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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Pharmacology: Pharmacodynamics:Mechanism of Action: Administered orally, Novacne 0.05% has a marked effect in severe forms of acne, which have proved insufficiently responsive to previous treatment. The mechanism of action of Novacne 0.05% 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 Novacne 0.05% 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 Novacne 0.05% 40 mg.
Taking Novacne 0.05% 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 Novacne 0.05% is ingested with food.
Distribution: Novacne 0.05% 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 Novacne 0.05% 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-Novacne 0.05%, 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 Novacne 0.05% 40 mg. Other metabolites have been detected but are not completely identified, which also includes glucuronide conjugates.
Novacne 0.05% 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 Novacne 0.05% and its metabolites.
Since Novacne 0.05% and tretinoin (all-trans retinoic acid) are reversibly metabolised (interconverted), the metabolism of tretinoin is linked with that of Novacne 0.05%. It has been estimated that 20-30% of an Novacne 0.05% dose is metabolised by isomerization.
Novacne 0.05% 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 Novacne 0.05%, 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 Novacne 0.05% to 4-oxo-Novacne 0.05% 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 Novacne 0.05% to 4-oxo-Novacne 0.05%. CYP2C9, CYP2B6 and possibly CYP2C8, CYP3A4, CYP2A6 and CYP2E1 contribute to the metabolism of Novacne 0.05%. CYP26 is also known to metabolise retinoids.
Elimination: Novacne 0.05% appears to be eliminated almost exclusively by hepatic metabolism and biliary excretion.
Following oral administration of Novacne 0.05%, 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.
Novacne 0.05% is a physiological retinoid and endogenous retinoid concentrations are reached within approximately 2 weeks following the end of Novacne 0.05% therapy.
Special Populations: Since Novacne 0.05% 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 Novacne 0.05%?
Novacne 0.05% comes with a patient information form and medication guide. It is very important that you read and understand this information. Be sure to carefully follow these instructions and ask your doctor if you have any questions.
Women of reproductive age must sign up for a pregnancy risk program called iPLEDGE™ in order to receive their Novacne 0.05% prescription each month. You can sign up on the internet (www.ipledge.com) or by telephone (1-866-495-0654). Be sure to ask your doctor if you have any questions about this program. It is very important that you understand and follow all of the requirements. You will not get another prescription unless you follow the instructions for the program.
Novacne 0.05% must not be taken by women of reproductive age unless two effective forms of contraception (birth control) have been used for at least 1 month before the beginning of treatment. Contraception must be continued during the period of treatment, which is up to 20 weeks, and for 1 month after Novacne 0.05% is stopped. Be sure you have discussed this information with your doctor.
If you are a woman who is able to have children, you must have 2 pregnancy tests before beginning treatment with Novacne 0.05% to make sure you are not pregnant. The second pregnancy test must be taken at least 19 days after the first test and during the first 5 days of the menstrual period immediately prior to beginning treatment. In addition, you must have a pregnancy test each month while you are taking Novacne 0.05% and one month after treatment is completed.
Swallow the capsule whole with a full glass (8 ounces) of water or other liquid. Novacne 0.05%(R) and its generic products should be taken with food. Novacne 0.05%(TM) may be taken with or without food. Do not crush, break, or chew the capsule.
It is very important that you take Novacne 0.05% only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance of side effects.
It is very important that you not share Novacne 0.05% with anyone else because of the risk of birth defects and other serious side effects.
Novacne 0.05%™ oral capsules should not be substituted with other forms of Novacne 0.05% (e.g., Novacne 0.05%®). Different brands may not work the same way. If you refill your medicine and it looks different, check with your pharmacist.
Dosing
The dose of Novacne 0.05% will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Novacne 0.05%. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
For oral dosage form (capsules):
For acne:
Adults and teenagers 12 years of age and older—Dose is based on body weight and must be determined by your doctor. The dose is usually 0.5 to 1 milligram (mg) per kilogram (kg) of body weight per day, divided and given in 2 doses. Your doctor may adjust your dose as needed.
Children younger than 12 years of age—Use and dose must be determined by your doctor.
Missed Dose
If you miss a dose of Novacne 0.05%, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Storage
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Novacne 0.05% 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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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 Novacne 0.05% 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 Novacne 0.05% at one time.
Always take Novacne 0.05% 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 Novacne 0.05% 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.
Novacne 0.05% 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.
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Mechanism of Action
Novacne 0.05% is a retinoid, which when administered in pharmacologic dosages of 0.5 to 1 mg/kg/day, inhibits sebaceous gland function and keratinization. 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 Novacne 0.05% and reflects a reduction in sebaceous gland size and an inhibition of sebaceous gland differentiation. The exact mechanism of action of Novacne 0.05% is unknown.
