Adverse drug reactions receptor

In general, the detection of adverse drug reactions early in the drug discovery process is becoming commonplace. So-called liability panels of receptors, hERG channel activity, and cytochrome enzymes are utilized to identify... 

Memantine is the first in a novel class of Alzheimer s disease medications acting a.o. on the NMDA receptor of the glutamatergic system. It also acts as an uncompetitive antagonist at different neuronal nicotinic receptors at potencies possibly similar to the NMDA receptor. Memantine is approved for treatment of moderate to severe Alzheimer s disease and its use is associated with a moderate decrease in clinical deterioration of the disease. Common adverse drug reactions (>1% of patients) include confusion, dizziness, drowsiness, headache, insomnia, agitation, and/or hallucinations. 

Sekine, Y., Rikihisa, T, Ogata, H., Echizen, H., and Arakawa, Y. (1999) Correlations between in vitro activity of antipsychotics to various central neurotransmitter receptors and clinical incidence of their adverse drug reactions. Eur J Clin Pharmacol 55 583— 587. 

Abbreviations NAT2, N-acetyltransferase 2 TPMT, thiopurine S-methyltransferase UGT1A1, UDP-glucuronosyltransferase 1A1 HER2, human epidermal growth factor receptor 2 (ErbB2) EICV, hepatitis C virus TCAs, tricyclic antidepressants ADRs, adverse drug reactions. 

Abbreviations CYP2D6, cytochrome P450 2D6 OPRMl, mu opioid receptor 1 ADR, adverse drug reaction. Data from Refs [53,60-62],... 

Estrogen receptor a variations increase or decrease the action of estrogens but, at present, no clinical studies are available that show that pharmacogenomic checking of ERa before estrogen-treatment (OCs or hormone replacement) can reduce the risk of adverse drug reactions. 

Cardiac function can be impaired by the action of drugs on specific receptors. To deal with every adverse reaction that is mediated via the effects of drugs acting on specific cardiac receptors is beyond the scope of this chapter. Among the most dominant membrane-bound receptors in the cardiac muscle that can contribute to adverse drug reactions are the p-adrenergic and cholinergic (muscarinic) receptors. 

In 2002,28 of 129 reports to the Australian Adverse Drug Reactions Advisory Committee of acute renal failure were associated with the combined use of ACE inhibitors or angiotensin II receptor antagonists. 

A patient may show a relatively serious adverse drug reaction that result from the drug s interaction with an off-target receptor. 

Meperidine is thought to inhibit both the 5-HT2A receptors and norepinephrine (NE) reuptake mechanism which may precipitate a serotonin syndrome, a toxic state secondary to excessive serotonin ago-nism of the CNS [3,4]. This adverse drug reaction occurs most commonly in patients who are using single or multiple medications that increase postsy-naptic serotonin levels. Inherited deficiencies in the metabolism of serotonin may contribute to the development of the syndrome. Hypertension, atherosclerosis, and hyperlipidemia are all associated with a reduction in endothelial MAO activity and thus a reduced capacity to metabolize serotonin may increase the risk of a serotonin crisis. The diagnosis... 

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