Hair Loss (Alopecia): Drug Therapy

Therapy target

Prevention of progression (progression) of alopecia.

Therapy recommendations

Therapy recommendations depending on the diagnoses (see below):

• Alopecia androgenetica (AGA).
  • Man:
    • Finasteride (5-α-reductase inhibitor); contraindicated (not allowed!) in women, children, and adolescents; minoxidil (vasodilator/drug that dilates blood vessels)Note: Men older than 45 years should have baseline PSA determined before initiating finasteride therapy.
  • Woman:
    • In hyperandrogenemia (excess of male sex hormones in women):
      • Oral antiandrogens (drugs that inhibit the action of male sex hormones): cyproterone acetate and chlormadinone acetate.
      • Antiandrogenic contraceptives (contraceptives).
      • Dexamethasone in adrenal hyperandrogenemia to reduce elevated DHEAS levels.
      • Antiandrogen and dexamethasone in combined ovarian and adrenal hyperandrogenemia.
      • Spironolactone in polycystic ovary syndrome (PCOS) with polymorphisms in androgen-related genes to reduce elevated serum androgen levels (in this case there is usually also hirsutism/increased terminal hair (long hair) in women, according to the male distribution pattern) [off-label use].
    • Without hyperandrogenemia: local therapy: 2% minoxidil solution/5% foam; 17α-estradiol or estradiol benzoate (hair tinctures).
• Alopecia areata: glucocorticoids, JAK1/2 inhibitor (tofacitinib; off-label use/use outside the indications or the group of people for which the drugs are approved by the drug authorities); individual remedy trial with diphencyprone (induces mild contact allergen), if necessary.
• Alopecia cicatrica (scarring alopecia): treatment of the underlying disease.
  • Frontal fibrosing alopecia (FFA): tofacitinib (JAK kinase inhibitor), oral (off-label use, i.e., prescription of a finished drug outside the use approved by drug regulatory authorities).
• Hypoestrogenemic effluvium (estrogen deficiency-related hair loss).
  • Topical (local/local): e.g., combination hair tonic of minoxidil 2%, estradiol 0.12%, finasteride 0.15%.
  • Systemic: substitution therapy with a natural estradiol and a progestin of the progesterone series; no norethisterone derivative.
• Diffuse acquired alopecia: finasteride (5-α-reductase inhibitor; administration in men only); minoxidil (vasodilator/vasodilator drug).
• See also under “Other therapy.”

Further notes

• Minoxidil (topical use) in women with AGA without hyperandrogenemia: continuous use is required because achieved result (hair weight and number of hairs) would otherwise revert to placebo level six months after treatment discontinuation.
• The Janus kinase (JAK) inhibitor tofacitinib, at an increased dose ( 10 mg twice daily; recommended dose: 5 mg twice daily) not approved in patients with rheumatoid arthritis (RA), resulted in partially fatal pulmonary emboli.
• The Pharmacovigilance Risk Assessment Committee (PRAC) of the European Medicines Agency (EMA) advises physicians to avoid daily doses of cyproterone above 10 mg if possible (risk of meningioma formation).

5-α-reductase inhibitors

• Mode of action of finasteride: irreversibly blocks the activity of 5α-reductase, in contrast, the binding affinity of finasteride to 5α-reductase-1 is relatively low, so that the enzyme is not irreversibly blocked; 5α-reductase-1 is produced esp. produced in the liver, brain, and sebaceous glands of the skin; this inhibits the conversion of testosterone to 5α-dihydrotestosterone (DHT) and reduces serum DHT concentrations (in serum and scalp) by up to 80%; after discontinuation of finasteride, DHT levels return to baseline levels within 14 daysEffects on scalp hair follicles: Prolongation of the shortened anagen phase and the house hair loss slowed or stopped.
• No influence on the testosterone effect
• Indications: Use in diffuse acquired alopeciaNote: Men older than 45 years should have baseline PSA determined before initiating finasteride therapy.
• Contraindications: Women, children and adolescents
• Side effects: Potency/ libido/ ejaculate ↓, testicular pain, gastrointestinal discomfort (abdominal pain; diarrhea, nausea), headache hypersensitivity reactions.
• Post-finasteride syndrome (PFS): symptoms that persisted for at least 3 months after discontinuation of treatment for androgenetic alopecia with 1 mg finasteride
  • Somatic symptoms
    • Gynecomastia, lethargy, fatigue, muscle atrophy, increased fat storage, loss of libido, erectile dysfunction, and depression; orgasmic disturbances,
  • Cognitive disorders
    • Severe memory loss, slow thought process
  • Mental disorders
    • Increased anxiety, affect inhibition, emotional lability, sleep disturbances, insomnia, suicidal ideation.

  Possible cause: the decrease in DHT levels could have effects on the expression of 5α-reductase.Therapy: transdermal substitution of dihydrotestosterone; antidepressants if necessary.

• Red-Hand.Letter:
  • Patients should be aware of the risk of sexual dysfunction (such as erectile dysfunction, ejaculatory dysfunction, decreased libido) and informed that these may persist for more than ten years after discontinuation of therapy.
  • Patients should be informed that mood changes (including depressed mood, depression, suicidal ideation) have been reported in association with finasteride treatment.

Caffeine

• In a noninferiority study, 210 men with androgenetic alopecia were treated for six months with a solution containing 0.2% caffeine or with minoxidil 5%: RESULT: There was non-inferiority of caffeine versus minoxidil with an increase in anagen rate of 10.6 versus 11.7% (p=0.574).
  • Frontal trichograms also showed an increase in anagen rate of 11.3 versus 11.9 percent (p=0.740)
  • Occipital trichograms showed increase in anagen rate for caffeine and minoxidil of 9.15 versus 11.1, percent (p=0.349)
• Mode of action of caffeine: phosphodiesterase inhibitor; raises intracellular cAMP levels, thereby increasing intracellular energy supply

Supplements (dietary supplements; vital substances)

Suitable dietary supplements should contain the following vital substances:

• Vitamins (vitamin A (retinol), biotin, vitamin D (calciferols), folic acid).
• Trace elements (iron, zinc)
• Fatty acids (polyunsaturated fatty acids)
• Other vital substances (beta-carotene, green tea polyphenols).