Isotretinoin – Product Information

Isotretinoin is a retinoid derivative of vitamin A used in the treatment of severe recalcitrant nodular acne. [R] 

The FDA authorized the first isotretinoin-containing product on May 7, 1982. It was most widely marketed under the generic Accutane (brand name), which has since been discontinued. [R] It is not possible to buy Accutane since the brand name has been discontinued. However, there are other brands of isotretinoin-containing products.

Isotretinoin is associated with significant risks during pregnancy and is therefore only available under the iPLEDGE program in the United States. [R]

Isotretinoin 

• CAS Number is stated as 4759-48-2
• Molar Mass is 300.442 g·mol−1
• It has a Chemical Formula of C20H28O2
• IUPAC Name:  (2Z,4E,6E,8E)-3,7-dimethyl-9-(2,6,6-trimethylcyclohexen-1-yl)nona-2,4,6,8-tetraenoic acid
• Also known by synonyms as 13-cis-retinoic acid

What is Isotretinoin?

The body produces isotretinoin, also known as 13-cis-retinoic acid, as a retinol (vitamin A) derivative by isomerizing tretinoin (all-trans-retinoic acid). [R] Isomerization is the process of changing a molecule into a new isomer; it can take either a cis or trans conformation. [R]

The US Food and Drug Administration (FDA) originally authorized oral isotretinoin (13-cis-retinoic acid) as a therapy for severe acne in 1982. [R] Its physical form or state is a solid form at 20°C with a melting point of around 172-177°C [R].

How does Isotretinoin work?

Isotretinoin works by reducing the size and activity of the sebaceous glands, which are responsible for producing oil in the skin. This can help to reduce the severity of acne. [R]

Isotretinoin is a highly effective therapy for acne as it impacts all of the major factors implicated in its development, including cell-cycle progression, cellular differentiation, cell survival, and apoptosis. It reduces sebum production, influences conidiogenesis, lowers surface and ductal propionibacterium acnes (P. acnes), and has anti-inflammatory properties. Its multifaceted mechanism of action makes it a successful treatment for severe acne that has not responded to other acne medicines. [R]

Isotretinoin Research

Research has been done to assess isotretinoin’s effectiveness and safety. For its potential benefits in treating a variety of other illnesses, isotretinoin has been well-researched. Several recent topics of tretinoin study are included below:

Isotretinoin and Acne Vulgaris

A study aimed to determine the efficacy of low-dose isotretinoin (20 mg/d) in the treatment of moderate acne. A total of 50 test subjects were enrolled, and good results were observed in 90.8% of test subjects aged 12 to 20 years and 89.6% of test subjects aged 21 to 35 years. Failure of treatment occurred in 5.2% and 7.4% of the two groups, respectively. During the 2-year follow-up period, relapses of acne occurred in a small percentage of test subjects, and elevated serum lipid levels and abnormal liver tests were observed in a small percentage of test subjects. The study concluded that low-dose isotretinoin is effective in treating moderate acne with a low incidence of severe side effects and at a lower cost than higher doses. [R]

Isotretinoin and Sebum Production

In a double-blind dose-response study, forty-eight test subjects with acne were treated orally with 13-cis-retinoic acid. The study found that there was a marked clinical improvement in the test subject’s acne, which was accompanied by a reduction in sebum excretion rate (SER) and production rate of free fatty acids (FFA). Furthermore, the study found that microbial numbers in the test subject’s acne skin decreased significantly, with the decrease in propionibacteria being greater than that of aerobic bacteria. It is important to note that the decline in micro-organisms occurred after the reduction in sebum and FFA production.

This suggests that the effect of the drug upon microorganisms is secondary to the change in sebum excretion, but it is nevertheless an important factor in the resolution of acne. Overall, the study suggests that the reduction in sebum and FFA production is the primary mechanism by which 13-cis-retinoic acid improves acne, with the reduction in microorganisms being a secondary effect. However, the decrease in microbial numbers is still an important factor in the resolution of acne. [R]

Isotretinoin and Androgen Production

Isotretinoin is a medication that is commonly used to treat severe acne. It works by reducing the size of the sebaceous glands in the skin, which helps to decrease the amount of oil released by the skin. Isotretinoin has been found to have different effects on precursor androgens, depending on the gender of the patient. In female test subjects, isotretinoin has been found to produce an elevation of free testosterone, which is a type of precursor androgen. However, it has no meaningful effects on other precursor androgens. In contrast, isotretinoin has been found to produce depressions in the serum levels of DHT and 3 alpha-diol G in female test subjects, as well as in 3 alpha-diol G in male test subjects. It is thought that these declines in precursor androgens are the outcome, not the cause, of the sebaceous glands becoming smaller. The magnitude of the observed decreases may represent the amount of tissue-derived androgens that sebaceous glands normally contribute to the circulating pool. This suggests that the reduction in precursor androgens is a secondary effect of isotretinoin treatment, rather than a direct effect on the production of androgens in the body.

