Ethanol antihistamines

Motion sickness. Effective prophylaxis can be achieved with the parasympatholytic scopolamine (p. 106) and H antihistamines (p. 114) of the diphenyl-methane type (e.g., diphenhydramine, meclizine). Antiemetic activity is not a property shared by all parasympatho-lytics or antihistamines. The efficacy of the drugs mentioned depends on the actual situation of the in vidual (gastric filling, ethanol consumption), environ-... 

CNS effects Because of the rapid onset of action, eszopiclone should only be ingested immediately prior to going to bed or after the patient has gone to bed and has experienced difficulty falling asleep. Eszopiclone may produce additive CNS-depressant effects when coadministered with other psychotropic medications, anticonvulsants, antihistamines, ethanol, and other drugs that produce CNS depression. Eszopiclone should not be taken with alcohol. Dose adjustment may be necessary when eszopiclone is administered with other CNS-depressant agents because of the potentially additive effects. 

Kirchner s book 1127 gave an overview on the TLC of antihistamines, and Boonen 1128] also dealt with the separation of various antihistamines using plain silica and a mixture of ethanol/acetic acid/water (5 3 2). Recent experiments used metal ion impregnated silica layers to improve the separation of antihistamines 1129-1311. Antihistamines are easily visualised by iodine vapour. Separation of seven antihistamines on plain silica as well as metal ion impregnated silica with a benzene/butanol/acetic acid/water (7 8 5 2) mixture is shown in Table 10.18. Metal ion impregnation improved the separation of these antihistamines, especially when two or more stationary phases were used for parallel separations. 

A 30% ethanol extract of the Japanese valerian root ( Hokkai-Kisso ) extract (4.1 g/kg and 5.7 g/kg) and imipramine (20 mg/kg) also demonstrated statistically significant antidepressant effects compared to placebo as measured by the forced swimming test in rats (26). As in the Oshima study, kessyl glycol diacetate exhibited no antidepressant activity in the forced swimming test. Because the forced swimming test can be affected by stimulants, anticholinergics, and antihistamines as well as antidepressants, the effect of the valerian extract on reserpine-induced hypothermia, a test for antidepressant activity and inhibition of neuronal reuptake of monoamines, was measured. Both valerian (11.2 g/kg) and imipramine (20 mg/kg) reversed reserpine-induced hypothermia, suggesting that the antidepressant effect of valerian is caused by reuptake of monoamine neurotransmitters, as with conventional antidepressants. 

Additive CNS depression commonly occurs with other drugs, including antihistamines, ethanol, sedative-hypnotics, and opioids. 

Hydrochloride, CjjH CINjS, Nulrol, Sergetyi, mp 160-163", Soluble in water, ethanol, methanol, acetone, chloroform. Practically insol in ether. theraP CAT Antihistaminic, therap cat (vet) Tranquilizer. 

Drug Interactions Barbiturates combine with other CNS depressants to cause severe depression ethanol is the most frequent offender, and interactions with first-generation antihistamines also are common. Isoniazid, methylphenidate, and monoamine oxidase inhibitors also increase the CNS-depressant effects. Other prominent drag interactions occin as a result of the induction of hepatic drug-metabolizing enzymes by barbiturates see above). 

Drug interactions The most important drug interactions involving opioid analgesics are additive CNS depression with ethanol, sedative-hypnotics, anesthetics, antipsychotic drugs, tricyclic antidepressants, and antihistamines. Concomitant use of certain opioids (eg, meperidine) with MAO inhibitors increases the incidence of hyperpyrexic coma. Meperidine has also been implicated in the serotonin syndrome when used together with selective serotonin rcuptake inhibitors. 

A) Additive CNS depression will occur with ethanol and with over-the-counter antihistamines... 

A series of amidoximes including cetoxime (213) was patented as long acting antihistamines. The aminonitrile (212) reacted directly with hydroxylamine in ethanol to give (213) or could first be converted into the thioamide (214) Scheme 5.49.) [272]. 

I tat A, Stubbs D, Dunmore C, Ulliac N, Sexton B, Zieleniuk I, Irvii A, J ies W. Lack of interaction between two antihistamines, mizolastine and cetirizine, and ethanol in pi chomo-tor and drivii perfrnnance in healthy subjects. EurJ Clin Pharmacol (1995) 48, 143-50. 

Hughes FW, Forney RB Comparative effect of three antihistaminics and ethanol on mental and motor performance Clin Pharmacol Ther( 964) 5,414-21... 

Franks HM, Hensley VR, Hensley WJ, Starmer GA, Teo RKC The interacticm between ethanol and antihistamines 2 Clemastine MedJAust( 979) 1,185-6... 

Franks HH Lawrie M, Schabinsly VV, Starmer GA, Teo RKC Interaction between ethanol and antihistamines 3 mebhydrolin hJedJAust( 9Z ) 2,477-9... 

Individuals who have become sensitized by topically applied diphenhydramine can acquire a systemic eczematous contact dermatitis when diphenhydramine or any of the other ethanolamines listed in Table 5 is ingested or injected (Fisher 1973 It is not generally realized that dimenhydrinate (Dramamine) is an ethanol-amine (the chlorotheophylline salt of the antihistaminic agent diphenhydramine). Dimenhydrinate contains between 53% and 56% diphenhydramine and therefore should not be administered to any individual with allergic hypersensitivity to the ethanolamine group of antihistamines. 

Figure 4.19 The stabilizing and lytic effects of various tranquilizers and antihistamines on human erythrocytes. Stabilization of the erythrocytes against hypotonic haemolysis is caused by butyrylperazine dimaleate, prochlorperazine ethane disulphonate, fluphenazine diHCl, reserpine phosphate, thioridazine HCl, trifluoperazine diHCl, chlorpromazine HCl, promethazine HCl, and haloperidol. High concentrations of all the compounds caused direct lysis. Stabilization by chlorpromazine sulphoxide occurred at concentrations higher than equiosmolar concentrations of NaCl or sucrose. All the compounds were dissolved in aqueous solution except haloperidol which was added to the final aqueous solution from concentrated stock ethanolic solutions. The final concentration of the erythrocytes was 2.4 x 10 cells ml A relative haemolysis of 1.0 indicates an absolute degree of haemolysis of around 40%. From Seeman and Weinstein [158] with permission.

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