Actions of Neutin-20 in details
Pharmacology: Pharmacodynamics: Mechanism of Action: Administered orally, Neutin-20 has a marked effect in severe forms of acne, which have proved insufficiently responsive to previous treatment. The mechanism of action of Neutin-20 has not yet been elucidated in detail, but it has been established that the improvement observed in the clinical picture of severe acne is associated with dose-related suppression of sebaceous gland activity and a histologically demonstrated reduction in the size of the sebaceous glands. Furthermore, a dermal anti-inflammatory effect of Neutin-20 has been established.
Pharmacokinetics: Time-related blood concentrations can be predicted on the basis of linear pharmacokinetics.
Absorption: Peak plasma concentrations (Cmax) of approximately 200-300 ng/mL have been achieved in healthy volunteers 3-4 hrs time to reach maximum plasma concentration (tmax) after administration of Neutin-20 40 mg.
Taking Neutin-20 with food increases bioavailability up to 2-fold relative to fasting conditions, probably as a result of easier absorption of this highly lipophilic medication. Furthermore, there is an overall decrease in fluctuations in systemic availability when Neutin-20 is ingested with food.
Distribution: Neutin-20 is extensively bound to plasma proteins (99.9%) with the result that the free active fraction of the substance is <0.1% of the total over a wide range of therapeutic concentrations. Albumin appears to be the major binding protein.
The volume of distribution of Neutin-20 is not known in humans since it is not available as an IV preparation.
Metabolism: Three (3) major metabolites have been identified in plasma: 4-oxo-Neutin-20, tretinoin (all-trans retinoic acid) and 4-oxo-tretinoin, which is rapidly formed following oral administration achieving peak concentrations of 100-140 ng/mL at about 2 hrs after administration of Neutin-20 40 mg. Other metabolites have been detected but are not completely identified, which also includes glucuronide conjugates.
Neutin-20 metabolites have shown biological activity in several in vitro tests. Thus, the observed clinical profile in patients could be the result of the pharmacological activity of Neutin-20 and its metabolites.
Since Neutin-20 and tretinoin (all-trans retinoic acid) are reversibly metabolised (interconverted), the metabolism of tretinoin is linked with that of Neutin-20. It has been estimated that 20-30% of an Neutin-20 dose is metabolised by isomerization.
Neutin-20 also isomerises in vivo via an alternative metabolic pathway to tretinoin (all-trans retinoic acid). Glucuronidation of the metabolites has not been conclusively demonstrated in humans but is strongly suggested by animal studies. Investigations in humans and dogs point to an enterohepatic recirculation of Neutin-20, which would contribute to the observed interindividual variability in plasma concentrations.
In vitro metabolism studies have demonstrated that several CYP enzymes are involved in the metabolism of Neutin-20 to 4-oxo-Neutin-20 and tretinoin. No single isoform appears to have a predominant role. CYP2C8, CYP2C9, CYP2B6 and possibly CYP3A4 appear to have the greatest contributions in the metabolism of Neutin-20 to 4-oxo-Neutin-20. CYP2C9, CYP2B6 and possibly CYP2C8, CYP3A4, CYP2A6 and CYP2E1 contribute to the metabolism of Neutin-20. CYP26 is also known to metabolise retinoids.
Elimination: Neutin-20 appears to be eliminated almost exclusively by hepatic metabolism and biliary excretion.
Following oral administration of Neutin-20, the elimination half-life (t½) of unchanged substance has ranged from 7-39 hrs (mean approximately 20 hrs) in both healthy volunteers and patients with cystic acne.
The mean elimination t½ of the 4-oxo-metabolite in patients with cystic acne is slightly longer (25 hrs, range: 17-50 hrs) than that of the parent substance.
Neutin-20 is a physiological retinoid and endogenous retinoid concentrations are reached within approximately 2 weeks following the end of Neutin-20 therapy.
