How long did you take this medication to work?
Actions of Benzolone in details
The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
Amphetamines stimulate the release of norepinephrine from central adrenergic receptors. At higher dosages, they cause release of dopamine from the mesocorticolimbic system and the nigrostriatal dopamine systems. Benzolone may also act as a direct agonist on central 5-HT receptors and may inhibit monoamine oxidase (MAO). In the periphery, amphetamines are believed to cause the release of noradrenaline by acting on the adrenergic nerve terminals and alpha- and beta-receptors. Modulation of serotonergic pathways may contribute to the calming affect. The drug interacts with VMAT enzymes to enhance release of DA and 5-HT from vesicles. It may also directly cause the reversal of DAT and SERT.
How should I take Benzolone?
Using Benzolone improperly can cause death or serious side effects on the heart.
Read all patient information, medication guides, and instruction sheets provided to you. Ask your doctor or pharmacist if you have any questions.
Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not use Benzolone in larger or smaller amounts or for longer than recommended.
Benzolone may be habit-forming. Never share Benzolone with another person, especially someone with a history of drug abuse or addiction. Keep the medication in a place where others cannot get to it. Selling or giving away this medicine is against the law.
You may take Benzolone with or without food. It is best to take this medicine first thing in the morning.
If your doctor changes your brand, strength, or type of stimulant medicine, your dosage needs may change. Use only the brand of Benzolone your doctor has prescribed.
Shake the oral suspension (liquid) well just before you measure a dose. Measure liquid medicine with the dosing syringe provided, or with a special dose-measuring spoon or medicine cup. If you do not have a dose-measuring device, ask your pharmacist for one.
To take the orally disintegrating tablet (Adzenys XR-ODT):
While using this medicine, your doctor will need to check your progress at regular visits. Your heart rate, blood pressure, height and weight may also need to be checked often.
Benzolone can cause unusual results with certain medical tests. Tell any doctor who treats you that you are using this medicine.
Store at room temperature away from moisture and heat. Keep the bottle tightly closed when not in use.
Keep track of the amount of medicine used from each new bottle. Benzolone is a drug of abuse and you should be aware if anyone is using your medicine improperly or without a prescription.
Throw away unused or expired Benzolone in a sealed container or bag. Ask your pharmacist where to locate a community pharmaceutical take back disposal program.
Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
Extended-release orally disintegrating tablet: Administer in the morning with or without food. Do not remove from blister until ready to administer. Using dry hands, peel backing off the blister; do not push tablet through foil. Remove tablet and immediately place on tongue and allow to disintegrate. Swallow with saliva. Do not chew or crush tablet.
Extended-release suspension: Administer in the morning with or without food; use the oral dosing dispenser provided. Administer directly into mouth from dispenser (do not add to food or mix with liquids); wash dispenser after each use. Shake bottle well prior to administration.
Immediate-release tablet: Administer with or without food; for short-term adjunct treatment of exogenous obesity, administer 30 to 60 minutes before meals. Administer the first dose on awakening; administer additional doses at intervals of 4 to 6 hours. Avoid late evening dosing.
Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
12.1 Mechanism of Action
Amphetamines are non-catecholamine sympathomimetic amines with CNS stimulant activity. The mode of therapeutic action in ADHD is not known. Amphetamines are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space.
Following a single, 18.8 mg oral dose of Benzolone in 29 healthy adult subjects in a crossover study under fasting conditions, d-Benzolone and l-Benzolone, the median (range) time to peak plasma concentrations (Tmax) were 4.0 (2 – 7) hours after dosing and peak concentration (Cmax) were 102% and 106%, respectively of the Cmax of immediate-release (IR) mixed Benzolone salts tablets. The relative bioavailability of Benzolone compared to an equal dose of mixed Benzolone salts IR tablets is 106% of d-Benzolone and 111% for l-Benzolone.
