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Indications

Minoxidil, also known as 2,4-pyrimidinediamine,6-(1-piperidinyl)-, 3-oxide, was initially developed as a potent peripheral vasodilator agent for treating severe refractory hypertension. However, owing to the significant adverse effects of oral minoxidil use, this drug is currently used only for patients with resistant hypertension who do not adequately respond to the maximum doses of 3 different antihypertensive medications.

Furthermore, approximately one-fifth of patients undergoing oral minoxidil treatment developed hypertrichosis. In 1987, a topical formulation of minoxidil was developed to treat androgenic alopecia, initially targeting males and later expanding its use to include females. This topic focuses on the clinical application of topical minoxidil therapy for androgenic alopecia and oral minoxidil therapy for resistant hypertension.[1][2]

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Topical minoxidil is available in both liquid solution and foam formulations. The liquid form of topical minoxidil contains alcohol and propylene glycol, the 2 crucial molecules that help dissolve the drug in a patient’s body, facilitating tissue absorption. Formulations containing 2% and 5% minoxidil commonly treat scalp alopecia in individuals aged 18 and above. Long-term use of minoxidil is necessary to uphold the achieved clinical outcomes of the medication, as these effects diminish when the drug is discontinued.[3][4]

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Topical Minoxidil

Androgenic alopecia is the only indication approved by the U.S. Food and Drug Administration (FDA) for topical minoxidil.

Off-label uses of topical minoxidil are as follows:

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Oral Minoxidil

According to the American College of Cardiology and the American Heart Association (AHA), resistant hypertension is characterized by elevated blood pressure levels exceeding the target range, despite the simultaneous utilization of 3 different classes of antihypertensive medications. These classes typically include a combination of a calcium channel blocker, a renin-angiotensin-aldosterone system blocker (angiotensin-converting enzyme inhibitor or angiotensin receptor blocker), and a diuretic. These drugs are administered at the highest daily doses a patient can tolerate. The FDA approves minoxidil for maintaining blood pressure levels in patients with resistant hypertension.[5]

Many forms of alopecia are off-label indications for oral or sublingual minoxidil. Recently, multiple studies have explored using low-dose oral minoxidil (<5 mg daily) for treating many forms of alopecia, including male-patterned and female-patterned hair loss, to treat hair loss without adverse reactions.[6] The low adverse-effect profile of low-dose oral minoxidil aids in long-term adherence to treatment and positive clinical response.[7][8] More studies are needed to test the efficacy of oral and sublingual minoxidil when treating various alopecia to improve patient outcomes and provide an alternative for those with difficulty with topical formulations.[6]

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