration, free radical toxicity, hypoxic conditions or hyperglycaemia. It has been approved by the FDA as “Generally Regarded as Safe (GRAS)”.

Clomocycline is the approved name of a methylol derivative of chlortetracycline. Clomocycline is a tetracycline antibiotic that is commonly prescribed by medical doctors for infections and to treat acne. It may also be used to treat urinary tract infections, gum disease, and other bacterial infections such as gonorrhea and chlamydia. Clomocycline is also used commonly as a prophylactic treatment for infection by Bacillus anthracis (anthrax). It is also effective against Yersinia pestis and malaria and is also prescribed for the treatment of Lyme disease. Clomocycline inhibits cell growth by inhibiting translation. It binds to the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. The binding is reversible in nature. Clomocycline is lipophilic and can easily pass through the cell membrane or passively diffuses through porin channels in the bacterial membrane. This drug has been reported to be noticeably free of side-effects such as nausea, vomiting, and diarrhea.

Prednisolone 21-diethylaminoacetate, also known as Prednisolamate, is a synthetic corticosteroid used in combination with bronchodilator for treating respiratory disease.

Cytarabine ocfosfate (commercial name: Starasid) is a prodrug having stearyl group attached to phosphoric acid at 5' position of arabinose moiety of cytosine arabinoside (Ara-C). This drug is given orally. The mode of action is in the inhibition of DNA synthesis after conversion to Ara-CTP as in Ara-C. The drug is metabolized in the liver, producing the intermediate metabolite, C-C3PCA which is converted to Ara-C gradually. This property results in the maintenance of relatively long time the blood Ara-C levels. This was proved to be active clinically against acute leukemia and MDS.