Coadministration of brivaracetam with carbamazepine may increase exposure to carbamazepine-epoxide, the active metabolite of carbamazepine, and could theoretically lead to reduced tolerability. (wikipedia.org)
3-Hydroxyisovaleric acid is also elevated in smokers, in subjects undergoing long-term anticonvulsant therapy with carbamazepine and/or phenytoin. (loinc.org)
Co-administration with carbamazepine may increase exposure to carbamazepine-epoxide, the active metabolite of carbamazepine. (com.bd)
Therefore, we investigated the potential capacity of zebrafish embryos/larvae to bioactivate two known mammalian proteratogens, carbamazepine (CBZ) and phenytoin (PHE) into their mammalian active metabolites, carbamazepine-10,11-epoxide (E-CBZ) and 5-(4-hydroxyphenyl)-5-phenylhydantoin (HPPH), respectively. (tpi.tv)
Some degree of distributional impairment at either the blood-CSF or the blood-brain barrier was indicated for 8 of the 11 remaining drugs (i.e., carbamazepine, midazolam, phenytoin, sulpiride, thiopental, risperidone, 9-hydroxyrisperidone, and zolpidem). (aspetjournals.org)
Phenobarbital1
The coadministration of phenytoin or phenobarbital will not affect plasma concentrations of calcitriol, but may reduce endogenous plasma levels of 25(OH)D 3 by accelerating metabolism. (rocaltrol.us)
Coadministration may increase active artesunate metabolite (DHA) by inhibiting UGT. (medscape.com)
Toxic metabolites3
Some drugs are converted to toxic metabolites by drug metabolizing enzymes. (hanstenandhorn.com)
For example, the analgesic acetaminophen is converted primarily to non-toxic metabolites, but a small amount is converted to a cytototoxic metabolite. (hanstenandhorn.com)
Sometimes toxic metabolites are also produced. (howmed.net)
Oxcarbazepine2
Population pharmacokinetics of oxcarbazepine active metabolite in Chinese paediatric epilepsy patients and its application in individualised dosage regimens. (usp.br)
Breastfeeding: Oxcarbazepine and its active metabolite MHO are excreted in human breast milk. (blogspot.com)
Recovered in the urine1
Brivaracetam is eliminated as urinary metabolites, with over 95% of a radioactive test dose recovered in the urine within 72 hours, including only 8.6% as unchanged brivaracetam. (wikipedia.org)
Inactive6
The three major metabolites (hydroxy, acid, and hydroxyacid) are pharmacologically inactive. (wikipedia.org)
As noted above, brivaracetam is primarily metabolized by hydrolysis, via amidase enzymes, to an inactive metabolite. (wikipedia.org)
After absorption, about 60% of the pharmacologically inactive R-form of ibuprofen slowly transforms into the active S-form. (bestpharmbuy.com)
70% is excreted in the urine (in the form of inactive metabolites) and 30% - with feces. (lekarstwo.ru)
Following absorption from the gastrointestinal tract, TKC is converted into several inactive metabolites. (sdrugs.com)
Most drugs are metabolized to inactive or less active metabolites by enzymes in the liver and intestine. (hanstenandhorn.com)
Sodium5
DILANTIN is available as 30 mg and 100 mg extended phenytoin sodium capsules. (nih.gov)
The rate of intravenous fosphenytoin sodium injection administration should not exceed 150 mg phenytoin sodium equivalents (PE) per minute in adults and 2 mg PE/kg/min (or 150 mg PE/min, whichever is slower) in pediatric patients because of the risk of severe hypotension and cardiac arrhythmias. (nih.gov)
Fosphenytoin sodium injection, USP can also be substituted, as short-term use, for oral phenytoin. (nih.gov)
Fosphenytoin sodium injection, USP should be used only when oral phenytoin administration is not possible. (nih.gov)
Active ingredients: Glucosamine sulfate in the form of D-glucosamine potassium chloride sulfate 250 mg, chondroitin sodium sulfate 1 200 mg ibuprofen 2 100 mg. (bestpharmbuy.com)
Concentrations5
Monitor unbound phenytoin concentrations in these patients. (nih.gov)
Some beta-blockers may increase the plasma concentrations of risperidone but not those of the active antipsychotic fraction. (mobilestores.org)
Tricyclic antidepressants may increase the plasma concentrations of risperidone but not those of the active antipsychotic fraction. (mobilestores.org)
Because Bivara can increase plasma concentrations of phenytoin, phenytoin levels should be monitored in patients when concomitant Bivara is added to or discontinued from ongoing phenytoin therapy. (com.bd)
Through the use of this approach, it appears that most CNS-active agents freely equilibrate across the blood-brain and blood-CSF barriers such that unbound drug concentrations in brain approximate those in the plasma. (aspetjournals.org)
Inhibitors of CYP2C9 can increase the risk of toxicity from phenytoin, tolbutamide, and oral anticoagulants such as warfarin. (hanstenandhorn.com)
Vitro4
In contrast, our in vitro drug metabolism assay showed that adult zebrafish metabolize both compounds into their active mammalian metabolites. (tpi.tv)
TKC is also active in vitro against a variety of fungi and yeast. (sdrugs.com)
The effect of bovine serum albumin (BSA) on human liver metabolism, in vitro , of 14 C-phenytoin (PHT) was studied. (aspetjournals.org)
Because phenytoin is principally bound to albumin, we also explored the effect of albumin on the V max and K m values obtained, in vitro . (aspetjournals.org)
