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Structural formula

Latin name of substance Isotretinoin
Isotretinoinum (genus Isotretinoini)
Chemical name:

13-cis-Retinoic acid
Gross formula:
Pharmacological group of substance Isotretinoin
Pharmacotherapeutic group: D10BA01 – means for systemic treatment of acne.

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Generic names:

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What Is Isotretinoin?

Isotretinoin (13-cis retinoic acid) is a vitamin-A derivative (retinoid). The liver naturally makes small amounts of isotretinoin from vitamin A, but the drug we prescribe is synthetically.

Isotretinoin was developed in the 1950s, but only started to be used in the mid-1970s. The original brand names were Accutane and Roaccutane, but there are now many generic versions on the market of varying potency.
What is isotretinoin used for?

Isotretinoin is a very effective drug for the treatment of acne. Originally licensed for use in severe disease, it is increasingly prescribed for all grades of acne.

Isotretinoin is also useful for other follicular conditions, such as:

Hidradenitis suppurativa
Scalp folliculitis

It is also prescribed for many other skin diseases. Examples include:

Discoid lupus erythematosus
Granuloma annulare
Grover’s disease
Extensive actinic keratosis
Prevention of squamous cell carcinoma
As an adjuvant in neuroblastoma

Contraindications to Isotretinoin

Isotretinoin must not be taken in pregnancy, or if there is a significant risk of pregnancy.

Blood donation by males and females isotretinoin is not allowed in case the blood is used for a pregnant woman.
Precautions when taking isotretinoin

Isotretinoin should be used with caution during breastfeeding.
Commercial pilots may be subject to flying restrictions if they take isotretinoin.
High dose of isotretinoin in very young children has been associated with premature epiphyseal closure, leading to shorter stature (not seen in low dose of acne treatment).

How does isotretinoin work

In acne, isotretinoin:

Reduces sebum production
Shrinks the sebaceous glands
Reduces follicular occlusion
Inhibits the growth of bacteria
Has anti-inflammatory properties

What is the usual dose of isotretinoin?

The range of doses used for every day for acne is less than 0.1 to over 1 mg / kg body weight. Some patients may only need a small dose once or twice a week. A course of treatment may be completed in a few months or continue for several years. For acne, some prescribers have targeted a total cumulative dose of 120-140 mg / kg, in the hope of reducing relapse, but the evidence for this is still controversial. The general trend has been to use lower dosages, unrelated to body weight (eg, 10 mg / day).

The individual dose prescribed by the dermatologist depends on:

Prescriber preference
Patient body weight
The particular condition being treated
Severity of the skin condition
Response to treatment
Other treatment used at the same time
Side effects experienced

Isotretinoin is better taken with water or milk after food to help with its absorption. It may be taken in the empty stomach, but absorption may be halved. There is no particular benefit in splitting the dose over the day. A newer formulation (isotretinoin-lidose) can be taken without food.

How long is isotretinoin taken?

Most patients should be treated until their skin condition clears and then for a further few months. However, courses have often been limited to 16-30 weeks (4-7 months) to minimize the risk of teratogenicity (risk of congenital abnormalities), and to comply with local regulatory authorities. Isotretinoin (otc) may be prescribed for years, usually in low dose or intermittently.
Drug interactions with isotretinoin

Care should be taken with the following medications:

Vitamin A (retinoic acid): Side effects are cumulative and could be severe. Beta-carotene (provitamin-A) is allowed.
Tetracyclines (including doxycycline, minocycline): These can increase the risk of headaches and blurred vision due to raised intracranial pressure.
Warfarin: Monitor the INR carefully.

What are the side effects and risks of isotretinoin?

The side effects of isotretinoin are dose dependent; At 1 mg / kg / day, almost all patients will have some side effects, whereas at 0.1 mg / kg / day, most patients will not. The range and severity of the side effects also depends on the personal factors and the disease being treated.

Patients with significant liver or kidney disease, high blood fats, diabetes and depression may be advised not to take isotretinoin or to receive a lower dose than usual and have regular follow-up visits.

Cutaneous and mucocutaneous side effects:

Most of the side effects due to isotretinoin are skin or mucocutaneous and relate to the mode of action of the drug. The most common are listed here. When side effects are troublesome, isotretinoin may need to be withdrawn or reduced.

Acne flare-up (especially if the starting dose is> 0.5 mg / kg / day)
Dry lips, cheilitis (sore, cracked or scaly lips) (100% of patients at 1 mg / kg / day)
Dry skin, fragile skin, eczema / dermatitis (itchy, red patches of skin).

Note: Atopic eczema may improve.
Increased sweating
Dry nostrils, epistaxis (nose bleeding)
Dry, watery or irritable eyes (especially in contact lens wearers), conjunctivitis, keratitis
Dry anal mucosa, bleeding at the time of a bowel movement
Dry genitals, dyspareunia (discomfort during intercourse)
Facial erythema
Sunburn is exposure to the sun
Temporary hair loss
Brittle nails
Skin infections: Impetigo, acute paronychia, pyogenic granuloma

Treatment of mucocutaneous side effects:

Reduce the dosage (eg, 5-10 mg / day)
Emollients, lip balm, petroleum jelly, sunscreen, eye drops and lubricants should be applied frequently and liberally when needed.
Dermatitis can be treated with topical steroids
Take short, cool showers without using soap
Use mild or diluted shampoo
Do not start wearing contact lenses for the first time
Do not have elective eye surgery while being isotretinoin or for 6 months afterwards.
Do not have ablative laser treatments (eg CO2 resurfacing) while isotretinoin or for 6 months afterwards. Other laser and light treatments may be performed with care
Shave rather than wax
Topical and / or oral antibiotics may be prescribed for impetigo

Other common-dose-related side effects of isotretinoin.