Special Populations: Since Neutin-20 is contraindicated in patients with hepatic impairment, there is no information on the pharmacokinetics of the substance in this population.
Patients with Renal Impairment: In patients with severe renal insufficiency, treatment should be started at a lower dose (eg, 10 mg/day) and afterwards individually adjusted according to tolerability.
How should I take Neutin-20?
Follow all directions on your prescription label and read all medication guides or instruction sheets. Use the medicine exactly as directed.
Each prescription of Neutin-20 (Eqv-Absorica) must be filled within 7 days of the date it was written by your doctor. You will receive no more than a 30-day supply of Neutin-20 (Eqv-Absorica) at one time.
Always take Neutin-20 (Eqv-Absorica) with a full glass of water. Do not chew or suck on the capsule. Swallow it whole.
Follow all directions about taking Neutin-20 (Eqv-Absorica) with or without food.
Use Neutin-20 (Eqv-Absorica) (Eqv-Absorica) for the full prescribed length of time. Your acne may seem to get worse at first, but should then begin to improve.
You may need frequent blood tests.
Never share this medicine with another person, even if they have the same symptoms you have.
Store at room temperature away from moisture, heat, and light.
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Neutin-20 administration
Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Each prescription of Neutin-20 must be filled within 7 days of the date it was prescribed by your doctor. You will receive no more than a 30-day supply of Neutin-20 at one time.
Always take Neutin-20 with a full glass of water to prevent the capsule from melting in your esophagus (food pipe), causing irritation. Do not chew or suck on the capsule. Swallow it as quickly as possible.
Take Neutin-20 with food or milk.
Take this medication for the entire length of time prescribed by your doctor. Your acne may seem to get worse at first, but should then begin to improve.
To be sure this medication is not causing harmful effects, your blood may need to be tested often. Your liver function may also need to be tested. Visit your doctor regularly.
Never share this medicine with another person, even if they have the same symptoms you have.
Store at room temperature away from moisture, heat, and light.
Neutin-20 pharmacology
Neutin-20 is a retinoid, which when administered in pharmacologic dosages of 0.5 to 1.0 mg/kg/day, inhibits sebaceous gland function and keratinization. The exact mechanism of action of Neutin-20 is unknown.
Nodular Acne
Clinical improvement in nodular acne patients occurs in association with a reduction in sebum secretion. The decrease in sebum secretion is temporary and is related to the dose and duration of treatment with Neutin-20 (Neutin-20), and reflects a reduction in sebaceous gland size and an inhibition of sebaceous gland differentiation.
Pharmacokinetics
Absorption
Due to its high lipophilicity, oral absorption of Neutin-20 is enhanced when given with a high-fat meal. In a crossover study, 74 healthy adult subjects received a single 80 mg oral dose (2 x 40 mg capsules) of Neutin-20 (Neutin-20) under fasted and fed conditions. Both peak plasma concentration (Cmax) and the total exposure (AUC) of Neutin-20 were more than doubled following a standardized high-fat meal when compared with Neutin-20 (Neutin-20) given under fasted conditions. The observed elimination half-life was unchanged. This lack of change in half-life suggests that food increases the bioavailability of Neutin-20 without altering its disposition. The time to peak concentration (Tmax) was also increased with food and may be related to a longer absorption phase. Therefore, Neutin-20 (Neutin-20) capsules should always be taken with food. Clinical studies have shown that there is no difference in the pharmacokinetics of Neutin-20 between patients with nodular acne and healthy subjects with normal skin.
Table 2 : Pharmacokinetic Parameters of Neutin-20 Mean (%CV), N=74
| Neutin-20 2 x 40 mg Capsules | AUC0-∞ (ng
References
ReviewsThe results of a survey conducted on ndrugs.com for Neutin-20 are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Neutin-20. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.User reportsConsumer reported administrationNo survey data has been collected yetConsumer reviews
Information checked by Dr. Sachin Kumar, MD Pharmacology More about Neutin-20Clinician Information
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