Urine3
3-Hydroxyisovaleric acid is a normal human metabolite excreted in the urine. (loinc.org)
Up to 90% of the dose can be detected in the urine as metabolites and their conjugates. (bestpharmbuy.com)
After single intravenous administration of [ 3 H] caspofungin acetate, excretion of caspofungin and its metabolites in humans was 35% of dose in feces and 41% of dose in urine. (theodora.com)
Metabolism6
Pharmacokinetic data indicate that oral TKC inhibits the metabolism of astemizole, resulting in elevated plasma levels of astemizole and its active metabolite desmethylastemizole which may prolong QT intervals. (sdrugs.com)
These findings for phenytoin metabolism suggest that the addition of albumin to incubation media for slices or microsome experiments may yield K m estimates that are more representative of in vivo values. (aspetjournals.org)
The conformation of the active site of the enzyme is a key determinant of binding affinity ( K m ), so we also wanted to investigate metabolism in an intact cellular system in which the enzyme is maintained as close as possible to the environment in situ . (aspetjournals.org)
Inhibition of the metabolism of these prodrugs may reduce the amount of active drug formed, and decrease or eliminate the therapeutic effect. (hanstenandhorn.com)
As rate of metabolism is decreased, plasma levels of parent drug are increased while that of metabolites are low. (howmed.net)
Sulfonamides decrease the metabolism of phenytoin so that its blood levels become toxic. (howmed.net)
Enzymes1
Competition for the active sites takes place between the enzymes and the given drugs. (howmed.net)
The primary metabolite of PHT, pHPPH, is generated via cytochrome P450, so initial experiments were conducted with human liver microsomes. (aspetjournals.org)
Teraflex ® Advance is a combined preparation containing chondroitin sulfate, glucosamine sulfate and ibuprofen as active ingredients. (bestpharmbuy.com)
Serious, life-threatening, or fatal respiratory depression has been reported with the use of opioids, including codeine, one of the active ingredients in Promethazine with Codeine Oral Solution. (drugcentral.org)
Hepatotoxicity1
Monoacetylhydrazine is associated with hepatotoxicity via formation of a reactive intermediate metabolite when N-hydroxylated by the cytochrome P450 mixed oxidase system. (illumina.com)
Enzyme1
Enzyme induction leads to a decreased levels of the parent dug and increased levels of metabolites. (howmed.net)
Epilepsy3
In 1940, phenytoin (PHT) was found to be an effective drug for the treatment of epilepsy, and since then it has become a major first-line antiepileptic drug (AED) in the treatment of partial and secondarily generalized seizures. (medscape.com)
In this study the anticonvulsant actions of norfluoxetine and fluoxetine were studied and compared to those of phenytoin and clonazepam in pentylenetetrazol-induced mouse epilepsy models. (unideb.hu)
Pretreatment with fluoxetine or norfluoxetine (20 mg/kg s.c.), as well as phenytoin (30 mg/kg s.c.) and clonazepam (0.1 mg/kg s.c.) significantly increased both the rate and duration of survival, demonstratinga significant protective effect against pentylenetetrazol-induced epilepsy. (unideb.hu)
Dose2
NCT04845646 was an open label, DDI study to evaluate effect of itraconazole (CYP3A strong inhibitor) and phenytoin (CYP3A strong inducer) on PK of ASC41 following a single dose of 5 mg ASC41 tablet and PK in NAFLD patients. (ascletis.com)
Because the half-life of clorazepate and its active metabolite are long, timing breastfeeding with respect to the dose is of little or no benefit in reducing infant exposure. (drugs.com)
Exposure1
Prenatal exposure to phenytoin may increase the risks for congenital malformations and other adverse developmental outcomes. (nih.gov)
Ethanol1
The kinetics characteristic of elimination of ethanol and high doses of phenytoin and aspirin is known as A. Distribution B. Excretion C. First-pass effect D. First-order elimination E. Zero-order elimination 13. (kupdf.net)
Acute1
E.g. acute paracetamol toxicity is due to one of its metabolites. (howmed.net)
Compound1
The biomarkers discussed are for the parent compound and the metabolites. (cdc.gov)
Ingredient2
Amiodarone hydrochloride, the active ingredient in Pacerone® Tablets, is a benzofuran derivative: 2-butyl-3-benzofuranyl 4-[2-(diethylamino)-ethoxy]-3,5-diiodophenyl ketone hydrochloride. (rxlist.com)
1 ml of solution contains calcium folinate equivalent to 10 mg of folinic acid as active ingredient. (janusinfo.se)
Patients2
PK of ASC41-A, the active metabolite of ASC41, was comparable among US and Chinese healthy subjects and NAFLD patients. (ascletis.com)
A small number of drugs are not active in the form administered to patients. (hanstenandhorn.com)
Plasma1
Unbound fractions in mouse brain and plasma were determined for 31 structurally diverse central nervous system (CNS) drugs and two active metabolites. (aspetjournals.org)
Substance1
Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. (medicines.org.uk)
Primary1
Clorazepate is a prodrug of nordiazepam (desmethyldiazepam) which is the primary active metabolite of diazepam. (drugs.com)