Minoxidil
Pronunciation: (min-OX-i-dil)Class: Peripheral vasodilator, Dermatological agent
Trade Names:
Minoxidil
- Tablets 2.5 mg
- Tablets 10 mg
Trade Names:
Rogaine for Men
- Topical foam 5%
- Topical solution 2%
- Topical solution 5%
Trade Names:
Rogaine for Women
- Topical solution 2%
Pharmacology
Compare with other drugs. | ||||||
Directly dilates vascular smooth muscle by mechanism possibly related to blockade of calcium uptake or stimulation of catecholamine release; reduces elevated systolic and diastolic BP by decreasing peripheral arteriolar resistance; triggers sympathetic, vagal inhibitory, and renal homeostatic mechanisms, including increased renin release, which results in increased cardiac rate and output, and fluid retention; stimulates hair growth by unknown mechanism, but likely is related to its arterial vasodilating action.
Pharmacokinetics
Absorption
At least 90% is absorbed. T max is 1 h.
Distribution
0% is protein bound.
Metabolism
Approximately 90% is primarily metabolized by glucuronic acid conjugation.
Elimination
Primary route of excretion is urine. Mean t ½ is 4.2 h. Hemodialysis can remove minoxidil and its metabolites.
Onset
Onset is 30 min.
Peak
Time to peak is 2 to 3 h.
Duration
Duration is approximately 75 h.
Indications and Usage
OralManagement of severe hypertension associated with target organ damage in patients who have failed to respond to max doses of a diuretic plus 2 other antihypertensive drugs.
TopicalTreatment of androgenic alopecia.
Unlabeled Uses
Treatment of alopecia areata (topical).
Contraindications
Pheochromocytoma; standard considerations.
Dosage and Administration
Adults and Children older than 12 yr of agePO 5 mg/day initially. If necessary, can increase to 10, 20, and then 40 mg/day in single or divided doses (max, 100 mg/day).
Children younger than 12 yr of agePO 0.2 mg/kg/day as single dose initially. May increase in 50% to 100% increments until optimal BP control is achieved (usually 0.25 to 1 mg/kg/day; max, 50 mg/day).
AdultsTopical Foam (men only) Apply ½ capful 2 times/day to scalp in hair loss area. Solution (regular strength [2%] or extra strength [5%] for men) 1 mL 2 times/day directly onto scalp in area of hair thinning/loss. Solution (2% for women) 1 mL 2 times/day onto scalp in area of hair thinning/loss.
Storage/Stability
Store at room temperature (68° to 77°F) in tightly closed container.
Drug Interactions
GuanethidineMay result in profound orthostatic hypotensive effects; discontinue guanethidine before minoxidil therapy.
Petrolatum, retinoids , or topical corticosteroidsMay enhance cutaneous drug absorption of topically applied minoxidil.
Laboratory Test Interactions
None well documented.
Adverse Reactions
Cardiovascular
Changes in T-waves (60%); pericardial effusion leading to tamponade (3%); BP changes, chest pain, heart rate changes (topical).
CNS
Dizziness, faintness (topical).
Dermatologic
Hypertrichosis (80%); rashes, including bullous eruptions and Stevens-Johnson syndrome, scalp irritation or redness (topical).
GI
Nausea, vomiting.
Genitourinary
Breast tenderness (less than 1%).
Hematologic
Hct, Hgb, and RBC counts may fall but return to normal (7%, systemic); thrombocytopenia, leukopenia (rare).
Lab Tests
Increased BUN and serum creatinine (7%); increased alkaline phosphatase.
Metabolic-Nutritional
Sudden weight gain.
Miscellaneous
Temporary edema (7%); swelling of the hands or feet (topical).
Precautions
WarningsSerious adverse reactions may occur with minoxidil tablets, including pericardial effusion, occasionally progressing to tamponade, which can exacerbate angina pectoris. When first administering minoxidil tablets, hospitalize and monitor patients with malignant hypertension and those patients already receiving guanethidine to avoid too rapid or large orthostatic decreases in BP. |
MonitorBecause of possible salt and water retention, closely monitor body weight. Monitor fluid and electrolytes; observe patients for pericardial effusion. |
Pregnancy
Category C .
Lactation
Excreted in breast milk. In general, breast-feeding should not be undertaken.
Children
Limited data available.
Elderly
Use with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.
Hypersensitivity
Can occur and is manifested by rash, bullous eruptions, and Stevens-Johnson syndrome.
Renal failure or dialysis
Patients may require smaller doses and should have close medical supervision to prevent exacerbation of renal failure or precipitation of cardiac failure.
Abnormal scalp
Use of topical form of drug may result in increased absorption and systemic effects; avoid use on scalps with decreased integrity.
ECG changes
T-wave changes may occur; significance unknown.
Fluid/Electrolytes imbalance
Sodium and water retention occur, leading to edema and possible CHF.
Heart disease
Patients may be predisposed to CV adverse reactions.
Pericardial effusion
Has occurred rarely, sometimes with tamponade.
Severe hypertension
Too rapid BP correction can precipitate syncope, cerebrovascular accidents, MI, and ischemia of special sense organs with resulting loss of vision or hearing. Hospitalize patients to monitor carefully.
Tachycardia
Can be prevented by concomitant use of a beta-blocker or other sympathetic nervous system suppressant agents.
Overdosage
Symptoms
Exaggerated hypotension, fluid retention, tachycardia.
Patient Information
- Advise patient not to change dose without health care provider direction.
- Tell patient that a diuretic and a beta-blocker are necessary to enhance effectiveness and decrease adverse reactions of minoxidil.
- Instruct patient to notify health care provider of angina symptoms, breathing difficulty, dizziness, heart rate at least 20 beats/min over normal, light-headedness, rapid weight gain of more than 5 lb, or unusual swelling.
- Tell patient to report the following symptoms to health care provider: diarrhea, rash, skin irritation, vomiting, or other bothersome physical complaints.
- Warn patient taking oral form that enhanced growth and darkening of fine body hair may occur. It may take 1 to 6 mo to return to pretreatment appearance.
- Inform patient using topical form that 4 months of continuous use is required before hair growth is seen and that stopping treatment will lead to hair loss within a few months.
- Advise patient using topical form that more frequent applications or use of larger doses will not enhance hair growth and may lead to adverse reactions.
- Inform patient using topical form to expect initial hair growth to be soft, downy, colorless, and barely visible, and that after further treatment new hair should match other scalp hair.
- Tell patient using topical form not to use it in conjunction with other topical scalp medications, to apply drug only to healthy areas of scalp, not to use it if scalp becomes irritated or sunburned, and not to use it on other parts of body.
- For topical application, instruct patient to dry head and scalp before application and to wash hands after application.
- Explain that product contains significant amount of alcohol as base. Caution patient to avoid having topical form coming into contact with eyes, mucous membranes, or sensitive skin areas. If accidental contact occurs, instruct patient to rinse area with large amounts of cool tap water and to notify health care provider.
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minoxidil - Includes detailed dosage instructions.
