Instruction for use: Minoxidil (Minoxidilum)

Pharmacological group

dermotropic means

Vasodilators

Nosological classification (ICD-10)

I10 Essential (primary) hypertension

Hypertension, Arterial hypertension, Arterial hypertension crisis course, Essential Hypertension, Primary hypertension, Arterial hypertension, complications of diabetes, hypertension, The sudden increase in blood pressure, Hypertensive disorders of blood circulation, hypertensive condition, hypertensive crises, hypertension, arterial Hypertension, malignant Hypertension, Hypertonic disease, Hypertensive crisis, Hypertension, accelerated hypertension, malignant hypertension, The aggravation of hypertensive disease, Transient hypertension, Isolated systolic hypertension

I15 Secondary hypertension

Arterial hypertension, complications of diabetes, hypertension, The sudden rise in blood pressure, Hypertensive disorders of blood circulation, hypertensive condition, hypertensive crises, hypertension, arterial hypertension, malignant hypertension, Hypertensive crisis, Hypertension, accelerated hypertension, malignant hypertension, hypertensive crisis, The aggravation of hypertensive disease, Transient hypertension, hypertension, Arterial hypertension, Arterial hypertension crisis course, renovascular hypertension, symptomatic hypertension, renal hypertension, Renovascular hypertension, Symptomatic hypertension

L64 Androgenic alopecia

Alopecia androgenic, Androgenetic alopecia, Androgenic alopecia of moderate severity, Severe Androgen-Dependent Alopecia, Male pattern hair loss

Code CAS 38304-91-5

Characteristics of Minoxidil

White or almost white crystalline powder odorless. Easily soluble in propylene glycol, methanol, ethanol, propanol, dimethylsulfoxide, soluble in water, practically insoluble in acetone, chloroform and ethyl acetate.

Pharmacology

Pharmacological action - hypotensive, vasodilating, stimulating hair growth.

Activates (opens) potassium channels in membranes of smooth muscle cells of the vascular wall. Has a peripheral vasodilating effect, expands resistive vessels (arterioles), lowers the SAD and DAD, reduces the load on the myocardium, causes reflex tachycardia and increases cardiac output. Increases the activity of renin plasma and promotes the retention of sodium and water.

Stimulates hair growth in androgen-dependent alopecia. The mechanism of hair growth enhancement is supposedly associated with vasodilation and improvement of microcirculation in the skin and trophic hair follicles, stimulation of the hair follicle transition from the resting phase (telogen phase) to the growth phase (anagen phase). Modulates the effect of androgens on hair follicles. Reduces the formation of 5-alpha-dehydrosterone (possibly indirectly), which plays a significant role in the formation of alopecia. The best effect is with a duration of the disease not exceeding 10 years, young patients, localization of the bald spot in the crown of the size of no more than 10 cm and the presence of more than 100 gun and terminal hair in the center of the bald head. Does not prevent hair loss caused by drugs, eating disorders (iron deficiency, vitamin A, etc.), tight hairstyles ("tail", "bun", etc.). A positive effect was noted in a significant proportion of patients with a disease duration of no more than 3-5 years.

Hair growth, as a rule, begins after 4 months of daily topical application of the solution. After the abolition of therapy, the growth of new hair stops and after 3-4 months, it is possible to restore the bald patches in the previous places.

In experimental tests, no mutagenic effect was detected. The presence of a carcinogenic effect in rats and rabbits is not established for topical application within 1 year. A dose-dependent decrease in the capacity for fertilization in females and male rats ingested in doses 1-5 times higher than MPDH was revealed. When administered orally to rats and rabbits, there was no teratogenic effect, but an increase in the probability of embryonic resorption in rabbits (but not in rats) was observed at doses 5 times that of MPD.

After oral intake of 90% of the dose taken. Cmax is achieved within 1 hour. Virtually does not bind to plasma proteins. Penetrates into breast milk. Undergoes biotransformation in the liver with the formation of low-activity metabolites. T1 / 2 from the plasma is 4.2 hours. It is excreted mainly by the kidneys (10% - unchanged).

When applied locally through intact skin, about 1.4% of the drug is absorbed. After discontinuation of topical application, 95% of the systemic absorption of minoxidil is excreted by the kidneys within 4 days.

Use of Minoxidil

Tablets: arterial hypertension (especially severe forms, resistant to combination therapy with other antihypertensive drugs).

Outside solution: male pattern baldness (androgenic alopecia) in men and women.

Contraindications

Hypersensitivity, pregnancy, breast-feeding; pheochromocytoma, mitral stenosis, secondary pulmonary hypertension (tablets); violation of the integrity of the skin, dermatosis of the scalp (external solution).

Restrictions for use

IHD, angina pectoris, heart failure, age under 12 years (experience of use is limited).

pregnancy and lactation

Contraindicated in pregnancy (adequate and strictly controlled studies in humans have not been performed). For the duration of treatment, breastfeeding should be discontinued.

Side effects of Minoxidil

From the nervous system and sensory organs: dizziness, headache, visual impairment (including reduced visual acuity).

From the cardiovascular system and blood (hematopoiesis, hemostasis): lowering blood pressure, tachycardia, arrhythmia, heart failure, inversion of the T wave on the ECG; in rare cases - hydrothorax, hydropericardium (in patients with heart failure), stenocardia (in patients with coronary insufficiency), exudative pericarditis, thrombopenia, and leukopenia.

From the skin: hypertrichosis, thinning and strengthening of pigmentation of hair on the body; with local application - dryness and flaking of the scalp, dermatitis (itching, rash), eczema, alopecia, burning sensation of the scalp, folliculitis (sensitivity or soreness in the hair roots), erythema

Allergic reactions: rash, face swelling, rhinitis, urticaria.

Other: delay of sodium and water in the body, swelling, shortness of breath, syncope, lowering of libido.

Interaction

Nitrates, diuretics, beta-adrenoblockers increase the hypotensive effect; estrogens, oral contraceptives, sympathomimetics, NSAIDs - weaken. Do not prescribe simultaneously with guanethidine (the risk of orthostatic hypotension).

Overdose

Symptoms: excessive vasodilation, pronounced hypotension, chest pain, tachycardia or arrhythmia, neuritis (immobility or trembling of hands, feet, head), sodium and water retention.

Treatment: symptomatic and maintenance therapy - the introduction of saline (IV), with hypotension - phenylephrine, angiotensin II, vasopressin, dopamine (should not use sympathomimetics, including norepinephrine and epinephrine).

Minoxidil and its metabolites are removed by hemodialysis.

Routes of administration

Inside, externally.

Precautions for Minoxidil

Avoid contact with the eyes.

The safety and effectiveness of the solution in patients under the age of 18 and after age 65 have not been determined.

special instructions

With arterial hypertension is usually prescribed in combination with beta-blockers and diuretics.

A comment

Currently in Russia minoxidil in the form of tablets does not have a valid registration.