How is sertraline metabolized?

The metabolism of sertraline is mainly catalyzed by CYP3A4 and CYP2B6, with some activity accounted for by CYP2C19 and CYP2D6. Since sertraline is extensively metabolized, excretion of unchanged drug in the urine is a minor route of elimination, with 12-14% of unchanged sertraline excreted in the feces.

Is sertraline metabolized in the liver?

ZOLOFT is extensively metabolized by the liver. In patients with chronic mild liver impairment, sertraline clearance was reduced, resulting in increased AUC, Cmax and elimination half-life. The effects of sertraline in patients with moderate and severe hepatic impairment have not been studied.

What enzyme is sertraline metabolized by?

Sertraline is metabolized by multiple cytochrome P450 enzymes, monoamine oxidases, and glucuronyl transferases in human: an in vitro study. Drug Metab Dispos.

How long does it take for your body to absorb sertraline?

Sertraline is slowly absorbed after oral administration, with peak plasma concentrations at 6-8 h. Plasma concentrations are linearly related to dose. The elimination half-life is about 32 h; metabolism is by demethylation to an inactive metabolite.

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What is sertraline pharmacokinetics?

Sertraline is slowly absorbed, with peak concentrations (Cmax) occurring at 4-10 hours following ingestion, and has a half-life of 24-32 hours in children, adolescents and adults [Articles:2949057, 3624397, 8941024, 9549959, 11452243, 12218424, 16438795, 18397687, 22011692, 29723928].

Is sertraline metabolized by CYP?

The metabolism of sertraline is mainly catalyzed by CYP3A4 and CYP2B6, with some activity accounted for by CYP2C19 and CYP2D6. Since sertraline is extensively metabolized, excretion of unchanged drug in the urine is a minor route of elimination, with 12-14% of unchanged sertraline excreted in the feces.

Can sertraline affect the kidneys?

Sertraline is a selective serotonin reuptake inhibitor, or SSRI. Patients with advanced CKD are at significantly increased risk for developing depression and as well as serious complications of kidney disease, she added.

What does zoloft do to metabolism?

Currently, there doesn’t appear to be any evidence to show that sertraline has a negative effect on your metabolism. In one study from 2009, researchers found that sertraline did not have any significant impact on thyroid function, limiting any potential metabolic effects.

What happens if you drink on sertraline?

The FDA recommends avoiding alcohol consumption while using sertraline. This is because alcohol may worsen some of the side effects of sertraline and increase your risk of injuring or otherwise harming yourself while using sertraline to treat depression.

Where are SSRI absorbed?

Generally, SSRIs are well absorbed from the gastrointestinal tract, although systemic bioavailability may be limited by first pass metabolism.

What happens if a drug is not metabolized?

If your body metabolizes a drug too slowly, it stays active longer, and may be associated with side effects. Because of this, your doctor may characterize you as being one of four metabolizer types, with respect to a specific enzyme. Poor metabolizers have significantly reduced or non-functional enzyme activity.

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Does your brain go back to normal after antidepressants?

The process of healing the brain takes quite a bit longer than recovery from the acute symptoms. In fact, our best estimates are that it takes 6 to 9 months after you are no longer symptomatically depressed for your brain to entirely recover cognitive function and resilience.

Why do I metabolize drugs so fast?

Some drugs are chemically altered by the body (metabolized)… read more ) drugs slowly. As a result, a drug may accumulate in the body, causing toxicity. Other people metabolize drugs so quickly that after they take a usual dose, drug levels in the blood never become high enough for the drug to be effective.

Is sertraline excreted in urine?

Less than 1% of a dose of sertraline is excreted as the unchanged parent drug in the urine (1, 2, 4, 7). Sertraline undergoes extensive first-pass metabolism in the liver via demethylation to form the primary metabolite, desmethylsertraline (Figure 1).

Does Zoloft have active metabolites?

Desmethylsertraline, the active metabolite of sertraline, has a half-life of 56–120 hours and reaches peak plasma concentrations 8–10 hours following administration [11, 23–25].

How is Zoloft distributed?

Sertraline has a volume of distribution of 20 l kg1, and is approximately 99% bound to plasma proteins [10]. It undergoes sequential oxidation and conjugation in the liver and is excreted mainly as metabolites in urine and faeces [10]. The primary metabolite, N-desmethylsertraline, is formed by cytochrome P4503A4.