Metabolism and Excretion
Benzolone contains d-Benzolone and l-Benzolone in a ratio of 3.2 to 1. Following a single 18.8 mg oral dose of Benzolone in 29 healthy adult subjects under fasting conditions, the mean (± SD) plasma terminal elimination half-life of d-Benzolone was 12.36 (± 2.95 h) hours and the mean (± SD) plasma terminal half-life for l-Benzolone was 15.12 (± 4.40 h) hours. Benzolone is reported to be oxidized at the 4 position of the benzene ring to form 4-hydroxyamphetamine, or on the side chain A or B carbons to form alpha-hydroxy-Benzolone or norephedrine, respectively. Norephedrine and 4-hydroxy-Benzolone are both active and each is subsequently oxidized to form 4-hydroxy-norephedrine. Alpha-hydroxy-Benzolone undergoes deamination to form phenylacetone, which ultimately forms benzoic acid and its glucuronide and the glycine conjugate hippuric acid. Although the enzymes involved in Benzolone metabolism have not been clearly defined, CYP2D6 is known to be involved with formation of 4-hydroxy-Benzolone. Since CYP2D6 is genetically polymorphic, population variations in Benzolone metabolism are a possibility.
Benzolone is known to inhibit monoamine oxidase, whereas the ability of Benzolone and its metabolites to inhibit various P450 isozymes and other enzymes has not been adequately elucidated. In vitro experiments with human microsomes indicate minor inhibition of CYP2D6 by Benzolone and minor inhibition of CYP1A2, 2D6, and 3A4 by one or more metabolites. However, due to the probability of auto-inhibition and the lack of information on the concentration of these metabolites relative to in vivo concentrations, no predications regarding the potential for Benzolone or its metabolites to inhibit the metabolism of other drugs by CYP isozymes in vivo can be made.
With normal urine pHs approximately half of an administered dose of Benzolone is recoverable in urine as derivatives of alpha-hydroxy-Benzolone and approximately another 30% to 40% of the dose is recoverable in urine as Benzolone itself. Since Benzolone has a pKa of 9.9, urinary recovery of Benzolone is highly dependent on pH and urine flow rates. Alkaline urine pHs result in less ionization and reduced renal elimination, and acidic pHs and high flow rates result in increased renal elimination with clearances greater than glomerular filtration rates, indicating the involvement of active secretion. Urinary recovery of Benzolone has been reported to range from 1% to 75%, depending on urinary pH, with the remaining fraction of the dose hepatically metabolized. Consequently, both hepatic and renal dysfunctions have the potential to inhibit the elimination of Benzolone and result in prolonged exposures. In addition, drugs that affect urinary pH are known to alter the elimination of Benzolone, and any decrease in Benzolone’s metabolism that might occur due to drug interactions or genetic polymorphisms is more likely to be clinically significant when renal elimination is decreased.
In a study in adult volunteers to investigate the effects of a high-fat meal on the bioavailability of Benzolone at a dose of 18.8 mg, the presence of food delayed the time to peak concentration of both d- and l-Benzolone by approximately 1 hour (fed: median [range] 5 [3 – 8] hours vs. fasted: 4 [2 – 7] hours). Overall, a high-fat meal increased the average Cmax of both isomers of Benzolone by about 2% and decreased the AUC by 5-7% (5.7% decrease for d-Benzolone and 7.4% for l-Benzolone). These changes are not considered clinically significant.
Following a single 10 mg oral dose of Benzolone in 12 pediatric subjects with ADHD (aged 6-12 years) under fasting conditions, d-Benzolone and l-Benzolone peak plasma concentrations occurred at a median time of 3.9 and 4.5 hours after dosing, respectively. The mean plasma terminal elimination half-life of d-Benzolone was 10.43 (± 2.01 h) hours and the mean plasma terminal half-life for l-Benzolone was 12.14 (± 3.15 h) hours.
There is no in vivo study conducted for the effect of alcohol on drug exposure. An in vitro dissolution study showed alcohol-induced dose dumping potential in the presence of 40% alcohol. Dose dumping was not observed in the presence of lower alcohol concentrations.
ReviewsThe results of a survey conducted on ndrugs.com for Benzolone 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 Benzolone. 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.
Consumer reported administrationNo survey data has been collected yet
Information checked by Dr. Sachin Kumar, MD Pharmacology