What Is Dutasteride?

Dutasteride is a white crystalline solid chemical. The molecular formula is C ₂₇ H ₃₀ F ₆ N ₂ O ₂ , the molecular weight is 528.53000, the density is 1.303 g / cm ³ , and the melting point is 242-250ºC.

It is mainly used clinically for prostate enlargement, male pattern alopecia, seborrheic alopecia, hereditary alopecia (do not take for women and children).

Chinese name: Dutasteride
Foreign name: Dutasteride

CAS number: 164656-23-9
Chemical formula: C27H30F6N2O2
Molecular weight: 528.5297

Introduction to Dutasteride Compounds

Dutasteride Basic Information

Chinese name: Dutastilamine

English name: dutasteride

English alias: Avodart; Dutasteride; Duagen;

CAS number: 164656-23-9

Molecular formula: C ₂₇ H ₃₀ F ₆ N ₂ O ₂

Chemical structure:

Molecular weight: 528.53000

Exact mass: 528.22100

PSA: 58.20000

LogP: 6.97790 ^[1]

Physicochemical properties of Dutasteride

Appearance and properties: white crystalline solid

Density: 1.303 g / cm3

Melting point: 242-250ºC

Boiling point: 620.3ºC at 760 mmHg

Flash point: 329ºC

Refractive index: 1.523

Vapor pressure: 0mmHg at 25 ° C

Insoluble in water, soluble in ethanol (44mg / ml), methanol (64mg / ml), polyethylene glycol 400 (4mg / ml) ^[1] .

Dutasteride Classification Name

Primary classification: Urinary system drugs Secondary classification: Prostatic hyperplasia medication Third classification:

Dutasteride drug name

English name

Dutasteride

Drug alias

Avodart, Duagen

Dutasteride drug dosage form

Dutasteride tablets: 5mg / tablet.

Dutasteride pharmacological effects

Testosterone is converted into dihydrotestosterone by 5-reductase, which can promote the growth and development of the prostate. There are two subtypes of 5-reductase, namely type I isoenzyme and type II isoenzyme, of which type I isoenzyme has reproductive activity, and type II isoenzyme is involved in the conversion of testosterone in skin and liver. This product is a relatively specific 5-reductase inhibitor, which inhibits type and type 5-reductase isoenzymes through the formation of enzyme complexes, inhibits the conversion of testosterone into dihydrotestosterone (DHT), and then inhibits the male hormone dihydrotestosterone. Formation and therefore inhibits prostate growth in patients with benign prostatic hyperplasia (BPH). 0.5mg per day, this product reduces the DHT effect to a peak after 1-2 weeks of administration, and plasma DHT can be reduced by 85% to 90%. Patients with enlarged prostate take 5 mg per day, and DHT decreases significantly at 12 weeks.

Dutasteride Pharmacokinetics

This product is quickly absorbed orally, bioavailability is about 60%, oral 0.5mg, peak blood concentration in 2 ~ 3h, when taken with food, the peak concentration (Cmax) is reduced by 10% ~ 15%. The product exhibits a distribution volume of 300-500L, a plasma protein binding rate of 99%, and an 1-acid glycoprotein binding rate of 96.6%. The concentration of drug in semen of healthy volunteers was 3.4ng / ml, which was similar to plasma. After continuous use of this product for 6 months, the plasma drug concentration reached steady state. This product is extensively metabolized by liver cytochrome CYP3A4, mainly excreted in feces, of which 5% are unmetabolic drugs, 40% are metabolites, and less than 1% are unmetabolic drugs in urine. The elimination half-life of this product is about 5 weeks ^[2] .

Dutasteride indications

This product is mainly used for the treatment of patients with benign prostatic hyperplasia, which can improve the symptoms of BPH for a long time, and it can also reduce the incidence of prostate cancer.

Dutasteride contraindications

1. Patients with a previous history of allergies to this product and other 5-reductase inhibitors are contraindicated. 2. Patients with uncertain BPH (cancerous) may be disabled. 3. The reproductive toxicity of this product is X, pregnant women are prohibited.

Dutasteride notes

1. Don't donate blood within 6 months after stopping using this product. 2. There is no specific antidote for this product, and supportive treatment should be taken after drug overdose. 3. Patients taking this product should use the serum prostate specific antigen (PSA) index to detect prostate cancer, and should ask the doctor to fully consider the important factors that lead to the decline of serum PSA value when patients take this product ^[2] .

Dutasteride adverse reactions

Long-term treatment has a low rate of side effects. The most common adverse reactions are male and female breast development (including breast enlargement, breast tenderness), impotence, ejaculation disorders, and decreased sexual desire. Use with caution in patients with heart disease. This product is mainly metabolized by the liver, and those with impaired liver function should be used with caution. ^[3]

Dutasteride dosage

Orally, 5 mg each time, once per day.

Corresponding effects of dutasteride

1. This product is mainly metabolized by CYP3A4. The CYP3A4 inhibitors ritonavir, ketoconazole, verapamil, diltiazem, cimetidine, ciprofloxacin can slow the metabolism of this product. 2. This product is used in combination with tandoxol, terazosin, warfarin, digoxin, and cholestyramine, and their pharmacokinetics do not affect each other. 3. This product does not inhibit CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4 of liver cytochrome P450.

Dutasteride Additional Information

How safe is Dutasteride (Avodart)?

1. Dutasteride will cause a decrease in the number of spermatozoa, and it will continue for a considerable period of time. Even after the drug is stopped, the reduction of the number of spermatozoa will continue for a long time. Does Dutasteride cause infertility? There are no conclusions in the current FDA report. In terms of reduced sexual performance, the incidence is higher than 1 mg of Finasteride.

2. In addition, because there are many receptors for type 5 reductase in the brain in the human body, it is currently unknown what kind of long-term effects the inhibition of type 5 reductase has on the brain after taking Dutasteride. Finasteride is less relevant because it specifically inhibits type 5 reductase.

3. The US Food and Drug Administration FDA has currently allowed Dutasteride to be used in elderly people with prostate hypertrophy disease. Therefore, if you are over 50 years old, you have hair loss problems. Dutasteride (also known as Avodart Dutasteride) Use is considered.

4. The US FDA report mentions that: The amount of saliva or semen in men taking Dutasteride will not affect the development of embryos. However, pregnant women must not touch the ruptured Dutasteride capsules to avoid malformations of the fetus through absorption from the skin.