Deoxy-Norephedrine Actions

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Actions of Deoxy-Norephedrine 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.
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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. Deoxy-Norephedrine 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 Deoxy-Norephedrine?

Using Deoxy-Norephedrine 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 Deoxy-Norephedrine in larger or smaller amounts or for longer than recommended.

Deoxy-Norephedrine may be habit-forming. Never share Deoxy-Norephedrine 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 Deoxy-Norephedrine 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 Deoxy-Norephedrine 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):

  • Keep the tablet in its blister pack until you are ready to take it. Open the package and peel back the foil. Do not push a tablet through the foil or you may damage the tablet.

  • Use dry hands to remove the tablet and place it in your mouth.

  • Do not swallow the tablet whole. Allow it to dissolve in your mouth without chewing. If desired, you may drink liquid to help swallow the dissolved tablet.

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.

Deoxy-Norephedrine 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. Deoxy-Norephedrine 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 Deoxy-Norephedrine in a sealed container or bag. Ask your pharmacist where to locate a community pharmaceutical take back disposal program.

Deoxy-Norephedrine administration

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.
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Oral:

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.

Deoxy-Norephedrine pharmacology

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.

12.3 Pharmacokinetics

Absorption

Following a single, 18.8 mg oral dose of Deoxy-Norephedrine in 29 healthy adult subjects in a crossover study under fasting conditions, d-Deoxy-Norephedrine and l-Deoxy-Norephedrine, 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 Deoxy-Norephedrine salts tablets. The relative bioavailability of Deoxy-Norephedrine compared to an equal dose of mixed Deoxy-Norephedrine salts IR tablets is 106% of d-Deoxy-Norephedrine and 111% for l-Deoxy-Norephedrine.

Metabolism and Excretion

Deoxy-Norephedrine contains d-Deoxy-Norephedrine and l-Deoxy-Norephedrine in a ratio of 3.2 to 1. Following a single 18.8 mg oral dose of Deoxy-Norephedrine in 29 healthy adult subjects under fasting conditions, the mean (± SD) plasma terminal elimination half-life of d-Deoxy-Norephedrine was 12.36 (± 2.95 h) hours and the mean (± SD) plasma terminal half-life for l-Deoxy-Norephedrine was 15.12 (± 4.40 h) hours. Deoxy-Norephedrine 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-Deoxy-Norephedrine or norephedrine, respectively. Norephedrine and 4-hydroxy-Deoxy-Norephedrine are both active and each is subsequently oxidized to form 4-hydroxy-norephedrine. Alpha-hydroxy-Deoxy-Norephedrine undergoes deamination to form phenylacetone, which ultimately forms benzoic acid and its glucuronide and the glycine conjugate hippuric acid. Although the enzymes involved in Deoxy-Norephedrine metabolism have not been clearly defined, CYP2D6 is known to be involved with formation of 4-hydroxy-Deoxy-Norephedrine. Since CYP2D6 is genetically polymorphic, population variations in Deoxy-Norephedrine metabolism are a possibility.

Deoxy-Norephedrine is known to inhibit monoamine oxidase, whereas the ability of Deoxy-Norephedrine 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 Deoxy-Norephedrine 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 Deoxy-Norephedrine 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 Deoxy-Norephedrine is recoverable in urine as derivatives of alpha-hydroxy-Deoxy-Norephedrine and approximately another 30% to 40% of the dose is recoverable in urine as Deoxy-Norephedrine itself. Since Deoxy-Norephedrine has a pKa of 9.9, urinary recovery of Deoxy-Norephedrine 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 Deoxy-Norephedrine 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 Deoxy-Norephedrine and result in prolonged exposures. In addition, drugs that affect urinary pH are known to alter the elimination of Deoxy-Norephedrine, and any decrease in Deoxy-Norephedrine’s metabolism that might occur due to drug interactions or genetic polymorphisms is more likely to be clinically significant when renal elimination is decreased.

Food Effect

In a study in adult volunteers to investigate the effects of a high-fat meal on the bioavailability of Deoxy-Norephedrine at a dose of 18.8 mg, the presence of food delayed the time to peak concentration of both d- and l-Deoxy-Norephedrine 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 Deoxy-Norephedrine by about 2% and decreased the AUC by 5-7% (5.7% decrease for d-Deoxy-Norephedrine and 7.4% for l-Deoxy-Norephedrine). These changes are not considered clinically significant.

Specific Populations

Pediatric

Following a single 10 mg oral dose of Deoxy-Norephedrine in 12 pediatric subjects with ADHD (aged 6-12 years) under fasting conditions, d-Deoxy-Norephedrine and l-Deoxy-Norephedrine 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-Deoxy-Norephedrine was 10.43 (± 2.01 h) hours and the mean plasma terminal half-life for l-Deoxy-Norephedrine was 12.14 (± 3.15 h) hours.

Alcohol Effect

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.


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References

  1. DailyMed. "AMPHETAMINE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. NCIt. "Amphetamine: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
  3. EPA DSStox. "Amphetamine: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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