1.Testosterone heptanoate or cyclopropionate
Usage: 150-200mg, intramuscular injection, once every 2 weeks or 75-100mg, once a week
Pharmacokinetic features: After a single intramuscular injection, serum testosterone levels rise to the superphysiological range and then gradually decline to the hypogonadal range at the end of the dosing interval
Dihydrotestosterone (DHT) and estradiol (E2) : The increase of DHT and E2 is directly proportional to the increase of testosterone; The ratio of DHT and T/E2 is constant
Advantages: Correct androgen deficiency symptoms; Self-administration is relatively inexpensive and the timing of administration is flexible.
Disadvantages: Requires intramuscular injection; There are peaks and troughs of serum testosterone.
2.Topical testosterone gel and axillary testosterone
Usage: Administration through small capsules, tubes and pumps.
Pharmacokinetic FEATURES: When administered at appropriate doses, this topical preparation restores serum T and E2 levels to normal male physiological levels.
Men with higher levels of DHT and E2 who received this transdermal patch had a higher T/DTH ratio than men with normal gonadal function.
Advantages: Correct androgen deficiency symptoms; The method of administration is flexible, easy to apply, and has good skin tolerance.
Disadvantages: Can be transmitted to female partners or children by direct skin contact; In a small proportion of treated men, skin allergies develop with relatively high DHT levels; There are inter-individual and intra-individual differences in T level.
3.Testosterone transdermal patch
Usage: 1-2 tablets, according to the design can be within 24 hours without external pressure area to provide 5-10 MGT
Pharmacokinetic characteristics: Serum T, DTH, and E2 levels were restored to normal male physiological range
DHT and E2: T/DTH and T/E2 levels are within the physiological range of males
Advantages: easy to apply, correct estrogen lack of physiological symptoms.
Disadvantages: Serum T levels may remain low to normal in some androgen deficient men, who may require a dose of two tablets per day; Skin irritation at the site of administration is often present.
4.Oral testosterone adhesive tablet
Usage: 30mg controlled release, biological adhesive tablets, twice a day
Pharmacokinetic characteristics: Absorption from buccal mucosa
DHT and E2: Normalize T or DTH levels in men with sexual dysfunction
Advantages: Corrects androgen deficiency in healthy men with low gonadal hormone levels
Cons: Gel-related adverse events occurred in 16% of treated men
5.Testosterone implants
Usage: 2-6 pellets implanted into SC, dose and protocol vary with preparation
Pharmacokinetic characteristics: serum T peak appeared in the first month and remained normal in 3-6 months, depending on different preparations
DHT and E2: T/DTH and T/E2 levels remain unchanged
advantages: correct androgen deficiency symptoms
Disadvantages: Need to surgically implant the ball, the ball has the risk of coming out
Vi. 17α-methyltestosterone
6.17α-methyltestosterone
Usage: This 17α-alkylating compound should not be used because of potential hepatotoxicity
Pharmacokinetic characteristics: oral activity
Disadvantages: Clinical responses vary; Potential hepatotoxicity
7.Oral administration of testosterone undecanoate
Usage: Oral 40-80mg twice a day or 3 times a day with meals
Pharmacokinetic characteristics: When treated with oil, it is absorbed into the portal system by lymphatic vessels, with great differences between individuals and within individuals
The levels of DHT and E2: T/DTH increased
Advantages: Oral administration is convenient
Disadvantages: Not yet commercially available in the United States, variable clinical response, variable serum T levels, high DTH/T
8.Long-acting undecanoate testosterone for injection
Usage: European dosing protocol: 1000mg intramuscular injection followed by 1000mg again after 6 weeks and 1000mg every 10 to 14 weeks thereafter
Pharmacokinetic profile: serum T levels remained normal in most treated men when 750 to 1000mg were administered intramuscular.
DHT and E2: DHT and E2 increased in equal proportion to serum T, while the ratio of T/DTH and T/E2 remained unchanged.
Advantages: Correction of androgen deficiency symptoms, no need for frequent administration.
Disadvantages: high dose intramuscular injection (4ml) is required, and cough occurs in a few patients after administration.
9.Testosterone adhesive matrix patch
Usage: 2X60cm2 patch can provide 4.8mgT/d
Pharmacokinetic characteristics: The levels of T, DTH and E2 reached the physiological range
The ratio of DHT and E2: T/DTH and T/E2 was within physiological range.
Advantage: Lasts 2 days
Disadvantages: Sometimes allergies occur
