Antihistamine
The vast majority of marketed H-antihistamines are receptor antagonists and only a minority of marketed compounds are inverse agonists at the receptor. Clinically, H-antihistamines are used to treat allergic reactions and mast cell-related disorders. Sedation is a common side effect of H-antihistamines that readily cross the blood–brain barrier; some of these drugs, such as diphenhydramine and doxylamine, are therefore used to treat insomnia. H-antihistamines can also reduce inflammation, since the expression of NF-κB, the transcription factor the regulates inflammatory processes, is promoted by both the receptor's constitutive activity and agonist (i.e., histamine) binding at the H receptor.
Aminoglutethimide
AG has many side effects and is a relatively toxic medication, although its side effects are described as usually relatively mild. The side effects of AG include lethargy, fatigue, weakness, malaise, drowsiness, somnolence, depression, apathy, sleep disturbances, stomach discomfort, nausea, vomiting ataxia, joint aches and pains, fever, skin rash, hypotension or hypertension, high cholesterol levels, virilization, hypothyroidism, thyroid abnormalities, elevated liver enzymes, jaundice, hepatotoxicity, weight gain, leg cramps, personality changes, blood dyscrasias, and adrenal insufficiency (e.g., hyponatremia, hypoglycemia, others). Lethargy is the most common side effect and has been found to occur in 31 to 70% of people treated with AG. It is the most common reason for discontinuation of AG. Skin rash and hypotension have both been observed in about 15% of people. At least one side effect will occur in 45 to 85% of people. Severe toxicity is seen in 10% of people, including circulatory collapse thought to be due to adrenal insufficiency. Hematological and bone marrow toxicity, including marked depression of white blood cell count, platelets, or both, occurs rarely, with an incidence of about 0.9%. It is usually seen within the first 7 weeks of treatment and resolves within 3 weeks following discontinuation. AG is discontinued in 5 to 10% of people due to intolerable side effects. The central nervous system side effects of AG are due to its nature as an anticonvulsant and relation to glutethimide.