Antidote activity

Quazepam (Doral) [C IV] [Sedative/Hypnotic/ Benzodiazepine] Uses Insomnia Action Benzodiazepine Dose 7.5-15 mg PO hs PRN i in elderly hqjatic failure Caution [X, /-] NA glaucoma Contra PRG, sleep apnea Disp Tabs SE Sedation, hangovCT, somnolence, resp depression Interactions T Effects W/ azole antifungals, cimetidine, digoxin, disulfiram, INH, levodopa, macrolides, neuroleptics, phenytoin, quinolones, SSRIs, verapamil, grapefruit juice, EtOH effects W/carbamazepine, rifampin, rifabutin, tobacco EMS Use caution w/ other benzodiazepines, antihistamines, opioids and verapamil, can T CNS depression concurrent EtOH and grapefruit juice use T CNS depression OD May cause profound CNS depression, confusion, bradycardia, hypotension, and altered reflexes flumazenil can be used as antidote activated charcoal may be effective... 

Potassium cyanide is a dangerously toxic substance. Ingestion of 100 to 150 mg can cause collapse and cessation of breathing in humans. At lower doses, the acute effects are nausea, vomiting, headache, confusion and muscle weakness (Patnaik, P. 1999. A Comprehensive Guide to the Hazardous Properties of Chemical Substances, ed. pp. 292-294. New York John Wdey Sons). Contact with acid can liberate highly toxic vapors of hydrogen cyanide. Sodium thiosulfate and sodium sulfate have shown antidotal activity to KCN toxicity. 

All the synthesized compounds were tested both in vivo on mice intoxieated by soman or tabun and in vitro on human erythrocyte AChE. In conclusion, nitro, sulfone, amino, and aminosulfonyl side-chain substituents caused high antidotal activity, where the optimum length of side-... 

Ivanusevic, M., Nikolic, S. and Trinajstic, N. (1991). A QSAR Study of Antidotal Activity of H-Oximes. Rev.Roum.Chim., 36,389-398. 

Knowing some of the major temptations that boredom can offer, parents can counter these risks by supporting antidote activities. 

Kassa makes a short overview of antidotal activity of the oxime reactivators of cholinesterase activity like antidote of OPC intoxications. 

In studying the mechanism of action of bisquatemary ammonium compounds upon mediator exchange in the vegetative nerve system, most attention has been concentrated on the part played by thiamine and panthothenic acid. The results obtained from these studies have shown that thiamine and calcium pantheonate as antidotes exert a certain positive effect in acute poisonings by one of the bisquatemary ammonium compounds, such as hexamethylen-bis-(4-nitrobenzene) chlorine ammonium. Calcium pantheonate has shown a high antidote activity. 

The introduction of inductors into the known combination of specific therapeutic agents (diethyxime ChR + atropine sulfate) results in its roused antidotic activity. In acute poisoning of rats with DDVP, IP increases from 5.5 to 7.0 in poisoning with furadane from 8.7 to 11.0. 

These also are direct capture agents for CN. The CN ion reacts with carbonyl groups to form cyanohydrins, resulting in a sequestering action. Among cyanohydrin formers, ct-ketoglutaric acid has shown some promise experimentally as a CN antidote (Hume et al, 1995 Moore et al., 1986), and there is a possible additional antidotal activity by causing a decrease in convulsions (Yamamoto, 1990). 

Note In Fig. 1 (left), crude plant extracts were used to detect antidote activity. In Table 2 B, the extracts were purer, and this presumably accounts for some observed differences in the position (RJ) and number of compounds detected. 

A. First screening test (TLC plate assay the test sample was equivalent to 250 mg of fresh plant material) Negative (except for weak antidote activity near the solvent front, presumably attributable to a-tocopheroi) ... 

Antidote activity Location of antidote on TLC plates (Rf) TLC solvent ... 

A preliminary screening test (TLC bioassay) for benzimidazole antidotes was carried out using 22 plant species, representing 18 plant families. As shown in Table 2 (A), out of the 22 plants tested, benzimidazole antidote activity was initially found only in Polygonum thunbergii (Polygonaceae). An aliquot, equivalent to 125 mg of fresh plant material, of the EtOAc soluble constituents from methanol extracts of P. thunbergii was sufficient to clearly show the antidote activity on a thin-layer plate [Table 2 (B)]. 

The relative antidote activity of various naturally occurring phenolics (17-21) and related compounds was examined using the TLC plate and paper... 

Fig. (7). Relative antidote activity of some classes of phenols on impregnated (20 nmol) paper disks against MBC contained in agar at 0.2 ppm.

Flavonofd compounds qualitatively tested for their antidote activity against MBC by TLC bloassay... 

Fig. (9). Threshold amounts of some flavones and a chromone exhibiting antidote activity (paper disk method).

Relationships Between Dosal Amount of MBC (12) and the Antidote Activity of Emodin (18)... 

Antidote Activity of Emodin Against Other Benzimidazole Fungicides... 

Although 5,7-dimethoxychromone (63) showed weak antidote activity against MBC (12) as described in PP. 472 and 473 (Fig. 7), another chromone derivative, 5-hydroxy-7-methoxychromone (64) synthesized in... 

Fungus tested Fungicide (dose ppm) Antidote activity of emodin (dose pg/disk)... 

Table 5. Antagonistic Effect of 5-Hydroxy-7-methoxychromone (64) on the Antidote Activity of 5-Methoxy-6,7-methylenedioxyf1avone (10) and Emodin (18) Against MBC (12)...

According to the results of Fujimura et al. [45], the minimum inhibitory concentrations (MICs) of MBC (12) and diethofencarb (15) for wild-type N. crassa were 0.2 ppm and >100 ppm, whereas for N. crassa F914 they were >100 ppm and 0.1 ppm, respectively. Therefore, an experiment using two combination systems, (1) benzimidazole-resistant strain + diethofencarb + emodin, and (2) benzimidazole-susceptible strain + MBC + emodin was carried out in order to obtain data on whether emodin could exhibit antidote activity in both systems. In this experiment, only emodin was used as an antidote because of the relatively weak activity of other antidotes in the interaction of MBC with wild-type N. crassa [44]. The results are summarized in Table 6, and indicate that emodin (18) can also act as an antidote against diethofencarb (15) in a benzimidazole-resistant strain of N. crassa. These and other results (Tables 4 and 6) are indicative of the versatility of emodin (18) as an antidote to the action of certain types of fungicide which possess an affinity for fungal P-tubulin, and may suggest that the antidote effect of emodin is closely linked to the function of P-tubulin. 

---