Pharmacodynamics
The pharmacodynamics of Novacne 0.05% are unknown.
Pharmacokinetics
Absorption
Due to its high lipophilicity, oral absorption of Novacne 0.05% is enhanced when given with a high-fat meal. Novacne 0.05% is bioequivalent to Novacne 0.05%® (Novacne 0.05%) capsule when both drugs are taken with a high-fat meal. Novacne 0.05% is more bioavailable than Novacne 0.05%® (Novacne 0.05%) capsules when both drugs are taken fasted; the AUC0-t of Novacne 0.05% is approximately 83% greater than that of Novacne 0.05%®. Novacne 0.05% is therefore not interchangeable with generic products of Novacne 0.05%®.
A single dose two-way crossover pharmacokinetic trial was conducted in 14 healthy adult male subjects comparing Novacne 0.05% 40 mg (1 x 40 mg capsules), dosed under fasted and fed conditions. Under fed conditions after a high-fat meal, it was observed that the mean AUC0-t and Cmax were approximately 50% and 26% higher, than that observed under fasting conditions (Table 2). The observed elimination half-life (T1/2) was slightly lower in the fed state versus fasted. The time to peak concentration (Tmax) increased with food and this may be related to a longer absorption phase.
Table 2: Pharmacokinetic parameters of Novacne 0.05% mean (%CV) following administration of 40 mg strength, N=14
Novacne 0.05%¶ (1 x 40 mg capsules)
AUC0-t
(ng x hr/mL)
Cmax
(ng/mL)
Tmax
(hr)
T1/2
(hr)
Fed
6095 (26 %)
395 (39 %)
6.4 (47 %)
22 (25 %)
Fasted
4055 (20 %)
314 (26 %)
2.9 (34 %)
24 (28 %)
Published clinical literature has shown that there is no difference in the pharmacokinetics of Novacne 0.05% between patients with nodular acne and healthy subjects with normal skin.
Distribution
Novacne 0.05% is more than 99.9% bound to plasma proteins, primarily albumin.
Metabolism
Following oral administration of Novacne 0.05%, at least three metabolites have been identified in human plasma: 4-oxo-Novacne 0.05%, retinoic acid (tretinoin), and 4-oxo-retinoic acid (4-oxo-tretinoin). Retinoic acid and 13-cis-retinoic acid are geometric isomers and show reversible interconversion. The administration of one isomer will give rise to the other. Novacne 0.05% is also irreversibly oxidized to 4-oxo-Novacne 0.05%, which forms its geometric isomer 4-oxo-tretinoin.
After a single 40 mg oral dose of Novacne 0.05% to 57 healthy adult subjects, concurrent administration of food increased the extent of formation of all metabolites in plasma when compared to the extent of formation under fasted conditions.
All of these metabolites possess retinoid activity that is in some in vitro models more than that of the parent Novacne 0.05%. However, the clinical significance of these models is unknown.
In vitro studies indicate that the primary P450 isoforms involved in Novacne 0.05% metabolism are 2C8, 2C9, 3A4, and 2B6. Novacne 0.05% and its metabolites are further metabolized into conjugates, which are then excreted in urine and feces.
Elimination
Following oral administration of an 80 mg dose of 14C-Novacne 0.05% as a liquid suspension, 14C-activity in blood declined with a half-life of 90 hours. The metabolites of Novacne 0.05% and any conjugates are ultimately excreted in the feces and urine in relatively equal amounts (total of 65% to 83%).
After a single 40 mg (2 x 20 mg) oral dose of Novacne 0.05% to 57 healthy adult subjects under fed conditions, the mean ± SD elimination half-lives (T1/2) of Novacne 0.05% and 4-oxo-Novacne 0.05% under fed states were 18 hours and 38 hours, respectively.
Special Patient Populations
The pharmacokinetics of Novacne 0.05% were evaluated after single and multiple doses in 38 pediatric patients (12 to 15 years) and 19 adult patients (≥18 years) who received Novacne 0.05% for the treatment of severe recalcitrant nodular acne. In both age groups, 4-oxo-Novacne 0.05% was the major metabolite; tretinoin and 4-oxo-tretinoin were also observed. There were no statistically significant differences in the pharmacokinetics of Novacne 0.05% between pediatric and adult patients.
References
DailyMed. "ISOTRETINOIN: 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).
NCIt. "Isotretinoin: 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).
EPA DSStox. "13-cis Retinoic acid: 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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