Sublingual Minoxidil for the Treatment of Male and Female Pattern Hair Loss

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• In this randomized, phase IB trial, 40 patients with androgenetic hair loss received 0.45 mg sublingual minoxidil (SM) or placebo daily for 24 weeks with 12 patients continuing into the 24-week open-label extension study with SM 1.35 mg or 4.05 mg daily. At 24 weeks, 45% of patients receiving 0.45 mg SM had improved frontal density and 55% had vertex improvement on macrophotography. There was a mean increase in terminal hair count/cm2 of 4 for the frontal area and 9 for the vertex scalp with 0.45 mg daily, of 10 and 26, respectively, with 1.35 mg daily, and of 38 and 88, respectively, with 4.05 mg daily. No significant change in blood pressure was detected in the placebo or treatment arms.

• SM produced a dose–dependent increase in mean terminal hair count of the frontal and vertex scalp and an improvement in hair density without affecting blood pressure.

–  Katherine M. Stiff, MD

Abstract 

Minoxidil is an approved medication for severe hypertension androgenetic alopecia.1 Oral minoxidil (OM) is a potent vasodilator used to treat hypertension. It is a pro-drug, activated by hepatic dehydroepiandrosterone sulfotransferase (SULT2A1) to minoxidil sulfate.2OM doses of 2.5 and 5 mg produced peak plasma concentrations of 16.8 and 37.2 ng/mL within 30 min post-dose.3 Side-effects include hypertrichosis, lower limb oedema, postural hypotension and tachycardia. Minoxidil lotion (ML) is approved for the treatment of hair loss. It is also a prodrug converted in hair bulbs by thermostable phenol sulfotransferase (SULT1A1) to minoxidil sulphate. There is a considerable inter subject variability in levels of both hepatic SULT2A1 and follicular SULT1A1. Low SULT1A1 predicts weak hair regrowth with both ML and OM.4,5 Weak hair growth due to low follicular SULT1A1 can be overcome with OM through dose escalation but cannot be overcome with ML due to low solubility and saturation absorption kinetics.6

Journal of the European Academy of Dermatology and Venereology: JEADV

Sublingual minoxidil for the treatment of male and female pattern hair loss: a randomized, double-blind, placebo-controlled, phase 1B clinical trial

J Eur Acad Dermatol Venereol 2021 Aug 22;[EPub Ahead of Print], L Bokhari, LN Jones, RD Sinclair 

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Benjamin Hidalgo-Matlock
Skin Care Physicians of Costa Rica

Clinica Victoria en San Pedro: 4000-1054
Momentum Escazu: 2101-9574

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