Myalgia (muscle aches) and arthralgia (joint aches), especially after exercise
Tiredness (lethargy and drowsiness)
Disturbed night vision and slow adaptation to the dark. Drivers may experience increased glare from car headlights at night
Hypertriglyceridemia (high levels of triglycerides in the blood), usually of no clinical relevance
Irregular or severe menstrual period

Rare side effects of Isotretinoin

Causality of the listed side effects may not have been confirmed
Severe headache with blurred vision due to raised intracranial pressure
Mood changes and depression. Note: Depression is more often related to the condition of the skin being treated or other health or psychosocial problems. Antidepressant medications may be helpful
Corneal opacities and cataracts
High-tone deafness
Accelerated diffuse interstitial scleral hyperoxosis (bony change)
Abnormal liver function tests or symptomatic hepatitis
Diarrhea or bleeding from the bowel
Allergy to isotretinoin causing liver disease and febrile illness

Treatment of systemic side effects:

Drink minimal alcohol
Take paracetamol for headache and for mild aches and pains
Seek medical attention early, if unwell

Monitoring isotretinoin
Pregnancy must be excluded before and during treatment with isotretinoin.

In an otherwise healthy individual, blood tests are generally not needed. However, consider the following if using high dose (1 mg / kg / day), prolonged courses (> 12 months), or if patients have specific risk factors (eg family history of dyslipidaemia, higher viral hepatitis risk, etc.):

Cholesterol and triglyceride levels
Liver function test
Blood count

Contraception in females considering isotretinoin

Isotretinoin must not be taken in pregnancy because of a very high risk of severe congenital abnormalities in the baby. Caution should be used during breast-feeding as it enters the breast milk and may affect the baby.

All females who could biologically have a child should take the following precautions during treatment with isotretinoin and for four weeks after the drug has been discontinued:

Abstinence The most reliable method of avoiding pregnancy is not to have sex. No method of contraception is completely reliable. “Natural” family planning is especially risky.
If sexually active, two reliable methods of contraception should be used. Discuss a contraception with your doctor (general practitioner, family planning specialist, gynaecologist or dermatologist). The combined oral contraceptive, IUD (intrauterine device), progesterone implant, or medroxyprogesterone injection may be appropriate.
The small-dose progesterone mini-pill is its own not recommended.

A prescription for emergency contraception may be available from a medical practitioner (GP or family planning clinic) or an accredited pharmacy. It prevents 85% of pregnancies if taken within 72 hours of unprotected sexual intercourse.

If contraception, termination of pregnancy (abortion) may be advised if pregnancy occurs during treatment with isotretinoin or within one month of discontinuing it.
What happens if a pregnant woman takes isotretinoin?

Isotretinoin has a very high chance of a spontaneous miscarriage or severe deformity if a fetus is exposed during the first half of pregnancy. The deformities affect the growth of the tissues developing at the time of exposure to the drug:

Cranium (skull and brain)
Eye, ear
No contraceptive precautions are necessary for men

Isotretinoin has no effect on sperm and male fertility and has not been shown to cause birth defects in children.
Does acne ever fail to clear isotretinoin?

Although isotretinoin is usually very effective for acne, occasionally it responds unexpectedly slowly and incompletely. Poor response is associated with:

Macrocomedones (large whiteheads)
Nodules (large, deep inflammatory lesions)
Secondary infection
Polycystic ovarian syndrome
Younger age (<14 years)

Options available to slow responders include:

Electrocautery of comedones
Prolonged course of isotretinoin
Additional treatment with oral antibiotics and oral steroids

Can Isotretinoin Be Used Again if Acne Recurs?

At least fifty percent of patients with acne have a long lasting response after a single appropriate course of isotretinoin. In others, acne may recur in a few months to a few years after the drug has been discontinued. Relapse is more common in females than in males, and in patients> 25 years of age. These patients may receive one or more further courses of isotretinoin.

Long-term treatment (> 1 year) is often used for patients with:

Persistent acne
Scalp folliculitis
Skin cancer

Special precautions for pilot considering isotretinoin

Good night vision is important for an airline pilot and those flying after dark. Night vision may be affected by isotretinoin. Pilots taking isotretinoin or considering a course of isotretinoin must report to their national aviation authority to discuss how this treatment affects their flying privileges.

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Precautions for the substance Isotretinoin

In the process of therapy, it is necessary to control the level of lipids, glucose, liver function. Patients with diabetes are encouraged to conduct more frequent monitoring of blood glucose.

Women of reproductive age need to apply reliable contraceptive measures 4 weeks before, during and for 1 month after the end of treatment. In case of pregnancy, it should be interrupted for medical reasons.

The treatment is stopped if there is colitis, visual impairment and symptoms of the pseudotumor of the brain. If a pseudo-tumor of the brain is suspected, a neurologic examination is performed.

Do not prescribe isotretinoin to patients receiving other drugs from the group of retinoids (to avoid hypervitaminosis A).

It is necessary to avoid high insolation, incl. UV therapy. Buy Accutane Online.

In the treatment of isotretinoin, a decrease in the tolerability of contact lenses is possible. Patients who wear contact lenses should wear eyeglasses in case of side effects.

Do not apply ointment on the skin around the eyes and with severe acute inflammation; Do not apply to mucous membranes.