Overall, the effects of isotretinoin on precursor androgens are complex and gender-dependent. While isotretinoin may produce an elevation of free testosterone in female test subjects, it appears to decrease the levels of other precursor androgens in both male and female test subjects. [R]

Isotretinoin and Folliculitis decalvans

This study aimed to determine the most effective dose and duration of oral isotretinoin monotherapy for achieving remission in folliculitis decalvans (FD) test subjects. The retrospective case series study included 39 male test subjects who received oral isotretinoin 0.1-1.02 mg/kg/day (10-90 mg/day) for a median duration of 2.5 months (range: 1-8 months). The study found that 82.0% of test subjects healed after the treatment, and patients that received oral isotretinoin ≥0.4 mg/kg/day for ≥3 months responded better, with 66% of them never relapsing. According to the study, oral isotretinoin monotherapy is a viable alternative therapy for FD that calls for additional study. [R]

Isotretinoin and Rosacea fulminans (pyoderma faciale)

A 3-year-old female test subject had severe acne-like lesions on her face that did not improve with various treatments, including antibiotics and corticosteroids. The lesions suddenly appeared on the cheeks and then rapidly spread to other areas of the face. Routine laboratory tests were normal, and bacterial cultures were negative. The test subject was initially treated with erythromycin, prednisolone, fluocinolone acetonide cream, and warm compresses, which resulted in moderate improvement. Isotretinoin was then prescribed at a dose of 10 mg daily, which led to significant improvement after 4 weeks and complete disappearance of the lesions after 8 weeks. The treatment with isotretinoin was continued for a total of 24 weeks, and the girl did not experience a relapse during the 1-year follow-up. [R]

Isotretinoin and Teratogenicity

Isotretinoin is a powerful medication used to treat severe acne, but it is also a teratogen, meaning it can cause birth defects in developing fetuses if taken during pregnancy. Research has shown that there is a significant risk of congenital defects in test subjects exposed to the drug in utero, with an estimated 20-35% risk. [R]

Additionally, studies have found that prenatal exposure to isotretinoin may also lead to neurocognitive impairment in test subjects, with around 30-60% of test subjects exposed to isotretinoin prenatally showing some form of cognitive impairment. [R]

Because of these risks, there are strict controls in place to ensure that isotretinoin is only prescribed to female test subjects who have no potential to become pregnant while taking the medication. Exposure to isotretinoin can lead to the termination of pregnancies due to the significant risk of birth defects. [R]

Isotretinoin and Mood Changes

Mood changes and depression are commonly reported among puberty-aged test subjects and test subjects with acne treated with isotretinoin. A recent controlled case cross-over study demonstrated a significant association between isotretinoin and depression, indicating a rare idiosyncratic reaction in some young vulnerable test subjects. The study demonstrated a relative risk for depression of 2.68 (95% CI = 1.03 to 3.89) for acne patients exposed to oral isotretinoin. This is the first controlled study to find a statistically significant association between isotretinoin and depression. [R]

Isotretinoin and Cancer

A solid pediatric tumor called neuroblastoma (NB) develops from undifferentiated neural cells. It continues to be one of the main causes of childhood cancer fatalities despite recent improvements in disease management and therapy, necessitating the creation of novel therapeutic agents and regimens. The vitamin A derivative retinoic acid (RA) is a potent substance that can promote differentiation in NB cells. Its isoform, 13-cis RA or isotretinoin, is utilized in NB therapy, although its efficacy is restricted to maintaining the progression of minimal residual disease. [R] It has been demonstrated that isotretinoin (13-cis-retinoic acid; 13-cisRA) dramatically increases survival for kids with high-risk neuroblastoma. [R]

Side Effects

It is known to have a number of side effects or symptoms, including dry skin, lips, and eyes, muscle, and joint pain, headaches, increased sensitivity to sunlight, changes in vision, mood changes, including depression and suicidal thoughts, hair loss or thinning, nosebleeds, increased cholesterol and triglyceride levels and liver damage. [R][R]

It is important to note that some of these side effects can be serious and require medical attention such as its known teratogenicity. [R]It is important to stop taking oral isotretinoin if known pregnant during treatment and users must undergo regular pregnancy tests. Additionally, some patients may experience an allergic reaction to the medication and should seek medical attention for other treatments.

Frequently Asked Questions (FAQs)

Half-life

Isotretinoin has a half-life of 16–20 hours and is undetectable in the serum after 4–5 days. [R]

Is it legal to use Isotretinoin?

The FDA permits the use of oral isotretinoin to treat severe nodular acne. [R]

Storage and Handling

Keep out of children’s reach. Do not store expired. The medication should be kept at room temperature in a closed container away from heat, moisture, and bright light. Avoid freezing. The gel form should not be exposed to fire or extreme heat since it is combustible. [R]

Store long-term at -20°C. [R]

Other Frequently Asked Questions (FAQs)

Is it safe during pregnancy? 

Due to its known teratogenicity, it is not safe during pregnancy as it can lead to severe birth defects. [R]

Is donating blood safe while on Isotretinoin?

Due to the teratogenic effects of isotretinoin, it is not advised to donate blood while taking the medication or within one month of stopping. For pregnant women, it can harm the fetus if it is transferred through donated blood. After taking isotretinoin, it’s important to follow the advised waiting period before giving blood.

Does isotretinoin raise the chance of becoming sunburned?

It’s crucial to be aware that isotretinoin may make your skin more sensitive to the sun if you want to spend a lot of time outside. Sunburns can occur suddenly and severely. [R]

How to safeguard skin when using isotretinoin?

Dermatologists advise isotretinoin users to safeguard their skin by looking for shade, putting on sun-protective clothing, and by applying sunscreen. [R]

Where to buy isotretinoin for sale? 

Behemoth Labz is the best place to buy isotretinoin online.

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Summary

The main purpose of the drug isotretinoin is to treat severe acne. It is a vitamin A derivative that lessens the quantity of oil that the skin’s oil glands produce. This helps to avoid clogged pores and the growth of zits and other acne lesions.

Orally administered isotretinoin is typically prescribed for a period of several months. The use of this powerful acne medicine, which has a variety of possible adverse effects, is often limited to severe acne cases that have not responded to previous therapies.

Isotretinoin frequently causes side effects such as dryness and peeling of the skin, dry eyes, nosebleeds, joint pain, and mood swings. It is crucial for women of reproductive age to utilize reliable birth control while taking isotretinoin because the drug can also result in birth abnormalities.

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