Methylphenobarbital (INN), also known as mephobarbital and mephobarbitone (BAN), marketed under brand names such as Mebaral, Mephyltaletten, Phemiton, and Prominal, is a drug which is a barbiturate derivative and is used primarily as an anticonvulsant, but also as a sedative and anxiolytic. It is the N-methylated analogue of phenobarbital and has similar indications, therapeutic value, and tolerability.
Emylcamate is an anxiolytic and muscle relaxant. It was patented in the US in 1961 and advertised for the treatment of anxiety and tension. It was claimed to be superior to meprobamate, which would eventually replace emylcamate.
Proxymetacaine (INN) or proparacaine (USAN) is a topical anesthetic drug of the aminoester group.
Halazepam is a benzodiazepine derivative that was marketed under the brand names Paxipam in the United States, Alapryl in Spain, and Pacinone in Portugal.
Levomethorphan (LVM) (INN, BAN) is an opioid analgesic of the morphinan family that has never been marketed. It is the L-stereoisomer of racemethorphan (methorphan). The effects of the two isomers of racemethorphan are quite different, with dextromethorphan (DXM) being an antitussive at low doses and a dissociative hallucinogen at much higher doses. Levomethorphan is about five times stronger than morphine.
Methyprylon, or Noludar, is a sedative of the piperidinedione derivative family first developed by Hoffmann-La Roche. This medicine was used for treating insomnia, but is now rarely used as it has been replaced by newer drugs with fewer side effects, such as benzodiazepines.
Piritramide(R-3365, trade names Dipidolor, Piridolan, Pirium and others) is a synthetic opioid analgesic that is marketed in certain European countries including: Austria, Belgium, Czech Republic, Slovenia, Germany and the Netherlands. It comes in free form, is about 0.75x times as potent as morphine and is given parenterally for the treatment of severe pain. Nausea, vomiting, respiratory depression and constipation are believed to be less frequent with piritramide than with morphine, and it produces more rapid-onset analgesia when compared to morphine and pethidine. After intravenous administration the onset of analgesia is as little as 1–2 minutes, which may be related to its great lipophilicity. The analgesic and sedative effects of piritramide are believed to be potentiated with phenothiazines and its emetic (nausea/vomiting-inducing) effects are suppressed. The volume of distribution is 0.7-1 L/kg after a single dose, 4.7-6 L/kg after steady-state concentrations are achieved and up to 11.1 L/kg after prolonged dosing.
Bezitramide is an opioid analgesic. Bezitramide itself is a prodrug which is readily hydrolyzed in the gastrointestinal tract to its active metabolite, despropionyl-bezitramide. Bezitramide was discovered at Janssen Pharmaceutica in 1961. It is most commonly marketed under the trade name Burgodin.
Pyrovalerone is a central nervous system (CNS) stimulant that acts as a norepinephrine–dopamine reuptake inhibitor (NDRI). It was developed in the 1980s and had briefly been approved in Spain and France for chronic fatigue or lethargy and as an appetite suppressant, but was withdrawn from both markets around 2001 due to safety concerns including problems with abuse and dependence. It is closely related on a structural level to a number of other cathinone stimulants, such as α-PVP, MDPV and prolintane.
Haloxazolam, is a drug which is a benzodiazepine derivative. It has similar hypnotic properties as the benzodiazepine drugs triazolam, temazepam, and flunitrazepam and as such is indicated for the treatment of insomnia. A study in cats comparing estazolam and haloxazolam found that haloxazolam only affects gamma motor neurons, whereas estazolam affects both alpha and gamma motor neurons.
Chloralodol (Chlorhexadol) is a hypnotic/sedative. It is a Schedule III drug in the USA; however, it is not currently marketed in the United States so it is no longer prescribed.
Clonitazene is an opioid analgesic of approximately three times the potency of morphine. It is related to etonitazene, an opioid of significantly higher potency. Clonitazene is not currently marketed. It is a controlled substance; in the United States it is a Schedule I Narcotic controlled substance with a DEA ACSCN of 9612 and an established manufacturing quota of 25 grams for 2022.
Benactyzine is an anticholinergic drug that was used in the treatment of clinical depression and anxiety disorders before it was pulled from the U.S. market by the FDA due to serious side effects.
Veralipride (Agreal, Agradil) is an atypical antipsychotic of the benzamide class. It is used for the treatment of vasomotor symptoms associated with menopause. It is a D2 receptor antagonist and it induces prolactin secretion without any estrogenic or progestagenic effects. It was first authorised for use in 1979. However, Veralipride has never gained approval in the United States.
Etafedrine, sold under the brand name Nethaprin among others and also known as N-ethylephedrine, is a sympathomimetic agent used as a bronchodilator to treat asthma. It was previously commercially available as both the free base and as the hydrochloride salt from Sanofi-Aventis but is now no longer marketed.
Moperone (Luvatren, since discontinued) is a typical antipsychotic of the butyrophenone class which is marketed in Japan for the treatment of schizophrenia. It is an antagonist for the D2 (Ki 0.7–1.9 nM), D3 (Ki 0.1–1 nM), and 5-HT2A (Ki 52 nM) receptors. It also has a high binding affinity for the sigma receptors.
Cyclarbamate, also known as cyclopentaphene, is a muscle relaxant and tranquilizer of the carbamate family which has been marketed by Cassenne in France since 1961.
Mefexamide, also known as mefexadyne and mexephenamide, is a central nervous system stimulant that is no longer marketed.
Hydroxyphenamate or oxyfenamate is a sedative and anxiolytic drug of the carbamate class which is no longer marketed in the US. Like other carbamate sedatives, it is chemically related to meprobamate (Miltown). It was introduced to the US market in 1961. The dosage for adults is 200 mg 3 to 4 times daily.
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